CN103987394A - 护肤制剂 - Google Patents
护肤制剂 Download PDFInfo
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- CN103987394A CN103987394A CN201280060617.1A CN201280060617A CN103987394A CN 103987394 A CN103987394 A CN 103987394A CN 201280060617 A CN201280060617 A CN 201280060617A CN 103987394 A CN103987394 A CN 103987394A
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract
公开了一种组合物及其使用方法,所述组合物包含积雪草、葡萄籽、木兰茎皮、茶树和/或二羟基甲基色酮中的任何一种、任意组合或全部。所述组合物可以用于处理毛细管扩张。
Description
相关申请的交叉引用
本申请要求2011年12月14日提交的美国临时申请61/570,719号和2011年12月9日提交的美国临时申请61/569,034号的利益。所引用的申请的内容通过引用并入本申请。
背景技术
A.技术领域
本发明一般涉及护肤组合物。在一个具体的方面,该组合物包含积雪草(Centella asiatica)提取物、葡萄(Vitis vinifera)籽提取物、木兰(Magnolia)茎皮提取物、茶树(Camellia sinensis)提取物和二羟基甲基色酮的组合。本发明人发现这种组合在处理毛细管扩张或蛛状静脉曲张方面尤其有效。
B.相关技术说明
一般意义上,毛细管扩张的特征可以为位于人的皮肤表面附近的小血管、例如静脉的扩张。这种扩张可以是在皮肤上以红色皮肤、蓝色皮肤、紫色皮肤或有斑点皮肤的形式可见的。在一些实例中,扩张的血管以树枝状、或席子或直线图案、或蛛网状外观存在于皮肤上,这通常被称为“蛛状静脉曲张”。通常出现在人的大腿、小腿和面部的蛛状静脉曲张是视觉上不好看的。
目前处理蛛状静脉曲张的方法包括硬化疗法、手术、射频和激光消融。这类处理方法可能对皮肤造成损伤,并且有时需要专业的帮助。
发明内容
本发明人已经发现,可以在局部皮肤用制剂中使用成分的组合来处理毛细管扩张或蛛状静脉曲张。除了处理患病的皮肤之外,该组合物还可以例如通过使皮肤润湿而有益于皮肤。因此,该组合物不像其它处理方法一样损伤皮肤。另外,该组合物可以由使用者施用而无需专业的帮助。
在一个实例中,公开了一种组合物和一种处理毛细管扩张的方法,所述方法包括对需要处理的皮肤局部地施用所述组合物。该组合物可以包含来自积雪草、葡萄籽、木兰茎皮、茶树和/或二羟基甲基色酮的提取物和/或成分的组合、或其任意组合(例如至少2、3、或4种所述提取物),所述提取物或成分的全部,或特定组合(例如来自积雪草和葡萄籽的提取物;来自积雪草和木兰茎皮的提取物;来自积雪草和茶树的提取物;来自积雪草和二羟基甲基色酮的提取物;来自葡萄籽和木兰茎皮的提取物;来自葡萄籽和茶树的提取物;来自葡萄籽和二羟基甲基色酮的提取物;来自木兰茎皮和茶树的提取物;来自木兰茎皮和二羟基甲基色酮的提取物;来自茶树和二羟基甲基色酮的提取物;等)。在一个实例中,木兰茎皮提取物为包含和厚朴酚与厚朴酚的荷花玉兰(Magnoliagrandiflora)茎皮提取物,积雪草提取物包含积雪草苷、羟基积雪草酸和积雪草酸,茶树提取物为包含表没食子儿茶素没食子酸酯的茶树叶提取物,并且葡萄籽提取物包含多酚。
“提取物的组合”可以包含单独地包含到组合物中的单独的提取物,或者可以包含首先组合然后添加到组合物的两种或更多种提取物。在具体的实施方案中,该组合物包含全部五种所述提取物和成分。本发明人发现,积雪草提取物和葡萄籽提取物可以用于促进内皮管破坏,这可以限制并破坏蛛状静脉曲张的形成。已经发现二羟基甲基色酮使表皮变厚,这可以有效减少蛛状静脉曲张的外观。已经发现木兰茎皮提取物抑制血管生成,这可以限制血管生长。茶树可以作为血管收缩剂,其可以将血液推出血管,从而使蛛状静脉曲张在皮肤表面较不明显。茶树提取物可以包含多酚化合物,例如表没食子儿茶素没食子酸酯。本发明人还发现,当组合这些成分的每一种时,它们在限制蛛状静脉曲张的形成同时减少现存静脉曲张的外观方面具有协同效应。因此,该组合在处理毛细管扩张、例如蛛状静脉曲张方面尤其有效。在特定的方面,该组合物施用到皮肤,并且在局部施用后在皮肤上保留至少5、10、15、30或更多分钟,或者1、4、8、12、16、20或24小时。该组合物可以施用到面部皮肤、腿部皮肤、踝部皮肤、臂部皮肤等上存在的毛细管扩张(例如蛛状静脉曲张)。在特定的方面,该组合物可以配制为膏霜、凝胶或润肤露。在一些实例中,该组合物为乳液(例如水包油、油包水、疏水包亲水、亲水包疏水、水包硅酮、硅酮包水等)。该组合物还可以包含保湿剂、紫外吸收剂、抗氧化剂、结构化剂、乳化剂、含硅酮的化合物、精油、增稠剂和/或防腐剂,例如本说明书全文中所公开的那些。该组合物可以包含药物成分,例如本说明书全文中所公开的那些。在一些实例中,该组合物还可以包含毛叶杯轴花(Tambourissa trichophylla)叶提取物。该组合物可以包含0.0001重量%至10重量%(或0.001重量%、0.01重量%、0.1重量%、1重量%、2重量%、3重量%、4重量%、5重量%、6重量%、7重量%、8重量%、9重量%或10重量%或更多)的来自积雪草的提取物、0.0001重量%至10重量%(或0.001重量%、0.01重量%、0.1重量%、1重量%、2重量%、3重量%、4重量%、5重量%、6重量%、7重量%、8重量%、9重量%或10重量%或更多)的来自葡萄籽的提取物、0.0001重量%至10重量%(或0.001重量%、0.01重量%、0.1重量%、1重量%、2重量%、3重量%、4重量%、5重量%、6重量%、7重量%、8重量%、9重量%或10重量%或更多)的来自木兰茎皮的提取物、0.0001重量%至10重量%(或0.001重量%、0.01重量%、0.1重量%、1重量%、2重量%、3重量%、4重量%、5重量%、6重量%、7重量%、8重量%、9重量%或10重量%或更多)的来自茶树的提取物和/或0.0001重量%至10重量%(或0.001重量%、0.01重量%、0.1重量%、1重量%、2重量%、3重量%、4重量%、5重量%、6重量%、7重量%、8重量%、9重量%或10重量%或更多)的二羟基甲基色酮。