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Ginsenoside (G-Re, G-Rg1, G-Rg2, G-F1, G-Rh1) and protopanaxatriol in human plasma and urine were simultaneously determined by LC-MS/MS and its application in a pharmacokinetic study of G-Re in volunteers.

Simultaneous determination of ginsenoside (G-Re, G-Rg1, G-Rg2, G-F1, G-Rh1) and protopanaxatriol in human plasma and urine by LC-MS/MS and its application in a pharmacokinetics study of G-Re in volunteers.

机构信息

Department of Pharmacy, Beijing Hospital, The Ministry of Health, East-City District, Beijing, PR China.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Jul 15;879(22):2011-7. doi: 10.1016/j.jchromb.2011.05.018. Epub 2011 May 23.

Abstract

Ginsenoside Re (G-Re) improved the memory function of experimental animals in a preclinical study. Several types of saponins including G-Rg1, G-Rg2, G-F1, G-Rh1, and protopanaxatriol (PPT) may be the metabolites of G-Re according to reports from preclinical trials. In order to support a study of the pharmacokinetics of G-Re, an analytical method for G-Re and the co-detection of its probable metabolites using liquid chromatography tandem mass spectrometry (LC-MS/MS) was developed and validated. Solid phase extraction was utilized in the sample preparation. Separation of the analytes was achieved using a gradient elution (0.05% formic acid-methanol-acetonitrile, each organic phase containing 0.05% formic acid) at a flow rate of 0.3 mL/min with a retention time of approximately 2.88 min for G-Re. Data were acquired in the multiple reaction mode (MRM) and the linear range of the standard curve of plasma and urine samples for G-Re was 0.05-20 ng/mL with r(2)≥0.99. In the analysis of probable metabolites, G-Re, G-Rg1, G-F1, G-Rh1 and PPT were all detected in samples; however, G-Rg2 was not detected.

摘要

在一项临床前研究中,人参皂苷 Re (G-Re) 改善了实验动物的记忆功能。根据临床前试验的报告,包括 G-Rg1、G-Rg2、G-F1、G-Rh1 和原人参三醇 (PPT) 在内的几种类型的皂苷可能是 G-Re 的代谢物。为了支持 G-Re 药代动力学的研究,开发并验证了一种使用液相色谱串联质谱 (LC-MS/MS) 同时检测 G-Re 及其可能代谢物的分析方法。样品制备采用固相萃取法。采用梯度洗脱(0.05%甲酸-甲醇-乙腈,各有机相含有 0.05%甲酸),流速为 0.3 mL/min,G-Re 的保留时间约为 2.88 min,实现了分析物的分离。数据以多反应监测模式 (MRM) 采集,血浆和尿液样品中 G-Re 的标准曲线线性范围为 0.05-20 ng/mL,r(2)≥0.99。在分析可能的代谢物时,在样品中均检测到 G-Re、G-Rg1、G-F1、G-Rh1 和 PPT;然而,未检测到 G-Rg2。

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