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Pharmacokinetics of enteric‐coated aspirin and inhibition of platelet thromboxane A 2 and vascular prostacyclin generation in humans
Author(s) -
Cerletti Chiara,
Marchi Stefano,
Lauri Davide,
Domanin Maurizio,
Lorenzi Giovanni,
Urso Renato,
Dejana Elisabetta,
Latini Roberto,
De Gaetano Giovanni
Publication year - 1987
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1987.128
Subject(s) - aspirin , prostacyclin , thromboxane a2 , platelet , medicine , cyclooxygenase , pharmacology , enteric coating , thromboxane , pharmacokinetics , chemistry , biochemistry , dosage form , enzyme
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 A 2 generation was inhibited by about 20% before any drug could be detected in the peripheral venous blood. A further decline in thromboxane A 2 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 A 2 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. Clinical Pharmacology and Therapeutics (1987) 42, 175–180; doi: 10.1038/clpt.1987.128