Stable emulsion as well as preparation method and application thereof

Abstract

The invention discloses a stable emulsion as well as a preparation method and application thereof. According to the composition, the hydrogenated lecithin, the emulsion stabilizer, the medium and high polarity grease, the anionic surfactant, the thickening agent, the pH regulator and other components are compounded, so that low-water-solubility substances can be uniformly dispersed in water and are not easy to separate out, precipitate or layer, and the stability of the composition is improved; meanwhile, the bioavailability of low-water-solubility substances can be improved, so that the efficacy advantages of the low-water-solubility substances can be fully exerted. The emulsion prepared by mixing the composition provided by the invention with low-water-solubility substances has the characteristics of stability and difficulty in deterioration, is fine and uniform in use, and is easy to push away and absorb. Therefore, the composition disclosed by the invention has a good application prospect in the fields of cosmetics and medicines.

Description

Technical Field

[0001] This invention relates to the fields of daily chemical products and pharmaceutical technology, and more specifically, to a stable emulsion, its preparation method, and its application. Background Technology

[0002] Phytosphingosine, also known as neurosphingosine, is chemically named 2-amino-1,3,4-octadecanetriol. It belongs to the sphingolipid class and is an important component of cell membranes. As a natural lipid-active ingredient, phytosphingosine exhibits unique bioactivity in the cosmetics field. Its molecular structure is highly similar to the sphingolipids in the stratum corneum of human skin, and it can achieve multiple effects such as moisturizing and repairing, soothing sensitivity, and anti-aging by replenishing epidermal lipids, enhancing barrier function, and regulating inflammatory responses. Related studies have found that phytosphingosine has highly effective inhibitory activity against various harmful bacteria, including Staphylococcus aureus, Propionibacterium acnes, and Malassezia. These microorganisms are closely related to atopic dermatitis, acne, and seborrheic dermatitis.

[0003] In recent years, with the increasing demand from consumers for natural and gentle functional ingredients, the application of phytosphingosine in emulsions, creams, and other systems has attracted much attention. However, phytosphingosine faces significant challenges in practical formulation applications: First, its molecular structure contains both hydrophobic long chains and hydrophilic polar groups, resulting in complex distribution behavior in the oil-water two-phase system, making it difficult to achieve stable and uniform dispersion. This can easily lead to poor emulsification, crystallization, coarsening of the material, or system stratification; consequently, the efficacy of phytosphingosine is greatly reduced, making it difficult to fully realize its efficacy advantages.

[0004] Similarly, derivatives of phytosphingosine, such as tetraacetylphytosphingosine and triacetylphytosphingosine, are also insoluble in water, making them unsuitable for practical formulations. Even when added to a formulation, they cannot fully exert their effects. Therefore, developing a formulation that is stable over a long period and can fully exert the efficacy of low-water-soluble active ingredients has become a key issue that the industry urgently needs to address.

[0005] In view of this, the present invention is proposed. Summary of the Invention

[0006] The purpose of this invention is to provide a stable emulsion, its preparation method, and its application. The composition of this invention can improve the stability of low water-soluble substances such as phytosphingosine and its derivatives in emulsion systems, thereby improving the bioavailability of phytosphingosine and allowing it to fully exert its efficacy advantages.

[0007] This invention is implemented as follows: In a first aspect, the present invention provides a composition for improving the stability of low water-soluble substances, comprising, by weight: 2-2.5 parts hydrogenated lecithin, 2-4 parts emulsifying stabilizer, 5-16 parts medium- to high polarity oil, 0.3-0.6 parts anionic surfactant, 0.5-1.5 parts thickener, and 0.35-0.45 parts pH adjuster.

[0008] In a second aspect, the present invention provides the use of the above composition in improving the stability of a low-water-soluble substance selected from at least one of phytosphingosine, acetyl phytosphingosine, diacetyl phytosphingosine, tetraacetyl phytosphingosine, and triacetyl phytosphingosine.

[0009] Thirdly, the present invention provides a stable emulsion comprising the above-described composition, a low-water-soluble substance, and water, wherein the mass ratio of the low-water-soluble substance to water is 0.1~1:55.15~88.05.

[0010] Fourthly, the present invention provides a method for preparing the above-mentioned stable emulsion, comprising: Hydrogenated lecithin, emulsifying stabilizer, low water-soluble substance, and medium-to-high polarity oil are mixed in a certain proportion, and the resulting oil phase mixture is heated to 70-85°C while stirring. Deionized water, anionic surfactant, and thickener are mixed in a certain proportion, and the resulting aqueous phase mixture is heated to 70-85°C while stirring. The oil phase mixture at 70-85°C is mixed with the aqueous phase mixture, homogenized, and then cooled to 20-45°C. A pH adjuster is then added. After mixing thoroughly, a stable emulsion is obtained.

[0011] Fifthly, the present invention provides the application of the above-mentioned stable emulsion in the preparation of daily chemical products and pharmaceuticals, wherein the daily chemical products include skin care products; and the pharmaceuticals include medicines for treating skin.

[0012] The present invention has the following beneficial effects: (1) The present invention obtains a composition by compounding components such as hydrogenated lecithin, emulsifying stabilizer, medium and high polarity oil, anionic surfactant, thickener and pH adjuster. This composition can make low water-soluble substances uniformly dispersed in water, making it difficult for them to precipitate or separate into layers, thus improving their stability. At the same time, it can improve the bioavailability of low water-soluble substances, allowing them to fully exert their efficacy advantages.

[0013] (2) The emulsion prepared by mixing the composition of the present invention with a low water-soluble substance and using the preparation method of the present invention is stable and not easily deteriorated. Moreover, it is relatively fine and uniform when used, and is easy to spread and absorb. Therefore, the composition of the present invention has good application prospects in the fields of cosmetics and pharmaceuticals containing low water-soluble substances. Attached Figure Description

[0014] 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.

[0015] Figure 1 The stability results of the emulsion prepared in Example 1 under different temperature conditions; Figure 2 The stability results of the emulsion prepared in Example 2 under different temperature conditions; Figure 3 The stability results of the emulsion prepared in Example 3 under different temperature conditions; Figure 4 The results show the stability of the emulsion prepared in Example 4 under different temperature conditions; Figure 5 The stability results of the emulsion prepared in Example 5 under different temperature conditions; Figure 6 The stability results of the emulsion prepared in Example 6 under different temperature conditions; Figure 7 The stability results of the emulsion prepared in Example 7 under different temperature conditions; Figure 8 The stability results of the emulsion prepared in Example 8 under different temperature conditions; Figure 9 The stability results of the emulsion prepared in Example 12 under different temperature conditions; Figure 10 A schematic diagram of the emulsion prepared in Comparative Example 1; Figure 11 A schematic diagram of the emulsion prepared in Comparative Example 2; Figure 12 A schematic diagram of the emulsion prepared in Comparative Example 3; Figure 13 A schematic diagram of the emulsion prepared in Comparative Example 4; Figure 14 A schematic diagram of the emulsion prepared in Comparative Example 5; Figure 15 The stability results are for Comparative Example 8; Figure 16 This is a schematic diagram of the initial application of the emulsion prepared in Example 2 onto the skin. Detailed Implementation

[0016] 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.

[0017] In view of the excellent efficacy of phytosphingosine and its derivatives in the field of skin care, as well as their shortcomings of being difficult to disperse evenly in emulsion systems and having low bioavailability, the present invention provides a composition that can stably disperse them. The composition mainly consists of hydrogenated lecithin, emulsion stabilizer, medium to high polarity oil, anionic surfactant, thickener and pH adjuster.

[0018] Specifically, by weight, the composition comprises: 2-2.5 parts hydrogenated lecithin, 2-4 parts emulsifying stabilizer, 5-16 parts medium- to high-polarity oil, 0.3-0.6 parts anionic surfactant, 0.5-1.5 parts thickener, and 0.35-0.45 parts pH adjuster.

[0019] In some embodiments, the emulsifying stabilizer is selected from at least one of cetearyl alcohol, cetyl alcohol, stearyl alcohol, or behenyl alcohol.

[0020] In some embodiments, the medium-to-high polarity oil is selected from at least one of octyl dodecanol, caprylic / capric triglyceride (GTCC), isopropyl myristate, isononyl isononanoate, and ethylhexyl palmitate.

[0021] By combining specific emulsifying stabilizers, medium- to high-polarity oils, and other components in this invention, the stability of low-water-soluble substances can be synergistically improved, making them uniformly dispersed and less prone to precipitation and stratification.

[0022] In some embodiments, the anionic surfactant is an anionic surfactant with an HLB value between 18 and 25.

[0023] In some embodiments, the anionic surfactant is selected from at least one of sodium cocoyl methyl taurate, sodium stearoyl taurate, disodium lauryl sulfosuccinate, disodium poissonyl ether sulfosuccinate, and sodium methyl stearoyl taurate (NIKKOL SMT).

[0024] In some embodiments, the thickener includes SIMULGEL INS 100 (hydroxyethyl acrylate / sodium acryloyl dimethyl taurate copolymer & isohexadecane & polysorbate-60 & water & sorbitan isostearate).

[0025] In some embodiments, the pH adjuster is an acidic adjuster. More preferably, the pH adjuster is selected from at least one of a 10 wt% aqueous solution of citric acid and lactic acid.

[0026] Experiments have shown that the above composition enables poorly water-soluble substances to be uniformly dispersed and stably exist in water; therefore, the composition can be used to improve the stability of poorly water-soluble substances. Thus, the present invention can also provide the application of the above composition in improving the stability of poorly water-soluble substances.

[0027] In some embodiments, the low water-soluble substance is phytosphingosine and its derivatives; more preferably, the low water-soluble substance is selected from at least one of phytosphingosine, acetyl phytosphingosine, diacetyl phytosphingosine, tetraacetyl phytosphingosine, and triacetyl phytosphingosine.

[0028] In some embodiments, the mass ratio of the components in the composition is: low water-soluble substance: hydrogenated lecithin: emulsion stabilizer: medium-to-high polarity oil: anionic surfactant: thickener: pH adjuster = 0.1-1:2-2.5:2-4:5-16:0.3-0.6:0.5-1.5:0.35-0.45; preferably, low water-soluble substance: hydrogenated lecithin: emulsion stabilizer: medium-to-high polarity oil: anionic surfactant: thickener: pH adjuster = 0.2:2:3:11:0.5:1:0.4.

[0029] An optional technical solution is that, when adding a low water-soluble substance to the above composition, the components, by weight, are: 0.2 parts of the low water-soluble substance, 2 parts of hydrogenated lecithin, 3 parts of emulsifying stabilizer, 11 parts of medium-to-high polarity oil, 0.5 parts of anionic surfactant, 1 part of thickener, and 0.4 parts of pH adjuster.

[0030] According to the above applications, the present invention also provides a stabilized emulsion comprising the above composition, as well as a low water-soluble substance and water.

[0031] The mass ratio of the low water-soluble substance to water is 0.1~1:55.15~88.05; more preferably, the mass ratio of the low water-soluble substance to water is 0.2:76.9.

[0032] In some embodiments, the components of the stabilized emulsion, by weight, include: 0.1 to 1 part of low water-soluble substances, 55.15 to 88.05 parts of water, 2 to 2.5 parts of hydrogenated lecithin, 2 to 4 parts of stabilizer, 5 to 16 parts of medium to high polarity oils, 0.3 to 0.6 parts of anionic surfactant, 0.5 to 1.5 parts of thickener, and 0.35 to 0.45 parts of pH adjuster.

[0033] An alternative technical solution is that the mass ratio of low water-soluble substances, water, hydrogenated lecithin, emulsion stabilizer, medium-to-high polarity oils, anionic surfactant, thickener, and pH adjuster in the stabilized emulsion is 0.2:76.9:2:3:11:0.5:1:0.4.

[0034] In some embodiments, the stabilized emulsion further includes at least one of 1,2-hexanediol, component C, and component D, wherein component C is at least one of raspberry ketone and p-hydroxyacetophenone; and component D is at least one of butylene glycol, glycerol, dipropylene glycol, isopentyl glycol, and 1,3-propylene glycol.

[0035] 1,2-Hexanediol and component D both function as cosolvents and humectants in the stable emulsion of this invention, helping to evenly disperse the low water-soluble ingredients in the formulation and absorbing moisture from the environment and "locking" it onto the skin surface. Component C acts as a preservative, inhibiting the growth and reproduction of microorganisms. An alternative technical solution is that the components of the stabilized emulsion are low water-soluble substances, water, hydrogenated lecithin, emulsion stabilizer, medium to high polarity oils, anionic surfactants, thickeners, pH adjusters, and 1,2-hexanediol.

[0036] An alternative technical solution is that the components of the stabilized emulsion are low water-soluble substances, water, hydrogenated lecithin, emulsion stabilizer, medium to high polarity oils, anionic surfactants, thickeners, pH adjusters, and raspberry ketones.

[0037] An alternative technical solution is that the components of the stabilized emulsion are low water-soluble substances, water, hydrogenated lecithin, emulsion stabilizer, medium to high polarity oils, anionic surfactants, thickeners, pH adjusters, and butanediol.

[0038] An alternative technical solution is that the components of the stabilized emulsion are low water-soluble substances, water, hydrogenated lecithin, emulsion stabilizer, medium to high polarity oils, anionic surfactants, thickeners, pH adjusters, raspberry ketones, and butylene glycol.

[0039] An alternative technical solution is that the components of the stabilized emulsion are low water-soluble substances, water, hydrogenated lecithin, emulsion stabilizer, medium to high polarity oils, anionic surfactant, thickener, pH adjuster, 1,2-hexanediol, raspberry ketone, and butylene glycol.

