Polyamino acid, preparation method thereof and drug-loaded gel

A polyamino acid and amino acid technology, applied in the field of polymers, can solve the problems of poor water solubility, fast metabolism, and low drug utilization, and achieve good biocompatibility

Inactive Publication Date: 2018-07-13
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In recent years, there have been new anti-tumor drugs, and the treatment plan has been continuously improved. However, there are many problems in the application of small-molecule anti-tumor drugs used in clinical practice, such as poor water solubility, fast metabolism, and drug utilization. Low, more toxic and side effects on normal tissue cells, some tumors are prone to drug resistance during chemotherapy, and the dose of chemotherapy drugs must be increased to achieve the purpose of treatment

Method used

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  • Polyamino acid, preparation method thereof and drug-loaded gel
  • Polyamino acid, preparation method thereof and drug-loaded gel
  • Polyamino acid, preparation method thereof and drug-loaded gel

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preparation example Construction

[0045] The present invention provides a method for preparing polyamino acid described in formula (I), comprising:

[0046] Reaction of amino-terminated polyethylene glycol monomethyl ether with the structure of formula (III) and amino acid-N-internal carboxylic acid anhydride in a solvent to obtain polyamino acid; the amino acid-N-internal carboxylic acid anhydride is glycine-N-internal carboxylic acid anhydride anhydride, valine-N-endocarboxylic anhydride, leucine-N-endocarboxylic anhydride or alanine-N-endocarboxylic anhydride;

[0047]

[0048] Among them, -R 1 -H and -R 2 for -H,

[0049] or, -R 1 for -CH 3 and-R 2 for -CH 3 ;

[0050] 50≤i≤200, 3≤j≤30;

[0051] In formula (III), 50≤i≤200.

[0052] In an organic solvent, the amino-terminated polyethylene glycol monomethyl ether is respectively mixed with glycine-N-endocarboxylic anhydride, valine-N-endocarboxylic anhydride, alanine-N-endocarboxylic anhydride, leucine-N - Internal carboxylic acid anhydride re...

Embodiment 1

[0110] Put 20g of polyethylene glycol monomethyl ether with a number average molecular weight of 2000 into a dry reaction bottle, then vacuumize it at 120°C for 2 hours while stirring, put the reaction bottle in an oil bath, and when the temperature is 60°C 10g of anhydrous magnesium sulfate and 200mL of dichloromethane were added to the reaction flask respectively, and 5mL of triethylamine and 30mL of methanesulfonyl chloride were added to the reaction flask in an ice-water bath. React for 72 hours under the condition of agitator stirring. After the reaction, the obtained reaction product was washed five times with saturated sodium chloride solution, and then dried overnight by adding anhydrous magnesium sulfate; After drying under vacuum for 24h, an intermediate product was obtained;

[0111]Dissolve the intermediate product and ammonium chloride with the same quality as the intermediate product in ammonia water, the volume of ammonia water is 10 times the mass of the interm...

Embodiment 2

[0119] Put 20g of polyethylene glycol monomethyl ether with a number-average molecular weight of 4000 into a dry reaction bottle, then vacuumize it at 120°C for 2 hours while stirring, put the reaction bottle in an oil bath, and when the temperature is 60°C , add 10g of anhydrous magnesium sulfate, 200mL of dichloromethane dehydrated into the reaction flask respectively, add 2.5mL of triethylamine and 15mL of methanesulfonyl chloride into the reaction flask under the condition of ice-water bath, at 25°C 1. Reaction 72h under stirring bar stirring condition, after the reaction finishes, the reaction product obtained is washed five times with saturated sodium chloride solution and then dried overnight by adding anhydrous magnesium sulfate; the product after drying is settled with anhydrous ether, and the After vacuum drying at ℃ for 24h, an intermediate product was obtained;

[0120] Dissolve the intermediate product and ammonium chloride with the same quality as the intermediat...

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Abstract

The invention provides polyamino acid, which has a structure shown in a formula (I). Aminated methoxypolyethylene glycol is used as an initiator for initiating glycine-N-carboxyl anhydride, alanine-N-carboxyl anhydride, leucine-N-carboxyl anhydride or valine-N-carboxyl anhydride for polymerization, so that four polyamino acid-polyethylene glycol-polyamino acid triblock copolymers containing different side chain alkyl groups (H, CH3<->, (CH3)2CHCH2<->and (CH3)2CH<->) can be prepared. The application also provides drug-loaded gel which is prepared from the polyamino acid and an antitumor drug loaded on the polyamino acid. The drug-loaded gel provided by the application is prepared from the polyamino acid, thus having low toxicity and good temperature sensibility.

Description

technical field [0001] The invention relates to the technical field of polymers, in particular to a polyamino acid, its preparation method and drug-loaded gel. Background technique [0002] Malignant tumors have become one of the most serious diseases threatening human beings. According to the report of the World Health Organization, malignant tumors have become the first cause of human death worldwide since 2010, accounting for more than 20% of all deaths. my country is the second highest incidence area of ​​malignant tumors outside of North America. In recent years, there have been new anti-tumor drugs, and the treatment plan has been continuously improved. However, there are many problems in the application of small-molecule anti-tumor drugs used in clinical practice, such as poor water solubility, fast metabolism, and drug utilization. Low, the toxicity to normal tissue cells is relatively large, and some tumors are prone to drug resistance during chemotherapy, so the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/40A61K9/06A61K47/34A61K45/00A61P35/00A61K31/704
CPCA61K9/0009A61K9/06A61K31/704A61K45/00A61K47/34C08G69/40
Inventor 丁建勋韩建东陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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