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Huperzine A polymorph, its preparation method, medicinal composition containing huperzine A polymorph and its application

A technology of huperzine A and its crystal form, which is applied in the field of preparation of huperzine A polymorph and its synthesis process, and can solve problems not involving the crystal form of huperzine A raw material

Active Publication Date: 2012-08-08
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Currently on the market, huperzine A is mainly administered in the form of oral tablets, capsules, and injections, but none of the formula patents involves the crystal form of the huperzine A raw material used

Method used

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  • Huperzine A polymorph, its preparation method, medicinal composition containing huperzine A polymorph and its application
  • Huperzine A polymorph, its preparation method, medicinal composition containing huperzine A polymorph and its application
  • Huperzine A polymorph, its preparation method, medicinal composition containing huperzine A polymorph and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1: Preparation of huperzine A crystal form I.

[0056] Mix 50 mg of huperzine A raw material (amorphous) with 1 ml of acetone, heat to 50° C. and keep stirring at 50° C. for 3 days, and filter to obtain a white solid. After evaporating the solvent at room temperature, the white solid was dried under reduced pressure with an oil pump for 12 hours to obtain a crystalline powder, which was determined by X-ray powder diffraction, showing that the obtained crystal form was Form I. The specific peak positions are shown in Table 1 below.

[0057] Table 1: X-ray powder diffraction data of Huperzine A crystal form I in Example 1 of the present invention

[0058]

[0059]

[0060] Other tests were carried out on the obtained sample, and the obtained DSC thermal spectrum, infrared spectrum and Raman spectrum were as follows: Figure 1b , 1c , 1d shown.

Embodiment 2

[0061] Example 2: Preparation of huperzine A crystal form II.

[0062] Put 25 mg of huperzine A crystal form I in an oven at 125 degrees Celsius and heat for 2 hours to obtain a crystalline powder, which was determined by X-ray powder diffraction to show that the obtained crystal form was crystal form II. The specific peak positions are shown in Table 2 below.

[0063] Table 2: X-ray powder diffraction data of Huperzine A crystal form II in Example 2 of the present invention

[0064]

[0065]

[0066] Other tests were carried out on the obtained sample, and the obtained DSC thermal spectrum, infrared spectrum and Raman spectrum were as follows: Figure 2b , 2c , as shown in 2d.

Embodiment 3

[0067] Example 3: Preparation of huperzine A crystal form III.

[0068] Mix 50 mg of huperzine A crystalline form I with 1 ml of acetonitrile, heat to 50° C. and keep stirring at 50° C. for 2 days, and filter to obtain a white solid. After evaporating the solvent at room temperature, the white solid was placed in a vacuum drying oven at 100°C, and dried for 24 hours under vacuum with an oil pump to obtain a crystalline powder, which was determined by X-ray powder diffraction, showing that the obtained crystal form was crystal Type III. The specific peak positions are shown in Table 3 below.

[0069] Table 3: X-ray powder diffraction data of Huperzine A crystal form III in Example 3 of the present invention

[0070]

[0071] Other tests were carried out on the obtained sample, and the obtained DSC thermal spectrum, infrared spectrum and Raman spectrum were as follows: Figure 3b , 3c , 3d shown.

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Abstract

The invention discloses a huperzine A polymorph, its preparation method, a medicinal composition containing huperzine A polymorph and its application. Part of the huperzine A polymorph has better dissolvability than currently saled medicinal crystal forms, thus being more conducive to medicine absorption. Also, part of the huperzine A polymorph has substantially lower hygroscopicity than saled medicinal crystal forms, thus being more conducive to preparation and storage of medicinal preparations.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry polymorph research, and specifically relates to the preparation of huperzine A polymorph by different crystallization methods and the research on its synthesis process. Background technique [0002] Polymorphism refers to the phenomenon that solid substances form solid states with different physical and chemical properties in two or more different spatial arrangements. In the field of pharmaceutical research, polymorphism also includes multi-component crystal forms such as organic solvates and hydrates. Drug polymorphism widely exists in the drug development process and is an inherent characteristic of small organic molecules. Theoretically, small-molecule drugs can have an infinite number of crystal packing methods - polymorphic forms. Studies have shown that the number of drug polymorphic forms discovered is proportional to the time and resources invested in research. Polymorphism is not onl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/22A61K31/4748A61P25/28A61P25/18
CPCC07D221/22A61K31/4748A61P25/18A61P25/28
Inventor 梅雪锋章海燕张奇陆骊烨戴文娟
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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