CN108366952A - 用于亮肤的包含烟酰胺和α-熊果苷的组合物 - Google Patents
用于亮肤的包含烟酰胺和α-熊果苷的组合物 Download PDFInfo
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- CN108366952A CN108366952A CN201680072501.8A CN201680072501A CN108366952A CN 108366952 A CN108366952 A CN 108366952A CN 201680072501 A CN201680072501 A CN 201680072501A CN 108366952 A CN108366952 A CN 108366952A
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- Prior art keywords
- arbutin
- skin
- alpha
- range
- niacinamide
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Abstract
本发明涉及包含烟酰胺和α‑熊果苷的新颖组合物,并涉及所述组合物用于亮肤的用途。更具体地,本发明涉及烟酰胺用于协同增强α‑熊果苷的亮肤活性的用途。
Description
本发明涉及包含烟酰胺和α-熊果苷的新颖组合物,并涉及所述组合物用于亮肤的用途。更具体地,本发明涉及烟酰胺用于协同增强α-熊果苷的亮肤活性的用途。
对稳定、安全和具有成本效益的亮肤产品一直存在不断增长的行业需要和不断增长的市场需求。
合成的亮肤剂(例如氢醌或曲酸)被认为是非常有效的亮肤成分,然而,其可能导致皮肤刺激或急性皮炎,因此不再受到美容行业的高度青睐。
α-熊果苷(4-羟基苯基α-吡喃葡萄糖苷;CAS:84380-01-8)目前被用作氢醌和曲酸的更安全替代物,但需要以高达2重量%的浓度应用以展示出可感知的提亮功效。然而,这种剂量方案导致显著的市场限制,因为α-熊果苷在使用成本方面不是很有吸引力。
据称,烟酰胺(CAS 98-92-0)是一种令人惊叹的成分,其能够减少细纹和皱纹、色素沉着过度的斑点、红斑、皮肤灰黄(发黄)和炎症,并增强角质层的弹性、水合作用和屏障功能。然而,其亮肤功效非常有限,并且如果有的话,也只有在相当高的浓度水平下才可以感知。
因此,一直需要克服现有技术缺点的经改进的亮肤产品。
出乎意料地,已发现烟酰胺能够协同增强α-熊果苷的亮肤功效,从而导致比得上曲酸的功效。这一发现现在允许配制高效、具有成本效益的亮肤组合物,因为只需使用少量的α-熊果苷。
本文中提到的术语“亮肤”是指减轻肤色不均、提亮/增亮皮肤、防止晒黑并/或防止再次色素沉着、防晒或防止UV诱导的皮肤变暗以及降低人类皮肤的黑色素水平。
本发明的第一个目标涉及包含烟酸酰胺和α-熊果苷的局部用组合物,其特征在于,基于所述局部用组合物的总重量,α-熊果甙的量选自0.05-0.5重量%的范围,烟酰胺与α-熊果苷的重量比选自50至5的范围。
在一个优选的实施方式中,基于局部用组合物的总重量,α-熊果甙的量选自0.075-0.3重量%的范围内,更优选0.1-0.25重量%的范围内,并且烟酰胺与α-熊果苷之比选自30至5的范围内,更优选25至5的范围内,最优选20至5的范围内,例如有利地15至6的范围内,更有利地12至8的范围内。
因此,在一个特别有利的实施方式中,α-熊果苷的量选自0.1-0.3重量%的范围内,烟酰胺与α-熊果苷的重量比选自15至6的范围内。在一个甚至更有利的实施方式中,α-熊果苷的量选自0.15-0.25重量%的范围内,并且烟酰胺与α-熊果苷的重量比选自12至8的范围内。
