Acne removing and whitening composition and application thereof
A stable skincare formulation using adipic acid, salicylic acid, and dimethoxybenzopyranol with a plant fermentation oil agent addresses solubility and irritation issues, enhancing acne and hyperpigmentation treatment efficacy.
Patent Information
- Application Number
- CN202510625381.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-05-15
- Publication Date
- 2025-07-15
- Estimated Expiration
- 2045-05-15
AI Technical Summary
In the prior art, salicylic acid and azelaic acid are combined in skin care products, and have problems such as poor compatibility stability, easy precipitation and crystallization, sticky skin feeling, and damaged skin barriers, which limit the development and application of efficient whitening and acne removal products.
Plant fermented oil agents (such as SynBiOil) are used to wrap azelaic acid, salicylic acid and dimethylmethoxybenzodihydropyranol to form inverse micelle particles, improve permeability and reduce irritation, and achieve stable compounding.
It achieves a stable combination of salicylic acid and azelaic acid, improves the acne removal effect, has a refreshing and non-stick skin, and is suitable for sensitive skin, with significant acne removal and whitening effect.
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Figure CN120305151A_ABST
Abstract
Description
Technical Field
[0001] The present invention relates to the technical field of cosmetics, and in particular to an acne-removing and whitening composition and application thereof. Background Art
[0002] In the field of skin care, as the demand for acne-removing skin care continues to rise, the market is calling for products that are both highly effective and mild. Whitening and acne removal have always been popular demands that have attracted much attention. Salicylic acid and azelaic acid are two skin care ingredients with significant effects, each of which performs well in whitening and acne removal. Salicylic acid can penetrate deep into the pores, effectively dissolve oil, remove aged cuticles, have a good therapeutic effect on acne and blackheads, and also has certain anti-inflammatory ability; azelaic acid can not only inhibit the growth of Propionibacterium acnes and reduce the occurrence of acne, but also improve pigmentation by inhibiting tyrosinase activity, thereby achieving the purpose of whitening.
[0003] However, there are currently many difficulties in compounding salicylic acid and azelaic acid for use in skin care products. On the one hand, due to the difference in solubility, the two have poor compatibility stability. Salicylic acid is a fat-soluble component and is difficult to dissolve in water, while azelaic acid is easy to precipitate crystals in conventional preparations due to its high melting point (105-106°C) and low water solubility (2.4g / L). When the two are compounded, they need to rely on a large amount of organic solvents or surfactants for solubilization, resulting in a sticky formula, poor skin feel, and insufficient long-term stability. For example, the existing technology improves solubility through cyclodextrin inclusion or alkaline salt formation, but the former requires a complex process and may reduce the concentration of active ingredients, and the latter is easy to destroy the chemical stability of azelaic acid. When designing the formula, it is difficult to make salicylic acid and azelaic acid coexist uniformly and stably in the same system, and it is easy to have component precipitation, stratification and other phenomena, affecting product quality and use effect. On the other hand, salicylic acid (pH 3-4) and azelaic acid (pH 2-6) are both acidic ingredients. Using them together may damage the skin barrier, causing dryness and dehydration of the skin. Long-term use may also cause the stratum corneum to thin. Therefore, it is generally not recommended to use azelaic acid and salicylic acid together. Although some studies have tried to add soothing ingredients such as panthenol, experiments have shown that it still cannot completely neutralize the irritation of the complex system, limiting the application of high concentrations.
[0004] These technical bottlenecks limit the development and application of salicylic acid and azelaic acid combination products. Innovative solutions are urgently needed to break through these bottlenecks and meet consumers' demand for highly effective whitening and acne-removing products. Summary of the invention
[0005] The purpose of the present invention is to overcome the shortcomings of the prior art and provide a non-irritating acne-removing and whitening composition containing salicylic acid and azelaic acid.
[0006] To achieve the above object, the technical solution adopted by the present invention is:
[0007] In a first aspect, the present invention provides an anti-acne and whitening composition, comprising the following components in parts by weight: 4-8 parts of azelaic acid, 0.1-4 parts of salicylic acid, 0.1-4 parts of dimethylmethoxy chroman-4-ol, and 40-60 parts of a plant fermented oil agent; the plant fermented oil agent is a mixture of macadamia ternifolia seed oil and the fermentation product of candida apicola / glucose / methyl oleate rapeseed oil.
