KR100368126B1 - Composition capable of inhibiting sebum secretion - Google Patents

Abstract

The present invention contains one or more extracts selected from the group consisting of casualties, white porcelain, and trademarked herb to inhibit sebum that is excessively secreted from the skin, thereby preventing sebum-related diseases such as acne, acne enlargement, pore enlargement, and seborrheic dermatitis. It relates to a composition that can be treated.

Description

Composition capable of inhibiting sebum secretion

The present invention relates to a composition capable of suppressing sebum that is excessively secreted from the skin by containing one or more extracts selected from the group consisting of casualties, white porcelains and trademarked herb.

In general, sebum in the skin including the scalp and face plays a role of keeping the skin moisturizing or preventing the invasion of microorganisms, but when the sebum is excessively secreted, acne worsens, promotes enlargement of pores by acne, and seborrheic dermatitis occurs. However, the substances developed so far are not substances that can eliminate the root cause, but are developed for the purpose of treating diseases such as acne. In addition, the preventive concept is absent.

The secretion of sebum is caused by a number of causes, the most important of which is the activation of cells of the sebaceous gland by the amount of dihydrotestosterone (DHT), one of the hormones involved in promoting sebaceous gland secretion. Sebum is over secreted.

That is, in the sebaceous glands of the skin, testosterone (T) is converted to dihydrotestosterone by 5-alpha-reductase type 1, which binds to receptor proteins in the cytoplasm and nucleus. By entering the inside of the sebaceous gland cells to promote differentiation, sebum (sebum) in the sebaceous glands (sebum) is to cause acne (J. Invest Dermatol 105: 209-214 Diane etc.).

Therefore, the cause of sebaceous hypersecretion was removed to treat and prevent diseases such as seborrheic dermatitis and acne caused by sebaceous hypersecretion.

Thus, the present inventors have studied a substance that can suppress sebum hypersecretion itself in order to prevent or treat the disease by removing the root cause, and search for an active substance among natural products that have already been proven safe as part of such research. As a result, one or more extracts selected from the group consisting of casualties, white porcelains, and trademarked herb have the inhibitory effect of 5-alpha-reductase and the inhibitory effect of lipid biosynthesis, and thus can be found to inhibit excessive secretion of sebum. To complete.

Accordingly, it is an object of the present invention to provide a composition capable of preventing or treating sebum-related diseases by inhibiting sebum excessively secreted from the skin.

In order to achieve the above object, the composition according to the present invention is characterized in that it contains one or more extracts selected from the group consisting of casualty, white porcelain and trademark herb.

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

The general properties, applications, and confirmatory test methods for casualties, white porcelains and trademark candles used in the present invention are as follows.

Tolis Fructus is a fruit of Torilis japonica Decanodolle (Apiaceae), an elliptical standing genus that is flat, 2-4 mm long, and 1 mm in diameter. The outer surface of the branch is grayish yellow to grayish brown with small protrusions at the end, and the lower part has a thin fruit disease. Dorsal side with 3 ribs, suture surface flat, but with 2 brown edges. Casualties are fragrant, taste is a little spicy and irritate the tongue. Man's genitals. It is used for the treatment of weaning, gynecological, arthralgia, and hypothermia (introduction to oriental science).

Thujae semen is a seed of Thuja orientalis, oval to long oval or long cylindrical, 3 to 5 mm long and 2 to 3 mm in diameter. The outer surface is pale yellow to yellowish white, and the old one gradually changes to yellowish brown color and oil leaks out. The outer surface of the seed is often wrapped with a thin membranous inner epidermis, the tip is usually pointed, and has a dark brown spot with a round triangular ridge. The lower part is a dull round and light in color. Microscopic examination of the cross-section of this drug is white to yellowish white, rich in oil, and rich in fat. Sweet, flat, nonpoisonous, and fragrant. The action is to see the heart, relax the mind, help the blood and sweat. The liver and kidneys are moisturized and the lower back is healed and healed. Baekjain has the efficacy of conscience of the god Anyang (안 心 安神) and Yun Jang Tongpyeon (潤腸 通便).

Mandidid ootheca, also known as dung beetle and single herb, is a boiled worm house containing mantidae eggs from the mantis family. This herb is columnar to semicircular, with thin layers of several membranes arranged, stacked 24 to 45 mm long, 2 to 3 cm wide, and 15 to 20 mm thick. The outer side is light brown to yellowish brown, the upper side is liquid intercalated, and the lower side is flat or has marks on the stem of the plant. The nature is sweet, salty, flat and nonpoisonous. It is used for elder oil well, establishment, uno incontinence, and abolition of menstruation.

The present invention provides a composition capable of inhibiting the secretion of sebum in the skin by using the above-mentioned extracts of filamentous, white porcelain and trademark herb as active ingredients.

