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Merck

Mesalamine delivery systems: do they really make much difference?

Advanced drug delivery reviews (2004-11-24)
Altamash I Qureshi, Russell D Cohen
ABSTRACT

Sulfasalazine's role as the first-line of therapy in patients with inflammatory bowel disease has led to the development of other "designer" aminosalicylates, which eliminate the sulfa-moiety, and attempt to target the topically active mesalamine to the inflamed bowel. Olsalazine sodium and balsalazide disodium utilize the same azo-bond structure as sulfasalazine, requiring release of active mesalamine by colonic bacteria, and thus targeting these agents to the colon. Other mesalamine delivery systems use pH-dependant- or moisture-release to liberate the active mesalamine in both the large and small bowel. Direct application of mesalamine via enema or suppository is also effective in patients with distal colitis. The pharmacology and thus the undesirable drug absorption rates differ between drugs, although the clinical importance of these characteristics is debatable. Differences in release-systems, the impact of the fed and fasting state, and unique patient intolerances to individual agents demand an understanding of each of these products, and their application to patient therapy.

MATERIALS
Product Number
Brand
Product Description

Mesalazine for system suitability, European Pharmacopoeia (EP) Reference Standard
Supelco
Mesalamine, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
5-Aminosalicylic acid, 95%
Sigma-Aldrich
5-Aminosalicylic acid, ≥99%
Mesalazine, European Pharmacopoeia (EP) Reference Standard