KR20070094340A - Composition capable of inhibiting sebum secretion - Google Patents

Abstract

A cosmetic composition is provided to control the metabolism of sebum by comprising ingredients contained in an extract of green tea or green tea and an extract of Thujae orientalis Semen in a certain ratio, thereby being effective for alleviating or improving acne and inhibiting excessive sebum. A cosmetic composition comprises 0.001-30.0 wt.% of an ingredient of green tea such as an extract of green tea, catechins, flavonols or derivatives thereof as an effective ingredient and an extract of Thujae orientalis Semen, wherein the catechins are epigallocatechingallate(EGCG), and gallocatechin gallate(GCG) and the flavonols are quercetin, kaempferol and myricetin.

Description

Composition for inhibiting sebum secretion {Composition capable of inhibiting sebum secretion}

1 is a diagram showing the sebum production inhibitory effect of the green tea component and white porcelain extract mixture using the primary cultured sebum cells.

Figure 2 is a diagram showing the interaction of the two extracts as an experiment to determine the optimal concentration ratio of the green tea extract and white porcelain extract mixture using sebum cells.

Figure 3 is a contour plot (Contour Plot) showing the optimal concentration ratio of the green tea extract and white porcelain extract mixture.

Figure 4 is a picture confirming the sebaceous gland growth inhibitory effect of the green tea extract and white porcelain extract mixture using the animal model hamster.

The present invention relates to a cosmetic composition containing a green tea component and white porcelain extract exhibiting sebum secretion inhibitory effect, and more particularly, catechins, flavonols, and derivatives of green tea extract or green tea component It relates to a cosmetic composition having an excess sebum inhibitory effect and acne alleviating effect by containing at least one selected from the group consisting of and white porcelain extract in a certain component ratio.

In general, the sebum in the skin including the scalp and face plays a role of keeping the skin moisturized or preventing the invasion of microorganisms, but when the sebum is excessively secreted, the acne worsens, the enlargement of the pores by acne is promoted, and seborrheic dermatitis occurs. Various skin diseases can be caused. Various substances have been developed to treat such skin diseases, but because they are developed for the purpose of treating symptoms such as acne or the disease itself, rather than removing the root cause, the healing effect is insignificant and the preventive concept is There is no situation, and the side effects such as skin redness, skin hypersensitivity reaction, photosensitization reaction and the like are frequently caused by synthetic drugs.

Thus, there was an effort to alleviate acne and suppress excess sebum without causing skin side effects by using a composition for skin using a herbal or natural extract.

In particular, green tea is made by harvesting the leaves of Camellia sinensis , a plant of theaceae, and dried or steamed in the sun. It is also known to have skin beauty effects such as cleansing and astringent effects.

For example, as a method using the green tea component, International Patent PCT / US1998 / 23041 “Methods and Compositions for Regulating 5-alpha Reductase Activity” is used to inhibit sebum production by using the ability of inhibiting 5-alpha reductase activity of green tea catechin. The international patent PCT / US1998 / 21675 “Topical composition for controlling the oily and / or greasy appearance of the skin” refers to an embodiment using green tea extract for the inhibition and anti-inflammatory effect of sebum secretion. Doing.

In addition, white porcelain (biota orientalis ) is a seed of the encyclopedia of white encyclopedia, and is steamed and dried in the sun after removing the remaining shells and shells. The fresh ones are pale yellow or yellowish white, but after a long time they turn yellowish brown and ooze oil. It mainly comes from China's Shandong, Yunnan, Henan, and Hebei, and the seeds contain about 15% of fatty oil and a small amount of essential oil and saponin. Inflammatory and sedative drugs have been used to treat nerve anxiety, restriction, constipation and hair loss.

For example, as a method using the white porcelain component, Korean Patent 2000-58768 "Sebum secretion inhibiting composition" is a composition containing white porcelain extract to prevent and treat sebum-related diseases, and the Korean patent 2002-48073 "acne Prophylactic and therapeutic external skin composition "is seeking the composition for inhibiting sebum secretion and acne prevention and treatment by using 5-alpha-reductase inhibitory effect of white porcelain. In addition, Korean patent 2003-86404 "external skin composition containing herbal extracts" includes white porcelain as one of the herbal compositions for treating or preventing skin diseases such as atopic dermatitis, contact dermatitis, psoriasis.

However, the methods described above have some problems such as concentration problems in terms of usability and irritation problems in terms of usability.

Therefore, it is necessary to implement a complex prescription that can reduce the respective disadvantages while utilizing the excellent effect of the green tea component and white porcelain extract.

Thus, the present inventors have studied the active substance among natural products that can inhibit excessive sebum secretion and have proven skin safety, and found that green tea component has an excellent effect on inhibiting sebum secretion, and mixed with white porcelain extract When prescribing low concentration white porcelain extract and green tea extract even when the treatment was found to exhibit a high sebum secretion inhibitory effect does not cause skin side effects and completed the present invention.

Accordingly, it is an object of the present invention to provide a cosmetic composition that is effective in alleviating or improving acne and suppressing excessive sebum by controlling the sebum metabolism process by containing the green tea extract or extract contained in the green tea and white porcelain extract in a certain component ratio.

In order to achieve the above object, the present invention provides a cosmetic composition having a sebum secretion inhibitory effect and acne relief effect containing the green tea component and white porcelain extract.

Hereinafter, the present invention will be described in more detail.

Green tea component of the present invention contains at least one selected from the group consisting of catechins (catechins), flavonols (flavonols), and derivatives thereof having a basic structure of flavan-3-ol as the green tea extract or green tea.

In addition, the catechins are epigallocatechin gallate (EGCG) and gallocatechin gallate (GCG), flavonols are characterized in that quercetin (quercetin), camphorol (kaempferol) and myricetin (myricetin) .

The content of the green tea component is preferably 0.001 to 30.0% by weight based on the total weight of the composition. This is because if the content is less than 0.001% by weight, it is difficult to expect an effective effect, and if it is more than 30% by weight, it is difficult to formulate.

The catechins used in the present invention, epigallocatechin gallate (EGCG) and gallocatechin gallate (GCG), are represented by the following formulas (1) and (2).

The EGCG and GCG are 2′-epimers and their structure is determined depending on whether the galyl group is cis-type or trans-type. In general, the amount of EGCG in green tea is known to be more than 10 times the content of GCG, and the conversion of EGCG to GCG is known to act as a factor of EGCG instability.

The flavonols used in the present invention, kaempferol, quercetin, and myricetin, respectively, are represented by the following Chemical Formulas 3, 4, and 5, and basically have the same back-bone structure. The difference is that the B-ring has one, two and three hydroxyl groups (-OH groups), respectively.

In addition, the present invention contains the extract of white porcelain in the green tea component in a certain component ratio. The white porcelain extract used in the present invention is extracted after removing the shells and shells of the encyclopedia baekbaek and dried in the sun.

The content of the white porcelain extract is preferably 0.001 to 30.0% by weight based on the total weight of the composition. This is because if the content is less than 0.001% by weight, it is difficult to expect an effective effect, and if it is more than 30% by weight, it is difficult to formulate.

Therefore, in the present invention, the green tea extract, epigallocatechin gallate (EGCG), gallocatechin gallate (GCG), quercetin (quercetin), camphorol (kaempferol), myricetin (myricetin) and derivatives thereof in the group consisting of By containing at least one selected and white porcelain extract to provide a cosmetic composition having a sebum secretion inhibitory effect and acne relieving effect.

In addition, the active ingredients are each an effective concentration, when the white porcelain extract is less than 0.01% green tea component 3-10%, when the white porcelain extract is 0.01 ~ 1% green tea component 1 ~ 3%, white porcelain extract 1 ~ 10% When the green tea component is contained at a ratio of less than 1%, the green tea component exhibits an optimum effect. When used at the above concentration ratio, only the low concentration of white porcelain extract is used. It is very effective to reduce the skin irritation and side effects by reducing the content of white porcelain extract.

The composition for skin of the present invention is not particularly limited in the formulation, for example, of various skin adhesion type cosmetics such as lotion, softening lotion, nourishing lotion, nourishing cream, massage cream, pack, gel, essence or solid soap. It may be a cosmetic composition having a formulation, and may also be a transdermal dosage form such as lotion, ointment, gel, cream, patch or spray.

