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Dexoxiracetam crystal form II and its preparation method and use

A crystal form and crystallization technology, which is applied in the field of Dexoxiracetam, can solve the problems of disclosure, less research on the crystal form of Dexoxiracetam, and no crystal form of Dexoxiracetam.

Active Publication Date: 2020-03-20
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few studies on the preparation method and crystal form of Dexoxiracetam, and there is no disclosure of the crystal form of Dexoxiracetam

Method used

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  • Dexoxiracetam crystal form II and its preparation method and use
  • Dexoxiracetam crystal form II and its preparation method and use
  • Dexoxiracetam crystal form II and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Dissolve 1g of dexoxiracetam (Chongqing Runze Pharmaceutical Co., Ltd.) in 6mL of mixed solvent (DMF 2mL, dichloromethane 4mL) solution, heat to dissolve at 50°C, filter, seal the filtrate, and dissolve at 100~ Stir at a speed of 150r / min for about 15h, and filter again. After filtration, the filtrate is placed in a desiccator to evaporate the solvent to form crystals, collect the crystals, and dry the collected crystals at 30±2°C and a relative humidity of 80-85%. After 5-6h, the crystals of D-oxiracetam were obtained.

Embodiment 2

[0041] The dextro-oxiracetam crystal that embodiment 1 obtains is carried out powder diffraction experiment:

[0042] Powder Diffraction Determination (XRPD):

[0043] Test instrument conditions: use Bruker D2 PHASER powder diffractometer to carry out normal temperature test, test conditions are: with Cu Ka ( ) is the light source, the voltage is 30kV, the current is 10mA, the test step size is 0.014°, the scanning speed is 0.1s / step, and the scanning range is 5-40° (2θ). After testing, the D-oxiracetam crystal prepared in Example 1 has diffraction angles 2θ of 10.54±0.2°, 13.76±0.2°, 14.14±0.2°, 16.64±0.2°, 17.76±0.2°, 18.72±0.2° , 20.16±0.2°, 21.20±0.2°, 21.52±0.2°, 23.25±0.2°, 24.17±0.2°, 25.88±0.2°, 27.61±0.2°, 28.57±0.2°, 29.24±0.2°, 31.40±0.2° There are diffraction peaks, for the sake of convenience, this crystal is called "dextro-oxiracetam crystal form II"; its powder diffraction pattern is shown in figure 1 . Depend on figure 1 It can be seen from the analytic...

Embodiment 3

[0049] Dissolve 1g of Dexoxiracetam in 5mL of mixed solvent (DMF 1mL, ethyl acetate 4mL), heat to dissolve at 35°C, filter, cover and seal the filtrate, and stir at a speed of about 150r / min for about 12h , filtered again, and after filtration, the filtrate was allowed to stand in a desiccator to evaporate the solvent to form crystals, and the crystals were collected, and the collected crystals were dried at 30±2° C. and a relative humidity of 75-80% for 4-5 hours to obtain crystals; According to the method identification in Example 2, it is Dexoxiracetam crystal form II.

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Abstract

The present invention provides a crystal form of dextro-oxiracetam, which has a diffraction angle of 2 θ is There are diffraction peaks at 17.76±0.2°, 20.16±0.2°, 21.20±0.2°, 24.17±0.2°, 25.88±0.2°; the crystal form of Dexoxiracetam can promote the synthesis of phosphorylcholine and o-acethanolamine, and promote Brain metabolism, stimulates specific central nervous pathways through the blood-brain barrier, and has special biological activities in the fields of sedation and antiepileptic. The dextro-oxiracetam crystal form of the present invention is a crystal form containing 0.5 water molecules, loses crystal water at 73.5±2°C, and melts and decomposes at 138.0±2°C. The dextro-oxiracetam crystal form of the present invention can exist stably at room temperature and relative humidity of 0-95%, does not undergo crystal transformation, is used for storage or preparation processing, and has relatively high requirements for processing humidity or storage condition humidity. Low.

Description

technical field [0001] The present invention relates to dexoxiracetam, in particular to the crystal form, preparation method and application of dexoxiracetam. Background technique [0002] Oxiracetam (Oxiracetam), CAS No. 62613-82-5, was synthesized for the first time in 1974 by the Italian company Skrbechem, and it is a new generation of brain metabolism-improving drug listed in 1987, which can promote phosphorylcholine and adjacent Acetyl ethanolamine synthesis, promote brain metabolism, stimulate specific central nervous pathways through the blood-brain barrier, improve intelligence and memory. Studies have shown that its dextrorotary form (dexoxiracetam) has special biological activities in the fields of sedation and antiepileptics, and its toxicity is low, and the drug safety range is large. It is expected to become the first choice of existing highly toxic antiepileptic drugs substitute. [0003] [0004] To effectively develop Dexoxiracetam into a pharmaceutical,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/273A61K31/4015A61P25/08
CPCC07D207/273C07B2200/07C07B2200/13A61P25/08A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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