CN101442981A - 增强水溶性活性物质渗透的方法 - Google Patents
增强水溶性活性物质渗透的方法 Download PDFInfo
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- CN101442981A CN101442981A CNA2007800175907A CN200780017590A CN101442981A CN 101442981 A CN101442981 A CN 101442981A CN A2007800175907 A CNA2007800175907 A CN A2007800175907A CN 200780017590 A CN200780017590 A CN 200780017590A CN 101442981 A CN101442981 A CN 101442981A
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Abstract
本发明描述了一种将水溶性护肤活性物质递送到角质组织中的方法,所述方法包括将包含水相和非水相的油包水乳液施用到角质组织上的步骤,其中所述水相包含水溶性护肤活性物质,并且在对所述组合物施用剪切应力时,所述水相与非水相视觉上分开。
Description
发明领域
本发明涉及个人护理组合物和使用它们的方法,所述方法增强水溶性活性物质向皮肤中的递送。
发明背景
有多种产品可供消费者使用以提供皮肤护理有益效果和消除大多数人认为不可取的“皮肤老化迹象”,如细纹、皱纹和不均匀皮肤肌理。为达到最佳效果,有些产品必须有规律地和在长期地施用。这在当产品旨在提供一种慢性或长期有益效果时可能尤其重要。为了鼓励经常使用,重要的是产品在施用时具有令人期望的感觉,并且也提供产品具有其预期效果的某些指示(也就是,即时有益效果)。因此,存在对提供某种个人护理组合物的持续需求,这种个人护理组合物提供直接有益效果,因此鼓励重复使用以提供长期有益效果。此外,存在对提供某种组合物的持续需求,这种组合物更有效地将活性成分递送到角质组织中以提供长期有益效果。
发明概述
本发明符合上述需求,并且描述了乳液形式的组合物,所述组合物在受到剪切力(例如,通过将所述组合物施用到皮肤上)时释放出含水相。所述组合物在施用时提供一种如水的清新感觉,并且留给消费者丝绸般柔和的用后感觉,这可以鼓励重复使用和有规律地使用所述产品。此外,申请人认为这些组合物增强了水溶性活性成分向皮肤中的递送和渗透。不受理论的限制,据信施用时,当所述组合物被施用到角质组织上时,水相结合成小滴。水溶性护肤活性物质将主要分布在水相中。在水相中,活性物质可以变得在水滴中浓度更高,并且产生有益于活性物质增强渗透到皮肤中的浓度梯度。人们通常认为,许多护肤活性物质增强渗透到皮肤中的结果将是增大活性物质的功效。
依照本发明的一个实施方案,提供了一种增强水溶性护肤活性物质向角质组织中的递送的方法,所述方法包括以下步骤:向角质组织上施用一种包含水相、非水相和至少一种水溶性护肤活性物质的油包水乳液。在对所述组合物施用剪切应力时,水相与非水相视觉上分开。
依照本发明的一个实施方案,提供了一种增强护肤活性物质向角质组织中的递送的方法,所述方法包括以下步骤:向角质组织上施用一种组合物,所述组合物包含:约0.1%至约15%的非乳化性交联的硅氧烷弹性体;约0.1%至约15%的乳化性交联的硅氧烷弹性体;约1%至约40%的非乳化性和乳化性交联的硅氧烷弹性体的溶剂;皮肤病学可接受的载体;和至少一种水溶性护肤活性物质,所述活性物质选自由下列组成的组:维生素B化合物、维生素C化合物、肽和肽衍生物、糖胺、控油剂、抗氧化剂前体、自由基清除剂、防晒剂、蛋白酶抑制剂、亮肤剂、免晒美黑剂、以及它们的混合物。
发明详述
本发明描述了一种以可见的水释放形式为消费者提供即时护肤有益效果同时通过增强水溶性护肤活性物质向角质组织中的递送来提供长期有益效果的方法。所述组合物可用于多种个人护理产品中,所述个人护理产品的非限制性实例包括保湿剂、调理剂、清洁剂、防晒剂、抗衰老化合物、以及它们的组合。所述组合物可为多种形式,包括但不限于乳液、洗剂、固体制剂、霜膏、凝胶、摩丝、油膏剂、糊剂、血清、棒状物等。
在本发明的所有实施方案中,除非另外特别说明,所有百分比均按所述总组合物的重量计。除非另外特别说明,所有比率均为重量比率。所有范围是包括界限的和可合并的。有效数字的数目既不表示对所指示量的限制,也不表示对测量精确性的限制。除非另外特别说明,所有数值应理解为被词“约”修饰。所有测量均被理解为是在25℃和环境条件下进行的,其中“环境条件”是指在约一个大气压和约50%相对湿度下的条件。除非另外指明,所有与所列成分相关的上述重量均基于活性物质的含量,并且不包括可能包含在可商购获得的材料中的载体或副产物。
本文中的“个人护理组合物”是指适于局部施用到哺乳动物角质组织上的组合物。本文所用的“护肤活性物质”或“活性物质”是指当涂敷到皮肤上时可向皮肤提供有益效果或改善的化合物。应当理解,护肤活性物质不仅可用于施用到皮肤上,而且可用于毛发、指/趾甲以及其它哺乳动物角质组织。
