抗炎症薬に関する研究(第32報) : 2-(5H-[1]Benzopyrano[2,3-b]pyridin-7-yl)-propionic Acid(Y-8004)のラット, マウスにおける吸収, 排泄, 分布および代謝

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Absorption, excretion, distribution, and metabolism of 2-(5H-[1] benzopyrano [2,3-b] pyridin-7-yl) propionic acid (Y-8004), a new anti-inflammatory agent, were investigated in rats and mice by the use of ^<14>C-labeled compound (^<14>C-Y-8004). When the radioactive compound was given to rats orally or intraperitoneally, about 50% of the given radio-activity (^<14>C) was excreted in urine and 40% in feces during 72 hr, while about 80% in urine and 20% in feces after oral administration to mice. Approximately 55-60% was recovered in rat bile during 24 hr after oral administration. The highest blood level of ^<14>C was obtained at 0.5-1 hr after oral administration to rats and mice. A good correlation was observed between blood level and dose level. However, apparent species difference in the blood ^<14>C concentration and its disappearance rate were observed between rats and mice. When ^<14>C-Y-8004 was orally administered to bileduct-cannulated rat, the blood ^<14>C concentration and its disappearance rate came close to those of normal mice. The highest concentration of ^<14>C was observed in the serum and relatively high levels in the liver and kidney of rats and mice after oral administration of ^<14>C-Y-8004. In both animals, most of ^<14>C in the serum existed as unchanged material bound to serum protein. Thin-layer chromatography after enzymic, acid, and alkaline hydrolysis experiments showed that the major metabolite in urine and bile of rats was Y-8004 acylglucuronide and in urine of mice Y-8004 acylglucoside. The present investigation provides the first evidence for the formation of an acylglucoside of a drug in mammals.
社団法人日本薬学会の論文
1976-07-25

抗炎症薬に関する研究(第32報) : 2-(5H-[1]Benzopyrano[2,3-b]pyridin-7-yl)-propionic Acid(Y-8004)のラット, マウスにおける吸収, 排泄, 分布および代謝

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