Abstract
Mesalazine microgranules are an ethylcellulose-coated formulation from which mesalazine is released throughout the intestinal tract and are expected to be effective for idiopathic inflammatory bowel disease, ulcerative colitis and Crohn's disease. Mesalazine microgranules were administered orally to investigate the distribution of mesalazine throughout the intestinal tract in rats. Mesalazine microgranules distributed sufficient amounts of mesalazine and its metabolite, N-acetyl-mesalazine, to the intestinal tissues, while pure mesalazine delivered lower amounts of both. In acetic acid-induced colitis in rats, mesalazine microgranules administered orally reduced the damage score significantly (P<0.05) at a dose of 50 mg/kg as assessed by macroscopic observation and at 100 mg/kg as assessed by histological evaluation. The number of ulcers in carrageenan-induced colitis in guinea pigs was inhibited at doses of 50, 100, 200 mg/kg, p.o. The colonic wet weight of rats in 2, 4, 6-trinitrobenzenesulfonic acid (TNB)-induced colitis was reduced significantly (P<0.05) at a dose of 50 mg/kg, p.o. Mesalazine microgranules showed the ability to distribute mesalazine efficiently throughout the intestinal tract and showed effectiveness against acetic acid-, carrageenan- and TNB-induced colitis. These studies strongly suggest that mesalazine microgranules are effective for idiopathic inflammatory bowel disease.
