CN108158836A - 用于增亮皮肤的方法 - Google Patents
用于增亮皮肤的方法 Download PDFInfo
- Publication number
- CN108158836A CN108158836A CN201711095416.6A CN201711095416A CN108158836A CN 108158836 A CN108158836 A CN 108158836A CN 201711095416 A CN201711095416 A CN 201711095416A CN 108158836 A CN108158836 A CN 108158836A
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- Prior art keywords
- acid
- skin
- composition
- method described
- acids
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Abstract
公开了用于增亮皮肤的非治疗目的的方法,其包括如下步骤:a)确定需要皮肤增亮的皮肤;b)使所述皮肤与包含如下组分的组合物接触:增亮皮肤的取代的脂族活性剂,其包含12‑羟基硬脂酸和/或其盐和/或其酯,和化妆品载体;以及c)增亮皮肤,其中所述取代的脂族活性剂增亮皮肤,所述组合物还包含另外的组分,该另外的组分选自烟酰胺、二元酸、硬脂酸、间苯二酚或它们的混合物。
Description
本申请是一项发明专利申请的分案申请,其母案的申请日为2009年6月4日、申请号为200980122854.4(PCT/EP2009/056886)、发明名称为“用于增亮肤色的组合物”。
技术领域
本发明涉及皮肤增亮添加剂以及包含其的组合物。更具体地说,本发明涉及一种化妆品组合物,其包含皮肤增亮添加剂,其中所述皮肤增亮添加剂包括杂取代的饱和或不饱和脂族酸,或其混合物。所述皮肤增亮添加剂在使用时导致化妆品组合物可以提供润湿好处。另外,意想不到地发现这种脂族酸在局部应用时具有皮肤增亮的好处。
背景技术
许多消费者都很关注他们皮肤的特征。例如,消费者会关注他们皮肤的着色度、雀斑和/或老年斑。其它消费者希望降低由暴露于日光下所引起的皮肤颜色变深。为符合消费者的需要,已经进行了许多尝试以开发改善皮肤特征的产品。迄今所开发的产品往往具有低效力,具有不希望的副作用或两者都有。此外,这种产品可能是昂贵的,通常不是低收入消费者的选用品。
开发一种包括新皮肤增亮添加剂的化妆品组合物引起越来越大的兴趣。本发明涉及包含新皮肤增亮添加剂的化妆品组合物。本发明的化妆品组合物优选包含作为增亮添加剂的化合物,如12-羟基硬脂酸、蓖麻油酸或两者。在比较用具有新发现的本发明皮肤增亮添加剂的组合物处理的MelanoDermTM培养物和未用其处理的MelanoDermTM培养物时,本发明的化妆品组合物导致黑色素含量降低,其降低至少8%(优选降低至少约11%)。
补充信息:
人们致力于制备皮肤护理化妆品组合物。在US 6875425中公开了具有4-取代的间苯二酚衍生物化合物的皮肤增亮剂。
已公开的其它努力致力于制备皮肤处理组合物。在US 7250158和US 7247294中公开了用皮肤增亮剂处理皮肤的方法。
已公开的另一些努力致力于处理皮肤。在US 5998423中公开了具有多环氮杂环的组合物。
以上补充信息中完全没有公开皮肤增亮组合物,其包含作为增亮添加剂的杂取代的饱和或不饱和脂族酸,或其混合物。
发明内容
在第一方面,本发明涉及一种皮肤增亮添加剂,所述皮肤增亮添加剂包括一种杂取代的饱和或不饱和脂族酸,或两者。