[0008] Salicylic acid and azelaic acid are traditional anti-acne ingredients. Azelaic acid focuses on anti-inflammatory and pigment management, while salicylic acid is stronger in pore dredging. Both azelaic acid and salicylic acid work by regulating keratin metabolism and antibacterial action, but the compounding technology threshold of the two is extremely high, and it is easy to irritate the skin especially at high concentration ratios. Dimethylmethoxy chroman-4-ol has a whitening effect and can fade acne marks. It fades acne marks, acne scars and common pigmentation by inhibiting the activity of endogenous human tyrosinase and the photoprotective effect on the skin. The present invention innovatively adds azelaic acid, salicylic acid, and dimethylmethoxy chroman-4-ol to the plant fermented oil agent for compounding, successfully enabling the stable compounding of salicylic acid and azelaic acid, and synergistically enhancing the anti-acne effect. The plant fermented oil agent added to the anti-acne and whitening composition of the present invention has an encapsulating effect on salicylic acid, azelaic acid, and dimethylmethoxy chroman-4-ol, forming reverse micelle particles with a microscopic diameter of less than 50 nm (appearing transparent), enabling the above-mentioned active ingredients to act synergistically after compounding. The compounding of azelaic acid and salicylic acid enhances the effect through regulating keratin metabolism and antibacterial action; the three ingredients act in multiple ways, significantly improving the anti-acne effect, which is better than the effect of a single action target.
[0009] The skin lipid layer is composed of keratinocytes, and the stratum corneum cells are proteins with tightly packed lipids. Due to this structural feature, the skin layer can both protect our body and become a key barrier for the penetration of active ingredients. This means that the active ingredients should be in a state similar to the lipid layer to improve the penetration level. The present invention precisely through the encapsulation of the plant fermented oil agent enables salicylic acid, azelaic acid, and dimethylmethoxy chroman-4-ol to easily penetrate into the skin lipid layer, reducing the irritation to the epidermis.
[0010] Preferably, it further comprises the following components in parts by weight: 24-55.8 parts of hexylene glycol.
[0011] Preferably, in the plant fermented oil agent, the mass ratio of macadamia ternifolia seed oil to the fermentation product of candida apicola / glucose / methyl oleate rapeseed oil is macadamia ternifolia seed oil: the fermentation product of candida apicola / glucose / methyl oleate rapeseed oil = 6:94.
[0012] More preferably, it comprises the following components in parts by weight: 5-8 parts of azelaic acid, 2-4 parts of salicylic acid, 2-4 parts of dimethylmethoxydihydrobenzopyranol, 50-60 parts of plant fermented oil agent, and 24-41 parts of hexylene glycol.
[0013] In a second aspect, the present invention provides a method for preparing the acne-removing and whitening composition as described above, comprising the following steps:
[0014] (1) Mix azelaic acid, salicylic acid, dimethylmethoxydihydrobenzopyranol, and hexylene glycol until they are dispersed and dissolved to obtain a mixture;
[0015] (2) Add the plant fermented oil agent to the mixture obtained in step (1) and stir to obtain the acne-removing and whitening composition.
[0016] Preferably, in step (1), it is stirred until completely dissolved by heating to 80°C - 95°C.
[0017] Preferably, in step (2), the temperature is first lowered to 65°C - 75°C, and then the plant fermented oil agent is added.
