KR100572003B1 - Composition Containing Bupyeongcho Extract_ - Google Patents

Abstract

The present invention relates to a composition containing a Bupyeongcho extract.

The present invention provides a composition comprising 0.01 to 10% by weight of the dry powdered Bupyeongcho extract.

The composition comprising the extract of Bupyeongcho of the present invention inhibits the activity of 5 alpha-reductase and has excellent antibacterial effect against propionibacterium acnes, resulting in acne, hair loss, seborrheic dermatitis, and seborrheic. It can be used for the prophylactic treatment of dandruff or sebum-related diseases caused by dermatitis.

Description

Composition containing Bupyeongcho extract

[Industrial use]

The present invention inhibits the activity of 5 alpha-reductase to fundamentally suppress the excessive production of sebum, and antibacterial against propionibacterium acnes, a bacterium that worsens acne It relates to a composition containing the Bupyeongcho extract excellent in action.

[Prior art]

Male hair loss, acne, seborrheic dermatitis and dandruff caused by seborrheic dermatitis and the like are known in J. invest. Dermatol, 102, p 221-226, 1994 as chronic skin diseases of androgen dependent disorders.

Male hair loss, which can cause serious mental pain among middle-aged men, is directly related to the amount of testosterone. Recently, many studies for preventing and treating hair loss through testosterone activity inhibition have been reported.

Among chronic skin diseases, acne and seborrheic dermatitis are sebum realted disorders, which are caused by excess sebum produced by testosterone. It must be restrained.

When explaining the action of testosterone in connection with the sebum production mechanism, testosterone, one of the testosterones, is converted to the active testosterone dihydrotesterone by 5 alpha-reductase. Abnormal hyperactivity acts as a substance that causes male hair loss and at the same time acts as a major causative agent for the excessive production of sebum in sebocytes.

If the sebum is abnormally produced or secreted by the above mechanism, sebum-related diseases such as acne, hair loss, seborrheic dermatitis, and the like are caused. As a result, male hair loss, acne, seborrheic dermatitis, and dandruff caused by seborrheic dermatitis are caused by the excessive production of dihydrotestosterone by the action of 5 alpha-reductase, so if the activity of 5 alpha-reductase is inhibited, The fundamental and effective prevention and treatment will be.

Among the diseases, acne is an important factor in the worsening of acne disease in addition to sebum produced excessively. Specifically, if the sebum produced by the mechanism described above is not discharged out of the pores due to the hyperkeratosis of the pores, the primary microsurface (micro comedones) are formed, and by the action of propionibacterium acnes (hereinafter referred to as P. acnes), an anaerobic skin flora present in the sebum of the pores, papules and pustules, chronic inflammatory diseases ), Cysts, nodules, and, if severe, scars. As a result, acne is a disease caused by a variety of complex factors, such as excessive production of sebum, hyperkeratosis of pores, and the action of acne.

Many studies have been attempted to inhibit the activity of 5 alpha-reductase in order to prevent or treat male hormone-related diseases such as acne, androgenetic alopecia, seborrheic dermatitis, and dandruff caused by seborrheic dermatitis, in particular, J. Invest. Dermatol, 104, p775-778, 1995) found several substances that inhibit these activities, but their effectiveness and practicality are small and their use requires considerable attention. In addition, acne is known to have a high possibility of causing side effects such as the appearance of resistant bacteria or photo-sensitization when using antibiotics such as tetracycline as an antibacterial substance against P. acnes.

Therefore, in view of the above problems, the present invention is an enzyme directly involved in the production of active testosterone, which is a fundamental cause of testosterone-related diseases such as acne, androgenetic alopecia, seborrheic dermatitis, and dandruff caused by seborrheic dermatitis. It strongly inhibits the activity of phosphorus 5 alpha-reductase and has excellent antibacterial activity against P. acnes, which is known as the main cause of acne deterioration. Studies have been conducted to strongly inhibit the activity of 5-alpha-reductase at low concentrations and to facilitate the preparation of dermatological compositions containing Bupyeongcho extract with potent antibacterial effects on P. acnes by conventional methods of preparation. will be.

