ABSTRACT

In this article, the study of recent advancement of Solid dosage form capsule is  studying for better kind of dosage forms. There are two way approach for capsule dosage form innovation in capsule shell and innovation in capsule system. The present review focuses on innovation in capsule system. In this the study is about to reduce the frequency of dosing or to increase effectiveness of the drug by localization at the site of action, reducing the dose required, or providing uniform drug delivery. By the study of this recent advancement new kind of drug delivery system is developed which is used to Enhanced bioavailability, reduced side effects, improved patient compliance, reduced peak to trough ratio of drug in systemic circulation. The development of new generation of capsules are beneficial for night time dosing and for the drugs having high first pass effect and having specific site of absorption in Gastrointestinal tract.

Keywords: - Hard Gelatin Capsule, Soft Gelatin Capsule, Recent Advancement, Innercap, Chewcaps, Duocaps.

ABSTRACT

Asteracantha longifolia (L.) Nees. belonging to the family Acanthaceae is known as Talmakhana in Unani and Kokilasha in Ayurveda system of medicine. It is found in India, Srilanka, Burma and Nepal. The plant contains alkaloids, flavonoids, terpenoids, essential oil and phytosterols. It has been using in traditional systems of medicine since centuries for the treatment of diseases like low libido, premature ejaculation, ascites, jaundice and diseases of urogenital tract etc. Many pharmacological studies have been conducted on Asteracantha longifolia which proved its aphrodisiac, hepatoprotective, antioxidant and analgesic activities etc. In this review, an attempt has been made to present its phytochemical, pharmacological and other important aspects.

Key words: Asteracantha longifolia, Talmakhana, aphrodisiac, Ayurveda, Unani.

ABSTRACT

Oral delivery is at this time the gold standard in the drug manufacturing where it is considered as the safest, most convenient and greatest economical method of drug delivery. One such problem can be solved in the novel drug delivery system by formulating “mouth dissolving tablets” (MDTs) which disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of superdisintegrant or maximizing pore structure in the formulation. Some tablets are designed to dissolve in saliva remarkably fast, within a few seconds, and are true fast-dissolving tablets. Others contain agents to enhance the rate of tablet disintegration in the oral cavity, and are more appropriately termed fast-disintegrating tablets, as they may take up to a minute to completely disintegrate. Mouth dissolving tablets are solid dosage forms containing drugs that disintegrate in the oral cavity within less than one minute leaving an easy-to-swallow residue. This is seen to affect about 35% of the general population and associated with a number of circumstances like Parkinsonism, mental disability, motion sickness, unconsciousness, unavailability of the water etc. Other groups that may experience problems using conventional oral dosage forms include the mentally ill, the developmentally disabled, and patients who are uncooperative, on reduced liquid-intake plans, or are nauseated. To overcome such difficulties, mouth dissolving tablets have been developed. The aim of this review article is to give an overview on desired characteristics, advantages, preparation techniques and patented technologies of FDTs formulation.

Keywords:  FDT, Patients compliance, super disintigrants,  Technology, Evaluation.

ABSTRACT

The budding regulatory professional who has just stepped in the new horizon of pharma field, may find starting and conducting clinical studies and getting relevant authorization or approval in the United Kingdom complicated and time-consuming process, which it is actually. But this article will help them giving an insight on what steps are followed to conduct clinical trial in general, how to apply for a clinical trial authorization in UK, what documents required in a nutshell and how to get clinical trial approval with less effort, and in more smooth and efficient manner. We all know that time for pharma field is equivalent to money, as pharma companies use to have a huge expenditure in research and development of a medicine and to recover that huge expenditure they would seek for regulatory approval as faster as they can manage so that they can market the drug, once the safety and efficacy data is established through clinical trials. And thus this article will aid to new regulatory professionals who are interested to involve in the regulatory activities pertaining to clinical trials in a highly regulated market like United Kingdom and thus with better understanding with regulatory process they can save the time of company and can go through this complex system successfully.

Keywords: UK MHRA, Clinical Trial, Notification Scheme.

ABSTRACT

The objective of this paper is to give insight and better understanding of the regulatory requirements for changes done for an approved New Drug Application (NDA) in United States (US). For technical advancements, there may be situations which demand/ necessitate modifications for an approved NDA. The changes must be in conformance with the regulatory requirements of the Food and Drug Administration (FDA), the ultimate authority for the Drug related approvals in US. The changes must be systematically reported to the regulatory authorities in the recommended formats, termed as “Post approval changes for an NDA”. Section 506A of Federal Food, Drug, and Cosmetic Act, provides requirements for making and reporting manufacturing changes to an approved application and for distributing a drug product made with such changes. The FDA has revised its regulations on supplements and other changes to an approved application (21 CFR 314.70) to conform to section 506A of the Act. The changes can be major, moderate or minor depending on the changes likely to affect the quality, safety and efficacy of the product. Irrespective of the category of the changes, every change is to be brought to the notice of the US FDA in stringent, structured and stipulated format that are recommended for the regulatory advancements. If manufacturers are to achieve the much-heralded desired state, it is essential to allow some manufacturing changes. Firms would still be responsible for ensuring product quality. The goal is well known, the components needing change are well understood and characterized and the process well defined.

Key words: NDA, USFDA, Post approval changes, Regulatory Authorities

ABSTRACT

A recent advance in Novel Drug Delivery System (NDDS) aims to enhance safety and efficacy of drug molecule by formulating a convenient dosage form for administration and to achieve better patient compliance. Mouth dissolving tablets or fast dissolving tablets have received ever-increasing demand during the last decade, and the field have been rapidly growing in  the pharmaceutical industry and gaining popularity due to ease of administration  and better patient compliance to all age groups. MDDDS have the unique property of dissolving and/or rapidly disintegrating and releasing the drug as soon as they come in contact with saliva, thus obviating the requirement of water during administration. This review focusses on various formulations and also technologies developed to achieve fast dissolution/dispersion of tablets in the oral cavity. The target population for these new fast dissolving/ disintegrating dosage forms have generally been pediatric, geriatric, and bedridden or developmentally disabled patients. Patients with persistent nausea, who are in traveling, or who have little or no access to water are also good candidates for MDDTs.

Keywords: Fast dissolving, orodispersible, taste masking, superdisintegrants, rapidly disintegrating.

ABSTRACT

The novel carriers have been exploited through almost all the routes of administration. Many newer carriers are evolving with the advent of technology and the demand of targeted delivery like microemulsions. Microemulsions are clear, stable, isotropic mixtures of oil, water and surfactant. These systems are currently of interest because of their considerable potential to act as drug delivery vehicles by incorporating a wide range of drug molecules. In addition to oral and intravenous delivery, they are amenable for sustained and targeted delivery through nasal, pulmonary, vaginal and topical routes. The intent of the paper focuses on use of microemulsion technology in intranasal drug delivery along with mechanism.

Keywords: Microemulsion, Intranasal, Drug delivery system

ABSTRACT

In view of digital global agenda, the time has come for Good eCTD Practices. This article holds discussion about the measures to be taken before preparing and while submitting the dossier in eCTD format. The eCTD is an interface between industry and agency for transferring regulatory information while at the same time taking into consideration the facilitation of the creation, review, lifecycle management and archival of the electronic submission. eCTD is an electronic arrangement with extension of CTD, whose structure is specified by XML (Extensible Markup Language) eCTD DTD (Document Type Definition). While many organizations have delayed their adoption of eCTD format, the USFDA and several other global agencies are pressing forward towards its mandate. Though eCTD specification lists the criteria that will make an electronic submission technically valid, many companies are suffering from delays that occur not due to lack of data but due to technical and other issues of eCTD submission. The eCTD submission requirements definitely pose great challenges to the industry and regulatory agencies. There has to be an investment in information and communication technology as well as development of digital competitiveness among the regulatory professionals within the industry and regulators, alike. The regulatory professionals should know the standards, groundwork, expertise and technology required to submit an electronic submission globally. Due to its cost effectiveness, and because it guarantees a response from the recipient regulatory agency, reducing time to market, the eCTD has become the standard for numerous regulatory agencies around the world.

Keywords: eCTD, Electronic Submission, Study Tagging Files, Granularity, eCTD validation

ABSTRACT

Liquisoild technique is a novel concept for delivery of drugs through oral route. This approach of delivering drugs is suitable mostly for lipophilic drugs and poorly or water insoluble drugs. With this approach sustained release formulation of hydrophilic drugs or freely water soluble drug can also be prepare. Release enhancement of poorly soluble drugs is achieved by choosing nonvolatile solvent with maximum drug solubility, Unlike this, in retardation of drug release nonvolatile solvent with lowest drug solubility is choosen. It was found from the study that if nonvolatile solvent alone is not sufficient for prolonging the drug release then various release retarding agent is used. The release retarding or sustained release agent used, may be of natural or synthetic origin.

Keywords: c

ABSTRACT

Density functional theory (DFT) and Time dependent density functional theory (TDDFT) calculations have been carried out to study the electronic structure and the UV absorption spectra of Tolperisone. The UV spectra have been investigated with inclusion of solvent effect. The B3LYP functional with cc-pVDZ basis sets have been used for geometry optimization and also to compute absorption energies. The solvent effects have been included using the polarizable continuum model (PCM). The vertical absorption energies both in gas phase and in polar solvents such as water, methanol and ethanol were computed. The absorption maximum both in gas phase and in polar solvents is discussed in terms of electrostatic interaction energy, oscillator strength and dipole moment.

Keywords: DFT; TDDFT; cc-pVDZ; PCM; Tolperisone.

ABSTRACT

Chitosan is a natural, biologically safe polymer synthesized from chitin by deacetylation reaction. It is a tough, biodegradable, biocompatible, non-toxic linear polysaccharide suitable for various applications in pharmaceutical drug delivery technology. Chitosan has unique physicochemical and biological characteristics demanded for the development of safe and effective drug delivery systems.  One of the most properties of chitosan is for chelation. It can selectively bind to desired materials such as cholesterol, fats, metal ions, and protein and tumor cells. It also does not cause allergic reactions and rejection and is biodegradable in nature. It is metabolized into harmless products (amino sugars), which are completely absorbed by the human body. Chitosan being a good cationic polymer for membrane formation; have also been useful as artificial kidney membranes. Along with these properties it also possesses certain medicinal applications such as analgesic, hypocholesterolemic, hemostatic  antitumor, anti-oxidant spermicidal, CNS depressant, immunoadjuvant properties, antacid, antiulcer activities, wound and burn healing action and has been found to be suitable for immobilization of enzymes and living cells in ophthalmology Important applications of chitosan in the pharmaceutical industry are in the development of nasal, vaginal, ophthalmic, transdermal & topical, buccal, parenteral, colon-specific and in implantable drug delivery systems. This paper discusses the potential of chitosan in the development of drug delivery systems.

Keywords: Chitosan, Structure, Drug delivery, Pharmaceutical applications

ABSTRACT

Conventionally, drugs are released in an instant or absolute manner. Nevertheless, in current days, Pulsatile Drug Release Systems (PDRS) are gaining upward attention. Pulsatile delivery is defined as the rapid and transient release of certain amounts of drug molecules within a short time period immediately after a predetermined off-release period, i.e., lag time. PDRS can be classified in single and multiple pulse systems. This system provides spatial and temporal delivery of the drug. These systems are designed according to the circadian rhythm or biological clock of the body. These deliver the drug at the right time and at the right place and in the right amount thus increasing patient compliance. Pulsatile systems are beneficial for drugs where night time dosing is required, such as anti-asthmatic and anti-arrhythmic drugs where the disease severity is time dependent. This concept has several advantages, notably maximum therapeutic benefit, minimum harm, improved patient convenience and compliance. Pharmacists must realize the need to develop and dispense such medications having potential therapeutic benefit. The current article focuses on the diseases requiring PDDS, methodologies involved for the existing systems, and PDDS product currently available in the market.

Keywords: Chronopharmacological, Port System, Pulsincap system, osmotic pumps.

