Emulsion containing anti-sugar and anti-oxidation composition and preparation method thereof

Abstract

The invention discloses an emulsion containing an anti-sugar and anti-oxidation composition and a preparation method of the emulsion. The emulsion comprises the following components in percentage by mass: 0.1-10% of the anti-sugar and anti-oxidation composition, the anti-sugar and anti-oxidation composition is prepared from an astaxanthin solution, ergothioneine, a lavender flower extract, an olein inclusion, thiotaurine and pyridine polyamine dihydrochloride; the preparation method comprises the following steps: weighing the polyol solution, the gel and the water phase in proportion, sequentially preparing the polyol solution, the gel and the water phase, adding the water phase into the gel, and homogenizing to obtain a finished product emulsion. The invention has the advantages of relatively better effect, relatively lower production cost and relatively better stability.

Description

TECHNICAL FIELD

[0001] The present application relates to the technical field of emulsion preparation, in particular to an emulsion containing an anti-sugar and anti-oxidation composition and a preparation method thereof. BACKGROUND

[0002] With age, external and internal factors can cause the human body to gradually age, which will manifest in skin as the appearance of wrinkles, decreased skin elasticity, deepening of expression wrinkles, dry and loose skin, thinning of subcutaneous fat, and other signs of aging. Glycation and oxidation play a very important role in this process.

[0003] First, oxidative reactions in the body produce free radicals, and oxidative stress caused by the accumulation of free radicals can change the intracellular redox state, damage lipids, proteins, nucleic acids, and organelles, leading to the occurrence of cell aging, and cause skin problems such as dull complexion, pigmentation, wrinkles, and loose skin, which is one of the core mechanisms of skin aging. At the same time, excess advanced glycation end products produced by glycation reactions can undergo glycation cross-linking reactions with skin elastic fibers and collagen, causing skin yellowing and reduced skin elasticity. With age, the protein metabolic turnover rate of the human body gradually slows down, and advanced glycation end products accumulate in the body, changing cell and protein function and causing skin problems. In addition, free radicals (ROS) are accelerators of glycation reactions, and the intermediate product of AGE formation, active carbonyl, is derived from oxidation, and oxidative stress environments significantly promote the occurrence of glycation reactions and the formation of AGEs. Proteins damaged by glycation are more susceptible to free radical attack.

[0004] Therefore, the anti-sugar and anti-oxidation effects are key to effectively solving a series of skin problems.

[0005] Transdermal penetration and absorption is a major problem in the skin care industry, and particle size is an important influencing factor. The emulsified products on the market are often limited by the formulation components and process equipment, with large and uneven particle size of the dispersed phase, generally in the micron level, with a few microns and often more than 10 microns. Therefore, the product has poor substance penetration, dispersion and stability, and it is difficult to play an effective role. Nanoemulsion is a kind of thermodynamically unstable but kinetically stable liquid-liquid dispersion system, with droplet size in the continuous phase between 20-500 nm. Based on its nanoscale particle size, the diffusion effect of Brownian motion can balance the sedimentation effect caused by gravity, avoid particle aggregation and gravity separation, make the system more stable, and the high specific surface area and small droplet size of nanoemulsion can also promote the rapid penetration of active ingredients. However, the method of preparing nanoemulsion often needs to add a large amount of emulsifier and high-energy shearing process, which is strict in equipment and formulation requirements, and high in energy consumption, and it is difficult to realize large-scale industrial production. By optimizing the emulsification system and preparation process, the emulsion particle size is reduced without increasing the amount of emulsifier, the stability and penetration and absorption of the product are improved, and the demand for industrial production is realized, which is a difficult problem to be solved in the industry.

[0006] The anti-sugar and anti-oxidation products on the market are relatively single, and the products cannot play the real anti-sugar and anti-oxidation effect. On the one hand, people cannot choose the anti-sugar and anti-oxidation composition scientifically and make it multi-pathway covered and synergistically effective. On the other hand, due to the limitation of emulsification equipment and components, the droplet size of most skin care emulsions is too large, usually in the micron level, with poor transdermal permeability, and the active ingredients are difficult to be well absorbed by the skin. SUMMARY

[0007] The purpose of the present application is to provide an emulsion containing an anti-sugar and anti-oxidation composition and a preparation method thereof. The present application has the advantages of relatively better effect, relatively lower production cost and relatively better stability.

[0008] The technical scheme of the present application is as follows: An emulsion containing an anti-sugar and anti-oxidation composition, comprising 0.1-10% of the anti-sugar and anti-oxidation composition, 0.03-1% of the emulsifier, 1-20% of the polyol, 1-20% of the humectant, 0.2-20% of the oil, 0.1-1% of the thickening agent, 0-2% of the PH regulator, 0.1-0.6% of the preservative and 50-95% of the water; the anti-sugar and anti-oxidation composition comprises astaxanthin solution, ergothioneine, lavender flower extract, oleuropein package, taurine and pyridoxamine dihydrochloride.

