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Polymer composite microspheres, and preparation method and application thereof

A technology of composite microspheres and polymers, applied in the directions of active ingredients of heterocyclic compounds, non-active ingredients of polymer compounds, microcapsules, etc. low release effect

Inactive Publication Date: 2019-10-08
GUANGDONG PROV MEDICAL INSTR INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the microspheres prepared by the above-mentioned prior art generally have (1) a strong burst release effect during application; (2) the problems of complex preparation process and difficulty in industrialization

Method used

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  • Polymer composite microspheres, and preparation method and application thereof
  • Polymer composite microspheres, and preparation method and application thereof
  • Polymer composite microspheres, and preparation method and application thereof

Examples

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preparation example Construction

[0024] The coating process can be general physical coating, and polymer compounds include water-soluble polymers and degradable polymers. Preferably, the preparation method of polymer composite microspheres comprises the following steps:

[0025] S1, preparation of pre-coating solution

[0026] Mix protein-binding functional molecules, albumin and water-soluble polymers to form a pre-coating solution, first use albumin and protein-binding functional molecules to combine, use the electrostatic force, hydrogen bond, affinity The combination of non-covalent bonds such as water force can make the sustained release performance of functional molecules prepared into microsphere materials better, and significantly reduce the burst release effect.

[0027] Specifically, the albumin is selected from any one or more of chicken serum albumin, bovine serum albumin, and human serum albumin. The specific functional molecules are combined to finally reduce the effect of burst release. The ...

Embodiment 1

[0048] The present embodiment provides a kind of preparation method of polymer composite microsphere, it comprises the following steps:

[0049] Dissolve 100mg warfarin sodium and 2000mg bovine serum albumin in 15mL aqueous solution containing 2000mg starch, and disperse for 30min at a speed of 500rpm to obtain a bovine serum albumin / starch aqueous solution loaded with warfarin sodium; take 1.0mL of the aqueous solution Pour into 10mL tetrahydrofuran solution containing 2.0g polybutylene succinate (molecular weight: 100,000 Daltons), and emulsify at 2000rpm for 2min; add the above emulsion into 500mL aqueous solution containing 1.0% methylcellulose , stirred at 550rpm at room temperature for 6h; washed 3 times, soaked in an aqueous solution containing potassium hydroxide, pH = 12 for 10min, washed 3 times again, centrifuged and freeze-dried at -50°C for 48h to obtain warfarin sodium release bovine serum albumin / polybutylene succinate composite microspheres.

Embodiment 2

[0051] The present embodiment provides a kind of preparation method of polymer composite microsphere, it comprises the following steps:

[0052] Dissolve 100 mg of dicoumarin and 1000 mg of human serum albumin in 15 mL of aqueous solution containing 3000 mg of cationic polyacrylamide, and disperse ultrasonically for 45 minutes to obtain a human serum albumin / cationic polyacrylamide aqueous solution loaded with dicoumarin; take 0.5 Pour this aqueous solution into 10 mL of tetrahydrofuran solution containing 1.5 g of polycaprolactone (molecular weight: 50,000 Daltons), and emulsify at 2000 rpm for 3 min; Stir at 350rpm for 8h; wash with water for 3 times, soak in an aqueous solution containing potassium hydroxide and pH=10 for 8min, wash with water again for 3 times, centrifuge and freeze-dry at -70°C for 36h to obtain the human dicoumarin release Serum albumin / polycaprolactone composite microspheres.

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Abstract

The invention discloses polymer composite microspheres, and a preparation method and application thereof, and relates to the technical field of microsphere materials. The polymer composite microspheres comprise macromolecular compounds, albumin and protein binding type functional molecules, wherein the macromolecular compounds are used for coating the albumin and the protein binding type functional molecules. According to the preparation method of the polymer composite microspheres, the macromolecular compounds are used for coating the albumin and the protein binding type functional moleculesto form a microsphere structure, through the effects of the albumin and the effects of the protein binding type functional molecules, the effect of slowly releasing the protein binding type functionalmolecules for a long term can be achieved, and the sudden release effects of the protein binding type functional molecules can be alleviated. The polymer composite microspheres can be applied as slowrelease functional materials, and can be particularly used as drug bearing microsphere for slow release of drugs.

Description

technical field [0001] The invention relates to the technical field of microsphere materials, and in particular to a polymer composite microsphere, its preparation method and application. Background technique [0002] Polymer microspheres usually refer to polymer aggregates with diameters ranging from nanometers to micrometers and spherical shapes. Polymer microspheres have attracted more and more scientists' interest due to their designability and multifunctionality. The matrix-type microspheres formed by dissolving or dispersing drugs in polymer materials are called drug-loaded microspheres, which is currently the most widely used way of polymer-loaded drugs. After the drug is entrapped in the microspheres, it can be administered orally, injected or implanted according to factors such as the particle size and surface properties of the microspheres. More importantly, by adjusting the molecular weight of the polymer, the particle size of the microspheres, drug distribution,...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/52A61K47/42A61K47/34A61K31/37A61K31/616A61K31/4164A61K31/167
CPCA61K9/5031A61K9/5052A61K31/167A61K31/37A61K31/4164A61K31/616
Inventor 许为康陈龙胜邹丽丽
Owner GUANGDONG PROV MEDICAL INSTR INST
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