液相色谱-串联质谱法快速高效测定大鼠血浆中对萼猕猴桃苷E的浓度及其药代动力学研究(英文)  

A rapid and sensitive liquid chromatography-tandem mass spectrometric method for determination of actinoside E in rat plasma and application to a pharmacokinetic study

作　　者：曲丽萍[1] 苏永华[1] 郑国银[1] 辛海量[1] 凌昌全[1] 

机构地区：[1]第二军医大学附属长海医院中医系,上海200433

出　　处：《中国天然药物》2013年第4期427-432,共6页

基　　金：supported by the National Natural Science Fund of China(Nos.81102336,81102849);the Special Project of Biological Medicine of Science and Technology Commission of Shanghai Municipality(No.10431900500)~~

摘　　要：目的:建立用于测定对萼猕猴桃苷E血药浓度的液相色谱-串联质谱分析方法,并探讨对萼猕猴桃苷E在大鼠体内的药代动力学。方法:血浆样品经乙酸乙酯萃取后,用LC-MS/MS进行测定分析。内标为对萼猕猴桃苷F,色谱柱为ZorbaxSB-C18(100mm×2.1mm,3.5μm),流动相为甲醇-0.1%甲酸溶液(50:50,V/V),流速0.3mLmin1。结果:对萼猕猴桃苷E浓度在0.52500ngmL1之间线性关系良好,提取回收率在83.2%85.5%之间,日内和日间精密度RSD分别在1.7%7.5%和2.0%8.9%之间,准确度在95.7%108.6%之间,大鼠口服100mgkg1和静注5mgkg1对萼猕猴桃苷E后,该药绝对生物利用度约0.27%。结论:建立的LC-MS/MS联用方法简单准确,灵敏度高,适用于大鼠血浆中对萼猕猴桃苷E的药代动力学研究。A highly sensitive liquid chromatography-tandem mass spectrometric （LC-MS/MS） method was developed for the determination of actinoside E in rat plasma. The analytes were extracted by ethyl acetate and an analogue of actinoside F was used as the internal standard. The mobile phase consisted of methanol-water （50 ： 50, V/V） containing 0.1% formic acid was delivered at a flow rate of 0.3 mL.min^-1 to a Zorbax SB-CI8 column （100 mm × 2.1 mm, 3.5μm）. The detection was performed by electrospray ionization mass spectrometry in the negative multiple reaction monitoring mode with a chromatograph run time of 3.0 min. Calibration curves of actinoside E were linear in the range of 0.5-2 500 ng＇mL-1. In this range, intra- and inter-day precision ranged from 1.7% to 7.5% and 2.0% to 8.9%, respectively. The accuracy ranged from 95.7% to 108.6%, and extraction recovery from 83.2% to 85.5%. This method was successfully applied to a pharmacokinetic study of actinoside E in rats after intravenous （5 mg＇kg-1） and oral （100 mg.kg^-1） administration, and the results showed that actinoside E was poorly absorbed with an absolute bioavailability being approximately 0.27%.

关 键 词：对萼猕猴桃苷E 大鼠血浆 LC-MS MS法 药代动力学 

分 类 号：R917[医药卫生—药物分析学]