Emulsified topical composition

Abstract

To provide an emulsified topical composition that reduces friction during application and enhances a cooling sensation.SOLUTION: An emulsified topical composition is prepared which contains 1.2 to 1.8 mass% of menthol, and 8.6 to 11 mass% of camphor, with a methyl salicylate content of less than 3 mass%.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to an emulsion composition for external use containing menthol and camphor. [Background technology]

[0002] Skin diseases such as hives, eczema, and rashes, as well as dry skin, are very uncomfortable for patients and can interfere with their daily lives. When the skin is subjected to irritation such as itching, the symptoms often worsen, leading to a vicious cycle.

[0003] In order to treat skin disorders, drugs containing antihistamines and antipruritic drugs containing steroids have been proposed (for example, Patent Document 1). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] JP 2023-59139 A Summary of the Invention [Problem to be solved by the invention]

[0005] However, depending on the skin condition or condition accompanied by discomfort or itchiness, the application of the topical agent itself may be irritating and place a heavy burden on the skin. Therefore, an object of the present invention is to provide an emulsified composition for external use which imposes less strain on the application site and has an excellent cooling sensation when applied. [Means for solving the problem]

[0006] As a result of intensive research into the above problems, the present inventors have found that by combining menthol and camphor to prepare an emulsion composition, it is possible to prepare a composition which imparts less strain to the application site when applied and has an excellent cooling sensation, and have thus completed the present invention.

[0007] That is, the present invention provides the emulsified topical compositions described below. Section 1. 1. An emulsified composition for external use, comprising 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor, and having a methyl salicylate content of less than 3% by mass. Section 2. Item 1. The emulsion composition for external use according to item 1, which is used to suppress itching. Section 3. Item 3. The emulsified composition for external use according to item 1 or 2, further comprising 30% by mass or more of water. Section 4. Item 4. The emulsified composition for external use according to any one of Items 1 to 3, which is in the form of a cream. Section 5 Item 5. The emulsified composition for external use according to any one of items 1 to 4, which is contained in a tube container.

[0008] Furthermore, the present invention provides the following methods. Section 6. A method for reducing friction when applying a composition for external use by adding 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor to the composition for external use to form an emulsion. Section 7. A method for enhancing the cooling sensation of a composition for external use by making 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor coexist in the composition for external use to form an emulsion. Effect of the Invention

[0009] The present invention makes it possible to provide an emulsified topical composition which imparts less stress to the application site when applied, particularly to areas affected by inflammation such as itching or rash, and further to provide an emulsified topical composition which provides an excellent cooling sensation. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0010] [Emulsified external composition] The emulsion composition for external use of the present invention is an emulsion composition for external use containing 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor.

[0011] (menthol) Menthol is not particularly limited as long as it is used in pharmaceuticals or quasi-drugs. Either natural or synthetic products can be used, and any of d-, l- or dl-isomers can be used. As menthol, essential oils containing menthol can also be used. Examples of such essential oils include peppermint oil, cool mint oil, spearmint oil, peppermint oil, etc. As menthol, particularly l-menthol and dl-menthol are preferred.

[0012] In the present invention, the content of menthol relative to the total amount of the composition is appropriately set depending on the balance with other components. The content of menthol relative to the total amount of the composition is 1.2% by mass to 1.8% by mass, preferably 1.2% by mass to 1.5% by mass, more preferably 1.25% by mass to 1.45% by mass, even more preferably 1.3% by mass to 1.4% by mass, and particularly preferably 1.35% by mass. When using an essential oil containing menthol, the content of menthol in the blended essential oil is set to be within the above range.

[0013] (camphor) The camphor used in the present invention is not particularly limited as long as it is used in pharmaceuticals or quasi-drugs. Either natural or synthetic camphor may be used, and any of d-, l- or dl-isomers may be used. Camphor may also be used as essential oil containing camphor. Examples of such essential oil include camphor oil. As camphor, dl-camphor is particularly preferred.

[0014] In the present invention, the camphor content relative to the total amount of the composition is appropriately set depending on the balance with other components, etc. The camphor content relative to the total amount of the composition is 8.6% by mass to 11% by mass, preferably 8.6% by mass to 10.6% by mass, more preferably 9% by mass to 10% by mass, and particularly preferably 9.6% by mass. When using an essential oil containing camphor, the camphor content in the essential oil to be blended is set to be within the above range.

[0015] In the present invention, the ratio of the content of camphor to the content of menthol is preferably 4.5 to 9.5 parts by mass, more preferably 5.0 to 9.0 parts by mass, 5.5 to 8.5 parts by mass, 6.0 to 8.0 parts by mass, or 7.0 to 7.5 parts by mass, per 1 part by mass of menthol, from the viewpoint of enhancing the effects of the present invention.

