External composition
The non-emulsified topical composition, formulated with specific ingredients such as hyaluronic acid, polyhydric alcohols, and hydrophobically modified alkyl cellulose, addresses the challenges of stretchability, sustained moisturizing, and viscosity stability against temperature and light exposure, achieving enhanced performance compared to existing formulations.
Patent Information
- Application Number
- JP2023150457
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2023-09-15
- Publication Date
- 2025-03-28
AI Technical Summary
Existing non-emulsified topical compositions struggle to simultaneously achieve stretchability, sustained moisturizing, prevention of stickiness, and stability against viscosity reduction due to high temperatures and light exposure, especially when formulated with limited ingredients for low irritation.
A non-emulsified topical composition formulation that includes hyaluronic acid and/or its salts, polyhydric alcohols at 15% by weight or more, oligosaccharides, a copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone, edetic acid and/or its salts, and hydrophobically modified alkyl cellulose or xanthan gum, which work together to enhance the composition's properties.
The composition achieves excellent stretchability, sustained moisturizing, and inhibition of stickiness while effectively suppressing viscosity reduction against high temperatures and light exposure, thereby addressing the challenges faced by existing formulations.
Smart Images

Figure 2025043129000001 
Figure 2025043129000002 
Figure 2025043129000003
Abstract
Description
[Technical field]
[0001] The present invention relates to a non-emulsified composition for external use that is excellent in usability and viscosity stability. [Background technology]
[0002] The product design of a topical composition is based on balancing the properties it provides to the living body, such as efficacy and functionality, with the properties of the preparation itself, such as quality stability. For example, Patent Document 1 discloses a gel-type cosmetic preparation that contains a carboxyl group-containing anionic polymer and at least one of the compounds hydroxypropylmethylcellulose and xanthan gum, as a gel-type cosmetic preparation that spreads easily, has an excellent feel when used, and exhibits reduced changes in viscosity over time. [Prior art documents] [Patent documents]
[0003] [Patent Document 1] JP 2019-127460 A Summary of the Invention [Problem to be solved by the invention]
[0004] The properties required for a topical composition vary greatly depending on the application site and the expected storage environment. For example, when the application site of the topical composition is expected to be a characteristic site that is difficult to see, has a complex shape, has thin skin, has hair, comes into contact with clothing, and is subjected to friction from clothing, the formulation properties require good spreadability as well as viscosity provided by the thickener, and the usage properties require sustained moisturizing sensation and suppression of stickiness. Furthermore, when the storage environment of the topical composition containing such a thickener is expected to be frequently exposed to both high temperature conditions and light such as artificial lighting or sunlight, it is also required that the viscosity decrease due to high temperature and light is suppressed. However, in many cases, the formulation that emphasizes the usability is aimed at low irritation, and considering the fact that the ingredients used are limited, it is extremely difficult to achieve many such properties in a topical composition. This difficulty is particularly noticeable in non-emulsion formulations.
[0005] Therefore, the present invention aims to provide a formulation for a non-emulsified topical composition containing a thickener that has good spreadability, sustained moisturizing feeling, and suppression of stickiness, as well as suppression of viscosity reduction due to high temperatures and light. [Means for solving the problem]
[0006] The present inventors have studied a formulation in which a moisturizing component is added to a non-emulsified topical composition containing a thickener. A formulation containing hyaluronic acid and / or its salt, 15% by weight or more of polyhydric alcohol, and oligosaccharides has excellent spreadability and long-lasting moisturizing feeling, but on the other hand, it has poor stickiness suppression and viscosity reduction suppression against sunlight and high temperature. Furthermore, when a copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone is used as a thickener, the stickiness suppression is good and the viscosity reduction suppression against high temperature is also slightly improved, but on the other hand, the viscosity reduction suppression against light is still poor and the viscosity reduction suppression against high temperature is not at a satisfactory level. Therefore, as a result of further study, it has been found that the viscosity reduction suppression against light is improved by adding edetic acid and / or its salt, and the viscosity reduction suppression against high temperature is improved by adding hydrophobically modified alkyl cellulose or xanthan gum. The present invention has been completed based on these findings and through further study.
