Medicaments comprising steroids and a novel anticholinergic

• US 20060276441A1
• Filed: 04/20/2006
• Published: 12/07/2006
• Est. Priority Date: 04/12/2002
• Status: Active Grant

• 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: Pairet, Michel, Pieper, Michael P., Meade, Christopher John Montague, Meissner, Helmut, Banholzer, Rolf, Speck, Georg, Pohl, Gerald, Morschhaeuser, Gerd, Reichl, Richard
• Granted Patent: US 7,851,483 B2
• Time in Patent Office: Days
• US Class Current: 514/171
• 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 31/4745 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 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/70 Carbohydrates; Sugars; Derivatives thereof sorbitol A61K31/047
• 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) a salt of formula 1 wherein:
X⁻ is an anion with a single negative charge; and (b) a steroid 2, processes for preparing such pharmaceutical composition, and their use in the treatment of respiratory complaints.

Claims

1. A method of treating a pulmonary disease in a patient in need thereof, the method comprising administering an effective amount of:

(a) a salt of formula 1

wherein X⁻

is an anion with a single negative charge; and

(b) a steroid 2.

2. The method according to claim 1, wherein the pulmonary disease is asthma or COPD.

3. The method according to claim 1, wherein the salt of formula 1 and the steroid 2 are in the form of a pharmaceutical composition.

4. The method according to claim 2, wherein the salt of formula 1 and the steroid 2 are in the form of a pharmaceutical composition.

5. The method according to claim 1, wherein a salt of formula 1 and the steroid 2 are administered once a day.

6. The method according to claim 2, wherein a salt of formula 1 and the steroid 2 are administered once a day.

7. The method according to claim 3, wherein the pharmaceutical composition is administered once a day.

8. The method according to claim 4, wherein the pharmaceutical composition is administered once a day.

9. The method according to claim 1, wherein X⁻

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

10. The method according to claim 1, wherein the steroid 2 is selected from flunisolide, beclomethasone, triamcinolone, budesonide, fluticasone, mometasone, ciclesonide, rofleponide, ST-126, and dexamethasone.

11. The method according to claim 10, wherein the steroid 2 is selected from budesonide, fluticasone, mometasone, ciclesonide, and ST-126.

12. The method according to claim 1, wherein the salt of formula 1 and the steroid 2 are administered by inhalation.

13. The method according to claim 2, wherein the salt of formula 1 and the steroid 2 are administered by inhalation.

14. The method according to claim 3, wherein the pharmaceutical composition is administered by inhalation.

15. The method according to claim 4, wherein the pharmaceutical composition is administered by inhalation.

16. The method according to claim 14, wherein the pharmaceutical composition is an inhalable powder, a propellant-containing metered-dose aerosol, or a propellant-free inhalable solution or suspension.

17. The method according to claim 15, wherein the pharmaceutical composition is an inhalable powder, a propellant-containing metered-dose aerosol, or a propellant-free inhalable solution or suspension.

18. The method according to claim 16, wherein the pharmaceutical composition is an inhalable powder comprising the salt of formula 1′

and the steroid 2 in admixture with a physiologically acceptable excipient selected from monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, salts, or mixtures thereof.

19. The method according to claim 17, wherein the pharmaceutical composition is an inhalable powder comprising the salt of formula 1′

and the steroid 2 in admixture with a physiologically acceptable excipient selected from monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, salts, or mixtures thereof.

20. The method according to claim 18, wherein the excipient has a maximum average particle size of 250 μ

m or less.

21. The method according to claim 19, wherein the excipient has a maximum average particle size of 250 μ

m or less.

22. The method according to claim 20, wherein the excipient has a maximum average particle size of between 10 μ

m and 150 μ

m.

23. The method according to claim 21, wherein the excipient has a maximum average particle size of between 10 μ

m and 150 μ

m.

24. The method according to claim 16, wherein the pharmaceutical composition is a propellant-containing metered-dose aerosol comprising the salt of formula 1′

and the steroid 2 in dissolved or dispersed form.

25. The method according to claim 17, wherein the pharmaceutical composition is a propellant-containing metered-dose aerosol comprising the salt of formula 1′

and the steroid 2 in dissolved or dispersed form.

26. The method according to claim 24, wherein the propellant gas is a hydrocarbon or halohydrocarbon.

27. The method according to claim 25, wherein the propellant gas is a hydrocarbon or halohydrocarbon.

28. The method according to claim 16, wherein the pharmaceutical composition is a propellant-free inhalable solution or suspension further comprising a solvent selected from water, ethanol, or a mixture thereof.

29. The method according to claim 17, wherein the pharmaceutical composition is a propellant-free inhalable solution or suspension further comprising a solvent selected from water, ethanol, or a mixture thereof.