Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Purification method of polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer for injection

A technology of polyethylene glycol monomethyl ether and amphiphilic block, which is applied in the field of medicine and chemical industry, can solve the problems of poor reconstitution stability, slow dissolution and difficult production of polymer micellar freeze-dried preparations, and improve reconstitution Effects of stability, improvement of physical properties, and improvement of solubility

Active Publication Date: 2016-02-10
XINAN PHARMA
View PDF5 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation method has the following disadvantages: 1) the tin content is higher in the product; 2) the product is a white blocky solid with large particle size differences and is slow to dissolve in a solvent; 3) the polymer micelles made from this product are freeze-dried The reconstitution stability of the preparation is poor, and the drug is quickly precipitated from the micelles, which is difficult to meet the requirements of clinical application; 4) The recrystallization solvent ether is flammable and explosive, which makes it difficult to produce the product in a clean GMP workshop, and microbial control cannot be guaranteed , it is difficult to be directly used in the preparation of lyophilized preparations for injection

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Purification method of polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer for injection
  • Purification method of polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer for injection
  • Purification method of polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1, preparation polyethylene glycol monomethyl ether-polylactic acid amphiphilic block copolymer (average molecular weight 4000)

[0021] Polyethylene glycol monomethyl ether (molecular weight 2000) and lactide were vacuum-dried for 12 hours under the conditions of a vacuum degree greater than 0.095MPa and a temperature of 40°C, and set aside; weigh polyethylene glycol monomethyl ether (molecular weight 2000) Add 30g of lactide, 30g of lactide and 0.15ml of stannous octoate into the reaction bottle, repeatedly fill with nitrogen, vacuumize, and then raise the temperature to 140°C for 6 hours; after the reaction is completed, cool to room temperature to obtain polyethylene glycol monomethyl ether -The crude product of polylactic acid amphiphilic block copolymer, recrystallize the crude product with dichloromethane-diethyl ether, filter the product and vacuum-dry it at room temperature for 72 hours to obtain polyethylene glycol monomethyl ether-polylactic acid am...

Embodiment 2

[0022] Embodiment 2, preparation polyethylene glycol monomethyl ether-polylactic acid amphiphilic block copolymer (average molecular weight 3000)

[0023] Polyethylene glycol monomethyl ether (molecular weight 2000) and lactide were vacuum-dried for 12 hours under the conditions of a vacuum degree greater than 0.095MPa and a temperature of 40°C, and set aside; weigh polyethylene glycol monomethyl ether (molecular weight 2000) Add 30g of lactide, 15g of lactide and 0.15ml of stannous octoate into the reaction bottle, repeatedly fill with nitrogen, vacuumize, and then raise the temperature to 140°C for 6 hours; after the reaction is completed, cool to room temperature to obtain polyethylene glycol monomethyl ether -The crude product of polylactic acid amphiphilic block copolymer, recrystallize the crude product with dichloromethane-diethyl ether, filter the product and vacuum-dry it at room temperature for 72 hours to obtain polyethylene glycol monomethyl ether-polylactic acid am...

Embodiment 3

[0024] Embodiment 3: prepare polyethylene glycol monomethyl ether-polylactic acid amphiphilic block copolymer (average molecular weight 6000)

[0025] Polyethylene glycol monomethyl ether (molecular weight 2000) and lactide were vacuum-dried for 12 hours under the conditions of a vacuum degree greater than 0.095MPa and a temperature of 40°C, and set aside; weigh polyethylene glycol monomethyl ether (molecular weight 2000) Add 20g of lactide, 40g of lactide and 0.15ml of stannous octoate into the reaction bottle, repeatedly fill with nitrogen, vacuumize, and then raise the temperature to 140°C for 6 hours; after the reaction is completed, cool to room temperature to obtain polyethylene glycol monomethyl ether -The crude product of polylactic acid amphiphilic block copolymer, recrystallize the crude product with dichloromethane-diethyl ether, filter the product and vacuum-dry it at room temperature for 72 hours to obtain polyethylene glycol monomethyl ether-polylactic acid amphip...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
concentrationaaaaaaaaaa
pore sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a purification method of a polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer for injection. The purification method comprises the following steps: dissolving polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer by water to prepare a water solution, making the water solution go through a strong acid cation exchange resin column to carry out chromatography, eluting the column by water, then filtering the eluent by a microporous filter membrane, sterilizing the eluent, freeze-drying the eluent so as to obtain purified polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer. The provided purification method can reduced the content of tin in polyethylene glycol monomethyl ether-polylactic acid amphiphilic segmented copolymer, and can improve the physical properties and solubility of the segmented copolymer. Moreover, the re-dissolution stability of a polymer micelle freeze-dried preparation, whose auxiliary material is the segmented copolymer, can be improved, the microbes can also be eliminated, and the microbes in the segmented copolymer will not exceed the standard.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and relates to a method for purifying pharmaceutical excipients. Background technique [0002] Solubilizing hydrophobic drugs with surfactants to increase drug water solubility is a conventional technical means in the field of pharmaceutical preparations. For example, docetaxel can be solubilized with polysorbate 80. However, this solubilization method has disadvantages such as high incidence of allergies and poor formulation stability. For example, the oleic acid contained in polysorbate 80 has certain allergies, and patients often need desensitization treatment before using the docetaxel preparation made from it; and when the docetaxel injection is compatible with the infusion, the best It is best to use normal saline, which should be used within 120 minutes after preparation. If it is compatible with 5% glucose solution, it should be used within 60 minutes. [0003] Th...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/90C08G63/664A61K9/51A61K47/34
Inventor 汪现廖祥伟秦少容郭敏贾利军王明辛龙涛郑飞鸣
Owner XINAN PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com