Extraction of a traditional Chinese medicine combination and use thereof in preparing a composition for removing cutin and improving acne

Abstract

The application discloses a traditional Chinese medicine combination extraction and application thereof in preparation of a composition for removing cutin and improving acne, and belongs to the field of cosmetics. In the application, traditional Chinese medicines (three or more than three of honeysuckle, ganoderma lucidum, Chinese cork tree, centella asiatica, yunnan paris, salvia miltiorrhiza and licorice) are extracted to obtain a traditional Chinese medicine extract; then, a water-soluble azelaic acid system, pyridoxine or a pyridoxine derivative, the traditional Chinese medicine extract and water are uniformly mixed to obtain the composition for removing cutin and improving acne; and the mass ratio of the water-soluble azelaic acid system, the pyridoxine or the pyridoxine derivative, the traditional Chinese medicine extract and water is 0.5-20:0.1-10:0.5-10:100. The composition prepared in the application can improve the effect of removing cutin and improving acne, has definite curative effect and is safe and free of side effects.

Description

Technical Field

[0001] This invention relates to the extraction of a traditional Chinese medicine combination and its application in the preparation of a composition for exfoliation and acne improvement, belonging to the field of cosmetics. Background Technology

[0002] Azelaic acid is a naturally occurring, straight-chain saturated dicarboxylic acid containing nine carbon atoms. It possesses good antibacterial properties and significant permeability to the skin surface, making it effective in treating acne and other skin problems. It can also balance sebum secretion, stimulate hair growth, inhibit tyrosinase activity, reduce pigmentation, and effectively fade acne scars. However, azelaic acid can cause local skin irritation, primarily manifesting as erythema, itching, scaling, and burning sensations. The mechanism of this irritation is currently unclear. The applicant has previously filed a series of patents involving cosmetic compositions related to azelaic acid. For example, CN117017850A relates to a topical cosmetic composition comprising: azelaic acid, bisabolol, white willow bark extract, Egyptian blue water lily extract, kale leaf extract, and yarrow extract; CN117530874A relates to a method for preparing a water-soluble azelaic acid system, comprising the following steps: mixing azelaic acid, salicylic acid, and panthenol evenly, and stirring and heating at 65-110℃ for 1-8 hours, so that azelaic acid, salicylic acid, and panthenol form a liquid organic body through intermolecular hydrogen bonds, i.e., a water-soluble azelaic acid system.

[0003] Salicylic acid is a lipid-soluble organic acid primarily used to treat acne, warts, and seborrheic dermatitis. Studies have shown that it is more effective than benzoyl peroxide in treating acne and blackheads; 1-4% salicylic acid removes surface keratinization, while concentrations above 5% can be used to remove deep keratinization. Salicylic acid is currently a mainstream ingredient in acne-removing products in the cosmetics industry, but its poor water solubility and strong irritant properties greatly limit its application. Therefore, azelaic acid and salicylic acid are both effective raw materials for exfoliation and acne improvement in this field, but their irritation and water solubility remain problems that urgently need to be addressed in the cosmetics industry.

[0004] Regarding the issue of water solubility, the applicant previously filed application CN117530874A, which provides a method for preparing a water-soluble azelaic acid system, including the following steps: mixing azelaic acid, salicylic acid, and panthenol uniformly, and stirring and heating at 65-110℃ for 1-8 hours, so that azelaic acid, salicylic acid, and panthenol form a liquid organic body through intermolecular hydrogen bonds, i.e., a water-soluble azelaic acid system. Optionally, the molar ratio of azelaic acid, salicylic acid, and panthenol is 1:0.3-15:1-12; this application selects salicylic acid and panthenol as co-component molecules, mixing and heating them together with azelaic acid, so that azelaic acid, salicylic acid, and panthenol form a liquid organic body through intermolecular hydrogen bonds, effectively improving the solubility of azelaic acid, and without requiring a large amount of solvent, making the operation very simple. In addition, salicylic acid, as a co-component molecule, can synergistically enhance the exfoliating ability of azelaic acid.

