KR100858196B1 - Dermal composition containning active ingradient extracted from Myristicae semen - Google Patents

Abstract

    The present invention relates to a composition containing a nutmeg extract, and provides a composition comprising 0.01 to 10 weight of lyophilized powdered nutmeg extract.

Composition containing nutmeg extract of the present invention is excellent antibacterial effect against propionibacterium acnes (propionibacterium acnes) can be used for the prevention and treatment of acne and excellent anti-oxidant power for hair products and human body cleansing It can be widely used for reducing skin trouble and improving stability of the product.

Nutmeg Extract, Acne Treatment

Description

Dermal composition containning active ingradient extracted from Myristicae semen}

    The present invention relates to a method for extracting the active ingredient from the nutmeg and a skin composition containing the same, more specifically, excellent antibacterial action against the causative bacteria that worsen acne, peroxidation and skin irritation of sebum components present on the skin surface And it relates to a method for extracting nutmeg active ingredient excellent in antioxidant power that can reduce the degeneration of the product by air contact and a composition for skin containing the same.

    Acne is an inflammatory disease of the fur branch and is a very common skin disease that causes inflammation of the facial skin hair follicles of puberty and young people. It occurs mainly on the face, sometimes on the chest, neck, shoulders, etc. It can remain in your body for a while. In particular, during puberty both male and female secretion of male hormones is active to stimulate the sebaceous gland next to the hair follicles, and as a result, the sebaceous gland becomes large, secreting a large amount of sebum. At the same time, the stratum corneum at the inlet of the pores becomes thicker and the adhesion increases, resulting in narrowing or clogging the pores. As a result, sebum accumulates in the hair follicles and bacteria that are parasitic in the hair follicles multiply and develop into inflammation. In addition to simple inflammation, it can form scars, papules, pustules, cysts and nodules, and when they become more severe, can leave scars, and for those who are sensitive to these lesions, lack of confidence, avoiding interpersonal relationships, anger and depression, etc. It is reported that it can give a disability.

    By the way, the cause of the harmful acne is not yet clear, but generally can be summarized as an increase in sebum secretion, skin keratinization and peroxidation of lipid components, the proliferation of acne-causing bacteria, causing and exacerbating inflammation. One of the important features related to the development of acne is the increase in sebum secretion, which is known to be closely related to the androgen, a male hormone. The secretion of male hormones above normal levels promotes sebaceous gland function, and the excess sebum is stagnated in the hair follicles due to the keratinization of the hair follicle wall, creating scleroderma. Sebum accumulated in the hair follicles, which cannot be discharged to the outside, blocks the pores and prevents the inflow of external air, so the inside of the hair follicles becomes an environment where propionibacterium acnes, which are anaerobic bacteria, can proliferate smoothly. Propionibacterium acnes secrete lipolytic enzymes and chemical factors to produce free fatty acids, trigger the immune response of leukocytes, and destroy the hair follicle walls, causing the contents to leak into the dermis, resulting in inflammatory reactions. . Therefore, the general treatment method for acne can be summarized into four cases, such as suppressing excessive sebum production, inhibiting keratinization of the hair follicle wall, inhibiting proliferation of propionibacterium acnes, and minimizing or inhibiting the inflammatory response.                         

