薬物併用時の代謝に関する研究(第1報)Aspirinのマウス体内動態におよぼすChlormezanoneの影響
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概要
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Effect of chlormezanone on the drug disposition of aspirin was studied in mice given orally aspirin [carboxyl-^<14>C] with or without chlormezanone. The concomitant administration of chlormezanone decreased the stomach content of aspirin-^<14>C, and significantly increased the peak blood level. The distribution of radioactivity in the tissues including the liver and kidneys also increased by the combined use of chlormezanone. In addition, significant difference in urinary excretion of radioactivity was found between aspirin alone and aspirin plus chlormezanone groups. These results indicated that chlormezanone facilitated the gastrointestinal absorption of aspirin and increased the distribution of the drug in the body. Influence of chlormezanone on the metabolism of aspirin was examined by comparing quantitatively the concentration of metabolites in the plasma, tissues, and urine between the two groups. In both groups, aspirin was metabolized in vivo to salicylic acid, salicylic acid glucuronide, o-hydroxyhippuric acid, and gentisic acid. These metabolites in the plasma, liver, and kidneys showed higher concentrations due to increase of total radioactivity in aspirin plus chlormezanone group than in aspirin alone group. However, it was considered that chlormezanone had no effect qualitatively on the in vivo metabolism of aspirin, since no difference in the composition of metabolites was found between the two groups.
- 公益社団法人日本薬学会の論文
- 1978-01-25
著者
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立沢 晴男
第一製薬株式会社中央研究所
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立沢 晴男
第一製薬株式会社研究所
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立沢 晴男
Drug Metabolism Research Center Research Institute Daiichi Seiyaku Co. Ltd.
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