KR20180075863A - A composition for skin whitening comprising roselle extracts - Google Patents

A composition for skin whitening comprising roselle extracts Download PDF

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Publication number
KR20180075863A
KR20180075863A KR1020160179745A KR20160179745A KR20180075863A KR 20180075863 A KR20180075863 A KR 20180075863A KR 1020160179745 A KR1020160179745 A KR 1020160179745A KR 20160179745 A KR20160179745 A KR 20160179745A KR 20180075863 A KR20180075863 A KR 20180075863A
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KR
South Korea
Prior art keywords
extract
composition
present
skin whitening
whitening
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KR1020160179745A
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Korean (ko)
Inventor
강연자
김진철
박종국
정용하
전동하
천정윤
박상미
정다운
한협우
김명준
장민정
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(주)튜링겐코리아
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Priority to KR1020160179745A priority Critical patent/KR20180075863A/en
Publication of KR20180075863A publication Critical patent/KR20180075863A/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin

Abstract

The present invention relates to a composition for whitening whitening comprising Roselle ( Hibiscus sabdariffa ) extract as an active ingredient, and more particularly, to a composition for whitening whitening comprising at least one of the rosewort extract of the present invention, particularly rosewood leaf extract, The composition containing the extract as an active ingredient is excellent in tyrosinase, elastase and collagenase inhibitory activity and is effective for skin whitening and has no cytotoxicity and skin side effects, and can be used safely in a cosmetic composition or a pharmaceutical composition.

Description

TECHNICAL FIELD [0001] The present invention relates to a composition for skin whitening comprising a rosin extract as an active ingredient, a composition for skin whitening,

The present invention relates to a composition for skin whitening comprising Roselle extract, and more particularly to a skin whitening composition comprising roselene extract, roselene leaf extract, rosewort extract or roselle stem skin extract as an active ingredient. ≪ / RTI >

In recent years, in advanced countries such as Europe, America, and Japan, cosmetic materials derived from animals have been rapidly replaced with materials derived from plants due to the incidence of mad cow disease. Plant derived materials include surfactants such as olive oil, palm oil and saponin, wheat germ oil, rice bran oil or phospholipids; A water-soluble component containing an amino acid, a protein, or a saccharide; Various natural products such as rosemary leaves, willow bark extract, niraji root, honey or carrot are used as moisturizers, film formers, skin protectants, lipsticks, and celery.

Recently, it has been proposed that a material inhibiting the activity of elastase and matrix metalloproteinase-1 (MMP-1), a material promoting the synthesis of hyaluronic acid, a material having active oxygen- Materials for promoting the proliferation of cells are being developed or used as raw materials for functional cosmetics, and cosmetics containing various types of natural materials are pouring out. However, scientific and systematic studies and verification of their efficacy have been lacking.

Melanin, a skin pigment factor, is produced against skin damage caused by ultraviolet rays and protects the skin. Melanin production starts with the oxidation of tyrosine by tyrosinase, and DOPA and DOPA chromium chrome), and then DHICA and DHI. DHI-eu melanin, DHICA-eu melanin, and pheo melanin are known to be produced.

Melanin pigmentation of skin caused by ultraviolet exposure is a cause of black spots in spiny freckles. In order to prevent and improve the blackening of such skin, kojic acid, arbutin, vitamin C derivatives and the like However, it has recently been reported that the effect of inhibiting melanogenesis in cell and in vivo is less than that inhibiting tyrosinase in vitro in the case of Nuruk acid, and that it may induce liver cancer in long-term use. In addition, arbutin has a problem of cytotoxicity of hydroquinone series, and vitamin C also has a problem of chemical stability, which makes it difficult to keep for a long time.

As the above-mentioned problems are known, studies on functional cosmetics or drugs using various natural extracts as alternative raw materials have been actively conducted, but there is insufficient verification of its efficacy and toxicity, and clinical effects are not satisfactory yet The development of new alternative raw materials and scientific and systematic efficacy verification are urgently needed.

