Preparation method of silibinin-polyene phosphatidylcholine compound

A technology of polyene phosphatidylcholine and silibinin, which is applied in the field of medicine, can solve the problems of low bioavailability, poor fat solubility, weak oral absorption ability, etc., achieves high efficacy, is beneficial to absorption, and enhances affinity The effect of water lipophilicity

Pending Publication Date: 2022-03-08
JIANGSU OCEAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, silibinin is almost insoluble in water, poor in fat solubility, weak in oral absorption, and extremely low in bioavailability, which greatly limits its clinical application and development of new drugs.

Method used

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  • Preparation method of silibinin-polyene phosphatidylcholine compound
  • Preparation method of silibinin-polyene phosphatidylcholine compound
  • Preparation method of silibinin-polyene phosphatidylcholine compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 disclosed a method of preparing a water-repellent-polykenne phosphatidylcholine complex, which steps were as follows:

[0057] 1) The 1 g of the thistle is dissolved in 20 ml of anhydrous ethantol to form a solution, and emulsified for 5 min in the emulsified shearing machine, then the solution was solemn at 40 ° C for 30 min;

[0058] 2) 1 g of a polyenephosphatidylcholine is dissolved in 10 ml of moisture anhydrous ethanol to form a solution and ultrasound at 40 ° C for 15 min;

[0059] 3) The above two solutions were mixed with the mass ratio of the water fly Guest and the polyelyphistolocylaltine and mixed at 40 ° C for 30 min at 40 ° C;

[0060] 4) The mixed solution was evaporated under reduced pressure at 40 ° C, 0.009 kp. After the solvent was completely evaporated to dryness.

Embodiment 2

[0062] Example 2 discloses a method of preparing a waterfast-a-polykenyl phosphatidylcholine complex, which is as follows:

[0063] 1) Dissolve 2G flyfatheribin in 40 mL of water to form a solution, and emulsified for 5 min in the emulsified shear machine, then the solution is 40 ° C for 30 min to the solution completely clarified;

[0064] 2) 4 g of a polyenephosphatidylcholine was dissolved in 40 ml of anhydrous ethanol to form a solution, and 15 min at 40 ° C;

[0065] 3) Mix the above two solutions in accordance with the mass ratio of the water flying Guest and the polyelycipated cholate of 1:10 and again at 40 ° C for 30 min;

[0066] 4) Evaporation of the mixed solution at 45 ° C, 0.009 kPa, and then the water fly gin phospholipid complex dry product is obtained after the solvent is completely evaporated.

Embodiment 3

[0068] Example 2 discloses a method of preparing a waterfast-a-polykenyl phosphatidylcholine complex, which is as follows:

[0069] 1) Dissolve 2G flyfatheribin in 40 mL of water to form a solution, and emulsified for 5 min in the emulsified shear machine, then the solution is 40 ° C for 30 min to the solution completely clarified;

[0070] 2) The 2 g of a polylehydripidylcholine was dissolved in 20 ml of anhydrous ethanol to form a solution, and 15 min at 40 ° C;

[0071] 3) Mix the above two solutions in accordance with the mass ratio of the water flying Guest and the polyelycene choline and mixed with 1: 15 at 40 ° C for 30 min;

[0072] 4) Evaporation of the mixed solution at 50 ° C, 0.009 kPa, and then the water flyer gin phospholipid complex dry matter is obtained after the solvent is completely evaporated.

[0073] In summary, the hydrophilic acid-polykenyl phosphatol-polykenylpholine obtained by this Example 1, Example 2 and Example 3 can significantly enhance the hydrophi...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of a silibinin-polyene phosphatidylcholine compound, which comprises the following steps: dissolving silibinin in absolute ethyl alcohol to form a solution, then sequentially carrying out emulsification and ultrasonic treatment to obtain a solution A, dissolving polyene phosphatidylcholine in absolute ethyl alcohol to form a solution, and carrying out ultrasonic treatment to obtain a solution B; after ultrasonic treatment, mixing with the solution A, and carrying out ultrasonic treatment and ethanol removal in sequence, so as to obtain the product. The device comprises an emulsifying and shearing device, an ultrasonic mixing device and a reduced pressure evaporation device which are sequentially fixed on a rack, the prepared compound can significantly enhance the hydrophilicity and lipophilicity of the silibinin, and the polyene phosphatidylcholine serves as a drug carrier and also serves as a functional component, so that the drug has the effects of the silibinin and the polyene phosphatidylcholine at the same time, a better raw material is provided for development of liver disease treatment drugs with higher effects, and the application prospect is wide. The designed preparation device realizes efficient and industrial production of the silibinin-polyene phosphatidylcholine compound.

Description

Technical field [0001] The present invention belongs to the field of medical technology, and more particularly to the preparation method of a water fly Guest - polykenyl phosphatidylcholine complex. Background technique [0002] Snorin refers to a flavonoid-like compound that extracts the resulting flavonoids from the seeds of the medicinal plant water thistle seeds, which are yellow powder, taste. The main active ingredients include four types of homomers such as Wi-fi Bin, Ishihydrate, and Waterfront and Silitan, which are from 50% -70% of the main functional ingredients. It is existing in the form of two diastereomers (water flying cobin a, water flying Bin B). [0003] The thistle is used to treat hepatobiliary diseases for more than 2,000 years. The water flying seeds can prevent chemical toxins, food toxins and drugs such as the damage to the liver, promote the regeneration and repair of hepatocytes, known as " Natural polishs. " Among them, Water Flyingman Show the activit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61K36/28A61K31/685A61K47/54A61K47/55A61P1/16B01F33/82B01F23/41B01D1/00B01D1/22B01F101/22A61K131/00
CPCA61K31/357A61K36/28A61K31/685A61K47/544A61K47/55A61P1/16B01D1/0041B01D1/0082B01D1/22A61K2300/00
Inventor 王松陈丽谢如良
Owner JIANGSU OCEAN UNIV
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