[0040] In some embodiments, the mass ratio of the low water-soluble substance to 1,2-hexanediol is 0.1~1:0.3~0.8; more preferably, the mass ratio of the low water-soluble active substance to 1,2-hexanediol is 0.2:0.5.

[0041] In some embodiments, the mass ratio of the low water-soluble substance to component C is 0.1-1:0.3-0.8; more preferably, the mass ratio of the low water-soluble active ingredient to component C is 0.2:0.5.

[0042] In some embodiments, the mass ratio of the low water-soluble substance to component D is 0.1-1:1~10; more preferably, the mass ratio of the low water-soluble active ingredient to component D is 0.2:4.

[0043] The present invention also provides a method for preparing the above-mentioned stable emulsion, comprising: S1. Mix hydrogenated lecithin, emulsifying stabilizer, low water-soluble substance, and medium-to-high polarity oil in a certain proportion, and heat the resulting oil phase mixture to 70~85℃ while stirring. S2. Mix deionized water, anionic surfactant, and thickener in a certain proportion, and heat the resulting aqueous mixture to 70~85℃ while stirring. S3. Mix the oil phase mixture at 70~85℃ with the water phase mixture, homogenize, and then cool to 20~45℃ before adding the pH adjuster; after mixing, a stable emulsion is obtained.

[0044] In some embodiments, during the preparation of the aqueous mixture in S2, 1,2-hexanediol, component C, and component D are added in proportion.

[0045] In some embodiments, the homogenization conditions in S3 are a rotation speed of 5500 rpm and a time of 5 min.

[0046] The stable emulsion obtained by the above preparation method can be used to prepare daily chemical products and pharmaceuticals, wherein the daily chemical products include skin care products and the pharmaceuticals include drugs for treating skin diseases.

[0047] In some embodiments, skin care products include facial cleansers, shampoos, lotions, emulsions, creams, and hair conditioners.

[0048] The skin care products of the present invention can be prepared from any dosage form commonly prepared in the art, such as solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactants (including detergents), oils, powder foundations, emulsion foundations, wax foundations, and sprays, but are not limited thereto.

[0049] The carriers included in the skin care products of the present invention may utilize carriers commonly used in the art, depending on the dosage form.

[0050] When the dosage form of the present invention is an ointment, paste, cream or gel, the carrier component may be animal oil, vegetable oil, paste, paraffin, starch, amine gum, cellulose derivatives, polyethylene glycol, silicon, bentonite, silica, talc or zinc oxide, etc.

[0051] When the dosage form of the present invention is powder or spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder can be used as the carrier component.

[0052] When the dosage form of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol, especially cottonseed oil, peanut oil, corn germ oil, olive oil, castor oil and sesame oil, glycerol aliphatic esters, polyethylene glycol or sorbitan fatty acid esters.

[0053] When the dosage form of the present invention is a suspension, the carrier component may be a liquid diluent such as water, ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester, microcrystalline cellulose, aluminum meta-hydroxide, bentonite, agar or amine yellow gum, etc.

[0054] In the case of a facial cleanser containing surfactants in the formulation of the present invention, the carrier ingredients may include fatty alcohol sulfate, fatty alcohol ether sulfate, sulfosuccineic acid monoester, isethionate, imidazoline derivatives, methyl taurate, sarcosinate, fatty acid amide ether sulfate, alkyl amidobetaine, fatty alcohol, fatty acid glycerides, fatty acid diethanolamide, vegetable oils, lanolin derivatives, or ethoxylated glycerol fatty acid esters.

[0055] When the dosage form of the present invention is soap, the carrier components may include alkaline metal salts of fatty acids, fatty acid half-esters, fatty acid protein hydrolysates, hydroxyethyl sulfonates, lanolin derivatives, fatty alcohols, vegetable oils, glycerin, sugars, etc.

[0056] Similarly, the pharmaceutical products of the present invention can be prepared from any dosage form commonly prepared in the art, and the excipients contained in the pharmaceutical products of the present invention may be excipients commonly used in the art, depending on the dosage form, and will not be listed here.

[0057] The features and performance of the present invention will be further described in detail below with reference to embodiments.

[0058] The materials and instruments used in this invention can all be purchased commercially.

[0059] Example 1 A stabilized emulsion comprising the following raw material components in parts by weight:

[0060] This stable emulsion was prepared by the following method: 1) Weigh hydrogenated lecithin, cetearyl alcohol, phytosphoprotein, and octyldodecyl alcohol into an oil phase beaker according to the above proportions, mix them evenly, and heat to 80°C while stirring.

