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人参皂苷Rg3的大鼠体内代谢及药代动力学研究

In vivo rat metabolism and pharmacokinetic studies of ginsenoside Rg3.

作者信息

Qian Tianxiu, Cai Zongwei, Wong Ricky N S, Mak Nai Ki, Jiang Zhi-Hong

机构信息

Department of Chemistry, Hong Kong Baptist University, 224 Waterloo Road, Kowloon, Hong Kong, SAR, China.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Feb 25;816(1-2):223-32. doi: 10.1016/j.jchromb.2004.11.036.

Abstract

Metabolism of an anti-tumor active component of Panax ginseng, ginsenoside (20R)-Rg(3), was studied for better understanding its pharmacokinetics in rat. LC-MS was used to determine Rg(3) and its metabolites in rat plasma, urine and feces samples. An average half-life of 18.5 min was obtained after the ginsenoside was intravenously dosed at 5 mg/kg. However, Rg(3) was not detected in rat plasma collected after oral administration at 100 mg/kg. Only 0.97-1.15% Rg(3) of the dosed amount was determined in feces. Hydrolysis and oxygenated metabolites were detected and identified in feces collected after oral administration by using LC-MS and MS-MS.

摘要

为了更好地了解人参抗肿瘤活性成分人参皂苷(20R)-Rg(3)在大鼠体内的药代动力学,对其代谢情况进行了研究。采用液相色谱-质谱联用技术测定大鼠血浆、尿液和粪便样本中的Rg(3)及其代谢产物。人参皂苷以5mg/kg静脉给药后,平均半衰期为18.5分钟。然而,口服100mg/kg后收集的大鼠血浆中未检测到Rg(3)。粪便中仅检测到给药量的0.97-1.15%的Rg(3)。通过液相色谱-质谱联用和串联质谱技术,在口服给药后收集的粪便中检测并鉴定出了水解代谢产物和氧化代谢产物。

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