Long-acting drug combinations for the treatment of respiratory complaints

• US 20050004228A1
• Filed: 04/16/2004
• Published: 01/06/2005
• Est. Priority Date: 05/27/2003
• 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: Konetzki, Ingo
• Granted Patent: US 7,332,175 B2
• Time in Patent Office: Days
• US Class Current: 514/612
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 31/63 Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]

Abstract

A pharmaceutical composition comprising:

• • (a) an anticholinergic of formula 1
    wherein X⁻ is an anion with a single negative charge; and
  • (b) a compound of formula 2 or the pharmacologically acceptable acid addition salts, solvates, and hydrates thereof.

Claims

1. A pharmaceutical composition comprising:

(a) an anticholinergic of formula 1

wherein X⁻

is an anion with a single negative charge; and

(b) a compound of formula 2

or the pharmacologically acceptable acid addition salts, solvates, and hydrates thereof.

2. 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, orp-toluenesulfonate

3. The pharmaceutical composition according to claim 1, further comprising a physiologically acceptable excipient.

4. The pharmaceutical composition according to claim 1, wherein the compound 2 is a salt of hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, methanesulfonic acid, acetic acid, fumaric acid, succinic acid, lactic acid, citric acid, tartaric acid, 1-hydroxy-2-naphthalenecarboxylic acid, or maleic acid.

5. The pharmaceutical composition according to claim 1, wherein the compound 2 is an R-enantiomer.

6. The pharmaceutical composition according to one of claims 1 to 4, wherein the weight ratio of 1′

7. The pharmaceutical composition according to claim 6, wherein the weight ratio of 1′

to 2 (based on the free base) are in the range from about 1;

25 to about 200;

1.

8. The pharmaceutical composition according to one of claims 1 to 6, wherein the pharmaceutical composition is suitable for inhalation.

9. The pharmaceutical composition according to claim 8, wherein the pharmaceutical composition is an inhalable powder, propellant-driven metered dose aerosol, or propellant-free inhalable solution.

10. The pharmaceutical composition according to claim 8, wherein the pharmaceutical composition is an inhalable powder including a physiologically acceptable excipient selected from monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, salts, or mixtures thereof.

11. The pharmaceutical composition according to one of claims 1, 2, or 5, wherein the pharmaceutical composition is an inhalable powder containing the compounds 1 and 2 as its sole ingredients.

12. The pharmaceutical composition according to claim 8, wherein the pharmaceutical composition is a propellant-containing inhalable aerosol containing the compounds 1 and 2 in dissolved or dispersed form.

13. The propellant-containing inhalable aerosol according to claim 12, wherein the propellant gas is a hydrocarbon or halohydrocarbon.

14. The propellant-containing inhalable aerosol according to claim 12, wherein the propellant gas is n-propane, n-butane, or isobutane, or a chlorinated and/or fluorinated derivative of methane, ethane, propane, butane, cyclopropane, or cyclobutane, or a mixture thereof.

15. The propellant-containing inhalable aerosol according to claim 12, wherein the propellant gas is TG11, TG12, TG134a, TG227, or a mixture thereof.

16. The pharmaceutical composition according to claim 8, wherein the pharmaceutical composition is a propellant-free inhalable solution containing water, ethanol, or a mixture thereof as solvent.

17. The pharmaceutical composition according to claim 16, further comprising a cosolvent and/or excipient.