[0016] (water) The composition of the present invention preferably contains water. The content of water is not limited, but is preferably 10% by mass or more, 20% by mass or more, 30% by mass or more, 40% by mass or more, 50% by mass or more, 55% by mass or more, 60% by mass or more, 70% by mass or more, or 80% by mass or more, based on the total amount of the composition. The content of water is not limited, but is preferably 90% by mass or less, 85% by mass or less, 80% by mass or less, 70% by mass or less, or 65% by mass or less, based on the total amount of the composition.

[0017] (Amino acids or their derivatives, vitamins) In addition to menthol and camphor, the pharmaceutical composition of the present invention may further contain the following ingredients:

[0018] Examples of components that may be contained include amino acids or derivatives thereof, and the amino acids or derivatives thereof are preferably basic amino acids, more preferably lysine, δ-hydroxylysine, arginine, etc., and arginine may be any of D-, L-, and DL-forms, with L-form being preferred. The content of the amino acids or derivatives thereof is not limited, but is preferably 0.0001% by mass to 1% by mass, more preferably 0.001% by mass to 0.5% by mass, even more preferably 0.01% by mass to 0.45% by mass, and particularly preferably 0.1% by mass to 0.45% by mass, based on the total amount of the composition.

[0019] Another example of a component that may be contained is vitamins, such as vitamin A, vitamin B, vitamin C, vitamin D, vitamin E, nicotinic acid, vitamin K, and other vitamins.

[0020] Among these, vitamin A includes retinol, retinal, retinoic acid, and their pharmacologically acceptable salts or derivatives.Specific examples include, but are not limited to, retinol, retinal, retinoic acid, retinol palmitate (retinol palmitate ester), retinol acetate (retinol acetate ester), etc.Among these, retinol palmitate and retinol acetate are preferred.

[0021] Examples of vitamin B include vitamin B1, vitamin B2, vitamin B6, vitamin B12, nicotinic acid, pantothenic acid, folic acid, biotin, etc. Examples of vitamin B1 include dibenzoyl thiamine, dibenzoyl thiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate ester, thiamine diphosphate ester, thiamine diphosphate ester hydrochloride, thiamine triphosphate ester, thiamine triphosphate ester monophosphate, etc. Examples of vitamin B2 include riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, riboflavin tetranicotinate. etc.; vitamin B6 compounds include pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5'-pyridoxal phosphate, pyridoxamine hydrochloride, etc.; nicotinic acids include nicotinic acid and nicotinamide, etc.; vitamin B12 compounds include cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin, etc.; nicotinic acids include dl-α-tocopherol nicotinate, benzyl nicotinate, methyl nicotinate, β-butoxyethyl nicotinate, 1-(4-methylphenyl)ethyl nicotinate, etc.; pantothenic acids include pantothenic acid, calcium pantothenate, pantothenyl alcohol (D-panthenol), D-panthesine, D-pantethine, coenzyme A, pantothenyl ethyl ether, etc.

[0022] Examples of vitamin C include ascorbigen-A, ascorbyl stearate, ascorbyl palmitate, L-ascorbyl dipalmitate, ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbyl phosphate, sodium ascorbyl phosphate, and magnesium ascorbyl phosphate.

[0023] Examples of vitamin D include methylhesperidin, ergocalciferol, and cholecalciferol.

[0024] Examples of vitamin E include dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, and dl-α-tocopherol calcium succinate.

[0025] Examples of vitamin K include phylloquinone and falnoquinone.

[0026] Of these vitamins, vitamin E is preferred, and the content is not particularly limited, but is preferably 0.0001% by mass to 2.0% by mass, 0.01% by mass to 1.0% by mass, or 0.1 to 0.5% by mass relative to the total amount of the composition.

[0027] Other examples of such components include glycyrrhetinic acids such as glycyrrhetinic acid, stearyl glycyrrhetinate, glycyrrhetinic acid and / or its salts (dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, etc.); mefenamic acid, allantoin, glycol salicylate, and anti-inflammatory agents such as pharma- ceutical acceptable salts thereof. Among them, glycyrrhetinic acids and allantoin are preferred, and the content is not particularly limited, but the content of glycyrrhetinic acids is preferably 0.0001% by mass to 1.0% by mass, 0.001% by mass to 0.5% by mass, 0.05% by mass to 0.5% by mass, or 0.1% by mass to 0.2% by mass, and the content of allantoin is preferably 0.0001% by mass to 1% by mass, 0.001% by mass to 0.5% by mass, 0.01% by mass to 0.3% by mass, or 0.05% by mass to 0.1% by mass, relative to the total amount of the composition. One or more of these drugs may be used in combination. However, from the viewpoint of exerting the effect of the refreshing feeling of the present invention and not generating an unpleasant odor, it is preferable that methyl salicylate among the anti-inflammatory drugs is not contained in an amount of 3% by mass or more of the entire composition, and it is preferable that it is 2.5% by mass or less, 2.0% by mass or less, 2% by mass or less, 1.5% by mass or less, 1% by mass or less, 0.5% by mass or less, 0.3% by mass or less, 0.1% by mass or less, 0.01% by mass or less, 0.001% by mass or less, or 0.0001% by mass or less, and it is more preferable that it is not substantially contained.

