Two-chamber container type external preparation for skin
A two-container system with cyclodextrin-wrapped retinol and amino acids in a viscosity-controlled liquid composition addresses retinol's stability and solubility issues, ensuring effective skin care products with prolonged retinol efficacy.
Patent Information
- Application Number
- JP2023118449
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2023-07-20
- Publication Date
- 2025-01-30
AI Technical Summary
Retinol, being oil-soluble, is difficult to mix with water-based preparations and is unstable under oxygen and UV exposure, leading to poor stability and solubility issues in existing formulations.
A two-container system where one container holds a cyclodextrin-wrapped retinol powder composition with amino acids and the other a viscosity-controlled liquid composition, allowing for efficient mixing and stabilization of retinol during storage and use.
Ensures retinol's stability and solubility over time, enabling effective skin care products with enhanced retinol benefits even after prolonged storage.
Smart Images

Figure 2025015197000001_ABST
Abstract
Description
[Technical field]
[0001] The present invention relates to a dual-chamber container-type external skin preparation. [Background technology]
[0002] Retinol (vitamin A1) is attracting a great deal of attention as an ingredient that is expected to have beauty effects such as reducing wrinkles and increasing skin elasticity by promoting the turnover of epidermal cells in the skin and promoting the biosynthesis of collagen, which affects wrinkles, and elastin, which affects elasticity.
[0003] However, retinol is easily oxidized by oxygen, and therefore has extremely low stability in preparations containing water with a high dissolved oxygen content, particularly in water-based preparations (e.g., lotions, oil-in-water emulsions, etc.).In addition, when exposed to ultraviolet light, it becomes unstable and converts from the trans form to the cis form.
[0004] For this reason, various techniques have been developed to stabilize retinol, including the combined use with phenolic antioxidants (see, for example, Patent Document 1) and the combined use with ultraviolet absorbers (see, for example, Patent Document 2).
[0005] Furthermore, as a stabilization technique for unstable ingredients such as retinol, preparation at the time of use can be mentioned. Preparation at the time of use is a method of use in which an active ingredient is mixed with a liquid ingredient just before use, and is effective as a method of increasing the stability of the active ingredient.
[0006] However, because retinol is an oil-soluble ingredient, it cannot be easily mixed with liquid ingredients that contain water, and various problems exist when preparing it just before use.
[0007] By incorporating retinol into cyclodextrin, it can be converted from a liquid to a powder and its properties can be changed from oil-soluble to water-soluble.
[0008] However, this cyclodextrin-encapsulated retinol powder had the problem that, for example, when stored for a long period of time in a high humidity environment, it became difficult to dissolve in liquid components when reconstituted just before use, significantly impairing its usability. [Prior art documents] [Patent documents]
[0009] [Patent Document 1] JP 2022-101891 A [Patent Document 2] Special Publication No. 2023-507488 Summary of the Invention [Problem to be solved by the invention]
[0010] The object of the present invention is to provide a two-chamber container-type external skin preparation that allows the function of retinol to be fully exerted at the time of use even when stored for a long period of time, and that enhances the solubility of cyclodextrin-encapsulated retinol in a liquid composition when prepared just before use. [Means for solving the problem]
[0011] Such an object can be achieved by the present invention described below in (1) to (5). (1) A two-chamber container having a first container and a second container whose interiors are capable of communicating with each other, a powder composition filled in the first container, and a liquid composition filled in the second container, a two-chamber container-type external skin preparation, the powder composition and the liquid composition being mixed by communicating an inside of the first container with an inside of the second container during use; The powder composition contains cyclodextrin-encapsulated retinol and amino acids, The liquid composition is a two-chamber container-type external skin preparation, characterized in that the viscosity of the liquid composition, measured at 60 rpm using a B-type viscometer in an environment of 25°C, is 20 mPa·s or more and 1000 mPa·s or less.
[0012] (2) The two-chamber container type external skin preparation according to (1) above, wherein the content of the cyclodextrin-encapsulated retinol in the powder composition is 20.0% by mass or more and 80.0% by mass or less.
[0013] (3) The two-chamber container type external skin preparation according to (1) or (2) above, wherein the amino acid is betaine.
[0014] (4) A two-chamber container-type topical skin preparation according to any one of (1) to (3), which satisfies the relationship 0.001≦Wi / Wo≦0.10, where Wi [g] is the mass of the powder composition and Wo [g] is the mass of the liquid composition.
[0015] (5) The two-chamber container-type external skin preparation according to any one of (1) to (4), wherein the liquid composition contains a fermented product obtained by fermenting rice bran and a bean-derived peptide with Bacillus subtilis. Effect of the Invention
[0016] According to the present invention, it is possible to provide a two-chamber container-type topical skin preparation that allows the function of retinol to be fully exerted at the time of use even when stored for a long period of time, and that enhances the solubility of cyclodextrin-encapsulated retinol in a liquid composition when prepared just before use. [Brief description of the drawings]
[0017] [Figure 1] FIG. 2 is a diagram showing an example of the configuration of a two-chamber container, illustrating the state before use. [Diagram 2] FIG. 2 is a diagram showing a state in which the two-chamber container shown in FIG. 1 is in use. [Diagram 3] FIG. 1 shows a method for preparation just before use using a two-chamber container. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0018] Preferred embodiments of the present invention will now be described in detail. [1] Two-compartment container-type topical skin preparation First, the two-chamber container-type external skin preparation of the present invention will be described.
[0019] The two-chamber container type topical skin preparation of the present invention has a two-chamber container with a first container and a second container whose interiors are capable of communicating with each other, a powder composition filled in the first container, and a liquid composition filled in the second container, and when in use, the powder composition and the liquid composition are mixed by connecting the interiors of the first container and the second container.
[0020] In the two-chamber container-type topical skin preparation of the present invention, the powder composition contains cyclodextrin-encapsulated retinol and amino acids, and the liquid composition has a viscosity of 20 mPa s or more and 1,000 mPa s or less, measured at a rotation speed of 60 rpm using a B-type viscometer in an environment of 25°C.
[0021] When in use, the two-chamber container type topical skin preparation of the present invention is used in a state in which the inside of the first container is connected to the inside of the second container, the powder composition filled in the first container and the liquid composition filled in the second container are mixed, and the powder composition is dissolved in the liquid composition by mixing them.
