A composition for quickly reducing redness and repairing sensitive skin

Abstract

The present invention relates to a composition for quickly reducing redness and repairing sensitive skin, belonging to the technical field of skin care products. The composition for quickly reducing redness and repairing sensitive skin comprises the following raw materials by mass parts: 20-30 parts of active substance gel, 0.2-0.5 part of collagen, 1-2 parts of glycerol, 0.5-0.7 part of Kochia scoparia, and 50-60 parts of water; the active substances in the active substance gel include 1.5-3 parts of N-acetylneuraminic acid, 1.2-2.5 parts of leonurine derivatives, and 1.2-1.5 parts of Acacia farnesiana extract. The in vitro cytotoxicity test of the composition for quickly reducing redness and repairing sensitive skin prepared by the present invention verifies its safety in vitro; when acting on the skin of patients with sensitive skin, it can significantly reduce swelling and relieve pain, and can achieve the purpose of repairing the skin barrier.

Description

Technical Field

[0001] The present invention belongs to the technical field of skin care products, and particularly relates to a composition for quickly reducing redness and repairing sensitive skin. Background Art

[0002] The skin is the largest organ in the human body. It directly contacts the external environment and has functions such as protection, excretion, body temperature regulation, and perception of external stimuli. With the increasing work pressure and accelerating life rhythm of modern people, a large number of cosmetics are frequently used on the face, and excessive skin cleansing is carried out, resulting in an increasing number of people with sensitive skin. Skin problems related to sensitive skin, such as skin burning, itching, erythema, and damaged skin barrier, have attracted increasing attention. Therefore, people now pay more and more attention to the care and maintenance of sensitive skin, and more and more products for repairing sensitive skin occupy the mainstream market. Summary of the Invention

[0003] The purpose of the present invention is to provide a composition for quickly reducing redness and repairing sensitive skin to solve the technical problems of erythema and damaged skin barrier caused by sensitive skin.

[0004] To achieve the above purpose, the technical solution adopted by the present invention is as follows:

[0005] A composition for quickly reducing redness and repairing sensitive skin, calculated by mass parts, includes the following raw materials: 20 - 30 parts of active substance gel, 0.2 - 0.5 parts of collagen, 1 - 2 parts of glycerol, 0.5 - 0.7 parts of Kochia scoparia, and 50 - 60 parts of water;

[0006] The active substances in the active substance gel, calculated by mass parts, include 1.5 - 3 parts of N-acetylneuraminic acid, 1.2 - 2.5 parts of leonurine derivatives, and 1.2 - 1.5 parts of Albizia lebbeck extract.

[0007] Further, the preparation method of the active substance gel is as follows:

[0008] S1: Mix the formulated amounts of the N-acetylneuraminic acid, leonurine derivatives, Albizia lebbeck extract, penetration enhancer, emulsifier, and co-emulsifier to obtain a mixed phase; add water to the mixed phase under stirring until the solution is clear, and obtain a microemulsion after shear mixing;

[0009] S2: Add a gel matrix to the microemulsion in S1 under stirring to obtain the product.

[0010] Further, the penetration enhancer is a mixture of azone and peppermint oil, and the mass ratio of azone to peppermint oil is 0.5:1.5 - 1:1.5.

[0011] Further, the emulsifier is Tween 80, the co-emulsifier is glycerol, and the gel matrix is chitosan.

[0012] Further, the content of the emulsifier is 40 to 60 parts by mass, and the content of the co-emulsifier is 40 to 50 parts by mass; the content of the gel matrix is 30 to 40 parts by mass, and the content of the penetration enhancer is 25 to 35 parts by mass.

[0013] Further, the structural formula of the leonurine derivative is shown in Formula (1):

[0014] , Formula (1).

[0015] Further, the preparation method of the leonurine derivative is as follows:

[0016] S1: Add leonurine hydrochloride and citric anhydride to dichloromethane, stir evenly at low temperature, then add N,N'-dicyclohexylcarbodiimide and 4-dimethylaminopyridine, and raise the temperature to room temperature for reaction to obtain Substance A;

[0017] S2: Add Substance A, 2-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate, N,N-diisopropylethylamine, and 2-aminoethanesulfonamide to N,N-dimethylformamide in sequence, and react at room temperature to obtain the product.

