KR20130083806A - Composition for enhancing elasticity and whitening - Google Patents

Abstract

The present invention relates to a composition for enhancing skin elasticity and whitening. Cistanoside A according to the present invention promotes collagen synthesis of fibroblasts of the skin, inhibits collagenase activity, thereby improving skin elasticity, inhibiting melanin production, and exhibits a whitening effect. There is also no toxicity, so it can be used as a medicine or cosmetic composition or health food.

Description

Composition for enhancing elasticity and whitening}

The present invention relates to a composition for enhancing skin elasticity and whitening.

Collagen is a major stromal protein produced by skin fibroblasts and is present in extracellular epilepsy.Its important functions include mechanical firmness of skin, resistance of connective tissue and tissue binding, support of cell adhesion, cell division and differentiation. Induction of growth or wound healing) is known. This collagen is reduced by age and light aging by ultraviolet radiation, which is known to be closely related to the elasticity of the skin. In addition, in recent years, extensive research on aging of the skin has been developed an important function of collagen in the skin.

Conventionally, products that combine collagen with cosmetics have been released from the skin moisturizing effect of collagen, but these cosmetics are applied to the surface of the collagen, and it is not expected to moisturize by the percutaneous absorption of collagen as a polymer, thereby improving the essential skin function. I can not say.

On the other hand, it is known that the active ingredients that promote the collagen synthesis to exhibit the elasticity promoting effect. For example, retinoic acid, transforming growth factor (TGF) [non-patent document 1], protein derived from animal placenta [patent document 1], betulinic acid (betulinic acid) [patent document 2], chlorella extract [ Patent Documents 3 and 4 are known as collagen synthesis promoting substances. However, the active ingredients are limited in the amount of use due to safety problems such as irritation and redness when applying the skin, or there is a problem in that the effect of improving the skin function is not expected by substantially promoting collagen synthesis of the skin. Therefore, there is an urgent need for the development of components that are safe for the living body, stable in active ingredients, and above all, have an elasticity improving activity which is superior in effect to conventional collagen synthesis promoting substances.

Also, to have white and fair skin is everyone's constant desire. It is genetically determined by the concentration and distribution of melanin in human skin, but is also influenced by environmental or physiological conditions such as sun ultraviolet rays, fatigue and stress. Melanin is a type of amino acid tyrosine (tyrosine) acts as an enzyme called tyrosinase (tyrosinase) is converted into dopa (DOPA), dopaquinone (dopaquinone) is produced through a non-enzymatic oxidation reaction. The pathway by which melanin is produced is known, but the mechanisms that induce melanin synthesis, the previous stages of tyrosinase action, are still unknown.

Meanwhile, as a general known whitening component, substances that inhibit tyrosinase enzyme activity such as kojic acid and arbutin, hydroquinone, vitamin-C (L-Ascorbic acid) and derivatives thereof and various There is a plant extract. By inhibiting the synthesis of melanin pigments, they not only brighten the skin tone to realize skin whitening, but also improve skin hyperpigmentation such as blemishes and freckles due to ultraviolet rays, hormones or heredity. However, like the collagen synthesis promoting materials, when applied to the skin, there is a limitation in the amount of use due to safety problems such as irritation and redness, or there is a problem that a substantial effect can not be expected due to a slight effect. Therefore, there is an urgent need for the development of a whitening component that is safe for the living body, the active ingredient is stable, and above all, the existing melanin synthesis inhibitory ability.

 [Prior Art]

[Patent Literature]

Japanese Patent Laid-Open No. 8-231370

Japanese Patent Laid-Open No. 8-208424

Japanese Patent Laid-Open No. 9-40523

Japanese Patent Laid-Open No. 10-36283

[Non-Patent Document]

Cardinale G. et al, Adv. Enzymol., 41, p. 425, 1974

Accordingly, the inventors of the present invention promoted collagen synthesis of fibroblasts of the skin by inhibiting collagenase activity, thereby improving skin elasticity and inhibiting melanin production, thereby exhibiting a whitening effect. It was confirmed that the present invention was completed.

Accordingly, it is an object of the present invention to provide a composition for skin elasticity enhancement and whitening containing cystanoside A as an active ingredient.

As means for solving the above problems,

It provides a pharmaceutical composition for skin elasticity enhancement and whitening comprising a compound represented by the formula (1).