Extracts of filamentous, white porcelain and trademark herb used in the present invention are concentrated, leached, leached or leached from the medicinal herb again or partially concentrated, or dried again to produce a leaching, premises, regular, flow extract (hereinafter extraction) Extracts) and the chemicals contained in the herb and which have a major effect.

Extraction method of the herbal medicine extract of the present invention is to extract the herbal medicine with lower alcohol, hexane, ethyl acetate or diethyl ether, or extract the fraction of hexane, ethyl acetate, water layer in anhydrous or hydrous ethanol or methanol extract. More detailed description is as follows. Commercially available casualties, white porcelains and trademarked candles are pulverized, and the organic solvents such as ethanol and methanol alone are added to a capacity of 3 to 5 times with respect to the dry weight of the pulverized product, and then 50 minutes in an extractor equipped with a cooling capacitor. Extract by heating for 1 to 10 hours at a temperature of ~ 100 ℃, or by dipping the herbal medicine at the temperature of 0 to 40 ℃ in the solvent for 1 to 30 days to extract the active ingredient. The three herbal extracts thus extracted were completely dried using a reduced pressure evaporator and used as dry powders.

In order to suppress the production of active male hormone which is the cause of excessive secretion of sebum, the activity of inhibiting the activity of 5-alpha-reductase, an enzyme directly involved in the production, the inhibition of Lipogenesis and the cotton wool using rabbit As a result of the reduction test, these herbal extracts were found to be able to inhibit the activity of 5-alpha-reductase and the synthesis of lipids and to reduce the scrim.

Therefore, the composition containing one or more extracts selected from the group consisting of casualties, white porcelain and trademark herb having such efficacy suppresses the excessive secretion of sebum, so diseases caused by the excessive secretion of sebum, for example, acne, seborrheic Dermatitis, dandruff caused by seborrheic dermatitis, pore enlargement by acne, etc. can be prevented or treated.

The composition of the present invention preferably contains one or more extracts selected from the group consisting of casualty, white porcelain, and trademark herb in an amount of 0.001 to 10% by weight, based on the total weight of the composition. This is because when used less than 0.001% by weight, there is no sebum secretion inhibitory effect, when used in excess of 10% by weight may cause irritation to the skin.

The composition of the present invention may be formulated in a conventional formulation that can be applied to the skin, for example, liquid soap, solid soap, facial foam (as well as cosmetics such as lotion, cream, lotion, skin lotion, pack, foundation, etc.) It may be formulated with a human cleanser such as foam). Each of these formulations may contain various bases and additives necessary and appropriate for the formulation of the formulations, and the types and amounts of these components can be readily selected by those skilled in the art.

Hereinafter, the present invention will be described in detail with reference to Examples and Test Examples, but the present invention is not limited to these examples.

Example 1 Preparation of Casualty Extract

150 g of 70% methanol was added to 100 g of the casualties, boiled for about 2 hours in an extractor equipped with a cooling condenser, and then filtered to remove debris to prepare a casualty extract. The extract was concentrated under reduced pressure at 60 ° C. using a distillation apparatus equipped with a cooling capacitor to obtain 2 g of a dry residue.

Example 2 Preparation of White Porcelain Extract

200 g of hexane, a non-polar solvent, was added to 100 g of white porcelain, boiled for about 2 hours in an extractor equipped with a cooling condenser, and then filtered to remove residue and white porcelain extract was prepared. The extract was concentrated under reduced pressure at 60 ° C. using a distillation apparatus equipped with a cooling capacitor to obtain 5 g of a dry residue.

Example 3 Preparation of Extract

200 ml of ethyl acetate was added to 100 g of trademark vinegar, boiled for 2 hours in an extractor equipped with a cooling capacitor, extracted, filtered to remove the residue, and the extract was extracted. The extract was concentrated under reduced pressure at 60 ° C. using a distillation apparatus equipped with a cooling capacitor to obtain 8 g of dry residue.

[Test Example 1] 5-alpha-reductase activity inhibitory effect

Mature Sprogue-Dawley male rats (7-8 weeks old) were killed with diethyl ether, the abdominal prostate was removed, the connective tissue was removed, and buffered (0.32 M sucrose, 0.1 mM dithiothreitol, 20 mM sodium acetate) was added. Finely chopped and then suspended in a grinder. The suspension was centrifuged to obtain the supernatant, partially purified with 5-alpha-reductase, and the activity inhibition experiment of this enzyme was performed.

Taking a portion of the supernatant obtained above was placed in a buffer containing 0.2M monobasic acid and 0.2M dibasic acid, is reacted with isotope substrate (testosterone) marked with ³ H measure the production of dihydro testosterone in product It was.