[0018] Further, the molar ratio of leonurine hydrochloride to citric anhydride is 1:1 to 1:1.2; the molar ratio of leonurine hydrochloride to N,N'-dicyclohexylcarbodiimide is 1:1.2 to 1:1.5; the molar ratio of leonurine hydrochloride to 4-dimethylaminopyridine is 1:1.2 to 1:1.5; the molar ratio of Substance A to 2-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate is 1:1 to 1:1.2; the molar ratio of Substance A to N,N-diisopropylethylamine is 1:3 to 1:3.6; the molar ratio of Substance A to 2-aminoethanesulfonamide is 1:1.2 to 1:1.6.

[0019] Further, the low temperature in S1 is 5 to 10 °C, and the reaction time is 12 to 16 h; the reaction time in S2 is 2 to 3 h.

[0020] Further, the preparation method of the composition is: Mix the formula amounts of the collagen, glycerol, Kochia scoparia, and water, and then add the active substance gel, and mix evenly to obtain the product.

[0021] Advantages of the present invention:

[0022] The in vitro cytotoxicity test of the composition for quickly reducing redness and repairing sensitive skin prepared by the present invention verifies its safety in vitro; when acting on the skin of patients with sensitive skin, it can significantly reduce swelling and relieve pain, and can achieve the purpose of repairing the skin barrier.

[0023] Acacia farnesiana extract can effectively relieve skin inflammation, reduce skin redness, itching and other discomforts, and also has good functions of soothing, moisturizing and improving skin defense. Leonurine derivatives have antibacterial, anti-inflammatory and blood-activating functions. N-acetylneuraminic acid can effectively eliminate reactive oxygen species (ROS) in the body, control the synthesis of glycosphingolipids, control and enhance cell activity and sensitivity, enable the normal physiological activities of cells to proceed normally, and is beneficial to restoring the skin barrier. The compound of N-acetylneuraminic acid, Acacia farnesiana extract and leonurine derivatives of the present invention can effectively improve the anti-inflammatory and antibacterial functions of the skin and promote skin repair.

[0024] The gel has good adhesiveness, and Kochia scoparia can improve the permeability of the skin. The present invention opens the skin permeability through Kochia scoparia, and the gel adheres to the skin, prolonging the residence time of the active substances on the skin, so that the active substances of the present invention can better act on skin cells. Brief Description of the Drawings

[0025] Figure 1 Schematic diagram of the synthesis route of leonurine derivatives in Example 1;

[0026] Figure 2 1H NMR spectrum of Substance A in Example 1;

[0027] Figure 3 1H NMR spectrum of leonurine derivatives in Example 1;

[0028] Figure 4 Effect diagram of using the composition for quickly reducing redness and repairing sensitive skin in Example 1. Detailed Description of the Invention

[0029] The present invention will be further described below in conjunction with the embodiments of the present invention and the accompanying drawings.

[0030] The Acacia farnesiana extract is commercially purchased. Example 1

[0031] The preparation method of the composition for quickly reducing redness and repairing sensitive skin in Example 1 includes the following steps: 0.2 kg of collagen, 1 kg of glycerol, 0.6 kg of Kochia scoparia, and 50 kg of water are mixed, and then 20 kg of active substance gel is added and mixed evenly to obtain the composition.

[0032] The preparation method of the active substance gel is as follows: Mix 1.5 kg of N-acetylneuraminic acid, 1.2 kg of leonurine derivative, 1.2 kg of bark extract of acacia farnesiana, 25 kg of penetration enhancer, 40 kg of Tween 80, and 40 kg of glycerol to obtain a mixed phase. Subsequently, add water to the solution under stirring until it becomes clear, and obtain a microemulsion after shear mixing. Add 30 kg of chitosan to the microemulsion under stirring to obtain the product. The penetration enhancer includes 7.5 kg of azone and 17.5 kg of peppermint oil.

