KR100681701B1 - Cosmetic composition for alleviating acne comprising hexanoyltripeptide as active ingredient - Google Patents

Abstract

A cosmetic composition is provided to show hyperkeratinization inhibition effect, comedo formation inhibition effect and alleviation effect by comprising hexanoyl tripeptide, thereby being effectively used for preventing, treating, improving and alleviating acne. The cosmetic composition for improving and alleviating acne comprises hexanoyl tripeptide as an effective ingredient. In the composition, the hexanoyl tripeptide is a peptide(Arg-Ala-Nle)-NH2 acetate salt represented by a hexanoyl-SEQ ID : NO. 1. Regarding the total weight of the composition, 0.0005-20.0 wt.% of the hexanoyl tripeptide is contained.

Description

Cosmetic composition for alleviating acne containing hexanoyl tripeptide as an active ingredient {Cosmetic Composition for alleviating Acne Comprising Hexanoyltripeptide as Active Ingredient}

The present invention relates to a cosmetic composition for acne relief and improvement.

In general, sebum is responsible for keeping the skin moisturized and microbes invading the skin, including the scalp and face, but it is a major cause of acne after puberty. In particular, women in their 20s and later cause a lot of problems in terms of beauty, such as skin lingering, makeup lifting and pores widening due to the excessive secretion of sebum. The combination of other factors in the excessive secretion of sebum causes acne. In general, the occurrence of acne is known to be caused by a complex action, such as sebum oversecretion due to the action of male hormones, keratinocyte hyperkeratosis in the sebaceous gland, and the involvement of Propionibacterium Acnes . Abnormal hyperkeratosis of the inner wall of sebaceous glands in the sebaceous gland causes thickening of the inner wall of the sebaceous gland, preventing the sebaceous glands from secreting the sebum. If sebum is not secreted and remains in the sebaceous gland, the growth of acne bacteria present in the sebaceous gland increases, which causes triglyceride, which is composed of acne, to be converted into free fatty acid and acts as an irritant. Or, it acts as a comedonogenic substance to promote acne production. It also progresses further and involves inflammatory reactions. By suppressing abnormal hyperkeratosis of the inner wall of the sebaceous glands in the sebaceous glands which are the cause of acne can be expected to suppress and relieve acne.

The stratum corneum is keratinocyte keratinocytes keratinocytes, dead cells are flattened keratinocyte cells are closely stacked about 10 or more layers, the thickness is about 20㎛. The cells of the stratum corneum are filled with intercellular lipids having a layered structure of sphingolipids, cholesterol, and fatty acids secreted from the lamellar granules in the keratinocytes of the epidermal layer. Cells and cells are tightly linked through glycoproteins, a cell adhesion factor called desmosomes.

The present inventors screened a substance having excellent acne alleviation and amelioration effect, and as a result, hexanoyl tripeptides have exfoliation effect, scavenge formation and restorative effect in experimental animals, and finally acne alleviation in volunteers who own actual acne. The effect was remarkable to complete the present invention.

Accordingly, it is an object of the present invention to provide a cosmetic composition for acne relief and improvement containing hexanoyl tripeptide as an active ingredient.

Other objects and advantages of the present invention will become apparent from the following examples and claims.

The present invention relates to a cosmetic composition for improving and alleviating acne containing hexanoyl tripeptide as an active ingredient.

“Acne” to which the composition of the present invention is applied includes any skin disease in the art, or any skin disease invented through a mechanism similar to acne, for example, collective acne, acne caused by bromide, general acne, Congoblate acne, acne from cosmetic use, acne dtergicans, adolescent acne, acne fulminans, acne furunculoid, acne caused by halogen, callous acne, Keloid acne, physical acne (mechanical acne), drug acne, necrotic acne, lip acne, acne neonatorum, acne oil, papule acne, pomade acne, Premenstrual acne, acne rosacea, swelling acne, tropical acne, addictive acne venenata, and vulgar acne Include.

In the cosmetic composition of the present invention, "hexanoyl tripeptide" used as an active ingredient showing an acne alleviating effect is linked to three peptides (arginine-alanine-norleucine) represented by SEQ ID NO: 1 at the end of the hexanoyl group. It refers to the structure in which the amide acetate salt is linked to the peptide, that is, Hexanoyl-Arg-Ala-Nle-NH ₂ Acetate Salt. The hexanoyl tripeptides of the present invention weaken the connection of a protein called desmosome that connects keratinocytes to help the aged keratin fall off naturally. Desmosomes consist of heterozygous bonds between two cells, called Cell Adhesion Recognition (Desmoglein) and Desmocollin (Desmocollin). The Arg-Ala-Nle tripeptide (SEQ ID NO: 1) portion of “hexanoyl tripeptide” binds to the cell adhesion recognition site of desmocoline and consequently binds to the cell adhesion recognition site of desmocholine. It weakens and speeds up skin renewal safely without skin irritation.

