ABSTRACT

Many oral dosage forms, bulking agents and beverage products have unpleasant taste. The bitter taste is an undesirable trait of the product or formulations and can considerably affects its acceptability by consumer. So, they should be formulated in a palatable form. Bitter taste in such systems can be reduced or eliminated by various methods, but no universally applicable technologies are yet recognized. This article is about the discussion of recent approaches for minimizing the unpleasant taste for oral pharmaceuticals.

Key words: Taste masking, Eudragit.

ABSTRACT

SLN’s are colloidal carriers developed in the 1990s as an alternative system to the existing traditional carriers (emulsions, liposomes, and polymeric nanoparticles)¹. Nanoparticles made from solid lipids are attracting major attention as novel colloidal drug carrier for various applications as they have been proposed as an alternative particulate carrier system. The SLN_S are submicron colloidal carriers (50-1000 nm) which are composed of physiological lipid, dispersed in water or in an aqueous surfactant solution².SLNs are particles consisting of a matrix made from solid lipids. In aqueous dispersion they are stabilised by surfactants or polymers. They consist of a solid matrix protecting incorporated active substances against chemical degradation and providing high flexibility to modify release profiles. The SLN combine the advantages (e.g. physical stability, protection of incorporated labile drugs from degradation, controlled release, excellent tolerability, and scalability to large-scale preparations, excellent biocompatibility) of other traditional colloidal systems³.

Keywords: Solid lipid nanoparticles (SLNs), Stability, Administration routes, Controlled release, Colloidal drug carrier.

ABSTRACT

Conventional dosage forms like tablets and capsules are now a days facing the problems like dysphagia, resulting in the high incidence of non compliance and making the therapy ineffective. To obviate the problems associated with conventional dosage forms, mouth dissolving tablets have been developed having good hardness, dose uniformity, easy administration and serves as the first choice of dosage form for paediatrics, geriatrics and travelling patients. The MDTs were developed with an aim of having sufficient hardness, integrity and faster disintegration without water. Various approaches for the formulation of MDTs include Direct compression, Wet granulation, Freeze drying, Spray drying, Moulding, Cotton candy process and Sublimation. Novel technologies like Zydis Orasolv, Durasolv, Flash dose technology, Wowtab etc are available as patented technologies, most commonly used in preparation of MDTs. Drugs belonging to antibiotics, antiviral etc are now formulated as MDTs to minimize the draw backs of conventional dosage forms. Examples of Marketed MDTs are Cefadur DT, Zofran ODT, Acivir DT etc. Due to wide significance of MDT, this drug delivery system may lead to better patient compliance and ultimate clinical output.

Keywords: Mouth dissolving tablet, Disintegration, Patented technologies, Marketed MDTs

ABSTRACT

Traditionally, drugs are released in an immediate or extended fashion. A pulsatile drug release, where the drug is released rapidly after a well defined lag-time, could be advantageous for many drugs or therapies. Pulsatile release systems can be classified in multiple-pulse and single-pulse systems. A popular class of single-pulse systems is that of rupturable dosage forms. Other systems consist of a drug-containing core, covered by a swelling layer and an outer insoluble, but semi-permeable polymer coating or membrane. The lag time prior to the rupture is mainly controlled by: (i) the permeation and mechanical properties of the polymer coating and (ii) the swelling behavior of the swelling layer. As is frequently found in the living body, many vital functions are regulated by pulsed or transient release of bioactive substances at a specific site and time. Thus it is important to develop new drug delivery systems to achieve pulsed delivery of a certain amount of drugs in order to mimic the function of the living systems, while minimizing undesired side effects. These dosage forms offer many advantages, such as nearly constant drug level at the site of action, prevention of peak-valley fluctuations, reduction in dose of drug, reduced dosage frequency, avoidance of side effects, and improved patient compliance.

Key words: Lag time, pulsatile drug release, Rupturable coating

ABSTRACT

Oral drug delivery is the most widely used and acceptable drug delivery amongst the other delivery. The orally disintegrating tablets are available in the market providing one to two minute of disintegration time. Among fast dissolving drug delivery systems, oral strip (OST) drug delivery system is an alternative to tablets, capsules, and syrups for paediatric and geriatric patients who experience in difficulties of swallowing traditional oral solid dosage forms. This technology has been used for local action, rapid release of products and for direct systemic circulation in the oral cavity to release drug in rapid fashion. And also this delivery protect drug from first pass metabolism and improve the dissolution. The main attention towards OST review article is providing knowledge of materials used in OST, critical manufacturing aspects, applications, commercial technologies.

Keywords: Oral strip, Solvent casting, Semisolid casting, Disintegration time

ABSTRACT

With oral and parenteral drug delivery systems, poor patient compliance is a frequent problem in daily clinical practice. So, the transdermal route of drug delivery has gained great interest of pharmaceutical research. But the big hurdle in transdermal delivery of drug is the skin, the stratum corneum, & the outermost envelop of the skin. Recently, various strategies have been used to augment the transdermal delivery of bioactive. Mainly, they include iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, micro needles, and vesicular system (liposomes, niosomes, elastic liposomes such as ethosomes and transfersomes). Transfersomes possess an infrastructure consisting of hydrophobic and hydrophilic moieties together and as a result can accommodate drug molecules with wide range of solubility. The high and self-optimizing deformability of typical composite transfersomes membrane, which are adaptable to ambient tress allow the ultra deformable transfersomes to change its membrane composition locally and reversibly, when it is pressed against or attracted into narrow pore. Transfersomes can deform and pass through narrow constriction (from 5 to 10 times less than their own diameter) without measurable loss. This high deformability gives better penetration of intact vesicles. They can act as a carrier for low as well as high molecular weight drugs e.g. analgesic, anesthetic, corticosteroids, sex hormone, anticancer, insulin, gap junction protein, and albumin.

Keywords: Transfersomes, Ultra-Deformable vesicles, Transdermal, osmotic gradient

ABSTRACT

Pharmacoinformatics is new emerging information technologies like neuroinformatics, immunoinformatics, bioinformatics, Metabolomics, chemo-informatics, toxico-informatics, cancer informatics, genome informatics, proteome informatics, biomedical informatics are basic tools provided for the purpose of drug discovery. There is an increasing recognition that information technology can be effectively used for drug discovery. The work in pharmacoinformatics can be broadly divided into two categories - scientific aspects and service aspects. The scientific component deals with the drug discovery and development activities whereas the service oriented aspects are more patient centric. The compelling drivers for the pharmaceutical industry are minimizing the time between a drug’s discovery and its delivery to the marketplace and maintaining high productivity in the manufacturing processes. During a product’s lifecycle many complex decisions must be made to achieve these goals. To better support the development and manufacturing processes at each stage, we have proposed a new epitome to facilitate the management and transfer of data information and knowledge. In future these information technology efforts are expected to grow both in terms of their reliability and scope. Thus, this emerging technology (pharmacoinformatics) is becoming an essential component of pharmaceutical sciences.

Keywords: - Informatics, Pharmaceutical informatics, Drug development, Chemoinformatics, Bioinformatics.

ABSTRACT

The traditional formulations like solution, suspension or emulsion suffer from certain limitations like high dose and low bioavailability, first pass metabolism, intolerance, instability and also exhibit fluctuations in plasma drug levels and do not provide sustained effect, therefore, there is a need for some novel carriers which could attain ideal requirements of a drug delivery system. Nanoparticles delivery system has been proved nearly ideal one. Nanoparticles are, a type of colloidal drug carrier system comprising particles with diameter of nano-metric range. The rapid development of nanotechnology and nano-materials has led to a need for nanoparticle surface modification for a variety of applications. The surface can be tailored to specific physical, optical, electronic, chemical, and biomedical properties by coating a thin film of material on the surface of the nanoparticles. The coating or encapsulation of nanoparticles has been found to be of particular interest for the controlled release of drugs, genes and other bioactive agents. Controlled release systems provide the benefits of protection from rapid degradation, targeting delivery, control of the release rate and prolonged duration of bioactive agents. This article have a keen emphasize on the techniques used for the formulation of nanoparticles and their coating too along with associated cautions and significance related to special applications which reveals a better way to choose the suitable and efficacious technique to obtain a nano-sized formulation. It also reveals the need of regulatory framework for handling of nanoparticles.

Keywords: Nanoparticles, coated nanoparticles, coating techniques, targeted drug delivery.

ABSTRACT

Surrogacy is an arrangement in which a woman carries a pregnancy and gives birth to a baby for another woman. Surrogate motherhood is one of many currently available forms of Assisted Reproductive Technologies (ARTs) that have developed in response to the increasing number of individuals/couples who find themselves unable to conceive a child on their own. The main aim of this study is to give an overview of legal aspect of surrogate mother. Surrogacy is gaining popularity as this may be the only method for a couple to have their own child and also because adoption process may be long. India is leading in this business because of the easy availability of surrogates at comparatively less cost. Many agencies have come forward with the intention of outsourcing pregnancy to foreign countries. In India this process had been regulated by the law from 2002. Though the regulation have been initiated, they are not so stringent when compare to other countries hence many foreigners are coming to India for surrogate mother. It may be concluded that Assisted Reproductive Technology (ART) Bill 2010 has provided for single parenthood by allowing “unmarried couples” and “single persons” from India and abroad to have children using ART procedure and surrogate mothers in India.

Keywords: Surrogacy Agency, Assisted Reproductive Technology (ART), IVF (In-Vitro Fertilization), Egg Donation, Commercial surrogacy, Gestational surrogacy.

ABSTRACT

ODTS are solid unit dosage form which dissolve or disintegrate rapidly in mouth without water. So, acceptability of this dosage form mainly depends on its taste i.e. mouth feel. So it becomes necessary to develop such an ODT for that must be acceptable in taste to patient many techniques are available to mask the taste of drugs. These techniques not only serve as to mask the taste of drug but also to enhance the bioavailability of drug. Taste masking technology involves the development of a system that prevents the active substance interacting with the taste buds, thereby eliminating or reducing the bitter taste. This review describes the commonly used techniques that are adopted for masking the taste of bitter drugs and dosage form palatable. The common methods include addition of sweeteners, coating of drugs adjusting the pH values, granulation, freeze drying, forming complex with ion exchange resins etc.

Key words: orodispersible tablets (ODTs), taste masking.

ABSTRACT

An orphan drug is a pharmaceutical agent that is used to treat a rare medical condition (viz., Huntington’s disease, myoclonus disease, Tourette syndrome etc.). They receive little attention from pharmaceutical companies as the small patient population could not justify the huge investment required for drug development. In the last 20 years, orphan drug act has been adopted in several countries around the world (USA, Japan, Australia, and the EU) and has successfully promoted R&D investments to develop new pharmaceutical products for the treatment of rare diseases, but it faces future challenges like returns on the huge R & D costs, funding sources and initiatives for development of orphan drugs.

Keywords: Rare Diseases, Incentives, Marketing Exclusivity, Challenges.

ABSTRACT

Drug regulation is totality of all measures- Legal, administrative and technical- which the governments take to assure the quality, efficacy and safety of drugs. With reports of number of tragic adverse events caused by use of drugs, more stringent controls have been imposed upon the procedures for marketing authorization of drugs. The research and development, manufacture, import and export of pharmaceuticals is regulated by different regulatory bodies in different countries with varying levels of regulation stickiness. This review article provides useful information regarding the regulatory framework and Pharmaceutical key role players in many countries which are actively engaged in licensing and approval activities.

Key Words: Drug regulation, Drug registration, Drug Approval, EMEA, Pharmaceuticals, USFDA.

ABSTRACT

A new multi-layer tablet design has recently been proposed for constant drug release: It consists of a drug-free barrier layer on one or both bases of an active core (hydrophilic matrix). This partial coating modulates the core hydration process and reduces the surface area available for drug release. The consequence is an extended release that draws close to a linear release profile. These devices are primarily intended for soluble drugs, while an excessive reduction of the release rate may be obtained with drugs of low solubility. In these devices, time-dependent polymeric barrier is planned to control the release of soluble drugs. Oral Controlled release matrix tablets and layered matrix tablets can be formulated for highly water soluble drugs and sparingly soluble drugs by using polymers in the matrix core and as release retardant layers. This devices delivery the drugs to the colon. This review focuses on the application of the multilayered matrix tablets in the design of controlled released dosage forms employing various types of polymers and layered on the matrices core.

Key words: Matrix core, multilayered matrix tablets, zero order release, release retardant layers

ABSTRACT

Neural tube defects (NTDs) are one of the commonest birth defects. They form a spectrum of disease ranging from anencephaly to spina bifida occulta. Anencephaly is a cephalic disorder that occurs when the cephalic (head) end of the neural tube fails to close, resulting in the absence of a major portion of the brain, skull, and scalp. However few studies have systematically looked into the etiopathogenesis of anencephaly which mainly includes nutritional deficiencies and genetic predisposition. Efforts are a foot for universal food fortification with folic acid in the hope of preventing NTDs. So we hereby conclude that caution should be exercised before widespread of anencephaly or the NTDs.

