JP7422261B1 - Emulsified external composition - Google Patents

Abstract

An object of the present invention is to provide an emulsified external composition with reduced friction during application and enhanced cooling sensation. [Solution] An emulsified topical composition is prepared that contains 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass of camphor, and the content of methyl salicylate is less than 3% by mass. do. [Selection diagram] None

Description

The present invention relates to an emulsified external composition containing menthol and camphor.

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 skin becomes irritated, such as itching, the symptoms often worsen, creating a vicious cycle.

In response to skin disorders, drugs containing antihistamines and antipruritics containing steroids have been proposed (for example, Patent Document 1).

Japanese Patent Application Publication No. 2023-59139

However, due to skin disorders or conditions that are accompanied by discomfort or itching, the application of the external preparation itself may be irritating, increasing the burden on the skin.
SUMMARY OF THE INVENTION Therefore, an object of the present invention is to provide an emulsified external composition that places less burden on the application site and provides an excellent refreshing feeling when applied.

As a result of intensive research into the above-mentioned problems, the present inventors have found that by combining menthol and camphor to form an emulsified composition, a composition that places less burden on the application site and has an excellent cooling sensation when applied. The inventors have discovered that it is possible to prepare a product, and have completed the present invention.

That is, the present invention provides the following emulsified external composition.
Item 1.
An emulsified external composition containing 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass of camphor, and the content of methyl salicylate is less than 3% by mass.
Item 2.
Item 2. The emulsified external composition according to item 1, which is for suppressing itch.
Item 3.
Item 3. The emulsified external composition according to Item 1 or 2, further comprising 30% by mass or more of water.
Item 4.
Item 4. The emulsified external composition according to any one of Items 1 to 3, which is in the form of a cream.
Section 5
Item 5. The emulsified external composition according to any one of Items 1 to 4, which is housed in a tube container.

Furthermore, the present invention provides the following methods.
Item 6.
By coexisting 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass of camphor in the external composition to form an emulsion, friction during application of the external composition is reduced. how to.
Section 7.
A method for enhancing the cooling sensation of an external composition by coexisting 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass of camphor to form an emulsion. .

ADVANTAGE OF THE INVENTION According to the present invention, there is provided an emulsified topical composition that reduces the burden on the application site when applied, and in particular reduces the burden on affected areas that are inflamed due to itching or rashes, and further provides an emulsified composition that has an excellent cooling sensation. It becomes possible to provide compositions for external use.

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

(menthol)
Menthol is not particularly limited as long as it is used in pharmaceuticals or quasi-drugs. Both natural products and synthetic products can be used, and any of the d-, l-, and dl-forms may 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, and peppermint oil. Especially preferred as menthol are l-menthol and dl-menthol.

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 is 1.2% by mass to 1.8% by mass, preferably 1.2% by mass to 1.5% by mass, more preferably 1% by mass, based on the total amount of the composition. .25% to 1.45% by weight, more preferably 1.3% to 1.4% by weight, particularly preferably 1.35% by weight. In addition, when using essential oil containing menthol, the content of menthol in the essential oil to be blended is set to be within the above range.

(camphor)
The camphor used in the present invention is not particularly limited as long as it is used in pharmaceuticals or quasi-drugs. Both natural products and synthetic products can be used, and any of the d-, l-, and dl-forms may be used. As camphor, essential oil containing camphor can also be used. Examples of such essential oils include camphor oil and the like. As camphor, dl-camphor is particularly preferred.

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

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

(water)
Preferably, the composition of the present invention contains water. The content of water is not limited, but is 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, based on the total amount of the composition. It is preferably at least 70% by mass, and preferably at least 80% by mass. The water content 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, 65% by mass or less based on the total amount of the composition. .

(Amino acids or their derivatives, vitamins)
The pharmaceutical composition of the present invention may further contain the following components in addition to menthol and camphor.

