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Carboxylated mPEG (polyethylene glycol methyl ether)-ICA (icariin) nanoparticle, preparation method and application

A technology of polyethylene glycol monomethyl ether and icariin, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, and medical preparations containing active ingredients, etc., which can solve the problem of poor water solubility and obvious first-pass effect of the liver And other issues

Pending Publication Date: 2019-03-15
HUBEI UNIVERSITY OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Based on this, it is necessary to provide a carboxylated polyethylene glycol monomethyl ether-icariin nanoparticle, preparation method and application for the problems of icariin with obvious liver first-pass effect and poor water solubility

Method used

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  • Carboxylated mPEG (polyethylene glycol methyl ether)-ICA (icariin) nanoparticle, preparation method and application
  • Carboxylated mPEG (polyethylene glycol methyl ether)-ICA (icariin) nanoparticle, preparation method and application
  • Carboxylated mPEG (polyethylene glycol methyl ether)-ICA (icariin) nanoparticle, preparation method and application

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preparation example Construction

[0040] A preparation method of carboxylated polyethylene glycol monomethyl ether-icariin nanoparticles, comprising the following steps:

[0041] Polyethylene glycol monomethyl ether is reacted with succinic anhydride to obtain carboxylated polyethylene glycol monomethyl ether;

[0042] Reaction of carboxylated polyethylene glycol monomethyl ether with icariin to obtain carboxylated polyethylene glycol monomethyl ether-icariin, and make carboxylated polyethylene glycol monomethyl ether-Epimedium Glycoside nanoparticles.

[0043] The preparation process adopts the combination of carboxylated activated polyethylene glycol monomethyl ether and icariin monomer for esterification, and adopts the esterification reaction of mPEG and succinic anhydride to realize the carboxylation of polyethylene glycol monomethyl ether because This method is relatively simple and easy to operate and has a high success rate compared with the other two.

[0044] Further, the step of making carboxylate...

Embodiment

[0055] 1.1 Experimental Instruments

[0056] Electronic balance JA302 (Shanghai Suzhan Measuring Instrument Co., Ltd.); constant temperature heating magnetic stirrer DF-1012 / DF-101S (Zhengzhou Great Wall Science, Industry and Trade Co., Ltd.); constant temperature water bath B-260 (Shanghai Yarong Biochemical Instrument Factory); Rotary evaporator RE52CS-1 (Shanghai Yarong Biochemical Instrument Factory); Circulating water multi-purpose vacuum pump SHB-Ⅲ (Zhengzhou Great Wall Science, Industry and Trade Co., Ltd.); Digital constant temperature magnetic stirrer 78HW-1 (Hangzhou Instrument Motor Co., Ltd.); Electric blast drying oven 101-OA type (Tianjin Telester Instrument Co., Ltd.); vacuum freeze dryer FD-1A-50 (Beijing Boyikang Experimental Instrument Co., Ltd.); ); UV-visible spectrophotometer (Beijing Rabote Instrument Co., Ltd.).

[0057] 1.2 Reagents and reagents

[0058] Reagent name Purity / specification / production batch number (manufacturer): Icariin (95% / 1g / DL070208...

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Abstract

The invention discloses a carboxylated mPEG (polyethylene glycol methyl ether)-ICA (icariin) nanoparticle, a preparation method and an application. The nanoparticle comprises ICA as a hydrophobic endand carboxylated mPEG as a hydrophilic end. In an aqueous solution, the mPEG part is linked to form a hydrophilic shell, ICA is used as a hydrophobic core, and a nano-scale mPEG-ICA polymer microsphere of a spherical core-shell structure is formed spontaneously. According to the carboxylated mPEG-ICA nanoparticle, the water solubility of ICA can be increased, the acting time of medicines in vivo can be prolonged, and the slow release effect can be enhanced.

Description

technical field [0001] The invention relates to the field of nano preparations, in particular to carboxylated polyethylene glycol monomethyl ether-icariin nanoparticles, in particular to a preparation method and application of carboxylated polyethylene glycol monomethyl ether-icariin nanoparticles . Background technique [0002] Ischemic heart disease results from insufficient blood supply to the heart due to the presence of coronary artery disease that blocks blood flow. In 2015, ischemic heart disease (IHD) was the leading cause of death worldwide, according to the top ten causes of death in the world according to the World Health Organization's 2017 Fact Report. Coronary heart disease is the most common cause of myocardial ischemia. At present, the main treatment methods for coronary heart disease include drug therapy and interventional surgery such as coronary artery bypass grafting, coronary angioplasty, etc. Since ischemic heart disease is a chronic disease, long-term...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/60A61K47/69A61K31/7048A61P9/10
CPCA61K47/60A61K47/6935A61P9/10A61K31/7048
Inventor 张秋芳陶晓军何纯莲路伶俐杨珊伊马杰
Owner HUBEI UNIVERSITY OF MEDICINE
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