PEGylation modified amifostine as well as preparation method and use of PEGylation modified amifostine

A technology for pegylated amifostine and polyethylene glycol, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problem of short action time, large side effects, and metabolic wait for the question
CN104693433AActive Publication Date: 2015-06-10THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
Publication Date
2015-06-10

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Abstract

The invention provides a PEGylation modified amifostine as well as a preparation method and use of the PEGylation modified amifostine. The polymer is of a structure formed by connecting the micromolecular medicine amifostine with polyethylene glycol (PEG) by use of a covalent bond, wherein the amino on the amifostine is in covalent linkage with the long chain of a PEG derivative by use of an amido bond. The invention also provides a preparation method of the PEGylation modified amifostine. The PEGylation modified amifostine also has an enhanced oxidation effect at the cellular level.
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Description

Technical field

[0001] The present invention belongs to the field of pharmaceutical preparations. Specifically, the present invention relates to a pegylated amifostine and a preparation method thereof. The present invention also relates to the use of the pegylated amifostine in the preparation of drugs for the treatment of anti-oxidative damage. use. Background technique

[0002] Amifostine (Formula I) is a small molecule prodrug. In cancer treatment, after amifostine enters the body, the thiophosphate structure at one end can be dephosphorylated by alkaline phosphatase in normal tissues to generate active metabolites with free sulfhydryl groups, which can be eliminated by radiotherapy. And the oxidative free radical (ROS) component caused by chemotherapy can effectively resist the oxidative damage of ROS to tissues. The distribution and pH of alkaline phosphatase in tumor tissues are lower than those in normal tissues, resulting in lower alkaline phosphatase activity than norm...

Claims

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