An acne-repairing composition that promotes microcirculation in acne-prone skin and its application.
By combining vitamin K2, Swertia japonica extract, Guaiac extract, cerium oxide microspheres, and mulberry root extract, the problem of insufficient skin microcirculation in existing acne treatments is addressed, resulting in improved skin cell vitality, reduced skin roughness, and promotion of skin regeneration and repair.
Patent Information
- Application Number
- CN202411535939.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2024-10-31
- Publication Date
- 2025-10-28
- Estimated Expiration
- 2044-10-31
AI Technical Summary
Current acne treatments neglect to improve skin microcirculation, resulting in skin cells not receiving sufficient oxygen and nutrients, slowing down skin renewal and metabolism, making acne prone to recurrence, and increasing skin roughness.
The combination of vitamin K2, Swertia trifasciata extract, Guaiac extract, cerium oxide microspheres and mulberry root extract promotes blood circulation, enhances the elasticity and toughness of capillary walls, reduces capillary dilation, and promotes skin cell regeneration and repair through synergistic effects.
It significantly improves redness and acne, reduces skin roughness, increases cell vitality, enhances facial skin microcirculation, and strengthens the skin barrier function.
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Figure CN119367228B_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of cosmetic technology, and in particular to an acne-repairing composition that promotes microcirculation in acne-prone and sensitive skin, and its application. Background Technology
[0002] The skin microcirculation is a complex system and an important structure of the skin, composed of two parallel vascular plexuses in the deep and superficial layers. It plays a crucial role in storing blood, nourishing the skin, and maintaining the stability of the skin's microcirculation. As an important component of the skin barrier, changes in skin blood flow are influenced by various physiological, pathological, and environmental factors. Different skin conditions and topical medications can cause changes in skin blood flow, altering the skin microcirculation. Improving skin microcirculation can enhance skin cell activity, provide skin cells with sufficient nutrients and substances, while simultaneously clearing cellular metabolic waste and harmful substances, reducing collagen fiber oxidation, and thus delaying skin aging. Monitoring skin microcirculation provides insight into the skin's condition and is of paramount importance for beauty and skincare. Currently, most treatments for acne focus on balancing the skin's oil and water levels. These treatments often have limited impact on the transport and regulation of substances, energy, and biological information between cells and tissues, neglecting the improvement of skin microcirculation. However, microcirculation disorders cause continuous and irreversible damage to skin cells. They prevent skin cells from receiving sufficient oxygen and nutrients, slowing down skin renewal and metabolism, hindering skin repair and health, leading to intermittent acne breakouts, frequent relapses, and skin lesions.
[0003] Therefore, an acne-repairing composition that can improve cell vitality, promote blood circulation, enhance facial skin microcirculation, further reduce skin roughness, and improve rosacea and acne has broad application prospects. Summary of the Invention
[0004] Based on this, the purpose of the present invention is to overcome the shortcomings of the prior art and provide an acne-repairing composition that can improve cell vitality, promote blood circulation, enhance facial skin microcirculation, further reduce skin roughness, and improve rosacea and acne, thereby promoting microcirculation in acne-prone skin, as well as its preparation method and application.
[0005] To achieve the above objectives, the technical solution adopted by the present invention is as follows: an acne-repairing composition, comprising the following components in parts by weight: Vitamin K2 0.05-1 parts, Swertia japonica extract 0.1-1.5 parts, Guaiac extract 0.1-2 parts, cerium oxide microspheres 0.005-0.1 parts, and mulberry root extract 0.5-5 parts; wherein the cerium oxide microspheres have an average particle size of 0.2-3 μm, and the cerium oxide microspheres contain Ce. 3+ The Ce 3+The molar percentage of the cerium oxide microspheres is 30-38%.
[0006] Optionally, the average particle size of the cerium oxide microspheres is tested as follows: the cerium oxide microspheres are observed by scanning electron microscopy to determine the average particle size of the cerium oxide microspheres.
[0007] The preparation method of the cerium oxide microspheres of this invention is based on the following patent, application number: 202310697002.X, invention title: Cerium Oxide Microspheres and Their Preparation Method, Application and Cosmetics. Specifically, a method for preparing cerium oxide microspheres includes the following steps:
[0008] A precursor solution was prepared by mixing a cerium-containing precursor with water.
[0009] A pH adjuster is added to the precursor solution to prepare a first solution;
[0010] A dispersion medium is added to the first solution to prepare a second solution; the cerium-containing precursor accounts for 3-7% of the mass of the second solution.
[0011] The second solution is then heated to react.
[0012] Preferably, the step of preparing the precursor solution includes at least one of the following conditions:
[0013] (1) The cerium-containing precursor includes one or more of cerium nitrate hexahydrate and cerium nitrate; (2) The mass-to-volume ratio of the cerium-containing precursor to the water is (20-120) g: (10-60) mL;
[0014] Preferably, the step of preparing the first solution includes at least one of the following conditions:
[0015] (1) The pH adjuster includes one or more of acetic acid, formic acid and propionic acid; (2) The mass-to-volume ratio of the cerium-containing precursor and the pH adjuster is (20-120) g: (20-120) mL;
[0016] Preferably, the step of preparing the second solution includes at least one of the following conditions:
[0017] (1) The dispersion medium includes ethylene glycol; (2) The mass-to-volume ratio of the cerium-containing precursor to the dispersion medium is (20-120) g: (600-700) mL;
[0018] Preferably, the heating reaction includes at least one of the following conditions:
[0019] (1) The pressure of the heating reaction is 0.5 MPa-4 MPa; (2) The temperature of the heating reaction is 160℃-170℃; (3) The time of the heating reaction is 140 min-180 min; (4) The heating reaction is carried out in a Hastelloy pressure-resistant reactor;
[0020] Optionally, the heating reaction is carried out in a Hastelloy pressure vessel with a volume of 1L.
