KR20080029055A - COSMETIC PRODUCTS IMPROVE ACNEGENIC SKIN THROUGH ANTI-MICROBIAL ACTION AND INHIBITING THE ACTIVITY OF 5 alpha;-REDUCTASE - Google Patents

Abstract

A cosmetic composition is provided to show excellent 5alpha-reductase inhibitory effect and excellent antibacterial activity against Propionibacterium acnes, thereby improving acnegenic skin and seborrheic skin. A cosmetic composition for improving acnegenic skin comprises 0.01-20% of N-acetyl phydosphingosine, 0.01-10% of an extract of soybean, 0.001-40% of an extract of Paeonia suffruticosa Andrews root bark, and 0.01-30% of an extract of Galla Rhois. The composition is in the formulation of face lotion, lotion, cream, essence, skin lotion, foundation, liquid soap, solid soap, or cleansing form.

Description

A cosmetic composition that is applied to the skin and helps to improve acne skin by antibacterial action and inhibitory action of 5 alpha-reductase. {Cosmetic Products improve acnegenic skin through anti-microbial action and inhibiting the activity of 5 α-reductase}

The present invention is applied to the surface of the skin to inhibit the growth of bacteria by the microorganisms in the skin lesions and to inhibit the sebum secretion by inhibiting the activity of antimicrobial activity and the activity of 5 alpha-reductase (5α-Reductase) to give acne skin It is about cosmetic compositions that help to improve the skin.

Through the present invention, as well as inhibiting the growth of propionibacterium acnes, a cause of skin acne, has an antimicrobial action against microorganisms in various skin conditions, and 5 alpha-reductase of 5 alpha-reductase By suppressing excessive sebum secretion due to activity, it solved the problem of acne skin and seborrheic skin.

Acne is an inflammatory disease of the sebaceous glands that occurs frequently on the face, especially on the cheeks and forehead. It occurs mainly in puberty and declines in the mid-20s. Acne is involved in a variety of factors and symptoms are caused by the interaction of several factors. Factors involved in acne development play an important role such as increased sebum secretion, abnormally increased hair follicle hyperkeratosis and pore closure, the growth of acne bacteria, inflammatory reactions, and the like.

During puberty, a large amount of testosterone is present in the blood, and testosterone, a male hormone, is converted to dihydrotestosterone (DHT) by 5 alpha-reductase (DiHT) and dihydrotestosterone (DHT). ) Acts as a major causative agent to produce sebum in the cells of the sebaceous glands to promote sebum production.

Acne may be caused by the overproduction of male hormone testosterone, excessive secretion of sebum due to abnormal action of 5 alpha-reductase, and the reproduction of microorganisms due to clogging of pores by keratinization of keratin. It happens. (See: Cations inhibit specifically type 1 5α- Reductase Found in Human Skin, J.invest.Dermatol, 104,775-778, 1995)

Inhibiting 5 alpha-reductase, a human enzyme that converts testosterone, a testosterone, to dihydrotestosterone (DHT), an active testosterone, reduces sebum production and keratinocytes in hair follicle cells. It basically suppresses hyperkeratosis and improves acne skin and seborrheic skin.

Currently, there are various treatments for acne caused by the complex action of various factors. The typical treatment is acne, which is an inflammatory reaction caused by the unsaturation of unsaturated fatty acids formed by the decomposition of fatty acids by Propionibacterium acnes. Inhibition of sebum production using anti-male hormones, by means of exfoliants in the form of dissolving keratin using substances with strong acidity, by applying directly to the acne-prone areas to remove fatty free acids, antibiotics ( Erythromycin, Clindamycin), Benzoyl peroxide, which has antibacterial activity against acne bacteria, Vitamin A retinol derivatives that reduce the number of cotton cloths by inhibiting the formation of cotton wool, etc. Taking drugs, physically using a laser There are methods such as the treatment of deureum.

