Acne removal composition with effects of removing acne pits and acne marks as well as application and cosmetics of acne removal composition
By using acne removal compositions of phytonol, small molecule peptides and lactonic acid, the problem of difficulty in removing acne pits and acne marks in the prior art is solved, effective antibacterial and skin repair effects are achieved, and skin elasticity and firmness are improved.
Patent Information
- Application Number
- CN202510087720.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-01-20
- Publication Date
- 2025-05-09
AI Technical Summary
The prior art is difficult to effectively remove acne pits and acne marks, and acne removal products usually cannot simultaneously inhibit bacterial growth and promote skin repair.
A composition for acne removal, including hyphenol, small molecule peptides and lactonic acid, is used, which synergistically act to remove acne pits and acne scars and promote skin repair by inhibiting bacterial growth, inhibiting the activity of tyrosinase and elastase.
This composition not only has good antibacterial effects, but also can effectively remove acne pits and acne marks, promote skin repair, and enhance skin elasticity and firmness.
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Figure CN119950327A_ABST
Abstract
Description
Technical Field
[0001] The invention relates to the technical field of daily chemical product production, and in particular to an acne-removing composition having the effects of removing acne pits and acne marks, an application thereof, and cosmetics. Background Art
[0002] Acne, a seemingly minor skin problem, can cause people far more trouble than they imagine. It not only affects the appearance, but also has important impacts on the individual's physiological, psychological and social aspects. The importance of acne treatment is worth our in-depth discussion.
[0003] From a physiological health perspective, the appearance of acne often means that the health of the skin is in danger. Acne, medically known as acne, is mainly caused by a combination of factors such as vigorous secretion of sebaceous glands, blockage of the hair follicle sebaceous gland ducts, bacterial infection and inflammatory response. If effective acne treatment is not carried out in time, acne may become more serious. Mild acne may only be acne and papules, while severe acne may develop into pustules, nodules and even cysts. These severe acne will not only destroy the integrity of the skin, but also easily cause infection, which may cause permanent damage to the skin, such as acne pits and acne marks.
[0004] Acne scars may last for a long time, making the skin look dull and uneven, giving people an unhealthy feeling. Moreover, if the inflammation caused by acne spreads to the surrounding tissues, it may cause more serious skin diseases and pose a potential threat to physical health.
[0005] The importance of acne treatment is self-evident. It is not only related to the health of the skin, but also affects a person's mental health and social life.
[0006] Chinese patent application 202410903738.2 discloses an acne-clearing and soothing acne patch and its preparation method and application. The acne-clearing and soothing acne patch of this scheme includes the following components in percentage by mass: 0.001-8% of acne-clearing and soothing composition, 0.1-35% of viscosity enhancer, 0.1-5% of plasticizer, 0.1-45% of liquid absorbent, and the balance is elastomer. The acne-clearing and soothing acne patch of this scheme selects lactobionic acid, royal acid, totarol, guaiazulene and Centella asiatica extract as acne-clearing and soothing effective ingredients. The above components improve the anti-acne performance and stability of the acne-clearing and soothing acne patch through synergistic effects; and this scheme uses sodium polyacrylate as a liquid absorbent, which improves the liquid absorption capacity of the acne-clearing and soothing acne patch, and improves the problem of traditional acne patches being prone to water loss, charring, yellowing and blackening due to improper selection of liquid absorbents.
[0007] Further observation of paragraph 10 of the instructions of the scheme shows that the role of lactobionic acid in the scheme is to accelerate the shedding of stratum corneum cells and relieve the blockage of hair follicles. It can dissolve and open the keratinous tissue layer on the surface of acne, increase the ductility of the skin, and allow the acne-removing ingredients of the acne patch to penetrate and directly play a role. Thus, the absorbent can absorb the pus secreted by acne and reduce the inflammation and redness of the skin.
[0008] The effects of totarol are: totarol has a bactericidal effect, has a good inhibitory effect on Gram-negative and Gram-positive bacteria, can inhibit the growth and further deterioration of acne, and effectively inhibit the breeding of pathogens.
[0009] And from observing the testing method of this solution, we can know that Example 1 has a good acne-clearing ability, but further observing the acne-clearing testing method of this solution shows that it mainly tests the redness and swelling of the skin, that is, this solution can effectively reduce the redness and swelling of acne, but it should be noted that for users, the removal of acne pits and acne marks is equally important.