[0028] (Base, carrier, additive, etc.) From the viewpoint of improving the feeling of use, stability, etc., the composition of the present invention may contain a base, carrier, additive, etc. in addition to menthol and camphor, so long as the effects of the present invention are not impaired.

[0029] Examples of the base, carrier, or additive include surfactants, higher fatty acids, higher alcohols, hydrocarbons, fats and oils, waxes, ester oils, silicone oils, moisturizing ingredients, polyhydric alcohols, thickeners, refreshing agents other than menthol or camphor, essential oils, preservatives or antiseptics, pH adjusters, chelating agents, etc. These ingredients can be used alone or in any combination of two or more.

[0030] The surfactant may be any of a nonionic surfactant, a cationic surfactant, an anionic surfactant, an amphoteric surfactant, and the like.

[0031] Examples of nonionic surfactants include sorbitan fatty acid esters (e.g., sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexyl acid, diglycerol sorbitan tetra-2-ethylhexyl acid, etc.); propylene glycol fatty acid esters (e.g., propylene glycol monostearate, etc.); hydrogenated castor oil derivatives (e.g., polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hydrogenated castor oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80 (HCO-80), etc.); polyoxyethylene sorbitan fatty acid esters (e.g., monolaurate, polyoxyethylene (20) sorbitan urate (polysorbate 20), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), polyoxyethylene (20) sorbitan monooleate (polysorbate 80), polyoxyethylene (20) sorbitan isostearate, etc.); glycerin derivatives (e.g., polyoxyethylene monococoyl glyceryl, glycerin alkyl ether); polyoxyalkylene alkyl ethers (e.g., polyoxyethylene cetyl ether, etc.); silicone surfactants (e.g., polyoxyethylene-methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, PEG-9 polydimethylsiloxyethyl dimethicone, etc.); alkyl glucosides; and the like.

[0032] Examples of cationic surfactants include benzalkonium chloride, benzethonium chloride, and the like.

[0033] Examples of anionic surfactants include fatty acid soaps (e.g., sodium laurate, sodium palmitate, potassium laurate, potassium myristate, potassium palmitate, potassium stearate, etc.); alkyl sulfates (e.g., sodium lauryl sulfate, potassium lauryl sulfate, etc.); alkyl ether sulfates (e.g., POE-lauryl sulfate triethanolamine, POE-lauryl sulfate sodium, sodium laureth sulfate, etc.); N-acylsarcosinates (e.g., sodium lauroyl sarcosinate, etc.); higher fatty acid amide sulfonates (e.g., sodium N-myristoyl-N-methyl taurine, sodium coconut oil fatty acid methyl taurine, sodium lauryl methyl taurine, etc.); phosphates (sodium POE-oleyl ether phosphate, sodium POE-stearyl ether phosphate, sodium lauryl phosphate, sodium polyoxyethylene lauryl ether phosphate, etc.); sulfosuccinates (e.g., sodium alkyl sulfosuccinate, sodium di-2-ethylhexyl sulfosuccinate, sodium polyoxyethylene sulfosuccinate, etc.). thorium, sodium lauryl polypropylene glycol sulfosuccinate, etc.; alkylbenzene sulfonates (e.g., sodium linear dodecylbenzene sulfonate, triethanolamine linear dodecylbenzene sulfonate, linear dodecylbenzene sulfonic acid, etc.); amino acid surfactants (e.g., sodium cocoyl glutamate, N-acyl glutamate, etc.); N-acyl glutamate (e.g., potassium lauroyl glutamate, monosodium N-lauroyl glutamate, disodium N-stearoyl glutamate, monosodium N-myristoyl-L-glutamate, etc.); higher fatty acid ester sulfates (e.g., sodium hydrogenated coconut oil fatty acid glycerin sulfate, etc.); sulfated oils (e.g., turmeric oil, etc.); ether carboxylates (e.g., polyoxyethylene alkyl ether carboxylates, polyoxyethylene alkyl allyl ether carboxylates, sodium polyoxyethylene lauryl ether acetate, etc.); α-olefin sulfonates; higher fatty acid ester sulfonates; secondary alcohol sulfates; higher fatty acid alkylol amide sulfates;Examples include sodium lauroyl monoethanolamide succinate; ditriethanolamine N-palmitoyl aspartate; and sodium caseinate.

