Central Laboratory, Guangdong Provincial Hospital of Traditional Chinese Medicine, Guangzhou University of Chinese Medicine, and Guangdong Provincial Academy of Chinese Medical Sciences, Guangzhou, China.
J Clin Pharmacol. 2010 Mar;50(3):285-92. doi: 10.1177/0091270009344334. Epub 2009 Nov 25.
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.
在健康的中国志愿者中评估了人参皂苷 Rd（Rd）的药代动力学和安全性。在单剂量研究中，采用了随机、开放标签、3 向交叉设计。参与者被分配接受 10、45 或 75 mg Rd 静脉输注，每个剂量间隔 2 周洗脱期。Rd 的血浆水平与剂量成正比，在所研究的剂量范围内，平均 C(max)和 AUC(0-无穷大)范围为 2.8-19.3 mg/L 和 27.9-212.5 mg x h/L。人参皂苷 Rd 从血浆中缓慢清除（t(1/2Z)=17.7-19.3 小时）。在多剂量研究中，每天给予 10 mg Rd 一次，连续 6 天。观察到轻微的药物蓄积。平均稳态 C(max)、AUC(0-无穷大)和 AUC(ss)分别为 4.0 mg/L、51.7 mg x h/L 和 26.4 mg x h/L。t(1/2Z)为 20.5 小时，与单剂量值相似。人参皂苷 Rd 耐受性良好，无剂量相关不良事件模式。它具有良好的药代动力学和安全性特征，使该药物能够在针对急性缺血性中风患者的未来临床研究中进行探索。
