Composition with stabilized active ingredient

Abstract

According to an embodiment of the present invention, a composition in which an active ingredient is stabilized is provided. The composition in which an active ingredient is stabilized comprises an active ingredient, a water-soluble polymer, and a hydrotrope component, wherein the active ingredient may be supported on the water-soluble polymer and stabilized by the hydrotrope component.

Description

Technology Field

[0001] The present invention relates to a composition in which an active ingredient is stabilized. Specifically, it is a composition in which an active ingredient having the property of being easily oxidized in an external environment is stabilized using a water-soluble polymer and a hydrotrope component. In particular, the present invention relates to a freeze-dried cosmetic composition in which an active ingredient having the property of being easily oxidized in an external environment is stabilized. Background Technology

[0002] Vitamins C, E, arbutin, adenosine, polyphenols, and various natural oils or extracts are known to provide diverse benefits to the skin, such as wrinkle prevention, whitening, antioxidant effects, and moisturization. Research is actively underway to incorporate these active ingredients into skin-improving compositions. However, active ingredients such as Vitamins C and E are sensitive to external environments like air, light, heat, and moisture, and are prone to oxidation, making it difficult to stably incorporate them into compositions.

[0003] To address these issues, a technology was developed to prevent the oxidation of active ingredients by loading them onto water-soluble polymers and then freeze-drying them. However, even when using this method, problems such as discoloration, changes in appearance, and a decrease in potency of the composition over time still occurred due to the hygroscopic properties of the freeze-dried formulations. The problem to be solved

[0004] The present invention aims to solve the above problems by additionally including a hydrotrope component in a water-soluble polymer to stabilize an active ingredient that is unstable to air, light, heat, moisture, etc., thereby providing a composition that can maintain a high content of the active ingredient without loss even after a long period of time.

[0005] The technical problems of the present invention are not limited to those mentioned above, and other unmentioned technical problems will be clearly understood by those skilled in the art from the description below. means of solving the problem

[0006] According to an embodiment of the present invention, a composition in which an active ingredient is stabilized is provided. The composition in which an active ingredient is stabilized comprises the active ingredient, a water-soluble polymer, and a hydrotrope component, and the active ingredient may be stabilized by the water-soluble polymer and the hydrotrope component.

[0007] In addition, the above active ingredient may be an ingredient having the property of being oxidized by at least one of air, light, heat, and moisture.

[0008] In addition, the active ingredient can be supported on a porous structure formed by the water-soluble polymer and stabilized through binding with the hydrotrope component.

[0009] In addition, the above active ingredient may be included in an amount of 6 to 80 weight percent relative to the total weight of the composition.

[0010] In addition, the active ingredient may include one or more selected from the group consisting of water-soluble vitamins including ascorbic acid or its derivatives, oil-soluble vitamins including retinoic acid or its derivatives; arbutin; water-soluble physiologically active ingredients including adenosine; astaxanthin; polyphenols; and natural extracts.

[0011] In addition, the above water-soluble polymer may be included in an amount of 5 to 55 weight percent relative to the total weight of the composition.

[0012] In addition, the water-soluble polymer may include one or more selected from the group consisting of sodium hyaluronate, calcium hyaluronate, potassium hyaluronate, hyaluronic acid, hydrolyzed hyaluronic acid, hydrolyzed sodium hyaluronate, hydrolyzed calcium hyaluronate, hydroxypropyltrimonium hyaluronate, sodium acetylated hyaluronate, and sodium hyaluronate crosspolymer; collagen and denatured collagen; algin; alginate; gelatin; carrageenan; starch; galactomannan; glucomannan; guar gum; locust bean gum; xanthan gum; gellan; cellulose; polyvinylpyrrolidone (PVP); and polyvinyl alcohol (PVA).

[0013] In addition, the above hydrotrope component may include one or more selected from the group consisting of niacinamide, urea, caffeine, citrate, and salicylate.

[0014] In addition, the hydrotrope component may be included in an amount of 8 to 80 weight percent relative to the total weight of the composition.

[0015] In addition, the hydrotrope component may be included in an amount of 8 to 30 weight percent relative to the total weight of the composition.

[0016] In addition, the weight ratio of the hydrotrope component to the active ingredient may be 1:0.1 to 10.

[0017] In addition, the composition in which the above active ingredient is stabilized can be formulated into a solid or semi-solid form.

[0018] In addition, the composition in which the above active ingredient is stabilized may be a freeze-dried formulation.