[0009] The emulsion containing the anti-glycative antioxidant composition of the foregoing comprises, by mass percentage, 2.532% of the anti-glycative antioxidant composition, 0.166% of the emulsifier, 4% of the polyol, 7% of the humectant, 1.03% of the oil, 0.26% of the thickening agent, 0.170% of the pH adjuster, 0.38% of the preservative, and 86.341% of the water.

[0010] The emulsion containing the anti-glycative antioxidant composition of the foregoing comprises, by mass percentage, 1.266% of the anti-glycative antioxidant composition, 0.083% of the emulsifier, 2% of the polyol, 9% of the humectant, 0.5% of the oil, 0.26% of the thickening agent, 0.17% of the pH adjuster, 0.38% of the preservative, and 86.994% of the water.

[0011] The emulsion containing the anti-glycative antioxidant composition of the foregoing comprises, by mass percentage, 2.532% of the anti-glycative antioxidant composition, 0.166% of the emulsifier, 4% of the polyol, 7% of the humectant, 1.03% of the oil, 0.26% of the thickening agent, 0.170% of the pH adjuster, 0.38% of the preservative, and 86.341% of the water.

[0012] The emulsion containing the anti-glycative antioxidant composition of the foregoing comprises, by mass percentage, 1% of astaxanthin and 99% of caprylic / capric triglyceride.

[0013] The emulsion containing the anti-glycative antioxidant composition of the foregoing comprises, by mass percentage, 35% of Bacillus Ferment, 32% of hydroxypropyl cyclodextrin, 18% of dipropylene glycol, 5-10% of glycerin, and 1-10% of naringin.

[0014] The emulsion containing the anti-glycative antioxidant composition of the foregoing comprises, by mass percentage, 2.532% of the anti-glycative antioxidant composition, 0.166% of the emulsifier, 4% of the polyol, 7% of the humectant, 1.03% of the oil, 0.26% of the thickening agent, 0.170% of the pH adjuster, 0.38% of the preservative, and 86.341% of the water.

[0015] The emulsion containing the anti-glycative antioxidant composition of the foregoing comprises, by mass percentage, 0.01-1% of hydrogenated lecithin and 0.01-1% of PEG-40 hydrogenated castor oil; the mass ratio of the hydrogenated lecithin to the PEG-40 hydrogenated castor oil is 1.51:1.

[0016] The polyol in the aforementioned emulsion containing the anti-glycation and anti-oxidation composition includes at least one of glycerol, propylene glycol, 1,3-propylene glycol, 1,3-butanediol, 1,2-hexanediol and 1,6-hexanediol; the polyol is a solvent of the product and also has a moisturizing effect; when the emulsion is applied to the skin, the polyol can absorb water from the environment to supplement the skin; and the polyol also has a certain bacteriostatic effect.

[0017] The oil in the aforementioned emulsion containing the anti-glycation and anti-oxidation composition can be derived from plants, minerals or artificial synthesis; specifically, the oil includes at least one of coco-caprylate / caprate, caprylic / capric triglyceride, pentaerythrityl tetraethylhexanoate, oat kernel oil, glyceryl triethylhexanoate, dimethicone, squalane, hydrogenated polydecene and hydrogenated polyisobutene.

[0018] The thickening agent in the aforementioned emulsion containing the anti-glycation and anti-oxidation composition includes at least one of xanthan gum, magnesium aluminum silicate, carbomer, succinoglucan and polyacrylamide; the thickening agent is used to increase the viscosity of the product, so that the product can maintain a uniform emulsion state.

[0019] The preservative in the aforementioned emulsion containing the anti-glycation and anti-oxidation composition includes at least one of nisin, lysozyme, lactic acid bacteria fermentation product, methylisothiazolinone, methylisothiazolinone, hydroxyacetophenone, phenoxyethanol, caprylhydroxamic acid and antimicrobial peptide; the preservative has a bacteriostatic effect in the product, so that the product can be stored for a longer period of time.

[0020] The pH regulator in the aforementioned emulsion containing the anti-glycation and anti-oxidation composition includes at least one of tromethamine, triethanolamine, aminomethylpropanol, potassium hydroxide, sodium hydroxide, lactic acid, inositol hexaphosphate, citric acid and malic acid; the pH regulator can balance the acidity and alkalinity of the emulsion, so that the emulsion can be more stable and the irritation to the skin is reduced.

[0021] The humectant in the aforementioned emulsion containing the anti-glycation and anti-oxidation composition includes but is not limited to β-glucan, betaine, glycerol glucoside and panthenol.