[0021] The vitamin K2 provided by this invention is a fat-soluble vitamin in the vitamin K family, an important family of nutrients that has a significant impact on normal human function. It can directly or indirectly participate in and regulate many physiological processes related to skin health. *Swertia indicum*, the dried whole herb of *Swertia indicum*, a plant in the Gentianaceae family, is one of the main sources of the Tibetan medicine Tida. It is an annual or perennial herb with antioxidant and anti-inflammatory effects. Cerium oxide microspheres are a type of oxide nanomaterial that has been extensively studied. Cerium oxide microspheres have good biocompatibility, and their surface Ce... 3+ and Ce 4+ Ions can rapidly interconvert, giving them excellent redox properties and self-regeneration properties, and exhibiting superior antibacterial activity in wound healing. The root bark of mulberry plants mainly contains flavonoids, coumarins, aromatic benzofuran derivatives, polysaccharides, and other chemical components, which have the effects of lowering blood pressure, inhibiting bacteria, and relieving pain.
[0022] This invention provides an acne-repairing composition. During actual experiments, the inventors discovered that when Vitamin K2, Swertia japonica extract, Guaiac wood extract, cerium oxide microspheres, and mulberry root extract are present simultaneously, the five components work synergistically to reduce skin roughness and improve rosacea and acne. Swertia japonica extract, mulberry root extract, and Guaiac wood extract work together to possess anti-inflammatory and antibacterial properties, inhibiting the growth of acne-causing bacteria such as Propionibacterium acnes and reducing inflammatory responses. The active ingredients in Swertia japonica extract and mulberry root extract, synergistically with Guaiac wood extract, can soothe and calm the skin, reduce vasodilation, promote local blood circulation, and alleviate rosacea. This application also includes vitamin K2 and cerium oxide microspheres, which can further protect vascular endothelial cells, enhance the elasticity and toughness of capillary walls, reduce capillary dilation, and enhance the resistance of capillary walls. At the same time, the addition of vitamin K2 and cerium oxide microspheres can further promote blood circulation, promote skin cell regeneration and repair, enhance skin barrier function, and improve skin roughness.
[0023] Preferably, the acne-repairing composition comprises the following components in parts by weight: 0.1-0.8 parts vitamin K2, 0.6-1.2 parts swertia extract, 0.8-1.5 parts guaiac extract, 0.01-0.05 parts cerium oxide microspheres, and 2-4 parts mulberry root extract.
[0024] Preferably, the total mass percentage of vitamin K2 and cerium oxide microspheres in the acne-repairing composition is 2-10%; and / or, the mass percentage of Swertia japonica extract in the acne-repairing composition is 10-20%; and / or, the mass percentage of mulberry root extract in the acne-repairing composition is 40-60%.
[0025] During the actual research process, the inventors discovered that the weight proportions of the components in the acne-repairing composition affect the performance of the product. When the weight proportions of the components are further selected within the above range, the resulting product has superior effects in improving cell vitality, promoting blood circulation, enhancing facial skin microcirculation, further reducing skin roughness, and improving redness and acne.
[0026] Preferably, the preparation method of the *Swertia argyi* extract is as follows:
[0027] (1) After drying, Indian swert sprouts are pulverized and sieved to obtain Indian swert sprout powder; the mesh size of the Indian swert sprout powder is 100-150 mesh;
[0028] (2) Extract the Indian swert powder with 15-30 times the amount of ethanol solution, concentrate it to a paste, and dry it to constant weight to obtain the Indian swert extract;
[0029] More preferably, the volume fraction of the ethanol solution is 70-90%; the extraction is ultrasonic extraction, the ultrasonic extraction temperature is 30-40℃, the ultrasonic extraction time is 0.5-1h, and the ultrasonic extraction power is 200-250W; the drying temperature is 60-70℃.
[0030] Optionally, the preparation method of the *Swertia argyi* extract is as follows:
[0031] (1) After drying, Indian swert sprouts are pulverized and sieved to obtain Indian swert sprout powder; the mesh size of the Indian swert sprout powder is 100-150 mesh;
[0032] (2) Extract the Indian swert sprout powder with 15-30 times the amount of ethanol solution, collect the supernatant and extract with organic solvent, concentrate the extract to paste, and dry to constant weight to obtain the Indian swert sprout extract.
[0033] Preferably, the volume fraction of the ethanol solution is 70-90%; the extraction is ultrasonic extraction, the ultrasonic extraction temperature is 30-40℃, the ultrasonic extraction time is 0.5-1h, and the ultrasonic extraction power is 200-250W; the organic solvent is at least one of chloroform, ethyl acetate, petroleum ether, and ethyl acetate; and the drying temperature is 60-70℃.
[0034] The preparation method of *Swertia natans* extract affects the performance of the final acne-repairing composition. The conventional method involves ultrasonic extraction followed by organic solvent extraction. This ultrasonic extraction followed by organic solvent extraction may affect the proportion of active ingredients in the *Swertia natans* extract. Different organic solvents result in different active ingredients in the extracted *Swertia natans* extract, and the proportions can vary significantly. During their research, the inventors discovered that a method that does not use organic solvent extraction, but only ultrasonic extraction, produces *Swertia natans* extract that synergizes better with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract. The resulting product exhibits superior effects in improving cell vitality, promoting blood circulation, enhancing facial skin microcirculation, further reducing skin roughness, and improving rosacea and acne.
[0035] Preferably, the preparation method of the mulberry root extract is as follows:
[0036] (1) After drying the mulberry root, crush it and sieve it to obtain mulberry root powder; the mesh size of the mulberry root powder is 100-150 mesh.
