Controlled release formulation for water soluble drugs in...

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/22 (2006.01) A61K 9/00 (2006.01) A61K 9/24 (2006.01) A61K 9/30 (2006.01)

Patent

CA 2217226

A controlled release pharmaceutical tablet is disclosed which is based on: (a) a compressed core which contains: i) a medicament; ii) from 5 to 20 % by weight of a water soluble osmotic agent based on the total weight of the compressed core; iii) a water soluble pharmaceutically acceptable polymeric binder; iv) a conventional pharmaceutical excipient; and (b) a dual layer membrane coating around said core which consists essentially of: i) a first inner coating layer for sustained release of the medicament, said inner coating layer consisting essentially of a plasticized water insoluble pharmaceutically acceptable polymer and a pharmaceutically acceptable water soluble polymer, and; ii) a second outer coating layer for immediate release of a medicament, said outer coating layer consisting essentially of an effective amount of a medicament and a water soluble polymer. The controlled release formulation is suitable for the once-a-day administration of medicaments.

La présente invention décrit une pastille pharmaceutique à libération lente, comprenant les éléments suivants: (a) un noyau comprimé contenant: i) un médicament; ii) de 5 à 20 % en poids d'un agent osmotique soluble dans l'eau, ce pourcentage étant basé sur le poids total du noyau comprimé; iii) un liant polymère pharmaceutiquement acceptable et soluble dans l'eau; iv) un excipient pharmaceutique classique; et (b) un revêtement constitué d'une membrane à double épaisseur autour du noyau, ce revêtement se composant essentiellement des éléments suivants: i) une première couche de revêtement intérieure permettant de libérer en continu le médicament, ladite couche se composant essentiellement d'un polymère pharmaceutiquement acceptable, plastifié et insoluble dans l'eau et d'un polymère pharmaceutiquement acceptable et soluble dans l'eau; et ii) une deuxième couche de revêtement extérieure permettant de libérer immédiatement le médicament, ladite couche se composant essentiellement d'une quantité efficace d'un médicament et d'un polymère soluble dans l'eau. Cette formulation à libération lente convient à tout médicament devant être administré une fois par jour.

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