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Curcumin vitamin E succinate prodrug, nanometer emulsion, preparation method and purpose thereof

A technology of succinate and curcumin, applied in the field of medicine, can solve the problems of poor preparation stability, uncontrollable drug release, easy metabolism, etc., and achieve the effects of improving compatibility, inhibiting tumor cell growth, and facilitating sample enrichment.

Inactive Publication Date: 2019-02-12
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although the dosage form research of curcumin has achieved certain results, there are still many problems, such as poor stability of the preparation, uncontrollable drug release, easy metabolism in the body, etc.

Method used

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  • Curcumin vitamin E succinate prodrug, nanometer emulsion, preparation method and purpose thereof
  • Curcumin vitamin E succinate prodrug, nanometer emulsion, preparation method and purpose thereof
  • Curcumin vitamin E succinate prodrug, nanometer emulsion, preparation method and purpose thereof

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Experimental program
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Effect test

Embodiment 1

[0035] The preparation of embodiment 1 curcumin vitamin E succinate (CUR-VE)

[0036] Accurately weigh 0.046g of vitamin E succinate and 0.047g of dicyclohexylcarbodiimide, add 5mL of dichloromethane to dissolve, stir in a bath at 15-25°C for 20-40min, and protect with nitrogen. Then, add curcumin pure product 0.0312g (self-made in the inventor's laboratory, purity>98%), 1mL of 4-dimethylaminopyridine solution (accurately weighed 0.0544g, dichloromethane is settled to 1mL), 20~30 ℃ reaction 7h, nitrogen protection.

Embodiment 2

[0037] The separation and purification of embodiment 2 curcumin vitamin E succinate

[0038] Column packing: take an appropriate amount of 100-200 mesh column chromatography silica gel, use petroleum ether: ethyl acetate = 4:1 as the solvent by volume ratio, wet-pack the column, and stand overnight for later use; pump the reaction solution after 7 hours of reaction Filter, mix the filtrate with 1g of column chromatography silica gel, evaporate the solvent to dry, and the sample mixing is completed;

[0039] Sample mixing: Accurately weigh an appropriate amount of curcumin vitamin E succinate silica gel powder, dissolve it in an evaporating dish with an appropriate amount of dichloromethane, add 2 times the amount of column chromatography silica gel, place in a 60-70°C water bath, and stir while stirring. After the solvent is evaporated to dryness, the sample mixing is completed;

[0040]Separation: Add the mixed sample to the silica gel column that has been left standing over...

Embodiment 3

[0041] The structure confirmation and purity determination of embodiment 3 curcumin vitamin E succinate

[0042] 1. Determination of the purity of curcumin vitamin E succinate

[0043] (1) Determination of the maximum absorption wavelength

[0044] Accurately weigh the pure curcumin vitamin E succinate, add an appropriate amount of methanol to dissolve, and prepare a sample stock solution with a concentration of 41.4mg / mL. Take a certain amount of stock solution, prepare a sample with a concentration of 20μg / mL, and scan in the wavelength range of 200-700nm according to spectrophotometry. Curcumin vitamin E succinate has a maximum absorption wavelength at 414nm.

[0045] (2) Chromatographic conditions

[0046] ColumnRedClassical C 18 Column, mobile phase: methanol:water (containing 0.1% phosphoric acid)=99:1, flow velocity is 1mL / min, injection volume is 20 μ L, detection wavelength is 414nm, column temperature 30 ℃.

[0047] (3) Purity determination

[0048] Accurately w...

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Abstract

The invention relates to curcumin vitamin E succinate prodrug, nanometer emulsion, a preparation method and a purpose thereof, and belongs to the technical field of medicine. Curcumin and vitamin E are connected through ester bonds to obtain the curcumin vitamin E succinate prodrug through preparation; the tumor cells are favorable for mother drug curcumin release through ester bond fracture to achieve the anti-tumor effect in acidic environment; in proliferation inhibition experiments of HepG2 liver cancer cells and Caco-2 colon cancer cells, the result shows that the prepared curcumin vitamin E succinate prodrug and nanometer emulsion have the identical tumor cell growth inhibition effect to the curcumin. Compared with curcumin nanometer emulsion, the curcumin vitamin E succinate prodrug, nanometer emulsion prepared by the method have the advantages of high stability, slow in vitro release speed, high encapsulation rate and the like.

Description

technical field [0001] The invention relates to a curcumin vitamin E succinate prodrug, a nanoemulsion, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] Curcumin has poor solubility, is almost insoluble in water, and has low solubility in organic solvents such as methanol and chloroform. The free drug is easily hydrolyzed, and the bioavailability is low. The high clearance rate in the organism becomes the main factor and development cost that limits its clinical application. The bottleneck of formulations for clinical application. At present, the bioavailability of curcumin is mainly improved by solid dispersion technology solubilization, carrier solubilization, clathrate technology and supercritical method. To improve the solubility of curcumin through structural modification, it can be divided into modification of benzene ring, modification of methylene group and modification of unsaturated carbony...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/12A61K47/34A61K47/54A61P35/00A61K31/353C07D311/72
CPCA61K9/1075A61K31/12A61K31/353A61K47/34A61K47/545A61P35/00C07D311/72
Inventor 马燕曹淑情李颖严霞黄梓鹏肖佩陈欣如
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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