[0010] The problem to be solved in this scheme is: how to develop an acne-removing composition capable of removing acne pits and acne scars. Summary of the invention
[0011] The purpose of the present application is to provide an acne-removing composition capable of removing acne pits and acne scars. The composition, through the mutual cooperation between lactobionic acid, small molecule peptides and totarol, has good antibacterial ability and also has good collagenase and tyrosinase inhibition ability, thereby achieving the repair and removal of acne pits and acne scars.
[0012] To achieve the above object, the present application discloses an acne-removing composition, which comprises the following components by weight:
[0013] Totarol 0.1-2 parts;
[0014] Small molecule peptide 0.1-1 part;
[0015] 15-30 parts of lactobionic acid;
[0016] The small molecule peptide is selected from at least one of palmitoyl pentapeptide-4, acetyl hexapeptide-8, acetyl octapeptide-3, acetyl heptapeptide-4, and palmitoyl tripeptide-5.
[0017] In the above composition, totarol has strong lipophilicity and can be integrated into the bacterial cell membrane, destroying the membrane structure to cause dysfunction and leakage of intracellular substances. It can also interfere with multiple metabolic pathways of bacteria and hinder their growth and reproduction. In addition, totarol can inhibit the activity of elastase. Elastase decomposes elastin in the skin, causing skin sagging. Totarol inhibits the enzyme, reduces the decomposition of elastin, maintains the content of elastin in the skin, and thus enhances skin elasticity;
[0018] Small molecule peptides are short-chain peptides composed of 2 to 10 amino acids connected by peptide bonds. With this unique structure, they have a high inhibition rate on tyrosinase. It can accurately bind to the active site of tyrosinase, change its spatial conformation, significantly reduce enzyme activity, and effectively reduce the conversion of tyrosine to DOPA, thereby inhibiting melanin production and gradually whitening the skin. In addition, small molecule peptides can inhibit the activity of elastase. With age, the activity of elastase increases, accelerating the decomposition of elastin and causing skin sagging. Small molecule peptides maintain skin elasticity by increasing the inhibition rate of elastase and reducing the decomposition of elastin;
[0019] Lactobionic acid can inhibit the activity of tyrosinase, reduce its catalytic effect on tyrosine by reducing the inhibition rate of tyrosinase, and thus inhibit the formation of melanin. Tyrosine is gradually converted into melanin under the action of tyrosinase. Lactobionic acid interferes with this process, reducing the production of pigments from the source, and can brighten the skin after use. Lactobionic acid can also increase the inhibition rate of elastase, slow down the degradation rate of elastin, maintain the elastin content in the skin, and maintain the elasticity and firmness of the skin.
[0020] Totarol, small molecule peptides and lactobionic acid work synergistically in improving acne scars. They work together to inhibit bacteria, reduce inflammation caused by bacteria, and reduce the risk of aggravation of acne scars; inhibit tyrosinase, reduce melanin production and deposition, and improve acne scars; inhibit elastase, promote elastin synthesis, accelerate acne scar repair, and help restore skin to smoothness.
[0021] Preferably, the following components are included by weight:
[0022] Totarol 0.1-2 parts;
[0023] Small molecule peptide 0.1-0.2 parts;
[0024] 15-30 parts of lactobionic acid.
[0025] Preferably, the small molecule peptide contains at least palmitoyl pentapeptide-4.
[0026] Preferably, it further comprises a solvent, wherein the solvent is selected from at least one of butylene glycol, hexylene glycol, phenoxyethanol, PEG-40 hydrogenated castor oil and water;
[0027] The mass fraction of the solvent in the anti-acne composition is 60 to 95 parts.
[0028] In addition, the present application also discloses the use of the above-mentioned acne-removing composition in preparing cosmetics.
[0029] In addition, the present application also discloses a cosmetic comprising 15 to 35 wt % of the above composition.
[0030] Preferably, the cosmetic is a patch, ointment, liquid, spray, gel, emulsion or cream.
[0031] Preferably, the cosmetic is a gel, an essence, a toner, a facial mask, a cleanser, a lotion, a perfume, a makeup remover, a lipstick, a blush or a spray.
