NEW DOSAGE FORMS FOR THE DELAYED RELEASE OF MESALAZINE TO THE COLON

  • ANGELIKI SIAMIDI Section of Pharmaceutical Technology, School of Health Sciences, National and Kapodistrian University of Athens, Zografou 15784, Athens, Greece
  • MARILENA VLACHOU Section of Pharmaceutical Technology, School of Health Sciences, National and Kapodistrian University of Athens, Zografou 15784, Athens, Greece
  • MANUEL EFENTAKIS Section of Pharmaceutical Technology, School of Health Sciences, National and Kapodistrian University of Athens, Zografou 15784, Athens, Greece

Abstract

Objective: The aim of the present work was to develop new solid pharmaceutical delivery systems of mesalazine (5-aminosalicylic acid, 5-ASA) for its colon targeted release.


Methods: Four different types of tablets of the same consistency (matrix and three-layered, with 5-ASA and dextran or pectin as excipients) were placed in a hard gelatin capsule. The 5-ASA release behavior from these formulations was compared to the release of the commercially available Asalazin® in three pH aqueous media in the presence of enzymes.


Results: The produced tablet formulations conformed to the Pharmacopoeia standards. The results showed delayed-release (<10%) during the first two hours, in acidic media (pH 1.5), and modified-release thereafter (pH 6 and 7.4). When dextran was used, the drug release showed more extended-release characteristics, in comparison to pectin formulations, due to the formation of a thicker hydrogel.


Conclusion: The new dosage forms could serve as a per os administration alternative dosage form for the delayed release of mesalazine to the colon

Keywords: Mesalazine, Delayed release, Pectin, Dextran, Tablets-in-capsule, Pectinex® Ultra SPL

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SIAMIDI, A., VLACHOU, M., & EFENTAKIS, M. (2020). NEW DOSAGE FORMS FOR THE DELAYED RELEASE OF MESALAZINE TO THE COLON. International Journal of Applied Pharmaceutics, 12(4), 192-196. https://doi.org/10.22159/ijap.2020v12i4.37816
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