ABSTRACT

Dubowitz syndrome is a genetic and chromosomal instability disorder characterized by growth hormone deficiency or defects in the cholesterol biosynthetic pathway. It is characterized by retarded growth, several craniofacial manifestations, skin eruption, soft-tissue syndactyly, central nervous system and oral manifestations. There are reports of even malignant tumors associated with this syndrome. This manuscript reviews the manifestations and management of the dubowitz syndrome.

Keywords: Dubowitz, Growth deficiency, Malignant 

ABSTRACT.

Until today the treatment of scorpion stings by means of plants occupies a significant place in traditional medicine, and in spite the emergence of modern medicine, people have kept on using plants, as the knowledge of which has been passed over centuries from one generation to the next as Ayurvedic medicine shows.

Keywords: Scorpion; Envenomation; Traditional remedies; Plants

ABSTRACT

The current practice of characterization and control of impurities in pharmaceuticals is reviewed with emphasis on issues specific to the generic industry. This review includes an overview of FDA, ICH, TGA, TPD and EMEA guidelines related to impurities in Drug Substance and Drug Products. This introduces the identification, characterization and qualification procedures for ANDAs and approaches to the establishment of acceptance criteria for both drug substance and drug product and significance of analytical methods in total process.

Keywords: Acceptance Criteria, Analytical Methods, Characterization, Drug Products, Drug Substance, Impurities, Qualification

ABSTRACT

To assure the quality of drugs, impurities must be monitored carefully. It is important to understand what constitutes an impurity and to identify potential sources of such impurities. Selective analytical methods need to be developed to monitor them. It is generally desirable to profile impurities to provide a yardstick for comparative purposes. New impurities may be observed as changes are made in the synthesis, formulation, or production procedures, albeit for improving them. At times it is necessary to isolate and characterize an impurity when hyphenated methods do not yield the structure or when confirmation is necessary with an authentic material. Availability of an authentic material can also allow toxicological studies and provide a standard for routine monitoring of the drug product.

Keywords: Impurity profiling, degradation products, hyphenated techniques, ICH guidelines, pharmaceutical analysis.

ABSTRACT

Phytosomes are recently introduced herbal formulations that are better absorbed, and as a result produce better bioavailability and actions than the conventional phytomolecules or botanical extracts. This is an advanced form of herbal formulations which contains the bioactive phytoconstituents of herbal extract bounded in a lipophilic carrier. Phytosome technology has been effectively used to enhance the bioavailability of many popular herbal extracts and phytoconstituents including Ginkgo biloba, milk thistle, grape seed, green tea, hawthorn, ginseng etc and can be developed for various therapeutic uses or dietary supplements.

Keywords: Phytosomes, absorption, phospholipids, bioavailability.

ABSTRACT

Solubility plays a vital role in achieving the therapeutic efficacy of a drug from a dosage form. Advances in molecular screening techniques for identification of potential drug molecules investigated an increased number of new pharmacologically active lipophilic compounds that are poorly water soluble. About 40% of new chemical entities have been discovered as poorly water soluble. Numbers of technical strategies have been investigated for improving bioavailability like solid dispersions, cyclodextrins, micronization, surfactants, nanoparticles, lipids, permeation enhancers etc. It is a great task for pharmaceutical scientist to formulate oral dosage forms of these drug candidates with sufficient bioavailability. Among the various approaches to improve oral bioavailability of these drug candidates, Self- dispersing lipid formulations (SDLF’s) is one of the approaches used to improve the bioavailability of lipophilic drugs. SDLF’s is very broad area which covers Self-emulsifying drug delivery systems (SEDDS), Self-microemulsifying drug delivery systems (SMEDDS) and Self-nanoemulsifying drug delivery systems (SNEDDS) as carrier systems that have been developed. This review article covers basics of SDLF’s particularly SMEDDS and recent research updates in SDLF’s i.e. the research carried out and most recent solid SDLF’s.

Keywords: self-dispersing lipid formulations, self-micro emulsifying drug delivery system, solubility, bioavailability, lipophilic.

ABSTRACT

The present study was aimed to study the requirements of bioequivalence for registration of pharmaceutical products in various countries. It is essential for pharmaceutical industry to study the guidelines of bioequivalence for respective country where industry would like to apply for ANDA and thus want to enter into generic market. This study gives insight about requirements of bioequivalence with study parameters such as study design, fasting or fed state studies, volunteers recruitment, study dose, sampling points, analytical method validation parameters, moieties to be measured in plasma, pharmacokinetic parameters, criteria for bioequivalence, GCP requirements etc. which are needed for pharmaceutical industry to carry out bioequivalence studies and to file ANDA. Test products for these bioequivalence studies are usually manufactured by a sponsor or manufacturer while reference is provided by the government laboratories of respective countries. Sampling points also varies with respect to the regulatory guidelines of these countries. India follows Indian GCP guidelines, South-Africa MCC GCP guidelines and Australia follows ICH GCP guidelines. Criteria of bioequivalence, for India and South-Africa is 90% CI 80-125% for C_max, AUC_t, AUC_o-inf. for Australia 90% CI 80-125% for C_max, hAUC_t, AUC_o-inf.

Keywords: Bioequivalence, Bioavailability, ANDA, Pharmacokinetics

ABSTRACT

The aim of writing this review is to put a light on the recent trends in development of Drug loaded Beads. Drug loaded beads are gastro retentive drug delivery systems based on multi Unit approach and are prepared to obtain prolonged or controlled drug delivery, to improve bioavailability, stability and target drug to specific sites. These are Spherical in shape and approximately 1.5 mm in diameter. These can be prepared by various methods like ionotropic gelation, hydrogel embedment, solvent evaporation and Melt Solidification by using different polymers. Promising enhancement in bioavailability and site specificity has been achieved by drug loaded beads.

Keywords: FDDS, Beads, Buoyancy, Polymers

ABSTRACT

High-resolution ultrasonic spectroscopy (HR-US) is an analytical technique based on the principle of measurement of velocity and attenuation of ultrasonic compression waves propagating through the analyzed sample. HR-US is advantageous over the other spectroscopic technique.This review directs toward the wide applications and recent advances in high-resolution ultrasonic spectroscopy. Ultrasonic velocity and ultrasonic attenuation are the key parameter in the material analysis, microscopic particle size determination in suspension, emulsion and in the analysis of other biochemical products. HR-US spectroscopy in combination with liquid chromatography system has great importance in the analysis of colloidal systems. Recently the HR-US system is used as a detector in titration technique to analyze the sample on the basis of their intermolecular interaction.

Keywords:Ultrasonic Spectroscopy, Optical transparency, ultrasonic attenuation and ultrasonic velocity.

ABSTRACT

A simple, accurate, precise and reproducible method has been developed for the simultaneous estimation of Vildagliptin and Metformin hydrochloride in combined tablet dosage forms. As there are no reported UV methods for the simultaneous estimation of Vildagliptin and Metformin hydrochloride in their combined dosage form, a need was felt to develop new methods to analyze the drugs simultaneously. The estimation was done by multi-wavelength technique, at wavelengths of 217 nm and 234 nm over the concentration ranges of 0.7µg/ml and 7 µg/ml with mean recovery 100% for both drugs Vildagliptin and Metformin hydrochloride respectively. The results of the analysis were validated statistically and recovery studies were carried out as per ICH guide lines. Thus the proposed method can be successfully applied for the simultaneous estimation of Vildagliptin and Metformin hydrochloride in routine analysis work.

Keywords: Vildagliptin, Metformin, Simultaneous, Multi-wavelength, spectro-photometric.

ABSTRACT

Sterculia foetida L. seed protein flour (SSPF) was produced by dehulling, defatting, drying, grinding, passing through mesh sieve 240 µ and evaluated its physico- chemical characteristics. The antioxidant activity increases with increasing in concentration of the SSPF. The total polyphenol content was determined by the Folin-Ciocalteu reagent. Amino acid composition by using Biochrom automatic amino acid analyzer and they were detected after post column derivatization with Ninhydrin reagent. The antioxidant activity was determined by DPPH and ferric reducing power methods and storage stability by sorption isotherm method. SSPF was possessed higher contents of protein (40.10%), calcium (58 mg) and phosphorus (1138 mg/100 g). Glutamic acid, arginine, aspartic acid, leucine, lysine, valine and phenylalanine are the major amino acids. The ratio of essential to nonessential amino acids was 0.45. All essential amino acids were higher than the reported amounts for 70 kg person (100 ± 5g SSPF) as per FAO/WHO/UNU requirements. The seed protein flour was rich in polyphenols, which showed considerable antioxidant activity. SDS-PAGE showed nine protein bands, in which five kDa proteins are matching with molecular marker. The antioxidant activity increases with increasing in concentration of the SSPF. The sorption isotherm studies indicated that the SSPF was non-hygroscopic in nature.

Keywords: Chemical composition, Mineral content, Amino acid composition, Antioxidant activity, Sterculia foetida seed protein flour, Sorption isotherm

ABSTRACT

The present investigation involves the Preparation and Characterization of etoposide loaded PCL Composite micropartices on account to control initial burst release. The prepared composite particles were characterized physicochemically for Encapsulation efficiency, Mean particle size, Release kinetic and compared with nanoparticles and simple microparticles prepared by the same double emulsion method. The major objective of the present study is to incorporate a hydrophilic drug etoposide within hydrophobic polymer poly (ε-caprolactone) for the preparation of composite micro particles to minimize initial burst release of the drug which is generally associated with micro and nanoparticles. Micro particles and nanoparticles were prepared by W/O/W emulsion solvent extraction and W/O/W solvent evaporation method respectively using different ratios of drug to polymer (0.1:1, 0.2:1 and 0.4:1). These prepared nanoparticles were further fabricated in micro particles using double emulsion method in ratio of (0.05:1, 0.1:1, 0.2:1).When PCL nanoparticles were encapsulated into the microparticles, there was a large decrease in the burst release again; this decrease is much more marked when p < 0.05. When nanoparticles formulated in to composite micropartices the burst released is suppressed only 50% of the drug was released in 8 hrs. Therefore, the advantage of encapsulating nanoparticles in microparticles (composite microparticles) has been definitely demonstrated for a hydrophilic drug.

Keywords: Ex-Vitro, Microparticles, Nanoparticles

ABSTRACT

The present study was planned to evaluate the effect of Sitopaladi churna & a herbal preparation on cell mediated immunity: by haematological parameters & by phagocytic activity of polymorpho nuclear  (PMN) cells in rats. Effect of Sitopaladi churna (1000 mg/ kg), Decoction of  herbs(10 ml/ kg) containing Embelia ribes seeds, Cymbopogon citratus(lemon grass), Zingiber officinale (ginger), Ocimum Sanctum(tulsi) on cell mediated immunity was evaluated by haematological parameters and by studying phagocytic activity by PMN cells. Both & herbal preparations shown increased cellular immunity as compared to control. Both herbal preparations shown comparable results with Septilin syrup (marketed by Himalaya) which was used as positive control (P>0.05). The study demonstrates that herbal preparations used in this study trigger cell mediated  immunity.

Keywords: Cell mediated immunity, Herbal preparations, Haematological parameters, Sitopaladi churna, Phagocytic activity

ABSTRACT

Grewia asiatica Linn. belonging to family Tiliaceae is commonly known as Phalsa found through out India. It is an important medicinal plant used in inflammation, diabetes, fever, blood disorders, cooling agent, astringent, postural eruption etc. As a herb it is used widely in the Indian traditional system, it was thought worthwhile to undertake the standardization of its aerial parts. Evaluation of the leaves were carried out to determine the effect of various drug extract on number of microbial and fungal strain. Leaves exhibited moderate to significant antibacterial and antifungal activity against all the tested bacterial strains. The chloroform extract exhibited moderate antibacterial and antifungal activity. The petroleum ether extract was devoid of any antibacterial and antifungal activity. While mentioned all the organisms are susceptible to alcoholic as well as  aqueous extracts.