[0022] In the two-chamber container-type external skin preparation of the present invention, the powder composition contains cyclodextrin-encapsulated retinol and amino acids.
[0023] Retinol (vitamin A1) is a pharmacologically active substance that has cosmetic effects such as promoting the turnover of epidermal cells and increasing skin elasticity, and is the main active ingredient in the two-chamber container-type external skin preparation of the present invention.
[0024] Retinol is also stabilized by being encapsulated (clathrated) in a host compound, cyclodextrin.
[0025] In this way, by encapsulating retinol, which is inherently unstable, in cyclodextrin and using a two-chamber container to prepare a liquid topical skin preparation just before use, users can use retinol in a fresher state.
[0026] The powder composition also contains amino acids. Amino acids function as a dissolution promoter and can increase the solubility of the cyclodextrin-encapsulated retinol in the liquid composition, allowing the cyclodextrin-encapsulated retinol to be suitably dissolved in the liquid composition during use. Furthermore, the inclusion of amino acids can provide excellent storage stability for the powder composition and the two-chamber container-type skin topical preparation according to the present invention.
[0027] In particular, in the two-chamber container-type external skin preparation of the present invention, the viscosity of the liquid composition measured at 25° C. using a B-type viscometer at a rotation speed of 60 rpm is 20 mPa·s or more and 1000 mPa·s or less.
[0028] This allows the powder composition and the liquid composition to be efficiently contacted and mixed in the two-chamber container when the liquid topical skin preparation is prepared just before use, and allows the cyclodextrin-encapsulated retinol to be suitably dissolved in the liquid composition. As a result, it is possible to suitably prevent undesired insoluble matter from being contained in the liquid topical skin preparation prepared just before use, and the feel of the topical skin preparation when used can be improved.
[0029] The two-chamber container type topical skin preparation of the present invention exerts each of the effects described above, and these effects act synergistically, so that, as described above, it is possible to provide a two-chamber container type topical skin preparation that allows the function of retinol to be fully exerted at the time of use even when stored for a long period of time, and that has increased solubility of cyclodextrin-encapsulated retinol in the liquid composition when prepared just before use.
[0030] On the other hand, if the above conditions are not met, satisfactory results will not be obtained. Specifically, for example, if retinol is not included in cyclodextrin, the retinol remains oil-soluble and cannot be sufficiently dissolved in a liquid composition containing water. In addition, retinol is not stabilized, resulting in significantly poor storage stability.
[0031] In addition, for example, if the powder composition does not contain amino acids, the solubility in the liquid composition is low, and the powder composition cannot be sufficiently dissolved in the liquid composition when preparing it for use, resulting in the presence of a large amount of unnecessary substances. In particular, such a problem becomes more pronounced when the two-chamber container-type external skin preparation is stored for a long period of time.
[0032] Furthermore, for example, if the viscosity of the liquid composition exceeds 1000 mPa·s, it becomes difficult to sufficiently dissolve the powder composition when preparing a liquid external skin preparation just before use.
[0033] Furthermore, if the viscosity of the liquid composition is less than 20 mPa·s, the powder composition will settle when the liquid topical skin preparation is prepared just before use, making it difficult to dissolve it sufficiently.
[0034] [1-1]Two-chamber container The two-chamber container constituting the two-chamber container-type external skin preparation of the present invention will be described below.
[0035] Fig. 1 is a diagram showing one example of the configuration of a two-chamber container, showing the state before use, and Fig. 2 is a diagram showing the state when the two-chamber container shown in Fig. 1 is in use.
[0036] In this embodiment, the two-chamber container comprises, for example, a first container (inner container) and a second container (outer container) having a larger internal volume than the first container, and the first container is inserted into the second container to combine the two containers.
[0037] When the external skin preparation is not in use (before use), the inside of the first container and the inside of the second container are not in communication with each other and are partitioned into two chambers. When the external skin preparation is in use, the inside of the first container and the inside of the second container are in communication with each other.
[0038] The two-chamber container 10 shown in FIG. 1 comprises a first container (inner container) 11, a second container (outer container) 12, a valve member 16, and an opening / closing part 21.
[0039] The first container (inner container) 11 has a cylindrical shape with a bottom, and the internal space of the first container 11 defines a first chamber 11a. The second container (outer container) 12 has a cylindrical shape with a bottom, and the internal space of the second container 12 defines a second chamber 12a.
[0040] The first container 11 is disposed with its open end facing downward and inserted into the second container 12. A valve member 16 is provided at the open end of the first container 11.
[0041] The valve member 16 is attached so as to be able to open and close the open end of the first container 11, and can take a closed position shown in FIG. 1 and an open position shown in FIG. 2 by operating the operating head 25 of the opening / closing part 21.
[0042] As a result, the two-chamber container 10 is divided into two chambers whose interiors can communicate with each other, in other words, into a first chamber 11a and a second chamber 12a.
[0043] The volume of the internal space (first chamber 11a) of the first container 11 is not particularly limited, but is preferably 1.0 cm 3 More than 7.0cm 3 Preferably less than 1.4cm 3 More than 5.0cm 3 Preferably less than 1.8 cm 3 More than 3.0cm 3 It is even more preferable that:
[0044] This makes it possible to prevent the two-chamber container 10 from becoming larger than necessary, while also allowing the powder composition P to be more suitably dissolved in the liquid composition L when prepared just before use.
[0045] The volume of the internal space of the second container 12 (the second chamber 12a; the portion of the internal space of the second container 12 excluding the space occupied by the first container 11) is not particularly limited, but is preferably 5 cm3 More than 60cm 3 Preferably less than 10cm 3 Over 45cm 3 Preferably less than 15cm 3 More than 30cm 3 It is even more preferable that:
[0046] This makes it possible to prevent the two-chamber container 10 from becoming larger than necessary, while also allowing the powder composition P to be more suitably dissolved in the liquid composition L when prepared just before use.
