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Huperzine A polymorphic substance and preparation method thereof, and medicinal composition

A technology for huperzine A and crystal forms, applied in the field of medicinal chemistry polymorph research, can solve the problems of cumbersome crystal form operations, unsuitable for industrial scale-up production, time-consuming and energy-consuming problems

Active Publication Date: 2018-05-08
ZHEJIANG WANBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] The method taught in the patent CN201210078474.9 is cumbersome in the preparation process of the crystal form, and consumes time and energy, and is not suitable for industrial scale-up production

Method used

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  • Huperzine A polymorphic substance and preparation method thereof, and medicinal composition
  • Huperzine A polymorphic substance and preparation method thereof, and medicinal composition
  • Huperzine A polymorphic substance and preparation method thereof, and medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Add 1.0 g of Huperzine A amorphous powder into 1.4 mL of ethanol containing water (ethanol: water = 95V: 5V), heat to reflux until completely dissolved, continue to stir for 10 minutes, slowly cool to room temperature, continue to stir for 1 hour, filter , the filter cake was rinsed once with ice-containing ethanol, and the solid was vacuum-dried at 45° C. for 3 hours to obtain 0.7 g of a crystalline powder, which was determined by X-ray powder diffraction to be polymorph A. The specific peak positions are shown in Table 6 below:

[0100] The XRPD data of table 6 huperzine A polymorphic form A

[0101]

[0102]

Embodiment 2

[0104]Add 1.0 g of huperzine A amorphous powder into 1.4 mL of water-containing propanol (propanol: water = 95V: 5V), heat to reflux until completely dissolved, continue stirring for 10 minutes, slowly cool to room temperature, and continue stirring for 1 hour , filtered, and the filter cake was rinsed with ice-water isopropanol once, and the solid was vacuum-dried at 45°C for 3 hours to obtain 0.72 g of crystalline powder, which was determined by X-ray powder diffraction to be polymorphic a.

Embodiment 3

[0106] Add 1.0g of huperzine A amorphous powder into 1.4mL of water-containing isopropanol (isopropanol: water = 95V: 5V), heat and reflux until completely dissolved, continue stirring for 10 minutes, slowly cool to room temperature, and continue stirring Filter for 1 hour, rinse the filter cake with icy isopropanol once, and dry the solid under vacuum at 45°C for 3 hours to obtain 0.75 g of crystalline powder, which was determined by X-ray powder diffraction to be polycrystalline Model A.

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Abstract

The invention discloses a huperzine crystal form A. An X-ray diffraction diagram is obtained through Cu-Ka radiation, the angle 2theta expressed by degrees has absorption peaks in the positions of 9.711, 9.969, 10.757, 12.591, 13.501, 13.838, 14.366, 16.225, 17.902, 19.443, 19.994, 21.298, 22.422, 22.758, 23.842, 24.057, 24.614, 25.916, 26.347, 27.239, 28.819, 29.431 and 30.202. In addition, the invention also discloses a preparation method of the huperzine crystal form A, and a medicine preparation. The huperzine A polymorphic substance provided by the invention has the advantages of excellent physical and chemical properties, high stability, and suitability for industrialized scale preparation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical chemistry polymorph research, and specifically relates to a polymorph of huperzine A. In addition, the invention also relates to a preparation method of the crystal and a pharmaceutical preparation thereof. technical background [0002] Huperzine A is a highly active alkaloid isolated from Huperzia serrata (Thunb) Thev.]. Usually use its optical isomer huperzine A as the active ingredient of the drug, and the structural formula of huperzine A is as follows: [0003] [0004] Huperzine A, its chemical name is: (5R,9R,11E)-5-amino-11-ethylene-5,6,9,10-tetrahydro-7-methyl-5,9-methylene Cyclooctacetraeno[b]pyridin-2-(1H)-one. [0005] Huperzine A is a highly efficient and highly selective reversible acetylcholinesterase inhibitor, which has the function of improving learning and memory, and can be used for the treatment of various neuropsychiatric diseases. [0006] Huperzine A Tablets was launched...

Claims

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Application Information

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IPC IPC(8): C07D221/22A61K31/4748A61P25/28
CPCC07B2200/13C07D221/22
Inventor 赵守明陈安陈忠彭少平庄银枪
Owner ZHEJIANG WANBANG PHARMA
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