ABSTRACT

Kalanchoe pinnata (Family: Crassulaceae) is an important plant which has many traditional medicinal uses. The main objective of this literature review was to give advance information for the drug discovery research for K. pinnata. It was found that this plant showed various pharmacological activities such as anthelmentic, immunosuppressive, wound healing, hepatoprotective, antinociceptive, anti-inflammatory, antidiabetic, nephroprotective, antioxidant activity, antimicrobial activity, analgesic, anticonvulsant, neuropharmacological and antipyretic. Anthelmentic activity was found due to the presence of tannins of the extract of K. pinnata and steroid glycosides such as bufadienolide showed wound healing activity. It was also found that the different flavonoids, polyphenols, triterpenoids and other chemical constituents of the plant were responsible for the antinociceptive, antiinflammatory and antidiabetic properties. Quercetin had a marked protective effect on cadmiuminduced nephrotoxicity and possessed potent oral efficacy against cutaneous leishmaniasis. The two new novel flavonoids such as 5Methyl 4, 5, 7 trihydroxyl flavone and 4, 3, 5, 7 tetrahydroxy 5-methyl 5 Ipropenamine anthocyanidines could be responsible for the antimicrobial activity of K. pinnata. Five bufadienolides (1-5) isolated from the leaves of K. pinnata were potential cancer chemopreventive agents. Quercitrin, a flavonoid, is a critical component of K. pinnata extract against an extreme allergic reaction. This literature review gave the evidence based information regarding the pharmacognostical, phytoconstituents and pharmacological activity of the medicinal plant, K. pinnata which could help researchers for more advanced qualitative research.

Keywords: Kalanchoe pinnata, Pharmacognostical, Phytochemical, Pharmacological

ABSTRACT

Drug delivery systems using colloidal particulate carriers such as liposomes and niosomes have distinct advantages over conventional dosage forms. This class of drug carrier systems will likely play an increasingly important role in drug delivery. However, there remain significant problems like instability in the general application of liposomes and niosomes for drug delivery. Pro vesicular drug delivery developed to overcome the stability problems associated with vesicular drug delivery systems composed of water soluble porous powder as a carrier drug is dissolved in an organic solvent to produce free-flowing granular product. To overcome the limitations (especially chemical and physical stability) of vesicular drug delivery systems like liposomes, niosomes, trans-ferosomes, and pharmacosomes, the pro-vesicular approach was introduced. The present article gives a brief overview of introduction on proliposomes, Pro-niosomes, Dry granular liposomes, mixed micellar proliposomes, Pro-transferosomes and its applications.

Keywords: Proliposomes, Pro-niosomes, Pro-transferosomes, Dry granular liposomes.

ABSTRACT

Herbal medicine has occupied special place in the world of pharmaceuticals. Lavendula stoechus Linn, known as Ustukhuddoos is such a plant origin drug documented in Unani literature, which possesses many pharmacological actions, few are scientifically evaluated and many are yet to be evaluated.  The present review attempts to encompass the up to date comprehensive literature analysis on Lavendula stoechus Linn with respect to its phytochemistry, pharmacognostic characters and its various pharmacological activities.

Keywords: Herbal medicine, Ustukhuddoos, Lavendula stoechus Linn, Nervine tonic

ABSTRACT

Glycogen synthase kinase-3 (GSK-3) is an intermediary enzyme in various cellular pathways, and has been implicated in the Pathophysiology and treatment of numerous diseases, including Alzheimer, diabetes, and bipolar disorder. Alzheimer’s disease (AD) is a disorder without a molecular marker in peripheral tissues or a disease modifying treatment. Evidence suggest that the co-relation of diabetes and Alzheimer is clear with the GSK-3. Now day’s researchers taking efforts basically to develop the new GSK-3 inhibitors like lithium. For the development of new GSK-3 inhibitors, we have to understand its molecular mechanism and their involvement in pathological condition. So here we summarize brief introduction and mechanism of GSK-3.

Keywords: Glycogen synthase kinase-3 (GSK-3), Alzheimer’s disease, diabetes, bipolar disorder

ABSTRACT

Enhancement of the solubility, dissolution and bioavailability of the drugs is the challenging task for the research sector. As many of the solubility enhancement techniques are available to achieve the desired goal, but the older techniques don’t show the expected results for solubility enhancement and bioavailability as well, and they are unstable also some time.  But today the scenario is different because the novel techniques of solubility enhancement are available, such as hydrotropy, supercritical fluid process, sonocrystallisation, inclusion complex system, spray drying, microwave assisted techniques, etc. this novel techniques have the ability to give the reproducible results for solubility enhancement in pharmaceutical product development.  present review article deals with the different techniques for the solubility enhancement of the poorly soluble drug candidates.

Keywords: Solubility, hydrophobic drugs, solubility enhancement, solid dispersion, beta cyclodextrin.

ABSTRACT

Microsphere is a carrier system for delivery of therapeutic candidate. Nasal microspheres offers significant advantages over other type of drug delivery system. It modulates absorption characteristics of the drug by enhancing drug residence time in the nasal cavity and subsequently may increase bioavailability profile of administered drug. Prior to formulation some physicochemical properties of drug are need to be considered like molecular weight, solubility, pKa and partition coefficient of drug etc. Till date various methods have been adopted for fabrication of nasal microspheres are like spray drying, emulsion crosslinking, Solvent Evaporation etc. Obtained microspheres can characterized for various properties like its morphology, drug content, and zeta potential etc. Present  review mainly focuses on overview of microsphere technology for nasal administration of drug.

Keywords: Microspheres, Nasal, Mucociliary Clearance

ABSTRACT

High-Throughput Screening (HTS) is an approach to drug discovery that has gained widespread popularity over the last two decades and has become a standard method for drug discovery in the pharmaceutical industry. Progress from traditional one-compound-at-a time approach, low throughput screening to high throughput screening involving fully automated robotic systems, enables testing of large numbers of compounds daily for different activities in miscellaneous areas of biology. HTS reveals screening of more than 100,000 samples per day. Compared to traditional drug screening methods, HTS is characterized by its simplicity, rapidness, low cost, and high efficiency. Identification of good hits using HTS can minimize the time span of drug discovery noticeably. However, synthetic chemistry for lead optimization and the low throughput of secondary assays for defining the crucial pharmacological properties of active compounds, limits the overall rate of identification of candidate molecules for clinical evaluation. Coupling of compound library with wide chemical diversity along with HTS shows massive drug discovery potential, but to be successful screening technique it depends on several factors. These include the number and quality of validated targets, the number and diversity of compounds in the collections, and the ability to screen these in a timely and cost effective manner using robust informative assays. In this review we have discussed the types of HTS assays, assay miniaturization automation and different detection techniques like fluorescence resonance energy transfer (FRET), fluorescence polarization (FP), homogeneous time resolved fluorescence (HTRF) etc.

Keywords: HTS, FRET, FP, HTRF, Cell based assays, Statistics.

ABSTRACT

The ethnopharmacologicalsurvey of differentplants was carried out in Tuting area located in the Upper Siang district of Arunachal Pradesh. The authors investigated about the use of different plants in the treatment of ailments. 51 different plants were documented in this study along with the information regarding the use of the plants in different formulations.

Keywords: Ethnopharmacology, Tuting, Medicinal Plants, Formulations

ABSTRACT

Chemistry of heterocyclic organic compounds is as logical as that of aliphatic/aromatic compounds and of great interests both from the theoretical as well as practical synthetic view to design novel compounds that becomes one of the most important areas of research today. Electron-flux of six member/annulated N heterocycles plays vital roles to exhibit diverse potent biological activities from pharmaceuticals to industrial materials. The Pyrimidine and fused pyrimidine annulated rings in the chemistry of biological systems has attracted much attention due to availability in the substructures of therapeutic imperative natural products. As a result of their prominent and remarkable pharmacological activity, pyrimidine derivative’s intensive research has been made especially focused on its anticancer activity. The present review gives brief information about anticancer activity of assorted six member/annulated pyrimidine derivatives.

Keywords: Annulated pyramidine, Heterocycles, anticancer activity, biological active

ABSTRACT

Aatrilal (Ammi majus Linn) is an important unani drug for treatment of vitiligo. It belongs to family Apiaceae. It is originated in Egypt. But now it is successfully cultivated in India. It is the principal commercial source of Xanthotoxin. Xanthotoxin is used in the treatment of Vitiligo (Leucoderma).It is also used as diuretic, blood purifier, detergent, emmenogogue, and has antispasmodic and anti inflammatory properties. In Unani system of Medicine Aatrilal is used both internally as well as externally in the patients of Bars (Vitiligo). A number of clinical studies have been carried out with the Aatrilal in the treatment of vitiligo. These trials have shown significant results.

Keywords: Aatrilal, Ammi majus, vitiligo, leucoderma

ABSTRACT

Quality by design is an essential part of the modern approach to pharmaceutical quality. Quality by design (QbD) is more scientific, risk based, holistic and proactive approach in pharmaceutical development for FDA and pharmaceutical industry in drug development. Quality by Design (QbD) is everything you do to directly to promote,  prove safety,  efficacy  and  quality  of your product from proof of concept to the point at which costumer are buying on regular basics.  This novel concept of QbD promotes industries in understanding product and manufacturing process starting with product development which aims basically building quality in product, not by testing it. A company needs to define desire product performance profile [Target product Profile (TPP), Target Product Quality Profile (TPQP)] and identify critical quality attributed (CQA) under this concept of QBD during designing and development of a product. On the basis of information obtained company can build consistent product quality by monitoring and updating its manufacturing processes. This systematic approach to product development and manufacturing has received a great deal from traditional approach. The purpose of present article is to discuss the concept of pharmaceutical Quality by Design (QbD) and describe how it can be help to ensure pharmaceutical quality.

keywords: quality by Design (QbD), Target Product Profile (TPP), Critical Quality Attributes (CQA), ICH guidelines. Food and Drug Administration (FDA)

ABSTRACT

Pharmaceutical cocrystals represents a class of Pharmaceutical materials with definite stoichiometries often stabilized by hydrogen bonding, which have recently emerged as interesting alternative solid forms with potential for improving the physical and biopharmaceutical properties of a drug substance. Pharmaceutical cocrystal is crystalline nonionic supramolecular complexes of two one being neutral molecules or an active pharmaceutical ingredient (API) and the other a cocrystal former. Cocrystal formation is studied in the development stage in order to solve an issue with solid form or formulation or to expand intellectual property. The review focuses on pharmaceutical cocrystals, cocrystal design, and methods of co crystallization, characterization, regulatory classification, cocrystals as intellectual property and some examples of candidate for preparation of cocrystals.

Keywords: Cocrystal, Co crystallization and Addition compound.

ABSTRACT

Over the past few decades, there has been an increased  interest for innovative drug delivery systems to improve safety, efficacy and patient compliance, thereby increasing the product patent life cycle. There are novel types of dosage forms that act very quickly after administration. The basic approach used in development tablets is the use of superdisintegrants like Cross linked carboxymelhyl cellulose (Croscarmeliose), Sodium starch glycolate (Primogel, Explotab), Polyvinylpyrrolidone (Polyplasdone) etc. which provide instantaneous disintegration of tablet after administration. Immediate release liquid dosage forms and parenteral dosage form have also been introduced for treating patients. Liquid dosage form can be suspensions with typical dispersion agents like hydroxypropyl methylcellulose, AOT (dioctylsulfosuccinate) etc. The development of immediate release therapy also provides an opportunity for a line extension in the marketplace, A wide range of drugs (e.g., neuroleptics, cardiovascular drugs, analgesics, antihistamines, and drugs can be considered candidates for this dosage form. In this regard, immediate release formulations are similar to many sustained release formulations that are now commonly available. oral film dosage form not only has certain advantages of other fast disintegrating systems but also satisfies the unmet needs of the market. The present review emphasizes on the potential benefits, design and development of robust, stable, and  innovative orally immediate and their future  scenarios on a global market as a pharmaceutical dosage form.

Keywords: Immediate release, polymers, superdisintegrant.