[0005] Subsequently, the applicant conducted efficacy studies on the product for exfoliation and acne improvement. The studies revealed that due to the inclusion of azelaic acid and salicylic acid, which are somewhat irritating components, the composition, despite the addition of panthenol as a deep-penetrating moisturizer and to reduce irritation, still exhibited irritation. Therefore, the technical problem this invention aims to solve is to provide, based on existing technology, a composition for reducing irritation and its preparation method, thereby improving exfoliation and acne improvement effects, with definite therapeutic efficacy and no side effects. Summary of the Invention

[0006] To address the aforementioned technical issues, the applicant first attempted to select and add oil-controlling and soothing components to the exfoliating and acne-improving composition provided in application CN117530874A. Prior application CN117442509A provided a low-dose oil-controlling and soothing composition, including azelaic acid and its derivatives, zinc salts, and vitamins, where the vitamins could be niacinamide (vitamin B3), pyridoxine (vitamin B6), etc. Furthermore, the experimental group 3 of this application used a combination of azelaic acid and pyridoxine for relevant experimental studies. This application also mentioned that vitamin B6 is one of the essential vitamins for human metabolism, capable of inhibiting sebaceous gland activity, reducing sebum secretion, participating in various skin metabolism processes, and providing multi-faceted assistance in regulating scalp health. Therefore, the preliminary experiments of this invention first screened relevant B vitamins and found that adding pyridoxine (vitamin B6) and its derivatives had the best effect on improving exfoliation and acne improvement, but still had some irritation.

[0007] Traditional Chinese medicine (TCM), a national treasure, classifies acne as a type of "lung-wind acne." Those prone to acne often have a "hot" constitution, oily skin, and are easily inflamed, resulting in red, swollen, and painful boils on the face, sometimes even suppurating. This reflects a heavy accumulation of damp-heat toxins in the body, requiring dietary adjustments to clear heat and toxins, reduce inflammation, and promote bowel movement, thereby improving the "hot" constitution that predisposes to acne. Chinese herbal medicine is often safe, low-irritant, and soothing when used for exfoliation and blackhead reduction. Therefore, TCM treatment for acne frequently emphasizes clearing heat and toxins, and its selection of medicinal herbs also prioritizes these properties. To address irritation and enhance the effectiveness of exfoliation and acne improvement, the applicant attempted to screen relevant components from heat-clearing and detoxifying Chinese herbal medicines and conduct efficacy and irritation tests. Therefore, in the early stages of this invention, common single-herb heat-clearing and detoxifying Chinese medicinal herbs were selected. Honeysuckle, forsythia, wild chrysanthemum, phellodendron bark, sophora flavescens, and licorice were extracted with 80% ethanol. Preliminary experiments on the inhibitory activity of the extracts against Propionibacterium acnes revealed that all six herbs—honeysuckle, forsythia, wild chrysanthemum, phellodendron bark, sophora flavescens, and licorice—had some inhibitory activity against Propionibacterium acnes, with honeysuckle extract showing the best antibacterial ability and the lowest irritation. However, considering that honeysuckle, forsythia, and wild chrysanthemum have similar efficacy, and preliminary experimental results indicate that honeysuckle has lower irritation than forsythia and wild chrysanthemum, and that phellodendron bark and sophora flavescens have similar efficacy, and that preliminary experimental results indicate that phellodendron bark has lower irritation than sophora flavescens, and that licorice is frequently added to Chinese medicine compositions to harmonize the medicinal properties, only honeysuckle, phellodendron bark, and licorice with relatively strong activity were selected from the above six herbs to simplify the composition.

[0008] Reishi mushroom is often used to replenish qi and improve complexion, while salvia miltiorrhiza can invigorate blood and remove blood stasis, and is also commonly used for acne and melasma. These two herbs are frequently used for pigmentation, and both reishi and salvia miltiorrhiza also have soothing effects. Acne patients often have red acne marks after treatment. To alleviate the severity of these marks, the inventor added reishi and salvia miltiorrhiza, which have certain effects on improving complexion and removing acne marks.

[0009] Centella asiatica extract has various effects in cosmetics, including antibacterial, anti-inflammatory, and promoting the synthesis of fibroblasts and collagen cells. Generally, the main active ingredients in Centella asiatica extract for treating acne are asiaticoside, asiatic acid, asiaticoside, and asiaticoside. Most of these ingredients are alcohol-soluble. For products targeting sensitive skin and redness, Centella asiatica extract is often used in combination with other ingredients, such as vitamin B5, to alleviate discomfort such as stinging. Paris polyphylla extract has excellent inhibitory effects on Propionibacterium acnes. When treating acne, Paris polyphylla generally also has heat-clearing, detoxifying, swelling-reducing, and pain-relieving effects. Regarding the combined use of Paris polyphylla extract and Centella asiatica extract, the inventor previously researched products currently on the market. Yunnan Baiyao's Caizhiji Paris polyphylla essence uses a combination of Paris polyphylla extract, Centella asiatica extract, and aloe vera extract to reduce skin irritation, soothe and repair, and effectively improve facial redness. Skin irritation and facial redness are also common problems encountered after using products containing salicylic acid and azelaic acid. Therefore, the inventors tried to further add Centella asiatica and Paris polyphylla to the ingredients of honeysuckle, Phellodendron amurense, licorice, Ganoderma lucidum and Salvia miltiorrhiza.

