JP2003206239A - Warming composition and external agent composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a warming composition applying excellent warm feeling even in the form of an external application agent such as lotion and cream and free from stimulation on the skin. <P>SOLUTION: The warming composition contains (A) zingerone, (B) a fatty acid ester and (C) a terpenoid compound. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a warming composition and an external preparation composition which are mild and have excellent warmth feeling.

[0002]

2. Description of the Related Art External skin preparations such as lotions, creams and patches are blended with a cooling stimulant which gives a refreshing feeling and a warming stimulant which gives a warm feeling in order to improve the feeling of use. Sometimes. As a warming stimulant, capsicum,
Capsaicin, a warming sensation ingredient in capsicum, and vanillylamide nonylate are widely used as external preparations. However, even if these components are blended alone in an external preparation, there are problems such as insufficient heat sensation, irritating odor, and skin irritation such as itchiness, redness and tingling sensation. Zingerone is a compound that causes less skin irritation among warming sensation components, but has a weak warming sensation, and satisfactory thermal sensation could not be obtained even if it was added alone to an external preparation. As a technique for imparting a warming sensation using zingerone, JP-A-60-13710 discloses a mild sensation warming patch containing a warming stimulant and a ginger solvent extract. With respect to the above-mentioned warming composition, in the case of a poultice type preparation, a good warm feeling is obtained because the preparation is in close contact with the skin during use. However, when this warming technique is applied to a lotion or cream which is applied to the skin and then exposed to the air, the warming feeling is not satisfactory. Therefore, there has been a demand for a warm sensation external preparation that provides excellent thermal sensation even in the application type external preparation and that does not cause skin irritation.

[0003]

DISCLOSURE OF THE INVENTION The present invention provides a warming composition having an excellent warming sensation even in an application type external preparation such as lotion or cream, and having no skin irritation. The present invention also provides an external preparation composition containing the warming composition.

[0004]

DISCLOSURE OF THE INVENTION As a result of studies, the present inventors have found that a composition containing zingerone and a fatty acid ester dramatically improves the thermal sensation. Further, they have found that the itching caused by the above composition is suppressed by adding terpenoids to this, and completed the present invention.

Accordingly, the present invention is a warming composition comprising <1> (A) zingerone, (B) fatty acid ester, and (C) terpenoid compound. <2> An external preparation composition containing (A) zingerone, (B) fatty acid ester, and (C) terpenoid compound. <3> The external preparation composition according to <2>, which is a coating type external preparation. I will provide a. The present invention will be described in detail below.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The zingerone used in the present invention is
A purified product may be used, or a plant extract containing zingerone may be used. Examples of plants containing zingerone include ginger, ginger and other ginger plants.

The content of zingerone in the composition is preferably 0.001 to 3% by mass. A more preferable content is 0.005 to 1% by mass, and particularly preferably 0.005.
Is 0.5% by mass. Within this range, a skin warming external preparation that effectively suppresses skin irritation and has a good odor can be obtained.

The fatty acid ester in the present invention has an effect as a thermal sensation enhancer for zingerone. The fatty acid ester used is a medium or long chain fatty acid ester,
An ester of a branched or straight chain fatty acid having 7 to 20 carbon atoms and a branched or straight chain alcohol having 2 to 20 carbon atoms, cholesterol or glycerin, preferably a branched or straight chain alcohol having 3 to 16 carbon atoms is preferable.

Specifically, butyl myristate, butyl stearate, cetyl isooctanoate (cetyl 2-ethylhexanoate), diethyl sebacate, diisopropyl adipate, diisopropyl sebacate, pivalic acid 2
-Octyldodecyl, ethyl oleate, 2-hexyldecyl isostearate, 2-hexyldecyl myristate, octyl palmitate, isopropyl isostearate, isopropyl myristate, isopropyl palmitate, isostearyl palmitate, myristyl myristate, palmitin. Cetyl acid, octyldodecyl myristate, ethyl linoleate, isopropyl linoleate, cholesteryl stearate, phytosteryl isostearate, propylene glycol dicaprate, pentaerythritol tetra-2-ethylhexanoate,
Propylene glycol monocaprate, propylene glycol dicaprylate, trimethylolpropane trioctanoate, trimethylolpropane triisostearate, glyceryl tri-2-ethylhexanoate, glyceryl tri (capryl-caprate), batyl monostearate, batyl isostearate can give. Among the above, preferred fatty acid ester is diisopropyl adipate,
Isopropyl myristate and isopropyl palmitate. These fatty acid esters may be used either individually or in combination of two or more, preferably two or more.