On the other hand, Roselle (Roselle, Hibiscus sabdariffa ) is a perennial herbaceous plant of the dicotyledonous plant, and is known as the origin of West Africa. The rosette's stem is split at the bottom with many branches, 2m in height, reddish and hairless. The leaves on the bottom of the stem are ovate, the leaves on the upper part of the stem are deeply divided into 3 pieces, and the leaves and petiole are in various colors such as red light or dark green. Rozel is also grown mainly in the tropics to obtain fibers. Young calyxes and pods are used as raw materials for raw food, jam, jelly, syrup, soft drinks, etc. and fermented to make wine. Leaves and petiole are used for salad And seeds are also used as emollients, diuretics, and tonic agents.

Korean Patent Publication No. 2005-0000255 discloses a Hibiscus sabdariffa extract having an inhibitory effect on lipid accumulation in the cytoplasm and an effect of inhibiting the differentiation of adipocytes, and Korean Patent Publication No. 2016-011435 Discloses a cosmetic composition for controlling skin temperature containing an extract of Hibiscus as an active ingredient, but no consideration has been given to skin whitening effect.

Accordingly, the inventors of the present invention have continued to develop a natural substance having a skin whitening effect and fewer side effects on human body, and as a result, discovered that the roselle extract has an excellent effect on skin whitening without cytotoxicity, Completed.

The object of the present invention is to provide a material having skin whitening effect and excellent human stability without cytotoxicity derived from natural materials.

In order to solve the above-mentioned technical problems, the present invention provides a composition for skin whitening comprising a rosin extract as an active ingredient.

Preferably, the composition comprising a rosin extract in the present invention may be a cosmetic composition or a pharmaceutical composition.

The " Roselle ( Hibiscus sabdariffa ) " of the present invention is an annual plant of the dicotyledonous plant,

The term "extract " of the present invention means a preparation which is obtained by squeezing a herbal medicine with an appropriate leaching solution and concentrating by evaporating the leaching solution, and is not limited thereto. The extract, the diluted solution, A dried product obtained by drying, a controlled preparation thereof, or a purified product thereof.

In the present invention, the roselle extract may be at least one selected from the group consisting of rosacea leaf extract, rosacea root extract and rosemary stem peel extract.

The rosin extract of the present invention can be extracted using a conventional extraction solvent known in the art, and the extracted solution can be used in a liquid form or can be used by concentration and / or drying. The extraction solvent may be, for example, (a) water, (b) anhydrous or hydrated lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, propanol, butanol, etc.), (c) Solvent, (d) acetone, (e) ethyl acetate, (f) chloroform or (g) 1,3-butylene glycol as the extraction solvent. Preferably, extraction is carried out using methanol, ethanol or butane. Depending on the extraction solvent, the degree of extraction and the degree of loss of the active ingredient of the extract may differ. Therefore, an appropriate extraction solvent should be selected and used. The extraction method is not particularly limited, and examples thereof include cold extraction, ultrasonic extraction, and reflux cooling extraction.

In addition, the rosewood extract may be obtained by a conventional purification process in addition to the extraction method using the extraction solvent. For example, by separation using an ultrafiltration membrane having a constant molecular weight cut-off value, separation by various chromatographies (made for separation by size, charge, hydrophobicity or affinity), and the like, The rosin extract or the gold extract can also be obtained through the fractionation.

In one specific embodiment of the invention, the rosewort extract is obtained by grinding rosicles, in particular roseweed leaves, rosewort roots or rosewell husks, in an extraction solvent such as water, anhydrous or lower alcohols having 1 to 3 carbon atoms, May be used as an extraction solvent, and the extraction solvent may be used in a volume ratio of 1: 2 to 1: 4.

In one specific embodiment of the present invention, the rosin extract is prepared by pulverizing rosewas and adding 60 to 80% ethanol (EtOH) at a volume ratio of 2 to 4 times at room temperature for 20 to 30 hours, preferably 22 to 26 hours , Followed by recovery by immersion and extraction, followed by concentration with a filter paper.

The composition containing the rosin extract of the present invention exhibits a skin whitening effect and has little cytotoxicity as a natural substance.

In one specific embodiment of the present invention, there is provided a cosmetic composition comprising a rosin extract as an active ingredient.

In one specific embodiment of the present invention, the cosmetic composition may contain, in addition to the rosin extract as an active ingredient, conventional additives such as antioxidants, stabilizers, solubilizers, vitamins, pigments and flavorings, May be further added.

The cosmetic composition of the present invention can be prepared into any of the formulations conventionally produced in the art and can be used as a solution, a suspension, an emulsion, a paste, a gel, a cream, a lotion, a powder, a soap, , Oil, powder foundation, emulsion foundation, wax foundation, spray, emulsion, multiple emulsion, liquid crystal, and the like. More specifically, it can be prepared as a nutritional cream, a convergent lotion, a soft lotion, a lotion, an essence, a nutritional gel or a massage cream.

When the formulation of the present invention is a paste, cream or gel, use is made of an animal oil, vegetable oil, wax, paraffin, starch, tragacanth gum, cellulose derivatives, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide .

When the formulation of the present invention is a powder or a spray, tosse, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. In the case of a spray, in particular, chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, a solubilizing agent or an emulsifying agent is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid esters.

In the case where the formulation of the present invention is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Castellulose, aluminum metahydroxide, bentonite, agar or tracert, etc. may be used.

When the formulation of the present invention is an interfacial active agent-containing cleansing, the carrier component may include aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters.

In one specific embodiment of the present invention, the pharmaceutical composition comprises a pharmaceutically acceptable carrier other than the rosin extract. The pharmaceutically acceptable carriers to be contained in the pharmaceutical composition of the present invention are those conventionally used in the present invention and include lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia rubber, calcium phosphate, alginate, gelatin, But are not limited to, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrups, methylcellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. It is not. The pharmaceutical composition of the present invention may further contain a lubricant, a wetting agent, a sweetening agent, a flavoring agent, an emulsifying agent, a suspending agent, a preservative, etc., in addition to the above components. Suitable pharmaceutically acceptable carriers and formulations are described in detail in Remington ' s Pharmaceutical Sciences (19th ed., 1995).

The pharmaceutical composition of the present invention can be administered orally or parenterally, and is preferably applied by parenteral administration, more preferably topical application by application.

A suitable dosage of the pharmaceutical composition of the present invention may vary depending on such factors as the formulation method, administration method, age, body weight, sex, pathological condition, food, administration time, route of administration, excretion rate, . The dosage of the pharmaceutical composition of the present invention is in the range of 0.001-100 mg / kg on an adult basis. When the composition is an external preparation, it is preferably applied in an amount of 1.0 to 3.0 ml on an adult basis once to five times a day, and continued for 1 month or more. However, the dose is not intended to limit the scope of the present invention.

The pharmaceutical composition of the present invention may be prepared in unit dosage form by formulating it using a pharmaceutically acceptable carrier and / or excipient according to a method which can be easily carried out by a person having ordinary skill in the art, Into the container. The formulations may be in the form of solutions, suspensions, syrups or emulsions in an oil or aqueous medium, or in the form of excipients, powders, powders, granules, tablets or capsules, and may additionally contain dispersing or stabilizing agents.

When the rosin according to the present invention is used in a composition for skin whitening, it is preferably 0.001 to 20.0% by weight, more preferably 0.01 to 10.0% by weight, based on the total weight of the composition. If the content is less than 0.001% by weight, the effect can not be expected. If the content is more than 20.0% by weight, safety or formability is difficult to manufacture. However, the amount of the above-mentioned rosin extract is not particularly limited.

On the other hand, the rosin extract of the present invention is a natural substance and is harmless to human body. Since it has little toxicity and side effects, it can be safely used for long-term use, and can be safely applied to the cosmetic composition or pharmaceutical composition as described above.

As described above, the composition comprising the rosin extract of the present invention as an effective ingredient has an excellent effect on skin whitening, and is free from cytotoxicity and skin side effects, and can be usefully used as a cosmetic composition or a pharmaceutical composition.

Hereinafter, embodiments of the present invention will be described in detail to facilitate understanding of the present invention. However, the embodiments according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the following embodiments. Embodiments of the invention are provided to more fully describe the present invention to those skilled in the art.

The rosin used in this experiment was the material obtained in May 2015.

Example  One: Rosel  Manufacture of leaf extract

70% ethanol (EtOH) was added at a volume ratio of 3 times of the roseline powder, and after repeating the immersion extraction for 24 hours at room temperature for 3 times, 1 filter paper, and the extracts were concentrated at 40 ° C or lower using a rotary vacuum evaporator, and then stored in a refrigerated room after lyophilization.

