CN1913866B - 减少皮肤色素沉着的整体组合物及方法 - Google Patents
减少皮肤色素沉着的整体组合物及方法 Download PDFInfo
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- CN1913866B CN1913866B CN2005800034346A CN200580003434A CN1913866B CN 1913866 B CN1913866 B CN 1913866B CN 2005800034346 A CN2005800034346 A CN 2005800034346A CN 200580003434 A CN200580003434 A CN 200580003434A CN 1913866 B CN1913866 B CN 1913866B
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- ascorbyl
- extract
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- ascorbic acid
- phosphate
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Abstract
本发明提供一种减少皮肤色素沉着的整体组合物和方法。
Description
本发明涉及减少皮肤色素沉着的整体组合物及方法,其包括多重色素沉着抑制剂、细胞保护剂、和功能性成分穿透增强剂。
目前需要减少皮肤色素沉着的产品。但是,由于色素产生包括许多途径,因此减少皮肤色素沉着的能力是复杂的。
黑素细胞是皮肤中的产生色素的细胞。黑素细胞产生两种形式的黑素、或皮肤色素,较深的真黑素和较浅的浅黑素。各类型黑素的数量决定人皮肤中色素沉着的颜色和程度。
黑素细胞产生黑素通过一系列的包括酪氨酸到多巴(Dopa)的转变的复杂的细胞进程,如图1所示。酪氨酸酶是负责这种转化的酶而且是黑素生物合成中涉及的主要酶。而多巴通过各种生物化学途径转化为真黑素或浅黑素。黑素一旦产生,其从存在于表皮下层的黑素细胞转移到见于表皮上层的角质化细胞。这种转移通过称为黑素体的黑素运送小囊而发生。
酪氨酸酶的产生和活性决定产生黑素的数量。转移到角质化细胞的黑素的数量和类型决定人的皮肤将出现怎样的着色。因此,如果一个人想使皮肤变白,调节酪氨酸酶的产生和活性、黑素体转移的黑素、以及真黑素与浅黑素之比是有用的。
除了提供皮肤颜色,黑素还用作阳光保护剂。黑素吸收有害的UV射线,以便使由UV诱导的自由基引起的损害最小化。因此,如果黑素的数量减少,那么提供一种UV保护的替换方式是有用的。
因此,目前需要通过调节黑素生成和转移途径中多个步骤以减少皮肤色素沉着,以及一旦色素沉着已被减少后的保护皮肤的方法。此外,还需要增加功能性成分的穿透力的方法。
本发明的整体方法通过形成本发明组合物的功能性成分的组合效果提高了皮肤增白的功效,本发明的功能除了提供细胞保护和强化功能性成分的穿透力,还涉及皮肤色素产生和转移的多个方面。
在一个方面,当前要求保护的发明是减少皮肤色素沉着的组合物。所述组合物包括功能性成分;酪氨酸酶产生抑制剂、酪氨酸酶活性抑制剂、黑素聚合作用竞争性抑制剂、抑制黑素转移到角质化细胞 的成分、改变真黑素与浅黑素之比的成分、以及通过脱落使皮肤变亮的成分。此外,此组合物可以含有细胞保护剂,其包括功能性成分;基质金属蛋白酶抑制剂、抗氧化剂、阳光保护剂、细胞代谢刺激剂、以及炎症抑制剂。此组合物还可以包括至少一种功能性成分穿透增强剂。此功能性成分穿透增强剂可以是水溶的和/或油溶的成分。
