Butixocort aerosol formulations in hydrofluorocarbon propellant

• US 5,653,961 A
• Filed: 03/31/1995
• Issued: 08/05/1997
• Est. Priority Date: 03/31/1995
• Status: Expired due to Fees

• Current Assignee: 3M Company
• Original Assignee: 3M Company
• Inventors: McNally, Rebecca A., Ward, Gary H.
• Primary Examiner(s): Bawa, Raj
• Application Number:
  US08/414,370
• Time in Patent Office: 858 Days
• Field of Search: 424/45, 424/47, 424/46, 514/958
• US Class Current: 424/45
• 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]

Abstract

Pharmaceutical solution aerosol formulations of butixocort propionate as the sole active drug agent 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. A solution aerosol formulation comprising:

a propellant system 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

a therapeutically effective amount of butixocort propionate, wherein the butixocort propionate is dissolved in the formulation and is the sole drug in the formulation.

2. An aerosol formulation according to claim 1, wherein the propellant comprises 1,1,1,2-tetrafluoroethane.

3. An aerosol formulation according to claim 1, wherein the propellant comprises 1,1,1,2,3,3,3-heptafluoropropane.

4. An aerosol formulation according to claim 1, wherein the propellant comprises a mixture of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane.

5. An aerosol formulation according to claim 1, wherein the butixocort propionate is present in an amount of about 0.1 percent to about 0.9 percent by weight.

6. An aerosol formulation according to claim 1, characterized in that it is free of chlorofluorocarbons.

7. An aerosol formulation according to claim 1, further comprising ethanol.

8. An aerosol formulation according to claim 7, wherein the ethanol is present in an amount of about 3 percent to about 30 percent by weight.

9. An aerosol formulation according to claim 8, wherein the ethanol is present in an amount of about 8 percent to about 16 percent by weight.

10. An aerosol formulation according to claim 1 further comprising about 0.005 percent to about 1 percent by weight water.

11. An aerosol formulation according to claim 1 further comprising a flavoring agent.

12. An aerosol formulation according to claim 1 comprising from about 0.1 percent to about 0.9 by weight butixocort propionate, from about 8 to about 16 percent by weight ethanol, and 1,1,1,2,3,3,3-heptafluoropropane.

13. An aerosol formulation according to claim 1 comprising from about 0.1 percent to about 0.9 percent by weight butixocort propionate, from about 8 to about 16 percent by weight ethanol, and 1,1,1,2-tetrafluoroethane.

14. An aerosol formulation according to claim 1, wherein the formulation exhibits at least 93 percent drug recovery after storage for ten months at 40°

C. in an aluminum aerosol canister.

15. A method of treating bronchial asthma comprising administering via inhalation an amount of a formulation according to claim 1 so as to control inflammation associated with bronchial asthma.

16. A metered dose inhaler comprising:

(i) an aerosol canister defining a formulation chamber; and

(ii) a formulation according to claim 1, wherein said formulation is contained within said formulation chamber.