CN101524315A - 3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮对抗色素沉着过度的应用 - Google Patents
3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮对抗色素沉着过度的应用 Download PDFInfo
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- CN101524315A CN101524315A CN200910134694A CN200910134694A CN101524315A CN 101524315 A CN101524315 A CN 101524315A CN 200910134694 A CN200910134694 A CN 200910134694A CN 200910134694 A CN200910134694 A CN 200910134694A CN 101524315 A CN101524315 A CN 101524315A
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Abstract
在美容用或皮肤病用制剂中应用3－(4－羟基－3－甲氧基苯基)－1－(4－羟基苯基)－丙烷－1－酮，用以治疗和预防发炎后的皮肤状况。3－(4－羟基－3－甲氧基苯基)－1－(4－羟基苯基)－丙烷－1－酮对抗色素沉着过度的应用。
Description
技术领域
本发明涉及美容用或皮肤病用的制剂，该制剂包含用于护理和保护皮肤的有效物质，所述皮肤尤其是指敏感性皮肤以及尤为突出的是指由于内部因素/外部因素引起的已经老化的或正在老化的皮肤，以及本发明还涉及这些有效物质和这些有效物质的组合在美容和皮肤病领域的应用。
背景技术
美容性皮肤护理首先理解为：增强或者修复皮肤的作为屏障的天然功能，所述屏障用于对抗环境的影响(例如：污物、化学品、微生物)以及用于防止身体自有物质的损耗(例如水、天然脂类、电解质)。
当这些功能被扰乱，则会导致对有毒物质或引起过敏的物质的更强烈地吸收，或者是受到微生物感染，结果导致中毒的皮肤反应或过敏的皮肤反应。
皮肤护理的目标还在于，对皮肤的由于每天的清洗而造成的脂类和水的损耗进行补偿。这在天然的再生能力不足时是尤为重要。另外，护肤品应该对外界环境的影响起防护作用，尤其是对阳光和风起防护作用，并且延迟皮肤老化。
皮肤的色素沉着归因于黑素细胞，这些黑素细胞作为-根据皮肤类型的不同，要么以分散的形式，要么或多或少聚积地出现的-形成色素的细胞存在于在表皮的最底层，也就是与底层细胞相邻的基底层组织内。
黑素细胞含有作为独特的细胞器的黑色素体，黑色素在黑色素体中形成。首要地在紫外线辐射的刺激下而使黑色素加强地形成。这些黑色素通过表皮的活化层(Keratinozyten(角质形成细胞))最后输送到角质层(Corneozyten(角层细胞))中，并引起了或多或少明显的、褐色至褐黑色的皮肤颜色。
黑色素作为氧化过程的最后阶段而形成，在该氧化过程中，酪氨酸在酶-酪氨酸酶的共同作用下，经过多个中间阶段转化为褐色或褐黑色的真黑色素(5，6-二羟基吲哚羧酸(DHICA)黑色素和5，6-二羟基吲哚(DHI)黑色素)或者在含硫化合物的参与下转化为略带红色的褐黑素
DHICA黑色素和DHI黑色素经过共同的中间阶段形成多巴醌(Dopachinon)和多巴色素(Dopachrom)，多巴色素在其它酶的参与下，部分地转化为吲哚-5，6-醌-羧酸，或者转化为吲哚-5，6-醌，由此形成所述的两种真黑色素。
褐黑素的形成首要地通过中间产物多巴醌和半胱氨酰基多巴(Cysteinyldopa)来进行的。用于合成黑色素的酶的表达是通过一种特异性转录因子(小眼相关转录因子，MITF)来控制。除了所介绍的黑色素-合成的酶过程外，在黑色素体中，还有其它蛋白质对于黑素原生成是很重要的。在这里，所谓的p-蛋白质显示出重要的作用，其中，确切的功能还不清楚。
除了之前所介绍的黑素细胞中黑色素-合成的过程外，在皮肤色素沉着时，黑色素体的迁移、黑色素体在表皮中的存留以及黑色素体的分解和黑色素的分解也起着决定性作用。可能显示出的是，对于黑色素体从黑素细胞到角质形成细胞中的输送过程，PAR-2-受体(蛋白酶激活受体-2)是重要的(M.Seiberg et al.，2000，J.Cell.Sci.，113：3093-101)。