[0022] A method for preparing an emulsion containing an anti-glycation and anti-oxidation composition includes the following steps: A. The anti-glycation and anti-oxidation composition, emulsifier, polyol, humectant, oil, thickening agent, pH regulator, preservative and water are weighed according to the following mass ratio: 0.1-10%, 0.03-1%, 1-20%, 1-20%, 0.2-20%, 0.1-1%, 0-2%, 0.1-0.6% and 50-95%, respectively; the anti-glycation and anti-oxidation composition includes astaxanthin solution, ergothioneine, lavender flower extract, oleanolic acid inclusion, taurine and pyridoxamine dihydrochloride; B, add emulsifier into polyol, heat and stir, dissolve completely, form polyol solution; C, slowly drop oil ester and astaxanthin solution into polyol solution under stirring, form gel; D, mix humectant, thickening agent, water and preservative, heat to appropriate temperature, stir and disperse evenly, cool down, add PH regulator, ergothioneine, lavender flower extract, oleuropein package, taurine and pyrrolidone dihydrochloride, stir evenly, form water phase; E, pour water phase obtained in step D into gel obtained in step C, homogenize with homogenizer at 5000 rpm for 3 minutes, obtain finished product emulsion containing anti-glycation and anti-oxidation composition.

[0023] Compared with the prior art, the present application has the following beneficial effects: 1. Multi-pathway covered anti-glycation and anti-oxidation composition: astaxanthin solution, ergothioneine, lavender flower extract, oleuropein package, taurine and pyrrolidone dihydrochloride are used synergistically, which can effectively remove DPPH and reduce the generation of glycation product AGEs, and has better anti-glycation and anti-oxidation effect; 2. Optimization of preparation process: the preparation method of the present application can directly convert the particle size of the emulsion from micrometer level to nanometer level without increasing energy consumption and emulsifier consumption, so that the size of the emulsion is smaller, the system is more stable, the skin feel is better, and the emulsion is more easily absorbed on the skin, thereby improving the utilization rate of active ingredients in the emulsion; Compared with the conventional emulsification method, the present application requires less high-energy consumption steps, can realize cost reduction and efficiency improvement, and achieves the goal of energy saving and environmental protection; 3. Combination of process and ingredients to reduce production difficulty: by optimizing the combination of emulsifiers, the adaptability of the emulsification process and the formula system is greatly improved, the preparation process difficulty is reduced, the emulsifier consumption is low, the irritation is low, and it is more mild and safe; The emulsion of the present application has the advantages of good stability, good skin feel, and easier penetration and absorption, and the ingredients synergistically enhance each other, which is more economical and efficient; the preparation method can improve the utilization rate of active ingredients while reducing energy consumption, achieve the goal of energy saving and environmental protection, cost reduction and efficiency improvement, and is simple to operate and easy to realize industrial production.

[0024] Therefore, the present application has the advantages of relatively better effect, relatively lower production cost and relatively better stability. BRIEF DESCRIPTION OF DRAWINGS

[0025] Figure 1 is a graph showing the influence of each anti-glycation and anti-oxidation composition B1-B6 on the content of CML in HDF cells in experiment 1; Figure 2Figure 1 is the immunofluorescence image of the carboxymethyl lysine (CML) content of HDF cells treated with each of the anti-glycating and anti-oxidizing compositions B1-B6 in Experiment 1; Figure 3 Figure 2 is a graph of the effect of each of the anti-glycating and anti-oxidizing compositions B6-B8 on the CML content of HDF cells in Experiment 1; Figure 4 Figure 3 is the immunofluorescence image of the carboxymethyl lysine (CML) content of HDF cells treated with each of the anti-glycating and anti-oxidizing compositions B6-B8 in Experiment 1; Figure 5 Figure 4 is a graph of the results of the stability test of each of the solutions for 1 month in Experiment 1; Figure 6 Figure 5 is a microscope image (400x magnification) of the emulsion of Example 1 in Experiment 2; Figure 7 Figure 6 is a graph of the particle size distribution of the emulsion of Example 1 in Experiment 2; the average particle size is 443.3 nm; Figure 8 Figure 7 is a microscope image (400x magnification) of the emulsion of Comparative Example 1 in Experiment 2; Figure 9 Figure 8 is a graph of the particle size distribution of the emulsion of Comparative Example 1 in Experiment 2; the average particle size is 1188.1 nm; Figure 10 is a comparison of the emulsion samples in Experiment 2 (left, Example 1; right, Comparative Example 1); 10-1 is a comparison of the emulsions, and 10-2 is a comparison of the emulsions after centrifugation, which was performed at 3000 rpm for 30 min; Figure 11 Figure 11 is a graph of the results of the 1-month stability test of the emulsion of Example 1 in Experiment 2; Figure 12 Figure 12 is a graph of the results of the ergothioneine transdermal test of Example 1 and Comparative Example 1 in Experiment 2; Figure 13 Figure 13 is a microscope image (400x magnification) of the emulsion of Example 2 in Experiment 3; Figure 14 Figure 14 is a graph of the particle size distribution of the emulsion of Example 2 in Experiment 3; the average particle size is 479.0 nm; Figure 15 Figure 15 is a microscope image (400x magnification) of the emulsion of Comparative Example 2 in Experiment 3; Figure 16 Figure 16 is a graph of the particle size distribution of the emulsion of Comparative Example 2 in Experiment 3; the average particle size is 655.2 nm; Figure 17 Figure 17 is a microscope image (400x magnification) of the emulsion of Comparative Example 3 in Experiment 3; Figure 18 Figure 18 is a graph of the particle size distribution of the emulsion of Comparative Example 3 in Experiment 3; the average particle size is 731.7 nm; Figure 19is the microscope picture of the emulsion of Comparative Example 4 in Experiment 3 (400 times magnification) ; Figure 20 is the particle size distribution chart of the emulsion of Comparative Example 4 in Experiment 3; the average particle size is 1617.8 nm; Figure 21 is the microscope picture of the emulsion of Comparative Example 5 in Experiment 3 (400 times magnification) ; Figure 22 is the particle size distribution chart of the emulsion of Comparative Example 5 in Experiment 3; the average particle size is 1062 nm; Figure 23 is the particle size distribution comparison chart of each emulsion in Experiment 3; Figure 24 is the emulsion sample comparison chart in Experiment 3 (from left to right: Comparative Example 2, Comparative Example 3, Example 2, Comparative Example 4, Comparative Example 5) ; 24-1 is the emulsion comparison chart, and 24-2 is the emulsion centrifugation comparison chart; Figure 25 is the penetration test result chart of taurine in the emulsion of Example 2 in Experiment 4; Figure 26 is the penetration test result chart of taurine in the emulsion of Comparative Example 5 in Experiment 4; Figure 27 is the penetration test result chart of ergothioneine in the emulsion of Example 2 in Experiment 4; Figure 28 is the penetration test result chart of ergothioneine in the emulsion of Comparative Example 5 in Experiment 4. DETAILED DESCRIPTION

[0026] The application will be further described below in conjunction with the drawings and examples, but it is not limited to the basis of the application.

[0027] Example 1. An emulsion containing an anti-sugar and anti-oxidant composition, the preparation raw materials are as follows in the table by mass percentage.

[0028] A method for preparing an emulsion containing an anti-sugar and anti-oxidant composition, the steps are as follows: A. Add the emulsifier combination to the polyol, heat and stir until completely dissolved to form a polyol solution; B. Slowly add the oil ester (room temperature, containing astaxanthin solution in the anti-sugar and anti-oxidant) to the polyol solution under stirring to form a gel; C. Heat the humectant 2, thickening agent, water and preservative to an appropriate temperature, stir and disperse evenly, cool down, add the PH adjuster and the remaining anti-sugar and anti-oxidant, stir evenly to form an aqueous phase; D. Pour the aqueous phase into the gel, homogenize with Promix homogenizer at 5000 rpm for 3 minutes to obtain the finished emulsion.

[0029] Example 2. Preparation of an emulsion containing an anti-glycation antioxidant composition, the raw materials are as follows in percentage by mass.

[0030] A method for preparing an emulsion containing an anti-glycation antioxidant composition is the same as example 1.

[0031] Verification experiment Experiment 1. Selection of ingredients in anti-glycation antioxidant Design different combination schemes of anti-glycation antioxidant ingredients, test the anti-glycation effect of the combination by the effect of each combination on the carboxymethyl lysine (CML) content of fibroblast (HDF) cells; Test the antioxidant capacity of the combination by DPPH free radical scavenging experiment; Thus, the anti-glycation antioxidant ingredients are selected and combined in multiple pathways, and the anti-glycation antioxidant efficacy of the combination is studied and verified.

[0032] According to Figure 1 and 2 ( Figure 1 " " indicates P < 0.05, " " indicates P < 0.01, and " " indicates P < 0.001 compared with the NC group; # indicates P < 0.05, ## indicates P < 0.01, and ### indicates P < 0.001 between groups; the test sample concentration of B1-B6 in the experiment is 0.16%, Figure 2 CML is carboxymethyl lysine, DAPI is 4', 6-diamidino-2-phenylindole, and Merge is fusion) The anti-glycation test results show that compared with the blank control group (BC), the CML expression of the negative control group (NC) is significantly up-regulated, indicating that the modeling is successful; compared with the negative control group (NC), the CML content of the sample group is significantly down-regulated; At the same test concentration of 0.16%, the CML content inhibition rate of sample B1 is 52.05%, the CML content inhibition rate of sample B2 is 19.94%, the CML content inhibition rate of sample B3 is 65.73%, the CML content inhibition rate of sample B4 is 53.87%, the CML content inhibition rate of sample B5 is 44.62%, and the CML content inhibition rate of sample B6 is 71.91%; compared with sample B6, the CML content inhibition rate of sample B6 is 71.91%, and the anti-glycation effect is the best, and the P value obtained by T test is much less than 0.05, which proves that there is a significant difference between groups; this shows that the anti-glycation effect is the best when all the ingredients in B6 group exist at the same time.

[0033] Figure 3 and 4The test results show that ( Figure 3 In the diagram, "*" indicates P < 0.05, "**" indicates P < 0.01, "***" indicates P < 0.001, and "****" indicates P < 0.0001; "#" indicates inter-group comparison, "#" indicates P < 0.05, "##" indicates P < 0.01, "###" indicates P < 0.001, and "####" indicates P < 0.0001; in the experiment, the concentration of the test samples B6-B8 was 0.04%. Figure 4 (CML is carboxymethyl lysine, DAPI is 4,6-diamidino-2-phenylindole, and Merge is fusion) Compared with the negative control group, the CML content in the sample group was significantly downregulated; At the same test concentration of 0.04%, the CML content inhibition rate of sample B6 was 43.53%, that of sample B7 was 74.32%, and that of sample B8 was 53.51%. Significant differences were found among the groups, indicating that sample B7 had a significantly better anti-glycation effect than B6 and B8; this suggests that the introduction of pyridoxine dihydrochloride into group B6 can significantly improve the anti-glycation efficacy of the composition. The synergy index calculated using the Bliss independent model method was 0.0057, indicating that the synergy effect of the combined use of samples B6 and B8 (sample B7) was positive, suggesting that the combined use of samples B6 and B8 (sample B7) had a synergistic effect. The two sets of tests above show that each component in the B7 combination is indispensable, and when combined, they can exert a better anti-glycation effect.

[0034] Based on the antioxidant test results in the table above, combinations B6 and B7 have a strong inhibitory effect on DPPH free radicals. The IC50 of combination B7 is 0.13%, which is lower than that of combination B6 (0.38%). This indicates that the introduction of pyridoxine dihydrochloride significantly improves the antioxidant efficacy of the original combination B6. In addition, the IC50 of the single component of combination B8, pyridoxine dihydrochloride, against DPPH was 39.38%, indicating that its antioxidant efficacy was relatively weak. The fact that it could improve the antioxidant effect of combination 6 at the same test concentration may be because it helped stabilize the components in B6 and had a synergistic effect with other components, thereby improving the overall antioxidant effect.

[0035] Astaxanthin is a yellow substance that is very unstable under light. Figure 5 You can see ( Figure 5In the experiment, group 1 only contains astaxanthin solution, group 2 contains corresponding anti-glycation and anti-oxidation combination B6 components, and group 3 contains corresponding anti-glycation and anti-oxidation combination B7 components, and the astaxanthin solution content in the three groups is the same, which is 0.03%, and the rest of the anti-glycation and anti-oxidation components are converted according to the proportion, and the solubilizer PEG-40 hydrogenated castor oil content is the same, which is 0.1%, and the rest is water. After one month of testing, the yellow color of group 1 containing only active ingredient astaxanthin completely disappeared under light conditions, indicating that the astaxanthin in the solution was completely degraded; And groups 2 and 3 containing other anti-glycation and anti-oxidation components can still maintain yellow under light, which shows that the addition of other components in the group plays a stabilizing and protecting role on astaxanthin; From the light condition, the color of group 2 deepens, indicating that other components may also have certain discoloration instability under light, and the color change of group 3 is relatively shallow, which shows that the addition of pyridoxamine dihydrochloride can also inhibit the discoloration phenomenon of other active components in group 2, further indicating the mutual protection effect between the components of combination B7.

[0036] The above results show that each component in the selected combination B7 is indispensable, and only when they coexist can they play a better effect; This is because the components in the B7 composition complement each other, especially the introduction of pyridoxamine dihydrochloride, which plays a synergistic effect, significantly improving the anti-glycation and anti-oxidation efficacy and stability of the composition; The B7 group in the present application adopts specific ratio of anti-oxidation and anti-glycation components, including: astaxanthin solution, ergothioneine, lavender flower extract, naringin coating, taurine, pyridoxamine dihydrochloride; Astaxanthin is a natural antioxidant that can neutralize active oxygen, especially singlet oxygen induced by ultraviolet light, and can absorb ultraviolet light, reduce UV-induced MMP-1 activity and expression, prevent collagen degradation, and inhibit the release of inflammatory mediators and the activation of inflammatory signaling pathways, and reduce inflammation; Ergothioneine is a naturally occurring sulfur-containing amino acid derivative that can enter cells and mitochondria, scavenge active oxygen free radicals, protect mitochondria from oxidative damage, and up-regulate antioxidant enzyme activity in cells, maintain redox balance in cells, effectively reduce the formation of fine lines, and also resist inflammation; Taurine can scavenge free radicals produced by polycyclic aromatic hydrocarbons and has a protective effect on fibroblast damage caused by polycyclic aromatic hydrocarbons. At the same time, taurine can inhibit protein carbonylation and reduce the formation of advanced glycation end products (AGES), thereby delaying the glycation process of the skin; Lavender flower extract can achieve anti-wrinkle and firming effects by improving tissue morphology, inhibiting the content of AGES, carbonyl products, mitochondrial active oxygen, ROS, TXNIP, and lipofuscin; Naringin has strong free radical scavenging and antioxidant capacity, and can inhibit the binding of AGEs and RAGE receptor by forming competition with the molecules causing glycosylation to occupy the site, thereby achieving the purpose of anti-glycation; Pyridoxamine dihydrochloride is a form of vitamin B6, which is almost non-toxic to the human body and safe to use. The vitamin B6 currently used in the cosmetic industry is in the form of pyridoxine hydrochloride, which has not been reported to have anti-glycation and antioxidant effects. Pyridoxamine, as another form of vitamin B6, has been reported to have a small amount of intervention effect on the early reaction of non-enzymatic glycosylation. The conversion of pyridoxamine to pyridoxamine dihydrochloride by hydrochlorination can improve the water solubility of the raw material, making it easier to be applied in water-soluble formulations. At the same time, the cost of the raw material after hydrochlorination is greatly reduced, and the activity of the raw material remains basically unchanged, thereby achieving the purpose of cost reduction. At present, pyridoxamine dihydrochloride is rarely used in the cosmetic field. The six synergistic compounds cover multiple anti-glycation and antioxidant targets, can remove free radicals and inhibit the glycosylation process from all directions, and can more effectively play the anti-glycation and antioxidant effects.

