Studies on aspirin derivatives with very little side effects. III. Absorption, distribution, excretion and metabolism of tritium-labeled aspirin-isopropylantipyrine (AIA) in rats.
The absorption, distribution, excretion, metabolism and protein binding of orally administered tritium-labeled aspirin-isopropylantipyrine (AIA) were demonstrated in rats. 3H-AIA having 0.1 micro Ci/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 3 h, 72% of the dose was excreted in the feces and urine during 5 d, and 10% was excreted in the bile in 24 h. The highest accumulation of 3H in most organs was found in one to three hr after oral administration and 3H was concentrated in the liver. THe major metabolites excreted in urine within 24 h 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 1 h after the administration was found with serum protein.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000378:metabolism*; D000983:Antipyrine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000378:metabolism; D001241:Aspirin / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000378:metabolism; D001798:Blood Proteins / Q000378:metabolism; D007408:Intestinal Absorption; D008297:Male; D011485:Protein Binding; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution; D014316:Tritium
D000893:Anti-Inflammatory Agents; D001798:Blood Proteins; C025764:N-3'a-propylphenazonyl-2-acetoxybenzamide; D014316:Tritium; D001241:Aspirin; D000983:Antipyrine