スルフイソキサゾールの体内変化に関する研究 (第2報)

Sulfisoxazole N-Glucuronideについて

抄録

Examinations were made on the formation of sulfisoxazole N-glucuronide, one of the biological metabolites of sulfisoxazole. The increased excretion of N-glucuronide into the urine after oral administration of sulfisoxazole and further increase in the N-glucuronide by the combined use of glucuronolactone were observed. Formation of sulfisoxazole N-glucuronide was recognized in the aqueous solution, blood, and urine when allowed to stand at 37° for 8 hours after addition of sulfisoxazole and glucuronic acid. It was also found that addition of sulfisoxazole to normal urine and allowing this to stand at 37° for 8 hours resulted in increased formation of the N-glucuronide and this was accompanied with the corresponding decrease of approximately equal amount of free glucuronic acid. From these results, it is pointed out that bioformation of sulfisoxazole N-glucuronide is non-enzymatic as well as being enzymatic, and the effect of (administered) glucuronolactone on detoxication of sulfisoxazole is chiefly acceleration of N-glucuronide-type detoxication process.