Keywords: Tiliaceae, Cup plate method, Antimicrobial activity, Antifungal activity

ABSTRACT

Two simple, rapid and inexpensive methods based on visible spectrophotometry have been developed for the determination of felodipine in pure form and in dosage forms with two acidic dyes [Bromophenol Blue (BPB) and Bromothymol Blue (BTB)] as the reagents. The proposed methods were based on the formation of ion-pair color complexes between the drug and the two acidic dyes in an acidic buffer. The ion-pair complexes formed, which has an absorption maximum at 420 and 424nm, and were quantitatively extracted into chloroform. All experimental variables for both the proposed methods were studied and optimized. Statistical analysis of the experimental results indicated that the proposed methods were precise and accurate. Excipients used as additives in pharmaceutical formulations did not interfere in the proposed procedures. The proposed procedures were successfully applied to the determination of the bulk drug and its pharmaceutical formulations.

Keywords: Spectrophotometry, Ion-pair color complex, Bromophenol Blue, Bromothymol Blue, pharmaceuticals

ABSTRACT

A series of 6-tetra-O-acetyl-β-D-glucopyranosylimino 2 dimethylamino-4 aryl/alkyl imino-1,4,5,6 tetrahydro-1,3,5 triazines have been synthesized by the interaction of tetra-O-acetyl α-D glucopyranosyl bromide and various 1,3,5 triazines. The latter were synthesized by following the interaction of metformin hydrochloride and N-aryl/alkyl imino isocyanodichloride in chloroform medium. The identities of these new N-glucosylated triazines have been established on the basis of elemental analysis, I.R., NMR and mass spectral studies. The newly synthesized compounds were screened for their antimicrobial and antifungal activities. Some of them showed moderate to less antimicrobial activity.

Keywords: N-glucosylated 1, 3 ,5 triazines, antimicrobial activity.

ABSTRACT

Traditional healing through herbs have been the experienced of many countries since ages, as they were generally whispered to be non toxic natural products. Contemporary medicine is more concern for the cure of diseases but remnants indifferent to health conservation. There is an urgent need to combine the best elements of traditional medicine and modern medicine to improve the health care system of human kind. For the reason that of the rapid progress of herbal drug an increasing need is felt to standardize the herbal products. It is needed to develop the scientific protocols such as SOP and pharmacopoeial standards of the poly herbal drug Majoon-a- Aaradkhurma. Majoon-e-aradkhurma is traditionally used to controls spermatorrhoea and nocturnal emissions and it increases the density of semen and sperm count. The pharmacognostical evaluation comprises of phytochemical screening, physical constants such as ash values, extractive values, heavy metal, pesticide residue and aflatoxin analysis. Study revealed that heavy metals such as lead, cadmium, mercury and arsenic were not detected in the drug. Pesticide residues and aflatoxin were also absent in the drug. The data evolved in the present work help to fix the scientific standards for Majoon-a- Aaradkhurma.

Keywords: Majoon-e-Aradkhurma, Extractive values, Ash values, Heavy metal, Pesticide, Aflatoxin

ABSTRACT

As a site for drug delivery the oral cavity offers advantages over the conventional gastrointestinal route and the parenteral and other alternative routes of drug administration. It provides direct entry into the systemic circulation thereby avoiding the hepatic first pass effect. Verapamil HCl belongs to a drug group of calcium channel antagonists. The oral absorption of the drug from these forms is 90% but its bioavailability approaches only 10–20%, due to a extensive first-pass effect. Here attempt is made to extract mucilage and use as gelling and mucoadhesive agent. The yield of natural mucoadhesive fenugreek extract was 28-29 percent. Fenugreek mucilage shows synergistic effect with xanthan gum and provide higher viscosity. Fenugreek is used with xanthan gum in the selected ratio of 2.5:1. Different parameters were evaluated like % yield of fenugreek, viscosity, gel strength, mucoadhesive study, in-vitro diffusion study, ex-vivo permeation study and differential scanning calorimetry. The mucosal permeation of drug from the formulation was evaluated using Franz diffusion cell, goat buccal mucosa as semi-permeable membrane. The amount of the drug released was determined by evaluating drug diffused through the membrane by using UV- spectrophotometry. The verapamil HCl release was sustained up to 6 hrs by optimizing concentration of fenugreek and xanthan gum.

Keywords: Fenugreek mucilage, Verapamil HCl, Buccal, Mucoadhesion, Xanthan gum

ABSTRACT

A simple, precise, accurate and stability-indicating reverse phase high performance liquid chromatography (RP-HPLC) method is developed for estimation of Isosorbide 5-Mononitrate in bulk drug and tablet dosage form. The method employed, with reverse phase phenomenex^® Luna 5µ C18 (2) 100A (250 × 4.60 mm) column in an isocratic mode, with mobile phase of methanol: water: acetonitrile in the ratio 55:28:17 (%v/v/v). The flow rate was 1.0 ml/min and effluent was monitored at 217 nm. Retention time was found to be 4.391±0.015 min. The method was validated in terms of linearity, accuracy, precision, limit of detection (LOD), limit of quantification (LOQ) etc. in accordance with ICH guidelines. Linear regression analysis data for the calibration plot showed that there was good linear relationship between response and concentration in the range of 1- 9 µg/ml respectively. The LOD and LOQ values for were found to be 2.5 and 10 ng/ml respectively. No chromatographic interference from tablet excipients and degradants were found. The proposed method was successfully used for estimation of Isosorbide 5-Mononitrate in tablet dosage form.

Keywords: Isosorbide 5-mononitrate, RP-HPLC, Validation, Stability-indicating method.

ABSTRACT

A total of 25 different types of actinomycetes were isolated from the soils of marine sediment soil. All the isolated actinomycetes were characterized and identified based on the morphological, biochemical, cultural characteristics. Both primary and secondary screening methods were used to screen actinomycetes for antibacterial activity. The result of the screening revealed that all the isolates were against bacterial culture. But the best strain was found to be Streptomyces sp as they showed broad spectrum activity with big zone of inhibition, even though the strain Staphylococcus and Streptomyces sp showed augmented antibacterial activity against all the tested human bacterial pathogens. Comparatively, when they were treated with pathogenic microorganisms all the isolates produced to maximum and minimum zone of inhibition with its responsible broad spectrum of bioactivity. Moreover, LAM-4 and LAM-11 strains were clearly showed significant activity against both Staphylococcus aureus and S. agaricus. From the HPLC peaks which had antimicrobial activity of Streptomyces sp was identified to be at 3.296. This is similar to oxohexaene antibiotic whereas, the antimicrobial compound of Streptomyces sp3 showed a retention time of 3.233 on HPLC, this peak was similar to Cephalexin. From the results highlight the most of the isolates inhibited growth of the Gram negative bacteria tested. All the antibiotic producing actinomycetes were isolated at different temperatures from marine soil. These microorganisms might have potential to produce a number of the most important medicines constantly developed.

Key words- Actinomycetes, pathogenic organisms, HPLC

ABSTRACT

Alleles A1 and A2 of the Bos taurus CSN2 gene are the most common in a number of dairy cattle breeds. A genetic variant of the bovine β-casein gene includes A1 and B which encodes a histidine residue at codon 67, resulting in potential liberation of a bioactive peptide, β-casomorphin, upon digestion. This is an opium family substance, and has been associated with a large number of clinical implications in humans. Study includes amplification of bovine β-casein gene and further differentiation of variants A1 and A2 beta casein in cows. Conventional PCR was done to amplify β-casein gene in three hundred and one specimens. Further eighty amplicons were sent for sequencing. From the sequenced data, 24 were A2 homozygous (A2A2), 11were A1 homozygous (A1A1) and 37 heterozygous (A1A2). Allele discrimination in cows will be significant for the farmers, breeding programmes as well as for dairy industries as the milk variant determination will predict the outcome of the beta casein variants which are of utmost clinical relevance.

Keywords: Cattle, β-Casein, Genetic Polymorphism, Polymerase Chain Reaction, opioid peptides, β-casomorphin.

ABSTRACT

A simple precise, rapid, accurate and sensitive non-aqueous potentiometric titration method was developed for quantitative determination of oxolamine citrate from pharmaceutical dosage form. The titration was carried out using standardized 0.1 N perchloric acid. The proposed method was found to be precise with % RSD <1 (n = 6). The method showed strict linearity (r² > 0.99 ) between 20 % to 100 % of 100 mg of drug substance weight. The percentage recovery of oxolamine citrate in the optimized method was between 99.773 to 101.229 %. The method is also found to be rugged when checked by different analysts and using different lots of reagents and different makes of titrators.

Keywords: Oxolamine citrate, perchloric acid , potassium hydrogen phthalate ,glacial acetic acid.

ABSTRACT

A simple, rapid, precise, and economical spectrophotometric method has been developed for quantitative analysis of Rilpivirine hydrochloride (RILH) in manufactured tablet formulations. The initial stock solution of RILH was prepared in dimethyl formamide: acetonitrile solvent and subsequent dilution were done in acetonitrile. The standard solution of RILH in acetonitrile showed absorption maxima at 281.6 nm. The drug obeyed Beer–Lambert’s law in the concentration range of 1–16 μg/mL with coefficient of correlation (R²) was 0.9999. It showed coefficient of variation below 2 % in intra-run and inter-run precision.  The results of analysis have been validated as per ICH guidelines. The method can be adopted in routine analysis of RILH in bulk and tablet dosage form and it involves relatively low cost solvents and no complex extraction techniques.

Keywords: ICH guidelines, Method validation, Rilpivirine Hydrochloride, UV Spectrophotometric

ABSTRACT

The non-aqueous potentiometric determination of pharmaceutically potent drug aspirin by using isopropyl alcohol as the solvent and alcoholic KOH as the titrant has been carried out. The effect of solvent and concentration on potentiometric determination of aspirin has been studied followed by the estimation of aspirin in single component tablets. The titrations were carried out using glass and calomel electrode pair. The method was found to be convenient for assay of aspirin and results obtained are comparable with those obtained by IP method. Solvent isopropyl alcohol gives much more accurate result as compare to other solvents with minimum % error. In study of effect of concentration, the results obtained are more accurate with positive errors at low concentration whereas, negative errors at high concentration. The error is just +0.11% when 1.804 mg of aspirin was titrated. Confidence level of weight titrated and weight found in respect of aspirin is 0.46 which is statistically non significant.

Keywords: Non-aqueous, potentiometric determination, aspirin

ABSTRACT

In the present study, a series of novel quinazoline derivatives were synthesized by condensation with different aromatic amines via cyclized intermediate 2-phenyl-1, 3-benzoxazin-4-one.The chemical structures were confirmed by means of IR, H¹ NMR. These compounds were screened for anti-bacterial (Staphylococcus aureus ATCC-9144, Escherichia coli ATCC-25922, activities by paper disc diffusion technique. The potency of antibiotic content in samples can be determined by chemical, physical or biological means. An assay was performed to determine the ability of an antibiotic to kill or inhibit the growth of living microorganism. The inhibition of microbial growth under standardized conditions may be utilized for demonstrating the therapeutic efficacy of drugs. Microorganisms employed in biological assay were of various types of bacteria for amino acid & antibiotics, fungi for vitamins & trace elements. The synthesized compounds were evaluated for anti-bacterial activity. Some of these synthesized compounds show significant anti-bacterial activity.

Keywords: Quinazoline derivatives, Aromatic amines, Paper Disc Diffusion Technique, Anti-bacterial activity.

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Gatifloxacin sesquihydrate and Prednisolone Acetate in  mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent.Gatifloxacin sesquihydrate has absorbance maxima at 293 nm and Prednisolone Acetate has absorbance maxima at 243 nm in methanol. The linearity was obtained in the concentration range of 2-12 μg/ml and 2-24 μg/ml for Gatifloxacin sesquihydrate and Prednisolone Acetate, respectively. The concentrations of the drugs were determined by using simultaneous equations at both the wavelengths. The mean recovery was 99.19 ± 0.22 and 99.64 ± 0.37 for Gatifloxacin sesquihydrate and Prednisolone Acetate, respectively. The method was successfully applied to laboratory prepared synthetic mixture because no interference from the mixture excipients was found. The suitability of this method for the quantitative determination of Gatifloxacin sesquihydrate and Prednisolone Acetate was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of  Gatifloxacin sesquihydrate and Prednisolone Acetate in combination. The results of analysis have been validated statistically and by recovery studies. 

Keywords: Gatifloxacin sesquihydrate, Prednisolone Acetate, Recovery, Simultaneous equations method, Validation.

ABSTRACT

The purpose of this research was to introduce and evaluate natural excipients (soy polysaccharides, CP) that have versatile property in the orally disintegrating tablets. The main objective of this work was to assess the excipient for its activity as a disintegrant and compare its properties with other synthetic superdisintegrants. Orodispersible tablets containing a model drug, Lornoxicam was prepared using different ratios of banana powder, soy polysaccharides, crosspovidone, croscarmellose sodium (CCS) and sodium starch glycollate (SSG) as disintegrants. The prepared tablets were evaluated for their physiochemical properties like wetting time, water absorption ratio, dispersion time, disintegration time and drug release studies. It was observed that the results obtained from formulations containing the soy polysaccharides and CP as superdisintegrant showed a better profile in comparison to banana powder, CCS and SSG. Disintegration time of the formulations varied from 15 to 36s for all the formulations. Dissolution studies suggested that the drug dissolution from formulations containing soy polysaccharides was more than 90% within 15min in comparison to 82% and 85% for CCS and SSG respectively. Stability studies of the prepared tablets showed non-significant drug loss and drug release. Hence, it was concluded that banana powder can be used as a natural disintegrant in orodispersible tablets. The excipient being available naturally and having nutritional benefits adds value to the formulation and can be utilized as an effective excipient in preparing tablets with less cost.

Keywords: Orodispersible tablet, soy polysaccharides, banana powder, dispersion time, dissolution studies.

ABSTRACT

Cadmium compounds are serious pollutants of aquatic environment because of their environmental persistence and ability to be accumulated by aquatic organisms. The present research was designed to study the sub lethal concentration of CdCl₂ on some biochemical parameters of Clarias batrachus. The fishes selected for the experiment were 20 in number, arranged in 4 groups, 5 in each group. The average length and weight of Clarias batrachus was 11 inches and 255 gms respectively. One of the 4 groups was kept as control and the rest three  groups were experimental ones exposed to 2.5 mg/litre sub lethal concentration of CdCl₂ for the time period of 15, 30 and 45 days respectively. After exposure, it was observed on one hand that the glucose level showed a significant decrease and on the other hand an increase was observed in total protein, cholesterol, albumin and globulin. The result of recent research work clearly indicates that the cadmium disturbs the energy metabolism of Clarias batrachus by and large. This in future will lead to death of fish species and finally affects the whole population of the individual organism.

Keywords: Clarias batrachus, Cadmium, Toxicity, Biochemical parameters, Aquatic organisms

ABSTRACT

Carvedilol is a non selective α and β receptor blocker which undergoes extensive hepatic first pass metabolism by liver and has poor oral bioavailability of 25% - 30%. In the present investigation Carvedilol was formulated as a bilayered buccal adhesive tablets in order to avoid the first-pass effect and decrease the drug loss using two different natural polymers and excipients. Six formulations were made using different concentrations (17%w/w, 35%w/w, 53%w/w) of Pectin and Guar gum. Formulation F5 was selected for further studies of permeability. Three concentrations of SLS (1%, 1.5% & 2%w/w) was used to study the effect of permeation enhancer and improve the permeability of drug. The formulations were tested for % weight variation, hardness, Friability, % Drug content, in-vitro drug release, surface pH, Swelling index and Mucoadhesive strength. Mucoadhesive strength was determined by the modified balance method in grams and was found to be between 23.75±0.332gm to 60.89±0.134gm and Surface pH was found to be 7. In-vitro release studies revealed that as polymer concentration increases from 17% to 53%w/w, rate of drug release was retarded and the data was fitted into pharmacokinetic models. Among all other formulations, formulations (F5) containing 35%w/w Guar gum were found to be best as the release was retarded upto 8 hours and they have good mucoadhesive strength and they follow zero order with non-fickian diffusion mechanism. Formulation F9 (2%w/w SLS) shows more permeability of drug (34%) compared to other formulations.

Keywords: Carvedilol, Pectin, Guar gum and Sodium lauryl sulphate(SLS).

ABSTRACT

The objective of this work was to develop and validate simple, rapid and accurate chromatographic methods (A and B) for determination of Desvenlafaxine succinate in solid dosage form. In method A - RP-HPLC method was based on Reversed Phase High Performance Liquid Chromatography, on ODS C₁₈ RP column (150 mm × 4.6 mm i.d., 5 µ), using Methanol : 50 mM Phosphate buffer (pH 8.0): Acetonitrile (50:40:10 % v/v) as the mobile phase, at a flow rate of 1 mL/min at ambient temperature. Quantification was achieved by UV detection at 225 nm over a concentration range of 5-25 µg/mL for Desvenlafaxine succinate. The mean retention time for Desvenlafaxine succinate was found to be 4.80 min. The amount of Desvenlafaxine succinate estimated as percentage label claim was found to be 99.83 ± 1.1093. In method B - HPTLC method was based on TLC separation of the drug using silica gel 60 F 254 aluminium sheets and Chloroform : Methanol : Water (60:30:10 v/v/v) as mobile phase. Detection was carried out at 226 nm over the concentration of 1 - 3.5 µg/mL Desvenlafaxine Succinate. The mean R_f value of Desvenlafaxine succinate was found to be 0.63. The amount of Desvenlafaxine succinate was estimated as percentage label claim found to be 101.57 ± 0.92668. Both of these methods were found to be simple, precise, accurate, selective and could be successfully applied for determination of pure laboratory prepared mixture and tablet.

Key words: RP-HPLC, HPTLC, Desvenlafaxine succinate, marketed formulation.

ABSTRACT

Phyllanthus amarus  S & T (Family: Euphorbeaceae) is an important medicinal plant. It is probably native to America but found throughout to India and almost all tropical countries.  Widespread throughout the tropics and subtropics in sandy regions as a weed in cultivated and waste lands. Whole plant is used as bitter, antipyretic, antiseptic, astringent, cooling agent,diuretic, in dropsy, gastrointestinal troubles like colic, diarrohea, dysentery, other genital disease and in jaundice. It also alleviates the anorexia and also used as a diuretic in dropsial affections, gonorrhea and other problems of genitor urinary tract. Whole plant material was subjected to macro-microscopic, physico-chemical, preliminary phytochemical, TLC to fix the quality standards of this drug. The experiment has resulted a set of diagnostic characters essential for its standardization. The experiments yielded a set of diagnostic characters comparable with standard literatures. This study would be useful for standardization of this raw drug derived from whole plant of Phyllanthus amarus S & T.

Keywords:  Phyllanthus amarus, Whole plant, Physicochemical parameters, Standardization

ABSTRACT

Depression is a heterogeneous disorder that affects a person’s mood, physical health and behaviour. Despite progress in pharmacotherapy, in majority of patients depression goes undiagnosed and untreated. Ayurveda, the Indian traditional system of medicine, mentions a number of single and compound drug formulations of plant origin that are used in the treatment of psychiatric disorders. Tribulus terrestris (Gokshura) is used in Indian and Chinese system of medicine for treating various male reproductive disorders. The present study was undertaken to evaluate the antidepressant potential of acute and chronic administration of Tribulus terrestris in forced swim test (FST) and tail suspension test (TST). Inbred Swiss Albino mice weighing 20-30g were used in the study. The vehicle distilled water ( (10ml/kg, p.o), imipramine (20mg/kg, p.o) and Tribulus terrestris  (100mg/kg, 200mg/kg, 400mg/kg, p.o. respectively) were administered 1hour prior to acute study. In chronic study, all drugs were given once a day for 10 days and the last dose was given 1hour before the experiment. Duration of immobility was noted in both the models. In our study, both imipramine and Tribulus terrestris significantly reduced the duration of immobility in both experimental models as compared to the animals in the control group. The antidepressant activity of Tribulus terrestris was comparable to that of standard drug imipramine. The results of the present study showed significant antidepressant activity of Tribulus terrestrisin animal models of depression

Keywords:Tribulus terrestris, Antidepressant, Forced swim test, Tail suspension test

ABSTRACT

Steroids are widely prescribed and used by practitioners due to powerful anti-inflammatory and immunosuppressive actions¹. So, care should be exercised in the rational selection of steroids^2. Hence this study was carried out to asses the prescribing pattern of steroid usage. This was a prospective, observational and an intervention study.The patient data was collected in well design data collection form and subjected to descriptive statistical analysis 165 cases assessments shows, the mean age of inpatient & out patient was 56.58/55.10 years and male patients were more in both the groups. The occupational results showed Farmers and businessman’s were more followed by House wife. 52.9% IP - 54.1% OP were alcoholics, 58.7% IP - 73.8% OP were smokers. Steroids were used more in respiratory diseases like COPD [18.2% IP /85.2% OP] , Acute bronchitis  [24.0% inpatients] and Bronchial Asthma [11.5% IP/ 9.9%OP]. Among steroids, Budesonide [64.4%IP/ 85.2%OP ] was frequently used followed by Prednisolone [(5.7%IP/ 14.8%OP ], and Dexamethasone 6(5.7%) and Hydrocortisone 25 (24.2%) in IP. 50.0% Nebulization forms were  used widely, followed by Injection(29.8%), 85.2%  OP was  used Inhalers, 55.8% IP& 14.8% (OP) prescriptions had steroidal drug interactions.  81.8% inpatients were counseled correct use of steroids. The mean hospital stay of inpatients was 6.11 with SD of 4.86 days. This study showed that the prescribing of steroids was rational &. Patient counseling services were helped them to understand their therapy, disease. Even though the drug interactions observed with the steroids, benefits of therapy were noticed more.

Keywords: Prescription pattern, Drug interactions (DI), Rational drug usage (RDU), IP; Inpatient, OP; Out patients

ABSTRACT

Solid dispersion of Oxcarbazepine (OXC) was prepared by hot melt extrusion of OXC with hydrophilic polymer. The main objective was to explore the potential of Hot Melt Extrusion technique (HME) as an industrial scalable green technique for the preparation of solid dispersion and therefore enhancement of dissolution of poorly soluble drug. Polymer for extrusion was selected on the basis of solubility parameters and glass transition (T_g). OXC solid dispersion was prepared using Kollidon VA 64 and Soluplus as hydrophilic carrier. OXC and polymer was mixed in different ratio and extrudates were evaluated for appearance, DSC, PXRD, flow property and dissolution characteristics. DSC and PXRD studies revealed the significant reduction in crystallinity of OXC. OXC-kollidon VA 64 extrudates have good flow property having angle of repose 29° and carr’s index 11.2 and good compressibility with hardness 5-6 kg/cm². Particle size of extrudates exhibited significant effect on disintegration time and dissolution. OXC release was found to be complete within 45 min from tablets of OXC hot melt extrudates while plain OXC showed just 39 % release. Solid dispersion of OXC was successfully developed using HME technology followed by formulating it into directly compressible tablets.

Keywords: Hot melt extrusion, Oxacarbazepine, Solid dispersion, Solubility enhancement, Glass transition temperature, Solubility parameter

ABSTRACT

Solubilization of poorly water‐soluble drugs has been a very important issue in screening studies of new chemical entities as well as formulation research. Hydrotropy is one of the solubility enhancement methods for aqueous solubility of poorly water-soluble compounds. Cefixime HCl is poorly water soluble drug which shows good aqueous solubility in 2 M Sodium Benzoate solution. For quantitative estimation of Cefixime HCl in bulk and tablet dosage form, a titrimetric analytical method and spectrophotometric methods has been developed using 2 M Sodium Benzoate as a hydrotrope. Hydrotropic solution was employed to solubilize a practically water insoluble drug, Cefixime HCl in bulk and tablet dosage form to carry out titrimetric and spectrophotometric analysis precluding the use of organic solvents. The bulk containing Cefixime HCl was analyzed successfully. Statistical data proved accuracy, reproducibility and the precision of the proposed method. The presence of hydrotropic agent Sodium Benzoate did not interfere in the analysis. The proposed methods are new, simple, accurate, reproducible and eco-friendly.

