Colon-targeted celecoxib ameliorates TNBS-induced rat colitis: A potential pharmacologic mechanism and therapeutic advantages

234In the small intestine, orally administered SA1C, colon-targeted celecoxib, is not absorbed and (bio)chemically stable, leading to delivery of large fraction of SA1C to the large intestine. In the large intestine, SA1C is metabolized by microbial enzyme(s), liberating celecoxib and carriers (succinic acid and aspartic acid). Therefore, compared with conventional celecoxib that is absorbed mostly in the small intestine, colon-targeted celecoxib can increase the colonic concentration of celecoxib and reduce systemic side effects of celecoxib, likely improving therapeutic properties of the COX-2 inhibitor.