title: Dissolution of Commercially Available Mesalamine Formulations at Various pH Levels.
abstract: BACKGROUND
  Mesalamine (5-aminosalicylic acid; 5-ASA) is recommended first-line therapy for mild-to-moderate ulcerative colitis. Many mesalamine formulations employ a pH-dependent release mechanism designed to maximize drug release in the colon. This study compared the in vitro release of 5-ASA from six commercially available mesalamine formulations at pH levels similar to those typically encountered in the human gastrointestinal tract.
  
  
  METHODS
  The release of 5-ASA from six mesalamine formulations [Mesalazin-Kohlpharma (Kohlpharma, Germany), Mesalazin-Eurim (Eurimpharm, Germany), Mesalazina-Faes (Faes Farma, Spain), Mesalazine EC (Actavis B.V., Netherlands), Mesalazine EC 500 PCH (Pharmachemie B.V., Netherlands); multimatrix mesalamine (Shire US Inc., USA)] was monitored separately at three different pH levels [1.0 (2 h), 6.4 (1 h), and 7.2 (8 h)] using United States Pharmacopeia dissolution apparatus II. The dissolution percentage was calculated as a mean of 12 units for each formulation.
  
  
  RESULTS
  At pH 1.0 and 6.4, <1 % of 5-ASA release was observed for each of the mesalamine formulations tested. At pH 7.2, complete release of 5-ASA occurred within 1 h for Mesalazine EC and Mesalazine EC 500 PCH, and within 2 h for Mesalazin-Kohlpharma, Mesalazin-Eurim, and Mesalazina-Faes; complete release of 5-ASA from multimatrix mesalamine occurred within 7 h. Little variability in rate of 5-ASA dissolution was observed between tablets of each formulation.
  
  
  CONCLUSIONS
  At pH 7.2, 5-ASA release profiles were variable among the commercially available mesalamine formulations that were tested.
authors.affiliation: Shire, 725 Chesterbrook Blvd., Wayne, PA, 19087, USA, stenjarla@shire.com.
authors.forename: Srini
authors.initials: S
authors.lastname: Tenjarla
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D041981:Gastrointestinal Tract / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D019804:Mesalamine / Q000737:chemistry*; D012995:Solubility; D013607:Tablets / Q000737:chemistry
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D013607:Tablets; D019804:Mesalamine