Medicinal aerosol formulations

A - Human Necessities – 61 – K

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A61K 9/12 (2006.01) C09K 3/30 (2006.01)

Patent

CA 2338753

A pressure-liquefied propellant mixture for aerosols, comprising dinitrogen monoxide and a hydrofluoroalkane having 1 to 3 carbon atoms, in particular 1,1,1,2-tetrafluoroethane and/or 1,1,1,2,3,3,3-heptafluoropropane, makes possible an improvement in the wetting properties of pharmaceutically active compounds, whereby the formulation problems existing with hydrofluoroalkanes can be overcome with respect to suspension and solution aerosols and thus improved medicinal aerosol formulations can be obtained. With the aid of dinitrogen monoxide, it is also possible to influence the pressure and thus the particle size distribution specifically and, by displacement of oxygen from the hydrofluoroalkanes, to improve the storage stability of oxidation-sensitive active compounds. If desired, the propellant mixture can additionally contain carbon dioxide.

L'invention concerne un mélange d'agents propulseurs fluidisé par pression pour aérosols, qui comprend du monoxyde de diazote et un hydrofluoroalcane ayant entre 1 et 3 atomes de carbone, notamment du 1,1,1,2-tétrafluoroéthane et/ou du 1,1,1,2,3,3,3-heptafluoropropane. Ce mélange permet d'améliorer les propriétés de mouillance de principes actifs pharmaceutiques, ce qui permet de pallier les problèmes de formulation inhérents aux hydrofluoroalcanes, par rapport aux aérosols en suspension et en solution et par conséquent d'obtenir de meilleures formulations médicales d'aérosols. Le monoxyde de diazote permet d'influer de manière ciblée sur la pression et par conséquent sur la répartition de la dimension des particules, ainsi que d'améliorer la stabilité au stockage de principes actifs sensibles à l'oxydation, par déplacement d'oxygène hors des hydrofluoroalcanes. Le mélange d'agents propulseurs peut le cas échéant contenir également du dioxyde de carbone.

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