Lipoic acid mixed micelle as well as preparation method and application thereof

A technology of mixing micelles and lipoic acid, which is applied in drug combinations, pharmaceutical formulations, cosmetic preparations, etc., can solve the problems of inconvenient product processing and preparation, low bioavailability, weak solubility, etc., to improve the overall antioxidant capacity, biological The effect of good compatibility and simple ingredients

Pending Publication Date: 2022-02-08
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still some limitations in the application of lipoic acid, which is mainly related to its special physical and chemical properties, which is manifested in its weak solubility in water, and the dissolved mass fraction is only 0.08% at room temperature, which brings inconvenience to the processing and preparation of subsequent products.
And lipoic acid is easily decomposed under oxygen and light, has low bioavailability, poor stability, and has certain irritation

Method used

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  • Lipoic acid mixed micelle as well as preparation method and application thereof
  • Lipoic acid mixed micelle as well as preparation method and application thereof
  • Lipoic acid mixed micelle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A lipoic acid mixed micelle, its preparation method comprises the following steps:

[0026] Weigh 150mg of soybean lecithin and 50mg of lipoic acid into a 50mL round bottom flask, then add 10mL of methanol therein for dissolution, and ultrasonically disperse evenly. When the temperature of the water bath is 40°C, the methanol is removed by rotary evaporation to form a layer of transparent lipoic acid micellar coprecipitate film. Dissolve 50 mg of sodium lipoic acid in 10 mL of purified water to obtain a mixed solution, and add the mixed solution to the above transparent film. Thin film, obtain the dispersion solution of drug-containing mixed micelles, probe ultrasonic (50W, interval 2s, 2min), then filter with 0.22μm microporous membrane, take filtrate, pack separately, obtain lipoic acid mixed micelles.

Embodiment 2

[0028] A lipoic acid mixed micelle, its preparation method comprises the following steps:

[0029] Weigh 150 mg of soybean lecithin and 50 mg of lipoic acid into a 50 mL round-bottomed flask, then add 10 mL of dichloromethane to dissolve it, and disperse evenly by ultrasonication. When the temperature of the water bath is 35°C, dichloromethane is removed by rotary evaporation, forming a layer of transparent lipoic acid micellar co-precipitate film, dissolving 50 mg of sodium lipoic acid in 10 mL of purified water to obtain a mixed solution, and adding the mixed solution to the above transparent film Hydrate the film in neutral to obtain a dispersion solution of drug-containing mixed micelles. Ultrasonic the probe (50W, interval 2s, 2min), then filter with a 0.22μm microporous membrane, take the filtrate and subpackage to obtain lipoic acid mixed micelles.

Embodiment 3

[0031] A lipoic acid mixed micelle, its preparation method comprises the following steps:

[0032] Weigh 150 mg of soybean lecithin and 50 mg of lipoic acid into a 50 mL round-bottomed flask, then add 10 mL of ethanol to dissolve it, and disperse evenly by ultrasonication. When the temperature of the water bath is 45°C, the ethanol is removed by rotary evaporation to form a layer of transparent lipoic acid micellar coprecipitate film. Dissolve 100 mg of sodium lipoic acid in 10 mL of purified water to obtain a mixed solution, and add the mixed solution to the above transparent film. Thin film, obtain the dispersion solution of drug-containing mixed micelles, probe ultrasonic (50W, interval 2s, 2min), then filter with 0.22 μm microporous membrane, take filtrate, pack separately, obtain lipoic acid mixed micelles.

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Abstract

The invention discloses a lipoic acid mixed micelle which is prepared from lipoic acid, phospholipid and sodium lipoate, the components are simple, the drug loading capacity is high, and the obtained mixed micelle has relatively strong stability and can still keep the properties of the micelle after different dilution ratios and long-term storage. The invention further discloses a preparation method of the mixed micelle, and the preparation method is simple in process, high in repeatability and suitable for industrial production. The mixed micelle does not need to be solubilized by ethanol, propylene glycol and other organic solvents with large stimulation, and the obtained mixed micelle has no side effect in use, is safe and reliable, and has the advantages of wide raw material source and low cost. The invention further discloses application of the mixed micelle, the mixed micelle can be used for preparing cosmetics and preparing pharmaceutical compositions from the mixed micelle and pharmaceutically acceptable pharmaceutic adjuvants, the lipoic acid mixed micelle can be prepared into injections, oral preparations and skin coatings and can be used after being diluted to different degrees, and clinical administration is greatly facilitated.

Description

technical field [0001] The invention relates to a lipoic acid mixed micelle, in particular to a lipoic acid mixed micelle and a preparation method and application thereof. Background technique [0002] α-lipoic acid (ALA) is a natural antioxidant with very strong antioxidant capacity, widely distributed in animal liver tissue and spinach, tomato and other plants. Lipoic acid belongs to vitamin B compounds and acts as a coenzyme in multi-enzyme complexes such as pyruvate dehydrogenase, α-ketoglutarate dehydrogenase, and aminocaproic acid decarboxylase. In recent years, the antioxidant properties of lipoic acid have received more and more attention and become a hot research topic in the scientific community. Alpha-lipoic acid (ALA, oxidized form) can be converted into dihydrolipoic acid (DHLA, reduced form) in the body. Both ALA and DHLA have strong antioxidant properties. They play a synergistic role in the body and are known natural antioxidants. One of the most effective ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/49A61K8/55A61K8/02A61Q19/02A61Q19/08A61K31/385A61K9/107A61K47/24A61P39/06A61P9/00A61P29/00A61P19/06A61P1/16
CPCA61K8/4986A61K8/553A61K8/0291A61Q19/02A61Q19/08A61K31/385A61K9/1075A61K47/24A61P39/06A61P9/00A61P29/00A61P19/06A61P1/16A61K2800/82A61K2300/00
Inventor 李建波张金洁徐雅茹栗庆连王辰旭吴哲杨洋其他发明人请求不公开姓名
Owner ZHENGZHOU UNIV
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