Deprecated: The each() function is deprecated. This message will be suppressed on further calls in /home/zhenxiangba/zhenxiangba.com/public_html/phproxy-improved-master/index.php on line 456
JPH0753654B2 - Skin whitening agent - Google Patents
[go: Go Back, main page]

JPH0753654B2 - Skin whitening agent - Google Patents

Skin whitening agent

Info

Publication number
JPH0753654B2
JPH0753654B2 JP61303931A JP30393186A JPH0753654B2 JP H0753654 B2 JPH0753654 B2 JP H0753654B2 JP 61303931 A JP61303931 A JP 61303931A JP 30393186 A JP30393186 A JP 30393186A JP H0753654 B2 JPH0753654 B2 JP H0753654B2
Authority
JP
Japan
Prior art keywords
hinokitiol
whitening agent
homocysteine
whitening
melanin
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
JP61303931A
Other languages
Japanese (ja)
Other versions
JPS63156708A (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 JP61303931A priority Critical patent/JPH0753654B2/en
Publication of JPS63156708A publication Critical patent/JPS63156708A/en
Publication of JPH0753654B2 publication Critical patent/JPH0753654B2/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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35Ketones, e.g. benzophenone
    • 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)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (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複数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 to which a plurality of substances that inhibit the production of melanin pigments have been added in order to prevent darkening of the skin.

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,コロイド硫黄等を主成分としたクリ
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(例えば特開昭59−128320号、特開昭61−
100509号)。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 whitening agents, cysteine, ascorbic acid and its derivatives, creams, lotions, powders, packs and the like containing, as a main component, colloidal sulfur are known to be commercialized (for example, JP-A-59- 128320, JP 61-
No. 100509). These whitening agents are activated by the oxidative enzyme tyrosinase in pigment cells (melanocytes) present in the basal layer of the epidermis, and oxidatively polymerize tyrosine, which is a type of amino acid, to produce black melanin. It is used as a skin whitening agent because it has an effect of inhibiting

また、β−ツヤプリシンと還元物質担持水化ケイ酸アル
ミニウム吸着剤とを配合してなるメラニン生成抑制外用
皮膚製剤が発明され知られている(特開昭59−157009
号)。
Further, an external skin preparation for inhibiting melanin production, which comprises blending β-tsuyapricin and a reducing substance-supporting aluminum borohydride adsorbent, has been invented and known (Japanese Patent Laid-Open No. 59-157009).
issue).

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 its 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
は優れているものの、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 is excellent in 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、ホモシステイン又はそのエステルに加
えてヒノキチオールを併用することにより、それぞれ単
独で使用するよりも大幅に低い濃度で美白効果が得られ
ると共に、安定性に優れることを見出し発明したのであ
る。
Therefore, the present inventors have made extensive studies in view of the drawbacks of the prior art, by using hinokitiol in addition to homocysteine or its ester, whitening effect at a significantly lower concentration than each used alone. The inventors of the present invention have found that, while being obtained, they are excellent in stability.

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)又はそのエステルとヒノ
キチオールとを配合したクリーム,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 provides a whitening agent such as cream, pack or lotion containing homocysteine or its ester represented by the chemical formula of C 4 H 9 NO 2 S and hinokitiol. To achieve.

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、メラニン生成反応を阻害するのであ
る。一方ヒノキチオール自体はチロシナーゼを阻害す
る。そしてこれらホモシステイン又はそのエステルとヒ
ノキチオールとを併用することにより相乗効果が見ら
れ、それぞれ単独で使用するよりも大幅に低い濃度でメ
ラニン色素の生成を阻害する。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 melanin production reaction. On the other hand, hinokitiol itself inhibits tyrosinase. When these homocysteine or its ester and hinokitiol are used in combination, a synergistic effect is observed, and the production of melanin pigment is inhibited at a significantly lower concentration than when used alone. 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。Practical Example Hereinafter, a detailed description will be given according to an example.

(実施例−1) 美白剤の美白効果は、薬剤中に含まれる主成分の濃度に
左右されることから、美白効果を有するヒノキチオー
ル,ホモシステイン,システイン及びアスコルビン酸に
ついて様々な濃度におけるメラニン色素の生成阻害作用
について波長475nmにおける吸光度を次に示す方法で比
較検討した。
(Example-1) Since the whitening effect of a whitening agent depends on the concentration of the main component contained in the drug, hinokitiol, homocysteine, cysteine and ascorbic acid having whitening effects of melanin pigments at various concentrations were used. The production inhibitory effect was compared and examined by the following method using the absorbance at a wavelength of 475 nm.

(試験方法) A:以下の溶液を調整する。(Test method) A: Prepare the following solutions.

(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
(0.3mg/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) B:(1)の溶液1.8ml,(2)の溶液2ml,(3)の溶液0.
1ml及び各美白剤のリン酸緩衝液(pH6.8)溶液1mlを混
合しよくかきまぜ、分光光度計で吸光度(475nm)を測
定する。
(1) Phosphate buffer (pH 6.8) (2) L-tyrosine phosphate buffer (pH 6.8) solution (0.3 mg / ml) (3) Phosphate buffer of tyrosinase (Mushroom, Sigma) Liquid (pH 6.8) Solution (0.5 mg / ml) B: Solution of (1) 1.8 ml, Solution of (2) 2 ml, Solution of (3) 0.
Mix 1 ml and 1 ml of phosphate buffer (pH 6.8) solution of each whitening agent, stir well, and measure the absorbance (475 nm) with a spectrophotometer.

結 果 第1図に示すように、それぞれの美白剤の濃度が高くな
るにつれて、吸光度が落ちる傾向が見られ、吸光度が0.
2以下となるためのそれぞれの主成分の濃度は、以下の
通りとなった。
Results As shown in Fig. 1, as the concentration of each whitening agent increased, the absorbance tended to decrease, and the absorbance was 0.
The concentration of each main component to be 2 or less is as follows.

ヒノキチオール 200μmol/ アスコルビン酸 640μmol/ システイン 540μmol/ ホモシステイン 120μmol/ (実施例−2) 次に、美白剤としてホモシステイン,システイン又はア
スコルビン酸を主成分として、これにヒノキチオールを
40,80(μmol/)を加えたものについて波長475nmにお
ける吸光度を比較検討した。尚、美白剤の主成分として
使用するホモシステイン,システイン又はアスコルビン
酸の濃度は、それぞれ10,20,40,80(μmol/)とし
た。
Hinokitiol 200 μmol / ascorbic acid 640 μmol / cysteine 540 μmol / homocysteine 120 μmol / (Example-2) Next, homocysteine, cysteine or ascorbic acid as a whitening agent as a main component, and hinokitiol to this
The absorption of 40,80 (μmol /) was compared and examined at a wavelength of 475 nm. The concentrations of homocysteine, cysteine and ascorbic acid used as the main components of the whitening agent were 10, 20, 40 and 80 (μmol /), respectively.

試験方法は、実施例−1の試験方法と同じように、各美
白剤のリン酸緩衝液(pH6.8)を作成して分光光度計で
吸光度を測定した。
The test method was the same as the test method of Example-1, and a phosphate buffer (pH 6.8) of each whitening agent was prepared and the absorbance was measured with a spectrophotometer.

結 果 次の表−1及び第2図から第4図に示すようにいずれの
場合もヒノキチオールと組み合わせたものが、単独の場
合よりもメラニン色素の生成阻害作用を示したが特にホ
モシステインとヒノキチオールの組合わせのものが、シ
ステインとヒノキチオールの組合わせのものに比較して
顕著なメラニン色素の生成阻害作用を示した。すなわち
ヒノキチオール40μmol/であってもホモシステインの
場合は、配合料が40μmol/以上添加するだけで、メラ
ニン色素の生成阻害作用を示した。
Results As shown in Table 1 below and FIGS. 2 to 4, in each case, the combination with hinokitiol exhibited a melanin pigment production-inhibiting effect more than the case where it was used alone, but particularly homocysteine and hinokitiol were used. The combination of No. 2 and No. 3 showed a remarkable melanin pigment production inhibitory effect as compared with the combination of cysteine and hinokitiol. That is, even in the case of hinokitiol 40 μmol /, in the case of homocysteine, the production inhibitory effect of melanin pigment was exhibited only by adding the compounding ingredient at 40 μmol / or more.

尚、アスコルビン酸とヒノキチオールの組合わせのもの
も、それぞれ単独で用いたよりもメラニン色素の生成阻
害作用を示した。
In addition, the combination of ascorbic acid and hinokitiol also exhibited a melanin pigment production inhibitory action as compared with the case where they were used alone.

