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

doi:10.5246/jcps.2020.11.073

中国药学(英文版) ›› 2020, Vol. 29 ›› Issue (11): 804-812.DOI: 10.5246/jcps.2020.11.073

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

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

收稿日期:2020-08-23 修回日期:2020-09-18 出版日期:2020-11-30 发布日期:2020-10-07
通讯作者: Tel.: +86-10-82801569, E-mail: xwyang@bjmu.edu.cn
作者简介:Dr. Xiuwei Yang got his doctorate in Toyama Medical and Pharmaceutical University of Japan in 1992. He worked as a postdoctoral research fellow at School of Pharmaceutical Sciences from Beijing Medical University in 1992–1994. In 1994.9, he joined Peking University School of Pharmaceutical Sciences and worked as a professor. His major research interests are the absorption, distribution, metabolism, excretion, toxicity and activity of drugs (ADMET/Act.), complex system exploration of traditional Chinese Medicine, biological transformation of natural drug and/or Chinese medicinal chemical compositions, innovative drug discovery and natural medicinal chemistry.
基金资助:
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), and Beijing Municipal Special-Purpose Science Foundation of China (Grant No. Z0004105040311).

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

Xiuwei Yang^*, Youbo Zhang, Wei Xu

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

Received:2020-08-23 Revised:2020-09-18 Online:2020-11-30 Published:2020-10-07
Contact: Tel.: +86-10-82801569, E-mail: xwyang@bjmu.edu.cn
About author:Dr. Xiuwei Yang got his doctorate in Toyama Medical and Pharmaceutical University of Japan in 1992. He worked as a postdoctoral research fellow at School of Pharmaceutical Sciences from Beijing Medical University in 1992–1994. In 1994.9, he joined Peking University School of Pharmaceutical Sciences and worked as a professor. His major research interests are the absorption, distribution, metabolism, excretion, toxicity and activity of drugs (ADMET/Act.), complex system exploration of traditional Chinese Medicine, biological transformation of natural drug and/or Chinese medicinal chemical compositions, innovative drug discovery and natural medicinal chemistry.
Supported by:
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), and Beijing Municipal Special-Purpose Science Foundation of China (Grant No. Z0004105040311).

摘要/Abstract

摘要：

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Diamonsil^TMODS 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0.05–5.0 μg/mL (r²= 0.9984), 灌胃给药时为0.5–10.0 μg/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: 茴香酸对羟基苯乙酯, 药代动力学, 生物利用度, RP-HPLC, 羌活

Abstract:

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 ofNotopterygium incisumand 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 HPAwas performed on an analytical Diamonsil^TMODS C₁₈ column with the mobile phase of MeOH–H₂O 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 0.05–5.0 μg/mL (r²= 0.9984) for i.v. and 0.5–10.0 μg/mL (r²= 0.9995) for i.g. administrationin rat plasma. The extraction recoveries were in the range of 82.01%–87.97%. The intra- and inter-day precisions were between 1.71% and 3.99%, with accuracies ranging from 91.22% to 110.5%. The absolute bioavailability of an orally administered HPA in rats was about 48.17%. The developed method was suitable for the determination and pharmacokinetic studyof HPA in rat plasma.

Key words: p-Hydroxyphenethyl anisate, Pharmacokinetic, Bioavailability, RP-HPLC, Notopterygium

中图分类号:

R969.1

Supporting:

杨秀伟, 张友波, 徐嵬. 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[J]. 中国药学(英文版), 2020, 29(11): 804-812.

Xiuwei Yang, Youbo Zhang, Wei Xu. Determination and pharmacokinetic study of p-hydroxyphenethyl anisate following intravenous and oral administration in rats by RP-HPLC method[J]. Journal of Chinese Pharmaceutical Sciences, 2020, 29(11): 804-812.

参考文献

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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

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

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