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  • Absorption kinetics of low-dose chewable aspirin--implications for acute coronary syndromes.

Absorption kinetics of low-dose chewable aspirin--implications for acute coronary syndromes.

European journal of clinical investigation (2014-11-18)
Eva-Luise Hobl, Rainer W Schmid, Thomas Stimpfl, Josef Ebner, Bernd Jilma
ABSTRACT

This study describes the implications of the pharmacokinetics of low-dose chewable aspirin for acute coronary syndromes. Current guidelines recommend the administration of 162-325 mg aspirin chewing tablets for the treatment of acute myocardial infarction. Although aspirin is widely used and a cornerstone in myocardial infarction, there is no information available on the pharmacokinetics of low doses of chewable aspirin. This prospective trial assessed the pharmacokinetics of acetylsalicylic acid and its metabolite salicylic acid after intake of 162 mg chewable low-dose aspirin in 35 healthy volunteers. Plasma drug and metabolite levels were analysed using high-performance liquid chromatography, and corresponding pharmacodynamics were determined by impedance aggregometry. Acetylsalicylic acid was rapidly absorbed with a mean Tmax of 27 ± 8 min. Tmax of salicylic acid was 69 ± 21 min. Mean Cmax was 1·8 ± 0·6 mg/L and 7·6 ± 1·4 for acetylsalicylic acid and salicylic acid, respectively. Arachidonic acid-induced aggregation showed maximum platelet inhibition 30 min after drug ingestion. The characterization of the plasma-time profile fills the gap between the lack of data on pharmacokinetics and the pharmacodynamics and the recommendation for using low-dose chewable aspirin for acute coronary syndromes. We describe for the first time that a 162-mg dose of chewable aspirin is rapidly absorbed and achieves plasma concentrations of the active metabolite salicylic acid required to maximally inhibit platelet aggregation. However, a 162-mg dose is truly a minimum, and doubling this dose might be better for patients with myocardial infarction.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Acetylsalicylic acid, analytical standard
Sigma-Aldrich
Acetylsalicylic acid, ≥99.0%
Acetylsalicylic acid, European Pharmacopoeia (EP) Reference Standard
Acetylsalicylic acid for peak identification, European Pharmacopoeia (EP) Reference Standard
USP
Aspirin, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Aspirin, meets USP testing specifications
Supelco
Aspirin (Acetyl Salicylic Acid), Pharmaceutical Secondary Standard; Certified Reference Material