CN102844017A - 含有藤黄酸、藤黄酸酯或藤黄酰胺的毛发护理组合物 - Google Patents
含有藤黄酸、藤黄酸酯或藤黄酰胺的毛发护理组合物 Download PDFInfo
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- CN102844017A CN102844017A CN2011800189516A CN201180018951A CN102844017A CN 102844017 A CN102844017 A CN 102844017A CN 2011800189516 A CN2011800189516 A CN 2011800189516A CN 201180018951 A CN201180018951 A CN 201180018951A CN 102844017 A CN102844017 A CN 102844017A
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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Abstract
本发明涉及一种化妆品组合物,其包含式(I)或式(II)的化合物或盐,其中R1和R2均独立地为氢(H),或饱和的、直链的或支化的C1-C8烷基。更具体地,本发明还涉及所述化妆品组合物在用于防止毛发变灰白和/或用于恢复和/或保持自然的毛发颜色中的用途。式(I):式(II):
Description
本发明涉及一种化妆品组合物,其包含如式(I)或式(II)所描述的藤黄酸(gambogic acid)、或其盐、其酯或其酰胺。更具体地,本发明涉及所述化妆品组合物在用于防止毛发变灰白和/或用于恢复和/或用于保持自然的毛发颜色以及修复或增强毛发生长的用途。
此外,本发明涉及一种用于防止毛发变灰白和/或用于恢复和/或用于保持自然的毛发颜色的方法,其包括下列步骤:将包含有效量的式(I)或式(II)所描述的藤黄酸、或其盐、其酯或其酰胺的局部用组合物涂覆到人类毛发的皮肤上。
本发明还涉及式(I)或式(II)所描述的藤黄酸、或其盐、其酯或其酰胺在用于增加毛囊中黑素细胞的总数和/或增大黑素细胞从毛鞘向毛基质分化和迁移中的用途。
毛发变灰白是人类衰老的明显信号,然而其机理至今基本上仍不明。毛发是由所谓角蛋白的蛋白质组成。毛发本身分为三层,外护膜、中间皮质和中心髓质。如果毛发有色,那么是由于存在颜料-黑色素(黑色或棕色)或褐黑素(红色或黄色)。如果缺少这些颜料,毛发变为白色。“白发病”是用于指代灰发的术语,灰发是由白色和彩色毛发的混合物产生的错觉。毛发从毛囊长出。毛囊的壁形成毛发的外根鞘。毛囊的下部加宽形成包含生发基质(这是毛发生长的根源)的毛球。皮肤组织伸出进入毛囊基底形成真皮乳头,这具有毛细血管网以提供生长所需的氧、能量和氨基酸。
黑素细胞存在于真皮乳头上部的毛球中,产生色素粒(黑素体),色素粒被转移到毛干形成上皮细胞(角化细胞),并分布在整个皮质中。同时,它们形成毛囊的色素单元。在毛囊中,具有三个层的内根鞘围绕着毛发。亨利氏层(Henle’s layer)为1个细胞厚,并且位于鞘的中间。赫胥黎层(Huxley′s layer)为2个或3个细胞厚,并且位于鞘的中间。该内根鞘的外皮与毛发的外皮相互扣住。毛发和内根鞘以相同的速率生长,但是内根鞘在毛囊上约三分之二处分解,所以只有毛发露出超过皮肤表面。
本领域公知的是,由于毛囊中黑素细胞的消失毛发变灰白(Tobin 2009,Int.J.Trichology 1(2):83-93)。该过程既影响位于毛囊底部并直接造成毛发纤维着色的色素单元的黑素细胞毛发,又影响位于毛囊的外根鞘的远侧部的先驱性黑素细胞,先驱性黑素细胞充当着色单元在各毛发周期中再生的仓库(Van Neste and Tobin 2004,Micron 35:193-200)。
尽可能地调整老龄化的影响具有不断增加的重要性。在本发明的上下文中,使用染色处理香波通常使得被认为不好看的白色毛发消失。然而,很明显的是,尽管该技术在抵消毛发变灰白的影响中证明很有效,但是对毛发变灰白的起因没有影响。因此,该解决方法是暂时的,并且需要随着毛发生长频繁地更新。
因此,在毛发护理业中仍存在期望已久的需要,来防止与年龄有关的毛发变灰白,防止毛发自然色的减少,甚至增强自然头发颜色的恢复,不仅仅是因为其持久效果,还因为其能中止老化过程的视觉文献。
本申请的发明人现在已经惊讶地发现,如下面所述的藤黄酸衍生物作为化妆品组合物具有巨大潜力,其可用于毛发护理应用中用于防止毛发变灰白和/或恢复和/或保持自然的毛发颜色,如所述化合物和衍生物增加毛囊中黑素细胞的总数以及增大黑素细胞从毛鞘向毛基质分化和迁移的能力所示。
因此,在第一个实施方式中,本发明提供了一种化妆品组合物,其包含式(I)或式(II)的化合物、或所述化合物的盐,
其中R1和R2均独立地为氢(H),或饱和的、直链的或支化的C1-C8烷基。
要理解的是,如上所示的式(I)和式(II)均包括所有可能的立体异构体。
在式(I)或式(II)化合物的上述定义中,优选的R1和R2基团均独立地为氢、甲基、乙基、丙基、异丙基、丁基、仲丁基、异丁基、戊基、新戊基、己基、2-乙基-己基、庚基和辛基。很容易理解的是,含有3个或更多个碳原子的任何低级烷基可以是直链或支化链。
最优选的R1和/或R2烷基选自甲基、乙基和丙基。
式(I)或式(II)的藤黄酸的盐或酰胺衍生物可以通过任何化妆品可接受的阳离子形成,所述化妆品可接受的阳离子意指任何金属阳离子以及对皮肤无毒和/或不会导致过敏反应的任何有机阳离子。所述阳离子的例子为铵盐和烷基铵盐、碱金属阳离子(例如钠离子和钾离子)以及碱土金属阳离子(例如钙离子和镁离子)。
在具体的实施方式中,R1基团为氢,因而将式(I)的化合物限定为藤黄酸或所述酸的盐,并且将式(II)化合物限定为藤黄酸的伯胺或仲胺衍生物,其中R2为氢、甲基、乙基、丙基、异丙基、丁基、仲丁基、异丁基、戊基、新戊基、己基、2-乙基-己基、庚基、或壬基。含有3个或更多个碳原子的任何低级烷基可以是直链或支化链。其中最优选的R2烷基选自甲基、乙基和丙基。
在一个优选的实施方式中,化妆品组合物包含藤黄酸、藤黄酰胺、或所述化合物的盐,包括所有可能的立体异构体。
