Morphine sulphate microgranules, method for preparing same...

A - Human Necessities – 61 – K

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A61K 31/485 (2006.01) A61K 9/50 (2006.01) A61K 9/52 (2006.01) A61P 25/04 (2006.01)

Patent

CA 2376339

The invention concerns a novel oral formulation with prolonged release of morphine sulphate in the form of microgranules. Each microgranule comprises a neutral support coated with an active layer and a prolonged release layer. The invention is characterised in that the prolonged release layer contains a methacrylic acid and methacrylate methyl ester copolymer whereof the relative proportion of carboxyl groups and ester groups is equal to about 0.5, and a silica exhibiting hydrophobic property. The invention also concerns a method for preparing said microgranules carried out entirely in an aqueous medium by producing neutral support grains.

La présente invention concerne une nouvelle formulation orale à libération prolongée de sulfate de morphine sous forme de microgranules. Chaque microgranule comprend un grain support neutre enrobé d'une couche active et d'une couche à libération prolongée, caractérisés en ce que la couche à libération prolongée contient un copolymère d'acide méthacrylique et d'ester méthyl méthacrylate dont la proportion relative des groupes carboxyles libres et des groupes esters est égale à 0,5 environ, et une silice présentant un caractère hydrophobe. La présente invention concerne également un procédé de préparation de ces microgranules entièrement réalisé en milieu aqueux par montages des grains supports neutres.

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