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Combined polymer-medicine micelle and its prepn process

A technology of polymers and drugs, which is applied in the direction of pharmaceutical formulations, drug delivery, and medical preparations of non-active ingredients. convenient effect

Inactive Publication Date: 2003-05-14
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, patents and related literatures have used a single amphiphilic block copolymer or its blend with polylactic acid and polyethylene glycol to load drugs, and the control of drug loading and release levels is mainly by controlling the polymer. The molecular weight, the length and ratio of hydrophobic and hydrophilic blocks can be realized, which makes it difficult to adjust the drug release rate. In order to meet the requirements of different drugs on the loading capacity and release rate, it is necessary to prepare different molecular weights and different hydrophobic / hydrophilic blocks. The proportion of polymers, which not only limits the application range of a molecular weight and structure of block polymers, but also greatly restricts the development of different drug controlled release formulations

Method used

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  • Combined polymer-medicine micelle and its prepn process
  • Combined polymer-medicine micelle and its prepn process
  • Combined polymer-medicine micelle and its prepn process

Examples

Experimental program
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Effect test

preparation example 1

[0029] 17g of 88% L-lactic acid and 15g of polyethylene glycol monomethyl ether (MePE6) with a molecular weight of 2000 were added to a round bottom flask. After sealing, under the protection of nitrogen, water was removed under reduced pressure at 140°C for 2 hours. Then 0.06 g of stannous octoate catalyst was added under normal pressure, and the melt polycondensation reaction was carried out for 8 hours at 200° C., under the pressure of 20 mmHg, and nitrogen flow. After the reaction is over, dissolve the product in chloroform, then add 4 to 10 parts of acetone / ether mixed solution with a volume ratio of 1:4 below 10°C for precipitation, centrifuge, and vacuum dry at 30°C to 50°C to obtain the product PLLA - MePE6 diblock copolymer.

preparation example 2

[0031] Repeat the steps of Preparation Example 1, except that polyethylene glycol (PEG) is used instead of polyethylene glycol monomethyl ether to prepare PLLA-PEG-PLLA.

preparation example 3

[0033] Repeat the steps of Preparation Example 1, replacing L-lactic acid with 85% D, L-lactic acid to obtain a PDLLA-MePEG diblock copolymer.

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Abstract

The present invention provides one kind of combined polymer-medicine micelle to control the release of hydrophobic medicine. The micelle contains two or more kinds of amphiphilic block copolymer and one or more kinds of hydrophobic medicine. The amphiphilic block copolymer includes hydrophilic segment of copolymer of ethanediol or ethylene epoxide and epoxypropane; and hydrophobic segment selected from biodegradable PDLLA, PDLA, PLGA and PCL or their mixture. The micelle exists in the state of water dispersing liquid or freeze dried powder. The combined poloymer-medicine may be prepared via solid phase melting and dispersing process, solvent evaporating process or dialysis process. The present invention makes it possible to control the release of medicine effectively.

Description

technical field [0001] The invention relates to a drug release system combining polymer micelles and a preparation method thereof, which is a micellar system composed of at least two amphiphilic block copolymers and at least one drug, and its freeze-dried powder is easy to redisperse In water, a drug micelle dispersion is formed, and by adjusting the proportion of the copolymer, a drug controlled release system that effectively controls drug release and has a more therapeutic effect can be obtained. Background technique [0002] Biodegradable polymer nanoparticles can realize the targeting and control of drugs, thereby improving the bioavailability of drugs, especially hydrophobic drugs, and enhancing the efficacy. However, polymer nanoparticles with a hydrophobic surface are easily recognized and captured by protein adsorption and reticuloendothelial cells, and the circulation time in the body is short. Therefore, it is very necessary to modify it...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/10A61K9/19A61K47/34
Inventor 董岸杰邓联东
Owner TIANJIN UNIV
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