[0018] In the present invention, hexylene glycol is first used to disperse and dissolve azelaic acid, salicylic acid, and dimethylmethoxydihydrobenzopyranol, and then added to the plant fermented oil agent and stirred to form reverse micelle particles. The plant fermented oil agent has a wrapping effect on salicylic acid, azelaic acid, and dimethylmethoxydihydrobenzopyranol. It can be proved by the transparent state of the appearance that reverse micelle particles with a microscopic diameter of less than 50 nm are formed, without turbidity or precipitation, that is, complete wrapping. Through the wrapping effect, it can help the skin build tolerance to azelaic acid, salicylic acid, and dimethylmethoxydihydrobenzopyranol, reduce the irritation of these three components to the epidermis, and enable them to better exert the acne-removing and whitening effects in the dermis layer of the skin. The present invention adopts the reverse micelle wrapping technology, which not only greatly improves the penetration efficiency of the active substances, but also effectively reduces the irritation, opening up a new path for the research and development of acne-removing products, and realizing "efficient acne clearance, gentle and skin-friendly". The obtained acne-removing and whitening composition of the present invention has a rapid acne-removing effect, will not cause skin damage, and balances the efficacy and safety.
[0019] The plant fermented oil agent of the present invention enhances the polarity of the oil through fermentation, thereby obtaining a highly polar oil-soluble reverse micelle encapsulation system, increasing the number of hydrophilic groups, and can encapsulate various types of water-soluble / oil-soluble active ingredients and polymer components, improving the stability of the active ingredients, increasing the transdermal absorption rate, and reducing irritation. The plant fermented oil agent has an excellent natural oil-soluble sustained-release system. When it contacts the epidermal lipids, it exhibits lipophilic properties, maintains the reverse micelle state, encapsulates components that are difficult to be stable in oil, protects them from dissolving in the skin lipid layer, and is transported to the inner dermis of the skin and then released; and excellent water-soluble and oil-soluble properties: it can dissolve and encapsulate various types of water-soluble / oil-soluble active ingredients. The plant fermented oil agent is biologically fermented, natural, environmentally friendly, and a green ingredient: through the fermentation metabolites of Candida and natural vegetable oil, it dissolves and encapsulates active ingredients and polymer components. Therefore, in the absence of synthetic surfactants, various components can be stabilized in the oil.
[0020] Preferably, the plant fermented oil agent of the present invention can select SynBiOil, which contains 94% of the fermentation product of Candida apicola / glucose / methyl rapeseedate and 6% of Macadamia ternifolia seed oil.
[0021] SynBiOil can encapsulate azelaic acid, salicylic acid, and dimethylmethoxy chromanol, and the components are transported to the inner dermis of the skin and then released, reducing the irritation to the epidermis. SynBiOil has low viscosity, good spreadability, presents a unique fresh and light oil texture, and has a strong moisturizing feeling. Therefore, the SynBiOil reverse micelle encapsulation technology can bring a strong sense of moisturizing sensory experience that general oil products do not have to the formula.
[0022] In the third aspect, the present invention provides the application of the above acne-removing and whitening composition in acne-removing and whitening cosmetics.
[0023] Preferably, the dosage form of the cosmetics includes water, milk, and cream.
[0024] In the fourth aspect, the present invention provides an acne-removing and whitening cosmetic, which includes the above acne-removing and whitening composition and auxiliary materials.
[0025] Preferably, the mass of the acne-removing and whitening composition accounts for 0.5%-10% of the total mass of the acne-removing and whitening cosmetic.
[0026] Concentration control: The content of azelaic acid does not exceed 5%, the content of salicylic acid does not exceed 2%, and the content of dimethylmethoxy chromanol does not exceed 2%. For sensitive skin, the frequency needs to be reduced (2-3 times a week).
[0027] The beneficial effects of the present invention are as follows:
[0028] The present invention innovatively adds azelaic acid, salicylic acid, and dimethylmethoxy chromanol to the plant fermented oil agent. The plant fermented oil agent has a reverse micelle encapsulation effect, which can reduce the irritation of these three active ingredients to the epidermis when azelaic acid, salicylic acid, and dimethylmethoxy chromanol are compounded in a high ratio, and rapidly improve the skin's tolerance to azelaic acid, salicylic acid, and dimethylmethoxy chromanol, enabling them to better exert the effects of acne treatment, acne mark fading, and whitening and freckle removal in the dermis layer inside the skin. The plant fermented oil agent added to the acne treatment and whitening composition of the present invention has an encapsulation effect on salicylic acid, azelaic acid, and dimethylmethoxy chromanol, enabling the above-mentioned active ingredients to act synergistically after compounding. The compounding of azelaic acid and salicylic acid enhances the effect through regulating keratin metabolism and antibacterial action; the three ingredients act in multiple directions, significantly improving the acne treatment effect, which is better than the effect of a single action target.
