Pharmacokinetics of acetylsalicylic acid and salicylic acid from slow-release formulations of aspirin in healthy Japanese volunteers.

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Acetylsalicylic acid (ASA) and salicylic acid (SA) concentrations in plasma were determined by high-pressure liquid chromatography in 14 healthy male Japanese volunteers after single oral administrations of two different aspirin formulations, enteric-coated granules (Minimax®) and a slow-release tablet (Verin®). Seven subjects received 650 mg and the other seven subjects received 1300 mg of each formulation in a randomly assigned cross-over study. Mean peak SA concentrations in the plasma were significantly higher with the enteric-coated granules than with the slow-release tablets (P<0.001 with both 650 mg and 1300 mg doses), although the times to peak SA concentration in the plasma were not different between the two formulations. Plasma ASA concentrations were detected only following administration of the enteric-coated granules. Mean elimination half-lives (t1/2) of plasma SA were significantly longer with the slow-release tablets at both doses (P<0.05 at 650 mg and P<0.01 at 1300 mg) and the mean areas under the curves (AUC<SUP>∞</SUP><SUB>0</SUB>) were significatly greater with the enteric-coated granules at both doses (P<0.001 at 650 mg and P<0.05 at 1300 mg). Racial differences in SA kinetics between the Japanese and the American subjects were suggested by the results of the study.
一般社団法人日本臨床薬理学会の論文