[Pharmacokinetics of acetylsalicylic acid for the prophylaxis of cardiovascular pathology].

BACKGROUND

The metaanalysis of clinical trials on the secondary prevention of myocardial infarction and cerebrovascular disease with antiplatelet drugs suggests that low doses of acetylsalicylic acid (ASA) reduce cardiovascular mortality and morbidity. The ideal galenic formulation should contain a low dose of ASA, should be enteric-coated--to reduce gastrointestinal toxicity--and should be slowly absorbed--to facilitate selective inhibition of thromboxane synthesis by platelets.

METHODS

The kinetics of a single dose of an enteric-coated sustained-release preparation containing 300 mg of ASA were studied in 6 healthy volunteers. Plasma concentrations of ASA and salicylic acid (SA) were measured during 12 hours after its administration.

RESULTS

The time elapsed to achieve maximum plasma concentrations in the systemic circulation was 1 to 4 hours, as compared with 0.25 to 1.5 hours with other conventional preparations of ASA. The maximum plasma concentration recorded in one subject was 1.2 micrograms/ml, as compared with 4.8, 12, and 14 micrograms/ml with other preparations.

CONCLUSIONS

The pharmacokinetic profile of this new preparation fits that proposed by others to produce a selective inhibition of thromboxane synthesis by platelets.