在第二方面,本发明涉及一种用于皮肤增亮的化妆品组合物,所述化妆品组合物包含皮肤增亮剂,所述皮肤增亮剂包括本发明第一方面的皮肤增亮添加剂。
在第三方面,本发明涉及一种用本发明第二方面的化妆品组合物增亮皮肤的方法。
参考详细说明和随后的实施例,本发明的所有其它方面将变得明显。
这里所用的“降低黑色素含量”意思是,在比较未用包含本发明皮肤增亮添加剂的组合物处理的两组三周龄的MatTek MelanoDerm培养物与用包含本发明皮肤增亮添加剂的组合物处理的两组三周龄的MatTek MelanoDerm培养物时,黑色素含量减少,其中处理意思是:
(a)将所述MelanoDerm培养物装在六孔组织培养皿内,并设置所述组织培养皿约0.3cm空着;
(b)使所述MelanoDerm培养物接触0.1-5微摩尔具有本发明皮肤增亮添加剂的组合物,所述组合物由10毫摩尔的皮肤增亮添加剂溶液和用Dulbecco's Modified Eagle Media稀释的载体(例如二甲亚砜)制备;
(c)通过获得黑色素平均含量(表示为微克)来比较处理和未处理的培养物,这通过从MelanoDerm提取黑色素并使用市售分光光度计如Hach分光光度计获得在490nm的吸光度读数(OD 490)。
这里所用的“化妆品组合物”意在包括用于局部施用到哺乳动物尤其是人皮肤的组合物。这种组合物可大致分类为留下型或冲掉型,意在包括调理剂或补剂,口红,彩色化妆品和普通的局部组合物,其呈一定款式并至少减小黑色素对角质细胞的影响。这里所用的“增亮”和“增白”意思相同,他们包括皮肤的直接增亮以及对皮肤上的斑点如老年斑和雀斑的增亮。“Dulbecco's Modified Eagle Media”指的是MatTek Corporation出售的营养液,其根据所提供的说明书进行处理和使用,所述产品以MEL 30010BBLLMM市售。皮肤增亮添加剂指的是用于导致物理增白,尤其是生物增白(即降低黑色素生成)的组分,因此所述皮肤增亮添加剂可以包括皮肤增亮添加剂,可以主要由皮肤增亮添加剂组成或由皮肤增亮添加剂组成。“MelanoDerm”指的是具有正常人源表皮角质细胞和黑色素细胞的产品,所述细胞已经经过培养,形式人表皮细胞的多层的高度分化的模型,所有这些都由MatTekCorporation市售。这里所用的“不饱和”意思是具有至少一个非sp3杂化键。这里所用的“包括”意在包括“主要由...组成”和“由...组成”。
本发明的化妆品组合物可以是以下形式:液体、洗液、乳膏、清液、凝胶、皂条或调色剂,或通过面具或贴片施加。本发明组合物是至少增亮皮肤的组合物,“皮肤”意在包括脸、脖子、胸部、背部、手臂、手、腿和头皮上的皮肤。在此指明的所有范围意在隐含包括所有在其中包容的所有范围,如果例如没有明确指出这些范围。
具体实施方式
可用于本发明的皮肤增亮添加剂的唯一限制是其可用于适用于人的局部组合物。优选的添加剂是杂取代的饱和或不饱和脂族酸,或其混合物。
在最优选的实施方案中,用于本发明的所述皮肤增亮添加剂包括具有下式的化合物:
或其混合物,
其中各个R独立地是氢、羟基、C1-6烷氧基、C1-6烷基、芳烷基或胺,条件是至少一个R基包括杂原子;各个R1独立地是氢、C1-6烷氧基、C1-6烷基、芳烷基或胺;n是7-19的整数;s和e各自独立地是0-8的整数,其中s+e>6;q是6-11的整数;各个r独立地是0-1的整数,条件是当x是1时r不是1;x是0-1的整数,条件是当至少一个r是1时x是0;和各个t独立地是1-7的整数。
适用于本发明的优选化合物(单独或为混合物)是紫胶桐酸、9,10,18-三羟基十八烷酸(phloionolic acid)、9,10,13-三羟基-11-十八碳烯酸、9,13-二羟基-12-乙氧基-10-十八碳烯酸、9-羟基-10,12-十八碳二烯酸、4,14-二羟基-十八烷酸、12-羟基硬脂酸(12-羟基十八烷酸)、14-羟基-顺-11-二十碳烯酸(lesquerolic acid)、反蓖麻酸、黄葵酸和蓖麻油酸(12-羟基-9-顺-十八烷酸),如结构式I或II所示。适用于本发明的其它优选化合物包括β-9-羟基-10,12-十八碳二烯酸(β-dimorphecolic acid)、12-羟基-9,15-十八碳二烯酸(densipolic acid)、8-甲氧基-13-羟基-9,11-十八碳二烯酸、7-氧-十八烷酸、9-氧-十八烷酸、12-氧-十八烷酸和10-氧-14-甲基-十五烷酸,如结构式III所示。此外,本发明的范围包括式I-III酸的任何衍生物(如酯衍生物)和/或盐,尤其是其Mg、Na和/或Ca盐.这种化合物是市售的,可以从厂商如Vertellus Specialties Inc.Welch,Home Clark Co.Inc.以及Croda Chemicals买到。
以本发明的化妆品组合物的总重量为基准,本发明的化妆品组合物一般包括0.001-15重量%,优选0.1-12重量%,最优选1-10重量%的皮肤增亮添加剂,也包括其中包容的所有的数值范围。
虽然本发明的范围包括所述皮肤增亮添加剂基本由以下物质组成以及由以下物质组成:杂取代的饱和或不饱和脂族酸或其混合物,但是在一个通常期望的实施方案中,以皮肤增亮添加剂的总重量为基准,本发明的皮肤增亮添加剂包括0.2-95重量%,优选10-85重量%,最优选30-65重量%的杂取代的饱和或不饱和脂族酸或其混合物,也包括其中包容的所有的数值范围。
在另一期望的实施方案中,以本发明的化妆品组合物的总重量为基准,本发明的化妆品组合物包括2-9重量%,优选3-8重量%,最优选3-6重量%的杂取代的饱和或不饱和脂族酸或其混合物,也包括其中包容的所有的数值范围。
在组合使用时,杂取代的饱和或不饱和脂族酸与杂取代的饱和脂族酸的重量比为5:95-95:5,优选20:80-80:20,最优选40:60-60:40,也包括其中包容的所有的数值范围。
应知道,可使用市购且常规的赋形剂作为稀释剂、分散剂和/或载体,用于所述皮肤增亮剂和这里所述的添加剂,以及任何其它任选的但经常优选的添加剂。因此,适用于本发明的化妆品可接受的赋形剂可以是水基的、无水的或乳液,通常优选油包水的或水包油的乳液。如果需要用水,水一般占所述化妆品组合物的余量,优选占所述化妆品组合物的5-99重量%,最优选40-80重量%,也包括其中包容的所有的数值范围。
除水外,本发明的组合物可任选包含有机溶剂用作载体或助载体。适用于本发明的有机溶剂类型的示例且非限制性实例包括链烷醇如乙醇和异丙醇、其混合物等。
其它适用的任选添加剂包括酯油如肉豆蔻酸异丙酯、肉豆蔻酸鲸蜡酯、肉豆蔻酸2-辛基十二烷基酯、鳄梨油、杏仁油、橄榄油、二癸酸新戊二醇酯、其混合物等。这类酯油一般协助乳化本发明的化妆品组合物,经常使用能够产生稳定乳液,最优选油包水乳液的有效量。
如果希望,也可在本发明化妆品组合物中使用润肤剂作为载体。经常希望使用醇如1-十六烷基醇(即鲸蜡醇)和苯氧乙醇作为润肤剂,还有通常被归类为硅油和合成酯。适用的硅油包括环状的或直链的聚二甲硅氧烷,包含3-9个,优选4-5个硅原子。在这里所述的本发明化妆品组合物中用作润肤物质的非挥发性硅油包括多烷基硅氧烷、多烷基芳基硅氧烷和聚醚硅氧烷共聚物。这里有用的基本不挥发的多烷基硅氧烷包括例如聚二甲硅氧烷。
可以任选使用的酯润肤剂是:
(1)具有10-20个碳原子的脂肪酸的链烯基或烷基酯。其实例包括新戊酸异二十烷基酯、异壬酸异壬酯、肉豆蔻酸油烯基酯、硬脂酸油烯基酯和油酸油烯基酯。
(2)醚-酯,如乙氧基化脂肪醇的脂肪酸酯。
(3)多元醇酯。乙二醇单和二脂肪酸酯、二甘醇单和二脂肪酸酯、聚乙二醇(200-6000)单和二脂肪酸酯、丙二醇单和二脂肪酸酯、聚丙二醇2000单油酸酯、聚丙二醇2000单硬脂酸酯、乙氧基化单硬脂酸丙二醇酯、甘油基单和二脂肪酸酯、聚甘油多脂肪酸酯、乙氧基化甘油基单硬脂酸酯、1,3-丁二醇单硬脂酸酯、1,3-丁二醇二硬脂酸酯、聚氧乙烯多羟基脂肪酸酯、失水山梨糖醇脂肪酸酯,并且聚氧乙烯失水山梨糖醇脂肪酸酯是令人满意的多元醇酯。
(4)蜡酯如蜂腊、鲸蜡、十八烷酰硬脂酸酯以及二十烷基山酸酯。
(5)甾醇酯,其实例为胆固醇脂肪酸酯。
润肤剂的使用量一般为所述化妆品组合物的0.1-50重量%,也包括其中包容的所有的数值范围。
本发明组合物中也可以包含具有10-30个碳原子的脂肪酸作为化妆品可接受的载体。这种脂肪酸的示例包括壬酸、月桂酸、肉豆蔻酸、棕榈酸、硬脂酸、异硬脂酸、油酸、亚油酸、花生酸、山酸或芥酸以及其混合物。被认为会增强皮肤渗透的化合物如二甲亚砜也可以用作任选的载体。
多元醇类的保湿剂也可用于本发明的化妆品组合物。保湿剂经常有助于增强润肤剂的效能、减少起皮、促进积累污垢的去除,并改善皮肤触感。典型的多元醇包括丙三醇、聚二醇,更优选亚烷基多羟基化合物及其衍生物,包括丙二醇、二丙二醇醚、聚丙二醇、聚乙二醇及其衍生物,山梨醇、羟丙基山梨醇、已二醇、1,3-丁二醇、1,2,6-己三醇、乙氧基化丙三醇、丙氧基化丙三醇及其混合物。为达到最好的效果,保湿剂优选为丙二醇或透明质酸钠。以所述化妆品组合物的总重量为基准,保湿剂的量可以是0.2-25重量%,优选0.5-15重量%范围内的任何数量,也包括其中包容所有的数值范围。
增稠剂也可以用作本发明化妆品组合物中化妆品可接受的载体的一部分。典型的增稠剂包括交联的丙烯酸酯(例如Carbopol 982)、疏水改性的丙烯酸酯(例如Carbopol1382)、纤维素衍生物以及天然树胶。有用的纤维素衍生物中有羧甲基纤维素钠、羟丙基甲基纤维素、羟丙基纤维素、羟乙基纤维素、乙基纤维素以及羟甲基纤维素。适用于本发明的天然树胶包括瓜耳胶、黄原胶、菌核、角叉菜胶、果胶以及这些树胶的组合。所述增稠剂的量可以为0.0-5重量%,通常为0.001-1重量%,最优为0.01-0.5重量%。
水、溶剂、硅酮、酯、脂肪酸、保湿剂和/或增稠剂总计组成1-99.9重量%,优选80-99重量%的所述化妆品可接受的载体。
本发明的化妆品组合物中也可以含表面活性剂。表面活性剂的总浓度为所述组合物的0-40重量%,优选0-20重量%,最优为0-5重量%。所述表面活性剂可以选自阴离子型、非离子型、阳离子型以及两性的活性物。特别优选的非离子型表面活性剂是C10-C20脂肪醇或酸疏水质,其与每摩尔疏水质2-100摩尔的环氧乙烷或环氧丙烷进行缩合;C2-C10烷基酚,其与2-20摩尔的环氧烷缩合;乙二醇的单和二脂肪酸酯;脂肪酸单酸甘油酯;脱水山梨糖醇、单和二C8-C20脂肪酸;嵌段共聚物(环氧乙烷/环氧丙烷);和聚氧乙烯脱水山梨糖醇,及其组合。烷基多苷和糖脂肪酰胺(例如甲基葡糖酰胺)也是适合的非离子型表面活性剂。
优选的阴离子表面活性剂包括皂、烷基醚硫酸盐和磺酸盐、烷基硫酸盐和磺酸盐、烷基苯磺酸盐、烷基和二烷基磺基丁二酸盐、C8-C20酰基异硫代硫酸盐、酰基谷氨酸盐、C8-C20烷基醚磷酸盐及其组合。
香料可用于本发明的化妆品组合物。可使用的香料种类示例的非限制性实例包括包含萜烯以及萜烯衍生物的那些,如Bauer,K.等人所著Common Fragrance and FlavorMaterials.VCH Publishers(1990)中所述的那些。
