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Gastrointestinal transit and 5-ASA release from a new mesalazine extended-release formulation
M Brunner1, R Assandri, K Kletter
1Department of Clinical Pharmacology, University of Vienna Medical School, Austria. martin.brunner@univie.ac.at
Alimentary Pharmacology & Therapeutics
|February 4, 2003
Summary
A new mesalazine formulation ensures continuous release of 5-aminosalicylic acid (5-ASA) throughout the colon. This well-tolerated treatment is ideal for inflammatory bowel diseases affecting the distal colon.
Area of Science:
- Gastroenterology
- Pharmacology
Background:
- Mesalazine (5-aminosalicylic acid, 5-ASA) is crucial for inflammatory bowel disease (IBD) treatment.
- A novel formulation aims for selective, homogeneous 5-ASA release, improving upon traditional systems.
Purpose of the Study:
- To evaluate the gastrointestinal transit and release profile of a new mesalazine formulation.
- To assess the pharmacokinetics, urinary excretion, and safety of the new mesalazine formulation in healthy volunteers.
Main Methods:
- Gamma-scintigraphy tracked tablet transit after a single 1200 mg dose in 12 healthy males.
- Plasma pharmacokinetics verified 5-ASA release.
- A 7-day multiple-dose study assessed steady-state pharmacokinetics, urinary excretion, and safety with twice-daily dosing.
Main Results:
- Tablet erosion began in the colon (6.9 ± 1.1 h), with homogeneous radioactivity indicating sustained 5-ASA release.
- Initial 5-ASA absorption occurred in the small intestine and ileum.
- Mean Cmax was observed in the ileo-caecal region; 80.1 ± 18.2% of 5-ASA was absorbed in the colon.
Conclusions:
- The new mesalazine formulation was well-tolerated.
- Continuous 5-ASA release along the entire colon was confirmed.
- This formulation is a promising option for treating distal inflammatory bowel diseases.