Details for Patent: 5,674,471
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| Title: | Aerosol formulations containing P134a and salbutamol |
| Abstract: | The invention relates to a pharmaceutical aerosol formulation consisting essentially of particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation contains less than 0.0001% surfactant based upon the weight of medicament, particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, with the provisos that when said formulation consists 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 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 or 0.866%. |
| Inventor(s): | Akehurst; Rachel Ann (Ware, GB3), Taylor; Anthony James (Ware, GB3), Wyatt; David Andrew (Ware, GB3) |
| Assignee: | Glaxo Group Limited (London, GB2) |
| Filing Date: | May 19, 1995 |
| Application Number: | 08/444,725 |
| Claims: | 1. A pharmaceutical aerosol formulation consisting essentially of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation contains less than 0.0001% surfactant based upon the weight of medicament, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, with the provisos that when said formulation consists 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 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 or 0.866%. 2. A formulation as claimed in claim 1 wherein the particulate medicament is present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 3. A formulation as claimed in claim 1 which has a respirable fraction of 20% or more by weight of particulate medicament. 4. A formulation as claimed in claim 1 wherein the salbutamol is in the form of its sulphate salt. 5. A pharmaceutical aerosol formulation consisting essentially of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, which formulation is free of surfactant, with the provisos that when said formulation consists of salbutamol and 1,1,1,2-tetrafluoroethane in a weight ratio of 0.05:18, said salbutamol is in the form of a physiologically acceptable salt and when said formulation consists 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 or 0.0866%. 6. A formulation as claimed in claim 5 wherein the particulate medicament is present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 7. A formulation as claimed in claim 5 which has a respirable fraction of 20% or more by weight of particulate medicament. 8. A formulation as claimed in claim 5 wherein the salbutamol is in the form of its sulphate salt. 9. A pharmaceutical aerosol formulation consisting of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethene as propellant, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, with the provisos that when said formulation consists 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 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 or 0.866%. 10. A formulation as claimed in claim 9 wherein the particulate medicament is present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 11. A formulation as claimed in claim 9 which has a respirable fraction of 20% or more by weight of particulate medicament. 12. A formulation as claimed in claim 9 wherein the salbutamol is in the form of its sulphate salt. 13. A pharmaceutical aerosol formulation consisting essentially of the particulate medicaments salbutamol and beclomethasone dipropionate, or physiologically acceptable salts or solvates thereof, and 1,1,1,2-tetrafluoroethane as propellant, which formulation contains less than 0.0001% w/w surfactant based upon the weight of particulate medicament, the particulate medicaments being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns. 14. A formulation as claimed in claim 13 wherein the salbutamol is in the form of its sulphate salt. 15. A formulation as claimed in claim 13 which formulation is free of surfactant. 16. A formulation as claimed in claim 13 wherein the particulate medicaments are present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 17. A pharmaceutical aerosol formulation consisting of the particulate medicaments salbutamol and beclomethasone dipropionate, or physiologically acceptable salts or solvates thereof, and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicaments 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. 18. A formulation as claimed in claim 17 wherein the salbutamol is in the form of its sulphate salt. 19. A formulation as claimed in claim 17 wherein the particulate medicaments are present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 20. A pharmaceutical aerosol formulation consisting essentially of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, which formulation is free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate there is present in an amount of less than 0.866% w/w based on the total weight of the formulation, with the proviso that when said formulation consists 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. 21. A pharmaceutical aerosol formulation consisting essentially of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, which formulation is 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, with the proviso that when said formulation consists 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. 22. A pharmaceutical aerosol formulation consisting essentially of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, which formulation is 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. 23. A pharmaceutical aerosol formulation consisting essentially of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, which formulation is 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. 24. A pharmaceutical aerosol formulation consisting essentially of a particulate medicament which is salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicament being present in an amount of 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, which formulation is free of surfactant, and wherein the weight ratio of salbutamol or a pharmaceutically acceptable or solvate thereof to propellant is less than 0.05:18. 25. A formulation as claimed in claim 20 wherein the salbutamol is in the form of its sulphate salt. 26. A formulation as claimed in claim 21 wherein the salbutamol is in the form of its sulphate salt. 27. A formulation as claimed in claim 22 wherein the salbutamol is in the form of its sulphate salt. 28. A formulation as claimed in claim 23 wherein the salbutamol is in the form of its sulphate salt. 29. A formulation as claimed in claim 24, wherein the salbutamol is in the form of its sulphate salt. 30. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of the pharmaceutical aerosol formulation of claim 1. 31. A method as claimed in claim 30 wherein the particulate medicament is present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 32. A method as claimed in claim 30 wherein the formulation has a respirable fraction of 20% or more by weight of particulate medicament. 33. A method as claimed in claim 30 wherein the salbutamol is in the form of its sulphate salt. 34. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of the pharmaceutical aerosol formulation of claim 5. 35. A method as claimed in claim 34 wherein the salbutamol is in the form of its sulphate salt. 36. A method as claimed in claim 34 wherein the particulate medicament is present in an amount of 0.01% to 1% w/w relative to the total weight of the formulation. 37. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of the pharmaceutical aerosol formulation of claim 9. 38. A method as claimed in claim 37 wherein the particulate medicament is present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 39. A method as claimed in claim 37 wherein the formulation has a respirable fraction of 20% or more by weight of particulate medicament. 40. A method as claimed in claim 37 wherein the salbutamol is in the form of its sulphate salt. 41. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of the pharmaceutical aerosol formulation of claim 13. 42. A method as claimed in claim 41 wherein the formulation has a respirable fraction of 20% or more by weight of particulate medicament. 43. A method as claimed in claim 41 wherein the salbutamol is in the form of its sulphate salt. 44. A method as claimed in claim 41 which formulation is free of surfactant. 45. A method as claimed in claim 41 wherein the particulate medicaments are present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 46. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of the pharmaceutical aerosol formulation of claim 17. 47. A method as claimed in claim 46 wherein the formulation has a respirable fraction of 20% or more by weight of particulate medicament. 48. A method as claimed in claim 46 wherein the salbutamol is in the form of its sulphate salt. 49. A method as claimed in claim 46 wherein the particulate medicaments are present in an amount of 0.01 to 1% w/w relative to the total weight of the formulation. 50. A pharmaceutical aerosol formulation consisting of a particulate medicament which is salbutamol sulphate and 1,1,1,2-tetrafluoroethane as propellant, the particulate medicament being present in an amount of 0.01% to 1% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, with the proviso that the weight to weight ratio of medicament to propellant is other than 69:7900 or 0.866%. 51. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of the pharmaceutical aerosol formulation of claim 50. |
