JP2003250829A - External remedy composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an external remedy composition which can give an excellent heat sense, has the high duration of the heat sense, and does not cause a smell, a stimulus or the like. <P>SOLUTION: The external remedy composition contains a heat sense component containing a 4-hydroxy-3-methoxyphenyl group (except a heat sensitive component containing a vanilylamide group), the heat sense component containing the vanilylamide group, and a chainlike nitrogen containing compound of at least one of a chainlike alkanol amine and chainlike carbonic acid. As a preferable embodiment, the chainlike compound is at least one kind selected from ethanolamine amine, propanolamine, tromethamine, EDTA, an amino acid, and an alkylbetaine. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an external preparation composition which is excellent in warm feeling and durability of warm feeling and does not cause unpleasant odor, skin irritation and the like.

[0002]

2. Description of the Related Art Conventionally, in order to impart a feeling of warmth to an external preparation for skin, a warming sensation-stimulating component such as pepper powder, pepper tincture, pepper extract, capsaicin, and nonyl acid vanillylamide has been used. However, although they have a warming effect, all of them have a problem in that they give rise to peculiar irritating odors, skin irritation, and the like and cause discomfort during use. With the development of technology in recent years, there has been a demand for an external preparation composition which has an excellent warming effect and which does not cause an unpleasant odor or skin irritation during use.

[0003]

SUMMARY OF THE INVENTION It is an object of the present invention to solve the various problems in the prior art and achieve the following objects. That is, an object of the present invention is to provide an external preparation composition capable of imparting an excellent warm feeling, having high durability of the warm feeling, and causing no unpleasant odor or irritation.

[0004]

Means for Solving the Problems As a result of earnest studies, the present inventor has alleviated unpleasant odors and alleviated irritation (irritating sensation, etc.) immediately after use such as application by the following means. The inventors have found that superior warmth and warmth sustainability can be obtained, and completed the present invention.

That is, the means for solving the above problems are as follows. <1> A warming component containing at least a 4-hydroxy-3-methoxyphenyl group (excluding a warming component containing a vanillylamide group), a warming component containing a vanillylamide group, a chain alkanolamine and a chain. A chain nitrogen-containing compound of at least one of the amino aminocarboxylic acids,
The external preparation composition is characterized by containing. <2> The external preparation composition according to <1>, wherein the chain nitrogen-containing compound is at least one selected from ethanolamine, propanolamine, tromethamine, EDTA (edetate disodium salt), amino acid, and alkyl betaine. It is a thing. <3> The external preparation composition according to <1> or <2>, further containing a compound having a local anesthetic action. <4> The external preparation composition according to any one of <1> to <3>, which is used as an external preparation for coating. <5> The external preparation composition according to any one of <1> to <3>, which is used for patches.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention will be described in detail below.
The external preparation composition of the present invention comprises a warming component containing a 4-hydroxy-3-methoxyphenyl group (excluding a warming component containing a vanillylamide group), a warming component containing a vanillylamide group, and a chain structure. At least one chain nitrogen-containing compound of alkanolamine and chain aminocarboxylic acid, containing, other components appropriately selected as necessary,
For example, it contains a compound having a local anesthetic effect.

[Warm Sensitive Component Containing 4-Hydroxy-3-Methoxyphenyl Group] The warm feeling component is not particularly limited as long as it contains a 4-hydroxy-3-methoxyphenyl group. For example, vanillyl. Examples thereof include butyl ether, ginger, ginger extract, ginger powder, ginger, ginger extract, ginger extract, gingerol, and zingerone. These may be used alone or in combination of two or more.

The content of the warming sensation component in the external preparation composition is preferably 0.001 to 3% by mass,
0.005-1 mass% is more preferable. The content is
If it is less than 0.001 mass%, the warming effect may not be sufficient, while if it exceeds 3 mass%, the warming effect commensurate with the blending amount may not be obtained, which may be economically disadvantageous. is there.

[Warming ingredient containing a vanillyl amide group] The warming ingredient is not particularly limited as long as it contains a vanillyl amide group, and examples thereof include nonyl acid vanillyl amide, capsaicin, capsicum, capsicum extract, and pepper powder. Can be mentioned. These may be used alone or in combination of two or more.

