Pharmaceutical Composition for Oral Administration Comprising Enzalutamide

Patent metadata

Field	Value
Publication number	US-2020146977-A1
Application number	US-201816609062-A
Country	US
Kind code	A1
Filing date	Apr 27, 2018
Priority date	Apr 28, 2017
Publication date	May 14, 2020
Grant date	—

Abstract

Provided is a pharmaceutical composition for oral administration in which the solubility and/or dissolution properties of enzalutamide are improved and supersaturation is maintained. Also provided is a pharmaceutical composition for oral administration in which the oral absorbability of enzalutamide is improved. The pharmaceutical composition for oral administration comprises enzalutamide and polyvinyl alcohol.

First claim

1 . A pharmaceutical composition for oral administration, comprising enzalutamide and polyvinyl alcohol.

2 . The pharmaceutical composition for oral administration according to claim 1 , wherein polyvinyl alcohol has a saponification degree of 30 mol % or more and 99 mol % or less.

3 . The pharmaceutical composition for oral administration according to claim 1 , wherein polyvinyl alcohol has a polymerization degree of 50 or more and 600 or less.

4 . The pharmaceutical composition for oral administration according to claim 1 , comprising a solid dispersion comprising enzalutamide and polyvinyl alcohol.

5 . The pharmaceutical composition for oral administration according to claim 1 , further comprising a substance having a functional group capable of functioning as a hydrogen bond acceptor.

6 . The pharmaceutical composition for oral administration according to claim 5 , wherein the substance having a functional group capable of functioning as a hydrogen bond acceptor is polyvinyl pyrrolidone and/or copolyvidone.

7 . The pharmaceutical composition for oral administration according to claim 1 , further comprising co-disintegrant.

8 . The pharmaceutical composition for oral administration according to claim 7 , wherein the co-disintegrant is a compound or two or more compounds selected from the group consisting of potassium chloride, sodium chloride, magnesium chloride, and potassium dihydrogen phosphate.

9 . The pharmaceutical composition for oral administration according to claim 7 , wherein the co-disintegrant is potassium chloride.

10 . The pharmaceutical composition for oral administration according to claim 1 , further comprising disintegrant.

11 . The pharmaceutical composition for oral administration according to claim 10 , wherein the disintegrant is a compound or two or more compounds selected from the group consisting of crospovidone and low substituted hydroxypropylcellulose.

12 . The pharmaceutical composition for oral administration according to claim 10 , wherein the disintegrant is crospovidone.

13 . The pharmaceutical composition for oral administration according to claim 1 , wherein the pharmaceutical composition is a tablet.

14 . The pharmaceutical composition according to claim 1 , wherein enzalutamide is amorphous.

15 . A method of producing a pharmaceutical composition for oral administration comprising enzalutamide and polyvinyl alcohol.

16 . The method of producing a pharmaceutical composition for oral administration according to claim 15 , said method comprising the step of preparing a solid dispersion comprising enzalutamide and polyvinyl alcohol.

17 . The method of producing a pharmaceutical composition for oral administration according to claim 16 , wherein the solid dispersion is prepared by a hot melt extrusion method.

18 . The method of producing a pharmaceutical composition for oral administration according to claim 16 , wherein the solid dispersion is prepared by a solvent method.

19 . (canceled)

Assignees

• Astellas Pharma Inc

Inventors

• Umemoto Yoshiaki
• Yoshida Takatsune
• Namiki Sachie
• Takagi Akira
• Kojima Ryo
• Sakai Toshiro
• Oba Shinsuke
• Aoki Hajime

Classifications

• A61K9/2027 Primary

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61K9/2009

  Inorganic compounds · CPC title

• A61K31/4166

  having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin · CPC title

• A61K9/0053 Primary

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title