ABSTRACT

Several five membered aromatic systems having three heteroatoms at symmetrical positions such as thiadiazoles have been studied extensively owing to their interesting pharmacological activities.  Compounds containing thiadiazole moiety possess interesting biological activity due to strong aromaticity of this ring system that leads to great in vivo stability and lack toxicity. Thiadiazoles are an important class of heterocyclic compounds that exhibit diverse applications in organic synthesis, pharmaceutical and biological applications that exhibits a wide variety of biological activities like antimicrobial, anti-inflammatory activity, antitubercular activity, antidiabetic activity, diuretics, antidepressant & cytotoxic activity. Modification of the thiadiazole ring has proven highly effective with improved potency and lesser toxicity. The present review highlights the recently synthesized thiadiazole possessing important biological activities.

Keywords: Thiadiazole ring, Antitubercular activity, Antidiabetic activity

ABSTRACT

Rheumatoid Arthritis is an autoimmune inflammatory disease where the immune system of the body which normally protects the body by fighting against infection and diseases instead targets the body. The immune system attacks the tissue that lines the joints causing pain, swelling and stiffness in the joint and affecting the ability to work properly. Early treatment to avoid permanent joint damage is the key for preventing disability and progression. The treatment for Rheumatoid Arthritis combines many approaches with drug, exercise, change in lifestyle etc. It also includes alternative methods i.e with herbal medicines. Many plants and plant products have been proven and many are under scientific exploration to develop a novel therapeutic agent for Rheumatoid Arthritis.

Keywords: Herbs, Rheumatoid Arthritis, Medicine, Immunity, Inflammation.

ABSTRACT

Micro-particulate systems have already shown their potential as a carrier in delivery of many therapeutic molecules. Due to this potential, such systems are now most preferred over other conventional systems of drug delivery. Micro-carriers (Microspheres) shows features like controlled release, improvement in the residence time and thus enhancing bioavailability of administered drug. Nasal microspheres are now a day’s becoming more popular for delivery of many therapeutic moieties. For building of microparticulate systems polymers from natural and synthetic origins are generally used. Drugs which are not suitable for oral administration due to high first pass effect (i:e presystemic metabolism), instability in gastrointestinal tract can be successfully delivered via nasal route. Systems like mucoadhesive microspheres provide sufficient time for drug to remain in contact with mucosal membrane so as to increase their absorption. This is the basic underlined reason suggests why most of the polar drugs have shown improvement in the bioavaibility when compared with their conventional intranasal formulations. This review mainly focuses on the basic aspects of microspheres as a potential carrier in the drug delivery.

Keywords: Microspheres, Nasal Drug Delivery, Mucoadhesive.

ABSTRACT

Gastro esophageal reflux disease is a chronic, recurrent disease that affects millions of people worldwide. Proton pump inhibitors are a group of drugs whose main action is a pronounced and long-lasting reduction of gastric acid production. These drugs are utilized in the treatment of many conditions such as Dyspepsia, Peptic ulcer disease, Gastro esophageal reflux disease. Currently proton pump inhibitors are available in both oral and injectable formulation. Proton pump inhibitors are substituted benzimidazoles that inhibit gastric acid secretion via inhibition of the gastric H+/K+ ATPase pump. Although there are some differences in pharmacokinetics and binding affinity for the pump, these drugs are comparatively similar in their efficacy in treatment of gastric diseases. The delayed release proton pump inhibitors effectively suppress gastric acid secretion and successfully treat acid-related disorders. Each differs somewhat in its formulations. The difference in the formulations has not been translated  into clinical advantages over the delayed release proton pump inhibitors. Novel multiple formulations approaches are required for proton pump inhibitors to enhance acid suppression. Although the individual proton pump inhibitors have similar efficacy in many cases, differences between them should be considered when choosing a treatment regimen.

Keyword: Gastro esophageal reflux disease, Proton pump inhibitors, Pharmacokinetics

ABSTRACT

Microgels/nanogels are crosslinked polymeric particles, which can be considered as hydrogels if they are composed of water soluble/swellable polymer chains. These polymeric particles possess high water content, biocompatibility, and desirable mechanical properties. Offers unique advantages for polymer-based drug delivery systems (DDS) such as a tunable size from nanometers to micrometers, a large surface area for multivalent bioconjugation, and an interior network for the incorporation of biomolecules. This review article describes the recent developments of microgel/nanogel particles as drug delivery carriers for biological and biomedical applications and also various synthetic strategies for the preparation of microgels/nanogels.

Keywords: Microgels, nanogels, polymers based drug delivery systems.

ABSTRACT

Nasal drug delivery is an excellent approach for avoiding first pass effect of oral dosage form. It offers a direct systemic delivery of drugs. Nasal administration can therefore be used as an alternative to oral administration for example tablets and capsules if a fast effect is desired or if the drug is extensively degraded in the gut or liver. The primary goal of this article is to study factors affecting nasal drug absorption and the in-vitro methods available for nasal absorption of drugs. There are many in-vitro models for testing absorption studies and it has many advantages over in-vivo methods such as a controlled environmental study of epithelial cell growth and differentiation, drug transport pathways and mechanisms are elucidated easily, it has very fast means of evaluating drug permeability and to minimize expensive use of animals. Cell culture and cell line models were found to be best for nasal in-vitro absorption studies. Similar results are obtained from in-vitro studies. So by using in-vitro methods one can mimic the in-vivo conditions. It avoids disadvantages of in-vivo study. It was concluded that in-vitro models mimics the results of in-vivo study. But up till now no any system is superior to one another.

Keywords- In-vitro methods, nasal drug absorption, PDMS and Culture models.

ABSTRACT

Over the past decade, numerous limitations of conventional dosage forms had attracted researchers to find a rational and appropriate drug delivery system. Microsponges were developed and studied as a novel programmable delivery system which is intended to deliver drug in controlled release pattern. It also aims epidermal localization of topical drug therapy to reduce their side effects by limiting systemic absorption through skin. Drug loaded microsponges are microporous beads, typically 10-25 µm in diameter which can entrap a wide variety of actives and can be formulated as creams, lotions, gels, ointments, powders, soaps. Microsponge formulations can increase product stability, enhance aesthetic qualities, and provide formulation flexibility and stability. Moreover, their non-antigenicity, non-toxicity, non-mutagenicity and non-biodegradability make them favourable candidates. Microsponge approach has also been applied in oral therapy, bone, tissue & cartilage engineering and showed remarkable results. This article provides description about the nature of microsponges, their characteristics, preparation, applications and commercial market status globally.

Keywords: Microsponges, topical delivery, controlled release, quasi-emulsification, programmable release

ABSTRACT

In society couple dreamed for momentous decision of child and  they dream a procure  disease free and healthy  (mentally, physically) baby endowed with excellence . Pre  conception care extension of antenatal care to provide optimal health to mother and baby . Ayurveda described regime and rituals  before pregnancy to take care of foetus from the state of gametes to promote the multistate well being of child promising the efficacy of body (Dosha, Dhatu, mala) metabolism (agni), perception element (indriyas),psyche (Manas) intelegence (buddhi)  and the inner spirit(Atma). Pre-requisites for healthy pregnancy described in ayurved Ritu (Fertile period), Kshetra( Uterus) ,Ambu (ahara rasa nutrient) , Beeja-( sperm and ovum) , Marga ( genital passage), .Hridi (pure controlled consciousness). Pre- conceptional care comprises of treatment methods like purva karm snehan , swedan, purificatory method Vaman, virechan , and nutritive vasti associated with diet restriction ,abstinence ,religious rituals to ensure Beeja-shudhi  , Kshetra –shudhi, and Mano Shudhi and putresti yajna .Above  the  pre conceptional  care  to bring healthy offspring and  in interest of future generation for benefit of society and nation and to maintain the health in the affluent society and to improve the health in developing countries.

Keywords:  Ritu,kshetra, ambu, beeja, Purv karm, Shodhan karma, Bramhacharya, Vajeekaran , Manoshudhi , Putresti yajna

ABSTRACT

Haematological complications (neutropenia, thrombocytopenia and anaemia) of pegylated interferon/ribavirin(PEG-IFN/RBV) in chronic hepatitis C can result in treatment cessation and suboptimal results. To investigate the nature, frequency of haematological side effects in the treatment of chronic hepatitis C infection and their impact on the response to PEG-IFN/RBV therapy. This cross sectional study of 3719 Egyptian patients with chronic HCV (genotype 4), who were received PEG-IFN/RBV therapy at Cairo-Fatemic Hospital, Egypt in the context of the national program was retrieved. Patients were defined as having hematological abnormalities if they had the presence of either/or a combination of following hematological parameters at least once during follow up period; drop in hemoglobin(Hb) level <10gm/dl, absolute neutrophil count(ANC)<750 cells/mm3, and platelet(PLT)count<80 x 10³/µL. At week 48, end of treatment response (ETR) was 61.6% and at week 72 the estimated sustained virological response (SVR) was 52.5%. Pre-treatment, Hb, white blood cell (WBCs)count, ANC, and PLT count; were not statistically related to the treatment response. However lower count of all parameters were associated with moderate or advanced hepatic fibrosis stages according to the METAVIR scoring (p<0.001). During anti-viral therapy, anaemia occurred in 31.8%, neutropenia in 22.3% while thrombocytopenia occurred in 10.5%. Univariate logistic regression analysis showed that drop in Hb, TLC and PLT count were significantly associated with response to treatment; p value < 0.01, 0.03,0.03 respectively. Baseline hematological parameters were not predictors of treatment response in chronic HCV (genotype 4); however; low Hb level, TLC, ANC, and PLT count were associated with advanced stages of hepatic fibrosis. Drop of Hb,TLC and PLT count during anti-viral therapy were significantly associated with response rates regardless to the type of PEG-IFN.

Keywords: HCV; IFN; Ribavirin, Haemtological, Anaemia, platelet and neutopenia.

ABSTRACT

Rheumatoid arthritis (RA) is an autoimmune disorder of unknown etiology, despite therapy may result in progressive joint destruction, deformity that lead to disability, and even premature death in some cases. Random Amplified DNA Polymorphism (RAPD) technology showed high efficiency in investigating the genetic diversity between healthy control group and RA patients and detecting the genetic diversity among RA patients and the effect of this diversity on the patients response to the drugs regimens used to treat RA. The primers GATGACCGC and ACAACGCCTC showed the best ability to discrimate between the healthy subjects and the RA patients, and the primers GATGACCGC, ACAACGCCTC and CAGCACCCAC showed the best ability to detect the genetic diversity among RA patients and detecting the effect of this diversity on the patients' response to treatments. Analysis of the resulted pattern of amplifications through the Unweighted Pair Group Method with Arithmetic mean (UPGMA) algorithm program revealed an important thing which is the fact that RAPD technology is an important relatively cheap and available technology that can be used in pharmacogenomics because of the fact that there is an association between the genetic content of the patients and their response to different treatment regimen.

Key words: RAPD/ PCR technology, rheumatoid arthritis genetics, population genetics, Iraqi population genetics

ABSTRACT

Today all over the world Salmonella typhimurium is one of the most frequent causes of food poisoning in humans. The antimicrobial resistance of salmonellas has increased rapidly during the last decade, creating a serious threat to the treatment of infectious diseases. This study will introduce the multi-drug resistance of 2931 Salmonella typhimurium strains isolated in patients diagnosed with salmonellosis or in carriers of salmonellas in the region of Elbasan, Albania during 1985-2004. All Salmonella typhimurium strains isolated during this period have been tested using impregnated discs with the most common used antimicrobial agents. S.typhimurium strains have shown resistance toward antibiotics as follows: Te+S, 64.04%, Te+C, 58.24%; S+C, 55.85%, Te+S+C, 53.46% while the multi-drug resistance shown is 87.17%. This multi-drug resistance of the strains isolated during 1985-2004 is comparable with the data represented by some native and international authors.

Keywords: antibiotics, double drug resistance, multi-drug resistance, Salmonella typhimurium.   