The content of the warming sensation component in the external preparation composition is preferably 0.001 to 3% by mass,
0.005-1 mass% is more preferable. The content is
If it is less than 0.001 mass%, the warming effect may not be sufficient, while if it exceeds 3 mass%, the warming effect commensurate with the blending amount may not be obtained, which may be economically disadvantageous. is there.

In the present invention, by using the above-mentioned two kinds of warming sensation components in combination, the warming sensation effect and the unpleasant odor suppressing effect which are remarkably superior to the case where these are used alone in the same amount. Will be provided.

[Chain nitrogen-containing compound] The chain nitrogen-containing compound is at least one of a chain alkanolamine and a chain aminocarboxylic acid.

The chain alkanolamine is not particularly limited, but examples thereof include alkanolamines such as monoethanolamine, diethanolamine, triethanolamine, diisopropanolamine, and tromethamine. These may be used alone or in combination of two or more.

The chain aminocarboxylic acid is not particularly limited, but for example, EDTA (edetic acid disodium salt), amino acid, glycine, alanine, trimethylglycine, tryptophan, phenylalanine, histidine, arginine, aspartic acid, and In addition to glutamic acid and the like, various amphoteric surfactants and the like can be mentioned. Examples of the amphoteric surfactant include alkyl betaines such as lauryl dimethyl betaine, alkyl amide betaines such as coconut oil fatty acid amide propyl betaine, alkyl sulfobetaines, and imidazoline. They are,
They may be used alone or in combination of two or more.

The content of the chain nitrogen-containing compound in the external preparation composition is preferably 0.01 to 20% by mass, more preferably 0.05 to 10% by mass. If the content is less than 0.01% by mass, irritation may occur during use.

[Compound Having Local Anesthetic Action] The compound having a local anesthetic action is not particularly limited, and examples thereof include ethyl aminobenzoate, tetracaine hydrochloride, procaine hydrochloride, dibucaine hydrochloride, lidocaine hydrochloride and oxybu hydrochloride. Local anesthetics such as procaine, T-caine, bupipacaine hydrochloride, lidocaine and its salts, dibucaine and its salts, diethylaminoethyl parabutylaminobenzoate hydrochloride, salicylic acid, salicylates, methyl salicylate,
Salicylic acids such as glycol salicylate, eugenol, pinene, cazinene, spilanthol, menthol,
Examples include borneol and camphor. These are 1
They may be used alone or in combination of two or more.
In the present invention, the warming component having the 4-hydroxy-3-methoxyphenyl group may cause an uncomfortable feeling such as itching and tingling in the skin, and in order to suppress this, the local anesthetic action is exerted. It is preferable to contain a compound.

[Other Components] As the other components, terpenoid compounds and the like are particularly preferable from the viewpoint of further improving the warming effect. Among the terpenoid compounds, monoterpenes, diterpenes, menthol, camphor and borneol are particularly preferable. , And geraniol are preferred. These may be used alone or in combination of two or more.

The content of the terpenoid compound in the external preparation composition is 1 / 0.1 to 1/0 in the content ratio of the warming sensation component and the terpenoid compound (mass ratio: warming sensation component / terpenoid compound). .0001 is preferable. When the content of the terpenoid compound is within this numerical range, the warming sensation-enhancing effect is particularly high, which is preferable.

In the external preparation composition of the present invention, in addition to the terpenoid compound, physiologically active ingredients, aliphatic alcohols and / or fatty acids, water, solubilizing agents, surfactants, polymer compounds, and patch bases. , Oily ingredients, powders, pH adjusters, chelating agents, dyes, fragrances, preservatives and the like.

The physiologically active ingredient is not particularly limited, but examples thereof include anti-inflammatory analgesics, anti-inflammatory agents, keratolytic agents, antipruritic agents, antihistamine agents, bactericidal agents, sulfa agents, steroid agents, antibacterial agents, antifungal agents, Examples thereof include painkillers, moisturizers, whitening agents, vitamins, mucopolysaccharides, protective agents, and ingredients effective for the treatment and / or care of skin diseases such as plant-derived ingredients.

