Details for Patent: 6,919,069
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| Title: | 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. |
| Inventor(s): | Akehurst; Rachel Ann (Hertsfordshire, GB), Taylor; Anthony James (Hertsfordshire, GB), Wyatt; David Andrew (Hertsfordshire, GB) |
| Assignee: | Glaxo Group Limited (Middlesex, GB) |
| Filing Date: | Apr 30, 2003 |
| Application Number: | 10/425,839 |
| Claims: | 1. A pharmaceutical aerosol formulation which comprises two or more particulate medicaments, a fluorocarbon or hydrogen-containing fluorocarbon propellant and up to 5% w/w based upon propellant of a polar co-solvent, which formulation is substantially free of surfactant and is free of chlorofluorocarbons. 2. A formulation as claimed in claim 1 wherein said medicaments are selected from the group consisting of an anti-allergic, a bronchodilator and an anti-inflammatory steroid. 3. A formulation as claimed in claim 1 wherein said medicaments are selected from the group consisting of salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates thereof. 4. A formulation as claimed in claim 1 which comprises a particulate bronchodilatory medicament and a particulate anti-inflammatory medicament. 5. A formulation as claimed in claim 1 which comprises salmeterol or a physiologically acceptable salt thereof in combination with fluticasone propionate. 6. A formulation as claimed in claim 1 which comprises salmeterol xinafoate in combination with fluticasone propionate. 7. A formulation according to claim 1 wherein the propellant comprises 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n-propane. 8. A formulation according to claim 1 wherein the polar co-solvent is ethanol. 9. A formulation according to claim 1 wherein the medicament is present in an amount of 0.005-5% w/w based on the total weight of the formulation. 10. A formulation according to claim 1 which has a respirable fraction of 20% or more based on the total weight of the formulation. 11. A formulation according to claim 1 wherein said particulate medicament is surface modified. 12. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation which comprises two or more particulate medicaments a fluorocarbon or hydrogen-containing fluorocarbon propellant and up to 5% w/w based upon propellant of a polar co-solvent, which formulation is substantially free of surfactant. 13. A formulation according to claim 1 wherein the polar co-solvent is present in an amount of 0.01 to 5% w/w based upon propellant of a polar co-solvent. 14. A formulation according to claim 1 wherein the polar co-solvent is present in an amount of 0.05 to 3% w/w based upon propellant of a polar co-solvent. 15. A formulation according to claim 1 wherein one of said medicaments is triamcinoline acetonide. 16. A formulation according to claim 1 wherein one of said medicaments is formoterol or a physiologically acceptable salt thereof. 17. A formulation according to claim 13 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 18. A formulation according to claim 14 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 19. A formulation according to claim 15 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 20. A formulation according to claim 16 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 21. A formulation according to claim 4 wherein the anti-inflammatory medicament is a steroidal anti-inflammatory medicament. 22. A method according to claim 12 wherein the respiratory disorder is asthma. 23. A method according to claim 12 wherein the polar co-solvent is present in an amount of 0.01 to 5% w/w based upon propellant of a polar co-solvent. 24. A method according to claim 12 wherein the polar co-solvent is present in an amount of 0.05 to 3% w/w based upon propellant of a polar co-solvent. 25. A method according to claim 12 wherein one of said medicaments is triamcinoline acetonide. 26. A method according to claim 12 wherein one of said medicaments is formoterol or a physiologically acceptable salt thereof. 27. A method according to claim 12 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 28. A method according to claim 23 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 29. A method according to claim 24 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 30. A method according to claim 25 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 31. A method according to claim 26 wherein the propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof. 32. A pharmaceutical aerosol formulation which comprises (a) a particulate bronchodilatory medicament (b) a particulate steroidal anti-inflammatory medicament (c) a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof and (d) 0.05-3% w/w based upon propellant of ethanol, which formulation is substantially free of surfactant and is free of chlorofluorocarbons. 33. A pharmaceutical aerosol formulation which consists essentially of (a) a particulate bronchodilatory medicament (b) a particulate steroidal anti-inflammatory medicament (c) a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane and mixtures thereof and (d) 0.05-3% w/w based upon propellant of ethanol, which formulation is substantially free of surfactant and is free of chlorofluorocarbons. 34. A formulation according to claim 32 wherein the bronchodilatory medicament is formoterol or a physiologically acceptable salt thereof. 35. A formulation according to claim 33 wherein the bronchodilatory medicament is formoterol or a physiologically acceptable salt thereof. 36. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation according to claim 32. 37. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation according to claim 33. 38. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation according to claim 34. 39. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation according to claim 35. 40. A method according to claim 36 wherein the respiratory disorder is asthma. 41. A method according to claim 37 wherein the respiratory disorder is asthma. 42. A method according to claim 38 wherein the respiratory disorder is asthma. 43. A method according to claim 39 wherein the respiratory disorder is asthma. |
