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Polyester material supported disulfiram nanoparticle and application thereof, pharmaceutical preparation and application thereof

A technology of pharmaceutical preparations and nanoparticles, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and drug combinations, etc., can solve the problem of low loading efficiency, few successful reports, and leakage of nanoparticles. drug and other problems, to achieve the effect of effective loading and ensuring drug stability

Active Publication Date: 2015-12-09
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

However, due to the special molecular structure of disulfiram, the loading efficiency of the usual amphiphilic nanomicelles is very low; due to the compatibility problem, the drug leakage phenomenon of the prepared nanoparticles is also very serious. Little effect on improving the stability of disulfiram
Therefore, although disulfiram has shown great potential in tumor therapy in vitro, there are very few successful reports of disulfiram in vivo in open literature.
The reason is that, so far, there is no effective and stable method for carrying disulfiram at home and abroad.

Method used

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  • Polyester material supported disulfiram nanoparticle and application thereof, pharmaceutical preparation and application thereof
  • Polyester material supported disulfiram nanoparticle and application thereof, pharmaceutical preparation and application thereof
  • Polyester material supported disulfiram nanoparticle and application thereof, pharmaceutical preparation and application thereof

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preparation example Construction

[0043] The preparation of disulfiram nanoparticles described in this application can be prepared by nano-precipitation method or film emulsification method, specifically:

[0044] Mix disulfiram or its derivatives, polyethylene glycol-polyester block copolymer, polycaprolactone and solvent, then mix with water for injection, stir, dialyze organic solvent and filter to obtain disulfiram nanoparticles solution.

[0045] Or prepare the disulfiram composition in the following manner:

[0046] The solution of disulfiram nanoparticles obtained above is mixed with trehalose, and freeze-dried to obtain freeze-dried powder of disulfiram nanoparticles.

[0047] The particle size of the disulfiram composition described in the present application is preferably 20-200 nm, and it is a solution or a dry powder.

[0048] The disulfiram nanoparticles provided by the present invention propose to use a mixed material of polyethylene glycol-polyester block copolymer and poly-caprolactone to wra...

Embodiment 1

[0054] The preparation of embodiment 1 disulfiram nanoparticles

[0055] Take disulfiram 1.0g, polyethylene glycol-polyethylene lactide block copolymer (number average molecular weight: polyethylene glycol 5000Da, polyethylene lactide 2000Da) 3.0g, polycaprolactone (number average molecular weight : 3400Da) 6.0g, dissolved in a mixed solvent of 500mL acetonitrile and DMF (v / v=1 / 1), then added dropwise to 2.0L of water for injection under stirring. After the dropwise addition was completed, stirring was continued for 2 h, and then the organic solvent was dialyzed, filtered, and the solution of disulfiram nanoparticles obtained was collected. like image 3 as shown, image 3 Transmission electron micrographs of disulfiram nanoparticles prepared for this example.

Embodiment 2

[0056] The preparation of embodiment 2 disulfiram nanoparticles freeze-dried powder

[0057] Mix the disulfiram nanoparticle solution prepared in Example 1 with trehalose (the mass of which is the volume of the disulfiram nanoparticle solution×5%), and freeze-dry to obtain a freeze-dried powder of disulfiram nanoparticles.

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Abstract

The invention provides a polyester material supported disulfiram nanoparticle, which is prepared from the following components: 1-20 parts by weight of disulfiram or derivatives thereof, 20-95 parts by weight of a polyethylene glycol-polyester segmented copolymer and 5-80 parts by weight of polycaprolactone. According to the disulfiram nanoparticle designed by the invention, a hydrophobic core, provided by polycaprolactone, is stably encapsulated inside the disulfiram, and the polyethylene glycol-polyester segmented copolymer is modified on the surface, so as to guarantee the solubility and the long-circulation capacity of the disulfiram nanoparticle. The application also provides application of the disulfiram nanoparticle on treating tumors.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a polyester material-loaded disulfiram nanoparticle and its application, a pharmaceutical preparation and its application. Background technique [0002] Disulfiram (disulfiram, DSF), also known as disulfide tetraethylthiuram or disulfiram, its structure is shown in formula Ⅰ. Since disulfiram was first synthesized in 1881, it has been used as a catalyst for rubber vulcanization in the rubber industry. In 1948, Jacobsen et al. in Copenhagen found that disulfiram could cause facial flushing, headache, abdominal pain, sweating, heart palpitations and dyspnea after being absorbed in a small amount. The manifestation is named "disulfiram-like reaction". The mechanism of disulfiram causing this reaction is that it can inhibit the acetaldehyde dehydrogenase (ALDH) in the liver, so that after ethanol is oxidized to acetaldehyde in the body, it cannot continue to oxi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/145A61K47/34A61P35/00
Inventor 汤朝晖宋万通于海洋张瑜陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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