Abstract
This report concerns the absorption and excretion of sulfanilamidopyridine (2-para-aminobenzene sulfonamidopyridine) in 2 normal adult humans, following the oral administration of a single dose of the drug. Such data are of immediate interest since experimental studies, 1 , 2 and preliminary clinical reports 3 , 4 , 5 indicate that sulfanilamidopyridine may be useful in the treatment of pneumococcus infections.
Each subject ingested 2 g of sulfanilamidopyridine suspended in 400 cc quantities of water. Blood samples were obtained 1, 2, 4, 8, 12, and 24 hours after ingestion of the drug; urine was collected quantitatively at the same intervals, and in one subject at the end of 32 hours. Both subjects took the drug one hour after breakfast and followed a normal routine of working, eating and sleeping.
Free and total sulfanilamidopyridine concentrations in blood and urine were determined colorimetrically according to Marshall's method 6 for estimation of sulfanilamide. Since sulfanilamide standards were used for comparison, the results were obtained in terms of sulfanilamide equivalents. These were converted to sulfanilamidopyridine concentrations by multiplying by the factors 1.25 in the free and 1.5 in the total sulfanilamidopyridine determinations.
As the data in Table I show, the maximum concentrations of sulfanilamidopyridine in the blood, 2.7 and 2.9 mg %, were found 4 hours after the drug had been ingested. These concentrations fell rather slowly and at the end of 12 hours were 1.5 and 2.1 mg %. The relative proportions of free and conjugated sulfanilamidopyridine changed considerably during this interval. At 4 hours the conjugated drug was 10 and 22% of the total; at 12 hours this fraction amounted to 39 and 60%.
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