JP2010189327A - Lactate formation promoter and skin cosmetic formulated with the formation promoter - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a skin cosmetic which moisturizes the skin not by imparting pseudo moisture thereto by using an external additive component using a moisturizer such as a polyhydric alcohol but by increasing the formation of a lactate, especially magnesium lactate, itself as a natural moisturizing factor inherent in the skin. <P>SOLUTION: A lactate formation promoter including urea and at least one member selected from the group consisting of sulfated polysaccharides, desirably chondroitin sulfate, dermatan sulfate and salts thereof is provided. The skin cosmetic includes the promoter. <P>COPYRIGHT: (C)2010,JPO&amp;INPIT

Description

  The present invention relates to a lactate production accelerator and a skin cosmetic comprising the production accelerator.

  The skin is continuously damaged by external factors such as ultraviolet rays and dryness. When these damages accumulate, the skin condition with fine moisture like that of baby's skin is lost, and the skin condition becomes dry with no moisture, resulting in a rough skin condition.

  Conventionally, polyhydric alcohols such as glycerin and 1,3-butylene glycol; sugar alcohols such as sorbitol, maltitol, xylitol, and erythritol; monosaccharides and polysaccharides Attempts have been made to impart moisture with various moisturizing agents such as hyaluronic acid, collagen, and plant extracts. For example, a skin external preparation containing a plant extract and a moisturizing agent such as hyaluronic acid (for example, see Patent Document 1), a skin external preparation containing a specific plant extract and a polyhydric alcohol (for example, Patent Document 2) Have been proposed).

  However, these moisturizers can be instantly moisturized, but because they are pseudo external additive components, if the moisturizer is highly blended to increase the moisturizing effect, the feeling of use such as stickiness will deteriorate. There's a problem. In addition, there is a problem that sufficient moisture cannot be imparted if the blending is low to reduce the sticky feeling.

  On the other hand, in the skin, amino acids such as serine, glycine, alanine and threonine; lactates such as magnesium lactate, potassium lactate and sodium lactate; urea; citrates such as sodium citrate; pyrrolidones such as sodium pyrrolidone carboxylate There exists a substance that retains moisture, called natural moisturizing factor (NMF), such as carboxylate. These substances have a function of suppressing moisture loss due to damage such as ultraviolet rays and drying, and maintaining a moist skin condition. Among them, lactate is said to be a natural (natural) moisturizing factor that also affects the pH in the skin and has an excellent water retention function.

  Therefore, attempts have been made to add moisture by blending the above-mentioned natural (natural) moisturizing factor into cosmetics. For example, a skin external preparation containing a specific fungal bed extract and a natural moisturizing factor (for example, see Patent Document 3), a skin care composition containing a polyhydric alcohol and a natural moisturizing factor (for example, Patent Document 4) Have been proposed).

  However, although it is possible to give a certain amount of moisture through these trials, there is a problem that the feeling of use is deteriorated and a sufficient effect cannot be expected because it is a pseudo moisture like the above moisturizing agent.

  Thus, conventionally used means for imparting moisture is pseudo-moisture imparting by an external additive component, and does not enhance the moisture retention function inherent to the skin. Therefore, the functions and trials required in the future are to try to enhance the moisture retention function inherent in the skin, that is, to develop a skin cosmetic that has the function of maintaining a moist skin condition by increasing the production of lactate itself. It is.

JP 2000-119155 A Japanese Patent Laid-Open No. 2002-154921 JP 2006-282596 A JP 2006-526570 A

  The present invention has been made in view of the above prior art, and is a natural (natural) moisturizing factor inherent in the skin, not artificial moisturizing by an external additional component using a moisturizing agent such as a polyhydric alcohol. It is an object to provide a skin cosmetic that leads to a moist skin condition by increasing the production of a certain lactate salt itself.

That is, the present invention
[1] Lactate production promoter containing urea and sulfated polysaccharide,
[2] The lactate production promoter according to [1], wherein the sulfated polysaccharide is at least one selected from the group consisting of chondroitin sulfate, dermatan sulfate, and salts thereof,
[3] The skin cosmetic comprising the lactate production promoter according to [1] or [2], and [4] a cosmetic for improving rough skin, Relating to skin cosmetics.

  Since the lactate production promoter of the present invention contains urea and sulfated polysaccharide as active ingredients, it can synergistically promote the production of lactate in the skin, especially magnesium lactate.

  Further, since the skin cosmetic of the present invention contains urea and sulfated polysaccharides as lactate production promoters, it synergistically promotes the production of lactate in the skin and reduces transdermal water loss (TWL). Since it suppresses, there exists an effect that it can lead to a moist skin state by suppressing rust.

It is a figure showing the test result of a skin moisturizing effect.

  Hereinafter, the lactate production promoter according to the present invention will be described in detail. The lactate production promoter of the present invention contains urea and sulfated polysaccharide as active ingredients.

  Urea will not be specifically limited if it is normally used for cosmetics and a quasi-drug. Examples of commercially available products include Proticute U Alpha (trade name, manufactured by Ichimaru Falcos); Hygroplex HHG, Cefplant Complex (trade names, both manufactured by Kotobuki Chemical); HYDROVITON 24 (trade name, Simrise); Examples include Complex (trade name, manufactured by Nikko Chemicals).

  The sulfated polysaccharide is, for example, D-glucosamine, D-galactosamine, D-glucuronic acid, L-iduronic acid, D-galacturon, in which the constituting monosaccharide may have a modifying group such as an acetyl group. The polysaccharide is composed of acid, D-glucose, D-galactose, D-xylose and the like, and is a sulfated polysaccharide composed of one or more of these. The sulfated polysaccharide used in the present invention also includes a polysulfated polysaccharide obtained by further sulfating a polysaccharide already having a sulfate group in nature.

  Specific sulfated polysaccharides include, for example, heparin, heparan sulfate, chitin sulfate, chitosan sulfate, ketalan sulfate, dermatan sulfate, pectin sulfate, galactan sulfate, polyglucose sulfate, chondroitin sulfate, sulfated trehalose, fucoidan, and Examples thereof include polysulfur oxides obtained by further sulfating them. One of these components may be used alone, or two or more thereof may be used in appropriate combination.

  Moreover, in this invention, it can also use as a salt of the above-mentioned sulfated polysaccharide and the polysulfur oxide obtained by further sulfation. Examples of the salt to be used include alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt and magnesium salt.

  As a suitable sulfated polysaccharide, it is preferable to use chondroitin sulfate, dermatan sulfate, and salts thereof from the viewpoint of exerting a desired effect. In addition, a commercial item can be used for the sulfated polysaccharide used for this invention as it is. As a commercial product of chondroitin sulfate, for example, sodium chondroitin sulfate (trade name, manufactured by Wako Pure Chemical Industries, Ltd.), and as a commercial product of dermatan sulfate, for example, Chondroitin sulfate B sodium salt (trade name, Sigma Aldrich Japan) For example).

  In the lactate production promoter according to the present invention, the contents of urea and sulfated polysaccharide are not particularly limited, but from the viewpoint of synergistically promoting the production of lactate, the weight ratio (urea / sulfated polysaccharide) So as to be 1/1 to 1/10, preferably 1/1 to 1/5, more preferably 1/1 to 1/2.

  The lactate production promotion effect exhibited by the combined use of urea and sulfated polysaccharides is not just an additive effect, but an unexpected level of production, in contrast to the individual lactate production promotion effect. Since it has an accelerating effect, loss of transdermal moisture can be suppressed, leading to a moist skin condition.

  The above-described lactate production promoter of the present invention can be used by blending it with skin cosmetics. Specifically, it can be applied to various dosage forms such as lotions, essences, creams, emulsions, gels, etc., and is used for skin cosmetics such as lotions, emulsions, skin creams, cosmetics, facial cleansers, after-shave lotions, etc. be able to. Especially, since it leads to a moistened skin state by suppressing the roughness, it can be suitably used as a skin cosmetic that improves rough skin.

