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Hydroxyl-alpha-sanshool nano-liposome and preparation method thereof

A technology of nano-liposome and sanshool, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve the problems of liposome drug leakage, low drug encapsulation rate, and instability in the body. and other problems, to achieve the effect of long storage time, good curative effect, and improved drug loading rate

Active Publication Date: 2022-01-28
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If hydroxy-alpha-sanshool is prepared into liposomes, it will help to solve the problem of its poor stability
[0005] However, the biggest problem that liposomes currently have is instability in the body and low encapsulation efficiency, and the instability of liposomes easily leads to drug leakage. resulting in lower drug encapsulation efficiency

Method used

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  • Hydroxyl-alpha-sanshool nano-liposome and preparation method thereof
  • Hydroxyl-alpha-sanshool nano-liposome and preparation method thereof
  • Hydroxyl-alpha-sanshool nano-liposome and preparation method thereof

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Effect test

Embodiment 1

[0052] Embodiment 1, the preparation of hydroxy-alpha-sanshool nano liposome

[0053] Weigh 3 mg of HAS, 5 mg of cholesterol and 25 mg of soybean lecithin. Add 10ml of chloroform under the condition of avoiding light. After ultrasonication, the solution in the bottle is mixed and dispersed evenly. The solvent is evaporated by a rotary evaporator. Dissolve completely in ultrapure water to form a uniform and stable mixture. The prepared hydroxyl-alpha-sanshool nanoliposome solution is filtered three times in a 200nm filter membrane to obtain the hydroxyl-alpha-sanshool nanoliposome.

Embodiment 2

[0062] Embodiment 2, the preparation of hydroxy-alpha-sanshool nano liposome

[0063] Weigh 3mg of HAS and auxiliary material lipid material (the lipid material is soybean lecithin and cholesterol with a mass ratio of 4:1) under dark conditions, the mass ratio of HAS and auxiliary material is 1:20, add 10mL chloroform, lightly Gently shake to fully dissolve the drug and excipients; evaporate the solvent with a rotary evaporator, add 10 mL of ultrapure water after vacuum drying, hydrate in an ice-water bath, and ultrasonically for 20 minutes to completely dissolve the film into ultrapure water to form a uniform and stable film. For the mixed solution, the prepared hydroxyl-alpha-sanshool nanoliposome solution is filtered three times in a 200nm filter membrane to obtain the hydroxyl-alpha-sanshool nanoliposome.

Embodiment 3

[0076] Embodiment 3, the preparation of hydroxy-alpha-sanshool nano liposome

[0077] Weigh 3 mg of HAS and lipid material as an auxiliary material (the lipid material is cholesterol and soybean lecithin, the total mass is 60 mg, and the mass ratio of cholesterol to soybean lecithin is 1:4) under dark conditions, add 10 mL of chloroform, lightly Gently shake to fully dissolve the drug and excipients; evaporate the solvent with a rotary evaporator, add 10 mL of ultrapure water after vacuum drying, hydrate in an ice-water bath, and ultrasonically for 20 minutes to completely dissolve the film into ultrapure water to form a uniform and stable film. For the mixed solution, the prepared hydroxyl-alpha-sanshool nanoliposome solution is filtered three times in a 200nm filter membrane to obtain the hydroxyl-alpha-sanshool nanoliposome.

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Abstract

The invention provides a hydroxyl-alpha-sanshool nano-liposome and a preparation method thereof, belongs to the field of pharmaceutical preparations, in particular relates to a hydroxyl-alpha-sanshool composition which is a preparation prepared from the following raw and auxiliary materials in parts by weight: 1 part of hydroxyl-alpha-sanshool and 10-30 parts of a lipid auxiliary material, the lipid auxiliary material is composed of cholesterol and phospholipid; the mass ratio of the cholesterol to the phospholipid is 1: (1-5). The preparation is a nano-liposome. The nano-liposome has very high encapsulation efficiency, and the drug loading rate of the liposome can be effectively improved. Meanwhile, the liposome is uniform in particle size dispersion and good in stability; and the liposome is high in safety and has a better curative effect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a hydroxy-alpha-sanshool nano liposome and a preparation method thereof. Background technique [0002] Hydroxy-α-sanshool (Hydroxy-α-sanshool, HAS) is an unsaturated chain fatty acid amide, which is an important material basis for the special pungent taste of Zanthoxylum bungeanum. In addition, studies have also found that hydroxy-α-sanshool has good biological activities, such as improving learning and memory impairment, inhibiting oxidative stress and apoptosis of nerve cells under pathological conditions, and regulating blood sugar. Therefore, hydroxy-α-sanshool can be used to prepare medicines and has great potential in clinical application. [0003] However, there are abundant cis-conjugated double bonds in the structure of hydroxy-α-sanshool, which makes it unstable at room temperature, and is very susceptible to chemical changes under the influence of temperatur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/16A61K47/28A61K47/24A61P25/28A61P3/08
CPCA61K9/127A61K31/16A61K47/28A61K47/24A61P25/28A61P3/08Y02A50/30
Inventor 彭伟吴纯洁李若兰张萌萌张青
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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