.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 7,070,800

« Back to Dashboard

Claims for Patent: 7,070,800

Title:Inhalable powder containing tiotropium
Abstract:The invention relates to powdered preparations containing tiotropium for inhalation, processes for preparing them as well as their use in preparing a pharmaceutical composition for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.
Inventor(s): Bechtold-Peters; Karoline (Biberach, DE), Walz; Michael (Bingen, DE), Boeck; Georg (Mainz, DE), Doerr; Rolf (Ober-Olm, DE)
Assignee: Boehringer Ingelheim Pharma KG (Ingelheim, DE)
Application Number:09/975,418
Patent Claims: 1. An inhalable powder comprising 0.04 to 0.8% of tiotropium in admixture with a physiologically acceptable excipient, wherein the excipient consists of a mixture of coarser excipient with an average particle size of 15 to 80 .mu.m and finer excipient with an average particle size of 1 to 9 .mu.m, the proportion of the finer excipient constituting 1 to 20% of the total amount of excipient, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

2. An inhalable powder according to claim 1, wherein the tiotropium is present in the form of the chloride, bromide, iodide, methanesulphonate, para-toluenesulphonate or methyl sulphate thereof.

3. An inhalable powder comprising between 0.048 and 0.96% of tiotropium bromide in admixture with a physiologically acceptable excipient, wherein the excipient consists of a mixture of coarser excipient with an average particle size of 15 to 80 .mu.m and finer excipient with an average particle size of 1 to 9 .mu.m, the proportion of the finer excipient constituting 1 to 20% of the total amount of excipient, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

4. An inhalable powder comprising between 0.05 and 1% of tiotropium bromide monohydrate in admixture with a physiologically acceptable excipient, wherein the excipient consists of a mixture of coarser excipient with an average particle size of 15 to 80 .mu.m and finer excipient with an average particle size of 1 to 9 .mu.m, the proportion of the finer excipient constituting 1 to 20% of the total amount of excipient, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

5. An inhalable powder according to one of claims 1, 2, 3 or 4, wherein the excipient consists of a mixture of coarser excipient with an average particle size of 17 to 50 .mu.m and finer excipient with an average particle size of 2 to 8 .mu.m.

6. An inhalable powder according to one of claims 1, 2, 3 or 4, wherein the proportion of finer excipient in the total amount of excipient is 3 to 15%.

7. An inhalable powder according to one of claims 1, 2, 3 or 4, wherein the tiotropium used has an average particle size of 0.5 to 10 .mu.m.

8. An inhalable powder according to one of claims 1, 2, 3 or 4, wherein one or more monosaccharides, disaccharides, oligo- or polysaccharides, polyalcohols, salts thereof, or mixtures thereof are used as the excipients.

9. An inhalable powder according to claim 8, wherein glucose, arabinose, lactose, saccharose, maltose, dextrane, sorbitol, mannitol, xylitol, sodium chloride, calcium carbonate or mixtures thereof are used as the excipients.

10. An inhalable powder according to claim 9, wherein glucose or lactose or mixtures thereof are used as the excipients.

11. A process for preparing an inhalable powder according to one of claims 1 to 4, comprising: (a) mixing coarser excipient fractions with finer excipient fractions to obtain an excipient mixture, and (b) mixing the excipient mixture thus obtained with the tiotropium.

12. A method of treating a disease that is responsive to the administration of tiotropium, comprising administering to a host in need thereof an inhalable powder according to one of claims 1 to 4 or 12.

13. A method according to claim 12, wherein the disease is asthma or COPD.

14. An inhalable powder according to claim 4 comprising 0.1 to 0.8% of tiotropium bromide monohydrate.

15. An inhalable powder according to claim 4 comprising 0.2 to 0.5% of tiotropium bromide monohydrate.

16. An inhalable powder according to one of claim 1, 2, 3 or 4, wherein the excipient consists of a mixture of coarser excipient with an average particle size of 20 to 30 .mu.m and finer excipient with an average particle size of 3 to 7 .mu.m.

17. An inhalable powder according to one of claim 1, 2, 3 or 4, wherein the proportion of finer excipient in the total amount of excipient is 5 to 10%.

18. An inhalable powder according to one of claim 1, 2, 3 or 4, wherein the tiotropium used has an average particle size of 1 to 6 .mu.m.

19. An inhalable powder according to one of claim 1, 2, 3 or 4, wherein the tiotropium used has an average particle size of 2 to 5 .mu.m.