ABSTRACT

Rapid and accurate High performance liquid chromatography method is described for Simultaneous estimation of Perindropil and Indapamide from the combination tablet dosage form. The separation of two drugs was achieved on Phenomenax (C₁₈) (4.6mm x 100mm, 3.5 mm) column. The mobile phase consists of Acetonitrile : Buffer Orthophosphoric acid 0.1% in the ratio of 40:60. The detection was carried out at a wavelength 230 nm. The method was validated for system suitability, linearity, accuracy, precision, robustness and stability of sample solution. The linear ranges for Perindropil and Indapamide were 8-40 μg/mL, 2.5- 12.5 μg/mL respectively with good recoveries i.e. 100.5% to 100.3%.

Keywords: Perindropil, Indapamide , High performance liquid chromatography.

ABSTRACT

Hospital acquired infections are commonly associated with Methicillin Resistant Staphylococcus aureus infection and treating these infections with chemotherapy is very perilous. The augment of multidrug-resistant strains makes it necessary to discover new classes of antimicrobials and compounds that restrain their resistance mechanisms. In the past few decades, the search for new anti-infective agents has betrothed many research groups in the field of ethno pharmacology. Many focus on determining the antimicrobial activity of plant extracts found in folk medicine, essential oils or isolated compounds. There are a large number of species that have been and are still used as medicinal plants, particularly in folk medicine. In the present study, we analyse the possibility of essential oils as potential antimicrobial crude drugs as well as a source for natural compounds that act as new anti-infectious agents.

Keywords: multi drug resistance, antimicrobial, medicinal

ABSTRACT

Drug delivery via nanoparticle-based carriers has shown promising results for different types of diseases. Delivery of anti-gout agents into body is a mature line of investigation that has yet to realize its full potential. In this study we report on the development of a delivery platform for febuxostat. The work presented here describes the development of nanoparticles based on compritol. The method employed for the preparation of SLN is micro emulsification technique followed by high pressure homogenization. Phase diagram was developed to know the region of stable micro emulsion formation. Eight different formulas were developed with different concentrations of lipid, surfactant and aqueous concentrations. The developed formulations were evaluated for particle size distribution, zeta potential, entrapment efficiency, DSC thermal analysis and in vitro drug release studies. Among all the formulations developed, F3 formulation is showing better drug entrapment efficiency and controlled release of drug up to 24h. There was 12 fold increase in the solubility of drug in the developed formulation. The solid lipid nanoparticles of febuxostat can be prepared by using simple micro emulsification technique. The formulations had shown better release profile and solubility characteristics.

Keywords: Febuxostat, micro emulsion, nanoparticles, phase diagram, in vitro drug release studies

ABSTRACT

Hyper-cholesterolaemia is one of the leading causes of the major diseases like angina pectoris, myocardial infarction, atherosclerosis which increases the mortality rate every year. This study includes the evaluation of sample Ayur NS01 for anti-cholesterolemic effect using two models HCD induced hypercholesterolemia and lipid emulsion tolerance test (LETT) in rats.  The evaluation was made in different doses (1.35gm/kg, 1.8gm/kg,2.25gm/kg ) of Ayur NS01 sample. The lipid profile parameters like LDL, total cholesterol, VLDL and lipid emulsion tolerance were studied in the normal, high cholesterol diet induced hypercholesterolemic , AyurNS01 and  the standard drug atorvastatin (10mg/kg) administered rats. The results of HCD alone administered rats (group II) were compared with normal rats. The results obtained in the HCD and various doses of rats of AyurNS01, atorvastatin were compared with HCD alone administered hypercholesterolemic rats. From the results of first model of this study it is confirmed that the sample of AYUR NS01 has shown a significant reduction in the total cholesterol, triglycerides, LDL levels when it is compared to the HCD induced hypercholesterolemia rats. From the results of Lipid emulsion tolerance test, it is also confirmed that the sample of has also shown a reduction in the serum triglyceride levels in the AYUR NS01 treated groups as compared to the control rats treated with lipid emulsion.

Keywords- Hyper-cholesterolemia, high cholesterol diet, lipid emulsion, Ayur NS-01

ABSTRACT

A rapid and stability indicating ion-pair reversed phase high performance liquid chromatographic method was developed for qualitative and quantitative estimation of three oxicam drugs: tenoxicam, meloxicam and lornoxicam. The method was validated according to ICH, FDA and USP guidelines with respect to accuracy, precision, specificity, linearity, solution stability, robustness, sensitivity and system suitability. The method was developed by using an isocratic condition of mobile phase comprising buffer pH 6.5 [tetra butyl ammonium hydroxide (0.008M) and sodium 1-heptane sulfonate (0.003M)] and acetonitrile in a ratio of 65:35 v/v ratio at a flow rate of 1.5 mL/min over C-18 (ODS, 250 x 4.6 mm) column at ambient temperature. The method showed linear response with correlation coefficient (r²) value of 0.999. The recoveries for all drugs were found more than 99% which demonstrated the accuracy of this method. Intraday and inter-day precision studies of the new method were less than the maximum allowable limit (RSD%£ 2.0). Forced degradation studies were carried on to check its stability indicating property. All the drugs gave sharp peaks within 7min with excellent symmetry and high resolution. Therefore, a rapid, sensitive and stability indicating ion pair RP-HPLC  method was developed for simultaneous separation of tenoxicam, meloxicam and lornoxicam in their any combination or in bulk raw materials.

Keywords: Ionpair, RP-HPLC, stability-indicating, tenoxicam, meloxicam, lornoxicam

ABSTRACT

The main objective of the study is to enhance the dissolution rate and solubility of paliperidone by using the solid dispersion technique which were wildly used in pharmaceutical company because of its less cost. Paliperidone is antipsychotic classes of drug that can be used for the treatment of schizophrenia. Initially preformulation studies were conducted to check the incompatibilities of drug substance. Initially phase solubility studies were performed with respect to different molar ratio. Drug polymer interactions were investigated using differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). As indicated from XRD and DSC data, paliperidone was in the amorphous form, which explains the better dissolution rate of then drug from its solid dispersion. Solid dispersion of paliperidone were prepared to check the solubility of paliperidone because of its poor solubility issue by using the different polymer and to find out the effect of various solubilizer on its solubility and dissolution rate.

Keywords:  Solid Dispersion, Solubilizer, Paliperidone, Dissolution Enhancement.

ABSTRACT

The objective of this study was to formulate and evaluate dispersible tablets of diltiazem HCl using direct compression method for enhanced patient compliance. Oro dispersible tablets prepared by using super disintegrants such as croscarmellose sodium, crospovidone, sodium starch glycolate. It was observed that all the formulations were acceptable with reasonable limits of standard required for oro dispersible tablets. It was concluded that dispersible tablets with enhanced dissolution rate can be made using selected super disintegrants.

Keywords: Orally disintegrating tablet, Improved bioavailability, super disintegrants.

ABSTRACT

The In-vitro antioxidant and anti-inflammatory activity of the leaf extract of Putranjiva roxburghii were studied along with preliminary phytochemical investigation. The leaf of the plant contains mainly anthracene, cardiac and flavonoid glycosides along with phenolic compounds. Since many flavonoids have remarkable anti inflammatory activity the present work aims at evaluating the anti inflammatory activity of Putranjiva roxburghii by HRBC membrane stabilization. The ethanolic extract of the leaf was anlysed for antioxidant activity by DPPH method at different concentrations. Throughout the studies leaf extract showed potent antioxidant activity. The antioxidant activity was found to be concentration dependent and may be attributed to the presence of high flavonoid content in the leaves of Putranjiva roxburghii

Key Words: Anti oxidant activity, Anti-inflammatory, Putranjiva roxburghii, HRBC Membrane stabilization, DPPH

ABSTRACT

Quinolines are a class of heterocyclic compounds, widely present in nature as quinoline alkaloids. Compounds having 2-quinolone moiety are associated with interesting biological activities such as antimalarial, tuberculostatic, antibacterial, antiviral, antifungal, anticancer, antidiabetic, cardiotonic and bronchodilator activity etc. The present work deals with the synthesis, characterization of substituted 7-amino-4-methyl-2-quinolone. The synthesized compounds were characterized by the IR, ¹H-NMR & Mass spectral studies. Out of 10 test compounds evaluated for their antibacterial activities, four test compounds 3,6,8 & 9 were found to be active against Bacillus subtilis while amoxycillin and gentamycin were used as standard.

Keywords: 2-quinolone; Schiff bases, antibacterial activity.

ABSTRACT

Peptic ulcer is the areas of degeneration and necrosis of gastrointestinal mucosa exposed to acid peptic secretion. Some other factors, such as inadequate dietary habits, excessive ingestion of non-steroidal anti-inflammatory agents, stress, hereditary predisposition and infection by Helicobacter pylori, may be responsible for the development of peptic ulcer. The several herbal formulations derived from Ayurveda and its additional systems of medicine, not yet to be scientifically validated that they have exhibited anti-ulcer activity. Our present study was to evaluate the ulcer protective activity of ethanolic extract of Gynocardia odorata (G.   ordata) seeds on cold restraint and ethanol induced ulcer model. Five groups were taken (n=6). First groups serve as negative control (Without any treatment). Second groups were treated with vehicles only. Third groups were treated with some standard marketed drugs (Ranitidine and sucralfate). Fourth and fifth groups were treated with ethanolic seed extract of G. odorata in two increasing dose (250 and 500mg/kg body weight p.o respectively). Both the group showed significant ulcer protective activity in a dose dependent manner.

Keywords: Gynocardia odorata, Cold restrain ulcer, Ethanol induced ulcer, Flavonoids. Ulcer  protective.

ABSTRACT

A potential mechanism of NSAID-mediated anti-proliferative activity may be through the induction of NAG-1. The present study was conducted to investigate the possible role of selective and non-selective COX inhibitors in inflammation associated angiogenesis and apoptosis. Wistar rats were classified into 5 experimental groups; 9 rats each. Group (1) normal control and group (2) injected s.c. with 0.3 % carrageenan in muscle. Groups (3, 4 and 5) were injected s.c. with carrageenan and at the same time given orally 10 mg/Kg Celecoxib, 12.5 mg/Kg Nimesulide or 10 mg/Kg Sulindac, respectively. NAG-1 gene expression in the liver was measured by RT-PCR. Serum TNFα and muscle caspase-3 were measured by ELISA.Immunohistochemical detection of VEGF in the muscle was investigated. Carrageenan untreated rats showed insignificant change in NAG-1 gene expression compared with control group. Serum TNFα and muscle caspase-3 as well as VEGF expression in carrageenan untreated group were significantly increased compared with normal control rats. In Sulindac treated group, NAG-1 gene expression in the liver and muscle caspase-3 were significantly increased compared with Celecoxib and Nimesulide groups. TNFα serum level was significantly decreased in Nimesulide and Celecoxib treated groups compared with carrageenan and Sulindac groups. The examined NSAIDs proved proapoptotic and antiangiogenic effects.

Keywords: NSAIDs,  NAG-1, Csapase-3,TNFα, carrageenan

ABSTRACT

The present study was carried out in fabricating gastro retentive formulation of an antipsychotic drug using semi synthetic and natural polymers. Floating tablets were prepared by direct compression method using directly compressible microcrystalline cellulose as vehicle. Gum Xanthan and hydroxypropyl methylcellulose (HPMC E4M) were used as polymers for sustaining the drug release and sodium bicarbonate was used as an effervescent agent. Tablets were characterized for their pre compression and post compression parameters. Floating characteristics like floating lag time, floating time were evaluated and were considered as one of the factor for selecting the best formulation. The in vitro release studies were carried out in pH 1.2 buffer for 8hrs. The content uniformity was found to be within the compendial requirements and the release was extended for more than 8hrs. The best fit release kinetics was achieved with zero order followed by higuchi and non-fickian diffusion. The release of Quetiapine fumarate was significantly influenced by the concentration of polymer.

