Title
Release of 5-aminosalicylate from an MMX mesalamine tablet during transit through a simulated gastrointestinal tract system
Author
Tenjarla, S.
Romasanta, V.
Zeijdner, E.
Villa, R.
Moro, L.
TNO Kwaliteit van Leven
Publication year
2007
Abstract
5-Aminosalicylate (5-ASA; mesalamine) is the current first-line treatment for mild to moderate ulcerative colitis, a chronic inflammatory condition that most commonly affects the distal part of the colon. MMX™ mesalamine (Lialda™ [US]; Mezavant™ XL [UK and Ireland]; Mezavant™ [elsewhere]; Shire Pharmaceuticals Inc., Wayne, Pa, under license from Giuliani SpA, Milan, Italy) was created to be a novel, once-daily 5-ASA formulation. MMX mesalamine in tablet form has a pH-dependent, gastroresistant coating and is designed to delay the release of 5-ASA during transit through the upper gastrointestinal tract; it consists of hydrophilic and lipophilic excipients that are designed to prolong the release of 5-ASA throughout the colon. The release kinetics of 5-ASA from an MMX mesalamine tablet were assessed with the use of a dynamic in vitro gastroin-testinal tract system (TNO GastroIntestinal Model) that simulates physiologic conditions in the adult human gastrointestinal tract under standardized fed and fasted conditions. This system incorporates removal of released drug via dialysis and automated sampling taken at various sections of the system. Less than 1 % of 5-ASA was found to be released from the tablet in the simulated stomach and small intestine (before introduction into the simulated colon). Most of the 5-ASA within each tablet was released in the simulated colon (fasted state conditions: 78.0%; fed state conditions: 68.5%). Substantial quantities were released during the 8- to 18-hour sampling period (49.6 mg/h [fasted] and 40.7 mg/h [fed]). In conclusion, with the use of an in vitro system, the investigators showed that 5-ASA release from an MMX mesalamine tablet was delayed until the tablet reached the simulated colon. Throughout the simulated colon, release of 5-ASA from an MMX mesalamine tablet was prolonged. ©2007 Health Communications Inc.
Subject
Biology
Biomedical Research
5-Aminosalicylate
Bioaccessibility
Gastrointestinal system
In vitro
Mesalamine
MultiMatrix System
Ulcerative colitis
mesalazine
mezavant
nonsteroid antiinflammatory agent
adult
article
controlled study
dialysis
drug clearance
drug coating
drug release
gastrointestinal transit
human
human experiment
in vitro study
normal human
tablet formulation
upper gastrointestinal tract
biological model
chemistry
delayed release formulation
gastrointestinal tract
kinetics
pH
pharmaceutics
Anti-Inflammatory Agents, Non-Steroidal
Delayed-Action Preparations
Gastrointestinal Tract
Hydrogen-Ion Concentration
Kinetics
Mesalamine
Models, Biological
Technology, Pharmaceutical
To reference this document use:
http://resolver.tudelft.nl/uuid:c0dcdc7b-5c60-48e6-80dd-81d4befef619
DOI
https://doi.org/10.1007/bf02849976
TNO identifier
240048
ISSN
0741-238X
Source
Advances in Therapy, 24 (4), 826-840
Document type
article