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Myricetin pharmaceutical eutectic crystal and preparation method thereof

A technology for myricetin and medicine, which is applied to the field of myricetin drug co-crystal and its preparation, can solve the problems of poor fat solubility, low bioavailability, limited application of myricetin, etc., and achieves wide application, improved dissolution rate and stability. Effect

Active Publication Date: 2014-05-28
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, myricetin, like other flavonoids, has poor water and fat solubility, and is unstable under weak acid, neutral and alkaline conditions, resulting in poor membrane permeability, short half-life, low bioavailability, etc., which greatly limits The application of myricetin in the treatment of diseases

Method used

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  • Myricetin pharmaceutical eutectic crystal and preparation method thereof
  • Myricetin pharmaceutical eutectic crystal and preparation method thereof
  • Myricetin pharmaceutical eutectic crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Accurately weigh 408.12mg of myricetin and 68.43mg of caffeine into 20mL transparent glass bottles, add 8mL of methanol, seal the glass bottles in a constant temperature water bath shaker, shake and react at 25°C for 12h; stop the reaction, filter, and take The filter cake is dried under a vacuum environment, and the product obtained is myricetin-caffeine eutectic.

Embodiment 2

[0057] Accurately weigh 525.13mg of myricetin and 129.13mg of caffeine into 20mL transparent glass bottles, add 10mL of methanol, seal the glass bottles in a constant temperature water bath shaker, shake and react at 25°C for 12h; stop the reaction, filter, and take The filter cake is dried under a vacuum environment, and the product obtained is myricetin-caffeine eutectic.

Embodiment 3

[0059] Accurately weigh 633.57mg myricetin and 228.76mg caffeine into a 20mL transparent glass bottle, add 10mL methanol, seal the glass bottle and place it in a constant temperature water bath shaker, shake and react at 25°C for 12h; stop the reaction, filter, and take The filter cake is dried under a vacuum environment, and the product obtained is myricetin-caffeine eutectic.

[0060] The differential thermal (DSC) spectrogram of the myricetin-caffeine eutectic that embodiment 1~3 gains is as follows figure 1 Shown: The melting point of the eutectic is different from that of the API and the precursor, and there is an endothermic peak at 275°C, which proves that a new phase is formed.

[0061] The X-ray powder diffraction (PXRD) spectrogram of the myricetin-caffeine cocrystal that embodiment 1~3 gains is as follows figure 2 Shown: 25.3°, 10.7°, 12.3°, 13.4°, 14.3°, 16.1°, 17.9°, 18.3°, 21.9°, 22.3°, 24.8°, 25.7°, 27.1°, 28.1°, 29.6° at 2θ A series of characteristic peaks a...

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Abstract

The invention discloses a myricetin pharmaceutical eutectic crystal and a preparation method thereof. The myricetin pharmaceutical eutectic crystal uses myricetin as the active pharmaceutical ingredients, uses theine, nicotinamide, pyrazinamide or 4-cyanopyridine as the precursors, and is a myricetin-theine eutectic crystal, a myricetin-nicotinamide eutectic crystal, a myricetin-pyrazinamide eutectic crystal or a myricetin-4-cyanopyridine eutectic crystal formed through intermolecular hydrogen bonds. The eutectic crystals are prepared by adopting the solution mediating crystal transformation method. The myricetin pharmaceutical eutectic crystal provided by the invention inherits the pharmacological activity of the myricetin; meanwhile, the solubleness, the dissolution rate and the stability of the myricetin pharmaceutical eutectic crystal are all significantly improved as compared with those of the myricetin; the myricetin pharmaceutical eutectic crystal facilitates the development of pharmaceutic preparation and the wide applications of the myricetin in the field of medicine.

Description

technical field [0001] The invention relates to myricetin drug co-crystal and a preparation method thereof, belonging to the technical field of drug co-crystal. Background technique [0002] At room temperature, active pharmaceutical ingredients exist in various solid forms, such as polymorphs, solvates, hydrates, co-crystals, amorphous forms, and salts. The curative effect of a drug largely depends on the physical and chemical properties of the drug itself and the selected dosage form, and the different solid forms of the drug have an impact on the solubility, stability, dissolution rate and bioavailability of the drug. [0003] Supramolecular chemistry is a science that studies molecular aggregates that are complex and orderly and have specific structures and functions formed by intermolecular interactions. Its core content is molecular recognition and supramolecular self-assembly through weak intermolecular interactions. "Chemistry beyond the scope of molecules", such mo...

Claims

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Application Information

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IPC IPC(8): C07D311/30C07D473/12C07D213/82C07D213/81C07D213/84
CPCC07D213/81C07D213/82C07D213/84C07D311/30C07D473/12
Inventor 谢燕洪超李国文姚雅淑孟厚君邓冰付情雪王慧珍沈红艺
Owner SHANGHAI UNIV OF T C M
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