A vitamin c derivative composition and preparation and use thereof

By using magnolol as a protectant and layered micellar gel technology, the problems of stability and activity loss of vitamin C derivatives in cosmetics have been solved, enabling long-term stable application in cosmetics.

CN122097189APending Publication Date: 2026-05-29ZHAOLAI HLDG (SUZHOU) CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHAOLAI HLDG (SUZHOU) CO LTD
Filing Date
2026-02-13
Publication Date
2026-05-29

AI Technical Summary

Technical Problem

Vitamin C derivatives are prone to instability and discoloration in cosmetic formulations, especially in aqueous solutions or high-water-content systems, and long-term loss of activity. Furthermore, there is a research gap in the existing technology regarding the synergistic effect of antioxidant stability.

Method used

A vitamin C derivative composition based on magnolol protectant, comprising vitamin C derivative, antioxidant protectant, nonionic surfactant and structural agent, is used to form a layered micelle gel. Polyglycerol fatty acid ester is used as a carrier, biphenyl compounds are used as antioxidants, and structural agent is used as an auxiliary surfactant to construct a stable gel carrier, thereby improving the stability and activity of vitamin C derivative.

Benefits of technology

It maintains good physical and activity stability under long-term storage, reduces the risk of discoloration and activity degradation of vitamin C derivatives, and is suitable for use in cosmetics, especially in aqueous solutions or high-water-content systems.

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Abstract

The present application relates to the field of cosmetic technology, and more particularly to a vitamin C derivative composition and its preparation and application. The vitamin C derivative composition comprises vitamin C derivative, antioxidant protective agent, non-ionic surfactant, structure aid, and water. The non-ionic surfactant of polyglycerol short-chain ester is selected as the structure carrier, the antioxidant protective agent is dispersed in the gel carrier of lamellar micelles, the structure aid is used as the lipophilic auxiliary surfactant to cooperate with the structure layer, the hydrophilic end exists in the water phase between layers in the form of the fusion of the vitamin C derivative active molecule and water, and finally the gel carrier with certain consistency can be constructed. As the gel matrix, the solid state characteristics are beneficial to reducing the risk of the stability decline and activity degradation of the vitamin C derivative, thereby providing a better solution for the stable application of the vitamin C derivative in cosmetics.
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Description

Technical Field

[0001] This invention relates to the field of cosmetic technology, and in particular to a vitamin C derivative composition and its preparation and application. Background Technology

[0002] Vitamin C (L-ascorbic acid), one of the strongest antioxidants in nature, can capture free radicals and resist damage caused by free radicals and reactive oxygen species. In cosmetics, it is commonly used as a reducing agent, ultraviolet absorber, and melanin synthesis inhibitor. However, vitamin C is easily degraded by pH, temperature, light, dissolved oxygen, and metal ions, and its effective concentration is high, often resulting in products with high irritation. Therefore, vitamin C derivatives have been developed to meet market demand. Currently, vitamin C derivatives mainly exist in three forms: VC salts, VC glycosides, and VC esters. VC ester derivatives are fat-soluble and mainly used in oil-based formulations, exhibiting excellent stability. VC salts and VC glycoside derivatives retain water-soluble properties. Although they possess a certain degree of stability and mildness compared to the original vitamin C in their chemical structure, their stability continues to decline when exposed to water, light, and air for extended periods. In particular, long-term storage in highly aqueous systems leads to severe discoloration and accelerated decline in activity.

[0003] Currently, the main challenges in the application of vitamin C and its derivatives in the market are addressed through methods such as polyol / polymer suspension technology, liposome encapsulation technology, dosage form innovation, and synergistic activity of compositions. Among the existing published patents, patent CN104994849 A discloses a transparent sol-gel composition of high-concentration vitamin C and vitamin C derivatives. This invention improves the activity and stability of vitamin C and derivatives by forming a high-viscosity sol system with high content of alcohol and viscous polysaccharides. However, the high content of alcohol inevitably causes a heat sensation, and the viscous polysaccharides inevitably cause a sticky feel on the skin. Patent CN113365599 B discloses a composition that uses a gel structure to stabilize vitamin C derivatives. This invention uses anionic surfactants and higher alcohols to form a viscous cream formulation containing VC derivatives. It only optimizes the stability of a single VC derivative. Patent CN 112120942 A discloses a non-surfactant cosmetic composition. This invention stabilizes vitamin C derivatives through a water-in-silicone (W / Si) formulation without surfactants, improving the heavy feel on the skin while increasing the stability of VC derivatives. However, the composition contains a lot of silicone powder and silicone oil, which may cause potential risks such as skin sensitivity and cannot be used in silicone-free skin care products. Patent CN 119185099 Patent A discloses a multiphase VC mixture and its storage and usage method, cosmetics, and storage packaging. This invention mixes and uses powdered prototype VC, water-soluble VC derivatives, and oil-soluble VC derivatives in a specific ratio, and ensures the stability of VC and its derivatives through compartmentalized storage design. Its main innovation lies in the dosage form. Patent CN 120131474 A discloses a whitening compound VC that achieves rapid whitening and spot-fading effects. This invention mainly focuses on simple effect superposition and does not truly solve the problem of the stability of VC derivatives in application.

