Niraparib formulations
AssigneeTesaro, Inc.
InventorsSimon McGurk, Padma Narayan, Aleksandar Rajlic
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Abstract
The present invention is directed to pharmaceutical tablet compositions comprising the compound niraparib as an active pharmaceutical ingredient, suitable for oral administration as well as to methods for their preparation. Also described herein are tablet compositions containing niraparib formed by the disclosed methods, and therapeutic uses of such tablet compositions for treating various disorders and conditions.
Claims23
-229. (canceled)
A pharmaceutical composition in the form of a tablet comprising:
- (i) an intragranular portion comprising:
- (a) 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole 7-carboxamide 4-methylbenzenesulfonate monohydrate and;
- (b) one or more intragranular excipients comprising a first diluent;
- a second diluent;
- a binder;
- a disintegrant;
- a glidant, adsorbent, or absorbent;
- or a lubricant;
- wherein the intragranular portion constitutes from about 80% to about 98% by weight of the tablet composition;
- and
- (ii) an extragranular portion comprising one or more excipients comprising a disintegrant;
- a glidant, or adsorbent, or absorbent;
- or a lubricant;
- wherein the extragranular portion constitutes from about 2% to about 15% by weight of the tablet composition, and
- wherein the tablet has a disintegration time of about 30-300 seconds.
A method of making a pharmaceutical composition in the form of a tablet comprising 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole 7-carboxamide 4-methylbenzenesulfonate monohydrate comprising:
- (a) forming an intragranular portion comprising
- i) combining 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole 7-carboxamide 4-methylbenzenesulfonate monohydrate and at least one pharmaceutically acceptable excipient to form a composition comprising 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole 7-carboxamide 4-methylbenzenesulfonate monohydrate and at least one pharmaceutically acceptable excipient;
- and
- ii) granulating the composition comprising 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole 7-carboxamide 4-methylbenzenesulfonate monohydrate and at least one pharmaceutically acceptable excipient to form granules;
- (b) forming an extragranular phase comprising
- iii) combining the granules with at least one pharmaceutically acceptable excipient to form a mixture;
- and
- (c) forming a tablet by compressing the mixture obtained from step iii);
- wherein the tablet has at least one of the following:
- (1) the amount of components used to form the intragranular phase is about 80% to about 98% by weight of the tablet composition;
- and
- (2) the amount of components used to form the extragranular phase is about 2% to about 15% by weight of the tablet composition.
Dependencies are inferred from the claim text.