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Calcium Alginate Beads as Core Carriers of 5-Aminosalicylic Acid

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Abstract

The utilization of calcium alginate beads as core carriers for delayed dissolution followed by burst release as a potential method of intestinal site specific drug delivery was investigated. 5-Aminosalicylic acid was spray-coated on dried calcium alginate beads and then coated with different percentages of enteric coating polymer and/or sustained-release polymer. Beads coated with more than 6% (w/w) methacrylic copolymer plastisized with dibutyl sebacate and triethyl citrate resisted release in 2-hr acid fluid challenge and allowed immediate dissolution upon transfer to simulated intestinal fluid. With 6% (w/w) methacrylic copolymer on top of 4% (w/w) ethylcellulose polymer, the major portion of drug did not release in 2 hr of acid treatment or the next 3 hr of simulated intestinal fluid treatment. This dosage form provides the possibility to deliver drug to the lower intestinal tract with minimal early release, followed by sustained release in the colon.

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Authors and Affiliations

  1. College of Pharmacy, Oregon State University, Corvallis, Oregon, 97331

    Shun Y. Lin & James W. Ayres

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  1. Shun Y. Lin
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  2. James W. Ayres
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Lin, S.Y., Ayres, J.W. Calcium Alginate Beads as Core Carriers of 5-Aminosalicylic Acid. Pharm Res 9, 1128–1131 (1992). https://doi.org/10.1023/A:1015887318767

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  • DOI: https://doi.org/10.1023/A:1015887318767

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