JP3520149B2 - External preparation for skin roughening - Google Patents

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention belongs to a technical field relating to a skin external preparation. More specifically, the present invention relates to a skin external preparation having a significantly improved rough skin improving effect.

[0002]

2. Description of the Related Art The imparting of a function of maintaining a beautiful skin condition is one of the most important purposes when developing a skin external preparation such as cosmetics. In order to maintain this beautiful skin condition, it is important to prevent or improve the roughness of the skin and prepare the skin groove and crest.

Conventionally, for the purpose of maintaining a beautiful skin condition,
Creams and emulsions that replenish the skin with water and oil have been used as skin care bases. Then, various moisturizers have been positively blended with various skin external preparations. However, glycerin, sorbitol, propylene glycol, maltitol, and the like, which are currently used moisturizers, tend to be sticky or have a hot sensation when mixed in a large amount. Further, amino acid-based humectants such as DL-threonine tend to have defects such as coloring and odor.

[0004]

SUMMARY OF THE INVENTION The problem to be solved by the present invention is to provide a skin external preparation having a truly excellent effect of improving rough skin.

[0005]

Means for Solving the Problems As a result of extensive studies aimed at solving the above-mentioned problems, the present inventor has achieved the above-mentioned problems by using a skin external preparation containing a specific aminoethyl compound and tranexamic acid or a salt thereof. It was found that can be solved.

That is, the present invention is an invention which provides a skin external preparation for improving rough skin (hereinafter also referred to as the skin external preparation of the present invention) comprising the following components (1) and (2). (1) One or two aminoethyl compounds represented by the formula NH ₂ CH ₂ CH ₂ X (I) (wherein, X is —SO ₂ H or —SO ₂ SH), as a whole skin external preparation. 0.0001% by weight or more and 1.0% by weight or less. (2) The amount of tranexamic acid or a salt thereof is 0.01% by weight or more and 5.0% by weight or less based on the total amount of the external preparation for skin.

[0007]

[0008]

[0009]

[0010]

[0011]

BEST MODE FOR CARRYING OUT THE INVENTION Embodiments of the present invention will be described below. A. The external preparation for skin of the present invention contains an aminoethyl compound represented by the above formula (I). An aminoethyl compound represented by formula (I), that is, 2-aminoethylsulfinic acid (hypotaurine) in which X is —SO ₂ H, that is, a sulfinic acid group, and X is —SO ₂ SH, that is, a thiosulfonic acid group. -Aminoethylthiosulfonic acid (thiotaurine) is a major organ in many mammals, including humans,
For example, it is contained in the heart, brain, liver and the like, and is also contained in a large amount in foods that are ingested daily. In addition, side effects such as skin irritation, itching and rash have not been reported. Therefore, it is clear that there is no problem in safety even if the aminoethyl compound represented by the formula (I) is added to the skin external preparation of the present invention.

Further, these aminoethyl compounds (I)
Can be easily produced from a readily available thio compound such as cysteine by a commonly known method, and a commercially available product can be added to the external skin preparation of the present invention. By incorporating these aminoethyl compounds (I) into the external preparation for skin of the present invention, it is possible to greatly contribute to the expression of the desired skin roughening improving effect in the external preparation for skin of the present invention.

The blending amount of these aminoethyl compounds (I) in the external preparation for skin of the present invention should be appropriately changed according to the kind or amount of other components to be added to the external preparation for skin of the present invention, and is generally defined. Although it is not necessary, it is preferable that the amount is generally 0.0001% by weight or more and 1.0% by weight or less based on the entire skin external preparation of the present invention. The compounding amount of the aminoethyl compound (I) in the external preparation for skin of the present invention is 0.0001 of the whole external preparation for skin of the present invention.
If it is less than wt%, it is difficult to exert the desired effect of improving the above-mentioned rough skin in the external preparation for skin of the present invention, which is not preferable. Further, even if the amount exceeds 1.0% by weight of the total external preparation for skin of the present invention, the above effects corresponding to the increase in the amount added are no longer observed, which is not preferable.

From the balance between the expression level of the above effect and the blending amount, the aminoethyl compound (I) in the external preparation for skin of the present invention is approximately 0.001% of the total amount of the external preparation for skin of the present invention.
It is particularly preferable to blend in the range of not less than 0.1 % by weight and not more than 0.1% by weight .

When the blending amount is 0.0001% by weight or more and less than 0.001% by weight based on the total weight of the external preparation for skin of the present invention, the effect of improving the rough skin is not sufficient when only the aminoethyl compound (I) is blended. However, as a result, it tends to be necessary to increase the amount of other auxiliary components and the like compounded.

The total weight of the external preparation for skin of the present invention is 0.1%.
%, And at a compounding amount of about 1.0% by weight or less, the desired effect on the increase of the compounding amount of the aminoethyl compound (I) is slowly enhanced, but rather other auxiliary components are positively added. As a result, the external preparation for skin of the present invention tends to exert a superior effect.

The above-mentioned two aminoethyl compounds (I)
It is needless to say that each of them can be individually incorporated in the external preparation for skin of the present invention, but they can also be incorporated in combination. Further, when two kinds of aminoethyl compounds (I) are both compounded in the skin external preparation of the present invention, the compounding ratio of both of them in the skin external preparation of the present invention is arbitrary and is not particularly limited.

