High-concentration azelaic acid acne-removing soothing emulsion

By constructing liquid supramolecular compounds of capryloylglycine, bisabolol, and menthol using DES technology, the solubility and stability issues of azelaic acid in skincare products were resolved, achieving stable loading of high-concentration azelaic acid and a skin-soothing effect.

CN121695018APending Publication Date: 2026-03-20WUXI ZHIYAN BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202511920102.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-12-18
Publication Date
2026-03-20

AI Technical Summary

Technical Problem

Azelaic acid has extremely low solubility and poor stability in skin care products, resulting in strong skin irritation. Existing technical solutions have not been able to completely solve the problems of stable loading and user experience at high concentrations.

Method used

A liquid supramolecular structure was constructed using DES technology with capryloylglycine, bisabolol, and menthol to improve the solubility and stability of azelaic acid and reduce its irritation.

Benefits of technology

This achieved a stable high-concentration loading of azelaic acid, significantly improving the product's skin tolerance and comfort, and enhancing the soothing function of azelaic acid.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention discloses a high-concentration azelaic acid acne-removing soothing emulsion, and belongs to the technical field of medicines and skin care products. The method successfully breaks through the technical bottleneck that the solubility of azelaic acid in a conventional water-oil system is extremely low (generally 1t; 1%). According to the invention, 13-19% high-mass-fraction stable loading of azelaic acid can be realized, the system is still kept in a uniform and transparent liquid state at room temperature and after high and low temperature circulation, no crystal is separated out, and the physical friction stimulation of azelaic acid solid crystal particles to the skin in the traditional formula is eliminated. Meanwhile, the bisabolol, capryloyl glycine and other components contained in the system have an instant soothing effect, chemical irritation of azelaic acid can be reduced, and skin tolerance and use comfort of the product are remarkably improved.
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Description

TECHNICAL FIELD

[0001] The application relates to a high-concentration azelaic acid acne-removing soothing emulsion and belongs to the technical field of medicines and skin care products. BACKGROUND

[0002] Azelaic acid is a naturally occurring straight-chain saturated dicarboxylic acid with a nine-carbon chain. Since the 1980s, its application potential in the field of dermatology has been gradually discovered and in-depth studied, and now it has become a widely recognized multi-effect active ingredient, especially in acne removal, whitening and skin repair, showing unique comprehensive advantages.

[0003] In terms of acne treatment, azelaic acid can effectively inhibit the growth of propionibacterium acnes and staphylococcus epidermidis, thereby reducing the inflammatory response caused by bacteria. At the same time, it can also significantly reduce the concentration of free fatty acids on the skin surface, regulate the keratinization process, and promote the recovery of hair follicle keratinization to normal, thereby achieving multi-target treatment of acne through the synergistic effect of multiple pathways such as antibacterial, anti-inflammatory and keratinization regulation.

[0004] In addition, azelaic acid can effectively improve various pigmentary problems such as post-inflammatory pigmentation, chloasma and acne marks by competitively inhibiting the activity of tyrosinase, interfering with the melanin synthesis process and reducing abnormal pigment deposition, and has the functions of whitening and freckle lightening. Its anti-inflammatory and antioxidant properties also help to soothe the skin and promote barrier repair, and it is a skin active ingredient with comprehensive functions and good tolerance.