[0010] Therefore, the topical Chinese medicine extract selected in this invention uses commonly used Chinese medicine raw materials for improving acne in clinical practice. The main treatment principle is to clear heat and detoxify, supplemented by herbs that replenish qi and blood, and soothe and stabilize the condition. That is, the composition of the Chinese medicine extract includes three or more of the following: honeysuckle, Ganoderma lucidum, Phellodendron chinense, Centella asiatica, Paris polyphylla, Salvia miltiorrhiza, and licorice.

[0011] Based on this, the present invention provides a topical preparation for exfoliation and acne improvement, comprising a combination of azelaic acid, salicylic acid, panthenol, pyridoxine or pyridoxine derivatives, and traditional Chinese medicine extracts. The product of the present invention is mild, has low irritation, and is more effective than commercially available clindamycin phosphate gel and supramolecular salicylic acid.

[0012] The first objective of this invention is to provide a method for preparing extracts of traditional Chinese medicine, comprising the following steps:

[0013] The Chinese herbal components are mixed, pulverized, and sieved to obtain a mixed powder. The mixed powder is then extracted with a 75-85% (v / v) ethanol aqueous solution and filtered. The residue is then repeatedly extracted, the extracts are combined, concentrated, and dried to obtain the Chinese herbal extract.

[0014] The herbal ingredients consist of three or more of the following: honeysuckle, Ganoderma lucidum, Phellodendron amurense, Centella asiatica, Paris polyphylla, Salvia miltiorrhiza, and licorice.

[0015] In one embodiment of the present invention, the ratio of the mixed powder of traditional Chinese medicine and the aqueous ethanol solution with a volume fraction of 75-85% is 1g:3-10mL.

[0016] In one embodiment of the present invention, when the traditional Chinese medicine components are honeysuckle, Ganoderma lucidum and Centella asiatica, the mass ratio of the three is 20-30:10-20:5-10.

[0017] In one embodiment of the present invention, when the traditional Chinese medicine components are honeysuckle, Ganoderma lucidum, Centella asiatica and Phellodendron amurense, the mass ratio of the four components is 20-30:10-15:5-10:10-15.

[0018] In one embodiment of the present invention, when the traditional Chinese medicine components are honeysuckle, Ganoderma lucidum, Centella asiatica, Phellodendron chinense, and Salvia miltiorrhiza, the mass ratio of the five components is 20-30:10-15:5-10:10-15:5-10.

[0019] In one embodiment of the present invention, when the traditional Chinese medicine components are honeysuckle, Ganoderma lucidum, Centella asiatica, Phellodendron chinense, Salvia miltiorrhiza, and Paris polyphylla, the mass ratio of the six components is 20-30:10-15:5-10:10-15:5-10:5-10.

[0020] In one embodiment of the present invention, when the traditional Chinese medicine components are honeysuckle, Ganoderma lucidum, Centella asiatica, Phellodendron chinense, Salvia miltiorrhiza, Paris polyphylla, and licorice, the mass ratio of the seven components is 20-30:10-15:5-10:10-15:5-10:5-10:3-5.

[0021] In one embodiment of the present invention, extraction is performed at 20-30℃ (room temperature) for 30-120 minutes.

[0022] In one embodiment of the present invention, extraction may be performed using ultrasonic extraction, reflux extraction, cold soaking extraction, etc.

[0023] In one embodiment of the present invention, the extraction is repeated 1-4 times.

[0024] The second objective of this invention is to prepare a traditional Chinese medicine extract using the method described herein.

[0025] A third objective of this invention is to provide a composition for exfoliation and acne improvement, comprising a water-soluble azelaic acid system, pyridoxine or pyridoxine derivatives, a traditional Chinese medicine extract, and water; wherein the mass ratio of the water-soluble azelaic acid system, pyridoxine or pyridoxine derivatives, the traditional Chinese medicine extract, and water is 0.5-20:0.1-10:0.5-10:100.

