Mesalazine vanishing time from rectal mucosa following its topical administration

J Crohns Colitis. 2010 Feb;4(1):102-5. doi: 10.1016/j.crohns.2009.08.003. Epub 2009 Oct 9.

Abstract

To investigate how long and how much Mesalazine (M) is available inside the rectal mucosa following its topical instillation, in patients (pts) with Ulcerative Colitis (UC). Two rectal biopsies for M concentration were obtained from 45 UC pts in clinical remission and on oral M treatment (OT), before a 4g enema randomly given to consentient pts every day (Group A, 15 pts), every 2 days (Group B, 15 pts) and every 3 days (Group C, 15 pts). Two additional biopsies were taken 1, 2 and 3 days after the last enema in group A, B and C respectively, at least 10 days later. All biopsies were immediately frozen at -80°C for later assay by means of high-performance light chromatography (HPLC). Data were analyzed using Student's t-test. Mean values±standard deviation of M mucosal concentration (ng/mg of tissue) were 1.32±1.41, 56.1±39.2, 9.65±6.60, and 6.39±5.03 in pts receiving OT alone, groups A, B and C, respectively. Values in Group A were statistically higher (p<0.001) than those in Groups B and C while no differences were found between Groups B and C. Values of OT were lower than groups A, B and C. M mucosal concentration rapidly decreases 2 days after a 4g enema, but after three days is still higher than OT alone. These results may provide data which would be useful to plan topical therapy and improve adherence to treatment.

MeSH terms

  • Administration, Oral
  • Administration, Rectal
  • Adult
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Biopsy
  • Colitis, Ulcerative / drug therapy*
  • Colitis, Ulcerative / pathology
  • Drug Administration Schedule
  • Enema
  • Female
  • Humans
  • Intestinal Mucosa / metabolism
  • Intestinal Mucosa / pathology
  • Male
  • Mesalamine / administration & dosage
  • Mesalamine / pharmacokinetics*
  • Proctoscopy
  • Rectum / metabolism
  • Rectum / pathology

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Mesalamine