JP3596835B2 - Hair restorer - Google Patents

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JP3596835B2
JP3596835B2 JP23260996A JP23260996A JP3596835B2 JP 3596835 B2 JP3596835 B2 JP 3596835B2 JP 23260996 A JP23260996 A JP 23260996A JP 23260996 A JP23260996 A JP 23260996A JP 3596835 B2 JP3596835 B2 JP 3596835B2
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hair
extract
growth
hair growth
hair restorer
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JPH1059829A (en
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耕一郎 田村
達郎 山村
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Noevir Co Ltd
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Noevir Co Ltd
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Description

【0001】
【発明の属する技術分野】
本発明は、良好な保水性を有して頭皮に水分を補給し、或いは頭皮からの水分蒸散を制御するとともに、育毛,養毛効果を有する成分を選択的且つ効率よく毛包に到達させることにより、頭皮を乾燥から保護して頭皮の乾燥に起因するふけ,痒み等の症状を緩和し、且つ非常に優れた育毛,養毛効果を発揮し得る養毛剤に関する。
【0002】
さらに詳しくは、アミノ酸,高級脂肪酸及び高級アルコールより選択される1種又は2種以上を含有する脂質二分子膜に、育毛,養毛効果を有する成分を内包させて配合することを特徴とする、養毛剤に関する。
【0003】
【従来の技術】
脱毛症は、栄養摂取不良,ふけの過剰発生による頭皮生理機能の低下、頭皮皮下組織,末梢血管の血流量減少に起因する毛包,毛球部の新陳代謝機能の低下、皮脂腺及び毛包,毛根部における男性ホルモンの関与による毛包機能の低下、及び精神的ストレスなど、種々多様な原因により発生する。
【0004】
かかる脱毛症を治療,改善するために、エストロン,エストラジオール,エチニルエストラジオール等の卵胞ホルモン、ビタミンE及びその誘導体,センブリ抽出物,ニンニク抽出物,ニンジン抽出物,アロエ抽出物,セファランチン,塩化カルプロニウム,ミノキシジル等の末梢血管血流促進剤、トウガラシチンキ,カンタリスチンキ,ショウキョウチンキ,ハッカ油,l−メントール,カンフル等の局所刺激剤、レゾルシン,サリチル酸,乳酸等の角質溶解剤、ピリドキシン及びその誘導体等の抗脂漏剤、ジンクピリチオン,塩化ベンザルコニウム,塩化ベンゼトニウム,クロルヘキシジン,ヒノキチオール等の殺菌剤、パントテン酸及びその誘導体,胎盤抽出物,ビオチン,ペンタデカン酸グリセリド等の毛根賦活剤、グリチルリチン酸及びその誘導体,β−グリチルレチン酸,アラントイン、アズレン,ε−アミノカプロン酸,ヒドロコルチゾン等の抗炎症剤、ビタミンA,B,B,B12,D等のビタミン剤、システイン,セリン,メチオニン,ロイシン,トリプトファン等のアミノ酸類などの多くの育毛,養毛成分の使用が行われてきた。
【0005】
また、主として男性型脱毛症の治療,改善を目的として、テストステロンから活性型のジヒドロテストステロンへの変換を触媒するテストステロン−5αリダクターゼの活性を阻害するものが多くスクリーニングされてきた。前記酵素の阻害剤としては、プロゲステロン,デオキシコルチコステロン等のステロイド物質の他、多種の植物の抽出物が知られている。また、オキセンドロン,スピロノラクトン,酢酸シプロテロン等はジヒドロキシテストステロンがその受容体に結合するのを阻害するといわれている。
【0006】
しかしながら、従来用いられている上記の育毛,養毛成分やテストステロン−5αリダクターゼ阻害剤の中には、副作用があるため配合可能な量が制限されたり、効果が不十分であったり、養毛剤製剤中での安定性が悪かったり、或いは一定の品質のものを得るのが困難であったりするものが多かった。
【0007】
育毛,養毛成分の安定性及び有効性を向上させるため、これらをリポソームに内包させて養毛剤に配合する試みもなされている。リポソームが毛包に選択的に到達することがすでに報告されており(Nature, Medicine, (7) 705−706 (1995))、毛髪の再生促進,抜け毛減少作用を有するラブダン誘導体をリポソームに内包させて配合する技術も開示されている(特表平5−503287)。
【0008】
【発明が解決しようとする課題】
従って本発明においては、安定性及び安全性が良好で、優れた養毛効果を発揮し、且つ頭皮に対する保湿効果にも優れた養毛剤を提供することを目的とした。
【0009】
【課題を解決するための手段】
上記の課題を解決するべく種々検討を行ったところ、水分保持効果に優れるとしてすでに開示しているアミノ酸,高級脂肪酸及び高級アルコールより選択される1種又は2種以上を含有する脂質二分子膜(特開平7−285827)に、育毛,養毛効果を有する成分を内包させて配合することにより、育毛,養毛効果を有する成分の安定性及び安全性が向上し、さらに育毛,養毛効果が相乗的に増強され、しかも頭皮に対し優れた保湿効果が得られることを見い出し、本発明を完成するに至った。
【0010】
本発明において育毛,養毛成分を内包させる脂質二分子膜は、アミノ酸,高級脂肪酸及び高級アルコールより選択される1種又は2種以上を含有する。ここで、脂質二分子膜はホスファチジルコリン,ホスファチジルエタノールアミン,ホスファチジルセリン,ホスファチジルイノシトール等のグリセロリン脂質、スフィンゴミエリン等のスフィンゴリン脂質、グルコシルアシルグリセロール等のグリセロ糖脂質、ホスファチジルグルコシルアシルグリセロール等のホスホグリセロ糖脂質、グルコセレブロシド,ガラクトセレブロシド等のスフィンゴ糖脂質を用いて調製することができる。かかる脂質を80〜90℃に攪拌しながら加温溶解し、アミノ酸等の1種又は2種以上を添加して含有させる。これらの添加量は脂質二分子膜複合体の1〜20重量%が適当である。