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, or arginine, and arginine is D-form. , L-form, or DL-form, but L-form is preferable. The content of amino acids or derivatives thereof, etc. 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, and more preferably 0.0001% by mass to 1% by mass, and It is preferably 0.01% to 0.45% by weight, particularly preferably 0.1% to 0.45% by weight.

Another example of the components that may be included is vitamins. As the vitamins, any of vitamin A, vitamin B, vitamin C, vitamin D, vitamin E, nicotinic acids, vitamin K, and other vitamins can be used.

Among these, examples of vitamin A include retinol, retinal, retinoic acid, and pharmacologically acceptable salts or derivatives thereof. Specific examples include retinol, retinal, retinoic acid, retinol palmitate (retinol palmitate), retinol acetate (retinol acetate), but are not limited to these. Among these, retinol palmitate and retinol acetate are preferred.

Examples of B vitamins include vitamin B1, vitamin B2, vitamin B6, vitamin B12, nicotinic acids, pantothenic acids, folic acid, biotin, and the like. Vitamin B1 types include dibenzoylthiamine, dibenzoylthiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, and thiamine monophosphate. Acid ester phosphate, thiamine monophosphate, thiamine diphosphate, thiamine diphosphate hydrochloride, thiamine triphosphate, thiamine triphosphate monophosphate, etc.; Vitamin B2 types include riboflavin, flavin mononucleotide, flavin Adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, sodium riboflavin 5'-phosphate, riboflavin tetranicotinate, etc.; as vitamin B6, pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, pyridoxal 5'-phosphate , pyridoxamine hydrochloride, etc.; Nicotinic acids include nicotinic acid, nicotinamide, etc.; Vitamin B12s include cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin, etc.; nicotinic acids include dl-α-tocopherol nicotinate, nicotinic acid Benzyl, methyl nicotinate, β-butoxyethyl nicotinate, 1-(4-methylphenyl)ethyl nicotinate, etc.; Pantothenic acids include pantothenic acid, calcium pantothenate, pantothenyl alcohol (D-panthenol), D- Examples include panthesain, D-pantethine, coenzyme A, pantothenyl ethyl ether, and the like.

Examples of vitamin C include ascorbigen-A, ascorbyl stearate, ascorbyl palmitate, L-ascorbyl dipalmitate, ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbic acid phosphate, and phosphorus ascorbyl. Examples include acid sodium salt, magnesium ascorbic acid phosphate, and the like.

Examples of vitamin D include methylhesperidin, ergocalciferol, cholecalciferol, and the like.

Examples of vitamin E include dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate, and the like.

Examples of vitamin K include phylloquinone and farnoquinone.

Among these vitamins, vitamin E is preferred, and the content is not particularly limited, but is 0.0001% by mass to 2.0% by mass, and 0.01% by mass to 1.0% by mass, based on the total amount of the composition. 0% by weight, preferably 0.1-0.5% by weight.

Other examples of such ingredients include glycyrrhetinic acids, such as glycyrrhetinic acid, stearyl glycyrrhetinate, glycyrrhizic acid and/or its salts (dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, etc.); mefenamic acid, allantoin, glycol salicylate, and Examples include anti-inflammatory agents such as pharmaceutically acceptable salts thereof. Among them, glycyrrhetinic acids and allantoin are preferred, and the content is not particularly limited, but glycyrrhetinic acids are 0.0001% by mass to 1.0% by mass, and 0.001% by mass to 0.5% by mass based on the total amount of the composition. %, 0.05 to 0.5 mass%, 0.1 mass% to 0.2 mass%, and allantoin is 0.0001 mass% to 1 mass%, 0.001 mass% to 0.5 mass%, 0.01% by mass to 0.3% by mass, preferably 0.05% by mass to 0.1% by mass. One type or a combination of two or more types of these drugs can also be used as appropriate. However, among the anti-inflammatory agents, methyl salicylate is preferably not contained in an amount of 3% by mass or more based on the entire composition, from the viewpoint of producing the cooling effect of the present invention and from the viewpoint of not generating unpleasant odor. Mass% or less, 2.0 mass% or less, 2 mass% or less, 1.5 mass% or less, 1 mass% or less, 0.5 mass% or less, 0.3 mass% or less, 0.1 mass% or less, 0 It is preferably .01% by mass or less, 0.001% by mass or less, or 0.0001% by mass or less, and it is even more preferred that it is substantially free.

