Beclomethasone solution aerosol formulations

• US 5,776,432 A
• Filed: 05/31/1995
• Issued: 07/07/1998
• Est. Priority Date: 10/18/1990
• Status: Expired due to Term

• Current Assignee: Ivax Corporation (Teva Pharmaceutical Industries, Ltd.)
• Original Assignee: 3M Company
• Inventors: Schultz, Robert K., Schultz, David W.
• Primary Examiner(s): Bawa, Raj
• Application Number:
  US08/455,872
• Time in Patent Office: 1,133 Days
• Field of Search: 424/45, 424/47
• US Class Current: 424/45
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• CPC Class Codes: A61K 9/124 characterised by the propellant

Abstract

Pharmaceutical solution aerosol formulations comprising beclomethasone 17,21 dipropionate, ethanol, and a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, and a mixture thereof.

Claims

1. An aerosol formulation comprising a therapeutically effective amount of beclomethasone 17,21 dipropionate, a propellant comprising a hydrofluorocarbon selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, and a mixture thereof, and ethanol in an amount effective to solubilize the beclomethasone 17,21 dipropionate in the propellant, the formulation being further characterized in that the beclomethasone 17,21 dipropionate is dissolved in the formulation, and that the formulation is free of any surfactant.

2. A solution aerosol formulation according to claim 1, comprising between 0.02 and about 0.6 percent by weight beclomethasone 17,21 dipropionate, between about 1 and about 20 percent by weight ethanol, and between about 80 and about 99 percent by weight of said propellant.

3. A solution aerosol formulation according to claim 1 wherein said beclomethasone 17,21 dipropionate is present in an amount of about 0.05 to about 0.5 percent by weight.

4. A solution aerosol formulation according to claim 1 wherein said ethanol is present in an amount of about 2 to about 12 percent by weight.

5. A solution aerosol formulation according to claim 1 wherein said ethanol is present in an amount of about 2 to 10 percent by weight.

6. A solution aerosol formulation according to claim 1 wherein said propellant is present in an amount of about 88 to about 98 percent by weight.

7. A solution aerosol formulation according to claim 1 comprising 1,1,1,2-tetrafluoroethane as substantially the only propellant.

8. A solution aerosol formulation according to claim 1 comprising 1,1,1,2,3,3,3-heptafluoropropane as substantially the only propellant.

9. A solution aerosol formulation according to claim 1 comprising beclomethasone 17,21 dipropionate in an amount of about 0.05 to about 0.5 percent by weight, ethanol in an amount of about 2 to about 12 percent by weight and said propellant in an amount of about 88 to about 98 percent by weight.

10. A solution aerosol formulation according to claim 1 comprising beclomethasone 17, 21 dipropionate in an amount of about 0.05 to about 0.45 percent by weight, ethanol in an amount of about 2 to about 10 percent by weight and said propellant in an amount of about 90 to about 98 percent by weight.

11. A solution aerosol formulation according to claim 1, consisting essentially of beclomethasone 17,21 dipropionate in an amount of about 0.05 to about 0.35 percent by weight, ethanol in an amount of about 2 to about 8 percent by weight, and 1,1,1,2-tetrafluoroethane.

12. A method of treating bronchial asthma in a mammal comprising administering to said mammal an amount of a formulation according to claim 1 sufficient to treat the asthmatic condition.