JP2937446B2 - Blackening agent to prevent gray hair - Google Patents

Blackening agent to prevent gray hair

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Publication number
JP2937446B2
JP2937446B2 JP24563390A JP24563390A JP2937446B2 JP 2937446 B2 JP2937446 B2 JP 2937446B2 JP 24563390 A JP24563390 A JP 24563390A JP 24563390 A JP24563390 A JP 24563390A JP 2937446 B2 JP2937446 B2 JP 2937446B2
Authority
JP
Japan
Prior art keywords
hair
blackening
effect
protein kinase
white hair
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
JP24563390A
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Japanese (ja)
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JPH04124122A (en
Inventor
憲寿 前田
實 福田
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Shiseido Co Ltd
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Shiseido Co Ltd
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Priority to JP24563390A priority Critical patent/JP2937446B2/en
Publication of JPH04124122A publication Critical patent/JPH04124122A/en
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Expired - Fee Related legal-status Critical Current

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Description

【発明の詳細な説明】 [産業上の利用分野] 本発明は白髪防止黒化剤、特に毛根の色素細胞を活性
化する成分の改良に関する。
Description: FIELD OF THE INVENTION The present invention relates to an improvement of an anti-whitening blackening agent, in particular, a component that activates pigment cells in hair roots.

[従来の技術] ヒト毛髪の白毛化は生理的老化の一現象であると共
に、円形脱毛症及びその他の皮膚疾患の一症侯としても
知られる。
[Background Art] Whitening of human hair is a phenomenon of physiological aging, and is also known as a symptom of alopecia areata and other skin diseases.

ところで、ヒト白毛化の機序は色素細胞系の種々の変
化による。
By the way, the mechanism of human whitening depends on various changes in the pigment cell line.

しかしながら、具体的な白髪発生機序については、19
65年にFitzpatrickらが毛母の色素細胞数の減少、チロ
シナーゼの減少、色素形成阻止物質の存在、チロシナー
ゼの活性部位の変化、表皮細胞へのメラニン顆粒の移動
の阻害、色素細胞母細胞の変化などの色素細胞系の変化
の可能性を示しているが、現在までに実証されているも
のは少ない。また毛のメラニン形成は毛の成長周期と共
に周期的に変化すること、老人性白毛毛母には色素細胞
が認められないことを、久木田らは示した。
However, regarding the specific mechanism of gray hair development, 19
In 1965, Fitzpatrick et al. Reduced the number of pigment cells in hair matrix, reduced tyrosinase, the presence of an inhibitor of pigment formation, altered the active site of tyrosinase, inhibited the transfer of melanin granules to epidermal cells, altered pigment cell mother cells Although there are potential changes in the pigment cell line such as these, few have been demonstrated to date. Hisagida and colleagues also showed that melanogenesis of hair changes periodically with the growth cycle of the hair and that pigment cells are not observed in senile gray hair mothers.

一方、ある種の疾患によって白毛が生じた場合には、
原因疾患の治療により毛髪の黒化が起こることがある。
On the other hand, if some disease causes white hair,
Treatment of the underlying disease may result in darkening of the hair.

[発明が解決しようとする課題] このように、白髪は毛母色素の欠如、活性の低下によ
り発生するが、その発生機序等については未だ不明な点
が多い。このため、白髪の防止あるいは黒化について
は、従来は対処療法的な対応が主体であり、毛母色素細
胞を十分に活性化させ、十分な白髪黒化効果を発揮させ
るという、根本的な対処は殆どなされていなかった。
[Problems to be Solved by the Invention] As described above, gray hair is generated due to a lack of hair matrix pigment and a decrease in activity, but there are still many unclear points about the mechanism of the generation. For this reason, in the past, prevention or blackening of gray hair has mainly been a countermeasure treatment, and a fundamental countermeasure of sufficiently activating hair matrix pigment cells and exerting a sufficient blackening effect on gray hair. Was almost never done.

本発明は前記従来技術の課題に鑑みなされたものであ
り、その目的は安全性が高く、しかも白髪防止効果、白
髪黒化効果に優れた白髪防止黒化剤を提供することにあ
る。
The present invention has been made in view of the above-mentioned problems of the prior art, and an object of the present invention is to provide a white hair preventing and blackening agent which has high safety and is excellent in a white hair preventing effect and a white hair blackening effect.

[課題を解決するための手段] 前記目的を達成するために本発明者らが鋭意検討した
結果、細胞内cAMP及びプロテインキナーゼCが白髪形成
の機作に極めて密接に関係していることを見出し、本発
明を完成するにいたった。
[Means for Solving the Problems] As a result of intensive studies by the present inventors to achieve the above object, it has been found that intracellular cAMP and protein kinase C are extremely closely related to the mechanism of gray hair formation. The present invention has been completed.

すなわち本出願の請求項1記載の白髪防止黒化剤は、
細胞内cAMPを増加させるcAMP増加剤のアデノシン、フォ
ルスコリン、ジブチリルcAMP、プロスタグランジンE1の
いずれか1種又は2種以上と、プロテインキナーゼC阻
害作用を有するプロテインキナーゼC阻害剤と、を配合
することを特徴とする。
That is, the blackening agent for preventing white hair according to claim 1 of the present application is:
One or more of adenosine, forskolin, dibutyryl cAMP, and prostaglandin E1, which are cAMP increasing agents that increase intracellular cAMP, and a protein kinase C inhibitor having a protein kinase C inhibitory action are blended. It is characterized by the following.

請求項2記載の白髪防止黒化剤は、プロテインキナー
ゼC阻害剤が、スタウロスポリン(staurosporine),
スフィンゴシン(sphingosine),フロレチン(phloret
in),フロリジン(phloridzin),ガングリオシド(go
nglioside),パルミトイルカルニチン(palmitoyl−DL
−carnitine),クエルセチン(quercetin),SOD(supe
roxidedismutase),ポリミキシンB(polymyxin B),
トリフルオペラジン(trifluoperazine),ビタミンD3
のいずれか1種又は2種以上であることを特徴とする。
The blackening agent for preventing gray hair according to claim 2, wherein the protein kinase C inhibitor is staurosporine,
Sphingosine, phloretin
in), phloridzin, ganglioside (go
nglioside), palmitoyl carnitine (palmitoyl-DL)
-Carnitine), quercetin, SOD (supe
roxidedismutase), polymyxin B,
Trifluoperazine, vitamin D 3
Or one or more of these.

以下、本発明について詳しく説明する。 Hereinafter, the present invention will be described in detail.

本発明で使用するcAMP増加剤のうち「ジブチリルcAM
P」(以下dbcAMPと略す。)は、ブクラデシンナトリウ
ムとも称されるcAMPのジブチル誘導体である。
Among the cAMP increasing agents used in the present invention, "dibutyryl cAM
"P" (hereinafter abbreviated as dbcAMP) is a dibutyl derivative of cAMP, also called bucladesin sodium.

本発明で使用するプロテインキナーゼC阻害剤は請求
項記載の薬剤に限定されるものではなく、このような使
用を有する物は本発明に適用可能である。
The protein kinase C inhibitor used in the present invention is not limited to the drugs described in the claims, and those having such uses are applicable to the present invention.

プロテインキナーゼCとは、細胞膜イノシトールリン
脂質代謝が細胞膜受容体特異的に活性化されたときに生
ずる二次伝達物質、ジアシルグリセロールによって活性
化されるタンパク質リン酸化酵素である。このプロテイ
ンキナーゼCの活性を抑制することによって色素細胞の
メラニン生成を活性化することができる。さらに細胞内
cAMPを増加させる薬剤と併用することによって、相乗的
に作用を増強することができる。
Protein kinase C is a protein kinase that is activated by diacylglycerol, a secondary messenger produced when cell membrane inositol phospholipid metabolism is activated specifically to cell membrane receptors. By suppressing the activity of protein kinase C, melanin production of pigment cells can be activated. More intracellular
When used in combination with an agent that increases cAMP, the action can be synergistically enhanced.

cAMP増加剤あるいはプロテインキナーゼC阻害剤は、
皮膚外用剤として用いる場合にはその全量中に0.001〜5
0重量%配合すればよく、好ましくは0.1〜10重量%であ
る。0.001重量%より少ない量では十分な効果が得られ
ず、50重量%より多く配合しても必要以上の効果は上が
らない。
cAMP enhancers or protein kinase C inhibitors
When used as an external preparation for skin, 0.001 to 5
0 wt% may be blended, and preferably 0.1 to 10 wt%. If the amount is less than 0.001% by weight, a sufficient effect cannot be obtained, and if the amount is more than 50% by weight, the effect is not increased more than necessary.

