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实验性片形吸虫病对大鼠肝脏中[3H]四环素和[14C]雷复尼特处置的影响

Incidence of experimental fascioliasis on hepatic disposition of [3H]tetracycline and [14C]rafoxanide in rats.

作者信息

Galtier P, Larrieu G, Franc M

出版信息

J Pharm Sci. 1985 Sep;74(9):1004-6. doi: 10.1002/jps.2600740921.

Abstract

[7-3H]Tetracycline and [carbonyl-14C]rafoxanide were injected intravenously into anesthetized controls and rats in which experimental fascioliasis had been induced by 20 Fasciola hepatica metacercariae. The biliary excretion (1 and 3 h, respectively) of the radioactivity consisted of approximately 4% of the administered dose. In 4-week infested rats, biliary excretion of [3H]tetracycline and hepatic levels of radioactivity were decreased, whereas bile flow did not vary and plasma clearance of the antibiotic was significantly decreased in comparison with control animals. These differences could be the result of the fascioliasis-induced decrease in the hepatic uptake of tetracycline and the limited active transport for its output into bile canaliculi. No change in [14C]rafoxanide disposition was shown in infested rats.

摘要

将[7-3H]四环素和[羰基-14C]雷复尼特静脉注射到麻醉的对照大鼠以及经20个肝片形吸虫囊蚴诱发实验性片形吸虫病的大鼠体内。放射性物质的胆汁排泄(分别为1小时和3小时)约占给药剂量的4%。在感染4周的大鼠中,[3H]四环素的胆汁排泄和肝脏放射性水平降低,而胆汁流量没有变化,与对照动物相比,抗生素的血浆清除率显著降低。这些差异可能是片形吸虫病导致肝脏对四环素摄取减少以及其向胆小管输出的主动转运受限的结果。感染大鼠的[14C]雷复尼特处置未显示变化。

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