在第二方面,当前要求保护的发明涉及减少皮肤色素沉着的方法。此方法包括对皮肤应用组合物。所述组合物包括功能性成分;酪氨酸酶产生抑制剂、酪氨酸酶活性抑制剂、黑素聚合作用竞争性抑制剂、抑制黑素转移到角质化细胞的成分、改变真黑素与浅黑素之比的成分、以及通过脱落使皮肤变亮的成分。此外,此组合物可以含有细胞保护剂,其包括功能性成分;基质金属蛋白酶抑制剂、抗氧化剂、阳光保护剂、细胞代谢刺激剂、以及炎症抑制剂。此组合物还可以包括至少一种功能性成分穿透增强剂。此功能性成分穿透增强剂可以是水溶的和/或油溶的成分。
附图简要说明
图1是黑素生成途径的说明。
图2表示在以当前要求保护的发明的整体组合物治疗后的皮肤样本中减少的黑素含量。
图3表示以当前要求保护的发明的整体组合物孵化一周之后的皮肤模型。
图4表示以当前要求保护的发明所述的整体组合物孵化两周之后的皮肤模型。
图5是来自于体内研究的结果的表格,所述研究说明斑点色素沉着、皮肤色调和皮肤透明度的改善。
发明详述
本发明提供减少皮肤色素沉着的整体的组合物及方法。此整体方法包括在沿着生物合成途径的许多位置抑制黑素产生和转移。由于皮肤中的色素沉着减少,使皮肤易于受到UV和氧化作用的损害,所述整体方法还提供皮肤保护剂。此外,加强这些功能性成分的穿透力也被这种整体方法所考虑。
因此,此发明包括3个主要方面:(I)色素沉着机制抑制剂;(II)细胞保护剂;以及(III)功能性成分穿透增强剂。
本发明的色素沉着机制抑制剂包括:(1)酪氨酸酶产生抑制剂,(2)酪氨酸酶活性抑制剂,(3)黑素聚合作用抑制剂,(4)真黑素与浅黑素之比的调节物,(5)黑素体从黑素细胞到角质化细胞的转移抑制剂,以及(6)皮肤脱落剂(exfoliator)。
由于减少酶的产生将导致黑素产生的减少,因此抑制酪氨酸酶的产生是一种减少皮肤色素沉着的方法。酪氨酸酶产生抑制剂包括,但不限于六聚肽-2(hexapeptide-2)。
抑制酪氨酸酶活性是减少黑素生成的同样有用的类似方法。以下化合物,或单独或组合,可以是有用的适于本发明的酪氨酸酶活性抑制剂:抗坏血酸及其衍生物,诸如L-抗坏血酸烷基酯,诸如L-抗坏血酸棕榈酸酯(palmitrate)、L-抗坏血酸异棕榈酸酯、L-抗坏血酸二棕榈酸酯、L-抗坏血酸异硬脂酸酯、L-抗坏血酸二硬脂酸酯、L-抗坏血酸二异硬脂酸酯、L-抗坏血酸肉豆蔻酸酯、L-抗坏血酸异肉豆蔻酸酯、L-抗坏血酸2-乙基己酸酯、L-抗坏血酸二-2-乙基己酸酯、L-抗坏血酸油酸酯、L-抗坏血酸二油酸酯;L-抗坏血酸磷酸酯,诸如L-抗坏血酸-2-磷酸酯和L-抗坏血酸-3-磷酸酯;L-抗坏血酸硫酸酯,诸如L-抗坏血酸-2-硫酸酯和L-抗坏血酸-3-硫酸酯;它们与诸如钙、钠和镁等碱土金属的盐;曲酸;熊果(arctostaphylos uva ursi,bearberry)叶提取物;甘草(glycyrrhiza glabra,licorice)提取物;地榆(sanguisorba officinalis,burnet)提取物;黄岑(scutellaria baicalensis,skull cap)根提取物;和桑树(morus alba,mulberry)提取物。
黑素聚合作用竞争性抑制是另一种减少黑素生成的方法。诸如那些富含咖啡酸(cafeic acid)的在聚合过程中与DOPA竞争的化合物使DOPA聚合速率降低,并因此导致黑素生成降低。以下单独的或组合的成分可以用于竞争地抑制黑素聚合:富含咖啡酸的提取物;和向日葵(helianthus annus,sunflower)籽提取物。
