Hydroxychloroquine amphiphilic polymer drug precursor, preparation method and application thereof

An amphiphilic polymer, hydroxychloroquine technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of poor water solubility of the system, long reaction time, difficult control of drug loading, etc., and reduce the binding capacity. , improve water solubility, improve the effect of pharmacokinetic behavior

Active Publication Date: 2020-01-17
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, the solution to this type of problem is mainly to connect hydroxychloroquine to polyglutamic acid or polysaccharides through chemical reactions, but due to the long reaction time of this type of reaction, and the drug loading is not easy to control, and when the content of hydroxychloroquine is too high , will also lead to poor water solubility of the whole system

Method used

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  • Hydroxychloroquine amphiphilic polymer drug precursor, preparation method and application thereof
  • Hydroxychloroquine amphiphilic polymer drug precursor, preparation method and application thereof
  • Hydroxychloroquine amphiphilic polymer drug precursor, preparation method and application thereof

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Embodiment

[0052] Synthesis of Hydroxychloroquine Amphiphilic Polymer Prodrug:

[0053] In this example, a hydroxychloroquine amphiphilic polymer prodrug with disulfide bonds was synthesized, with a molecular weight of about 10,000 and a uniform molecular weight distribution, wherein the molecular weight of polyethylene glycol monomethyl ether was 5,000.

[0054] 1. Synthesis of polyethylene glycol monomethyl ether chain transfer agent (PEG-PETTC):

[0055] Take 4g polyethylene glycol monomethyl ether (molecular weight 5000, 0.8mmol) and reflux toluene to remove water, spin dry, add 100mL dichloromethane to dissolve, add 5 equivalents of 4-cyano-4-(2-phenylethanesulfide Alkylthiocarbonyl) sulfanyl valeric acid (PETTC) and 0.5 equivalent of 4-dimethylaminopyridine (DMAP), drop 5 equivalents of dicyclohexylcarbodiimide (DCC) dichloromethane under ice bath conditions (DCM) solution, the ice bath was removed after the dropwise addition, and stirred at room temperature for 48 hours. The rea...

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Abstract

The present invention discloses a hydroxychloroquine amphiphilic polymer drug precursor. The hydroxychloroquine amphiphilic polymer drug precursor is composed of hydrophilic polyethylene glycol monomethyl ether and a hydrophobic hydroxychloroquine polymer. The hydroxychloroquine polymer is bonded to the polyethylene glycol monomethyl ether via a cleavable chemical bond. The hydroxychloroquine amphiphilic polymer drug precursor can be self-assembled into nanoparticles with a particle sizeof 20-300 nm in water, which improves pharmacokinetic behaviors of free hydroxychloroquine and enables the hydroxychloroquine amphiphilic polymer drug precursor to have significant long-cycle characteristics. At the same time, the hydroxychloroquine amphiphilic polymer drug precursor nanoparticles can loada variety of hydrophobic drugs, including camptothecin and derivatives thereof, paclitaxel, doxorubicin and bortezomib as well as various types of negatively charged drug molecules, and have a wide range of application values.

Description

technical field [0001] The invention belongs to the field of drug prodrugs and its preparation, and in particular relates to a hydroxychloroquine amphiphilic polymer drug prodrug and its preparation method and application. Background technique [0002] Hydroxychloroquine (as shown in formula A) is a 4-aminoquinoline antimalarial drug, which can be used to treat systemic lupus erythematosus, rheumatoid arthritis and other immune diseases. Hydroxychloroquine is clinically used as oral hydroxychloroquine sulfate, and its pharmacology and mechanism of action are similar to chloroquine, but its toxicity is lower than that of chloroquine. The structural difference between hydroxychloroquine and chloroquine is that the N-ethyl group at the end of the side chain of chloroquine is hydroxylated, so it is named hydroxychloroquine. [0003] [0004] In recent years, more and more studies have found that hydroxychloroquine and chloroquine have various biological and pharmacological a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/60A61K31/4706A61P37/02A61P29/00A61P19/02A61P37/00
CPCA61K31/4706A61K47/6935A61P19/02A61P29/00A61P37/00A61P37/02
Inventor 刘祥瑞王惠芳白皓宇王砾莹唐建斌周珠贤申有青
Owner ZHEJIANG UNIV
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