(base, carrier, additives, etc.)
The composition of the present invention may contain, in addition to menthol and camphor, a base, a carrier, an additive, etc. from the viewpoint of improving the feeling of use and stability, etc., as long as they do not impede the effects of the present invention. .

Examples of bases, carriers, additives, etc. include surfactants, higher fatty acids, higher alcohols, hydrocarbons, oils and fats, waxes, ester oils, silicone oils, moisturizing ingredients, polyhydric alcohols, and thickeners. , a cooling agent other than menthol or camphor, an essential oil, a preservative or preservative, a pH adjuster, a chelating agent, and the like. Note that these components can be used alone or in combination of two or more.

The surfactant may be any of nonionic surfactants, cationic surfactants, anionic surfactants, amphoteric surfactants, and the like.

Examples of nonionic surfactants include sorbitan fatty acid esters (for example, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol pent-2-ethylhexylate, sorbitan tetra -2-ethylhexylate diglycerol sorbitan, 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 (for example, monolauryl Acid Polyoxyethylene (20) Sorbitan (Polysorbate 20), Polyoxyethylene Monostearate (20) Sorbitan (Polysorbate 60), Polyoxyethylene Monooleate (20) Sorbitan (Polysorbate 80), Polyoxyethylene Isostearate (20) ) sorbitan, etc.); glycerin derivatives (e.g., polyoxyethylene monococo fatty acid glyceryl, glycerin alkyl ether); polyoxyalkylene alkyl ethers (e.g., polyoxyethylene cetyl ether, etc.); silicone surfactants (e.g., polyoxyethylene cetyl ether, etc.); Examples include ethylene/methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, PEG-9 polydimethylsiloxyethyl dimethicone, etc.); alkyl glucoside;

Examples of the cationic surfactant include benzalkonium chloride and benzethonium chloride.

Examples of anionic surfactants include fatty acid soaps (e.g., sodium laurate, sodium palmitate, potassium laurate, potassium myristate, potassium palmitate, potassium stearate, etc.); alkyl sulfate salts (e.g., lauryl sodium sulfate, potassium lauryl sulfate, etc.); alkyl ether sulfate salts (e.g., POE-triethanolamine lauryl sulfate, POE-sodium lauryl sulfate, sodium laureth sulfate, etc.); N-acyl sarcosinate (e.g., sodium lauroyl sarcosine, etc.) ; Higher fatty acid amide sulfonates (e.g., sodium N-myristoyl-N-methyltaurate, sodium coconut oil fatty acid methyltaurate, sodium lauryl methyltaurate, etc.); phosphate ester salts (POE-sodium oleyl ether phosphate, POE-stearyl ether phosphoric acid, sodium lauryl phosphate, sodium polyoxyethylene lauryl ether phosphate, etc.); sulfosuccinates (e.g., sodium alkyl sulfosuccinate, sodium di-2-ethylhexyl sulfosuccinate, sodium polyoxyethylene sulfosuccinate, sodium lauryl polypropylene) sodium 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-acylglutamate (e.g., potassium lauroylglutamate, monosodium N-lauroylglutamate, disodium N-stearoylglutamate, monosodium N-myristoyl-L-glutamate, etc.); Higher fatty acid ester sulfate Ester salts (e.g., hydrogenated coconut fatty acid glycerin sodium sulfate, etc.); Sulfated oils (e.g., funnel oil, etc.); Ether carboxylates (e.g., polyoxyethylene alkyl ether carboxylic acid, polyoxyethylene alkyl allyl ether carboxylate, polyoxyethylene lauryl ether sodium acetate, etc.); α-olefin sulfonate; higher fatty acid ester sulfonate; secondary alcohol sulfate salt; higher fatty acid alkylolamide sulfate salt; sodium lauroyl monoethanolamide succinate; N- Examples include palmitoylaspartate ditriethanolamine; sodium caseinate, and the like.