[0007] That is, the present disclosure provides the inventions of the following aspects. Item 1. A non-emulsified composition for external use comprising: (A) hyaluronic acid and / or a salt thereof; (B) 15% by weight or more of a polyhydric alcohol; (C) an oligosaccharide; (D) a copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone; (E) edetic acid and / or a salt thereof; and (F) a hydrophobically modified alkylcellulose and / or xanthan gum. Item 2. The non-emulsified composition for external use according to Item 1, wherein the component (D) is contained in an amount of 1 part by weight or more per 100 parts by weight of the component (B). Item 3. The non-emulsified composition for external use according to Item 1 or 2, wherein the component (F) is contained in an amount of 0.1 part by weight or more per 100 parts by weight of the component (B). Item 4. The non-emulsified composition for external use according to any one of Items 1 to 3, wherein the component (C) is an α-glucan oligosaccharide. Item 5. The non-emulsified composition for external use according to any one of Items 1 to 4, wherein the component (F) is xanthan gum. Item 6. The non-emulsified composition for external use according to any one of Items 1 to 5, wherein the component (E) is contained in an amount of 0.02 to 0.1% by weight. Item 7. The non-emulsified composition for external use according to any one of Items 1 to 6, wherein the component (F) is contained in an amount of 0.05 to 1 part by weight per 1 part by weight of the component (D). Item 8. The non-emulsified composition for external use according to any one of Items 1 to 7, which has a viscosity at 25°C of 3 to 12 Pa s. Effect of the Invention
[0008] According to the present invention, a formulation is provided in a non-emulsified topical composition containing a thickener, which has good spreadability, sustained moisturizing feeling, and suppression of stickiness, as well as suppression of viscosity reduction due to high temperatures and light. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0009] The topical composition of the present disclosure is characterized in that it contains (A) hyaluronic acid and / or a salt thereof (hereinafter also referred to as "(A) component"); (B) 15% by weight or more of a polyhydric alcohol (hereinafter also referred to as "(B) component"); (C) an oligosaccharide (hereinafter also referred to as "(C) component"); (D) a copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone (hereinafter also referred to as "(D) component"); (E) edetic acid and / or a salt thereof (hereinafter also referred to as "(E) component"); and (F) a hydrophobically modified alkyl cellulose and / or xanthan gum (hereinafter also referred to as "(F) component"). In this specification, the numerical range indicated by two numerical values and "-" includes the two numerical values as the lower limit and the upper limit. For example, the expression "2-15% by weight" means 2% by weight or more and 15% by weight or less.
[0010] (A) Hyaluronic acid and / or its salt The topical composition of the present disclosure contains hyaluronic acid and / or a salt thereof as component (A).
[0011] Hyaluronic acid is a polysaccharide in which the disaccharide unit of D-glucuronic acid and N-acetyl-D-glucosamine are linked.The salt of hyaluronic acid is not particularly limited as long as it is pharmacologic acceptable in external preparation, and examples thereof include alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt; zinc salt, magnesium salt, ammonium salt, etc.These salts may be used alone or in combination of two or more.
[0012] In the topical composition of the present disclosure, the content of component (A) is not particularly limited, but may be, for example, 0.01 to 0.2 wt %, and from the viewpoint of enhancing the effect of improving the sustained moisturizing feeling, the content is preferably 0.05 to 0.2 wt %, more preferably 0.08 to 0.2 wt %, and from the viewpoint of enhancing the effect of suppressing stickiness, the content is preferably 0.01 to 0.15 wt %, more preferably 0.01 to 0.12 wt %.
[0013] (B) Polyhydric alcohol The topical composition of the present disclosure contains 15% by weight or more of polyhydric alcohol as component (B). When the content of polyhydric alcohol in a topical composition containing a thickener and hyaluronic acid and / or a salt thereof is 15% by weight, stickiness and viscosity loss at high temperatures may increase, but the topical composition of the present disclosure is excellent in suppressing stickiness and viscosity loss at high temperatures.
[0014] The polyhydric alcohol is not particularly limited as long as it is pharma- ceutical acceptable in external preparations, and examples thereof include dihydric alcohols such as propylene glycol, 1,3-butylene glycol, ethylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, etc.; trihydric alcohols such as glycerin, etc. These polyhydric alcohols may be used alone or in combination of two or more.
[0015] Among these polyhydric alcohols, a combination of a dihydric alcohol and a trihydric alcohol is preferable, and a combination of glycerin and 1,3-butylene glycol is more preferable.
[0016] In the topical composition of the present disclosure, the content (total amount) of the (B) component is 15% by weight or more, preferably 18% by weight or more, more preferably 20% by weight or more, and even more preferably 22% by weight or more. In the topical composition of the present disclosure, the content (total amount) of the (B) component is not particularly limited in its upper limit, but may be, for example, 30% by weight or less, preferably 28% by weight or less, more preferably 26% by weight or less, and even more preferably 24% by weight or less.
[0017] When a dihydric alcohol and a trihydric alcohol are used in combination as component (B), the ratio thereof is not particularly limited, but the ratio of trihydric alcohol to 1 part by weight of dihydric alcohol is, for example, 0.8 to 1.7 parts by weight, preferably 1 to 5 parts by weight, and more preferably 1.2 to 1.3 parts by weight.
[0018] When component (B) contains a dihydric alcohol, the specific content of the dihydric alcohol is, for example, 5 to 15% by weight, preferably 8 to 12% by weight.When component (B) contains a trihydric alcohol, the specific content of the trihydric alcohol is, for example, 5 to 15% by weight, preferably 9 to 14% by weight, more preferably 11 to 13% by weight.
[0019] (C) Oligosaccharides The topical composition of the present disclosure contains an oligosaccharide as component (C).
[0020] The oligosaccharide is not particularly limited as long as it is an oligomer having 2 to 20 sugar residues. Preferably, the oligosaccharide is an oligomer having 2 to 10 sugar residues. Examples of the constituent sugars of the oligosaccharide include galactose, glucose, mannose, fructose, etc. The oligosaccharide may be composed of one of these constituent sugars alone, or may be composed of a combination of two or more constituent sugars. Preferably, the oligosaccharide contains at least glucose among these constituent sugars, more preferably glucose and fructose. Examples of the bond type of the constituent sugar include α-glycosidic bond and β-glycosidic bond, and preferably α-glycosidic bond. More preferred examples of the oligosaccharide include condensates of maltose and sucrose, and particularly preferably α-glucan oligosaccharide.
[0021] In the topical composition of the present disclosure, the content of component (C) is not particularly limited, but may be, for example, 0.1 to 1.5 wt. %, and from the viewpoint of enhancing the effect of improving the sustained moisturizing feeling, preferably 0.5 to 1.5 wt. %, more preferably 0.8 to 1.5 wt. %, and from the viewpoint of enhancing the stickiness suppression effect, preferably 0.1 to 1.3 wt. %, more preferably 0.1 to 1.1 wt. %.
[0022] (D) Copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone The topical composition of the present disclosure contains a copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone (VP) as component (D). "(Meth)acrylic" means "acrylic", "methacrylic", or both. In the topical composition of the present disclosure, component (D) not only contributes to thickening, but also contributes to suppressing stickiness and partially contributes to suppressing viscosity reduction at high temperatures.
[0023] (Meth)acryloyldimethyltaurate, which is a structural unit of the copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone, is not particularly limited as long as it is pharma- ceutical acceptable in an external preparation. Examples of (meth)acryloyldimethyltaurate include alkali metal salts such as sodium salts and potassium salts; ammonium salts, and organic amine salts such as triethanolamine salts and monoethanolamine salts.
[0024] The component (D) may be a copolymer of one type of (meth)acryloyldimethyltaurate salt among the above structural units and vinylpyrrolidone, or may be a copolymer of two or more types of (meth)acryloyldimethyltaurate salts among the above structural units and vinylpyrrolidone.
[0025] As the component (D), these copolymers of (meth)acryloyldimethyltaurate and vinylpyrrolidone may be used alone or in combination of two or more.
[0026] As the (D) component, among these copolymers of (meth)acryloyldimethyltaurate and vinylpyrrolidone, a copolymer of an organic amine salt of (meth)acryloyldimethyltaurate and vinylpyrrolidone is preferable, and a copolymer of ammonium (meth)acryloyldimethyltaurate and vinylpyrrolidone is more preferable.
[0027] The sequence classification of (meth)acryloyldimethyltaurate and vinylpyrrolidone is not particularly limited, and may be any of random copolymerization, alternating copolymerization, block copolymerization, and graft copolymerization. Among these sequence classifications, preferred are random copolymerization and alternating copolymerization, and more preferred are random copolymerization.
[0028] In the topical composition of the present disclosure, the content of the (D) component is not particularly limited, but may be, for example, 1 part by weight or more per 100 parts by weight of the (B) component, and from the viewpoint of further enhancing the effect of suppressing stickiness and / or suppressing viscosity reduction at high temperatures, etc., preferably 1.3 parts by weight or more, more preferably 1.7 parts by weight or more, even more preferably 2 parts by weight or more, and even more preferably 2.2 parts by weight or more. The content of the (D) component per 100 parts by weight of the (B) component is not particularly limited in its upper limit, but may be, for example, 3.2 parts by weight or less, preferably 2.7 parts by weight or less, more preferably 2.5 parts by weight or less, and even more preferably 2.4 parts by weight or less.
[0029] In the topical composition of the present disclosure, the specific content of component (D) is not particularly limited, but can be, for example, 0.3% by weight or more, preferably 0.4% by weight or more, more preferably 0.45% by weight or more, even more preferably 0.48% by weight or more or 0.49% by weight or more. The specific content of component (D) is not particularly limited in its upper limit, but can be, for example, 0.7% by weight or less, preferably 0.7% by weight or less, more preferably 0.6% by weight or less, 0.55% by weight or less, or 0.53% by weight or less.