[Means for solving the problem]

The present invention comprises 0.01 to 10% by weight of Bupyeongcho extract in the composition to inhibit the activity of 5 alpha-reductase and antibacterial against propionibacterium acnes It provides a composition for the prevention and treatment of acne, hair loss, seborrheic dermatitis, seborrheic dermatitis and sebum-related diseases exhibiting an effect.

The Bupyeongcho extract is a) powdering the purified Bupyeongcho root; b) extracting the powdered Bupyeongcho root by cooling at room temperature with an extraction solvent; c) filtering the extraction stock solution; d) concentrating the filtered extraction stock solution; And e) lyophilizing the concentrated extraction stock solution to prepare it as a dry powder.

In addition, the extraction solvent is 1 from the group consisting of purified water, methanol, ethanol, propanol, butanol, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, hexane, diethyl ether, dichloromethane. More than one species is selected.

Bupyeongcho of the present invention belongs to lemnaceae, Hakgo is dried dried grass of spirodela polyrrhiza or remna polyrrhiza and was used to heat or edema from ancient times, even in hives It is used.

In the present invention, the extract from the roots of Bupyeongcho as described above, the extract revealed the inhibition rate by the inhibitory evaluation test of 5 alpha-reductase, and the antimicrobial activity against P. acne was found to have an excellent antibacterial effect. Came out.

By this result, Bupyeongcho extract, which strongly inhibits the activity of 5 alpha-reductase, can be easily used as a composition for the prevention and treatment of sebum-related diseases such as acne, male hair loss, seborrheic dermatitis and dandruff caused by seborrheic dermatitis. By using a strong antimicrobial action against P. acnes is to make it easier to manufacture and use compositions for preventing and treating acne.

In addition, Bupyeongcho extract from the efficacy of the Bupyeongcho extract to include in the composition such as face wash, soap, cream, etc. As a result of a clinical experiment (washing agent) to evaluate the bactericidal power for the Ag. There were no side effects such as redness, and the acne treatment effect was excellent.

Bupyeongcho extract containing composition having the activity inhibitory action of 5 alpha-reductase and the antibacterial action against P. acne according to the present invention is applicable to any of the properties such as liquid, cream, paste or solid phase which are different formulations. It is possible.

The composition of the face wash, soap, cream for acne prevention treatment containing the Bupyeongcho extract of the present invention is based on a general product that does not contain excessive fat.

The present invention will be described in detail by the following examples and comparative examples. However, these Examples are only for illustrating the present invention and the present invention is not limited thereto.

EXAMPLE

Example 1

Preparation of Bupyeongcho Extract

The roots of Bupyeongcho were purified, powdered, chilled for 5 days in 10 times the amount of the extraction solvent, and then the extracted extract was filtered, concentrated and freeze-dried to obtain Bupyeongcho extract dried powder.

The extraction solvent used at this time is one or two or more of purified water, methanol, ethanol, propanol, butanol, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, hexane, diethyl ether, dichloromethane Was mixed and used for extraction.

Evaluation of 5 Alpha-reductase Inhibitory Activity of Bupyeongcho Extract

5-alpha-reductase used in 5-alpha-reductase inhibition experiments was obtained from rat liver (adult, sprague-dawley, male rat [8-10 weeks], liver), and a certain amount of protein was determined by protein quantification. A protein suspension was prepared. In addition, an enzyme reaction solution was prepared in a general manner.

As a reaction substrate of 5 alpha-reductase, radiolabeled testosterone (3H testosterone) was used, and the weight ratio of enzyme reaction solution: protein suspension: Bupyeong sec. Extract was mixed at 70: 20: 10. After reacting in an incubator for 2 minutes, the reaction solvent is blown out, the remaining material is dissolved in the developing solvent and developed on a thin layer chromatogram (TLC), and the amount of testosterone and the dihydrotestosterone amount that are developed are measured using a densitometer. Quantitative analysis was carried out to determine the conversion rate of testosterone to dihydrotestosterone by 5 alpha-reductase.

