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Brexpiprazole crystal, its preparation method and application, and pharmaceutical composition comprising brexpiprazole crystal

A technology of epirazole and a composition, applied in the field of medicinal chemistry, can solve the problems such as few crystal forms of epirazole, and achieve the effects of low cost, good stability and simple preparation

Inactive Publication Date: 2017-05-10
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are very few reports on the crystal form of epirizopridine

Method used

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  • Brexpiprazole crystal, its preparation method and application, and pharmaceutical composition comprising brexpiprazole crystal
  • Brexpiprazole crystal, its preparation method and application, and pharmaceutical composition comprising brexpiprazole crystal
  • Brexpiprazole crystal, its preparation method and application, and pharmaceutical composition comprising brexpiprazole crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation method of the crystalline form of Epirizopril:

[0036] Put 500.0mg of epirazole powder in a test tube, slowly add isopropanol at 80°C until it just completely dissolves (approximately 12mL of isopropanol is added), cool slowly to 20°C, gradually crystallize, pump Filter and air-dry at 85±5°C for 4 hours to obtain a white powder. Table 1 shows the X-ray powder diffraction data of the crystal form of the sample obtained in this embodiment.

[0037] The X-ray powder diffraction pattern (XRPD pattern) of crystal form is as figure 1 Shown; The crystal form begins to show an endothermic peak when it is heated to 184.3 ° C, and its differential scanning calorimetry (DSC chart) is shown in figure 2 Shown; When the crystal form is heated to 340 ° C, it has a weight loss gradient, and its thermogravimetric analysis diagram (TGA diagram) is as follows image 3 shown.

[0038] The X-ray powder diffraction data of table 1 epizopra crystal form

[0039]

[0...

Embodiment 2

[0042] The preparation method of the crystalline form of Epirizopril:

[0043] Put 500.0 mg of Epirizopam powder in a test tube, add 10 ml of tetrahydrofuran at 65°C, dissolve, slowly cool to 0°C, gradually crystallize, filter with suction, and air-dry at 85±5°C for 5 hours to obtain white powder.

Embodiment 3

[0045] The preparation method of the crystalline form of Epirizopril:

[0046] Put 500.0mg of Epirizopam powder in a test tube, slowly add 25mL of ethyl acetate at 78°C, dissolve it, cool slowly to -10°C, gradually crystallize, filter with suction, and air-dry at 85±5°C for 4h A white powder was obtained.

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Abstract

The invention belongs to the technical field of pharmaceutical chemistry and particularly relates to brexpiprazole crystal, its preparation method and application, and a pharmaceutical composition comprising the brexpiprazole crystal. X-ray powder diffraction spectrum of the brexpiprazole crystal has characteristic peaks at 2Theta=6.7+ / -0.2 degree, 12.2+ / -0.2 degree, 14.4+ / -0.2 degree, 17.3+ / -0.2 degree, 19.1+ / -0.2 degree, 20.1+ / -0.2 degree, 21.3+ / -0.2 degree and 23.1+ / -0.2 degree. The brexpiprazole crystal has good stability and low hygroscopicity; the brexpiprazole crystal is simple to prepare, low in cost, suitable for industrial production, and is of important value to the development of pharmaceutical preparations in future.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a crystal form of epirazole, a preparation method and use thereof, and a pharmaceutical composition. Background technique [0002] Brexpiprazole (brexpiprazole) is the first dopamine, partial 5-HT1A receptor agonist and 5-HT2A receptor antagonist compound developed by Otsuka Pharmaceutical Co., Ltd., which has a wide range of activities in multiple monoamine systems. The activity of partial agonists of dopamine D2 receptors is decreased, and the affinity for specific 5-HT receptors (such as 5-HT1A, 5-HT2A, 5-HT7) is increased, which has better efficacy and tolerance, and can reduce the risk of Adverse effects such as akathisia, restlessness and / or insomnia. On July 10, 2015, the US FDA approved its marketing. Epirizoprazole is the next-generation product of aripiprazole developed by Otsuka Pharmaceutical Co., Ltd. It is a clinically meaningful multi-targ...

Claims

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Application Information

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IPC IPC(8): C07D409/12A61K31/496A61P25/18
CPCC07D409/12C07B2200/13
Inventor 苗得足胡清文王宏光李乐祥于志波
Owner REYOUNG PHARMA
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