[0032] The beneficial effects of this application are:
[0033] In the anti-acne composition of the present application, totarol has strong lipophilicity and can be integrated into the bacterial cell membrane, destroying the membrane structure to cause functional disorders and leakage of intracellular substances. It can also interfere with multiple metabolic pathways of bacteria and hinder their growth and reproduction. In addition, totarol can inhibit the activity of elastase. Elastase decomposes elastin in the skin, causing skin sagging. Totarol inhibits the enzyme, reduces the decomposition of elastin, maintains the content of elastin in the skin, and thus enhances skin elasticity;
[0034] Small molecule peptides are short-chain peptides composed of 2 to 10 amino acids connected by peptide bonds. With this unique structure, they have a high inhibition rate on tyrosinase. It can accurately bind to the active site of tyrosinase, change its spatial conformation, significantly reduce enzyme activity, and effectively reduce the conversion of tyrosine to DOPA, thereby inhibiting melanin production and gradually whitening the skin. In addition, small molecule peptides can inhibit the activity of elastase. With age, the activity of elastase increases, accelerating the decomposition of elastin and causing skin sagging. Small molecule peptides maintain skin elasticity by increasing the inhibition rate of elastase and reducing the decomposition of elastin;
[0035] Lactobionic acid can inhibit the activity of tyrosinase, reduce its catalytic effect on tyrosine by reducing the inhibition rate of tyrosinase, and thus inhibit the formation of melanin. Tyrosine is gradually converted into melanin under the action of tyrosinase. Lactobionic acid interferes with this process, reducing the production of pigments from the source, and can brighten the skin after use. Lactobionic acid can also increase the inhibition rate of elastase, slow down the degradation rate of elastin, maintain the elastin content in the skin, and maintain the elasticity and firmness of the skin.
[0036] Totarol, small molecule peptides and lactobionic acid work synergistically in improving acne scars. They work together to inhibit bacteria, reduce inflammation caused by bacteria, and reduce the risk of aggravation of acne scars; inhibit tyrosinase, reduce melanin production and deposition, and improve acne scars; inhibit elastase, promote elastin synthesis, accelerate acne scar repair, and help restore skin to smoothness. BRIEF DESCRIPTION OF THE DRAWINGS
[0037] Figure 1 This is a photo of the tail of a fish embryo in the model control group;
[0038] Figure 2This is a photograph of the tail of a fish embryo in the positive control group;
[0039] Figure 3 This is a photo of the tail of fish embryos in the test substance group;
[0040] Figure 4 The facial image of the subject on Day 0 who used the essence prepared from the composition of Example 1;
[0041] Figure 5 The facial image of the subject on the 14th day who used the essence prepared from the composition of Example 1;
[0042] Figure 6 The facial image of the subject on Day 0 who used the essence prepared from the composition of Example 2;
[0043] Figure 7 This is a facial image of the test subject on the 14th day who used the essence prepared from the composition of Example 2. DETAILED DESCRIPTION
[0044] The present invention will be described clearly and completely below in conjunction with the embodiments of the present invention. In the description of the present invention, it should be noted that, if no specific conditions are specified in the embodiments, the conditions are carried out according to conventional conditions or conditions recommended by the manufacturer. If the manufacturer of the reagents or instruments used is not specified, they are all conventional products that can be purchased commercially.
[0045] Before presenting the examples, the extraction process of the plant extracts used in the examples and the raw materials involved in each example are first explained as follows:
[0046] Totarol was purchased from Shaanxi Huatai Biological Fine Chemical Co., Ltd., with an effective substance content of 100%, and the product number is Totarol;
[0047] Palmitoyl pentapeptide-4 was purchased from Shenzhen Readlin Biotechnology Co., Ltd., with an active substance content of 100%, and the product number is palmitoyl pentapeptide-4;
[0048] Acetyl hexapeptide-8 was purchased from Shenzhen Readlin Biotechnology Co., Ltd., with an active substance content of 100%, and the product number is acetyl hexapeptide-8;
[0049] Palmitoyl tripeptide-5 was purchased from Shenzhen Readline Biotechnology Co., Ltd., with an active substance content of 100%, and the product number is palmitoyl tripeptide-5;
[0050] Lactobionic acid was purchased from Shanghai Xuntian Biotechnology Co., Ltd., with an effective substance content of 98%, and the product number is lactobionic acid;
[0051] Preparation method of anti-acne composition:
[0052] Step 1: Heat 20 parts of butanediol, 0.5 parts of hexanediol, and 0.5 parts of cinnamic acid to 60° C., stir and dissolve to obtain a material;
[0053] Step 2: Then cool the material to 35°C, add the small molecule peptide and stir to dissolve, then add 45 parts of water and lactobionic acid, stir to dissolve completely, finally add the pre-dissolved phase of tocopherol and 5 parts of PEG-40 hydrogenated castor oil, stir evenly to obtain a composition.
