July 2012

About Authors:
Sriharsha Vardhan
SRM College of Pharmacy,
Chennai, Tamil Nadu
sriharshavardhan.51@gmail.com

ABSTRACT
The present study is formulating Rabeprazole modified release beads (Immediate and Time, Pulsatile Release) and to target the release of the drug in intestine and to avoid stability related problems. Preparation of immediate release (IR) Rabeprazole beads has done by drug layering process and barrier coated beads by providing an enteric coating membrane on IR beads. Timed release beads has done by providing a Film coating for IR and lag time coating for TPR (Timed, Pulsatile Release)  on enteric coated beads. Encapsulation Process and evaluation of enteric coated IR and TPR beads has done by physical evaluation and chemical evaluation. Stability studies have done for best quality Rabeprazole IR and TPR enteric coated beads formulations. Based on the results Formulation 3 and Formulation 9 were selected as the best formulation developed for Rabeprazole Dual Drug Release Capsules.

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About Authors:
Pritesh R. Patel^*, Priyank Patel, Jagath Pillai, Nilesh Darji, Bhagirath Patel
Department of Pharmaceutical Chemistry,
Sat Kaival College of Pharmacy, Sarsa,
Ta & Dist: Anand (Gujarat), India-388365
*prit.pharma@gmail.com

ABSTRACT
As part of ongoing studies in developing new antimicrobials, a novel series of 4-acetamido-N-(substituted 1, 3-benzothiazol-2-yl) benzenesulphonamide and N-(substituted 1, 3-benzothiazol-2-yl)-4-(substituted aryl diazenyl) benzenesulphonamide were synthesized in order to determine their antibacterial and antifungal activity. The synthesized compounds were tested in vitro against two Gram-positive bacteria like Staphylococcus aureus, Bacillus subtilis; two Gram-negative bacteria like Escherichia coli, Pseudomonas aeruginosaand one fungal strain Candida albicans in comparison with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial and antifungal activity against the tested microorganisms. The compounds with a 6-chloro (SK5b), 7-chloro-6-fluoro(SK5d) and 6-nitro (SK5e) on 2-amino benzothiazole ring possessing azo linkage showed better antimicrobial activity; almost similar or less to that of standard drugs thus they could be promising candidates for novel drugs. The novel heterocyclic derivatives were characterized by Physical characterization (Melting point, TLC) and different Spectroscopy techniques (IR, ¹H NMR and Mass spectroscopy).

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About Authors:
Rakesh Bhatia*
School of Pharmaceutical Sciences,
Department of Pharmaceutical Chemistry,
Jaipur National University,
Jaipur-302025 (Rajasthan), India
*rakesh.mpharm1304@yahoo.com

Abstract
Chemical synthesis data and their biological screening have provided a vast amount of experimental data. As a result of that, availability of large amount of biological data information through molecular biology has made drug discovery and development a more complex method. To combat these problems, Quantitative structure-activity relationships (QSAR) emerged as a very useful tool in drug design. QSAR has been applied extensively and successfully over several decades to find predictive models for activity of bioactive agents. QSAR have brought revolution in drug discovery process by thedevelopment of mathematicalrelationships linking chemical structures and pharmacological activity in quantitative manner of series of compounds. Description of the molecular structure, electronic orbital reactivity and the role of structural and steric components has been the subject of mathematical and statistical analysis. Computational drug design method in QSAR is a rapidly growing field which is now a very important component in the discipline of medicinal chemistry. Virtual filtering and screening of combinatorial libraries have recently gained attention as methods complimenting the high-throughput screening and combinatorial chemistry. These chemoinformatic techniques rely heavily on quantitative structure-activity relationships (QSAR) analysis, a field with established methodology and successful history.By characterize a specific aspect of a molecule that is numbers containing structural information derived from the structural representation used for molecules under study called “Molecular descriptors” to find appropriate representations of the molecular structure of drug compoundsto obtain the structure-activity relationships in which these theoretical and computational methods are based, the ability to predict physicochemical, pharmacokinetic and toxicological properties of these leads are becoming increasingly important in reducing the number of expensive methods and late development failures. Thus thereby, QSAR certainly decreases the number of compounds to be synthesized by easing the selection of the most promising candidates. This review seeks to provide a review on role of molecular descriptors in the drug design in QSAR.

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