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Planta Med 2009; 75(8): 797-802
DOI: 10.1055/s-0029-1185400
Pharmacology
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Characterization of Pharmacokinetic Profiles and Metabolic Pathways of 20(S)-Ginsenoside Rh1 in vivo and in vitro

Li Lai1 , Haiping Hao1 , Yitong Liu1 , Chaonan Zheng1 , Qiong Wang1 , Guangji Wang1 , Xijin Chen1
  • 1Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, P. R. China
Further Information

Publication History

received Sept. 24, 2008 revised January 12, 2009

accepted January 20, 2009

Publication Date:
05 March 2009 (online)

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Abstract

20(S)-Ginsenoside Rh1 is one of the important protopanaxatriol ginsenosides and has been reported to be the main hydrolysis product reaching the systemic circulation after oral ingestion of ginseng. However, its pharmacokinetic characteristics and metabolic fate have never been reported. The present study was therefore designed to elucidate its pharmacokinetic profiles and metabolic pathways both in vivo and in vitro. The absolute bioavailability of 20(S)-ginsenoside Rh1 in rats was only 1.01 %. Identification of metabolites showed that, after intragastrical administration of ginsenoside Rh1, two mono-oxygenated metabolites were detected from the urine, bile, liver tissue, and intestinal tract content, while the de-glucosylated product, 20(S)-protopanaxatriol, was only found in the contents of the intestinal tract. An in vitro incubation study confirmed that the CYP450-catalyzed mono-oxygenation, the intestinal bacteria mediated de-glucosylation, and the gastric acid mediated hydration reaction were the main metabolic pathways of 20(S)-ginsenoside Rh1. The presystemic metabolism as evidenced from this study may partially explain its poor bioavailability.

Key words

20(S)‐ginsenoside Rh1 - metabolism - pharmacokinetics - Panax ginseng C. A. Meyer - Araliaceae

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Prof. Dr. Guangji Wang

Key Lab of Drug Metabolism and Pharmacokinetics
China Pharmaceutical University

24 Tong jia xiang street Mail Box 210

Nanjing 210009

People's Republic of China

Phone: + 86 25 83 27 11 28

Fax: + 86 25 85 30 67 50

Email: guangjiwang@hotmail.com

Dr. Haiping Hao

Key Lab of Drug Metabolism and Pharmacokinetics
China Pharmaceutical University

24 Tong jia xiang street Mail Box 210

Nanjing 210009

People's Republic of China

Phone: + 86 25 85 39 10 89

Fax: + 86 25 85 30 67 50

Email: hhp_770505@yahoo.com.cn

    www.thieme-connect.de/ejournals/toc/plantamedica