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Effect of aspirin metabolites on pharmacokinetics of aspirin in human blood

Effect of aspirin metabolites on pharmacokinetics of aspirin in human blood

Yakuzaigaku 55(4): 261-265

The effect of aspirin (ASP) metabolites (salicylic acid (SA), salicyluric acid (SAU), gentisic acid (GA) and gentisuric acid (GAU)) on the pharmacokinetics of ASP was investigated. ASP permeated rapidly into erythrocytes and SA was released into the outer was not varied only by adding GA and GAU. Two inhibitor kinetic studies of hemolysate solution (cytosol component) gave patterns intersecting lines on a double-reciprocal plot, which indicated a competitive inhibition of the two drugs. The values of inhibitory constants, K-i obtained from a Dixon plot were 23.4 mu-mol/ml for SA and 18.4 mu-mol/ml for SAU. It is suggested that ASP should be administered with care because ASP is usually administrated continuously.

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