目的:建立测定人血浆中罗格列酮的液相色谱-质谱-质谱联用法,并用于临床药动学研究。方法: 血浆样品经液-液萃取后,以乙腈-水-甲酸(90:10:0．5)为流动相,采用Zorbax SB—C18柱分离,通过电喷雾离子化四极杆串联质谱,以选择反应监测(SRM)方式进行检测。用于定量分析的离子反应分别为m／z 358→ 135(罗格列酮)和m／z 256→167(内标苯海拉明)。结果:标准曲线线性范围为0．50～1 000μg·L-1,定量下限为0．50μg·L-1,日内、日间精密度(RSD)均小于7．4％。应用此法测试了20名男性健康受试者口服酒石酸罗格列酮片(相当于罗格列酮4 mg)后血浆中罗格列酮的浓度。结论:该法灵敏、快速、准确,操作简便、线性范围宽,适用于罗格列酮的临床药动学研究。 Objective: To establish a liquid chromatography-mass spectrometry-mass spectrometry (LC-MS / MS) method for the determination of rosiglitazone in human plasma and to study it in clinical pharmacokinetics. METHODS: Plasma samples were separated by liquid-liquid extraction using acetonitrile-water-formic acid (90: 10: 0.5) as mobile phase and separated on a Zorbax SB-C18 column by electrospray ionization quadrupole mass spectrometry Select the reaction monitoring (SRM) way to detect. The ion reactions used for quantitative analysis were m / z 358 → 135 (rosiglitazone) and m / z 256 → 167 (diphenhydramine internal standard), respectively. Results: The linear range of the standard curve was 0.50-1 000 μg · L-1, and the lower limit of quantification was 0.50 μg · L-1. The RSD of intra-day and inter-day were less than 7.4%. Using this method, rosiglitazone tartrate tablets (equivalent to 4 mg rosiglitazone tablets) were tested for plasma rosiglitazone concentrations in 20 healthy male subjects. Conclusion: The method is sensitive, rapid, accurate, simple and easy to operate with wide linear range and is suitable for clinical pharmacokinetic study of rosiglitazone.