[0047] The volume of the internal space (first chamber 11a) of the first container 11 is V1 [cm 3 ], and the volume of the internal space of the second container 12 (the second chamber 12a; the portion of the internal space of the second container 12 excluding the space occupied by the first container 11) is V2 [cm 3 When V1 / V2 is 0.05≦V1 / V2≦0.20, V1 / V2 preferably satisfies the relationship 0.08≦V1 / V2≦0.14, and V1 / V2 preferably satisfies the relationship 0.10≦V1 / V2≦0.12.
[0048] This makes it possible to prevent the two-chamber container 10 from becoming larger than necessary, while also allowing the powder composition P to be more suitably dissolved in the liquid composition L when prepared just before use.
[0049] An opening / closing part 21 is provided at the open end of the second container 12. The opening / closing part 21 is, for example, a spray mechanism, and has a circular top wall 22, a spray base 23, a straw 24, an operating head 25, and a nozzle 26.
[0050] The top wall 22 covers the open end of the second container 12. The spray base 23 is provided at approximately the center of the top wall 22 and protrudes outward from the end face of the top wall 22. The straw 24 extends toward the bottom of the second container 12.
[0051] The operating head 25 is slidably attached to the spray base 23, and can be moved between a closed position shown in Fig. 1 and an ejection position retracted from the closed position into the spray base 23 as shown in Fig. 2 by a spring (not shown) provided inside the spray base 23. The nozzle 26 is an ejection port for the liquid stored in the second container 12, and is provided on the side of the operating head 25.
[0052] Before use, the first container 11 is filled with the powder composition P, and the second container 12 is filled with the liquid composition L. Here, before use, the first container 11 is closed by the valve member 16, and therefore the liquid composition L does not flow from the second container 12 to the first container 11 side.
[0053] Furthermore, when the operating head 25 is in the closed position, the opening / closing part 21 is closed and the path from the straw 24 to the nozzle 26 is closed.
[0054] The method for preparing the topical skin preparation just before use using such a two-chamber container will be described in detail later.
[0055] [1-2] Powder composition Next, the powder composition will be described.
[0056] The powder composition contains cyclodextrin-encapsulated retinol and amino acids, and is filled in a first container (inner container) of a two-chamber container.
[0057] [1-2-1] Cyclodextrin-encapsulated retinol Retinol (vitamin A1) is a compound that has an isoprenoid polyene alcohol as its basic structure.
[0058] In this specification, "retinol" includes pharma- ceutically acceptable salts and pharma-ceutically acceptable derivatives. Examples of the derivatives include carboxylic acid esters of retinol, etc. More speci?cally, examples of the derivatives include esters having 1 to 30 carbon atoms, such as retinol acetate and retinol palmitate. In the present invention, the retinol may be used alone or in combination of tWo or more.
[0059] By including retinol in a host compound such as cyclodextrin to form an inclusion compound, the water solubility of retinol is increased, and the stability and duration of the effect of retinol itself are improved.
[0060] Examples of cyclodextrin include hydroxypropyl β-cyclodextrin, sulfobutyl ether β-cyclodextrin, methyl β-cyclodextrin (MβCD), and the like. One or a combination of two or more selected from these can be used.
[0061] The content of cyclodextrin-encapsulated retinol in the powder composition is preferably 20.0% by mass or more and 80.0% by mass or less, more preferably 30.0% by mass or more and 70.0% by mass or less, and even more preferably 35.0% by mass or more and 65.0% by mass or less.
[0062] This makes it possible to ensure that the content of amino acids in the powder composition is sufficiently high, and while fully exerting the effects described above, it is possible to ensure that the content of cyclodextrin-encapsulated retinol in the powder composition and the content of cyclodextrin-encapsulated retinol in the liquid topical skin preparation obtained by preparation just before use are sufficiently high, allowing the functions of retinol to be more effectively exerted in the topical skin preparation.
[0063] [1-2-2] Amino acids The powder composition contains amino acids.
[0064] In the present invention, the term "amino acids" refers to compounds that have an amino group and a carboxy group or a sulfo group in the molecule, and compounds that belong to the group consisting of derivatives thereof.
[0065] Examples of amino acids include amino acids and mucopolysaccharides, and salts thereof.
[0066] Among the amino acids, examples of the amino acids include monoaminomonocarboxylic acids such as glycine, alanine, γ-aminobutyric acid, γ-aminovaleric acid, etc., monoaminodicarboxylic acids such as aspartic acid, glutamic acid, etc., diaminomonocarboxylic acids such as arginine, lysine, etc., and derivatives such as aminoethylsulfonic acid (taurine), etc. The amino acids may be in any of the L-, D-, and DL-forms.
[0067] Among amino acids, mucopolysaccharides and derivatives thereof include, for example, acidic mucopolysaccharides such as derivatives of chondroitin sulfate, hyaluronic acid, alginic acid, and the like.
[0068] Examples of salts of amino acids and salts of mucopolysaccharides include salts with organic acids (e.g., monocarboxylates (acetates, trifluoroacetates, butyrates, palmitates, stearates, etc.), polycarboxylates (fumarates, maleates, etc.), oxycarboxylates (lactates, tartrates, citrates, succinates, malonates, etc.), organic sulfonates (methanesulfonates, toluenesulfonates, etc.), etc.), salts with inorganic acids (e.g., hydrochlorides, sulfates, nitrates, hydrobromides, phosphates, etc.), salts with organic bases (e.g., salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, picoline, etc.), salts with inorganic bases (e.g., ammonium salts; salts with alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), aluminum, etc.), etc.).
[0069] In the present invention, the amino acids include betaines. In the present invention, betaines refer to compounds (inner salts) that have a positive charge and a negative charge at non-adjacent positions in the same molecule, and the positively charged atom is not bound to dissociable hydrogen, and the molecule as a whole does not have a charge. Examples of the chemical structure (cation structure) that is constituted by the positively charged atom include quaternary ammonium, sulfonium, phosphonium, etc.
[0070] The above-mentioned betaines generally exhibit high water solubility themselves and also function as a dissolution promoter for cyclodextrin-included retinol, thereby increasing the solubility of cyclodextrin-included retinol in a liquid composition. In addition, betaines can increase the storage stability of cyclodextrin-included retinol by coexisting with cyclodextrin-included retinol in a powder composition. Furthermore, by including betaines, a liquid skin topical preparation prepared just before use can exhibit excellent moisturizing effect (water retention). Furthermore, by including betaines, an antistatic effect can be exhibited.
