Drug-loaded microsphere and preparation method thereof

A technology of drug-loaded microspheres and microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., which can solve problems such as high production costs, cumbersome procedures, and increased production costs. Achieve good physical and chemical properties, reduce preparation procedures, and reduce production costs

Active Publication Date: 2021-04-06
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the common dehumidification phenomenon in the preparation process, the polypeptide and protein drugs dissolved in the inner water phase are easy to enter the outer water phase, resulting in drug leakage, encapsulation efficiency and drug loading decrease.
This will not only increase production costs, but also reduce treatment efficiency, reduce patient compliance, and even produce toxic side effects
In addition, the double emulsion method involves two emulsification processes, the process is cumbersome, the production cost is high, and it brings a lot of uncertainty to the final microspheres

Method used

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  • Drug-loaded microsphere and preparation method thereof
  • Drug-loaded microsphere and preparation method thereof
  • Drug-loaded microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] This example discloses the preparation of ultra-high-loaded polypeptide, protein microspheres, and spermine-modified acetalized dextran (AcDX-SP)-coated insulin (INS) microspheres (INS@AcDX-SP).

[0049] Acetone and INS (20 mg / mL) hydrochloric acid solution were used as the first reactant and the second reactant respectively, and INS nanoparticles were formed under stirring conditions. AcDX-SP dimethyl carbonate solution and 1% povidone (PVA) solution were used as the third reactant and the fourth reactant respectively. The oil-in-water emulsion is prepared by a microfluidic device and solidified by a solvent extraction method to obtain microspheres. A series of microspheres were obtained by adjusting the feeding ratio of INS and framework materials, with an average particle size of 35-65 μm and a drug loading of 37.0-76.6% ( figure 1 ), the encapsulation efficiency is 95.0-99.9% ( figure 2 ).

Embodiment 2

[0051] This example discloses the preparation of ultra-high-loaded polypeptide and protein microspheres, AcDX-SP-coated bovine serum albumin (BSA) microspheres (BSA@AcDX-SP).

[0052] Acetonitrile and BSA (20 mg / mL) aqueous solution were used as the first reactant and the second reactant respectively, and BSA nanoparticles were formed under stirring conditions. AcDX-SP dimethyl carbonate solution and 1% povidone (PVA) solution were used as the third reactant and the fourth reactant respectively. The oil-in-water emulsion is prepared by a microfluidic device and solidified by a solvent extraction method to obtain microspheres. A series of microspheres were obtained by adjusting the feeding ratio of BSA and the framework material, and the drug loading was 40.0-58.5% ( Figure 8 ), the encapsulation efficiency is 73.2-99.9% ( Figure 9 ).

Embodiment 3

[0054] This example discloses the preparation of ultra-high-loaded polypeptide and protein microspheres, AcDX-SP-wrapped β-lactoglobulin (β-LG) microspheres (β-LG@AcDX-SP).

[0055] An aqueous solution of tetrahydrofuran and β-LG (50 mg / mL) was used as the first reactant and the second reactant respectively, and β-LG nanoparticles were formed under stirring conditions. AcDX-SP dimethyl carbonate solution and 1% povidone (PVA) solution were used as the third reactant and the fourth reactant respectively. The oil-in-water emulsion is prepared by a microfluidic device and solidified by a solvent extraction method to obtain microspheres. A series of microspheres were obtained by adjusting the feeding ratio of β-LG and the framework material, and the drug loading was 39.3-61.1% ( Figure 15 ), the encapsulation efficiency is 51.4-100.0% ( Figure 16 ).

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Abstract

The invention discloses a drug-loaded microsphere and a preparation method thereof. The drug-loaded microsphere comprises nanoparticles containing active pharmaceutical ingredients and a framework material for wrapping a drug and controlling drug release, wherein the mass of the active pharmaceutical ingredients accounts for 1-80% of the mass of the whole microsphere; the encapsulation efficiency of the active pharmaceutical ingredients in the encapsulation process is 50-100%; and the particle size of the microspheres is 0.5-2000 [mu] m. The preparation method comprises the steps of precipitating the active pharmaceutical ingredients to form drug nanoparticles; then dispersing the drug nanoparticles in an oil phase to prepare an oil-in-water emulsion; and curing the oil-in-water type emulsion to form microspheres. The microspheres are relatively high in encapsulation efficiency and drug loading capacity, the treatment efficiency is improved, and extremely high application value is achieved.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a drug-loaded microsphere and a preparation method thereof. Background technique [0002] Polypeptides and proteins are essential components of life in nature. In 1982, the U.S. Food and Drug Administration approved the marketing of human insulin produced by recombinant DNA technology for the treatment of diabetes. Since then, peptide and protein drugs have attracted much attention as an alternative treatment plan. Compared with traditional drugs, peptide and protein drugs show obvious advantages, such as higher affinity and selectivity, good tolerance, lower toxicity, shorter time to market and standard synthesis scheme . Over the years, the number and frequency of use of peptide and protein drugs have increased dramatically. According to reports, the market for peptide and protein drugs grew at an annual rate of 8% in 2014, twice that of small ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/26A61K47/34A61K47/38A61K45/00A61K47/54
CPCA61K9/1623A61K9/1647A61K9/1652A61K9/1641A61K45/00A61K47/543Y02A50/30
Inventor 刘东飞孙宏斌张佩
Owner CHINA PHARM UNIV
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