Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
DC
First Claim
Patent Images
1. Anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have one or more of the following properties;
a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;
an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;
an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); and
an endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min).
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Abstract
The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
30 Citations
310 Claims
-
1. Anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
- C. and a humidity level of 100%,
-
12. Anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray. - View Dependent Claims (13, 14, 15, 16, 17, 18)
- C. and a humidity level of 100%,
-
19. Anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (20, 21, 22, 23, 24, 25, 26, 27, 28, 29)
- C. and a humidity level of 100%,
-
30. Anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray. - View Dependent Claims (31, 32, 33, 34, 35, 36)
- C. and a humidity level of 100%,
-
37. A process for preparing anhydrous aripiprazole crystals having low hygroscopicity, wherein said process comprises heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=12.6°
, 15.4°
, 17.3°
, 18.0°
, 18.6°
, 22.5°
, and 24.8°
using a Cu Kα
x-ray;an endothermic curve comprising a first endothermic peak at about 71°
C. and a second endothermic peak around 60°
to 120°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan infrared absorption spectrum comprising infrared absorption bands at 2951, 2822, 1692, 1577, 1477, 1378, 1187, 963, and 784 cm−
1 on the IR (KBr) spectrum,wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (38, 39, 40, 41, 49, 50, 51, 52, 53)
-
-
42. A process for preparing anhydrous aripiprazole crystals having low hygroscopicity, wherein said process comprises heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=12.6°
, 15.4°
, 17.3°
, 18.0°
, 18.6°
, 22.5°
, and 24.8°
using a Cu Kα
x-ray;an endothermic curve comprising a first endothermic peak at about 71°
C. and a second endothermic peak around 60°
to 120°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan infrared absorption spectrum comprising infrared absorption bands at 2951, 2822, 1692, 1577, 1477, 1378, 1187, 963, and 784 cm−
1 on the IR (KBr) spectrum,wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (43, 44, 45, 46)
-
-
47. A process for preparing anhydrous aripiprazole crystals having low hygroscopicity, wherein said process comprises heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 3 using a Cu Kα
x-ray; andan endothermic curve which is substantially the same as the thermogravimetric or differential thermal analysis (heating rate 5°
C./min) curve shown inFIG. 1 ,wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
-
-
48. A process for preparing anhydrous aripiprazole crystals having low hygroscopicity, wherein said process comprises heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 3 using a Cu Kα
x-ray; andan endothermic curve which is substantially the same as the thermogravimetric or differential thermal analysis (heating rate 5°
C./min) curve shown inFIG. 1 ,wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
-
-
54. Anhydrous aripiprazole crystals having low hygroscopicity prepared by a process comprising heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=12.6°
, 15.4°
, 17.3°
, 18.0°
, 18.6°
, 22.5°
, and 24.8°
using a Cu Kα
x-ray;an endothermic curve comprising a first endothermic peak at about 71°
C. and a second endothermic peak around 60°
to 120°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan infrared absorption spectrum comprising infrared absorption bands at 2951, 2822, 1692, 1577, 1477, 1378, 1187, 963, and 784 cm−
1 on the IR (KBr) spectrum,wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (55, 56, 57, 58, 66, 67, 68, 69, 70)
-
-
59. Anhydrous aripiprazole crystals having low hygroscopicity prepared by a process comprising heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=12.6°
, 15.4°
, 17.3°
, 18.0°
, 18.6°
, 22.5°
, and 24.8°
using a Cu Kα
x-ray;an endothermic curve comprising a first endothermic peak at about 71°
C. and a second endothermic peak around 60°
to 120°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan infrared absorption spectrum comprising infrared absorption bands at 2951, 2822, 1692, 1577, 1477, 1378, 1187, 963, and 784 cm−
1 on the IR (KBr) spectrum,wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (60, 61, 62, 63)
-
-
64. Anhydrous aripiprazole crystals having low hygroscopicity prepared by a process comprising heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 3 using a Cu Kα
x-ray; andan endothermic curve which is substantially the same as the thermogravimetric or differential thermal analysis (heating rate 5°
C./min) curve shown inFIG. 1 ,wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
-
-
65. Anhydrous aripiprazole crystals having low hygroscopicity prepared by a process comprising heating hydrous aripiprazole having one or more of the following properties:
-
a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 3 using a Cu Kα
x-ray; andan endothermic curve which is substantially the same as the thermogravimetric or differential thermal analysis (heating rate 5°
C./min) curve shown inFIG. 1 ,wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
-
-
71. A pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity and at least one pharmaceutically acceptable carrier, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (72, 73, 74, 75, 77, 78, 79, 80, 81)
- C. and a humidity level of 100%,
-
76. A pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity and at least one pharmaceutically acceptable carrier, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
82. A pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity and at least one pharmaceutically acceptable carrier, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (83, 84, 85, 86, 88, 89, 90, 91, 92)
- C. and a humidity level of 100%,
-
87. A pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity and at least one pharmaceutically acceptable carrier, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
93. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (94, 95, 96, 97)
- C. and a humidity level of 100%,
-
98. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
99. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (100, 101, 102, 103)
- C. and a humidity level of 100%,
-
104. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
105. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (106, 107, 108, 109)
