文章基本信息

标题：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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作者：SHIGERU AONUMA ; YASUHIRO KOHAMA ; SHIGEKO FUJIMOTO 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1982
卷号：5
期号：4
页码：252-258
DOI：10.1248/bpb1978.5.252
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：serum protein binding