JPS5988409A - Hair tonic - Google Patents

Hair tonic

Info

Publication number
JPS5988409A
JPS5988409A JP19829582A JP19829582A JPS5988409A JP S5988409 A JPS5988409 A JP S5988409A JP 19829582 A JP19829582 A JP 19829582A JP 19829582 A JP19829582 A JP 19829582A JP S5988409 A JPS5988409 A JP S5988409A
Authority
JP
Japan
Prior art keywords
hair
effect
hair tonic
compound
deoxycorticosterone
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.)
Pending
Application number
JP19829582A
Other languages
Japanese (ja)
Inventor
Makoto Uzuka
宇塚 誠
Yoichi Oota
陽一 太田
Shinichi Hirama
平間 伸一
Toshio Nishiyama
西山 敏夫
Kenichi Tomita
健一 富田
Keisuke Nakajima
啓介 中嶋
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shiseido Co Ltd
Original Assignee
Shiseido Co Ltd
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 Shiseido Co Ltd filed Critical Shiseido Co Ltd
Priority to JP19829582A priority Critical patent/JPS5988409A/en
Publication of JPS5988409A publication Critical patent/JPS5988409A/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00Preparations for affecting hair growth

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)
  • Cosmetics (AREA)

Abstract

PURPOSE:To provide a hair tonic free from undesirable side effects such as the action of hormone, etc, and having excellent hair tonic effect, by using a deoxycorticosterone compound as a component. CONSTITUTION:The deoxycorticosterone compound of formula (R is H or 2-11C acyl) is compounded in a hair tonic in an amount of 0.0001-1wt%. The compound has the effect to inhibit the testosterone-5alpha-reductase activity as well as the effect to inhibit the bonding of 5alpha-dihydrotestosterone with receptor protein, and is effective to mitigate or prevent the male baldness and alopecia.

Description

【発明の詳細な説明】 本発明はホルモン作用等の好ましくない副作用を有さす
、かつ優れた養毛効果をもっ養毛料に関する〇 男性型の禿頭や脂漏などの生理学上の徴候は、男性ホル
モンの過剰苦情に基づく男性ホルモン刺激の増大による
と言われているが一最近、毛根1皮脂腺等の器官におけ
るこの男性ホルモン活性の本体はへこれら標的器官にお
いてテストステロンがテストステロン−6α−レダクタ
ーゼという名の酵素(以下、レダクターゼと略す、)に
よって還元された5α−ジヒドロテストステロン(以下
、5α−DHTと略す。)であることが周知となってき
ている。即ち、畢丸や副腎で作られたテストステロン(
男性ホルモン)は血流にのって皮脂腺に行き、皮脂腺細
胞の中にあるレダクターゼによって、より強力な男性ホ
ルモンである5α−DHTに変換される・この6α−D
HTは細胞内の受容体と結合し、核に働いて皮脂腺細胞
の増殖を促す一方、それ自体が皮脂腺細■3外に出て血
流にのり、毛母の細胞に働き毛球部の毛母細胞の分裂を
抑制し、毛の成長を妨げるものとされている。
DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a hair nourishing agent that does not have undesirable side effects such as hormonal effects and has an excellent hair nourishing effect.Physiological symptoms such as male pattern baldness and seborrhea are caused by the It is said that this is due to increased stimulation of androgens due to excessive complaints of men, but recently it has been revealed that the main body of this androgen activity in organs such as hair roots and sebaceous glands has changed. It has become well known that 5α-dihydrotestosterone (hereinafter abbreviated as 5α-DHT) is reduced by 5α-dihydrotestosterone (hereinafter abbreviated as 5α-DHT). In other words, testosterone (
The male hormone) travels through the bloodstream to the sebaceous glands, where it is converted into the more powerful male hormone 5α-DHT by reductase in the sebaceous gland cells.This 6α-D
HT binds to intracellular receptors and acts on the nucleus to promote the proliferation of sebaceous gland cells, while HT itself exits the sebaceous gland cells and enters the bloodstream, acting on hair matrix cells and stimulating the growth of hair in the hair bulb. It is said to suppress the division of mother cells and prevent hair growth.

