Development and Evaluation of Clopidogrel Bisulphate Multi-Unit Floating Mini-Tablets
The objective of the present work was to formulate and characterize multi-unit floating drug delivery system of Clopidogrel bisulphate to increase the bioavailability and sustain the drug release properties up to 8 h with more predictable drug release kinetics that avoids all or nothing emptying effect wherefore to improve patient compliance. Clopidogrel bisulphate floating mini-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 of prepared mini tablet formulations. 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 Clopidogrel bisulphate floating mini tablet formulations followed zero order kinetics. As per Korsmeyer-Peppas equation, the release exponent “n” ranged 0.561-0.758 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. Based on the results, Clopidogrel bisulphate floating mini tablets prepared by employing combination of 20% w/w HPMC K100M and 20% w/w Compritol 888 ATO offered desired in-vitro floating time and drug dissolution profile.
Keywords: Bioavailability, Clopidogrel bisulphate, floating mini-tablets, release kinetics, sustained release.
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