代谢
某些动物研究表明,在氯甲酚的皮肤应用后,吸收迅速,血药浓度峰值出现在1-2小时内,并且给药物质主要通过肾脏排泄,在24小时内几乎完全消除。在排泄的尿液中发现的初级代谢物是葡萄糖醛酸苷和硫酸盐。一些氯甲酚专著将其药代动力学特征比作另一种消毒剂——三氯生——它也作为葡萄糖醛酸苷代谢物迅速通过尿液排泄,这在人体模型中得到了观察。此外,在一项研究中,一名受试者通过肌内注射给药5毫克,三天内14%以葡萄糖醛酸形式排泄,17%以硫酸形式排泄。任何被身体吸收的氯甲酚都可能被肝脏广泛代谢并迅速排泄,主要是通过尿液,以硫酸盐和葡萄糖醛酸苷结合物的形式。
Certain animal studies have shown that following dermal application of chloroxylenol, that the absorption was rapid with a Cmax = 1-2 hours, and that the administered substance was excreted via the kidney with almost complete elimination within 24 hours. The primary metabolites discovered in the excreted urine were glucuronides and sulfates. Some chloroxylenol monographs liken its pharmacokinetic profile to that of another antiseptic - triclosan - which is rapidly excreted in the urine also as a glucuronide metabolite, as observed in the human model. Moreover, In one human subject administered 5 mg intragluteally, 14% was excreted with glucuronic acid and 17% with sulfuric acid at 3 days. Any chloroxylenol absorbed into the body is likely extensively metabolized by the liver and rapidly excreted, mainly in the urine, as sulphate and glucuronide conjugates.
来源:DrugBank