Compound with high water dispersibility as well as preparation method and application thereof

By mixing emulsion dilution and freeze-drying, the problem of ceramides and phytosphingosines being poorly soluble in water was solved, and a complex powder with small and uniform particle size and good water dispersibility was prepared, which is suitable for daily chemical products and improves the skin barrier protection effect.

CN121754430APending Publication Date: 2026-03-31HANGZHOU VIABLIFE BIOTECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-09-29
Publication Date
2026-03-31

AI Technical Summary

Technical Problem

In the existing technology, ceramides and phytosphingosine are not easily soluble in water, which limits their application in the daily chemical industry. In addition, the existing aqueous dispersions have uneven particle size, poor stability, and low content of effective ingredients.

Method used

A mixed emulsion was formed by mixing an oil phase with an aqueous phase containing a non-water-soluble compound, an amphiphilic substance, and at least two surfactants. The emulsion was then diluted and freeze-dried to prepare a composite powder with small and uniform particle size and good water dispersibility.

Benefits of technology

A complex powder with small and uniform particle size and good water dispersibility was prepared. It has a high content of active ingredients and good stability in water dispersion, making it suitable for mass production and application in daily chemical products, and enhancing the skin barrier function.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention discloses a compound with high water dispersibility and a preparation method and application thereof.The preparation method of the compound with the high water dispersibility comprises the steps that an oil phase containing a water-insoluble compound, an amphiphilic substance and at least two surfactants is mixed with a water phase to obtain a mixed emulsion, then the mixed emulsion is diluted, and the compound with the high water dispersibility is obtained. The compound with high water dispersibility is obtained. The prepared compound with high water dispersibility can be subjected to freeze-drying treatment to obtain compound powder with high water dispersibility, the content of ceramide substances and / or sphingosine substances is high, the compound powder is easily dispersed in water, and the compound powder can stably exist and be dispersed in water under a long-time storage condition, so that the compound powder has good water dispersibility. The phenomena of layering, floccules, precipitation and the like are not easy to occur, and the preparation of daily chemical products is facilitated.
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Description

Technical Field

[0001] This invention relates to the field of ceramide technology, and more specifically, to a complex with high water dispersibility, its preparation method, and its application. Background Technology

[0002] Currently, there are many high-performance raw materials available in the daily chemical industry, such as ceramides and phytosphingosine.

[0003] Ceramides are a class of amide compounds (mainly ceramides 1-11) formed by the dehydration of the amino groups of long-chain fatty acids and sphingosine. Ceramide 3 is obtained by acylation of phytosphingosine with stearic acid, while ceramide 3B is synthesized from phytosphingosine and oleic acid. 40%-50% of sebum in the stratum corneum is composed of ceramides, which are a major component of the intercellular matrix and play a crucial role in maintaining the moisture balance of the stratum corneum. Ceramides have a strong ability to associate water molecules, maintaining skin moisture by forming a network structure in the stratum corneum. Therefore, ceramides have a role in maintaining skin moisture. Ceramides (Cers) are present in all eukaryotic cells and play an important regulatory role in cell differentiation, proliferation, apoptosis, aging, and other life activities. As a major component of the intercellular lipids of the stratum corneum, ceramides not only act as second messenger molecules in the sphingomyelin pathway but also play an important role in the formation of the epidermal stratum corneum, thus having functions such as maintaining the skin barrier, moisturizing, anti-aging, whitening, and disease treatment.

[0004] Phytosphingosine, also known as neurosphingosine, is a precursor to ceramides. It exists in the epidermis and superficial layers of the skin and is an important lipid component of the human epidermis. Its structure is similar to that of the stratum corneum, allowing it to quickly penetrate the skin and combine with water in the stratum corneum to form a network structure that locks in moisture. Phytosphingosine can repair the skin barrier; as a natural component of skin lipids, it has a barrier-repairing effect. Phytosphingosine can also combat aging; loss of phytosphingosine leads to dry and rough skin. Furthermore, it can inhibit the growth of harmful bacteria and fight inflammatory responses.

[0005] However, most ceramides and phytosphingosines are poorly soluble in water, cannot disperse uniformly in water, and are prone to precipitation, limiting their widespread application in the daily chemical industry. For example, adding ceramide 3B or ceramide 3 to water fails to form a homogeneous solution, resulting in solid precipitation; similarly, when ceramide 3B or ceramide 3 is added to cosmetic compositions, precipitation also occurs, meaning that when applied to the skin, it cannot be effectively absorbed and its efficacy cannot be fully realized. Similarly, while phytosphingosines can bind with water and help retain skin moisture, their water solubility is not high.

[0006] For compounds that are poorly soluble in water (such as ceramides and phytosphingosine), there are currently some preparation methods to increase their water solubility or dispersibility. However, some problems still exist. For example, the resulting water-dispersed ceramide complexes have large and uneven particle sizes. Even initially uniform ceramide aqueous dispersions may precipitate out after a period of time, indicating instability. Furthermore, the stability of ceramide complex aqueous dispersions is even worse at high or low temperatures. The ceramide content in ceramide complexes prepared in existing technologies is low, not exceeding 10%.

[0007] Therefore, it is essential to develop a preparation method that produces particles with small and uniform size, good water dispersibility, high stability of the aqueous dispersion, and high content of effective substances (ceramides or phytosphingosine). Summary of the Invention

[0008] The purpose of this invention is to overcome the defects of the prior art and provide a complex with high water dispersibility, its preparation method and application.

[0009] The technical problem solved by this invention is achieved by the following technical solution.

[0010] The present invention provides a method for preparing a complex with high water dispersibility, comprising: mixing an oil phase of an insoluble compound, an amphiphilic substance, and at least two surfactants with an aqueous phase to obtain a mixed emulsion, and then diluting the mixed emulsion to obtain a complex with high water dispersibility.

[0011] The present invention also provides a method for preparing a complex powder with high water dispersibility, comprising: freeze-drying a diluted mixed emulsion prepared by the above preparation method to obtain a complex powder with high water dispersibility.

[0012] The present invention also provides a complex powder with high water dispersibility, the complex powder being prepared by the preparation method described above, and the content of ceramide and / or sphingosine in the complex powder with high water dispersibility is 16-78%.

[0013] The present invention also provides the application of the above-mentioned complex with high water dispersibility or the complex powder with high water dispersibility prepared by the above preparation method in the preparation of daily chemical products or pharmaceuticals.

[0014] The present invention has the following beneficial effects:

[0015] This invention provides a complex with high water dispersibility, its preparation method, and its application. The method provided by this invention can prepare a complex with small and uniform particle size and good water dispersibility. After freeze-drying, the complex powder has small and uniform particle size, good water dispersibility, and high stability in the aqueous dispersion. This complex powder has a high content of active ingredients (ceramides or phytosphingosines). The preparation method is simple to operate and suitable for the preparation and storage of large quantities of ceramide or phytosphingosine complex powders, making it more advantageous for application in the preparation of daily chemical products. Attached Figure Description

[0016] To more clearly illustrate the technical solutions of the embodiments of the present invention, the accompanying drawings used in the embodiments will be briefly introduced below. It should be understood that the following drawings only show some embodiments of the present invention and should not be regarded as a limitation on the scope. For those skilled in the art, other related drawings can be obtained based on these drawings without creative effort.

[0017] Figure 1 The particle size distribution diagram is shown for the ceramide complex powder prepared in Example 1.

[0018] Figure 2 The particle size distribution diagram is shown for the ceramide complex powder obtained in Example 2.

[0019] Figure 3 The particle size distribution diagram is shown for the ceramide complex powder prepared in Comparative Example 3.

[0020] Figure 4 The particle size distribution diagram is shown for the ceramide complex powder prepared in Comparative Example 1.

[0021] Figure 5 The particle size distribution diagram is shown for the ceramide complex powder prepared in Comparative Example 2.

[0022] Figure 6 To disperse the powders obtained in Examples 1, 2, and 3 in water to obtain a powder aqueous dispersion with a mass fraction of 0.5%, the initial dispersion state diagram is shown.

[0023] Figure 7 for Figure 6 The state diagram of the powder aqueous dispersion after being dispersed at 40℃ and stirred at 200 rpm for 10 min;

[0024] Figure 8 The image shows the state of the aqueous dispersion of the powder prepared in Comparative Example 3 after being placed at room temperature for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0025] Figure 9The image shows the state of the aqueous dispersion of the powder prepared in Example 2 after being placed at room temperature for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0026] Figure 10 The image shows the state of the aqueous dispersion of the powder prepared in Example 1 after being placed at room temperature for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0027] Figure 11 The image shows the state of the aqueous dispersion of the powder prepared in Comparative Example 3 after being refrigerated at 4°C for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0028] Figure 12 The image shows the state of the aqueous dispersion of the powder prepared in Example 2 after being refrigerated at 4°C for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0029] Figure 13 The image shows the state of the aqueous dispersion of the powder prepared in Example 1 after being refrigerated at 4°C for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0030] Figure 14 The image shows the aqueous dispersion of the powder prepared in Comparative Example 3; the state diagram after freezing and thawing at -20℃ for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0031] Figure 15 The image shows an aqueous dispersion of the powder prepared in Example 2; the state diagram after freezing and thawing at -20°C for 3 days; from left to right, the mass fractions of the composite powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0032] Figure 16 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after freezing and thawing at -20°C for 3 days; from left to right, the mass fractions of the composite powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0033] Figure 17 The image shows an aqueous dispersion of the powder prepared in Comparative Example 3; the state diagram after being placed at 40°C for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0034] Figure 18 The image shows an aqueous dispersion of the powder prepared in Example 2; the state diagram after being placed at 40°C for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0035] Figure 19 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after being placed at 40°C for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0036] Figure 20 The image shows an aqueous dispersion of the powder prepared in Example 1; its state after being left at room temperature for 3 months; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0037] Figure 21 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after being placed at 4°C for 3 months; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0038] Figure 22 Aqueous dispersion of the powder prepared in Example 1; state diagram after freeze-thaw at -20°C for 3 months; from left to right, the mass fractions of the composite powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively;

[0039] Figure 23 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after being placed at 40°C for 3 months; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively. Detailed Implementation

[0040] To make the objectives, technical solutions, and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below. Where specific conditions are not specified in the embodiments, conventional conditions or conditions recommended by the manufacturer shall apply. Reagents or instruments whose manufacturers are not specified are all conventional products that can be purchased commercially.

[0041] The following is a detailed description of a complex with high water dispersibility, its preparation method, and its application provided by embodiments of the present invention.

[0042] In a first aspect, embodiments of the present invention provide a method for preparing a complex with high water dispersibility, comprising: mixing an oil phase containing a non-water-soluble compound, an amphiphilic substance, and at least two surfactants with an aqueous phase to obtain a mixed emulsion, and then diluting the mixed emulsion to obtain a complex with high water dispersibility.

[0043] This invention provides a method for preparing a complex with high water dispersibility. In the preparation process, an oil phase containing a non-water-soluble compound, an amphiphilic substance, and at least two surfactants are mixed with an aqueous phase to obtain a mixed emulsion. The amphiphilic substance has an amphiphilic molecular structure and also has emulsifying function, which can serve as a good wall material to encapsulate the non-water-soluble compound. The at least two surfactants can improve the stability of the mixed solution, so as to prepare a complex with good water dispersibility and high stability of the aqueous dispersion.

[0044] In some alternative embodiments, a method for preparing a complex with high water dispersibility includes: mixing an oil phase containing a non-water-soluble compound, an amphiphilic substance, a sucrose ester surfactant, and a polyglycerol ester surfactant with an aqueous phase to obtain a mixed emulsion, and then diluting the mixed emulsion to obtain a complex with high water dispersibility.

[0045] This invention provides a method for preparing a complex with high water dispersibility. In the preparation process, an oil phase containing a non-water-soluble compound, an amphiphilic substance, and at least two surfactants is mixed with an aqueous phase to obtain a mixed emulsion. The amphiphilic substance has an amphiphilic molecular structure and also possesses emulsifying capabilities, serving as a good wall material to encapsulate the non-water-soluble compound. Sucrose ester surfactants have good emulsifying, dispersing, and solubilizing effects, as well as strong hydrophilicity; therefore, adding sucrose ester surfactants is highly advantageous when preparing O / W emulsions. Furthermore, sucrose ester surfactants also have good surface activity, enabling them to adsorb onto solid particles, resulting in uniform dispersion of the dispersed solid particles and preventing precipitation. Sucrose ester surfactants can stabilize O / W emulsions, ensuring the stability of the substance during freeze-drying.

[0046] Polyglycerol ester surfactants are a class of nonionic surfactants formed by the esterification reaction of polyglycerol and fatty acids. These compounds possess multiple hydrophilic hydroxyl groups and hydrophobic fatty acid chains. This structure endows polyglycerol ester surfactants with dual hydrophilic and lipophilic properties, enabling them to form a stable film at the water-oil interface, preventing direct contact between the two phases and achieving an emulsifying effect. When polyglycerol ester surfactants are dispersed in water, their hydrophilic groups (hydroxyl groups) form hydrogen bonds with water molecules, while their hydrophobic groups (fatty acid chains) point towards the oil phase, thus forming a thin film at the oil-water interface. This film reduces surface tension, prevents droplet coalescence, and maintains the stability of the emulsion. Furthermore, the acid resistance and high-temperature resistance of polyglycerol ester surfactants further enhance their emulsifying effect under various environments.