従って、男性型の禿や脱毛などの徴候は、レダクターゼ
の活性を阻害すること、および5α−DHTと受容体タ
ンパクとの結合を阻害することにより低減または防止す
ることができると考えられ、この観点に基づいてこれま
でにいくっがの物質が見い出されている。しかし、これ
らの物質はレダクターゼ活性の阻害率は大きくても好ま
しくない副作用があったり、5α−DHTと受容体タン
パクとの結合阻害率が非常に低かったりして、実質上の
養毛効果に劣るという欠点があった。
Therefore, it is thought that symptoms such as male pattern baldness and hair loss can be reduced or prevented by inhibiting the activity of reductase and the binding of 5α-DHT to receptor proteins; So far, a number of substances have been discovered based on this. However, even though these substances have a high inhibition rate of reductase activity, they have undesirable side effects, and their inhibition rate of binding between 5α-DHT and receptor protein is very low, so they are inferior to the actual hair growth effect. There was a drawback.

本発明者らは、上記事情に鑑み、ホルモン作用等の好ま
しくない副作用を持たず、安全で、かつレダクターゼ活
性の阻害と、5α−D II Tと受容体タンパクとの
結合阻害の両方の効果を併せ持つ物質を探究し、これを
配合するとにより養毛効果の優れた養毛料を得るべく鋭
意研究を重ねた結果、アンドロステンジオンが上記目的
を達成することを見い出し、この知見にもとづいて本発
明を完成するに致った。
In view of the above circumstances, the present inventors have developed a method that does not have undesirable side effects such as hormonal effects, is safe, and has the effect of inhibiting both reductase activity and binding of 5α-D II T to receptor protein. As a result of intensive research in search of substances that have the same properties and in order to obtain a hair nourishing agent with excellent hair nourishing effects by blending them, it was discovered that androstenedione achieves the above object, and based on this knowledge, the present invention was developed. It was completed.

(以下余白) すなわち本発明は上記一般式 ) で表わされるテ1ギシコルチコステロン系1ヒ合物のう
ち]種スζ」2種以上を配合してなる養し1′1である
(Hereinafter in the margin) That is, the present invention is a nutritional supplement 1'1 which is a mixture of two or more types of ``species ζ'' among the ``gicicorticosterone compound'' represented by the above general formula.

以I:、本発明のtj1′t+Jすについて、11述す
る。
Hereinafter, tj1't+J of the present invention will be described in 11.

本発明に用いるデオギノコ?レチコス70ン(以F、]
)O(j Sと略す。)系化合物は、rjij記−・般
式の1シが水素、又は炭素数2〜」jのアンノ[、Jl
l、(1rJ鎖飽和の他、小飽和、分岐、芳占環等もa
む)のものである◇具体例としては、l(が水素の時の
])OOS、アシルノ^の時のI)OOSアセブート、
+10 !’ Sプロピオネ−1・、I)OCSヘンシ
ェード等があげちれ、このうち、1種又は2挿具−にが
配合される。配合喰は0.0001〜1屯lit%程度
である。
Deoginoko used in the present invention? Reticos 70n (F, hereafter)
) O (abbreviated as S) type compounds are represented by rjij-, where 1 of the general formula is hydrogen, or where the number of carbon atoms is 2 ~
l, (1rIn addition to J chain saturation, small saturation, branching, aromatic rings, etc.
◇Specific examples include l (when is hydrogen)) OOS, I) OOS acebuto when acylno^,
+10! 'S Propione-1, I) OCS Henshade, etc., among which one or two types are blended. The blending weight is about 0.0001 to 1 ton liter%.

本発明における養毛料の基AAとしては、特に限定され
るものではなく、ローション、乳液、クリーム等種々の
タイプが11丁能である。
The base AA of the hair nourishing agent in the present invention is not particularly limited, and various types such as lotion, milky lotion, cream, etc. can be used.

