Multi-layered controlled-release methylphenidate pellet

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/50 (2006.01) A61K 9/20 (2006.01) A61K 9/28 (2006.01)

Patent

CA 2566497

The present invention relates to a type of controlled-release multi~layered methylphenidate pellet that does not need to be combined with another type of pellet. It allows the maintenance of therapeutic levels in the plasma during 12 hours with a single daily dose, avoiding repeated administrations throughout the day. The controlled-release multi-layered pellet is comprised of an inert core, a first layer that contains methylphenidate and an acid buffering system, a protective layer, a layer of ethylcellulose, that performs the function of controlling the extended release of most of the methylphenidate, and a second layer of methylphenidate, that is responsible for the immediate release of the aforesaid within one hour of administration. The weight ratio between the methylphenidate present in the first active layer and the ethylcellulose is between 1.40:1 and 1.90:1. The multi-layered pellet may possibly have an external coating to protect it from erosion during processing.

L'invention concerne un type de pastille de méthylphénidate multicouche à libération contrôlée ne nécessitant pas d'être associé à un autre type de pastille. Cette pastille permet de maintenir les niveaux thérapeutiques dans le plasma pendant 12 heures avec une dose quotidienne unique, ce qui permet d'éviter les administrations répétées au cours de la journée. La pastille multicouche selon l'invention est constituée : d'un noyau inerte ; d'une première couche contenant du méthylphénidate et un système de tampon acide ; d'une couche de protection ; d'une couche d'éthylcellulose destinée à contrôler la libération prolongée de la majeure partie du méthylphénidate ; et d'une deuxième couche de méthylphénidate, responsable de la libération immédiate de méthylphénidate, dans l'heure qui suit l'administration. Le rapport de poids entre le méthylphénidate présent dans la première couche active et l'éthylcellulose est compris entre 1,40:1 et 1,90:1. La pastille selon l'invention peut également comporter un revêtement externe destiné à la protéger de l'érosion pendant le traitement.

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