KR20170045085A - Composition for improving skin and its use - Google Patents

Abstract

The present invention relates to a composition for improving skin. A complex containing a pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid according to the present invention promotes synthesis of elastin of fibroblasts of skin, promotes superoxide dismutase-like activity, normalizes an inflammatory cytokine level, inhibits proliferation of skin resident, and promotes synthesis of hyaluronic acid. Therefore, the composition of the present invention can be used for manufacture of health functional food, medicines or cosmetic products, for skin elasticity improvement, pore contraction, antibiosis, acne inhibition, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble decrease, skin moisturization and skin texture improvement.

Description

Composition for improving skin and use thereof

The present invention relates to a composition for skin improvement which shows skin elasticity improvement, pore contraction, antibacterial, acne control, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturization and skin texture improvement.

Aging is a phenomenon of life, and all life begins from the birth of aging. Due to the improvement of sanitation and health environment, human life span has been significantly extended, and the proportion of the elderly population is steadily increasing [Non-Patent Document 1]. Aging occurs entirely in the body, which deteriorates physiological functions of organs such as general physical dysfunction and lifestyle diseases such as cardiovascular diseases and diabetes [Non-Patent Document 2].

Skin is an important organ that performs various roles such as body temperature control, skin sensory function, and immune function while preventing moisture, electrolytes and proteins from disappearing from the outermost part of the body.

As with other organs, skin ages with age. Skin aging consists of intrinsic skin aging and photoaging, and endogenous skin aging is characterized by functional changes rather than gross morphological changes. Photoaging due to chronic UV exposure overlaps with endogenous aging and is not systemic or unavoidable, but it has significant structural and physiological changes. In the aged epidermis, not only the inherent functions such as wrinkles of the skin, loss of the barrier, immunity abnormality, etc. are lost, but also affect the appearance of the body aesthetically. There is no way to prevent aging of the skin, but various attempts have been made to prevent and slow the aging of the skin.

On the other hand, pine bark extract was extracted from pine belonging to Pinus (pine), and various papers on pycnogenol which is a French sea otopus extract among various pine bark extracts have been published. The effects of pycnogenol include circulating blood vessel-related improvement effects [Non-Patent Document 3], antioxidant effects [Non-Patent Documents 4, 5 and 6], inhibition of skin blackening and inflammation inhibition [Non-Patent Documents 7 and 8] Effect [Non-Patent Document 9] and the like.

In addition, ascorbic acid and vitamin E are vitamins that are highly antioxidant and have no harmful effects on the human body. Ascorbic acid and vitamin E have been reported to increase the minimum erythemal dose (MED) when administered in combination with an overdose, which is presumed to have an inflammation-suppressing effect upon overdose (Non-Patent Documents 10 and 11).

In addition, gamma linolenic acid is a component that is contained in large amounts in sunflower seed oil, borage oil, pumpkin seed oil, burdock seed oil, and the like. It has been reported that gamma linolenic acid can be converted into 13-hydroxyoctadecadienoic acid (13-HODE) from the epidermis of the skin, and then incorporated into phospholipids to inhibit skin hyperplasia and also to have skin moisturizing function [Non-Patent Document 12].

The prior art patents disclose whitening, wrinkle-improving and inhibiting functional effects of pine bark extract, ascorbic acid, vitamin E, and gamma linolenic acid-mixed complex [Patent Literatures 1 and 2]. However, a complex of pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid improves skin elasticity, shrinks pores, improves skin barrier, normalizes skin immunity, anti-inflammation, improves trouble, There has been no reported effect on the regulation.

Under these circumstances, the present inventors have made efforts to develop a natural material having an effect of inhibiting skin aging. As a result, it has been found that a complex of pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid improves skin elasticity of skin, The present invention has been completed upon confirming that the present invention is effective in improving skin immunity, improving skin irritation, improving anti-inflammation, improving trouble, antibacterial, skin moisturizing, skin texture and sebum control.

Korean Patent Publication No. 0580070 Korean Patent Publication No. 0563673

Kang Tae Jin, BioWave. 2011; 13 (3): 1-15 Choi, Hyun - Chul, Korean Journal of Dermatology, 1997; 35: 292-302 Fitzpatrick, J Cardiovasc Pharmacol. 1998; 32 (4): 509-15. Chida, Ophthalmic Res. 1999; 31 (6): 407-15. Cossins, Biochem Mol Biol Int. 1998; 45 (3): 583-97. Devaraj, Lipids. 2002; 37 (10): 931-4. Saliou, Free Radic Biol Med. 2001; 30 (2): 154-60. Ni, Phytother Res. 2002 Sep; 16 (6): 567-71 Grimm, Free Radic Biol Med. 2004; 36 (6): 811-22 Flush, Free Radic Biol Med. 1998; 25 (9): 1006-12. Keller, J Am Acad Dermatol. 1998; 39 (4): 611-25. Cho, YH, Korean Skin Barrier Journal, 2003; 5 (1): 53-60.

Accordingly, the inventors of the present invention found that pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex promotes elastin synthesis of fibroblasts of skin to improve skin elasticity and pore shrinkage effect, and to achieve superoxide dismutase- It exhibits antioxidative effect and normalizes the level of inflammatory cytokine to normalize skin immunity, anti-inflammation, trouble-improving effect, inhibits skin supernatant proliferation, suppresses acne, has antibacterial effect, promotes synthesis of hyaluronic acid, Thereby completing the present invention.

Accordingly, an object of the present invention is to provide a method for improving skin elasticity, pore contraction, antibacterial effect, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, Anti-inflammation, trouble-improving, antibacterial, skin moisturizing, and skin texture improvement.

As a means for solving the above problems, the present invention relates to a composition for improving skin elasticity, pore contraction, antibacterial activity, antioxidant activity, anti-inflammatory activity, anti- The present invention provides a composition for suppressing acne, controlling sebum, improving skin barrier, normalizing skin immunity, anti-inflammation, improving trouble, antibacterial, skin moisturizing and skin texture improvement.

The pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex according to the present invention promotes elastin synthesis of fibroblasts of the skin to improve skin elasticity, exhibit antioxidative effect through superoxide dismutase-like activity, Normalizing the level of inflammatory cytokine, exhibiting skin immunity normalization, anti-inflammation, trouble-improving effect, suppression of skin supernatant proliferation, suppression of acne, antibacterial effect, promotion of hyaluronic acid synthesis, Health functional food, medicine or cosmetic preparation.

BRIEF DESCRIPTION OF THE DRAWINGS FIG. 1 is a graph showing the production rate of elastin according to the control group and the example of the present invention. FIG.

Hereinafter, the configuration of the present invention will be described in detail.

In order to exert an excellent effect when applied to actual skin, it is necessary to improve the skin elasticity, pore contraction, antibacterial effect, acne control, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, Exhibits activity of improving skin elasticity of active, antibacterial, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin tone improving activity, It is excellent in the ability of the skin to exhibit the above-mentioned effect or penetrate through the skin and to improve skin elasticity, pore contraction, antibacterial effect, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, The composition is low in volatility so as to be able to stay in the skin for a sufficient time to exhibit the improvement effect, Is stable and easily produced in health functional foods, medicines or cosmetics, and is safe in the body and skin. However, the components satisfying all of the above-mentioned characteristics among the known components are not common. For example, some skin elasticity improvement, pore contraction, antibacterial, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin tone improving activity are excellent, It is difficult to apply to real skin because of its ability to absorb. Other active ingredients have low hydrophilicity and are difficult to formulate into health functional foods, medicines and cosmetics. In addition, when the skin is exposed to heat, light, or oxygen, it is possible to improve the skin elasticity, pore contraction, antibacterial effect, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, The active ingredient may be degraded or transformed into another compound and the effect may already be lost before it is applied to the body or skin.

As can be seen in the following examples, pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complexes promote elastin synthesis of fibroblasts, which are superior at low concentrations, superoxide dismutase-like activity, inflammatory cytokine levels It is possible to improve skin elasticity, pore contraction, antibacterial effect, acne control, sebum control, skin barrier improvement, normalization of skin immunity, anti-inflammation, trouble improvement, skin moisturization, Can be used as an active ingredient of a health functional food, a medicine, or a cosmetic composition for improvement.

Accordingly, the present invention relates to a composition for improving skin elasticity, pore contraction, antibacterial effect, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, anti- A composition for improving trouble, skin moisturizing, and skin texture improvement.

In the present invention, the pine bark extract is a main ingredient of a raw material for food, and its main ingredient is tannin and flavonoid including proanthocyanidin, which has been used since ancient times and is harmless to human body.

The pine bark extract may be extracted by a method known in the art, and the method is not particularly limited. Alternatively, commercially available extracts can be used.

The pine bark extract can be obtained by, for example, cooling or warming with a solvent such as water and / or ethanol, extracting an active ingredient, filtering, and concentrating the filtrate under reduced pressure.

Preferably, the pine bark extract may be an extract obtained by extracting pine bark with water and / or an organic solvent. The organic solvent may be a polar organic solvent, a nonpolar organic solvent or a mixture thereof. The polar organic solvent may be a lower alcohol having 1 to 5 carbon atoms, ethyl acetate or acetone, and the nonpolar organic solvent may be ether, chloroform, benzene, hexane or dichloromethane. For example, the lower alcohol having 1 to 5 carbon atoms may be methanol, ethanol, propanol, butanol or isopropanol.

In one embodiment, the pine bark extract may be an extract obtained by extraction with water and / or ethanol.

In one embodiment, the pine bark extract may include a fraction obtained by fractionating the primary extract extracted using the above-described extraction solvent with an extraction solvent having a different polarity. For example, the pine bark extract may be a fraction obtained by extracting with an alcohol having 1 to 5 carbon atoms and then fractionating again with a solvent having a different polarity such as ether, benzene, or hexane. Two or more kinds of solvents may be used for the fractionation, and the solvent extracts may be sequentially used or mixed according to the polarity of the solvent.

In the present invention, the extracted extract or the fraction obtained by performing the fractionation process may be filtered, concentrated or dried to remove the solvent, and the filtration, concentration, and drying may all be performed. Specifically, the filtration can be performed using a filter paper or a vacuum filter, and the concentration can be reduced by using a reduced pressure concentrator or the like, and the freeze-drying method can be carried out for drying.

The fractions obtained by performing the above-described extract or the fractionation process can be further purified by silica gel column chromatography, thin layer chromatography or high performance liquid chromatography Further purification can be achieved by purification using various chromatographic techniques.

In the present invention, the pine bark extract may be a French sea bream peel extract.

In the present invention, the composition includes pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid.

Since the pine bark extract, ascorbic acid, vitamin E, and gamma linolenic acid have been used for a long time as a natural substance and proved to be stable, they can be manufactured in the form of health functional foods while being common sense.

The composition for improving the skin elasticity, pore contraction, antibacterial effect, acne control, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin texture improvement of the present invention can be used for manufacturing food formulations.