本文中的“稳定”和“稳定性”是指在暴露于运输、储藏和使用中合理预料带来的条件下,例如在约0℃至约40℃的温度下约30天的时间,化学状态、物理同质性和/或颜色基本不变的组合物。可以通过经验观察或通过本领域技术人员已知的适当的化学和/或物理分析方法来测定稳定性。
本文所用的“角质组织”是指作为哺乳动物最外层保护覆盖物的含角蛋白的层,其包括但不限于皮肤、毛发、指/趾甲、表皮等。
本文所用的“皮肤病学可接受的”是指所述组合物或组分适用于与人类的角质组织接触,而没有不适当的毒性、不相容性、不稳定性、变应性反应等。
本文所用的“水溶性”是指所述护肤活性物质充分地溶解于水相中并且用裸眼观察固体形式如沉淀或结晶时视觉上不明显。“水溶性”应理解为包括水分散性活性物质。“水分散性”是指悬浮于水相中但不充分溶解的活性物质。
本文中的“即时”是指如本文所定义的在水相从组合物的剩余部分视觉上分开时有益效果即产生。
本文所用关于活性物质渗透到组织中的“增强”是指如本文所述通过施用释放水相的组合物而被吸收到角质组织中的护肤活性物质的浓度,统计上相对于当施用基本上类似量的包含相同护肤活性物质且施用时不释放水相的组合物时被吸收到角质组织中的量是增加的。
本文所用“视觉上分开”是指当包含至少两个相、水相和非水相的乳液被施用到角质组织上时,所述水相包含单个小滴,例如具有约1mm至约1cm的直径,并且可由具有基本未损伤视力的人在没有放大的帮助下辨认出在油相上。
本文所用的“施用的”或“施用”是指用一个或多个手指和/或工具,采用一种连续的、单向运动和轻微压力将所述组合物铺展在角质组织表面上,例如,就像一个人想要将霜膏涂敷到面部皮肤上一样。
本文中的“增强递送装置”是指相对于不使用该装置递送的活性成分量,可增加施用到皮肤上和/或皮肤中的活性成分量的任何装置。
本文中的“调节皮肤状况”是指改善皮肤的外观和/或感觉,例如通过提供有益效果,如更光滑的外观和/或感觉。本文中的“改善皮肤状况”是指在视觉上和/或触觉上获得皮肤外观和感觉方面显而易见的积极改变。所述有益效果可以是慢性的有益效果并且可以包括以下一种或多种:减少皱褶和粗深皱纹、细纹、裂纹、肿块以及粗大毛孔的出现;使角质组织增厚(例如构建皮肤的表皮和/或真皮和/或真皮下层,并且其中可施用于指/趾甲和毛干的角质层以减少皮肤、毛发或指/趾甲的萎缩);增加真皮-表皮边界(也被称为网缘)的卷绕;防止皮肤或毛发弹性的丧失,例如由于功能性皮肤弹性蛋白的损失、破坏和/或失活,而导致诸如弹性组织变性、松垂、皮肤或毛发的变形回弹力损失等症状;减少脂肪团;改变皮肤、毛发或指/趾甲的色调,例如黑眼圈、疹斑(例如,由于例如红斑痤疮而造成的不均匀的红色调)、灰黄、由色素沉积等造成的变色。
本文所用的“皮肤老化迹象”包括但不限于由于角质组织老化而造成的所有外观视觉和触觉上可察觉的表象,以及任何宏观或微观现象。这些迹象可能缘自一些作用,所述作用包括但不限于组织上不连续的产生如皱褶和粗深皱纹、细纹、皮肤细纹、裂纹、肿块、粗大毛孔、不光滑性或粗糙性;丧失皮肤弹性;变色(包括黑眼圈);疹斑;灰黄;色素沉着的皮肤区域如老年斑和雀斑;角质化;不正常分化;过度角质化;弹性组织变性;胶原蛋白分解;以及角质层、真皮、表皮、脉管系统(例如,毛细管扩张或蛛状血管)及皮下组织(如脂肪和/或肌肉),尤其是接近皮肤的那些组织中的其它组织学变化。
本文中的“受侵害的角质组织”是指表现出不适、过敏、令人不愉快或不规则外观和诸如此类的角质组织,例如在暴露于物理和/或化学刺激之后。受侵害的角质组织的非限制性实例包括:晒伤和其它类型的灼伤;皮疹,如尿布皮疹、剃刮皮疹和过敏原诱发的皮疹;变色,如漂白、牙齿变色或色素沉着过度;具有由于例如剃刮造成割伤和切口的皮肤;由于暴露于例如风、寒冷和/或低湿度造成的干燥、裂开或粗糙的皮肤等。侵害的非限制性实例包括辐射、风、低湿度、过敏原、污染源、化学和天然刺激物、体液、身体排泄物、过多水分、细菌、真菌等。
本文所用的“非挥发性的”是指在25℃和一个大气压下蒸气压不超过约0.2mmHg的材料和/或在一个大气压下沸点为至少约300℃的材料。本文所用的“挥发性的”是指不是如本文所定义的“非挥发性”的所有材料。
本文所用的“非极性”是指所述材料具有低于约6.5(cal/cm3)0.5的平均溶解度参数,其中“cal”是指卡路里。如果当此类油与其它油类共混时,油共混物溶解度参数的加权平均数低于约6.5,则可以使用具有比6.5更高溶解度参数的油类。在本文中,“加权平均数”是指在计算平均溶解度参数时考虑多种油的体积和溶解度参数。本文所用的“极性”是指所述材料具有比如本文所定义的非极性化合物更高的平均溶解度参数。溶解度参数详尽地论述于C.D.Vaughan的“The Solubility Parameter:Whatis it?”(Cosmetics & Toiletries,第106卷,1991年11月,第69至72页,以及C.D.Vaughan在“Using Solubility Parameters inCosmeticsFormulation”,第36卷,J.Soc.Cosmetic Chemists,第319至333页,1988年9月/10月。
I.组合物
