Novel modified release formulation

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/16 (2006.01) A61K 9/20 (2006.01) A61K 9/22 (2006.01) A61K 9/52 (2006.01) A61K 47/00 (2006.01) A61P 1/04 (2006.01)

Patent

CA 2434542

The present invention is directed to a multiparticulate, modified release solid dispersion formulation, comprising a drug substance having a pH- dependent solubility, said drug substance being a compound of the formula I, or a pharmaceutically acceptable salt thereof; a hydrophobic matrix former which is a water-insoluble, non-swelling amphiphilic lipid; and a hydrophilic matrix former which is a meltable, water-soluble excipient; wherein the weight ratio hydrophobic matrix former/hydrophilic matrix former is >=1; and the particle size is less than 300 ~m. Also a unit dosage of the same, as well as a process for the preparation thereof and the use of the formulation and unit dosage is claimed.

L'invention concerne une préparation multiparticulaire de dispersion solide à libération modifiée comprenant une substance médicamenteuse dont la solubilité dépend du pH, cette substance étant un composé de formule I ou un sel acceptable sur le plan pharmaceutique de celui-ci; un agent hydrophobe de formation de matrice qui est un lipide insoluble dans l'eau, non gonflant et amphiphile; et un agent hydrophile de formation de matrice qui est un excipient fusible hydrosoluble; le rapport pondéral entre l'agent hydrophobe de formation de matrice et l'agent hydrophile de formation de matrice étant >=1; et la granulométrie étant inférieure à environ 300 µm. L'invention concerne également un dosage unitaire de celle-ci et un procédé de préparation et d'utilisation associé, ainsi qu'un dosage unitaire.

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