[0026] In one embodiment of the present invention, the mass ratio of the water-soluble azelaic acid system, pyridoxine or pyridoxine derivative, traditional Chinese medicine extract, and water is 0.5-10:0.1-7:0.5-7:100; preferably, the mass ratio of the water-soluble azelaic acid system, pyridoxine or pyridoxine derivative, traditional Chinese medicine extract, and water is 1-7:0.1-4:0.5-5:100; more preferably, the mass ratio of the water-soluble azelaic acid system, pyridoxine or pyridoxine derivative, traditional Chinese medicine extract, and water is 2-5:0.2-2:1-3:100; most preferably, the mass ratio of the water-soluble azelaic acid system, pyridoxine or pyridoxine derivative, traditional Chinese medicine extract, and water is 3:0.5:2:100 or 2:0.2:1:100.

[0027] In one embodiment of the present invention, the pyridoxine derivative is pyridoxine tri-hexyldecanoate.

[0028] In one embodiment of the present invention, the water-soluble azelaic acid system is prepared using azelaic acid, salicylic acid, and panthenol, wherein the molar ratio of azelaic acid, salicylic acid, and panthenol is 1:0.3-15:1-12; preferably, the molar ratio of azelaic acid, salicylic acid, and panthenol is 1:1.5:2 or 1:1:4; panthenol includes, but is not limited to, DL-panthenol.

[0029] In one embodiment of the present invention, the water-soluble azelaic acid system is prepared as follows:

[0030] Azelaic acid, salicylic acid and panthenol are mixed evenly and stirred and heated at 65-110℃ for 1-8 hours, so that azelaic acid, salicylic acid and panthenol form a liquid organic body through intermolecular hydrogen bonds, namely the water-soluble azelaic acid system.

[0031] The stirring and heating speed is 300-1000 rpm; the stirring and heating atmosphere is air, argon or carbon dioxide.

[0032] In one embodiment of the present invention, excipients may also be added to the composition for exfoliation and acne improvement, including but not limited to one or more of preservatives, pH adjusters, and fragrances.

[0033] In one embodiment of the present invention, the composition for exfoliation and acne improvement is a liquid formulation.

[0034] A fourth object of the present invention is to provide a method for preparing a composition for exfoliation and acne improvement, comprising the following steps:

[0035] A composition for exfoliation and acne improvement can be obtained by mixing water-soluble azelaic acid system, pyridoxine or pyridoxine derivatives, traditional Chinese medicine extracts, and water evenly.

[0036] A fifth object of the present invention is to provide a cosmetic product that uses the composition described herein for exfoliation and acne improvement.

[0037] A sixth objective of this invention is the application of the composition described herein for exfoliation and acne improvement in daily chemical products.

[0038] A seventh objective of this invention is to provide a method for improving the exfoliating and acne-reducing properties of cosmetics, wherein the method employs the composition for exfoliation and acne reduction described in this invention.

[0039] [Beneficial Effects]

[0040] (1) In the water-soluble azelaic acid system of the present invention, azelaic acid, salicylic acid and panthenol form an organic whole through supramolecular hydrogen bond interaction, thereby effectively improving the water solubility of azelaic acid and enhancing the exfoliating and acne-improving effects of azelaic acid.

[0041] (2) This invention contains raw materials such as salicylic acid and azelaic acid. After adding pyridoxine or pyridoxine derivatives and traditional Chinese medicine extracts, the efficacy of exfoliation and acne improvement is increased, and the problems of skin irritation and facial redness are also alleviated to a certain extent.

[0042] (3) The process of preparing the composition for exfoliation and acne improvement of the present invention is simple, safe and easy to operate, and the other added raw materials are also commonly used in the field, reasonably priced, and can be directly applied to cosmetics, making it easy to promote.

[0043] (4) The composition prepared by the present invention for exfoliation and acne improvement is mild and less irritating, and its effect is better than that of commercially available clindamycin phosphate gel and Brøndal supramolecular salicylic acid. Detailed Implementation

[0044] 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.

[0045] Raw materials used in the examples:

[0046] Honeysuckle, Ganoderma lucidum, Phellodendron amurense, Centella asiatica, Paris polyphylla, Salvia miltiorrhiza, and Glycyrrhiza uralensis: commercially available;

[0047] Pyridoxine; ≥98%, commercially available;

[0048] Pyridoxine tri-hexyldecanoate: 98%, commercially available;

[0049] Azelaic acid: Particle size 500nm-100μm, particle size has no effect, the particle size selected in the examples and comparative examples is 30μm, commercially available;

[0050] Panthenol: D-panthenol or DL-panthenol can be used in the examples and comparative examples, and are commercially available.

