N1-乙酰基和N4-乙酰基磺胺甲恶唑在人体中的药代动力学
Pharmacokinetics of N1-acetyl- and N4-acetylsulphamethoxazole in man.
作者信息
Vree T B, Hekster Y A, Damsma J E, van der Kleijn E, O'Reilly W J
出版信息
Clin Pharmacokinet. 1979 Jul-Aug;4(4):310-9. doi: 10.2165/00003088-197904040-00004.
The pharmacokinetics of N1-acetylsulphamethoxazole and N4-acetylsulphamethoxazole in man are described. N1-Acetylsulphamethoxazole is deacetylated to sulphamethoxazole and acetylated to N4-acetylsulphamethoxazole. N4-Acetylsulphamethoxazole is excreted almost unchanged in the urine. The renal excretion rate is independent of the urine flow and urinary pH. N4-Acetylsulphonamides are less lipid soluble and more acidic than their corresponding parent sulphonamides.
描述了N1 - 乙酰磺胺甲恶唑和N4 - 乙酰磺胺甲恶唑在人体中的药代动力学。N1 - 乙酰磺胺甲恶唑会脱乙酰基生成磺胺甲恶唑，并乙酰化生成N4 - 乙酰磺胺甲恶唑。N4 - 乙酰磺胺甲恶唑几乎以原形经尿液排泄。肾脏排泄率与尿流和尿液pH无关。N4 - 乙酰磺胺类药物比其相应的母体磺胺类药物脂溶性更低且酸性更强。
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