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Preparation of degradable pollutant polyalcohol stephanoporate microballoons and uses thereof

A technology of porous microspheres and polymers, applied in the field of biomedical engineering, can solve the problems affecting the efficacy of active proteins and polypeptides, adverse effects of drug properties, and reduced drug properties, etc., to maintain activity and efficacy, avoid damage, and compare The effect of large surface area

Inactive Publication Date: 2008-08-27
SOUTHWEST JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the preparation process of this method, the degradable polymer and the drug are dissolved in the organic solvent at the same time, which has a great impact on the drug, especially the protein active drug, and even leads to the loss of drug activity, which greatly affects the protein and polypeptide active drug. curative effect; at the same time, the stirring in the process of adding the organic solvent makes the drug bear the effect of shear force, and the oil-water interface will also have an adverse effect on the drug properties of the drug, further reducing the drug properties of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A preparation method of biodegradable polymer porous microspheres, the specific method is:

[0030] a Prepare the oil phase Dissolve 0.3 g of polylactic acid, a biodegradable polymer, in 3 ml of methylene chloride organic solvent to form an oil phase with a mass-volume concentration of 10% (g / ml).

[0031] b Preparation of the inner water phase Dissolve 0.03 g of sodium oleate as a porogen (10% of 0.3 g of polylactic acid) in water to form the inner water phase.

[0032] c to form colostrum, add the inner water phase prepared in step b to the oil phase prepared in step a dropwise at a volume ratio of 10:100 (inner water to oil phase), stir to emulsify, and the emulsification time After 10 minutes, water-in-oil colostrum is formed.

[0033] d Preparation of the external water phase Prepare an aqueous solution of polyvinyl alcohol with a mass volume ratio concentration of 1% (g / ml) as the external water phase.

[0034] e prepare the double emulsion, inject the colostrum...

Embodiment 2

[0039] This example is basically the same as Example 1, except that: when preparing the inner aqueous phase in step b, ammonium bicarbonate is used as the porogen. The prepared degradable polymer porous microsphere has an average particle diameter of 12 microns, a porosity of 98±5%, and an average pore diameter of 0.5 microns. The microsphere can be used for the adsorption of protein and polypeptide active drugs as a drug carrier.

[0040] The biodegradable polymer porous microspheres prepared in this example can be used as active drug carriers. Into the drug solution, the drug is adsorbed for 5 minutes, and after drying, the active drug is carried in the biodegradable polymer porous microsphere.

Embodiment 3

[0042] This example is basically the same as Example 1, except that: when preparing the inner aqueous phase in step b, polyoxyethylene-polyoxypropylene copolymer (Pluronic F127) is used as the porogen. The prepared degradable polymer porous microsphere has an average particle diameter of 10 microns, a porosity of 98±5%, and an average pore diameter of 0.5 microns. The microsphere can be used for the adsorption of protein and polypeptide active drugs as a drug carrier.

[0043] The biodegradable polymer porous microspheres prepared in this example can be used as active drug carriers. Immerse in the drug solution for drug adsorption for 200 minutes. After drying, the active drug is carried in the biodegradable polymer porous microspheres.

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PUM

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Abstract

A preparation method for porous microspheres of a biodegradable polymer is provided. The method comprises the following steps: (a) dissolving a biodegradable polymer in an organic solvent to form an oil phase of 1-30% (g / ml) concentration; (b) selecting a pore-forming agent 1-50% of the biodegradable polymer in the step (a) and dissolving the pore-forming agent in water to form an internal water phase; (c) adding dropwise the internal water phase into the oil phase at a volume ratio of (1-30):100, and stirring to form a primary emulsion; (d) preparing a polyvinyl alcohol aqueous solution of 0.5-10% (g / ml) concentration, which serves as an external water phase; (e) pouring the primary emulsion into the external water phase at a volume ratio of (3-30):100, stirring or performing ultrasonic treatment to form a double-emulsion, and allowing the polymer in the double-emulsion to solidify, thereby forming microspheres; (f) freeze-drying the microspheres to obtain the final product. The obtained porous microspheres of the biodegradable polymer have high porosity, large specific surface area and good adsorption and encapsulation properties; and are used for the adsorption and encapsulation of unstable protein drugs, polypeptide drugs and growth factors and can retain pharmaceutical activity and effectiveness thereof.

Description

technical field [0001] The invention relates to biomedical engineering, in particular to a method for preparing biodegradable polymer microspheres and the use of the prepared biodegradable polymer porous microspheres. Background technique [0002] With the development of biopharmaceutical technology, protein and peptide active drugs have advantages in recent years due to their good therapeutic effect, less toxic and side effects, and certain effects on disease prevention, clinical treatment and solving the problems of protein quantity deficiency and function loss in the body. The use of protein-based drugs is on the rise. However, protein drugs have the characteristics of large molecular weight and complex spatial structure, and are easily damaged by the physiological environment, especially enzymes, during drug delivery. In addition, its inherent weak penetration ability and natural instability determine its easy inactivation characteristics. Therefore, it is of great sig...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/18A61K38/16A61K47/34A61K47/32
Inventor 周绍兵孙林蒋婧王卫佳汪建新李孝红翁杰
Owner SOUTHWEST JIAOTONG UNIV
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