本文中使用的术语“局部用”应被理解为是指外用到角质物质,特别是皮肤、头皮、睫毛、眉毛、指甲、粘膜和毛发。
优选地,局部用组合物是美容组合物或药物组合物。最优选地,其是美容组合物。
由于根据本发明的组合物旨在用于局部应用,因此其包含生理学上可接受的介质,即与角质物质(例如皮肤、粘膜和角质纤维)相容的介质。特别地,生理学上可接受的介质是美容上可接受的载体。
术语“美容上可接受的载体”是指美容组合物中常规使用的所有载体和/或赋形剂和/或稀释剂。
根据本发明的优选美容组合物是皮肤护理制剂。
皮肤护理制剂的实例有,特别是,亮肤制剂、用于处理光老化的制剂、光保护制剂(遮光剂)、抗老化制剂、处理霜(treatment creams)以及BB霜和CC霜。
在一个具体的实施方式中,根据本发明的局部用组合物是皮肤护理制剂,例如乳、洗剂、水分散体、粉底、霜、凝胶霜、精华、柔肤水、面膜或凝胶。
根据本发明的局部用组合物可以是在溶剂或脂肪物质中的悬浮物或分散体的形式,或者其形式可以是乳剂或微乳剂(特别是水包油(O/W)或油包水(W/O)型,水包硅酮(Si/W)或硅酮包水(W/Si)型,PIT-乳剂,多重乳剂(例如油包水包油(O/W/O)或水包油包水(W/O/W)型),皮克林乳剂(pickering emulsion),水凝胶,醇凝胶,脂质凝胶,单相溶液或多相溶液或泡状分散体或其它常用形式,还可以通过笔、作为面膜或喷雾来应用。
在一个实施方式中,根据本发明的局部用组合物有利地为水包油(O/W)乳剂的形式,其包含在O/W乳化剂的存在下分散在水相中的油相。这种O/W乳剂的制备是本领域技术人员公知的。
如果根据本发明的局部用组合物是O/W乳剂,那么其有利地含有至少一种的O/W-乳化剂或Si/W-乳化剂,所述O/W-乳化剂或Si/W-乳化剂选自PEG-30二聚羟基硬脂酸酯、PEG-4二月桂酸酯、PEG-8二油酸酯、PEG-40失水山梨醇全油酸酯、PEG-7椰油酸甘油酯、PEG-20杏仁甘油酯、PEG-25氢化蓖麻油、硬脂酸甘油酯(和)PEG-100硬脂酸酯、PEG-7橄榄油酸酯、PEG-8油酸酯、PEG-8月桂酸酯、PEG-60杏仁甘油酯、PEG-20甲基葡糖倍半硬脂酸酯、PEG-40硬脂酸酯、PEG-100硬脂酸酯、PEG-80失水山梨醇月桂酸酯、硬脂醇聚醚-2、硬脂醇聚醚-12、油醇聚醚-2、鲸蜡醇聚醚-2、月桂醇聚醚-4、油醇聚醚-10、油醇聚醚-10/聚氧乙烯10油醇醚、鲸蜡醇聚醚-10、异硬脂醇聚醚-20、鲸蜡硬脂醇聚醚-20、油醇聚醚-20、硬脂醇聚醚-20、硬脂醇聚醚-21、鲸蜡醇聚醚-20、异鲸蜡醇聚醚-20、月桂醇聚醚-23、硬脂醇聚醚-100、硬脂酸柠檬酸甘油酯、硬脂酸甘油酯SE(自乳化)、硬脂酸、硬脂酸的盐、聚甘油基-3-甲基葡萄糖二硬脂酸酯。其他合适的乳化剂为磷酸酯及其盐,如鲸蜡醇磷酸酯(A)、二乙醇胺鲸蜡醇磷酸酯(DEA)、鲸蜡醇磷酸酯钾(K)、鲸蜡硬脂醇硫酸酯钠、甘油油酸酯磷酸酯钠、氢化植物油甘油酯类磷酸酯及其混合物。其他合适的乳化剂为失水山梨醇油酸酯、失水山梨醇倍半油酸酯、失水山梨醇异硬脂酸酯、失水山梨醇三油酸酯、鲸蜡硬脂基葡糖苷、月桂基葡糖苷、癸基葡糖苷、硬脂酰谷氨酸钠、蔗糖多硬脂酸酯和水合聚异丁烯。此外,一种或多种合成聚合物可被用作乳化剂。例如,PVP二十碳烯共聚物、丙烯酸酯/C10-30烷基丙烯酸酯交联聚合物、丙烯酸酯/硬脂醇聚醚-20甲基丙烯酸酯共聚物、PEG-22/十二烷基甘醇共聚物、PEG-45/十二烷基甘醇共聚物及其混合物。
