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Pharmacokinetic profile of atenolol aspirinate

  • Ana C. Montes-Gil
    ,
  • Marcos Zanfolin
    ,
  • Cristina E. Okuyama
    ,
  • Sergio Lilla
    ,
  • Delma P. Alves
    ,
  • Vincenzo Santagada
*Corresponding author for this work
  • Universidade Estadual de Campinas
    ,
  • Galeno Research Unit
    ,
  • University of Naples Federico II
    ,
  • Physiology
Scholary Output:
Contribution to journal
Article
 Peer-review

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.

Publication Information

Output type

Scholary Output:
Contribution to journal
Article
 Peer-review

Original language

English (US)

Pages from-to (Number of pages)

Pages 445-455 (11 pages)

Journal (Volume, Issue Number)

Archiv der Pharmazie (Volume 340, Issue 9)

Publication milestones

  • Published - 09/2007

Publication status

Published - 09/2007

ISSN

0365-6233

Publication IDs

  • Scopus: 34748819542
  • PubMed: 17763375

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SciVal
Author count
15
SciVal
citations
3
SciVal
Paper percentile
44
Scopus
citations
5, opens in new tab
Fractional count
1
Fractional count
0.07
Fractional count
14
Fractional count
0.93
Fractional count
1
Fractional count
1

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Citation count
5
Captures
15

Funding Details

The work described in this paper was in part, supported as part of the Esprit Me"sto project, the British Aerospace Dependable Computing Systems Centre and the BAe Centre of Excellence in Cockpit Automation Research. I am also indebted to John McCarthy and Pat Healey for the article that inspired some of our thinking in this paper (Healey & McCarthy, 1997). Thanks are due to the anonymous referees who were patient enough to read a rough version of this paper and make highly constructive comments.