Levalbuterol salt

1. Levalbuterol L-tartrate.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 15, 17)
- - 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.
  - 15. A metered dose inhaler comprising a canister containing an aerosol formulation as defined in claim 7, 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.

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.
- View Dependent Claims (13, 14, 16)
- - 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.
  - 16. A metered dose inhaler comprising a canister containing an aerosol formulation as defined in claim 12, a metering valve and a valve stem.

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.
- View Dependent Claims (19, 20, 21, 22, 23, 25)
- - 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.
  - 25. Levalbuterol L-tartrate crystals obtained by the process of claim 18.

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.
- View Dependent Claims (26)
- - 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.
- View Dependent Claims (28, 29)
- - 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.

Specification

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Litigation Campaign Assessment

Litigation Data

Current Assignee
Lupin Inc. (Lupin Limited)
Original Assignee
Sepracor Incorporated
Inventors
McGlynn, Paul, Sturge, Craig, Bakale, Roger
Primary Examiner(s)
PUTTLITZ, KARL J

Application Number

US10/728,873
Publication Number

US 20040115136A1
Time in Patent Office

1,345 Days
Field of Search

564/305, 564/463, 564/355, 568/700, 568/704, 568/705, 568/715, 568/717, 568/763, 568/840
US Class Current

564/355
CPC Class Codes

A61K 31/205   Amine addition salts of org...

A61K 9/008   comprising drug dissolved o...

A61K 9/14   Particulate form, e.g. powd...

A61M 15/002   with air flow regulating means

A61M 15/009   using medicine packages wit...

A61M 2202/0484   Alcohol

A61M 2202/0488   Surfactant, e.g. for the lung

A61M 2202/064   Powder

A61P 11/00   Drugs for disorders of the ...

A61P 11/06   Antiasthmatics

A61P 11/08   Bronchodilators

C07B 2200/07   Optical isomers

C07B 2200/13   Crystalline forms, e.g. pol...

C07C 215/60   the chain having two carbon...

C07C 59/255   Tartaric acid

C09K 3/30   for aerosols aerosol contai...

Levalbuterol salt

First Claim

5 Assignments

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Abstract

10 Citations

29 Claims

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Levalbuterol salt

First Claim

5 Assignments

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Litigations

0 Petitions

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Accused Products

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Abstract

10 Citations

29 Claims

Specification

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Solutions

Use Cases

Quick Links