Keywords: Neural tube defect, Anencephaly

ABSTRACT

A continued need to develop safe and effective analgesics and anti-inflammatory drugs fuels the ongoing investigations of cyclooxygenase (COX). Since the early 1990s, it has been appreciated that there are two cyclooxygenase enzymes, cyclooxygenase-1 and cyclooxygenase-2, responsible for the production of prostaglandin H2, the first step in prostanoid biosynthesis. Cyclooxygenase-1 was responsible for the physiological production of prostanoids and cyclooxygenase- 2 was responsible for the elevated production of prostanoids that occurred in sites of disease and inflammation COX-3 is an enzyme that is encoded by the PTGS1 (COX1) gene and is the third and most recently discovered cyclooxygenase (COX) isozyme. The COX-3 isozyme is encoded by the same gene as COX-1, with the difference that COX-3 retains an intron that is not retained in COX-1. In dogs the resulting protein resembles the other two COX enzymes, but in mice and humans it does not, owing to a frame-shift mechanism.

Key words: Cyclooxygenase, COX-3, Prostaglandins, Inflammation, NSAIDs

ABSTRACT

The mortality associated with scorpion sting rates from 3-22% worldwide. Out of 1500 scorpion species, 50 are dangerous to humans & can cause wide range of conditions including local as well as systemic symptoms. The plant and plant products have augmented human culture since time immemorial. The tribal peoples are custodian of unique traditional knowledge systems and their ambient flora and fauna. Traditional medicine practices and ethnobotanical information play an important role in the scientific research. 80% of world’s population depends on traditional Medicine and in India about 65% people from rural area uses Ayurveda and herbal medicines for the treatment various ailments including venomous bites. The present paper deals with the documentation & review of various ethnomedicinal plants used effectively by the tribal particularly for the management of Scorpion sting cases.

Keywords: Traditional medicine, Scorpion sting, Ethnomedicinal herbs

ABSTRACT

Transdermal drug delivery offers an attractive alternative to the conventional drug delivery methods of oral administration and injection. However, the stratum corneum acts as a barrier that limits the penetration of substances through the skin. Application of ultrasound to the skin increases its permeability (sonophoresis) and enables the delivery of various substances into and through the skin. Ultrasound has been used extensively for medical diagnostics and to a certain extent in medical therapy (physiotherapy, ultrasonic surgery, and hyperthermia). The generation of ultrasound and mechanism of sonophoresis with particular emphasis on the role of cavitation (both inside and outside the skin), thermal effects, convective transport, and mechanical effects also included. There are certain findings in the field of sonophoresis, namely transdermal drug delivery and transdermal monitoring. The article also encompasses a discussion on the variation of sonophoretic enhancement from drug to drug, possible applications of sonophoresis in near future, some commercially available sonophoretic systems and future trends. Particular attention is paid to proposed enhancement mechanisms and future trends in the field of cutaneous vaccination and gene delivery.

Key words: Ultrasound, Sonophoresis, Transdermal, Stratum corneum, cavitation, thermal effects, convective transport, and mechanical effects, Hyperthermia.

ABSTRACT

Gestational diabetes mellitus (GDM) is defined as glucose intolerance of various degrees that is first detected during pregnancy.  Insulin deficiency in turn leads to chronic hyperglycemia with disturbances of carbohydrate, fat and protein metabolism. As with diabetes mellitus in pregnancy in general, babies born to mothers with gestational diabetes are typically at increased risk of problems such as being large for gestational age (which may lead to delivery complications), low blood sugar, and jaundice. There are 2 subtypes of gestational diabetes. One is Type A1 gestational diabetes where abnormal oral glucose tolerance test (OGTT) but normal blood glucose levels during fasting and 2 hours after meals; diet modification is sufficient to control glucose levels) and other is Type A2 gestational diabetes where abnormal OGTT compounded by abnormal glucose levels during fasting and/or after meals; additional therapy with insulin or other medications is required. The goal of treatment is to reduce the risks of GDM for mother and child. A repeat OGTT should be carried out 2–4 months after delivery, to confirm the diabetes has disappeared. Afterwards, regular screening for type 2 diabetes is advised. If a diabetic diet or G.I. Diet, exercise, and oral medication are inadequate to control glucose levels, insulin therapy may become necessary. Glyburide and Metformin, a second generation sulfonylurea, has been shown to be an effective alternative to insulin therapy. In one study, 4% of women needed supplemental insulin to reach blood sugar targets.

Key words: Gestational diabetes mellitus, etiology, Management, oral hypoglycemic agents.

ABSTRACT

Inappropriate use of drugs for self-medication leads to emergence of drug resistant pathogens and poses serious health hazards. To assess the pattern of self-medication among residents of Hyderabad city. The study was conducted in December 2011. It was a community based cross-sectional survey on a sample of 238 households, which were selected randomly.  Data was collected by pre-designed questionnaire. The most common system involved was the respiratory system (21.34 %). Analgesics were most commonly used drugs for self medication (18.48%) followed by usage of antibiotics (16.80%). Most of the drugs for self-medication were obtained from drug retail outlets (35.71%) followed by friends/ neighbors’/ family practice (34.45%). The major reason for using self-medication was attitude of not to waste money on doctors’ fees (37.81%) followed by inability to afford doctors’ fees (25.63%).From the study it was concluded that majority of the persons go for self medication without proper knowledge of dose, adverse drug reactions, drug interactions. Hence, the issue needs to be addressed by the responsible authorities of State Pharmacy Council/Ministry of Health. The availability of drugs in informal sectors contributed to the increase in self-medication. Though self-medication is hard to eliminate, drug law enforcement and educating the public at large is vital.

Keywords: Self medication, Hyderabad.

ABSTRACT

The present study deals with the elaborated overview of comparative study of in-process and finished product quality control tests for parenteral products taking compendia specifications of Indian Pharmacopoeia (IP), British Pharmacopoeia (BP), United States Pharmacopoeia (USP), European Pharmacopoeia (EP) and Japanese Pharmacopoeia (JP) into consideration. When it comes to most sensitive parts of body i.e.; veins, a high degree of precautions should be taken during and after production of product for it to avoid any hitches. The sterility of these parenteral products, as well as accuracy in the calculation and preparation of doses is of great importance and a must in terms of compliance. The high graded quality product always refers to a product which is within the compendia limits. This article focuses on the comparison of Pharmacopoeial specifications of parenteral preparations, the procedures that are employed to maintain the quality and sterility of these ophthalmic products. This covers specifications and limits of different dosage forms according to different Pharmacopeia (like IP, BP, USP, JP etc.) which helps in comparative study of specifications provided in different Pharmacopeia as well as highlighting the differences in standards and also focussing on the specifications of different nations. Different regulatory requirements of the respective countries demand products with different specific limits so this comparative study will help in meeting all the requirements of all the pharmacopoeias and later the regulatory requirements of that particular country.

Keywords: Indian Pharmacopoeia (I.P), British Pharmacopoeia (B.P), United States Pharmacopoeia (USP), European Pharmacopoeia (EP), Japanese Pharmacopoeia (JP) and parenteral.

ABSTRACT

Ultra performance liquid chromatography (UPLC) system involves significant technological advances in particle size performance, system optimization, data processing, detector design and control. When all brought together, the specific achievements in each area have created a step-function progress in chromatographic performance. This new technique of analytical separation science uses the principles and practicality of HPLC with increasing the attributes of speed, sensitivity and resolution. Now a day’s pharmaceutical industries are in search of new ways to reduce cost and time for analysis of drugs. Analytical laboratories are not exception in this trend. Ultra high performance liquid chromatography (UPLC) with better resolution, assay sensitivity and high sample throughput allows a greater number of analysis to be performed in a shorter period of time and it also impart cost effective advantage over HPLC analysis. So that conventional assay was transferred and optimized for UPLC system. This review introduces the theory of UPLC, and involves some of the most advanced work in the field.

Keywords: Ultra performance liquid Chromatography, High performance liquid chromatography, High pressure liquid chromatography, Liquid chromatography.

ABSTRACT

RNA interference (RNAi) is a post-transcriptional mechanism of gene silencing that involves the generation of small interfering RNA (siRNA), micro RNA (miRNA), short hairpin RNA (shRNA) molecules from double stranded RNA (dsRNA) that are capable of binding to host mRNA molecules and inhibiting their translation and enhancing the degradation of the mRNA, so that leads to inhibition of gene expression of defective gene by suppression of the protein synthesis. This robust silencing effect of RNAi makes it a valuable research tool both in cell culture and in living organisms, in various diseases like cancer, metabolic syndrome, viral disease (HIV-1, Hepatitis B), neural and neuromuscular diseases (Muscular dystrophy, Spinal muscular atrophy, Alzheimer disease), Poly(Q), Parkinson, Asthma and Diabetes. Although introducing siRNA into cells in vivo remains a significant obstacle, as it is imperative for siRNA to reach the cytoplasm of the targeted cells because naked RNAs cannot penetrate cellular lipid membranes by themselves to become effective and induce silencing. So to overcome this challenges of delivery viral vectors like adenovirus and lentivirus and nonviral vectors like naked RNA, lipid based delivery vectors, cell penetrating peptides, polymer, inorganic molecules, chemical conjugates.

Key words: dsRNA, siRNA, miRNA, shRNA

ABSTRACT

Development of fancy oral drug delivery systems has always attracted scientists because of improved patient compliance. Among them, mouth dissolving drug delivery systems (MDDDS) have acquired an important position in the market by overcoming previously encountered administration problems. A fast-dissolving drug delivery system, in most cases, is a tablet which is designed to allow administration in the mouth in the absence of water and readily dissolves or disintegrates in the saliva generally within <60 seconds with rapid dissolution of drug and absorption of which may produce rapid onset of action and ease of administration to patients who refuse to swallow a tablet, such as pediatric and geriatric patients and psychiatric patients. In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. The risk of chocking or suffocation during oral administration is avoided, thus providing improved safety. Several techniques have been developed in the recent past, to improve the disintegration quality of these delicate dosage forms without affecting their integrity. This article focuses on the technologies available and the advances made so far in the field of fabrication of mouth dissolving tablets. Apart from the conventional methods of fabrication, this review also provides the detailed concept of some unique patented technologies like Zydis, Lyoc, Quicksolv, Orasolv, Durasolv, Flashtab, Oraquick, Wowtab and Ziplet along with their advantages and limitations.

Key words: Rapidly Disintegrating Tablet, Mouth Dissolving Tablet, Fast Disintegrating Tablet, Fast Dissolving Tablet, Orally Disintegrating Tablet, Orodispersible Tablet.

ABSTRACT

The medicinal plants are widely used by the traditional medical practitioners for curing various diseases in their day to day practice. In traditional systems of medicine, different parts (leaves, stem, root, fruit, seeds, latex and even whole plant) of Ficus Racemosa Linn (commonly known in all over India as udumbara, gular fig.) have been recommended for the treatment of diarrhea, diabetes, hypertension, gastric ulcer, wound healing etc. Ficus Racemosa Linn. Showed a wide range of pharmacological actions like hypoglycemic, hypolipidemic, renal anti-carcinogenic, anti-diuretic, anti-tussive, hepatoprotective, radioprotective, anti-ulcer, anti-inflammatory, anti-diarrhoel and anti-fungal. β-sitosterol, glauanol acetate, the active constituent present in Ficus Racemosa L., has been found to be largely responsible for the therapeutic potentials of gular. Although because of its great therapeutic potentials and wide occurrence in India the practitioners of traditional systems of medicine have been using Ficus Racemosa L. for curing various ailments, a rational approach to this traditional medical practice with modern system of medicine is, however, not much available. In order to establish the therapeutic uses of Ficus Racemosa L. in modern medicine, in last few decades several Indian scientists and researchers have studied the pharmacological effects of ethanolic, methanolic & aqueous extracts of various parts of gular plant. These pharmacological studies have established a scientific basis for therapeutic uses of this plant. Thereby, the objective of this review is an attempt to provide a detailed survey of literature on traditional uses and pharmacological properties of the plant as a boon for ailments of human kind.

Keywords: Ficus Racemosa Linn, anti-convulsant, radio protective/anti-oxidant, anti-diarrhoeal.

