Topical composition
By adding diazepam and nonionic surfactant of HLB 5.0 or lower to the top agent with high content of petrolatum, the quality and safety problems caused by the release of petrolatum over time were solved, and an effective inhibitory effect was achieved.
Patent Information
- Application Number
- JP2023185100
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2023-10-27
- Publication Date
- 2025-05-13
AI Technical Summary
High content of petrolatum in the top agent over time can lead to a loss of quality and safety, especially when containing 50% or higher petrolatum, the prior art is difficult to effectively inhibit its release.
The separation of petrolatum is further inhibited by adding diphenhydramine and HLB 5.0 or lower nonionic surfactant to the top agent.
It effectively inhibits the release of petrolatum and maintains the quality and safety of the top agent, especially in the case of high content of petrolatum.
Smart Images
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Abstract
Description
[Technical field]
[0001] The present invention relates to a composition for external use which contains 50% by weight or more of petrolatum and has excellent syneresis-inhibiting properties. [Background technology]
[0002] Among the oily bases used in topical preparations, petrolatum is particularly versatile due to its low irritation, excellent protective effect due to its covering effect on the skin, and excellent skin permeability of drugs. In order to fully exert the covering effect of petrolatum, it is effective to increase the amount of petrolatum in the topical composition. On the other hand, it is also known that petrolatum undergoes syneresis over time. If syneresis occurs in a topical preparation containing petrolatum, it can cause a loss of confidence in the quality of the topical preparation.
[0003] As a method for suppressing syneresis of topical preparations containing petrolatum, Patent Document 1 discloses a technique in which a paste-like oil composition in which liquid oil is gelled with a cross-linked alkyl polyether modified silicone is mixed with semi-solid oils and fats such as petrolatum, and Patent Document 2 discloses a technique in which a rubber elastomer is mixed with an oil or fat such as petrolatum by heating to melt or swell. [Prior art documents] [Patent documents]
[0004] [Patent Document 1] JP 2005-015407 A [Patent Document 2] JP 2006-335734 A Summary of the Invention [Problem to be solved by the invention]
[0005] The loss of confidence in the quality of topical agents caused by the syneresis of petrolatum over time is particularly noticeable in formulations containing 50% or more petrolatum by weight.
[0006] The technology of Patent Document 1 requires the incorporation of a large amount of a paste-like oil composition to suppress syneresis, and cannot be applied to a formulation that incorporates petrolatum at a high concentration of 50% by weight or more. Also, the technology of Patent Document 2 requires a process such as heat melting or swelling mixing to incorporate the rubber elastomer, making the production complicated.
[0007] Therefore, an object of the present invention is to provide a new formulation that can suppress syneresis of petrolatum over time in a topical composition containing 50% by weight or more of petrolatum. [Means for solving the problem]
[0008] The present inventors have conducted extensive research to solve the above problems, and have unexpectedly found that by incorporating diphenhydramine into a topical composition containing 50% by weight or more of petrolatum, the separation of petrolatum over time can be suppressed. Even more unexpectedly, the inventors have found that by incorporating a combination of diphenhydramine and a nonionic surfactant with an HLB of 5.0 or less into a topical composition containing 50% by weight or more of petrolatum, the separation of petrolatum over time can be further suppressed. The present invention was completed through further research based on these findings.
