AbstractGinsenoside H dripping pill (GH) is a novel clinical‐stage adjuvant for the treatment of non‐small cell lung cancer. In this study, the pharmacokinetics of ginsenoside Rh2, the major anticancer ingredient of GH, was investigated in healthy volunteers. Enrolled volunteers were assigned to 3 cohorts—7.8, 15.6, and 31.2 mg—and received single and/or multiple GH orally. Blood samples were assayed by a validated bioanalytical method, and drug concentrations were analyzed using a noncompartmental methodology. The results showed that ginsenoside Rh2 was absorbed with medium speed and reached Cmax a median of 3 hours after administration. The exposure of ginsenoside Rh2 was approximately dose‐dependent in terms of AUC and Cmax. The plasma concentration of ginsenoside Rh2 reached steady state after oral administration of GH twice daily for 5 days. There was no obvious accumulation in exposure parameters in the multiple‐dose study.