减少皮肤色素沉着出现的另一方法是改变真黑素与浅黑素之比,从而使得更浅的浅黑素成为主导。能够改变真黑素与浅黑素之比的成分的一个例子是小麦(triticum vulgare,wheat)胚芽提取物。
抑制黑素体将黑素从黑素细胞转移到角质化细胞是另一种减少皮 肤色素沉着现象的方法。皮肤色素沉着受到转移到角质化细胞的黑素体的数量的控制,因此通过抑制这种转移,皮肤色素沉着将可能被减少。含有凝集素的植物提取物,包括小麦胚芽提取物,可用于抑制黑素转移到角质化细胞。
通过脱落使皮肤变亮是减少皮肤色度沉着现象的另外的方法。下述或单独的或组合的成分可用于加速皮肤脱落:抗坏血酸磷酸镁、抗坏血酸磷酸钠、抗坏血酸磷酸钙、燕麦(avena sativa,oat)籽提取物;以及糖蛋白。
本发明的细胞保护剂包括:(1)基质金属蛋白酶(MMP)抑制剂;(2)抗氧化剂;(3)阳光保护剂;(4)细胞代谢刺激剂;以及(5)炎症和/或炎性后高度色素沉着抑制剂。
MMP抑制剂作为细胞保护剂是有用的。UV射线激活皮肤中的MMPs。过度活化的MMPs降解胶原和弹性蛋白并因此加速皮肤老化进程。当抑制MMP活性时皮肤被保护。马铃薯(solanum tuberosum,potato)提取物是用于抑制MMP活性的成分的一个实例。
抗氧化剂是强大的细胞保护剂。通过UV射线以及通过正常代谢过程产生有害的自由基。抗氧化剂帮助中和自由基并因此保护细胞的完整性和功能。下述或单独的或组合的成分可以用作抗氧化剂:抗坏血酸及衍生物,诸如抗坏血酸磷酸钠和/或镁;向日葵籽提取物;柑桔(citrus unshiu)皮提取物;柠檬(citrus medica limonum,lemon)提取物;黄瓜(cucumis sativus,cucumber)果实提取物;甘草提取物;生育酚、及生育酚衍生物,诸如维生素E磷酸(VEP)钠、月桂基亚氨基二丙酸生育酚磷酸酯(Lauryl Imino Dipropionic Acid Tocopheryl Phosphate)、生育酚葡糖苷、生育酚琥珀酸酯、托可索仑(Tocophersolan,聚乙二醇1000生育酚琥珀酸酯)、月桂基亚氨基二丙酸生育酚磷酸二钠(Disodium laurimino dipropionate tocopheryl phosphate)、Tocophereth-5,10,12,18,和50(聚乙二醇(PEG)生育酚酯)、维生素E磷酸(VEP)钠、月桂基亚氨基二丙酸生育酚磷酸酯、月桂基亚氨基二丙酸生育酚磷酸二钠。
有机和无机的阳光保护剂使皮肤对有害的阳光/UV射线的暴露最小化。以下或单独的或是组合的成分可以用作UV保护剂:甲氧基肉桂酸辛酯(Octinoxate)和二氧化钛。
细胞代谢刺激剂导致更加抗环境损害的更健康的皮肤。例如,糖蛋白是刺激细胞代谢的有效成分。
炎症和/或炎症后高度色素沉着抑制剂也用作细胞保护剂。以下或单独的或是组合的成分可以用于抑制炎症和相关的高度色素沉着:α-葡聚寡糖;甘草酸二钾;甘草提取物;尿囊素;燕麦籽提取物;桑树提取物;以及黄瓜果实提取物。
本发明减少皮肤色素沉着的整体方法还涉及运输上述功能性成分的方面。为了实现所述功能性成分的益处,它们必须能够穿透皮肤并到达它们的作用位点。提高功能性成分的穿透力导致皮肤色素沉着更加显著减少。双重穿透增强系统包括产品的水相中的水溶性穿透增强剂和产品的油相中的油溶性穿透增强剂。适合的水溶性穿透增强剂的例子是乙氧基二甘醇。适合的油溶性穿透增强剂的例子是PPG-12/SMDI共聚物。
