Claims for Patent: 11,311,532

Summary for Patent: 11,311,532

Title:	High dosage valbenazine formulation and compositions, methods, and kits related thereto
Abstract:	Solid pharmaceutical compositions with high drug loading are provided. A formulation useful for the solid pharmaceutical composition includes valbenazine, or a pharmaceutically acceptable salt thereof, silicified microcrystalline cellulose, isomalt, hydroxypropyl methylcellulose, partially pregelatinized maize starch, and magnesium stearate.
Inventor(s):	Moore, Jr.; Richard Alexander (San Diego, CA), McClelland; Gregory A. (San Diego, CA), O'Brien; Christopher F. (Vashon, WA)
Assignee:	Neurocrine Biosciences, Inc. (San Diego, CA)
Application Number:	17/074,383
Patent Claims:	1. A solid pharmaceutical composition comprising: a ditosylate salt of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[- 2,1-a]isoquinolin-2-yl ester; at least one water-insoluble filler; at least one water-soluble diluent; at least one binder; at least one disintegrant; and at least one lubricant, wherein the ditosylate salt is present in the solid pharmaceutical composition at a level of at least 30% by weight of the solid pharmaceutical composition. 2. The solid pharmaceutical composition of claim 1, wherein the ditosylate salt is present in the solid pharmaceutical composition at a level of at least 35% by weight of the solid pharmaceutical composition. 3. The solid pharmaceutical composition of claim 1, wherein the ditosylate salt is present in the solid pharmaceutical composition at a level of at least 38% by weight of the solid pharmaceutical composition. 4. The solid pharmaceutical composition of claim 1, wherein the ditosylate salt is present in the solid pharmaceutical composition at a level of at least 40% by weight of the solid pharmaceutical composition. 5. The solid pharmaceutical composition of claim 1, wherein said dosage form comprises: between 20% w/w and 40% w/w of the at least one water-insoluble filler; between 20% w/w and 40% w/w of the at least one water-soluble diluent; between 0.5% w/w and 5% w/w of the at least one binder; between 1% w/w and 10% w/w of the at least one disintegrant; and between 0.25% w/w and 5% w/w of the at least one lubricant. 6. The solid pharmaceutical composition of claim 5, wherein the at least one water-insoluble filler is microcrystalline cellulose. 7. The solid pharmaceutical composition of claim 5, wherein the at least one water-soluble diluent is isomalt. 8. The solid pharmaceutical composition of claim 5, wherein the binder is hypromellose. 9. The solid pharmaceutical composition of claim 5, wherein the at least one disintegrant is partially pregelatinized maize starch. 10. The solid pharmaceutical composition of claim 5, wherein the at least one lubricant is magnesium stearate. 11. The solid pharmaceutical composition of claim 5, wherein the at least one water-insoluble filler is microcrystalline cellulose and is present in an amount of about 25% w/w. 12. The solid pharmaceutical composition of claim 5, wherein the at least one water-soluble diluent is isomalt and is present in an amount of about 20% w/w. 13. The solid pharmaceutical composition of claim 5, wherein the at least one binder is hypromellose and is present in an amount of about 5% w/w. 14. The solid pharmaceutical composition of claim 5, wherein the at least one disintegrant is partially pregelatinized maize starch and is present in an amount of about 7.5% w/w. 15. The solid pharmaceutical composition of claim 5, wherein the at least one lubricant is magnesium stearate and is present in an amount of about 2.5% w/w. 16. The solid pharmaceutical composition of claim 1, wherein the solid pharmaceutical composition is suitable for oral administration. 17. The solid pharmaceutical composition of claim 1, wherein the solid pharmaceutical composition has a bulk density of at least about 0.5 mg/mL. 18. The solid pharmaceutical composition of claim 1, wherein the solid pharmaceutical composition has a tapped density of at least about 0.6 mg/mL. 19. The solid pharmaceutical composition of claim 1, wherein the solid pharmaceutical composition has a blend uniformity between about 90% and about 110% with a relative standard deviation of the blend uniformity of less than about 2%. 20. The solid pharmaceutical composition of claim 1, wherein the ditosylate salt has a d(0.9) particle size distribution less than 100 .mu.m. 21. The solid pharmaceutical composition of claim 1, wherein: the ditosylate salt is present in the solid pharmaceutical composition at a level of at least 38% by weight of the solid pharmaceutical composition; the at least one water-insoluble filler is microcrystalline cellulose and is present in an amount of about 25% w/w; the at least one water-soluble diluent is isomalt and is present in an amount of about 20% w/w; the at least one binder is hypromellose and is present in an amount of about 5% w/w; the at least one disintegrant is partially pregelatinized maize starch and is present in an amount of about 7.5% w/w; and the at least one lubricant is magnesium stearate and is present in an amount of about 2.5% w/w. 22. A method of treating a hyperkinetic movement disorder in a patient in need thereof, comprising orally administering to the patient the solid pharmaceutical composition of claim 1. 23. The method according to claim 22, wherein the hyperkinetic movement disorder is tardive dyskinesia. 24. The method according to claim 22, wherein the hyperkinetic movement disorder is chorea. 25. The method according to claim 24, wherein chorea is associated with Huntington's disease. 26. A method of treating a hyperkinetic movement disorder in a patient in need thereof, comprising orally administering to the patient the solid pharmaceutical composition of claim 21. 27. The method according to claim 26, wherein the hyperkinetic movement disorder is tardive dyskinesia. 28. The method according to claim 26, wherein the hyperkinetic movement disorder is chorea. 29. The method according to claim 28, wherein chorea is associated with Huntington's disease. 30. The solid pharmaceutical composition of claim 1, wherein the solid pharmaceutical composition comprises granules, wherein the granules comprise the ditosylate salt. 31. The solid pharmaceutical composition of claim 5, wherein the solid pharmaceutical composition comprises granules, wherein the granules comprise the ditosylate salt. 32. The solid pharmaceutical composition of claim 21, wherein the solid pharmaceutical composition comprises granules, wherein the granules comprise the ditosylate salt.