异佛司可林在人肝微粒体与人工胃肠液中的代谢与降解  

Metabolism and degradation of isoforskolin in human liver microsomes and simulated gastrointestinal fluids

作　　者：汪亚勤[1] 殷嘉珺[1] 毛玉昌 胡卓汉[1,2] 黄建明[1] 

机构地区：[1]复旦大学药学院,上海201203 [2]瑞德肝脏疾病研究(上海)有限公司,上海201203

出　　处：《中成药》2016年第6期1244-1248,共5页Chinese Traditional Patent Medicine

基　　金：上海市科学技术委员会科技支撑项目(13401900502)

摘　　要：目的研究异佛司可林在人肝微粒体及人工胃肠液中的代谢与降解动力学。方法将异佛司可林与人肝微粒体、人工胃液、人工肠液进行体外共孵育,采用高效液相色谱-串联质谱(HPLC-MS/MS)法测定人肝微粒体孵育体系中异佛司可林的剩余浓度,高效液相色谱-紫外检测(HPLC-UV)法测定人工胃液、人工肠液中异佛司可林的剩余浓度。结果异佛司可林在人肝微粒体的t1/2为(34.90±3.42)min,CLint为(16.71±1.64)m L/(kg·min);在人工胃液和人工肠液中的t1/2分别为(46.97±6.46)h和(91.67±8.26)h。结论异佛司可林在人肝微粒体中代谢显著,在人工胃液和肠液中较稳定。AIM To investigate the in vitro metabolism and degradation of isoforskolin in human liver microsomes and simulated gastrointestinal fluids.METHODS Isoforskolin was incubated with human liver microsomes,simulated gastric fluid（SGF） and simulated intestinal fluid（SIF）,respectively.The residual concentrations of isoforskolin in microsomal incubates were determined by HPLC-MS/MS,and the concentrations in SGF and SIF were detected by HPLC-UV.RESULTS In human liver microsomes,the t1/2and CLintof isoforskolin were（34.90 ± 3.42） min and（16.71 ± 1.64） m L/（kg·min）,respectively.The t1/2values of isoforskolin in SGF and SIF were（46.97 ± 6.46） h and（91.67 ± 8.26） h,respectively.CONCLUSION Isoforskolin can be metabolized significantly in human liver microsomes,while it remains stable in SGF and SIF.

关 键 词：异佛司可林 代谢 降解 人肝微粒体 人工胃液 人工肠液 HPLC-MS/MS HPLC-UV 

分 类 号：R969.1[医药卫生—药理学]