[0047] Therefore, after mixing the oil phase containing active substances such as ceramides and / or sphingosine with the aqueous phase to form a homogeneous mixed emulsion, the mixed emulsion is then diluted to obtain a complex with high water dispersibility.

[0048] In some alternative embodiments, the non-water-soluble compounds in the oil phase are non-water-soluble ceramides and / or sphingosines;

[0049] Preferably, the non-water-soluble ceramide substances include at least one of non-water-soluble ceramides, their derivatives and analogs, and the non-water-soluble sphingosine substances include at least one of non-water-soluble sphingosine, its derivatives and analogs.

[0050] Preferably, the non-water-soluble sphingosine compounds include at least one of sphingosine, phytosphingosine, tetraacetyl phytosphingosine, N-acetyl phytosphingosine, and salicyl phytosphingosine;

[0051] Preferably, the non-water-soluble ceramide substances include at least one of ceramide 3 (ceramide NP), ceramide 3B, ceramide 2 (ceramide NS), ceramide 1 (ceramide EOS), ceramide 4 (ceramide EOH), ceramide 5 (ceramide AS), ceramide 6 (ceramide AP), ceramide 7 (ceramide AH), ceramide 8 (ceramide NH), ceramide 9 (ceramide EOP), ceramide 10 (ceramide NDS), and ceramide 11 (ceramide ADS);

[0052] Preferably, the amphiphilic substance includes at least one of hydrogenated lecithin, sunflower lecithin, soybean lecithin, lecithin, and lysophosphatidylcholine;

[0053] Preferably, the sucrose ester surfactant has an HLB value of 8-18, more preferably 10-16, and preferably, the sucrose ester surfactant includes at least one of sucrose citrate, sucrose palmitate, sucrose laurate, and sucrose stearate.

[0054] Preferably, the HLB value of the polyglycerol ester surfactant is 10-16, more preferably 10-13, and preferably, the polyglycerol ester surfactant includes at least one of polyglycerol monostearate, decapolyglycerol monostearate, tripolyglycerol monostearate, and polyglycerol-4-stearate.

[0055] Preferably, the oil phase contains 20-70 parts by mass of the non-water-soluble compound, 5-20 parts by mass of the amphiphilic substance, 5-30 parts by mass of the sucrose ester surfactant, and 10-50 parts by mass of the polyglycerol ester surfactant.

[0056] Preferably, the mass fraction of the non-water-soluble compound is 35-65 parts, more preferably 40-60 parts;

[0057] Preferably, the amphiphilic substance is present in 5-15 parts by mass, more preferably 6-12 parts by mass;

[0058] Preferably, the sucrose ester surfactant is present in 10-20 parts by mass, more preferably in 12-18 parts by mass;

[0059] Preferably, the polyglycerol ester surfactant is present in a mass fraction of 20-40 parts, more preferably 25-35 parts.

[0060] In some optional embodiments, the preparation of the mixed emulsion includes: adding a molten oil phase to a hot water phase for homogenization or stirring; after the addition of the molten oil phase is completed, homogenization or stirring is continued to obtain a uniform mixed emulsion.

[0061] Preferably, the preparation of the molten oil phase includes: mixing a non-water-soluble compound, an amphiphilic substance, a sucrose ester surfactant, and a polyglycerol ester surfactant in a certain mass ratio, heating to 90-200°C to melt the four substances, and stirring until a homogeneous solution is obtained, wherein: the melting temperature is 120-200°C, preferably 130-190°C, more preferably 130-160°C; and the melting time is 25-70 min, preferably 30-60 min.

[0062] Preferably, the temperature of the hot water phase is 80-95℃;

[0063] Preferably, the preparation of the mixed emulsion includes: adding the molten oil phase to a hot water phase at 80-95°C for homogenization or stirring. During homogenization or stirring, the temperature of the mixed system is maintained at 80-95°C and the rotation speed is 7000-50000 rpm. After the molten oil phase is added, homogenization or stirring continues to obtain the mixed emulsion. The mass ratio of the hot water phase to the molten oil phase is 5:1-15:1.

[0064] In the preparation of the above mixed solution, insoluble compounds, amphiphilic substances, sucrose ester surfactants, and polyglycerol ester surfactants are mixed in a specific mass ratio and then melted to obtain a molten oil phase. This molten oil phase is then added to the hot water phase, allowing for better dispersion of the insoluble compounds and resulting in a homogeneous emulsion. After emulsification, an ice bath provides a low-temperature environment during the hardening process of the nanoparticles. This low temperature condition facilitates the hardening process because the reduced temperature promotes the hardening of the nanoparticles in the emulsion, thereby improving the stability and quality of the emulsion.

[0065] Therefore, after mixing the oil phase containing active substances such as ceramides and / or sphingosine with the aqueous phase to form a homogeneous mixed emulsion, the mixed emulsion is then diluted to obtain a complex with high water dispersibility.

[0066] In some optional embodiments, the preparation of the mixed emulsion includes: adding the oil phase to the hot water phase for homogenization or stirring, and continuing homogenization or stirring after the oil phase addition is completed to obtain a uniform mixed emulsion;

[0067] Preferably, the preparation of the oil phase includes: mixing a non-water-soluble compound, an amphiphilic substance, a sucrose ester surfactant, and a polyglycerol ester surfactant in a mass ratio;

[0068] Preferably, the temperature of the hot water phase is 110-150℃;

[0069] Preferably, the preparation of the mixed emulsion includes: adding the oil phase to a hot water phase at 110-150°C for homogenization or stirring; during homogenization or stirring, maintaining the temperature of the mixed system at 100°C-150°C, rotating at 100-300 rpm, and stirring for 10-60 min; then cooling to 85-95°C and continuing homogenization or stirring for 4-12 h to obtain a uniform mixed emulsion; the mass of the oil phase is 0.1-30% of the mass of the hot water phase.

[0070] In the preparation of the above mixed solution, insoluble compounds, amphiphilic substances, sucrose ester surfactants, and polyglycerol ester surfactants are mixed in a specific mass ratio to form the oil phase. This oil phase is then added to the hot water phase. This process allows for better dispersion of the oil phase containing the insoluble compounds in the hot water, simplifies the preparation steps, and yields a homogeneous emulsion. After emulsification, an ice bath is used to provide a low-temperature environment during the hardening process of the nanoparticles. This low-temperature condition facilitates the hardening process because the reduced temperature promotes the hardening of the nanoparticles in the emulsion, thereby improving the stability and quality of the emulsion.