(実施例−3) 前記実施例で最も生成阻害作用に優れたホモシステイン
とヒノキチオールとの関係をより詳細に検討する為に表
−2に示す配合について、メラニン色素の生成阻害作用
について再度比較検討した。
(Example-3) In order to examine in more detail the relationship between homocysteine and hinokitiol, which have the most excellent production inhibiting action in the above examples, the formulations shown in Table-2 were compared and compared again for the production inhibiting action of melanin pigment. did.

枠内の100〜123の数字は、各美白剤の組合わせの番地を
表わす。
The numbers from 100 to 123 in the box indicate the address of the combination of each whitening agent.

試験方法は実施例−1及び実施例−2と同様に各濃度の
リン酸緩衝液を作成し、分光光度計により吸光度(475n
m)を測定した。
The test method was to prepare a phosphate buffer solution of each concentration in the same manner as in Example-1 and Example-2, and use a spectrophotometer to measure the absorbance (475 n
m) was measured.

結 果 表−3及び第2図に示すようにヒノキチオールが80μmo
l/の時が美白剤の相乗効果が最も大きいことが判明し
た。また、ホモシステインが10〜40μmol/であって
も、ヒノキチオールを40〜80μmol/配合することによ
り強いメラニン生成阻害作用を示すことが判明した。
Results As shown in Table 3 and Fig. 2, hinokitiol contained 80 μmo
It was found that the synergistic effect of the whitening agent was the largest at l /. It was also found that even if homocysteine was 10 to 40 μmol /, by adding hinokitiol 40 to 80 μmol /, a strong melanin production inhibitory effect was exhibited.

又、この実施例で得られた美白剤は安定性にも優れ、1
ケ月放置したものでも同様の美白効果を示した。
In addition, the whitening agent obtained in this example also has excellent stability.
The same whitening effect was exhibited even when left for a month.

効果 以上の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、ホモシステインとヒノキチオールとを組
み合わせることにより、それぞれ単独で用いた場合より
も相乗的な作用により従来より少ない量でメラニン色素
生成阻害作用を示す。
Effects As described above, the whitening agent according to the present invention has a smaller amount than conventional whitening agents due to a synergistic action by combining homocysteine and hinokitiol, compared to the case of using each alone. Shows an inhibitory effect on melanin pigment formation.

さらに従来のものよりも安定性に優れ、製品としての市
場性に優れている。
Furthermore, it is superior in stability to conventional products and has excellent marketability as a product.

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

第1図は、各美白剤の濃度とメラニン色素の生成阻害作
用を示す片対数グラフ,第2図はヒノキチオールとホモ
システインを組み合わせた場合のメラニン色素の生成阻
害作用に対する相乗効果を示す片対数グラフ,第3図は
ヒノキチオールとシステインとを組み合わせた場合のメ
ラニン色素の生成阻害作用に対する相乗効果を示す片対
数グラフ,第4図はヒノキチオールとアスコルビン酸と
を組み合わせた場合のメラニン色素の生成阻害作用に対
する相乗効果を示す片対数グラフである。
FIG. 1 is a semilogarithmic graph showing the concentration of each whitening agent and melanin pigment production inhibitory effect, and FIG. 2 is a semilogarithmic graph showing the synergistic effect on the melanin pigment production inhibitory effect when hinokitiol and homocysteine are combined. , FIG. 3 is a semilogarithmic graph showing the synergistic effect on the melanin pigment production inhibitory effect when hinokitiol and cysteine are combined, and FIG. 4 is the melanin pigment production inhibitory effect when hinokitiol and ascorbic acid are combined. It is a semi-logarithmic graph which shows a synergistic effect.

───────────────────────────────────────────────────── フロントページの続き (56)参考文献 特開 昭63−132812(JP,A) 特開 昭59−157009(JP,A) 特開 昭59−128320(JP,A) 特開 昭61−100509(JP,A) 化学大辞典編集委員会編「化学大辞典 7」共立出版株式会社(1987年2月15日発 行)P.486 ─────────────────────────────────────────────────── --- Continuation of the front page (56) Reference JP-A-63-132812 (JP, A) JP-A-59-157009 (JP, A) JP-A-59-128320 (JP, A) JP-A-61- 100509 (JP, A) "Chemical Encyclopedia 7" edited by the Editorial Committee for Chemistry, Kyoritsu Shuppan Co., Ltd. (Published February 15, 1987) 486