[0071] Examples of betaines include alkyl betaines, N-alkylamide betaines and derivatives thereof, and sultaines. More specifically, N-trialkyl substituted amino acids such as betaine (trimethylglycine), γ-butyrobetaine, β-alanine betaine, glutamic acid betaine, phenylalanine betaine, alanine betaine, valine betaine, lysine betaine, ornithine betaine, taurobetaine, homarine, trigonelline, carnitine, atrinin, homoserine betaine, anthopleurin, and stachydrine can be used alone or in combination of two or more selected from these.
[0072] Among these, betaine (trimethylglycine) is preferred as the amino acid. This makes it possible to make the above-mentioned effects more pronounced.
[0073] The content of amino acids in the powder composition is preferably 10.0% by mass or more and 80.0% by mass or less, more preferably 15.0% by mass or more and 70.0% by mass or less, and even more preferably 17.5% by mass or more and 65.0% by mass or less.
[0074] This allows the effects of containing amino acids as described above to be fully exerted, while also making it possible to sufficiently increase the content of cyclodextrin-encapsulated retinol in the powder composition and the content of cyclodextrin-encapsulated retinol in the liquid topical skin preparation obtained by preparation just before use, allowing the functions of retinol to be more effectively exerted in the topical skin preparation.
[0075] [1-2-3]Polysaccharides The powder composition may further contain a polysaccharide. The polysaccharide functions as a dissolution promoter and can increase the solubility of the cyclodextrin-encapsulated retinol in the liquid composition, and can suitably dissolve the cyclodextrin-encapsulated retinol in the liquid composition during use. Furthermore, by containing a polysaccharide, the storage stability of the powder composition and the two-chamber container-type external skin preparation according to the present invention can be improved.
[0076] As used herein, a polysaccharide refers to a compound having a chemical structure in which two or more monosaccharide molecules are linked together via glycosidic bonds.
[0077] Examples of polysaccharides include sucrose, lactose, maltose, trehalose, starch, glycogen, cellulose, chitin, pectin, etc., and one or more selected from these may be used in combination.
[0078] Among these, trehalose is preferred as the polysaccharide. This makes it possible to make the above-mentioned effects more pronounced.
[0079] When the powder composition contains a polysaccharide, the content of the polysaccharide in the powder composition is preferably 0.5 mass% or more and 40.0 mass% or less, more preferably 1.0 mass% or more and 35.0 mass% or less, and even more preferably 2.0 mass% or more and 32.5 mass% or less, relative to the total amount of the powder composition. This makes it possible to make the above-mentioned effects more pronounced.
[0080] When the content of cyclodextrin-encapsulated retinol in the powder composition is Xr [% by mass], the content of amino acids in the powder composition is Xa [% by mass], and the content of polysaccharides in the powder composition is Xs [% by mass], it is preferable to satisfy the relationship of 0.25≦(Xa+Xs) / Xr≦4.00, it is more preferable to satisfy the relationship of 0.43≦(Xa+Xs) / Xr≦2.33, and it is even more preferable to satisfy the relationship of 0.54≦(Xa+Xs) / Xr≦1.86. This makes it possible to make the above-mentioned effects more pronounced.
[0081] [1-2-4] Other ingredients The powder composition may contain components other than those mentioned above. Hereinafter in this section, such components will be referred to as "other components".
[0082] Examples of other ingredients include plant extracts, vitamins, vitamin-like substances, mineral antioxidants, UV absorbers, pigments, preservatives, fragrances, other active ingredients (medicinal ingredients), and the like.
[0083] However, the content of other components in the powder composition is preferably 5% by mass or less, and more preferably 1% by mass or less.
[0084] [1-3]Liquid composition Next, the liquid composition will be described. The liquid composition is filled into the second container (the outer container) of the two-chamber container.
[0085] The liquid composition contains as a main component a liquid diluent that functions as a solvent and a dispersion medium for the above-mentioned powder composition.
[0086] As described above, the viscosity of the liquid composition, measured at 60 rpm using a B-type viscometer in an environment of 25°C, is from 20 mPa·s to 1000 mPa·s, but the viscosity of the liquid composition is preferably from 20 mPa·s to 800 mPa·s, and more preferably from 20 mPa·s to 500 mPa·s. This makes it possible to make the above-mentioned effects of the present invention more pronounced.
[0087] The viscosity of the liquid composition can be adjusted to fall within the above range, for example, by adding a component that functions as a thickener or by adjusting the concentration of the components contained in the liquid composition.
[0088] [1-3-1] Diluent The liquid composition contains as a main component a liquid diluent that functions as a solvent and a dispersion medium for the above-mentioned powder composition.
[0089] Such a liquid diluent is not particularly limited as long as it is liquid at room temperature (25°C) and can dissolve the above-mentioned powder composition, particularly the cyclodextrin-encapsulated retinol, and examples thereof include water, monohydric alcohols such as ethanol, and polyhydric alcohols such as 1,3-butylene glycol, propanediol, glycerin, and ethylhexylglycerin. In particular, the above-mentioned polyhydric alcohol components can function as a solvent and a dispersion medium, and can also function as a moisturizing component. In addition, by including these polyhydric alcohol components and mixing them with the powder composition during use, the above-mentioned moisturizing effect can be more significantly exhibited due to the synergistic effect with the effect of retinol in promoting the turnover of epidermal cells.
[0090] The content of the diluent in the liquid composition is preferably 60.0% by mass or more and 99.9% by mass or less, more preferably 70.0% by mass or more and 99.8% by mass or less, and even more preferably 80.0% by mass or more and 99.7% by mass or less.
[0091] This allows the cyclodextrin-encapsulated retinol to be more suitably dissolved when preparing a liquid topical skin preparation just before use.
[0092] It is preferable that the diluent contains at least water, and the water content in the liquid composition is preferably 50.0% by mass or more and 93.0% by mass or less, more preferably 60.0% by mass or more and 90.0% by mass or less, and even more preferably 65.0% by mass or more and 87.0% by mass or less.
