Anticholinergic powder formulations for inhalation

• US 20050226818A1
• Filed: 06/30/2004
• Published: 10/13/2005
• 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, Trunk, Michael
• Granted Patent: US 7,462,367 B2
• Time in Patent Office: Days
• US Class Current: 424/46
• 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 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles

Abstract

An inhalable powder comprising:
(a) an active substance consisting essentially of a compound of formula 1

• • wherein X⁻ is a pharmaceutically acceptable anion; and (b) a physiologically acceptable excipient having an average particle size of 10 μm to 50 μm, processes for preparing the inhalable powder, and methods of administration for the treatment of respiratory complaints, particularly for the treatment of chronic obstructive pulmonary disease (COPD) and asthma.

Claims

1. An inhalable powder comprising:

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

wherein X⁻

is a pharmaceutically acceptable anion; and

(b) a physiologically acceptable excipient having an average particle size of 10 μ

m to 50 μ

m.

2. The inhalable powder 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.

3. The inhalable powder according to claim 1, wherein the amount of active substance based on the pharmacologically active cation of formula 1

4. The inhalable powder according to claim 2, wherein the amount of active substance based on the pharmacologically active cation of formula 1′

5. The inhalable powder according to claim 1, wherein the physiologically acceptable excipient is selected from the monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, cyclodextrins, amino acids, or the salts thereof.

6. The inhalable powder according to claim 2, wherein the physiologically acceptable excipient is selected from the monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, cyclodextrins, amino acids, or the salts thereof.

7. The inhalable powder according to claim 3, wherein the physiologically acceptable excipient is selected from the monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, cyclodextrins, amino acids, or the salts thereof.

8. The inhalable powder according to claim 4, wherein the physiologically acceptable excipient is selected from the monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, cyclodextrins, amino acids, or the salts thereof.

9. The inhalable powder according to claim 1, wherein the excipient has an average particle size of 12 μ

m to 35 μ

m.

10. The inhalable powder according to claim 2, wherein the excipient has an average particle size of 12 μ

m to 35 μ

m.

11. The inhalable powder according to claim 3, wherein the excipient has an average particle size of 12 μ

m to 35 μ

m.

12. The inhalable powder according to claim 4, wherein the excipient has an average particle size of 12 μ

m to 35 μ

m.

13. The inhalable powder according to claim 5, wherein the excipient has an average particle size of 12 μ

m to 35 μ

m.

14. The inhalable powder according to claim 1, wherein the excipient has a 10% fine content of 0.5 μ

m to 6 μ

m.

15. The inhalable powder according to claim 2, wherein the excipient has a 10% fine content of 0.5 μ

m to 6 μ

m.

16. The inhalable powder according to claim 3, wherein the excipient has a 10% fine content of 0.5 μ

m to 6 μ

m.

17. The inhalable powder according to claim 4, wherein the excipient has a 10% fine content of 0.5 μ

m to 6 μ

m.

18. The inhalable powder according to claim 5, wherein the excipient has a 10% fine content of 0.5 μ

m to 6 μ

m.

19. The inhalable powder according to claim 9, wherein the excipient has a 10% fine content of 0.5 μ

m to 6 μ

m.

20. The inhalable powder according to claim 1, wherein the excipient has a specific surface area of 0.1 m²/g to 2 m²/g.

21. The inhalable powder according to claim 2, wherein the excipient has a specific surface area of 0.1 m²/g to 2 m²/g.

22. The inhalable powder according to claim 3, wherein the excipient has a specific surface area of 0.1 m²/g to 2 m²/g.

23. The inhalable powder according to claim 4, wherein the excipient has a specific surface area of 0.1 m²/g to 2 m²/g.

24. The inhalable powder according to claim 5, wherein the excipient has a specific surface area of 0.1 m²/g to 2 m²/g.

25. The inhalable powder according to claim 9, wherein the excipient has a specific surface area of 0.1 m²/g to 2 m²/g.

26. The inhalable powder according to claim 19, wherein the excipient has a specific surface area of 0.1 m²/g to 2 m²/g.

27. A capsule containing the inhalable powder according to one of claims 1, 2, 3, 4, 5, 9, 13, 14, 18, 19, 20, 25, or 26.

28. A capsule according to claim 27, wherein the capsule material comprises synthetic plastics.

29. A kit comprising a capsule according to claim 27, and an inhaler for administering the inhalable powder from the capsule.

30. A kit comprising a capsule according to claim 27, and an Hochrainer-Kinnear inhaler for administering the inhalable powder from the capsule.