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液质联用法测定人血浆中佐米曲普坦的浓度及其药动学研究

姚金成, 瞿延晖, 赵绪元, 胡领*, 朱荣华, 李焕德, 丁劲松   

  1. 1.湖南中医学院, 湖南 长沙 410007;
    2.中南大学湘雅二医院药剂科临床药学研究室, 湖南 长沙 410011
  • 收稿日期:2004-09-18 修回日期:2005-02-10 出版日期:2005-03-15 发布日期:2005-03-15
  • 通讯作者: 胡领*

Determination of Zolmitriptan in Human Plasma by High-Performance Liquid Chromatography-Electrospray Mass Spectrometry and Study on Its Pharmacokinetics

YAO Jin-cheng, QU Yan-hui, ZHAO Xu-yuan, Hu Ling*, ZHU Rong-hua, LI Huan-de, DING Jing-song   

  1. 1.Hunan College of TCM, Changsha 410007, China;
    2.Clinical Pharmacy Research Institute, The Second Xiangya Hospital of Central South University, Changsh a 410011, China
  • Received:2004-09-18 Revised:2005-02-10 Online:2005-03-15 Published:2005-03-15
  • Contact: Hu Ling*

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 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。

关键词: 佐米曲普坦, 佐米曲普坦, 佐米曲普坦, 药代动力学, 药代动力学, 药代动力学, 液质联用, 液质联用, 液质联用

Abstract: 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.

Key words: zolmitriptan, zolmitriptan, pharmacokinetics, pharmacokinetics, HPLC-MS, HPLC-MS

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Supporting: *Corresponding author. Tel.: 86-731-5524222-2363