[0071] Therefore, after the oil phase containing active substances such as ceramides and / or sphingosine is mixed with the aqueous phase to form a homogeneous mixed emulsion, the mixed emulsion is then diluted to obtain a complex with high water dispersibility.

[0072] In some optional embodiments, the specific steps for diluting the mixed emulsion are as follows: adding the mixed emulsion to the ice-water phase and stirring to obtain a diluted emulsion;

[0073] Preferably, the total mass of the non-water-soluble compound, the amphiphilic substance, and at least two surfactants is 0.1-30% of the mass of the ice-water phase, more preferably 1-25%, and even more preferably 10-20%.

[0074] Preferably, the temperature of the ice-water phase is below 20°C;

[0075] Preferably, the preparation of the dilute emulsion includes: maintaining the temperature of the mixed emulsion at 60-100°C, adding it to the ice-water phase and stirring, and maintaining the temperature of the mixed system below 20°C during the dilution process to obtain the dilute emulsion.

[0076] Secondly, the present invention provides a method for preparing a composite powder with high water dispersibility, comprising: freeze-drying a diluted mixed emulsion prepared by the above preparation method to obtain a composite powder with high water dispersibility.

[0077] The method for preparing the highly water-dispersible complex powder provided by this invention can produce a complex powder with high content of effective substances (ceramides or phytosphingosines) and small, uniform particle size. This complex powder exhibits good water dispersibility and high stability in its aqueous dispersion. When added to subsequent formulations such as daily chemical products, it will not precipitate, which facilitates the penetration of ceramides or phytosphingosines into the skin to exert their effects, strengthen the skin barrier, protect the skin, and resist some external stimuli. Furthermore, this preparation method is simple to operate and suitable for the large-scale preparation of ceramide or phytosphingosine complex powders.

[0078] Thirdly, embodiments of the present invention provide a composite powder with high water dispersibility, the composite powder being prepared by the preparation method described above.

[0079] In some alternative embodiments, the content of ceramides and / or sphingosines in the highly water-dispersible complex powder is 16-78%.

[0080] Fourthly, the embodiments of the present invention also provide the application of a complex with high water dispersibility prepared by the preparation method described above, or a complex powder with high water dispersibility prepared by the preparation method described above, or the complex powder with high water dispersibility described above, in the preparation of daily chemical products or pharmaceuticals.

[0081] In some alternative embodiments, the daily chemical products include at least one of facial cleanser, skin lotion, skin cream, hair conditioner, and hair conditioner; the pharmaceutical products include skin treatment products; and the dosage forms of the daily chemical products and pharmaceutical products include any one or more of ointments, pastes, lotions, gels, solutions, suspensions, emulsions, patches, and sprays.

[0082] The present invention will be further described below with reference to embodiments.

[0083] Example 1

[0084] A method for preparing a composite powder with high water dispersibility includes the following steps:

[0085] (1) Place A, B, C, and D in the same container and heat to 130°C. A is ceramide 3B, with a mass fraction of 50 parts; B is hydrogenated lecithin, with a mass fraction of 10 parts; C is sucrose stearate, with a mass fraction of 10 parts; and D is decaglycerol monostearate, with a mass fraction of 30 parts. Heat the container to 130°C and melt the four substances in the container. Stir until a homogeneous mixture is obtained, which will be used as the molten oil phase for later use.

[0086] (2) Take pure water into another container and heat it to 95°C to prepare it as a hot water phase for later use. The ratio of the mass of the hot water phase to the mass of the molten oil phase in step (1) is 9:1.

[0087] (3) Add the molten oil phase obtained in step (1) to the hot water phase in step (2) for homogenization or stirring. During homogenization or stirring, maintain the temperature of the mixed system at 85-95℃ and the rotation speed at 14000rpm. After the molten oil phase in step (1) is added, continue homogenization or stirring for 2-5 minutes to obtain a mixed emulsion.

[0088] (4) The mixed emulsion obtained in step (3) is kept at a constant temperature of 80-90°C and added to the ice-water phase. The total mass of A, B, C, and D is 10% of the mass of the ice-water phase. The mixture is stirred continuously, and the temperature of the mixed system is kept below 20°C throughout the process to obtain a thinner emulsion.

[0089] (5) The dilute emulsion obtained in step (4) is freeze-dried to obtain a composite powder with high water dispersibility.

[0090] Example 2

[0091] A method for preparing a composite powder with high water dispersibility includes the following steps:

[0092] (1) Add 2L of water to the container, pressurize it to 0.03MP, and heat it with steam until the water temperature in the container is 130℃. Use this as the hot water phase for later use.

[0093] (2) Place A, B, C, and D in another container, wherein A is ceramide 3B with a mass of 50 parts; B is hydrogenated lecithin with a mass of 10 parts; C is sucrose stearate with a mass of 10 parts; and D is decaglycerol monostearate with a mass of 30 parts. Stir the mixture evenly to form an oil phase for later use. The total mass of A, B, C, and D is 5% of the mass of the hot water phase in step (1). Add the oil phase to the container in step (1) for homogenization or stirring. During homogenization or stirring, first maintain the temperature of the mixture at 120°C for 30 minutes at a speed of 200 rpm, and then cool it down to 95°C and maintain it for 4 hours to obtain a uniform mixed emulsion.

[0094] (3) The mixed emulsion obtained in step (2) is kept at a constant temperature of 80-90℃ and added to the ice-water phase (the total mass of A, B, C, and D is 10% of the mass of the ice-water phase). The mixture is added dropwise while stirring at a speed of 300 rpm. The temperature of the mixed system is kept below 20℃ throughout the process to obtain a thinner emulsion.

[0095] (4) The dilute emulsion obtained in step (3) is freeze-dried to obtain a composite powder with high water dispersibility.

[0096] Example 3

[0097] A method for preparing a composite powder with high water dispersibility includes the following steps:

[0098] (1) Place A, B, C, and D in the same container, wherein A is ceramide 2 with a mass of 50 parts; B is sunflower phospholipid with a mass of 10 parts; C is sucrose palmitate with a mass of 10 parts; and D is decaglycerol monostearate with a mass of 30 parts. Heat the container to 130°C and melt the four substances simultaneously in the container. Stir until a homogeneous mixture is obtained, which will be used as the molten oil phase for later use.

[0099] (2) Take pure water into another container and heat it to 95°C as a hot water phase for later use. The ratio of the mass of the hot water phase to the mass of the molten oil phase in step (1) is 9:1.

[0100] (3) Add the molten oil phase obtained in step (1) to the hot water phase in step (2) for homogenization or stirring. During homogenization or stirring, maintain the temperature of the mixed system at 85-95℃ and the rotation speed at 14000rpm. After the molten oil phase in step (1) is added, continue homogenization or stirring for 2-5 minutes to obtain a mixed emulsion.