可用于本发明的香料种类的又一示例非限制性实例包括桂叶烯、二氢桂叶醇、柠檬醛、万寿菊酮、顺-香叶酸、香茅酸或顺香叶酸腈、其混合物,等等。
优选,用于本发明化妆品组合物的香料的量为0.0-10wt%,更优选0.00001-5wt%,最优选0.0001-2wt%。
各种类型的任选附加活性成分可用于本发明化妆品组合物中。“活性成分”定义为除润肤剂及其它仅仅改善所述组合物的物理特性的成分之外的皮肤有益试剂。虽然不限于这个种类,通常实例包括滑石和二氧化硅,以及α-羟基酸,β-羟基酸,过氧化合物,锌盐和防晒剂。
β-羟基酸包括例如水杨酸。氧巯基吡啶锌是用于本发明化妆品组合物的所述锌盐的实例。
防晒剂包括常用于阻挡紫外线的材料。示例的化合物是PABA的衍生物、肉桂酸酯和水杨酸酯。例如,可以使用丁基甲氧基二苯甲酰基甲烷(avobenzophenone)(Parsol)、甲氧基肉桂酸辛酯和2-羟基-4-甲氧基苯酮(也称作氧苯酮)。甲氧基肉桂酸辛酯和2-羟基-4-甲氧基苯酮分别以商标Parsol MCX和Benzophenone-e市售。用于所述组合物的防晒剂的精确量可以根据希望对太阳的紫外辐射的防护程度而变化。也可以使用反射或散射太阳光线的添加剂。这些添加剂包括氧化物,如氧化锌和二氧化钛。
许多化妆品组合物,尤其是那些含水的化妆品组合物,应该避免潜在有害微生物的生长。抗微生物的化合物,如三氯生(triclosan),和防腐剂通常是必要的。适合的防腐剂包括对羟基苯甲酸的烷基酯、乙内酰脲衍生物、丙酸盐和各种季铵化合物。本发明特别优选的防腐剂是对羟苯甲酸甲酯、对羟苯甲酸丙酯、苯氧乙醇和苯甲醇。防腐剂通常用量为所述组合物的0.1-2重量%。
可用于本发明化妆品组合物的另外的其它任选成分包括二元酸(例如丙二酸和癸二酸)、抗氧化剂如维生素E、维生素如烟酰胺和维生素C和其衍生物、间苯二酚及其衍生物(包括用例如阿魏酸、香草酸等等酯化的那些)和类视黄醇,包括视黄酸、视黄醛、视黄醇和视黄酯、共轭亚油酸、岩芹酸和其混合物,以及任何用于减少皱纹、皮肤增白、消除粉刺和降低皮脂影响的其它已知常规成分。
本发明化妆品组合物意在主要用作局部施用于人皮肤的产品,尤其是至少用作用于增亮所述皮肤的产品。因此,发明人已经发现,所述脂族酸具有优异的皮肤增亮能力,从而其可以在局部化妆品组合物中用作皮肤增亮添加剂,所述局部化妆品组合物局部应用于皮肤上希望增亮或增白的区域。其它的好处可以包括润湿皮肤、减少皮脂对皮肤的影响和减少皮肤皱纹。通常本发明的化妆品组合物的熔点为30-45℃,包括其中包容的所有范围。在一个尤其优选的实施方案中,本发明的化妆品组合物的pH为4.5-7.5,包括其中包容的所有范围。
在制备本发明化妆品组合物时,在温度为70-80℃,在大气压力下,混合希望的成分,没有特别的顺序。
本发明组合物的包装可以是贴片、瓶子、管、走珠施用器、推进剂驱动的气溶胶器件、压挤容器或加盖的罐子。
随后提供的实施例用于举例说明和帮助理解本发明。所述实施例不意在限制权利要求的范围。
实施例
获得市售的人皮肤等同物(来自MatTek的MelanoDermTM),以测试杂取代的饱和或不饱和脂族酸对黑色素生成的影响。从10毫摩尔二甲亚砜母液制备最终浓度为0.1-5微摩尔的溶液,在三周期间内加料十次到MelanoDerm培养物的介质中。根据生产商的说明书制备和处理由市售基础Dulbecco's Modified Eagles media组成的培养基。为长期维护保养MelanoDerms,向所述基础培养基中补充碱性成纤维细胞生长因子(bFGF)和α促黑素细胞激素(MSH),以刺激黑色素细胞形成和黑色素生成。各处理条件是双份的,对各处理以及对对照(未用所述脂族酸处理的培养物)制备三组。所述培养物维持在37℃的温度下,并在加料期间,在加湿的5%二氧化碳细菌培养箱中培养,但是在进行加料时移去。