In addition, in the composition for skin of each formulation, other components than the essential components described above may be appropriately selected and blended by those skilled in the art without difficulty according to other skin compositions or purposes of use.

Hereinafter, the present invention will be described in more detail with reference to Examples and Test Examples. However, these examples are for illustrating the present invention, and the present invention is not limited only to these examples.

[Test Example 1] Sebum production inhibition experiment of the green tea component and white porcelain extract mixture

Step 1. Sebum Cell Culture

In the present invention, sebum cells were primary cultured for experiments. Sebum cells were extracted from sebaceous glands attached to hair follicles, in cooperation with an affiliated hospital. In the extraction method, the epidermis was first isolated from the hair follicle pieces obtained by treating 3 units / ml of dipase at 4 ° C. for 20 hours. The epidermis was separated and treated with 0.02% deoxyribonuclease at 37 ° C. for 15 minutes, followed by microablation of sebaceous glands. Isolated sebocyte lobules were incubated with mitomycin C-inactivated 3T3 cells. The medium was DMEM: F12 (3: 1), 10% fetal bovine serum (FBS), 10ng / ml human recombinant epidermal growth factor (EGF), 10ng / ml keratinocyte growth factor ( keratinocyte growth factor (KGF), 10-9M cholera toxin (Sigam), 2mM glutamax (200mM stock, Gibco) and 10ug / ml gentamycin (Gentamycin (Amresco)) Incubated. Passage number of sebum cells used for the experiment was limited to 4 or less (ref. J. Invest. Dermatol., 110: 84-89, 1998).

Step 2. Sebum Cell Differentiation and Sample Processing

Differentiation of sebum cells in culture was induced through changes in medium composition. To this end, each cell was washed twice with PBS, then without adding FBS, 50 ug / ml bovine pituitary extract (BPE), 1 mg / ml fat-free bovine serum albumin (1 mg / ml faf-BSA), 0.042 ug / ml Linoleic acid (LIN) was added to DMEM: F12 (1: 1) and further incubated for 48 hours. After that, the samples were processed for each experimental group. Samples were dissolved in DMSO at a concentration of 1000 ×, diluted with medium, and added to plates for each experimental group.

Step 3. Flow cytometry analysis

After 72 hours of treatment, each cell was treated with HyQtase (detaching solution, Hyclone) for 15 minutes at 37 ° C to remove the cells from the plate, neutralized by adding medium, and then centrifuged at 250 g for 10 minutes. Immersed. Thereafter, Nile red (fluorescent dye, Sigma) stock solution (10mg / ml) was diluted in PBS and added to the cells, and stained to a final concentration of 10ug / ml. Dyeing was performed at 37 degreeC for 30 minutes in the light-shielded state. After staining, the cells were allowed to settle and then dispersed in PBS, and fluorescence was measured for 10000 cells per sample using FACScalibur (Becton Dickinson, Plymouth, UK). Fluorescence by nile red was measured for both green fluorescence (FL-1) and red fluorescence (FL-2). The comparison of each experimental group was obtained by the average value of the fluorescence value of each experimental group (means) and expressed as a percentage compared to the untreated group. Each fluorescence value reflects the lipid content of each experimental group (ref. J. Invest. Dermatol., 121: 441-447, 2003).

Sebum production inhibition experiment of the present invention was carried out by the above method using sebum cells (sebocytes). As a control group, the untreated group of Comparative Example 1 was used, and as a positive control group, finasteride (finasteride, Cipla Co., Ltd.) of Comparative Example 2 was used. Samples and amounts used are as shown in Table 1 below, the results are shown in Table 1 and FIG.

