羟乙基芦丁（HR）的代谢：人体内[14C]-HR的代谢

Metabolism of hydroxyethylrutosides (HR): metabolism of [14C]-HR in man.

Hackett A M, Griffiths L A, Luyckx A S, van Cauwenberge H

Arzneimittelforschung. 1976;26(5):925-8.

Abstract

following oral administration of a [14C]-hydroxyethylrutoside (Paroven, Venoruton) preparation (HR) to three subjects, 3.05--5.97% of the administered [14C] was excreted in urine. Unchanged urinary [14C]-hydroxyethylrutosides represented 1.57--1.96% of the total dose. 2. Significant levels of [14C] were detected in plasma within 1 h of oral administration of HR. Peak levels were observed from 2--9 h. 3. The presence in urine of [14C]-3',4',5,7-tetra-O-(beta-hydroxyethyl)rutoside, [14C]-3',4',7-tri-O-(beta-hydroxyethyl)rutoside and [14C]-4',7-di-O-(beta-hydroxyethyl)rutoside was shown by radioscanning and/or spectal methods. 4. Administration of a second oral dose of [14C]-HR to each of the three subjects following extended dosage of nonlabelled HR did not result in any increase in urinary [14C] excretion over that observed after administration of a single oral dose. 5. Observations on urinary excretion in man are compatible with the finding in experimental animals that the major route of hydroxyethylrutoside excretion is via the biliary-enteric route.

摘要

给三名受试者口服[14C]-羟乙基芦丁（帕罗文，维脑路通）制剂（HR）后，给药的[14C]中有3.05 - 5.97%经尿液排出。尿液中未变化的[14C]-羟乙基芦丁占总剂量的1.57 - 1.96%。2. 口服HR后1小时内血浆中检测到显著水平的[14C]。在2 - 9小时观察到峰值水平。3. 通过放射性扫描和/或光谱方法显示尿液中存在[14C]-3',4',5,7-四-O-（β-羟乙基）芦丁、[14C]-3',4',7-三-O-（β-羟乙基）芦丁和[14C]-4',7-二-O-（β-羟乙基）芦丁。4. 在给三名受试者长期服用非标记HR后再口服第二剂[14C]-HR，尿液中[14C]的排泄量并未比单次口服剂量后观察到的增加。5. 人体尿液排泄观察结果与实验动物中的发现一致，即羟乙基芦丁的主要排泄途径是通过胆汁-肠途径。