荷叶碱在大鼠体内的药代动力学研究

Pharmacokinetics of nuciferine in rats

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.