[Formula 1]

As another means for solving the above problems,

It provides a skin external preparation for skin elasticity enhancement and whitening comprising the compound of Formula 1.

As another means for solving the above problems, the present invention provides a cosmetic composition for skin elasticity enhancement and whitening comprising the compound of formula (1).

As another means for solving the above problems, the present invention provides a health food for skin elasticity enhancement and whitening comprising the compound of formula (1).

Cistanoside A according to the present invention promotes collagen synthesis of fibroblasts of the skin, inhibits the activity of collagenase, improves skin elasticity, inhibits melanin production, and exhibits a whitening effect. It is also non-cytotoxic and can be used in medicines, cosmetics or health foods without side effects.

EMBODIMENT OF THE INVENTION Hereinafter, the structure of this invention is demonstrated concretely.

In order to enhance skin elasticity and whitening effect, it shows high activity elasticity and whitening activity at low concentration, excellent ability to absorb and penetrate through skin, and improve skin elasticity and whitening effect. It is desirable to have low volatility so as to stay for a sufficient time for the phase, to keep the active ingredient stable on the composition or the skin, to be easily formulated into a medicament or cosmetic, and to be safe for the skin. However, among the known skin elasticity enhancing and whitening effect improving ingredients, components satisfying all of the above properties are rare. For example, some skin elasticity enhancing and whitening ingredients have excellent skin elasticity enhancing and whitening activity even at low concentrations in vitro, but are difficult to apply to actual skin due to their poor ability to penetrate and absorb the skin. Other skin elasticity enhancing and whitening ingredients are difficult to formulate into medicine or cosmetics due to their low hydrophilicity. In addition, some skin elasticity enhancing and whitening effect ingredients may be decomposed or transformed into other compounds when exposed to heat, light, or oxygen, and the skin elasticity enhancing and whitening effect may already disappear before application to the skin.

As can be seen in the following examples, cystanoside A (cistanoside A) shows an excellent effect at low concentrations, it can be used as an active ingredient such as medicines or cosmetics or health food for skin elasticity enhancement and whitening.

Accordingly, the present invention provides a pharmaceutical composition or skin external preparation or cosmetic composition or health food for enhancing skin elasticity and whitening comprising a compound represented by the following formula (1):

[Formula 1]

The compound of Formula 1 may be synthesized or used a commercially available compound.

As a specific example according to the present invention, the present invention provides a pharmaceutical composition for skin elasticity enhancement and whitening comprising the compound of Formula 1.

The pharmaceutical composition for enhancing skin elasticity and whitening of the present invention may include a pharmaceutically acceptable salt of the compound of Formula 1.

The pharmaceutically acceptable salt of the compound of Formula 1 may be an acid addition salt formed using an organic acid or an inorganic acid, and the organic acid may be, for example, formic acid, acetic acid, propionic acid, lactic acid, butyric acid, isobutyric acid or trifluoroacetic acid. , Malic acid, maleic acid, malonic acid, fumaric acid, succinic acid, succinic acid monoamide, glutamic acid, tartaric acid, oxalic acid, citric acid, glycolic acid, glucuronic acid, ascorbic acid, benzoic acid, phthalic acid, salicylic acid, anthranilic acid, dichloroacetic acid, aminooxyacetic acid And benzenesulfonic acid, p-toluenesulfonic acid and methanesulfonic acid salts and inorganic acids include, for example, hydrochloric acid, bromic acid, sulfuric acid, phosphoric acid, nitric acid, carbonic acid and boric acid salts. Preferably in the hydrochloride or acetate form, more preferably in the hydrochloride form.

The above-mentioned acid addition salts may be a) directly mixing the compound of formula 1 and an acid, b) dissolving and mixing one of them in a solvent or a hydrous solvent, or c) solvent or submerging the compound of formula 1 It is prepared by a general salt preparation method which is placed in an acid in a solvent and mixed with them.

In addition to the above, additionally saltable forms include, but are not limited to, the salts of gabapentin, pregabalin, nicotinate, adipate, hemimarate, cysteine, acetylcysteine, methionine, arginine, Aspartate and the like.

In addition, when using the compound of Formula 1 of the present invention as a medicine, it may further contain one or more active ingredients exhibiting the same or similar functions. For example, it may include known skin elasticity enhancing and whitening ingredients. When the additional skin wrinkle improvement component, elasticity enhancement component, whitening component is included, wrinkle improvement, elasticity enhancement, whitening effect of the composition of the present invention may be further enhanced. When the ingredient is added, skin safety, ease of formulation, and stability of the active ingredients may be considered. In one embodiment of the present invention, the composition is a wrinkle and elasticity improving component known in the art, retinoic acid, TGF, protein from animal placenta, betulinic acid and chlorella extract, as a whitening component known in the art, Selected from the group consisting of substances that inhibit tyrosinase enzyme activity such as kojic acid, arbutin, hydroquinone, vitamin-C (L-ascorbic acid) and derivatives thereof and various plant extracts It may further comprise one or two or more components. The added skin elasticity enhancing and whitening component may be included in 0.0001% to 10% by weight based on the total weight of the composition, the content range is collagen synthesis promoting activity, skin safety, ease of formulating the compound of Formula 1 It may be adjusted according to the requirements of the.

In addition, the pharmaceutical composition for skin elasticity enhancement and whitening of the present invention may further comprise a pharmaceutically acceptable carrier.

Pharmaceutically acceptable carriers may contain various components such as buffers, sterile water for injection, general saline or phosphate buffered saline, sucrose, histidine, salts, polysorbates and the like.

The pharmaceutical composition of the present invention may be administered orally or parenterally, and may be administered in the form of a general pharmaceutical preparation, for example, in various dosage forms, orally and parenterally, during clinical administration. , Diluents or excipients such as extenders, binders, wetting agents, disintegrants, surfactants and the like.

Solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, and such solid preparations include at least one excipient in the pharmaceutical composition of the present invention, for example, starch, calcium carbonate, It may be prepared by mixing sucrose or lactose, gelatin and the like.

In addition to simple excipients, lubricants such as magnesium stearate talc are also used. Liquid preparations for oral use include suspensions, solutions, emulsions, syrups, and the like, and various excipients such as wetting agents, sweeteners, fragrances, and preservatives, in addition to water and liquid paraffin, which are commonly used simple diluents.

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

In the present invention, 'elasticity enhancement' refers to regaining reduced skin elasticity by generating new collagen with the effect of shrinking the stretched skin tissue.

 In the present invention, the term "whitening effect" means not only brightening skin tone by inhibiting the synthesis of melanin pigment, but also improving skin hyperpigmentation such as blemishes and freckles due to ultraviolet rays, hormones or heredity.

The pharmaceutical composition of the present invention may provide desirable elasticity enhancing and whitening effects when an effective amount of the compound of Formula 1 is included. In the present invention, the term 'effective amount' refers to an amount of a compound that can generate new collagen and exhibit skin elasticity enhancement and whitening efficacy. The effective amount of the compound of formula 1 included in the composition of the present invention will vary depending on the form in which the composition is commercialized, how the compound is applied to the skin, the time it stays on the skin, and the like. For example, when the composition is productized as a medicine for dermatological treatments due to wrinkles, reduced elasticity, blemishes, freckles, etc., when the product is commercialized as cosmetics that are routinely applied to the skin, it is commercialized as cosmetics that are routinely applied to the skin. It may include the compound of Formula 1 in a higher concentration than if. Therefore, the daily dosage is 0.1 to 100 mg / kg, preferably 30 to 80 mg / kg, more preferably 50 to 60 mg / kg, 1 to 1 day, based on the amount of the compound of Formula 1 Can be administered six times

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

As a specific example according to the present invention, the present invention provides a skin external preparation for skin elasticity enhancement and whitening comprising the compound of Formula 1.

When the compound of Formula 1 is provided as an external preparation for skin, it is not limited thereto, and may have a formulation such as an ointment, a patch, a gel, a cream, or a spray.

Although not limited thereto, in one embodiment of the present invention, the composition may include 0.0001 wt% to 10 wt%, more specifically 0.001 wt% to 1 wt% of the compound of Formula 1, based on the total weight of the composition. have. When the composition of the present invention comprises less than 0.0001% by weight of the compound of Formula 1 can not expect sufficient skin elasticity enhancement and whitening effect, when containing more than 10% by weight unwanted reactions such as allergy or There may be a problem with the safety of the skin is to prevent this.

