JP2005289811A - Melanogenesis regulator - Google Patents

Melanogenesis regulator Download PDF

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Publication number
JP2005289811A
JP2005289811A JP2002095549A JP2002095549A JP2005289811A JP 2005289811 A JP2005289811 A JP 2005289811A JP 2002095549 A JP2002095549 A JP 2002095549A JP 2002095549 A JP2002095549 A JP 2002095549A JP 2005289811 A JP2005289811 A JP 2005289811A
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Prior art keywords
skin
melanin production
melanogenesis
melanin
skin color
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JP2002095549A
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Inventor
Kenji Sakamoto
賢二 坂本
Hideo Nagoshi
秀夫 名越
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SAKAMOTO BIO KK
Sakamoto Bio Co Ltd
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SAKAMOTO BIO KK
Sakamoto Bio Co Ltd
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Priority to JP2002095549A priority Critical patent/JP2005289811A/en
Priority to AU2003227273A priority patent/AU2003227273A1/en
Priority to PCT/JP2003/003838 priority patent/WO2003082227A1/en
Publication of JP2005289811A publication Critical patent/JP2005289811A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/04Preparations for care of the skin for chemically tanning the skin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Birds (AREA)
  • Molecular Biology (AREA)
  • Toxicology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Cosmetics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a composition such as a melanogenesis regulator having a function of effectively controlling skin pigmentation or skin pigment loss, a skin color controller, and a skin care preparation for external use having a function of regulating melanogenesis or a function of controlling the skin color. <P>SOLUTION: The followings are provided: a melanogenesis regulator containing a melanogenesis inhibitor and a melanogenesis promotor, a skin color controller, a composition containing a melanogenesis inhibitor and a melanogenesis promotor, a skin care preparation for external use, and a skin care preparation for external use for controlling the skin color. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

