小青龙颗粒中麻黄碱及伪麻黄碱在大鼠体内的药代动力学研究  

Pharmacokinetics of Ephedrine and Pseudoephedrine in Xiaoqinglong Granules by HPLC

作　　者：张建军[1] 欧丽娜[1] 李伟[1] 王景霞[1] 龙锐[1] 刘海波[1] 刘洋[1] 

机构地区：[1]北京中医药大学基础医学院,北京100029

出　　处：《中华中医药杂志》2010年第12期1991-1995,共5页China Journal of Traditional Chinese Medicine and Pharmacy

基　　金：国家中医药管理局中医药科学技术研究专项资助项目(No.06-07ZP03);教育部"211工程"三期项目~~

摘　　要：目的:建立测定小青龙颗粒中麻黄碱(ephedrine,E)、伪麻黄碱(pseudoephedrine,PE)血药浓度的HPLC法,并探讨二者在大鼠体内的药代动力学特征。方法:以盐酸苯丙醇胺为内标物,用HPLC内标法测定给药后不同时间点大鼠的血药浓度,将所得数据用3P97药代动力学程序处理,求出相关药代动力学参数。结果:E、PE分别在0.0152-1.52mg/mL和0.01485-1.485mg/mL的范围内线性关系良好(r=0.9995、r=0.9991),检测限分别为0.005、0.01mg/mL,平均回收率分别为100.6%和102.6%。两者平均日内、日间精密度分别为3.04%、4.82%和4.84%、3.99%;大鼠在灌服小青龙颗粒后,麻黄碱血药浓度-时间曲线呈一室模型,半衰期1.39h、清除速率0.50/h、生物利用度0.55(mg/mL)×h;伪麻黄碱血药浓度-时间曲线呈一室模型,半衰期2.65h、清除速率0.26/h、生物利用度0.44(mg/mL)×h。结论:小青龙颗粒中麻黄在配伍后,吸收过程加速,起效时间缩短。配伍加速了麻黄的代谢过程,减少了药物蓄积。Objective： To develop a HPLC method for the determination of ephedrine （E） and pseudoephdrine （PE） and to study the pharmacokinetics features of E and PE in SD rats. Methods： The plasma samples were extracted by ether. Phenylalanine hydrochloride （Phen） was used as the internal standard. The plasma concentrations of E and PE were measured by HPLC. The pharmacokinetic parameters were computed with 3P97 program. Results： A good linearity was obtained in E from 0.0152 to 1.52 μg/mL and in PE from 0.01485 to 1.485 μg/mL. The limits of identification were 0.005 μg/mL for E and 0.01 lag/mL for PE. The recoveries were in the range of 93.1% to 102.8%and 110.4% to 95.57% for E and PE respectively. The inter-day RSD and intraday RSD of E and PE were both less than 6%. The E and PE plasma solutions were steady within 60 days. The main pharmacokinetic parameters were as follows, tl/2 of E and PE were 1.39 h and2.65 h; ke of E and PE were 0.50/h and 0.26/h; AUCof E and PE were 0.55 and 0.44 （μg/Ml）xh respectively. Conclusions： To build a method for analyzing E and PE in the blood of human simultaneous, and to research pharmacokinetics of E and PE in Xiaoqinglong Granules in blood of rat, to lay a foundation for researching mechanism of chinese medicine compound by pharmacokinetics and for conducting rational administration of drug.

关 键 词：HPLC法 麻黄碱 伪麻黄碱 药代动力学 

分 类 号：R285[医药卫生—中药学]