[0037] (2) Extract mulberry root powder with 20-60 times the amount of methanol solution, concentrate it to a paste, and dry it to constant weight to obtain the mulberry root extract;
[0038] Preferably, the volume fraction of the methanol solution is 70-90%; the extraction is a flash extraction, the flash extraction temperature is 25-30℃, the flash extraction time is 50-80s, the flash extraction voltage is 150-250V, and the flash extraction speed is 4000-5500r / min; the drying temperature is 40-50℃.
[0039] More preferably, in step (2), 40-50 times the amount of methanol solution is used to extract mulberry root powder.
[0040] This invention provides a method for preparing the aforementioned acne-repairing composition, as detailed below:
[0041] (1) Dissolve vitamin K2 completely in GTCC (high-purity oil esterified from caprylic / capric acid and glycerol) to obtain the oil phase; the mass ratio of vitamin K2 to GTCC is 1:18-20;
[0042] (2) Dissolve guaiac extract, swine extract, mulberry root extract and cerium oxide microspheres in deionized water according to their weight proportions to obtain an aqueous phase; wherein the weight ratio of the total amount of guaiac extract, swine extract, mulberry root extract and cerium oxide microspheres to deionized water is 1:5-8.
[0043] (3) The oil phase and the water phase are ultrasonically mixed in a certain ratio to obtain the acne repair composition; the ratio of the oil phase and the water phase is 1:8-10.
[0044] Furthermore, the present invention provides the application of the acne-repairing composition in the preparation of skin care products.
[0045] Furthermore, the present invention provides a skin product comprising the aforementioned acne-repairing composition.
[0046] Preferably, the skin product further includes excipients, which are at least one of moisturizer, thickener, pH adjuster, emulsifier, preservative, fragrance, and deionized water.
[0047] Preferably, the skin care products include one of the following: toner, lotion, cream, mask, serum, and spray.
[0048] Optionally, the present invention provides an emulsion comprising the following components in weight percentage: 0.5-3% acne-repairing composition, 1-20% moisturizer, 0.05-0.5% thickener, 0.05-0.1% pH adjuster, 0.5-10% emulsifier, 0.2-3% preservative, 0.05-0.5% fragrance, and the balance being deionized water.
[0049] For example, the humectant includes at least one of glycerin, butylene glycol, and low molecular weight sodium hyaluronate; the thickener includes at least one of xanthan gum, carbomer 980, and high molecular weight cellulose; the emulsifier includes at least one of cocoyl oleate / caprylate, polydimethylsiloxane, hydrogenated palm kernel oil, cetearyl alcohol, polyglycerol-6 distearate, and polymethylsilsesquioxane; the preservative includes at least one of 1,3-propanediol, 1,2-hexanediol, and p-hydroxyacetophenone; and the pH adjuster includes at least one of arginine and disodium EDTA.
[0050] Compared to existing technologies, the beneficial effects of this invention are as follows: This invention provides an acne-repairing composition. In actual experiments, the inventors discovered that when Vitamin K2, Swertia japonica extract, Guaiac wood extract, cerium oxide microspheres, and mulberry root extract are present simultaneously, the five components work synergistically to reduce skin roughness and improve rosacea and acne. Swertia japonica extract, mulberry root extract, and Guaiac wood extract work together to possess anti-inflammatory and antibacterial properties, inhibiting the growth of acne-causing bacteria such as Propionibacterium acnes and reducing inflammatory responses. The active ingredients in Swertia japonica extract and mulberry root extract, synergistically with Guaiac wood extract, can soothe and calm the skin, reduce vasodilation, promote local blood circulation, and alleviate rosacea. This application also includes vitamin K2 and cerium oxide microspheres, which can further protect vascular endothelial cells, enhance the elasticity and toughness of capillary walls, reduce capillary dilation, and enhance the resistance of capillary walls. At the same time, the addition of vitamin K2 and cerium oxide microspheres can further promote blood circulation, promote skin cell regeneration and repair, enhance skin barrier function, and improve skin roughness. Attached Figure Description
[0051] Figure 1 The results of the acne treatment test using the lotion in Application Example 1 on days D0 and D28 are shown in the figure.
[0052] Figure 2 The graph shows the results of the redness reduction test using the emulsion in Application Example 1 on days D0 and D28;
[0053] Figure 3 The results of the acne treatment test using the contrasting application example 1 lotion on day D0 and day D28 are shown in the figure.
[0054] Figure 4 The results of the redness reduction test of the emulsion on day D0 and day D28 are shown in the comparative application example 1. Detailed Implementation
[0055] To better illustrate the purpose, technical solution, and advantages of this invention, the invention will be further described below in conjunction with the accompanying drawings and specific embodiments. The purpose is to provide a detailed understanding of the invention, not to limit it. All other embodiments obtained by those skilled in the art without inventive effort are within the scope of protection of this invention. Unless otherwise specified, the experimental reagents and instruments designed in the embodiments and comparative examples of this invention are commonly used reagents and instruments, all of which are commercially available. Unless otherwise specified, the experimental methods used in the embodiments and comparative examples are conventional methods; and unless otherwise specified, the raw materials used in parallel experiments are from the same batch.
[0056] Further explanation of the raw materials used in this invention:
[0057] Vitamin K2: HPLC ≥ 98%, catalog number V140453, purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.
[0058] Vitamin K1: HPLC ≥ 98%, catalog number V820401, purchased from Shanghai Maclean Biochemical Technology Co., Ltd.
[0059] Vitamin C: HPLC ≥ 98%, product number TC1384, purchased from Sichuan Jingcui Tiancheng Pharmaceutical Technology Co., Ltd.