- C. and a humidity level of 100%,
-
110. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
111. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (112, 113, 114, 115)
- C. and a humidity level of 100%,
-
116. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
117. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (118, 119, 120, 121)
- C. and a humidity level of 100%,
-
122. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
123. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (124, 125, 126, 127)
- C. and a humidity level of 100%,
-
128. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
129. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (130, 131, 132, 133)
- C. and a humidity level of 100%,
-
134. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
135. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (136, 137, 138, 139)
- C. and a humidity level of 100%,
-
140. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
141. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (142, 143, 144, 145)
- C. and a humidity level of 100%,
-
146. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
147. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (148, 149, 150, 151)
- C. and a humidity level of 100%,
-
152. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
153. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (154, 155, 156, 157)
- C. and a humidity level of 100%,
-
158. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
159. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (160, 161, 162, 163)
- C. and a humidity level of 100%,
-
164. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
165. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (166, 167, 168, 169)
- C. and a humidity level of 100%,
-
170. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
171. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (172, 173, 174, 175)
- C. and a humidity level of 100%,
-
176. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
177. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (178, 179, 180, 181)
- C. and a humidity level of 100%,
-
182. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
183. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (184, 185, 186, 187)
- C. and a humidity level of 100%,
-
188. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
189. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (190, 191, 192, 193)
- C. and a humidity level of 100%,
-
194. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
195. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (196, 197, 198, 199)
- C. and a humidity level of 100%,
-
200. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
201. A method for the treatment of autism which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (202, 203, 204, 205)
- C. and a humidity level of 100%,
-
206. A method for the treatment of autism which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
207. A method for the treatment of autism which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (208, 209, 210, 211)
- C. and a humidity level of 100%,
-
212. A method for the treatment of autism which comprises administering to a patient in need thereof an effective amount of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
213. A method for the treatment of autism which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (214, 215, 216, 217)
- C. and a humidity level of 100%,
-
218. A method for the treatment of autism which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
219. A method for the treatment of autism which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (220, 221, 222, 223)
- C. and a humidity level of 100%,
-
224. A method for the treatment of autism which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals having low hygroscopicity per 1 kg of body weight, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
225. A method for the treatment of autism which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (226, 227, 228, 229)
- C. and a humidity level of 100%,
-
230. A method for the treatment of autism which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
231. A method for the treatment of autism which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (232, 233, 234, 235)
- C. and a humidity level of 100%,
-
236. A method for the treatment of autism which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
- C. and a humidity level of 100%,
-
237. A kit comprising:
-
a pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity in an amount effective to treat schizophrenia and at least one pharmaceutically acceptable carrier, and instructions for using the pharmaceutical composition to treat schizophrenia, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (238, 239, 240, 241)
-
-
242. A kit comprising:
-
a pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity in an amount effective to treat schizophrenia and at least one pharmaceutically acceptable carrier, and instructions for using the pharmaceutical composition to treat schizophrenia, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
-
-
243. A kit comprising:
-
a pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity in an amount effective to treat schizophrenia and at least one pharmaceutically acceptable carrier, and instructions for using the pharmaceutical composition to treat schizophrenia, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have one or more of the following properties; a powder x-ray diffraction spectrum comprising characteristic peaks at 2θ
=11.0°
, 16.6°
, 19.3°
, 20.3°
, and 22.1°
, using a Cu Kα
x-ray;an infrared absorption spectrum comprising infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960, and 779 cm−
1 on the IR (KBr) spectrum;an endothermic curve comprising an endothermic peak at about 141.5°
C. in a thermogravimetric or differential thermal analysis (heating rate 5°
C./min); andan endothermic curve comprising an endothermic peak at about 140.7°
C. in a differential scanning calorimetry analysis (heating rate 5°
C./min). - View Dependent Claims (244, 245, 246, 247)
-
-
248. A kit comprising:
-
a pharmaceutical composition comprising anhydrous aripiprazole crystals having low hygroscopicity in an amount effective to treat schizophrenia and at least one pharmaceutically acceptable carrier, and instructions for using the pharmaceutical composition to treat schizophrenia, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the anhydrous aripiprazole crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%,wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially the same as the powder x-ray diffraction spectrum shown in FIG. 5 using a Cu Kα
x-ray.