[0030] (E) edetic acid and / or its salts The topical composition of the present disclosure contains edetic acid and / or a salt thereof as component (E). In the topical composition of the present disclosure, component (E) contributes to suppression of viscosity reduction due to light.
[0031] Edetic acid is a compound also called ethylenediaminetetraacetic acid.In the topical composition of the present disclosure, the salt of edetic acid may be any pharmaceutically acceptable salt in topical preparations, and is not particularly limited, but may include, for example, alkali metal salts such as monosodium salt, disodium salt, trisodium salt, tetrasodium salt, dipotassium salt, tripotassium salt, and tetrapotassium salt.One of these salts may be used alone, or two or more may be used in combination.Among these edetic acids and their salts, preferred is edetate, and more preferred is disodium edetate.
[0032] In the topical composition of the present disclosure, the content of component (E) is not particularly limited, but may be, for example, 0.02 to 0.1% by weight, and from the viewpoint of further enhancing the effect of inhibiting viscosity reduction due to light, preferably, the content is 0.04 to 0.1% by weight, 0.04 to 0.8% by weight, or 0.04 to 0.6% by weight.
[0033] In the topical composition of the present disclosure, the content of component (E) is, for example, 5 to 20 parts by weight, preferably 7 to 17 parts by weight, and more preferably 9 to 15 parts by weight, relative to 100 parts by weight of the total amount of components (A), (B), (C), and (D).
[0034] (F) Hydrophobically modified alkyl cellulose and / or xanthan gum The topical composition of the present disclosure contains hydrophobically modified alkyl cellulose and / or xanthan gum as component (F). In the topical composition of the present disclosure, component (F) contributes to suppression of viscosity reduction at high temperatures.
[0035] The hydrophobically modified alkyl cellulose is a cellulose ether modified with an alkyl group to impart hydrophobicity, and is a compound known as a thickener. The hydrophobically modified alkyl cellulose is preferably a compound represented by the following formula (I):
[0036] [ka]
[0037] In formula (I), R 1 , R 2 and R 3 are the same or different, a hydrogen atom, a lower alkyl group having 1 to 6 carbon atoms, -[CHCH 2-s (CH3) s O] m a first group represented by H, or -CH2CH(OH)CH2OC t H 2t+1where n is an integer of 100 to 10,000, s is an integer of 0 or 1, m is an integer of 1 to 10, and t is an integer of 6 to 26, and the molecule contains at least the second group.
[0038] The hydrophobically modified alkyl cellulose preferably has a lower alkyl group content of, for example, 10 to 40% by weight, preferably 20 to 30% by weight in formula (I); a first group content of, for example, 3 to 20% by weight, preferably 6 to 12% by weight; and a second group content of, for example, 0.1 to 5% by weight, preferably 0.3 to 4% by weight. The contents of the lower alkyl group, the first group, and the second group contained in the hydrophobically modified alkyl cellulose are values measured in accordance with the section on "hydroxypropyl methylcellulose 2208" in the 13th edition of the Japanese Pharmacopoeia.
[0039] As the hydrophobically modified alkyl cellulose, one of these may be used alone, or two or more of them may be used in combination.
[0040] The hydrophobically modified alkyl cellulose preferably has an alkyl group (which constitutes the second group in formula (I), -C t H 2t+1 The hydroxypropyl methylcellulose is a hydroxypropyl methylcellulose modified by an alkyl group in the above formula (I). 1 , R 2 and R 3 are the same or different and are a hydrogen atom, a methyl group, or a first group (where s=1), and the compound contains at least the first group (where s=1) in the molecule.
[0041] A preferred example of the hydrophobically modified alkyl cellulose is a -C t H 2t+1In the alkyl group represented by the formula: wherein t is preferably 8 to 26, more preferably 12 to 24, further preferably 16 to 20, and particularly preferably 18. A particularly suitable example of the hydrophobically modified alkyl cellulose is stearyl group-modified hydroxypropyl methyl cellulose (stearoxy hydroxypropyl methyl cellulose).
[0042] Suitable examples of hydrophobically modified alkyl cellulose include those having an alkoxy group (preferably a methoxyl group) content represented by -O-[the above-mentioned lower alkyl group having 1 to 6 carbon atoms] of 20 to 30% by weight, preferably 27 to 30% by weight, a group (preferably a hydroxypropoxyl group) content represented by -O-[the above-mentioned first group] of 5 to 15% by weight, preferably 7 to 11% by weight, and an alkyloxyhydroxyalkoxy group (preferably a stearyloxyhydroxypropoxyl group) content represented by -O-[the above-mentioned second group] of 0.3 to 4% by weight, preferably 0.3 to 2% by weight, more preferably 0.3 to 0.6% by weight.