B. The external preparation for skin of the present invention further comprises
Xamic acid or its salts are mixed. These are generally used as antiplasmin agents and are generally known as highly safe ingredients for cosmetic use (Japanese Patent Publication No. 47-1479). In addition, the manufacturing method is the second patent.
40611, Patent 242664, Patent 4804
No. 11, Japanese Patent No. 488168.

Tranexamic acid has a melting point of 386 to 390.
White crystals or powder at ℃, odorless, and bitter in taste. Torane
As the salts of xamic acid, those commonly used include
Metal salts such as magnesium salt, calcium salt, potassium salt
And sulfates.

In the present invention, the above tranexamic acid is used.
Alternatively, one kind or two or more kinds are arbitrarily selected and mixed from the salts thereof. This tranexamic acid or its
The amount of salts in the external preparation for skin of the present invention should be appropriately changed according to the type or amount of other components to be added to the external preparation for skin of the present invention, and should not be specified unconditionally, but the skin of the present invention is generally used. 0.01% by weight of the total external preparation
Above, preferably blended in the range of 5.0 wt% or less ,
It is particularly preferably mixed in an amount of 0.1% by weight or more and 1.0% by weight or less . Tranexam in the external preparation for skin of the present invention
When the content of the acid or its salt is less than 0.01% by weight based on the total weight of the external preparation for skin of the present invention, it is difficult to exert the desired effect of improving rough skin on the external preparation for skin of the present invention, which is not preferable. Further, even if the amount exceeds 5.0% by weight of the total skin external preparation of the present invention, the above effect corresponding to the increase in the amount added is no longer observed, which is not preferable.

[0021] Incidentally, the aminoethyl compound (I) bets
The mixing ratio with lanexamic acid or its salts is not particularly limited as long as both components are within the above range, and is appropriately adjusted according to the specific dosage form of the external preparation for skin of the present invention. be able to. However, even within the above range, when one of the above components is blended in a large amount and the other is blended in a small amount, only the properties of one of the blended components tend to be excessively reflected in the skin external preparation of the present invention. There is no denying that aspect.

Surprisingly, when the above aminoethyl compound (I) and tranexamic acid or a salt thereof are blended together with the external preparation for skin of the present invention, the anti-inflammatory effect inherent to each blending component is merely additively added. In addition to exhibiting the above, it is possible to synergistically prevent or improve rough skin. The external preparation for skin of the present invention containing the above-mentioned active ingredient can sufficiently exhibit the intended effect of improving rough skin by blending only the active ingredient.

However, if necessary, other medicinal ingredients are added to the skin external preparation of the present invention for the purpose of imparting an effect that the skin external preparation will generally exhibit, by adding other medicinal ingredients. Can be added within the range that does not impair the intended effect of the present invention.

For example, imparting a moisturizing effect is useful for the purpose of preventing rough skin due to dry skin. In this case, for example, polyethylene glycol, propylene glycol, glycerin, 1,3-butylene glycol,
Hexylene glycol, xylitol, sorbitol,
Maltitol, chondroitin sulfate, hyaluronic acid, mucoitin sulfate, caronic acid, atelocollagen, cholesteryl-12-hydroxystearate, sodium lactate, bile salt, dl-pyrrolidone carboxylate, short chain soluble collagen, diglycerin (EO) PO It is possible to add a moisturizer such as an adduct, an extract of Ibiza rose, an extract of sawtooth grass and an extract of meliloth to the external preparation for skin of the present invention.

Providing an anti-ultraviolet effect is useful for suppressing damage to the skin due to excessive exposure of the skin to ultraviolet rays. In this case, for example methyl anthranilate, homomenthyl -N- acetyl anthranilate anthranilic acid UV absorbers such as anthranilate; 2, 4-dihydroxybenzophenone, 2, 2 ^'- dihydroxy-4-methoxybenzophenone, 2, 2' -Dihydroxy-4,4 '
-Dimethoxybenzophenone, 2,2 ', 4,4'-tetrahydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2-hydroxy-4-
Methoxybenzophenone-5-sulfonate, 4-phenylbenzophenone, 2-ethylhexyl-4'-phenyl-benzophenone-2-carboxylate, 2-hydroxy-4-n-octoxybenzophenone, 4-hydroxy-3-carboxybenzophenone benzophenone ultraviolet absorbers and the like; 2, 2'-hydroxy-5-methylphenyl benzotriazole, 2- (2 ^'- hydroxy-5'-t-octylphenyl) benzotriazole, 2- ^(2' - hydroxy-5 '-Methylphenyl)
Benzotriazole ultraviolet absorbers such as benzotriazole; Ziani soil methane, 4-methoxy -4 ^'-t-
A long-wavelength ultraviolet absorber such as butyldibenzoylmethane (parsol A) can be added to the skin external preparation of the present invention.