[0009] That is, the present disclosure provides the inventions of the following aspects. Item 1. A composition for external use comprising (A) 50% by weight or more of petrolatum and (B) diphenhydramine. Item 2. The composition for external use according to Item 1, further comprising (C) a nonionic surfactant having an HLB of 5.0 or less. Item 3. The composition for external use according to Item 1 or 2, wherein the content of the component (B) per 100 parts by weight of the component (A) is 0.1 parts by weight or more. Item 4. The composition for external use according to any one of Items 1 to 3, wherein the content of the component (C) per 100 parts by weight of the component (A) is 0.2 parts by weight or more. Item 5. The composition for external use according to any one of Items 1 to 4, wherein the content of the liquid oil per 100 parts by weight of the component (A) is 10 parts by weight or less. Item 6. The composition for external use according to any one of Items 1 to 5, which is a water-in-oil emulsion composition. Item 7. The composition for external use according to any one of Items 1 to 6, which is a non-steroidal preparation. Effect of the Invention
[0010] According to the present disclosure, in a composition for external use containing 50% by weight or more of petrolatum, syneresis of the petrolatum over time can be suppressed. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0011] The topical composition of the present disclosure is characterized by containing (A) 50% by weight or more of petrolatum (hereinafter also referred to as "component (A)") and (B) diphenhydramine (hereinafter also referred to as "component (B)"). The topical composition of the present disclosure will be described in detail below. In this specification, a numerical range indicated by two numbers and "to" includes the two numbers as the lower limit and the upper limit. For example, the expression "2 to 15% by weight" means 2% by weight or more and 15% by weight or less.
[0012] (A) Vaseline The topical composition of the present disclosure contains petrolatum as component (A). Petrolatum is a semi-solid substance obtained by refining a mixture of hydrocarbons, and any substance that can be incorporated into cosmetics, topical quasi-drugs, or topical medicines can be used without any particular restrictions. As for the type of petrolatum, either yellow petrolatum or white petrolatum may be used, but white petrolatum is preferably used.
[0013] White petrolatum can be any one that complies with the Japanese Pharmacopoeia. White petrolatum that can be used in the composition for external use of the present disclosure can be any commercially available product, such as Sunwhite P-150, Sunwhite P-200, Sunwhite S-200 (all manufactured by Nikko Rica Co., Ltd.), Nomcoat W (manufactured by Nisshin Oillio Co., Ltd.), CROLATUM V (manufactured by Croda Japan Co., Ltd.), Peren Snow, Snow V, Ultima White, Vaseline Base No. 4 (all manufactured by Penreco Co., Ltd.), PROTOPET Super White, SONNECONE DM1, SONNECONE CM, MINERAL GELLY#10, MINERAL GELLY#14, MINERAL GELLY#17, SONOJELL#4, SONOJELL#9 (all manufactured by Sonneborn Co., Ltd.) and the like.
[0014] The content of component (A) in the topical composition of the present disclosure is 50% by weight or more. In a topical composition containing 50% by weight or more of petrolatum, the sense of security in the quality of the topical agent caused by the syneresis of petrolatum over time is significantly impaired, but the topical composition of the present disclosure is excellent in suppressing the syneresis of petrolatum over time.
[0015] Since the topical composition of the present disclosure has excellent suppression of syneresis over time of petrolatum, even if it contains a larger amount of component (A), it can effectively suppress syneresis over time. From this viewpoint, suitable examples of the content of component (A) in the topical composition of the present disclosure include preferably 53% by weight or more, more preferably 56% by weight or more, even more preferably 59% by weight or more, and even more preferably 62% by weight or more, 65% by weight or more, 68% by weight or more, or 71% by weight or more.
[0016] The upper limit of the content of component (A) in the topical composition of the present disclosure is not particularly limited, but may be, for example, 99% by weight or less, preferably 95% by weight or less, more preferably 90% by weight or less, even more preferably 85% by weight or less, even more preferably 80% by weight or less, and particularly preferably 75% by weight or less, 70% by weight or less, or 65% by weight or less.
[0017] The content of component (A) in the topical composition of the present disclosure is, for example, 65 to 90 parts by weight, preferably 70 to 85 parts by weight, 72 to 80 parts by weight, or 74 to 78 parts by weight, relative to 100 parts by weight of the total amount of the oily base (the total of component (A), solid oil described below, other semi-solid oil described below, and liquid oil described below). The total amount of the oily base in the topical composition of the present disclosure is, for example, 60 to 95% by weight, preferably 70 to 90% by weight, and more preferably 75 to 85% by weight.
