Studies on Metabolism of Bromazepam. I. Isolation and Identification of the Metabolites of Bromazepam in Urine

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  • Bromazepamの代謝に関する研究(第1報)尿中代謝産物の単離と同定
  • Bromazepamの代謝に関する研究-1-尿中代謝産物の単離と同定
  • Bromazepam ノ タイシャ ニ カンスル ケンキュウ 1 ニョウ チュウ タイシャ サンブツ ノ タンリ ト ドウテイ

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Abstract

Besides the unchanged drug, two major metabolites were found from the urine of animals that received orally high doses of bromazepam, 7-bromo-1, 3-dihydro-5-(2-pyridyl)-2H-1, 4-benzodiazepin-2-one. The metabolites were purified by column chromatography on silica gel and recrystallization. From the spectral and elemental analysis data, the structure of these metabolites were identified as 2-amino-5-bromobenzoylpyridine and assumed to be 2-amino-5-bromo-3-hydroxybenzoylpyridine, the latter being excreted as its glucuronide in the urine. It may be concluded that bromazepam after opening of the diazepine ring undergoes a process of hydroxylation.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 92 (10), 1237-1241, 1972

    The Pharmaceutical Society of Japan

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