JP2787451B2 - Hair restoration - Google Patents

Hair restoration

Info

Publication number
JP2787451B2
JP2787451B2 JP63256370A JP25637088A JP2787451B2 JP 2787451 B2 JP2787451 B2 JP 2787451B2 JP 63256370 A JP63256370 A JP 63256370A JP 25637088 A JP25637088 A JP 25637088A JP 2787451 B2 JP2787451 B2 JP 2787451B2
Authority
JP
Japan
Prior art keywords
hair
present
growth
phase
hair growth
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 - Lifetime
Application number
JP63256370A
Other languages
Japanese (ja)
Other versions
JPH02167213A (en
Inventor
勝 末継
好守 藤沼
善春 辻
章博 石野
城太郎 仲西
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 JP63256370A priority Critical patent/JP2787451B2/en
Publication of JPH02167213A publication Critical patent/JPH02167213A/en
Application granted granted Critical
Publication of JP2787451B2 publication Critical patent/JP2787451B2/en
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • 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
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • 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)

Description

【発明の詳細な説明】 [産業上の利用分野] 本発明は優れた脱毛防止、発毛効果等の養毛作用を持
つ養毛料に関する。本発明は、特に医薬品或は化粧品分
野において利用される。
DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to a hair restorer having an excellent hair growth-inhibiting effect such as hair loss prevention and hair growth effect. The invention finds particular use in the pharmaceutical or cosmetic field.

[従来の技術] 従来より、禿や脱毛の原因としては、毛根、皮脂腺等
の器官における男性ホルモンの活性化、毛包への血流量
の低下、皮脂の分泌過剰、過酸化物の生成等による頭皮
の異常等が考えられている。このため従来の養毛料に
は、前記の原因を取り除いたり、または、軽減する作用
を持つ化合物が一般に配合されている。
[Prior art] Conventionally, causes of baldness and hair loss include activation of androgens in organs such as hair roots and sebaceous glands, decreased blood flow to hair follicles, excessive secretion of sebum, and generation of peroxide. Abnormalities of the scalp are considered. For this reason, a compound having an action of removing or reducing the above-mentioned causes is generally added to the conventional hair restoration.

例えば、ビタミンB6、ビタミンE等のビタミン類、セ
リン、メチオニンなどのアミノ酸類、センブリエキス、
アセチルコリン誘導体などの血管拡張剤、紫根エキス、
ヒノキチオール等の抗炎症剤、エストラジオールなどの
女性ホルモン剤、セファランチンなどの皮膚機能亢進剤
などが配合され、脱毛症の予防および治療に用いられて
いる。
For example, vitamins such as vitamin B 6 and vitamin E, amino acids such as serine and methionine, assembly extract,
Vasodilators such as acetylcholine derivatives, purple root extract,
An anti-inflammatory agent such as hinokitiol, a female hormone such as estradiol, a skin function enhancer such as cepharanthin, etc. are blended and used for the prevention and treatment of alopecia.

[発明が解決しようとする課題] 従来技術の問題点 しかしながら、従来の養毛料はフケ、カユミ、脱毛な
どの予防および改善に有効で、発毛や育毛を促進すると
されているが、脱毛や発毛の機構は非常に複雑であり、
従来の養毛料による男性ホルモンの活性化の阻害や毛包
の血流量の増加だけでは、充分な脱毛防止、発毛効果は
認められなかった。
[Problems to be Solved by the Invention] Problems of the Prior Art However, conventional hair nourishes are effective in preventing and improving dandruff, Kayumi, hair loss and the like, and promote hair growth and hair growth. The mechanism of hair is very complex,
Inhibition of androgen activation by the conventional hair restorer or increase in the blood flow of the hair follicle alone did not provide sufficient hair loss prevention and hair growth effects.

発明の目的 本発明者は、上記の事情に鑑み、脱毛に対して有効で
あり、優れた脱毛防止、発毛効果等の養毛作用を持つ物
質を探求した結果、塩酸エカラジンが強力な養毛作用を
持つことを見出し、本発明を完成するに至った。
SUMMARY OF THE INVENTION In view of the above circumstances, the present inventor has searched for a substance that is effective for hair loss and has an excellent hair growth-inhibiting effect such as hair loss prevention and hair growth. They have found that they have an effect, and have completed the present invention.

