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新型抗高血压药FCE 22716及其N-氧化物(FCE 24220)在大鼠体内的代谢命运。

Metabolic fate of FCE 22716, a new antihypertensive agent, and of its N-oxide (FCE 24220) in the rat.

作者信息

Cocchiara G, Battaglia R, Fontana E, Benedetti M S

机构信息

Department of Pharmacokinetics and Metabolism, Farmitalia Carlo Erba, Erbamont Group, Milan, Italy.

出版信息

Drug Metabol Drug Interact. 1992;10(3):185-97. doi: 10.1515/dmdi.1992.10.3.185.

DOI:10.1515/dmdi.1992.10.3.185
PMID:1424640
Abstract

[3H]-FCE 22716 and [3H]-FCE 24220 were given both orally and intravenously to the rat. Radioactivity was mainly eliminated by the faecal route after oral administration in both cases. After intravenous administration, renal excretion was twice the faecal one in the case of FCE 22716, whereas for FCE 24220 the two routes were equal. In urine FCE 22716 was eliminated almost completely unchanged after both oral and intravenous administration. FCE 24220 was extensively reduced to FCE 22716 after oral administration, whereas after intravenous treatment, this reduction, although important, was not complete.

摘要

给大鼠口服和静脉注射[³H]-FCE 22716和[³H]-FCE 24220。两种情况下,口服给药后放射性主要通过粪便途径消除。静脉注射后,FCE 22716的肾排泄量是粪便排泄量的两倍,而对于FCE 24220,两种途径的排泄量相等。口服和静脉注射后,尿液中的FCE 22716几乎完全以原形消除。口服给药后,FCE 24220大量转化为FCE 22716,而静脉注射后,这种转化虽然显著,但并不完全。

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