  When preparing a skin cosmetic using the lactate production accelerator of the present invention, within the range not impairing the effects of the present invention, in addition to the above-described components, components usually used for cosmetics and quasi drugs, For example, oily components such as fats and oils, waxes, hydrocarbons, silicones, fatty acid esters, higher alcohols, higher fatty acids; nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants Surfactants; alcohols such as lower alcohols, polyhydric alcohols, saccharides and sterols; thickening polymers such as viscosity minerals and water-soluble polysaccharides; antioxidants; ultraviolet absorbers; sequestering agents; Additives such as polymer compounds, inorganic pigments, powders, pigments, pigments, dyes, vitamins, amino acids, astringents, whitening agents, animal and plant extracts, acids, alkalis, etc., depending on the purpose It can be Yibin arbitrarily blended.

  Specifically, examples of oil components include oils and fats such as olive oil, camellia oil, macadamia nut oil and avocado oil; waxes such as carnauba wax, candelilla wax, jojoba oil, beeswax and lanolin; liquid paraffin, paraffin, petrolatum, Hydrocarbons such as ceresin, microcrystalline wax, squalene, squalane; methylpolysiloxane, methylphenylpolysiloxane, methylcyclopolysiloxane, octamethylcyclotetrasiloxane, octamethylcyclopentasiloxane, decamethylcyclopentasiloxane, methylhydrogenpoly Silicones such as siloxane; isopropyl myristate, 2-octyldodecyl myristate, cetyl 2-ethylhexanoate, 2-ethylhexyl palmitate, di-2-ethyl Neopentyl glycol xanthate, glycerol tri-2-ethylhexanoate, 2-octyldodecyl oleate, glycerol triisostearate, glycerol tri-2-ethylhexanoate, 2-octyldodecyl oleate, diisostearyl malate, tri Fatty acid esters such as glycerol isostearate and 2-ethylhexanoic acid diglyceride; higher alcohols such as cetyl alcohol, stearyl alcohol, isostearyl alcohol, 2-octyldodecanol and oleyl alcohol; lauric acid, myristic acid, palmitic acid, stearic acid And higher fatty acids such as isostearic acid and oleic acid.

  Surfactants include sorbitan fatty acid ester, glycerin fatty acid ester, castor oil, hydrogenated castor oil and their alkylene oxide adducts, polyglycerin fatty acid ester, polyoxyalkylene alkyl ether, polyoxyalkylene fatty acid ester, polyoxyalkylene alkylphenol, Nonionic surfactants such as polyoxyethylene sorbite fatty acid ester, polyoxyethylene alkylphenyl formaldehyde condensate, polyoxyethylene sterol and its derivatives, polyoxyethylene lanolin and its derivatives, polyoxyethylene beeswax derivatives, sugar esters, etc. Fatty acid soap, alkyl sulfate ester salt, alkyl phosphate, polyoxyethylene alkyl ether sulfate, polyoxyethylene Alkyl phenyl ether sulfate, alkyl ether phosphate, alkyl ether carboxylate, acylmethyl taurate, N-acyl-N-methyl-β-alanine, N-acyl glycine, N-acyl glutamate, polyoxy Anionic surfactants such as ethylene alkylcarboxylate, alkylphenyl ether sulfonate, alkylsulfosuccinic acid and salts thereof, N-acyl sarcosine and salts thereof, polyoxyethylene coconut oil fatty acid monoethanolamide sulfate; alkylamine salts , Fatty acid amide amine salts, amine salts such as ester-containing tertiary amine salts, monoalkyl type quaternary ammonium salts, dialkyl type quaternary ammonium salts, trialkyl type quaternary ammonium salts, alkyl such as benzalkonium type quaternary ammonium salts 4 Cationic surfactants such as quaternary ammonium salts such as quaternary ammonium salts and alkylpyridinium salts, benzethonium chloride; alkyl glycine salts, carboxymethyl glycine salts, N-acylaminoethyl-N-2-hydroxyethyl glycine salts, etc. Glycine-type amphoteric surfactants, amino-propionic acid-type amphoteric surfactants such as alkylaminopropionate and alkyliminodipropionate, beta-amino acids such as alkyldimethylaminoacetic acid betaine and fatty acid amidopropyldimethylaminoacetic acid betaine Examples of amphoteric surfactants include amphoteric surfactants and sulfobetaine-type amphoteric surfactants such as alkylhydroxysulfobetaine.

