Abstract
A pharmacokinetic profile for sulfisoxazole was defined following the intravenous administration of 2.0-g. single doses to seven human volunteers. The pharmacokinetic profile was determined utilizing a two-compartment open-system model and indicated the following physiological disposition characteristics. The drug distributes from the central compartment rapidly and exhibits a calculated volume of distribution ranging from 13 to 20% of body weight. The drug is eliminated from the body at a fairly rapid rate, with an apparent half-life range of 4.6–6.9hr. Sulfisoxazole is ultimately eliminated from the body solely by means of urinary excretion, with a mean of 54% of the dose excreted as “free” drug and the remainder as the N4-acetylated biotransformation product. Following intramuscular and oral administration of the drug, absorption was rapid and complete. Plasma levels peaked by 2hr. postadministration in most instances, with plasma level maxima ranging from 121 to 210 mcg./ml. The apparent half-lives of elimination of sulfisoxazole from the plasma following intramuscular and oral routes of administration ranged from 5.0 to 7.6hr. and from 4.6 to 7.8 hr., respectively.
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