According to a preferred embodiment of the present invention, hexanoyl tripeptide used as an active ingredient in the cosmetic composition is excellent in the exfoliation effect of the skin, it is excellent in inhibiting the formation of scrim formed before the inflammation of acne. In addition, it also shows an acne improvement effect on actual acne patients (see Experimental Examples 1 to 4). That is, the inner wall of the sebaceous gland is thickened by abnormal hyperkeratinization of the sebaceous gland in the sebaceous gland, so that the sebaceous glands are blocked, and as sebum is continuously accumulated in the sebaceous gland, acne occurs. The cosmetic composition of hexanoyl tripeptide having excellent exfoliation effect by inhibiting abnormal hyperkeratosis prevents sebum produced in the sebaceous gland to delay acne development and improve and alleviate acne. In addition, due to the cotton-causing substance is accompanied by an inflammatory response to promote acne production, the cosmetic composition of the present invention can exhibit an excellent acne relief effect and improvement effect by containing hexanoyl tripeptipeptide excellent in scleroform inhibition effect. .

According to a preferred embodiment of the present invention, the content of hexanoyl tripeptide included as an active ingredient in the cosmetic composition is 0.0005-20.0% by weight based on the total weight of the cosmetic composition, more preferably 0.001-10.0% by weight.

In this case, when the content of hexanoyl tripeptide is less than 0.0005% by weight, the whitening effect is less likely to occur, and when the content of the ingredient is 10.0% by weight and 10.0 ppm or more, the skin is highly likely to cause irritation and has a great effect on the stabilization of the formulation. Can be crazy

The cosmetic composition of the present invention may further include a component exhibiting an exfoliation effect, a component exhibiting an anti-follicle formation effect, in addition to hexanoyl tripeptide having an excellent acne improving effect.

Cosmetic compositions of the present invention may be prepared in any formulation conventionally prepared in the art and include, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing , Oils, powder foundations, emulsion foundations, wax foundations and sprays, and the like, but are not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, nutrition lotion, nutrition cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder.

The cosmetic composition of the present invention includes components commonly used in cosmetic compositions in addition to hexanoyl tripeptides, which are included as active ingredients, and include, for example, conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments and flavorings, and Carrier.

When the formulation of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, trakant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide, etc. may be used as carrier components. Can be.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, in particular in the case of a spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizing agent or emulsifying agent is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethyleneglycol or sorbitan.

When the formulation of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystals Soluble cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is a surfactant-containing cleansing, the carrier component is aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide. Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

Hereinafter, the present invention will be described in more detail through experimental examples. These examples are only for illustrating the present invention in more detail, and the scope of the present invention is not limited by these examples in accordance with the gist of the present invention to those skilled in the art. Will be self-evident.

Experimental Example 1 Exfoliation Effect of Hexanoyl Tripeptide

All the cells that make up the experimental skin are continuously produced during the life of the living body, die after the proper metabolic process, and are separated into the skin. In order to maintain skin homeostasis, the rate of cell production and detachment is kept constant. . Therefore, in general, the regeneration rate of the skin can be indirectly measured by measuring the rate at which the stratum corneum is peeled off, and the peeling rate of the skin is measured by measuring the degree of discoloration of the skin according to the exfoliation of the skin. The discoloration of the skin was using dihydroxyacetone (DHA), which is used in self-tanning products.

Twenty men and women with relatively light skin color were selected from mid-twenties to early thirties. After measuring the brightness of the skin with a colorimeter before starting the experiment, the skin was colored by applying 10% dihydroxyacetone solution twice a day. After coloring the skin, hexanoyl tripeptides (Mibelle, Switzerland) were prepared at concentrations of 1% and 2%, respectively, and applied twice a day, and then measured at 3 days, 6 days, 8 days and 10 days with a colorimeter. . After the application of dihydroxy acetone, tanning was completely made 100, and the extent of exfoliation with time was calculated in terms of% according to Equation 1 below.

division Exfoliation effect (%) 3 days 6 days 9th 12 days 15th Control 15.72 24.73 32.97 43.25 52.80 Hexanoyl Tripeptide 1% 15.36 25.71 52.96 68.39 84.67 Hexanoyl Tripeptide 2% 14.86 26.71 59.78 74.67 95.50

As shown in Table 1, while the normal state showed a 50% exfoliation effect after 15 days, 2% hexanoyl tripeptides showed more than 95% exfoliation effect, hexanoyl tripeptides The exfoliation effect of was found to be very good.