(Sample description: EGCG, GCG, quercetin, camphorol, mycetin are purchased from Sigma, green tea (GTE) is freeze-dried by extracting Jeju green tea from 95% EtOH for 24 hours at room temperature, and white porcelain (BJI) Provided by

division Treatment Sample % of FL-1 Inhibition Rate (%) Comparative Example 1 No treatment group 100.0 ± 4.9 - Comparative Example 2 + Finasteride (10 uM) 86.6 ± 11.4 13.6 Example 1 + EGCG (10 uM) 86.2 ± 5.1 13.8 Example 2 + GCG (10 uM) 89.1 ± 2.5 10.9 Example 3 + Quercetin (10 uM) 88.8 ± 0.3 11.2 Example 4 + Camphorol (10 uM) 88.8 ± 1.5 11.2 Example 5 + Mycetin (10 uM) 94.6 ± 3.4 5.4 Example 6 + GTE (10 ppm) 78.0 ± 0.9 22.0 Example 7 + BJI (10 ppm) 67.2 ± 0.2 32.8 Example 8 + Finasteride (10uM) + BJI (10ppm) 61.5 ± 3.9 38.5 Example 9 + EGCG (10uM) + BJI (10ppm) 60.9 ± 0.3 39.1 Example 10 + GCG (10uM) + BJI (10ppm) 62.9 ± 2.7 37.1 Example 11 + Quercetin (10uM) + BJI (10ppm) 67.2 ± 2.4 32.8 Example 12 + Camperol (10 uM) + BJI (10 ppm) 57.6 ± 4.8 43.4 Example 13 + GTE (10 ppm) + BJI (10 ppm) 64.3 ± 2.1 35.7

 As can be seen in Table 1 and Figure 1, green tea (GTE) extract (Example 6), EGCG and GCG (category 1 and 2) of catechins, green tea components, quercetin, camphorol and milo It was confirmed that sebum production was inhibited by the cetin (Examples 3 to 5) component. In addition, it was confirmed that the sebum production inhibitory effect was further increased when the white porcelain (BJI) extract mixing treatment (Examples 8 to 13), in particular, when the white porcelain extract 10ppm and camphorol 10uM mixed treatment (Example 12) The highest score was 43.4%.

However, the mixing experiment with the high concentration (10ppm) white porcelain extract has a disadvantage in that the inherent effects of the green tea component shown in the green tea treatment experiment was buried, so the synergistic effect between the two extracts was not sufficiently expressed. Therefore, further experiments were conducted to determine the optimal concentration ratio of the green tea component and white porcelain extract mixture.

Test Example 2 Experiment of Determination of Optimal Concentration Ratio of Green Tea Component and White Porcelain Extract Mixture

In order to determine the optimal concentration ratio of the green tea component and white porcelain extract mixture was tested as follows. Detailed experimental methods are the same as in Test Example 1, and the sample treatment was based on the protocol provided by Minitab 14 s / w using Design of Experiment (DOE), and detailed experimental plans and results are shown in Table 2 and FIGS. Shown in

division Stdorder RunOrder PtType Blocks BJI GTE % of FL-1 Example 14 One One One One 0.01 ppm 0 ppm 92.2 Example 15 2 2 One One 0.01 ppm 1 ppm 83.1 Example 16 3 3 One One 0.01 ppm 10 ppm 80.6 Example 17 4 4 One One 0.1 ppm 0 ppm 84.9 Example 18 5 5 One One 0.1 ppm 1 ppm 79.0 Example 19 6 6 One One 0.1 ppm 10 ppm 75.4 Example 20 7 7 One One 1 ppm 0 ppm 81.9 Example 21 8 8 One One 1 ppm 1 ppm 70.0 Example 22 9 9 One One 1 ppm 10 ppm 69.7 Example 23 10 10 One One 10 ppm 0 ppm 67.2 Example 24 11 11 One One 10 ppm 1 ppm 66.4 Example 25 12 12 One One 10 ppm 10 ppm 64.3

 As can be seen in Figure 2, under the concentration of 10 ppm of white porcelain (BJI) extract, the effect of the green tea (GTE) extract is hardly exhibited because the white porcelain alone can sufficiently saturate the sebum production inhibitory effect, which is Test Example 1 The conclusion is similar to that discussed in.

Importantly, when 1 ppm of BJI and 1 ppm of GTE are mixed (Example 21), sebum production inhibition rate is estimated to be about 30%, which is almost the same effect as the inhibition rate (about 33%) when BJI 10 ppm treatment (Example 7). Can be. These results can also be seen in the contour plot of FIG. 3, which shows that the pink region (the region having a sebum generation rate of 60 to 70%) starts at 1 ppm of BJI and 1 ppm of GTE.

