Glycosyl polyether compound liposome as well as preparation method and medicine thereof

A polyether compound and liposome technology, which is applied in liposome delivery, drug combination, nano-drugs, etc., can solve the problems of low bioavailability, affecting drug delivery effect, and short drug delivery time, so as to ensure physiological efficacy , small particle size and narrow particle size distribution

Active Publication Date: 2021-10-01
WUHAN HESHENG TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, oral or intraperitoneal administration makes most of it easily metabolized, resulting in low bioavailability, short administration time, and small action area, which affects the administration effect.

Method used

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  • Glycosyl polyether compound liposome as well as preparation method and medicine thereof
  • Glycosyl polyether compound liposome as well as preparation method and medicine thereof
  • Glycosyl polyether compound liposome as well as preparation method and medicine thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1 liposome encapsulated maduramycin (also known as maduramycin liposome)

[0053] Example 1 uses maduramycin as a representative compound of the compound shown in formula I for liposome encapsulation. Wherein the specific structural formula of maduramycin is as follows:

[0054]

[0055] Concrete preparation steps are as follows:

[0056] (1) Take by weighing 20g soybean lecithin, 10g cholesterol and 5g maduramycin, and place them in a round bottom bottle;

[0057] (2) Dissolve the mixed solvent of 15mL of chloroform and 2mL of methanol;

[0058] (3) the dissolved solution is placed in a rotary evaporator at normal temperature, and most of the organic solvent is removed by distillation under reduced pressure, and then the residual organic solvent is removed with a nitrogen blower;

[0059] (4) After removing the organic solvent, add a certain amount of sucrose buffer (2125mg sucrose, 94mg glycine and 7mg calcium chloride dihydrate can be mixed and disso...

Embodiment 2

[0060] Example 2 Liposome encapsulation J1-001-1 (also known as J1-001-1 liposome)

[0061] Example 2 uses J1-001-1 as a representative compound of the compound represented by formula II for liposome encapsulation. The specific structural formula of J1-001-1 is as follows:

[0062] (J1-001-1),

[0063] Concrete preparation steps are as follows:

[0064] (1) Weigh 25g of gangliosides, 10g of cholesterol and 5g of J1-001-1, and place them in a round bottom bottle;

[0065] (2) Dissolve the mixed solvent of 15mL of chloroform and 2mL of methanol;

[0066] (3) After the solution is dissolved, it is placed in a rotary evaporator at normal temperature, and most of the organic solvent is removed by distillation under reduced pressure, and then the residual organic solvent is removed with a nitrogen blower;

[0067] (4) After removing the organic solvent, add a certain amount of sucrose buffer solution, ultrasonicate for 20 minutes in a water bath at 50°C, place in a high-pressu...

Embodiment 3

[0068] Example 3 Liposome encapsulation J1-001-2 (also known as J1-001-2 liposome)

[0069] Example 3 uses J1-001-2 as a representative compound of the compound represented by formula II for liposome encapsulation. Wherein the concrete structure of this compound is as follows:

[0070] (J1-001-2),

[0071] Concrete preparation steps are as follows:

[0072] (1) Weigh 25g of gangliosides, 10g of cholesterol and 5g of J1-001-2, and place them in a round bottom bottle;

[0073] (2) Dissolve the mixed solvent of 15mL of chloroform and 2mL of methanol;

[0074] (3) After the solution is dissolved, it is placed in a rotary evaporator at normal temperature, and most of the organic solvent is removed by distillation under reduced pressure, and then the residual organic solvent is removed with a nitrogen blower;

[0075] (4) After removing the organic solvent, add a certain amount of phosphate buffer, ultrasonicate for 20 minutes in a water bath at 50°C, place in a high-pressure ...

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Abstract

The invention provides glycosyl polyether compound lipidosome as well as a preparation method and a medicine thereof. The glycosyl polyether compound lipidosome comprises a glycosyl polyether compound and a lipidosome, and the lipidosome wraps the glycosyl polyether compound to form a double-layer membrane. The preparation method comprises the following steps: dissolving lipidosome and a glycosyl polyether compound by using an organic solvent; and carrying out suspended evaporation to remove the organic solvent, mixing with a water-phase medium, and carrying out ultrasonic treatment. The provided medicine comprises the glycosyl polyether compound liposome. The glycosyl polyether compound lipidosome provided by the invention is small in particle size and narrow and uniform in particle size distribution, fully ensures the physiological efficacy of the glycosyl polyether compound, and is simple in preparation method.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a glycosyl polyether compound liposome, a preparation method thereof and a medicine. Background technique [0002] Glycosyl polyether compounds are a class of fat-soluble substances and have good application prospects, whether in the field of cancer treatment or in the field of anti-virus, especially in the field of anti-RNA virus, they all show good therapeutic effects. However, oral or intraperitoneal administration makes most of it easily metabolized, resulting in low bioavailability, short administration time and small action area, which affects the administration effect. [0003] Therefore, for glycosyl polyether compounds, it is very necessary to develop a new dosage form with good water solubility, fast absorption, certain targeting effect, long-term effect and controlled release. Contents of the invention [0004] The present invention solves at least one of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61P31/12A61P31/14A61P35/00B82Y5/00B82Y40/00
CPCA61K9/127A61P35/00A61P31/12A61P31/14A61K31/7048B82Y5/00B82Y40/00A61P31/18A61K31/351Y02A50/30
Inventor 刘天罡黄敏坚
Owner WUHAN HESHENG TECH CO LTD
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