Composition for rapidly fading red and repairing sensitive skin

Abstract

The invention relates to a composition for rapidly fading red and repairing sensitive skin, and belongs to the technical field of skin care products. The composition for rapidly fading red and repairing sensitive skin is prepared from the following raw materials in parts by mass: 20 to 30 parts of active substance gel, 0.2 to 0.5 part of collagen, 1 to 2 parts of glycerol, 0.5 to 0.7 part of fructus kochiae and 50 to 60 parts of water, the active substance gel is prepared from the following active substances in parts by weight: 1.5 to 3 parts of N-acetylneuraminic acid, 1.2 to 2.5 parts of leonurine derivative and 1.2 to 1.5 parts of schefflera octophylla extract. The in-vitro cytotoxicity test of the composition for rapidly fading red and repairing sensitive skin verifies the safety of the composition acting in vitro; when acting on the skin of a sensitive skin patient, the traditional Chinese medicine composition can obviously relieve swelling and pain, and can achieve the purpose of repairing the skin barrier.

Description

Technical Field

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

[0002] The skin is the largest organ in the human body. It is in direct contact with the external environment and has the functions of protection, excretion, regulating body temperature and sensing external stimuli. With the increasing work pressure and faster pace of life of modern people, a large number of cosmetics are frequently used on the face, and the skin is over-cleaned, resulting in an increasing number of people with sensitive skin. Skin problems caused by sensitive skin, such as skin burning, itching, erythema, and damaged skin barrier, are increasingly attracting attention. Therefore, people are now paying more and more attention to the care and maintenance of sensitive skin, and more and more products to repair sensitive skin are occupying the mainstream market. Summary of the invention

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

[0004] In order to achieve the above purpose, the technical solution adopted by the present invention is: A composition for rapidly fading redness and repairing sensitive skin, comprising the following raw materials by weight: 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 sapodilla extract, calculated by weight.

[0005] Furthermore, the preparation method of the active substance gel is: S1: Mix the N-acetylneuraminic acid, leonurine derivative, Quillaja sylvestris extract, penetration enhancer, emulsifier and co-emulsifier in the formula amount 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; S2: Add the gel matrix to the microemulsion in S1 under stirring to obtain.

[0006] Furthermore, 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.

[0007] Furthermore, the emulsifier is Tween 80, the co-emulsifier is glycerol, and the gel matrix is ​​chitosan.

[0008] Furthermore, the content of the emulsifier is 40 to 60 parts by mass, 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.

[0009] Furthermore, the structural formula of the leonurine derivative is shown in formula (1): , formula (1).

[0010] Furthermore, 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.

[0011] Furthermore, 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.

[0012] Furthermore, 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.

[0013] Furthermore, the preparation method of the composition is: 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.

[0014] Beneficial effects of the present invention: The in vitro cytotoxicity test of the composition for rapidly fading 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.

[0015] The extract of the Quillaja sapodilla tree can effectively relieve skin inflammation, reduce skin discomfort such as redness, swelling and itching, and also has good soothing, moisturizing and skin defense-enhancing functions. The leonurine derivatives have antibacterial, anti-inflammatory and blood-activating functions. N-acetylneuraminic acid can effectively eliminate active oxygen free radicals ROS in the body, control the synthesis of glycosphingolipids, control and enhance cell activity and sensitivity, so that normal physiological activities of cells can proceed normally, which is beneficial to restore the skin barrier. The combination of N-acetylneuraminic acid, Quillaja sapodilla tree extract and leonurine derivatives of the present invention can effectively improve the skin's anti-inflammatory and antibacterial functions and promote skin repair.

[0016] The gel has good adhesion, and the Kochia seeds can improve the permeability of the skin. The present invention opens the permeability of the skin through the Kochia seeds, and the gel adheres to the skin, prolonging the residence time of the active substance on the skin, so that the active substance of the present invention can better act on the skin cells. BRIEF DESCRIPTION OF THE DRAWINGS

[0017] Figure 1 The schematic diagram of the synthesis route of the leonurine derivative of Example 1;

[0018] Figure 2 is the NMR spectrum of substance A in Example 1; Figure 3 is the NMR spectrum of the leonurine derivative in Example 1; Figure 4 This is a diagram showing the effect of using the composition of Example 1 for rapidly fading redness and repairing sensitive skin. DETAILED DESCRIPTION

[0019] The present invention will be further described below in conjunction with the embodiments of the present invention and the accompanying drawings.

