JP5789901B2 - 皮膚化粧用組成物におけるオリゴマーバイオサーファクタント - Google Patents
皮膚化粧用組成物におけるオリゴマーバイオサーファクタント Download PDFInfo
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Description
本出願は2008年5月29日に出願された米国仮出願第61/071,985号の優先権を主張する。本願は、また、米国特許出願第12/227,825号の一部継続出願、2008年11月28日に35USC§371の下で出願された米国国内段階出願である。米国特許出願第12/227,825号は国際出願PCT/US2007/012799に基づき、2007年5月31日に出願された。米国特許出願第12/227,825号及びPCT/US2007/012799の両方が、2006年6月1日に出願された米国仮出願第60/809,825号の優先権を主張する。米国出願第61/071,985号、第60/809,825号、及び第12/227,825号ならびにPCT/US2007/012799の開示は、それらの全体において参照により本明細書に含まれる。
本発明は、オリゴマーミセル構造中に自己集合又は自己会合することができるバイオサーファクタント及び局所適用される皮膚科用製品におけるそれらの使用に関する。本発明は、特に、水性MEM環境中での表面張力を約50ダイン/cm2未満まで下げることができ、代謝性可溶性タンパク質及び/又は細胞外皮膚マトリックスタンパク質の合成及び/又は細胞ターンオーバー速度を増加させる能力を有し、一方で同時に、比較的低い毒性、好ましくは37歳の女性の線維芽細胞において200ppmを上回るLD50を示す、基礎培地の水溶液において約1.0ppm〜約200ppm、好ましくは約50ppm未満の低い臨界ミセル濃度(「CMC」)を有するオリゴマーアシル化バイオサーファクタント(「OAB」)に関する。本発明の別の態様は、局所適用される製剤中でのOABの使用に関し、その製剤とは、皮膚、毛髪、及び爪ならびに目、耳、鼻、口、肛門、及び腟の粘膜と直接接触するように置かれる製剤を意味する。
PCT/US2007/012799は、国際特許出願WO/2007/143006として公開されており、(i)水性MEM環境中での表面張力を約50ダイン/cm2未満まで下げることができ、(ii)代謝性可溶性タンパク質を増加させる能力を有する、基礎培地(MEM)の水性環境において低い臨界ミセル濃度(主に約100ppm未満)を有するOABの使用を記載する。各々が異なる特性を有する、特定のOABを含むクリーム、ローション、ゲル、及び美容液が開示される。WO/2007/143006において開示されるOABの特性には、皮膚マトリックスタンパク質(例、エラスチン、フィブロネクチン、コラーゲン)の合成を増加させ、及び/又は細胞ターンオーバー速度を増加させる能力を有するが、これらのタンパク質を分解する酵素(例、マトリクスメタロプロテイナーゼ)の合成を同時に増加させない。また、開示されるOABのいくつかが(i)炎症性タンパク質(特にインターロイキン6及びインターロイキン8)の増加を引き起こさず、及び/又は(ii)広域スペクトラムの抗菌活性(即ち、種々の微生物の増殖を阻害する又は殺す能力)を有することが教示される。
A Ala アラニン
D Asp アスパラギン酸
E Glu グルタミン酸
G Gly グリシン
H His ヒスチジン
I Ile イソロイシン
K lys リジン
L Leu ロイシン
M Met メチオニン
R Arg アルギニン
P Pro プロリン
S Ser セリン
T Thr スレオニン
V Val バリン
本発明は、MEM溶液の表面張力を約50ダイン/cm2未満まで低下させ、MEM溶液の水性環境において約200ppm未満、好ましくは約50ppm未満の臨界ミセル濃度を有するオリゴマーアシル化バイオサーファクタント(「OAB」)に関し、ここでOABは本質的に(i)分岐又は非分岐、飽和又は不飽和、好ましくはミリストイル化した8〜22員の炭素鎖;(ii)3〜9個のアミノ酸残基(その内の少なくとも1つ、好ましくは2つが荷電している);及び(iii)酸性C末端又はアミドC末端から成る。
