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中国临床药理学与治疗学 ›› 2014, Vol. 19 ›› Issue (2): 171-175.

• 定量药理学 • 上一篇    下一篇

荷叶碱在大鼠体内的药代动力学研究

顾圣莹, 朱冠华, 康雷, 李晓宇, 刘皋林   

  1. 上海交通大学附属第一人民医院临床药学室,上海 200080
  • 收稿日期:2013-03-21 修回日期:2014-02-17 出版日期:2014-02-26 发布日期:2014-03-31
  • 通讯作者: 刘皋林,男,教授,博士研究生导师,研究方向:临床药理学。Tel: 021-63244200 E-mail: gaolinliu@aliyan.com;李晓宇,男,副教授,硕士研究生导师,研究方向:临床药理学。Tel: 021-37798312 E-mail: xyljaylxb@163.com
  • 作者简介:顾圣莹,女,硕士,药师,研究方向:药代动力学。Tel: 021-37798731 E-mail: gsy15815@163.com
  • 基金资助:
    上海交通大学医学院科研基金项目(JYY0906);教育部高等学校博士学科点专项科研基金(20110073120097);科技部十二五重大新药创制专项(2011ZX09302-007-02)

Pharmacokinetics of nuciferine in rats

GU Sheng-ying, ZHU Guan-hua, KANG Lei, LI Xiao-yu, LIU Gao-lin   

  1. Clinical Department of Pharmacy, Shanghai First People's Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200080, China
  • Received:2013-03-21 Revised:2014-02-17 Online:2014-02-26 Published:2014-03-31

摘要: 目的: 建立大鼠血浆中荷叶碱的HPLC测定方法并进行大鼠体内药代动力学研究。方法: 大鼠尾静脉注射后,不同时间点眼底静脉丛取血,乙酸乙酯提取大鼠血浆样品的荷叶碱,HPLC测定大鼠血浆中荷叶碱的含量,DAS软件计算药代动力学参数。结果: 荷叶碱在大鼠体内的t1/2β为(1.73±0.58) h,V为(5.03±0.24) L/kg,CL为(4.23±0.78)L·h-1·kg-1,药时曲线下面积(AUC0-inf)为(2.35±0.46) mg·L-1·h;在血浆中的平均驻留时间(MRT)为(1.51±0.31)h。结论: 所建立的HPLC分析方法快速、准确、简便,能够满足荷叶碱药代动力学的研究要求。按 10 mg/kg 单剂量单次静脉给药后,荷叶碱主要在血浆中分布,消除速度较快。

关键词: 荷叶碱, 药代动力学, 高效液相色谱法

Abstract: AIM: To study the pharmacokinetics of nuciferine after intravenous administration in rats using high performance liquid chromatogram (HPLC).METHODS: Nuciferine was administered by intravenous injection in rats and plasma was collected from fundus oculi venous plexus. Liquid-liquid extract procedure was employed for the extraction of nuciferine in rat plasma. The concentrations of nuciferine in plasma were measured by using HPLC method and the pharmacokinetic parameters were calculated by DAS.RESULTS: The main pharmacokinetic parameters of nuciferine after intravenous injection were as follows: t1/2 was (1.73±0.58) h, V was (5.03±0.24) L/kg, CL was (4.23±0.78) L·h-1·kg-1, AUC0-inf was (2.35±0.46) mg·L-1·h, MRT was (1.51±0.31) h.CONCLUSION: The HPLC method for the determination of nuciferine in rat plasma is sensitive, stable and rapid, which is successfully employed for the pharmacokinetic study of nuciferine in rats. After intravenous injection in a dose of 100 mg/kg, intensity distribution of nuciferine in plasma and a high elimination rate are investigated.

Key words: nuciferine, pharmacokinetic, HPLC

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