JP2017200904A - External composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an external composition having excellent stability and a good feeling in use.SOLUTION: An external composition is prepared that contains (A) acidic mucopolysaccharide, (B) C-Csaturated fatty acid, (C) higher alcohol, and (D) arginine, an arginine derivative, and/or a salt thereof.SELECTED DRAWING: Figure 1

Description

The present invention, (A) an acidic _{mucopolysaccharide, (B) C} 10 _{~C 24} saturated fatty acids, about external composition containing (C) a higher alcohol, and (D) arginine, an arginine derivative and / or salts thereof, .

  Liquid preparations, cream preparations, lotions, and emulsions are widely used as cosmetics that impart moisture retention and moisture to the skin and hair. Moisturizing is performed by retaining moisture in the skin and hair and preventing evaporation of moisture.

  In general, high-viscosity preparations such as creams and emulsions, and cosmetics that contain a lot of oil and are sticky tend to have better moisturizing properties than low-viscosity preparations and solubilized liquids.

  As a solubilizing liquid agent with improved moisturizing properties, Patent Document 1 proposes a cosmetic containing a vitamin E derivative and having excellent usability.

JP 2008-156326 A

  An object of the present invention is to provide a composition for external use that is stable and has a good feeling of use.

The present inventors have made extensive and intensive studies to solve this problem, (A) _{mucopolysaccharide, (B) C} 10 _{~C 24} saturated fatty acids, (C) a higher alcohol, and (D) arginine, an arginine derivative And / or the use of salts thereof has found that a composition for external use having good usability, high stability, and / or moisturizing effect can be obtained, and the present invention has been completed.

That is, this invention provides the composition for external use hung up below.
Item 1.
(A) acidic mucopolysaccharide,
_{(B) C} 10 ~C ₂₄ saturated fatty acids,
An external composition containing (C) a higher alcohol, and (D) arginine, an arginine derivative, and / or a salt thereof.
Item 2.
Item 2. The composition for external use according to Item 1, wherein the viscosity at 25 ° C is 100 to 300,000 mPa · s.
Item 3.
Item 3. The topical composition according to Item 1 or 2, further comprising 30 w / w% or more of water.
Item 4.
The acidic mucopolysaccharide is at least one selected from the group consisting of hyaluronic acid, alginic acid, hyaluronic acid derivative, alginic acid derivative, hyaluronic acid salt, alginic acid salt, hyaluronic acid derivative salt, and alginic acid derivative salt. The external composition of any one of claim | item 1-3.
Item 5.
The _C 10 _{-C 24} saturated fatty acid _is a C 16 _{-C 22} saturated fatty acid, any one external composition according to claim 1-4.
Item 6.
Item 6. The external composition according to any one of Items 1 to 5, wherein the higher alcohol is a C _{10 to} C ₂₄ aliphatic alcohol.
Item 7.
The arginine, arginine derivative, and / or salt thereof is L-arginine, D-arginine, L-arginine derivative, D-arginine derivative, L-arginine salt, D-arginine salt, L-arginine derivative salt, Item 7. The composition for external use according to any one of Items 1 to 6, which is at least one selected from the group consisting of salts of D-arginine derivatives.
Item 8.
Item 8. The composition for external use according to any one of Items 1 to 7, wherein the content of the acidic mucopolysaccharide is 0.001 to 1 w / w%.
Item 9.
The method for producing an external composition according to any one of Items 1 to 8,
(A) acidic mucopolysaccharide and (D) arginine, an arginine derivative heated to 50 ° C. or higher in a phase containing (B) a C ₁₀ -C ₂₄ saturated fatty acid heated to 50 ° C. or higher, and (C) a higher alcohol. The manufacturing method of the composition for external use including the process of adding the phase containing the salt / or those.

  According to the present invention, it is possible to provide an external composition that is stable and has a good feeling of use.

FIG. 1 is a graph showing the relative ratio (%) of the amount of moisture transpiration using an external composition of the present invention and cosmetics other than the external composition of the present invention.

  In the present specification, the unit of content “w / w%” is synonymous with “g / 100 g”.

The composition for external use of the present invention contains (A) an acidic mucopolysaccharide, (B) a C _{10 to} C ₂₄ saturated fatty acid, (C) a higher alcohol, and (D) arginine, an arginine derivative, and / or a salt thereof. .

[(A) Acid mucopolysaccharide]
In the present invention, (A) acidic mucopolysaccharide is used synonymously with glycosaminoglycan, and refers to a polysaccharide that is widely present in tissues mainly from connective tissues of animals.

  Such acidic mucopolysaccharides include, but are not limited to, hyaluronic acid, chondroitin, chitosan, jalluronic acid, heparan, keratan and alginic acid, and derivatives or salts thereof.

  Examples of the derivatives include, but are not limited to, ester derivatives in which a hydrogen atom in an acidic mucopolysaccharide is substituted with an alkyl group, an alkenyl group, an aryl group, etc .; an ester derivative in which a hydrogen atom of a hydroxyl group is substituted with an acyl group; Ether derivatives substituted with alkyl groups, alkenyl groups, aryl groups, etc .; hydrogen atoms of amino groups in mucopolysaccharides are substituted with amide derivatives substituted with acyl groups, alkyl groups, alkenyl groups, aryl groups, etc. Amine derivatives; and the like.

  The salt may be a pharmaceutically or physiologically acceptable salt, for example, an alkali metal salt such as sodium or potassium; an alkaline earth metal salt such as magnesium or calcium; a zinc salt; an ammonium salt; Examples thereof include sulfates; alkanolamine salts such as monoethanolamine. Among these, alkali metal salts are preferable, and sodium salts are more preferable.

  Preferred specific examples of acidic mucopolysaccharide salts include sodium hyaluronate, potassium hyaluronate, calcium hyaluronate, magnesium hyaluronate, zinc hyaluronate, ammonium hyaluronate, monoethanolamine hyaluronate, sodium acetylated hyaluronate, acetylated hyaluronan Potassium acid, acetylated calcium hyaluronate, magnesium acetylated hyaluronate, zinc acetylated hyaluronate, ammonium acetylated hyaluronate, hyaluronic acid crosspolymer, hydrolyzed hyaluronic acid, acetylated hyaluronic acid monoethanolamine, sodium chondroitin sulfate, chondroitin Potassium sulfate, sodium dermatan sulfate, potassium dermatan sulfate, chitosan ascorbic acid, chitosan glycolic acid, chito Down lactic acid, chitosan hydroxypropyltrimonium chloride, sodium heparan sulfate, potassium heparan sulfate, and sodium alginate.

  Among acidic mucopolysaccharides, hyaluronic acid, sodium hyaluronate, chondroitin sulfate, sodium chondroitin sulfate, sodium acetylated hyaluronate, potassium acetylated hyaluronate, calcium acetylated hyaluronate, magnesium acetylated hyaluronate, zinc acetylated zinc hyaluronate Sodium alginate is preferable, hyaluronic acid, sodium hyaluronate, chondroitin sulfate, sodium chondroitin sulfate, sodium acetylated hyaluronate, potassium acetylated hyaluronate, zinc acetylated hyaluronate, sodium alginate is more preferable, hyaluronic acid, sodium hyaluronate Even more preferred is sodium alginate.

  The average molecular weight of the acidic mucopolysaccharide is not particularly limited. For example, the weight average molecular weight is about 1000 to 4 million, preferably about 1000 to 3 million, more preferably about 5000 to 3 million, and particularly preferably about 5,000 to 2,000,000.

