Composition for ph dependent controlled release of active...

A - Human Necessities – 61 – K

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Details

A61K 47/36 (2006.01) A61K 9/20 (2006.01) A61K 9/22 (2006.01) C08B 31/04 (2006.01)

Patent

CA 2222372

The present invention is related to a composition for pH dependent or pH regulated controlled release of active ingredients especially drugs. The composition consists of a compactible mixture of the active ingredient and starch molecules substituted with acetate and dicarboxylate residues. The preferred dicarboxylate acid is succinate. The average substitution degree of the acetate residue is at least 1 and 0.2 - 1.2 for the dicarboxylate residue. The starch molecules can have the acetate and dicarboxylate residues attached to the same starch molecule backbone or attached to separate starch molecule backbones. The present invention also discloses methods for preparing said starch acetate dicarboxylates by transesterification or mixing of starch acetates and starch dicarboxylates respectively.

La présente invention concerne une composition pour la libération contrôlée de constituants actifs, en particulier de médicaments, en fonction du pH ou réglée par le pH. Cette composition consiste en un mélange comprimable du constituant actif et de molécules d'amidon substituées avec des résidus d'acétate et de dicarboxylate. Le dicarboxylate préférentiel est un succinate. Le taux de substitution moyen du résidu d'acétate est d'au moins 1, et de 0,2 à 1,2 pour le résidu de dicarboxylate. Les résidus d'acétate et de dicarboxylate peuvent être fixés à la même ossature des molécules d'amidon ou à des ossatures différentes. La présente invention concerne aussi des procédés de préparation des dicarboxylates et acétates d'amidon mentionnés, à savoir par transestérification ou mélange d'acétates et de dicarboxylates d'amidon.

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