【0011】
脂質二分子膜に含有させるアミノ酸としては、特にL−プロリン,L−イソロイシン,L−ロイシン,L−アラニン,L−スレオニン及びL−リジンより成る群から選択することが好ましい。アミノ酸を含有させた場合には、さらに水溶性高分子の1種又は2種以上を含有させてもよい。前記水溶性高分子としては、ポリアクリル酸及びその塩,カルボキシビニルポリマー及びその塩,ヒドロキシエチルセルロース,カルボキシメチルセルロース及びその塩,ヒアルロン酸及びその塩等が好ましいものとして挙げられる。これら水溶性高分子の配合量としては、脂質二分子膜複合体の0.05〜1.0重要%程度が適当である。
【0012】
また、脂質二分子膜に含有させる高級脂肪酸としては、炭素数14〜22の飽和又は不飽和脂肪酸が好ましく、高級アルコールとしては、炭素数14〜22の飽和又は不飽和脂肪族アルコールが好ましい。
【0013】
本発明において、アミノ酸等を含有する脂質二分子膜に内包させる育毛,養毛成分としては、女性ホルモンであるエストラジオール,エストロン,プロゲステロン、テストステロン−5αリダクターゼ阻害作用を有する酢酸コルチコステロン,酢酸デオキシコルチコステロン,セージ(Salvia officinalis L.)抽出物,ホップ(Humulus lupulus L.)抽出物,ローズマリー(Rosmarinus officinalis)抽出物,オトギリソウ(Hypericum erectum Thunb.)抽出物,ハッカ(Mentha arvensis L.var.piperascens Malinv.)抽出物,セイヨウハッカ(Mentha piperita L.)抽出物,カミツレ(Matricaria chamomilla L.)抽出物,アルニカ(Arnica montana L.)抽出物,タイム(Thymus vulgaris L.)抽出物、ジヒドロテストステロンの受容体への結合を阻害する作用を有するスピロノラクトン,酢酸シプロテロン,シス−ジャスモン(cis−jasmone),メチルジヒドロイソジャスモネイト(methyl dihydroisojasmonate),メチルジヒドロジャスモネイト(methyl dihydrojasmonate),ジヒドロジャスモン(dihydrojasmone)、血流促進作用を有する2,4−ジアミノ−6−ピペリジノピリミジン−3−オキシド(ミノキシジル)、毛包細胞の賦活活性を有するグリチルリチン,コウハク抽出物及びハトムギモヤシ抽出物等が好ましいものとして挙げられ、これらより1種又は2種以上を選択して用いる。なお、前記植物等の抽出物は、植物を生のままで、或いは乾燥後細切又は粉砕して、水、メタノール,エタノール,プロパノール等の低級アルコール、1,3−ブチレングリコール,プロピレングリコール,ジプロピレングリコール,グリセリン等の多価アルコール、アセトン、酢酸エチルといった極性溶媒或いはこれらの混合物を抽出溶媒として用い、浸漬等の抽出操作により得ることができる。
【0014】
育毛,養毛成分を内包させたアミノ酸等含有脂質二分子膜は、多重膜の層状(ラメラ)構造を形成させたり、球状のリポソームを形成させて養毛剤の基剤に分散させる。
【0015】
【作用】
本発明による養毛剤においては、アミノ酸等を含有する脂質二分子膜に内包された育毛,養毛成分が有効に毛包に到達し、さらに頭皮に対する保湿効果も相まって、相乗的な育毛,養毛効果の向上が認められる。
【0016】
一例として、2,4−ジアミノ−6−ピペリジノピリミジン−3−オキシド(ミノキシジル)を、プロリン及びイソロイシンを各10.0重量%含有するホスファチジルコリンリポソームに内包させ(内包率;10重量%)、ミノキシジルの最終濃度が0.2(W/V)%となるようにリン酸緩衝塩類溶液(PBS)に分散させた。このリポソーム分散液0.1mlを、除毛したマウス背部に1日1回連続して塗布し、除毛部位の色調の変化を測色した。除毛部位に発毛が見られる場合、発毛が進むにつれ測色値は低下する。実験はマウス3匹を1群として行った。結果は各群の測色値の平均値にて図1に示した。
【0017】
図1において、ミノキシジルをアミノ酸含有脂質二分子膜より成るリポソームに内包させて塗布した群(3)では、塗布開始後4週間経過後ぐらいから測色値の顕著な低下が認められ、発毛度の増加が確認された。これに対し、ミノキシジルをエタノールに溶解して塗布した群(2)では、PBSのみを塗布した対照群(1)と比べて差は認められなかった。
【0018】
さらに本発明においては、育毛,養毛成分の安定性が向上し、養毛剤への配合量も少量でよいため、副作用の発現もなく、頭皮や顔面,頸部の皮膚に対する刺激性や感作性、眼粘膜刺激性も認められない。
【0019】
【発明の実施の形態】
本発明に係る養毛剤は、ローション剤,乳剤,ゲル剤,クリーム,軟膏等の形態で提供することができ、ヘアーローション,ヘアートニック,ヘアーミルク,ヘアージェル,ヘアークリーム,ヘアーパック,ヘアートリートメント,ヘアーシャンプー,ヘアーリンスといった形態の養毛剤及び毛髪用化粧料として実施することができる。
【0020】
【実施例】
さらに本発明の特徴について、実施例により詳細に説明する。まず、各実施例において基剤に分散させた育毛,養毛成分を内包するアミノ酸等含有脂質二分子膜の調製例を表1に示した。これらは表1中の構成脂質を80〜90℃に攪拌しながら加温溶解し、アミノ酸等の添加物質を加えて混合した後冷却し、次いで育毛,養毛成分を添加し内包させて調製する。養毛剤基剤にはリポソーム又は多重膜層状物の形態として添加した。なお、表1中の構成脂質は各脂質の等重量の混合物であり、ホップ等の植物などの抽出物は50容量%エタノール溶液を用いて調製した。
【表1】

Figure 0003596835
【0021】
Figure 0003596835
製法:(1)〜(4)を順次(5)に添加,溶解して均一とし、次いで(6)を分散させる。
【0022】
Figure 0003596835
製法:(1)〜(4)を順次(5)に添加,溶解して均一とし、次いで(6)を分散させる。
【0023】
Figure 0003596835
