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Method for preparing hydrophobic drug-carrying core-shell structure micro/nanoparticles through electrostatic spraying

A hydrophobic drug, core-shell structure technology, applied in the field of pharmacy, can solve the limitations of the wide application of drug-loaded micro/nanoparticles, the poor stability of drug-loaded micro/nanoparticles, and the particle size distribution of drug-loaded micro/nanoparticles. It can achieve the effect of prolonging the action time of the drug, high affinity, and reducing the early burst release.

Inactive Publication Date: 2014-07-30
杨晔
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main problems faced by the existing preparation technology of drug-loaded micro / nanoparticles are: (1) The stability of the prepared drug-loaded micro / nanoparticles is not good, and the phenomenon of drug aggregation is serious; (2) Steps such as crushing and sieving are often required, The process is complicated, there are many influencing factors, and the obtained drug-loaded micro / nanoparticles have a wide particle size distribution; (3) Some non-degradable materials, such as surfactants, are often added during the preparation process; (4) The residual organic solvent is high, and it is difficult to effectively remove, etc.
These problems limit the further widespread application of drug-loaded micro / nanoparticles

Method used

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  • Method for preparing hydrophobic drug-carrying core-shell structure micro/nanoparticles through electrostatic spraying
  • Method for preparing hydrophobic drug-carrying core-shell structure micro/nanoparticles through electrostatic spraying
  • Method for preparing hydrophobic drug-carrying core-shell structure micro/nanoparticles through electrostatic spraying

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] A. Dissolve neogambogic acid, the active ingredient of anti-tumor plant medicine, and polylactic acid, a fat-soluble polymer material, in chloroform to form a homogeneous solution. The ratio of neogambogic acid to polylactic acid is 1:250, and the solution viscosity is 100 m·Ps;

[0022] B, dissolving the water-soluble polymer material chitosan in water to form a homogeneous aqueous phase solution, the solution viscosity is 100 m·Ps;

[0023] C. Slowly drop the solution of step A into the solution of step B. The ratio of the solution of step A to the solution of step B is 1:25. After forming an oil-in-water emulsion, spray it with a high-voltage electrostatic spraying method. The diameter of the nozzle is 0.4 mm. The speed is 0.02 ml / min, the voltage is 20 kV, and the collection distance is 15 cm. After collection and drying, the hydrophobic drug-loaded core-shell structure micro / nanoparticles are neogambogic acid-polylactic acid / chitosan.

Embodiment 2

[0025] This embodiment is the same as Embodiment 1, except that the hydrophobic drug in step A is the antipsychotic drug haloperidol, and the fat-soluble polymer material is polypropylene resin, and haloperidol and polypropylene The resin ratio is 1:100, the solution viscosity is 200 m·Ps; the water-soluble polymer material in step B is sodium carboxymethyl cellulose, and the solution viscosity is 200 m·Ps; The ratio of the solution is 1:50. After forming an oil-in-water emulsion, it is sprayed by a high-voltage electrostatic spraying method. The diameter of the nozzle is 0.5 mm, the spray speed is 0.05 ml / min, the voltage is 18 kV, and the collection distance is 17 cm. Finally, the hydrophobic drug-loaded core-shell structure micro / nano particles are haloperidol-polypropylene resin / carboxymethyl cellulose sodium.

Embodiment 3

[0027]This example is the same as Example 1, except that the hydrophobic drug in step A is the lipid-regulating drug lovastatin, the fat-soluble polymer material is polyisobutene, and the ratio of lovastatin to polyisobutene is 1:500 , the solution viscosity is 1500 m·Ps; the water-soluble polymer material in step B is gelatin, and the solution viscosity is 1500 m·Ps; the ratio of step A solution to step B solution is 1:100, after forming an oil-in-water emulsion The injection was carried out by high-voltage electrostatic spraying method, the diameter of the nozzle was 0.7 mm, the injection speed was 0.10 ml / min, the voltage was 15 kV, and the collection distance was 20 cm. Vastatin - polyisobutylene / gelatin.

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Abstract

The invention discloses a method for preparing hydrophobic drug-carrying core-shell structure micro / nanoparticles through electrostatic spraying, and relates to the field of pharmaceutics. The method comprises the following steps: jointly dissolving a hydrophobic drug and a lipid solubility high polymer material in an organic solvent, emulsifying and dissolving in an aqueous solution containing a water-soluble polymer material; and putting the obtained oil-in-water emulsion in a trace propeller, carrying out electrostatic spraying under the effect of a high-voltage electrostatic field, and thus finally obtaining the hydrophobic drug-carrying core-shell structure micro / nanoparticles. The preparation method is simple to operate, low in cost, environment-friendly and suitable for industrial production. The prepared hydrophobic drug-carrying core-shell structure micro / nanoparticles are controllable in particle sizes, have targeting property on tissues and organs and are beneficial to prolonging of action time of the drug.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a method for preparing hydrophobic drug-loaded core-shell structure micro / nano particles by electrostatic spraying technology. Background technique [0002] Micro / nanoparticle drug delivery systems are mainly used in drug dosage forms that improve the bioavailability of poorly soluble drugs. At present, the commonly used preparation techniques of drug-loaded micro / nanoparticles include melting method, solvent method, solvent-melting method, grinding method, solvent spray drying method, freeze drying method and so on. The main problems faced by the existing preparation technology of drug-loaded micro / nanoparticles are: (1) The stability of the prepared drug-loaded micro / nanoparticles is not good, and the phenomenon of drug aggregation is serious; (2) Steps such as crushing and sieving are often required, The process is complicated, there are many influencing factors, and the obtained drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K45/00A61K31/352A61J3/00
Inventor 杨晔尹登科
Owner 杨晔
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