Controlled release formulation for water soluble drugs

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/58 (2006.01) A61K 9/50 (2006.01) A61K 9/60 (2006.01) A61K 9/62 (2006.01) A61K 31/554 (2006.01)

Patent

CA 2349696

A once-a-day controlled release diltiazem formulation comprises: (a) 20-50 wt.% of enteric polymeric membrane coated pellets comprising a polymer membrane coated core which comprises a biologically inert core which is coated with a first layer consisting essentially of diltiazem and polymeric binder; and a second layer which comprises a membrane comprising a pH dependent polymeric material; and (b) 50-80 wt.% of delayed pulse polymeric membrane coated pellets comprising a polymeric membrane coated core comprising a biologically inert core which is coated with a first layer which consists essentially of diltaziem and a polymeric binder and a second layer which comprises a polymeric membrane and an alkaline earth metal stearate which will substantially maintain its integrity in the varying pH conditions of the gastrointestinal tract but is permeable to diltiazem, and (c) a unit dose containment system.

L'invention concerne une formulation de diltiazem à libération régulée, à monodose quotidienne. Cette formulation comprend : (a) 20-50 % en poids de granules enrobées d'une membrane polymère entérique, formées d'un noyau enrobé d'une membrane polymère et comprenant un noyau biologiquement inerte enrobé d'une première couche composée principalement de diltiazem et d'un liant polymère, et d'une seconde couche formée d'une membrane comprenant un matériau polymère dépendant du pH, et (b) 50-80 % en poids de granules enrobées d'une membrane polymère à pulse différé, formées d'un noyau enrobé d'une membrane polymère et comprenant un noyau biologiquement inerte enrobé d'une première couche composée principalement de diltiazem et d'un liant polymère et d'une seconde couche constituée d'une membrane polymère et d'un stéarate de métal terreux alcalin qui conserve sensiblement son intégrité dans les conditions de pH variées régnant dans le tractus gastro-intestinal mais est perméable au diltiazem, et (c) un système de conditionnement pour une dose unitaire.

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