Preferably, the composition is mixed at a ratio of 1 to 45% by weight of pine bark extract, 18 to 75% by weight of ascorbic acid, 4 to 35% by weight of vitamin E and 2 to 45% by weight of gamma linolenic acid. It is difficult to expect a skin improvement effect due to the mutual synergistic effect when the recommended amount of each ingredient is less than the recommended minimum use amount. When the amount of the ingredient exceeds the recommended maximum use amount, the skin improvement effect is directly increased And is also not commercially suitable because the cost of the raw material is too high.

In addition, in one embodiment of the present invention, the composition comprises the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex in an amount of 0.0001 wt% to 10 wt% (preferably 0.0001 wt% to 1 wt% Weight%). When the composition of the present invention contains less than 0.0001% by weight of the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex, sufficient skin elasticity improvement, pore shrinkage, antibacterial effect, acne suppression, sebum control, It can not be expected that the skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin texture improving effect can be expected. If it is contained in an amount exceeding 10% by weight, it can prevent unwanted reactions such as allergies or skin safety problems. .

The food formulation is defined as a food prepared by adding the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex to a food material such as beverage, tea, spice, gum and confectionery, or by encapsulation, powdering, do.

Since the food preparation can be taken on a daily basis, the food formulation can be expected to have high skin elasticity, pore contraction, antibacterial effect, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin texture improvement It is very useful.

When the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex are used as food additives, the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex may be added intact or used together with other food or food ingredients And can be suitably used according to a conventional method. The amount of the active ingredient to be mixed can be suitably determined according to its intended use (prevention, health or therapeutic treatment). In general, the composition of the present invention is added in an amount of not more than 15% by weight, preferably not more than 10% by weight based on the raw material, in the production of food or beverage. However, in the case of long-term consumption intended for health and hygiene purposes or for health control purposes, the amount may be less than the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount exceeding the above range .

There is no particular limitation on the kind of the food. Examples of the food to which the above substance can be added include dairy products including meat, sausage, bread, chocolate, candy, snack, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, Alcoholic beverages, and vitamin complexes, all of which include health functional foods in a conventional sense.

In the present invention, the term "health functional food" refers to a food having high medical effect and processed to show a biological control function in addition to nutrition supply. The food may be prepared in any one form selected from the group including powders, granules, tablets, capsules, liquids, and pills in order to obtain a useful effect for skin improvement. Can be used.

When the food is a beverage, various flavors or natural carbohydrates may be added as an additional ingredient such as a normal drink. The above-mentioned natural carbohydrates are sugar alcohols such as monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and xylitol, sorbitol and erythritol. Examples of sweeteners include natural sweeteners such as tau martin and stevia extract, synthetic sweeteners such as saccharin and aspartame, and the like. The ratio of the natural carbohydrate is generally about 0.01 to 0.04 g, preferably about 0.02 to 0.03 g per 100 mL of the composition of the present invention.

The composition may contain additional ingredients which are commonly used in food compositions and which can improve odor, taste, visual appearance, and the like. For example, vitamins A, D, B1, B2, B6, B12, niacin, biotin, folate, panthotenic acid and the like. In addition, it may include minerals such as zinc (Zn), iron (Fe), calcium (Ca), chromium (Cr), magnesium (Mg), manganese (Mn) and copper (Cu) It may also include amino acids such as lysine, tryptophan, cysteine, valine, and the like. In addition, it is also possible to use antiseptics (such as potassium sorbate, sodium benzoate, salicylic acid, sodium dehydroacetate), disinfectants (such as bleaching powder and highly bleached white powder, sodium hypochlorite), antioxidants (butylhydroxyanilide (BHA), butylhydroxytoluene BHT), etc.), coloring agents (such as tar pigments), coloring agents (such as sodium nitrite and sodium acetic acid), bleaching agents (sodium sulfite), seasoning (such as MSG sodium glutamate), sweeteners (such as hypoglycemia, , Food additives such as flavorings (vanillin, lactones, etc.), swelling agents (alum, potassium hydrogen D-tartrate), emulsifiers, emulsifiers, thickeners, encapsulating agents, gum bases, foam inhibitors, ) Can be added. The additives are selected according to the type of food and used in an appropriate amount.

In addition to the above, the food formulations may contain various nutrients, vitamins, electrolytes, flavors, colorants, pectic acid and salts thereof, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, And the like. Other food formulations may contain flesh for the production of natural fruit juices, fruit juice drinks and vegetable drinks. These components may be used independently or in combination. The proportion of such an additive is not critical, but is generally selected in the range of 0.01 to 0.1% by weight per 100% by weight of the composition of the present invention.

The food composition of the present invention can be prepared by a method commonly used in the art and can be prepared by adding raw materials and ingredients which are conventionally added in the art. Also, unlike general medicine, there is an advantage that there is no side effect that can occur when a medicine is used for a long time by using food as a raw material, and it is excellent in portability.

The composition for improving skin elasticity, pore contraction, antibacterial effect, acne control, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin texture improvement of the present invention can be used for the production of pharmaceutical formulations .

The pharmaceutical formulations may be in the form of solutions, suspensions or emulsions in oils or aqueous media, or in the form of excipients, powders, granules, tablets or capsules.

In addition, the composition may further contain one or more active ingredients showing the same or similar functions. For example, it may include known skin elasticity improvement, pore contraction, antibacterial, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble-improving, skin moisturizing and skin texture improving ingredients. The composition of the present invention can improve the elasticity of the skin, improve the skin elasticity of the pores, improve the skin elasticity of the composition of the present invention, and improve the skin elasticity, pore contraction, antibacterial effect, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, Shrinkage, antibacterial, acne suppression, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin texture improvement effect can be further enhanced. When the above ingredients are added, skin safety, easiness of formulation, and stability of effective ingredients can be considered according to the combined use.