Production Example  One: Hexanoyl tripeptide  Containing Cosmetic  Produce

A cosmetic containing hexanoyl tripeptides confirmed as excellent in exfoliation effect in Experimental Example 1 was prepared in the composition of Table 2 below.

ingredient Example 1 (% by weight) Comparative Example 1 (% by weight) Hexanoyl Tripeptide 2 - A Cetostearyl alcohol 2.0 2.0 Glyceryl Stearate 1.5 1.5 Mikey-Crystalline 0.7 0.7 Squalane 5.0 5.0 Liquid paraffin 3.0 3.0 Trioctanoine 5.0 5.0 Polysorbate 1.2 1.2 Sorbitan stearate 0.5 0.5 Tocopherol Acetate 0.2 0.2 Micromethicone 3.0 3.0 BHT 0.05 0.05 B glycerin 4.0 4.0 1,3 ?? butylene glycol 2.0 2.0 EDTA 0.05 0.05 Purified water To 100 To 100 Incense, preservative Quantity Quantity

Experimental Example 2: Exfoliation effect of a cosmetic containing hexanoyl tripeptide

Experiment using the cosmetic prepared in Preparation Example 1 in the same manner as in Experiment 1 to confirm the exfoliation effect of the cosmetic containing hexanoyl tripeptide and the results are shown in Table 3 below.

Cosmetic division Exfoliation effect (%) 3 days 6 days 9th 12 days 15th Comparative Example 1 19.6 20.3 34.14 37.37 45.38 Example 1 16.28 24.7 49.7 71.25 91.8

As shown in Table 3, the cosmetic of Example 1 containing hexanoyl tripeptides showed an excellent exfoliation effect as in hexanoyl tripeptides.

Experimental Example 3 Slab Inhibition Test

Treating a cotton-causing agent in the rabbit's ears will cause the cotton to grow after one week, but the larger cotton usually looks the same as before acne's inflammation. As the scalp grows, there is an excess of sebum in the pores, which causes the pores to become larger than normal. Thus, scalp outbreak experiments are somewhat different from acne outbreaks in humans, but they are currently the most acne-like model. Thus, the following experiment was conducted to determine whether the hexanoyl tripeptides have scrim suppression ability.

200 μl of 50% oleic acid / paraffin oil, a cotton-causing substance, is applied to the rabbit's ears once a day to induce cotton cloth, while hexanoyl tripeptide is a cosmetic raw material and does not induce cotton cloth. Dissolved in 1% in glycol, it was applied 200 μl twice a day. Experiments were performed by treating oleic acid and not applying hexanoyl tripeptides as a control group. The number of cotton cloth was based on the size of the cotton cloth being 0.2 mm or more. After exfoliation of the tissues of the scleroderma site by 0.8 mm, the size of the scrim was measured by an optical microscope. A to E measure the size of the cotton cloth by randomly selecting 6 among the well-developed cotton cloths among the whole tissues in the sliced tissue to measure the size of the cotton cloth. The results are shown in Table 4.

Treatment group The number of animals Cotton catcher Cotton cloth size measurement A B C D E Average Oleic Acid Treatment Group (Control) 3 16 6 6 5 4 5 5.2 5.1 4 5 5 6 4 4.8 5 4 6 5 6 5.2 Oleic acid treatment + hexanoyl tripeptide treatment group (experimental group) 3 7 3 3 4 2 3 3.0 2.8 2 3 3 2 3 2.6 4 3 3 2 2 2.8

As can be seen in Table 4, it was confirmed that the hexanoyl tripeptides of the present invention has an effect of suppressing the generation of scrim. In other words, the hexanoyl tripeptides of the present invention resulted in improving the hyperkeratosis of the stratum corneum of the skin, thereby reducing the number and size of the cotton cloth, thereby inhibiting the progression to acne.

Experimental Example 4: Acne Improvement

Acne 10 males and females were subjected to the cosmetic formulations according to the formulation of Formulation Example 1 was applied to the entire face for 4 weeks in the morning and evening. The determination of the effect was evaluated by 1 to 3 points according to the following evaluation items according to the degree felt by the person who participated in the test, and the results are shown in Table 5.

Evaluation of the state before the test

1 = some acne, 2 = some acne, 3 = severe acne

Acne Effect Determination

-: Almost no effect +: Slight effect

++: Relaxed a lot +++: Completely healed

Subject Pre-test status Acne effect determined after 2 weeks Acquired acne after 4 weeks Subject 1 3 + ++ Subject 2 2 + ++ Subject 3 2 - + Subject 4 One - + Subject 5 2 + + Subject 6 3 + ++ Subject 7 2 ++ +++ Subject 8 2 + ++ Subject 9 One + + Subject 10 3 + ++

As can be seen in Table 5, the cosmetic formulations containing hexanoyl tripeptide were used for 4 weeks, and most of the subjects answered that acne was improved.

Hereinafter, based on the results of the above test examples, a cosmetic composition containing hexanoyl tripeptide as an active ingredient is provided. However, the composition of the present invention is not limited to the following formulation examples.