本发明适用于减少总体色素沉着以及用于改善不均匀的色素沉着。本发明可以采用的形式包括,但不限于:乳剂、洗剂、爽肤水(toner)、条、糊剂,或任何适用于对皮肤局部给药的其它介质。
本发明的组合物可以用于整个身体,包括脸部。该组合物可以根据需要施用,或替换的作为皮肤护理常规程序的一部分而施用。优选的,该组合物每周施用。更优选的,该组合物每日施用一次或两次。当组合物每日施用两次时,优选的方式为一次在早晨,一次在晚上。当组合物每日施用两次的时候,每次施用的所述组合物可以是相同的或不同的。例如,相同的组合物可以每日施用两次,或替换的,一种组合物可以在早晨施用,第二种不同的组合物可以在晚上施用。
本发明的方法包括将以上描述的组合物施用于皮肤。
以下实施例意图为说明并非限制本发明。
实施例1
体外功效测试在3-D重建的皮肤模型上进行。此皮肤模型包含角质层、表皮层、和真皮层。黑素细胞存在于此皮肤模型中。接下来,使用该整体组合物的3种不同的配方之一或对照每周治疗3.5次持续三周,分析皮肤样本。提取所含的黑素并用分光光度计测量。在图2中示出的结果说明以整体组合物的三种不同配方治疗后黑素含量减少,组合物的活性成分在表1-3中示出。图2中的图表说明本发明减少皮肤 中黑素含量的有效性。与对照比较,所有三种测试配方都减少黑素含量30%以上。
表4显示了另一示范性的配方。配方1-4的活性成分以总体积的百分比给出。但是,本领域技术人员可以改变此百分比以适应所需的特定类型组合物。此外,可以与本发明一同使用的载体、缓冲剂、芳香剂等是广泛熟知的并易于由本领域技术人员选定。
表1
活性成分 | 配方1 |
α-葡聚寡糖 | 0.50 |
甘草酸二钾 | 0.50 |
糖蛋白 | 0.05 |
水解马铃薯蛋白 | 0.01 |
燕麦提取物 | 0.01 |
柑桔皮提取物 | 1.00 |
六聚肽-2 | 0.50 |
乙氧基二甘醇 | 0.50 |
抗坏血酸磷酸钠 | 3.00 |
桑树(Morus Bombycis)提取物甘草提取物地榆提取物黄岑根提取物 | 1.50 |
柠檬提取物黄瓜提取物 | 0.50 |
向日葵籽提取物 | 0.01 |
熊果叶提取物抗坏血酸磷酸镁 | 0.50 |
小麦胚芽提取物 | 0.01 |
尿囊素 | 0.05 |
载体、辅剂、药物化妆品(Cosmeceuticals) | Q.S. |
总和 | 100.00 |
[0043] 表2
活性成分 | 配方2 |
甘草酸二钾 | 0.01 |
糖蛋白 | 0.05 |
水解马铃薯蛋白 | 0.10 |
燕麦提取物 | 0.50 |
PPG-12/SMDI共聚物 | 0.10 |
柑桔皮提取物 | 1.00 |
六聚肽-2 | 0.05 |
乙氧基二甘醇 | 0.25 |
桑树提取物甘草提取物地榆提取物黄岑根提取物 | 0.50 |
抗坏血酸磷酸钠 | 3.00 |
柠檬提取物黄瓜提取物 | 0.50 |
向日葵籽提取物 | 0.05 |
生育酚醋酸酯 | 1.0 |
熊果叶提取物抗坏血酸磷酸镁水、丙三醇 | 0.10 |
小麦胚芽提取物 | 0.05 |
尿囊素 | 0.10 |
载体、辅剂、药物化妆品 | Q.S. |
总和 | 100.00 |
[0045] 表3
活性成分 | 配方3 |
糖蛋白 | 0.05 |
水解马铃薯蛋白 | 0.10 |
燕麦提取物水 | 1.00 |
柑桔皮提取物 | 1.00 |