[0060] Guaiac extract: L2-DZ-SCB3675-X, purchased from Zhenghe (Guangzhou) Biotechnology Co., Ltd.;
[0061] Cerium oxide microspheres: trade name: luminescence-stimulating factor TM The cerium oxide microspheres, purchased from Huawai Technology (Beijing) Co., Ltd., have an average particle size of 200 nm and contain Ce. 3+ The Ce 3+ The molar percentage of the cerium oxide microspheres is 32%;
[0062] Ordinary cerium oxide-1: Product number R005967, particle size 0.8-2mm, purchased from Shanghai Ron Reagent Co., Ltd.;
[0063] Ordinary cerium oxide-2: Product number C141507, particle size <5μm, purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.;
[0064] Mulberry leaf extract: Product number S28490, purchased from Shanghai Yuanye Biotechnology Co., Ltd.;
[0065] Sandalwood extract: Product number TZ095, purchased from Xi'an Tongze Biotechnology Co., Ltd.;
[0066] Licorice extract: Product number L860791, purchased from Shanghai Maclean Biochemical Technology Co., Ltd.;
[0067] Swertia trifasciata extract-1
[0068] The preparation method of the Swertia chili extract-1 includes the following steps:
[0069] (1) After drying, the Indian swert sprouts are crushed and sieved to obtain Indian swert sprout powder; the mesh size of the Indian swert sprout powder is 120 mesh.
[0070] (2) The Indian swert sprout powder was ultrasonically extracted with 20 times the amount of ethanol solution. The extraction was repeated twice. The extract was then passed through a 300-mesh sieve, and the filtrate was collected. The extract was concentrated under reduced pressure to a paste and dried to constant weight to obtain the Indian swert sprout extract. The volume fraction of the ethanol solution was 70%. The extraction temperature was 30°C, the extraction time was 1 hour, and the extraction power was 250W. The drying temperature was 60°C.
[0071] Swertia trifasciata extract-2
[0072] The preparation method of the Swertia chili extract-2 includes the following steps:
[0073] (1) After drying, the Indian swert sprouts are pulverized and sieved to obtain Indian swert sprout powder; the mesh size of the Indian swert sprout powder is 150 mesh.
[0074] (2) The Indian swert sprout powder was ultrasonically extracted with 30 times the amount of ethanol solution. The extraction was repeated twice. The extract was then passed through a 300-mesh sieve, and the filtrate was collected. The extract was concentrated under reduced pressure to a paste and dried to constant weight to obtain the Indian swert sprout extract. The volume fraction of the ethanol solution was 90%. The extraction temperature was 40°C, the extraction time was 0.5 h, and the extraction power was 200 W. The drying temperature was 70°C.
[0075] Swertia trifasciata extract-3
[0076] The preparation method of Swertia japonica extract-3, compared with Swertia japonica extract-1, only adds an organic solvent extraction process, including the following steps:
[0077] (1) After drying, the Indian swert sprouts are crushed and sieved to obtain Indian swert sprout powder; the mesh size of the Indian swert sprout powder is 120 mesh.
[0078] (2) The powder of Indian swert sprouts was extracted with 20 times the amount of ethanol solution. After the extraction was repeated twice, the supernatant was collected and extracted with organic solvent. The extraction was repeated three times. The extract was concentrated under reduced pressure to a paste and dried to constant weight to obtain the Indian swert sprout extract.
[0079] The volume fraction of the ethanol solution is 70%; the extraction is ultrasonic extraction, the ultrasonic extraction temperature is 30℃, the ultrasonic extraction time is 1h, and the ultrasonic extraction power is 250W; the drying temperature is 60℃; the organic solvent is chloroform.
[0080] Swertia trifasciata extract-4
[0081] The preparation method of the Swertia chilonis extract-4 is the same as that of Swertia chilonis extract-3, except that the organic solvent used for extraction is ethyl acetate. All other components, weight parts and preparation methods are exactly the same.
[0082] Swertia trifasciata extract-5
[0083] The preparation method of the Swertia chilonis extract-5 is the same as that of Swertia chilonis extract-3, except that the organic solvent used for extraction is petroleum ether. The other components, weight parts and preparation methods are exactly the same.
[0084] Mulberry Root Extract-1
[0085] The preparation method of the mulberry root extract-1 includes the following steps:
[0086] (1) After drying the mulberry root, crush it and sieve it to obtain mulberry root powder; the mesh size of the mulberry root powder is 100 mesh;
[0087] (2) Mulberry root powder was extracted with 40 times the amount of methanol solution. The extraction was repeated twice. The extract was then passed through a 300-mesh sieve, and the filtrate was collected. The extract was concentrated under reduced pressure to a paste and dried to constant weight to obtain the mulberry root extract. The volume fraction of the methanol solution was 75%. The extraction was a flash extraction with a temperature of 30°C, a time of 80 seconds, a voltage of 220V, and a rotation speed of 4000 r / min. The drying temperature was 40°C.
[0088] Mulberry Root Extract-2
[0089] The preparation method of the mulberry root extract-2 is the same as that of mulberry root extract-1, except that step (2) uses 50 times the amount of methanol solution to extract mulberry root powder. The other components, weight parts and preparation methods are exactly the same.
[0090] Mulberry Root Extract-3
[0091] The preparation method of the mulberry root extract-3 is the same as that of mulberry root extract-1, except that the volume fraction of the methanol solution in step (2) is different. The volume fraction of the methanol solution is 90%, and the other components, weight parts and preparation methods are exactly the same.
[0092] Mulberry Root Extract-4
[0093] The preparation method of the mulberry root extract-4 is the same as that of mulberry root extract-1, except that step (2) uses 20 times the amount of methanol solution to extract mulberry root powder. The other components, weight parts and preparation methods are exactly the same.
[0094] Mulberry Root Extract-5
[0095] The preparation method of the mulberry root extract-5 is the same as that of mulberry root extract-1, except that step (2) uses 60 times the amount of methanol solution to extract mulberry root powder. The other components, weight parts and preparation methods are exactly the same.
[0096] Examples and Comparative Examples
[0097] This application provides an acne-repairing and repairing composition. The components and weight parts of the acne-repairing and repairing composition in the examples and comparative examples are shown in Tables 1-1, 1-2, and 2 below.