[0093] This allows the cyclodextrin-encapsulated retinol to be more suitably dissolved when the liquid topical skin preparation is prepared just before use.
[0094] [1-3-2] Fermented products The liquid composition preferably contains a fermentation product obtained by fermenting rice bran and legume-derived peptides with Bacillus subtilis.
[0095] This allows the skin external preparation to have excellent collagen synthesis and cell proliferation effects.
[0096] Furthermore, when mixed with the retinol contained in the powder composition at the time of use, the above-mentioned effects can be more pronounced due to a synergistic effect with the effect of retinol to promote the turnover of epidermal cells in the skin.
[0097] Examples of rice bran include rice bran, defatted rice bran, rice germ, and defatted rice germ, and one or more selected from these can be used in combination. The rice bran is not limited to commercially available rice bran, and various types of rice bran can be used.
[0098] The specific type and structure of the legume-derived peptide is not particularly limited as long as it is a peptide contained in legumes or a peptide derived from a protein contained in legumes. The legume-derived peptide is not limited to commercially available legume-derived peptides, and various types of legume-derived peptides can be used. Examples of the legume-derived peptide include soybean peptide, adzuki bean peptide, pea peptide, and broad bean peptide. The legume-derived peptide is preferably soybean peptide. The legume-derived peptide may be used alone or in combination of two or more types.
[0099] There is no particular limitation on the method for obtaining the legume-derived peptide. For example, the legume-derived peptide can be obtained by extracting legumes (e.g., one or more types selected from soybeans, red beans, peas, broad beans, etc.) with a solvent (water, hot water, an organic solvent such as alcohol (ethanol, etc.), or a water-organic solvent mixture). In this process, fractionation and purification, etc. can be performed as necessary. Furthermore, the obtained legume-derived peptide or legume protein can be further fragmented by hydrolysis treatment with protease, acid, or alkali. Furthermore, the legume-derived peptide may be a peptide artificially synthesized by chemically bonding amino acids together into peptide bonds or by known genetic engineering techniques.
[0100] The form of the bean-derived peptide is not particularly limited. The bean-derived peptide can be a solid (e.g., powder or granules) solidified by drying or the like after the above-mentioned extraction. The extract itself can be used as the bean-derived peptide. That is, an extract containing the bean-derived peptide (bean extract, particularly soybean extract, etc.) can be used as the bean-derived peptide. For example, an extract obtained by extracting beans (e.g., one or more selected from soybeans, red beans, peas, broad beans, etc.) with a solvent (water, hot water, organic solvent such as alcohol (ethanol, etc.), or a water-organic solvent mixture) can be used as the bean-derived peptide. In particular, an extract containing soybean peptide (soybean extract) and the like can be preferably used.
[0101] There are no particular limitations on the extraction method and extraction conditions for obtaining an extract containing the bean-derived peptide. For example, the beans used as the extraction raw material may be unground or ground. As long as the quality of the extract can be maintained, pretreatment such as removal of impurities may be performed. As the extraction solvent, in addition to water or hot water, alcohols such as methanol and ethanol, esters such as ethyl acetate, organic solvents such as n-hexane, and mixed solvents of these organic solvents with water or hot water can be used. As the extraction solvent, water or hot water, alcohols (e.g., methanol and ethanol), and mixed solvents of water or hot water with alcohol are preferred.
[0102] The temperature of the hot water is, for example, 40°C or more and 100°C or less, preferably 50°C or more and 80°C or less, and more preferably 50°C or more and 70°C or less.
[0103] The pH of the extraction solvent during extraction is, for example, 3 or more and 7 or less, preferably 4 or more and 6 or less, and more preferably 4 or more and 5 or less. This allows the stability of the various components contained in the extraction raw material to be maintained.
[0104] The extraction may be performed at room temperature or may be performed with heating. When the extraction is performed with heating, the heating temperature is, for example, from 40°C to 100°C, preferably from 50°C to 80°C, and more preferably from 50°C to 70°C. This allows the extraction to be carried out efficiently.
[0105] The ratio of the rice bran to the legume-derived peptide is not particularly limited. Usually, the ratio of the rice bran is, for example, 1 part by mass to 20 parts by mass, preferably 5 parts by mass to 20 parts by mass, and more preferably 8 parts by mass to 18 parts by mass, based on 100 parts by mass of the legume-derived peptide. This makes it possible to obtain a fermented product having superior collagen synthesis activity, etc.
[0106] The Bacillus subtilis is a representative type of aerobic spore-forming bacteria. The type of the Bacillus subtilis is not particularly limited as long as its safety is guaranteed. For example, Bacillus natto can be used as the Bacillus subtilis. As the Bacillus subtilis, Bacillus natto is preferable because it is easy to obtain and inexpensive. In addition, as the Bacillus subtilis, a general Bacillus subtilis that is commercially available can be used. In addition, as long as a fermented product having collagen synthesis activity and the like can be obtained, the Bacillus subtilis can be a mutant strain that has been generated naturally or artificially by means of chemical substances such as nitrosoguanidine, X-rays, ultraviolet rays, etc., and has mutated bacteriological properties.
[0107] The fermented product is obtained by fermenting the rice bran and the legume-derived peptide with Bacillus subtilis. The fermented product is usually obtained by inoculating Bacillus subtilis into a medium containing the rice bran and the legume-derived peptide, and culturing the mixture under appropriate conditions. There are no particular limitations on the fermentation culture conditions for obtaining the fermented product. The fermentation culture is usually performed by aeration and stirring.
[0108] The medium is not particularly limited as long as it allows the Bacillus subtilis to grow in. The medium is usually a liquid medium, but may be a solid medium.
[0109] The pH of the medium (particularly during fermentation) is, for example, from 5.5 to 8.5, preferably from 6.0 to 8.0, and more preferably from 6.5 to 7.5. This allows the stability of the various components contained in the extraction raw material to be optimally maintained.
[0110] Furthermore, the culture temperature is not particularly limited as long as fermentation is performed, and is, for example, from 15°C to 50°C, preferably from 20°C to 45°C, more preferably from 30°C to 45°C, and even more preferably from 35°C to 43°C.