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とヒノキ
チオールとを主剤とする皮膚美白剤。
1. A skin whitening agent comprising homocysteine or its ester and hinokitiol as main ingredients.
【請求項2】ホモシステイン又はそのエステルを10μmo
l/以上含有しており、ヒノキチオールを40μmol/以
上含有していることを特徴とする特許請求の範囲第1項
記載の皮膚美白剤。
2. Homocysteine or its ester is added in an amount of 10 μmo.
The skin lightening agent according to claim 1, wherein the skin whitening agent contains 1 / or more and 40 μmol / or more of hinokitiol.
JP61303931A 1986-12-22 1986-12-22 Skin whitening agent Expired - Fee Related JPH0753654B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP61303931A JPH0753654B2 (en) 1986-12-22 1986-12-22 Skin whitening agent

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP61303931A JPH0753654B2 (en) 1986-12-22 1986-12-22 Skin whitening agent

Publications (2)

Publication Number Publication Date
JPS63156708A JPS63156708A (en) 1988-06-29
JPH0753654B2 true JPH0753654B2 (en) 1995-06-07

Family

ID=17927001

Family Applications (1)

Application Number Title Priority Date Filing Date
JP61303931A Expired - Fee Related JPH0753654B2 (en) 1986-12-22 1986-12-22 Skin whitening agent

Country Status (1)

Country Link
JP (1) JPH0753654B2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2602069B2 (en) * 1988-08-12 1997-04-23 株式会社資生堂 Cosmetics
CZ365996A3 (en) * 1994-06-15 1997-10-15 Procter & Gamble Use of mercapto derivatives for preparing pharmaceutical preparation for making lighter of skin
JP2005194203A (en) * 2003-12-26 2005-07-21 Dai Ichi Seiyaku Co Ltd Bleaching composition
KR100589716B1 (en) * 2004-01-20 2006-06-15 주식회사 웰스킨 Melanin production inhibitory composition
JP6241779B2 (en) * 2013-03-29 2017-12-06 株式会社ピカソ美化学研究所 Preservative and composition for external use, and coloring reduction method

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59128320A (en) * 1983-01-08 1984-07-24 Kanebo Ltd Lightening cosmetic
JPS59157009A (en) * 1983-02-25 1984-09-06 Yakurigaku Chuo Kenkyusho:Kk External skin drug for suppressing formation of melanin
JPS61100509A (en) * 1984-10-19 1986-05-19 Shizenbi Shiyouyaku Kk Gelatinous beautifying and whitening cosmetic

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
化学大辞典編集委員会編「化学大辞典7」共立出版株式会社(1987年2月15日発行)P.486

Also Published As

Publication number Publication date
JPS63156708A (en) 1988-06-29

Similar Documents

Publication Publication Date Title
CN113768818B (en) Whitening and anti-aging composition, cosmetic and preparation method thereof
RU2764769C2 (en) Products for external application with a two-phase system
HUT67820A (en) Cosmetic composition containing n-acetyl-l-cysteine as active ingredient and use thereof for regulating skin wrinkles and skin atrophy
FR2474864A1 (en) BUCCAL COMPOSITION USEFUL FOR THE TREATMENT OF GINGIVITY, BASED ON TRANS-4- (AMINOMETHYL) -CYCLOHEXANE-1-CARBOXYLIC ACID
JPS63316711A (en) Beautifying and whitening cosmetic
JPH0753654B2 (en) Skin whitening agent
JPS6416709A (en) Cosmetic containing extract of puerariae radix blended therein
JPH03275613A (en) Skin external agent
JP2004517857A (en) Whitening agent containing arbutin and glucosidase as active ingredients
JPH03153609A (en) Skin-beautifying cosmetic
JP2986262B2 (en) Whitening cosmetics
JPH1112117A (en) Cosmetic composition or pharmaceutical composition
JPH0245408A (en) Skin-beautifying cosmetic
JPS5716810A (en) Cosmetic
EP0801947B1 (en) Use of octopirox as skin depigmentation agent
JPS6270309A (en) Skin beautifying cosmetic
JPH10182404A (en) Preparation for external use for skin
JPS6236305A (en) Cosmetic
JPH0425249B2 (en)
JPS6219510A (en) Cosmetic
JPS60188306A (en) Cosmetic
ES2897401T3 (en) Composition comprising an antiseptic, a neutralizer of volatile sulfur compounds and an anticariogenic agent
CN1121850C (en) Use of unfermented honey as decolouring agent
JP3026616B2 (en) Whitening cosmetics
JPS62226910A (en) Skin cosmetic

Legal Events

Date Code Title Description
R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees