KR102322441B1 - Composition for skin whitening containing an extract derived from a petiole of Green tea - Google Patents

Abstract

The present invention relates to a skin whitening composition containing an extract derived from green tea leaf stalk which is safe for the skin, has excellent skin whitening effect and has high stability.
The present invention has excellent use value in terms of utilization of waste resources by using green tea leaf stalks that have not been utilized and have been discarded. In addition, the composition of the present invention contains green tea leaf stalk-derived extract, which is safe for skin and has high formulation stability, exhibits excellent skin whitening effect, reduces pigmentation symptoms such as spots and freckles, improves skin dullness, and improves skin color. make it look bright.

Description

Composition for skin whitening containing an extract derived from green tea leaf stalk {Composition for skin whitening containing an extract derived from a petiole of Green tea}

The present invention relates to a skin whitening composition containing an extract derived from green tea leaf stalk which is safe for the skin, has excellent skin whitening effect and has high stability.

A person's skin color is determined by several factors, such as the activity of melanocytes that make melanin pigment, the distribution of blood vessels, the thickness of the skin, and the presence or absence of pigments inside and outside the human body such as carotenoids and bilirubin. In particular, the most important factor is the black pigment called melanin, which is produced by the action of several enzymes such as tyrosinase in melanocytes. The formation of melanin is influenced by genetic factors, hormone secretion, physiological factors related to stress, etc., and environmental factors such as UV irradiation. Melanin exists in the skin and plays an important role in protecting the body from UV rays, but it is known that melanin is overproduced to promote pigmentation and skin aging, and to play a major role in inducing skin cancer. Ascorbic acid, kojic adcid, arbutin, and hudroquinone have been previously used to treat or alleviate skin pigmentation symptoms and excessive melanin pigmentation caused by UV exposure. , glutathione or derivatives thereof, and substances with tyrosinase inhibitory activity have been used in combination with cosmetics or pharmaceuticals. Its use is restricted due to stability issues and the like.

Accordingly, the present inventors have completed the present invention by discovering that the extract of green tea petiole, which was not utilized and discarded, can provide an excellent skin whitening effect without irritation to the skin.

Accordingly, an object of the present invention is to provide a composition exhibiting an excellent skin whitening effect by using an extract derived from green tea leaf stalk.

In order to achieve the above object, the present invention provides a composition for external application for skin whitening containing an extract derived from green tea leaf stalk as an active ingredient.

The present invention has excellent use value in terms of utilization of waste resources by using green tea leaf stalks that have not been utilized and have been discarded. In addition, the composition of the present invention contains green tea leaf stalk-derived extract, which is safe for skin and has high formulation stability, exhibits excellent skin whitening effect, reduces pigmentation symptoms such as spots and freckles, improves skin dullness, and improves skin color. make it look bright.

1 is a graph showing the results of high performance liquid chromatography (HPLC) analysis of green tea leaf stalk extracts.

The composition of the present invention contains green tea leaf stalk extract as an active ingredient, thereby providing an excellent skin whitening effect.

Green tea has generally been made using the leaves of the tea tree (Camellia sinensis). However, in the present invention, although there is no limitation on the type of tea tree and the number of cultivation days, it is characterized in that the used part is the petiole. In addition, as the petiole used in the present invention, both dried or non-dried petioles may be used.

The petiole of green tea used in the present invention is a part called petiole, and the vascular bundle in the petiole serves to connect the vascular bundle of the stem and the vascular bundle of the leaf body, and was previously discarded after collecting the leaves from the tea tree. However, as a result of the present inventors' analysis of green tea petioles, it could be predicted that there would be a difference in the effect provided from green tea leaves as it showed a large difference in the type and content of ingredients contained in green tea leaves.

In addition, by preparing an extract derived from green tea leaf stalk, which was not utilized and discarded in the past, and applying it to a product, it can be used as a high value-added functional material and applied product, so the present invention is excellent in terms of utilization of waste resources worth it

The green tea petiole-derived extract used in the present invention can be prepared by a method known in the art, and the method is not particularly limited, but a method of extracting the water-soluble component contained in the green tea petiole is preferably used.