製法:(1)〜(3)を加熱溶解し、80℃とする。一方(4)〜(9)の水相成分を混合,加熱溶解し、80℃とする。これに前記油相を攪拌しながら加え、ホモジナイザーにより均一に乳化する。冷却後30℃にて(10)を添加し、(11),(12)を分散させる。
【0024】
Figure 0003596835
製法:(1)を(3)と(7)の一部に分散する。(2),(4)〜(6)を(7)の残部に溶解し、攪拌しながら前記分散物に添加する。次いで、(8),(9)を分散させる。
【0025】
Figure 0003596835
製法:(4)に(1)〜(3)を加えて均一に溶解する。一方、(5)〜(7)の水相を混合,溶解し、前記溶液に加えて混合して均一とし、次いで(8)を分散させる。
【0026】
Figure 0003596835
製法:(1)〜(5)を混合し、均一に溶解する。一方、(6)を(7)に溶解し、前記アルコール相に加え、ろ過した後(8)を分散させる。
【0027】
Figure 0003596835
製法:(1)を(2)と(8)の一部に分散する。(3)〜(7)を(8)の残部に溶解し、攪拌しながら前記分散物に添加する。次いで、(9),(10)を分散させる。
【0028】
Figure 0003596835
製法:(3)を(2)と(4)の溶解物に添加し、ホモミキサーで均一に乳化する。これを(1),(5)〜(7)の溶液に添加した後、(8),(9)を分散させる。充填は缶に原液を充填し、バルブ装着後液化石油ガスを充填する。
【0029】
Figure 0003596835
製法:(9)を70℃に加熱し、(1)〜(8)を加え均一に溶解した後冷却し(10)〜(12)を分散させる。
【0030】
Figure 0003596835
製法:(5)〜(9)の水相成分を混合,溶解して70℃に加熱する。一方(1)〜(4)の油相成分を混合し、70℃に加熱する。前記水相に油相を添加してホモミキサーにて乳化し、冷却後(10)〜(12)を分散させる。
【0031】
上記本発明の実施例のうち、実施例1〜実施例4について毛髪の成長促進効果の評価を行った。各実施例において、育毛,養毛成分をそれぞれアミノ酸等を含有する脂質二分子膜に内包させずに配合し、全量を精製水で100重量%としたものをそれぞれ比較例1〜比較例4とし、男性型脱毛症患者における使用試験を行った。使用試験は男性型脱毛症患者20名を1群とし、各群に実施例及び比較例をそれぞれブラインドにて1日2回、6カ月間連続使用させ、6カ月後の発毛の程度を写真撮影により評価して行った。評価は表2に示す判定基準に従って行い、各評価点数を得たパネラー数にて表3に示した。
【表2】
Figure 0003596835
【0032】
【表3】
Figure 0003596835
表3において、本発明の実施例使用群では、ほとんどのパネラーで全体的な生毛が認められ、45%以上ののパネラーで硬毛の発生が見られる等、いずれも良好な発毛状況が認められる。これに対して、育毛,養毛成分をアミノ酸等を含有する脂質二分子膜に内包させないで配合した比較例使用群では、いずれも対応する実施例使用群に比べ発毛の程度は低く、比較例1及び比較例2使用群では、硬毛の発生を認めたパネラーは見られなかった。
【0033】
なお上記の使用試験期間中において、実施例1〜実施例4のいずれにおいても製剤の変質や状態の悪化は見られず、各実施例を使用したパネラーにおいても、紅斑や浮腫の発生といった皮膚刺激反応や、皮膚感作性反応は全く認められなかった。
【0034】
次いで、本発明の実施例5〜実施例10について使用試験を行った。この際にも、各実施例において育毛,養毛成分をアミノ酸等を含有する脂質二分子膜に内包しないで配合し、全量を精製水で100重量%としたものを比較例5〜比較例10とした。使用試験は薄毛の気になる男女パネラー20名を1群とし、1日2回、6カ月間連続して使用させ、薄毛の改善状況,使用時のしっとり感及び使用時の刺激感,不快感の有無について官能評価させて行った。官能評価結果は、薄毛の改善状況については、「改善された;5点」,「やや改善された;4点」,「変化なし;3点」,「やや悪化した;2点」,「悪化した;1点」、使用時のしっとり感については「ある;5点」,「ややある;4点」,「どちらともいえない;3点」,「ややない;2点」,「ない;1点」として点数化し、20名の平均値を求めた。使用時の刺激感及び不快感については、表4に示す判定基準に従って評価させ、20名の平均値を求め、刺激指数とした。結果は表5にまとめて示した。
【表4】
Figure 0003596835
【0035】
【表5】
Figure 0003596835
表5において明らかなように、本発明の実施例使用群では、育毛,養毛成分の含有量が少ないにもかかわらず薄毛症状の改善傾向が認められている。これに対し、育毛,養毛成分をアミノ酸等を含有する脂質二分子膜に内包させないで配合した比較例使用群では、いずれにおいてもはっきりした改善は認められていなかった。また使用時のしっとり感について、本発明の実施例使用群では、いずれにおいてもそれぞれ対応する比較例使用群に比べて有意に高い評価を得ていた。さらに、いずれの実施例使用群においても特に問題となる刺激感及び不快感は認められておらず、特に実施例7〜実施例10使用群では、比較例7〜比較例10使用群に比べて有意に低い刺激指数を示していた。
【0036】
なお上記の使用試験期間中において、実施例5〜実施例10のいずれにおいても製剤の変質や状態の悪化は見られず、各実施例を使用したパネラーにおいても、紅斑や浮腫の発生といった皮膚刺激反応や、皮膚感作性反応は全く認められなかった。
【0037】
【発明の効果】
以上詳述したように、本発明により、安定性及び安全性が良好で、優れた養毛効果を発揮し、且つ頭皮に対する保湿効果にも優れた養毛剤を提供することができた。
【図面の簡単な説明】
【図1】2,4−ジアミノ−6−ピペリジノピリミジン−3−オキシド(ミノキシジル)を、アミノ酸を含有する脂質二分子膜にてリポソーム化して塗布した場合と、エタノールに溶解して塗布した場合の発毛のようすを示す図である。
【符号の説明】
1 対照群
2 ミノキシジルのエタノール溶液塗布群
3 ミノキシジル内包リポソーム塗布群[0001]
TECHNICAL FIELD OF THE INVENTION
The present invention is to replenish water to the scalp with good water retention, or to control water evaporation from the scalp, and to allow components having hair growth and hair growth effects to reach the hair follicle selectively and efficiently. Accordingly, the present invention relates to a hair restorer capable of protecting the scalp from drying, relieving symptoms such as dandruff and itch caused by drying of the scalp, and exhibiting excellent hair growth and hair growth effects.
[0002]
More specifically, it is characterized in that a lipid bilayer containing one or more selected from amino acids, higher fatty acids and higher alcohols is incorporated with a component having a hair-growth and hair-growth effect, and is blended. Related to hair restorer.
[0003]
[Prior art]
Alopecia is caused by poor nutrition intake, decreased scalp physiological function due to excessive dandruff, hair follicles caused by decreased blood flow in the scalp subcutaneous tissue and peripheral blood vessels, decreased metabolic function in the hair bulb, sebaceous glands and hair follicles, hair roots It is caused by a variety of causes, such as reduced hair follicle function due to the involvement of androgens in the head and mental stress.
[0004]
In order to treat and improve such alopecia, estrogen such as estrone, estradiol, ethinyl estradiol, vitamin E and its derivatives, assembly extract, garlic extract, carrot extract, aloe extract, cepharanthin, carpronium chloride, minoxidil And other peripheral stimulating agents such as pepper tincture, tincture tincture, ginger tincture, peppermint oil, l-menthol, camphor, etc., keratolytic agents such as resorcin, salicylic acid, lactic acid, pyridoxine and derivatives thereof. Antiseborrheic agents, fungicides such as zinc pyrithione, benzalkonium chloride, benzethonium chloride, chlorhexidine, hinokitiol, pantothenic acid and its derivatives, placental extracts, hair root activators such as biotin and pentadecanoic acid glyceride, glycyrrhizin And its derivatives, beta-glycyrrhetinic acid, allantoin, azulene, .epsilon.-aminocaproic acid, anti-inflammatory agents such as hydrocortisone, vitamin A, B 2, B 6, B 12, vitamin agents such as D, cysteine, serine, methionine, leucine Many hair growth and hair growth components such as amino acids such as tryptophan and the like have been used.
[0005]
In addition, for the purpose of treating and improving male pattern baldness, many screenings have been screened for those that inhibit the activity of testosterone-5α reductase, which catalyzes the conversion of testosterone to active dihydrotestosterone. Known inhibitors of the enzyme include steroid substances such as progesterone and deoxycorticosterone, as well as various plant extracts. Also, oxendrone, spironolactone, cyproterone acetate and the like are said to inhibit dihydroxytestosterone from binding to its receptor.
