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Composition of protein and double chain polyethylene glycol

A polyethylene glycol and protein technology, applied in the field of polyethylene glycol, can solve the problems of poor biological activity of the conjugate, loss of favorable properties, disconnection of the linking agent, etc., and achieve the effect of reducing immunogenicity and not easy to hydrolyze and break.

Inactive Publication Date: 2003-06-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One is that the method of forming these protein-conjugates inactivates the protein, making the resulting conjugates less biologically active
In addition, some linkers used in the formation of these PEG-protein conjugates are prone to hydrolysis and cleavage in vivo. When such cleavage occurs after administration, these conjugates lose the beneficial properties brought by PEG.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1: the preparation of N, N-dipolyethylene glycol acetamido-methic acid succinimidyl ester 4000 (Bis-PEG4000)

[0015] Dissolve 10g of monomethoxypolyethylene glycol amine 4000 in 50ml of toluene, dissolve 500mg of TSAT (triethylamine trisuccinate) in 5ml of DMSO, add dropwise in 50ml of toluene, and react the resulting mixture for 16 hours under electromagnetic stirring , evaporate most of the solvent in vacuo. The resulting precipitate was redissolved in 100 ml of ethyl acetate at 60°C, and placed at 4°C for recrystallization. The filtered crystals were dried in a vacuum dryer to obtain 8.7 g of Bis-PEG white powder.

Embodiment 2

[0016] Embodiment 2: the preparation of N, N-dipolyethylene glycol acetamido-methic acid succinimidyl ester 8000 (Bis-PEG8000)

[0017] Dissolve 20g of monomethoxypolyethylene glycol amine 8000 in 50ml of toluene, dissolve 500mg of TSAT (triethylamine trisuccinate) in 5ml of DMSO, add dropwise in 50ml of toluene, and react the resulting mixture for 16 hours under electromagnetic stirring , evaporate most of the solvent in vacuo. The resulting precipitate was redissolved in 100 ml of ethyl acetate at 60°C, and placed at 4°C for recrystallization. The filtered crystals were dried in a vacuum desiccator to obtain 16.5 g of Bis-PEG white powder.

Embodiment 3

[0018] Embodiment 3: Preparation of N, N-dipolyethylene glycol acetamido-methic acid succinimidyl ester 20000 (Bis-PEG20000)

[0019] Dissolve 40g of monomethoxypolyethylene glycol amine 20000 in 80ml of toluene, dissolve 500mg of TSAT (triethylamine trisuccinate) in 5ml of DMSO, add dropwise in 50ml of toluene, and react the resulting mixture for 16 hours under electromagnetic stirring , evaporate most of the solvent in vacuo. The resulting precipitate was redissolved in 100 ml of ethyl acetate at 60°C, and placed at 4°C for recrystallization. The filtered crystals were dried in a vacuum dryer to obtain 32.1 g of Bis-PEG white powder.

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Abstract

A compound of dual-chain polyethanediol and protein is prepared through dissolving monomethoxy polyethanediol amine in toluene, dissolving triethylamine trisuccinate in dimethyl sulfoxide (DMSO), dropping the latter to the former, electromagnetic stirring, reacting, vacuumizing for evaporating the most of solvent, dissolving deposit in ethylacetate, recrystallizing, filtering, vacuum drying, and reacting with protein in weak-alkaline condition.

Description

technical field [0001] The invention relates to a kind of polyethylene glycol which can be combined with protein, especially refers to double-chain polyethylene glycol and the combination with protein. Background technique [0002] The safety and effectiveness of clinical application of protein drugs has always been a focus of attention and research. Due to poor stability, high plasma clearance rate, short half-life in vivo, protein drugs are prone to antigen-antibody reactions, so they are greatly limited in clinical treatment. Genetic engineering technology has made it possible to synthesize human recombinant proteins on a large scale, which has largely solved the immunogenicity problems caused by heterologous proteins, but still cannot overcome the shortcomings of fast plasma clearance and low bioavailability. These problems can be solved by polyethylene glycol-protein modification technology. The technology of modifying protein with polyethylene glycol is a new technol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/02
Inventor 田浤
Owner CHINA PHARM UNIV
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