[0051] Example 1

[0052] A method for preparing a water-soluble azelaic acid system includes the following steps:

[0053] Weigh out 0.01 mol of azelaic acid, 0.015 mol of salicylic acid, and 0.02 mol of DL-panthenol, stir them thoroughly, and place them in a sealed reaction vessel. Place the reaction vessel in an argon protective atmosphere and keep it at a constant temperature of 600 rpm and 95°C for 3 hours. Then, cool the reaction vessel to room temperature, so that azelaic acid, salicylic acid, and panthenol form a liquid organic substance through intermolecular hydrogen bonds, i.e., a water-soluble azelaic acid system.

[0054] The water-soluble azelaic acid system is homogeneous and transparent;

[0055] The azelaic acid content in the water-soluble azelaic acid system was 23 wt%, and its pH was measured to be 4.37 using a pH meter.

[0056] The water-soluble azelaic acid system was diluted with water to azelaic acid content of 3% of the total mass, and the system remained homogeneous and transparent.

[0057] The water-soluble azelaic acid system and the diluted system were subjected to high and low temperature cycling tests (15 cycles at -5℃ and 40℃ respectively). Both systems were able to maintain a stable and homogeneous liquid state without phase separation or precipitation of solids.

[0058] Example 2

[0059] A method for preparing a water-soluble azelaic acid system includes the following steps:

[0060] Weigh out 0.01 mol azelaic acid, 0.01 mol salicylic acid, and 0.04 mol D-panthenol, stir them thoroughly, and place them in a sealed reaction vessel. Place the reaction vessel in a natural air atmosphere and keep it at a constant temperature of 500 rpm and 85°C for 2 hours. Then, cool the reaction vessel to room temperature, so that azelaic acid, salicylic acid, and panthenol form a liquid organic substance through intermolecular hydrogen bonds, i.e., a water-soluble azelaic acid system.

[0061] The water-soluble azelaic acid system is homogeneous and transparent;

[0062] The azelaic acid content in the water-soluble azelaic acid system was 16 wt%, and its pH was measured to be 5.03 using a pH meter.

[0063] The water-soluble azelaic acid system was diluted with water to azelaic acid content of 2% of the total mass, and the system remained homogeneous and transparent.

[0064] The water-soluble azelaic acid system and the diluted system were subjected to high and low temperature cycling tests (15 cycles at -5℃ and 40℃ respectively). Both systems were able to maintain a stable and homogeneous liquid state without phase separation or precipitation of solids.

[0065] Example 3

[0066] A method for preparing extracts of traditional Chinese medicine includes the following steps:

[0067] Mix 30g of honeysuckle, 20g of Ganoderma lucidum and 8g of Centella asiatica, crush them and sieve them to obtain a mixed powder of traditional Chinese medicine.

[0068] Add 58g of mixed Chinese herbal medicine powder to 600mL of 80% ethanol aqueous solution, and perform ultrasonic extraction at room temperature for 60min, followed by filtration.

[0069] The residue was extracted twice, for a total of three extractions. The extracts were combined, concentrated under reduced pressure, and dried to obtain the Chinese herbal extract.

[0070] Example 4

[0071] A method for preparing extracts of traditional Chinese medicine includes the following steps:

[0072] Mix 30g of honeysuckle, 10g of Ganoderma lucidum, 8g of Centella asiatica and 10g of Phellodendron chinense, grind them, and sieve them to obtain a mixed powder of traditional Chinese medicine.

[0073] Add 58g of mixed Chinese herbal medicine powder to 600mL of 80% ethanol aqueous solution, and perform ultrasonic extraction at room temperature for 60min, followed by filtration.

[0074] The residue was extracted twice, for a total of three extractions. The extracts were combined, concentrated under reduced pressure, and dried to obtain the Chinese herbal extract.

[0075] Example 5

[0076] A method for preparing extracts of traditional Chinese medicine includes the following steps:

[0077] Mix 28g of honeysuckle, 10g of Ganoderma lucidum, 5g of Centella asiatica, 10g of Phellodendron chinense, and 5g of Salvia miltiorrhiza, grind them, and sieve them to obtain a mixed powder of traditional Chinese medicine.

[0078] Add 58g of mixed Chinese herbal medicine powder to 600mL of 80% ethanol aqueous solution, and perform ultrasonic extraction at room temperature for 60min, followed by filtration.

[0079] The residue was extracted twice, for a total of three extractions. The extracts were combined, concentrated under reduced pressure, and dried to obtain the Chinese herbal extract.

