High-efficiency acne-removing and mark-eliminating composition and preparation method thereof

Abstract

The invention relates to the technical field of skin care products, and particularly discloses an efficient acne-removing and mark-eliminating composition and a preparation method thereof. The high-efficiency acne-removing and mark-eliminating composition comprises rosa damascena water, a pelargonium graveolens extract, CalmYangPro and water-soluble azelaic acid, and all the components cooperate to realize a closed loop of'acne removal, mark fading and recurrence prevention '. Wherein the water-soluble azelaic acid is prepared from azelaic acid, hydroxypropyl cyclodextrin, disodium hydrogen phosphate, methyl cyclodextrin, Arabic gum and maltodextrin through a specific process, the water solubility of the azelaic acid can be improved, and the irritation can be reduced. Meanwhile, the invention discloses a preparation method of the composition and an efficient acne-removing and mark-eliminating cosmetic prepared from the composition. The product has the advantages of being good in stability, remarkable in acne removing and mark eliminating effect and safe to use.

Description

Technical Field

[0001] This invention relates to the field of skincare technology, and in particular to a highly effective acne-removing and acne-scar-fading composition and its preparation method. Background Technology

[0002] "Pimples" is the common name for acne vulgaris, also known as "zits," "acne," or "blackheads." It is a skin condition caused by the blockage and inflammation of hair follicles and sebaceous glands. Although the disease usually does not affect the patient's overall health, it often occurs on exposed areas such as the face. If not treated in time, it may leave scars that affect appearance, thus often causing significant psychological stress for patients.

[0003] With acne (commonly known as "pimples") prevalent among teenagers and young adults, and acne scars often becoming a core cause of appearance anxiety, acne treatment and scar fading products have already generated enormous consumer demand. Azelaic acid (also known as azelaic acid) is a complex molecule with multiple activities. As clinical research continues, its anti-inflammatory, anti-infective, and antibacterial effects have been gradually discovered and confirmed, and it is currently widely used in the treatment of acne, melanoma, melasma, rosacea, hyperpigmentation, and sclerosis. Especially in the field of acne treatment and scar fading, azelaic acid shows great potential—as a highly effective acne-fighting ingredient, it can simultaneously address acne-prone skin by inhibiting the activity of Propionibacterium acnes, reducing sebum secretion, and inhibiting tyrosinase activity, thus addressing both acne-fighting and scar-fading effects. However, azelaic acid has poor water solubility, which presents numerous technical challenges for its application in cosmetics. Firstly, when added to cosmetics, it exhibits poor stability, easily crystallizing and resulting in a rough texture that severely affects the skin's feel. Secondly, to achieve the desired acne-reducing and scar-fading effects, the concentration of azelaic acid typically needs to be above 10%, at which point the product becomes highly acidic, significantly increasing irritation and potentially damaging the skin's surface. These issues collectively limit the widespread application of azelaic acid in the cosmetics industry.

[0004] In response to the aforementioned technologies, the inventors believe that a composition should be developed that can solve the application problems of azelaic acid, and has good acne removal and scar fading effects, fast onset of action, and is skin-friendly. Summary of the Invention

[0005] To address the technical deficiencies of existing technologies, this application provides a highly effective acne-removing and scar-fading composition and its preparation method.

[0006] In the first aspect, this application provides a highly effective acne-removing and scar-fading composition, which adopts the following technical solution: A highly effective acne-removing and scar-fading composition, comprising, by weight percentage: 5%–12% of Rosa damascena flower water, 0.01%–0.05% of Geranium wilfordii extract, 0.1%–0.5% of CalmYangPro, and 15%–25% of water-soluble azelaic acid as described in any one of claims 1-2; wherein CalmYangPro comprises Centella asiatica extract, Polygonum cuspidatum root extract, Scutellaria baicalensis root extract, tea extract, Glycyrrhiza glabra extract, Chamomile extract, and Rosmarinus officinalis leaf extract.

[0007] By employing the above technical solution, water-soluble azelaic acid, relying on its inclusion structure, exerts its core acne-removing effect by inhibiting Propionibacterium acnes and reducing sebum secretion. Rosa damascena flower water soothes and moisturizes, relieving skin redness and potential irritation from azelaic acid. Geranium extract assists in anti-inflammation and accelerates acne reduction. CalmYangPro regulates oil balance and strengthens the skin barrier to prevent recurrence. With the synergistic effect of these ingredients, the product not only rapidly reduces acne (41.86% improvement rate in facial blackheads within 14 days) but also effectively fades acne scars (over 90% of users experience scar improvement within 28 days). Moreover, only 1-3 people experience acne recurrence after 28 days. This solves the problems of traditional acne products having single efficacy and easy recurrence, while also being low in irritation and suitable for various skin types.

[0008] Preferably, the water-soluble azelaic acid comprises, by mass percentage: 55%–65% azelaic acid, 18%–22% hydroxypropyl cyclodextrin, 10%–14% disodium hydrogen phosphate, 5%–7% methyl cyclodextrin, 0.8%–1.2% gum arabic, and 0.8%–1.2% maltodextrin.