另外，黑色素体的大小和形状会对黑色素体的光散射特性产生影响进而对肤色外观产生影响。于是，对于非洲黑色人种，发现了加强地大的球形的、单个存在的黑色素体，对于高加索人，则发现较小的、以组的形式存在的黑色素体。
对于皮肤色素沉着过度的问题具有各式各样的原因，或者说是许多生物过程的伴随现象，例如：紫外线辐射(例如雀斑、黄褐斑)、遗传特质、伤口愈合或伤口结疤时皮肤的不合适的色素沉着(发炎后的色素沉着过度)或者皮肤老化(例如：老年斑)。
经过炎性反应后，皮肤的色素沉着系统产生部分排异的反应。这不但可以导致发炎后的色素沉着过度，而且可以引起色素沉着不足。发炎后的黑色素体不足首要地通常与特异性皮炎、红斑狼疮和银屑病相联系地出现。由于发炎现象而引起的、人类皮肤色素沉着系统的不同的反应方式还只是被非常不完全地理解。
发炎后的色素沉着过度的问题通常发生在深色皮肤类型中。尤其对于男性的有色人种，胡须假毛囊炎的问题已为人所知，该问题与美容后不希望的不合适的色素沉着同时出现，或者说不合适的色素沉着紧接着胡须假毛囊炎出现。那些尤其是对于亚裔妇女在脸上和领口暴露部位出现的黄褐斑(Melasma)的形式以及皮肤的非规律性的色素沉着的各种形式都属于发炎后的色素沉着过度。另外，黑眼圈也被认为是发炎后的色素沉着过度，其中，所基于的炎症大多在亚临床期间就终止了。
在多数情况下，这种发炎后的不合适的色素沉着由于太阳光(紫外光)的作用还会加重，即使并未发生紫外线诱发的炎症(太阳灼伤)。
已经公知一些用于抵御皮肤色素沉着的有效物质和制剂。在实际使用中，主要是基于氢醌的试剂，但是所述试剂一方面在使用数周后才显现其作用，另一方面，该试剂过度的、长期的使用由于毒理学上的原因也是令人担忧的。由Albert Kligman等人研发了所谓的Triformula，该物质是由0.1％的维甲酸、5.0％的氢醌、0.1％的地塞米松组成的组合物(A.Kligman，1975，Arch.Dermatol.，111：40-48)。但是，由于在皮肤色素沉着系统中可能的不可逆转的改变，该方案也很受争议。
此外，还使用皮肤脱皮的方法(化学的和机械的“脱皮法”)，但该方法接下来常常引发一些炎性反应，并且由于接下来出现的发炎后的色素沉着过度，而不仅没有避免色素沉着，甚至可能导致更强烈的色素沉着。所有这些即便对于治疗发炎后的色素沉着过度能用的方法都表现出决定性的副作用。
下面的发明的目标在于，设法对具有缺点的现有技术进行补救。
因此，尤其在至今还没有完全理解的皮肤色素沉着系统的反应的背景下，我们极为惊奇地发现，将3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮用于美容用或皮肤病用的制剂中，用以治疗和预防色素沉着过度，尤其是治疗和预防作为发炎后的皮肤状态的色素沉着过度，是有着极其卓越的功效的，因而有助于皮肤均匀的色素沉着。
在一种特别优选的应用方式中，3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮适合于治疗以下色素沉着过度状况：即，尤其是与剃须相关的、炎性反应后的发炎后色素沉着过度、黄褐斑(Melasma)、特别是由于过度的阳光辐射而形成的不均衡的皮肤色调。在此表明，在特别优选的应用方式中，3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮与紫外线过滤剂结合使用。除了通过作为特别优选的实施方式的根据本发明的制剂来预防和治疗发炎后的色素沉着过度之外，一种优选的实施方式表明，根据本发明的制剂即使对于治疗色素沉着不足也是有效的。
由于胡须假毛囊炎导致的发炎后的色素沉着过度以及黄褐斑被视为特别优选的适应症领域。
发明内容
因此，本发明的任务在于，找到一条途径来避免现有技术的缺点。尤其是对那些与由于内因、年龄和外因而引起的皮肤老化相关的损害进行消除的作用和预防应该是持续的、耐久的，并且无副作用的危险。
尤其是根据本发明的应用是有利的，其特征在于，该制剂含有占该制剂的总重量0.0001至5重量％，尤其是0.001至1重量％，更特别是0.005至0.15重量％的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮。
