Polymer composite microsphere as well as preparation method and application thereof

A technology of composite microspheres and macromolecules, which is applied in the directions of non-active ingredients of macromolecular compounds, medical preparations of non-active ingredients, and medical preparations containing active ingredients, etc. Problems such as poor batch stability and uncontrollable degradation behavior of microspheres

Pending Publication Date: 2022-03-04
INST OF MEDICINE & HEALTH GUANGDONG ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Degradable polyesters are basically hydrophobic materials, which have made significant progress in the field of controlled release of hydrophilic drugs, but the main component of human body fluids is water, so if it is used as a carrier for hydrophobic drugs, it will Lead to increased release resistance of hydrophobic drugs, resulting in failure to achieve the expected curative effect of hydrophobic drugs
[0005] In order to improve the above problems in related technologies, two ideas have been proposed. One is to still use hydrophobic polymers as the carrier material of hydrophobic drugs, but to prepare drug-loaded microspheres with a porous interconnected structure on the drug-loaded materials to improve hydrophobicity. The amount of released drugs, the batch stability of degradable microspheres prepared by this method is poor; the second is to use water-soluble polymers such as chitosan, sodium alginate, hyaluronic acid, gelatin, etc. as hydrophobic Carrier materials for drugs, but the degradation behavior of these water-soluble polymers is uncontrollable, which may easily lead to excessive burst release and other phenomena that are not conducive to drug controlled release

Method used

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  • Polymer composite microsphere as well as preparation method and application thereof
  • Polymer composite microsphere as well as preparation method and application thereof
  • Polymer composite microsphere as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0072] In this embodiment, a polymer composite microsphere is prepared, and the specific process is as follows:

[0073] D1. Mix 100mg of naringin with 4mL of an aqueous solution containing 100mg / mL of polyethyleneimine, and stir at 20000rpm for 8min;

[0074] Continue to stir at 3000 rpm for 2 hours at 60°C under nitrogen protection to carry out the wrapping reaction;

[0075] After the reaction was completed, the mixture was centrifugally washed with deionized water for 5 times (the mass volume ratio of each cleaning solid to deionized water was 1:200g / ml), freeze-dried for 48 hours to obtain drug granules;

[0076] D2. Dissolve 2 g of polylactic acid-glycolic acid copolymer (molecular weight is about 30,000 Daltons) in 10 mL of dichloromethane, then add 4,000 mg of the drug granules obtained in step D1, and then stir at 10,000 rpm for 5 min;

[0077] D3. The mixture obtained in step D2 was poured into 300 mL of an aqueous solution containing 1% polyvinyl alcohol 1799, stir...

Embodiment 2

[0080] In this embodiment, a polymer composite microsphere is prepared, and the specific process is as follows:

[0081] D1. 100mg melatonin was mixed with 4.5mL aqueous solution containing 200mg / mL carboxymethyl chitosan, stirred at 12000rpm for 10min;

[0082] Pour it into a 1mol / L sodium hydroxide solution at 95°C under nitrogen protection, and continue to stir at 2500rpm for 4h;

[0083] After the reaction, centrifuge and wash 7 times with deionized water (the mass volume ratio of solid to deionized water is 1:150g / ml), and freeze-dry for 48 hours to obtain drug particles;

[0084] D2. Dissolve 3.6g of poly 3-hydroxybutyrate-co-3-hydroxyvalerate (molecular weight is about 150,000 Daltons) in 10mL of tetrahydrofuran, then add 800mg of the drug granules obtained in step D1, and stir at 18000rpm 2min;

[0085] D3. Pour the mixture obtained in step D2 into 400 mL of an aqueous solution containing 0.8% polyvinyl alcohol 1788, continue stirring at 1500 rpm for 15 h, and then c...

Embodiment 3

[0088] In this embodiment, a polymer composite microsphere is prepared, and the specific process is as follows:

[0089] D1. Mix 100mg of resveratrol with 10mL of an aqueous solution containing 70mg / mL of polyethyleneimine, and stir at 18000rpm for 15min;

[0090] 60°C, under the protection of nitrogen, continue to stir at 4000rpm for 1h to carry out the coating reaction;

[0091] After the reaction, centrifuge and wash the solid with deionized water (the mass volume ratio of solid to deionized water is 1:250g / ml) and freeze-dry the obtained solid for 8 times for 48 hours to obtain drug granules;

[0092] D2. Dissolve 1.4g of polylactic acid (molecular weight is about 3,000 Daltons) in 10mL of dichloromethane, then add 600mg of the drug granules obtained in step D1, and then stir at 12000rpm for 8min;

[0093] D3. Pour the mixture obtained in step D2 into 200 mL of an aqueous solution containing 1.5% methylcellulose, continue stirring at 1000 rpm for 18 hours, and then centri...

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Abstract

The invention discloses a polymer composite microsphere as well as a preparation method and application thereof. The polymer composite microsphere comprises a microsphere matrix, and the preparation raw materials of the microsphere matrix comprise a hydrophobic degradable polymer; the drug particles are dispersed in the microsphere matrix, and each drug particle comprises a hydrophobic drug inner core and a water-soluble polymer layer wrapping the surface of the hydrophobic drug inner core; the surface of the microsphere matrix is coated with the coating film, and preparation raw materials of the coating film comprise natural macromolecules. According to the high-molecular composite microsphere disclosed by the invention, the loading capacity, the release capacity and the controlled release effect of the high-molecular composite microsphere on hydrophobic drugs can be effectively improved through regulation and control of components.

Description

technical field [0001] The invention belongs to the technical field of polymer medicine, and in particular relates to a polymer composite microsphere and its preparation method and application. Background technique [0002] Biodegradable microspheres are tiny spherical materials made of bioabsorbable materials. Affected by the properties of raw materials and processing technology, the particle size is mainly distributed between tens of nanometers and hundreds of microns, and the microspheres are neat in shape and uniformly dispersed. With the development of drug preparation technology, biodegradable microspheres have become the representative of the third generation of drug preparations, which can be used as carriers to load drugs and release drugs slowly through active degradation; re-administration has the advantages of short drug cycle, long drug action time, and safety. High, good curative effect and other significant advantages have attracted the attention of more and m...

Claims

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Application Information

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IPC IPC(8): A61K9/64A61K9/62A61K9/58A61K47/36A61K47/34A61K47/42A61K45/00A61K31/7048A61K31/4045A61K31/05A61K31/496A61K31/155A61P43/00A61P1/00A61P9/00
CPCA61K9/5036A61K9/5031A61K9/5052A61K9/5089A61K9/5073A61K45/00A61K31/7048A61K31/4045A61K31/05A61K31/496A61K31/155A61P43/00A61P1/00A61P9/00
Inventor 许为康王丽艳李桂香
Owner INST OF MEDICINE & HEALTH GUANGDONG ACAD OF SCI
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