[0006]
However, some of the conventionally used hair growth and hair growth components and testosterone-5α reductase inhibitors have side effects, so that the amount that can be incorporated is limited, the effect is insufficient, In many cases, the stability at the time was poor, or it was difficult to obtain a product of a certain quality.
[0007]
In order to improve the stability and effectiveness of hair growth and hair growth components, attempts have been made to incorporate them into liposomes and blend them into hair growth agents. It has already been reported that liposomes selectively reach hair follicles (Nature, Medicine, 1 (7) 705-706 (1995)), and liposome encapsulation of a labdone derivative having an action of promoting hair regeneration and reducing hair loss. A technique of blending by blending is also disclosed (Japanese Patent Publication No. 5-503287).
[0008]
[Problems to be solved by the invention]
Accordingly, an object of the present invention is to provide a hair restorer having good stability and safety, exhibiting an excellent hair restore effect, and also having an excellent moisturizing effect on the scalp.
[0009]
[Means for Solving the Problems]
Various studies have been made to solve the above-mentioned problems. As a result, a lipid bilayer membrane containing one or two or more selected from amino acids, higher fatty acids and higher alcohols already disclosed as having excellent water retention effect ( Japanese Patent Application Laid-Open No. 7-285827) incorporates a component having a hair-growth and hair-growth effect, and mixes it, thereby improving the stability and safety of the component having a hair-growth and hair-growth effect, and further improving the hair growth and hair-growth effect. The inventors have found that synergistically enhanced and an excellent moisturizing effect on the scalp can be obtained, thereby completing the present invention.
[0010]
In the present invention, the lipid bilayer membrane encapsulating hair growth and hair growth components contains one or more selected from amino acids, higher fatty acids and higher alcohols. Here, the lipid bilayer is composed of glycerophospholipids such as phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, sphingolipids such as sphingomyelin, glyceroglycolipids such as glucosylacylglycerol, and phosphoglyceroglycolipids such as phosphatidylglucosylacylglycerol. And glycosphingolipids such as glucocerebroside and galactocerebroside. The lipid is heated and dissolved at 80 to 90 ° C. with stirring, and one or more amino acids and the like are added and contained. The appropriate amount of these additives is 1 to 20% by weight of the lipid bilayer complex.
[0011]
The amino acid to be contained in the lipid bilayer is preferably selected from the group consisting of L-proline, L-isoleucine, L-leucine, L-alanine, L-threonine and L-lysine. When an amino acid is contained, one or more water-soluble polymers may be further contained. Preferred examples of the water-soluble polymer include polyacrylic acid and salts thereof, carboxyvinyl polymer and salts thereof, hydroxyethyl cellulose, carboxymethyl cellulose and salts thereof, and hyaluronic acid and salts thereof. A suitable amount of these water-soluble polymers is about 0.05 to 1.0% by weight of the lipid bilayer membrane complex.
[0012]
The higher fatty acid contained in the lipid bilayer is preferably a saturated or unsaturated fatty acid having 14 to 22 carbon atoms, and the higher alcohol is preferably a saturated or unsaturated aliphatic alcohol having 14 to 22 carbon atoms.
[0013]
In the present invention, the hair growth and hair growth components to be encapsulated in a lipid bilayer containing an amino acid or the like are estradiol, estrone, progesterone, and testosterone-5α reductase, which are female hormones. Kosuteron, sage (Salvia officinalis L.) extract, hop (Humulus lupulus L.) extracts, rosemary (Rosmarinus officinalis) extract, St. John's wort (Hypericum erectum Thunb.) extract, peppermint (mentha arvensis L.var. piperascens Malinv.) extract, peppermint (mentha piperita L.) extract, chamomile (M tricaria chamomilla L.) extract, arnica (Arnica montana L.) extract, thyme (Thymus vulgaris L.) extract, spironolactone having the effect of inhibiting the binding of dihydrotestosterone receptors, cyproterone acetate, cis - jasmone (Cis-jasmone), methyldihydroisojasmonate, methyldihydrojasmonate, dihydrojasmone, dihydrojasmone, 2,4-diamino having a blood flow promoting action Pyrimidine-3-oxide (minoxidil), glycyrrhizin having hair follicle cell activating activity, amber extract Fine pearl barley sprouts extract and the like as preferred, selected and used one or more from these. The extract of the plant or the like may be obtained by cutting the plant as it is, or by drying and then shredding or pulverizing the same into water, lower alcohols such as methanol, ethanol, and propanol, 1,3-butylene glycol, propylene glycol, A polar solvent such as polyhydric alcohols such as propylene glycol and glycerin, acetone and ethyl acetate, or a mixture thereof can be used as an extraction solvent and can be obtained by an extraction operation such as immersion.
[0014]
The lipid bilayer containing amino acids and the like containing hair growth and hair growth components forms a multilamellar (lamella) structure or forms spherical liposomes and is dispersed in a hair growth agent base.
[0015]
[Action]
In the hair restorer according to the present invention, the hair-growth and hair-growth components contained in the lipid bilayer containing amino acids and the like effectively reach the hair follicle, and further have a moisturizing effect on the scalp, so that a synergistic hair-growth and hair-growth effect is obtained. Improvement is recognized.
