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A carvanol solubilize solid composition and its preparation method and application

A carvacrol, solidification technology, applied in the field of pharmacy, can solve the problems of not significantly improving the solubility of carvacrol, easy volatilization, poor stability, etc., and achieve the effect of increasing drug loading, solubility, and high inclusion rate

Active Publication Date: 2019-01-15
陕西医药控股医药研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because carvacrol is insoluble in water, and is volatile in the air, easy to oxidize, and has poor stability, etc., it greatly affects its bioavailability and scope of application.
It is reported in the prior art that carvacrol and β-cyclodextrin are prepared into clathrates to improve its stability, but the clathrate rate of this clathrate is not high (61.89%), and it does not significantly improve the quality of carvacrol and β-cyclodextrin. Solubility of phenol

Method used

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  • A carvanol solubilize solid composition and its preparation method and application
  • A carvanol solubilize solid composition and its preparation method and application
  • A carvanol solubilize solid composition and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Example 1 Preparation of β-cyclodextrin polymer

[0032] Dissolve β-cyclodextrin (5.0g) in sodium hydroxide solution (10.0g) with a mass fraction of 20%, add epichlorohydrin (5.0g) at room temperature, and react for 4 hours, then add an appropriate amount of acetone to terminate the reaction , and adjust the pH to 7.0 with 1mol / L hydrochloric acid, put it into a dialysis bag with a molecular weight cut-off of 8000-12000, and after 2 days of dialysis, freeze-dry to obtain a white powder (4.86g), which is the β-cyclodextrin polymer (from infrared spectroscopy). , successful grafting).

Embodiment 2

[0033] Preparation of embodiment 2 chitosan grafted β-cyclodextrin

[0034] Dissolve chitosan (2.0g) in hydrochloric acid solution (100g) with a mass fraction of 1%, add epichlorohydrin (4.0g) under stirring, heat up to 85°C, react for 5 hours, cool to room temperature, filter , Dissolve the filter cake in water (100mL), add potassium carbonate (4.0g) and β-cyclodextrin (2.0g), heat to reflux temperature and react for 3 hours, cool to room temperature, add an appropriate amount of acetone to terminate the reaction, and use Adjust the pH to 7.0 with 1mol / L hydrochloric acid, put it into a dialysis bag with a molecular weight cut-off of 8000-12000, and after 2 days of dialysis, freeze-dry to obtain chitosan-grafted β-cyclodextrin (3.76g). branch success.

Embodiment 3

[0036] (1) Dissolve the β-cyclodextrin polymer (5.0 g) prepared in Example 1 in water (15.0 g) at 50° C. to obtain a clear solution A;

[0037] (2) Mix 0.5 mL of carvacrol with 0.5 mL of absolute ethanol to form solution B;

[0038] (3) Add solution B dropwise to solution A, keep stirring at 50°C for 6 hours, cool to room temperature, place in a refrigerator at 4°C for 10 hours, filter, and precipitate in turn with water (4°C cold water), absolute ethanol (4 ℃ cold absolute ethanol) after washing, vacuum drying to obtain the carvacrol solubilized solid composition (5.10g, measured the absorbance at 295nm by ultraviolet spectrophotometer, draw inclusion rate 89.4%, carvacrol Content 8.55%, hereinafter referred to as product A).

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Abstract

The invention relates to a carvanol solubilizing solid composition and a preparation method and application thereof, wherein the preparation method of the carvanol solubilizing solid composition comprises the following steps: (1) modifying beta; Cyclodextrin is dissolved in water at 50 DEG C to obtain a clarified solution A; 2. Prepare solution B from carvanol and absolute ethanol according to that volume ratio of 1: 1; 3) drop solution B into solution A, stirring at 50 DEG C for 6 hour, cooling to room temperature, placing in refrigerator at 4 DEG C for 10 hours, filter, precipitating with water in turn, washing with absolute ethanol, and vacuum drying to obtain that carvanol solubilizing solid composition.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a carvacrol solubilized and solidified composition, a preparation method and application thereof. Background technique [0002] Carvacrol (Carvacrol), also known as carvacrol and isothymol, is a colorless to pale yellow liquid with a thymol smell, often present in the volatile oil of oregano, thyme volatile oil, and the whole plant of chrysanthemum And camphor. It has been reported that carvacrol has the functions of anti-oxidation, antibacterial, deworming, and reducing ischemia-reperfusion injury of rat brain and spinal cord. However, carvacrol is insoluble in water, volatile and easily oxidized in the air, and has poor stability, which greatly affects its bioavailability and scope of application. It is reported in the prior art that carvacrol and β-cyclodextrin are prepared into clathrates to improve its stability, but the clathrate rate of this clathrate is not high (61....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/40A61K31/05A61P9/10
CPCA61K31/05A61K47/6951A61P9/10
Inventor 王四旺何俊婷曹爱兰肖志强许璐张芳侠
Owner 陕西医药控股医药研究院有限公司
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