More specifically, when the white porcelain extract is less than 0.01%, the green tea component is 3-10%, when the white porcelain extract is 0.01-1%, the green tea component is 1-3%, when the white porcelain extract is 1-10%, the green tea component is 1% When it contains in less than ratio, an optimal effect is shown.

Therefore, when applied to various formulations containing excessive amounts of white porcelain extract, only the white porcelain extract corresponding to 1/10 of the existing content is added, and even the same amount of green tea extract, the same sebum production inhibitory effect is realized as the existing formulation. It may be the first advantage, and according to the decrease in the content of white porcelain and the total extract, it is considered that there is a second advantage in reducing skin irritation and the likelihood of causing skin trouble / side effects.

[Test Example 3] hamster sebaceous gland growth inhibition experiment

The sebaceous gland growth inhibitory effect of the composition was tested through animal experiments. A male 4-5 week old male (Syrian golden hamster) was purchased, adapted to a new environment for a week, and then removed from the back hair to reveal the flank organs. Three animals were selected for each group, and the test substance was applied twice a day for two weeks. Plank organs have been widely used to measure androgen effects as a collection organ of melanocytes, sebaceous glands, and hair follicles. Two weeks after the start of the experiment, the size and color of the flank organs over time were measured and compared. As a control group, alcohol, testosterone (hereinafter referred to as T, Sigam), and finasteride (finasteride, Cipla) were used as vehicles. In one application, the total volume of the test substance was 5 ul, 1 ug of testosterone and 1 mg of each test substance. The results are shown in Table 3 and FIG.

division Treatment Sample Plank engine area increased in two weeks (mm ² ) Inhibition Rate (%) P-value Comparative Example 3 Vehicle 20.41 ± 6.07 - - Comparative Example 4 T 42.32 ± 12.57 - - Comparative Example 5 T + finasteride 16.32 ± 7.22 61.4 <0.05 Example 26 T + EGCG 29.55 ± 9.75 30.2 <0.05 Example 27 T + GCG 19.85 ± 8.61 53.1 <0.05 Example 28 T + Camphorol 11.63 ± 15.21 72.5 <0.05 Example 29 T + GTE 18.50 ± 6.25 56.3 <0.05 Example 30 T + BJI 17.94 ± 8.54 57.6 <0.05 Example 31 T + GTE + BJI 8.24 ± 10.24 80.5 <0.05

As can be seen in Table 3 and Figure 4, even using some components of the green tea was able to obtain a relatively high level of sebaceous gland growth inhibitory effect, as shown in Example 31 green tea extract (GTE) and white porcelain extract (BJI) In the mixed regimen, the hamster's sebaceous gland growth inhibition effect was confirmed by the animal model experiment.

[Test Example 4] sebum secretion suppression and acne alleviation effect

Nine men and women who feel a lot of sebum secretion and 10 men and women who suffer from acne were separately selected and prescribed according to the following Formulation Example 1 to correct the acne site and the lot of sebum secretion of the face every day for 4 weeks. Judgment of the effect was scored according to the degree felt by the person who participated in the test, sebum secretion inhibition was measured using a sebum measuring device. The results of the sebum secretion inhibitory effect is shown in Table 4, the acne relief effect is shown in Table 5.

Tester Pre-test amount (ug / cm ² h) After 2 weeks of testing (ug / cm ² h) After 4 weeks of testing (ug / cm ² h) One 79 66 61 2 65 40 46 3 48 43 44 4 23 33 38 5 71 65 55 6 88 71 62 7 35 43 45 8 55 38 43 9 77 65 63

Tester Pretest State After 2 weeks of exam After 4 weeks of exam One 3 - ++ 2 2 ++ +++ 3 One + ++ 4 2 + + 5 2 + ++ 6 One - + 7 3 ++ ++ 8 2 + ++ 9 One + + 10 2 - + * Pre-test: 1-acne slightly, 2-acne slightly, 3-acne severe * Effect determination: (-) almost no effect, (+) slight effect, (++) much less, (++ +) Completely healed

 From the results of Table 4 and Table 5, it can be seen that the composition according to the present invention can suppress sebum secretion, thus relieving acne.

