CN105663018B - 化妆品组合物 - Google Patents
化妆品组合物 Download PDFInfo
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- CN105663018B CN105663018B CN201510882539.9A CN201510882539A CN105663018B CN 105663018 B CN105663018 B CN 105663018B CN 201510882539 A CN201510882539 A CN 201510882539A CN 105663018 B CN105663018 B CN 105663018B
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- skin
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- extract
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- exfoliating
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Abstract
本发明涉及化妆品组合物。具体而言,公开了能够用于改善皮肤视觉外观的组合物和方法。在一些方面,本文公开的组合物可以包括例如用于去角质、减少或消除由于去角质引起的刺激、使皮肤更新、增加皮肤光泽、舒缓皮肤、或增加皮肤光滑度的成分的组合。成分的这种组合可以被包含在宽范围的产品制剂中(例如,精华、眼霜、爽肤水、凝胶、面膜、面膜等)。
Description
相关申请的交叉引用
本申请要求2014年12月3日提交的美国临时申请第62/086790号、2015年1月15日提交的美国临时申请第62/103942号的权益,其内容通过引用并入到本申请中。
技术领域
本发明一般涉及能够用于改善皮肤视觉外观的组合物和方法。在一些方面,本文公开的组合物可以包括例如用于去角质、减少或消除由于去角质引起的刺激、使皮肤更新、增加皮肤光泽、舒缓皮肤、和/或增加皮肤光滑度的成分的组合。
背景技术
衰老、长期暴露于不利的环境因素、营养失调、疲劳等会以被认为在视觉上不期望的方式改变皮肤的视觉外观、物理性能或生理功能。最显著和明显的改变包括细纹和皱纹的发展、弹性的损失、增加的下垂、坚实度的损失、颜色均匀性或色调的损失、粗糙的表面纹理和斑驳的着色。随着皮肤老化或经历长期的环境损害而发生的稍不明显但可测量的改变包括细胞和组织活性的普遍降低、细胞复制速率的降低、减少的皮肤血流、降低的水分含量、累积的结构和功能错误、普通生化过程正常调节的变化以及皮肤改造和修复自身的能力的降低。皮肤的外观和功能的许多变化由皮肤的外表皮层的改变导致,而其他的变化由下面真皮的改变导致。
之前的利用已知的皮肤活性成分改善皮肤视觉外观的尝试已经显示出具有各种缺点,例如皮肤刺激性和较长的恢复期。
发明内容
本发明人确定多种化合物、组合物和提取物具有治疗效果。具体地,本发明人识别了用来去角质、减少或消除由于为皮肤去角质引起的皮肤刺激、使皮肤更新和/或增加皮肤光泽和/或光滑度的一组制剂。这得到了具有优异的去角质性质而不具有一些典型地与去角质产品有关的负面作用的产品和/或能够减少皮肤去角质的不期望的副作用的产品。已经确认一组制剂一起起作用以提供在制剂的单个成分中不存在的活性。
就这一点而言,公开了包括以下成分的组合物:4-叔丁基环己醇、浮游生物提取物、芦苇(Phragmites communis)提取物、茯苓(Poria cocos)提取物、西葫芦(CucurbitaPepo)籽提取物、米赫毛霉(Mucor miehei)提取物、芽孢杆菌发酵产物、胭脂仙人掌(Opuntia coccinellifera)花提取物和/或水解梨果仙人掌(Opuntia ficus-indica)花提取物。在具体的方面,本文公开的组合物可以包含所述化合物、组合物和提取物中的任何一种、任意组合、全部或至少1、2、3、4、5、6、7或8种。在具体的实例中,4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物和西葫芦(Cucurbita Pepo)籽提取物的组合特别好地用于减少或消除来自去角质的刺激、使皮肤更新和/或增加皮肤光泽和光滑度。在另一个具体实例中,米赫毛霉提取物、芽孢杆菌发酵产物、浮游生物提取物和胭脂仙人掌花提取物或水解梨果仙人掌花提取物的组合特别好地用于去角质、减少或消除来自去角质的刺激、使皮肤更新和/或增加皮肤光泽和光滑度。在另一个具体实例中,以上组合物很好地用于减少由于皮肤暴露于去角质成分(exfoliant)、α羟基酸或组合物中可能存在或可能不存在的酸而引起的皮肤刺激。在又一个具体实例中,以上组合物是能够给皮肤去角质的面膜的组分。
在一个实例中,公开了能够去角质、能够减少或消除来自去角质的刺激、能够进行皮肤更新和或/能够增加皮肤光泽和/或光滑度的局部皮肤用组合物,其包含以下成分的任何一种、任意组合、或全部:水、三乙醇胺、羟基乙酸、甘油、丁二醇、海水、鲸蜡硬脂醇、花生醇、异硬脂酸失水山梨醇酯、碳酸二辛酯、生物糖胶-1、二十二醇、丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、丙烯酰基二甲基牛磺酸铵/VP共聚物、戊二醇、二氢茉莉酮酸甲酯、异十六烷、阿拉伯胶树(Acacia senegal)胶提取物、鲸蜡硬脂基葡糖苷、花生基葡萄糖苷、4-叔丁基环己醇、硅酸镁铝、聚二甲基硅氧烷、巴西酸亚乙酯、黄原胶、乙基芳樟醇、聚山梨醇酯60、EDTA二钠、二氧化钛、浮游生物提取物、芦苇提取物、茯苓提取物和/或西葫芦(Cucurbita Pepo)籽提取物。组合物中成分的量可以改变。这些成分的浓度的范围可以为以组合物的重量或体积计从0.00001%到99%,或者是如本说明书其他部分中所说明的其中可得到的任意的整数或范围,其通过引用并入本段。在一个实例中,组合物包含25重量%至80重量%(w/w)的水、3重量%至15重量%的三乙醇胺、2重量%至20重量%的羟基乙酸、1重量%至10重量%的甘油、1重量%至10重量%的丁二醇、0.1重量%至5重量%的海水、0.1重量%至5重量%的鲸蜡硬脂醇、0.1重量%至5重量%的花生醇、0.1重量%至5重量%的异硬脂酸失水山梨醇酯、0.1重量%至3重量%的碳酸二辛酯、0.1重量%至3重量%的生物糖胶-1、0.1重量%至3重量%的二十二醇、0.1重量%至3重量%的丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、0.1重量%至3重量%的丙烯酰基二甲基牛磺酸铵/VP共聚物、0.1重量%至3重量%的戊二醇、0.1重量%至3重量%的二氢茉莉酮酸甲酯、0.1重量%至3重量%的异十六烷、0.1重量%至1.5重量%的阿拉伯胶树胶提取物、0.1重量%至1.5重量%的鲸蜡硬脂基葡糖苷、0.1重量%至1.5重量%的花生基葡萄糖苷、0.1重量%至1.5重量%的4-叔丁基环己醇、0.01重量%至1重量%的硅酸镁铝、0.01重量%至1重量%的聚二甲基硅氧烷、0.01重量%至1重量%的巴西酸亚乙酯、0.01重量%至1重量%的黄原胶、0.01重量%至1重量%的乙基芳樟醇、0.01重量%至1重量%的聚山梨醇酯60、0.01重量%至1重量%的EDTA二钠、0.01重量%至1重量%的二氧化钛、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物和/或0.0001重量%至0.01重量%的西葫芦(Cucurbita Pepo)籽提取物。在具体的方面,水的浓度可以是至少35重量%至80重量%的水。
在另一个实例中,公开了能够去角质、能够减少或消除来自去角质的刺激、能够进行皮肤更新和或/能够增加皮肤光泽和/或光滑度的局部皮肤用组合物,其包含以下成分的任何一种、任意组合、或全部:水、米赫毛霉提取物、芽孢杆菌发酵产物、浮游生物提取物、胭脂仙人掌花提取物和/或水解梨果仙人掌花提取物。在一些实例中,组合物还包含聚硅氧烷-11、环戊硅氧烷、聚二甲基硅氧烷、甘油、PEG-10聚二甲基硅氧烷、丁二醇、双-PEG-18甲基醚二甲基硅烷、苯氧乙醇、丙烯酰基二甲基牛磺酸铵/VP共聚物、丙二醇、生物糖胶-1、阿拉伯胶树胶提取物、丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、角鲨烷、癸二醇、柠檬酸钠、羟乙基纤维素、1,2-己二醇、柠檬酸、甘草酸二钾、生育酚乙酸酯、黄原胶、羟丙基环糊精、三乙醇胺、聚山梨醇酯60、EDTA二钠、异硬脂酸失水山梨醇酯和/或山梨酸钾。这些成分的浓度的范围可以为以组合物的重量或体积计从0.00001%到99%,或者是如本说明书其他部分中所说明的其中可得到的任意的整数或范围,其通过引用并入本段。在具体的方面,组合物包含40重量%至60重量%的水、0.01重量%至1重量%的米赫毛霉提取物、0.001重量%至1重量%的芽孢杆菌发酵产物、0.001重量%至0.1重量%的浮游生物提取物、0.01重量%至1重量%的水解梨果仙人掌花提取物或胭脂仙人掌花提取物、10重量%至30重量%的聚硅氧烷-11、5重量%至20重量%的环戊硅氧烷、1重量%至10重量%的聚二甲基硅氧烷、1重量%至10重量%的甘油、1重量%至10重量%的PEG-10聚二甲基硅氧烷、0.5重量%至5重量%的丁二醇、0.5重量%至5重量%的双-PEG-18甲基醚二甲基硅烷、0.1重量%至3重量%的苯氧乙醇、0.1重量%至3重量%的丙烯酰基二甲基牛磺酸铵/VP共聚物、0.1重量%至3重量%的丙二醇、0.1重量%至3重量%的生物糖胶-1、0.1重量%至1.5重量%的阿拉伯胶树胶提取物、0.1重量%至1.5重量%的丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、0.1重量%至1.5重量%的角鲨烷、0.01重量%至1重量%的癸二醇、0.01重量%至1重量%的柠檬酸钠、0.01重量%至1重量%的羟乙基纤维素、0.01重量%至1重量%的1,2-己二醇、0.01重量%至1重量%的柠檬酸、0.01重量%至1重量%的甘草酸二钾、0.01重量%至1重量%的生育酚乙酸酯、0.01重量%至1重量%的黄原胶、0.01重量%至1重量%的羟丙基环糊精、0.01重量%至1重量%的三乙醇胺、0.01重量%至1重量%的聚山梨醇酯60、0.01重量%至1重量%的EDTA二钠、0.001重量%至0.1重量%的异硬脂酸失水山梨醇酯、和/或0.001重量%至0.1重量%的山梨酸钾。
在具体的方面,水的浓度可以是至少35重量%至80重量%的水。在一些实例中,组合物还包含腺苷。在一些实例中,组合物包含0.001重量%至1重量%的腺苷。在一些实例中,组合物还可以包含仙人果(Oputia tuna)果提取物。在一些实例中,组合物包含0.00001重量%至0.01重量%的仙人果果提取物。在一些实例中,组合物还可以包含α-羟基酸。在一些实例中,α-羟基酸是羟基乙酸。在一些实例中,组合物是乳液。
还公开了抵消由去角质成分引起的皮肤刺激的方法,其包括对有此需要的皮肤局部施用本文公开的组合物中的任何一种。在一个实例中,皮肤刺激可以是由α羟基酸引起的。在另一个方面,公开了一种使皮肤去角质的方法,其包括局部地施用本文公开的组合物中的任何一种。还公开了本文公开的方法的任一种还可以包括对面部施用组合物。