ABSTRACT

Most leading causes of death, disease and disability in developing countries can be prevented, treated, or at least alleviated with cost effective essential medicines. Despite this fact, millions of people are deprived of access to essential medicines. Many of those who do have access, are given the wrong treatment, receive too little or too much medicine for their illness, or do not use the medicine correctly, adding to the problem of irrational use of medicines. Rational use of medicines is essential in today's situation, especially in a country like India, where there is a wide disparity in the availability of medicines amongst cities and villages. The concept of the rational use of medicines has not yet penetrated the minds of health care providers and the public, and as a result there is rampant irrationality in both the medicines available, as well as the medicines prescribed. This article, attempts to explain to all, the various aspects related to essential medicines, their rational use, their irrational use, the concept of Fixed Dose Combinations (FDCs), and the role of Education in the Rational Use of Medicines.

Keywords: RUM, Essential Medicine, Nonessential Medicine, FDC.

ABSTRACT

In spite of wide spread biological uses of Psidium guajava, there is a dearth of information on its hepatoprotective activity especially during inflammation. This work was therefore conducted to evaluate the effects of methanolic stem bark and leave extracts of the plant on acute-phase proteins during acute-phase response in rats. Forty albino Wistar rats (twenty in each group) were divided into two groups (stem bark and leave extracts). Inflammation was induced using egg albumin while treatment with the extracts commenced as soon as the inflammation was established and this lasted for 90 minutes. Initial, inflammation and recovery phase blood samples were obtained for analysis of acute-phase proteins (Albumin & C-reactive protein) using standard methods. Even though the stem bark extract showed more potent effects on both parameters in either dose-dependent and time-dependent fashions, both were perpetuating their anti-inflammatory potency through significant reduction on C-RP and increment on Albumin levels purporting a possible mechanism of action for anti-inflammatory activity of Psidium guajava. Results were considered significant at P≤0.05.

Keyword: Psidium guajava, C-reactive protein, Albumin, acute-phase response, anti-inflammatory, egg albumin, albino Wistar rats.

ABSTRACT

The glidant and binding properties of starches extracted from three local potato tubers have been evaluated and compared with corn starch BP. The glidant properties studied include angle of repose, flow rate and flow factor while the binding properties were assessed by crushing strength and friability. The result indicated that potato starches employed as glidant were not as efficient as talc or corn starch but produced tablets with higher crushing strength and lower friability values. The results indicate that potato starches can be employed as an alternative binder to corn starch BP in the formulation of paracetamol tablets.

Keywords: comparative, glidant, binder, potato starches,

ABSTRACT

In an effort to scientifically appraise the mechanism of action of Psdium guajava stem bark and leaves, the present study was carried out to investigate the cell membrane stabilizing anti-inflammatory activities of methanol extracts of psidum guajava on experimental animal model at three different dose levels – 5mg/kg, 10mg/kg and 15mg/kg. Aspirin (10mg/kg) was used as standard reference cell membrane stabilizing agent for comparison. This research work was carried out using Wistar strain albino rats weighing 150g-175g. The extractive inhibited heat- induced haemolysis of erythrocytes in vitro. The methanol extract of Psidum guajava stem- bark demonstrated 89.23%, 93.94% and 103.66% inhibition while the leave extract demonstrated 51.40%, 51.43%, 61.40% and 44.29% of hemolysis of RBC caused by heat, in a dose- dependent manner – 5mg/kg, 10mg/kg and 15mg/kg respectively. Results were considered significant at p ≤0.05.

Keyword: Psidium guajava, membrane stability, albino Wistar rats, hemolysis, erythrocytes.

ABSTRACT

The study was aimed at comparing the mechanical strength and lamination tendencies of three local potato (Sweet, Kaffir and Irish) starches. The compressional properties of the formulation were analysed using density measurement and assessed by Heckel and Kawakita equations while the lamination tendencies were assessed by the brittle fracture index (BFI).Tablets produced with potato starches have higher mechanical strength as seen in their tensile strengths. Sweet potato starch showed superiority over other potato starches in that respect. The lamination tendency was lower with corn starch BP than the potato starches.Starches obtained locally from potato tubers produced stronger tablets and hence can be used in formulation of tablets.

Key words: potato starches, lamination tendency, tensile strength, Heckel equation

ABSTRACT

Eye infections caused by pathogenic bacterial agents have an interesting social history, often with somewhat unsavoury associations. Corneal scrapings were obtained from 100 hospitalised patients from eye hospitals of Baghdad city, Iraq and inoculated directly onto enriched and differential culture media. Subcultures were performed on selective media. The necessary biochemical tests were conducted and the organisms identified using standard procedures. Susceptibility of isolated pathogens to commonly-used ocular antibacterial was examined using Kirby-Bauer’s standard disc diffusion technique. The results were showed that 38 different organisms from total 100 corneal scraping samples of suppurative keratitis were isolated. Gram-positive bacteria accounted for 23(60.5%) and gram-negative bacteria for 15(39.4%). Staphylococcus aureus 11(28.9%), Strep. Pneumoniae 8(20.05%), Pseudomonas aeruginosa 6(15.7%), Staph. epidermidis 4(10.5%), Klebsiella pneumoniae 4(10.5%), E. coli 3(7.8%) and Moraxella catarrhalis 2(5.2%) were the most commonly-isolated organisms. In susceptibility testing, Gentamycin had significant effects against Gram positive bacteria which constituted the majority (82.5%) of isolates. Besides the coverage of this agent against Gram positive and negative organisms was also significant antibacterial activity that ranged from 50-100% sensitivity. Ofloxacin showed highly inhibition rate (75-100%) against all isolated pathogens except Moraxella catarrhalis (100%) resistance. Ampicillin coverage of against Moraxella catarrhalis 2(100%) and E. coli 2(66.6%). All the tested gram-positive cocci Staph. Species showed highly resistance to Chloramphenicol range from 90.9-100%. The coverage of Vancomycin against Staphy. aureus was 7(63.6%), Moraxella catarrhalis 2(100%), but all the isolates of E. coli  were resistant to Vancomycin. Susceptibility analysis revealed that antibiotic with the greatest coverage was Gentamycin (82.5 % of 38 isolates). Gentamycin also had good coverage against Gram-positive cocci, which constituted the majority (100 %) of suppurative keratitis isolates.

Keywords: antibiotic susceptibility, bacteria, ocular infection, susceptibility patterns.

ABSTRACT

Thyroid surgery commonly associated with perioperatively and postoperative bleeding and some initial pain on swallowing after surgery, and these are a common problems encountered till now. The use of certain medications might help to minimize blood loss during and after surgery with reduction of pain and operative time. The aim is to have a better surgical field with a good analgesia.A randomized study in Al Karkh hospital was performed including 22 cases submitted to bilateral subtotal thyroidectomy surgery divided into 2 groups; group A; 10 patients had the usual type of surgery with using the combination of bupivacaine 0.25% and adrenaline 1:200000 after induction of anesthesia to be injected in the operative site. The second group B involves the other 12 patients who were operated on without local infiltration. This study was designed to compare differences in both groups regarding to total blood loss, analgesic effect and duration of surgery Our study included 20 females and 2 male with enlarging goiter involving both lobes, with less blood loss in suction apparatus and drains as well as there was a less scores regarding pain relief during and after surgery in group A than group B. No significant statistical differences in term of morbidity and mortality for both groups regarding the local bleeding control during thyroid, peri-incisional infiltration provided better pain relief in early postoperative period.

Key words: Thyroid surgery, Bupivacaine, Adrenaline, Pain scores, Bleeding and Suction drains, suction apparatus

ABSTRACT

This study aimed at comparing the disintegrant properties of three potato starches with Maize starch BP as well as effect of method of incorporation of disintegrant on release of paracetamol tablet formulation. The disintegrant property was assessed by both disintegration and dissolution times of the formulation. The results showed that tablets produced with potato starch were similar in disintegration and dissolution times with those formulated with Maize starch BP. Disintegrants employed extra-granularly showed better disintegration than intra-granular or intra-extra-granular. Therefore the potato starches can be used as a disintegrant in paracetamol tablets formulation

Keywords: disintegrants, potato starch, formulation, dissolution time, incorporation

ABSTRACT

This research work evaluated the effects of Psidium guajava leaf extract on differential white blood cell count, % Packed Cell Volume(PCV) and Hemoglobin (Hb) concentration in acute -induced inflamed wistar rats. The study involved the use of forty five rats (in two groups) and were each divided into various subgroups (5mg/kg, 10mg/kg, 15mg/kg of extract and aspirin and control groups), with average weight of 150-270g. The initial, inflamed, and treated values of rats paw volumes were taken and after inducing inflammation with egg albumin and after a period of administration of the extract and aspirin, the rats were sacrificed and blood samples were collected. The results obtained at the end of the experiment showed that there were differences in values (i.e. initial, inflamed and treated). There was an increase in %PCV, WBC, Hb concentration after administration of extract and aspirin which led to a decrease in inflammatory effect. The effect may be due to the anti-inflammatory components present in P. guajava leaf and stem bark extracts which not only inhibit the production of inflammatory mediators but equally have multiplier effects on acutely low hematologic parameters. Based on these results, it is clear that P. guajava extracts possess components that sustain prompt recovery of these hematologic parameters during inflammation, a possible mechanism of action of its anti-inflammatory effect on animals.

Keywords: Psidium guajava, anti-inflammatory, %PCV, WBC, Hb concentration, egg albumin.

ABSTRACT

The aim of the study is to assess the usage of alteplase in stroke patients which is second leading cause in worldwide. Its beneficial effect in stroke patients is to disperse the thrombus within an occluded cerebral vessel and to limit ischemic damage within surrounding tissue (ischemic penumbra) and is safety and efficacy towards the stroke patient. This is prospective observational study, which assed the current usage of tissue Plasminogen activator (tPA) alteplase in stroke patients. This study was conducted in Stroke patients in Adichunchanagiri Hospital and Research Center. Duration of our study is sixteen months. A total of 140 stroke patients were assigned to receive alteplase. In which 102 (72.85%) Patients were treated before 3 hours (Window period) the study population were elderly with the age between 53-57 were 40.70% (n=48), and followed by 63-67 were 22.03 % (n=26), where as in female elderly patients the age group between 48-52 were 59.10% (n=13) and followed by 53-57 were 18.18 (n=4), elderly patients are more prone to have stroke. Therefore 54.23% (n=64) were recoverd in the post intervention benefit of alteplase in stroke patients,as in female patients were 68.18% (n=15) and age between 78-82 years only one patient died during the treatment. This study shows that efficacy and safety of thrombolytic in stroke patients within 3 hours and recover of the patients from the stroke is high rate. The findings encourages wider use of thrombolytic therapy for suitable patients treated in stroke centres can be a beneficial in future endeavours.

Keywords: Alteplase, Stroke Patients and Thromobolytic.

ABSTRACT

A simple, rapid and specific RP-HPLC method has been developed and validated for determination of Carvedilol in bulk and tablet formulations. Chromatographic separation was performed by Phenomenex Luna C-18 (250 x 4.6mm, 5μm particle size) column with a mobile phase consisting of a mixture of phosphate buffer, acetonitrile and methanol in the ratio (30:45:25 v/v/v), pH adjusted to 4.8 with ortophosphoric acid. The mobile phase was was filtered through a 0.45μ cellulose nitrate filter, sonicated for 15 min and delivered at a flow rate of 1ml/min. Detection was performed at a wave length of 241 nm at ambient temperature. Linearity was obtained in a concentration range of 30 to130 µg/ml with a correlation coefficient (r²) of 0.999. The limit of detection and limit of quantification were 1.08 and 3.24 μg/ml, respectively. No interference of excipients in determining tablet formulation; identical results were obtained like that of the standard sample.  The proposed RP-HPLC method is simple, accurate, precise, rapid and economical to be employed for routine analysis of carvedilol in pharmaceutical dosage forms. 

Keywords: Carvedilol, RP-HPLC, Validation, Tablet formulation

ABSTRACT

Hypoglycemic and hypolipidemic effects of Lepidium sativum (Garden cress) seed powder (3.0g/kg) was evaluated on diabetes and oxidative stress built up in alloxan induced diabetic male Wistar rats. Experimental animals were divided into six groups comprising of six animals each. Animals were supplemented with isoenergic diets (~3600) for a period of 45 days. Hyperlipidemia was induced by feeding high fat high cholesterol diet and diabetes was induced by single injection of alloxan (150mg/kg body weight) intraperitoneally. High fat feeding and alloxan induced diabetes resulted in marked alterations in blood glucose, lipid profile and antioxidant status in blood serum and hepatic tissue of albino rats. Garden cress treated rats showed a significant decrease (p≤ 0.05) in fasting blood glucose levels (FBG); glycosylated haemoglobin (Hb A_1C %); lipid profile (total cholesterol (TC), triglycerides (TG) and lipoprotein fractions (Low density lipoprotein cholesterol (LDL-C) and very low density lipoprotein cholesterol (VLDL-C)) with a significant increase in high density lipoprotein cholesterol levels (HDL-C). A significant increase (p≤0.05) in thiobarbituric acid reactive substances (TBARS) levels with concomitant decrease in reduced glutathione (GSH) and antioxidant enzyme activity was also observed in diabetic control and HFHC diet fed experimental rats. Lepidium sativum neutralized the effect and restored the levels. Lepidium sativum seed powder thus lends credence for the prevention and management of diabetes mellitus and related complications.

