Prednisolone metasulphobenzoate preparation for the...

A - Human Necessities – 61 – K

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A61K 31/57 (2006.01) A61K 9/16 (2006.01) A61K 9/30 (2006.01) A61K 9/48 (2006.01)

Patent

CA 2229283

The dissolution at pH 6.5 of prednisolone metasulphobenzoate or a pharmacologically acceptable salt thereof from a non-disintegratable solid enteric composition comprising the prednisolone metasulphobenzoate in an excipient matrix is increased by the presence in the matrix of a rheological modifying agent, especially croscarmellose, in an amount of at least 5 percent by weight of the composition but insufficient to cause disintegration. Preferably the composition is in the form of pellets coated with an enteric coating which is substantially insoluble below pH 7 and contained in a capsule or tablet coated with an enteric coating which is soluble at a pH in the range pH 5.5 to pH 7. The coated capsules and tablets are for use in the treatment of inflammatory bowel disease, especially ulcerative colitis and Crohn's disease.

On améliore la dissolution, à un pH de 6,5, du prednisolone métasulphobenzoate ou d'un sel pharmacologiquement acceptable de ce dernier obtenu à partir d'une composition entérique solide ne se dissolvant pas comprenant le prednisolone métasulphobenzoate dans une matrice d'excipient, en incorporant dans la matrice un agent modifiant rhéologique, plus spécifiquement de la croscarmellose, en dose égale à au moins 5 pour cent en poids de la composition mais cependant insuffisante pour provoquer la dissolution. La composition se présente de préférence sous forme de granules enrobés d'un pelliculage gastro-résistant qui est sensiblement insoluble à un pH inférieur à 7 et contenu dans une capsule ou un comprimé enrobé d'un pelliculage gastro-résistant qui est soluble à un pH compris entre 5,5 et 7. Les capsules ou les comprimés enrobés sont destinés à être utilisés dans le traitement d'affections intestinales inflammatoires non spécifiques, notamment la rectocolite hémorragique et la maladie de Crohn.

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