KR20170142632A - Composition of functional cosmetics and over the counter drugs for treating and improving acne - Google Patents

Abstract

The present invention provides a composition for treating and alleviating acne, which comprises tranexamic acid (TXA), phytosphingosine-1-phosphate, and a microalgae extract as effective components. By comprising tranexamic acid (TXA), phytosphingosine-1-phosphate, and a microalgae extract as effective components, the composition for treating and alleviating acne according to the present invention is highly effective in treating acne and restoring the skin, and can effectively remove scars and discoloration caused by acne, and thus may be effectively utilized in the production of quasi-drugs or cosmeceutical products relating to acne treatment and alleviation.

Description

TECHNICAL FIELD [0001] The present invention relates to a composition for treating and improving acne,

The present invention relates to a composition for treating and improving acne.

Acne is one of the inflammatory skin diseases that occur in various age groups, and the age range of onset is increasing due to genetic factors, westernization of diet, hormone imbalance or stress.

Although the precise cause of acne is not known, it is mainly caused by an increase in sebum secretion, secretion of hormones that stimulate sebaceous glands such as androgen, and the production of Propionibacterium acnes acnes ), follicular abnormal keratinization, and genetic problems are known to play a multiplicative role. In addition, it is known that aerobic dermatophytes are known to further exacerbate inflammation and thereby exacerbate acne. Ultimately, it is known that sebum secreted from the skin can not escape from the skin and accumulate in the skin.

Recently, as interest in skin beauty has increased, the occurrence of acne has caused various psychological diseases such as psychological pressure, loss of self-confidence, and depression, and various studies for treating acne have been conducted .

Conventionally, in order to treat the above-mentioned acne, acne is treated by various methods such as topical treatment, light treatment, physical treatment or systemic treatment. In particular, topical treatment is an anti-androgen agent for suppressing sebum production, Steroidal anti-inflammatory agents, resorcinols having antimicrobial effects, or various antibiotics. However, these methods are effective for the treatment and prevention of acne, but may cause adverse effects such as impairing the stability of the skin. In order to minimize side effects, research has been carried out on methods of using natural products to treat acne.

For example, the prior art document 1 discloses a technical content of a composition for preventing or treating acne including natural antibiotics such as burdock extract, willow extract, green tea extract, papaya extract, chitosan and phytosphingosine have.

As another example, the prior art document 2 discloses a composition for treating acne containing azelaic acid as an active ingredient and a cosmetic composition for improving acne using the same.

However, since the compositions disclosed in the above documents 1 and 2 are limited only for the purpose of treating acne, it is difficult to effectively manage scars and pigmentation caused by acne after acne, The wound healing and regenerating ability of the skin is reduced, and the type of treatable acne is limited. Therefore, there is a problem in that people who experience acne disease have limitations in using it for improving skin beauty. There is a need for research on how to do this.

Korean Patent Publication No. 10-2010-0096394 (Disclosure Date: Sep. 2, 2010) Korean Patent Laid-Open No. 10-2011-0133198 (published on December 12, 2011) Korean Patent Publication No. 10-2013-0089045 (Publication date: 2013.08.09) Korean Patent No. 10-1427035 (Publication date: 2014.08.05)

Disclosure of the Invention The present invention has been conceived to solve the problems of the prior art as described above, and it is an object of the present invention to provide an acne treatment method and an acne treatment method which can effectively manage acne, And to provide a technical content of the composition for treatment and improvement.

In order to accomplish the above object, the present invention provides a method for treating and improving acne including tranexamic acid (TXA), phytosphingosine-1-phosphate and microalgae extract ≪ / RTI >

Also, the present invention is characterized in that the above-mentioned extracts of tranexamic acid, phytosphingosine-1-phosphate and microalgae are contained in an amount of 1 to 20% by weight based on the total weight of the composition.

Also, the microalgae extract may include polysaccharides including fucans and galactan; And omega-3, omega-6, dihomo-gamma-linolenic acid, eicosapentaenoic acid (EPA), benzoyl peroxide, And a fatty acid containing at least one member selected from the group consisting of salicylic acid.

In addition, the composition is characterized by having a formulation selected from the group consisting of lotion, milky lotion, cream, essence, cosmetic lotion, spray, gel, pack, sunscreen, makeup base, foundation, powder and detergent.

In addition, the present invention provides an external preparation for skin for treating and improving acne, which comprises tranexamic acid, phytosphingosine-1-phosphate and microalgae extract as an active ingredient.

Also, the external preparation is characterized in that it has a formulation selected from the group consisting of ointments, patches, gels, creams and sprays.

The composition for the treatment and improvement of acne according to the present invention is a composition for treating and improving acne, which comprises tranexamic acid, phytosphingosine-1-phosphate and microalgae extract as an active ingredient and has high acne treatment and regenerative effect, It can effectively be applied to quasi-drugs or cosmeceutical products related to the treatment and improvement of acne.

1 is a table showing compositions of acne treatment compositions of Examples and Comparative Examples.

Hereinafter, the present invention will be described in detail.

The present invention provides a composition for treating and improving acne comprising, as an active ingredient, tranexamic acid (TXA), phytosphingosine-1-phosphate and microalgae extract.

The above-mentioned tranexamic acid is an amino acid derived from lysine, has a function of restoring skin barrier and restoring damaged skin, and has an effect of improving and converging skin condition. In addition, it acts as a plasmin inhibitor that inhibits activated mast cells, thereby preventing the melanin pigment from spreading widely, and thus has an excellent effect of improving the chloasma, which has a clear brown or blackish brown hue.

However, the above-mentioned tranexamic acid acts as a hemostatic agent, which can cause blood clots, interfere with blood circulation, and has a very high crystallinity, so crystals can easily be formed when exposed to oxygen.

The above-mentioned phytosphingosine-1-phosphate is a derivative of trimethylphytosphingosine, which is abundantly present in platelet rich plasma (PRP), and has an effect of proliferating human hypodermal cells even at a low concentration It can be expected that an excellent regeneration effect can be expected when it is introduced into the skin and can be effectively included in the composition because scars generated by the onset of acne or wound areas generated after acne removal can be effectively treated.

The microalgae extract can exhibit inflammatory acne treatment and improvement effect, prevention of skin aging and skin regeneration effect, and can be included in a composition for treating and improving acne. The above extracts of polysaccharides and fatty acids include polysaccharides and fatty acids.

In more detail, the microalgae extract contains a polysaccharide to effectively treat inflammatory acne and has an excellent skin improving effect. The polysaccharide may be exemplified by fucan and galactan.

The fucan is excellent in anticoagulant and antithrombotic activity and can effectively inhibit the inflammatory reaction caused by stimulation of keratinocytes forming the skin and prevent the blood coagulation action of the tranexamic acid, Can be included in a composition for treating and improving acne, and fucans extracted from fucus- derived fucus sp. Can be preferably used.

The galactan is excellent in water retention ability and can maintain the moisture of the skin constantly, thereby preventing crystal formation of the truncated triacid and minimizing skin irritation due to crystal formation. In addition, it has a pH control function that keeps the concentration of the ionic substance constant, and it can act as a skin osmotic pressure control, and has anticoagulant activity, antiviral activity, and anti-inflammatory activity, And galactan extracted from red algae derived asparagraphs ( Asparagopsis sp) can be preferably used.

In addition, the microalgae extract has an antibacterial activity against causative bacteria that cause acne including fatty acids, and effectively treats acne, thereby exhibiting an excellent skin improving effect. The fatty acids are omega-3, omega- 6 omega-6, dihomo-gamma-linolenic acid, eicosapentaenoic acid (EPA), benzoyl peroxide, and salicylic acid.

In order to effectively treat and treat acne caused by various causes, the composition for treating and improving acne according to the present invention is characterized in that the above-mentioned extracts of tranexamic acid, phytosphingosine-1-phosphate and microalgae To 20% by weight of the composition. In order to prepare a composition for treating and improving acne suitable for the application, the content of each component can be adjusted.

In addition, the concentration of the above-mentioned tranexamic acid may be 0.01 to 30 mg / g to maximize the effect of the tranexamic acid. When the concentration of the tranexamic acid is less than 0.1 mg / g, it is difficult to expect skin regeneration and whitening effect due to the low concentration of tranexamic acid, and when the concentration of tranexamic acid exceeds 300 mg / g , The further increase in skin regeneration and whitening effect of tranexamic acid is no longer increased.