[0101] (4) The mixed emulsion obtained in step (3) is kept at a constant temperature of 80-90°C and added to the ice-water phase. The total mass of A, B, C, and D is 10% of the mass of the ice-water phase. The mixture is stirred continuously, and the temperature of the mixed system is kept below 20°C throughout the process to obtain a thinner emulsion.

[0102] (5) The dilute emulsion obtained in step (4) is freeze-dried to obtain a composite powder with high water dispersibility.

[0103] Example 4

[0104] A method for preparing a composite powder with high water dispersibility includes the following steps:

[0105] (1) Place A, B, C and D in the same container, wherein A is 50 parts by mass of phytosphingosine; B is 10 parts by mass of soybean lecithin; C is 10 parts by mass of sucrose citrate; and D is 30 parts by mass of decaglycerol monostearate. Heat to 130°C and melt the four substances simultaneously in the container. Stir until a homogeneous mixture is obtained, which will be used as the molten oil phase for later use.

[0106] (2) Take pure water into another container and heat it to 95°C as a hot water phase for later use. The ratio of the mass of the hot water phase to the mass of the molten oil phase in step (1) is 9:1.

[0107] (3) Add the molten oil phase obtained in step (1) to the hot water phase in step (2) for homogenization or stirring. During homogenization or stirring, maintain the temperature of the mixed system at 85-95℃ and the rotation speed at 14000rpm. After the molten oil phase in step (1) is added, continue homogenization or stirring for 2-5 minutes to obtain a mixed emulsion.

[0108] (4) The mixed emulsion obtained in step (3) is kept at a constant temperature of 80-90°C and added to the ice-water phase. The total mass of A, B, C, and D is 10% of the mass of the ice-water phase. The mixture is stirred continuously, and the temperature of the mixed system is kept below 20°C throughout the process to obtain a thinner emulsion.

[0109] (5) The dilute emulsion obtained in step (4) is freeze-dried to obtain a composite powder with high water dispersibility.

[0110] Example 5

[0111] This embodiment uses the same preparation method as Example 1, but the components are different; wherein, A is ceramide 3, with a mass fraction of 50 parts; B is sunflower phospholipid, with a mass fraction of 10 parts; C is sucrose palmitate, with a mass fraction of 10 parts; and D is decaglycerol monostearate, with a mass fraction of 30 parts.

[0112] The final product is a composite powder with high water dispersibility.

[0113] Example 6

[0114] This embodiment has the same components and mass ratios as Example 1, but the preparation methods are not exactly the same;

[0115] A method for preparing a composite powder with high water dispersibility includes the following steps:

[0116] (1) Place A, B, C and D in the same container, heat the container to 150°C, melt the four substances in the container, stir until a uniform mixture is obtained, and use it as the molten oil phase for later use;

[0117] (2) Take pure water into another container and heat it to 85°C to prepare it as a hot water phase. The ratio of the mass of the hot water phase to the mass of the molten oil phase in step (1) is 15:1.

[0118] (3) Add the molten oil phase obtained in step (1) to the hot water phase in step (2) for homogenization or stirring. During homogenization or stirring, maintain the temperature of the mixed system at 85°C and the rotation speed at 10000 rpm. After the molten oil phase in step (1) is added, continue homogenization or stirring for 2-5 minutes to obtain a mixed emulsion.

[0119] (4) The mixed emulsion obtained in step (3) is kept at a constant temperature of 90°C and added to the ice-water phase. The total mass of A, B, C, and D is 10% of the mass of the ice-water phase. Stir continuously and keep the temperature of the mixed system below 20°C throughout the process to obtain a thinner emulsion.

[0120] (5) The dilute emulsion obtained in step (4) is freeze-dried to obtain a composite powder with high water dispersibility.

[0121] Example 7

[0122] The preparation method of the composite powder with high water dispersibility in this embodiment is the same as that in Example 1;

[0123] However, the component mass ratios are different; among them, A is ceramide 3B, with a mass fraction of 70 parts; B is hydrogenated lecithin, with a mass fraction of 5 parts; C is sucrose stearate, with a mass fraction of 5 parts; and D is decaglycerol monostearate, with a mass fraction of 10 parts.

[0124] The final product is a composite powder with high water dispersibility.

[0125] Example 8

[0126] The preparation method of the composite powder with high water dispersibility in this embodiment is the same as that in Example 1;

[0127] However, the component mass ratios are different; among them, A is ceramide 3B, with a mass fraction of 20 parts; B is hydrogenated lecithin, with a mass fraction of 20 parts; C is sucrose stearate, with a mass fraction of 30 parts; and D is decaglycerol monostearate, with a mass fraction of 50 parts.

[0128] The final product is a composite powder with high water dispersibility.

[0129] Comparative Example 1

[0130] (1) In this comparative example, the components A, B, C, and D, as well as their mass ratios, are the same as in Example 1. Substances A, B, and C are weighed into beaker 1 according to the formula ratio, and substance D is weighed into beaker 2.

[0131] Beaker No. 1: Heat the oil bath to 130°C, and melt the three substances simultaneously in the oil bath while stirring until a homogeneous mixture is obtained. Pour the mixture into beaker No. 1 as the molten oil phase for later use.

[0132] Beaker No. 2: Heat the water bath to 95°C, heat the pure water to 95°C, pour it into beaker No. 2, then add D into beaker No. 2, maintain the temperature at 85-95°C, rotate at 200 rpm, disperse evenly, and use it as the hot water phase for later use;

[0133] (2) The molten oil phase obtained in step (1) is added dropwise to the hot water phase obtained in step (2) for homogenization or stirring. During the homogenization or stirring process, the temperature of the mixed system is maintained at 85-95℃ and the rotation speed is 14000rpm. After the molten oil phase in step (1) is added, continue to homogenize or stir for 2-5 minutes to obtain a mixed emulsion.

[0134] (3) The above mixed emulsion is kept at a constant temperature of 80-90℃ and added dropwise to the ice-water phase while being added dropwise and stirred at a speed of 300 rpm. The temperature of the mixed system is kept below 20℃ throughout the process to obtain a thinner emulsion.

[0135] (4) The above-obtained dilute emulsion is freeze-dried to obtain powder.

[0136] Particle size testing was performed; for details on particle size and distribution, please refer to [link / reference]. Figure 4 Because it did not meet expectations, stability testing of the powder-aqueous dispersion was not conducted.

[0137] Comparative Example 2

[0138] (1) The components A, B, C, and D, as well as their mass ratios, are the same in this comparative example as in Example 1. Substances A, B, and D are weighed into beaker 1 according to the formula ratio, and substance C is weighed into beaker 2.

