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首页> 外文期刊>Asian journal of drug metabolism and pharmacokinetics >Urinary excretion of the enantiomers of trans tramadol and its active metabolite, trans O-demethyltramadol, in human subjects
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Urinary excretion of the enantiomers of trans tramadol and its active metabolite, trans O-demethyltramadol, in human subjects

机译：反式曲马多及其活性代谢物反式O-去甲基曲马多对映体的尿排泄

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摘要

To investigate the urinary excretion of the enantiomers of trans tramadol (trans T) and its active metabolite,trans O-demethyltramadol (Ml), in human subjects. Methods Twenty healthy volunteers (10 men, 10 women) were included in the study. After an overnight fast, a single 100-mg oral dose of trans T hydrochloride was ingested. Urine samples were collected for 24 h after dosing. The enantiomers of trans T and Ml were determined with a high performance capillary electrophoresis method. The enantiomers of Ml glucuronide conjugate (M1_c) was determined as the enantiomers of free Ml (M1_f) after enzymatic cleavage with beta-glucronidase. Results In urine, (+)-trans T was more than (-)-trans T. There were no significant differences in the urine amount of (+)-trans T, (-)-trans T, or trans T between the male and female subjects. In urine, (+)-Ml_f was more than (-)Ml_f, (+)-Ml_c was less than (-)-Ml_c, but (+)-Ml [(+)-Ml_f plus (+)-Ml_c] was almost equal to (-)-Ml [(-)-Mlf plus (-)-Ml_c]. There were no significant differences in the urine amounts of Ml_f, Ml_c, Ml or their enantiomers between the male and female subjects. The glucuronide rate of (+)-Ml was lower than that of (-)-Ml. There were no significant differences in the glucuronide rates of Ml or its enantiomers between the male and female subjects. Conclusion The urinary excretion of the enantiomers of trans T is different in human, (+)-trans T being excreted more. The urinary excretion of the enantiomers of Ml is stereoselective in human, (+)-Ml and (-)-Ml being excreted mainly as (+)-Ml_f and (-)-Ml_c, respectively. There are no gender-related differences in the urinary excretion of the enantiomers of trans T or M1.
机译：为了研究反式曲马多（反式T）及其活性代谢物反式O-去甲基曲马多（M1）的对映体在人体中的排泄情况。方法纳入20名健康志愿者（10名男性，10名女性）。禁食过夜后，摄入100毫克口服剂量的反式T盐酸盐。给药后24小时收集尿液样品。反式T和M1的对映体用高效毛细管电泳法测定。将M1葡糖醛酸苷缀合物（M1_c）的对映体确定为用β-葡糖醛酸苷酶酶切后的游离M1（M1_f）的对映体。结果在尿液中，（+）-反式T比（-）-反式T多。男性之间（+）-反式T，（-）-反式T或反式T的尿量无显着差异。和女性。尿液中（+）-Ml_f大于（-）Ml_f，（+）-Ml_c小于（-）-Ml_c，但（+）-M1 [（+）-Ml_f加（+）-Ml_c]几乎等于（-）-Ml [（-）-Mlf加（-）-Ml_c]。在男性和女性受试者之间，M1_f，M1_c，M1或其对映异构体的尿量没有显着差异。 （+）-M1的葡糖醛酸苷比率低于（-）-M1的葡糖醛酸化物比率。在男性和女性受试者之间，M1或其对映异构体的葡糖醛酸苷比率没有显着差异。结论反式T的对映异构体的尿排泄在人体内是不同的，（+）-反式T的排泄更多。 M1的对映异构体的尿排泄在人中是立体选择性的，（+）-M1和（-）-M1分别主要以（+）-M1_f和（-）-M1_c排泄。反式T或M1对映异构体的尿排泄没有性别相关的差异。

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