Purpose: Cordyceps sinensis (Dongchongxiacao) is popularly used as tonic and herbal medicine in Taiwan and Mainland China. Cyclosporin is a widely used immunosuppressive agent with narrow therapeutic window. Any factor altering the absorption or disposition of cyclosporin would cause toxic effects or graft rejection. Our study attempted to investigate the effects of coadministration of cordyceps powder concomitantly and 1 hour before cyclosporin dosing on the absorption and disposition of cyclosporin in rats. Methods: Rats were intravenously and orally administered cyclosporin with and without cordyceps powder in crossover designs. Blood samples were withdrawn via cardiopuncture and assayed by FPIA method. The pharmacokinetic parameters of cyclosporin were calculated by using WINNONLIN. Results: Our results indicated that coadministration of cordyceps powder significantly decreased the Cmax and AUC of cyclosporin by 82.5% and 77.1%, respectively. In addition, when rats were giving cordyceps powder 1 hr before cyclosporin dosing, the Cmax and AUC of cyclosporin was significantly decreased by 85.3% and 83.6%, respectively. However, when cyclosporin was given as an intravenous bolus, the disposition of cyclosporin was not altered, indicating that the interaction occurred at the absorption site. Conclusion: Concurrent use of cordyceps profoundly decreased the oral bioavailability of cyclosporin. Patients using cyclosporin are suggested to avoid concurrent intake of cordyceps.
關聯:
2nd World congress of the board of Pharmaceutical sciences of FIP
