Preparation method of alpha crystal form of vortioxetine hydrobromide

A technology for vortioxetine hydrobromide salt and crystal form, which is applied in the field of pharmaceutical preparation, can solve the problems of large particle size and low purity of vortioxetine hydrobromide α crystal form, and achieves high crystal form purity and high crystallinity. Better performance and stability

Inactive Publication Date: 2018-05-25
ZHEJIANG JINGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Aiming at the problems of desolvation in the prior art, low purity of α crystal form of vortioxetine hydrobromide and large particle size, the present invention provides a simpler vortioxetine hydrobromide Preparation method of α crystal form

Method used

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  • Preparation method of alpha crystal form of vortioxetine hydrobromide
  • Preparation method of alpha crystal form of vortioxetine hydrobromide
  • Preparation method of alpha crystal form of vortioxetine hydrobromide

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Take 4 g of crude vortioxetine hydrobromide, add it to 35 ml of 40% v / v ethanol aqueous solution, heat to 70° C. and reflux and stir for 2 hours until clarification. The clarified solution was lowered to room temperature, then 0.1 g of vortioxetine hydrobromide α crystal form was added as a seed crystal, cooled and crystallized in an ice-water bath for half an hour, suction filtered and dried to obtain 3.8 g of vortioxetine Hydrobromide crystals. According to the X-ray powder diffraction determination, it is the α crystal form of vortioxetine hydrobromide. For the results, see figure 2 .

Embodiment 2

[0033] Take 4 g of crude vortioxetine hydrobromide, add it into 16 ml of chloroform, heat to 50°C and stir to clarify. Cool down to room temperature or place in an ice-water bath, then add 0.2g vortioxetine hydrobromide α crystal form as seed crystal, cool and crystallize for 2 to 4 hours, suction filter and dry to obtain 3.8g vortioxetine Hydrobromide crystals. Determined by X-ray powder diffraction, it is vortioxetine hydrobromide α crystal form, and the result is the same as figure 2 match.

Embodiment 3

[0035] Take 4 g of crude vortioxetine hydrobromide, add it into 50% v / v methanol aqueous solution (16 ml), heat up and stir to dissolve, and obtain a clear solution. The clear solution was placed in an ice bath, and 0.1 g of vortioxetine hydrobromide α crystal was added as a seed crystal. After crystallization, filtration and drying, 3.2 g of vortioxetine hydrobromide crystals were obtained. Determined by X-ray powder diffraction, it is vortioxetine hydrobromide α crystal form, and the result is the same as figure 2 match.

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Abstract

The invention discloses a preparation method of an alpha crystal form of vortioxetine hydrobromide. The alpha crystal form, obtained with the method, of vortioxetine hydrobromide has high purity, goodcrystallinity, high stability and particle uniformity. The preparation process is simple, good in repeatability, high in yield and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and relates to the preparation of antidepressant drug vortioxetine hydrobromide crystal form, in particular to a preparation method of vortioxetine hydrobromide α crystal form. Background technique [0002] Depression is a mental disorder with a high prevalence rate, high recurrence rate, and high suicide rate. It is prone to physical dysfunction and cognitive impairment, causing great harm to individuals and families. According to the report of the World Health Organization, it is estimated that by 2020, depression will become the second most burdensome disease after heart disease. [0003] Vortioxetine, the chemical name is 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine, which can inhibit the reuptake of serotonin and has 5-HT1A receptor 5-HT1B receptor agonists, 5-HT1B receptor partial agonists, and 5-HT3, 5-HT1D, and 5-HT7 receptor antagonists; the diversity of the drug's actions allo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/096
CPCC07D295/096C07B2200/13
Inventor 朱建荣周薪波张中良张林海胡秀荣
Owner ZHEJIANG JINGXIN PHARMA
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