Specifically, hot water 5 times the weight of green tea petiole, specifically purified water having a temperature of 80 to 90° C., is added to the dried green tea petiole for extraction. After heating and stirring for 2 hours while maintaining the temperature, and cooling the temperature to room temperature, only the water-soluble component is separated, and this is first filtered. Ethanol corresponding to twice the total weight of the filtrate is added while stirring slowly, the chlorophyll of the supernatant is removed, and only the precipitates are collected and dried with hot air. When drying with hot air, it maintains 30~40℃ to prevent thermal deterioration. In this way, the extract derived from the green tea leaf stalk used in the present invention can be prepared.

The green tea leaf stalk-derived extract prepared in this way contains 0.90% of catechin and 0.12% of caffeine, and the content of the components is different from that of general green tea leaf extract, which contains 22.1% of catechin and 4.61% of caffeine, The effects exhibited by this are also different from each other.

The composition of the present invention may contain the green tea leaf stalk-derived extract in an amount of 0.001 to 20% by weight based on the total weight of the composition. When the green tea leaf stalk-derived extract is contained in an amount of less than 0.001% based on the total weight of the composition, the expression of the whitening effect is weak, and when it is contained in an amount of 20% by weight or more, skin irritation may occur.

The composition of the present invention has excellent skin whitening effect, is safe for the skin, and has high stability, so it is preferable for industrial use.

The composition of the present invention may be formulated as a composition for external application to the skin, particularly a cosmetic composition, and may be formulated containing a cosmetically or dermatologically acceptable medium or base. In addition, the composition of the present invention may be provided in any dosage form suitable for topical application, for example, a solution, an emulsion obtained by dispersing an oil phase in an aqueous phase, an emulsion obtained by dispersing an aqueous phase in an oil phase, suspension, solid, gel, powder, It may be provided in the form of a paste, foam or aerosol composition. Compositions of such formulations can be prepared according to conventional methods in the art.

In addition, the composition according to the present invention may include other components that can give a synergistic effect to the main effect, preferably within a range that does not impair the main effect, in addition to the above substances. In addition, the composition according to the present invention may further comprise a humectant, emollient, ultraviolet absorber, preservative, bactericide, antioxidant, pH adjuster, organic and inorganic pigment, fragrance, cooling agent or limiting agent. The blending amount of the component can be easily selected by those skilled in the art within the range that does not impair the purpose and effect of the present invention, and the blending amount may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight, based on the total weight of the composition .

In addition, the composition of the present invention may be formulated as a pharmaceutical composition. When the composition according to the present invention is applied to pharmaceuticals, it can be formulated for oral or parenteral administration in solid, semi-solid or liquid form by adding an inorganic or organic carrier that is compatible with the active ingredient used in the present invention. , The pharmaceutical composition according to the present invention may be administered orally, parenterally, rectally, topically, transdermally, intravenously, intramuscularly, intraperitoneally, subcutaneously, or the like.

Formulations for oral administration include tablets, pills, granules, capsules, powders, fine granules, powders, emulsions, syrups, pellets, and the like. In addition, formulations for parenteral administration include injections, drops, ointments, lotions, sprays, suspensions, emulsions, suppositories, and the like. The composition according to the present invention can be easily formulated by carrying out a conventional method, and in this case, surfactants, excipients, colorants, spices, preservatives, stabilizers, buffers, suspending agents, and other commercially available adjuvants can be appropriately used. have.

The dosage of the active ingredient of the pharmaceutical composition of the present invention will vary depending on the age, sex, weight, pathological condition and severity of the subject to be administered, the route of administration or the judgment of the prescriber. Determination of an appropriate dose based on these factors is within the level of one skilled in the art, and its daily dose is for example 0.1 mg/kg/day to 100 mg/kg/day, more specifically 5 mg/kg/day to 50 mg/kg It can be, but is not limited to, /work.

Hereinafter, the present invention will be described in more detail through examples. These examples are only for illustrating the present invention, and it will be apparent to those of ordinary skill in the art that the scope of the present invention is not to be construed as being limited by these examples.