[0016]
As an example, 2,4-diamino-6-piperidinopyrimidine-3-oxide (minoxidil) is encapsulated in phosphatidylcholine liposomes each containing 10.0% by weight of proline and isoleucine (encapsulation rate: 10% by weight), Minoxidil was dispersed in phosphate buffered saline (PBS) so that the final concentration of minoxidil was 0.2 (W / V)%. 0.1 ml of this liposome dispersion was continuously applied to the back of the hair-removed mouse once a day, and the color change of the hair-removal site was measured. When hair growth is observed at the hair removal site, the colorimetric value decreases as hair growth proceeds. The experiment was performed with three mice as one group. The results are shown in FIG. 1 as the average of the colorimetric values of each group.
[0017]
In FIG. 1, in the group (3) in which minoxidil was encapsulated in a liposome comprising an amino acid-containing lipid bilayer and applied, a remarkable decrease in the colorimetric value was observed about 4 weeks after the start of application, and the hair growth degree was observed. Increase was confirmed. In contrast, no difference was observed in the group (2) to which minoxidil was dissolved in ethanol and applied, as compared to the control group (1) to which only PBS was applied.
[0018]
Furthermore, in the present invention, the stability of the hair growth and hair growth components is improved, and the amount of the hair growth agent to be used may be small, so that there are no side effects, irritation and sensitization to the skin of the scalp, face and neck. No mucosal irritation was observed.
[0019]
BEST MODE FOR CARRYING OUT THE INVENTION
The hair restorer according to the present invention can be provided in the form of a lotion, an emulsion, a gel, a cream, an ointment and the like, and includes a hair lotion, a hair tonic, a hair milk, a hair gel, a hair cream, a hair pack, a hair treatment, and a hair. It can be implemented as a hair restorer in the form of a shampoo or a hair rinse and a hair cosmetic.
[0020]
【Example】
Further, features of the present invention will be described in detail with reference to examples. First, Table 1 shows examples of preparation of a lipid bilayer containing amino acids and the like containing hair growth and hair growth components dispersed in a base material in each Example. These are prepared by heating and dissolving the constituent lipids in Table 1 while stirring at 80 to 90 ° C., adding and mixing additional substances such as amino acids, cooling, and then adding and growing hair growth and hair growth ingredients. . The hair restorer base was added in the form of liposomes or multilamellar materials. The constituent lipids in Table 1 were a mixture of equal weights of each lipid, and extracts of plants such as hops were prepared using a 50% by volume ethanol solution.
[Table 1]
Figure 0003596835
[0021]
Figure 0003596835
Production method: (1) to (4) are sequentially added to (5) and dissolved to make uniform, and then (6) is dispersed.
[0022]
Figure 0003596835
Production method: (1) to (4) are sequentially added to (5) and dissolved to make uniform, and then (6) is dispersed.
[0023]
Figure 0003596835
Production method: (1) to (3) are heated and melted to 80 ° C. On the other hand, the aqueous phase components (4) to (9) are mixed and dissolved by heating to 80 ° C. The oil phase is added thereto with stirring, and the mixture is uniformly emulsified by a homogenizer. After cooling, (10) is added at 30 ° C. to disperse (11) and (12).
[0024]
Figure 0003596835
Production method: (1) is dispersed in a part of (3) and (7). (2), (4) to (6) are dissolved in the remainder of (7) and added to the dispersion while stirring. Next, (8) and (9) are dispersed.
[0025]
Figure 0003596835
Production method: (1) to (3) are added to (4) and uniformly dissolved. On the other hand, the aqueous phases (5) to (7) are mixed and dissolved, added to the solution and mixed to make the mixture uniform, and then (8) is dispersed.
[0026]
Figure 0003596835
Production method: (1) to (5) are mixed and uniformly dissolved. On the other hand, (6) is dissolved in (7), added to the alcohol phase, filtered, and (8) is dispersed.
[0027]
Figure 0003596835
Production method: (1) is dispersed in a part of (2) and (8). (3) to (7) are dissolved in the remainder of (8) and added to the dispersion while stirring. Next, (9) and (10) are dispersed.
[0028]
Figure 0003596835
Production method: (3) is added to the melts of (2) and (4) and emulsified uniformly with a homomixer. After this is added to the solutions (1), (5) to (7), (8) and (9) are dispersed. For filling, a can is filled with a stock solution, and after mounting a valve, liquefied petroleum gas is filled.
[0029]
Figure 0003596835
Manufacturing method: (9) is heated to 70 ° C., (1) to (8) are added and uniformly dissolved, and then cooled to disperse (10) to (12).
[0030]
Figure 0003596835
Production method: The aqueous phase components (5) to (9) are mixed and dissolved and heated to 70 ° C. On the other hand, the oil phase components (1) to (4) are mixed and heated to 70 ° C. The oil phase is added to the water phase, emulsified by a homomixer, and after cooling, (10) to (12) are dispersed.