「ペニシリン−ストレプトマイシン溶液」は、0.85%生理食塩水中5,000μg/mlのペニシリンGナトリウム及び5,000μg/mlの硫酸ストレプトマイシンから成る調製物であり、同じくInvitrogenから入手可能である。
以下の実施例は、本発明をさらに例示する。構成成分及び特定の成分が典型的であるとして提示され、種々の改変は、前述の開示に照らして本発明の範囲内でもたらされ得る。特に指摘のない限り、パーセンテージは全組成物の重量による。
A相
脱イオン水 70〜90%
B相
中鎖トリグリセリド(C6−C12) 2〜8%
レシチン2〜8%中鎖脂肪酸(C6−C12) 2〜8%
リジン又はアルギニン 1〜2%
配列番号12(P228) 10〜1,000ppm*
*Therapeutic Peptides Inc.(Baton Rouge, LA)から
30〜40℃で約10分間10,000〜1200rpmの高速ホモジナイザーを用いてB相をA相中に混合する。次に、得られた混合物をコロイドミル中で、約10,000psi超で処理し、約200nm未満のサイズの粒子を作成する。得られた濃縮物を、濃度約1%〜約20%で通常のマクロエマルジョンクリームに加える。
1.脱イオン水 95〜98%
2.キサンタンガム 0.1〜0.3%
3.アスコルビン酸リン酸マグネシウム 1〜3%
4.配列番号14(P266)* 10〜1,000ppm
5.ヒドロキシメチルグリシンナトリウム** 0.3〜1%
*Therapeutic Peptides Inc.(Baton Rouge, LA)から
**Sutton Labs(Chatham, NJ)からのSuttocide A
成分2〜5を、均質になるまでSilversonミキサー中で1,000rpmで混合しながら脱イオン水に加える。
パートA
アスコルビン酸パルミテート 1.00
BHT 0.20
SDアルコール40−B 1.50
パートB
Sesamum Indicum(ゴマ)種油 1.00
セラミド3 0.50
パートC
グリセリン 1.50
PEG−60アーモンドグリセリド 1.00
イソプロピルパラベン、イソブチルパラベン、
ブチルパラベン 1.00
パートD
レチニルパルミテート 1.00
酢酸トコフェロール 1.00
C30−45アルキルメチコン 1.00
C12−15安息香酸アルキル 7.50
ジメチコン 2.00
パートE
アスコルビン酸リン酸マグネシウム 3.00
エチルヘキシルパルミテート、トリベヘニン、ソルビタン
イソステアリン酸、配列番号22(P382) 3.00
パートF
SDアルコール40−B、配列番号23(P387) 0.50
PEG−60アーモンドグリセリド、
配列番号25(P394) 0.04
シクロメチコン、ジメチコンクロスポリマー 71.81
ダイズ油、レチノール 1.00
香料 0.45
A相の成分を主容器に加える、45〜55℃に加熱しながら400rpmで混合する。続いて、400〜800rpmで混合しながらパートB、次にパートC、次にパートDを主容器に加える。パートEを加えながら、Silversonミキサーを用いて2500rpmでホモジナイズする。1000〜1700rpmで混合しながらパートFを加え、2500rpmでホモジナイズする。
パートA
シクロペンタシロキサン、二酸化チタン、アルミナ、
PEG−10ジメチコン、メチコン 60.00
酸化亜鉛、シクロペンタシロキサン、
PEG−10ジメチコン、メチコン 8.00
シクロメチコン、ジメチコノール 1.00
イソステアリン酸ソルビタン 1.50
パートB
ジメチコン/ビニルジメチコンクロスポリマー 4.00
酸化鉄(黒) 0.02
酸化鉄(赤) 0.09
酸化鉄(黄) 0.25
パートC
シクロメチコン、ジメチコンクロスポリマー 21.90
パートD
トリベヘニン、ベヘン酸カルシウム 2.25
パートE
レシチン、SDアルコール40−B 0.50
カプリル酸/カプリン酸トリグリセリド、セラミドIIIA、
コレステロール、酢酸トコフェロール、スクアレン、
レチニルパルミテート、配列番号1(P291) 10.50
パートAを主容器に加える。300〜600rpmで混合しながら110℃まで加熱する。パートBの成分を一緒に、Silversonミキサーを用いてホモジナイズする。パートBをパートAに加える。パートC及びDをパートA及びBに加える。Silversonミキサーを用いて1500〜2500rpmでホモジナイズする。混合しながら70℃まで冷却する。パートEを上記混合物に加え、均質になるまで混合を続ける。
