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.