[0009] By adopting the above technical solution, the content of the core active ingredient azelaic acid is sufficient, laying the foundation for subsequent acne-removing effects. Hydroxypropyl cyclodextrin and methyl cyclodextrin form a complex inclusion system, effectively overcoming the limitation of traditional azelaic acid's poor water solubility and significantly improving its water solubility. Disodium hydrogen phosphate can stably regulate the pH of the system, avoiding the impact of environmental acidity and alkalinity fluctuations on product performance. Gum arabic and maltodextrin respectively optimize the product's dispersibility and powdering properties, preventing clumping during use. Ultimately, this water-soluble azelaic acid does not precipitate even after prolonged storage at 25% concentration in environments with normal temperature, 45℃ high temperature, and 5℃ low temperature. At the same time, the inclusion structure reduces the irritation of azelaic acid, expanding its application range in sensitive skin products.

[0010] Preferably, the azelaic acid has a particle size of less than or equal to 50 μm.

[0011] By adopting the above technical solution, smaller particle size can increase the contact area between azelaic acid and cyclodextrin, further improving the inclusion efficiency and uniformity, avoiding a rough feeling when applied due to excessively large particles. At the same time, finer particles also help the skin absorb the active ingredients, enhancing the acne-removing effect of azelaic acid, thus optimizing both the skin feel and efficacy of the product.

[0012] Preferably, the water-soluble azelaic acid is prepared by the following method: S1: Disodium hydrogen phosphate is added to purified water and stirred to dissolve. The pH is adjusted to 6.5-7.5 to prepare a buffer solution. S2: Heat the buffer solution to 55°C, then add hydroxypropyl cyclodextrin and methyl cyclodextrin sequentially and stir until homogeneous; S3: Add azelaic acid in three portions at 55℃, with a 15-minute interval between each addition. After each addition, sonicate and stir until the system meets the specific conditions. S4: Cool to 40℃, then add gum arabic and maltodextrin and stir to obtain a liquid inclusion complex; S5: Water-soluble azelaic acid is prepared by removing water from the liquid inclusion complex by spray drying or freeze drying to obtain a solid inclusion complex.

[0013] By adopting the above technical solution, the buffer solution in S1 provides a stable chemical environment for subsequent reactions; the specific temperature in S2 ensures that the cyclodextrin is fully dissolved and has a suitable viscosity; the fractional addition and ultrasonic stirring in S3 prevent azelaic acid from clumping and ensure thorough and uniform inclusion (the system is pale yellow and transparent with turbidity ≤5 NTU); the cooling operation in S4 protects the inclusion complex structure; and the two drying methods in S5 can be selected according to needs. This allows for the rapid acquisition of solid products with moisture content ≤3% (spray drying undersize yield ≥95%), and is also adaptable to heat-sensitive scenarios. The overall process is convenient to operate, requires no complex equipment, can achieve industrial production, and can stably control product quality, avoiding performance fluctuations between batches.

[0014] Secondly, this application provides a method for preparing a highly effective acne-removing and scar-fading composition, employing the following technical solution: A method for preparing a highly effective acne-removing and scar-fading composition includes the following steps: S1: Add 70% of the total amount of deionized water to the mixing container, stir at 150-200 rpm, slowly add water-soluble azelaic acid, and stir for 15-20 minutes until completely dissolved; S2: Add geranium extract and CalmYangPro in sequence, stirring at 250-300 rpm for 10-15 minutes after each addition; S3: Slowly pour in rose damascena flower water, stirring at 200-250 rpm for 15-20 minutes. S4: Add the remaining 30% deionized water and stir at 150-200 rpm for 10-15 minutes to obtain a highly effective acne-removing and scar-fading composition.

[0015] By adopting the above technical solution, the 70% water volume and appropriate rotation speed in S1 ensure that the water-soluble azelaic acid is fully dissolved without excessive bubbles, the higher rotation speed in S2 accelerates the dispersion of the extract and avoids uneven local concentration, the rotation speed in S3 balances the fusion effect and system stability, and the addition of water in S4 adjusts the concentration. The overall process does not require complex equipment, and the feeding sequence and rotation speed control ensure uniform mixing of components without damaging the active structure. It can be mass-produced and ensures consistent batch quality.

[0016] Thirdly, this application provides a highly effective acne-removing and acne-scar-fading cosmetic product, which adopts the following technical solution: A highly effective acne-removing and acne-scar-fading cosmetic product includes the above-mentioned highly effective acne-removing and acne-scar-fading composition and a cosmetic base.

[0017] By adopting the above technical solution, the active composition with acne-removing and scar-fading effects is combined with a cosmetic matrix, overcoming the limitations of simple liquid compositions that are prone to dripping and have a thin skin feel. This allows the product to be transformed into a form that is more in line with daily skincare habits. At the same time, the matrix ingredients supplement the composition's shortcomings in moisturizing, skin feel adjustment, and shelf life extension, so that the product retains its core acne-removing and scar-fading effects while meeting consumers' basic needs for skincare product experience, thus expanding the product's practical application scenarios.

[0018] Preferably, the acne-removing and scar-fading cosmetic is a face cream or lotion.

[0019] By adopting the above technical solutions, face cream and lotion are well-known and frequently used skin care product formulations that do not require additional learning of usage methods, thus lowering the acceptance threshold for consumers. Face cream has stronger occlusive properties and can form a protective film on the skin surface, making it suitable for dry seasons or dry skin types and prolonging the action time of active ingredients. Lotion has a lighter texture and is less likely to cause greasiness, making it suitable for oily, combination skin types or summer use. The two forms cover different skin types and seasonal needs, improving the market adaptability of the products.

[0020] Preferably, the cosmetic matrix includes emulsifiers, emollients, moisturizers, thickeners, preservatives, and deionized water.

[0021] By adopting the above technical solution, each matrix component has a clear division of labor and works synergistically: the emulsifier solves the problem of oil-water component blending and avoids product separation; the emollient improves skin dryness and enhances the smoothness during application; the moisturizer replenishes skin moisture and relieves possible dryness and discomfort in acne-prone skin; the thickener adjusts the product viscosity to ensure stable form without disintegration; the preservative inhibits microbial growth and extends the product's shelf life; and deionized water, as a solvent, provides a uniform dispersion medium for all components, ultimately allowing the matrix and active composition to blend perfectly, comprehensively improving the product's stability and user experience without affecting the acne-removing and scar-fading efficacy.

[0022] Preferably, the emulsifier is one or more of cetearyl alcohol, cetearyl glucoside, glyceryl stearate, PEG-100 stearate, potassium cetearyl phosphate, and cetearyl alcohol polyether-25.

[0023] By adopting the above technical solutions, these emulsifiers have excellent compatibility with the core ingredient, water-soluble azelaic acid, and can effectively disperse azelaic acid particles, avoiding problems such as crystallization and rough texture during product storage. At the same time, they have strong emulsification stability, ensuring that face creams or lotions do not separate after long-term storage. Furthermore, these emulsifiers themselves have low irritation and will not increase the burden on the skin, which is in line with the product's pursuit of gentleness, making them especially suitable for acne-prone skin that may have sensitive issues.

[0024] Preferably, the emollient is one or more selected from caprylic / capric triglyceride, polydimethylsiloxane, ethylhexyl palmitate, isohexadecane, and polydimethylsiloxane; The moisturizer is one or more of propylene glycol or glycerin; The preservative is one or more of phenoxyethanol, 1,2-hexanediol and chlorphenesin.

[0025] By adopting the above technical solutions, the selected moisturizer has a light texture and is easily absorbed by the skin. It can form a breathable protective film on the skin surface, providing moisturization without producing a greasy feeling, which meets the refreshing skin feel requirement of acne treatment products. Propylene glycol and glycerin are safe ingredients with clear moisturizing effects, which can effectively lock in skin moisture and improve the dryness that may be accompanied by abnormal sebum secretion in acne-prone skin. The selected preservatives have a broad antibacterial spectrum, which can effectively inhibit the growth of bacteria and fungi, ensuring that the product is safe and does not deteriorate within the shelf life. They are also low in irritation and have been verified to have no adverse reactions through human skin patch testing, further ensuring the safety of product use. Consumers can enjoy the acne-removing and scar-fading effects without worrying about skin irritation or product deterioration.

[0026] In summary, this application has the following beneficial effects: 1. This application utilizes multiple ingredients to synergistically construct a closed loop of "acne treatment - fading marks - preventing recurrence." The core principle is the precise synergy of "water-soluble azelaic acid + auxiliary ingredients": water-soluble azelaic acid encapsulated with hydroxypropyl cyclodextrin and methyl cyclodextrin not only solves the problems of traditional azelaic acid being difficult to dissolve and irritating, but also works efficiently—reducing bacterial infection by inhibiting the activity of Propionibacterium acnes, reducing sebum secretion by inhibiting 5α-reductase (preventing pore blockage from the source), and simultaneously inhibiting tyrosinase activity to reduce melanin production (aiding in fading acne marks); the accompanying Rosa damascena flower water can soothe acne redness and neutralize the mild irritation of azelaic acid, geranium extract accelerates inflammation reduction, and CalmYangPro (containing ingredients such as Centella asiatica) regulates oil balance, repairs the skin barrier, and prevents acne recurrence. The ingredients form a synergistic closed loop rather than acting alone, ultimately achieving a 41.86% improvement rate in facial acne count and a 17.18% improvement rate in red area of ​​acne lesions within 14 days. The number of people with acne scars improved within 28 days exceeded 90%, and the acne recurrence rate after 28 days was only 3.3% to 10%, solving the pain points of traditional products such as "incomplete acne removal, easy recurrence, and no effect on fading scars".

