中国健康志愿者S－美芬妥英和苯妥英4’－羟化代谢的相关性研究  

RELATIONSHIP BETWEEN S-MEPHENYTOIN AND PHENYTOIN 4'-HYDROXYLATION METABOLISM IN CHINESE HEALTHY VOLUNTEERS

作　　者：阮邹荣[1] 赵奕[1] 周君富[1] 潘以正[1] 程源深[1] 丁德云[1] 

机构地区：[1]浙江医科大学临床药理研究所

出　　处：《中国临床药理学杂志》1994年第1期22-26,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：１６名汉族健康志愿者进行Ｓ－美芬妥英４’－羟化代谢分型，１３名为强代谢者（ＥＭｓ），３名为弱代谢者（ＰＭｓ）。口服苯妥英１００ｍｇ，应用ＨＰＬＣ法测定服药后２４ｈ尿中苯妥英和４’－羟苯妥英（４’－ＯＨ－ＰＨＴ）的排泄量。１３名Ｓ－美芬妥英强代谢者Ｌｇ苯妥英／４’－羟苯妥英比值为－２．１７±０．２６；３名弱代谢者为－２．２７±０．１０，两组无显著性差异Ｐ＞０．０５）。１６名受试者Ｓ－美芬妥英和苯妥英的羟化代谢比值无相关性（ｒ＝－０．１０８，Ｐ＞０．００５）。本文结果表明，Ｓ－美芬妥英和苯妥英虽同为乙内酰脲类抗癫痫药，化学结构和羟化反应均相似，但在人体内不属同一羟化途径代谢，无交叉代谢障碍。Single oral 100mg dose of phenytoin( PHT)was given to 16 healthy subjeets on different occations, urine was collected up to 24 hours. The excreted PHT and 4’-hydroxylation metabolite (4’-OH-PHT) were measured by HPLC method. The subjects were phenotyped 3 poor metabolizers (PMs) and 13 extensive metabolizers(EMs) of s-mephenytoin(S-MP) hydroxylation by metabolic ratio (MR) and hydroxylation index(HI). The log10 PHT /4’-OH-PHT of PMs and EMs were-2.27± 0.10 and-2. 17 ± 0. 26. respectively. There was no significant difference in PMs and EMs of log10 PHT /4’-OH-PHT (p>0. 05).No correlations were found between the log10 PHT/4’-OH-PHT of PHT and the log10 MR and log10 HI of S-MP.These findings suggested that they are antiepileptic drugs of hydantoinis and 4’-hydroxylation metabolism, but dissociation of S-MP polymorphism and PHT hydroxlation.

关 键 词：美芬妥英 苯妥英 羟化代谢 

分 类 号：R971.6[医药卫生—药品]