Drug nanoparticle preparation based on complexing coating and preparation method and application

A technology of nanoparticles and complexes, which is applied in the field of drug nanoparticle preparations based on complex coating, can solve the problems of difficult promotion and high cost, and achieve controllable size and shape, low cost, good shape and Effects with easy size control

Active Publication Date: 2014-07-30
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the introduction of metal Au in this method ha

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  • Drug nanoparticle preparation based on complexing coating and preparation method and application
  • Drug nanoparticle preparation based on complexing coating and preparation method and application
  • Drug nanoparticle preparation based on complexing coating and preparation method and application

Examples

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[0044] Example 1:

[0045] Configure an ethanol solution of paclitaxel with a volume mass concentration of 40 mg / mL, an aqueous solution of tannic acid with a volume mass concentration of 80 mg / mL and FeCl with a volume mass concentration of 20 mg / mL 2 Under ultrasonic conditions, add 1ml of the ethanol solution of paclitaxel to 100ml of water to obtain a dispersion system containing paclitaxel particles; quickly add 1ml of tannic acid aqueous solution (concentration of 80mg / mL) to the dispersion system ) And 1ml volume mass concentration is 20mg / mL FeCl 2 After 30 seconds of continuous ultrasound, a stable paclitaxel nanoparticle solution preparation is obtained; the suspension is centrifuged to obtain paclitaxel nanoparticle powder.

[0046] The particle size distribution of the obtained nanoparticles is as attached figure 1 (a); The Zeta potential of the nanoparticles is -21.7eV (attached figure 2 In a), it shows that it is negatively charged; the scanning electron microscope ph...

Example Embodiment

[0047] Example 2:

[0048] Configure paclitaxel with a volume mass concentration of 2mg / mL in glycerol, a volume mass concentration of 200mg / mL gallic acid in water, and a volume mass concentration of 2mg / mL CuSO 4 Under ultrasonic conditions, add 10ml of the glycerol solution of paclitaxel to 100ml of water to obtain a dispersion system containing paclitaxel particles; quickly add 1ml of gallic acid aqueous solution (concentration of 200mg / mL) to the dispersion system And 1ml volume mass concentration is 2mg / mL CuSO 4 After 5 seconds of continuous ultrasound, a stable paclitaxel nanoparticle solution formulation is obtained;

[0049] The particle size distribution of the obtained nanoparticles is as attached figure 1 (b); The Zeta potential of the measured nanoparticles is -24.3eV (attached figure 2 In b). The scanning electron microscope picture of the obtained nanoparticles is attached image 3 (b).

Example Embodiment

[0050] Example 3:

[0051] Configure an ethanol solution of docetaxel with a volume mass concentration of 2 mg / mL, an aqueous solution of catechol with a volume mass concentration of 80 mg / mL, and an aqueous solution of zinc oxalate with a volume mass concentration of 20 mg / mL; under ultrasonic conditions, 1ml Add the above-mentioned docetaxel ethanol solution to 100ml of water to obtain a dispersion system containing docetaxel particles; quickly add 1ml of catechol aqueous solution (with a concentration of 80mg / mL) and 1ml volume mass concentration to the above dispersion system It is an aqueous solution of 20 mg / mL zinc oxalate; and after continuous ultrasound for 30 seconds, a stable docetaxel nanoparticle solution formulation is obtained;

[0052] The size distribution diagram of the obtained nanoparticles is as attached figure 1 (c).

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Abstract

The invention discloses a drug nanoparticle preparation based on complexing coating, a preparation method and an application. The preparation comprises a complex formed by a poorly-soluble drug, a polyphenol compound, and metal ions; Firstly, a suspension of the poorly-soluble drug particles is obtained by solvent exchange; then with the rapid complexation effect of the polyphenol compound and metal ions, a stable coating layer is formed on the drug particle surfaces, so as to obtain the stable poorly-soluble drug nanoparticle preparation. The invention also discloses a monodisperse nanoparticle preparation of the poorly-soluble drug obtained by the method, and an application thereof. The poorly-soluble drug nanoparticle preparation of the invention is controllable in particle size, uniform in distribution, high in drug loading ratio, and good in stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, relates to the application of nanocarriers in the field of biotechnology, and specifically discloses a drug nanoparticle preparation based on complexation coating, its preparation method and application, and the prepared nanomedicine has a high drug loading capacity and good biological properties. technical background [0002] In recent years, the rapid development of high-throughput screening technology has enabled the development and utilization of a large number of active compounds and drugs. However, more than 40% of the drugs have insoluble problems, and this ratio is as high as more than 60% in the synthetic drugs, which has brought great obstacles to clinical drug delivery. As we all know, the solubility and dissolution rate of microparticle drugs will increase with the increase of surface area, so a large number of patent methods that adopt mechanical grinding and precipitation...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K9/14A61K9/19A61P35/00
Inventor 闫学海沈桂芝陈成军邹千里马光辉
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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