Prevention of Loxoprofen-Induced Small Intestinal Mucosal Injuries by Irsogladine Maleate

Abstract

Background: Irsogladine maleate (IM) is a widely used antiulcer drug and protects the small bowel against nonsteroidal anti-inflammatory drug (NSAID)-induced injury in rats. However, the protective effect of IM against mucosal injury of the small intestine in humans has not been evaluated. Methods: This is a prospective, randomized, crossover pilot study of IM versus placebo, administered with NSAIDs in healthy volunteers. IM or placebo plus loxoprofen was administered with omeprazole for 14 days, and for an additional 14-day period with the treatments reversed in the same subjects, with a 4-week washout period between treatment courses. Before and after each administration period, all subjects underwent fecal calprotectin monitoring as well as capsule endoscopy (CE) to observe the degree of mucosal injury of the small intestine. Results: A total of 19 healthy volunteers (21–49 years) were evaluated. The mean number of red spots, reddened folds, and denuded areas per subject increased significantly (from 1.4±1.6 to 7.4±11.0, p<0.0001) in the placebo group, but not significantly in the IM group (from 1.3±1.4 to 2.9±3.0, p=0.059). Moreover, the mean number in the IM group at post-treatment was significantly less than that in the placebo group (p=0.038). However, the percentage of subjects with severe mucosal injuries including at least one mucosal break and/or ulcer after treatment was not significantly different between the placebo (47%) and IM (42%) groups. Conclusions: NSAID-induced small-intestinal mucosal injuries including red spots, reddened folds and denuded areas were suppressed by IM, but the incidence of severe mucosal injuries was not significantly different.