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Details for Patent: 8,901,130

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Details for Patent: 8,901,130

Title:Low hygroscopic aripiprazole drug substance and processes for the preparation
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.
Inventor(s): Bando; Takuji (Tokushima, JP), Aoki; Satoshi (Naruto, JP), Kawasaki; Junichi (Tokushima, JP), Ishigami; Makoto (Tokushima, JP), Taniguchi; Youichi (Tokushima, JP), Yabuuchi; Tsuyoshi (Tokushima, JP), Fujimoto; Kiyoshi (Naruto, JP), Nishioka; Yoshihiro (Tokushima, JP), Kobayashi; Noriyuki (Tokushima, JP), Fujimura; Tsutomu (Naruto, JP), Takahashi; Masanori (Tokushima, JP), Abe; Kaoru (Tokushima, JP), Nakagawa; Tomonori (Tokushima, JP), Shinhama; Koichi (Tokushima, JP), Utsumi; Naoto (Naruto, JP), Tominaga; Michiaki (Tokushima, JP), Ooi; Yoshihiro (Tokushima, JP), Yamada; Shohei (Tokushima, JP), Tomikawa; Kenji (Tokushima, JP)
Assignee: Ostuka Pharmaceutical Co., Ltd. (Tokyo, JP)
Filing Date:May 21, 2012
Application Number:13/476,758
Claims:1. Anhydrous Aripiprazole Crystals F.

2. A process for preparing Anhydrous Aripiprazole Crystals F comprising separating said Anhydrous Aripiprazole Crystals F from a heated suspension of aripiprazole in acetone.

3. The process according to claim 2, wherein the aripiprazole is chosen from type-I anhydrous aripiprazole crystals, type-II anhydrous aripiprazole crystals, and mixtures thereof.

4. The process according to claim 2, wherein the aripiprazole is chosen from Anhydrous Aripiprazole Crystals B, Anhydrous Aripiprazole Crystals C, Anhydrous Aripiprazole Crystals D, Anhydrous Aripiprazole Crystals E, Anhydrous Aripiprazole Crystals G, and mixtures thereof.

5. The process according to claim 2, wherein the aripiprazole is Anhydrous Aripiprazole Crystals B.

6. A process for preparing granules comprising: wet granulating Anhydrous Aripiprazole Crystals F and one or more pharmaceutically acceptable carriers to obtain granules of Anhydrous Aripiprazole Crystals F; drying the obtained granules at 70.degree. C. to 100.degree. C.; sizing the dried granules; and then drying the sized granules at 70.degree. C. to 100.degree. C. for 1 to 6 hours.

7. The process according to claim 6, wherein the granules are sized by the use of a sieve or a mill.

8. A process for preparing a pharmaceutical solid oral composition comprising drying a preparation comprising Anhydrous Aripiprazole Crystals F and at least one pharmaceutically acceptable carrier at 70.degree. C. to 100.degree. C.

9. A pharmaceutical solid oral composition comprising Anhydrous Aripiprazole Crystals F and at least one pharmaceutically acceptable carrier, wherein said pharmaceutical solid oral composition has at least one dissolution rate selected from the group consisting of 60% or more at pH 4.5 after 30 minutes, 70% or more at pH 4.5 after 60 minutes, and 55% or more at pH 5.0 after 60 minutes.

10. A pharmaceutical composition comprising Anhydrous Aripiprazole Crystals F and at least one pharmaceutically acceptable carrier.

11. Anhydrous Aripiprazole Crystals F prepared by a process comprising separating said Crystals from a heated suspension of aripiprazole in acetone.

12. The Anhydrous Aripiprazole Crystals F according to claim 11, wherein the aripiprazole is chosen from type-I anhydrous aripiprazole crystals, type-II anhydrous aripiprazole crystals, and mixtures thereof.

13. The Anhydrous Aripiprazole Crystals F according to claim 11, wherein the aripiprazole is chosen from Anhydrous Aripiprazole Crystals B, Anhydrous Aripiprazole Crystals C, Anhydrous Aripiprazole Crystals D, Anhydrous Aripiprazole Crystals E, Anhydrous Aripiprazole Crystals G, and mixtures thereof.

14. The Anhydrous Aripiprazole Crystals F according to claim 11, wherein the aripiprazole is Anhydrous Aripiprazole Crystals B.

15. A method of treating at least one disorder of the central nervous system comprising administering an effective amount of Anhydrous Aripiprazole Crystals F to a patient in need thereof, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism.

16. The method according to claim 15, wherein the at least one disorder of the central nervous system is schizophrenia.

17. The method according to claim 15, wherein the at least one disorder of the central nervous system is bipolar disorder.

