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Details for Patent: 5,916,540

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Details for Patent: 5,916,540

Title: Aerosol formulations containing P134A and/or P227 and particulate medicament
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 (Ware, GB), Taylor; Anthony James (Ware, GB), Wyatt; David Andrew (Ware, GB)
Assignee: Glaxo Group Limited (Middlesex, GB)
Filing Date:Apr 06, 1998
Application Number:09/055,253
Claims:1. A pharmaceutical aerosol formulation consisting essentially of (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.

2. A formulation as claimed in claim 1 wherein the polar cosolvent is present in an amount from 0.05 to 3% w/w based upon the propellant.

3. A formulation as claimed in claim 1 wherein the polar cosolvent is present in an amount of 0.05 to 5% w/w based upon the propellant.

4. A formulation as claimed in claim 2 wherein said medicament is an anti-allergic, a bronchodilator or an anti-inflammatory steroid.

5. A formulation as claimed in claim 2 wherein said medicament is selected from the group consisting of salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates thereof.

6. A formulation as claimed in claim 2 wherein said medicament is beclomethasone dipropionate or a physiologically acceptable solvate thereof.

7. A formulation as claimed in claim 2 wherein said medicament is selected from the group consisting of ephedrine, adrenaline, isoprenaline, metaproterenol, phenylephrine, phenylpropanolamine, rimiterol, terbutaline, (-)4-amino-3,5-dichloro-.alpha.-[[[6-[2-(2-pyridinyl)ethoxy]h exyl]-amino]methyl]benzene-methanol and physiologically acceptable salts thereof.

8. A formulation as claimed in claim 2 wherein said medicament is selected from the group consisting of pirbuterol and physiologically acceptable salts thereof.

9. A formulation as claimed in claim 2 wherein said medicament is selected from the group consisting of formoterol and physiologically acceptable salts thereof.

10. A formulation as claimed in claim 2 wherein said medicament is selected from the group consisting of fenoterol, reproterol, isoetharine and tolubuterol.

11. A formulation as claimed in claim 2 which contains two or more particulate medicaments.

12. A formulation as claimed in claim 2 which contains a particulate bronchodilatory medicament and a particulate anti-inflammatory medicament.

13. A formulation as claimed in claim 2 which contains salmeterol xinafoate in combination with fluticasone propionate.

14. A formulation as claimed in claim 2 which is free of surfactant.

15. A formulation as claimed in claim 2 wherein the medicament is present in an amount from 0.01 to 1% w/w relative to the total weight of the formulation.

16. A formulation as claimed in claim 2 which has a respirable fraction of 20% or more by weight of the medicament.

17. A formulation as claimed in claim 2 wherein said medicament is an anti-allergic medicament selected from the group consisting of ketotifen, nedocromil and physiologically acceptable salts thereof.

18. A formulation as claimed in claim 2 wherein said medicament is selected from the group consisting of cromoglycate and physiologically acceptable salts thereof.

19. A formulation as claimed in claim 2 wherein said medicament is an anti-inflammatory medicament selected from the group consisting of budesonide and triamcinolone acetonide.

20. A formulation as claimed in claim 2 wherein said medicament is flunisolide.

21. A formulation as claimed in claim 2 wherein said medicament is an anti-cholinergic medicament selected from the group consisting of ipratropium, atropine, oxitropium, and physiologically acceptable salts thereof.

22. A formulation as claimed in claim 2 wherein said medicament is a xanthine selected from the group consisting of aminophylline, choline theophyllinate, lysine theophyllinate, theophylline and physiologically acceptable salts thereof.

23. A pharmaceutical aerosol formulation consisting of (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.

24. A formulation as claimed in claim 23 wherein the polar cosolvent is present in an amount from 0.05 to 3% w/w based upon the propellant.

25. A formulation as claimed in claim 24 wherein said medicament is selected from the group consisting of salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates thereof.

26. A formulation as claimed in claim 24 wherein said medicament is beclomethasone dipropionate or a physiologically acceptable solvate thereof.

27. A formulation as claimed in claim 24 wherein said medicament is selected from the group consisting of ephedrine, adrenaline, isoprenaline, metaproterenol, phenylephrine, phenylpropanolamine, rimiterol, terbutaline, orciprenaline, (-)4-amino-3,5-dichloro-.alpha.-[[[6-[2-2(-pyridinyl)ethoxy]hexyl]-amino]m ethyl]benzene-methanol and physiologically acceptable salts thereof.