Keywords: Cefixime HCl;  Sodium Benzoate, Hydrotropy, Titrimetry, Spectrophotometry .

ABSTRACT

A New simple, precise, accurate and rapid RP-HPLC method was proposed for determination of Dorzolamide hydrochloride from pure and its dosage form. A Symmetry Hypersil C₁₈   (250 × 4.6mm, 5µ) column in isocratic mode with mobile phase phosphate buffer (pH 6.2): Acetonitrile (60:40) at a flow rate of 1ml/min. The effluent was monitored at 254nm. The retention time was 3.337min for Dorzolamide hydrochloride. The linearity range was found to be 20 – 120 µg/ml. The developed method was validated for parameters like specificity, accuracy, ruggedness and robustness and ascertained values were found to be within limits. The method has significant advantages in terms of shorter analysis time, selectivity and accuracy then previously reported method and indicates that the method can be considered suitable for carrying out quality control &routine determination of Dorzolamide hydrochloride in bulk and pharmaceutical dosage form.

Keywords: Dorzolamide hydrochloride, RP-HPLC, isocratic, Validation.

ABSTRACT

Acne is a disease appearing simple but chronic in nature with multiple causative factors like bacteria, inflammation, hormones etc. The present study was conducted to formulate and evaluate the topical anti acne formulation of coriander aqueous extract. The antibacterial activity of aqueous extract against Propionibacterium acne (P. acne) and Staphylococcus epidermidis(S. epidermidis)  was investigated using disc diffusion method and minimum inhibitory concentration was determined by agar dilution method. The results showed that coriander aqueous extract showed the MIC values of 1.7 mg/ml and 2.1 mg/ml against P.acne and S. epidermidis respectively. The zone of inhibition exhibited by the aqueous extract was 21.5±1.4mm and 20.6±1.09mm against P.acne and S. epidermidis respectively. The topical formulations were developed using menthol as the penetration enhancer and tested for physical parameters, drug content uniformity, spreadibility, extrudability and in-vitro diffusion. It was reveled from the results that all the formulations showed the increased zone of inhibition for both of the bacteria. The formulations with the addition of penetration enhancer showed the increased drug content as well as the invitro release which increased with increase in the concentration of menthol. The formulation Fa₁₁ showed the drug content (97.9%), in-vitro- diffusion (96.8%) and maximum stability among all the formulations. The optimized formulation showed the thixotropic behavior and first order release rate.

Keywords: acne vulgaris, antibacterial activity, coriander, penetration enhancer, in-vitro activity.

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical Q-absorbance ratio method for the simultaneous determination of ibuprofen and chlorzoxazone in bulk and synthetic mixture. 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. Ibuprofen and Chlorzoxazone show an isoabsorptive point at 227 nm in methanol. The second wavelength used is 221 nm, which is the λ-max of Ibuprofen in methanol. The linearity was obtained in the concentration range of 2-20 μg/ml for both Ibuprofen and Chlorzoxazone. The concentrations of the drugs were determined by using ratio of absorbances at isoabsorptive point and at the λ-max of Ibuprofen. The method was successfully applied for the determination of these two drugs in synthetic mixture. No interference was observed from excipients present in the synthetic mixture. The suitability of this method for the quantitative determination of Ibuprofen and Chlorzoxazone was proved by validation. The proposed method was found to be simple and sensitive for the routine analysis of these two drugs in synthetic mixture. The results of analysis have been validated statistically and by recovery studies. 

Keywords: Ibuprofen, Chlorzoxazone, Recovery, Absorbance ratio method, Isoabsorptive point, Validation.

ABSTRACT

Inflammation is a complex biological response of vascular tissues to harmful stimuli. The stimulus may be thermal (heat or cold), chemical (foreign substances, foreign organisms, drugs), or mechanical (trauma). Anti-inflammatory agents are the agents which relieves the inflammation. Amino acids L-tyrosine was refluxed in presence of thionyl chloride and methanol for 8 hrs to form its methyl ester hydrochloride(a). Compound (a) and taurine were refluxed with Salicylic acid in 30 % NaOH solution for 2 hrs and neutralized with conc. hydrochloric acid to precipitate target compounds (b, c). These compounds were characterized on basis of melting point, TLC (R_f value), IR and ¹H NMR spectra and evaluated for analgesic and anti-inflammatory activity. Target compound (b) was found to be most active with 96.3 % protection for analgesic and anti-inflammatory activity.

Keywords: Salicylic acid, Amino acids, Analgesic, Anti-inflammatory.

ABSTRACT

A novel, simple, rapid and stability-indicating reversed-phase ultra performance liquid chromatographic method was developed and subsequently validated for quantitation of Emtricitabine (ECB) from drug substance matrix. The separation was achieved in less than 2.0 minutes on Waters ACQUITY UPLC BEH C₁₈ (50 x 2.1) mm, 1.7µm column in isocratic mode with flow rate 0.25 mL/min. Mobile phase used was 0.015 M potassium dihydrogen phosphate buffer pH 2.2 and acetonitrile in ratio 75:25 v/v. Detection was carried out at the maximum wavelength of 284 nm using a photodiode array detector. The retention time of emtricitabine was 1.2 minutes. A forced degradation study was performed. Specificity of the method was established on drug substance by hydrolytic and oxidative stress conditions. Validation of analytical method was carried out as per the current ICH guidelines for linearity, recovery, precision, limit of detection, limit of quantification and robustness parameters.

Keywords: Emtricitabine (ECB), Ultra Performance Liquid Chromatography, Antiretroviral, Stability indicating, ICH

ABSTRACT

4-(4′-chlorophenyl)-thiazol-2-carbohydrazide(2) obtained from Ethyl-4-(4′-chloro phenyl)-thiazol-2-carboxylate(1) by the treatment with hydrazine hydrate. The synthesis of Potassium-[4-(4′-chlorophenyl)-thiazol]-2-dithiocarbazinate(3) was performed from reaction of 2 with alcoholic potassium hydroxide and carbon disulphide. Moreover 4-amino-5-(4′-(4′′-chlorophenyl)thiazol-2′-yl)-3-mercapto-4H-1,2,4-triazole(4) were obtained by refluxed in the presence of compound 3 and hydrazine hydrate with water. The condensation of 4 with substituted aromatic aldehydes generated the corresponding different triazole Derivatives (5a-m). The structures of the compounds were confirmed by elemental analysis and spectral analysis. Antibacterial activity of the synthesized compounds was evaluated by tube dilution method against two gram positive and two gram negative bacteria using ciprofloxacin as standard.

Keywords: Synthesis, Triazoles, Anti bacterial activity

ABSTRACT

The main aim of present study is to formulation & optimize Gliclazide alginate microspheres by plackett burman’s factorial design. Which offers a flexible and easily controllable process for the manipulating the characteristics of the beads which is important in controlling the release rate and consequently the absorption of Gliclazide from the GIT, variation in polymer, concentration, time of gelation in the external phase were examined systemically for their effects on rate release and entrapment efficiency by Plackett Burman’s factorial design. The swelling behavior strongly depends on the polymer concentration. The result of the study will depends on the release profile of the drug from the formulation. The formulations follows zero order kinetics for the drug release. The in vitro release study indicates that the swelling is the main parameter in controlling the release rate from microcapsules.

Keywords: Ionic gelation, Gliclazide, Plackett Burman’s.

ABSTRACT

A simple, sensitive, accurate and precise high performance thin layer chromatographic method was developed and validated for simultaneous determination of efavirenz (EFA), emtricitabine (EMT) and tenofovir (TEN) in combined tablet formulation and forced degradation studies were performed as per ICH guidelines. Precoated silica gel 60F 254 was used as stationary phase and the mobile phase used was chloroform: methanol (90:10), gives high resolution for each drug. The densitometric evaluation of each drug was carried out at 262 nm. The developed method was simple, accurate and is suitable for analysis of the drugs and degradation products in stability studies of samples.

Keywords: HPTLC; Forced degradation studies; efavirenz (EFA); emtricitabine (EMT); tenofovir (TEN); ICH guidelines.

ABSTRACT

The most common skin disease, acne vulgaris is inflammatory in nature and is caused by bacteria P. acne and S.epidermidis. The present study was carried out to formulate separately the topical anti acne formulations of coriander aqueous extract and its oil using carbopol as gelling agent and to compare them with marketed formulation. The developed formulations were compared for antimicrobial studies, viscosity and spreadibility, kinetics of release, in-vitro diffusion and permeation. The antibacterial study was conducted by well diffusion method. The permeation of the developed formulations was more than that of marketed one. The marketed formulation was found to be less effective than the coriander formulation.

Keywords: acne vulgaris, antibacterial activity, coriander, penetration enhancer, in-vitro activity.

ABSTRACT

A simple, rapid, and precise RP-HPLC method for simultaneous analysis of Losartan potassium and Atorvastatin calcium in bulk and its pharmaceutical formulations has been developed and validated. Atorvastatin was separated from losartan by using Grace Smart Altima C-18 column (25 cm × 4.6 mm, 5-μm) with a mobile phase consisting of acetonitrile: 10mM phosphate buffer (55:45 %v/v, pH 3.0) a flow rate of 1mL/min and detection wavelength at 240 nm. Aceclofenac was used as an internal standard in this method. Losartan, atorvastatin and aceclofenac were eluted with retention times of 4.85 min, 8.31min and 9.51 min respectively. The method was validated for accuracy, precision, linearity and sensitivity in accordance with ICH (Q2B) guidelines and the results of all the validation parameters were found to be within the acceptable limits. The calibration plots were linear over the concentration ranges from 200-30000ng/mL (r² = 0.999) for both the drugs. Accuracy and precision were determined by QC sample covering low, medium, and high concentration levels. Intra and inert-day accuracy were found to be 97.16-102.57% for losartan and 97.01-103.05% for atorvastatin. The limit of quantification was found to be166ng/mL and 179ng/mL for losartan and atorvastain respectively. The method was successfully applied for the assay of the dosage form, recovery of the individual drugs from the combined tablet dosage was found to be >97% for both the drugs. From the results it is suggested that the proposed method is simple, reproducible, accurate and precise.

Keywords: Aceclofenac, Atorvastatin, Losartan, RP-HPLC, Simultaneous estimation, Validation.

ABSTRACT

In the present study Liquisolid preparations of nifedipine were prepared by dissolving the drug in a chosen non-toxic, non-volatile solvent and adsorbing onto carrier materials. Various carrier and coating materials were employed in the study. Avicel PH 101 was used as the carrier material and Aerosil was used as the coating material as conventional liquisolid systems, apart from that novel excipients like Fujicalin^® and Neusilin^® were employed and their effects on the dissolution rate of the drug was studied. The results showed that the solubility of the drug was maximum in polysorbate 20 amongst the selected non volatile solvents i.e. Polyethylene glycol 400, 600, propylene glycol, glycerol and Tween 20. The solution of nifedipine in polysorbate 20 was found to be stable for at least 15 days. It was also found out that Fujicalin^® and Neusilin^® were much better adsorbents as compared to microcrystalline cellulose. Fujicalin^® enhanced the drug release where as Neusilin^® when used as an adsorbent retarded the rate of release. Liquisolid systems in general showed enhanced dissolution profile as compared to their directly compressed counterparts. The prepared liquisolid systems were subjected to tests such as FT-IR spectroscopy, differential scanning calorimetry (DSC) and X-Ray crystallography (PXRD) for evaluating the physiochemical properties of the drug in the liquisolid systems. Differential scanning calorimetry and X-Ray crystallography conclusively proved the loss of crystalline structure of nifedipine in the liquisolid systems, thus confirming the enhanced solubility. The optimized liquisolid compact was then compared with commercially available soft gelatine capsules.