The results were compared with the control (conversion rate without the addition of Bupyeongcho extract) to evaluate the inhibition rate of 5 alpha-reductase.

The inhibition rate evaluation calculation method used the following formula (1).

[Calculation 1]

% Inhibition = [(A-B) / A] x 100

In the above formula, A is the conversion rate of testosterone to dihydrotestosterone when no extract is added, and B is the conversion rate of testosterone to dihydrotestosterone when the extract is added.

Test results by the inhibition rate calculation method is shown in Table 1 below.

TABLE 1

Evaluation of Antimicrobial Activity of Bupyeongcho Extract against Blood Agnes

The antimicrobial activity of the Bupyeongcho extract obtained above was added to a certain concentration of Bupyeongcho extract in P. acnes cultured in liquid medium, and then cultured in an anaerobic culture tank. The minimum inhibitory concentration (MIC) was determined to suppress the growth of Acnes. As a result, the minimum inhibitory concentration (MIC) range of Bupyeongcho extract from each extracting solvent was 50-300 ppm. It was evaluated to exhibit an antimicrobial effect.

Examples 2-7, Comparative Examples 1-3

Preparation of face wash

The dry powder of the face wash base (including water) and the Bupyeongcho extract were prepared in a homo mixer using a homomixer, followed by stirring, heating, and cooling, to prepare a face wash composition having a uniform composition.

TABLE 2

The bactericidal power of the cleanser composition against P. acnes

In order to confirm the effect of preventing and treating acne for the cleanser composition prepared above, P. acnes was inoculated in a petri dish (bacterial dish), and then cultured in an anaerobic culture tank for 3 days, and colonies of P. acnes were collected. The number (N ₁ ) was measured, and the colony water (N ₂ ) was measured after incubating in an anaerobic culture vessel for 3 days or more by dropping 5% aqueous solution of the compositions of Table 2 on a petri dish. The sterilization rate for P. acnes from the colony was evaluated by the formula (2).

[Calculation 2]

% Sterilization rate for P. acnes = (N ₁ -N ₂ ) / N ₁ x 100

N ₁ is the number of colonies of P. acnes first cultured, and N ₂ is the number of colonies of P. acnes after the addition of a face wash. When the sterilization rate of the P. acnes is more than 90% was determined to have a sterilization effect, the results are shown in Table 3.

TABLE 3

Clinical trial of acne prevention and treatment effect of face wash composition

The clinical effects of acne prevention and treatment were measured using a face wash containing the Bupyeongcho extract (experimental group) and a face wash containing no control (control).

Here, the effects of acne prevention and treatment were evaluated by using 10 males in their late teens to late 20's in the experimental group and 10 control groups three times a day for a month.

The determination method was given a certain grade according to the condition of acne before the start of the experiment, and then confirmed the reduction of cotton cloth by visual observation. The determination criteria are as Table 4 below.

TABLE 4

If the grade of acne of clinical trial subjects showed a reduction of grade 3 or more, the effect was excellent. If the grade of 1 or 2 showed a decrease, the effect was moderate. If the decrease did not appear, there was no effect.

The test results for this are shown in Table 5.

TABLE 5

As shown in Table 2, Table 3, and Table 5, the bactericidal power against P. acnes was better than that of the cleanser containing the Bupyeongcho extract, and less than 0.01% by weight of the Bupyeongcho extract was added in the clinical results. The bactericidal power was found to be somewhat low, and addition of more than 10% by weight was excellent in sterilizing power, but there was difficulty in manufacturing.

Therefore, the content of Bupyeongcho extract in the face wash used in the present invention is excellent in sterilizing power and manufacturing workability for P. acnes within the range of 0.01 to 10% by weight.

Examples 8-13, Comparative Examples 4-6

Manufacture of soap

The dry powder of the soap base (including moisture and various additives) and the Bupyeongcho extract were mixed well in the mixer at the composition ratio of Table 6, and then extruded, cut, and molded in a soap maker to prepare a solid soap composition. In addition to the general soap, it could be prepared by including in the synthetic soap and complex soap by a conventional soap manufacturing method.