根据本发明最优选的组合物包含根据式(II)的藤黄酰胺,其中R1和R2均为氢,具有如式(III)所示的立体化学,其具有下列CA下标名:2-丁烯酰胺、2-甲基-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-四氢-8-羟基-3,3,11-三甲基-13-(3-甲基-2-丁烯-1-基)-11-(4-甲基-3-戊烯-1-基)-7,15-二氧代-1,5-亚甲基-1H,3H,11H-呋[3,4-g]吡喃[3,2-b]呫吨-1-基]-,(2Z)-和下列CAS编号(286935-60-2)
在另一个实施方式中,根据本发明的化妆品组合物包含含有藤黄酸和/或藤黄酰胺的粗制藤黄树脂(crude gamboges resin)、或来自Garciniahandburryi树中渗出的树脂的天然提取物,如WO2008/148008所述。
本发明的化合物可以源自化学品供应商,例如Sigma。藤黄酸可以通过下列方法简单地提纯:由藤黄树脂制备粗制提取物的嘧啶盐,随后在乙醇中反复进行盐的重结晶。该树脂从Garcinia handburyi树中渗出,该树是生长于亚洲的树。提纯方法在WO2008/148008中有所描述,此外,藤黄酰胺可以用藤黄酸作为前驱体使用标准的酰胺化化学反应来制备,这在P.N.A.S.(2007),104:16329-16334中也有所描述。
在另一个实施方式中,根据本发明的化妆品组合物可以进一步包含常用于化妆品组合物、更具体是用于局部用毛发护理组合物的辅助剂(载体和/或赋形剂或稀释剂)。
常用于根据本发明的毛发护理组合物中的合适的辅助剂选自Ullmann’sEncyclopedia of Industrial Chemistry(1989),Vol.A 12,Hair Preparations中更具体地,例如在国际专利申请号WO 00/06094,WO 00/07550和WO 01/06994中以一般性术语公开的那些。
在本发明的另一个实施方式中,根据本发明的化妆品组合物包含上述的式(I)、式(II)、或式(III)化合物,基于组合物的总重,其含量介于0.00001重量%和20重量%之间。基于组合物的总重,根据本发明的优选的含量介于0.0001重量%和1重量%之间。
根据本发明优选的化妆品组合物是下列形式的局部用毛发护理组合物:化妆品用毛发处理制剂(例如生发油(hair tonics)和调理剂),毛发护理制剂(例如预处理制剂),造型霜,造型啫哩,润发油,毛发冲洗剂,护理套装(treatment pack),深层毛发护理剂(例如免洗和冲洗深层调理剂),发型造型(hair-structuring)制剂(例如用于持久卷发(热卷发、适中卷发、冷卷发)的卷发制剂),毛发拉直制剂,液体毛发造型制剂,毛发泡沫,毛发喷雾,漂白制剂(例如过氧化氢溶液),闪亮香波(lightening shampoo),漂白霜,漂白粉,漂白膏或油,临时的、半永久性的或永久性的染发剂,含自身氧化染料的制剂,或天然染发剂(如散沫花或甘菊)。
最优选的毛发护理制剂为选自生发油、调理剂、处理剂和造型霜的免洗组合物。
基于应用,毛发护理制剂可以是如下形式的:(气雾剂)喷雾、(气雾剂)摩丝、啫哩、啫哩喷雾、乳霜、乳液或蜡。毛发喷雾还包括不含推进剂的泵喷射的气雾剂喷雾。毛发摩丝还包括不含推进剂的泵起泡的气雾剂摩丝。毛发喷雾和毛发摩丝主要包含或专门包含可水溶组分或可水分散组分。如果用在本发明的毛发喷雾或毛发摩丝中的组分是可水分散的,那么它们可以是粒子尺寸通常为1至350nm,优选为1至250nm的微分散系形式。此类制剂的固含量通常占制剂总重的0.5至20重量%。此类微分散系通常不要其它乳化剂或表面活性剂来稳定。
因此,根据本发明的组合物可以进一步包含用于保护毛发免受不利环境冲击以改善毛发健康的成分。因此,根据本发明的毛发护理组合物可以包含额外的化妆品用或皮肤用佐剂和/或添加剂(化妆品载剂),它们优选选自:
1)水
2)水溶性有机溶剂,优选地,C1-C4烷醇
3)油、脂质、蜡
4)C6-C30单羧酸与一价、二价或三价醇的与3)不同的多种酯
5)饱和的非环和环状烃类
6)脂肪酸
7)脂肪醇
8)硅油
9)表面活性成分
及其混合物。
根据本发明的毛发护理组合物可含有其它佐剂和添加剂,例如,防腐剂,抗氧化剂,硅酮,增稠剂,软化剂,阴离子、阳离子、非离子或两性乳化剂,遮光剂(screening agent),消泡剂,保湿剂,香料,表面活性剂,填充剂,掩蔽剂,阴离子、阳离子、非离子或两性聚合物或其混合物,推进剂,酸化或碱化剂,染料,着色剂,颜料或纳米颜料,光稳定剂,抗虫剂,抗菌剂,或通常被配制进毛发护理组合物中的任何其它成分。佐剂和添加剂的必需量可由本领域技术人员基于想要的产品容易地加以选择,这将在实施例中阐述,而并不限于此。
具有本发明化合物的示例性发用啫喱可以包含:
1.0.1至20wt.-%,优选1至10wt.-%的至少一种发用聚合物;
2.0至10wt.-%的至少一种载体(溶剂),其选自C2-C5醇,优选乙醇;
3.0.01至5重量%,优选0.2至3重量%的至少一种增稠剂;
4.0至50重量%的推进剂;
5.0至10重量%,优选0.1至3重量%的不同于1)的造型聚合物,优选为水溶性非离子聚合物;
6.0-1重量%的至少一种再油化剂,优选选自甘油和甘油衍生物;
7.0全30重量%的其它常规添加剂,例如硅酮组分;
8.0.005至5wt.-%的根据本发明的式(I)或式(II)化合物;
9.水,加至100wt.-%。
根据本发明的示例性的调理制剂可以包含:
1.0.05至10重量%的发用聚合物;
2.5至95wt.-%的水;
3.5至50wt.-%的表面活性剂;
4.0至5wt.-%的其它调理试剂;
5.0至10wt.-%的其它常规添加剂;
6.至多20wt.-%的根据本发明的式(I)或式(II)的化合物,
所有成分总计100wt.-%。
具有根据本发明的化合物的示例性造型组合物可以包含:
1.0.1至10wt.-%的至少一种发用聚合物;
2.20至99wt.-%的水和/或醇;
3.0至70wt.-%的至少一种推进剂;
4.0至20wt.-%的常规添加剂;
5.0.005至5wt.-%的根据本发明的式(I)或式(II)的化合物。
具有根据本发明的化合物的示例性造型啫喱可以包含:
1.0.1至10wt.-%的发用聚合物;
2.60至99.85wt.-%的水和/或醇;
3.0.05至10wt.-%的啫哩形成剂;
4.0至20wt.-%的其它常规添加剂;
5.0.005至5wt.-%的根据本发明的式(I)或式(II)的化合物。
具有根据本发明的化合物的示例性毛发护理组合物(喷雾)可以包含:
1.0.005至5wt.-%的根据本发明的式(I)或式(II)的化合物;
2.30至99.5wt.-%,优选40至99wt.-%的至少一种选自如下的溶剂:水、可与水混溶的溶剂及其混合物;
3.0至70wt.-%的推进剂;
4.0.1至10wt.-%的至少一种水溶性或水可分散的发用聚合物;
5.0至0.3重量%的至少一种水不可溶硅酮;
6.0至0.5重量%的至少一种蜡,优选地,至少一种脂肪酸酰胺;和
7.常规添加剂。
具有根据本发明的化合物的另一种毛发护理组合物可以包含:
1.0.05至20wt.-%的至少一种发用聚合物;
2.20至99.95wt%的水和/或醇;
3.0至79.5wt.-%的常规添加剂;
4.0.005至5wt.-%的根据本发明的式(I)或式(II)的化合物。
具有根据本发明的化合物的示例性气雾剂摩丝组合物可以包含:
1.0.1至10wt.-%的至少一种发用聚合物;
2.55至99.8wt.-%的水和/或醇;
3.5至20wt.-%的推进剂;
4.0.1至5wt.-%的乳化剂;
5.0至10wt.-%的常规添加剂;
6.0.005至5wt.-%的根据本发明的式(I)或式(II)的化合物。
根据本发明的毛发护理组合物可以包含至少一种其它的水溶或水可分散的发用聚合物。用于本发明的典型的发用聚合物是可商购的毛发护理(例如毛发造型)用聚合物或调理聚合物,例如乙酸乙烯酯和巴豆酸的共聚物、甲基乙烯基醚和马来酸酐的共聚物、丙烯酸或甲基丙烯酸与其他单体的共聚物、聚氨酯、N-乙烯基吡咯烷酮和硅酮聚合物。
发用聚合物的含量,基于组合物的总重,通常为按重量计约0.1至10%。本文中,优选使用水溶性或水可分散的聚氨酯,如果需要的话,该聚氨酯额外包括共聚形式的硅氧烷基团。
根据本发明的组合物可包含至少一种水不可溶硅酮,特别是聚二甲基硅氧烷,例如得自Goldschmidt的硅酮的含量,基于组合物的总重,通常为按重量计约0.0001至约2%,优选为按重量计月0.001至1%。根据本发明的优选的蜡是脂肪酸酰胺(例如芥酸酰胺)。
如果适当的话,根据本发明的毛发护理组合物还可以包括消泡剂,例如基于硅酮的消泡剂。消泡剂的含量,基于组合物的总量,通常按重量计至多0.001%。根据本发明的组合物具有如下优点:一方面它们具有所需的对毛发的抓力;另一方面所述聚合物易于洗掉(可再分散的)。通常,赋予毛发自然的外观和光泽,即使毛发本身具有非常浓密和/或乌黑的性质。
术语“醇”指通常用于化妆品中的所有醇,例如乙醇、正丙醇、异丙醇,但并不局限于此。
根据本发明其它合适的成分是化妆用佐剂和添加剂,例如,推进剂、消泡剂、表面活性成分(例如表面活性剂、乳化剂)、起泡剂和增溶剂。所用的表面活性成分可以是阴离子、阳离子、两性或中性的。其它成分可以是防腐剂、抗氧化剂、芳香油、油脂性再油化剂(lipidic refatter)、活性和/或护理成分(例如泛酰醇、胶原质、维生素、蛋白质水解产物、α和β羟基碳酸)、稳定剂、pH调理剂、遮光剂、着色剂、染料、凝胶形成剂、盐、保湿剂、复合物形成剂、粘度调理剂或遮光剂,但并不局限于此。
为了获得某些性质,毛发护理组合物还可以包括以下基于硅酮的调理化合物,所述化合物例如是聚烷基硅氧烷、聚芳基硅氧烷、聚芳基烷基硅氧烷、硅酮树脂、聚醚硅氧烷或Dimethicon Copolyole(CTFA)和氨基官能化的硅酮化合物(例如,氨二甲基硅酮(CTFA)、GP 4 Silicone和GP(Genesee))、(Dow Corning)、AFL(UnionCarbide)或EP-B 852 488中所公开的聚合物。
其它合适的成分包括硅酮Propfpolymer,其具有聚合硅酮主链和不含硅酮的侧链或者具有不含硅酮的主链和硅酮侧链,例如Silk或EP-B 852 488中公开的聚合物。
可以使用发用喷雾或气雾剂摩丝所用的典型推进剂。优选的是,丙烷/丁烷的混合物、戊烷、二甲基醚、1,1-二氟乙烷(HFC-152a)、二氧化碳、氮气或压缩空气。
气雾剂摩丝所有的乳化剂或香波制剂的表面活性剂可以是常规使用的非离子、阴离子、阳离子或两性乳化剂/表面活性剂。
非离子乳化剂的例子是(INCI命名法)Laureth类的,例如Laureth-4;Cetheth类的,例如Cetheth-1、聚乙二醇十六烷基醚;Cetheareth类的,例如cetheareth-25、聚乙二醇脂肪酸甘油酯、羟基化卵磷脂、脂肪酸的乳酸基酯、烷基聚糖苷。
非离子表面活性剂的例子是,具有6至20个碳原子的线性烷基链或支化烷基链的脂族醇或烷基酚与环氧乙烷和/或环氧丙烷的反应产物。亚烷基氧化物的含量相对于1摩尔醇为约6至60摩尔。此外,烷基胺氧化物、单烷基或二烷基烷醇酰胺、聚乙二醇的脂肪酸酯、烷基多苷或山梨聚糖醚酯也适于加入到本发明的毛发护理制剂中。
阳离子乳化剂/表面活性剂的例子是,季铵化的铵化合物,例如十六烷基三甲基氯化铵或溴化铵(INCI:西曲氯铵或西曲溴铵)、硬脂基苄基二甲基氯化铵、二硬脂基二甲基氯化铵、硬脂酰胺丙基二甲胺、羟乙基十六烷基二甲基磷酸铵(INCI:Quaternium-44)、Mono LS(INCI:椰油三甲基甲氧基硫酸铵(Cocotrimoniummethosulfate))、聚(氧-1,2-乙二基)、三-(羟基)磷酸(十八烷基次氮基)三-2,1-乙二基酯(INCIQuaternium-52)。此外,阳离子瓜尔豆衍生物,例如瓜尔豆羟丙基三甲基氯化铵(INCI)可用于调理剂和/或香波制剂。
阴离子乳化剂/表面活性剂可以选自:烷基硫酸盐、烷基醚硫酸盐、烷基磺酸盐、烷基芳基磺酸盐、烷基琥珀酸盐、烷基磺基琥珀酸盐、N-烷酰基肌氨酸盐、酰基牛磺酸盐、酰基羟乙基磺酸盐、烷基磷酸盐、烷基醚磷酸盐、烷基醚羧酸盐、α-烯烃磺酸盐、尤其是碱金属盐和碱上金属盐(如钠盐、钾盐、镁盐、钙盐)以及铵盐和三乙醇胺盐。所述烷基醚硫酸盐、烷基醚磷酸盐和烷基醚羧酸盐在分子中可以包括1至10个乙烯氧化物或丙烯氧化物单元,优选包括1至3个乙烯氧化物单元。