[0034] Examples of amphoteric surfactants include glycine type surfactants such as alkyldiaminoethylglycine, acetate betaine type surfactants such as lauryldimethylaminoacetate betaine, imidazoline type surfactants, and phospholipid surfactants such as lecithin.

[0035] In the present invention, the surfactant is preferably a phospholipid, and more preferably lecithin.

[0036] As the higher fatty acid, for example, a saturated or unsaturated straight-chain or branched-chain fatty acid having 12 to 22 carbon atoms can be used. For example, preferred examples include straight-chain saturated fatty acids (solid at room temperature) such as lauric acid, myristic acid, palmitic acid, stearic acid, or behenic acid; unsaturated fatty acids (liquid at room temperature) such as oleic acid, linoleic acid, linolenic acid, palmitoleic acid, eicosapentaenoic acid, vaccenic acid, or docosahexaenoic acid; or branched fatty acids such as isostearic acid or lanolin fatty acid, or 12-hydroxystearic acid.

[0037] In the present invention, the higher fatty acid is preferably stearic acid.

[0038] Examples of higher alcohols include higher alcohols having 12 to 22 carbon atoms, sterols, etc. Preferred examples include linear saturated alcohols (solid at room temperature) such as lauryl alcohol, myristyl alcohol, cetanol, cetostearyl alcohol, stearyl alcohol, arachyl alcohol, and behenyl alcohol; unsaturated alcohols (liquid at room temperature) such as oleyl alcohol and selachyl alcohol; or hexyldecanol, isostearyl alcohol, octyldodecanol, decyltetradecanol, and lanolin alcohol.

[0039] In the present invention, the higher alcohol is preferably one or more selected from the group consisting of stearyl alcohol, cetanol, and behenyl alcohol.

[0040] Examples of hydrocarbons include petrolatum, paraffin, ceresin, isoparaffin, hard fat, microcrystalline wax, polybutene, polyethylene powder, liquid paraffin, squalane, gelled hydrocarbons (such as plastibase), ozokerite, α-olefin oligomers, light liquid paraffin, and hydrocarbons such as light liquid paraffin.

[0041] Examples of fats and oils include avocado oil, linseed oil, camellia oil, macadamia nut oil, corn oil, olive oil, safflower oil, apricot kernel oil, jojoba oil, grape seed oil, sunflower oil, almond oil, camellia oil, rapeseed oil, sesame oil, castor oil, cacao butter, coconut oil, hardened coconut oil, palm oil, palm kernel oil, wheat germ oil, rice germ oil, rice bran oil, cottonseed oil, soybean oil, peanut oil, tea seed oil, evening primrose oil, kukui nut oil, hazelnut oil, shea butter, orange oil, and chamomile oil.

[0042] Examples of waxes include candelilla wax, rice bran wax, cotton wax, carnauba wax, lanolin, lanoline fatty acid isopropyl, POE lanolin alcohol ether, POE lanolin alcohol acetate, lanoline fatty acid polyethylene glycol, POE hydrogenated lanolin alcohol ether, shellac wax, beeswax, and Japan wax.

[0043] Ester oils include isopropyl myristate, butyl myristate, decyl myristate, myristyl myristate, cetyl myristate, isopropyl palmitate, cetyl palmitate, ethyl stearate, butyl stearate, stearyl stearate, isocetyl stearate, hexyl laurate, ethyl oleate, ethyl linoleate, isopropyl linoleate, cetyl caprylate, decyl oleate, oleyl oleate, isodecyl oleate, cetyl octanoate, 2-octyldodecyl myristate, 2-Octyldodecyl Dimethyloctanoate, Hexyldecyl Dimethyloctanoate, 2-Hexyldecyl Myristate, 2-Hexyldecyl Palmitate, Diisopropyl Adipate, 2-Hexyldecyl Adipate, Diethyl Sebacate, Diisopropyl Sebacate, Isocetyl Isostearate, Isostearyl Isostearate, Isononyl Isononanoate, Isotridecyl Isononanoate, Cholesteryl 12-Hydroxystearate, Cholesteryl Stearate, Cholesteryl Oleate, Phytos Macadamia Nut Fatty Acid teryl, phytosteryl oleate, inulin stearate, ethylene glycol di-2-ethylhexanoate, cetyl 2-ethylhexanoate, N-alkyl glycol monoisostearate, neopentyl glycol dicaprate, glycerin di-2-heptylundecanoate, tri-2-ethylhexyl trimellitate, tritridecyl trimellitate, trimethylolpropane tri-2-ethylhexylate, trimethylolpropane triisostearate, pentaerythritol tetra-2-ethylhexanoate, tri-2-ethylhexyl Glyceryl xanthate, trimethylolpropane triisostearate, cetyl 2-ethylhexanoate, glyceryl trimyristate, tri(caprylic / capric)glyceryl, tri(caprylic / capric / myristic / stearic)glyceryl, medium chain triglyceride, castor oil fatty acid methyl ester, di(phytosteryl / octyldodecyl) lauroyl glutamate, di(octyldodecyl / phytosteryl / behenyl) lauroyl glutamate, cetyl lactate, myristyl lactate, cyclohexane-1,Examples of suitable glyceryl triglyceride include bisethoxydiglycol 4-dicarboxylate, lanolin acetate, ethyl acetate, butyl acetate, amyl acetate, triethyl citrate, dimer dilinoleate (phytosteryl / isostearyl / cetyl / stearyl / behenyl), dimer dilinoleyl dimer dilinoleate, dipentaerythrityl tripolyhydroxystearate, and tri(behenic acid / isostearic acid / eicosanedioic acid)glyceryl.