Also, the phytosphingosine-1-phosphate may be contained at a concentration of 0.001 to 1 mg / g to maximize the effect of phytosphingosine-1-phosphate. If the concentration of the phytosphingosine-1-phosphate is less than 0.001 mg / g, the concentration of the phytosphingosine-1-phosphate is low and the skin regeneration and whitening by the phytosphingosine- If the concentration of the phytosphingosine-1-phosphate exceeds 1 mg / g, the further increase in the skin regeneration and whitening effect of the phytosphingosine-1-phosphate is further increased I never do that.

In addition, the microalgae extract may be contained in an amount of 1 to 20% by weight to maximize the effect of the microalgae extract. When the microalgae extract is contained in an amount of less than 1% by weight, it is difficult to expect a therapeutic effect by the microalgae extract because the concentration of the microalgae extract is low. When the microalgae extract is contained in an amount of more than 20% No further increase in the effect of the microalgae extract is further increased.

The composition for treating and ameliorating acne according to the present invention may be used singly in the form of a hydrate or solvate of a composition or a composition, and may be pharmaceutically acceptable Nutritional acceptable carriers, excipients, stabilizers, foaming agents, fragrances, surfactants, water, ionic or nonionic emulsifiers, fillers, sequestering and chelating agents, preservatives, vitamins, May contain adjuvants conventionally used in the field of dermatology, such as topical agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or any other ingredient commonly used in external preparations for skin.

In addition, the composition for treating and improving acne according to the present invention can be prepared in the form of a hydrogel containing a water-soluble polymer, and it is also possible to provide an effective treatment of acne when the active ingredient is sufficiently contained, The active ingredient can be released continuously.

Particularly, the water-soluble polymer may be at least one selected from the group consisting of bio-cellulose, gelatin,? -Lactoglobulin, whey, soy protein, potato protein, hazelnut protein, wheat protein, poly-L-lysine, casein, casein, soybean glycine, Corn starch, methyl cellulose, ethyl cellulose, hydroxypropylmethyl cellulose, cellulose nitrate, carboxymethyl cellulose, gum arabic, xanthan gum, mesquat gum, guar gum, carrageenin, tragacanth gum, arabinogalactan , Galactomannan, pectin, agar, dextran, chitosan, zein, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate, polyvinylacetate phthalate, poly (p-dioxanone), poly (? -valerolactone), poly (? -hydroxybutyrate), poly (? -hydroxybutyrate) and? -hydroxy valerate Poly (? -Hydroxypropionate), methyl acrylate copolymer, dimethylaminoethyl methacrylate copolymer, trimethylammonium ethyl methacrylate copolymer, polymers and copolymers of lactic acid and glycolic acid, lactic acid and glycolic acid And polymers and copolymers of polyethylene glycol, or mixtures thereof. Preferably, a bio-cellulose or fermented bio-cellulose made of natural materials is used, so that a good adhesion property of natural materials and a low- A hydrogel pack can be prepared.

Alternatively, a water-soluble polymer such as polyacrylic acid, sodium polyacrylate, polyacrylamide, polyvinyl alcohol, polyvinyl pyrrolidone or a mixture thereof may be used.

As described above, the composition for treating and improving acne according to the present invention can be used in formulations such as lotion, milky lotion, cream, essence, cosmetic ointment, spray, gel, pack, sunscreen, makeup base, foundation, powder or detergent .

The composition for treating and improving acne according to the present invention may further comprise at least one selected from the group consisting of a nutrient, a vitamin, an electrolyte, a flavoring agent, a colorant, a thickening agent, a pectic acid, an alginic acid, an organic acid, a protective colloid thickening agent, a pH adjusting agent, a stabilizer, Alcohols, carbonating agents used in carbonated drinks, and the like.

As described above, the composition for treating and improving acne according to the present invention contains tranexamic acid, phytosphingosine-1-phosphate and microalgae extract as an active ingredient and has high therapeutic and regenerating effect against acne, , Pigmentation and the like can be effectively removed, and thus it can be effectively applied to the production of quasi-drugs or cosmeceutical products related to the treatment and improvement of acne.