合适的阴离子表面活性剂是,例如,月桂基硫酸钠、月桂基硫酸铵、月桂基醚硫酸钠、月桂基醚硫酸铵、月桂酰基肌氨酸钠、油基琥珀酸钠、月桂基磺基琥珀酸铵、十二烷基苯磺酸钠、十二烷基苯磺酸三乙醇胺盐。
合适的两性表面活性剂是,例如,烷基甜菜碱、烷基酰氨基丙基甜菜碱、烷基磺基甜菜碱、烷基甘氨酸酯、烷基羧基甘氨酸酯、烷基两性乙酸酯或丙酸酯、烷基两性二乙酸酯或二丙酸酯,例如椰油二甲基磺基丙基甜菜碱、月桂基甜菜碱、椰油酰氨基丙基甜菜碱或椰油两性丙酸钠。
所有常用的啫哩形成剂都可以用作啫哩形成剂,例如微交联的聚丙烯酸(例如卡波姆(INCI))、纤维素衍生物、多糖(例如黄原胶)、癸酸/辛酸甘油三酯、丙烯酸钠共聚物、聚季铵盐-32(和)矿物油(INCI)、丙烯酸酯钠共聚物(和)矿物油(和)PPG-1 Trideceth-6、聚季铵盐-37(和)丙二醇二癸酸酯二丙烯酸酯(和)PPG-1 Trideceth-6、聚季铵盐-7、聚季铵盐-44。
为了向制剂提供光芒四射的外观或提供更华美或更多乳的产品,毛发护理组合物可以额外地包含遮光剂和/或赋予珍珠般色泽的物质,例如羧酸的脂肪酸盐或盐、含有阳离子的阳离子聚合物、二甲基硅酮(INCI)或氨基二甲基硅酮(INCI)。
常规添加剂为例如长链脂肪醇,如鲸蜡醇、硬脂醇、鲸蜡硬脂醇、二甲基十八胺。此外,毛发护理组合物可以包含脂质,例如二甲基硅酮、氨基二甲基硅酮、矿物油、或硅酮衍生物(例如二甲基硅酮共聚醇)。
本发明还提供了上述组合物在用于防止毛发变灰白、用于恢复和/或保持自然的毛发颜色、和/或用于修复和/或增强毛发生长中的用途。
更优选地,本发明提供了上述组合物在用于防止毛发变灰白、用于恢复和/或保持自然的毛发颜色、和/或用于修复和/或增强毛发生长中的用途。
式(I)或式(II)的化合物,特别是式(III)的藤黄酰胺可用在哺乳动物中用于防止毛发变灰白、用于恢复和/或保持自然的毛发颜色。
根据本发明的式(I)或式(II)的化合物在防止毛发变灰白、用于恢复和/或保持自然的毛发颜色中的使用功效在实施例中举例说明、或者通过下面的过程示出:
作为参照(对照),从头皮上整齐地剪切含有约100根毛发的一绺毛发。从根部到末梢测量该绺毛发的颜色。这可以通过下列方法来进行:1)目视评分,2)用高密度图片文件并评分3)在毛发降解和黑色素提取之后,通过色素分析并确定毛发中的黑色素含量。在后一种情况下,可以通过光度法或者通过化学反应测量黑色素,所述化学反应即为:由真黑色形成吡咯-2,3,5-三羧酸,形成褐黑素用的氨基羟基苯丙氨酸异构体,随后进行定量的色谱分析、光谱分析或分光光度分析。
随后将含有优选量的式(I)或式(II)的化合物的局部用组合物的样品(2-10mL或mg/cm2,取决于制剂的类型;优选为免洗产品,例如生发油、乳液或乳霜)涂覆到头皮上,每天至少一次,通常为每天1到4次,连续使用至少3个月,具体为6个月(因为毛发的生长速率为约1cm/月),并且在头皮上按摩使其均匀分布。涂覆之后产品不需要洗掉。在处理期的最后,从头皮的相同位置取第二毛发样品,并按上述方法分析。
比较处理期之前和之后的黑色素含量、毛发颜色或灰白程度。
在另一个实施方式中,本发明进一步提供了根据本发明的化妆品组合物的用途,其中如上面所定义的组合物进一步包含至少一种额外的活性物质,选自由下面所述的抗氧化剂、遮光剂、着色剂和生物活性剂组成的组。
因而,根据本发明的式(I)或式(II)的化合物可以与其他成分组合使用,以保护毛发免受不利环境冲击并改善毛发健康。
抗氧化剂
基于本发明,可以使用通常配制进毛发护理组合物中的所有已知抗氧化剂。尤其优选的是选自下述组的抗氧化剂,所述组由氨基酸(例如,甘氨酸、组氨酸、酪氨酸、色氨酸)及其衍生物、咪唑(例如,尿刊酸)和衍生物、肽(例如D,L-肌肽、D-肌肽、L-肌肽和衍生物(例如,鹅肌肽))、类胡萝卜素、胡萝卜素(例如,α-胡萝卜素、β-胡萝卜素、番茄红素)和衍生物、绿原酸和衍生物、硫辛酸和衍生物(例如,二羟基硫辛酸)、金硫代葡萄糖、丙基硫脲嘧啶和其它硫醇(例如,硫氧还蛋白、谷胱甘肽、半胱氨酸、胱氨酸、胱胺和其糖基-、N-乙酰基-、甲基-、乙基-、丙基-、戊基-、丁基-和月桂基-、棕榈基-;油基-、y-6,7,9,10-十八碳二烯-1-基-(y-linoleyl)、胆甾醇基-和甘油基的酯)及其盐、硫代二丙酸二月桂酯、硫代二丙酸二硬脂酯、硫代二丙酸及其衍生物(酯、醚、肽、脂质、核苷酸、核苷和其盐)以及非常低的相容剂量的(例如,pmol/kg~μmol/kg)亚砜胺(sulfoximine)化合物(例如,丁硫氨酸亚砜胺(buthionine sulfoximine)、高半胱氨酸亚砜胺、丁硫氨酸砜(buthioninsulfone)、五、六、七硫堇亚砜胺)、额外地(金属)-螯合剂(例如,α-羟基脂肪酸、棕榈酸、肌醇六磷酸、乳铁蛋白)、β-羟基酸(例如,柠檬酸、乳酸、苹果酸)、腐殖酸(huminic acid)、五倍子酸、五倍子提取物(gallic extracts)、胆红素、胆绿素、EDTA、EGTA及其衍生物、不饱和脂肪酸和其衍生物(例如,γ-亚油酸、亚油酸、油酸)、叶酸及其衍生物、泛醌和泛醌醇及其衍生物、维生素C和衍生物(例如,棕榈酸抗坏血酸酯和四异棕榈酸抗坏血酸酯、抗坏血酸磷酸Mg、抗坏血酸磷酸Na、抗坏血酸乙酸酯)、生育酚和衍生物(例如,维生素-E-乙酸酯)、天然维生素E的混合物)、维生素A和衍生物(维生素-A-棕榈酸酯和乙酸酯)以及松柏基苯甲酸酯、芸香亭酸和衍生物、α-糖基芸香苷、阿魏酸、亚糠基葡萄糖醇、肌肽、丁基羟基甲苯、丁基羟基苯甲醚、三羟基丙基苯基甲酮、脲和其衍生物、甘露糖和衍生物、锌和衍生物(例如,ZnO、ZnSO4)、硒和衍生物(例如,硒代蛋氨酸)、芪和衍生物(例如,芪氧化物、反式芪氧化物)和所述活性成分的合适衍生物(盐、酯、醚、糖、核苷酸、核苷、肽和脂类)构成。一种或多种防腐剂/抗氧化剂可以以本发明组合物总重的至少0.01重量%的量存在。优选地,存在本发明组合物总重的大约0.01重量%至大约10重量%。最优选地,一种或多种防腐剂/抗氧化剂以大约0.1重量%至大约1重量%的量存在。
遮光剂