In addition, the composition of the present invention may further comprise a pharmaceutically acceptable carrier.

As used herein, the term "pharmaceutically acceptable carrier" may mean a carrier or diluent that does not disturb the biological activity and properties of the compound being injected, without irritating the organism. The type of the carrier that can be used in the present invention is not particularly limited, and any carrier conventionally used in the art and pharmaceutically acceptable may be used. Non-limiting examples of such carriers may contain various components such as buffer, injectable sterile water, normal saline or phosphate buffered saline, sucrose, histidine, salts and polysorbates. These may be used alone or in combination of two or more. The carrier may comprise a non-naturally occuring carrier.

The composition of the present invention can be administered orally or parenterally, and can be administered in the form of a general pharmaceutical preparation, for example, various forms of oral and parenteral administration at the time of clinical administration. In the case of formulation, a filler, , A binder, a wetting agent, a disintegrant, a surfactant, and the like.

Solid formulations for oral administration include tablets, pills, powders, granules, capsules and the like. These solid preparations can be prepared by mixing the pharmaceutical composition of the present invention with at least one excipient such as starch, calcium carbonate, Sucrose, lactose, gelatin and the like can be prepared.

In addition to simple excipients, lubricants such as magnesium stearate talc are also used. Examples of liquid formulations for oral administration include suspensions, solutions, emulsions, syrups and the like. Various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included in addition to water and liquid paraffin, which are simple diluents commonly used.

Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like can be used as the non-aqueous solvent and suspension agent. Examples of the suppository base include witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin and the like.

In the present invention, 'skin elasticity improving effect' refers to an increase in elasticity to the skin, which suppresses or inhibits the loss of skin elasticity, or alleviates the elasticity that has already been reduced.

In the present invention, the term 'pore shrinkage effect' refers to a reduction in the size of pores of enlarged skin. The pore size may be enlarged due to various factors such as aging, excess sebum secretion, keratinization, and the like.

In the present invention, the 'skin barrier improvement effect' refers to smooth skin barrier function, and the skin barrier can prevent intrusion of foreign substances from outside by the lamellar structure of intercellular lipid surrounding keratinocytes and keratinocytes And prevent the body from losing moisture and electrolytes in the body at the same time.

In the present invention, the term 'skin immunity normalization effect' refers to normalizing immunity when skin immunity is excessive, and normalizing skin immunity when the skin immunity is weakened.

In the present invention, the 'anti-inflammatory effect' refers to inhibition of inflammation, and the inflammation is one of defensive reactions of biological tissue against certain stimuli, and is a complex reaction involving tissue degeneration, circulatory disorder and exudation, Lesion. More specifically, inflammation is part of congenital immunity and, like in other animals, human congenital immunity recognizes a pattern of cell surfaces that are specifically present in a pathogen. Phagocytes recognize cells with such surfaces as non-magnetic and attack pathogens. If pathogens break through the physical barriers of the body, an inflammatory reaction occurs. Inflammation is a nonspecific defense that creates hostile environments for microorganisms entering the wound. In the inflammatory response, white blood cells that are responsible for the early stage of immune response, when wounded or infected, enter the body to express cytokines. Therefore, the expression level of intracellular cytokine is an index of inflammatory response activation. Examples of skin diseases associated with inflammation include atopic dermatitis, psoriasis, radiation, chemical substances, inflammatory diseases caused by burns, acid burns, vesicular dermatosis, visceral type diseases, itching due to allergies, seborrheic eczema, rose acne, Inflammatory hair loss such as pemphigus vulgaris, polymorphous exudative erythema, erythema nodosum, erythematosus, pharyngitis, alopecia areata, skin T-cell lymphoma, and the like.

In the present invention, the 'trouble improving effect' means a secondary trouble such as allergy, dermatitis, abnormal keratinization, itching and inflammation caused thereby, and means an effect of suppressing and improving the inflammation.

In the present invention, the term " antibacterial effect " refers to the ability to resist bacteria and means all mechanisms that are performed to defend against the action of microorganisms such as bacteria or fungi.

In the present invention, the term 'skin moisturizing effect' refers to inhibiting or reducing the decrease of moisture in the skin, or increasing the moisture content of the skin to smooth and smooth the surface of the skin.

In the present invention, the term " skin texture improving effect " refers to smoothing the skin surface, imparting gloss, and brightening the skin tone by inhibiting or inhibiting roughness of the skin surface due to aging, stress, .

In the present invention, the term 'acne suppression' and 'sebum control effect' refers to suppression of acne by regulating the secretion of sebum as the sebaceous glands are clogged as well as the skin is bundled if sebum is secreted too much.

In the present invention, the term 'effective amount' means an amount effective to improve skin elasticity, to improve skin barrier, to normalize skin immunity, to suppress inflammation, to inhibit antibacterial effect, moisturizing effect, Means the amount of extract that can improve or control sebum. When the composition of the present invention contains an effective amount of the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex, it is desirable to improve skin elasticity, pore contraction, antibacterial effect, acne suppression, sebum control, skin barrier improvement, Anti-inflammation, trouble-improving, skin moisturizing, and skin texture improving effect. The effective amount of the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex contained in the composition of the present invention will vary depending on the form in which the composition is commercialized, the method in which the compound is applied to the skin, and the time on the skin. For example, when the composition is commercialized as a pharmaceutical formulation, it may contain the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex at a higher concentration than when commercialized into cosmetics that are routinely applied to the skin . Therefore, the daily dose is 0.1-100 mg / kg, preferably 30-80 mg / kg, more preferably 50-50 mg / kg, based on the amount of the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex. To 60 mg / kg, and can be administered 1 to 6 times a day.