[0018] (B) Diphenhydramine The topical composition of the present disclosure contains diphenhydramine as component (B). In a topical composition containing 50% by weight or more of component (A), the petrolatum undergoes syneresis over time, but by adding component (B) to the topical composition, the syneresis of the petrolatum over time can be suppressed.
[0019] Diphenhydramine is a lipid-soluble compound and is a known drug known to have antihistamine effects.
[0020] The content of the (B) component in the topical composition of the present disclosure is not particularly limited, and may be appropriately set according to the degree of the effect of suppressing the syneresis of petrolatum over time to be imparted, but the content of the (B) component relative to 100 parts by weight of the (A) component is, for example, 0.1 parts by weight or more, and from the viewpoint of enhancing the effect of suppressing the syneresis of petrolatum over time, preferably 0.25 parts by weight or more, more preferably 0.5 parts by weight or more, even more preferably 1 part by weight or more, even more preferably 1.2 parts by weight or more, and even more preferably 1.5 parts by weight or more. The content of the (B) component relative to 100 parts by weight of the (A) component is not particularly limited in its upper limit, but may be, for example, 5 parts by weight or less, preferably 3 parts by weight or less, more preferably 2.5 parts by weight or less, and even more preferably 2 parts by weight or less or 1.7 parts by weight or less.
[0021] The specific content of the (B) component in the topical composition of the present disclosure is determined according to the content of the (A) component and the content ratio of the (B) component, and may be, for example, 0.1% by weight or more. From the viewpoint of enhancing the effect of suppressing the syneresis of Vaseline over time, it is preferably 0.2% by weight or more, more preferably 0.3% by weight or more, even more preferably 0.5% by weight or more, even more preferably 0.7% by weight or more, and even more preferably 0.9% by weight or more. The specific content of the (B) component in the topical composition of the present disclosure is not particularly limited in its upper limit, and may be, for example, 5% by weight or less, preferably 3% by weight or less, more preferably 2.5% by weight or less, even more preferably 2% by weight or less, even more preferably 1.7% by weight or less, 1.5% by weight or less, or 1.3% by weight or less.
[0022] (C) a specific nonionic surfactant The topical composition of the present disclosure may further comprise a nonionic surfactant having an HLB of 5.0 or less as component (C). By further adding component (C) to a topical composition containing 50% by weight or more of components (A) and (B), the syneresis of petrolatum over time can be further suppressed.
[0023] The HLB (Hydrophile-Lipophile Balance) value generally indicates the affinity of a nonionic surfactant to water and oil, and is determined by a measurement method based on the actual measurement of HLB value by emulsification method described in "Handbook - Cosmetics and Pharmaceutical Raw Materials - Revised Edition", Nikko Chemicals Co., Ltd., revised edition published on February 1, 1977, pages 854-855. Specifically, component (C) is combined with polyoxyethylene sorbitan monostearate (NIKKOL TS-10, HLB 14.9) as a standard substance of emulsifier, and the total amount of these two emulsifiers is kept constant, and only the ratio is changed to emulsify liquid paraffin (HLB 10.1) to be emulsified, and after leaving it overnight, the optimal ratio of emulsifiers is determined for stability from the amount of creaming, white turbidity, and water separation from the lower layer, and the HLB value x of component (C) is calculated by the following formula (1). y=(x×Amount used (mass%)+z×Amount used (mass%)) / 100...Formula (1) In the formula (1), x represents the HLB value of the component (C), y represents the HLB value of the liquid paraffin, and z represents the HLB value of polyoxyethylene sorbitan monostearate (NIKKOL TS-10). The HLB value of the liquid paraffin can be determined in a similar manner using a combination of sorbitan monostearate (NIKKOL SS-10, HLB 4.7) and POE sorbitan monostearate (NIKKOL TS-10, HLB 14.9).