本发明的组合物为乳液形式并且包含非水相和水相。本文中的术语“非水”和“油性”被交替使用,与术语“含水”和“水”一样。适用的乳液类型包括但不限于:水包油、油包水、水包油包水和油包水包油乳液。油可源自动物、植物、或石油,可以是天然或合成的,并且可包括硅油。在一个实施方案中,皮肤病学可接受的载体包括水包油乳液和油包水乳液。在一个实施方案中,所述组合物是油包水乳液。在施用剪切力或剪切应力时,所述水相视觉上与油相分开,并且水相可以在油相之内和/或之上结合以形成可见的小滴。所述油相通常充分地均匀分布在皮肤上。在施用时、或者在施用后约三秒内、或者在施用后约十秒内,水相可以立即形成可见的小滴。
剪切力的实例包括涂敷到所述皮肤或其它角质组织上,例如通过涂抹、揉搓、轻敷、涂搽等,用手指、手掌、工具和/或增强递送装置。分开的水相可以提供即时有益效果,包括但不限于:施用时产品使角质组织水合和/或增强舒适感觉(“柔滑”)的即时指示。在各相分开后,水相可以例如被揉搓到皮肤内或可以使其蒸发。
在一个实施方案中,所述本体组合物在施用到角质组织上之前是白色的或基本无色。
A.非水相
所述组合物可包含约1.2%至约70%、或者约5%至约60%、或者约10%至约35%的非水相。非水相可以包含乳化性和/或非乳化性硅氧烷弹性体、弹性体溶剂、一种或多种油溶性护肤活性物质、以及它们的混合物。
1.弹性体
本发明的组合物包含硅氧烷弹性体,适用于降低组合物的粘著性和提供施用后的舒适感。一个适用的硅氧烷弹性体的非限制性实例是如美国专利公布2003/0049212A1中所描述的交联的有机聚硅氧烷(或硅氧烷)弹性体。所述弹性体可以包括乳化性和非乳化性硅氧烷弹性体。本文所用的“乳化性”是指具有至少一种聚氧化烯(例如聚氧乙烯或聚氧丙烯)或聚甘油分子的交联的有机聚硅氧烷弹性体。相反,“非乳化性”是指基本上不含聚氧化烯或聚甘油分子的交联的有机聚硅氧烷弹性体。
本发明的组合物可包含约0.1%至约15%,或者约0.1%至约5%,或者约0.1%至约2%的非乳化性交联的硅氧烷弹性体。在一个实施方案中,所述非乳化性交联的硅氧烷弹性体是聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷交联聚合物,这些由多个供应商提供,包括Dow CorningTM(DC 9040和DC 9041)、General ElectricTM(SFE 839)、Shin EtsuTM(KSG-15,16,18[聚二甲基硅氧烷/苯基乙烯基聚二甲基硅氧烷交联聚合物]),和Grant Industries(GRANSILTM系列弹性体)。可用于本发明的交联硅氧烷弹性体及其制备方法进一步描述于Sakuta等人的美国专利4,970,252、Kilgour等人的美国专利5,760,116,和1997年8月5日公布的Schulz,Jr.等人的美国专利5,654,362中。可用于本发明的其它交联的有机聚硅氧烷弹性体公开于转让给Pola Kasei Kogyo KK的日本专利申请JP61-18708中。此外,适用的有机聚硅氧烷弹性体粉末包括乙烯基聚二甲基硅氧烷/聚甲基硅氧烷倍半硅氧烷交联聚合物如KSP-100、KSP-101、KSP-102、KSP-103、KSP-104、KSP-105(Shin-Etsu);包含氟代烷基基团的混合硅氧烷粉末如KSP-200(Shin-Etsu);以及包含苯基基团的混合硅氧烷粉末例如KSP-300(Shin-Etsu);和DC-9506(Dow Corning)。
本发明的组合物可以包含约0.1%至约15%,或者约0.2%至约5%,或者约0.2%至约2%的乳化性交联的有机聚硅氧烷弹性体,如美国专利5,412,004、5,837,793和5,811,487中所描述。适用的乳化弹性体的非限制性实例包括由二乙烯基化合物形成的聚氧化烯改性弹性体,例如具有至少两个游离乙烯基并在聚硅氧烷主链上通过Si-H而键合的硅氧烷聚合物。在一个实施方案中,乳化性交联的有机聚硅氧烷弹性体是二甲基聚硅氧烷,其由Si-H位点在分子球形MQ树脂(R3SiO1/2SiO4/2)上交联而成,和作为另外一种选择聚二甲基硅氧烷共聚多元醇交联聚合物和聚二甲基硅氧烷,其可以商品名KSG-21从Shin Etsu商购获得。
2.弹性体溶剂
本发明的组合物可以包含按非水相的重量计约1%至约70%,或者约4%至约50%,或者约5%至约40%的交联的有机聚硅氧烷弹性体的适合溶剂。适用的溶剂的非限制性实例描述于美国专利公布2003/0049212A1中。在本发明的化妆品组合物中,溶剂的浓度可以根据溶剂和所使用的交联的硅氧烷弹性体的类型和量而变化,并且当与本发明的交联的有机聚硅氧烷弹性体颗粒结合时,所述浓度使所述弹性体颗粒悬浮和溶胀以提供弹性的、似凝胶的网状物或基质。用于交联硅氧烷弹性体的载体在环境条件下是液体,并且在一个具体实施方案中具有低粘度以改善在皮肤上的扩散。