还公开了本发明的以下实施方案1至132。实施方案1是抵消由去角质成分引起的皮肤刺激的方法,其包括对有此需要的皮肤局部地施用包含以下成分的组合物:水、4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物、和西葫芦(Cucurbita Pepo)籽提取物。实施方案2是实施方案1的方法,其中所述组合物包含:25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物、和0.0001重量%至0.01重量%的西葫芦(Cucurbita Pepo)籽提取物。实施方案3是实施方案1的方法,其中西葫芦(Cucurbita Pepo)籽提取物增加皮肤中胶原蛋白的产生。实施方案4是实施方案1的方法,其中西葫芦(Cucurbita Pepo)籽提取物增加皮肤中的胶原蛋白生成。实施方案5是实施方案1的方法,其中4-叔丁基环己醇减少皮肤的刺激。实施方案6是实施方案1的方法,其中浮游生物提取物调节皮肤。实施方案7是实施方案1的方法,其中浮游生物提取物减少皮肤的炎症。实施方案8是实施方案1的方法,其中芦苇提取物和茯苓提取物减少皮肤的炎症。实施方案9是实施方案1的方法,其中芦苇提取物和茯苓提取物增加皮肤屏障的修复和/或皮肤屏障的维护。实施方案10是实施方案1的方法,其中组合物被配制成面膜。实施方案11是实施方案1的方法,其中去角质成分是α羟基酸。实施方案12是实施方案10的方法,其中组合物还包含去角质成分。实施方案13是实施方案12的方法,其中去角质成分是α羟基酸。实施方案14是实施方案13的方法,其中组合物包含2重量%至20重量%的α羟基酸。实施方案15是实施方案14的方法,其中α羟基酸是羟基乙酸。实施方案16是实施方案1的方法,其还包括对面部施用组合物。实施方案17是给皮肤去角质的方法,其包括局部地施用包含以下成分的组合物:水、4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物、西葫芦(Cucurbita Pepo)籽提取物和去角质成分。实施方案18是实施方案17的方法,其中所述组合物包含:25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物、和0.0001重量%至0.01重量%的西葫芦(CucurbitaPepo)籽提取物。实施方案19是实施方案17的方法,其中西葫芦(Cucurbita Pepo)籽提取物增加皮肤中胶原蛋白的产生。实施方案20是实施方案17的方法,其中西葫芦(CucurbitaPepo)籽提取物增加皮肤中的胶原蛋白生成。实施方案21是实施方案17的方法,其中4-叔丁基环己醇减少皮肤的刺激。实施方案22是实施方案17的方法,其中浮游生物提取物调节皮肤。实施方案23是实施方案17的方法,其中浮游生物提取物减少皮肤的炎症。实施方案24是实施方案17的方法,其中芦苇提取物和茯苓提取物减少皮肤的炎症。实施方案25是实施方案17的方法,其中芦苇提取物和茯苓提取物增加皮肤屏障修复和/或皮肤屏障维护。实施方案26是实施方案17的方法,其中组合物被配制成面膜。实施方案27是实施方案17的方法,其中去角质成分是α羟基酸。实施方案28是实施方案27的方法,其中组合物包含2重量%至20重量%的α羟基酸。实施方案29是实施方案28的方法,其中α羟基酸是羟基乙酸。实施方案30是实施方案17的方法,其还包括对面部施用组合物。实施方案31是增加皮肤中胶原蛋白生成的方法,其包括局部地施用包含以下成分的组合物:水、4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物和西葫芦(Cucurbita Pepo)籽提取物,其中,皮肤中的胶原蛋白生成增加。实施方案32是实施方案31的方法,其中所述组合物包含:25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物和0.0001重量%至0.01重量%的西葫芦(Cucurbita Pepo)籽提取物。实施方案33是实施方案31的方法,其中西葫芦(Cucurbita Pepo)籽提取物增加皮肤中胶原蛋白的产生。实施方案34是实施方案31的方法,其中西葫芦(Cucurbita Pepo)籽提取物增加皮肤中的胶原蛋白生成。实施方案35是实施方案31的方法,其中4-叔丁基环己醇减少皮肤的刺激。实施方案36是实施方案31的方法,其中浮游生物提取物调节皮肤。实施方案37是实施方案31的方法,其中浮游生物提取物减少皮肤的炎症。实施方案38是实施方案31的方法,其中芦苇提取物和茯苓提取物减少皮肤的炎症。实施方案39是实施方案31的方法,其中芦苇提取物和茯苓提取物增加皮肤屏障修复和/或皮肤屏障维护。实施方案40是实施方案31的方法,其中组合物被配制成面膜。实施方案41是实施方案40的方法,其中组合物还包含去角质成分。实施方案42是实施方案41的方法,其中去角质成分是α羟基酸。实施方案43是实施方案42的方法,其中组合物包含2重量%至20重量%的α羟基酸。实施方案44是实施方案43的方法,其中α羟基酸是羟基乙酸。实施方案45是实施方案31的方法,其还包括对面部施用组合物。实施方案46是抑制皮肤中MMP3活性的方法,其包括局部地施用包含以下成分的组合物:水、4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物和西葫芦(Cucurbita Pepo)籽提取物,其中,皮肤中的MMP3活性降低。实施方案47是实施方案46的方法,其中所述组合物包含:25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物和0.0001重量%至0.01重量%的西葫芦(Cucurbita Pepo)籽提取物。实施方案48是实施方案46的方法,其中西葫芦(Cucurbita Pepo)籽提取物增加皮肤中胶原蛋白的产生。实施方案49是实施方案46的方法,其中西葫芦(Cucurbita Pepo)籽提取物增加皮肤中的胶原蛋白生成。实施方案50是实施方案46的方法,其中4-叔丁基环己醇减少皮肤的刺激。实施方案51是实施方案46的方法,其中浮游生物提取物调节皮肤。实施方案52是实施方案46的方法,其中浮游生物提取物减少皮肤的炎症。实施方案53是实施方案46的方法,其中芦苇提取物和茯苓提取物减少皮肤的炎症。实施方案54是实施方案46的方法,其中芦苇提取物和茯苓提取物增加皮肤屏障修复和/或皮肤屏障维护。实施方案55是实施方案46的方法,其中组合物被配制成面膜。实施方案56是实施方案55的方法,其中组合物还包含去角质成分。实施方案57是实施方案56的方法,其中去角质成分是α羟基酸。实施方案58是实施方案57的方法,其中组合物包含2重量%至20重量%的α羟基酸。实施方案59是实施方案58的方法,其中α羟基酸是羟基乙酸。实施方案60是实施方案46的方法,其还包括对面部施用组合物。实施方案61是抵消由去角质成分引起的皮肤刺激的方法,其包括对有此需要的皮肤局部地施用包含以下成分的组合物:米赫毛霉提取物、芽孢杆菌发酵产物、浮游生物提取物、和水解梨果仙人掌花提取物或胭脂仙人掌花提取物。实施方案62是实施方案61的方法,其中至有此需要的皮肤的所述组合物包含:40重量%至60重量%的水、0.01重量%至1重量%的米赫毛霉提取物、0.001重量%至1重量%的芽孢杆菌发酵产物和0.001重量%至1重量%的水解梨果仙人掌花提取物或胭脂仙人掌花提取物。实施方案63是实施方案61的方法,其中组合物还包含25重量%至80重量%的水。实施方案64是实施方案61的方法,其中米赫毛霉提取物使皮肤去角质。实施方案65是实施方案61的方法,其中芽孢杆菌发酵产物使皮肤去角质。实施方案66是实施方案61的方法,其中浮游生物提取物调节皮肤。实施方案67是实施方案61的方法,其中浮游生物提取物减少皮肤的炎症。实施方案68是实施方案61的方法,其中组合物包含水解梨果仙人掌花提取物,并且水解梨果仙人掌花提取物使皮肤去角质。实施方案69是实施方案61的方法,其中组合物还包含:腺苷。实施方案70是实施方案69的方法,其中组合物包含0.001重量%至0.1重量%的腺苷。实施方案71是实施方案61的方法,其中组合物还包含:仙人果果提取物。实施方案72是实施方案71的方法,其中组合物包含0.00001重量%至0.01重量%的仙人果果提取物。实施方案73是实施方案61的方法,其中组合物被配制成面膜。实施方案74是实施方案73的方法,其中组合物还包含α羟基酸。实施方案75是实施方案74的方法,其中组合物包含2重量%至20重量%的α羟基酸。实施方案76是实施方案75的方法,其中α羟基酸是羟基乙酸。实施方案77是实施方案61的方法,其中皮肤刺激是由α羟基酸引起的。实施方案78是实施方案61的组合物,其中组合物为乳液。实施方案79是实施方案61的方法,其还包括对面部施用组合物。实施方案80是使皮肤去角质的方法,其包括局部地施用包含以下成分的组合物:米赫毛霉提取物、芽孢杆菌发酵产物、浮游生物提取物和水解梨果仙人掌花提取物或胭脂仙人掌花提取物。实施方案81是实施方案80的方法,其中至有此需要的皮肤的所述组合物包含:40重量%至60重量%的水、0.01重量%至1重量%的米赫毛霉提取物、0.001重量%至1重量%的芽孢杆菌发酵产物、0.001重量%至0.1重量%的浮游生物提取物、和0.01重量%至1重量%的水解梨果仙人掌花提取物或胭脂仙人掌花提取物。实施方案82是实施方案80的方法,其中组合物还包含25重量%至80重量%的水。实施方案83是实施方案80的方法,其中米赫毛霉提取物使皮肤去角质。实施方案84是实施方案80的方法,其中芽孢杆菌发酵产物使皮肤去角质。实施方案85是实施方案80的方法,其中浮游生物提取物调节皮肤。实施方案86是实施方案80的方法,其中浮游生物提取物减少皮肤的炎症。实施方案87是实施方案80的方法,其中组合物包含水解梨果仙人掌花提取物,并且水解梨果仙人掌花提取物使皮肤去角质。实施方案88是实施方案80的方法,其中组合物还包含:腺苷。实施方案89是实施方案88的方法,其中组合物包含0.001重量%至1重量%的腺苷。实施方案90是实施方案80的方法,其中组合物还包含:仙人果果提取物。实施方案91是实施方案90的方法,其中组合物包含0.00001重量%至0.01重量%的仙人果果提取物。实施方案92是实施方案80的方法,其中组合物被配制成面膜。实施方案93是实施方案92的方法,其中组合物还包含α羟基酸。实施方案94是实施方案93的方法,其中组合物包含2重量%至20重量%的α羟基酸。实施方案95是实施方案94的方法,其中α羟基酸是羟基乙酸。实施方案96是实施方案80的组合物,其中组合物为乳液。实施方案97是实施方案80的方法,其还包括对面部施用组合物。实施方案98是包含以下成分的局部皮肤用组合物:水、4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物和西葫芦(Cucurbita Pepo)籽提取物。实施方案99是实施方案98的局部皮肤用组合物,其包含25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物和0.0001重量%至0.01重量%的西葫芦(Cucurbita Pepo)籽提取物。实施方案100是实施方案98的局部皮肤用组合物,其还包含:三乙醇胺、甘油、丁二醇、海水、鲸蜡硬脂醇、花生醇、异硬脂酸失水山梨醇酯、碳酸二辛酯、生物糖胶-1和二十二醇。实施方案101是实施方案100的局部皮肤用组合物,其包含:3重量%至15重量%的三乙醇胺、1重量%至10重量%的甘油、1重量%至10重量%的丁二醇、0.1重量%至5重量%的海水、0.1重量%至5重量%的鲸蜡硬脂醇、0.1重量%至5重量%的花生醇、0.1重量%至5重量%的异硬脂酸失水山梨醇酯、0.1重量%至3重量%的碳酸二辛酯、0.1重量%至3重量%的生物糖胶-1和0.1重量%至3重量%的二十二醇。实施方案102是实施方案100的局部皮肤用组合物,其还包含:丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、丙烯酰基二甲基牛磺酸铵/VP共聚物、戊二醇、二氢茉莉酮酸甲酯、异十六烷、阿拉伯胶树胶提取物、鲸蜡硬脂基葡糖苷、花生基葡萄糖苷、硅酸镁铝、聚二甲基硅氧烷、巴西酸亚乙酯、黄原胶、乙基芳樟醇、聚山梨醇酯60、EDTA二钠和二氧化钛。实施方案103是实施方案102的局部皮肤用组合物,其包含:0.1重量%至3重量%的丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、0.1重量%至3重量%的丙烯酰基二甲基牛磺酸铵/VP共聚物、0.1重量%至3重量%的戊二醇、0.1重量%至3重量%的二氢茉莉酮酸甲酯、0.1重量%至3重量%的异十六烷、0.1重量%至1.5重量%的阿拉伯胶树胶提取物、0.1重量%至1.5重量%的鲸蜡硬脂基葡糖苷、0.1重量%至1.5重量%的花生基葡萄糖苷、0.01重量%至1重量%的硅酸镁铝、0.01重量%至1重量%的聚二甲基硅氧烷、0.01重量%至1重量%的巴西酸亚乙酯、0.01重量%至1重量%的黄原胶、0.01重量%至1重量%的乙基芳樟醇、0.01重量%至1重量%的聚山梨醇酯60、0.01重量%至1重量%的EDTA二钠和0.01重量%至1重量%的二氧化钛。实施方案104是实施方案98的局部皮肤用组合物,其中组合物能够抵消由去角质成分引起的皮肤刺激。实施方案105是实施方案104的局部皮肤用组合物,其中组合物能够抵消由α羟基酸引起的皮肤刺激。实施方案106是实施方案98的局部皮肤用组合物,其中组合物被配制成面膜。实施方案107是实施方案106的局部皮肤用组合物,其还包含去角质成分。实施方案108是实施方案107的局部皮肤用组合物,其中去角质成分是α羟基酸。实施方案109是实施方案108的局部皮肤用组合物,其包含2重量%至20重量%的α羟基酸。实施方案110是实施方案109的局部皮肤用组合物,其中α羟基酸是羟基乙酸。实施方案111是实施方案98的局部皮肤用组合物,其中组合物能够增加皮肤中的胶原蛋白生成。实施方案112是实施方案98的局部皮肤用组合物,其中组合物能够抑制皮肤中MMP3活性。实施方案113是一种局部皮肤用组合物,其包含:米赫毛霉提取物、芽孢杆菌发酵产物、浮游生物提取物和水解梨果仙人掌花提取物或胭脂仙人掌花提取物。实施方案114是实施方案113的局部皮肤用组合物,其中所述组合物包含:40重量%至60重量%的水、0.01重量%至1重量%的米赫毛霉提取物、0.001重量%至1重量%的芽孢杆菌发酵产物、0.001重量%至0.1重量%的浮游生物提取物、和0.01重量%至1重量%的水解梨果仙人掌花提取物或胭脂仙人掌花提取物。实施方案115是实施方案113的局部皮肤用组合物,其还包含:聚硅氧烷-11、环戊硅氧烷、聚二甲基硅氧烷、甘油、PEG-10聚二甲基硅氧烷、丁二醇和双-PEG-18甲基醚二甲基硅烷。实施方案116是实施方案115的局部皮肤用组合物,其包含:10重量%至30重量%的聚硅氧烷-11、5重量%至20重量%的环戊硅氧烷、1重量%至10重量%的聚二甲基硅氧烷、1重量%至10重量%的甘油、1重量%至10重量%的PEG-10聚二甲基硅氧烷、0.5重量%至5重量%的丁二醇和0.5重量%至5重量%的双-PEG-18甲基醚二甲基硅烷。