A method for preparing bis-tocopheryl azelate and its use

Abstract

The application discloses a preparation method of bis-tocopheryl azelate and application thereof, and belongs to the technical field of compound synthesis. The application provides a preparation method of bis-tocopheryl azelate, and the yield and purity of bis-tocopheryl azelate are improved. The bis-tocopheryl azelate prepared by the application overcomes the limitations of poor permeability and high irritability of azelaic acid, and can also improve the overall efficacy through synergistic effect, so that a more optimal solution is provided for skin care and treatment.

Description

Technical Field

[0001] This invention relates to a method for preparing bis(tocopherol) azelaate and its application, belonging to the field of compound synthesis technology. Background Technology

[0002] Azelaic acid is a naturally occurring dicarboxylic acid widely used in skin care, pharmaceuticals, and industrial applications. In dermatology, azelaic acid is used to treat skin problems such as acne, rosacea, and pigmentation due to its anti-inflammatory, antibacterial, and keratin-regulating properties. It can inhibit the growth of Propionibacterium acnes and reduce sebum oxidative damage, thereby improving inflammatory skin conditions. Furthermore, azelaic acid also has a whitening effect by inhibiting tyrosinase activity to reduce melanin synthesis, and is therefore used to treat pigmentation disorders. Beyond skin care, azelaic acid also has applications in plastics, lubricants, and chemical synthesis, serving as a plasticizer or lubricant for polymer materials, improving their flexibility and stability.

[0003] Despite its promising applications in various fields, azelaic acid also faces certain limitations and challenges. Firstly, its poor water and oil solubility restricts its use in water-based systems, making formulation design more difficult. In skin applications, azelaic acid's limited permeability leads to low bioavailability, requiring specific carriers or formulation technologies to improve transdermal absorption. Furthermore, high concentrations of azelaic acid can cause skin irritation, particularly in individuals with sensitive skin, potentially leading to redness, stinging, and other adverse reactions. Therefore, careful control of its concentration and formulation methods is crucial during formulation development. In industrial applications, the relatively high production cost of azelaic acid, coupled with the complex synthesis of some of its derivatives, limits its further promotion and application.

[0004] To address the limitations of azelaic acid, researchers have developed various derivatives to improve its functional properties and application adaptability. Tocopherol, also known as vitamin E, is a powerful antioxidant that neutralizes free radicals and reduces oxidative stress damage. In the cosmetics and pharmaceutical fields, tocopherol is widely used for anti-aging and skin barrier repair.

[0005] Therefore, the preparation of azelaic acid compounds based on azelaic acid and tocopherol, further optimization of its preparation process, improvement of production efficiency, and expansion of its application in the pharmaceutical and industrial fields, in order to better leverage its comprehensive advantages, has extremely high practical and economic value. Summary of the Invention

[0006] To address the aforementioned problems, this invention provides a method for preparing bis(tocopherol) azelaate, which improves the yield and purity of bis(tocopherol) azelaate. The bis(tocopherol) azelaate prepared by this invention overcomes the limitations of azelaic acid, such as poor permeability and high irritation, and may also enhance its overall efficacy through synergistic effects, providing a better solution for skin care and treatment.

[0007] The first objective of this invention is to provide a method for synthesizing bis(tocopherol) azelaate, comprising the steps of:

[0008] (1) Mix tocopherol, DCM and DMAP, and slowly add TEA to obtain mixture 1; mix azeloyl chloride and DCM to obtain mixture 2, and slowly add mixture 2 to mixture 1 to react;

[0009] The molar ratio of tocopherol, azelaic chloride, TEA and DMAP is 1:0.2-5:0.5-10:0.01-3, and it is dissolved in DCM (the ratio of tocopherol to DCM is 1g:8mL).

[0010] (2) After the reaction is completed, water is added to quench the liquid, and after stirring, methanol is added for extraction and separation. The lower liquid is added to quench the liquid, and after stirring, methanol is added for extraction and separation. The lower liquid is dried, filtered, and concentrated using anhydrous sodium sulfate to obtain a concentrate. The concentrate is dissolved in n-hexane-DCM solution, filtered using thin-layer silica gel, washed with n-hexane, and the filtrate is concentrated and dried to obtain ditocopherol azelate.

[0011] In one embodiment, the molar ratio of tocopherol, azelaic chloride, TEA and DMAP in step (1) is 1:1 to 5:0.5 to 5:0.01 to 1;

[0012] Optionally, in step (1), the molar ratio of tocopherol, azelaic chloride, TEA and DMAP is 1:1 to 3:1 to 3:0.1 to 0.5.

