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Puerarin-proline eutectic crystal and preparation method thereof

A technology of proline and puerarin, applied in the field of puerarin-proline co-crystal and its preparation, to achieve the effect of increasing the application range and improving bioavailability

Inactive Publication Date: 2021-02-23
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At this stage, foreign research on drug co-crystals has gradually increased and deepened; while domestic research on it is still relatively small

Method used

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  • Puerarin-proline eutectic crystal and preparation method thereof
  • Puerarin-proline eutectic crystal and preparation method thereof
  • Puerarin-proline eutectic crystal and preparation method thereof

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preparation example Construction

[0055] The present invention also provides a preparation method of puerarin-L-proline co-crystal I, the specific steps are as follows: adding puerarin and L-proline with a molar ratio of 1:1 to a mixed solvent of alcohol and water, Heat to 65-85°C, stir or sonicate until completely dissolved, continue to stir or sonicate for 0.5-2 hours, slowly cool to 35-50°C, stand or stir to crystallize to obtain puerarin-L-proline co-crystal 1; Alcohol is methanol, ethanol, propanol, butanol or pentanol, and alcohol is preferably ethanol; The volume mL of alcohol in the mixed solvent and the volume mL ratio of water are 10:1~8:2, solute content in the reaction solution system It is 100~310mg / mL.

[0056] The invention also discloses a puerarin-L-proline co-crystal II, which uses puerarin as a drug active ingredient and L-proline as a co-crystal former. Two puerarin molecules, one L-proline molecule, two water molecules and 0-1 ethanol molecules constitute the basic structural unit of puer...

Embodiment 1

[0070] The preparation of embodiment 1 puerarin-L-proline cocrystal I

[0071]Accurately weigh 0.832g (0.5mmol) of puerarin and 0.230g (0.5mmol) of proline into a 25mL round bottom flask, add 6mL of 80% (volume ratio) ethanol, put it into a water bath and heat to 85°C while stirring, After dissolving, continue to stir. After about 5 to 10 minutes, solids are precipitated. Continue to stir for 1 hour, then lower the temperature to 50°C while stirring, keep warm for 0.5 hours to crystallize, filter with suction, and dry at 50°C for 2 hours to obtain the product.

Embodiment 2

[0072] The preparation of embodiment 2 puerarin-L-proline cocrystal I

[0073] Accurately weigh 0.832g (0.5mmol) of puerarin and 0.230g (0.5mmol) of proline into a 25mL round-bottomed flask, add 7mL of 90% (volume ratio) ethanol, put it into a water bath and heat to 80°C while stirring, After dissolving and stirring for about 5-10 minutes, the solid precipitates out. Continue stirring for 1-2 hours. While stirring, naturally cool down to 45°C, stop stirring, stand for crystallization for about 0.5 hours, suction filter, and dry at 40°C for 4 hourly product.

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Abstract

The invention discloses a puerarin-proline eutectic crystal and a preparation method thereof, and particularly relates to two puerarin pharmaceutical eutectic crystals and a preparation method thereof, the pharmaceutical eutectic crystals take puerarin as a pharmaceutical active ingredient (API), a selected eutectic crystal forming matter is L-proline, the puerarin is connected with the proline through a hydrogen bond, and the proline is connected with the puerarin through a hydrogen bond. The molar ratio of the two co-crystals is 1: 1 and 2: 1 respectively, the solvents selected in the preparation process of the pharmaceutical co-crystal are alcohol and water, the adopted crystallization method is a cooling crystallization method, and the prepared co-crystal inherits the pharmacological activity of puerarin and is obviously improved in the aspects of solubility, dissolution rate, stability and the like.

Description

technical field [0001] The invention belongs to the field of industrial crystallization, and in particular relates to a puerarin-proline co-crystal and a preparation method thereof. Background technique [0002] Puerarin is a drug species recorded in the Chinese Pharmacopoeia, and its chemical name is 8-(β-D-glucopyranosyl-7-hydroxyl-3-(4-hydroxyphenyl)-4H-1-benzopyridine Pyran-4-one, the molecular formula is C 21 h 20 o 9 , the molecular structure is shown in the figure below: [0003] [0004] Puerarin is an isoflavone compound extracted from the traditional Chinese medicine Pueraria root, which has the functions of lowering blood sugar, lowering blood fat, protecting blood vessels, anti-oxidative stress, anti-infection and improving insulin sensitivity index, etc., and has few adverse reactions. It is used to treat diseases such as cardiovascular and cerebrovascular diseases, cancer, Parkinson's disease, Alzheimer's disease, diabetes and diabetic complications. Ho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D407/04C07D207/16A61P1/16A61P9/00A61P37/02A61P39/00A61P3/10A61P3/06A61P9/14A61P39/06A61P31/00A61P5/48
CPCA61P1/16A61P3/06A61P3/10A61P5/48A61P9/00A61P9/14A61P31/00A61P37/02A61P39/00A61P39/06C07B2200/13C07D207/16C07D407/04
Inventor 汤谷平胡秀荣伊纳姆·穆罕穆德俞卡茜
Owner ZHEJIANG UNIV
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