Keywords: Dissolution Modification, Liquisolid, Nifedipine, Neusillin, Fujicalin

ABSTRACT

Hisar district is situated in the Haryana state of India and is endowed with various food plant species promi­nently employed in traditional medicine. The information on medicinal uses of plants is based on the exhaustive interviews with local physicians practicing indigenous system of medicine, village headmen, priests and denizens. The present research highlights useful ethnobotanical information about the uses of plants by the inhabitants of Hisar district of Haryana state. The study may open doors of unexplored medicinal plants to be used in treatments in future.

Keywords: Traditional medicine, ethobotanical information, food plants.

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical derivative spectroscopic method for the simultaneous determination of Pantoprazole and Levosulpiride in pharmaceutical dosage form. In this study a first-derivative spectroscopic method was used for simultaneous determination of pantoprazole and levosulpiride using the zero-crossing technique. The measurements were carried out at wavelengths of 269 and 249 nm for Pantoprazole and Levosulpiride respectively. The method was found to be linear (r2>0.9929) in the range of 10-50 μg/ml for Pantoprazole at 269 (ZCP of Levosulpiride) nm. The linear correlation was obtained (r2>0.9948) in the range of 10-50 μg/ml for Levosulpiride at 249 (ZCP of Pantoprazole) nm. The limit of determination was 0.69 and 0.58 μg/ml for pantoprazole and levosulpiride respectively. The limit of quantification was 2.06 and 1.69 μg/ml. The method was successfully applied for simultaneous determination of Pantoprazole and Levosulpiride in pharmaceutical dosage form.

Keywords: Pantoprazole, Levosulpiride, Derivative spectroscopic method, Zero-crossing point.

ABSTRACT

Accurate, precise, rapid and economical first order derivative spectroscopic method was developed and validated for the estimation of Cefixime and levofloxacin in tablet. The wavelengths selected for quantitation were 289.45 nm for levofloxacin (zero cross for cefixime) and 317.0 nm for cefixime (zero cross for levofloxacin). Linearity for detector response was observed in the concentration range of 2-12 μg/ml for both Cefixime and Levofloxacin using methanol as a solvent with correlation coefficient 0.991 and 0.993 respectively. The proposed method was successfully applied for the simultaneous estimation of both drugs in tablet.

Keywords: Cefixime, levofloxacin, UV specroscopy, method validation, tablet

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Eperisone hydrochloride and Aceclofenac sodium in mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Eperisone hydrochloride has absorbance maxima at 255 nm and Aceclofenac sodium has absorbance maxima at 275 nm in methanol. The linearity was obtained in the concentration range of 4-20 μg/ml and 4-20 μg/ml for Eperisone hydrochloride and Aceclofenac sodium, respectively. The concentrations of both drugs in synthetic mixture were determined by using simultaneous equations. The mean recovery was 100.34 ± 0.27 and 100.64 ± 0.71 for Eperisone hydrochloride and Aceclofenac sodium, respectively. The method was applied for the determination of these drugs in mixture. The suitability of this method for the quantitative determination of Eperisone hydrochloride and Aceclofenac sodium was proved by evaluating different validation parameters. The proposed method was found to be simple and sensitive for the routine estimation of these drugs in combination. The results of analysis have been validated statistically and by recovery studies.  

Keywords: Eperisone hydrochloride, Aceclofenac sodium, Recovery, Simultaneous equations method, Validation.

ABSTRACT

The aim of the present study was to prepare buccoadhesive sustained release tablets of sumatriptan succinate using various permeation enhancers to release the drug for extended period of time with reduction in dosing frequency. In the present work sumatriptan succinate was used as a model drug and interaction studies performed using FTIR spectroscopy and DSC revealed that there was no drug, polymer and permeation enhancer interaction. Fulvic acid was extracted from shilajit by using resins. Fulvic acid was characterized by various spectroscopic techniques. Buccoadhesive sustained release tablets of sumatriptan succinate with various permeation enhancers were prepared by direct compression method using bioadhesive polymers like Carbopol 934 and HPMC K100M. The physical characteristics like surface p^H, swelling index, in vitro mucoadhesion time, in vitro mucoadhesion strength, in vitro drug release study and in vitro permeation study. The in vitro release study showed 99.88%, 99% and 99.40% of drug release with fulvic acid, chitosan and beta cyclodextrin respectively. The permeation study showed 90%, 82% and 78% of drug permeated with fulvic acid, chitosan and beta cyclodextrin respectively. Sumatriptan succinate release from the buccoadhesive system was extended and exhibited a non fickian drug release kinetics approaching to first order as the values of release rate exponent varied between 0. 97 to 0.99 resulting in a regulated and complete release until 8 hours.

Keywords: - Buccal drug delivery system, Sumatriptan succinate, Fulvic acid, In-vitro drug release study, In-vitro permeation study.

ABSTRACT

An accurate, precise and reproducible high performance liquid chromatographic method was developed for quantitative estimation of abacavir, lamivudine and zidovudine simultaneously in tablet dosage forms. Separation of the drugs was achieved within 15.0 min on a Hichrom RP-select B column (250 x 4.6 mm; 5µ) by gradient elution using mixtures of 0.02M ammonium acetate and methanol as the mobile phase. The analytes in the eluate were monitored at 250 nm. The retention times obtained for abacavir, lamivudine and zidovudine were 12.172, 1.884 and 4.378 min respectively. The calibration curves were linear over the range of 25-200 µg/mL for abacavir, 12.5-100 µg/mL for lamivudine and 25-200 µg/mL for zidovudine. The performance of the method was validated according to ICH guidelines. The method was found to be suitable for accurate determination of these drugs in tablet dosage forms without any interference from the excipients or endogenous substances.

Key words: Abacavir, Lamivudine, Zidovudine, Determination, HPLC, Gradient elution.

ABSTRACT

An accurate, precise and reproducible high performance liquid chromatographic method was developed for quantitative estimation of telmisartan in bulk drug samples and tablet dosage forms. Chromatographic separation of the drug was achieved on a Kromasil C18 column (150 x 4.6 mm; 5µ) using a mixture of phosphate buffer (pH 4.0) and acetonitrile (40:60 v/v) as the mobile phase at a flow rate of 1.0 mL/min. Under optimized conditions, the retention time of the drug was found to be 2.887 min. Good detecting sensitivity for the analyte was observed at 224 nm. The quantitation calibration curve for the drug was linear over the range of 20-60 µg/mL. The performance of the proposed method was validated as per ICH guidelines. The method was proved to be suitable for the estimation of telmisartan in tablet dosage forms.

Key words: Telmisartan, Estimation, Tablets, HPLC.

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical Q-absorbance ratio method for the simultaneous determination of diclofenac sodium and eperisone hydrochloride in bulk and synthetic mixture. 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. Eperisone hydrochloride and diclofenac sodium show an isoabsorptive point at 270 nm in methanol. The second wavelength used is 255 nm, which is the λ-max of eperisone hydrochloride in methanol. The linearity was obtained in the concentration range of 2-20 μg/ml for both eperisone hydrochloride and diclofenac sodium. The concentrations of the drugs were determined by using ratio of absorbances at isoabsorptive point and at the λ-max of eperisone hydrochloride. The method was successfully applied to pharmaceutical dosage form because no interference from the synthetic mixture excipients was found. The suitability of this method for the quantitative determination of eperisone hydrochloride and diclofenac sodium was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of eperisone hydrochloride and diclofenac sodium in synthetic mixture or pharmaceutical dosage form. The results of analysis have been validated statistically and by recovery studies. 

Keywords: Diclofenac sodium, Eperisone hydrochloride, Recovery, Absorbance ratio method, Isoabsorptive point, Validation.

ABSTRACT

The increasing search and utilization of phytochemicals for medicinal purposes necessitated this comparative isolation and characterization of the medicinal constituents in aqueous, hydro-methanolic (1:4, v/v), hydro-ethanolic (1:4, v/v) leaf extracts of Cnidoscolus aconitifolius. The extracts were tested for twelve important medicinal constituents. Alkaloids, tannins, saponins, flavonoids, Salkowski’s test were positive though at different strengths in the three extracts. The presence of combined anthraquinons, saponins, free anthraquinones, terpenes and Liberman’s test appeared weak (33.3%) in aqueous and hydro-ethanolic (1:4, v/v) extracts though totally absent in hydro-methanolic (1:4, v/v) extract. Phlobatanins and cyanogenetic glycosides were absent in the three extracts. Hydromethanolic (1:4, v/v) extract contained at least 66.7% alkaloids, tannins, flavonoids, Salkowski’s test and Kellerkillian’s test and these gave cumulative percent – strength of 300.1% compared to aqueous extract that had 233.3% and hydroethanolic  (1:4, v/v) extract that had 200%. The results implied that hydromethanolic (1:4, v/v) extraction yields more medicinal constituents than aqueous and hydroethanolic (1:4, v/v) extractions. Further analysis of these isolated phytomedicinal constituents are recommended to understand the physiological and therapeutic implications of Cnidoscolus aconitifolius utilizations.

Keywords: Cnidoscolus aconitifolius, aqueous, hydro-methanolic, hydro-ethanolic, phytomedicinal constituents

ABSTRACT

An efficient and cost effective micropropagation protocol using MS medium developed for Catharanthus roseus, a commercially important medicinal plant. Shootlets were regenerated from nodal explants of stem through axillary shoot proliferation. The induction of multiple shoots from nodal segments were premier in MS medium supplemented with 0.5 mg/l BAP ± 1mg/l NAA. For rooting, different concentration of IBA were used and maximum rooting was recorded on MS medium with 5 mg/l IBA. The rooted plantlets were hardened initially in culture room conditions and then transferred to misthouse.

Keywords: Micropropagation, shoot proliferation, anti-cancer plant

ABSTRACT

Hydrodistilled volatile oil obtained from the rhizomes of Curcuma oligantha Trimen var. oligantha (Zingiberaceae) was analyzed by GC and GC-MS. The volatile oil was composed mainly of cinnamyl cinnamate (88.0 %), linalool (2.9 %) and α-phellandrene (2,2 %).  Among the nine monoterpenes (6.9 %) present in the oil, the prominent ones were linalool  (2.9%) and α-phellandrene (2.2 %). The oil contained ten sesquiterpenes (2.8 %) comprising mainly (2Z,6E)-farnesyl acetate (1.2%). The aliphatic constituents (2.5 %) were characterized as n-heptadecane, n-octadecanal, n-hexadecanol (1.4 %)  and n- hexadecanoic acid. About 15 components occurred in trace amounts in the oil. The volatile oil and ethanolic extract of the rhizomes showed significant antimicrobial activity.

Keywords: Curcuma oligantha var. oligantha, Rhizomes, Volatile oil composition,    Antimicrobial activity.

ABSTRACT

There appears to be a gap in the awareness level and the life–style practices adopted by youngsters regarding non–communicable diseases. A study was done to  assess  the  awareness, attitude and practices and the gap between awareness and practices adopted by the university students regarding the non-communicable diseases. This cross- sectional descriptive study carried over a period of 3 months from August 2010, involving a cohort of 1067 students, admitted during the first-semester 2010 of a reputed all-India technology university was done to assess their awareness, dietary and exercise behaviors in relation to non–communicable diseases using a predesigned and pre–tested questionnaire. Physical examination of 70 randomly selected students was also done to calculate difference between perceived and actual BMI. Roger’s diffusion of innovation model was used to classify them into different groups. 65.96% responded with majority 79.26% being less than 20years of age.34.04% were laggards.73.6% had a positive family history while 58.2% were aware of non-communicable diseases and 70.9% knew ill effects of excessive body weight on it.62.9% skipped their breakfast and 90.9% consumed fast foods regularly. Only 5.4% consumed fruits and 24.3% consumed milk daily while and only 15.2% engaged in some form of physical activity. The need of the hour is an enabling environment along with innovative strategies with multi-sectoral coordination to address the issue of non-communicable diseases and also bridging the gap between awareness and action in adolescents.

