JPH0692291B2 - Skin whitening agent - Google Patents

Skin whitening agent

Info

Publication number
JPH0692291B2
JPH0692291B2 JP27846086A JP27846086A JPH0692291B2 JP H0692291 B2 JPH0692291 B2 JP H0692291B2 JP 27846086 A JP27846086 A JP 27846086A JP 27846086 A JP27846086 A JP 27846086A JP H0692291 B2 JPH0692291 B2 JP H0692291B2
Authority
JP
Japan
Prior art keywords
solution
whitening agent
sample
prepared
homocysteine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP27846086A
Other languages
Japanese (ja)
Other versions
JPS63132812A (en
Inventor
武彦 阿部
重夫 海老塚
進 波羅
Original Assignee
株式会社肌粧品科学開放研究所
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 株式会社肌粧品科学開放研究所 filed Critical 株式会社肌粧品科学開放研究所
Priority to JP27846086A priority Critical patent/JPH0692291B2/en
Publication of JPS63132812A publication Critical patent/JPS63132812A/en
Publication of JPH0692291B2 publication Critical patent/JPH0692291B2/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A61K8/447Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof containing sulfur

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Dermatology (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Cosmetics (AREA)

Description

【発明の詳細な説明】 産業上の利用分野 本発明は、皮膚の黒化を防止するためにメラニン色素の
生成を阻害する物質を添加した皮膚美白剤に関するもの
である。
TECHNICAL FIELD The present invention relates to a skin lightening agent containing a substance that inhibits the formation of melanin pigment in order to prevent skin blackening.

従来技術 従来の皮膚美白剤としては、システイン,アスコルビン
酸及びその誘導体,コロイド硫黄等を含有させたクリー
ム,ローション,パウダー,パック等が製品化されて知
られている。これらの美白剤は、表皮の基底層に存在し
ている色素細胞(メラノサイト)の中にある酸化酵素チ
ロシナーゼが活性を帯び、アミノ酸の一種であるチロシ
ンを酸化重合して、黒色のメラニンを生成するのを阻害
する作用を持つために、皮膚の美白剤として使用されて
いる。
2. Description of the Related Art As conventional skin lightening agents, creams, lotions, powders, packs and the like containing cysteine, ascorbic acid and its derivatives, colloidal sulfur and the like have been commercialized and known. In these whitening agents, the oxidase tyrosinase in the pigment cells (melanocytes) present in the basal layer of the epidermis is activated, and oxidative polymerization of tyrosine, which is a type of amino acid, produces black melanin. It is used as a skin whitening agent because it has an effect of inhibiting

発明が解決しようとする問題点 しかしながらかかる従来の美白剤は、次のような問題点
を有していた。
Problems to be Solved by the Invention However, such conventional whitening agents have the following problems.

アスコルビン酸を製剤中に配合した場合、水分,温度,
光,pHの影響を受けやすく、容易に酸化されて着色して
しまい、メラニン生成阻害作用が失われてしまうため
に、当然美白作用もなくなってしまうという不都合があ
った。そのため、アスコルビン酸をエステル化して安定
性を向上させた誘導体が開発されているが、安定性の面
においていまだ充分とはいえない。さらにアスコルビン
酸のエステル化には製造コストがかかり過ぎるといった
不都合もあった。
When ascorbic acid is added to the formulation, the water content, temperature,
Since it is easily affected by light and pH, it is easily oxidized and colored, and the melanin production inhibitory action is lost, so naturally there is a disadvantage that the whitening action is also lost. Therefore, a derivative in which ascorbic acid is esterified to improve the stability has been developed, but it is still insufficient in terms of stability. Further, there is a disadvantage that esterification of ascorbic acid requires too much manufacturing cost.

システインは酸化を受けやすく、長期に保存した場合に
美白作用がなくなってしまうという不都合があった。
Cysteine is susceptible to oxidation and has a disadvantage that the whitening effect is lost when it is stored for a long period of time.

コロイド硫黄を利用した美白剤の場合は、安定性の面で
はすぐれているものの、特有のにおいがあり、製品とし
て好ましくないといった不都合があった。
The whitening agent using colloidal sulfur has excellent stability, but has a peculiar odor and is not preferable as a product.

そこで、本発明者達は、かかる従来技術の欠点に鑑み鋭
意検討した結果、ホモシステインにメラニン生成阻害作
用があり、且つ安定性を有することを見出し発明したの
である。
Therefore, as a result of intensive studies in view of the drawbacks of the prior art, the present inventors have found that homocysteine has a melanin production inhibitory action and is stable, and has invented.

問題を解決するための手段 すなわち、本発明はC4H9NO2Sの化学式であらわされるホ
モシステイン(homocysteine)又はそのエステルを主剤
としたクリーム,パック,ローション等の美白剤により
本目的を達成する。
Means for Solving the Problem That is, the present invention achieves this object by a whitening agent such as cream, pack, lotion and the like, which is mainly composed of homocysteine represented by the chemical formula of C 4 H 9 NO 2 S or its ester. To do.

作用 本発明の美白剤は、その主成分であるホモシステインの
SH基が、酵素のチロシナーゼによりチロシンからメラニ
ンを生成する過程において中間生成物であるドーパキノ
ンなどと結合し、ソラニン生成反応を阻害するのであ
る。したがって、メラニン色素が生成されないので、皮
膚は黒化せずに済む。
Action The whitening agent of the present invention comprises homocysteine
The SH group binds to an intermediate product such as dopaquinone in the process of producing melanin from tyrosine by the enzyme tyrosinase and inhibits the solanine production reaction. Therefore, the melanin pigment is not produced, so that the skin is not blackened.

実施例 以下に実施例に従って詳細に説明する。Example Hereinafter, the example will be described in detail.

実施例−1[クリーム] 以下に示す配合よりなるクリームを作成し、それらのメ
ラニン生成阻害作用を比較検討した。
Example-1 [Cream] Creams having the formulations shown below were prepared and their melanin production inhibitory effects were compared and examined.

Aの成分を混合し加熱溶解し、これにかきまぜながら加
熱混合したBの成分を加えて攪拌する。その後香料を適
量加え、攪拌しながら冷却し、放置してクリームを得
る。こうして得られたクリームにつき次に示す方法でメ
ラニン色素生成の阻害作用を試験した。
The component A is mixed and dissolved by heating, and the component B heated and mixed is added to this while stirring, and the mixture is stirred. After that, an appropriate amount of fragrance is added, cooled with stirring, and left to stand to obtain a cream. The cream thus obtained was tested for its inhibitory effect on melanin pigment formation by the following method.

試験方法 まず以下の溶液を調整する。Test method First, the following solutions are prepared.

(1)リン酸緩衝液(pH6.8) (2)L−チロシンのリン酸緩衝液(pH6.8)溶液(0.3
mg/ml) (3)チロシナーゼ(きのこ製,シグマ社)のリン酸緩
衝液(pH6.8)溶液(0.5mg/ml) 次に、リン酸緩衝液(1),L−チロシンのリン酸緩衝液
溶液(2)及びチロシナーゼのリン酸緩衝液溶液(3)
並びに比較例及び本発明のクリームを下記に示すよ
うに混合し、よくかきまぜて、以下に示す試料を三つ作
成する。
(1) Phosphate buffer (pH 6.8) (2) L-tyrosine phosphate buffer (pH 6.8) solution (0.3
(3) Phosphate buffer solution (pH 6.8) of tyrosinase (manufactured by Mushroom, Sigma) (0.5 mg / ml) Next, phosphate buffer solution (1), phosphate buffer of L-tyrosine Solution (2) and tyrosinase phosphate buffer solution (3)
In addition, the comparative examples and the cream of the present invention are mixed as shown below and stirred well to prepare three samples shown below.

試料−1:(1)の溶液2ml,(2)の溶液2ml,(3)の溶
液0.1mlを混合しかきまぜたもの4.1ml 試料−2:(1)の溶液1.8ml,(2)の溶液2ml,(3)の
溶液0.1ml及び本発明のクリーム0.2mlを混合しかきま
ぜたもの4.1ml 試料−3:(1)の溶液1.8ml,(2)の溶液2ml,(3)の
溶液0.1ml及び比較例のクリーム0.2mlを混合しかきま
ぜたもの4.1ml 作成した試料−1,2,3について分光光度計で層長10mm,波
長475nmにおける吸光度を測定し、経時的変化を記録計
に記録する。
Sample-1: 2 ml of solution of (1), 2 ml of solution of (2), 0.1 ml of solution of (3) mixed and stirred 4.1 ml Sample-2: 1.8 ml of solution of (1), solution of (2) 2 ml, 0.1 ml of the solution of (3) and 0.2 ml of the cream of the present invention were mixed and stirred 4.1 ml Sample-3: 1.8 ml of the solution of (1), 2 ml of the solution of (2), 0.1 ml of the solution of (3) And 0.2 ml of the cream of the comparative example mixed and stirred 4.1 ml Measure the absorbance at a layer length of 10 mm and wavelength of 475 nm with the spectrophotometer for the prepared samples-1, 2 and 3 and record the change over time in a recorder. .

