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Effect of resveratrol on the pharmacokinetics of oral and intravenous nicardipine in rats: possible role of P-glycoprotein inhibition by resveratrol.

Author(s): Choi JS, Choi BC, Kang KW

Affiliation(s): College of Pharmacy, Chosun University, Gwangju, Korea.

Publication date & source: 2009-01, Pharmazie., 64(1):49-52.

The present study aimed to assess the effect of resveratrol on the bioavailability of nicardipine in rats. Nicardipine was administered orally (12 mg kg(-1)) or intravenously (4 mg kg(-1)) with or without oral administration of resveratrol (0.5, 2.5 or 10 mg kg(-1)). The oral administration of 2.5 or 10 mg kg(-1) of resveratrol significantly increased both the area under the plasma concentration-time curve (AUC) (P < 0.01, 111-126%) and the peak plasma concentration (Cmax) (P < 0.01, 105-121%), and significantly decreased the total body clearance (CL/F) (P < 0.01, 52.8-55.8%) of orally administered nicardipine. In contrast, resveratrol did not significantly change the pharmacokinetic parameters of i.v. nicardipine. Resveratrol significantly reduced rhodamine123 efflux via P-gp in MCF-7/ADR cells overexpressing P-gp. Resveratrol also inhibits CYP3A4, suggesting that the enhanced oral bioavailability of nicardipine by resveratrol may result from decreased P-gp-mediated efflux or inhibition of intestinal CYP3A4 metabolism. Based on these results, nicardipine dosage should be adjusted when given with supplements containing resveratrol.

Page last updated: 2009-10-20

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