Aerosol formulation for inhalation comprising an anticholinergic

• US 7,579,358 B2
• Filed: 09/07/2004
• Issued: 08/25/2009
• Est. Priority Date: 09/26/2003
• Status: Active Grant

• 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: Boeck, Georg, Schmidt, Friedrich
• Primary Examiner(s): Richter; Johann R
• Assistant Examiner(s): ALSTRUM ACEVEDO, JAMES HENRY
• Application Number:
  US10/935,502
• Publication Number:
  US 20050101625A1
• Time in Patent Office: 1,813 Days
• Field of Search: None
• US Class Current: 514/291
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• 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 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

A pharmaceutical composition comprising:

• • (a) an active substance consisting of a compound of formula 1

wherein X⁻ is an anion;

• • (b) ethanol or a mixture of ethanol and water;
  • (c) a pharmacologically acceptable acid.

Claims

1. A pharmaceutical composition comprising:

(a) an active substance consisting of a compound of formula 1

2. The pharmaceutical composition according to claim 1, further comprising a pharmacologically acceptable excipient or complexing agent.

3. The pharmaceutical composition according to claim 1, wherein X⁻

is chloride, bromide, iodide, sulfate, phosphate, methanesulfonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate, or p-toluenesulfonate.

4. The pharmaceutical composition according to claim 1, wherein X⁻

is chloride, bromide, p-toluenesulfonate, or methanesulfonate.

5. The pharmaceutical composition according to claim 1, wherein component (b) is a mixture of ethanol and water.

6. The pharmaceutical composition according to claim 5, wherein the proportion by mass of ethanol in component (b) is in the range from 5% to 99%.

7. The pharmaceutical composition according to claim 5, wherein the proportion by mass of ethanol in component (b) is in the range from 10% to 96%.

8. The pharmaceutical composition according to one of claims 1 to 7, wherein the pharmacologically acceptable acid is hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, ascorbic acid, citric acid, malic acid, tartaric acid, maleic acid, succinic acid, fumaric acid, acetic acid, formic acid, or propionic acid.

9. The pharmaceutical composition according to one of claims 1 to 7, wherein the content of 1'"'"' is about 4 mg to 2000 mg per 100 mL of the composition.

10. The pharmaceutical composition according to claim 1, further comprising a complexing agent.

11. The pharmaceutical composition according to claim 10, wherein the amount of complexing agent is 1 mg to 100 mg per 100 mL of solution.

12. The pharmaceutical composition according to claim 1, further comprising benzalkonium chloride.

13. The pharmaceutical composition according to claim 10, wherein the amount of benzalkonium chloride is 1 mg to 50 mg per 100 mL of solution.

14. The pharmaceutical composition according to claim 1, wherein the composition has a pH from 3.0 to 5.0.

15. The pharmaceutical composition according to claim 14, wherein the composition has a pH from 3.5 to 4.5.

16. A nebulizer containing the pharmaceutical composition according to one of claims 1 to 7.