Key words: Lepidium Sativum, Garden Cress, Alloxan, Antihyperglycaemic, Antihyperlipidemic, Oxidative stress, Blood glucose, Lipid peroxidation 

ABSTRACT

The purpose of this research was to develop a desired topical formulation containing clotrimazole for treatment of fungal infections like eczema, itching, pruritis etc. Topical formulation enriched with SLN of clotrimazole were prepared. The solid lipid nanoparticulate dispersion of clotrimazole was prepared by hot homogenization technique using polymers like Carbopol 934, mannitol and PEG 6000. The nanoparticulate dispersion was evaluated for various parameters such as physical evaluations, particle size, diffusion studies, DSC, SEM, stability studies. The solid lipid nanoparticulate dispersion showed mean particle size less than 1000 nm. Differential scanning Calorimetry studies revealed no drug excipient incompatibility. Diffusion studies release profile of clotrimazole from nanoparticulate dispersion showed prolonged drug release. And all other evaluations were found to be complied the limits. Thus it can be concluded that formulation of SLN containing clotrimazole can be successfully formulated to localize the drug in the skin for to treat topical fungal infections.

KEYWORDS: Solid lipid nanoparticles (SLN), Clotrimazole, Hot homogenization, fungal infections.

ABSTRACT

Dental caries is the major public health problem that disturbs all countries in the world. Streptococcus mutans is considered as a chief culprit of this infectious disease and biofilm formation potential is the major virulence trait of this pathogen. In the era of antimicrobial resistance it is important to understand the virulence mechanism and antimicrobial sensitivity of S. mutans globally. The objective of the study was to investigate the biofilm formation potential and antimicrobial sensitivity of clinical isolates of S. mutans. Biofilm formation potential of 100 clinical isolates was studied by microtiter plate assay and coverslip assay and antimicrobial sensitivity was assessed by disc diffusion method. Our results showed that out of 100 clinical isolates 92 (92%) showed strong biofilm forming capability and 8 (8%) clinical isolates showed moderate biofilm formation potential. Antimicrobial sensitivity results showed that 72 (72%) isolates were resistant to amoxicillin, 65 (65%) isolates were resistant to chloramphenicol, 40 (40%) isolates were resistant to doxicycline, 46 (46%) isolates were resistant to erythromycin, 32 (32%) isolates were resistant to ofloxacin, 61 (61%) isolates were  resistant to tetracycline and only 17 (17%) isolates of S. mutans were resistant to amoxicillin/clavulanate. Our results suggest that combination therapy is more effective against cariogenic S. mutans and biofilm formation potential of this organism indicates the powerful contribution in pathogenesis. Ultimately, new combination therapies and inhibitors of biofilm formation are urgently needed.

Key words: antimicrobial, biofilm, dental caries, S. mutans, therapy, virulence

ABSTRACT

Benzotriazole was condensed stoichiometrically with ethyl chloro acetate in presence of potassium carbonate. The resulting ethyl-1H-benzotriazole-1yl-acetate was reacted with hydrazine hydrate in ethanolic solution. The resulting 2-(1H-benzotriazole-1-yl) aceto hydrazide was characterized by physical data and spectral studies and further it was condensed with 1H-indole-2,3-dione derivatives to form 2-(1H-benzotriazole-1-yl)-N'-[(3Z)-2-oxo-1,2-dihydro-3H-indol-3-ylidene] aceto hydrazide derivatives. These derivatives were characterized by melting point, TLC, IR, ¹H-NMR and Mass spectrum. From the biological activity profile it was revealed that they have considerable anti-inflammatory activity & antimicrobial activity against S. aureus, B. subtilis, Klebsiella and E. Coli.

Keywords: Indole-2, 3-diones, Benzotriazole, Antimicrobial and invitro anti-inflammatory activities;

ABSTRACT

In the present investigations, methanolic extracts of four marketed Aegle marmelos formulations (F₁, F₂, F₃, and F₄) were prepared and subjected to simultaneous quantitative determination of two biologically active compounds; umbelliferone and quercetin. Analysis of umbelliferone and quercetin was performed on TLC aluminum plates pre-coated with silica gel 60F-254 as stationary phase. Linear ascending development was carried out in twin trough glass chamber saturated with mobile phase consisting of toluene: ethyl acetate: formic acid (6:4:1, v/v/v), and densitometric determination of these compounds was carried out at 300nm in reflectance/absorbance mode. The system was found to give compact spots for umbelliferone and quercetin with Rf value of 0.66 and 0.68, respectively. The present method was validated for precision, recovery, repeatability, and accuracy in accordance with International Conference on Harmonisation (ICH Q2) guidelines. Statistical analysis of the data showed that the method is reproducible and selective for estimation of umbelliferone and quercetin. This method may be used for routine quality control and standardization of the herbal drugs and there formulations.

Key words: Aegle marmelos, Quercetin, Umbelliferone, HPTLC

ABSTRACT

An antimicrobial activity of Omphalotus olivascens wild mushroom was evaluated. The mycelia culture filtrate extracts showed varying degree of inhibition on the test organisms (Bacillus cereus, Escherichia coli, Salmonella paratyphi A, Klebsiella pnemoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Candida albicans).  The antimicrobial activity of mushroom sample varied according to the solvents. The ethyl acetate extract was the most active when compared with other extracts, to inhibit the growth of Acinetobacter baumannii (32mm), Klebsiella pnuemoniae (31mm), Bacillus cereus (31mm), and E.coli (28mm), Pseudomonas aeruginosa (28mm) Salmonella paratyphi A (27mm) and Canidida albicans (24mm). The bioactive contents of the mushroom are promising natural antimicrobial agents that can be harnessed as antimicrobial toxicants.

Keywords: antimicrobial, Omphalotus olivascens, culture filtrate

ABSTRACT

In the recent years, scientific and technological advancements have been made in the research and development of novel drug delivery systems by overcoming physiological troubles such as short gastric residence times and unpredictable gastric emptying times. Several approaches are currently utilized in the prolongation of the gastric residence times, including floating drug delivery systems, swelling and expanding systems, polymeric bioadhesive systems, modified-shape systems, high-density systems and other delayed gastric emptying devices. This review entitled the detailed scenario related to Bilayer floating drug delivery system with their advantages over the conventional drug delivery system and also limitation, which are helpful in development of dosages form. Various types of techniques employed for development of this dosages form. Review focused on formulation aspect of effervescent floating drug delivery system with their evaluation techniques. The purpose of this comprehensive review is to compile the work going on this delivery system. Which provide the valuable information related to formulation aspect to achieve gastric retention and discussed the various factors affect and to overcome it

Keywords: Gastric residence time, Floating drug delivery system, Effervescent, Non-effervescent.

ABSTRACT

One of the most feasible approaches for achieving a prolonged and predictable drug delivery profiles in the GIT is to control the gastric residence time (GRT) using gastroretentive dosage forms. The aim of the present study is to prepare the floating microspheres of ketoprofen to sustain the drug release for longer time to overcome the short half life of the drug. The microspheres were prepared by emulsification-solvent evaporation technique using ethyl cellulose and heat denaturation technique using egg albumin as a natural polymer. The optimization of microspheres was carried out based on pentagonal design using response surface methodology. The floating microspheres were evaluated for micromeritic properties, particle size, percentage yield, in-vitro buoyancy, entrapment efficiency, drug polymer compatibility, scanning electron microscopy and in-vitro drug release studies. The prepared microspheres exhibited prolonged drug release (> 9 h) and remained buoyant for > 24 h. The mean particle size increased and the drug release rate decreased at higher polymer concentration. The optimized formulation of ethyl cellulose microspheres (KEC-OP) exhibited prolonged drug release of 88.31 % up to 10 h demonstrating zero order kinetics and Case II transport release mechanism where as optimized formulation of egg albumin (KEA-OP) showed drug release of 96.78 % up to 9 h demonstrating peppas kinetics and Case II transport release mechanism.

Keywords: Ketoprofen, ethyl cellulose, egg albumin, floating microspheres, bioavailability, pentagonal design.

ABSTRACT

A novel, precise and selective high performance liquid chromatographic method was developed for the estimation of paliperidone using paracetamol as the internal standard. Separation was achieved on a LiChrospher® RP-18 HPLC column (5 μ particle size and 25 cm × 4.6 mm internal diameter) using 10 mM ammonium acetate: methanol in the ratio of 10:90 (v/v) as the mobile phase, at flow rate of 0.7 ml/min and the eluate was monitored at 277 nm. The method was validated in compliance with ICH guidelines. The correlation coefficient of the calibration graph was 0.99946±0.00037 over the concentration range 1 to 5 µg mL^-1. The limit of detection and limit of quantification were 0.569 µg mL^-1 and 1 µg mL^-1, respectively. Overall percentage recovery of paliperidone ranged between 98.92±0.595 to 100.30±0.693. Relative standard deviations for intra- and inter-day precision studies were <2%. The method was simple, rapid, economic and suitable for the regular quality control of paliperidone in tablet dosage forms.   

Keywords: Paliperidone, RP-HPLC, paracetamol, validation, ICH guidelines

ABSTRACT

The main objective of this study was to formulate and evaluate the fast dissolving tablets of Gliclazide with natural superdisintegrants. Various formulations were prepared by direct compression using different concentrations of natural superdisintegrant i.e. isolated mucilage of Plantago ovata, isolated mucilage of Aloe vera and extracted mucilage of Hibiscus rosasinesis. The initial compatibility studies between the drug and excipients were carried out using FTIR spectroscopy. The blend was evaluated for additive properties. The tablets were evaluated for physical parameters and in vitro drug release. The disintegration time and in vitro drug release of optimized formulation (P4) was found to be 2.41±0.05 secs. The optimized formulation was subjected to stability studies for three months. The formulation was found to be stable, with insignificant change in the hardness, disintegration time, drug content and in vitro drug release pattern.

Keywords: Fast dissolving tablet, isolated mucilage of Plantago ovata, isolated mucilage of Aloe vera and mucilage of Hibiscus rosasinesis

ABSTRACT

The present manuscript describe simple, sensitive, rapid, accurate, precise and economical Q-absorbance ratio method for the simultaneous determination of Cefpodoxime proxetil and ofloxacin in combined tablet dosage form. Absorbance ratio method uses the ratio of absorbances at two selected wavelengths, one which is an isoabsorptive point and other being the λ-max of one of the two components. Cefpodoxime proxetil and ofloxacin show an isoabsorptive point at 272 nm in methanol. The second wavelength used is 236 nm, which is the λ-max of Cefpodoxime proxetil in methanol. The linearity was obtained in the concentration range of 5-17 μg/ml for both Cefpodoxime proxetil and Ofloxacin. The concentrations of the drugs were determined by using ratio of absorbances at isoabsorptive point and at the λ-max of ofloxacin. The method was successfully applied to pharmaceutical dosage form because no interference from the tablet excipients was found. The results of analysis have been validated statistically and by recovery studies.

Key Words: Cefpodoxime proxetil, Ofloxacin, Absorption ratio method Tablets, Validation.

ABSTRACT

Isoxsuprine hydrochloride, a β₂ agonist used in peripheral vascular disease was formulated into sustain release matrix tablets, by wet granulation method using HPMC K15M as release retardant in different proportions and PVP K25 as a binder. The parameter optimized using 3² factorial designs. The tablets of all batches were evaluated for drug content, hardness, friability, weight variation and in vitro drug release profile. The dissolution profiles of formulated tablets were compared with a marketed product. The similarity factor (f₂) was calculated to check the similarity with marketed product. Different dissolution models were applied to drug release data in order to evaluate release mechanisms and kinetics. Mathematical treatment of the in vitro drug release data suggests that, the drug release of all the formulations exhibited nearly zero-order kinetics, the release exponent n ranged from 0.69 to 0.8 indicate that drug release from the all batches occurred by non-Fickian diffusion mechanism (anomalous transport), i.e. the release is ruled by both diffusion of the drug and dissolution of the polymer. According to SUPAC guidelines the formulation containing combination of 25% HPMC K15M and 10% PVP K25 is the most similar formulation to marketed product.

