Crew M C, Di Carlo F
Drug Metab Dispos. 1976 Mar-Apr;4(2):147-53.
The fate of oxisuran in the pig was studied with 14C-labeled drug to quantify its biotransformation and disposition. Despite interanimal differences, it was clear that the compound absorbed rapidly and biotransformed extensively to metabolites which were excreted principally in urine rather than in feces. Direct attacks upon oxisuran involved reduction to diastereo-isomeric oxisuran alcohol sulfoxides and oxidation to oxisuran sulfone. Subsequently, the oxisuran alcohol sulfoxides were reduced to a sulfide and oxidized to a sulfone. Phase II reactions appeared to be limited to sulfation of oxisuran alcohol sulfoxides and oxisuran alcohol sulfone. Pharmacokinetics were investigated for oxisuran and its metabolites.
用14C标记的药物研究了奥昔舒仑在猪体内的命运，以量化其生物转化和处置情况。尽管动物个体之间存在差异，但很明显该化合物吸收迅速，并广泛生物转化为代谢产物，这些代谢产物主要通过尿液而非粪便排出。对奥昔舒仑的直接作用包括还原为非对映异构的奥昔舒仑醇亚砜和氧化为奥昔舒仑砜。随后，奥昔舒仑醇亚砜被还原为硫化物并氧化为砜。第二相反应似乎仅限于奥昔舒仑醇亚砜和奥昔舒仑醇砜的硫酸化。对奥昔舒仑及其代谢产物进行了药代动力学研究。