  For example, when the acidic mucopolysaccharide is hyaluronic acid or a salt thereof, the weight average molecular weight is a value measured by size exclusion chromatography. The conditions are as follows (column: TSKgel GMPWXL 7.8 mm × 30 cm (manufactured by Tosoh Corporation)), column temperature: constant temperature around 40 ° C., detector: differential refractometer, mobile phase: 0.2 mol / L NaCl, flow rate: 0.3 mL / min, injection amount: 100 μL, standard substance: pullulan standard product (STANDARD P-82, manufactured by Showa Denko KK)).

  Similarly, in the case of chondroitin, chondroitin sulfate or a salt thereof, the weight average molecular weight can be measured by a static light scattering method. Specifically, a dynamic light scattering photometer [DLS-8000 (Otsuka Electronics Co., Ltd.)] is used under the following conditions. A sample is dissolved in purified water to prepare a concentration of 10 mg / mL. This solution is further diluted with purified water to prepare concentrations of 2, 4, 6, 8 mg / mL. Static light scattering measurements at 20, 30, 40, 60, 90, 120, and 150 degrees at 25 ° C. and dn / dc measurements that are intrinsic refractive index increments, and from the Zimm square root plot and Debye plot, the weight average molecular weight Is calculated. Before the scattering measurement, the sample is filtered with a filter having a pore size of 0.22 μm. The dn / dc measurement can be performed with a DRM-3000 manufactured by Otsuka Electronics.

Similarly, the weight average molecular weight of other mucopolysaccharides such as alginic acid is also measured by GPC analysis.
For example, as a method for measuring the weight average molecular weight of alginic acid, the following method can be employed.
An analytical sample is obtained by taking 0.1 g of alginic acid (salt) and making a constant volume of 0.1% solution with distilled water. Next, 100 μL of the analysis sample is measured by gel permeation chromatography (GPC). The GPC operating conditions are as follows. A standard pullulan (Shodex STANDARD P-82 (Showa Denko KK) is used for the calibration curve for calculating the molecular weight. From this, the weight average molecular weight of alginic acid (salt) in the sample can be measured.
column:
(1) Super AW-L (Tosoh Corporation)
(2) TSK-GEL Super AW4000 (Tosoh Corporation)
Exclusion limit molecular weight 4 × 10 ⁵ PEO / DMF, length 15 cm, inner diameter 6 mm, TSK-GEL Super AW 2500 (Tosoh Corporation) manufactured by Tosoh Corporation
Exclusion limit molecular weight 2 × 10 ³ PEO / DMF, length 15 cm, inner diameter 6 mm, manufactured by Tosoh Corporation The above columns are connected in the order of AW-L, AW4000, and AW2500.
Column temperature: 40 ° C
Detector: differential refractometer mobile phase: 0.2 mol / L sodium nitrate aqueous solution flow rate: 0.6 mL / min
Injection volume: 100 μL

  These acidic mucopolysaccharides can be used alone or in combination of two or more.

  By using acidic mucopolysaccharide, the viscosity of the composition for external use of the present invention can be appropriately adjusted. The acidic mucopolysaccharide can contribute to making the composition for external use of the present invention non-sticky and having a refreshing composition. An acidic mucopolysaccharide can be synthesized and used, or a commercially available product can be used as it is.

Specifically, as an acidic mucopolysaccharide, sodium hyaluronate HA12 N (SHISEIDO CO., LTD.), Sodium acetylated hyaluronate (SHISEIDO CO., LTD.), Hyaro-oligo (Cuppy), hyaluronan HA-LQ (Cuppy Inc.), hyaluronic acid FCH-120 (Kikkoman Biochemifa), biohyaluronate sodium HA20N (SHISEIDO CO., LTD.), Hyaluronic acid FCH-60 (Kikkoman Biochemifa), duck algin NSPM-R
(Kimbun Food Chemifa Co., Ltd.), Kimika Argin IL-2 (Kimika), Duck Argin NSPH2R (Kikkoman Biochemifa) and the like are exemplified.

  In the external composition of the present invention, the total content of the component (A) with respect to the total amount of the external composition is appropriately set depending on the balance with other components. The total content of component (A) is preferably 0.001 w / w% or more, more preferably 0.005 w / w% or more, and still more preferably 0 with respect to the total amount of the external composition. 0.007 w / w% or more, most preferably 0.01 w / w% or more. The total content of component (A) is preferably 1 w / w% or less, more preferably 0.8 w / w% or less, more preferably 0.7 w / w% or less with respect to the total amount of the external composition. More preferably, it is 0.5 w / w% or less, most preferably 0.3 w / w% or less. The total content of component (A) is preferably 0.001 w / w% to 1 w / w%, more preferably 0.007 w / w% to 0.8 w / w% with respect to the total amount of the external composition. More preferably, it is 0.01 w / w% to 0.5 w / w%, and most preferably 0.05 w / w% to 0.3 w / w%.

_{[(B) C} 10 ~C ₂₄ saturated fatty acid]
In the present invention, (B) C ₁₀ ~C ₂₄ saturated fatty acids do not have a double bond or triple bond to a carbon chain, which is saturated with hydrogen, and that the fatty acids having 10 to 24 carbon atoms It is. Specifically, capric acid, undecylic acid, lauric acid, tridecylic acid, myristic acid, pentadecylic acid, palmitic acid, margaric acid, stearic acid, nonadecylic acid, arachidic acid, heicosyl acid, behenic acid, tricosylic acid, or lignoceric acid Say.

Such _{(B) C} 10 ~C ₂₄ saturated fatty acids, but are not limited to, from the viewpoint of the effect of the present invention is _remarkable, a C 16 _{-C 22} saturated fatty acids, palmitic acid, stearic acid Nonadecylic acid, arachidic acid, henicosylic acid, or behenic acid, particularly palmitic acid, stearic acid, and behenic acid are preferred.

These _C 10 _{-C 24} saturated fatty acids can also be used alone or in combination of two or more thereof.

C by use of a ₁₀ -C ₂₄ saturated fatty acids, can be a topical composition uniformity and stability excellent composition of the present invention. C ₁₀ -C ₂₄ saturated fatty acid that is used to synthesize, or a commercially available product can be used as it is.

  In the external composition of the present invention, the total content of the component (B) relative to the total amount of the external composition is appropriately set depending on the balance with other components. The total content of component (B) is preferably 0.01 w / w% or more, more preferably 0.1 w / w% or more, and even more preferably 0.2 w / w with respect to the total amount of the external composition. % Or more, more preferably 0.3 w / w% or more, and most preferably 0.5 w / w% or more. Moreover, the total content of the component (B) is preferably 8 w / w% or less, more preferably 7 w / w% or less, still more preferably 6 w / w% or less, more preferably with respect to the total amount of the external composition. Is 5 w / w% or less, most preferably 3 w / w% or less. The total content of component (B) is preferably 0.01 w / w% to 8 w / w%, more preferably 0.1 w / w% to 6 w / w%, based on the total amount of the external composition. Preferably, it is 0.3 w / w% to 5 w / w%, and most preferably 0.5 w / w% to 3 w / w%.

  In the composition for external use of the present invention, the ratio of the amount of the component (B) to the component (A) is such that the total content of the component (B) is 0.1 parts by weight with respect to 1 part by weight of the total content of the component (A). 01-8000 weight part is preferable, 0.1-1400 weight part is more preferable, 0.25-860 weight part is further more preferable, 0.42-500 weight part is still more preferable, 1-100 weight part is the most preferable.

[(C) higher alcohol]
In the present invention, the (C) higher alcohol refers to an alcohol having 6 or more carbon atoms, and may have either a linear or branched structure. As the higher alcohol, but are not limited, in _particular, C 10 _{-C 24} fatty alcohols are preferred. Such alcohols include capryl alcohol, lauryl alcohol, myristyl alcohol, cetyl alcohol (cetanol), stearyl alcohol, oleyl alcohol, or linoleyl alcohol, behenyl alcohol. Cetanol, stearyl alcohol, and behenyl alcohol are particularly preferable from the viewpoint that the effects of the present invention appear remarkably.

  These higher alcohols can be used alone or in combination of two or more.

  By using a higher alcohol, the composition for external use of the present invention can be made into a composition excellent in uniformity and stability. The higher alcohol can be synthesized and used, or a commercially available product can be used as it is.

  In the external composition of the present invention, the content of the (C) higher alcohol with respect to the total amount of the external composition is preferably 0.01 w / w% or more, more preferably 0.05 w / w% or more, and still more preferably. 0.1 w / w% or more, even more preferably 0.2 w / w% or more, and most preferably 0.5 w / w% or more. The total content of component (C) is preferably 10 w / w% or less, more preferably 7 w / w% or less, even more preferably 6 w / w% or less, even more based on the total amount of the external composition. Preferably it is 5 w / w% or less, Most preferably, it is 3 w / w% or less. The total content of component (C) is preferably 0.01 w / w% to 10 w / w%, more preferably 0.05 w / w% to 7 w / w%, based on the total amount of the external composition. More preferably, it is 0.1 w / w% to 5 w / w%, and most preferably 0.5 w / w% to 3 w / w%.

  In the composition for external use of the present invention, the ratio of the amount of component (C) to component (A) is such that the total content of component (C) is 0.1 parts by weight relative to the total content of component (A). It is preferably from 01 to 10,000 parts by weight, more preferably from 0.05 to 1400 parts by weight, even more preferably from 0.12 to 860 parts by weight, still more preferably from 0.28 to 500 parts by weight, and most preferably from 1 to 100 parts by weight.

[(D) Arginine, Arginine Derivative, and / or Their Salt]
In the present invention, (D) arginine, an arginine derivative, and / or a salt thereof is L-arginine or D-arginine, or a derivative thereof, or a salt of L-arginine or D-arginine, L-arginine or D- It refers to a salt of a derivative of arginine, and any of these may be used.

  Examples of the derivatives include, but are not limited to, ester derivatives in which a hydrogen atom in arginine is substituted with an alkyl group, an alkenyl group, an aryl group, or the like; an ester derivative in which a hydrogen atom of a hydroxyl group is substituted with an acyl group, or an alkyl derivative Ether derivatives substituted with groups, alkenyl groups, aryl groups, etc .; amide derivatives in which the hydrogen atom of the amino group is substituted with acyl groups, amine derivatives substituted with alkyl groups, alkenyl groups, aryl groups, etc .; Can be mentioned.

  The salt may be a pharmaceutically or physiologically acceptable salt, for example, an alkali metal salt such as sodium or potassium; an alkaline earth metal salt such as magnesium or calcium; a zinc salt; an ammonium salt; Examples thereof include sulfates; alkanolamine salts such as monoethanolamine.

  In the present invention, although not limited, L-arginine, a derivative thereof, or a salt thereof is preferably used as it is.

  Use of arginine, an arginine derivative, and / or a salt thereof, in combination with other components, can provide a composition that is particularly excellent in component stability and moisturizing effect.

  Moreover, these can also be synthesize | combined and a commercial item can also be used as it is.

  In the composition for external use of the present invention, the content of (D) arginine, arginine derivative, and / or salt thereof with respect to the total amount of the composition for external use is preferably 0.005 w / w% or more, more preferably 0. 05 w / w% or more, more preferably 0.1 w / w% or more, more preferably 0.15 w / w% or more, and most preferably 0.5 w / w% or more. The total content of (D) arginine, arginine derivatives, and / or their salts is preferably 4 w / w% or less, more preferably 3.5 w / w% or less, based on the total amount of the composition for external use. More preferably, it is 3 w / w% or less, More preferably, it is 2.5 w / w% or less, Most preferably, it is 1.5 w / w% or less. The total content of (D) arginine, arginine derivatives, and / or their salts is preferably 0.005 w / w% to 4 w / w%, more preferably 0. 05 w / w% to 3 w / w%, more preferably 0.15 w / w% to 2.5 w / w%, and most preferably 0.5 w / w% to 1.5 w / w%.

  In the composition for external use of the present invention, the ratio of the amount of the component (D) to the component (A) is such that the total content of the component (D) is 0.1 parts by weight with respect to 1 part by weight of the total content of the component (A). 005 to 4000 parts by weight is preferred, 0.05 to 700 parts by weight is more preferred, 0.12 to 430 parts by weight is still more preferred, 0.21 to 250 parts by weight is even more preferred, and 1 to 100 parts by weight is most preferred.

The ratio of the blending amount of the component (D) to the component (B) is preferably 0.0006 to 400 parts by weight of the total content of the component (D) with respect to 1 part by weight of the total content of the component (B). 0.007-35 weight part is more preferable, 0.02-15 weight part is further more preferable, 0.04-8.4 weight part is still more preferable, 0.2-3 weight part is the most preferable. (B) When the blending ratio of (D) arginine, arginine derivative, and / or salt thereof to the C ₁₀ -C ₂₄ saturated fatty acid is within this range, the composition for external use is not separated and the state of emulsification is also present Especially good.

  The composition for external use of this invention has a favorable usability | use_condition, high stability, and a moisturizing effect by containing (A) component, (B) component, (C) component, and (D) component. Here, a favorable feeling of use means that, when applied mainly to the skin or hair, it is preferably easy to spread and less squeaky. Or it may be included that there is little stickiness etc. depending on the case. High stability means maintaining uniformity within at least 60 minutes immediately after preparation of the composition for external use, for example. Having a moisturizing effect refers to retaining moisture in the skin, preventing or reducing moisture evaporation from the skin, or preventing transpiration of moisture applied to the skin.

Moreover, although it is not limited, in the composition for external use of the present invention, it may be preferable that the carbon numbers of the component (B) and the component (C) are the same. For example, as the component _(B), if included palmitic acid _{C 16} is Setano of _{C 16} as component (C) - is preferably included Le, likewise, as the component _(B), the _{C 18} When stearic acid is contained, it is preferable that _C18 stearyl alcohol is contained as the (C) higher alcohol. By matching these carbon numbers, the stability of the composition for external use of the present invention becomes higher.

  The composition for external use of the present invention may contain an appropriate amount of various pharmacologically active ingredients and physiologically active ingredients in addition to the components (A) to (D) as long as the effects of the present invention are not hindered.

  For example, terpenes can be blended in the composition for external use of the present invention in order to improve the refreshing feeling and the feeling of use such as stickiness. The terpenes are not particularly limited as long as they are terpenes that are usually used in skin external preparations. For example, monoterpenes such as camphor, menthol, borneol, eugenol, cineol, thymol, bisabolol, α-pinene, or limonene, farnesol, neroli Examples thereof include sesquiterpenes such as dolls, and diterpenes such as phytol and semblene. Monoterpenes are preferable, and menthol and camphor are more preferable. These terpenes can be either natural products or synthetic products, and may be either d-form, l-form or dl-form. These terpenes can also be used in skin preparations as essential oils containing terpenes, such as eucalyptus oil, mint oil, clove oil, cinnamon oil, peppermint oil, mint oil, tea tree oil, chamomile oil, Examples include rosemary oil, lemon oil, orange oil, thyme oil, sage oil, and clove oil. Eucalyptus oil, mint oil or tea tree oil is preferable, and eucalyptus oil or mint oil may be used as a skin external preparation. These terpenes can be used alone or in combination.

