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Xenobiotica
the fate of foreign compounds in biological systems
Volume 37, 2007 - Issue 7
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Research Article

Absorption, distribution and excretion of the new thienopyridine agent prasugrel in rats

, , , , , , & show all
Pages 788-801 | Received 26 Feb 2007, Accepted 14 Apr 2007, Published online: 22 Sep 2008
 

Abstract

Prasugrel is converted to the pharmacologically active metabolite after oral dosing in vivo. In this study, 14C-prasugrel or prasugrel was administered to rats at a dose of 5 mg kg–1. After oral and intravenous dosing, the values of AUC0–∞ of total radioactivity were 36.2 and 47.1 µg eq. h ml–1, respectively. Oral dosing of unlabeled prasugrel showed the second highest AUC0–8 of the active metabolite of six metabolites analyzed. Quantitative whole body autoradiography showed high radioactivity concentrations in tissues for absorption and excretion at 1 h after oral administration, and were low at 72 h. The excretion of radioactivity in the urine and feces were 20.2% and 78.7%, respectively, after oral dosing. Most radioactivity after oral dosing was excreted in bile (90.1%), which was reabsorbed moderately (62.4%). The results showed that orally administered prasugrel was rapidly and fully absorbed and efficiently converted to the active metabolite with no marked distribution in a particular tissue.

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