[0027] 2. This application overcomes the limitations of azelaic acid application through cyclodextrin inclusion technology and process optimization: the cyclodextrin complex inclusion technology allows azelaic acid to be stably dissolved in a water-based system at a high concentration of 25% (no precipitation was observed after 3 months at room temperature, 1 month at 45℃, and 1 month at 5℃), and the inclusion structure reduces its acidic irritation, making it suitable for sensitive skin; simultaneously, the particle size of azelaic acid is controlled to ≤50μm, and combined with the "partial addition + ultrasonic stirring" process during preparation, the contact area between azelaic acid and cyclodextrin is increased, improving the uniformity of inclusion and skin absorption rate, allowing the active ingredients to act quickly on acne sites; the emulsifiers (such as cetearyl alcohol) suitable for subsequent cosmetic matrix further ensure that azelaic acid is evenly dispersed in creams / lotions, avoiding a grainy feel and maintaining long-term product stability. These technological optimizations guarantee the activity of azelaic acid from the entire "dissolution-stabilization-absorption" chain, ensuring the continuous performance of highly effective acne-removing and scar-fading effects, significantly superior to ordinary azelaic acid or single-component systems. Detailed Implementation

[0028] The present application will be further described in detail below with reference to the embodiments.

[0029] Cetearyl alcohol and cetearyl glucoside were purchased from SEPPIC SA. Glyceryl stearate and PEG-100 stearate were purchased from Croda Chemicals Ltd., UK. Potassium cetyl phosphate was purchased from Suzhou Yuansuji Chemical Industry Co., Ltd. Cetearyl alcohol polyether-25 was purchased from Croda Singapore Pte Ltd. Caprylic / capric triglycerides and ethylhexyl palmitate were purchased from KL-KEPONG OLEOMASSDN BHD. Polydimethylsiloxane investment Dow (Zhangjiagang) Holding Co., Ltd.; Isohexadecane was purchased from Idemitsu Kosan Co., Ltd., Japan; Propylene glycol was purchased from SKPICGLOBAL CO.,LTD. Xanthan gum was purchased from DSM Runbang (Inner Mongolia) Biotechnology Co., Ltd. Polyacrylate crosspolymer-6 was purchased from SEPPIC SA; The water from the Turkish rose was purchased from Liangdang Qinxiangyi Rose Biotechnology Co., Ltd. Hydroxypropyl cyclodextrin and methyl cyclodextrin were purchased from Shandong Binzhou Zhiyuan Biotechnology Co., Ltd. Disodium hydrogen phosphate was purchased from Xi'an Xinfengda Pharmaceutical Excipients Co., Ltd. The gum arabic was purchased from Guangzhou Zhuoxin Biotechnology Co., Ltd. Maltodextrin was purchased from Dongguan Xinyao Biotechnology Co., Ltd. Phenoxyethanol, 1,2-hexanediol, and chlorophenoxyether were purchased from Tor Specialty Chemicals (Zhenjiang) Co., Ltd. Geranium geranium extract was purchased from Anhui Yinfeng Pharmaceutical Co., Ltd.; Polydimethylsiloxane was purchased from Dow (Zhangjiagang) Investment Co., Ltd. CalmYang Pro was purchased from BioSpectrum, Inc. CalmYang Pro comprises Centella asiatica extract, Polygonum cuspidatum root extract, Scutellaria baicalensis root extract, tea extract, Glycyrrhiza glabra extract, Chamomile extract, Rosmarinus officinalis leaf extract, butylene glycol, and water in a mass ratio of 5:2:2:1:1:0.5:0.5:50:38.

[0030] Witch hazel water was purchased from Hubei Yuanmeng Biotechnology Co., Ltd. Centella asiatica extract was purchased from Guangxi Changzhou Natural Pharmaceutical Co., Ltd. Bisabolol was purchased from Xi'an Kangnuo Chemical Co., Ltd. Polyquaternium-73 was purchased from Hubei Langbowan Biomedical Co., Ltd. Niacinamide was purchased from Lonza Group in Switzerland.

[0031] Example 1 A water-soluble azelaic acid comprises, by weight percentage: 60% azelaic acid, 20% hydroxypropyl cyclodextrin, 12% disodium hydrogen phosphate, 6% methyl cyclodextrin, 1% gum arabic, and 1% maltodextrin.

[0032] The highly effective acne-removing and scar-fading composition in this embodiment is prepared by the following method: S1 Raw Material Pretreatment: Azelaic acid was pulverized to a particle size ≤50μm using an air jet mill with an inlet pressure of 0.7MPa; hydroxypropyl cyclodextrin and methyl cyclodextrin were dried at 40℃ and -0.09MPa vacuum for 4h to make the moisture content ≤1.5%; anhydrous disodium hydrogen phosphate was passed through a 100-mesh sieve before dissolution.