[0139] Beaker No. 1: Heat the oil bath to 130°C, and melt the three substances simultaneously in the oil bath while stirring until a homogeneous mixture is obtained. Pour the mixture into beaker No. 1 as the molten oil phase for later use.

[0140] Beaker No. 2: Heat the water bath to 95°C, heat the pure water to 95°C, pour it into beaker No. 2, then add C to beaker No. 2, maintain the temperature at 85-95°C, rotate at 200 rpm, disperse evenly, and use it as the hot water phase for later use;

[0141] (2) The molten oil phase obtained in step (1) is added dropwise to the hot water phase obtained in step (2) for homogenization or stirring. During the homogenization or stirring process, the temperature of the mixed system is maintained at 85-95℃ and the rotation speed is 14000rpm. After the molten oil phase in step (1) is added, continue to homogenize or stir for 2-5 minutes to obtain a mixed emulsion.

[0142] (3) The above mixed emulsion is kept at a constant temperature of 80-90℃ and added dropwise to the ice-water phase while being added dropwise and stirred at a speed of 300 rpm. The temperature of the mixed system is kept below 20℃ throughout the process to obtain a thinner emulsion.

[0143] (4) The above-obtained dilute emulsion is freeze-dried to obtain powder.

[0144] Particle size testing was performed; for details on particle size and distribution, please refer to [link / reference]. Figure 5 The result was not as expected; no stability test was conducted on the powder-aqueous dispersion.

[0145] Comparative Example 3

[0146] (1) Take ethanol and heat it to 80°C;

[0147] (2) The components A, B, C, D and their mass ratios in this comparative example are the same as in Example 1. Weigh substances A, B, C, and D according to the formula ratio, add them to ethanol (the mass ratio of ethanol to the total mass of A, B, C, and D is 9:1), keep the rotation speed at 300 rpm, and stir until the ethanol solution is completely clear and transparent.

[0148] (3) Evaporate the ethanol by rotary evaporation and obtain a viscous substance on the wall of the rotary evaporation flask. Add 90 ml of pure water (40℃) to the rotary evaporation flask. The mass ratio of ethanol to the total mass of A, B, C and D is 9:1. Shake at 2000 rpm until the viscous substance is completely dispersed in the water.

[0149] (4) Take out the dispersion from step (3) and homogenize it at 13000 rpm for 2-5 min to obtain an emulsion;

[0150] (5) The above emulsion is freeze-dried to obtain powder.

[0151] Comparative Example 4

[0152] Similar to the steps in Example 1, the only difference is that in step (4), water at 25°C is used instead of ice water, and the temperature of the mixing system is maintained at 25°C throughout the process. The other steps are the same as in Example 1.

[0153] The final powder has a large and uneven particle size, poor water dispersibility, and unstable water dispersion, making it prone to flocculent precipitation.

[0154] Comparative Example 5

[0155] Similar to the steps in Example 1, except that in step (1), the temperature is raised to 80°C for melting, and the other steps are the same as in Example 1.

[0156] In step (1), when the temperature is raised to 80°C, components A, B, C, and D cannot melt well, resulting in some unmelted or incompletely melted substances. Furthermore, the components cannot be mixed uniformly, affecting the subsequent preparation of the composite powder and leading to the failure of the composite powder preparation.

[0157] The resulting powder has uneven particle size, poor water dispersibility, and unstable water dispersion.

[0158] Performance testing

[0159] 1. The particle size was measured using a particle size analyzer. See the particle size test results for details. Figure 1-5 .

[0160] 2. Water dispersibility test of ceramide complex powder

[0161] The powders obtained in Examples 1, 2, and 3 were dispersed in water to prepare an aqueous dispersion of the powder with a mass fraction of 0.5%. The initial dispersion state was as follows: Figure 6 As shown.

[0162] Example 1: The white powder exhibits good water dispersibility: it can be dispersed into a homogeneous phase at room temperature (10-30℃) with stirring at 200 rpm, and also dispersed into a homogeneous phase with heating at 40℃ and stirring at 200 rpm. The dispersion is clear and slightly transparent, and the homogeneous phase shows a slight blue sheen, indicating that the powder particles in the aqueous dispersion are small. After dispersing for 10 minutes... Figure 7 As shown.

[0163] Example 2: A homogeneous phase can be dispersed in water by stirring at 200 rpm at room temperature (10-30℃). A homogeneous phase can also be dispersed by stirring at 200 rpm while heating at 40℃, with low transparency and no blue light. Dispersion for 10 minutes... Figure 7 As shown.

[0164] Comparative Example 3: At room temperature (10-30℃), stirring at 200 rpm resulted in a homogeneous water dispersion. Heating at 40℃ and stirring at 200 rpm also resulted in a homogeneous dispersion with low transparency and no blue light. Dispersion for 10 minutes showed... Figure 7 As shown.

[0165] The above Figure 6 and Figure 7 In the image, the left side shows the aqueous dispersion of the powder prepared in Comparative Example 3, the middle side shows the aqueous dispersion of the powder prepared in Example 2, and the right side shows the aqueous dispersion of the powder prepared in Example 1.

[0166] 3. Stability test of aqueous dispersion of ceramide complex powder

[0167] 3.1 Stability Test: Placed at room temperature for 3 days

[0168] Figure 8 The image shows the state of the aqueous dispersion of the powder prepared in Comparative Example 3 after being placed at room temperature for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0169] Figure 9 The image shows the state of the aqueous dispersion of the powder prepared in Example 2 after being placed at room temperature for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0170] Figure 10 The image shows the state of the aqueous dispersion of the powder prepared in Example 1 after being placed at room temperature for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0171] Depend on Figure 8-10 It can be seen that:

[0172] 1) The aqueous dispersion of the powder prepared in Example 1 remained clear and transparent after being left at room temperature for 3 days, and the powder was uniformly dispersed in water.

[0173] 2) The aqueous dispersion of the powder prepared in Comparative Example 3 showed no significant changes after being left at room temperature for 3 days.

[0174] 3) The aqueous dispersion of the powder prepared in Example 2 showed no significant changes after being left at room temperature for 3 days.

[0175] 3.2 Stability Test: Refrigerated at 4℃ for 3 days

[0176] Figure 11 The image shows the state of the aqueous dispersion of the powder prepared in Comparative Example 3 after being refrigerated at 4°C for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0177] Figure 12 The image shows the state of the aqueous dispersion of the powder prepared in Example 2 after being refrigerated at 4°C for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0178] Figure 13 The image shows the state of the aqueous dispersion of the powder prepared in Example 1 after being refrigerated at 4°C for 3 days. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0179] Depend on Figure 11-13 It can be seen that:

[0180] 1) The aqueous dispersion of the powder prepared in Example 1 remained clear after being refrigerated for 3 days, with no significant change in transparency, and the powder was uniformly dispersed in water.