その結果第1図に示すように試料−1及び3のものでは
経時的に吸光度が増大したが、試料−2のものではその
ような変化はみられなかった。
As a result, as shown in FIG. 1, the absorbances of Samples 1 and 3 increased with time, but no such change was observed in Sample-2.

実施例−2[乳液] 以下に示す配合よりなる乳液を作成し、それらのメラニ
ン生成阻害作用を比較検討した。
Example-2 [Emulsion] Emulsions having the formulations shown below were prepared and their melanin production inhibitory effects were compared and examined.

Aの成分を混合し加熱溶解し、これにかきまぜながら加
熱混合したBの成分を加えて攪拌する。その後香料を適
量加え、攪拌しながら冷却し、放置して乳液を得る。
The component A is mixed and dissolved by heating, and the component B heated and mixed is added to this while stirring, and the mixture is stirred. Thereafter, an appropriate amount of perfume is added, the mixture is cooled with stirring, and left to stand to obtain an emulsion.

以上のようにして得られた乳液について実施例−1で示
した試験方法のように試料−1,試料−2′,試料−3′
を作成し、吸光度を測定した。
Regarding the emulsion obtained as described above, the sample-1, sample-2 ', sample-3' were prepared in the same manner as in the test method shown in Example-1.
Was prepared and the absorbance was measured.

その結果は第2図に示すようになった。The result is shown in FIG.

実施例−3[ローション] 以下に示す配合よりなるローションを作成し、それらの
メラニン生成阻害作用を比較検討した。
Example-3 [Lotion] A lotion having the following formulation was prepared and their melanin production inhibitory effects were compared and examined.

精製水にグリセリン,プロピレングリコールを加え、室
温下に溶解する。一方エタノールに他の成分を加えて室
温下に溶解し、前述の水溶液に加え、濾過してローショ
ン液を得る。
Glycerin and propylene glycol are added to purified water and dissolved at room temperature. On the other hand, other components are added to ethanol, dissolved at room temperature, added to the above aqueous solution, and filtered to obtain a lotion solution.

以上のようにして得られたローションについて実施例−
1で示した試験方法のように試料−1,試料−2″,試料
−3″を作成し、吸光度を測定した。その結果は第3図
に示すようになった。
Example regarding the lotion obtained as described above-
Sample-1, Sample-2 ", and Sample-3" were prepared in the same manner as the test method shown in 1, and the absorbance was measured. The result is shown in FIG.

実施例−4[パック] 以下に示す配合よりなるパックを作成し、それらのメラ
ニン生成阻害作用を比較検討した。
Example-4 [Pack] A pack having the following formulation was prepared and their melanin production inhibitory effects were compared and examined.

精製水にプロピレングリコール,ホモシステインを加え
て溶解する。それにポリビニアルコール及びカルボキシ
メチルセルロースナトリウムを加え、70℃に加熱し、攪
拌しながら溶解する。これにアルコールに香料,防腐剤
を溶解したものを加え混合した後冷却してパックを得
る。
Add propylene glycol and homocysteine to purified water and dissolve. Polyvinyl alcohol and sodium carboxymethyl cellulose are added thereto, heated to 70 ° C. and dissolved with stirring. To this is added a mixture of alcohol with a perfume and a preservative, and the mixture is mixed and cooled to obtain a pack.

以上のようにして得られたパックについて実施例−1で
示した試験方法のように試料−1,試料−2,試料−3
を作成し、吸光度を測定した。その結果は第4図に示
すようになった。
For the packs obtained as described above, Sample-1, Sample-2, and Sample-3 were prepared in the same manner as the test method shown in Example-1.
Was prepared and the absorbance was measured. The result is shown in FIG.

実施例−5 リン酸緩衝液(pH4.5)に3.0mmol/lのホモシステインと
システイン及びアスコルビン酸をそれぞれ溶かした溶液
を1ケ月放置したものについて、実施例−1で示した方
法にてそれらのメラニン色素生成の阻害作用を測定し
た。
Example-5 A solution prepared by dissolving 3.0 mmol / l of homocysteine, cysteine and ascorbic acid in a phosphate buffer (pH 4.5) was allowed to stand for 1 month and then subjected to the same method as shown in Example-1. Of melanin pigment production was measured.

その結果ホモシステインは、調整直後と同程度の美白作
用を示したが、システインは調整直後活性がみられたも
のでも、放置したものではメラニン色素生成の阻害作用
は全くみられなかった。
As a result, homocysteine showed the same whitening effect as immediately after the adjustment, but even if cysteine was found to be active immediately after the adjustment, no inhibitory effect on melanin pigment formation was observed when left alone.

また、1ケ月放置したときに、アスコルビン酸の溶液の
方では黄褐色の着色がみられたが、ホモシステインでは
着色はみられなかった。
Further, when left for one month, the solution of ascorbic acid was colored yellowish brown, but the homocysteine was not colored.

