Details for Patent: 5,922,306
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Title: | Aerosol formulations containing P134a and particulate medicament |
Abstract: | A pharmaceutical formulation comprising (i) one or more particulate medicaments, and (ii) 1,1,1,2-tetrafluoroethane 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 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 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. |
Inventor(s): | Akehurst; Rachel Ann (Ware, GB), Taylor; Anthony James (Ware, GB), Wyatt; David Andrew (Ware, GB) |
Assignee: | Glaxo Group Limited (Greenford, GB) |
Filing Date: | Apr 15, 1998 |
Application Number: | 09/060,110 |
Claims: | 1. A pharmaceutical formulation consisting essentially of (i) one or more particulate medicaments, and (ii) 1,1,1,2-tetrafluoroethane 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 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 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. 2. A formulation as claimed in claim 1 which is free of surfactant. 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 a bronchodilator. 5. A formulation as claimed in claim 1 wherein said medicament is pirbuterol or a physiologically acceptable salt thereof. 6. A formulation as claimed in claim 1 which contains two or more particulate medicaments. 7. A formulation as claimed in claim 1 which comprises a particulate bronchodilatory medicament and a particulate anti-inflammatory medicament. 8. A formulation as claimed in claim 1 which comprises a particulate bronchodilatory medicament and a particulate anti-allergic medicament. 9. A formulation as claimed in claim 1 which comprises isoprenaline and cromoglycate or a physiologically acceptable salt thereof. 10. A formulation as claimed in claim 1 which contains 0.01 to 1% w/w of medicament relative to the total weight of the formulation. 11. A formulation as claimed in claim 1 which has a respirable fraction of 20% or more by weight of medicament. 12. A formulation as claimed in claim 1 wherein said medicament is an anti-allergic medicament selected from the group consisting of ketotifen, nedocromil and physiologically acceptable salts thereof. 13. A formulation as claimed in claim 1 wherein said medicament is an anti-inflammatory medicament selected from the group consisting of budesonide and triamcinolone acetonide. 14. A formulation as claimed in claim 1 wherein said medicament is an anti-inflammatory medicament which is flunisolide. 15. A formulation as claimed in claim 1 wherein said medicament is an anti-cholinergic medicament selected from the group consisting of ipratropium, atropine, oxitropium and physiologically acceptable salts thereof. 16. A formulation as claimed in claim 1 wherein said medicament is a xanthine selected from the group consisting of aminophylline, choline theophyllinate, lysine theophyllinate, theophylline and physiologically acceptable salts thereof. 17. A formulation as claimed in claim 1 wherein said medicament is cromoglycate or a physiologically acceptable salt thereof. 18. A pharmaceutical aerosol formulation consisting of (i) one or more particulate medicaments, and (ii) 1,1,1,2-tetrafluoroethane as propellant, 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, 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. 19. A formulation as claimed in claim 1 wherein said medicament is an anti-allergic, a bronchodilator or an anti-inflammatory steroid. 20. A formulation as claimed in claim 1 wherein said medicament is a bronchodilator. 21. A formulation as claimed in claim 1 wherein said medicament is pirbuterol or a physiologically acceptable salt thereof. 22. A formulation as claimed in claim 1 which contains two or more particulate medicaments. 23. A formulation as claimed in claim 1 which comprises a particulate bronchodilatory medicament and a particulate anti-inflammatory medicament. 24. A formulation as claimed in claim 1 which comprises a particulate bronchodilatory medicament and a particulate anti-allergic medicament. 25. A formulation as claimed in claim 1 which comprises isoprenaline and cromoglycate or a physiologically acceptable salt thereof. 26. A formulation as claimed in claim 1 which contains 0.01 to 1% w/w of medicament relative to the total weight of the formulation. 27. A formulation as claimed in claim 1 which has a respirable fraction of 20% or more by weight of medicament. 28. A formulation as claimed in claim 1 wherein said medicament is an anti-allergic medicament selected from the group consisting of ketotifen, nedocromil and physiologically acceptable salts thereof. 29. A formulation as claimed in claim 1 wherein said medicament is an anti-inflammatory medicament selected from the group consisting of budesonide and triamcinolone acetonide. 30. A formulation as claimed in claim 1 wherein said medicament is an anti-inflammatory medicament which is flunisolide. 31. A formulation as claimed in claim 1 wherein said medicament is an anti-cholinergic medicament selected from the group consisting of ipratropium, atropine, oxitropium and physiologically acceptable salts thereof. 32. A formulation as claimed in claim 18 wherein said medicament is a xanthine selected from the group consisting of aminophylline, choline theophyllinate, lysine theophyllinate, theophylline and physiologically acceptable salts thereof. 33. A pharmaceutical aerosol formulation consisting essentially of (i) one or more particulate medicaments, and (ii) 1,1,1,2-tetrafluoroethane as propellant, which formulation is free of surfactant, 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, with the proviso that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof and which formulation contains less than 0.866% w/w of medicament relative to the total weight of the formulation. 34. A pharmaceutical aerosol formulation consisting essentially of (i) one or more particulate medicaments, and (ii) 1,1,1,2-tetrafluoroethane as propellant, which formulation is free of surfactant, 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, with the proviso that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt of solvate thereof and which formulation contains 0.005 to 0.659% w/w medicament relative to the total weight of the formulation. |