[0004] In summary, the application challenges of vitamin C derivatives in cosmetic formulations, especially those involving aqueous solutions or the presence of water in the formulation, which can easily lead to instability, discoloration, and long-term loss of activity, still need to be addressed. Furthermore, there is a lack of research on the synergistic effect of vitamin C derivatives combined with citronellol as a protective agent in terms of antioxidant stability. Summary of the Invention

[0005] The purpose of this invention is to overcome the shortcomings of the existing technology and provide a vitamin C derivative composition gel formulation based on magnolol protectant, which can improve the stability of vitamin C derivatives in cosmetic formulations.

[0006] To achieve the above objectives, the technical solution adopted by the present invention is as follows: In a first aspect, the present invention provides a vitamin C derivative composition comprising the following components in parts by weight: 5-15 parts of vitamin C derivative, 1-3 parts of antioxidant, 45-65 parts of nonionic surfactant, 1-5 parts of structural auxiliaries, and water to make up to a total of 100 parts by weight. The vitamin C derivatives include at least two of the following: vitamin C ether derivatives, vitamin C salt derivatives, and vitamin C glycoside derivatives; The antioxidant protective agents include biphenyl compounds; The nonionic surfactant includes polyglycerol fatty acid ester surfactants; the polyglycerol fatty acid ester surfactants conform to the following general structural formula: , Where n is the degree of polymerization of the polyglycerol structure, n=2-10; R-COOH is a fatty acid group, including caprylic acid, capric acid, lauric acid, coconut acid, myristic acid, oleic acid or isostearic acid; The structural aid includes sorbitan fatty acid ester surfactants; the sorbitan fatty acid ester surfactants conform to the following general structural formula: , R2-COOH is a fatty acid group, including lauric acid, palmitic acid, stearic acid or oleic acid.

[0007] To address the instability of vitamin C derivatives in cosmetic formulations, this invention designs a stable vitamin C derivative composition, specifically a gel formulation. Micelle formation occurs when surfactants are dispersed in a solvent and, at a certain concentration, molecular association occurs, forming micelles. When the nonionic surfactant in the system reaches a specific concentration, it self-assembles into an associative aggregate with parallel aqueous and hydrophobic layers in the presence of water, forming a viscoelastic gel-like substance. Polyglycerol fatty acid esters, as nonionic surfactants generated by the esterification of polyglycerol and fatty acids, are derived from natural renewable resources and possess safety and low irritation, making them an ideal choice as a carrier for vitamin C derivative micelle gels. At a specific concentration, polyglycerol fatty acid ester surfactants can disperse magnolol molecules at the lipophilic end of the gel layered structure. The structural auxiliaries, acting as auxiliary surfactants, have good lipophilicity and can stabilize the hydrophobic end, preventing damage to the structural layers; while the hydrophilic end exists in the aqueous phase between the layers as vitamin C derivative active molecules fused with water.

[0008] This invention selects polyglycerol fatty acid esters as the main surfactant, which has good water solubility and can be dispersed in aqueous solvents containing vitamin C derivatives. Because the polyglycerol backbone contains multiple hydroxyl groups, it can form layered gel micelles through hydrogen bonding. The fatty acid residues, acting as lipophilic groups, can carry water-insoluble antioxidant components (craniol) into the hydrophobic layer. The antioxidant is selected from biphenyl compounds; the phenolic hydroxyl structure of biphenyl gives its compounds strong antioxidant capabilities, which can slow down the active oxidation of vitamin C derivatives, while also possessing anti-inflammatory and antibacterial effects. The structural aid is a lipophilic surfactant with higher fatty acids as hydrophobic groups; its addition stabilizes the lipophilic ends, ultimately constructing a gel carrier with a certain consistency. Furthermore, as a gel matrix, its solid-state properties help reduce the risk of instability (discoloration) and active degradation of vitamin C derivatives, thus providing a better solution for the stable application of vitamin C derivatives in cosmetics.