[0080] Example 6

[0081] A method for preparing extracts of traditional Chinese medicine includes the following steps:

[0082] Mix 23g of honeysuckle, 10g of Ganoderma lucidum, 5g of Centella asiatica, 10g of Phellodendron chinense, 5g of Salvia miltiorrhiza, and 5g of Paris polyphylla, pulverize, and sieve to obtain a mixed powder of traditional Chinese medicine.

[0083] Add 58g of mixed Chinese herbal medicine powder to 600mL of 80% ethanol aqueous solution, and perform ultrasonic extraction at room temperature for 60min, followed by filtration.

[0084] The residue was extracted twice, for a total of three extractions. The extracts were combined, concentrated under reduced pressure, and dried to obtain the Chinese herbal extract.

[0085] Example 7

[0086] A method for preparing extracts of traditional Chinese medicine includes the following steps:

[0087] Mix 20g of honeysuckle, 10g of Ganoderma lucidum, 5g of Centella asiatica, 10g of Phellodendron chinense, 5g of Salvia miltiorrhiza, 5g of Paris polyphylla, and 3g of licorice, pulverize, and sieve to obtain a mixed powder of traditional Chinese medicine.

[0088] Add 58g of mixed Chinese herbal medicine powder to 600mL of 80% ethanol aqueous solution, and perform ultrasonic extraction at room temperature for 60min, followed by filtration.

[0089] The residue was extracted twice, for a total of three extractions. The extracts were combined, concentrated under reduced pressure, and dried to obtain the Chinese herbal extract.

[0090] Example 8

[0091] A method for preparing extracts of traditional Chinese medicine includes the following steps:

[0092] Mix 30g of honeysuckle, 15g of Ganoderma lucidum, 15g of Phellodendron chinense, 10g of Centella asiatica, 10g of Paris polyphylla, 10g of Salvia miltiorrhiza, and 5g of licorice, grind them, and sieve them to obtain a mixed powder of traditional Chinese medicine.

[0093] Add 95g of mixed Chinese herbal medicine powder to 600mL of 80% ethanol aqueous solution, and perform ultrasonic extraction at room temperature for 60min, followed by filtration.

[0094] The residue was extracted twice, for a total of three extractions. The extracts were combined, concentrated under reduced pressure, and dried to obtain the Chinese herbal extract.

[0095] Example 9

[0096] A method for preparing extracts of traditional Chinese medicine includes the following steps:

[0097] Mix 25g of honeysuckle, 12g of Ganoderma lucidum, 12g of Phellodendron chinense, 8g of Centella asiatica, 8g of Paris polyphylla, 8g of Salvia miltiorrhiza, and 4g of licorice, pulverize, and sieve to obtain a mixed powder of traditional Chinese medicine.

[0098] Add 77g of mixed Chinese herbal medicine powder to 500mL of 80% ethanol aqueous solution, and perform ultrasonic extraction at room temperature for 60min, followed by filtration.

[0099] The residue was extracted twice, for a total of three extractions. The extracts were combined, concentrated under reduced pressure, and dried to obtain the Chinese herbal extract.

[0100] Example 10

[0101] A method for preparing a composition for exfoliation and acne improvement includes the following steps:

[0102] A composition for exfoliation and acne improvement can be obtained by mixing water-soluble azelaic acid system, pyridoxine or pyridoxine derivatives, traditional Chinese medicine extracts, and water evenly.

[0103] The specific components and formulations are shown in Table 1:

[0104] Table 1

[0105]

[0106] Example 11 Antibacterial effect

[0107] Evaluation of the antibacterial effects of items 1-15 on Propionibacterium acnes.

[0108] (1) Experimental strain:

[0109] Propionibacterium acnes ATCC6919: purchased from Shanghai Huzheng Biotechnology Co., Ltd.

[0110] (2) Experimental methods:

[0111] a. Preparation of Propionibacterium acnes cells:

[0112] The Propionibacterium acnes strain preserved on slant culture medium was transferred to liquid anaerobic medium and cultured at 37°C for 36 hours under anaerobic conditions. The bacterial suspension was then diluted with sterile physiological saline to a concentration of 1×10⁻⁶. 7 CFU / mL was used to obtain a bacterial suspension.

[0113] b. Antibacterial test:

[0114] The determination was performed using the agar diffusion method. A 12 cm diameter petri dish was taken, 10 mL of culture medium was added, and under aseptic conditions, 100 μL of the bacterial suspension was taken and evenly spread on the cooled and solidified culture medium.

