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中国药学(英文版)

• 【研究论文】 • 上一篇    下一篇

基于UPLC-MS方法的金丝桃苷静脉给药后大鼠体内药代动力学研究

檀爱民, 林萍*, 张斐   

  1. 江苏先声药业有限公司, 江苏 南京 210042
  • 收稿日期:2013-05-10 修回日期:2013-06-13 出版日期:2013-11-15 发布日期:2014-01-22
  • 通讯作者: 林萍*

Determination of hyperoside in rat plasma after intravenous administration by UPLC-MS

Aimin Tan, Ping Lin*, Fei Zhang   

  1. Jiangsu Simcere Pharmaceutical Co., Ltd, Nanjing 210042, China
  • Received:2013-05-10 Revised:2013-06-13 Online:2013-11-15 Published:2014-01-22
  • Contact: Ping Lin*

摘要:

建立用于测定金丝桃苷血药浓度的超高效液相-质谱联用分析方法(UPLC-MS), 应用超高效液相-质谱法, 采用 电喷雾离子源(ESI), 负离子模式检测, 对大鼠血浆中的金丝桃苷进行定量测定, 并研究金丝桃苷静脉给药后在大鼠体内的药代动力学过程。在10分钟内完成大鼠血浆样品内金丝桃苷的分析。金丝桃苷线性关系良好(r2>0.999), 日间差和日内差小于15%, 定量限为4 ng/mL, 符合生物样品分析要求。本方法的定量限低于文献报道, 且所需的血浆体积只有50 µL, 优于文献方法。本方法可成功应用于大鼠静脉给药后金丝桃苷的血药浓度测定, 为金丝桃苷临床应用及临床药物监测提供帮助。

关键词: 金丝桃苷, 选择性离子监测, 负离子, 药代动力学特征

Abstract:

Hyperoside is one of the major components of Hypericum perforatum L. and also present in many plant species such as Abelmoschus manihot (L.) Medik., Ribes nigrum L. and Rosa agrestis Savi (Rosaceae). Because hyperoside exhibits many biological activities, the pharmacokinetics profile of hyperoside needs to be studied for further elucidating its mechanism of action. A simple method for the determination of hyperoside in rat plasma was developed by using ultra-high performance liquid chromatography coupled with mass spectrometry (UPLC-MS). Only 50 µL plasma samples were required for sample preparation. The quantitative detection of hyperoside was accomplished by selected ion monitoring (SIM) in negative ion mode. Hyperoside was analyzed in less than 10 min. Good linearity was obtained (r2>0.999) and the intra- and inter-day precision of the method were lower than 15%. Lower limit of quantification (LLOQ) was 4 ng/mL for hyperoside in rat plasma. Our method showed advantage in the lower LLOQ compared with the reported method; furthermore, smaller amount of plasma was needed. The method was successfully applied for the pharmacokinetics study of hyperoside in rat after intravenous administration of hyperoside.

Key words: Hyperoside, Selected ion monitoring mode, Negative ion mode, Pharmacokinetics profile

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*Corresponding author. Tel.: 86-25-85560000; #These authors contributed equally to this work.