  The content of the terpenes can be appropriately selected without any particular limitation, but usually 0.001 to 10 w / w% with respect to the total amount of the composition for external use is preferable in consideration of the feeling of use and the degree of irritation. More preferably, it can be used in the range of 0.001 to 8 w / w%, particularly preferably 0.01 to 8 w / w%, and most preferably 0.01 to 5 w / w%.

  In addition to the above, the composition for external use of the present invention can be blended with one or more active ingredients that can be usually used in the field of pharmaceuticals, quasi drugs or cosmetics. Examples of these components include, but are not particularly limited to, medicinal components used in skin external preparations or hair external preparations. For example, antioxidants, whitening active ingredients, anti-inflammatory ingredients, local anesthetic ingredients, antipruritic ingredients Anti-inflammatory and analgesic ingredients, anti-wrinkle / anti-aging agents, keratin softening ingredients, cell activation ingredients, vitamins, moisturizing ingredients, ingredients that prevent DNA damage and / or have side effects, antibacterial ingredients, astringent ingredients, and the like. These components can be blended alone or in combination of two or more. Moreover, the compounding quantity of these components can be selected and used suitably. Specifically, 0.0001 to 10 w / w%, preferably 0.0005 to 5 w / w%, particularly preferably 0.001 to 3 w / w% is arbitrarily used for the entire external preparation. Can do.

Antioxidants: for example
(A) Tocopherols and derivatives thereof or salts thereof (for example, α-tocopherol, δ-tocopherol, acetic acid-α-tocopherol, tocotrienol), pyrroloquinoline quinone and derivatives thereof or salts thereof, ubiquinones and derivatives thereof or them Vitamin antioxidants, such as salts, retinols and derivatives thereof or salts thereof, pantothenic acid and derivatives or salts thereof, erythorbic acid or salts thereof;
(B) thiotaurine, cysteine, homocysteine, acetylcysteine, methionine, thioglycerol, sodium sulfite, sodium metabisulfite, sodium thiosulfate, sodium pyrosulfite, thioredoxin, dithiothreitol, alpha lipoic acid, ergothioneine, glutathione, glutathione peroxidase, Sulfur-containing antioxidants such as glutathione-S-transferase;
(C) phenols such as dibutylhydroxytoluene, dibutylhydroxyanisole, bisethylhexylhydroxydimethoxybenzyl malonate, diethylhexylsyringylidene malonate, gallic acid and its derivatives or their salts, chlorogenic acid and its derivatives or their salts Antioxidants;
(D) components derived from plants (eg, grapes, ginseng, comfrey, etc.) (eg, grape seed extract, grape leaf extract, ginseng extract, comfrey leaf extract, etc.); proanthocyanidins, hesperidins, glucosyl hesperidins, flavonoids Polyphenolic antioxidants, etc.

Whitening active ingredients: for example
(A) hydroquinone and derivatives thereof or salts thereof (for example, α-arbutin, β-arbutin); kojic acid; ellagic acid; phytic acid; lucinol; ascorbic acid and its derivatives or salts thereof (for example, ascorbic acid phosphate ester) Sodium, magnesium ascorbate phosphate, ascorbyl tetraisopalmitate (ascorbyl tetra-2-hexyldecanoate), 2-O-ethylascorbic acid, 3-O-ethylascorbic acid, ascorbic acid glucoside, etc.), potassium 4-methoxysalicylate Tyrosinase inhibitors such as salts, tranexamic acid and derivatives thereof or salts thereof;
(B) an endothelin-1 receptor inhibitor such as chamomile ET;
(C) a tyrosinase proteolytic promoter such as free linoleic acid;
(D) a melanin excretion enhancer such as adenosine monophosphate disodium salt;
(E) a melanin transport inhibitor such as niacinamide;
(F) Other plant components having a whitening effect (for example, plant extracts and essential oils).

  Anti-inflammatory component: for example, a component derived from a plant (for example, Comfrey leaf extract); allantoin, calamine, glycyrrhizic acid and derivatives thereof or salts thereof (dipotassium glycyrrhizinate, sodium glycyrrhizinate, etc.), glycyrrhetinic acid and derivatives thereof Or a salt thereof (stearyl glycyrrhetinate, 18α-hydroxyglycyrrhetinic acid, etc.), zinc oxide, guaiazulene, pyridoxine hydrochloride, menthol, camphor, turpentine oil, indomethacin, salicylic acid and its derivatives, epsilon aminocaproic acid, etc.

  Local anesthetic components: lidocaine; lidocaine hydrochloride; dibucaine; dibucaine hydrochloride; ethyl aminobenzoate; eucalyptus oil; eugenol; camphor; menthol; mint oil;

  Antipruritic ingredients: crotamiton; chlorpheniramine; chlorpheniramine maleate; diphenhydramine; diphenhydramine hydrochloride; diphenhydramine salicylate; salicylic acid; nonylic acid vanillylamide; mequitazine;

  Anti-inflammatory analgesic component: indomethacin; felbinac; salicylic acids such as methyl salicylate and glycol salicylate; allantoin or derivatives thereof; ibuprofen; ibuprofen piconol; bufexamac; butyl fenfenamic acid; bendazac; piroxicam;

  Anti-wrinkle, anti-aging ingredient: hydrolyzed soy protein, retinoid (retinol and its derivatives, retinoic acid, retinal etc.), pangamic acid, kinetin, ursolic acid, turmeric extract, sphingosine derivative, silicon, silicic acid, N-methyl-L -Serine, mevalonolactone, etc.

  Keratin soft component: Lanolin, urea, α-hydroxy acid (phytic acid, lactic acid, lactate, glycolic acid, salicylic acid, malic acid, etc.), citric acid, etc.

  Cell activating components: components derived from plants (for example, bilberry); amino acids such as γ-aminobutyric acid and ε-aminoproic acid; α-hydroxy acids such as glycolic acid and lactic acid; tannins, flavonoids, saponins, allantoins, photosensitivity Element 301 etc.

  Vitamins: Retinol, retinol acetate, retinol derivatives such as retinol palmitate, retinal, retinoic acid, methyl retinoic acid, ethyl retinoic acid, retinol retinoic acid, d-δ-tocopheryl retinoate, α-tocopheryl retinoate, β Vitamin A such as tocopheryl retinoate; provitamin A such as β-carotene, α-carotene, γ-carotene, δ-carotene, lycopene, zeaxanthin, cryptoxanthin, echinone; δ-tocopherol, α-tocopherol, Vitamin Es such as β-tocopherol, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate, δ-tocopherol, tocopherol nicotinate; riboflavin, flavin mononucleotide, flavin Vitamin B2 such as denine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, riboflavin tetranicotinate; nicotinic acids such as methyl nicotinate, nicotinic acid, nicotinamide; stearic acid Vitamin Cs such as ascorbyl, L-ascorbyl dipalmitate, ascorbyl tetraisopalmitate (ascorbyl tetra-2-hexyldecanoate); vitamin Ds such as methyl hesperidin, ergocalciferol, cholecalciferol; phylloquinone, farnoquinone, etc. Vitamin Ks: dibenzoyl thiamine, dibenzoyl thiamine hydrochloride, thiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl salt Acid salt, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate phosphate, thiamine monophosphate, thiamine diphosphate, thiamine diphosphate hydrochloride, thiamine triphosphate, Vitamin B1 such as thiamine triphosphate monophosphate; vitamin B6 such as pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5′-phosphate pyridoxal hydrochloride, pyridoxamine hydrochloride, vitamin B12 such as cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin Folic acids such as folic acid and pteroylglutamic acid; pantothenic acid, calcium pantothenate, pantothenyl alcohol (panthenol), D-pantothein, D-panthetin, complement Biotins such as biotin, biocytin; containing A, pantothenic acids such as pantothenyl ethyl ether other, carnitine, ferulic acid, alpha-lipoic acid, orotic acid, vitamin-like acting factors such γ- oryzanol.