Keywords: Gastro retentive floating tablet, HPMC, Quetiapine fumarate, Xanthan gum

ABSTRACT

In the present work ethylacetate and methanolic bark extract of Aegle marmelos(L) Correa, Alstonia scholaris (L)R.Br, Alstonia venenata (L)R.Br, Cyclea peltata (Lam) Hook .F.Thoms, Dilenia pentagyna Roxb, Macaranga peltata Roxb Mueller, Oroxylum indicum (L)Vent, Pterocarpus marsupium Roxb, Zanthoxylum armatum DC and Zizipus oenoplia (L) Mill, were tested against Trychophyton rubrum a clinical isolate from skin scrapings of Taenia Corporis  using Agarwell diffusion method and its minimal inhibition concentration (MIC) was also determined by Broth dilution method. Out of all the Methanolic bark extracts Oroxylum indicum Vent showed highest zone of inhibition followed by Alstonia venenata Linn, at 50 µgrams concentration. Clotrimazole was used as standard antifungal drug. MIC was found to be between 10µg - 1000µg per ml. Oroxylum indicum and Alstonia venenata showed MIC proportional to their zone of inhibition. Both bark extracts could be potential natural healing agents against Ringworm  or Taenia disease . Further investigation is needed to identify the compound which was present in both the plant barks to develop a novel drug.

Keywords : Antidermatophytic , Oroxylum indicum, Alstonia venenata, Trichophyton rubrum.

ABSTRACT

The present study was aimed at formulating and evaluating a herbal ointment comprising of Ethanolic extracts of the parts of morindacitrifolia, and rubiacordifolia. The parameters evaluated for wound healing were period of contraction and tensile strength using excision and incision models. The animals were divided into groups and were treated with herbal formulation, standard group and one served as control group.  Nitrofurazone (0.2% w/w) was used as reference standard. The period of epithelization in the excision wound mode was found to be 13.20 days, while in case of incision wound model the tensile strength was 540 when compared to the controls ,the results were  extremely significant. Different parameters like pH, viscosity, Spreadability and stability were evaluated. The formulation showed good spread ability, good consistency, homogeneity, there was no change in the appearance, pH, and no phase separation noticed at the end of the stability studies. There was no evidence of skin irritation. This study has revealed that the herbal ointment has shown the wound healing effect due to the synergistic activity of the phytoconstituents present in the extracts and may be used as potential herbal formulation for wound healing.

Keywords: morindacitrifolia, rubiacordifolia, Ethanolic extract, wound healing.

ABSTRACT

Heteroacyclic and Heterocyclic containing drugs showed remarkable and noticeable drug absorption, transmission and drug effects; hence they created their own identity and importance in pharmaceutical, medicinal, agricultural and drug sciences. Benzonido and pyridino, dithiazolo, quinolino and alkylamino heterocycles showed important applications in industrial, pharmaceutical, medicinal and drug chemistry.  Considering all these facts into consideration recently in this laboratory interaction of N-(7-chloroquinoline-4-yl)-N,N-diethyl-pentane-1,4-diamine (1) was carried out with thiourea (2) in ethanol medium to isolate N-(7-thiocarbamidoquinoline-4-yl)-N,N-diethyl-pentane-1,4-diamines (3). N-(7-thiocarbamido quinoline-4-yl)-N,N-diethyl-pentane-1,4-diamines on further interactions with various isothiocynates (4) in acetone-ethanol medium produces N-[7-(1- substituted) -2,4-dithiobiureto)-4-yl]-N,N-diethyl-pentane-1,4-diamine (5) which were successfully  oxidatively cyclised into N-[7-(5-substitutedimino-3-amino)-1,2,4-dithiazo-4-yl]-N,N-diethyl-pentane-1,4-diamine (6) these reactions are hither to unknown. The justification and identification of the structure of these newly synthesized compounds had been established on the basis of chemical characterization, elemental analysis and through spectral data.

Keywords: Substituted isothiocynates, N-(7-substitutedthiocarbamidoquinoline-4-yl)-N,N-diethyl-pentane-1,4-diamines, Green synthesis, bromine, acetone, ethanol and carbon tetrachloride.

ABSTRACT

The aim of the present work was to characterize the in vitro transdermal absorption of tramadol hydrochloride (TH) through pig ear skin. Studies of electrical and physicochemical factors acting on the permeation  kinetics of in vitro iontophoresis were performed. Iontophoresis increased the transdermal permeation flux of TH as compared to the diffusion. Increase in applied current density or enhanced the flux of the drug. Continuous current was more potent than pulsed current in promoting TH transdermal permeation. Increasing the frequency or on:off ratio of pulse current induced an enhancement of the flux through the skin. The binary system did not cause an enhancement in the permeation of TH compared to water alone. An increase in donor drug loading dose or increasing the duration of current application resulted in enhancement of the drug flux. Based on these results, and taking into account the pharmacokinetics of TH, therapeutic drug plasma levels could be achieved via transdermal iontophoresis using a reasonably sized (around 20 cm²) patch.

Keywords: analgesic; anodal iontophoresis; tramadol hydrochloride; transdermal delivery

ABSTRACT

The present study was conducted to demonstrate the clinically efficacy of few probiotic strains freeze dried in the laboratory in acute and chronic diarrhea. The strains used in the study were isolated from commercially available probiotics and identified in the laboratory and finally subjected to freeze drying in pure cultures. After freeze drying these probiotics were filled in capsule aseptically and given to the patients with acute and chronic diarrhea to demonstrate their clinical effectiveness. This was a blind placebo control study which included healthy volunteers as well. The effectiveness of the treatment was assessed by the recovery of the ailment and improvement of the symptoms associated with the illness. Dehydrated skimmed milk was used as placebo. From the result of clinical studies it can be concluded that probiotics make a significant alternate treatment to control acute diarrhea and improve chronic diarrhea.

Keywords: Probiotcs, acute and chronic diarrhea, strains, skimmed milk and placebo

ABSTRACT

The bacterial and fungal inhibitory efficiency of the Argemone mexicana Linn. (Papaveraceae) and Aerva javanica (Burm.f.) Juss. Ex. Schult. (Amaranthaceae) were evaluated against bacterial species like Staphylococus aureus, Streptococcus pyrogens, Klebsiella pneumonia and Escherichia coli and two fungal species such as Aspergillus niger and Penicillium notatum. The susceptibility of the microorganism to the extracts of these plants was compared with each other and with selected antibiotics. All these plants were effective against three of the pathogenic microorganisms. This in vitro study corroborated the antimicrobial activity of the selected plants used in folklore medicine.

Key words: Antibacterial activity, Antifungal activity, Disc diffusion method, Well diffusion method.

ABSTRACT

A number of resins (2,4DHAPDF) were synthesized by condensation of 2,4 dihydroxyacetophenone (2,4-DHA) and p-phenylenediamine (p-PD )with formaldehyde (F) in the presence of 2 M HCl as a catalyst with three different molar ratios of reacting monomers (1:1:2, 2:1:3, 3:1:4) at 130⁰C ±2⁰C. Resins have been characterized by elemental analysis, infrared (IR) spectroscopy and nuclear magnetic resonance (¹HNMR) spectroscopy and the morphology of the resin was examined by SEM technique. The number average molecular weight of the resin was determined by non –aqueous conductometric titration. The antimicrobial activities of the terpolymer were screened on various bacteria and fungi. All the synthetic terpolymer showed excellent antimicrobial activities with increasing molar ratios of reacting monomers.

Keywords:  Synthesis; Characterization; Molecular Weight; SEM; Antimicrobial activity.

ABSTRACT

Epilepsy is one of the most common chronic diseases of the nervous system. In recent years many plants have been tested for their Anti-epileptic properties. This study aims in evaluating the anti-epileptic activity of the Capsicum annuum and Sapindusemarginatus and a polyherbal formulation prepared by the combination of Capsicum annuum, Sapindus emarginatus, Withania somnifera, Hemidesmus indicus (Formepi-4). Study was carried out using albino mice (25 – 30 grams) 8-10 weeks old, of either sex. The animals were divided into five groups containing six animals in each group. The results for maximal electroshock induced seizures, pentylenetetrazole induced seizures and strychnine induced seizures were expressed as Mean ± Standard Error of Mean. Paired Student’s t-test was used to analyze the level of significance. Maximal electroshock induced seizures, Pentelenetetrazole induced seizures and strychnine induced seizures were significantly protected in mice by ethanolic extract of C.annuum, and Methanolic extract of S.emarginatus, with Formepi-4 showing a 100% protection. The alcoholic e xtract of fruits of Capsicum annuum and Sapindus emarginatus and polyherbal formulation (Formepi-4) possesses Anti-Epileptic activity against seizures induced by different mechanisms.

Keywords: Capsicum annuum, Sapindus emarginatus, Withania somnifera, Hemidesmus indicus, Anti- epileptic activity, Experimental animals

ABSTRACT

A study on pharmacokinetics of pefloxacin and kinetic interaction between pefloxacin (5 mg/kg) and meloxicam (0.5 mg/kg) was carried out through intravenous route in 5 female goats weighing 18-22 kg. A wash out period of 3 weeks was used before each injection. Blood (0.042-48 h) and urine (0.042-72 h) samples were collected. Estimation of pefloxacin and its active metabolite norfloxacin were carried out by using High Performance Liquid chromatography (HPLC). Shorter distribution half life (t_1/2 α) of 0.16 h and elimination half life (t_1/2 β) of 2.42 h were noted in pefloxacin alone administration and non-significant differences were noted in combination with meloxicam.  Significantly (P<0.05) longer t_1/2 β was obtained for norfloxacin in combined administration as compared to alone administration of pefloxacin. Significantly (P<0.05) lower total body clearance (Cl_B) of 5.92 ml/kg/min was obtained for norfloxacin in combined administration as compared to alone administration (16.62 ml/kg/min). Significantly (P<0.05) higher Vd_area of 0.98 L/kg was obtained in combined administration as compared to alone administration (Vd_area = 0.76 L/kg). This may be the reason that significantly (P<0.05) higher approximate tissue to plasma concentration ratio (T P) of 8.56 was noted for pefloxaxcin in combined administration as compared to alone administration (3.95). Significantly (P<0.05) higher % conversion of pefloxacin to norfloxacin (60.70) was noted in combined administration as compared to alone administration (22.34). Further, the calculated dosage regimen for maintaining minimum therapeutic concentration was found to be significantly (P<0.05) lower in combination as compared to alone administration.

Keywords: - Kinetics, Pefloxacin, Meloxicam, Goats

ABSTRACT

The main objective of current research work was to develop a stable pharmaceutically equivalent combined dosage form of immediate release Atorvastatin calcium and extended release Metoprolol succinate formulation, which is comparable to that of innovator’s. Combination therapy affords the physician and the patient the opportunity to more effectively treat diseases that may stem from more than one cause. When used correctly and appropriately, combination therapy leads to better outcomes than mono therapy by treating more than one cause of the disease and/or by synergistically enhancing the action of one of the component drugs. The purpose of the study was to develop a capsule of Atorvastatin calcium (IR) and Metoprolol succinate (ER) having different release pattern, which is indicated for the management of hypertension. The study was planned in three stages. In the first stage three batches (A1, A2, and A3) of immediate release blend of Atorvastatin calcium was prepared using pre-gelatinized starch as super disintegrate. In the second stage, nine batches (M1-M9) of Metoprolol succinate sustained release pellets were prepared using various polymers and levels of coatings as rate retardants. Preformulation studies were performed after granulation. In the third stage capsules were evaluated for weight variation, drug content, and disintegration time and in vitro drug release using RP-HPLC. FTIR studies revealed no disturbances in the principle peaks of pure drugs and it confirms the integrity and compatibility of pure drugs with their excipients.

Keywords: Atorvastatin calcium, Metoprolol succinate, Coating, Pellets and HPLC.

ABSTRACT

In this paper the authors proposed a simple, sensitive and selective liquid chromatography–tandem mass spectrometry (LC–MS/MS) assay method for the determination of darifenacin in human plasma. This method employed solifenacin as an internal standard (IS). Analyte and the IS were extracted form 200 µL of human plasma using protein precipitation technique. The chromatographic separation was achieved on a C₁₈ column by using a mixture of acetonitrile and 5mM ammonium formate in 0.01% formic acid (90:10, v/v) as the mobile phase at a flow rate of 1.0 mL/min. The linearity of the method was established in the concentration range 0.05–20.5 ng/mL with r² ³ 0.99. The intra–day and inter–day precision (%CV) and accuracy results in three validation batches across five concentration levels were well within the acceptance limits. The validated method was successfully applied to a pharmacokinetic study in humans under fasting condition with 15 mg darifenacin extended release tablet.