Keywords: Non-communicable diseases, Awareness, Practices, Attitude, Adolescents

ABSTRACT

Bark of Ormosia robusta (Fabaceae) Baker has been investigated for isolation of secondary metabolites and evaluation of bioactivities. Two prenylated isoflavones, Warangalone (1) and Erysenegalensein M (2), along with two triterpenoids, Betulinic acid (3) and Lupeol (4), have been  isolated from the methanolic extract of the bark by using chromatographic analysis. Structures of these compounds were elucidated by extensive spectroscopic analysis and by comparing the data with the published one. This is the first report of isolation of these compounds from this plant. Subsequently the methanolic extract was fractionated with four organic solvents and all the fractions were studied to evaluate their in vitro bioactivities. Significant variance is observed for polyphenol content as well as free radical scavenging activity (4.17 - 270.42 mg of gallic acid equivalent/gm of extract and DPPH IC₅₀ value: 1.21-6.80 μg/ml) depending on the nature of the solvent partitioned with. The results of the brine shrimp lethality bioassay (LC₅₀ value: 1.49 -33.15 μg/ml) indicate that the plant possesses cytotoxic principal and have considerable toxic potencies.

Keywords: Ormosia robusta, Fabaceae, Isoflavones, Triterpenoids 

ABSTRACT

Osmotic systems use the principle of osmosis as delivery force to deliver the drug from the system, and the release rate is unaffected by the body’s pH and other physiological and gastrointestinal factors. Osmotic tablet of lornoxicam is prepared successfully to deliver drug in controlled release form for once day therapy in arthritis by overcoming all the side effect and enhancing bioavailability. The objective of the present work was to design osmotically driven oral drug delivery system containing Lornoxicam as an active ingredient and evaluate the effect of various membranes( microporous and semipermiable) on release of drug from osmotic tablet. Core tablet of lornoxicam is prepared, coated with cellulose acetate (39.8 D.S.) in which batch 6b (semipermiable) give the maximum of 91.04% release from osmotic tablet of lornoxicam in control passion as compare to other(microporous membrane coated batches.

Keywords: Osmotic tablet, Lornoxicam, NSAID’s, oral osmotic table, cellulose acetate.

ABSTRACT

The objective of this study was to develop pH independent immediate release (IR) tablet formulation of Glipizide (GPZ) incorporating β-cyclodextrin (β-CD) and a ternary agent produced by high energy air jet milling complexation technique. GPZ (pKa of 5.9) is poorly water soluble (3.9µgm/ml) exhibiting pH dependent solubility (1.1µgm/ml at pH 2.0 and 26.6 µgm/ml at pH 6.8) owing to which it demonstrates dissolution rate limited absorption and bioavailability. Several complexation techniques involving formation of binary and ternary complexes were evaluated for achieving pH independent release of GPZ. Ternary complex involving GPZ:β-CD: Arginine (1:2:1) prepared using high energy air jet milling was found to be most promising in terms of significant enhancement in solubility, further attaining pH independent dissolution. Molecular modelling (MM) was carried out in order to understand the GPZ:β-CD orientation and GPZ group interactions with the cyclodextrin cavities. Molecular modelling suggested interaction of cyclohexyl and methylpyrazinecarboxamido groups of GPZ with the cyclodextrin cavities and favorability of head to tell (HT) orientation due to its minimum interaction energy. XRD and DSC study showed partial amorphization of GPZ. Scanning electron microscopy (SEM) studies revealed formation of new solid phase of ternary complex indicating partial amorphization. Tablets prepared using optimized ternary complex of GPZ showed immediate and pH independent drug release as compared to marketed tablet formulation and plain drug.

Keywords: Glipizide, Immediate release, β-Cyclodextrin, Ternary complex, pH independent

ABSTRACT

The research illuminates DHFR from Pneumocystis jiroveci as a newly potential drug target against pneumonia. P. jiroveci DHFR sequence Q9UUP5 was obtained from Swiss-Prot database and deployed for 3-dimensional structure prediction. Sequence similarity templates searching found between P.j DHFR against 1CD2, 1VJ3 and 1DR1 paved the modeling with high confidence. The superimposition of the predicted template structures revealed the sequence identity of more than 30% and  RMSD values of 4vs.1, 4vs.2, 4vs.3 and 4vs.5 and RMSD values 0.094, 0.093, 0.094 and 0.108 respectively; it comes under the expected range of <2Ȧ. The structure showed overall conservation domains involved in binding affinity, energy minimization value, as well as inter-subunit interactions. Our results provided a basis of structural modeling (threading), energy minimization, RMSD value, structural validation and evaluation, to compare the overall structure and functional amino acids dependent on P.j DHFR in Pneumocystis. Further analysis to show the differences found between the inter and intra species of P.j DHFR is a leeway to design inhibitors targeted specifically against Pneumocystis jiroveci pneumonia (PJP).

Keywords: Threading, RMSD value, Templates, Superimposition and Pneumonia.

Abbreviations: Pneumocystis carinii Pneumonia (PCP), Pneumocystis jiroveci Pneumonia (PJP), Dihydrofolate reductase (DHFR), Root Mean Square Deviation (RMSD).

ABSTRACT

The objective of the current study was to develop and optimize an orally disintegrating tablet formulation of Metoprolol tartrate which is an effective drug in the treatment of hypertension. Metoprolol tartrate orally disintegrating tablets were prepared by direct compression method using different ingredients such as Mannitol, Microcrystalline cellulose, Aspartame, Crospovidone, Sodium starch glycolate, Croscarmellose sodium, Powder flavours Strawberry, peppermint & orange, Colloidal silicon dioxide and Magnesium stearate. Tablets were evaluated for the physical properties, out of which disintegration time and wetting time were considered as responses in a 3² full factorial experimental plan. Results were statistically examined using design expert software and polynomial mathematical equations; found to be statistically significant (p<0.05) for disintegration time and wetting time data. The obtained results were used to generate optimized overlay plot. The physical data from the numerical optimization were verified and found to be very close to those predicted from the regression analysis. Accelerated stability study was also performed on the optimum formulation. All results were in accordance with the requirements of a orally disintegrating tablet.

Keywords: Metoprolol tartrate; orally disintegrating tablet; 3² full factorial design; Optimization

ABSTRACT

The present work was aimed to prepare respirable slow release formulation for isoniazid by spray drying method using hydrophilic carrier, chitosan. The chitosan microspheres were crosslinked with glutaraldehyde to modify release characteristics. Microspheres were prepared and evaluated for % yield, drug loading, moisture content, morphological characteristics, particle size, tapped densities, in vitro drug release, in vitro aerosolization and pharmacokinetic parameters. The scanning electron microscopy revealed that microspheres produced were spherical shaped with slight rough surface. The drug loading efficiency of microspheres showed drug loading efficiency was in the range of 84.44 % to 98.24 %. The in-vitro drug deposition revealed that mass median aerodynamic diameter of crosslinked chitosan microspheres (2.82 µm) was better than the uncrosslinked chitosan microspheres (3.85μm). The complete drug release was seen with uncrosslinked microspheres in two hour while crosslinked chitosan microspheres showed sustained drug release for more than 12 hrs. All the formulation batches showed Carr’s index in the range of 28.7 to 34.3 %. The fine particle fraction for crosslinked chitosan microspheres was found to be 69.1%. Pharmacokinetic differ among the free, crosslinked and uncrosslinked formulations. The crosslinked chitosan microspheres showed sustained drug release lasted for more than 3 days with half life of 31.67 hrs. In vitro and in vivo evaluation studies suggested that chitosan microspheres prepared with spray drying method showed promising aerosol properties having potential to use as sustained drug release formulation for isoniazid as inhalable microparticles. 

Keywords: Microspheres, Isoniazid, hydrophilic carrier, dry powder inhalation, Sustained drug release.

ABSTRACT

Complex of Carboxymethyl cellulose (CMC) sodium salt and β-cyclodextrin (β-CD) were evaluated as sustained release polymers. Diclofenac sodium (DS), CMC sodium salt and β-CD were taken for the preparation of spray dried sustained release microparticles in the different ratio of 1: 0.125:0.125, 1:0.188:0.187 and 1: 0.25: 0.25 (wt/wt) respectively. The DS loaded microparticles were evaluated for particle size, surface morphology by atomic force microscopy (AFM), structural interaction by Fourier transform infrared spectroscopy (FTIR) and thermal characterization by differential scanning calorimetry(DSC). These microparticles further formulated into the tablet dosage form and evaluated for different parameters. Several kinetic models were employed to evaluate the possible changes in the release mechanism. The drug: polymer ratio of 1:0.25:0.25 shows better result of sustained release than the other ratios. The particle size of the optimized microparticles was found to be in the range of 300 nm to 5 µm. FTIR and DSC result reveals the complex formation between DS, CMC sodium and β-CD. X-ray diffraction results indicated that the degree of crystallinity was reduced and most of the drug existed in amorphous state. . The reported method is easy and reproducible and can be used for the batch scale production.

Keywords: Drug, Polymer, Micro particles, Spray-drying, Encapsulation, etc.

ABSTRACT

The study was designed to investigate the anti-inflammatory activity of methanol extract of fruit of Coccinia indica (cucurbitaceae) (MECI) was evaluated against several models of inflammation in rats. Inflammation was induced by subplanter injection into right hind paws of rats by injecting 1%w/v of carrageenan, histamine and dextran solution individually in each groups and antiinflammatory action of methanolic extract of the fruits of Coccinia indica (MECI) (100, 150 and 200 mg/kg, p.o.) was evaluated and compared with standard drug indomethacine (20mg/kg,p.o). The rats were also implanted with cotton pellet and granuloma formation was compared of methanolic extract of the fruits of Coccinia indica (MECI) against diclofenac sodium. (10 mg/kg, p.o.) The extract showed 44.66%, 26.81% and 32.74% inhibition at the dose level of 200 mg/kg, p.o. for carageenan, histamine and dextran induced paw oedema respectively; when compared to that of control group. The effect was comparable with that of the standard drug indomethacin (20 mg/kg, p.o.). The extract also has effectively and significantly reduced the cotton pellet induced granuloma in rats. The percentage inhibition was 59.05% at the dose level of 200 mg/kg, p.o. From the present research work it was concluded that methanol extract of fruit of Coccinia indica (cucurbitaceae) (MECI) has shown significant activity which may be due to some short of phytochemicals such as tannins, saponins, reducing sugars and triterpenoids. and compared with Dexamethasone as standard drug.

Keywords: Coccinia indica, carrageenan, histamine, dextran, cotton-pellet.

ABSTRACT

The aim of the present study was to prepare buccoadhesive sustained release tablets of sumatriptan succinate using novel permeation enhancer to release the drug for extended period of time with reduction in dosing frequency. In the present work sumatriptan succinate was used as a model drug and interaction studies performed using FTIR spectroscopy and DSC revealed that there was no drug, polymer and permeation enhancer interaction. Fulvic acid was extracted from shilajit by using resins. Fulvic acid was characterized by various spectroscopic techniques. Buccoadhesive sustained release tablets of sumatriptan succinate with novel permeation enhancer were prepared by direct compression method using bioadhesive polymers like carbopol 934 and HPMC. The physical characteristics like surface pH, swelling index, in vitro mucoadhesion strength, in vitro drug release and in vitro permeation of formulated tablets were shown to be dependent on characteristics and composition of bioadhesive materials used. The in vitro release study showed 99.88% of drug release with fulvic acid, respectively. Fulvic acid containing tablet has shown enhancement in permeation of drug of 93 % in 12 hours across buccal mucosa in comparison with plain sumatriptan succinate tablet. Sumatriptan succinate release from the buccoadhesive system was extended and exhibited a non fickian drug release kinetics approaching to first order as the values of release rate exponent varied between 0.97 to 0.99 resulting in a regulated and complete release until 8 hours.

Keywords: Buccal drug delivery system, Sumatriptan succinate, Fulvic acid, In-vitro drug release, In-vitro permeation study.

ABSTRACT

2 (H/substituted)-4-aryl-5H,6H, 7-arylimino-1,2,3,5,6-thiatetraazepines (6) have been obtained by basification of 2-(H/substituted)-4-aryl-5H,6H-7-arylmino-1,2,3,5,6-thiatetraazepine monohydrochloride (5).  The latter were synthesized by the interaction of N-aryl-S-chloro isothiocarbamoyl chloride (4) and 1-(H / substituted)-3-aryl-dihydroformazan (3), which were prepared initially by the condensation of aryl acid hydrazide (1) and hydrazine hydrate or substituted hydrazine (2). Compound (6) on benzoylation with benzoyl chloride and excess 10 % sodium hydroxide solution afforded benzoyl derivatives (7) and on boiling with aqueous ethanolic sodium hydroxide solution isomerizes into corresponding 1, 2, 3, 5, 6-pentaazepines (8).  The structures of all the synthesized compounds were established on the basis of elemental analysis, equivalent weight determination, spectral analysis like IR, ¹H-NMR and Mass.  These newly synthesized compounds (6) were screened for their antifungal and antibacterial activity.

Keywords: Synthesis, 1, 2, 3, 5, 6-thiatetraazepine, antibacterial antifungal activity, isomerisation into 1, 2, 3, 5, 6-pentaazepine.

ABSTRACT

A new series of novel substituted Gallic acid derivatives were synthesized by reacting methylated Gallic acid with hydrazine hydrate and then with various substituted aromatic aldehyde in mild and facile synthetic route to form various Schiff base derivatives.  Melting points of the synthesized compounds were determined by open capillary and are uncorrected. The purity of the compounds was checked using precoated TLC plates (MERCK, 60F) using chloroform: methanol (8:2) solvent system. The developed chromatographic plates were visualized under UV at 254nm. IR spectra were recorded using KBr on Josco FTIR model 8400 spectrophotometer, 1H NMR spectra in DMSO on a BRUKER FT-NMR instrument using TMS as internal standard. FAB mass spectra were recorded on JEOL SX 102 (DA-6000 mass Spectrometer) Data system using Argon (6KV.10MA) as the FAB gas. The designed compounds were screened for Antibacterial activity against Staphylococcus aureus and Escherichia coli and Antifungal activity against Aspergillus Niger in comparison with Ofloxacin and Fluconazole as standard to reveal the potency of synthesized derivatives. In accordance with the data obtained from antimicrobial activity, all the synthesized Schiff bases of substituted gallic acid have shown good activity against the tested microbes. Among these Schiff bases, compound bearing p-chloro group, o-chloro group, p-nitro group and m-nitro group has shown good activity against all the tested bacteria and fungi.

Keywords: Gallic acid, Schiff base, Nutrient Broth, 90% Ethanol, Antimicrobial Activity.

ABSTRACT

The major problems associated with the anti-tubercular (TB) drug therapy include loss of efficacy through bacterial resistance, side effects, low patient compliance and duration and complexity of treatment. The present study attempts to confront them through a combined approach consisting of microspheres and bioenhancers. Microspheres containing rifampicin were prepared by emulsification technique using stearic acid as a cross-linking agent. Extract of Carum carvi were added as a bioenhancer in variable amount of 5 to 15 mg for each dose of rifampicin. The loading efficiency and release behavior of loaded microparticles were found to be dependent on the cross-linker concentration, cross-linking time and drug-polymer ratio. Prolonged release of the drug from the microspheres was demonstrated in a simulated intestinal fluid. In-vitro release of rifampicin from the microspheres containing 15 mg of bioenhancer showed significant increase in release profile (87.42% in formulation containing bioenhancer against 51.41% for the formulation without bioenhancer) and the release rates were reduced upon increasing the amount of cross-liking agent and prolonging the cross-linking time.

Keywords: microspheres, rifampicin, sodium alginate, bioenhancer, Carum carvi.

ABSTRACT

The present article is designed for screening and evaluation of biomolecules, antimicrobial potential from extracts of A. nallamalayana (root), belongs to the family Acanthaceae. A. nallamalayana is the rare and endemic to the forests of Nallamalais, the nucleus of Eastern Ghats, India. It has been used in the folklore system of medicine for the treatment of mouth ulcers, leucorrhoea and abortion / sterility. Phytochemical screening and antimicrobial activity of the test species is hither to not reported. The phytochemical investigation on all such extracts revealed the presence of flavonoids, alkaloids, phenols, steroids and triterpenoids. The antimicrobial activity of various extracts (petroleum ether, ethyl acetate and methanol) of A. nallamalayana revealed that the methanolic extract (root) exhibited maximum inhibition on all test pathogens followed by ethyl acetate while petroleum ether failed to show inhibition. Klebsiella pneumoniae, Salmonella typhimurium, Staphylococcus aureus were proved as most sensitive while Bacillus subtilis as resistant strain to the test extracts.

Keywords: Andrographis nallamalayana, Phytochemical screening, Antimicrobial activity.

ABSTRACT

Anal stricture is a rare but serious complication of anorectal surgery, most commonly seen after hemorrhoidectomy (1-2 months postoperatively). Simple cases with anal stricture can be managed conservatively with stool softeners or fiber supplements, otherwise surgery is indicated, meanwhile anal stricture may be prevented with the use of certain antioxidants (zinc sulphate) locally.Thirty five patients aged 20– 45years; 11 female 24 male, with hemorrhoidectomy surgery randomly allocated as a control , group A; (15 cases) with frequent manual dilatation, 2 weeks postoperatively for 3 weeks , matching with group  B (20 cases) had frequent  manual dilatation along with application of zinc sulphate ointment  5% four times daily , 2 weeks postoperatively for 3 weeks. Compared with control group, group B showed no incidence of stricture following hemorroidectomy cases while in other cases within group A, there were 2 cases had stricture treated by dilatation and sphincterotomy (surgery) later. Zinc sulphate ointment 5% seemed to be effective in preventing anal stricture along with frequent manual dilatation two weeks postoperatively for at least two weeks.

Keywords: Zinc sulphate ointment, Anal stricture, Hemorrhoidectomy, Digital dilatation, Proctoscopy.

ABSTRACT

A simple, fast and precise reverse phase, isocratic HPLC method was developed for the separation and quantification of Sildenafil and Duloxetine in pharmaceutical dosage form. The quantification was carried out using Symmetry C18-ODS 4.6X150mm, 3µm enhanced polar selectivity column and mobile phase comprised of potassium dihydrogen phosphate buffer and acetonitrile and water in proportion of ratio 30:65:5 and degassed under ultra-sonication. The flow rate was 0.6mL/min and the effluent was monitored at 244nm. The retention time of Sildenafil and Duloxetine were 4.3 and 3.4 respectively. The method was validated in terms of linearity, precision, accuracy, and specificity, limit of detection and limit of quantization. Linearity of Sildenafil and Duloxetine were in the range of 100 to 300µg/mL and 30 to 90µg/mL respectively. The percentage recoveries of both the drugs were 98.7% and 99.8% for Sildenafil and Duloxetine respectively from the tablet formulation.The method was found to be precise, accurate and specific during the study. The proposed method enables rapid quantification and simultaneous analysis of both drugs from commercial formulations without any excipients interference. The method can be used for routine analysis of marketed products of Sildenafil and Duloxetine in combined tablet formulation

Keywords: Sildenafil, Duloxetine, RP-HPLC, Validation, stability studies

ABSTRACT

The objective of the present study was to prepare in situ hydrogel for controlled release of ofloxacin using various polymers such as Poloxamer P407, Sodium Alginate and Polyox. In situ were characterized for the Appearance, pH determination, In vitro Gelation studies and viscosity, Rheological studies, Drug Content, In vitro Drug release study, Sterility testing. Drug-excipient compatibility was determined by FTIR. Infrared spectroscopy studies of Ofloxacin, Polyox, Sodium alginate, Poloxamer and HPMC K4M alone and their physical mixture revealed that, Ofloxacin is compatible with all the polymers used. The clarity of the prepared formulations was found satisfactory. The pH of all formulations was found to be satisfactory in the range. The drug content of the prepared formulation was within the acceptable range, and ensures dose uniformity. The curve fitting data revealed that the release followed zero order kinetics.

Keywords: In situ Hydrogel, Ofloxacin, Controlled Release, Polyox, Poloxamer.

ABSTRACT

The present manuscript describes sensitive, rapid, accurate, and precise second order derivative spectrophotometry method for the simultaneous determination of tramadol hydrochloride and aceclofenac in combined dosage form. The absorbance values at 225 nm and 215 nm of second derivative spectrum was used for the estimation of tramadol hydrochloride and aceclofenac in combined dosage form, respectively without mutual interference. This method obeyed beer’s law in the concentration range of 5-80μg/ml and 4-28μg/ml for tramadol hydrochloride and aceclofenac respectively. The method was successfully applied to combined dosage form because no interference from the excipients was found. The suitability of this method for the quantitative determination of tramadol hydrochloride and aceclofenac was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of tramadol hydrochloride and aceclofenac in combined dosage form. The results of analysis have been validated by recovery studies.

Keywords tramadol hydrochloride, aceclofenac, second order derivative spectrophotometry method.

ABSTRACT

The objective of this study was to investigate hydrogenated vegetable oil (Lubritab) and hydrogenated castor oil (HCO) as potential lipophilic binders in melt granulation process for the preparation of sustained release matrices of venlafaxine hydrochloride, a highly water soluble drug. The effect of concentration, type of polymer and method of preparation (direct compression of physical mixtures and melt granulation technique) were studied. Granules prepared by melt granulation method were evaluated for micromeritic properties, FT-IR, DSC, XRD and SEM. The compressed tablets were subjected to thickness, hardness, friability, mass variation test, drug content and in vitro release studies. The result of dissolution study showed that formulations containing drug: HCO (1:3 m/m) retarded drug release more than those containing drug: Lubritab (1:3 m/m) ratio. In conclusion, melt granulation technique was found to be more appropriate in retarding the release compared to compression of physical mixtures of drug and lipophilic binder. The study showed that HCO and Lubritab are the appropriate meltable binders that can be utilized as matrix-forming agent to sustained the release of highly water soluble drugs.

Keywords: sustained release, melt granulation, hydrogenated castor oil, hydrogenated vegetable oil

ABSTRACT

An immediate action of Metformin HCl is essential for emergency treatment of diabetes. With an objective of finding the best suitable disintegrant for immediate release tablet of Metformin HCl, different formulations were prepared by incorporating varying ratios of three widely used superdisintegrants both by intra and extra granularly. Wet granulation method was adopted to formulate the tablets by using Maize Starch as diluent; Povidone k-30 as binder; Sodium Starch Glycolate/Kollidon CL/Crosscarmellose Sodium as superdisintegrants in different concentration (2-3.5%), Aerosil-200 as flow promoter and Magnesium Stearate as lubricant. To evaluate the rheological properties of powdered blend, some pre-compression characteristics including bulk and tapped densities, compressibility index, Hausner’s ratio, angle of repose were studied. The compressed tablets were evaluated for hardness, thickness, diameter, friability, drug content, weight variation, in vitro dispersion time, in vitro disintegration time, in vitro wetting time and finally for in vitro dissolution studies. It was found that wetting time, dispersion time and the disintegration time of the tablets were governed by the type and quantity of the superdisintegrants. In vitro drug release data obtained at phosphate buffer at pH 6.8 also found reliant on successful incorporation of right disintegrating agent. Higher the disintegrant ratio in the formulation, lower the disintegration time and hence, higher percentage of drug release was obtained. Based upon results of different studies, Sodium Starch Glycolate has been proven successful in rapid disintegration of tablets and enhancing dissolution behavior.

Keywords: Superdisintegrants, wetting time, dispersion time, Hausner’s ratio, compressibility, flow promoter.