在三周时间之后,取出MelanoDerm培养物,并在60℃的烘箱中,以十六小时(过夜),溶解在装有250微升溶解反应剂(GNE 9100,Packard)的离心机试管中。在溶解之后,在12,000g下旋转装有样品的所述离心机试管五分钟。取出200微升上清液,并放入96孔培养盘中。用分光光度计在490nm测定所述上清液的吸光度。平行建立使用合成黑色素的标准曲线,以定量化样品中的黑色素,以微克计。所述结果提供如下:
表:
i=蓖麻油酸(0.1μM),
ii=12-羟基硬脂酸(5μM),
*MC=黑色素含量,
所述结果涉及MelanoDerm培养物,其表明具有本发明脂族酸的化妆品组合物出人预料地导致皮肤增亮。
Claims (17)
1.用于增亮皮肤的非治疗目的的方法,其包括如下步骤:
a)确定需要皮肤增亮的皮肤;
b)使所述皮肤与包含如下物质的组合物接触:
0.001至15重量%的皮肤增亮添加剂,所述皮肤增亮添加剂选自(a)蓖麻油酸和12-羟基硬脂酸,和(b)12-羟基硬脂酸和烟酰胺;和
化妆品载体;以及
c)增亮皮肤。
2.根据权利要求1所述的方法,其中所述组合物还包含α-羟基酸、β-羟基酸、防晒剂或它们的混合物。
3.根据权利要求1所述的方法,其中所述组合物还包含共轭亚油酸、岩芹酸或这两者。
4.根据权利要求1所述的方法,其中所述组合物还包含维生素E。
5.根据权利要求1所述的方法,其中所述组合物包含选自以下的组分:紫胶桐酸、9,10,18-三羟基十八烷酸、9,10,13-三羟基-11-十八烷酸、9,13-二羟基-12-乙氧基-10-十八烷酸、9-羟基-10,12-十八烷酸、4,14-二羟基-十八烷酸、14-羟基-顺-11-二十碳烯酸、反蓖麻酸、黄葵酸、β-9-羟基-10,12-十八碳二烯酸、12-羟基-9,15-十八碳二烯酸、8-甲氧基-13-羟基-9,11-十八烷酸、7-氧-十八烷酸、9-氧-十八烷酸、12-氧-十八烷酸、10-氧-14-甲基-十五烷酸,或它们的混合物。
6.根据权利要求1所述的方法,其中所述组合物还包含12-氧-十八烷酸。
7.根据权利要求1所述的方法,其中增亮皮肤的添加剂占所述组合物的0.1至12重量%。
8.根据权利要求1所述的方法,其中增亮皮肤的添加剂占所述组合物的0.1至10重量%。
9.根据权利要求1所述的方法,其中所述组合物为液体、乳膏、凝胶或调色剂的形式,或者借助贴片或面膜施用。
10.根据权利要求1所述的方法,其中将所述组合物直接施用到皮肤上以增亮需要皮肤增亮的斑点。
11.根据权利要求1所述的方法,其中将所述组合物直接施用到皮肤上以降低黑色素生成,并且所述组合物包含间苯二酚。
12.根据权利要求1所述的方法,其中所述组合物还包含防晒剂、防腐剂、纤维素衍生物、维生素C,或它们的混合物。
13.根据权利要求12所述的方法,其中所述防晒剂选自二氧化钛和氧化锌。
14.根据权利要求1所述的方法,其中所述皮肤是脸上或手上的皮肤,并且所述组合物包含增稠剂、甲氧基肉桂酸辛酯或这两者。
15.根据权利要求1所述的方法,其中所述组合物为驻留型乳液、乳膏或清液。
16.根据权利要求1所述的方法,其中所述组合物还包含防晒剂,并且具有4.5至7.5的pH值。
17.根据权利要求1所述的方法,其中所述组合物还包含苯氧乙醇。
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