Examples of the anti-inflammatory agent include tolfenamic acid, mefenamic acid, flufenamic acid, allantoin, guaiazulene, dipotassium glycyrrhizinate, glycyrrhetinic acid, stearyl glycyrrhetinate, salicylic acid, methyl salicylate, glycol salicylate, sodium salicylate, aspirin, sazapyrine. , Alclofenac, suprofen, ibuprofen, naproxen, flurbiprofen, ketoprofen, fenbufen, indomethacin, methiazic acid, protidic acid,
Examples thereof include sulindac, pranoprofen, fenthiazac, diflunisal, thiaprofenic acid, oxaprozin, diclofenac sodium, oxyphenbutazone, piroxicam, felbinac, bufexamac, glycol salicylate, phenacetin, phenylbutazone, and tolmetin sodium. These may be used alone or in combination of two or more.

Examples of the antipruritic agent include crotamiton, isothipendyl hydrochloride, diphenylpyraline hydrochloride, diphenhydramine and salts thereof, triperenamine hydrochloride, chlorpheniramine and salts thereof and the like. These may be used alone or in combination of two or more.

Examples of the bactericide include acrinol, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, chlorhexidine hydrochloride, benzyl alcohol, povidone iodine, phenol, resorcin, hydrogen peroxide, mercury chrome, iodine tincture, and sulfur. To be These may be used alone or in combination of two or more. Examples of the sulfa drug include sulfadiazine, sulfisomidine, homosulfamine and the like. They are,
They may be used alone or in combination of two or more. Examples of the steroid agents include dexamethasone acetate, hydrocortisone acetate, prednisolone acetate, dexamethasone, prednisolone and the like. These may be used alone or in combination of two or more. Examples of the antifungal agent include miconazole nitrate, econazole nitrate, clotrimazole, pyrrolnitrin and the like. These may be used alone or in combination of two or more. Examples of the analgesic include acetaminophen and etenzamid. These may be used alone or in combination of two or more.

Examples of the moisturizers include urea and polyhydric alcohols. Preferable examples of the polyhydric alcohol include glycerins, alkylene glycols, dialkylene glycols, polyalkylene glycols and sugar alcohols. The glycerin, glycerin, diglycerin, triglycerin,
Examples of the alkylene glycols include polyglycerin, and the like, 1,3-butanediol, ethylene glycol, propylene glycol, butylene glycol,
Examples include isoprene glycol and amylene glycol, and examples of the dialkylene glycols include diethylene glycol, dibutylene glycol, dipropylene glycol, and diethylene glycol monoalkyl ether, and examples of the polyalkylene glycol include polyethylene glycol and polypropylene glycol. , Polyethylene glycol, polypropylene glycol and the like, and examples of the sugar alcohols include sucrose, lactose, maltose, mannitol, erythritol, xylitol, glucose and sorbitol. These may be used alone or in combination of two or more.

Examples of the whitening agents include peroxides such as zinc peroxide and magnesium peroxide, ascorbic acid, vitamin Cs, ellagic acid, kojic acid, tocopherol, and tocopherol acetate. These may be used alone or in combination of two or more. Examples of the vitamins include pyridoxine hydrochloride, palmitic acid, retinol, vitamin A and the like. These may be used alone or in combination of two or more. Examples of the mucopolysaccharide include sodium chondroitin sulfate, heparin and heparin-like substances. These may be used alone or in combination of two or more. Examples of the protective agent include calamine and zinc oxide. These may be used alone or in combination of two or more. Examples of the plant-derived component include choleus, arnica, melissa, senburi, cinnamon syrup, clove, spearmint, cardamom, eucalyptus, touki, peony, bellflower, hawthorn, sausage, rosemary, hawthorn, lavender, garlic, safflower, fennel, Korean carrot. , Ginseng, carrot, pearl oyster, buckthorn, horse chestnut, Chinese mackerel, zelkova, button pie,
Examples thereof include chamomile, salamander, seaweed, and the like, and also include powders of these plants, extracts such as extracts and essential oils, and the like. These may be used alone or in combination of two or more.

Among these, suprofen, ketoprofen, glycyrrhetinic acid, indomethacin, flurbiprofen, felbinac and the like are particularly preferable.