Formulation Example 1 Flexible Lotion

ingredient Content (% by weight) Hexanoyl Tripeptide 1.0 glycerin 6.0 1,3-butylene glycol 3.0 PEG 1500 1.0 Allantoin 0.1 DL-panthenol 0.3 EDTA-2Na 0.02 Benzophenone-9 0.04 Sodium hyaluronate 5.0 ethanol 10.0 Octicdodeceth-16 0.2 Polysorbate 20 0.2 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 2: Convergence Lotion

ingredient Content (% by weight) Hexanoyl Tripeptide 1.0 glycerin 2.0 1,3-butylene glycol 2.0 Allantoin 0.2 DL-panthenol 0.2 EDTA 0.02 Benzophenone-9 0.04 Sodium hyaluronate 3.0 ethanol 15.0 Polysorbate 20 0.3 Witch hazel extract 2.0 Citric acid a very small amount Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 3: Nutritional Lotion

ingredient Content (% by weight) Hexanoyl Tripeptide 3.0 Glyceryl Stearate SE 1.5 Stearyl alcohol 1.5 lanolin 1.5 Polysorbate 1.3 Sorbitan stearate 0.5 Cured Vegetable Oil 1.0 Mineral oil 5.0 Squalane 3.0 Trioctanoine 2.0 Dimethicone 0.8 Tocopherol Acetate 0.5 Carboxyvinyl Polymer 0.12 glycerin 5.0 1,3-butylene glycol 3.0 Sodium hyaluronate 5.0 Triethanolamine 0.12 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 4: Cream

ingredient Content (% by weight) Hexanoyl Tripeptide 3.0 Lipophilic monostearate 2.0 Cetearyl Alcohol 2.2 Stearic acid 1.5 Beeswax 1.0 Polysorbate 60 1.5 Sorbitan stearate 0.6 Cured Vegetable Oil 1.0 Squalane 3.0 Mineral oil 5.0 Trioctanoine 5.0 Dimethicone 1.0 glycerin 5.0 Betaine 3.0 Triethanolamine 1.0 Sodium hyaluronate 4.0 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 5: Massage Cream

ingredient Content (% by weight) Hexanoyl Tripeptide 3.0 Lipophilic Monostearic Acid Glycerin 1.5 Stearyl alcohol 1.5 Stearic acid 1.0 Polysorbate 60 1.5 Sorbitan stearate 0.6 Isostearyl Isosterate 5.0 Squalane 5.0 Mineral oil 35.0 Dimethicone 0.5 Hydroxyethyl cellulose 0.12 glycerin 6.0 Triethanolamine 0.7 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 6: Essence

ingredient Content (% by weight) Hexanoyl Tripeptide 3.0 glycerin 10.0 Betaine 5.0 PEG 1500 2.0 Allantoin 0.1 DL-panthenol 0.3 EDTA-2Na 0.02 Benzophenone-9 0.04 Hydroxyethyl cellulose 0.1 Sodium hyaluronate 8.0 Carboxyvinyl Polymer 0.2 Triethanolamine 0.18 Octyldodecanol 0.3 Octyldodeceth-16 0.4 ethanol 6.0 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 7: Pack

ingredient Content (% by weight) Hexanoyl Tripeptide 3.0 Polyvinyl alcohol 15.0 Cellulose gum 0.15 glycerin 3.0 PEG 1500 2.0 Chicdestrin 0.15 DL-panthenol 0.4 Allantoin 0.1 Glycyrisin Monoammonium 0.3 Nicotinamide 0.5 ethanol 6.0 PEG 40 Cured Castor Oil 0.3 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

As described in detail above, the hexanoyl tripeptides of the present invention not only have an excellent exfoliation effect, but also have excellent scrim formation inhibitory effect and acne improvement effect when the cosmetic composition containing the same is used in humans.

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Claims (5)

Cosmetic composition for acne improvement and alleviation containing hexanoyl tripeptide as an active ingredient. According to claim 1, wherein the hexanoyl tripeptide is' hexanoyl (hexanoyl)-peptide represented by SEQ ID NO: 1 (Arg-Ala-Nle)-NH ₂ acetate salt, characterized in that the cosmetic for improving and alleviating acne Composition. According to claim 1, wherein the content of the hexanoyl tripeptide is a cosmetic composition for acne improvement and alleviation, characterized in that 0.0005 to 20.0% by weight relative to the total weight of the cosmetic composition. According to claim 3, wherein the content of the hexanoyl tripeptide is a cosmetic composition for acne improvement and alleviation, characterized in that 0.001 to 10.0% by weight relative to the total weight of the cosmetic composition. The composition of claim 1 wherein the cosmetic composition consists of a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation and spray Cosmetic composition for acne improvement and alleviation, characterized in that it has a formulation selected from the group.