[0115] c. Using sterile forceps, place a 6mm diameter sterile Oxford cup onto an agar plate and apply gentle pressure to ensure good contact. Add 200μL of the composition to each Oxford cup; the blank control group is water. Incubate at 37℃ for 72 hours under anaerobic conditions. Measure the diameter of the effective inhibition zone of the test solution in each petri dish. Repeat the measurement four times for each concentration and calculate the average value.

[0116] Criteria for judging antibacterial effect:

[0117] An inhibition zone diameter >20mm is considered highly sensitive; 10mm-20mm is considered moderately sensitive; <10mm is considered lowly sensitive; and the absence of an inhibition zone is considered resistant.

[0118] The antibacterial results are shown in Table 2 below (unit: mm):

[0119] Table 2

[0120] Serial Number Average of 4 measurements (mm) Blank control group 6 (cup diameter) 1 22.5 2 24.6 3 25.8 4 26.7 5 29.4 6 26.4 7 27.5 8 26.7 9 29.2 10 28.5 11 28.2 12 29.6 13 14.6 14 16.4 15 19.3

[0121] As can be seen from Table 2, numbers 1-12 all have an inhibitory effect on Propionibacterium acnes. The antibacterial effect will decrease if the component is missing.

[0122] Products numbered 1-12 all have an average inhibition zone diameter greater than 20 mm against Propionibacterium acnes, indicating a highly sensitive effect. Products numbered 13-15 have a moderately sensitive effect against Propionibacterium acnes.

[0123] Furthermore, according to statistical analysis, the improvement effect of numbers 1-12 was significantly greater than that of numbers 13-15, with P values ​​all less than 0.01.

[0124] Through the above-mentioned antibacterial effect test on Propionibacterium acnes, the inventors unexpectedly discovered that, based on the water-soluble azelaic acid system, when combined with the extract and pyridoxine, it has a synergistic effect in inhibiting Propionibacterium acnes.

[0125] Example 12: Irritation, Effectiveness, and Functional Effects

[0126] Experiments were conducted to evaluate the irritant, efficacy, and functional effects of samples numbered 5-7.

[0127] The testing method is as follows: Sixty acne patients aged 20-45 years were selected, with half being male and half female. The patients frequently experienced acne and had large acne areas.

[0128] The formulations obtained from numbers 5-7 were used, and the positive control drugs clindamycin phosphate gel and Brøndal supramolecular salicylic acid were used as controls.

[0129] 40 people were selected, 10 people were selected for clindamycin phosphate gel, and 10 people were selected for Boralda supramolecular salicylic acid.

[0130] Apply once each morning and evening after cleansing, for 10 consecutive days;

[0131] On days 5 and 10, patients were surveyed using questionnaires to assess the product's effectiveness and irritation.

[0132] The specific standards are as follows:

[0133] Table 3 Validity Criteria

[0134]

[0135] Table 4 Irritation Standards

[0136] Irritating standard Significant stimulation Stinging sensation, obvious redness, peeling, dryness More exciting There is a stinging sensation, noticeable redness, slight peeling, and dryness. Milder Slight stinging sensation, no peeling, no redness, and minimal dryness. mild The product is comfortable, non-irritating, does not cause redness, and does not dry out the skin.

[0137] The results are shown in Table 5:

[0138] As can be seen from Table 5, the products prepared by numbers 5, 6 and 7 have good effects and are significantly less irritating than clindamycin phosphate gel and Boralda supramolecular salicylic acid. They are mild and effective, and their effects are better than those of clindamycin phosphate gel and Boralda supramolecular salicylic acid commonly used in clinical practice.

[0139] Table 5 Comparison of Patient Usage

[0140]

[0141] Example 13 Exfoliation Effect

[0142] Exfoliation effectiveness tests were conducted on samples numbered 5, 6, 13, and 14.

[0143] The specific experimental method is generally similar to the applicant's prior patent CN117530874A, as follows:

[0144] The stratum corneum of human skin was tested using the German CK Visioscan (VC20) skin texture scanner, including initial value testing, product use, efficacy testing, and statistical analysis. All tests were conducted on the sample in accordance with the physicochemical testing methods in Chapter 4 of the "Cosmetic Safety Technical Specifications".

[0145] (1) Subjects and testing conditions:

[0146] In a constant temperature test environment with a temperature of (21±1)℃ and a humidity of (40-60)%, 30 volunteers with more stratum corneum on their elbows were selected.

