Extended release tablet

• US 20060257473A1
• Filed: 04/06/2006
• Published: 11/16/2006
• Est. Priority Date: 05/11/2005
• Status: Abandoned Application

• Current Assignee: L. Perrigo Company (Perrigo Company PLC)
• Original Assignee: L. Perrigo Company (Perrigo Company PLC)
• Inventors: Puranajoti, Porranee
• Application Number:
  US11/399,203
• Publication Number:
  US 20060257473A1
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00

Abstract

A single tablet layer having an extended release profile comparable to the release profile of a bi-layer tablet having both an immediate release and an extended release layer is prepared from a pharmaceutical granulation containing a pharmaceutically active compound, a hydrophilic polymer, and a water in-soluble, non-swellable particulate channeling agent.

Claims

1. A pharmaceutical granulation, comprising:

a pharmaceutically active compound;

a hydrophilic polymer; and

a water-insoluble, non-swellable particulate channeling agent in an amount of at least 0.1 percent by weight.

2. The granulation of claim 1, wherein the pharmaceutically active compound is guaifenesin.

3. The granulation of claim 1, wherein the hydrophilic polymer is hydroxyethyl cellulose.

4. The granulation of claim 1, wherein the channeling agent is silicon dioxide.

5. The granulation of claim 1, wherein the hydrophilic polymer is present in an amount of from 3 to 30 percent by weight.

6. The granulation of claim 1 further comprising a non-hygroscopic diluent.

7. The granulation of claim 6, wherein the non-hygroscopic diluent is dicalcium phosphate anhydrous.

8. The granulation of claim 1, wherein the non-hygroscopic diluent is dicalcium phosphate anhydrous and the channeling agent is silicon dioxide.

9. The granulation of claim 1, further comprising a polymeric binder.

10. The granulation of claim 9, wherein the water-soluble channeling agent is compressible sugar.

11. The granulation of claim 1, further comprising a polymeric binder in an amount of from 0.5 to 5 percent by weight.

12. The granulation of claim 1, further comprising copovidone in an amount of from 0.5 to 5 percent by weight.

13. A pharmaceutical granulation comprising:

guaifenesin;

a hydrophilic polymer; and

a water-insoluble, non-swellable particulate channeling agent.

14. The granulation of claim 13, wherein the channeling agent is present in an amount of from 0.1 to 4.0 percent by weight.

15. The granulation of claim 13, wherein the hydrophilic polymer is hydroxyethyl cellulose.

16. The granulation of claim 13, wherein the channeling agent is silicon dioxide.

17. The granulation of claim 13, wherein the hydrophilic polymer is present in an amount of from 3 to 30 percent by weight.

18. The granulation of claim 13, wherein the granulation further comprises a non-hygroscopic diluent.

19. The granulation of claim 13, further comprising dicalcium phosphate anhydrous.

20. The granulation of claim 13, further comprising a polymeric binder.

21. The granulation of claim 13, further comprising a polymeric binder in an amount of from 0.5 to 5 percent by weight.

22. The granulation of claim 13, further comprising copovidone in an amount of from 0.5 to 5 percent by weight.

23. A process for preparing a pharmaceutical granulation, comprising:

blending a pharmaceutically active compound with a water-insoluble, non-swellable particulate channeling agent to obtain a first mixture;

adding a hydrophilic polymer, polymeric binder and any optional diluents and/or excipients to the first mixture, and blending to obtain a second mixture; and

wet granulating the second mixture to produce granules.

24. The process of claim 23, wherein the pharmaceutically active compound is guaifenesin.

25. The process of claim 23, wherein the hydrophilic polymer is hydroxyethyl cellulose.

26. The process of claim 23, wherein the channeling agent is silicon dioxide.

27. The process of claim 23, wherein the hydrophilic polymer is present in an amount of from 3 to 30 percent by weight.

28. The process of claim 23, wherein the granulation further comprises a non-hygroscopic diluent.

29. The process of claim 23, further comprising dicalcium phosphate anhydrous.

30. The process of claim 23, further comprising a polymeric binder.

31. The granulation of claim 23, further comprising a polymeric binder in an amount of from 0.5 to 5 percent by weight.

32. The process of claim 23, further comprising copovidone in an amount of from 0.5 to 5 percent by weight.

33. A compressed tablet or compressed tablet layer or portion comprising:

a therapeutically effective amount of a granulation including a pharmaceutically active compound, a hydrophilic polymer, and a water-insoluble, non-swellable particulate channeling agent in an amount of from 0.1 to 4.0 percent by weight of the granulation; and

one or more extragranular excipients, including a channeling agent.

34. The compressed tablet or compressed tablet layer or portion of claim 33, and one or more additional compressed tablet layers or portions.

35. A compressed guaifenesin tablet comprising:

a therapeutically effective amount of a granulation consisting essentially of guaifenesin, hydroxyethyl cellulose in an amount of from 3 to 30 percent by weight of the granulation, silicon dioxide in an amount of from 0.1 to 4.0 percent by weight of the granulation, copovidone in an amount of from 0.5 to 5 percent by weight of the granulation, dicalcium phosphate anhydrous in an amount up to 25 percent by weight of the granulation, and a compressible sugar in an amount up to 10 percent by weight of the granulation; and

one or more extragranular excipients, including a binder.