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邻苯二甲酸酯的生化研究。IV. 大鼠体内邻苯二甲酸二庚酯的代谢

Biochemical studies on phthalic esters. IV. Metabolism of diheptyl phthalate in rats.

作者信息

Sato M, Adachi T, Tanaka A, Yamaha T

出版信息

Drug Metab Dispos. 1984 Jul-Aug;12(4):517-22.

PMID:6148222
Abstract

Excretion, organ distribution, and metabolism of di(5-methylhexyl) phthalate (DMHP) were studied in male rats. Orally administered 14C-DMHP was rapidly absorbed and 60 and 30%, respectively, of the radioactivity were found excreted into the urine and feces after 7 days. Biliary excretion amounted to about 15% of the dose after 4 days. No specific high concentrations were found in the organs and tissues. Four major metabolites were isolated by HPLC from the ethyl acetate extract of the urine. All of these compounds were monoesters and determined as 5-hydroxy-5-methylhexyl phthalate, 6-hydroxy-5-methylhexyl phthalate, 5-carboxyhexyl phthalate, and 3-carboxypropyl phthalate by spectral analysis (MS, 1H NMR, 13C NMR, UV, IR, etc.). Unchanged DMHP and mono-5-methylhexyl phthalate (MMHP) were found together with a small amount of phthalic acid in the feces. MMHP and its glucuronide conjugate were detected in the bile.

摘要

研究了邻苯二甲酸二(5-甲基己基)酯(DMHP)在雄性大鼠体内的排泄、器官分布及代谢情况。经口给予14C-DMHP后,其迅速被吸收,7天后分别有60%和30%的放射性物质经尿液和粪便排出。4天后,胆汁排泄量约占给药剂量的15%。在各器官和组织中未发现特异性的高浓度分布。通过高效液相色谱法(HPLC)从尿液的乙酸乙酯提取物中分离出4种主要代谢产物。所有这些化合物均为单酯,通过光谱分析(质谱、1H核磁共振、13C核磁共振、紫外、红外等)确定为邻苯二甲酸5-羟基-5-甲基己酯、邻苯二甲酸6-羟基-5-甲基己酯、邻苯二甲酸5-羧基己酯和邻苯二甲酸3-羧基丙酯。粪便中发现有未变化的DMHP和单-5-甲基己基邻苯二甲酸酯(MMHP)以及少量邻苯二甲酸。胆汁中检测到MMHP及其葡萄糖醛酸结合物。

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