In addition, in the case of using the compound of Formula 1 as an external preparation for skin, a fatty substance, an organic solvent, a dissolving agent, a thickening agent and a gelling agent, an emollient, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, an interface To active agents, water, ionic or nonionic emulsifiers, fillers, metal ion sequestrants and chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or external preparations for the skin It may contain adjuvants commonly used in the field of dermatology, such as any other ingredients commonly used. The components can also be introduced in amounts commonly used in the field of dermatology.

As a specific example according to the present invention, the present invention provides a cosmetic composition for skin elasticity enhancement and whitening comprising the compound of Formula 1.

When the compound of Formula 1 is used as a cosmetic, the cosmetic prepared by containing the compound of Formula 1 as an active ingredient may be prepared in the form of a general emulsion formulation and solubilized formulation. For example, lotions such as flexible lotions or nourishing lotions, emulsions such as facial lotions, body lotions, creams such as nourishing creams, moisture creams, eye creams, essences, cosmetic ointments, sprays, gels, packs, sunscreens, makeup bases, liquids Formulations such as foundations, powders, cleansing creams, cleansing lotions, makeup removers such as cleansing oils, cleansing foams, soaps, body washes and the like.

In addition, the cosmetic may further include auxiliaries and carriers such as stabilizers, solubilizers, vitamins, pigments or flavorings commonly used in cosmetic compositions in addition to the compound of Formula 1. For example, fatty substances, organic solvents, solubilizers, thickening and gelling agents, emollients, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water, ionic or nonionic emulsifiers, fillers, Commonly used in the field of cosmetics such as metal ion sequestrants and chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic actives, lipid vesicles or any other ingredients commonly used in cosmetics. It may contain an adjuvant used.

The compound of Formula 1 may include a relatively high concentration of Formula 1 in the case of a wash-off type cosmetic such as a makeup remover, a detergent, etc., in which the active ingredient stays on the skin within a short time when it is commercialized. Could be. On the other hand, in the case of a leave-on type cosmetic such as a lotion, an emulsion, a cream, an essence, etc., in which the active ingredient stays on the skin for a long time, a lower concentration of cystanoside A (cistanoside) is used than in the wash-off type cosmetic. A) may be included. Although not limited thereto, in one embodiment of the present invention, the composition may include the compound of Formula 1 in an amount of 0.0001 wt% to 10 wt%, more specifically 0.001 wt% to 1 wt% based on the total composition weight). Can be. When the composition of the present invention comprises less than 0.0001% by weight of the compound of Formula 1 can not expect a sufficient whitening effect, when containing more than 10% by weight unwanted reactions such as allergy or skin safety problems There is a possibility to prevent this.

The present invention also relates to a health food for skin elasticity enhancement and whitening comprising the compound of Formula 1.

In the present specification, "health food" is a food prepared by adding the compound of Formula 1 to food materials, such as beverages, teas, spices, gums, confectionery, encapsulated, powdered, suspensions, etc. It means to bring a certain effect, but unlike the general medicine has the advantage that there are no side effects that can occur when taking a long-term use of the drug as a raw material.

Since the health food of the present invention thus obtained can be consumed on a daily basis, a high skin wrinkle improvement and elasticity enhancing effect can be expected, which is very useful.

When the compound of Formula 1 is used as a food additive, the compound of Formula 1 may be added as it is or used with other foods or food ingredients, and may be appropriately 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). Although not limited thereto, in one embodiment of the present invention, the health food may include the compound of Formula 1 in an amount of 0.0001 wt% to 10 wt%, more specifically 0.001 wt% to 1 wt% based on the total weight of the composition. Can be. 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 substance may be added include meat, sausages, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, beverages, teas, drinks, Alcoholic beverages and vitamin complexes, and the like and include all of the health foods in the conventional sense.

The health beverage of the present invention may contain various flavors or natural carbohydrates and the like as additional ingredients, as in general beverages. The above-mentioned natural carbohydrates include monosaccharides such as glucose and fructose; Disaccharides such as maltose and sucrose; Polysaccharides such as dextrin, cyclodextrin; Or sugar alcohols such as 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 health beverage of the present invention.

In addition to the above, the health food of the present invention includes various nutrients, vitamins, electrolytes, flavors, coloring agents, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloid thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols. And carbonation agents used in carbonated beverages.

In addition, the health food of the present invention may contain a flesh for preparing natural fruit juice, fruit juice drink and vegetable drink. These components may be used independently or in combination. The ratio of such additives is not critical but is generally selected in the range of 0.01 to 0.1 parts by weight per 100 parts by weight of the health food of the present invention.

