摘要
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。
Aim To establish a new and sensitive HPLC-MS method for the determination ofzolmitriptan 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 inplasma was analyzed by HPLC-MS. Results The plasma concentration-time course fitted well atwo-compartment open model with a lag time, giving the following pharmacokinetic parameters: T_(max)1.60 ± 0.24 h, C_(max) 9.73 ± 1.43 ng·mL^(-1). T_(1/2α)1.72±0.46 h, T_(1/2β) 4.52 + 0.97 h,and AUC_(0-t) 55.59 ± 5.12 ng·mL^(-1)·h. Conclusion The improved analytical method forzolmitriptan is rapid, sensitive and suitable for application to pharmacokinetic studies and routinedetermination of numerous samples.