遮光剂可有利地选自UV-A、UV-B、UV-C和/或广谱滤光剂(filter)。UV-B或广谱遮光剂(即在约290和340nm之间具有最大吸光率的物质)的例子可以是有机和无机化合物。有机UV-B或光谱遮光剂是,例如,丙烯酸酯,例如2-氰基-3,3-二苯基丙烯酸2-乙基己基酯(氰双苯丙烯酸辛酯(octocrylene),340),2-氰基-3,3-二苯基丙烯酸乙酯等等;樟脑衍生物,例如4-甲基亚苄基樟脑3-亚苄基樟脑、甲基硫酸樟脑苯甲烷铵(camphor benzalkoniummethosulfate)、聚丙烯酰胺基甲基亚苄基樟脑、磺基亚苄基樟脑、磺基甲基亚苄基樟脑、对苯二亚甲基二樟脑酰胺磺酸等等;肉桂酸酯衍生物,例如甲氧基肉桂酸辛酯甲氧基肉桂酸乙氧基乙基酯、甲氧基肉桂酸二乙醇胺酯甲氧基肉桂酸异戊酯等等,以及键合到硅氧烷上的肉桂酸衍生物;对氨基苯甲酸衍生物,例如对氨基苯甲酸、对二甲基氨基苯甲酸2-乙基己基酯、N-氧丙烯化的对氨基苯甲酸乙酯、对氨基苯甲酸甘油酯;二苯甲酮,例如二苯甲酮-3、二苯甲酮-4、2,2′,4,4′-四羟基-二苯甲酮、2,2′-二羟基-4,4′-二甲氧基二苯甲酮等等;亚苄基丙二酸酯,例如4-甲氧基亚苄基丙二酸二-(2-乙基己基)酯;2-(4-乙氧基-苯胺亚甲基)丙二酸的酯,例如欧洲专利公开文本EP 0895 776中所述的2-(4-乙氧基-苯胺亚甲基)丙二酸二乙酯;如欧洲专利公开文本EP 0358584B1、EP 0538431B1和EP 0709080A1中所述的含有苯丙二酸基的有机硅氧烷化合物,例如聚硅酮-15甲酚曲唑三硅氧烷(Drometrizole trisiloxane(Mexoryl XL));咪唑衍生物,例如2-苯基苯并咪唑磺酸及其盐2-苯基苯并咪唑磺酸的盐是,例如,碱金属盐(如钠盐或钾盐),铵盐,吗啉盐,伯、仲和叔胺盐(例如单乙醇胺盐、二乙醇胺盐)等等;水杨酸酯衍生物,例如水杨酸异丙基苄酯、水杨酸苄酯、水杨酸丁酯、水杨酸辛酯(EHS,NEO HeliopanOS)、水杨酸异辛酯或水杨酸3,3,5-三甲基环己酯(胡莫柳酯(homosalate),EHS,Helipan OS)等等;三嗪衍生物,例如辛基三嗪酮(Uvinul T-150)、二辛基丁酰胺基三嗪酮(Uvasorb HEB)。胶囊化的UV滤光剂,例如胶囊化的甲氧基肉桂酸乙基己酯(Eusolex UV-珍珠)或负载有UV滤光剂的微胶囊,如EP 1471995中所公开的等等。无机化合物是颜料,例如微粒化的ZnO、TiO2等等。术语“微粒化的”是指从约5nm到约200nm,特别是从约15nm到约100nm的颗粒尺寸。TiO2颗粒还可被金属氧化物(例如氧化铝或氧化锆)或有机涂层(例如多元醇、甲基硅酮、硬脂酸铝、烷基甲硅烷)包覆。这类涂层是本领域公知的。
广谱遮光剂或UV-A遮光剂(即,在约320至400nm间具有最大吸光率的物质)的例子可以是有机和无机化合物,例如,二苯甲酰甲烷衍生物,例如4-叔丁基-4’-甲氧基二苯甲酰甲烷二甲氧基二苯甲酰甲烷、异丙基二苯甲酰甲烷等等;苯并三唑衍生物,例如2,2’-亚甲基-二(6-(2H-苯并三唑-2-基)-4-(1,1,3,3-四甲基丁基)-苯酚(TINOSORBM)等等;二-乙基己基氧苯酚甲氧苯基三嗪(Tinosorb S)等等;亚苯基-1,4-二苯并咪唑磺酸或其盐,例如2,2-(1,4-亚苯基)-二(1H-苯并咪唑-4,6-二磺酸)(Neoheliopan AP);经氨基取代的羟基二苯甲酮,例如欧洲专利公开文本EP 1046391中描述的2-(4-二乙氨基-2-羟基苯甲酰基)-苯甲酸己酯(Uvinul A plus);在国际专利公开文本WO2005080341A1中所描述的离子性UV-A滤光剂。颜料,例如微粒化的ZnO或TiO2等等。术语“微粒化的”是指从约5nm到约200nm,特别是从约15nm到约100nm的颗粒尺寸。TiO2颗粒还可被金属氧化物(例如氧化铝或氧化锆)或有机涂层(例如多元醇、甲基硅酮、硬脂酸铝、烷基甲硅烷)包覆。这类涂层是本领域公知的。
因为二苯甲酰甲烷衍生物具有有限的光稳定性,因此可能需要对这些UV-A遮光剂加以光稳定。因此,术语“常规UV-A掩蔽剂”也指经下述物质稳定的二苯甲酰甲烷衍生物(例如,),所述物质例如为,欧洲专利公开文本EP A-0514491B1和EP A-0780119A1中所描述的3,3-二苯基丙烯酸酯衍生物;US专利No.5605680中所描述的亚苄基樟脑衍生物;欧洲专利公开文本EP 0358584B1、EP 0538431B1和EP0709080A1中所描述的含有苯丙二酸酯基团的有机硅氧烷化合物。
着色剂
一般而言,为了使根据本发明的毛发护理产品着色,在电磁辐射的可见光(400-4000nm)下具有吸收率的所有物质都是合适的。通常如下发色团引起吸收:偶氮-、(一、二、三或多)茋-、类胡萝卜素-、二芳基亚甲基-、三芳基亚甲基-、氧杂蒽-、吖啶-、喹啉-、次甲基-(也可以为多次甲基)噻唑-、吲达胺-、靛酚-、吖嗪-、噁嗪-、噻嗪-、蒽醌-、靛青-、酞氰染料以及其它合成、天然和/或无机发色团。
可用于本发明的毛发护理产品中的FD&C(美国联邦食品、药品和化妆品法)和D&C例如是,姜黄色素、核黄素(riboflavin)、核黄素(1actofiavin)、酒石黄、喹啉黄(chinolinyellow)、胭脂虫红铝、偶氮玉红、紫红色、鲜红色4R、赤藓红、红2G、靛青、叶绿素、叶绿酸、焦糖、药用碳、类胡萝卜素、胡萝卜素、胭脂树橙、降红木素、橙红、胭脂树果肉色质(orlean)、辣椒红、辣椒红玉素、番茄红素、叶黄素(flavoxanthin)、毛莨黄素、叶黄素(lutein)、隐黄素(kryptoaxanthin)、玉红黄质、紫黄质、枚红黄质、斑蝥黄、甜菜苷、花色甙,但并不局限于此。染料的例子是,例如,无机颜料,例如氧化铁(氧化铁红、氧化铁黄、氧化铁黑等)、蓝色颜料、氧化铬绿或碳黑。可用本发明的稳定组合物稳定的其它着色剂和染料包括天然或合成的有机颜料、可以溶于溶剂中的分散染料(如HC型直发染料,例如HC红No.3、HC黑No.2和International Cosmetic Ingredient Dictionary Handbook 7thedition 1997中所列举的所有其它发用染料或Color Index InternationalSociety of Dyers and Colorist中所列举的分散染料、有色清漆(可溶染料的不溶盐,如阴离子染料的Ca盐、Ba盐或Al盐)、可溶的阴离子或阳离子染料(例如酸性染料(阴离子)、碱性染料(阳离子))、直接染料、反应性染料或溶剂染料、荧光染料、荧光素和异硫氰酸酯。