  Moisturizing ingredients: ingredients derived from plants (eg, Tigaya); amino acids such as alanine, serine, leucine, isoleucine, threonine, glycine, proline, hydroxyproline, glucosamine, theanine and derivatives thereof; collagen, water-soluble collagen, gelatin, Proteins and peptides such as elastin and their hydrolysates; polyhydric alcohols such as glycerin, 1,3-butylene glycol, propylene glycol, dipropylene glycol, diglycerin; sugar alcohols such as sorbitol and xylitol; lecithin, hydrogenated Phospholipids such as lecithin; NMF-derived components such as lactic acid, sodium pyrrolidonecarboxylate, urea; polyglutamic acid; phospholipid polarities such as MPC polymers (eg LIPIDURE ™) Polyoxypropylene methyl glucoside; PPG-10 methyl glucose (for example, Macbiobride MG (trademark) series (manufactured by NOF Corporation)), PEG / PPG / polybutylene glycol-8 / 5/3 Glycerin (for example, Wilbride (trademark) S-753 (manufactured by NOF Corporation)); trimethylglycine (betaine); hydroxyethyl urea; acrylic acid / acrylamide / dimethyldiallylammonium chloride copolymer; petrolatum, squalane and the like.

  Of these, polyhydric alcohols such as glycerin, 1,3-butylene glycol, propylene glycol, dipropylene glycol, and diglycerin are preferred to give a moisturizing function and a moist use feeling, and glycerin is particularly preferred.

Although not limited, the content of the polyhydric alcohol with respect to the total amount of the composition for external use is preferably 0.01 w / w% or more and 20 w / w% or less, from the viewpoint of a balance between moist feeling and moisture retention, and 0.5 w / w % To 10 w / w% is more preferable, 2.0 w / w% to 8.0 w / w% is more preferable, 3.0 w / w% to 5.0 w / w% is particularly preferable. In addition, in this invention, a polyhydric alcohol component may be used individually by 1 type, or may be used in combination of 2 or more type.

  Ingredients having action of preventing and / or repairing DNA damage: components derived from animals (for example, Artemia); components derived from plants (for example, cat's claw); nucleic acid components such as DNA, DNA salts, RNA, RNA salts, etc. Such.

  Antibacterial components: chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, benzethonium chloride, cresol, gluconic acid and its derivatives, popidone iodine, potassium iodide, iodine, isopropylmethylphenol, triclocarban, triclosan, photosensitizer 101, photosensitizer 201 No., paraben, phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride and the like.

Astringent components: metal salts such as alum, chlorohydroxyaluminum, aluminum chloride, allantoin aluminum salt, zinc sulfate and aluminum potassium sulfate; organic acids such as tannic acid, citric acid, lactic acid and succinic acid.

[Other bases or carriers]
The composition for external use of the present invention can contain a known base or carrier used for cosmetics and quasi drugs as long as the effects of the present invention are not impaired. A base or a carrier can be used singly or in combination of two or more.

  Bases or carriers include paraffin, liquid paraffin, squalane, white wax, gelled hydrocarbons (plastibase, etc.), ozokerite, ceresin, petrolatum, hard fat, microcrystalline wax, α-olefin oligomer, light liquid paraffin, etc. Hydrocarbons; fatty acids such as lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, isostearic acid; such as glyceryl tri-2-ethylhexanoate (trioctanoin), tri (caprylic acid / capric acid) glyceryl Tri-fatty acid glycerides; higher alcohols such as cetanol, stearyl alcohol, behenyl alcohol; methylpolysiloxane, dimethylpolysiloxane (dimethicone), didemethylcyclopentasiloxane, methylsiloxane network Polymers, silicones such as methyl hydrogen polysiloxane; esters such as isopropyl myristate, octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, pentaerythrite tetra-2-ethylhexanoate A polysaccharide such as dextrin and maltodextrin; a lower alcohol such as ethanol and isopropanol; a glycol ether such as ethylene glycol monoethyl ether; and an aqueous base such as water.

  However, in the composition for external use of the present invention, the content of the lower alcohol is preferably smaller for reasons such as reducing irritation. For example, the external composition of the present invention preferably has an ethanol content of 10 w / w% or less, more preferably 8 w / w% or less, still more preferably 7 w / w% or less, even more preferably, based on the total amount of the external composition. May be 6 w / w% or less, most preferably 5 w / w% or less. In the composition for external use of the present invention, the ethanol content relative to the total amount of the composition for external use may be zero, 0.001 w / w% or more, 0.01 w / w% or more, or 0.1 w / w. % Or more.

  Among them, hydrocarbons (particularly α-olefin oligomers, squalane, light liquid paraffin, liquid paraffin), trifatty acid glycerides (particularly glyceryl tri-2-ethylhexanoate, tri (caprylic acid / capric acid) glyceryl), silicones Silicone oils, esters (especially isononyl isononanoate, pentaerythritol tetra-2-ethylhexanoate), polysaccharides other than acidic mucopolysaccharides (especially dextrin, maltodextrin), glycol ethers (especially diethylene glycol) Monoethyl ether) and water are preferred.

  The external composition of the present invention preferably contains silicone oil as a base. By containing silicone oil, foaming when using the composition for external use can be prevented, and the feeling of stopping the finger when applied to the skin can be prevented. As the silicone oil, methylpolysiloxane, ethyltrisiloxane, methyltrimethicone, methylsiloxane network polymer, polyoxyethylene / methylpolysiloxane copolymer, triethoxysilylethylpolydimethylsiloxyethylhexyl dimethicone, dimethylpolysiloxane are particularly preferable. Low viscosity such as siloxane, tristrimethylsiloxymethylsilane, caprylylmethicone, phenyltrimethicone, tetrakistrimethylsiloxysilane, methylphenylpolysiloxane, methylhexylpolysiloxane, methylhydrogenpolysiloxane, dimethylsiloxane / methylphenylsiloxane copolymer To high viscosity linear or branched organopolysiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxa Cyclic organopolysiloxanes such as dodecamethylcyclohexasiloxane, tetramethyltetrahydrogencyclotetrasiloxane, tetramethyltetraphenylcyclotetrasiloxane, amino-modified organopolysiloxane, pyrrolidone-modified organopolysiloxane, pyrrolidone carboxylic acid-modified organopolysiloxane, Silicone rubber such as gum dimethylpolysiloxane with high polymerization degree, gum-like amino-modified organopolysiloxane, gum-like dimethylsiloxane / methylphenylsiloxane copolymer, and cyclic organopolysiloxane solution of silicone gum or rubber, trimethylsiloxysilicate Acid, cyclic siloxane solution of trimethylsiloxysilicic acid, higher alkoxy modified silicone such as stearoxy silicone, higher fatty acid modified silicone, Alkyl-modified silicones, long chain alkyl-modified silicones, amino-modified silicones, fluorine-modified silicone, dissolution products of silicone resin and silicone resin and the like. In particular, methylpolysiloxane or dimethylpolysiloxane is preferably used.