[0029] The acne treatment and whitening combination provided by the present invention is used for preparing cosmetics, with a refreshing and non-greasy skin feel, subverting the greasy feeling of traditional acids, suitable for sensitive skin and oily acne-prone skin, and can precisely and gently solve skin problems such as acne and roughness. BRIEF DESCRIPTION OF THE DRAWINGS
[0030] Figure 1 It is the observation result of transmission electron microscopy.
[0031] Figure 2 It is the result diagram of the chicken embryo chorioallantoic membrane test for negative control and positive control.
[0032] Figure 3 It is the result diagram of the chicken embryo chorioallantoic membrane test for the test groups of Example 2 and Comparative Example 4.
[0033] Figure 4 It is the result diagram of the inhibitory zone of Propionibacterium acnes for the test groups of Examples 1-3.
[0034] Figure 5 It is the result diagram of the inhibitory zone of Propionibacterium acnes for the test groups of Comparative Examples 1-5. DETAILED DESCRIPTION OF THE INVENTION
[0035] To better illustrate the purpose, technical solution, and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.
[0036] The experimental methods used in the present invention are all conventional methods unless otherwise specified, and the materials, reagents, etc. used can be obtained from commercial channels unless otherwise specified.
[0037] Among the raw materials used in the present invention:
[0038] Candida bombicola / Glucose / Methyl Rapeseedate Ferment: The INCI name is CANDIDA BOMBICOLA / GLUCOSE / METHYL RAPESEEDATE FERMENT. This raw material is included in the "List of Cosmetic Raw Materials in Use (2021 Edition)" with the serial number 03364.
[0039] Macadamia ternifolia Seed Oil: The INCI name is MACADAMIA TERNIFOLIA SEED OIL. This raw material is included in the "List of Cosmetic Raw Materials in Use (2021 Edition)" with the serial number 01070.
[0040] The plant fermented oil agent selected in the present invention is SynBiOil (purchased from Boyao Biology), which contains 94% of Candida bombicola / Glucose / Methyl Rapeseedate Ferment and 6% of Macadamia ternifolia Seed Oil.
[0041] Appearance and physical and chemical indexes of the anti-acne and whitening composition prepared in the present invention:
[0042] Appearance: Light yellow to red transparent liquid;
[0043] Heat resistance (45 ± 2°C): 3 months, return to room temperature, no abnormality;
[0044] Cold resistance (-15 ± 2°C): 3 months, return to room temperature, no abnormality;
[0045] Circulation test (45°C, room temperature, -5°C): 3 months, return to room temperature, no abnormality.
[0046] Observed by a transmission electron microscope (model: JEM-F200, manufacturer: JEOL, USA), the anti-acne and whitening composition of the present invention can form reverse micelle particles with a microscopic diameter of less than 50 nm ( Figure 1 ).
[0047] Examples 1-3:
[0048] Examples of the anti-acne and whitening composition described in the present invention; the components and their mass ratios of the anti-acne and whitening composition described in Examples 1-3 are shown in Table 1.
[0049] Table 1 (unit: mass percentage%)
[0050] Component Example 1 Example 2 Example 3 Azelaic acid 4 5 8 Salicylic acid 0.1 2 4 Dimethylmethoxy chromanol 0.1 2 4 Vegetable ferment oil agent 40 50 60 Hexylene glycol To 100 To 100 To 100
[0051] The plant fermented oil agent selected in the present invention is SynBiOil, which contains 94% of Candida bombicola / Glucose / Methyl Rapeseedate Ferment and 6% of Macadamia ternifolia Seed Oil.
[0052] The preparation method of the anti-acne and whitening composition comprises the following steps:
[0053] (1) Mix azelaic acid, salicylic acid, dimethylmethoxy chroman-4-ol, and hexylene glycol, heat to 80°C - 95°C, and stir until dispersed and dissolved to obtain a mixture;
[0054] (2) Add the plant fermented oil agent to the mixture obtained in step (1) (first cool down to 65°C - 75°C, or do not cool down) and stir to obtain the anti-acne and whitening composition.