Although the above methods are effective in treating acne to some extent, they can cause various serious side effects when used for a long time. The use of anti-androgens can reduce the effects of androgen, a male hormone that affects the development of acne, but the use of anti-androgens is limited to women, and corticosteroids, which are steroids, also remove the beneficial microorganisms present on the skin. It also makes the body more resistant to antibiotics, making it more difficult to fight the causative organism. In the case of exfoliation by drugs or physical exfoliation by laser, there are various side effects, such as frequent procedures or long-term use, rupture of the blood vessels or weakening of the epidermal layer. Since the procedure is repeated several times instead of one, the burden on the consumer and patient is increased in the psychological and economic aspects.

The cosmetic composition of the present invention relates to a cosmetic composition that is safer and more effective for the human body and helps to improve acne and seborrheic skin.

In order to solve the problems caused by acne treatment, the present inventors found that the activity of 5 alpha-reductase, an enzyme that is directly involved in the production of active male hormone, is a fundamental cause of male hormone-related diseases. It strongly inhibits the release of excess sebum and inhibits the action of harmful microorganisms such as propionibacterium acnes, which causes acne worsening. Inhibits skin inflammation caused by acne and quickly recovers skin wounds caused by acne, and combines excellent ingredients to make skin clean without leaving skin wounds. It was completed.

The present invention is a general cosmetic composition that can be used for a long time universal without restriction on age without burdening the skin by the synergistic effect of the ingredients effective for acne and seborrheic skin and helps people who suffer from acne and seborrheic skin It is an object to provide a cosmetic composition.

The present invention is the main component of the antibody and skin protective film specific to the propionibacterium acnes, which is the cause of acne, in the cosmetic composition containing an effective ingredient for acne and seborrheic skin, inhibiting skin inflammation and damaged skin. N-Acetyl Phydosphingosine, a soybean extract effective for membrane regeneration, and soybean extract, 5 alpha-reductase, an enzyme that catalyzes dihydrotestosterone, known to cause sebum secretion and acne production. It is characterized by containing the extract of bark and the gall bladder extract to inhibit the activity.

Hereinafter, the present invention will be described in detail.

N-Acetyl Phydosphingosine Most of the stratum corneum lipids, it is one of the intermediates of ceramide that make up the skin protective layer. It has excellent moisturizing antibacterial effect and helps to improve skin immunity.

The stratum corneum, the skin barrier, is the tissue with the most sphingolipids among many tissues of the human body. ceramide accounts for up to 50% of the stratum corneum lipids. The Elias group reports that ceramides 2 and 5 are derived from sphingomyelin (Epidermal sphingomyelins are precursors for selected stratum corneum ceramides. J Lipid Res 2000; 41: 2071-82, Uchida Y, Hara M, Nishio H et al. This finding is supported by the fact that ceramide 2 and 5 are still found in the stratum corneum of Gaucher disease due to lack of beta-glucocerebrosidase.

ceramides 1,2,4 and 5 contain sphingosine as a backbone and ceramides 3 and 6 contain Phytospingosine.

The major component of the skin barrier is a large amount of sphingoid bases such as neutral ceramide and sphingosine. N-acetyl sphingosine has potent PKC inhibitory activity and shows various physiological activities such as controlling cell growth and differentiation and inducing apoptosis.

Soybean extract, or lecithin, is termed phosphatidylcholine (PC) in academic terms and is the most representative glycerol fatty acid. It has a structure in which glycerin is combined with fatty acid, phosphoric acid, and choline, and is an important component of brain and nervous system.

Lecithin (also known as phospholipids) is a major component of biological membranes and has recently been found to play an important role in the functioning of the biological function, lecithin is the most common phospholipids found in foods are contained in eggs, soybeans and so on.

 Phospholipids are the major components that make up the cell membrane as cell constituents, and play an important role in regulating enzymatic reactions by providing a working environment for various enzymes. They also act as secondary intracellular transporters by various stimuli. There are many different roles.

Cells, whether regenerated or not, have cell membranes that absorb nutrients or excrete waste products through the cell membranes. This cell metabolism is the basis of life and can not be achieved without the role of the cell membrane, the so-called body membrane that is the filter is composed of lecithin as the center. Lecithin is made up of double, and in between, proteins, glycolipids, cholesterol, vitamin E, etc. are sandwiched between the structure.

The PC of lecithin promotes the hydrolysis of cholesterol esters by activating the cholesterol ester hydrolase attached to the membrane by enhancing the function of the lysosomal membrane.

Peel extract is a root extract of peony (Paeonia Suffruticosa Andrews / INCI Name: Paeonia Suffruticosa Root Extract), which is a plant extract that is harmless to the human body and is used as a medicine in oriental medicine. It is native to northern China and has been cultivated for medicinal and ornamental purposes since the Three Kingdoms. Peony root bark is used for medicinal purposes. Peony skin contains Paeonol, Paonoono, Paeonolide, Tannin, etc.

The gall extract is a hump-like pouch of Rhus javanica L., distributed in the foothills and valleys of Korea, and is a deciduous arborescent of about 5-7m in height. When a gallant aphid parasitic on a red tree cuts off a leaf to lay eggs, the cells divide abnormally, forming a lump-like bag, and a larva of the gallant aphid grows in it. This is called a gallant. Pick up the steam before the insects come out, kill the insects, and use the dried ones as medicine.

N-Acetyl Phydosphingosine (N-Acetyl Phydosphingosine) 0.01 ~ 20%, soybean extract 0.01 ~ 10%, bark skin extract 0.001 ~ 40%, the acinar skin composition containing 0.01 ~ 30% as an active ingredient.

The composition for acne skin of the present invention may have a conventional formulation as a skin external agent, and may be formulated with a lotion, lotion, cream, essence, skin lotion, foundation, as well as a human cleanser such as liquid soap, solid soap, and cleansing foam. Can be. The composition of each of these formulations may contain a variety of bases and additives necessary for the formulation of the formulation and are suitable, and the types and amounts of these components can be readily selected by those skilled in the art.

Hereinafter, the effects of the composition for acne skin of the present invention will be described in detail with reference to Examples and Examples, but the present invention is not limited to these Examples.

The following example was tested using the basic lotion prescription for the efficacy effect experiment of the acne skin composition.

(Example)

Ingredient (wt%) Example One 2 3 4 5 6 7 8 Purified water Final 100 Final 100 Final 100 Final 100 Final 100 Final 100 Final 100 Final 100 Moisturizer 5 5 5 5 5 5 5 5 Ethyl Alcohol 5 5 5 5 5 5 5 5 N-Acetyl Phydosphingosine 0.01 0.01 3 3 5 5 10 20 Soybean Extract (Lecithin) 0.01 5 5 10 10 3 3 3 Paeonia Suffruticosa Root Extract 0.01 5 10 5 5 20 40 10 Ginseng Extract (Rhus javanica L.) 0.01 10 10 20 30 5 5 5

Comparative Example 1

Ingredient (% by weight) Comparative Example One 2 3 4 Purified water Final 100 Final 100 Final 100 Final 100 Moisturizer 5 5 5 5 Ethyl Alcohol 5 5 5 5 Erythromycin - 2 2 - Clindamycin - 2 - 2

In order to compare with the case of the examples, a composition containing an excipient and an antibiotic was prepared, respectively.

Test Example 1 Antibacterial Activity Test against Acne Bacteria (Propionibacterium acnes)

1) Disc Plate Method

Each of the cosmetic compositions prepared in the compositions of Examples 1 to 8 and Comparative Examples 1 to 4 were tested for antibacterial activity against Propionibacterium acnes, a strain of acne-causing strains, and the results are shown in Table 3 below. Disc plate method was used as an irradiation method. This method is characterized by spreading Propionibacterium acnes on agar plate medium, and then placing a flat disc treated with the composition of the Examples and Comparative Examples to examine the size of the growth inhibition zone (Inhibition Zone). The antimicrobial activity was investigated.

