Comparison of Biorelevant and Compendial Dissolution Media and Prediction of In-vivo Plasma Profile of BCS Class II Drug

The performance of biorelevant and compendial media was compared to test dissolution of drugs belonging to class II according to Biopharmaceutic Classification Scheme (BCS) and their potential was determined in predicting in-vivo profile. The solubility of Carbamazepine was determined in various media having different pH (water, SGF_SP, SIF_SP, SGF_SPSLS, FaSSIF and FeSSIF), to calculate D/S values in different media. Dissolution of Carbamazepine, a neutral drug was studied using USP apparatus II in water, SGF_SP, SIF_SP, SGF_SPSLS, FaSSIF and FeSSIF. Hixson- Crowell model was applied to determine drug release kinetics. The invivo profile was predicted from invitro dissolution data using modified form of model proposed by Nicolaides in 2001. Dissolution of Carbamazepine from tablet formulation was found to be dependent upon concentration of solubilizing agents. The similarity factor indicated pH independent dissolution of carbamazepine in different dissolution media. The invivo profiles predicted using invitro dissolution of carbamazepine in biorelevant media supported better absorption in the presence of food which matches the literature facts. The Biorelevant Media therefore are better at discriminating invitro release characteristics for forecasting invivo performance of poorly soluble drugs.