实施方案117是实施方案115的局部皮肤用组合物,其还包含:苯氧乙醇、丙烯酰基二甲基牛磺酸铵/VP共聚物、丙二醇、生物糖胶-1、阿拉伯胶树胶提取物、丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、角鲨烷、癸二醇、柠檬酸钠、羟乙基纤维素、1,2-己二醇、柠檬酸、甘草酸二钾、生育酚乙酸酯和黄原胶。实施方案118是实施方案117的局部皮肤用组合物,其包含:0.1重量%至3重量%的苯氧乙醇、0.1重量%至3重量%的丙烯酰基二甲基牛磺酸铵/VP共聚物、0.1重量%至3重量%的丙二醇、0.1重量%至3重量%的生物糖胶-1、0.1重量%至1.5重量%的阿拉伯胶树胶提取物、0.1重量%至1.5重量%的丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、0.1重量%至1.5重量%的角鲨烷、0.01重量%至1重量%的癸二醇、0.01重量%至1重量%的柠檬酸钠、0.01重量%至1重量%的羟乙基纤维素、0.01重量%至1重量%的1,2-己二醇、0.01重量%至1重量%的柠檬酸、0.01重量%至1重量%的甘草酸二钾、0.01重量%至1重量%的生育酚乙酸酯和0.01重量%至1重量%的黄原胶。实施方案119。实施方案117的局部皮肤用组合物,其还包含:羟丙基环糊精、三乙醇胺、聚山梨醇酯60、EDTA二钠、异硬脂酸失水山梨醇酯和山梨酸钾。实施方案120。权利要求119所述局部皮肤用组合物,其包含:0.01重量%至1重量%的羟丙基环糊精、0.01重量%至1重量%的三乙醇胺、0.01重量%至1重量%的聚山梨醇酯60、0.01重量%至1重量%的EDTA二钠、0.001重量%至0.1重量%的异硬脂酸失水山梨醇酯和0.001重量%至0.1重量%的山梨酸钾。实施方案121是实施方案113的局部皮肤用组合物,其包含25重量%至80重量%的水。实施方案122是实施方案113的局部皮肤用组合物,其还包含:腺苷。实施方案123是实施方案122的局部皮肤用组合物,其中组合物包含0.001重量%至1重量%的腺苷。实施方案124是实施方案113的局部皮肤用组合物,其中组合物还包含:仙人果果提取物。实施方案125是实施方案124的局部皮肤用组合物,其中组合物包含0.00001重量%至0.01重量%的仙人果果提取物。实施方案126是实施方案113的局部皮肤用组合物,其中组合物能够抵消由去角质成分引起的皮肤刺激。实施方案127是实施方案126的局部皮肤用组合物,其中组合物能够抵消由α羟基酸引起的皮肤刺激。实施方案128是实施方案113的局部皮肤用组合物,其中组合物被配制成面膜。实施方案129是实施方案128的局部皮肤用组合物,其还包含α羟基酸。实施方案130是实施方案129的局部皮肤用组合物,其包含2重量%至20重量%的α羟基酸。实施方案131是实施方案130的局部皮肤用组合物,其中α羟基酸是羟基乙酸。实施方案132是实施方案113的局部皮肤用组合物,其中组合物是乳液。
在局部施用后组合物的任一种可以在皮肤上保留30秒、1、2、3、4、5、6、7、8、9、10、15、20、30、40、50或60分钟或更长时间。需要组合物的皮肤可以是具有细纹或皱纹的皮肤或者不均匀的皮肤。不均匀的皮肤可以是具有色素过度沉着皮肤、黄褐斑、雀斑、暗斑、老年斑、褐斑等的皮肤。在已经施用组合物后,可以保护皮肤免于受刺激、变红、变干燥、片状剥落或皲裂。保护包括减小在使用皮肤去角质组合物后皮肤形成所述症状的可能性。
在具体的方面,本文公开的组合物配制为局部皮肤用组合物。组合物可以具有用于化合物、组合物和提取物的皮肤病学可接受的载剂或载体。组合物可以还包含保湿剂或湿润剂、表面活性剂、含硅酮的化合物、UV剂、油、非天然存在的化合物和/或本说明书中确定的其他成分或本领域中已知的成分。组合物可以包含另外的非天然存在的成分。组合物可以是蜜露、乳霜、凝胶、精华、乳剂(例如水包油、油包水、水包硅酮、硅酮包水、水包油包水、水包油、油包水包油、硅酮包水包油等)、溶液(例如水的或水-醇溶液)、无水赋形剂(例如口红或粉末)、软膏、乳液、糊剂、气溶胶、固体形式、眼部凝胶等。组合物可以是粉末形式(例如,干燥的、冻干的颗粒等)。组合物可以配制用于在使用期间每天局部皮肤施用至少1、2、3、4、5、6、7或更多次。本文公开的其它方面中,组合物可以是储存稳定或颜色稳定的,或是两者。还期望可以选择组合物的黏度以达到希望的结果,例如根据希望的组合物类型,该组合物的黏度可以为1cps到远超过1百万cps,或者是其中可得到的任意范围或整数(例如,在25℃下用TC轴以2.5rpm在布氏黏度计上测量的2cps、3、4、5、6、7、8、9、10、20、30、40、50、60、70、80、90、100、200、300、400、500、600、700、800、900、1000、2000、3000、4000、5000、6000、7000、8000、9000、10000、20000、30000、40000、50000、60000、70000、80000、90000、100000、200000、300000、400000、500000、600000、700000、800000、900000、1000000、2000000、3000000、4000000、5000000、10000000cps等)。
在具体的实例中,组合物中的提取物可以来自整个生物体或植物,并且可以是水提取物。然而,预期除了整个生物体或植物以外,可以使用生物体或植物的部分(例如根、茎皮、汁、茎、叶、花、种子、叶、茎、根、花、种子、汁、茎皮等),如此使得在排除生物体或植物的其他部分的条件下使用生物体或植物的一部分以制备提取物。如上所述,提取物可以是水提取物,但也可以是非水提取物。可以用醇(例如甲醇、乙醇、丙醇、丁醇等)、二醇(例如丁二醇、丙二醇等)、油、水等来提取提取物。提取物可以包含不天然地存在于一起的、或者不以自然中存在的比例或浓度天然地存在于一起的部分、化学品等。提取物可以被包含在组合物中,例如局部皮肤用组合物、可食用组合物、可注射组合物、口服组合物、药物组合物、毛发护理组合物等。组合物可以包含0.0001重量%至20重量%的所述生物体或植物、生物体部分或植物部分、和/或其提取物(或者0.001、0.01、0.1、0.2、0.3、0.4、0.5、0.6、0.7、0.8、0.9、1、2、3、4、5、6、7、8、9、10、11、12、13、14、15、16、17、18、19、20、30、40、50、60、70、80、90、99%或更多,或者其中的任意整数或范围)。
还可以对本文公开的组合物进行改变以具有期望的氧自由基吸收能力(ORAC)值。在某些非限制性方面,可以改变本说明书通篇涉及的本文公开的组合物或植物、植物部分或其提取物以具有每毫克至少约1、2、3、4、5、6、7、8、9、10、11、12、13、14、15、16、17、18、19、20、21、22、23、24、25、26、27、28、29、30、35、40、45、50、55、60、70、80、90、95、100、200、300、400、500、600、700、800、900、1000、2000、3000、4000、5000、6000、7000、8000、9000、10000、15000、20000、30000、50000、100000或更多,或者其中可得到的任意范围的ORAC值。
该组合物在非限制性方面可以具有约6至约9的pH值。在其它方面,pH可以是1、2、3、4、5、6、7、8、9、10、11、12、13或14。组合物可以包含甘油三酸酯。非限制性实例包括小的、中等的和大的链甘油三酸酯。在一些方面,甘油三酸酯是中链甘油三酸酯(例如三辛酸癸酸甘油酯)。组合物还可以包含防腐剂。防腐剂的非限制性实例包括对羟基苯甲酸甲酯、对羟基苯甲酸丙酯或对羟基苯甲酸甲酯和对羟基苯甲酸丙酯的混合物。
本文公开的组合物还可以包含以下另外的成分的任意一种、任意组合或全部:水、螯合剂、保湿剂、防腐剂、增稠剂、含硅酮的化合物、精油、结构化剂、维生素、药物成分、非天然存在的化合物、或抗氧化剂、或这类成分的任意组合或这类成分的混合物。在某些方面,该组合物可以包含在之前句子中所指出的这些附加成分的至少二、三、四、五、六、七、八、九、十种或全部。这些附加成分的非限制性实例在本说明书通篇指出并通过引用并入本部分。这类成分的量可以是以组合物的重量或体积计的0.0001%至99.9%,或者如本说明书其它部分中所公开的任意整数或范围中,其通过引用并入本段。
还预期包含本文公开的组合物的试剂盒。在某些实施方案中,该组合物包含在容器中。该容器可以是瓶子、分配器或包装。该容器可以分配预定量的组合物。在某些方面,以喷雾、团块或流体分配组合物。容器可以在其表面上包含标记。该标记可以是单词、缩写、图片或符号。
还预期的是本说明书通篇所公开的所述组合物可以被用作免洗型或洗去型组合物。举例来说,免洗型组合物可以是被局部地施用至皮肤并在皮肤上保留一段时间(例如,至少5、6、7、8、9、10、20或30分钟,或至少1、2、3、4、5、6、7、8、9、10、11、12、13、14、15、16、17、18、19、20、21、22、23或24小时,或者整夜或整个白天)的组合物。或者,洗去型组合物可以是意在施用至皮肤、然后在一段时间如小于5、4、3、2或1分钟内从皮肤去除或洗去(比如用水)的产品。洗去型组合物的实例可以是皮肤清洁剂、洗发水、护发素或肥皂。免洗型组合物的实例子可以是皮肤保湿剂、防晒剂、面膜、晚霜或日霜。
预期的是本说明书中所讨论的任何实施方案可以针对本发明的任何方法或组合物来实施,反之亦然。此外,本文公开的组合物可以用于实现本发明的方法。
在一个实施方案中,本文公开的组合物可以是可药用的或可化妆用的,或可以具有舒适的触觉性质。“可药用的”、“可化妆用的”和/或“舒适的触觉性质”描述具有令皮肤感觉舒适的特定的触觉性质的组合物(例如,不是太水或太油的组合物、具有丝滑质地的组合物、非粘性或粘性的组合物等)。可药用的或可化妆用的还可以涉及组合物的乳脂状或润滑性能,或组合物的水分保留性能。
“局部施用”是指施用或涂敷组合物到嘴唇或角质组织的表面上。“局部皮肤用组合物”包括适合在嘴唇或角质组织局部施用的组合物。这类组合物一般为皮肤病学可接受的,这是因为当施用到嘴唇或皮肤时,其不具有异常毒性、不相容性、不稳定性、过敏反应等。本文公开的局部护肤组合物可以具有选定的黏度以避免施用到皮肤后明显的滴落或淤积。
“角质组织”包括配置作为哺乳类最外保护层的含有角质的层,并且包括但不限于嘴唇、皮肤、毛发和指甲。
术语“大约”或“约”定义为如本领域普通技术人员所理解的接近于,并且在一个非限制性实施方案中该术语定义为在10%以内,优选在5%以内,更优选在1%以内,最优选在0.5%以内。
术语“基本上”及其变体定义为如本领域普通技术人员所理解的大部分但不一定为所指定的全部,并且在一个非限定性实施方案中基本上指的是在10%以内、5%以内、1%以内或0.5%以内的范围。
术语“抑制”或“减少”或这些术语的任何变体包括实现期望结果的任何可测量的减少或完全的抑制。术语“促进”或“增加”或这些术语的任何变体包括实现期望结果的蛋白质或分子(例如,基质蛋白如纤连蛋白、层粘连蛋白、胶原蛋白或弹性蛋白,或者分子如透明质酸)的任何可测量的增加或产生。
如本说明书和/或权利要求所使用的术语,术语“有效的”表示足以实现期望的、预期的或想要的结果。
当在权利要求和/或说明书中与术语“包含”一起使用时,要素前面不使用数量词可以表示“一个”,但是其也符合“一个或更多个”、“至少一个”和“一个或多于一个”的意思。
如本说明书和权利要求所使用的,单词“包含”、“具有”、“包括”或“含有”是包括性的或开放式的,并且不排除另外的、未列举的元素或方法步骤。
组合物和其使用方法可以“包含”本说明书通篇所公开的成分或步骤的任一个、“主要由其组成”或“由其组成”。对于过渡短语“基本上由……构成”,在一个非限制性方面,本说明书中公开的组合物和方法的基本且新的特征包括组合物减少或预防与敏感性皮肤相关的症状(例如红斑)在使用者皮肤上出现的能力。
本发明的其它目的、特征和优点通过以下详细的描述会变得明显。然而,应理解详细的描述和实施例在表明本发明的具体实施方案时仅以举例说明的方式给出。另外,预期的是通过该详细描述,本发明的精神和范围内的变化和修改对于本领域技术人员会变得明显。
具体实施方式
在具体的实施方案中,可以使用以下任意任一种或者其任意组合:4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物、西葫芦(Cucurbita Pepo)籽提取物、米赫毛霉提取物、芽孢杆菌发酵产物、和胭脂仙人掌花提取物或水解梨果仙人掌花提取物。可以在宽范围的产品制剂(例如,精华素、眼霜、化妆水、凝胶、面膜、面膜等)中包含成分的这种组合。
如上所示,在此公开的本发明的几个独特的方面是使皮肤去角质、在去角质之后或期间消除由于皮肤去角质引起的皮肤刺激、使皮肤再生、和/或增加皮肤的光泽和/或光滑度。这能够实现皮肤去角质(其可以通过去除不想要的斑点如黄褐斑、皮肤色素沉着、老年斑、雀斑、暗斑等来减少细纹和皱纹的出现,或者甚至肤色)的益处且同时减少一些不必要的副作用。