【0001】
【発明の属する技術分野】
本発明は、メラニン生成を調整する機能や肌色をコントロールする機能を有した、メラニン生成調整剤、肌色コントロール剤及び皮膚外用剤等の組成物に関する。
【0002】
【従来の技術】
従来の美白化粧料等のメラニン抑制外用組成物は、メラニンの生成を抑制する成分を配合することが行われてきた。しかしながら、実際の皮膚におけるメラニンの生成並びにその分配過程は非常に複雑であり、メラニン生成の一機序を阻害抑制し得る成分を配合した化粧料であっても、肌の色素の沈着や消失を効果的にコントロールするに至っていない。
【0003】
【発明が解決しようとする課題】
本発明は上記事情に鑑みてなされたもので、その目的は、肌の色素の沈着や消失を効果的にコントロールする機能をもったメラニン生成調整剤、肌色コントロール剤、さらにメラニン生成を調整する機能や肌色をコントロールする機能を有した皮膚外用剤等の組成物を提供することにある。
【0004】
【課題を解決するための手段】
本発明者らは上記課題を解決するために鋭意研究を行った結果、メラニン生成抑制作用をもつ物質とメラニンの生成促進作用をもつ物質を併用することにより上記課題が解決されることを見出し、本発明を完成するに至った。
【0005】
すなわち、本発明は、メラニン生成抑制剤とメラニン生成促進剤とを含有するメラニン生成調整剤である。
【0006】
さらに、本発明は、メラニン生成抑制剤とメラニン生成促進剤とを含有する肌色コントロール剤である。
【0007】
さらに、本発明は、メラニン生成抑制剤とメラニン生成促進剤とを含有する組成物である。
【0008】
本発明において、前記組成物は皮膚外用剤であることができ、さらに肌色コントロール用皮膚外用剤であることができる。
【0009】
【発明の実施の形態】
以下、本発明の実施形態について詳述する。
【0010】
本発明において用いられるメラニン生成抑制剤としては、メラニン生成抑制作用をもつ物質であれば特に制限されない。
メラニン生成抑制剤の例を挙げれば、例えば、アルブチン、コウジ酸、ビタミンC、ハイドロキノン等である。
【0011】
本発明において用いられるメラニン生成促進剤としては、メラニンの生成促進作用をもつ物質であれば特に制限されない。
メラニン生成促進剤の例を挙げれば、例えば、ルペオール、キク科植物抽出物、サンショウ(実)抽出物等である。
【0012】
本発明の前記メラニン生成抑制剤とメラニン生成促進剤との混合物は、後述するようにそれぞれの混合比率により所望のメラニン生成をコントロールすることができる。したがって、当該混合物を含有してメラニン生成調整剤として用いることができる。また、当該混合物を肌に注目すれば肌色をコントロールする機能を発揮する肌色コントロール剤として用いることができる。さらに、当該混合物を配合した組成物は、メラニン生成調整機能、肌色コントロール機能を有し、組成物として、例えば皮膚や毛髪等を対象とした医薬品、食品、化粧品、入浴剤等に応用することができる。
【0013】
特に、当該混合物を配合した皮膚外用剤は、メラニン生成調整機能、肌色コントロール機能を有した皮膚外用剤、特に肌色コントロール用皮膚外用剤として化粧品、医薬品等に応用することができる。
【0014】
本発明の皮膚外用剤を調製するに当たって、前記メラニン生成抑制剤とメラニン生成促進剤の混合物の配合量は、特に限定されないが、当該物質の安全性を考慮すれば混合物として皮膚外用剤全量中10質量%以下が好ましく、効果を有効に発揮させるためには、0.1〜10質量%が好ましい。さらに好ましくは、1〜10質量%である。
【0015】
本発明の前記皮膚外用剤は、通常化粧品、医薬部外品、医薬品等に一般に配合される成分、例えば油分、界面活性剤、保湿剤、増粘剤、水溶性高分子、皮膜剤、非水溶性高分子、高分子エマルション、粉末、顔料、染料、低級アルコール、多価アルコール、糖類、紫外線吸収剤、アミノ酸類、ビタミン類、薬剤、植物抽出物、有機酸、有機アミン、金属イオン封鎖剤、pH調整剤、酸化防止剤、抗菌剤、防腐剤、収斂剤、清涼剤、香料、水等を必要に応じて、本発明の効果を損なわない範囲で適宜配合して調製される。
【0016】
本発明の皮膚外用剤としては、例えば、軟膏剤、溶液、クリーム、乳液、化粧水、ローション、ジェル、エッセンス(美容液)、ファンデーション、パック・マスク、スティック等の形態で化粧品、医薬部外品を含む広い範囲で適用可能である。
【0017】
また、皮膚外用剤の剤型も、溶液系、可溶化系、乳化系、粉末系、粉末分散系、油液系、ゲル系、軟膏系、エアゾール系、水−油2層系、水−油−粉末3層系等、幅広い剤型を採り得る。
【0018】
【実施例】
以下実施例を挙げて本発明を具体的に説明する。配合量については質量%である。
【0019】
[B16メラノーマ細胞におけるメラニン生成調整作用]
メラニン生成調整作用は、マウス由来のメラニン生成細胞であるB16 10F7メラノーマ細胞を用い、メラニン生成抑制物質としてアルブチンを、メラニン生成促進物質としてルペオールを用いた。試料を培養液で稀釈した溶液を細胞に作用させメラニンの生成を観察し評価した。B−16細胞は70%コンフルエントの細胞をPBSにて洗いトリプシンを加え剥離し、トリプシンと同量の血清入り培地(E−MEM+10%FBS)を加え細胞を集め遠心した(800rpm,5min.)。細胞数をカウントし、約10cells/ml(E−MEM+10%FBS)に調整した。アルブチン、ルペオールは、培養液中の最終濃度100μg/mL〜1μg/mLになるように希釈し、この希釈液(20μL)の入ったプレートに細胞浮遊液を80μLずつ分注した。さらに、37℃、COインキュベーターにて72時間培養し、顕微鏡により、細胞におけるメラニン生成を観察した。さらに、メラニンが生成されている場合、培地を除き300μLの1N、NaOHで、メラニンを溶かし、470nmの紫外線吸収を測定することでメラニン生成量を評価した。溶媒であるメタノールを反応させた値を100%とし、アルブチン、ルペオールを用量変化させ、それぞれの濃度でのメラニンの生成率(%)を求めた。この結果を表1に示す。表1中のメラニンの生成率の単位は%である。表1においては、例えば、アルブチン100μg/mLとルペオール100μg/mLの混合系でのメラニンの生成率は68%と読むことができる。
【0020】
【表1】