[0009] This invention has revealed that a stable gel composition can only be obtained by combining the components within the scope of this invention. If the amount of surfactant added is insufficient, the formation of the layered gel structure is difficult, or it can only stabilize the interface and is easily damaged by external environmental influences, making it difficult to achieve long-term stability. If the total amount of vitamin C derivative added is too low, the effective activity concentration is low, making it difficult to achieve efficacy and lacking application value.

[0010] Preferably, the VC ether derivative includes at least one of 2-o-ethyl ascorbic acid and 3-o-ethyl ascorbic acid.

[0011] Preferably, the VC salt derivative includes at least one of sodium ascorbate, magnesium ascorbate, calcium ascorbate, and sodium isoascorbate.

[0012] Preferably, the VC glycoside derivative includes ascorbate glucoside.

[0013] More preferably, the vitamin C derivative is a compound of 3-o-ethyl ascorbic acid and ascorbate glucoside.

[0014] Specifically, 3-o-ethyl ascorbic acid accounts for 20-80% of the total mass of vitamin C derivatives. For example, the ratio of 3-o-ethyl ascorbic acid to VC glucoside can be 4 / 1, 3 / 2, 1 / 1, 2 / 3, 1 / 4, etc., and is not limited to the above ratios.

[0015] For example, when the total mass percentage of vitamin C derivatives is 5%, the mass ratio of 3-o-ethyl ascorbic acid to VC glucoside can be 4:1, 3:2, 2.5:2.5, 2:3, or 1:4; when the total mass percentage of vitamin C derivatives is 10%, the mass ratio of 3-o-ethyl ascorbic acid to VC glucoside can be 8:2, 6:4, 5:5, 4:6, or 2:8; and when the total mass percentage of vitamin C derivatives is 15%, the mass ratio of 3-o-ethyl ascorbic acid to VC glucoside can be 12:3, 9:6, 7.5:7.5, 6:9, or 3:12.

[0016] More preferably, 3-o-ethyl ascorbic acid accounts for 60-80% of the total mass of the vitamin C derivative. For example, the ratio of 3-o-ethyl ascorbic acid to VC glucoside can be 4 / 1 or 3 / 2; based on the fact that the vitamin C derivative accounts for 10% of the total mass of the composition, the optimal mass ratio of 3-o-ethyl ascorbic acid to VC glucoside is 8:2 and 6:4.

[0017] Among numerous vitamin C derivatives, 3-o-ethyl ascorbic acid is the closest to the original vitamin C, possessing amphiphilic properties with both hydrophilic and lipophilic structures, making it easily penetrate the stratum corneum and absorbed by the skin. Ascorbate glucoside has good hydrophilicity, high safety, and can exert antioxidant and whitening effects without the need for high concentrations. Therefore, this invention combines these two vitamin C derivatives to maximize their advantages and solve the problem of poor stability in application.

[0018] Preferably, the biphenyl compounds include at least one of magnolol and honokiol.

[0019] The general structural formula of biphenyl compounds is as follows: ; Where R3 = H or OH; R4 = H or OH; For example, when R3=OH and R4=H, the chemical structure is magnolol (also known as magnolol). When R3=H and R4=OH, the chemical structure is magnolol.

[0020] Magnoliosol, also known as magnolol, is an isomer of magnolol and is the main active ingredient of magnolia bark. It is a natural product extracted from the dried bark, root bark and branch bark of magnolia bark, a plant of the Magnoliaceae family. It has poor water solubility and has anti-inflammatory, antibacterial and antioxidant effects.

[0021] Preferably, the polyglycerol fatty acid ester is a colorless to pale yellow water-soluble viscous liquid with an HLB value in the range of 8-12.

[0022] Preferably, the nonionic surfactant comprises at least two of polyglycerol-2-decanoate, polyglycerol-3-laurate, polyglycerol-3-cocoate, polyglycerol-4-laurate, polyglycerol-5-myristate, polyglycerol-5-isostearate, polyglycerol-6-didecanoate, polyglycerol-6-caprylate, polyglycerol-6-laurate, polyglycerol-10-myristate, and polyglycerol-10-oleate.

[0023] Preferably, the nonionic surfactant is a compound of polyglycerol-10 oleate and polyglycerol-6 laurate; the mass ratio of polyglycerol-10 oleate to polyglycerol-6 laurate is polyglycerol-10 oleate: polyglycerol-6 laurate = (20-30): (25-35).

[0024] Preferably, the structural additive includes at least one of sorbitan laurate, sorbitan palmitate, sorbitan stearate, and sorbitan oleate.