The composition of the present invention may be used alone or in combination with methods using surgery, radiation therapy, hormone therapy, chemotherapy, and biological response modifiers.

The pharmaceutical formulations of the present invention may include external preparation for skin.

When the pine bark extract, ascorbic acid, vitamin E, and gamma linolenic acid complex are used as an external preparation for skin, it is possible to further include a fatty substance, an organic solvent, a solubilizing agent, a thickening agent and a gelling agent, a softening agent, an antioxidant, a suspending agent, A surfactant, a water, an ionic or nonionic emulsifier, a filler, a sequestering and chelating agent, a preservative, a vitamin, a barrier, a wetting agent, an essential oil, a dye, a pigment, An oily active agent, a lipid vesicle or any other ingredient conventionally used in external preparations for skin, as well as adjuvants conventionally used in the field of skin science. The components can also be introduced in amounts commonly used in the field of dermatology.

When the pine bark extract, ascorbic acid, vitamin E, and gamma linolenic acid complex are provided as an external preparation for skin, they may have formulations such as, but not limited to, ointments, patches, gels, creams or sprays.

Further, the composition for improving skin elasticity, pore contraction, antibacterial effect, acne control, sebum control, skin barrier improvement, skin immunity normalization, anti-inflammation, trouble improvement, skin moisturization and skin texture improvement of the present invention can be used for manufacturing cosmetic formulations .

The cosmetic formulation may be in the form of a conventional emulsion formulation and a solubilized formulation. For example, creams, essences, cosmetic creams, sprays, gels, packs, sunscreens, make-up bases, liquids such as lotions such as lotion, facial lotion, body lotion, A powder, a cleansing lotion, a makeup removing agent such as a cleansing oil, a cleansing foam, a soap, a body wash, and the like.

In addition, the cosmetic product may further comprise, in addition to the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex, a fat substance, an organic solvent, a solubilizing agent, a thickening agent and a gelling agent, a softening agent, an antioxidant, a suspending agent, a stabilizing agent, a surfactant, a water, an ionic or nonionic emulsifier, a filler, a sequestering and chelating agent, a preservative, a vitamin, a barrier, a wetting agent, an essential oil, a dye, a pigment, a hydrophilic or lipophilic active agent, Lipid vesicles, or any other ingredient conventionally used in cosmetics, as well as adjuvants commonly used in the cosmetics field.

In the case of the wash-off type cosmetics such as make-up remover, detergent and the like in which the active ingredient remains on the skin in a short period of time, the cosmetic formulation contains a relatively high concentration of the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid Complex. ≪ / RTI > On the other hand, in the case of leave-on type cosmetics such as lotion, cream, essence and the like in which the active ingredient remains on the skin for a long period of time, the pine bark extract, Columbic acid, vitamin E, and gamma linolenic acid complex. In one embodiment of the present invention, but not limited thereto, the composition comprises 1 to 45% by weight of pine bark extract, 18 to 75% by weight of ascorbic acid, 4 to 35% by weight of vitamin E and 2 to 45% by weight of gamma linolenic acid, As shown in FIG. When the components of the composition of the present invention are used in an amount less than the recommended minimum use amount, it is difficult to expect a skin improvement effect due to mutual synergistic effect. In the case of using an amount exceeding the recommended maximum use amount of each component, The improvement effect of the skin is not increased, and the price of the raw material is too expensive, which is not commercially suitable.

In addition, in one embodiment of the present invention, the composition comprises the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex in an amount of 0.0001 wt% to 10 wt% (preferably 0.0001 wt% to 1 wt% Weight%). When the composition of the present invention contains less than 0.0001% by weight of the pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid complex, sufficient skin elasticity improvement, pore shrinkage, antibacterial effect, acne suppression, sebum control, It can not be expected that the skin immunity normalization, anti-inflammation, trouble improvement, skin moisturizing and skin texture improving effect can be expected. If it is contained in an amount exceeding 10% by weight, it can prevent unwanted reactions such as allergies or skin safety problems. .

Hereinafter, the present invention will be described in detail with reference to examples. However, the following examples are illustrative of the present invention, and the present invention is not limited to the following examples.

Example  1 to 13: Preparation of composite composition

Pine bark extract (pycnogenol), ascorbic acid, vitamin E and gamma linolenic acid were mixed to a total amount of 100 mg according to the content ratio (unit:%) shown in the following Table 1, Respectively. Pycnogenol was used as a pine extract, and as the content of gamma linolenic acid, the content of sunflower seed oil (containing 59% gamma linolenic acid) was used.

Pine extract
(Pycnogenol) Ascorbic acid Vitamin E Gamma linolenic acid Total Comparative Example 1 100 - - - 100 Comparative Example 2 - 100 - - 100 Comparative Example 3 50 50 - - 100 Comparative Example 4 50 - 50 - 100 Comparative Example 5 - 50 - 50 100 Comparative Example 6 33.3 33.3 33.4 - 100 Comparative Example 7 33.3 - 33.3 33.4 100 Comparative Example 8 - 33.3 33.3 33.4 100 Example 1 25 25 25 25 100 Example 2 10 40 10 40 100 Example 3 40 10 40 10 100 Example 4 5 45 5 45 100 Example 5 45 5 45 5 100

Experimental Example  1: Fibroblast elastin of the composite composition ( Elastin ) Synthesis Promotion Effect

Elastin is a protein that exists in connective tissue together with collagen. It is elastic like rubber, and it is involved in flexibility and stretchability of tissue. The skin consists of epidermis and dermis, and the dermis is divided into two layers. The upper layer is the papillary layer and the lower layer is the reticular layer. There is a lot of collagen mainly in the reticular layer, but there is a lot of elastin in the papilla. Because of its abundance in the skin, Elastin has a lot of impact on human appearance, especially compared to other proteins. (Aestheric & Spa, 2014 (10)), which plays a crucial role in maintaining youthfulness through skin-elasticity and deep involvement in the inhibition of pore enlargement.

