Preparation method of long-acting sustained-release microspheres containing bevacizumab

A technology of bevacizumab and slow-release microspheres, which is applied in the direction of antibody, anti-tumor drug, block delivery, etc., can solve the problem of disputes about the time interval of repeated drug injection, and achieve convenient clinical use, protection of activity, and improvement of The effect of encapsulation rate

Inactive Publication Date: 2013-03-27
WENZHOU MEDICAL UNIV
View PDF4 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The half-life of bevacizumab in the vitreous is about 3-5 days, many patients need repeated injection

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
  • Preparation method of long-acting sustained-release microspheres containing bevacizumab
  • Preparation method of long-acting sustained-release microspheres containing bevacizumab
  • Preparation method of long-acting sustained-release microspheres containing bevacizumab

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation method of the long-acting slow-release microsphere containing bevacizumab comprises the following steps:

[0038] (1) Prepare a bevacizumab solution with a concentration of 200mg / ml;

[0039] (2) Take the bevacizumab solution prepared in step (1), add sodium alginate, and prepare a bevacizumab solution with a sodium alginate concentration of 15 mg / ml as the inner water phase; the prepared concentration is 150 mg / ml The dichloromethane solution of PLGA of ml, as oil phase, wherein, the polymerization ratio of PLGA is 75 / 25,3W; Prepare the polyvinyl alcohol aqueous solution containing 1000mg / ml calcium ion, the percentage composition of polyvinyl alcohol is 0.25%, as the external aqueous phase;

[0040] (3) Preparation of sustained-release microspheres by W / O / W double emulsion method

[0041] First, the sodium alginate solution as the inner water phase is dispersed into the organic solvent solution of the degradable biomedical polymer material as the oil...

Embodiment 2

[0047] The preparation method of the long-acting slow-release microsphere containing bevacizumab comprises the following steps:

[0048] (1) Concentrate the commercially available bevacizumab injection to obtain a bevacizumab solution with a concentration of 50 mg / ml;

[0049] (2) Take the bevacizumab solution prepared in step (1), add sodium alginate, and prepare a bevacizumab solution with a sodium alginate concentration of 10 mg / ml as the inner water phase; the prepared concentration is 300 mg / ml The dichloromethane solution of the PLGA of ml, as oil phase, wherein, the polymerization ratio of PLGA is 50 / 50, 10W;

[0050] Prepare polyvinyl alcohol aqueous solution containing 1000mg / ml calcium ion, the percentage composition of polyvinyl alcohol is 2%, as the external water phase;

[0051] (3) Preparation of sustained-release microspheres by W / O / W double emulsion method

[0052] First, the sodium alginate solution as the inner water phase is dispersed into the organic solv...

Embodiment 3

[0058] The preparation method of the long-acting slow-release microsphere containing bevacizumab comprises the following steps:

[0059] (1) Concentrate the commercially available bevacizumab injection to obtain a bevacizumab solution with a concentration of 500 mg / ml;

[0060] (2) Take the bevacizumab solution prepared in step (1), add sodium alginate, and prepare a bevacizumab solution with a sodium alginate concentration of 5 mg / ml as the inner water phase; the prepared concentration is 10 mg / ml ml of PLGA in dichloromethane, as the oil phase,

[0061] Prepare polyvinyl alcohol aqueous solution containing 1000mg / ml calcium ion, the percentage composition of polyvinyl alcohol is 15%, as the external water phase;

[0062] (3) Preparation of sustained-release microspheres by W / O / W double emulsion method

[0063] First, the sodium alginate solution as the inner water phase is dispersed into the organic solvent solution of the degradable biomedical polymer material as the oil ...

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
Concentrationaaaaaaaaaa
Concentrationaaaaaaaaaa
Concentrationaaaaaaaaaa
Login to view more

Abstract

The invention discloses a preparation method of long-acting sustained-release microspheres containing bevacizumab, which is a preparation method of the sustained-release microspheres formed by encapsulating water-soluble drug protein bevacizumab in a degradable biomedical polymer material. The microspheres are prepared by a W/O/W (water-in-oil-in-water) solvent evaporation method, which comprises the steps of: dispersing bevacizumab and a solution thereof and alginate as inner water phases into a solution which uses the degradable biomedical polymer material as an oil phase to form colostrum; dispersing the colostrum into an outer water phase which is water liquid containing emulsifier to form multiple emulsion; and stirring, distilling in reduced pressure, centrifuging, washing and drying to obtain the bevacizumab sustained-release microspheres. According to the long-acting sustained-release microspheres containing bevacizumab prepared by the method, the encapsulation efficiency of the water-soluble protein drug can be effectively improved, the drug protein activity is not influenced, the releasing time of water-soluble protein can be effectively prolonged, and the sustained release period can be 2-3 months, even longer, so that the number of injection times can be reduced. The preparation method is convenient for clinical application.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a method for preparing long-acting sustained-release microspheres containing bevacizumab. Background technique [0002] Bevacizumab, namely rhMAb VEGF, bevacizumab, and Avastin, was developed by Roche. It is a full-length monoclonal antibody that inhibits vascular endothelial growth factor VEGF, with a molecular weight of 149kDa. It has specific affinity for all subtypes of human VEGF and can Combine and block all isomers of VEGF, and inhibit angiogenesis by inhibiting VEGF. The U.S. FDA obtained the approval of the U.S. Food and Drug Administration at the end of February 2004, and it was launched in the U.S. in March of the same year. Antibody drugs. The drug was first approved for the first-line treatment of advanced colorectal cancer in combination with chemotherapy. In ophthalmology, Bevacizumab has considerable application prospects in the treatment of...

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): A61K9/16A61K39/395A61K47/36A61P35/00A61P27/02A61P9/10
Inventor 孟永春郑钦象南开辉任月萍陈浩
Owner WENZHOU MEDICAL UNIV
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

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap