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戊巴比妥抑制有机酸的胆汁排泄:大鼠琥珀酰磺胺噻唑的研究。

Pentobarbital inhibits the billiary excretion of organic acids: a study with succinysulfathiazole in the rat.

作者信息

Bailey D G, Paul H, Johnson G E

出版信息

Can J Physiol Pharmacol. 1975 Jun;53(3):470-4. doi: 10.1139/y75-066.

Abstract

The present study was undertaken to determine whether the use of pentobarbital as an anesthetic reduces the biliary excretion of acidic drugs in rats. The drug chosen for the experiment was succinylsulfathiazole, a compound excreted unmetabolized in the bile. Animals anesthetized with urethane excreted 22.1% of the dose in the bile as compared to only 8.4% for the same time period in pentobarbital anesthetized animals. The choice of anesthetic did not affec the bile flow but did influence the bile/liver concentration gradient of succinylsulfathiazole, with the pentobarbital treated rats demonstrating a significantly lower value. Despite the higher biliary excretion of succinylsulfathiazole in the urethane treated rats, the total amount in the bile plus urine was 60% of the dose in the urethane anesthetized animals as compared with 62% in the pentobarbital treated rats. These results suggest that pentobarbital reduced the hepatic transport of succiylsulfathiazole into the bile. The question whether urethane is a preferred anesthetic for biliary excretion studies warrants further investigation.

摘要

本研究旨在确定使用戊巴比妥作为麻醉剂是否会降低大鼠体内酸性药物的胆汁排泄。实验选用的药物是琥珀酰磺胺噻唑,这是一种在胆汁中未代谢而排泄的化合物。用氨基甲酸乙酯麻醉的动物在胆汁中排泄了剂量的22.1%,而在戊巴比妥麻醉的动物中,同一时间段内仅排泄了8.4%。麻醉剂的选择不影响胆汁流量,但确实影响了琥珀酰磺胺噻唑的胆汁/肝脏浓度梯度,戊巴比妥处理的大鼠该值显著较低。尽管在氨基甲酸乙酯处理的大鼠中琥珀酰磺胺噻唑的胆汁排泄较高,但胆汁加尿液中的总量在氨基甲酸乙酯麻醉的动物中为剂量的60%,而在戊巴比妥处理的大鼠中为62%。这些结果表明,戊巴比妥减少了琥珀酰磺胺噻唑向胆汁中的肝脏转运。氨基甲酸乙酯是否是胆汁排泄研究的首选麻醉剂这一问题值得进一步研究。

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