Pharmacokinetics and Safety of Ginsenoside Rd Following a Single or Multiple Intravenous Dose in Healthy Chinese Volunteers

Abstract

The pharmacokinetics and safety of ginsenoside Rd (Rd) were assessed in healthy Chinese volunteers. In the single-dose study, a randomized, open-label, 3-way crossover design was used. Participants were assigned to receive 10, 45, or 75 mg Rd by intravenous infusion, with a 2-week washout period between dosing periods. Plasma levels of Rd were found to be proportional to dose, with the mean C(max) and AUC(0-infinity) ranging from 2.8 to 19.3 mg/L and 27.9 to 212.5 mg x h/L over the dose range studied. Ginsenoside Rd was slowly cleared from plasma (t(1/2Z) = 17.7-19.3 hours). In the multiple-dose study, 10 mg Rd was administered once daily for 6 days. Slight drug accumulation was noted. The mean steady-state C(max), AUC(0-infinity), and AUC(ss) were 4.0 mg/L, 51.7 mg x h/L, and 26.4 mg x h/L, respectively. The t(1/2Z) was 20.5 hours, which was similar to the single-dose value. Ginsenoside Rd was well tolerated with no pattern of dose-related adverse events. It had a favorable pharmacokinetic and safety profile that enables the drug to be explored in future clinical studies that target patients with acute ischemic stroke.