Aerosol formulation containing particulate formoterol, propellant and polar cosolvent

Abstract

A pharmaceutical aerosol formulation comprising (i) particulate medicament, (ii) 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3,-heptafluoro-n-propane or a mixture thereof as propellant, and (iii) 0.01 to 5% w/w based upon the propellant of a polar cosolvent, the particulate medicament being present in an amount from 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, and which formulation contains less than 0.0001% w/w surfactant based upon the weight of medicament.

1 . A pharmaceutical aerosol formulation which comprises particulate medicament, a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant and up to 5% w/w based upon propellant of a polar cosolvent, which formulation is substantially free of surfactant.  
     
     
         2 . A pharmaceutical aerosol formulation consisting essentially of one or more particulate medicament, one or more fluorocarbon or hydrogen-containing chlorofluorocarbon propellant and 0.01 to 5% w/w based upon propellant of a polar cosolvent.  
     
     
         3 . A formulation as claimed in  claim 1  wherein said medicament is an anti-allergic, a bronchodilator or an anti-inflammatory steroid.  
     
     
         4 . A formulation as claimed in  claim 1  wherein said medicament is selected from salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates thereof.  
     
     
         5 . A formulation as claimed in  claim 1  which contains two or more particulate medicaments.  
     
     
         6 . A formulation as claimed in  claim 1  which comprises a particulate bronchodilatory medicament and a particulate anti-inflammatory medicament.  
     
     
         7 . A formulation as claimed in  claim 1  which comprises salmeterol or a physiologically acceptable salt thereof in combination with fluticasone propionate.  
     
     
         8 . A formulation as claimed in  claim 1  which comprises salmeterol xinafoate in combination with fluticasone propionate.  
     
     
         9 . A formulation as claimed in  claim 1  wherein the propellant comprises 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n-propane.  
     
     
         10 . A formulation as claimed in  claim 1  wherein the polar cosolvent is ethanol.  
     
     
         11 . A formulation as claimed in  claim 1  wherein the medicament is present in an amount of 0.005 to 10% w/w based on the total weight of the formulation.  
     
     
         12 . A formulation as claimed in  claim 1  which has a respirable fraction of 20% or more by weight of the medicament.  
     
     
         13 . A formulation as claimed in claims  1  wherein said particulate medicament is surface-modified.  
     
     
         14 . A canister suitable for delivering a pharmaceutical aerosol formulation which comprises a container capable of withstanding the vapour pressure of the propellant used, which container is closed with a metering valve and contains a pharmaceutical aerosol formulation which comprises particulate medicament, a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant and up to 5% w/w based upon propellant of a polar cosolvent, which formulation is substantially free of surfactant.  
     
     
         15 . A metered dose inhaler which comprises a canister as claimed in  claim 14  fitted into a suitable channelling device.  
     
     
         16 . A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation which comprises particulate medicament, a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant and up to 5% w/w based upon propellant of a polar cosolvent, which formulation is substantially free of surfactant.