Solid composition for controlled release of ionizable active...

A - Human Necessities – 61 – K

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A61K 9/20 (2006.01) A61K 31/19 (2006.01) A61K 31/192 (2006.01) A61K 31/405 (2006.01) A61K 31/517 (2006.01) A61P 7/02 (2006.01) A61P 9/00 (2006.01)

Patent

CA 2743639

A novel solid composition and methods for making and using the solid composition are provided. The solid composition comprises: (a) at least one active agent with a solubility of less than about 0.3 mg/ml in an aqueous solution with a pH of at most about 6.8 at a temperature of about 37°C; and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCEL.TM., POLYOX.TM. WSR 1105 and combinations thereof; and optionally ii) a hydrophobic polymer selected from the group consisting of Ethocel 20 premium; and (c) an alkalizer selected from the group consisting of calcium carbonate, magnesium oxide heavy and sodium bicarbonate; wherein the composition provides at least about 70% release of the active between about 7 to about 12 hours following oral administration.

La présente invention concerne une nouvelle composition solide et des procédés de fabrication et d'utilisation de celle-ci. Cette composition comprend : (a) au moins un agent actif avec une solubilité inférieure à environ 0,3 mg/ml dans une solution aqueuse dont le pH vaut au plus à peu près 6,8 à une température d'environ 37 °C; (b) une composition de matrice polymère hydrophile comprenant i) un polymère hydrophile choisi dans le groupe constitué par le METHOCELTM, le POLYOXTM WSR 1105 et les combinaisons de ceux-ci, et éventuellement ii) un polymère hydrophobe, lEthocel 20 Premium; et (c) un agent alcalinisant choisi dans le groupe constitué par le carbonate de calcium, l'oxyde de magnésium et le bicarbonate de sodium. La composition permet une libération d'au moins 70 % environ du principe actif entre environ 7 et environ 12 heures après administration orale.

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