Method for preparing ultrafine drug particles in process of improving supercritical anti-solvent by nonsolvent method

A supercritical anti-solvent, non-solvent technology, applied in solution crystallization and other directions, can solve the problems of drugs that cannot fully exert their curative effect, difficult to absorb, and intense preparation process.

Inactive Publication Date: 2011-05-18
HUAQIAO UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] More than 40% of candidate drugs have poor water solubility, slow dissolution rate, and difficult absorption, resulting in low bioavailability, which often prevents some important candidate drugs from being marketed or prevents some drugs from fully exerting their curative effect
[0003] Traditional micronization methods include crushing, grinding, spray drying

Method used

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  • Method for preparing ultrafine drug particles in process of improving supercritical anti-solvent by nonsolvent method
  • Method for preparing ultrafine drug particles in process of improving supercritical anti-solvent by nonsolvent method
  • Method for preparing ultrafine drug particles in process of improving supercritical anti-solvent by nonsolvent method

Examples

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Embodiment 1

[0021] A full factorial experimental design was used to investigate the influence of factors such as solvent / non-solvent ratio, concentration and flow rate on the miniaturization of puerarin particles by supercritical carbon dioxide anti-solvent method. Such as figure 1 a experimental condition a).2:1, 1.0%, the implementation process of 1.0ml / min is as follows: the puerarin of 300mg is dissolved in the dehydrated alcohol of 20ml, then adds the non-solvent-dichloromethane of 10ml, obtains solvent / The non-solvent ratio is 2:1, and the concentration is 1.0% puerarin solution. After the carbon dioxide in the steel cylinder is liquefied by the refrigeration system, it is pressurized by the high-pressure plunger pump, and then pumped into the autoclave after the temperature is raised by the constant temperature water bath in the pipeline. The air release valve releases air at a certain rate, and adjusts the temperature of the external drying oven and pipeline water bath of the au...

Embodiment 2

[0026] Dissolve methotrexate in dimethyl sulfoxide, and then add non-solvent acetone to obtain dimethyl sulfoxide / acetone ratios of 1:2 and 1:4, and a concentration of 0.5% methotrexate solution, with a flow rate of 0.5 ml / min is processed with the supercritical carbon dioxide anti-solvent process parameters in Example 1. The morphology of the obtained methotrexate ultrafine particles is as follows: figure 2 As shown, the average particle diameters are 1243nm and 446nm, respectively.

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Abstract

The invention discloses a method for preparing ultrafine drug particles in process of improving supercritical anti-solvent by a nonsolvent method. The method comprises the following steps: dissolving a material in the mixed solution of an organic solvent and a non solvent to obtain an initial material solution with low concentration and high degree of saturation, wherein the organic solvent is a solvent which can be miscible with the supercritical fluid and the non solvent is another solvent which can be miscible with the organic solvent and can not dissolve the material; and then performing supercritical fluid anti-solvent treatment to obtain the ultrafine particles of the material. Experimental result shows that by adding the non solvent in the drug solution, the concentration can be reduced and the degree of saturation can be increased; then the supercritical carbon dioxide fluid anti-solvent process is performed so as to obviously reduce the particle size of the product and increase the recovery rate; and before the solution is supersaturated, the higher non solvent content is, the smaller drug particles are and the higher recovery rate is.

Description

technical field [0001] The invention relates to a novel method for preparing medicine ultrafine particles, that is, a method for preparing medicine ultrafine particles by using a non-solvent method to improve a supercritical antisolvent process. Specifically, a non-solvent is added to the drug solution in the conventional supercritical antisolvent method system to increase the saturation of the drug solution while reducing its concentration, so that the drug solution is precipitated faster when the drug solution is acted on by the supercritical fluid antisolvent And form smaller drug ultrafine particles. Background technique [0002] More than 40% of candidate drugs have poor water solubility, slow dissolution rate, and are difficult to absorb, resulting in low bioavailability, which often prevents some important candidate drugs from being marketed or prevents some drugs from fully exerting their curative effects. The ultra-micronization of drug particles is a fast and effe...

Claims

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Application Information

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IPC IPC(8): B01D9/02
Inventor 陈爱政王士斌李翼李莉
Owner HUAQIAO UNIVERSITY
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