[0054] (It should be noted that, unless otherwise specified, the preparation methods of the compositions in the remaining embodiments and comparative examples are all this method, and the butanediol, hexanediol, cinnamaldehyde, PEG-40 hydrogenated castor oil, and water in the above preparation method do not play any practical role in actual use. The role of the above substances is only to dissolve small molecule peptides, lactobionic acid, and tocopherol; that is, the above substances essentially only play the role of solvents.)
[0055] Examples 1-7
[0056] An acne-removing composition, the formula of which is shown in Table 1:
[0057] Table 1
[0058]
[0059]
[0060] Example 8
[0061] The method is substantially the same as Example 1, except that acetyl hexapeptide-8 is used to replace palmitoyl pentapeptide-4.
[0062] Example 9
[0063] The method is substantially the same as Example 1, except that palmitoyl tripeptide-5 is used to replace palmitoyl pentapeptide-4.
[0064] Example 10
[0065] The method is basically the same as Example 1, except that a mixture of palmitoyl tripeptide-5 and acetyl hexapeptide-8 is used to replace palmitoyl pentapeptide-4, and the mass ratio of palmitoyl tripeptide-5 to acetyl hexapeptide-8 is 1:1.
[0066] Embodiment 11
[0067] The method is basically the same as Example 1, except that a mixture of palmitoyl pentapeptide-4 and acetyl hexapeptide-8 is used to replace palmitoyl pentapeptide-4, and the mass ratio of palmitoyl pentapeptide-4 to acetyl hexapeptide-8 is 1:1.
[0068] Comparative Examples 1-6
[0069] A composition, the formula is shown in Table 2:
[0070] Table 2
[0071]
[0072] Comparative Examples 7-16
[0073] A composition, the formula is shown in Table 3:
[0074] Table 3
[0075]
[0076]
[0077] It should be noted that the comparative mixture in the above comparative example is a mixture of lysine, threonine and serine, and the molar ratio of lysine, threonine and serine is 2:2:1.
[0078] Performance Testing
[0079] 1. Propionibacterium acnes (ATCC6919) inhibition zone test
[0080] ATCC6919 Propionibacterium acnes was activated at 36°C to prepare 10 8 CFU / mL of bacterial suspension, take 200μL of bacterial suspension, add it to brain heart infusion agar plate and evenly spread it, and dry it naturally. Soak the test sample (the composition prepared in Example 1 is diluted to a mass fraction of 15% with pure water) in a circular filter paper with a diameter of 6mm used in the test. Take out the filter paper after 5 minutes, remove the excess sample, and place it on a clean plate to dry for 30 minutes. Place the sample soaked filter paper on the surface of the plate, turn it upside down and put it into an anaerobic tank, and culture it anaerobically at 37°C for 48 hours. Three sample filter papers of the same sample and one negative control filter paper are placed on each plate. The centers of the samples are more than 25mm apart. The average diameter of the antibacterial ring of the filter paper of the three samples is the antibacterial ring diameter of the sample. The experiment was repeated three times.
[0081] Table 4
[0082]
[0083] After testing, the remaining embodiments and comparative examples all have antibacterial effects.
[0084] 2Zebrafish embryo neutrophil test method
[0085] Pick healthy 3-day-post-fertilization (DPF) zebrafish embryos.
[0086] 2.1 Test Grouping
[0087] The test set up a blank control group (fish embryo culture medium), a model control group (copper sulfate working solution), a positive control group (copper sulfate working solution + indomethacin working solution) and a test substance group (copper sulfate working solution + test substance). If a co-solvent is used, the solubility of the co-solvent in each group should be the same.
[0088] Blank control group setting
[0089] Randomly select 24 fish embryos and place them in a 3 cm culture dish, and add 5 mL of fish embryo culture medium.
[0090] Model control group setting
[0091] Randomly select 24 fish embryos and place them in a 3 cm culture dish, and add 5 mL of fish embryo culture medium containing 0.16 mg / L anhydrous copper sulfate.
[0092] Positive control group setting
[0093] Randomly select 24 fish embryos and place them in a 3 cm culture dish, and add 5 mL of fish embryo culture medium containing 0.16 mg / L anhydrous copper sulfate and 0.0036 mg / L indomethacin.
[0094] Test substance treatment group setting
[0095] 24 fish embryos were randomly selected and placed in a 3 cm culture dish, and 5 mL of fish embryo culture medium containing 0.16 mg / L anhydrous copper sulfate and the test substance (the composition prepared in Example 1) was added, wherein the mass fraction of the test substance in the fish embryo culture medium was 5%.