[課題を解決するための手段] すなわち、本発明は塩酸エカラジンを有効成分として
配合することを特徴とする養毛料である。
[Means for Solving the Problems] That is, the present invention is a hair restorer characterized by incorporating ecarazine hydrochloride as an active ingredient.

以下、本発明の構成について詳述する。 Hereinafter, the configuration of the present invention will be described in detail.

本発明で使用する塩酸エカラジンは公知の物質であ
り、血圧降下作用、血管拡張作用、子宮筋弛緩作用、脳
血管拡張作用、利尿作用などの薬理作用を持ち、そのLD
50は、マウスにおける経口投与量で894mg/kgであり、副
作用の少ない安全性の高い薬剤であることが従来から知
られており、すでに医薬品として使用されている。(日
本医薬品集、1988、薬業時報社)しかしながら、外用に
する用途は知られておらず、さらに、養毛作用を持つこ
とは全く知られていない。
Ecarazine hydrochloride used in the present invention is a known substance and has pharmacological actions such as blood pressure lowering action, vasodilator action, uterine muscle relaxation action, cerebral vasodilator action, diuretic action, and its LD.
50 is an oral dose of 894 mg / kg in mice, and has been known to be a highly safe drug with few side effects, and has already been used as a drug. (Nippon Pharmaceutical Collection, 1988, Pharmaceutical Times Co., Ltd.) However, there is no known use for external use, and it is not known at all that it has a hair-growth effect.

本発明で使用する塩酸エカラジンは公知の方法で得ら
れるものであり、その配合量は本発明の養毛料中、0.00
1〜15重量%、好ましくは0.1〜5重量%である。
Ecarazine hydrochloride used in the present invention is obtained by a known method, and its compounding amount is 0.000 in the hair restorer of the present invention.
It is 1 to 15% by weight, preferably 0.1 to 5% by weight.

本発明に係る養毛料には、塩酸エカラジンのほか、塩
化カルプロニウム、センブリエキス、アセチルコリン誘
導体等の血管拡張剤、セリン。メチオニン等のアミノ酸
類、ビタミンB6、ビタミンE及びその誘導体、ビオチン
等のビタミン類、パントテン酸及びその誘導体、グリチ
ルレチン酸及びその誘導体、ニコチン酸ベンジルなどの
ニコチン酸エステル類、セファランチン等の皮膚機能亢
進剤、エストラジオール等の女性ホルモン剤等を同時に
配合してもよい。さらに、通常、養毛料に用いられる添
加剤、例えば、ヒノキチオール、ヘキサクロロフェン、
ベンザルコニウムクロリド、セチルピリジニウムクロリ
ド、ウンデシレン酸、トリクロロカルバニリドおよびビ
チオノール等の抗菌剤、メントール等の清涼剤、サリチ
ル酸、亜鉛及びその誘導体、乳酸及びそのアルキルエス
テルなどの薬剤、クエン酸等の有機酸類、アルギニン等
のアミノ酸類、オリーブ油、スクワラン、流動パラフィ
ン、イソプロピルミリステート、高級脂肪酸、高級アル
コール等の油分、グリセリン、プロピレングリコール等
の多価アルコール、その他界面活性剤、香料、酸化防止
剤、紫外線吸収剤、色素、エタノール、水、保湿剤、増
粘剤等が本発明の効果を損なわない範囲で適宜配合する
ことができる。
The hair restorer according to the present invention includes, in addition to ecarazine hydrochloride, vasodilators such as carpronium chloride, assembly extract and acetylcholine derivatives, and serine. Amino acids such as methionine, vitamin B 6 , vitamin E and its derivatives, vitamins such as biotin, pantothenic acid and its derivatives, glycyrrhetinic acid and its derivatives, nicotinic acid esters such as benzyl nicotinate, and skin function enhancement such as cepharanthin Agent, a female hormone agent such as estradiol and the like may be simultaneously added. Further, additives usually used for hair restoration, for example, hinokitiol, hexachlorophene,
Antibacterial agents such as benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide and bithionol, cooling agents such as menthol, salicylic acid, zinc and derivatives thereof, drugs such as lactic acid and its alkyl esters, and organic compounds such as citric acid Acids, amino acids such as arginine, olive oil, squalane, liquid paraffin, isopropyl myristate, higher fatty acids, higher alcohols such as higher alcohols, polyhydric alcohols such as glycerin and propylene glycol, other surfactants, fragrances, antioxidants, ultraviolet rays An absorbent, a dye, ethanol, water, a humectant, a thickener, and the like can be appropriately added as long as the effects of the present invention are not impaired.

本発明の養毛料の性状は、液状、乳液、軟膏など外皮
に適用できる性状のものであればいずれでもよい。
The properties of the hair restorer of the present invention may be any properties that can be applied to the outer skin, such as liquids, emulsions and ointments.

本発明の養毛料は皮膚に直接に塗布または散布する経
皮投与による投与方法をとる。
The hair restoration of the present invention employs an administration method by transdermal administration, which is applied or sprayed directly on the skin.

また、本発明の養毛料の投与量は、年齢、個人差、病
状等により変化するので明確には確定できないが、一般
に人に投与する場合の投与量は体重1Kg及び1日当たり
0.01〜100mg、好ましくは0.1〜10mgであり、この量を1
日1回または2〜4回に分け投与することができる。
In addition, the dosage of the hair nourishes of the present invention cannot be clearly determined because it varies depending on age, individual differences, medical conditions, etc. However, in general, when administered to humans, the dosage is 1 kg of body weight and per day.
0.01 to 100 mg, preferably 0.1 to 10 mg.
It can be administered once or twice or four times a day.

[実施例] 次に実施例をあげて本発明の養毛料の製法および養毛
作用をさらに具体的に説明する。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 production method and hair-growth action of the hair-growth material of the present invention will be described more specifically with reference to examples. The present invention is not limited by this. The compounding amount is% by weight.

(製造法) 95%エタノールに塩酸エカラジンおよび硬化ヒマシ油
エチレンオキシド(40モル)付加物を添加し、撹拌溶解
させ、次いでイオン交換水を添加、混合して実施例1の
液状の養毛料を得た。実施例2〜3並びに比較例1も実
施例1と同様にして得た。
(Production method) Ecarazine hydrochloride and hydrogenated castor oil ethylene oxide (40 mol) adduct were added to 95% ethanol, dissolved by stirring, and then ion-exchanged water was added and mixed to obtain a liquid hair nourishes of Example 1. . Examples 2 and 3 and Comparative Example 1 were obtained in the same manner as in Example 1.

[発毛試験] 実施例1〜3及び比較例1の発毛試験を毛周期の休止
期にあるC3H/HeNCrJマウスを用い、小川らの方法(ノー
マル アンド アブノーマル エピダーマル ディファ
レンシェーション[Normal and Abnormal Epidermal Di
fferentiation]、M.Seiji及びI.A.bernstein編集、第1
59〜170頁、1982年、東大出版)により行なった。
[Hair Growth Test] The hair growth tests of Examples 1 to 3 and Comparative Example 1 were carried out using C3H / HeNCrJ mice in the telogen phase of the hair cycle, according to the method of Ogawa et al. (Normal and Abnormal Epidermal Differentiation [Normal and Abnormal]). Epidermal Di
fferentiation], edited by M. Seiji and IAbernstein, No. 1
59-170, 1982, The University of Tokyo Press).

すなわち、マウスを1群10匹とし、無塗布、実施例1
〜3及び比較例1の各群に分け、バリカン及びシェーバ
ーでマウスの背部を剃毛し、それぞれのサンプリングを
1日1回、0.1mlずつ塗布した。各サンプルの発毛効果
はマウス背部の発毛部分を測定して面積比によって比較
した。各サンプルによる50%発毛率に要する日数を表2
に示した。
That is, a group of 10 mice, no application, Example 1
3 and Comparative Example 1, the back of the mouse was shaved with a clipper and a shaver, and 0.1 ml of each sample was applied once a day. The hair growth effect of each sample was measured by measuring the hair growth portion on the back of the mouse, and was compared based on the area ratio. Table 2 shows the number of days required for 50% hair growth rate by each sample
It was shown to.

以上のように、本発明に係わる養毛料は、優れた発毛
効果を有している。
As described above, the hair restorer according to the present invention has an excellent hair growth effect.

[養毛作用試験] 次に本発明の養毛料の脱毛防止、発毛効果等の養毛作
用を調べるために、人に対して、トリコグラム試験を実
施した。実施例1〜3、比較例1の養毛料について行っ
た。
[Hair-growing action test] Next, in order to examine the hair-growing action such as the hair loss-preventing effect and the hair-growth effect of the hair-growing agent of the present invention, a tricogram test was performed on humans. Examples 1 to 3 and Comparative Example 1 were performed on the hair nourishes.