[0005] Although azelaic acid has remarkable effects on improving acne, regulating sebum secretion, and whitening and lightening spots, its inherent physicochemical properties (such as extremely low water solubility, high melting point, and the tendency to cause skin irritation such as redness, stinging, or dryness and peeling during use) severely restrict its application in skin care product formulations, especially in the field of high-end skin care products with higher requirements for use and safety. In order to overcome these defects, various solutions have been proposed in the prior art. For example, patent CN112624918A discloses a co-crystal formed by melting and mixing azelaic acid and niacinamide, which effectively improves the water solubility and stability of azelaic acid in the formulation. Niacinamide itself has a skin irritation risk at a certain concentration for some people. When niacinamide and azelaic acid, which also has a certain irritation, form a supramolecular complex through co-crystal technology, the solubility and transdermal delivery efficiency of both in the formulation are improved, but the irritation may also be simultaneously enhanced and concentrated on the skin surface. Another patent CN118526445A proposes to build a eutectic solvent system by selecting betaine and any one of an amino-containing compound, an alcohol, or a carboxylic acid for compounding, achieving high loading capacity, excellent skin permeability, and controlled release performance of azelaic acid. In addition, CN118178240A uses ultrafine grinding technology to process azelaic acid raw materials, enabling them to disperse uniformly in the material body and avoid agglomeration. Patent CN120346136A introduces a method for preparing azelaic acid by nanoemulsion technology, which requires first embedding azelaic acid with cyclodextrin to form an aqueous phase with niacinamide and other substances, then mixing with a complex oil phase to form a nanoemulsion, and finally mixing with additives such as carbomer to form a skin care product with comfortable feel. This scheme has a complex formulation system containing various emulsifiers, preservatives, and pH adjusters, which not only has a complicated process and high production cost, but also may increase the burden and allergy risk of the skin. In addition, the different active ingredients (such as ferulic acid) in the formulation may have conflicting pH requirements, causing some components to be inactivated and affecting the overall efficacy.

[0006] However, despite these technical attempts, azelaic acid still exists mostly in the form of insoluble solid particles in the final product, which not only affects the skin feel but also may reduce the bioavailability; on the other hand, some components in the eutectic solvent system used may still cause irritation to some sensitive skin, so azelaic acid has not yet fully exerted its repair efficacy and user experience. Therefore, there is an urgent need for a new technical solution that can fundamentally solve the solubility of azelaic acid, achieve stable loading at high concentrations, and at the same time has a simple process, mild ingredients, and can effectively reduce skin irritation. SUMMARY

[0007] [TECHNICAL SOLUTION] In order to solve the above problems, the application selects octanoyl glycine, farnesol and menthol as the compatible molecules, and forms a stable liquid supramolecular body by spontaneous recognition of DES technology and azelaic acid. The system significantly improves the solubility and stability of azelaic acid, and at the same time, gives the system excellent soothing and non-irritating performance, and widens the application range of high-concentration azelaic acid in various cosmetic and external drug formulations.

[0008] The first object of the application is to provide a preparation method of an azelaic acid eutectic solubilization system, comprising the following steps: (a) mixing octanoyl glycine, farnesol and menthol, and reacting under heating and stirring conditions to form a first homogeneous liquid system; (b) adding azelaic acid to the first homogeneous liquid system prepared in step (a), and mixing under heating and stirring conditions to obtain a second homogeneous liquid system containing azelaic acid.

[0009] In an embodiment of the application, in step (a), the molar ratio of octanoyl glycine, farnesol and menthol is (2-3): (1-2): 1.

[0010] Preferably, in step (a), the molar ratio of octanoyl glycine, farnesol and menthol is 2:1:1, or 3:2:1, or 2.5:1.5:1.

[0011] In an embodiment of the application, step (a) is carried out under inert gas protection.

[0012] In an embodiment of the application, in step (a), the stirring rate is 400-700 rpm, the temperature is 75-90℃, and the reaction time is 1-5 h.

[0013] Preferably, the stirring rate is 500-600 rpm.

[0014] Preferably, the temperature is 80-90℃.

[0015] Preferably, the reaction is carried out for 2-4 h.

[0016] In an embodiment of the application, in step (b), the stirring rate is 300-500 rpm, the temperature is 60-70℃, and the reaction time is 1-3 h.

[0017] In an embodiment of the application, in step (a), after mixing, the system is cooled to room temperature.

[0018] The second object of the application is to provide an azelaic acid eutectic solubilization system prepared according to the above method.

[0019] In an embodiment of the present application, the mass content of azelaic acid in the system is 10-20 wt%.

[0020] A third object of the present application is to provide the use of the azelaic acid eutectic compounding system in the preparation of daily chemicals or medicines.

[0021] In an embodiment of the present application, the daily chemicals include cosmetics, shampoos, hair conditioners, body washes.

[0022] In an embodiment of the present application, the cosmetics include serums, essences, sprays, skin care foams, lotions, shampoos.

[0023] A fourth object of the present application is to provide a cosmetic containing the azelaic acid eutectic compounding system.

[0024] In an embodiment of the present application, the dosage form of the cosmetic includes but is not limited to: serum oil, serum, spray, lotion, cream, mask, shampoo, skin care foam.

[0025] A fifth object of the present application is to provide a medicine for acne treatment containing the azelaic acid eutectic compounding system.

[0026] In an embodiment of the present application, the dosage form of the medicine includes but is not limited to: gel, spray, liquid medicine, cream, ointment or patch.

[0027] A sixth object of the present application is to provide a method for synergistically solubilizing azelaic acid and reducing its irritation using capryloyl glycine, bisabolol and menthol, which comprises mixing capryloyl glycine, bisabolol and menthol and heating to form a liquid eutectic system, and dissolving azelaic acid in the liquid eutectic system.

[0028] [Advantages] The present application constructs a ternary deep eutectic solvent (DES) supramolecular system with capryloyl glycine as the hydrogen bond acceptor and bisabolol and menthol as the hydrogen bond donors, and loads high-concentration azelaic acid, achieving the following outstanding advantages: 1. The present application successfully breaks through the technical bottleneck of the extremely low solubility of azelaic acid in conventional water-oil systems (usually <1%). The present application can achieve stable loading of azelaic acid at a high mass fraction of 13% to 19%, and the system remains uniform and transparent in liquid state at room temperature and after experiencing high and low temperature cycles, without any crystal precipitation, fundamentally solving the problems of formulation instability and physical irritation caused by the presence of solid particles. The obtained DES system has excellent anti-dilution ability, even if diluted with water to a practical concentration of 10% azelaic acid, it still does not separate or precipitate active substances, providing a solid foundation for flexible formulation and skin feel adjustment.

[0029] 2. This invention eliminates the physical friction irritation to the skin caused by azelaic acid solid crystal particles in traditional formulations through DES. Simultaneously, the system itself contains bisabolol, capryloyl glycine, and other components that provide immediate soothing effects, counteracting and reducing the chemical irritation of azelaic acid, significantly improving skin tolerance and user comfort. Experimental data shows that placing azelaic acid in this DES system greatly enhances its soothing function (indicated by hyaluronidase inhibition rate). At the same test concentration (e.g., 1% azelaic acid), the inhibition rate of the DES system of this invention reaches up to 67.2%. Detailed Implementation

[0030] The preferred embodiments of the present invention are described below. It should be understood that the embodiments are for better explanation of the present invention and are not intended to limit the present invention.

[0031] Test method: 1. High and low temperature cycling test: The DES system was frozen at -5°C and then transferred to a constant temperature of 40°C to completely dissolve. This freeze-dissolve process was defined as one complete cycle. A total of 15 cycles were repeated. After each dissolution, the system state was carefully observed to confirm that it could maintain a stable and homogeneous liquid state without any solid precipitation or phase separation.

[0032] 2. Hyaluronidase inhibition rate test (1) Treatment of control materials and test samples Sample group: Dilute with pure water to a sample concentration of 5%; Positive control (dipotassium glycyrrhizate, purity >98%): diluted with water to a concentration of 3%; Negative control: pure water.

[0033] (2) Experimental Operation Procedures Set up a sample group, a sample background group, a solvent group, and a solvent background group. Each group should have 3 replicates. Add different reagent solutions to each of the four groups, shake well, and let stand at room temperature for 30 min for color development. Measure the absorbance value at a wavelength of 528 nm using a UV spectrophotometer.

[0034] (3) Calculation formula Hyaluronidase inhibition rate (%) = [1 - (CD) ÷ (AB)] × 100 In the formula: A - absorbance of the reaction solution without sample; B - absorbance of the reaction solution without sample and enzyme; C - absorbance of the reaction solution containing sample and enzyme; D - absorbance of the reaction solution containing sample and without enzyme.

[0035] 3. Skin lactic acid sting test Refer to the skin lactic acid stinging test in the group standard T / BDCA 021-2022.

[0036] 4. Skin pimple volume test Refer to the skin comedone volume test in the group standard T / GDCDC 023-2022.

[0037] Raw materials used in the examples: Azelaic acid: Particle size 500 nm~100 μm, particle size has no effect, the particle size selected in the examples and comparative examples is 30 μm, commercially available; Capryloylglycine: CAS 14246-53-8; Bisabolol: CAS515-69-5; Menthol: CAS 89-78-1; White willow bark extract: purchased from Xi'an Lvtian Biotechnology Co., Ltd.; Sodium EDTA2: 99%, purchased from Shanghai Yuanye Biotechnology Co., Ltd.; Centella asiatica extract: purchased from Xi'an Lvtian Biotechnology Co., Ltd.; Unless otherwise specified, the percentages mentioned in the examples and comparative examples refer to mass percentages.

[0038] Example 1: A method for preparing a high-concentration azelaic acid liquid DES system In this example, the amounts of 0.02 mol capryloylglycine, 0.01 mol bisabolol, 0.01 mol menthol, and 0.01 mol azelaic acid are determined using the following steps: (1) Accurately weigh capryloylglycine, bisabolol and menthol and place them in a sealed reaction vessel. Purge with nitrogen for protection and heat continuously at 80°C and 550 rpm for 3 h with stirring. After heating, allow to cool naturally to room temperature (25°C) to form a homogeneous, clear, non-layered transparent oily liquid capryloylglycine / bisabolol / menthol DES system.

[0039] (2) Add azelaic acid powder to the liquid capryloyl glycine / bisabolol / menthol DES system in step (1) and stir at 60°C and 400 rpm for 1 h to obtain a homogeneous and transparent liquid system.

[0040] The liquid system obtained in step (2) has a mass fraction of 19% azelaic acid; when it is diluted with water to a mass concentration of 10% azelaic acid, no phase separation occurs and no solid is precipitated. The liquid system obtained in step (2) and the system diluted with water were subjected to high and low temperature cycling tests (at -5℃). o C and 40 oAfter being circulated at C for 15 cycles, both systems were able to maintain a stable, homogeneous liquid state without any solid precipitation.

[0041] Example 2: A method for preparing a high-concentration azelaic acid liquid DES system In this example, the amounts of capryloylglycine (0.03 mol), bisabolol (0.02 mol), menthol (0.01 mol), and azelaic acid (0.01 mol) are determined using the following steps: (1) Accurately weigh capryloylglycine, bisabolol and menthol and place them in a sealed reaction vessel. Purge with nitrogen for protection and heat continuously at 85°C and 500 rpm for 2 h with stirring. After heating, allow to cool naturally to room temperature (25°C) to form a homogeneous, clear, non-layered transparent oily liquid capryloylglycine / bisabolol / menthol DES system.

[0042] (2) Add azelaic acid powder to the liquid capryloylglycine / bisabolol / menthol DES system in step (1) and stir at 70°C and 300 rpm for 1.5 h to obtain a homogeneous and transparent liquid system.

[0043] The liquid system obtained in step (2) has a mass fraction of 13.51% azelaic acid; when diluted with water to a mass concentration of 10% azelaic acid, no phase separation occurs and no solid precipitates. The liquid system obtained in step (2) and the system diluted with water were subjected to high and low temperature cycling tests (at -5℃). o C and 40 o After being circulated at C for 15 cycles, both systems were able to maintain a stable, homogeneous liquid state without any solid precipitation.