[0024] The HLB value of component (C) is not particularly limited, but is limited to 5.0 or less, and is preferably 4.6 or less, and more preferably 4.2 or less. The HLB value of component (C) is not particularly limited at its lower limit, but is, for example, 1.5 or more, preferably 2 or more, more preferably 3 or more, and even more preferably 3.5 or more.
[0025] Examples of the component (C) used in the topical composition of the present disclosure include glycerin fatty acid esters and / or sorbitan fatty acid esters.
[0026] Glycerol fatty acid esters having an HLB of 5.0 or less include monoglycerol fatty acid esters and polyglycerol fatty acid esters. Examples of glycerol fatty acid esters having an HLB of 5.0 or less include glycerol myristate and glycerol monostearate. Examples of polyglycerol fatty acid esters having an HLB of 5.0 or less include polyglycerol stearates (e.g., decaglycerol deca-stearate, hexaglycerol pentastearate, tetraglycerol tristearate, decaglycerol pentastearate, tetraglycerol pentastearate, pentaglycerol hexastearate, diglycerol monostearate, diglycerol distearate, hexaglycerol tristearate, etc.), polyglycerol oleates (e.g., decaglycerol decaoleate, decaglycerol pentaoleate, hexaglycerol pentaoleate, tetraglycerol pentaoleate, etc.), polyglycerol behenates (e.g., decaglycerol heptabehenate, decaglycerol dodecabehenate, hexaglycerol tetrabehenate, etc.), and polyglycerol erucate (e.g., decaglycerol octaerucate, etc.).
[0027] Examples of sorbitan fatty acid esters having an HLB of 5.0 or less include sorbitan monostearate, sorbitan sesquistearate, sorbitan tristearate, sorbitan sesquiisostearate, sorbitan oleate, sorbitan sesquioleate, and sorbitan trioleate.
[0028] The above nonionic surfactants having an HLB of 5.0 or less may be used alone or in combination of two or more kinds.
[0029] The content of the (C) component in the topical composition of the present disclosure is not particularly limited, and may be appropriately set according to the degree of the effect of suppressing the syneresis of petrolatum over time to be imparted, but the content of the (C) component relative to 100 parts by weight of the (A) component is, for example, 0.2 parts by weight or more, and from the viewpoint of enhancing the effect of suppressing the syneresis of petrolatum over time, preferably 1 part by weight or more, more preferably 1.5 parts by weight or more, even more preferably 2 parts by weight or more, even more preferably 2.5 parts by weight or more, 2.8 parts by weight or more, or 3 parts by weight or more. The content of the (C) component relative to 100 parts by weight of the (A) component is not particularly limited in its upper limit, but for example, 10 parts by weight or less, preferably 6 parts by weight or less, more preferably 5 parts by weight or less, even more preferably 4 parts by weight or less, or 3.5 parts by weight or less.
[0030] The specific content of the (C) component in the topical composition of the present disclosure is determined according to the content ratio of the above-mentioned (A) component and the (C) component, and may be, for example, 0.2% by weight or more. From the viewpoint of enhancing the effect of suppressing the syneresis of Vaseline over time, it is preferably 0.6% by weight or more, more preferably 1% by weight or more, even more preferably 1.4% by weight or more, and even more preferably 1.8% by weight or more. The specific content of the (C) component in the topical composition of the present disclosure is not particularly limited in its upper limit, and may be, for example, 10% by weight or less, preferably 6% by weight or less, more preferably 5% by weight or less, even more preferably 4% by weight or less, and even more preferably 3.5% by weight or less, 3% by weight or less, or 2.5% by weight or less.
[0031] The ratio of component (B) to component (C) in the topical composition of the present disclosure is determined depending on the respective contents of component (B) and component (C). The content of component (C) per 1 part by weight of component (B) is, for example, 0.1 to 10 parts by weight, preferably 0.5 to 5 parts by weight, more preferably 0.8 to 3.2 parts by weight, even more preferably 1.2 to 2.8 parts by weight, even more preferably 1.5 to 2.5 parts by weight, and particularly preferably 1.8 to 2.2 parts by weight.