[0020] Quillaja sapodilla extract was purchased commercially. Example 1

[0021] The method for preparing the composition for rapidly fading redness and repairing sensitive skin of Example 1 comprises the following steps: 0.2 kg of collagen, 1 kg of glycerin, 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.

[0022] The preparation method of the active substance gel is as follows: 1.5 kg of N-acetylneuraminic acid, 1.2 kg of leonurine derivative, 1.2 kg of Quillaja sylvestris extract, 25 kg of a penetration enhancer, 40 kg of Tween 80, and 40 kg of glycerol are mixed to obtain a mixed phase, and then water is added under stirring until the solution is clear, and a microemulsion is obtained after shear mixing. 30 kg of chitosan is added to the microemulsion under stirring to obtain the active substance gel. The penetration enhancer includes 7.5 kg of azone and 17.5 kg of peppermint oil.

[0023] The preparation method of the leonurine derivative is as follows: S1: 10 mmol of leonurine hydrochloride and 11 mmol of citric anhydride (CAS: 24555-16-6) were added to 20 mL of dichloromethane, stirred evenly at 8 °C, and then 13 mmol of N,N-dicyclohexylcarbodiimide and 13 mmol of 4-dimethylaminopyridine were added, and the temperature was raised to 25 °C for reaction for 14 h; then concentrated, purified by reversed-phase high performance liquid chromatography, and the fractions were concentrated and freeze-dried 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] + .

[0024] S2: Add 5 mmol of substance A and 5.5 mmol of 2-(7-azabenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate to 15 mL of N,N-dimethylformamide, stir evenly, add 16 mmol of N,N-diisopropylethylamine, stir evenly, then add 7 mmol of 2-aminoethanesulfonamide, and react at room temperature for 2.5 h; then purify by reverse phase high performance liquid chromatography, concentrate the fractions, and lyophilize to obtain the leonurine derivative. 1 H NMR( C 22 H 33 N5O12 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

[0025] The method for preparing the composition for rapidly fading redness and repairing sensitive skin of Example 2 comprises the following steps: 0.4 kg of collagen, 2 kg of glycerin, 0.5 kg of Kochia scoparia seeds, and 60 kg of water are mixed, and then 30 kg of active substance gel is added and mixed evenly to obtain the composition.

[0026] The preparation method of the active substance gel is as follows: 2.5 kg of N-acetylneuraminic acid, 2 kg of leonurine derivative, 1.5 kg of Quillaja sylvestris extract, 35 kg of permeation enhancer, 48 kg of Tween 80, and 45 kg of glycerol are mixed to obtain a mixed phase, and then water is added under stirring until the solution is clear, and a microemulsion is obtained after shear mixing. 40 kg of chitosan is added to the microemulsion under stirring to obtain the active substance gel. The permeation enhancer includes 14 kg of azone and 21 kg of peppermint oil.

[0027] The preparation method of the leonurine derivative is as follows: S1: 10 mmol of leonurine hydrochloride and 12 mmol of citric anhydride were added to 20 mL of dichloromethane, stirred evenly at 5°C, and then 15 mmol of N,N-dicyclohexylcarbodiimide and 12 mmol of 4-dimethylaminopyridine were added, and the temperature was raised to 25°C for reaction for 16 h; then concentrated, purified by reversed-phase high performance liquid chromatography, and the fractions were concentrated and freeze-dried to obtain substance A; S2: Add 5 mmol of substance A and 6 mmol of 2-(7-azabenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate to 15 mL of N,N-dimethylformamide, stir evenly, add 18 mmol of N,N-diisopropylethylamine, stir evenly, then add 9 mmol of 2-aminoethanesulfonamide, and react at room temperature for 2.5 h; then purify by reverse phase high performance liquid chromatography, concentrate the fractions, and lyophilize to obtain the leonurine derivative. Example 3

[0028] The preparation method of the composition for rapidly fading redness and repairing sensitive skin of Example 3 comprises the following steps: 0.5 g of collagen, 1.8 g of glycerin, 0.7 g of Kochia scoparia, and 52 g of water are mixed, and then 28 g of active substance gel is added and mixed evenly to obtain the composition.

[0029] The preparation method of the active substance gel is as follows: 3 g of N-acetylneuraminic acid, 2.5 g of leonurine derivative, 1.5 g of Quillaja sylvestris extract, 28 g of a penetration enhancer, 50 g of Tween 80, and 50 g of glycerol are mixed to obtain a mixed phase, and then water is added under stirring until the solution is clear, and a microemulsion is obtained after shear mixing. 38 g of chitosan is added to the microemulsion under stirring to obtain the obtained product. The penetration enhancer includes 13 g of azone and 15 g of peppermint oil.