[0181] 2) The aqueous dispersion of the powder prepared in Comparative Example 3 showed a large amount of white flocculent precipitate after being refrigerated for 3 days.

[0182] 3) The aqueous dispersion of the powder prepared in Example 2 was refrigerated for 3 days, and white flocculent matter precipitated out. The mass of the precipitate was less than that of Comparative Example 3.

[0183] 3.3 Stability test: Freeze-thaw at -20℃ for 3 days. After taking it out, wait for the sample to return to room temperature liquid state before observation.

[0184] Figure 14 The image shows the aqueous dispersion of the powder prepared in Comparative Example 3; the state diagram after freezing and thawing at -20℃ for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0185] Figure 15 The image shows an aqueous dispersion of the powder prepared in Example 2; the state diagram after freezing and thawing at -20°C for 3 days; from left to right, the mass fractions of the composite powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0186] Figure 16 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after freezing and thawing at -20°C for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0187] Depend on Figure 14-16 It can be seen that:

[0188] 1) The aqueous dispersion of the powder obtained in Example 1: exhibits a uniform dispersion state, with no solid precipitation and no stratification;

[0189] 2) The aqueous dispersion of the powder prepared in Comparative Example 3: white particles adhered to the bottle wall, a layer of white substance floated on the surface of the liquid, and after shaking, it turned into white flocculent precipitate.

[0190] 3) Aqueous dispersion of powder prepared in Example 2: White flocculent material precipitated in the sample, and the mass of the precipitate was less than that of Comparative Example 3.

[0191] 3.4 Stability Test: Placed at 40℃ for 3 days

[0192] Figure 17The image shows an aqueous dispersion of the powder prepared in Comparative Example 3; the state diagram after being placed at 40°C for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0193] Figure 18 The image shows an aqueous dispersion of the powder prepared in Example 2; the state diagram after being placed at 40°C for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0194] Figure 19 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after being placed at 40°C for 3 days; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0195] Depend on Figure 17-19 It can be seen that:

[0196] 1) The aqueous dispersion of the powder obtained in Example 1: exhibits a uniform dispersion state, with no solid precipitation and no stratification;

[0197] 2) The aqueous dispersion of the powder prepared in Comparative Example 3: white particles adhered to the bottle wall, a layer of white substance floated on the surface of the liquid, and after shaking, it turned into white flocculent precipitate.

[0198] 3) Aqueous dispersion of powder prepared in Example 2: White flocculent material precipitated in the sample, and the mass of the precipitate was less than that of Comparative Example 3.

[0199] 4. Stability test of ceramide complex powder aqueous dispersion (after 3 months of storage)

[0200] 4.1 Stability Test: After being placed at room temperature for 3 months

[0201] Figure 20 The image shows the state of the aqueous dispersion of the powder prepared in Example 1 after being placed at room temperature for 3 months. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0202] Depend on Figure 20 It can be seen that the aqueous dispersion of the powder prepared in Example 1 remained clear after being left at room temperature for 3 months, with no significant change in transparency, and the powder was uniformly dispersed in water.

[0203] The aqueous dispersion of the powder prepared in Comparative Example 3 showed solid precipitation after being left at room temperature for 3 months.

[0204] 4.2 Stability Test: After being refrigerated at 4℃ for 3 months

[0205] Figure 21The image shows the state of the aqueous dispersion of the powder prepared in Example 1 after being refrigerated at 4°C for 3 months. From left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0206] Depend on Figure 21 It can be seen that the aqueous dispersion of the powder prepared in Example 1 still maintains a uniform dispersion state after being refrigerated for 3 months.

[0207] 4.3 Stability test: After freezing and thawing for 3 months at -20℃, the sample was taken out and observed after it returned to room temperature liquid state.

[0208] Figure 22 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after 3 months of freeze-thaw cycles at -20°C; from left to right, the mass fractions of the composite powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0209] Depend on Figure 22 It can be seen that the aqueous dispersion of the powder prepared in Example 1 still maintains a uniform dispersion state, with no solid precipitation or stratification.

[0210] 4.4 Stability Test: After being placed at 40℃ for 3 months

[0211] Figure 23 The image shows an aqueous dispersion of the powder prepared in Example 1; the state diagram after being placed at 40°C for 3 months; from left to right, the mass fractions of the complex powder in the aqueous dispersion are 0.1%, 0.5%, and 1%, respectively.

[0212] Depend on Figure 23 It can be seen that the aqueous dispersion of the powder prepared in Example 1 still maintains a uniform dispersion state, with no solid precipitation or stratification.

[0213] Application examples

[0214]

[0215]

[0216] The powder obtained in Example 1 was added to the subsequent formulation as shown in the table above, and finally a ceramide-containing emulsion was obtained. No ceramide precipitation occurred during the preparation process, and the compatibility of each component was good. The obtained ceramide emulsion had good skin feel, moisturizing properties and permeability, which is conducive to skin absorption and allows the active ingredient (ceramide) to fully exert its efficacy.

[0217] As can be seen from the above, the solution provided by the embodiments of the present invention has the following advantages and features:

[0218] (1) The preparation method of the present invention is relatively reasonable and can produce composite powder with small and uniform particle size, and the content of effective components (ceramides or phytosphingosines) in the composite powder is high. In addition, the preparation method is simple to operate and is suitable for the preparation of large quantities of ceramide or phytosphingosine composite powder.

[0219] (2) The composite powder prepared by the method of the present invention has good water dispersibility and its aqueous dispersion has high stability. When added to subsequent formulations, it will not precipitate, which is conducive to the penetration of ceramides or phytosphingosine into the skin to exert their effects, enhance the skin barrier, protect the skin, and resist some external stimuli.

[0220] (3) The composite powder prepared by the method of the present invention is easy to package, store and transport, and is relatively stable, not easily deteriorated, and easy to use and develop in subsequent formulations. Existing water-dispersible composition systems are usually in solution form, which are not easy to package, are prone to bacterial growth, have short shelf life and are not easy to transport.

[0221] (4) The composite powder prepared by this invention has a high content of effective components (ceramides or phytosphingosines), up to 78%, without introducing excessive amounts of other substances and without affecting the preparation of subsequent formulations. In contrast, the composites prepared in the prior art have a lower content of effective components, with a maximum of 10%, which is disadvantageous for the preparation of subsequent formulations because using ceramides or phytosphingosines introduces more other substances.

[0222] The above are merely preferred embodiments of the present invention and are not intended to limit the present invention. Various modifications and variations can be made to the present invention by those skilled in the art. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the scope of protection of the present invention.