[0031]
Of the above examples of the present invention, the effects of promoting hair growth were evaluated for Examples 1 to 4. In each example, hair growth and hair growth components were blended without encapsulation in a lipid bilayer containing amino acids and the like, respectively, and the total amount was adjusted to 100% by weight with purified water, as Comparative Examples 1 to 4, respectively. And a use test in male pattern baldness patients. In the use test, 20 male alopecia patients were grouped into one group, and each group was allowed to use the examples and comparative examples twice a day for 6 months consecutively with a blind, and photographed the degree of hair growth after 6 months. The evaluation was performed by photographing. The evaluation was performed according to the criteria shown in Table 2, and the number of panelists who obtained each evaluation score is shown in Table 3.
[Table 2]
Figure 0003596835
[0032]
[Table 3]
Figure 0003596835
In Table 3, in the group using the examples of the present invention, overall hair growth was observed in most of the panelists, and hard hair was observed in 45% or more of the panelists. Is recognized. On the other hand, in the comparative group using the hair growth and hair growth components without encapsulating them in the lipid bilayer containing amino acids, the degree of hair growth was lower than in the corresponding group using the examples. In the group using Example 1 and Comparative Example 2, there was no paneler who observed the generation of hard hair.
[0033]
During the above-mentioned use test period, no deterioration or deterioration of the preparation was observed in any of Examples 1 to 4, and skin irritation such as occurrence of erythema and edema was observed in panelists using each Example. No reaction or skin sensitization reaction was observed.
[0034]
Next, use tests were performed on Examples 5 to 10 of the present invention. Also in this case, in each of Examples, hair growth and hair growth components were blended without encapsulation in a lipid bilayer containing amino acids and the like, and the total amount was adjusted to 100% by weight with purified water. And In the use test, 20 male and female panelists who are worried about thinning hair are used as a group twice a day for 6 consecutive months, and the improvement of thinning hair, moist feeling at the time of use, irritation at the time of use, and discomfort during use The presence / absence was evaluated by sensory evaluation. The results of the sensory evaluation were as follows: Regarding the improvement status of the thin hair, "Improved; 5 points", "Slightly improved; 4 points", "No change; 3 points", "Slightly worse; 2 points", "Worse" 1 point, and the moist feeling during use was "5 points", "Somewhat; 4 points", "Neither; 3 points", "Slightly low; 2 points", "No;1" The points were scored as "points", and the average value of 20 persons was obtained. The irritation and discomfort during use were evaluated according to the criteria shown in Table 4, and the average value of the 20 subjects was determined and used as the irritation index. The results are summarized in Table 5.
[Table 4]
Figure 0003596835
[0035]
[Table 5]
Figure 0003596835
As is evident from Table 5, in the group using the examples of the present invention, the tendency of improving the hair thinning symptom is recognized despite the low content of the hair growth and hair growth components. On the other hand, no clear improvement was observed in any of the comparative example groups in which the hair growth and hair growth components were blended without being encapsulated in the lipid bilayer containing amino acids and the like. In addition, the moist feeling during use was significantly higher in the group using the example of the present invention than in the corresponding group using the comparative example. Furthermore, no irritating sensation and discomfort, which are particularly problematic, were observed in any of the groups using Examples, and particularly in the groups using Examples 7 to 10, compared with the groups using Comparative Examples 7 to 10. It showed a significantly lower stimulation index.
[0036]
During the above use test period, no deterioration or deterioration of the preparation was observed in any of Examples 5 to 10, and even in the panel using each Example, skin irritation such as erythema and edema occurred. No reaction or skin sensitization reaction was observed.
[0037]
【The invention's effect】
As described in detail above, according to the present invention, it was possible to provide a hair restorer having good stability and safety, exhibiting an excellent hair restore effect, and also having an excellent moisturizing effect on the scalp.
[Brief description of the drawings]
FIG. 1 shows a case where 2,4-diamino-6-piperidinopyrimidine-3-oxide (minoxidil) is applied in the form of a liposome using a lipid bilayer membrane containing an amino acid, and a case where it is dissolved in ethanol and applied. It is a figure which shows the state of hair growth in the case.
