title: 5-ASA colonic mucosal concentrations resulting from different pharmaceutical formulations in ulcerative colitis.
abstract: OBJECTIVE
  To compare the mucosal concentrations of 5-aminosalicylic acid (5-ASA) resulting from different pharmaceutical formulations and analyse the influence of inflammation on the mucosal concentrations.
  
  
  METHODS
  The study included 130 inflammatory bowel disease (IBD) patients receiving 5-ASA as pH-dependent-release formulations (73 patients), time-dependent-release formulations (11 patients), or pro-drugs (18 patients). In addition, 28 patients were receiving topical treatment (2-4 g/d) with pH-dependent-release formulations. Endoscopic biopsies were obtained from the sigmoid region during the colonoscopy. The 5-ASA concentrations (ng/mg) were measured in tissue homogenates using high-pressure liquid chromatography with electrochemical detection. The t test and Mann-Whitney test, when appropriate, were used for statistical analysis.
  
  
  RESULTS
  Patients receiving pH-dependent-release formulations showed significantly higher mucosal concentrations of 5-ASA (51.75 ± 5.72 ng/mg) compared with patients receiving pro-drugs (33.35 ± 5.78 ng/mg, P = 0.01) or time-dependent-release formulations (38.24 ± 5.53 ng/mg, P = 0.04). Patients with endoscopic remission had significantly higher mucosal concentrations of 5-ASA than patients with active disease (60.14 ± 7.95 ng/mg vs 35.66 ± 5.68 ng/mg, P = 0.02). Similar results were obtained when we compared patients with the histological appearance of remission and patients with active histological inflammation (67.53 ± 9.22 ng/mg vs 35.53 ± 5.63 ng/mg, P < 0.001). Significantly higher mucosal concentrations of 5-ASA were detected in patients treated with both oral and topical treatments in combination compared with patients who received oral treatment with pH-dependent-release formulations alone (72.33 ± 11.23 ng/mg vs 51.75 ± 5.72 ng/mg, P = 0.03).
  
  
  CONCLUSIONS
  IBD patients showed significant variability in mucosal 5-ASA concentrations depending on the type of formulation, and the highest mean concentration was achieved using pH-dependent-release formulations.
authors.affiliation: Renata D'Incà, Martina Paccagnella, Romilda Cardin, Surajit Pathak, Giacomo Carlo Sturniolo, Department of Surgical, Oncological and Gastroenterological Sciences, University of Padua, 35127 Padova, Italy.
authors.forename: Renata
authors.initials: R
authors.lastname: D'Incà
authors.forename: Martina
authors.initials: M
authors.lastname: Paccagnella
authors.forename: Romilda
authors.initials: R
authors.lastname: Cardin
authors.forename: Surajit
authors.initials: S
authors.lastname: Pathak
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Baldo
authors.forename: Maria Cecilia
authors.initials: MC
authors.lastname: Giron
authors.forename: Giacomo Carlo
authors.initials: GC
authors.lastname: Sturniolo
mesh_terms: D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003093:Colitis, Ulcerative / Q000188:drug therapy*; D003106:Colon / Q000378:metabolism*; D003692:Delayed-Action Preparations; D005260:Female; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism*; D008297:Male; D019804:Mesalamine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008875:Middle Aged; D055815:Young Adult
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D019804:Mesalamine
keywords: 5-aminosalicylic acid; Inflammatory bowel diseases; Mucosal concentration
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