PHARMACEUTICAL COMPOSITIONS CONTAINING QUETIAPINE FUMARATE

• US 20080193527A1
• Filed: 04/19/2007
• Published: 08/14/2008
• Est. Priority Date: 02/14/2007
• Status: Abandoned Application

• Current Assignee: Laboratorios Lesvi, S.L.
• Original Assignee: Laboratorios Lesvi, S.L.
• Inventors: Diez Martin, Ignacio, Ruiz Amenos, Anna, Ubeda Perez, Carmen
• Application Number:
  US11/737,462
• Publication Number:
  US 20080193527A1
• Time in Patent Office: Days
• US Class Current: 424/465
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/5015 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

Abstract

A granule formulation useful for preparation of pharmaceutical compositions. The granule formulation includes a core containing quetiapine or a pharmaceutically acceptable salt thereof as an active ingredient, and a binder agent. The core is coated with a coating layer including a lubricant agent. Solid pharmaceutical compositions containing quetiapine, and their preparation, are described.

Claims

1. A granule formulation for the preparation of pharmaceutical compositions, each granule comprising:

a) a core comprising (i) quetiapine, or a pharmaceutically acceptable salt thereof, as active ingredient, and (ii) a binder agent; and

b) a coating layer comprising a lubricant agent.

2. The granule formulation according to claim 1 wherein the core further comprises a diluent agent and/or a disintegrant agent.

3. The granule formulation according to claim 1 wherein the binder agent is selected from the group consisting of povidone, corn starch, hydroxypropylcellulose and copovidone.

4. The granule formulation according to claim 2 wherein the diluent agent is selected from the group consisting of microcrystalline cellulose, lactose monohydrate and dibasic calcium phosphate.

5. The granule formulation according to claim 2 wherein the disintegrant agent is selected from the group consisting of sodium glycolate starch, crospovidone and sodium croscarmellose.

6. The granule formulation according to claim 1 wherein the lubricant agent is selected from the group consisting of glyceryl behenate, glyceryl palmitoestearate and macrogol.

7. The granule formulation according to claim 1 wherein the active ingredient comprises quetiapine hemifumarate.

8. The granule formulation according to claim 1 comprising:

a) a core comprising quetiapine hemifumarate, microcrystalline cellulose, sodium starch glycolate and povidone; and

b) a coating layer comprising glyceryl behenate.

9. The granule formulation according to claim 1 comprising the lubricant agent in an amount of from about 5% to about 25% by weight, based on the total weight of the granule formulation.

10. A process for the preparation of a granule formulation as defined in claim 1 comprising:

a) providing quetiapine or a pharmaceutically acceptable salt thereof, optionally in mixture with a disintegrant agent and/or a diluent agent, as an active ingredient composition;

b) combining the active ingredient composition with binder agent and solvent to form a mixture, comprising a combination sequence selected from among (i) and (ii);

(i) adding the binder agent to the active ingredient composition to form a binder-containing composition, and adding solvent to the binder-containing composition to form said mixture; and

(ii) adding a solution or suspension comprising the binder agent and solvent to the active agent composition to form said mixture;

c) wet granulating said mixture to form granules;

d) drying said granules to form dried granules;

e) sieving said dried granules to recover product granules; and

f) coating the product granules with a lubricant agent, to yield said granule formulation.

11. The process according to claim 10 wherein said solvent comprises a solvent composition selected from the group consisting of water, alcohols and hydroalcoholic mixtures.

12. The process according to claim 10 wherein the wet granulating is conducted in a low shear mixer.

13. The process according to claim 10 wherein said drying is conducted so that said dried granules have a humidity content below 5%.

14. A method of making a pharmaceutical composition, comprising formulating same with a granule formulation according to claim 1.

15. A pharmaceutical composition comprising a granule formulation according to claim 1, optionally in combination with at least one pharmaceutically acceptable excipient.

16. The pharmaceutical composition according to claim 15 in an immediate release form.

17. The pharmaceutical composition according to claim 15 in a sustained release form.

18. The pharmaceutical composition according to claim 15 in a tablet form.

19. An immediate release tablet comprising a granule formulation according to claim 1, wherein the lubricant agent has a concentration in a range of from 5 weight % to 10 weight %, based on total weight of the granule formulation.

20. A sustained release tablet comprising a granule formulation according to claim 1, wherein the lubricant agent has a concentration in a range of from 15 weight % to 25 weight %, based on total weight of the granule formulation.

21. A process for the preparation of a tablet selected from among (i) an immediate release tablet comprising a granule formulation according to claim 1, wherein the lubricant agent has a concentration in a range of from 5 weight % to 10 weight %, based on total weight of the granule formulation, and (ii) a sustained release tablet comprising a granule formulation according to claim 1, wherein the lubricant agent has a concentration in a range of from 15 weight % to 25 weight %, based on total weight of the granule formulation, said process comprising:

(a) preparing a granule formulation according to claim 10, wherein said granule formulation is optionally mixed with at least one pharmaceutically acceptable excipient;

(b) tableting said granule formulation optionally mixed with at least one pharmaceutically acceptable excipient, to form tablets containing said granule formulation; and

(c) coating said tablets.