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Polyamino acid, a preparation method, and drug loading gel

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

Inactive Publication Date: 2018-05-08
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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, a preparation method, and drug loading gel
  • Polyamino acid, a preparation method, and drug loading gel
  • Polyamino acid, a preparation method, and drug loading gel

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preparation example Construction

[0046] The present application also provides a preparation method of the polyamino acid described in formula (I), including:

[0047] The amino-terminated polyethylene glycol with the structure of formula (IV) is reacted with amino acid-N-internal carboxylic acid anhydride in a solvent to obtain polyamino acid; the amino acid-N-internal carboxylic anhydride is glycine-N-internal carboxylic anhydride, Amino acid-N-endocarboxylic anhydride, leucine-N-endocarboxylic anhydride or alanine-N-endocarboxylic anhydride;

[0048]

[0049] Among them, in formula (I), -R 1 -H and -R 2 for -H,

[0050] or, -R 1 for -CH 3 and-R 2 for -CH 3 ;

[0051] 50≤i≤200, 3≤j≤30.

[0052] In formula (IV), 50≤i≤200.

[0053]In the present invention, in an organic solvent, the amino-terminated polyethylene glycol is respectively mixed with glycine-N-inner carboxylic anhydride, valine-N-inner carboxylic anhydride, alanine-N-inner carboxylic anhydride, leucine-N- Internal carboxylic acid anh...

Embodiment 1

[0111] Put 20 g of polyethylene glycol with a number average molecular weight of 2000 into a dry reaction bottle, then vacuumize it at 120°C for 2 hours while stirring, place the reaction bottle in an oil bath, and when the temperature is 60°C, add Add 10g of anhydrous magnesium sulfate and 200mL of dehydrated dichloromethane to the reaction flask, add 1.25mL of triethylamine and 7.5mL of methanesulfonyl chloride to the reaction flask in an ice-water bath, and stir at 25°C React under sub-stirring conditions for 72 hours. 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 vacuum drying for 24h, an intermediate product was obtained;

[0112] 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 intermediate product, and reac...

Embodiment 2

[0118] Put 20 g of polyethylene glycol with a number-average molecular weight of 4000 into a dry reaction bottle, then vacuumize it at 120°C for 2 hours while stirring, place the reaction bottle in an oil bath, and when the temperature is 60°C, add Add 10g of anhydrous magnesium sulfate and 200mL of dehydrated dichloromethane to the reaction flask, add 1.25mL of triethylamine and 7.5mL of methanesulfonyl chloride to the reaction flask in an ice-water bath, and stir at 25°C React under sub-stirring conditions for 72 hours. 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 vacuum drying for 24h, an intermediate product was obtained;

[0119] 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 intermediate product, and reac...

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Abstract

The invention provides polyamino acid which has a structure shown as a formula (I). Four polyamino acid-polyethylene glycol-polyamino acid triblock copolymers containing different side chain alkyl (H,CH3-, (CH3)2CHCH2-and (CH3)2CH-) are prepared by taking aminated polyethylene glycol as an initiating agent to initiate glycine-N-carboxylic anhydride, alanine-N-carboxylic anhydride, leucine-N-carboxylic anhydride or proline-N-carboxyl anhydride to polymerize. The invention further provides drug loading gel which comprises the polyamino acid and an anti-tumor drug loaded on the polyamino acid; as the drug loading gel provided by the invention comprises the polyamino acid, the drug loading gel has low toxicity and good temperature sensitivity.

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