Keywords: Isoxsuprine HCl, factorial design, release kinetics, sustained release

ABSTRACT

The present manuscript describe simple, sensitive, rapid, accurate, precise and cost effective dual wavelength spectrophotometric method for the simultaneous determination of Rifampicin and Piperine in combined capsule dosage form. The utility of dual wavelength data processing program is its ability to calculate unknown concentration of components of interest in a mixture containing an interfering component. The principle for dual wavelength method is “the absorbance difference between two points on the mixture spectra is directly proportional to the concentration of the component of interest”. The method was based on determination of Rifampicin at the absorbance difference between 286 nm and 357 nm and Piperine at the absorbance difference between 356 nm and 479 nm. The linearity was obtained in the concentration range of 10-60 μg/ml for Rifampicin and 1-10 μg/ml for Piperine. The mean recovery was 98.40 ± 0.48 and 98.59 ± 0.46 for Rifampicin and Piperine, respectively. The method was successfully applied to pharmaceutical dosage form because no interference from the capsule excipients was found. The suitability of these methods for the quantitative determination of Rifampicin and Piperine was proved by validation. The proposed methods were found to be simple and sensitive for the routine quality control application of Rifampicin and Piperine in pharmaceutical capsule dosage form. The results of analysis have been validated statistically and by recovery studies.

Keywords: Rifampicin, Dual wavelength, Piperine, Validation, Recovery, Drug analysis.

ABSTRACT

We synthesized a new series of bis-amide and hydrazide-containing derivatives of malonic acid and hypophosphorousadducts of acid hydrazones by the reaction of 2-[N- (acetyl) 2, 5-dichloroanilido acetohydrazide with various Carbonyl Compounds in 31 to 64% yield.  Newly synthesized compounds have been tested for their anti-bacterial activity against gram positive bacteria S.albus, S.aureus and gram negative bacteria E.coli and Pseudomonas piosineus. The compound (1, 2, 3, 7, 10, 12, 15) shown significant activities and compound (4, 9, 13, 14, 17) have shown moderate activity. The same compounds were tested for their anti-fungal activity against Candida albicans, Aspergillus niger and Alternaria alternata at concentration of 30 mg/ml using Savored dextrose agar media. The compound (3, 5, 9, 11, 14) shown significant activities and compound (2, 4, 6, 13, 16) have shown moderate activity against Candida albicans and Aspergillus niger. All the other compounds did not show significant activity against the fungi at the concentration used.

Keywords: Malonic acid, bis-amides, acid hydrazides, hydrazones, hypo phosphorous adducts

ABSTRACT

Development and validation of an analytical UV derivatives spectrophotometric method to quantify carbimazole as a single active principle in pharmaceutical formulation were done. Based on the spectrophotometric characteristics of carbimazole, a signal of first (314 nm), second (300 nm), third (289 nm), fourth (320 nm) order derivative spectrum was found to be adequate for quantification. The method obeyed Beer's law in the concentration range of (2-18 µg/ml) with square correlation coefficient (r² = 0.999). The mean percentage recovery was found to be 99.56 ± 0.7179. As per ICH guidelines the results of the analysis were validated in terms of linearity, precision, accuracy, limit of detection and limit of quantification, and were found to be satisfactory.

Key Words: Carbimazole, Derivative spectrophotometry, ICH, Validation.

ABSTRACT

The present study was carried out to evaluate the antioxidant activities of methanolic extract of Passiflora nepalensis Smith. (Passifloraceae) ripe fruits in various systems. The free radical scavenging potential was studied by using different antioxidants models of screening using vitamin C (5mM) as standard. About 200, 400, 600 & 800 μg/ml methanolic extract inhibited the FeSO4 induced lipid peroxidation in a dose dependent manner and showed IC50 value 510 ± 2.59μg/ml. The methanolic fraction at 800 μg/ml exhibited significant antioxidant activity in ferrous sulphate induced lipid peroxidation and Superoxide scavenging models with simultaneous improvement in hepatic glutathione (10.22 ± 0.2333µg GSH/mg of wet tissue) and catalase levels (136.27 ± 0.4867µM of H₂O₂ consumed /min/mg tissue) compared to standard group. The results suggest that the methanolic extract of Passiflora nepalensis Smith. Fruits play an important role in the modulation of oxidative stress.

Key Words: Passiflora nepalensis Smith. Antioxidant activity, Lipid peroxidation, Ripe Fruit Extract.

ABSTRACT

In the present study, a series of S-[5-(phenylamino)-1,3,4-thiadiazole-2-yl] benzenecarbothioate and S-[5-(phenyl amino)- 1,3,4-thiadiazole-2-yl] ethanethioate were prepared by refluxing benzoyl chloride and acetyl chloride in presence of potassium carbonate with 5-(phenyl amino)-1,3,4-thiadiazole-2-thiol. 5-(Phenyl amino)-1, 3, 4-thiadiazole-2-thiol were prepared by cyclization of arylthiosemicarbazide with carbondisulphide. The structure of new compounds prepared during present investigation have been authentically established by their IR, ¹H NMR and Mass spectral studies. The antibacterial and antifungal activities of thiadiazole derivatives also reported. Some of these derivatives exhibit significant antimicrobial activity.

Key words: thiadiazole, thiosemicarbazide, antibacterial, antifungal.

ABSTRACT

The present investigation is focused on to study influence of excipients on physical characteristics of combination dry powder inhaler formulation and to compare it with traditional combination Dry Powder for Inhalation. Formulation contains salmeterol xinafoate (SX) and fluticasone propionate (FP).  The formulation was prepared by Spray drying of suspensions obtained by solvent displacement method. The excipients used were α-lactose monohydrate and Poloxamer 188. The powders generated were of a suitable size for inhalation with satisfactory yield. It was found that in optimum concentration with poloxamer 188; lactose gave increased spray drying thermal efficiency. FTIR study showed the close agreement among the spectra of all spray dried formulations and APIs. Effect of excipients was further investigated by different physical characters of spray-dried formulations. The formulation was evaluated for in vitro drug release and in vitro aerosolization study by the modified USP II dissolution apparatus and using an Andersen cascade impactor (ACI). Dissolution study gave immediate drug release profiles. In vitro aerosolisation showed better degree of FPF as compared to marketed formulation containing lactose. The stability study indicated that all the formulations were quite stable at accelerated storage conditions. The results obtained from all observations indicate that in presence of poloxamer.188; lactose was found to be superior over traditional combination dry powder inhaler formulation containing salmeterol xinafoate and fluticasone propionate.

Key Words: Dry Powder for Inhalation, Combination Inhalation Therapy, Long-acting β-2 agonist, Long acting corticosteroid, Pulmonary Drug Delivery.

ABSTRACT

Disadvantage in presently available synthetic drugs for inflammation is that they cause gastrointestinal irritation and reappearance of symptoms after discontinuation. Need for screening and development of novel, but better anti-inflammatory drugs and indigenous medicinal plants could be a logical source to find these. Herbal therapy is used to treat a large variety of ailment and symptoms, e.g., inflammation, fever and pain; however, there are no adequate experimental evidences about their effectiveness. The purpose of this investigation was study to the anti-inflammatory and anti-pyretic properties of stem bark extract of Haldinia cordifolia in rats. Haldinia cordifolia (rubiaceae) has been extensively used in folk medicine for the treatment of ulcers, burns, fevers, antiseptic, diarrhoea and dysentery. The ethanolic extract of dried stem bark of Haldinia cordifolia was investigated for anti-inflammatory (carragenan induced rat paw oedema) and anti-pyretic (brewer’s yeast induced pyrexia) activities. Pre treatment with the extract (200 - 400 mg/kg, p.o.) significantly prevented increase in volume of paw oedema in dose dependent manner. Its effects on antipyretic activity were also significant and reduce fever at higher doses. In conclusion, this study has established the anti-inflammatory activity and antipyretic activity of Haldinia cordifolia and thus justifies the ethnic uses of the plant.

Key words: Inflammation, Pyretic, Haldinia cordifolia, Ethanol, Carrageenan, Paw oedema.

ABSTRACT

Curcumin a hydrophobic poly-phenol is derived from turmeric, the rhizome of the herb Curcuma longa L. Curcumin has been shown to exert anti-depressant effects in rodent models. However, poor bioavailability of curcumin curbs its usage as a therapeutic agent. In view of the above curcumin loaded solid lipid nanoparticles (C-SLNs) were prepared and evaluated for the antidepressant effect of acute administration of C-SLNs (1, 2.5, 5 and 10 mg/kg, p.o.) in the forced swim model of depression in mice. C-SLNs exhibited 47.42%, 67.39%, 31.67% and 36.2% reduction in immobility time after administration of 1, 2.5, 5 or 10 mg/kg dose (p.o.) respectively. Free curcumin however did not result in a significant reduction, except at 2.5 mg/kg, which could produce a reduction of 21.7% but was still 2.83 times lower than the effect obtained with a similar dose of C-SLNs. The results obtained may be assigned to the therapeutic amounts of curcumin reaching the brain. Thus, C-SLNs with their improved bioavailability and permeability possess higher anti-depressant potential upon administration of a single and a much lower dose when compared to free curcumin.

Keywords: Curcumin, solid lipid nanoparticles, antidepressant, bioavailability, forced swim test

ABSTRACT

The Antioxidant potential of ethanol extract as well as petroleum ether, chloroform, ethyl acetate and aqueous soluble fractions of Tephrosia purpurea (Linn.) Pers., which is widely used in indigenous system of medicine for different purposes. The ethanol extract as well as petroleum ether, chloroform, ethyl acetate and aqueous soluble fraction were analysed for total phenolics content, total flavonoid content and free radical scavenging activity using DPPH (1,1- diphenyl- 2- picryl hydrazyl) radical. The ethanol extract was found more effective than four different fractions of ethanol extract of Tephrosia purpurea. Total phenolics content and total flavonoid content are found to be highest in ethyl acetate fraction and least in petroleum ether and more or less similar in aqueous and chloroform fractions. In general, the results indicate that the ethanol extract and ethyl acetate fraction are rich in phenolic content and flavonoid content with potent free radical scavenging activity implying their importance to human health.

Key Words: Antioxidant, Tephrosia purpurea, DPPH.

ABSTRACT

Nicotinic acid (NA) although known since decades, as an lipid lowering agent drug has not become a first-line treatment due to the strong side effect called flushing occurs when given in Immediate release (IR)dosage form. In the present research, an attempt has been made to formulate extended release matrix tablets of Nicotinic acid (NA). The tablets were prepared by wet granulation method and the prepared tablets of NA will remain intact up to 2 hrs even in pH 1.2 due to eudragit L 100-55 and its release is not only initiated but tact fully retarded up to 12 hrs and were found to be superior in physical properties, dissolution characteristics, and drug content uniformity. The in vitro NA release data justified the release mechanism to be Case-III and dissolution control release was found to be a mixed pattern of zero order and Korsmeyer-Peppas release models. Moreover, lactose shows moderately affected drug release due to channeling action and hence causing drug release at desired rate and amount. 

Keyword: Nicotinic acid (NA), Extended release (ER), HPMC K15M. Eudragit L 100-55, di calcium phosphate (DCP). 

ABSTRACT

Natural dyes are now-a-days very common for every cloth industry because the harmfulness of synthetic dyes on the skin of human beings. In cotton, silk and also in wool these colours are stable and very much eco-friendly to human skin. So now, several attempts are taken by the scientists through out the world to isolate natural dyes from different vegetables and flowers. Here in this study an attempt has been taken to isolate natural dyes from the flowers of Hibiscus rosa-sinensis. In the result, three different colours like blue, purple and green were prepared from the above said flowers and they are well stable on cotton cloths after washing by hot water and soap too. The intensity of the three colours are also high, they are bright and really eco-friendly to the human skin.

Keywords: Natural dyes, Hibiscus rosa-sinensis, mordant

ABSTRACT

Peucedanum grande has been found to be associated with the multiple therapeutic properties. In the present study, we have used P. grande as an ameliorating agent against nephrotoxic effects of Mercuric chloride (HgCl₂). The rats were given pretreatment of P. grande orally at a dose of 60 and 120 mg/kg body weight for five consecutive days. Mercury chloride 4 mg/kg body .wt was used as renal toxicant, and injected subcutaneously in the neck region in a volume of 1 ml/kg. The modulatory effects of P. grande on HgCl₂ induced nephrotoxicity was investigated by assaying oxidative stress biomarkers, lipid peroxidation, serum kidney toxicity markers and by histopathological examination of kidney. The HgCl₂ induced nephrotoxicity by depleting antioxidant levels, elevating the level of serum creatinine and BUN, as well as damaging the normal architecture of kidney. P. grande pretreatment prevented deteriorative effects induced by HgCl₂ through a protective mechanism that involved reduction of increased oxidative stress as well as by restoration of histopathological change against HgCl₂ administration.

Keywords: Peucedanum grande, Mercuric chloride, Kidney, histopathology, oxidative stress.