    On the other hand, the treatment of acne includes a topical application and oral therapy, and the surgical treatment such as laser treatment, dermabrasion that is being recently performed. Western medicine uses antibiotics such as tetracycline, azelaic acid and salicylic acid for the antibacterial action of propionibacterium acnes, or for dissolving the scalp. Retinoids, corticosteroids, and the like have been used for the purpose of inhibiting the function of benzoyl peroxide, sebaceous gland and hair follicle wall destruction. However, these preparations require side effects such as skin rashes and dry skin when over-coated and allergic phenomena may be caused by the individual. Therefore, salicylic acid is low in terms of effectiveness and acne due to side effects such as skin rashes. In addition, tetracycline, erythromycin, and clindarmycin, which are used as antimicrobial agents, are excellent in terms of effects, but have side effects such as inducing resistant bacteria and hypersensitivity by light. . In addition, hormone preparations have the disadvantage of increasing capillaries and dilating pores. On the other hand, in oriental medicine, acne is regarded as a chronic inflammatory disease caused by weakened skin immunity due to dysfunction of respiratory system or autonomic dysfunction. The basic principle of acne treatment is clear heat detoxification. The most fundamental treatment is to restore the skin's immune function and blood circulation to normal, and according to the cause of acne, prescribing Cheongsangbangpungtang, Samultang, Byeolhyeoljaktang, and Dangguijaktang, etc. In addition to treating acne by regulating function and blood circulation, it is known to have good effects on intractable skin diseases such as atopic dermatitis and psoriasis. However, the above medicine has the disadvantage of oral medicine, which has the advantage of fundamentally blocking acne by treating internal organs and improving the constitution, but it is not easy to heal long-term constitution problems with short-term oral medicine as well. Even if it is solved, the problem of the onset, advanced acne and other skin diseases remains a problem. Therefore, in consideration of various aspects such as the speed and economical effects of acne treatment, it may be judged that an external medicine used directly on the skin is more effective than the conventional treatment with internal medicine.

    Accordingly, an object of the present invention is to provide a composition that can solve the disadvantages of the conventional acne treatment described above and can easily prevent and treat acne.

    Moreover, another object of the present invention is to provide a method for preparing the composition for treating acne.

    The present inventors have performed a number of studies to achieve the object of the present invention as a result, there is an excellent antimicrobial action against propionibacterium acnes acting as the main causative agent of acne exacerbation, The present invention has been completed by providing a method for finding a natural product containing a highly safe substance and effectively extracting the active ingredient therefrom and a composition containing the same.

    One configuration for achieving the above object of the present invention has excellent antibacterial action against propionibacterium acnes acting as the main causative agent of acne exacerbation and has excellent antioxidant power, inhibiting and peroxidation of sebum components It can be expected to alleviate the phenomenon, extracting and using high-safety material from Myristicae semen, long-term use, containing 0.001% to 10.0% by weight of Myristicae semen extract It is characterized by providing a composition for skin having an effective effect on the treatment of acne.

    Nutmeg, which is a constituent of the present invention, is dried mature fruit of Myristica fragrans Houtt belonging to Myristicaceae. Malaysia, Indonesia, and Sri Lanka are mainly produced in April to June or November to December. Remove the peel and use it. Nutmeg has been used to improve blood circulation, lung function, and sterilization effect, and have been used to improve blood flow, respiratory disorders and skin diseases.

    As described above, the content of the nutmeg extract in the composition for preventing and treating acne according to the present invention is more preferably used 0.005% by weight to 5.0% by weight. If the amount is less than 0.005% by weight, the antimicrobial activity against propionibacterium acnes may be somewhat insufficient, and the antioxidant effect is low, so it is difficult to expect the peroxidation inhibitory effect of the sebum component. This will be halved. On the other hand, when using 5.0% by weight or more, it is difficult to manufacture the composition and ensure long-term stability.                     

    The nutmeg extract-containing skin composition can be applied to any shape, such as liquid, cream, paste or solid, so that it can be used on face creams, lotions, skin lotions, packs, foundations, makeup bases, as well as soaps, facial foams and body cleansers. It is also applicable to hair products such as cleaning agents, shampoos and rinses, and, if necessary, components commonly used in external preparations for skin within the scope of not impairing the effects of the present invention, for example, aqueous components, oily components, and surfactants. It can be combined with a moisturizer, a thickener, a preservative, a fragrance, a pigment, and the like.

    Moreover, it can also be used together with antibacterial agents, such as benzoyl peroxide, tetracycline, erythromycin, and triclosan, which are used for the conventional acne treatment, hormones, such as androgens, steroids, and vitamin A derivatives, such as a retinoid.

    The active ingredient of nutmeg according to the present invention can be extracted by the extraction method of the plant extract using a conventional solvent, it can be extracted by the following method as one embodiment.

a) powdering the nutmeg;

b) extracting the powdered nutmeg with a solvent;

c) filtering the extract filtrate;

d) concentration of the filtrate by distillation under reduced pressure;

e) freeze drying the concentrated filtrate to powder.

    The solvent used in the b) extraction step is purified water, methanol, ethanol, propanol, isopropanol, butanol, acetone, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, hexane, diethyl ether , Dichloromethane is selected from the group consisting of at least one.

    It is more preferable to use polar solvents, such as purified water, methanol, ethanol, acetone, glycerol, propylene glycol, 1, 3- butylene glycol, in the said extraction solvent. Nutmeg extracts obtained using nonpolar solvents such as hexane, diethyl ether, and dichloromethane also exhibit antimicrobial and antioxidant effects on propionibacterium acnes, but are relatively relatively extracted compared to extracts using polar solvents. The yield is low, solubility and ease of emulsification may be difficult when preparing the composition for the skin.

    The composition of the present invention having the above-described composition is a nutmeg extract contained in the composition shows a strong antimicrobial effect against propionibacterium acnes, and excellent antioxidant power to alleviate the peroxidation and keratinization of sebum components It can be good for acne treatment.

    In addition, nutmeg of the present invention is a plant that has been used in herbal medicine for a long time, even in the case of ingestion of the body, the stability of the human body is confirmed, and it is an excellent safety plant having almost no irritation to the skin and mucous membranes.

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

Example 1

100 g of powdered powdered nutmeg (dried herbal) was added to 1000 g of methanol (80%), which was immersed at room temperature for 1 week, followed by repeated extraction and filtration twice. The filtrate was concentrated by distillation under reduced pressure, and freeze-dried again. 19.5 g of powder were obtained.

Examples 2-3, Comparative Examples 1-2

Soap and skin lotion containing 0.5% by weight of the nutmeg extract obtained according to Example 1 was prepared by the composition shown in Tables 1 and 2. Each comparative example is the same as the composition of each Example except not containing the nutmeg extract.

Composition of face-wash soap for measuring effect Name Example 2 Comparative Example 1 Palm oil fatty acid 2.0 2.0 glycerin 0.5 0.5 Titanium dioxide 0.3 0.3 EDTA-2Na 0.1 0.1 Spices Quantity Quantity Color Quantity Quantity Nutmeg Extract 0.5 - Soap Chips (Base) Remaining amount Remaining amount Sum 100 100

(weight %)

Composition of skin lotion for measuring effect Name Example 3 Comparative Example 2 ethanol 5.0 2.0 glycerin 3.0 0.5 1,3-butylene glycol 3.0 0.3 Polyoxyethylene alkyl ether 0.5 0.1 Spices Quantity Quantity Nutmeg Extract 0.5 - Purified water Remaining amount Remaining amount Sum 100 100

                                                                (weight %)

Examples 4-8

Cream, lotion, liquid foundation, essence and cleansing foam containing 0.5% by weight of the nutmeg extract obtained according to Example 1 were prepared in the compositions shown in Tables 3 to 7.

Cream composition stearic acid 8.0  glycerin 5.0  Squalene 5.0  Propylene glycol 3.0  Self-emulsifying glycerin monostearate 2.5  Monostearic acid polyoxyethylene sorbitan (20 E.O.) 1.5  Vaseline 1.5  Spices Quantity  antiseptic Quantity  Nutmeg Extract 0.5  Purified water Remaining amount  Sum 100

(weight %)

The composition of lotion  Liquid paraffin 5.0  glycerin 3.0  Squalene 3.0  Propylene glycol 3.0  Vaseline 2.0  ethanol 2.0  Monostearic acid polyoxyethylene sorbitan (20 E.O.) 1.5  Triethanolamine 0.5  Spices Quantity  antiseptic Quantity  Nutmeg Extract 0.5  Purified water Remaining amount  Sum 100

(weight %)

Liquid foundation composition  Titanium dioxide 8.0  Myristic acid isopropyl 5.0  Talc powder 5.0  Liquid lanolin 3.0  Liquid paraffin 3.0  glycerin 3.0  Bentonite 0.5  Cetostearyl alcohol 0.5  Carboxymethyl Cellulose Sodium 0.3  Coloring pigment Quantity  Spices Quantity  antiseptic Quantity  Nutmeg Extract 0.5  Purified water Remaining amount  Sum 100

(weight %)

Essence composition  Sorbitol 8.0  Polyoxyethylene glycol 1500 6.0  ethanol 5.0  glycerin 3.0  1,3-butylene glycol 3.0  Polyoxyethylene oleyl alcohol ether 1.0  olive oil 0.3  Hyaluronic acid 0.2  Spices Quantity  antiseptic Quantity  Nutmeg Extract 0.5  Purified water Remaining amount  Sum 100

(weight %)

Lenzing Foam Composition  Myristic acid 15.0  Stearic acid 12.0  Potassium hydroxide 5.0  glycerin 3.0  1,3-butylene glycol 3.0  Monostearic acid polyoxyethylene sorbitan (20 E.O.) 2.0  EDTA-2Na 0.1  Pigment Quantity  Spices Quantity  antiseptic Quantity  Nutmeg Extract 0.5  Purified water Remaining amount  Sum 100

                                                               (weight %)

Test Example 1.

 Determination of Antimicrobial Activity

Antibacterial activity was measured by a broth dilution method using a 96-well microplate. Each well of a 96-well microplate is infused with heat-sterilized Brainheart Infusion Broth Medium (BHI broth), followed by two-fold dilution of the extract sample. After injecting the test cell suspension into all wells, the cells are incubated anaerobicly at 37 ° C. After incubation for 3 to 4 days, the alamar blue solution is dispensed into each well and incubated for about 1 hour, and then the color development is observed to determine the concentration of the color change from blue to pink as the MIC value. . The results are shown in Table 8 below.

Antimicrobial Activity against Propionibacterium acnes sample MIC (ppm) ATCC 6919 Nutmeg Extract 20 to 40 Triclosan 20 to 40 Benzoyl peroxide 1000

As shown in Table 8, the nutmeg extract obtained in Example 1 not only shows a very good antibacterial activity compared to benzoyl peroxide, which has been used as an active ingredient in conventional acne treatment, but also compared with triclosan, which is known to have a wide range of antibacterial activity. It had an equivalent effect. Therefore, when the nutmeg extract of the present invention is formulated into a skin composition for the purpose of preventing and treating acne, it is expected to exhibit an excellent healing effect.

Test Example 2

 Measurement of Antioxidant Effect

After dissolving the extract sample in an appropriate concentration in ethanol, a sample solution of various concentrations is prepared through step dilution. 50 μl of each sample solution is added to each well of a 96-well microplate, and then 100 μl of DPPH (1,1-Diphenyl-2-picrylhydrazyl) solution dissolved in ethanol at 20 mM concentration. The change in absorbance is measured at 517 nm over a fixed time. The reaction was carried out for 30 minutes, and the concentration of the sample showing 50% of the initial absorbance was represented _by the value of SC ₅₀ , and the antioxidant effect was evaluated using the result, and the results are shown in Table 9 below.

Antioxidant Effect through DPPH Radical Scavenging Activity sample SC50 (517 nm.ppm) Nutmeg Extract 201.9 Butylene hydroxy toluene (BHT) 243.3

As shown in the table, the nutmeg extract obtained in Example 1 has been shown to have an excellent antioxidant effect compared to BHT which has been commonly used as an antioxidant. From the above results, when the nutmeg extract is used in combination with the skin composition, it can be expected not only to suppress the peroxidation and keratinization of lipid components, but also to improve the safety on the skin and the phase stability of the composition.

