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A novel dissolution method relevant to intestinal release behaviour and its application in the evaluation of modified

R C A Schellekens1, F E Stuurman, F H J van der Weert

  • 1Department of Clinical Pharmacy, University Medical Center Groningen, University of Groningen, The Netherlands. R.C.A.Schellekens@apoth.umcg.nl

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
|November 7, 2006
PubMed

Insights

Mesalazine (5-ASA) drug release profiles are crucial for inflammatory bowel disease (IBD) treatment efficacy. Biorelevant dissolution testing helps evaluate and compare 5-ASA products, guiding personalized patient therapy.

Area of Science:

  • Pharmacology
  • Gastroenterology
  • Drug Delivery Systems

Background:

  • Mesalazine (5-ASA) is a key therapeutic agent for inflammatory bowel disease (IBD).
  • The efficacy of 5-ASA relies on its local activity and targeted drug release at the inflammation site.
  • Variability in IBD inflammation location necessitates precise control over 5-ASA release profiles for optimal bioavailability and reduced systemic absorption, minimizing side effects.

Purpose of the Study:

  • To evaluate the dissolution profiles of various commercially available mesalazine (5-ASA) products under biorelevant conditions.
  • To assess the utility of a gastro-intestinal simulation system (GISS) in discriminating between different modified-release technologies for 5-ASA formulations.
  • To determine if current modified-release 5-ASA products achieve sufficient colon-selectivity and to explore potential improvements.

Main Methods:

  • Utilized a gastro-intestinal simulation system (GISS), based on pharmacopeial dissolution testing, to analyze drug release.
  • Tested several commercial 5-ASA products including Salofalk tablets and granules, Asacol tablets, and Pentasa tablets and granules.
  • Monitored the release profiles of these products to assess their performance under simulated physiological conditions.

Main Results:

  • All tested 5-ASA products demonstrated release profiles consistent with their intended modified-release technologies.
  • The gastro-intestinal simulation system (GISS) effectively differentiated between products employing various release mechanisms.
  • A minimal percentage of the total dose was released in the simulated colon for all evaluated products, suggesting room for improvement in colon-selectivity.

Conclusions:

  • The gastro-intestinal simulation system (GISS) is a robust tool for evaluating and comparing mesalazine (5-ASA) drug products based on their release characteristics.
  • Commercially available oral 5-ASA dosage forms exhibit diverse release profiles, indicating that patient-specific product selection may be necessary.
  • Further enhancements in colon-selectivity for modified-release 5-ASA products could potentially optimize therapeutic outcomes in inflammatory bowel disease management.

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