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.
Pharmacokinetic profile of atenolol aspirinate / A. C., MONTES GIL; M., Zanfolin; C. E., Okuyama; S., Lilla; D. P., Alves; Santagada, Vincenzo; Perissutti, Elisa; Lavecchia, Antonio; Fiorino, Ferdinando; Severino, Beatrice; Caliendo, Giuseppe; F. B. M., Priviero; G. D., Mendes; J. L., Donato; G., DE NUCCIA. - In: ARCHIV DER PHARMAZIE. - ISSN 0365-6233. - ELETTRONICO. - 340:(2007), pp. 445-455. [10.1002/ardp.200700070]
Pharmacokinetic profile of atenolol aspirinate
SANTAGADA, VINCENZO;PERISSUTTI, ELISA;LAVECCHIA, ANTONIO;FIORINO, FERDINANDO;SEVERINO, BEATRICE;CALIENDO, GIUSEPPE;
2007
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 (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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