六聚肽-2(Hexapeptide-2) | 0.05 |
乙氧基二甘醇 | 0.25 |
PPG-12/SMDI共聚物 | 0.25 |
桑树提取物甘草提取物地榆提取物黄岑根提取物 | 0.50 |
抗坏血酸磷酸钠 | 3.00 |
柠檬提取物黄瓜提取物 | 0.50 |
向日葵籽提取物 | 0.05 |
生育酚醋酸酯 | 0.50 |
熊果叶提取物抗坏血酸磷酸镁 | 0.1 |
小麦胚芽提取物 | 0.05 |
载体、辅剂、药物化妆品 | Q.S. |
总和 | 100.00 |
[0047] 表4
活性成分 | 配方4 |
二氧化钛 | 7.0 |
甘草酸二钾 | 0.02 |
糖蛋白 | 0.01 |
水解马铃薯蛋白 | 0.01 |
燕麦提取物 | 0.01 |
甲氧基肉桂酸辛酯 | 7.50 |
柑桔皮提取物 | 1.00 |
六聚肽-2 | 0.50 |
乙氧基二甘醇 | 0.50 |
向日葵籽提取物 | 0.01 |
桑树提取物甘草提取物地榆提取物黄岑根提取物 | 1.00 |
抗坏血酸磷酸钠 | 3.00 |
柠檬提取物黄瓜提取物 | 0.50 |
生育酚 | 0.10 |
熊果叶提取物抗坏血酸磷酸镁 | 0.50 |
小麦胚芽提取物 | 0.01 |
载体、辅剂药物化妆品 | Q.S. |
总和 | 100.00 |
参考图3和4,在以配方2的整体组合物分别孵化一周和两周之后,与对照相比显示3-D皮肤模型。皮肤模型中的黑点是在皮肤模型表面上的负载黑素体的角质化细胞。此示出的模型代表功效测试中得到的结果。被治疗的皮肤的色素沉着现象的变化大于黑素含量的百分 比变化。这样的原因是双重的。不受任何特定理论所束缚,人们相信(1)黑素体转移抑制和(2)真黑素与浅黑素之比的改变导致了较浅的浅黑素的优势,这为色素沉着现象的惊人的减少而负责。根据黑素体转移抑制理论,虽然仍旧产生黑素,但其不转移到角质化细胞。因此,即使黑素存在,其是不可见的,且皮肤呈现比其实际上的更少的着色。类似的,真黑素与浅黑素之比的改变引起皮肤呈现为更加明亮(lighter)。即使总体黑素含量可能是相同的,以浅黑素作为黑素主导形式的皮肤比带有更高含量的更黑的真黑素的皮肤呈现为更明亮的。因此,增加浅黑素的含量并降低真黑素的含量将引起皮肤呈现为更少着色。通过使用多重抑制法,达到了皮肤色素沉着现象惊人的降低。
实施例2
进行体内研究,在研究中测量皮肤透明度(clarity)、皮肤色调和斑点色素沉着的变化。在12周的期间内研究54位女性受试者。受试者的年龄在25和65岁之间并检测轻微到中等的面部斑点高度色素沉着的存在。采用了10cm的模拟标准(analog scale),其中,0分表示没有斑点高度色素沉着,10分表示非常黑的过分色素沉着。具有分数在3和8之间的受试者有资格参与所述研究且这些原始分数用作所述研究的基线值。受试者以皮肤增白方案治疗,包括四种增白产品,每日施用两次,三种产品在早上以及三种在晚上,持续12周。斑点色素沉着、皮肤透明度和皮肤色调的变化在2、4、8和12周通过临床分级器测量。研究结果报告为从基线的百分比变化并在图5中示出。皮肤色调、皮肤透明度和斑点色素沉着的显著改善早在进入研究的2周时被记录。在12周的时候,皮肤色调和斑点色素沉着有大于20%的改善,且皮肤透明度有几乎30%的改善。
有利的,本发明提供通过靶向黑素产生和转移的多个途径而减少皮肤色素沉着的整体方法。此外,还提供了细胞保护剂和功能性成分的增强穿透力。
因此,前述详细说明应被认为是说明性的而非限制性的,应当理解,以下的权利要求包括所有等同物意为限定本发明的主旨和范围。