Figure 2005289811
【0021】
表1から分かるように、本発明に係る、当該混合物は、メラノーマB16細胞に対し、広い範囲でのメラニン生成調整作用を示しており、メラニン生成調整剤として有用であることが明らかである。また、当該混合物は、肌等に適用することにより肌色のカラーコントロール効果を持つことを示している。
【0022】
以下、本発明の当該混合物を配合した化粧料を常法により調製し、本発明の組成物の実施例として示す。なお、いずれの実施例においても優れたメラニン生成調整効果、肌色コントロール効果が見られた。
【0023】
Figure 2005289811
【0024】
Figure 2005289811
【0025】
Figure 2005289811
【0026】
Figure 2005289811
【0027】
Figure 2005289811
【0028】
Figure 2005289811
【0029】
Figure 2005289811
【0030】
Figure 2005289811
【0031】
【発明の効果】
以上、詳述したように、本発明のメラニン生成調整剤は、メラニン生成抑制剤とメラニン生成促進剤とを適当な割合で混合することにより、所望のメラニン量を得るようにすることができる。そして、肌色コントロール剤として、肌の色を使用者が望む色にコントロールすることができる。したがって、当該混合物を配合した組成物は、医薬品、食品、化粧品、入浴剤等としてメラニン生成調整、肌色コントロール等の機能を有したものとすることができる。特に、当該組成物はメラニン生成調整機能、肌色コントロール機能を有した皮膚外用剤として、例えば肌色コントロール用皮膚外用剤として化粧品、医薬部外品、医薬品等に応用することができる。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to compositions such as a melanin production regulator, a skin color control agent, and a skin external preparation, which have a function of regulating melanin production and a function of controlling skin color.
[0002]
[Prior art]
Conventional melanin-suppressing compositions such as conventional whitening cosmetics have been formulated with ingredients that suppress the production of melanin. However, the production and distribution process of melanin in the actual skin is very complex, and even cosmetics containing ingredients that can inhibit and suppress one mechanism of melanin production can cause skin pigmentation and disappearance. It has not been effectively controlled.
[0003]
[Problems to be solved by the invention]
The present invention has been made in view of the above circumstances, and its purpose is to provide a melanin production regulator, a skin color control agent having a function of effectively controlling skin pigmentation and disappearance, and a function of regulating melanin production. Another object of the present invention is to provide a composition such as an external preparation for skin having a function of controlling skin color.
[0004]
[Means for Solving the Problems]
As a result of diligent research to solve the above problems, the present inventors have found that the above problems can be solved by using a substance having a melanin production inhibitory action and a substance having a melanin production promoting action, The present invention has been completed.
[0005]
That is, this invention is a melanin production regulator containing a melanin production inhibitor and a melanin production promoter.
[0006]
Furthermore, this invention is a skin color control agent containing a melanin production inhibitor and a melanin production promoter.
[0007]
Furthermore, this invention is a composition containing a melanin production inhibitor and a melanin production promoter.
[0008]
In the present invention, the composition may be an external preparation for skin, and may further be an external preparation for skin color control.
[0009]
DETAILED DESCRIPTION OF THE INVENTION
Hereinafter, embodiments of the present invention will be described in detail.
[0010]
The melanin production inhibitor used in the present invention is not particularly limited as long as it is a substance having a melanin production inhibitory action.
Examples of melanin production inhibitors include arbutin, kojic acid, vitamin C, hydroquinone and the like.
[0011]
The melanin production promoter used in the present invention is not particularly limited as long as it has a melanin production promotion effect.
Examples of melanin production promoters include lupeol, asteraceae plant extracts, and salamander (fruit) extracts.
[0012]
As described later, the mixture of the melanin production inhibitor and the melanin production accelerator of the present invention can control the production of desired melanin by the respective mixing ratios. Therefore, the mixture can be used as a melanin production regulator. Moreover, if the said mixture pays attention to skin, it can be used as a skin color control agent which exhibits the function which controls skin color. Furthermore, the composition containing the mixture has a melanin production adjustment function and a skin color control function, and can be applied as a composition to, for example, pharmaceuticals, foods, cosmetics, bathing agents and the like for the skin and hair. it can.
[0013]
In particular, a skin external preparation blended with the mixture can be applied to cosmetics, pharmaceuticals, etc. as a skin external preparation having a melanin production adjustment function and a skin color control function, particularly as a skin external control skin color control function.
[0014]
In preparing the external preparation for skin of the present invention, the amount of the mixture of the melanin production inhibitor and the melanin production accelerator is not particularly limited, but considering the safety of the substance, 10% of the total amount of the external preparation for skin as a mixture. The mass% is preferable, and 0.1 to 10 mass% is preferable for effectively exhibiting the effect. More preferably, it is 1-10 mass%.
[0015]
The external preparation for skin of the present invention is a component generally blended in cosmetics, quasi drugs, pharmaceuticals, etc., such as oils, surfactants, humectants, thickeners, water-soluble polymers, film agents, water-insoluble Polymers, polymer emulsions, powders, pigments, dyes, lower alcohols, polyhydric alcohols, sugars, UV absorbers, amino acids, vitamins, drugs, plant extracts, organic acids, organic amines, sequestering agents, A pH adjuster, an antioxidant, an antibacterial agent, an antiseptic, an astringent, a refreshing agent, a fragrance, water and the like are appropriately blended and prepared as necessary within a range not impairing the effects of the present invention.
