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

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...

AI Technical Summary

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 and other methods. The disadvantages are that the preparation process is more intense, it is easy to cause thermal denaturation, and it has higher requirements on the stability of drugs. It is not suitable for peptides and protein macromolecules. Drugs or other heat-sensitive substances, and the product particle size distribution is wide, easy to introduce pollutants

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