Feng P C, Fenselau C C, Jacobson R R
Drug Metab Dispos. 1981 Nov-Dec;9(6):521-4.
We have identified two metabolites of clofazimine (B663; Lamprene; 3-(p-chloroanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine) in our initial investigation of its metabolism in leprosy patients. Based on mass, ultraviolet, and visible spectrometry, we characterized an unconjugated (metabolite I, 3-(p-hydroxyanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine ) and a conjugated (metabolite II, 3-(beta-D-glucopyranosiduronic acid)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine) metabolite from the urine of patients. Both metabolites were red in color, similar to clofazimine; however, both were considerably more polar than the parent drug. We suggest that metabolite I was formed by a hydrolytic dehalogenation reaction, and metabolite II by hydrolytic deamination followed by glucuronidation.
在对氯法齐明（B663；氯苯吩嗪；3-（对氯苯胺基）-10-（对氯苯基）-2,10-二氢-2-异丙基亚氨基吩嗪）在麻风病患者体内代谢的初步研究中，我们鉴定出了两种代谢产物。基于质谱、紫外光谱和可见光谱，我们对患者尿液中的一种未结合代谢产物（代谢产物I，3-（对羟基苯胺基）-10-（对氯苯基）-2,10-二氢-2-异丙基亚氨基吩嗪）和一种结合代谢产物（代谢产物II，3-（β-D-葡萄糖醛酸苷）-10-（对氯苯基）-2,10-二氢-2-异丙基亚氨基吩嗪）进行了表征。两种代谢产物均呈红色，与氯法齐明相似；然而，两者的极性均比母体药物大得多。我们认为代谢产物I是由水解脱卤反应形成的，而代谢产物II是由水解脱氨后再进行葡萄糖醛酸化形成的。