Examples of the amphoteric surfactant include surfactants such as glycine type such as alkyldiaminoethylglycine, acetate betaine type such as lauryldimethylaminoacetic acid betaine, imidazoline type, and phospholipid such as lecithin.

In the present invention, as the surfactant, phospholipids are preferred, and lecithin is particularly preferred.

As the higher fatty acid, for example, saturated or unsaturated linear or branched fatty acids having 12 to 22 carbon atoms can be used, preferably lauric acid, myristic acid, palmitic acid, stearic acid or behenic acid. Linear saturated fatty acids (solid at room temperature) such as; unsaturated fatty acids (liquid at room temperature) such as oleic acid, linoleic acid, linolenic acid, palmitoleic acid, eicosapentaenoic acid, paxenoic acid or docosahexaenoic acid; or isostearic acid or Examples include branched fatty acids such as lanolin fatty acids, 12-hydroxystearic acid, and the like.

In the present invention, stearic acid is preferred as the higher fatty acid.

Examples of higher alcohols include higher alcohols having 12 to 22 carbon atoms and sterols. Preferably, straight chain saturated alcohols (solid at room temperature) such as lauryl alcohol, myristyl alcohol, cetanol, cetostearyl alcohol, stearyl alcohol, aracyl alcohol, behenyl alcohol; unsaturated alcohols such as oleyl alcohol and cerakyl alcohol (solid at room temperature) and hexyldecanol, isostearyl alcohol, octyldodecanol, decyltetradecanol, lanolin alcohol and the like.

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

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, and light Hydrocarbons such as liquid paraffin and light liquid paraffin may be mentioned.

Oils and fats include avocado oil, linseed oil, camellia oil, macadamia nut oil, corn oil, olive oil, safflower oil, kyonin oil, jojoba oil, grape seed oil, sunflower oil, almond oil, sasanqua oil, rapeseed oil, sesame oil, Castor oil, cocoa butter, coconut oil, hydrogenated 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, Examples include fats and oils such as hazelnut oil, shea butter, orange oil, and chamomile oil.

Waxes include candelilla wax, rice bran wax, cotton wax, carnauba wax, lanolin, lanolin fatty acid isopropyl, POE lanolin alcohol ether, POE lanolin alcohol acetate, lanolin fatty acid polyethylene glycol, POE hydrogenated lanolin alcohol ether, shellac wax, beeswax, and Japanese wax. Examples include waxes such as.

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, and laurine. hexyl acid, ethyl oleate, ethyl linoleate, isopropyl linoleate, cetyl caprylate, decyl oleate, oleyl oleate, isodecyl oleate, cetyl octoate, 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, isononanoic acid Isononyl, isotridecyl isononanoate, cholesteryl 12-hydroxystearate, cholesteryl stearate, cholesteryl oleate, phytosteryl macadamia nut fatty acid, phytosteryl oleate, inulin stearate, ethylene glycol di-2-ethylhexylate, cetyl 2-ethylhexanoate, mono N-alkyl glycol isostearate, neopentyl glycol dicaprate, glycerin di-2-heptylundecanoate, tri-2-ethylhexyl trimellitate, tridecyl trimellitate, trimethylolpropane tri-2-ethylhexylate, trimethylolpropane triisostearate , pentaerythritol tetra-2-ethylhexanoate, glyceryl tri-2-ethylhexanoate, trimethylolpropane triisostearate, cetyl 2-ethylhexanoate, glyceryl trimyristate, glyceryl tri(caprylic/capric acid), Tri(caprylic acid/capric acid/myristic acid/stearic acid) glyceryl, medium chain fatty acid triglyceride, castor oil fatty acid methyl ester, di(phytosteryl/octyldodecyl) lauroylglutamate, di(octyldodecyl/phytosteryl/behenyl) lauroylglutamate, lactic acid Cetyl, myristyl lactate, bisethoxydiglycol cyclohexane-1,4-dicarboxylate, lanolin acetate, ethyl acetate, butyl acetate, amyl acetate, triethyl citrate, dimer dilinoleic acid (phytosteryl/isostearyl/cetyl/stearyl/behenyl) , dimer dilinoleyl dimer dilinoleate, dipentaerythrityl tripolyhydroxystearate, tri(behenic acid/isostearic acid/eicosandioic acid) glyceryl, and the like.

