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前列环素类似物ZK 36 374在比格犬体内的药代动力学和生物转化

Pharmacokinetics and biotransformation of the prostacyclin analogue, ZK 36 374, in the beagle dog.

作者信息

Krause W

出版信息

Prostaglandins Leukot Med. 1984 Feb;13(2):143-51. doi: 10.1016/0262-1746(84)90004-0.

Abstract

Tritium-labelled ZK 36 374 was administered to three female beagle dogs intravenously and orally in a dose of 200 micrograms/kg. Blood and plasma levels and excretion with urine and feces of drug and metabolites were measured. ZK 36 374 was rapidly absorbed. The bioavailability was estimated as about 10% of the dose. The concentration of radio-labelled compounds in the plasma declined in three phases with half-lives of 3 min, 46 min and approx. 2 d. The half-life of the unchanged drug was 14 min. ZK 36 374 was totally metabolized and excreted mainly via the kidneys.

摘要

将氚标记的ZK 36 374以200微克/千克的剂量静脉注射和口服给予三只雌性比格犬。测量了药物和代谢物在血液、血浆中的水平以及尿液和粪便中的排泄情况。ZK 36 374吸收迅速。生物利用度估计约为给药剂量的10%。血浆中放射性标记化合物的浓度呈三个阶段下降,半衰期分别为3分钟、46分钟和约2天。原形药物的半衰期为14分钟。ZK 36 374完全代谢,主要通过肾脏排泄。

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