Pharmacokinetic profile of atenolol aspirinate

Ana C. Montes-Gil; Marcos Zanfolin; Cristina E. Okuyama; Sergio Lilla; Delma P. Alves; Vincenzo Santagada; Elisa Perissutti; Antonio Lavecchia; Ferdinando Fiorino; Beatrice Severino; Giuseppe Caliendo; Fernanda Priviero; Gustavo D. Mendes; Jose L. Donato; Gilberto De Nucci

doi:10.1002/ardp.200700070

Pharmacokinetic profile of atenolol aspirinate

Ana C. Montes-Gil, Marcos Zanfolin, Cristina E. Okuyama, Sergio Lilla, Delma P. Alves, Vincenzo Santagada, Elisa Perissutti, Antonio Lavecchia, Ferdinando Fiorino, Beatrice Severino, Giuseppe Caliendo, Fernanda Priviero, Gustavo D. Mendes, Jose L. Donato, Gilberto De Nucci

Physiology

Research output: Contribution to journal › Article › peer-review

3 Scopus citations

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.

Original language	English (US)
Pages (from-to)	445-455
Number of pages	11
Journal	Archiv der Pharmazie
Volume	340
Issue number	9
DOIs	https://doi.org/10.1002/ardp.200700070
State	Published - Sep 1 2007

Keywords

Antihypertensive therapy
Atenolol
Microwave synthesis
Pharmacokinetics
Prodrug

ASJC Scopus subject areas

Pharmaceutical Science
Drug Discovery

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10.1002/ardp.200700070

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Pharmacokinetic profile of atenolol aspirinate. / Montes-Gil, 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; Mendes, Gustavo D.; Donato, Jose L.; De Nucci, Gilberto.

In: Archiv der Pharmazie, Vol. 340, No. 9, 01.09.2007, p. 445-455.

Research output: Contribution to journal › Article › peer-review

Montes-Gil, 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 ; Mendes, Gustavo D. ; Donato, Jose L. ; De Nucci, Gilberto. / Pharmacokinetic profile of atenolol aspirinate. In: Archiv der Pharmazie. 2007 ; Vol. 340, No. 9. pp. 445-455.

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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{\textregistered}) 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.",

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AU - Santagada, Vincenzo

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