在特定的方面,该组合物可以包含0.0001重量%至10重量%(或0.001重量%、0.01重量%、0.1重量%、1重量%、2重量%、3重量%、4重量%、5重量%、6重量%、7重量%、8重量%、9重量%或10重量%或更多)的来自毛叶杯轴花的提取物。木兰茎皮提取物可以是荷花玉兰茎皮提取物、厚朴(Magnolia officinalis)茎皮提取物或和厚朴(Magnolia obovata)茎皮提取物。在特定的方面,提取物来自荷花玉兰茎皮。积雪草提取物可以是来自积雪草分生组织的培养物。茶树提取物可以是茶树叶提取物,和/或可以包含多酚化合物,例如表没食子儿茶素没食子酸酯。积雪草提取物、葡萄籽提取物、木兰茎皮提取物和/或茶树提取物可以是基于水、醇、水-醇或油的提取物。在具体的实施方案中,提取物是醇提取物或水/醇提取物的组合。
还公开了一种组合物和一种使用该组合物来处理皮肤的方法,所述方法包括对需要处理的皮肤局部地施用所述组合物。该组合物可以包含积雪草提取物、葡萄籽提取物、木兰茎皮提取物、茶树提取物和/或二羟基甲基色酮中的至少一种、两种、三种、四种或全部。在一些实例中,该组合物可以施用到毛细管扩张的皮肤、呈现出蛛状静脉曲张的皮肤和/或呈现出静脉曲张的皮肤。在特定的方面,该组合物可以用于束缚血液在血管和小血管,例如小动脉、毛细血管和/或小静脉中的流动。该组合物还可以包含毛叶杯轴花也提取物。在一个实例中,成分的组合可以是积雪草提取物和葡萄籽提取物。在一个实例中,该组合可以是积雪草提取物和木兰茎皮提取物。在一个实例中,该组合可以是积雪草提取物和茶树提取物。在一个实例中,该组合可以是积雪草提取物和二羟基甲基色酮。在一个实例中,该组合可以是葡萄籽提取物和木兰茎皮提取物。在一个实例中,该组合可以是葡萄籽提取物和茶树提取物。在一个实例中,该组合可以是葡萄籽提取物和二羟基甲基色酮。在一个实例中,该组合可以是木兰茎皮提取物和茶树提取物。在一个实例中,该组合可以是木兰茎皮提取物和二羟基甲基色酮。在一个实例中,该组合可以是茶树提取物和二羟基甲基色酮。该组合物的其它方面可以与在上一段落中描述的相似,其通过引用并入(例如成分的量、附加成分、组合物的配制、特定的提取物等)。在一个实例中,木兰茎皮提取物为包含和厚朴酚与厚朴酚的荷花玉兰茎皮提取物,积雪草提取物包含积雪草苷、羟基积雪草酸和积雪草酸,茶树提取物为包含表没食子儿茶素没食子酸酯的茶树叶提取物,并且葡萄籽提取物包含多酚。
本发明的组合物可以配制为局部护肤组合物。该组合物可以是化妆品组合物。在其它方面,该组合物可以包含在化妆品载剂中。化妆品载剂的非限制性实例在本说明的其它章节中公开,并且对于本领域技术人员是已知的。化妆品载剂的实例包括乳液(例如水包油和油包水乳液)、膏霜、润肤露、溶液(例如水溶液或水-醇溶液)、无水基质(例如口红或粉末)、凝胶和软膏。在其它非限制性实施方案中,本发明的组合物可以包含在抗老化、清洁或保湿产品中。该组合物还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。在本发明的其它方面中,该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从1cps到远超过1百万cps,或是其间可得到的任意范围或整数(举例来说,如在25℃下在布氏黏度计上用TC轴以2.5rpm的转速测量的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、1000000cps等)。在非限制性方面中组合物可以具有大约6至大约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。本发明的组合物可以具有UVA和UVB吸收性质。该组合物可以具有2、3、4、5、6、7、8、9、10、11、12、13、14、15、20、25、30、35、40、45、50、55、60或更大的防晒指数(SPF),或是其中可以得到的任何整数。该组合物可以是防晒露、喷雾或霜。在具体的方面,该组合物可以是无油的、基本上无水的和/或无水的。其它方面包括具有水的组合物。
本发明的组合物还可以包含以下附加成分中的任何一种、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。在特定的方面,该组合物可以包含在之前句子中确定的这些附加成分中的至少二、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全文确定,并通过引用并入本章节。这类成分的量的范围以组合物的重量或体积计可以从0.0001%到99.9%,或者是在如本说明书其它章节中所公开的范围之间的任何整数或范围,其通过引用并入本段。
该组合物还可以用于处理或预防与毛细管扩张不同的多种皮肤症状。例如,该组合物可以用于处理或预防细纹或皱纹、干燥或开裂的皮肤、红斑、敏感性皮肤或发炎的皮肤。在具体的方面,红斑、敏感性皮肤或发炎的皮肤是由皮肤晒伤、皮肤的电处理、皮肤烧伤、接触性过敏、系统性过敏、皮肤中毒、运动、昆虫叮咬、细菌感染、病毒感染、真菌感染、原生动物感染、按摩或风吹性皮肤伤导致的。在其它方面,以下额外地皮肤症状可以根据本说明书和权利要求书全文所公开的方法和组合物来处理或预防:瘙痒症、雀斑、老年斑、老年性紫癜、角化病、黄褐斑、疹块、结节、晒伤皮肤、皮炎(包括但不限于脂溢性皮炎、钱币形皮炎、接触性皮炎、过敏性皮炎、剥脱性皮炎、口周皮炎和停滞性皮炎)、银屑病、毛囊炎、酒渣鼻、痤疮、脓疱病、丹毒、红癣、湿疹和其它炎性皮肤症状。在某些非限制性方面,皮肤症状可以是由暴露于紫外线、衰老、刺激、长期日照、环境污染、空气污染、风、寒冷、高温、化学品、疾病病理性、烟熏或营养不良导致的。皮肤可以是面部皮肤或非面部皮肤(例如手臂、腿、手、胸、后背、脚等)。该方法还可以包括确定需要皮肤处理的个体。个体可以是男性或女性。个体的年龄可以是至少1、2、3、4、5、6、7、8、9、10、15、20、25、30、35、40、45、50、55、60、65、70、75、80、85、90、95或更大,或者其中可得出的任何范围。该方法还可以包括局部地施用对以下情况有效的量:提高皮肤的角质层更新速率;增加成纤维细胞中的胶原蛋白合成;提高细胞的抗氧化防御机制(例如抗氧化剂的外源性添加可以支撑、补充或者预防皮肤细胞(例如角化细胞、黑色素细胞、朗格汉斯细胞等)中的细胞抗氧化剂,例如过氧化氢酶和谷胱甘肽的损失,所述抗氧化剂会减少或预防对皮肤、细胞、蛋白质和脂质的氧化性损伤);抑制黑色素细胞中的黑素生成;减少或预防对皮肤的氧化性损伤(包括减少皮肤中脂质过氧化物的量和/或蛋白氧化)。
