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Medicine carrying polymer micelle and preparation method thereof

A drug-loaded polymer and micelle technology, which is used in pharmaceutical formulations, drug delivery, medical preparations with inactive ingredients, etc., can solve the problems of large particle size and large particle dispersion coefficient, and achieve good particle performance and micelles. The effect of stable state and ingestion avoidance

Inactive Publication Date: 2010-07-07
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to provide a drug-loaded polymer micelle in order to overcome the defects of the existing drug-loaded polymer micelle particles with large particle size and large particle dispersion coefficient.

Method used

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  • Medicine carrying polymer micelle and preparation method thereof
  • Medicine carrying polymer micelle and preparation method thereof
  • Medicine carrying polymer micelle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The synthesis of embodiment 1 monomethyl polyethylene glycol polylactic acid block copolymer

[0041] The lactide was recrystallized twice with ethyl acetate, and then dried under reduced pressure for 24 h. Monomethyl polyethylene glycol (MPEG, weight average molecular weight 5000) was dried under reduced pressure at 60° C. for 48 h. Weigh 2g of MPEG, 12g of lactide, and 0.03g of stannous octoate (catalyst) into a round-bottomed flask, add 10ml of toluene, heat up to 60°C, dissolve the reactant, then distill under reduced pressure to remove the toluene, leaving Down the white crystals. Use an oil pump to vacuum the bottle, then seal the flask, adjust the temperature of the oil bath to 150°C, and react for 40 hours. After the end, dissolve the product with 10ml of dichloromethane, and then add 40ml of ether to precipitate it. Repeat twice. , Dry under reduced pressure at 40°C for 40h to obtain the product, weighing 10.2g.

[0042] HNMR hydrogen spectrum was used to de...

Embodiment 2

[0043] The synthesis of embodiment 2 monomethyl polyethylene glycol polylactic acid block copolymers

[0044] The lactide was recrystallized twice with ethyl acetate, and then dried under reduced pressure for 24 h. Monomethyl polyethylene glycol (MPEG, weight average molecular weight 5000) was dried under reduced pressure at 60° C. for 48 h. Weigh 2.5g of MPEG, 10g of lactide, and 0.6g of stannous octoate (catalyst) into a round-bottomed flask, add 10ml of toluene, heat up to 60°C, dissolve the reactants, and then distill under reduced pressure to remove the toluene. White crystals remained. Use an oil pump to vacuum the bottle, then seal the flask, adjust the temperature of the oil bath to 120°C, and react for 50 hours. After the end, dissolve the product with 10ml of dichloromethane, and then add 40ml of ether to precipitate it. Repeat twice. , Dry under reduced pressure at 40°C for 40h to obtain the product, weighing 9.2g.

[0045] The block structure was determined by H...

Embodiment 3

[0046] The synthesis of embodiment 3 monomethyl polyethylene glycol polylactic acid block copolymers

[0047] The lactide was recrystallized twice with ethyl acetate, and then dried under reduced pressure for 24 h. Monomethyl polyethylene glycol (MPEG, weight average molecular weight 5000) was dried under reduced pressure at 60° C. for 48 h. Weigh 2g of MPEG, 16g of lactide, and 0.04g of stannous octoate (catalyst) into a round-bottomed flask, add 10ml of toluene, heat up to 60°C, dissolve the reactant, then distill under reduced pressure to remove the toluene, leaving Down the white crystals. Use an oil pump to vacuum the bottle, then seal the flask, adjust the temperature of the oil bath to 140°C, and react for 30 hours. After the end, dissolve the product with 10ml of dichloromethane, and then add 40ml of ether to precipitate it. Repeat twice. , Dry under reduced pressure at 40°C for 40h to obtain the product, weighing 15.2g.

[0048] The block structure was determined b...

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Abstract

The invention discloses medicine carrying polymer micelle which is methyl polyethylene glycol polylactic acid segmented copolymer micelle carried with hydrophobicity drugs; the grain size is 50-100nm, and the dispersion coefficient PI of the grains is more than or equal to 0.05 and is less than or equal to 0.09; the invention further discloses a preparation method of the medicine carrying polymer micelle; the grain size of the medicine carrying polymer micelle is small, the grain size distribution range is centralized, the stability is good, and the in vitro releasing experiment and the in vitro macrophagocyte cytophagy experiment can reach good effect. The preparation method of the medicine carrying polymer micelle has the following characteristics: the operation is simple and convenient; the encapsulating rate is high, and the highest encapsulating rate can be up to more than 90%; in addition, the prepared medicine carrying polymer micelle has good performance.

Description

technical field [0001] The invention relates to a pharmaceutical preparation technology, in particular to a drug-loaded polymer micelle and a preparation method thereof. Background technique [0002] Many antineoplastic drugs are poorly soluble in water, which makes them difficult to be prepared into suitable formulations. Many methods are often required, such as preparing the drug into a salt, adding a latent solvent, adding a co-solvent, and solubilizing a surfactant, etc. For some drugs with poor water solubility, it is even necessary to take multiple measures at the same time, which often affects the drug. role. For example docetaxel due to its poor water solubility, the existing injection (40g L -1 ) uses Tween-80 (tween-80) as a solvent, and is equipped with a solvent containing 13% ethanol at the same time. Because Tween-80 has hemolytic properties and high viscosity, it brings inconvenience to clinical medication, and it is easy to use in clinical practice. Advers...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34
Inventor 祝林李瑞新战丹
Owner SHANGHAI INST OF PHARMA IND CO LTD
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