Examples of silicone oils include methylpolysiloxane, methylphenylpolysiloxane, decamethyltetrasiloxane, methylcyclopentasiloxane, highly polymerized methylpolysiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, methylhydrogenpolysiloxane, and methyltrisiloxane. Siloxanes such as methicone, dimethiconol, dimethiconol crosspolymer, alkyl-modified silicones such as caprylyl methicone, amino-modified silicones such as aminopropyl dimethicone and amodimethicone, cross-linked methylpolysiloxane, cross-linked alkyl-modified silicones, amino-modified silicones, Ether-modified silicone, polyglycerin-modified silicone, cross-linked polyether-modified silicone, cross-linked alkyl polyether-modified silicone, silicone/alkyl chain co-modified polyether-modified silicone, silicone/alkyl chain co-modified polyglycerin-modified silicone, polyether-modified branched silicone Examples include silicone, polyglycerin-modified branched silicone, acrylic silicone, phenyl-modified silicone, and silicone oil such as silicone resin.

Examples of moisturizing ingredients include hyaluronic acid (including hydrolyzed hyaluronic acid, low-molecular-weight hyaluronic acid, etc.); salts of hyaluronic acid (such as sodium hyaluronate, zinc hyaluronate, low-molecular-weight zinc hyaluronate, etc.); hyaluronic acid derivatives (Acetylated hyaluronic acid or its salts (e.g., acetylated sodium hyaluronate, acetylated zinc hyaluronate, etc.), crosslinked hyaluronic acid derivatives (hyaluronic acid crosspolymer Na, etc.), carboxymethyl hyaluronate Na, unsaturated hyaluronic acid, its salts, hydrolyzed alkyl (C12-13) hyaluronate glyceryl, cationized hyaluronic acid derivatives (hydroxypropyltrimonium hyaluronate, etc., dimethylsilanol hyaluronate, etc.); chondroitin sulfate or its salts (sodium chondroitin sulfate, potassium chondroitin sulfate) , dermatan sulfate sodium, dermatan sulfate potassium, etc.); heparin analogues, amino acids and their derivatives such as alanine, serine, aspartic acid, glycine, proline, hydroxyproline, glucosamine, theanine, arginine; polyhydric alcohols; PPG-17 butes- 17, PPG-25 sorbitol, polyoxyalkylene alkyl glucoside, PEG/PPG/polybutylene glycol-8/5/3 glycerin, alkylene oxide such as polyoxyalkylene diglyceryl; glycosyl trehalose, trehalose; ceramide, glucosyl ceramide, cholesterol, Phytosterols, cholesterol derivatives, phytosterol derivatives; 2-methacryloyloxyethylphosphorylcholine/butyl methacrylate copolymer liquid, 2-methacryloyloxyphosphorylcholine-containing polymers such as polymethacryloyloxyethylphosphorylcholine; lactic acid, sodium lactate, sodium pyrrolidone carboxylate, NMF-derived components such as urea; collagen, elastin, keratin, chitin, chitosan, etc. and their hydrolysates; hydroxyethyl urea; , grapefruit, Jiaogulan, etc.).