[0033] The preparation method of the leonurine derivative is as follows:

[0034] S1: Add 10 mmol of leonurine hydrochloride and 11 mmol of citric anhydride (CAS: 24555-16-6) to 20 mL of dichloromethane. After stirring evenly at 8 °C, add 13 mmol of N,N'-dicyclohexylcarbodiimide and 13 mmol of 4-dimethylaminopyridine, and raise the temperature to 25 °C for reaction for 14 h. Subsequently, concentrate, purify by reverse-phase high-performance liquid chromatography, and concentrate and freeze-dry the fractions to obtain Substance A; 1 H NMR( C 20 H 27 N3O 11 , 400 MHz, d 6 - DMSO) δ 14.35 (s, 1H), 13.50(s, 1H), 8.72 (s, 1H), 7.82 (s, 1H), 6.95 (s, 2H), 6.62 (s, 1H), 4.32 (t,2H), 3.83 (s, 6H), 3.58 (t, 2H), 2.69(t, 2H), 2.48-2.42 (m, 3H), 2.00 (s,1H), 1.79(q, 2H), 1.51(q, 2H); MS (ESI) m / z = 486.16 [M+H] + 。

[0035] S2: Add 5 mmol of Substance A and 5.5 mmol of 2-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate to 15 mL of N,N-dimethylformamide. After stirring evenly, add 16 mmol of N,N-diisopropylethylamine, stir evenly, and then add 7 mmol of 2-aminoethanesulfonamide, and react at room temperature for 2.5 h. Subsequently, purify by reverse-phase high-performance liquid chromatography, and concentrate and freeze-dry the fractions to obtain the leonurine derivative. 1 H NMR( C 22 H33 N5O 12 S, 400 MHz, d 6 -DMSO) δ 14.35 (s, 1H), 8.72 (s, 1H), 8.01 (s, 1H), 7.82 (s, 1H), 7.12 (s,2H), 6.95 (s, 2H), 6.62 (s, 1H), 4.32 (t, 2H), 3.83 (s, 6H), 3.76-3.58 (m,6H), 2.69(t, 2H), 2.48-2.42 (m, 3H), 2.00 (s, 1H), 1.79(q, 2H), 1.51(q, 2H); MS (ESI) m / z = 592.19[M+H] + 。 Example 2

[0036] The preparation method of the composition for quickly reducing redness and repairing sensitive skin in Example 2 includes the following steps: Mix 0.4 kg of collagen, 2 kg of glycerol, 0.5 kg of Kochia scoparia, and 60 kg of water, and then add 30 kg of active substance gel and mix evenly to obtain it.

[0037] The preparation method of the active substance gel is as follows: Mix 2.5 kg of N-acetylneuraminic acid, 2 kg of leonurine derivative, 1.5 kg of Bauhinia extract, 35 kg of penetration enhancer, 48 kg of Tween 80, and 45 kg of glycerol to obtain a mixed phase. Then add water to the solution under stirring until it is clear, and obtain a microemulsion after shear mixing. Add 40 kg of chitosan to the microemulsion under stirring to obtain it. The penetration enhancer includes 14 kg of azone and 21 kg of peppermint oil.

[0038] The preparation method of the leonurine derivative is as follows:

[0039] S1: Add 10 mmol of leonurine hydrochloride and 12 mmol of citric anhydride to 20 mL of dichloromethane, stir evenly at 5 °C, then add 15 mmol of N,N-dicyclohexylcarbodiimide and 12 mmol of 4-dimethylaminopyridine, and react at 25 °C for 16 h; then concentrate, purify by reverse-phase high-performance liquid chromatography, and concentrate and freeze-dry the fractions to obtain Substance A;

[0040] S2: Add 5 mmol of substance A and 6 mmol of 2-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate to 15 mL of N,N-dimethylformamide. After stirring evenly, add 18 mmol of N,N-diisopropylethylamine and stir evenly. Then add 9 mmol of 2-aminoethanesulfonamide and react at room temperature for 2.5 h. Subsequently, purify by reverse-phase high-performance liquid chromatography, concentrate the fractions, and freeze-dry to obtain the leonurine derivative. Example 3

[0041] The preparation method of the composition for rapidly reducing redness and repairing sensitive skin in Example 3 includes the following steps: Mix 0.5 g of collagen, 1.8 g of glycerol, 0.7 g of Kochia scoparia, and 52 g of water, and then add 28 g of the active substance gel and mix evenly to obtain the product.

[0042] The preparation method of the active substance gel is as follows: Mix 3 g of N-acetylneuraminic acid, 2.5 g of the leonurine derivative, 1.5 g of Bauhinia extract, 28 g of the penetration enhancer, 50 g of Tween 80, and 50 g of glycerol to obtain a mixed phase. Subsequently, add water to the solution under stirring until it is clear, and obtain a microemulsion after shear mixing. Add 38 g of chitosan to the microemulsion under stirring to obtain the product. The penetration enhancer includes 13 g of azone and 15 g of peppermint oil.

