Nicotinamide whitening, moisturizing and beautifying cream and preparation method thereof

Abstract

The invention provides nicotinamide whitening, moisturizing and beautifying cream and a preparation method thereof, and belongs to the technical field of cosmetics. According to the nicotinamide whitening, moisturizing and beautifying cream, the nicotinamide derivative, the fermentation extract and other components are added, so that the prepared nicotinamide whitening, moisturizing and beautifying cream has better functions of whitening, moisturizing, diminishing inflammation, resisting bacteria and enhancing skin barrier, the absorption of active components by skin can be improved, the addition amount of the active components is reduced, the cost is reduced, the effect is improved, and the nicotinamide whitening, moisturizing and beautifying cream has a good application prospect. Wide application prospects are realized.

Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, and in particular to a niacinamide whitening, moisturizing and beautifying cream and a preparation method thereof. Background Art

[0002] Whitening, from the perspective of skin microstructure, means reducing the deposition and production of pigments, and blocking the activity of enzymes required to induce pigment expression.

[0003] Melanin is essentially an amino acid derivative, which exists in everyone's body. The age of 20-25 is the active period for the formation of melanin deposition. They exist among the cells in the basal layer of the skin, and are a substance called "melanin protosubstance", also called "pigment mother cells". Pigment mother cells secrete melanin. When ultraviolet rays (B waves, A waves) irradiate the skin (B waves, namely UVB, act on the basal layer of the skin), the skin will be in a state of "self-protection", that is, ultraviolet rays stimulate melanin and activate the activity of tyrosinase to protect our skin cells. Dopa is actually the precursor of melanin, which is oxidized by tyrosine and releases melanin. Melanin moves through layers of cell metabolism and reaches the epidermis of the skin to form freckles, sun spots, and dark spots.

[0004] Adequate water content is the basis of skin health. The effect of whitening care is closely related to the moisture of the skin. The better the moisturizing work is, the more obvious the care effect is. This is because the skin is most likely to lose water. The moisture of the skin mainly comes from the body. With the increase of age and changes in the external environment, the protective effect of the sebum film will weaken or be damaged, and the natural moisturizing factor of the stratum corneum will also be lost. At this time, the stratum corneum of the skin is prone to lack of water, which can easily lead to poor keratin metabolism, impurities and metabolites in the cells cannot be removed in time, resulting in the so-called "thick keratin" phenomenon, affecting the skin color, making the skin look dull and dull, and also hindering the penetration of skin care products. Even if whitening care is performed, the effect is limited. Therefore, after the age of 25, any skin should be hydrated and moisturized regularly. Summary of the invention

[0005] The purpose of the present invention is to provide a niacinamide whitening and moisturizing beauty cream and a preparation method thereof, which has good whitening, moisturizing, anti-inflammatory, antibacterial, and skin barrier enhancement functions, can improve the skin's absorption of active components, reduce the amount of active components added, reduce costs, improve effects, and has broad application prospects.

[0006] The technical solution of the present invention is achieved in this way:

[0007] The invention provides a niacinamide whitening, moisturizing and beautifying cream, which is prepared by mixing component A, component B, component C, component D and component E, with a mass ratio of 15-20: 3-4: 0.5-1: 2-4: 0.01-0.015; the component A is prepared by the following raw materials in parts by weight: 8-12 parts of butylene glycol, 0.2-0.5 parts of acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, 0.05-0.25 parts of xanthan gum, 0.05-0.25 parts of disodium EDTA, 0.2-0.5 parts of carboxymethyl deacetylated chitosan, and 70-80 parts of water; the component B is prepared by the following raw materials in parts by weight: 0.5-1 parts of cetearyl alcohol, 2-3 parts of C12-20 acid PEG-8 ester, 1-3 parts of glyceryl stearate, 1-3 parts of caprylic / capric triglyceride, and 5-8 parts of cyclopentasiloxane , tocopherol acetate 0.2-0.5 parts, cetearyl alcohol 1-3 parts, butylated hydroxytoluene 0.2-0.5 parts, p-hydroxyacetophenone 0.2-0.5 parts, licorice (GLYCYRRHIZAURALENSIS) root extract 1-3 parts; the C component is prepared from the following raw materials by weight: sodium acrylate / sodium acryloyldimethyl taurate copolymer 0.1-0.2 parts, polysorbate-80 0.1-0.2 parts, sorbitan oleate 0.05-0.1 parts, water 0.5-1 parts; the D component is prepared from the following raw materials by weight: niacinamide derivative 1-2 parts, fermentation extract 1-3 parts, water 12-18 parts, phenoxyethanol 0.3-0.4 parts, glycerol 0.5-1 parts, arginine 0.2-0.5 parts, glyceryl acrylate / acrylic acid copolymer 0.3-0.6 parts; the E component is flavor.