[0032] Other oil-based The topical composition of the present disclosure can contain other oily bases other than the above-mentioned (A) component.The other oily bases include solid oils, other semi-solid oils other than the (A) component, and liquid oils.As the other oily bases, any one of solid oils, other semi-solid oils other than the (A) component, and liquid oils may be used, or two or more of them may be used in combination.
[0033] The solid oil is an oil that is solid at 25°C. The solid oil used in the topical composition of the present disclosure may be any oil that is used in cosmetics, topical quasi-drugs, or topical medicines, and examples thereof include solid fats and oils, waxes, synthetic ester waxes, solid hydrocarbon oils, higher alcohols, higher fatty acids, and silicone waxes. Examples of solid fats and oils include cocoa butter, lanolin, ozokerite, hydrogenated jojoba oil, and hydrogenated castor oil. Examples of solid waxes include candelilla wax, rice bran wax, beeswax, white beeswax, cotton wax, carnauba wax, shellac wax, Japan wax, and jojoba wax. Examples of synthetic ester waxes include myristyl myristate, cetyl myristate, stearyl stearate, cetyl stearate, cetyl palmitate, cholesteryl stearate, cholesteryl oleate, dextrin palmitate, and inulin stearate. Examples of solid hydrocarbon oils include polyethylene wax, paraffin wax, ceresin wax, and microcrystalline wax. Examples of higher alcohols include cetyl alcohol, stearyl alcohol, and behenyl alcohol. Examples of higher fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, 12-hydroxystearic acid, and undecylenic acid. These solid oils may be used alone or in combination of two or more. Among these solid oils, preferred examples include solid waxes (more preferably white beeswax) and solid hydrocarbon oils (more preferably microcrystalline wax).
[0034] When the topical composition of the present disclosure contains a solid oil, the content of the solid oil is, for example, 1 to 45 parts by weight, preferably 5 to 35 parts by weight, more preferably 10 to 30 parts by weight, even more preferably 13 to 27 parts by weight, and even more preferably 15 to 25 parts by weight, per 100 parts by weight of component (A).
[0035] When the topical composition of the present disclosure contains a solid oil, the specific content of the solid oil is, for example, 3 to 30% by weight, preferably 5 to 25% by weight, more preferably 10 to 20% by weight, and even more preferably 13 to 18% by weight.
[0036] The other semi-solid oil is an oil that is semi-solid at 25°C (it deforms irreversibly in response to stress, but does not have fluidity). The other semi-solid oil used in the topical composition of the present disclosure may be any oil that is used in cosmetics, topical quasi-drugs, or topical medicines, and may be, for example, semi-solid hydrocarbon oils and semi-solid waxes. Examples of semi-solid hydrocarbon oils include gelled hydrocarbons. Examples of semi-solid waxes include lanolin and refined lanolin. These other semi-solid oils may be used alone or in combination of two or more. Among these other semi-solid oils, preferably, semi-solid hydrocarbon oils (more preferably, gelled hydrocarbons) are used.
[0037] When the topical composition of the present disclosure contains a semi-solid oil, the content of the semi-solid oil is, for example, 1 to 15 parts by weight, preferably 2 to 13 parts by weight, more preferably 4 to 11 parts by weight, and even more preferably 6 to 9 parts by weight, per 100 parts by weight of component (A).
[0038] When the topical composition of the present disclosure contains a semi-solid oil, the specific content of the semi-solid oil is, for example, 1 to 13 wt %, preferably 2 to 10 wt %, more preferably 3 to 8 wt %, and even more preferably 4 to 6 wt %.
