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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 2 0名健康男性志愿者口服单剂量佐米曲普坦 5mg,给药后 ,连续采集血样至 2 4h ,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 ,Tmax1 .6 0± 0 . 2 4h ,Cmax9 .73±1. 4 3ng·mL-1 T1/ 2α1. 72± 0 .4 6h ,T1/ 2 β4 . 5 2± 0 . 97h ,AUC0 -t5 5 . 5 9± 5 . 12ng·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。
Objective To establish a liquid chromatography-mass spectrometry (LC-MS / MS) method for the determination of zolmitriptan in human plasma and study the pharmacokinetics of zolmitriptan in Chinese healthy volunteers. Methods Twenty healthy male volunteers were given a single oral dose of 5 mg of zolmitriptan. After administration, blood samples were collected continuously for 24 hours. Plasma was obtained and the concentration of zolmitriptan was analyzed by LC-MS. Results Zolmitriptan’s time curve was in accordance with the two-compartment model of oral absorption with lag time, Tmax1.60 ± 0.24h, Cmax9.73 ± 1.4ng · mL-1 T1 / 2α1.72 ± 0. 4 6h, T1 / 2 β4. 5 2 ± 0. 97h, AUC0-t5 5. 5 9 ± 5 12ng · mL-1 · h. Conclusion The method is convenient and sensitive, and provides a methodological basis for the determination of its plasma concentration and pharmacokinetics.