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Effects of Processing on the Release Profiles of Matrix Systems Containing 5-Aminosalicylic Acid

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Abstract

The aim of this study was to investigate the influence of different processing methods on the profiles of 5-aminosalicylic acid dissolution from controlled-release matrix systems based on Eudragit® RL and Eudragit® RS water-insoluble polymers. The pure polymers and their mixtures were studied as matrix formers using different processing methods, i.e., direct compression, wet granulation of the active ingredient with the addition of polymer(s) to the external phase, wet granulation with water, and wet granulation with aqueous dispersions. In comparison with the directly compressed tablets, tablets made by wet granulation with water demonstrated a 6–19% increase in final drug dissolution, whereas when polymers were applied in the external phase during compression, a 0–13% decrease was observed in the amount of drug released. Wet granulation with aqueous polymer dispersions delayed the release of the drug; this was especially marked (a 54–56% decrease in drug release) in compositions, which contained a high amount of Eudragit RL 30D. The release profiles were mostly described by the Korsmeyer–Peppas model or the Hopfenberg model.

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Abbreviations

E RS:

Eudragit® RS

E RL:

Eudragit® RL

5-ASA:

5-Aminosalicylic acid

E RL 30D:

Eudragit® RL 30D aqueous dispersion

E RS 30D:

Eudragit® RS 30D aqueous dispersion

DC:

Direct compression

S 12 :

Spreading coefficient

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ACKNOWLEDGMENTS

The Project named “TÁMOP-4.2.1/B-09/1/KONV-2010-0005—Creating the Center of Excellence at the University of Szeged” is supported by the European Union and co-financed by the European Social Fund.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, 6720, Szeged, Hungary

    Anita Korbely, András Kelemen, Péter Kása Jr & Klára Pintye-Hódi

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  1. Anita Korbely
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  2. András Kelemen
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  3. Péter Kása Jr
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  4. Klára Pintye-Hódi
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Correspondence to Klára Pintye-Hódi.

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Korbely, A., Kelemen, A., Kása, P. et al. Effects of Processing on the Release Profiles of Matrix Systems Containing 5-Aminosalicylic Acid. AAPS PharmSciTech 13, 1341–1347 (2012). https://doi.org/10.1208/s12249-012-9861-9

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