Abstract
4,4'-Diformamidodiphenylsulfone (DFD) was given to six human volunteers as a single 1600-mg p.o. dose. Maximum plasma levels were 2.9 ± 0.6 µg/ml at five to eight hours with a T½, of 24 to 36 hours. No difference was seen among plasma levels of total amine, free amine or 35S-sulfone, indicating all plasma drug consists of 4, 4'-diaminodiphenylsulfone. DFD is deformylated at a rapid rate. Loss of 14CO2 in expired air was 50% complete six to eight hours after 14C-formyl-DFD administration. Analysis of plasma after 14C-formyl-DFD administration demonstrated less than 10% of plasma drug to be formyl derivatives. Urinary excretion of total amine was 12.7 ± 2.3% of dose with 31 to 71% of urinary metabolites as free amine. The amount of drug deformylated agreed well with urinary excretion of total amine. Biliary excretion accounted for 13 to 25% of absorbed drug. DFD thus represents a way of administering 4,4'-diaminodiphenylsulfone, characterized by low oral absorption and low sustained plasma levels. Whether this conveys an advantage in terms of efficacy and lower toxicity can Only be evaluated in the field.
Footnotes
- Received January 17, 1972.
- Accepted April 4, 1972.
- © 1972, by The Williams & Wilkins Company
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