[0013] In one embodiment, in step (1), the mixture 2 is added to the mixture 1 at a dropping rate of 2 to 50 L / h.

[0014] Optionally, in step (1), the mixture 2 is added to the mixture 1 at a dropping rate of 2 to 5 L / h.

[0015] In one embodiment, the reaction in step (1) is carried out at 30-70°C for 3-6 hours.

[0016] In one embodiment, the ratio of n-hexane to DCM in the n-hexane-DCM solution in step (2) is 10 to 20:1.

[0017] In one embodiment, the filtration in step (2) is performed using a thin layer of silica gel with a mesh size of 300 to 400.

[0018] A second objective of this invention is to provide the application of bis(tocopherol) azelaate in the preparation of cosmetics, wherein the structural formula of bis(tocopherol) azelaate is shown in Formula I.

[0019]

[0020] The above chemical formula is systematically named 9-oxo-9-{[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2H-chromen-6-yl]oxy}nonanoic acid-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2H-chromen-6-yl ester; 2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2H-chromen-6-yl9-oxo-9-{[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2H-chromen-6-yl]oxy}nonanoate.

[0021] In one embodiment, the cosmetic includes serum, essence water, spray, skin care foam, lotion, and shampoo.

[0022] A third object of the present invention is to provide a cosmetic containing bis(tocopherol) azelaate.

[0023] The chemical structural formula of bis(tocopherol) azelaate is shown in Formula I.

[0024]

[0025] In one embodiment, the cosmetic includes serum, essence water, spray, skin care foam, lotion, and shampoo.

[0026] The fourth objective of this invention is to provide a method for improving the properties of azelaic acid by preparing bis(tocopherol) azelaic acid ester from azelaic acid and tocopherol.

[0027] The chemical structural formula of bis(tocopherol) azelaate is shown in Formula I.

[0028]

[0029] Beneficial effects of the present invention

[0030] This invention provides a method for preparing bis(tocopherol) azelaate, which improves the yield and purity of bis(tocopherol) azelaate. The bis(tocopherol) azelaate prepared by this invention overcomes the limitations of azelaic acid, such as poor permeability and high irritation, and may also enhance its overall efficacy through synergistic effects, providing a better solution for skin care and treatment. Specifically,

[0031] (1) The purity of the tocopherol azelate prepared in this application reaches more than 97.13%, and can reach up to 97.95%;

[0032] (2) The tocopherol azelate prepared in this application has lower cell irritation than azelaic acid, and it is also non-cytotoxic when the concentration reaches 250 μg / mL (the cell viability of azelaic acid is only 67.71% when the concentration reaches 130 μg / mL).

[0033] (3) The tocopherol azelaic acid and tocopherol prepared in this application have a stronger inhibitory effect on cell adipogenesis. When the concentration is 30-60 μg / mL, it is significantly better than azelaic acid, tocopherol and isotretinoin.

[0034] (4) The bis(tocopherol) azelaic acid ester prepared in this application has stronger antioxidant properties, and its IC50... 50 Only 10 μg / mL;

[0035] (5) The bis(tocopherol) azelaate prepared in this application has a higher solubility (w / w) in dibutyl adipate, reaching 10%, which is significantly better than azelaic acid at 0.1%. Attached Figure Description

[0036] Figure 1 The 1H NMR spectrum of bis(tocopherol) azelaate;

[0037] Figure 2 This is the carbon spectrum of ditocopherol azelate. Detailed Implementation

[0038] The preferred embodiments of the present invention are described below. It should be understood that the embodiments are for better explanation of the present invention and are not intended to limit the present invention.

[0039] Raw materials used in the examples:

[0040] Azelaic acid was purchased from Shandong Aigelin Pharmaceutical Co., Ltd.

[0041] Thionyl chloride was purchased from Shanghai Baishun Biotechnology Co., Ltd.

[0042] Tocopherol was purchased from Zhejiang Weishi Biotechnology Co., Ltd.

[0043] DMF (N,N-dimethylformamide) was purchased from Shanghai Chutai Chemical Technology Co., Ltd.

[0044] DCM (dichloromethane) was purchased from Shanghai Chutai Chemical Technology Co., Ltd.

[0045] DMAP (4-dimethylaminopyridine) was purchased from Jiangsu Haosheng Chemical Co., Ltd.

[0046] TEA (triethylamine) was purchased from Shanghai Chutai Chemical Technology Co., Ltd.