[Example 1] Preparation of green tea leaf stalk-derived extract

Purified water having a temperature of 80 to 90° C. was added to the dried green tea petiole (purchased from Jangwon Co., Ltd.) in an amount 5 times the weight of the green tea petiole, and the mixture was heated and stirred for 2 hours while maintaining the temperature. After cooling to room temperature, only water-soluble components were separated, and Adventec No. 131 (Adventec MFS, Inc., Japan) was used for primary filtration. Ethanol equivalent to twice the total weight of the filtrate is added with stirring slowly, the chlorophyll of the supernatant is removed, only the precipitates are collected, and dried with hot air while maintaining a temperature of 30 to 40 ° C. It was obtained as (yield: 1-3%).

[Comparative Example 1] Preparation of green tea leaf extract

At the Amorepacific Sulloc Tea Plant, purified water with a temperature of 80-90° C. was added to Okrok No. 2 leaf tea in an amount 5 times the weight of green tea leaves, and the temperature was maintained while heating and stirring for 2 hours. After cooling to room temperature, only water-soluble components were separated, and Adventec No. 131 (Adventec MFS, Inc., Japan) was used for primary filtration. After filtration, the mixture was concentrated using a vacuum distillation apparatus and then dried using a freeze dryer to obtain a green tea leaf extract as a yellowish brown powder.

[Test Example 1] Quantitative analysis of components extracted from green tea petioles

In order to determine the components contained in green tea petiole, HPLC analysis was performed on the green tea petiole extract prepared in Example 1, and the results are shown in FIG. 1 and Table 1.

The liquid chromatography used in the experiment is an Alliance 2695 of Waters, and a 2996 photodiode array UV detector (PDA) is connected thereto. As a column, a symmetry C18 column (4.6 mm x 7.5 cm, 3.5 μm) from Waters was used, and Empower II program from Waters was used for data processing. The injection volume was 20.00 μl.

Peak Name RT Area % Area Height Amount One GC 5.832 33599 2.26 3547 10.230 2 EGC 9.519 106220 7.13 6820 34.724 3 C 12.990 25360 1.70 1474 2.517 4 CAF 15.324 574818 38.59 35113 12.677 5 EC 21.903 70493 4.73 3923 6.050 6 EGCG 22.999 547080 36.73 23985 26.005 7 GCG 27.178 74962 5.03 3896 8.583 8 ECG 39.105 56849 3.82 3028 3.946 9 CG 40.724

(C: catechin, GC: gallocatechin, CG: catechin gallate, GCG: gallocatechin gallate, EC: epicatechin, EGC: epigallocatechin, ECG: epicatechin gallate, EGCG: epigallocatechin gallate, CAF (caffeine)

The % Area for each component in Table 1 means the area of the graph shown in FIG. 1, which increases in proportion to the amount of the component contained therein. As a result of quantifying the components of the green tea petiole extract by comparing the area ratio of each component with the standard area, it was confirmed that the green tea petiole extract contained 0.90% of total catechin and 0.12% of caffeine.

[Test Example 2] Melanin production inhibitory ability evaluation using melan-a (Melan-a) cells

The melanin production inhibitory effect of the green tea leaf stalk-derived extract obtained in Example 1 was evaluated by comparing it with the green tea leaf-derived extract obtained in Comparative Example 1 and arbutin, a known skin lightening material. As cells, melan-a cells derived from normal epidermal melanoblasts of C57BL mouse embryos syngeneic were used.

After seeding in a 48-well plate at 1.5 X 10 ⁴ cells/well, the cells were cultured for 24 hours. After culturing for 24 hours and culturing for 4 days, the test material was treated, and the extract obtained in Example 1 and Comparative Example 1, which is the test material used at this time, used a stock dissolved in DMSO, and 1% stock dissolved in arbutin in water. was diluted in the medium to match the experimental concentrations shown in Table 2 below. In addition, at this time, for comparison, the control group was not treated with any test substance.

After treatment with the test substance, the medium was removed and the cells were washed with DPBS and removed by tapping. Then, 100 μl of 2N NaOH was added, and incubated in an incubator for 1 hour. 90 μl of the cell lysate was transferred to a 96-well plate and absorbance was measured at 475 nm in an ELISA Reader (Synergy 2, BIOTEK, USA).