[0025] Secondly, the present invention provides a method for preparing the above-mentioned vitamin C derivative composition, comprising the following steps: (1) Mix the nonionic surfactant, antioxidant and structural additive, and dissolve them evenly to obtain mixture a; (2) Add some water to the vitamin C derivative to dissolve it, mix well, and obtain mixture b; (3) Mix mixture a and mixture b, add the remaining water and mix until a uniform and transparent micelle gel is formed; reduce pressure and cool down to obtain the vitamin C derivative composition.

[0026] Preferably, the vitamin C derivative composition is a gel.

[0027] Preferably, the viscosity of the gel is in the range of 15,000-20,000 mPa·s.

[0028] The vitamin C derivative composition obtained by this invention has the appearance of a transparent micelle gel and good water dispersibility.

[0029] This invention uses a nonionic surfactant based on short-chain polyglycerol esters as a structural carrier, and with the synergistic effect of structural aids, employs a special process to obtain a special dispersion carrier for better dispersing biogel formulations that use magnolol molecular structure as the system antioxidant and vitamin C derivative.

[0030] Preferably, the mixing temperature in step (1) is controlled at 70-80°C.

[0031] Preferably, step (2) involves dissolving the material using ultrasound.

[0032] Preferably, in step (3), the temperature of stirring and mixing is controlled at 70-75℃ and the rotation speed is 6000-8000 rpm.

[0033] Preferably, in step (3), the vacuum drying oven is depressurized and repeated 2-3 times. The temperature of the vacuum drying oven is set to 70-80℃, the vacuum degree is set to -0.04 to -0.1MPa, and the processing time is 15-45min.

[0034] Reduced pressure treatment can remove residual air from the gel and lower the oxygen content, thereby reducing the impact of vitamin C derivatives on oxidative discoloration in micellar gels.

[0035] Thirdly, the present invention provides the application of the above-mentioned vitamin C derivative composition in the preparation of cosmetics.

[0036] Preferably, the dosage form of the cosmetic includes cream, lotion, serum, gel, and moisturizer.

[0037] Fourthly, the present invention provides a cosmetic comprising the above-described vitamin C derivative composition and cosmetic excipients.

[0038] Preferably, the vitamin C derivative composition is added to the cosmetic at an amount of 1-50%.

[0039] More preferably, the vitamin C derivative composition is added to cosmetics at an amount of 3-10%.

[0040] Preferably, the excipients include at least one of a thickener, chelating agent, humectant, skin feel conditioner, preservative, and water.

[0041] Preferably, the cosmetic comprises the following components by weight percentage: 3-10% vitamin C derivative composition, 0.5-3% thickener, 0.03-0.2% chelating agent, 3-10% moisturizer, 1-8% skin feel conditioner, 0.5-2% preservative, and water to 100%.

[0042] Preferably, the thickener comprises at least one of xanthan gum, Carrageenan extract, Sphingomonas fermentation product extract, hydroxyethyl cellulose, carbomer, acrylate / C10 30 alkanol acrylate crosspolymer, ammonium acryloyl dimethyl taurate / VP copolymer, and polyacrylate crosspolymer-6.

[0043] Preferably, the chelating agent includes at least one of disodium ethylenediaminetetraacetate, tetrasodium ethylenediaminetetraacetate, sodium gluconate, sodium metabisulfite, citric acid, sodium citrate, and sodium phytate.

[0044] Preferably, the moisturizer includes at least one of polyols, polyglycerols, betaine, trehalose, allantoin, sodium hyaluronate, and ceramides.

[0045] The polyol includes at least one of glycerol, propylene glycol, hexanediol, and butylene glycol.

[0046] Preferably, the skin-feeling conditioner includes at least one of glyceryl polyether-26, PEG / PPG-14 / 7 dimethyl ether, PEG / PPG-17 / 6 copolymer, PEG / PPG / polybutylene glycol-8 / 5 / 3 glyceryl, methyl glucetol polyether-20, water-soluble silicone oil, and water-soluble vegetable oil.

[0047] Preferably, the preservative includes at least one of phenoxyethanol, benzoic acid, parabens, p-hydroxyacetophenone, capryloyl hydroxamic acid, and chlorphenesin.

[0048] Preferably, the cosmetic is an essence.

[0049] Preferably, the preparation method of the cosmetic (essence) includes the following steps: 1. Mix thickener, humectant, chelating agent, skin feel modifier, preservative and some water, heat to 70-85℃, homogenize at high speed, and swell evenly to obtain mixture A; 2. Disperse the vitamin C derivative composition with the remaining water by stirring (vitamin C derivative composition: water = 1:(2-5)) to obtain mixture B; 3. Stir and cool mixture A to below 50°C, add mixture B, stir evenly, cool, and filter to obtain the cosmetic (essence).