[0037] Experiment 2 Optimization of preparation process Different addition process schemes of each component in the preparation process of anti-glycation and antioxidant emulsion were designed, and the performance changes of the product were tested. The emulsion particle size changes were tested by microscope shooting and laser particle size analyzer. The sample stability changes were tested by centrifugal test and accelerated stability test. The permeability changes of the active ingredients of the emulsion in different processes were tested by pig skin permeation experiment. The preparation process of the anti-glycation and antioxidant emulsion was optimized, and the influence of the preparation process on the emulsion was studied and verified.

[0038] Comparative Example 1 The ingredient ratio and example 1 are the same, and the difference lies in the preparation method.

[0039] Comparative Example 1 adopts the conventional preparation method, which includes the following steps: A. Heat the emulsifier hydrogenated lecithin, humectant 1, humectant 2, thickening agent, water and preservative to an appropriate temperature, stir and disperse uniformly to form an aqueous phase; B. Disperse the emulsifier PEG-40 hydrogenated castor oil in the oil phase, stir uniformly at room temperature to form an oil phase; C. Add the oil phase to the aqueous phase, and homogenize it with a Promix homogenizer at 5000 rpm for 3 minutes; D. Cool to room temperature, add PH adjuster and anti-glycation and antioxidant agent, and homogenize it with a Promix homogenizer at 4000 rpm for 3 minutes to obtain the emulsion 2 of comparative example 1.

[0040] Compared with the traditional preparation process (dissolving and dispersing the emulsifier in the water phase or the oil phase, and then adding the oil phase into the water phase to obtain the emulsion by high-speed homogenization emulsification), the preparation process provided by the application is to add the emulsifier into the polyol to form a solution, then add the oil phase into the polyol solution to form a gel, and finally add the water phase to emulsify to obtain the emulsion. By Figure 6-1 It can be seen that the emulsion prepared by the special process (the preparation process of the application) is whiter in appearance than the emulsion prepared by the conventional emulsification, which is due to the smaller particle size of the emulsion of Example 1. The test results show that the average particle size of the emulsion of Example 1 is only 443.3 nm. Due to the precision problem of the microscope, the nanoscale emulsion droplets cannot be clearly imaged, but under the shooting magnified by 400 times, it can be seen that the particle size distribution of the emulsion is very uniform. Correspondingly, the average particle size of the emulsion 2 prepared by the conventional emulsification process is 1188.1 nm, and the particle size is very uneven under the microscope shooting. From the appearance diagram, the product is also more transparent and the color is deeper, which may be due to the fact that astaxanthin is not completely wrapped. At the same time, there will be oil flower phenomenon on the surface of the emulsion 2. The centrifugal stability test results show that the emulsion prepared by the conventional emulsification method is not stable under centrifugal force, and obvious separation and oiling phenomenon will occur, while the emulsion prepared by the special process can pass the centrifugal test. As Figure 11 In the 1-month accelerated stability test, Example 1 also showed excellent stability test results and was very stable at various temperatures.

[0041] The above results fully show that by optimizing the process, the particle size of the anti-sugar and anti-oxidation emulsion can be greatly reduced, and the product is more uniform and stable. By comparing the specific operation steps of the two processes, it can be found that the special preparation process provided by the application requires less energy consumption for heating and high-speed homogenization, so the process is more energy-saving and environmentally friendly, thereby achieving the purpose of reducing cost and increasing efficiency. The reason why the process can prepare products with fine particle size and good stability is that by selecting a suitable emulsification system, almost no additional energy input is needed, and the emulsion with small particle size and good stability can be prepared under low energy consumption.

[0042] The emulsion prepared by the process also has excellent skin-friendly penetration effect, can carry more active ingredients, has higher utilization of active ingredients, and has better skin feel. The following tests are compared.

[0043] The emulsions in Example 1 and Comparative Example 1 were subjected to penetration comparison test, and pigskin penetration test was carried out by using ergothioneine as a marker. The results are as follows Figure 12 and the following table, From the above test results, it can be seen that the permeability of ergothioneine in the two emulsions gradually increases with the extension of time, and the permeability of ergothioneine in Example 1 is obviously stronger than that in Comparative Example 1; At the time of experiment 1h, the difference between the two is 0.06%, at which time there is already a difference but it is not particularly obvious; with the extension of test time, the difference between the two gradually increases, at 8h, the difference increases to 1.29%, and the residual amount in the skin is also more in Example 1; In combination with the difference between the two emulsions, it is fully illustrated that when the particle size of the emulsion is smaller, the active ingredient therein is more easily penetrated into the deep layer of the skin to play the efficacy, so under the condition of the same active ingredient addition amount, the product is more economical and efficient, so as to realize the goal of cost reduction and efficiency increase.

