Dried milled granulate and methods

• US 20070048373A1
• Filed: 08/21/2006
• Published: 03/01/2007
• Est. Priority Date: 08/30/2005
• Status: Abandoned Application

• Current Assignee: Cima Labs Incorporated (Teva Pharmaceutical Industries Limited)
• Original Assignee: Cima Labs Incorporated (Teva Pharmaceutical Industries Limited)
• Inventors: Habib, Walid, Moe, Derek, Chastain, Sara
• Application Number:
  US11/507,240
• Publication Number:
  US 20070048373A1
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/473 ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/7052 having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1682 Processes
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention relates to a method of producing a dried wet granulate having a desirable average particle size and particle size distribution and dosage forms made from that granulate.

Claims

1. A method of producing a wet granulate having a desirable particle size distribution comprising the steps of:

drying a wet granulate having an initial moisture content comprising at least one pharmaceutically active ingredient to a predetermined first relative moisture content to form a partially dried wet granulate;

milling said partially dried wet granulate to obtain a milled partially dried wet granulate predetermined particle size distribution; and

drying said milled partially dried wet granulate to produce a final dried wet granulate, wherein said predetermined first relative moisture content is at least about 30% less than the initial moisture content of said wet granulate.

2. The method of claim 1, wherein said final dried wet granulate has an average particle size of between about 150 and about 600 microns and no more than about 40% of the particles by weight have a particle size of 105 microns.

3. The method of claim 2, wherein said step of milling said partially dried wet granulate is accomplished using a screen which is 20 and 140 mesh.

4. The method as in any one of claims 1, 2 and 3, wherein said predetermined first relative moisture content is between about 30% and about 85% less than said initial moisture content of said wet granulate.

5. The method of claim 4, wherein said predetermined first relative moisture content is between about 40% and about 80% less than said initial moisture content of said wet granulate.

6. The method of claim 5, wherein said predetermined first relative moisture content is between about 50% and about 80% less than said initial moisture content of said wet granulate.

7. The method of claim 6, wherein said predetermined first relative moisture content is between about 60% and about 75% less than said initial moisture content of said wet granulate.

8. The method of claim 4, wherein said final dried wet granulate has an average particle size of between about 175 and about 600 microns and no more than about 35% of the particles by weight have a particle size of 105 microns.

9. The method of claim 8, wherein said final dried wet granulate has an average particle size of between about 200 and about 600 microns and no more than about 35% of the particles by weight have a particle size of 105 microns.

18. A final dried wet granulate produced according to the steps of claim 1.

19. A final dried wet granulate produced according to the steps of claim 4.

10. A method of producing a wet granulate having a desirable particle size distribution comprising the steps of:

drying a wet granulate comprising at least one pharmaceutically active ingredient to a predetermined first relative moisture content to form a partially dried wet granulate, wherein said predetermined first relative moisture content is at least about 30% less than the initial moisture content of said wet granulate;

milling said partially dried wet granulate using a screen which is between about 20 and about 140 mesh to obtain a predetermined particle size distribution; and

drying said milled partially dried wet granulate to produce a final dried wet granulate having an average particle size of between about 175 and about 600 microns and no more than about 35% of the particles by weight have a particle size of 105 microns.

11. The method of claim 10, wherein said predetermined first relative moisture content is between about 40% and about 80% less than said initial moisture content of said wet granulate.

12. The method of claim 11, wherein said predetermined first relative moisture content is between about 50% and about 80% less than said initial moisture content of said wet granulate.

13. The method of claim 12, wherein said final dried wet granulate has an average particle size of between about 200 and about 600 microns and no more than about 30% of the particles by weight have a particle size of 105 microns.

14. The method of claim 10, wherein said wet granulate further comprises at least one excipient.

15. The method of claim 10, wherein said at least one pharmaceutically active ingredient is fexofenadine, desloratadine, fentanyl, tramadol, modafinil, armodafinil, clozapine, azithromycin or oxycodone.

16. The method of claim 10, further comprising coating said final dried wet granulate.

17. The method of claim 16, wherein said coating is a taste masking coating.

20. A final dried wet granulate produced according to the steps of claim 10.

21. A final dried wet granulate produced according to the steps of claim 17.

22. A dried wet granulate comprising:

at least one pharmaceutically active ingredient granulate and at least one excipient, said dried wet granulate having an average particle size of between about 150 and about 600 microns and no more than about 40% of the particles by weight have a particle size of 105 microns.

23. The dried wet granulate of claim 22, further comprising at least one coating.

24. The dried wet granulate of claim 23, wherein said coating is a taste masking coating.

25. A compressed tablet comprising:

dried wet granulate comprising at least one pharmaceutically active ingredient granulate and at least one excipient, said dried wet granulate having an average particle size of between about 150 and about 600 microns and no more than about 40% of the particles by weight have a particle size of 105 microns; and

at least one excipient, which have been compressed into a tablet.

26. The method of claim 25, wherein said at least one pharmaceutically active ingredient is fexofenadine, desloratadine, fentanyl, tramadol, modafinil, armodafinil, clozapine, azithromycin or oxycodone.

27. The method of claim 26, wherein said at least one pharmaceutically active ingredient is fexofenadine, desloratadine, or fentanyl.