待用于根据本发明的局部用组合物中的一种特别合适的O/W乳化剂为鲸蜡醇磷酸酯钾,例如,可在DSM Nutritional Products Ltd Kaiseraugst以商品名K商购获得。
基于所述组合物的总重量,至少一种O/W乳化剂和Si/W乳化剂的用量优选分别为0.5-10重量%,特别是0.5-6重量%,例如更特别是0.5-5重量%,例如最特别是1-4重量%。
其他的合适的O/W乳化剂为聚乙二醇(PEG)酯或二酯,如[INCI名]PEG-100硬脂酸酯、PEG-30二聚羟基硬脂酸酯、PEG-4二月桂酸酯、PEG-8二油酸酯、PEG-40失水山梨醇全油酸酯、PEG-7椰油酸甘油酯、PEG-20杏仁甘油酯、PEG-25氢化蓖麻油、PEG-7橄榄油酸酯、PEG-8油酸酯、PEG-8月桂酸酯、PEG-60杏仁甘油酯、PEG-20甲基葡糖倍半硬脂酸酯、PEG-40硬脂酸酯、PEG-100硬脂酸酯、PEG-80失水山梨醇月桂酸酯。
根据本发明特别优选的是由Croda以商品名ArlacelTM 165(INCI硬脂酸甘油酯(和)PEG-100硬脂酸酯)出售的PEG-100硬脂酸酯。
另一类特别合适的O/W乳化剂是从橄榄油衍生的非离子型自乳化体系,例如以商品名OLIVEM 1000出售的(INCI名)鲸蜡硬脂醇橄榄油酸酯和失水山梨醇橄榄油酸酯(化学组成:橄榄油脂肪酸的失水山梨醇酯和鲸蜡硬脂酯)。
在一个具体的实施方式中,本发明涉及具有本文给出的所有限定和优选的O/W乳剂形式的局部用组合物,其包含在O/W乳化剂的存在下分散在水相中的油相,其中所述O/W乳化剂是鲸蜡醇磷酸酯钾。
根据本发明的美容组合物可以通过本领域中的常规方法来制备,例如,通过将根据本发明的处于各自的量和比的烟酰胺和α-熊果苷与美容上可接受的载体混合来制备。
本发明的美容组合物(包括载体)可以包含其它常规的美容佐剂和添加剂,例如防腐剂/抗氧化剂(例如焦亚硫酸钠),脂肪物质/油,水,有机溶剂,硅酮,增稠剂,软化剂,乳化剂,消泡剂,美学组分例如香料,表面活性剂,填充剂,阴离子聚合物、阳离子聚合物、非离子聚合物或两性聚合物或其混合物,推进剂,酸化剂或碱化剂,染料,着色剂/染色剂,研磨剂,吸收剂,螯合剂(chelating agents)和/或螯合分散剂(sequestering agents),精油,皮肤感觉剂(skin sensates),收敛剂,颜料或通常配制到这种组合物中的任何其他成分。
依照本发明,根据本发明的美容组合物还可以包含美容组合物中常规使用的其它美容活性成分。示例性的活性成分包括UV-过滤剂,用于处理色素沉着过度的试剂;预防或减轻炎症的试剂;紧致剂、保湿剂、舒缓剂和/或活力剂(energizing agent)以及改善弹性和皮肤屏障的试剂。
适用于本发明美容组合物中的皮肤护理行业中常用的美容赋形剂、稀释剂、佐剂、添加剂以及活性成分的实例例如描述于可通过在线INFOBASE(http://online.personalcarecouncil.org/jsp/Home.jsp)访问的个人护理产品委员会的国际化妆品原料字典和手册(International Cosmetic Ingredient Dictionary&Handbook byPersonal Care Product Council;http://www.personalcarecouncil.org/),但不限于此。
基于期望的产品形式和应用,本领域技术人员可以容易地确定活性成分以及美容赋形剂、稀释剂、助剂、添加剂等的必需量。可以视情况将额外的成分加入到油相中,水相中或者分别加入。
本文中可用的美容活性成分在一些情况下能够提供多于一种益处或通过多于一种作用模式发挥作用。
