Delivery and fate of oral mesalamine microgranules within the human small intestine☆
References (51)
- et al.
Oral mesalamine (Pentasa) as maintenance treatment in Crohn's disease: a multicenter placebo-controlled study
Gastroenterology
(1993) - et al.
Mesalamine capsules for the treatment of active Crohn's disease: results of a 16-week trial
Gastroenterology
(1993) - et al.
5-aminosalicylic acid in a slow-release preparation: bioavailabitity, plasma level and excretion in humans
Gastroenterology
(1982) - et al.
Colonic N-acetylation of 5-aminosalicylic acid in inflammatory bowel disease
Gastroenterology
(1989) - et al.
Simplified high-performance liquid chromatographic method for 5-aminosalicylic acid in plasma and urine
J Chromatogr
(1981) - et al.
Simultaneous measurements of total pancreatic, biliary, and gastric outputs in man using a perfusion technique
Gastroenterology
(1970) - et al.
Effects of decreasing intraluminal amylase activity on starch digestion and postprandial gastrointestinal function in humans
Gastroenterology
(1986) - et al.
Feedback regulation of human pancreatic secretion: effects of protease inhibition on duodenal delivery and small intestinal transit of pancreatic enzymes
Gastroenterology
(1990) - et al.
Comparison of delayed-release 5-aminosalicylic acid (5-ASA) and sulfasalazine as maintenance treatment for patients with ulcerative colitis
Gastroenterology
(1988) - et al.
5-aminosalicylic acid enema in the treatment of distal ulcerative colitis, proctosigmoiditis, and proctitis
Gastroenterology
(1987)
Randomised comparison of olsalazine and mesalazine in prevention of relapse in ulcerative colitis
Lancet
Human postprandial emptying of 1–3 mm spheres
Gastroenterology
Medical therapy of ulcerative colitis
Lancet
An experiment to determine the active therapeutic moiety of sulphasalazine
Lancet
Kinetics of 5-aminosaticylic acid after jejunal instillation in man
Br J Clin Pharmacol
Metabolism and urinary excretion of 5-aminosalicylic acid in healthy volunteers when given intravenously or released for absorption at different sites in the gastrointestinal tract
Gut
Disposition of 5-aminosalicylic acid by 5-aminosalicylic acid—delivering compounds
Scand J Gastroenterol
Coated oral 5-aminosalicylic acid versus placebo in maintaining remission of inactive Crohn's disease
Aliment Pharmacol Ther
Placebo-controlled trial of oral mesalamine in relapse prevention of Crohn's disease
Dig Dis Sci
A new slow-release form of 5-aminosalicylic acid for the oral treatment of inflammatory bowel disease
Pharmacokinetic properties of mesalazine (5-aminosalicylic acid)
Delayed-release mesalazine (5-aminosalicylic acid): coat dissolution and excretion in ileostoma subjects
Br J Clin Pharmacol
Topical and systemic availability of 5-aminosalicylate: comparisons of three controlled release preparations in man
Aliment Pharmacol Ther
Pharmacokinetic properties of 5-amino-salicylic acid (mesalazine)
Gastrointestinal transit of an enteric-coated delayed-release 5-aminosalicylic acid tablet
Aliment Pharmacol Therap
Cited by (77)
Mesalamine in the Initial Therapy of Ulcerative Colitis
2020, Gastroenterology Clinics of North AmericaCitation Excerpt :Pentasa contains mesalamine microgranules coated in a moisture-sensitive ethyl cellulose semipermeable membrane with release beginning in the duodenum and continuing throughout the GI tract.4 Therefore, 20% is released in the small bowel and the rest in the colonic epithelium; however, there may also be release in the stomach or proximal small bowel, depending on transit time.17 Balsalazide and olsalazine are prodrugs that require breakdown of enzyme-sensitive diazo bonds to produce active metabolites.
In vitro biorelevant models for evaluating modified release mesalamine products to forecast the effect of formulation and meal intake on drug release
2015, European Journal of Pharmaceutics and BiopharmaceuticsCitation Excerpt :The intake of a meal is known to alter the composition of the luminal gastrointestinal contents with regard to pH, buffer capacity, lipids, viscosity and osmolality [1–5]. In addition, the gastric emptying time of particles greater than approximately 2–7 mm, such as non-disintegrating monolithic dosage forms, can be greatly prolonged [4,6–10]. All of these factors can change the dissolution environment for solid oral dosage forms and may lead to an undesired change in the release rate.
Designing a biocompatible hydrogel for the delivery of mesalamine
2015, International Journal of PharmaceuticsCitation Excerpt :Numerous in vitro studies found that the beneficial effects of 5-ASA are related to its anti-inflammatory and anti-oxidant properties within the inflamed gut (Clemett and Markham, 2000). One major drawback of 5-ASA is its fast absorbance in the upper gastrointestinal tract, leading to a relatively small amount reaching the colon (Layer et al., 1995). Additionally, this treatment has gastrointestinal, hematological and general side effects.
Aminosalicylates
2011, Best Practice and Research: Clinical GastroenterologyPancreatic disorders in children with inflammatory bowel disease
2021, Medicina (Lithuania)
- ☆
Supported by Deutsche Forschungsgemeinschaft, grant La 483/5-2, Robert Bosch Foundations (Stuttgart, Germany), and Ferring GmbH (Kiel, Germany).