[0008] As a further improvement of the present invention, the preparation method of the nicotinamide derivative is as follows:

[0009] S1. Add natural borneol and terephthalic acid to toluene, add concentrated sulfuric acid dropwise, heat to reflux and stir to react, cool to room temperature after the reaction, remove the solvent under reduced pressure, wash, separate by column chromatography, and obtain natural borneol terephthalate;

[0010] S2. Adding natural bornyl terephthalate, nicotinamide, EDCI and a catalyst into dichloromethane, stirring for reaction, removing the solvent under reduced pressure, washing, and separating by column chromatography to obtain a nicotinamide derivative.

[0011] As a further improvement of the present invention, in step S1, the molar ratio of natural borneol to terephthalic acid is 1.1-1.2:1, the amount of concentrated sulfuric acid added is 1-2wt%, and the heating reflux stirring reaction time is 4-6h.

[0012] As a further improvement of the present invention, the molar ratio of natural bornyl terephthalate, nicotinamide, EDCI and catalyst in step S2 is 1.1-1.2:1:1.2-1.3:0.3-0.5, the catalyst is 4-dimethylaminopyridine, 1,4-diazabicyclo[2.2.2]octane or 1,8-diazabicyclo[5.4.0]undec-7-ene, and the stirring reaction time is 3-5h.

[0013] As a further improvement of the present invention, the preparation method of the nicotinamide derivative is as follows:

[0014] S1. Add 1.1-1.2 molar equivalents of natural borneol and 1 molar equivalent of terephthalic acid to toluene, add concentrated sulfuric acid dropwise, the amount of concentrated sulfuric acid added is 1-2wt%, and heat to reflux with stirring to react for 4-6h. After the reaction is completed, cool to room temperature, remove the solvent under reduced pressure, wash, and separate by column chromatography to obtain natural borneol terephthalate;

[0015] S2. Add 1.1-1.2 molar equivalents of natural bornyl terephthalate, 1 molar equivalent of nicotinamide, 1.2-1.3 molar equivalents of EDCI, and 0.3-0.5 molar equivalents of catalyst into dichloromethane, stir and react for 3-5 hours, remove the solvent under reduced pressure, wash, and separate by column chromatography to obtain a nicotinamide derivative.

[0016] As a further improvement of the present invention, the preparation method of the fermentation extract is as follows:

[0017] T1. Inoculate Lactobacillus plantarum into a slant culture medium, activate the culture, and prepare a bacterial seed solution;

[0018] T2. The spring flowers are crushed, dried, added to water, sterilized, inoculated with Lactobacillus plantarum seed liquid, fermented, filtered, and the filtrate is the fermentation product;

[0019] T3. The fermentation product was dialyzed, the non-permeated solution was collected, and freeze-dried to obtain a fermentation extract.

[0020] As a further improvement of the present invention, the activation culture conditions in step T1 are 35-38°C, 100-200r / min, activation culture 18-24h, and the bacterial content of the bacterial seed liquid is 10 8 -10 9 cfu / mL.

[0021] As a further improvement of the present invention, the mass ratio of the flos dasyphylla and water in step T2 is 7-12:100, the inoculation amount of the plant lactobacillus seed liquid is 2-3v / v%, and the fermentation culture conditions are 35-38°C, 100-200r / min, and the activation culture is 36-48h.

[0022] As a further improvement of the present invention, the dialysis bag used in step T3 has a pore size of 10-20 KDa and the time is 10-12 hours.

[0023] The present invention further protects a method for preparing the above-mentioned niacinamide whitening, moisturizing and beautifying cream, comprising the following steps:

[0024] (1) Weigh the components of phases A, B, C, D, and E in proportion;

[0025] (2) Heat the water in phase A to 80-90°C and add other raw materials in phase A and stir to disperse evenly;

[0026] (3) Add phase B into an oil pan and heat to 80-90°C until completely dissolved;

[0027] (4) Add the dissolved phase B to phase A and stir and disperse for 10-20 minutes;

[0028] (5) Add phase C to phase A+B and stir and disperse for 10-20 minutes;

[0029] (6) Mix and dissolve phase D separately in advance, and after cooling to 40-50°C, add it to phase A+B+C and stir to mix evenly;

[0030] (7) Finally, add phase E, stir and disperse for 10-20 minutes, emulsify at 5000-8000 r / min for 10-15 minutes, and discharge the material to obtain niacinamide whitening and moisturizing beauty cream.

[0031] The present invention has the following beneficial effects:

[0032] Niacinamide can inhibit the deposition of melanin, block the transfer of melanin to surface cells, and accelerate the shedding of keratin containing melanin, thereby fading spots and reducing the size and number of spots. It can also reduce the yellowing of protein after saccharification through anti-glycosylation and brighten the skin. Niacinamide can promote microcirculation in the dermis, maintain the moisture content of the skin, reduce the damage of free radicals to the skin, thereby slowing down skin aging and enhancing the skin's defense. Niacinamide can also enhance the skin barrier function and improve the skin's water retention capacity by increasing the ceramide content in the stratum corneum. Niacinamide can relieve skin inflammation and redness, repair damaged skin barriers, stimulate collagen production, increase skin elasticity and firmness, reduce the appearance of fine lines and wrinkles, and delay skin aging. However, niacinamide is easy to decompose and produce niacin, which can easily irritate the skin when used in large quantities, causing skin intolerance. It is also not suitable for mixing with other acid products. If mixed, it will cause the pH value of the skin to change, and niacinamide will release a large amount of niacin, causing irritation to the skin. Niacinamide cannot inhibit the activity of tyrosinase, nor can it affect the formation of melanin in melanocytes. This means that using niacinamide will not essentially prevent the skin from producing melanin. Stopping the use of niacinamide will cause a large amount of melanin that was not decomposed to be released back into the epidermis, flowing into keratinocytes, causing the skin to darken again.

[0033] Borneol has a wide range of pharmacological effects such as analgesia, anti-inflammatory, and antibacterial. It can not only be used as a transdermal drug, but also is a good transdermal enhancer. However, in long-term clinical medication, it is found that borneol is easy to sublimate and has certain toxic and side effects. The present invention couples borneol and nicotinamide through terephthalic acid, which overcomes the problems of nicotinamide being easy to decompose into nicotinic acid and producing irritation, and at the same time, it also overcomes the problems of borneol being easy to sublimate and having certain toxic and side effects. The prepared nicotinamide derivative has a good transdermal enhancement effect, can promote the transdermal absorption of other active components, including fermented extracts, and at the same time, can also play the moisturizing, whitening, and anti-inflammatory effects of nicotinamide, greatly improving the effect of the beauty cream and reducing the cost.

[0034] In addition, the fermented extract prepared by the present invention is obtained by fermenting and breaking the wall of Flos Formosans, and the fermentation of Lactobacillus plantarum can produce functional substances such as polysaccharides, proteins and lactic acid, and its bacteria and polysaccharides have antioxidant effects. These macromolecular structures such as polysaccharides and proteins have good effects of inhibiting tyrosinase and replenishing water and moisturizing, thereby inhibiting the production of melanin, and complementing niacinamide. Niacinamide can inhibit the deposition of melanin and block the transfer of melanin to surface cells, thereby fundamentally inhibiting the production of melanin, avoiding the problem of blackening after discontinuation of use, so that the product prepared by the present invention is more effective and the effect is more lasting.

[0035] The niacinamide whitening and moisturizing beauty cream prepared by the present invention has good whitening, moisturizing, anti-inflammatory, antibacterial and skin barrier enhancement functions, can improve the skin's absorption of active components, reduce the amount of active components added, reduce costs, improve effects, and has broad application prospects. DETAILED DESCRIPTION

[0036] The technical solutions in the embodiments of the present invention are described clearly and completely below. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0037] EDCI, 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride.

[0038] Lactobacillus plantarum, 10 billion cfu / g, was purchased from Shanghai Zhongfeng Biotechnology Co., Ltd.

[0039] Preparation Example 1 Preparation of Nicotinamide Derivatives

[0040] The synthetic route is as follows:

[0041]

[0042] The specific method is as follows:

[0043] S1. Add 11mmol natural borneol and 10mmol terephthalic acid into 100mL toluene, add concentrated sulfuric acid dropwise, the amount of concentrated sulfuric acid added is 1wt%, heat reflux and stir to react for 4h, cool to room temperature after the reaction, remove the solvent under reduced pressure, wash, and separate by column chromatography (ethyl acetate: petroleum ether = 3:1) to obtain natural borneol terephthalate; ESI-MS calculated value: C 18 H 23 O4(M+H) + 303.15, found: 303.2, yield 47%.

[0044] NMR results: 1 H NMR (300MHz, CDCl3) δ11.0 (br, 1H), 8.24 (d, J = 6.4Hz, 2H), 8.2 (d, J = 6.3Hz, 2H), 3.87(s, 1H), 1.82(d, 2H), 1.36-1.42(m, 5H), 1.17(s, 3H), 1.10(s, 6H).

[0045] S2. Add 11mmol of natural bornyl terephthalate, 10mmol of nicotinamide, 12mmol of EDCI, and 3mmol of catalyst into 100mL of dichloromethane, stir and react for 3h, remove the solvent under reduced pressure, wash, and separate by column chromatography (ethyl acetate: petroleum ether = 1:1) to obtain nicotinamide derivatives. ESI-MS calculated value: C 24 H 27 N2O4(M+H) + 407.19, found: 407.2, yield: 79%.

[0046] NMR results: 1 H NMR (300MHz, CDCl3) δ10.0 (br, 1H), 9.17 (s, 1H), 8.84 (d, J = 5.6Hz, 1H), 8.32 (d, J = 6.1Hz, 1H), 7.92 (m, 2H), 7.72(m, 2H), 7.62(m, 1H), 3.85(s, 1H), 1.80(d, 2H), 1.38-1.45(m, 5H), 1.19(s, 3H), 1.14(s, 6H).

[0047] Preparation Example 2 Preparation of Nicotinamide Derivatives

[0048] The specific method is as follows:

[0049] S1. Add 12 mmol of natural borneol and 10 mmol of terephthalic acid to 100 mL of toluene, add concentrated sulfuric acid dropwise, the amount of concentrated sulfuric acid added is 2 wt%, heat to reflux and stir to react for 6 h, cool to room temperature after the reaction, remove the solvent under reduced pressure, wash, and separate by column chromatography (ethyl acetate: petroleum ether = 3:1) to obtain natural borneol terephthalate;

[0050] S2. Add 12 mmol of natural bornyl terephthalate, 10 mmol of nicotinamide, 13 mmol of EDCI and 5 mmol of catalyst into 100 mL of dichloromethane, stir and react for 5 h, remove the solvent under reduced pressure, wash and separate by column chromatography (ethyl acetate: petroleum ether = 1:1) to obtain a nicotinamide derivative.

[0051] Preparation Example 3 Preparation of Nicotinamide Derivatives

[0052] The specific method is as follows:

[0053] S1. Add 11.5 mmol of natural borneol and 10 mmol of terephthalic acid to 100 mL of toluene, add concentrated sulfuric acid dropwise, the amount of concentrated sulfuric acid added is 1.5 wt %, heat to reflux and stir to react for 5 h, cool to room temperature after the reaction, remove the solvent under reduced pressure, wash, and separate by column chromatography (ethyl acetate: petroleum ether = 3:1) to obtain natural borneol terephthalate;

[0054] S2. Add 11.5 mmol of natural bornyl terephthalate, 10 mmol of nicotinamide, 12.5 mmol of EDCI and 4 mmol of catalyst into 100 mL of dichloromethane, stir and react for 4 h, remove the solvent under reduced pressure, wash and separate by column chromatography (ethyl acetate: petroleum ether = 1:1) to obtain a nicotinamide derivative.

[0055] Preparation Example 4 Preparation of fermentation extract

[0056] Here’s how:

[0057] T1. Inoculate Lactobacillus plantarum into the slant culture medium, and activate and culture for 18 hours at 35°C and 100 r / min to obtain a culture medium with a bacterial count of 10 8 -10 9 cfu / mL of bacterial seed solution;

[0058] T2. 7g of spring flowers were crushed, dried, added to 100mL of water, sterilized, inoculated with Lactobacillus plantarum seed solution, the inoculation amount was 2v / v%, 35°C, 100r / min, activated and cultured for 36h, filtered, and the filtrate was the fermentation product;

[0059] T3. The fermentation product was dialyzed using a dialysis bag with a pore size of 10 KDa for 10 h, the non-permeated liquid was collected, and freeze-dried to obtain a fermentation extract.

[0060] Preparation Example 5 Preparation of fermentation extract

[0061] Here’s how:

[0062] T1. Inoculate Lactobacillus plantarum into the slant culture medium, and activate and culture for 24 hours at 38°C and 200r / min to obtain a culture medium with a bacterial count of 10 8 -10 9 cfu / mL of bacterial seed solution;

[0063] T2. 12g of spring flowers were crushed, dried, added to 100mL of water, sterilized, inoculated with Lactobacillus plantarum seed solution, the inoculation amount was 3v / v%, 38°C, 200r / min, activated and cultured for 48h, filtered, and the filtrate was the fermentation product;

[0064] T3. The fermentation product was dialyzed using a dialysis bag with a pore size of 20 KDa for 12 h, and the non-permeated liquid was collected and freeze-dried to obtain a fermentation extract.

[0065] Preparation Example 6 Preparation of fermentation extract

[0066] Here’s how:

[0067] T1. Inoculate Lactobacillus plantarum into the slant culture medium, and activate and culture for 21 hours at 37°C and 150r / min to obtain a culture medium with a bacterial count of 10 8 -10 9 cfu / mL of bacterial seed solution;

[0068] T2. 10g of spring flowers were crushed, dried, added to 100mL of water, sterilized, inoculated with Lactobacillus plantarum seed solution, the inoculation amount was 2.5v / v%, 37°C, 150r / min, activated and cultured for 42h, filtered, and the filtrate was the fermentation product;

[0069] T3. The fermentation product was dialyzed using a dialysis bag with a pore size of 15 KDa for 11 h, the non-permeated liquid was collected, and freeze-dried to obtain a fermentation extract.

[0070] Comparative Preparation Example 1

[0071] Compared with Preparation Example 6, the difference is that step T3 is not performed.

[0072] The details are as follows:

[0073] T1. Inoculate Lactobacillus plantarum into the slant culture medium, and activate and culture for 21 hours at 37°C and 150r / min to obtain a culture medium with a bacterial count of 10 8 -10 9 cfu / mL of bacterial seed solution;

[0074] T2. Crush 10g of Flos Forsythiaes, dry it, add it into 100mL of water, sterilize it, inoculate it with 2.5v / v% of Lactobacillus plantarum seed solution, inoculate it at 37℃, 150r / min, activate and culture it for 42h, filter it, freeze-dry the filtrate, and obtain the fermentation extract.

[0075] Test Example 1

[0076] The fermentation extracts obtained in Preparation Examples 1-3 and Comparative Preparation Example 1 were formulated into 0.05 mg / mL sample solutions. Take 2.0 mL of the sample solution in a stoppered colorimetric tube, add 2.0 mL of 0.0002 mol / L DPPH solution, adjust the volume, react in the dark for 30 minutes, and measure its absorbance A0 at a wavelength of 517 nm. According to the above method, the absorbance values ​​of the control group (the DPPH solution was replaced by an equal volume of ethanol solution) were measured as A1, and the absorbance value of the blank group (2.0 mL of each sample solution in the test group was replaced by 2.0 mL of anhydrous ethanol) was A2. Prepare an equal concentration of vitamin C solution as a control, and determine its clearance rate by the same method. The results are shown in Table 1. The calculation formula is as follows:

[0077] DPPH free radical scavenging rate (%) = 1-(A0-A1)A2×100

[0078] Table 1

[0079] Group DPPH free radical scavenging rate (%) VC Group 78.9 Preparation Example 1 93.3 Preparation Example 2 93.5 Preparation Example 3 94.0 Comparative Preparation Example 1 82.3

[0080] It can be seen from the above table that the extract 1 obtained by the preparation examples 1-3 of the present invention has good antioxidant activity.

[0081] Example 1

[0082] This embodiment provides a method for preparing a niacinamide whitening, moisturizing and beautifying cream.

[0083] It is prepared by mixing component A, component B, component C, component D and component E, with a mass ratio of 15:3:0.5:2:0.01.

[0084] The component A is prepared from the following raw materials in parts by weight: 8 parts of butanediol, 0.2 parts of acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, 0.05 parts of xanthan gum, 0.05 parts of disodium EDTA, 0.2 parts of carboxymethyl deacetylated chitosan, and 70 parts of water.

[0085] The B component is prepared from the following raw materials in parts by weight: 0.5 parts of cetearyl alcohol, 2 parts of C12-20 acid PEG-8 ester, 1 part of glyceryl stearate, 1 part of caprylic / capric triglyceride, 5 parts of cyclopentasiloxane, 0.2 parts of tocopheryl acetate, 1 part of cetearyl alcohol, 0.2 parts of butylated hydroxytoluene, 0.2 parts of p-hydroxyacetophenone, and 1 part of liquorice root extract.

[0086] The C component is prepared from the following raw materials in parts by weight: 0.1 part of sodium acrylate / sodium acryloyldimethyl taurate copolymer, 0.1 part of polysorbate-80, 0.05 part of sorbitan oleate, and 0.5 part of water.

[0087] The D component is prepared from the following raw materials in parts by weight: 1 part of the nicotinamide derivative prepared in Preparation Example 1, 1 part of the fermentation extract prepared in Preparation Example 4, 12 parts of water, 0.3 parts of phenoxyethanol, 0.5 parts of glycerol, 0.2 parts of arginine, and 0.3 parts of glyceryl acrylate / acrylic acid copolymer.

[0088] The E component is fragrance.

[0089] The following steps are involved:

[0090] (1) Weigh the components of phases A, B, C, D, and E in proportion;

[0091] (2) Heat the water in phase A to 80°C and add other raw materials in phase A and stir to disperse evenly;

[0092] (3) Add phase B into an oil pan and heat to 80°C until completely dissolved;

[0093] (4) Add the dissolved phase B into phase A and stir and disperse for 10 minutes;

[0094] (5) Add phase C to phase A+B and stir and disperse for 10 minutes;

[0095] (6) Mix and dissolve phase D separately in advance, and after cooling to 40°C, add it to phase A+B+C and stir to mix evenly;

[0096] (7) Finally, add phase E, stir and disperse for 10 minutes, emulsify at 5000 r / min for 10 minutes, and discharge the mixture to obtain niacinamide whitening and moisturizing beauty cream.

[0097] Example 2

[0098] This embodiment provides a method for preparing a niacinamide whitening, moisturizing and beautifying cream.

[0099] It is prepared by mixing component A, component B, component C, component D and component E, with a mass ratio of 20:4:1:4:0.015.

[0100] The component A is prepared from the following raw materials in parts by weight: 12 parts of butanediol, 0.5 parts of acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, 0.25 parts of xanthan gum, 0.25 parts of disodium EDTA, 0.5 parts of carboxymethyl deacetylated chitosan, and 80 parts of water.

[0101] The B component is prepared from the following raw materials in parts by weight: 1 part of cetearyl alcohol, 3 parts of C12-20 acid PEG-8 ester, 3 parts of glyceryl stearate, 3 parts of caprylic / capric triglyceride, 8 parts of cyclopentasiloxane, 0.5 parts of tocopheryl acetate, 3 parts of cetearyl alcohol, 0.5 parts of butylated hydroxytoluene, 0.5 parts of p-hydroxyacetophenone, and 3 parts of liquorice root extract.

[0102] The C component is prepared from the following raw materials in parts by weight: 0.2 parts of sodium acrylate / sodium acryloyldimethyltaurate copolymer, 0.2 parts of polysorbate-80, 0.1 parts of sorbitan oleate, and 1 part of water.