[0019] In addition, the composition in which the above active ingredient is stabilized has a density of 150 dyne / cm 2 It can have a hardness greater than that.

[0020] According to an embodiment of the present invention, a cosmetic composition for improving skin is provided, comprising a composition in which the active ingredient is stabilized. Effects of the invention

[0021] According to the present invention, as an active ingredient having the property of being oxidized by air, light, heat, moisture, etc. is stabilized by a water-soluble polymer and a hydrotrope component, the efficacy and potency of the active ingredient are maintained, and formulation can be easily achieved.

[0022] In addition, according to the present invention, even if freeze-drying is performed on the composition, the formulation and efficacy of the composition can be stably maintained without problems such as browning, shrinkage, or decrease in potency over time.

[0023] Furthermore, according to the present invention, the weight is lighter than that of a conventional cosmetic composition containing moisture through a freeze-drying process, thereby reducing carbon emissions during the product distribution process. In particular, since the use of preservatives is not required, it can be more environmentally friendly.

[0024] In addition, according to the present invention, a solid or semi-solid composition in which an active ingredient is stabilized can be rehydrated and used in the form of application, ingestion, etc. In particular, the solid or semi-solid composition in which an active ingredient is stabilized can dissolve rapidly, making it easy to use. Brief explanation of the drawing

[0025] A brief description of each drawing is provided to help to better understand the drawings cited in the detailed description of the invention. Figure 1 is an SEM image of a composition according to an embodiment of the present invention. Figures 2a and 2b are photographs illustrating the dissolution rate of a composition according to an example and a comparative example of the present invention. Figure 3 is a graph showing the results of a potency stability test according to an embodiment and a comparative example of the present invention. Specific details for implementing the invention

[0026] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by a skilled expert in the art to which the present invention pertains. In general, the nomenclature used herein is well known and commonly used in the art. Furthermore, in describing embodiments of the present invention, detailed descriptions of related known components or functions are omitted if it is determined that such detailed descriptions would hinder understanding of the embodiments of the present invention. Additionally, while embodiments of the present invention will be described below, the technical concept of the present invention is not limited or restricted thereto and can be modified and implemented in various ways by those skilled in the art.

[0028] According to an embodiment of the present invention, a composition in which an active ingredient is stabilized is provided. The composition in which an active ingredient is stabilized according to the present invention may include an active ingredient, a water-soluble polymer, and a hydrotrope component. In this case, the active ingredient may be stabilized by the water-soluble polymer and / or the hydrotrope component. Accordingly, in the present invention, oxidation of the active ingredient is prevented, and the potency may not decrease over time. Here, “potency” refers to the total amount of the composition required to produce a given effect. Furthermore, “high content” of the active ingredient may mean that the active ingredient is included in an amount of 10% by weight or more relative to the total weight of the composition, but is not limited thereto.

[0029] In the present invention, the term “active ingredient” refers to an ingredient that exhibits skin-improving efficacy. Here, skin-improving efficacy may include all known efficacy related to improving skin condition, such as, for example, antioxidant, anti-inflammatory, whitening, moisturizing, skin soothing, wrinkle improvement, and exfoliation.

[0030] The active ingredient of the present invention may be a component having the property of being oxidized by at least one of air, light, heat, and moisture. In the present invention, the oxidation of such active ingredient may be prevented by a water-soluble polymer and / or hydrotrope component.

[0031] According to the examples, the active ingredient may be included in an amount of 6 to 80 weight% relative to the total weight of the composition, specifically 20 to 80 weight%, and more specifically 50 to 80 weight%. If the active ingredient is included in an amount of less than 6 weight%, the skin improvement efficacy may not be sufficiently displayed, and if the active ingredient is included in an amount exceeding 80 weight%, the active ingredient may precipitate or its potency may decrease over time. Additionally, in the present invention, the active ingredient may be stably included in an amount of 6 weight%, 20 weight%, or 50 weight% or more by means of a water-soluble polymer and / or hydrotrope component.

[0032] According to the examples, the active ingredient may include one or more selected from the group consisting of water-soluble vitamins including ascorbic acid or derivatives thereof; oil-soluble vitamins including retinoic acid or derivatives thereof; water-soluble bioactive ingredients including arbutin; adenosine; astaxanthin; polyphenols; and natural extracts. However, this is exemplary, and the active ingredient may be selected from various active ingredients having skin-improving efficacy.

[0033] Water-soluble polymers can stabilize active ingredients. For example, water-soluble polymers can form a framework for supporting active ingredients by forming a porous structure, and the active ingredients can be supported on this porous structure.

