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A kind of naringenin nano composition and its preparation method and application

A nano-composition, naringenin technology, applied in the direction of application, drug combination, skin care preparations, etc., can solve the problem of poor skin permeability and retention, low fat solubility and water solubility of naringenin, which limit the wide range of naringenin Application and other issues, to achieve the effects of long residence time, increased drug encapsulation rate, excellent skin permeability and retention

Active Publication Date: 2019-07-09
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, naringenin has the following three disadvantages in application: the one is that the fat-soluble water solubility of naringenin is small and the water dispersibility is poor, and the active ingredient mass percentage content of the usual water-soluble naringenin composition is only 0.05~ 0.4%, naringenin with low content is difficult to achieve the tissue absorption drug effect; the second is that naringenin is easy to oxidize, which reduces the stability of the finished preparation; The existing naringenin carrier has a large particle size, poor skin permeability and retention, which affects bioavailability
These defects seriously limit the wide clinical application of naringenin. At present, there is no preparation product with naringenin as an effective therapeutic ingredient on the market, and the research on naringenin drug delivery system is currently mostly stuck in some traditional oral dosage forms.

Method used

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  • A kind of naringenin nano composition and its preparation method and application
  • A kind of naringenin nano composition and its preparation method and application
  • A kind of naringenin nano composition and its preparation method and application

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preparation example Construction

[0043] The present invention provides the preparation method of the naringenin nano-composition described in above-mentioned scheme, comprises the steps:

[0044] (1) melting solid lipid, liquid lipid and caprylic acid macrogolglyceride to obtain an oil phase;

[0045] (2) mixing naringenin with polyols to obtain a naringenin polyol solution;

[0046] (3) dissolving vitamin E polyethylene glycol succinate in water to obtain an aqueous phase;

[0047] (4) mixing the naringenin polyol solution obtained in the step (2) with the oil phase obtained in the step (1) to obtain a mixed oil phase;

[0048] (5) performing shear emulsification treatment after mixing the mixed oil phase obtained in the step (4) with the water phase obtained in the step (3), to obtain a micron-scale dispersion;

[0049] (6) homogenize the micron-scale dispersion obtained in the step (4) to obtain a naringenin nano composition;

[0050] There is no chronological order limitation between the step (1), step...

Embodiment 1

[0064] Melt 2.0% lauric acid, 4.5% phospholipids, 2.0% caprylic capric triglyceride, and 1.0% polyethylene glycol caprylic capric glyceride in a water bath at 70°C to obtain an oil phase for later use;

[0065] Add 2.0% naringenin to 14% glycerin, and mix evenly in a water bath at 70°C to obtain a naringenin alcohol solution for later use;

[0066] Add 2.0% vitamin E polyethylene glycol succinate to 72.5% purified water, stir and dissolve in a water bath at 70°C to obtain an aqueous phase, and set aside;

[0067] Add the naringenin alcohol solution dropwise to the oil phase at a rate of 3 drops / second, and stir evenly to obtain a mixed oil phase;

[0068] Then add the above-mentioned mixed oil phase to the water phase at a speed of 5 drops / second, and control the stirring rate to 500r / min during the dropping process. After the mixing is completed, high-speed shear emulsification is carried out at a speed of 5000rpm for 6min to obtain micron-sized Dispersions;

[0069] The mi...

Embodiment 2

[0072] Melt 6.5% stearic acid, 2.0% cholesterol, 4.0% diethyl sebacate, and 1.5% caprylic capric acid macrogolglyceride in a water bath at 80°C, and mix them uniformly to obtain an oil phase, which is set aside;

[0073] Add 4.5% naringenin to 45.0% 1,2-propanediol, mix evenly at 80°C to obtain a naringenin alcohol solution, and set aside;

[0074] Add 1.5% vitamin E polyethylene glycol succinate to 35.0% purified water, stir and dissolve in a water bath at 80°C to obtain an aqueous phase, and set aside;

[0075] Add the prepared naringenin alcohol solution dropwise into the oil phase at a rate of 2 drops / second, and stir evenly to obtain a mixed oil phase;

[0076] Add the mixed oil phase to the water phase at a rate of 3 drops / second, and control the stirring rate at 600r / min during the dropping process. After the mixing is completed, high-speed shear emulsification at 7000rpm for 6min to make a micron-sized dispersion ;

[0077]The micron-scale dispersion is subjected to ...

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Abstract

The invention provides a naringenin nano composition, which comprises the following components by weight: 0.05%-6% of naringenin, 2.0%-15.0% of solid lipid, 1.0-10.0% of liquid lipid, 0.1%-5.0% capric polyethylene glycol glyceride, 0.1%-5.0% of vitamin E polydiethylene glycol succinate, 1.0%-45.0% of polyol and the balance of water. The naringenin nano composition has large drug loading, can promote permeation of naringenin through the skin, has the advantages of high concentration staying for a long time, quick skin absorption, good biocompatibility, wide application range, and good stability and security. The preparation method is simple, easy to control, and suitable for industrial production.

Description

technical field [0001] The present invention relates to the technical field of a pharmaceutical composition, in particular to a naringenin nano composition and its preparation method and application. Background technique [0002] Naringenin is derived from citrus plants of Rutaceae. It is obtained from the hydrolysis of naringin. It belongs to dihydroflavonoids. In recent years, there have been many studies on the pharmacodynamics, pharmacological effects and mechanisms of naringenin at home and abroad. Naringenin has strong biological activities in reducing blood fat, sedation, anti-oxidation, anti-tumor, anti-fungal, anti-atherosclerosis, and anti-ultraviolet radiation damage repair. [0003] However, naringenin has the following three disadvantages in application: the one is that the fat-soluble water solubility of naringenin is small and the water dispersibility is poor, and the active ingredient mass percentage content of the usual water-soluble naringenin composition i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K47/22A61K8/49A61K8/86A23L33/105A23L33/10A61P29/00A61P37/08A61Q17/04A61Q19/00A61Q19/08A61P3/06A61P9/10A61P35/00A61P31/10
CPCA23V2002/00A61K8/498A61K8/86A61K31/352A61K47/14A61K47/22A61Q17/04A61Q19/00A61Q19/08A23V2200/30A23V2200/304A23V2200/308A23V2200/326A23V2200/3262A23V2250/2116
Inventor 刘卫郭凤凤许琦杨祥良
Owner HUAZHONG UNIV OF SCI & TECH
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