Preparation method of sustained-release particles

Preparation method of sustained-release particles

  • CN 105,963,258 B
  • Filed: 04/26/2016
  • Issued: 01/22/2021
  • Est. Priority Date: 04/26/2016
  • Status: Active Grant
First Claim
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1. A method for preparing sustained-release microparticles, which is characterized in that:

  • the method comprises the following steps;

    1) preparing a solid dispersion of a water-soluble drug and a biodegradable and biocompatible poorly water-soluble polymer;

    2) dissolving the solid dispersion prepared in the step

         1) in an organic solvent C to form a solid dispersion emulsion, wherein the organic solvent C is an organic solvent which can not dissolve the water-soluble drug but can dissolve the water-insoluble polymer and has a boiling point lower than that of water and can not dissolve or hardly dissolve water;

    3) injecting the solid dispersion emulsion obtained in the step

         2) into an aqueous solution containing a surfactant to form a uniform emulsion;

    4) solidifying the particles in the emulsion by solvent volatilization or solvent extraction, collecting the particles, washing the particles for a plurality of times by ultrapure water to remove the surfactant attached to the surfaces of the particles, and then drying the particles to obtain the slow-release particles;

    the step

         1) is implemented by the following steps;

    11) completely dissolving biodegradable and biocompatible water-insoluble polymer and water-soluble drug in an organic solvent A to form a mixed solution of the drug and the polymer;

    12) injecting the mixed solution into an organic solvent B or injecting the organic solvent B into the mixed solution to generate uniform fine precipitates, collecting the precipitates, washing the precipitates for a plurality of times by using the organic solvent B, and removing the organic solvent B to obtain a solid dispersion of the water-soluble drug and the water-insoluble polymer;

    wherein the organic solvent B is incapable of dissolving the poorly water-soluble polymer and the water-soluble drug;

    the organic solvent A is selected from at least one of glacial acetic acid, acetonitrile, trifluoroacetic acid and dimethyl sulfoxide;

    the organic solvent B is at least one of anhydrous ether, hexane and n-heptane;

    the water-soluble drug is a protein, a nucleic acid and a peptide having no more than 30 amino acid residues;

    in the solid dispersion, the mass ratio of the water-soluble drug to the water-insoluble polymer is 1;



    the organic solvent C is at least one selected from aliphatic hydrocarbon, halogenated hydrocarbon, aliphatic ester, aromatic hydrocarbon and ether.

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