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Preparation method of oleum fructus bruceae nano structure lipid carrier and freeze-dried powder thereof

A technology of nanostructured lipids and javanica javanica oil, which is applied in the field of medicine, can solve the problems of high water content of SLN dispersion liquid, low drug loading of active substances, and limited carrier capacity, so as to improve long-term storage stability, improve curative effect, The effect of increasing drug loading

Active Publication Date: 2015-02-11
EAST CHINA UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Brucea javanica oil liposome intravenous injection can solve the above problems, but the liposome itself has certain limitations: firstly, its preparation technology brings certain difficulties to industrial production; in addition, the drug is easy to leak from the liposome; stable Poor sex is also a problem that urgently needs to be solved in the commercialization process of liposomes
At the same time, organic solvents will be used in the preparation of liposomes, and the residue of organic solvents may increase the toxicity
[0007] Solid lipid nanoparticles also have the following disadvantages as the first generation of lipid nanoparticles: 1) the drug loading capacity for some active substances is very low; 2) the leakage of active substances during storage, a single solid lipid matrix will form a lipid Crystal, which limits its carrier capacity, and will gradually transform into a perfect crystal, which will cause drugs, nutrients, etc. to be expelled from the crystal lattice during storage; 3) The water content in the SLN dispersion is too high

Method used

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  • Preparation method of oleum fructus bruceae nano structure lipid carrier and freeze-dried powder thereof
  • Preparation method of oleum fructus bruceae nano structure lipid carrier and freeze-dried powder thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1. Take 0.6g of glyceryl monostearate, 0.6g of stearic acid, and 0.6g of caprylic and capric triglycerides, and dissolve them in a water bath at 70°C. After the oil is cooled to room temperature, add 0.6g of javanica javanica oil to make It is miscible with fats and oils in a 70°C water bath.

[0033] 2. Take 0.0625g of poloxamer 188 and 0.0625g of polyoxyethylene castor oil to fully dissolve in 100ml of ultrapure water, and preheat in a 70°C water bath.

[0034] 3. Mix the aqueous solution in step 2 with the fat in step 1, and cut for 2 minutes with a high-speed shearing machine to make colostrum.

[0035] 4. Pour the colostrum prepared in step 3 into the material cup of the high-pressure homogenizer, and circulate 6 times under the pressure of 60 MPa. Place the finally obtained javanica oil nanostructure lipid carrier overnight.

[0036] 5. Take javanica javanica oil nanostructured lipid carrier and mannitol aqueous solution and mix uniformly at a volume ratio of 1:...

Embodiment 2

[0039] 1. Take 1.2g of glyceryl monostearate, 0.6g of stearic acid, and 0.6g of caprylic and capric triglycerides, and dissolve them in a water bath at 70°C. After the oil is cooled to room temperature, add 1.5g of javanica javanica oil to make It is miscible with fats and oils in a 70°C water bath.

[0040] 2. Take 0.25g poloxamer 188 and 0.25g polyoxyethylene castor oil to fully dissolve in 100ml ultrapure water, and preheat in a 70°C water bath.

[0041] 3. Mix the aqueous solution in step 2 with the fat in step 1, and cut for 2 minutes with a high-speed shearing machine to make colostrum.

[0042] 4. Pour the colostrum prepared in step 3 into the material cup of the high-pressure homogenizer, and circulate 5 times under the pressure of 70MPa. Place the finally obtained javanica oil nanostructure lipid carrier overnight.

[0043] 5. Take Brucea javanica oil nanostructured lipid carrier and trehalose aqueous solution and mix uniformly at a volume ratio of 1:1, freeze-dry f...

Embodiment 3

[0046] 1. Take 1.2g of glyceryl monostearate, 1.2g of stearic acid, and 0.6g of caprylic and capric triglycerides, and dissolve them in a water bath at 70°C. After the oil is cooled to room temperature, add 2.0g of javanica javanica oil to make It is miscible with fats and oils in a 70°C water bath.

[0047] 2. Take 0.125g of poloxamer 188 and 0.125g of polyoxyethylene castor oil to fully dissolve in 100ml of ultrapure water, and preheat in a 70°C water bath.

[0048] 3. Mix the aqueous solution in step 2 with the fat in step 1, and cut for 2 minutes with a high-speed shearing machine to make colostrum.

[0049] 4. Pour the colostrum prepared in step 3 into the material cup of the high-pressure homogenizer, and circulate 5 times under the pressure of 70MPa. Place the finally obtained javanica oil nanostructure lipid carrier overnight.

[0050] 5. Take Brucea javanica oil nano-structured lipid carrier and glucose aqueous solution, mix uniformly at a volume ratio of 1:1, and f...

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Abstract

The invention discloses a preparation method of an oleum fructus bruceae nano structure lipid carrier and freeze-dried powder thereof. The method comprises the following steps: (1) respectively dissolving an oil phase and oleum fructus bruceae at 70 DEG C, wherein the oil phase is solid grease or a mixture of solid grease and liquid grease; and the mass ratio of the oil phase to the oleum fructus bruceae is (1: 1) to (2: 1); (2) dissolving an emulsifier into ultra-pure water, and preheating at 70 DEG C, wherein the mass ratio of the emulsifier to the ultra-pure water is (1: 200) to (1: 800); the mass ratio of the emulsifier to the oleum fructus bruceae is (1: 1.5) to (1: 12); (3) mixing a water solution obtained in the step (2) with the grease obtained in the step (1), and preparing colostrum by adopting a high-speed shearing machine in a shearing manner; and (4) pouring the colostrum obtained in the step (3) into a high-pressure homogenizer, and circulating for 5-7 times under the pressure of 50-70MPa to obtain the oleum fructus bruceae nano structure lipid carrier. The drug-loading capacity is improved by oleum fructus bruceae nano lipid disclosed by the invention; the oleum fructus bruceae nano structure lipid carrier has relatively good stability; the curative effect of the oleum fructus bruceae is improved; and the toxic and side effects are reduced.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically relates to a preparation method of javanica javanica oil nanostructure lipid carrier and freeze-dried powder thereof with anticancer effect. Background technique [0002] Brucea javanica, another name called old javanica, is bitter and poisonous. It is the dry and mature fruit of Brucea javanica of the bitter wood family plant, produced in Guangdong, Hainan, Guangxi, and Fujian of China. Brucea javanica has been widely used in the treatment of cancer and tumors since the early 1980s, after researchers at Shenyang Pharmaceutical University discovered that Brucea javanica had significant biological activity, especially for various stages of cancer such as esophageal cancer, gastric cancer, intestinal Cancer and liver cancer curative effect is excellent. Its main active ingredients are oleic acid and linoleic acid, which can strongly inhibit the oxygen uptake of cancer cells, reduce t...

Claims

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Application Information

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IPC IPC(8): A61K36/185A61K9/127A61K9/19A61P35/00
Inventor 邹爱华赵双妮龚亚斌陈奕茵许玲
Owner EAST CHINA UNIV OF SCI & TECH
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