[0043] Xanthan gum is a polysaccharide produced by Xanthomonas campestris and is a component known as a thickening agent.
[0044] In the topical composition of the present disclosure, both hydrophobically modified alkyl cellulose and xanthan gum have excellent effects in inhibiting viscosity reduction at high temperatures, but from the viewpoint of further enhancing the spreadability in addition to the viscosity reduction inhibition effect, xanthan gum is preferred.
[0045] In the topical composition of the present disclosure, the content of component (F) is not particularly limited, but may be, for example, 0.1 part by weight or more per 100 parts by weight of component (B). From the viewpoint of further enhancing the effect of inhibiting viscosity reduction at high temperatures, the amount is preferably 0.2 parts by weight or more, 0.3 parts by weight or more, 0.4 parts by weight or more, or 0.5 parts by weight or more, more preferably 0.6 parts by weight or more, 0.7 parts by weight or more, and even more preferably 0.8 parts by weight or more or 0.85 parts by weight or more.
[0046] The content of the (F) component per 100 parts by weight of the (B) component is not particularly limited in its upper limit, and may be, for example, 3 parts by weight or less, 2 parts by weight or less, 1.6 parts by weight or less, or 1.4 parts by weight or less. Since the topical composition of the present disclosure has excellent viscosity reduction suppression effect at high temperatures, even if the content of the (F) component is even smaller, the viscosity reduction suppression effect at high temperatures can be effectively obtained. From this viewpoint, the content of the (F) component per 100 parts by weight of the (B) component may be 1.2 parts by weight or less or 1 part by weight or less. In addition, when using a hydrophobized modified alkyl cellulose as the (F) component, from the viewpoint of enhancing stickiness suppression, the content of the hydrophobized modified alkyl cellulose per 100 parts by weight of the (B) component is preferably 0.9 parts by weight or less, 0.7 parts by weight or less, more preferably 0.5 parts by weight or less or 0.45 parts by weight or less, and even more preferably 0.3 parts by weight or less or 0.25 parts by weight or less.
[0047] In the topical composition of the present disclosure, the specific content of component (F) is not particularly limited, but may be, for example, 0.023% by weight or more. From the viewpoint of further enhancing the effect of inhibiting viscosity reduction at high temperatures, the content is preferably 0.045% by weight or more, 0.07% by weight or more, 0.09% by weight or more, or 0.1% by weight or more, more preferably 0.14% by weight or more, 0.16% by weight or more, and even more preferably 0.18% by weight or more or 0.19% by weight or more.
[0048] The specific content of the (F) component is not particularly limited in its upper limit, and may be, for example, 0.6% by weight or less, 0.45% by weight or less, 0.35% by weight or less, or 0.32% by weight or less. Since the topical composition of the present disclosure has excellent viscosity reduction suppression effect at high temperatures, even if the content of the (F) component is even smaller, the viscosity reduction suppression effect at high temperatures can be effectively obtained. From this viewpoint, the content of the (F) component may be 0.25% by weight or less or 0.23% by weight or less. In addition, when using a hydrophobized modified alkyl cellulose as the (F) component, from the viewpoint of enhancing stickiness suppression, the content of the hydrophobized modified alkyl cellulose is preferably 0.2% by weight or less, 0.15% by weight or less, more preferably 0.12% by weight or less or 0.1% by weight or less, and even more preferably 0.07% by weight or less or 0.06% by weight or less.
[0049] In the topical composition of the present disclosure, the content of component (F) per 1 part by weight of component (D) is, for example, 0.05 to 1 part by weight, preferably 0.1 to 0.9 parts by weight, 0.15 to 0.8 parts by weight, 0.2 to 0.75 parts by weight, or 0.25 to 0.7 parts by weight, more preferably 0.28 to 0.65 parts by weight, and even more preferably 0.38 to 0.62 parts by weight, 0.38 to 0.55 parts by weight, or 0.38 to 0.5 parts by weight.
[0050] In the topical composition of the present disclosure, the content of component (F) is, for example, an amount such that the total amount of components (D) and (F) is 0.4 to 1.5 wt %, preferably 0.5 to 1.2 wt %, more preferably 0.54 to 1 wt %, even more preferably 0.64 to 0.9 wt %, and even more preferably 0.68 to 0.85 wt %, 0.68 to 0.8 wt %, or 0.68 to 0.75 wt %.