Claims

1. A method for producing a composite having high water dispersibility, characterized by, It comprises: The oil phase containing non-water-soluble compound, amphiphilic substance, at least two surfactants is mixed with water phase to obtain mixed emulsion, and then the mixed emulsion is diluted to obtain complex with high water dispersibility.

2. The production method according to claim 1, characterized by, It comprises: The oil phase containing non-water-soluble compound, amphiphilic substance, at least two surfactants is mixed with water phase to obtain mixed emulsion, and then the mixed emulsion is diluted to obtain complex with high water dispersibility.

3. The production method according to claim 2, characterized by, The non-water-soluble compound in the oil phase is non-water-soluble ceramide and / or sphingosine; Preferably, the non-water-soluble ceramide includes at least one of non-water-soluble ceramide, its derivative and its analogue, and the non-water-soluble sphingosine includes at least one of non-water-soluble sphingosine, its derivative and its analogue; Preferably, the non-water-soluble sphingosine includes at least one of sphingosine, phytosphingosine, tetraacetyl phytosphingosine, N-acetyl phytosphingosine, salicyl phytosphingosine; Preferably, the non-water-soluble ceramide includes at least one of ceramide 3, ceramide 3B, ceramide 2, ceramide 1, ceramide 4, ceramide 5, ceramide 6, ceramide 7, ceramide 8, ceramide 9, ceramide 10, ceramide 11; Preferably, the amphiphilic substance includes at least one of hydrogenated lecithin, sunflower lecithin, soybean lecithin, lecithin, lysophospholipid; Preferably, the HLB value of the sucrose ester surfactant is 8-18, preferably 10-16; preferably, the sucrose ester surfactant includes at least one of sucrose citrate, sucrose palmitate, sucrose laurate, sucrose stearate; Preferably, the HLB value of the polyglyceryl ester surfactant is 10-16, preferably 10-13; preferably, the polyglyceryl ester surfactant includes at least one of polyglyceryl monostearate, decaglyceryl monostearate, triglyceryl monostearate, polyglyceryl-4 stearate; Preferably, the mass fraction of the non-water-soluble compound in the oil phase is 20-70 parts, the mass fraction of the amphiphilic substance is 5-20 parts, the mass fraction of the sucrose ester surfactant is 5-30 parts, and the mass fraction of the polyglyceryl ester surfactant is 10-50 parts; Preferably, the mass fraction of the non-water-soluble compound is 35-65 parts, more preferably 40-60 parts; Preferably, the mass fraction of the amphiphilic substance is 5-15 parts, more preferably 6-12 parts; Preferably, the mass fraction of the sucrose ester surfactant is 10-20 parts, more preferably 12-18 parts; Preferably, the mass fraction of the polyglyceryl ester surfactant is 20-40 parts, more preferably 25-35 parts.

4. The production method according to claim 2, characterized by, The preparation of the mixed emulsion includes: adding the molten oil phase into the hot water phase for homogenization or stirring, and continuing the homogenization or stirring after the addition of the molten oil phase is completed to obtain a uniform mixed emulsion. Preferably, the preparation of the molten oil phase comprises: mixing the non-water-soluble compound, the amphiphilic substance, the sucrose ester surfactant and the polyglycerol ester surfactant in a mass ratio, heating to 90-200℃ to melt the four substances, and stirring until a uniform solution is obtained, wherein: the melting temperature is 120-200℃, preferably the melting temperature is 130-190℃, and further preferably 130-160℃; the melting time is 25-70min, preferably the melting time is 30-60min; Preferably, the temperature of the hot water phase is 80-95℃; Preferably, the preparation of the mixed emulsion comprises: adding the molten oil phase to the hot water phase at 80-95℃ for homogenization or stirring, and during the homogenization or stirring, the temperature of the mixed system is maintained at 80-95℃, and the rotation speed is 7000-50000rpm; after the addition of the molten oil phase is completed, the homogenization or stirring is continued to obtain the mixed emulsion; the mass ratio of the hot water phase to the molten oil phase is 5:1-15:

1.

5. The preparation method according to claim 2, characterized in that, The preparation of the mixed emulsion comprises: adding the oil phase to the hot water phase for homogenization or stirring, and after the addition of the oil phase is completed, the homogenization or stirring is continued to obtain a uniform mixed emulsion; Preferably, the preparation of the oil phase comprises: mixing the non-water-soluble compound, the amphiphilic substance, the sucrose ester surfactant and the polyglycerol ester surfactant in a mass ratio; Preferably, the temperature of the hot water phase is 110-150℃; Preferably, the preparation of the mixed emulsion comprises: adding the oil phase to the hot water phase at 110-150℃ for homogenization or stirring, and during the homogenization or stirring, the temperature of the mixed system is maintained at 100-150℃, the rotation speed is 100-300rpm, and the time is 10-60min; then the temperature is lowered to 85-95℃ for further homogenization or stirring for 4-12h to obtain a uniform mixed emulsion; the mass of the oil phase is 0.1-30% of the mass of the hot water phase.

6. The production method according to claim 1 or 2, characterized by, The specific steps of diluting the mixed emulsion are: adding the mixed emulsion to the ice water phase for stirring to obtain a diluted emulsion; Preferably, the total mass of the non-water-soluble compound, the amphiphilic substance and the at least two surfactants is 0.1-30% of the mass of the ice water phase, preferably 1-25%, and more preferably 10-20%; Preferably, the temperature of the ice water phase is lower than 20℃; Preferably, the preparation of the diluted emulsion comprises: maintaining the temperature of the mixed emulsion at 60-100℃, adding the mixed emulsion to the ice water phase for stirring, and during the dilution, the temperature of the mixed system is maintained at lower than 20℃ to obtain the diluted emulsion.

7. A method for producing a composite powder having high water dispersibility, characterized by, comprises: The diluted mixed emulsion prepared by the preparation method of any one of claims 1-6 is freeze-dried to obtain a complex powder with high water dispersibility.

8. A composite powder having high water dispersibility, characterized by, The complex powder is prepared by the preparation method of claim 7, and the content of the ceramide and / or sphingosine in the complex powder with high water dispersibility is 16-78%.

9. Use of the composite with high water dispersibility prepared by the preparation method according to any one of claims 1-6 or the composite powder with high water dispersibility prepared by the preparation method according to claim 7 or the composite powder with high water dispersibility according to claim 8 in the preparation of daily-use cosmetics or medicines.

10. Use according to claim 9, characterized in that, The daily-use cosmetics include at least one of facial cleanser, skin care water, skin care milk, skin care cream, hair care milk and hair care water, the medicines include skin treatment medicines, and the dosage forms of the daily-use cosmetics and medicines include any one or several of ointment, paste, emulsion, gel, solution, suspension, emulsion, patch, spray.