Rapid Quantification of Astilbin in Rat Plasma by Liquid Chromatography-tandem Mass Spectrometry and Its Application to Pharmacokinetic Study  

作　　者：YIN Lei ZHANG Yun-hui ZHAO Sen CHENG Long-mei SHI Mei-yun YANG Yan SUN Yan-tong LIU Xi-dong FAWCETT J. Paul 

机构地区：[1]School of Life Sciences, Jilin University, Changchun 130012, P.R.China [2]Clinical Pharmacology Center, Research Institute of Translational Medicine, the First Hospital of Jilin University, Changchun 130061, P.R.China [3]National Engineering Laboratory for AIDS Vaccine,the Ministry of Education,Jilin University, Changchun 130012, P.R.China [4]Key Laboratory for Molecular Enzymology and Engineering, the Ministry of Education,Jilin University, Changchun 130012, P.R.China [5]School of Pharmaceutical Sciences, Jilin University, Changchun 130021, P. R. China [6]School of Pharmacy, University of Otago, Dunedin 9054, New Zealand

出　　处：《Chemical Research in Chinese Universities》2013年第6期1078-1082,共5页高等学校化学研究（英文版）

基　　金：the National Natural Science Foundation of China，the Science and Technology Major Specialized Projects for ＂Significant New Drugs Creation＂ of the 12th Five-year Plan of China，the National Key Technology R＆D Program of the Ministry of Science and Technology,China

摘　　要：Astilbin is a potential immunosuppressive agent with minor cytotoxicity. Its oral bioavailability is supposed to be rather low and therefore a sensitive analytical method is required for its pharmacokinetic study after oral administration. A simple, sensitive and rapid liquid chromatography-tandem mass spectrometry（LC-MS/MS） method was developed and validated for the determination of astilbin in rat plasma. Plasma samples were subjected to liquid-liquid extraction with ethyl acetate and separated by reversed phase high performance liquid chromatography（HPLC） with methanol-0.01%（volume fraction） formic acid（50：50, volume ratio） as mobile phase. Quantitive determination was achieved on negative LC-MS/MS by a multiple reaction moitoring method with transitions m/z 449.1→150.9（quantifier） and m/z 449.1→284.9（qualifier） for astilbin and m/z 128.9→42.0 for internal standard（IS）. A lower limit of quantification（LLOQ） of ng/mL was achieved within a short cycle time of 3.4 min. The method was successfully applied to a pharmacokinetic study involving oral and intravenous administrations of 6 mg/kg astilbin to six rats.Astilbin is a potential immunosuppressive agent with minor cytotoxicity. Its oral bioavailability is supposed to be rather low and therefore a sensitive analytical method is required for its pharmacokinetic study after oral administration. A simple, sensitive and rapid liquid chromatography-tandem mass spectrometry（LC-MS/MS） method was developed and validated for the determination of astilbin in rat plasma. Plasma samples were subjected to liquid-liquid extraction with ethyl acetate and separated by reversed phase high performance liquid chromatography（HPLC） with methanol-0.01%（volume fraction） formic acid（50：50, volume ratio） as mobile phase. Quantitive determination was achieved on negative LC-MS/MS by a multiple reaction moitoring method with transitions m/z 449.1→150.9（quantifier） and m/z 449.1→284.9（qualifier） for astilbin and m/z 128.9→42.0 for internal standard（IS）. A lower limit of quantification（LLOQ） of ng/mL was achieved within a short cycle time of 3.4 min. The method was successfully applied to a pharmacokinetic study involving oral and intravenous administrations of 6 mg/kg astilbin to six rats.

关 键 词：ASTILBIN Liquid chromatography-tandem mass spectrometry（LC-MS/MS） PHARMACOKINETICS RAT Plasma 

分 类 号：S859.796[农业科学—临床兽医学] O657.72[农业科学—兽医学]