[0051] Other Ingredients In addition to the above-mentioned components (A) to (F), the topical composition of the present disclosure may or may not further contain additives and / or bases, as long as they do not impair the present invention. The additives and bases, which may or may not be contained, are not particularly limited as long as they are pharma- ceutically acceptable, and include water, other thickeners (other than components (D) and (F)), pH adjusters, preservatives, surfactants, isotonicity agents, dispersants, moisturizers, etc. These additives and / or bases may be used alone or in combination of two or more. The content of these additives and bases is appropriately set according to the types of additives and bases used, the formulation form of the topical composition of the present invention, etc.
[0052] The topical composition of the present disclosure typically contains water. The content of water in the topical composition of the present disclosure is, for example, 65 to 84% by weight, preferably 68 to 82% by weight, and more preferably 70 to 80% by weight.
[0053] Examples of other thickening agents include dextrin, carboxyvinyl polymer, hydroxypropylmethylcellulose, and hydroxyethylcellulose. These other thickening agents may be used alone or in combination of two or more. In a preferred embodiment of the topical composition of the present disclosure, among these other thickening agents, hydroxyethylcellulose is included. Examples of hydroxycellulose include those having a viscosity in a 1% by weight aqueous solution (25°C) of, for example, 2000 to 6000 mPa·s, preferably 2200 to 4000 mPa·s, and more preferably 2400 to 3000 mPa·s. When the topical composition of the present disclosure includes hydroxyethylcellulose, the content thereof is, for example, 0.03 to 0.2% by weight, preferably 0.05 to 0.15% by weight, and more preferably 0.08 to 0.12% by weight. In a preferred embodiment of the topical composition of the present disclosure, among these other thickening agents, dextrin, carboxyvinyl polymer, and / or hydroxypropylmethylcellulose are not included.
[0054] Examples of pH adjusters include inorganic acids (e.g., hydrochloric acid, sulfuric acid, phosphoric acid, etc.), organic acids (e.g., lactic acid, acetic acid, citric acid, malic acid, gluconic acid, adipic acid, tartaric acid, etc.) or salts thereof. These pH adjusters may be used alone or in combination of two or more. In a preferred embodiment of the topical composition of the present disclosure, among these pH adjusters, preferably an organic acid is included, more preferably lactic acid.
[0055] Examples of preservatives include methylparaben, ethylparaben, butylparaben, and phenoxyethanol. These preservatives may be used alone or in combination of two or more. In a preferred embodiment of the topical composition of the present disclosure, among these preservatives, phenoxyethanol is preferably contained. When the topical composition of the present disclosure contains phenoxyethanol, the content thereof is, for example, 0.1 to 0.9% by weight, preferably 0.2 to 0.7% by weight, and more preferably 0.3 to 0.5% by weight.
[0056] In addition to the above-mentioned components (A) to (F), the topical composition of the present disclosure may or may not contain a medicinal ingredient, as long as it does not impair the present invention. Examples of the medicinal ingredient that may or may not be contained include antihistamines, local anesthetics, anti-inflammatory agents, bactericides, antipruritic agents, blood circulation promoting ingredients, vitamins, etc. These medicinal ingredients may be used alone or in combination of two or more. In addition, when these medicinal ingredients are contained in the topical composition of the present invention, the content thereof is appropriately set depending on the type of medicinal ingredient used, the expected effect, etc.
[0057] Formulation The formulation form of the topical composition of the present disclosure is not particularly limited, as long as it is a non-emulsion form and can be used externally. Examples of the formulation form of the topical composition of the present disclosure include, for example, liquids, gels, etc. In addition, the topical composition of the present disclosure may be in a suspension form or a non-suspension form. Since the topical composition of the present disclosure has excellent viscosity reduction suppression properties against light, it can effectively obtain the effect of suppressing viscosity reduction against light even if it is transparent. From this viewpoint, the topical composition of the present disclosure is preferably in a non-suspension form.
[0058] viscosity The viscosity of the topical composition of the present disclosure is not particularly limited, and the viscosity at 25°C (measured with a Brookfield viscometer (rotor: M4, rotation speed: 30 rpm, 30 seconds after the start of rotation)) is, for example, 3 to 12 Pa·s. From the viewpoint of obtaining good application properties to areas with complex shapes or areas where body hair is present, the viscosity is preferably 3.5 to 12 Pa·s, more preferably 4 to 12 Pa·s, even more preferably 4.5 to 12 Pa·s, and even more preferably 4.7 to 11 Pa·s, 4.7 to 10 Pa·s, 4.7 to 9 Pa·s, 4.7 to 8 Pa·s, 4.7 to 7 Pa·s, or 4.7 to 6.2 Pa·s.
