Hydrophilic polymer-puerarin specific conjugated non-hemolytic conjugate
A technology of hydrophilic polymers and conjugates, which can be used in drug combinations, organic active ingredients, cardiovascular system diseases, etc., and can solve the problems of reducing the active potency of active ingredients, inapplicability, difficulties in preparation and purification, etc.
Inactive Publication Date: 2010-12-22
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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However, this patent not only describes in general terms, but also fails to scientifically evaluate the efficacy of the final product, water solubility, hemolysis, etc., and more seriously, the conjugation of PEG to puerarin is not specific, or the conjugation is carried out by excessive PEG. All hydroxyl groups on puerarin, or conjugation to carboxyl groups on the flavone sugar ring
The former has many by-products due to various incomplete conjugations, which makes preparation and purification...
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Abstract
The invention relates to a conjugate shown in formula 1 or pharmaceutically acceptable salt thereof. The conjugate has good water solubility, overcomes the defects of poor water solubility, low bioavailability and the like of puerarin, greatly reduces or eliminates the adverse reactions such as puerarin haemolysis and the like, has simple synthesis method and low preparation cost, and is suitable for industrialized production. In addition, the invention also relates to a pharmaceutical composition based on the conjugate, a preparation method and the application in the medicine aspect.Formula 1.
Description
technical field The invention belongs to the field of medicinal chemistry, in particular, the invention relates to a conjugate formed by specifically conjugating biodegradable puerarin and its derivatives with polyethylene glycol through the 7-position phenolic hydroxyl group. In addition, the present application also relates to the pharmaceutical composition based on the conjugate, the preparation method and the application as a medicine. Background technique Puerarin (Puerarin, hereinafter referred to as Pur, chemical name 7,4'-dihydroxy-β-C-D-glucosyl isoflavone) is produced from the roots of leguminous plants Pueraria lobata and Pueraria thomsonii. An extracted isoflavone glycoside, which has the functions of myocardial protection, renal protection, brain tissue protection, anti-oxidation, anti-inflammation, anti-atherosclerosis, anti-arrhythmia, anti-ischemia-reperfusion injury, anti-alcohol central inhibition, anti-cancer It has important pharmacological activities in...
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Login to view more IPC IPC(8): A61K47/48A61K47/34A61K31/7048A61P9/00A61P3/10A61P9/10A61P27/16A61K47/60
Inventor 丁志山蒋福升余美荣刘霞李伟平金波高承贤陈铌铍吕圭源
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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