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High-molecular mPEG-PLGA-mPEG accessory medicine for medicine use, prepu. method and application thereof

A technology of polymers and excipients, applied in the field of amphiphilic tri-block copolymers, can solve the problems of difficult acquisition of synthetic raw materials and harsh conditions for the synthesis of choline phospholipids

Inactive Publication Date: 2004-10-20
四川大学华西药学院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the synthesis conditions of choline phospholipids with anticoagulant structure are very harsh, which is difficult for general laboratories to meet, and the synthetic raw materials are also very difficult to obtain

Method used

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  • High-molecular mPEG-PLGA-mPEG accessory medicine for medicine use, prepu. method and application thereof
  • High-molecular mPEG-PLGA-mPEG accessory medicine for medicine use, prepu. method and application thereof
  • High-molecular mPEG-PLGA-mPEG accessory medicine for medicine use, prepu. method and application thereof

Examples

Experimental program
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Embodiment 1

[0028] Get lactide (LA), glycolide (GA) with a molar ratio of 4:1 and 10% polyethylene glycol (mPEG) accounting for the total weight and mix them in a sealed container, add 0.05% stannous octoate Catalyst, sealed tube under vacuum. After reacting at 150°C for 8 hours, the sealed tube was opened to dissolve the product, filtered and slowly added dropwise to methanol for precipitation under stirring conditions, and the precipitated product was vacuum-dried at room temperature to constant weight to obtain the PELGA material. Take a certain amount of prepared PELGA and place it in a two-neck bottle, add a certain amount of toluene, after the material is dissolved, slowly add 10% diisocyanate dropwise, slowly raise the temperature to 80°C and react for 12 hours, then raise the temperature to 115°C to reflux After 6 hours, after the toluene was dried by rotary evaporation, the dissolved product was slowly added dropwise to methanol for precipitation under stirring conditions, and th...

Embodiment 2

[0030]Take a certain amount of poly(lactic-co-glycolic acid) (PLGA) (where LA:GA is 70:30) mixed with polyethylene glycol and placed in a fusion-sealed container, add 0.03% stannous octoate, and seal in a vacuum state. Tube. After reacting at 160°C for 10 hours, the sealed tube was opened to dissolve the product, filtered and slowly added dropwise to excess ether to precipitate under stirring conditions, and the precipitated product was vacuum-dried at room temperature to constant weight to obtain the PELGA material. Take a certain amount of prepared PELGA and place it in a two-necked bottle, add a certain amount of toluene, after the material is dissolved, slowly add 7% diisocyanate, slowly raise the temperature to 70°C and react for 10 hours, then heat up to 110°C and reflux for 10 hours hours, after rotary evaporation to dry the toluene, dissolve the product, and slowly add it dropwise to 10-30 parts of diethyl ether to precipitate under stirring conditions, and vacuum-dry ...

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Abstract

A high-molecular mPEG-PLGA-mPEG (PELGE) used as the axcessory of injection, oral-applied medicine, and the water-soluble medicine or the medicine difficult to dissolve in water is an amphipathic three-block copolymer, which is prepared from stannous octoate as catalyst, diisocyanate as coupling agent, polyethene glycol with single terminated end, glycollide, and lactide or polylactic acid-glycollic acid copolymer.

Description

technical field [0001] The invention relates to a medical polymer mPEG-PLGA-mPEG auxiliary material, a preparation method and an application, which belongs to an amphiphilic triblock copolymer. technical background [0002] General biodegradable polymer nanoparticle carrier materials include natural and synthetic types, serum albumin, hemoglobin, collagen, gelatin, dextran, albumin, chitin and its derivatives, lecithin, cholesterol Natural biodegradable polymer materials such as biocompatibility are good, but the preparation is difficult, the cost is high, the quality cannot be controlled, and it cannot be produced on a large scale. Therefore, people have turned their attention to synthetic biodegradable polymers that are easier to obtain. Synthetic biodegradable polymers used for drug carriers mainly include polylactic acid (PLA), lactic acid-glycolic acid copolymer (PLGA), polyacrylates, etc. As degradable synthetic polymer materials, PLA and PLGA have...

Claims

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Application Information

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IPC IPC(8): A61K47/34C08G81/00
Inventor 张志荣段友容
Owner 四川大学华西药学院
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