18. The method according to claim 15, wherein the at least one disorder of the central nervous system is depression.

19. The method according to claim 15, wherein the at least one disorder of the central nervous system is autism.

20. A method of treating at least one disorder of the central nervous system comprising administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of Anhydrous Aripiprazole Crystals F per kilogram of patient body weight, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism.

21. A method of treating at least one disorder of the central nervous system comprising administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of Anhydrous Aripiprazole Crystals F, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism.

22. Anhydrous aripiprazole crystals having one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

23. The anhydrous aripiprazole crystals according to claim 22, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

24. The anhydrous aripiprazole crystals according to claim 22, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

25. The anhydrous aripiprazole crystals according to claim 22, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

26. Anhydrous aripiprazole crystals having one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

27. The anhydrous aripiprazole crystals according to claim 26, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

28. The anhydrous aripiprazole crystals according to claim 26, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

29. The anhydrous aripiprazole crystals according to claim 26, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

30. The anhydrous aripiprazole crystals according to any one of claim 22 or 26, wherein the anhydrous aripiprazole crystals are prepared by a process comprising separating the anhydrous aripiprazole crystals from a heated suspension of aripiprazole in acetone.

31. The anhydrous aripiprazole crystals according to claim 30, wherein said aripiprazole is chosen from type-I anhydrous aripiprazole crystals, type-II anhydrous aripiprazole crystals, and mixtures thereof.

32. The anhydrous aripiprazole crystals according to claim 30, wherein said aripiprazole is chosen from Anhydrous Aripiprazole Crystals B, Anhydrous Aripiprazole Crystals C, Anhydrous Aripiprazole Crystals E, Anhydrous Aripiprazole Crystals F, Anhydrous Aripiprazole Crystals G, and mixtures thereof.

33. The anhydrous aripiprazole crystals according to claim 30, wherein said aripiprazole is Anhydrous Aripiprazole Crystals B.

34. A process for preparing anhydrous aripiprazole crystals comprising separating the anhydrous aripiprazole crystals from a heated suspension of aripiprazole in acetone, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

35. The process according to claim 34, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

36. The process according to claim 34, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

37. The process according to claim 34, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

38. A process for preparing anhydrous aripiprazole crystals comprising separating the anhydrous aripiprazole crystals from a heated suspension of aripiprazole in acetone, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

39. The process according to claim 38, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

40. The process according to claim 38, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

41. The process according to claim 38, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

42. A process for preparing granules comprising: wet granulating anhydrous aripiprazole crystals and one or more pharmaceutically acceptable carriers to obtain granules of the anhydrous aripiprazole crystals; drying the obtained granules at 70.degree. C. to 100.degree. C.; sizing the dried granules; and then drying the sized granules at 70.degree. C. to 100.degree. C. for 1 to 6 hours, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

43. The process according to claim 42, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

44. The process according to claim 42, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

45. The process according to claim 42, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

46. A process for preparing granules comprising: wet granulating anhydrous aripiprazole crystals and one or more pharmaceutically acceptable carriers to obtain granules of the anhydrous aripiprazole crystals; drying the obtained granules at 70.degree. C. to 100.degree. C.; sizing the dried granules; and then drying the sized granules at 70.degree. C. to 100.degree. C. for 1 to 6 hours, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

47. The process according to claim 46, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

48. The process according to claim 46, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

49. The process according to claim 46, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

50. The process according to any one of claims 42 to 49, wherein the granules are sized by the use of a sieve or a mill.

51. A process for preparing a pharmaceutical solid oral composition comprising drying a preparation comprising anhydrous aripiprazole crystals and at least one pharmaceutically acceptable carrier at 70.degree. C. to 100.degree. C., wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

52. The process according to claim 51, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

53. The process according to claim 51, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

54. The process according to claim 51, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

55. A process for preparing a pharmaceutical solid oral composition comprising drying a preparation comprising anhydrous aripiprazole crystals and at least one pharmaceutically acceptable carrier at 70.degree. C. to 100.degree. C., wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

56. The process according to claim 55, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

57. The process according to claim 55, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

58. The process according to claim 55, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

59. A pharmaceutical solid oral composition comprising anhydrous aripiprazole crystals and at least one pharmaceutically acceptable carrier, wherein said pharmaceutical solid oral composition has at least one dissolution rate selected from the group consisting of 60% or more at pH 4.5 after 30 minutes, 70% or more at pH 4.5 after 60 minutes; and 55% or more at pH 5.0 after 60 minutes, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

60. The pharmaceutical solid oral composition according to claim 59, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

61. The pharmaceutical solid oral composition according to claim 59, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

62. The pharmaceutical solid oral composition according to claim 59, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