该溶剂可包括挥发性的、非极性的油;非挥发性的、极性的油;非挥发性的、非极性的油;以及非挥发性的石蜡烃油。适用的非极性挥发性油的非限制性实例公开于授予Luebbe等人的美国专利4,781,917中,并且包括聚癸烷如异十二烷和异癸烷(例如:得自PresperseTMInc.的Permethy1-99A)和C7-C15异链烷烃(例如:得自ExxonTM Chemicals的合成异构烷油系列);不同粘度的环状聚甲基硅氧烷(cyclomethicone),例如:Dow Corning TM 200、Dow CorningTM 244、Dow CorningTM 245、DowCorning TM 344和Dow CorningTM 345、可从G.E.Silicones商购获得的有机硅液(例如:SF-1204、SF-1202、GE 7207和GE 7158)和SWS-03314(可从SWSSiliconesTM Corp.商购获得)。
可用于本发明的极性非挥发性油包括但不限于硅油、烃油、脂肪醇、脂肪酸、一价和二价羧酸与一元和多元醇形成的酯、聚氧乙烯、聚氧丙烯、聚氧乙烯和聚氧丙烯与脂肪醇形成的醚的混合物、以及它们的混合物。在一个实施方案中,极性非挥发性油选自由下列组成的组:具有丙氧基化度小于约50的C14-C18脂肪醇的丙氧基化醚、C2-C8醇和C12-C26羧酸生成的酯(例如肉豆蔻酸乙酯、棕榈酸异丙酯)、C12-C26醇和苯甲酸生成的酯(例如由FinetexTM提供的FinsolvTM TN)、C2-C8醇和己二酸、癸二酸和邻苯二甲酸生成的二酯(例如:癸二酸二异丙基酯、己二酸二异丙基酯、邻苯二甲酸二正丁基酯)、C6-C26羧酸的多元醇酯(例如:丙二醇的二癸酸酯/二辛酸酯、丙二醇的异硬脂酸酯);以及它们的混合物。
适用的非挥发性的非极性油的实例包括但不限于非挥发性的聚硅氧烷、石蜡烃油、以及它们的混合物。可用于本发明的聚硅氧烷选自由下列组成的组:聚烷基硅氧烷、聚芳基硅氧烷、聚烷基芳基硅氧烷、聚醚硅氧烷共聚物、以及它们的混合物。可用的油类的实例包括ViscasilTM系列(General Electric);Dow Corning 200系列(Dow Corning Corp.);SF1075甲基苯基流体(General Electric)和556化妆品级液体(DowCorning Corp.)。
可用于本发明的非挥发性的石蜡烃油被描述于授予Tanner等人的美国专利5,019,375和2003/0049212A1中,并且包括矿物油和支链烃如PermethylTM 102A、103A和104A(Permethyl Corporation);和EthylfloTM 364(Ethyl Corp.)。另外可用于本文的适用溶剂被描述于Guskey等人的美国专利5,750,096中。
B.水相
本发明的组合物包含水相。在一个实施方案中,所述组合物包含约25%至约98.8%,或者约40%至约95%,或者约65%至约90%的水相。水相可以继而包含附加乳化剂、一种或多种水溶性护肤活性物质、以及它们的混合物。
1.附加乳化剂
本发明的组合物可以包含附加乳化剂来用于使油相中的水相分散和悬浮于油包水乳液。所述组合物可以包含约0.001%至约5%、或者约0.01%至约5%、或者约0.1%至约3%、或者约0.1%至约2%的至少一种附加乳化剂。
多种乳化剂可用于本文以形成包水硅氧烷乳剂,这些乳化剂被描述于美国专利公布2003/0049212A1中。在一个实施方案中,附加乳化剂是硅氧烷乳化剂,包括有机改性的有机聚硅氧烷(硅氧烷表面活性剂)如聚二甲基硅氧烷共聚多元醇。可用于本文的可商购获得的聚二甲基硅氧烷共聚多元醇的实例是Dow 190、193、Q2-5220、2501 Wax、2-5324流体和3225C;ABILTM EM-90、ABILTM WE-09和 WS-08(Goldschmidt)、KF-6028和KF-6106(Shin-EtsuTM)。
在一个实施方案中,附加乳化剂是非硅氧烷乳化剂,其非限制性实例包括非离子和阴离子乳化剂如糖酯和聚酯、烷氧基化糖酯和聚酯、C1-C30脂肪醇的C1-C30脂肪酸酯、C1-C30脂肪醇的C1-C30脂肪酸酯的烷氧基化衍生物、C1-C30脂肪醇的烷氧基化醚、C1-C30脂肪酸的聚甘油基酯、多羟基化合物的C1-C30酯、多羟基化合物的C1-C30醚、烷基磷酸酯、聚氧化烯脂肪醚磷酸酯、脂肪酸酰胺、酰基乳酸酯、皂、以及它们的混合物。
2.活性物质
本发明的组合物包含至少一种水溶性护肤活性物质,并且可以包含至少一种附加油溶性护肤活性物质,两者均可用于调节和/或改善哺乳动物的皮肤状况。水和油中的溶解度在本领域技术人员的知识范围内,并且可以用已知的分析方法测定。本领域的技术人员还将理解,溶解度可以受到组合物中其它组分的类型和浓度以及其它条件如pH、离子强度等影响。许多护肤活性物质可以提供一种以上的有益效果,或通过一种以上的动作模式操作。因此,本文分类只是为了方便起见,并非旨在将活性物质限制于特定应用或已列出的应用。
维生素
本发明的组合物可包含约0.0001%至约50%,或者约0.001%至约10%,或者约0.01%至约5%,或者约0.1%至约1%的一种或多种维生素。本文中的“维生素”是指维生素、维生素原、以及它们的盐、异构体和衍生物。适宜的维生素非限制性实例包括:维生素B化合物(包括B1化合物,B2化合物,诸如烟酰胺、烟酸、生育酚烟酸酯、C1-C18烟酸酯和烟基醇的B3化合物,诸如泛醇或“原-B5”、泛酸、泛基的B5化合物,诸如吡多醇、吡哆醛、吡哆胺的B6化合物,肉毒碱,硫胺素,核黄素);维生素A化合物,以及所有维生素A天然和/或合成类似物,包括类视色素、视黄醇、乙酸视黄酯、棕榈酸视黄酯、视黄酸、视黄醛、丙酸视黄酯、类胡萝卜素(前维生素A)和其它具有维生素A生物活性的化合物;维生素D化合物;维生素K化合物;维生素E化合物或生育酚,包括生育酚山梨酸酯、生育酚乙酸酯、生育酚的其它酯和生育酚化合物;维生素C化合物,包括抗坏血酸盐、脂肪酸抗坏血酸酯和抗坏血酸衍生物,例如,抗坏血酸磷酸酯,如抗坏血酸磷酸酯镁和抗坏血酸磷酯钠、抗坏血酸基葡糖苷和抗坏血酸山梨酸酯;以及维生素F化合物,如饱和的和/或不饱和的脂肪酸。在一个实施方案中,所述组合物包含选自由下列组成的组的维生素:维生素B化合物、维生素C化合物、维生素E化合物以及它们的混合物。作为另外一种选择,所述维生素选自由下列组成的组:烟酰胺、生育酚烟酸酯、吡多醇、泛醇、维生素E、维生素E乙酸酯、抗坏血酸磷酸酯、抗坏血酸基葡糖苷、以及它们的混合物。
肽和肽衍生物
本发明的组合物可包含一种或多种肽。本文中的“肽”是指包含十个或更少氨基酸的肽、它们的衍生物、异构体、以及与其它物质如金属离子(例如,铜、锌、锰和镁)的配合物。本文所用的肽既指天然存在的肽又指合成的肽。在一个实施方案中,所述肽为二肽、三肽、四肽、五肽和六肽、它们的盐、异构体、衍生物、以及它们的混合物。可用的肽衍生物实例包括但不限于源自大豆蛋白的肽(得自Silab的Ridulisse CTM,法国)、肌肽(β-丙氨酸-组氨酸)、棕榈酰-赖氨酸-苏氨酸(pal-KT)和棕榈酰-赖氨酸-苏氨酸-苏氨酸-赖氨酸-丝氨酸(pal-KTTKS,以被称为的组合物获得)、棕榈酰-甘氨酸-谷氨酰胺-脯氨酸-精氨酸(pal-GQPR,以被称为的组合物获得),这三种得自Sederma,France,乙酰基-谷氨酸盐-谷氨酸盐-甲硫氨酸-谷氨酰胺-精氨酸-精氨酸(Ac-EEMQRR、)和Cu-组氨酸-甘氨酸-甘氨酸(Cu-HGG,也称作)的肽。
所述组合物可包含约1x10-7%至约20%,或者约1x10-6%至约10%,或者约1x10-5%至约5%的肽。
糖胺
本发明的组合物可包含也被称为氨基糖的糖胺、以及它们的盐、异构体、互变异构体和衍生物。糖胺来源于合成或天然,并且可用作纯化合物或化合物的混合物(例如得自天然源的提取物或合成物质的混合物)。例如,葡糖胺通常存在于许多甲壳类动物中,并且也可源自真菌源。可用于本发明中的糖胺化合物包括例如N-乙酰基葡糖胺,以及描述于授予Yu等人的PCT公布WO 02/076423和美国专利6,159,485中的那些。在一个实施方案中,所述组合物包含约0.01%至约15%,或者约0.1%至约10%,或者约0.5%至约5%的糖胺。
防晒剂
本主题发明的组合物可包含一种或多种防晒活性物质(或“防晒剂”)和/或紫外线吸收剂。本文的“防晒活性物质”包括防晒剂和物理防晒霜。防晒剂活性物质和紫外线吸收剂可以是有机或无机的。适用的防晒活性物质和紫外线吸收剂的实例公开于The Cosmetic,Toiletry,andFragrance Association的“The International Cosmetic IngredientDictionary and Handbook”第10版(Gottschalck,T.E.和McEwen,Jr.编辑,2004年)第2267和第2292至2293页。尤其适合的防晒活性物质包括:二苯甲酮、二苯甲酮-1、二苯甲酮-2、二苯甲酮-3、二苯甲酮-4、二苯甲酮-5、二苯甲酮-6、二苯甲酮-7、二苯甲酮-8、二苯甲酮-9、二苯甲酮-10、二苯甲酮-11、二苯甲酮-12、苯并三唑基十二烷基对-甲酚、3-亚苄基樟脑、亚苄基樟脑磺酸、水杨酸苄基酯、双-乙基己氧苯酚甲氧苯基三嗪、波尼酮、布美三唑、丁基甲氧基二苯甲酰基甲烷、PABA(对-氨基苯甲酸)丁酯、肉桂酰胺丙基三甲基氯化铵、西诺沙酯、甲氧基肉桂酸DEA盐、二苯并噁唑基萘、二叔丁基羟基-亚苄基樟脑、二乙氨基羟苯甲酰基苯甲酸己酯、二乙基己基丁酰胺基三嗪酮、2,6-萘二甲酸二乙基己酯、二异丙基肉桂酸乙酯、二异丙基肉桂酸甲酯、双-甲氧基肉桂酰胺丙基乙基二甲基氯化铵醚、二甲基PABA乙基鲸蜡硬脂基二甲基铵甲苯磺酸盐、二吗啉哒嗪酮、双乙苯基三氨基三嗪茋二磺酸二钠、联苯乙烯二苯基二磺酸二钠、苯基二苯并咪唑四磺酸酯二钠、甲酚曲唑、甲酚曲唑三硅氧烷、二羟丙基PABA乙酯、二异丙基肉桂酸乙酯、乙基己基双-异戊基苯并噁唑基苯基三聚氰胺、二甲氧基亚苄基二氧代咪唑啉丙酸乙酯、二甲基PABA乙基己酯、甲氧基肉桂酸乙基己酯、乙基己基甲氧基二苯甲酰甲烷、水杨酸乙基己酯、乙基己基三嗪酮、甲氧基肉桂酸乙酯、PABA乙酯、尿刊酸乙酯、依托立林、4-(2-β-吡喃葡糖甲硅氧基)丙氧基-2-羟基二苯甲酮、甘油乙基己酸酯二甲氧基肉桂酸酯、甘油PABA酯、乙二醇水杨酸酯、1,6-己二醇二水杨酸酯、胡莫柳酯、肉桂酸异戊酯、对-甲氧基肉桂酸异戊酯、异戊醇三甲氧基肉桂酸酯三硅氧烷、异丙苄醇水杨酸酯、异丙基二苯甲酰甲烷、甲氧基肉桂酸异丙酯、山柰根提取物、薄荷醇邻氨基苯甲酸酯、薄荷醇水杨酸酯、甲氧基肉桂酰胺丙基羟基磺基甜菜碱、甲氧基肉桂酰胺丙基月桂基二甲基铵甲苯磺酸酯、4-甲基苄亚基樟脑、亚甲基双-苯并三唑基四甲基丁基酚、奥克立林、奥克三唑、PABA、PEG-25PABA、苯基苯并咪唑磺酸、聚丙烯酰胺甲基亚苄基樟脑、聚酰胺-2、聚季铵盐-59、聚硅氧烷-15、甲氧基肉桂酸钾、苯基苯并咪唑磺酸钾、红色凡士林、苯并三唑基丁苯酚磺酸钠、苯基苯并咪唑磺酸钠、尿刊酸钠、苯基苯并咪唑磺酸TEA盐、水杨酸TEA盐、对苯二亚甲基二樟脑磺酸、四丁基苯酚羟基苯甲酸酯、二氧化钛、尿刊酸、氧化铈锌、氧化锌、以及它们的混合物。