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New brand of Aripipazole, and preparation method

A technology of aripiprazole and aripiprazole is applied in the application field of preparing medicine for treating schizophrenia, and can solve the problems of increased cost, complicated process, unfavorable industrialized production and the like

Active Publication Date: 2006-04-19
重庆凯林制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 1. Its bioavailability and solubility are worse than that of anhydrous aripiprazole;
[0007] 2. The change in the quantity of water-containing and anhydrous aripiprazole in each batch cannot meet the specifications set by the drug management agency;
[0008] 3. Grinding may cause the drug to be adsorbed on the equipment, resulting in increased cost and reduced yield;
Although the different crystal forms of aripiprazole prepared by the method described in this patent have low hygroscopicity, the process is cumbersome and consumes a lot of power costs, which is not conducive to large-scale industrial production of products

Method used

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  • New brand of Aripipazole, and preparation method
  • New brand of Aripipazole, and preparation method
  • New brand of Aripipazole, and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Add 10g of aripiprazole and 150ml of absolute ethanol into the three-port reaction with a reflux condenser, heat to reflux with stirring, and stop heating and stirring after the aripiprazole is completely dissolved. Cool the crystallization system to 50°C naturally, keep it warm at 50°C for 3 hours, let it cool down to room temperature naturally, crystallize at room temperature for 24 hours, freeze and crystallize at -4°C for 24 hours, suction filter, wash, and The obtained crystals were placed in a desiccator at 50°C, and dried under normal pressure for 24 hours to obtain 9.0 g of flaky aripiprazole crystals, yield: 90%, mp: 137.0-138.0°C.

Embodiment 2

[0061] Add 10g of aripiprazole and 120ml of absolute ethanol into the three-port reaction with a reflux condenser, heat to reflux under stirring, and stop heating and stirring after the aripiprazole is completely dissolved. Cool the crystallization system to room temperature naturally, crystallize at room temperature for 36 hours, freeze and crystallize at -10°C for 8 hours, suction filter, wash, place the obtained crystals in a desiccator at 60°C, and dry at normal pressure for 8 hours 9.3 g of flaky aripiprazole crystals were obtained, yield: 93%, mp: 137.5-138.5°C.

Embodiment 3

[0063] Add 10g of aripiprazole and 100ml of absolute ethanol into the three-port reaction with a reflux condenser, and heat to reflux under stirring. After the aripiprazole is completely dissolved, quickly drop 50ml of tetrahydrofuran into the crystallization system under stirring, about The dropwise addition was completed in 5 minutes, and after the stirring was even, stop heating and stirring. The crystallization system was naturally lowered to 60°C for 6 hours, then allowed to drop to 40°C, kept at 40°C for 2 hours, and finally allowed to cool down to room temperature, crystallized at room temperature for 6 hours, then frozen at -5°C After 18 hours of crystallization, suction filtration, washing, the obtained crystals were placed in a dryer at 75°C, and dried under normal pressure for 6 hours to obtain 8.8 g of flaky aripiprazole crystals, yield: 88%, mp: 137.0~ 138.0°C.

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Abstract

The novel crystal forms alpha and beta of airpiprazole, their preparing process, and their application in preparing medicine for treating schizophrenia are disclosed.

Description

technical field [0001] The invention relates to two new crystal forms of aripiprazole, a preparation method thereof, and an application in the preparation of medicaments for treating schizophrenia. In addition, the present invention also provides a pharmaceutical composition containing these specific crystal forms of aripiprazole. Background technique [0002] As we all know, aripiprazole is a quinolinone derivative, its chemical name is 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3 , 4-Dihydro-2(1H)-quinolinone. Invented by Otsuka Corporation of Japan in 1988, it was jointly developed with Bristol-Myers Bristol-Myers Squibb in the United States. It was approved by the U.S. FDA in 2002 and was marketed. It is currently clinically used to treat schizophrenia. [0003] Regarding the crystal form of aripiprazole, the fourth Japan-Korea Separation Technology Symposium Discussion Collection (October 6-8, 1996) pointed out that crystals of anhydrous aripiprazole exist as ...

Claims

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Application Information

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IPC IPC(8): C07D215/22A61K31/496A61K9/20A61K9/48A61P25/18
Inventor 诸葛明邢乃果张道林
Owner 重庆凯林制药有限公司
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