Abstract: Objective: To study the pharmacokinetics of 20(R)-Ginsenoside Rg3 in the human body. Methods: High-performance liquid chromatography-ultraviolet detection method was used in this study. Results: The pharmacokinetics of Ginsenoside Rg3 in 14 healthy volunteers were investigated. After a single oral dose of 3.2 mg·kg^-1 Ginsenoside Rg3 in 8 male volunteers, the plasma concentration-time course fitted in well with a two-compartment open model, with the following pharmacokinetic parameters: Tmax 0.66±0.10 h, Cmax 166 ng·mL^-1, T1/2α 0.46±0.12 h, T1/2β 4.9±1.1 h, T1/2(Ka) 0.28±0.04 h, AUC0-∞ 7726 ng·mL^-1·h, respectively. No kinetic analysis was made after an oral dose of 0.8 mg·kg^-1 Rg3 in other 6 volunteers because of the low concentration, but there was a good correlation between Cmax and dosage of the two groups. Conclusion: The absorption of Rg3 was rapid in the human body, and its elimination was rapid too after oral administration of Ginsenoside Rg3. The pharmacokinetic results shows that it exhibited the first-order kinetic characteristics.

Key words: 20R-Ginsenoside Rg3, HPLC, Pharmacokinetics, Human