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Nasal nano-preparation puerarin liquid crystal nanoparticle and preparation method thereof

A technology of puerarin and nanoparticles, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problems of poor brain targeting and targeting index Te less than 2%.

Active Publication Date: 2017-09-22
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Animal experiments show that intravenous administration has extremely poor brain targeting, and the targeting index Te is less than 2%.

Method used

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  • Nasal nano-preparation puerarin liquid crystal nanoparticle and preparation method thereof
  • Nasal nano-preparation puerarin liquid crystal nanoparticle and preparation method thereof
  • Nasal nano-preparation puerarin liquid crystal nanoparticle and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0065] The composition and preparation method of the puerarin lipid cubic liquid crystal nanoparticles described in the present embodiment are as follows:

[0066] Raw materials consist of glyceryl monooleate (GMO), poloxamer 407 (F127), 5% glycerin-water solution, puerarin, and the formula consumption of vitamin E acetate is as follows:

[0067] (1) The total amount of the preparation formula is 100g. Take 2g of glyceryl monooleate, 2.13g of poloxamer 407, and 1g of vitamin E acetate, add 100mL of absolute ethanol as a solvent, dissolve in a hot water bath at 55°C, recover the ethanol under reduced pressure, and obtain a uniform oil phase in the form of a uniform film Scattered on the inner wall of the round bottom flask;

[0068] (2) Add glycerin, the penetration enhancer material, into distilled water until mixed and dissolved to obtain 5% glycerin-water, add 0.5 g of puerarin in a hot water bath to dissolve and add to 100 g;

[0069] (3) Add the water phase to the oil ph...

Embodiment 2

[0072] Raw materials consist of glyceryl monooleate (GMO), poloxamer 407 (F127), 5% glycerin-water solution, puerarin, and the formula consumption of vitamin E acetate is as follows:

[0073] (1) The total amount of the preparation formula is 100g. Take 4.5g of glyceryl monooleate, 5g of poloxamer 407, and 1g of vitamin E acetate, add 100mL of absolute ethanol as a solvent, dissolve in a hot water bath at 55°C, recover the ethanol under reduced pressure, and obtain a uniform oil phase in the form of a uniform film Scattered on the inner wall of the round bottom flask;

[0074] (2) Add glycerin, the penetration enhancer material, into distilled water until mixed and dissolved to obtain 5% glycerin-water, add 0.3 g of puerarin in a hot water bath to dissolve and add to 100 g;

[0075] (3) Add the water phase to the oil phase, add glass beads, and rotate and mix at 60°C and 70r / min until uniform.

[0076] (4) Ultrasound the above-mentioned liquid probe for 5 min (4 s, 3 s inter...

Embodiment 3

[0078] Raw materials consist of glyceryl monooleate (GMO), poloxamer 407 (F127), 5% glycerin-water solution, puerarin, and the formula consumption of vitamin E acetate is as follows:

[0079] (1) The total amount of the preparation formula is 100g. Take 4.5g of glyceryl monooleate, 1g of poloxamer 407, and 5g of vitamin E acetate, add 100mL of absolute ethanol as a solvent, dissolve in a hot water bath at 55°C, recover the ethanol under reduced pressure, and obtain a uniform oil phase in the form of a uniform film Scattered on the inner wall of the round bottom flask;

[0080] (2) Add glycerin, the penetration enhancer material, into distilled water until mixed and dissolved to obtain 5% glycerin-water, add 0.4 g of puerarin in a hot water bath to dissolve and add to 100 g;

[0081] (3) Add the water phase to the oil phase, add glass beads, and rotate and mix at 60°C and 110r / min until uniform.

[0082] (4) Ultrasonic the above-mentioned liquid probe for 7 minutes (4 s, 3 s ...

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Abstract

The invention provides a nasal drug delivery nano-preparation puerarin liquid crystal nanoparticle and a preparation method thereof. The puerarin liquid crystal nanoparticle comprises the following raw materials: 1-4.5 parts by weight of glycerol monooleate, 1-3 parts by weight of poloxamer 407, 0.2-0.8 part by weight of puerarin, 0.5-2 parts by weight of vitamin E acetate, and the balance 5% glycerin-water. According to the invention, lipid cubic liquid crystal is adopted as the drug carrier to encapsulate puerarin to prepare the puerarin lipid cubic liquid crystal nanoparticle. The puerarin liquid crystal nanoparticle prepared by the method provided by the invention has high encapsulation efficiency, good stability, slower in vitro release than a puerarin aqueous solution, and high cell penetration rate than a puerarin solution, thus proving that liquid crystal nanoparticle is a good drug delivery dosage form for puerarin in treatment of brain diseases.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to puerarin cubic liquid crystal nanoparticles and a preparation method thereof. Background technique [0002] Puerarin is the main active ingredient of Pueraria lobata, a commonly used traditional Chinese medicine. It has definite curative effect in treating ischemic stroke and has a wide range of pharmacological effects. A number of clinical trials have shown that puerarin can effectively reduce the levels of plasma endothelin, homocysteine, and oxidized low-density lipoprotein in stroke patients; it can improve the neurological function of patients and improve the ability of daily life. However, because puerarin is an isoflavone carbon glycoside with low solubility, the absolute bioavailability of oral administration is only 3.77%. Caco-2 and MDCK cell transport experiments further show that its apparent permeability coefficient Papp is only 1×10 -...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/14A61K47/10A61K47/22A61K31/352A61P9/10
CPCA61K9/0043A61K9/1274A61K31/352A61K47/10A61K47/14A61K47/22
Inventor 谭宁李鹏跃陆洋杜守颖
Owner BEIJING UNIV OF CHINESE MEDICINE
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