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Zawar Laxmikant R.,Hr Patel Institute Of Pharmaceutical Education And Research | Savaliya Pankaj J.,R C Patel Institute Of Pharmaceutical Education And Research | Bari Sanjay B.,R C Patel Institute Of Pharmaceutical Education And Research | Gattani Surendra G.,Hr Patel Institute Of Pharmaceutical Education And Research
International Journal of Pharma and Bio Sciences | Year: 2010

The objective of the present study was to formulate and evaluate Floating-mucoadhesive tablets of clarithromycin for the treatment of Helicobacter pyloric (H.pylori) infection. Tablets were prepared by direct compression using directly compressible polymers such as HPMC K4M, HPMC K15M and carbopol 974P and were evaluated for drug - excipient compatibility, density, buoyancy test, mucoadhesion force, swelling study, drug content and in-vitro release profile. Sodium bicarbonate and citric acid were used for producing effervescent base for buoyancy of tablets. Analysis of drug release from tablet indicates drug release by zero order rate kinetics. No significant change was observed in physical appearance, drug content, floatability or in vitro dissolution pattern after storage at 45 °C/75% RH for three months.


Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research | Haswani N.G.,Rc Patel Institute Of Pharmaceutical Education And Research
Journal of Saudi Chemical Society | Year: 2014

In an attempt to find a new class of antimicrobial agents, a series of thienopyrimidin-4(3H)-thiones 4(H1-H36) were synthesized and evaluated for in vitro antifungal activity against Candida albicans (NCIM 3471), Aspergillus niger (NCIM 545), and Penicillium chrysogenum (NCIM 709). The title compounds were synthesized by thionation of thienopyrimidin-4(3H)-ones 3(H1-H36) using Lawesson's reagent. All the compounds were characterized using elemental analytical (C, H, and N) and spectral (FT-IR, 1H NMR, 13C NMR and MS) data. Among the tested compounds, 5-(4-chlorophenyl)-2-(pyridin-3-yl)thieno[2,3-d]pyrimidine-4(3H)-thione 4(H11), 2-sulfanyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-4(3H)-thione 4(H18), and 2-(butylsulfanyl)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-4(3H)-thione 4(H32) were identified as potentially excellent antifungal agents. They exhibited potent antifungal activity against C. albicans (MIC; 4 μg/mL), A. niger (MIC; 2 μg/mL), and P. chrysogenum (MIC; 2 μg/mL) comparable with that of ketoconazole. The binding mode of compounds by SP docking studies shows that it fits well into the active site cavity of DHFR. Lipinski's rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use thereby indicating their potential as drug-like molecules. © 2014.


Patil P.O.,Rc Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research
Arabian Journal of Chemistry | Year: 2014

The present review highlights the synthetic methods of monoamine oxidase inhibitors (MAO) belonging to a group of nitrogen heterocycles such as pyrazoline, indole, xanthine, oxadiazole, benzimidazole, pyrrole, quinoxaline, thiazole and other related compounds (1990-2012). Moreover, it emphasizes salient findings related to chemical structures and the bioactivities of these heterocycles as MAO inhibitors. The aim of this review is to find out different methods for the synthesis of nitrogen containing heterocycles and their bioactivity related aspects as MAO inhibitors. © 2013.


Patil P.O.,Rc Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research | Firke S.D.,Hr Patel Institute Of Pharmaceutical Education And Research | Deshmukh P.K.,Hr Patel Institute Of Pharmaceutical Education And Research | And 2 more authors.
Bioorganic and Medicinal Chemistry | Year: 2013

Monoamine oxidase (MAO) enzyme inhibition is a crucial target for the management of depression and Alzheimer disease and inhibitors of MAO are the most important drugs for their management. Coumarins are a large family of compounds, of natural and synthetic origin, that exhibit a variety of pharmacological activities, including MAO inhibition. The current review highlights the design and synthetic methods of coumarin derivatives as well as coumarins obtained from plant source as MAO inhibitors for treatment of depression and Alzheimer disease with salient finding related to structure-activity relationship. The aim of present review is to find out natural as well as synthetic coumarins as MAO inhibitors. © 2013 Elsevier Ltd. All rights reserved.


Firake S.D.,Rc Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research
Current Enzyme Inhibition | Year: 2015

Benzenesulfonamide is versatile motif employed for the discovery in the field of medicinal and pharmaceutical chemistry. Over the years of active research, sulfonamide has evolved as important privileged pharmacophore in medicinal chemistry, encompassing a diverse range of biological activities including antiviral, carbonic anhydrase inhibitors, diuretic, and a protease inhibitor, hypoglycemic, anticancer and anti-inflammatory. On the other hand, owing to the fast development of new drugs possessing sulfonamide pharmacophore many research reports generated in a short span of time. Thus, there is a need to couple the most recent data with the prior data to comprehend the present status of benzenesulfonamide as anti-inflammatory agent. The present review highlights the molecular modeling and synthetic methods of benzenesulfonamide scaffold bearing various heterocyclic or carbocyclic rings such as thiazole, triazole, imidazole, isoxazoline, pyridine, pyranone, pyridazone, pyrimidine, pyran, indole, benzothiazole, benzotriazole, benzimidazole and benzopyran as central ring scaffold. In addition to this, the manuscript will be a guideline to medicinal chemists for rationally designing a novel benzenesulfonamide bearing compounds as COX-2 inhibitors. © 2015 Bentham Science Publishers.