本発明を皮膚外用剤として用いる場合、請求項記載の
必須成分の他に現行の白髪防止作用を有する薬剤、保湿
作用を有する薬剤など通常の医薬品、化粧品や医薬部外
品等の皮膚化粧料に用いられている薬剤及び製剤上許容
し得る基材との混合物として使用に供することができ
る。
When the present invention is used as an external preparation for skin, in addition to the essential components described in the claims, the present pharmaceuticals having an effect of preventing gray hair, agents having a moisturizing effect, ordinary skincare products such as cosmetics and quasi-drugs. It can be used as a mixture with the drug being used and a pharmaceutically acceptable substrate.

特に発毛を促進する薬剤として、ジアゾキシド、ミノ
キシジル、ビタミンB2,ビタミンB6,ビタミンB12,葉酸,
パラアミノ安息香酸,ビタミンD3,エチニルニストラジ
オール,海藻抽出物,黒胡麻抽出物,あるいは紫外線吸
収剤を配合すると一層、効果的である。
In particular, diazoxide, minoxidil, vitamin B 2 , vitamin B 6 , vitamin B 12 , folic acid,
It is more effective to add paraaminobenzoic acid, vitamin D 3 , ethinyl nistradiol, seaweed extract, black sesame extract, or ultraviolet absorber.

上記した基材としては、賦形剤,結合剤,滑沢剤,崩
壊剤,界面活性剤,緩衝剤,保存剤,香料,色素,油
分,顔料,水,アルコール,増粘剤,防腐剤,酸化防止
剤,キレート剤が挙げられ、これらは1種または2種以
上混合して使用される。但し、これらに限定するもので
はない。
The above-mentioned base materials include excipients, binders, lubricants, disintegrants, surfactants, buffers, preservatives, fragrances, pigments, oils, pigments, water, alcohols, thickeners, preservatives, Examples thereof include an antioxidant and a chelating agent, and these are used alone or in combination of two or more. However, it is not limited to these.

本発明の剤型は、皮膚外用剤として用いる場合には、
この薬効を得るのに適したものであれば通常の医薬品,
化粧品,医薬部外品等に用いられる任意の形態が使用で
き、例えばローション,リニメント,水溶液,乳液等の
外用液剤,パウダー,溶解錠等の外用固形剤、及びクリ
ーム,皮膜剤,軟膏,ゼリー等の外用半固形剤,石鹸等
が挙げられる。
When the dosage form of the present invention is used as an external preparation for skin,
Ordinary medicines that are suitable for obtaining this medicinal effect,
Any form used for cosmetics, quasi-drugs, etc. can be used, for example, external preparations such as lotions, liniments, aqueous solutions and emulsions, solid preparations for external use such as powders and dissolving tablets, and creams, coatings, ointments, jellies, etc. External semi-solid agents, soaps and the like.

なお内服剤,注射剤等でも効果が得られることがあ
り、いくつかの方法を併用しても良い。
In addition, an effect may be obtained with an internal medicine, an injection, and the like, and some methods may be used in combination.

[発明の効果] 以上説明したように、本発明にかかる白髪防止黒化剤
は、cAMP増加剤及びプロテインキナーゼC阻害剤の相乗
作用により優れた白髪防止効果、白髪黒化効果を奏す
る。
[Effects of the Invention] As described above, the gray hair preventing / blackening agent according to the present invention exerts an excellent white hair preventing effect and a white hair darkening effect due to the synergistic action of the cAMP increasing agent and the protein kinase C inhibitor.

[実施例] 次に実施例を挙げて本発明をさらに詳細に説明する。
本発明はこれにより限定されるものではない。配合量は
重量%である。
EXAMPLES Next, the present invention will be described in more detail with reference to examples.
The present invention is not limited by this. The compounding amount is% by weight.

まず、白髪防止黒化効果の評価方法について説明す
る。白髪防止黒化効果は、累積塗布による白髪発生防止
及び白髪黒化効果から評価した。
First, a method for evaluating the blackening effect of preventing white hair will be described. The whitening prevention and blackening effect was evaluated based on the prevention of whitening and the blackening effect by cumulative application.

累積塗布による白髪防止効果 (試験方法) 本発明の有効成分を配合したローションを毎日塗布し
ながら、黒色マウスにストレスを与える。白毛の発生を
防止する割合を白髪防止度(%)として計測し、白髪防
止効果として評価した。
Effect of Preventing Gray Hair by Cumulative Application (Test Method) While applying a lotion containing the active ingredient of the present invention daily, a black mouse is stressed. The ratio of preventing the generation of white hair was measured as the degree of white hair prevention (%) and evaluated as the white hair preventing effect.

