Glycopeptide conjugate microsphere or microcapsule and its prepn process

A conjugate and glycopeptide technology, applied in the field of glycopeptide conjugate microspheres or microcapsules and their preparation through interfacial polymerization, can solve the problems of complex microcapsule steps and achieve good tissue compatibility and degradability properties, simple preparation process, and mild reaction conditions

Inactive Publication Date: 2007-03-21
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation of microcapsules

Method used

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  • Glycopeptide conjugate microsphere or microcapsule and its prepn process
  • Glycopeptide conjugate microsphere or microcapsule and its prepn process
  • Glycopeptide conjugate microsphere or microcapsule and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Dissolve 4 grams of chitosan in 100ml of deionized water (containing 2.8ml of glacial acetic acid), add 100ml of absolute ethanol and 32ml of pyridine after all dissolve, stir until clear, then add 3.6ml of acetic anhydride, and stir at room temperature for 2 hours. The reaction solution was poured into ethanol and filtered with suction to obtain a white precipitate. The crude product was dissolved in water, and the insoluble matter was removed by centrifugation. The filtrate was added with 200ml of absolute ethanol, and the supernatant was discarded after centrifugation. The precipitate was washed with acetone and anhydrous ether in turn, and dried in vacuum at room temperature for 24 hours to obtain a white flocculent solid. The degree of deacetylation of the product measured by acid-base titration was 43%.

[0047] Under Ar protection, prepare 0.1g / 10ml above-mentioned chitosan aqueous solution in 100ml three-neck flask. Weigh 0.6825g L-leucine-N-carboxylic acid int...

Embodiment 2

[0049] Dissolve 4 grams of chitosan in 100ml of deionized water (containing 2.8ml of glacial acetic acid), add 100ml of absolute ethanol and 32ml of pyridine in turn after all the dissolution, stir until clear, then add 3.6ml of acetic anhydride, and stir at room temperature for 3 hours. The reaction solution was poured into ethanol and filtered with suction to obtain a white precipitate. Dissolve the crude product with an appropriate amount of deionized water, centrifuge to remove insoluble matter, add 200ml of absolute ethanol to the filtrate, discard the supernatant after centrifugation, wash the precipitate with acetone and anhydrous ether in turn, and dry it in vacuum at room temperature for 24 hours to obtain a white flocculent solid. The degree of deacetylation of the product measured by acid-base titration was 43%.

[0050] Under Ar protection, prepare 0.1g / 10ml above-mentioned chitosan aqueous solution in 100ml three-neck flask. Weigh 0.4263g L-leucine-N-carboxylic ...

Embodiment 3

[0053] Dissolve 4 grams of chitosan in 100ml of deionized water (containing 2.8ml of glacial acetic acid). After all of the solution is dissolved, add 100ml of absolute ethanol and 32ml of pyridine in turn, stir until clear, then add 3.4ml of acetic anhydride, and stir at room temperature for 4 hours. The reaction solution was poured into ethanol and filtered with suction to obtain a white precipitate. Dissolve the crude product with an appropriate amount of deionized water, centrifuge to remove insoluble matter, add 200ml of absolute ethanol to the filtrate, discard the supernatant after centrifugation, wash the precipitate with acetone and anhydrous ether in turn, and dry it in vacuum at room temperature for 24 hours to obtain a white flocculent solid. The degree of deacetylation of the product measured by acid-base titration was 50%.

[0054] Under Ar protection, prepare 0.1g / 10ml above-mentioned chitosan aqueous solution in 100ml three-neck flask. Weigh 1.3382g N ε -Ben...

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Abstract

The present invention discloses one kind of glycopeptides conjugate microsphere or microcapsule and its preparation process. The glycopeptides conjugate microsphere or microcapsule has polysaccharide to form the glycosyl part of the glycopeptides conjugate and polypeptide to form the peptide chain part of the glycopeptides conjugate, and the polysaccharide and the polypeptide are connected in covalent bond form. The preparation process includes the first preparation of water soluble chitosan, and the subsequent initiating the ring-opening polymerization of several kinds of amino acid and carboxylic acid inner anhybride monomers by means of the nucleophilicity of the amino group in chitosan to form polysaccharide with chitosan as main chain and peptide chain segment grafted to the side chain and the glycopeptides conjugate with polysaccharide and polypeptide connected via covalent bond. Microsphere or microcapsule may be formed with the amphiphilic chitosan for medicinal use.

Description

technical field [0001] The invention relates to a glycopeptide conjugate microsphere or microcapsule and a preparation method thereof through interfacial polymerization. Background technique [0002] As a new type of controlled / sustained-release drug delivery system, microspheres or microcapsules have the advantages of protecting drugs from damage, controlling drug release speed, prolonging drug action time, reducing adverse drug reactions and reducing dosage. received great attention. In clinical treatment, microspheres are passive targeting agents, which can be endocytosed by the reticuloendothelial system (RES) of organ tissues or fused by cells, concentrate in the target area and gradually diffuse to release drugs or be degraded by enzymes in lysosomes to release the drug. At present, research on the controlled release behavior of microspheres has been carried out quite extensively. Among them, controlled / sustained-release research on drugs such as antibiotics, contra...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K9/16A61K9/50A61K9/52A61K47/36
Inventor 刘昌胜王靖
Owner EAST CHINA UNIV OF SCI & TECH
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