Further, para-aminobenzoic acid (hereinafter referred to as PAB
A), PABA monoglycerin ester, N, N
-Dipropoxy PABA ethyl ester, N, N-diethoxy PABA ethyl ester, N, N-dimethyl PA
Benzoic acid type ultraviolet absorbers such as BA ethyl ester, N, N-dimethyl PABA butyl ester, N, N-dimethyl PABA amyl ester; dipropylene glycol salicylate, ethylene glycol salicylate, myristyl salicylate, methyl salicylate, amyl salicylate, menthyl salicylate. , Homomenthyl salicylate, octyl salicylate, phenyl salicylate,
Salicylic acid-based UV absorbers such as benzyl salicylate and p-isopropanol phenyl salicylate; octyl cinnamate, ethyl-4-isopropyl cinnamate, methyl-2,5-diisopropyl cinnamate, ethyl-2,4-diisopropyl cinnamate, methyl-
2,4-diisopropyl cinnamate, propyl-p-
Methoxycinnamate, isopropyl-p-methoxycinnamate, isoamyl-p-methoxycinnamate,
Octyl-p-methoxycinnamate (2-ethylhexyl-p-methoxycinnamate), 2-ethoxyethyl-p-methoxycinnamate, cyclohexyl-p-
Methoxycinnamate, ethyl-α-cyano-β-phenylcinnamate, 2-ethylhexyl-α-cyano-
β-phenylcinnamate, glyceryl mono-2-ethylhexanoyl-diparamethoxycinnamate, octyl methoxycinnamate, 3,4,5-trimethoxycinnamate-3-methyl-4- [methylbis (trimethylsiloxy) ) Silyl] butyl, cinnamic acid-based UV absorbers such as p-dimethoxycinnamic acid monoethyl ester; 3- (4'-
Camphor derivatives such as methylbenzylidene) -d, 1-camphor, 3-benzylidene-d, 1-camphor, 5- (3,3-dimethyl-2-norbornylidene) -3-penten-2-one; urocanic acid, urocanine Medium wavelength ultraviolet (UVB) absorbers such as acid ethyl ester, 2-phenyl-5-methylbenzoxazole and dibenzalazine can be added to the external skin preparation of the present invention.

Further, an ultraviolet blocking agent such as titanium oxide (TiO ₂ ), talc (MgSiO ₂ ), carmine (FeO ₂ ), bentonite, kaolin, zinc oxide (ZnO) can be added to the external skin preparation of the present invention. Is.

It is also beneficial to impart a whitening effect to the external preparation for skin of the present invention. In this case, a whitening agent such as a placenta extract, glutathione, and Yukinoshita extract can be added to the external skin preparation of the present invention.

Adding an anti-inflammatory effect is also useful for suppressing skin inflammation and preventing rough skin. in this case,
An anti-inflammatory agent such as a glycyrrhizinic acid derivative, a glycyrrhetinic acid derivative, a salicylic acid derivative, hinokitiol, zinc oxide, and allantoin can be added to the external skin preparation of the present invention.

Similarly, for the purpose of alleviating skin damage caused by ultraviolet rays, activating agents such as royal jelly, photosensitizer, cholesterol derivative, and calf blood extract; nonylvalerenamide, nicotinic acid benzyl ester, nicotinic acid β-
Butoxyethyl ester, capsaicin, zingerone,
Cantharis tincture, ictamol, caffeine, tannic acid, α-borneol, tocopherol nicotinate,
Inositol hexanicotinate, cyclanderate,
Blood circulation promoters such as cinnarizine, trazoline, acetylcholine, verapamil, cepharanthin, γ-oryzanol, etc .; antiseborrheic agents such as sulfur, thiantol, etc. can be added to the external preparation for skin of the present invention.

In addition, for various purposes, oyster extract component, laurel extract component, shikon extract component, peony extract component, assembly extract component, birch extract component, sage extract component, loquat extract component, carrot extract component, aloe extract component, Mallow extract component, iris extract component, grape extract component, Yokuinin extract component, loofah extract component, lily extract component, saffron extract component, senkyu extract component, ginger extract component, Hypericum extract component, Ononis extract component, rosemary extract component, Garlic extract ingredient,
It is also possible to mix a pepper extract component, an Iza oyster rose extract component, a western saw grass extract component, a merlot extract component, a botanical extract such as chimpi, and Japanese clover in the skin external preparation of the present invention.

Further, in order to further impart a unique effect of each vitamin, such as a skin activating effect, to the external preparation for skin of the present invention, vitamin A oils such as vitamin A oil, retinol and retinol acetate; riboflavin, riboflavin butyrate. , Flavin adenine nucleotides and other vitamin B ₂
S; pyridoxine hydrochloride, vitamin B ₆ such as pyridoxine dioctanoate; L-ascorbic acid, L- ascorbic acid dipalmitate ester, L- ascorbic acid-2-sodium sulfate, L- ascorbic acid phosphoric acid ester, Vitamin Cs such as DL-α-tocopherol-L-ascorbic acid phosphoric acid diester dipotassium; pantothenic acids such as calcium pantothenate, D-pantothenyl alcohol, pantothenyl ethyl ether, acetylpantothenyl ethyl ether; ergocalciferol, cole Vitamin Ds such as calciferol; Nicotinic acid, nicotinic acid amide, nicotinic acid such as benzyl nicotinate; α-tocopherol, tocopherol acetate, DL-α-tocopherol nicotinate, DL-α succinate
-Vitamin Es such as tocopherol; other vitamins such as vitamin P and biotin can be incorporated into the external preparation for skin of the present invention.

