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Aspartate of vortioxetine or hydrate thereof as well as preparation method and application thereof

A technology of aspartate and vortioxetine, which is applied in the field of medicine and can solve the problems of human injury and harm

Active Publication Date: 2015-05-13
SHANGYU JINGXIN PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, salts such as hydrobromide of vortioxetine may have inactive anions with unfavorable or even harmful properties, which in turn may cause damage to the human body

Method used

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  • Aspartate of vortioxetine or hydrate thereof as well as preparation method and application thereof
  • Aspartate of vortioxetine or hydrate thereof as well as preparation method and application thereof
  • Aspartate of vortioxetine or hydrate thereof as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0083] Embodiment 1: Preparation of vortioxetine aspartate dihydrate

[0084] Suspend 2.9g vortioxetine in 15ml water, heat to 80°C, add 1.3g aspartic acid, stir to dissolve, continue to stir for 2 hours, cool down naturally, and slowly precipitate white crystals after reaching room temperature, filter with suction , to obtain a white solid, put it in a vacuum drying oven (40-50° C.) and dry it to obtain vortioxetine aspartate dihydrate.

Embodiment 2

[0085] Embodiment 2: Preparation of vortioxetine aspartate dihydrate

[0086] Dissolve 15g of vortioxetine in 150ml of ethyl acetate, dissolve 6.5g of aspartic acid in 10ml of hot water and add dropwise into the vortioxetine solution, stir for 1 hour, cool down naturally, and slowly precipitate out after reaching room temperature White crystals. After 48 hours, the white solid was obtained by suction filtration, and dried in a vacuum oven (40-50° C.) to obtain vortioxetine aspartate dihydrate.

Embodiment 3

[0087] Embodiment 3: Preparation of vortioxetine aspartate dihydrate

[0088] Dissolve 2.9g of vortioxetine in 120ml of 5% ethanol aqueous solution, add 1.3g of aspartic acid, heat to 70°C, continue to stir, after dissolving, cool down naturally, and slowly precipitate white crystals after reaching room temperature, after 24 hours , filtered with suction to obtain a white solid, which was dried in a vacuum oven (40-50° C.) to obtain vortioxetine aspartate dihydrate.

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Abstract

The invention provides aspartate of vortioxetine or hydrate thereof, comprising anhydrous crystal form, semihydrate crystal form and dihydrate crystal form of aspartate of vortioxetine, as well as a preparation method and application thereof. The preparation method comprises the following steps: performing a reaction on the vortioxetine and the aspartic acid in the organic solvent or the mixed solvent of the organic solvent and the water for generating the aspartate, keeping the temperature or cooling and crystallizing. The aspartate of the vortioxetine has the function of treating major depressive disorder and also has the function of the aspartic acid, so that the defect of the inorganic acid salt to the human body is effectively compensated by the aspartate. The solubility, stability and bioavailability of the aspartate are greatly improved. The equilibrium solubility shows that the solubility of the aspartate of the vortioxetine (at 37 DEG C) is more than 7 times of that of the hydrobromide of the vortioxetine.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an aspartate salt of vortioxetine, a preparation method and an application thereof. Background technique [0002] Major depressive disorder (MDD) is a common mood disorder that is widespread worldwide, causing great harm to individuals and families, and seriously affecting social and economic development. Current antidepressants include tricyclic antidepressants (TCAs), selective norepinephrine reuptake inhibitors (NARIs), reversible, selective monoamine oxidase inhibitors (RIMAs), selective serotonin (5- HT) reuptake inhibitors (SSRIs) and selective serotonin (5-HT) and norepinephrine reuptake inhibitors (SNRIs). [0003] Vortioxetine (Vortioxetine), the chemical name is 1-[2-(2,4-dimethylphenylsulfanyl) phenyl] piperazine, an antidepressant developed by Takeda Pharma (Takeda), It mainly treats CNS-related diseases. In September 2013, it was approved by the US FDA under the tra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/096A61K31/495A61P25/24A61P1/16A61P37/00A61P9/04
CPCC07D295/096
Inventor 胡秀荣周新波
Owner SHANGYU JINGXIN PHARMA
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