Pharmaceutical aerosol formulations containing fluoroalkanes and budesonide

Abstract

Provided is a solution aerosol formulation adapted for use in a pressurized aerosol container. The aerosol formulation is formulated from a composition containing Budesonide, at least one fluoroalkane propellant, and a cosolvent present in an amount that dissolves or solubilizes the Budesonide in the mixture of cosolvent and propellant.

1 . A pressurized metered dose inhaler comprising a container equipped with a metering valve and containing a pressurized solution aerosol formulation formulated from a composition comprising: 
 Budesonide;    at least one fluoroalkane propellant; and    a cosolvent present in an amount that dissolves or solubilizes said Budesonide in the mixture of cosolvent and propellant.    
     
     
         2 . A pressurized metered dose inhaler according to  claim 1 , wherein said cosolvent comprises ethanol.  
     
     
         3 . A pressurized metered dose inhaler according to  claim 2 , wherein said ethanol is present in an amount of at least 10% by weight.  
     
     
         4 . A pressurized metered dose inhaler according to  claim 2 , wherein said ethanol is present in an amount of at least 15% by weight.  
     
     
         5 . A pressurized metered dose inhaler according to  claim 2 , wherein said ethanol is present in an amount of at least 20% by weight.  
     
     
         6 . A pressurized metered dose inhaler according to  claim 2 , wherein said ethanol is present in an amount of at least 25% by weight.  
     
     
         7 . A pressurized metered dose inhaler according to  claim 1 , wherein said formulation is free of a surfactant.  
     
     
         8 . A pressurized metered dose inhaler according to  claim 1 , wherein said propellant comprises 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoropropane.  
     
     
         9 . A pressurized metered dose inhaler according to  claim 1 , wherein said Budesonide is present in an amount of from about 0.01 to about 1% by weight, based on the total weight of the composition.  
     
     
         10 . A pressurized metered dose inhaler according to  claim 1 , wherein said formulation is substantially free of chlorofluorocarbons.  
     
     
         11 . A pressurized metered dose inhaler according to  claim 1 , wherein said propellant is present in an amount of from about 70 to about 94% by weight.  
     
     
         12 . A pressurized metered dose inhaler according to  claim 1 , wherein said cosolvent comprises an aliphatic alcohol having from 1 to about 6 carbon atoms.  
     
     
         13 . A pressurized metered dose inhaler according to  claim 1 , wherein said cosolvent is present in an amount sufficient to maintain said Budesonide in solution at 0° C.  
     
     
         14 . A pressurized metered dose inhaler according to  claim 1 , wherein said Budesonide is present in an amount of about 0.05 to about 0.5% by weight, said cosolvent comprises ethanol in an amount of about 10 to about 40% by weight, and said propellant is present in an amount of from about 60% to about 90% by weight, all weights based on the total weight of said aerosol formulation.  
     
     
         15 . A pressurized metered dose inhaler according to  claim 1 , wherein said aerosol formulation is adapted to be stable under conditions up to about 40° C. and about 75% relative humidity for at least about four weeks.  
     
     
         16 . A pressurized metered dose inhaler comprising a container equipped with a metering valve and containing a pressurized solution aerosol formulation formulated from a composition comprising: 
 Budesonide;    1,1,1,2-tetrafluoroethane as a propellant; and    at least about 10% ethanol, wherein the ethanol is present in an amount that dissolves or solubilizes said Budesonide in the mixture of 1,1,1,2-tetrafluoroethane and propellant.    
     
     
         17 . A pressurized metered dose inhaler comprising a container equipped with a metering valve and containing a pressurized solution aerosol formulation formulated from a composition comprising: 
 Budesonide;    1,1,1,2,3,3,3-heptafluoropropane as a propellant; and    at least about 10% ethanol, wherein the ethanol is present in an amount that dissolves or solubilizes said Budesonide in the mixture of 1,1,1,2,3,3,3-heptafluoropropane and propellant.    
     
     
         18 . A solution aerosol formulation adapted for use in a pressurized aerosol container, said aerosol formulation being formulated from a composition comprising: 
 Budesonide;    at least one fluoroalkane propellant; and    a cosolvent present in an amount that dissolves or solubilizes said Budesonide in the mixture of cosolvent and propellant.    
     
     
         19 . A solution aerosol formulation according to  claim 18 , wherein said cosolvent comprises ethanol.  
     
     
         20 . A solution aerosol formulation according to  claim 19 , wherein said ethanol is present in an amount of at least 10% by weight.  
     
     
         21 . A solution aerosol formulation according to  claim 19 , wherein said ethanol is present in an amount of at least 15% by weight.  
     
     
         22 . A solution aerosol formulation according to  claim 19 , wherein said ethanol is present in an amount of at least 20% by weight.  
     
     
         23 . A solution aerosol formulation according to  claim 19 , wherein said ethanol is present in an amount of at least 25% by weight.  
     
     
         24 . A solution aerosol formulation according to  claim 18 , wherein said formulation is free of a surfactant.  
     
     
         25 . A solution aerosol formulation according to  claim 18 , wherein said propellant comprises 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoropropane.  
     
     
         26 . A solution aerosol formulation according to  claim 18 , wherein said Budesonide is present in an amount of from about 0.01 to about 1% by weight, based on the total weight of the composition.  
     
     
         27 . A solution aerosol formulation according to  claim 18 , wherein said formulation is substantially free of chlorofluorocarbons.  
     
     
         28 . A solution aerosol formulation according to  claim 18 , wherein said propellant is present in an amount of from about 70 to about 94% by weight.  
     
     
         29 . A solution aerosol formulation according to  claim 18 , wherein said cosolvent is present in an amount sufficient to maintain said Budesonide in solution at 0° C.  
     
     
         30 . A solution aerosol formulation according to  claim 18 , wherein said cosolvent comprises an aliphatic alcohol having from 1 to about 6 carbon atoms.  
     
     
         31 . A solution aerosol formulation according to  claim 18 , wherein said Budesonide is present in an amount of about 0.05 to about 0.5% by weight, said cosolvent comprises ethanol in an amount of about 10 to about 40% by weight, and said propellant is present in an amount of from about 60% to about 90% by weight, all weights based on the total weight of said aerosol formulation.  
     
     
         32 . A solution aerosol formulation according to  claim 18 , wherein said aerosol formulation is adapted to be stable under conditions up to about 40° C. and about 75% relative humidity for at least about four weeks.  
     
     
         33 . A solution aerosol formulation adapted for use in a pressurized aerosol container, said aerosol formulation being formulated from a composition comprising: 
 Budesonide;    1,1,1,2-tetrafluoroethane as a propellant; and    at least about 10% ethanol, wherein the ethanol is present in an amount that dissolves or solubilizes said Budesonide in the mixture of 1,1,1,2-tetrafluoroethane and propellant.    
     
     
         34 . A solution aerosol formulation adapted for use in a pressurized aerosol container, said aerosol formulation being formulated from a composition comprising: 
 Budesonide;      1 , 1 , 1 , 2 , 3 , 3 , 3 -heptafluoropropane as a propellant; and    at least about 10% ethanol, wherein the ethanol is present in an amount that dissolves or solubilizes said Budesonide in the mixture of 1,1,1,2,3,3,3-heptafluoropropane and propellant.