(判定基準) ◎ 著効 :白髪防止度が20%以上 ○ 有効 :白髪防止度が20%未満10%以上 △ やや有効:白髪防止度が10%未満 × 無効 :白髪防止度が0% 累積塗布による白髪黒化効果 (試験方法) 黒色マウスにストレスの与えて、白毛を発生させ、本
発明の有効成分を配合したローションを、白毛発生部位
に毎日塗布して、全白毛数に対する黒毛数の割合を白髪
黒化度(%)として測定し、白髪黒化効果として評価し
た。
(Judgment criteria) ◎ Significant effect: The degree of prevention of white hair is 20% or more ○ Effective: The degree of prevention of white hair is less than 20% 10% or more △ Somewhat effective: The degree of prevention of white hair is less than 10% × Invalid: The degree of prevention of white hair is 0% Cumulative application (Determination of black hair by applying stress to black mice to generate white hair and applying a lotion containing the active ingredient of the present invention daily to the site where white hair is generated. The ratio of the numbers was measured as the degree of blackening of white hair (%), and evaluated as the blackening effect of white hair.

(判定基準) ◎ 著効 :白髪黒化度が20%以上 ○ 有効 :白髪黒化度が20%未満10%以上 △ やや有効:白髪黒化度が10%未満 × 無効 :白髪黒化度が0% 次の配合組成により各種白髪防止黒化ローションを調
整し、その累積塗布による白髪黒化効果について調べ
た。
(Judgment criteria) ◎ Significant effect: Degree of darkening of gray hair is 20% or more ○ Effective: Degree of darkening of gray hair is less than 20% 10% or more △ Somewhat effective: Degree of darkening of white hair is less than 10% × Invalid: Degree of darkening of white hair 0% Various types of whitening preventing blackening lotions were prepared according to the following composition, and the blackening effect of the cumulative whitening was examined.

配合 重量% 被験物質 1.0 95%エチルアルコール 10.0 POE(20)ラウリルエーテル 0.5 香料 適 量 プロピレングリコール 1.0 グリセリン 2.0 蒸留水 残 余 100% <製法> 95%エチルアルコールに、POE(20)ラウリルエーテ
ル及び香料を混合し、次いでこの中に、後述する各種被
験物質を配合する。そして、プロピレングリコールとグ
リセリンの混合物を加え、さらに、蒸留水を全量100gに
なるように必要量添加した。
Formulation Weight% Test substance 1.0 95% Ethyl alcohol 10.0 POE (20) lauryl ether 0.5 Perfume Appropriate amount Propylene glycol 1.0 Glycerin 2.0 Distilled water Residual 100% <Production method> POE (20) lauryl ether and perfume are added to 95% ethyl alcohol. After mixing, various test substances to be described later are mixed therein. Then, a mixture of propylene glycol and glycerin was added, and further, distilled water was added in a required amount so that the total amount became 100 g.

次の表−1はcAMP増加剤、プロテインキナーゼC阻害
剤を各単独で配合した場合の白髪防止度、白髪黒化度を
示す。
The following Table 1 shows the degree of prevention of gray hair and the degree of blackening of gray hair when each of the cAMP increasing agent and the protein kinase C inhibitor is used alone.

上記表−1より明らかなように、アデノシン、フォル
スコリン、dbcAMPはそれぞれ単独でも白髪防止効果、白
髪黒化効果は有するものの、さほど顕著ではない。
As is clear from Table 1, adenosine, forskolin, and dbcAMP each have an effect of preventing gray hair and an effect of blackening gray hair, but are not so remarkable.

次の表−2はcAMP増加剤としてアデノシンを選択し、
プロテインキナーゼC阻害剤を各種変更した場合の白髪
防止効果、白髪黒化効果を示す。なお、cAMP増加剤、プ
ロテインキナーゼC阻害剤は0.5重量%づつ配合した。
Table 2 below selects adenosine as a cAMP increasing agent,
Fig. 3 shows the gray hair preventing effect and the gray hair darkening effect when various changes are made to the protein kinase C inhibitor. In addition, the cAMP increasing agent and the protein kinase C inhibitor were added at 0.5% by weight.

上記表−2から明らかなように、白髪防止度、白髪黒
化度いずれも改善され、cAMP増強剤、プロテインキナー
ゼC阻害剤は相乗作用により優れた白髪防止黒化作用を
有することが理解される。
As is evident from Table 2, both the degree of white hair prevention and the degree of blackening of the white hair are improved, and it is understood that the cAMP enhancer and the protein kinase C inhibitor have an excellent white hair preventing and blackening action due to the synergistic action. .

