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Method for preparing temperature-sensitive three-segmented copolymer

A copolymer, tri-block technology, used in the field of polymer pharmaceutical materials and medicine

Inactive Publication Date: 2008-04-09
CHONGQING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

while ignoring the study of gel-sol phase transition in drug delivery systems

Method used

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  • Method for preparing temperature-sensitive three-segmented copolymer

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] PEG1000 and PEG1500 (mass ratio 1:1) were dried in a three-necked flask under nitrogen protection at 160°C for 2 hours under stirring, and after adding D,L-lactide and glycolide (molar ratio 3:1) for 30 minutes, the stirring was stopped. Add two drops of stannous diethylhexanoate, and react under nitrogen protection at 150°C for 8 hours. The crude product is dissolved in ice water, and after it is completely dissolved, heat and precipitate at 80°C, remove the supernatant, and repeat three times. After freeze-drying, PLGA-PEG-PLGA is obtained.

Embodiment 1

[0019] The polymer obtained in Example 1 was prepared into an aqueous solution with a mass fraction of 10wt%-25wt%, and the gelation state of the solution was observed every time the temperature increased by 1 °C. And when measuring each specific temperature, the sample remains stable for 20 minutes. A gel is considered to have formed when an aqueous polymer solution remains stagnant for 1 min when inverted in a test tube. Figure 1 is a phase transition diagram for different concentrations of polymers.

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Abstract

The present invention relates to a preparation method of temperature-sensitive triblock polymer (PLGA-PEG-PLGA), which pertains to the field of high polymer medical materials and medical technology. The copolymer makes use of an open-loop copolymerization method, takes the polyethylene glycol (PEG), D, L-lactide, glycolic as the raw materials and is prepared by the polymerization with the involvement of an initiator. The gel-sol phase transition temperature (40 DEG C to 44 DEG C) can meet the requirements on the clinical application of local temperature-oriented drug target, which can not only be higher than the human physiological temperature, but also be in the affordable scope of the human body at the same time. The polymer is the pharmaceutical material, which can be mixed with the drug to prepare the microcapsules, micro-particles, nanoparticles and other preparations, so the present invention has potential application in a local temperature-oriented targeting delivery system.

Description

technical field [0001] The invention belongs to the field of polymer medicinal materials and medical technology, and specifically relates to the preparation of a temperature-sensitive tri-block copolymer and the potential application of the polymer in a local temperature-guided targeted drug delivery system. Background technique [0002] Temperature-sensitive polymers are widely used in drug sustained-release injection drug delivery systems, among which polyethylene glycol-polylactide-glycolide-polyethylene glycol (PEG-PLGA-PEG, U.S. Patent No.6 117 949,) and polylactide-glycolide-polyethylene glycol-polylactide-glycolide (PLGA-PEG-PLGA, U.S. Patent No.6 004 573, Chinese Patent Publication No. 200510046409.8) are researched in recent years Comparing two classes of biodegradable temperature-sensitive triblock polymers. When the temperature is lower than body temperature, this type of polymer material can be directly dissolved in water to form a free-flowing sol, while at bod...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/08C08G63/85C08G65/48A61K47/34
Inventor 李军王伯初王亚洲刘朋周太刚
Owner CHONGQING UNIV
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