5-Fluorouracil-6-^<14>Cの経皮投与時での生体内運命について

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The metabolic fate of 5-fluorouracil was studied in the rat by using ^<14>C-labeled compound in ointment. Following the percutaneous administration of 5-fluorouracil in ointment, the rat excreted about 4% of the administered radioactivity in urine, 0.2% in feces, and 2.7% in respiratory CO_2 within 72 hr, and about 90% of administered radioactivity remained at the site of application. Absorption of 5-fluorouracil in ointment from the skin was almost completed within the first 1 hr after ointment application and the maximum levels of radioactivity in rat tissues and blood also reached in about 1 hr after the application. Distribution of radioactivity in rat tissues was more highly located in the liver, kidneys, and in dermic and hypodermic tissues than in other tissues. After application of 0.5g per rat, of ointment containing radioactive 5-fluorouracil, the radioactive substances excreted in urine after 72 hr were unchanged 5-fluorouracil, α-fluoro-β-ureidopropionic acid, α-fluoro-β-guanidopropionic acid, and α-fluoro-β-alanine which were present in about 7.9%, 13.5%, 5.8%, 66.1%, and 3.7% of total radioactivity in the urine, respectively.
公益社団法人日本薬学会の論文
1973-06-25