Examples of polyhydric alcohols include low molecules having two or more hydroxy groups, such as glycerin, diglycerin, triglycerin, propylene glycol, dipropylene glycol, 1,3-butanediol, ethylene glycol, diethylene glycol, and isoprene glycol. , 1,3-butylene glycol, 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, decanediol, neopentyl glycol, sorbitol, xylitol, erythritol, mannitol can be mentioned.

Examples of the thickener include vinyl thickeners such as polyvinyl alcohol, polyvinylpyrrolidone, polyvinyl methyl ether, and carboxyvinyl polymer, methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, Cellulose thickeners such as carboxyethyl cellulose, hydrophobized hydroxypropyl methyl cellulose, 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 distearylammonium hectorite, sodium alginate, polyethylene glycol, trimethylammonium chloride hydroxypropyl guar gum, trimethylammoniochloride hydroxypropyl hydroxyethyl cellulose, (acrylic acid) Hydroxyethyl/acryloyl dimethyl taurine Na) copolymer, (acryloyl dimethyl taurate ammonium/vinyl pyrrolidone) copolymer, and the like.

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

Examples of essential oils include eucalyptus oil, bergamot oil, fennel oil, cinnamon oil, rose oil, turpentine oil, and lavender oil. However, from the viewpoint of more significantly enhancing 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, and more preferably 1.45% by mass or less. , more preferably 1.4% by mass or less, even more preferably 1.35% by mass or less, particularly preferably 1.3% by mass or less. When contained, 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, 1.0% by mass or more of the entire composition Particularly preferred.
Eucalyptus oil may not be included.

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

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 their salts, inorganic bases (potassium hydroxide, sodium hydroxide, etc.), and the like.

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

Although not limited, the external composition of the present invention is preferably a composition consisting only of natural raw materials or naturally derived raw materials. Here, natural raw materials have the same meaning as natural raw materials defined in ISO 16128, and refer to raw materials obtained from animals, plants, or minerals and not subjected to intentional chemical modification. Naturally derived raw materials have the same meaning as naturally derived raw materials defined in ISO 16128, and refer to raw materials obtained from animals, plants, or minerals and subjected to intentional chemical modification. Alternatively, the emulsified external composition of the present invention preferably has a natural origin index of 50 or more, 60 or more, 70 or more, 80 or more, 90 or more, more preferably 95 or more, taking water into consideration. Most preferably, it is 100.

[Production method]
The method for producing the pharmaceutical composition of the present invention is not particularly limited, and can be set as appropriate.

Specifically, a method may be mentioned in which each component is dissolved by heating if necessary, mixed, stirred while cooling in a water bath, and then allowed to stand at room temperature, but is not particularly limited to this method.

[Preparation form]
The composition of the present invention is mixed with, for example, a base or carrier commonly used for pharmaceuticals or quasi-drugs, and optionally additives to form an emulsified external composition. The emulsified external composition may be either an oil-in-water emulsion composition or a water-in-oil emulsion composition, but is preferably an oil-in-water emulsion composition.

Although the form of the composition of the present invention is not particularly limited, 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, and the like. These preparations can be manufactured according to the methods described in the 18th revised Japanese Pharmacopoeia General Rules for Preparations. Among these, cream agents are preferred from the viewpoints of less sticky feeling, good feeling on use, and achieving the effects of the present application.

[pH]
The pH of the composition of the present invention is usually pH 4.0 to 8.0, pH 4.5 to 7.5, pH 5.0 to 7.5, pH 5.5. ~7.5, pH 6.0 ~ 7.5 pH 6.5 ~ 7.5, pH 7.0 ~ 7.5 can be exemplified as preferred values. Note that this 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.