In order to confirm the promoting effect of the elastin synthesis of the composite composition, 2 × 10 ⁵ human-derived normal fibroblasts were cultured in a 6-well plate for 24 hours, and the mixture of the control group and the example An experimental group treated with 50 μg / mL of sample was prepared. After 48 hours of incubation, the amount of newly synthesized elastin in fibroblasts was measured using a commercially available Human elastin ELISA kit (MyBioSource, Inc., USA), and the amount of elastin was corrected to the amount of protein. Experimental results are shown in Fig. 1, in which the control group in which nothing is treated is regarded as 100%.

As shown in FIG. 1, the production rate of elastin significantly increased when four kinds of pine extract (pycnogenol), ascorbic acid, vitamin E and gamma linolenic acid were used alone or in combination of two or three kinds thereof . This can be confirmed by the synergistic effect of each component.

Experimental Example  2: Superoxide Dismutase  Identify similar activity

Free-Radicals refers to oxygen molecules that have lost one state due to their interaction with other molecules. These molecules are very unstable and damage cell tissue. Active oxygen acts as a causative agent of aging, especially skin aging. Active oxygen is also produced during normal metabolism, but active oxygen, which affects skin aging, is produced mainly by the action of ultraviolet rays on the skin. They break down skin antioxidant defenses consisting of antioxidant enzymes and non-enzymatic antioxidants, inhibit lipid peroxidation, activation of proteolytic enzymes that promote protein oxidation, chain cleavage of collagen and elastin, and skin immune function As a result, elasticity reduction, pore enlargement, wrinkles and spots, freckles and skin aging is accelerated. Therefore, in order to protect the skin cells and delay or prevent aging of the skin, it is necessary to inhibit the excessive production of active oxygen and to remove the active oxygen (Hong Ji Kee, 2009; 7 (2): 51-62) .

This superoxide dismutase (SOD) -like activity of the composite composition is determined by the amount of pyrogallol that catalyzes the conversion of hydrogen peroxide (H ₂ O ₂ ) according to the method of Marklund & Marklund (1974) Were measured and expressed as SOD-like activity. That is, 260 μl of Tris-HCl buffer (50 mM tris + 10 mM EDTA, pH 8.5) and 20 μl of 7.2 mM pyrogallol were added to a sample solution of 50 μg / mL and reacted at 25 ° C. for 10 minutes. Then, 10 μl of 5N HCl was added And the amount of oxidized pyrogallol in the reaction solution was measured at an absorbance of 420 nm. The experimental results show the difference in absorbance between the sample-treated group and the control group as a percentage, and the results are shown in Table 2 below.

The experimental results are shown in Table 2 below. In Table 2 below, the numerical value of the increase in p63 is a multiple of the control group (CNT-57 medium supplemented with BPE).

sample SOD-like activity (%) Control group 100 Comparative Example 1 162 Comparative Example 2 192 Comparative Example 3 162 Comparative Example 4 158 Comparative Example 5 159 Comparative Example 6 172 Comparative Example 7 159 Comparative Example 8 147 Example 1 189 Example 2 171 Example 3 162 Example 4 170 Example 5 181

As shown in Table 2, when four kinds of pine tree extract (pycnogenol), ascorbic acid, vitamin E and gamma-phenolic acid were used in combination of two or three kinds, ascorbic acid (a powerful antioxidant) Similar to Example 2, SOD-like activity was observed. This can be confirmed by the synergistic effect of each component.

Experimental Example  3: Normalization of Inflammatory Cytokine Levels of Composite Compositions

The immune system refers to biological structures and processes that have the function of protecting living organisms from diseases by detecting pathogens, tumor cells, and the like in living organisms and then killing them. If the immune system does not function properly in the human body, various immune diseases such as allergy, autoimmune disease, immune deficiency and the like may be caused.

Recently, as pollutants such as dust and fine dust are gradually increasing in the atmosphere, the immune unbalance problem of the skin exposed to the external environment becomes serious. The number of patients who are allergic to double immunosuppression is increasing. There are various symptoms of skin allergy, among which atopic dermatitis and psoriasis are the most common skin allergic diseases

Atopic dermatitis is immunologically mediated mainly by type 2 Auxiliary T cells and is commonly accompanied by elevated levels of allergen specific IgE and total IgE. On the other hand, psoriasis is mainly mediated by type I Auxiliary T cells, accompanied by high levels of interferon-γ, and high levels of interleukin-17A, interleukin-17F, and interleukin-22 (O, Young, Joon, Korean Journal of Dermatology, 2014; 52 (3): 207-208).