[0047] Test method:

[0048] High performance liquid chromatography, hydrogen nuclear magnetic resonance (HMR) spectroscopy, and carbon nuclear magnetic resonance (CMR) spectroscopy.

[0049] Example 1: A method for preparing bis(tocopherol) azelaate

[0050] 1. Preparation of azelaic chloride

[0051] Azelaic acid, toluene, and DMF were added to the reaction flask according to the proportions in Table 1, and stirred at room temperature for 30 min. Thionyl chloride was slowly added, and the reaction was carried out at 50 °C for 6 hours. After the reaction was completed, the system was concentrated to dryness as much as possible and packaged to obtain azeloyl chloride.

[0052] Table 1

[0053] Substrate MW Feeding amount eq azelaic acid 188.22 g / mol 200g 1.0eq thionyl chloride 118.97 g / mol 568.81g 4.5eq Toluene 600g 3w / w DMF 6g 0.03w / w

[0054] 2. Preparation of bis(tocopherol) azelaate

[0055] Add tocopherol, DCM (6 vol), and DMAP according to the proportions in Table 2, start stirring, and add TEA while controlling the temperature below 5℃ to obtain mixture 1; prepare a mixture of azeloyl chloride and DCM (2 vol) according to Table 2 to obtain mixture 2; add mixture 2 dropwise to mixture 1 at a uniform rate over 10 minutes, and after the addition is complete, raise the temperature to 30-35℃ and react for 7 hours (quench with methanol on TLC: use PE:EA = 10:1 as the developing solvent, and observe the color development of phosphomolybdic acid at the same time);

[0056] After the reaction was complete, 5 w / w (1000 g) of water was added to quench the reaction. After stirring for 30 minutes, 1 w / w (200 g) of methanol was added, and the mixture was extracted and separated. The lower layer was washed a second time with 5 w / w (1000 g) of water and 2 w / w (200 g) of methanol. After separation, the lower layer was dried with anhydrous sodium sulfate, filtered, and concentrated. The concentrate was dissolved in 4 w / w (800 g) of n-hexane-DCM at a volume ratio of 15:1, filtered through a 300-400 mesh thin-layer silica gel filter, washed with n-hexane, and the filtrate was concentrated and dried. The solvent was removed by vacuum pumping. 221 g of bis(tocopherol) azelaic acid ester (m / z 1013.85) with a purity of 97.95% was obtained.

[0057] Table 2

[0058] Substrate MW Feeding amount eq Tocopherol 430.69 g / mol 200g 1.0eq Azelaic chloride 225.11 g / mol 188.16g 1.8eq TEA 101.19 g / mol 94g 2.0eq DMAP 122.17 g / mol 11.35g 0.2eq DCM 1200mL + 400mL 6vol+2vol

[0059] Example 2: A method for preparing bis(tocopherol) azelaate

[0060] Based on Example 1, step 2 is modified as follows:

[0061] Add tocopherol, DCM (6 vol), and DMAP according to the proportions in Table 2, start stirring, and add TEA while controlling the temperature below 10℃ to obtain mixture 1; prepare a mixture of azeloyl chloride and DCM (2 vol) to obtain mixture 2; add mixture 2 dropwise to mixture 1 at a uniform rate over 10 minutes, and after the addition is complete, raise the temperature to 25-30℃ and react for 8 hours (quench with methanol on TLC: use PE:EA = 10:1 as the developing solvent, and observe the color development of phosphomolybdic acid at the same time);

[0062] After the reaction was complete, 1000 g of water (5 w / w) was added to quench the reaction. After stirring for 30 minutes, 200 g of methanol (1 w / w) was added, and the mixture was extracted and separated. The lower layer was washed a second time with 1000 g of water (5 w / w) and 200 g of methanol (1 w / w). After separation, the lower layer was dried over anhydrous sodium sulfate, filtered, and concentrated. The concentrate was dissolved in 800 g of n-hexane:DCM in a 20:1 ratio (4 w / w). The solution was filtered through a 300-400 mesh silica gel filter, washed with n-hexane, and the filtrate was concentrated and dried. The solvent was removed by vacuum pumping. 217 g of bis(tocopherol) azelaic acid ester was obtained with a purity of 97.46%.