在一个实施方案中,所述组合物可包含按所述组合物的重量计约1%至约10%,或者约2%至约20%的防晒活性物质和紫外线吸收剂。确切的量将根据所选的防晒活性物质和/或紫外线吸收剂以及所期望的防晒因子(SPF)而变化,并且在本领域技术人员的理解和判断范围内。
控油剂
本发明的组合物可包含一种或多种化合物来用于调节皮肤油或皮脂的产生以及用于改善油性皮肤外观。适用的控油剂的实例包括水杨酸、脱氢乙酸、过氧化苯甲酰、间苯二酚、硫、红霉素、锌、维生素B3化合物(例如,烟酰胺或生育酚烟酸酯)、它们的异构体、酯、盐和衍生物、以及它们的混合物。所述组合物可包含约0.0001%至约15%,或者约0.01%至约10%,或者约0.1%至约5%,或者约0.2%至约2%的控油剂。
类黄酮
本发明的组合物可包含类黄酮。类黄酮可以是合成物质,或作为得自天然源的提取物,其还可被进一步衍生。适用的类黄酮类型的实施例公开于授予Bissett的美国专利6,235,773中,并且包括但不限于未取代的黄烷酮、甲氧基黄烷酮、未取代的查耳酮、以及它们的混合物。在一个实施方案中,所述类黄酮是未取代的黄烷酮、未取代的查耳酮(尤其是反式异构体)、它们的葡糖基衍生物、以及它们的混合物。合适类黄酮的其它实施例包括黄烷酮,诸如橘皮苷和葡糖基橘皮苷,异黄酮,诸如大豆异黄酮,包括但不限于染料木黄酮、黄豆甙原、五羟黄酮和牛尿酚,它们的葡糖基衍生物,2′,4-二羟基查耳酮、以及它们的混合物。
本发明的组合物可包含约0.01%至约20%,或者约0.1%至约10%,或者约0.5%至约5%的类黄酮。
亮肤剂
本组合物可以包含约0.1%至约10%,或者约0.2%至约5%的亮肤剂。所述亮肤剂可以改善皮肤的外观和/或减少色素沉着过度。可用于本文的适宜美白剂包括:壬二酸、丁基羟基苯甲醚、没食子酸、hydroquinoine、曲酸、熊果苷和脱氧熊果苷、桑树提取物、十一碳烯酰基苯基丙氨酸、十八碳烯二酸、十八碳烯二酸,和上述任何物质的盐和衍生物、以及它们的混合物。
其它护肤活性物质
本发明的组合物还可包含非维生素抗氧化剂和自由基清除剂、矿物、防腐剂、毛发生长调节剂、植物甾醇和/或植物激素、蛋白酶抑制剂、酪氨酸酶抑制剂和抗炎剂。
适用的非维生素抗氧化剂和自由基清除剂包括但不限于BHT(丁基化羟基甲苯)、丁基化羟基苯甲酸、L-麦角硫因(以商品名THIOTANETM)、四氢姜黄素、氯化十六烷基吡啶、亚丁香基丙二酸二乙基己酯(以商品名OXYNEXTM)、6-羟基-2,5,7,8-四甲基苯并二氢吡喃-2-羧酸(以商品名TroloxTM)、十六碳-8-烯-1,16-二羧酸(十八烯二酸;以商品名ARLATONETM Dioic DCA得自Uniqema)、泛醌(辅酶Q10)、茶叶提取物,包括绿茶提取物、酵母提取物或酵母培养液(如PiteraTM)、没食子酸、尿酸、山梨酸、硫辛酸、胺(如N,N-二乙基羟基胺、氨基胍)、巯基化合物包括谷胱甘肽,二羟基富马酸、氧哺氨酸甜菜碱、氧哺氨酸精氨酸、去甲二氢愈创木酸、姜黄素、赖氨酸、蛋氨酸、脯氨酸、超氧化物歧化酶、水飞蓟素、葡萄皮/籽提取物、黑素、迷迭香提取物、任何上述物质的盐和衍生物、以及它们的组合。
适用的毛发生长调节剂包括但不限于去氧苯比妥、丁基化羟基甲苯(BHT)、己二醇、泛醇和泛酸衍生物、它们的异构体、盐和衍生物,以及它们的混合物。
适用的矿物包括锌、锰、镁、铜、铁、硒和其它矿物增补剂。“矿物”被认为包括各种氧化状态、矿物复合物、盐、衍生物、以及它们的组合的矿物。
适用的植物甾醇(植物甾醇)和/或植物激素的实例包括但不限于谷甾醇、豆甾醇、菜油甾醇、芸苔甾醇、激动素、玉米素、以及它们的衍生物和它们的混合物。
适用的蛋白酶抑制剂包括但不限于去氧苯比妥、香草醛乙酸酯、薄荷基邻氨基苯甲酸盐、大豆胰蛋白酶抑制剂、Bowman-Birk抑制剂、以及它们的混合物。
适宜的酪氨酸酶抑制剂包括但不限于sinablanca(芥菜籽提取物)、四氢姜黄素、氯化十六烷基吡啶鎓、以及它们的混合物。
适用的抗炎剂包括但不限于非甾族抗炎剂(NSAIDS),包括但不限于布洛芬、萘普生、氟芬那酸、依托芬那酯、阿司匹林、甲芬那酸、甲氯芬那酸、吡罗昔康和联苯乙酸;甘草酸(也被称为甘草素、甘草甜素和甘草皂甙)、甘草次酸、其它甘草提取物;小烛树蜡、红没药醇(如α-红没药醇)、茜草提取物(提取自茜草属植物,尤其是茜草)和乳香树脂(提取自没药属植物,尤其是印度穆库尔没药)、可乐果提取物、春黄菊、红三叶草提取物和海鞭提取物,任何上述物质的衍生物、以及它们的混合物。