  Among these, dimethylpolysiloxane is particularly preferable and is not limited. For example, specific examples include: Shin-Etsu Chemical Co., Ltd .: KF series (trade name), particularly KF-96A-2cs, KF-96A-5cs, KF- 96A-6cs, KF-96A-10cs, KF-96A-20cs, KF-96A-30cs, KF-96A-50cs, KF-96A-100cs, KF-96A-200cs, and the like.

The preferred viscosity of the silicone oil at 25 ° C. is 1 to 300 mm ² / s, more preferably ^{2 to} 200 mm ² / s. The preferred specific gravity at 25 ° C. of the silicone oil is about 0.85 to 0.97, and more preferably about 0.9 to 0.95. The preferable refractive index of the silicone oil at 25 ° C. is about 1.38 to 1.41, more preferably about 0.90 to 0.96.

  Although not limited, the content of the silicone oil relative to the total amount of the composition for external use is preferably 0.001 w / w% or more and 20 w / w% or less, preferably 0.01 w / w% or more, from the viewpoint of the balance between stickiness and moisture retention. 10 w / w% or less is more preferable, 0.1 w / w% or more and 8.0 w / w% or less is more preferable, and 1.0 w / w% or more and 5.0 w / w% or less is especially preferable. In addition, in this invention, a silicone oil component may be used individually by 1 type, or may be used in combination of 2 or more type.

  When the composition for external use of the present invention contains base water, the content of water is preferably 30 w / w% or more, more preferably 40 w / w% or more, and more preferably, based on the total amount of the composition for external use. Preferably, it is 50 w / w% or more, still more preferably 53 w / w% or more, more preferably 55 w / w% or more, and most preferably 60 w / w% or more. The content of water with respect to the total amount of the composition for external use of the present invention may be 99 w / w% or less, 95 w / w% or less, or 90 w / w% or less. The composition for external use of the present invention is most preferably an O / W emulsion composition containing 55 w / w% or more and 99 w / w% or less of water.

[Additive]
In the composition for external use of the present invention, known additives to be added to cosmetics and quasi-drugs, for example, surfactants, preservatives, pH adjusters, chelating agents, as long as the effects of the present invention are not impaired. Stabilizers, irritation reducers, preservatives, colorants and the like can be added. An additive can be used individually by 1 type or in combination of 2 or more types.

Examples of the surfactant include sorbitan distearate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexylate, di-2-tetrahexylhexylate Sorbitan fatty acid esters such as glycerol sorbitan; glyceryl monostearate, glyceryl fatty acid such as glyceryl monostearate malate; polyglyceryl fatty acids such as polyglyceryl monostearate, polyglyceryl monoisostearate, polyglyceryl diisostearate; mono Propylene glycol fatty acid esters such as propylene glycol stearate; polyoxyethylene hydrogenated castor oil 40 (HCO-40) Cured castor oil derivatives such as polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hydrogenated castor oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80; polyoxyethylene (20) sorbitan monolaurate (Polysorbate 20), polyoxyethylene (20) sorbitan monostearate (20) sorbitan (polysorbate 60), polyoxyethylene (20) sorbitan monooleate (polysorbate 80), polyoxyethylene (20) sorbitan isostearate Sorbitan fatty acid esters; polyoxyethylene monococonut oil fatty acid glyceryl; glycerin alkyl ether; alkyl glucoside; polyoxyalkylene alkyl ether such as polyoxyethylene cetyl ether Examples include amines such as stearylamine and oleylamine; silicone surfactants such as polyoxyethylene / methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, and PEG-9 polydimethylsiloxyethyl dimethicone. be able to.

  Among them, glycerin fatty acids (particularly glyceryl monostearate, glyceryl behenate), polyglycerin fatty acids (particularly polyglyceryl monostearate), hardened castor oil derivatives (particularly polyoxyethylene hardened castor oil 50 (HCO-50)) ), Polyoxyethylene hydrogenated castor oil 60 (HCO-60)), polyoxyethylene sorbitan fatty acid esters (especially polyoxyethylene (20) sorbitan isostearate, polyoxyethylene (20) sorbitan monostearate (polysorbate 60)) ), Polyoxyalkylene alkyl ether (especially polyoxyethylene cetyl ether), silicone surfactant (especially polyoxyethylene-methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxye) Dimethicone, PEG-9 polydimethylsiloxyethyl dimethicone) is preferred.

  The composition for external use of the present invention may be a composition containing no surfactant. Alternatively, the amount of the surfactant relative to the total amount of the external composition of the present invention is preferably 2 w / w% or less, more preferably 1 w / w% or less, and even more preferably 0.1 w / w% or less. it can. The amount of the surfactant relative to the total amount of the external composition of the present invention can be 0.0001 w / w% or more and 0.001 w / w% or more. In particular, depending on applications such as lotion, for example, a composition that does not contain a surfactant such as polyoxyethylene hydrogenated castor oil may be preferable due to the feeling of use.

  Preservatives and preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, paraoxybenzoic acid Examples thereof include benzyl, methyl paraoxybenzoate, and phenoxyethanol. Of these, methyl paraoxybenzoate, propyl paraoxybenzoate, and phenoxyethanol are preferable.

  Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, phosphoric acid, polyphosphoric acid, boric acid, etc.), organic acids (lactic acid, acetic acid, citric acid, sodium citrate, tartaric acid, malic acid, succinic acid, sodium succinate, Oxalic acid, gluconic acid, fumaric acid, propionic acid, acetic acid, aspartic acid, ε-aminocaproic acid, glutamic acid, aminoethylsulfonic acid, etc.), gluconolactone, ammonium acetate, inorganic base (sodium bicarbonate, sodium carbonate, hydroxylation) And potassium (sodium hydroxide, calcium hydroxide, magnesium hydroxide, etc.), organic bases (monoethanolamine, triethanolamine, diisopropanolamine, triisopropanolamine, lysine, etc.). Of these, succinic acid, sodium succinate, citric acid, sodium citrate, triethanolamine, potassium hydroxide, and sodium hydroxide are preferable.

  Chelating agents include ethylenediaminetetraacetic acid (edetic acid), ethylenediaminetetraacetic acid salt (sodium salt (sodium edetate: Japanese Pharmacopoeia, EDTA-2Na, etc.), potassium salt, etc.), phytic acid, gluconic acid, polyphosphoric acid, metalin Acids can be raised. Of these, sodium edetate is preferred.

  Examples of the stabilizer include butylhydroxyanisole.

  Examples of the irritation reducing agent include licorice extract, sodium alginate, 2-methacryloyloxyethyl phosphorylcholine and the like.

  Examples of the colorant include inorganic pigments and natural pigments.

[Production method]
The composition for external use of the present invention, for example, weighs an oil phase component (fatty acid and higher alcohol) and an aqueous phase component (components other than fatty acid and higher alcohol), for example, 50 ° C or higher, preferably 70 to 80 ° C. After heating, the aqueous phase component is gradually added to the oil phase component to emulsify, and the mixture is stirred to prepare a uniform composition.

