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抗菌剂尼布罗烷(5-溴-2-甲基-5-硝基间二氧杂环戊烷)在大鼠体内的代谢

Metabolism of the antimicrobial agent nibroxane, 5-bromo-2-methyl-5-nitro-m-dioxane, in the rat.

作者信息

Sullivan H R, Marshall F J, Bopp R J

出版信息

Xenobiotica. 1978 Aug;8(8):495-502. doi: 10.3109/00498257809056151.

Abstract
  1. The metabolism of nibroxane, a topically effective antimicrobial agent has been studied in the rat after oral and dermal administrations. 2. Plasma level studies in vitro and in vivo showed nibroxane to be rapidly debrominated to 2-methyl-5-nitro-m-dioxane. 3. Nibroxane is rapidly absorbed and extensively metabolized in the rat regardless of the route of administration. 4. Enzymic hydrolysis of the m-dioxane ring was of major importance in the biotransformation of nibroxane. The major eliminated metabolite in the rat was 2-nitropropan-1,3-diol.
摘要
  1. 已对局部有效的抗菌剂尼布罗烷在大鼠口服和经皮给药后的代谢情况进行了研究。2. 体外和体内的血浆水平研究表明,尼布罗烷迅速脱溴生成2-甲基-5-硝基间二氧杂环己烷。3. 无论给药途径如何,尼布罗烷在大鼠体内均能迅速吸收并广泛代谢。4. 间二氧杂环己烷环的酶促水解在尼布罗烷的生物转化中起主要作用。大鼠体内主要的消除代谢产物是2-硝基丙-1,3-二醇。

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