HFC solution formulations containing an anticholinergic

• US 20050008578A1
• Filed: 07/01/2004
• Published: 01/13/2005
• Est. Priority Date: 07/11/2003
• 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: Schmidt, Friedrich
• Granted Patent: US 7,273,603 B2
• Time in Patent Office: Days
• US Class Current: 424/45
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• 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 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• CPC Class Codes: A61K 9/124 characterised by the propellant
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

An aerosol solution formulation comprising:
(a) a salt of formula 1

• • wherein X⁻ is an anion (b) an HFC propellant; (c) a cosolvent; and (d) an inorganic or an organic acid, wherein the concentration of the acid is in a range that corresponds with a pH range of 2.5 to 5.5 in aqueous solution.

Claims

1. An aerosol solution formulation comprising:

(a) a salt of formula 1

wherein X⁻

is an anion

(b) an HFC propellant;

(c) a cosolvent; and

(d) an inorganic or an organic acid, wherein the concentration of the acid is in a range that corresponds with a pH range of 2.5 to 5.5 in aqueous solution.

2. The aerosol solution formulation according to claim 1, wherein X⁻

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

3. The aerosol solution formulation according to claim 1, wherein the aerosol solution formulation contains 0.00008% to 4% of the pharmacologically active cation of formula 1′

4. The aerosol solution formulation according to claim 1, wherein the HFC propellant is HFC-134(a), HFC-227, HFC-32, HFC-143(a), HFC-134, HFC-152a, or a mixture thereof.

5. The aerosol solution formulation according to claim 2, wherein the HFC propellant is HFC-134(a), HFC-227, HFC-32, HFC-143(a), HFC-134, HFC-152a, or a mixture thereof.

6. The aerosol solution formulation according to claim 3, wherein the HFC propellant is HFC-134(a), HFC-227, HFC-32, HFC-143(a), HFC-134, HFC-152a, or a mixture thereof.

7. The aerosol solution formulation according to claim 1, wherein the acid is hydrochloric acid, sulfuric acid, nitric acid, or phosphoric acid.

8. The aerosol solution formulation according to claim 2, wherein the acid is hydrochloric acid, sulfuric acid, nitric acid, or phosphoric acid.

9. The aerosol solution formulation according to claim 3, wherein the acid is hydrochloric acid, sulfuric acid, nitric acid, or phosphoric acid.

10. The aerosol solution formulation according to claim 1, wherein the acid is ascorbic acid, citric acid, lactic acid, malic acid, benzoic acid, or tartaric acid.

11. The aerosol solution formulation according to claim 2, wherein the acid is ascorbic acid, citric acid, lactic acid, malic acid, benzoic acid, or tartaric acid.

12. The aerosol solution formulation according to claim 3, wherein the acid is ascorbic acid, citric acid, lactic acid, malic acid, benzoic acid, or tartaric acid.

13. The aerosol solution formulation according to claim 1, wherein the aerosol solution formulation contains water in an amount of up to about 5%.

14. The aerosol solution formulation according to claim 2, wherein the aerosol solution formulation contains water in an amount of up to about 5%.

15. The aerosol solution formulation according to claim 3, wherein the aerosol solution formulation contains water in an amount of up to about 5%.

16. The aerosol solution formulation according to claim 1, wherein the cosolvent is an alcohol, glycol, glycol ether, block copolymer of oxyethylene and oxypropylene, glycerol, polyoxyethylene alcohol, polyoxyethylene fatty acid ester, or glycofurol.

17. The aerosol solution formulation according to claim 2, wherein the cosolvent is an alcohol, glycol, glycol ether, block copolymer of oxyethylene and oxypropylene, glycerol, polyoxyethylene alcohol, polyoxyethylene fatty acid ester, or glycofurol.

18. The aerosol solution formulation according to claim 3, wherein the cosolvent is an alcohol, glycol, glycol ether, block copolymer of oxyethylene and oxypropylene, glycerol, polyoxyethylene alcohol, polyoxyethylene fatty acid ester, or glycofurol.

19. The aerosol solution formulation according to claim 1, wherein the cosolvent is present in an amount in the range of 5% to 50% (w/w).

20. The aerosol solution formulation according to claim 16, wherein the cosolvent is present in an amount in the range of 5% to 50% (w/w).

21. The aerosol solution formulation according to claim 17, wherein the cosolvent is present in an amount in the range of 5% to 50% (w/w).

22. The aerosol solution formulation according to claim 18, wherein the cosolvent is present in an amount in the range of 5% to 50% (w/w).

23. The aerosol solution formulation according to claim 1, wherein the aerosol solution formulation contains no water.

24. The aerosol solution formulation according to claim 2, wherein the aerosol solution formulation contains no water.

25. The aerosol solution formulation according to claim 3, wherein the aerosol solution formulation contains no water.