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

WANG Ya-qin;YIN Jia-jun;MAO Yu-chang;HU Zhuo-han;HUANG Jian-ming;School of Pharmacy,Fudan University;Ruide Research Institute for Liver Diseases [Shanghai] Co.,Ltd.;  
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.
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