  Examples of alcohols include lower alcohols such as ethanol, isopropanol, and butanol; 1,3-butanediol, glycerin, diglycerin, polyglycerin, ethylene glycol, polyethylene glycol, polypropylene glycol, 1,2-pentanediol, 1, Polyhydric alcohols such as 2-hexanediol, 1,2-heptanediol, 1,2-octanediol, 1,2-nonanediol, 1,2-decanediol; sorbitol, mannitol, glucose, sucrose, xylitol, Examples include saccharides such as lactose and trehalose; sterols such as cholesterol and phytosterol.

  As the thickening polymer, for example, bentonite, smectite, beidellite, nontronite, saponite, hectorite, soconite, stevensite, and other viscous minerals; carrageenan, guar gum, xanthan gum, gum arabic, Examples thereof include karaya gum, tragacanth gum, dextran, amylose, amylopectin, agarose, pullulan, sodium pectate, alginic acid, methylcellulose, ethylcellulose, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, and the like.

  Examples of antioxidants include ascorbic acid and / or derivatives thereof, triterpenes, tocopherol, tocopherol acetate, astaxanthin, coenzyme Q10, platinum colloid, and the like.

  Specific examples of the ascorbic acid derivative include, for example, ascorbic acid sodium salt, ascorbic acid potassium salt, divalent metal salt ascorbic acid magnesium salt, ascorbic acid calcium salt, which is a monovalent metal salt of ascorbic acid, 3 Ascorbic acid aluminum salt which is a valent metal salt; Ascorbic acid phosphate sodium salt, ascorbic acid phosphate potassium salt which is a monovalent metal salt of ascorbic acid phosphate ester, Ascorbic acid phosphate magnesium which is a divalent metal salt Salt, ascorbic acid phosphate calcium calcium salt, trivalent metal salt ascorbic acid phosphate aluminum salt; ascorbic acid sulfate sodium salt, ascorbic acid sulfate sodium salt, ascorbic acid sulfate potassium Salts, divalent ascorbic acid sulfate ester magnesium salt is a metal salt, ascorbic acid sulfate ester calcium salt, can be exemplified as ascorbic acid sulfate ester aluminum salt is trivalent metal salt.

  Examples of the triterpenes include squalene, saponin, limonin, cameliagenin, hopane, lanosterol, facyclol, ursolic acid, oleonolic acid, and betulinic acid.

  Examples of the ultraviolet absorber include benzoic acid-based ultraviolet absorbers such as paraaminobenzoic acid and paraaminobenzoic acid monoglycerin ester; anthranilic acid-based ultraviolet absorbers such as methyl anthranilate and homomenthyl-N-acetylanthranilate; methyl salicylate Salicylic acid UV absorbers such as: octyl paramethoxycinnamate, cinnamate UV absorbers such as ethyl-4-isopropylcinnamate; benzophenone UV absorbers such as 2,4-dihydroxybenzophenone; amyl salicylate, menthyl Examples include salicylic acid-based UV absorbers such as salicylate and benzyl salicylate; urocanic acid-based UV absorbers such as urocanic acid and ethyl urocanate.

  Examples of the sequestering agent include edetate, phosphoric acid, sodium polyphosphate, sodium metaphosphate, alanine, sodium oxalate, nitrilotriacetic acid, 1,2-diaminocyclohexane-tetraacetic acid, N-oxyethylethylenediamine- Triacetic acid, ethylene glycol bis-tetraacetic acid, ethylenediamine-tetrapropionic acid, 1-hydroxyhexane-1,1-diphosphonic acid, phosphonoacetic acid, diethylenetriaminepentaacetic acid, 1,2-cyclohexanediaminetetraacetic acid, ethylenediaminediacetic acid, triethylene Examples thereof include tetramine hexaacetic acid.