[0034] In the examples, the water-soluble polymer can be freeze-dried together with the active ingredient and / or hydrotrope component. That is, a freeze-dried structure loaded with the active ingredient can be formed. Freeze-drying prevents problems such as browning, shrinkage, and reduced potency, and allows the formulation and efficacy of the composition to be maintained more stably. In particular, it is very eco-friendly as it not only reduces the weight of the composition and carbon emissions during distribution, but also allows for the absence of preservatives.

[0035] For example, a water-soluble polymer can form a porous structure by removing moisture through freeze-drying, and an active ingredient can be supported on such a porous structure. However, this is merely an example, and various methods may be applied, such as the water-soluble polymer existing as a porous structure at room temperature and the active ingredient being supported thereon.

[0036] According to the example, the porous structure has a g / cm³ of 0.02 to 0.3 g / cm³ 3 , specifically 0.02~0.28 g / cm³ 3 , more specifically 0.02~0.25 g / cm³ 3 It may have an apparent density. Here, “apparent density” may refer to the total density including the pore portion in a porous structure having a solid portion and a pore portion within an object, such as a powder, particle, fiber, or foam. In the present invention, the apparent density can be calculated by dividing the mass of the porous structure by the total volume including both the solid portion and the pore portion. When the apparent density of the porous structure satisfies the above range, the shape of the composition is stably maintained, and the composition can dissolve at a rapid rate upon rehydration.

[0037] According to the examples, the water-soluble polymer may be included in an amount of 5 to 55 weight% relative to the total weight of the composition. If the water-soluble polymer is included in an amount of less than 5 weight%, for example, the stability of the active ingredient may be reduced, such as by precipitation of the active ingredient, and if the water-soluble polymer is included in an amount of more than 55 weight%, it may interfere with the efficacy of the active ingredient.

[0038] According to the examples, the water-soluble polymer may include one or more selected from the group consisting of sodium hyaluronate, calcium hyaluronate, potassium hyaluronate, hyaluronic acid, hydrolyzed hyaluronic acid, hydrolyzed sodium hyaluronate, hydrolyzed calcium hyaluronate, hydroxypropyltrimonium hyaluronate, sodium acetylated hyaluronate, and sodium hyaluronate crosspolymer; collagen and modified collagen; algin; alginate; gelatin; carrageenan; starch; galactomannan; glucomannan; guar gum; locust bean gum; xanthan gum; gellan; cellulose; polyvinylpyrrolidone (PVP); and polyvinyl alcohol (PVA). However, this is merely an example, and the water-soluble polymer may be selected from among various water-soluble polymers capable of forming a porous structure.

[0039] The hydrotropy component is a component that exhibits the “hydrotropy” phenomenon. Here, the hydrotropy phenomenon refers to the phenomenon in which the solubility in water increases when a third substance is added to a substance that is insoluble or sparingly soluble in water, and the hydrotropy component refers to the said third substance for increasing the solubility of the insoluble or sparingly soluble substance.

[0040] For example, a hydrotrope component can stabilize an active ingredient through binding with the active ingredient. In the embodiments of the present application, as a hydrotrope component is added to the composition, the active ingredient can be stabilized even if it is included in a high amount, and the potency may not decrease over time. Specifically, when an active ingredient is supported on a framework formed by freeze-drying of a water-soluble polymer, problems such as browning of the composition, shrinkage of its appearance, or a decrease in potency occur over time due to moisture absorption issues. However, in the embodiments of the present application, these problems can be effectively solved as the active ingredient is stabilized within the framework through binding by the hydrotrope component.

[0041] According to the examples, the hydrotrope component may be included in an amount of 8 to 80 weight% relative to the total weight of the composition, specifically in an amount of 8 to 50 weight% relative to the total weight of the composition, more specifically in an amount of 8 to 40 weight%, and most specifically in an amount of 8 to 30 weight%. Within the above range, the stability and efficacy of the active ingredient are maximized, and if the hydrotrope component content falls outside the above weight range, the active ingredient may precipitate, or browning or shrinkage of the appearance may occur over time, and the potency may decrease.

[0042] According to the examples, the hydrotrope component may include one or more selected from the group consisting of niacinamide, urea, caffeine, citrate, and salicylate. However, this is exemplary, and the hydrotrope component may be freely selected from components having hydrotropic properties.

