Formulations for inhalation

Abstract

A pharmaceutical aerosol formulation comprising (i) a compound of formula (I) or a solvate thereof as medicament, (ii) a liquified hydrofluoroalkane (HFA) gas as propellant; and characterised in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.

1 . A pharmaceutical aerosol formulation comprising (i) a compound of formula (I)  
       
         
           
           
               
               
           
         
       
       or a solvate thereof as medicament, (ii) a liquified hydrofluoroalkane (HFA) gas as propellant, wherein the propellant gas is a mixture of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoro-n-propane; and characterised in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.  
     
     
         2 . A formulation according to  claim 1  which contains a hydroxy containing co-solvent liquid as solubilising agent.  
     
     
         3 . A formulation according to  claim 2  wherein the solubilising agent is ethanol.  
     
     
         4 . A formulation according to  claim 1  further comprising a low volatility component.  
     
     
         5 . A formulation according to  claim 4  wherein the low volatility component is glycerol.  
     
     
         6 - 9 . (canceled)  
     
     
         10 . A pharmaceutical aerosol formulation according to  claim 1  wherein 1,1,1,2,3,3,3-heptafluoro-n-propane comprises the propellant, and said formulation further comprising: 
 a solubilising agent to assist the solubilisation of the medicament in the propellant and    optionally, a low volatility component;    characterised in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.    
     
     
         11 . A formulation according to  claim 10  which contains ethanol as solubilising agent and glycerol as low volatility component.  
     
     
         12 . A formulation according to  claim 10  wherein the solubilising agent is an oligolactic acid or derivative thereof.  
     
     
         13 . A formulation according to  claim 12  wherein the solubilising agent is a compound of formula (IIA)  
         CH 3 —CO—[O—CH(CH 3 )—CO] n —OH   (IIA)  
       or a derivative thereof, wherein n is an integer from 3 to 15.  
     
     
         14 . A canister comprising a container containing a formulation according to  claim 1  and fitted with a metering valve.  
     
     
         15 . A metered dose inhaler comprising a canister according to  claim 14  fitted with an actuator adapted for topical administration of the formulation to the lung.  
     
     
         16 . A metered dose inhaler comprising a canister according to  claim 14  fitted with an actuator adapted for topical administration of the formulation to the nose.  
     
     
         17 . A canister comprising a container containing a formulation according to  claim 10  and fitted with a metering valve.  
     
     
         18 . A metered dose inhaler comprising a canister according to  claim 17  fitted with an actuator adapted for topical administration of the formulation to the lung.  
     
     
         19 . A metered dose inhaler comprising a canister according to  claim 17  fitted with an actuator adapted for topical administration of the formulation to the nose.  
     
     
         20 . A method of treatment of an individual having an inflammatory or allergic condition or disease comprising administration to said individual the formulation of  claim 1 .  
     
     
         21 . The method of treatment of  claim 20  wherein said inflammatory or allergic condition or disease is asthma.  
     
     
         22 . The method of treatment of  claim 20  wherein said inflammatory or allergic condition or disease is chronic obstructive pulmonary disease.  
     
     
         23 . A method of treatment of an individual having an inflammatory or allergic condition or disease comprising administration to said individual the formulation of  claim 10 .  
     
     
         24 . The method of treatment of  claim 23  wherein said inflammatory or allergic condition or disease is asthma.  
     
     
         25 . The method of treatment of  claim 23  wherein said inflammatory or allergic condition or disease is chronic obstructive pulmonary disease.