以下小节进一步详细地描述本发明的非限制性的方面。
A.去角质和修复组合物
在此公开的具体的去角质组合物设计为用于减少或消除由于皮肤的去角质引起的皮肤刺激、使皮肤去角质且同时减少或者消除由于皮肤的去角质引起的皮肤刺激、使皮肤再生、和/或增加皮肤光泽和/或光滑度。组合物依赖于4-叔丁基环己醇、浮游生物提取物、芦苇提取物、茯苓提取物、和/或西葫芦(Cucurbita Pepo)籽提取物的独特组合。这种组合物的一个实例在实施例1、表1和表2中提供。虽然羟基乙酸可以被用作活性皮肤去角质成分,但是也可以使用其它酸和其它去角质成分(例如乳酸、柠檬酸、酶去角质成分等)。
在此公开的另一种具体的去角质组合物设计为减少或消除由于皮肤的去角质引起的皮肤刺激、在使皮肤去角质的同时减少或者消除由于皮肤的去角质引起的皮肤刺激、使皮肤再生、和/或增加皮肤光泽和/或光滑度。组合物依赖于米赫毛霉提取物、芽孢杆菌发酵产物、浮游生物提取物、水解梨果仙人掌花提取物、和/或胭脂仙人掌花提取物的独特组合。这种组合物的一个实例在实施例1、表3和表4中提供。虽然芽孢杆菌发酵产物可以被用作活性皮肤去角质成分,但是也可以使用羟基乙酸或其它酸和其它去角质成分(例如乳酸、柠檬酸、酶去角质成分等)。
在此公开的具体的修复组分设计为用于减少或消除由于皮肤的去角质引起的皮肤刺激、使皮肤再生、和/或增加皮肤光泽和/或光滑度。组合物依赖于在具有或者没有能够使皮肤去角质的额外成分的情况下的米赫毛霉提取物、芽孢杆菌发酵产物、浮游生物提取物、水解梨果仙人掌花提取物、和/或胭脂仙人掌提取物的独特组合。这种组合物的一个在实施例1、表3和表4中提供。
4-叔丁基环己醇是具有下式的有机化合物:
它是对减少皮肤的灼伤和刺痛有用的抗刺激剂。其可从各种不同来源商购得到(参见国际化妆品成分词典和手册,第12版,第1卷,第331页(2008),其通过引用并入本文)。
浮游生物提取物是从海洋生物质获得的提取物。它已知为皮肤调节剂。它还可以对皮肤提供脂肪酸、抗氧化剂和锌,以及减少皮肤的炎症和保护皮肤以防晒伤。浮游生物提取物可以通过商品名Benoitine从Barnet Products Corp.(USA)购买。在一些实施方案中,浮游生物提取物是由称为溶藻弧菌(Vibrio alginolyticus)和属于海洋浮游生物(Thalassoplankton)家族的微生物合成的表多糖。在一些实施方案中,浮游生物提取物是糖同分异构体,即一种由溶藻弧菌合成的胞外多糖。在一些实施方案中这个成分是商业上可获得的,例如,从Barnet获得,其提供商品名Benoiderm的糖同分异构体。
芦苇提取物和茯苓提取物有助于减少皮肤炎症。它具有屏障修复和屏障维护功能并有助于皮肤变得较不易于遭受外部攻击。它由Chemisches Laboratorium(CLR)(德国)通过商品名SyriCalmTMCLR提供。
西葫芦(Cucurbita Pepo)籽提取物为来自西葫芦籽的提取物,其可以从DracoNatural Products Inc.(美国)通过商品名PUMPKIN EXTRACTTM、从Naturex(美国)通过商品名PUMPKIN SEED GLYCOLIC EXTRACTTM、从Greentech S.A.(法国)通过商品名ARP 100TM和ARP 100TMHuileux、或者从Soliance(法国)通过商品名Ocaline PF购买。
米赫毛霉提取物可以从Active Organics(美国)通过商品名ActizymeTME3M-M购买。在一些实施方案中,米赫毛霉提取物为得自蘑菇的、天冬氨酸依赖的水溶性酶、或酸性蛋白酶类。在一些实施方案中,米赫毛霉提取物可以软化皮肤。
芽孢杆菌发酵产物可以从Sederma(法国)以商品名KeratolineTM购买。在一些实施方案中,芽孢杆菌发酵产物是枯草杆菌(Bacillus Subtilis)的发酵产物。在一些实施方案中,芽孢杆菌发酵产物可以使皮肤去角质。
水解梨果仙人掌花提取物可以从SiLab(法国)通过商品名ExfolactiveTMEL PX购买。在一些实施方案中,水解梨果仙人掌花提取物可以使皮肤去角质。
胭脂仙人掌花提取物是胭脂仙人掌的花的提取物。在一些实施方案中,该提取物可以调节皮肤。
腺苷酸是通常具有以下结构的杂环有机化合物:
腺苷酸可从各种不同来源商购得到(参见国际化妆品成分词典和手册,第12版,第1卷,第60页(2008),其通过引用并入本文)。
上述去角质和修复组合物可以应用于皮肤并在皮肤上保持一段时间(例如,至少1、2、3、4、5、10、20、30或60分钟或更多)。之后,如果需要可以将组合物从皮肤洗去或者从皮肤剥离。
C.成分的量
预期的是本文公开的组合物可以包含任意量的本说明书中讨论的成分。组合物还可包含任意数目的在本说明书全文中所描述的另外成分的组合(例如,颜料或另外的化妆品或药物成分)。在组合物中任意成分的浓度可以改变。例如,在非限制性实施方案中,组合物在其最终形式中可以包含、主要由以下组分组成或由以下组分组成:例如至少约0.0001%、0.0002%、0.0003%、0.0004%、0.0005%、0.0006%、0.0007%、0.0008%、0.0009%、0.0010%、0.0011%、0.0012%、0.0013%、0.0014%、0.0015%、0.0016%、0.0017%、0.0018%、0.0019%、0.0020%、0.0021%、0.0022%、0.0023%、0.0024%、0.0025%、0.0026%、0.0027%、0.0028%、0.0029%、0.0030%、0.0031%、0.0032%、0.0033%、0.0034%、0.0035%、0.0036%、0.0037%、0.0038%、0.0039%、0.0040%、0.0041%、0.0042%、0.0043%、0.0044%、0.0045%、0.0046%、0.0047%、0.0048%、0.0049%、0.0050%、0.0051%、0.0052%、0.0053%、0.0054%、0.0055%、0.0056%、0.0057%、0.0058%、0.0059%、0.0060%、0.0061%、0.0062%、0.0063%、0.0064%、0.0065%、0.0066%、0.0067%、0.0068%、0.0069%、0.0070%、0.0071%、0.0072%、0.0073%、0.0074%、0.0075%、0.0076%、0.0077%、0.0078%、0.0079%、0.0080%、0.0081%、0.0082%、0.0083%、0.0084%、0.0085%、0.0086%、0.0087%、0.0088%、0.0089%、0.0090%、0.0091%、0.0092%、0.0093%、0.0094%、0.0095%、0.0096%、0.0097%、0.0098%、0.0099%、0.0100%、0.0200%、0.0250%、0.0275%、0.0300%、0.0325%、0.0350%、0.0375%、0.0400%、0.0425%、0.0450%、0.0475%、0.0500%、0.0525%、0.0550%、0.0575%、0.0600%、0.0625%、0.0650%、0.0675%、0.0700%、0.0725%、0.0750%、0.0775%、0.0800%、0.0825%、0.0850%、0.0875%、0.0900%、0.0925%、0.0950%、0.0975%、0.1000%、0.1250%、0.1500%、0.1750%、0.2000%、0.2250%、0.2500%、0.2750%、0.3000%、0.3250%、0.3500%、0.3750%、0.4000%、0.4250%、0.4500%、0.4750%、0.5000%、0.5250%、0.0550%、0.5750%、0.6000%、0.6250%、0.6500%、0.6750%、0.7000%、0.7250%、0.7500%、0.7750%、0.8000%、0.8250%、0.8500%、0.8750%、0.9000%、0.9250%、0.9500%、0.9750%、1.0%、1.1%、1.2%、1.3%、1.4%、1.5%、1.6%、1.7%、1.8%、1.9%、2.0%、2.1%、2.2%、2.3%、2.4%、2.5%、2.6%、2.7%、2.8%、2.9%、3.0%、3.1%、3.2%、3.3%、3.4%、3.5%、3.6%、3.7%、3.8%、3.9%、4.0%、4.1%、4.2%、4.3%、4.4%、4.5%、4.6%、4.7%、4.8%、4.9%、5.0%、5.1%、5.2%、5.3%、5.4%、5.5%、5.6%、5.7%、5.8%、5.9%、6.0%、6.1%、6.2%、6.3%、6.4%、6.5%、6.6%、6.7%、6.8%、6.9%、7.0%、7.1%、7.2%、7.3%、7.4%、7.5%、7.6%、7.7%、7.8%、7.9%、8.0%、8.1%、8.2%、8.3%、8.4%、8.5%、8.6%、8.7%、8.8%、8.9%、9.0%、9.1%、9.2%、9.3%、9.4%、9.5%、9.6%、9.7%、9.8%、9.9%、10%、11%、12%、13%、14%、15%、16%、17%、18%、19%、20%、21%、22%、23%、24%、25%、26%、27%、28%、29%、30%、35%、40%、45%、50%、60%、65%、70%、75%、80%、85%、90%、95%或99%或其中可得到的任何范围的在本说明书和权利要求通篇所提及的成分中的至少一种。在非限制性方面,该百分比可以按整个组合物的重量或体积进行计算。本领域普通技术人员会理解,给定组合物中的浓度可以根据成分的添加、替换和/或减少而改变。
D.载剂
本文公开的组合物可以并入到所有类型的载剂中。非限制性实例包括乳液(例如,油包水、水包油包水、水包油、水包硅酮、硅酮包水、油包水包油、硅酮包水包油型乳液)、乳霜、洗剂、溶液(水溶液或者水-乙醇溶液)、无水赋形剂(例如口红和粉末)、凝胶和软膏。变化方案和其它合适的载剂对于本领域的普通技术人员是明显的,并且适用于本发明。在某些方面,重要的是,以组合化学相容并且不形成从最终产物中沉淀的络合物的方式选择化合物、成分和试剂的浓度和组合。
E.另外的成分
除了本发明人公开的成分的组合之外,组合物还可以包含另外的成分,例如化妆品成分和药物活性成分。这些另外的成分的非限制性实例在以下子章节中进行描述。
1.化妆品成分
CTFA国际化妆品成分词典和手册(2004和2008)描述了多种可以在本发明的情况下使用的非限制性化妆品成分。这些成分种类的实例包括:芳香剂(人造的和天然的)、染料和着色成分(例如蓝色1号、蓝色1号色淀、红色40号、二氧化钛、D&C蓝色4号、D&C绿色5号、D&C橙色4号、D&C红色17号、D&C红色33号、D&C紫色2号、D&C黄色10号和D&C黄色11号)、吸附剂、润滑剂、溶剂、保湿剂(包括例如润肤剂、湿润剂、成膜剂、闭塞剂和影响皮肤天然保湿机制的试剂)、拒水剂、紫外吸收剂(物理和化学吸收剂,例如对-氨基苯甲酸(“PABA”)和相应的PABA衍生物、二氧化钛、氧化锌等)、精油、维生素(例如A、B、C、D、E和K)、微量金属(例如锌、钙和硒)、抗刺激物(例如类固醇和非类固醇类抗炎药)、植物提取物(例如芦荟、柑橘、黄瓜提取物、银杏、人参和迷迭香)、抗菌剂、抗氧化剂(例如BHT和生育酚)、螯合剂(例如乙二胺四乙酸二钠和乙二胺四乙酸四钠)、防腐剂(例如对羟基苯甲酸甲酯和对羟基苯甲酸丙酯)、pH调节剂(例如氢氧化钠和柠檬酸)、吸收剂(例如淀粉辛烯琥珀酸铝、高岭土、玉米淀粉、燕麦淀粉、环糊精、滑石和沸石)、皮肤漂白和光亮剂(例如氢醌和烟酰胺乳酸酯)、湿润剂(例如山梨醇、脲、甲基葡糖醇聚醚-20和甘露醇)、去角质成分、防水剂(例如氢氧化钠镁/铝硬脂酸盐)、皮肤调节剂(例如芦荟提取物、尿囊素、没药醇、神经酰胺、聚二甲基硅氧烷、透明质酸、生物糖胶-1、乙基己基甘油、戊二醇、氢化聚癸烯、辛基十二醇油酸酯和甘草酸二钾)。这些成分中一些的非限制性实例在以下子章节中提供。
a.紫外吸收剂
可以与本文公开的组合物组合使用的紫外吸收剂包括化学和物理防晒物质。可以使用的化学防晒物质的非限制性实例包括对氨基苯甲酸(PABA)、PABA酯(PABA甘油酯、戊基二甲醇PABA酯和辛基二甲醇PABA酯)、PABA丁酯、PABA乙酯、乙基二羟基丙醇PABA酯、二苯甲酮(氧苯酮、磺异苯酮、二苯甲酮和二苯甲酮-1到12)、肉桂酸盐/酯(甲氧基肉桂酸辛酯、对甲氧基肉桂酸异戊酯、辛基甲氧基肉桂酸酯、西诺沙酯、二异丙基肉桂酸甲酯、甲氧基肉桂酸DEA盐、二异丙基肉桂酸乙酯、甘油辛酸酯二甲氧基肉桂酸酯和甲氧基肉桂酸乙酯)、肉桂酸酯、水杨酸酯(均甲基水杨酸酯、水杨酸苄酯、乙二醇水杨酸酯、异丙基苄醇水杨酸酯等)、邻氨基苯甲酸盐/酯、尿刊酸乙酯、原膜散酯、水杨酸辛酯、二苯甲酰基甲烷衍生物(例如阿伏苯宗)、奥克立林、辛基三嗪酮、棓酰棓酸三油酸酯、氨基苯甲酸甘油酯、2-羟基-1,4-萘醌和二羟基丙酮、乙基己基三嗪酮、二辛基丁酰胺基三嗪酮、苯亚甲基丙二酸脂聚二甲基硅氧烷、对苯二亚甲基二莰酮磺酸、苯基二苯并咪唑四磺酸酯二钠、二乙氨基羟基苯甲酰基苯甲酸己酯、双二乙氨基羟基苯甲酰基苯甲酸酯、双苯并恶唑基苯基乙基己基亚氨基三嗪、甲酚曲唑三硅氧烷、亚甲基双苯并三唑基四甲基丁基苯酚和双乙基己基氧苯酚甲氧苯基三嗪、4-甲基苯亚甲基莰酮和4-甲氧基肉桂酸异戊酯。物理防晒物质的非限制性实例包括高岭土、滑石、凡士林和金属氧化物(例如二氧化钛和氧化锌)。