Claims (21)
1.一种减少皮肤色素沉着的组合物,其包括:
a.多重色素沉着抑制剂,其包括选自由以下组成的组的至少5种成分:
i.六聚肽-2,
ii.至少一种酪氨酸酶活性抑制剂,选自抗坏血酸、抗坏血酸衍生物、熊果叶提取物、甘草提取物、地榆提取物、黄岑根提取物、桑树提取物、及其混合物组成的组;其中所述抗坏血酸衍生物选自L-抗坏血酸烷基酯,L-抗坏血酸磷酸酯,L-抗坏血酸硫酸酯,它们与碱土金属的盐,抗坏血酸与钠的盐,及其混合物组成的组;
iii.黑素聚合作用竞争性抑制剂,选自富含咖啡酸的化合物和向日葵籽提取物;
iv.抑制黑素体到角质化细胞的转移的成分,选自包含凝集素的植物提取物和小麦胚芽提取物;
v.改变真黑素与浅黑素之比率的成分,由小麦胚芽提取物组成;
vi.通过脱落使所述皮肤变亮的成分,选自抗坏血酸磷酸钠、抗坏血酸磷酸钙、抗坏血酸磷酸镁、燕麦籽提取物、糖蛋白、及其混合物组成的组;
b.细胞保护剂,其包括选自由以下组成的组的至少4种成分:
i.马铃薯提取物,
ii.抗氧化剂,选自抗坏血酸、抗坏血酸磷酸钠、抗坏血酸磷酸镁、向日葵籽提取物、柑桔皮提取物、柠檬提取物、黄瓜果实提取物、甘草提取物、生育酚和生育酚衍生物、及其混合物组成的组;其中所述的生育酚衍生物选自维生素E磷酸钠、月桂基亚氨基二丙酸生育酚磷酸酯、生育酚葡糖苷、生育酚琥珀酸酯、托可索仑、月桂基亚氨基二丙酸生育酚磷酸二钠、
Tocophereth-5,10,12,18,和50;
iii.阳光保护剂,选自甲氧基肉桂酸辛酯、二氧化钛、及其混合物组成的组,
iv.细胞代谢刺激剂,包括一种或更多种糖蛋白,和
v.炎症抑制剂,选自α-葡聚寡糖、甘草酸二钾、甘草提取物、尿囊素、燕麦籽提取物、桑树提取物、黄瓜果实提取物、及其混合物组成的组;及
c.至少一种功能性成分穿透增强剂,其选自水溶性穿透增强剂成分和油溶性穿透增强剂成分组成的组。
2.如权利要求1所述的组合物,其中所述L-抗坏血酸烷基酯选自由L-抗坏血酸棕榈酸酯、L-抗坏血酸异棕榈酸酯、L-抗坏血酸二棕榈酸酯、L-抗坏血酸异硬脂酸酯、L-抗坏血酸二硬脂酸酯、L-抗坏血酸二异硬脂酸酯、L-抗坏血酸肉豆蔻酸酯、L-抗坏血酸异肉豆蔻酸酯、L-抗坏血酸2-乙基己酸酯、L-抗坏血酸二-2-乙基己酸酯、L-抗坏血酸油酸酯和L-抗坏血酸二油酸酯构成的组。
3.如权利要求1所述的组合物,其中所述L-抗坏血酸磷酸酯选自由L-抗坏血酸-2-磷酸酯和L-抗坏血酸-3-磷酸酯构成的组。
4.如权利要求1所述的组合物,其中所述L-抗坏血酸硫酸酯选自由L-抗坏血酸-2-硫酸酯和L-抗坏血酸-3-硫酸酯构成的组。
5.如权利要求1-4之一所述的组合物,其中所述酪氨酸酶活性抑制剂由熊果叶提取物组成。
6.如权利要求5所述的组合物,其中抑制黑素体到角质化细胞的所述转移的所述成分由小麦胚芽提取物组成。
7.如权利要求5所述的组合物,其中所述通过脱落使所述皮肤变亮的所述成分由抗坏血酸磷酸钠组成。
8.如权利要求1-4之一所述的组合物,其中所述阳光保护剂是选自甲氧基肉桂酸辛酯、二氧化钛、及其混合物组成的组。
9.如权利要求1-4之一所述的组合物,其中所述细胞代谢刺激剂包括一种或更多种糖蛋白。
10.如权利要求1-4之一所述的组合物,其中所述炎症抑制剂是选自α-葡聚寡糖、甘草酸二钾、甘草提取物、尿囊素、燕麦籽提取物、桑树提取物、黄瓜果实提取物、及其混合物组成的组。
11.如权利要求1-4之一所述的组合物,其中所述水溶性穿透增强剂包括乙氧基二甘醇。