[0063] Example 3: A method for preparing bis(tocopherol) azelaate

[0064] Based on Example 1, step 2 is modified as follows:

[0065] Add tocopherol, DCM (6 vol), and DMAP according to the proportions in Table 2, start stirring, and add TEA while controlling the temperature below 10℃ to obtain mixture 1; prepare a mixture of azeloyl chloride and DCM (2 vol) to obtain mixture 2; add mixture 2 dropwise to mixture 1 at a uniform rate over 10 minutes, and after the addition is complete, raise the temperature to 35-40℃ and react for 5-6 hours (quench with methanol on TLC: use PE:EA = 10:1 as the developing solvent, and observe the color development of phosphomolybdic acid at the same time);

[0066] After the reaction was complete, 1000 g of water (5 w / w) was added to quench the reaction. After stirring for 30 minutes, 200 g of methanol (1 w / w) was added, and the mixture was extracted and separated. The lower layer was washed a second time with 1000 g of water (5 w / w) and 200 g of methanol (1 w / w). After separation, the lower layer was dried over anhydrous sodium sulfate, filtered, and concentrated. The concentrate was dissolved in 800 g of n-hexane:DCM in a 20:1 ratio (4 w / w). The solution was filtered through a 300-400 mesh silica gel filter, washed with n-hexane, and the filtrate was concentrated and dried. The solvent was removed by vacuum pumping. 187 g of bis(tocopherol) azelaic acid ester was obtained with a purity of 97.13%.

[0067] Example 4: A method for preparing bis(tocopherol) azelaate

[0068] Based on Example 1, step 2 is modified as follows:

[0069] Add tocopherol, DCM (6 vol), and DMAP according to the proportions in Table 2, start stirring, and add TEA while controlling the temperature below 5℃ to obtain mixture 1; prepare a mixture of azeloyl chloride and DCM (2 vol) to obtain mixture 2; add mixture 2 dropwise to mixture 1 at a uniform rate over 30 seconds, and after the addition is complete, raise the temperature to 25-35℃ and react for 5-6 hours (quench with methanol on TLC: use PE:EA = 10:1 as the developing solvent, and observe the color development of phosphomolybdic acid at the same time);

[0070] After the reaction was complete, 1000 g of water (5 w / w) was added to quench the reaction. After stirring for 30 minutes, 200 g of methanol (1 w / w) was added, and the mixture was extracted and separated. The lower layer was washed a second time with 1000 g of water (5 w / w) and 200 g of methanol (1 w / w). After separation, the lower layer was dried over anhydrous sodium sulfate, filtered, and concentrated. The concentrate was dissolved in 800 g of n-hexane:DCM in a 20:1 ratio (4 w / w). The solution was filtered through a 300-400 mesh silica gel filter, washed with n-hexane, and the filtrate was concentrated and dried. The solvent was removed by vacuum pumping. 178 g of bis(tocopherol) azelaic acid ester was obtained with a purity of 96.96%.

[0071] Example 5: A method for preparing bis(tocopherol) azelaate

[0072] Based on Example 1, step 2 is modified as follows:

[0073] Add tocopherol, DCM (6 vol), and DMAP according to the proportions in Table 2, start stirring, and add TEA while controlling the temperature below 5℃ to obtain mixture 1; prepare a mixture of azeloyl chloride and DCM (2 vol) to obtain mixture 2; add mixture 2 dropwise to mixture 1, and after the addition is complete, raise the temperature to 25-35℃ and react for 5-6 hours (quench with methanol on TLC: use PE:EA = 10:1 as the developing solvent, and observe the color development of phosphomolybdic acid at the same time);

[0074] After the reaction was complete, 1000 g of water (5 w / w) was added to quench the reaction. After stirring for 30 minutes, 200 g of methanol (1 w / w) was added, and the mixture was extracted and separated. The lower layer was washed a second time with 1000 g of water (5 w / w) and 200 g of methanol (1 w / w). After separation, the lower layer was dried with anhydrous sodium sulfate, filtered, and concentrated. The concentrate was dissolved in 800 g of n-hexane:DCM in a 10:1 ratio (4 w / w). The solution was filtered through a 300-400 mesh silica gel filter, washed with n-hexane, and the filtrate was concentrated and dried. The solvent was removed by vacuum pumping. 221 g of bis(tocopherol) azelaic acid ester was obtained. TLC showed a small amount of impurities, and the purity was 95.43%.