The content of the physiologically active ingredient in the external preparation composition is preferably 0.01 to 30% by mass, more preferably 0.01 to 20% by mass, and 0.1 to 1% by mass.
0% by weight is particularly preferred.

Examples of the aliphatic alcohol include:
Lauryl alcohol, cetyl alcohol, cetostearyl alcohol, stearyl alcohol, oleyl alcohol, behenyl alcohol, eicosonyl alcohol,
Examples thereof include linear fatty alcohols such as elaidyl alcohol and linoleyl alcohol, cyclic fatty alcohols such as cholesterol, dihydrocholesterol, phytosterol and lanolin alcohol, synthetic fatty alcohols such as octyldodecanol, hexyldecanol, and isostearyl alcohol. These may be used alone or in combination of two or more.

Examples of the fatty acids include saturated fatty acids such as lauric acid, myristic acid, palmitic acid and stearic acid, and unsaturated fatty acids such as oleic acid, linoleic acid, linolenic acid, arachidonic acid and undecylenic acid. . These may be used alone or in combination of two or more.

The content of the aliphatic alcohol and the fatty acid in the external preparation composition is 0.05 to 50.
Mass% is preferable, and 0.1-30 mass% is more preferable.

Examples of the water include purified water and ordinary water. The content of the water in the external preparation composition is preferably 1 to 90% by mass, more preferably 10 to 60% by mass.

The above-mentioned solubilizer is particularly preferably added when the poorly water-soluble drug is added. Examples of the solubilizing agent include alcohols having 1 to 4 carbon atoms, specifically, methanol, ethanol, various denatured alcohols (methanol, geraniol, octaacetylsucrose, 10 mass% desodium benzoate denatured alcohol solution, etc.). Alcohol), propanol, isopropanol, butanol, isobutanol and the like, preferably ethanol, octaacetyl sucrose modified alcohol, isopropanol and the like. These may be used alone or in combination of two or more.

The content of the solubilizer in the external preparation composition is preferably 5 to 80% by mass.
-70 mass% is more preferable, and 20-60 mass% is still more preferable. If the content exceeds 80% by mass, skin irritation may occur.

Examples of the surfactants include anionic surfactants, cationic surfactants, nonionic surfactants, and amphoteric surfactants. These are 1
They may be used alone or in combination of two or more.
Among these, nonionic surfactants are particularly preferable.

Examples of the nonionic surfactant include ether compounds such as polyoxyethylene alkyl ether and polyoxyethylene polypropylene alkyl ether, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, glycerin fatty acid ester, and polyglycerin fatty acid ester. , Ester compounds such as polyoxyethylene glycerin fatty acid ester, polyethylene glycol fatty acid ester and sucrose fatty acid ester, polyoxyethylene castor oil / hardened castor oil, polyoxyethylene polyoxypropylene polymer and the like. These may be used alone,
You may use 2 or more types together.

Examples of the anionic surfactants include saturated higher fatty acid salts, alkyl sulfonates, alkyl ether sulfonates, and alkyl ether sulfonates. These may be used alone or in combination of two or more.

Examples of the cationic surfactants include quaternary ammonium salts such as trimethylalkylammonium chloride and alkylamine salts such as dimethylalkylamine hydrochloride. These may be used alone or in combination of two or more.

The content of the surfactant in the external preparation composition is preferably 0.01 to 10% by mass, more preferably 0.05 to 5% by mass.

