Method for preparing polymer microsphere

A technology of polymers and polymer materials, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of poor preparation repeatability, inability to embed hemoglobin, and difficulty in controlling particle size and other problems, to achieve the effect of simple operation and expanding the scope of application

Active Publication Date: 2008-09-24
INST OF PROCESS ENG CHINESE ACAD OF SCI
View PDF4 Cites 43 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional preparation methods use mechanical stirring, homogenization, and other methods to prepare emulsions. Although the process conditions are simple, the preparation repeatability is very poor, and there are large differences in performance between different batches of products, which is not easy for industrial scale-up production. The particle size uniformity is very poor, and the particle size is difficult to control
[0003] Chinese patent (publication number CN1605359) discloses a preparation method of polymer microspheres with uniform size for embedding hydrophilic drugs. , has high requirements on the stability of colostrum, and the preparation efficiency is low. In addition, organic solvents and hydrophobic polymer materials with a solubility in water of less than 2% must be used in the preparation process to prepare uniform and controllable particle sizes. drug microspheres
However, all three methods use a large amount of organic solvents, which can easily denature the drug.
Although the particle size of the microspheres formed by the emulsification diffusion method is small, about 0.1 μm, it cannot effectively entrap hemoglobin
Generally speaking, when preparing nanospheres and nano drug-loaded microspheres, the nanoparticles prepared by the existing technology have uneven particle size, poor repeatability, and high energy consumption, which is not easy for industrial production.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for preparing polymer microsphere
  • Method for preparing polymer microsphere
  • Method for preparing polymer microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The hydrophilic SPG membrane with a pore size of 5.2 μm was soaked in water to fully wet the porous membrane. Dissolve 10 mg of lysozyme in 2 mL of deionized water as the inner water phase, and dissolve 0.2 g of PLGA membrane material (molecular weight: 30,000) in 4 mL of dichloromethane as the oil phase. Mix the inner water phase with the oil phase, and ultrasonically emulsify for 15 seconds in an ice-water bath to obtain W / O colostrum. This colostrum is added in the 1%wt PVA aqueous solution of 40mL, magnetic stirring 300rpm stirs 30s to prepare pre-multiplex emulsion, then this pre-multiplex emulsion is pressed through the microporous membrane device under the operating pressure of 300kPa, obtains multi-emulsion ( Optical micrograph of complex emulsion figure 2 Shown), the time for the emulsion to pass through the membrane is less than 1s, and then the double emulsion is stirred at room temperature for 24 hours to remove the organic solvent methylene chloride, and ...

Embodiment 2

[0054] The hydrophilic SPG membrane with a pore size of 5.2 μm was soaked in water to fully wet the porous membrane. Dissolve 0.2g of PLGA membrane material (molecular weight: 30,000) in 4mL of dichloromethane as the oil phase, then add 10mg of lysozyme solid particles into the oil phase, and ultrasonically emulsify in an ice-water bath for 15s to obtain the S / O type initial phase. milk. The colostrum was added to 40mL of 1%wt PVA aqueous solution, magnetically stirred at 300rpm for 30s to prepare a pre-multiplex emulsion, and then the pre-multiplex emulsion was pressed through a microporous membrane device at an operating pressure of 300kPa to obtain a multi-emulsion, Stir the double emulsion at room temperature for 24 hours to remove the organic solvent dichloromethane, and then centrifuge and wash to obtain drug-loaded microcapsules. The obtained microcapsules were vacuum-dried for 48 h to obtain finished microcapsules. The electron micrograph of the microcapsule obtained...

Embodiment 3

[0056] The hydrophilic SPG membrane with a pore size of 5.2 μm was soaked in water to fully wet the porous membrane. With 0.8ml of 2mg / mL hepatitis B surface antigen solution as the inner aqueous phase, the copolymer of 0.2g polylactic acid-polyglycolic acid and polyethylene glycol (molecular weight 40,000, the ratio of polylactic acid and polyglycolic acid is 50 / 50, the mass fraction of polyethylene glycol is 20%) was dissolved in 4mL of dichloromethane, as the oil phase, then the inner water phase was added to the oil phase, ultrasonic emulsification in ice-water bath for 15s, to obtain W / O type colostrum. Add the colostrum to 40mL of 1%wt PVA in 0.9wt%NaCl aqueous solution, magnetically stir at 300rpm and stir for 30s to prepare the pre-multiplex emulsion, and then press the pre-multiplex emulsion through the microporous membrane device under the operating pressure of 300kPa , to obtain a double emulsion, and then stir the double emulsion at room temperature for 24 hours ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Apertureaaaaaaaaaa
Volume average particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
Login to view more

Abstract

The invention discloses a preparation method of polymer microballoon sphere with uniform size, which can dissolve biodegradable polymer material in at least one organic solvent to form an O phase, and then adds the optional aqueous solution W1 containing medicine or medicine granule S into a fat phase O for emulsification to prepare colostrum; the obtained colostrum is added into an outer water phase W containing stabilizing agent to form pre-compound emulsion; then, the pre-compound emulsion is pressed through a microporous film by pressure to obtain compound latex; at last, after being solidified, the compound latex is centrifugated, washed, frozen and dried, so as to obtain the polymer microballoon sphere. The method of the invention is simple in technique, uniform in the grain diameter of the obtained product, good in repetitiveness of each batch product and easy in commercial process.

Description

technical field [0001] The invention relates to a preparation method of polymer microspheres in the fields of medicine, biochemical industry, etc., more specifically, relates to a preparation method of rapidly preparing polymer microspheres with uniform size. Background technique [0002] Drug-loaded polymers play an important role in the controlled release system of drugs. The solvent evaporation / extraction method has been used to prepare drug microspheres for a long time, but most of them are still in the stage of laboratory research, and there are still many problems. This restricts the clinical application of microsphere preparations. Traditional preparation methods use mechanical stirring, homogenization, and other methods to prepare emulsions. Although the process conditions are simple, the preparation repeatability is very poor, and there are large differences in performance between different batches of products, which is not easy for industrial scale-up production. ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/16A61K47/34A61K45/00A61K48/00C08J3/12
Inventor 马光辉卫强苏志国宋薇赖波
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products