[container]
The composition of the present invention can be used by being stored in a container having an appropriately selected shape and material depending on the intended use and use. Specific examples of the container 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 stopper, a container with a hinge cap, a sponge head container, a roll-on container, and the like. Among these, tube containers are particularly preferred. By storing the composition in these containers, the composition of the present invention can be applied directly or indirectly to a desired affected area. The nozzle or sponge can be designed to be tapered or have a large diameter so that it can be applied to a narrow or wide area of the affected area. After applying the composition according to the present embodiment to the affected area, it is also possible to use it by spreading it with a nonwoven fabric, fingers, or the like.

In addition, the 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, Examples include polystyrene, glass, and metals (aluminum etc.). In addition, these materials may be treated with various coatings, combined by mixing, or laminated, taking into account strength, flexibility, weather resistance, or stability of ingredients. , can be used as a container material.

[Friction reduction method]
The present invention also reduces friction during application of the external composition by coexisting 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass to form an emulsion. Regarding methods of reducing "Reducing friction during application" leads to a reduction in the burden on the application site, especially the inflamed affected area, when the composition is applied to the skin. This reduction in friction further improves the medicinal efficacy and feeling of use, and makes it easier to spread the product by hand. Here, conditions such as content, ratio, and other components of each component are in accordance with the contents described in [Emulsified external composition].

[Method for enhancing cooling sensation]
The present invention also enhances the cooling sensation of the external composition by coexisting 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass to form an emulsion. Regarding the method. By increasing the cooling sensation, an itching suppressing effect is imparted. Therefore, the composition of the present invention is particularly effective as an itch suppressant even when the natural origin index is increased. Here, conditions such as content, ratio, and other components of each component are in accordance with the contents described in [Emulsified external composition].

[Application]
The emulsified external composition of the present invention is particularly effective for suppressing itching, redness, or itching, and is used depending on the symptoms and conditions. Although not limited to, the composition of the present invention can be used to treat, for example, senile skin pruritus, eczema (skin eczema including scalp eczema and hand eczema), dermatitis, itch, rash, hives, sores, heat rash, chilblains, It has an effect on itching caused by insect bites or dryness. The composition of the present invention also has an effect on sensations such as tingling or tingling, itching that spreads redness when scratched, and itching that repeatedly itch.

In view of its effects on the skin, the present invention is preferably used in products applied as external preparations for the skin (preparations for external skin). Application sites on the skin include the skin on the hands (palms, backs of hands, fingers), face, feet, head (scalp), neck, chest, armpits, back, waist, backs of elbows, and backs of knees. Applications for the hands, face, feet, and neck are particularly preferred, and applications for the hands and face are particularly preferred. For example, it can be suitably used as an anti-itch cream for pharmaceuticals or quasi-drugs. The pharmaceutical composition of the present invention can be divided into one to several doses per day depending on the intended use, and can be used in a known or commonly used manner and dosage.

Next, the present invention will be specifically explained with reference to examples, but the present invention is not limited to the following examples.

[Test Example 1. Friction test]
External compositions of Examples and Comparative Examples were prepared by conventional methods. The components and contents of each composition are shown in Table 1. Note that Examples 1 to 3 and Comparative Example 1 are emulsified compositions, Comparative Example 2 is a composition in the form of an ointment, and Examples 1 to 3 are oil-in-water emulsified compositions.
Friction tests were conducted on these compositions to examine whether there was a difference in the frictional resistance of the formulations depending on the concentration of menthol and camphor. A portable tactile system (TRIBOGEAR TYPE: 33, manufactured by Shinto Kagakusha) was used for the friction test. Strat-M Membrane (Size 25 mm Discs, Qty 60, Lot 0000162464) was fixed to the center of the device with double-sided tape. Thereafter, 5 μl 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 reciprocation/sec.

