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开发一种用于测定大鼠血浆中牛蒡子苷元的液相色谱-串联质谱法:其在药代动力学研究中的应用。

Development of an LC/MS/MS method in order to determine arctigenin in rat plasma: its application to a pharmacokinetic study.

作者信息

Zou Quanfei, Gu Yuan, Lu Rong, Zhang Tiejun, Zhao Guang-Rong, Liu Changxiao, Si Duanyun

机构信息

Key Laboratory of Systems Bioengineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.

出版信息

Biomed Chromatogr. 2013 Sep;27(9):1123-8. doi: 10.1002/bmc.2916. Epub 2013 May 3.

Abstract

In this study, a simple and sensitive LC/MS/MS method was developed and validated for the determination of arctigenin in rat plasma. The MS detection was performed using multiple reaction monitoring at the transitions of m/z 373.2 → 137.3 for arctigenin and m/z 187.1 → 131.0 for psoralen (internal standard) with a Turbo IonSpray electrospray in positive mode. The calibration curves fitted a good linear relationship over the concentration range of 0.2-500 ng/mL. It was found that arctigenin is not stable enough at both room temperature and -80 °C unless mixed with methanol before storage. The validated LC/MS/MS method was successfully applied for the pharmacokinetic study of arctigenin in rats. After intravenous injection of 0.3 mg/kg arctigenin injection to rats, the maximum concentration, half-life and area under the concentration-time curve were 323 ± 65.2 ng/mL, 0.830 ± 0.166 and 81.0 ± 22.1 h ng/mL, respectively.

摘要

在本研究中,开发并验证了一种简单且灵敏的液相色谱-串联质谱(LC/MS/MS)方法,用于测定大鼠血浆中的牛蒡子苷元。质谱检测采用多反应监测模式,牛蒡子苷元的质荷比跃迁为m/z 373.2 → 137.3,补骨脂素(内标)的质荷比跃迁为m/z 187.1 → 131.0,采用Turbo IonSpray电喷雾正离子模式。校准曲线在0.2 - 500 ng/mL的浓度范围内呈现良好的线性关系。研究发现,牛蒡子苷元在室温及-80 °C条件下均不够稳定,除非在储存前与甲醇混合。所验证的LC/MS/MS方法成功应用于牛蒡子苷元在大鼠体内的药代动力学研究。给大鼠静脉注射0.3 mg/kg牛蒡子苷元注射液后,其最大浓度、半衰期和浓度-时间曲线下面积分别为323 ± 65.2 ng/mL、0.830 ± 0.166和81.0 ± 22.1 h·ng/mL。

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