[0050] The beneficial effects of this invention are as follows: This invention provides a vitamin C derivative composition (gel formulation) based on gentian alcohol as a protective agent, which maintains good physical and activity stability over long-term storage and can be applied in cosmetics. The vitamin C derivative composition of this invention includes a vitamin C derivative, an antioxidant protective agent, a nonionic surfactant, a structural aid, and water. This invention uses a nonionic surfactant made from a short-chain polyglycerol ester as a structural carrier, dispersing the antioxidant protective agent in a layered micelle gel carrier; the structural aid, as a lipophilic auxiliary surfactant, synergistically stabilizes the structural layers; the hydrophilic ends exist in the aqueous phase between layers in the form of vitamin C derivative active molecules fused with water, ultimately constructing a gel carrier with a certain consistency. As a gel matrix, its solid-state properties help reduce the risk of vitamin C derivative instability (discoloration) and activity degradation, thus providing a better solution for the application of vitamin C derivatives in cosmetics. Attached Figure Description

[0051] Figure 1 The initial appearance of the samples in Examples 1-11 is compared with their appearance after 3 months of storage.

[0052] Figure 2 This is a comparison of the initial appearance of Comparative Examples 1-6 and their appearance after 3 months of storage.

[0053] Figure 3 This is a comparison of the initial appearance of Comparative Example 7-15 samples and their appearance after 3 months of storage.

[0054] Figure 4 The appearance of the sample in Example 6. Detailed Implementation

[0055] To better illustrate the purpose, technical solution, and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.

[0056] Unless otherwise specified, the experimental methods used in this invention are conventional methods, and the materials and reagents used are commercially available products that can be obtained through commercial channels.

[0057] The polyglycerol-10 oleate and polyglycerol-6 laurate of this invention were purchased from Shandong Binzhou Jinsheng New Material Technology Co., Ltd.; ascorbate glucoside, 3-o-ethyl ascorbic acid, sodium ascorbate, magnolol, and honokiol were purchased from Zhuanglai Holdings (Suzhou) Co., Ltd.

[0058] Examples 1-11: Examples 1-11 are vitamin C derivative compositions of the present invention, the composition of which is shown in Table 1.

[0059] Table 1 (Unit: parts by weight) The preparation method of the vitamin C derivative composition includes the following steps: (1) Mix polyglycerol-10 oleate and polyglycerol-6 laurate in a certain proportion, heat to 75-80℃, add magnolol or honokiol and stir to dissolve, then add sorbitan palmitate and dissolve until a semi-transparent and viscous premixed solution is obtained; (2) Mix 3-o-ethyl ascorbic acid, ascorbate glucoside / sodium ascorbate with some water, heat to 60-70℃, and sonicate to dissolve evenly to obtain a second solution; (3) Slowly add the second solution to the pre-mixed solution, set the rotation speed to 6000 rpm, stir and mix, then add the remaining water, and form a uniform and transparent micelle gel material through shearing action; (4) Place the gel material obtained in step (3) on the partition in the vacuum drying oven, turn on the vacuum pump and vacuum valve, set the vacuum degree to -0.08MPa, set the temperature inside the oven to 75℃, perform decompression and evacuation, repeat 3 times, cool down to room temperature, and obtain the vitamin C derivative composition.

[0060] Comparative Examples 1-6: Comparative Examples 1-6 are comparative examples of the vitamin C derivative compositions described in this invention, the composition of which is shown in Table 2, and the preparation method is the same as in the Examples.

[0061] Table 2 (Unit: parts by weight) Among them, the vitamin C derivative compositions of Comparative Examples 1-4 contain only a single vitamin C derivative.

[0062] In the vitamin C derivative compositions of Comparative Examples 5-6, the amount of vitamin C derivative added exceeded the scope of this invention.

[0063] Comparative Examples 7-15: Comparative Examples 7-15 are comparative examples of the vitamin C derivative compositions described in this invention, the composition of which is shown in Table 3, and the preparation method is the same as in the Examples.

[0064] Table 3 (Unit: parts by weight) In the vitamin C derivative compositions of Comparative Examples 7-8, the amount of nonionic surfactant added exceeded the scope of this invention.

[0065] In the vitamin C derivative compositions of Comparative Examples 9-10, only a single nonionic surfactant was used.

[0066] The vitamin C derivative composition of Comparative Example 11 did not contain any added antioxidants.

[0067] In the vitamin C derivative composition of Comparative Example 12, the amount of antioxidant added exceeds the scope of this invention.

