Capsules Containing Inhalable Tiotropium

• US 20090137621A1
• Filed: 10/09/2008
• Published: 05/28/2009
• Est. Priority Date: 06/01/2001
• Status: Abandoned Application

• Current Assignee: Boehringer Ingelheim Pharmaceuticals Incorporated (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim Pharmaceuticals Incorporated (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Trunk, Michael, Bechtold-Peters, Karoline, Hochrainer, Dieter, Walz, Michael
• Application Number:
  US12/248,574
• Publication Number:
  US 20090137621A1
• Time in Patent Office: Days
• US Class Current: 514/291
• CPC Class Codes: A61K 31/451 having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• CPC Class Codes: A61K 31/4523 containing further heterocyclic ring systems
• 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 9/4816 Wall or shell material
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61M 11/003 by passing the aerosol trough sieves or filters
• CPC Class Codes: A61M 15/0028 using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up
• CPC Class Codes: A61M 15/0033 Details of the piercing or cutting means
• CPC Class Codes: A61M 2202/064 Powder

Abstract

The invention relates to capsules for inhalation (inhalettes) made from specific capsule materials with a reduced moisture content, which contain the active substance tiotropium in the form of powdered preparations and are characterised by increased stability.

Claims

1. A capsule for inhalation which contains as an inhalable powder a mixture consisting of tiotropium salt and a physiologically acceptable excipient selected from the group consisting of lactose, glucose and mixtures thereof, wherein the material forming the capsule is a synthetic plastic and has a TEWS or halogen drier moisture content of less than 3% by weight.

15. A capsule for inhalation according to claim 1, wherein the material forming the capsule is selected from the group consisting of polyethylene, polycarbonate, polyester, polypropylene and polyethylene terephthalate.

16. A capsule for inhalation according to claim 15, wherein the material forming the capsule is selected from the group consisting of polyethylene, polycarbonate and polyethylene terephthalate.

18. A capsule for inhalation according to claim 1, 15, or 16, wherein the material forming the capsule has a TEWS or halogen drier moisture content of ≦

1% by weight.

21. A capsule for inhalation according to claim 1, wherein the inhalable powder contains 0.001 to 2% tiotropium by weight.

22. A capsule for inhalation according to claim 21, wherein the excipient consists of a mixture of coarser excipient with an average particle size of 15 to 80 μ

m and finer excipient with an average particle size of 1 to 9 μ

m, the proportion of finer excipient in the total quantity of excipient being 1 to 20% by weight.

23. A capsule for inhalation according to claim 22, wherein the tiotropium salt is in the form of its chloride, bromide, iodide, methanesulphonate, para-toluenesulphonate or methylsulphate salt.

24. An inhaler suitable for administering inhalable powders containing a capsule for inhalation according to claim 1.

25. A method of treating asthma or chronic obstructive pulmonary disease (COPD) in a patient in need thereof comprising administering to said patient an inhalable powder using an inhaler according to claim 24.

26. A method of making a capsule for inhalation according to claim 1 comprising drying the capsule to a TEWS or halogen drier moisture content of less than 3% and filling an capsule with the mixture of tiotropium with the physiologically acceptable excipient.

27. The capsule according to claim 1, wherein the tiotropium is a bromide salt.

28. The capsule according to claim 1, wherein the physiologically acceptable excipient is lactose.

29. The capsule according to claim 1, wherein the physiologically acceptable excipient is lactose monohydrate.

30. The capsule according to claim 1, wherein the synthetic plastic is polyethylene.

31. The capsule according to claim 28, wherein the material forming the capsule has a TEWS or halogen drier moisture content of ≦

1% by weight.

32. The capsule according to claim 28, wherein the polyethylene has a density of between 900 and 1000 kg/m³.

33. The capsule according to claim 30, wherein the polyethylene has a density of between 940 and 980 kg/m³.

34. The capsule according to claim 28, wherein the polyethylene has a density of 960 kg/m³.

2-14. -14. (canceled)

17. (canceled)

19-20. -20. (canceled)