[0098] The preparation method of the acne-repairing composition is as follows:
[0099] Vitamin K2 was fully dissolved in GTCC (a high-purity oil esterified from caprylic / capric acid and glycerol) to obtain the oil phase; the mass ratio of vitamin K2 to GTCC was 1:18.
[0100] Guaiac extract, Swertia agallocha extract, mulberry root extract, and cerium oxide microspheres were dissolved in deionized water in parts by weight to obtain an aqueous phase; wherein the total weight ratio of guaiaac extract, Swertia agallocha extract, mulberry root extract, and cerium oxide microspheres to deionized water was 1:5.
[0101] The oil phase and water phase are ultrasonically mixed in a certain ratio to obtain the acne-repairing composition; the ratio of oil phase to water phase is 1:10.
[0102] When preparing the proportionate acne-repairing composition, if the relevant component is unavailable, it can be omitted. If other components are available, they can be substituted according to the preparation method described above to obtain the final product.
[0103] Table 1-1
[0104] Components (parts by weight) Example 1 Example 2 Example 3 Example 4 Example 5 Example 6 Vitamin K2 0.5 0.1 0.8 0.3 0.05 1 Swertia trifasciata extract-1 1 0.8 0.7 1.2 1.5 0.1 Guaiac extract 1.5 1.2 1 0.8 0.1 2 Cerium oxide microspheres 0.01 0.05 0.03 0.04 0.005 0.1 Mulberry Root Extract-1 4 2 3 4 5 0.5
[0105] Table 1-2
[0106]
[0107]
[0108] Table 2
[0109]
[0110]
[0111] Application examples
[0112] Application Examples 1-15, Comparative Application Examples 1-14 and Blank Application Examples of the present invention provide an emulsion, the components (mass percentage) of which are shown in Table 3;
[0113] The acne-repairing compositions used in Application Examples 1-14 are the acne-repairing compositions prepared in Examples 1-14, while the acne-repairing compositions used in Comparative Application Examples 1-14 are the acne-repairing compositions prepared in Comparative Examples 1-14. For example, the acne-repairing composition used in Application Example 1 is the acne-repairing composition prepared in Example 1, the acne-repairing composition used in Application Example 2 is the acne-repairing composition prepared in Example 2, and the acne-repairing composition used in Comparative Application Example 1 is the acne-repairing composition prepared in Comparative Example 1, and so on.
[0114] The acne repair composition used in Application Example 15 is the acne repair composition prepared in Example 1.
[0115] The method for preparing the emulsion according to the present invention includes the following steps:
[0116] (1) Mix phase A with water and stir. Heat to 80°C and homogenize at 1200 rpm for 5 minutes. After homogenization, keep warm for later use to obtain pre-prepared phase A.
[0117] (2) Mix the B phase, heat it to 80°C, and then homogenize it at 1200 rpm for 5 minutes. After homogenization, keep it warm for later use to obtain the pre-made B phase.
[0118] (3) Mix the C phase and heat it to 60°C to melt it, thus obtaining the pre-made C phase;
[0119] (4) Heat the pre-prepared phase A to 80°C, add the pre-prepared phase B at 300 rpm, stir and mix, then cool down to 60°C, add the pre-prepared phase C at 300 rpm and stir and mix, then cool down to below 45°C, add the acne repair composition and fragrance and continue stirring for 5 minutes, finally add arginine to adjust the pH to 6.0, then stop stirring, discharge the material, and obtain the emulsion.
[0120] The preparation methods for the emulsions provided in the other application examples are consistent with those in application example 1; if the relevant components are not available, they can be omitted.
[0121] The selection of application components and their mass percentages is shown in Table 3 below.
[0122] Table 3
[0123]
[0124]
[0125] Performance testing
[0126] Performance Testing - 1. Cell Viability Test
[0127] Experimental materials: Phosphate-buffered saline (PBS), Shanghai Solarbio; Thiazol blue (MTT), Yuanye Biotechnology; Dimethyl sulfoxide (DMSO), Tianjin Damao; Complete culture medium, Maclean; High glucose medium 1×DMEM, Gibco; Fetal bovine serum (FBS), Gibco; Keratinocytes purchased from Guangzhou Customs Technology Center; Human skin fibroblasts HSF purchased from Kunming Cell Bank, Chinese Academy of Sciences.
[0128] Experimental procedure: The cell suspension was seeded into 96-well cell culture plates and incubated for 24 hours. The complete culture medium was aspirated from the wells, PBS was added, and the plates were exposed to UVB light for 15 minutes (irradiation intensity: 80 μW / cm²). 2 Irradiation dose: 80 mJ / cm 2 );
[0129] The blank control group was given complete culture medium and did not require irradiation.
[0130] After irradiation for 15 min, the PBS solution was aspirated. The experimental group was given complete culture medium, with 100 μL of 0.5% acne-repairing composition added to each well. The model group received only PBS, without the acne-repairing composition. Cells in each group were cultured for 24 h. The culture plates were then removed, and 20 μL of MTT solution was added to each well. The plates were incubated for 3 h. The liquid in the wells was removed, and 100 μL of DMSO was added to each well. After shaking for 15 min, the absorbance (OD value) was measured at 570 nm using a microplate reader, and cell viability was calculated.
[0131] All experiments were performed in parallel at least three times. Experimental data are expressed as mean ± standard deviation (Mean ± SD). Cell viability was calculated using the following formula:
[0132] Cell viability = (OD value of sample wells - OD value of zeroing wells) / (OD value of blank control wells - OD value of zeroing wells) × 100%.
[0133] The test results are shown in Table 4.
[0134] Table 4
[0135]
[0136]
[0137] Note: When performing statistical analysis using the t-test method, the significance of the model group compared with the blank control group is indicated by #, with P-value < 0.05 indicated by # and P-value < 0.01 indicated by ##; the significance of the sample group compared with the blank control group is indicated by *, with P-value < 0.05 indicated by *, P-value < 0.01 indicated by **, and P-value < 0.001 indicated by ***.