[0096] 2.2 Fish embryo fixation and staining
[0097] After the fish embryos of each test group were fixed in paraformaldehyde for at least 1 h, the fish embryos were treated with PBST 3 times, each time for 5 min, and then treated with 50% ethanol for 3 min.
[0098] After the fish embryos were stained with Sudan black staining solution at room temperature for 1 hour, they were washed with 70% ethanol 4 times, 5 minutes each time, and then treated with PBST 2 times, 5 minutes each time.
[0099] Treat the fish embryos with bleach solution for 10 minutes. If treated in a test tube, keep the lid open. Then treat with 70% ethanol solution for 5 minutes, PBST for 1 minute, clear solution 1 for 15 minutes, clear solution 2 for 10 minutes, and PBST for 3 minutes.
[0100] 2.3 Microscopic analysis of samples
[0101] Place the fish embryo sideways and then place it under a stereo microscope to take a picture of the fish embryo's tail.
[0102] 2.4 Data and result calculation
[0103] Count the number of neutrophils in the lateral line region of the tail three quarters of the way from the anus of each fish embryo. Calculate the neutrophil aggregation inhibition rate:
[0104]
[0105] (1) Where:
[0106] S is the average number of neutrophils in fish embryos in the test substance treatment group, with the unit of neutrophils per tail (granules / tail);
[0107] M is the average number of neutrophils in fish embryos of the model control group, with the unit of granules per tail (granules / tail);
[0108] B is the average number of neutrophils in fish embryos of the blank control group, with the unit being granules per tail (granules / tail);
[0109] The data were analyzed by variance analysis using statistical software, and the number of neutrophils between the test group and the model control group was tested by two-tailed T test to obtain the P value. p<0.05 indicated a significant difference.
[0110] refer to Figure 1-3 , Figure 1 This is a photograph of the tail of a fish embryo in the model control group, where a large number of stained neutrophils can be seen in the lateral line region;
[0111] Further observation Figure 2 It can be seen that in the photos of the tail of the fish embryos in the positive control group, the number of neutrophils in the lateral line region showed a clear downward trend, which produced a certain soothing effect;
[0112] Further observation of Table 3 shows that the test group Figure 1 , Figure 2 The number of neutrophils in the lateral line area further decreased, indicating that it has a more excellent soothing ability;
[0113] At the same time, according to the calculation results, the neutrophil aggregation inhibition rate was 0% in the model control group, 30% in the positive control group, and 88% in the test substance group.
[0114] 3. Elastase inhibition test
[0115] 20 μL of sample (the composition prepared in Example 1-11 and Comparative Example 1-16 was diluted to a mass fraction of 20% with pure water) was mixed with 100 μL of elastase (100 mU / mL) in a well of a 96-well plate, incubated at 37°C for 20 min, 80 μL of Nsuccinyl-Ala-Ala-Ala-pNA (2 mmol / L) was added, and incubated at 37°C for 20 min. All substances were dissolved in 50 mM Tris-HCl buffer at pH 8.0. Each sample was analyzed in triplicate. The absorbance of the reaction product was recorded at 410 nm. Tris-HCl buffer was used as a blank control. The elastase inhibition rate was calculated as follows:
[0116]
[0117] In formula 1, A1 is the absorbance of the control group before the reaction, A2 is the absorbance of the control group after the reaction, B1 is the absorbance of the sample group before the reaction, and B2 is the absorbance of the sample group after the reaction;
[0118] The specific test results are shown in Table 5:
[0119] Table 5:
[0120]
[0121]
[0122] Result analysis:
[0123] 1. It can be seen from Examples 1-7 that when the amount of totarol, palmitoyl pentapeptide-4, and lactobionic acid added in the formula is slightly adjusted, the fluctuation range between Examples 1-3 and Examples 6-7 is relatively small. Further observation of Examples 4-5 shows that the elastase inhibition rate of the two has a certain degree of downward trend relative to Examples 6-7. It can be seen that when the proportion of palmitoyl pentapeptide-4 in the composition is too large, the elastase inhibition rate of the composition decreases, and the change in the elastase inhibition rate means that the ability of the composition to smooth acne pits has changed, and the relationship between the two is positively correlated. The reason is that when the elastase inhibition rate is high, the body's elastin production and elastin level are relatively excellent, which leads to the acne pits being smoothed more quickly;
[0124] 2. Further observation of Examples 8-9 shows that when other small molecule peptides are used to replace palmitoyl pentapeptide-4, the elastase inhibition rate of Examples 8-9 is lower than that of Example 1. It can be seen that the combination of palmitoyl pentapeptide-4 with totarol and lactobionic acid in this case is more advantageous for smoothing acne scars;
[0125] At the same time, further observation of Examples 10-11 shows that when acetyl hexapeptide-8 and palmitoyl tripeptide-5 are used in combination, the elastase inhibition rate of Example 10 is between that of Examples 8-9;
[0126] When acetyl hexapeptide-8 and palmitoyl pentapeptide-4 were used together, the elastase inhibition rate of Example 11 exceeded that of any of Examples 1 and 8. It can be seen that when the small molecule peptide contains palmitoyl pentapeptide-4, adding other types of small molecule peptides into this solution can further produce a synergistic effect between the composite small molecule peptides, thereby further improving the elastase inhibition ability of the composition.