[0039] The liquid oil is an oil that is liquid at 25°C. The liquid oil used in the topical composition of the present disclosure may be any oil that is used in cosmetics, topical quasi-drugs, or topical medicines, and examples thereof include vegetable oils, fatty acids, ester oils, liquid silicone oils, and liquid hydrocarbon oils. Examples of vegetable oils include avocado oil, camellia oil, macadamia nut oil, olive oil, and jojoba oil. Examples of fatty acids include oleic acid and isostearic acid. Examples of ester oils include cetyl ethylhexanoate, ethylhexyl palmitate, octyldodecyl myristate, neopentyl glycol diethylhexanoate, glyceryl tri-2-ethylhexanoate, octyldodecyl oleate, isopropyl myristate, glyceryl triisostearate, and glyceryl divaleroxycinnamate-monoethylhexanoate. Examples of liquid silicone oils include dimethylpolysiloxane, methylhydrogenpolysiloxane, methylphenylpolysiloxane, and octamethylcyclotetrasiloxane. Examples of liquid hydrocarbon oils include liquid paraffin, squalene, and squalane. These liquid oils may be used alone or in combination of two or more. Among these liquid oils, fatty acids (more preferably isostearic acid) and liquid hydrocarbon oils (more preferably liquid paraffin) are preferred.
[0040] The content of the liquid oil in the topical composition of the present disclosure is, for example, 10 parts by weight or less (i.e., 0 to 10 parts by weight) relative to 100 parts by weight of the component (A), and from the viewpoint of enhancing syneresis inhibition, is preferably 9 parts by weight or less, more preferably 8 parts by weight or less, and even more preferably 7 parts by weight or less. Since the topical composition of the present disclosure has excellent syneresis inhibition properties, syneresis can be effectively inhibited even when it contains liquid oil. From this viewpoint, a suitable example of the content of the liquid oil in the topical composition of the present disclosure is preferably 2 to 10 parts by weight, preferably 4 to 10 parts by weight, and more preferably 5 to 10 parts by weight relative to 100 parts by weight of the component (A).
[0041] A specific example of the content of liquid oil in the topical composition of the present disclosure is 8% by weight or less (i.e., 0 to 8% by weight), and from the viewpoint of enhancing syneresis inhibition, the content is preferably 7% by weight or less, more preferably 6.5% by weight or less, and even more preferably 5.5% by weight or less. Since the topical composition of the present disclosure has excellent syneresis inhibition properties, syneresis can be effectively inhibited even if it contains liquid oil. From this viewpoint, a suitable example of the content of liquid oil in the topical composition of the present disclosure is preferably 1 to 8% by weight, preferably 2 to 8% by weight, and more preferably 3 to 8% by weight.
[0042] Oil-based gelling agent The topical composition of the present disclosure may further comprise an oily gelling agent (oil-soluble thickener). Examples of the oily gelling agent include dextrin fatty acid ester, sucrose fatty acid ester, and benzylidene derivatives of sorbitol. Examples of the dextrin fatty acid ester include dextrin palmitate, dextrin oleate, dextrin stearate palmitate, and dextrin (palmitic acid / ethylhexanoic acid). Examples of the sucrose fatty acid ester include sucrose fatty acid esters in which three or less of the eight hydroxyl groups of sucrose are esterified with higher fatty acids, and the higher fatty acids are stearic acid and / or palmitic acid, and examples of the benzylidene derivatives of sorbitol include monobenzylidene sorbitol and dibenzylidene sorbitol. These oily gelling agents may be used alone or in combination of two or more. Among these oil-based gelling agents, dextrin fatty acid esters are preferable, and dextrin palmitate is more preferable.
[0043] When the topical composition of the present disclosure contains an oily gelling agent, its content is not particularly limited, but can be, for example, 0.1 to 3 parts by weight, preferably 0.3 to 2 parts by weight, more preferably 0.6 to 1.5 parts by weight, and even more preferably 0.8 to 1.2 parts by weight per 100 parts by weight of the total amount of the oily base (the total of component (A), solid oil, other semi-solid oil, and liquid oil).
