Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS:Rg1 excretion in rat bile, urine and feces

作     者：Chiyu He Ru Feng Yupeng Sun Shifeng Chu Ji Chen Chao Ma Jie Fu Zhenxiong Zhao Min Huang Jiawen Shou Xiaoyang Li Yuzhu Wang Jinfeng Hu Yan Wang Juntian Zhang 

作者机构：State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences Beijing Analytical Application Center Shimadzu (China) Co. Ltd. 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2016年第6卷第6期

页      面：593-599页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1004[医学-公共卫生与预防医学(可授医学、理学学位)] 1001[医学-基础医学(可授医学、理学学位)] 10[医学] 100602[医学-中西医结合临床] 

基　　金：supported by the National Natural Science Foundation of China(Nos.81173578 and 81573493) Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD study(No.Z141102004414062) National 863 Program of China(No.2014AA020803) the PUMC Youth Fund and Fundamental Research Funds for the Central Universities(No.3332015136) the Fundamental Research Funds for Central Public Institutes(No.2015CX12) 

主　　题：Ginsenoside Rg1 Ginsenoside Rh1 Protopanaxatriol Excretion LC–MS/MS 

摘      要：Ginsenoside Rg1(Rg1), the major effective component of ginseng, has been shown to have multiple bioactivities, but low oral bioavailability. The aim of this study was to develop a simple, sensitive and rapid high performance liquid chromatography–tandem mass spectrometry(LC–MS/MS) method, which could be used to validate and quantify the concentrations of Rg1 and its metabolites in Sprague-Dawley rat bile,urine, and feces after oral administration(25 mg/kg). Calibration curves offered satisfactory linearity(r40.995)within the determined ranges. Both intra-day and inter-day variances were less than 15%, and the accuracy was within 80–120%. The excretion recoveries of Rg1, ginsenoside Rh1(Rh1), and protopanaxatriol(Ppt) in bile,urine, and feces combined were all greater than 70%. The fecal excretion recoveries of Rg1, Rh1, and Ppt were40.11%, 22.19%, and 22.88%, respectively, whereas 6.88% of Rg1 and 0.09% of Rh1 were excreted in bile.Urinary excretion accounted for only 0.04% of Rg1. In conclusion, the observed excretion profiles for Rg1 and its metabolites after oral administration are helpful for understanding the poor oral bioavailability of Rg1 and will aid further investigations of Rg1 as a pharmacologically active component.