又、本発明に係る養毛オ′1には、デ」キシフルヂコス
テロン系化合物の(l1通常養しt・1に用いられる添
加剤たとえば・ヒノギチi−ル、カチ〕ン界面活V1.
剤等の殺菌1’FII、メント−ル等の清涼剤、3リー
ブ油・スクワラン、高級アル:I−ル等の′/lli分
、その低界面活性剤、香料、酸化l!/j +l剤、紮
夕(彩i!吸収剤・色素・エタノール・水′6を配合す
ることができる。
In addition, the hair nourishing oil'1 according to the present invention contains dexyfludicosterone-based compounds (11) and additives commonly used in hair nourishing oils (11) such as hinogitil, cation surfactant V1. ..
Sterilizing agents such as 1'FII, cooling agents such as menthol, 3 leave oil, squalane, high alcohols, etc., low surfactants, fragrances, oxidized l! /j +l agent, 紮ゆ(sai i! absorbent, pigment, ethanol, water'6) can be blended.

次ニ’F 56明に用いるテし1・IJ−!ルてコスデ
ロン系化合物の安全性テスト結果について述べる。
Teshi 1・IJ- used for the next Ni'F 56 Akira! This paper describes the safety test results of cosderone-based compounds.

(対象) 成人1tr、”J“)乙 (試料) 1 デ刈−V−シ:フルチ:Iスデ[1シ5
%流動パラフィン溶液 2 デメキシコルf〜:Iスデロン′j七テート5%流
動パラフィン溶液 3 流動パラフィン溶液 (試験方法) 24 時間人体前腕クローズドパ、チテスト(判定基べ
If)  廿 強紅斑 十  紅  斑 十ii’&かな紅斑 −陰  性 (結 果) 上記した結果から明、らかなように、本発明に用いるデ
メキンコルチコステijン糸化合物には・皮膚刺激性は
全くない。
(Target) Adult 1tr, "J") Otsu (sample) 1.
% liquid paraffin solution 2 Detexol f~: I Suderon'j 7tate 5% liquid paraffin solution 3 Liquid paraffin solution (test method) 24-hour human forearm closed test, test (judgment basis If) 廿 Strong erythema 10 Erythema 10 ii '& Kana Erythema - Negative (Results) As is clear from the above results, the demequin corticosteroid compound used in the present invention has no skin irritation at all.

(以 1 ホ 1−1) 次に実施例をあ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。
(Hereinafter referred to as 1-1) Next, the present invention will be explained in more detail by giving examples. The present invention is not limited thereby. The blending amount is in weight%.

実施例に先たち試験法を説明する◇ 養毛効果測定法 養毛料使用前後の洗髪時脱毛本数の変化で判定した。被
験者は実施例1〜3および比較例1の計4種類の各々の
群ごとに10名とした。測定期間は4力月間とし、最初
の2力月間は養毛料無塗布の期間、後半の2力月間を養
毛料塗布の期間とし1この間・2日おきに洗髪し・1週
間に1良法毛を回収しその本数を数えた。各期間の抜毛
本数の表示は、養毛料無塗布の2力月間、計8回の抜毛
本数のデータと養毛料塗布の2力刀間、818回の抜単
位は本である。効果の判定は、夫々の期間の平均値の差
から次のように表示した。
The test method will be explained in the Examples.◇ Hair growth effect measurement method Judgment was made based on the change in the number of strands of hair removed during hair washing before and after using the hair growth agent. There were 10 subjects in each of the four groups of Examples 1 to 3 and Comparative Example 1. The measurement period was 4 months, with the first 2 months being a period of no application of hair tonic, and the latter 2 months being a period of applying hair tonic. They were collected and counted. The number of hairs pulled out for each period is shown as data for a total of 8 hairs pulled out for 2 months without hair tonic application, and 818 hairs pulled out for 2 months with hair tonic applied. The effectiveness was determined based on the difference between the average values for each period as shown below.

廿:抜毛本数が70本以上減って おり著しい効果を認
めた。
廿:The number of hairs pulled was reduced by more than 70, indicating a significant effect.

十・払毛木数が開本以上減っておりかなりの効果を認め
た。
The number of brushed trees was reduced by more than the number of open trees, indicating a considerable effect.

±:抜毛木数が10本以上減っておりやや効果ありとい
えた。
±: The number of hairs removed was reduced by 10 or more, indicating that it was somewhat effective.

一:抜毛木数の減少が10本未満であり効果ありとはい
えない。
1: The number of hairs removed was less than 10, and it could not be said to be effective.

