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Pharmacokinetic Profile of Atenolol Aspirinate
Author(s) -
MontesGil Ana C.,
Zanfolin Marcos,
Okuyama Cristina E.,
Lilla Sergio,
Alves Delma P.,
Santagada Vincenzo,
Perissutti Elisa,
Lavecchia Antonio,
Fiorino Ferdinando,
Severino Beatrice,
Caliendo Giuseppe,
Priviero Fernanda B. M.,
Mendes Gustavo D.,
Donato Jose L.,
Nucci Gilberto de
Publication year - 2007
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700070
Subject(s) - atenolol , chemistry , salicylic acid , hydrolysis , pharmacokinetics , aspirin , metabolite , chromatography , intramolecular force , stereochemistry , pharmacology , organic chemistry , biochemistry , medicine , blood pressure
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 (aspirin®) 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.