[viscosity]
The composition for external use of the present invention can be prepared as a composition having an appropriate viscosity desired when using the composition for external use particularly used for application to hair and skin. The viscosity of the external composition of the present invention is not particularly limited. For example, the viscosity when measured at 25 ° C. using a B-type viscometer is usually about 100 to 300,000 mPa · s, preferably 100 to 100, It is about 000 mPa · s, more preferably about 200 to 50,000 mPa · s, and most preferably about 200 to 20,000 mPa · s. Depending on the application, it may be about 100 to 5,000 mPa · s. Even if the external composition of the present invention has a low viscosity of, for example, 20,000 mPa · s or less, it has an excellent moisture transpiration preventing action and can maintain a high moisturizing effect.

[pH]
Although the composition for external use of this invention should just be normally provided with the liquid property of pH 2-11, from a viewpoint of the mild irritation | stimulation with respect to skin and a mucous membrane, and a good feeling of use, Preferably it is pH 3-10, More preferably, it is pH 4- 9, particularly preferably pH 5-8.

[Usage]
Since the composition for external use of the present invention can be used as a pharmaceutical, quasi-drug or cosmetic with good moisturizing effect, it can be used for any skin external preparation or hair external preparation that is expected to have a moisturizing effect. Since the composition for external use of the present invention can be applied to the face, the periphery of the face, and the hair, it is particularly suitable for cosmetics and hair preparations.

  As the use of the composition for external use of the present invention, since the moisturizing effect is high, for example, treatment of symptoms caused by drying of skin and hair, prevention or amelioration use, imparting moisture, exerting a strong sealing force, water retention ability Examples thereof include imparting, imparting keratin flexibility, exhibiting the ability to retain moisture for a long time, and imparting skin to the skin. Specific examples of symptoms caused by dry skin include desquamation of the skin surface, dusting, bristle, roughness, cracks, scratches, keratinization of elbows, knees, heels and ankles, fine lines on the face, There are skin lines, reduced skin flexibility, finger tingling, itching, dry skin, sensitive skin, skin irritation, erythema, atopic skin, rough skin. Specific examples of symptoms caused by dry hair include dryness, dryness, split ends, and broken hair.

[Formulation]
Moreover, the composition for external use in this invention can be prepared by mixing and stirring each component according to a conventional method, for example.

  The form of the medicine in the composition for external use in the present invention is not particularly limited, and can take a form known as a form of cosmetics or quasi drugs. Among such known forms, for example, sheets for liquids, suspensions, emulsifiers, creams, gels, liniments, lotions, aerosols, powders, poultices, non-woven fabrics and the like for skin or hair Examples thereof include a sheet agent impregnated with a chemical solution, a stick agent such as a lipstick, and a spray agent. Especially, a liquid agent, a suspension agent, an emulsion, a cream agent, a gel agent, a lotion agent, and a spray agent are preferable and a liquid agent and a spray agent are more preferable at the point which is easy to use. The composition for external use of the present invention is preferably in the form of an aqueous solution, aqueous suspension, aqueous emulsion, aqueous gel, or aqueous lotion. Also, depending on the formulation, oil-in-water type (O / W), water-in-oil type (W / O) and the like can be appropriately selected according to the purpose of use and desired feeling of use. / W).

  The composition for external use of the present invention can be used in the form of a basic cosmetic product such as a skin emulsion, cream, lotion, body lotion, body cream. Or the composition for external use of this invention can also be used for the hair rinse, hair treatment, hair conditioner, hair gel, hair mousse, hair mist, hair lotion, hair oil, styling agent etc. for hair.

  The composition for external use of the present invention can be provided in the form of a foundation containing titanium oxide, for example, but is preferably provided in a form not containing titanium oxide.

EXAMPLES Next, the present invention will be specifically described with reference to examples, but the present invention is not limited to the following examples.
In addition, the unit of each component amount in Tables 2 to 5 and Table 8 is w / w%.

  External compositions having the compositions shown in Tables 2 to 5 were prepared according to a conventional method. Specifically, an oil phase component (fatty acid and higher alcohol) and an aqueous phase component (components other than fatty acid and higher alcohol) were weighed and heated to 70 ° C. Thereafter, the aqueous phase component was gradually added to the oil phase component to emulsify, and the mixture was stirred with a triple emulsion tester (Nikko Chemicals) to prepare a uniform composition.

[Evaluation of stability]
According to the compositions in Tables 2 to 5, 50 g of each of the prepared compositions for Examples 1 to 8 and Comparative Examples 1 to 7 was dispensed into a 50 mL headspace vial, sealed, and the stability immediately after production was confirmed. Observed. Here, “immediately after production” means a state within 60 minutes after preparation. Furthermore, it preserve | saved on each condition of the point shown in Table 1 about the composition for external use shown to Tables 2-3.

Stability immediately after production <Evaluation criteria>
5 points: not separated at all 4 points: hardly separated 3 points: somewhat separated 2 points: clearly separated 1 point: completely separated

Long-term storage stability

<Evaluation criteria>
A: Neither separation nor precipitation occurred under all the storage conditions shown in Table 1.
X: Separation and precipitation occurred at 60 ° C for 1 week.

The state of the composition was observed by visually observing the state in the sample before and after storage.
The results are shown in Tables 2 to 3, respectively.

[Usability test]
Applying the compositions for external use of Examples 1 to 4, Examples 6 to 8, or Comparative Examples 1 to 4 in the hands of healthy persons, Observation was made at the time of thirst after application, and the results were scored in five stages according to the following evaluation criteria. Tables 2 to 3 and Table 5 show the total of the scores and the evaluation results.

Evaluation during coating was performed as follows.
<Evaluation criteria>
"Usage"
5 points: easy to spread 4 points: easy to spread 3 points: slightly easy to spread 2 points: slightly difficult to spread 1 point: difficult to spread

Similarly, evaluation at the time of thirst after application was performed as follows.
<Evaluation criteria>
"Usage"
5 points: No squeaking 4 points: Less squeaking 3 points: Slight squeaking 2 points: Slight squeaking 1 point: Squeaking

  In addition, the use feeling score in the table is an average value of evaluation points during and after application.

[Irritation test]
The compositions for external use of Examples 1, 3, and 4 to 6 were applied to the hands of healthy persons, and the irritation was observed 2 minutes after the application, and the results were scored in 5 stages according to the following evaluation criteria. Tables 3 and 5 show the sum of the scores and the results of the evaluation.

[Viscosity and pH measurement]
The composition for external use immediately after the production was incubated at 25 ° C. for 1 hour, and then the viscosity and pH were measured. The viscosity was measured using VISCOMETER TV-10M (Toyo Sangyo) and STOP TIME was measured for 60 seconds as measurement conditions. ROTOR NO and SPEED are listed in Table 2. The pH was measured using pH METER F-52 (HORIBA).

As shown in the table, the examples showed good results.

Similarly, the compositions of Examples 6 to 8 shown in Table 5 were prepared and evaluated. However, with regard to long-term storage, a sample having no separation and precipitation in a state of 60 ° C. for one week was marked as “◯”.

[Measurement of moisture transpiration]
70 mg each of the composition for external use of Example 1, emulsion (manufactured by Rohto Pharmaceutical Co., Ltd.) and cream (manufactured by Rohto Pharmaceutical Co., Ltd.) was uniformly applied to a 28.6 mm size cellulose membrane (manufactured by Nippon Medical Science Co., Ltd.). Here, emulsions, including sodium hyaluronate and a higher alcohol, free of arginine or a salt or derivative thereof, are those not containing C ₁₀ -C ₂₄ saturated fatty acids. Here, cream, including higher alcohols, having no acidic mucopolysaccharides, arginine or a salt or derivative thereof, and a C ₁₀ -C ₂₄ saturated fatty acids. The cellulose membrane coated with the arginine derivative was attached to the mouth of a transparent vial (30 ml capacity) containing 10 ml of water, and left at 30 ° C. and 75% RH for 24 hours. After 24 hours, the amount of water transpiration was detected by measuring the amount of water in the vial. The results are shown in Table 6 in a ratio where the water transpiration amount in the case of no application is 100%. Each value was calculated according to the following formula.
(Equation 1) Relative ratio of moisture transpiration (%) = (moisture transpiration when each cosmetic is applied / water transpiration when not applied) x 100

For all items, the average number of samples N = 3.