[0033] Preparation of S2 buffer: Take 2.5 times the total amount of purified water, add disodium hydrogen phosphate at 25℃, stir at 300 rpm for about 15 min until completely dissolved, and test the pH. If pH < 6.5, add 0.1 mol / L sodium hydroxide solution to adjust; if pH > 7.5, add 0.1 mol / L phosphate solution to adjust to pH 6.5-7.5.

[0034] S3 Cyclodextrin Dissolution: Heat the buffer solution to 55℃ (fluctuation ±1℃), first add hydroxypropyl cyclodextrin, stir at 300 rpm for 10 min until transparent, then add methyl cyclodextrin, stir at 55℃ for 5 min, and control the viscosity at 150-200 cP.

[0035] S4 Inclusion reaction: At 55℃, pretreated azelaic acid was added in 3 portions, with an interval of 15 min between each addition. After each addition, 300W sonication was turned on (5s operation + 10s pause, 5 min each time), while stirring at 300 rpm. The inclusion reaction lasted for 60 min until the system was pale yellow and transparent with a turbidity ≤5 NTU.

[0036] Additive S5: Cool to 40°C, add gum arabic, stir at 250 rpm for 15 minutes until dissolved, then add maltodextrin and stir for 10 minutes to make the solid content about 28%.

[0037] S6 Spray Drying: A centrifugal spray dryer is used, with the atomizing disc speed set at 25,000 rpm, the inlet air temperature at 185℃, the outlet air temperature at 78℃, and the feed rate at 4 ml / min. The product moisture content is checked every 30 minutes. If the moisture content exceeds the standard, the feed rate is reduced by 0.5 ml / min until the moisture content is ≤3%.

[0038] S7 Post-processing: The material is sieved through an 80-mesh stainless steel sieve with a vibration frequency of 50Hz to ensure a yield of ≥95% for the undersize material and return the oversize material to the airflow pulverizer; it is then vacuum-sealed in an aluminum-plastic composite bag containing 1g / 100g of food-grade silica gel desiccant at a vacuum degree of -0.08MPa.

[0039] Example 2 A water-soluble azelaic acid comprises, by weight percentage: 65% azelaic acid, 18% hydroxypropyl cyclodextrin, 10% disodium hydrogen phosphate, 5% methyl cyclodextrin, 0.8% gum arabic, and 1.2% maltodextrin.

[0040] The preparation method of water-soluble azelaic acid in this embodiment is the same as that in Example 1.

[0041] Example 3 A water-soluble azelaic acid comprises, by weight percentage: 55% azelaic acid, 22% hydroxypropyl cyclodextrin, 14% disodium hydrogen phosphate, 7% methyl cyclodextrin, 1.2% gum arabic and 0.8% maltodextrin.

[0042] The method for preparing water-soluble azelaic acid in this embodiment is basically the same as that in Example 1, except that step S6 is performed by freeze drying using a freeze dryer.

[0043] Example 4 A highly effective acne-removing and scar-fading composition comprises, by weight percentage: 9% Rosa damascena flower water, 25% azelaic acid (Example 1), 0.02% geranium extract, 0.3% CalmYangPro, and deionized water to 100%.

[0044] The above-mentioned highly effective acne-removing and scar-fading composition is prepared by the following method: S1: Add 70% of the total amount of deionized water to a mixing container, stir at 150 rpm, slowly add water-soluble azelaic acid, and stir for 15 minutes until completely dissolved.

[0045] S2: Add geranium extract and CalmYangPro in sequence, stirring at 250 rpm for 10 minutes after each addition.

[0046] S3: Slowly pour in the Turkish rose water and stir at 200 rpm for 15 minutes.

[0047] S4: Add the remaining 30% deionized water, stir at 150 rpm for 10 minutes to obtain a highly effective acne-removing and scar-fading composition.

[0048] Example 5 A highly effective acne-removing and scar-fading composition comprises, by weight percentage: 5% Rosa damascena flower water, 15% azelaic acid (Example 2), 0.01% geranium extract, 0.1% CalmYangPro, and deionized water to 100%.

[0049] The above-mentioned highly effective acne-removing and scar-fading composition is prepared by the following method: S1: Add 70% of the total amount of deionized water to a mixing container, stir at 200 rpm, slowly add water-soluble azelaic acid, and stir for 20 minutes until completely dissolved.

[0050] S2: Add geranium extract and CalmYangPro in sequence, stirring at 300 rpm for 15 minutes after each addition.

[0051] S3: Slowly pour in the Turkish rose water and stir at 250 rpm for 20 minutes.

[0052] S4: Add the remaining 30% deionized water, stir at 200 rpm for 15 minutes to obtain a highly effective acne-removing and scar-fading composition.

[0053] Example 6 A highly effective acne-removing and scar-fading composition comprises, by weight percentage: 12% Rosa damascena flower water, 20% Azelaic acid (Example 3), 0.05% Geranium geranium extract, 0.5% CalmYangPro, and deionized water to 100%.