ABSTRACT

In the present investigation, pH-dependent and controlled drug release polymeric microspheres of Ornidazole were developed to deliver the active molecule to the colonic region. Microspheres were prepared by emulsion cross-linking method with some modifications, using different proportions of Ornidazole and Polymers (guar gum and gelatin). Gelatin microspheres were coated with Acrycoat L100 to achieve pH sensitive properties and specific biodegradability for colon targeted delivery of Ornidazole. Microspheres were evaluated for size, morphology, sphericity study, % yield, loose surface crystal study, drug content and entrapment efficiency. In vitro drug release study was conducted by buffer change method to mimic GIT environment using buffer solutions of varying pH. The investigations revealed that microspheres prepared with Ornidazole: guar gum ratio (1:2) shows only 10.003±0.885 % drug was released in first 5 hours and 38.849 ± 0.62 % in 12 hours, which proves the potentiality of guar gum for colonic delivery of drugs. While for microspheres prepared with Ornidazole: gelatin (1:2) and coated with Arycoat L100 shows 16.596 ± 3.18 % drug release in first 5 hours and 45.921 ± 3.07 % in 12 hours.

Key Words: colon specific drug delivery, biodegradable polymers, pH-dependent release, In vitro drug release

ABSTRACT

The present manuscript describe simple, sensitive, rapid, accurate, precise and economical first derivative spectrophotometric method for the simultaneous determination of nebivolol and hydrochlorothiazide in combined tablet dosage form. The derivative spectrophotometric method was based on the determination of both the drugs at their respective zero crossing point (ZCP). The first order derivative spectra were obtained in methanol and the determinations were made at 270.5 nm (ZCP of hydrochlorothiazide) for nebivolol and 282.5 nm (ZCP of nebivolol) for hydrochlorothiazide. The linearity was obtained in the concentration range of 5-100 μg/ml for nebivolol and 2-14 μg/ml for hydrochlorothiazide. The mean recovery was 100.04 + 0.93 and 99.87 + 1.16 for nebivolol and hydrochlorothiazide, respectively. The method was found to be simple, sensitive, accurate and precise and was applicable for the simultaneous determination of nebivolol and hydrochlorothiazide in pharmaceutical tablet dosage form. The results of analysis have been validated statistically and by recovery studies.

Key words: Nebivolol, hydrochlorothiazide, recovery, first order derivative spectrophotometric method, tablet, validation.

ABSTRACT

A simple, economic and precise RP-HPLC method has been developed and validated for simultaneous estimation of thiocolchicoside (THC) and diclofenac (DCF) both in bulk drug and in capsule formulation. Reversed-phase chromatography was performed on a C₁₈ Phenomenex-Gemini column with mobile phase acetonitrile: water (70:30 % v/v, adjusted at pH 3.0) at a flow rate of 1.0 ml/min. Detection was performed at 258 nm and sharp peaks were obtained for THC and DCF at a retention time of 1.537 min and 4.010 min respectively. The method was validated for accuracy, precision, detection and quantification limits, and system suitability in accordance with ICH guidelines. Linear regression analysis data for the calibration plot showed there was a linear relationship between response and concentration for THC in the range 4 - 24 μg/ml with the correlation coefficient 0.9998 and the linear regression equation y = 20.64x + 26.08. Linearity was observed in the range of 25 - 150 μg/ml with the correlation coefficient 0.9998 and the linear regression equation y = 11.13x + 65.27 for DCF. The detection (LOD) and quantification (LOQ) limits for THC were found to be 1.052 and 3.187 μg/ml and for DCF it was found to be 1.475 and 4.470 μg/ml. Statistical analysis proved that the method was precise, reproducible and accurate for simultaneous estimation of THC and DCF. The wide linearity range, sensitivity, accuracy, short retention time, and simple mobile phase imply that the method is suitable for routine quantification of THC and DCF with high precision and accuracy.

Keywords: Thiocolchicoside, Diclofenac, Simultaneous estimation, Reverse Phase-HPLC

ABSTRACT

The present research work discusses the two new, simple, accurate, precise and reproducible UV spectrophotometric methods have been developed and validated for the simultaneous determination of Prasugrel (PRASU) and Aspirin (ASP) in their combined dosage form.  Method- I is based on simultaneous equation method using two wavelengths, 254 nm (λmax of PRASU) and 276 nm (λmax of ASP). Method - II Q‐absorption ratio method using two wavelengths, 274.7 nm (Isoabsorptive point) and 254 nm (λmax of PRASU). Methanol was the solvent used in all methods. This method obeyed Beer’s law in the concentration range of 5-60 µg /ml for PRASU and 20-140 μg/ml ASP. All methods were validated statistically and recovery studies were carried out. Hence, the methods herein described can be successfully applied in quality control of combined pharmaceutical dosage form.

Keywords: Prasugrel, Aspirin, Simultaneous equation method, Q-absorbance ratio method, Validation

ABSTRACT

The aim of this study was to develop a new intra-gastric floating in situ gelling system for controlled delivery of levetiracetam for the treatment of partial onset seizures. High dose of levetiracetam (750 to 1000 mg) is difficult to incorporate in floating tablets but can easily be given in liquid dosage form released. Sodium alginate-based in-situ gelling systems were prepared by dissolving various concentrations of sodium alginate in deionized water, to which drug and calcium carbonate were added. Fourier transform infrared spectroscopies (FTIR) were used to check the presence of any interaction between the drug and the excipients. A 3² full factorial design was used for optimization. The concentrations of sodium alginate (X1) and calcium carbonate (X2) were selected as the independent variables. The amount of the drug released after 1 h (Q1) and 6 h (Q6) and 12 h (Q12) and the viscosity of the solution were selected as the dependent variables. The gels were studied for their viscosity, in-vitro buoyancy and drug release. Other ingredient like HPMC K100M used for strength forming polymer, sodium citrate is used for liquefying solution. The drug release from the in-situ gel follows the Higuchi model and Korsemeyer-peppas model, which indicates a diffusion-controlled release.

Key word: In situ gel, Levetiracetam, Floating.

ABSTRACT

The aim of present investigation was to develop press coated tablet for pulsatile drug delivery of lornoxicam using hydrophilic and hydrophobic polymers. The drug delivery system was designed to deliver the drug at such a time when it could be most needful to patient of rheumatoid arthritis. The press coated tablets containing lornoxicam in the inner core was formulated with an outer shell by different weight ratio of hydrophobic polymer (ethyl cellulose) and hydrophilic polymers (sodium alginate). The release profile of press coated tablet exhibited a lag time followed by burst release, in which outer shell ruptured into two halves. The effect of formulation composition on the barrier layer comprising both hydrophobic and hydrophilic excipients on the lag time of drug release was investigated. It was observed that lag time decreases with increasing concentration of sodium alginate. The optimized formulation (F5) comprised 10: 90%w/w concentration ratio of sodium alginate: Ethocel 10 cps with a 245 mg coating weight, and showed a desired lag time of 308 minutes, which mimics the fluctuating symptoms of rheumatoid arthritis, followed by rapid release of lornoxicam.

Keyword: Press-coated pulsatile tablet, lag time, ethyl cellulose, Sodium alginate, pulsatile drug delivery, Rheumatoid arthritis

ABSTRACT

Tuberculosis is a contagious infection caused by air borne bacteria Mycobacterium tuberculosis. Tuberculosis is a growing health problem in the developing world. India accounts for one-fifth of the global TB incident cases, each year nearly two million people in India develop TB¹. This was a retrospective record based survey carried at AH & RC (Adichunchanagiri Hospital & Research Centre) Tertiary care teaching hospital, B.G Nagara. Twelve month data of all TB patients i.e. from Sep-09 to Aug-10 that were diagnosed in the Directly Observed Treatment Short Course Centre was taken, which included 120 diagnosed patients. Out of 120 patients diagnosed, the male to female ratio was 2.5:1, and 29 were from age group of 40 to 49 years. Pulmonary TB cases were more i.e. 85 (75.83%) when compared to extra pulmonary i.e. 35 (29.17%), new smear positive cases were 62 (51.67%) and new smear negative cases were 58 (48.33%). Total 67 (55.83%) patients were categorized in CAT-I, 25 (20.83%) patients in CAT-II and 28 (23.33%) in CAT-III.The Treatment Completion Rate (TCR) and rate of cure was not known since all patients were transferred to their nearest peripheral RNTCP/DOTS Centers, and those centers failed to provide proper feedback. So, for transferred TB cases a better system of follow up should be done in order to know about the TCR and rate of cure.

Key Words: RNTCP/DOTS centre, Category, Tuberculosis, TCR (Treatment Completion Rate).

ABSTRACT

This work investigates the development and evaluation of hydrodynamically balanced systems (HBSs) of aceclofenac as single unit capsule. The various HBS capsules were formulated by physical blending of aceclofenac with carbopol 934, hydroxypropyl methyl cellulose, pectin in different ratios. These HBS capsules were evaluated for weight uniformity, drug content uniformity, in vitro floating behavior and drug release in simulated gastric fluids (pH 1.2). All these formulated HBS capsules containing aceclofenac were floated well over 5 hours with no floating lag time, and also showed sustained in vitro drug release in simulated gastric fluid over 5 hours. The aceclofenac release was found to be more sustaining with the addition of polymer i.e. carbopol 934 and hydroxyl propyl methyl cellulose. The drug release pattern of these aceclofenac HBS capsules (F-1, F-4, F-5 and F-8) were correlated well with first order model where F-6 to F-7 and F-2 toF-3 was correlated well with Higuchi model Korsmeyer-Peppas model with Fickian diffusion mechanism. All the experimental results showed that the aceclofenac HBS capsule successfully sustain the drug release along with improve the oral bioavailability of candidate drug.

Keywords: Hydrodynamically balanced system, gastroretention, aceclofenac, capsules.

ABSTRACT

Over the years, inclusion complexation of drugs with β-cyclodextrin has emerged as a viable attempt to improve the dissolution of water insoluble drugs. The aim of the present work was to improve the dissolution rate of Glimepiride, by inclusion complexation with β-cyclodextrin. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of glimepiride with β-cyclodextrin was 1:1, 1:2, & 1:5. The solubility of glimepiride increased with increasing amount of β-cyclodextrin in water. Complexes of glimepiride were prepared with β-cyclodextrin by kneading method and physical mixture. The complexes were characterized by Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) patterns. These studies indicated the inclusion of glimepiride in the cavity of β-cyclodextrin. The complexation resulted in a marked improvement in the solubility of glimepiride. An optimum increase in the dissolution rate of the drug was observed at a drug-polymer concentration of 1:5 concentrations. Mean dissolution time of glimepiride decreased significantly after preparation of complexes of glimepiride with β-cyclodextrin.

Keywords: Glimepiride, β-cyclodextrin, inclusion complexation, in vitro dissolution studies.

ABSTRACT

The present study deals with the dissolution of an angiotensin II receptor antagonist drug, candesartan. Candesartan cilexetil is a poorly water-soluble prodrug. The in vitro dissolution testing of Candesartan cilexetil in water and buffer solutions is not possible. In the present study, an attempt was made to develop a dissolution medium for in vitro testing of the drug. A Kromacil C18, 5µm column having 150x4.6 mm internal diameter in isocratic mode with mobile phase containing mixture of buffer (pH 4.5) and acetonitrile in ratio of 45:55 was used. The flow rate was 1.5 mL/min and effluents were monitored by UV at 257 nm. The selection of the medium was made on the basis of solubility data of Candesartan cilexetil in different dissolution medium at 37 °C. Solubility data revealed that phosphate buffer (pH 6.5) consisting of 0.35% w/v tween 20 could be a suitable dissolution medium.

Key words: Candesartan, solubility, buffer, dissolution.

ABSTRACT

The purpose of the present study was to design, characterize and evaluate extended release coated tablets of Metoprolol Succinate (MS) to reduce its dosing frequency. Core tablets were prepared using various matrix forming agents like HPMC, HPC, and HEC, and further subjected for coating using blend of aqueous dispersion of a hydrophobic and hydrophilic polymer, (Surelease®: HPMC E15) to control the drug release of the highly water soluble drug Metoprolol Succinate. Varying the matrix forming agent concentrations in the core tablets and percentage coating build up on core tablets showed range of drug release patterns in phosphate buffer pH 6.8. The present study dealt with the suitable grade of cellulose polymer and optimized coating composition which can modify the drug release to match up with the USP dissolution specifications and marketed product for the MS. The optimized formulation containing Metolose 90 SH 100000 and 3% coating with plasticized Surelease: hydroxypropyl methylcellulose (HPMC E15) showed extended drug release up to 24hrs and the drug release pattern was similar with the specifications. The in-vitro dissolution studies revealed that the release rate is inversely proportional to the concentration of matrix former in the core tablet and percent of coating thickness. The kinetic treatment illustrate that the optimized formulation HMC5 followed zero order kinetics with diffusion mediated drug release which is evidenced from n value of (0.73) Peppas equation. FT-IR and DSC studies indicated no interaction between the drug and excipients and prepared formulations showed good stability as per ICH guidelines.