[0103] The D component is prepared from the following raw materials in parts by weight: 2 parts of the nicotinamide derivative prepared in Preparation Example 2, 3 parts of the fermentation extract prepared in Preparation Example 5, 18 parts of water, 0.4 parts of phenoxyethanol, 1 part of glycerol, 0.5 parts of arginine, and 0.6 parts of glycerol acrylate / acrylic acid copolymer.

[0104] The E component is fragrance.

[0105] The following steps are involved:

[0106] (1) Weigh the components of phases A, B, C, D, and E in proportion;

[0107] (2) Heat the water in phase A to 90°C and add other raw materials in phase A and stir to disperse evenly;

[0108] (3) Add phase B into an oil pan and heat to 90°C until completely dissolved;

[0109] (4) Add the dissolved phase B into phase A and stir and disperse for 20 minutes;

[0110] (5) Add phase C to phase A+B and stir and disperse for 20 minutes;

[0111] (6) Mix and dissolve phase D separately in advance, and after cooling to 50°C, add it to phase A+B+C and stir to mix evenly;

[0112] (7) Finally, add phase E, stir and disperse for 20 minutes, emulsify at 8000 r / min for 15 minutes, and discharge the mixture to obtain niacinamide whitening and moisturizing beauty cream.

[0113] Example 3

[0114] This embodiment provides a method for preparing a niacinamide whitening, moisturizing and beautifying cream.

[0115] It is prepared by mixing component A, component B, component C, component D and component E, with a mass ratio of 17:3.5:0.7:3:0.012.

[0116] The component A is prepared from the following raw materials in parts by weight: 10 parts of butanediol, 0.3 parts of acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, 0.15 parts of xanthan gum, 0.15 parts of disodium EDTA, 0.3 parts of carboxymethyl deacetylated chitosan, and 75 parts of water.

[0117] The B component is prepared from the following raw materials in parts by weight: 0.7 parts of cetearyl alcohol, 2.5 parts of C12-20 acid PEG-8 ester, 2 parts of glyceryl stearate, 2 parts of caprylic / capric triglyceride, 6 parts of cyclopentasiloxane, 0.35 parts of tocopheryl acetate, 2 parts of cetearyl alcohol, 0.35 parts of butylated hydroxytoluene, 0.3 parts of p-hydroxyacetophenone, and 2 parts of liquorice root extract.

[0118] The C component is prepared from the following raw materials in parts by weight: 0.15 parts of sodium acrylate / sodium acryloyldimethyltaurate copolymer, 0.15 parts of polysorbate-80, 0.07 parts of sorbitan oleate, and 0.7 parts of water.

[0119] The D component is prepared from the following raw materials in parts by weight: 1.5 parts of the nicotinamide derivative prepared in Preparation Example 3, 2 parts of the fermentation extract prepared in Preparation Example 6, 16 parts of water, 0.35 parts of phenoxyethanol, 0.7 parts of glycerol, 0.3 parts of arginine, and 0.45 parts of glycerol acrylate / acrylic acid copolymer.

[0120] The E component is fragrance.

[0121] The following steps are involved:

[0122] (1) Weigh the components of phases A, B, C, D, and E in proportion;

[0123] (2) Heat the water in phase A to 85°C and add other raw materials in phase A and stir to disperse evenly;

[0124] (3) Add phase B into an oil pan and heat to 85°C until completely dissolved;

[0125] (4) Add the dissolved phase B into phase A and stir and disperse for 15 minutes;

[0126] (5) Add phase C to phase A+B and stir and disperse for 15 minutes;

[0127] (6) Mix and dissolve phase D separately in advance, and after cooling to 45°C, add it to phase A+B+C and stir to mix evenly;

[0128] (7) Finally, add phase E, stir and disperse for 15 minutes, emulsify at 7000 r / min for 12 minutes, and discharge to obtain niacinamide whitening and moisturizing beauty cream.

[0129] Comparative Example 1

[0130] Compared with Example 3, the difference is that the nicotinamide derivative is replaced by a mixture of nicotinamide and natural borneol in a molar ratio of 1:1.

[0131] Comparative Example 2

[0132] Compared with Example 3, the difference is that the nicotinamide derivative is replaced by nicotinamide.

[0133] Comparative Example 3

[0134] Compared with Example 3, the difference is that the nicotinamide derivative is replaced by natural borneol.

[0135] Comparative Example 4

[0136] Compared with Example 3, the difference is that no nicotinamide derivative is added.

[0137] Comparative Example 5

[0138] Compared with Example 3, the difference is that the fermentation extract is prepared by Comparative Preparation Example 1.

[0139] Comparative Example 6

[0140] Compared with Example 3, the difference is that no fermentation extract is added.