Antimicrobial Activity Test Using Disc Plate Method for P.acnes Example Comparative example 2 4 6 8 One 2 3 4 Propionibacterium acnes ATCC6919 6 mm 10.25mm 12 mm 15 mm 0 mm 17 mm 7 mm 7.25 mm Propionibacterium acnes ATCC11827 6 mm 9 mm 12 mm 13.5mm 0 mm 18.5mm 9 mm 8.5mm

2) Minimum Inhibitory Concentration (MIC)

The antimicrobial activity test for acne bacteria (Propionibacterium acnes) was used liquid dilution method.

2 ml of liquid medium BHI medium was diluted at 100 ppm intervals from 0 to 1000 ppm, and then inoculated with 20 µl of 10 ⁶ / ml of bacterial solution and incubated for 48 hours. Turbidity was defined as the minimum concentration that inhibited growth as the minimum growth inhibitory concentration (MIC: Minimum Inhibitory Concentration) and the results are shown in Table 4.

Antimicrobial Activity Test Using Minimum Growth Inhibition Concentration Method Minimum growth inhibition (ppm) Example Comparative example 2 4 6 8 One 2 3 4 Propionibacterium acnes ATCC6919 1000 650 700 550 TNTC 500 1000 800 Propionibacterium acnes ATCC11827 1000 650 720 550 TNTC 500 1000 800

<Test Example 2>

Inhibitory Activity Test of 5alpha-Reductase

Experiments that were inhibitors that inhibit the activity of 5 alpha -reductase of Examples 1 to 8 were performed.

 1) A male Sprogue-Dawley rat (7-8 weeks of age) was killed with a deciduous rat, and then 0.32M sucrose in which the abdominal prostate was removed to remove connective tissue. A buffer containing 0.1 mM dithiothreitol, 20 mM sodium acetate, was added, finely chopped and suspended in a grinder. After centrifugation of the suspension, the supernatant was taken. 5α-reductase is partially purified in this supernatant.

Radiolabeled testosterone (3H testosterone) was used as the reaction substrate of 5 alpha-Reductase. Enzyme Reaction Solution: 5 alpha-Reductase: Example 3, 7 was reacted in an incubator at a ratio of 70: 70:10 for 2 minutes, the solvent was removed, and the remaining material was dissolved in a developing solvent. In the graph 9TLC, the amount of testosterone and the amount of dihydrotestosterone were quantitatively analyzed using a tensiometer to evaluate the inhibition rate of 5 alpha -reductase.

As a control, enzyme reaction solution: 5 alpha -reductase (5α-Reductase): Comparative Example 1 was tested in the same ratio 70: 70:10 dml.

To determine the isotope levels of testosterone and dihydrotestosterone, a bath system was used to determine the amount of isotopes remaining on the film.

The degree of production of dihydrotestosterone (3H) from substrate testosterone (3H) was measured to measure 5alpha-reductase activity.

5alpha-Reductase Activity Inhibition Results T (dpm) DHT (dpm) % Conversion Example 3 12671 1230.0 7.4 Example 7 11820.0 1737.7 11.3 Comparative Example 1 9708.0 3839.2 26.7

* T: 3H radioactivity in the testosterone region DHT: 3H radioactivity in the dihydrotestosterone region * Conversion rate:% of radioactivity / total radiation inhibition in the DHT region: 100 × (conversion rate of the control-sample) / As shown in the results of the conversion rate of the control group, N-Acetyl Phydosphingosine, soybean extract, bark skin extract, and gallnut extracts contained in Examples 3 and 7 inhibited the activity of 5α-reductase, 5α. -It can be seen that there is an effect of suppressing the amount of dihydrotestosterone, a male hormone related to reductase. In addition, it can be seen that the extract of Example 7 has the most inhibitory effect on the amount of production of dihydrotestosterone, a male hormone associated with 5α-reductase.

<Test Example 3> Clinical trial

1) Clinical trial results for acne patients

Example 15 and Comparative Example 1 were applied twice daily to a place where the sebum secretion of the face is large, mainly in the acne-prone lesions of 15 acne patients. The effect was scored according to the degree felt by the person who participated in the test. The results are shown in Table 6 below.