[Explanation of symbols]
1 Control group 2 Minoxidil ethanol solution group 3 Minoxidil-encapsulated liposome group

Claims (7)

アミノ酸と、水溶性高分子を含有する脂質二分子膜に、育毛,養毛効果を有する成分を内包させて配合することを特徴とする、養毛剤。 A hair restorer, characterized by incorporating a component having a hair-growth and hair-growth effect into a lipid bilayer containing an amino acid and a water-soluble polymer and blending them. 脂質二分子膜がさらに高級脂肪酸及び高級アルコールより選択される1種又は2種以上を含有することを特徴とする、請求項1に記載の養毛剤。The hair restorer according to claim 1, wherein the lipid bilayer further comprises one or more selected from higher fatty acids and higher alcohols. アミノ酸の1種又は2種以上が、L-プロリン,L-イソロイシン,L-ロイシン,L-アラニン,L-スレオニン及びL-リジンより成る群から選択されることを特徴とする、請求項1又は請求項2に記載の養毛剤。2. The method of claim 1, wherein one or more of the amino acids is selected from the group consisting of L-proline, L-isoleucine, L-leucine, L-alanine, L-threonine and L-lysine. The hair restorer according to claim 2. 高級脂肪酸の1種又は2種以上が、炭素数14〜22の飽和又は不飽和の脂肪酸より選択されることを特徴とする、請求項2又は請求項3に記載の養毛剤。The hair restorer according to claim 2 or 3 , wherein one or more of the higher fatty acids are selected from saturated or unsaturated fatty acids having 14 to 22 carbon atoms. 高級アルコールの1種又は2種以上が、炭素数14〜22の飽和又は不飽和の脂肪族アルコールより選択されることを特徴とする、請求項2〜請求項4の一に記載の養毛剤。The hair restorer according to any one of claims 2 to 4, wherein one or more of the higher alcohols is selected from saturated or unsaturated aliphatic alcohols having 14 to 22 carbon atoms. 育毛,養毛効果を有する成分が、エストラジオール,エストロン,プロゲステロン,酢酸コルチコステロン,酢酸デオキシコルチコステロン,スピロノラクトン,酢酸シプロテロン,2,4-ジアミノ-6-ピペリジノピリミジン-3-オキシド(ミノキシジル),グリチルリチン,シス-ジャスモン(cis-jasmone),メチルジヒドロイソジャスモネイト(methyl dihydroisojasmonate),メチルジヒドロジャスモネイト(methyl dihydrojasmonate),ジヒドロジャスモン(dihydrojasmone),セージ(SalviaofficinalisL.)抽出物,ホップ(HumuluslupulusL.)抽出物,ローズマリー(Rosmarinusofficinalis)抽出物,オトギリソウ(HypericumerectumThunb.)抽出物,ハッカ(MenthaarvensisL.var.piperascensMalinv.)抽出物,セイヨウハッカ(MenthapiperitaL.)抽出物,カミツレ(MatricariachamomillaL.)抽出物,アルニカ(ArnicamontanaL.)抽出物,タイム(ThymusvulgarisL.)抽出物,コウハク抽出物及びハトムギモヤシ抽出物より成る群から選択される1種又は2種以上であることを特徴とする、請求項2〜請求項5の一に記載の養毛剤。The components having hair growth and hair growth effects are estradiol, estrone, progesterone, corticosterone acetate, deoxycorticosterone acetate, spironolactone, cyproterone acetate, 2,4-diamino-6-piperidinopyrimidine-3-oxide (minoxidil) ), Glycyrrhizin, cis-jasmone, methyl dihydroisojasmonate, methyl dihydrojasmonate, dihydrojasmone, sage ( Salviaofficinalis L.) extract, hops (Humuluslupulus L.) extracts, rosemary (Rosmarinusofficinalis) extract, Hypericum (Hypericumerectum Thunb.) extract, peppermint (Menthaarvensis L.var. piperascens Malinv.) extract, peppermint (Menthapiperita L.) extract, chamomile ( Matricariachamomilla L.) extract, Arnica (Arnicamontana L.) extract, wherein the time (Thymusvulgaris L.) extract is one or more selected from the group consisting of red and white extract and pearl barley sprouts extract, claim 2 The hair restorer according to claim 5 . 養毛剤が、毛髪用化粧料であることを特徴とする、請求項1〜請求項6の一に記載の養毛剤。Hair tonic, characterized in that a hair cosmetic, hair tonic according to one of claims 1 to 6.
JP23260996A 1996-08-13 1996-08-13 Hair restorer Expired - Fee Related JP3596835B2 (en)

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GB9704050D0 (en) * 1997-02-27 1997-04-16 Unilever Plc Hair treatment composition
GB9912085D0 (en) * 1999-05-24 1999-07-21 Unilever Plc Use of amino acids in hair treatment
JP3663404B2 (en) * 2001-01-17 2005-06-22 株式会社バイオテック Hair restorer
NL1018637C2 (en) * 2001-07-26 2003-01-28 Adriaan Emanuel Hendricus Wiel Composition useful for e.g. promoting breast growth or preventing breast or prostrate cancer, comprises hops, choline and/or cystine
DE10243626A1 (en) * 2002-09-19 2004-04-01 Henkel Kgaa Hair treatment composition containing an active ingredient combination with liposomes
US20040185075A1 (en) 2003-01-31 2004-09-23 Maria Dalko Use of at least one (dihydro)jasmonic acid derivative for treating dry skin
FR2850571B1 (en) * 2003-01-31 2006-07-07 Oreal USE OF A JASMONIC ACID (DIHYDRO) DERIVATIVE FOR THE TREATMENT OF DRY SKINS
BRPI0804172A2 (en) * 2008-07-15 2010-07-06 Pereira Lopes Jose Emilio Fehr chemical compounds formed from nanocapsulations and element complexation
ES2834006T3 (en) * 2008-09-27 2021-06-16 Jina Pharmaceuticals Inc Lipid-based pharmaceutical preparations for topical application
US9505820B2 (en) 2010-09-01 2016-11-29 Zotos International, Inc. Hair treatment composition with naturally - derived peptide identical to human hair
JP5885186B2 (en) * 2011-05-19 2016-03-15 株式会社ミルボン Cosmetic composition for scalp
MX370253B (en) 2011-09-16 2019-12-06 Nanocare Tech Inc Compositions of jasmonate compounds and methods of use.
JP6097901B2 (en) * 2012-03-01 2017-03-22 株式会社サイエンスリン Testosterone 5α-reductase activity inhibitor
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EP3431505B1 (en) 2016-03-18 2022-09-07 Caregen Co., Ltd. Conjugate of finasteride with peptide

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