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

< Reference Example  1> Formula 1  Information of the compound

bD-Glucopyranoside, 2- (4-hydroxy-3-methoxyphenyl) ethyl O-6-deoxy-aL-mannopyranosyl- (1®3) -O- [bD-glucopyranosyl- (1®6]-, 4-[( 2E) -3- (3,4-dihydroxyphenyl) -2-propenoate

CAS No .: 93236-42-1

Where to buy: alibaba

Plant of Origin: Cistanche deserticola

Example  1: collagen synthesis effect

The substances shown in Table 1 below were added to the culture solution of human-derived fibroblasts to test collagen synthesis promoting effects at the cellular level.

The synthesis of collagen was quantified using a PICP EIA kit (Procollagen Type I C-Peptide Enzyme ImmunoAssay KIT).

Evaluation of cytotoxicity at concentrations of 10 ppm, 1 ppm, 0.1 ppm, 0.01 ppm, and 0.001 ppm in human-derived fibroblasts before the experiment (method of culturing fibroblasts for MTT test [Reference: Mossman T. (1983) Rapid Colorimetric Assay for Cellular Growth & Survival: application to proliferation & cytotoxicity assays.Journal of Immunological Methods 65, 55-63]).

In the experiments, the final concentrations of cystanoside A were 1 ppm and 10 ppm, and each sample was added to the culture medium of human fibroblasts, incubated for 1 day, and then the culture medium was taken and collagen at each concentration was collected using PICP EIA kit. The degree of synthesis was measured at 450 nm using a spectrophotometer. For comparison of the effects, the degree of collagen synthesis was measured by the same method for the culture medium (control) of the fibroblasts to which nothing was added and the sample to which the vitamin C was added at a final concentration of 52.8 μg / ml. Collagen production was measured as UV absorbance, the collagen production increase rate was calculated as the ratio of collagen production relative to the control, the results are summarized in Table 1 below.

Collagen Biosynthesis Effect of Cysanoside A (Repeat Number = 4,)
sample
Absorbance Absorbance average Collagen growth rate (%) Sistanoside A
10 ppm 408.78
436.9
252.5 457.27 427.09 454.4 Sistanoside A
1 ppm 330.76
333.3
192.7 316.21 322.24 364.07 Control group 173 173 - Vitamin C
(52.8 μg / ml) 221.4
221.4
128.0

As can be seen from the results of Table 1, cystanoside A (cistanoside A) showed a better collagen synthesis effect at a lower concentration than when applying the vitamin C generally known to have collagen synthesis ability.

Example  2: whitening effect experiment

Confirmation of melanin production inhibitory effect

The compound of formula 1 was added to the culture solution of mouse melanoma cells (B-16 mouse melanoma cells) to test the whitening effect at the cellular level. (Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980).

Before the experiment, rat melanoma cells were assessed for toxicity, and non-toxic concentrations were selected for whitening evaluation.

The compound of formula 1 was tested in a final concentration of 0.01ug / ml, 0.1ug / ml, 1ug / ml, 10ug / ml in the culture medium, Arbutin as a control was added to the medium to 200ug / ml, respectively, B-16 The cells were treated with melanoma cells and cultured for 3 days.

Then, cells were trypsin-treated (trypsin) was removed from the culture vessel and centrifuged to extract melanin. The detached cells were added with 1 ml of sodium hydroxide solution (1 N concentration), boiled for 10 minutes to dissolve the melanin, and the absorbance was measured at 400 nanometers (nm) using a spectrophotometer to measure the amount of melanin produced.

The melanin amount was measured by the absorbance of the unit cell count (10 ⁶ cells). The relative melanin production relative to the control group was calculated as the inhibition rate (%) and the results are summarized in Table 2. In addition, the experiment was repeated three times.

Inhibitory effect of melanin production at the cellular level sample Melanin production Inhibition rate (%) Control group (no addition) 0.065 ± 0.002 - Control Group 1: Arbutin (200 mg / ml) 0.033 ± 0.001 49% Compound of Formula 1 (0.01 mg / ml) 0.044 ± 0.001 32% Compound of Formula 1 (0.1mg / ml) 0.007 ± 0.000 89% Compound of Formula 1 (1 mg / ml) 0.003 ± 0.000 95% Compound of Formula 1 (10 mg / ml) 0.003 ± 0.000 95%

As can be seen from the results of Table 2, the compound of Formula 1 has a superior melanin production inhibitory ability against the cultured mouse melanoma cells compared with the known whitening material Arbutin (Arbutin).

