DEVELOPMENT AND EVALUATION OF PRASUGREL HYDROCHLORIDE FLOATING TABLETS

摘要

The objective of the present work was to formulate and characterize floating drug delivery system of Prasugrel hydrochloride that releases the drug slowly up to 8 h in order to minimize its potential side effect bleeding and to improve the bioavailability with enhance patient compliance. Prasugrel floating tablets were prepared by effervescent approach with melt granulation and direct compression techniques alone and in combination using Hydroxypropyl methylcellulose (HPMC) K100M and Compritol 888 ATO at different concentrations (20%, 30% and 40% w/w) alone and in combination. Sodium bicarbonate at concentration 10% w/w was optimized as gas generating floating agent. Evaluations were carried out on physical parameters, floating behavior and influence of type of polymer on drug release rate. All the formulations were subjected to various quality control and in-vitro dissolution studies and corresponding dissolution data were fitted to popular release kinetic equations in order to evaluate release mechanisms and kinetics. All the prasugrel floating tablet formulations followed zero order kinetics. As per Korsmeyer-Peppas equation, the release exponent “n” ranged 0.550-0.776 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. Based on the results, prasugrel hydrochloride floating tablets prepared by employing combination of 15% w/w HPMC K100M and 15% w/w Compritol 888 ATO offered desired in-vitro floating time and drug dissolution profile.