[0075] Example 6: A method for preparing bis(tocopherol) azelaate

[0076] Based on Example 1, step 2 is modified as follows:

[0077] Add tocopherol, DCM (6 vol), and DMAP according to the proportions in Table 2, start stirring, and add TEA while controlling the temperature below 5℃ to obtain mixture 1; prepare a mixture of azeloyl chloride and DCM (2 vol) to obtain mixture 2; add mixture 2 dropwise to mixture 1, and after the addition is complete, raise the temperature to 25-35℃ and react for 5-6 hours (quench with methanol on TLC: use PE:EA = 10:1 as the developing solvent, and observe the color development of phosphomolybdic acid at the same time);

[0078] After the reaction was complete, 5 w / w (1000 g) of water was added to quench the reaction, and the mixture was stirred for 30 minutes before separation. The lower layer was washed a second time with 5 w / w (1000 g) of water, and after separation, the lower layer was dried with anhydrous sodium sulfate, filtered, and concentrated. The concentrate was dissolved in a solvent with a hexane:DCM ratio of 20:1 (4 w / w (800 g)), filtered through a 300-400 mesh silica gel filter, washed with hexane, and the filtrate was concentrated, dried, and the solvent was removed by vacuum pumping. 205 g of bis(tocopherol) azelaic acid ester was obtained. TLC showed a small amount of impurities, and the purity was 95.17%. Comparative Example 1: Preparation of azelaic acid compounds using other substances.

[0079] Based on Example 1, p-methoxyphenol was used to replace tocopherol, and the remaining steps were the same as in Example 1 to prepare azelaic acid-methoxyphenol diester.

[0080] Example 7: Performance testing of bis(tocopherol) azelaate

[0081] The performance test results of the bis(tocopherol) azelaate prepared in Examples 1-6 and the azelaic acid-methoxyphenol diester prepared in Comparative Example 1 are as follows:

[0082] 1. Structural data

[0083] (1) 1H NMR

[0084] The 1H NMR spectrum of bis(tocopherol) azelate is as follows: Figure 1 As shown, the details are as follows:

[0085] 1 H NMR(400MHz,Chloroform-d)δ2.59(q,J=7.1,6.6Hz,8H),2.08(s,6H),2.01(s,6H),1.96(s,6H),1.82(d,J=6.8Hz, 4H),1.76(dd,J=14.2,7.1Hz,4H),1.59–1.44(m,8H),1.39(m,4H),1.32–1.20(m,19H),1.10(m,8H),0.85(m,24H).

[0086] (2) 13C NMR

[0087] The carbon-13 NMR results of bis(tocopherol) azelate are as follows: Figure 2 As shown, the details are as follows:

[0088] 13 C NMR(101MHz,Chloroform-d)δ172.38,149.39,140.52,126.72,124.94,123.06,117.40,75.08,39.44,37.61,37.52,37.47,37.42,37.35,34.17,32 .85,32.77,31.12,29.23,29.04,28.05,25.17,24.89,24.52,22.80,22.7 1,21.11,20.67,19.82,19.76,19.73,19.70,19.67,13.06,12.21,11.91.

[0089] 2. Performance Data

[0090] (1) Irritation to cells

[0091] The steps for detecting the effect of compounds on cell activity include:

[0092] 1) Cell seeding:

[0093] Press 1×10 4 SZ95 cells were seeded into 96-well plates at a seeding density of cells / well and incubated overnight in an incubator (37°C, 5% CO2).

[0094] 2) Experimental Groups:

[0095] The experiment included a blank control group, a positive control group (10% DMSO), and a sample group. In the sample group, each sample was set up with 8 concentration gradients, and 3 replicate wells were set up for each concentration gradient.

[0096] 3) Administration:

[0097] When the cell seeding rate in the 96-well plate reached 40%–60%, the drug was administered. For the control group, 200 μL of culture medium containing 10% PBS was added to each well; for the positive control group, 200 μL of culture medium containing 10% DMSO was added to each well; for the sample group, 200 μL of culture medium containing the concentrations of the samples shown in Table 3 was added to each well; for the zeroing group, no cells were seeded, only 200 μL of cell culture medium was added. After drug administration, the 96-well plate was placed in an incubator for culture.

[0098] 4) Vitality test:

[0099] After 24 hours of cell incubation, the supernatant was discarded, and MTT working solution (0.5 mg / mL) was added. The cells were incubated at 37°C in the dark for 4 hours. After incubation, the supernatant was discarded, and 100 μL of DMSO was added to each well. The OD value was read at 490 nm. Cell viability was calculated as follows:

[0100]

[0101] Table 3. Dosage concentration and detection results

[0102]

[0103] The results are shown in Table 3. The results indicate that bis(tocopherol) azelaate has low irritant effect on cells, which is superior to azelaic acid and other azelaic acid compounds.

