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Type: Artigo de periódico
Title: Pharmacokinetic profile of atenolol aspirinate
Author: Montes-Gil, AC
Zanfolin, M
Okuyama, CE
Lilla, S
Alves, DP
Santagada, V
Perissutti, E
Lavecchia, A
Fiorino, F
Severino, B
Caliendo, G
Priviero, FBM
Mendes, GD
Donato, JL
de Nucci, G
Abstract: We report microwave-assisted synthetic routes, the pharmacokinetic profile along with results from ulcerogenicity and mutagenicity studies of atenolol aspirinate, and an already described derivative, in which acetyl salicylic acid (aspiring) was connected to atenolol by an ester linkage. Atenolol aspirinate was stable towards aqueous hydrolysis but rapidly hydrolyzed in plasma (t(1/2) = 7.6 min). The results showed that the rapid and complete hydrolysis generates atenolol salicylate, which assumes a conformation stabilized by two intramolecular H-bonds, avoiding its further hydrolysis to salicylic acid and atenolol.
Subject: antihypertensive therapy
microwave synthesis
Country: Alemanha
Editor: Wiley-v C H Verlag Gmbh
Rights: fechado
Identifier DOI: 10.1002/ardp.200700070
Date Issue: 2007
Appears in Collections:Unicamp - Artigos e Outros Documentos

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