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Preparation method of curcumenol derivative nanocrystal

The technology of a derivative, curcumamol, applied in the field of curcumitol derivative nanocrystals and preparation thereof, can solve the problems of low bioavailability, limited efficacy of drugs, etc., and achieves improved solubility, small difference between batches, and dissolution rate. The effect of promotion

Active Publication Date: 2019-01-08
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] With the continuous emergence of new chemical entities with strong pharmacological effects, there are more and more insoluble compounds in water. Studies have found that about 40% of the active compounds have low bioavailability due to poor water solubility, which limits their medicinal value. effective play

Method used

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  • Preparation method of curcumenol derivative nanocrystal
  • Preparation method of curcumenol derivative nanocrystal
  • Preparation method of curcumenol derivative nanocrystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] (1) Effect of stabilizer on properties of curcumol derivative CD-2e nanocrystals

[0021] 1) Weigh 0.1 g each of PVA-124, PVA05-88, and PVA17-88, and dissolve them in 20 ml of distilled water to obtain a stabilizer solution.

[0022] 2) Weigh 2 mg of curcumol derivative CD-2e into 25 ml beakers, add 10 ml of acetonitrile solution to dissolve, and obtain an organic phase.

[0023] 3) Use a high-speed shearing machine to add the organic phase to the stabilizer solution drop by drop at a shear rate of 5000r / min. After the addition, adjust the rotation speed to 10000r / min and shear for 10min to obtain a coarsely dispersed initial milk.

[0024] 4) The colostrum was subjected to high-pressure homogenization, sheared 30 times under a pressure of 70 MPa, and then rotated at 50° C. for 5 minutes to obtain curcumol derivative CD-2e nanocrystals.

[0025] Table 1

[0026]

[0027] It can be seen from Table 1 that the encapsulation efficiency is higher when PVA-124 and PVA17...

Embodiment 2

[0054] 1) Weigh 0.1 g of PVA-124 and dissolve it in 20 ml of distilled water to obtain a stabilizer solution.

[0055] 2) Weigh 2 mg of curcumol derivative CD-2e into a 25 ml beaker, add 10 ml of acetonitrile solution to dissolve, and obtain an organic phase.

[0056] 3) Using a high-speed shearing machine at a shear speed of 5000r / min, add the organic phase to the stabilizer solution drop by drop, after the addition is completed, adjust the rotation speed to 10000r / min, and cut for 10min to obtain coarsely dispersed colostrum .

[0057] 4) The colostrum was subjected to high-pressure homogenization treatment, circulated for 30 times under a pressure of 70 MPa, and then rotated at 50° C. for 5 minutes to prepare the curcumol derivative CD-2e nanocrystals.

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Abstract

The invention relates to a preparation method of a curcumenol derivative nanocrystal. The method comprises the following steps: dissolving a stabilizing agent in distilled water to form a stabilizingagent solution, dissolving a curcumenol derivative in acetonitrile to form an organic phase, dropwise adding the organic phase into the stabilizing agent solution through a high-speed shearing machineat a shearing speed of 5000r / min, after addition, regulating the rotating speed to 8000-12000r / min for shearing for 10min to form coarse dispersion primary emulsion, and performing high-pressure homogenization treatment, cyclic shearing at 70MPa for 15-35 times and rotary evaporation for 5min at 50 DEG C on the primary emulsion to form the curcumenol derivative nanocrystal. The method can increase solubility and a dissolution speed of the curcumenol derivative, and promotes transmembrane transport of the curcumenol derivative in gastrointestinal tracts, and the curcumenol derivative exerts atreatment effect better.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and in particular relates to a curcumol derivative nanocrystal and a preparation method thereof. Background technique [0002] Curcumol is an important component of traditional Chinese medicine zedoary and modern Chinese medicine zedoary oil. Its pharmacological effects include anti-tumor, anti-virus, anti-inflammatory, anti-early pregnancy, and enzyme-lowering. As a class of natural products, curcumol has the advantages of low toxicity and side effects, good compatibility with human tissue, etc., especially in the anti-tumor aspect, showing good therapeutic effect, but due to its poor water solubility and low bioavailability, it is limited. its clinical application. Improving its solubility and then its bioavailability through preparation methods has become a research hotspot. [0003] With the continuous emergence of new chemical entities with strong pharmacological effects, there are more...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/352A61K47/32A61P35/00A61P31/12A61P29/00A61P15/04A61P43/00
CPCA61K9/1075A61K31/352A61K47/32A61P15/04A61P29/00A61P31/12A61P35/00A61P43/00
Inventor 骆芙瑶马藢微陈立江
Owner LIAONING UNIVERSITY
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