[0043] According to the examples, the weight ratio of the hydrotrough component to the active ingredient may be 1:0.1 to 10, specifically 1:0.1 to 8, more specifically 1:0.1 to 5, and even more specifically 1:1 to 5. Within the above range, the stability and efficacy of the active ingredient are maximized, and if the weight ratio of the hydrotrough component to the active ingredient deviates from the above range, the active ingredient may precipitate, or browning or shrinkage of the external appearance may occur over time, and the potency may decrease.

[0044] According to the examples, the weight ratio of the hydrotrope component to the water-soluble polymer may be 1:0.1 to 10, specifically 1:0.1 to 8, and more specifically 1:0.1 to 5. Within the above weight ratio range, the solubility of the active ingredient or the rehydration rate of the composition may be optimized, and if it falls outside the above weight ratio range, the active ingredient may precipitate or the rehydration rate may decrease.

[0045] According to the embodiments, the composition in which the active ingredient is stabilized may further include at least one of a moisturizer, a powder, an oil, and an additive. Herein, the moisturizer is a component that imparts a skin moisturizing function to the composition; the powder is a component that imparts functions such as imparting color to the composition or improving the texture of application; the oil is a component for dissolving fat-soluble components or improving the texture of application; and the additive is a component that imparts other functions to the composition and may include various substances such as antioxidants, binders, and metal ion chelators. Furthermore, as this is exemplary, the composition in which the active ingredient is stabilized may additionally include all types of additives known in the art, such as preservatives and fragrances.

[0046] According to the examples, a composition in which the active ingredient is stabilized may be formulated into a solid or semi-solid form. For example, the composition may be formulated into a solid or semi-solid form by freeze-drying. In this case, freeze-drying may be performed to stabilize the active ingredient through water-soluble polymers and / or hydrotropes. As moisture is removed, the freeze-dried material is converted into a solid or semi-solid formulation in the form of a solid or powder. In the case of the present invention, the active ingredient, water-soluble polymers, and hydrotropes may be mixed and then formulated into a solid or semi-solid form by freeze-drying.

[0047] According to the examples, when a composition in which the active ingredient is stabilized is formulated into a solid or semi-solid form, the composition may be used after rehydration. Specifically, the solid or semi-solid composition may be prepared in a liquid form by dissolving it in a solvent such as water, and then used by applying it to the skin. However, this method of use is exemplary, and various other methods may be used, such as applying the solid or semi-solid composition directly to the skin or ingesting it.

[0048] According to an example, when a composition in which a solid or semi-solid active ingredient is stabilized is rehydrated and used, the dissolution rate of the composition in water is 50 mm 3 / sec, especially 150 mm 3 It may be greater than / sec. In this case, the dissolution rate may be measured based on the time required for a composition measuring 1.2 cm in width x 1.2 cm in length x 0.9 cm in height to be completely dissolved in 1 mL of solvent (particularly water). In the embodiments of the present application, a composition in which the active ingredient is stabilized at a high content by a water-soluble polymer and / or hydrotrope component is 50 mm 3 / sec, especially 150 mm 3 It can be easily used after rehydrating at a fast dissolution rate of more than 1 / sec.

[0049] According to the example, the composition with the active ingredient stabilized is 150 dyne / cm² 2 It can have a hardness greater than or equal to the above. In this case, the hardness can be measured using a Fudoh rheo meter. For example, the maximum load value can be measured by applying pressure at a speed of 30 cm / min to a depth of 5 mm using a 20 mm Φ spindle. In the present invention, as the active ingredient is stabilized by water-soluble polymer and / or hydrotrope components, 150 dyne / cm 2 It is possible to stably achieve the above hardness.

[0050] According to the examples, a composition in which the active ingredient is stabilized can maintain a stable potency level of 90% or higher three months after manufacturing compared to the potency level immediately after manufacturing. In the present invention, a high content of the active ingredient can be included through water-soluble polymer and / or hydrotrope components, while ensuring that the potency does not decrease to less than 90% over time, thereby maximizing the skin improvement efficacy by the active ingredient.

[0052] According to an embodiment of the present invention, a method for stabilizing an active ingredient is provided. According to the method, a composition in which the above-described active ingredient is stabilized can be prepared.

[0053] First, an active ingredient, a water-soluble polymer, and a hydrotrope component can be mixed to form a mixture. Mixing can be carried out, for example, at room temperature using a mixer, but is not limited to this and can be carried out under various conditions and using various devices.

