Medicaments

Abstract

This invention relates to aerosol formulations of use for the administration of medicaments by inhalation, in particular a pharmaceutical aerosol formulation which comprises particulate salbutamol and physiologically acceptable salts and solvates thereof and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.

We claim:  
     
         1 . A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, with the proviso that when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:7900 (0.866%).  
     
     
         2 . A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, with the provisos that when said formulation consists essentially of salbutamol and 1,1,1,2-tetrafluoroethane in a weight ratio of 0.05:18, said salbutamol is present in the form of a physiologically acceptable salt and when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:7900 (0.866%).  
     
     
         3 . A pharmaceutical aerosol formulation consisting essentially of a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, with the proviso that when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:7900 (0.866%).  
     
     
         4 . A pharmaceutical aerosol-formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of less than 0.866% w/w based on the total weight of the formulation.  
     
     
         5 . A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvat thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of 0.005 to 0.594% w/w based on the total weight of the formulation.  
     
     
         6 . A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of 0.005 to 0.264% w/w based on the total weight of the formulation.  
     
     
         7 . A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of 0.005 to 0.174% w/w based on the total weight of the formulation.  
     
     
         8 . A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the weight ratio of salbutamol or a pharmaceutically acceptable salt or solvate thereof to propellant is less than 0.05:18.  
     
     
         9 . A formulation as claimed in any one of  claims 1  to  8  wherein the medicament is salbutamol sulphate.  
     
     
         10 . A formulation as claimed in any one of  claims 1  to  8  which contains salbutamol or a physiologically acceptable salt or solvate thereof in combination with an anti-inflammatory steroid or an anti-allergic.  
     
     
         11 . A formulation as claimed in any one of  claims 1  to  8  which contains salbutamol or a physiologically acceptable salt or solvate thereof in combination with fluticasone propionate or beclomethasone dipropionate or a physiologically acceptable solvate thereof.  
     
     
         12 . A formulation as claimed in any one of  claims 1  to  8  which contains salbutamol and beclomethasone dipropionate.  
     
     
         13 . A formulation as claimed in any one of  claims 1  to  8  which has a respirable fraction of 20% or more by weight of the salbutamol or a physiologically acceptable salt or solvate thereof.  
     
     
         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 a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially-free of surfactant and with the proviso that when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:7900 (0.866%).  
     
     
         15 . A canister as claimed in  claim 14  wherein the container is a metal can.  
     
     
         16 . A metered dose inhaler which comprises a canister as claimed in  claim 14  fitted into a suitable channelling device.  
     
     
         17 . A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation which comprises particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant.