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目的建立测定人血浆中佐米曲普坦血药浓度的液质联用方法, 研究佐米曲普坦在中国健康志愿者体内药代动力学.方法 20名健康男性志愿者口服单剂量佐米曲普坦5 mg, 给药后, 连续采集血样至24 h, 分离得到血浆, 采用液质联用分析佐米曲普坦血药浓度.结果佐米曲普坦药时曲线符合口服吸收有滞后时间的二房室模型,Tmax 1.60±0.24 h, Cmax 9.73±1.43 ng·mL-1. T1/2α1.72±0.46 h, T1/2β 4.52±0.97 h, AUC0-t 55.59±5.12 ng·mL-1·h.结论本方法操作便捷, 灵敏度高, 为其血药浓度测定及药代动力学研究提供了方法学基础.“,”Aim To establish a new and sensitive HPLC-MS method for the determination of zolmitriptan in human plasma and study the pharmacokinetics of zolmitriptan in healthy volunteers. Methods A single oral dose of 5 mg of zolmitriptan tablet was given to 20 healthy male volunteers. After dosing, blood samples were collected for a period of 24 h, and zolmitriptan concentration in plasma was analyzed by HPLC-MS. Results The plasma concentration-time course fitted well a two-compartment open model with a lag time, giving the following pharmacokinetic parameters: Tmax 1.60±0.24 h, Cmax 9.73±1.43 ng·mL-1. T1/2α1.72±0.46 h, T1/2β 4.52±0.97 h, and AUC0-t 55.59±5.12 ng·mL-1·h. Conclusion The improved analytical method for zolmitriptan is rapid,sensitive and suitable for application to pharmacokinetic studies and routine determination of numerous samples.