Key words: Metoprolol Succinate, Extended Release, HPMC E15, Surelease, Coated Tablet

ABSTRACT

The objective of this study was to develop effective buccoadhesive bilayered tablets of Eletriptan hydrobromide containing bioadhesive layer and drug free backing layer, expected to release the drug in unidirectional for extended period of time. Buccoadhesive tablets were prepared by using HPMC K4M, Carbopol 941NF and Carbopol 974p as mucoadhesive polymers with varying concentrations. The formulations were tested for in-vitro drug release, bioadhesive strength, moisture absorption, residence time and drug permeation through porcine buccal mucosa. Optimized formulation F3 of HPMC K4M showed maximum release of the drug (97.83±0.41), best fit in the peppas model and permeated 73.52% of the drug through porcine buccal membrane.

Keywords: Eletriptan  Hydrobromide, ex vivo permeation studies, mucoadhesive buccal tablet, mechanical properties, in vitro studies, buccoadhesive

ABSTRACT

The present study involves the formulation and evaluation of o/w nanoemulsions with two simple edible oils in micro-liter quantities, avoiding large quantities of surfactants and co-surfactants. The nanoemulsions were prepared by high energy emulsification technique. The process optimization was based on the particle size, size distribution and entrapment efficiency in relation with the quantity of oil and concentration of surfactant. The percent drug content was determined by HPLC with UV detector. The particle size, polydispersity index (PDI), and zeta potential of nanoemulsions were determined by using particle sizer. Stability studies at 4°C for two months, centrifugation and freeze-thaw cycling were carried out.  Pharmacokinetic studies of nanoemulsion and marketed dosage form were performed in male SD rats and blood plasma samples were analyzed by LC-MS/MS. The particle size, polydispersity index (PDI), and zeta potential of nanoemulsions were found to be in the range of 26.8±0.72 to 154.6±11.4 nm, 0.09±0.01 to 0.28±0.06 and 0.07±0.01 to -28±0.65 mv respectively. Transmission electron microscopy (TEM) and stability studies revealed the physical stability of the nanoemulsions. The percent drug content was found to be in the range of 73.74±3.79 to 101.16±1.35. The oral bio-availability was significantly increased in nanoemulsion compared with the marketed dosage form. These results showed a successful incorporation of felodipine into nanoemulsion with high drug loading efficiency and good stability.

Key words: Sesame oil, olive oil, felodipine, sonication, Oral bioavailability.

ABSTRACT

Vanilla planifolia grown for its attractive aroma has rich medicinal value as evidenced by its antimutagenic, antinvasive, anti-metastatic, antinociceptive property and protection against amygdala-kindled seizures. Lack of scientific data authentifying its antiepileptic potential prompted us to evaluate its antiepileptic activity in chemically and electrically induced seizures. Swiss albino mice and Wistar albino rats of either sex (n=6) were induced with seizures using Pentylenetetrazole (PTZ) 60mg/kg i.p. and Maximal electro shock (MES) (50mA for 0.2 seconds) respectively. Sodium valproate 100mg/kg and Phenytoin 25mg/kg served as controls for the respective groups. Vanillin was administered at 100, 200 and 500mg/kg per oral one hour prior to induction of convulsions. The parameters studied include: Onset and duration of tonic flexion and extension, onset of clonic seizure, time for recovery/ death (MES model); Onset of myoclonic jerks and number of episodes (PTZ model). Data were analyzed by one-way ANOVA followed by Dunnet’s test. P < 0.05 was considered as statistically significant. In the MES model, vanillin showed a dose dependent significant decrease in the onset and duration of extension when compared to Phenytoin (P< 0.01). A similar decrease in the onset and duration of flexion was also noted at 100 and 200mg/kg but this was not significant at 500mg/kg dose. In the PTZ induced seizure model, acute administration of vanillin increased latency of onset and decreased the duration of seizures in treated animals as compared to the control. To conclude, the results suggest that vanillin has anticonvulsive property.

Keywords: Vanillin, maximal electroshock seizures, pentylenetetrazole, anticonvulsant

ABSTRACT

To study the antitumor effect of Drosera indica L against Ehrlich ascites carcinoma (EAC) tumor in mice. Antitumor activity of ethanol and aqueous extracts (250 and500 mg/kg) of D. indica L was evaluated against Ehrlich ascites carcinoma (EAC) tumor in mice. Acute toxicity study was conducted to find out the safety of both extracts of D. indica L. After 24 h of tumor inoculation, the extracts were administered daily for 14 days. On day 15, mice were sacrificed for observation of antitumor activity. The effect of both extracts on the growth of transplantable murine tumor, life span of EAC bearing hosts and simultaneous alterations in the hematological profile and peritoneal fluid analysis (DNA, RNA, caspase-3 and total protein) were estimated.  Both the extracts showed decrease in packed cell volume and viable cell count and increased in mean survival time thereby increasing life span of EAC tumor bearing mice. Hematological profile reverted to more or less normal levels in extracts treated mice. Treatment with extracts decreased the levels of RNA, DNA and increased level of caspase-3.The ethanol and aqueous extracts of D. indica L exhibited antitumor effect in EAC bearing mice.

Key words: Drosera indica L, Ehrlich ascites carcinoma, hematological profile, peritoneal fluid analysis

ABSTRACT

Several pharmacological activities like anti-cancer, anti-microbial, antibacterial, antifungal, and anti-viral activity have been attributed to tetrahydrocarbazole. The above observations prompted us to synthesize some novel tetrahydrocarbazole derivatives as possible anticancer agents. A series of novel tetrahydrocarbazole derivatives have been synthesized by the reaction of tetrahydrocarbazole with substituted aromatic aldehydes. The starting material, tetrahydrocarbazole were prepared by Fischer indolisation reaction of cyclohexanone with phenylhydrazine in the presence of acetic acid. The cycloaddition of tetrahydrocarcazole and substituted aromatic aldehydes gives tetrahydrocarbazole derivatives (A₁-A₁₀). The structures of synthesized derivatives were confirmed by IR, ¹HNMR and Mass spectrum. The synthesized compounds were screened for their in-vitro anticancer activity. The anticancer activity data of the synthesized derivatives were found to be potent activity.

Key words: Phenyl hydrazine, Cyclohexanone, Tetrahydrocarbazole derivatives, In-vitro anticancer activity.

ABSTRACT

In present investigation, methanolic extract of different marketed Aegle marmelos formulations (F₁, F₂, F₃, and F₄) screened for determination of total phenolic and flavanoid contents.  Highest phenolic (6.145 ± 0.05 mg/kg) and flavonoid (8.134 ± 0.044 mg/kg) contents were noticed in formulation F₄. Free radical scavenging activity of all the studied formulations were evaluated by using DPPH (1,1-Diphenyl-2-picryl hydrazyl) method. Whereas, each formulation showed good scavenging of DPPH radical with IC₅₀ values (F₁-2.185, F₂-2.216, F₃-2.243 and F₄-2.143 µg/ml), and is comparable to standard compounds (BHT, ascorbic acid and rutin).

Key-Words: Aegle marmelos, Total phenolic contents, Total flavanoid contents, DPPH

ABSTRACT

The aim of present study was to estimate the in vitro antioxidant activity of alcoholic extract of Cucumis callosus (Rottl.) Cogn (Cucurbitaceae) seeds which is commonly known as “Kachri” in Rajasthan (India) evaluated by using DPPH radical scavenging activity and hydrogen peroxide radical scavenging activity assay. The antioxidant activity was compared with ascorbic acid as standard. The IC₅₀ values of Cucumis callosus and ascorbic acid were found 41.99 μg/ml and 24.27 μg/ml respectively for the DPPH radical scavenging activity while 95.27 μg/ml and 153.35 μg/ml respectively for hydrogen peroxide radical scavenging activity. Thus, alcoholic extract of Cucumis callosus seeds possess potent antioxidant activity in hydrogen peroxide model and may be useful for preparation of neutraceuticals as potent antioxidant to treat various human diseases.

Key words: Cucumis callosus, Seeds, Antioxidant, Free radical scavenging, DPPH

ABSTRACT

The methanol extract of Callistemon salignus was subjected to different phytochemical tests  and gives positive results for glycosides, tannin, carbohydrate, volatile oil, flavonoid and steroid. This extract leads to the isolation of 3′, 4′, 5, 7-tetra-hydroxy flavonol by chromatographic separation through a graded elution. The identity of the isolated compound was checked by preliminary phytochemical test, TLC study, solubility, melting point determination. Finally the structure was elucidated by different spectroscopic methods such as UV, IR, NMR (13 _C NMR and Proton NMR) and LCMS. On the basis of this chemical and spectral evidence and upon comparison with the literature data, the isolated compound is identified .The compound was isolated first time from this plant extract.

Keywords:Callistemon salignus, 3′, 4′, 5, 7-tetra-hydroxy flavonol, graded elution, spectroscopic methods.

ABSTRACT

Floating drug delivery system is one of the novel drug delivery system. Floating drug delivery system have a bulk density less than gastric fluids and so remain buoyant in the stomach without affecting gastric emptying rate for a prolonged period of time. The aim of the present study was to develop floating microspheres of Rabeprazole sodium(RPS), which belong to class of proton pump inhibitor. Floating microspheres of Rabeprazole were prepared by emulsion solvent evaporation method using HPMC K15M and ethyl cellulose as polymer. Six different formulations were developed. The floating microsphere was evaluated for angle of repose, particle size, percentage yield, in vitro buoyancy, incorporation efficiency, drug polymer compatibility (IR study), scanning electron microscopy, drug release and DSC(Differential Scanning colorimetry), X-Ray Diffraction(XRD) of microsphere. Results show that as the concentration of polymer increases it affects the particle size, percentage yield, in vitro buoyancy and drug release of microsphere. Formulations prepared with HPMC K15M exhibited excellent Micromeritic properties, percentage yield, in vitro buoyancy, incorporation efficiency and percentage drug release when compared to ethyl cellulose polymer. Results of our present study suggest that floating microsphere of Rabeprazole sodium can be successfully designed to develop controlled drug delivery which can reduce dosing frequency thus this formulation can be considered as an alternative to conventional dosage forms.

Key words: floating drug delivery systems, Rabeprazole sodium (RPS), incorporation efficiency, dosing frequency, DSC(Differential Scanning colorimetry)  X-Ray Diffraction (XRD)

ABSTRACT

Glimepiride loaded polymeric blend matrices were prepared using hydrogel forming polysaccharide like agar, isabgol, aloe vera and gelatin by solution blending method. The polymeric blends were characterized by Fourier-transform infrared spectroscopy revealed that there was no reaction between drug and polymers. The surface morphology of prepared polymeric blends was studied by scanning electron microscopy which suggested that polymeric blend matrices have smooth/rough surface with vacuoles. All the polymeric blend matrices were evaluated for weight variation, hardness, thickness and drug content which suggested that all these parameters were uniform as the total amount of the polymers was fixed to 10%. The polymer blend matrices show good hardness of more than 8 kg/cm² and drug content more than 95 % suggested that the solution blending method used was suitable for the preparation of polymeric blends. The polymeric blend showed good swelling in the range of 244.12 to 411.22 % within 8 h maintaining integrity of formulation. The in vitro release of the glimepiride was rapid in phosphate buffer pH 6.8 with more than 81.96% released within 8 h. Increases in the amount of agar enhance the in vitro release whereas increases in the amount of gelatin decrease the release of glimepiride. Hence the polymeric blends prepared with agar or gelatins with other polysaccharide as binary or ternary system extend the glimepiride up to 8 h and can be used for effective management of diabetes and also presence of aloe vera may provide synergistic hypoglycemic effect.

Keywords: Glimepiride; Polymer blend; In-vitro swelling; In-vitro release

ABSTRACT

Dental implant is a pharmaceutical device in the form of strip with very small loading and size of 0.25 sq cm. For site-specific one-time continuous delivery of Gatifloxacin an antimicrobial compound with excellent activity against anaerobic micro-organism in the treatment of periodontal disease was prepared by solvent casting technique using ethyl cellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose K4M and Eudragit RL-100 with dibutylphthalate as plasticizer. The physicochemical parameters like thickness, weight variation, content uniformity and release characteristics were evaluated The drug release was initially high on day one to achieve immediate therapeutic level of drug in pocket, followed by marked fall in release by day two, and progressive moderate release profile to maintain therapeutic level following anomalous transport mechanism. Formulation F6 released 97.34% of drug at the end of 144 h and was considered as best formulation. In vitro antibacterial activity was carried out on Streptococcus mutans .

Keywords: Dental Implant, Gatifloxacin, In vitro, physicochemical, antimicrobial, streptococcus.