(以」−°余白) 実施例1 養毛料(「コーショ■タイプ)(佃I) 95%エタノール            80デオキ
シコルチコステロン       10ヒノキチオール
            00]ビオチン      
          0.01硬化ヒマシNI+ (E
O) 40モル(J加物0.5精製水        
       J848香料、色素         
    適 1.)(製法) エタノールにデ」キシコルチコステロン、ヒノキチ刈−
ル、ビ副ヂン、硬化ヒマン油(1!:o) 40モルイ
XJ加物、香料、色素を添加し、攪J′1゛溶解させ、
次に精製水を添加、混合して透明液状養毛刺をrISた
○ 実施例2 養毛料(ローションタ・rブ)(市■じ) グ リ セ リ  ン               
                       10
.0プロピレングリコール         50オレ
イルアルコール          0.31ノ ポリオキシエチレン1ルビタン モノラウリン酸エステス(2DEf1.)     1
.0ポリオキシエチレンラウリル エーテル(2:1En)            10
95%エタノール           10.0デオ
キシコルチコステロン プロピオネート             O,0CI
01デオキシコルチフステロン       0.05
精製水               ’16499香
料、色素、防腐剤 (製法) 精製水にグリセリン、プロピレングリコールを加え、室
温下で溶解する。一方、エタノールに残りの成分を加え
て溶解し、それを前述した精製水1’一 部〜加えて可溶化し、調色、p過後、養毛料を得1° 
               (以下余白)実施例3
 養毛料(乳液タイプ) 香料、色素、防腐剤       適 量(製法) 上記成分(A)および(B)をそれぞれ80 ’Cに加
熱し、同温度で両成分を混合乳化し、攪拌しながら常温
まで冷却し、養毛料を得た。
(hereinafter -° margin) Example 1 Hair nourishing agent (Kosho type) (Tsukuda I) 95% ethanol 80 Deoxycorticosterone 10 Hinokitiol 00] Biotin
0.01 hardened castor NI+ (E
O) 40 mol (J additive 0.5 purified water
J848 fragrance, pigment
Appropriate 1. ) (Manufacturing method) Ethanol, xycorticosterone, and hinokichi kari.
Add 40 moles of alcohol, vinegar, hydrogenated human oil (1!:o), additives, fragrances, and pigments, stir to dissolve J'1,
Next, purified water was added and mixed to create a transparent liquid hair growth agent.Example 2 Hair growth agent (lotion) (city)
10
.. 0 Propylene Glycol 50 Oleyl Alcohol 0.31 Nopolyoxyethylene 1 Rubitan Esthes Monolaurate (2DEf1.) 1
.. 0 polyoxyethylene lauryl ether (2:1En) 10
95% ethanol 10.0 deoxycorticosterone propionate O,0CI
01 Deoxycortyphsterone 0.05
Purified Water '16499 Fragrance, Pigment, Preservative (Production Method) Add glycerin and propylene glycol to purified water and dissolve at room temperature. On the other hand, add and dissolve the remaining ingredients in ethanol, add 1 part of the above-mentioned purified water to solubilize it, adjust the color, pass through the water, and obtain a hair nourishing agent.
(Left below) Example 3
Hair nourishing agent (emulsion type) Fragrance, pigment, preservative Appropriate amount (manufacturing method) Heat each of the above ingredients (A) and (B) to 80'C, mix and emulsify both ingredients at the same temperature, and bring to room temperature while stirring. It was cooled and a hair nourishing agent was obtained.