In addition, the present invention provides an external preparation for skin for treating and improving acne, which comprises tranexamic acid, phytosphingosine-1-phosphate and microalgae extract as an active ingredient.

The external preparation for skin may be formulated into ointments, patches, gels, creams, or spray formulations, and may be formulated with a base such as vaseline or stearyl alcohol, a surfactant such as polysorbate or sorbitan sesquioleate, a moisturizing agent such as glycerin, The present invention can be produced by a method for producing a conventional external preparation for skin, which comprises uniformly mixing a flavor, a colorant, a stabilizer, a tackifier, a pharmaceutically acceptable solvent, and the like.

Hereinafter, the present invention will be described in more detail with reference to examples.

The embodiments presented are only a concrete example of the present invention and are not intended to limit the scope of the present invention.

<Examples>

A mixed solution containing acetone and chloroform in a weight ratio of 9: 4 was added to a culture of microalgae ( Asparagopsis armata (KIOST) microalgae and brown algae derived fucus vesiculosus (KIOST) Nitric acid was added sequentially, followed by centrifugation at 10,000 rpm for 10 minutes to precipitate proteins and lipids, and supernatant was obtained. The resulting supernatant was filtered through a polysulfone nanofiltration membrane which excluded a molecular weight of 100,000 Mw and the supernatant was filtered to separate polysaccharides from microalgae derived from algae and brown algae. The supernatant was separated and purified by HPLC to separate and purify galactan from red algae, and the fucan derived from brown algae was separated and purified. The HPLC column used a 5 占 C18 column (5 占 퐉, 4.6 占 250 nm). The solvent for the analysis was a 0.1% trifluoroacetic acid (TFA) aqueous solution (solvent A) and acetonitrile (solvent B) and was detected at a wavelength of 300-400 nm at a flow rate of 1 ml / min.

In addition, microalgae fatty acids were isolated using a microalgae culture of the genus Aurantiochytrium limacinum (KIOST). Separation of fatty acids was performed by supplying the supernatant with a lyophilized culture powder and extracting the fatty acid under the condition of supercritical carbon dioxide to obtain a fatty acid powder by separating fatty acids contained in the microalgae.

The composition for treating acne including fungi, galactan and fatty acid derived from microalgae obtained as described above was prepared from LTBio (Product No. 4166) and Phytosphingosine-1-phosphate (BASF) The composition of the prepared composition is shown in Fig.

The prepared acne treatment composition was mixed with a hydrogel composition containing polyvinyl alcohol and a polyacrylate resin in a composition as shown in Table 1 to prepare a hydrogel ointment for treating acne. The hydrogel composition was prepared by mixing.

<Experimental Example 1> Confirmation of whitening effect

(1) Melanocyte inhibitory ability assay

An aqueous solution of the composition prepared by the method according to the Example was mixed with purified water so as to have a final volume of 150 g, and the aqueous solution of the composition was added to the culture solution of mouse melanoma cells (B-16 mouse melanoma cell) And cultured for 2 days. After replacing the culture medium, trypsin was added to the cell culture for another 2 days, and the melanin was extracted by centrifuging the culture. The absorbance was measured by adding NaOH to the mixed melanin solution and compared with the control , The whitening effect of the aqueous composition solution was analyzed at the cell level using the following equation (1). The results are shown in Table 2 below.

[Equation 1]

Melanin production inhibition rate (%) = 100 X (absorbance of test substance / absorbance of control group)

(TXA) and phytosphingosine-1-phosphate (P-1-P) in the samples treated with the compositions for treating acne in Examples 1-1 to 1-4, It was confirmed that the melanin production inhibitory effect was increased with the increase of the content of the antioxidant, and the melanin production inhibitory effect of the composition for treating acne in Comparative Example 1 was insignificant, and the content of the composition for treating acne in Comparative Example 2 was increased It was confirmed that no additional melanin formation inhibitory effect was observed.

(2) Analysis of human skin whitening effect

To examine the whitening effect of the human skin on the hydrogel ointments of Examples 2-1 to 2-4, 20 healthy male and female subjects were divided into three rows each having three holes each having a diameter of 20 mm at the lower part of both arms of the subject Using a solar simulator at a distance of 15 cm from the arm, apply a fine aluminum foil and induce skin blackening by irradiating an ultraviolet B (UV B) of 1.5 to 2 times the Minimal Erythma Dose Respectively.

