AEROSOL FORMULATION FOR THE INHALATION OF BETA AGONISTS

• US 20120058980A1
• Filed: 11/11/2011
• Published: 03/08/2012
• Est. Priority Date: 08/18/2006
• Status: Abandoned Application

• Current Assignee: Boehringer Ingelheim International GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim International GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: RADAU, Kirsten, AVEN, Michael, WEITZEL, Rainer
• Application Number:
  US13/294,449
• Publication Number:
  US 20120058980A1
• Time in Patent Office: Days
• US Class Current: 514/171
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 9/0078 for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
• 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: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 33/10 Anthelmintics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14

Abstract

The present invention relates to a propellant-free aerosol formulation which contains one or more compounds of general formula 1,

wherein the groups R¹, R², R³ and X⁻ may have the meanings indicated in the claims and in the specification, and two further active substances 2 and 3, for inhalation.

Claims

1. Medicament formulation comprising:

as active substance a compound of the formula 1

2. Medicament formulation according to claim 1, wherein X⁻

is chloride.

3. Medicament formulation according to claim 1, further comprising:

pharmacologically acceptable excipients; and

ethanol or a mixture of water and ethanol as the solvent.

4. Medicament formulation according to claim 1, wherein one or more said active substance is in the form of the tautomers, enantiomers, mixtures of the enantiomers, racemates, solvates or hydrates thereof.

16. Medicament formulation according to claim 1, wherein the pharmacologically acceptable acid is selected from the group consisting of the inorganic acids hydrochloric acid, phosphoric acid, hydrobromic acid, nitric acid and sulphuric acid or from the group consisting of the organic acids ascorbic acid, citric acid, malic acid, tartaric acid, maleic acid, succinic acid, fumaric acid, acetic acid, formic acid, propionic acid, sorbic acid, benzoic acid, methanesulphonic acid and benzenesulphonic acid.

17. Medicament formulation according to claim 1, wherein the pH of said formulation is 2.0 to 6.5.

18. Medicament formulation according to claim 1, wherein the content of 1, 2 and 3 independently of one another is about 0.5 to 6000 mg per 100 ml solution in each case.

19. Medicament formulation according to claim 1, wherein said formulation comprises a complexing agent as a further pharmacologically acceptable excipient.

20. Medicament formulation according to claim 19, wherein the content of complexing agent is 0.1 to 200 mg per 100 ml solution.

23. Medicament formulation according to claim 1, wherein said formulation comprises a mixture of water and ethanol as solvent.

24. Medicament formulation according to claim 1, wherein said formulation comprises benzylalcohol, γ

-butyrolactone or diethyleneglycol monoethylether as co-solvent.

25. Medicament formulation according to claim 23, wherein said formulation comprises as solvent a mixture of water and ethanol in which the percentage amount of ethanol by volume is in the range between 30 and 99% ethanol.

33. A method of treating respiratory complaints comprising administering to a patient in need thereof a therapeutically effective amount of a medicament formulation according to claim 1.

34. Inhalation kit consisting of a medicament formulation according to claim 1 and an inhaler suitable for nebulising the medicament formulation.

5-15. -15. (canceled)

21-22. -22. (canceled)

26. Medicament formulation comprising:

as active substance a free base of formula 1′

27. Medicament formulation according to claim 26, further comprising:

pharmacologically acceptable excipients; and

ethanol or a mixture of water and ethanol as the solvent.

28. Medicament formulation according to claim 26, wherein one or more of said active substances is in the form of the tautomers, enantiomers, mixtures of the enantiomers, racemates, solvates or hydrates thereof.

29-31. -31. (canceled)

35. (canceled)