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Crystal forms of vortioxetine organic acid salt and preparation method thereof

A technology of vortioxetine and crystal form, applied in organic chemistry, nervous system diseases, drug combination, etc., can solve the problems of strong corrosion, toxicity, and difficult handling of hydrobromic acid, and achieve improved water solubility and bioavailability Improve and enhance the effect of the application range

Inactive Publication Date: 2015-05-20
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Hydrobromide has disadvantages due to the hydrobromic acid used in its production process, namely hydrobromic acid is highly corrosive and toxic and difficult to handle industrially

Method used

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  • Crystal forms of vortioxetine organic acid salt and preparation method thereof
  • Crystal forms of vortioxetine organic acid salt and preparation method thereof
  • Crystal forms of vortioxetine organic acid salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Embodiment 1: Preparation of vortioxetine p-hydroxybenzoate hydrate

[0102] Add 2.9g of vortioxetine into 15ml of acetone:water (1:1) mixed solvent, and heat to 60°C, add 1.4g of p-hydroxybenzoic acid, stir and dissolve, continue to stir for 2 hours, then cool down naturally to At 30°C, a white solid precipitated, filtered with suction, and dried in a vacuum oven (40-50°C) to obtain Vortioxetine p-hydroxybenzoate hydrate.

Embodiment 2

[0103] Embodiment 2: Preparation of vortioxetine p-hydroxybenzoate hydrate

[0104] Add 15g of vortioxetine to 150ml of ethyl acetate, heat to 50°C to dissolve, dissolve 7.0g of p-hydroxybenzoic acid in 10ml of hot water and add dropwise to the vortioxetine solution, stir for 1 hour, and cool down naturally to At 20°C, white crystals slowly precipitated. After 48 hours, the white solid was obtained by suction filtration, and dried in a vacuum oven (40-50°C) to obtain vortioxetine p-hydroxybenzoate hydrate.

Embodiment 3

[0105] Embodiment 3: Preparation of vortioxetine p-hydroxybenzoate hydrate

[0106] Dissolve 2.9g of vortioxetine in 120ml of 10% ethanol aqueous solution, add 1.4g of p-hydroxybenzoic acid, heat to 70°C, continue to stir for 2h, after dissolving, take it to an ice-water bath for crystallization at 0°C, and slowly precipitate white crystals After 24 hours, the white solid was obtained by suction filtration, and dried in a vacuum oven (40-50° C.) to obtain vortioxetine p-hydroxybenzoate hydrate.

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PUM

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Abstract

The invention belongs to the technical field of medicines and particularly relates to vortioxetine p-hydroxy benzoate comprising an anhydrous crystal form and a hydrate crystal form of vortioxetine p-hydroxy benzoate as well as a preparation method and application of vortioxetine p-hydroxy benzoate. The preparation method comprises the following steps of reacting vortioxetine and p-hydroxy benzoic acid in an organic solvent or a mixed solvent system of an organic solvent and water to produce salt, carrying out heat preservation or cooling and crystallizing to obtain vortioxetine p-hydroxy benzoate. The solubility, stability, flowability, compressibility and the like of prepared vortioxetine p-hydroxy benzoate are greatly improved compared with those of vortioxetine, which is conductive to preparing pharmaceutical preparations and improving the quality.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to vortioxetine p-hydroxybenzoate, a preparation method and its application in the manufacture of medicines for treating depression. Background technique [0002] Salt formation of drugs is currently the main method to modify the physical and chemical properties of drug molecules, which can improve some unsatisfactory physicochemical or biological properties of drugs, such as changing the solubility or dissolution rate of drugs, reducing hygroscopicity, improving stability, changing melting point, improving Grindability and compressibility, easy preparation and purification, improved permeability, etc. Each salt form of a drug has unique properties, and the final determination of the salt form is actually to find a balance between physicochemical properties and biological properties. Polymorphic forms of a salt form may exist. The phenomenon of polymorphism is not on...

Claims

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Application Information

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IPC IPC(8): C07D295/096A61K31/495A61P25/24
CPCC07D295/096
Inventor 胡秀荣周新波吴素香顾建明
Owner ZHEJIANG UNIV
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