[0044] Other Ingredients The topical composition of the present disclosure may or may not contain other additives, as necessary, in addition to the above components, within the scope of not impairing the effects of the present invention. Examples of additives that may or may not be contained include water, monohydric lower alcohols having 1 to 5 carbon atoms, polyhydric alcohols (dihydric alcohols, trihydric alcohols, etc.), surfactants other than component (C) (anionic surfactants, nonionic surfactants other than component (C), amphoteric surfactants, etc., preferably nonionic surfactants other than component (C)), polyhydric alcohols, aqueous thickeners, pH regulators, buffers, solubilizers, chelating agents, preservatives, preservatives, antioxidants, stabilizers, fragrances, colorants, etc. These other additives may be used alone or in combination of two or more. In addition, when these additives are contained in the topical composition of the present disclosure, the content thereof may be appropriately set according to the type of additive used and the formulation form of the topical composition.
[0045] When the topical composition of the present disclosure contains water, the content of water is, for example, 0.5 to 10% by weight, preferably 1 to 6% by weight, and more preferably 2 to 4% by weight. When the topical composition of the present disclosure contains other surfactants, the content of the other surfactants is, for example, 0.2 to 10% by weight, preferably 0.6 to 6% by weight, and more preferably 1 to 3% by weight.
[0046] The topical composition of the present disclosure may or may not contain other medicinal ingredients, if necessary, in addition to the above-mentioned ingredients, so long as the effects of the present invention are not impaired. Examples of medicinal ingredients that may or may not be contained include antihistamines other than component (B), anti-inflammatory agents (allantoin, glycyrrhetinic acid, glycyrrhizic acid, stearyl glycyrrhetinate, aluminum chlorhydroxyl allantoin, aluminum dihydroxyl allantoin, azulene, guaiazulene, and salts thereof, other nonsteroidal anti-inflammatory drugs, and steroidal anti-inflammatory drugs), local anesthetics (lidocaine, mepivacaine, bromide, etc.), and the like. Examples of the other medicinal ingredients include pivacaine, anti-aging agents, astringents, antioxidants, moisturizers (heparinoids, hyaluronic acid, 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer (polyquaternium-51)), blood circulation promoters, antibacterial agents, bactericides (isopropylmethylphenol, etc.), cooling agents, warming agents, vitamins (vitamins A, B, C, E, etc.), amino acids, wound healing promoters, irritation relievers, analgesics, cell activators, enzyme components, herbal ingredients, etc. These other 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 disclosure, the content thereof may be appropriately set according to the type of medicinal ingredient used, the expected effect, etc. Preferably, the topical composition of the present disclosure is a non-steroidal preparation that does not contain a steroidal anti-inflammatory drug.
[0047] Formulation The formulation of the topical composition of the present invention is not particularly limited, and examples thereof include ointments, creams (specifically, water-in-oil emulsion compositions), and gels.
[0048] The product classification of the topical composition of the present invention may be any of medicines, quasi-drugs, and cosmetics, with medicines and quasi-drugs being preferred. EXAMPLES
[0049] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.
[0050] Test Example 1 The topical compositions shown in Table 1 were prepared. Specifically, an oil phase consisting of an oil component (I) and an aqueous phase consisting of an aqueous component (III) were heated and mixed at 80°C to prepare the topical compositions. The obtained topical compositions were centrifuged using a centrifuge at a rotation speed of 4000 rpm, a temperature of 40°C, and for 4 hours. Regarding the subsequent syneresis of the petrolatum, three expert panelists evaluated the degree of comfort with the quality of the topical compositions using a four-point scale: "4 points: comforting, 3 points: somewhat comforting, 2 points: somewhat less comforting, 1 point: less comforting."
[0051] [Table 1]
[0052] For the topical composition of Reference Example 1, no panelists gave a score of 1, but for the topical composition of Reference Example 2, all panelists gave a score of 1. In other words, the loss of confidence in the quality of the topical agent caused by the syneresis of petrolatum over time was significant in formulations with a petrolatum content of 50% by weight or more.