[0068] The vitamin C derivative composition of Comparative Example 13 did not contain any structural additives.

[0069] In the vitamin C derivative composition of Comparative Example 14, the amount of structural auxiliaries added exceeded the scope of this invention.

[0070] Comparative Example 15 is a simple water-soluble vitamin C derivative, prepared by mixing 3-o-ethyl ascorbic acid and ascorbate glucoside with water until completely dissolved in a transparent aqueous solution to obtain the water-soluble substance.

[0071] The present invention conducts thermodynamic stability tests and viscosity tests on the obtained vitamin C derivative composition for 3 months to ensure the physical stability of the composition, and characterizes the active content of vitamin C derivative by high performance liquid chromatography (HPLC) to verify the active stability of the composition.

[0072] Test Example 1: Viscosity Test Test samples: Vitamin C derivative compositions prepared in Examples 1-11 and Comparative Examples 1-14.

[0073] Measuring instrument: Digital viscometer NDJ-5S, rotation speed: 30 RPM, rotor: #4.

[0074] The results are shown in Table 4-5.

[0075] Table 4 Table 5 Viscosity data results show that the vitamin C derivative compositions prepared in Examples 1-11 of this invention are gel formulations with stable viscosity.

[0076] The viscosity data from Examples 1-4 and Comparative Examples 1-4 show that the viscosity of Comparative Examples 1-4 is less than 15000 mPa·s. The gel viscosity of the composition sample prepared by compounding two VC derivatives in a specific ratio is better than that of the composition sample prepared by adding any one of the VC derivatives alone.

[0077] A comparison of the viscosity values ​​of Examples 1-4 and Comparative Examples 7-8 shows that the viscosity characteristics of the vitamin C derivative gel formulation prepared in this invention are mainly determined by the amount of nonionic surfactant added. When the amount of nonionic surfactant added is lower than the specified concentration, the proportion of water solvent is relatively high, the formed layered micelles are relatively loose, and a stable structure cannot be formed. Macroscopically, this results in a decrease in the overall viscosity of the composition, and it is prone to problems such as poor stability when affected by external factors.

[0078] The viscosity data from Examples 5-6 and Comparative Examples 9-10 show that the gel of the sample in Examples 5-6 has low flowability. Since the combination of the two polyglycerol fatty acid esters can form tightly parallel stacked layered micelles, the steric hindrance is increased by fatty acid chains of different lengths, which hinders the relative flow between micelles, thereby improving the overall viscosity of the composition gel, which is better than the composition prepared using a single polyglycerol fatty acid ester.

[0079] The viscosity results from Examples 6-8 and Comparative Examples 11-14 show that the samples of Comparative Examples 12-13 have a certain fluidity and the gel viscosity is significantly thinner, while the viscosity of the sample of Comparative Example 14 shows an upward trend. This indicates that both the antioxidant and structural additives in the composition have a certain impact on the viscosity of the composition. When the amount of magnolol added is too high, the hydrophobic ends of the micelles cannot support the excess magnolol, and the layered structure is destroyed, resulting in a significant decrease in the viscosity of the composition. On the other hand, the structural additives, as hydrophobic auxiliary emulsifiers, can enhance the compactness of the layered micelle structure, further demonstrating that the viscosity of the gel composition has increased.

[0080] Test Example 2: Stability Test Test samples: Vitamin C derivative composition samples prepared in Examples 1-11 and Comparative Examples 1-14, and water-soluble vitamin C derivative of Comparative Example 15.

[0081] Test samples were placed in transparent glass bottles, sealed, and placed at room temperature, 45°C, -18°C, and under light conditions for 1-3 months. After being removed and brought back to room temperature, the appearance changes were observed. The results are shown in Table 6-7.

[0082] Table 6 Table 7 The vitamin C derivative-containing gel compositions prepared in Examples 1-11 of this invention all exhibited good stability during a 3-month thermodynamic stability test, and no serious discoloration was observed.

[0083] A comparison of the stability results of the examples and comparative examples shows that the composition samples prepared by combining two vitamin C derivatives (Examples 1-4) did not exhibit significant discoloration in terms of light and heat stability. However, the composition samples prepared using only a single vitamin C derivative (Comparative Examples 1-4) all showed discoloration in terms of light and heat stability, indicating degradation of the active ingredient. Therefore, gel compositions prepared by combining vitamin C derivatives in suitable proportions are superior to those prepared by single components.