[0044] Example 3: A method for preparing a high-concentration azelaic acid liquid DES system In this example, 0.025 mol of capryloylglycine, 0.015 mol of bisabolol, 0.01 mol of menthol, and 0.01 mol of azelaic acid were used. The specific steps are as follows: (1) Accurately weigh capryloylglycine, bisabolol and menthol and place them in a sealed reaction vessel. Nitrogen gas is introduced for protection, and the mixture is continuously stirred and heated at 75°C and 600 rpm for 4 h. After heating, the mixture is allowed to cool naturally to room temperature (25°C) to form a homogeneous, clear, non-layered transparent oily liquid capryloylglycine / bisabolol / menthol DES system.

[0045] (2) Add azelaic acid powder to the liquid capryloyl glycine / bisabolol / menthol DES system in step (1) and stir at 65°C and 350 rpm for 2 hours to obtain a homogeneous and transparent liquid system.

[0046] The liquid system obtained in step (2) has a mass fraction of 15.9% azelaic acid; when diluted with water to a mass concentration of 10% azelaic acid, no phase separation occurs and no solid precipitates. The liquid system obtained in step (2) was subjected to high and low temperature cycling tests (at -5℃). o C and 40 o After being circulated at C for 15 cycles, both systems were able to maintain a stable, homogeneous liquid state without any solid precipitation.

[0047] To verify the soothing efficacy of the azelaic acid liquid DES system prepared in this invention, a hyaluronidase inhibition rate test was conducted. The systems obtained in Examples 1-3 were diluted to a final azelaic acid concentration of 1.0%, and a propylene glycol dispersion of azelaic acid at the same concentration was used as a comparative example. The results are shown in Table 1: the hyaluronidase inhibition rates of all examples of this invention were significantly higher than those of the conventional formulation comparative example. The hyaluronidase inhibition rate of Example 1 reached as high as 67.2 ± 2.02%, approaching the level of the positive control dipotassium glycyrrhizate. This indicates that by constructing a liquid system, this invention not only achieves high-concentration liquefaction and stable storage of azelaic acid, but also significantly enhances its soothing activity, producing an unexpected synergistic effect.

[0048] Table 1 Hyaluronidase Inhibition Rate Test

[0049] Comparative Example 1 This comparative example replaces capryloylglycine with betaine in Example 1, resulting in the following system formulation: 0.01 mol betaine, 0.01 mol bisabolol, 0.01 mol menthol, and 0.01 mol azelaic acid. All other components remain the same as in Example 1, as detailed below: (1) Accurately weigh betaine, bisabolol and menthol and place them in a sealed reaction vessel. Purge with nitrogen for protection and heat continuously at 80°C and 550 rpm for 3 h with stirring. After heating, allow to cool naturally to room temperature (25°C) to form a homogeneous, clear, non-layered transparent oily liquid betaine / bisabolol / menthol DES system.

[0050] (2) Add azelaic acid powder to the liquid betaine / bisabolol / menthol DES system in step (1) and stir at 60°C and 400 rpm for 1 h to obtain a homogeneous and transparent liquid system.

[0051] Compared with Example 1, by changing the octanoylglycine in the system to betaine, a homogeneous, clear, and non-layered transparent oily liquid was obtained after heating and stirring.

[0052] Subsequently, the liquid system obtained in step (2) and the system diluted with water were subjected to high and low temperature cycling tests (at -5℃). o C and 40 o (After being stored in a C-shaped cycle for 15 times), solids eventually precipitated, making it impossible to maintain a homogeneous system.

[0053] Comparative Example 2 This comparative example replaces octanoylglycine with propylene glycol in Example 1, resulting in a system formulation of 0.01 mol propylene glycol, 0.01 mol bisabolol, 0.01 mol menthol, and 0.01 mol azelaic acid, with the other components remaining the same as in Example 1, as detailed below: Accurately weigh propylene glycol, bisabolol, and menthol, and place them in a sealed reaction vessel. Purge with nitrogen for protection, and heat continuously at 80°C and 550 rpm for 3 hours with stirring. After heating, allow to cool naturally to room temperature (25°C).

[0054] Compared to Example 1, changing the octanoylglycine in the system to propylene glycol did not yield a homogeneous and transparent liquid system; the system was a solid-liquid mixture and could not be used to dissolve azelaic acid.

