A kind of flavonoid nano-preparation and preparation method thereof

A nano-formulation and flavonoid technology, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as difficult absorption and utilization, and improve transdermal absorption and oral absorption efficiency. The effect of improving stability and prolonging the validity period

Inactive Publication Date: 2016-09-14
WUHAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the water insolubility of flavonoids, these active ingredients of flavonoids are difficult to be fully absorbed and utilized through oral or transdermal routes no matter in the form of original medicine or compound preparation or flavonoid extract.

Method used

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  • A kind of flavonoid nano-preparation and preparation method thereof
  • A kind of flavonoid nano-preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0022] The preparation process of the flavonoid nano-preparation is as follows:

[0023] Dissolve the flavonoid powder with ethanol and add SDS to make the organic phase; dissolve the chitosan with 2wt% acetic acid, adjust the pH to 5.3-5.4 to make the water phase; add Tween-80 aqueous solution to the water phase, Under stirring, inject the organic phase into the water phase, then add PEG400 aqueous solution and continue stirring for 30-60 minutes, and after standing for defoaming, the suspension is obtained, which is the flavonoid nano-preparation. The average particle size distribution is 300-500nm, belonging to the nanoscale range, and the system is stable. At the same time, due to the antibacterial effect of chitosan, the prepared flavonoid nano-preparation can be placed at room temperature for 3-4 weeks without any treatment, and then freeze-dried or sprayed. After being dried and made into powder, it is easier to store and extend the validity period.

[0024] Optimally,...

Embodiment 1

[0028] (1) Preparation of mulberry flavonoids

[0029] The flavonoids used in this method are extracted from the roots of the tree. Dry and pulverize the root of the tree, according to the ratio of root powder: 75% ethanol = 1g: 9mL, weigh the root powder of the tree and add it to 75% ethanol, soak for 30 minutes, ultrasonic treatment 2 to 3 times, about 20 minutes each time, Filtrate, repeat the treatment of the filter residue once, combine the filtrate, the filtrate is yellow or yellow-green. The filtrate was concentrated under reduced pressure and decolorized with petroleum ether to obtain an orange-red transparent decolorized liquid. The decolorized concentrate was chromatographed with AB-8 macroporous resin, washed with 20% ethanol until colorless, then eluted with 95% ethanol, collected 95% ethanol eluate, concentrated under reduced pressure to obtain yellow Add an appropriate amount of distilled water to the paste, stir slowly, let stand, centrifuge at 5000rpm for 20m...

Embodiment 2

[0047] (1) Preparation of mulberry flavonoids

[0048] This method adopts the flavonoids prepared in Example 1. Rutin (Sigma Company) was used as a standard product, and the flavonoid content determined by the nitrate chromogenic method [Chinese patent medicine, 2006, 28 (10): 1521-1522] was 81.56%.

[0049] (2) Preparation of the solution:

[0050] Weigh 80.0 mg of mulberry flavonoid product (content 81.56%), dissolve it in 20 mL of absolute ethanol, add 0.6 mL of 0.3% SDS solution, and stir until completely dissolved, which is the organic phase;

[0051] Weigh 100.0mg chitosan (deacetylation degree 85%, viscosity average molecular weight 300,000), dissolve in 100mL 2% acetic acid solution, stir on a magnetic stirrer until it becomes a uniform and transparent solution, then add 0.5mol L -1 Adjust the pH value of the NaOH solution to 5.3, which is the water phase;

[0052] PEG400 was dissolved in deionized water to form a 5.0% aqueous solution as an emulsifier.

[0053] Tw...

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Abstract

The invention discloses a paper mulberry flavone nanometer preparation and a preparing method thereof. The preparing method includes: dissolving paper mulberry flavone powder with ethanol, and adding SDS to prepare an organic phase; dissolving chitosan with an acetic acid solution having a concentration of 2 wt% and adjusting the pH to 5.3-5.4 to prepare a water phase; adding an aqueous tween-80 solution into the water phase; injecting the organic phase into the water phase under high-speed stirring; adding an aqueous PEG 400 solution; stirring continuously for 30-60 min; and allowing the mixture to stand and be defoamed to obtain a suspension namely the paper mulberry flavone nanometer preparation. Operations are simple and equipment requirements are low. The main raw materials are natural biomolecules, and are good in biocompatibility, nontoxic, biodegradable, free of in-vivo accumulation, simple, easily available and low in cost. After nanocrystallization, the water solubility of the flavones is improved and the oral absorption efficiency is increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid polymer nano-preparation using natural biological macromolecules as a carrier to wrap water-insoluble traditional Chinese medicine component flavonoids and a preparation method thereof. Background technique [0002] Flavonoids widely exist in various tissues of plants in nature, and are active ingredients of many traditional Chinese medicines. The flavonoid content of mulberry is high, and its pharmacological effects are extensive, and the resources of mulberry are abundant in our country. More than 70 kinds of flavonoids have been isolated from mulberry, and many mulberry flavonoids have shown encouraging biological activities, such as anti-oxidation and free radical scavenging, anti-depression, anti-myocardial ischemia, anti-tumor, anti- Osteoporosis and protection against chemical liver damage, etc., especially antioxidant activity and free radic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K36/60A61K47/36
Inventor 熊燕飞刘东郭海英刘科付博华王艺峰
Owner WUHAN UNIV OF TECH
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