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Activator-cyclodextrin inclusion with protamine and preparation and application thereof

A technology of cyclodextrin inclusion complex and protamine, which can be used in medical preparations containing active ingredients, preparations for skin care, cosmetic preparations, etc., and can solve problems such as the decrease of total concentration

Active Publication Date: 2019-09-20
SHANGHAI JAHWA UNITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, under the action of ultraviolet light, although the concentration of cis-resveratrol will gradually increase over a period of time, the total concentration of the two resveratrols will still decrease due to the consumption of resveratrol at the same time due to side reactions.

Method used

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  • Activator-cyclodextrin inclusion with protamine and preparation and application thereof
  • Activator-cyclodextrin inclusion with protamine and preparation and application thereof
  • Activator-cyclodextrin inclusion with protamine and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Weigh 1g of resveratrol and 0.02g of coumarin, dissolve in 10ml of ethanol to obtain a resveratrol solution. Take 9 g of hydroxypropyl-β-cyclodextrin and dissolve it in 20 ml of purified water. The resveratrol solution was slowly added dropwise into the hydroxypropyl-β-cyclodextrin under magnetic stirring (300r / min), and the stirring was continued for 2 hours, and the solution was clear, colorless and transparent. Ethanol was distilled off under reduced pressure at 45°C, and after continuous stirring for 0.5h, freeze-drying, sublimation drying was set at -80 to -40°C, vacuum degree was 1-30Pa, time was 3-21 hours, analytical drying was set at -10-+20°C, The degree of vacuum is 1-30 Pa, the time is 1-10 hours, the water content is controlled between 0-6%, and white loose porous, spongy amorphous powder is obtained. Grind and sieve through 300 mesh to obtain a white composition for later use.

Embodiment 2

[0096] Weigh 1g of resveratrol and 0.02g of coumarin, dissolve in 10ml of ethanol to obtain a resveratrol solution. Take 11 g of hydroxypropyl-β-cyclodextrin and dissolve it in 20 ml of purified water. The resveratrol solution was slowly added dropwise into the hydroxypropyl-β-cyclodextrin under magnetic stirring (300r / min), and the stirring was continued for 2 hours, and the solution was clear, colorless and transparent. Ethanol was distilled off under reduced pressure at 45°C, and after continuous stirring for 0.5h, freeze-drying, sublimation drying was set at -80 to -40°C, vacuum degree was 1-30Pa, time was 3-21 hours, analytical drying was set at -10-+20°C, The degree of vacuum is 1-30 Pa, the time is 1-10 hours, the water content is controlled between 0-6%, and white loose porous, spongy amorphous powder is obtained. Grind and sieve through 300 mesh to obtain a white composition for later use.

Embodiment 3

[0098] Weigh 1g of resveratrol and 0.02g of coumarin, dissolve in 10ml of ethanol to obtain a resveratrol solution. Take 6.5 g of hydroxypropyl-β-cyclodextrin and dissolve it in 20 ml of purified water. The resveratrol solution was slowly added dropwise into the hydroxypropyl-β-cyclodextrin under magnetic stirring (300r / min), and the stirring was continued for 2 hours, and the solution was clear, colorless and transparent. Ethanol was distilled off under reduced pressure at 45°C, and after continuous stirring for 0.5h, freeze-drying, sublimation drying was set at -80 to -40°C, vacuum degree was 1-30Pa, time was 3-21 hours, analytical drying was set at -10-+20°C, The degree of vacuum is 1-30 Pa, the time is 1-10 hours, the water content is controlled between 0-6%, and white loose porous, spongy amorphous powder is obtained. Grind and sieve through 300 mesh to obtain a white composition for later use.

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Abstract

The invention discloses an activator-cyclodextrin inclusion comprising an activator and cyclodextrin in a molar ratio of 1:5 to 1:1, as well as protamine, wherein the weight ratio of the protamine to the activator is 2:1 to 1:2. The invention also relates to preparation and application of the activator-cyclodextrin inclusion with protamine.

Description

technical field [0001] The invention belongs to the technical field of cosmetics, and in particular relates to an active agent-cyclodextrin inclusion compound containing protamine and its preparation and application. Background technique [0002] Many active agents are chemically unstable and often degrade during storage, or decompose or isomerize easily upon exposure to light. The water solubility of these active agents is poor (for example, the solubility of resveratrol in water is 0.03g / L), and the bioavailability is low, resulting in relatively limited applications. [0003] Resveratrol (Resveratrol for short Res.), also known as stilbene triphenols, is a stilbene compound, an antitoxin produced by plants under fungal infection, ultraviolet radiation or pathological conditions, and also acts as an antioxidant And anti-mutagenic agent, widely exist in plants such as knotweed, peanut, grape, mulberry, hemp vine, smilax, at least 72 species of plants in 21 families and 31 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/73A61K8/64A61K8/34A61Q17/04A61Q19/00A61Q19/08
CPCA61K8/738A61K8/64A61K8/347A61Q19/00A61Q19/08A61Q17/04A61K2800/56A61K2800/84Y02A50/30
Inventor 冯春波乔小玲
Owner SHANGHAI JAHWA UNITED