[0061] 2) Weigh deionized water, 1,2-hexanediol, raspberry ketone, NIKKOL SMT, and SIMULGEL INS 100 into an aqueous phase beaker according to the above proportions, mix well, and heat to 80°C while stirring.

[0062] 3) While homogenizing, slowly pour the material from the oil phase beaker into the water phase beaker, start homogenizing at 5500 rpm for 5 minutes, and start stirring and cooling after homogenization.

[0063] 4) When the temperature drops to 25℃, pour a 10wt% citric acid aqueous solution into a beaker and stir for 3-5 minutes.

[0064] 5) Stop stirring and discharge the material.

[0065] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 1 As shown.

[0066] Example 2 A stabilized emulsion comprising the following raw material components in parts by weight:

[0067] Preparation method: 1) Weigh hydrogenated lecithin, cetearyl alcohol, phytosphoprotein and octyldodecyl alcohol into an oil phase beaker according to the above proportions and mix them evenly. Heat to 80°C while stirring.

[0068] 2) Weigh deionized water, 1,2-hexanediol, raspberry ketone, butylene glycol, NIKKOL SMT, and SIMULGEL INS 100 into an aqueous phase beaker according to the above proportions, mix well, and heat to 80°C while stirring.

[0069] 3) While slowly homogenizing, slowly pour the material from the oil phase beaker into the water phase beaker, and start homogenizing at 5500 rpm for 5 minutes. After homogenization, start stirring and cooling.

[0070] 4) When the temperature drops to 25℃, pour 10wt% citric acid aqueous solution into a beaker and stir for 3~5 minutes.

[0071] 5) Stop stirring and discharge the material.

[0072] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 2 As shown.

[0073] Example 3 A stabilized emulsion comprising the following raw material components in parts by weight:

[0074] The preparation of the stable emulsion in this embodiment is consistent with the preparation method in Example 2. The difference between this embodiment and Example 2 is that isopropyl myristate is used instead of octyldodecyl alcohol.

[0075] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 3 As shown.

[0076] Example 4 A stabilized emulsion comprising the following raw material components in parts by weight:

[0077] The preparation method of the stable emulsion described in this embodiment is the same as that in Example 2. The difference between this embodiment and Example 2 is that 5 parts of octyldodecyl alcohol, 4 parts of GTCC, and 2 parts of isopropyl myristate are used.

[0078] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 4 As shown.

[0079] Example 5 In this embodiment, the components are the same as in Example 2, but the mass fraction of phytosphingosine is 0.5 parts, while the mass fractions of other components remain unchanged. Deionized water is added to make the total mass fraction of all components 100 parts.

[0080] The preparation method of the stabilized emulsion in this embodiment is the same as that in Example 2.

[0081] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 5 As shown.

[0082] Example 6 In this embodiment, the components are the same as in Example 2, but the mass fraction of phytosphingosine is 1 part, while the mass fractions of other components remain unchanged. Deionized water is added to make the total mass fraction of all components 100 parts.

[0083] The preparation method of the stabilized emulsion in this embodiment is the same as that in Example 2.

[0084] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 6 As shown.

[0085] Example 7 In this embodiment, an equal amount of behenol is used to replace cetearyl alcohol, and the preparation method is the same as in Example 2.

[0086] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 7 As shown.

[0087] Example 8 In this embodiment, an equal amount of ethylhexyl palmitate was used to replace octyldodecyl alcohol, and the preparation method was the same as in Example 2.

[0088] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows... Figure 8 As shown.

[0089] Example 9 In this embodiment, an equal amount of sodium cocoyl methyl taurate was used to replace NIKKOL SMT, and the preparation method was the same as in Example 2.

[0090] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃.

[0091] Example 10 In this embodiment, all components and their proportions are the same as in Example 2, and the preparation method includes the following steps: 1) Weigh hydrogenated lecithin, cetearyl alcohol, phytosphoprotein, and octyldodecyl alcohol into an oil phase beaker according to the above proportions, mix them evenly, and heat to 85°C while stirring.

[0092] 2) Weigh deionized water, 1,2-hexanediol, raspberry ketone, butylene glycol, NIKKOL SMT, and SIMULGEL INS 100 into an aqueous phase beaker according to the above proportions, mix well, and heat to 85°C while stirring.

[0093] 3) While slowly homogenizing, slowly pour the material from the oil phase beaker into the aqueous phase beaker, and start homogenizing at 5500 rpm for 5 minutes. After homogenization, start stirring and cooling.