[0054] S1: In a mixing container, add 70% of the required amount of deionized water and stir at 180 rpm. Slowly add water-soluble azelaic acid and stir for 18 minutes until completely dissolved.

[0055] S2: Add geranium extract and CalmYangPro in sequence, stirring at 280 rpm for 12 minutes after each addition.

[0056] S3: Slowly pour in the Turkish rose water and stir at 220 rpm for 18 minutes.

[0057] S4: Add the remaining 30% deionized water and stir at 180 rpm for 12 minutes to obtain a highly effective acne-removing and scar-fading composition.

[0058] Comparative Example 1 An acne treatment composition comprising, by weight percentage, 25% of the water-soluble azelaic acid of Example 1 and up to 100% deionized water.

[0059] Comparative Example 2 An acne-removing composition, by weight percentage, comprises 15% azelaic acid, 9% Rosa damascena flower water, 0.02% Geranium geranium extract, 0.3% CalmYangPro, and up to 100% deionized water.

[0060] The azelaic acid used in this comparative example is ordinary azelaic acid.

[0061] Comparative Example 3 An acne-removing composition, by weight percentage, comprises 9% witch hazel water, 25% azelaic acid of Example 1, 0.02% centella asiatica extract, 0.3% bisabolol, and deionized water to 100%.

[0062] Comparative Example 4 An acne-removing composition, by weight percentage, comprises 11% azelaic acid, 0.2% polyquaternium-73, 0.2% bisabolol, 2% niacinamide, and deionized water to 100%.

[0063] The azelaic acid has an average particle size of 4 μm and a sieve passing rate of ≥95.0%.

[0064] Performance testing 1. Product stability test The compositions obtained in Examples 4-6 and Comparative Examples 1-4 were placed in test tubes and placed at room temperature, -18°C and 50°C for 30 days, respectively. The results are shown in Table 1.

[0065] Table 1 Stability Test Results As shown in Table 1, the highly effective acne-removing and scar-fading compositions of Examples 4-6 of the present invention are stable and do not exhibit stratification or crystallization in high or low temperature environments.

[0066] 2. Acne Removal and Scar Fading Test Subjects: 240 women aged 18-35 years with mild to moderate acne on their faces were selected as volunteers. These volunteers were divided into 8 groups, corresponding to the compositions of Examples 4-6, the compositions of Comparative Examples 1-4, and deionized water, respectively. The deionized water group was used as a blank control group.

[0067] Test method: 1. Preparation Phase: Before the experiment begins, volunteers must thoroughly cleanse their faces, ensuring no cosmetics or other acne treatment products are used. Additionally, detailed records of the volunteers' facial acne, including the number, distribution, and shape, will be kept as baseline data for subsequent comparisons.

[0068] 2. Experimental Phase: Each group of volunteers applied their respective sample evenly to the acne-prone areas of their face every morning and evening. Volunteers must strictly adhere to the test sample during the testing period and are strictly prohibited from using any other products with acne-removing effects or that may interfere with the test results.

[0069] During the experiment, volunteers are prohibited from consuming any preparations that may affect or potentially affect test results, such as anti-inflammatory drugs and injectable medications. Volunteers should maintain a regular lifestyle and pay attention to a healthy diet during the experiment.

[0070] Data were recorded on day 0 (D0), day 7 (D7), and day 14 (D14). Specifically, the area of ​​red lesions, the number of facial blackheads, and the skin α value (α value, which is the skin erythrin content and can represent the skin inflammation state) of the acne-prone areas were measured using a VISA instrument. The improvement rate was calculated by comparing the data with that of day 0. The test results are shown in Table 2.

[0071] Continue using the product until day 28 (D28). Record the acne scar removal status on day 7 (D7), day 14 (D14), and day 28 (D28). Significant fading or elimination of acne scars is recorded as effective improvement. Calculate the number of people in each group who have improved on day 7 (D7), day 14 (D14), and day 28 (D28), and record whether volunteers have acne again after 28 days of product use. The test results are shown in Table 3.

[0072] Table 2 Acne Treatment Test Results As shown in Table 2, the highly effective acne-removing and scar-fading compositions of Examples 4-6 exhibit significant acne-removing effects, considerably higher than those of Comparative Examples 1-4. Further analysis reveals that Comparative Example 1 used only water-soluble azelaic acid, indicating that while water-soluble azelaic acid alone can achieve good acne-removing effects, it is still inferior to the highly effective acne-removing and scar-fading composition of this invention. Compared to the highly effective acne-removing and scar-fading composition of Example 4, Comparative Example 2 used ordinary azelaic acid instead of the water-soluble azelaic acid of this invention, resulting in a significant decrease in acne-removing ability. Comparative Example 3 retained water-soluble azelaic acid but replaced other components of the highly effective acne-removing and scar-fading composition of Example 4 with similar substances, also showing a decrease in acne-removing ability, indicating that the synergistic effect of these components is not as strong as the original components. Comparative Example 4, using micron-sized azelaic acid, showed the best acne-removing ability among the comparative examples, but it is still inferior to the highly effective acne-removing and scar-fading composition of this invention.