优选地，根据本发明的美容用或皮肤病用的制剂含有占该制剂的总重量0.001至30重量％，优选0.1至15重量％，特别优选0.5至5重量％的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮。
3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮
的制备方法可以有利地由以下列步骤组成或者说包括下列步骤：
a)对-羟基苯乙酮与香草醛反应生成3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-2-丙烯-1-酮，和
将步骤a)中获得的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-2-丙烯-1-酮氢化生成3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯苯)-丙烷-1-酮。
在对于式1的化合物的根据本发明的制备方法的优选方案中，对-羟基苯乙酮与香草醛的反应在步骤a)中这样进行：在升高的温度下，将对-羟基苯乙酮与香草醛加入到氢氧化钾与二甘醇二乙醚的混合物中。温度通常在50℃至200℃的范围内，优选为在80℃至140℃的范围内，进一步优选为在100℃至120℃之间的范围内。
紧接着，所形成的化合物优选水解生成3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-2-丙烯-1-酮。pH值优选在6至7的范围内进行调整。
在对于式1的化合物的根据本发明的制备方法的优选方案中，在步骤(a)中所获得的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-2-丙烯-1-酮是这样被实施氢化生成3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮的：将所形成的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-2-丙烯-1-酮溶于四氢呋喃中，并混入适量的活性炭负载的Pd(Pd含量：5重量％，水含量约50％，分别为占催化剂的总重量而言)。该反应优选在常压下进行，进一步优选在室温(约20℃)下进行。
3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-1-丙酮的合成示例
(a)对-羟基苯乙酮与香草醛的反应：
首先将20g氢氧化钾溶入100g二甘醇二乙醚中，在搅拌下加热至120℃，在1小时内掺入14g对-羟基苯乙酮与15g香草醛的混合物。配料结束后，再继续搅拌20分钟，水解，并将pH值调整至6-7。在相分离后，去除溶剂，获得25g的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-2-丙烯-1-酮，产率：理论上为93％。
(b)对在步骤(a)中获得的反应产物的氢化
将10g的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-2-丙烯-1-酮溶于100g四氢呋喃中，掺入0.2g的、由活性炭负载的Pd(Pd含量：5重量％，水含量约50重量％，分别为占催化剂总重量而言)，并在常压和室温(约20℃)下进行氢化。在除去催化剂和溶剂后，得到9g的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮，产率：理论上为89％。
3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮(式1)的光谱数据：
13C-NMR(CDC13；75.5MHz)：δ(ppm)＝197.42(s)，161.85(s)，147.24(s)，144.44(s)，132.03(s)，130.37(d)，130.37(d)，128.18(s)，120.27(d)，115.11(d)，115.07(d)，115.07(d)，112.53(d)，55.42(q)，39.30(t)，29.42(t)；
MS：m/z(％)＝M+-Ion 272(82)，151(24)，137(77)，121(100)，93(19)，65(22)。