[0054] Subsequently, the mixture can be freeze-dried. When the mixture is freeze-dried, the moisture of the water-soluble polymer is removed to form a porous structure, and the active ingredient is supported and stabilized in this porous structure, while the active ingredient can be further stabilized by the attractive force with the hydrotrope component.

[0056] According to an embodiment of the present invention, a cosmetic composition comprising a composition in which an active ingredient is stabilized may be provided.

[0057] According to the embodiments, the cosmetic composition of the present invention can be manufactured into various products effective for skin improvement. In the present invention, “skin improvement” may refer to efficacy that improves skin condition, such as antioxidant, anti-inflammatory, whitening, moisturizing, skin soothing, wrinkle improvement, and exfoliation, but is not limited thereto and may include various known skin-related efficacys.

[0058] In addition, according to the embodiments, the cosmetic composition of the present invention may be manufactured as a functional cosmetic such as a nourishing cream, essence, or ampoule, or as a basic cosmetic such as a toner or lotion. In addition, it may be manufactured as a soap, cleanser, cleansing cream, cleansing water, etc., or as a color cosmetic such as a lipstick, lip balm, mascara, blush, shading, highlighter, makeup base, foundation, compact, concealer, skin cover, etc. It may also be manufactured as a hair cleansing product such as a shampoo, rinse, hair conditioner, hair gel, etc. Furthermore, it may be manufactured as a product that adheres to the skin, such as a pack or hydrogel slimming patch, or as a product that is sprayed onto the skin, such as a mist or aerosol.

[0059] According to the examples, the cosmetic composition of the present invention may be provided in formulations conventionally manufactured in the art. For example, it may be provided in formulations such as a solution, an emulsion obtained by dispersing an oil phase in an aqueous phase, an emulsion obtained by dispersing an aqueous phase in an oil phase, a suspension, an emulsion, a gel, etc. Additionally, the cosmetic composition of the present invention may be formulated into a solid or semi-solid form and processed into a powder, bead form, stick form, etc.

[0060] According to the embodiments, the cosmetic composition of the present invention may further include other ingredients commonly used in the art, such as thickeners, pH adjusters, isotonic agents, surfactants, stabilizers, preservatives, antimicrobial agents, UV absorbers, disinfectants, moisturizers, blockers, antioxidants, organic pigments, inorganic pigments, fragrances, vitamins, etc., within a range that does not impair the effects of the present invention. The amount of the above ingredients can be easily selected by a person skilled in the art within a range that does not impair the purpose and effects of the present invention.

[0062] According to an embodiment of the present invention, a food composition comprising a composition in which an active ingredient is stabilized may be provided.

[0063] According to the embodiments, the food composition of the present invention can be manufactured into various products effective for improving skin. For example, the food composition of the present invention can be manufactured into products such as functional foods, nutritional supplements, health foods, food additives, special nutritional foods, processed meat products, seasoned foods, pickled foods, and dairy products. However, this is merely illustrative, and according to the embodiments, the food composition of the present invention can be manufactured into products having various effects, such as anti-inflammatory effects that improve inflammation caused by atopy, acne, insect bites, etc.

[0064] According to the embodiments, the food composition of the present invention may be provided in various forms commonly manufactured in the art. For example, it may be provided in formulations such as powder, granules, pills, tablets, capsules, candies, syrups, and beverages.

[0065] According to the embodiments, the food composition of the present invention may further include other ingredients commonly used in the art, such as flavors, extracts, nutritional components, food additives, food materials, etc., within a range that does not impair the effects of the present invention. For example, food materials may include flavoring agents, natural carbohydrates, nutritional agents, vitamins, electrolytes, flavoring agents, coloring agents, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohol, carbonating agents used in carbonated beverages, fruit pulp used in beverages, etc. For example, as a flavoring agent, natural flavoring agents including taumatin, stevia extract, etc., or synthetic flavoring agents including saccharin, aspartame, etc. may be used, and natural carbohydrates may include monosaccharides such as glucose and fructose, disaccharides including maltose and sucrose, polysaccharides including dextrin and cyclotensin, etc., and sugar alcohols including xylitol, sorbitol, erythritol, etc. The amount of the above ingredients can be easily selected by a person skilled in the art within a range that does not impair the purpose and effect of the present invention.

[0067] In the following, embodiments for further explaining the present invention in more detail are presented, but the present invention is not limited thereto.

[0069] Preparation of Examples and Comparative Examples

[0071] (1) Preparation of Examples 1 to 5

[0072] Examples of compositions were prepared using the components listed in Table 1 below. The unit of the component content in Table 1 is weight%.