Examples of the polymer compound include cellulose derivatives such as hydroxypropyl cellulose, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, carmellose, croscarmellose and methyl cellulose, crystalline cellulose, methyl vinyl ether-
Maleic anhydride copolymer Na salt crosslinked product, modified starch such as partially pregelatinized starch, corn starch, polyvinyl alcohol, polyvinylpyrrolidone, crospovidone, polyethylene glycol, xanthan gum, carrageenan, sodium alginate, gum arabic, tragacanth gum,
Karaya gum, guar gum, locust bean gum, pullulan, gelatin, carboxyvinyl polymer, (meth)
Acrylic acid / (meth) acrylic acid ester copolymer, N
- methacryloyl ethyl -N, N-dimethylammonium-.alpha.-N-methyl carboxy betaine polymers, acrylic acid-meth A acrylic acid alkyl copolymer, polyacrylic acid, polyacrylic acid salt crosslinked product, sodium polyacrylate, Acrylic acid / starch graft polymer and / or salt thereof, starch / polyacrylonitrile copolymer,
Isobutylene / maleic anhydride copolymer and / or salt thereof, N-vinylacetamide copolymer, crosslinked polyvinylpyrrolidone, crosslinked polyalkylene oxide, alginic acid, croscarmellose sodium, polyacrylamide, sodium carboxymethylcellulose, polyvinyl acetate , Alkyl vinyl ether / maleic anhydride copolymer, poly N-vinyl acetamide, polymethoxy polyethylene glycol (meth) acrylate, polyphenoxy polyethylene glycol (meth) acrylate, polyhydroxyethyl (meth) acrylate, polyhydroxypropyl (meth) acrylate , Mixtures thereof, and the like. These may be a cross-linked product in which a part thereof is cross-linked. These may be used alone or in combination of two or more.

The molecular weight of the polymer compound is preferably 10,000 to 10,000,000, particularly preferably 100,000 to 5,000,000. When the molecular weight of the polymer compound is within the above range, good gel forming property can be obtained. The content of the polymer compound in the external preparation composition,
It is appropriately selected depending on the set viscosity, but is 0.01 to 5% by mass.
Is preferable, and 0.05-2 mass% is more preferable.

The patch base is preferably an aqueous adhesive base, more preferably an aqueous adhesive base obtained by crosslinking a water-soluble or swelling polymer compound with a crosslinking agent. The aqueous pressure-sensitive adhesive base contains a water-soluble or swellable polymer compound, a cross-linking agent, a cross-linking modifier, and the like. The water-soluble or swellable polymer compound can be preferably selected from the polymer compounds, and among these, polyacrylic acid, polyacrylate cross-linked product, sodium polyacrylate, hydroxyethyl cellulose. , Hydroxypropyl cellulose, methyl cellulose, carboxyl vinyl polymer,
Crystalline cellulose, alginic acid, gelatin and polyvinylpyrrolidone are particularly preferable. These may be used alone or in combination of two or more. Preferred embodiments of the polymer compound used as the water-soluble or swellable polymer compound of the patch base are described below.

The polyacrylic acid may be unneutralized or partially neutralized, and the partially neutralized polyacrylic acid having a neutralization ratio of less than 20 mol% is dissolved in a polyhydric alcohol. It is preferable because it is easy to do, and non-neutralized polyacrylic acid is more preferable. The polyvinyl acetate may be a copolymer containing a vinyl acetate monomer as a main component, for example,
Vinyl acetate / crotonic acid copolymer, vinyl acetate / itaconic acid copolymer and the like are preferable. Preferable examples of the polyvinyl alcohol include completely or partially saponified polyvinyl acetate. The alkyl vinyl ether / maleic anhydride copolymer may be an alkyl vinyl ether / maleic anhydride copolymer and a hydrolyzate thereof, a neutralized product of the hydrolyzate, or a half ester, for example, methyl vinyl ether / anhydrous. A maleic acid copolymer is preferred. In the polymethoxy polyethylene glycol (meth) acrylate and the polyphenoxy polyethylene glycol (meth) acrylate, the ethylene glycol addition mole number (n) of the polyethylene glycol side chain contained therein is, for example, n = 2 to 50. Is preferable, and it is more preferable that n = 2 to 23. The polymethoxy polyethylene glycol (meth) acrylate and the polyphenoxy polyethylene glycol (meth) acrylate may be, for example, a copolymer with (meth) acrylic acid alkyl ester or the like.

The content of the water-soluble or swellable polymer in the external composition is 0.01 to 40% by mass.
Is preferable, and 0.1-30 mass% is more preferable. Suitable examples of the cross-linking agent include aluminum and polyvalent metal salts containing magnesium, and examples of the polyvalent metal salts include magnesium aluminate silicate, magnesium hydroxide aluminate, and magnesium aluminometasilicate, Examples thereof include synthetic hydrotalcite and dihydroxyaluminum aminoacetate. These may be used alone or in combination of two or more.