[0055] Comparative Examples 1 - 5:
[0056] Comparative examples of the anti-acne and whitening composition of the present invention; the components and their mass ratios of the anti-acne and whitening compositions in Comparative Examples 1 - 5 are shown in Table 2.
[0057] Table 2 (unit: mass percentage%)
[0058]
[0059] Among them, the differences between the anti-acne and whitening compositions in Comparative Examples 1 - 4 and Example 2 are only as follows: azelaic acid is not added in Comparative Example 1; salicylic acid is not added in Comparative Example 2; dimethylmethoxy chroman-4-ol is not added in Comparative Example 3; the plant fermented oil agent is not added in Comparative Example 4; the missing components are supplemented with an equal amount of water.
[0060] The preparation method of the anti-acne and whitening composition is the same as that in Example 2.
[0061] Test Example 1: Chicken embryo chorioallantoic membrane test for eye irritation / corrosion
[0062] Test samples: The anti-acne and whitening compositions prepared in Example 2 and Comparative Example 4; negative control 0.9% NaCl sodium chloride; positive control 0.1 mol / L sodium hydroxide.
[0063] The test method refers to "SN / T 2329-2009 Chicken embryo chorioallantoic membrane test for eye irritation / corrosion of cosmetics".
[0064] Test method for chicken embryo chorioallantoic membrane test (HET-CAM test):
[0065] 1. Basic principle:
[0066] In this experiment, taking advantage of the characteristics of the intact, clear, and transparent vascular system of the chorioallantoic membrane (CAM) in the mid-term of hatched chicken embryos, a certain amount of the test substance was directly contacted with the chicken embryos. After acting for a period of time, the changes in the irritant effect indicators of the chorioallantoic membrane (such as bleeding, blood coagulation, and vascular lysis) were observed. These indicators reflect the changes in the morphological structure, color, and permeability of blood vessels and vascular networks, as well as phenomena such as protein denaturation of the chorioallantoic membrane and the degree of its damage. Then, a score was combined to evaluate the eye irritation of the test substance.
[0067] 2. Preparation of CAM:
[0068] Examine the eggs of 9-day-old chicken embryos by candling, mark the position of the air chamber on the eggshell surface, and use a dental curved forceps with serrations to peel off the marked part of the eggshell to expose the white egg membrane. Drop a few mL of 0.9% sodium chloride (NaCl) solution with a pipette to moisten the egg membrane, and then pour out the 0.9% sodium chloride solution. Carefully remove the inner membrane with forceps, observe the structure of the vascular system again, and make a judgment on its integrity and suitability for the experiment.
[0069] 3. Formal experiment (endpoint evaluation method)
[0070] Take 0.3 mL of the test substance and directly act on the CAM, and ensure that at least 50% of the CAM surface is covered by the test substance. After acting for 3 minutes, gently rinse the test substance on the CAM membrane with physiological saline, and observe the degree of change in each irritant effect. If the total score of 6 chicken embryos is above moderate (total score ≥ 12), the experiment should be repeated once.
[0071] 4. Result observation, the scoring criteria are shown in Table 3:
[0072] Table 3 Scoring criteria
[0073]
[0074]
[0075] 5. For the experiment using the endpoint evaluation method, the end point score (ES, end point score) should be calculated: Score for each chicken embryo = sum of the degrees of bleeding, blood coagulation, and vascular lysis observed in each chicken embryo;
[0076] ES = mathematical sum of the scores of 6 chicken embryos.
[0077] Classify the eye irritation of the test substance according to the ES value (Table 4).
[0078] Table 4 ES value evaluation criteria (HET-CAM)
[0079] Final evaluation score ES value Irritation classification ES≤12 No / light irritation 12 < ES < 16 Moderate irritation
[0080] 6. The test results are asFigure 2-3 as shown in Table 5.