[0044] Experiment 3 System emulsifier and proportion optimization The sample emulsions of Example 2 and Comparative Examples 2-4 are prepared by a special preparation process (the preparation method of Example 1), and the sample emulsion of Comparative Example 5 is prepared by a conventional preparation process (the preparation method of Comparative Example 1); The emulsion particle size change is tested by microscope shooting and laser particle size instrument; The sample stability change is tested by centrifugation; The emulsifier and proportion in the anti-sugar and anti-oxidation emulsion formula are optimized.

[0045] Comparative Example 2: The ingredients are The preparation method adopts a special preparation process (the preparation method of Example 1).

[0046] Comparative Example 3: The ingredients are The preparation method adopts a special preparation process (the preparation method of Example 1).

[0047] Comparative Example 4: The ingredients are The preparation method adopts a special preparation process (the preparation method of Example 1).

[0048] Comparative Example 5: The ingredients are The preparation method adopts a conventional preparation process (the preparation method of Comparative Example 1).

[0049] From the above test results, it can be seen that under the same special preparation process, different emulsifiers and emulsifier combination ratio have a greater influence on the particle size of the emulsion; As Figure 13-2 4, it can be seen that in various emulsifier combinations, the emulsion particle size in Example 2 is the smallest, 479 nm, and the distribution is the most uniform, and the appearance is also whiter as shown in the figure; compared with the emulsion of 443 nm in Example 1, the particle size is slightly increased, but the difference is not significant; This shows that the emulsification system has universality, and the decrease of the content of sugar antioxidant, oil and emulsifier has no obvious influence on the emulsion particle size. As long as the proportion of the oil phase, the emulsifier phase and the polyol phase is consistent, the corresponding nano-sized emulsion can be prepared.

[0050] The emulsion particle sizes in Comparative Example 2 and Comparative Example 4 are 655.2 nm and 1617.8 nm respectively, and the particle size distribution is not uniform; this shows that when a single hydrogenated lecithin or PEG-40 hydrogenated castor oil is used as an emulsifier, the special preparation process of the present application cannot be well completed; Especially when PEG-40 hydrogenated castor oil is used alone, the emulsion particle size is larger than 1062 nm of the emulsion prepared by the conventional process in Comparative Example 5, and the emulsification system is unstable, and obvious oil floating phenomenon occurs, and the stratification is more serious after centrifugation; This shows that the presence of hydrogenated lecithin in the system plays a crucial role in the implementation of the preparation process of the present application.

[0051] The emulsion particle size in Comparative Example 3 is 731.7 nm, which is much higher than the emulsion particle size of 479 nm in Example 2, which shows that when the ratio of hydrogenated lecithin to PEG-40 hydrogenated castor oil is 1:1, the emulsification effect is not as good as that when the ratio is 1.5:1.

[0052] In the case, 1.5:1 is the optimal ratio of hydrogenated lecithin to PEG-40 hydrogenated castor oil, the emulsification effect is the best, the obtained emulsion particle size is the smallest, and the product is the most uniform; This is because the content of phosphatidylcholine (PC) in the hydrogenated lecithin in the experiment is >70%, PC itself is a zwitterion (choline is positively charged, and phosphate group is negatively charged), which has strong emulsification capacity; the polar-nonpolar structure of the hydrogenated lecithin molecule can be anchored at the water-oil interface to form a stable film to wrap the droplets; PEG-40 hydrogenated castor oil is a non-ionic surfactant, and the HLB value is higher than that of hydrogenated lecithin, about 14-16, which has stronger emulsification capacity; Through suitable proportioning, the two can reduce the difficulty of forming nano-emulsion by emulsifier, therefore, the formulation can be adjusted in a wider range, the operation is easier, and after water phase emulsification, the interface film of oil and water phases is more firm; Therefore, the emulsifier combination of the present application is preferably hydrogenated lecithin: PEG-40 hydrogenated castor oil in a ratio of 1.5:1.

[0053] Experiment 4 Human penetration test In order to further prove the penetration advantage of the emulsion in the present application, the corresponding emulsions in Example 2 and Comparative Example 5 were subjected to human Raman penetration test.

[0054] The human penetration test was carried out with taurine and ergothioneine as markers, and the results are shown in the table. Figure 25-28

[0055] From the experimental results, the penetration rates of taurine in Example 2 at 0h, 1h, 2h, 4h were 0%, 3.15%, 8.14%, 10.89% respectively; In Comparative Example 5, the corresponding data were 0%, 2.89%, 5.28%, 8.73% respectively; This shows that there is no taurine in the measured skin to exclude interference, and as the sample is used, the penetration of taurine gradually increases, and at 6h, it can penetrate into the dermis, and at each test time point, the penetration of Example 2 is stronger than that of Comparative Example 5; Combined with the particle size test data of the previous samples, it shows that the smaller the particle size, the stronger the penetration of taurine on human skin.