Keywords: Darifenacin, Human plasma, Protein precipitation (PP), LC–MS/MS, Pharmacokinetics

ABSTRACT

A simple, sensitive, accurate, precise and economical visible spectrophotometric method was developed and validated for the estimation of lurasidone Hydrochloride in synthetic mixture. The method is based on the reaction of lurasidone Hydrochloride with bromocresol green dye in dichloromethane giving yellow color chromogen, which shows maximum absorbance at 418 nm against reagent blank. The chromogen obeyed Beer’s law in the concentration range of 4-12 µg/ml for lurasidone Hydrochloride. The results of the analysis have been validated statistically and by recovery studies.

Keywords: Lurasidone Hydrochloride, Chromogen, Bromocresol green, Visible spectrophotometric.

ABSTRACT

Mucuna pruriens commonly known as cowhage plant has been claimed to possess various beneficial effects like anti-parkinsonian, anti-tumor, neuroprotective, antioxidant, anti-diabetic and antidepressant activities. Previous studies have reported that Mucuna pruriens contains L-DOPA and 5-hydroxy tryptophan (5-HT) as a major constituent with higher concentration in seeds. However, literature search revealed no scientific data on its anxiolytic activity. So the present study was designed to evaluate the anxiolytic activity of Mucuna pruriens in a murine model. Wistar albino rats were divided into five groups (n=6). Mucuna pruriens administered at doses of 250,500,750mg/kg/day orally, was compared with the standard drug Diazepam (1.0mg/kg/day, oral) fed for 14 days. Three pharmacologically validated models elevated plus maze, bright and dark arena and open field test were used. The data presented was analyzed using one way ANOVA followed by Dunnett’s post hoc test. A value of p<0.05 was considered as statistically significant. Mucuna pruriensat all three doses used significantly reduced the time spent in closed arm, increased the entries into open arm in elevated plus maze (p < 0.05). In bright & dark arena model, there was an increase in number of entries, time spent in bright chamber (p < 0.05) and in  open field test, the time spent and squares crossed in central chambers were increased (p < 0.05). To conclude, the present study demonstrates the anxiolytic activity of chronic administration of Mucuna pruriens in Wistar Albino rats.

Keywords: Anxiolytic, Mucuna pruriens, diazepam, elevated plus maze, bright & dark arena model, open field test.

ABSTRACT

Alprazolam (ALP) is benzodiazepine derivative which produce symptomatic relief of anxiety and tension state resulting from a stressful enviourment or emotional factors. The First method was based on simultaneous equation method.  In the proposed simultaneous equation method, the signals were measured at 222.0 nm and 227.0 nm corresponding to the absorbance maxima of ALP and FLU in methanol.  The method was validated statistically.  Recovery study was performed to confirm the accuracy of the method.  This method is suitable technique for the reliable analysis of commercial formulation containing combination of ALP and FLU.  Simplicity, sensitivity and rapidity of simultaneous equation method render it suitable for routine analysis for ALP and FLU from their combination dosage forms. The Second method was based on absorbance ratio method (Q. analysis).  The absorbance was measured at two-wave lengths 222.0 nm (max) of ALP and 227.0 nm, which is an isoabsorptive point, were found adequate for quantification.  The method is validated statistically. The recovery more than 99% with low SD suggests the accuracy of the method. In addition, the above-proposed UV spectroscopic methods are simple, easy to apply, low cost, does not use polluting reagents and requires relatively inexpensive instruments.

Keywords - Alprazolam; Fluoxetine; Anxiety, Isoabsorptive

ABSTRACT

To evaluate the effect of methanolic extract of leaves of Ocimum gratissimum linn. on neutrophil phagocytic function. Were we used different concentrations (50,100,200μg/ml) of methanolic extract of Ocimum gratissimum was subjected to study its effect on different in-vitro methods of phagocytosis. such as neutrophil locomotion, chemotaxis, immunostimulant activity of phagocytosis of killed Candida albicans and qualitative Nitro Blue Tetrazolium test using human neutrophils. This preliminary study revealed that Ocimum gratissimum extract has stimulated chemotactic, phagocytic and intracellular killing potency of human neutrophils at the different concentration. From the results obtained it can be observed that the methanolic extract of Ocimum gratissimum leaves stimulates cell-mediated immune system by increasing neutrophil function phagocytic activity.

Keywords: Immonostimulant activity, Ocimum gratissimum, neutrophils, Phagocytosis.

ABSTRACT

The objectives of this study were to maximize; a) the in vitro transcorneal release, b) the IOP-lowering effect and, c) the duration of action, of Latanoprost acid (LAT) ophthalmic gels. The in vitro transcorneal release of LAT from a 1^st set of gel formulations that containing different concentrations of Azone^™ (as enhancer) with fixed concentration of C-974^® (as mucoadhesive) were studied. Formulation that showed greatest permeability parameters at lowest Azone^™ concentration was selected for preparation of a 2^nd set of ocular gels containing various C-974^® concentrations. The in vitro transcorneal release was assessed, and the best C-974^® concentration required for preparation of formulations that can be conceded as ideal ophthalmic LAT gels hve been pinpointed and scaled up for in vivo IOP-lowering efficacy study using TONO-PEN^™ AVIA tonometer in rabbits for 4-consecutive days.  Various test formulations have showed significant but varied augmentations in both, in vitro and in vivo results. Formulations (GAZ-4) & GC-4 have shown the highest therapeutic IOP lowering effects; i.e., (7.8±1.8), (6.5±2.1), respectively. Particularly noteworthy with both formulations the IOP base-line didn’t re-established after 24 hours, and their durations of action in the single-dose study were 47±2.25, and 48±1.5, respectively. The in vitro release, onset, magnitude & duration of action of action of LAT gels have been enhanced and extended for up to 2-day with two gel formulations.  Nonetheless, the success in developing a novel ophthalmic formulation depended for great extent upon the crucial net outcomes of a very sensitive interplay/balance between the drug and additives.

Keywords: Azone; Corneal transport; Ocular delivery; Ocular enhancers; Carbopol-974; Glaucoma; IOP lowering effect; Mucoadhesive

ABSTRACT

Indomethacin-loaded nanoparticles (IMC-NPs) were obtained by emulsifier-free radical polymerization of vinyl acetate (VAc) in the presence of indomethacin (IMC) in the aqueous solution of Carbopol® (Cbp) or chitozan (CH). The purpose of this study was to investigate the influence of nature and quantity of the added to the reaction system polymer on IMC loading and its kinetic release properties in terms of the future development of topical ophthalmic formulations. CH was chosen as a cationic polysaccharide and Cbp as an anionic crosslinked polymer. TEM and DLS were used to observe the morphology and to determine the average particle size which was in the range of 178.20÷297.90 nm and the polydispersity index (PDI) which was within 0.149÷0.339. A monomodal particle size distribution (PSD) was observed for the CH-coated NPs and bimodal PSD was observed in the models, obtained in the presence of Cbp. FTIR analysis showed that the models were a result of interactions with hydrogen bonds. UV-spectroscopy was used for the determination of IMC inclusion and in vitro release characteristics. The results of release kinetic analyses showed that IMC was released from the investigated models following the first order. The polymer shell (Cbp or CH) around the pVAc–core had an impact on the rate and degree of the released drug.

Keywords: Indomethacin-loaded nanoparticles, radical polymerization, polymer coated nanoparticles, carbopol coated nanoparticles, homopolymers of vinyl(acetate)

ABSTRACT

Fructose consumption from sucrose and high-fructose corn syrup have Increased both plasma insulin and leptin act in the central nervous system in the long-term regulation of energy homeostasis. Because fructose does not stimulate insulin secretion from pancreatic β cells, the consumption of foods and beverages containing fructose produces smaller postprandial insulin excursions than does consumption of glucose-containing carbohydrate. Because leptin production is regulated by insulin responses to meals, fructose consumption also reduces circulating leptin concentrations. The combined effects of lowered circulating leptin and insulin in individuals who consume diets that are high in dietary fructose could therefore increase the likelihood of weight gain and its associated metabolic sequelae. In addition, fructose, compared with glucose, is preferentially metabolized to lipid in the liver. Fructose consumption induces insulin resistance, impaired glucose tolerance, hyper insulinemia, hyper triacylglycerolemia, and hypertension in animal models. The data in humans are less clear. Although there are existing data on the metabolic and endocrine effects of dietary fructose that suggest that increased consumption of fructose may be detrimental in terms of body weight and adiposity and the metabolic indexes associated with the insulin resistance syndrome, much more research is needed to fully understand the metabolic effect of dietary fructose in humans. We investigated the effects of NCE-9 on fructose-induced hypertriglyceridemia and liver steatosis in rats. NCE-9 reduced serum TG and VLDL levels and also improve glucose intolerance in fructose-fed rats. This PTP1B inhibitory property may be a promising therapeutic strategy for NCE-9 to treat fructose-induced hepatic steatosis.

Keywords: NSE-9, Protein tyrosine phosphatase 1B , Insulin resistant, High Fructose Fed, rat, Hypertriglyceridemia, Hepatic Steatosis

ABSTRACT

Two simple, accurate, precise, reproducible, requiring no prior separation and economical procedures for simultaneous estimation of difluprednate and moxifloxacin hydrochloride in combined dosage form have been developed. First method employs formation and solving of simultaneous equation using 241nm and 288 nm as two analytical wavelengths for both drugs in distilled water. The second method is a Q value analysis based on measurement of absorptivity at 241nm and 264nm (as an ISO-absorptive point). Difluprednate at their respective λmax 241 nm and 288 nm and at iso-absorptive point 264 nm shows linearity in a concentration range of 10-20 μg/mL and similarly moxifloxacin at their respective λmax 288 nm and 241 nm and at iso-absorptive point 264 nm shows linearity in a concentration range of 1-5 μg/mL. The results of the analysis have been validated statistically.

Keywords Difluprednate, Moxifloxacin, UV spectroscopy, Simultaneous equations, Q – analysis

ABSTRACT

H₂O-mediated efficient, tandem synthesis of barbituryl thiocarbamides by the nucleophilic addition reaction of uramil and aryl isothiocyanates using Amberlyst-15 as a heterogeneous solid catalyst is being reported. The novel and clean methodology offers the advantages that includes short reaction time, good yields, and operational simplicity, less leaks, environmentally benign procedure apart from recyclable, reusable catalyst.

Keywords; Thiocarbamides, green synthesis, Amberlyst-15.

ABSTRACT

Breast cancer is one of the most serious problems in oncology. It is a leading cause of death among women in many countries. Environmental factors, of either biological or chemical origin, may act as initiators and promoters of  the carcinogenesis. Chemical carcinogens such as 7,12-dimethylbenz[a] anthracene [DMBA],benz[a]pyrene [BP], and N-nitroso-N-methylurea are commonly employed to initiate and promote neoplastic transformation in experimental animals. DMBA is well established as a highly potent carcinogen. Cancer chemoprevention is recognized as the most promising and novel approach to prevent, inhibit or reverse the carcinogenic processes by intervention with natural products or synthetic chemical substances. Taurine is a sulfur containing beta amino acid with a wide range of vital, biological functions, ranging modulation, cell membrane stabilization to bearing an antioxidant and scavenging agent. In from neuro the last decade it has been widely used in the field of oncology as a chemo protective agent against hepatocarcinogenesis and colon carcinogenesis. The aim of this study was to get insight into the process of chemo resistance acquisition for a better understanding of the breast cancer therapy. Therefore, the current study has been undertaken to examine the effect of taurine on DMBA induced breast cancer in rats. At the end of the experimental period, the homogenized breast tissue was investigated and recorded the body weight, tumor weight and antitumor activity of Taurine in the experimental rats. Overall, these results suggested that the taurine treatment provided antioxidant defense with strong chemopreventive activity against the genesis of DMBA-induced mammary carcinoma.

