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Method for preparing azelaic acid hydroxypropyl betacyclodextrin clathrate compound

A technology of hydroxypropyl azelaic acid and beta-cyclodextrin, which is applied in skin care preparations, medical preparations of non-active ingredients, drug combinations, etc., and can solve problems such as low solubility, limited application value, and irritation problem, to achieve simple production process, significant inclusion effect, and improve water solubility

Inactive Publication Date: 2018-06-22
SHANDONG BINZHOU ZHIYUAN BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The solubility of azelaic acid in water is low. Azelaic acid has a destructive effect on the stability of the emulsified system. Free azelaic acid has a certain stimulating effect on the skin, eyes, mucous membranes and upper respiratory tract, and the poor water solubility of azelaic acid is not conducive to use
It can be seen that the solubility of azelaic acid is low and irritating, which greatly limits its application value in cosmetics.

Method used

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  • Method for preparing azelaic acid hydroxypropyl betacyclodextrin clathrate compound

Examples

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Effect test

Embodiment 1

[0026] Embodiment 1 A preparation method of azelaic acid hydroxypropyl beta cyclodextrin inclusion compound, the steps are as follows:

[0027] (1) In the reaction kettle, first add 25 kg of hydroxypropyl beta cyclodextrin, then add 50 kg of purified water, stir to dissolve it, and finally add 4.0 kg of azelaic acid, start heating, and heat up while stirring;

[0028] (2) Heating up to 80°C and keeping it for 0.5 hours, then cooling to 50°C for later use;

[0029] (3) Spray-dry the product obtained in step (2) with an LPG-20 spray dryer, control the inlet air temperature to 165°C, and the outlet air temperature to 60°C, and dry for 1 hour to obtain hydroxypropylbetazelate Cyclodextrin inclusion complex. Properties: This product is white or off-white amorphous or crystalline powder; strong hygroscopicity; easily soluble in water. The effective content of azelaic acid is 10%.

Embodiment 2

[0030] Embodiment 2 A preparation method of azelaic acid hydroxypropyl beta cyclodextrin inclusion compound, the steps are as follows:

[0031] (1) In the reaction kettle, first add 75 kg of hydroxypropyl beta cyclodextrin, then add 150 kg of purified water, stir to dissolve it, and finally add 12 kg of azelaic acid, start heating, and heat up while stirring;

[0032] (2) Heating up to 80°C and keeping it for 0.5 hours, then cooling to 50°C for later use;

[0033] (3) Spray-dry the product obtained in step (2) with an LPG-20 spray dryer, control the inlet air temperature to 205°C, and the outlet air temperature to 100°C, and dry for 2 hours to obtain hydroxypropylbetazelate Cyclodextrin inclusion complex. Properties: This product is white or off-white amorphous or crystalline powder; strong hygroscopicity; easily soluble in water; effective content of azelaic acid is 12%.

Embodiment 3

[0034] Embodiment 3 A preparation method of azelaic acid hydroxypropyl beta cyclodextrin inclusion compound, the steps are as follows:

[0035] (1) In the reaction kettle, first add 50 kg of hydroxypropyl beta cyclodextrin, then add 100 kg of purified water, stir to dissolve it, and finally add 8.0 kg of azelaic acid, turn on the heating, and heat up while stirring;

[0036] (2) Heating up to 80°C and keeping it for 0.5 hours, then cooling to 50°C for later use;

[0037] (3) The product obtained in step (2) is spray-dried using an LPG-20 spray dryer, the air inlet temperature is controlled at 185°C, the air outlet temperature is 80°C, and the product is dried for 1.5 hours to obtain hydroxypropylbetazelate Cyclodextrin inclusion complex. Properties: This product is white or off-white amorphous or crystalline powder; strong hygroscopicity; easily soluble in water; effective content of azelaic acid is 15%.

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Abstract

The invention discloses a method for preparing azelaic acid hydroxypropyl betacyclodextrin clathrate compound. The method comprises the steps that firstly hydroxypropyl betacyclodextrin is added intoa reaction kettle, then purified water is added, the mixture is stirred to make hydroxypropyl betacyclodextrin being dissolved, lastly azelaic acid is added, heating is started, and stirring and heating are simultaneously performed; the temperature is risen to 80 DEG C and is kept for 0.5 hour, then the mixture is cooled to 50 DEG C, spray drying is carried out, the air inlet temperature is controlled to 165 DEG C-205 DEG C, the air outlet temperature is 60 DEG C-100 DEG C, and drying is carried out for 2 hours, and the azelaic acid hydroxypropyl betacyclodextrin clathrate compound is obtained. The prepared azelaic acid hydroxypropyl betacyclodextrin clathrate compound avoids the defects of the azelaic acid during the use of cosmetics, the functions of the azelaic acid are maintained, thewater solubility is improved, the irritation is reduced, the prepared azelaic acid hydroxypropyl betacyclodextrin clathrate compound is more conductive to using in skin drugs, cosmetics and nursing products, and greatly expands the application of the azelaic acid.

Description

technical field [0001] The invention relates to the fields of pharmaceutical preparations and cosmetics, in particular to a preparation method of azelaic acid hydroxypropyl beta cyclodextrin inclusion compound. Background technique [0002] Azelaic acid, commonly known as azelaic acid, is a naturally occurring saturated dicarboxylic acid containing nine carbon atoms. It is widely used in cosmetics. Azelaic acid has good antibacterial properties and has significant permeability on the surface of the skin. , can treat skin problems such as acne and acne, and can also balance oil secretion, stimulate hair growth, and inhibit the activity of tyrosinase. [0003] The appearance and properties of azelaic acid are colorless to light yellow crystals or crystalline powder, slightly soluble in cold water, soluble in hot water, ether, and easily soluble in ethanol. Azelaic acid has the ability to inhibit or kill aerobic bacteria and anaerobic bacteria on the skin The effect of bacteri...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/194A61P31/04A61P17/10A61P17/00A61K8/73A61K8/362A61Q17/00
CPCA61K31/194A61K8/362A61K8/732A61Q17/005
Inventor 顾秋香张波安伟李媛媛梁宁宁陈晋波
Owner SHANDONG BINZHOU ZHIYUAN BIO TECH CO LTD
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