b.保湿剂
可以与本文公开的组合物一起使用的保湿剂的非限制性实例包括氨基酸、硫酸软骨素、双甘油、赤藓糖醇、果糖、葡萄糖、甘油、甘油聚合物、乙二醇、1,2,6-己三醇、蜂蜜、透明质酸、氢化蜂蜜、氢化淀粉水解物、肌醇、乳糖醇、麦芽糖醇、麦芽糖、甘露醇、天然保湿因子、PEG-15丁二醇、聚甘油山梨醇、吡咯烷酮羧酸的盐、PCA钾、丙二醇、葡糖醛酸钠、PCA钠、山梨醇、蔗糖、海藻糖、脲和木糖醇。
其它实例包括乙酰化羊毛脂、乙酰化羊毛脂醇、丙氨酸、藻类提取物、翠叶芦荟、翠叶芦荟提取物、翠叶芦荟凝胶、药蜀葵提取物、杏(prunus armeniaca)仁油、精氨酸、精氨酸天冬氨酸盐/酯、山金车提取物、天冬氨酸、鳄梨(persea gratissima)油、屏障鞘脂、丁醇、蜂蜡、山萮醇、β-谷甾醇、白桦(betula alba)树皮提取物、琉璃苣(Borago officinalis)提取物、假叶树(ruscus aculeatus)提取物、丁二醇、金盏花提取物、金盏花油、小烛树(euphorbia cerifera)蜡、菜籽油、辛酸/癸酸甘油三酯、豆蔻(elettaria cardamomum)油、巴西棕榈(copernicia erifera)蜡、胡萝卜(daucus carota sativa)油、蓖麻(ricinuscommunis)油、神经酰胺、地蜡、十六/十八醇聚氧乙烯(5)醚、十六/十八醇聚氧乙烯(12)醚、十六/十八醇聚氧乙烯(20)醚、鲸蜡硬脂醇辛酸酯、十六醇聚氧乙烯(20)醚、十六醇聚氧乙烯(24)醚、鲸蜡醇乙酸酯、鲸蜡醇辛酸酯、鲸蜡醇棕榈酸酯、洋甘菊(anthemis nobilis)油、胆固醇、胆固醇酯、胆甾醇羟基硬脂酸酯、柠檬酸、鼠尾草(salvia sclarea)油、可可(theobroma cacao)脂、椰油醇-辛酸酯/癸酸酯、椰子(cocos nucifera)油、胶原蛋白、胶原蛋白氨基酸、玉米(zea mays)油、脂肪酸、癸基油酸酯、聚二甲基硅氧烷共聚醇、聚二甲基硅氧烷醇、己二酸二辛酯、琥珀酸二辛酯、二聚季戊四醇六辛酸酯/六癸酸酯、DNA、赤藓糖醇、乙氧基二乙二醇、亚油酸乙酯、蓝桉油、月见草(oenothera biennis)油、脂肪酸、斑点老鹳草油、葡萄糖胺、葡糖谷氨酸酯、谷氨酸、甘油聚氧乙烯(26)醚、甘油、丙三醇、二硬脂酸甘油酯、羟基硬脂酸甘油酯、月桂酸甘油酯、亚油酸甘油酯、豆蔻酸甘油酯、油酸甘油酯、硬脂酸甘油酯、硬脂酸甘油酯SE、甘氨酸、乙二醇硬酯酸酯、乙二醇硬酯酸酯SE、葡糖氨基葡聚糖、葡萄(vitis vinifera)籽油、榛子(corylus americana)坚果油、己二醇、透明质酸、红花(carthamus tinctorius)油、氢化蓖麻油、氢化椰油酸甘油酯、氢化椰子油、氢化羊毛脂、氢化卵磷脂、氢化棕榈油甘油酯、氢化棕榈仁油、氢化大豆油、氢化牛脂酸甘油酯、氢化植物油、水解胶原蛋白、水解弹性蛋白、水解葡糖氨基葡聚糖、水解角蛋白、水解大豆蛋白、羟基化羊毛脂、羟基脯氨酸、硬脂酸异鲸蜡醇酯、异鲸蜡醇硬脂酰基硬脂酸酯、油酸异癸酯、异硬脂酸异丙酯、羊毛脂酸异丙酯、肉豆蔻酸异丙酯、棕榈酸异丙酯、硬脂酸异丙酯、异硬脂酰胺DEA、异硬脂酸、异硬脂醇乳酸酯、异硬脂醇新戊酸酯、茉莉(jasminum officinale)油、霍霍巴(buxus chinensis)油、巨藻、石栗(aleurites moluccana)坚果油、乳酰胺MEA、羊毛脂醇聚氧乙烯(16)醚、羊毛脂醇聚氧乙烯(10)醚乙酸酯、羊毛脂、羊毛脂酸、羊毛脂醇、羊毛脂油、羊毛脂蜡、薰衣草(lavandula angustifolia)油、卵磷脂、柠檬(citrus medicalimonum)油、亚油酸、亚麻酸、澳洲坚果油、麦芽糖醇、母菊(chamomilla recutita)油、甲基葡糖倍半硬脂酸酯、甲基硅烷醇PCA、矿物油、貂油、被孢霉油、肉豆蔻醇乳酸酯、肉豆蔻醇肉豆蔻酸酯、肉豆蔻醇丙酸酯、新戊二醇二辛酸酯/二癸酸酯、辛基月桂醇、辛基月桂醇肉豆蔻酸酯、辛基月桂醇硬脂酰基硬脂酸酯、羟基硬脂酸辛酯、棕榈酸辛酯、水杨酸辛酯、硬脂酸辛酯、油酸、橄榄(olea europaea)油、橙(citrus aurantium dulcis)油、棕榈(elaeisguineensis)油、棕榈酸、泛硫乙胺、泛醇、泛醇基乙基醚、石蜡、PCA、桃(prunus persica)仁油、花生(arachis hypogaea)油、PEG-8C12-18酯、PEG-15椰油烷基胺、PEG-150二硬脂酸酯、PEG-60甘油异硬脂酸酯、PEG-5甘油硬脂酸酯、PEG-30甘油硬脂酸酯、PEG-7氢化蓖麻油、PEG-40氢化蓖麻油、PEG-60氢化蓖麻油、PEG-20甲基葡糖倍半硬脂酸酯、PEG40失水山梨醇全油酸酯、PEG-5大豆甾醇、PEG-10大豆甾醇、PEG-2硬脂酸酯、PEG-8硬脂酸酯、PEG-20硬脂酸酯、PEG-32硬脂酸酯、PEG-40硬脂酸酯、PEG-50硬脂酸酯、PEG-100硬脂酸酯、PEG-150硬脂酸酯、十五内酯、薄荷(mentha piperita)油、凡士林、磷脂、多氨基酸多糖缩合物、聚甘油-3二异硬脂酸酯、聚季铵盐-24、聚山梨醇酯20、聚山梨醇酯40、聚山梨醇酯60、聚山梨醇酯80、聚山梨醇酯85、肉豆蔻酸钾、棕榈酸钾、丙二醇、丙二醇二辛酸酯/二癸酸酯、丙二醇二辛酸酯、丙二醇二壬酸酯、丙二醇月桂酸酯、丙二醇硬脂酸酯、丙二醇硬脂酸酯SE、PVP、吡哆醇二棕榈酸酯、视黄醇、视黄醇棕榈酸酯、米(oryza sativa)糠油、RNA、迷迭香(rosmarinusofficinalis)油、玫瑰油、红花(carthamus tinctorius)油、鼠尾草(salvia officinalis)油、檀香(santalum album)油、丝氨酸、血清蛋白、芝麻(sesamum indicum)油、牛油果(butyrospermum)脂、蚕丝粉、软骨素硫酸钠、透明质酸钠、乳酸钠、棕榈酸钠、PCA钠、聚谷氨酸钠、可溶胶原、失水山梨醇月桂酸酯、失水山梨醇油酸酯、失水山梨醇棕榈酸酯、失水山梨醇倍半油酸酯、失水山梨醇硬脂酸酯、山梨醇、大豆(glycine soja)油、鞘脂、角鲨烷、角角鲨烷、硬脂酰胺MEA-硬脂酸酯、硬脂酸、硬脂氧基聚二甲基硅氧烷、硬脂氧基三甲基硅烷、硬脂醇、硬脂醇甘草亭酸酯、硬脂醇庚酸酯、硬脂醇硬脂酸酯、向日葵(helianthus annuus)籽油、甜杏仁(prunus amygdalus dulcis)油、合成蜂蜡、生育酚、乙酸生育酚酯、生育酚亚油酸酯、三山嵛精、十三烷醇新戊酸酯、十三烷醇硬脂酸酯、三乙醇胺、三硬脂酸精、脲、植物油、水、蜡、小麦(triticum vulgare)胚芽油和依兰(cananga odorata)油。
c.抗氧化剂
可以与本文公开的组合物一起使用的抗氧化剂的非限制性实例包括乙酰半胱氨酸、抗坏血酸多肽、抗坏血酸二棕榈酸酯、抗坏血酸甲基硅烷醇果胶酸酯、抗坏血酸棕榈酸酯、抗坏血酸硬脂酸酯、BHA、BHT、叔丁基氢醌、半胱氨酸、半胱氨酸HCI、二戊基氢醌、二叔丁基氢醌、二鲸蜡醇硫代二丙酸酯、二油基生育酚甲基硅烷醇、抗坏血酸硫酸酯二钠、二硬脂醇硫代二丙酸酯、双十三烷醇硫代二丙酸酯、没食子酸月桂酯、异抗坏血酸、抗坏血酸酯、阿魏酸乙酯、阿魏酸、没食子酸酯、氢醌、巯基乙酸异辛酯、曲酸、抗坏血酸镁、抗坏血酸磷酸酯镁、甲基硅烷醇抗坏血酸酯、天然植物抗氧化剂例如绿茶或葡萄籽提取物、去甲二氢愈创木酸、没食子酸辛酯、苯巯基乙酸、磷酸抗坏血酸酯生育酚酯钾、亚硫酸钾、没食子酸丙酯、醌、迷迭香酸、抗坏血酸钠、亚硫酸氢钠、异抗坏血酸钠、偏亚硫酸氢钠、亚硫酸钠、超氧化物歧化酶、巯基乙酸钠、山梨醇缩糠醛、硫二甘醇、亚硫基二乙酰胺、硫二乙酸、巯基乙酸、硫代乳酸、硫代水杨酸、生育酚聚氧乙烯醚-5、生育酚聚氧乙烯醚-10、生育酚聚氧乙烯醚-12、生育酚聚氧乙烯醚-18、生育酚聚氧乙烯醚-50、生育酚、托可索伦、乙酸生育酚酯、生育酚亚油酸酯、生育酚烟酸酯、生育酚琥珀酸酯和三(壬基酚)亚磷酸酯。
d.结构化剂
在其它非限制性方面,本文公开的组合物可以包含结构化剂。在某些方面,结构化剂帮助给组合物提供流变学特征以有助于组合物的稳定性。在其它方面,结构化剂还可以起乳化剂或表面活性剂的作用。结构化剂的非限制性实例包括硬脂酸、棕榈酸、硬脂醇、鲸蜡醇、山嵛醇、硬脂酸、棕榈酸、具有平均约1到约21个亚乙基氧单元的硬脂醇的聚乙二醇醚、具有平均约1到约5个亚乙基氧单元的鲸蜡醇的聚乙二醇醚及其混合物。
e.乳化剂
在本发明的一些方面,组合物不包含乳化剂。然而,在其它方面,组合物可以包含一种或更多种乳化剂。乳化剂可以降低相间表面张力并改善乳液的剂型和稳定性。乳化剂可以是非离子的、阳离子的、阴离子的和两性离子的乳化剂(参见McCutcheon's(1986);美国专利5,011,681号;4,421,769号;3,755,560号)。非限制性实例包括甘油酯、丙二醇酯、丙二醇的脂肪酸酯、聚丙二醇的脂肪酸酯、山梨醇的酯、失水山梨醇酐酯、羧酸共聚物、葡萄糖的酯和醚、乙氧基化的酯、乙氧基化的醇、磷酸烷基酯、聚氧乙烯脂肪醚磷酸酯、脂肪酸酰胺、酰基乳酸酯、脂肪酸盐、TEA硬脂酸酯、DEA油醇聚氧乙烯醚-3磷酸酯、聚乙二醇20失水山梨醇单月桂酸酯(聚山梨醇酯20)、聚乙二醇5大豆甾醇、硬脂醇聚氧乙烯醚-2、硬脂醇聚氧乙烯醚-20、硬脂醇聚氧乙烯醚-21、鲸蜡硬脂醇聚氧乙烯醚-20、鲸蜡硬脂基葡糖苷、鲸蜡硬脂醇、C12-C13链烷醇聚醚-3、PPG-2甲基葡萄糖醚二硬脂酸酯、PPG-5-鲸蜡醇聚醚-20、双-PEG/PPG-20/20聚二甲基硅氧烷、鲸蜡醇聚氧乙烯醚-10、聚山梨醇酯80、鲸蜡醇磷酸酯、鲸蜡醇磷酸酯钾、二乙醇胺鲸蜡醇磷酸酯、聚山梨醇酯60、甘油硬脂酸酯、PEG-100硬脂酸酯、花生醇、花生基葡糖苷及其混合物。
f.含硅酮的化合物
在非限制性方面,含硅酮的化合物包括分子主链由交替的硅和氧原子与连接在硅原子上的侧基组成的聚合产物家族中的任何成员。通过改变-Si-O-链的长度、侧基和交联,硅酮可以合成为各种各样的材料。它们的稠度可以从液体到凝胶到固体改变。
可以在本发明的环境下使用的含硅酮的化合物包括在本说明书中所描述的或本领域普通技术人员已知的那些。非限制性实例包括硅油(例如挥发性和非挥发性油)、凝胶和固体。在特定的方面,含硅酮的化合物包括硅油,例如聚有机硅氧烷。聚有机硅氧烷的非限制性实例包括聚二甲基硅氧烷、环聚二甲基硅氧烷、聚硅氧烷-11、苯基聚三甲基硅氧烷、聚三甲基硅氨基二甲基硅氧烷、硬脂氧基三甲基硅烷或它们的混合物和其它任何给定比例的有机硅氧烷材料,以根据预期的应用(举例来说,对特定区域例如皮肤、毛发或眼睛)达到期望的稠度和应用特征。“挥发性硅油”包括具有低气化热的硅油,例如通常低于约50卡每克硅油。挥发性硅油的非限制性实例包括:环聚二甲基硅氧烷,例如道康宁344流体、道康宁345流体、道康宁244流体和道康宁245流体、挥发硅7207(康涅狄格州,丹伯里,联合碳化物公司);低黏度聚二甲基硅氧烷,例如黏度大约为50cst或更低的聚二甲基硅氧烷(举例来说,聚二甲基硅氧烷,例如道康宁200-0.5cst流体)。Dow Corning Fluid可以从密歇根州米德兰的Dow Corning Corporation购得。在CTFA化妆品成分词典的第三版中(通过引用并入),环聚二甲基硅氧烷和聚二甲基硅氧烷分别被描述为环状聚二甲基硅氧烷化合物和用三甲基硅氧基单元封端的完全甲基化的线性硅氧烷混合物。可以在本发明的环境下使用的其它非限制性挥发性硅油包括从纽约州沃特福德的General Electric Co.,SiliconeProducts Div.和密歇根州艾德里安的SWS Silicones Div.of Stauffer Chemical Co.购得的那些。
g.精油
精油包括来自药草、花朵、树木和其它植物的油。这类油一般以植物细胞间微小的液滴存在,并可以用本领域技术人员已知的数种方法进行提取(例如,蒸气蒸馏、花香提取(例如,使用脂肪提取)、浸渍、溶剂提取或机械压榨)。当这些类型的油暴露于空气时,其易于挥发(例如,挥发性油)。因此,虽然许多精油是无色的,但是随着时间其被氧化并且颜色变得更深。精油不溶于水,但溶于醇、醚、固定油(植物的)和其它有机溶剂。在精油中发现的一般物理特征包括从约160℃到240℃变化的沸点和从约0.759到约1.096的密度。
精油一般通过油被发现的来源植物命名。例如,玫瑰油或薄荷油分别来自玫瑰或薄荷植物。可以在本发明的环境下使用的精油的非限制性实例包括芝麻油、澳洲坚果油、茶树油、月见草油、西班牙鼠尾草油、西班牙迷迭香油、芫荽油、百里香油、众香果油、玫瑰油、大茴香油、凤仙花油、香柠檬油、玫瑰木油、香柏油、甘菊油、鼠尾草油、香紫苏油、丁香油、柏木油、桉油、茴香油、海茴香油、乳香油、香叶油、姜油、葡萄柚油、茉莉油、杜松子油、薰衣草油、柠檬油、柠檬草油、梨莓油、橘子油、甘牛至油、没药油、苦橙花油、橙油、绿叶油、胡椒油、黑胡椒油、苦橙叶油、松油、奥图玫瑰油、迷迭香油、檀香油、绿薄荷油、甘松油、香根草油、冬青油、依兰依兰。还预期本领域技术人员已知的其它精油在本发明的环境下是有用的。
h.增稠剂
