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A kind of preparation method of curcumol derivative nanocrystal

The technology of a derivative, curcumol, is applied in the field of nanocrystals of curcumol derivatives and its preparation, which can solve the problems of low bioavailability and limited drug efficacy, and achieve improved solubility, small differences between batches, and dissolution speed Promoted effect

Active Publication Date: 2021-03-05
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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  • A kind of preparation method of curcumol derivative nanocrystal
  • A kind of preparation method of curcumol derivative nanocrystal
  • A kind of preparation method of curcumol derivative nanocrystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] (1) Effects of stabilizers on the properties of curcumol derivative CD-2e nanocrystals

[0020] 1) Weigh 0.1 g of PVA-124, PVA05-88 and PVA17-88 respectively, dissolve them in 20 ml of distilled water to obtain a stabilizer solution.

[0021] 2) Weigh 2 mg of curcumitol derivative CD-2e respectively in a 25 ml beaker, add 10 ml of acetonitrile solution to dissolve, and obtain an organic phase.

[0022] 3) Using a high-speed shearing machine, at a shearing speed of 5000r / min, add the organic phase dropwise to the stabilizer solution, adjust the rotation speed to 10000r / min after the addition, and shear for 10min to obtain a coarsely dispersed initial milk.

[0023] 4) The colostrum is subjected to high-pressure homogenization treatment, sheared 30 times under a pressure of 70 MPa, and then rotary evaporated at 50° C. for 5 min to obtain the curcumitol derivative CD-2e nanocrystals.

[0024] Table 1

[0025]

[0026] It can be seen from Table 1 that the encapsulatio...

Embodiment 2

[0052] 1) Weigh 0.1 g of PVA-124 and dissolve it in 20 ml of distilled water to obtain a stabilizer solution.

[0053] 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.

[0054] 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 cut for 10min to obtain coarsely dispersed colostrum .

[0055] 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 obtain curcumol derivative CD-2e nanocrystals.

[0056] (2) Detection

[0057] 1, adopt transmission electron microscope to observe the nanocrystalline form of the curcumol derivative CD-2e nanocrystal that embodiment 2 prepares, figure 1 It is the transmission electron microscope picture o...

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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 pharmaceutical preparation, in particular to a curcumitol derivative nanocrystal and a preparation method thereof. Background technique [0002] Curcuma alcohol is an important component of traditional Chinese medicine Curcuma curcuma and modern Chinese medicine Curcuma curcuma oil. Its pharmacological effects include anti-tumor, anti-virus, anti-inflammatory, anti-early pregnancy, and enzyme-lowering. As a kind of natural product, curcumol has the advantages of less toxic and side effects and good compatibility with human tissues, especially in anti-tumor, showing good therapeutic effect. However, due to its poor water solubility and low bioavailability, it is limited. its clinical application. It has become a research hotspot to improve its solubility and thus its bioavailability by means of preparations. [0003] With the continuous emergence of new chemical entities with strong pharmacological effects, there ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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