  The blending amount of the lactate production promoter to the skin cosmetic of the present invention is not particularly limited as long as the desired effect is sufficiently imparted, but is preferably 0.1 to 5% by weight in the cosmetic. Preferably it is 0.5 to 3 weight%. If it is less than 0.1%, it is inferior in the effect of promoting the formation of lactate, inferior in leading to a moist skin condition, and when it exceeds 5% by weight, not only a further effect cannot be expected, It is not preferable because the feeling of use is inferior.

  EXAMPLES Hereinafter, although this invention is demonstrated further in detail based on an Example, this invention is not limited only to these Examples. The blending amount represents “% by weight” unless otherwise specified. The measurement was performed under conditions of room temperature 23 ° C. and humidity 60%.

(Sample preparation)
According to the composition described in Table 1 and Table 2, each sample of Examples 1-4 and Comparative Examples 1-4 was prepared, and it used for the following evaluation.

(Test Example 1: Lactate salt formation promoting effect test)
A total of 10 marks (5 on one arm x 2: both arms) were placed on the inner side of the upper arm of 10 subjects. Next, 50 μL of each sample of the example and the comparative example was applied to a place excluding one place (one arm) as a comparative control, allowed to acclimate, and then allowed to stand for 30 minutes and dried. After leaving for 30 minutes, tape stripping was performed once to remove the stratum corneum, followed by extraction with 50 μL of water and quantitative analysis of magnesium lactate using ODS-HPLC.
In addition, the comparative part which is not applied with the data was also extracted in the same manner as described above and subjected to quantitative analysis.

(HPLC measurement conditions)
Equipment: SHIMADZU classLC-10
Column: Intersil ODS-3
Column temperature: 45 ° C
Flow rate: 0.4 mL / min
Injection volume: 20 μL
Detection: 210nm
Moving layer: 0.1M NH ₄ H ₂ PO ₄ + H ₃ PO ₄ (pH 2.5)

  The lactate production promotion rate (%) was calculated by setting the quantitative value of lactate in the comparison control (average value of two locations on both arms) to 100% of the production rate of magnesium lactate, and calculating the quantitative value of magnesium lactate in each sample application part. . Each lactate production promotion rate (%) was calculated from an average value of 10 subjects and evaluated according to the following calculation criteria. The results are shown in Tables 1 and 2.

◎: Lactate production promotion rate is 200% or more ○: Lactate production promotion rate is 150% to less than 200% Δ; Lactate production promotion rate is 100% to less than 150% ×: Lactate production promotion The rate is 50% or more and less than 100%

(Test Example 2: Transdermal moisture loss (TWL) suppression effect test)
About 1 mL of each sample of Examples and Comparative Examples was continuously applied to 10 subjects twice a morning and evening for 4 weeks, and TWL values before and after application were measured by a device for measuring skin moisture transpiration (TEWAMETER TM210 type; (Courage + Khazaka electronic). The reduction rate of the TWL value was calculated as follows, and the effect of suppressing transdermal water loss was evaluated according to the following evaluation criteria. The results are shown in Tables 1 and 2.

The reduction rate of the TWL value was calculated by substituting the TWL value before and after the sample application, that is, the TWL value (T ₀ ) before the sample application and the TWL value (T ₁ ) after the sample application into the following equation. In addition, the case where the reduction rate of the TWL value was 20% or more was evaluated as “effective”.

Reduction rate of TWL value (%) = (1−T ₁ / T ₀ ) × 100

<Evaluation criteria>
◎; Nine out of 10 people are “valid”
○: 6 to 8 out of 10 people are “valid”
Δ: 3 to 5 out of 10 people are “valid”
×: 2 or less of 10 people are “valid”

(Test Example 3; skin moisturizing effect test)
The skin moisturizing effect of each sample of Examples and Comparative Examples was evaluated by 10 subjects. That is, the face of each subject was washed with warm water using a facial cleanser and allowed to rest in a constant temperature and humidity room at a temperature of 21 ± 2 ° C. and a humidity of 50 ± 5% for 15 minutes. Was measured with a skin surface horn layer water content measuring device (SKICON-200EX type; manufactured by IBI S Co., Ltd.). The measurement is to measure the initial value of the skin moisture content, apply each sample of Example and Comparative Example after 30 minutes, measure each skin moisture content after 30 minutes, 3 hours and 6 hours after application, The average value was adopted. The results are shown in FIG.