[0111] In addition, various nutrients such as sugar, and acids and alkalis for adjusting the pH, etc. may be added to the medium. Furthermore, the fermentation may be mixed fermentation or continuous fermentation.
[0112] The form of the fermented product is not particularly limited. The fermented product may be a fermentation liquid obtained by fermentation culture or a liquid obtained by filtering the fermented liquid. The fermented product may be a fermented liquid that has been sterilized or pH adjusted as necessary, or that has been subjected to post-treatment such as deodorization and decolorization using an ion exchange resin, an activated carbon column, or a dialysis membrane. The fermented product may be a concentrated liquid or a paste-like product obtained by concentrating the fermented liquid. The fermented product may also be a solid product obtained by removing the solvent from the fermented liquid by a known method such as freeze-drying, or a powder product obtained by powdering the fermented liquid. The fermented product may be a solution or dispersion obtained by adding the fermented liquid or the solid product or powder product to water or an organic solvent such as ethanol, propylene glycol, or 1,3-butylene glycol, or a mixture thereof.
[0113] The solid content of the fermented product in the liquid composition is preferably 0.001% by mass or more and 2.0% by mass or less, more preferably 0.01% by mass or more and 1.0% by mass or less, and even more preferably 0.03% by mass or more and 0.5% by mass or less.
[0114] This ensures that the solubility of the cyclodextrin-encapsulated retinol in the liquid composition is sufficiently excellent, while the effect of including the fermentation product as described above becomes more pronounced.
[0115] When the mass of amino acids contained in the two-chamber vessel 10 is WA [mg] and the mass of the solid content of the fermentation product contained in the two-chamber vessel 10 is WF [mg], it is preferable to satisfy the relationship 0.01≦WF / WA≦1.0, it is more preferable to satisfy the relationship 0.03≦WF / WA≦0.50, and it is even more preferable to satisfy the relationship 0.05≦WF / WA≦0.30.
[0116] This makes it possible to provide a more excellent moisturizing sensation when the liquid skin topical preparation prepared just before use is applied to the skin, and the excellent moisturizing sensation can be maintained for a longer period of time.
[0117] [1-3-3] Sphingomonas culture extract Preferably, the liquid composition comprises a Sphingomonas culture extract.
[0118] The Sphingomonas culture extract acts as a thickener in the liquid composition, and can adjust the viscosity of the liquid composition to the above-mentioned range. The Sphingomonas culture extract also acts as a dissolution promoter and dispersant for the components of the powder composition, and can disperse the powder composition, particularly the cyclodextrin-encapsulated retinol, in the liquid composition when mixed with the powder composition during use. This makes it possible to make the above-mentioned effects of the present invention even more remarkable.
[0119] In addition, Sphingomonas culture extract has excellent cosmetic effects, specifically, for example, moisturizing effect, cell activation effect (skin roughness prevention effect), anti-atopic effect, etc. Therefore, when the liquid composition contains Sphingomonas culture extract, the cosmetic effect of the external skin preparation can be made more excellent.
[0120] Furthermore, when mixed with the retinol contained in the powder composition during use, a synergistic effect with the effect of retinol in promoting the turnover of epidermal cells in the skin can be achieved, thereby more significantly exerting the above-mentioned beauty effects (moisturizing effect, skin roughness prevention effect, anti-atopic effect, etc.).
[0121] Sphingomonas culture extract is an extract obtained by a manufacturing method including a step of extracting a culture of a bacterium belonging to the genus Sphingomonas, and contains, as an active ingredient, sphingoglycolipids, which are glycolipids in which various sugars are bound to ceramide, a sphingolipid.
[0122] More specifically, for example, as disclosed in JP-A-10-330273, it can be obtained by a production method including a step of culturing a bacterium belonging to the genus Sphingomonas, washing it with acetone, and then extracting it with alcohol or an alcohol / water mixture.
[0123] Such Sphingomonas culture extract is commercially available, for example, as "Kelcocare Diutan Gum" from Lubrizol Corporation (Kelcocare is a trademark of CP Kelco).
[0124] The content of Sphingomonas culture extract in the liquid composition (in the case where the Sphingomonas culture extract contains volatile liquid components, the content of solids excluding the liquid components) is preferably 0.001 mass% or more and 0.6 mass% or less, more preferably 0.01 mass% or more and 0.5 mass% or less, and even more preferably 0.02 mass% or more and 0.4 mass% or less.
[0125] This makes it possible to make the above-mentioned effects of the present invention even more pronounced, and also makes the cosmetic effects of the topical skin preparation (moisturizing effect, skin roughness prevention effect, anti-atopic effect, etc.) even more excellent.
[0126] When the mass of amino acids contained in the two-chamber container 10 is WA [mg] and the mass of Sphingomonas culture extract contained in the two-chamber container 10 (if the Sphingomonas culture extract contains volatile liquid components, the mass of the solids excluding the liquid components) is WS [mg], it is preferable to satisfy the relationship of 0.01≦WS / WA≦1.0, it is more preferable to satisfy the relationship of 0.03≦WS / WA≦0.50, and it is even more preferable to satisfy the relationship of 0.05≦WS / WA≦0.30.
[0127] This allows the liquid skin topical preparation obtained by preparation just before use to have a smoother feel on the skin when applied to the skin, and provides an after-skin feel with more effectively suppressed stickiness.
[0128] [1-3-4] Other ingredients The liquid composition may contain components other than those mentioned above. Hereinafter in this section, such components will be referred to as "other components".
[0129] Other ingredients include, for example, plant extracts, vitamins, vitamin-like substances, minerals, oils and fats, thickeners, gelling agents, pH adjusters, antioxidants, colorants, stabilizers such as lactose, solubilizers such as glutamic acid and aspartic acid, preservatives, pH adjusters, surfactants, wetting agents, emulsifiers, dispersants, emulsions, solutions, suspensions, elixirs, fragrances, flavors, other active ingredients (medicinal ingredients), and the like.
[0130] An example of a thickening agent is xanthan gum. By including a thickener in the liquid composition, the viscosity of the liquid composition can be more suitably adjusted to fall within the above-mentioned range.
[0131] Examples of pH adjusters include citric acid and sodium citrate. An example of a preservative is phenoxyethanol. An example of the surfactant is hydrogenated castor oil (PEG-4).
