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

Research output: Contribution to journalArticle

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 languageEnglish (US)
Pages (from-to)445-455
Number of pages11
JournalArchiv der Pharmazie
Volume340
Issue number9
DOIs
StatePublished - Sep 1 2007

Keywords

  • Antihypertensive therapy
  • Atenolol
  • Microwave synthesis
  • Pharmacokinetics
  • Prodrug

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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  • Cite this

    Montes-Gil, A. C., Zanfolin, M., Okuyama, C. E., Lilla, S., Alves, D. P., Santagada, V., Perissutti, E., Lavecchia, A., Fiorino, F., Severino, B., Caliendo, G., Priviero, F., Mendes, G. D., Donato, J. L., & De Nucci, G. (2007). Pharmacokinetic profile of atenolol aspirinate. Archiv der Pharmazie, 340(9), 445-455. https://doi.org/10.1002/ardp.200700070