The hydrogel ointments of Examples 2-1 to 2-4 were applied twice a day to each site where skin blackening was induced. After 45 days, skin tone was measured using a colorimeter. The determination of the whitening effect exhibited by the hydrogel ointment was determined by determining the light value (L) of the skin. The L value was measured using a colorimeter (Chromameter, Minolta CR-200). In addition, the whitening effect was determined by the difference in skin chromaticity difference (? L) between the time before the application of the hydrogel ointment and the time after 45 days from the application using the following formula (2), and the results are shown in the following Table 3 .

&Quot; (2) &quot;

ΔL = L value at the end of 45 days of application - L value at the time of application

As shown in Table 3, it was confirmed that the hydrogel ointment of Comparative Example 3 had a negligible whitening effect, and the hydrogel ointment of Examples 2-1 to 2-4 showed an excellent whitening effect by increasing the whitening effect I could. However, as can be seen from the hydrogel ointment of Comparative Example 4, it was confirmed that the whitening effect was not further increased even when the content of the trinectamic acid and the phytosphingosine-1-phosphate was increased.

Further, it was confirmed that no crystals were formed on the surface even after 45 days from the opening of the hydrogel ointment so that the tranexamic acid can be stably carried.

&Lt; Experimental Example 2 >

(1) Inhibitory effect on erythema formation

In order to analyze the acne disease improving effect of the same composition as in Experimental Example 1, the effect of an aqueous solution of composition for improving acne against erythema induced by Propionibacterium acnes ATCC 6919 was confirmed in vivo.

A mixture of 10 μl of the culture broth of Propionibacterium acnes strain at a concentration of 5 × 10 ⁸ CFU / ml and 20 μl of the aqueous solution of the composition for improving acne according to Example 1-3 was injected subcutaneously in the left ear of the mouse, and after 36 hours At the time point, erythema of the mouse ear was observed with a microscope, and a mouse injected with the same amount of the culture solution of Propionibacterium acnes strain was used as a control.

As a result, it was visually confirmed that the rate of erythema reduction in the mouse injected with the aqueous solution of the composition for improving acne according to Example 1-3 was reduced by 70% or more as compared with that of the mice of the control group.

(2) Confirming the growth inhibitory effect of acne causing bacteria

10 μl of the culture broth of Propionibacterium acnes strain at a concentration of 5 × 10 ⁸ CFU / ml, and 20 μl of the aqueous solution of the composition for improving acne according to Examples 1-1 to 1-4 and Comparative Example 1 in a BHI medium The cultures were cultured under anaerobic conditions. The cultures were cultured in the presence of 10 μl of a culture medium containing no aqueous solution of acne improving composition as a control. Respectively.

As a result, it was confirmed that acne causative bacteria were proliferated in the medium treated with the control group and the aqueous solution of the composition for improving acne according to Comparative Example 1. However, in the medium treated with the aqueous solution of the composition for improving acne according to Examples 1-1 to 1-4 It was confirmed that the composition for improving acne effectively inhibited the growth of the causative agent of acne.

Claims (6)

A composition for treating and improving acne comprising tranexamic acid (TXA), phytosphingosine-1-phosphate and microalgae extract. The method according to claim 1,
Wherein the extract of tranexamic acid, phytosphingosine-1-phosphate and microalgae is contained in an amount of 1 to 20% by weight based on the total weight of the composition. The method according to claim 1,
Wherein the microalgae extract comprises fucan and galactan; And omega-3, omega-6, dihomo-gamma-linolenic acid, eicosapentaenoic acid (EPA), benzoyl peroxide, And a fatty acid comprising at least one member selected from the group consisting of salicylic acid. The method according to claim 1,
Wherein the composition has a formulation selected from the group consisting of a lotion, an emulsion, a cream, an essence, a cosmetic ointment, a spray, a gel, a pack, a sunscreen, a makeup base, a foundation, a powder and a detergent. An external skin preparation for the treatment and improvement of acne comprising tranexamic acid, phytosphingosine-1-phosphate and microalgae extract as active ingredients. 6. The method of claim 5,
Wherein the external preparation has a formulation selected from the group consisting of ointments, patches, gels, creams and sprays.

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