[0055] Comparative Example 3 This comparative example replaces bisabolol with L-proline in Example 1, adjusting the system formulation to 0.01 mol of capryloyl glycine, 0.01 mol of L-proline, 0.01 mol of menthol, and 0.01 mol of azelaic acid, with other components remaining the same as in Example 1, as detailed below: Accurately weigh capryloylglycine, L-proline, and menthol, and place them in a sealed reaction vessel. Purge with nitrogen for protection, and heat continuously at 80°C and 550 rpm for 3 hours with stirring. After heating, allow to cool naturally to room temperature (25°C).

[0056] Compared to Example 1, changing bisabolol to L-proline in the system did not yield a homogeneous and transparent liquid system; the system was a solid-liquid mixture and could not be used to dissolve azelaic acid.

[0057] Comparative Example 4 This comparative example replaces bisabolol with oxalic acid in Example 1, adjusting the system formulation to 0.01 mol capryloyl glycine, 0.01 mol oxalic acid, 0.01 mol menthol, and 0.01 mol azelaic acid, with the other components remaining the same as in Example 1, as detailed below: Accurately weigh capryloylglycine, oxalic acid, and menthol, and place them in a sealed reaction vessel. Purge with nitrogen for protection, and heat continuously at 80°C and 550 rpm for 3 hours with stirring. After heating, allow to cool naturally to room temperature (25°C).

[0058] Compared to Example 1, changing bisabolol to oxalic acid in the system does not yield a homogeneous and transparent liquid system; the system is a solid-liquid mixture and cannot be used to dissolve azelaic acid.

[0059] Comparative Example 5 This comparative example replaces menthol with lactic acid in Example 1, adjusting the system formulation to 0.02 mol capryloyl glycine, 0.01 mol bisabolol, 0.01 mol lactic acid, and 0.01 mol azelaic acid. The specific steps are as follows: Accurately weigh capryloylglycine, bisabolol, and lactic acid, and place them in a sealed reaction vessel. Purge with nitrogen for protection, and heat continuously at 80°C and 550 rpm for 3 hours with stirring. After heating, allow to cool naturally to room temperature (25°C).

[0060] Compared to Example 1, changing menthol to lactic acid in the system does not yield a homogeneous and transparent liquid system; the system is a solid-liquid mixture and cannot be used to dissolve azelaic acid.

[0061] Comparative Example 6 This comparative example replaces menthol with nicotinamide in Example 1, adjusting the system formulation to 0.02 mol capryloyl glycine, 0.01 mol bisabolol, 0.01 mol nicotinamide, and 0.01 mol azelaic acid. The specific steps are as follows: Accurately weigh capryloylglycine, bisabolol, and nicotinamide and place them in a sealed reaction vessel. Purge with nitrogen for protection and heat continuously at 80°C and 550 rpm for 3 hours with stirring. After heating, allow to cool naturally to room temperature (25°C).

[0062] Compared to Example 1, changing menthol to nicotinamide in the system did not yield a homogeneous and transparent liquid system; the system was a solid-liquid mixture and could not be used to dissolve azelaic acid.

[0063] Comparative Example 7 The amount of bisabolol in Example 1 was adjusted to 0.025 mol, while other aspects remained the same as in Example 1, and the product was obtained.

[0064] The results showed that increasing the amount of bisabolol did not yield a homogeneous and transparent liquid system, and therefore could not be used to dissolve azelaic acid.

[0065] Comparative Example 8 The amount of menthol in Example 1 was adjusted to 0.02 mol, while other parameters remained the same as in Example 1, and the product was obtained.

[0066] The results showed that increasing the amount of menthol did not produce a homogeneous and transparent liquid system, and therefore could not be used to dissolve azelaic acid.

[0067] Example 4: Application in cosmetics The soluble azelaic acid liquid system prepared in Example 1 was used in the preparation of cosmetics, as detailed below: Add ingredients 1-3 and 6 to the main cup and dissolve them evenly. Heat to 75°C. Cool down to 45℃, add raw materials No. 4, 5, and 7, stir well, and the preparation is complete.