还公开了一种减少不均匀肤色外观的方法,其包括对具有不均匀肤色的皮肤局部地施用本说明书和权利要求书全文所公开的组合物中的任何一种,其中对不均匀肤色局部地施用所述组合物减少不均匀肤色的外观。在一个实例中,该组合物包含二羟基甲基色酮、积雪草提取物、葡萄籽提取物、木兰茎皮提取物和/或茶树提取物。
在另一实施方案中,公开了一种减少与红斑、敏感性皮肤或发炎的皮肤相关的疼痛的方法,其包括对红斑皮肤、敏感性皮肤或发炎的皮肤局部地施用本说明书和权利要求书全文所公开的组合物中的任何一种,其中对红斑皮肤、敏感性皮肤或发炎的皮肤局部地施用所述组合物减少与红斑、敏感性皮肤或发炎的皮肤相关的疼痛。在一个实例中,该组合物包含二羟基甲基色酮、积雪草提取物、葡萄籽提取物、木兰茎皮提取物和/或茶树提取物。
在另一方面,公开了一种减少与红斑、敏感性皮肤或发炎的皮肤相关的症状的外观的方法,其包括对红斑皮肤、敏感性皮肤或发炎的皮肤局部地施用本说明书和权利要求书全文所公开的组合物中的任何一种,其中对红斑皮肤、敏感性皮肤或发炎的皮肤局部地施用所述组合物减少与红斑、敏感性皮肤或发炎的皮肤相关的症状的外观。在一个实例中,该组合物包含二羟基甲基色酮、积雪草提取物、葡萄籽提取物、木兰茎皮提取物和/或茶树提取物。
在其它方面,公开了一种增加皮肤细胞中胶原蛋白合成的方法,其包括对需要胶原蛋白合成的皮肤细胞局部地施用本说明书和权利要求书全文所公开的组合物中的任何一种,其中对皮肤细胞局部地所述组合物增加皮肤细胞中的胶原蛋白合成。这类细胞的非限制性实例包括人类表皮角化细胞、人类成纤维细胞真皮细胞、人类黑色素细胞、三维人类细胞衍生的体外组织等同物,包括人类角化细胞、人类成纤维细胞或人类黑色素细胞、或其任意组合(例如人类角化细胞和人类成纤维细胞的组合,或人类角化细胞和人类黑色素细胞的组合)。在一个实例中,该组合物包含二羟基甲基色酮、积雪草提取物、葡萄籽提取物、木兰茎皮提取物和/或茶树提取物。
还公开了一种增亮皮肤或均匀肤色的方法,其包括对皮肤施用本说明书和权利要求书全文所公开的组合物中的任何一种。该方法还可以包括确定需要增亮皮肤或均匀肤色的个体。该方法还可以包括抑制皮肤细胞中的黑素生成,抑制皮肤细胞中的酪氨酸酶或酪氨酸酶合成,或抑制皮肤细胞中黑色素转移到角质细胞。该组合物可以作为α-黑色素刺激激素拮抗剂。该组合物可以使皮肤的色素沉着均匀。在非限制性方面,增亮皮肤可以包括通过对具有老年斑、皮肤色素减退或雀斑等的皮肤局部地施用该组合物来减少老年斑、皮肤色素减退或雀斑的外观。在一个实例中,该组合物包含二羟基甲基色酮、积雪草提取物、葡萄籽提取物、木兰茎皮提取物和/或茶树提取物。
还公开了一种处理过度色素沉着的方法,其包括对皮肤施用本说明书和权利要求书全文所公开的组合物中的任何一种。该方法还可以包括确定需要处理过度色素沉着的个体。本发明人预期的另外的方法包括用于减少老年斑、皮肤色素减退或雀斑的外观,减少或预防皮肤中细纹或皱纹的外观,或者增加皮肤的坚实度的方法。在一个实例中,该组合物包含二羟基甲基色酮、积雪草提取物、葡萄籽提取物、木兰茎皮提取物和/或茶树提取物。
还预期包含本说明书和权利要求书全文所公开的组合物中的任何一种的试剂盒。在特定的实施方案中,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。在特定的方面,该组合物以喷雾、团块或液体分配。该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。
还预期了一种包含本发明的组合物的产品。在非限制性方面,该产品可以是化妆品。该化妆品可以是本说明书其它章节所述的那些,或是本领域技术人员已知的那些。产品的非限制性实例包括保湿霜、膏霜、润肤露、柔肤水、粉底、晚霜、口红、清洁剂、爽肤水、防晒霜、面膜或抗老化产品。
该组合物及其使用方法可以“包含”任何说明书全文所公开的成分,“基本上由所述成分构成”或“由所述成分构成”。“基本上由……构成”表示在组合物中包含附加成分不实质上影响用于处理毛细管扩张或蛛状静脉曲张的组合物的有益性能。例如,当组合物“基本上由二羟基甲基色酮、积雪草提取物、葡萄籽提取物、木兰茎皮提取物和茶树提取物中的任何一种、任意组合、或2、3、4、或全部5种构成”时,所述组合物不包含会实质上影响组合物用于处理毛细管扩张或蛛状静脉曲张的有益性能的任何成分。例如,可以作为血管扩张剂的成分会使毛细管扩张或蛛状静脉曲张的外观恶化,而不是处理所述症状。
期望对于本发明的任何方法或组合物,可以实施本说明书中所讨论的任何实施方案,反之亦然。此外,本发明的组合物可以用于实现本发明的方法。
在一个实施方案中,本发明的组合物可以是可药用的或可化妆用的。“可药用的”和/或“可化妆用的”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、非黏性或非黏着的组合物等)。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角质组织的表面上。“局部皮肤用组合物”包含适合在角质组织上局部施用的组合物。这类组合物一般为皮肤病学上可接受的,这是因为当施用到皮肤时,其不具有异常毒性、不相容性、不稳定性、过敏反应等。本发明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”包含配置作为哺乳类最外保护层的含有角质的层,并且包括但不限于皮肤、毛发和指甲。
“非挥发性油”包括在常温或室温不会挥发的那些物质。
当在权利要求和/或说明书中使用时,术语“混合物”、“混合”或这些术语的任何变体包括搅拌、共混、分散、碾磨、均匀化和其它相似的方法。所公开组合物的组分或成分的混合可以形成为溶液。在其它实施方案中,混合物不可以形成溶液。成分/组分还可以作为未溶解的胶态悬浮液存在。
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必全部地为指定的事物,并且在一个非限定性实施方案中基本上涉及的范围在10%以内、在5%以内、在1%以内或在0.5%以内。