[0104] (2) Inhibition of cell adipogenesis

[0105] 1) Cell seeding: at 1×10 5 Cells were seeded at a density of cells / well into 24-well plates and incubated overnight in an incubator (37°C, 5% CO2).

[0106] 2) Solution preparation: Prepare working solutions of different concentrations of the test substance according to the experimental design table shown in Table 4.

[0107] 3) Drug administration: According to Table 4, when the cell deposition rate in the 24-well plate reaches 40% to 60%, the cells are administered to groups, with 3 replicates per group, and the cells are incubated for another 24 hours.

[0108] 4) Staining: Discard the culture medium, rinse the cells with PBS, fix them, add Nile Red for 15 min, rinse and take pictures with a fluorescence microscope.

[0109] 5) Analysis results: The fluorescence intensity was quantitatively analyzed using Image Pro Plus software.

[0110] The results are shown in Table 4. Tocopherol itself does not have an inhibitory effect on lipid droplets, while the inhibitory effect of bistocopherol azelaate on lipid droplets is significantly better than that of azelaic acid and other azelaic acid compounds.

[0111] Table 4. Dosage Concentration and Detection Results

[0112]

[0113] (3) Antioxidant performance testing

[0114] Preparation of DPPH solution: Weigh 7.9 mg of DPPH using an electronic analytical balance, dissolve it in anhydrous ethanol, and dilute to 200 mL in a volumetric flask to a concentration of 0.1 mmol / L. Shake well, protect from light, and set aside.

[0115] A0 is 3 mL DPPH solution + 3 mL anhydrous ethanol;

[0116] Aj is 3 mL DPPH solution + 3 mL sample solution;

[0117] Ai is 3 mL of sample solution + 3 mL of anhydrous ethanol.

[0118] Shake vigorously to mix well. After standing at 37℃ for 10 minutes, add the sample to a cuvette for absorbance measurement. Measure the absorbance values ​​of Ao, Aj, and Ai, representing the sample. Calculate the clearance rate using the formula:

[0119] SA(%)=1-(A i -A j ) / A0×100%.

[0120] The results are shown in Table 5. The results indicate that the antioxidant properties of bis(tocopherol) azelaate are significantly better than those of tocopherol and other azelaic acid compounds.

[0121] Table 5. Results of Antioxidant Tests

[0122]

[0123]

[0124] (4) Solubility test

[0125] The solubility (w / w) of the compounds was tested, and the results showed that azelaic acid was only 0.1% soluble in dibutyl adipate, while bis(tocopherol) azelaic acid ester had a solubility of 10% in dibutyl adipate.

[0126] Example 8: Application of bis(tocopherol) azelaate in product preparation

[0127] 1. Take the bis(tocopherol) azelaic acid ester prepared in Example 1 and prepare cosmetics. The composition is shown in Table 6.

[0128] Table 6 Cosmetic Ingredients

[0129] Element percentage water 62.1 glycerin 5 PHCG 0.8 Xanthan Gum 0.1 PEG-100, Glyceryl Stearate 3 Cetearyl alcohol 2 Cetiol B (dibutyl adipic acid ester) 22 Bistocopherol Azelate 5

[0130] 2. Prepare cosmetics using equal amounts of azelaic acid and tocopherol.

[0131] Cosmetics were prepared by replacing the ditocopherol azelate in step 1 with azelaic acid and tocopherol. The stability of the cosmetics was tested (the cosmetics were tested for precipitation and discoloration at 40℃ for 60 days). The results are shown in Table 7.

[0132] Table 7 Stability Testing

[0133]

[0134] Although the present invention has been disclosed above with reference to preferred embodiments, it is not intended to limit the present invention. Anyone skilled in the art can make various modifications and alterations without departing from the spirit and scope of the present invention. Therefore, the scope of protection of the present invention should be determined by the claims.

Claims

1. A cosmetic product for inhibiting lipid droplet formation, characterized in that, The cosmetic's components, by mass fraction, are: 62.1% water, 5% glycerin, 0.8% PHCG, 0.1% xanthan gum, and 3% PEG. 100, 2% cetearyl alcohol, 22% Cetiol B and 5% bis(tocopherol) azelaic acid ester; The chemical structural formula of bis(tocopherol) azelaate is shown in Formula I. Formula I.

2. The application of the cosmetic product according to claim 1 in the preparation of cosmetic products that inhibit lipid droplet formation.

3. The application according to claim 2, characterized in that, The cosmetics are selected from serums, essences, sprays, skin foams, lotions, and shampoos.

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