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生脉散配方口服后大鼠血浆中五味子甲素、五味子醇 B、五味子酯甲、五味子乙素和五味子醇乙的药代动力学研究

Pharmacokinetic study of schisandrin, schisandrol B, schisantherin A, deoxyschisandrin, and schisandrin B in rat plasma after oral administration of Shengmaisan formula by UPLC-MS.

机构信息

National TCM Key Laboratory of Serum Pharmacochemistry, Heilongjiang University of Chinese Medicine, and Key Pharmacometabolomics Platform of Chinese Medicines, Harbin, P R China.

出版信息

J Sep Sci. 2013 Feb;36(3):485-91. doi: 10.1002/jssc.201200887. Epub 2013 Jan 10.

DOI:10.1002/jssc.201200887
PMID:23303577
Abstract

Shengmaisan (SMS) is a traditional Chinese medicine prescription widely used for the treatment of cardiovascular diseases in Asia. Its lignans are major components responsible for therapeutic action. A rapid and specific UPLC-Q-TOF/MS has been developed and validated for simultaneous quantification of the five main bioactive components, i.e. schisandrin, schisandrol B, schisantherin A, deoxyschisandrin, and schisandrin B, in rat plasma after oral administration of SMS. All calibration curves showed excellent linearity within the test ranges. Validation proved the repeatability of the method was good and recovery was satisfactory. The separation of these compounds was carried out on a Waters ACQUITY HSS T(3) column (2.1 × 100 mm, 1.8 μm) by linear gradient elution using a mobile phase consisting of 0.01% formic acid in water and ACN containing 0.01% formic acid. In this work, plasma pharmacokinetic characteristics of lignans components after oral administration SMS were investigated using UPLC-Q-TOF/MS method. MS was performed on a Waters Micromass high-definition technology with an ESI source. Data were analyzed and estimated by compartmental methods and pharmacokinetic parameters calculated using WinNonlin Professional version 6.1. Results demonstrated that the proposed UPLC-Q-TOF/MS method was successfully applied to pharmacokinetic study of all components in rat plasma after oral administration of the SMS.

摘要

升麻散(SMS)是一种传统的中药方剂,在亚洲被广泛用于治疗心血管疾病。其木脂素是主要的治疗作用成分。本研究建立了一种快速、特异的 UPLC-Q-TOF/MS 法,用于同时定量测定大鼠灌胃 SMS 后血浆中的 5 种主要生物活性成分,即五味子甲素、五味子醇 B、五味子酯甲、去氧五味子素和五味子乙素。所有校准曲线在测试范围内均表现出良好的线性。验证结果表明,该方法的重复性良好,回收率令人满意。这些化合物的分离是在 Waters ACQUITY HSS T(3)柱(2.1×100mm,1.8μm)上进行的,采用含有 0.01%甲酸的水和 ACN 作为流动相进行线性梯度洗脱。本工作采用 UPLC-Q-TOF/MS 法研究了大鼠灌胃 SMS 后木脂素成分的血浆药代动力学特征。MS 在 Waters Micromass 高清晰度技术上采用 ESI 源进行。数据通过房室模型进行分析和估计,使用 WinNonlin Professional 版本 6.1 计算药代动力学参数。结果表明,该 UPLC-Q-TOF/MS 法可成功应用于 SMS 灌胃后大鼠血浆中所有成分的药代动力学研究。

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