ABSTRACT

During present laboratory experiment, comparative analysis of three dominant edible and medicinal macro fungal species viz., Laccaria lacata, Lycoperdon pyriforme and Ramaria botrytis with reference to protein, carbohydrate and fat was done. The biochemical analysis revealed that the studied macro fungi contained 25.71, 38.0, 13.55% protein, 58.5, 49.88, 72.88% carbohydrate and 3.3, 9.6, 4.22% fat respectively. Besides this, the studied mycotaxon have promising moisture, dry matter, ash and crude fibers contents. In addition, pH of individual fungal species was determined in order to verify their edibility test. Thus, this study proves that aforesaid macro fungi can be used in well balanced diets due to their nutritional value.

Keyword: Wild macro fungi, Nutritive value, Kathmandu valley

ABSTRACT

A Reversed-Phase High Performance liquid chromatographic (RP-HPLC) method was developed for the simultaneous determination of Ambroxol Hydrochloride and Cefpodoxime Proxetile in combined tablet dosage form. The analysis was carried out using Phenomenex Luna C – 18, pre-packed column. Mobile phase, containing Acetonitrile: 0.05 M Potassium Dihydrogen Ortho Phosphate Buffer (70:30) pH adjusted to 6.7 with Tri ethyl Amine was pumped at a flow rate of 1.0 mL/min with UV-detection at 245 nm. Retention time was 3.34 ± 0.01 min and 4.77 ± 0.01 min for Ambroxol Hydrochloride and Cefpodoxime Proxetile, respectively. The method was validated for linearity, accuracy, precision, and specificity. The method showed good linearity in the range of 30 - 60 μg/ml for Ambroxol Hydrochloride and 50 - 100 μg/ml for Cefpodoxime Proxetile. The detection limit of the proposed method was 4.56 and 12.51 μg/ml and the quantification limit was 13.82 and 37.92 μg/ml for Ambroxol Hydrochloride and Cefpodoxime Proxetile, respectively. The % recovery was within the range between 99.57% and 100.27% for Ambroxol Hydrochloride and % recovery was within the range between 99.89% and 100.86% for Cefpodoxime Proxetile. The % R.S.D for precision and accuracy of the method was found to be less than 2%. The method was validated as per the ICH guidelines. The method was successfully applied for routine analysis of Ambroxol Hydrochloride and Cefpodoxime Proxetile in combined tablet dosage form.

Keywords Ambroxol Hydrochloride, Cefpodoxime Proxetile, High Performance Liquid Chromatography Method, Validation 

ABSTRACT

Present work describes a selective, precise and accurate Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) method for simultaneous estimation of Escitalopram Oxalate (ESC) and Etizolam (ETI) on Kromasil 100 C18, 5µ(150×4.6 mm) Column using Acetonitrile:0.005 M Hexane Sulfonic Acid pH 3.0 (adjusted with o-phosphoric acid) (40:60 v/v) as mobile phase, at a flow rate of 1.0 ml/min and the detection wavelength was 254 nm. The retention time for ESC and ETI was found to be 3.66 and 8.07 min, respectively. The ion-pairing reagent improved the retention of polar ESC on Reverse-phase column. The method was validated for linearity, precision, accuracy, LOD, LOQ robustness, solution stability and specificity. The method was linear in the concentration range of 20-160µg/ml for ESC and 2-16 µg/ml for ETI with a correlation coefficient of 0.9994 and 0.9993 for respective drugs. The percent recovery was found in the range of 98.14-101.72% and 98.83-101.12 % for ESC and ETI, respectively. The specificity of method was established based on peak purity data. The proposed method was successfully applied for quantitative determination of escitalopram oxalate and Etizolam in combined tablet dosage form for routine analysis.

Keywords: RP-HPLC, Simultaneous, Escitalopram Oxalate, Etizolam, Hexane Sulfonic Acid 

ABSTRACT

In this present work Erythromycin stearate nanosuspension has been formulated. Since Erythromycin stearate is insoluble in water, it has been formulated as nanosuspension to improve bioavailability of the drug. The formulation was carried out using High Pressure Homogenization method using different variables like drug-surfactants ratio, stirring speed and rotation time, to optimize the final formulation while keeping the quantities of active ingredient constant. An optimized final formulation was prepared by using drug, poloxamer 188 and tween20 in 1:2:2 ratios with stirring speed of 25000 rpm for 25 minutes using High Pressure Homogenizer (Polytron PT 1600E) followed by lyophilisation. The optimized final formulation was subjected to in-vitro parameters such as compatibility, drug content, particle size analysis, zeta-potential, SEM, in-vitro release profile. All the in vitro evaluation parameters complied the limits. Stability studies were also conducted as per ICH guidelines and from the result it may be concluded that the optimized formulation is stable. Finally, it is concluded that the drug is compatible and stable with the excipients, hence Erythromycin stearate can be formulated as nanosuspension by this method.

Key words: Erythromycin stearate, Poloxamer 188, Nanosuspension, Zeta potential, DSC, SEM.

ABSTRACT

The present study involves the formulation and evaluation of buccal tablets of venlafaxine hydrochloride, an antidepressant drug belongs to class SNRI(serotonin-nonepinephrine reuptake inhibitor)has high first pass metabolism, So buccal drug delivery has been considered an alternative to the oral dosing for compound subjected to degradation in the gastrointestinal tract or to first pass metabolism. An attempt has been made to developed muccoadhesive buccal tablets comprising of drug containing mucoadhesive layers and drug free backing layer ethyl cellulose of to release the drug for extended period of time with reduction in dosing frequency, dose related side effects and improve bioavaibility of drug. Tablets of Venlafaxine Hydrochloride were prepared by direct compression using muccoadhesive polymers Carbopol 934-P and HPMC K4M.Buccal tablets were evaluated by different parameters such as thickness, hardness, weight uniformity, content uniformity, swelling index, surface pH, ex vivo bioadhesive strength, in vitro drug release, ex vivo drug permeation and FTIR studies. The modified in vitro assembly was used to measure the bioadhesive strength of tablets with fresh goat buccal mucosa as model tissue. In order to determine the mode of release, the data was subjected to Krosmeyer and Peppas diffusion model. All the formulations followed Fickian release mechanism. Tablet containing Carbopol 934P and HPMC K4M in the ratio of 1:1(25%) had maximum in vitro drug release for 8 hrs.

Keywords: Buccal tablets, Venlafaxine hydrochloride, in vitro drug release, ex vivo studies, kinetic model.

ABSTRACT

Benz-fused compounds have been employed in the synthesis of various compounds which show very potential pharmacological activities. Carbohydrate is the key element in variety of biological phenomena and its N-linked sugar derivatives also exhibit wide range of medicinal activities. Keeping in this view, when one biological active molecule is linked to another, the resultant molecule generally has increased potency.Hence for the first time, in present work, we have interacted two pharmocophores, hepta-O-benzoyl-β-D-lactosyl isothiocyanate  and substituted 2-hydrazino-1,3-benzothiazoles in acetone medium to yield hepta-O-benzoyl-β-D-lactosyl-3-(2)-hydrazino-1,3-benzothiazolyl thiocarbamides. The identities of these newly synthesised hepta-O-benzoyl-β-D-lactosyl-3-(2)-hydrazino-1,3-benzothiazolyl thiocarbamides have been established on the basis of usual chemical transformations and IR , ¹H NMR and Mass spectral studies. The antibacterial and antifungal activities of also reported. Some of these derivatives exhibit significant antimicrobial activity.

Key words: Lactosyl isothiocyanate, hydrazino benzothiazoles, lactosyl hydrazino benzothiazolyl thiocarbamides, antimicrobial activity.

ABSTRACT

The objective of this study was to develop and evaluate a pulsatile drug delivery system based on drug-containing core tablet, which were coated with a swelling layer. Core tablets of Salbutamol Sulphate were prepared by direct compression using a croscarmellose sodium as disintegrant, micro crystalline cellulose as diluent and other. Core tablets were evaluated for uniformity of weight and thickness, hardness, friability, disintegration and dissolution. Compression coating over the prepared core tablets were done using various grade of HPC. Different formulae S1 to S9 were prepared using different coat % weights gain and polymer ratio. The compression forces were kept constant by adjusting constant distance between the upper and lower punches. The prepared Salbutamol Sulphate tablets were evaluated for the Lag time and in vitro release characteristics at variant pH media mimicking the gastrointestinal media. The results showed that the developed core tablets of Salbutamol Sulphate comprised excellent physical characteristics and complied with the USP criteria. For the pulsatile system, a quick releasing core was formulated in order to obtain a rapid drug release after the rupture of the polymer coating. The lag time prior to the rapid drug release phase increased with increasing % coating level.

Key word: disintegrant, swelling layer, pulsatile release tablets, compression coating, lag time.

ABSTRACT

The objective of this study was to develop and evaluate controlled porosity osmotic pump tablet (CPOP) system to deliver Verapamil HCl inacontrolledmannerupto24 h. The porous osmotic pump contains pore forming water soluble additives in the coating membrane, which after coming in contact with water, dissolve, resulting in an in situ formation of a microporous structure. Mannitol was used as an osmotic agent and cellulose acetate (CA) was used as semipermeable membrane. Polyethylene glycol 400(PEG-400) was employed as a pore forming agent as well as plasticizer for controlling membrane porosity. The influences of drug: osmogent ratio, concentration of PEG-400 and membrane thickness on the release profiles were investigated using 2³ full factorial design and optimized batch was investigated in different environmental media and stirring rates. It was found that drug release rate increased with the amount of osmogent due to the increased water uptake, and hence increased driving force for drug release. This could be retarded by the proper concentration of channelling agent and membrane thickness in order to achieve the desired zero order release profile. This system was found to deliver Verapamil HCl at a zero order rate for24 h. The optimized formulations were subjected to stability studies as per ICH guidelines at different temperature and humidity conditions.

Keywords: verapamil hydrochloride; osmotic pump; kinetic study; 2³ factorial designs.

ABSTRACT

The study aim was concerned with formulation and in vitro evaluation of mucoadhesive buccal patch of carvedilol, which is extensively metabolized by liver. During last few years mucoadhesive dosage forms have promoted an area of drug delivery system that renders the treatment more effective and safe, not only for topical disorders but also for systemic problems. Therefore the present investigation is concerned with the development of the bucco-mucoadhesive patches, which were designed to prolong the buccal residence time, to increase penetration through buccal mucosa and thus increase the bioavailability. Various formulations were developed by using release rate controlling patches forming polymers like HPMC (K15, K4), HPC-L, Sodium alginate, PVP K30& Carbopol 934P in  alone & various combinations by solvent casting technique using plasticizer glycerol. For unidirectional release, backing layer prepared using ethyl cellulose 2.5%w/v dissolve in isopropyl alcohol and acetone. Glycerol used as a plasticizer was casted on the patches. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH, In vitro release studies, in vitro residence time, in vitro diffusion study. Patches exhibited drug release (diffusion) in the range of 75.69% to 96.53%. Kinetic models i.e. Higuchi, Korsemeyer-peppas, zero order were applied on data of diffusion release to explain release. The optimized formulation (F1) shows the zero order release.

Keyword: Buccal Patch, Carvedilol, Bioadhesion, Mucoadhesion, Buccal Drug Delivery.

ABSTRACT

Although pharmacotherapy in cardiovascular diseases can improve the well being, its benefit can be compromised by drug-related problems (DRPs). The objectives of the present study were to examine the number and nature of drug related problems in patients with cardiovascular diseases and to demonstrate the role of pharmacist in ensuring safe and efficient use of medicines in daily practice in the inpatient settings. A prospective cross sectional study was carried out for 8 months in the general medicine department of a 640 bedded multi-specialty private corporate hospital. The nature, prevalence and incidence of DRPs were studied and documented using the PCNE (Pharmaceutical Care Network Europe Foundation) classification system. A total of 1051 drugs were prescribed during the study period. Most commonly prescribed categories of drugs were antihypertensive (21.05%), anticoagulants and antiplatelet drugs (11.13%), antiulcers (8.84%), insulin and oral hypoglycemic agents (6.95%) and anti infectives (5.42%). Drug interactions (46.19%), drug over dosage (17.26%) and drug duplication (11.17%) were the most frequently occurring DRPs. Most common clinical risk factors identified were polypharmacy (66.21%) and diabetes mellitus (20.31%). Antihypertensive presented the highest drug risk ratio. Statistical analysis showed positive correlation between age and number of DRPs in the study population. Pharmacist interventions were mostly on drug interactions, dosing and drug choice and 59% of them were accepted, resulting in prevention of DRP occurrence. The current study demonstrated the importance of routine medication review and the need of a pharmacist in a multidisciplinary team in treating cardiovascular diseases.

Key words: Drug related problems; cardiovascular diseases; drug interactions; clinical risk factors