28. A formulation as claimed in claim 24 wherein said medicament is selected from the group consisting of pirbuterol and physiologically acceptable salts thereof.

29. A formulation as claimed in claim 24 wherein said medicament is selected from the group consisting of formoterol and physiologically acceptable salts thereof.

30. A formulation as claimed in claim 24 wherein said medicament is selected from the group consisting of fenoterol, reproterol, isoetharine and tolubuterol.

31. A formulation as claimed in claim 24 which contains two or more particulate medicaments.

32. A formulation as claimed in claim 24, which contains a particulate bronchodilatory medicament and a particulate anti-inflammatory medicament.

33. A formulation as claimed in claim 24, which contains salmeterol xinafoate in combination with fluticasone propionate.

34. A formulation as claimed in claim 24 wherein said medicament is an anti-allergic, a bronchodilator or an anti-inflammatory steroid.

35. A formulation as claimed in claim 24 wherein the medicament is present in an amount from 0.01 to 1% w/w relative to the total weight of the formulation.

36. A formulation as claimed in claim 24 which has a respirable fraction of 20% or more by weight of the medicament.

37. A formulation as claimed in claim 24 wherein said medicament is an anti-allergic medicament selected from the group consisting of ketotifen, nedocromil and physiologically acceptable salts thereof.

38. A formulation as claimed in claim 24 wherein said medicament is an anti-inflammatory medicament selected from the group consisting of budesonide and triamcinolone acetonide.

39. A formulation as claimed in claim 24 wherein said medicament is an anti-cholinergic medicament selected from the group consisting of ipratropium, atropine, oxitropium, and physiologically acceptable salts thereof.

40. A formulation as claimed in claim 24 wherein said medicament is a xanthine selected from the group consisting of aminophylline, choline theophyllinate, lysine theophyllinate, theophylline and physiologically acceptable salts thereof.

41. A pharmaceutical aerosol formulation consisting essentially of (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) 0.05 to 5% w/w based upon the propellant of a polar cosolvent, the particulate medicament being present in an amount from 0.01 to 1 % 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.

42. A formulation as claimed in claim 41 which is free of surfactant.

43. A formulation as claimed in claim 41 which contains 0.05 to 3% w/w based upon the propellant of a polar cosolvent.

44. A formulation as claimed in claim 42 which contains 0.05 to 3% w/w based upon the propellant of a polar cosolvent.

45. A formulation as claimed in claim 42 wherein said medicament is flunisolide.

46. A formulation as claimed in claim 42 wherein said medicament is formoterol or a physiologically acceptable salt thereof.

47. A formulation as claimed in claim 42 wherein said medicament is selected from the group consisting of ephedrine, adrenaline, isoprenaline, metaproterenol, phenylephrine, phenylpropanolamine, rimiterol, terbutaline, (-)-4-amino-3,5-dichloro-.alpha.-[[[6-[2-(2-pyridinyl)ethoxy] hexyl]-amino]methyl]benzene-methanol and physiologically acceptable salts thereof.

48. A formulation as claimed in claim 42 wherein said medicament is selected from the group consisting of pirbuterol and physiologically acceptable salts thereof.

49. A formulation as claimed in claim 42 wherein said medicament is selected from the group consisting of fenoterol, reproterol, isoetharine and tolubuterol.

50. A formulation as claimed in claim 42 wherein said medicament is an anti-allergic medicament selected from the group consisting of ketotifen or nedocromil and physiologically acceptable salts thereof.

51. A formulation as claimed in claim 42 wherein said medicament is selected from the group consisting of cromoglycate and physiologically acceptable salts thereof.

52. A formulation as claimed in claim 42 wherein said medicament is an anti-inflammatory medicament selected from the group consisting of budesonide and triamcinolone acetonide.

53. A formulation as claimed in claim 42 wherein said medicament is an anti-cholinergic medicament selected from the group consisting of ipratropium, atropine, oxitropium, and physiologically acceptable salts thereof.

54. A formulation as claimed in claim 42 wherein said medicament is a xanthine selected from the group consisting of aminophylline, choline theophyllinate, lysine theophyllinate, theophylline and physiologically acceptable salts thereof.

55. A pharmaceutical aerosol formulation consisting of (i) particulate medicament, (ii) 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3,-heptafluoro-n-propane or a mixture as propellant and (iii) 0.05 to 5% w/w based upon the propellant of a polar cosolvent, the particulate medicament being present in an amount from 0.01 to 1% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns.