Formulation example  1: Preparation of pharmaceutical preparations

1. Manufacturing of powder

0.001 g of compound of Formula 1

1g lactose

The above components were mixed and packed in airtight bags to prepare powders.

2. Preparation of tablets

0.2 mg of compound of Formula 1

100 mg of corn starch

Lactose 100mg

Stearic acid  Magnesium 2mg

After mixing the above components, tablets were prepared by tableting according to a conventional method for producing tablets.

3. Preparation of Capsule

0.2 mg of compound of Formula 1

100 mg of corn starch

Lactose 100mg

Stearic acid  Magnesium 2mg

After mixing the above components, the capsules were filled in gelatin capsules according to the conventional preparation method of capsules.

4. Manufacture of rings

0.003 g of compound of Formula 1

Lactose 1.5 g

1 g of glycerin

Xylitol  0.5 g

After mixing the above components, they were prepared so as to be 4 g per one ring according to a conventional method.

5. Manufacture of granules

2 mg of compound of formula 1

Soybean Extract 50mg

Glucose 200 mg

Starch 600 mg

After mixing the above components, 100 mg of 30% ethanol was added and dried at 60 ° C. to form granules, and then filled in fabric.

Formulation example  2: manufacture of cosmetics

1. Preparation of Soft Cosmetics (Skin Lotion)

Like the following composition, a flexible longevity containing the compound of formula 1 as an active ingredient was prepared according to a conventional method.

0.1 wt% of a compound of Formula 1

Beta-1,3-Glucan 1.0 wt%

Butylene Glycol 2.0 wt%

Propylene Glycol 2.0 wt%

Carboxy vinyl polymer 0.1 wt%

Fiji-12 nonylphenyl ether 0.2% by weight

Polysorbate 80 0.4 wt%

Ethanol 10.0 wt%

0.1% by weight of triethanolamine

0.05 wt% preservative

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100% by weight

2. Preparation of Nutrients (Milk Lotion)

As shown in the following composition, nutrient longevity containing the compound of Formula 1 as an active ingredient was prepared according to a conventional method.

0.1 wt% of a compound of Formula 1

Beta-1,3-Glucan 1.0 wt%

Beeswax 4.0 wt%

Polysorbate60 1.5 wt%

Sorbanthesquioleate 1.5 wt%

0.5% by weight of liquid paraffin

Caprylic / Capric Triglycerides 5.0 wt%

Glycerin 3.0 wt%

Butylene Glycol 3.0 wt%

Propylene Glycol 3.0 wt%

Carboxy vinyl polymer 0.1 wt%

0.2% by weight of triethanolamine

0.05 wt% preservative

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100% by weight

3. Manufacture of nutritional cream

As in the following composition, a nourishing cream containing the compound of formula 1 as an active ingredient was prepared according to a conventional method.

0.2 wt% of a compound of Formula 1

Beta-1,3-Glucan 5.0 wt%

Beeswax 10.0 wt%

Polysorbate60 1.5 wt%

Sebum 60 Cured Castor Oil 2.0 wt%

0.5 wt% sorbitan sesquioleate

10.0% by weight of liquid paraffin

Squalane 5.0 wt%

Caprylic / Capric Triglycerides 5.0 wt%

Glycerin 5.0 wt%

Butylene Glycol 3.0 wt%

Propylene Glycol 3.0 wt%

0.2% by weight of triethanolamine

0.05 wt% preservative

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100% by weight

4. Preparation of Massage Cream

As in the following composition, a massage cream containing a compound of Formula 1 as an active ingredient was prepared according to a conventional method.

0.1 wt% of a compound of Formula 1

Beta-1,3-Glucan 3.0 wt%

Beeswax 10.0 wt%

Polysorbate60 1.5 wt%

Sebum 60 Cured Castor Oil 2.0 wt%

Sorbanthesquioleate 0.8 wt%

40.0% by weight of liquid paraffin

Squalane 5.0 wt%

Caprylic / Capric Triglyceride 4.0 wt%

Glycerin 5.0 wt%

Butylene Glycol 3.0 wt%

Propylene Glycol 3.0 wt%

0.2% by weight of triethanolamine

0.05 wt% preservative

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100% by weight

5. Manufacture of pack

As in the following composition, a pack containing the compound of formula 1 as an active ingredient was prepared according to a conventional method.