当然,本领域技术人员应小心地选择上述任选的额外的一种或多种化合物和/或其量,使得与根据本发明的组合内在相关的有利性质不受或基本上不受所设想的一种或多种添加的不利影响。
根据本发明的局部用组合物的pH范围通常具有3至10范围内的pH,优选4至8范围内的pH,最优选4至7.5范围内的pH。可以根据需要用合适的酸或碱根据本领域的标准方法容易地调节pH,所述酸例如柠檬酸,所述碱例如氢氧化钠(例如作为水溶液)、三乙醇胺(TEACare)、氨基丁三醇(Trizma Base)和氨甲基丙醇(AMP-Ultra PC 2000)。
待应用到皮肤上的局部用组合物的量不是关键的,且可由本领域的技术人员容易地调节。优选地,所述量选自0.1-3mg/cm2皮肤的范围,例如优选0.1-2mg/cm2皮肤的范围,最优选0.5-2mg/cm2皮肤的范围。
本发明的另一个目标是烟酰胺和α-熊果苷用于亮肤的(美容)用途,例如特别是用于减轻肤色不均、防止晒黑并/或防止再次色素沉着、防晒或防止UV诱导的皮肤变暗以及降低人类皮肤的黑色素水平,其特征在于,烟酰胺与α-熊果苷的重量比选自50至5的范围,优选30至5的范围,更优选25至5的范围,最优选20至5的范围,例如有利地15至6的范围,更有利地12至8的范围。
在另一个实施方式中,本发明还涉及烟酰胺和α-熊果苷在用于处理和预防皮肤色素沉着失调的局部用药物组合物中的用途,其中所有限定和优选均如上文关于局部用组合物所给出。
本发明的另一个目标是烟酰胺用于增强α-熊果苷的亮肤活性的用途,其中优选地烟酰胺与α-熊果苷的重量比选自50至5的范围,优选30至5的范围,更优选25至5的范围,最优选20至5的范围,例如有利地15至6的范围,更有利地12至8的范围。
本发明还涉及提亮人类皮肤的(美容)方法,例如特别是减轻肤色不均、防止晒黑并/或防止再次色素沉着、防晒或防止UV诱导的皮肤变暗以及降低人类皮肤的黑色素水平,所述方法包括:将有效量的根据本发明的组合物局部施用到需要这种处理的人的适当皮肤区域,并任选地评价效果。
此外,本发明还涉及处理或预防色素沉着失调的方法,所述方法包括:将有效量的根据本发明的组合物局部施用到需要这种处理的人的适当皮肤区域,并任选地评价效果。
术语“有效量”是指获得生理效果所必需的量。可以通过一个应用剂量或通过重复应用来实现所述生理效果。当然,所施用的剂量可以因已知的因素而异并能够由本领域技术人员调节,所述因素例如特定组合物的生理学特性及其施用模式和途径;接受者的年龄、健康状况和体重;症状的性质和程度;并存处理的种类;处理频率;和所期望的效果。优选地,待应用到皮肤的局部用组合物的量选自0.1-3mg/cm2皮肤的范围,例如优选0.1-2mg/cm2皮肤的范围,最优选0.5-2mg/cm2皮肤的范围。
本发明还涉及如上所述的方法,其中每平方厘米皮肤每天应用约0.2μg至约200μg的烟酰胺和α-熊果苷(以两种化合物的量的总和计算)。
提供以下实施例以进一步说明本发明的组合物和效果。这些实施例仅仅是说明性的,并不意图以任何方式限制本发明的范围。
实施例:3D表皮模型的方法和结果
细胞培养
在无菌条件下在琼脂糖斑块上接受皮肤等同物。到达后,根据制造商的说明,将其转移到6孔板中,并供应2ml维持培养基在37℃下过夜以进行平衡。为了开始试验,以无毒浓度在上面施加25μL的体积。每隔一天给药一次,同时更换培养基。将皮肤模型保持在6孔培养板的孔中,并在37℃和5%CO2气氛的培养箱中培养9天。
测定细胞毒性
