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新型1,3,8-三取代黄嘌呤呋拉茶碱的一些药代动力学特征。

Some pharmacokinetic characteristics of furafylline, a new 1,3,8-trisubstituted xanthine.

作者信息

Segura J, Garcia I, Tarrus E

出版信息

J Pharm Pharmacol. 1986 Aug;38(8):615-8. doi: 10.1111/j.2042-7158.1986.tb03092.x.

Abstract

After administration of furafylline, a, 1,3,8-trisubstituted xanthine, to beagle dogs at 0.5 and 10 mg kg-1 an elimination half-life 2-10 times longer than that of theophylline was observed. The kinetics were dose-dependent but no phase I metabolites were detected. When the compound was given orally to humans at a dose of 1.3-1.9 mg kg-1 a mean beta elimination half-life of 48.1 +/- 10.8 h was obtained after an initial distribution phase. Evidence of non-linear kinetics for plasma levels below 0.6 microgram ml-1 was also obtained. Other 1,3,8-trisubstituted xanthines, may also have a lower elimination rate than theophylline.

摘要

在以0.5和10毫克/千克的剂量给比格犬施用1,3,8 - 三取代黄嘌呤呋拉茶碱后,观察到其消除半衰期比茶碱长2至10倍。动力学呈剂量依赖性,但未检测到I相代谢物。当该化合物以1.3 - 1.9毫克/千克的剂量口服给予人类时,在初始分布相后获得的平均β消除半衰期为48.1±10.8小时。还获得了血浆水平低于0.6微克/毫升时非线性动力学的证据。其他1,3,8 - 三取代黄嘌呤的消除速率可能也比茶碱低。

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