[0094] 4) When the temperature drops to 40℃, pour 10wt% citric acid aqueous solution into a beaker and stir for 3~5 minutes.

[0095] 5) Stop stirring and discharge the material.

[0096] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃.

[0097] Example 11 In this embodiment, the components are the same as in Example 2, but the mass fractions are different, as shown below:

[0098] The preparation method of the stable emulsion in this embodiment is the same as that in Example 2. This embodiment can produce a uniform and stable emulsion. After stability testing, it is stable at -20℃ to room temperature cycling, 4℃, room temperature, and 45℃.

[0099] Example 12 In this embodiment, tetraacetyl phytosphingosine is used instead of phytosphingosine, and the other components and mass fractions are the same as in Example 2, and the preparation method is also the same as in Example 2.

[0100]

[0101] This embodiment can produce a uniform and stable emulsion. Stability tests showed that it was stable under cycling conditions from -20℃ to room temperature, at 4℃, at room temperature, and at 45℃. The stability test results are as follows: Figure 9 As shown.

[0102] Comparative Example 1 An emulsion comprising the following raw material components in parts by weight:

[0103] The preparation method of the emulsion described in this comparative example is the same as that in Example 2. The difference is that glyceryl stearate and PEG-55 stearate are used instead of hydrogenated lecithin. The resulting emulsion is as follows: Figure 10 As shown in the figure, the emulsion was initially uneven, with particles precipitating out.

[0104] Comparative Example 2 An emulsion comprising the following raw material components in parts by weight:

[0105] This comparative example does not contain NIKKOL SMT, and glyceryl stearate and PEG-55 stearate are used instead of hydrogenated lecithin. The emulsion preparation method is the same as that in Example 1; the resulting emulsion is as follows: Figure 11 As shown in the figure, the emulsion was initially uneven, with particles precipitating out.

[0106] Comparative Example 3 An emulsion comprising the following raw material components in parts by weight:

[0107] The preparation method of the stable emulsion described in this embodiment is the same as that in Example 1, and the resulting emulsion is as follows: Figure 12 As shown in the figure, the emulsion was initially uneven, with particles precipitating out.

[0108] Comparative Example 4 A stabilized emulsion comprising the following raw material components in parts by weight:

[0109] The preparation method of the stable emulsion described in this embodiment is the same as that in Example 1, and the resulting emulsion is as follows: Figure 13 As shown in the figure, the emulsion was initially uneven, with particles precipitating out.

[0110] Comparative Example 5 A stabilized emulsion comprising the following raw material components in parts by weight:

[0111] The preparation method of the emulsion described in this comparative example is the same as that in Example 1, and the resulting emulsion is as follows: Figure 14 As shown in the figure, the emulsion was initially uneven, with particles precipitating out.

[0112] Comparative Example 6 In this comparative example, the components and their mass fractions are the same as in Example 2, but the preparation methods are different.

[0113] The method for preparing an emulsion includes the following steps: 1) Weigh hydrogenated lecithin, cetearyl alcohol, phytosphoprotein, and octyldodecyl alcohol into an oil phase beaker according to the above proportions, mix them evenly, and heat to 65°C while stirring.

[0114] 2) Weigh deionized water, 1,2-hexanediol, raspberry ketone, butylene glycol, NIKKOL SMT, and SIMULGEL INS 100 into an aqueous phase beaker according to the above proportions, mix well, and heat to 65°C while stirring.

[0115] 3) While slowly homogenizing, slowly pour the material from the oil phase beaker into the aqueous phase beaker, and start homogenizing at 5500 rpm for 5 minutes. After homogenization, start stirring and cooling.

[0116] 4) When the temperature drops to 25℃, pour the 10% citric acid aqueous solution into the beaker and stir for 3~5 minutes.

[0117] 5) Stop stirring and discharge the material.

[0118] In the preparation process of this comparative example, after cooling down in step (4), oil and water separation occurred, the material became uneven and coarse, and a uniform and stable emulsion could not be obtained.

[0119] Comparative Example 7 This comparative example does not contain cetearyl alcohol, and the other components and their mass fractions are the same as in Example 2. The preparation method of the emulsion in this comparative example is the same as that in Example 1. During the stability test, the obtained emulsion showed stratification at room temperature, 4°C, freezing, and high temperature (45°C).

[0120] Comparative Example 8 In this comparative example, a 0.1% (w / w) aqueous dispersion of phytosphingosine was prepared.

[0121] Prepare a 0.1% (w / w) aqueous dispersion of plant sphingosine as follows: Figure 15 As shown in the image, the 0.1% phytosphingosine aqueous dispersion is turbid because phytosphingosine has low water solubility, and most of it settles at the bottom.