ABSTRACT

Synthesis of silver nanoparticle (SNP) has become an emerging trend in the field of nanotechnology. Here a greener method was approached to develop silver nanoparticles using extracted exopolysaccharides (EPS) from Pseudomonas fluorescens, a soil isolate from rhizosphere of the medicinal plant, Catharanthus roseus. The exopolysaccharide acted as a reducing and stabilizing agent in converting silver nitrate to silver nanoparticles. The fabricated SNPs were characterized by UV-Visible Spectroscopy, Scanning Electron Microscopy (SEM) and FT-IR Spectroscopy. The FT-IR analysis revealed that proteins present in the polysaccharide served as a capping agent. This simple process was carried out for 5 days at room temperature at optimum pH 7. The dried SNP sample is found to be stable for more than 6 months. The present work also focused on SNPs’ antimicrobial effect by agar well diffusion technique and antioxidant activity by DPPH method. The EPS reduced SNP was found to be more active against Gram negative than Gram positive and also worked in inhibiting Candida sp. DPPH radical scavenging effect of SNP was highly effective than standard at a maximum concentration of 1mg/ml. The investigation thus showed that EPS stabilized SNP could be employed in several pharmaceutical purposes.

Keywords: Pseudomonas fluorescens, exopolysaccharide, silver nanoparticle, SEM, EDS, Agar diffusion, DPPH scavenging activity

ABSTRACT

This investigation deals with the formulation of sustained release niosome based system of silver sulfadiazine for the treatment of burn and thereby decreasing the dosing frequency which is really important for severe burn patient as every reapplication is very painful to them. In this investigation, the effect of different processing variables on entrapment efficiency of drug was evaluated. The vesicle size, photomicroscopy, in vitro release, scanning electron microscopy, stability and in vitro antimicrobial activity of niosomal vesicles formed were also characterized. Niosomes were developed from span 60 and cholesterol in different molar ratio by ether injection, thin film hydration and non solvent methods. Results indicated that the niosomes manufactured with span 60 and cholesterol in 50:50 molar ratio using 100mg of drug by thin film hydration method gives highest entrapment of 92.11%. The method of preparation and contents of cholesterol as well as drug were found to affect the entrapment. The optimized niosomal formulation exhibited significantly retarded in vitro release of 98.04% over 28 hours by a higuchi controlled mechanism. The in vitro antimicrobial study using Staphylococcus aureus revealed that niosomal formulation of silver sulfadiazine shows better zone of inhibition (18mm) in comparison to conventional dosage form (17mm). In conclusion this study showed that the niosomal formulation can be used as promising sustained release approach for the topical delivery of silver sulfadiazine in the treatment of burn.

Keywords: Silver sulfadiazine; Antimicrobial study; Burn; Entrapment efficiency; Span 60

ABSTRACT

Flavones, have been synthesized by the oxidative cyclization of 2'-hydroxychalcones using catalytic amount of iodine in presence of dimethyl sulfoxide (DMSO) in maximum yield. The synthesized compounds were evaluated for anti-oxidant and anti-inflammatory potential. Two compounds showed good anti-inflammatory activity as compared to their antioxidant activities. The synthesized compounds were characterized by IR, ¹HNMR and MS Spectroscopy.

Keywords: Flavones, anti-oxidant, anti-inflammatory, oxidative-cyclization, DMSO.

ABSTRACT

The aim of present study was to design and development of a proniosomal transdermal drug delivery system of lornoxicam for the treatment of rheumatoid arthritis and enhanced skin targeting effect, sustained & prolonged drug release, enhanced skin bioavailability by using different type of non ionic surfactant & cholesterol. Proniosomes of Lornoxicam were prepared by coacervation-phase separation method. The formulation systems were characterized in vitro for size, vesicle count, drug entrapment, drug release profile and vesicular stability. The method used for preparing proniosome resulted in an encapsulation yield of 67.71-87.64%. Proniosomes were characterized by transmission electron microscopy. In vitro studies showed prolonged release of entrapped lornoxicam. A successful attempt was made to develop proniosomal gel for transdermal delivery of lornoxicam using different grades of nonionic surfactant.

Keywords: Proniosomes, Niosomes, skin penetration, stability, transdermal, coacervation.

ABSTRACT

The objective of this study was to assess the drug utilization pattern and cost analysis among the inpatients of medical intensive care unit (ICU) of NIMS hospital, Jaipur. After taking Ethics permission , records of 356 patients admitted in the medical ICU of a NIMS hospital were noted. Demographic profile, commonly prescribed drugs as per Anatomical Therapeutic Chemical Classification (ATC) and WHO core indicators were assessed from the records. Out of 356 inpatients, 224(62.9% ) were males . Most of the patients were in the age group of 61-70 for males 51-60 for females. Most commonly prescribed drugs were antibiotics followed by i.v. fluids. The average number of drugs per prescription was 11.99. Out of 4271 drugs prescribed, 1152(26.97%) were prescribed by generic names. Drugs on WHO EML were only 41% while that of NLEM 2011 were 68% . Drugs used as fixed dose combination were 19.26%. Average cost per prescription was INR 1975. Median length of stay was 6 days. Inspite of the fact that respiratory complications are one of the leading cause of death in critically ill patients and rational drug use plays a pivotal role in reverting the condition , there is a lack of pioneer drug utilization studies in this field. This study gives a message to adopt a cost effective and rational use of drug.

Keywords: Drug utilization studies, rational use of drugs, ATC code.

ABSTRACT

Simple, sensitive and accurate spectrophotometric method  has been developed for sequential separation of Co ^II,Ni^II and Pb^II with α-oximinoacetoacetaanilidebenzoylhydrazone(HINABH). HINABH forms Yellowish brown  complex with Co ^II and yellow colored complexes with Ni^II and Pb^II.Co^II-HINABH complex was extracted in to n-butanol  in the pH range 6.0-7.0 at λ max 425 nm., whereas Ni ^II and Pb^II complexes were extracted into isoamylalcohol quantitatively in the pH range 8.5-9.5 at λ max 420nm and 410 nm respectively. HINABH complexes of Co ^II,Ni^II and Pb^II obeyed Beer’s law in the range of 0.2-5.0 ppm,1-14 ppm and 2-16 ppm respectively. The method had been successfully employed for the determination of Co ^II,Ni^II and Pb^II in the synthetic mixtures and alloys.

Keywords: Spectrophotometric determination, α-oximinoacetoacetaanilidebenzoylhydrazone, cobalt, nickel and lead samples.

ABSTRACT

Aim of the present work was to formulate and evaluate an oral, time controlled drug delivery system to achieve timed release of Montelukast sodium, for the treatment of nocturnal asthma. An asthmatic attack mainly takes place early in the morning. Time controlled delivery system is capable of delivering drug when and where it is required most. Time-delayed tablets, designed to release drug after a predictable lag time, are intended for oral chronotherapy. A time dependant pulsed release system consisting of a core surrounded by coat layer of different ratios of swellable erodible hydrophilic layer HPMC K100M and rupturable hydrophobic layer Eudragit L 100 and Eudragit S 100 were prepared. These pulsatile tablets were evaluated for the drug content, thickness and in-vitro release profile, etc. and  two optimized formulation were selected and subjected to further studies. .

Keywords: Pulsatile drug delivery ,time controlled drug delivery; Chronotherapeutics; Circadian rhythm; Nocturnal asthma; Montelukast sodium; Eudragit L 100:Eudragit S 100; HPMC K100M.

ABSTRACT

Screening and expression of protease producing 5 strains of Alternaria sp. were obtained from the various places in Chennai, Vellore, Tamilnadu, India. The isolates were positive on tyrosin caesin nitrate agar (1%) and thus are selected as protease producing strain. The microbial growth is revealed by the mycelial dry weight determination. Maximum growth is observed in the case of Alternaria tenuis (0.47 mg). Equally, the maximum growth is observed in Alternaria solani (0.45 mg). Total protein was determined using BSA as standard. Proteinase activity was estimated using casein as the substrate. Finally the enzyme protease was purified by column chromatography. The protein was characterized using SDS-PAGE. Maximum protein content is observed in the case of Alternaria triticola (0.902 mg) and Alternaria triticina (0.753 mg). Maximum proteinase content  is observed in Alternaria triticina  (0.591 mg). This results showed that microbes under study is a good producer of extra cellular protease, which can be beneficial for industries.

Keywords: Mycelial dry weight, Alternaria, chromatography, protein content, Proteinase.

ABSTRACT

The present study was undertaken to develop and validate a simple, accurate, precise, reproducible and cost effective UV-Visible spectrophotometric method for the estimation of cefpodoxime proxetil in bulk and pharmaceutical formulation. The solvent used throughout the experiment was methanol and water. Absorption maximum (λ_max) of the drug was found to be 231 nm. The quantitative determination of the drug was carried out at 231 nm and Beer’s law was obeyed in the range of 5-25μg/mL. The method was shown linear in the mentioned concentrations having line equation y = 0.0331x + 0.0151 with correlation coefficient R²of 0.9998. The recovery values for cefpodoxime proxetil ranged from 99.80% - 100.02%.The percent relative standard deviation (RSD %) of interday precision range was 0.118 – 0.181% and intraday precision range was 0.139 – 0.446%. The limit of detection and limit of quantification was 0.081μg/mL and 0.121μg/mL. The percent relative standard deviation of robustness and ruggedness of the method was 0.126 – 0.313%.Cefpodoxime proxetil content in two pharmaceutical dosage forms (tablet and suspension) were determine which were in good agreement with the label claims with RSD value of 0.02% for tablet and 0.01% for suspension. Hence, proposed method was precise, accurate and cost effective. This method could be applicable for quantitative determination of the bulk drug as well as dosage formulation.

Keywords: UV-Vis Spectrophotometer, Method Validation, Recovery studies.

ABSTRACT

The aceclofenac sodium loaded calcium alginate (CA) based microbeads prepared by ionotropic external gelation technique with calcium chloride as cross-linking agent. Calcium alginate microbeads represent a useful tool for oral sustained/ controlled drug delivery but show several problems, mainly related to the stability, and rapid drug release at higher pH that, in most cases, is too fast due to increase porosity. To overcome such inconveniences, which was to develop CA microbeads coated with xyloglucan (XG) as drug release modifier to improve stability and prolong the drug release. The mean particle sizes of drug-loaded microbeads were found to be in the range 476.45±12 to 765.10 ± 0.22. The drug entrapment efficiency was obtained in the range of 62.24±0.66 to 102.75 ± 0.87.The shape and surface characteristics were determined by scanning electron microscopy (SEM). No significant drug-polymer interactions, physical changes and crystallinity of the drug in the formulations were determined by FT-IR spectroscopy, differential scanning calorimetry (DSC) and X-ray powder diffraction [XPRD]. In-vitro drug release profiles of microbeads were pH dependent and were analyzed by different kinetic models. The mechanism of drug release from microbeads depends on swelling and erosion process resulting CA microbeads was diffusion controlled followed by First order kinetics and whereas CA microbeads coated with XG approaching to near Zero- order kinetics.

Keywords: Sodium alginate, Xyloglucan aceclofenac sodium, Oral bioavailability, Natural hydrogels, pH dependent, Zero-order kinetics

ABSTRACT

A facile synthesis of 1,4-bis-(6-arylimino-[1,2,4]-triazolo-(3,4-b)-[1,3,4]-thiadiazol-3-yl)-benzenes have been carried out by reacting 1,4-bis-(4-amino-3-mercapto-4H-[1,2,4]-triazol-5-yl-benzene with N-aryl isocyanodichlorides followed by the basification with dilute ammonium hydroxide solution. 1,4-bis-(4-amino-3-mercapto-4H-[1,2,4]-triazol-5-yl-benzene was synthesized by the interaction of terephthalic acid dihydrazide with carbondisulphide and potassium hydroxide followed by the addition of hydrazine hydrate. The acetylation of bis-triazolo-dithiadiazines afforded di-acetyl derivatives. The structures of synthesized compounds have been established on the basis of chemical transformation, elemental analysis, equivalent weight determination and IR, ¹H-NMR, mass spectral studies. The title compounds have been assayed for their antimicrobial activity against gram-positive as well as gram-negative micro-organisms.

Keywords: Synthesis; antimicrobial screening; novel bis-triazolo-thiadiazoles.

