Payan J P, Fabry J P, Beydon D, de Ceaurriz J
Institut National de Recherche et de Sécurité, Vandoeuvre, France.
J Appl Toxicol. 1991 Dec;11(6):437-42. doi: 10.1002/jat.2550110610.
Renal, biliary, pulmonary and faecal excretion experiments were carried out with labelled hexachloro-1,3-butadiene [( 14C]HCBD) in male Sprague-Dawley rats, given orally (p.o.) and intravenously (i.v.) in doses of 1 and 100 mg kg-1 as a solution in polyethylene glycol. The radioactivity excreted over 72 h was determined in rats fitted with exteriorized biliary cannulae and in rats whose bile ducts remained fully functional, respectively. In addition, bile duct-duodenum cannula-linked rats, of which the donor was given 100 mg kg-1 [14C]HCBD orally and the recipient had also a bile fistula, were examined within 30 h for radioactivity in the excreta, the kidney, the liver and the plasma. In non-cannulated rats, fractional urinary excretion decreased when the dosage increased and amounted to 23% and 8.6% after i.v. injection or 18.5% and 8.9% after p.o. administration of 1 and 100 mg kg-1, respectively. Pulmonary excretion of radioactivity was less than 9% and was not affected by the increase in dosage. In bile duct-cannulated rats, fractional urinary excretions were similar irrespective of the dose and the route of administration and amounted to ca. 7.5% of the dose. Decrease in fractional biliary excretion occurred with increase in dosage (88.7% vs 72%) after i.v. injection and (66.8% vs 58%) after gavage. In cannulated rats, faecal excretion was less than 0.5% after i.v. injection and accounted for 3% and 16% of the dose after p.o. administration of 1 and 100 mg kg-1, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
在雄性斯普拉格 - 道利大鼠中,采用标记的六氯 - 1,3 - 丁二烯[(14C)六氯 - 1,3 - 丁二烯]进行了肾脏、胆汁、肺部和粪便排泄实验。大鼠经口(p.o.)和静脉内(i.v.)给予剂量为1和100 mg kg-1的聚乙二醇溶液。分别对装有外置胆管插管的大鼠和胆管功能完全正常的大鼠,测定72小时内排泄的放射性。此外,对胆管 - 十二指肠插管连接的大鼠进行了检查,供体经口给予100 mg kg-1 [14C]六氯 - 1,3 - 丁二烯,受体也有胆瘘,在30小时内检测排泄物、肾脏、肝脏和血浆中的放射性。在未插管的大鼠中,静脉注射或经口给予1和100 mg kg-1后,随着剂量增加,尿排泄分数下降,分别为23%和8.6%(静脉注射后)或18.5%和8.9%(经口给药后)。肺部放射性排泄小于9%,且不受剂量增加的影响。在胆管插管的大鼠中,尿排泄分数与剂量和给药途径无关,约占剂量的7.5%。静脉注射后(88.7%对72%)和灌胃后(66.8%对58%),随着剂量增加,胆汁排泄分数下降。在插管大鼠中,静脉注射后粪便排泄小于0.5%,经口给予1和100 mg kg-1后分别占剂量的3%和16%。(摘要截于250字)