The above-mentioned medicinal components are not limited to other medicinal components which can be incorporated into the external preparation for skin of the present invention. The medicinal effects corresponding to the other medicinal components listed above are not limited to the above. For example, vitamin Cs can be used as a whitening component and also as an antioxidant aid. Further, the other medicinal ingredients listed above may be blended alone in the external preparation for skin of the present invention, or two or more medicinal ingredients may be blended in an appropriate combination according to the purpose. .

INDUSTRIAL APPLICABILITY The present invention can be widely applied to cosmetics, pharmaceuticals, quasi-drugs and the like applied to the outer skin, and its dosage form is also an aqueous solution type, a solubilizing type, an emulsifying type, a powder type, an oil type. A wide variety of dosage forms such as liquid type, gel type, ointment type, aerosol type, water-oil two-layer type, water-oil-powder three-layer type can be adopted. In other words, in the case of basic cosmetics, the form of facial cleansers, lotions, milky lotions, creams, gels, essences (cosmetics), packs and masks, and hair cosmetics such as hair tonics, hair creams, shampoos and hair rinses In addition, it is widely applicable in the above various dosage forms. Further, makeup cosmetics can be widely applied to forms such as foundations. Furthermore, as long as it is a drug or a quasi drug, it can be widely applied in the form of various ointments and the like.
The forms that the external preparation for skin of the present invention can take are not limited to these forms and forms.

In the external preparation for skin of the present invention, generally known base components are blended widely according to the above-mentioned desired dosage form and form within the range in which the intended effect of the present invention is not impaired by the blending thereof. You can