In addition, the protein was quantified using the BCA method. After 200 μl of BCA (Bicinchoninic acid) solution (solution a: thermo 23228, solution b: PIERCE 1859078) was added to 10 μl of sample per well, it was left in an incubator for 30 minutes, and then absorbance was measured at 560 nm.

The results are shown in Table 2 below by calculating the value of the amount of melanin when the test substance was treated with respect to the amount of melanin in the control group as in Equation 1 below. In addition, at this time, the amount of melanin was used as a protein correction value corrected using the results measured by the BCA method.

test substance Amount of melanin (%) Control (no additive) 100 Example 1 (3.12 ppm) 83.1 Example 1 (6.25 ppm) 78.4 Example 1 (12.5 ppm) 73.9 Example 1 (25 ppm) 68.3 Comparative Example 1 (25 ppm) 97.6 Arbutin (25 ppm) 73.5

Referring to Table 2, when the green tea leaf extract, Comparative Example 1, was treated, the amount of melanin was hardly reduced, whereas when the green tea petiole extract was treated, the amount of melanin was reduced even when treated with a much lower amount. can confirm that In addition, it can be confirmed that even when treated with a concentration lower than the treatment concentration of arbutin, a melanin reduction effect equivalent to that of arbutin can be obtained, and when treated with the same amount, it can be confirmed that a much better melanin reduction effect can be obtained.

From this, it can be seen that the green tea petiole extract exhibits different efficacy from the green tea leaf extract, and can be used as a very excellent skin whitening material.

[Test Example 3] Skin stability evaluation

In order to find out the extent to which the green tea leaf stalk-derived extract used in the present invention stimulates the skin, a human skin primary stimulation test was performed.

The test was conducted twice. In the first round, a total of 40 healthy adult females and 6 males (average age 35.1 years) were targeted, and in the second round, 28 females and 2 males total 30 people (average age). The subjects were 30.1 years old).

Specifically, a solution prepared by dissolving the green tea leaf stalk-derived extract obtained in Example 1 to a concentration of 10% in water was uniformly applied to the skin of the back in an amount of ^{20 mg/cm 2 .}

After application, a patch was attached to the site, the patch was removed after 24 hours, and the first reading was taken 30 minutes later, the second reading was taken after 24 hours, and the last reading was considered definitive. To find out the strength of the skin irritation of the sample, weights are given according to the degree of the positive reaction of the skin (-, +, ++, +++, ++++, 0, 1, 2, 3, 4 respectively) ) to obtain the average reactivity of the skin, and when the average reactivity was 1 or more, the stimulus was read as positive. Specific criteria are presented in Table 3 below. In addition, the skin average reactivity was calculated by Equation 2 below, and the result determination criteria are presented in Table 4.

Criteria reaction weight criteria for judgment - 0 : no response + One : faint erythema ++ 2 : Demarcated but mild erythema, edema and papules +++ 3 : Distinct erythema, papules and blisters ++++ 4 : cannon

Result Judgment Criteria average skin reactivity Criteria 0.0 to 0.9
1.0 to 2.9
3.0 to 4.9
5.0 or higher non-irritant
mild stimulation
central stimulus
strong stimulus

As a result of the measurement, the average skin reactivity after using the green tea leaf stalk-derived extract was between 0.0 and 0.9, and it was finally determined that there was no irritation to the skin.

Hereinafter, a formulation example of the composition according to the present invention will be described, but the pharmaceutical composition and the cosmetic composition can be applied in various formulations, which is not intended to limit the present invention, but merely to describe it in detail.

