Enhancement of Solubility, Dissolution And Stability Properties of Griseofulvin

ABSTRACT 

Good aqueous solubility and permeability of a drug is essential for the desired concentration (bioavailability) to be achieved in systemic circulation. Poor solubility of drugs remains a major challenge in pharmaceutical firms. Such drugs lead to poor bioavailability, dissolution rates, stability, permeation through membrane and extensive presystemic metabolism. Oral route remains the preferred choice of drug administration but the poor solubility of Griseofulvin, a class II drug of Biopharmaceutics Classification System (BCS) threatens its use as an oral therapy. This study addressed the challenge by developing various formulations to enhance the solubility and dissolution properties of Griseofulvin tablets. Four different formulations of Griseofulvin were investigated using the wet granulation method. Formulation A contained gelatin as a binder and formulations B, C and D contained PVP with varying amount of SLS. At both the granules and tablets stages, the relevant test parameters were carried out. The formulations with PVP (B, C, and D) gave better dissolutions than that of the gelatin (A). Dissolution values for formulation A tablets were lower while formulations B, C, D tablets gave values above the standard 80 %. Of the three PVP-formulations D emerged the best formulation which was adopted to produce a confirmatory batch. Tablets of this confirmatory batch were subjected to stability testing as done previously and further to both ICH accelerated and real time conditions. After both studies (6 months for accelerated and 12 months for real time), there was no significant change in accordance to ICH definition. The control samples also confirmed the dissolution of formulation D to the original formulation A.