The content of the cross-linking agent in the patch base is appropriately selected depending on the type and the polymer compound to be incorporated, but is preferably 0.005 to 3% by mass, and 0.03 to 1 Mass% is more preferable. If the content of the crosslinking agent is less than 0.005 mass%, sufficient gel strength cannot be obtained, and if it exceeds 3 mass%, it may be difficult to adjust the curing rate. As the crosslinking regulator,
For example, citric acid, malic acid, tartaric acid, disodium edetate and the like can be mentioned. These may be used alone or in combination of two or more. The content of the crosslinking regulator in the patch base is 0.00
1 to 10 mass% is preferable. When the content of the cross-linking regulator is within the above range, a good cross-linking speed can be adjusted.

Examples of the oily component include hydrocarbons such as squalane, vegetable squalane, liquid paraffin, petrolatum and microcrystalline wax, and silicone oils such as methylpolysiloxane, methylphenylpolysilochine and dimethylcyclopolysiloxane. Waxes such as beeswax, octyldodecyl oleate, oleyl oleate, cetyl octanoate, isopropyl oleate, glycerin monooleate, dioleate, octyldodecyl oleate, isopropyl palmitate, isopropyl myristate, myristyl myristate. , Fatty acid esters such as cetyl octanoate, diisopropyl adipate and 2-hexyldecyl isostearate, metals such as aluminum stearate and magnesium stearate鹸類, and the like. They are,
They may be used alone or in combination of two or more.

The content of the oily component in the external preparation composition is preferably 0.05 to 50% by mass,
0.1-30 mass% is more preferable.

Examples of the powder include inorganic powder and organic powder. Examples of the inorganic powder include talc, kaolin, bentonite, layered silicate minerals such as magnesium aluminum silicate, titanium oxide, and zinc oxide. These may be used alone or in combination of two or more. Examples of the organic powder include spherical powder of nylon, silica, polymethylmethacrylate, etc., polyethylene beads, cellulose powder, starch and the like. These may be used alone or in combination of two or more.

As the pH adjuster, the liquidity of the external preparation composition is easily adjusted to pH 3 to 8 (preferably pH 4 to 4).
Those which can be adjusted to 7) are particularly preferable. Examples of the pH adjusting agent include inorganic acids such as hydrochloric acid, phosphoric acid and boric acid, organic acids such as lactic acid, tartaric acid and citric acid, sodium hydroxide,
Examples thereof include phosphates such as potassium hydroxide, potassium hydrogen phosphate, sodium hydrogen phosphate, and organic salts such as sodium citrate and sodium lactate. These may be used alone or in combination of two or more.

Examples of the chelating agent include pyrophosphate, hexametaphosphate, gluconate and the like. These may be used alone or in combination of two or more.

Examples of the dye include acid dyes, basic dyes, and oxidation dyes. These are 1
They may be used alone or in combination of two or more.

Examples of the flavor include vegetable flavors such as peppermint oil, spearmint oil, jasmine oil, lemon oil, orange oil, lime oil, mandarin oil, rose oil, and rosemary oil, monoterpenes, diterpenes. , Synthetic fragrances such as sesquiterpenes, and the like. Specific examples thereof include geraniol, linalool, citronellol, nerol, limonene, pinene, camphene, citral, citronellal, cineol, curcumene, hinokinoic acid, hinokiol, and phytol.
These may be used alone or in combination of two or more.

Examples of the preservatives include dibutylhydroxytoluene, benzoic acids, parabens, benzalkonium chloride, benzethonium chloride, sorbic acid and salts thereof, boric acid, borax, salicylic acid and salts thereof, and the like. These may be used alone, or 2
You may use together 1 or more types. Among these, dibutylhydroxytoluene, citric acid and salts thereof are preferable.

The content of the preservative in the external preparation composition is preferably 0.01 to 50% by mass,
0.02 to 30 mass% is more preferable, and 0.05 to 10
Mass% is more preferable.