[0138] The test results are shown in Table 4. The acne repair composition prepared in the embodiments provided in this application can effectively promote the vitality of keratinocytes in the epidermis and fibroblasts in the dermis under UVB irradiation damage.
[0139] In this application, the acne-repairing composition optimizes the extraction conditions of *Swertia natans* extract and mulberry root extract. During actual research, the inventors discovered that in the preparation method of *Swertia natans* extract, extraction without organic solvents, but only by ultrasonic extraction, results in a better synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract, leading to a product with superior cell-enhancing effects. Similarly, the inventors found that extracting mulberry root powder with 40-50 times the volume of methanol solution results in a synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract, leading to a product with superior cell-enhancing effects.
[0140] During their research, the inventors discovered that vitamin K2 and cerium oxide microspheres can further protect vascular endothelial cells, enhance the elasticity and resilience of capillary walls, reduce capillary dilation, and strengthen the resistance of capillary walls, resulting in products with superior cell vitality enhancement effects. When vitamin K2, any one of the following—Swertia argyi extract, Guaiac extract, cerium oxide, or mulberry root extract—is lacking, or when any one of the active ingredients is lacking, increasing the weight proportions of other ingredients results in acne-repairing compositions in Comparative Examples 1-7, where the skin cell activation effect is far less than in the examples, with a significant decrease in keratinocyte and fibroblast vitality. Furthermore, when other functionally similar components are used to replace any one of vitamin K2, Swertia argyi extract, Guaiac extract, cerium oxide, or mulberry root extract, the effects in the comparative examples are also far inferior to those obtained using the technical solution of this application.
[0141] When the above-mentioned components are within the scope of this application, they have a relatively ideal synergistic effect.
[0142] Example 2: ATP test
[0143] Experimental Procedure: Keratinocytes were cultured in vitro and incubated in DMEM medium with or without an acne-repairing composition (the acne-repairing composition was diluted to 0.005% using the medium solution). A blank control group was used without the acne-repairing composition. After 48 hours of incubation, intracellular ATP levels were measured at 24 and 48 hours using a commercially available kit (catalog number S0026, purchased from Beyotime). Intracellular ATP levels were determined using a bioluminescence assay. A positive control group was used with 0.01% cytochrome C. The relative ATP levels were calculated as follows:
[0144] Relative ATP content (% blank control group) = ATP content experimental group / ATP content blank control group * 100%. The experimental results are shown in Table 5.
[0145] Table 5
[0146]
[0147]
[0148] Note: When performing statistical analysis using the t-test method, significance compared with the blank control group is indicated by *, P-value < 0.05 is indicated by *, P-value < 0.01 is indicated by **, and P-value < 0.001 is indicated by ***.
[0149] As can be seen from the table above, the acne-repairing composition prepared in the embodiments provided in this application has a relatively higher ATP content.
[0150] In this application, the acne-repairing composition optimizes the extraction conditions of *Swertia natans* extract and mulberry root extract. During actual research, the inventors discovered that in the preparation method of *Swertia natans* extract, extraction without organic solvents, but only ultrasonic extraction, results in a better synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract, leading to a product with a superior effect in increasing relative ATP content. Similarly, the inventors found that extracting mulberry root powder with 40-50 times the volume of methanol solution results in a synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract, leading to a product with a superior effect in increasing relative ATP content.
[0151] During their research, the inventors discovered that vitamin K2 and cerium oxide microspheres can further protect vascular endothelial cells, enhance the elasticity and toughness of capillary walls, reduce capillary dilation, and strengthen the resistance of capillary walls. The resulting product has a superior effect in increasing relative ATP content.
[0152] When any one of the following is lacking—vitamin K2, Swertia japonica extract, guaiac wood extract, cerium oxide, or mulberry root extract—or any one of the active ingredients, increasing the weight percentage of other ingredients results in acne-repairing compositions in Comparative Examples 1-7 where the increase in relative ATP content is far less than in the examples. Furthermore, when other functionally similar components are used to replace any one of vitamin K2, Swertia japonica extract, guaiac wood extract, cerium oxide, or mulberry root extract, the effects in the comparative examples are also far less than those obtained using the technical solution of this application.
[0153] When the above-mentioned components are within the scope of this application, they have a relatively ideal synergistic effect.
[0154] Example 3: Blood Flow Test
[0155] Zebrafish embryos are completely transparent and have become a classic research model for studies related to the human cardiovascular system. Under a microscope, the flow of blood cells in the blood vessels is clearly visible, making zebrafish embryos ideal for testing the effects of samples on promoting blood circulation.
[0156] (1) Zebrafish source and culture: Spawning tests were conducted using wild-type AB strain zebrafish (Danio rerio) from a reliable source (China National Zebrafish Resource Center). Broodstock should have good reproductive capacity—ideally 6-12 months old. Sidecrossing should be used as much as possible to maintain genetic diversity. Purebred broodstock should be replaced with a new batch after 5 generations. Broodstock should not have obvious signs of infection or disease and should not have undergone drug treatment within the past 2 months. Broodstock should be acclimatized to the laboratory for at least 14 days before being introduced for spawning tests.
[0157] (2) Test grouping: Select healthy zebrafish embryos that are 3 days old after fertilization. The test requires setting up a blank control group (fish embryo culture medium / solvent solution) and a test group (test substance).
[0158] Forty fish embryos were randomly selected and transferred to a 6cm culture dish, and 8mL of fish embryo culture medium was added.
[0159] Forty fish embryos were randomly selected and transferred to a 6cm culture dish. 8mL of 0.05g / L caffeine solution was added (the working solution was prepared using fish embryo culture medium to obtain the 0.05g / L caffeine solution).