The reaction solution was added 1 mM dithiothreitol, 40 mM sodium phosphate (pH 6.5), 50 μM NADPH, [1,2,6,7-3H] testosterone / testosterone (2.2 × 10 ⁹ mol), and enzyme suspension (0.8 mg). The total volume was brought to 565 μl.

The sample was dissolved in 10% ethanol to 0.1%, and then 5.65 μl was added to the reaction solution so that the final concentration was 0.001%. The same volume of solvent was used as a control experiment and riboflavin was used as a positive control experiment.

The reaction was started with addition of the enzyme suspension and proceeded at 37 ° C. for 30 minutes, followed by extraction by adding 1 ml of ethyl acetate. 100 μl of ethyl acetate was extracted from silica plastic sheet kieselgel 60 254 (Silica plastic sheet kieselgel). 60 F254), the developing solvent system was developed with acetate-cyclohexane (1: 1).

After air drying the plastic sheet, the bath system was used to measure the isotope amount. The isotopic amount of testosterone and dihydrotestosterone remaining in the film after one week by placing the dried plastic sheet and the x-ray film together in the bath cassette. Was measured.

The results for each inhibition rate are shown in Table 1. On the other hand, the mixing ratio of each embodiment in the sample in Table 1 is 1: 1.

sample T (dpm) DHT (dpm) % Conversion % Inhibition Example 1 7730 2355 23.4 44 Example 2 9330 2721 22.6 46 Example 3 6878 2100 23.4 44 Example 1+ Example 2 6850 1220 15.1 64 Example 1+ Example 3 7350 1400 16.0 62 Example 2+ Example 3 7255 1117 13.3 68 Example 1 + Example 2 + Example 3 9412 1133 10.7 74.5 Control 7530 5546 42 - Positive control 6300 2533 28.7 31.6 (1) T: ³ H radioactivity in the testosterone region (2) DHT: ³ H radio activity (3) conversion in the dihydrotestosterone region (3) Conversion rate: Radio activity / total radio activity in the DHT region (4) inhibition rate : 100 × (conversion rate-conversion rate of sample) / conversion rate of control

From Table 1, it can be seen that one or more extracts selected from the group consisting of filamentous, white porcelain and trademark herb has an effect of inhibiting 5-alpha reductase.

Test Example 2 Lipogenesis Synthesis Inhibitory Effect

The degree of lipid synthesis in sebaceous glands was evaluated by quantifying the uptake of carbon elements required for lipid synthesis to evaluate the degree of inhibition of lipid synthesis.

That is, the degree of inhibition was evaluated by biopsy of hamster ear tissues with many sebaceous glands and comparing the control group and the sample group with a radiometer for 6 hours in a C ¹⁴ labeled medium. As a sample group, 0.01% of the sample solution was added to the medium using hamster right ear tissue, and 0.01% of physiological saline was added to the medium using the hamster left ear tissue as a control group. The results are shown in Table 2.

On the other hand, the inhibition rate in Table 2 is calculated according to the following equation 1, the value is the average value for the four hamsters.

sample % Inhibition Example 1 55 Example 2 43 Example 3 47 Example 1+ Example 2 58 Example 1+ Example 3 66 Example 2+ Example 3 75 Positive control (retinoic acid) 52

From Table 2, it can be seen that the filamentous, white porcelain and trademark herb extracts have an inhibitory effect on lipid biosynthesis, and the effect is increased when used in a mixture rather than in each case.

These results were similar to those of Test Example 1, a testosterone suppression test.

Test Example 3 Cotton Cloth Reduction Effect

In order to confirm the effect of reducing the cotton cloth dry powder (Examples 1 to 3) of the herbal extract, white porcelain and trademark herb extracts used in the present invention were dissolved in 1,3-butylene glycol to 1% solution, It was used as a test material for rabbit clinical trials.

The rabbit's ears are applied with 0.2ml of 50% oleic acid / paraffin oil, a cotton-causing substance, in the morning and rubbed with a cotton swab. It is applied twice a day in the morning (50% oleic acid / paraffin oil), in the afternoon (material) and for a month during the total experiment. Cotton cloth was generated from about 10 days, and the number and size of the cotton cloth gradually decreased from 2 weeks after applying 0.2ml of the material in the afternoon.

After each tissue was biopsied and exfoliated, the scrim size was measured under a microscope. The results are shown in Table 3.

sample Average name cloth size measurement (0.1mm) N = 3 Untreated 1.78 Oleic acid (OA) 3.5 OA + Example 1 3.0 OA + Example 2 2.5 OA + Example 3 2.8 OA + Example 1+ Example 2 2.5 OA + Example 1+ Example 3 2.3 OA + Example 2+ Example 3 2.4 OA + Example 1+ Example 2+ Example 3 2.1

From Table 3, it can be seen that the cotton cloth of the rabbit treated with the herbal medicine according to the present invention was significantly reduced. That is, it can be estimated that sebum reduction is caused by the herbal medicine, and as a result, skin hyperkeratosis is reduced, thereby reducing the cotton cloth.