That is, avocado oil, camellia oil, evening primrose oil, turtle oil, macadamia nut oil, corn oil, mink oil, olive oil, rapeseed oil, egg yolk oil, sesame oil, persic oil, wheat germ oil, southern oil, castor oil, linseed oil. Oil, safflower oil, cottonseed oil, eno oil, soybean oil, peanut oil, teaseed oil, kaya oil, rice bran oil, cinnamon oil, Japanese kiri oil, jojoba oil, germ oil, triglycerin,
Liquid fats and oils such as glycerin trioctanoate and glycerin triisopalmitate; cocoa butter, coconut oil, horse fat, hardened coconut oil, palm oil, beef tallow, sheep fat, hardened beef tallow, palm kernel oil,
Solid fats and oils such as pork fat, beef bone fat, mokuro kernel oil, hydrogenated oil, beef leg oil, mokuro, hydrogenated castor oil; beeswax, candelilla wax, cotton wax, carnauba wax, bayberry wax, ivotaro, whale wax, montan wax, nukarou, lanolin,
Kapok wax, lanolin acetate, liquid lanolin, sugar cane wax, lanolin fatty acid isopropyl, hexyl laurate, reduced lanolin, jojoba wax, hard lanolin,
Shellac wax, POE lanolin alcohol ether, P
Waxes such as OE lanolin alcohol acetate, POE cholesterol ether, lanolin fatty acid polyethylene glycol, POE hydrogenated lanolin alcohol ether; oils such as liquid paraffin, ozokerite, squalene, pristane, paraffin, ceresin, squalene, petrolatum, microcrystalline wax, etc. Hydrocarbon oils; lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, 12-
Hydroxystearic acid, undecylenic acid, tallic acid,
Isostearic acid, linoleic acid, linoleic acid, eicosapentaenoic acid (EPA), docosahexaenoic acid (DH
Higher fatty acids such as A); lauryl alcohol, cetyl alcohol, stearyl alcohol, behenyl alcohol,
Linear alcohols such as myristyl alcohol, oleyl alcohol, and cetostearyl alcohol, monostearyl glycerin ether (batyl alcohol), 2-decyltetradecinol, lanolin alcohol, cholesterol, phytosterols, hexyldecanol, isostearyl alcohol, octyldodecanol, etc. Branched alcohols such as isopropyl myristate, cetyl octanoate, octyldodecyl myristate, isopropyl palmitate, butyl stearate,
Hexyl laurate, myristyl myristate, decyl oleate, hexyldecyl dimethyloctanoate, cetyl lactate, myristyl lactate, lanolin acetate, isocetyl stearate, isocetyl isostearate, cholesteryl 12-hydroxystearylate, ethylene glycol di-2-ethylhexylate. , Dipentaerythritol fatty acid ester, N-alkyl glycol monoisostearate, neopentyl glycol dicaprate, diisostearyl malate, glycerin di-2-heptylundecanoate, tri-2-ethylhexyl trimethylolpropane, triisostearate tri Methylol propane, tetra-2-ethylhexyl pentane erythritol, tri-2-ethylhexyl glycerin, triisostearate Trimethylol propane, cetyl-2
Ethyl hexanoate, 2-ethylhexyl palmitate, glycerin trimyristate, glyceride tri-2-heptylundecanoate, castor oil fatty acid methyl ester, oleic acid oil, cetostearyl alcohol,
Acetoglyceride, 2-heptylundecyl palmitate, diisobutyl adipate, N-lauroyl-L-
Glutamic acid-2-octyldodecyl ester, di-2-heptylundecyl adipate, ethyl laurate,
Di-2-ethylhexyl sebacate, myristic acid 2-
Hexyldecyl, 2-hexyldecyl palmitate, 2-hexyldecyl adipate, diisopropyl sebacate, 2-ethylhexyl succinate, synthetic ester oils such as ethyl acetate, butyl acetate, amyl acetate, triethyl citrate; dimethylpolysiloxane, methyl Chain polysiloxanes such as phenylpolysiloxane and methylhydrogenpolysiloxane, cyclic polysiloxanes such as decamethylpolysiloxane, dodecamethylpolysiloxane, and tetramethyltetrahydrogenpolysiloxane, and silicone resins that form a three-dimensional network structure. , Silicones such as silicone rubber; base for soap, fatty acid soap such as sodium laurate, sodium palmitate, etc., higher alkyl sulfate ester salt such as sodium lauryl sulfate, K lauryl sulfate, P E triethanolamine lauryl sulfate, alkyl ether sulfate salts such as POE sodium lauryl sulfate, sodium lauroyl sarcosinate, etc. N- acyl sarcosinates, N- myristoyl -N-
Methyl taurine sodium, coconut oil fatty acid methyl tauride sodium, lauryl methyl tauride sodium and other higher fatty acid amide sulfonates, POE oleyl ether phosphate sodium, POE stearyl ether phosphate and other phosphate ester salts, di-2-ethylhexyl Sodium sulfosuccinate, monolauroyl monoethanolamide polyoxyethylene sodium sulfosuccinate, sulfosuccinates such as sodium lauryl polypropylene glycol sulfosuccinate, sodium linear dodecylbenzenesulfonate, triethanolamine linear dodecylbenzenesulfonate, linear dodecylbenzenesulfonic acid, etc. Alkylbenzene sulfonate, N-
Monosodium lauroyl glutamate, disodium N-stearoyl glutamate, N-myristoyl-L
-N-acyl glutamate such as monosodium glutamate, higher fatty acid ester sulfate such as hydrogenated coconut oil fatty acid glycerin sodium sulfate, sulfated oil such as funnel oil, POE alkyl ether carboxylic acid, POE alkyl allyl ether carboxylate, α-olefin sulfonate, higher fatty acid ester sulfonate, secondary alcohol sulfate ester salt, higher fatty acid alkylolamide sulfate ester salt, lauroyl monoethanolamide sodium succinate, N-palmitoyl aspartate ditriethanolamine, sodium caseinate, etc. Anionic surfactants; alkyl trimethyl ammonium salts such as stearyl trimethyl ammonium chloride, lauryl trimethyl ammonium chloride, distearyl dimethyl ammonium chloride Alkylpyridinium salts, such as alkyl dimethylammonium salts, poly (N, N'-dimethyl-3,5-methylenepiperidinium chloride), cetylpyridinium chloride, alkyl quaternary ammonium salts, alkyldimethylbenzylammonium salts, alkylisoxy Cationic surfactants such as norinium salts, dialkylmorphonium salts, POE alkylamines, alkylamine salts, polyamine fatty acid derivatives, amyl alcohol fatty acid derivatives, benzalkonium chloride, benzethonium chloride;
2-Undecyl-N, N, N- (hydroxyethylcarboxymethyl) -2-imidazoline sodium, 2-cocoyl-2-imidazolinium hydroxide-1-carboxyethyloxy disodium salt, etc., imidazoline-based amphoteric interface Amphoteric surfactants such as activators, betaine-based surfactants such as 2-heptadecyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, lauryldimethylaminoacetic acid betaines, alkyl betaines, amidobetaines, sulfobetaines; sorbitan Monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan sesquioleate,
Sorbitan fatty acid esters such as sorbitan trioleate, penta-2-ethylhexyl diglycerol sorbitan, tetra-2-ethylhexyl diglycerol sorbitan, mono cottonseed oil fatty acid glycerin, monoerucic acid glycerin, sesquioleate glycerin, monostearate glycerin, α , α'-glyceryl pyroglutamate oleate, glycerol monostearate glycerin polyglycerin fatty acids such as malic acid, propylene glycol fatty acid esters such as propylene glycol monostearate, hydrogenated castor oil derivative, glycerin alkyl ether, polyoxyethylene Lipophilic nonionic surfactant such as methylpolysiloxane copolymer; PO
