Aerosol formulation for inhalation comprising an anticholinergic

• US 7,611,694 B2
• Filed: 06/15/2006
• Issued: 11/03/2009
• Est. Priority Date: 08/14/2002
• Status: Expired due to Term

• Current Assignee: Boehringer Ingelheim Pharma GmbH & Company Kg (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim Pharma GmbH & Company Kg (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Schmidt, Friedrich
• Primary Examiner(s): Haghighatian; Mina
• Application Number:
  US11/424,541
• Publication Number:
  US 20060222598A1
• Time in Patent Office: 1,237 Days
• Field of Search: 424/45, 514/291, 514/826, 128/200.14
• US Class Current: 424/45
• CPC Class Codes: A61K 31/33 Heterocyclic compounds
• CPC Class Codes: A61K 31/4745 condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48
• CPC Class Codes: A61K 31/5375 1,4-Oxazines, e.g. morpholine
• 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

Abstract

The present invention relates to a propellant-free, aqueous aerosol formulation for anticholinergics of formula 1

wherein X⁻ denotes an anion.

Claims

1. An propellant-free aqueous pharmaceutical formulation for inhalation comprising at least one compound of formula 1 as the only active substance

2. The propellant-free aqueous pharmaceutical formulation according to claim 1 further comprising one or more pharmaceutically acceptable excipients or complexing agents or mixtures thereof.

3. The propellant-free aqueous pharmaceutical formulation according to claim 1, containing at least one compound of formula 1 wherein X⁻

is selected from the group consisting of chloride, bromide, 4-toluenesulphonate and methanesulphonate.

4. The propellant-free aqueous pharmaceutical formulation according to claim 1, wherein the pharmacologically acceptable acid is selected from the inorganic acids hydrochloric acid, hydrobromic acid, nitric acid, sulphuric acid and phosphoric acid or from the organic acids ascorbic acid, citric acid, malic acid, tartaric acid, maleic acid, succinic acid, fumaric acid, acetic acid, formic acid and propionic acid.

5. The propellant-free aqueous pharmaceutical formulation according to claim 3, characterised by a pH of 2.5 to 6.5.

6. The propellant-free aqueous pharmaceutical formulation according to claim 2, wherein the pharmaceutical excipient is benzalkonium chloride.

7. The propellant-free aqueous pharmaceutical formulation according to claim 6, characterised in that the content of benzalkonium chloride is from 1 to 50 mg per 100 ml of solution.

8. The propellant-free aqueous pharmaceutical formulation according to claim 1, characterised in that a pharmacologically active cation of the compound of 1 is present in the formulation in an amount of about 4 to 2000 mg per 100 ml of formulation.

9. The propellant-free aqueous pharmaceutical formulation according to claim 2, which comprises at least one complexing agent.

10. The propellant-free aqueous pharmaceutical formulation according to claim 9, characterised in that the content of the complexing agent is 5 to 20 mg per 100 ml of formulation.

11. The propellant-free aqueous pharmaceutical formulation according to claim 1 in an inhaler suitable for nebulising the formulation.