医薬品の吸収, 排泄および代謝に関する研究(第8報)新消炎鎮痛剤2-Oxo-3-[4-(1-oxo-2-isoindolinyl)phenyl]butanamide(OIB)のラットにおける代謝

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The blood concentration, urinary, fecal and biliary excretion and urinary metabolites were studied in rats after the oral administration of 2-oxo-3-[4-(1-oxo-2-isoindolinyl)-phenyl] butamide (OIB) and its ground mixture with PVP (1 : 4 w/w) as a suspension in 1% gum arabic solution. The experiments with the labelled compound revealed that a maximum blood concentration of the radioactivity was about seven times higher after the administration of the ground mixture than after that of ^<14>C-OIB. During a 48 h period after the administration, 8.3% of the given dose was recovered from the urine in the case of ^<14>C-OIB and 37.9% in the case of the ground mixture. After the single administration of ^<14>C-OIB, 5.5% of the dose was excreted in the bile and 87.1% in feces for 48 hours. On the other hand, metabolites of OIB were analyzed by thin-layer chromatography and mass-spectrometry. Sixteen metabolites were detected. Unchanged compound and six metabolites, M1,M4,M7,M10,M12 and M13 were identified by comparison with the corresponding authentic samples. The other metabolites were considered to be hydroxylated on the aromatic ring in the 1-oxo-isoindolinyl moiety.
社団法人日本薬学会の論文
1982-09-25