In the recent literature there are many reports of renal obstruction during therapy with sulfapyridine, sulfathiazole and sulfadiazine. This complication is attributed to the poor solubility of these drugs and their acetyl derivatives.1 It is important to realize that the sulfonamide compounds differ considerably in their solubility. Sulfanilamide, for example, is a relatively soluble drug, and renal complications are rare. Sulfapyridine, sulfathiazole, sulfadiazine and their acetyl forms, on the other hand, are relatively insoluble2 and renal complications occur frequently. If the solubility of these drugs in urine could be increased, this complication might be prevented. The data presented here will show that the solubility of sulfathiazole and sulfadiazine and their acetyl forms can be increased and renal precipitation thereby prevented.
The first procedure in our studies was to determine the solubility of sulfathiazole and sulfadiazine and their acetyl derivatives in normal human urine over the pH range
FOX CL, JENSEN OJ, MUDGE GH. THE PREVENTION OF RENAL OBSTRUCTION DURING SULFADIAZINE THERAPY. JAMA. 1943;121(14):1147–1150. doi:10.1001/jama.1943.02840140031006
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