Hereinafter, although the formulation of the composition of this invention is given as an example, this invention is not limited only to these formulation examples.

Formulation Example 1 Nutritional Cosmetics

ingredient Content (% by weight) White porcelain + green tea extract (1: 1) 1.00 Beeswax 4.00 Polysorbate 1.50 Sorbitan sesquioleate 0.70 Liquid paraffin 5.00 Caprylic / Capric Triglycerides 5.00 glycerin 3.00 Butylene glycol 3.00 Propylene glycol 3.00 Carboxy Vinyl Polymer 0.10 Triethanolamine 0.20 antiseptic Quantity Pigment Quantity Spices Quantity Purified water To 100

Formulation Example 2 Cream

ingredient Content (% by weight) White porcelain + green tea extract 0.1 Liquid paraffin 15.0 Cetostearyl alcohol 2.0 Beeswax 3.0 Methylpolysiloxane 0.5 Lipophilic monostearic acid 2.0 Stearate stearic acid 2.0 Sorbitan sesquioleate 0.8 Monostearic acid 1.0 Polyoxyethylene sorbitan (EO = 20) 1.2 Methylparaben 0.2 Propylparaben 0.1 Spices 0.2 Ethylenediaminetetradiacetic acid sodium 0.02 glycerin 5.0 Propylene glycol 5.0 Triethanolamine 0.2 Imidazolidinylurea 0.3 Purified water To 100

[Formulation Example 3] Lotion

ingredient Content (% by weight) White porcelain + green tea extract 0.1 Multi Wax 3.6 Steric acid 0.5 Liquid paraffin 5.0 Dihidegwax 0.8 Bee wax 17 0.05 Nicole MGS-B 1.9 Aracell # 165 0.7 glycerin 7.0 Methylparaben 0.12 Propylparaben 0.03 Liquid paraben 5.0 Twin # 60 0.5 Carbomer 0.12 Purified water To 100

[Formulation Example 4] Pack

ingredient Content (% by weight) White porcelain + green tea extract 0.1 Citric acid 1.0 Polyvinyl alcohol 14.0 Cellulose gum 0.1 glycerin 1.0 Polyoxyethylene Glycol 400 1.0 Octyldodecyl ether (EO = 16) 0.4 ethanol 0.6 antiseptic Quantity Pigment Quantity incense Quantity Purified water to 100

[Formulation Example 5] Cosmetic Soap

ingredient Content (% by weight) White porcelain + green tea extract 0.1 Titanium dioxide 0.2 Polyethylene glycol 0.8 glycerin 0.5 Ethylenediaminetetraacetic acid 0.05 salt 1.0 Pigment Quantity Soap Quantity Toilet soap base (13% moisture, parts by weight) To 100

As described above, sebum secretion inhibiting composition containing the green tea extract of the present invention or one or more selected from the green tea-containing components and white porcelain extract is very safe when applied to human skin, and excellent sebum secretion effect, acne, It can be used in effective concentrations for the prevention or treatment of sebum-related diseases such as seborrheic dermatitis and acne enlargement.

Claims (6)

Cosmetic composition containing green tea component and white porcelain extract as an active ingredient. The composition of claim 1, wherein the green tea component is one or more selected from the group consisting of green tea extracts or catechins, flavonols, and derivatives thereof. The method of claim 2, wherein the catechins are epigallocatechin gallate (EGCG) and gallocatechin gallate (GCG), and flavonols are quercetin (quercetin), kaempferol and myricetin (myricetin) Characterized in that the composition. The composition of claim 1, wherein the active ingredient is contained in an amount of 0.001 to 30.0 wt% based on the total weight of the composition. The method according to claim 1 or 2, wherein the active ingredients are each effective concentration When the white porcelain extract is less than 0.01%, the green tea component is 3-10%; Green tea component is 1-3% when white porcelain extract is 0.01-1%; Green tea extract less than 1% when white porcelain extract is 1 ~ 10%; A composition comprising a phosphorus ratio range. The composition according to any one of claims 1 to 5, wherein the composition maximizes sebum metabolism control, excess sebum inhibition, acne alleviation or improvement, or alleviation of seborrheic dermatitis.

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