[0059] pH The pH of the topical composition of the present disclosure is not particularly limited, and may be, for example, a pH of 4.5 to 6.5 at 25° C., preferably 4.7 to 6, more preferably 4.8 to 5.5, and even more preferably 4.9 to 5.2.
[0060] Purpose The topical composition of the present disclosure is used for any external use. The topical composition of the present disclosure has good spreadability, long-lasting moisturizing feeling, and stickiness suppression properties, and is therefore preferably used for application to areas of the body that are difficult to see, have complex shapes, have thin skin, are hairy, come into contact with clothing, and / or are subject to friction from clothing. Such areas are preferably delicate zones (particularly, genital areas and / or anal area), more preferably female delicate zones (particularly, external genital areas and / or anal area). The topical composition of the present disclosure has viscosity reduction suppression properties against high temperatures and light, and is therefore preferably placed in a storage environment exposed to high temperatures (e.g., dressing rooms, bathrooms, etc.) and / or light (artificial lighting (e.g., direct lighting in dressing rooms, bathrooms, etc.) and / or sunlight). In addition, the topical composition of the present disclosure has viscosity reduction suppression properties against light, and is therefore preferably stored in a transparent container. EXAMPLES
[0061] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.
[0062] (1) Preparation of topical composition Non-emulsified compositions for external use were prepared having the compositions shown in Tables 1 and 2. Details of each component used in the preparation of each composition for external use are as follows. α-Glucan oligosaccharide: 2-10 sugar residues, condensation product of maltose and sucrose (Acrylate dimethyltaurate ammonium / VP (vinylpyrrolidone)) copolymer Stearoxyhydroxypropylmethylcellulose: 27-30% by weight of methoxyl groups, 7-11% by weight of hydroxypropoxyl groups, 0.3-0.6% by weight of stearyloxyhydroxypropoxyl groups Hydroxyethyl cellulose: Viscosity of 1% by weight aqueous solution (25°C) is 2400-3000 mPa·s
[0063] (2) Evaluation of usability The spreadability, sustained moisturizing sensation, and stickiness suppression were evaluated by expert panelists (N=10). Specifically, the topical compositions were applied to the forearm and evaluated based on the following criteria. The results are shown in Tables 1 and 2.
[0064] (2-1) Good stretchability Regarding the quality of growth, participants were asked to rate it on a five-point scale: satisfied, somewhat satisfied, neither satisfied nor dissatisfied, somewhat dissatisfied, and dissatisfied, and the evaluation was based on the number of people who answered "satisfied." ◎:9 or more people ○: 7~8 people △:5~6 people ×: 4 people or less
[0065] (2-2) Duration of moisturizing sensation The duration of moisturizing sensation was evaluated based on the number of people who responded that they felt moisturized 90 minutes after application. ○:6 or more people △:4~5 people ×: 3 or less people
[0066] (2-3) Anti-stickiness Stickiness was assessed on a three-point scale: felt, felt but not uncomfortable, felt and uncomfortable, and the evaluation was based on the number of people who answered that it was uncomfortable. ×: 3 or more people △:2 people ○: 1 person or less
[0067] (3) Evaluation of viscosity stability The ability to suppress viscosity decrease due to light and high temperature was evaluated by the following method. Viscosity (Pa s) was measured at 25°C using a B-type viscometer (rotor: M4, rotation speed: 30 rpm, 30 seconds after the start of rotation).
[0068] (3-1) Inhibition of viscosity decrease due to light The topical compositions were exposed to sunlight for two weeks. The ability to inhibit viscosity reduction due to light was evaluated based on the relative value (%) of the viscosity after two weeks, with the initial viscosity (viscosity immediately after preparation) taken as 100%. ○: Relative value 80% or more ×: Relative value less than 80%
[0069] (3-2) Viscosity reduction suppression at high temperatures The topical compositions were stored for one week at 50° C. The ability to inhibit viscosity decrease at high temperatures was evaluated based on the relative value (%) of the viscosity after one week, assuming the initial viscosity (viscosity immediately after preparation) to be 100%. +8: 94% or more +7: 91% to less than 94% +6: 88% to less than 91% +5: 85% or more but less than 88% +4: 82% or more but less than 85% +3: 79% or more but less than 82% +2: 76% or more but less than 79% +1: 73% to less than 76% 0: Between 70% and 73% -1: Between 67% and 70% -2: Between 64% and 67% -3: 61% to less than 64% -4: Less than 61%
[0070] [Table 1]
[0071] [Table 2]
[0072] As shown in Table 1, the non-emulsified topical composition containing the moisturizing ingredients (A) and (B) and a thickener (Comparative Example 1) had poor moisturizing sensation durability and poor viscosity reduction inhibition. The non-emulsified topical composition (Comparative Example 2) in which the moisturizing ingredients (B) were increased and another moisturizing ingredient (C) was also added improved moisturizing sensation durability, but on the other hand, stickiness increased and, in particular, viscosity reduction inhibition against high temperatures was significantly deteriorated (in light of the comparison with Comparative Examples 3 and 4 described below, it is believed that the (B) ingredient contributed to the increase in stickiness and the deterioration of viscosity reduction inhibition against high temperatures). In addition, Comparative Example 2 still had poor viscosity reduction inhibition against light.