<Container for Injecting and Preserving External Agent Composition> The container for injecting and storing the external agent composition of the present invention is not particularly limited, but its material is, for example, polyethylene terephthalate (PET). , Polypropylene (PP), polyethylene (high density polyethylene: HDP
E, low-density polyethylene (LDPE), glass, polystyrene, EVAL, aluminum, and metals such as a laminate of aluminum and resin. These materials are
They may be used alone or in combination of two or more. Examples of the shape of the container include various shapes such as tubes, bottles, cans, and jars.

<Dosage form of external preparation composition> The dosage form of the external preparation composition of the present invention is not particularly limited.
Lotions, emulsions, gels, gel lotions, ointments, creams, aerosols and the like can be mentioned. Also, the external preparation composition of the present invention may be applied to various supports (for example, polyethylene terephthalate (PET) non-woven fabric, polyethylene (PE) / polyethylene terephthalate (PET) non-woven fabric, etc.) and used as a patch. preferable.

<Use of external preparation composition> The external preparation composition of the present invention is widely and suitably used in various fields such as pharmaceuticals, quasi drugs and cosmetics.

[0057]

EXAMPLES The present invention will be described in more detail below with reference to Examples and Comparative Examples, but the present invention is not limited to the following Examples.

(Examples 1 to 5 and Comparative Examples 1 to 5) Known by each formulation described in Table 1 (however, each component composition in the table is expressed in "g" unit). The external preparation composition (lotion) was prepared by the method for preparing. The liquidity (pH) of the obtained external preparation composition was adjusted within the range of 3 to 8 and filled in polypropylene containers.

<Evaluation> Each of the obtained external preparation compositions (lotions) was evaluated as follows. The results are shown in Table 1.

<< Evaluation of Thermal Sensation >> Predetermined environment (22 ° C., 50
% RH), each of the obtained external preparation compositions was
An appropriate amount was applied to the shoulder of a well-known panel and the warmth was evaluated according to the following evaluation criteria.

-Evaluation Criteria for Warm Feeling- 4 points: Feels very warm 3 points: I feel a strong sense of warmth 2 points: Feeling warmth 1 point: Feels a little warm 0 points: No warm feeling

In the evaluation of warmth, "strength of warmth"
Indicates the average score of the evaluation points of each panel after applying the sample, and shows the evaluation score with the largest number among the evaluation scores of all the panelists.
In addition, "persistence of warmth" means that from the beginning of application, over time,
When the "strength of warmth" is evaluated, the evaluation point is 2
It indicates the time (in minutes) until it becomes less than the point (the degree of feeling warmth), and if it is practically 15 minutes or more, it can be said that the durability is high.

<< Evaluation of Smell >> In the above-mentioned “evaluation of warm feeling”, the 100 panelists evaluated the smell based on whether or not the smell was noticed when the external preparation composition (lotion) was applied. . In the evaluation, the number of panelists who were worried about the odor was expressed as a percentage (100) of 100. In the evaluation, the smaller the evaluation value, the less the odor.
If it is 5% or less, there is no problem in practical use.

<< Evaluation of Skin Irritation >> In the above “Evaluation of warm feeling”, the 100 panelists evaluated the presence or absence of tingling sensation on the skin when the external preparation composition (lotion) was applied. . In the evaluation, the ratio of the number of panelists who felt tingling out of 100 (%)
Expressed as In the evaluation, the smaller the evaluation value, the less the tingling sensation during application and the lower the irritation. 5
If it is less than or equal to%, there is no problem in practical use.

[0065]

[Table 1]

(Example 6, Comparative Examples 6 to 8) Known preparations were made according to each formulation shown in Table 2 (however, each component composition in the table is expressed in "g" unit). The external preparation composition (cream) was prepared by the method. The liquidity (pH) of the obtained external preparation composition was adjusted to fall within the range of 3 to 8 and filled in an aluminum laminate tube container. Then, each evaluation was performed like Example 1-5 and Comparative Examples 1-5. The results are shown in Table 2.

[0067]

[Table 2]

Example 7 Each formulation described in Table 3 (however,
All component compositions in the table are expressed in "g" units. ), The external preparation composition (gel) by a known preparation method.
Was prepared. The liquidity (pH) of the obtained external preparation composition was adjusted within the range of 3 to 8 and filled in an aluminum laminate tube container. Then, each evaluation was performed like Example 1-5 and Comparative Examples 1-5. The results are shown in Table 3.
Shown in.

