Claims for Patent: 7,256,310

Summary for Patent: 7,256,310

Title:	Levalbuterol salt
Abstract:	Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
Inventor(s):	McGlynn; Paul (Marlborough, MA), Bakale; Roger (Shrewsbury, MA), Sturge; Craig (Falmouth, CA)
Assignee:	Sepracor Inc. (Marlborough, MA)
Application Number:	10/728,873
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,256,310
Patent Claims:	1. Levalbuterol L-tartrate. 2. Levalbuterol L-tartrate as claimed in claim 1, which is in crystalline form. 3. Levalbuterol L-tartrate as claimed in claim 2, containing from 0.3 to 0.7% ethanol. 4. Levalbuterol L-tartrate as claimed in claim 2, which is in micronized form. 5. Levalbuterol L-tartrate as claimed in claim 4, which is in the form of needle-like particles. 6. A pharmaceutical composition, which comprises levalbuterol L-tartrate as claimed in claim 1, together with a pharmaceutically acceptable carrier. 7. A pharmaceutical composition as claimed in claim 6, which is an aerosol formulation adapted for administration using a metered dose inhaler, the aerosol formulation comprising levalbuterol L-tartrate in crystalline form and a propellant. 8. A pharmaceutical composition as claimed in claim 7, in which the propellant is 1,1,1,2-tetrafluoroethane. 9. A pharmaceutical composition as claimed in claim 7, which further comprises a surfactant. 10. A pharmaceutical composition as claimed in claim 7, which further comprises a co-solvent. 11. A pharmaceutical composition as claimed in claim 10, in which the co-solvent is ethanol. 12. An aerosol formulation adapted for administration using a metered dose inhaler, the aerosol formulation comprising levalbuterol L-tartrate crystals in the form of micronized, needle-like particles, and a propellant. 13. An aerosol formulation as claimed in claim 12, in which the propellant is 1,1,1,2-tetrafluoroethane. 14. An aerosol formulation as claimed in claim 13, which further comprises from 2 to 6% by weight of ethanol as a co-solvent. 15. A metered dose inhaler comprising a canister containing an aerosol formulation as defined in claim 7, a metering valve and a valve stem. 16. A metered dose inhaler comprising a canister containing an aerosol formulation as defined in claim 12, a metering valve and a valve stem. 17. A pharmaceutical composition as claimed in claim 6, which is adapted for administration using a dry powder inhaler or insufflator. 18. A process for the preparation of levalbuterol L-tartrate crystals, which comprises combining a solution of levalbuterol with a solution of L-tartaric acid and recovering levalbuterol L-tartrate crystals. 19. A process as claimed in claim 18, in which the solvent in each solution comprises ethanol. 20. A process as claimed in claim 18, in which the crystallization conditions are selected so as to provide crystals having a length of 10 to 50 microns and a width of 0.2 to 4 microns. 21. A process as claimed in claim 18, in which the levalbuterol has been prepared by hydrogenating R-benzylalbuterol in the presence of palladium on carbon. 22. A process as claimed in claim 21, in which the hydrogenation has been conducted under conditions selected to effect conversion of at least 99.9% of the R-benzylalbuterol without over reduction of other functional groups. 23. A process as claimed in claim 18, in which the crystals are dried and micronized, the crystallization and drying conditions being selected so as to afford needle-like particles after micronization. 24. A process for the preparation of levalbuterol L-tartrate crystals, which comprises combining a solution of levalbuterol with a solution of L-tartaric acid, recovering levalbuterol L-tartrate crystals, and then drying and micronizing the recovered crystals, the crystallization and drying conditions being selected so as to afford needle-like particles after micronization. 25. Levalbuterol L-tartrate crystals obtained by the process of claim 18. 26. Levalbuterol L-tartrate crystals obtained by the process of claim 24. 27. A method of effecting bronchodilation in a patient in need of treatment, which comprises administering to said patient an effective amount of levalbuterol L-tartrate. 28. A method as claimed in claim 27, in which micronized crystals of levalbuterol L-tartrate are administered by inhalation using a metered dose inhaler. 29. A method as claimed in claim 28, in which the micronized crystals of levalbuterol L-tartrate are in the form of needle-like particles.