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A nanometer cordyceps militaris peptide liposome and its preparation method and an oral liquid preparation

A technology of Cordyceps militaris and liposomes, applied in the directions of liposome delivery, peptide/protein components, pharmaceutical formulations, etc., can solve the problem of inability to obtain Cordyceps militaris peptide liposomes, decreased liposome encapsulation rate, and lipid The problem of low body encapsulation rate, etc., is conducive to transdermal absorption and in vivo delivery, high encapsulation rate, and small molecular size.

Active Publication Date: 2020-05-22
JILIN SERICULTURE SCI RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The film dispersion method is to dissolve lecithin, cholesterol and other lipids and fat-soluble drugs in chloroform (or other organic solvents), and then rotate to evaporate to form a film on the inner wall of the bottle, and dissolve water-soluble drugs in phosphate buffered saline. solution, add it into the flask and keep stirring to obtain macroporous liposomes with larger molecular radius, but this method requires a high concentration of organic solvents, and the addition of phosphate is required to dissolve the embedded drug. The encapsulation of this liposome The rate is generally high, but the permeability is poor; the ultrasonic method is to mix the aqueous solution of the drug with the organic solvent dissolved in the lipid and then ultrasonically treat it to prepare liposomes. This method is simple and easy, but the obtained liposomes encapsulate The efficiency is low; the freeze-drying method is particularly suitable for heat-unstable drugs, but the encapsulation efficiency of liposome preparation will be reduced by freeze-drying; the reverse phase evaporation method is a relatively common method for preparing liposomes, and the obtained The liposomes are large unilamellar liposomes, generally larger in size, this method is suitable for wrapping water-soluble drugs and macromolecular bioactive substances, the method has high encapsulation volume, but the encapsulation efficiency is low, and the obtained by the above method Liposome molecular particle size is greater than 100nm
The prior art cannot obtain a kind of highly efficient and stable Cordyceps militaris peptide liposome

Method used

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  • A nanometer cordyceps militaris peptide liposome and its preparation method and an oral liquid preparation
  • A nanometer cordyceps militaris peptide liposome and its preparation method and an oral liquid preparation
  • A nanometer cordyceps militaris peptide liposome and its preparation method and an oral liquid preparation

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preparation example Construction

[0035] In the present invention, the molecular weight of the nano cordyceps militaris peptide is not greater than 5000 Daltons; the nano cordyceps militaris peptide is mixed with the film in the form of a nano cordyceps militaris peptide solution, and the pH value of the nano cordyceps militaris peptide solution is is 6.5 to 8.0. In the present invention, the pH value of the nano cordyceps militaris peptide solution is preferably 6.8. In the present invention, the preparation method of the nano cordyceps militaris peptide solution includes the following steps: pulverizing the fruiting body of cordyceps militaris by nanometer ball milling for 30 minutes to obtain nano cordyceps militaris powder; dissolving the nano cordyceps militaris powder in water, at pH The obtained supernatant is subjected to 5000 Dalton molecular weight cut-off ultrafiltration, and the obtained filtrate is a nano cordyceps militaris peptide solution. In the present invention, the nano cordyceps militaris...

Embodiment 1

[0060] Take 50 grams of soybean hydrogenated lecithin and 50 grams of cholesterol and dissolve it in a mixed solvent of 150 grams of n-hexane and 150 grams of chloroform. After fully dissolving, pour it into a dry round-bottomed flask, spin and evaporate the organic solvent to dryness, and put it in the flask. A uniform film was formed on the inner wall, 200 ml of nano cordyceps militaris peptide solution with pH 6.8 was added, 83.3 g of water was used, hydrated at 50°C for 40 minutes, sonicated for 5 minutes and then centrifuged at 4,000 rpm, and the supernatant was taken for freeze-drying , the obtained white powder was canned.

[0061] The transmission electron microscope photos of nanometer cordyceps militaris peptide liposome microspheres are as follows: figure 1 shown, figure 1 The photo of liposome single molecule, liposome is spherical structure. The transmission electron microscope photos of the nano-Cordyceps militaris peptide liposome solution are as follows: fi...

Embodiment 2

[0063] Take 500 grams of soybean hydrogenated lecithin and 500 grams of cholesterol and dissolve them in a mixed solvent of 1,500 grams of n-hexane and 1,500 grams of chloroform. After fully dissolving, pour into a dry round-bottomed flask, spin to evaporate the organic solvent, and put it in the flask. A uniform film was formed on the inner wall, 2000 ml of nano Cordyceps militaris peptide solution with pH 6.8 was added, 800 grams of water was used, hydrated at 50°C for 40 minutes, sonicated for 4 minutes and then centrifuged at 4,000 rpm, and the supernatant was taken for freeze-drying , the obtained white powder was canned.

[0064] The particle size of liposomes is 21-57nm.

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Abstract

The invention relates to a nano cordyceps militaris peptide lipidosome, a preparation method thereof and an oral liquid preparation, belonging to the technical field of preparation of lipidosomes. Thenano cordyceps militaris peptide lipidosome provided by the invention comprises nano cordyceps militaris peptide and a lipidosome membrane layer, wherein the nano cordyceps militaris peptide is wrapped inside the lipidosome membrane layer, input materials of the lipidosome membrane layer comprise the following components in parts by weight: 6-7 parts of soybean hydrogenated lecithin, 6-9 parts ofcholesterol, 17-18 parts of normal hexane, 18-19 parts of chloroform and 9-10 parts of water; and raw materials for forming the lipidosome membrane layer comprise soybean hydrogenated lecithin and cholesterol. The nano cordyceps militaris peptide lipidosome provided by the invention has high encapsulation efficiency and good cell compatibility, and a production technology of the nano cordyceps militaris peptide lipidosome is simple.

Description

technical field [0001] The invention relates to the technical field of liposome preparation, in particular to a nanometer cordyceps militaris peptide liposome, a preparation method thereof, and an oral liquid preparation. Background technique [0002] Cordyceps militaris peptides have antioxidant and hypoglycemic activities, and can be used for adjuvant treatment of diabetes. However, due to the special acidic environment in the stomach, it is easily decomposed, and the small absorption area of ​​the gastric mucosa affects the absorption and utilization of peptide substances. [0003] Liposomes are artificially prepared closed sac-like structures formed spontaneously in water by the hydrophobic interaction between phospholipid molecules, and drugs are encapsulated inside the liposomes. Liposomes are simple to prepare, non-toxic to the body and non-immunogenic, and are mainly phagocytosed by grid cells after entering the body, so the utilization rate of drugs can be improved...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/24A61K38/01A61P3/10
CPCA61K9/0095A61K9/127A61K38/011A61K47/24
Inventor 杨淑芳李森张海东朱兴友韩建华孙继红钱琨张春杨朴玉兰王茹薛强
Owner JILIN SERICULTURE SCI RES INST