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Blank mixed micelle, and preparation method and applications thereof

A mixed micelle and blank technology, which is applied to blank mixed micelles and their preparation and application fields, can solve the problems of membrane toxicity, large particle size, and non-single molecular structure components of membrane materials.

Active Publication Date: 2018-08-21
XIAMEN GINPOSOME PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome defects such as too strong hemolysis of the existing ginsenoside nano-micelle drug-loading system, instability in animals, etc., and at the same time in order to solve the problem of insufficient biodegradability of polymer micellar membrane materials, The molecular structure of the membrane material is not single, the particle size is large, the membrane material is likely to cause potential toxicity, and the membrane material is expensive. A blank mixed micelle and its preparation method and application are provided.

Method used

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  • Blank mixed micelle, and preparation method and applications thereof
  • Blank mixed micelle, and preparation method and applications thereof
  • Blank mixed micelle, and preparation method and applications thereof

Examples

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preparation example Construction

[0206] Preparation of 2% erythrocyte suspension: Take blood from healthy rabbits, put it into a conical flask containing glass beads and shake it for 10 minutes, or stir the blood with a glass rod to remove fibrinogen and make it into defibrillated blood. Add about 10 times the amount of 0.9% sodium chloride solution, shake well, centrifuge at 1000-1500 rpm for 15 minutes, remove the supernatant, and wash the precipitated red blood cells with 0.9% sodium chloride solution for 2-3 times according to the above method. until the supernatant does not appear red. The resulting erythrocytes were made into a 2% suspension with 0.9% sodium chloride solution for testing.

[0207] Inspection method: Take 5 clean glass test tubes, No. 1 and No. 2 tubes are the test sample tubes, No. 3 tube is the negative control tube, No. 4 tube is the positive control tube, and No. 5 tube is the test product control tube. Add 2% erythrocyte suspension, 0.9% sodium chloride solution, and purified water...

preparation Embodiment 1

[0231] Preparation Example 1 Preparation of Ginsenoside Rg5H

[0232] Dissolve 10g of 20(R)-ginsenoside Rg3 in 20mL of pyridine, add 10mL of acetic anhydride dropwise in an ice-water bath, then add an appropriate amount (usually a catalytic amount, such as 1g) of catalyst DMAP, slowly warm up to room temperature, and react for 10 hours. TLC detected that the raw material point disappeared, concentrated under reduced pressure to remove the organic solvent, extracted 3 times with 200 mL / ethyl acetate, combined the organic phases, washed 3 times with 2M hydrochloric acid, washed 3 times with saturated sodium bicarbonate, dried over anhydrous sodium sulfate, and reduced pressure Concentration to dryness afforded Rg3 acetylated product.

[0233] Dissolve 10g of Rg3 acetylated product in 50mL of dichloromethane, add 1g of boron trifluoride diethyl ether and 1g of triethylsilane successively in an ice-water bath, slowly warm up to room temperature, continue the reaction at room tempe...

preparation Embodiment 2

[0239] Preparation Example 2 Preparation of Ginsenoside Rg5H1(E), Rg5H1(Z), Rk1H

[0240] Weigh 10g of the 20(R)-Rg3 acetylation product, dissolve it in 50mL of methanol, add 1g of palladium carbon, under normal temperature and pressure, pass in hydrogen, stir for 4-6 hours until the reaction liquid does not absorb hydrogen, TLC detects to the raw material point Disappeared, filtered off the palladium carbon, concentrated under reduced pressure to remove methanol, and dried to obtain 20(R)-Rg3 acetylated hydrogenation product.

[0241] Weigh 10g of 20(R)-Rg3 acetylated hydrogenation product, dissolve it in 50mL of toluene, add 10g of p-toluenesulfonic acid, slowly raise the temperature to 90°C and reflux, react for 4 hours, TLC detects that the raw material point disappears, cool, 100mL / Washed three times with subsaturated sodium bicarbonate solution, dried over anhydrous sodium sulfate, and concentrated to dryness under reduced pressure to obtain a mixture of crude acetylate...

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Abstract

The invention discloses blank mixed micelle, and a preparation method and applications thereof. The blank mixed micelle comprises an amphiphilic copolymer and ginsenoside represented by formula I, ishigh in efficiency, is safe, is stable, is high in targeting performance, is excellent in homogeneity, is stable in quality, is convention in preparation technology, can be used for coating one or a plurality of active substances in drugs or cosmetics and health care substances, and is capable of forming mixed micelle containing loaded active substances. Compared with conventional nanometer micelle, the blank mixed micelle possesses following advantages: the mixed micelle loaded with active substances is excellent in drug forming performance, multiple drug resistance, stability, homogeneity, and safety performance, and is small in particle size; and the curative effect of loaded active drugs on drug resistant cells is better.

Description

technical field [0001] The invention relates to a blank mixed micelle, a preparation method and application thereof. Background technique [0002] The general feature of polymer micelles is that they are amphiphilic, that is, they have both hydrophilic groups and hydrophobic groups. The hydrophobic groups generally form an inner core in the middle, and the hydrophilic groups generally form an outer shell. Polymer micelles can wrap fat-soluble drugs in their hydrophobic centers to form drug-loaded polymer micelles, and can dissolve in water or alcohol with their hydrophilic ends. Polymer micelles can wrap drugs inside the micelles, prolong the circulation time and biological half-life of drugs in the blood, or increase the accumulation of drugs in lesion sites, reduce adverse reactions, or can be connected to special carriers, antibodies or ligands , so that it can bind to the receptors of target cells and improve the therapeutic effect. [0003] Genexol-PM, developed by So...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K47/24A61K47/10A61K47/28A61K31/337A61P35/00A61K8/85A61K8/86A61K8/63A61K8/06A61Q19/00
CPCA61K8/068A61K8/63A61K8/85A61K8/86A61K9/1075A61K31/337A61K47/10A61K47/24A61K47/28A61K47/34A61K2800/10A61Q19/00
Inventor 王丹李翀王亚华詹华杏
Owner XIAMEN GINPOSOME PHARM CO LTD
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