パートA
水 70.27
1,3−β−D−グルカン乳酸(非酵母由来) 0.04
アスコルビン酸リン酸マグネシウム 0.40
パートB
ベヘノキシジメチコン 1.60
シクロメチコン 5.10
酢酸トコフェロール 0.20
ベヘントリモニウムメトサルフェート、セテアリルアルコール 3.60
ジメチコン 2.10
ベヘニルアルコール 1.60
グリセリン、レシチン、パルミトイル ミリスチルセリナート 0.50
パルミトイル加水分解コムギタンパク質 0.30
セテアリルアルコール、セテアリルグルコシド 2.00
パートC
PEG−7ヤシ脂肪酸グリセリル、PPG−2−セテアレス−9、
シマセンブリ(Centaurium Erythraea)抽出物 4.00
グリセリン、水、Siegesbeckia Orientalis抽出物 4.00
ポリメタクリル酸グリセリル、PEG−8、
配列番号60(P373) 2.00
PEG−60アーモンドグリセリド、
配列番号27(P401) 1.00
パートD
フェノキシエタノール、メチルパラベン、ブチルパラベン、
エチルパラベン、プロピルパラベン、イソブチルパラベン 0.70
香料 0.50
パートAの成分を主容器に加える。70℃まで加熱しながら500rpmで混合する。パートBの成分を75℃まで500rpmで混合及び加熱する。500〜1500rpmで混合しながらパートBをパートAに加える。1200〜1600rpmで混合しながら55℃まで冷却する。1200〜1600rpmで混合しながらパートCを加える。1200〜1600rpmで混合しながら45℃まで冷却する。パートDをA−B−Cに加え、Silversonオーバーヘッドホモジナイザーを用いて3000rpmで10kg当たり5分間ホモジナイズする。
A相
クオタニウム−91(及び)セトリモニウムメトサルフェート
(及び)セテアリルアルコール1 1.50
ベヘントリモニウムメトサルフェート(及び)セチルアルコール
(及び)ブチレングリコール2 0.80
クオタニウム−93(及び)ジプロピレングリコール3 0.50
ステアラミドプロピルジメチルアミン 0.30
セチルエステル 1.50
ステアリルアルコール 3.00
PPG−3ミリスチン酸ベンジルエーテル 4.00
Olea Europea(オリーブ)果実油 1.00
Prunus Amygdalus Dulcis(スイートアーモンド)油 1.00
Limnanthes Alba(メドウフォーム)種油 1.00
B相
脱イオン水 100mlにするのに十分な量
クエン酸結晶 0.05
C相
グリセリン(及び)水(及び)Camellia sinensis抽出物4 0.05
プロピレングリコール(及び)水及びRheum Palmatum抽出物5 0.05
ブチレングリコール(及び)水(及び)Chamomilla Recutita6 0.05
フェノキシエタノール(及び)メチルパラベン(及び)エチルパラベン
(及び)プロピルパラベン(及び)ブチルパラベン
(及び)イソブチルパラベン7 0.05
配列番号75(P226) 10〜1,000ppm
配列番号69(P288) 10〜1,000ppm
D相
加水分解された植物タンパク質PG−プロピルシラントリオール
1,2,3,4それぞれ商標名Crodazosoft DBQ、Incroquat Behenyl TMS-50、Incroquat 18-MEA-40、及びCrodarom Green Teaの下でCroda Inc.(Edison, NJ)から市販されている。
5,6商標名Actiphyte of Rhubarb PG50及びActiphyte of Chamomile BG50の下でActive Organics LP(Lewisville, TX)から市販されている。
7PhenonipとしてClariant Corp.(Mount Holly, NC)から市販されている。
75〜80℃まで混合及び加熱しながらA及びB相の成分を別々に合わせる。B相をA相に加えて、十分に混合する。50℃まで冷却し、混合しながら成分をC相に加える。35℃まで冷却し、D相を加える。室温まで冷却し、必要に応じてpHを4.5に調整する。
A相
水素化ポリシクロペンタジエン(及び)イソドデカン 14.29
