Abstract: 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: T_max (0.66±0.10) h, C_max (16±6) ng.mL^-1, T_1/2α (0.46±0.12) h, T_1/2β (4.9±1.1) h, T_1/2(Ka) (0.28±0.04) h, AUC_0-∞ (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 C_max 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.