In vivo Bioavailability Studies of Buccoadhesive Compacts of Lercanidipine Hydrochloride Tablets”

摘要

Buccoadhesive compacts of lercanidipine HCl showed better drug control release property during in vitro drug release studies. Optimized formulation of buccoadhesive compacts (FLCR2) was subjected to pharmacokinetic evaluation with an objective to evaluate their rate controlling efficiency and drug release by in vivo method using rabbits. Bilayered buccoadhesive compacts of lercanidipine HCl containing core layer and backing layer were prepared by direct compression method using different polymers such as HPMC, Carbopol 934P and Ethyl cellulose. The compacts were calculated peak plasma concentration (Cmax), time at which peak occurred (tmax), area under the curve (AUC), elimination rate constant (Ke), biological half life (t1/2), absorption rate constant (ka), Clearance(Cl) and volume of distribution(Vd) from in vivo study data. The in vivo study results showed that, the absorption of lercanidipine HCl was slow over longer period of time with a rate constant (Ka) of 2.531 h-1. The mean residence time, Cmax and tmax was found to be observed from 12 h 30 min, 19.804 μg/ml and 3h. It was also observed that AUC was found to be 235.687 μg/ml. From pharmacokinetic studies, the lercanidipine HCl was released and absorbed slowly over longer period of time.