Dextro-oxiracetam crystal form II, and preparation method and application thereof

A crystal form and crystallization technology, which is applied in the field of Dexo-oxiracetam, can solve the problems that there are few researches on the crystal form of Dexo-oxiracetam, and there are no crystal forms and disclosures of Dexo-oxiracetam.

Active Publication Date: 2018-05-01
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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  • Dextro-oxiracetam crystal form II, and preparation method and application thereof
  • Dextro-oxiracetam crystal form II, and preparation method and application thereof
  • Dextro-oxiracetam crystal form II, and preparation method and application thereof

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 dextro-oxiracetam crystal form. The crystal form has diffraction peaks at diffraction angles 2theta of 17.76+/-0.2 DEG, 20.16+/-0.2 DEG, 21.20+/-0.2 DEG, 24.17+/-0.2 DEG, and 25.88+/-0.2 DEG. The dextro-oxiracetam crystal form can promote synthesis of phosphorylcholine and o-phosphorylethanolamine, promote brain metabolism, and generate stimulatory effect on specific central nervous pathways through a blood-brain barrier, and has special biological activity in areas such as sedation, anti-epilepsy and the like. The dextro-oxiracetam crystal form can exist stably under conditions of room temperature and relative humidity of 0-95% without crystal transition, and has relatively low requirements for processing humidity or storage conditions when used for storage or preparation processing.

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 alternatives. [0003] [0004] To effectively develop Dexoxiracetam into a pharmaceutica...

Claims

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Application Information

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Patent Type & Authority Applications(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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