FABRICATION AND OPTIMIZATION OF NOVEL GLIPIZIDE SUSTAINED RELEASE MATRICES FOR SOLUBILITY AND DISSOLUTION ENHANCEMENT BY SOLID DISPERSION THROUGH HYDROPHILLIC CARRIERS

Abstract

The present research work was to improve the dissolution rate of glipizide which belongs to BCS II drug by enhancing its aqueous solubility using different hydrophilic carriers like PEG 6000 and hydroxypropyl methylcellulose E15 (HPMC E15). The solid dispersion was embedded into the matrix of polymers to sustain the release pattern of drug. The various solid dispersion formulations were prepared by employing fusion method using different carriers. Further solid dispersion formulations were subjected to different in-vitro evaluation tests for solubility, drug content uniformity, drug-polymer interaction, DSC study and in-vitro drug release study. Tablets were prepared by direct compression method and evaluated for various physical parameters. A direct compression method using response surface methodology, followed by optimization of the evaluated parameters was employed to get the final optimized formulation. The results of drug content uniformity showed the uniform dispersion of glipizide in solid dispersion formulations. The DSC endothermic peak at 216.08°C due to glipizide was partially and completely disappeared in solid dispersion formulation indicating that drug was completely dispersed in formulations. In-vitro drug release showed 80.35% in 60 minutes for the best solid dispersion formulation S3 (ratio 1:3). Among all the formulations, F4 shows 92.87% better sustained release at the end of 12 hrs. The release co-efficient values ‘n’ (E‚0.5) indicated that the drug release followed fickian diffusion mechanism based on formulation factors. The stability studies were carried out according to ICH guideline and result found of selected formulation was stable.Keywords: Glipizide, Solid dispersion, Xanthan gum, MatricesÂ