The aim of this study was to investigate the effect of quercetin on the bioavailability of diltiazem after administering diltiazem (15 mg/kg) orally to rabbits either co-administered or pretreated with quercetin (2, 10, 20 mg/kg). The plasma concentrations of diltiazem in the rabbits pretreated with quercetin were increased significantly (p<0.05, at 2 mg/kg; p<0.01, at 10 and 20 mg/kg) compared with the control, but the plasma concentrations of diltiazem co-administered with quercetin were not significant. The areas under the plasma concentration-time curve (AUC) and the peak concentrations (Cmax) of the diltiazem in the rabbits pretreated with quercetin were significantly higher (p<0.05, at 2 mg/kg; p<0.01, at 10 and 20 mg/kg) than the control. The absolute bioavailability (AB%) of diltiazem in the rabbits pretreated with quercetin was significantly (p<0.05 at 2 mg/kg, p<0.01 at 10 and 20 mg/kg) higher (9.10-12.81%) than the control (4.64%). AUC, AB% and Cmax of diltiazem co-administered with quercetin were higher than the control, but these were not significant. The bioavailibility of diltiazem in the rabbits pretreated with quercetin is increased significantly compared with the control, but not in the rabbits co-administered with quercetin. The increased bioavailability of diltiazem in the rabbits pretreated with quercetin might have been resulted result from the quercetin, which inhibits the efflux pump P-glycoprotein and the first-pass metabolizing enzyme CYP 3A4.