To evaluate this level of inflammatory cytokine inhibition of the composite composition, mouse macrophage RAW 264.7 cells were cultured in a 96-well plate at a concentration of 1 x 10 ⁵ cells / ml for 24 hours, and LPS (1 μg / ml). The amount of IgE and INF-γ produced after culturing for 24 hours was measured by using a commercially available IgE Mouse ELISA Kit (abcam, Inc. UK), Interferon gamma (IFNG) Mouse ELISA Kit (abcam, Inc., UK). Experimental results were shown in Table 3 below, except that LPS (1 μg / ml) was treated only and the control group without treatment was 100%.

sample LPS (1 [mu] g / ml) IgE (%) IFN-y (%) Control group X 48 40 Comparative Example 1 ○ 100 100 Comparative Example 2 ○ 88 76 Comparative Example 3 ○ 85 81 Comparative Example 4 ○ 88 88 Comparative Example 5 ○ 88 73 Comparative Example 6 ○ 67 61 Comparative Example 7 ○ 60 52 Comparative Example 8 ○ 58 48 Example 1 ○ 44 48 Example 2 ○ 40 42 Example 3 ○ 39 45 Example 4 ○ 44 43 Example 5 ○ 35 41

As shown in Table 3, when four kinds of pine extract (pycnogenol), ascorbic acid, vitamin E and gamma linolenic acid were used singly or in combination of two or three kinds, the inflammatory cytokine level was normal . This can be confirmed by the synergistic effect of each component.

Experimental Example  4: Skin of the composite composition Supernatant  Confirming the proliferation inhibitory effect

There are many different microorganisms in the skin, and beneficial bacteria and harmful bacteria are balanced. However, when the balance is broken, various skin diseases are caused by the harmful skin scab. The harmful skin supernatant is typical of acne bacteria, stomach bacteria, staphylococcus. Acne bacterium is generally caused by hormones and external influences, sebum can not be discharged out of the hair follicle, and when the skin pores are clogged, they multiply and cause acne. Staphylococcus aureus is a skin-damaging bacterium found all over the world and causes various diseases in the epidermis of humans and animals (Park, Soo-nam, Korea Microbiology Journal, 2010; 38 (1): 112-115).

The inhibition effect on skin flora was measured by liquid medium dilution method using Minimum Inhibitory Concentration (MIC) for acne and Staphylococcus aureus. Acne bacteria were cultured at 35 ℃ for 48 hours under anaerobic conditions. Staphylococci were cultured at 37 ℃ for 18 hours. Each of the bacteria was adjusted to 2 × 10 ⁶ CFU / well and incubated with the sample for 18 hours. The bacterial growth was observed with the naked eye and a microscope, and the absorbance was measured at an absorption wavelength of 540 nm. Was determined as the minimum inhibitory concentration. The minimum inhibitory concentrations of acne and staphylococci are shown in Table 4 below.

sample MIC (μg / ml) Acne bacteria
( Propionibacterium acnes ) Staphylococcus
( Staphylococcus aureus ) Comparative Example 1 0.121 0.118 Comparative Example 2 0.110 0.113 Comparative Example 3 0.122 0.111 Comparative Example 4 0.092 0.099 Comparative Example 5 0.101 0.089 Comparative Example 6 0.085 0.097 Comparative Example 7 0.087 0.091 Comparative Example 8 0.081 0.079 Example 1 0.057 0.059 Example 2 0.048 0.047 Example 3 0.049 0.042 Example 4 0.061 0.041 Example 5 0.055 0.051

As shown in Table 4, when four kinds of pine extract (pycnogenol), ascorbic acid, vitamin E and gamma linolenic acid were used alone or in combination of two or three kinds, the growth of harmful skin growth bacteria was inhibited . This can be confirmed by the synergistic effect of each component.

Experimental Example  5: Promotion of hyaluronic acid synthesis promotion of the composite composition

As the aging of the skin progresses, collagen and elastin, which are the fibrous tissues that serve as the basic backing for supporting the structure of the skin, are hardened and become insoluble. Cells, collagen, and elastin are called substrates, and their ability to retain moisture is very strong. Typical of these substrates are hyaluronic acid and mucopolysaccharides to be. Hyaluronic acid (Hyaluronic acid) is a polysaccharide widely distributed in intracellular tissues such as joint fluid and skin. It is a polymer of hyaluronan, which is a combination of N-acetylglucosamine and glucuronic acid, and has moisturizing and viscosity. As aging progresses, a decrease in these substances causes dry skin and weakens the elasticity of the skin (Kim, Yoon Bum, Journal of Physiology and Pathology, 2010; 24 (4): 533-542).

In order to confirm the effect of hyaluronic acid synthesis of the composite composition, human-derived normal fibroblasts were cultured in the same manner as in Experimental Example 1, and treated with samples. The newly generated hyaluronic acid from the culture was measured using a commercially available Human Hyaluronic Acid ELISA Kit (MyBioSource, Inc., USA), and the amount was corrected to the amount of protein. The experimental results are shown in Table 5 below.

sample Hyaluronic acid production (%) Control group 100 Comparative Example 1 110 Comparative Example 2 103 Comparative Example 3 119 Comparative Example 4 115 Comparative Example 5 125 Comparative Example 6 131 Comparative Example 7 141 Comparative Example 8 137 Example 1 184 Example 2 189 Example 3 182 Example 4 178 Example 5 181

As shown in Table 5, hyaluronic acid production rate was significantly increased when all four kinds of pine extract (pycnogenol), ascorbic acid, vitamin E and gamma linolenic acid were used alone or in combination of two or three kinds . This can be confirmed by the synergistic effect of each component.

Hereinafter, formulation examples of the composition containing the complex of the present invention will be described, but the present invention is not intended to be limited thereto but is specifically described.