20. An inhalable powder according to claim 10, wherein lactose monohydrate is used as the excipient.

21. An inhalable powder comprising between 0.2 and 0.5% of tiotropium bromide monohydrate in admixture with lactose monohydrate as the physiologically acceptable excipient, wherein the excipient consists of a mixture of coarser excipient with an average particle size of 20 to 30 .mu.m and finer excipient with an average particle size of 3 to 7 .mu.m, the proportion of the finer excipient constituting 5 to 10% of the total amount of excipient, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

22. An inhalable powder comprising 0.04 to 0.8% of tiotropium in admixture with a physiologically acceptable excipient, said inhalable powder prepared by a process comprising: (a) mixing coarser excipient having an average particle size of 15 to 80 .mu.m and finer excipient having an avenge particle size of 1 to 9 .mu.m, wherein the proportion of the finer excipient constitutes 1 to 20% of the total amount of excipient, to obtain an excipient mixture, and (b) mixing the excipient mixture thus obtained with the tiotropium, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

23. An inhalable powder according to claim 22, wherein the tiotropium is present in the form of the chloride, bromide, iodide, methanesulphonate, para-toluenesulphonate or methyl sulphate thereof.

24. An inhalable powder comprising between 0.048 and 0.96% of tiotropium bromide in admixture with a physiologically acceptable excipient, said inhalable powder prepared by a process comprising: (a) mixing coarser excipient having an average particle size of 15 to 80 .mu.m and finer excipient having an average particle size of 1 to 9 .mu.m, wherein the proportion of the finer excipient constitutes 1 to 20% of the total amount of excipient, to obtain an excipient mixture, and (b) mixing the excipient mixture thus obtained with the tiotropium bromide, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

25. An inhalable powder comprising between 0.05 and 1% of tiotropium bromide monohydrate in admixture with a physiologically acceptable excipient, said inhalable powder prepared by a process comprising: (a) mixing coarser excipient having an average particle size of 15 to 80 .mu.m and finer excipient having an average particle size of 1 to 9 .mu.m, wherein the proportion of the finer excipient constitutes 1 to 20% of the total amount of excipient, to obtain an excipient mixture, and (b) mixing the excipient mixture thus obtained with the tiotropium bromide monohydrate, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

26. An inhalable powder according to claim 25 comprising 0.1 to 0.8% of tiotropium bromide monohydrate.

27. An inhalable powder according to claim 25 comprising 0.2 to 0.5% of tiotropium bromide monohydrate.

28. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein the coarser excipient has an average particle size of 17 to 50 .mu.m and the finer excipient has an average particle size of 2 to 8 .mu.m.

29. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein the coarser excipient has an average particle size of 20 to 30 .mu.m and the finer excipient has an average particle size of 3 to 7 .mu.m.

30. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein the proportion of finer excipient in the total amount of excipient is 3 to 15%.

31. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein the proportion of finer excipient in the total amount of excipient is 5 to 10%.

32. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein the tiotropium used has an average particle size of 0.5 to 10 .mu.m.

33. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein the tiotropium used has an average particle size of 1 to 6 .mu.m.

34. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein the tiotropium used has an average particle size of 2 to 5 .mu.m.

35. An inhalable powder according to one of claim 22, 23, 24 or 25, wherein one or more monosaccharides, disaccharides, oligo- or polysaccharides, polyalcohols, salts thereof, or mixtures thereof are used as the excipients.

36. An inhalable powder according to claim 35, wherein glucose, arabinose, lactose, saccharose, maltose, dextrane, sorbitol, mannitol, xylitol, sodium chloride, calcium carbonate or mixtures thereof are used as the excipients.

37. An inhalable powder according to claim 36, wherein glucose or lactose or mixtures thereof are used as the excipients.

38. An inhalable powder according to claim 37, wherein lactose monohydrate is used as the excipient.

39. An inhalable powder comprising between 0.2 and 0.5% of tiotropium bromide monohydrate in admixture with lactose monohydrate as a physiologically acceptable excipient, said inhalable powder prepared by a process comprising: (a) mixing coarser lactose monohydrate excipient having an average particle size of 20 to 30 .mu.m and finer lactose monohydrate excipient having an average particle size of 3 to 7 .mu.m, wherein the proportion of the finer lactose monohydrate excipient constitutes 5 to 10% of the total amount of excipient, to obtain an excipient mixture, and (b) mixing the excipient mixture thus obtained with the tiotropium bromide monohydrate, wherein the inhalable proportion of active substance is released reproducibly in low variability amounts when administered to a patent.

40. A method of treating a disease that is responsive to the administration of tiotropium, comprising administering to a host in need thereof an inhalable powder according to one of claim 22, 23, 24 or 25 or 39.

41. A method according to claim 40, wherein the disease is asthma or COPD.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc