Abstract

Vitexin was isolated from the leaves of Crataegus pinnatifida Bge. var major, and its pharmacokinetics and bioavailability were carried out via validated high-performance liquid chromatography (HPLC) method using hesperidin as internal standard in healthy rats after intravenous and oral administration at a dose of 10 mg/kg and 30 mg/kg, respectively. The pharmacokinetic parameters were calculated by both compartmental and non-compartmental approach. When intravenous administration was used，the elimination half-life (t_1/2β), the mean residence (MRT_0→t), the total body clearance (CL) were 46.01 ± 0.810 min, 26.23 ± 1.51 min and 0.031 ± 0.035 L/kg·min. When oral administration was used, the t_max and C_max were 15.82 ± 0.172 min and 0.51 ± 0.015 μg/ml, the MRT_0→t and CL were 60.41 ± 5.41 min and 0.71 ± 0.056 L/kg·min. The result showed that vitexin was rapidly eliminated and presented a low absolute bioavailability (F), 4.91 ± 0.761%.

Key words: Bioavailability, high-performance liquid chromatography (HPLC), pharmacokinetics, rat plasma, vitexin.