TABLE 6

Test of bactericidal power on P. acnes

In order to confirm the effect of preventing and treating acne on the soap compositions prepared above, inoculated P. acnes in a petri dish (bacterial dish), and then cultured in an anaerobic culture tank for 3 days, and colonized P. acnes. The number (N ₁ ) was measured, and the colony water (N ₂ ) was measured after incubating in an anaerobic culture vessel for 3 days or more by dropping 5% aqueous solution of the compositions of Table 2 on a petri dish. The sterilization rate for P. acnes from the colony was evaluated by the above formula 2.

When the sterilization rate of the P. acnes is more than 90% was determined to have a sterilization effect, the results are shown in Table 7.

TABLE 7

As shown in Table 6 and Table 7, the bactericidal power of P. acnes was better than the soap containing no Bupyeongcho extract, and the addition of less than 0.01% by weight of Bupyeongcho extract was shown to be somewhat lower. The addition of more than 10% by weight was good sterilization but difficult manufacturing.

Therefore, the content of Bupyeongcho extract in the soap used in the present invention is excellent in sterilizing power and manufacturing workability for P. acnes within the range of 0.01 to 10% by weight.

Examples 14-19, Comparative Examples 7-9

Manufacture of cream

A dry powder of a combination of an oil-based component, an aqueous component, a surfactant, and a Bupyeongcho extract, which is a cream base, was emulsified well in a mixer at a composition ratio shown in Table 8 below, and degassed, filtered, and cooled to prepare a cream composition. Preservatives, chelating agents, fragrances and pigments were added to the composition, and the formulation was prepared in oil / water to have a small amount of oily ingredients. The Bupyeongcho extract was used as a foam cleaning, lotion, It could be added to basic cosmetics such as essences and prepared as a preventive and therapeutic agent for acne.

TABLE 8

Test of bactericidal power on P. acnes

In order to confirm the effect of preventing and treating acne for the cream compositions prepared above, inoculated P. acnes in a petri dish (bacterial dish), and then incubated in an anaerobic culture tank for 3 days, and colonized P. acnes The number (N ₁ ) was measured, and the colony water (N ₂ ) was measured after incubating in an anaerobic culture vessel for 3 days or more by dropping 5% aqueous solution of the compositions of Table 2 on a petri dish. The sterilization rate for P. acnes from the colony was evaluated by the above formula 2.

When the sterilization rate of the P. acnes is more than 90% was determined to have a sterilization effect, the results are shown in Table 9.

TABLE 9

As shown in Table 8 and Table 9, the bactericidal power of P. acnes was superior to the cream containing no cream containing Bupyeongcho extract, and the addition of less than 0.01% by weight of Bupyeongcho extract appeared to be slightly lower. The addition of more than 10% by weight was good sterilization but difficult manufacturing.

Therefore, the content of Bupyeongcho extract in the cream used in the present invention is excellent in sterilizing power and manufacturing workability for P. acnes within the range of 0.01 to 10% by weight.

The composition comprising 0.01 ~ 10% by weight of the Bupyeongcho extract of the present invention inhibits the activity of 5 alpha-reductase and excellent antibacterial effect against propioni bacterium acnes acne, It can be used for the prophylactic treatment of alopecia, seborrheic dermatitis, seborrheic dermatitis or sebum-related diseases.

Claims (3)

Contains Bupyeongcho extract, which inhibits the activity of 5alpha-reductase and has antibacterial effects against propionibacterium acnes, related to dandruff or sebum caused by acne, seborrheic dermatitis, seborrheic dermatitis Composition for preventing or treating a disease. The method of claim 1, The Bupyeongcho extract is contained in the composition 0.01 to 10% by weight. The method of claim 1, The Bupyeongcho extract is a) powdering the purified Bupyeongcho root; b) extracting the powdered Bupyeongcho root by cooling at room temperature with an extraction solvent selected from the group consisting of purified water, methanol, ethanol, propanol and butanol at room temperature; c) filtering the extraction stock solution; d) concentrating the filtered extraction stock solution; And e) freeze-drying the concentrated extraction stock solution to prepare a dry powder Composition prepared by the method comprising a.