大鼠体内苯酰苯胺和水杨酰苯胺的代谢与消除比较。

A comparison of the metabolism and elimination of benzanilide and salicylanilide in the rat.

Mitchell S C, Norbury H M, Waring R H, Gadsden P M, Wood P B

Xenobiotica. 1982 Feb;12(2):93-9. doi: 10.3109/00498258209046782.

Abstract

The metabolism and elimination of benzanilide and salicylanilide in rats were compared. 2. For both compounds, greater than 70% dose was excreted in urine with 20% in faeces, in 3 days. 3. With [14C]benzanilide and [14C]salicylanilide, 40% and 35% respectively of the 14C was excreted in the bile in 24 h. 4. Benzanilide was metabolized to 4'-hydroxybenzanilide (24%), 2-hydroxybenzanilide (salicylanilide, 19%) and 2'-hydroxybenzanilide (13%), with small amounts of 4-hydroxybenzanilide. 5. Salicylanilide was excreted unchanged (56%) with small amounts of the 5-hydroxy and 4'-hydroxy-derivatives. 6. All metabolites were present as glucuronide conjugates; the free aglycones were not found.

摘要

对大鼠体内苯甲酰苯胺和水杨酰苯胺的代谢及排泄情况进行了比较。2. 对于这两种化合物，在3天内，超过70%的剂量经尿液排泄，20%经粪便排泄。3. 给予[14C]苯甲酰苯胺和[14C]水杨酰苯胺后，24小时内分别有40%和35%的14C经胆汁排泄。4. 苯甲酰苯胺代谢为4'-羟基苯甲酰苯胺（24%）、2-羟基苯甲酰苯胺（水杨酰苯胺，19%）和2'-羟基苯甲酰苯胺（13%），还有少量的4-羟基苯甲酰苯胺。5. 水杨酰苯胺以原形排泄（56%），还有少量的5-羟基和4'-羟基衍生物。6. 所有代谢物均以葡萄糖醛酸结合物形式存在；未发现游离苷元。