[0053] Test Example 2 The topical compositions shown in Tables 2 and 3 were prepared. Specifically, an oil phase consisting of an oil component (I) and a surfactant (II) and an aqueous phase consisting of an aqueous component (III) were heated and mixed at 80°C, and then the aqueous phase was gradually added to the oil phase while mixing to prepare each topical composition. In the following tables, "Polyquaternium-51-containing solution" refers to Lipidure (R)-PMB (NOF Corporation), containing 5% by weight of polyquaternium-51, and the remainder being water. 10 mL of each of the obtained external compositions was placed in a 15 mL centrifuge tube, and centrifuged using a centrifuge at a rotation speed of 4000 rpm, a temperature of 40 ° C, and for 4 hours. Regarding the amount of syneresis of the petrolatum that occurs thereafter, in Table 2, the syneresis amounts of each Example and Comparative Example were derived when the syneresis amount in Comparative Example 1 (expressed as a relative value of the height of the petrolatum syneresis phase that occurs in the centrifuge tube) was set to 5, and in Table 3, the syneresis amount of Example 8 was derived when the syneresis amount in Comparative Example 4 was set to 5. The smaller the syneresis amount, the higher the syneresis inhibition.
[0054] [Table 2]
[0055] [Table 3]
[0056] As shown by comparing Comparative Examples 1 to 4 with Examples 1 to 8, the amount of syneresis was suppressed by adding component (B) to a topical composition containing 50% by weight or more of component (A). Moreover, as shown by comparing Examples 1 to 4 with Examples 5 to 7, the amount of syneresis was more significantly suppressed by further adding component (C), a nonionic surfactant with an HLB of 5.0 or less. Considering that component (C) alone cannot suppress the syneresis of component (A) as shown in Comparative Example 3, it was found that the significant suppression of the amount of syneresis in Examples 5 to 7 and Example 8 is a unique effect due to the combination of component (B) and component (C).
[0057] Test Example 3 The topical compositions shown in Table 4 were prepared. Specifically, an oil phase consisting of an oily component (I) and a surfactant (II) and an aqueous phase consisting of an aqueous component (III) were heated and mixed at 80°C, and then the aqueous phase was gradually added to the oil phase while mixing to prepare each topical composition. The obtained topical compositions were centrifuged under the same conditions as in Test Example 2 to confirm the amount of syneresis. For Formulation Examples 1 to 3, the amount of syneresis was confirmed when the amount of syneresis of the topical composition of the formulation of Formulation Example 1, which was modified to lack only the (B) component, was set to 5, and for Formulation Examples 4 to 11, the amount of syneresis was confirmed when the amount of syneresis of the topical composition of Comparative Example 1 in Test Example 2 (which was the same as the amount of syneresis of the topical composition of Comparative Example 2) was set to 5. As a result, the amount of syneresis was suppressed in all of Formulation Examples 1 to 11, and further, in comparison with Formulation Examples 1 to 3, the amount of syneresis was more significantly suppressed in Formulation Examples 2 and 3 than in Formulation Example 1.
[0058] [Table 4]
Claims
1. A composition for topical use comprising (A) 50% by weight or more of petrolatum and (B) diphenhydramine.
2. The topical composition according to claim 1 , further comprising (C) a nonionic surfactant having an HLB of 5.0 or less.
3. The composition for external use according to claim 1 , wherein the content of the (B) component per 100 parts by weight of the (A) component is 0.1 parts by weight or more.
4. The composition for external use according to claim 1 , wherein the content of the (C) component per 100 parts by weight of the (A) component is 0.2 parts by weight or more.
5. 2. The composition for external use according to claim 1, wherein the content of the liquid oil per 100 parts by weight of component (A) is 10 parts by weight or less.
6. The composition for external use according to claim 1 , which is a water-in-oil emulsion composition.
7. The composition for external use according to claim 1 , which is a non-steroidal preparation.
Citation Information
Patent Citations
Hydrophobic ointment composition
JP2005015407A
Oily base agent for external use
JP2006335734A