[0122] Experimental Example The effects of the emulsions prepared in the examples and comparative examples were tested, as detailed below: 1. Stability Test Test conditions: -20℃ to room temperature cycling, 4℃, room temperature, 45℃ Test duration: 48 hours at -20℃ to 48 hours at room temperature constitutes one cycle, 6 cycles are performed for a total of 24 days; 3 months of static placement at 4℃, room temperature and 45℃.

[0123] Figure 1-14 The stability assessment results at various temperatures at the end of the stability test (all images were taken after the temperature had returned to room temperature): Figure 1-9 The test results are for the emulsions prepared in Examples 1-8 and Example 12; Figure 10-14 This diagram illustrates the initial state of the emulsions prepared in Comparative Examples 1-5. The emulsions prepared in these examples are uniformly stable under various temperature conditions, with no solid precipitation or oil-water separation. The emulsions prepared in Comparative Examples 1-5, however, were not initially homogeneous and contained particles.

[0124] The results of Comparative Example 8 are as follows Figure 15 The figure shows the state of a 0.1% (w / w) aqueous solution of phytosphingosine at room temperature. As can be seen from the figure, phytosphingosine has poor solubility in water, with a large number of undissolved particles. Even with stirring or heating the solution to 85°C, it still cannot be well dissolved or uniformly dispersed.

[0125] To further verify the long-term stability of the examples, the emulsions prepared in Examples 1-12 were placed at room temperature and tested periodically. It was found that after 6 months and 1 year, the emulsions remained uniform and stable, with no solid precipitation and no oil-water separation.

[0126] 2. Antibacterial test: Testing organization: Engel Testing Technology Service (Shanghai) Co., Ltd.

[0127] Test method: QB / T2738-2023 Evaluation method for antibacterial and bacteriostatic effects of daily chemical products 7.9 Test method for bacteriostatic effect of antibacterial daily chemical products (carrier immersion quantitative method).

[0128] Test bacterial species and their numbers: Staphylococcus aureus ATCC 6538, Propionibacterium acnes BNCC 336649, Malassezia ATCC 44344.

[0129] Bacterial concentration: Staphylococcus aureus 8.5 × 10⁻⁶ 6 CFU / mL, Propionibacterium acnes 5.3×10 6 CFU / mL, Malassezia ATCC 8.8×10 6 CFU / mL.

[0130] Sample test concentration: control group (without phytosphingosine, otherwise the components of the emulsion prepared in Example 2 are the same), experimental group contains 0.2% phytosphingosine (experimental group uses the emulsion prepared in Example 2).

[0131] The test results of the control group are shown in Table 1: Table 1. Antibacterial effects of the control group and the experimental group

[0132] Judgment criteria: If the antibacterial rate is ≥50%~90%, the product has antibacterial effect; if the antibacterial rate is ≥90%, the product has strong antibacterial effect.

[0133] Evaluation of antibacterial effect: The experimental group (emulsion containing 0.2% phytosphingosine) showed strong inhibitory effects on Staphylococcus aureus, Propionibacterium acnes, and Malassezia after 60 minutes of action. This indicates that the emulsion prepared by the present invention has a strong antibacterial effect. The emulsion containing phytosphingosine prepared by the present invention is not only relatively stable, but also allows the phytosphingosine to fully exert its efficacy.

[0134] Furthermore, the emulsion obtained in Example 2 of this invention is as follows: Figure 16 As shown, the lotion is quite fine and even, easy to spread and absorb, and quite moisturizing after full application, with good moisturizing properties.

[0135] The above description is merely a preferred embodiment of the present invention and is not intended to limit the 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 composition for improving the stability of substances with low water solubility, characterized in that, By weight, its components include: 2-2.5 parts hydrogenated lecithin, 2-4 parts emulsifying stabilizer, 5-16 parts medium- to high-polarity oils, 0.3-0.6 parts anionic surfactant, 0.5-1.5 parts thickener, and 0.35-0.45 parts pH adjuster.

2. The composition according to claim 1, characterized in that, The emulsifying stabilizer in the composition is selected from at least one of cetearyl alcohol, cetyl alcohol, stearyl alcohol, or behenyl alcohol; Preferably, the medium-to-high polarity oil is selected from at least one of octyl dodecanol, caprylic / capric triglyceride, isopropyl myristate, isononyl isononanoate, and ethylhexyl palmitate. Preferably, the anionic surfactant is an anionic surfactant with an HLB value between 18 and 25; Preferably, the anionic surfactant is selected from at least one of sodium cocoyl methyl taurate, sodium stearoyl taurate, disodium lauryl sulfosuccinate, disodium poissonyl ether sulfosuccinate, and sodium methyl stearoyl taurate. Preferably, the thickener comprises SIMULGEL INS 100; Preferably, the pH adjuster is an acidic adjuster; Preferably, the pH adjuster is selected from at least one of 10wt% citric acid aqueous solution and lactic acid.