包括增稠剂或凝胶剂在内的增稠剂,包括可以增加组合物黏度的物质。增稠剂包括可以增加组合物黏度而基本上不改变组合物内活性成分功效的那些。增稠剂还可以增加本文公开的组合物的稳定性。在本文公开的一些方面,增稠剂包括氢化聚异丁烯、三羟基硬脂精、丙烯酰基二甲基牛磺酸铵/VP共聚物、或它们的混合物。
可以在本发明的环境下使用的另外的增稠剂的非限制性实例包括羧酸聚合物、交联的聚丙烯酸酯聚合物、聚丙烯酰胺聚合物、多糖和胶。羧酸聚合物的实例包括含有一种或更多种衍生自丙烯酸的单体的交联化合物、取代的丙烯酸和这些丙烯酸和取代的丙烯酸的盐和酯,其中所述交联剂含有两个或更多个碳-碳双键,并衍生自多元醇(参见美国专利5,087,445号;4,509,949号;2,798,053号;CTFA国际化妆品成分词典,第四版,1991,第12和80页)。市售羧酸聚合物的实例包括卡波姆,其为丙烯酸与蔗糖或季戊四醇的烯丙基醚交联的均聚物(例如,购自B.F.Goodrich的CarbopolTM900系列)。
交联的聚丙烯酸酯聚合物的非限制性实例包括阳离子型和非离子型聚合物。在美国专利5,100,660号;4,849,484号;4,835,206号;4,628,078号;4,599,379号中描述了实例。
聚丙烯酰胺聚合物(包括非离子的聚丙烯酰胺聚合物,其包括取代支化的或未支化的聚合物)的非限制性实例包括聚丙烯酰胺、异构烷烃和月桂醇聚氧乙烯(7)醚、丙烯酰胺与被丙烯酸和取代的丙烯酸取代的丙烯酰胺的多嵌段共聚物。
多糖的非限制性实例包括纤维素、羧甲基羟乙基纤维素、乙酸丙酸羧酸纤维素、羟乙基纤维素、羟乙基乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素、甲基羟乙基纤维素、微晶纤维素、纤维素硫酸钠及其混合物。其他实例为烷基取代的纤维素,其中纤维素聚合物的羟基被羟烷基化(优选地羟乙基化或羟丙基化)以形成羟烷基化的纤维素,其然后用C10-C30直链或支链烷基基团通过醚键进行进一步改性。一般这些聚合物为C10-C30直链或支链醇与羟烷基纤维素的醚。其它有用的多糖包括硬葡聚糖类,其包含每三个单元具有一个(1-6)连接的葡萄糖的(1-3)连接的葡萄糖单元的直链。
本发明可以使用的胶的非限制性实例包括阿拉伯树胶、琼脂、藻胶、藻酸、藻酸铵、支化淀粉、藻酸钙、角叉菜胶钙、肉毒碱、角叉菜胶、糊精、明胶、结冷胶、瓜尔豆胶、瓜尔胶羟丙基三甲基氯化铵、锂蒙脱石、透明质酸、水合二氧化硅、羟丙基壳聚糖、羟丙基瓜尔胶、卡拉亚胶、巨藻、角豆胶、纳豆胶、藻酸钾、角叉菜胶钾、藻酸丙二醇酯、菌核胶、羧甲基葡聚糖钠、角叉菜胶钠、黄蓍胶、黄原胶及其混合物。
i.防腐剂
在本发明的环境下可以使用的防腐剂的非限制性实例包括季铵盐防腐剂(例如聚季铵盐-1和苄烷铵卤化物(例如苯扎氯铵(“BAC”)和苯扎溴铵))、尼泊金酯(例如对羟基苯甲酸甲酯和对羟基苯甲酸丙酯)、苯氧基乙醇、苄醇、氯丁醇、苯酚、山梨酸、硫汞撒或其组合。
2.药物成分
还预期药物活性成分对于本文公开的组合物是有用的。药物活性成分的非限制性实例包括抗粉刺剂、用于处理酒渣鼻的试剂、止痛剂、麻醉剂、肛门直肠的、抗组胺药、包括非甾族消炎药在内的消炎剂、抗生素、抗菌剂、抗病毒素、抗微生物剂、抗癌活性物、抗疥螨剂、灭虱剂、抗肿瘤药、防汗药、止痒剂、抗牛皮癣药、抗脂溢剂、生物活性蛋白质和多肽、烧伤处理剂、烧灼剂、脱色剂、脱毛剂、尿布疹处理剂、酶、毛发生长刺激剂、包括DFMO及其盐和类似物在内的毛发生长抑制剂、止血剂、角质分离剂、口疮处理剂、唇疱疹处理剂、牙科或牙周处理剂、光敏感活性物、皮肤保护剂/屏障剂、包括激素和皮质激素的类固醇、晒伤处理剂、遮光剂、经皮活性物、鼻活性物、阴道活性物、疣处理剂、创伤处理剂、创伤愈合剂等。
F.试剂盒
还预期试剂盒用于本发明的特定方面。例如,本文公开的组合物可以被包括在试剂盒内。试剂盒可以包括容器。容器可以包括瓶子、金属管、层压管、塑料管、分配器、高压容器、屏障容器、包装、分室、口红容器、压缩容器、能够保存化妆品组合物的化妆品盘或其它类型的容器,例如注射或吹塑成型的塑料容器,其中保存分散体或组合物或期望的瓶子、分配器或包装。试剂盒和/或容器在其表面可包含标记。举例来说,标记可以是字词、短语、缩写、图片或符号。
所述容器可以分配预定量的组合物。在其他实施方案中,可以挤压容器(例如金属、层压或塑料管)以分配期望量的组合物。组合物可以分配为喷雾、气溶胶、液体、流体或半固体。容器可以具有喷雾、抽吸或挤压机构。试剂盒还可以包含使用试剂盒组分以及使用任何包含于容器内的组合物的说明书。说明书可以包含如何施用、使用和保存组合物的解释。
实施例
以下实施例用来说明本发明的一些实施方案/实例。本领域技术人员应理解,以下实施例中所公开的技术代表本发明人确定的在本发明的实践中发挥良好作用的技术,因此可以认为构成了用于其实施的优选模式。然而,根据本公开,本领域技术人员应理解,在所公开的具体实施方案中可以做出许多改变,并仍然获得相同或相似的结果,而不脱离本发明的精神和范围。
实施例1
制备具有来自实施例1的成分的制剂作为面膜。制备表1、表2和表3中的制剂作为去角质面膜。制备表4中的制剂作为修复或去角质面膜。
表1
成分 | %浓度(以重量计) |
水 | 63.7 |
三乙醇胺 | 8.75 |
羟基乙酸 | 8 |
甘油 | 3 |
丁二醇 | 2 |
海水 | 1.7 |
鲸蜡硬脂醇 | 1.6 |
花生醇 | 1.4 |
异硬脂酸失水山梨醇酯 | 1 |
碳酸二辛酯 | 1 |
生物糖胶-1 | 1 |
二十二醇 | 0.75 |
丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物 | 0.75 |
丙烯酰基二甲基牛磺酸铵/VP共聚物 | 0.7 |
戊二醇 | 0.7 |
二氢茉莉酮酸甲酯 | 0.55 |
异十六烷 | 0.5 |
阿拉伯胶树胶提取物 | 0.4 |
鲸蜡硬脂基葡糖苷 | 0.4 |
癸基葡萄糖苷 | 0.4 |
4-叔丁基环己醇 | 0.3 |
硅酸镁铝 | 0.2 |
聚二甲基硅氧烷 | 0.2 |
巴西酸亚乙酯 | 0.2 |
黄原胶 | 0.15 |
乙基芳樟醇 | 0.15 |
聚山梨醇酯60 | 0.1 |
EDTA二钠 | 0.1 |
二氧化钛 | 0.1 |
浮游生物提取物 | 0.01 |
芦苇提取物 | 0.01 |
茯苓提取物 | 0.01 |
西葫芦(Cucurbita Pepo)籽提取物 | 0.002 |
赋形剂** | 适量 |
**添加赋形剂以改变组合物的流变性能。或者,水的量可以改变,只要组合物中水的量为至少45重量%、优选为50重量%至75重量%即可。
表2
成分 | %浓度(以重量计) |
水 | 72.3 |
三乙醇胺 | 5 |
羟基乙酸 | 4 |
甘油 | 3 |
丁二醇 | 2 |
海水 | 1.7 |
鲸蜡硬脂醇 | 1.6 |
花生醇 | 1.4 |
异硬脂酸失水山梨醇酯 | 1 |
碳酸二辛酯 | 1 |
生物糖胶-1 | 1 |
二十二醇 | 0.75 |
丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物 | 0.3 |
丙烯酰基二甲基牛磺酸铵/VP共聚物 | 0.7 |
戊二醇 | 0.7 |
二氢茉莉酮酸甲酯 | 0.55 |
异十六烷 | 0.2 |
阿拉伯胶树胶提取物 | 0.4 |
鲸蜡硬脂基葡糖苷 | 0.4 |
癸基葡萄糖苷 | 0.4 |
4-叔丁基环己醇 | 0.3 |
硅酸镁铝 | 0.2 |
聚二甲基硅氧烷 | 0.2 |
巴西酸亚乙酯 | 0.2 |
黄原胶 | 0.15 |
乙基芳樟醇 | 0.15 |
EDTA二钠 | 0.1 |
二氧化钛 | 0.1 |
聚山梨醇酯60 | 0.04 |
浮游生物提取物 | 0.01 |
芦苇提取物 | 0.01 |
茯苓提取物 | 0.01 |
西葫芦(Cucurbita Pepo)籽提取物 | 0.002 |
赋形剂** | 适量 |
**添加赋形剂以改变组合物的流变性能。或者,水的量可以改变,只要组合物中水的量为至少60重量%、优选70重量%至80重量%即可。
表3
成分 | %浓度(以重量计) |
水 | 49.4 |
聚硅氧烷-11 | 20 |
环戊硅氧烷 | 9 |
聚二甲基硅氧烷 | 5 |
甘油 | 4 |
PEG-10聚二甲基硅氧烷 | 3 |
丁二醇 | 2 |
双-PEG-18甲基醚二甲基硅烷 | 2 |
苯氧乙醇 | 0.9 |
丙烯酰基二甲基牛磺酸铵/VP共聚物 | 0.7 |
丙二醇 | 0.5 |
生物糖胶-1 | 0.5 |
阿拉伯胶树胶提取物 | 0.4 |
丙烯酸羟乙基/丙烯酰基二甲基牛磺酸钠共聚物 | 0.4 |
角鲨烷 | 0.3 |
癸二醇 | 0.2 |
米赫毛霉提取物 | 0.2 |
柠檬酸钠 | 0.2 |
羟乙基纤维素 | 0.15 |
胭脂仙人掌花提取物和/或水解梨果仙人掌花提取物 | 0.14 |
1,2-己二醇 | 0.12 |
柠檬酸 | 0.11 |
甘草酸二钾 | 0.1 |
乙酸生育酚酯 | 0.1 |
黄原胶 | 0.1 |
羟丙基环糊精 | 0.07 |
芽孢杆菌发酵产物 | 0.07 |
三乙醇胺 | 0.06 |
聚山梨醇酯60 | 0.06 |
EDTA二钠 | 0.05 |
腺苷酸 | 0.04 |
异硬脂酸失水山梨醇酯 | 0.02 |
山梨酸钾 | 0.01 |
糖同分异构体 | 0.01 |
仙人果果提取物(任选) | 0.0005 |
赋形剂** | 适量 |
**添加赋形剂以改变组合物的流变性能。或者,水的量可以改变,只要组合物中水的量为至少重量40%、优选45重量%至65重量%即可。
表4
成分 |
水 |
米赫毛霉提取物 |
芽孢杆菌发酵产物 |
浮游生物提取物 |
水解梨果仙人掌花提取物 |
羟基乙酸(任选) |
赋形剂** |
**添加赋形剂以改变组合物的流变性能。或者,水的量可以改变,只要组合物中水的量为至少15重量%、优选25重量%至85重量%即可。
实施例2
增加在真皮/表皮交界处存在的真皮基质蛋白:
皮肤包含由基质产生的成纤维细胞组成的结缔组织的收缩带、脂肪产生的脂肪细胞和血液网络。结缔组织厚度可以不同且通过为肌肉和器官提供缓冲的纤维网络保持在位。该缓冲或胞外基质主要是由胶原蛋白组成,以帮助皮肤提供支持和基础。当真皮强健且在结构上稳固时,脂肪细胞不能穿透并在皮肤表面上变得可见。申请人已确定,西葫芦籽的提取物可以增加胶原蛋白的产生和抑制降解多种类型的胶原蛋白的酶。Ocaline PF被用在实施例的组合物中。
胶原蛋白是结缔组织中最主要的蛋白。它是由成纤维细胞分泌,通过其它蛋白质熟化。与未经处理的对照组相比,西葫芦籽的提取物使由人类成纤维细胞分泌的I型胶原蛋白的产生增加了41.6%。
基质蛋白通过被称为基质金属蛋白酶(MMP)即一组依赖锌的酶(内肽酶)的酶在结缔组织中降解。MMP基本上不在皮肤中表达但是它们的活性可以被调节。这些酶以特定的方式降解胞外基质;不同的MMP降解特定的基质蛋白。在皮肤中发现的许多胶原蛋白(胶原蛋白I、III、IV和VII)是MMP-3(溶基质素1)的靶标。酶的活性的抑制防止对于皮肤的结构基础来说是必不可少的基质蛋白的破坏。西葫芦籽的提取物抑制>90%的来自纯化的MMP-3酶的活性。
实施例3
(附加分析)
可以通过本领域普通技术人员已知的方法来确定可用于确定说明书和权利要求书全文所公开的成分、或成分的任意组合或具有所述成分的组合的组合物的任一种的功效。以下是可以在本发明的情况下使用的非限制性。应认识到,可以使用其它测试过程,包括例如客观的和主观的过程。
B16色素沉着分析:黑素生成是黑素细胞产生黑色素的过程,黑色素是一种天然产生的给予皮肤、毛发和眼睛颜色的色素。抑制黑素生成有益于预防皮肤变黑和减轻与老化有关的黑斑。该生物分析采用B16-F1黑素细胞(ATCC),一种永生化的小鼠黑色素瘤细胞系,来分析化合物对黑素生产的效果。该分析的终点是黑色素产生和细胞活性的分光光度测量。可以在10%CO2中,在37℃下在具有10%的胎牛血清(Mediatech)的标准DMEM生长培养基中培养B16-F1黑素细胞,然后用本说明书中所公开活性成分、成分的组合或具有所述组合的组合物中的任一种处理。培育之后,通过在405nm处的吸收测量黑色素分泌,定量细胞活性。
胶原蛋白刺激分析:胶原蛋白是对皮肤结构关键的一种细胞外基质蛋白。增加的胶原蛋白合成帮助改善皮肤坚实度和弹性。该生物分析可以用来检测本说明书中所公开活性成分、成分的组合或具有所述组合的组合物中的任一个对人类表皮纤维母细胞产生前胶原肽(胶原蛋白的前体)的影响。该分析的终点是反映前胶原肽的存在和细胞活性的分光光度测量。该分析采用定量的夹心酶免疫分析技术,因此对前胶原肽特异的单克隆抗体预先涂覆在微孔板上。可以将标准品和样品移液到孔中,存在的所有前胶原肽由固定化的抗体结合。冲走所有未结合的物质后,将对前胶原肽特异的酶联多克隆抗体添加到孔。冲洗以去除所有未结合的抗体-酶反应物之后,可以将底物溶液添加到孔,显色与最初步骤中结合的前胶原肽的量成比例,使用酶标仪在450nm处检测,。可以停止显色,并测量颜色的强度。可以将在37℃下10%的CO2中利用10%的胎牛血清(Mediatech)在标准DMEM生长培养基中培养的亚融合正常人类成熟表皮成纤维母细胞(Cascade Biologics)用本说明书中所公开的成分的组合或具有所述组合的组合物的每一种处理3天。培养之后,可以收集细胞培养基,并可以使用Takara的夹心酶联免疫吸附分析(ELISA)(#MK101)定量前胶原肽分泌的量。