[0043] The preparation method of the leonurine derivative in Example 3 is the same as that in Example 1.

[0044] Comparative Example 1

[0045] The preparation method of the composition for rapidly reducing redness and repairing sensitive skin in Comparative Example 1 is substantially the same as that in Example 1. The difference between the preparation method of the composition for rapidly reducing redness and repairing sensitive skin in Comparative Example 1 and that in Example 1 is that in Comparative Example 1, N-acetylneuraminic acid is replaced with an equal mass of the leonurine derivative.

[0046] Comparative Example 2

[0047] The preparation method of the composition for rapidly reducing redness and repairing sensitive skin in Comparative Example 2 is substantially the same as that in Example 1. The difference between the preparation method of the composition for rapidly reducing redness and repairing sensitive skin in Comparative Example 2 and that in Example 1 is that in Comparative Example 2, N-acetylneuraminic acid is replaced with an equal mass of the leonurine derivative, and the Bauhinia extract is replaced with an equal mass of the leonurine derivative.

[0048] Comparative Example 3

[0049] The preparation method of the composition for rapidly reducing redness and repairing sensitive skin in Comparative Example 3 is substantially the same as that in Example 1. The difference between the preparation method of the composition for rapidly reducing redness and repairing sensitive skin in Comparative Example 3 and that in Example 1 is that in Comparative Example 3, the leonurine derivative is replaced with an equal mass of N-acetylneuraminic acid.

[0050] Test Example 1

[0051] According to the filter membrane diffusion test in the in vitro cytotoxicity test GB / T16886.5-2017, the biological responses of the test samples prepared in Example 1 and Comparative Examples 1 to 3 to L-929 mammalian fibroblasts were evaluated. The specific results are shown in Table 1.

[0052] Table 1 Results of cytotoxicity test

[0053]

[0054] Note: When the level is greater than level 2, it is considered to have a cytotoxic effect. The lower the level, the lower the toxicity of the composition.

[0055] As can be seen from Table 1, the cytotoxicity level of the tested test samples is level 0, and the corresponding reaction degree is no cytotoxicity. The in vitro cytotoxicity test result of the composition for rapidly reducing redness and repairing sensitive skin of the present invention is: no cytotoxicity.

[0056] Test Example 2

[0057] Take the compositions of Example 1 and Comparative Examples 1 to 3, and test the TEWL value (trans-epidermal water loss TEWL, which reflects the barrier function of the stratum corneum and can be used to evaluate the repair ability of cosmetics on the skin barrier), the degree of pain reduction, and the degree of redness and swelling subsidence. The specific results are shown in Table 2.

[0058] Female volunteers aged 25 to 35 who met the acne diagnostic criteria were selected and randomly divided into 5 groups, with 10 people in each group. An appropriate amount of the composition was evenly applied to the red and swollen parts, and then gently massaged for 3 to 5 minutes. It was applied twice a day for 7 consecutive days. During the whole process, the diet and daily routine must be regular, and the affected area should not be squeezed or frequently touched.

[0059] The test process of the TEWL value: After cleansing the face with water and sitting still for 30 minutes, the TEWL value was measured using a TM300 trans-epidermal water loss measuring instrument, and the stable average result was taken as the TEWL value.

[0060] Table 2 Test results for curing sensitive skin

[0061]

[0062] Note: The corresponding levels of the degree are: slight - 1, general - 2, relatively obvious - 3, obvious - 4, very obvious - 5.

[0063] As can be seen from Table 2, the composition of the present invention has a good repair effect, can significantly reduce the pain and the degree of swelling and redness in a short time; in addition, it can reduce the TEWL value, effectively relieve the speed of water loss through the epidermis, and then achieve the repair effect on the skin barrier.

[0064] Test Example 3

[0065] A female volunteer aged 27 who met the acne diagnosis criteria was selected. The composition for rapid redness removal and sensitive skin repair in Example 1 was evenly applied to the swollen and red areas, and then gently massaged for 3 - 5 minutes. The facial condition of the patient was observed 30 minutes and 1 hour later. The results are as Figure 4 shown. As can be seen from Figure 4 it, 30 minutes later, the swelling and inflammation on the patient's face improved significantly, and 60 minutes later, the swelling and inflammation on the patient's face basically completely disappeared, indicating that the composition for rapid redness removal and sensitive skin repair of the present invention has good functions of redness removal, anti - inflammation and repair.

