新鎮痛剤l-1,4-Dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine Hydrobromide(l-ST-2121)の生体内運命(第3報)マウス, ラット, ウサギ, イヌ, サルおよびヒトにおける吸収, 排泄および代謝について

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The biological fate of l-1,4-dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine hydrobromide (l-ST-2121) was studied in mouse, rat, rabbit, dog, monkey and man after i.v. or s.c. administration. Plasma levels of unchanged l-ST-2121 showed typical two-phase elimination curve after i.v. adminstration to rat and rabbit, and conjugated l-ST-2121 reached the maximum in about 30 min after the injection to rabbit. After s.c. administration to mouse, rat, rabbit, dog, and man, plasma levels of the unchanged drug reached the maximum (for example about 2 μg/ml in mouse) within about 40 min and the peak was shifted to the later time in larger animals. The plot of the biological half-life vs. body weight of each animals in log-log scale gave a linear function curve except for rat, and the maximum plasma levels of the unchanged form were approximately proportional to each dose. Urinary excretion percentage of the unchanged form, the conjugated, 9,10-dihydroxy compound and nor-compound were measured after s.c. administration to each animals and man. Total excretion percentages were 65-99% and the speeies differences were observed in the excretion pattern of the unchanged and nor-compound, that is, the largest excretion of the unchanged form is 36% in mouse and the least is 5% in dog, and the largest excretion of nor-compound is 13% in man and the least is 1% in dog.
公益社団法人日本薬学会の論文
1980-09-25