[0068] Stability testing was conducted, and the results showed that the serum's stability was up to standard.

[0069] Table 2 Serum Formula Table

[0070] Skin lactic acid stinging test results showed that Table 3 Results of Skin Lactic Acid Sting Test

[0071] Table 4 Results of Skin Acne Volume Test

[0072] Comparative Example 9 According to the formula of the serum in Table 1, the soluble azelaic acid liquid system of Example 1 was replaced with 5% w / w azelaic acid, 10.6% w / w capryloyl glycine, 6% w / w bisabolol, and 4% w / w menthol, as shown in Table 5 below to prepare the serum: The preparation process is as follows: Add ingredients 1-3 and 6 to the main cup and dissolve them evenly. Heat to 75°C. Cool down to 45℃, add raw materials 4-8 and 10, stir well, and the preparation is complete.

[0073] Stability testing revealed that the serum failed stability tests, with solids precipitating out.

[0074] Table 5 Serum Formula Table

[0075] Although the present invention has been disclosed above with reference to preferred embodiments, it is not intended to limit the present invention. Any person skilled in the art can make various modifications and alterations without departing from the spirit and scope of the present invention. Therefore, the scope of protection of the present invention should be determined by the claims.

Claims

1. A method for preparing an azelaic acid eutectic solubilization system, characterized in that, Includes the following steps: (a) Capryloyl glycine, bisabolol and menthol are mixed and reacted under heating and stirring conditions to form a first homogeneous liquid system; (b) Azelaic acid is added to the first homogeneous liquid system obtained in step (a), and mixed under heating and stirring conditions to obtain a second homogeneous liquid system containing azelaic acid; wherein, The molar ratio of capryloylglycine, bisabolol and menthol is (2~3):(1-2):

1.

2. The preparation method according to claim 1, characterized in that, Step (a) is carried out under inert gas protection.

3. The preparation method according to claim 1, characterized in that, In step (a), the stirring rate is 400~700 rpm, the temperature is 75~90℃, and the reaction time is 1~5 h; Preferably, the stirring rate is 500-600 rpm; preferably, the temperature is 80-90℃; preferably, the reaction time is 2-4 h.

4. The preparation method according to claim 1, characterized in that, In step (b), the stirring rate is 300-500 rpm, the temperature is 60-70℃, and the reaction time is 1-3 h.

5. The preparation method according to claim 1, characterized in that, In step (a), after mixing, the system is cooled to room temperature.

6. The azelaic acid eutectic compatibilization system prepared by the method according to any one of claims 1 to 5.

7. The use of the azelaic acid eutectic compatibilizing system according to claim 6 in the preparation of daily chemical products or pharmaceuticals; Preferably, the daily chemical products include cosmetics, shampoos, conditioners, and shower gels; Preferably, the cosmetics include serums, essences, sprays, skin foams, lotions, and shampoos.

8. A cosmetic product, characterized in that, Contains the azelaic acid eutectic compatibilizer system as described in claim 6; Preferably, the dosage forms of the cosmetics include, but are not limited to: essential oils, serums, sprays, lotions, creams, masks, shampoos, and skin foams.

9. A medicine for treating acne, characterized in that, Contains the azelaic acid eutectic compatibilizer system as described in claim 6; Preferably, the dosage form of the drug includes, but is not limited to: gel, spray, liquid, cream, ointment or patch.

10. A method for synergistically solubilizing azelaic acid and reducing its irritation using capryloylglycine, bisabolol, and menthol, characterized in that, The method involves mixing capryloylglycine, bisabolol, and menthol and heating them to form a liquid eutectic system, and then dissolving azelaic acid in the liquid eutectic system.

Citation Information

Patent Citations

  • Eutectic of azelaic acid and organic alkali as well as preparation method and application of eutectic

    CN112624918A

  • Preparation and application of cyclodextrin-coated azelaic acid oil-control skin-care product

    CN120346136A