	US 12,465,570 B2
	Methods
Peng Li, New Milford, NJ (US); Robert Davis, San Diego, CA (US); and William Paul Findlay, Massapequa, NY (US)
Assigned to INTRA-CELLULAR THERAPIES, INC., Bedminster, NJ (US)
Filed by INTRA-CELLULAR THERAPIES, INC., New York, NY (US)
Filed on Mar. 1, 2024, as Appl. No. 18/593,060.
Application 18/593,060 is a continuation of application No. 17/270,573, granted, now 11,957,791, previously published as PCT/US2019/049061, filed on Aug. 30, 2019.
Claims priority of provisional application 62/779,920, filed on Dec. 14, 2018.
Claims priority of provisional application 62/725,944, filed on Aug. 31, 2018.
Prior Publication US 2024/0245610 A1, Jul. 25, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/4985 (2006.01)

CPC A61K 9/2013 (2013.01) [A61K 9/2009 (2013.01); A61K 9/2054 (2013.01); A61K 9/284 (2013.01); A61K 31/4985 (2013.01); C07B 2200/13 (2013.01)]

22 Claims

1. A solid oral dosage form, comprising lumateperone:

in mono-tosylate salt form, in admixture with one or more pharmaceutically acceptable diluents or carriers, wherein the dosage form is an immediate release dosage form formulated for oral (gastrointestinal) administration, and wherein the dosage form dissolves in 500 mL of 0.1N aqueous hydrochloric acid to the extent of at least 75% after 15 minutes;

wherein the dosage form comprises the pharmaceutically acceptable diluents or carriers:

(a) 60-90% by weight of a diluent/filler selected from cellulose, microcrystalline cellulose, mannitol, lactose monohydrate, dicalcium phosphate, and isomalt,

(b) 1-10% by weight of a binder selected from hydroxypropyl cellulose, hydroxypropyl methyl cellulose, and copovidone,

(d) 0.1-5% by weight of a lubricant selected from magnesium stearate and glyceryl monostearate, and

(e) 0.1-5% by weight of a glidant selected from silicon dioxide and talc.