Journal of Bioequivalence & Bioavailability

Effect of CAP on the pharmacokinetics of cyclosporin A (CyA) in rats and the mechanism of this food-drug interaction

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Yongning Lu

Posters-Accepted Abstracts: J Bioequiv Availab

Abstract:

Capsaicin (CAP) is the main ingredient responsible for the hot pungent taste of chilli peppers. This study investigated the effect
of CAP on the pharmacokinetics of cyclosporin A (CyA) in rats and the mechanism of this food-drug interaction. The results
indicated that after 7 days of low or middle dose of CAP (0.3 or 1.0 mg/kg), the blood concentration of CyA was not significantly
changed compared with that of vehicle-treated rats, whereas the blood concentration of CyA in high dose group (3.0 mg/kg) was
significantly increased. The total clearance (CL/F) of CyA was decreased, and the bioavailability was significantly increased to about
1.44 fold of that in vehicle-treated rats after 7 days of high dose CAP treatment. At this time, the P-gp and CYP3A1/2 in the liver
and intestine were decreased at both the mRNA and protein levels. These results demonstrated that chronic ingestion of high doses
of CAP will increase the bioavailability of CyA to a significant extent in rats and the food-drug interaction between CAP and CyA
appears to be due to modulation of P-gp and CYP3A gene expression by CAP, with differential dose-dependence.