Yamaguchi H, Kubo J, Sekine K, Naruchi T, Hashimoto Y, Kato R
Drug Metab Dispos. 1979 Sep-Oct;7(5):340-4.
Two male volunteers received 400 mg of nonlabeled feprazone, 1,2-diphenyl-3,5-dioxo-4-(3'-methyl-but-2'-enyl)pyrazolidine. Metabolites were extracted and isolated by chromatography on silica gel. Isolated metabolites were unchanged drug, E-1,2-diphenyl-3,5-dioxo-4-(3'-hydroxymethyl-but-2'-enyl)pyrazolidine, and feprazone (C4)-beta-glucuronide. Feprazone (C4)-beta-glucuronide was the main metabolite and it belongs to a novel type of conjugate, (C)-beta-glucuronide.
两名男性志愿者服用了400毫克未标记的非普拉宗,即1,2-二苯基-3,5-二氧代-4-(3'-甲基-丁-2'-烯基)吡唑烷。通过硅胶柱色谱法提取并分离代谢产物。分离出的代谢产物有未变化的药物、E-1,2-二苯基-3,5-二氧代-4-(3'-羟甲基-丁-2'-烯基)吡唑烷以及非普拉宗(C4)-β-葡萄糖醛酸苷。非普拉宗(C4)-β-葡萄糖醛酸苷是主要代谢产物,它属于一种新型的结合物,即(C)-β-葡萄糖醛酸苷。