[0073] In the non-emulsified topical composition (Comparative Example 4) in which the thickener was changed to component (D), as is clear from a comparison with Comparative Example 2, the stickiness suppression property improved, and the viscosity reduction suppression property against high temperatures was slightly improved (this tendency is also observed in Example 1 compared to Example 5, and Example 2 compared to Example 6, which will be described later). However, in Comparative Example 4, the improvement effect of the viscosity reduction suppression property against high temperatures was insufficient, and the viscosity reduction suppression property against light was still poor.
[0074] Furthermore, in the non-emulsified topical composition containing the component (E) (Comparative Example 5), the viscosity reduction suppression property against light was improved. However, in Comparative Example 5, the improvement effect of the viscosity reduction suppression property against high temperatures remained insufficient.
[0075] Therefore, when other thickeners were further added (Comparative Examples 6 to 8, Example 1), the non-emulsified general composition containing the (F) component (Example 1) was able to improve its ability to suppress viscosity reduction at high temperatures without compromising the feel in use (good spreadability, sustained moisturizing sensation, and suppression of stickiness).
[0076] As shown in Table 2, all of the non-emulsified general compositions (Examples 1 to 9) containing all of the components (A) to (F) were able to simultaneously achieve both usability (good spreadability, sustained moisturizing sensation, and suppression of stickiness) and viscosity stability (suppression of viscosity decrease due to light and suppression of viscosity decrease due to high temperatures).While the use of either hydrophobically modified alkyl cellulose (stearoxy hydroxypropyl methylcellulose) or xanthan gum as the component (F) improved the suppression of viscosity decrease due to high temperatures, the effect of achieving both excellent levels of viscosity decrease suppression effect due to high temperatures and good spreadability was superior in the cases where xanthan gum was used (Examples 7 to 9).
[0077] As described above, the non-emulsified general compositions (Examples 1 to 9) containing all of the components (A) to (F) have a feeling of use (good spreadability, long-lasting moisturizing feeling, and anti-stickiness), and are therefore suitable as external compositions to be applied to delicate zones, particularly female delicate zones, which are difficult to see, have complex shapes, have thin skin, may have pubic hair, come into contact with clothing, and are subject to friction from clothing. External compositions for delicate zones are often used (or used and stored) in changing rooms and / or bathrooms, where these locations are frequently exposed to high temperatures and direct lighting. The non-emulsified general compositions (Examples 1 to 9) containing all of the components (A) to (F) have the ability to inhibit viscosity reduction due to light and high temperatures, and are therefore suitable as external compositions for delicate zones, taking into consideration the use (or use and storage) environment of external compositions for delicate zones.
Claims
1. A non-emulsified topical composition comprising: (A) hyaluronic acid and / or a salt thereof; (B) 15% by weight or more of a polyhydric alcohol; (C) an oligosaccharide; (D) a copolymer of (meth)acryloyldimethyltaurate and vinylpyrrolidone; (E) edetic acid and / or a salt thereof; and (F) a hydrophobically modified alkylcellulose and / or xanthan gum.
2. The non-emulsified topical composition according to claim 1 , wherein the (D) component is contained in an amount of 1 part by weight or more per 100 parts by weight of the (B) component.
3. The non-emulsified topical composition according to claim 1, wherein the (F) component is contained in an amount of 0.1 part by weight or more per 100 parts by weight of the (B) component.
4. 2. The non-emulsified composition for external use according to claim 1, wherein the component (C) is an α-glucan oligosaccharide.
5. The non-emulsified topical composition according to claim 1, wherein the component (F) is xanthan gum.
6. The non-emulsified topical composition according to claim 1, wherein the component (E) is contained in an amount of 0.02 to 0.1% by weight.
7. The non-emulsified topical composition according to claim 1, wherein the (F) component is contained in an amount of 0.05 to 1 part by weight per 1 part by weight of the (D) component.
8. 2. The non-emulsified composition for external use according to claim 1, having a viscosity of 3 to 12 Pa·s at 25°C.
Citation Information
Patent Citations
Gelatinous cosmetic
JP2019127460A