E sorbitan monooleate, POE-sorbitan monostearate, POE-sorbitan monooleate, PO
POE sorbitan fatty acid esters such as E-sorbitan tetraoleate, POE-sorbit monolaurate, POE-sorbit monooleate, POE-sorbit pentaoleate, POE-sorbit monostearate, and other POE sorbit fatty acid esters, PO
POE glycerin fatty acid esters such as E-glycerin monostearate, POE-glycerin monoisostearate, POE-glycerin triisostearate, P
OE monooleate, POE distearate, POE monodioleate, POE fatty acid esters such as ethylene glycol distearate, POE lauryl ether,
POE oleyl ether, POE stearyl ether,
POE alkyl ethers such as POE behenyl ether, POE 2-octyldodecyl ether, POE cholestanol ether, POE octyl phenyl ether,
POE alkyl phenyl ethers such as POE nonyl phenyl ether and POE dinonyl phenyl ether, Pluronic types such as Bourronic, POE / POP cetyl ether, POE / POP 2-decyl tetradecyl ether, POE / POP monobutyl ether, POE
・ POE hydrogenated lanolin, POE / POP alkyl ethers such as POE / POP glycerin ether, tetra POE / tetra POP ethylenediamine condensates such as Tetronic, POE castor oil, POE hydrogenated castor oil, PO
E hydrogenated castor oil monoisostearate, POE hydrogenated castor oil triisostearate, POE hydrogenated castor oil monopyroglutamic acid monoisostearate diester, PO
E hydrogenated castor oil POE castor oil such as maleic acid hydrogenated castor oil derivative, POE beeswax lanolin derivative such as POE sorbit beeswax, alkanol amide such as coconut oil fatty acid diethanolamide, lauric acid monoethanolamide, fatty acid isopropanolamide, POE propylene glycol Fatty acid ester, POE alkylamine, POE fatty acid amide, sucrose fatty acid ester, PO
E Nonylphenyl formaldehyde condensates, hydrophilic nonionic surfactants such as alkylethoxydimethylamine oxide, trioleylphosphoric acid, etc .; preservatives such as ethylparaben, butylparaben; arabia gum, tragacanth gum, galactan, guar gum, carob gum, karaya gum, carrageenan , Pectin, agar, quince seed (quince), arge colloid (cassius extract),
Starch (rice, corn, potato, wheat), plant-based macromolecules such as glycyrrhizinate, microbial-based macromolecules such as xanthan gum, dextran, succinoglucan, and vullan, collagen, casein, albumin,
Natural water-soluble polymers such as animal polymers such as gelatin; starch-based polymers such as carboxymethyl starch and methyl hydroxypropyl starch Methyl cellulose, nitrocellulose, ethyl cellulose, methyl hydroxypropyl cellulose, hydroxyethyl cellulose, sodium cellulose sulfate, hydroxy Propyl cellulose,
Cellulosic polymers such as sodium carboxymethyl cellulose (CMC), crystalline cellulose, and cellulose powder,
Semi-synthetic water-soluble polymers such as alginic acid-based polymers such as sodium alginate and propylene glycol alginate; vinyl-based polymers such as polyvinyl alcohol, polyvinyl methyl ether, polyvinyl pyrrolidone, carboxyvinyl polymer (Carbopol), and alkyl-modified carboxyvinyl polymer. Polymer, polyethylene glycol 2
Polymers such as 000, 4000, 6000, polyoxyethylene-polyoxypropylene copolymer copolymers, sodium polyacrylate, polyethyl acrylate, polyacrylamide and other acrylic polymers, polyethyleneimine, Synthetic water-soluble polymer such as cationic polymer; bentonite, silicic acid A1Mg
(Veegum), laponite, hectorite, inorganic water-soluble polymers such as silicic acid; gum arabic, carrageenan, karaya gum, tragacanth gum, carob gum, quince seed (quince), casein, dextrin,
Gelatin, sodium pectate, sodium alginate, methylcellulose, ethylcellulose, CMC, hydroxyethylcellulose, hydroxypropylcellulose, PVA, PVM, PVP, sodium polyacrylate, carboxyvinyl polymer, locust bean gum, guar gum, tamarind gum, dialkyldimethylammonium sulfate. Thickeners such as cellulose, xanthan gum, magnesium aluminum silicate, bentonite, hectorite; talc, carion, mica, sericite, muscovite, phlogopite, synthetic mica, phlogopite, biotite, lithia mica, Permiculite, magnesium carbonate, calcium carbonate, aluminum silicate, barium silicate, calcium silicate, magnesium silicate, strontium silicate, tan Sten acid metal salt, magnesium, silica, zeolite, barium sulfate, calcined calcium sulfate (calcined gypsum), calcium phosphate, fluorine apatite, hydroxyapatite, ceramic powder, metal soap (zinc myristate, calcium palmitate,
Aluminum stearate), inorganic powder such as boron nitride, polyamide resin powder (nylon powder), polyethylene powder, polymethylmethacrylate powder, polystyrene powder, copolymer resin powder of styrene and acrylic acid, benzoguanamine resin powder, polytetrafluorocarbon Powder components such as organic powders such as ethylene oxide and cellulose powder; inorganic white pigments such as titanium dioxide and zinc oxide; inorganic red pigments such as iron oxide (red iron oxide) and iron titanate; inorganic brown such as γ-iron oxide. -Based pigments, inorganic yellow pigments such as yellow iron oxide and loess, inorganic black pigments such as black iron oxide, carbon black and low order titanium oxide, inorganic purple pigments such as mango violet and cobalt violet, chromium oxide, chromium hydroxide , Inorganic green pigments such as cobalt titanate, inorganic blue pigments such as ultramarine blue and navy blue,
Titanium oxide coated mica, titanium oxide coated bismuth oxychloride, titanium oxide coated talc, colored titanium oxide coated mica, bismuth oxychloride, pearl pigments such as fish scale foil, metal powder pigments such as aluminum powder, copper powder, red 201, red 202
No., Red No. 204, Red No. 205, Red No. 220, Red No. 226, Red No. 228, Red No. 405, Orange No. 203
No. 204, Orange No. 204, Yellow No. 205, Yellow No. 401 and Blue No. 404 and other organic pigments, Red No. 3, Red No. 104,
Red 106, Red 227, Red 230, Red 40
No. 1, Red No. 505, Orange No. 205, Yellow No. 4, Yellow 5
No., Yellow No. 202, Yellow No. 203, Green No. 3, Blue No. 1, etc., organic pigments such as zirconium, barium or aluminum lake, natural pigments such as chlorophyll, β-caroline, etc., titanium yellow, cursamine, safflower red etc. Coloring agents and the like; further, fragrances, water, alcohols and the like can be appropriately added to the external preparation for skin of the present invention as necessary. The specific formulation of the external preparation for skin of the present invention will be described in Examples described later.

