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A kind of nanoparticle of insoluble drug and its preparation method and application

A technology of insoluble drugs and nanoparticles, applied in application, nanotechnology, pharmaceutical formulations, etc., can solve problems such as poor solubility and low bioavailability, and achieve the effects of improved solubility, good application prospects, and nano-drug purity.

Active Publication Date: 2020-07-10
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Flavonoids include quercetin, apigenin and other polyphenolic compounds, which have many biological activities such as anti-oxidation, anti-inflammation, anti-tumor and anti-fibrosis, but their bioavailability is low due to their poor solubility in water

Method used

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  • A kind of nanoparticle of insoluble drug and its preparation method and application
  • A kind of nanoparticle of insoluble drug and its preparation method and application
  • A kind of nanoparticle of insoluble drug and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0024] This example provides a kind of insoluble drug nanoparticles. The specific preparation method is: weigh 500mg of quercetin and 10mg of polyvinylpyrrolidone, mix them thoroughly in a mortar, and compress them on an infrared tablet machine. The target is placed in 10 mL of pure water, a laser with an energy of 30 mJ is focused on the sheet-shaped target, and ablated for 30 min under magnetic stirring at a rotational speed of 1000 rpm to obtain the final product.

[0025] figure 1 The TEM image of the quercetin nano drug particles prepared in this example. figure 1 The particle size of the quercetin nano-medicine particles in the drug is 50-100nm, uniform in size and good in dispersibility.

[0026] A. The solubility of the obtained nanoparticles was detected according to the following method: different concentrations of quercetin powder (2, 4, 8, 16, 32 μg / mL) were dissolved in DMSO, and a standard curve was obtained by UV quantification. The quercetin powder and the na...

Embodiment 2

[0032] This example provides a poorly soluble drug nanoparticle. Compared with Example 1, the only difference is that the dosage of polyvinylpyrrolidone is 25 mg, and the ablation time is 10 minutes.

[0033] image 3 SEM image of the nanoparticles prepared in this example. It can be seen from the figure that the uniformity of particle size and shape is better, but due to the coating of a large number of polymer materials, the yield of nano drug particles is significantly reduced.

[0034] According to the same method as in Example 1, the solubility and dissolution rate of the product obtained in this example were evaluated. As can be seen from the results, drug solubility and dissolution rate have no significant change compared with Example 1.

Embodiment 3

[0036] This example provides a poorly soluble drug nanoparticle. Compared with Example 1, the difference is only that: the amount of polyvinylpyrrolidone is 5 mg; and the laser power is 50 mJ, and the ablation time is 20 min.

[0037] Figure 4 SEM image of the nanoparticles prepared in this example. It can be seen from the figure that due to the high energy of laser ablation, when the polymer material is 5 mg, the large amount of nano drug particles cannot be effectively coated, resulting in the formation of rod-shaped drug particles.

[0038] According to the same method as in Example 1, the solubility and dissolution rate of the product obtained in this example were evaluated. As can be seen from the results, the solubility and dissolution rate of the product of this embodiment are slightly worse than those of Example 1.

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Abstract

The invention relates to a preparation method of nanoparticles of an indissolvable drug. The method comprises steps as follows: the indissolvable drug and a medical polymer material are mixed and pressed into tablets, and a tablet target material is immersed in water; laser is focused on the tablet target material, ablation is performed under the condition of magnetic stirring, and the nanoparticles can be obtained. According to the provided method, the preparation process is simple and easy to operate, the prepared nano drug is pure and has no chemical residues, the dissolubility and the drugdissolution in water are notably improved, the bioavailability is remarkably enhanced and the nanoparticles have good application prospects.

Description

technical field [0001] The invention belongs to the field of preparation of novel nano-medicines, and relates to a preparation method of insoluble drug nano-particles. Background technique [0002] Insoluble drugs often have problems such as poor solubility, low dissolution rate, slow dissolution rate, and incomplete absorption in the digestive juice of the gastrointestinal tract, which affect their curative effect and greatly limit their application. Increasing the solubility and dissolution rate of poorly soluble drugs and improving their bioavailability are important contents of pharmaceutical research. [0003] Flavonoids include quercetin, apigenin and other polyphenolic compounds, which have many biological activities such as anti-oxidation, anti-inflammation, anti-tumor and anti-fibrosis, but their bioavailability is low due to their poor solubility in water . [0004] In recent years, the application of nanotechnology in the field of pharmacy has been paid more and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K45/00A61K47/32A61K47/10A61K47/34A23P10/22B82Y5/00
CPCA23P10/22A61K9/146A61K45/00B82Y5/00
Inventor 杨蓉韩秋森王新环杨琳王琛
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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