[0044] Examples of silicone oils include siloxanes such as methylpolysiloxane, methylphenylpolysiloxane, decamethyltetrasiloxane, methylcyclopentasiloxane, highly polymerized methylpolysiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, methylhydrogenpolysiloxane, methyltrimethicone, dimethiconol, dimethiconol crosspolymer, alkyl-modified silicones such as caprylyl methicone, amino-modified silicones such as aminopropyl dimethicone and amodimethicone, crosslinked methylpolysiloxane, crosslinked alkyl-modified silicone, amino-modified silicone, polyether-modified silicone, polyglycerin-modified silicone, crosslinked polyether-modified silicone, crosslinked alkyl polyether-modified silicone, silicone / alkyl chain co-modified polyether-modified silicone, silicone / alkyl chain co-modified polyglycerin-modified silicone, polyether-modified branched silicone, polyglycerin-modified branched silicone, acrylic silicone, phenyl-modified silicone, and silicone resin.

[0045] Examples of moisturizing components include hyaluronic acid (including hydrolyzed hyaluronic acid, low molecular weight hyaluronic acid, etc.); salts of hyaluronic acid (for example, sodium hyaluronate, zinc hyaluronate, low molecular weight zinc hyaluronate, etc.); hyaluronic acid derivatives (acetylated hyaluronic acid or its salts (for example, sodium acetylated hyaluronate, zinc acetylated hyaluronate, etc.), crosslinked hyaluronic acid derivatives (sodium hyaluronate crosspolymer, etc.), sodium carboxymethyl hyaluronate, unsaturated hyaluronic acid or its salts, hydrolyzed hyaluronic acid, etc.), and the like. Alkyl (C12-13) glyceryl hyaluronate, cationic hyaluronic acid derivatives (hydroxypropyltrimonium hyaluronate, etc.), dimethylsilanol hyaluronate, etc.); chondroitin sulfate or its salts (sodium chondroitin sulfate, potassium chondroitin sulfate, sodium dermatan sulfate, potassium dermatan sulfate, etc.); heparinoids, amino acids such as alanine, serine, aspartic acid, glycine, proline, hydroxyproline, glucosamine, theanine, arginine, and their derivatives. Conductors; polyhydric alcohols; alkylene oxides such as PPG-17 buteth-17, PPG-25 sorbitol, polyoxyalkylene alkyl glucosides, PEG / PPG / polybutylene glycol-8 / 5 / 3 glycerin, polyoxyalkylene diglyceryl; glycosyl trehalose, trehalose; ceramide, glucosyl ceramide, cholesterol, phytosterol, cholesterol derivatives, phytosterol derivatives; 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolyester Examples of such ingredients include 2-methacryloyloxyphosphorylcholine-containing polymers such as polymer liquid and polymethacryloyloxyethyl phosphorylcholine; NMF-derived components such as lactic acid, sodium lactate, sodium pyrrolidone carboxylate, and urea; collagen, elastin, keratin, chitin, chitosan, and the like and their hydrolysates; hydroxyethyl urea; and components derived from plants (for example, aloe, seaweed, pueraria lobata, chlorella, lemongrass, chamomile, witch hazel, tea, shiso, grapefruit, and gynostemma pentaphyllum).

[0046] Examples of polyhydric alcohols include low molecular weight alcohols having two or more hydroxyl groups, such as glycerin, diglycerin, triglycerin, propylene glycol, dipropylene glycol, 1,3-butanediol, ethylene glycol, diethylene glycol, isoprene glycol, 1,3-butylene glycol, 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, decanediol, neopentyl glycol, sorbitol, xylitol, erythritol, and mannitol.