[0081] Table 5
[0082]
[0083]
[0084] The results show that the reaction results of the negative control and the positive control are within the classification range of non-stimulating and stimulating, and the selected chicken embryos meet the test requirements. The endpoint score (ES = Endpoint score) of the test sample in Example 2 is 0.00, showing no irritation; the endpoint score (ES = Endpoint score) of the test sample in Comparative Example 4 is 10.00, showing mild irritation.
[0085] Test Example 2: Whitening and freckle-removing efficacy test
[0086] 1. Test purpose and principle
[0087] The tyrosinase inhibition activity evaluation method is a method for in vitro simulating the determination of skin melanin content. In the biosynthesis of skin melanin, tyrosinase acts on dopa to form dopaquinone and finally form melanin. In a phosphate solution with a pH of 6.8, tyrosinase can catalyze the conversion of dopa into dopaquinone, and the absorbance value can be measured at 475 nm of a spectrophotometer. The degree of change in absorbance is also linearly related to the tyrosinase inhibition activity, that is, the stronger the tyrosinase inhibition activity, the smaller the absorbance.
[0088] 2. Test indicators
[0089] If the tyrosinase inhibition rate of the test sample is greater than that of the negative control and the statistical analysis P < 0.05, then a significant difference is judged.
[0090] 3. Test method
[0091] (1) Reagent preparation
[0092] The test samples are: the acne-removing and whitening compositions prepared in Examples 1-3 and Comparative Examples 1-5.
[0093] Instrument reagents: analytical balance, 10 mL test tubes; adjustable pipette, constant temperature water bath, ultraviolet-visible spectrophotometer, disodium hydrogen phosphate-citric acid buffer solution with a pH of 6.8, tyrosinase, L-dopa, positive control: kojic acid.
[0094] The positive control is diluted with a disodium hydrogen phosphate-citric acid buffer solution with a pH of 6.8 into a series of concentration gradients of 1 mg / mL, 0.2 mg / mL, 0.04 mg / mL, and 0.008 mg / mL to verify the test system.
[0095] Treatment of test substance: The test substance is used in its stock solution (disodium hydrogen phosphate - citric acid diluent is used as the negative control).
[0096] (2) Referring to Table 6, use 10 mL test tubes to set up sample tubes (T), sample blanks (T0), enzyme reaction tubes (C), and solvent blanks (C0). For each test concentration of each sample, 3 parallel tubes of the sample tube (T) need to be set up, and at the same time, 3 parallel tubes of the enzyme reaction tube (C) also need to be set up. Add 1 mL of the sample solution with the same concentration to each of the sample tube (T) and the sample blank (T0), and add 1 mL of disodium hydrogen phosphate - citric acid buffer to the enzyme reaction tube (C) and the solvent blank (C0) respectively.
[0097] Add 0.5 mL of tyrosinase solution to each of the sample tube (T) and the enzyme reaction tube (C). Replace the sample blank (T0) and the solvent blank (C0) with 0.5 mL of disodium hydrogen phosphate - citric acid buffer. Mix the sample and tyrosinase thoroughly and incubate in a 37 °C water bath for 10 minutes.
[0098] Add 2 mL of L - dopa solution to each tube in sequence, control the reaction time of each tube to be 5 minutes, immediately transfer the reaction solution of each tube into a cuvette, and measure the absorbance at 475 nm.
[0099] Table 6 Requirements for adding liquid to samples
[0100]
[0101] 4. Calculate the tyrosinase inhibition rate according to formula (1):
[0102]
[0103] In the above formula:
[0104] T - Absorbance of the sample blank, that is, the absorbance of the solution after the reaction of the sample and tyrosinase;
[0105] T0 - Absorbance of the sample blank;
[0106] C - Average value of the absorbance of the enzyme reaction tube for 3 times, that is, the absorbance of the reaction of tyrosinase and dopa without adding the sample; The test results are the arithmetic mean of the three data, and the SD value of the three data needs to be ≤ 3%.
[0107] The results are shown in Table 7.
