Abstract
Synthesis and kinetic studies of mutual azo prodrugs of 5-aminosalicylic acid with sulfamethoxazole and trimethoprim as models for colon targeting
Highlights
In this study, two mutual azo prodrugs were synthesized for colon targeting in a treatment of colonic diverticular disease
٥-ASA is very effective in diverticulitis but it is absorbed mainly in the upper gastrointestinal tract that it usually fails to reach the colon leading to significant adverse effects
In the first mutual prodrug, the hydrolysis of azo linkage leads to release of the sulfamethoxazole and ٥-ASA
Summary
Two mutual azo prodrugs were synthesized for colon targeting in a treatment of colonic diverticular disease. In vitro kinetic studies of these mutual prodrugs in hydrochloric acid buffer (pH ١.٢) and in phosphate buffer (pH ٧.٤) were monitored. Hydrolysis of these mutual prodrugs was established in rat fecal matter. The release of ٥-aminosalicylic acid and sulfamethoxazole or trimethoprim from these mutual prodrugs was almost complete and it followed first order kinetics. D iverticulitis of colon is quite frequent in developed countries and its prevalence rises with age.[١] Perforated colonic diverticular disease is a condition associated with high mortality and morbidity. ٢٠١٠ Mosul College of Pharmacy causative bacteria.٧ ٥-aminosalicylic acid (٥ASA) is among the oldest anti-inflammatory agents in use today for the treatment of inflammatory bowel diseases.[٨]
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