[ Formulation example  1] Manufacturing of food

1. Manufacture of health food

Pine bark extract 20 mg

Ascorbic acid 300 mg

Vitamin E 100mg

Gamma linolenic acid 300 mg

Vitamin mixture quantity

70 [mu] g of vitamin A acetate

Vitamin E 1.0 mg

0.13 mg vitamin B1

0.15 mg of vitamin B2

0.5 mg vitamin B6

0.2 [mu] g vitamin B12

10 mg vitamin C

Biotin 10 μg

Nicotinic acid amide 1.7 mg

50 ㎍ of folic acid

Calcium pantothenate 0.5 mg

Mineral mixture quantity

1.75 mg of ferrous sulfate

0.82 mg of zinc oxide

Magnesium carbonate 25.3 mg

15 mg of potassium phosphate monobasic

Secondary calcium phosphate 55 mg

Potassium citrate 90 mg

100 mg of calcium carbonate

24.8 mg of magnesium chloride

Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with a composition suitable for health food as a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional method for producing healthy foods , Granules can be prepared and used in the manufacture of health food compositions according to conventional methods.

2. Manufacture of health drinks

Pine bark extract 20 mg

Ascorbic acid 300 mg

Vitamin E 100mg

Gamma linolenic acid 300 mg

Citric acid 1000 mg

100 g of oligosaccharide

Plum concentrate 2 g

Taurine 1 g

Purified water was added to a total of 900 ml

The above components were mixed according to a conventional health drink manufacturing method, and the mixture was heated at 85 DEG C for about 1 hour with stirring, and the solution thus prepared was filtered to obtain a sterilized 2-liter container, which was sealed and sterilized, ≪ / RTI >

Although the composition ratio is a mixture of the components suitable for the preferred beverage as a preferred embodiment, the blending ratio may be arbitrarily varied according to the regional and national preferences such as the demand level, the demanding country, and the intended use.

[ Formulation example  2] Manufacture of pharmaceutical preparations

1. Preparation of capsules

Pine bark extract 20 mg

Ascorbic acid 300 mg

Vitamin E 100mg

Gamma linolenic acid 300 mg

Lecithin 15 mg

Soybean oil 165 mg

Capsule base 300 mg

After mixing the above components, they were prepared according to the usual capsule manufacturing method.

[ Formulation Example 3] Production of cosmetics

1. Manufacture of nutritional cream

A nutritional cream containing, as an active ingredient, a complex containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid as the following composition was prepared according to a conventional method.

0.2% by weight of pine bark extract

1% by weight ascorbic acid

1% by weight of vitamin E

1% by weight of gamma linolenic acid

Beta-1,3-glucan 5.0 wt%

Wax 10.0 wt%

Polysorbate 60 1.5 wt%

≪ tb > < tb > < tb >

0.5% by weight of sorbitan sesquioleate

Liquid paraffin 10.0 wt%

Squalane 5.0 wt%

Caprylic / capric triglyceride 5.0 wt%

Glycerin 5.0 wt%

3.0% by weight of butylene glycol

3.0% by weight of propylene glycol

0.2% by weight triethanolamine

Preservative 0.05 wt%

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100%

[ Formulation example  4] Production of external preparation for skin

1. Manufacture of ointment

An ointment containing, as an active ingredient, a composite containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid, as the following composition, was prepared according to a conventional method.

0.2% by weight of pine bark extract

1% by weight ascorbic acid

1% by weight of vitamin E

1% by weight of gamma linolenic acid

Beta-1,3-glucan 10.0 wt%

Wax 10.0 wt%

Polysorbate 60 5.0 wt%

≪ tb > < tb > < tb >

0.5% by weight of sorbitan sesquioleate

Vaseline 5.0 wt%

Liquid paraffin 10.0 wt%

Squalane 5.0 wt%

SHARE BUTTER 3.0 wt%

Caprylic / capric triglyceride 5.0 wt%

Glycerin 10.0 wt%

Propylene glycol 10.2 wt%

0.2% by weight triethanolamine

Preservative 0.05 wt%

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100%

Claims (15)

A composition containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid as an active ingredient.
The method according to claim 1,
Wherein the pine bark extract is an extract obtained by extracting pine bark from any one solvent selected from the group consisting of water, ethanol and a mixture thereof.
The method according to claim 1,
Wherein the composition is for the production of a health functional food, a medicine or a cosmetic composition for improving skin elasticity.
The method according to claim 1,
Wherein the composition is mixed at a ratio of 1 to 45% by weight of pine bark extract, 18 to 75% by weight of ascorbic acid, 4 to 35% by weight of vitamin E and 2 to 45% by weight of gamma linolenic acid.
The method according to claim 1,
On the basis of 100% by weight of the total composition,
Wherein the content of the composite containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid is 0.001 to 100% by weight.
A composition containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid as active ingredients.
The method according to claim 6,
Wherein the composition is for the production of a health functional food, a medicine or a cosmetic for pore contraction, antibacterial, acne inhibition and sebum control, a composition for shrinking pores, antibacterial, acne inhibiting and sebum control.
A composition containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid as an active ingredient.
9. The method of claim 8,
Wherein the composition is for the manufacture of a health functional food, a medicament or a cosmetic for improving skin barrier.
A composition for improving normalization of skin immunity, anti-inflammation, and trouble, comprising a complex containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid as an active ingredient.
11. The method of claim 10,
A composition for skin immunization normalization, anti-inflammation, and trouble-improving, wherein the composition is for the preparation of a health functional food, a medicine or a cosmetic preparation for skin immunization normalization, anti-inflammation, trouble improvement.
A composition containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid as an active ingredient.
13. The method of claim 12,
Wherein the composition is for the production of a health functional food, a medicine or a cosmetic for skin moisturizing.
A composition containing pine bark extract, ascorbic acid, vitamin E and gamma linolenic acid as an active ingredient.
15. The method of claim 14,
Wherein the composition is for the manufacture of a health functional food, a medicament or a cosmetic composition for improving skin texture.

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