根据本发明地，所述美容用或皮肤病用的制剂可以象通常那样进行组合，并用于对皮肤和/或毛发进行治疗、护理和清洁，还可以在修饰性美容中用作化妆产品。
所述美容用或皮肤病用的制剂含有占制剂的总重量优选为0.001重量％至10％重量％，优选为0.05重量％至5％重量％，尤其是0.1-2.0重量％的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮。
根据本发明的美容用和皮肤病的制剂可以以多种形式存在。例如该制剂可以是溶液、无水制剂、一种油包水型(W/O)或水包油型(O/W)的乳液或微乳液、多重乳液(例如水-油-水型(W/O/W))、凝胶、固态的笔型剂、软膏、或者也可以是气溶胶。
根据本发明同样有利的是，3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮可以以胶囊的形式给出，例如采用骨胶原基质和其它通用的胶囊材料(例如，作为纤维素胶囊)，用明胶，蜡模或脂质体制成胶囊。特别是如在DE-OS 4308282中描述的蜡模被证实是有利的。
在本发明意义上，将3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮加入水性体系或者表面活性剂制剂中以用于皮肤和毛发的清洁是可行的并且是有利的。
根据本发明的美容用和皮肤病用的制剂可以含有美容用的助剂，如它们通常用于这样的制剂中一样，例如：防腐剂、杀菌剂、香料、消泡剂、具有染色作用的颜料和染料、增稠剂、表面活性剂、乳化剂、软化物质、润湿物质和/或保湿物质、脂类、油类、蜡或其它在美容用或皮肤病用配方中的常用的组分，诸如醇类、多元醇、聚合物、凝胶形成体、稳泡剂、电解质、有机溶剂或者硅的衍生物。
用于这类制剂的有利的凝胶形成体例如是由C10-30烷基丙烯酸酯和丙烯酸的、甲基丙烯酸的或丙烯酸的酯的、甲基丙烯酸的酯的一种或多种单体形成的共聚物。这类化合物的国际专业命名化妆品原料(INCI)名称为“丙烯酸酯/C10-30烷基丙烯酸酯交联共聚物”。特别有利的是Fa.Goodrich(Noveon)公司的TR1、TR2和TRZ型号的
卡伯波(Carbopol)是对于这类制剂来说有利的凝胶形成体。卡伯波是丙烯酸的聚合物，尤其也是丙烯酸酯-烷基丙烯酸酯-共聚物。有利的卡伯波例如为型号980、981、984、1342、1382、2984和5984，同样也可以是ETD-型号2001、2020、2050以及卡伯波Ultrez 10、PVM/MA癸二烯交联聚合物(商品名称
06)、聚甲基丙烯酸甘油酯以及聚丙烯酰胺、二甲基牛磺酰胺铵盐/乙烯基甲酰胺共聚物、如下的共聚物或交联共聚物，所述共聚物或交联聚合物包括丙烯酰二甲基牛磺酸酯、聚丙烯酰二甲基牛磺酰胺、聚乙烯基吡咯烷酮及它们的共聚物。
用于这类制剂的其它有利的凝胶形成体是黄原胶、聚乙烯基吡咯烷酮、纤维素衍生物(尤其是纤维素醚，例如羟丙基甲基纤维素)、淀粉和淀粉衍生物、透明质酸、卡拉胶、二氧化硅和硅酸铝。
优选的水包油乳化剂是甘油硬脂酸酯柠檬酸酯、聚甘油基-3-甲基葡萄糖二硬脂酸酯、鲸蜡硬脂基葡糖苷、PEG-40-硬脂酸酯、PEG-100-硬脂酸酯、硬脂酸、鲸蜡硬脂醇醚-20、硬脂醇聚醚-20、硬脂醇聚醚-2、硬脂醇聚醚-21和硬脂酸甘油酯。
在制剂中抗氧化剂(一种或多种化合物)的数量优选为占制剂的总重量0.001至30重量％，特别优选为0.05-20重量％，尤其是1-10重量％。
抗氧化剂有利地选自如下的组：类胡萝卜素(例如β-胡萝卜素，菌脂色素)及其衍生物、硫辛酸及其衍生物、硫醇(例如硫氧还蛋白、谷胱甘肽、半胱氨酸、胱氨酸、胱胺)及其盐类、其它(金属)螯合剂(例如α-羟基脂肪酸、肌醇六磷酸、乳铁蛋白、乙二胺四乙酸)、不饱和脂肪酸及其衍生物(例如γ-亚麻酸、亚油酸)、叶酸及其衍生物、泛醌和泛醌醇及其衍生物(尤其是泛醌Q10)、维生素C及衍生物(例如抗坏血酸棕榈酸酯、抗坏血酸磷酸钠)、维生素E及衍生物(例如维生素E-乙酸酯)、维生素A及衍生物(维生素A-棕榈酸酯)、芸香苷及其衍生物(α-葡糖基芸香苷)、槲皮素、异黄酮、染料木黄酮、大豆黄酮、阿魏酸、丁基甲基苯酚。
脂质相可以有利地选自以下的物质组：
-矿物油、矿物蜡；
-油类，诸如癸酸的三甘油酯或辛酸的三甘油酯，还有诸如月见草油的天然油类。
-脂类、蜡以及其它天然的和合成的脂类物质，优选为脂肪酸与低碳值的醇类(如与异丙醇，丙二醇或甘油)的酯，或者为脂肪醇与低碳值的链烷酸或与脂肪酸的酯；
