Pharmaceutical composition of darolutamide
AssigneeOrion Corporation
InventorsSusanna Ilmonen, Juha Lintunen, Petteri Lyytinen, Marko Saalasti
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Abstract
The present invention relates to a pharmaceutical composition for oral administration, particularly in the form of a tablet, comprising darolutamide or a pharmaceutically acceptable salt thereof as an active ingredient. Darolutamide is a potent androgen receptor (AR) modulator useful in the treatment of cancer, particularly AR dependent cancer such as prostate cancer, and other diseases where AR antagonism is desired.
Claims10
A pharmaceutical composition in the form of a tablet comprising
- (a) 45-80%, per weight of the composition, of darolutamide or a pharmaceutically acceptable salt thereof;
- (b) 5-60%, per weight of the composition, of a filler;
- (c) 0.5-10%, per weight of the composition, of a disintegrant;
- (d) 0.5-10%, per weight of the composition, of a binder;
- and
- (e) 0.2-5%, per weight of the composition, of a lubricant;
- wherein the darolutamide or pharmaceutically acceptable salt thereof is present in an amount of 300 mg or 600 mg,
- wherein the tablet comprises an intragranular part and an extragranular part, and
- wherein the intragranular part comprises darolutamide or a pharmaceutically acceptable salt thereof, the filler, the binder and a portion of the disintegrant and the extragranular part comprises the lubricant and the rest of the disintegrant, and wherein the tablet has a compact tensile strength of at least about 3.5 MPa at average punch pressure of 200 MPa.
A tablet composition comprising a tablet core and a film coating, wherein the tablet core comprises:
- (a) about 300 mg of darolutamide or a pharmaceutically acceptable salt thereof;
- (b) about 60 mg of calcium hydrogen phosphate;
- (c) about 180 mg of lactose monohydrate;
- (d) about 30 mg of croscarmellose sodium;
- (e) about 24 mg of polyvinylpyrrolidone;
- and
- (f) about 5.4 mg of magnesium stearate,
- wherein the tablet core comprises an intragranular part and an extragranular part, and wherein the intragranular part comprises the darolutamide or a pharmaceutically acceptable salt thereof, the calcium hydrogen phosphate, the lactose monohydrate, the polyvinylpyrrolidone and a portion of the croscarmellose sodium and the extragranular part comprises the magnesium stearate and the rest of the croscarmellose sodium, and wherein the tablet composition has a compact tensile strength of at least about 3.5 MPa at average punch pressure of 200 MPa.
A tablet composition comprising a tablet core and a film coating, wherein the tablet core comprises:
- (a) 300 mg of darolutamide or a pharmaceutically acceptable salt thereof;
- (b) 60 mg of calcium hydrogen phosphate;
- (c) 180 mg of lactose monohydrate;
- (d) 30 mg of croscarmellose sodium;
- (e) 24 mg of polyvinylpyrrolidone;
- and
- (f) 5.4 mg of magnesium stearate,
- wherein the tablet core comprises an intragranular part and an extragranular part, and wherein the intragranular part comprises the darolutamide or a pharmaceutically acceptable salt thereof, the calcium hydrogen phosphate, the lactose monohydrate, the polyvinylpyrrolidone and a portion of the croscarmellose sodium and the extragranular part comprises the magnesium stearate and the rest of the croscarmellose sodium.
Dependencies are inferred from the claim text.