Kit and composition of imidazole with enhanced bioavailability

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/4164 (2006.01) A61K 9/107 (2006.01) A61K 9/12 (2006.01) A61K 31/4174 (2006.01) A61K 31/496 (2006.01) A61K 31/52 (2006.01) A61K 31/522 (2006.01) A61K 33/00 (2006.01) A61K 38/00 (2006.01) A61K 47/36 (2006.01) A61K 47/38 (2006.01) A61M 37/00 (2006.01) A61M 11/00 (2006.01)

Patent

CA 2602042

A composition and therapeutic kit provide a therapeutic azole with increased solubility. The kit includes an aerosol packaging assembly containing a container accommodating a pressurized product and an outlet capable of releasing the pressurized product as a foam. The pressurized product includes a foamable composition including: i. a therapeutic azole, wherein the solubility of the azole in the composition before foaming is less than the solubility of the azole in the composition after foaming; ii. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, a co-solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight; iii. a surface-active agent; iv. about 0.01% to about 5% by weight of at least one polymeric additive selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent; v. water; and vi. liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition.

L'invention concerne une composition et une trousse thérapeutique fournissant un azole thérapeutique à solubilité accrue. La trousse comprend un ensemble conditionnement d'aérosol qui contient un contenant renfermant un produit sous pression, et un système de sortie pouvant libérer le produit sous pression sous forme de mousse. Le produit sous pression comprend une composition moussable qui comprend: 1) un azole thérapeutique, la solubilité de l'azole dans la composition, avant moussage, étant inférieure à sa solubilité après moussage; 2) au moins un excipient organique choisi dans le groupe constitué par un excipient organique hydrophobe, un cosolvant, un émollient et des mélanges de ceux-ci, à une concentration d'environ 2 % à environ 50 % en poids; 3) un agent de surface; 4) d'environ 0,01 % à environ 5 % en poids d'au moins un additif polymère choisi dans le groupe constitué par un agent bioadhésif, un agent gélifiant, un agent filmogène et un agent à changement de phase; 5) de l'eau; et 6) un agent propulseur liquéfié ou sous forme de gaz comprimé, dont la concentration est d'environ 3 % à environ 25 % en poids de la composition totale.

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