生物活性剂
生物活性剂有利地选自黑色素生成用的一般活化剂,例如酪氨酸酶激活剂、肽类激素、cAMP-活化剂和神经营养因子。
优选的酪氨酸酶激活剂是增大酪氨酸酶表达或酶活性的任何物质,例如来自甘草的甘草甜素。
属于黑皮质素组的肽类激素是优选的肽类激素,包括ACTH、α-MSH、β-MSH和γ-MSH;这些肽是所谓的促阿片-黑素细胞皮质素原(POMC)的大前体肽的分裂产物。α-MSH是用于着色的最重要的黑皮质素。促黑素细胞激素(被统称为MSH或促黑激素)由脑下垂体的垂体中叶细胞自然产生的一类肽激素。它们刺激皮肤和毛发中的黑素细胞产生并释放黑色素(黑色素生成)。因此,它们将有利地与本发明的化合物组合。
本发明进一步涉及一种用于防止毛发变灰白、和/或用于恢复和/或保持自然的毛发颜色、和/或用于修复和/或增强毛发生长的方法,所述方法包括下列步骤:将包含有效量的式(I)或式(II)化合物的局部用组合物涂覆到具有人类毛发的皮肤上。
术语“具有毛发的皮肤”指的是具有毛发的所有皮肤部分,例如特别是头皮和脸(睫毛、眉毛、胡须)。最优选地,将局部用组合物涂覆到人(任何年龄的男人或女人)的头皮上。
在根据本发明的方法中使用的“有效量”指的是获得生理效应所需的量。生理效应可以通过单剂量或多剂量实现。当然施用的剂量可以根据已知的因素(例如具体组合物的生理特性以及给药模式和途径;受试者的年龄、健康和重量;症状的性质和程度;并行处理的类型;处理的频率;和/或期望的效果)变化,并且可由本领域技术人员调整。
术语″有效量”通常表示基于局部用组合物的总重至少0.00001wt.-%。优选地,基于局部用组合物的总重,局部用组合物以0.00001wt.-%到20wt.-%的量、最优选以0.0001wt.-%到1wt.-%的量包含根据本发明的式(I)或式(II)的化合物。
优选地,局部用组合物每天涂覆至少两次,例如早晨一次,晚上一次。
在本文中使用时,术语“局部用组合物”指的是适合局部涂覆于哺乳动物角质组织(例如具有毛发的皮肤)、特别是涂覆于人类头皮的任何组合物。特别地,局部用组合物是毛发护理组合物,例如调理剂、处理剂、生发油、造型啫喱、摩丝、香波、毛发喷雾、润发油、造型霜、染色和持久卷发组合物。本发明的目的中特别感兴趣的是生发油、调理剂、处理剂、造型啫喱(可以是啫喱、乳液、酊剂、喷雾、摩丝、漂白组合物或泡沫的形式),可以根据个人需要来涂覆,例如作为乳液、酊剂、摩丝或喷雾每天一次;或者作为调理剂或处理剂每周一次或两次。
根据本发明的用于防止毛发变灰白、和/或用于恢复和/或保持自然的毛发颜色、和/或修复和/或增强毛发生长的方法中使用的局部用组合物可以进一步包含常用于局部用组合物的其他成分,例如5,6-二羟基吲哚啉HBr、与2-甲基间苯二酚和/或精氨酸组合的5,6-二羟基吲哚啉HBr。
本发明进一步提供了如本发明所述的式(I)或式(II)的化合物用于增加毛囊中黑素细胞的总数和/或用于增大黑素细胞从毛鞘向毛基质分化和迁移中的用途。
毛囊中黑素细胞的数量可以通过标准方法来评估,例如用全黑素细胞(pan-melanocyte)标记物NKI-beteb对黑素细胞进行免疫组织化学染色,随后计数NKI-beteb+细胞。
黑素细胞从毛鞘向毛基质分化和迁移可以通过下列方法测量:将毛囊中的c-kit+黑素细胞免疫组织化学染色,随后评估其在毛囊内的分布。
通过以下非限制性实施例以进一步阐述本发明。
实施例
实施例1:藤黄酰胺对所培养毛囊的影响
从随意选择的面部手术干预中得到处于毛发周期的生长阶段(生长期anagen)的含有人发毛囊的组织。根据本领域已确立的方法(Philpott et al.1990,J Cell Sci.97:463-471)分离毛囊并将其保留在培养基中。在7天的培养时间内,每隔一天以不同的浓度(介于10纳摩尔和1微摩尔之间,与之相比对照组不添加GA)将藤黄酰胺(GA)施用于经着色的所培养的毛发生长初期VI毛囊。
测量毛干伸长作为评估GA的可能毛发生长促进或抑制效应的方法。在介于0.1和1微摩尔之间的浓度下,与对照组相比时,即使观察到涂覆GA没有毛发周期的发展也测出了毛干伸长的增加。在浓度高达1微摩尔时,未观察到中毒的迹象。因此从第一个观察结果中可以推断出,GA可以使用的剂量范围介于10纳摩尔和1微摩尔之间,GA可以用作毛发生长促进剂或修复剂。
毛囊色素的宏观分析显示出在7天的培养时间对照组中有效的色素沉着的缓慢减少(体外变灰白)。在介于0.1和1微摩尔之间的GA的浓度下,观察到毛囊色素沉着明显且显著的改善了,GA能有效地在所培养的生长初期毛囊中维持毛囊色素沉着。
根据标准方法进行毛囊的免疫组织化学分析。使用全黑素细胞标记物NKI-beteb和增殖标记物Ki67的免疫组织化学染色来估算GA存在下所培养的毛囊中黑素细胞的总数。当GA以介于0.1和0.5微摩尔之间的浓度使用时,保持在毛发周期的生长初期的毛囊中的黑素细胞的总数增加。该增加是剂量依赖性的。该观察显示了GA对着色单元的加强维护以及外根鞘中黑素细胞库的动员。
使用Trp2作为黑素细胞前体用的标记物,我们发现对照组毛囊中Trp2+黑素细胞的数量较高。这些细胞主要在着色单元中发现,这表明在该隔间中有大量残留的黑素细胞前体。用cKit示踪得到的结果证实了这些结果,cKit是迁移、活化的早期黑素细胞的标记物,在用0.1和1微摩尔GA处理的毛囊中最明显地发现了迁移、活化的早期黑素细胞。
结果归纳在下面的表1中:
实施例2:去头屑香波
INCI命名法 | 重量% |
水 | 添加至100 |
十二烷基醚硫酸铵 | 35.00 |
十二烷基硫酸铵 | 15.00 |
乙二醇二硬脂酸酯 | 1.00 |
二甲基硅酮 | 1.00 |
鲸蜡醇 | 0.50 |
椰油酰胺MEA | 3.00 |
ZPT | 1.00 |
瓜尔豆羟丙基三甲基氯化铵 | 0.20 |
氢化聚癸烯 | 1.00 |
聚季铵盐10 | 0.10 |
PEG 7m | 0.50 |
三羟甲基丙烷三辛酸/三癸酸酯 | 1.00 |
防腐剂 | 适量 |
香精 | 0.30 |
E 104,E 110,E 132 | 0.02 |
