Levalbuterol salt

• US 20080119564A1
• Filed: 08/08/2007
• Published: 05/22/2008
• Est. Priority Date: 12/10/2002
• Status: Abandoned Application

• Current Assignee: Sunovion Pharmaceuticals Inc. (Sumitomo Chemical Company Limited)
• Original Assignee: Sunovion Pharmaceuticals Inc. (Sumitomo Chemical Company Limited)
• Inventors: McGlynn, Paul, Sturge, Craig, Bakale, Roger
• Application Number:
  US11/891,048
• Publication Number:
  US 20080119564A1
• Time in Patent Office: Days
• US Class Current: 514/653
• CPC Class Codes: A61K 31/205 Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• 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 9/14 Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51
• CPC Class Codes: A61M 15/002 with air flow regulating means
• CPC Class Codes: A61M 15/009 using medicine packages with incorporated spraying means, e.g. aerosol cans pocket atomiser of the injector type A61M11/08
• CPC Class Codes: A61M 2202/0484 Alcohol
• CPC Class Codes: A61M 2202/0488 Surfactant, e.g. for the lung
• CPC Class Codes: A61M 2202/064 Powder
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: C07B 2200/07 Optical isomers
• CPC Class Codes: C07B 2200/13 Crystalline forms, e.g. polymorphs
• CPC Class Codes: C07C 215/60 the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• CPC Class Codes: C07C 59/255 Tartaric acid
• CPC Class Codes: C09K 3/30 for aerosols aerosol containers B65D83/14

Abstract

Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.

Claims

1-29. -29. (canceled)

30. Levalbuterol L-tartrate, which is a hemitartrate.

31. A pharmaceutical composition comprising the levalbuterol L-tartrate of claim 30.

32. The pharmaceutical composition of claim 31, which further comprises a propellant.

33. The pharmaceutical composition of claim 32, wherein the propellant is 1,1,1,2-tetrafluoroethane.

34. The pharmaceutical composition of claim 31, which further comprises a surfactant.

35. The pharmaceutical composition of claim 34, wherein the surfactant is oleic acid.

36. The pharmaceutical composition of claim 31, which further comprises a co-solvent.

37. The pharmaceutical composition of claim 36, wherein the co-solvent is ethanol.

38. The pharmaceutical composition of claim 37, wherein the ethanol is dehydrated ethanol.

39. The pharmaceutical composition of claim 31, which is adapted for administration by inhalation using a metered dose inhaler.

40. The pharmaceutical composition of claim 39, which is adapted for administration of from about 45 μ

g to about 90 μ

g levalbuterol free base per actuation.

41. A pharmaceutical composition comprising levalbuterol L-tartrate, 1,1,1,2-tetrafluoroethane, oleic acid, and ethanol.

42. The pharmaceutical composition of claim 41, wherein the ethanol is dehydrated ethanol.

43. The pharmaceutical composition of claim 42, which is adapted for administration by inhalation using a metered dose inhaler.

44. The pharmaceutical composition of claim 43, wherein one gram of the composition contains about 1.04 mg of levalbuterol L-tartrate, about 0.951 g of 1,1,1,2-tetrafluoroethane, about 0.0521 mg of oleic acid, and about 0.0476 g of dehydrated ethanol.

45. The pharmaceutical composition of claim 43, wherein one gram of the composition contains about 2.08 mg of levalbuterol L-tartrate, about 0.95 g of 1,1,1,2-tetrafluoroethane, about 0.104 mg of oleic acid, and about 0.0475 g of dehydrated ethanol.