0.2 wt% of a compound of Formula 1

Beta-1,3-Glucan 1.0 wt%

Polyvinyl Alcohol 13.0 wt%

Sodium Carboxymethyl Cellulose 0.2% by weight

Glycerin 5.0 wt%

Allantoin 0.1 wt%

Ethanol 6.0 wt%

0.3% by weight of sebum-12 nonylphenyl ether

Polysorbate 60 0.3 wt%

0.05 wt% preservative

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100% by weight

Formulation example  3: External skin preparations  Produce

1. Preparation of Gel

As in the following composition, a gel containing the compound of formula 1 as an active ingredient was prepared according to a conventional method.

0.1 wt% of a compound of Formula 1

Beta-1,3-Glucan 0.1 wt%

0.05% by weight of ethylenediamine sodium acetate

Glycerin 5.0 wt%

Carboxy vinyl polymer 0.3 wt%

Ethanol 5.0 wt%

Fiji-60 Cured Castor Oil 0.5 wt%

0.3% by weight of triethanolamine

0.05 wt% preservative

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100% by weight

2. Manufacture of ointments

As shown in the following composition, an ointment containing the compound of formula 1 as an active ingredient was prepared according to a conventional method.

0.5% by weight of compound of formula 1

Beta-1,3-Glucan 10.0 wt%

Beeswax 10.0 wt%

Polysorbate 60 5.0 wt%

Sebum 60 Cured Castor Oil 2.0 wt%

Sorbanthesquioleate 0.5 wt%

Vaseline 5.0 wt%

10.0% by weight of liquid paraffin

Squalane 5.0 wt%

Shea Butter 3.0 wt%

Caprylic / Capric Triglycerides 5.0 wt%

Glycerin 10.0 wt%

Propylene Glycol 10.2 wt%

0.2% by weight of triethanolamine

0.05 wt% preservative

0.05% by weight of pigment

0.05% by weight fragrance

Purified water to 100% by weight

3. Preparation of Topical Drug (Gel Ointment)

As the following composition, a gel ointment comprising the compound of formula 1 as an active ingredient was prepared according to a conventional method.

0.5% by weight of compound of formula 1

Beta-1,3-Glucan 10.0 wt%

1.5% by weight of polyacrylic acid (Carbopol 940)

Isopropanol 5.0 wt%

Hexylene glycol 25.0 wt%

Triethanolamine 1.7 wt%

Deionized water to 100% by weight

4. Preparation of medicament (patch) for topical administration

As in the following composition, a patch containing the compound of Formula 1 as an active ingredient was prepared according to a conventional method.

0.5% by weight of compound of formula 1

Beta-1,3-Glucan 3.0 wt%

Hexylene glycol 20.0 wt%

Diethylamine 0.7 wt%

1.0% by weight of polyacrylic acid (Carbopol 934P)

Sodium sulfite 0.1 wt%

1.0 weight% of polyoxyethylene lauryl ether (E.O = 9)

1.0% by weight of polyhydroxyethylene cetyl stearyl ether (Cetomacrogol 1000)

Viscous paraffin oil 2.5% by weight

Caprylic acid ester / capric acid ester (Cetiol LC) 2.5% by weight

Polyethylene glycol 400 3.0 wt%

Deionized water to 100% by weight

Formulation example  4: manufacture of food

Food containing the compound of formula 1 of the present invention was prepared as follows.

1. Manufacture of Flour Food

0.05 to 1.0 parts by weight of the compound of Formula 1 was added to flour, and bread, cake, cookies, crackers and noodles were prepared using this mixture to prepare health food.

2. Manufacturing of Dairy Products

0.2 parts by weight of the compound of Formula 1 was added to milk, and various dairy products such as butter and ice cream were prepared using the milk.

3. Manufacture of wire

Brown rice, barley, glutinous rice, and yulmu were alphad by a known method, and then dried and roasted to prepare a powder having a particle size of 60 mesh. Black beans, black sesame seeds, and sesame seeds were also steamed and dried in a known manner, and then roasted to prepare a powder having a particle size of 60 mesh. The compound of Chemical Formula 1 was concentrated under reduced pressure in a vacuum concentrator, and dried by spraying and drying with a hot air drier to grind the dried product to a particle size of 60 mesh using a grinder to obtain a dry powder.