肿瘤坏死因子-α(TNF-α)分析:TNF超家族的原型配体即TNF-α是一种在炎症中起主要作用的多效细胞因子。其表达的增加与促炎活性上调有关。该生物分析可以用来检测本说明书中所公开的活性成分、成分的组合或具有所述组合的组合物中的任一种对人类表皮角化细胞产生TNF-α的影响。该分析的终点可能是反映TNF-α的存在和细胞活性的分光光度测量。该分析采用定量的夹心酶免疫分析技术,因此已经将对TNF-α特异的单克隆抗体预先涂覆在微孔板上。可以将标准品和样品移液到孔中,存在的所有TNF-α由固定化的抗体结合。在冲走所有未结合的物质后,可以将对TNF-α特异性的酶联多克隆抗体添加到孔。在冲洗去除所有未结合的抗体-酶反应物之后,可以将底物溶液添加到孔,显色与最初步骤中结合的TNF-α的量成比例,使用酶标仪在450nm处检测。可以停止显色,并测量颜色的强度。可以用佛波醇-12-豆蔻酸酯-13-乙酸酯(PMA,10ng/ml,Sigma Chemical,#P1585-1MG)和本说明书中所公开的活性成分、成分的组合或具有所述组合的组合物的任一种对在5%CO2中在37℃下在EpiLife标准生长培养基(Cascade Biologics)中培养的亚融合的正常人类成熟角质细胞(Cascade Biologics)进行处理6小时。已经表明PMA导致TNF-α分泌明显的增加,所述TNF-α分泌在处理6小时后达到峰值。培育之后,可以收集细胞培养基,并使用来自R&DSystems(#DTA00C)的夹心酶联免疫吸附分析(ELISA)定量TNF-α分泌的量。
抗氧化(AO)分析:体外生物分析测量本说明中所公开的成分、成分的组合或具有所述组合的组合物中的任一种的总抗氧化能力。所述分析依赖样品中抗氧化剂的能力抑制(2,2'-联氮-双-[3-乙基苯并噻唑啉磺酸盐])被正铁肌红蛋白氧化成生物体的抗氧化系统包含酶,例如超氧化物歧化酶、过氧化氢酶和谷胱甘肽过氧化物酶;高分子,例如白蛋白、血浆铜蓝蛋白和铁蛋白;和大量小分子,包括抗坏血酸、α-生育酚、β-胡萝卜素、还原型谷胱甘肽、尿酸和胆红素。內源的源自食物的抗氧化剂的总和表示细胞外液的总抗氧化能力。所有不同抗氧化剂的协作提供比单独的任何单个化合物更强的对抗反应性氧或氮自由基侵袭的保护。因此,总的抗氧化能力与测量单独组分获得的相比可以给出更相关的生物信息,因为其考虑了血浆和体液中存在的所有抗氧化剂的累积效应。样品中抗氧化剂预防ABTS氧化的能力与Trolox即一种水溶性生育酚类似物的能力进行比较,并以Trolox的摩尔当量进行定量。可以使用来自Cayman Chemical(密歇根州安阿伯,USA)的抗氧化能力试剂盒#709001作为测量本说明中所公开的成分、成分的组合或具有所述组合的组合物中的任一种的总抗氧化能力的体外生物分析。方案可以根据制造商的建议进行。所述分析依赖样品中的抗氧化剂来抑制(2,2'-联氮-双-[3-乙基苯并噻唑啉磺酸盐])被正铁肌红蛋白氧化成可以将样品中抗氧化剂预防ABTS氧化的能力与Trolox即一种水溶性生育酚类似物的能力进行比较,并以Trolox的摩尔当量进行定量。
ORAC分析:本说明书中公开的活性成分、成分的组合或具有所述组合的组合物的任一种的氧自由基吸收(或吸收率)能力(ORAC)还可以通过测量这类成分或组合物的抗氧化活性进行分析。该分析可以定量抑制氧化剂,例如已知导致损害细胞(例如皮肤细胞)的氧自由基,的活动的程度及所用时间。本说明书中公开的活性成分、成分的组合或具有所述组合的组合物的任一种的ORAC值可以通过本领域普通技术人员已知的方法进行确定(参见U.S.公开号2004/0109905和2005/0163880;Cao等人(1993),其全部内容通过引用并入)。总之,Cao等人(1993)描述的分析测量了抗氧化化合物在测试材料中抑制氢过氧自由基生成物AAPH引起的B-藻红蛋白荧光(B-PE)下降的能力。
蘑菇酪氨酸酶活性分析:在哺乳动物细胞中,酪氨酸酶在来自酪氨酸(和来自多巴色素聚合)的黑色素生物合成中催化两个步骤。酪氨酸酶位于黑素细胞中,并产生赋予皮肤、毛发和眼睛颜色的黑色素(芳香醌化合物)。可以将蘑菇络氨酸酶(Sigma)在本说明书所公开的活性成分的每一个、成分的组合或具有所述组合的组合中的任一种存在下或不存在下利用其底物L-Dopa(Fisher)培养。可以在490nm处通过比色板读数来评估色素形成。蘑菇络氨酸酶活性的抑制百分比可以通过与未处理的对照相比较来计算,以确定测试成分或其组合抑制纯化的酶的活性的能力。试验提取物的抑制与曲酸(Sigma)的抑制进行比较。
基质金属蛋白酶活性(MMP3;MMP9)分析:体外的基质金属蛋白酶(MMP)抑制分析。MMP是胞外蛋白酶,其凭借宽的底物特异性在许多正常的和疾病状态起作用。MMP3底物包括胶原蛋白、纤维粘连蛋白和层粘连蛋白;而MMP9底物包括胶原蛋白VII、纤维粘连蛋白和层粘连蛋白。使用来自BioMol International的用于MMP3(AK-400)和MMP-9(AK-410)的Colorimetric Drug Discovery试剂盒,该分析设计用于测量MMP的蛋白酶活性,使用含硫多肽作为显色底物(Ac-PLG-[2-巯基-4-甲基-戊酰基]-LG-OC2H5)5,6。MMP裂解位点的肽键由含硫多肽中的硫酯键替代。该键被MMP水解产生巯基,其与DTNB[5,5'-二硫代双(2-硝基苯甲酸),埃尔曼试剂]反应生成2-硝基-5-硫代苯甲酸,可以通过其在412nm处的吸光度进行检测(在pH 6.0和高于7时,ε=13600M-1cm-1)。可以分析本说明书中公开的活性成分、成分的组合或具有所述组合的组合物中的任一种。
环氧合酶(COX)分析:体外环氧合酶-1和-2(COX-1、-2)抑制分析。COX是一种展现环氧合酶和过氧化物酶两者活性的双功能酶。环氧合酶活性将花生四烯酸转换为过氧化氢内过氧化物(前列腺素G2;PGG2),过氧化物酶组分将内过氧化物(前列腺素H2;PGH2)还原为相应的醇,前列腺素、凝血噁烷和环前列腺素的前体。该COX抑制筛选分析测量环氧合酶的过氧化物酶组分。过氧化物酶活性通过监测氧化的N,N,N',N'-四甲基-对苯二胺(TMPD)的出现进行比色分析。该抑制筛选分析包括COX-1和COX-2酶两者,以筛选同工酶特异性抑制剂。可以使用比色COX(绵羊)抑制剂筛选分析(#760111,Cayman Chemical)来分析本说明书中所公开的活性成分的每一种、成分的组合、或具有所述组合的组合物对纯化的环氧合酶(COX-1或COX-2)的影响。根据制造商的使用说明,纯净的酶、血红素和试验提取物可以在分析缓冲液中混合,并在室温下摇动培育15分钟。培育之后,可以加入花生四烯酸和比色底物以启动反应。可以在590nm下通过比色板读数来评估颜色进展。COX-1或COX-2活性的抑制百分比可以通过与未处理的对照物比较进行计算,以确定试验提取物抑制纯净酶活性的能力。
脂肪氧合酶(LO)分析:体外的脂肪氧合酶抑制分析。LO是非血红素的含铁的加双氧酶,其催化分子氧加成到脂肪酸。亚油酸盐/酯和花生四烯酸盐/酯是植物中和动物中LO的主要底物。然后,花生四烯酸可以转换为羟基二十三烯(HETE)酸衍生物,其随后转换为白三烯,有效的炎症介质。该分析通过测量利用花生四烯酸培养的脂肪氧合酶(5-、12-或15-LO)产生的氢过氧化物提供一种精确的和方便的用于筛选脂肪氧合酶抑制剂的方法。可以使用比色LO抑制剂筛选试剂盒(#760700,Cayman Chemical)来确定本说明书中所公开的活性成分的每一种、成分的组合、或具有所述组合的组合物的任一种抑制酶活性的能力。可以将经纯化的15-脂肪氧合酶和测试成分在分析缓冲液中混合,并在室温下摇动培育10分钟。培育之后,可以加入花生四烯酸开始反应,混合物在室温下再培育另外10分钟。可以添加比色底物以终止催化,并在490nm下通过荧光板读数来评估颜色进展。可以与未处理的对照相比较来评估脂肪氧合酶活性的抑制百分比,以确定本说明书中所公开的活性成分的每一种、成分的组合、或具有所述组合的组合物的任一种抑制纯化酶的活性的能力。
弹性蛋白酶分析:可以使用Molecular Probes(俄勒冈州尤金,USA)的弹性蛋白酶分析(试剂盒#E-12056)作为用于测量本说明书中所公开的活性成分的每一种、成分的组合或具有所述组合的组合物的任一种的弹性蛋白酶活性抑制的体外酶抑制分析。EnzChek试剂盒含有可溶的牛颈韧带弹性蛋白,其可以用染料标记以使共轭荧光能够被淬灭。非荧光的底物可以被弹性蛋白酶或其他蛋白酶消化以产生高荧光的片段。产生的荧光增强可以用荧光微孔板测定仪进行监测。来自弹性蛋白底物的消化产物在约505nm处具有吸收最大值,在约515nm处具有荧光发射最大值。当使用EnzChek弹性蛋白酶分析试剂盒以筛选弹性蛋白酶抑制剂时,可以将肽、氯甲基酮用作选择性的、共同的弹性蛋白酶抑制剂。
油控制分析:用于测量皮脂腺中皮脂分泌的减少和/或皮脂腺中皮脂产生的减少的分析可以通过使用本领域普通技术人员已知的标准技术进行分析。在具体的例子中,可以使用前额。可以将本说明书中所公开的活性成分的每一种、成分的组合或具有所述组合的组合物的任一种每天一次或两次地施用到前额的一部分一段固定的日子(例如1、2、3、4、5、6、7、8、9、10、11、12、13、14或更多天),而前额的其他部分不用所述组合物处理。在一段固定的日子期满后,皮脂分泌可以通过将细吸墨纸施用到处理过的和未处理的前额皮肤上进行分析。这是通过首先用湿的和干的布从处理过的和未处理的区域去除所有皮脂完成的。然后吸墨纸施用到处理过的和未处理的前额区域,可以绕着前额放置橡皮筋以轻轻地将吸墨纸压到皮肤上。2小时后,吸墨纸可以移去,使其干燥,然后进行透照。越深的吸墨纸对应于越多的皮脂分泌(或较浅的吸墨纸对应于减少的皮脂分泌。
红斑分析:测量皮肤发红减少的分析可以使用Minolta Chromometer进行评估。皮肤红斑可以通过在受试者前臂施用0.2%的十二烷基硫酸钠溶液来引发。该区域用封闭的贴片保护24小时。24小时后,除去贴片,可以使用Minolta Chroma Meter的a*值对刺激引发的发红进行评估。a*值测量肤色在红色区域的变化。在读数后,立即用本说明中所公开的活性成分、成分的组合或具有所述组合的组合物中的任一种处理该区域。可以定期进行重复测量以确定制剂减少发红和刺激的能力。
皮肤水分/水合分析:皮肤水分/水合的益处可以通过利用以Nova Dermal PhaseMeter进行的阻抗测量进行测量。阻抗计测量皮肤水分含量的变化。皮肤外层具有不同的电性质。当皮肤干燥时,其导电很差。当其变得更加含水时,产生增加的导电性。因此,皮肤阻抗(与导电性有关)的变化可以用于评价皮肤水合的变化。装置可以根据仪器说明针对每个测试日进行校准。还可以对温度和相对湿度进行标记。对受试者可以进行如下评估:测量前其可以在具有确定湿度(例如30-50%)和温度(例如68-72℃)的室内进行平衡。在脸的每一侧进行三个独立的阻抗测定,并对其进行记录和平均。阻抗计可以使用T5设定,其对施用到脸上每五秒的阻抗值进行平均。变化可以以统计方差和显著性进行报道。根据该方法可以分析本说明书中公开的活性成分的每一种、成分的组合或具有所述组合的组合物中的任一种。
皮肤清透度和雀斑与老年斑减少的分析:皮肤清透度和雀斑与老年斑减少使用Minolta Chromometer进行评价。肤色的变化可以使用Minolta Chroma Meter的a*值进行评估以确定由于产品处理引起刺激的可能性。a*值测量肤色在红色区域的变化。这用来确定本说明中所公开的活性成分的每一种、成分的组合或具有所述组合的组合物中的任一种是否引起刺激。测量可以在脸的每一侧进行并进行平均,作为左边和右边脸的值。皮肤清透度也可以使用Minolta Meter进行测量。测量是Minolta Meter的a*、b、和L值的组合,并与皮肤的亮度有关,而且非常好的对应皮肤的光滑度和水合。皮肤测定如上进行。在一个非限制性方面,皮肤清透度可以描述为L/C,其中C是色度并定义为(a2+b2)1/2。
皮肤干燥、表面细纹、皮肤光滑度和肤色分析:皮肤干燥、表面细纹、皮肤光滑度和肤色可以用临床评分技术进行评估。例如,皮肤干燥的临床评分可以通过五点标准Kligmanscale进行确定:(0)皮肤是柔软和湿润的;(1)皮肤呈现正常而没有可见的干燥;(2)皮肤触摸感觉轻微干燥而没有可见的剥落;(3)皮肤感觉干燥、坚韧并且具有有些鳞屑的发白的外观;以及(4)皮肤感觉非常干燥、粗糙并且具有有鳞屑的发白的外观。评估可以由两个临床医师独立进行并进行平均。
肤色临床评分分析:肤色的临床评分可以通过十点模拟数值刻度实施:(10)平滑的均匀的皮肤、粉红棕色的颜色。手持放大镜检查时没有暗的、发红的或有鳞的斑块。皮肤的微观纹理摸上去非常均匀;(7)不用放大镜观察均匀的肤色。没有鳞状区域,但是有由于色素淀积或红斑引起的疹斑。没有直径大于1cm的疹斑;(4)轻易地注意到皮肤疹斑和不均匀的纹理。少量鳞片。某些区域摸上去粗糙的皮肤;以及(1)不均匀的皮肤着色和纹理。多个区域的鳞片和疹斑,色素减退型、发红的或黑色的斑点。大面积的直径超过1cm的不均匀着色。评估由两个临床医师独立进行并进行平均。
