STUDIES ON ASPIRIN DERIVATIVES WITH VERY LITTLE SIDE EFFECTS. III. ABSORPTION, DISTRIBUTION, EXCRETION AND METABOLISM OF TRITIUM-LABELED ASPIRIN-ISOPROPYLANTIPYRINE (AIA) IN RATS

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The absorption, distribution, excretion, metabolism and protein binding of orally administered tritium-labeled aspirin-isopropylantipyrine (AIA) were demonstrated in rats. ^3H-AIA having 0.1μCi/mg of specific activity and 93.2% of radiochemical purity was prepared by the Wilzbach's method. When ^3H-AIA was administered orally to rats, about 20% of the given ^3H was absorbed from gastro-intestinal tracts in 30 min and about 50% in 3h, 72% of the dose was excreted in the feces and urine during 5d, and 10% was excreted in the bile in 24h. The highest accumulation of ^3H in most organs was found in one to three hr after oral administration and ^3H was concentrated in teh liver. The major metabolites excreted in urine within 24h after administration were salicylic acid-isopropylantipyrine (SIA) sulfate (57.7%) and SIA glucuronide (30.5%). The amount of free SIA excreted in urine was 1.2%. The carboxylamide bond of AIA was never cleaved in vivo to give salicylic acid and 3-aminomethylisopropylantipyrine. About 58% of ^3H in blood 1h after the administration was bound with serum protein.
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