Next, the external compositions of Examples 4 to 6, the emulsion (manufactured by Rohto Pharmaceutical Co., Ltd.), and the cream (manufactured by Rohto Pharmaceutical Co., Ltd.) were uniformly 70 mg each on a 28.6 mm cellulose membrane (manufactured by Nippon Medical Science Co., Ltd.) It applied one by one. Here, emulsions, including sodium hyaluronate and a higher alcohol, free of arginine or a salt or derivative thereof, are those not containing C ₁₀ -C ₂₄ saturated fatty acids. Here, cream, including higher alcohols, having no acidic mucopolysaccharides, arginine or a salt or derivative thereof, and a C ₁₀ -C ₂₄ saturated fatty acids. The cellulose film coated with the arginine derivative was attached to the mouth of a transparent vial (30 ml capacity) containing 10 ml of water, and left at 30 ° C. and 75% RH for 18 hours. After 18 hours, the amount of water transpiration was detected by measuring the amount of water in the vial. The results are shown in Table 7 in a ratio where the water transpiration amount in the case of no application is 100%. The calculation formula is the same as Formula 1. For all items, the average number of samples N = 3.

  As a result, it was found that the composition for external use of the present invention has a remarkable blocking effect both when compared with an emulsion and when compared with a general cream having a high viscosity.

[Prescription example]
Table 8 below shows formulation examples. Each of Formulation Examples 1 to 6 is an external composition for an O / W emulsion. The contents in the formulation examples are all w / w%.

(Table 8)
Formulation Example 1 (Lotion)
Allantoin 0.2
Tranexamic acid 2
Salicylic acid 0.05
1,3-butylene glycol 5
Dipropylene glycol 2
Palmitic acid 1.5
Arginine 0.5
Sodium hyaluronate 0.05
Cetanol 2.5
Inositol 0.1
Absolute ethanol 7
Hydrolyzed hyaluronic acid 0.05
Dimethylpolysiloxane 5
Diethoxyethyl succinate 0.5
Acetylated sodium hyaluronate 0.01
Polyethylene glycol 1540 1
Purified water Total remaining amount 100w / w%

Formulation Example 2 (Lotion)
3-O-Ethylascorbic acid 1
Glycerin 5
Dipropylene glycol 2
Stearic acid 1.5
Arginine 0.5
Sodium hyaluronate 0.1
Stearyl alcohol 2.5
Tocopherol 0.1
Absolute ethanol 5
Methyl polysiloxane 3
Polyoxypropylene methyl glucoside 0.5
Acetylated sodium hyaluronate 0.01
Polyethylene glycol 1500 1
Hydroxyethyl cellulose 0.05
Purified water Total remaining amount 100w / w%

Formulation Example 3 (Emulsion)
Dipotassium glycyrrhizinate 0.1
L-ascorbic acid 2-glucoside 2
Dipropylene glycol 3
Palmitic acid 1.3
Arginine 0.5
Sodium hyaluronate 0.05
Cetanol 2
Stearic acid 0.2
Stearyl alcohol 0.2
Carboxyvinyl polymer 0.2
Tocopherol 0.1
Dimethylpolysiloxane 3
Glyceryl tri-2-ethylhexanoate 1
Liquid paraffin 2
Squalane 1
Hydrolyzed hyaluronic acid 0.05
Absolute ethanol 5
Purified water Total remaining amount 100w / w%

Formulation Example 4 (Emulsion)
Dipropylene glycol 5
Palmitic acid 1.3
Arginine 0.5
Sodium alginate 0.1
Cetanol 2
Stearic acid 0.2
Stearyl alcohol 0.2
Carboxyvinyl polymer 0.2
Isononyl isononanoate 1
Methyl polysiloxane 3
Meadow foam oil 1
Liquid paraffin 2
Squalane 0.5
Behenyl alcohol 0.2
α-Olefin oligomer 0.5
Purified water Total remaining amount 100w / w%

Formulation Example 5 (Cream)
Tranexamic acid 2
Dipropylene glycol 4
Diglycerin 4
Palmitic acid 1.3
Sodium chloride 0.06
Arginine 0.5
Cetanol 2.5
Stearic acid 0.2
Stearyl alcohol 0.2
Carboxyvinyl polymer 0.1
Phytosterol 0.1
Dimethylpolysiloxane 1
Vaseline 4
Tri (Capryl / Caprin / Myristine / Stearin Sun) Glycerol 1
Collagen tripeptide F 0.1
Xanthan gum 0.1
Pullulan 0.5
Purified water Total remaining amount 100w / w%

Formulation Example 6 (Cream)
Epsilon-aminocaproic acid 0.1
Isopropylmethylphenol 0.1
Dipropylene glycol 5
Glycerin 2
Palmitic acid 1.3
Sodium hyaluronate 0.05
Arginine 0.5
Cetanol 2.5
Stearic acid 0.2
Stearyl alcohol 0.2
Carboxyvinyl polymer 0.1
Tocopherol 0.1
Dimethylpolysiloxane 3
Vaseline 3
Shea fat 1
Hydrolyzed hyaluronic acid 0.05
Absolute ethanol 5
Xanthan gum 0.1
Purified water Total remaining amount 100w / w%

Claims (9)

(A) acidic mucopolysaccharide,
_{(B) C} 10 ~C ₂₄ saturated fatty acids,
An external composition containing (C) a higher alcohol, and (D) arginine, an arginine derivative, and / or a salt thereof.   The external composition of Claim 1 whose viscosity in 25 degreeC is 100-300,000 mPa * s.   Furthermore, the composition for external use of Claim 1 or 2 containing 30 w / w% or more of water.   The acidic mucopolysaccharide is at least one selected from the group consisting of hyaluronic acid, alginic acid, hyaluronic acid derivative, alginic acid derivative, hyaluronic acid salt, alginic acid salt, hyaluronic acid derivative salt, and alginic acid derivative salt. The external composition of any one of Claims 1-3. The _C 10 _{-C 24} saturated fatty acid _is a C 16 _{-C 22} saturated fatty acid, any one composition for external use according to claims 1-4. It said higher alcohol _is a C 10 _{-C 24} fatty alcohols, any one composition for external use according to claims 1-5.   The arginine, arginine derivative, and / or salt thereof is L-arginine, D-arginine, L-arginine derivative, D-arginine derivative, L-arginine salt, D-arginine salt, L-arginine derivative salt, The composition for external use of any one of Claims 1-6 which is at least 1 sort (s) selected from the group which consists of a salt of D-arginine derivative.   The external composition of any one of Claims 1-7 whose content of the said acidic mucopolysaccharide is 0.001-1 w / w%. It is a manufacturing method of the external composition of any one of Claims 1-8,
(A) acidic mucopolysaccharide and (D) arginine, an arginine derivative heated to 50 ° C. or higher in a phase containing (B) a C ₁₀ -C ₂₄ saturated fatty acid heated to 50 ° C. or higher, and (C) a higher alcohol. The manufacturing method of the composition for external use including the process of adding the phase containing the salt / or those.