[0108] Table 7
[0109]
[0110] The results show that the tyrosinase inhibition rate of the anti-acne and whitening composition prepared in the examples of the present invention is greater than 45.27%. Compared with the negative control, the P value < 0.05, showing a significant difference, indicating that the anti-acne and whitening composition prepared in the examples of the present invention has a significant effect of whitening and removing spots. Azelaic acid has an anti-inflammatory effect, salicylic acid is stronger in dredging pores, and dimethylmethoxybenzodihydropyran alcohol fades acne marks, acne spots and common pigmentation spots through inhibiting the activity of endogenous human tyrosinase and the photoprotective effect on the skin. The plant fermented oil agent added in the anti-acne and whitening composition of the present invention has a wrapping effect on salicylic acid, azelaic acid and dimethylmethoxybenzodihydropyran alcohol, enabling the above-mentioned active ingredients to have a synergistic effect after compounding. The compounding of azelaic acid and salicylic acid enhances the antibacterial effect by regulating keratin metabolism; the three ingredients act in multiple directions, significantly improving the anti-acne effect, which is better than the effect of a single action target. Compared with the samples of Comparative Examples 1-5, the tyrosinase inhibition rate of Comparative Examples 1-5 decreased significantly, indicating that when the ratio of azelaic acid, salicylic acid, dimethylmethoxybenzodihydropyran alcohol and plant fermented oil agent exceeds the scope of the present invention or lacks any component, the whitening and spot-removing effect of the present invention cannot be achieved.
[0111] Test Example 3: Evaluation of Anti-acne Efficacy
[0112] 1. Test Purpose and Principle
[0113] According to Propionibacterium acnes being a component of the normal flora of hair follicles, Propionibacterium acnes multiplies during the inflammatory process of acne. The antibacterial effect of the test sample on Propionibacterium acnes is detected to evaluate the anti-acne efficacy of the sample. Propionibacterium acnes proliferates. This bacterium is a component of the normal flora of hair follicles. It uses sebum as its substrate and partially converts it into free fatty acids. Propionibacterium acnes can also activate the complement pathway and produce at least two chemotactic factors, promoting inflammation. Therefore, inhibiting Propionibacterium acnes can achieve the anti-acne effect. An antibacterial agent is continuously dissolved to form different concentration gradients by agar diffusion to show its antibacterial effect. The test judges whether it has antibacterial ability through the size of the inhibition zone.
[0114] 2. Test Indexes
[0115] The test samples are: the anti-acne and whitening compositions prepared in Examples 1-3 and Comparative Examples 1-5.
[0116] The antibacterial ability is evaluated through the size of the inhibition zone of the test group against Propionibacterium acnes. If the diameter of the inhibition zone is greater than 7 mm, it is judged to have an antibacterial effect; if the diameter of the inhibition zone is less than or equal to 7 mm, it is judged to have no antibacterial effect.
[0117] 3. Test Strains
[0118] Propionibacterium acnes (ATCC11827) was provided by Guangdong Huankai Technology Co., Ltd. in the third generation.
[0119] 4. Antibacterial and Bacteriostatic Ring Test in QB / T 2738-2023 "Evaluation Method for Antibacterial and Bacteriostatic Effects of Daily Chemical Products" 7.5
[0120] Method:
[0121] (1) Preparation of test group specimens: Drop 20 μL of the sample at the actual use concentration on each specimen, then place the filter paper flat in a clean sterile petri dish, open the lid and dry it in an incubator (37 °C), or let it dry naturally at room temperature for later use. Group every 4 specimens together.
[0122] (2) Preparation of negative control specimens: Take sterile dry filter paper, drop 20 μL of sterile distilled water on each specimen, and dry it for later use.
[0123] (3) Inoculation of test bacteria: Dip a sterile cotton swab into the test bacterial suspension with a concentration of 5×10 5 ~5×10 6 and smear it evenly on the surface of the reinforced Clostridium medium plate 3 times. Each time it is smeared, the plate should be rotated 60°. Finally, smear the cotton swab around the edge of the plate once. Cover the petri dish and let it dry at room temperature for 5 min.