[0147] Inclusion criteria:

[0148] ① Age 20-45 years old, all are indoor workers (excluding pregnant or breastfeeding women);

[0149] ② Individuals without serious systemic diseases, immunodeficiency, or autoimmune diseases;

[0150] ③ Individuals without active allergic diseases;

[0151] ④ No one with a highly sensitive constitution;

[0152] ⑤ Those who have not used hormone-based drugs or immunosuppressants in the past month;

[0153] ⑥ Individuals who have not participated in other clinical trials at the current or recent three-month testing location;

[0154] Termination and exclusion criteria:

[0155] ① The volunteer requested to terminate the experiment for his own reasons;

[0156] ② Adverse reactions in volunteers prevented the continuation of the trial;

[0157] ③ Poor volunteer compliance, for example, the use of other skin care products that could affect the trial during the test.

[0158] (2) Data testing:

[0159] Thirty volunteers were selected. The test was conducted using a randomized, double-blind approach. The skin around the left or right elbow with more keratinized skin was randomly selected as the test area. The test area was marked and kept in place. During the test, no other products such as shower gels or cosmetics that could affect the test results were used on the test area. Volunteers numbered 5, 6, 7, 13, and 14 applied the product to the same location for 14 consecutive days, once in the morning and once in the evening. During the test, other cosmetics or bath products with exfoliating effects could not be used at the same time.

[0160] Volunteers numbered 5, 6, 7, 13, and 14 were tested for the number of exfoliated stratum corneum cells (SEsc) on days 0, 7, and 14, respectively. The test area was kept dry for one hour before each test. During the test, subjects were required to sit quietly for at least 20 minutes in a constant temperature and humidity environment (20-22℃, relative humidity 40%-60%). The SEsc value of the fixed area was measured by the measurement personnel, and three measurements were taken for each area, with the average value taken. The lower the SEsc value, the less stratum corneum in the test area, and the better the exfoliation effect.

[0161] (3) Experimental results:

[0162] Table 6. Effects of stratum corneum shedding

[0163]

[0164] Table 6 shows that products prepared in numbers 5, 6, and 7 reduced the number of stratum corneum exfoliations (SEsc) in volunteers, with a reduction of more than 24% after 14 days. This indicates that products prepared in numbers 5, 6, and 7 have a good effect on reducing stratum corneum exfoliation.

[0165] Although the present invention has been disclosed above with reference to preferred embodiments, it is not intended to limit the present invention. Anyone 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 composition for exfoliation and acne improvement, characterized in that, Its components include a water-soluble azelaic acid system, pyridoxine or pyridoxine derivatives, traditional Chinese medicine extracts, and water; The mass ratio of the water-soluble azelaic acid system, pyridoxine or pyridoxine derivatives, traditional Chinese medicine extract and water is 0.5-20:0.1-10:0.5-10:

100. The preparation method of traditional Chinese medicine extract includes the following steps: The Chinese herbal components are mixed, pulverized, and sieved to obtain a mixed powder. The mixed powder is then extracted with an ethanol aqueous solution of 75-85% by volume and filtered. The residue is then extracted repeatedly, the extracts are combined, concentrated, and dried to obtain the Chinese herbal extract. The Chinese herbal medicine is a combination of honeysuckle, ganoderma lucidum, phellodendron bark, centella asiatica, Paris polyphylla, salvia miltiorrhiza, and licorice in a mass ratio of 20-30:10-15:5-10:10-15:5-10:5-10:3-5.

2. The composition for exfoliation and acne improvement according to claim 1, characterized in that, The ratio of mixed Chinese herbal medicine powder to an ethanol aqueous solution with a volume fraction of 75-85% is 1g:3-10mL.

3. The composition for exfoliation and acne improvement according to claim 1, characterized in that, The preparation method of the water-soluble azelaic acid system is as follows: Azelaic acid, salicylic acid, and panthenol are mixed evenly and heated at 65-110℃ for 1-8 hours with stirring, so that azelaic acid, salicylic acid, and panthenol form a liquid organic substance through intermolecular hydrogen bonds, namely the water-soluble azelaic acid system.

4. A method for preparing the composition for exfoliation and acne improvement according to any one of claims 1-3, characterized in that, Includes the following steps: A composition for exfoliation and acne improvement can be obtained by mixing water-soluble azelaic acid system, pyridoxine or pyridoxine derivatives, traditional Chinese medicine extracts, and water evenly.

5. A cosmetic product, characterized in that, The composition for exfoliation and acne improvement according to any one of claims 1-3 is used.

6. The use of the composition for exfoliation and acne improvement according to any one of claims 1-3 in the preparation of daily chemical products.

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