[0127] 3. It can be seen from Example 1 and Comparative Examples 1-6 that when any one of totarol, palmitoyl pentapeptide-4 and lactobionic acid is missing in Comparative Examples 1-3, the elastase inhibition ability of Comparative Examples 1-3 has a more obvious downward trend relative to Example 1. It can be seen that in this solution, totarol, palmitoyl pentapeptide-4 and lactobionic acid are indispensable for removing acne pits. At the same time, when only totarol, palmitoyl pentapeptide-4 and lactobionic acid are added to Comparative Examples 4-6, the elastase inhibition ability thereof is further reduced relative to Comparative Examples 1-3;
[0128] 4. It can be seen from Comparative Examples 7-10 that when palmitoyl pentapeptide-4 is replaced with the basic components of palmitoyl pentapeptide-4 such as lysine, threonine or serine, the elastase inhibition rate of Comparative Examples 7-10 is significantly reduced relative to Example 1. It can be seen that the replacement of a single amino acid for a small molecule peptide is difficult for the composition to maintain a good acne pit removal ability. Further, when Comparative Example 11 uses an amino acid mixture with a molar ratio of lysine, threonine and serine of 2:2:1 to replace palmitoyl pentapeptide-4, Comparative Example 11 still finds it difficult to achieve an elastase inhibition level similar to that of Example 1. It can be seen that the good elastase inhibition ability of palmitoyl pentapeptide-4 is not only due to the amino acids it contains, but also the connection structure between its multiple amino acids also plays a key role.
[0129] 5. It can be seen from Example 1, Comparative Example 3, Comparative Example 5, Comparative Example 11, Comparative Example 13, and Comparative Example 15 that palmitoyl pentapeptide-4 and cono peptide have very similar inhibitory abilities for elastase. Further observation of Comparative Example 3 and Comparative Example 15 shows that when the two are used in combination with totarol, the inhibition rates of elastase obtained in Comparative Example 3 and Comparative Example 15 are close to the sum of the inhibition rates of elastase of totarol and the two. It can be seen that when the two are mixed with totarol, they cannot produce a synergistic effect, but further observation of Comparative Example 3 and Comparative Example 15 shows that when the two are used in combination with totarol, the inhibition rates of elastase obtained in Comparative Example 3 and Comparative Example 15 are close to the sum of the inhibition rates of elastase of totarol and the two. By further observing Example 1 and Comparative Example 11, it can be seen that when lactobionic acid is added to the components, the elastin inhibition rate of Comparative Example 11 is almost equal to the sum of the elastin inhibition rates of totarol, lactobionic acid, and conopeptide, while the elastin inhibition rate obtained in Example 1 exceeds the sum of the elastin inhibition rates of totarol, lactobionic acid, and palmitoyl pentapeptide-4. It can be seen that on the one hand, totarol, lactobionic acid, and palmitoyl pentapeptide-4 produce a synergistic effect, and after using a substance similar to palmitoyl pentapeptide-4 to replace them, this synergistic effect is significantly weakened or even non-existent;
[0130] On the other hand, totarol and palmitoyl pentapeptide-4 cannot produce synergistic effects when used together. Only when lactobionic acid is added can the three achieve good elastase inhibition ability.
