Simulated comparison of topical and oral formulations of 5-aminosalicylate for the treatment of ulcerative colitis

Derrick J. Stobaugh, Parakkal Deepak, Matthew Thorpe, Bruce Hannon, Eli D. Ehrenpreis

Research output: Contribution to journalArticlepeer-review

4 Scopus citations


Background: 5-Aminosalicylate (5-ASA) formulations are approved for the treatment of ulcerative colitis (UC). Determination of the colonic pharmacokinetics of 5-ASA is challenging. A dynamic model of 5-ASA colonic amounts after oral delayed-release 5-ASA (Asacol), oral extended delayed-release 5-ASA (Lialda), 5-ASA enema (Rowasa), foam and suppositories (Canasa) was developed to determine the colonic kinetics of these agents. Methods: We created a model with Stella software. Colonic 5-ASA in the right, transverse, descending, sigmoid colon, and rectum were estimated for adults after recommended doses of the above formulations. Simulations of active mild/moderate UC and in remission were performed and compared using Student's t-test for differences in means. Results: For UC in remission, the highest amounts of 5-ASA were from Asacol in the right and transverse colon (P , 0.01), Lialda in the descending and sigmoid colon (P , 0.01), and Rowasa in the rectum (P , 0.01). For active UC, sigmoid amounts were highest with foam (P , 0.01), and rectal amounts highest with Rowasa (P , 0.01). Differences in rectosigmoid amounts of 5-ASA from enemas and suppositories for UC in remission occurred based on the relationship between the timing of administration relative to the daily bowel movement (P , 0.01). Conclusions: Compared to Asacol, Lialda results in higher 5-ASA amounts in the left colon. Asacol with Rowasa provides highest 5-ASA amounts across the entire colon. Higher 5-ASA amounts from topical formulations occur when the insertion occurs soon after the daily bowel movement. This model provides a rationale for further investigation.

Original languageEnglish
Pages (from-to)301-308
Number of pages8
JournalInflammatory bowel diseases
Issue number2
StatePublished - Feb 2013


  • Colitis
  • Mesalamine
  • Models
  • Theoretical
  • Therapeutics
  • Ulcerative


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