[0141] Test Example 2 Skin Moisturizing Test

[0142] 100 female volunteers aged 28-54 were selected on a voluntary basis and randomly divided into 10 groups, each with 10 people, namely, Examples 1-3, Comparative Examples 1-6 and a control group. No drugs or cosmetics irrelevant to the test were applied during the test. The subjects used samples on both sides of their faces. The sample group used the nicotinamide whitening and moisturizing beauty cream prepared in Examples 1-3 and Comparative Examples 1-6, and the control group used an equal amount of water. Once in the morning and evening for a total of 14 days. Before the test, the subjects washed the test site with clean water, exposed the test site after drying, and sat quietly for 30 minutes at 23±2°C and a relative humidity of 50±5%. The stratum corneum water content of the test site was tested using a CM825 skin moisture test probe, and the average value of 3 times was taken. The stratum corneum water content was measured before the start of the test. One hour after the sample was used on the 14th day, the stratum corneum water content of the test subject was tested, and the skin water content change rate (%) was calculated.

[0143] Skin moisture content change rate (%) = (moisture content after use - moisture content before use) / moisture content before use × 100%. The results are shown in Table 2.

[0144] Table 2

[0145] Group Skin moisture content change rate (%) Example 1 32 Example 2 31 Example 3 34 Comparative Example 1 27 Comparative Example 2 29 Comparative Example 3 24 Comparative Example 4 22 Comparative Example 5 25 Comparative Example 6 20 Control group 12

[0146] It can be seen from the above table that the niacinamide whitening and moisturizing beauty creams prepared in Examples 1-3 of the present invention have good skin moisturizing effects.

[0147] Test Example 3 Cellular tyrosinase activity and melanin content experiment

[0148] The experiment was divided into a normal group, a model group, example 1-3 groups, and a comparative example 1-6 groups.

[0149] B16F10 cells were collected at 5×10 4 Each well was inoculated with 500 μL of α-MSH in two 24-well plates. After 24 hours of culture, 100 nmol / L melanocyte stimulating hormone (α-MSH) was added to the other groups except the normal group to induce the α-MSH-induced melanin high expression model, and then the sample solution (nicotinamide whitening and moisturizing cream was prepared with deionized water to a concentration of 0.01 mg / mL) was added. Three replicate wells were set up in each group and cultured for 48 hours.

[0150] The supernatant of a 24-well plate of cells was discarded, the cells were washed with PBS, and the cells were lysed. 60 μL of the supernatant was taken into a 96-well plate, 140 μL of 0.1 wt% L-dopamine was added, and the plates were incubated at 37°C for 1 h. The absorbance of each well was measured at a wavelength of 490 nm to determine the tyrosinase activity.

[0151] After washing the cells in another 24-well plate with PBS, add 60 μL of 1.0 mmoL / L NaOH solution (containing 10 wt% DMSO) to each well, lyse the cells at 80°C for 1 h, measure the absorbance of each well at a wavelength of 405 nm, and determine the cellular melanin content.

[0152] The results are shown in Table 2.

[0153] Table 2

[0154] Group Tyrosinase activity (%) Cell melanin content (%) Normal group 52.52 69.56 Model Group 100 100 Example 1 39.56 65.25 Example 2 39.19 65.54 Example 3 39.75 64.75 Comparative Example 1 42.29 70.24 Comparative Example 2 45.56 72.66 Comparative Example 3 62.15 79.09 Comparative Example 4 64.66 81.25 Comparative Example 5 60.82 78.52 Comparative Example 6 72.59 88.13

[0155] It can be seen from the above table that the niacinamide whitening and moisturizing beauty cream prepared in Examples 1-3 of the present invention has a good effect of inhibiting tyrosinase activity and inhibiting cellular melanin production.

[0156] The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principle of the present invention should be included in the protection scope of the present invention.

Claims

1. A niacinamide whitening and moisturizing beauty cream, characterized in that: The invention is prepared by mixing component A, component B, component C, component D and component E, with a mass ratio of 15-20: 3-4: 0.5-1: 2-4: 0.01-0.015; the component A is prepared by the following raw materials in parts by weight: 8-12 parts of butylene glycol, 0.2-0.5 parts of acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, 0.05-0.25 parts of xanthan gum, 0.05-0.25 parts of disodium EDTA, 0.2-0.5 parts of carboxymethyl deacetylated chitosan, and 70-80 parts of water; the component B is prepared by the following raw materials in parts by weight: 0.5-1 parts of cetearyl alcohol, 2-3 parts of C12-20 acid PEG-8 ester, 1-3 parts of glyceryl stearate, 1-3 parts of caprylic / capric triglyceride, 5-8 parts of cyclopentasiloxane, 0. 2-0.5 parts, cetearyl alcohol 1-3 parts, butylated hydroxytoluene 0.2-0.5 parts, p-hydroxyacetophenone 0.2-0.5 parts, licorice (GLYCYRRHIZAURALENSIS) root extract 1-3 parts; the C component is prepared from the following raw materials by weight: sodium acrylate / sodium acryloyldimethyl taurate copolymer 0.1-0.2 parts, polysorbate-80 0.1-0.2 parts, sorbitan oleate 0.05-0.1 parts, water 0.5-1 parts; the D component is prepared from the following raw materials by weight: niacinamide derivative 1-2 parts, fermentation extract 1-3 parts, water 12-18 parts, phenoxyethanol 0.3-0.4 parts, glycerol 0.5-1 parts, arginine 0.2-0.5 parts, glyceryl acrylate / acrylic acid copolymer 0.3-0.6 parts; the E component is flavor.