当在权利要求和/或说明书中使用时,术语“抑制”、“减少”、“处理”或这些术语的任何变体包括达到预期结果的任何可测量的减少或完全的抑制。
作为本说明书和/或权利要求所使用的术语,术语“有效的”表示适于实现希望的、期望的或预期的结果。
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,并且不排除附加的、未列举的要素或方法步骤。
本发明的其它目的、特征和优点通过下面的详细描述会变得明显。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给出。另外,期望通过该详细描述,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。
示例性实施方案的描述
毛细管扩张的皮肤是视觉上不好看的。其可以导致皮肤表面附近扩张的血管(例如静脉),其在皮肤上呈现为红纹、紫纹和/或蓝纹,有时被称为“蛛状静脉曲张”。该纹可以宽小于1至3mm,长几毫米至几厘米。毛细管扩张在健康人中是常见的,并且可以由暴露于太阳或衰老导致。其有时困扰人脸上的鼻子、面颊和下巴,或大腿,膝盖下方和脚踝上,其全部为人体的高度可见区域。
代替使用传统的方法,例如硬化疗法、手术、射频和激光消融,本发明人发现当组合时对降低毛细管扩张、例如蛛状静脉曲张的外观有效,同时还对皮肤提供额外的益处的成分的组合。在以下子章节中描述本发明的这些和其它非限制性方面。
A.活性成分
如上文所说明的,本发明的局部护肤组合物可以包含积雪草提取物、葡萄籽提取物、木兰茎皮提取物、茶树提取物和/或二羟基甲基色酮。在特定的方面,毛叶杯轴花叶提取物也可以包含在组合中。关于积雪草提取物,积雪草植物为一种原产于例如印度、斯里兰卡、澳大利亚、印度尼西亚、马来西亚、美拉尼西亚、巴布亚新几内亚和亚洲其它部分的国家的小型草本植物。该植物的提取物是可以从多种来源(参见国际化妆品成分词典和手册,第12版,2008(“CTFA”),第1卷,第458-60页,其通过引用并入)商购获得的。在具体的实施方案中,可以使用全株提取物(参见CTFA的第458-59页)。在实施例中使用的来源是从Bayer Sante Familiale SAS(法国)以商品名TECA(积雪草的滴定提取物,Titrated Extract of Centella Asiatica)获得的,其包含积雪草苷、羟基积雪草酸和积雪草酸。
关于葡萄籽提取物,葡萄植物为一种原产于地中海地区、中欧和西南亚的藤本植物。提取物是从所述植物的籽中获得的。另外,葡萄籽提取物是可以从多种来源(参见例如CTFA,第3卷,第2891-93页,其通过引用并入)商购获得的。该提取物可以包含多酚,例如儿茶素、表儿茶素和类黄酮。
转向木兰茎皮提取物,木兰植物原产于北美、中国、日本和俄罗斯。其为一种具有棕色茎皮的大型落叶乔木。在具体的方面,木兰茎皮来自荷花玉兰,其原产于北美。在其它方面,其来自厚朴,其也原产于中国。在其它实例中,其可以来自和厚朴,其原产于日本和俄罗斯。该提取物是从木兰植物,例如荷花玉兰、厚朴或和厚朴的茎皮中获得的。其可以包含诸如厚朴酚与和厚朴酚的化合物。木兰茎皮提取物是可以从多种来源(参见例如CTFA,第2卷,第1500页,其通过引用并入)商购获得的。在实施例中使用的来源是从DSM(北美)获得的,包含来自荷花玉兰茎皮的提取物,所述提取物包含厚朴酚与和厚朴酚。
关于茶树提取物,茶树植物原产于中国,并且为一种开花植物。该提取物可以是从所述植物的全株或部分中获得的。在具体的实例中,其来自所述植物的叶、根、花或种子,尤其是叶。在具体的实例中,茶树提取物可以包含多酚化合物,例如表没食子儿茶素没食子酸酯。茶树提取物,无论来自所述植物的全株或部分,都是可以从多种来源(参见例如CTFA,第1卷,第400-07页,其通过引用并入)商购获得的。在实施例中使用的来源是从DSM(北美)获得的,包含表没食子儿茶素没食子酸酯(EGCG)——其以商品名销售。
转向二羟基甲基色酮(DHMC),其具有以下化学式:
其是可以从EMD Chemicals(美国)以商品名LureminTM商购获得的。这是实施例中使用的来源。
关于毛叶杯轴花叶提取物,毛叶杯轴花为一种原产于马达加斯加的植物。该提取物是从叶中获得的。毛叶杯轴花叶提取物是可以从多种来源(参见例如CTFA,第3卷,第2713页,其通过引用并入)商购获得的。
除了可以商购获得上文确定的提取物之外,所述提取物还可以通过获得相应的植物或其部分以通过本领域普通技术人员已知的提取物方法制备提取物来制备。例如,本领域普通技术人员通过本领域已知的任何合适的方法能够从相应植物的全株或部分分离上文确定的提取物的任何一种。在一个非限制性实例中,可以通过机械手段使植物(或植物的任意部分)破裂,这产生泥。然后加工该泥使其基本上不含杂质或不期望的固体。然后将该泥倒入浅的器皿中,并迅速暴露于低温,即速冻,例如在-20℃或更低,优选为了移除水分在真空条件下进行(冻干)。然后,得到的提取物可以用在本发明的组合物中。
在其它方面,可以对其全株或任何部分使用基于水、醇、水-醇或油的提取技术或其组合来制备提取物。在这种方法中,将期望的植物部分或全株粉碎(例如搅拌机),然后使其经受期望的溶剂(例如基于水、醇、水/醇或油的溶剂)以获得期望的提取物。然后提取物可以以液体形式储存,冻干,或进行进一步的加工技术(例如加热、冷却等)。提取方法对提取领域普通技术人员来说是众所周知的(例如浸渍、浸泡、渗滤、消化、煎煮、热连续提取、水-醇提取、逆流提取、微波辅助提取、超声提取、超临界流体提取、植物提取(例如用氢-氟-碳溶剂)等)。
B.本发明的组合物
期望本发明的组合物可以包含本说明书全文所描述的任何皮肤活性物或其任意组合。在具体的方面,可以组合皮肤活性物(例如积雪草、葡萄籽、木兰茎皮、茶树和二羟基甲基色酮)。该组合物可以包含本说明书全文所描述的附加成分的任意量的组合。在该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,该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:例如至少大约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%或其间任意可推出的范围的至少一种在本说明书的全文和权利要求所提及的成分。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。