[0037]

EXAMPLES Next, the present invention will be described more specifically by way of examples. However, this does not limit the technical scope of the present invention. In addition, the following weight%
The term "all" means% by weight based on the whole skin external preparation.

First, the evaluation method of the external preparation for skin of the present invention in Examples described later will be explained. Skin Roughness Prevention Test The skin on the back of healthy men was treated with a 3% sodium dodecyl sulfate aqueous solution to artificially induce skin roughness. Two hours after the above treatment, 20 μl of each sample was applied to the rough skin area caused by 20 μl. This was repeated for 5 days, and on the 6th day, the state of rough skin was visually observed and scored according to the criteria in Table 1. The higher the score, the better the effect of improving rough skin.

Table 1 Score Criterion Standard 1 A wide range of horny layer dryness, swelling and strong erythema are observed. 2 Exfoliation of the stratum corneum, swelling, and moderate erythema are observed. 3 Dryness of the stratum corneum is observed, but no curling is observed. Weak erythema. 4 Dryness and turning of the stratum corneum are not observed, but some erythema is observed. 5 Dryness, swelling and erythema of the stratum corneum are not observed.

There were 10 test males in each group, and the rough skin improving effect of each sample was judged based on the average value of the scores of these 10 test subjects.

Judgment ⊚: Average score is 4 or more ○: Average score is 3 or more and less than 4 Δ: Average score is 2 or more and less than 3 ×: Average score is less than 2

[Examples 1 to 5] Lotions Lotions having the formulations shown in Table 2 were prepared through the following process, and their rough skin improving effects were examined (see the same table).

[0043]

[Table 1] Table 2

<Production method> 95% ethyl alcohol, POE
(20) A lauryl ether and a fragrance are mixed, and then glycerin, propylene glycol, citric acid, tranexamic acid and 2-aminoethylthiosulfonic acid are mixed therein (in the comparative example, the essential components of the skin external preparation of the present invention are blended). The above is the same as in the description of the production method of the following examples.), And a desired amount of purified water is added so that the total weight becomes 100, and the mixture is mixed with the desired amount. A lotion was prepared.

In Table 2, tranexamic acid and 2-
The lotion of this example, which was prepared by combining both aminoethylthiosulfonic acid, was found to have an extremely excellent effect of improving rough skin in the combination of various compounding amounts. On the other hand, it was revealed that the lotion of Comparative Example in which either or both of tranexamic acid and 2-aminoethylthiosulfonic acid were not mixed was inferior in the rough skin improving effect to the above Examples. As a result, tranexamic acid and 2-
A synergistic effect on the rough skin improving effect was observed in the external preparation for skin formulated by combining aminoethylthiosulfonic acid.

Examples 6 to 10 Emulsions (1) Emulsions having the formulations shown in Table 3 were prepared through the following steps, and their rough skin improving effects were examined (see the same table).

[0047]

[Table 2] Table 3

<Production Method> POE (20) POP (2) cetyl alcohol ether, silicone KF96, liquid paraffin, perfume and preservative are dissolved at 70 ° C., and this dissolved product is composed of propylene glycol, glycerin and ethyl alcohol at 78 ° C. Of the carboxyvinyl polymer and hydroxypropyl cellulose previously dissolved in ion-exchanged water are heated to 70 ° C. and put into this aqueous phase.
Finally, 2-aminomethylpropanol, placenta liquid, tranexamic acid and 2-aminoethylsulfinic acid were further added, and the mixture was emulsified at 70 ° C. with a homomixer and stirred to cool to prepare an emulsion.

From Table 3, it is apparent that even in the emulsion containing a combination of 2-aminoethylsulfinic acid and tranexamic acid, a synergistic effect similar to the lotions of Examples 1 to 5 described above for improving rough skin is recognized. became. Therefore, a synergistic effect for improving rough skin in the external preparation for skin prepared by combining 2-aminoethylsulfinic acid and tranexamic acid in combination was also recognized.

[Examples 11 to 15] Emulsion (2) Emulsions having the formulations shown in Table 4 were prepared through the following steps, and their rough skin improving effects were examined (see the same table).