[Formulation Example 1] Softening lotion (skin lotion)

A softening lotion was prepared in a conventional manner according to the composition shown in Table 5 below.

compounding ingredients content (% by weight) Green tea leaf stalk-derived extract of Example 1 0.2 glycerin 3.0 butylene glycol 2.0 propylene glycol 2.0 Carboxyvinyl Polymer 0.1 PEG-12 Nonylphenyl Ether 0.2 Polysorbate 80 0.4 ethanol 10.0 triethanolamine 0.1 Preservatives, Colors, Flavors appropriate amount Purified water remaining amount

[Formulation Example 2] Nutrient lotion (milk lotion)

Nutrient lotion was prepared in a conventional manner according to the composition shown in Table 6 below.

compounding ingredients content (% by weight) Green tea leaf stalk-derived extract of Example 1 1.0 glycerin 3.0 butylene glycol 3.0 propylene glycol 3.0 Carboxyvinyl Polymer 0.1 beeswax 4.0 Polysorbate 60 1.5 Caprylic/Capric Triglycerides 5.0 squalane 5.0 Sorbitasequioleate 1.5 liquid paraffin 0.5 cetearyl alcohol 1.0 triethanolamine 0.2 Preservatives, Colors, Flavors appropriate amount Purified water remaining amount

[Formulation Example 3] Nourishing cream

Nutrient creams were prepared in a conventional manner according to the composition shown in Table 7 below.

compounding ingredients content (wt%) Green tea leaf stalk-derived extract of Example 1 2.0 glycerin 3.0 butylene glycol 3.0 liquid paraffin 7.0 beta glucan 7.0 Carbomer 0.1 Caprylic/Capric Triglycerides 3.0 squalane 5.0 cetearyl glucoside 1.5 Sorbitan Stearate 0.4 Polysorbate 60 1.2 triethanolamine 0.1 Preservatives, Colors, Flavors appropriate amount Purified water remaining amount

[Formulation Example 4] Massage Cream

A massage cream was prepared in a conventional manner according to the composition shown in Table 8 below.

compounding ingredients content (wt%) Green tea leaf stalk-derived extract of Example 1 3.0 glycerin 8.0 butylene glycol 4.0 liquid paraffin 45.0 beta glucan 7.0 Carbomer 0.1 Caprylic/Capric Triglycerides 3.0 beeswax 4.0 cetearyl glucoside 1.5 Sesqui oleate sorbitan 0.9 Vaseline 3.0 paraffin 1.5 Preservatives, Colors, Flavors appropriate amount Purified water remaining amount

[Formulation Example 5] Pack

A pack was prepared in a conventional manner according to the composition shown in Table 9 below.

compounding ingredients content (wt%) Green tea leaf stalk-derived extract of Example 1 0.2 glycerin 4.0 polyvinyl alcohol 15.0 Hyaluronic Acid Extract 5.0 beta glucan 7.0 allantoin 0.1 nonyl phenyl ether 0.4 Polysorbate 60 1.2 ethanol preservative 6.0 Appropriate amount Preservatives, Colors, Flavors appropriate amount Purified water remaining amount

[Formulation Example 6] Ointment

An ointment was prepared in a conventional manner according to the composition shown in Table 10 below.

compounding ingredients content (wt%) Green tea leaf stalk-derived extract of Example 1 0.2 glycerin 8.0 butylene glycol 4.0 liquid paraffin 15.0 beta glucan 7.0 Carbomer 0.1 Caprylic/Capric Triglycerides 3.0 squalane 1.0 cetearyl glucoside 1.5 Sorbitan Stearate 0.4 cetearyl alcohol 1.0 beeswax 4.0 Preservatives, Colors, Flavors appropriate amount Purified water remaining amount

As the specific parts of the present invention have been described in detail above, for those of ordinary skill in the art, these specific descriptions are only preferred embodiments, and it is clear that the scope of the present invention is not limited thereby. something to do. Accordingly, it is intended that the substantial scope of the present invention be defined by the appended claims and their equivalents.

Claims (4)

A cosmetic composition for skin whitening containing extracts derived from green tea leaf stalks as an active ingredient. The cosmetic composition for skin whitening according to claim 1, wherein the extract is contained in an amount of 0.001 to 20% by weight based on the total weight of the composition. The cosmetic composition for skin whitening according to claim 1, wherein the extract derived from green tea petioles is extracted from green tea petioles using water as a solvent. The cosmetic composition for skin whitening according to claim 1, wherein the composition inhibits melanin production.

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