Improving Solubility and Bioavailability of Poorly Water Soluble Drugs by Solid Dispersion Technique – A Review”

摘要

The objective of this study was to develop sustained release mucoadhesive tablets of lovastatin by using hydrophilic polymers like chitosan, xanthan gum, karaya gum and HPMC K15M. Lovastatin is an anti-hyperlipidimic agent which has low bioavailability due to extensive first pass metabolism. It was sought to increase gastric retention time of lovastatin by development of sustained release mucoadhesive tablets leading to reduce fluctuation in the plasma concentration and improved bioavailability. Lovastatin tablets were prepared by wet granulation method the drug polymer mixtures were subjected to preformulation studies. FTIR studies showed that there was no interaction between drug and polymer. The granules were evaluated for angle of repose, bulk density, Carr’s index, Hausner’s ratio and the tablets were subjected to thickness, weight variation, drug content, hardness, friability, surface pH, swelling index, mucoadhesive strength and In-vitro studies. The results were found to be within the limits. The drug release studies were carried out for 12hours. In which formulation with combination of chitosan and karaya gum with the ratio of (1:1.5:1.5) was selected as an optimized formulation which have drug release of 98.89% in 12hours. Mathematical analysis of the release kinetics indicates that nature of drug release from the mucoadhesive tablets follows non-fickian diffusion mechanism. Formulation F9 was selected as optimized batch from all the formulations due to their improved bioavailability.