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黄芩药材口服给药后大鼠血浆中黄芩苷、汉黄芩苷、野黄芩苷及其主要葡萄糖醛酸轭合代谢物的鉴定与定量。

Identification and quantification of baicalein, wogonin, oroxylin A and their major glucuronide conjugated metabolites in rat plasma after oral administration of Radix scutellariae product.

机构信息

School of Pharmacy, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, China.

出版信息

J Pharm Biomed Anal. 2011 Mar 25;54(4):750-8. doi: 10.1016/j.jpba.2010.10.005. Epub 2010 Oct 16.

Abstract

The current study aims to identify and quantify three flavones (baicalein, wogonin and oroxylin A) and their major metabolites (baicalin, wogonoside and oroxylin A-7-O-glucuronide) in rat plasma after oral administration of Radix scutellariae product. A simple HPLC/UV method has been developed to simultaneously determine the three flavones and their major metabolites in rat plasma. The chromatographic separation of the six analytes was achieved by a Thermo C(18) column with linear gradient elution of a mobile phase containing acetonitrile and 20mM sodium dihydrogen phosphate buffer (pH 4.6). All the tested analytes were detected by PDA detector at a wavelength of 320nm. The intra-day and inter-day precision for the current assay of the six analytes was within the range of -2.23% to 15.13% and -10.83% to 6.42%, respectively. All the studied analytes could be efficiently extracted from the rat plasma using HLB cartridge with extraction recoveries above 70% and were stable under different storage conditions. The developed assay method was successfully applied to the pharmacokinetic study of baicalin, wogonoside after oral administration of a commercially available Radix scutellariae containing capsule at a dose of 3.2g/kg to Sprague-Dawley rats. In addition to wogonoside, a new metabolite of wogonin has been identified using LC/MS/MS for the first time.

摘要

本研究旨在鉴定和定量测定黄芩药材口服后大鼠血浆中的三种黄酮类化合物(黄芩素、汉黄芩素和氧化黄芩素 A)及其主要代谢产物(黄芩苷、汉黄芩苷和氧化黄芩素 A-7-O-葡萄糖醛酸苷)。建立了一种简单的 HPLC/UV 方法,可同时测定大鼠血浆中的三种黄酮类化合物及其主要代谢产物。六种分析物的色谱分离采用 Thermo C(18)柱,通过含有乙腈和 20mM 磷酸二氢钠缓冲液(pH 4.6)的流动相进行线性梯度洗脱。所有测试分析物均在 PDA 检测器处于 320nm 波长下检测。当前测定的六种分析物的日内和日间精密度分别在-2.23%至 15.13%和-10.83%至 6.42%的范围内。所有研究的分析物均可用 HLB 小柱从大鼠血浆中高效提取,提取回收率均高于 70%,并且在不同的储存条件下稳定。该方法成功应用于 3.2g/kg 剂量的市售黄芩胶囊口服后黄芩苷、汉黄芩苷的药代动力学研究。此外,首次使用 LC/MS/MS 鉴定了汉黄芩素的一种新代谢物。

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