[0160] Forty fish embryos were randomly selected and transferred to a 6cm culture dish. 8mL of the test solution was added (the test solution was a 0.1% acne repair composition prepared with dimethyl sulfoxide solvent).
[0161] Each group was incubated in a constant temperature incubator at 28±1℃ for 2±0.5h.
[0162] Anesthetize fish embryos for 2 minutes with tricaine working solution (weigh 200 mg tricaine (analytical grade) and dissolve in 48.95 mL of water to prepare the stock solution, refrigerate, effective within 30 days; dilute the stock solution to 0.04% with fish embryo culture medium, and prepare fresh before use). Take a 20-second photograph of the dorsal aorta of the fish embryo under a microscope.
[0163] (3) Data and results calculation: The relative velocity of blood flow in the dorsal aorta of each fish embryo was measured using software such as DanioScope and the average value was taken.
[0164] Calculate the blood circulation promotion rate: Promotion rate = (TC) / C × 100%;
[0165] Where: T—the average relative velocity of blood flow in the dorsal aorta of fish embryos in the test substance treatment group; C—the average relative velocity of blood flow in the dorsal aorta of fish embryos in the blank control group;
[0166] Table 6
[0167]
[0168]
[0169] Note: When performing statistical analysis using the t-test method, the significance of the model group compared with the blank control group is indicated by #, with P-value < 0.05 indicated by # and P-value < 0.01 indicated by ##; the significance of the sample group compared with the blank control group is indicated by *, with P-value < 0.05 indicated by * and P-value < 0.01 indicated by **.
[0170] As can be seen from the table above, the acne-repairing composition prepared in the embodiments provided in this application has a better effect on promoting blood circulation.
[0171] In this application, the acne-repairing composition optimizes the extraction conditions of *Swertia argyi* extract and mulberry root extract. During actual research, the inventors discovered that in the preparation method of *Swertia argyi* extract, extraction without organic solvents, but only by ultrasonic extraction, results in a better synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract, leading to a product with superior blood circulation-promoting effects. Similarly, the inventors found that extracting mulberry root powder with 40-50 times the volume of methanol solution results in a synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract, leading to a product with superior blood circulation-promoting effects.
[0172] During their research, the inventors discovered that vitamin K2 and cerium oxide microspheres can further protect vascular endothelial cells, enhance the elasticity and toughness of capillary walls, reduce capillary dilation, and strengthen the resistance of capillary walls, resulting in a product with superior blood circulation-promoting effects.
[0173] When any one of the following is lacking—vitamin K2, Swertia japonica extract, guaiac wood extract, cerium oxide, or mulberry root extract—or any one of the active ingredients, increasing the weight proportions of other ingredients results in acne-repairing compositions in Comparative Examples 1-7 that are far less effective in promoting blood circulation than those in the Examples. Furthermore, when other functionally similar components are used to replace any one of the following—vitamin K2, Swertia japonica extract, guaiac wood extract, cerium oxide, or mulberry root extract—the resulting comparative examples are also far less effective than those obtained using the technical solution of this application.
[0174] When the above-mentioned components are within the scope of this application, they have a relatively ideal synergistic effect.
[0175] Example of effect 4
[0176] This invention verifies the safety of its application on human skin using efficacy examples. Following the "Cosmetic Safety Technical Specifications" (2015) for human skin patch testing, 33 volunteers aged 18-60 years were recruited. The testing environment was a temperature of (21±1)℃ and a humidity of (50±10)%. Volunteers washed their forearms with water. After 5-10 minutes, once the moisture had evaporated, the testers applied 0.020-0.025 mL of each sample emulsion to each chamber of a 10-well patch applicator. The inner sides of both forearms of the volunteers were selected, avoiding the skin around the joints of the front and back of the hands. Each arm was fitted with a patch applicator and marked accordingly. The patch application lasted for 24 hours. After removing the patch applicator and wiping away any remaining sample, skin reactions were observed at 0.5h, 24h, and 48h. The results were recorded according to the skin reaction grading standards in the "Cosmetic Safety Technical Specifications" (2015). As shown in Table 7, skin reactions were divided into four rating levels; the higher the score, the more severe the skin irritation.
[0177] The test results are as follows: 0 cases of withdrawal and 0 cases of adhesive tape allergy were observed in the technical solution provided by this invention. No adverse reactions occurred in the application case, control application case, and blank application case.
[0178] Table 7
[0179]
[0180]
[0181] Example 5: Human Efficacy Test
[0182] This effect test examines the effects of application examples 1-15, comparative application examples 1-14, and a blank application example on improving human skin TEWL, moisturizing, roughness, acne count, and rosacea.
[0183] The specific testing method is as follows: Volunteers with sensitive skin aged 18-50 (lactate stinging score >3) were selected according to the "Cosmetic Safety Technical Specifications" (2015) and randomly divided into 30 groups of 8 people each. The volunteers had obvious acne, blackheads and papules. Under normal circumstances, the volunteers used the product on their entire face for 28 days. After cleansing and moisturizing, the volunteers applied an appropriate amount of lotion to their face every morning and evening and massaged it into the skin. The lotion could be layered on acne-prone areas. The product was used on the entire face once in the morning and once in the evening. Follow-up visits were conducted on days 1, 3, 7, 14 and 28.
[0184] On the day of their visit, volunteers washed their faces with water in the test area without applying any products and sat quietly for 20 minutes in an air-conditioned room with a temperature of 21±1℃ and humidity of 50±10%. The improvement in facial acne indicators was quantified and photographed using instruments, including acne count (categorical count: comedones and papules, assessed using VISIA and by a doctor, respectively), Tewameter™ Hex to measure transepidermal water loss (TEWL), Corneometer CM 825 to measure hydration, VC 20Plus to measure skin roughness, and MX 18 to measure telangiectasia.