皮肤平滑度的临床评分分析:皮肤光滑度的临床评分可以通过一个十点模拟数值刻度进行分析:(10)光滑的,皮肤是湿润的和闪光的,手指划过表面时没有阻力;(7)一定程度光滑的,微小的阻力;(4)粗糙的、可见地改变的,摩擦时有摩擦力;以及(1)粗糙的、片状的、不均匀的表面。评估由两个临床医师独立进行并进行平均。
用Packman等人(1978)公开的方法进行的皮肤光滑度和皱纹减少的分析:皮肤光滑度和皱纹的减少也可以通过使用Packman等人(1978)公开的方法进行可视化评估。例如,每一受试者就诊时,对每一受试者的表面面线(SFL)的深度、浅度和总数量都可以进行认真的评分和记录。通过将数量因子乘以深度/宽度/长度因子得到数字的分数。获得眼睛区域和嘴巴区域(左侧和右侧)的分数,加到一起作为总的皱纹分数。
用Hargens Ballistometer进行的皮肤紧致度分析:皮肤紧致度可以用HargensBallistometer,一种通过在皮肤上落下一个小物体并记录前两个反弹峰来评估皮肤弹性和紧致度的装置,进行测量。ballistometry是使用相对钝的探头(4平方毫米-接触面积)的小的轻量探测器。探测器轻轻地穿透进入皮肤,导致依赖于皮肤外层性质的测量,所述皮肤外层包括角质层和外表皮以及部分真皮层。
用Gas Bearing Electrodynamometer进行的皮肤柔软度/柔韧性分析:皮肤柔软度/柔韧性可以使用Gas Bearing Electrodynamometer,一种测量皮肤压力/张力性质的仪器,进行评估。皮肤的黏弹性与皮肤保湿有关。可以通过用双面胶将探测器附着在皮肤表面实现对脸颊区域特定位点的测量。大约3.5gm的力平行施加于皮肤表面,精确地测量皮肤的位移。然后可以计算皮肤的柔韧性,并表达为DSR(动态弹簧刚度,以gm/mm计)。
用复制品进行的线条和皱纹的显现分析:皮肤上线条和皱纹的显现可以使用复制品进行评估,所述复制品是皮肤表面的印模。可以使用如硅橡胶的材料。复制品可以通过图像分析进行分析。线条和皱纹可见性的变化可以通过利用硅复制品形成受试者的脸并用计算机图像分析系统分析复制品图像进行客观地定量。复制品可以从眼睛区域和颈部区域获得,并用数码相机以低照明入射角进行拍摄。数字图像可以用图像处理程序进行分析并确定复制品被皱纹和细纹覆盖的区域。
用表面光度仪/记录针的方法进行的皮肤表面轮廓分析:皮肤表面轮廓可以通过使用表面光度仪/记录针的方法进行测量。这包括闪光或拖动记录针穿过复制品表面。记录针的垂直位移通过距离传感器可以录入计算机,在扫描复制品的一定距离后,皮肤轮廓的分析可以以二维曲面产生。该扫描可以沿着固定的轴重复任意次数以产生模拟的皮肤3-D图像。使用记录针技术可以获得十个随机的复制品截面,并组合产生平均值。感兴趣的值包括Ra,其为通过积分相对于平局轮廓高度的轮廓高度计算得到的所有粗糙度(高度)值的算术平均数。Rt,其为最高峰和最低谷之间的最大垂直距离,以及Rz,其为平均峰振幅减去平均峰高度。数值以用mm为单位标定的数值给出。设备应在每次使用前通过扫描已知数值的金属标准物进行标准化。Ra值可以通过下式计算:Ra=标准化粗糙度;lm=横向(扫描)长度;以及y=轮廓位置相对于平均轮廓高度的绝对值(x-轴)。
MELANODERMTM分析:在其他非限制性方面,本说明书公开的活性成分、成分的组合或具有所述组合的组合物的任一种的功效可以通过使用皮肤类似物,例如MELANODERMTM来进行评估。黑素细胞,皮肤类似物中细胞的一种,当暴露于L-二羟苯基丙氨酸(L-DOPA)即黑色素的前体时明确地污染。皮肤类似物MELANODERMTM可以用各种含有本说明书中公开的活性成分的每一种、成分的组合或具有所述组合的组合物的任一种的基质进行处理,或仅使用作为对照物的基质进行处理。或者,未处理的皮肤类似物样品可以用作对照物。
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本文中所公开和要求保护的所有组合物和/或方法可以根据本公开不需要不合适的实验即制成和实现。尽管本文公开的组合物和方法已经以优选实施方案的方式进行了描述,但是对于本领域技术人员明显的是,在不脱离本发明的概念、精神和范围的情况下可以对本文描述的组合物和/或方法以及方法的步骤或步骤的顺序中实施变化。更具体地,明显的是化学和生理两方面都相关的一些试剂可以替代本文所描述的试剂,同时会得到相同或相似的结果。所有对本领域技术人员明显的这类相似的替代和改变都被视为在如由所附权利要求限定的本发明的精神、范围和概念内。
Claims (65)
1.一种制备用于抵消由使用去角质成分给皮肤去角质引起的皮肤刺激的组合物的方法,所述组合物包含:25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物、0.0001重量%至0.01重量%的西葫芦籽提取物和去角质成分,其中所述组合物能够抵消由使用去角质成分给皮肤去角质引起的皮肤刺激,其中所述浮游生物提取物包含糖同分异构体,即由溶藻弧菌合成的胞外多糖。
2.根据权利要求1所述的方法,其中所述西葫芦籽提取物增加皮肤中的胶原蛋白生成。
3.根据权利要求1所述的方法,其中所述西葫芦籽提取物抑制皮肤中的MMP3活性。
4.根据权利要求1所述的方法,其中所述4-叔丁基环己醇减少皮肤的刺激。
5.根据权利要求1所述的方法,其中所述浮游生物提取物调节皮肤。
6.根据权利要求1所述的方法,其中所述浮游生物提取物减少皮肤的炎症。
7.根据权利要求1所述的方法,其中所述芦苇提取物和茯苓提取物减少皮肤的炎症。
8.根据权利要求1所述的方法,其中所述芦苇提取物和茯苓提取物增加皮肤屏障修复和/或皮肤屏障维护。
9.根据权利要求1所述的方法,其中所述组合物被配制成面膜。
10.根据权利要求1所述的方法,其中所述去角质成分是α羟基酸。
11.根据权利要求10所述的方法,其中所述组合物包含2重量%至20重量%的α羟基酸。
12.根据权利要求10所述的方法,其中所述α羟基酸是羟基乙酸。
13.根据权利要求1所述的方法,其中所述组合物能够被施用到面部。
14.一种制备用于通过使用去角质成分使皮肤去角质的组合物的方法,所述组合物包含:25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物、0.0001重量%至0.01重量%的西葫芦籽提取物、和去角质成分,其中所述浮游生物提取物包含糖同分异构体,即由溶藻弧菌合成的胞外多糖。
15.根据权利要求14所述的方法,其中所述西葫芦籽提取物增加皮肤中的胶原蛋白生成。
16.根据权利要求14所述的方法,其中所述西葫芦籽提取物抑制皮肤中的MMP3活性。
17.根据权利要求14所述的方法,其中所述4-叔丁基环己醇减少皮肤的刺激。
18.根据权利要求14所述的方法,其中所述浮游生物提取物调节皮肤。
19.根据权利要求14所述的方法,其中所述浮游生物提取物减少皮肤的炎症。
20.根据权利要求14所述的方法,其中所述芦苇提取物和茯苓提取物减少皮肤的炎症。
21.根据权利要求14所述的方法,其中所述芦苇提取物和茯苓提取物增加皮肤屏障修复和/或皮肤屏障维护。
22.根据权利要求14所述的方法,其中所述组合物被配制成面膜。
23.根据权利要求14所述的方法,其中所述去角质成分是α羟基酸。
24.根据权利要求14所述的方法,其中所述组合物包含2重量%至20重量%的α羟基酸。
25.根据权利要求23所述的方法,其中所述α羟基酸是羟基乙酸。
26.根据权利要求14所述的方法,其中所述组合物能够被施用到面部。
27.根据权利要求14所述的方法,其中所述组合物被制备用于进一步增加皮肤中的胶原蛋白生成。
28.根据权利要求27所述的方法,其中所述西葫芦籽提取物增加皮肤中的胶原蛋白生成。
29.根据权利要求27所述的方法,其中所述西葫芦籽提取物抑制皮肤中的MMP3活性。
30.根据权利要求27所述的方法,其中所述4-叔丁基环己醇减少皮肤的刺激。
31.根据权利要求27所述的方法,其中所述浮游生物提取物调节皮肤。
32.根据权利要求27所述的方法,其中所述浮游生物提取物减少皮肤的炎症。
33.根据权利要求27所述的方法,其中所述芦苇提取物和茯苓提取物减少皮肤的炎症。
34.根据权利要求27所述的方法,其中所述芦苇提取物和茯苓提取物增加皮肤屏障修复和/或皮肤屏障维护。
35.根据权利要求27所述的方法,其中所述组合物被配制成面膜。
36.根据权利要求27所述的方法,其中所述去角质成分是α羟基酸。
37.根据权利要求36所述的方法,其中所述组合物包含2重量%至20重量%的α羟基酸。
38.根据权利要求36所述的方法,其中所述α羟基酸是羟基乙酸。
39.根据权利要求27所述的方法,其中所述组合物能够被施用到面部。
40.根据权利要求14所述的方法,其中所述组合物被制备用于进一步抑制皮肤中的MMP3活性。
41.根据权利要求40所述的方法,其中所述西葫芦籽提取物增加皮肤中的胶原蛋白生成。
42.根据权利要求40所述的方法,其中所述西葫芦籽提取物抑制皮肤中的MMP3活性。
43.根据权利要求40所述的方法,其中所述4-叔丁基环己醇减少皮肤的刺激。
44.根据权利要求40所述的方法,其中所述浮游生物提取物调节皮肤。
45.根据权利要求40所述的方法,其中所述浮游生物提取物减少皮肤的炎症。
46.根据权利要求40所述的方法,其中所述芦苇提取物和茯苓提取物减少皮肤的炎症。
47.根据权利要求40所述的方法,其中所述芦苇提取物和茯苓提取物增加皮肤屏障修复和/或皮肤屏障维护。
48.根据权利要求40所述的方法,其中所述组合物被配制成面膜。
49.根据权利要求40所述的方法,其中所述去角质成分是α羟基酸。
50.根据权利要求49所述的方法,其中所述组合物包含2重量%至20重量%的α羟基酸。
51.根据权利要求49所述的方法,其中所述α羟基酸是羟基乙酸。
52.根据权利要求40所述的方法,其中所述组合物能够被施用到面部。
53.一种局部皮肤用组合物,其包含25重量%至80重量%的水、0.1重量%至1.5重量%的4-叔丁基环己醇、0.001重量%至0.1重量%的浮游生物提取物、0.001重量%至0.1重量%的芦苇提取物、0.001重量%至0.1重量%的茯苓提取物、0.0001重量%至0.01重量%的西葫芦籽提取物和去角质成分,其中所述浮游生物提取物包含糖同分异构体,即由溶藻弧菌合成的胞外多糖。
54.根据权利要求53所述的局部皮肤用组合物,其还包含:三乙醇胺、甘油、丁二醇、海水、鲸蜡硬脂醇、花生醇、异硬脂酸失水山梨醇酯、碳酸二辛酯、生物糖胶-1、和二十二醇。
55.根据权利要求54所述的局部皮肤用组合物,其包含:3重量%至15重量%的三乙醇胺、1重量%至10重量%的甘油、1重量%至10重量%的丁二醇、0.1重量%至5重量%的海水、0.1重量%至5重量%的鲸蜡硬脂醇、0.1重量%至5重量%的花生醇、0.1重量%至5重量%的异硬脂酸失水山梨醇酯、0.1重量%至3重量%的碳酸二辛酯、0.1重量%至3重量%的生物糖胶-1、和0.1重量%至3重量%的二十二醇。
56.根据权利要求54所述的局部皮肤用组合物,其还包含:丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、丙烯酰基二甲基牛磺酸铵/VP共聚物、戊二醇、二氢茉莉酮酸甲酯、异十六烷、阿拉伯胶树胶提取物、鲸蜡硬脂基葡糖苷、花生基葡萄糖苷、硅酸镁铝、聚二甲基硅氧烷、巴西酸亚乙酯、黄原胶、乙基芳樟醇、聚山梨醇酯60、EDTA二钠、和二氧化钛。
57.根据权利要求56所述的局部皮肤用组合物,其包含:0.1重量%至3重量%的丙烯酸羟乙酯/丙烯酰基二甲基牛磺酸钠共聚物、0.1重量%至3重量%的丙烯酰基二甲基牛磺酸铵/VP共聚物、0.1重量%至3重量%的戊二醇、0.1重量%至3重量%的二氢茉莉酮酸甲酯、0.1重量%至3重量%的异十六烷、0.1重量%至1.5重量%的阿拉伯胶树胶提取物、0.1重量%至1.5重量%的鲸蜡硬脂基葡糖苷、0.1重量%至1.5重量%的花生基葡萄糖苷、0.01重量%至1重量%的硅酸镁铝、0.01重量%至1重量%的聚二甲基硅氧烷、0.01重量%至1重量%的巴西酸亚乙酯、0.01重量%至1重量%的黄原胶、0.01重量%至1重量%的乙基芳樟醇、0.01重量%至1重量%的聚山梨醇酯60、0.01重量%至1重量%的EDTA二钠、和0.01重量%至1重量%的二氧化钛。
58.根据权利要求53所述的局部皮肤用组合物,其中所述组合物能够抵消由去角质成分引起的皮肤刺激。
59.根据权利要求58所述的局部皮肤用组合物,其中所述去角质成分为α羟基酸。
60.根据权利要求53所述的局部皮肤用组合物,其中所述组合物被配制成面膜。
61.根据权利要求53所述的局部皮肤用组合物,其中所述去角质成分是α羟基酸。
62.根据权利要求61所述的局部皮肤用组合物,其包含2重量%至20重量%的α羟基酸。
63.根据权利要求61所述的局部皮肤用组合物,其中所述α羟基酸是羟基乙酸。
64.根据权利要求53所述的局部皮肤用组合物,其中所述组合物能够增加皮肤中的胶原蛋白生成。
65.根据权利要求53所述的局部皮肤用组合物,其中所述组合物能够抑制皮肤中的MMP3活性。
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DE202015008361U1 (de) | 2016-04-21 |
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