[0056] Similarly, for ergothioneine, the penetration rates of Example 2 at 0h, 1h, 2h, 4h were 0%, 3.74%, 6.11%, 7.32% respectively; In Comparative Example 5, the corresponding data were 0%, 1.99%, 2.87%, 5.01% respectively; This shows that ergothioneine also penetrates more strongly because the particle size of the emulsion is smaller.

[0057] Combining the two, it shows that the decrease in the particle size of the emulsion can promote the penetration and absorption of active ingredients on human skin, thereby achieving high efficiency and economic effect; this further proves the important role of the special preparation process in the present application.​

Claims

1. An emulsion containing an anti-glycation and antioxidant composition, characterized in that: It comprises 0.1-10% by weight of an anti-glycation and antioxidant composition, 0.03-1% of an emulsifier, 1-20% of a polyol, 1-20% of a moisturizer, 0.2-20% of an oil, 0.1-1% of a thickener, 0-2% of a pH adjuster, 0.1-0.6% of a preservative, and 50-95% of water; the anti-glycation and antioxidant composition includes astaxanthin solution, ergothioneine, lavender flower extract, oleuropein encapsulation, thiotaurine, and pyridoxine dihydrochloride.

2. The emulsion containing an anti-glycation and antioxidant composition according to claim 1, characterized in that: It includes 2.532% by weight of anti-glycation and antioxidant composition, 0.166% emulsifier, 4% polyol, 7% humectant, 1.03% oil, 0.26% thickener, 0.170% pH adjuster, 0.38% preservative and 86.341% water.

3. The emulsion containing an anti-glycation and antioxidant composition according to claim 1, characterized in that: It comprises 1.266% by weight of anti-glycation and antioxidant composition, 0.083% emulsifier, 2% polyol, 9% humectant, 0.5% oil, 0.26% thickener, 0.17% pH adjuster, 0.38% preservative and 86.994% water.

4. The emulsion containing an anti-glycation and antioxidant composition according to claim 1, characterized in that: The mass ratio of the astaxanthin solution, ergothioneine, lavender flower extract, oleuropein encapsulation, thiotaurine, and pyridoxine dihydrochloride is 0.32:1:20:2:1:

1.

5. The emulsion containing an anti-glycation and antioxidant composition according to claim 1, characterized in that: The astaxanthin solution comprises 1% astaxanthin and 99% caprylic / capric triglycerides by mass percentage.

6. The emulsion containing an anti-glycation and antioxidant composition according to claim 1, characterized in that: The naringin encapsulation comprises 35% by weight of Bacillus fermentation product, 32% by weight of hydroxypropyl cyclodextrin, 18% by weight of dipropylene glycol, 5-10% by weight of glycerol, and 1-10% by weight of naringin.

7. An emulsion containing an anti-glycation and antioxidant composition according to claim 1, characterized in that: The emulsifier comprises at least one or more ionic surface emulsifiers and one or more nonionic surfactants with an HLB value ≥12; the ionic surfactants include, but are not limited to, hydrogenated lecithin, glyceryl stearate citrate, cetyl phosphate potassium, and sodium stearoyl glutamate; the nonionic surfactants include, but are not limited to, PEG-40 hydrogenated castor oil, polyglycerol-3-methylglucose distearate, and PEG-100 stearate.

8. An emulsion containing an anti-glycation and antioxidant composition according to claim 7, characterized in that: The emulsifier comprises 0.01-1% hydrogenated lecithin and 0.01-1% PEG-40 hydrogenated castor oil by mass percentage; the mass ratio of hydrogenated lecithin to PEG-40 hydrogenated castor oil is 1.51:

1.

9. A method for preparing an emulsion containing an anti-glycation and antioxidant composition according to any one of claims 1-8, characterized in that, Includes the following steps: A. Weigh out the following components according to the corresponding mass ratio: 0.1-10% anti-glycation and antioxidant composition, 0.03-1% emulsifier, 1-20% polyol, 1-20% moisturizer, 0.2-20% oil, 0.1-1% thickener, 0-2% pH adjuster, 0.1-0.6% preservative, and 50-95% water; the anti-glycation and antioxidant composition includes astaxanthin solution, ergothioneine, lavender flower extract, oleuropein encapsulation, thiotaurine, and pyridoxine dihydrochloride; B. Add the emulsifier to the polyol, heat and stir until completely dissolved to form a polyol solution; C. While stirring, slowly drip oil ester and astaxanthin solution into polyol solution to form a gel; D. Mix the humectant, thickener, water and preservative, heat to a suitable temperature, stir and disperse evenly, cool down, add pH adjuster, ergothioneine, lavender flower extract, oleuropein encapsulation, thiotaurine and pyridoxine dihydrochloride, stir evenly to form an aqueous phase. E. Pour the aqueous phase obtained in step D into the gel obtained in step C, and homogenize it at 5000 rpm for 3 minutes to obtain the finished emulsion containing the anti-glycation and antioxidant composition.

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