本发明公开的组合物还可以包含多种抗氧化剂以阻止一种或更多种组分的氧化。另外,可以通过防腐剂,例如多种抗细菌剂和抗真菌剂,包括但不限于对羟基苯甲酸酯(例如对羟基苯甲酸甲酯、对羟基苯甲酸丙酯)、氯丁醇、苯酚、山梨酸、硫汞撒或其组合来防止微生物的作用。
C.载剂
本发明的组合物可以并入到所有类型的载剂中。合适载剂的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、硅酮包水包油的乳液)、膏霜、润肤露、溶液(水的或者水-醇的)、无水基质(例如口红和粉末)、凝胶和软膏,或通过其它方法或本领域普通技术人员会知道的前述方法的任意组合(Remington's,1990)。变体和其它合适的载剂对于熟练技术人员是明显的,并且适用于本发明。在特定的方面,重要的是,选择化合物、成分和试剂的浓度和组合,使得该组合是化学相容的并且不形成从最终产物中沉淀出来的络合物。
还预期本说明书全文所确定的成分,包括但不限于积雪草、葡萄籽、木兰茎皮、茶树或二羟基甲基色酮、或其任意组合可以单独地或组合地包封用于递送到目标区域,例如皮肤。包封技术的非限制性实例包括使用脂质体、囊泡和/或纳米颗粒(例如生物可降解的和生物不可降解的胶体颗粒,其包含其中捕获、包封和/或吸附有所述成分的聚合材料——实例包括纳米球和纳米胶囊),所述脂质体、囊泡和/或纳米颗粒可以用作递送载剂以将该成分递送到皮肤(参见例如美国专利6,387,398;美国专利6,203,802;美国专利5,411,744;Kreuter1998)。
D.化妆品产品和制品
本发明的组合物还可以用在许多化妆品产品中,包括但不限于防晒产品、免晒皮肤美黑产品、毛发产品、手指甲产品、保湿霜、益肤霜和润肤露、柔软剂、日用乳液、凝胶、软膏、粉底、晚霜、口红、清洁剂、爽肤水、面膜或其它已知的化妆品产品或应用。另外,化妆品产品可以配制为保留型或洗去型产品。在特定的方面,本发明的组合物为独立的产品。
E.附加成分
除了本说明书全文所公开的积雪草、葡萄籽、木兰茎皮和茶树以及二羟基甲基色酮之外,本发明的组合物还可以包含附加成分,例如化妆品成分和药物活性成分。这些附加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环境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)、痕量金属(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、黄春菊、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、脲和甘露醇)、剥离剂、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、透明质酸和甘草酸二钾)。这些附加成分中一部分的非限制性实例在以下子章节中提供。
a.紫外吸收剂
可以与本发明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
可以与本发明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(perseagratissima)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(ricinus communis)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(aleuritesmoluccana)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 medica limonum)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(elaeis guineensis)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(rosmarinus officinalis)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、角鲨烯、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(canangaodorata)油。
c.抗氧化剂
可以与本发明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(5)醚、生育酚聚氧乙烯(10)醚、生育酚聚氧乙烯(12)醚、生育酚聚氧乙烯(18)醚、生育酚聚氧乙烯(50)醚、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,本发明的组合物可以包含结构化剂。在特定的方面,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
在本发明的特定方面,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(3)醚磷酸酯、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(2)醚、硬脂醇聚氧乙烯(20)醚、硬脂醇聚氧乙烯(21)醚、十六/十八醇聚氧乙烯(20)醚、PPG-2甲基葡萄糖醚二硬脂酸酯、鲸蜡醇聚氧乙烯(10)醚、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、聚硅酮(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,即通常低于约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DowCorning344Fluid、Dow Corning345Fluid、Dow Corning244Fluid和DowCorning245Fluid、Volatile Silicon7207(康涅狄格州丹伯里的Union CarbideCorp.);低黏度聚二甲基硅氧烷,即黏度大约为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Dow Corning200-0.5cst Fluid)。