Pharmacokinetics and safety of ginsenoside Rd following a single or multiple intravenous dose in healthy Chinese volunteers.
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.
Zeng
Xing
X
Central Laboratory, Guangdong Provincial Hospital of Traditional Chinese Medicine, Guangzhou University of Chinese Medicine, and Guangdong Provincial Academy of Chinese Medical Sciences, Guangzhou, China.
Deng
Yuanhui
Y
Feng
Yi
Y
Liu
Yiming
Y
Yang
Liu
L
Huang
Yu
Y
Sun
Jing
J
Liang
Weixiong
W
Guan
Yongyuan
Y
D000328:Adult; D019540:Area Under Curve; D044466:Asian People; D002681:China; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D005260:Female; D036145:Ginsenosides / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics*; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D008657:Metabolic Clearance Rate; D012016:Reference Values; D053719:Tandem Mass Spectrometry
D036145:Ginsenosides; C049863:ginsenoside Rd