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Composite pharmaceutical ingredient loaded nanoparticle

A nanoparticle and drug technology, applied in the field of medical materials, can solve problems such as releasing toxins, effectiveness and safety issues, and affecting the efficacy of DES, and achieve the effect of increasing adsorption force and increasing residence time

Inactive Publication Date: 2017-12-08
BEIJING ANZHEN HOSPITAL AFFILIATED TO CAPITAL MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although DES has entered clinical application, there are still some effectiveness and safety issues in DES.
The important defect of DES is that the drug concentration is highest on the struts of the stent, and antiproliferative drugs can inhibit the healing of the endothelium, which is the most important part of the endothelium
On the other hand, the area between the edge of the stent and the struts cannot completely inhibit the formation of neointima, thus affecting the efficacy of DES.
In addition, DES cannot be applied to lesions of small vessels and branch vessels, nor is it suitable for coronary artery bypass grafting.
Some important safety issues are not fully clarified, such as perioperative thrombosis, late stent malapposition, aneurysm formation, edge effects, late inflammatory response caused by polymers selected for binding drugs, release of toxins, etc.

Method used

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Experimental program
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Embodiment 1

[0032] Nano-microspheres loaded with heparin, paclitaxel and fluvastatin were modified with cationic surfactant didodecyldimethylammonium bromide (DMAB) by physical adsorption method to increase their residence in the vascular endothelium. Leave time. The specific preparation method is to use the double emulsification-solvent volatilization method, and the preparation process is shown in figure 1 .

[0033] 1) Preparation of compound drug solution: heparin, paclitaxel, and fluvastatin were dissolved in distilled water, and the mass concentrations of the three drugs were 20% heparin, 15% paclitaxel, and 30% fluvastatin.

[0034] 2) Dissolve an appropriate amount of polylactic acid-glycolic acid copolymer (PLGA 50:50, intrinsic viscosity 1.13dl / g) with a dichloromethane / acetone organic solution with a volume ratio of 1:1.5, with a mass concentration of 50%, and the organic solution contains a mass percentage of 0.05% of Pluronic F68 (Pluronic F68) as emulsifier. Add compound ...

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Abstract

The invention provides a composite pharmaceutical ingredient loaded nanoparticle. The nanoparticle is modified by a cationic surfactant; the nanoparticle is loaded with a composite medicine of heparin, taxol and fluvastatin; and the cationic surfactant is dilauryl dimethyl ammonium bromide. The invention also provides a preparation method and an application of the composite pharmaceutical ingredient loaded nanoparticle. According to the nanoparticle provided by the invention, a polylactic acid-glycolic acid copolymer nano-microsphere which is loaded with the heparin, the taxol and the fluvastatin is adopted, and the nano-microsphere is subjected to surface modification by virtue of the cationic surfactant, namely dilauryl dimethyl bromide, through a physical adsorption method, so that a novel intravascular drug delivery system is formed. The adsorption force of the drug delivery system is enhanced, and the residence time of the system in vascular endothelium is prolonged.

Description

technical field [0001] The invention belongs to the field of medical materials, and in particular relates to a nanometer material loaded with compound medicine and a preparation method thereof. Background technique [0002] With the continuous improvement of people's living standards in our country and the aggravation of population aging, coronary atherosclerotic heart disease has increasingly become a disease that seriously threatens people's lives and health. Coronary artery stent implantation (PCI) and coronary artery bypass grafting (CABG) are two major methods for the treatment of coronary heart disease at present, but the incidence of vascular restenosis after PCI and CABG is as high as 15-60%. Drug-eluting stents (Dmg-eluting stenl, DES) and balloon-catheter-based drug delivery systems are mainly used in the treatment of vascular restenosis. Although DES has entered clinical application, there are still some problems of effectiveness and safety of DES. The important...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/727A61L31/16A61L31/14A61L29/16A61L29/14A61P9/10A61P7/02A61K31/405A61K31/337
CPCA61K31/337A61K31/405A61K31/727A61L29/14A61L29/16A61L31/14A61L31/16A61L2300/216A61L2300/236A61L2300/416A61L2300/45A61L2300/624A61K2300/00
Inventor 于洋于文渊高铭鑫王鹏程唐田
Owner BEIJING ANZHEN HOSPITAL AFFILIATED TO CAPITAL MEDICAL UNIV
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