Van Boven M, Daenens P
J Pharm Sci. 1982 Oct;71(10):1152-7. doi: 10.1002/jps.2600711019.
The metabolic disposition of 14C-labeled nitromethaqualone was investigated in rats. Unlabeled nitromethaqualone was used for studies on humans. nitromethaqualone was eliminated from the body after most of it had undergone biotransformation. Both humans and rats reduced the nitro group of nitromethaqualone to the corresponding amino derivative, which was partially transformed to the corresponding acetylated form. Cleavage of the quinazolinone nucleus resulting in 2-methoxyl-4-nitroaniline was also observed in humans. In rats additional major metabolites arose from the oxidation of the 2-methyl group into hydroxymethyl resulting in 2-hydroxymethyl-3-(2'-methoxy-4-nitrophenyl)-4(3H)-quinazolinone and concomitant in vivo reduction of the latter resulting in 2-hydroxymethyl-3-(2'-methoxy-4'-aminophenyl)-4(3H)-quinazolinone. Both metabolites were also excreted as glucuronides. In rats fecal excretion accounted for 55-60% of the administered dose, while 24-27% was excreted in the urine. Protracted excretion in both humans and rats indicated an extensive enterohepatic circulation.
在大鼠中研究了14C标记的硝甲喹酮的代谢情况。未标记的硝甲喹酮用于人体研究。硝甲喹酮在大部分发生生物转化后从体内消除。人和大鼠都将硝甲喹酮的硝基还原为相应的氨基衍生物，该氨基衍生物部分转化为相应的乙酰化形式。在人体中也观察到喹唑啉酮核的裂解产生2-甲氧基-4-硝基苯胺。在大鼠中，额外的主要代谢产物来自2-甲基氧化为羟甲基，生成2-羟甲基-3-(2'-甲氧基-4-硝基苯基)-4(3H)-喹唑啉酮，且后者在体内伴随还原生成2-羟甲基-3-(2'-甲氧基-4'-氨基苯基)-4(3H)-喹唑啉酮。这两种代谢产物也以葡萄糖醛酸苷的形式排泄。在大鼠中，粪便排泄占给药剂量的55 - 60%，而24 - 27%通过尿液排泄。人和大鼠的排泄过程都很漫长，表明存在广泛的肠肝循环。
