放射性同位元素による医薬品の分析(第8報)l-Ephedrine代謝における種差

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The metabolism of l-ephedrine [α-^<14>C] (I) in mice, rats, guinea pigs, and rabbits was studied by a tracer technique to clarify the species differences in metabolic pathways. I was subcutaneously administered in a dose of 5 mg/kg and the urine excreted during 24 hr after the administration was analyzed. In mice, the major part of ^<14>C activity was excreted as unchanged I. In guinea pigs, a large quantity of norephedrine and considerable amounts of benzoic acid and 1-phenyl-1,2-propanediol were excreted, but the amount of p-hydroxyephedrine and its metabolites was very small. In rats, the metabolic activity was low next to mice and the excretion of a considerable amount of substrate was observed ; the p-hydroxylation activity, however, was the highest in animals tested here, so that the main metabolites were p-hydroxyephedrine and its conjugated metabolite. In rabbits, both the N-demethylation and deamination activities were extremely high, and the major part of administered I was excreted as deaminated products. A remarkable amount of 1-phenyl-1,2-propanediol and its conjugated metabolite were also detected in rabbit urine.
公益社団法人日本薬学会の論文
1972-10-25