Flunisolide aerosol formulations

• US 5,776,433 A
• Filed: 05/31/1995
• Issued: 07/07/1998
• Est. Priority Date: 12/20/1993
• Status: Expired due to Term

• Current Assignee: Minnesota Mining and Manufacturing Co (3M Company)
• Original Assignee: Minnesota Mining and Manufacturing Co (3M Company)
• Inventors: Schultz, Robert K., Tzou, Tsi-Zong, Ross, Danna L.
• Primary Examiner(s): Bawa, Raj
• Application Number:
  US08/456,029
• Time in Patent Office: 1,133 Days
• Field of Search: 424/45, 424/46, 514/958, 514/959
• 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 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• 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 aerosol formulations substantially free of chlorofluorocarbons and comprising a therapeutically effective amount of flunisolide in solution with 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 are used for the treatment of bronchial asthma. The formulation may be delivered by a metered dose inhaler with a canister that is inert to flunisolide.

Claims

1. A solution aerosol formulation consisting essentially of about 0.1 percent to about 0.9 percent by weight of flunisolide in solution;

a propellant comprising a hydrofluorocarbon propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3 -heptafluoropropane, and a mixture thereof;

about 3 percent to about 30 percent by weight and ethanol in an amount effective to solubilize the flunisolide 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, characterized in that it is free of chlorofluorocarbon propellants.

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

7. An aerosol formulation according to claim 1 further comprising about 0.001 percent to about 0.1 percent by weight sorbitan trioleate.

8. An aerosol formulation according to claim 1 further comprising about 0.001 percent to about 0.2 percent by weight cetylpyridinium chloride.

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

10. An aerosol formulation according to claim 1 further comprising about 0.3 percent by weight menthol.

11. An aerosol formulation according to claim 1 comprising from about 0.2 percent to about 0.5 by weight flunisolide, from about 10 to about 20 percent by weight ethanol, and 1,1,1,2,3,3,3-heptafluoropropane.

12. An aerosol formulation according to claim 11 comprising from about 0.2 percent to about 0.5 percent by weight flunisolide, from about 10 to about 20 percent by weight ethanol and from about 0.001 percent to about 0.005 percent by weight sorbitan trioleate.

13. An aerosol formulation according to claim 1 comprising from about 0.2 percent to about 0.5 by weight flunisolide, from about 10 to about 20 percent by weight ethanol, and 1,1,1,2-tetrafluoroethane.

14. An aerosol formulation according to claim 13 comprising from about 0.2 percent to about 0.5 percent by weight flunisolide, from about 10 to about 20 percent by weight ethanol and from about 0.001 percent to about 0.005 percent by weight sorbitan trioleate.

15. A method of treating bronchial asthma comprising administering via inhalation an amount of a formulation according to claim 1 sufficient to treat 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.

17. An inhaler according to claim 16, wherein the formulation chamber, is coated with a resin that is inert to flunisolide.

18. An inhaler according to claim 17, wherein the resin is an epoxy resin.

19. An inhaler according to claim 16, wherein the aerosol canister is glass.