[0124] (4) Placement of specimens: Place 4 test specimens and 1 negative control specimen on each plate, a total of 5 specimens. Use sterile forceps to pick up the specimens and place them on the surface of the plate. The distance between the centers of each specimen should be more than 25 mm, and the distance from the periphery of the plate should be more than 15 mm. After placement, gently press the specimens with sterile forceps to make them close to the surface of the plate. Cover the petri dish and place it in a 37 °C incubator for anaerobic culture for 48 h to observe the results.
[0125] (5) Measure the diameter of the antibacterial ring (including the specimen patch) with a vernier caliper and record it. Repeat the test 3 times. When measuring the antibacterial ring, select the antibacterial ring with uniform and completely sterile growth. The measurement of its diameter should be based on the outer edge of the antibacterial ring.
[0126] Table 8
[0127]
[0128]
[0129] The results are shown in Table 8, Figure 4-5As shown in the figure. The results show that the average diameter of the inhibition zone of the acne-removing and whitening composition test samples prepared in the embodiments of the present invention is greater than 10.44 mm, showing a significant difference compared with the negative control, indicating that the acne-removing and whitening composition prepared in the embodiments of the present invention has an inhibitory effect on Propionibacterium acnes and has a significant acne-removing effect. Compared with the samples of Comparative Examples 1-5, the average diameter of the inhibition zone of Comparative Examples 1-5 decreased significantly, indicating that when the ratio of azelaic acid, salicylic acid, dimethylmethoxydihydrobenzopyranol, and plant fermented oil exceeds the scope of the present invention or lacks any component, the acne-removing effect of the present invention cannot be achieved.
[0130] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention rather than to limit the protection scope of the present invention. Although the present invention has been described in detail with reference to the preferred embodiments, those of ordinary skill in the art should understand that the technical solutions of the present invention can be modified or equivalently replaced without departing from the essence and scope of the technical solutions of the present invention.
Claims
1. A acne-removing and whitening composition, characterized in that, It comprises the following components in parts by weight: 4-8 parts of azelaic acid, 0.1-4 parts of salicylic acid, 0.1-4 parts of dimethylmethoxy chromanol, 40-60 parts of plant fermented oil agent; the plant fermented oil agent is a mixture of macadamia ternifolia seed oil and the fermentation product of candida apicola / glucose / methyl oleate rapeseed oil.
2. The anti-acne and whitening composition according to claim 1, characterized in that, It further comprises the following components in parts by weight: 24-55.8 parts of hexylene glycol.
3. The anti-acne and skin-whitening composition according to claim 1, wherein In the plant fermented oil agent, the mass ratio of macadamia ternifolia seed oil to the fermentation product of candida apicola / glucose / methyl oleate rapeseed oil is macadamia ternifolia seed oil: the fermentation product of candida apicola / glucose / methyl oleate rapeseed oil = 6:
94.
4. The anti-acne and skin-whitening composition according to claim 2, wherein It comprises the following components in parts by weight: 5-8 parts of azelaic acid, 2-4 parts of salicylic acid, 2-4 parts of dimethylmethoxy chromanol, 50-60 parts of plant fermented oil agent, 24-41 parts of hexylene glycol.
5. A method for preparing an anti-acne and skin-whitening composition according to any one of claims 1-4, characterized in that, It comprises the following steps: (1) Mix azelaic acid, salicylic acid, dimethylmethoxy chromanol, and hexylene glycol until they are dispersed and dissolved to obtain a mixture; (2) Add the plant fermented oil agent to the mixture obtained in step (1) and stir to obtain the anti-acne and skin-whitening composition.
6. Use of the anti-acne and skin-whitening composition according to any one of claims 1-4 in anti-acne and skin-whitening cosmetics.
7. The application according to claim 6, wherein The dosage forms of the cosmetics include lotion, milk, and cream.
8. A kind of acne-removing and whitening cosmetics, characterized in that, It comprises the anti-acne and skin-whitening composition according to any one of claims 1-4 and excipients.
9. The anti-acne and whitening cosmetic according to claim 8, characterized in that The mass of the anti-acne and skin-whitening composition accounts for 0.5%-10% of the total mass of the anti-acne and skin-whitening cosmetics.
Citation Information
Patent Citations
Acne-removing composition and application thereof to cosmetics
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