NOVEL METHODS
The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
1 - 30 . (canceled)
31 . A sustained or delayed release pharmaceutical composition comprising an effective amount of Compound of Formula I:
wherein X is —N(CH 3 )— and Y is —O—, in free base form, and a polymeric matrix, wherein the Compound of Formula I is dispersed or dissolved in the polymeric matrix, and wherein the polymeric matrix comprises poly(d,l-lactide) or poly(d,l-lactide-co-glycolide) polymer with either carboxylic acid or carboxylic ester end groups.
32 . The pharmaceutical composition according to claim 31 , wherein the composition is a long-acting injectable composition.
33 . The pharmaceutical composition according to claim 31 , wherein the polymeric matrix comprises poly(d,l-lactide) polymer.
34 . The pharmaceutical composition according to claim 31 , wherein the polymeric matrix comprises poly(d,l-lactide-co-glycolide) polymer, wherein the ratio of lactide to glycolide monomeric units is from 50:50 to 75:25.
35 . The pharmaceutical composition according to claim 34 , wherein the poly(d,l-lactide-co-glycolide) polymer has a weight average molecular weight of 24,000 to 38,000 Daltons.
36 . The pharmaceutical composition according to claim 31 , wherein the polymeric matrix is not composed in microparticles or microspheres.
37 . The pharmaceutical composition of claim 31 , wherein the composition degrades and releases the Compound of Formula I over a period of about 30 days.
38 . The pharmaceutical composition of claim 31 , wherein the composition is formulated for intramuscular, intraperitoneal, intrathecal, epidural or subcutaneous injection.
39 . The pharmaceutical composition of claim 31 , further comprising an antioxidant.
40 . The pharmaceutical composition according to claim 31 , wherein the effective amount of the compound of Formula I is from 100 mg to 600 mg per month.
41 . The pharmaceutical composition according to claim 31 , wherein the effective amount of the compound of Formula I is from 150 to 300 mg per month.
42 . A method for the treatment of bipolar disorder I and/or bipolar II disorder comprising administering to a patient in need thereof an effective amount of the pharmaceutical composition according to claim 31 .
43 . The method according to claim 42 , wherein the bipolar disorder is bipolar I disorder.
44 . The method according to claim 42 , wherein the bipolar disorder is bipolar II disorder.
45 . A method for the treatment of the negative symptoms of schizophrenia comprising administering to a patient in need thereof an effective amount of the pharmaceutical composition according to claim 31 .