Drug-loading microsphere as well as preparation method and applications thereof

A technology of drug-loaded microspheres and drugs, which can be used in pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., and can solve problems such as difficulty in controlling the sustained release rate of drugs

Active Publication Date: 2017-08-11
SANJIE BIOLOGICAL SCI & TECH BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to overcome the defect that the slow-release rate of the drug is difficult to control in the prior a

Method used

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  • Drug-loading microsphere as well as preparation method and applications thereof
  • Drug-loading microsphere as well as preparation method and applications thereof
  • Drug-loading microsphere as well as preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] This example is used to illustrate the drug-loaded microspheres of the present invention and its preparation method and application.

[0061] (1) Preparation of water phase: Weigh 2g of polyvinyl alcohol PVA (the weight average molecular weight is 20000g / mol, purchased from Acros Organics), slowly add 100ml of water, then stir for 10 minutes at 500r / min speed, then mix polyvinyl alcohol with The water mixture was placed in a water bath at 90°C, heated in the water bath for 10 minutes, taken out, left for 1 hour, and cooled to room temperature for later use.

[0062] (2) Oil phase preparation: 90mg 5-fluorouracil (5-FU) and 3ml dichloromethane were stirred and mixed at 500r / min for 12h, and then 450mg L-polylactic acid PLLA (weight-average molecular weight 80000g / mol, purchased (from Jinan Daigang Bioengineering Co., Ltd.) vortexed for 1 minute, then added 150 μl of absolute ethanol, and vortexed for 1 min.

[0063] (3) Preparation of microspheres: Pour 3ml of the oil p...

Embodiment 2

[0068] This example is used to illustrate the drug-loaded microspheres of the present invention and its preparation method and application.

[0069] (1) Water phase preparation: Weigh 2g polyvinyl alcohol (weight average molecular weight is 30000g / mol, purchased from Acros Organics), slowly add 100ml water, then stir at 500r / min for 10 minutes, then mix polyvinyl alcohol with water The mixed solution was placed in a water bath at 90°C, heated in the water bath for 10 minutes, taken out, left for 1 hour, and cooled to room temperature for later use.

[0070] (2) Oil phase preparation: 60mg 5-fluorouracil (5-FU) and 3ml dichloromethane were stirred and mixed at 500r / min for 12h, and then 450mg polylactic acid-glycolic acid copolymer PLGA (weight average molecular weight 40000g / mol, the monomer ratio is 75 / 25, purchased from Jinan Daigang Bioengineering Co., Ltd.) Vortex to dissolve for 1 minute, then add 30 μl of isopropanol, and vortex to mix for 1 min.

[0071] (3) Preparati...

Embodiment 3-4

[0074] This example is used to illustrate the drug-loaded microspheres of the present invention and its preparation method and application.

[0075] The drug-loaded microspheres were prepared according to the method of Example 2, except that the amount of isopropanol was 150 μl and 300 μl, respectively, to prepare polylactic acid-glycolic acid copolymer microspheres loaded with 5-FU.

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Abstract

The invention relates to the field of medicine preparation, and discloses a method for preparing a drug-loading microsphere. The method comprises the following steps: mixing a surfactant and water, thus obtaining a water phase; mixing a medicine, a polymer material for a medicine carrier, a first solvent and a second solvent, thus preparing an oil phase; adding the oil phase into the water phase, and carrying out mixing, wherein the first solvent is different from the second solvent, the second solvent and the first solvent are mutually soluble, the second solvent is at least one of C1-C3 alcohols, C1-C3 fatty acids, C1-C3 aliphatic esters, C1-C2 ethers, and acetonitrile, and the use amount of the first solvent is greater than the use amount of the second solvent. The invention further relates to the drug-loading microsphere prepared by adopting the method, and applications of the drug-loading microsphere. The release amount within 0.5h of the drug-loading microsphere prepared by adopting the method provided by the invention is required to be lower than 20% which conforms to the pharmacopoeia criterion, and in addition, the microsphere can be used for preparing medicines for treating tumor and mucosa-relevant diseases, and is taken as the component of the suppository, mucosa flushing fluid, effervescent tablets, ointment, powder and medical membranes.

Description

technical field [0001] The present invention relates to the field of drug preparation, in particular to a drug-loaded microsphere and its preparation method and application. Background technique [0002] Drug-loaded microspheres generally refer to spherical particles with a particle size of 1-500 microns, which mainly include two components, one is the skeleton material of the microspheres, and the other is the raw material drug entrapped in the microspheres. Drug-loaded microspheres need to be in contact with human tissue to exert their clinical efficacy. Therefore, the skeleton material is generally a material with good biocompatibility and can be degraded in the human body, including artificially synthesized polymers and natural polymers. Polymers, etc., the above two types of materials are described in detail in the Pharmacopoeia, and are widely used as excipients in the field of biomedicine. Drug-loaded microspheres prolong the release period of drugs and reduce toxic ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/513A61K47/32A61K47/34A61P35/00
CPCA61K9/1635A61K9/1641A61K31/513A61K9/16A61K47/32A61K47/34
Inventor 张悦梁捷杜建英
Owner SANJIE BIOLOGICAL SCI & TECH BEIJING
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