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Crystallization form of dihydromyricetin, preparation method thereof and pharmaceutical composition containing the same

A technology of dihydromyricetin and crystal form, applied in the field of medicine, can solve the problems of poor solubility, unfavorable preparation of pharmaceutical raw materials, storage, influence on quality stability, etc., and achieves the effects of simple preparation method, stable crystal form and good solubility

Inactive Publication Date: 2015-09-02
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventors found in the research that the amorphous powder of DMY has poor solubility compared with the crystalline state sample, and also has hygroscopicity, which affects the quality stability and is not conducive to the preparation of preparations and storage as medicinal raw materials.

Method used

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  • Crystallization form of dihydromyricetin, preparation method thereof and pharmaceutical composition containing the same
  • Crystallization form of dihydromyricetin, preparation method thereof and pharmaceutical composition containing the same
  • Crystallization form of dihydromyricetin, preparation method thereof and pharmaceutical composition containing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Take 1g of crude dihydromyricetin, add 2ml of acetone to dissolve, then add 2ml of glacial acetic acid to the solution, shake well, and place it at room temperature for crystallization. The obtained crystals were filtered, and after standing at room temperature for 24 hours, they were placed in an oven and dried at 100°C for 24 hours to obtain Form I.

Embodiment 2

[0027] Take 1g of crude dihydromyricetin, add 3ml of acetone to dissolve, then add 6ml of glacial acetic acid to the solution, shake well, and place it at room temperature for crystallization. The obtained crystals were filtered, placed at room temperature for 24 hours, then placed in an oven, and dried at 105°C for 24 hours to obtain Form I. With Cu-Ka radiation, the X-ray powder diffraction pattern of the crystalline form I of dihydromyricetin represented by the 2θ angle and the interplanar spacing is shown in the appendix figure 1 , see Table 1 for the description of the spectrum.

[0028] Table 1

[0029]

Embodiment 3

[0031] Take 1g of crude dihydromyricetin, add 2ml of acetone to dissolve, then add 8ml of glacial acetic acid to the solution, shake well, and place it at room temperature for crystallization. The obtained crystals were filtered, left at room temperature for 12 hours, placed in an oven, dried at 80°C for 24 hours, and then dried at 120°C for 12 hours to obtain Form I.

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Abstract

The invention belongs to the field of medical technology, and relates to the crystallization form of dihydromyricetin, and a preparation method thereof and a pharmaceutical composition containing the same. The invention discloses the crystallization form I, II, III, IV and an X-ray powder diffraction pattern of the dihydromyricetin, simultaneously provides the preparation method of the crystallization form and the pharmaceutical composition containing the crystallization form. The crystallization form I provided by the invention has the advantages of stable crystal form, good dissolvability, simple preparation method, and yield in steps, and medicinal preparation and storage of dihydromyricetin as medicinal raw material.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a crystal form of dihydromyricetin, a preparation method and a pharmaceutical composition thereof. Background technique [0002] Dihydromyricetin (dihydromyricetin, abbreviated as DMY) chemical name is 3,5,7,3',4',5'-hexahydroxy-2,3-dihydroflavonol, widely distributed in grape family, bayberry in nature Among the various plants such as Rhododendronaceae, Garciniaceae, Euphorbiaceae, Salixaceae, etc., the content of Vitaceae Vitaceae is particularly high. DMY has various pharmacological effects such as antibacterial and anti-inflammatory, lowering blood fat, protecting liver, lowering blood sugar, lowering blood pressure, anti-tumor, etc., and has high development and application value. [0003] The extraction and purification technology of DMY is relatively mature, but there is no literature report on the study of its crystal form. The inventors found in the research that the am...

Claims

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Application Information

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IPC IPC(8): C07D311/32C07D311/40A61K31/352A61P31/00A61P29/00A61P3/06A61P1/16A61P9/12A61P3/10A61P35/00
CPCC07D311/32C07B2200/13C07D311/40
Inventor 韩英梅赵娜夏
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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