実施例−6 リン酸緩衝液(pH6.8)にホモシステイン,システイ
ン,アスコルビン酸をそれぞれ溶かして、0.1,0.2,0.5,
1.0,1.5,2.0,2.5,3.0(mmol/l)の溶液を作成した。こ
の溶液1mlにリン酸緩衝液(pH6.8)を2ml,L−チロシン
のリン酸緩衝液(pH6.8)溶液(0.3mg/l)を1ml,チロシ
ナーゼ(きのこ製,シグマ社)のリン酸緩衝液(pH6.
8)溶液(0.5mg/l)を0.1ml加えて混合し、分光光度計
で、吸光度(475nm)を測定した。但し吸光度は経時的
に変化するので、その最大値を読み取って比較した。
Example-6 Homocysteine, cysteine, and ascorbic acid were dissolved in a phosphate buffer (pH 6.8) to give 0.1, 0.2, 0.5,
Solutions of 1.0, 1.5, 2.0, 2.5, 3.0 (mmol / l) were prepared. To 1 ml of this solution, 2 ml of phosphate buffer (pH 6.8), 1 ml of L-tyrosine phosphate buffer (pH 6.8) solution (0.3 mg / l), and phosphoric acid of tyrosinase (manufactured by Mushroom, Sigma) Buffer solution (pH 6.
8) 0.1 ml of the solution (0.5 mg / l) was added and mixed, and the absorbance (475 nm) was measured with a spectrophotometer. However, since the absorbance changes with time, the maximum value was read and compared.

その結果は表−1に示す通りとなった。The results are shown in Table-1.

以上のようにホモシステインは他の美白剤よりも低濃度
で有効に作用することがわかる。
As described above, it can be seen that homocysteine acts effectively at a lower concentration than other whitening agents.

効果 以上述べたように本発明にかかる美白剤は、従来の美白
剤に比較して安定性に優れていると共に低濃度にてメラ
ニン生成阻害作用を発揮することができる。
Effect As described above, the whitening agent according to the present invention is superior in stability to conventional whitening agents and can exhibit a melanin production inhibitory effect at a low concentration.

【図面の簡単な説明】[Brief description of drawings]

第1図から第4図は、それぞれ本発明の美白剤と比較例
の美白剤との吸光度の時間的変化を示すグラフである。
FIG. 1 to FIG. 4 are graphs showing temporal changes in absorbance of the whitening agent of the present invention and the whitening agent of the comparative example, respectively.

───────────────────────────────────────────────────── フロントページの続き (56)参考文献 特開 昭59−157009(JP,A) 特開 昭59−128320(JP,A) 特開 昭58−198421(JP,A) 特開 昭55−15429(JP,A) 特開 昭52−136925(JP,A) 実開 昭62−3537(JP,U) 特公 昭33−6799(JP,B1) ─────────────────────────────────────────────────── ─── Continuation of the front page (56) Reference JP 59-157009 (JP, A) JP 59-128320 (JP, A) JP 58-198421 (JP, A) JP 55- 15429 (JP, A) JP-A-52-136925 (JP, A) Actually developed S62-3537 (JP, U) JP-B-33-6799 (JP, B1)

Claims (2)

【特許請求の範囲】[Claims] 【請求項1】ホモシステイン又はそのエステルを主剤と
する皮膚美白剤。
1. A skin lightening agent containing homocysteine or an ester thereof as a main ingredient.
【請求項2】ホモシステイン又はそのエステルを0.5mmo
l/l以上含有していることを特徴とする皮膚美白剤。
2. 0.5 mmo of homocysteine or its ester
A skin whitening agent characterized by containing l / l or more.
JP27846086A 1986-11-21 1986-11-21 Skin whitening agent Expired - Fee Related JPH0692291B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP27846086A JPH0692291B2 (en) 1986-11-21 1986-11-21 Skin whitening agent

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP27846086A JPH0692291B2 (en) 1986-11-21 1986-11-21 Skin whitening agent

Publications (2)

Publication Number Publication Date
JPS63132812A JPS63132812A (en) 1988-06-04
JPH0692291B2 true JPH0692291B2 (en) 1994-11-16

Family

ID=17597640

Family Applications (1)

Application Number Title Priority Date Filing Date
JP27846086A Expired - Fee Related JPH0692291B2 (en) 1986-11-21 1986-11-21 Skin whitening agent

Country Status (1)

Country Link
JP (1) JPH0692291B2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW233264B (en) * 1992-02-03 1994-11-01 Otsuka Pharma Co Ltd

Also Published As

Publication number Publication date
JPS63132812A (en) 1988-06-04

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