(トリコグラム試験) 養毛料の使用前と使用後の抜去毛髪の毛根を顕微鏡下
で観察し、毛根の形態から休止期毛根数を計数し、その
割合の増減によって養毛料の養毛作用を比較した。休止
期毛根とは成長の止まった毛の毛根であり、脱毛を訴え
る人は正常な人よりもこの休止期毛根の割合が多いこと
が認められている。
(Trichogram test) Observation of the roots of the extracted hair before and after using the hair restoration under a microscope, counting the number of telogens from the root form, and comparing the hair growth effect of the hair restoration by increasing or decreasing the ratio did. The telogen follicles are the hair follicles that have stopped growing, and it has been recognized that those who report hair loss have a higher percentage of these telogen follicles than normal people.

実施例1〜3および比較例1の各養毛料をそれぞれ男
性被験者10名の頭皮に1日2回、1回2mlずつ6カ月間
連続して塗布し、塗布直前および6カ月間塗布終了直後
に被験者1名につき100本ずつ毛髪を抜去し、それぞれ
の毛根を調べた。結果を表3に示した。
Each of the hair restorations of Examples 1 to 3 and Comparative Example 1 was applied to the scalp of 10 male subjects twice a day, 2 ml at a time, continuously for 6 months, immediately before the application and immediately after the completion of the application for 6 months. One hundred hairs were removed from each subject, and the hair roots were examined. The results are shown in Table 3.

なお、この試験において、試験開始後、養毛料を塗布
しないものの休止期率が上昇し、塗布したものの休止期
率が維持されれば、脱毛防止作用があると判断し、休止
期率が下がれば、発毛効果があるものと判断できる。
In this test, after the start of the test, if the hair resting rate is not applied but the resting rate increases, and if the resting rate of the applied hair is maintained, it is determined that there is a hair loss preventing action, and if the resting rate decreases, It can be determined that there is a hair growth effect.

以上のように本発明に係る養毛料は、優れた脱毛防
止、発毛効果等の養毛作用を有している。
As described above, the hair nourishing material according to the present invention has excellent hair nourishing effects such as hair loss prevention and hair growth effects.

実施例4 (A 相) 塩酸エカラジン 1.0 ポリオキシエチレン(60モル)付加硬化ヒマシ油2.0 グリセリン 10.0 ジプロピレングリコール 10.0 1,3−ブチレングリコール 5.0 ポリエチレングリコール1500 5.0 (B 相) セチルイソオクタネート 10.0 スクワラン 5.0 ワセリン 2.0 プロピルパラベン 2.0 (C 相) カルボキシビニルポリマー1%水溶液 30.0 ヘキサメタリン酸ソーダ 0.03 イオン交換水 8.35 (D 相) イオン交換水 4.5 (E 相) カセイカリ 0.12 イオン交換水 5.0 (製造法) A相、B相をそれぞれ60℃で加熱溶解し、混合してホ
モミキサー処理しゲルを作る。これにD相を徐々に添加
しホモミキサーで分散する。
Example 4 (Phase A) Ecarazine hydrochloride 1.0 Polyoxyethylene (60 mol) addition hydrogenated castor oil 2.0 Glycerin 10.0 Dipropylene glycol 10.0 1,3-butylene glycol 5.0 Polyethylene glycol 1500 5.0 (Phase B) Cetyl isooctanoate 10.0 Squalane 5.0 Vaseline 2.0 Propylparaben 2.0 (C phase) 1% aqueous solution of carboxyvinyl polymer 30.0 Sodium hexametaphosphate 0.03 Ion exchange water 8.35 (D phase) Ion exchange water 4.5 (E phase) Kaseikari 0.12 Ion exchange water 5.0 (Production method) A phase, B The phases are each heated and dissolved at 60 ° C., mixed and homogenized to form a gel. Phase D is gradually added thereto and dispersed with a homomixer.

次にこれに溶解したC相を加え、最後に溶解したE相
を添加しホモミキサーで乳化してO/W乳液型の養毛料を
得た。
Next, the dissolved C phase was added thereto, and finally the dissolved E phase was added and emulsified with a homomixer to obtain an O / W emulsion type hair restorer.