The content of the fatty acid ester in the present invention is preferably 0.01 to 50% by mass. More preferably 0.05 to 20 mass%, particularly preferably 0.1 to
It is 20% by mass. Within this range, a particularly good thermal sensation can be obtained.

By containing the above-mentioned zingerone and a fatty acid ester, a good warm feeling can be obtained, but this combination causes an itch problem. By blending a terpenoid compound, this itch can be effectively suppressed.

The terpenoid compound (C) used in the present invention can be classified into terpene hydrocarbons, terpene alcohols, terpene aldehydes and terpene ketones based on its structure. Further, depending on the number of carbon atoms, there are monoterpenes, sesquiterpenes, diterpenes, sesterterpenes, triterpenes, tetraterpenes and polyterpenes.

Examples of monoterpenes include geraniol, nerol, citronellol, linalool, citral, citronellal, limonene, α-terpineol, menthol, 1-menthol, menthone, citronellal, neomenthol, isomenthol, neoisomenthol,
Isopulegol, neoisopulegol, pinene, menthone, carvone, cineole, ascaridol, ionone, iron, nepetalactone, matatabilactone, actinidine, asperloside, actin, premieride, gentiopicrin, swertiamarin, curren,
There are caron, α-tujene, tujyl alcohol, tusion, camphor, camphene, borneol, and the like.

As sesquiterpenoids, farnesol, nerolidol, ipomeamarone, nugaion, bisabolens, bisaboren, juvavion, germacrans, pyrethrosin, heliandin, humulans, humulene, abscisic acid, cadyanans, eudesmans, udesmol , Atractylone, santonin, artemisin, ψ-santonin, allantolactone, elemophyllans, notecatons, drimans, iridin,
Farnesifol A, tutin, choriamiltin, caryophyllene, hydroazulenes, guaiol, lactusin, matricin, gagegerin, hydrovetibasulene, tujopsene, sedren, longifolene, helminsosporol, anisamine, and the like.

Examples of the diterpenoids are phylol, phytol, geranylgeraniol, camphorene, mannol, sucrerol, manoyl oxide, ketomanoyl oxide, agatic acid, malbiin, andrographolide, rearrangelabdans, clerodin, columbin, pimarans. , Pimaric acid, isopimaric acid,
There are abietanes, abietic acid, levopimaric acid, neoabietic acid, ferguilol, podocarpic acid, totarol, kawrans, phylocladene, kaurene, stevioside, cafestol, rearrange kaurenes, emmain, gibberellin, geranyl farnesol and the like.

As the triterpenoid, squalene,
Dehydrosqualene, lansic acid, α-onoserine,
Lanostane, lanosterol, ebricoic acid, tumulosic acid, polyporenic acid, cycloartenol,
Cycloeucarenol, Euphor, Chilcarol,
Butylrospermole, euphorbol, α-elemoic acid, betulafolien triol, herbolic acid, cephalosporins, eratericin, ovaknone, limonin, erythrodiol, chelic acid, germanicol, carotenoid and the like.

In the case of an optically active substance among the above compounds,
Any of the optical isomers can be used. Of the above, the preferred terpene is monoterpene. Particularly preferred are l-menthol, dl-camphor, borneol, geraniol and limonene.

The terpenoid compound of the present invention may be a synthetic product or a refined product of the compounds exemplified above, but a plant extract such as an essential oil containing the terpenoid compound may be used. Examples of such plant extracts include peppermint oil, eucalyptus oil, cinnamon oil, reneol, fennel oil, mint oil and the like.

The content of the terpenoid compound in the present invention is preferably 0.01 to 20% by mass. More preferably 0.05 to 10% by mass, particularly preferably 0.1.
Is about 5% by mass. Within this range, an excellent external preparation for warm sensation having no itching and having a good warm feeling can be obtained.

When the warming agent composition of the present invention contains a compound selected from water-soluble polymer compounds, organic amine compounds such as alkanolamines and aminocarboxylic acids, in addition to the above essential components, the warming feeling sustaining effect is obtained. It is preferable because it improves.

<Water-soluble biopolymer compound> Hydroxypropylcellulose, hydroxypropylmethylcellulose,
Cellulose derivatives such as hydroxyethyl cellulose, carmellose, croscarmellose and methyl cellulose,
Processed starch such as partially pregelatinized starch, polyvinyl alcohol,
Polyvinylpyrrolidone, crospovidone, polyethylene glycol, xanthan gum, carrageenan, sodium alginate, gum arabic, guar gum, locust bean gum, pullulan, gelatin, carboxyvinyl polymer, acrylic acid / alkyl methacrylate copolymer,
Examples thereof include sodium polyacrylate. Preferred water-soluble polymers are hydroxypropyl cellulose, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, carboxyvinyl polymer, and acrylic acid / alkyl methacrylate copolymers. These can be used alone or in combination of two or more.

