el Dareer S M, Kalin J R, Tillery K F, Hill D L
Southern Research Institute, Birmingham, Alabama.
J Toxicol Environ Health. 1987;22(4):405-15. doi: 10.1080/15287398709531082.
The disposition of 14C-labeled decabromobiphenyl ether (DBBE) in male Fischer rats dosed by feeding (0.025-5.0% of the diet) or intravenously (1 mg/kg) was determined. For rats dosed by feeding, intestinal absorption of DBBE was evident in that the intact compound was present in extracts of liver. For these rats, the size of the liver increased with increasing concentration of DBBE in the diet. Liver contained a maximum of 0.449% of the administered radioactivity at 24 h after feeding rats a diet containing 0.0277% [14C]DBBE; no other organ or tissue contained more than 0.26%. The total amount of radioactivity found in tissues was less than 1% of the dose. Of the radioactivity recovered in the feeding experiments, more than 99% was in the feces and gut contents at 72 h; a maximum of 0.012% of the dose was in the urine. In the feces of rats fed [14C]DBBE, there were three metabolites, which together comprised 1.5-27.9% of the radioactivity. Since absorption was minimal, most of the metabolism of [14C]DBBE apparently took place in the gastrointestinal tract. The metabolites increased in percent of total radioactivity with the content of DBBE in the diet, an indication that enzyme induction in intestinal bacteria may have occurred at the higher doses. More extensive metabolism of [14C]DBBE occurred after intravenous administration; only 37% of the radioactivity in the feces was unchanged DBBE. At 72 h after dosing, fecal excretion accounted for 70% of the dose; only 0.129% appeared in the urine. Muscle retained 12.9% and skin 7.25% of the radioactivity administered. In 4 h, rats with biliary cannulas excreted in the bile 7.17% of the intravenously administered radioactivity; less than 1% was excreted as intact DBBE. Biliary excretion was apparently the major route for elimination of the intravenously administered compound. The rapid excretion and extensive metabolism of DBBE, relative to other polyhalogenated compounds, are advantageous properties that may allow it to be used in place of structurally similar compounds presently employed in industrial applications.
测定了雄性Fischer大鼠经口(占饮食的0.025 - 5.0%)或静脉注射(1 mg/kg)给予14C标记的十溴联苯醚(DBBE)后的处置情况。对于经口给药的大鼠,DBBE在肠道的吸收很明显,因为完整的化合物存在于肝脏提取物中。对于这些大鼠,肝脏大小随着饮食中DBBE浓度的增加而增大。给大鼠喂食含0.0277% [14C]DBBE的饮食后24小时,肝脏中所含放射性最多占给药放射性的0.449%;没有其他器官或组织所含放射性超过0.26%。组织中发现的放射性总量不到剂量的1%。在喂食实验中回收的放射性中,72小时时超过99%存在于粪便和肠道内容物中;尿液中最多占剂量的0.012%。在喂食[14C]DBBE的大鼠粪便中,有三种代谢物,它们总共占放射性的1.5 - 27.9%。由于吸收极少,[14C]DBBE的大部分代谢显然发生在胃肠道。代谢物占总放射性的百分比随着饮食中DBBE的含量增加,这表明在较高剂量下肠道细菌中可能发生了酶诱导。静脉注射后[14C]DBBE发生了更广泛的代谢;粪便中只有37%的放射性是未变化的DBBE。给药72小时后,粪便排泄占剂量的70%;尿液中仅出现0.129%。肌肉保留了给药放射性的12.9%,皮肤保留了7.25%。在4小时内,胆管插管的大鼠胆汁中排泄了静脉注射放射性的7.17%;以完整DBBE形式排泄的不到1%。胆汁排泄显然是静脉注射化合物消除的主要途径。与其他多卤代化合物相比,DBBE的快速排泄和广泛代谢是有利的特性,这可能使其能够替代目前工业应用中使用的结构相似的化合物。