Medicinal aerosol formulations
First Claim
1. A pressure-liquefied propellant mixture for aerosols, comprising dinitrogen monoxide and a hydrofluoroalkane of formula
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Accused Products
Abstract
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.
126 Citations
51 Claims
- 1. A pressure-liquefied propellant mixture for aerosols, comprising dinitrogen monoxide and a hydrofluoroalkane of formula
- 11. A medicinal aerosol formulation, comprising an efficacious amount of a pharmaceutically active compound and a pressure-liquefied propellant mixture, comprising dinitrogen monoxide and a hydrofluoroalkane of formula
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25. A process for the preparation of a medicinal aerosol formulation, comprising an efficacious amount of a pharmaceutically active compound and a pressure-liquefied propellant mixture, comprising dinitrogen monoxide and a hydrofluoroalkane of formula
- 47. An inhalable medicinal aerosol formulation, administrable by a metered dose inhaler, comprising an effective amount of a pharmaceutically active compound and a pressure-liquefied homogeneous propellant mixture comprising dinitrogen monoxide and a hydrofluoroalkane of formula
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51. An inhalable medicinal aerosol formulation administrable by a metered dose inhaler, comprising an effective amount of a pharmaceutically active compound selectd from the group consisting of salbutamol, formoterol, salmeterol, fluticasone, dudesonide, ciclesonide, glycopyrronium, tiotropium, cromoglycic acid, nedocromil, mometasone, sildenafil, becomethasone, levalbuterol and pharmaceutically acceptale salts and derivatibves thereof, and a pressure-liquefied homogeneous propellant mixure comprising dinitrogen monoxide and a hydrofluoroalkane selected from the group consisting of 1,1,1,2,-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane and 1,1,1,2-tetrafluoroethane in the presence of 1,1,1,2,3,3,3-heptafluoropropane, the dinitrogen monoxide being present in an amount of from 0.01% to 2% by weight, based on the total weight of the formulation, and the hydrofluoroalkane being present in an amount of at least 64% by weight, on the total weight of the formulation.
Specification