12.如权利要求1-4之一所述的组合物,其中所述油溶性穿透增强剂包括PPG-12/SMDI共聚物。
13.组合物用于制备通过将该组合物施用于皮肤来减少皮肤色素沉着的药物的用途,所述组合物包括:
a.多重色素沉着抑制剂,其包括选自六聚肽-2、酪氨酸酶活性抑制剂、黑素聚合作用竞争性抑制剂、抑制黑素体到角质化细胞的转移的成分、改变真黑素与浅黑素之比率的成分、以及通过脱落使所述皮肤变亮的成分组成的组的至少5种成分;
其中所述酪氨酸酶活性抑制剂选自抗坏血酸、抗坏血酸衍生物、曲酸、熊果叶提取物、甘草提取物、地榆提取物、黄岑根提取物、白桑(morus alba)提取物、鸡桑(morus bombycis)提取物、及其混合物组成的组;其中所述抗坏血酸衍生物选自L-抗坏血酸烷基酯,L-抗坏血酸磷酸酯,L-抗坏血酸硫酸酯,它们与碱土金属的盐,抗坏血酸与钠的盐,及其混合物组成的组;
所述黑素聚合作用竞争性抑制剂选自包含咖啡酸的化合物和向日葵籽提取物;
所述抑制黑素体到角质化细胞的转移的成分选自包含凝集素的植物提取物和小麦胚芽提取物;
所述改变真黑素与浅黑素之比率的成分由小麦胚芽提取物组成;
所述通过脱落使所述皮肤变亮的成分选自抗坏血酸磷酸钠、抗坏血酸磷酸钙、抗坏血酸磷酸镁、燕麦籽提取物、糖蛋白、及其混合物组成的组;
b.细胞保护剂,其包括选自马铃薯提取物、抗氧化剂、阳光保护剂、细胞代谢刺激剂、和炎症抑制剂组成的组的至少4种成分;以及
c.至少一种功能性成分穿透增强剂,其选自水溶性穿透增强剂和油溶性穿透增强剂组成的组。
14.如权利要求13所述的用途,其中所述L-抗坏血酸烷基酯选自由L-抗坏血酸棕榈酸酯、L-抗坏血酸异棕榈酸酯、L-抗坏血酸二棕榈酸酯、L-抗坏血酸异硬脂酸酯、L-抗坏血酸二硬脂酸酯、L-抗坏血酸二异硬脂酸酯、L-抗坏血酸肉豆蔻酸酯、L-抗坏血酸异肉豆蔻酸酯、L-抗坏血酸2-乙基己酸酯、L-抗坏血酸二-2-乙基己酸酯、L-抗坏血酸油酸酯和L-抗坏血酸二油酸酯构成的组。
15.如权利要求13所述的用途,其中所述L-抗坏血酸磷酸酯选自由L-抗坏血酸-2-磷酸酯和L-抗坏血酸-3-磷酸酯构成的组。
16.如权利要求13所述的用途,其中所述L-抗坏血酸硫酸酯选自由L-抗坏血酸-2-硫酸酯和L-抗坏血酸-3-硫酸酯构成的组。
17.如权利要求14-16之一所述的用途,其中所述多重色素沉着抑制剂包括的成分选自六聚肽-2、抗坏血酸、抗坏血酸衍生物、熊果叶提取物、甘草提取物、地榆提取物、黄岑根提取物、桑树提取物、包含咖啡酸的化合物、向日葵籽提取物、小麦胚芽提取物、包含凝集素的植物提取物和小麦胚芽、曲酸、燕麦籽提取物、糖蛋白、及其混合物组成的组;其中所述抗坏血酸衍生物选自L-抗坏血酸烷基酯,L-抗坏血酸磷酸酯,L-抗坏血酸硫酸酯,它们与碱土金属的盐,抗坏血酸与钠的盐,及其混合物组成的组。
18.如权利要求14-16之一所述的用途,其中所述细胞保护剂包括的成分选自抗坏血酸、抗坏血酸磷酸钠、抗坏血酸磷酸镁、向日葵籽提取物、柑桔皮提取物、柠檬提取物、黄瓜果实提取物、甘草提取物、生育酚和生育酚衍生物、马铃薯提取物、甲氧基肉桂酸辛酯、二氧化钛、一种或更多糖蛋白、α-葡聚寡糖、甘草酸二钾、尿囊素、燕麦籽提取物、桑树提取物、及其混合物组成的组;其中所述生育酚衍生物选自由维生素E磷酸钠、月桂基亚氨基二丙酸生育酚磷酸酯、生育酚葡糖苷、生育酚琥珀酸酯、托可索仑、月桂基亚氨基二丙酸生育酚磷酸二钠、Tocophereth-5,10,12,18,和50构成的组。