根据本发明的式(I)或式(II)化合物,例如特别是藤黄酰胺 | 0.01 |
组合所有成分并猛烈混合,直到得到均一的溶液。最后在缓慢搅拌下加入水,并等待,直到泡沫消失。
实施例3:调理香波
INCI命名法 | 重量% |
水 | 添加至100 |
十二烷基醚硫酸钠 | 25.00 |
椰油酰胺丙基甜菜碱 | 5.00 |
氯化钠 | 2.50 |
乙二醇二硬脂酸酯 | 1.00 |
甘油 | 2.00 |
二甲基硅酮 | 0.50 |
香精 | 0.50 |
椰油-葡萄糖苷 | 3.00 |
卡波姆 | 0.10 |
精氨酸 | 0.05 |
油酸甘油酯 | 0.05 |
硬脂酸甘油酯 | 1.00 |
瓜尔豆羟丙基三甲基氯化铵 | 0.10 |
泛酰醇 | 1.00 |
EDTA二钠 | 0.05 |
防腐剂 | 适量 |
水解角蛋白 | 0.10 |
柠檬酸/氢氧化钠 | 适量 |
根据本发明的式(I)或式(II)化合物,例如特别是藤黄酰胺 | 0.005 |
E 102,E 110,FD&C蓝 | 0.01 |
组合所有成分并猛烈混合,直到得到均一的溶液。最后在缓慢搅拌下加入水,并等待,直到泡沫消失。然后小心地加入增稠剂(例如氯化钠)。
实施例4:含植物提取物的香波
INCI命名法 | 重量% |
水 | 添加至100 |
十二烷基醚硫酸钠 | 25.00 |
十二烷基葡糖苷 | 10.00 |
椰油酰胺丙基甜菜碱 | 5.00 |
丙二醇 | 2.0 |
香精 | 1.25 |
柠檬酸钠 | 0.25 |
苯甲酸钠 | 0.20 |
泛酰醇 | 1.00 |
甲酸钠 | 0.20 |
聚季铵盐-10 | 0.20 |
羟丙基瓜尔豆羟丙基三甲基氯化铵 | 0.05 |
PEG-35蓖麻油 | 1.00 |
海盐(Maris sal) | 1.25 |
聚山梨醇酯20 | 1.00 |
乙酸生育酚酯 | 0.20 |
Prunus armeniaca(Apricot)水果提取物 | 0.20 |
Echinacea purpurea提取物 | 0.05 |
棕榈酸视黄酯 | 0.05 |
生育酚 | 0.05 |
亚油酸 | 0.20 |
防腐剂 | 1.00 |
根据本发明的式(I)或式(II)化合物,例如特别是藤黄酰胺 | 0.01 |
CI 77891 | 0.02 |
组合所有成分并猛烈混合,直到得到均一的溶液。最后在缓慢搅拌下加入水,并等待,直到泡沫消失。
实施例5:闪亮香波
INCI命名法 | 重量% |
水 | 添加至100 |
十二烷基醚硫酸钠 | 15.00 |
椰油两性二乙酸二钠 | 15.00 |
氯化钠 | 2.00 |
乙二醇二硬脂酸酯 | 1.00 |
椰油酰胺基丙基PYL甜菜碱 | 2.00 |
月桂基二甲基铵羟丙基水解的小麦蛋白 | 1.00 |
PEG-12二甲基硅酮 | 1.00 |
瓜尔豆羟丙基三甲基氯化铵 | 0.05 |
水解的小麦蛋白 | 0.20 |
Laureth-4 | 1.00 |
椰油酸PEG-7甘油酯 | 2.00 |
氢化蓖麻油 | 1.00 |
Laureth-2 | 0.50 |
PEG-55丙二醇油酸酯 | 2.00 |
丙二醇 | 2.00 |
云母 | 0.20 |
柠檬酸 | 0.01 |
香精 | 1.00 |
E 110,E 104,E 122 | 0.05 |
根据本发明的式(I)或式(II)化合物,例如特别是藤黄酰胺 | 0.05 |
组合所有成分并猛烈混合,直到得到均一的溶液。最后缓慢搅拌下加入水,并等待,直到泡沫消失。然后小心地加入增稠剂(例如氯化钠)。
实施例6:用于色彩保护的水合香波
加入部分1中的所有成分,猛烈混合,直到获得均一的溶液。然后,在缓慢搅动下加水,等待,直到泡沫消失。然后小心地加入增稠剂,例如氯化钠或Crothix LVR。
实施例7:超级闪亮活力发膏
在适度搅动下,将部分1和部分2分别加热至65℃。当其具有同样的温度时,在搅动下将部分2加入到部分1中。令其冷却至40℃,在搅动下加入部分3,均质。冷却至环境温度。
实施例8:毛发修复处理
将部分A加热到70℃。搅拌下将部分A加入部分B中并均质。在中等搅拌下,将混合物添加至部分C中并均质,并且使其冷却。
实施例9:颜色膏
将部分A加热到70℃。搅拌下将部分A加入部分B中并均质。搅拌下加入部分C。
实施例10:丝滑毛发混合物
分别将部分A和部分B加热到70℃。将部分A加入部分B中并均质。搅拌下冷却。
实施例11:油润光彩保湿剂
分别将部分A和部分B加热到70℃。将部分A加入部分B中并均质。搅拌下加入部分C。
实施例12:高光定型膏
分别将部分A和部分B加热到70℃。将部分A加入部分B中并均质。搅拌下加入部分C。
实施例13:发用啫哩
加入部分1的所有成分,猛烈混合,直到获得均质啫哩。
实施例14:发用啫哩
加入部分1的所有成分,猛烈混合,直到获得均质啫哩。
实施例15:发用啫哩
加入部分1的所有成分,猛烈混合,直到获得均质啫哩。
实施例16:沐浴油
组合部分1的所有成分,猛烈混合,直到获得均质溶液。
实施例17:半永久的染发制剂
将部分1和部分2加热到70℃。搅拌下将部分2加入部分1中。然后加入部分3。
实施例18:永久的染发制剂
INCI命名法 | 重量% | |
A | 鲸蜡硬脂醇 | 9.00 |
鲸蜡硬脂醇硫酸钠 | 3.00 | |
硬脂酸甘油酯 | 2.50 | |
月桂醇聚醚-2 | 2.00 | |
硬脂酰胺MEA-硬脂酸酯 | 0.75 | |
PEG-5椰油酰胺 | 0.50 | |
油酸 | 0.50 | |
染发剂 | 0.30 | |
B | 水 | 添加至100 |
硫酸铵 | 2.00 | |
亚硫酸钠 | 0.50 | |
EDTA二钠 | 0.05 | |
根据本发明的式(I)或式(II)化合物,例如特别是 | 0.1 |
藤黄酰胺 | ||
抗坏血酸 | 0.50 | |
氢氧化铵 | 2.50 |
部分II
INCI命名法 | 重量% | |
A | 鲸蜡硬脂醇 | 6.00 |
B | 水 | Ad 100 |
过氧化氢 | 9.00 | |
十二烷基硫酸钠 | 3.00 | |
磷酸氢二钠 | 0.15 | |
磷酸 | pH 2.0 |