Dow CorningFluid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二甲基聚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.,Silicone Products 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。这类油一般作为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一些方法进行提取(例如,蒸气蒸馏、花香提取(即使用脂肪提取)、浸渍、溶剂提取或机械压榨)。当这些类型的油暴露于空气时,其趋于挥发(即挥发性油)。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发明的组合物的稳定性。在本发明的特定方面,增稠剂包括氢化聚异丁烯或三羟基硬脂酸甘油酯,或两者的混合物。
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。其它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直链或带支链的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直链或带支链的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
可以在本发明的环境下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))、对羟基苯甲酸酯(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本发明的组合物是有用的。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、牙科和牙周处理剂、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,本发明的组合物可以包括在试剂盒内。试剂盒可以包括容器。容器可以包括瓶子、金属管、层合管、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。在其它实施方案中,可以挤压容器(例如金属管、层合管或塑料管)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
列出以下实施例以说明本发明的特定非限制性方面。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发现的在本发明的实践中发挥良好作用的技术。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
发现积雪草提取物和葡萄籽提取物都促进内皮管破坏。发现二羟基甲基色酮使表皮变厚。发现木兰茎皮提取物抑制血管生成。发现具有表没食子儿茶素没食子酸酯的茶树为血管和小血管,例如小动脉、毛细血管和小静脉的血管收缩剂。数据未示出。
对36名18至65岁的女性小组成员进行活体研究以评价以上所提及的五种成分的组合处理毛细管扩张的能力。每一小组成员具有轻微的至中等的毛细管扩张。该研究要求在12周的周期内4次访视测试机构。在第一次访视时(基线),实验室技术员使用皮肤标记物标记小组成员腿上的关注区域(大约5×5cm2)。在所有访视期间,由专业评分员使用0至5(0=没有,5=严重)的等级对小组成员的毛细血管颜色、毛细血管分支、蛛状静脉曲张周围的可视红斑和干燥度以及蛛状静脉曲张的总体外观进行视觉评分。评分之后,使用Fuji S2数码相机拍摄一组测试位点的照片。使用Image Pro软件分析照片上的毛细血管长度和毛细血管数量。指示小组成员对一条腿上的指定测试位点施用表3中所描述类型的组合物,一天两次,持续12周(不认为表3制剂中的附加成分(即与上述五种活性物不同的成分)对以下表1和2中的数据有贡献)。在访视测试机构之前8小时,限制小组成员在其腿上施用任何保湿剂。使用配对t检验将在第4周、第8周和第12周获得的视觉评分分数变化和图像分析数据与基线进行比较。认为统计显著性在p值≤0.05。表1提供了关于专业评分的数据,表2提供了关于图像分析的数据。
表1(专业评分)
*在95%的置信水平与基线相比统计显著的;NS在95%的置信水平是不显著的。
**在基线处基于N=6
表2(图像分析)
*在95%的置信水平与基线相比统计显著的;NS在95%的置信水平是不显著的。
表31
1可以通过在相A中添加所有成分,接着添加相B成分,然后添加相C成分来制备。可以将相A加热至70至75℃,然后在搅拌下添加相B,接着在连续搅拌下添加相C,将混合物冷却至室温(大约20至25℃)并继续搅拌直到得到均匀凝胶。
2特殊变性(SD)醇为乙醇与变性剂(即苯甲地那铵)的混合物。
3由DSM(北美)销售。其为从荷花玉兰的茎皮中获得的提取物。
4由Bayer Sante Familiale SAS(法国)以商品名TECA(积雪草的滴定提取物)销售。提取物从积雪草的叶中获得。
5可以从多个来源获得(参见CTFA)。
6由Laboratoires Serobiologiques(法国)销售。其为水/剌阿干树(Argania spinosa)仁提取物/椰油酰谷氨酸钠/卡波姆的混合物。
7由为BASF(美国)的一部分的Cognis Corporation销售。其为来自豌豆植物的蛋白。
8由DSM(北美)以商品名销售。包含表没食子儿茶素没食子酸酯(EGCG)的绿茶提取物。
9由EMD Chemicals(美国)以商品名LureminTM销售。
10由Clariant(美国)销售。其为用作用于水性体系的凝胶剂和用作用于水包油乳液的组织形成剂和增稠剂的合成聚合物。
与基线相比,在第4周、第8周和第12周,蛛状静脉曲张用制剂明显地减少了蛛状静脉曲张周围的毛细血管颜色。与基线相比,在第4周、第8周和第12周,蛛状静脉曲张用膏霜明显地降低了蛛状静脉曲张周围的可视干燥度(在基线处N=6)。与基线相比,在第8周和第12周,蛛状静脉曲张用膏霜明显地减少了蛛状静脉曲张周围的毛细血管长度和毛细血管数量。
