建立一种简便、灵敏、准确的液相色谱-串联质谱法以同时测定人血浆中氟吡汀及其活性代谢物D-13223浓度.本文采用三重四级杆液质联用仪,电喷雾电离源(ESI),多反应离子监测(MRM)的正离子模式进行检测,以C18柱为色谱柱,乙腈-水-氨(55∶45∶0.1,v/v/v)为流动相,液液萃取法提取血浆样品中氟哌汀、D-13223及稳定同位素内标以进行色谱分析.氟吡汀在10.00-2000.00 ng/mL浓度范围内线性关系良好,D-13223在2.00-400.00 ng/mL浓度范围内线性关系良好.氟吡汀及D-13223质量控制(QC)样品的批内和批间精密度均小于9.26％,准确度范围-5.80％-3.31％.氟吡汀、D-13223及内标的提取回收率均在88.3％-97.2％之间.本法已成功应用于健康男性志愿者口服100 mg马来酸氟吡汀胶囊后血浆中氟吡汀及其活性代谢物D-13223的药代动力学研究.“,”In the present study,we developed a simple,sensitive,precise,and accurate liquid chromatography-tandem mass spectrometric(LC-MS/MS)method and validated such approach for simultaneous determination of flupirtine and its active metabolite D-13223 in human plasma.The flupirtine,D-13223,and stable isotope internal standard(IS)were extracted from plasma samples by liquid-liquid extraction and chromatographed on a Ci8 column with a mobile phase consisting of acetonitrile-water-ammonia(55∶45∶0.1,v/v/v)at a flow rate of 0.25 mL/min.Detection was performed on a triple quadrupole tandem mass spectrometer with an electrospray ionization source(ESI)by multiple reaction monitoring(MRM)in positive ion mode.The linear calibration curves were obtained within the concentration range of 10.00-2000.00 ng/mL for flupirtine and 2.00-400.00 ng/mL for D-13223.The intra-and inter-run RSD,calculated from quality control(QC)samples,was less than 9.26％for flupirtine and D-13223.The accuracy was-5.80％-3.31％for flupirtine and D-13223.The extraction recoveries of flupirtine,D-13223,and their IS were all between 88.3％-97.2％.The method was successfully applied to investigate the pharmacokinetic profiles of flupirtine and its active metabolite D-13223 in human plasma following peroral administration of 100 mg flupirtine maleate capsules in healthy male Chinese volunteers.