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A kind of eutectic of azelaic acid and organic base and its preparation method and application

A technology of azelaic acid and organic base, which is applied in the field of eutectic and preparation of azelaic acid and organic base, which can solve the problems of instability and poor water solubility of azelaic acid, and achieve high stability

Active Publication Date: 2022-02-11
SHENZHEN SHINESKY BIOLOGICAL TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to provide a co-crystal of azelaic acid and an organic base and its preparation method and application in view of the above-mentioned defects of the prior art, aiming at solving the problem of the poor water solubility of azelaic acid in the prior art. stability problem

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  • A kind of eutectic of azelaic acid and organic base and its preparation method and application
  • A kind of eutectic of azelaic acid and organic base and its preparation method and application
  • A kind of eutectic of azelaic acid and organic base and its preparation method and application

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preparation example Construction

[0028] Such as Figure 5 Shown, the preparation method of the eutectic of a kind of azelaic acid of the present invention and organic base, comprises the following steps:

[0029] Step S100 , providing azelaic acid and an organic base, and mixing the azelaic acid and the organic base to obtain a mixture; wherein, the water solubility of the organic base is greater than that of the azelaic acid.

[0030] Specifically, azelaic acid may be 1,9-azelaic acid, and an organic base refers to an organic compound containing an amino group in its molecule. The organic base may be an alkaloid, and an alkaloid refers to a nitrogen-containing basic organic compound existing in nature. Specifically, the organic base may be one or more of niacinamide, matrine, choline, triethanolamine, acetyl-L-carnitine, cytisine and L-carnitine. The structural formula of 1,9-azelaic acid is as follows: The structural formula of niacinamide is as follows: The structural formula of L-carnitine is as fol...

specific Embodiment 1

[0050] A preferred method for the preparation of 3-pyridinecarboxamide 1,9-azelaic acid co-crystal:

[0051] Step 1: Weigh 0.01 mol of 3-pyridinecarboxamide and 1,9-azelaic acid, place them in a reactor, and feed an inert gas into the reactor so that the entire reaction is carried out in an oxygen-free state. After sealing the reactor, the temperature was slowly raised to 115° C., and after reacting for 3 hours, the reactor was naturally cooled to room temperature to obtain the crude product of 3-pyridinecarboxamide 1,9-azelaic acid eutectic.

[0052] Second step: recrystallization of the crude eutectic product. Dissolve the crude product of 3-pyridinecarboxamide 1,9-azelaic acid eutectic with isopropanol:ethyl acetate at a ratio of 1:3 (according to the ratio of 6ml to 1g). After it is completely dissolved, filter the membrane to remove Impurities in the crude product. The eutectic solution after impurity removal was concentrated to a supersaturated state (the remaining vol...

specific Embodiment 2

[0093] A method for preparing 3-pyridinecarboxamide 1,9-azelaic acid co-crystal: Step 1: Place the reactor in an ice-salt bath at 0°C, weigh 0.01mol of 3-pyridinecarboxamide and add it to the reaction In the reactor, add 0.015mol of 1,9-azelaic acid into the reactor, and pass argon gas into the reactor, so that the whole reaction process is carried out in an oxygen-free state. After the reaction is sealed, the temperature is slowly raised to 85°C. After reacting for 6 hours, the eutectic solution of 3-pyridinecarboxamide 1,9-azelaic acid was obtained. Second step: recrystallization of the crude eutectic product. Dissolve the crude product of 3-pyridinecarboxamide 1,9-azelaic acid eutectic with isopropanol:ethyl acetate at a ratio of 1:3 (according to the ratio of 6ml to 1g). After it is completely dissolved, filter the membrane to remove Impurities in the crude product. The eutectic solution after impurity removal was concentrated to a supersaturated state (the remaining vol...

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Abstract

The invention discloses a co-crystal of azelaic acid and an organic base and its preparation method and application. The method comprises the steps of: providing azelaic acid and an organic base, and mixing the azelaic acid and the organic base to obtain a mixture; Wherein, the water solubility of the organic base is greater than the water solubility of the azelaic acid; under an inert atmosphere, the mixture is stirred and heated to melt, the mixture is cooled to normal temperature after the reaction, and purified to obtain azelaic acid and organic Alkaline eutectic. By using a highly water-soluble organic base and azelaic acid to form a co-crystal, the water solubility of the obtained co-crystal of azelaic acid and organic base is higher than that of azelaic acid monomer, and the organic base is formed by heating. The eutectic of alkali and azelaic acid, the obtained eutectic of azelaic acid and organic base has high stability.

Description

technical field [0001] The invention relates to the technical field of eutectics, in particular to a eutectic of azelaic acid and an organic base, a preparation method and an application thereof. Background technique [0002] In the prior art, azelaic acid has good antibacterial and bactericidal effects, so it often appears in the field of cosmetics with skin cleaning functions such as oil control, acne removal, exfoliation and pore refinement. However, due to its poor water solubility, it is difficult to evenly distribute it in skin care products that use water as a solution during the preparation process, which may easily cause problems such as product instability and difficulty in storage, and at the same time cause the skin to not absorb the product well and reduce the functional effect of the product . [0003] Therefore, the prior art still needs to be improved and developed. Contents of the invention [0004] The technical problem to be solved by the present inven...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C55/18C07C51/43C07C51/41C07D213/82C07C215/12C07C213/08C07C213/10C07C215/40C07D471/22C07D471/18C07C229/22C07C227/42C07C227/18A61K8/362A61K8/41A61K8/49A61K8/67A61K31/194A61K47/54A61P17/00A61P29/00A61P31/04A61P39/06A61Q17/00A61Q19/02A61Q19/08A61Q19/10
CPCC07C55/18C07C51/43C07C51/412C07D213/82C07C215/12C07C213/08C07C213/10C07C215/40C07D471/22C07D471/18C07C229/22C07C227/42C07C227/18A61K8/362A61K8/675A61K8/494A61K8/416A61K8/41A61Q17/005A61Q19/02A61Q19/10A61Q19/08A61K31/194A61K47/545A61K47/54A61K47/542A61P31/04A61P29/00A61P39/06A61P17/00C07B2200/13
Inventor 王振元张嘉恒王天晓李嘉奇干瑞靖吴称玉
Owner SHENZHEN SHINESKY BIOLOGICAL TECH CO LTD
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