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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
【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。
【Abstract】 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.
【Key words】 s-mephenytoin; phenytoin; hydroxylation metabolism; phenotype;
- 【文献出处】 中国临床药理学杂志 ,THE CHINESE JOURNAL OF CLINICAL PHARMACOLOGY , 编辑部邮箱 ,1994年01期
- 【分类号】R969
- 【被引频次】2
- 【下载频次】82