Mesalamine

Background. Use of sulphasalazine in ulcerative colitis patients is hampered by a variety of side-effects, including male infertility. 5-aminosalicylic acid is better tolerated and has been increasingly used to treat patients intolerant/allergic to sulphasalazine but it may also be associated with side-effects.Aim. To evaluate tolerance of long-term treatment with sulphasalazine and 5-aminosalicylic acid in ulcerative colitis.Methods. Side-effects to sulphasalazine (2–3

Recently, there has been concern by regulatory authorities of the risk of alcohol-induced dose dumping of oral modified release (MR) formulations. The aim of this work was to use in vitro dissolution methodology to investigate the vulnerability of MR products to alcohol under different physiological conditions of the upper gastrointestinal tract. A variety of dissolution scenarios with ethanol concentrations in the range of 5-40% v/v were explored. Mesalazine (5-aminosalicylic acid) was selected as the model drug and the release behaviour of three commercially available MR, monolithic and multi-particulate preparations with pH-dependent or independent release mechanisms was evaluated (Salofalk, Asacol and Pentasa). Each product was found to have a distinctive release profile and behaved differently in the scenarios screened. In the case of Pentasa, complete dose dumping occurred on exposure to 40% ethanol in acid for 2h. Asacol, however, displayed a contrarian trend with drug releas...

Microwave-initiated synthesis of polyacrylamide-grafted sodium alginate, a graft copolymer with wide variety of applications has been reported in this study. The effect of reaction parameters (i.e., irradiation time and monomer concentration) onto the percentage grafting has been investigated. The resulting polymer has been characterized by a variety of characterization techniques such as intrinsic viscosity measurement, Fourier transform infrared spectra, 13C NMR spectra, elemental analysis, thermogravimetric analysis, molecular weight determination using static light scattering analysis, and scanning electron micrographs. Further, the flocculation efficiency of this graft copolymer has been investigated in coal suspension. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2010

Background and aims Literature data about the outcome of segmental colitis associated with diverticulosis (SCAD) are scarce. Our aim was to assess the clinical outcome of SCAD according to the type of disease. Patients/methods Twenty-seven SCAD patients underwent a 5-year follow-up (13 males, 14 females; mean age, 63.71 years; range, 50–85 years). Eleven patients were affected by type A, eight by type B, four by type C and four by type D SCAD. During the follow-up, all type B, C, and D patients were under continuous medical treatment. Five type A patients refused any maintaining treatment, but accepted to undergo the clinical, endoscopic, and histological follow-up. Results/findings Five type A patients taking therapy (83.33%), two type A not taking therapy (50%), all type C patients (100%), five type B patients (62.5%) and none of type D (0%) were under continuous remission at the end of the follow-up. All type D patients required further steroid course to obtain remission, and two patients required azathioprine to maintain remission. Interpretations/conclusions SCAD B and D patients fail to maintain long-term remission, often requiring immunosuppressive treatment. SCAD A and C patients show a more benign course; however, long-term treatment guarantees longer remission also in those patients.

Background: Pentasa is a controlled-release tablet made from semipermeable microspheres and designed to continuously deliver therapeutic quantities of 5-ASA (5-aminosalicylic acid) throughout the gastrointestinal tract. Scintigraphic studies in healthy subjects have documented that 5-ASA release could occur in the small intestine. We tested here the disintegration of Pentasa in the digestive tract of nine patients with Crohn's disease of the small intestine.Materials: Each patient was given, after breakfast, a 250 mg tablet of Pentasa containing samarium-153 oxide. For 8 h the progression of the isotope in the gastrointestinal tract was followed using gamma camera scintigraphy. Plasma measurement of 5-ASA and acetylated 5-ASA was used to verify the liberation and absorption of 5-ASA.Results: The Pentasa tablet appeared completely dissolved in the stomach by 117 ± 18 min. Samarium oxide was first detected in the small intestine 60 ± 5 min after its ingestion; it reached the colon after 280 ± 13 min and it was completely absent from the small intestine at 360 ± 26 min. Plasma concentrations of 5-ASA started to rise after 67 ± 7 min and were maximal at 222±25 min.Conclusion: In patients with Crohn's disease of the small intestine, Pentasa microgranules start releasing 5-ASA in the proximal small intestine, acting locally to exert its beneficial effect.

An increased prevalence of elevated serum anti-Saccharomyces cerevisiae antibody (ASCA) levels in patients with Crohn's disease (CD) has been described. The aim of the present work was to investigate serum ASCA levels during the courses of prednisolone and mesalamine therapy in CD patients. Serum samples of 25 patients with active CD were studied for ASCA levels before as well as 2 and 9 wk after initiation of a prednisolone tapering regimen. The influence of mesalamine (4 g o.d.) on serum ASCA levels compared to that of placebo was tested over 1 yr in 38 patients (20 mesalamine and 18 placebo) participating in a postoperative prophylaxis study. Serum IgG and IgA ASCA levels were measured by ELISA. Sera of 91 CD and 40 ulcerative colitis (UC) patients as well as 334 healthy donors were tested for ASCA to recalculate new cut-off values. For IgG ASCA cut-off values were determined to be 17.0 U and 25.0 U, and for IgA ASCA 9.3 U and 14.0 U. At baseline visit, 73.0% (46/63) of patie...

Prognostic factors for postoperative recurrence of Crohn's disease (CD) have been widely investigated but not yet clearly identified. PURPOSE: Aim of this study was, therefore, to analyze the association between demographic, clinical, laboratory, and surgical characteristics of patients and the cumulative probability of endoscopic postoperative recurrence. METHODS: The study was performed in 110 patients who were enrolled in the Italian multicenter, randomized, controlled trial on the effectiveness of 5-aminosalicylic acid (5-ASA) in the prevention of postoperative recurrence in CD. Patients had undergone their first intestinal resection for CD of the terminal ileum with or without involvement of cecum ascending colon. Recurrence was defined on the basis of endoscopy. The following variables were evaluated as potential prognostic factors: gender, age, years since diagnosis, clinical course (perforative and nonperforative), Crohn's Disease Activity Index score, white blood count, erythrocyte sedimentation rate, C-reactive protein, and orosomucoids assessed before the operation. Timing of operation (elective or urgent), type of anastomosis (end-to-end, end-to-side, side-to-end, side-to-side), and prophylactic treatment were also evaluated. Colon ileoscopy was performed at 6, 12, 24, and 36 months after operation. The association between variables and the cumulative proportion of recurrence was analyzed both by univariate analysis (life table method, log-rank test) and multivariate regression analysis (Cox's model, stepwise procedure). RESULTS: Results of this study indicate that, of the features considered before surgery, only leukocytosis (white blood count, >9,000 ml) was significantly associated with an increased risk of recurrence (P <0.05) at univariate analysis. This finding was not confirmed by multivariate analysis. A trend toward a higher risk of recurrence for patients who have had a resection with end-to-end anastomosis compared with those who have had a resection and other types of anastomosis was also observed. This trend reached significancy in the group of patients submitted to treatment with 5-ASA. The multivariate analysis showed that 5-ASA-treated patients with end-to-end anastomosis had a risk of recurrence more than threefold higher than those with other types of anastomosis (relative risk, 3.40; 95 percent confidence interval, 1.00–11.96;P <0.03). CONCLUSIONS: From a practical point of view, it has been estimated that the combination of intestinal resection plus side-to-side or end-to-side anastomosis with oral 5-ASA treatment reduces by 64 percent the postoperative recurrence rate in CD at three years follow-up.