次の表−3はcAMP増加剤としてフォルスコリンを選択
し、プロテインキナーゼC阻害剤を各種変更した場合の
白髪防止効果、白髪黒化効果を示す。なお、cAMP増加剤
プロテインキナーゼC阻害剤は0.5重量%づつ配合し
た。
The following Table 3 shows the effect of preventing gray hair and the effect of darkening gray hair when forskolin was selected as a cAMP increasing agent and the protein kinase C inhibitor was variously changed. The cAMP increasing protein kinase C inhibitor was added at 0.5% by weight.

上記表−3から明らかなように、フォルスコリンにつ
いても各種プロテインキナーゼC阻害剤との相乗作用が
認められる。
As is clear from Table 3 above, synergistic effect of forskolin with various protein kinase C inhibitors is also observed.

次の表−4はcAMP増加剤としてdbcAMPを選択し、プロ
テインキナーゼC阻害剤を各種変更した場合の白髪防止
効果、白髪黒化効果を示す。なお、cAMP増加剤、プロテ
インキナーゼC阻害剤は0.5重量%づつ配合した。
Table 4 below shows dbcAMP as a cAMP increasing agent, and shows the effect of preventing and graying gray hair when various changes are made to the protein kinase C inhibitor. In addition, the cAMP increasing agent and the protein kinase C inhibitor were added at 0.5% by weight.

dbcAMPについてもプロテインキナーゼ阻害剤との相乗
作用が認められ、特にスフィンゴシン、スタウロスポリ
ンとの相乗作用により白髪黒化作用が顕著に向上する。
Synergism with dbkAMP is also observed with protein kinase inhibitors. In particular, synergism with sphingosine and staurosporine significantly improves the blackening effect of gray hair.

以上の各実施例から明らかなように、本発明の皮膚外
用剤はcAMP増加剤とプロテインキナーゼC阻害剤との相
乗作用により、白髪防止黒化効果に優れることが確認で
きた。
As is clear from the above Examples, it was confirmed that the external preparation for skin of the present invention was excellent in the effect of preventing and blackening gray hair due to the synergistic action of the cAMP increasing agent and the protein kinase C inhibitor.

本剤は、白髪に著効であり、かつ長期連用に耐える安
全性の高い白髪治療、白髪防止化粧料である。
The agent is a highly safe gray hair treatment and gray hair prevention cosmetic that is extremely effective for gray hair and can withstand long-term use.

次に本発明にかかる白髪防止黒化剤のより具体的な配
合例についてその効果とともに説明する。
Next, more specific examples of the compounding of the blackening agent for preventing white hair according to the present invention will be described together with their effects.

実施例1 ヘアトニック 次の処方により、常法に従って0.5%dbcAMPと0.5%SO
Dを配合した白髪防止黒化ヘアトニック、及びdbcAMP1.0
%のみを配合したヘアトニックを製造した。
Example 1 Hair Tonic According to the following formulation, 0.5% dbcAMP and 0.5% SO were used according to a conventional method.
Prevents whitening blackening hair tonic with D, and dbcAMP1.0
% To produce a hair tonic.

(アルコール相) 重量% 95%エチルアルコール 10.0 ポリオキシエチレン硬化ヒマシ油 2.0 プロピレングリコール 4.0 オレイルアルコール 0.1 L−メントール 0.1 dbcAMP 0.5 SOD 0.5 (水相) イオン交換水 残 余 紫外線吸収剤 適 量グリセリン 5.0 100.0 <製法> 水相、アルコール相を調整後可溶化する。(Alcohol phase) Weight% 95% Ethyl alcohol 10.0 Polyoxyethylene hydrogenated castor oil 2.0 Propylene glycol 4.0 Oleyl alcohol 0.1 L-menthol 0.1 dbcAMP 0.5 SOD 0.5 (Aqueous phase) Ion-exchange water Residual UV absorber Appropriate amount of glycerin 5.0 100.0 < Production method> After adjusting the aqueous phase and alcohol phase, solubilize.

上記白髪防止黒化ヘアトニックを白髪のある20名の男
性(40〜60歳)に1日2回、3ヵ月間、本発明品と比較
例を各々左右頭皮に別々に使用させ、塗布部位の頭髪を
試験前後で比較し、白髪防止効果、白髪黒化効果を判定
した。結果を次に示す。
Twenty men (40-60 years old) with gray hair were allowed to use the product of the present invention and the comparative example separately on the left and right scalp twice a day for three months, respectively, using the above-mentioned black hair preventing black tonic. The hair was compared before and after the test, and the effect of preventing white hair and the effect of blackening white hair were determined. The results are shown below.

