Current Research in Pharmaceutical Sciences

31-44

Authors: Sanjay J Ingle and K K Tapar

With a view to the rational design of a series of selected 48 substituted benzisoxazoles, 3D-QSAR and docking studies have been performed for the prediction of antipsychotic activity. Overall model classification accuracy was 76.00% (q2 = 0.7600, representing internal validation) in training set and 68.33% (Pred_r2 = 0.6833, representing external validation) in test set using sphere exclusion and forward–backward as a method of data selection and variable selection, respectively. The docking studies suggest that compound 38 interact with GLU43, THR48, GLN79, GLN147, LEU148, ASN149, ASP150, SER151, ARG178, LYS270, LEU273, THR327, GLU43, GLN79, GLN147, ASN149, ASP150, SER151 and GLU43 amino acid residues. Both QSAR and docking study of such derivatives provide guidance for further lead optimization and designing of more potent antipsychotic agents.

50-54

Authors: Bhawna Mishra, Rizwana Khan, Manish Rajoriya and Anil Kharia

Glimepiride is a first third generation sulphonyl urea agent for the treatment type II diabetes mellitus. The main objective of present work was to formulate and evaluate fast dissolving tablet of glimepiride by using different concentration of super disintegrating agents. Glimepiride is given once daily in doses from 1-8 mg. The fast dissolving tablets of glimepiride was prepared from F1- F4 by direct compression method.The drug and excipients were evaluated for angle of repose, bulk density, tapped density, Carr’s index and hausner’s ratio for the determination of flow property of powder. The formulated tablets were evaluated for thickness, hardness, friability, wetting time, water absorption and dispersion time. The obtained results were clearly indicating that the formulated tablets results are within the range and when compared with all formulations, F4 was the best formulation among the four formulations.