-苯甲酸烷基酯；
-硅油，诸如二甲硅油、环甲硅脂、二甲基聚硅氧烷、二乙基聚硅氧烷、二苯基聚硅氧烷以及它们的混合物形式。
本发明意义上的乳液的油相、油液凝胶以及水分散体或脂分散体有利地选自如下的组：由饱和的和/或不饱和的、带支链的和/或不带支链的、链长为3到30个碳原子的链烷羧酸以及饱和的和/或不饱和的、带支链的和/或不带支链的、链长为3到30个碳原子的醇类形成的酯的组；由芳香族的羧酸与饱和的和/或不饱和的、带支链的和/或不带支链的、链长为3到30个碳原子的醇类形成的酯的组。这样的酯油可以有利地选自如下的组：肉豆蔻酸异丙酯、棕榈酸异丙酯、硬脂酸异丙酯、油酸异丙酯、硬脂酸正丁酯、月桂酸正己酯、油酸正癸酯、硬脂酸异辛酯、硬脂酸异壬酯、异壬酸异壬酯、棕榈酸2-乙基己酯、月桂酸2-乙基己酯、硬脂酸2-己基癸酯、棕榈酸2-辛基十二烷酯、油酸油醇酯、芥酸油醇酯、油酸瓢儿菜醇酯、瓢儿菜酸瓢儿菜醇酯以及这些酯类的合成的、半合成的和天然的混合物，例如：荷荷巴油。
根据本发明的制剂的水性相在需要时有利地含有：醇类、二醇类或低碳值的多元醇以及它们的醚，优选为乙醇、异丙醇、丙二醇、丁二醇、甘油、泛醇、乙二醇、己二醇、辛二醇、乙二醇单乙醚或乙二醇单丁醚、丙二醇单甲醚、丙二醇单乙醚或丙二醇单丁醚、二甘醇单甲醚或二甘醇单乙醚以及类似的产物。
尤其是使用上述溶剂的混合物。对于醇类溶剂而言，水可以是另一种组分。
根据本发明的乳液是有利的，并例如包含所述的脂类、油、蜡和其它脂类物质、以及水和比如通常用于这种类型配方的乳化剂。
依据本发明的凝胶通常含有低碳值的醇类，例如乙醇、异丙醇、1，2-丙二醇、甘油和水或在增稠剂存在下的上述的油类，所述增稠剂对于油性-醇类凝胶优选为二氧化硅或硅酸铝，而对于水性-醇类凝胶或醇类凝胶优选为聚丙烯酸酯。
通常已知的易于挥发的液化的推进剂，例如烃类(丙烷、丁烷、异丁烷)都是适合作为能从气溶胶容器中喷出的根据本发明制剂的推进剂，它们可以单独地或彼此以混合物的形式使用。同样，有利地使用压缩空气。
此外，根据本发明的制剂可以有利地含有吸收UVB区域内紫外辐射的物质，其中，过滤物质的总量为占制剂的总重量：例如0.1重量％至30重量％，优选0.5至10重量％，特别是1.0至6.0重量％，以便提供美容用制剂，所述制剂在整个紫外辐射范围来保护毛发和皮肤。所述制剂也可以用作毛发或皮肤的防晒剂。
具体实施方式
以下示例对本发明进行阐释，而非对本发明进行限制。所有的数量说明、份额和百分数份额，在没有另外说明的情况下，都是占制剂的重量和总量或者占制剂总重量的重量百分数。
pH 5
| 护理霜 | 重量％ |
| 硬脂酸甘油酯，进行自乳化 | 5 |
| 硬脂醇 | 3 |
| 硬酯酸 | 1 |
| 葡萄籽油 | 1 |
| 二甲基硅氧烷醇 | 0.5 |
| 环甲硅脂 | 4 |
| 辛基十二烷醇 | 3 |
| 氢化的椰油甘油酯 | 2 |
| 维生素H | 0.05 |
| 3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮 | 0.2 |
| 淀粉辛烯基琥珀酸钠盐 | 1 |
| 卡波姆 | 0.2 |
| 泛醇 | 0.5 |
| 甘油 | 9 |
| 乙二胺四乙酸 | 0.1 |
| 香料 | 0.3 |
| 维生素E乙酸酯 | 0.5 |
| 辅酶Q10 | 0.1 |
| 甲基丙二醇 | 1 |
| 氢氧化钠溶液 | 适量 |
| 水 | 补足至100 |
pH：7
| 对抗老年斑的润肤霜 | 重量％ |
| 聚甘油-3甲基葡萄糖二硬脂酸酯 | 2 |
| 失水山梨醇硬脂酸酯 | 2 |
| 硬脂醇 | 2 |
| 二甲基硅酮 | 2 |
| C12-15烷醇苯甲酸酯 | 2 |
| 辛酸三酸甘油酯/癸酸三酸甘油酯 | 3 |
| 环甲硅脂 | 4 |
| 乙基己基三嗪酮 | 1 |
| 2，2’-亚甲基-双-(6-(2H-苯并三唑-2-基)-4-(1，1，3，3-四甲基丁基)-苯酚) | 2 |
| 乙基己基-2-氰基-3，3-二苯基丙烯酸酯(Octocrylene) | 3 |
| 3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮 | 0.5 |
| 卡拉胶 | 0.1 |
| 交联的烷基丙烯酸酯(烷基丙烯酸酯交联聚合物) | 0.1 |
| 鞣花酸 | 0.2 |