[0073] Specifically, Examples 1 and 2 are compositions in which the type of active ingredient is changed within the scope of the examples, Example 3 is a composition in which the type of hydrotrough component is changed within the scope of the examples, and Examples 4 and 5 are compositions in which the weight ratio of hydrotrough to active ingredient is changed within the scope of the examples.

[0074] In addition, the weight ratio with the water-soluble polymer or active ingredient is listed in Table 2 below based on the hydrotrope component.

[0076] division ingredient Example 1 Example 2 Example 3 Example 4 Example 5 Water-soluble polymer Hyaluronic acid 10 10 10 10 10 collagen 1.9 1.9 1.9 1.9 1.9 Hydrotrope component Niacinamide 19.5 19.5 - 13.0 8.65 caffeine - - 19.5 - - Active ingredient Ascorbic acid 65.5 - 65.5 72.0 76.35 Astaxanthin - 65.5 - - - additives Phenoxyethanol 0.1 0.1 0.1 0.1 0.1 moisturizer propanediol 1.0 1.0 1.0 1.0 1.0 1,3-Butylene Glycol 1.0 1.0 1.0 1.0 1.0 Panthenol 1.0 1.0 1.0 1.0 1.0 total 100 100 100 100 100

[0078] Example 1 Example 2 Example 3 Example 4 Example 5 Hydrotrope component: Water-soluble polymer 1 : 0.61 1 : 0.61 1 : 0.61 1 : 0.92 1 : 1.38 Hydrotrope ingredient: Active ingredient 1 : 3.36 1 : 3.36 1 : 3.36 1 : 5.54 1 : 8.83

[0080] (2) Preparation of Comparative Examples 1 to 4

[0081] A comparative example of the composition was prepared using the components listed in Table 2 below. The unit of the component content in Table 2 is weight%.

[0082] Specifically, Comparative Example 1 is a composition that does not contain a hydrotrope component, Comparative Example 2 is a composition in which a cyclodextrin performing a similar function is added instead of a hydrotrope component, and Comparative Examples 3 and 4 are compositions in which the weight ratio of hydrotrope to active ingredient is changed outside the range of the examples.

[0083] In addition, the content ratio with water-soluble polymers or active ingredients is listed in Table 4 below, based on the hydrotrope component.

[0085] division ingredient Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Water-soluble polymer Hyaluronic acid 20 10 10 10 collagen 11.4 1.9 1.9 1.9 Hydrotrope component Niacinamide - - 80 7 Cyclodextrin - 19.5 - - Active ingredient Ascorbic acid 65.5 65.5 5 78 Adenosine - - - - additives Phenoxyethanol 0.1 0.1 0.1 0.1 moisturizer propanediol 1.0 1.0 1.0 1.0 1,3-Butylene Glycol 1.0 1.0 1.0 1.0 Panthenol 1.0 1.0 1.0 1.0 total 100 100 100 100

[0087] Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Hydrotrope component: Water-soluble polymer - 1 : 0.61 1 : 0.15 1 : 1.70 Hydrotrope ingredient: Active ingredient - 1 : 3.36 1 : 0.06 1 : 11.14

[0089] Experimental Example

[0091] (1) Stability measurement experiment immediately after freeze-drying

[0092] After freeze-drying the compositions of Examples 1 to 5 and Comparative Examples 1 to 4, their hardness and the presence of precipitation of active ingredients were measured and are shown in Table 5. Hardness was measured using a Fudoh rheo meter. Specifically, hardness was measured by measuring the maximum load value when a 20 mm Φ spindle was applied at a speed of 30 cm / min to a depth of 5 mm. Additionally, a scanning electron microscope (SEM) image of the freeze-dried Example 1 is shown in Figure 1.

[0094] As a result of the experiment, referring to Fig. 1, it can be confirmed that in the case of Example 1, the active ingredient is stably contained within the porous structure. It is expected that the same will be observed in the cases of Examples 2 to 5.

[0095] In addition, for Examples 1 to 5, the hardness was 180 dyne / cm immediately after freeze-drying. 2 As measured above, it was confirmed that the solid formulation was stably formed. On the other hand, in the case of Comparative Examples 1 to 4, the hardness immediately after freeze-drying was 130 dyne / cm 2 As it was measured to be less than [amount], it was confirmed that the solid formulation was not stably formed.

[0096] In addition, in the case of Examples 1 to 4, no precipitation of the active ingredient was observed immediately after freeze-drying, but in the case of Comparative Examples 1 to 4, precipitation of the active ingredient was observed in all of them.

