Pharmacokinetics of enteric-coated aspirin and inhibition of platelet thromboxane A2 and vascular prostacyclin generation in humans

Chiara Cerletti, Stefano Marchi, Davide Lauri, Maurizio Domanin, Giovanni Lorenzi, Renato Urso, Elisabetta Dejana, Roberto Latini, Giovanni de Gaetano

Research output: Contribution to journalArticlepeer-review

Abstract

We evaluated whether an enteric-coated aspirin formulation showed a "presystemic" component in its antiplatelet effect and if so would spare vascular cyclooxygenase. In six healthy volunteers, 30 to 45 minutes after ingestion of 325 mg enteric-coated aspirin, platelet thromboxane AZ generation was inhibited by about 20% before any drug could be detected in the peripheral venous blood. A further decline in thromboxane A2 generation occurred with appearance of aspirin in blood between 60 and 240 minutes. No presystemic component could be detected after 325 mg aspirin tablets. Ten patients undergoing saphenectomy received 325 mg of either aspirin tablet or enteric-coated aspirin; 12 hours later platelet thromboxane A2 and peripheral vascular prostacyclin generation were significantly reduced by 98% and 58%, respectively. The effects of the two aspirin formulations were not different. Aspirin formulations with "presystemic" component in their antiplatelet effect may not necessarily result in sparing of peripheral vascular cyclooxygenase.

Original languageEnglish
Pages (from-to)175-180
Number of pages6
JournalClinical Pharmacology and Therapeutics
Volume42
Issue number2
Publication statusPublished - Aug 1987

ASJC Scopus subject areas

  • Pharmacology

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