[0051]

[Table 3] Table 4

<Production Method> POE (20) POP (2) cetyl alcohol ether, silicone KF96, liquid paraffin, perfume and preservative are dissolved at 70 ° C., and this dissolved product is composed of propylene glycol, glycerin and ethyl alcohol at 78 ° C. Of the carboxyvinyl polymer and hydroxypropyl cellulose previously dissolved in ion-exchanged water are heated to 70 ° C. and put into this aqueous phase.
Finally, 2-aminomethylpropanol, placenta liquid, tranexamic acid, 2-aminoethylsulfinic acid and 2-aminoethylthiosulfonic acid were further added, emulsified with a homomixer at 70 ° C., and cooled with stirring to prepare an emulsion.

According to Table 4, the emulsion prepared by combining 2-aminoethylsulfinic acid and 2-aminoethylthiosulfonic acid together with tranexamic acid was prepared by adding one of the aminoethyl compounds (I) of the present invention to tranexamic acid. It was revealed that the effect of improving rough skin is comparable to that of the case of blending with acid.

Examples of compounding the external preparation for skin of the present invention in various dosage forms will be described below as examples. In addition, each external preparation for skin exhibited an excellent effect of improving rough skin. [Example 16] Nourishing cream% by weight Stearic acid 2.0 Stearyl alcohol 7.0 Reduced lanolin 2.0 Squalane 5.0 Octyldodecanol 6.0 POE (25) cetyl ether 3.0 Glyceryl monostearate 2.0 Propylene glycol 5.0 1,3-Butylene glycol 5.0 Tranexamic acid 2.0 2-Aminoethylsulfinic acid 0.5 Preservative proper amount Perfume proper amount Distilled water balance

<Production Method> The oil phase part was heated and mixed at 70 ° C., then the aqueous phase containing tranexamic acid and 2-aminoethylsulfinic acid was heated to 70 ° C., the oil phase was added to this aqueous phase, and the homomixer was added. After stirring and mixing with, and cooling, the desired nutritional cream was obtained.

[Example 17] Peel-off type pack Weight% Alcohol phase 95% Ethanol 10.0 POE (15) Oleyl alcohol ether 2.0 Preservative proper amount Perfume proper amount Water phase tranexamic acid vitamin C ester 1.0 2-aminoethyl Thiosulfonic acid 0.5 Polyvinyl alcohol 12.0 Glycerin 3.0 Polyethylene glycol 1500 1.0 Deionized water balance

<Production Method> Polyvinyl alcohol was stirred and dissolved in ion-exchanged water at 70 ° C., then tranexamic acid vitamin C ester, 2-aminoethylthiosulfonic acid, glycerin and polyethylene glycol 1500 were added, and the alcohol phase was further heated to 70 ° C. The mixture was heated to 1, added to the above mixture, stirred and uniformly mixed, and cooled to obtain a desired peel-off type pack.

[0058]   Example 18 Emulsion (3)                                                               weight%   POE (20) POP (2) cetyl alcohol ether 1.0   Silicone KF96 (manufactured by Shin-Etsu Chemical) 2.0   Liquid paraffin 3.0   Propylene glycol 5.0   Glycerin 2.0   Ethyl alcohol 15.0   Carboxy vinyl polymer 0.3   Hydroxypropyl cellulose 0.1   2-aminomethyl propanol 0.1   Potassium tranexamate 0.1   2-aminoethylsulfinic acid 0.01   Preservative Suitable amount   Fragrance suitable amount   Distilled water balance

<Production Method> An oil phase, which was also heated to 70 ° C., was added to the aqueous phase prepared at 70 ° C., emulsified by a homomixer treatment, and the emulsion was cooled to obtain a desired emulsion.

[0060]

According to the present invention, the effect of improving rough skin is excellent.
An external preparation for skin for improving rough skin is provided.

Continuation of the front page (56) Reference JP-A-6-80964 (JP, A) JP-A-7-126148 (JP, A) JP-A-6-329621 (JP, A) JP-A-6-72975 (JP , A) JP-A-6-41032 (JP, A) JP-A-7-206624 (JP, A) JP-B-47-1479 (JP, B1) (58) Fields investigated (Int.Cl. ⁷ , DB) Name) A61K 7/00-7/50

Claims (3)

(57) [Claims] 1. A skin comprising the following components (1) and (2):
A skin external preparation for improving roughness . (1) One or two aminoethyl compounds represented by the formula NH ₂ CH ₂ CH ₂ X (I) (wherein, X is —SO ₂ H or —SO ₂ SH), as a whole skin external preparation. 0.0001% by weight or more and 1.0% by weight or less. (2) The amount of tranexamic acid or a salt thereof is 0.01% by weight or more and 5.0% by weight or less based on the total amount of the external preparation for skin. 2. A compounding amount of the aminoethyl compound (I) is 0.001% by weight or more and 0.1% by weight or more based on the whole skin external preparation.
The external preparation for skin roughness improvement according to claim 1, which is as follows. 3. The skin external preparation for improving rough skin according to claim 1, wherein the content of tranexamic acid or a salt thereof is 0.1% by weight or more and 1.0% by weight or less based on the total weight of the external preparation for skin.