20(R)-人参皂苷Rg3人体药代动力学研究

目的　研究20(R)-人参皂苷Rg3(GRg3)人体药代动力学。方法高效液相色谱－紫外检测法。结果　8名健康志愿者单剂量口服3.2mg.kg^-1GRg3,其药时曲线符合口服吸收有滞后时间的二房室模型,T_max为(0.66±0.10)h,C_max为(16±6)ng.mL^-1,T_1/2α为(0.46±0.12)h,T_1/2β为(4.9±1.1)h,T_1/2(Ka)为(0.28±0.04)h,AUC_0-∞为(77±26)ng.mL^-1.h;6名健康志愿者单剂量口服0.8mg.kg^-1GRg3,由于血药浓度低,可测数据点少,未进行模型模拟;两组给药剂量与相应C_max实测值比较,二者成正比关系。结论　本品口服吸收快,消除也较快,但血药浓度很低。在所试剂量范围内,GRg3属一级动力学吸收、消除过程。

PHARMACOKINETIC STUDIES OF 20(R)-GINSENOSIDE RG3 IN HUMAN VOLUNTEERS

AIM: To study the pharmacokinetics of 20 (R)-ginsenoside Rg3 (GRg3) in human. METHODS: High-performance liquid chromatography-ultraviolet detection method was used in this study. RESULTS: The pharmacokinetics of GRg3 in 14 healthy volunteers were investigated. After a single oral dose of 3.2 mg.kg-1 in 8 male volunteers, the plasma concentration-time course fitted well to a two-compartment open model, with the following pharmacokinetic parameters: Tmax(0.66 +/- 0.10) h, Cmax(16 +/- 6) ng.mL-1, T1/2 alpha(0.46 +/- 0.12) h, T1/2 beta(4.9 +/- 1.1) h, T1/2(Ka)(0.28 +/- 0.04) h, AUC0-infinity(77 +/- 26) ng.mL-1.h. No kinetic analysis was made after an oral dose of 0.8 mg.kg-1 GRg3 in 6 other volunteers because of the low concentration, but a good correlation between Cmax and dosage of the two groups was found. CONCLUSION: The absorption of GRg3 was rapid in man, and its elimination was rapid after oral administration of ginsenoside Rg3. The pharmacokinetic results shows that it exhibited first order kinetic characteristics.