[0132] However, the content of other components in the liquid composition is preferably 5% by mass or less, and more preferably 1% by mass or less.
[0133] [2] Method for preparing topical skin preparations just before use Next, a method for preparing an external skin preparation just before use using a two-chamber container will be described. FIG. 3 is a diagram showing a method for preparation just before use using the two-chamber container shown in FIG. 1 and FIG.
[0134] As described above, before use, the first container (inner container) 11 of the two-chamber container 10 is filled with the powder composition P, and the second container (outer container) 12 is filled with the liquid composition L.
[0135] Here, when not in use, the open end of the first container 11 is closed by the valve member 16, so that the liquid composition L does not flow from the second container 12 into the first container 11 side.
[0136] When using the topical skin preparation, the powder composition P in the first container 11 and the liquid composition L in the second container 12 are mixed, and the powder composition P is dissolved in the liquid composition L before use.
[0137] Specifically, when in use, when the user presses the operating head 25 with the fingers of his / her hand, the valve member 16 is pushed down, forming a gap 17 between the open end of the first container 11 and the valve member 16, thereby connecting the first chamber 11a and the second chamber 12a.
[0138] The liquid composition L flows from the second container 12 into the first container 11 through this gap 17 and is mixed with the powder composition P.
[0139] In this case, the size of the gap 17 indicated by d in FIG. 2 is preferably 1 mm or more and 20 mm or less, more preferably 2 mm or more and 15 mm or less, and even more preferably 3 mm or more and 10 mm or less.
[0140] This prevents the two-chamber container 10 from becoming unnecessarily large, while allowing the liquid composition L to flow more efficiently into the first container 11, and allows the powder composition P to be more efficiently dissolved in the liquid composition L.
[0141] The powder composition P is then dissolved in the liquid composition L to prepare the external skin preparation. In particular, in the present invention, by specifying the viscosity of liquid composition L, the cyclodextrin-encapsulated retinol can be sufficiently dissolved in liquid composition L when prepared just before use, allowing the functions of retinol to be fully exerted and improving the feel of the topical skin preparation when used. Furthermore, by preparing just before use, the user can use retinol in a fresher state.
[0142] As shown in FIG. 3, when preparing the liquid just before use, it is preferable to shake the two-chamber container 10 with the first chamber 11a and the second chamber 12a in communication with each other. This makes it possible to dissolve the powder composition P in the liquid composition L more reliably.
[0143] The number of shaking times is not particularly limited, but is preferably 10 times or more, and more preferably 20 times or more. This makes it possible to dissolve the powder composition P in the liquid composition L more reliably.
[0144] When the user further presses the operating head 25 with the fingers of the hand, the opening / closing part 21 opens, opening the path from the straw 24 to the nozzle 26. This causes the liquid stored in the second container 12, in other words, the prepared topical skin agent, to be taken out, and a predetermined amount of liquid is measured by the spray base 23 and sprayed from the nozzle 26 to the outside of the container.
[0145] In the two-chamber container-type topical skin preparation of the present invention, when the mass of powder composition P is Wi [g] and the mass of liquid composition L is Wo [g], it is preferable to satisfy the relationship of 0.001≦Wi / Wo≦0.10, it is more preferable to satisfy the relationship of 0.003≦Wi / Wo≦0.07, and it is even more preferable to satisfy the relationship of 0.007≦Wi / Wo≦0.05. This makes it possible to make the above-mentioned effects of the present invention more pronounced.
[0146] The skin topical preparation prepared as described above may be any product that is used by contacting the skin (including nails) or mucous membrane of an animal (including human), and examples of such products include medicines; quasi-drugs; skin care products such as lotions, creams, milky lotions, beauty essences, whitening agents, and face washes (including face cleansers); hair removal-related products such as shaving lotions, depilatories, and skin conditioners for after shaving; hair care products such as hair treatments; and other products such as body soaps, hand washing detergents (hand soaps), anti-aging agents, antiperspirants, sunscreens, sunburn accelerators, perfumes, cooling sprays, and bath additives. Among these, the skin topical preparation according to the present invention is preferably selected from the group consisting of lotions, milky lotions, and beauty essences.
[0147] Although the preferred embodiments of the present invention have been described above, the present invention is not limited to these.
[0148] For example, in the above description, a two-chamber container is described that includes a first container (inner container) and a second container (outer container) having a larger internal volume than the first container, and the first container is inserted inside the second container. However, the present invention is not limited to this, and any two-chamber container can be used as long as it is divided into two chambers and the two chambers can communicate with each other when used. For example, the two-chamber container may include a first container as an outer container and a second container as an inner container. In addition, the two-chamber container may include a first container and a second container that are arranged in parallel, not in the relationship of an inner container and an outer container (one container is not inserted inside the other container). In addition, the two-chamber container may include at least two chambers including at least a first chamber and a second chamber, and may include three or more chambers. EXAMPLES
[0149] Next, specific examples of the present invention will be described. However, the present invention is not limited to the descriptions in these examples.
[0150] [3] Manufacturing of two-compartment container-type topical skin preparations Example 1 First, a powder composition was prepared as follows.
[0151] A powder composition was prepared by mixing the cyclodextrin-encapsulated retinol and betaine in the ratio shown in Table 1.
[0152] As the cyclodextrin-encapsulated retinol, "CAVAMAX W8 Retinol Complex" manufactured by CycloChem was used.
[0153] Next, a liquid composition was prepared as follows. A liquid composition was prepared by mixing water, a fermentation product obtained by fermenting rice bran and bean-derived peptides using Bacillus subtilis, powdered Sphingomonas culture extract (Lubrizol, Kelcocare Diutan Gum), butylene glycol, propanediol, glycerin, ethylhexylglycerin, citric acid, sodium citrate, hydrogenated castor oil (PEG-40), and fragrance in the proportions shown in Table 1.
[0154] The fermented product obtained by fermenting rice bran and bean-derived peptides with Bacillus subtilis was prepared as follows.