[0131] Similarly, it can be seen from comparative examples 5 and 14 that the elastase inhibition ability of palmitoyl pentapeptide-4 and retinol / saccharomyces polypeptide is close. Further observation of comparative examples 1 and 16 shows that when the two are used together with lactobionic acid, no synergistic effect is produced; however, it can be seen from example 1 and 12 that the elastin inhibition rate of comparative example 12 is almost equal to the sum of the elastin inhibition rates of totarol, lactobionic acid, and retinol / saccharomyces polypeptide, while the elastin inhibition rate obtained in example 1 exceeds the sum of the elastin inhibition rates of totarol, lactobionic acid, and palmitoyl pentapeptide-4. It can be seen that totarol, lactobionic acid, and palmitoyl pentapeptide-4 produce a synergistic effect, and after using a similar substance to palmitoyl pentapeptide-4 to replace it, this synergistic effect is significantly weakened or even non-existent;
[0132] On the other hand, lactobionic acid and palmitoyl pentapeptide-4 cannot produce a synergistic effect when used together. Only when totarol is added can the three achieve good elastase inhibition ability.
[0133] 4.Tyrosinase inhibition test
[0134] 4.1 Instruments and Equipment
[0135] BSA224S Analytical Balance
[0136] RT-6100 ELISA Analyzer
[0137] 4.2 Reagents
[0138] Polyphenol oxidase (mushroom), BR
[0139] Levodopa, BR
[0140] 4.3 Test methods
[0141] (1) Treatment of control and test samples
[0142] Sample: Dilute with pure water until the mass fraction of the composition prepared in Examples 1-11 and Comparative Examples (1-10, 13, 15) is 20%;
[0143] Blank control: pure water.
[0144] (2) Test operation steps
[0145] Set up sample tubes, sample background tubes, enzyme reaction tubes, and solvent background tubes. Set up 3 parallel tubes for each group. Add different reagent solutions to the four groups, shake gently, and let stand at room temperature for 5 minutes. Transfer each group of reaction solutions into a 1 cm cuvette and measure the absorbance at 475 nm.
[0146] 4.4 Calculation formula
[0147] As shown in formula 2:
[0148]
[0149] In formula 2, T is the absorbance of the sample tube, i.e., the absorbance of the solution after the sample reacts with tyrosinase;
[0150] T0 is the background absorbance of the sample;
[0151] C is the average of three absorbance values of the enzyme reaction tube, that is, the absorbance value of the tyrosinase and DOPA reaction when no sample is added;
[0152] C0 is the background absorbance of the solvent.
[0153] 4.5 Data Analysis
[0154] The statistical analysis software was SPSS. P>0.05 indicated that there was no significant difference between the two groups; P<0.05 indicated that there was a significant difference between the two groups. The test results are shown in Table 6:
[0155] Table 6
[0156]
[0157]
[0158] Result analysis:
[0159] 1. It can be seen from Examples 1-7 that when the amount of totarol, palmitoyl pentapeptide-4, and lactobionic acid added in the formula is slightly adjusted, the fluctuation range of the tyrosinase inhibition rate between Examples 1-3 and Examples 6-7 is relatively small. Further observation of Examples 4-5 shows that the tyrosinase inhibition rates of the two have a certain degree of downward trend relative to Examples 6-7. It can be seen that when the proportion of palmitoyl pentapeptide-4 in the composition is too large, the tyrosinase inhibition rate of the composition decreases, and the change in the tyrosinase inhibition rate means that the ability of the composition to eliminate acne marks has changed, and the relationship between the two is positively correlated. The reason is that when the tyrosinase inhibition rate is high, the body's melanin production and melanin level are relatively low, which leads to the acne marks being eliminated more quickly;
[0160] 2. It can be seen from Examples 1 and 8-9 that when other small molecule peptides are used to replace palmitoyl pentapeptide-4, the tyrosinase inhibition rate of Examples 8-9 is lower than that of Example 1. It can be seen that the combination of palmitoyl pentapeptide-4 with totarol and lactobionic acid in this case is more advantageous for eliminating acne scars;
[0161] At the same time, further observation of Examples 10-11 shows that when acetyl hexapeptide-8 and palmitoyl tripeptide-5 are used in combination, the tyrosinase inhibition rate of Example 10 is between that of Examples 8-9;
[0162] When acetyl hexapeptide-8 and palmitoyl pentapeptide-4 were used together, the tyrosinase inhibition rate of Example 11 exceeded that of either Example 1 or Example 8. It can be seen that when the small molecule peptide contains palmitoyl pentapeptide-4, adding other types of small molecule peptides into this solution can further produce a synergistic effect between the composite small molecule peptides, thereby further improving the tyrosinase inhibition ability of the composition.