56. A formulation as claimed in claim 55 which contains 0.05 to 3% w/w based upon the propellant of a polar cosolvent.

57. A formulation as claimed in claim 56 wherein said medicament is an anti-allergic medicament selected from the group consisting of ketotifen, nedocromil and physiologically acceptable salts thereof.

58. A formulation as claimed in claim 56 wherein said medicament is selected from the group consisting of cromoglycate and physiologically acceptable salts thereof.

59. A formulation as claimed in claim 56 wherein said medicament is an anti-inflammatory medicament selected from the group consisting of budesonide and triamcinolone acetonide.

60. A formulation as claimed in claim 56 wherein said medicament is flunisolide.

61. A formulation as claimed in claim 56 wherein said medicament is an anti-cholinergic medicament selected from the group consisting of ipratropium, atropine, oxitropium, and physiologically acceptable salts thereof.

62. A formulation as claimed in claim 56 wherein said medicament is a xanthine selected from the group consisting of aminophylline, choline theophyllinate, lysine theophyllinate, theophylline and physiologically acceptable salts thereof.

63. A formulation as claimed in claim 56 wherein said medicament is selected from the group consisting of ephedrine, adrenaline, fenoterol, formoterol, isoprenaline, metaproterenol, phenylephrine, phenylpropanolamine, pirbuterol, reproterol, rimiterol, terbutaline, isoetharine, tolubuterol, (-)4-amino-3,5-dichloro-.alpha.-[[[6-[2-(2-pyridinyl)ethoxy]hexyl]-amino]m ethyl]benzene-methanol and physiologically acceptable salts thereof.

64. A pharmaceutical aerosol formulation consisting of (i) a particulate medicament which is triamcinalone acetonide (ii) 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3,-heptafluoro-n-propane or a mixture as propellant and (iii) 0.05 to 3% w/w based upon the propellant of a polar cosolvent, the particulate medicament being present in an amount from 0.01 to 1% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns.

65. A formulation as claimed in claim 64 wherein the polar cosolvent is ethanol.

66. A formulation as claimed in claim 64 wherein the propellant is 1,1,1,2-tetrafluoroethane.

67. A formulation as claimed in claim 65 wherein the propellant is 1,1,1,2-tetrafluoroethane.

68. 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 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.

69. A formulation as claimed in claimed 68 wherein the polar cosolvent is present in an amount of from 0.05% to 3% w/w based upon the propellant.

70. A formulation as claimed in claim 68 wherein the polar cosolvent is present in an amount from 0.05% to 5% w/w based upon the propellant.

71. A formulation as claimed in claim 70 wherein the polar cosolvent is ethanol.

72. A formulation as claimed in claim 70 wherein the medicament is formoterol or a physiologically acceptable salt thereof.

73. A formulation as claimed in claim 69 wherein the medicament is formoterol or a physiologically acceptable salt thereof.

74. A formulation as claimed in claim 73 wherein the polar cosolvent is ethanol.

75. A formulation as claimed in claim 9 wherein the polar cosolvent is ethanol.

76. A formulation as claimed in claim 29 wherein the polar cosolvent is ethanol.

77. A formulation as claimed in claim 46 wherein the polar cosolvent is ethanol.

78. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 1.

79. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 23.

80. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 41.

81. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 55.

82. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 9.

83. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 68.

84. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 2.

85. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 24.

86. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 43.

87. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 56.

88. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 65.

89. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 46.

90. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 69.

91. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as a claimed in claim 74.

92. A formulation as claimed in claim 1 wherein the polar cosolvent is ethanol.

93. A formulation as claimed in claim 23 wherein the polar cosolvent is ethanol.

94. A formulation as claimed in claim 41 wherein the polar cosolvent is ethanol.

95. A formulation as claimed in claim 35 wherein the polar cosolvent is ethanol.

96. 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.

97. A formulation as claimed in claim 23 wherein the propellant is 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n-propane.

98. A formulation as claimed in claim 41 wherein the propellant is 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n-propane.

99. A formulation as claimed in claim 55 wherein the propellant is 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n-propane.

100. A formulation as claimed in claim 68 wherein the propellant is 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n-propane.

101. A formulation as claimed in claim 64 wherein the propellant is 1,1,1,2,3,3,3-heptafluoro-n-propane.

102. A formulation as claimed in claim 68 wherein the propellant is 1,1,1,2,3,3,3-heptafluoro-n-propane.
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