COMPOSITIONS AND METHODS FOR TREATING SCHIZOPHRENIA
The disclosure provides a novel polymorph of Compound (I): 2-((1-(2-(4-Fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-one monohydrochloride dihydrate, i.e., Form (A) of Compound (I)·HCl·2H 2 O. Pharmaceutical compositions comprising Form (A) of Compound (I)·HCl·2H 2 O and related methods of treatment are also disclosed.
1 .- 42 . (canceled)
43 . A pharmaceutical formulation comprising a release modifier and about 64 mg of Compound (I)
or a pharmaceutically acceptable salt and/or hydrate thereof, provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 50 ng/ml.
44 . A pharmaceutical formulation comprising a release modifier and 64 mg of Compound (I)
or a pharmaceutically acceptable salt and/or hydrate thereof, provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 50 ng/ml.
45 . The pharmaceutical formulation of claim 43 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 40 ng/ml.
46 . The pharmaceutical formulation of claim 44 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 40 ng/mL.
47 . The pharmaceutical formulation of claim 43 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 30 ng/mL.
48 . The pharmaceutical formulation of claim 44 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 30 ng/mL.
49 . The pharmaceutical formulation of claim 43 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 25 ng/mL.
50 . The pharmaceutical formulation of claim 44 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 25 ng/mL.
51 . The pharmaceutical formulation of claim 43 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 20 ng/mL.
52 . The pharmaceutical formulation of claim 44 , provided that when the formulation is administered to a human, the maximum plasma concentration (C max ) of Compound (I) detected in the human is below 20 ng/mL.
53 . The pharmaceutical formulation of claim 43 , wherein the release modifier is a hypromellose.
54 . The pharmaceutical formulation of claim 44 , wherein the release modifier is a hypromellose.
55 . The pharmaceutical formulation of claim 53 , wherein the hypromellose is hypromellose K100LV CR.
56 . The pharmaceutical formulation of claim 54 , wherein the hypromellose is hypromellose K100LV CR.
57 . The pharmaceutical formulation of claim 43 , further comprising a filler, a glidant, and a lubricant.
58 . The pharmaceutical formulation of claim 44 , further comprising a filler, a glidant, and a lubricant.
59 . The pharmaceutical formulation of claim 57 , wherein the filler is microcrystalline cellulose, lactose, or a combination thereof.
60 . The pharmaceutical formulation of claim 58 , wherein the filler is microcrystalline cellulose, lactose, or a combination thereof.
61 . The pharmaceutical formulation of claim 57 , wherein the glidant is silica colloidal anhydrous.
62 . The pharmaceutical formulation of claim 58 , wherein the glidant is silica colloidal anhydrous.
63 . The pharmaceutical formulation of claim 57 , wherein the lubricant is magnesium stearate.
64 . The pharmaceutical formulation of claim 58 , wherein the lubricant is magnesium stearate.