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Coenzyme Q10 precursor liposome and preparation method

A proliposome and liposome technology, which is applied in liposome delivery, pharmaceutical formulations, cosmetic preparations, etc., can solve problems such as instability, unstable drugs, and liposome instability, and achieve improved stability Sexuality, improved transdermal absorption, simple preparation

Inactive Publication Date: 2003-08-27
SHANGHAI JAHWA UNITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 1. Liposome, as a colloidal particle, is a thermodynamically unstable system, which is prone to aggregation, fusion, and sedimentation in aqueous solution, oxidative decomposition of phospholipids, leakage of encapsulated drugs, etc., resulting in instability of liposomes;
[0005] 2. Coenzyme Q 10 The instability of the structure makes the drug more unstable in aqueous solution;
[0006] 3. Coenzyme Q 10 The content of the drug in the liposome suspension is generally fixed, while the content of coenzyme Q in different cosmetics 10 The content requirements are different, resulting in coenzyme Q 10 liposomal suspension containing coenzyme Q 10 The formulation of cosmetics is not flexible

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] coenzyme Q 10 120g, ceramide 50g, egg yolk lecithin 50g, cholesterol 100g, sucrose 140g, pH 7.4 phosphate buffer to 1000mL.

[0029] Coenzyme Q in the above prescription 10 , ceramide, egg yolk lecithin, and cholesterol are placed in an Erlenmeyer flask, heated and melted, and placed in a constant temperature water bath at 80°C for later use. Dissolve the prescribed amount of sucrose in 800 mL of pH 7.4 phosphate buffer, filter, heat the filtrate in a water bath to the same temperature as the lipid solution, oscillate and mix the aqueous solution and lipid solution, cool, and dilute the mixed liquid with pH 7.4 phosphate buffer Added to 1000mL, subjected to high-pressure homogenization treatment (high pressure 50MPa, low pressure 10MPa), to obtain a liposome suspension, spray-dried to obtain ceramide-containing coenzyme Q 10 Proliposomes.

Embodiment 2

[0031] coenzyme Q 10 30g, ceramide 50g, soybean lecithin 30g, cholesterol 100g, poloxamer F 68 40g, glucose 200g, chloroform 200mL, pH 7.4 phosphate buffer to 1000mL.

[0032] Coenzyme Q in the above prescription 10 , Ceramide, Soy Lecithin, Poloxamer F 68 Cholesterol was added to a 10000mL round-bottomed flask, and the above-mentioned lipid components were dissolved in chloroform, and placed in a constant temperature water bath at 25-40°C for rotary film evaporation, so that the lipids formed a thin film at the bottom of the round-bottomed flask for later use. Dissolve the prescribed amount of glucose with 800 mL of pH 7.4 phosphate buffer, filter, pour the filtrate into the above-mentioned flask, hydrate, shake, add the mixed liquid to 1000 mL with pH 7.4 phosphate buffer, and process it with ultrasonic waves (output 4, duty cycle 50%, time 10 mins) to obtain a liposome suspension, which was freeze-dried (temperature -50°C, vacuum 50 millitorr) to obtain loose ceramide-co...

Embodiment 3

[0034] coenzyme Q 10 50g, Ceramide 50g, Hydrogenated Lecithin 60g, Cholesterol 40g, Poloxamer F 68 50g, trehalose 80g, ether 200mL, pH7.4 phosphate buffer to 1000mL.

[0035] Coenzyme Q in the above prescription 10 , Ceramide, Hydrogenated Lecithin, Poloxamer F 68, Cholesterol is added in the 500mL Erlenmeyer flask, and above-mentioned lipid component is dissolved with ether, set aside. Dissolve the prescribed amount of trehalose in 800 mL of pH 7.4 phosphate buffer solution, filter, pour the filtrate into a Erlenmeyer flask, place it in a constant temperature water bath at 30-60°C, stir with magnetic force at a stirring speed of 200-1000 rpm, and volatilize the organic solvent to obtain lipid The plastid suspension was freeze-dried (temperature -50°C, vacuum degree 50 millitorr) to obtain loose coenzyme Q containing ceramide 10 Proliposomes.

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PUM

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Abstract

The present invention relates to a coenzyme Q10 liposome containing ceramide, its preparation method and application. Said invention also contains other lipid component in its structure, and can be made into granular material by means of freeze-drying or spray-drying process, then further freeze-dried to obtain the solid preparation. Before use, a certain quantity of water is mixed with it, and shaken, so that the coenzyme Q10 liposome can be obtained. Said invention can promote transdermal absorption of coenzyme Q10 raise the application effect of coenzyme Q10 in the cosmetics, and raise stability of coenzyme Q10 and liposome.

Description

technical field [0001] The invention relates to the fields of pharmaceutical preparations and cosmetics, in particular to a coenzyme Q 10 Proliposomes, especially involving ceramide-containing coenzyme Q 10 Proliposomes and methods for their preparation and use. Background technique [0002] coenzyme Q 10 (coenzyme Q 10 , ubidecarenone) is a class of fat-soluble quinone compounds with the same characteristics as vitamins. It has obvious anti-oxidation and free radical scavenging effects, and is one of the important functional ingredients in many anti-aging products. Studies have shown that coenzyme Q 10 It can promote skin metabolism, promote face and hand skin cell respiratory chain transmission and ATP production, and at the same time inhibit skin lipid peroxidation, thus nourishing and activating the skin. It has been reported that coenzyme Q 10 The firming milk and after-sun cream have obvious anti-wrinkle, whitening, and make skin elastic and other effects. coenz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/14A61K8/35A61K8/68A61K9/127A61K31/122A61K31/164A61P17/00A61P17/02A61P17/14A61P17/16A61Q19/00
CPCA61K8/14A61K31/164A61K8/68A61Q19/00A61K8/355A61K9/1271A61K31/122A61K9/0014A61P17/00A61P17/02A61P17/14A61P17/16A61K9/127
Inventor 陈建明高申李慧良林惠芬魏少敏张仰眉吕洛钟延强史青郭亦光管斐王巍马来记顾娟
Owner SHANGHAI JAHWA UNITED
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