除了上述测试之外,本领域普通技术人员还可以使用表4和5中的测试载剂来确定该成分的组合对毛细管扩张的效果。
表4*
成分 | 浓度(以重量计)% |
相A | |
水 | 补足到100 |
黄原胶 | 0.1 |
M-苯甲酸酯 | 0.15 |
P-苯甲酸酯 | 0.1 |
柠檬酸 | 0.01 |
相B | |
鲸蜡醇 | 4.0 |
硬脂酸甘油酯+PEG100 | 4.0 |
棕榈酸辛酯 | 4.0 |
聚二甲基硅氧烷 | 1.0 |
生育酚乙酸酯 | 0.2 |
相C | |
有效成分** | 2.0 |
*将黄原胶撒入水中并混合10分钟。然后,添加相A中的所有成分并加热到70至75℃。添加相B中的所有条目到单独的烧杯中并加热到70至75℃。在70至75℃下混合相A和B。继续搅拌并使组合物冷却到30℃。然后,边搅拌边添加相C的成分。
**可以使用本说明书中所描述的任何活性成分(或其组合)。例如,活性成分可以包括积雪草提取物、葡萄籽提取物、木兰茎皮提取物、茶树提取物和/或二羟基甲基色酮、或其任意组合。虽然表1制剂中活性成分的总量为2%(w/w),但是预期可以增加或减少活性成分的量以获得预期的结果,其中水量可以相应地增加/减少(例如足量)。
表5*
成分 | 浓度(以重量计)% |
相A | |
水 | 补足到100 |
M-苯甲酸酯 | 0.2 |
P-苯甲酸酯 | 0.1 |
Na2EDTA | 0.1 |
牛油果脂 | 4.5 |
凡士林 | 4.5 |
甘油 | 4.0 |
丙二醇 | 2.0 |
Finsolve TN | 2.0 |
相B | |
Sepigel305 | 2.0 |
相C | |
有效成分** | 2.0 |
*将相A中的成分添加到烧杯中并边搅拌边加热到70至75℃。然后,将相B的成分与相A添加到一起并随着搅拌冷却到30℃。然后,边搅拌边添加相C的成分。
**可以使用本说明书中所描述的任何活性成分(或其组合)。例如,活性成分可以包括积雪草提取物、葡萄籽提取物、木兰茎皮提取物、茶树提取物和/或二羟基甲基色酮、或其任意组合。虽然表1制剂中活性成分的总量为2%(w/w),但是预期可以增加或减少活性成分的量以获得预期的结果,其中水量可以相应地增加/减少(例如足量)。
实施例2
(可以用于测试组合物的另外的分析)
本说明书和权利要求书全文所公开的成分的组合的功效可以通过使用以下分析来确定。
氧自由基吸收能力(ORAC)分析:测量成分或组合物的抗氧化活性的分析。本质上,其可以对抑制氧化剂、例如已知导致损伤细胞(例如皮肤细胞)的氧自由基的作用的程度及所用时间进行定量。本发明的组合物的ORAC值可以通过本领域普通技术人员已知的方法进行确定(参见美国公开2004/0109905号和2005/0163880号;Cao等人(1993),其全部通过引用并入)。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(B-PE)荧光下降的能力。
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MinoltaChroma 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。测定之后,立即用本发明的组合物处理该区域。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 DermalPhase Meter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。
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。肤色改变可以使用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。这用来确定组合物是否导致刺激。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Kligman Scale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:皮肤光滑度和周围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Hargens Ballistometer,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。皮肤的粘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线条覆盖的区域。
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:在其它非限制性方面,本发明的组合物的功效可以通过使用皮肤类似物,例如举例来说MELANODERMTM,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)(黑色素的前体)时明确地污染。皮肤类似物MELANODERMTM可以用各种含有本发明的组合物和增白剂的赋形剂进行处理,或仅使用赋形剂作为对照物。或者,未处理的皮肤类似物样品可以用作对照物。
ORAC分析:芳香的皮肤活性成分和组合物的氧自由基吸收(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。芳香的皮肤活性成分和组合物的ORAC值可以通过本领域普通技术人员已知的方法进行确定(参见美国公开号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(B-PE)荧光下降的能力。
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BioMolInternational的用于MMP3(AK-400)和MMP-9(AK-410)的比色药物发现试剂盒,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pH6.0和高于7时,ε=13600M-1cm-1)。
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本说明书中所公开和要求保护的所有皮肤活性成分、组合物或方法根据本公开不需要不合适的实验即可制成和实现。尽管本发明的皮肤活性成分、组合物或方法按照具体的实施方案进行了描述,但是对于本领域技术人员明显的是,可以对所述皮肤活性成分、组合物或方法以及在本文所描述方法的步骤或步骤的顺序中实施变化,而不脱离本发明的概念、精神和范围。
