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A kind of dihydromyricetin-berberine hydrochloride pharmaceutical co-crystal and its preparation method

A technology of berberine hydrochloride and dihydromyricetin, applied in the field of drug crystallization, to achieve the effect of simple and easy preparation method and clear crystal structure

Active Publication Date: 2021-04-27
MINJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no public report on the formation of drug-drug co-crystals between dihydromyricetin and berberine hydrochloride

Method used

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  • A kind of dihydromyricetin-berberine hydrochloride pharmaceutical co-crystal and its preparation method
  • A kind of dihydromyricetin-berberine hydrochloride pharmaceutical co-crystal and its preparation method
  • A kind of dihydromyricetin-berberine hydrochloride pharmaceutical co-crystal and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Suspend and stir 0.356 g of dihydromyricetin (dihydrate) and 0.407 g of berberine hydrochloride (dihydrate) in 20 mL of absolute ethanol for 24 hours, filter with suction, wash the resulting precipitate with absolute ethanol, and dry in the air; The obtained powder is recrystallized in absolute ethanol to obtain dihydromyricetin-berberine hydrochloride eutectic powder.

[0032] figure 1 It is the XRD figure of the dihydromyricetin-berberine hydrochloride cocrystal prepared in the present embodiment. Depend on figure 1 It can be seen that the prepared crystals are represented by diffraction angle 2θ° ± 0.1 as: 7.4°, 8.2°, 10.2°, 11.0,° 12.6°, 13.9°, 14.5°, 14.8°, 15.8°, 16.5°, 17.2°, 17.5°, 18.3°, 19.0°, 19.4°, 19.7°, 20.0°,20.4°, 20.7°, 21.2°, 22.2°, 23.2°, 24.3°, 25.2°, 26.0°, 26.4°, 27.1°, 27.4° , 27.6 °, 29.1 °, 29.7 °, 30.0 °, 30.8 °, 31.5 °, 32.6 ° have characteristic diffraction peaks.

[0033] figure 2 It is the hydrogen bonding situation between dihydrom...

Embodiment 2

[0037] Mix 0.356 g of dihydromyricetin (dihydrate) and 0.407 g of berberine hydrochloride (dihydrate) in a grinding jar, add 0.2 mL of absolute ethanol dropwise to moisten, and grind in a ball mill for 20 minutes to obtain dihydromyricetin Myricetin-berberine hydrochloride eutectic powder.

Embodiment 3

[0039] Dissolve 0.356 g of dihydromyricetin (dihydrate) and 0.407 g of berberine hydrochloride (dihydrate) in 100 mL of absolute ethanol under heating and stirring conditions, continue to stir after cooling, filter, and stand still to volatilize to obtain di Hydromyricetin-berberine hydrochloride eutectic crystal.

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Abstract

The invention discloses a drug co-crystal of dihydromyricetin-berberine hydrochloride, which belongs to the technical field of drug crystallization. The present invention combines dihydromyricetin and berberine hydrochloride through intermolecular hydrogen bonding to form the dihydromyricetin-berberine hydrochloride drug eutectic. The preparation method of the invention is simple and easy, and the cost is low. The prepared dihydromyricetin-berberine hydrochloride drug eutectic structure is clear, without hygroscopicity, and the dissolution rate of dihydromyricetin and berberine hydrochloride in water is similar, and can be dissolved simultaneously, showing a synergistically enhanced effect on specific tumor cells. inhibition.

Description

technical field [0001] The invention belongs to the technical field of medicine crystallization, and in particular relates to a dihydromyricetin-berberine hydrochloride medicine co-crystal and a preparation method thereof. Background technique [0002] Drug co-crystals can be formed by combining pharmaceutically active molecules with other physiologically safe small organic molecules through supramolecular interactions. On the premise of not destroying the molecular structure of the drug, the physicochemical properties and druggability of the active drug molecule can be improved by co-crystal formation. Drug-drug co-crystals formed by combining two known pharmaceutically active molecules are expected to exhibit therapeutic effects superior to those of a single drug. After two drug molecules with synergistic therapeutic effects are combined, the respective solubility properties may achieve an optimal balance, which is conducive to maximizing the therapeutic effect. The uniq...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/32C07D455/03A61P35/00A23L33/105
CPCA23V2002/00A23L33/105A61P35/00C07D311/32C07D455/03A23V2200/308A23V2250/21
Inventor 娄本勇李沛哲张梅张燕杰黄雅丽
Owner MINJIANG UNIV
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