[0069]

[Table 3]

(Examples 8 to 15) According to each formulation described in Tables 4 to 5 (however, each component composition in the table is expressed in "g" unit) by a known preparation method. An external preparation composition was prepared. In addition, the liquidity (p
All of H) were adjusted to 5. Then, each external preparation composition,
Warmness, odor, and skin when the patch was prepared by applying on the support described in Tables 4 to 5 and applying the patch in the same manner as in Examples 1 to 5 and Comparative Examples 1 to 5. Each irritation was evaluated. The results are shown in Tables 4-5.

[0071]

[Table 4]

[0072]

[Table 5]

From the above, it was confirmed that in Examples 1 to 15, an excellent warm feeling was imparted, the warm feeling was highly durable, and odor and irritation were less likely to occur. It was also confirmed that the cream had a slightly inferior warming effect as compared to the lotion, but had low irritation. Further, it was confirmed that the gel agent has a longer lasting warmth than the lotion. Further, it was confirmed that the patch has a longer warm feeling than the lotion, but has a slightly poorer warm feeling than the gel.

(Examples 16 to 26, Comparative Examples 8 to 9) Table 6
The external preparation composition (patch) was prepared by a known preparation method according to each formulation described in (1) to (7) (however, each component composition in the table is expressed in “mass%” unit). . The liquidity (pH) of the obtained external preparation composition (patch) was adjusted to 3.5 to 5 in all.

<Evaluation> Each of the obtained external preparation compositions (patches) was evaluated as follows. The results are shown in Tables 6 to 7.
Shown in.

<< Evaluation of skin discomfort >> Predetermined environment (22
Each of the obtained external preparation compositions (patches) was applied to the shoulders of 100 panelists at 50 ° C. and 50% RH), and the discomfort to the skin (itchiness, tingling sensation) was evaluated according to the following evaluation criteria. . -Evaluation criteria for skin discomfort-4 points: Very uncomfortable 3 points: Very uncomfortable 2 points: Somewhat uncomfortable 1 point: Somewhat uncomfortable 0 points: No uncomfortable feeling <<< Warm feeling evaluation> In the "evaluation of skin discomfort", the 100 panelists evaluated the warmth on the basis of the time (minutes) when they felt the warmth when they applied the external preparation composition (patch). In the evaluation, the average value of the time (minutes) when the panelist began to feel warmth was determined and used as the evaluation value.
It should be noted that the smaller the evaluation value, the quicker the feeling of warmth starts.

[0077]

[Table 6]

[0078]

[Table 7]

From the above, it was confirmed that in Examples 16 to 26, excellent warm feeling was imparted, the immediate effect of the warm feeling was high, and the skin did not feel uncomfortable.

[0080]

Industrial Applicability According to the present invention, it is possible to provide an external preparation composition capable of imparting an excellent warmth sensation, having high durability of the warmth sensation, and causing no odor or irritation.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61P 23/02 A61P 23/02 29/00 29/00 F term (reference) 4C076 AA11 AA72 BB31 DD09 DD23 DD28 DD30 DD34 DD37 DD38 DD39 DD41 DD43 DD44 DD49 DD50 DD59 EE09 EE32 4C099 AA01 CA19 EA08 GA01 JA03 TA04

Claims (5)

[Claims] 1. A warming component containing at least a 4-hydroxy-3-methoxyphenyl group (excluding a warming component containing a vanillylamide group), a warming component containing a vanillylamide group, and a chain alkanolamine. And a chain nitrogen-containing compound of at least one of a chain aminocarboxylic acid, and an external preparation composition comprising: 2. The external preparation according to claim 1, wherein the chain nitrogen-containing compound is at least one selected from ethanolamine, propanolamine, tromethamine, EDTA (disodium edetate), amino acid, and alkylbetaine. Composition. 3. The external preparation composition according to claim 1, further comprising a compound having a local anesthetic action. 4. The method according to any one of claims 1 to 3, which is used as an external preparation for coating.
The external preparation composition according to any one of 1. 5. The external preparation composition according to any one of claims 1 to 3, which is used as a patch.