荷叶碱在大鼠体内的药代动力学研究  

Pharmacokinetics of nuciferine in rats

作　　者：顾圣莹[1] 朱冠华[1] 康雷[1] 李晓宇[1] 刘皋林[1] 

机构地区：[1]上海交通大学附属第一人民医院临床药学室,上海200080

出　　处：《中国临床药理学与治疗学》2014年第2期171-175,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：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)

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10mg/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。ABSTRACT AIM： To study the pharmacoki netics of nuciferine after intravenous administra- tion in rats using high performance liquid chro matogram （HPLC）. METHODS： Nuciferine was administered by intravenous injection in rats and plasma was collected from fundus oculi venous plexus. Liquid-liquid extract procedure was em ployed for the extraction of nuciferine in rat plasma. The concentrations of nuciferine in plas ma were measured by using HPLC method and the pharmacokinetic parameters were calculated by DAS. RESULTS： The main pharmacokinetic parameters of nuciferine after intravenous injec tion were as follows： tl/2 was （1.73±0.58） h,Vwas （5.034±0.24） L/kg, CL was （4.23± 0.78） L. h-1 . kg-1, AUC0-i.f was （2.35 ± 0.46） mg ~ L-1 . h, MRT was （1.51±0.31） h. CONCLUSION： The HPLC method for the de- termination of nuciferine in rat plasma is sensi tive, stable and rapid, which is successfully em ployed for the pharmacokinetic study of nucifer ine in rats. After intravenous injection in a dose of 100 mg/kg, intensity distribution of nucifer ine in plasma and a high elimination rate are in vestigated.

关 键 词：荷叶碱 药代动力学 高效液相色谱法 

分 类 号：R965.2[医药卫生—药理学]