[0016]
Examples of the external preparation for skin of the present invention include cosmetics and quasi drugs in the form of ointments, solutions, creams, emulsions, lotions, lotions, gels, essences (essentials), foundations, packs, masks, sticks and the like. It is applicable in a wide range including.
[0017]
Further, the dosage form of the external preparation for skin is also a solution system, solubilization system, emulsification system, powder system, powder dispersion system, oil liquid system, gel system, ointment system, aerosol system, water-oil two-layer system, water-oil. -A wide range of dosage forms such as a powder three-layer system can be adopted.
[0018]
【Example】
Hereinafter, the present invention will be specifically described with reference to examples. About a compounding quantity, it is the mass%.
[0019]
[Adjustment of melanin production in B16 melanoma cells]
For the melanin production regulating action, B16 10F7 melanoma cells that are mouse-derived melanin cells were used, arbutin was used as a melanin production inhibitor, and lupeol was used as a melanogenesis promoter. A solution obtained by diluting a sample with a culture solution was allowed to act on cells to observe and evaluate the production of melanin. For B-16 cells, 70% confluent cells were washed with PBS, trypsin was added and detached, the same amount of serum-containing medium as trypsin (E-MEM + 10% FBS) was added, and the cells were collected and centrifuged (800 rpm, 5 min.). The number of cells was counted and adjusted to about 10 4 cells / ml (E-MEM + 10% FBS). Arbutin and lupeol were diluted to a final concentration in the culture solution of 100 μg / mL to 1 μg / mL, and 80 μL of the cell suspension was dispensed into the plate containing this diluted solution (20 μL). Further, the cells were cultured for 72 hours in a CO 2 incubator at 37 ° C., and melanin production in the cells was observed with a microscope. Furthermore, when melanin was produced | generated, the melanin production amount was evaluated by melt | dissolving melanin with 300 microliters 1N, NaOH except the culture medium and measuring a 470 nm ultraviolet-ray absorption. The reaction rate of methanol as a solvent was taken as 100%, the doses of arbutin and lupeol were changed, and the production rate (%) of melanin at each concentration was determined. The results are shown in Table 1. The unit of the melanin production rate in Table 1 is%. In Table 1, for example, the production rate of melanin in a mixed system of arbutin 100 μg / mL and lupeol 100 μg / mL can be read as 68%.
[0020]
[Table 1]
Figure 2005289811
[0021]
As can be seen from Table 1, the mixture according to the present invention exhibits a wide range of melanin production regulating action on melanoma B16 cells, and is clearly useful as a melanin production regulator. Moreover, it has shown that the said mixture has the color control effect of skin color by applying to skin etc.
[0022]
Hereinafter, cosmetics formulated with the mixture of the present invention are prepared by a conventional method and shown as examples of the composition of the present invention. In any of the examples, excellent melanin production adjustment effect and skin color control effect were observed.
[0023]
Figure 2005289811
[0024]
Figure 2005289811
[0025]
Figure 2005289811
[0026]
Figure 2005289811
[0027]
Figure 2005289811
[0028]
Figure 2005289811
[0029]
Figure 2005289811
[0030]
Figure 2005289811
[0031]
【The invention's effect】
As described above in detail, the melanin production regulator of the present invention can obtain a desired amount of melanin by mixing a melanin production inhibitor and a melanin production promoter at an appropriate ratio. As a skin color control agent, the skin color can be controlled to a color desired by the user. Therefore, the composition containing the mixture can have functions such as melanin production adjustment and skin color control as a pharmaceutical, food, cosmetics, bathing agent and the like. In particular, the composition can be applied as a skin external preparation having a melanin production adjusting function and a skin color control function, for example, as a skin color control skin external preparation, in cosmetics, quasi drugs, pharmaceuticals and the like.

Claims (5)

メラニン生成抑制剤とメラニン生成促進剤とを含有するメラニン生成調整剤。  A melanin production regulator containing a melanin production inhibitor and a melanin production accelerator. メラニン生成抑制剤とメラニン生成促進剤とを含有する肌色コントロール剤。  A skin color control agent comprising a melanin production inhibitor and a melanin production promoter. メラニン生成抑制剤とメラニン生成促進剤とを含有する組成物。  A composition comprising a melanin production inhibitor and a melanin production promoter. 皮膚外用剤である請求項3記載の組成物。  The composition according to claim 3, which is an external preparation for skin. 肌色コントロール用皮膚外用剤である請求項3記載の組成物。  The composition according to claim 3, which is a skin external preparation for skin color control.
JP2002095549A 2002-03-29 2002-03-29 Melanogenesis regulator Pending JP2005289811A (en)

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JP2001199873A (en) * 2000-01-17 2001-07-24 Masaaki Okubo Composition for external use
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