The friction coefficient ratio relative to Comparative Example 1 was calculated from the average value of the friction coefficient up to 120 seconds after the start of the test.
Friction coefficient ratio = average value of the friction coefficient for 120 seconds in each test example/average value of the friction coefficient for 120 seconds in Comparative Example 1.
The evaluation results are listed according to the calculated friction coefficient ratio values (Table 2).
0.86 or less: ◎
0.86-0.93:〇0.93 or more:×

As a result, it was confirmed that the emulsion composition of the example had a friction reducing effect compared to the comparative example.

[Test Example 2. Usability evaluation]
The emulsified external composition shown in Table 3 was prepared by a conventional method.
Example 1 and Comparative Example 3 were evaluated for usability.
Take the length of the first joint (1 FTU = approximately 0.5 g) from the tip of the index finger and apply it to the cheeks around the left and right cheekbones of four professional panelists who routinely prepare and evaluate the formulation. The applied composition was gently spread over an area of 3 cm x 3 cm to the extent that it was slightly shiny. The "cool feeling (refreshing feeling/soothing feeling)" immediately after application was evaluated relatively.

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

It was confirmed that compared to the composition of Comparative Example 3, the composition of Example 1 provided a stronger sense of cooling. Furthermore, the composition of Comparative Example 3 had an unpleasant odor similar to that of a compress, and did not have a good feeling of use.

The emulsified external composition shown in Table 5 was prepared by a conventional method. Note that Example 4 is an oil-in-water emulsion composition.
Example 3 and Example 4 were evaluated for usability.
Take the length of the first joint (1 FTU = approximately 0.5 g) from the tip of the index finger and apply it to the cheeks around the left and right cheekbones of two professional panelists who routinely prepare and evaluate the formulation. The applied composition was gently spread over an area of 3 cm x 3 cm to the extent that it was slightly shiny. The "cool feeling (refreshing feeling/soothing feeling)" immediately after application was evaluated relatively.

As a result, both Examples 3 and 4 had a good cooling sensation immediately after application, but the cooling sensation in Example 3 was felt to be stronger. In Example 4, there was a tendency for the refreshing feeling to be slightly weaker than in Example 3.

[Test Example 3. Itching suppression evaluation]
Contains 1.35% by mass of l-menthol and 9.6% by mass of dl-camphor, and also contains water, sugar squalane, stearyl alcohol, glycerin, cetanol, stearic acid, eucalyptus oil, behenyl alcohol, lavender oil, L-arginine, An emulsified composition of Example 5 containing turpentine and turpentine was prepared. Note that Example 5 is an oil-in-water emulsion composition. This emulsified composition was evaluated for its itch suppressing effect. Six adults with itching symptoms applied the preparation to the areas where they felt itchy, and the results were 1 each: immediate effect of suppressing itching caused by insect bites, sustained effect of suppressing itching caused by insect bites, and immediate effect of suppressing itching other than insect bites such as rashes. Rated on a scale of ~5. The closer the value is to 5, the more noticeable the effect is.

[evaluation]
1: I don't feel it at all 2: I feel it a little 3: I feel it 4: I feel it very much 5: I feel it very strongly

The results (individual scores and average value of the six people) are also shown in Table 6.

It was confirmed that the composition of Example 5 was effective in suppressing itching by applying it to a site with symptoms of itching.

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

Claims (7)

An emulsified external composition containing 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass of camphor, and the content of methyl salicylate is less than 3% by mass. The emulsified external composition according to claim 1, which is used for suppressing itch. The emulsified external composition according to claim 1 or 2 , further comprising 30% by mass or more of water. The emulsified external composition according to claim 1 or 2, which is in the form of a cream. The emulsified external composition according to claim 1 or 2 , which is housed in a tube container. By allowing 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass of camphor to coexist in the external composition to form an emulsion, the external composition can reduce friction during application. How to apply effects . By allowing 1.2% to 1.8% by mass of menthol and 8.6% to 11% by mass of camphor to coexist in a composition for external use to form an emulsion, the composition for external use has a cooling sensation enhancing effect. How to grant .