Claims (16)
1.一种处理毛细管扩张的方法,其包括对需要处理的皮肤局部地施用包含以下组分的组合物:
(a)来自积雪草、葡萄籽、木兰茎皮和茶树的提取物的组合;和
(b)二羟基甲基色酮。
2.权利要求1所述的方法,其中将所述组合物施用于蛛状静脉曲张。
3.权利要求1至2中任一项所述的方法,其中所述组合物在局部施用后在皮肤上保留至少5分钟。
4.权利要求1至3中任一项所述的方法,其中所述毛细管扩张存在于面部皮肤、腿部皮肤、踝部皮肤或臂部皮肤上。
5.权利要求1至4中任一项所述的方法,其中所述组合物为膏霜、凝胶或润肤露。
6.权利要求1所述的方法,其中所述组合物为乳液。
7.权利要求1至6中任一项所述的方法,其中所述组合物还包含保湿剂、紫外吸收剂、抗氧化剂、结构化剂、乳化剂、含硅酮的化合物、精油、增稠剂和防腐剂。
8.权利要求1至7中任一项所述的方法,其中所述组合物还包含毛叶杯轴花叶提取物。
9.权利要求1至8中任一项所述的方法,其中所述组合物包含:
-0.01重量%至1重量%的来自积雪草的提取物;
-0.01重量%至1重量%的来自葡萄籽的提取物;
-0.01重量%至1重量%的来自木兰茎皮的提取物;
-0.01重量%至1重量%的来自茶树的提取物;和
-0.01重量%至1重量%的二羟基甲基色酮。
10.权利要求1至9中任一项所述的方法,其中所述木兰茎皮提取物为包含和厚朴酚与厚朴酚的荷花玉兰茎皮提取物,其中所述积雪草提取物包含积雪草苷、羟基积雪草酸和积雪草酸,其中所述茶树提取物为包含表没食子儿茶素没食子酸酯的茶树叶提取物,并且其中所述葡萄籽提取物包含多酚。
11.一种局部护肤组合物,其包含:
(a)来自积雪草、葡萄籽、木兰茎皮和茶树的提取物的组合;和
(b)二羟基甲基色酮。
12.权利要求11所述的局部护肤组合物,其中所述组合物出现于患有毛细管扩张的皮肤上。
13.权利要求11至12中任一项所述的局部护肤组合物,其中所述组合物还包含保湿剂、紫外吸收剂、抗氧化剂、结构化剂、乳化剂、含硅酮的化合物、精油、增稠剂和/或防腐剂。
14.权利要求11至13中任一项所述的局部护肤组合物,其中所述组合物还包含毛叶杯轴花叶提取物。
15.权利要求11至14中任一项所述的局部护肤组合物,其中所述组合物包含:
-0.01重量%至1重量%的来自积雪草的提取物;
-0.01重量%至1重量%的来自葡萄籽的提取物;
-0.01重量%至1重量%的来自木兰茎皮的提取物;
-0.01重量%至1重量%的来自茶树的提取物;和
-0.01重量%至1重量%的二羟基甲基色酮。
16.权利要求11至15中任一项所述的局部护肤组合物,其中所述木兰茎皮提取物为包含和厚朴酚与厚朴酚的荷花玉兰茎皮提取物,其中所述积雪草提取物包含积雪草苷、羟基积雪草酸和积雪草酸,其中所述茶树提取物为包含表没食子儿茶素没食子酸酯的茶树叶提取物,并且其中所述葡萄籽提取物包含多酚。
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- 2012-12-10 DE DE202012013021.8U patent/DE202012013021U1/de not_active Expired - Lifetime
- 2012-12-10 KR KR1020147018936A patent/KR102099993B1/ko active IP Right Grant
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106420590A (zh) * | 2015-08-07 | 2017-02-22 | 玫琳凯有限公司 | 局部用化妆品组合物 |
JP2018538320A (ja) * | 2015-12-22 | 2018-12-27 | トレル、 ジャン ノエル | 乾癬、アトピー性皮膚炎、慢性蕁麻疹、抗ヒスタミン薬抵抗性掻痒、及び老人性掻痒の治療のためのアンボラエキス及び緑茶エキスを含む組成物 |
CN108478585A (zh) * | 2018-03-30 | 2018-09-04 | 上海璞萃生物科技有限公司 | 一种抗炎组合物及其制备方法和应用 |
CN115068389A (zh) * | 2022-07-22 | 2022-09-20 | 广州东森医药科技有限公司 | 一种多效组合物、精华霜及其制备方法 |
CN115068389B (zh) * | 2022-07-22 | 2024-04-19 | 广州东森医药科技有限公司 | 一种多效组合物、精华霜及其制备方法 |
Also Published As
Publication number | Publication date |
---|---|
EP2788010B1 (en) | 2018-10-24 |
DE202012013021U1 (de) | 2014-11-28 |
WO2013086518A1 (en) | 2013-06-13 |
EP2788010A1 (en) | 2014-10-15 |
US20130171283A1 (en) | 2013-07-04 |
US20200230195A1 (en) | 2020-07-23 |
HK1201047A1 (zh) | 2015-08-21 |
US10639344B2 (en) | 2020-05-05 |
US12016895B2 (en) | 2024-06-25 |
KR102099993B1 (ko) | 2020-04-10 |
KR20140101418A (ko) | 2014-08-19 |
EP2788010A4 (en) | 2015-06-17 |
CN103987394B (zh) | 2018-05-11 |
CA2858211C (en) | 2018-08-21 |
US20170065656A1 (en) | 2017-03-09 |
US9526689B2 (en) | 2016-12-27 |
CA2858211A1 (en) | 2013-06-13 |
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