Arbutin-carbamide eutectic crystal as well as preparation method, preparation and application thereof

A technology of arbutin and carbonamide, which is applied in the field of arbutin-carbonamide co-crystal and its preparation, and achieves the effects of good crystallization effect, improved bioavailability and good solubility

Pending Publication Date: 2021-05-28
强悠悠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, co-crystal technology has become a new way of drug research and development. The synthesis and properties of drug co-crystals have shown attractive application prospects in the fields of pharmacology and biomedicine. However, the current reports on arbutin drug co-crystals hardly

Method used

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  • Arbutin-carbamide eutectic crystal as well as preparation method, preparation and application thereof
  • Arbutin-carbamide eutectic crystal as well as preparation method, preparation and application thereof
  • Arbutin-carbamide eutectic crystal as well as preparation method, preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0028] A preparation method of arbutin-carbamide co-crystal, comprising the steps of:

[0029] The mixed powder that arbutin and carbonamide are formed with a mol ratio of 1:1 is placed in a mixed solvent composed of water and ethanol, wherein, V (mixed solvent): m (mixed powder) is 15mL:1g, The volume ratio of the water and the ethanol in the mixed solvent is 1:1;

[0030] Then ultrasonically mix for 20min under the conditions of 20°C, ultrasonic power 250W, and ultrasonic frequency 40KHz, then continue to stir at a constant speed for 20min at a speed of 25rmp, and finally reduce the speed to 10rmp, lower the temperature to 5°C, and continue to stir at a constant speed for 10min. Finally, let stand for 24 hours, remove the solvent by rotary evaporation under reduced pressure, and dry for 1 hour under the conditions of vacuum pressure 45Pa and temperature 55°C to obtain arbutin-carbamide eutectic.

Embodiment 2

[0032] A preparation method of arbutin-carbamide co-crystal, comprising the steps of:

[0033] The mixed powder that arbutin and carbonamide are formed with a mol ratio of 1:1 is placed in a mixed solvent composed of water and ethanol, wherein, V (mixed solvent): m (mixed powder) is 15mL:1g, The volume ratio of the water and the ethanol in the mixed solvent is 1:1;

[0034] Then ultrasonically mix for 30min under the conditions of 25°C, ultrasonic power 250W, and ultrasonic frequency 40KHz, then continue to stir at a constant speed for 30min at a speed of 30rmp, and finally reduce the speed to 12rmp, lower the temperature to 8°C, and continue to stir at a constant speed for 15min. Finally, let stand for 24 hours, remove the solvent by rotary evaporation under reduced pressure, and dry for 1 hour under the conditions of vacuum pressure 45Pa and temperature 55°C to obtain arbutin-carbamide eutectic.

Embodiment 3

[0036] A preparation method of arbutin-carbamide co-crystal, comprising the steps of:

[0037] The mixed powder that arbutin and carbonamide are formed with a mol ratio of 1:1 is placed in a mixed solvent composed of water and ethanol, wherein, V (mixed solvent): m (mixed powder) is 15mL:1g, The volume ratio of the water and the ethanol in the mixed solvent is 1:1;

[0038]Then ultrasonically mix for 25min under the conditions of 30°C, ultrasonic power 250W, and ultrasonic frequency 40KHz, then continue to stir at a constant speed for 25min at a speed of 28rmp, and finally reduce the speed to 11rmp, lower the temperature to 10°C, and continue to stir at a constant speed for 12min. Finally, let stand for 24 hours, remove the solvent by rotary evaporation under reduced pressure, and dry for 1 hour under the conditions of vacuum pressure 45Pa and temperature 55°C to obtain arbutin-carbamide eutectic.

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Abstract

The invention relates to an arbutin-carbamide eutectic crystal as well as a preparation method, a preparation and application thereof. XRD (X-Ray Diffraction) characteristic diffraction peaks of the arbutin-carbamide eutectic crystal appear at 8.379 degrees + / -0.2 degrees, 14.896 degrees + / -0.2 degrees, 16.734 degrees + / -0.2 degrees, 17.361 degrees + / -0.2 degrees, 22.402 degrees + / -0.2 degrees, 25.342 degrees + / -0.2 degrees, 31.018 degrees + / -0.2 degrees, and 34.179 degrees + / -0.2 degrees. The preparation method comprises the following steps: placing mixed powder composed of arbutin and carbamide according to a molar ratio of 1: 1 into a mixed solvent composed of water and ethanol, carrying out ultrasonic mixing at 20-30 DEG C for 20-30 min, continuously stirring at a constant speed for 20-30 min at a rotating speed of 25-30 rmp, and carrying out ultrasonic stirring at a temperature of 20-30 DEG C for 20-30 min to obtain the arbutin-carbamide composite material; finally, reducing the rotating speed to 10-12rmp, reducing the temperature to 5-10 DEG C, continuously performing stirring at a constant speed for 10-15 minutes, finally standing for 24 hours, carrying out reduced-pressure rotary evaporation to remove the solvent, and performing drying to obtain the arbutin-carbamide eutectic crystal. The arbutin-carbamide eutectic crystal provided by the invention is good in stability, the solubility is improved, and the bioavailability of an arbutin medicine is favorably improved.

Description

technical field [0001] The application belongs to the technical field of pharmaceutical co-crystals, and in particular relates to an arbutin-carbamide co-crystal and a preparation method, preparation and application thereof. Background technique [0002] Arbutin, also known as arbutin, arbutin, arbutin, arbutin or myricetin, is a combination of "green", "safety" and "high efficiency" concepts in All in one skin lightening active. It can quickly penetrate into the skin, effectively inhibit the activity of tyrosinase in the skin without affecting the concentration of skin cell proliferation, block the formation of melanin, and accelerate the decomposition and excretion of melanin through the combination of itself and tyrosinase , thereby reducing skin pigmentation, removing spots and freckles. It does not produce toxic, irritating, sensitizing and other side effects on melanocytes, and it also has the effects of moisturizing, healing, bactericidal and synergistic anti-inflam...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/00C07C275/00C07C273/02C07C273/16A61K31/7034A61P31/04A61P29/00
CPCA61P29/00A61P31/04C07B2200/13C07C273/02C07C273/16C07C275/00C07H1/00C07H15/203
Inventor 强悠悠
Owner 强悠悠
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