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波叶大黄中大黄酸的药代动力学分析

Pharmacokinetic analysis of rhein in Rheum undulatum L.

作者信息

Lee Je-Hyun, Kim Jong Moon, Kim Chungsook

机构信息

Drug Research and Development Team, Korea Institute of Oriental Medicine, 129-11 Chungdam-dong, Sejin Building, Kangnam-ku, Seoul 135-100, South Korea.

出版信息

J Ethnopharmacol. 2003 Jan;84(1):5-9. doi: 10.1016/s0378-8741(02)00222-2.

DOI:10.1016/s0378-8741(02)00222-2
PMID:12499069
Abstract

This research aims to identify the main active compounds of Rhei undulati Rhizoma (roots of Rheum undulatum LINNE) and determine the types of anthraquinones absorbed into the body and their pharmacokinetic parameters. The boiling-water extract of the herb was administered to 12 healthy volunteers (9 men/3 women) at a dosage of 100 mg/kg the anthraquinone levels in plasma were determined with TLC, HPLC, and LC-MS. Rhein was the only anthraquinone compound absorbed by the body as determined for plasma analysis of the volunteers. The elimination rate constant of rhein in Rhei undulati Rhizoma was 0.23+/-0.02/h and the half life was 3.38+/-0.35 h. This experiment confirmed that rhein is the most important active compound absorbed by the body among anthraquinones contained in Rhei undulati Rhizoma, indicating that rhein is a promising marker substance to evaluate Rhei Rhizoma and Rhei undulati Rhizoma.

摘要

本研究旨在鉴定波叶大黄根茎(掌叶大黄的根)的主要活性成分,确定吸收进入体内的蒽醌类型及其药代动力学参数。以100mg/kg的剂量将该草药的沸水提取物给予12名健康志愿者(9名男性/3名女性),采用薄层色谱法(TLC)、高效液相色谱法(HPLC)和液相色谱-质谱联用(LC-MS)测定血浆中的蒽醌水平。对志愿者血浆分析确定,大黄酸是唯一被人体吸收的蒽醌化合物。波叶大黄中大黄酸的消除速率常数为0.23±0.02/h,半衰期为3.38±0.35h。本实验证实,大黄酸是波叶大黄所含蒽醌中被人体吸收的最重要活性成分,表明大黄酸是评价大黄和波叶大黄的一种有前景的标志物。

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