A double‐blind dose‐escalating trial comparing novel mesalazine pellets with mesalazine tablets in active ulcerative colitis

Abstract

SUMMARYBackground: Mesalazine as the treatment standard for ulcerative colitis can be applied in different galenical preparations. Aim: A novel formulation of mesalazine pellets with delayed and prolonged release characteristics was compared with conventional Eudragit L-coated tablets. Furthermore, the effect of mesalazine dose escalation on nonresponders was evaluated in both treatment groups. Methods: A total of 233 patients with mild to moderately active ulcerative colitis were randomized to receive either mesalazine (1.5 g/day in three doses) as pellets

Once-daily mesalamine granules for ulcerative colitis

“…The safety profile of mesalamine extended-release capsules and MG is shown in Table 2 [21][22][23][24][25]. The adverse events noted are similar to previous trials with other mesalamine compounds, and the occurrence of adverse events is equally broad; they occur in 31-60% of patients on MG.…”

“…Marakhouski et al randomized 233 patients with mild-tomoderately active UC to mesalamine (0.5 g three-times daily) as either granules or tablets (both coated in Eudragit-L ® ), with dose escalation to 1 g three-times daily if there was an insufficient response [22]. At 3 weeks, the remission rates were similar between the two groups (47% in the granule group and 42% in the tablet group).…”

“…[34] Induce remission [22] Kruis et al Once-daily mesalamine granules for ulcerative colitis Drug Profile in clinical remission for at least 1 month, but with at least one flare within the previous 12 months. In total, 562 patients were included in the two trials, and were randomized to mesalamine extendedrelease capsules 1.5 g once daily (four capsules) or placebo in a 2:1 ratio -373 enrolled in the mesalamine extended-release capsules group and 189 in the placebo group.…”

“…Mesalamine dose 1.5 g daily [24,25] 3 g daily [23] 1.5-4.5 g daily [21] 1.5 g daily [22] Number Once-daily mesalamine granules for ulcerative colitis Drug Profile extended-release capsules), to those that release it at a pH of 7 or more (Asacol and Lialda). A recent study that compared a mesalamine formulation released early in the intestinal tract (Pentasa) to a pH-dependent release form (Asacol) reported that only the pH-dependent form was superior to placebo in patients with proctitis [33].…”

Multiparticulate systems containing 5-aminosalicylic acid for the treatment of inflammatory bowel disease

“…Olsalazine comprises two molecules of 5-ASA linked by an azo-bond as a dimer, and balsalazide consists of 5-ASA linked by an azo-bond to inert carrier 4-aminobenzoyl-β-alanine 36,38,41 . Due to the azo linkage, the compounds pass unchanged through the small intestine and undergo their metabolism by the bacterial azoreductase enzymes when they reach the colon releasing 5-ASA 42,43 . Prodrugs are available either in a form of tablet or gelatine capsule and are listed in Table 2.…”