[0185] Improvement rate before and after use = |X mean before use -X mean after use| / X mean before use × 100%; The calculation results are shown in Table 8. The improvement rate presented in Table 8 is the improvement rate at the follow-up visit on day 28.
[0186] Table 8
[0187]
[0188]
[0189]
[0190]
[0191] Note: * indicates that the difference is statistically significant compared with the blank application example (P < 0.05).
[0192] As shown in the table above, the acne-repairing composition prepared in the embodiments of this application, when formulated into an emulsion, exhibits excellent effects in improving facial skin microcirculation, further reducing skin roughness, and improving rosacea and acne. Among these, Figure 1 The graph shows the acne treatment test results of the lotion used in Example 1 on days D0 and D28. Figure 2 The graph shows the results of the redness reduction test using the emulsion in Application Example 1 on days D0 and D7. Figure 3 The image shows the acne treatment test results of the lotion on day D0 and day D28 in Example 1. Figure 4 The results of the redness reduction test of the emulsion on days D0 and D28 in Example 1 are shown in the comparative application diagram. Figure 1-4As can be seen from the comparison, the lotion of Example 1 of the present invention has a very obvious effect on improving rosacea and acne.
[0193] In this application, the acne-repairing composition optimizes the extraction conditions of *Swertia argyi* extract and mulberry root extract. During actual research, the inventors discovered that in the preparation method of *Swertia argyi* extract, extraction without organic solvents, but only by ultrasonic extraction, results in a better synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract. The resulting product exhibits superior effects in improving facial skin microcirculation, further reducing skin roughness, and improving rosacea and acne. Similarly, the inventors found that extracting mulberry root powder with 40-50 times the amount of methanol solution results in a better synergistic effect with vitamin K2, guaiac extract, cerium oxide microspheres, and mulberry root extract, leading to a product with superior effects in improving facial skin microcirculation, further reducing skin roughness, and improving rosacea and acne.
[0194] During their research, the inventors discovered that vitamin K2 and cerium oxide microspheres can further protect vascular endothelial cells, enhance the elasticity and toughness of capillary walls, reduce capillary dilation, and strengthen the resistance of capillary walls. The resulting product has superior effects in improving facial skin microcirculation, further reducing skin roughness, and improving rosacea and acne.
[0195] When any of the following ingredients are lacking, such as vitamin K2, swertia extract, guaiac extract, cerium oxide, or mulberry root extract, or any of the active ingredients, increasing the weight proportions of other ingredients, the resulting acne-repairing compositions in Comparative Examples 1-7 are far less effective than those in the examples in improving facial skin microcirculation, reducing skin roughness, and improving rosacea and acne.
[0196] Furthermore, when other functionally similar components are substituted for one of vitamin K2, Swertia japonica extract, guaiacol, cerium oxide, or mulberry root extract, the comparative results are far inferior to those obtained by using the technical solution of this application.
[0197] When the above-mentioned components are within the scope of this application, they have a relatively ideal synergistic effect.
[0198] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and are not intended to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the essence and scope of the technical solutions of the present invention.
Claims
1. An acne-removing and repairing composition, characterized in that, The product comprises the following components in parts by weight: Vitamin K2 0.05-1 part, Swertia japonica extract 0.1-1.5 parts, Guaiac extract 0.1-2 parts, Cerium oxide microspheres 0.005-0.1 parts, and Morus alba root extract 0.5-5 parts; wherein the average particle size of the Cerium oxide microspheres is 0.2-3 μm, and the Cerium oxide microspheres contain Ce. 3+ The Ce 3+ The molar percentage of cerium oxide microspheres is 30-38%; the preparation method of the Swertia chia extract is as follows: (1) After drying, Indian swert sprouts are pulverized and sieved to obtain Indian swert sprout powder; the mesh size of the Indian swert sprout powder is 100-150 mesh; (2) The Indian swert sprout powder was extracted by ultrasonic extraction with 15-30 times the amount of ethanol solution, concentrated to a paste, and dried to constant weight to obtain the Indian swert sprout extract; The preparation method of the mulberry root extract is as follows: (a) After drying the mulberry root, pulverize and sieve it to obtain mulberry root powder; the mesh size of the mulberry root powder is 100-150 mesh; (b) The mulberry root powder was flash-extracted with 40-50 times the amount of methanol solution, concentrated to a paste, and dried to constant weight to obtain the mulberry root extract.
2. The acne-removing and repairing composition as described in claim 1, characterized in that, It includes the following components in parts by weight: Vitamin K2 0.1-0.8 parts, Swertia japonica extract 0.6-1.2 parts, Guaiac wood extract 0.8-1.5 parts, Cerium oxide microspheres 0.01-0.05 parts, and Mulberry root extract 2-4 parts.
3. The acne-removing and repairing composition as described in claim 1, characterized in that, The total mass percentage of vitamin K2 and cerium oxide microspheres in the acne-removing and repairing composition is 2-10%. And / or, in the acne-repairing composition, the mass percentage of Swertia japonica extract is 10-20%; And / or, in the acne-repairing composition, the mass percentage of mulberry root extract is 40-60%.
4. The acne-removing and repairing composition as described in claim 1, characterized in that, In step (2), The volume fraction of the ethanol solution is 70-90%; the ultrasonic extraction temperature is 30-40℃, the ultrasonic extraction time is 0.5-1h, and the ultrasonic extraction power is 200-250W; the drying temperature is 60-70℃.
5. The acne-removing and repairing composition as described in claim 1, characterized in that, In step (b), The volume fraction of the methanol solution is 70-90%; the flash extraction temperature is 25-30℃, the flash extraction time is 50-80s, the flash extraction voltage is 150-250V, and the flash extraction speed is 4000-5500r / min; the drying temperature is 40-50℃.
6. The use of the acne-repairing composition as described in any one of claims 1-5 in the preparation of facial skin care products.
Citation Information
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