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Claims for Patent: 8,399,469

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Claims for Patent: 8,399,469

Title:Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
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: Otsuka Pharmaceutical Co., Ltd. (Chiyoda-ku, Tokyo, JP)
Application Number:11/790,604
Patent Claims: 1. Hydrate A of aripiprazole characterized by one or more of the properties chosen from: a powder x-ray diffraction spectrum comprising characteristic peaks at 20=12.6.degree. , 15.4.degree. , 17.3.degree. , 18.0.degree. , 18.6.degree. , 22.5.degree. and 24.8.degree. using a Cu K.sub..alpha.x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2951, 2822, 1692, 1577, 1447, 1378, 1187, 963 and 784 cm.sup.-1 on the IR (KBr) spectrum; and an endothermic trace comprising an endothermic peak at about 71.degree. C. and a second endothermic peak around 60.degree. C. to 120.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C/min).

2. Hydrate A of aripiprazole according to claim 1, wherein said Hydrate has a mean particle size of 50 .mu.m or less.

3. Hydrate A of aripiprazole accoding to claim 2, wherein said Hydrate has a mean particle size range of 36 to 14 .mu.m.

4. A process for preparing Hydrate A of aripiprazole wherein said process comprises milling Aripiprazole Hydrate characterized by one or more of the properties chosen from: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=12. 6.degree. , 15.1.degree. , 17.4.degree. , 18.2.degree. , 18.7.degree. , 24.8.degree. and 27.5.degree. using a Cu K.sub..alpha.x-ray; and an endothermic trace comprising endothermic peaks at 75.0.degree. C., 123.5.degree. C. and 140. 5.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min) to a mean particle size of 50 .mu.m or less.

5. A process according to claim 4, wherein said milling is performed by an atomizer using a rotational speed of 5000-15000 rpm for the main axis, a feed rotation of 10-30 rpm and a screen hole size of 1-5 mm.

6. Hydrate A of aripiprazole made by a pocess comprising milling Aripiprazole Hydrate characterized by one or more of the properties chosen from: a powder x-ray diffraction spectrum having characteristic peaks at 2.theta.=12.6.degree. , 15.1.degree. , 17.4.degree. , 18.2.degree. , 18.7.degree. , 24.8.degree. and 27.5.degree. using a Cu K.sub..alpha.x-ray; and an endothermic trace comprising endothermic peaks at 75.0.degree. C., 123.5.degree. C. and 140. 5.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C/min) to a mean particle size of 50 .mu.m or less.

7. Hydrate A of aripiprazole according to claim 6, wherein said milling is performed by an atomizer using a rotational speed of 5000-15000 rpm for the main axis, a feed rotation of 10-30 rpm and a screen hole size of 1-5 mm.

8. Hydrate A of aripiprazole according to claim 2, wherein said hydrate has a mean particle size of 20 .mu.m or less.

9. Hydrate A of aripiprazole according to claim 2, wherein the mean particle size is measured using a laser diffraction particle size analyzer.

10. Hydrate A of aripiprazole according to claim 3, wherein the mean particle size is measured using a laser diffraction particle size analyzer.

11. Hydrate A of aripiprazole according to claim 8, wherein the mean particle size is measured using a laser diffraction particle size analyzer.

12. The process according to claim 4, wherein the Hydrate A of aripiprazole is characterized by one or more properties chosen from: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=12.6.degree. , 15.4.degree. , 17.3.degree. , 18.0.degree. , 18.6.degree. , 22.5.degree. and 24.8.degree. using a Cu K.sub..theta.x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2951, 2822, 1692, 1577, 1447, 1378, 1187, 963 and 784 cm.sup.-1 on the IR (KBr) spectrum; an endothermic trace comprising an endothermic peak at about 71.degree. C. and a second endothermic peak around 60.degree. C. to 120.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 520 C./min); and a mean particle size of 50 .mu.m or less.

13. Hydrate A of aripiprazole according to claim 6, wherein the Hydrate A of aripiprazole is characterized by one or more properties chosen from: a powder x-ray diffraction spectrum comprising characteristic peaks at 2.theta.=12.6.degree. , 15.4.degree. , 17.3.degree. , 18.0.degree. , 18.6.degree. , 22.5.degree. and 24.8.degree. using a Cu K.sub..alpha.x-ray; an infrared absorption spectrum comprising infrared absorption bands at 2951, 2822, 1692, 1577, 1447, 1378, 1187, 963 and 784 cm.sup.-1 on the IR (KBr) spectrum; an endothermic trace comprising an endothermic peak at about 71.degree. C. and a second endothermic peak around 60.degree. C. to 120.degree. C. in a thermogravimetric or differential thermal analysis (heating rate 5.degree. C./min); and a mean particle size of 50 .mu.m or less.

14. Hydrate A of aripiprazole according to any one of claims 9, 10, or 11, wherein the mean particle size is measured by suspending 0.1 g of the Hydrate A of aripiprazole in a 20 mL n-hexane solution of 0.5 g soy lecithin.

15. Hydrate A of aripiprazole according to any one of claims 6, 7, or 13, wherein the mean particle size is measured by suspending 0.1 g of the Hydrate A of aripiprazole in a 20 mL n-hexane solution of 0.5 g soy lecithin using a laser diffraction particle size analyzer.

16. The process according to any one of claim 4 or 12, wherein the mean particle size is measured by suspending 0.1 g of the Hydrate A of aripiprazole in a 20 mL n-hexane solution of 0.5 g soy lecithin using a laser diffraction particle size analyzer.
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