[0163] 3. It can be seen from Comparative Examples 1-6 that only when tortol and palmitoyl pentapeptide-4 are present at the same time, Comparative Example 3 can achieve good tyrosinase inhibition ability, and tortol and palmitoyl pentapeptide-4 produce a synergistic effect, and when tortol or palmitoyl pentapeptide-4 are mixed with lactobionic acid, Comparative Examples 1-2 do not produce a synergistic effect. It can be seen that the key to making the composition have good tyrosinase inhibition ability lies in the coordination between tortol and palmitoyl pentapeptide-4. Further observation of Comparative Examples 13 and 15 shows that the tyrosinase inhibition ability of conopeptide and palmitoyl pentapeptide-4 is close, but when Comparative Example 15 uses conopeptide and tortol together, the tyrosinase inhibition ability of the two is almost equivalent to the simple superposition of the tyrosinase inhibition rate when the two are used separately. It can be seen that not all substances similar to palmitoyl pentapeptide-4 can produce a good synergistic effect with tortol on tyrosinase inhibition ability.
[0164] 5. Photo test
[0165] 5.1 Test Purpose
[0166] The clinical efficacy of the essence is studied through clinical tests, and the changes in various skin indicators before and after application are studied to verify its effects in removing acne, scars and acne marks.
[0167] 5.2 Test samples
[0168] The samples were prepared according to the formula shown in Table 7:
[0169] Table 7
[0170]
[0171]
[0172] 5.3 Subject selection
[0173] Twenty subjects aged between 20 and 30 years old (excluding pregnant or lactating women) were selected and divided into two groups, with 10 subjects in each group to test the essence prepared by the composition prepared in Example 1 and the essence prepared by the composition prepared in Example 2 respectively; the subjects had no serious systemic diseases, no immunodeficiency or autoimmune diseases; the tested parts had not received skin treatment, beauty treatment and other tests that may affect the results; no active allergic diseases; no highly sensitive constitution; no hormone drugs and immunosuppressants in the past month; the tested parts had not participated in other clinical trials in the past month;
[0174] 5.4 Test Instruments
[0175] Facial Image Analysis VISIA
[0176] 5.5 Usage
[0177] The subjects applied the samples to the test areas once a day for 2 weeks and performed skin tests on the 0th and 14th days respectively.
[0178] 5.5 Test steps:
[0179] After cleaning their faces, the subjects sat in a laboratory at 21±1℃ and 50±10%RH for 30 minutes, and then took facial images with a VISIA skin image analyzer to observe the differences in their facial analysis before and after application;
[0180] observe Figure 4-7 It can be seen that the essences finally prepared from the compositions prepared in Example 1 and Example 2 have good ability to remove acne pits and acne marks.
Claims
1. An acne-removing composition having the effect of removing acne pits and acne scars, characterized in that: By mass, it includes the following components: Totarol 0.1-2 parts; Small molecule peptide 0.1-1 part; 15-30 parts of lactobionic acid; The small molecule peptide is selected from at least one of palmitoyl pentapeptide-4, acetyl hexapeptide-8, acetyl octapeptide-3, acetyl heptapeptide-4, and palmitoyl tripeptide-5.
2. The acne-removing composition having the effect of removing acne pits and acne scars according to claim 1, characterized in that: By mass, it includes the following components: Totarol 0.1-2 parts; Small molecule peptide 0.1-0.2 parts; 15-30 parts of lactobionic acid.
3. The acne-removing composition having the efficacy of removing acne pits and acne scars according to claim 1, characterized in that: The small molecule peptide at least contains palmitoyl pentapeptide-4.
4. The acne-removing composition having the efficacy of removing acne pits and acne scars according to claim 1, characterized in that: Also includes a solvent, the solvent is selected from at least one of butylene glycol, hexylene glycol, chloranol, PEG-40 hydrogenated castor oil, and water; The mass fraction of the solvent in the anti-acne composition is 60 to 95 parts.
5. Use of the anti-acne composition according to any one of claims 1 to 4 for preparing cosmetics having the efficacy of removing acne pits and acne marks.
6. A cosmetic, characterized in that: The acne removing composition having the effect of removing acne pits and acne marks contains 1 to 35 wt % of any one of claims 1 to 4.
7. The cosmetic according to claim 6, characterized in that: The cosmetic is a patch, ointment, liquid, spray, gel, emulsion or cream.
8. The cosmetic according to claim 6, characterized in that: The cosmetics are gel, essence, toner, facial mask, cleanser, lotion, perfume, make-up remover, lipstick, blush or spray.
Citation Information
Patent Citations
Acne cleaning and relieving patch as well as preparation method and application thereof
CN118845575A