From Test Examples 1 to 3, it can be seen that the filamentous, white porcelain and trademark herb extracts contained in the composition of the present invention are substances effective in suppressing sebum secretion.

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

In addition to 10 men and women who are suffering from acne, 9 men and women who feel sebum secretion on the face were selected and prescribed according to the formulation example 1 below for 4 weeks for acne and facial sebum secretion.

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.

Formulation Example 1 Nutritional Lotion

ingredient Content (% by weight) Sasangjo + white porcelain + trademark 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

Sebum secretion inhibitory effect Tester Pre-test skin level (㎍ / ㎠h) After 2 weeks of exam 4 weeks after the exam One 77 65 63 2 55 38 43 3 35 43 45 4 88 71 62 5 71 65 55 6 23 33 38 7 48 43 44 8 65 40 46 9 79 66 61

Acne Relief Tester Pre-test state After 2 weeks of exam 4 weeks after the exam One One - + 2 3 ++ ++ 3 2 + ++ 4 One + + 5 2 - + 6 3 - ++ 7 2 ++ +++ 8 One + ++ 9 2 + + 10 2 + ++ * Pre-test: 1-acne slightly 2-acne slightly 3-acne * effect determination; -: Almost no effect +: Slight effect ++: Much less +++: Completely healed

From the results of Tables 4 and 5, it can be seen that the composition according to the present invention can inhibit sebum, and thus alleviate acne.

Below. Although the formulation of the composition of the present invention is exemplified, the present invention is not limited only to these formulation examples.

Formulation Example 2 Cream

Raw material name weight% Filamentous free flowing paraffin cetostearyl alcohol beeswax methyl polysiloxane lipophilic monostearic acid stearate stearic acid sorbitan sesquioleate monostearic acid polyoxyethylene sorbitan (EO = 20) methyl paraben propyl paraben perfume ethylene diamine tetra acetate disodium glycerol propylene glycol triethanol amine Imidazolidinyl urea 0.115.02.03.00.52.02.00.81.01.20.20.10.20.025.05.00.20.3to 100

[Formulation Example 3] Lotion

Raw material name weight% White porcelain Multi wax Sterile EX liquid paraffin dihydride wax be wax 17 Nicol MGS-B alasel ＃ 165 glycerin methyl paraben propyl paraben liquid paraben twin ＃ 60 carbomer tablet water 0.13.60.55.00.80.051.90.77.00.120.035.00.50.12to 100

Formulation Example 4 Flexible Lotion

Raw material name weight% Super paraffin methyl methyl siloxane methyl paraben flavoring polyoxyethylene noryl phenyl ether polyoxyethylene hardening castor oil tocopherol ethanol glycerol ethylene diamine tetra acetate disodium propylene glycol triethanol amine 0.10.050.50.20.20.30.50.110.08.00.023.00.2to 100

[Formulation Example 5] Pack

Raw material name weight% White porcelain + trademark polyvinyl citrate polyvinyl alcohol cellulose gum glycerin polyoxyethylene glycol 400 octyldodecyl ether (E.O. = 16) ethanol preservative pigment flavor water 0.11.014.00.11.01.00.40.6appropriate quantityto 100

[Formulation Example 6] Pack

Raw material name weight% Casualty + trademark Citric acid Polyvinyl alcohol Cellulose gum Glycerin Polyoxyethylene glycol 400 Octyl dodecyl ether (E.O. = 16) Ethanol Preservative Pigment 0.11.014.00.11.01.00.40.6appropriate quantityto 100

Formulation Example 7 Solid Soap

Raw material name weight% Casualty + White porcelain + Trademark Titanium dioxide Polyethylene glycol Glycerine Ethylenediamine Sodium sodium acetate Soap flavoring equipment Nubase (moisture 13%, parts by weight) 0.10.20.80.50.051.0 Suitable for 100

As described above, sebum secretion inhibiting composition containing one or more extracts selected from casualties, white porcelain and trademark herb is very safe when used in humans and has an excellent effect of reducing sebum secretion, thus acne, seborrheic dermatitis, It can be used in effective concentrations for the prevention or treatment of sebum-related diseases such as enlarged pores caused by acne.

Claims (3)

Sebum secretion, white porcelain and trademark herb secretion sebum secretion composition characterized in that it contains one or more extracts selected from the group consisting of. The composition of claim 1, wherein the at least one extract selected from the group consisting of casualties, white porcelains, and trademarked herbs is contained in an amount of 0.001 to 10% by weight, based on the total weight of the composition. The composition according to claim 1 or 2, wherein the composition is an agent for preventing or treating pore enlargement caused by acne or acne.