Pharmaceutically acceptable solubilizing composition and...

A - Human Necessities – 61 – K

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A61K 9/20 (2006.01) A61K 9/14 (2006.01) A61K 31/427 (2006.01) A61K 31/513 (2006.01) A61K 47/14 (2006.01) A61K 47/22 (2006.01)

Patent

CA 2658395

A pharmaceutically acceptable solubilizing composition comprising (i) at least one tocopheryl compound having a polyalkylene glycol moiety and (ii) at least one alkylene glycol fatty acid monoester or mixture of alkylene glycol fatty acid mono- and diester is disclosed. The solubilizing composition is useful in the manufacture of a pharmaceutical dosage form which comprises a melt-processed mixture of at least one active ingredient, at least one pharmaceutically acceptable polymer. The active ingredient(s) may be inhibitors of HIV protease. The solubilizing composition enhances the bioavailability of the active ingredient after oral intake.

La présente invention porte sur une composition solubilisante de qualité pharmaceutique qui comprend (i) au moins un tocophéryle portant une fonction polyalkylène glycol et (ii) au moins un monoester d'acide gras avec un alkylène glycol ou un mélange de mono- et de diester d'acide gras avec un alkylène glycol. La composition solubilisante peut être employée dans la fabrication d'une forme galénique qui comprend un mélange transformé à l'état fondu d'au moins un principe actif et d'au moins un polymère de qualité pharmaceutique. Le ou les principes actifs peuvent être des inhibiteurs de la protéase du VIH. La composition solubilisante augmente la biodisponibilité du principe actif après absorption orale.

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