【作者】 顾琦； 陈笑艳； 刘丹； 王英武； 钟大放；

【Author】 GU Qi~1, CHEN Xiao-yan~1, LIU Dan~1, WANG Ying-wu~1, ZHONG Da-fang~(1,2,*)(1. Laboratory of Drug Metabolism and Pharmacokinetics,Shenyang Pharmaceutical University, Shenyang 110016, China;2. Research Center of Drug Metabolism, Jilin University,Changchun 130023, China)

【机构】 沈阳药科大学药物代谢与药物动力学实验室； 吉林大学药物代谢研究中心；

【摘要】 <正>依那普利属第二代血管紧张素转换酶抑制药,其乙酯部分在体内被迅速水解,转化成活性代谢物依那普利拉,同时测定人体血浆中依那普利及依那普利拉对其药物动力学研究具有重要意义。文献报道多以免疫法测定体液中依那普利和依那普利拉,近年来,有报道采用GC/MS法和LC-MS/MS法同时测定人体血浆中依那普利及依那普利拉,这些方法依那普利及依那普利拉定量下限最低仅为0.2和1.0ng/mL。本工作旨在建立一种更快速、灵敏的LC-MS/MS法同时测定人体血浆中的依那普利及更多还原

【Abstract】 A rapid, sensitive and specific liquid chromatography-tandem mass spectrometry method was developed and validated for simultaneous determination of enalapril and its major active metabolite enalaprilat in human plasma. The analytes were extracted from plasma samples by liquid-liquid extraction, separated on a Zorbax Extend-C₁₈ column and detected by tandem mass spectrometry with a TurboIonSpray ionization interface. Daidzein was used as the internal standard.The method has a lower limit of quantification （LLOQ） of 0. 1 ng/mL for both enalapril and enalaprilat. The standard calibration curves for both enalapril and enalaprilat were linear in the concentration ranges 0. 10～100.0 ng/mL in human plasma. The intra-and inter-run precisions, were less than 7. 7 and 7.8%, determined from QC samples for enalapril and enalaprilat, and accuracy was within ±3. 9% and ±2.7 %, respectively. The method was successfully applied for the evaluation of the pharmacokinetics of enalapril and enalaprilat in 20 volunteers after an oral dose of 10 mg enalapril maleate.更多还原