title: 5-aminosalicylic acid release from a new controlled-release mesalazine formulation during gastrointestinal transit in healthy volunteers.
abstract: BACKGROUND
  Mesalazine (5-aminosalicylic acid, 5-ASA) containing formulations represent a cornerstone in the treatment of inflammatory bowel diseases. A novel formulation with an Eudragit L/S mixture coating has been developed to provide selective release of 5-ASA to the ileo-caecal region and the colon.
  
  
  OBJECTIVE
  To determine the release of 5-ASA during the gastrointestinal transit.
  
  
  METHODS
  A single oral dose of mesalazine EC 500 mg gastroresistant tablets (Asamax) was administered to eight healthy male volunteers. Gastrointestinal transit and tablet disintegration were monitored by scintigraphy. 5-ASA release was verified by assessing plasma pharmacokinetics.
  
  
  RESULTS
  Initial tablet disintegration was observed 5.65 +/- 0.86 h after dosing, corresponding to the detection of 5-ASA in plasma. This occurred in the ileo-caecal region in three subjects and the ascending colon in the remaining five. The relative percentage of 5-ASA absorption was more pronounced in the ascending colon (41 +/- 27.4%) than the ileo-caecal region (6.6 +/- 9.2%).
  
  
  CONCLUSIONS
  This mesalazine EC gastroresistant tablets release locally active 5-ASA specifically in the ileo-caecal region and the ascending colon.
authors.affiliation: Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria. martin.brunner@meduniwien.ac.at
authors.forename: M
authors.initials: M
authors.lastname: Brunner
authors.forename: E
authors.initials: E
authors.lastname: Lackner
authors.forename: P S
authors.initials: PS
authors.lastname: Exler
authors.forename: H C
authors.initials: HC
authors.lastname: Fluiter
authors.forename: K
authors.initials: K
authors.lastname: Kletter
authors.forename: M
authors.initials: M
authors.lastname: Tschurlovits
authors.forename: R
authors.initials: R
authors.lastname: Dudczak
authors.forename: H-G
authors.initials: HG
authors.lastname: Eichler
authors.forename: M
authors.initials: M
authors.lastname: Müller
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000097:blood / Q000652:urine; D001682:Biological Availability; D003692:Delayed-Action Preparations; D041981:Gastrointestinal Tract / Q000737:chemistry* / Q000000981:diagnostic imaging; D005772:Gastrointestinal Transit / Q000502:physiology; D006801:Humans; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy; D008297:Male; D019804:Mesalamine / Q000008:administration & dosage* / Q000097:blood / Q000652:urine; D011877:Radionuclide Imaging; D013607:Tablets / Q000008:administration & dosage
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D013607:Tablets; D019804:Mesalamine