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

Authors

  • Derrick J. Stobaugh BA, BS,

    1. Gastroenterology Department, NorthShore University HealthSystem, Highland Park, Illinois
    2. Center for the Study of Complex Diseases, Research Institute, NorthShore University HealthSystem, Evanston, Illinois
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  • Parakkal Deepak MD,

    1. Gastroenterology Department, NorthShore University HealthSystem, Highland Park, Illinois
    2. Center for the Study of Complex Diseases, Research Institute, NorthShore University HealthSystem, Evanston, Illinois
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  • Matthew Thorpe BA,

    1. Division of Nutritional Sciences, University of Illinois, Urbana, Illinois
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  • Bruce Hannon PhD,

    1. Department of Geography/NCSA, University of Illinois, Urbana, Illinois
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  • Eli D. Ehrenpreis MD

    Corresponding author
    1. Gastroenterology Department, NorthShore University HealthSystem, Highland Park, Illinois
    2. Center for the Study of Complex Diseases, Research Institute, NorthShore University HealthSystem, Evanston, Illinois
    • Medical Director, Center for the Study of Complex Diseases, Research Institute, NorthShore University HealthSystem, Evanston, IL
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  • Supported by the Keyser Family Research Fund and the Center for the Study of Complex Diseases.

Abstract

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. (Inflamm Bowel Dis 2012)

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