[0047] Examples of thickeners include vinyl thickeners such as polyvinyl alcohol, polyvinylpyrrolidone, polyvinyl methyl ether, and carboxyvinyl polymers; cellulose thickeners such as methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, carboxyethylcellulose, and hydrophobized hydroxypropylmethylcellulose; guar gum, sclerotium gum, tamarind gum, xanthan gum, dextran, pectin, pullulan, gelatin, locust bean gum, carrageenan, agar, biosaccharide gum, acrylic acid alkyl methacrylate copolymer, sodium polyacrylate, bentonite, dextrin fatty acid ester, dimethyl distearyl ammonium hectorite, sodium alginate, polyethylene glycol, trimethylammonium chloride hydroxypropyl guar gum, trimethylammonio chloride hydroxypropyl hydroxyethyl cellulose, (hydroxyethyl acrylate / Na acryloyldimethyl taurate) copolymer, (ammonium acryloyldimethyl taurate / vinylpyrrolidone) copolymer, and the like.

[0048] Examples of cooling agents other than menthol and camphor include terpenes such as borneol, geraniol, cineol, anethole, limonene, and eugenol (which may be in any of the d-, l- or dl-forms).

[0049] Examples of essential oils include eucalyptus oil, bergamot oil, fennel oil, cinnamon oil, rose oil, turpentine oil, and lavender oil. However, in order to more significantly enhance the cooling sensation of the composition of the present invention, the amount of eucalyptus oil is preferably less than 1.5% by mass of the entire composition, more preferably 1.45% by mass or less, even more preferably 1.4% by mass or less, even more preferably 1.35% by mass or less, and particularly preferably 1.3% by mass or less. When contained, the amount is preferably 0.0001% by mass or more, 0.001% by mass or more, 0.01% by mass or more, 0.1% by mass or more, 0.5% by mass or more, or 1.0% by mass or more of the entire composition. Eucalyptus oil may not be included.

[0050] Examples of preservatives or antiseptics include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, benzyl paraoxybenzoate, methyl paraoxybenzoate, phenoxyethanol, benzyl alcohol, methylisothiazoline, iodopropynyl butylcarbamate, chlorobutanol, 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediol.

[0051] Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, citric acid, tartaric acid, malic acid, succinic acid), organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.), as well as salts thereof, inorganic bases (potassium hydroxide, sodium hydroxide, etc.), and the like.

[0052] Examples of chelating agents include ethylenediaminetetraacetic acid (edetic acid), ethylenediaminetetraacetate (sodium salt (sodium edetate: Japanese Pharmacopoeia, EDTA-2Na, etc.), potassium salt, etc.), phytic acid, gluconic acid, polyphosphoric acid, metaphosphoric acid, etc.

[0053] Although not limited, the topical composition of the present invention is preferably a composition consisting of only natural or naturally derived raw materials. Here, the term "natural raw materials" refers to raw materials obtained from animals, plants, or minerals and not intentionally chemically modified, which is the same as the term "natural raw materials" defined in ISO 16128. The term "natural raw materials" refers to raw materials obtained from animals, plants, or minerals and intentionally chemically modified. Alternatively, the emulsified topical composition of the present invention preferably has a natural index of 50 or more, 60 or more, 70 or more, 80 or more, or 90 or more, more preferably 95 or more, and most preferably 100, taking water into consideration.

[0054] [Manufacturing method] The method for producing the pharmaceutical composition of the present invention is not particularly limited and can be appropriately determined.

[0055] Specifically, the components may be heated to dissolve as necessary, mixed, and then stirred while cooling in a water bath, and then allowed to stand at room temperature, but the method is not particularly limited thereto.

[0056] [Formulation] The composition of the present invention is, for example, mixed with a base or carrier normally used in pharmaceuticals or quasi-drugs, and, if necessary, with additives to prepare an emulsified composition for external use. The emulsified composition for external use may be either an oil-in-water type emulsion composition or a water-in-oil type emulsion composition, but is preferably an oil-in-water type emulsion composition.

[0057] The form of the composition of the present invention is not particularly limited, but it is preferably in the form of an emulsified external composition. Examples of such forms include creams, suspensions, emulsions, milky lotions, gels, liniments, lotions, patches, etc. These preparations can be manufactured according to the method described in the General Provisions of Preparations of the Japanese Pharmacopoeia, 18th Edition. Among them, creams are preferred from the viewpoint of being less sticky, having a good feel when used, and exerting the effects of the present application.