[0073] It is evident that the synergistic effect among the components of this invention is significant and irreplaceable.

[0074] Table 3. Results of the ink removal test As shown in Table 3, the acne scar removal and blemish-removing compositions of Examples 4-6 of this invention are superior to those of Comparative Examples 1-4 in their ability to eliminate acne scars. The acne scar removal and blemish-removing compositions of this invention can effectively remove blemishes in 7 days, demonstrating high efficiency. Furthermore, by day 28, almost all blemishes are removed, resulting in excellent scar removal effects. Moreover, the probability of acne recurrence after 28 days of use is low, indicating a strong overall effect in removing acne scars.

[0075] For ease of practical use, the highly effective acne-removing and scar-fading composition of the present invention can also replace deionized water with a cosmetic base to prepare a face cream or lotion.

[0076] The cosmetic base includes emulsifiers, emollients, moisturizers, thickeners, preservatives, and deionized water.

[0077] The emulsifier is preferably one or more of the following, which have better compatibility with azelaic acid: cetearyl alcohol, cetearyl glucoside, glyceryl stearate, PEG-100 stearate, potassium cetyl phosphate, and cetearyl alcohol polyether-25.

[0078] The emollient is preferably one or more of caprylic / capric triglyceride, polydimethylsiloxane, ethylhexyl palmitate, isohexadecane, and polydimethylsiloxane.

[0079] The moisturizer is preferably one or more of propylene glycol or glycerin.

[0080] The preservative is preferably one or more of phenoxyethanol, 1,2-hexanediol and chlorphenesin.

[0081] The thickener is preferably one or more of xanthan gum or polyacrylate crosslinker-6.

[0082] Application Example 1 A highly effective acne-removing and scar-fading face cream comprises the following ingredients by weight percentage: 9% Rosa damascena flower water, 25% water-soluble azelaic acid from Example 1, 0.02% Geranium geranium extract, 0.3% CalmYangPro, 8% emulsifier, 6.6% emollient, 10% moisturizer, 0.75% thickener, and 100% deionized water.

[0083] The emulsifier is a compound of cetearyl alcohol, cetearyl glucoside, glyceryl stearate, PEG-100 stearate, cetearyl phosphate potassium and cetearyl alcohol polyether-25, with a compound mass ratio of 5.6:0.4:0.6:0.4:0.5:0.5.

[0084] The emollient is a compound of caprylic / capric triglyceride, polydimethylsiloxane, ethylhexyl palmitate, isohexadecane and polydimethylsiloxane in a mass ratio of 2:0.6:3:4:1.

[0085] The humectant is propylene glycol.

[0086] The preservative is a compound of phenoxyethanol, 1,2-hexanediol and chlorphenesin, with a mass ratio of 2:2:1.

[0087] The thickener is a blend of xanthan gum and polyacrylate crosspolymer-6 in a mass ratio of 1:4. Application Example 2 A highly effective acne-removing and scar-fading face cream, comprising the following ingredients by weight percentage: 5% Rosa damascena flower water, 15% azelaic acid (Example 2), 0.01% Geranium geranium extract, 0.1% CalmYangPro, 12% emulsifier, 8% emollient, 12% moisturizer, 1% thickener, and 100% deionized water.

[0088] The emulsifier is a compound of cetearyl alcohol, glyceryl stearate and potassium cetyl phosphate, with a mass ratio of 9:2:1.

[0089] The emollient is a compound of caprylic / capric triglyceride, isohexadecane and polydimethylsiloxane in a mass ratio of 2:3:1.

[0090] The moisturizer is glycerin.

[0091] The preservative is phenoxyethanol.

[0092] The thickener is xanthan gum.

[0093] Application Example 3 A highly effective acne-removing and scar-fading face cream, comprising the following ingredients by weight percentage: 12% Rosa damascena flower water, 20% water-soluble azelaic acid (Example 3), 0.05% Geranium geranium extract, 0.5% CalmYangPro, 6% emulsifier, 5% emollient, 8% moisturizer, 0.5% thickener, and 100% deionized water.

[0094] The emulsifier is cetearyl alcohol.

[0095] The emollient is isohexadecane.

[0096] The moisturizer is a blend of propylene glycol and glycerin in a 1:1 mass ratio.

[0097] The preservative is phenoxyethanol.

[0098] The thickener is polyacrylate crosspolymer-6.