| 烟酰胺 | 0.5 |
| 甘油 | 8 |
| 乙基己基甘油 | 0.4 |
| 乙二胺四乙酸 | 0.1 |
| 尼泊金乙酯 | 0.2 |
| 苯氧乙醇 | 0.4 |
| 添加剂(尼龙，淀粉磷酸酯) | 2 |
| 柠檬酸，钠盐 | 适量 |
| 水 | 补足至100 |
pH：6
| 防晒霜 | 重量％ |
| 硬脂酸甘油酯 | 3 |
| PEG-40-硬酯酸酯 | 1 |
| 十六烷醇 | 2 |
| C12-15烷醇苯甲酸酯 | 2 |
| 二辛基醚 | 2 |
| 辛基十二烷醇 | 2 |
| 环甲硅脂 | 2 |
| 肉豆蔻酸肉豆蔻酯 | 1 |
| 二氧化钛 | 1 |
| 乙基己基甲氧基肉桂酸酯 | 6 |
| 苯基苯并咪唑磺酸 | 1 |
| 茴香三嗪(2，4-双-{[4-(2-乙基-己氧基)-2-羟基]-苯基}-6-(4-甲氧基苯基)-1，3，5-三嗪) | 2 |
| 3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮 | 0.2 |
| 卡拉胶 | 0.2 |
| 卡波姆 | 0.2 |
| 甘油 | 7 |
| 丁二醇 | 3 |
| 乙二胺四乙酸 | 0.2 |
| 防腐剂 | 适量 |
| 香料 | 适量 |
| 氢氧化钠溶液 | 适量 |
| 水 | 补足至100 |
pH：7
| 须后香脂 | 重量％ |
| 三鲸蜡硬脂醇聚醚-4磷酸酯 | 1 |
| 环甲硅脂 | 3 |
| C12-15烷醇苯甲酸酯 | 2 |
| 二淀粉磷酸酯 | 1 |
| 卡波姆 | 0.2 |
| 黄原胶 | 0.1 |
| 尼泊金甲酯 | 0.2 |
| 苯氧乙醇 | 0.4 |
| 3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮 | 0.4 |
| 甘油 | 6 |
| 乙二胺四乙酸 | 0.1 |
| 香料 | 0.3 |
| 氢氧化钠溶液 | q.s |
| 水 | 补足至100 |
pH：7
Claims (6)
1.3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮在美容用或皮肤病用制剂中的应用，用于治疗和预防色素沉着过度。
2.根据权利要求1所述的应用，其特征在于，所述制剂含有占制剂的总重量的0.0001至5重量％，尤其是0.001至1重量％，尤其特别是0.005至0.15重量％的3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮。
3.3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮用于减少色素干扰的应用，所述色素干扰由于先前的炎症而产生。
4.3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮用于减少色素干扰的应用，所述色素干扰由于先前的紫外线暴露而产生。
5.根据前述权利要求之一所述的应用，其特征在于，局部地涂敷所述组合物，以治疗选自下面的组的皮肤状况，所述组由雀斑、深色斑、变色、黄褐斑、色素沉着过度、炎症后的色素沉着过度以及这些状况的各种组合组成。
6.根据前述权利要求之一所述的应用，其特征在于，3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮在美容用或皮肤病用制剂中的浓度选择为0.01至10重量％。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102008009799.3A DE102008009799B4 (de) | 2008-02-18 | 2008-02-18 | Verwendung von 3-(4-Hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-propan-1-on gegen Hyperpigmentierung |
| DE102008009799.3 | 2008-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101524315A true CN101524315A (zh) | 2009-09-09 |