2. The niacinamide whitening and moisturizing beauty cream according to claim 1, characterized in that: The preparation method of the nicotinamide derivative is as follows: S1. Add natural borneol and terephthalic acid to toluene, add concentrated sulfuric acid dropwise, heat to reflux and stir to react, cool to room temperature after the reaction, remove the solvent under reduced pressure, wash, separate by column chromatography, and obtain natural borneol terephthalate; S2. Adding natural bornyl terephthalate, nicotinamide, EDCI and a catalyst into dichloromethane, stirring for reaction, removing the solvent under reduced pressure, washing, and separating by column chromatography to obtain a nicotinamide derivative.

3. The niacinamide whitening and moisturizing beauty cream according to claim 2, characterized in that: In step S1, the molar ratio of natural borneol to terephthalic acid is 1.1-1.2:1, the amount of concentrated sulfuric acid added is 1-2wt%, and the heating reflux stirring reaction time is 4-6h.

4. The niacinamide whitening and moisturizing beauty cream according to claim 2, characterized in that: In step S2, the molar ratio of natural bornyl terephthalate, nicotinamide, EDCI and catalyst is 1.1-1.2:1:1.2-1.3:0.3-0.5, the catalyst is 4-dimethylaminopyridine, 1,4-diazabicyclo[2.2.2]octane or 1,8-diazabicyclo[5.4.0]undec-7-ene, and the stirring reaction time is 3-5h.

5. The niacinamide whitening and moisturizing beauty cream according to claim 2, characterized in that: The preparation method of the nicotinamide derivative is specifically as follows: S1. Add 1.1-1.2 molar equivalents of natural borneol and 1 molar equivalent of terephthalic acid to toluene, add concentrated sulfuric acid dropwise, the amount of concentrated sulfuric acid added is 1-2wt%, and heat to reflux with stirring to react for 4-6h. After the reaction is completed, cool to room temperature, remove the solvent under reduced pressure, wash, and separate by column chromatography to obtain natural borneol terephthalate; S2. Add 1.1-1.2 molar equivalents of natural bornyl terephthalate, 1 molar equivalent of nicotinamide, 1.2-1.3 molar equivalents of EDCI, and 0.3-0.5 molar equivalents of catalyst into dichloromethane, stir and react for 3-5 hours, remove the solvent under reduced pressure, wash, and separate by column chromatography to obtain a nicotinamide derivative.

6. The niacinamide whitening and moisturizing beauty cream according to claim 1, characterized in that: The preparation method of the fermentation extract is as follows: T1. Inoculate Lactobacillus plantarum into a slant culture medium, activate the culture, and prepare a bacterial seed solution; T2. The spring flowers are crushed, dried, added to water, sterilized, inoculated with Lactobacillus plantarum seed liquid, fermented, filtered, and the filtrate is the fermentation product; T3. The fermentation product was dialyzed, the non-permeated solution was collected, and freeze-dried to obtain a fermentation extract.

7. The niacinamide whitening and moisturizing beauty cream according to claim 6, characterized in that: The activation culture conditions in step T1 are 35-38°C, 100-200r / min, activation culture for 18-24h, and the bacterial content of the bacterial seed liquid is 10 8 -10 9 cfu / mL.

8. The niacinamide whitening and moisturizing beauty cream according to claim 6, characterized in that: In step T2, the mass ratio of the flos dasyphylla and water is 7-12:100, the inoculation amount of the plant lactobacillus seed solution is 2-3v / v%, and the fermentation culture conditions are 35-38°C, 100-200r / min, and the activation culture is 36-48h.

9. The niacinamide whitening and moisturizing beauty cream according to claim 6, characterized in that: The dialysis bag used in step T3 has a pore size of 10-20 KDa and the dialysis time is 10-12 hours.

10. A method for preparing the niacinamide whitening, moisturizing and beautifying cream according to any one of claims 1 to 9, characterized in that: The following steps are involved: (1) Weigh the components of phases A, B, C, D, and E in proportion; (2) Heat the water in phase A to 80-90°C and add other raw materials in phase A and stir to disperse evenly; (3) Add phase B into an oil pan and heat to 80-90°C until completely dissolved; (4) Add the dissolved phase B to phase A and stir and disperse for 10-20 minutes; (5) Add phase C to phase A+B and stir and disperse for 10-20 minutes; (6) Mix and dissolve phase D separately in advance, and after cooling to 40-50°C, add it to phase A+B+C and stir to mix evenly; (7) Finally, add phase E, stir and disperse for 10-20 minutes, emulsify at 5000-8000 r / min for 10-15 minutes, and discharge the material to obtain niacinamide whitening and moisturizing beauty cream.

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