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Polyesthylene glycol modified zidovudine conjugate and its prepn process and application

A technology of polyethylene glycol and zidovudine, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. question

Inactive Publication Date: 2007-11-07
江西润泽药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And it is very easy to produce drug resistance when used alone
[0006] The above and these problems of AZT have a lot to do with its short half-life, which requires multiple and high-dose administration. The current clinical treatment dose is generally 200mg, given once every 4 hours. Such frequent large-dose administration will inevitably increase the weight of the drug. Toxic side effects, and will induce mutations in different amino acids in RT, resulting in drug-resistant strains
And if the half-life of AZT can be extended, the dose and frequency of use of the drug can be reduced, which can reduce the probability of toxic side effects, and the probability of mutations of different amino acids in RT induced by low doses of drugs will also be greatly reduced.

Method used

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  • Polyesthylene glycol modified zidovudine conjugate and its prepn process and application
  • Polyesthylene glycol modified zidovudine conjugate and its prepn process and application
  • Polyesthylene glycol modified zidovudine conjugate and its prepn process and application

Examples

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Effect test

Embodiment 1

[0034] Example 1: Preparation of monomethoxy polyethylene glycol 2000 zidovudine conjugated prodrug

[0035] Put 1g mPEG2000 (0.5mmol) in a 50ml round-bottom flask, add 20ml of toluene, install the upper separator and steam out 10ml of toluene, then add 0.5g (5mmol) succinic anhydride to the round-bottom flask, continue heating and reflux for 5h , TLC detection (I 2 dyeing), after the reaction is completed, toluene is evaporated under reduced pressure, the solid is dissolved with 5 mL of dichloromethane and filtered, and 50 times the volume of glacial ether is added to the filtrate to obtain a white precipitate, which is monomethoxypolyethylene glycol succinic acid Monoester (mPEG-SA), 1.02 g was obtained, and the yield was 97.1%.

[0036] Add 0.134g (0.5mmol) of AZT, 0.015g (0.125mmol) of DMAP and 0.233g (1mmol) of DCC into a 50ml round bottom flask, add 5ml of dichloromethane and stir until dissolved, and dropwise add 5ml of 1.05g (0.5 mmol) mPEG-SA dichloromethane solutio...

Embodiment 2

[0042] Example 2: Preparation of monomethoxy polyethylene glycol 6000 zidovudine conjugated prodrug

[0043] Put 3g of mPEG6000 (0.5mmol) in a 50ml round bottom flask, add 20ml of toluene, install the upper water separator and steam out 10ml of toluene, then add 0.5g (5mmol) of succinic anhydride to the round bottom flask, continue heating and reflux for 5h , TLC detection (I 2 dyeing), after the reaction is completed, toluene is evaporated under reduced pressure, the solid is dissolved with 5 mL of dichloromethane and filtered, and 55 times the volume of glacial ether is added to the filtrate to obtain a white precipitate, which is monomethoxypolyethylene glycol succinic acid Monoester (mPEG-SA). Obtained 3.01 g, yield 98.7%.

[0044] Add 0.134g (0.5mmol) of AZT, 0.015g (0.125mmol) of DMAP and 0.233g (1mmol) of DCC into a 50ml round bottom flask, add 5ml of dichloromethane and stir until dissolved, and dropwise add 5ml of 3.05g (0.5 mmol) mPEG-SA dichloromethane solution. ...

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Abstract

The present invention relates to one kind of polyethylene glycol modified zidovudine conjugate and its preparation process and application. The polyethylene glycol modified zidovudine conjugate with the structure as shown is prepared through dissolving zidovudine, p-dimethyl aminopyridine and dicyclohexyl carbon diimide in proper amount of dichloromethane, dropping equi-molar ratio dichloromethane solution of mPEG-SA to react, filtering, adding cold ether in 45-55 times volume into the filtrate to obtain white precipitate, filtering to separate the precipitate, and drying to obtain precursor methoxy polyethylene glycol zidovudine conjugate for preparing anti-AIDS medicine.

Description

technical field [0001] The invention relates to an anti-AIDS drug and a preparation method, in particular to the polyethylene glycol conjugated prodrug structure, preparation method and application of zidovudine, and belongs to the technical field of anti-AIDS drug prodrugs. Background technique [0002] AIDS (acquiredimmuneficiency syndrome, AIDS) caused by human immunodeficiency virus (human immunodeficiency virus, HIV) is an infectious disease that seriously affects human health. Since the first case of AIDS was discovered in 1981, more than 25 million people around the world have died from this disease known as the "plague of the century". In some countries, AIDS has even become one of the "four major killers" that endanger public health. Its spread not only threatens the life safety of individuals, but also brings serious social problems. Although highly active antiretroviral therapy (HAART), which is widely used in clinical practice, can effectively prolong the survi...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/7072A61P31/18A61K47/60
Inventor 刘新泳常昱
Owner 江西润泽药业有限公司
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