Extended release formulations of erythromycin derivatives

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/7048 (2006.01) A61K 9/20 (2006.01) A61K 9/22 (2006.01)

Patent

CA 2387621

Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically significantly lower Cmax in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.

L'invention concerne une composition pharmaceutique permettant d'obtenir une libération prolongée d'un dérivé d'érythromycine dans le milieu gastro-intestinal. La composition contient un dérivé d'érythromycine et un polymère pharmaceutiquement acceptable, de sorte qu'à l'ingestion, elle entraîne une C¿max? dans le plasma considérablement inférieure, d'un point de vue statistique, par rapport à une composition du dérivé d'érythromycine à libération immédiate, tout en permettant de maintenir une biodisponibilité et une concentration minimale sensiblement équivalentes à celles de la composition du dérivé d'érythromycine à libération immédiate en doses multiples. Les compositions de l'invention présentent un profil organoleptique amélioré et des effets secondaires gastro-intestinaux réduits par rapport à ceux de la composition à libération immédiate.

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