[0030] The preparation method of the leonurine derivative of Example 3 is the same as that of Example 1.

[0031] Comparative Example 1 The preparation method of the composition for rapidly fading 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 fading redness and repairing sensitive skin in Comparative Example 1 and Example 1 is that in Comparative Example 1, N-acetylneuraminic acid is replaced with an equal mass of a leonurine derivative.

[0032] Comparative Example 2 The preparation method of the composition for quickly removing redness and repairing sensitive skin in Comparative Example 2 is roughly the same as that in Example 1. The difference between the preparation method of the composition for quickly removing redness and repairing sensitive skin in Comparative Example 2 and Example 1 is that in Comparative Example 2, N-acetylneuraminic acid is replaced with an equal mass of a leonurine derivative, and the Quillaja saponaria extract is replaced with an equal mass of a leonurine derivative.

[0033] Comparative Example 3 The preparation method of the composition for rapidly removing 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 removing redness and repairing sensitive skin in Comparative Example 3 and Example 1 is that in Comparative Example 3, the leonurine derivative is replaced with an equal mass of N-acetylneuraminic acid.

[0034] Test Example 1 According to the 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.

[0035] Table 1 Cytotoxicity test results

[0036] Note: Levels greater than 2 are considered to be cytotoxic; the lower the level, the less toxic the composition.

[0037] As can be seen from Table 1, the cytotoxicity level of the tested sample is level 0, and the corresponding reaction degree is non-cytotoxic. The in vitro cytotoxicity test result of the composition for rapidly fading redness and repairing sensitive skin of the present invention is: non-cytotoxic.

[0038] Test Example 2 The compositions of Example 1 and Comparative Examples 1 to 3 were tested for TEWL value (transepidermal water loss, TEWL, reflects the barrier function of the stratum corneum and can be used to evaluate the ability of cosmetics to repair the skin barrier), pain reduction, and redness and swelling reduction. The specific results are shown in Table 2.

[0039] Female volunteers aged between 25 and 35 who met the diagnostic criteria for acne were selected and randomly divided into 5 groups, with 10 people in each group. Apply an appropriate amount of the composition evenly to the red and swollen area, and then gently massage for 3 to 5 minutes, twice a day, for 7 consecutive days. During the whole process, the diet and rest must be standardized, and the affected area should not be squeezed or frequently touched.

[0040] TEWL value testing process: After cleansing your face with water, sit quietly for 30 minutes, use TM300 transepidermal water loss meter to measure TEWL value, and take the average result with stable value as TEWL value.

[0041] Table 2 Sensitive skin healing test results

[0042] Note: The corresponding level of degree is: slight -1, general -2, obvious -3, obvious -4, very obvious -5.

[0043] As can be seen from Table 2, the composition of the present invention has a good repairing effect, and can significantly reduce the pain and redness and swelling in a short period of time; in addition, it can reduce the TEWL value, effectively slow down the rate of water loss through the epidermis, and thus achieve the repair effect on the skin barrier.

[0044] Test Example 3 A 27-year-old female volunteer who met the diagnostic criteria for acne was selected, and the composition for rapid redness fading and sensitive skin repair of Example 1 was evenly applied to the red and swollen area, and then gently massaged for 3 to 5 minutes. The patient's facial condition was observed after 30 minutes and 1 hour. The results were as follows: Figure 4 As shown, from Figure 4 It can be seen that after 30 minutes, the patient's facial redness, swelling and inflammation were significantly improved, and after 60 minutes, the patient's facial redness, swelling and inflammation were basically completely gone, indicating that the composition for rapidly removing redness and repairing sensitive skin of the present invention has good redness removal, anti-inflammatory and repair functions.

[0045] The above-mentioned embodiments are only 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 technicians in this field on the basis of the present invention shall fall within 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 sapodilla extract, calculated by weight.

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: Mix the N-acetylneuraminic acid, leonurine derivative, Quillaja sapodilla extract in the formula amount with a penetration enhancer, an emulsifier, and an emulsifier 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; 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 structural formula of the leonurine derivative is shown in formula (1): , formula (1).

7. The composition for rapidly fading redness and repairing sensitive skin according to claim 6, 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.

8. The composition for rapidly fading redness and repairing sensitive skin according to claim 7, 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.

9. The composition for rapidly fading redness and repairing sensitive skin according to claim 7, 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.

10. 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, the composition is obtained.

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