Pharmaceutical compositions containing flibanserin

• US 20070196473A1
• Filed: 04/27/2007
• Published: 08/23/2007
• Est. Priority Date: 05/22/2002
• Status: Abandoned Application

• Current Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Original Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Inventors: FRIEDL, Thomas, RADTKE, Guido
• Application Number:
  US11/740,959
• Publication Number:
  US 20070196473A1
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 31/497 containing further heterocyclic rings
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• 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 9/2813 Inorganic compounds
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: C07D 235/26 Oxygen atoms

Abstract

The invention relates to oral pharmaceutical compositions containing flibanserin, methods for the preparation thereof and use thereof as a medicament.

Claims

1. ) A pharmaceutical composition for oral administration comprising a tablet core containing flibanserin polymorph A having an endothermic maximum at about 161°

C., as determined using DSC, in admixture with at least one pharmaceutically acceptable excipient and further comprising a film coating enveloping said tablet core.

2. ) A pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable excipient is a filler selected from lactose monohydrate, spray-dried lactose, agglomerated lactose, anhydrous lactose, microcrystalline cellulose, dibasic calcium phosphate, cornstarch, sugar alcohols and mixtures thereof.

3. ) A pharmaceutical composition according to claim 2, wherein the pharmaceutically acceptable excipient is selected from lactose monohydrate, spray-dried lactose, agglomerated lactose, anhydrous lactose, microcrystalline cellulose and mixtures thereof.

4. ) A pharmaceutical composition according to claim 2, wherein the pharmaceutically acceptable excipient is lactose monohydrate.

5. ) A pharmaceutical composition according to claim 2, wherein the pharmaceutically acceptable excipient is a mixture of lactose monohydrate and microcrystalline cellulose.

6. ) A pharmaceutical composition according to claim 2, wherein the pharmaceutically acceptable excipient is a mixture of dibasic calcium phosphate and microcrystalline cellulose.

7. ) A pharmaceutical composition according to claim 1, wherein flibanserin polymorph A is present in an amount of 1 to 50 wt. % based on the total mass of the core.

8. ) A pharmaceutical composition according to claim 1, wherein flibanserin polymorph A is present in an amount of 15 to 35 wt. % based on the total mass of the core.

9. ) A pharmaceutical composition according to claim 1, wherein the core contains filler in an amount of 50 to 99 wt. % based on the total mass of the core.

10. ) A pharmaceutical composition according to claim 1, wherein the core contains filler in an amount of 65 to 85 wt. % based on the total mass of the core.

11. ) A pharmaceutical composition according to claim 1, wherein the core additionally contains a binding agent selected from povidone, copovidone, hydroxypropyl methylcellulose, hydroxypropylcellulose, corn starch and mixtures thereof.

12. ) A pharmaceutical composition according to claim 11, wherein the binding agent is hydroxypropyl methylcellulose.

13. ) A pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable excipient is a mixture of lactose monohydrate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose.

14. ) A pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable excipient is a mixture of dibasic calcium phosphate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose.

15. ) A pharmaceutical composition according to claim 1, wherein the core additionally contains a disintegrant selected from among sodium starch glycolate, crospovidone, croscarmellose sodium, sodium-carboxymethylcellulose, dried corn starch and mixtures thereof.

16. ) A pharmaceutical composition according to claim 15, wherein the disintegrant is croscarmellose sodium.

17. ) A pharmaceutical composition according to claim 1, wherein the core additionally contains one or more flow regulators, lubricants and mould release or antiadhesive agents selected from silicon dioxide, talc, magnesium stearate and mixtures thereof.

18. ) A pharmaceutical composition according to claim 1, wherein the film coating enveloping the core contains at least one film-forming agent selected from hydroxypropylmethylcellulose, hydroxypropylcellulose, methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose and poly(ethylacrylate) methylmethacrylate.

19. ) A pharmaceutical composition according to claim 18, wherein the film coating enveloping the core contains hydroxypropylmethylcellulose.

20. ) A pharmaceutical composition according to claim 1, wherein the film coating enveloping the core contains one or more emulsifiers or plasticizers selected from polyethylene glycol, glycerol and propylene glycol.

21. ) A pharmaceutical composition according to claim 20, wherein the film coating enveloping the core contains polyethylene glycol.

22. ) A pharmaceutical composition according to claim 1, wherein the film coating enveloping the core contains hydroxypropylmethylcellulose and polyethylene glycol.

23. ) A pharmaceutical composition according to claim 1, wherein the film coating enveloping the core contains hydroxypropylmethylcellulose, polyethylene glycol and titanium dioxide.

24. ) A pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable excipient is a mixture of lactose monohydrate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose and the film coating enveloping the core contains hydroxypropylmethylcellulose and polyethylene glycol.

25. ) A pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable excipient is a mixture of dibasic calcium phosphate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose and the film coating enveloping the core contains hydroxypropylmethylcellulose and polyethylene glycol.

26. ) A method for treating a disease that is treatable with a compound having an affinity for the 5-HT_1A or 5-HT₂-receptors in a patient, comprising administering to said patient a therapeutically effective amount of a pharmaceutical composition according to claim 1.

27. ) A method for treating a disease selected from depression, schizophrenia, Parkinson'"'"'s, anxiety, sleep disturbances, sexual and mental disorders and age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of a pharmaceutical composition according to claim 1.