薬物併用時の代謝に関する研究(第2報)Chlormezanoneのマウス体内動態およびAspirinとの相互作用

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概要

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• Drug disposition of chlormezanone-^<14>C and its interaction with aspirin were studied in mice. Chlormezanone-^<14>C was well and rapidly absorbed from the gastrointestinal tract after oral administration of 24mg/kg. Blood levels of radioactivity reached a peak 60 min later. Tissue concentration became lower in the order of the adrenal gland, kidney, liver, pituitary, lung, brain and muscle. The high affinity of chlormezanone-^<14>C for the tissues was deduced from the fact that the concentration ratio of tissue to blood was larger than 1.0. Urinary excretion of radioactivity was approximately 21% of the administered dose within 120min. Examination of metabolites in the plasma, liver, kidneys and brain indicated that chlormezanone-^<14>C was mainly found in the tissues in an unchanged form but its metabolites such as p-chlorobenzoic acid, p-chlorohippuric acid, N-methyl-p-chlorobenzamide, 2-[N-methyl-N-(p-chlorobenzoyl)] carbamoylethylsulfonic acid and p-chlorobenzoic acid glucuronides showed a low concentration. Aspirin administered concomitantly had no effect on the absorption, distribution and metabolism of chlormezanone-^<14>C, but significantly inhibited urinary excretion of chlormezanone-^<14>C and its metabolites. These results suggest that chlormezanone-^<14>C is well and rapidly absorbed and is distributed highly into tissues without the effect of combination of aspirin and exerts its pharmacological effect in an unchanged form.

• 公益社団法人日本薬学会の論文
• 1978-02-25

著者

• 立沢 晴男

  第一製薬株式会社中央研究所

• 立沢 晴男

  第一製薬株式会社研究所

• 立沢 晴男

  Drug Metabolism Research Center Research Institute Daiichi Seiyaku Co. Ltd.

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