Moleplant seed fatty oil-cholate mixed micelle containing euphorbetin, preparation method and application thereof

A technology of azalea and mixed micelles, which is applied in the directions of medical preparations containing active ingredients, medical preparations with non-active ingredients, and non-active ingredients of oil/fat/wax, etc. The problem of poor water solubility and unsatisfactory gastrointestinal absorption effect of vegan can achieve the effect of improving intestinal absorption effect and improving solubility.

Active Publication Date: 2017-10-10
SHANDONG UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the problems of poor water solubility of stephenin, unsatisfactory gastrointestinal absorption effect, and insufficient potential activity, the present invention provides a stephardin-containing fatty oil-bile salt mixed micelle

Method used

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  • Moleplant seed fatty oil-cholate mixed micelle containing euphorbetin, preparation method and application thereof
  • Moleplant seed fatty oil-cholate mixed micelle containing euphorbetin, preparation method and application thereof
  • Moleplant seed fatty oil-cholate mixed micelle containing euphorbetin, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1 Preparation of Fructus Stephanae Fatty Oil.

[0056] (1) Pulverize the daughter of the daughter of a daughter into a daughter of the daughter of a daughter through a 20-mesh sieve;

[0057] (2) Extract 1,000g of Fructus Rhizome powder with 20,000g of ethanol three times, and combine to obtain the ethanol extract;

[0058] (3) Recover the alcohol extract to remove ethanol, then pass it through silica gel column chromatography with a particle size of 100-200 mesh, and use petroleum ether (60-90°C) as the eluting solvent for elution, and the eluate is the fatty oil .

Embodiment 2

[0059] Example 2 Preparation of Stephaniae Fatty Oil-Bile Salt Mixed Micelle Containing Stephanin.

[0060] (1) Dissolve 200 mg of sodium deoxycholate in 0.01 M phosphate buffer (PBS) at pH=7.4 to obtain a 0.2 mg / mL sodium deoxycholate solution;

[0061] Weighed 5mg of stephartine L1, L2, L3 and L8 and dissolved in ethyl acetate to obtain a stepharutin mixed solution with the concentration of each monomer being 1 mg / mL;

[0062] Weigh 2 g of the Fructus Stephanae fatty oil obtained in Example 1 and dissolve it in ethyl acetate to obtain a 20 mg / mL fatty oil solution.

[0063] (2) Take 1 mL of the above-mentioned stephenin mixed solution and stephaezi fatty oil solution respectively, put them in the same round-bottomed flask, evaporate in a water bath at 40°C, evaporate the ethyl acetate, and put the round-bottomed flask in a vacuum drying oven , evacuated overnight at room temperature to remove residual ethyl acetate to form a lipid film.

[0064] (3) Take 80 mL of sodium de...

Embodiment 3

[0070] Example 3 Characterization of Stephaniae Fatty Oil-Bile Salt Mixed Micelle Containing Stephanin.

[0071] 3.1 Form

[0072] The solutions in Example 2 and Comparative Example 1 are characterized by a high-resolution transmission electron microscope, and the photomicrograph of the stephaezi fatty oil-bile salt mixed micelles solution containing stephenin is as follows: figure 1 As shown, the photomicrographs of the spironocin-bile salt micellar solution are shown as figure 2 shown. Depend on figure 1 and figure 2 It can be seen that the micelles formed by the diterpene alcohol esters of stephenae in sodium deoxycholate solution are more regular in shape, more uniform in particle size, and more uniform in distribution in the presence of stephatia fatty oil.

[0073] 3.2 Particle size distribution and Zeta potential

[0074] Zetasizer 3000 HS instrument (Malvern Instruments, Malvern, UK) measured the particle size and Zeta potential of the sample solution S1 of Exam...

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Abstract

The invention provides a moleplant seed fatty oil-cholate mixed micelle containing euphorbetin,which contains euphorbetin, moleplant seed fatty oil and deoxycholate, wherein the mass ratio of euphorbetin to moleplant seed fatty oil to deoxycholate is (1-3):(20-200):(8-16). The moleplant seed fatty oil-cholate mixed micelle is prepared according to the method which comprises the following steps: respectively dissolving euphorbetin, moleplant seed fatty oil and deoxycholate in suitable solvents; mixing a euphorbetin solution with a moleplant seed fatty oil solution, removing the solvents and preparing into a fat film; mixing a deoxycholate solution with the fat film and then ultrasonically treating, centrifuging, taking supernate and filtering and then acquiring a filtrate, namely, a moleplant seed fatty oil-cholate mixed micelle solution containing euphorbetin; performing freeze drying, thereby acquiring the moleplant seed fatty oil-cholate mixed micelle preparation containing euphorbetin. The moleplant seed fatty oil-cholate mixed micelle containing euphorbetin solves the problems of poor water solubility of euphorbetin, unsatisfying stomach and intestine absorbing effect and incapability of fully utilizing the potential activity and can be used for preparing an antitumor drug.

Description

technical field [0001] The invention relates to a stephenia fatty oil-bile salt mixed micelle containing stephenin, a preparation method and application thereof, and belongs to the technical field of preparation of antitumor drugs. Background technique [0002] Stephania diterpene alcohol ester compounds, also known as stephenzi, have pharmacological effects such as diarrhea, anti-tumor, and anti-leukemia. Modern studies have confirmed that this type of compound is mainly through the cytotoxic effect on cancer cells or the increase in multidrug resistance. The sensitivity of cells to conventional anti-tumor drugs exerts anti-tumor effects. [0003] Cytotoxic effect of stepharutin on cancer cells: Zhang JY, Liang YJ, Chen HB, et al. Structure identification of Euphorbia factor L3 and its induction of apoptosis through the mitochondrial pathway[J]. Molecules, 2011, 16(4 ): 3222-3231) Detection of Paleurin L by MTT method 1 IC on human lung cancer A549 cells 50 51.34±3.28 µM...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/336A61K31/4402A61K31/235A61K47/44A61K47/28A61P35/00
CPCA61K9/1075A61K31/235A61K31/336A61K31/4402A61K47/28A61K47/44
Inventor 张超郭菲王英姿林桂涛高慧慧杨立梅
Owner SHANDONG UNIV OF TRADITIONAL CHINESE MEDICINE
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