Synthesis and evaluation of dual acting esters of aspirin and ketorolac

Authors

  • PK HALEN Pharmacy Department, Faculty of Technology and Engineering, Kalbahavan, The M.S. University of Baroda, Vadodara-390001. India
  • MR YADAV Pharmacy Department, Faculty of Technology and Engineering, Kalbahavan, The M.S. University of Baroda, Vadodara-390001. India
  • KK CHAGTI Pharmacy Department, Faculty of Technology and Engineering, Kalbahavan, The M.S. University of Baroda, Vadodara-390001. India
  • CS RESHMI Pharmacy Department, Faculty of Technology and Engineering, Kalbahavan, The M.S. University of Baroda, Vadodara-390001. India
  • R GIRIDHAR Pharmacy Department, Faculty of Technology and Engineering, Kalbahavan, The M.S. University of Baroda, Vadodara-390001. India

Keywords:

Aspirin, Ketorolac, Local irritation

Abstract

To overcome the gastric toxicity of aspirin and ketorolac fi ve different N,N-disubstitutedaminoethyl ester derivatives foreach were synthesized and evaluated. The intact esters were specially designed to satisfy the structural requirement forpossessing the anticholinergic activity before cleavage. Besides blocking the acidic carboxyl group by esterifi cation thisactivity was incorporated into the synthesized esters with an expected additional benefi t of having reduced gastric acidsecretion and thereby abolishing the local irritation by a dual mechanism. This report describes the synthesis, hydrolysiskinetics and the biological activity of these esters. All the ester derivatives were found to be stable in buffers (pH 2.0and 7.4) for suffi cient time period, assuring them to be absorbed intact and to successfully overcome the local gastricirritation of the parent drug. A fast enzymatic hydrolysis was observed for all the derivatives in 80% pooled humanserum. The synthesized esters were found to possess the proposed anticholinergic activity. The ulcerogenic potential ofthe evaluated derivatives was signifi cantly reduced. However, the anti-infl ammatory activity in case of aspirin derivativeswas much lower.

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References

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Published

2006-03-20

How to Cite

1.
HALEN P, YADAV M, CHAGTI K, RESHMI C, GIRIDHAR R. Synthesis and evaluation of dual acting esters of aspirin and ketorolac. Ars Pharm [Internet]. 2006 Mar. 20 [cited 2024 Jul. 22];47(1):61-79. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/5017

Issue

Vol. 47 No. 1 (2006)

Section

Original Articles

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