Tanaka A, Matsumoto A, Yamaha T
Toxicology. 1978 Feb;9(1-2):109-23. doi: 10.1016/0300-483x(78)90036-7.
The excretion, distribution and metabolism of DBP were studied in rats. More than 90% of the dose was excreted in the urine within 48 h following intravenous or oral administration, but the faecal excretion was low. Biliary excretion was remarkably higher than that in the faeces when DBP was given orally. No significant retention was observed in organs and tissues at 24 h after dosing. In vitro experiments showed that DBP was hydrolysed very rapidly to MBP by the esterase of rat liver microsome. DBP was found to be a strong inhibitor for the succinate dehydrogenase of rat liver. DBP and its metabolites, MBP and phthalic acid, did not produce any striking effect upon hepatic and serum enzyme activities in vitro. Urinary metabolites of orally ingested DBP were investigated in 3 species, namely, rats, hamsters and guinea pigs. MBP was a common major metabolite in all 3 species. A further increment was apparently excreted as the glucuronide in the rat, hamster and guinea pig together with a small amount of phthalic acid and unchanged DBP. Omega- or omega-1 oxidation products of MBP were also detected in the urine.
在大鼠体内研究了邻苯二甲酸二丁酯(DBP)的排泄、分布和代谢情况。静脉注射或口服给药后48小时内,超过90%的剂量经尿液排泄,但经粪便排泄量较低。口服DBP时,胆汁排泄显著高于粪便排泄。给药后24小时,在器官和组织中未观察到明显的潴留现象。体外实验表明,DBP在大鼠肝微粒体酯酶作用下迅速水解为单丁基邻苯二甲酸酯(MBP)。DBP被发现是大鼠肝脏琥珀酸脱氢酶的强抑制剂。DBP及其代谢产物MBP和邻苯二甲酸在体外对肝脏和血清酶活性未产生任何显著影响。研究了大鼠、仓鼠和豚鼠这3个物种口服摄入DBP后的尿液代谢产物。MBP是所有3个物种中常见的主要代谢产物。在大鼠、仓鼠和豚鼠体内,MBP进一步代谢生成的产物显然以葡萄糖醛酸苷形式排泄,同时伴有少量邻苯二甲酸和未代谢的DBP。尿液中还检测到了MBP的ω-或ω-1氧化产物。