ABSTRACT

A series of chalcones was synthesized by the Claisen-Schmidt condensation and the structures of 1-(4-bromophenyl)-3-phenylprop-2-en-1-ones were established with the help of IR and NMR study, then their effect was observed on bovine serum albumin. We have found that the synthesized chalcones interacted with bovine serum albumin irrespective of position and nature of substituent. 1-(4-bromophenyl)-3-(3-methoxyphenyl)-prop-2-en-1-one has been found to interact with BSA maximally.

Keywords: Bovine serum albumin, interaction studies, chalcones of p-bromoacetophenone.

ABSTRACT

The hepatoprotective effects of Methanolic Extract of Justicia Beddomei (MEJB)on Isoniazid and Rifampicin (INH and RIF) induced hepatotoxicity and the probable mechanism(s) involved in this protection were investigated in rats. Male wistar rats were divided in to five groups and used for the study. Hepatotoxicity was induced in animal models and was compared with the protective effect of standard drug Silymarin. In the present study it was noted that the administration of INH, Rifampicin decreased the level of total protein, albumin and increased the level of liver enzymes AST, ALT, ALP and TC. These parameters were brought back to the near normal level in control group treated with MEJB. The histopathological studies also revealed that treatment with Methanolic Extract of Justicia Beddomei (MEJB) showed a protection against injuries due to the effect of INH, Rifampicin. These results suggets that MEJB showed significant hepatoprotective activity against Isoniazid and Rifampicin induced hepatotoxicity and this might be due to the presence of flavanoids and phenolics. Further research is sought to explore the mechanism of action and phytoconstituents responsible for the pharmacological action.

Keywords:- INH ,Rifampicin, Hepatoprotective, Justicia Beddomei

ABSTRACT

A series of chalcones was synthesized by the Claisen-Schmidt condensation and the structures of 1-(4-bromophenyl)-3-phenylprop-2-en-1-ones were established with the help of IR and NMR study, then their effect was observed on bovine serum albumin. We have found that the synthesized chalcones interacted with bovine serum albumin irrespective of position and nature of substituent.  1-(4-bromophenyl)-3-(3-methoxyphenyl)-prop-2-en-1-one has been found to interact with BSA maximally.

Keywords: Bovine serum albumin, interaction studies, chalcones of p-bromoacetophenone.

ABSTRACT

Verapamil hydrochloride has a short half-life 2.8 to 7.4 hours, a narrow absorption window and is mainly absorbed in proximal areas of GIT. The present investigation aimed to formulate a floating drug delivery system of Verapamil Hydrochloride by Quality by design approach. In risk assessment, the effects of process and formulation variables on particle drug release and floating lag time were investigated. Design of experiments (DoE) and multivariate data analysis were used to identify important process and formulation parameters. A 2² factorial design in replicate was employed to produce controlled release floating tablet. The effect of critical formulation variables i.e. levels of HPMC K15M and gas generating agent (i. e. Sodium bicarbonate and citric acid) on % Drug release after 12 hr (% DRel₁₂) and floating lag time (FLT) were analyzed. Verapamil HCl tablets were evaluated for hardness, friability, weight variation, drug content, floating behavior and drug release studies were conducted in 0.1 N HCl (pH 1.2) at 37 ± 0.5^OC. The tablets showed acceptable physicochemical properties. The two independent variables studied exhibited a significant influence (P < 0.05) on % DR 12 Hr and FLT. Numerical and graphical optimization technique employing design space approach was used to develop a new formulation by setting constrains on the dependent and independent variables. The experimental values of % DR 12 Hr and FLT for optimized batch were found to be in close agreement with those predicted by mathematical model. Experimental values obtained from the optimized formulations were in both cases close to the predicted values, thus confirming the validity of the generated mathematical model. These results demonstrated the effectiveness of the proposed floating tablet, as well as the usefulness of the QbD approach for the development of Verapamil floating tablet with optimized properties.

Keywords: Floating drug delivery system, Quality by design, Verapamil Hydrochloride, HPMCK15M, factorial design, Design space.

ABSTRACT

In recent year there has been rapid increase in the standardization of selected medicinal plant of potential therapeutic significance. The rhizome of Curcuma longa reported to have good medicinal values in traditional system of medicines. The present study deals with pharmacognostic parameters for the rhizomes of Curcuma longa which mainly consist of Macromorphology, Physico-chemical constants and Phytochemical screening. This information will be used for further pharmacological and instrumental evaluation of the species and will assist in standardization for quality, purity and sample identification. Physicochemical parameters such as total ash value, acid insoluble ash value and water soluble ash value were determined which were 14.69, 1.20 and 4.12% w/w respectively. The alcohol soluble extractive and water soluble extractive were also determined. Preliminary phytochemical analysis of ethanol extract was carried out. The results were positive for steroids terpenoids, phenols, tannins and flavonoids. HPTLC analysis confirms the presence of Curcuminoids. These secondary metabolites were the active constituents of Curcuma longa Linn. that may be responsible for its pharmacological activities.

Keywords: Curcuma longa, Curcuminoids, Rhizome, Physicochemical constants.

ABSTRACT

The study was designed to determine the in-vitro antibacterial and cytotoxic activities of methanolic extract of Melia azedarach leaves.  Dried powder of leaves of Melia azedarach was extracted with methanol. The Melia azedarach extract was assayed for antibacterial and cytotoxic activities using agar well diffusion technique and brine shrimp lethality test, respectively. The methanolic extract of Melia azedarach showed moderate antibacterial activity against three bacterial strains such as Bacillus subtilis, Escherichia coli and Staphylococcus aureus. The methanolic extract of the plant exhibited strong cytotoxicity in the brine shrimp lethality bioassay test. These results indicated the use of Melia azedarach to treat infections with emphasis to isolate and characterize the active principle responsible for antibacterial and cytotoxic activities and its exploitation as therapeutic agent.

Keywords: Melia azedarach, antibacterial activity, cytotoxic activity, brine shrimp lethality test.

ABSTRACT

This dissertation describes the biological investigations of Diospyros peregrina gurke; a plant belonging to the family Ebenaceae.Present study was designed to test the cytotoxic activity and antimicrobial effect of crude extract. The study protocol consists cold extraction of powdered unripe fruit and seed of Diospyros peregrina gurke for cytotoxicity effect using Brine shrimp bioassay lethality and tested against four Gram negative and three Gram positive bacteria for antimicrobial activity. From the results of the brine shrimp lethality bioassay it can be well predicated that crude extracts of Diospyros peregrina gurke possess cytotoxic principles (with LD₅₀  9.12011µg/ml and 10.8893µg/ml).For antimicrobial activity, the extracts were tested against standard microbial strains of gram positive and gram-negative, by means of Agar-Disc Diffusion Method and minimum inhibitory concentration (MIC) was noted.Although, both extracts were found to be effective in inhibiting pathogens to varying degrees to the tested organisms, the unripe fruit pulp extract of Diospyros peregrina gurke was found to be more effective than seed extract of Diospyros peregrina gurke .When both extracts were used in combination, they have shown strong synergistic effect against all the pathogens tested in the present study. Plant extracts  can be used to source antitumor and antibiotic substances for possible treatment.

Keywords: Cytotoxicity, synergism effect, antimicrobial, Diospyros peregrina gurke,deshi ghab, Gaub persimmon .

ABSTRACT

Liver plays a major role in detoxification. Any injury to it or impairment of its function may lead to many implications on one’s health. Management of liver diseases is still a challenge to modern medicine. The allopathic medicine has little to offer for the alleviation of hepatic ailments whereas the most important representatives are of phytoconstituents. The work presented in this paper is on plant Limnanthemum indicum which is reported that the whole plant is traditionally used as hepatoprotective. The study was aimed at evaluation of the hepatoprotective activity of the whole plant of Limnanthemum indicum on the BRL3A (Rat, Liver cell line) cell line. The various solvent extracts were tested for its inhibitory effect on BRL3A (Rat, Liver cell line) cell line. The percentage viability of the cell line was carried out. The cytotoxicity of Limnanthemum indicum on rat liver cell was evaluated by the MTT assay [(3-(4,5 dimethylthiazole –2 yl)-2,5 diphenyl tetrazolium bromide) assay]. The principle involved is the cleavage of tetrazolium salt MTT into a blue coloured derivative by living cells which contains mitochondrial enzyme succinate dehydrogenase However, the information available on the pharmacological activity of the plant is very limited. Hence, it was proposed to carry out a preliminary in vitro analysis of the hepato protective activity of the plant. Out of the various extracts evaluated, ethanolic extract of Limnanthemum indicum gave promising results.

Keywords: Hepatoprotective, Rat liver cell line, MTT, Mitochondrial

ABSTRACT

Streptococcus gordonii are one among the early colonisers of tooth surfaces of humans and are present in coronal plaque, gingival crevices and buccal and pharyngeal mucosal surfaces. One of the main virulence factor that is involved in S. gordonii adhesion and coaggregation is ScaA protein. Inactivation of scaA genes resulted in both impaired growth of cells and inhibition of Mn2+ intake. Thus the inhibitors of ScaA protein can act as an effective drug against S. gordonii especially in the prevention and treatment of infective endocarditis and dental caries. The three dimensional structure of ScaA protein is predicted by homology modelling. It is the method to determine 3D structure of protein with the help of 3D structure of homologous proteins. Softwares used are Modeller 9.11 and Easy modeller 2.0 GUI. A total of 500 ligands in 2D format were derived from myricetin with the help of software ACD chemsketch. Rapid virtual screenings of these compounds were performed in the docking tool iGEMDOCK v2.0. Based on the binding energy a total of three ligands were selected for the further study. Three ligands thus generated possessed very good docking energy. Thus three ligands with good inhibitory properties were generated among which 5-[3,4-dihydroxy-6-(pyridin-2-yl)-8aH-chromen-2-yl]benzene-1,2,3-triol, a novel compound is found to be very excellent drug candidate based on the molecular docking studies and its ADME properties.

Keywords: Streptococcus gordonii, ScaA protein, homology modelling, molecular docking, drug candidate

ABSTRACT

Fe(II) complexes [Fe(mqs)(B)₂](PF₆)(1)-(3) of  2-thiol 4-methylquinoline and phenanthroline bases (B), viz 1,10-Phenanthroline (phen in 1), Dipyrido[3,2-d:2',3'-f]quinoxaline (dpq in 2) and Dipyrido[3,2-a:2′,3′-c]phenazine (dppz in 3) have been prepared and characterized. The DNA-binding behaviors of these three complexes were investigated by absorption spectra, viscosity measurements and thermal denaturation studies. The DNA-binding constants for complexes 1, 2 and 3 were determined to 2.4 x10⁴, 1.3 x 10⁵ and 4.2 x10⁵ M^-1, respectively. The experimental results suggest that these complexes interact with DNA through groove binding mode. The photo induced cleavage studies shows that the complexes possess photonuclease property against pUC19 DNA under UV–Visible irradiation via a mechanistic pathway involving formation of singlet oxygen as the reactive species. Antibacterial PDT for E. coli strain, the control group showed a significantly higher (p<0.05) bacterial growth (1.5 x 10⁸ CFU/mL), while the complex (3) group presented no significant reduction (p>0.05) in the CFU counts. The complex (3)/Light group presented a significant decrease in the CFU counts (p<0.05) compared with the control group (71.64% for E. coli).

Keywords: groove binding; metal complexes; singlet oxygen; photonuclease activity; antibacterial PDT.

ABSTRACT

High blood pressure is a major cause of various diseases such as stroke and high cholesterol. High cholesterol and cause a variety of deadly diseases. The aim of this study was to conclude if a reduction in serum lipoproteins, especially LDL cholesterol, is a preventive approach against  atherosclerosis. Phlebotomy has been a recommended method to reduce serum lipoprotein levels. As cholesterol affects the blood flow it can also impact cardiovascular fitness and sufferers may find that they get out of breath more easily or just generally feel less fit and healthy or more tired. The present study was conducted to investigate the effects of wet cupping on serum lipoprotein concentrations. In this case it is observed that cupping therapy may be an effective method of reducing LDL cholesterol in men and consequently may have a preventive effect against atherosclerosis.

