Inhalant Propellant-Free Aerosol Formulation

• US 20090197841A1
• Filed: 05/09/2007
• Published: 08/06/2009
• Est. Priority Date: 05/20/2006
• 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: Kreher, Christoph, Spallek, Michael
• Application Number:
  US12/301,292
• Publication Number:
  US 20090197841A1
• Time in Patent Office: Days
• US Class Current: 514/169
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/439 the ring forming part of a bridged ring system, e.g. quinuclidine 8-azabicyclo [3.2.1] octanes A61K31/46
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 31/47 Quinolines; Isoquinolines
• CPC Class Codes: A61K 47/02 Inorganic compounds
• 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 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• 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: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61K 9/124 characterised by the propellant
• 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 11/16 Central respiratory analeptics

Abstract

The invention relates to inhalant propellant-free aerosol formulations containing at least one inert, non-volatile auxiliary substance for adjusting defined droplet sizes.

Claims

1-10. -10. (canceled)

11. Solution formulation for inhalation which contain one or more active substances in a solvent selected from among water, ethanol and water-ethanol mixtures;

and

at least one inert, non-volatile excipient in an amount such that the total concentration of non-volatile constituents in the formulation is ≧

3 wt. %.

12. Solution formulation according to claim 11, characterised in that the one or more active substances is selected from anticholinergics, betamimetics, corticosteroids, PDE4-inhibitors, LTD4-antagonists, dopamine agonists and H1-antihistamines.

13. Solution formulation according to claim 11, characterised in the at least one inert, non-volatile excipients is a preservatives or a complexing agent.

14. Solution formulation according to claim 11, characterised in that the at least one inert, non-volatile excipient is selected from monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, or a salt thereof.

15. Solution formulation according to claim 11, characterised in that the total concentration of non-volatile constituents in the formulation is ≧

5 wt. %.

16. Solution formulation according to claim 11, characterised in that the total concentration of non-volatile constituents in the formulation is ≧

10 wt. %.

17. Solution formulation according to claim 11, characterised in that the solvent contains pure water.

18. Solution formulation according to claim 11, characterised in that the solvent contains ethanol or mixtures of ethanol and water.

19. Solution formulation according to claim 18, characterised in that the solvent contains a mixture of ethanol and water, wherein the percentage proportion of ethanol by weight is in the range between 5 and 99%.

20. Solution formulation according to claim 18, characterised in that the solvent contains a mixture of ethanol and water, wherein the percentage proportion of ethanol by weight is in the range between 10 to 96%.

21. Solution formulation according to claim 11, characterised in that the pH of the formulation is in the range from 2.0 to 6.5.

22. Use of a solution formulation according to claim 11 for the treatment of a respiratory complaint selected from obstructive pulmonary diseases of various origins, pulmonary emphysema of various origins, restrictive pulmonary diseases, interstitial pulmonary diseases, cystic fibrosis, bronchitis of various origins, bronchiectasis, adult respiratory distress syndrome, and all forms of pulmonary oedema.