[0099] Human skin patch testing was conducted on face creams corresponding to test cases 1-3. Referring to the human skin patch test in the 2022 edition of the "Cosmetic Safety Technical Specifications," the composition of the above embodiments was tested to determine whether it would cause skin irritation or sensitization. The specific experimental steps are as follows: (1) Ninety people aged 18-60 years were selected and divided into three groups to apply face creams 1-3 respectively. Each group consisted of 15 men and 15 women, none of whom had serious skin diseases, allergies or immune diseases. (2) Select an area not exceeding 50mm²2 A qualified patch test apparatus with a depth of approximately 1 mm was used. 0.02 mL of the face cream corresponding to cases 1-3 above was placed in the small chamber of the patch test apparatus. The control well was a blank control (without any substance). The patch test apparatus containing the finished product was applied to the healthy skin on both sides of the spine on the subject's back using hypoallergenic adhesive tape. Gently press with the palm of the hand to ensure even application to the skin, and leave for 24 hours. Skin reactions were observed 30 minutes (after the indentation disappeared), 24 hours, and 48 hours after the finished product was removed.

[0100] The test results all showed "Level 0", indicating that no allergic reactions occurred, which means that the face cream prepared by the highly effective acne-removing and scar-fading composition of the present invention has low irritation and is safe to use.

[0101] This specific embodiment is merely an explanation of this application and is not intended to limit it. After reading this specification, those skilled in the art can make modifications to this embodiment without contributing any inventive step, but such modifications are protected by patent law as long as they fall within the scope of the claims of this application.

Claims

1. A highly effective acne-removing and acne-scar-fading composition, characterized in that, The product comprises, by weight percentage: 5%–12% Rosa damascena flower water, 0.01%–0.05% Geranium geranium extract, 0.1%–0.5% CalmYangPro, and 15%–25% water-soluble azelaic acid; wherein CalmYangPro comprises Centella asiatica extract, Polygonum cuspidatum root extract, Scutellaria baicalensis root extract, tea extract, Glycyrrhiza glabra extract, Chamomile extract, and Rosmarinus officinalis leaf extract.

2. The highly effective acne-removing and scar-fading composition according to claim 1, characterized in that: The water-soluble azelaic acid comprises, by mass percentage: 55%–65% azelaic acid, 18%–22% hydroxypropyl cyclodextrin, 10%–14% disodium hydrogen phosphate, 5%–7% methyl cyclodextrin, 0.8%–1.2% gum arabic, and 0.8%–1.2% maltodextrin.

3. The highly effective acne-removing and scar-fading composition according to claim 2, characterized in that: The azelaic acid has a particle size of less than or equal to 50 μm.

4. The highly effective acne-removing and scar-fading composition according to claim 2, characterized in that, The water-soluble azelaic acid is prepared by the following method: S1: Dissolve disodium hydrogen phosphate in purified water by stirring, adjust the pH to 6.5-7.5, and prepare a buffer solution; S2: Heat the buffer solution to 55°C, then add hydroxypropyl cyclodextrin and methyl cyclodextrin sequentially and stir until homogeneous; S3: Add azelaic acid in 3 portions at 55℃, with an interval of 15 minutes between each addition. After each addition, sonicate and stir until the system meets the specific conditions. S4: Cool to 40℃, then add gum arabic and maltodextrin and stir to obtain a liquid inclusion complex; S5: Water-soluble azelaic acid is prepared by removing water from the liquid inclusion complex by spray drying or freeze drying to obtain a solid inclusion complex.

5. A method for preparing the highly effective acne-removing and scar-fading composition according to any one of claims 1 to 4, characterized in that, Includes the following steps: S1: Add 70% of the total amount of deionized water to the mixing container, stir at 150-200 rpm, slowly add water-soluble azelaic acid, and stir for 15-20 minutes until completely dissolved; S2: Add geranium extract and CalmYangPro in sequence, stirring at 250-300 rpm for 10-15 minutes after each addition; S3: Slowly pour in the Rosa damascena flower water and stir at 200-250 rpm for 15-20 minutes; S4: Add the remaining 30% of deionized water and stir at 150-200 rpm for 10-15 minutes to obtain a highly effective acne-removing and scar-fading composition.

6. A highly effective acne-removing and acne-scar-fading cosmetic, characterized in that: Includes the highly effective acne-removing and scar-fading composition and cosmetic base as described in any one of claims 1 to 4.

7. The highly effective acne-removing and acne-scar-fading cosmetic according to claim 6, characterized in that: The highly effective acne-removing and acne-fading cosmetic is a face cream or lotion.

8. The highly effective acne-removing and acne-scar-fading cosmetic according to claim 6, characterized in that: The cosmetic base includes emulsifiers, emollients, moisturizers, thickeners, preservatives, and deionized water.

9. A highly effective acne-removing and acne-scar-fading cosmetic according to claim 8, characterized in that: The emulsifier is one or more of cetearyl alcohol, cetearyl glucoside, glyceryl stearate, PEG-100 stearate, potassium cetyl phosphate, and cetearyl alcohol polyether-25.

10. A highly effective acne-removing and acne-scar-fading cosmetic according to claim 8, characterized in that: The emollient is one or more of the following: caprylic / capric triglyceride, polydimethylsiloxane, ethylhexyl palmitate, isohexadecane, and polydimethylsiloxane; The moisturizer is one or more of propylene glycol or glycerin; The preservative is one or more of phenoxyethanol, 1,2-hexanediol and chlorphenesin.

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