63. A pharmaceutical solid oral composition comprising anhydrous aripiprazole crystals and at least one pharmaceutically acceptable carrier, wherein said pharmaceutical solid oral composition has at least one dissolution rate selected from the group consisting of 60% or more at pH 4.5 after 30 minutes, 70% or more at pH 4.5 after 60 minutes; and 55% or more at pH 5.0 after 60 minutes, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

64. The pharmaceutical solid oral composition according to claim 63, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

65. The pharmaceutical solid oral composition according to claim 63, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

66. The pharmaceutical solid oral composition according to claim 63, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

67. A pharmaceutical composition comprising anhydrous aripiprazole crystals and at least one pharmaceutically acceptable carrier, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

68. The pharmaceutical composition according to claim 67, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

69. The pharmaceutical composition according to claim 67, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

70. The pharmaceutical composition according to claim 67, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

71. A pharmaceutical composition comprising anhydrous aripiprazole crystals and at least one pharmaceutically acceptable carrier, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

72. The pharmaceutical composition according to claim 71, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

73. The pharmaceutical composition according to claim 71, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

74. The pharmaceutical composition according to claim 71, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

75. A method of treating at least one disorder of the central nervous system comprising administering an effective amount of anhydrous aripiprazole crystals, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min), wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism.

76. The method according to claim 75, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 28=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

77. The method according to claim 75, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

78. The method according to claim 75, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

79. A method of treating at least one disorder of the central nervous system comprising administering an effective amount of anhydrous aripiprazole crystals, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism.

80. The method according to claim 79, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

81. The method according to claim 79, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

82. The method according to claim 79, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

83. The method according to any one of claims 75 to 82, wherein the at least one disorder of the central nervous system is schizophrenia.

84. The method according to any one of claims 75 to 82, wherein the at least one disorder of the central nervous system is bipolar disorder.

85. The method according to any one of claims 75 to 82, wherein the at least one disorder of the central nervous system is depression.

86. The method according to any one of claims 75 to 82, wherein the at least one disorder of the central nervous system is autism.

87. A method of treating at least one disorder of the central nervous system comprising administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals per 1 kg of body weight, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

88. The method according to claim 87, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

89. The method according to claim 87, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

90. The method according to claim 87, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

91. A method of treating at least one disorder of the central nervous system comprising administering to a patient in need thereof from about 0.1 milligrams to about 10 milligrams of anhydrous aripiprazole crystals per 1 kg of body weight, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

92. The method according to claim 91, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

93. The method according to claim 91, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

94. The method according to claim 91, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

95. A method of treating at least one disorder of the central nervous system comprising administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

96. The method according to claim 95, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=11.3.degree., 13.3.degree., 15.4.degree., 22.8.degree., 25.2.degree., and 26.9.degree., using a Cu K.sub..alpha. x-ray.

97. The method according to claim 95, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum comprising infrared absorption bands at 2940, 2815, 1679, 1383, 1273, 1177, 1035, 963, and 790 cm.sup.-1 on the IR (KBr) spectrum.

98. The method according to claim 95, wherein the anhydrous aripiprazole crystals have an endothermic curve comprising endothermic peaks at about 137.5.degree. C. and about 149.8.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min).

99. A method of treating at least one disorder of the central nervous system comprising administering to a patient in need thereof a unit dose comprising from about 1 milligram to about 100 milligrams of anhydrous aripiprazole crystals, wherein the at least one disorder of the central nervous system is chosen from schizophrenia, anxiety, mania, bipolar disorder, depression, and autism, wherein the anhydrous aripiprazole crystals have one or more of the following properties: a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray; an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25; and an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

100. The method according to claim 99, wherein the anhydrous aripiprazole crystals have a powder x-ray diffraction spectrum which is substantially identical to the powder x-ray diffraction spectrum shown in FIG. 24 using a Cu K.sub..alpha. x-ray.

101. The method according to claim 99, wherein the anhydrous aripiprazole crystals have an infrared absorption spectrum which is substantially identical to the IR (KBr) spectrum shown in FIG. 25.

102. The method according to claim 99, wherein the anhydrous aripiprazole crystals have an endothermic curve which is substantially identical to the thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) curve shown in FIG. 22.

103. The process according to any one of claims 2, 37, and 38, wherein the suspension is heated at about the boiling point of acetone for about 5 to 10 hours.

104. The Anhydrous Aripiprazole Crystals F according to claim 11, wherein the suspension is heated at about the boiling point of acetone for about 5 to 10 hours.

105. The anhydrous aripiprazole crystals according to claim 30, wherein the suspension is heated at about the boiling point of acetone for about 5 to 10 hours.
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