[0058] [pH] The pH of the composition of the present invention is usually pH 4.0 to 8.0, and examples of preferred values ​​include pH 4.5 to 7.5, pH 5.0 to 7.5, pH 5.5 to 7.5, pH 6.0 to 7.5, pH 6.5 to 7.5, and pH 7.0 to 7.5. The pH can be adjusted, for example, by using a pH adjuster. However, this does not apply to formulations in which pH measurement is impossible or difficult.

[0059] [container] The composition of the present invention can be stored and used in a container of a shape and material appropriately selected according to the purpose and application. Specific examples of containers include a container with a nozzle, a container with a pump, a jar container, a tube container, a container with a hole in the inner plug, a container with a hinge cap, a sponge head container, a roll-on container, and the like. Among these, a tube container is particularly preferred. By storing in these containers, the composition of the present invention can be applied directly or indirectly to the desired affected area. The nozzle or sponge can also be designed to have a tapered or large diameter so that it can be applied to a narrow or wide area of ​​the affected area. After applying the composition according to this embodiment to the affected area, it can also be used by spreading it with a nonwoven fabric, fingers, or the like.

[0060] Examples of materials for the container include polyethylene terephthalate, polybutylene terephthalate, polyethylene naphthalate, polypropylene, polyethylene (HDPE, LDPE, LLDPE, etc.), ABS resin, polycarbonate, fluororesin, polyvinyl chloride, polyamide, ethylene vinyl alcohol resin, polystyrene, glass, and metal (aluminum, etc.). Taking into consideration strength, flexibility, weather resistance, stability of components, etc., these materials can be used as container materials by performing various coating treatments, combining these materials by, for example, mixing them, or laminating them.

[0061] [Methods for reducing friction] The present invention also relates to a method for reducing friction during application of the topical composition by coexisting 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor to form an emulsion. "Reducing friction during application" reduces the burden on the application site, particularly on the inflamed affected area, when the composition is applied to the skin. This reduction in friction further improves the medicinal effect and usability, and also leads to ease of spreading when spreading by hand. Here, the contents, ratios, and other conditions of each component are as described in [Emulsion topical composition].

[0062] [Method to enhance cooling sensation] The present invention also relates to a method for enhancing the cooling sensation of the composition for external use by coexisting 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor to form an emulsion. The enhanced cooling sensation provides an itching suppression effect. Therefore, the composition of the present invention is particularly effective as an itching suppressant even when the natural origin index is increased. Here, the contents, ratios, and other conditions of each component are in accordance with those described in [Emulsion composition for external use].

[0063] [Application] The emulsion composition for external use of the present invention is particularly effective for suppressing itching, redness, or itching, and is used according to symptoms and conditions.The composition of the present invention has an effect on, but is not limited to, senile skin pruritus, eczema (skin eczema including scalp eczema and hand eczema), dermatitis, itching, rash, hives, sores, heat rash, chilblains, insect bites, dryness, etc.The composition of the present invention also has an effect on itching caused by a sensation of burning or tingling, redness spreading when scratched, and repeated itching.

[0064] From the viewpoint of the effect on the skin, the present invention is preferably used in a product applied as a skin external preparation (a preparation for the skin). The application site of the skin includes the skin of the hands (palms, backs of the hands, fingers), face, feet, head (scalp), neck, chest, armpits, back, waist, back of the elbows, and back of the knees. In particular, the use for the hands, face, feet, and neck is preferable, and the use for the hands or face is particularly preferable. For example, it can be suitably used as an anti-itch cream for medicines or quasi-drugs. The pharmaceutical composition of the present invention can be used in a known or commonly used dosage and administration manner, once or several times a day, depending on the purpose. EXAMPLES

[0065] Next, the present invention will be specifically described with reference to examples, but the present invention is not limited to the following examples.

[0066] [Test Example 1. Friction test] The topical compositions of the Examples and Comparative Examples were prepared by a conventional method. The components and contents of each composition are as shown in Table 1. Examples 1 to 3 and Comparative Example 1 are emulsion compositions, Comparative Example 2 is a composition in the form of an ointment, and Examples 1 to 3 are oil-in-water emulsion compositions. A friction test was carried out on these compositions to examine whether there was a difference in the friction resistance of the formulations depending on the concentration of menthol and camphor. A portable tactile system (TRIBOGEAR TYPE:33, manufactured by Shinto Scientific Co., Ltd.) was used for the friction test. A Strat-M Membrane (Size 25mm Discs, Qty 60, Lot 0000162464) was fixed to the center of the device with double-sided tape. Then, 5μl of each composition was dropped onto the center of the membrane, and the index finger was slid in a circular motion on the membrane for 120 seconds. The sliding speed was 3.3 round trips / sec.