Skin condition before test 2 weeks after use 4 weeks after use Investigator 1 Example 3 One - + Comparative Example 1 - - Investigator 2 Example 3 2 + ++ Comparative Example 1 - - Investigator 3 Example 3 One ++ +++ Comparative Example 1 + - Investigator 4 Example 3 One + ++ Comparative Example 1 - - Investigator 5 Example 3 One - + Comparative Example 1 - + Investigator 6 Example 3 3 + + Comparative Example 1 + - Investigator 7 Example 3 2 + ++ Comparative Example 1 - + Investigator 8 Example 3 2 - ++ Comparative Example 1 + - Investigators 9 Example 3 3 + + Comparative Example 1 - - Investigator 10 Example 3 2 - + Comparative Example 1 - - Investigator 11 Example 3 3 - + Comparative Example 1 - - Investigators 12 Example 3 2 ++ ++ Comparative Example 1 - - Investigators 13 Example 3 3 + ++ Comparative Example 1 + + Investigators 14 Example 3 One + + Comparative Example 1 - - Investigators 15 Example 3 3 - + Comparative Example 1 - -

Pre-test status: 1 = slight acne, 2 = slight, 3 = severe acne

Effectiveness judgment:-: Almost no effect +: Some effect ++: Much relieved +++: Completely healed

As shown in the results shown in Table 6, soft cosmetics containing N-Acetyl Phydosphingosine, soybean extract, bark extract, and gall bladder extract reduces acne and worsens those who suffer from sebum secretion. It was confirmed to suppress sebum secretion in each part of the face.

2) Skin irritation experiment

Skin irritation test was performed on the composition of the present invention The skin irritation test is a test for evaluating the potential for contact dermatitis in a cosmetic composition to ensure the safety of the cosmetic composition and to minimize skin side effects.

Distilled water, petrolatum, imidazolidinyl urea as a control group was tested by placing the present acne improving cosmetic composition and each active ingredient as a comparison group.

Distilled water and petrolatum on the Finn chamber, Examples 3, 7 were applied to the skin as it is. N-Acetyl Phydosphingosine, soybean extract, bark extract, and gallnut extract were applied to the skin as it is.

A total of 15 women and 10 men were selected as test examiners, and the application site was attached to the medial side of the upper arm of both arms for 30 hours.

False positive reaction (±) Weak positive reaction (+) Probability of Contact Dermatitis (%) Distilled water 0 0 Vaseline 0 0 0 Imidazolidinyl urea 0 3 20 Example 3 0 0 0 Example 7 0 0 0 N-Acetyl Phydosphingosine, 0 0 0 Soybean Extract 0 0 0 Bark Extract 0 0 0 Gallnut extract 0 0 0

As can be seen in the examples and experiments according to the present invention, the N-Acetyl Phydosphingosine, soybean extract, bark extract, and gallnut extract provided by the present invention are excellent in inhibiting 5α-reductase effect. In addition, it was confirmed that the excellent antibacterial effect against P. acnes bacteria, which are acne causing bacteria. In addition, it is a very safe composition that has excellent acne relieving effect when used in humans as a cosmetic composition and does not cause human toxicity and skin irritation, and is applied to the skin at concentrations that do not affect the safety of the product. It is a cosmetic composition that helps to improve acne skin by inhibiting action.

Claims (2)

N-Acetyl Phydosphingosine (N-Acetyl Phydosphingosine) 0.01 ~ 20%, Soybean Extract 0.01 ~ 10%, Bark Skin Extract 0.001 ~ 40%, Barley Extract 0.01 ~ 30% Cosmetic composition characterized in that N-Acetyl Phydosphingosine (N-Acetyl Phydosphingosine) 0.01 ~ 20%, Soybean Extract 0.01 ~ 10%, Bark Skin Extract 0.001 ~ 40%, Barley Extract 0.01 ~ 30% Cosmetic composition comprising a combination of two or more