Modification of theophylline release with alginate gel formed in hard capsules

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Springer-Verlag

RESUMO

The aim of this work was to establish whether alginate gel formed spontaneously in hard gelatin capsules which modifies release of a model drug, theophylline. The effects of the alginate composition, the calcium addition, and the dissolution medium on drug release were also investigated. After the capsule shell dissolved in water, at neutral pH the gel layer of sodium alginate was formed immediately as the sodium alginate hydrated and swelled on contact with the aqueous medium. In acidic pH, the contents remained intact and the matrix shape was the same. Theophylline release from capsules containing different grades of alginate demonstrated different release patterns, depending on alginate composition and the pH of the medium. The capsules containing sodium/calcium salts of alginate showed the slowest drug release at neutral pH but the fastest in acidic medium. The presence of calcium acetate in the formulations influenced the drug release kinetics. The drug release in acidic medium showed a non-Fickian diffusion-controlled release, while those in water at neutral pH exhibited a Super Case II transport mechanism. The study also provides evidence that the behavior of alginate in forming the hydrated gel layer may explain the drug release behavior at different pHs.

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