Test Example 3

 Evaluation of Antimicrobial Activity of Nutmeg Extract Containing Composition

In order to evaluate the antimicrobial effect of the nutmeg extract-containing composition according to the present invention, a paper-disk method was used for the facial soap prepared according to Example 2 and Comparative Example 1. After diluting each composition with a 10% solution, the paper-disk (diameter 8 mm) was immersed in the solution for the same time, taken out, and placed on an agar plate inoculated with the test bacteria and incubated. After incubation for 1 to 2 days, the antimicrobial effect of the composition was qualitatively determined by measuring the presence or absence of the development zone around the paper-disk and the results are shown in Table 10.

Antimicrobial Activity against Propionibacterium acnes sample Diameter of growth inhibition zone (mm) ATCC 6919 Example 2 (10% solution) 14 Comparative Example 1 (10% solution) Lowland not formed

As a result of evaluating the antimicrobial effect on the diluted solution of the face-wash soap containing the nutmeg extract of the present invention, as shown in Table 10 above showed a very excellent effect. According to these results, the skin composition containing the nutmeg extract of the present invention, that is, it can be expected to prevent and treat the acne of the facial soap.

Test Example 4

 Evaluation of Acne Treatment Effects

In order to evaluate the clinical effect of the nutmeg extract-containing composition according to the present invention on the prevention and treatment of acne, the skin lotion prepared according to Example 3 and Comparative Example 2 was tested in acne holders. That is, using the skin lotion prepared according to Example 3 and Comparative Example 2 twice a day for 3 weeks targeting 40 women with acne symptoms and classified the condition of acne according to the criteria of Table 11 Judgment was made by comparison with the naked eye and photographing, and the results are shown in Table 12.

Rating Skin condition 0 normal One Small number of cotton veins 2 Medium cotton patch without inflammation 3 Scalp of inflammatory papules 4 Small nodules and inflammatory scalp 5 Papular nodules 6 Moderate inflammatory nodules 7 Large number of inflammatory nodules 8 Severe nodular scalp 9 Severe cystic and inflammatory nodules

※ If the skin condition of acne in clinical trial subjects showed more than 3 grade reduction compared with the beginning of the experiment, it is excellent. It was.

Evaluation of Acne Treatment Effects division Grading system Great Good no effect worse Example 3 15 (75%) 5 (25%) - - 20 (100%) Comparative Example 2 - 4 (20%) 14 (70%) 2 (10%) 20 (100%)

Acne prevention and treatment of the skin composition according to Example 3 in the present invention was found to have a very excellent effect compared to the comparative example as shown in Table 11.

As described above, the method of extracting the nutmeg active ingredient according to the composition of the present invention and the composition for skin containing the same provide a method of easily obtaining the nutmeg active ingredient exhibiting an excellent effect on the prevention and treatment of acne, A composition for skin containing in proportion is a useful invention that shows an excellent effect on the prevention and treatment of acne.

Claims (4)

A composition for preventing and treating acne, characterized in that it contains extracts of nutmeg (Myristicae semen). The composition for preventing and treating acne of claim 1, wherein the extract contains 0.005% to 5.0% by weight on a dry weight basis. Using the mature fruit of Myristica fragrans Houtt belonging to the Myristicaceae a) powdering the nutmeg; b) powdered nutmeg consists of purified water, methanol, ethanol, propanol, isopropanol, butanol, acetone, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, hexane, diethyl ether, dichloromethane Extracting with at least one solvent selected from the group; c) filtering the extract filtrate; d) concentration of the filtrate by distillation under reduced pressure; e) extracting the nutmeg active ingredient, characterized in that it comprises the step of lyophilizing the concentrated filtrate into a powder. The method of claim 3, wherein the extraction solvent is at least one solvent selected from purified water, methanol, ethanol, acetone, glycerol, propylene glycol, 1,3-butylene glycol.