Keywords: Cupping therapy, High blood cholesterol

ABSTRACT

5-Hydroxytryptamine (serotonin) (5-HT) and norepinephrine (NE) are implicated in modulating descending inhibitory pain pathways in the central nervous system. Milnacipran (MLN) is a selective and potent dual 5-HT and NE reuptake inhibitor (SNRI). In the present study, the effects of HMG-CoA reductase inhibitor atorvastatin (ATR) on antidepressant- induced anti-nociception have been investigated. Anti-nociceptive effects were evaluated using formalin test in rats after administration of atorvastatin and milnacipran alone as well as in combination. Fifty microlitre of 2.5% formalin solution was injected subcutaneously into the plantar surface of the right hind paw and nociceptive behavior was observed up to 45 min in the blocks of 5 min. Milnacipran induced a dose-dependent anti-nociception in the first phase as well as in the second phase of the formalin test at the dose levels of 10, 20, 40 and 60 mg/kg, p.o.. Milnacipran significantly attenuated the duration of licking and licking frequency both in second phase. Atorvastatin (1, 5, 10 and 20 mg/kg, p.o.) did not inhibit the nociceptive behavior of formalin significantly when treated alone. A combination of sub-therapeutic doses of the milnacipran (20 and 40 mg/kg, p.o.) with atorvastatin (10 and 20 mg/kg, p.o.) potentiate anti-nociception induced by antidepressant significantly. It is concluded that the atorvastatin modulate the antidepressant-induced anti-nociception in formalin induced inflammatory pain model. However, studies in chronic models of neuropathic pain are required to evaluate the efficacy of milnacipran and atorvastatin combination in rats.

Keywords: Atorvastatin, Formalin Test, Inflammatory Pain, Milnacipran 

ABSTRACT

Indian herbs are known for their antidiabetic and weight management properties. Tinospora cordifolia is one of them; it is known for boosting immune system and the body defense mechanism against pathogenic microorganisms. In the present study, the effect of Tinospora cordifolia powder on blood sugar level in 20 diabetic male and female in the age group of 40-50 years were studied having high blood sugar level from the normal range. 2gm of Tinospora cordifolia leaf powder was given orally twice a day for two months. Fasting blood samples were investigated in respect of sugar in subjects before the start and at the end of the study. Initially the blood sugar level was high which was decreased significantly in all the subjects of experimental group only in 60 days of oral consumption of Tinospora cordifolia leaf powder.

Keywords: Blood sugar, weight, Oral administration, leaf powder, Tinospora cordifolia.

ABSTRACT

A new class of heterocyclic compounds 1,3,4-thiadiazolo[3,2-a]-s-triazine have been synthesized as schiff’s base of 1,3,4- thiadiazole mix with ammonium acetate and various aromatic aldehyde treated in MW irradiation at 480 W. Reaction is based on microwave mediate multi-component reaction (MCRs). The structures of these compounds have been elucidated by spectral (IR, NMR & Mass) analysis. The title compounds were then evaluated for their in-vitro microbial activity against 2 gram –Ve bacteria (E.coli, K. pneumoniae), 2 gram +Ve bacteria (S.aerues, B.subtilis) and 1 fungal specie (A.niger). The some newly synthesized compounds have shown promising antimicrobial activity.

Keywords: 1,3,5-Triazine, 1,3,4-Thiadiazole, Thiosemicarbazone, Schiff’s base, Antibacterial, Antifungal,  Multi-component reaction (MCRs)

ABSTRACT

Modern synthetic medicines are highly effective in curing various diseases, but many of them show significant side effects. A large number of Indian herbs are claimed to possess anthelmintic properties. However, systematic study and standardization of activities are lacking. The present investigations are undertaken to evaluate and standardize anthelmintic activities of common Indian herbs. Aqueous and ethanolic extracts of Plumbago zeylanica, Myristica fragrance and Saraca asoca are studied with respect to in vitro anthelmintic activity against Eisenia foetida and Pheretima posthuma. Results are expressed in terms of time for paralysis and time for death. Albendazole (20mg/ml) is used as a reference standard. Ethanolic extract of Saraca asoca (50 mg/ml) proved to be the best death inducer against Eisenia foetida, whereas ethanolic extract of Plumbago zeylanica at concentration 50mg/ml showed highest anthelmintic activity against Pheretima posthuma.

Keywords: Anthelmintic, Pheretima posthuma, Eisenia foetida, Plumbago zeylanica, Myristica fragrance, Saraca asoca.

ABSTRACT

A series of substituted 1, 4-benzothiazine derivatives were designed keeping in view the structural requirement of pharmacophore and evaluated for in silico antihypertensive activity. Docking procedures allows virtually screening a database of compounds and predict the strongest binder based on various scoring functions. In the docking study, the most active compounds of the series was, AR 1, AR 2and AR 3 exhibited good binding properties. Result reveals that the protein-ligand interaction energy of derivatives AR 1, AR 2and AR 3 were -8.08 kcal/mol, -8.48 kcal/mol and -7.75 kcal/mol, which is better than the standard antihypertensive Losartan drug as -5.51 kcal/mol, so that the derivatives have satisfactory affinity with established hypertensive receptor namely Angiotensin converted enzyme 2. A computational study was also carried out including prediction of pharmacokinetic properties, toxicity and bioactivity studies. The percentage of absorption (%ABS) was calculated and observed that all titled compounds exhibited a great %ABS ranging 90.54, 91.42 and 90.54, with respectively and compared than standard Losartan drug as %ABS 77.06. These compounds emerged as a lead in this series and making them potentially promising agents for hypertension therapy. 

Keywords:1, 4-benzothiazine derivatives, Anti hypertension activity, Computational study and ACE-2.

ABSTRACT

The artificial dipeptide sweetener aspartame [APM; L- aspartyl-L- phenylalanine methyl ester] is present in many products especially unsweetened and sugar products. These products are frequently utilized by people trying to lose weight or patients with diabetes. Concern relating to the possible adverse effect has been raised due to aspartames metabolic components. Aspartame is rapidly and completely metabolized in humans and experimental animals to aspartic acid (40%), phenylalanine (50%) and methanol (10%). Methanol, a toxic metabolite is primarily metabolized by oxidation to formaldehyde and then to formate these processes are accompanied by the formation of superoxide anion and hydrogen peroxide. This study focus is to understand whether the oral administration of aspartame (40 mg/kg b.w) for 90 days, have any effect on membrane bound ATPases in RBC, antioxidant status in blood cell and neutrophil function of rats. To mimic human methanol metabolism, folate deficient rats were used. After 90 days of aspartame administration, shows a significant change in membrane bound ATPases, antioxidant level and immune response. This study concludes that oral administration of aspartame (40mg/kg b.w) for longer duration may cause oxidative stress in blood cell and altered the neutrophil function

Keywords: Aspartame, ATPases, antioxidant, Neutrophil, RBC , immunization

ABSTRACT

Medicinal plants and their secondary metabolites have been used since last few centuries as remedies to treat diseases and disorders. As per WHO report (1993), 80% of world population continues to depend on medicine isolated from medicinal plants. Presently there is an increasing interest in herbal medicine related to isolation, characterization and pharmacological screening of extracts obtained from medicinal plants. The ethanolic extract of Leucas indica var. martinicensis was studied for preliminary phytochemical screening and anthelmintic activity at various concentrations (i.e., 10mg/ml, 25mg/ml, 50mg/ml, 100mg/ml) by using adult Indian earth worm, pheretima posthuma from in nalgonda region. Phytochemical Screening revealed the presence of Alkaloids, carbohydrates, and saponins. The mean paralysis time and mean death time for each sample was calculated and compared with the Albendazole which is taken as standard. The result was found that Leucas indica var. martinicensis had an anthelmintic activity which was greater than standard Albendazole.

Keywords: Leucas indica var. martinicensis, standard Albendazole, preliminary phytochemical screening, anthelmintic activity, pheretima posthuma.

ABSTRACT

In this paper an attempt is made to prepare IPN beads of the drug by taking alginate solution in combination with a polymer (PVA/Kennel powder /Guar gum). The prepared copolymer solution is dropped in to 2% CaCl₂. The beads are hardened by cross linking with a common cross-linking agent, glutaraldehyde. The beads are characterized by Fourier transform infra-red spectroscopy and scanning electron microscopy. Additionally quality control tests such as swelling index, bead water uptake, entrapment efficiency and drug release studies are performed. The extent of cross-linking is studied in terms of the size and release characteristics of the beads. Most of the formulations indicated erosion based release pattern. The size of the beads ranged from 250 to 400 µm. The entrapment efficiency of the formulation ranged from 73.6% to 94.50%.  

Keywords: Sodium alginate, Venlafaxine, Interpenetrating network, dissolution

ABSTRACT

Sulfones are known to possess various biological activities. Their great potential as bioactive compounds, combined with the easy method of synthesis, make this class a strong candidate for the production of medicines economically. This article deals with the synthesis of a series of ten diaryl sulfones, their antibacterial activity, individually, synergistic antibacterial activity with trimethoprim against E. coli and preliminary QSAR studies. The antibacterial activity was performed by agar diffusion method, against Gram positive and Gram negative bacteria. Few derivatives exhibited antibacterial activity comparable to or better than the standard, sulphamethoxazole, against Gram negative organisms (E. coli and S. dysentrae). Sulfones being folic acid inhibitors, their synergistic effect was checked with trimethoprim on E. coli. Most of the compounds exhibited synergistic effect with trimethoprim, which was better than the combination of trimethoprim and sulfamethoxazole (1:5). Quantitative structure activity relationships studies were performed by multiple linear regression analysis. The antibacterial activity of sulfones was found to correlate well with their dipole moment and ionization potential.

Keywords: Diaryl sulfones, Antimicrobial activity, Synergistic effect, QSAR

ABSTRACT

Artemether-lumefantrine (ART-LUME) off late has become the first-line treatment for uncomplicated malaria in many Sub-Saharan Africa, Asia and America. Vigorous monitoring of the therapeutic efficacy of this treatment is needed. This requires high-quality studies following standard protocols; ideally, such studies should incorporate measurement of drug levels in human plasma in biological matrices. A specific and reliable isocratic mode RP-HPLC method has been developed and validated for simultaneous determination of artemether (ART) in combination with lumefantrine (LUME) in human plasma using diode array detector (DAD) at 238 nm. The analyte was separated on NUCLEOSIC-CN Cyano coloumn (150 mm × 4.6 mm, particle size 5 μm) using a mobile phase consisting of acetonitrile and acidic buffer (adjusted to pH 2.5 with H₃PO_{4 ­}– 2 %) in the ratio of 37: 63 v/v and flow rate was 1 ml/min. The method is linear over a range of 100-1600 µg/ml (r² ≥ 0.999) and 1-16µg/ml (r² ≥0.998) for the assay of ART and LUME respectively. Itraconazole (ITZ) (10µg/ml) was used as internal standard. The retention times of ART and LUME was found to be 4.3 min and 14.3 respectively. Mean extraction recovery for ART and LUME were 87.3 % and 89.1 %, respectively. Inter and intraday coefficients of variation for ART and LUME were ≤ 10%. The lower limits of quantification for ART and LUME were 0.22 and 0.66 μg/ml, respectively. The results of the study showed that the proposed RP-HPLC validated method described is efficient and has the necessary accuracy and precision for the rapid quantitative simultaneous determination of ART and LUME in human plasma and is thus highly suitable for use in pharmacokinetic /bioavailability/bioequivalence studies in healthy human subjects.

Keywords: RP-HPLC method, Artemether, Lumefantrine, human plasma

ABSTRACT

The principal objective for our study was to evaluate the efficacy of Saccharomyces boulardii against Giardia  lamblia infection and investigated  the mechanism of this anti diarrheal effect on electrolyte (sodium,potassium and chloride) changes compared with metronidazole by using mice models.A single oral dose of S.boulardii of up to 5 x10⁶cfu/0.1 of viable cells reduced parasite appear in feces and disappear completely at the 7^th day compared with metronidazole the cysts parasite continued till 8^th day. The yeast also caused increased potassium and sodium while decrease chloride level in serum. The histo morphological study findings showed in the group which was given S. boulardii the majority of intestinal villi return to normal shape. These finding indicated  that S.boulardii may be effective  in treating giardiasis also  has specific  effects on electrolyte  secretary  response.

Keywords: Saccharomyces boulardii ; Giardia lamblia ; probiotic