(結果) 被験物質 白髪防止度 白髪黒化度 dbcAMP(比較例) ○ ○ dbcAMP+SOD ◎ ◎ 実施例2 乳液 次の処方により、常法に従って0.5%dbcAMPと0.5%パ
ルミトイルカルニチンを配合した白髪防止黒化乳液及び
dbcAMP1.0%のみを配合した乳液を製造した。
(Results) Test substance Degree of prevention of gray hair Degree of blackening of white hair dbcAMP (Comparative Example) ○ ○ dbcAMP + SOD ◎ ◎ ◎ Example 2 Emulsion According to the following formula, 0.5% dbcAMP and 0.5% palmitoylcarnitine were blended according to a conventional method. as well as
An emulsion containing only 1.0% of dbcAMP was produced.

配 合 重量% ステアリン酸 2.5 セチルアルコール 1.5 ワセリン 5.0 流動パラフィン 10.0 ポリオキシエチレン(10モル) モノオレイン酸エステル 2.0 ポリエチレングリコール1500 3.0 トリエタノールアミン 1.0 エスクレチン 1.0 dbcAMP 0.5 パルミトイルカルニチン 0.5 イオン交換水 残 余 香料 適 量防腐剤・酸化防止剤 適 量 100.0 <製法> イオン交換水にポリエチレングリコール1500とトリエ
タノールアミンを加え、加熱溶解して70℃に保つ(水
相)。他の成分を混合し加熱融解して70℃に保つ(油
相)。水相に油相を加え予備乳化を行ない、ホモミキサ
ーで均一に乳化し、乳化後よくかきまぜながら30℃まで
冷却する。
Composition Weight% Stearic acid 2.5 Cetyl alcohol 1.5 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) Monooleate 2.0 Polyethylene glycol 1500 3.0 Triethanolamine 1.0 Esculetin 1.0 dbcAMP 0.5 Palmitoylcarnitine 0.5 Ion-exchange water Residual perfume Appropriate amount Preservative / antioxidant qs 100.0 <Production method> Add polyethylene glycol 1500 and triethanolamine to ion-exchanged water, dissolve by heating and maintain at 70 ° C (aqueous phase). Mix the other ingredients, heat and melt to keep at 70 ° C (oil phase). The oil phase is added to the water phase, pre-emulsification is performed, and the mixture is uniformly emulsified with a homomixer. After the emulsification, the mixture is cooled to 30 ° C. while stirring well.

上記白髪防止黒化乳液を白髪のある20名の男性(40〜
60歳)に1日2回、3ヵ月間、本発明品と比較例を各々
左右頭皮に別々に使用させ、塗布部位の頭髪を試験前後
で比較し、白髪防止効果、白髪黒化効果を判定した。結
果を次に示す。
The above whitening prevention blackening emulsion was applied to 20 men with white hair (40 ~
(60 years old) twice a day for 3 months, using the product of the present invention and the comparative example separately on the left and right scalp, comparing the hair at the application site before and after the test to determine the whitening prevention effect and blackening effect did. The results are shown below.

(結果) 被験物質 白髪防止度 白髪黒化度 dbcAMP(比較例) ○ ○ dbcAMP +パルミトイル カルニチン ◎ ◎ 実施例3 ヘアクリーム 次の処方により、常法に従って0.5%dbcAMPと0.5%フ
ロレチンを配合した白髪防止黒化ヘアクリーム、及びdb
cAMP1.0%のみを配合した乳液を製造した。
(Results) Test substance Degree of prevention of white hair Degree of blackening of white hair dbcAMP (Comparative Example) ○ ○ dbcAMP + palmitoyl carnitine ◎ ◎ Example 3 Hair Cream According to the following formulation, white hair prevention formulated with 0.5% dbcAMP and 0.5% phloretin according to a conventional method. Blackening hair cream and db
An emulsion containing only cAMP 1.0% was produced.

配 合 重量% ステアリルアルコール 7.0 ステアリン酸 2.0 水添ラノリン 2.0 スクワラン 5.0 2−オクチルドテシルアルコール 6.0 ポリオキシエチレン(25モル) セチルアルコールエーテル 3.0 グリセリンモノステアリン酸エステル 2.0 プロピレングリコール 5.0 dbcAMP 0.5 フロレチン 0.5 香料 適 量 防腐剤・酸化防止剤 適 量イオン交換水 残 余 100.0 <製法> イオン交換水にプロピレングリコール及びdbcAMP,フ
ロレチンを加え加熱して70℃に保つ(水相)。他の成分
を混合し加熱溶解して70℃に保つ(油相)。水相に油相
を加え予備乳化を行ない、ホモミキサーで均一に乳化し
た後、よくかきまぜながら30℃まで冷却する。
Weight% Stearyl alcohol 7.0 Stearic acid 2.0 Hydrogenated lanolin 2.0 Squalane 5.0 2-Octyldotesyl alcohol 6.0 Polyoxyethylene (25 mol) Cetyl alcohol ether 3.0 Glycerin monostearate 2.0 Propylene glycol 5.0 dbcAMP 0.5 Phloretin 0.5 Perfume Preservative / Antioxidant Appropriate amount of ion-exchanged water Residual 100.0 <Production method> Add propylene glycol, dbcAMP and phloretin to ion-exchanged water and heat to 70 ° C (aqueous phase). Mix and heat other components and keep at 70 ° C (oil phase). The oil phase is added to the water phase, pre-emulsification is carried out, and after uniform emulsification with a homomixer, the mixture is cooled to 30 ° C. while stirring well.

上記白髪防止黒化乳液を白髪のある20名の男性(40〜
60歳)に1日2回、3ヵ月間、本発明品と比較例を各々
左右頭皮に別々に使用させ、塗布部位の頭髪を試験前後
で比較し、白髪防止効果、白髪黒化効果を判定した。結
果を次に示す。
The above whitening prevention blackening emulsion was applied to 20 men with white hair (40 ~
(60 years old) twice a day for 3 months, using the product of the present invention and the comparative example separately on the left and right scalp, comparing the hair at the application site before and after the test to determine the whitening prevention effect and blackening effect did. The results are shown below.

(結果) 被験物質 白髪防止度 白髪黒化度 dbcAMP(比較例) ○ ○ dbcAMP +フロレチン ◎ ◎ 実施例1,2,3の結果から、cAMP増加剤と、プロテイン
キナーゼC阻害剤の1種または2種以上を各々同時に有
効成分として配合することを特徴とする白髪防止黒化剤
は、細胞内cAMPを増加させる薬剤群から選ばれた1種ま
たは2種以上を配合したものより、顕著な白髪防止効
果、白髪黒化効果を示すことがわかった。
(Results) Test substance Degree of prevention of white hair Degree of darkening of white hair dbcAMP (Comparative Example) ○ ○ dbcAMP + phloretin ◎ ◎ From the results of Examples 1, 2 and 3, one or two of cAMP increasing agent and protein kinase C inhibitor A whitening-preventing blackening agent characterized in that at least one kind is simultaneously formulated as an active ingredient, is more effective than one containing at least one selected from a group of drugs that increase intracellular cAMP. The effect and the blackening effect of the gray hair were shown.

なお、上記白髪防止黒化剤は3ヵ月間の使用中及び使
用後において、皮膚に異常な症状は認められなかった。
In addition, no abnormal symptom was recognized on the skin during and after use of the above-mentioned whitening preventing blackening agent for 3 months.

───────────────────────────────────────────────────── フロントページの続き (56)参考文献 特開 平2−108636(JP,A) 特開 昭64−79107(JP,A) 特開 平2−273610(JP,A) 特開 昭62−45527(JP,A) 特開 平1−316308(JP,A) (58)調査した分野(Int.Cl.6,DB名) A61K 7/00 - 7/50 ──────────────────────────────────────────────────続 き Continuation of the front page (56) References JP-A-2-108636 (JP, A) JP-A-64-79107 (JP, A) JP-A-2-273610 (JP, A) JP-A 62-79 45527 (JP, A) JP-A-1-316308 (JP, A) (58) Fields investigated (Int. Cl. 6 , DB name) A61K 7/00-7/50

Claims (2)

(57)【特許請求の範囲】(57) [Claims] 【請求項1】細胞内のcAMPを増加させるcAMP増加剤のア
デノシン、フォルスコリン、ジブチリルcAMP、プロスタ
グランジンE1のいずれか1種又は2種以上と、 プロテインキナーゼC阻害作用を有するプロテインキナ
ーゼC阻害剤と、 を配合することを特徴とする白髪防止黒化剤。
1. Inhibition of protein kinase C having one or more of adenosine, forskolin, dibutyryl cAMP and prostaglandin E1, which are cAMP increasing agents for increasing intracellular cAMP, and a protein kinase C inhibitory action A blackening agent for preventing white hair, comprising:
【請求項2】請求項1記載の白髪防止黒化剤において、
プロテインキナーゼC阻害剤は、スタウロスポリン、ス
フィンゴシン、ガングリオシド、フロレチン、フロリジ
ン、パルミトイルカルニチン、クエルセチン、SOD、ポ
リミキシンB、トリフルオペラジン、ビタミンD3のいず
れか1種又は2種以上であることを特徴とする白髪防止
黒化剤。
2. The blackening agent for preventing white hair according to claim 1,
Protein kinase C inhibitors, characterized staurosporine, sphingosine, gangliosides, phloretin, phlorizin, palmitoyl carnitine, quercetin, SOD, polymyxin B, trifluoperazine, that either one or more vitamins D 3 Blackening agent to prevent white hair.
JP24563390A 1990-09-14 1990-09-14 Blackening agent to prevent gray hair Expired - Fee Related JP2937446B2 (en)

Priority Applications (1)

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Application Number Priority Date Filing Date Title
JP24563390A JP2937446B2 (en) 1990-09-14 1990-09-14 Blackening agent to prevent gray hair

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JPH04124122A JPH04124122A (en) 1992-04-24
JP2937446B2 true JP2937446B2 (en) 1999-08-23

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4139921A1 (en) * 1991-12-04 1993-06-09 Wella Ag, 6100 Darmstadt, De USE OF RADICAL CATCHERS AND / OR SUBSTANCES SUITABLE FOR THE DEACTIVATION OF NON-RADICAL, REACTIVE OXYGEN SPECIES TO PREVENT OR DELAY THE GRAYING OF HUMAN HAIR
EP0711558A1 (en) * 1994-10-21 1996-05-15 Unilever Plc Compositions for topical application to skin, hair and nails
EP0711541A1 (en) * 1994-11-11 1996-05-15 Harry H. Leveen Use of glucose blockers for inhibiting hair growth
FR2729296B1 (en) * 1995-01-12 1997-03-28 Europlanaire PHARMACEUTICAL COMPOSITIONS COMPRISING A SUPEROXIDE DISMUTASE
KR100499190B1 (en) * 1996-03-29 2006-04-17 교와 핫꼬 고교 가부시끼가이샤 Hair restorer
US7795246B2 (en) 1998-08-06 2010-09-14 Cephalon, Inc. Particle-forming compositions containing fused pyrrolocarbazoles
US6200968B1 (en) * 1998-08-06 2001-03-13 Cephalon, Inc. Particle-forming compositions containing fused pyrrolocarbazoles
FR2812192B1 (en) * 2000-07-28 2003-01-31 Oreal USE OF PROSTAGLANDIN EP-3 RECEPTOR ANTAGONISTS AS A COSMETIC AGENT FOR MITIGATING, REDUCING OR STOPPING HAIR AND HAIR LOSS
FR2812190B1 (en) * 2000-07-28 2003-01-31 Oreal USE OF NON-PROSTANOIC AGONISTS OF EP-2 AND / OR EP-4 PROSTAGLANDIN RECEPTORS AS A COSMETIC AGENT FOR MITIGATING, DECREASING OR STOPPING HAIR AND HAIR LOSS
FR2840531B1 (en) * 2002-06-11 2004-10-29 Oreal COSMETIC COMPOSITION COMPRISING A MIMETIC AGENT FOR THE ACTIVITY OF DOPACHROME TAUTOMERASE (TRP-2) FOR COMBATING CANITIS
WO2003103616A2 (en) * 2002-06-11 2003-12-18 L'oreal Use of an agent mimicking dopachrome tautomerase (trp-2) activity as protective agent for hair follicle melanocytes and uses thereof
JP2006111544A (en) * 2004-10-13 2006-04-27 Shiseido Co Ltd Anti-white hair agent
JP5596251B2 (en) * 2005-10-14 2014-09-24 丸善製薬株式会社 Skin cosmetics and hair cosmetics
US20090325857A1 (en) * 2006-04-21 2009-12-31 Raphael Beumer Use of opioid receptor antagonists
JP5836666B2 (en) * 2011-06-28 2015-12-24 日華化学株式会社 MITF-M production promoter, hair cosmetic composition and skin cosmetic composition containing the MITF-M production promoter
JP2012092138A (en) * 2011-12-27 2012-05-17 Maruzen Pharmaceut Co Ltd Skin cosmetic and hair cosmetic
US20240285501A1 (en) * 2021-06-19 2024-08-29 Adjuvant Holdings Co., Ltd. Hair growth agent

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