人体中[14C]-异喹胍的代谢
The metabolism of [14C]-debrisoquine in man.
作者信息
Idle J R, Mahgoub A, Angelo M M, Dring L G, Lancaster R, Smith R L
出版信息
Br J Clin Pharmacol. 1979 Mar;7(3):257-66. doi: 10.1111/j.1365-2125.1979.tb00930.x.
Abstract
1 The synthesis of [14C]-debrisoquine hydrochloride and 4-hydroxy-debrisoquine sulphate is described. 2 The metabolic fate and excretion profile in both urine and faeces of 14C-labelled debrisoquine was studied in five healthy human subjects. 3 Investigations showed that the drug is well-absorbed after a single oral dose of 32 mg and quantitatively eliminated from the body within three days. 4 4-Hydroxy-debrisoquine is the major metabolite of debrisoquine, although significant amounts of 5-,6-, 7- and 8-hydroxy-debrisoquine are also formed. 5 Electron-capture gas chromatography is a useful method for measuring debrisoquine and its five hydroxylated metabolites in urine at the pg level.
摘要
描述了盐酸[14C]-地布喹和硫酸4-羟基-地布喹的合成。
在5名健康人体受试者中研究了14C标记的地布喹在尿液和粪便中的代谢命运及排泄情况。
研究表明，单次口服32毫克后该药物吸收良好，并在三天内从体内定量消除。
4-羟基-地布喹是地布喹的主要代谢产物，不过也会形成大量的5-、6-、7-和8-羟基-地布喹。
电子捕获气相色谱法是一种在皮克水平测量尿液中地布喹及其五种羟基化代谢产物的有用方法。
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