イソドデカン 24.64
B相
リチウムケイ酸マグネシウム 2.00
SDアルコール 1.00
C相
酸化鉄[C.I.77499] 7.00
ポリメチルシルセスキオキサン 2.00
シリカ 1.00
雲母(及び)二酸化チタン 1.00
シクロメチコン(及び)ポリエチレングリコール/
PPG−20/15ジメチコン 3.00
イソドデカン 10.00
D相
塩化ナトリウム 0.25
脱イオン水 11.50
メチルパラベン 0.10
E相
C18−36トリグリセリド 5.00
密ろうSP422 6.00
カルナウバロウ 3.00
ポリエチレン617A 3.00
プロピルパラベン 0.10
F相
脱イオン水 2.00
パンテノール 0.35
イミダゾリジニル尿素 0.25
配列番号85(P222) 10〜1,000ppm
配列番号80(P214) 10〜1,000ppm
G相
イソドデカン 2.00
セルロース 0.50
A相の材料を合わせる。少しずつリチウムケイ酸マグネシウムを加える。高速で20分間撹拌する。SDアルコールを加え、さらに20分間撹拌する。C相の成分を合わせ、高速で45分間撹拌する。ゲル相(A−B)をC相に加え、基剤を形成する。D相の成分を合わせ、透明になるまで撹拌する。少しずつD相を基剤(A−B−C相)に加え、85℃まで加熱しながらホモジナイズを続ける。ろう(E相)を70℃で基剤(A−B−C−D相)に加え、ホモジナイズを続ける。空冷を開始する。65℃で、QS溶媒を飛ばす。42℃で、F相の溶液を加える。38℃で、G相のスラリーを加える。ホモジナイズを続け、25℃まで冷却する。
Claims (9)
- (i)分岐又は非分岐、飽和又は不飽和の8〜22員の炭素鎖;(ii)3〜9個のアミノ酸残基(その内の少なくとも1つが荷電している);及び(iii)酸性C末端又はアミドC末端から成るオリゴマーアシル化バイオサーファクタントを含むヘアケア製剤であって、
前記オリゴマーアシル化バイオサーファクタントが、配列番号75;配列番号99;配列番号69;及び配列番号85から成る群より選択される少なくとも1種である、ヘアケア製剤。 - 毛髪に適用される、請求項1に記載のヘアケア製剤。
- 毛髪が、頭部の毛髪又は顔の毛髪である、請求項2に記載のヘアケア製剤。
- オリゴマーアシル化バイオサーファクタントが、配列番号75;及び配列番号99から成る群より選択される、請求項1〜3のいずれかに記載のヘアケア製剤。
- マスカラ、まつ毛伸長剤、まつ毛コンディショナー、アイライナー、アイブローペンシル、クリーム、ローション、ゲル、美容液、メーキャップ、コンディショニングヘアパック又はコンディショニングマスカラである、請求項1〜4のいずれかに記載のヘアケア製剤。
- 指で塗る、拭く、軽くたたくことにより、あるいは、スポンジ又はスポンジを先に付けた塗布具、スワブ、ペン、ブラシ、ティッシュ、パッド又はペーパータオルにより、皮膚又は毛髪に接触して置かれる、請求項1〜5のいずれかに記載のヘアケア製剤。
- (i)分岐又は非分岐、飽和又は不飽和の8〜22員の炭素鎖;(ii)3〜9個のアミノ酸残基(その内の少なくとも1つが荷電している);及び(iii)酸性C末端又はアミドC末端から成る、配列番号75;配列番号99;配列番号69;及び配列番号85から成る群より選択される少なくとも1種のオリゴマーアシル化バイオサーファクタントを含む毛髪の成長刺激剤。
- (i)分岐又は非分岐、飽和又は不飽和の8〜22員の炭素鎖;(ii)3〜9個のアミノ酸残基(その内の少なくとも1つが荷電している);及び(iii)酸性C末端又はアミドC末端から成る、配列番号75;配列番号99;配列番号69;及び配列番号85から成る群より選択される少なくとも1種のオリゴマーアシル化バイオサーファクタントを含む脱毛症又は薄毛の処置又は改善剤。
- (i)分岐又は非分岐、飽和又は不飽和の8〜22員の炭素鎖;(ii)3〜9個のアミノ酸残基(その内の少なくとも1つが荷電している);及び(iii)酸性C末端又はアミドC末端から成る、配列番号75;配列番号99;配列番号69;及び配列番号85から成る群より選択される少なくとも1種のオリゴマーアシル化バイオサーファクタントを含む毛髪の喪失の阻害又は低下剤。
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