(結果) 実施例1 ノ体仏  無塗布期間 養毛料塗布期間 効果1   
  214±46       161±45    
   +2361±35   241±36   −1
−)3473±29   365±34++4193±
46   145±31十′5174±51121±4
4+ 6     368±25       268±29
       −H−7151±41    135±
34      ±8     411±39    
   309±36       ++9315±41
251±35+ 10     425±50      314±32
      +十実施例2 パネル應 無塗布期間 養毛料塗布期間 効果1   
  415±54      301±46     
 ++2365±36   345±38   −1+
3241±41209±31+ 4352±29   261±25   −H−546
1±37      351±38       ++
       ()体ル煮 無塗布期間 養毛料塗布期
間 効果6     254±21       21
3±59      4−7194±18   171
±31    ±8     168±24     
  141±19       +9295±4423
9±24+ 10     345±48      231±36
      +十実施例 ペネル煮 無塗布期間 養毛料塗布期間 効果1   
 545±35      461±39      
++2375±41296±25丹 3     .416±29       321±3
6      ++4218±36361±41+ 5     198±25       171±21
       +6356±46241±23丹 7256±29’ 201±35+ 8     195±25       171±21
        +9265±41245±29+ 10     312±39       209±3
1      ++以上の効果試験の結果から明らかな
ように、D+、osJ化合物を配合した本発明冷に係る
養毛料は優れた効果を有するものである。
(Results) Example 1 No body Buddha No application period Hair tonic application period Effect 1
214±46 161±45
+2361±35 241±36 -1
-)3473±29 365±34++4193±
46 145±310'5174±51121±4
4+ 6 368±25 268±29
-H-7151±41 135±
34 ±8 411±39
309±36 ++9315±41
251±35+ 10 425±50 314±32
+10 Example 2 Panel sintering Non-application period Hair tonic application period Effect 1
415±54 301±46
++2365±36 345±38 -1+
3241±41209±31+ 4352±29 261±25 -H-546
1±37 351±38 ++
()Non-application period Hair tonic application period Effect 6 254±21 21
3±59 4-7194±18 171
±31 ±8 168±24
141±19 +9295±4423
9±24+ 10 345±48 231±36
+10 Examples Penel boil Non-application period Hair tonic application period Effect 1
545±35 461±39
++2375±41296±25tan3. 416±29 321±3
6 ++4218±36361±41+ 5 198±25 171±21
+6356±46241±23 7256±29' 201±35+ 8 195±25 171±21
+9265±41245±29+ 10 312±39 209±3
As is clear from the results of the effect test of 1 ++ or more, the hair nourishment according to the present invention containing the D+ and osJ compounds has excellent effects.

実施例4 養毛料(クリームタイプ) 香料、色素、防腐剤       適量(製法) (4)を70−75 Cにて均一に溶解し、あらかじめ
調製しておいたω)を加えて攪拌し、得られるエマルジ
ョンを冷却して、養毛料を得た。
Example 4 Hair nourishing agent (cream type) Fragrance, pigment, preservative Appropriate amount (manufacturing method) Dissolve (4) uniformly at 70-75 C, add ω) prepared in advance and stir to obtain. The emulsion was cooled to obtain a hair nourishing agent.

特許出願人 株式会社 資 生 堂Patent applicant Shiseido Co., Ltd.

Claims (1)

【特許請求の範囲】 下記一般式 %式%( ) で表わされるデ〕キシコルチコステロン系化合物のうぢ
1種または2種以上を配合してなる養毛イr’t 0(
以−1ミ 全 白)
[Scope of Claims] A hair nourishing treatment r't 0 (
I-1 mi all white)
JP19829582A 1982-11-11 1982-11-11 Hair tonic Pending JPS5988409A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP19829582A JPS5988409A (en) 1982-11-11 1982-11-11 Hair tonic

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP19829582A JPS5988409A (en) 1982-11-11 1982-11-11 Hair tonic

Publications (1)

Publication Number Publication Date
JPS5988409A true JPS5988409A (en) 1984-05-22

Family

ID=16388749

Family Applications (1)

Application Number Title Priority Date Filing Date
JP19829582A Pending JPS5988409A (en) 1982-11-11 1982-11-11 Hair tonic

Country Status (1)

Country Link
JP (1) JPS5988409A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4567038A (en) * 1985-03-06 1986-01-28 Revlon, Inc. Sunscreen composition for hair protection
JPH03161426A (en) * 1989-11-20 1991-07-11 Kobayashi Kose Co Ltd Hair tonic

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4567038A (en) * 1985-03-06 1986-01-28 Revlon, Inc. Sunscreen composition for hair protection
JPH03161426A (en) * 1989-11-20 1991-07-11 Kobayashi Kose Co Ltd Hair tonic

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