この養毛料を実施例1と同様に人に対して、実使用テ
ストを行ったところ、その脱毛防止、発毛効果等の養毛
作用が優れていることが確認された。
When a real use test was performed on a person using the hair regrowth in the same manner as in Example 1, it was confirmed that the hair regrowth was excellent in hair growth prevention effects such as hair loss prevention and hair growth effects.

[発明の効果] 本発明の養毛料は優れた脱毛防止、発毛効果等の養毛
作用を持つ養毛料である。
[Effects of the Invention] The hair restorer of the present invention is a hair restorer having an excellent hair loss-promoting effect such as hair loss prevention and hair growth effect.

───────────────────────────────────────────────────── フロントページの続き (72)発明者 石野 章博 神奈川県横浜市港北区新羽町1050番地 株式会社資生堂研究所内 (72)発明者 仲西 城太郎 神奈川県横浜市港北区新羽町1050番地 株式会社資生堂研究所内 (56)参考文献 特開 昭61−40210(JP,A) 特開 昭62−135409(JP,A) 特開 昭62−270519(JP,A) 特開 昭62−126109(JP,A) 特開 昭62−270515(JP,A) 特開 昭56−65811(JP,A) 特開 平1−172322(JP,A) 特公 昭44−27320(JP,B1) 国際公開88/40(WO,A1) 大阪府病院薬剤師会編 「全訂 医薬 品要覧」 (昭61−9−10) 薬業時報 社 P.442 (58)調査した分野(Int.Cl.6,DB名) A61K 7/06 - 7/155 CA(STN)──────────────────────────────────────────────────続 き Continued on the front page (72) Inventor Akihiro Ishino 1050 Nippa-cho, Kohoku-ku, Yokohama-shi, Kanagawa Prefecture Inside Shiseido Research Laboratories (72) Inventor Jotaro Nakanishi 1050 Nippa-cho, Kohoku-ku, Yokohama-shi, Kanagawa Shiseido Research Inc. (56) References JP-A-61-40210 (JP, A) JP-A-62-135409 (JP, A) JP-A-62-270519 (JP, A) JP-A-62-126109 (JP, A) JP-A-62-270515 (JP, A) JP-A-56-65811 (JP, A) JP-A-1-172322 (JP, A) JP-B-44-27320 (JP, B1) International publication 88/40 ( WO, A1) Osaka Prefectural Hospital Pharmacists Association, “Complete Handbook of Pharmaceuticals” (61-9-10, 1986) 442 (58) Field surveyed (Int.Cl. 6 , DB name) A61K 7/06-7/155 CA (STN)

Claims (1)

(57)【特許請求の範囲】(57) [Claims] 【請求項1】塩酸エカラジンを有効成分として配合する
ことを特徴とする養毛料。
1. A hair restorer comprising an ecarazine hydrochloride as an active ingredient.
JP63256370A 1988-09-09 1988-10-12 Hair restoration Expired - Lifetime JP2787451B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP63256370A JP2787451B2 (en) 1988-09-09 1988-10-12 Hair restoration

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP22445488 1988-09-09
JP63-224454 1988-09-09
JP63256370A JP2787451B2 (en) 1988-09-09 1988-10-12 Hair restoration

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FR2717381B1 (en) * 1994-03-15 1996-04-19 Oreal Compositions based on alpha-pyrones to induce and stimulate hair growth and / or slow down hair loss and use.

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DE2942666A1 (en) * 1979-10-23 1981-05-07 Wella Ag, 6100 Darmstadt COSMETIC AGENT FOR TREATING THE HAIR AND SCALP
JPS6140210A (en) * 1984-06-01 1986-02-26 ロシデイ・イスマイル Skin treating and protecting drug
JPS62126109A (en) * 1985-11-25 1987-06-08 Kanebo Ltd Hair tonic cosmetic
JPS62135409A (en) * 1985-12-10 1987-06-18 Lion Corp Hair tonic cosmetic
JPS62270519A (en) * 1986-05-20 1987-11-24 Kanebo Ltd Hair tonic cosmetic
JPS62270515A (en) * 1986-05-20 1987-11-24 Kanebo Ltd Hair tonic cosmetic
WO1988000040A1 (en) * 1986-07-02 1988-01-14 American Health Products Corporation Topical hair growing composition and kit
JPS63308991A (en) * 1987-06-10 1988-12-16 Nec Corp Heat sink for semiconductor laser

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