[0155] That is, first, 3 kg of rice bran, 0.4 kg of soybean peptide, 0.5 kg of glucose, 0.01 kg of alkaline protease, and 50 kg of purified water were mixed to prepare a medium. Thereafter, the pH of the medium was adjusted to 6.0 to 8.0, and then Bacillus subtilis natto was inoculated and cultured at 37°C for 38 hours to carry out fermentation. Thereafter, the fermented liquid was squeezed and filtered, and then decolorized and deodorized with activated carbon. Thereafter, the fermented liquid was filtered again and purified to produce a fermented product.
[0156] The viscosity of the liquid composition was 50 mPa·s when measured at 60 rpm using a Brookfield viscometer in an environment of 25° C.
[0157] A two-chamber container-type external skin preparation was produced by filling the inner container with 0.2 g of the powder composition and filling the outer container with 14 mL of the liquid composition as shown in FIG.
[0158] The volume V1 of the internal space (first chamber) of the inner container (first chamber) of a two-chamber container is 2.0 cm 3 The volume V2 of the internal space of the outer container (second container) of the two-chamber container (the second chamber, excluding the space occupied by the first container) is 20 cm 3 It was.
[0159] (Examples 2 to 5) A two-chamber container-type external skin preparation was produced in the same manner as in Example 1, except that the powder composition and liquid composition had the configurations shown in Table 1.
[0160] (Comparative Examples 1 to 4) A two-chamber container-type external skin preparation was produced in the same manner as in Example 1, except that the powder composition and liquid composition had the configurations shown in Table 1.
[0161] [4] Evaluation In each of the above-mentioned examples and comparative examples, the two-chamber container-type topical skin preparations were each prepared by pressing the operating head of the two-chamber container to release the inner container, and then shaking the container 20 times while holding it in the hand. The state inside the two-chamber container was then visually observed, and the solubility of the powder composition in the liquid composition was evaluated according to the following criteria.
[0162] A: No residual powder composition is found. B: Almost no residual powder composition is observed. C: A small amount of undissolved powder composition was observed. D: Undissolved powder composition is clearly observed. E: Residual powder composition is significantly found.
[0163] In addition, after shaking the two-chamber container 20 times as described above, it was left at room temperature for one week, after which the state inside the two-chamber container was visually observed and the degree of settling of the solids was evaluated according to the following criteria.
[0164] A: No settling of solids was observed. B: Almost no settling of solids is observed. C: Slight settling of solids is observed. D: Sedimentation of solids is clearly observed. E: Sedimentation of solids is clearly observed.
[0165] The compositions and blending amounts of the powder composition and liquid composition, the viscosity of the liquid composition, and the evaluation results for each of the above-mentioned Examples and Comparative Examples are summarized in Table 1. In Table 1, the unit of the content of each component is parts by mass, and the solid content of the fermented product obtained by fermenting the rice bran and bean-derived peptide obtained as described above with Bacillus subtilis is shown as "fermented product with Bacillus subtilis," and Kelcocare Diutan Gum, manufactured by Lubrizol Corporation, is shown as "Sphingomonas culture extract." In addition, the viscosity value of the liquid composition is the viscosity value measured for the liquid composition at 25°C using a B-type viscometer at a rotation speed of 60 rpm.
[0166] [Table 1]
[0167] As is clear from Table 1, in each of the above examples, no residual powder composition was found, and it was confirmed that the powder composition was suitably dissolved in the liquid composition. Furthermore, no sedimentation of solids was observed even one week after mixing.
[0168] In contrast, the comparative examples did not provide satisfactory results. Specifically, residual powder composition was observed in Comparative Example 4, in which the powder composition did not contain amino acids, and in Comparative Example 2, in which the liquid composition had a viscosity of more than 1000 mPa s. Moreover, in Comparative Example 1, in which the liquid composition had a viscosity of less than 20 mPa s, the powder composition settled and was not sufficiently dissolved, resulting in residual powder composition.
[0169] Two-chamber container-type topical skin preparations were produced in the same manner as above, except that the viscosity of the liquid composition measured under the above conditions was variously changed within the range of 20 mPa·s or more and 1000 mPa·s or less by changing the ratio of each component constituting the liquid composition. These were then evaluated in the same manner as above, and similarly good results were obtained.
[0170] In addition, two-chamber container-type topical skin preparations were produced in the same manner as above, except that the value of Wi / Wo, where Wi [g] is the mass of the powder composition and Wo [g] is the mass of the liquid composition, was changed within the range of 0.001 or more and 0.10 or less, and these were evaluated in the same manner as above, and similarly good results were obtained. [Explanation of symbols]
[0171] 10:2-chamber container 11: First container 11a: Room 1 12: Second container 12a: 2nd room 16: Valve member 17: Gap 21: Opening and closing section 22: Top wall 23: Spray base 24: Straw 25:Operation head 26: Nozzle L: Liquid composition P: Powder composition d: Size of the gap
Claims
1. A two-chamber container having a first container and a second container whose interiors are capable of communicating with each other, a powder composition filled in the first container, and a liquid composition filled in the second container, a dual-chamber container-type external skin preparation, the powder composition and the liquid composition being mixed by communicating an inside of the first container with an inside of the second container during use; The powder composition contains cyclodextrin-encapsulated retinol and amino acids, The liquid composition is a two-chamber container-type external skin preparation characterized in that the viscosity of the liquid composition, measured at a rotation speed of 60 rpm using a B-type viscometer in an environment of 25° C., is 20 mPa·s or more and 1000 mPa·s or less.
2. 2. The two-chamber container type external skin preparation according to claim 1, wherein the content of the cyclodextrin-encapsulated retinol in the powder composition is 20.0% by mass or more and 80.0% by mass or less.
3. 3. The two-chamber container type external skin preparation according to claim 1, wherein the amino acid is betaine.
4. 3. A two-chamber container type topical skin preparation according to claim 1 or 2, wherein when the mass of the powder composition is Wi [g] and the mass of the liquid composition is Wo [g], the relationship of 0.001≦Wi / Wo≦0.10 is satisfied.
5. 3. The two-chamber container type external skin preparation according to claim 1, wherein the liquid composition contains a fermented product obtained by fermenting rice bran and a peptide derived from beans with Bacillus subtilis.
Citation Information
Patent Citations
External composition for skin
JP2022101891A
Retinol-based compositions
JP2023507488A