Pharmacokinetic comparison of orally disintegrating, β-cyclodextrin inclusion complex and conventional tablets of nicardipine in rats

The goal of this study was to compare the pharmacokinetics of nicardipine hydrochloride orally disintegrating tablets and β-cyclodextrin inclusion complex with its conventional tablets. Forty-five rats were divided into three groups evaluating the effect of dosage forms on the pharmacokinetics of nicardipine hydrochloride. Blood samples were taken at predefined sampling points 0–24h after medication, and the plasma concentrations of nicardipine hydrochloride orally disintegrating tablets, β-cyclodextrin inclusion complex and its conventional tablets were determined by high-performance liquid chromatography. The orally disintegrating tablets increased in Cmax, AUC and tβ1/2 were observed, tmax occurred at 1.0 and 2.0h with orally disintegrating tablets and conventional tablets. The orally disintegrating tablets exhibited a longer elimination half-life (t 1/2 β 5.5h) compared with its conventional tablets (t1/2 β 1.4 h ). The mean dose corrected area under the plasma concentration-time curve extrapolated to infinity AUC (0−∞) of orally disintegrating tablets was 5.60 times greater than its conventional tablets. This research showed that formulation of nicardipine hydrochloride orally disintegrating tablets and β-cyclodextrins inclusion complex resulted in increase of bioavailability and prolong its activity time. [Life Science Journal 2010;7(2):80-84]. (ISSN: 1097-8135).