Redasani V.K.,Rc Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research
Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry | Year: 2015

The present work is an agreement with simple and efficient method of improving the therapeutic efficacy of ibuprofen by masking its acidic moiety. It aims to reduce gastrointestinal side effects by controlling the rate, duration and site of release. This is achieved by synthesis and evaluation of polymeric prodrug of ibuprofen with natural polymer sodium alginate. The synthesis was supported by N-protected serine as spacer due to chemical incompatibility of drug and polymer. Synthesized prodrug was characterized for confirmation of said structures. The in-vitro dissolution profile of ibuprofen-alginate prodrug showed that the release of the drug is significantly higher in case of pH 7.2 buffer as compared to ibuprofen, which might be due to ester group adjacent to drug get hydrolyzed. The hydrolysis was found to be with faster rate in alkaline media than that of in acidic media. © 2015 Bentham Science Publishers.


Sonawane R.O.,Hr Patel Institute Of Pharmaceutical Education And Research | Patil S.D.,Hr Patel Institute Of Pharmaceutical Education And Research
Polymer - Plastics Technology and Engineering | Year: 2016

Nowadays, pellets are playing a dominating role in the world of multiparticulate oral drug delivery. These pellets have many advantages over single-unit dosage forms like extended release. The present review highlights various formulation aspects for the designing of extended release pellets with a special emphasis on effect of key formulation variables. Design includes pellets–matrix and pellets–reservoir systems. Formulation variables such as effect of polymer, plasticizer, pore former, pH adjuster, antitacking agents, and wetting liquids are considered as key formulation variables. The authors lead to a conclusion that designing approaches and formulation factors should be considered and will assist while preparing extended release pellets. © 2016, Copyright © Taylor & Francis Group, LLC.


PubMed | Hr Patel Institute Of Pharmaceutical Education And Research
Type: Journal Article | Journal: Current drug delivery | Year: 2016

In present investigation, an innovative attempt has been made to enhance the solubility and dissolution rate of Repaglinide (RPGD) using hydrothermally treated water insoluble dietary bamboo fibers (HVBF) as potential nutraceutical used in the treatment of diabetes mellitus. RPGD was selected as a model drug due to its low aqueous solubility and dissolution rate. Characterization of HVBF demonstrated the outstanding features like high surface area, maximum drug loading and increase dissolution rate and making HVBF as an excellent drug carrier. RHVBF (Repaglinide loaded HVBF) tablets were prepared using direct compression method. Pre and post-compression parameters for blend and tablets were studied and found within acceptable limits. RHVBF and tablet showed significantly improved dissolution rate, when compared with pure crystalline RPGD, physical mixture, RVBF and commercial marketed tablet. This fact was further supported by FT-IR, DSC, XRPD and FESEM studies followed by in-vitro drug release profile. Stability studies showed no changes after exposing to accelerated conditions for a period of 3 months with respect to physical characteristics and in-vitro drug release studies. In a nut shell, it can be concluded that HVBF is a novel, smart and promising carrier for poorly water soluble drugs, when administered orally.


PubMed | Hr Patel Institute Of Pharmaceutical Education And Research
Type: | Journal: Journal of pharmaceutics | Year: 2015

In the present investigation, pulsatile release beads were prepared by ionic gelation technique. Lornoxicam dual cross-linked beads were prepared by dropping dispersed phase of lornoxicam, pectin, and sodium alginate into the dispersion phase of different concentrations of calcium chloride solution followed by aluminium chloride solution. The formulated beads were further coated by Eudragit L & S 100 in the ratio 1:2 w/w in order to achieve desired lag time. In vitro release study showed lag time of 5-8h before release of lornoxicam from the formulated beads. Thus, formulated dual cross-linked beads when administered at bed time may release lornoxicam when needed most for chronotherapeutics of early morning rheumatoid arthritis attacks in chronic patients.


PubMed | Hr Patel Institute Of Pharmaceutical Education And Research
Type: Journal Article | Journal: Advanced pharmaceutical bulletin | Year: 2014

The objective of this work was to develop a bioadhesive topical gel of sertaconazole nitrate with the help of response-surface approach.Experiments were performed according to a 3-level factorial design to evaluate the effects of two independent variables [amount of Carbapol 934 = X1) and Sodium carboxymethylcellulose (NaCMC) = X2)] on the bioadhesive character of gel, rheological property of gel (consistency index), and in-vitro drug release. The best model was selected to fit the data.Mathematical equation was generated by Design Expert software for the model which assists in determining the effect of independent variables. Response surface plots were also generated by the software for analyzing effect of the independent variables on the response. The effect of formulation variables on the product characteristics can be easily predicted and precisely interpreted by using a 3-level factorial design and generated quadratic mathematical equations.On the basis of product characteristics viscosity, bioadhesiveness, permeation study, in-vitro release, in-vivo studies, TPA and spreadability it can be concluded that the best batch of topical bioadhesive gel of Sertaconazole nitrate would be with 1% Carbopol 934 and 1% NaCMC.

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