Polyethylene glycol modified sterol copolymer and its uses

A polyethylene glycol and copolymer technology, applied in the field of medicine, can solve the problems that it cannot be used as an auxiliary material for injection

Inactive Publication Date: 2007-05-16
张文芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Searching the patents and documents related to the present invention, we found that the invention patent 00110157.9 discloses a compound in which polyethylene glycol and cholesterol are linked by ester bonds with succinic acid. We found that the compound injection has strong hemolytic property and basically cannot be used as Excipients for injection

Method used

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  • Polyethylene glycol modified sterol copolymer and its uses
  • Polyethylene glycol modified sterol copolymer and its uses
  • Polyethylene glycol modified sterol copolymer and its uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Embodiment one (subnanometer emulsion type)

[0089] Prescription 1: paclitaxel 0.01%-3.0%, co-solvent 0.01%-5.0%, phospholipid 0.5%-6.0%, PGC 0.1%-5.0%, triglyceride 5%-30%, glycerin 1.0%-6.0%, Oleic acid 1.0% ~ 6.0%, add water for injection to 100ml.

[0090] Weigh 100-500 mg of paclitaxel, dissolve it in an appropriate amount of co-solvent (absolute ethanol) 1, dissolve it in 15 g of triglyceride and 0.1-5 g of oleic acid, stir at 50 ° C to 80 ° C at high speed to mix evenly, and make an oil phase; Remove ethanol by evaporation; weigh 1.0 g of egg yolk lecithin, 1.0 g of PGC, and 3 g of glycerin, add the prescribed amount of water, stir at 50°C to 80°C at high speed to fully disperse, and make an aqueous phase. Mix the two phases of oil and water, and stir at a high speed at 50°C to 80°C to make colostrum. Take the colostrum, adjust the volume to the prescribed amount with water for injection, adjust the pH value to 5.0-7.0, transfer to the high-pressure homogeni...

Embodiment 2

[0091] Embodiment two (nanometer microemulsion formulation)

[0092] Prescription 1: Doxorubicin 0.01%-2.0%, Adriamycin co-solvent 0.01%-5.0%, PGC 0.1%-5.0%, co-surfactant (absolute ethanol, propylene glycol) appropriate amount, add water for injection to 100ml .

[0093] Weigh 100-500mg of doxorubicin and dissolve it in doxorubicin co-solvent (absolute ethanol), add PGC2.0g, 1.0g of propylene glycol and appropriate amount of water and stir at 20°C-80°C to mix evenly, keep stirring, add appropriate amount of no Titrate with water and ethanol until it becomes a translucent solution, adjust the pH value to 5.0-7.0, sterilize, filter, fill with nitrogen, and sterilize.

Embodiment 3

[0094] Embodiment three (micelle)

[0095] Prescription 1: Nimodipine 0.01%-2.0%, nimodipine co-solvent 0.01%-5.0%, PGC 0.1%-5.0%, polyoxyethylene-polyamino acid copolymer appropriate amount, and water for injection is added to 100ml.

[0096] Dissolve nimodipine, PGC, and polyoxyethylene-polyamino acid copolymer with an appropriate amount of solvent, evaporate the solvent under reduced pressure, add the prescribed amount of aqueous solution, stir evenly, and stir at high speed until the average particle size of the emulsion drops is ≤0.5 microns. After the emulsion is filtered, Nitrogen filled filling, sterilization vested.

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Abstract

The invention discloses a synthesizing method of PGC through grafting PEG on the ChOL at ether bond as surface activator, which can be nanometer emulsion and liposome as well as one of carrier component in the water gel beam and solid liposome nanometer particle or nanometer particle. The invention can be auxiliary material of superior cosmetics, which is injected hypodermally to eliminate wrinkle.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a polyethylene glycol (PEG) modified sterol copolymer and the application of the copolymer as an auxiliary material. Background technique [0002] Polyethylene glycol (PEG) is a mixture of ethylene oxide and water polycondensation, and its molecular weight ranges from 200 to 20,000. [0003] Polyethylene glycol (PEG) is the most commonly used modifier, which has low toxicity, no antigenicity, good amphiphilicity, and biocompatibility has been approved by FDA. It is often used to modify phosphatidylcholine and fatty acids as excipients for the preparation of emulsions or liposomes; polyethylene glycol is also used to modify proteins (also known as protein PEGylation), including physical combinations and chemical combinations of PEG, proteins and polypeptide drugs. Modifications, the advantages brought by PEGylation of drugs to drugs include: increased solubility, red...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00C08G65/06A61K47/34A61K47/08A61K8/86
CPCA61K47/488A61K8/63A61K9/127A61K9/5123A61Q19/08A61K47/34A61K2800/57A61K9/0019A61Q19/00A61K47/14A61K47/44A61K47/48215A61K9/0095A61K9/1075A61K2800/91A61K47/48884C07J9/00A61K47/10A61K47/48815A61K8/86A61K47/60A61K47/6907A61K47/6911A61K47/6929A61K47/549A61K47/28C08G65/3314C08G65/485
Inventor 张文芳
Owner 张文芳
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