Silymarin compound nanoparticle and preparation method thereof

A technology of silymarin and compound, which is applied in the direction of drug combination, pharmaceutical formula, plant raw material, etc., can solve the problems of easy agglomeration between particles, difficult control of particle size, etc., and achieves high dissolution rate and controllable ultra-fine operation. , the effect of good stability

Active Publication Date: 2012-08-01
晨光生物科技集团天津有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The second object of the present invention is to provide a method for preparing silymarin complex nanoparticles with small standard deviation of particle size and good dispersion. Disadvantages of easy agglomeration between particles

Method used

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  • Silymarin compound nanoparticle and preparation method thereof
  • Silymarin compound nanoparticle and preparation method thereof
  • Silymarin compound nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A method for preparing silymarin complex nanoparticles, comprising the following steps:

[0036] (1) Take 1Kg of silymarin, 0.5Kg of hypromellose phthalate and 1Kg of water and mix them uniformly, and mix them for 40 minutes with a twin-screw extruder at a screw speed of 400 rpm to obtain a silymarin solid dispersion;

[0037] (2) The silymarin solid dispersion is mixed with 3Kg of soybean lecithin, 2Kg of Benzaze 35 and 300Kg of ethanol to obtain an ethanol suspension;

[0038] (3) passing the ethanol suspension through supercritical CO 2 Fluid equipment, at a temperature of 40°C, a pressure of 20MPa, CO 2 The flow rate is 10L / min, the solution flow rate is 1.2ml / min, and the nozzle diameter is 0.1mm, and the supercritical fluid anti-solvent technology is used to obtain silymarin composite nanoparticles, and the obtained composite nanoparticles have a particle size of 86nm-106nm. In view figure 1 -Figure 4.

Embodiment 2

[0040] A method for preparing silymarin complex nanoparticles, comprising the following steps:

[0041] (1) Take 1Kg of silymarin, 0.2Kg of hypromellose phthalate and 2Kg of water and mix them evenly, and mix them for 60 minutes with a twin-screw extruder at a screw speed of 300 rpm to obtain a silymarin solid dispersion;

[0042] (2) The silymarin solid dispersion is mixed with 1Kg of soybean lecithin, 3Kg of Benzaze 35 and 300Kg of ethanol to obtain an ethanol suspension;

[0043] (3) passing the ethanol suspension through supercritical CO 2 Fluid equipment, at a temperature of 35°C, a pressure of 15MPa, CO 2 The flow rate is 5L / min, the solution flow rate is 0.5ml / min, and the nozzle diameter is 0.08mm, and the supercritical fluid anti-solvent technology is used to obtain silymarin composite nanoparticles, and the obtained composite nanoparticles have a particle size of 89nm-110nm.

Embodiment 3

[0045] A method for preparing silymarin complex nanoparticles, comprising the following steps:

[0046] (1) Get 1Kg of silymarin, 0.4Kg of hypromellose phthalate and 0.5Kg of water and mix them evenly, and mix them for 20min with a twin-screw extruder at a screw speed of 500rpm to obtain a silymarin solid dispersion ;

[0047] (2) Mix the silymarin solid dispersion with 3Kg of egg yolk lecithin, 1Kg of Benzaze 35 and 500Kg of ethanol to obtain an ethanol suspension;

[0048] (3) passing the ethanol suspension through supercritical CO 2 Fluid equipment, at a temperature of 40°C, a pressure of 20MPa, CO 2The flow rate is 10L / min, the solution flow rate is 1.2ml / min, and the nozzle diameter is 0.1mm, and the supercritical fluid anti-solvent technology is used to obtain silymarin composite nanoparticles, and the obtained composite nanoparticles have a particle size of 93nm-115nm.

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Abstract

The invention discloses a silymarin compound nanoparticle and a preparation method thereof. The silymarin compound nanoparticle is prepared through the following steps of: (1) uniformly mixing silymarin, hypromellose phthalate and water by using a dual-screw extruder to obtain a silymarin solid dispersant; (2) mixing the silymarin solid dispersant with phospholipid, brij 35 and ethanol to obtain an ethanol suspension; and (3) making the ethanol suspension flow through supercritical CO2 fluid equipment, and preparing the silymarin compound nanoparticle by applying a supercritical fluid anti-solvent technology. A nanoparticle system has very high stability and high medicament dissolution rate. The method provided by the invention is simple, refining operation is controlled. The nanoparticle prepared by using the method disclosed by the invention has a small particle diameter standard difference, the dispersant is in a good state, and the defects of easiness in agglomerating, poor refining operation safety and the like existing in the prior art are overcome.

Description

technical field [0001] The invention relates to a natural medicine extract nanoparticle and a preparation method thereof, in particular to a silymarin complex nanoparticle and a preparation method thereof. Background technique [0002] Silymarin is a flavonoid compound isolated from the fruit of the genus Silymarin in the family Asteraceae. It is a yellow powder or crystalline powder with a bitter taste. The main components are silybin and isosilibinin. , silymarin and silymarin and other flavonoids. Silymarin has the inhibitory effect on lipoxygenase and peroxidase, can protect the enzyme system of liver cells, thereby improving the detoxification ability of the liver (damaged by taking liver toxic drugs, drinking, etc.), and is clinically used for liver poisoning, Liver dysfunction. [0003] However, due to the poor water solubility and fat solubility of silymarin, its oral absorption is poor and its bioavailability is low, which greatly limits the clinical application o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/28A61K9/14A61K47/24A61P1/16
Inventor 张卫军李娜
Owner 晨光生物科技集团天津有限公司
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