-
-
249. Anhydrous Aripiprazole Crystals B having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%,
wherein the Anhydrous Aripiprazole Crystals B have a mean particle size of 50 μ
m or less. - View Dependent Claims (250, 251, 252, 253, 254)
- C. and a humidity level of 100%,
-
255. Anhydrous Aripiprazole Crystals B having low hygroscopicity, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60°
- C. and a humidity level of 100%, wherein the Anhydrous Aripiprazole Crystals B have a mean particle size of 50 μ
m or less. - View Dependent Claims (256, 257, 258, 259, 260)
- C. and a humidity level of 100%, wherein the Anhydrous Aripiprazole Crystals B have a mean particle size of 50 μ
-
261. Anhydrous Aripiprazole Crystals B having low hygroscopicity prepared by a process comprising heating Hydrate A of aripiprazole,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
- View Dependent Claims (262, 263, 264, 265, 266)
-
267. Anhydrous Aripiprazole Crystals B having low hygroscopicity prepared by a process comprising heating Hydrate A of aripiprazole,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
- View Dependent Claims (268, 269, 270, 271, 272)
-
273. A pharmaceutical composition comprising Anhydrous Aripiprazole Crystals B having low hygroscopicity and at least one pharmaceutically acceptable carrier,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
- View Dependent Claims (274, 275, 276, 277, 278)
-
279. A pharmaceutical composition comprising Anhydrous Aripiprazole Crystals B having low hygroscopicity and at least one pharmaceutically acceptable carrier,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
- View Dependent Claims (280, 281, 282, 283, 284)
-
285. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
286. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
287. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
288. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
289. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
290. A method for the treatment of schizophrenia which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
291. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
292. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
293. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
294. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
295. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
296. A method for the treatment of bipolar disorder which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
297. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
298. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
299. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
300. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
301. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
302. A method for the treatment of anxiety, depression, or mania which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
303. A method for the treatment of autism which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
304. A method for the treatment of autism which comprises administering to a patient in need thereof an effective amount of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
305. A method for the treatment of autism which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
306. A method for the treatment of autism which comprises administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity per 1 kg of body weight,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
307. A method for the treatment of autism which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
308. A method for the treatment of autism which comprises administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals B having low hygroscopicity,
wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60° - C. and a humidity level of 100%.
-
309. A kit comprising:
-
a pharmaceutical composition comprising Anhydrous Aripiprazole Crystals B having low hygroscopicity in an amount effective to treat schizophrenia and at least one pharmaceutically acceptable carrier, and instructions for using the pharmaceutical composition to treat schizophrenia, wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%.
-
-
310. A kit comprising:
-
a pharmaceutical composition comprising Anhydrous Aripiprazole Crystals B having low hygroscopicity in an amount effective to treat schizophrenia and at least one pharmaceutically acceptable carrier, and instructions for using the pharmaceutical composition to treat schizophrenia, wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when the Anhydrous Aripiprazole Crystals B are placed for 24 hours in a dessicator maintained at a temperature of 60°
C. and a humidity level of 100%.
-
Specification
-
- Resources
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Litigation Data
-
Current AssigneeOtsuka Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
-
Original AssigneeOtsuka Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
-
InventorsBando, Takuji, Aoki, Satoshi, Kawasaki, Junichi, Ishigami, Makoto, Taniguchi, Youichi, Yabuuchi, Tsuyoshi, Fujimoto, Kiyoshi, Nishioka, Yoshihiro, Kobayashi, Noriyuki, Fujimura, Tsutomu, Takahashi, Masanori, Abe, Kaoru, Nakagawa, Tomonori, Shinhama, Koichi, Utsumi, Naoto, Tominaga, Michiaki, Ooi, Yoshihiro, Yamada, Shohei, Tomikawa, Kenji
-
Primary Examiner(s)Wilson, James O
-
Assistant Examiner(s)Sackey, Ebenezer O
-
Application NumberUS14/049,777Publication NumberTime in Patent Office972 DaysField of Search544/363, 514/253.07US Class Current1/1CPC Class CodesA61P 1/08 for nausea, cinetosis or ve...A61P 15/00 Drugs for genital or sexual...A61P 15/10 for impotenceA61P 25/00 Drugs for disorders of the ...A61P 25/04 Centrally acting analgesics...A61P 25/06 Antimigraine agentsA61P 25/16 Anti-Parkinson drugsA61P 25/18 Antipsychotics, i.e. neurol...A61P 25/20 Hypnotics; SedativesA61P 25/22 AnxiolyticsA61P 25/24 AntidepressantsA61P 25/28 for treating neurodegenerat...A61P 25/30 for treating abuse or depen...A61P 25/32 Alcohol-abuseA61P 3/04 Anorexiants; Antiobesity ag...C07B 2200/13 Crystalline forms, e.g. pol...C07D 215/22 attached in position 2 or 4C07D 215/227 only one oxygen atom which ...Y10T 428/2982 Particulate matter [e.g., s...