简而言之,将MTT储备溶液(5mg/mL)在PBS中稀释至1mg/mL。向新的24孔板的每个孔中加入300μL工作溶液。然后将组织转移到孔中,并在37℃和5%CO2加湿气氛下孵育板3小时。之后,将800μL 2-丙醇填充到新的24孔板的每个孔中,并将组织从MTT板转移至新板。为了用2-丙醇完全覆盖组织,将700μL 2-丙醇添加到插入物(inserts)中。将板用石蜡膜密封并在室温下孵育2小时,同时在摇动器上温和搅动。然后用枪头(tip)刺穿组织,并通过上下吸取来均化溶液。之后将这种提取溶液以200μL/孔转移到96孔板中,进行三次。使用2-丙醇作为空白。在吸光度读数器中在570nm波长处读取OD。以媒介物(vehicle)对照作为比较,使用仅一个组织插入物将细胞毒性评估为单一值。
利用Fontana-Masson方法检测黑色素
将涂有硅烷的载玻片上的3-5μm厚的石蜡切片脱石蜡并再水化,将所述载玻片与5%氨化硝酸银溶液一起在加湿室中在56℃下孵育30分钟。通过更换几次蒸馏水来充分洗涤。将切片用5%硫代硫酸钠水溶液处理1分钟,随后在流动水中洗涤2-3分钟。将细胞核用苏木精染色5分钟,并再次在流动水中充分洗涤5分钟。在Entellan的存在下,将载玻片脱水并盖上盖玻片。通过使用Olympus的cellSense软件测量每微米组织切片的黑色素面积来量化黑色素含量。
表1:黑色素染色和量化的结果
显著性(t-检验):
“媒介物”相较于“0.4%的α-熊果苷”,p<0.01
“媒介物”相较于“0.2%的α-熊果苷+1.8%的烟酰胺”,p<0.01
“0.4%的α-熊果苷”相较于“0.2%的α-熊果苷+1.8%的烟酰胺”,p<0.05
从表1中所示的数据可以看出:烟酰胺本身不导致皮肤提亮,而比例为9:1的烟酰胺与α-熊果苷的组合导致显著的改善,比得上曲酸的效果。
Claims (13)
1.一种局部用组合物,其特征在于,α-熊果苷的量选自0.1-0.3重量%的范围,且烟酰胺与α-熊果苷的重量比选自15至6的范围。
2.根据权利要求1所述的局部用组合物,其特征在于,α-熊果苷的量选自0.15-0.25重量%的范围,且烟酰胺与α-熊果苷的重量比选自12至8的范围。
3.根据权利要求1至2中任一项所述的局部用组合物,其特征在于,其为美容组合物。
4.根据权利要求3所述的局部用组合物,其特征在于,所述美容组合物是皮肤护理制剂。
5.根据权利要求3或4所述的局部用组合物,其特征在于,所述美容组合物为乳、洗剂、水分散体、粉底、霜、凝胶霜、精华、柔肤水、面膜或凝胶的形式。
6.烟酰胺和α-熊果苷用于亮肤的用途,其特征在于,烟酰胺与α-熊果苷的重量比选自15至6的范围,更有利地12至8的范围。
7.根据权利要求6所述的用途,其用于减轻肤色不均、防止晒黑并/或防止再次色素沉着、防晒或防止UV诱导的皮肤变暗以及降低人类皮肤的黑色素水平。
8.烟酰胺用于增强α-熊果苷的亮肤活性的用途。
9.一种提亮人类皮肤的方法,所述方法包括将有效量的根据权利要求1至5中任一项所述的局部用组合物局部施用到需要这种处理的人的适当皮肤区域。
10.根据权利要求9所述的方法,其用于减轻肤色不均、防止晒黑并/或防止再次色素沉着、防晒或防止UV诱导的皮肤变暗以及降低人类皮肤的黑色素水平。
11.一种处理或预防色素沉着失调的方法,所述方法包括将有效量的根据权利要求1至5中任一项所述的局部用组合物局部施用到需要这种处理的人的适当皮肤区域。
12.权利要求9至11中所述的方法,其中每平方厘米皮肤每天应用约0.2μg至约200μg的烟酰胺和α-熊果苷。
13.烟酰胺和α-熊果苷在用于处理和预防皮肤色素沉着失调的局部用药物组合物中的用途,其特征在于,基于所述局部用组合物的总重量,α-熊果苷的量选自0.1-0.3重量%的范围,且烟酰胺与α-熊果苷的重量比选自15至6的范围。
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