Determination and pharmacokinetic study of p-hydroxyphenethyl anisate following intravenous and oral administration in rats by RP-HPLC method  

静脉和灌胃给予大鼠茴香酸对羟基苯乙酯的RP-HPLC法测定和药代动力学研究

作　　者：Xiuwei Yang Youbo Zhang Wei Xu 杨秀伟;张友波;徐嵬(北京大学医学部药学院天然药物及仿生药物国家重点实验室,天然药物学系,北京100191)

机构地区：[1]State Key Laboratory of Natural and Biomimetic Drugs and Department of Natural Medicines,School of Pharmaceutical Sciences,Peking University Health Science Center,Beijing 100191,China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2020年第11期804-812,共9页中国药学（英文版）

基　　金：The National Natural Science Foundation of China(Grant No.30672609);National High Technology Research and Development Program of China(Grant No.2002AA2Z343C,2004AA2Z3783);National Sciences and Technology Program of China(Grant No.2006BAI06A01-02);Beijing Municipal Special-Purpose Science Foundation of China(Grant No.Z0004105040311)。

摘　　要：In the present study,we developed a rapid and specific reversed-phase high-performance liquid chromatographic(RP-HPLC)method for the quantification of p-hydroxyphenethyl anisate(HPA),one of the main bioactive constituents of the roots and rhizomes of Notopterygium incisum and N.franchetii,in rat plasma after an intravenous(20 mg/kg,i.v.)and an intragastrical(200 mg/kg,i.g.)administration to rats,respectively.The method involved a plasma clear-up step using liquid-liquid extraction by EtOAc,followed by RP-HPLC separation and detection.Separation of HPA was performed on an analytical DiamonsilTM ODS C18 column with the mobile phase of MeOH-H2 O at ratios of 75:25(v/v)for i.v.and 70:30(v/v)for i.g.administration.The flow-rate was 1.0 mL/min,and UV detection was performed at 256 nm.The calibration curves were linear over the ranges of 0.05-5.0μg/mL(r2=0.9984)for i.v.and 0.5-10.0μg/mL(r2=0.9995)for i.g.administration in rat plasma.The extraction recoveries were in the range of82.01%-87.97%.The intra-and inter-day precisions were between 1.71%and 3.99%,with accuracies ranging from 91.22%to110.5%.The absolute bioavailability of an orally administered HPA in rats was about 48.17%.The developed method was suitable for the determination and pharmacokinetic study of HPA in rat plasma.茴香酸对羟基苯乙酯(HPA)是中药羌活和宽叶羌活的主要生物活性成分之一。本文建立了一种快速、特异的反相高效液相色谱法(RP-HPLC)用于静脉(20 mg/kg)和灌胃(200 mg)/kg)给予大鼠HPA后其在大鼠血浆的测定和药代动力学研究。血浆样品经乙酸乙酯液液萃取净化后,进样RP-HPLC系统分离和测定。分析型色谱柱为DiamonsilTMODS C18;血浆样品分析的流动相为MeOH-H2O(v/v),静脉给药样品分析时为75:25,灌胃给药样品分析时为70:30;流速为1.0 mL/min,UV检测波长为256 nm。HPA标准曲线线性范围,静脉给药时为0.05-5.0μg/mL(r2=0.9984),灌胃给药时为0.5-10.0μg/mL(r2=0.9995);萃取回收率为82.01%-87.97%,日内和日间精密度为1.71%-3.99%,准确度范围为91.22%-110.5%;HPA在大鼠口服时的绝对生物利用度为48.17%。以上结果表明所建方法适合用于HPA在大鼠血浆中的测定和药代动力学研究。

关 键 词：p-Hydroxyphenethyl anisate PHARMACOKINETIC BIOAVAILABILITY RP-HPLC NOTOPTERYGIUM 

分 类 号：R969.1[医药卫生—药理学]