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Methoxypolyethylene glycol-polyester-amino acid modified disordered copolymer as well as preparation method and application thereof

A technology of polyethylene glycol monomethyl ether and amino acids, which is applied in the direction of drug combinations, pharmaceutical formulas, organic active ingredients, etc., can solve the problems of untimely release of drugs, uncertainty of chemical bonds, increased physiological toxicity, etc., and achieve improved stability Safety, good safety, high safety effect

Active Publication Date: 2018-08-10
苏州品焌生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the disadvantage of bonding is that the drug cannot be released in time, and there is also uncertainty in the chemical bond of degradation, which may lead to a certain increase in physiological toxicity and a decrease in drug efficacy in the preparation.

Method used

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  • Methoxypolyethylene glycol-polyester-amino acid modified disordered copolymer as well as preparation method and application thereof
  • Methoxypolyethylene glycol-polyester-amino acid modified disordered copolymer as well as preparation method and application thereof
  • Methoxypolyethylene glycol-polyester-amino acid modified disordered copolymer as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 Preparation of polyethylene glycol monomethyl ether-polylactic acid-poly(glycolic acid-phenylalanine) disordered copolymer (MPEG: MD: DL-LA=10:2:10)

[0052] (1) Synthesis of 3-benzyl-morpholine dione

[0053] Dissolve 16.5g (0.1mol) of phenylalanine with 4mol / L sodium hydroxide aqueous solution until the pH is about 10, control the temperature in an ice-salt bath below 5°C, and add dropwise 16.9g (0.15mol) of chloroacetyl chloride (20ml of Dioxane or diethyl ether), after the dropwise addition, react at room temperature for 1 hour, heat up to 35°C, react for 1 hour, remove the organic solvent by rotary evaporation, adjust the pH to about 2, and extract chloroacetyl-phenylpropanoid with ethyl acetate amino acid, and spin-dried to obtain the first step product, chloroacetyl-phenylalanine, with a yield of about 60%.

[0054] Weigh 24.2g (0.1mol) of chloroacetyl-phenylalanine, dissolve it in DMF to a concentration of 0.1mol / L, slowly add it dropwise to 0.6 times...

Embodiment 2

[0057] Example 2: Preparation of polyethylene glycol monomethyl ether-polylactic acid-poly(glycolic acid-phenylalanine) disordered copolymer (MPEG: MD: DL-LA=10:3:13)

[0058] Synthesis process: add 10 parts of MPEG2000 to the reaction bottle, protect with nitrogen, vacuum dry at 110°C for 1-2 hours, replace with nitrogen, weigh 3 parts of MD monomer into the reaction bottle, remove water for 5-10 minutes, Nitrogen replacement, weigh 13 parts of D,L-LA (dried at 30°C for 48 hours) and add to the reaction flask, nitrogen replacement, add 0.3%wt stannous octoate as catalyst, nitrogen replacement, nitrogen protection, heat up to React at 140°C for 6-8 hours, cool down to about 50°C, dissolve with 0.3 times the volume of dichloromethane, precipitate with 10 times the volume of 0°C anhydrous ice ether, filter with suction, and dry in vacuum for 24 hours to obtain a white loose block Things, get excipients.

Embodiment 3

[0059] Example 3: Preparation of polyethylene glycol monomethyl ether-polylactic acid-poly(glycolic acid-phenylalanine) disordered copolymer (MPEG: MD: DL-LA=10:3:9)

[0060] Synthesis process: add 10 parts of MPEG2000 to the reaction bottle, protect with nitrogen, vacuum dry at 110°C for 1-2 hours, replace with nitrogen, weigh 3 parts of MD monomer into the reaction bottle, remove water for 5-10 minutes, Nitrogen replacement, weigh 9 parts of D,L-LA (dried at 30°C for 48 hours) and add to the reaction flask, nitrogen replacement, add 0.3%wt stannous octoate as catalyst, nitrogen replacement, nitrogen protection, heat up to React at 140°C for 6-8 hours, cool down to about 50°C, dissolve with 0.3 times the volume of dichloromethane, precipitate with 10 times the volume of 0°C anhydrous ice ether, filter with suction, and dry in vacuum for 24 hours to obtain a white loose block Things, get excipients.

[0061] NMR of polyethylene glycol monomethyl ether-polylactic acid-poly(gly...

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Abstract

The invention discloses a methoxypolyethylene glycol-polyester-amino acid modified disordered copolymer. The methoxypolyethylene glycol-polyester-amino acid modified disordered copolymer is characterized in that the copolymer is a segmented copolymer prepared through ring opening polymerization of morpholine diketone or a derivate thereof, lactone and methoxypolyethylene glycols, wherein the massratio of methoxypolyethylene glycol to morpholine diketone to derivate to lactone is 1:(0.01-2.5):(0.01-2.5); the lactone is any one or more of glycolide, lactide, caprolactone, carbonic ester or derivates. The methoxypolyethylene glycol-polyester-amino acid modified disordered copolymer is capable of improving the stability of a drug micelle during preparing a drug micelle carrier and can be realized after being stabilized for a long time under the temperature of 37 DEG C.

Description

technical field [0001] The invention belongs to the field of polymer material synthesis, and in particular relates to a polyethylene glycol monomethyl ether-polyester-amino acid modified disordered copolymer and its preparation method and application. Background technique [0002] Most of the anticancer drugs currently used are small molecules, which have poor selectivity (targeting) to tumors, but are widely distributed in normal tissues, causing serious side effects (such as bone marrow transplantation, hair loss, diarrhea, severe nausea) , poor patient compliance, or even stop treatment or can not adhere to treatment. [0003] In recent years, it has been reported that nanosystems and polymer micelle systems using biodegradable polymers are useful technical systems to improve the solubility of poorly soluble drugs, which can change the in vivo distribution of drugs to reduce adverse side effects, and can provide With improved efficacy, controlled release of the drug to a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/44A61K47/34A61K31/337A61K9/107A61K9/19A61P35/00
CPCA61K9/1075A61K9/19A61K31/337A61K47/34A61P35/00C08G69/44
Inventor 不公告发明人
Owner 苏州品焌生物技术有限公司
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