其它可用的护肤活性物质包括保湿和/或调理剂,如甘油、凡士林、芦荟、尿囊素、红没药醇、甘草酸二钾盐和尿素;脱氢表雄甾酮(DHEA),其类似物和衍生物;脱落剂,包括α-和β-羟基酸、α-酮酸、乙醇酸和水杨酸辛酰基酯;脱屑活性物质,包括两性离子表面活性剂;抗微生物剂;抗蜂窝炎剂,如咖啡因、茶碱、可可碱和氨茶碱;去头皮屑剂,如羟甲辛吡酮乙醇胺、3,4,4′-三氯碳酰苯胺(三氯生)、三氯卡班和1-氧-2-巯基吡啶锌;二甲基氨基乙醇(DMAE);肌酸;(免晒)美黑剂,如二羟基丙酮(DHA);螯合剂,例如糠偶酰二肟和糠偶酰一肟;二烷酰基羟脯氨酸化合物;大豆提取物,如豆浆、豆酱和日本豆酱盐;氨基酸;橄榄油衍生物如PEG-7橄榄油羧酸钠,局部麻醉剂,如苯佐卡因、利多卡因、布比卡因、氯普鲁卡因、狄布卡因、依替卡因、马比佛卡因、丁卡因、达克罗宁、已卡因、普鲁卡因、可卡因、开他敏、普莫卡因、苯酚;任何上述物质的盐和衍生物;以及它们的混合物。
C.其它成分
增稠剂
本发明的组合物可包含约0.1%至约5%,或者约0.1%至约4%,或者约0.25%至约3%的增稠剂。增稠剂的非限制性类别包括但不限于羧酸聚合物、交联聚丙烯酸酯聚合物、聚丙烯酰胺聚合物、多糖、树胶、以及它们的混合物。
II.使用方法
本发明描述了一种调节哺乳动物皮肤状况,给消费者即时或敏锐有益效果的迹象和增加水溶性护肤活性物质渗透到角质组织中的方法。所述方法包括如本文所述局部地将个人护理组合物施用到哺乳动物皮肤上的步骤。作为另外一种选择,所述方法可以包括如本文所述将组合物施用到受侵害的角质组织上的步骤,以调节和/或改善此类组织状况,和/或提供减轻受侵害的影响。
所述组合物可施用到任何角质组织上,包括需要一种或多种有益效果的角质组织。有益效果包括:调节和/或改善角质组织状况,其非限制实例包括减少皱纹出现、减少深纹出现、减少细纹出现、减少粗大毛孔出现、减少角质组织的厚度、增加真皮-表皮边界的褶合、增加弹性、减少脂肪团出现、减少变色出现、减少色素沉着过度出现、减少黑眼圈出现、减少灰黄出现、以及它们的组合。作为另外一种选择,所述有益效果可以包括减少皱纹、减少深纹、减少细纹、减少粗大毛孔、减少脂肪团、减少色素沉着过度、减少黑线圈、减少虚胖、以及它们的组合。
所述组合物可以按照多种方法施用,包括揉搓、涂搽或用手或手指轻敷,或通过工具和/或增强递送装置的方式。工具的非限制性实例包括海绵或海绵端涂敷器,药签(例如:棉端药签),任选地包括泡沫或海绵涂敷器的笔、刷子、擦拭物、以及它们的组合。增强递送装置的非限制性实例包括机械的、电动的、超声的和/或其它动力装置。在一个实施方案中,所述组合物被轻轻地铺展到皮肤上以有利于水相与油相分开。当水相分开且结合成视觉上增大的小滴时,所述组合物可以按原样保留在角质组织上。作为另外一种选择,所述组合物在被揉搓到角质组织中之前,可以在皮肤上保留5秒、10秒、30秒或1分钟。
所施用的组合物量、施用频次和使用周期将根据给定组合物的组分含量和所需的调节水平广泛地变化。例如,每平方厘米的角质组织可施用约0.01g至约1g的组合物。在一个实施方案中,至少每日一次施用所述组合物,其中“每日”和“每天”是指24小时的时间。例如,可每日施用所述组合物连续30天,或者连续14天,或者连续7天,或者连续2天。
所述方法可包括引起所述组合物和/或角质组织温度变化的步骤,所述步骤与施用所述组合物步骤同时或相续。所述方法还可包括构成处理或施用摄生法一部分的附加步骤,包括施用至少一种附加组合物的步骤,摄取一种或多种饮食增补剂的步骤,清洁步骤等。
实例1至6
以下为根据本文所述的方法可以被施用到角质组织的组合物的非限制性实例。
1.E.g.,Tospearl 145A或CF 600,得自GE Toshiba Silicone。
2.12.5%的聚二甲基硅氧烷交联聚合物的环戊硅氧烷溶液,得自Dow Corning
3.12.5%的聚二甲基硅氧烷的环戊硅氧烷溶液,得自Dow Corning
4.5%的聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷交联聚合物的聚二甲基硅氧烷溶液,得自Shin-Etsu
5.25%的聚二甲基硅氧烷PEG-10/15交联聚合物的聚二甲基硅氧烷溶液,得自Shin-Etsu
6.PEG-9聚二甲基硅氧乙基聚二甲基硅氧烷,得自Shin-Etsu
7.PEG-10聚二甲基硅氧烷,得自Shin-Etsu
8.二氧化硅、氧化铝、二氧化钛、表面被聚二甲基硅氧烷/聚甲基硅氧烷共聚物覆盖的滑石,得自Catalysts & Chemicals。
9.25%的聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷交联聚合物的聚二甲基硅氧烷溶液,得自Shin-Etsu
10.另外或作为另外一种选择,所述组合物可以包含一种或多种如本文所公开的其它护肤活性物质、它们的盐和衍生物,也如本文所公开的由本领域技术人员认为适宜的量。
11.二羟乙基磺酸己氧苯醚,得自Laboratoires Serobiologiques。
12.DMDM乙内酰脲、碘代丙炔基氨基甲酸丁酯、1,3-丁二醇的水溶液,得自LonzaInc.
