Erianin nano preparation, and preparation method and application thereof

A nano-formulation, Erianin technology, applied in the directions of pharmaceutical formulations, medical preparations with non-active ingredients, emulsion delivery, etc., can solve the problems of easy stratification, hidden safety hazards, increase the risk of intravenous administration, etc., and achieve a good target. tropic effect

Inactive Publication Date: 2019-06-07
中国人民解放军西部战区总医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The current application of Erianin mainly has the following problems: ①Erianin is a new anti-cancer drug with great potential, but there is currently a lack of a formable preparation for clinical application
② At present, some scholars try to prepare Erianin into an emulsion injection, but this dosage form has poor stability, easy to stratify, flocculate, phase inversion and rancidity, which further increases the risk of intravenous administration, and there are great problems. security risks
At the same time, the drug preparation is not on the market, and there is a lack of corresponding data for clinical application
③The solubility of erianin in the water phase is not high. Some scholars try to form salt compounds of this drug, but the improvement of solubility and bioavailability is not obvious

Method used

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  • Erianin nano preparation, and preparation method and application thereof
  • Erianin nano preparation, and preparation method and application thereof
  • Erianin nano preparation, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 proposes a kind of erianin nano preparation, comprises the raw material of following parts by weight: 15 parts of erianin monomers, 30 parts of glyceryl monostearate, 70 parts of lecithin, 20 parts of dehydrated alcohol and spit 45 parts of temperature-80 aqueous solution. The mass concentration of the Tween-80 aqueous solution is 0.5%-1%.

[0031] The method for the erianin nano-preparation of embodiment 1, comprises the steps:

[0032] (1) Dissolve Tween-80 in distilled water to fully dissolve, and then heat to 73°C to obtain an aqueous phase.

[0033] (2) The glyceryl monostearate, the lecithin and the erianin monomer were dissolved in 18 mL of absolute ethanol, and heated to 73° C. to obtain an oil phase.

[0034] (3) Stir the water phase at a rotating speed of 1000r / min and add the oil phase dropwise into the water phase with a skin test syringe for emulsification until the mixture is concentrated into 13 mL of nanoemulsion.

[0035] (4) The nanoemu...

Embodiment 2

[0037] Embodiment 2 proposes a kind of erianin nano preparation, comprises the raw material of following parts by weight: 25 parts of erianin monomers, 20 parts of glyceryl monostearate, 80 parts of lecithin, 10 parts of dehydrated alcohol and spit 55 parts of temperature-80 aqueous solution. The mass concentration of the Tween-80 aqueous solution is 0.5%-1%.

[0038] The method for the erianin nano-preparation of embodiment 2, comprises the steps:

[0039] (1) Dissolve Tween-80 in distilled water to fully dissolve, and then heat to 78°C to obtain an aqueous phase.

[0040] (2) The glyceryl monostearate, the lecithin and the erianin monomer were dissolved in 13 mL of absolute ethanol, and heated to 78° C. to obtain an oil phase.

[0041] (3) Stir the water phase at a rotational speed of 10000 r / min and add the oil phase dropwise into the water phase with a skin test syringe for emulsification until the mixture is concentrated into 18 mL of nanoemulsion.

[0042] (4) Dispers...

Embodiment 3

[0044] Embodiment 3 proposes a kind of Erianin nano preparation, comprises the raw material of following parts by weight: 20 parts of Erianin monomers, 25 parts of glyceryl monostearate, 75 parts of lecithin, 15 parts of dehydrated alcohol and spit 50 parts of warm-80 aqueous solution. The mass concentration of the Tween-80 aqueous solution is 0.5%-1%.

[0045] The method for the erianin nano-preparation of embodiment 3 may further comprise the steps:

[0046] (1) Dissolve Tween-80 in distilled water to fully dissolve, and then heat to 75°C to obtain an aqueous phase.

[0047] (2) The glyceryl monostearate, the lecithin and the erianin monomer were dissolved in 15 mL of absolute ethanol, and heated to 75° C. to obtain an oil phase.

[0048](3) Stir the water phase at a rotating speed of 5000r / min and add the oil phase dropwise into the water phase with a skin test syringe for emulsification until the mixture is concentrated into 15 mL of nanoemulsion.

[0049] (4) Disperse ...

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Abstract

The invention provides an Erianin nano preparation and a preparation method and application thereof. The Erianin nano preparation comprises the following raw materials by weight: 15 to 25 parts of Erianin monomers, 20 to 30 parts of a W / O type emulsifier, 70 to 80 parts of lecithin, 10 to 20 parts of ethanol, and 45 to 55 parts of an O / W type emulsifier. The Erianin nano preparation of the invention breaks through the bottleneck of poor water solubility of the Erianin and cannot be applied clinically, focuses on preparing the poorly soluble monomeric Erianin into related nano preparations, andpushes the Erianin to a clinical application stage. The Erianin nano preparation can solve the defects of poor targetability and many adverse reactions of conventional chemotherapeutic drugs. The nano preparation prepared by the invention has good targeting to the liver of mice, and is expected to be a related targeted preparation for treating primary liver cancer.

Description

technical field [0001] The invention relates to an erianin nano-preparation and its preparation method and application. Background technique [0002] The incidence rate of liver cancer in my country remains high, which mainly has the following characteristics: the number of deaths from liver cancer in my country is large every year, and about 383,000 people die from liver cancer every year, accounting for 51% of the global number of deaths from liver cancer; from the perspective of epidemiological surveys , HBV chronic persistent infection is the main cause of liver cancer; in diagnosis and treatment, it presents the characteristics of difficult early diagnosis, rapid development, high degree of malignancy, and poor prognosis. At present, the main treatment for liver cancer is surgery, but more than 80% of liver cancers have lost the best period of surgery when they are diagnosed. At present, drugs related to liver cancer mainly include sorafenib, gefitinib and other drugs. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/10A61K47/24A61K31/09A61P1/16A61P35/00
Inventor 于波涛陈相旭徐文强宋宗辉王玲洁
Owner 中国人民解放军西部战区总医院
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