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天然产物中新型抗肿瘤物质人参皂苷Rh2的高效液相色谱-质谱分析方法的建立及其在犬体内的药代动力学研究

Development of a HPLC-MS assay for ginsenoside Rh2, a new anti-tumor substance from natural product and its pharacokinetic study in dogs.

作者信息

Xie Hai-Tang, Wang Guang-Ji, Lv Hua, Sun Rui Wang Jian-Guo, Jiang Xi-Ling, Li Hao, Wang Wei, Huang Chen-Rong, Xu Mei-Juan

机构信息

Key laboratory of pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu.

出版信息

Eur J Drug Metab Pharmacokinet. 2005 Jan-Jun;30(1-2):63-7. doi: 10.1007/BF03226409.

Abstract

To develop a HPLC-MS method of determining ginsenoside Rh2 in dog plasma based on solid-phase extraction for pharmacokinetic studies. Six dogs were randomly assigned to two groups, either given 0.1 mg/kg dose intravenously or 1 mg/kg dose through oral gavage. Analysis using high performance liquid chromatography (HPLC) with ODS column, followed by detection with electrospray ionization(ESI) mass spectrometry(MS) in negative ion mode with 500 microM ammonium chloride in the mobile phase. The assays were validated over the concentration range of 2.0-1250.0 ng/ml in dog plasma. The intra- and inter- day precision were less than 10% in terms of RSD. The overall recovery was more than 80%. The validated assay was suitable for pharmacokinetic studies of ginsenoside Rh2 and the observed oral bioavailabilities of Rh2 were 17.6% and 24.8% for male and female dogs respectively.

摘要

建立一种基于固相萃取的高效液相色谱-质谱法测定犬血浆中人参皂苷Rh2,用于药代动力学研究。将6只犬随机分为两组,分别静脉注射0.1 mg/kg剂量或经口灌胃1 mg/kg剂量。采用高效液相色谱(HPLC),以ODS柱进行分析,随后在负离子模式下用电喷雾电离(ESI)质谱(MS)检测,流动相中含有500 microM氯化铵。该测定法在犬血浆浓度范围2.0 - 1250.0 ng/ml内得到验证。日内和日间精密度的相对标准偏差(RSD)均小于10%。总回收率超过80%。验证后的测定法适用于人参皂苷Rh2的药代动力学研究,观察到雄性和雌性犬Rh2的口服生物利用度分别为17.6%和24.8%。

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