19.如权利要求14-16之一所述的用途,其中所述功能性成分穿透增强剂包括的成分选自乙氧基二甘醇、PPG-12/SMDI共聚物、及其混合物组成的组。
20.如权利要求1-4之一所述的组合物,其中所述马铃薯提取物包括水解马铃薯蛋白。
21.如权利要求14-16之一所述的用途,其中所述马铃薯提取物包括水解马铃薯蛋白。
Applications Claiming Priority (3)
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US10/769,556 | 2004-01-30 | ||
US10/769,556 US7429391B2 (en) | 2004-01-30 | 2004-01-30 | Holistic composition and method for reducing skin pigmentation |
PCT/US2005/000481 WO2005074880A1 (en) | 2004-01-30 | 2005-01-07 | Holistic composition and method for reducing skin pigmentation |
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CN1913866B true CN1913866B (zh) | 2013-03-13 |
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US (1) | US7429391B2 (zh) |
JP (1) | JP2007519722A (zh) |
KR (1) | KR20060130631A (zh) |
CN (1) | CN1913866B (zh) |
HK (1) | HK1100896A1 (zh) |
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WO (1) | WO2005074880A1 (zh) |
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- 2005-01-07 JP JP2006551115A patent/JP2007519722A/ja active Pending
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Also Published As
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US20050169860A1 (en) | 2005-08-04 |
JP2007519722A (ja) | 2007-07-19 |
TWI361084B (en) | 2012-04-01 |
CN1913866A (zh) | 2007-02-14 |
TW200526263A (en) | 2005-08-16 |
KR20060130631A (ko) | 2006-12-19 |
US7429391B2 (en) | 2008-09-30 |
WO2005074880A1 (en) | 2005-08-18 |
HK1100896A1 (en) | 2007-10-05 |
WO2005074880B1 (en) | 2005-12-08 |
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