Aerosol formulations containing P134a and particulate medicament

Abstract

A pharmaceutical formulation comprising (i) one or more particulate medicaments, and (ii) 1,1,1,2-tetrafuoroethane as propellant, which formulation contains less than 0.0001% w/w surfactant based upon the weight of medicament, particulate medicament being present in an amount from 00005 to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 micrions, with the proviso that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof and with the proviso that when said formulation consists of betamethasone, ergotamine tartrate or sodium cromoglycate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:7900 or 0.866% w/w.

1 . A pharmaceutical aerosol formulation which comprises particulate medicament and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant and with the proviso that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof.  
     
     
         2 . A pharmaceutical aerosol formulation consisting essentially of one more particulate medicament and one or more fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, with the proviso that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof.  
     
     
         3 . A formulation as claimed in  claim 1  wherein said medicaments is an anti-allergic, a bronchodilator or an anti-infammatory steroid.  
     
     
         4 . A formualtion as claimed in  claim 1  wherein said medicament is cromoglycate, terbutaline, reproterol or (−)-4-amino-3,5-dichloro-α-[[[6-[2-(2-pyridinyl)ethoxy]hexyl]amino]methyl]benzenemethanol or a physiologically acceptable salt 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 antiinflammatory medicament.  
     
     
         7 . A formulation as claimed in  claim 1  which comprises a particulate bronchodilatory medicament and a particulate antiallergic medicament.  
     
     
         8 . A formulation as claimed in  claim 7  which comprises isoprenaline and cromogylcate or a physiologically acceptable salt thereof.  
     
     
         9 . A formulation as claimed in  claim 1  which contains 0.005 to 10% w/w of medicament relative to the total weight of the formulation.  
     
     
         10 . A formulation as claimed in  claim 1  wherein the propellant is 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n-propane.  
     
     
         11 . A formulation as claimed in  claim 1  which has a respirable fraction of 20% or more by weight of the medicament.  
     
     
         12 . A formulation as claimed in  claim 1  wherein said particulate medicament is surface-modified.  
     
     
         13 . Surface-modified medicament prepared by admixture of particles of a medicament other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof, with a substantially non-polar, non-solvent liquid, followed by removal of the liquid.  
     
     
         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 and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant and with the proviso that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof.  
     
     
         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 and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant and with the provision that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof.