Studies on the Metabolism of Sulfadiazine. II. Quantitative Separation of Excrements in the Human Urine after Administration of Sulfadiazine

Abstract

Excretion of sulfadiazine, N⁴-acetylsulfadiazine, sulfadiazine-N⁴-glucuronide, sulfadiazine-N⁴-sulfonate, and sulfanilamide into human urine was separately determined by paper chromatography by the following method. One tenth ml. of urine obtained after oral administration of sulfadiazine was spotted lineary on a filter paper (Toyo Roshi No.51 40×40 cm.) and developed ascendingly with a solvent system of butanol saturated with water and a solvent of BuOH-AcOh-H₂O(5 : 1 : 4) for about 20 hours. The paper was dried in air, portions corresponding to the products were cut out, and eluted descendingly with N/4 ammonium hydroxide. Each of these metabolites was hydrolyzed with hydrochloric acid and determined by the colorimetric method using the Ehrlich's reagent as sulfadiazine. The content was calculated from a calibration curve prepared beforehand. The amount excreted 48 hours after oral administration of 2 g. of sulfadiazine was 1620 mg., calculated as sulfadiazine, including 862 mg. of sulfadiazine, 730 mg.of N⁴-acetylsulfadiazine, 11 mg. of sulfadiazine-N⁴-glucuronide, 14 mg. of sulfadiazine-N⁴-sulfonate, and 5 mg. of sulfanilamide, calculated as sulfadiazine respectively.