[0067] The ratio of the friction coefficient to that of Comparative Example 1 was calculated from the average value of the friction coefficient from the start of the test until 120 seconds had elapsed. Friction coefficient ratio = average value of friction coefficients in each test example for 120 seconds / average value of friction coefficients in Comparative Example 1 for 120 seconds. The evaluation results are shown according to the calculated friction coefficient ratio (Table 2). 0.86 or less: ◎ 0.86~0.93:〇 0.93 or higher: ×

[0068] [Table 1]

[0069] [Table 2]

[0070] As a result, it was confirmed that the emulsion compositions of the Examples had a friction reducing effect compared to the Comparative Examples.

[0071] [Test Example 2. Evaluation of Usability] The emulsified compositions for external use shown in Table 3 were prepared by conventional methods. Example 1 and Comparative Example 3 were each evaluated for usability. A quantity of the index finger (1 FTU = approximately 0.5 g) was taken from the tip to the first joint, and applied to the cheeks around the cheekbones of four expert panelists (professionals) who regularly prepare and evaluate formulations, and gently spread the applied composition over an area of ​​3 cm x 3 cm until it was slightly shiny. The "cooling sensation (refreshing sensation / refreshing sensation)" immediately after application was evaluated relatively.

[0072] [Table 3]

[0073] The results are also shown in Table 4. Note that the stronger the cooling sensation, the stronger the perceived medicinal effect on itching symptoms. [Table 4]

[0074] It was confirmed that the composition of Example 1 provided a stronger cooling sensation than the composition of Comparative Example 3. Furthermore, the composition of Comparative Example 3 had an unpleasant odor similar to that of a compress, and did not feel good when used.

[0075] The emulsified compositions for external use shown in Table 5 were prepared by a conventional method. Example 4 is an oil-in-water type emulsion composition. For each of Examples 3 and 4, an evaluation of the feeling of use was carried out. A quantity of the index finger, the length of which was extended from the tip to the first joint (1 FTU = approximately 0.5 g), was taken and applied to the cheeks around the cheekbones of two expert panelists (professionals) who regularly prepare and evaluate formulations, and the composition was gently spread over an area of ​​3 cm x 3 cm so that the applied composition was slightly shiny. The "cooling sensation (refreshing sensation / refreshing sensation)" immediately after application was evaluated relatively.

[0076] [Table 5]

[0077] As a result, both Examples 3 and 4 provided a good cooling sensation immediately after application, but Example 3 provided a stronger cooling sensation. Example 4 provided a slightly weaker cooling sensation than Example 3.

[0078] [Test Example 3. Evaluation of Itch Suppression] An emulsion composition of Example 5 was prepared, which contains 1.35% by mass of l-menthol and 9.6% by mass of dl-camphor, and further contains water, sugar squalane, stearyl alcohol, glycerin, cetanol, stearic acid, eucalyptus oil, behenyl alcohol, lavender oil, L-arginine, and turpentine. Example 5 is an oil-in-water emulsion composition. The itching suppression effect of this emulsion composition was evaluated. Six adults with itching symptoms applied the preparation to the site where they felt itchy, and the immediate effect of suppressing itching caused by insect bites, the duration of the effect of suppressing itching caused by insect bites, and the immediate effect of suppressing itching other than insect bites, such as rashes, were each evaluated on a scale of 1 to 5. The closer the number is to 5, the more pronounced the effect is.

[0079] [evaluation] 1: No feeling at all 2: Somewhat 3: Feel 4: I feel it very much 5: I feel very strongly

[0080] The results (six individual scores and average scores) are shown in Table 6. [Table 6]

[0081] It was confirmed that the composition of Example 5 had the effect of suppressing itching by applying it to the area experiencing itchy symptoms.

[0082] [Formulation example] Formulation examples are shown in Table 7 below. All units are mass %. All formulation examples are creams or emulsions.

[0083] [Table 7]

Claims

1. An emulsified composition for external use comprising 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor, and a methyl salicylate content of less than 3% by mass.

2. 2. The emulsified topical composition according to claim 1, which is for suppressing itching.

3. The emulsified composition for external use according to claim 1 , further comprising 30% by mass or more of water.

4. 2. The emulsified composition for external use according to claim 1, which is in the form of a cream.

5. The emulsified composition for external use according to claim 1 , which is contained in a tube container.

6. A method for reducing friction during application of a composition for external use by making 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor coexist in the composition for external use to form an emulsion.

7. A method for enhancing the cooling sensation of a composition for external use by making 1.2% by mass to 1.8% by mass of menthol and 8.6% by mass to 11% by mass of camphor coexist in the composition for external use to form an emulsion.

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