Gilbert J N, Hetherington W L, Powell J W, Whalley W B
J Pharm Pharmacol. 1975 May;27(5):343-7. doi: 10.1111/j.2042-7158.1975.tb09452.x.
The human metabolism of (+/-)-5-allyl-5-(1'-methylbutyl) barbituric acid (I), quinalbarbitone, taken orally, has been studied. Comparison of g.c. and g.c.-m.s. data from derivatized extracts of urine with similar data from synthetic samples confirmed the presence of the two diastereoisomeric forms of 5-allyl-5-(3'hydroxy-1'-methylbutyl)barbituric acid (II), 5-allyl-5-(3'-oxo-1'-methylbutyl)barbituric acid (III), 5-allyl-5-(1'-methyl-3'-carboxypropyl)barbituric acid (IV), and 5-(2',3'-dihydroxypropyl)-5-(1'-methylbutyl)barbituric acid (V) in the urine. There was no evidence for the urinary excretion of unchanged drug. The rate of excretion of these metabolites has been examined in some detail, and rate-limited kinetics shown to apply for excretion of the acid (IV) and the diol (V).
已对口服的（±）-5-烯丙基-5-（1'-甲基丁基）巴比妥酸（I）即速可巴比妥的人体代谢情况进行了研究。将尿液衍生化提取物的气相色谱（g.c.）和气相色谱-质谱联用（g.c.-m.s.）数据与合成样品的类似数据进行比较，证实尿液中存在5-烯丙基-5-（3'-羟基-1'-甲基丁基）巴比妥酸（II）、5-烯丙基-5-（3'-氧代-1'-甲基丁基）巴比妥酸（III）、5-烯丙基-5-（1'-甲基-3'-羧丙基）巴比妥酸（IV）和5-（2',3'-二羟基丙基）-5-（1'-甲基丁基）巴比妥酸（V）的两种非对映异构体形式。没有证据表明有未变化的药物经尿液排泄。已较为详细地研究了这些代谢物的排泄速率，结果表明酸（IV）和二醇（V）的排泄符合限速动力学。
