PHARMACEUTICAL FORMULATIONS COMPRISING DULOXETINE

• US 20090226517A1
• Filed: 02/05/2009
• Published: 09/10/2009
• Est. Priority Date: 02/06/2008
• Status: Abandoned Application

• Current Assignee: Dr. Reddy's Lab., Inc. (Dr. Reddy's Laboratories Ltd.), Dr. Reddy's Laboratories Ltd.
• Original Assignee: Dr. Reddy's Lab., Inc. (Dr. Reddy's Laboratories Ltd.), Dr. Reddy's Laboratories Ltd.
• Inventors: Vyas, Vinita Umashankar, Mittapalli, Pavan Kumar, Nagesh, Nagaraju
• Application Number:
  US12/366,246
• Publication Number:
  US 20090226517A1
• Time in Patent Office: Days
• US Class Current: 424/472
• CPC Class Codes: A61K 31/381 having five-membered rings
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61P 25/24 Antidepressants

Abstract

A pharmaceutical formulation comprising: a core particle comprising duloxetine or its salts; a separating layer; and an enteric layer disposed over the separating layer; wherein the formulation comprises at least one amino acid, a plasticizer, or both, in at least one of the core, the separating layer, and the enteric layer.

Claims

1. A delayed release duloxetine formulation comprising:

(a) a pharmacologically inert solid core;

(b) a drug layer comprising duloxetine or a salt thereof disposed over the core;

(c) an optional subcoating layer disposed over the drug layer; and

(d) an outer enteric coating layer.

2. The delayed release duloxetine formulation of claim 1, further comprising at least one chemically reactive substance present in a drug layer or a subcoating layer.

3. The delayed release duloxetine formulation of claim 2, wherein a chemically reactive substance comprises an α

-amino acid.

4. The delayed release formulation of claim 2, wherein a chemically reactive substance is present in an amount ranging from about 0.1% to about 20% by weight of the formulation.

5. The delayed release formulation of claim 1, wherein a subcoating layer comprises a copolymer of N-vinyl-2-pyrrolidone and vinyl acetate.

6. The delayed release formulation of claim 1, wherein a subcoating layer comprises at least one water-insoluble or water-soluble plasticizer, or a combination thereof.

7. The delayed release formulation of claim 1, wherein an enteric coating layer comprises at least one water-insoluble or water-soluble plasticizer, or a combination thereof.

8. The delayed release formulation of claim 1, wherein the formulation is in the form of multi-particulates filled into a capsule, or is a tablet.

9. The delayed release formulation of claim 8, wherein multi-particulates are in the form of a powder, granules, pellets, or minitablets.

10. The delayed release duloxetine formulation of claim 1 comprising:

(a) a solid core comprising duloxetine hydrochloride;

(b) an optional subcoating layer; and

(c) an enteric coating layer;

further comprising at least one chemically reactive substance, a plasticizer, or a combination thereof.

11. A process for preparing a delayed release pharmaceutical formulation comprising:

(i) providing a pharmacologically inert core;

(ii) coating the inert core with a composition comprising duloxetine hydrochloride;

(iii) optionally, coating the product of (ii) with a subcoating layer; and

(iv) coating the product of (ii) or (iii) with an enteric layer;

wherein the formulation comprises an amino acid in at least one of a composition comprising duloxetine hydrochloride and a subcoating layer.

12. The process of claim 11, wherein a composition comprising duloxetine hydrochloride comprises an amino acid.

13. The process of claim 11, wherein a subcoating layer comprises an amino acid.

14. The process of claim 11, wherein a subcoating layer comprises a plasticizer.

15. The process of claim 11, wherein an enteric layer comprises a plasticizer.

16. A process for preparing a delayed release pharmaceutical formulation comprising:

(i) providing a core comprising duloxetine hydrochloride;

(ii) optionally, coating the core with a subcoating layer; and

(iii) coating the product of (i) or (ii) with an enteric layer;

wherein the formulation comprises at least one α

-amino acid in at least one of a core and a subcoating layer.

17. The process of claim 16, wherein a core comprises an amino acid.

18. The process of claim 16, wherein a subcoating layer comprises an amino acid.

19. The process of claim 16, wherein a subcoating layer comprises a plasticizer.

20. The process of claim 16, wherein an enteric layer comprises a plasticizer.