(Test Example 4: Skin roughness improvement effect test)
About 1 mL of each sample of Examples and Comparative Examples was applied twice a morning and evening to 10 female subjects suffering from rough skin for 4 weeks in succession, and the skin condition after 4 weeks was observed with a microscope. The improvement effect was evaluated according to the following evaluation criteria. The results are shown in Tables 1 and 2.

<Evaluation criteria>
◎: Improved to normal skin with no desquamation and fine mesh texture ○: Improved to almost normal skin with mesh texture △; Slightly improved ×: Clearly There is desquamation and it is not improved at all

  From the results shown in Tables 1 and 2, since the lactate production promoter of the present invention contains urea and sulfated polysaccharide as active ingredients, it synergistically promotes the production of magnesium lactate in the skin. It can be seen that it has the effects of reducing transdermal moisture loss (TWL), reducing rustiness, leading to a moist skin condition, and improving rough skin.

  Hereinafter, the formulation example of the skin external preparation composition which concerns on this invention is shown. The content is% by weight.

(Formulation example 1; emollient lotion)
Ethanol 5.0
POE (50) hydrogenated castor oil 1.0
Glycerin 15.0
1,3-butylene glycol 1.5
1,2-octanediol 0.1
Urea 0.3
Sodium chondroitin sulfate 0.3
Coenzyme Q10 0.01
Citric acid 0.05
Sodium citrate 0.1
Methylparaben 0.3
Perfume appropriate amount UV absorber appropriate amount
Purified water balance part Total 100.0

(Formulation example 2; emollient emulsion)
Liquid paraffin 15.0
Beeswax 2.0
Lanolin 1.5
Sorbitan sesquioleate 2.5
Polyoxyethylene sorbitan monooleate 1.0
1,2-hexanediol 1.0
Urea 0.5
1,2-octanediol 0.05
Glycerin 10.0
Sodium dermatan sulfate 0.5
1,3-butylene glycol 3.0
Xanthan gum 0.5
Coenzyme Q10 0.03
Perfume appropriate amount UV absorber appropriate amount
Purified water balance part Total 100.0

(Formulation example 3; emollient cream)
Stearyl alcohol 5.0
Stearic acid 2.0
Vaseline 5.0
Squalane 5.0
Glyceryl tri-2-ethylhexanoate 1.0
Jojoba oil 1.0
Olive oil 1.0
1,3-butylene glycol 3.0
1,2-pentanediol 3.0
1,2-octanediol 0.05
Glycerin 10.0
Urea 1.0
Sodium chondroitin sulfate 1.0
Coenzyme Q10 0.03
Propylene glycol monostearate 2.5
Polyoxyethylene cetyl ether 3.0
Triethanolamine 1.0
Methylparaben 0.15
Propylparaben 0.1
Perfume appropriate amount Antioxidant appropriate amount
Purified water balance part Total 100.0

(Formulation example 4: massage cream)
Solid paraffin 5.0
Beeswah 8.0
Vaseline 8.0
Liquid paraffin 30.0
Glyceryl tri-2-ethylhexanoate 1.0
Jojoba oil 1.0
Olive oil 1.0
1,2-octanediol 0.15
Glycerin 10.0
Urea 0.25
Coenzyme Q10 0.03
Sodium dermatan sulfate 0.5
Polyoxyethylene sorbitan monolaurate 2.0
Glyceryl monostearate 1.6
Methylparaben 0.15
Propylparaben 0.15
Perfume appropriate amount Antioxidant appropriate amount
Purified water balance part Total 100.0

Claims (4)

  A lactate production accelerator comprising urea and a sulfated polysaccharide.   The lactate production promoter according to claim 1, wherein the sulfated polysaccharide is at least one selected from the group consisting of chondroitin sulfate, dermatan sulfate, and salts thereof.   A skin cosmetic comprising the lactate production promoter according to claim 1 or 2.   The skin cosmetic according to claim 3, which is a skin roughening cosmetic.

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