Mayo B C, Brodie R R, Chasseaud L F, Hawkins D R
Drug Metab Dispos. 1978 Sep-Oct;6(5):518-27.
A major metabolite of ciclobendazole (methyl 5-cyclopropylcarbonyl-2-benzimidazolecarbamate) excreted in the urine, bile, and feces of rats was methyl 5-cyclopropylcarbonyl-6-hydroxy-benzimidazolecarbamate, established by comparison of the proton magnetic resonance and mass spectra with that of the authentic compound. This compound represented 8.2% and 7.1% of the dose, respectively, in extracts of 24-hr urine and 48-hr feces samples of rats, but was only a minor metabolite in dog urine (1% of the dose). The unchanged drug was only detected in dog feces, the major route of excretion of radioactivity in the dog. 5-Cyclopropylcarbonyl-2-amino-benzimidazole was present in rat urine (2.5% of the dose). A major metabolite in dog bile was probably 5-cyclopropylcarbinol-2-aminobenzimidazole, formed by loss of the methoxycarbonyl group and reduction of the carbonyl function in the 5-position.
环苯达唑（5 - 环丙基羰基 - 2 - 苯并咪唑氨基甲酸甲酯）在大鼠尿液、胆汁和粪便中排泄的一种主要代谢物是5 - 环丙基羰基 - 6 - 羟基 - 苯并咪唑氨基甲酸甲酯，通过将其质子磁共振谱和质谱与 authentic 化合物的谱图进行比较得以确定。在大鼠24小时尿液和48小时粪便样品的提取物中，该化合物分别占给药剂量的8.2%和7.1%，但在犬尿液中只是一种次要代谢物（占给药剂量的1%）。未变化的药物仅在犬粪便中检测到，犬体内放射性物质的主要排泄途径是粪便。5 - 环丙基羰基 - 2 - 氨基苯并咪唑存在于大鼠尿液中（占给药剂量的2.5%）。犬胆汁中的一种主要代谢物可能是5 - 环丙基甲醇 - 2 - 氨基苯并咪唑，它是由甲氧基羰基的丢失以及5位羰基功能的还原形成的。
