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 journalArticlepeer-review

5 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 (t1/2 = 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 2007

Keywords

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

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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