Oral Dosage Forms for Modified Release Comprising Tasocitinib

• US 20130344149A1
• Filed: 01/26/2012
• Published: 12/26/2013
• Est. Priority Date: 01/27/2011
• Status: Abandoned Application

• Current Assignee: Ratiopharm GmbH (Teva Pharmaceutical Industries Limited)
• Original Assignee: Ratiopharm GmbH (Teva Pharmaceutical Industries Limited)
• Inventors: Stefan, Ralph, Sievert, Frank
• Application Number:
  US13/981,741
• Publication Number:
  US 20130344149A1
• Time in Patent Office: Days
• US Class Current: 424/474
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/1676 having a drug-free core with discrete complete coating layer containing drug adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921
• CPC Class Codes: A61K 9/2022 Organic macromolecular compounds
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/28 Dragees; Coated pills or tablets , e.g. with film or compression coating A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2893 Tablet coating processes mechanical aspects A61J3/06
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/02 specific for leukemia
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The invention essentially relates to oral dosage forms comprising a JAK3 inhibitor, preferably tasocitinib, suitable for modified release, and processes of preparing such oral dosage forms.

Claims

1. Oral dosage form for modified release comprising

(a) tasocitinib, and

(b) a non-erodible material,

wherein the non-erodible material (b) is selected from ethylcellulose, celluloseester, copolymers of methacryl acid or methacrylic acid esters, polyvinyl acetate and polyvinyl acetate copolymers.

2. Oral dosage form according to claim 1, wherein tasocitinib is contained in an amount of 1 to 60 wt. %, based upon the total weight of the oral dosage form.

3. Oral dosage form according to claim 1, wherein the non-erodible material has a solubility in water at 25°

C. at a pH of 5.0 of less than 33 g/l.

4. Oral dosage form according to claim 1, wherein the non-erodible material has a solubility in water at 25°

C. at a pH of 7.0 of more than 33 g/l.

5. Oral dosage form according to claim 1, wherein the non-erodible material is a non-erodible polymer.

6. Oral dosage form according to claim 1, wherein the non-erodible material is contained in an amount of 5 to 80 wt. %, based upon the total weight of the oral dosage form.

7. Oral dosage form according to claim 1, further comprising a pore-forming material (c).

8. Oral dosage form according to claim 7, wherein the pore-forming material has a solubility in water at 25°

C. and at a pH of 5.0 of more than 50 g/l.

9. Oral dosage form according to claim 7, wherein the pore-forming material is contained in an amount of 1 to 50 wt. %, based upon the total weight of the oral dosage form.

10. Oral dosage form according to claim 1, further comprising at least one excipient (d) selected from solubilizers, fillers, lubricants, disintegrants, glidants, anti-sticking agents, plasticizers and mixtures thereof.

11. Oral dosage form according to claim 1 in the form of a matrix tablet.

12. Oral dosage form according to claim 1 in the form of a tablet comprising a core and a shell, wherein the core comprises tasocitinib (a) and wherein the shell comprises non-erodible material (b).

13. Oral dosage form according to claim 1 in the form of a multiple unit pellet system.

14. Process for manufacturing a tablet according to claim 11 comprising the steps of

(1-I) providing tasocitinib (a) and non-erodible material (b),

(1-II) agglomerating the components of step (I) to yield granules,

(1-III) compressing the mixture resulting from step (I) and (II) into tablets;

and

(1-IV) film-coating the tablets,

wherein the non-erodible material (b) is selected from ethylcellulose, celluloseester, copolymers of methacryl acid or methacrylic acid esters, polyvinyl acetate and polyvinyl acetate copolymers.

15. Process for manufacturing a tablet according to claim 19 comprising the steps of

(2-I) mixing tasocitinib (a) and pore-forming material (c) and/or an excipient (d),

(2-II) agglomerating the components of step (I) to yield granules,

(2-III) compressing the mixture resulting from step (I) and (II) into tablets, and

(2-IV) coating the tablets with a coating comprising non-erodible material (b) and pore-forming material (c) and/or at least one further excipient (d),

wherein the non-erodible material (b) is selected from ethylcellulose, celluloseester, copolymers of methacryl acid or methacrylic acid esters, polyvinyl acetate and polyvinyl acetate copolymers.

16. Process for manufacturing an oral dosage form according to claim 1 comprising the steps of

(3-I) providing a pellet core,

(3-II) spraying a solution or suspension comprising tasocitinib (a) onto the pellet core,

(3-III) spraying a solution or suspension comprising tasocitinib (b) onto the pellet resulting from step (3-II),

(3-IV) blending the pellets with non-erodible material (b) and pore-forming material (c) and/or at least one excipient (d);

and

(3-V) further processing the resulting mixture into a final oral dosage form,

wherein the non-erodible material (b) is selected from ethylcellulose, celluloseester, copolymers of methacryl acid or methacrylic acid esters, polyvinyl acetate and polyvinyl acetate copolymers.

17. Oral dosage form according to claim 5, wherein the non-erodible polymer has a weight average molecular weight from 30,000 to 3,000,000 g/mol.

18. Oral dosage form according to claim 7, wherein the pore-forming material is contained in an amount of 5 to 40 wt. %, based upon the total weight of the oral dosage form.

19. Oral dosage form according to claim 12, wherein the core and the shell further comprise pore-forming material (c) and/or at least one excipient (d).