USRE38912EExpiredUtility

Process for preparing powder formulations

93
Assignee: BOEHRINGER INGELHEIM PHARMAPriority: Oct 12, 2000Filed: Jan 28, 2004Granted: Dec 6, 2005
Est. expiryOct 12, 2020(expired)· nominal 20-yr term from priority
Inventors:Michael WalzGeorg Boeck
A61P 43/00A61P 11/06A61P 11/00A61K 9/14A61K 9/0075A61K 9/145A61K 31/439
93
PatentIndex Score
51
Cited by
16
References
35
Claims

Abstract

The invention relates to a new process for producing powdered preparations for inhalation.

Claims

exact text as granted — not AI-modified
1. A process for preparing an inhalable powder, wherein N+m substantially equal portions of an excipient having a larger average particle size distribution  and N equal portions of an active substance having a smaller average particle size distribution  are added in alternate layers into a suitable mixing vessel and after all the excipient and active substance have been added the 2N+m layers of the two components are mixed together using a suitable mixer, wherein a portion of the excipient having the larger particle size is added first, and wherein N is an integer >5 and m denotes 0 or 1. 
     
     
       2. A process according to  claim 1 , wherein N is an integer >5. 
     
     
       3. A process according to  claim 1 , characterised in that the individual portions of excipient and active substance are added in layers through a suitable screening apparatus. 
     
     
       4. A process according to  claim 1 , characterised in that m denotes 1. 
     
     
       5. A process according to  claim 1 , characterised in that the inhalable powder obtained contains less than 5% of active substance. 
     
     
       6. A process according to  claim 5 , characterised in that the inhalable powder obtained contains less than 2% of active substance. 
     
     
       7. A process according to  claim 1 , characterised in that the active substance has an average particle size of from 0.5 to 10 μm. 
     
     
       8. A process according to  claim 7 , characterised in that the active substance has an average particle size of from 1 to 6 μm. 
     
     
       9. A process according to  claim 1 , characterised in that the excipient has an average mean  particle size of from 10 to 100 μm. 
     
     
       10. A process according to  claim 9 , characterised in that the excipient has an average mean  particle size of from 15 to 80 μm. 
     
     
       11. A process according to  claim 1 , wherein the excipient is a single excipient or a mixture of different excipients. 
     
     
       12. A process according to  claim 1 , characterised in that the excipient consists of a mixture of coarser excipient with an average particle size of 15 to 80 μm and finer excipient with an average particle size of 1 to 9 μm, the proportion of finer excipient constituting 1 to 20% of the total amount of excipient. 
     
     
       13. A process according to  claim 1 , wherein the active substance is a single active substance or two or more different active substances. 
     
     
       14. A process according to  claim 1 , characterised in that the active substance consists of one or more compounds selected from among the betamimetics, anticholinergics, corticosteroids and dopamine agonists. 
     
     
       15. An inhalable powder obtained by the process according to  claim 1 . 
     
     
       16. The process according to  claim 1  wherein the active substance is selected from the group consisting of betamimetics, anticholinergics, corticosteroids, dopamine agonists, and pharmaceutically acceptable salts, solvates or hydrates thereof, and mixtures thereof. 
     
     
       17. The process according to  claim 16  wherein the active substance consists of an anticholinergic compound or its pharmaceutically acceptable solvate, hydrate or salt. 
     
     
       18. The process according to  claim 17  wherein the anticholinergic compound comprises tiotropium. 
     
     
       19. The process according to  claim 17  wherein the pharmaceutically acceptable salt of the anticholinergic compound comprises tiotropium bromide. 
     
     
       20. The process according to  claim 17  wherein the pharmaceutically acceptable solvate or hydrate of the anticholinergic compound comprises tiotropium bromide monohydrate. 
     
     
       21. The process according to  claim 1  wherein the excipient is selected from the group consisting of monosaccharides, disaccharides, oligosaccharides, polysaccharides, polyalcohols, salts, and mixtures thereof, each optionally in its hydrate forms. 
     
     
       22. The process according to  claim 21  wherein the excipient consists of a monosaccharide or a disaccharide, or a combination thereof. 
     
     
       23. The process according to  claim 21  wherein the excipient consists of glucose or lactose or a combination thereof, each optionally in its hydrate form. 
     
     
       24. The process according to  claim 22  wherein the excipient consists of a disaccharide. 
     
     
       25. The process according to  claim 23  wherein the excipient consists of lactose or lactose monohydrate. 
     
     
       26. The inhalable powder according to  claim 15  wherein the active substance is selected from the group consisting of betamimetics, anticholinergics, corticosteroids, dopamine agonists, and pharmaceutically acceptable salts, solvates or hydrates thereof, and mixtures thereof. 
     
     
       27. The inhalable powder according to  claim 26  wherein the active substance consists of an anticholinergic compound or its pharmaceutically acceptable solvate, hydrate or salt. 
     
     
       28. The inhalable powder according to  claim 27  wherein the anticholinergic compound consists of tiotropium. 
     
     
       29. The inhalable powder according to  claim 27  wherein the pharmaceutically acceptable salt of the anticholinergic compound consists of tiotropium bromide. 
     
     
       30. The inhalable powder according to  claim 27  wherein the pharmaceutically acceptable solvate or hydrate of the anticholinergic compound consists of tiotropium bromide monohydrate. 
     
     
       31. The inhalable powder according to  claim 1  wherein the excipient is selected from the group consisting of monosaccharides, disaccharides, oligosaccharides, polysaccharides, polyalcohols, salts, and mixtures thereof, each optionally in its hydrate form. 
     
     
       32. The inhalable powder according to  claim 31  wherein the excipient consists of a monosaccharide or a disaccharide or a combination thereof. 
     
     
       33. The inhalable powder according to  claim 32  wherein the excipient consists of glucose or lactose or combinations thereof, each optionally in its hydrate form. 
     
     
       34. The inhalable powder according to  claim 32  wherein the excipient consists of a disaccharide. 
     
     
       35. The inhalable powder according to  claim 33  wherein the excipient consists of lactose or lactose monohydrate.

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