Capsules containing inhalable tiotropium

• US 20030070679A1
• Filed: 05/31/2002
• Published: 04/17/2003
• Est. Priority Date: 06/01/2001
• Status: Abandoned Application

• Current Assignee: Boehringer Ingelheim Pharma GmbH & Company Kg (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim Pharmaceuticals Incorporated (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Hochrainer, Dieter, Bechtold-Peters, Karoline
• Application Number:
  US10/159,451
• Publication Number:
  US 20030070679A1
• Time in Patent Office: Days
• US Class Current: 128/203.15
• 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 of tiotropium with at least one physiologically acceptable excipient, wherein the material forming the capsule has a TEWS or halogen drier moisture of content of less than 15%.

2. ) A capsule for inhalation according to claim 1, wherein the material forming the capsule is selected from gelatine, cellulose derivatives, starch, starch derivatives, chitosan and synthetic plastics.

3. ) A capsule for inhalation according to claim 1, wherein the material forming the capsule is a mixture of gelatine with at least one other additive selected from PEG, glycerol, sorbitol, propyleneglycol, PEO-PPO block copolymer, a polyalcohol and a polyether.

4. ) A capsule for inhalation according to claim 3, wherein the material forming the capsule contains, in addition to gelatine, PEG in an amount of 1-10% by weight.

5. ) A capsule for inhalation according to claim 3, wherein the material forming the capsule contains, in addition to gelatine, PEG in an amount of 3-8% by weight.

6. ) A capsule for inhalation according to claim 3, wherein the material forming the capsule has a TEWS or halogen drier moisture content of less than 12%.

7. ) A capsule for inhalation according to claim 3, wherein the material forming the capsule has a TEWS or halogen drier moisture content of ≦

10%.

8. ) A capsule for inhalation according to claim 4, wherein the material forming the capsule has a TEWS or halogen drier moisture content of less than 12%.

9. ) A capsule for inhalation according to claim 4, wherein the material forming the capsule has a TEWS or halogen drier moisture content of ≦

10%.

10. ) A capsule for inhalation according to claim 5, wherein the material forming the capsule has a TEWS or halogen drier moisture content of less than 12%.

11. ) A capsule for inhalation according to claim 5, wherein the material forming the capsule has a TEWS or halogen drier moisture content of ≦

10%.

12. ) A capsule for inhalation according to claim 2, wherein the material forming the capsule is selected from hydroxypropylmethylcellulose, hydroxypropylcellulose, methylcellulose, hydroxymethylcellulose and hydroxyethylcellulose.

13. ) A capsule for inhalation according to claim 12, wherein the material forming the capsule has a TEWS or halogen drier moisture content of less than 8%.

14. ) A capsule for inhalation according to claim 12, wherein the material forming the capsule has a TEWS or halogen drier moisture content of ≦

5%.

15. ) A capsule for inhalation according to claim 2, wherein the material forming the capsule is selected from 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 polyethylene, polycarbonate and polyethylene terephthalate.

17. ) A capsule for inhalation according to claim 15, wherein the material forming the capsule has a TEWS or halogen drier moisture content of less than 3%.

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

1%.

19. ) A capsule for inhalation according to claim 16, wherein the material forming the capsule has a TEWS or halogen drier moisture content of less than 3%.

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

1%.

21. ) A capsule for inhalation according to claim 1, wherein the inhalable powder contains a mixture of at least one physiologically acceptable excipient with 0.001 to 2% tiotropium.

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%.

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

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

25. ) A method of treating asthma or 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 filling an empty capsule having a TEWS or halogen drier moisture content of less than 15% with a mixture of tiotropium with at least one physiologically acceptable excipient.