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Dihydromyricetin-berberine hydrochloride pharmaceutical co-crystals and preparation method thereof

A technology of berberine hydrochloride and dihydromyricetin, which is applied in the directions of drug combination, food science, anti-tumor drugs, etc., achieves the effects of anti-tumor effect, clear crystal structure, and simple and easy preparation method

Active Publication Date: 2019-07-26
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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  • Dihydromyricetin-berberine hydrochloride pharmaceutical co-crystals and preparation method thereof
  • Dihydromyricetin-berberine hydrochloride pharmaceutical co-crystals and preparation method thereof
  • Dihydromyricetin-berberine hydrochloride pharmaceutical co-crystals and preparation method thereof

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 expressed 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 dihydromyricetin and berberine hydrochlor...

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 dihydromyricetin-berberine hydrochloride pharmaceutical co-crystals and belongs to the technical field of pharmaceutical crystals. The pharmaceutical co-crystals are formed bycombining dihydromyricetin with berberine hydrochloride through intermolecular hydrogen bond action. A preparation method of the co-crystals is simple, convenient and easy to implement and low in cost. The pharmaceutical co-crystals prepared by the method are clear in structure and free of hygroscopicity; dihydromyricetin and berberine hydrochloride in water are similar in dissolution rates and can be dissolved synchronously, and the pharmaceutical co-crystals show synergistic enhanced inhibition effect on specific tumor cells.

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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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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