目的建立一种简便、灵敏的测定人体血浆和尿液中罗通定浓度的高效液相色谱-串联质谱(HPLC-MS/MS)方法。方法血浆、尿液样品分别采用乙腈沉淀处理后,进样分析。采用Agilent-ECLIPSE-C18柱(2.1mm×150mm,5μm),以乙腈-0.2%甲酸溶液=85∶15为流动相,采用正离子,多反应监测方式测定样品浓度。检测离子为m/z356.3→192.3(罗通定)和m/z 285.0→193.0(地西泮,内标)。结果罗通定血浆及尿样均在2.5～1 000ng.mL-1与峰面积线性关系良好(r=0.999 4);最低定量浓度均为2.5ng.mL-1。日内与日间RSD均<10%,血浆样品回收率在91.4%～109.2%,尿样回收率在88.63%～115.8%。结论本方法简便快速、灵敏准确,适用于罗通定在人体内的药物动力学研究。 Objective To establish a simple and sensitive method for the determination of lootidine in human plasma and urine by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS / MS). Methods Plasma and urine samples were treated with acetonitrile precipitation and injection analysis. Agilent-ECLIPSE-C18 column (2.1mm × 150mm, 5μm) with acetonitrile-0.2% formic acid solution = 85:15 was used as the mobile phase, and the concentration of the sample was determined by the method of positive ion and multiple reaction monitoring. The detection ions were m / z 356.3 → 192.3 (Rotundine) and m / z 285.0 → 193.0 (diazepam, internal standard). The results of lovastatin plasma and urine samples were 2.5 ~ 1000ng.mL-1 and the peak area of ​​a good linear relationship (r = 0.999 4); the lowest quantitative concentrations were 2.5ng.mL-1. Intra-day and inter-day RSD were <10%, plasma sample recovery was 91.4% ~ 109.2%, urine sample recovery was 88.63% ~ 115.8%. Conclusion The method is simple, rapid, sensitive and accurate and is suitable for the study of pharmacokinetics of Luo Tong Ding in the human body.