将部分I的A相和B相加热到70℃。搅拌下将A相加入B相中。将pH调节为11.2。
分别将部分II的A相和B相加热到70℃。搅拌下将A相加入B相中。调节pH。
使用前组合部分I和II。
实施例19:药用香波
部分I
部分II
INCI命名法 | 重量% | |
A | 十二烷基醚硫酸钠 | 44.50 |
羟苯乙酯 | 0.20 |
将根据本发明的式(I)或式(II)化合物(特别是藤黄酰胺)溶于水,加入甲基纤维素并搅拌,直到溶解;使羟苯乙酯与十二烷基醚硫酸钠混合。
混合部分1和部分2
实施例20:清洁香波
加入部分1)和部分2)中的所有成分,猛烈混合,直到获得均一的溶液。然后,在缓慢搅动下加水,等待,直到泡沫消失。最后,小心地加入增稠剂,例如氯化钠或Crothix LVR。
实施例21:水合香波(hydrating shampoo)
加入所有成分,猛烈混合,直到获得均一的溶液。然后,在缓慢搅动下加水,等待,直到泡沫消失。小心地加入增稠剂,例如氯化钠或CrothixLVR。
Claims (15)
2.如权利要求1所述的化妆品组合物,其中,R1为氢,R2为饱和的、直链的或支化的C1-C8烷基
3.如权利要求1或2中任意一项所述的化妆品组合物,其中,R1和R2均为氢,并且包括所有可能的立体异构体。
5.一种化妆品组合物,其包含含有藤黄酸和/或藤黄酰胺的粗制藤黄树脂和来自Garcinia handburryi树的树脂的提取物。
6.如权利要求1至5中任意一项所述的化妆品组合物,其额外地包含常用于化妆品组合物的载体。
7.如权利要求1至6中任意一项所述的化妆品组合物,其中,基于所述组合物的总重,权利要求1和4所描绘的式(I)、式(II)、或式(III)化合物的含量为约0.00001重量%、优选0.0001重量%到约20重量%、优选到约1重量%。
8.权利要求1至7中任意一项所述的组合物在用于防止毛发变灰白、用于恢复和/或保持自然的毛发颜色、和/或用于修复和/或增强毛发生长中的用途。
9.如权利要求8所述的用途,其中,如权利要求1至7中任意一项所定义的组合物进一步包含至少一种选自由抗氧化剂、遮光剂、着色剂和生物活性剂组成的组中的额外的活性物质。
10.一种用于防止毛发变灰白、和/或用于恢复和/或保持自然的毛发颜色、和/或用于修复和/或增强毛发生长的方法,所述方法包括下列步骤:将包含有效量的权利要求1所描绘的式(I)或式(II)化合物的局部用组合物涂覆到具有人类毛发的皮肤上。
11.如权利要求10所述的方法,其中,所述式(I)或式(II)的化合物是如权利要求4所描绘的藤黄酰胺、或来自Garcinia handburryi树的树脂的提取物。
12.如权利要求10或11所述的方法,其中,基于所述局部用组合物的总重,所述式(I)或式(II)的化合物的有效量选自0.00001wt.-%到20wt.-%的范围内。
13.如权利要求10至12中任意一项所述的方法,其中,基于所述局部用组合物的总重,所述式(I)或式(II)的化合物的有效量选自0.0001wt.-%到1wt.-%的范围内。
14.如权利要求10至13所述的方法,其中,所述局部用组合物是选自生发油、处理剂、调理剂或造型啫喱的毛发护理组合物。
15.权利要求1至7中任意一项所述的组合物或化合物在用于增加毛囊中黑素细胞的总数和/或用于增大黑素细胞从毛鞘向毛基质分化和迁移中的用途。
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EP10159608 | 2010-04-12 | ||
EP10159608.8 | 2010-04-12 | ||
PCT/EP2011/055724 WO2011128339A1 (en) | 2010-04-12 | 2011-04-12 | Hair treatment composition containing gambogic acid, ester or amide |
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CN102844017A true CN102844017A (zh) | 2012-12-26 |
CN102844017B CN102844017B (zh) | 2015-10-21 |
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Country Status (4)
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US (1) | US9445979B2 (zh) |
EP (1) | EP2558055B1 (zh) |
CN (1) | CN102844017B (zh) |
WO (1) | WO2011128339A1 (zh) |
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CN102603767A (zh) * | 2012-03-07 | 2012-07-25 | 广州牌牌生物科技有限公司 | 一种藤黄酸分离纯化生产工艺 |
CN112174978B (zh) * | 2020-09-29 | 2022-05-20 | 中国药科大学 | 一种能改善长循环的基于疏水性前药的藤黄酸纳米制剂 |
WO2023274774A1 (en) * | 2021-07-01 | 2023-01-05 | Unilever Ip Holdings B.V. | Hair care composition |
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EP2558055A1 (en) | 2013-02-20 |
WO2011128339A1 (en) | 2011-10-20 |
US9445979B2 (en) | 2016-09-20 |
CN102844017B (zh) | 2015-10-21 |
EP2558055B1 (en) | 2016-08-17 |
US20130195777A1 (en) | 2013-08-01 |
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