在一个适合的容器中,混合A相的成分。在另外一个适合的容器中,混合B相的成分。用适合的搅拌器(例如,锚定剂刀片、推进器刀片,IKAT25)混合各个相直到各个相均一化。将B相缓慢加入到A相中,并且持续搅拌以混合A相。继续搅拌直至此批均匀。将产物倒入适合的容器中并且在室温下保存。
实施例7
以下实施例描述了受侵害的角质组织如何可以通过施用适合的组合物来得到调节和/或改善。这些实施例仅仅为了例证性的目的,它们不旨在限制可被施用到特定受侵害的皮肤区域的活性物质的类型。所有的活性物质均为水溶性形式。
将以下描述的组合物施用到受侵害的皮肤区域,所用量为大约每平方厘米皮肤区域0.1g的组合物。将所述组合物擦拭到皮肤上,直到出现视觉上不同的小滴。作为另外一种选择,所述组合物可以用工具例如药签或棒状涂敷器轻敷到受影响的区域以产生视觉上不同的小滴。将所述组合物保留在皮肤上大约1分钟。然后可将所述组合物进一步揉搓到皮肤内。
组合物 | 附加的水溶性活性物质 | 侵害 |
实施例2 | 抗炎剂试剂,例如甘草次酸 | 晒伤、灼伤 |
实施例3 | 亮肤剂,如十一碳烯酰基苯基丙氨酸 | 色素沉着过度 |
实施例1 | 肽,例如棕榈酰-KTTKS、防晒剂、抗氧化剂 | 紫外线伤害,例如细纹、皱纹、干燥和/或剥裂皮肤 |
本文所公开的量纲和值不应被理解为严格地限于所述精确值。相反,除非另外指明,每个这样的量纲是指所述数值和围绕那个数值的功能上等同的范围。例如,所公开的量纲“40mm”旨在表示“约40mm”。
在发明详述中引用的所有文件都在相关部分中以引用方式并入本文中。对于任何文件的引用不应当解释为承认其是有关本发明的现有技术。当本发明中术语的任何含义或定义与以引入方式并入的文件中术语的任何含义或定义矛盾时,应当服从在本发明中赋予该术语的含义或定义。
虽然已经举例说明和描述了本发明的特定实施方案,但是对于本领域技术人员来说显而易见的是,在不脱离本发明精神和范围的情况下可以做出多个其他改变和变型。因此,权利要求书意欲包括在本发明范围内的所有这样的改变和变型。
Claims (9)
1.一种增强水溶性护肤活性物质向角质组织中的递送的美容方法,所述方法包括将包含油包水乳液的组合物施用到角质组织上的步骤,所述乳液包含水相和非水相,其中所述水相包含水溶性护肤活性物质,优选地包含维生素B化合物、维生素C化合物、肽和肽衍生物、糖胺、控油剂、抗氧化剂前体、自由基清除剂、防晒剂、蛋白酶抑制剂、亮肤剂、免晒美黑剂、或它们的混合物,更优选地包含烟酰胺、抗坏血酸基葡糖苷、N-乙酰基葡糖胺、二羟基丙酮、五肽、去氧苯比妥化合物、脱氢乙酸钠、对苯二酚、十一碳烯酰基苯基丙氨酸、氯化十六烷基吡啶鎓、它们的盐和衍生物、或它们的混合物;并且在对所述组合物施用剪切应力时,所述水相与所述非水相视觉上分开。
2.如权利要求1所述的方法,其中所述组合物包含1.2%至70%的非水相。
3.如前述任一项权利要求所述的方法,其中所述非水相包含优选0.1%至15%的量的乳化性交联的硅氧烷弹性体,优选0.1%至15%的量的非乳化性交联的硅氧烷弹性体,或它们的混合物。
4.如前述任一项权利要求所述的方法,其中所述组合物包含按所述非水相的重量计1%至70%的弹性体溶剂。
5.如前述任一项权利要求所述的方法,其中所述非水相还包含油溶性护肤活性物质,优选地包含维生素E化合物、防晒剂、紫外线吸收剂、或它们的混合物。
6.如前述任一项权利要求所述的方法,其中所述含水相包含0.001%至5%的至少一种附加乳化剂,优选包含硅氧烷乳化剂、非硅氧烷乳化剂、或它们的混合物。
7.一种为消费者提供即时有益效果,优选水滴的出现,和增强护肤活性物质向角质组织中的递送的美容方法,所述方法包括将包含1.2%至70%的非水相和30%至98.8%的水相的组合物施用到需要有益效果的角质组织上,优选地施用到哺乳动物皮肤上,并且更优选地施用到受侵害的哺乳动物皮肤上的步骤,其中:
a.所述非水相包含:
i.按所述组合物的重量计0.1%至15%的非乳化性交联的硅氧烷弹性体;
ii.按所述组合物的重量计0.1%至15%的乳化性交联的硅氧烷弹性体;
iii.按所述非水相的重量计1%至70%的用于非乳化性和乳化性交联的硅氧烷弹性体的溶剂;
iv.任选地油溶性护肤活性物质,所述油溶性护肤活性物质包含维生素E化合物、防晒剂、紫外线吸收剂、或它们的混合物;
b.所述含水相包含至少一种水溶性护肤活性物质和皮肤病学可接受的载体,所述水溶性护肤活性物质包含维生素B化合物、维生素C化合物、肽和肽衍生物、糖胺、控油剂、抗氧化剂前体、自由基清除剂、防晒剂、蛋白酶抑制剂、亮肤剂、免晒美黑剂、或它们的混合物。
8.如权利要求7所述的美容方法,其中所述护肤活性物质提供慢性有益效果,优选地包括减少老化迹象、减少皱纹出现、减少深纹出现、减少细纹出现、减少粗大毛孔出现、减少角质组织厚度、增加真皮-表皮边界的褶合、增加弹性、减少脂肪团出现、减少变色出现、减少色素沉着过度出现、减少黑眼圈出现、减少灰黄出现、或它们的组合。
9.如权利要求7或8所述的方法,其中所述受侵害的哺乳动物皮肤包括:灼伤的、晒伤的、受皮疹影响的、受尿布皮疹影响的、受剃刮皮疹影响的、受过敏原诱发的皮疹影响的、漂白的、玷污的、色素沉着的;有缺痕的皮肤、有割伤的皮肤、干燥的皮肤、粗糙的皮肤、或它们的组合。
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2007
- 2007-05-15 CN CNA2007800175907A patent/CN101442981A/zh active Pending
- 2007-05-15 WO PCT/US2007/011616 patent/WO2007133768A2/en active Application Filing
- 2007-05-15 EP EP07794882A patent/EP2018148A2/en not_active Withdrawn
- 2007-05-15 US US11/803,532 patent/US20070264210A1/en not_active Abandoned
- 2007-05-15 JP JP2009511020A patent/JP2009536965A/ja active Pending
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CN106535994A (zh) * | 2013-12-20 | 2017-03-22 | 莱雅公司 | 水溶性活性组分的载体系统 |
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CN106109861A (zh) * | 2016-08-24 | 2016-11-16 | 钟桂冰 | 保持牲畜身体凉爽的方法 |
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Also Published As
Publication number | Publication date |
---|---|
WO2007133768A2 (en) | 2007-11-22 |
US20070264210A1 (en) | 2007-11-15 |
JP2009536965A (ja) | 2009-10-22 |
EP2018148A2 (en) | 2009-01-28 |
WO2007133768A3 (en) | 2008-01-10 |
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