The content of the water-soluble biopolymer compound in the composition is preferably 0.01 to 5% by mass, more preferably 0.05 to 2% by mass. Within this range, an external preparation having excellent warmth sensation and good usability can be obtained. When used as a coating agent-type external preparation, it is preferable to add the composition in such a range that the composition has a viscosity of 100 to 100,000 mPa · S at 20 ° C.

<Alkanolamine> Monoethanolamine, diethanolamine, triethanolamine, diisopropanolamine, tromethamine and the like can be mentioned. These can be used alone or in combination of two or more. The content is preferably 0.05 to 10
It is% by mass.

<Aminocarboxylic acid> Disodium edetate, amino acid, glycine, alanine, trimethylglycine, tryptophan, phenylalanine, histidine,
Examples include arginine, aspartic acid, glutamic acid and betaines. The content is preferably 0.05 to
It is 10% by mass.

In addition, when the warming agent composition of the present invention is applied as an external preparation, the following components can be used.

<Physiologically active ingredient> Compounds such as antiphlogistic analgesic, anti-inflammatory agent, keratolytic agent, antipruritic agent, antihistamine agent, local anesthetic agent, bactericidal agent, antibacterial agent and antifungal agent are mixed as active ingredients of the external preparation can do.

Specific examples of anti-inflammatory agents include tolfenamic acid, mefenamic acid, flufenamic acid, allantoin, aluminum chlorohydroxy allantoinate, ictamol, guaiazulene, dipotassium glycyrrhizinate, glycyrrhetinic acid, stearyl glycyrrhetinate, and salicylic acid. , Methyl salicylate, Glycol salicylate, Sodium salicylate, Indo persimmon,
Sikon, Touki, Aspirin, Sazapyrine, Alclofenac, Suprofen, Ibuprofen, Naproxen, Flurbiprofen, Ketoprofen, Fenbufen, Indomethacin, Acemethacin, Methiazic acid,
Protizic acid, sulindac, planoprofen, fenthiazac, diflunisal, thiaprofenic acid, oxaprozin, diclofenac sodium, oxyphenbutazone, piroxicam, felbinac, bufexamac, glycol salicylate, phenacetin phenylbutazone, tolmetin sodium and the like can be mentioned.

Examples of the antipruritic agents include crotamiton, isothipendyl hydrochloride, diphenylpyraline hydrochloride, diphenhydramine and its salts, triperenamine hydrochloride, chlorpheniramine and its salts, diphenylimidazole and the like.

Examples of the local anesthetic include ethyl aminobenzoate, lidocaine and its salts, dibucaine and its salts, diethyl aminoethyl parabutylaminobenzoate hydrochloride, oxypolyethoxydodecane and the like.

Examples of the bactericides include acrinol, alkylpolyaminoethylglycine, cetylpyridinium chloride, decalinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, chlorhexidine gluconate, chlorhexidine hydrochloride, cetrimide, trichlorocarbanilide, benzyl. Alcohol, povidone iodine, phenol, resorcin, hydrogen peroxide, cresol, mercury chrome, iodine tincture,
Examples thereof include sulfur.

Examples of the sulfa drug include sulfadiazine, sulfysomidine, homosulfamine and the like.

Examples of the antibiotic include bacitracin,
Examples include colistin sulfate, fradiomycin sulfate, and the like.

Examples of the steroid agents include dexamethasone acetate, hydrocortisone acetate, prednisolone acetate, dexamethasone, prednisolone and the like.

Examples of antifungal agents include miconazole nitrate, econazole nitrate, ciclopirox, olamine,
Examples include clotrimazole and pyrrolnitrin.

Examples of the analgesic include acetaminophen and etenzamid.

Examples of moisturizers include urea, ethylene glycol, diethylene glycol, propylene glycol, butylene glycol, dibutylene glycol, glycerin, diglycerin, polyglycerin, sucrose, lactose, maltose, mannitol, erythritol, xylitol, glucose, sorbitol. Etc.

Examples of the whitening agent include peroxides such as zinc peroxide and magnesium peroxide, ascorbic acid, hydroquinone, vitamin Cs, ellagic acid, kojic acid, placenta extract and licorice extract.

Examples of vitamins include pyridoxine hydrochloride, palmitic acid, retinol, vitamin A, tocopherol acetate and the like.

