Microparticles with modified release of at least one active...

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/50 (2006.01) A61K 9/20 (2006.01) A61K 9/48 (2006.01) A61K 31/155 (2006.01) A61K 31/522 (2006.01)

Patent

CA 2624372

The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel multimicroparticulate galenic system operating in accordance with a dual time-dependent and pH-dependent release mechanism, which enables the following three parameters to be adjusted independently of one another: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGIT® L100-55) and a hydrophobic compound (B2) (LUBRITAB®).The invention also concerns medicines based on said microparticules.

Le domaine de la présente invention est celui des systèmes microparticulaires à libération modifiée, de principe(s) actifs) (PA) oraux. Le but de l'invention est de fournir un nouveau système galénique multimicroparticulaire fonctionnant selon un double mécanisme de libération "temps dépendant" et "pH dépendant", qui permette d'ajuster indépendamment les uns des autres les trois paramètres suivants : a) le temps de latence précédant la libération du PA dans l'estomac ; b) le pH de déclenchement de la libération du PA dans l'intestin ; c) la vitesse de libération du PA. L'invention atteint ce but grâce aux microparticules enrobées faites de particules de PA recouvertes chacune de 2 pellicules d'enrobage A & B. A comprend : (co)polymère filmogène (A1) insoluble dans les liquides du tractus gastro-intestinal -éthylcellulose- / (co)polymère (A2) soluble dans les liquides du tractus gastro-intestinal - Polyvinylpyrrolidone- / plastifiant (A3)- huile de ricin- / éventuellement un agent tensio-actif et/ou lubrifiant (A4)-stéarate de magnésium. B comprend un polymère (B1) hydrophile porteur de groupements ionisés à pH neutre (EUDRAGIT~ L100-55) et un composé hydrophobe (B2) (LUBRITAB~). L'invention concerne les médicaments à base de ces microparticules.

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