The dry powder of the grains, seeds and the compound of Formula 1 prepared in the above was prepared by blending in the following ratio with respect to 100 parts by weight of the mixed powder.

(30 parts by weight of brown rice, 15 parts by weight of yulmu, 20 parts by weight of barley)

Seeds (7 parts by weight of perilla, 8 parts by weight of black beans, 7 parts by weight of black sesame seeds)

Compound of formula 1 (0.1 parts by weight),

(0.5 part by weight),

Foxglove (0.5 Weight portion )

Formulation example  5: manufacture of beverages

1. Manufacture of health drinks

0.1 mg of compound of Formula 1

Citric acid 1000 mg

100 g of oligosaccharide

Plum concentrate 2 g

Taurine 1 g

Purified water  By adding a full 900 mL

After mixing the above components according to the conventional healthy beverage production method, and stirred and heated at 85 ℃ for about 1 hour, the resulting solution is filtered and obtained by sterilization in a sterilized 2L-container, sealed sterilization and then stored in the refrigerator It was used to prepare a healthy beverage composition of the invention.

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.

2. Preparation of Vegetable Juice

1 g of the compound of Chemical Formula 1 of the present invention was added to 1,000 mL of tomato or carrot juice to prepare vegetable juice for health promotion.

3. Preparation of Fruit Juice

1 g of the compound of Formula 1 was added to 1,000 mL of apple or grape juice to prepare fruit juice for health promotion.

Claims (20)

A pharmaceutical composition for enhancing skin elasticity comprising a compound represented by the following Chemical Formula 1.
[Formula 1]

The method according to claim 1,
Compound represented by the formula (1) is a skin composition for enhancing the pharmaceutical composition, characterized in that it comprises 0.0001 to 10% by weight relative to the total composition.
Skin external preparation for enhancing skin elasticity comprising a compound represented by the formula (1).
[Formula 1]

The method according to claim 3,
The external preparation is an external preparation for skin elasticity enhancement in the form of an ointment, patch, gel, cream or spray.
The method according to claim 3,
The compound represented by the formula (1) is a skin external preparation for skin elasticity, characterized in that it comprises 0.0001 to 10% by weight compared to the total skin external preparation.
Cosmetic composition for enhancing skin elasticity comprising a compound represented by the formula (1).
[Formula 1]

The method of claim 6,
The cosmetic composition is a cosmetic composition for enhancing skin elasticity is a formulation of a lotion, essence, lotion, cream, pack, gel, powder, foundation or detergent.
The method of claim 6,
The compound represented by the following Formula 1 is a cosmetic composition for enhancing skin elasticity, characterized in that it comprises 0.0001 to 10% by weight relative to the total composition.
Health functional food for skin elasticity containing a compound represented by the formula (1).
[Formula 1]

The method of claim 9,
The compound represented by the following formula (1) is a health functional food for skin elasticity, characterized in that it comprises 0.0001 to 10% by weight compared to the total health functional food.
Whitening pharmaceutical composition comprising a compound represented by the formula (1).
[Formula 1]

12. The method of claim 11,
Compound represented by the formula (1) is a whitening pharmaceutical composition, characterized in that it comprises 0.0001 to 10% by weight relative to the total composition.
A skin external preparation for whitening comprising a compound represented by the following Chemical Formula 1.
[Formula 1]

The method of claim 13,
The external preparation for skin whitening is a formulation of an ointment, patch, gel, cream or spray.
The method of claim 13,
The compound represented by the formula (1) is a skin external preparation for whitening, characterized in that it comprises 0.0001 to 10% by weight compared to the total skin external preparation.
A cosmetic composition for whitening comprising a compound represented by the following formula (1).
[Formula 1]

The method of claim 16,
The cosmetic composition is a cosmetic composition for whitening, the formulation of a lotion, essence, lotion, cream, pack, gel, powder, foundation or detergent.
The method of claim 16,
The compound represented by the following formula (1) is a whitening cosmetic composition, characterized in that it comprises 0.0001 to 10% by weight relative to the total composition.
Health functional food for whitening comprising a compound represented by the formula (1).
[Formula 1]

The method of claim 19,
The compound represented by Formula 1 is a whitening health functional food, characterized in that it comprises 0.0001 to 10% by weight compared to the total health functional food.