[0084] Comparative Example 5 contained more than 15% of a compound vitamin C derivative, while Comparative Example 8 contained more than 65% of a nonionic surfactant. The samples exhibited discoloration or precipitation, which is presumably due to the low proportion of dispersion medium (water) in the system. On the one hand, this required a longer heating time to dissolve the vitamin C derivative, resulting in a certain degree of activity loss during the preparation process; on the other hand, the system lacked sufficient solvent (water) to form uniform layered micelles.

[0085] The sample in Comparative Example 6 showed good stability, but due to the low activity content of vitamin C derivatives in the composition, a higher addition amount was required to achieve a certain efficacy in product application, resulting in low cost-effectiveness and limited application value.

[0086] The stability results of Examples 6-8 and Comparative Examples 11-12 show that adding an appropriate amount of antioxidant (magnoliol or magnolol) to the composition can reduce the stability discoloration caused by light and heat on vitamin C derivatives. When combined with vitamin C derivatives, it can synergistically resist oxidation, improve the stability of the composition, and play a synergistic role.

[0087] Test Example 3: Determination of Activity Content Since there is a close relationship between the color change and activity of vitamin C derivatives, the color change of the composition can reflect its degree of oxidation, that is, directly reflect the change in its activity loss.

[0088] The initial appearance of the samples from Examples 1-11 and Comparative Examples 7-15 and the appearance of the material after being stored at room temperature for 3 months were recorded and compared. The results are as follows: Figure 1-3 As shown.

[0089] Furthermore, the final active contents of 3-o-ethyl ascorbic acid and VC glucoside in the samples prepared in the examples and comparative examples were determined by high performance liquid chromatography (HPLC). The test method was based on the "Test Methods for 11 Raw Materials including Magnesium Ascorbate Phosphate in Cosmetics".

[0090] Determination conditions: Column: C18 (4.6) Column diameter: 250 nm (5 μm); Mobile phase: methanol, 0.02 mol / L potassium dihydrogen phosphate solution; Wavelength: 250 nm; Flow rate: 1 mL / min; Injection volume: 20 μl; Column temperature: 30 °C. The retention rate of the active ingredient was calculated using the following formula: Retention rate = (Retention value / Initial value) × 100%.

[0091] The results are shown in Table 8-9: Table 8 Table 9 Depend on Figure 1 A comparison of the color and appearance of the pre- and post-treatment samples shows that none of the gel compositions in Examples 1-11 exhibited significant color change, directly reflecting low activity loss during prolonged storage at room temperature. Further analysis using high-performance liquid chromatography (HPLC) to determine the activity content revealed in Table 8 that the retention rate of 3-o-ethyl ascorbic acid in the composition reached a maximum of 96.4%, and the final retention rate of ascorbate glucoside reached 94.7%. In contrast, the untreated Comparative Example 15 solution showed a retention rate of only 34.6% for 3-o-ethyl ascorbic acid and a final retention rate of 29.7% for ascorbate glucoside, with the sample exhibiting a dark brown color and retaining less than half of its active content. Therefore, this invention, in a gel formulation system, can maximize the retention of vitamin C derivative activity and minimize activity loss.

[0092] like Figure 2 As shown, the samples in Comparative Examples 1-5 exhibited a distinct yellow gel appearance after 3 months of storage, indicating a significant decrease in the activity content of the vitamin C derivative in the composition. A comparison of the discoloration levels between Comparative Examples 11-12 and Example 5 shows that adding an appropriate amount of magnolol to the composition can improve the instability caused by discoloration and activity degradation during storage, providing good protection for the active ingredients. Furthermore, the results of the activity content changes in Table 9 show that without the addition of antioxidants, the retention rate of 3-o-ethyl ascorbic acid in Comparative Example 11 was only 44.1%, and the final retention rate of ascorbate glucoside was 41.3%.

[0093] Therefore, this invention, by selecting specific nonionic surfactants and structural additives and using a special process, constructs a gel formulation carrier capable of supporting 5-15% of added vitamin C derivatives, and synergistically enhances the effect with magnolol molecules, protecting the activity retention rate of vitamin C derivatives to over 85%, thereby improving the thermodynamic stability and activity stability of the overall composition.

[0094] Application Examples: This application example provides a VC antioxidant serum, comprising the vitamin C derivative composition of Example 6 ( Figure 4 The specific formula is shown in Table 10.

[0095] Table 10 The preparation method of the essence includes the following steps: 1. Mix the thickener with butylene glycol and polyglycerol-10, add some deionized water for premixing, heat to 70-85℃, swell evenly, then add the remaining moisturizer, chelating agent, preservative and skin feel conditioner, homogenize at high speed (10000-12000 rpm) until evenly mixed to obtain a transparent and uniform viscous liquid; 2. Mix the vitamin C derivative composition with water at a weight ratio of 1:2, stir to dissolve, and obtain a vitamin C derivative mixture; 3. Cool the viscous liquid obtained in step (1) to below 50°C, add the vitamin C derivative mixture, stir evenly, cool, and filter to obtain the essence.