Family
ID=40874094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200910134694A Pending CN101524315A (zh) | 2008-02-18 | 2009-02-17 | 3-(4-羟基-3-甲氧基苯基)-1-(4-羟基苯基)-丙烷-1-酮对抗色素沉着过度的应用 |
Country Status (3)
| Country | Link |
|---|---|
| CN (1) | CN101524315A (zh) |
| DE (1) | DE102008009799B4 (zh) |
| WO (1) | WO2009103427A2 (zh) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2974300B1 (fr) * | 2011-04-19 | 2013-05-10 | Inneov Lab | Utilisation d'une combinaison d'un carotenoide, d'un phytoestrogene et de la vitamine c pour la prevention et/ou le traitement de desordres pigmentaires |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4308282C2 (de) | 1993-03-16 | 1994-12-22 | Beiersdorf Ag | Vorzugsweise in Form von Mikrosphärulen vorliegende galenische Matrices |
| JP3636423B2 (ja) * | 1997-12-16 | 2005-04-06 | 三井化学株式会社 | ハイドロカルコン誘導体を有効成分とする化粧料 |
| EP1818060A1 (en) * | 2005-11-23 | 2007-08-15 | ARTSANA S.p.A. | Cosmetic composition comprising Fadogia ancylantha extracts |
| EP1977655B1 (de) * | 2007-03-29 | 2011-05-18 | Symrise AG | Aromakompositionen von Alkamiden mit Hesperetin und/oder 4-Hydroxydihydrochalkonen und deren Salzen zur Verstärkung süßer sensorischer Eindrücke |
| EP2173697A1 (en) * | 2007-07-25 | 2010-04-14 | Symrise GmbH & Co. KG | 3-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-1-propanone and its use as antioxidant |
-
2008
- 2008-02-18 DE DE102008009799.3A patent/DE102008009799B4/de not_active Expired - Fee Related
-
2009
- 2009-02-05 WO PCT/EP2009/000785 patent/WO2009103427A2/de active Application Filing
- 2009-02-17 CN CN200910134694A patent/CN101524315A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009103427A2 (de) | 2009-08-27 |
| WO2009103427A3 (de) | 2009-11-19 |
| DE102008009799A1 (de) | 2009-08-20 |
| DE102008009799B4 (de) | 2017-07-20 |
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