3. The use of the composition according to claim 1 or 2 in improving the stability of poorly water-soluble substances, characterized in that, The low water-soluble substance is phytosphingosine and its derivatives; Preferably, the low water-soluble substance is selected from at least one of phytosphingosine, acetyl phytosphingosine, diacetyl phytosphingosine, tetraacetyl phytosphingosine, and triacetyl phytosphingosine.

4. The application according to claim 3, characterized in that, The mass ratio of each component in the composition is as follows: low water-soluble substance: hydrogenated lecithin: emulsifying stabilizer: medium-to-high polarity oil: anionic surfactant: thickener: pH adjuster = 0.1-1: 2-2.5: 2-4: 5-16: 0.3-0.6: 0.5-1.5: 0.35-0.45; Preferably, the ratio of low water-soluble substance: hydrogenated lecithin: emulsifying stabilizer: medium to high polarity oil: anionic surfactant: thickener: pH adjuster is 0.2:2:3:11:0.5:1:0.

4.

5. A stabilized emulsion, characterized in that, The composition comprises the composition of claim 1 or 2, a low water-soluble substance and water, wherein the mass ratio of the low water-soluble substance to water is 0.1~1:55.15~88.05; Preferably, the mass ratio of the low water-soluble substance to water is 0.2:76.

9.

6. The stabilized emulsion according to claim 5, characterized in that, The stabilized emulsion comprises, by weight, 0.1-1 parts of low water-soluble substances, 55.15-88.05 parts of water, 2-2.5 parts of hydrogenated lecithin, 2-4 parts of stabilizer, 5-16 parts of medium- to high-polarity oils, 0.3-0.6 parts of anionic surfactant, 0.5-1.5 parts of thickener, and 0.35-0.45 parts of pH adjuster; Preferably, the mass ratio of low water-soluble substances, water, hydrogenated lecithin, emulsifying stabilizer, medium-to-high polarity oils, anionic surfactant, thickener, and pH adjuster in the stabilized emulsion is 0.2:76.9:2:3:11:0.5:1:0.

4.

7. The stabilized emulsion according to claim 5, characterized in that, The stabilized emulsion further includes at least one of 1,2-hexanediol, component C, and component D; Component C is at least one of raspberry ketone and p-hydroxyacetophenone; component D is at least one of butanediol, glycerol, dipropylene glycol, isopentyl glycol, and 1,3-propanediol.

8. The stabilized emulsion according to claim 7, characterized in that, The mass ratio of the low water-soluble substance to 1,2-hexanediol is 0.1~1:0.3~0.8; The mass ratio of the low water-soluble substance to component C is 0.1-1:0.3-0.8; The mass ratio of the low water-soluble substance to component D is 0.1-1:1~10; Preferably, the mass ratio of the low water-soluble active ingredient to 1,2-hexanediol is 0.2:0.5; Preferably, the mass ratio of the low water-soluble active ingredient to component C is 0.2:0.5; Preferably, the mass ratio of the low water-soluble active ingredient to component D is 0.2:

4.

9. The method for preparing the stable emulsion according to any one of claims 5-8, characterized in that, include: Hydrogenated lecithin, emulsifying stabilizer, low water-soluble substances, and medium-to-high polarity oils are mixed in proportion, and the resulting oil phase mixture is heated to 70-85°C while stirring. Deionized water, anionic surfactant, and thickener are mixed in a certain proportion, and the resulting aqueous mixture is heated to 70-85°C while stirring. Mix the oil phase mixture at 70~85℃ with the water phase mixture, homogenize, and then add the pH adjuster when the temperature is lowered to 20~45℃. After mixing, the stable emulsion is obtained. Preferably, the preparation method further includes adding 1,2-hexanediol, component C, and component D in proportion when preparing the aqueous mixture.

10. The use of the stabilized emulsion according to any one of claims 5-8 in the preparation of daily chemical products and pharmaceuticals, characterized in that, The daily chemical products include skin care products; the medicines include medicines for treating skin conditions; Preferably, the skin care products include facial cleanser, shampoo, skin lotion, skin cream, and hair conditioner; Preferably, the dosage forms of the daily chemical products and pharmaceuticals include ointments, pastes, emulsions, gels, solutions, suspensions, emulsions, patches, and sprays.

Images