[0096] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and are not intended to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the essence and scope of the technical solutions of the present invention.

Claims

1. A vitamin C derivative composition, characterized in that, The product comprises the following components by weight: 5-15 parts of vitamin C derivative, 1-3 parts of antioxidant protectant, 45-65 parts of nonionic surfactant, 1-5 parts of structural aid, and water to make up to a total weight of 100 parts. The vitamin C derivatives include at least two of the following: vitamin C ether derivatives, vitamin C salt derivatives, and vitamin C glycoside derivatives; The antioxidant protective agents include biphenyl compounds; The nonionic surfactant includes polyglycerol fatty acid ester surfactants; the polyglycerol fatty acid ester surfactants conform to the following general structural formula: , Where n is the degree of polymerization of the polyglycerol structure, n=2-10; R-COOH is a fatty acid group, including caprylic acid, capric acid, lauric acid, coconut acid, myristic acid, oleic acid or isostearic acid; The structural aid includes sorbitan fatty acid ester surfactants; the sorbitan fatty acid ester surfactants conform to the following general structural formula: , R2-COOH is a fatty acid group, including lauric acid, palmitic acid, stearic acid or oleic acid.

2. The vitamin C derivative composition according to claim 1, characterized in that, The VC ether derivatives include at least one of 2-o-ethyl ascorbic acid and 3-o-ethyl ascorbic acid; And / or, the VC salt derivatives include at least one of sodium ascorbate, magnesium ascorbate, calcium ascorbate, and sodium isoascorbate; And / or, the VC glycoside derivatives include ascorbate glucoside.

3. The vitamin C derivative composition according to claim 2, characterized in that, The vitamin C derivative is a compound of 3-o-ethyl ascorbic acid and ascorbate glucoside; the 3-o-ethyl ascorbic acid accounts for 20-80% of the total mass of the vitamin C derivative.

4. The vitamin C derivative composition according to claim 1, characterized in that, The biphenyl compounds include at least one of magnolol and honokiol.

5. The vitamin C derivative composition according to claim 1, characterized in that, The nonionic surfactant includes at least two of the following: polyglycerol-2-decanoate, polyglycerol-3-laurate, polyglycerol-3-cocoate, polyglycerol-4-laurate, polyglycerol-5-myristate, polyglycerol-5-isostearate, polyglycerol-6-didecanoate, polyglycerol-6-caprylate, polyglycerol-6-laurate, polyglycerol-10-myristate, and polyglycerol-10-oleate.

6. The vitamin C derivative composition according to claim 5, characterized in that, The nonionic surfactant is a compound of polyglycerol-10 oleate and polyglycerol-6 laurate; the mass ratio of polyglycerol-10 oleate to polyglycerol-6 laurate is polyglycerol-10 oleate: polyglycerol-6 laurate = (20-30): (25-35).

7. The vitamin C derivative composition according to claim 1, characterized in that, The structural additives include at least one of sorbitan lauryl ester, sorbitan palmitate, sorbitan stearate, and sorbitan oleate.

8. A method for preparing a vitamin C derivative composition according to any one of claims 1-7, characterized in that, Includes the following steps: (1) Mix the nonionic surfactant, antioxidant and structural agent and dissolve them evenly to obtain mixture a; (2) Add some water to the vitamin C derivative to dissolve it, mix well, and obtain mixture b; (3) Mix mixture a and mixture b, add the remaining water and mix until a uniform and transparent micelle gel is formed; reduce pressure and cool down to obtain the vitamin C derivative composition.

9. The use of the vitamin C derivative composition according to any one of claims 1-7 in the preparation of cosmetics.

10. A cosmetic product, characterized in that, Includes excipients required for the vitamin C derivative composition and cosmetic as described in any one of claims 1-7; the amount of the vitamin C derivative composition added to the cosmetic is 1-50%.

Citation Information

Patent Citations

  • Transparent sol, gel composition containing high concentrations of vitamin c and vitamin c derivative

    CN104994849A

  • Surfactant-free cosmetic composition

    CN112120942A

  • Compositions that stabilize vitamin C derivatives using gel structures

    CN113365599B

  • Multi-phase VC mixture, storage and use method thereof, cosmetic and storage package

    CN119185099A

  • Composite VC whitening and spot-fading composition, preparation method thereof and application of cosmetic

    CN120131474A