[0066] The above - mentioned embodiments are only the preferred embodiments of the present invention and cannot be used to limit the scope of protection of the present invention. Any non - substantial changes and substitutions made by those skilled in the art based on the present invention belong to the scope of protection required by the present invention.

Claims

1. A composition for rapidly fading redness and repairing sensitive skin, characterized in that: The following raw materials are included by mass: 20-30 parts of active substance gel, 0.2-0.5 parts of collagen, 1-2 parts of glycerin, 0.5-0.7 parts of Kochia scoparia seeds and 50-60 parts of water; The active substances in the active substance gel include 1.5 to 3 parts of N-acetylneuraminic acid, 1.2 to 2.5 parts of leonurine derivatives and 1.2 to 1.5 parts of Quillaja sylvestris extract in parts by mass; The structural formula of the leonurine derivative is shown in formula (1):

2. The composition for rapidly fading redness and repairing sensitive skin according to claim 1, characterized in that: The preparation method of the active substance gel is: S1: mixing the N-acetylneuraminic acid, the leonurine derivative and the Quillaja sylvestris extract in the formula amount with a penetration enhancer, an emulsifier and an emulsifier co-emulsifier to obtain a mixed phase; adding water to the mixed phase under stirring until the solution is clear, and obtaining a microemulsion after shear mixing; S2: Add the gel matrix to the microemulsion in S1 under stirring to obtain.

3. The composition for rapidly fading redness and repairing sensitive skin according to claim 2, characterized in that: The penetration enhancer is a mixture of azone and peppermint oil, and the mass ratio of azone to peppermint oil is 0.5:1.5 to 1:1.

5.

4. The composition for rapidly fading redness and repairing sensitive skin according to claim 2, characterized in that: The emulsifier is Tween 80, the auxiliary emulsifier is glycerol, and the gel matrix is ​​chitosan.

5. The composition for rapidly fading redness and repairing sensitive skin according to claim 2, characterized in that: The content of the emulsifier is 40 to 60 parts by weight, the content of the auxiliary emulsifier is 40 to 50 parts by weight; the content of the gel matrix is ​​30 to 40 parts by weight, and the content of the penetration enhancer is 25 to 35 parts by weight.

6. The composition for rapidly fading redness and repairing sensitive skin according to claim 1, characterized in that: The preparation method of the leonurine derivative is: S1: Add leonurine hydrochloride and citric anhydride to dichloromethane, stir evenly at low temperature, then add N,N-dicyclohexylcarbodiimide and 4-dimethylaminopyridine, and heat to room temperature to react to obtain substance A; S2: Add substance A, 2-(7-azabenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate, N,N-diisopropylethylamine and 2-aminoethanesulfonamide to N,N-dimethylformamide in sequence, and react at room temperature to obtain the product.

7. The composition for rapidly fading redness and repairing sensitive skin according to claim 6, characterized in that: The molar ratio of the motherwort hydrochloride and citric anhydride is 1:1 to 1:1.2; the molar ratio of the motherwort hydrochloride and N,N-dicyclohexylcarbodiimide is 1:1.2 to 1:1.5; the molar ratio of the motherwort hydrochloride and 4-dimethylaminopyridine is 1:1.2 to 1:1.5; the molar ratio of the substance A and 2-(7-azabenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate is 1:1 to 1:1.2; the molar ratio of the substance A to the N,N-diisopropylethylamine is 1:3 to 1:3.6; the molar ratio of the substance A to the 2-aminoethanesulfonamide is 1:1.2 to 1:1.

6.

8. The composition for rapidly fading redness and repairing sensitive skin according to claim 6, characterized in that: The low temperature in S1 is 5-10° C., and the reaction time is 12-16 h; the reaction time in S2 is 2-3 h.

9. The composition for rapidly fading redness and repairing sensitive skin according to claim 1, characterized in that: The preparation method of the composition is as follows: after mixing the collagen, glycerin, Kochia scoparia seeds and water in the formula amount, adding the active substance gel, and mixing evenly to obtain the composition.

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