Example  2: Rosel  Eggplant extract

70% ethanol (EtOH) was added at a ratio of 3 times the volume of the rosell crushed product, and after repeating the immersion extraction for 24 hours at room temperature for 3 times, 1 filter paper, and the extracts were concentrated at 40 ° C or lower using a rotary vacuum evaporator, and then stored in a refrigerated room after lyophilization.

Example  3: Rosel  Stem skin extract

70% Ethanol (EtOH) was added at a ratio of 3 times the volume of the roseline crushed product after the rosemal stem peel was pulverized, and after repeating the immersion extraction for 24 hours at room temperature for 3 times, 1 filter paper, and the extracts were concentrated at 40 ° C or lower using a rotary vacuum evaporator, and then stored in a refrigerated room after lyophilization.

Test Example  One: Skin whitening  For effect verification Tyrosinase  Measurement of inhibitory activity

Tyrosinase is an enzyme containing copper, which is an L-tyrosine (L-3,4-dihydroxyphenylalanine (DOPA)) in the early stage of melanin synthesis. , DOPA to L-dopaquinone (L-dopaquinone). The mitosis of the melanocyte occurs by ultraviolet light and then the melanocyte is activated. In activated melanocytes, tyrosinase synthesis is promoted and melanin is produced and transported out of the epidermis, causing pigmentation such as spots and freckles. Therefore, tyrosine activity inhibitors can effectively inhibit the synthesis of melanin polymers in the skin, so that inhibition of tyrosinase activity in the development of skin whitening agents has been recognized as a useful evaluation method. Thus, tyrosinase plays an important role in the melanin biosynthesis process, so that tyrosinase inhibitors can be used as a substance capable of controlling the melanin pigment production of the skin.

The tyrosinase inhibitory activity was measured according to the Yagi method. To the reaction mixture was added 0.2 mL of mushroom tyrosinase (110 U / mL) to a mixed solution of 0.5 mL of a 1 / 15M sodium phosphate buffer solution (sodium phosphate buffer, pH 6.8), 0.2 mL of a substrate solution in which 10 mM of DOPA had been dissolved and 0.1 mL of a sample solution And the mixture was reacted at 25 DEG C for 2 minutes to measure DOPA chromium generated in the reaction solution in the light having a wavelength of 475 nm. The tyrosinase inhibitory activity was expressed by the absorbance reduction rate of the sample solution added and the non-added sample. Nuruk acid was used as a positive control for comparative analysis.

Table 1 below shows the tyrosinase inhibitory activity of rosewood leaf extract (sample 1), rosemary root extract (sample 2), and rosemary stem bark extract (sample 3)). In Table 1, nuruk acid was used as a positive control.

Samples Inhibitory activity (%) 1000ug / mL 500 ug / mL 250 ug / mL 125 ug / mL 62.5 ug / mL 31.3 ug / mL Sample 1 35.4 30.2 23.4 15.8 11.2 8.7 Sample 2 31.7 26.4 19.3 14.5 10.1 7.8 Sample 3 32.2 27.8 20.7 14.8 11.0 8.1 Kojic acid 94.4 84.8 70.5 50.7 31.7 12.7

Claims (4)

A cosmetic composition for skin whitening comprising Roselle ( Hibiscus sabdariffa ) extract as an active ingredient. The method according to claim 1,
Wherein the rosewort extract is at least one selected from the group consisting of rosel leaf extract, rosel branch extract, and rosemary stem peel extract.
A pharmaceutical composition for skin whitening comprising rosin extract as an active ingredient. The method of claim 3,
Wherein the rosele extract is at least one selected from the group consisting of rosewise leaf extract, rosewort eggplant extract and rosewort stem bark extract.
KR1020160179745A 2016-12-27 2016-12-27 A composition for skin whitening comprising roselle extracts KR20180075863A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020094019A (en) * 2018-12-14 2020-06-18 日本製粉株式会社 Trpa1 activation composition
KR102299846B1 (en) * 2021-03-04 2021-09-09 농업회사법인 (주)로가 Cosmetic composition comprising collagen peptides derived from Hibiscus

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020094019A (en) * 2018-12-14 2020-06-18 日本製粉株式会社 Trpa1 activation composition
KR102299846B1 (en) * 2021-03-04 2021-09-09 농업회사법인 (주)로가 Cosmetic composition comprising collagen peptides derived from Hibiscus

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