20(S)原人参二醇奥克梯隆型差向异构体大鼠排泄研究(4)
[13] 杨秀伟，桂方晋，宋燕，等. 人参皂苷Rg2的排泄试验研究[J]. 中国中药杂志，2009，34(10)：1281.
[14] Gu Y， Wang G J， Sun J G，et al. Pharmacokinetic characterization of ginsenoside Rh2， an anticancer nutrient from ginseng， in rats and dogs [J]. Food Chem Toxicol，2009，47：2257.
Study on excretion of 20(S)-protopanaxadiolocotillol type epimers in rats
WU Xiang-meng， WANG Li， NI Ying-ying， WANG Hui， WANG Wen-yan*， MENG Qing-guo
(Pharmaceutical School， Yantai University， Yantai 264005， China)
[Abstract] Gindenosides are the active ingredients of Panax ginseng. 20(S)-protopanaxadiolocotillol type epimers are the main metabolites of 20(S)-protopanaxadiol. The previous studies showed that there are stereoselectivity difference in pharmacodynamics and pharmacokinetics between 24R-epimer and 24S-epimer. The purpose of this study was to explore the excretion of the epimers in bile， feces and urine of rat. Liquid chromatography tandem mass spectrometry method has been performed for determination of 24R-epimer and 24S-epimer in bile， feces and urine. 24R-epimer or 24S-epimer was intragastric administered to rats at a single dose of 10 mg·kg-1. Results showed that after administration the recovery of 24R-epimer and 24S-epimer in feces was 17.69% and 17.09%， respectively， while both of the two epimers were hardly detected in urine. The 48 h cumulative biliary excretion rate of 24R-epimer was 8.01% after administration， while only 1.47% for 24S-epimer. It indicated that there are stereoselectivity in biliary excretion of the epimers with intragastric administration.
[Key words] 20(S)-protopanaxadiol； ocotillol type； epimer； drug excretion
doi：10.4268/cjcmm20140730, 百拇医药(吴祥猛 王莉 倪莹莹 王慧 王文艳 孟庆国)
[14] Gu Y， Wang G J， Sun J G，et al. Pharmacokinetic characterization of ginsenoside Rh2， an anticancer nutrient from ginseng， in rats and dogs [J]. Food Chem Toxicol，2009，47：2257.
Study on excretion of 20(S)-protopanaxadiolocotillol type epimers in rats
WU Xiang-meng， WANG Li， NI Ying-ying， WANG Hui， WANG Wen-yan*， MENG Qing-guo
(Pharmaceutical School， Yantai University， Yantai 264005， China)
[Abstract] Gindenosides are the active ingredients of Panax ginseng. 20(S)-protopanaxadiolocotillol type epimers are the main metabolites of 20(S)-protopanaxadiol. The previous studies showed that there are stereoselectivity difference in pharmacodynamics and pharmacokinetics between 24R-epimer and 24S-epimer. The purpose of this study was to explore the excretion of the epimers in bile， feces and urine of rat. Liquid chromatography tandem mass spectrometry method has been performed for determination of 24R-epimer and 24S-epimer in bile， feces and urine. 24R-epimer or 24S-epimer was intragastric administered to rats at a single dose of 10 mg·kg-1. Results showed that after administration the recovery of 24R-epimer and 24S-epimer in feces was 17.69% and 17.09%， respectively， while both of the two epimers were hardly detected in urine. The 48 h cumulative biliary excretion rate of 24R-epimer was 8.01% after administration， while only 1.47% for 24S-epimer. It indicated that there are stereoselectivity in biliary excretion of the epimers with intragastric administration.
[Key words] 20(S)-protopanaxadiol； ocotillol type； epimer； drug excretion
doi：10.4268/cjcmm20140730, 百拇医药(吴祥猛 王莉 倪莹莹 王慧 王文艳 孟庆国)