[0098] division Hardness (dyne / cm) immediately after freeze-drying 2 ) Precipitation immediately after freeze-drying Example 1 180 X Example 2 190 X Example 3 180 X Example 4 210 X Example 5 212 X Comparative Example 1 34 ● Comparative Example 2 42 ● Comparative Example 3 105 ● Comparative Example 4 121 ● ●: Active ingredient precipitated X: Active ingredient not precipitated

[0100] (2) Experiment to measure ease of dissolution upon rehydration

[0101] The freeze-dried compositions of Examples 1 to 5 and Comparative Examples 1 to 4 were each taken in a size of 1.2 cm x 1.2 cm x 0.9 cm and dissolved in 1 mL of solvent (water). The time and speed required for complete dissolution were measured, and the presence of remaining lumps after dissolution was observed and shown in Table 6. Among these, Example 1 and Comparative Example 1 are shown in Figures 2a and 2b. Specifically, Figure 2a is a photograph of Example 1 and Comparative Example 1 immediately after dissolution, and Figure 2b is a photograph of Example 1 and Comparative Example 1 60 seconds after dissolution.

[0103] As a result of the experiment, the dissolution rate was 50 mm for all of Examples 1 to 5. 3 / sec, especially 150 mm 3 Although the ease of use of the composition was confirmed as it was observed to be greater than / sec, in the case of Comparative Examples 1 to 4, the dissolution rate was all 50 mm 3 As it was observed to be less than / sec, it was confirmed that the use of the composition was inconvenient.

[0104] In addition, in the case of Examples 1 to 5, it was confirmed that no lumps remained after dissolution and the composition was completely dissolved, whereas in the case of Comparative Examples 1 and 2, the composition was not completely dissolved in water, the active ingredients were not evenly dispersed, and lumps remained, so it is judged that it would not be easy to use.

[0106] division Dissolution time (sec) Dissolution rate (mm) 3 / sec) Whether lumps remain after dissolution Example 1 1 1296 X Example 2 3 432 X Example 3 3 432 X Example 4 4 324 X Example 5 8 162 X Comparative Example 1 63 20.57 ● Comparative Example 2 71 18.25 ● Comparative Example 3 28 46.28 X Comparative Example 4 31 41.80 X ●: No lumps remain X: No lumps remain, completely dissolved

[0108] (3) Time-dependent stability measurement experiment

[0109] The compositions of Examples 1 to 5 and Comparative Examples 1 to 4 were each freeze-dried and then stored for 3 months under conditions of 25°C and 60% relative humidity or 40°C and 75% relative humidity, and then the color, size, and hardness of each were measured and are shown in Table 7. In the case of Comparative Examples 1 and 2, the formulation was not maintained after 3 months, so the hardness could not be measured.

[0111] As a result of the experiment, no changes in color or size were observed in Examples 1 to 5, and the hardness also showed no significant difference compared to immediately after freeze-drying, confirming that the composition remains stable over time.

[0112] On the other hand, in the case of Comparative Examples 1 to 4, after 3 months, the color turned brown and the external appearance shrank, and a decrease in hardness was observed compared to immediately after freeze-drying, confirming that the stability of the composition was insufficient.

[0114] division Stability - Color Stability - Size Stability - Physical property (hardness) 25℃, 60% RH 40℃, 75% RH 25℃, 60% RH 40℃, 75% RH 25℃, 60% RH 40℃, 75% RH Example 1 Good Good Good Good 179 181 Example 2 Good Good Good Good 181 190 Example 3 Good Good Good Good 177 183 Example 4 Good Good Good Good 205 211 Example 5 Good Good Good Good 217 210 Comparative Example 1 ● ● ● ● Unmeasurable Unmeasurable Comparative Example 2 ● ● ● ● Unmeasurable Unmeasurable Comparative Example 3 ○ ◐ ○ ◐ 104 79 Comparative Example 4 ○ ◐ ◐ ◐ 46 42 * Stability - Color Judgment Criteria ●: Turns brown ◐: Turns yellow ○: Turns pale yellow * Stability - Size Judgment Criteria ●: Shrinks 90% or more compared to original size ◐: Shrinks 10–60% compared to original size ○: Shrinks less than 10% compared to original size

[0116] (4) Experiment to measure change in potency

[0117] Immediately after freeze-drying the compositions of Examples 1 to 5 and Comparative Examples 1 to 4, the content of the active ingredient remaining in each composition (i.e., potency) was measured using HPLC (High Performance Liquid Chromatography). In addition, after storing the compositions for 3 months under conditions of 25°C and 60% relative humidity or 40°C and 75% relative humidity, the content of the active ingredient remaining in each composition (potency) was measured using HPLC, and the ratio (%) of the potency after 3 months to the potency immediately after freeze-drying is shown in Table 8 and Figure 3.

[0119] As a result of the experiment, it was measured that in all of Examples 1 to 5, the potency remained above 90% even after 3 months, confirming that the potency is stably maintained even when the active ingredient is contained in a high amount.

[0120] On the other hand, in the case of Comparative Examples 1 to 4, the potency was measured to be less than 85% after 3 months, indicating a lack of stability and confirming that the potency did not remain stable over time and decreased due to the active ingredient.

[0122] division Change in potency (%) 25℃, 60% RH 40℃, 75% RH Example 1 99.5 99.8 Example 2 102.1 100.6 Example 3 101.2 100.7 Example 4 100.8 99.4 Example 5 100.0 97.8 Comparative Example 1 66.7 45.6 Comparative Example 2 69.9 44.5 Comparative Example 3 82.3 82.9 Comparative Example 4 83.7 77.1

[0124] Foregoing, specific parts of the content of the present invention have been described in detail. It will be apparent to those skilled in the art that such specific descriptions are merely preferred embodiments and do not limit the scope of the present invention. Accordingly, the actual scope of the present invention is defined by the appended claims and their equivalents.

Claims

Claim 1 A composition in which an active ingredient is stabilized, comprising the active ingredient, a water-soluble polymer, and a hydrotrope component, wherein the active ingredient is stabilized by the water-soluble polymer and the hydrotrope component, wherein the active ingredient is supported on a porous structure formed by the water-soluble polymer and stabilized through bonding with the hydrotrope component, and wherein the active ingredient comprises 50 to 80 weight% based on the total weight of the composition. Claim 2 A composition in which the active ingredient is stabilized, wherein the active ingredient is a component having the property of being oxidized by at least one of air, light, heat, and moisture. Claim 3 delete Claim 4 delete Claim 5 A composition in which the active ingredient is stabilized, wherein the active ingredient comprises one or more selected from the group consisting of: a water-soluble vitamin comprising ascorbic acid or a derivative thereof; a water-soluble vitamin comprising retinoic acid or a derivative thereof; a water-soluble physiologically active ingredient comprising arbutin; adenosine; astaxanthin; polyphenol; and natural extracts. Claim 6 A composition in which the active ingredient is stabilized, wherein the water-soluble polymer is included in an amount of 5 to 55 weight% relative to the total weight of the composition. Claim 7 A composition having an active ingredient stabilized according to claim 1, wherein the water-soluble polymer comprises one or more selected from the group consisting of sodium hyaluronate, calcium hyaluronate, potassium hyaluronate, hyaluronic acid, hydrolyzed hyaluronic acid, hydrolyzed sodium hyaluronate, hydrolyzed calcium hyaluronate, hydroxypropyltrimonium hyaluronate, sodium acetylated hyaluronate, and sodium hyaluronate crosspolymer; collagen and denatured collagen; algin; alginate; gelatin; carrageenan; starch; galactomannan; glucomannan; guar gum; locust bean gum; xanthan gum; gellan; cellulose; polyvinylpyrrolidone (PVP); and polyvinyl alcohol (PVA). Claim 8 A composition in which an active ingredient is stabilized, wherein the hydrotrope component comprises one or more selected from the group consisting of niacinamide, urea, caffeine, citrate, and salicylate. Claim 9 A composition in which the active ingredient is stabilized, wherein the hydrotrope component is included in an amount of 8 to 80 weight% relative to the total weight of the composition. Claim 10 A composition in which the active ingredient is stabilized, wherein the weight ratio of the hydrotrope component to the active ingredient is 1:0.1 to 10 in claim 1. Claim 11 In claim 1, the composition in which the active ingredient is stabilized is formulated into a solid or semi-solid form. Claim 12 In claim 1, the composition in which the active ingredient is stabilized is a freeze-dried formulation. Claim 13 In claim 1, the composition in which the active ingredient is stabilized has a density of 150 dyne / cm 2 A composition in which the active ingredient is stabilized, having a hardness greater than or equal to the above. Claim 14 A cosmetic composition for skin improvement comprising a composition in which the active ingredient according to claim 1 is stabilized.

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