Examples of mucopolysaccharides include sodium chondroitin sulfate. As an amino acid,
Examples thereof include glycine, alanine, trimethylglycine, tryptophan, phenylalanine, histidine, arginine, aspartic acid and glutamic acid. Examples of the protective agent include calamine, zinc oxide and the like.

Among these, suprofen, ketoprofen, glycyrrhetinic acid, indomethacin and flurbiprofen are particularly preferably used. These drugs are used alone or in combination of two or more.

The amount of the physiologically active ingredient to be added should be an effective amount of each ingredient. For example, 0.1 to 5% by mass for suprofen and 0.1 to 5 for ketoprofen.
In the case of glycyrrhetinic acid, it is 0.1 to 10% by mass, in the case of indomethacin, it is 0.1 to 2% by mass, and in the case of flurbiprofen, it is 0.1 to 5% by mass.

<Other warming ingredients> Capsaicin derivatives such as nonyl acid vanillyl amide, benzyl nicotinate, nicotinic acid amide, methyl nicotinate, vanillyl butyl ether, capsaicin, capsicum, capsicum extract, capsicum powder, processed ginger, carrot tincture, Horse chestnut etc. are mentioned.

<Fatty Alcohol> As the fatty alcohol, lauryl alcohol, cetyl alcohol, cetostearyl alcohol, stearyl alcohol, oleyl alcohol, behenyl alcohol, eicosonyl alcohol, elaidyl alcohol, linoleyl alcohol and other straight-chain fatty alcohols, cholesterol , Cyclic fatty alcohols such as dihydrocholesterol, phytosterol and lanolin alcohol, synthetic fatty alcohols such as octyldodecanol, hexyldecanol and isostearyl alcohol. The incorporation of a fatty alcohol is preferable because it improves the percutaneous absorption of the physiologically active ingredient. The content is preferably 0.01 to 20% by mass.

<Fatty acids and / or salts thereof> Fatty acids and fatty acid salts include saturated fatty acids such as lauric acid, myristic acid, palmitic acid and stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonic acid and undecylenic acid. Examples thereof include unsaturated fatty acids and salts thereof. fatty acid,
It is preferable to add a fatty acid salt, because percutaneous absorption of the physiologically active ingredient is improved. More preferably, it is a fatty acid. The content is preferably 0.05 to 50% by mass in the composition,
More preferably, it is 0.1 to 30 mass%.

<Surfactant> The surfactant has the effect of maintaining the physical stability of the composition and the effect of dispersing the insoluble component. Any of anionic surfactants, cationic surfactants, nonionic surfactants and amphoteric surfactants can be used, but nonionic surfactants and amphoteric surfactants are preferred.

Examples of nonionic surfactants 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, polyglycerin fatty acid ester, and polyoxy. Examples thereof include ester compounds such as ethylene glycerin fatty acid ester, polyethylene glycol fatty acid ester, and sucrose fatty acid ester, polyoxyethylene castor oil / hardened castor oil, and polyoxyethylene polyoxypropylene polymer.

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.
Examples of the anionic surfactant include saturated higher fatty acid salts, alkyl sulfonates, alkyl ether sulfonates, alkyl ether sulfonates and the like.

As the cationic surfactant, a quaternary ammonium salt such as trimethylalkylammonium chloride,
Examples thereof include alkylamine salts such as dimethylalkylamine hydrochloride.

These can be used alone or in combination of two or more. The content of the surfactant is preferably 0.01 to 10% by mass, more preferably 0.05 to 5% by mass in the composition.

<Oil component> Liquid paraffin, petrolatum,
Hydrocarbons such as microcrystalline wax, silicone oils such as methylpolysiloxane, methylphenylpolysiloxane, dimethylcyclopolysiloxane, waxes such as beeswax, and metallic soaps such as aluminum stearate and magnesium stearate. To be The content of the oily component in the composition is preferably 0.05 to 50% by mass, more preferably 0.1 to 30% by mass.

<Powder> The powder is adsorbed or impregnated with a preparation for external use containing a warming composition, and remains on the skin after application to retain the warming composition on the skin, so that the external preparation has a warm feeling. It is preferable because it gives a lasting effect.

Examples of the inorganic powder include talc, kaolin, bentonite, layered silicate minerals such as aluminum magnesium silicate, titanium oxide, zinc oxide and the like.
Examples of the organic powder include spherical powders of nylon, silica, polymethylmethacrylate, etc., polyethylene beads, cellulose powder, starch, super absorbent polymers (polyacrylic acid starch, etc.) and the like. Preferred are layered silicate minerals and superabsorbent polymers.

