Benziger D, Dorrbecker S, Goehl T, Edelson J
Drug Metab Dispos. 1978 Jan-Feb;6(1):8-15.
Oxarbazole (9-benzoyl-1,2,3,4-tetrahydro-6-methoxycarbazole-3-carboxylic acid) was absorbed by human volunteers, rats, dogs, guinea pigs, and monkeys. In all species of laboratory animals studied, the major urinary metabolite was the product of O-demethylation, 9-benzoyl-1,2,3,4-tetrahydro-6-hydroxycarbazole-3-carboxylic acid; this metabolite was conjugated in all species except the guinea pig. The dog and monkey excreted small quantities of a conjugate of 1,2,3,4-tetrahydro-6-methoxycarbazole-3-carboxylic acid in the urine. Enterohepatic circulation was demonstrated in bile duct-cannulated rats, in which almost 90% of the radioactivity of a dose of 14C-oxarbazole had been excreted into the bile within 24 hr. At the time of peak blood radioactivity, intact oxarbazole was the major constituent circulating in the bloodstream of rats and monkeys that had received 14C-oxarbazole orally. The clearance of either intact oxarbazole in man and guinea pig, or undifferentiated radioactivity in rat, dog, and monkey, did not follow the kinetics of a simple model.
奥沙巴唑（9-苯甲酰基-1,2,3,4-四氢-6-甲氧基咔唑-3-羧酸）可被人类志愿者、大鼠、狗、豚鼠和猴子吸收。在所有研究的实验动物物种中，主要的尿液代谢产物是O-去甲基化产物，即9-苯甲酰基-1,2,3,4-四氢-6-羟基咔唑-3-羧酸；除豚鼠外，该代谢产物在所有物种中均会发生结合反应。狗和猴子在尿液中排泄出少量的1,2,3,4-四氢-6-甲氧基咔唑-3-羧酸结合物。在胆管插管的大鼠中证实了肠肝循环，在这些大鼠中，一剂14C-奥沙巴唑的放射性在24小时内几乎90%已排泄到胆汁中。在血液放射性达到峰值时，完整的奥沙巴唑是口服14C-奥沙巴唑的大鼠和猴子血液中循环的主要成分。人及豚鼠体内完整奥沙巴唑的清除率，或大鼠、狗和猴子体内未分化放射性的清除率，均不符合简单模型的动力学。
