Enzalutamide solid dispersion and method for producing same, and enzalutamide-containing preparation and method for producing same

Abstract

One embodiment of the present invention provides an enzalutamide solid dispersion that maintains the amorphous state of enzalutamide and has improved dissolution properties. Alternatively, one embodiment of the present invention provides an enzalutamide-containing preparation that maintains the amorphous state of enzalutamide and has improved dissolution properties. Alternatively, one embodiment of the present invention provides a method for producing an enzalutamide solid dispersion that maintains the amorphous state of enzalutamide and has improved dissolution properties. Alternatively, one embodiment of the present invention provides a method for producing an enzalutamide-containing preparation that maintains the amorphous state of enzalutamide and has improved dissolution properties. According to one embodiment of the present invention, an enzalutamide solid dispersion which includes enzalutamide in an amorphous state and hydroxypropyl cellulose that serves as an amorphousness-maintaining polymer is provided.

Claims

1. An enzalutamide solid dispersion comprising an amorphous form of enzalutamide and hydroxypropyl cellulose as an amorphous maintaining polymer.

2. The enzalutamide solid dispersion of claim 1, further comprising one or more amorphous maintaining polymers selected from the group consisting of copolyvidone, methylcellulose and methacrylic acid copolymers.

3. The enzalutamide solid dispersion of claim 1, wherein the mass ratio of enzalutamide:HPC is in the range of 1:3 to 1:

6.

4. An enzalutamide-containing formulation comprising the enzalutamide solid dispersion described in any one of claims 1 to 3.

5. A method for producing an enzalutamide solid dispersion, comprising heating enzalutamide and hydroxypropyl cellulose as an amorphous maintaining polymer, melting the enzalutamide, softening the hydroxypropyl cellulose, mixing and homogenizing a molten material containing the enzalutamide and the hydroxypropyl cellulose, and cooling the molten material while extruding to obtain a hot melt extrudate containing the enzalutamide and the hydroxypropyl cellulose.

6. A method for producing an enzalutamide solid dispersion as described in claim 5, wherein when heating the enzalutamide and hydroxypropyl cellulose as the amorphous maintaining polymer, the maximum temperature is controlled to a range of 190°C to 230°C.

7. A method for producing the enzalutamide solid dispersion of claim 5, further comprising grinding the hot melt extrudate.

8. A method for producing an enzalutamide solid dispersion as described in claim 7, wherein when the hot-melt extrudate is pulverized, light anhydrous silicic acid is added and the hot-melt extrudate is pulverized.

9. A method for producing an enzalutamide-containing formulation, comprising mixing an enzalutamide solid dispersion obtained by the method for producing an enzalutamide solid dispersion according to any one of claims 5 to 8 with one or more pharma- ceutically acceptable additives, and compressing the resulting mixture into tablets.

Images