The preferred average particle size of the powder is 0.
001 to 1000 μm. The content of the powder in the composition is preferably 0.01 to 10% by mass, more preferably 0.01 to 5% by mass.

<PH Adjusting Agent> The external preparation composition for skin of the present invention is preferably adjusted to pH 3 to 8, more preferably 4 to 7.

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, potassium hydroxide, monoethanolamine, diethanolamine, triethanolamine, Examples include various amines such as diisopropanolamine, triisopropanolamine and tromethamine, phosphates such as potassium hydrogenphosphate and sodium hydrogenphosphate, and organic salts such as sodium citrate and sodium lactate.
Diisopropanolamine and triisopropanolamine are preferable because they have good pH stability particularly when an acidic drug is used. The amount of pH adjuster is the set pH
Can be selected as appropriate.

<Chelating Agent> Examples include edetic acid, pyrophosphate, hexametaphosphate, gluconate and the like. Preferred is sodium edetate. The content is preferably 0.01 to 10 mass% in the composition. <Dye> Acid dyes, basic dyes, oxidation dyes and the like can be arbitrarily used. <Fragrance> A fragrance used for external preparations such as cosmetics can be arbitrarily used.

<Preservative> dibutylhydroxytoluene,
Examples thereof include benzoic acid or its salt, paraben, benzalkonium chloride, benzethonium chloride, sorbic acid and its salt, boric acid, borax, salicylic acid and its salt, and the like. Preferred are dibutylhydroxytoluene, sodium edetate, citric acid and its salts, and paraben. The content of the preservative is preferably 0.01 to 50 in the composition.
% By weight. More preferably 0.02 to 30% by weight,
It is particularly preferably 0.05 to 10% by weight.

<Solubilizer> Alcohol having 1 to 4 carbon atoms such as methanol, ethanol, various denatured alcohols (methanol, geraniol, octaacetyl sucrose, 1
Denatured alcohols such as 0% disodium benzoate alcohol solution), propanol, isopropanol, butanol, isobutanol and the like. Preferred are ethanol, octaacetyl sucrose denatured alcohol, and isopropanol. These may be used alone or in combination of two or more. The content of the solubilizing agent in the composition is preferably 5 to 80% by mass, more preferably 10 to 70% by mass,
It is particularly preferably 20 to 60% by weight.

<Water> The warming composition of the present invention can be used as both an aqueous external preparation and a non-aqueous external preparation, but an aqueous preparation is preferable in that the warm feeling is relatively strong. The content of water is preferably 1 to 90% by mass, and more preferably 10 to 60% by mass of the whole preparation. Is. In addition, various components which are usually used for external preparations can be optionally used within a range that does not impair the effects of the present invention.

The external preparation composition of the present invention comprises a lotion,
It can be formulated as dosage forms such as emulsions, gels, gel lotions, ointments, creams, aerosols and patches. Depending on the dosage form, the external preparation may be a suitable container such as a bottle for lotion or emulsion, a tube or jar for ointment, gel lotion, cream, a pressure-resistant can for aerosol, and a sealed for patch. It is stored in a bag.

As the material of the container, PET, polypropylene (PP), polyethylene (high density polyethylene: H
Examples include metals such as DPE, low density polyethylene (LDPE), glass, polystyrene, EVAL, and aluminum. The above materials may be used alone or in combination of two or more.

[0062]

EXAMPLES The present invention will now be specifically described with reference to examples, but the present invention is not limited to the following examples.

[Evaluation of Thermal Sensation] 50 at RH of 22 ° C. and 50%
Lotions, creams and gels were applied to the famous panelists by applying 0.5 g of the composition to the shoulders and evaluated. The patch is 10x7c
A preparation having a size of m was put on the shoulder and evaluated. The evaluation criteria are as follows, and the average score was shown. Very strong thermal sensation: 4 points Very strong thermal sensation: 3 points Thermal sensation: 2 points Some thermal sensation: 1 point No thermal sensation: 0 points

[Itching] It was evaluated whether the above 50 panelists felt itching when the composition was applied. The evaluation criteria are indicated by the percentage (%) of the panelists who had itching. The smaller the value, the less itchy and the better the feeling of use.

[0065]

[Table 1]

[0066]

[Table 2]

[0067]

[Table 3]

[0068]

[Table 4]

[0069]

[Table 5]

[0070]

[Table 6]

Claims (3)

[Claims] 1. A warming composition comprising (A) zingerone, (B) fatty acid ester, and (C) terpenoid compound. 2. An external preparation composition comprising (A) zingerone, (B) fatty acid ester, and (C) terpenoid compound. 3. The external preparation composition according to claim 2, which is a coating type external preparation.