CN111053730A - 化妆品组合物 - Google Patents
化妆品组合物 Download PDFInfo
- Publication number
- CN111053730A CN111053730A CN201911081227.2A CN201911081227A CN111053730A CN 111053730 A CN111053730 A CN 111053730A CN 201911081227 A CN201911081227 A CN 201911081227A CN 111053730 A CN111053730 A CN 111053730A
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- Prior art keywords
- skin
- extract
- composition
- ingredients
- dimethicone
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 164
- 239000002537 cosmetic Substances 0.000 title abstract description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 42
- 238000000034 method Methods 0.000 claims abstract description 35
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims abstract description 30
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims abstract description 30
- 230000000699 topical effect Effects 0.000 claims abstract description 28
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 28
- 239000004205 dimethyl polysiloxane Substances 0.000 claims abstract description 27
- 229940008099 dimethicone Drugs 0.000 claims abstract description 20
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- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 claims abstract description 12
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims abstract description 12
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- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 17
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- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 claims description 9
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- WYVVKGNFXHOCQV-UHFFFAOYSA-N 3-iodoprop-2-yn-1-yl butylcarbamate Chemical compound CCCCNC(=O)OCC#CI WYVVKGNFXHOCQV-UHFFFAOYSA-N 0.000 claims description 9
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- XMSXQFUHVRWGNA-UHFFFAOYSA-N Decamethylcyclopentasiloxane Chemical compound C[Si]1(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O1 XMSXQFUHVRWGNA-UHFFFAOYSA-N 0.000 claims description 9
- MVORZMQFXBLMHM-QWRGUYRKSA-N Gly-His-Lys Chemical compound NCCCC[C@@H](C(O)=O)NC(=O)[C@@H](NC(=O)CN)CC1=CN=CN1 MVORZMQFXBLMHM-QWRGUYRKSA-N 0.000 claims description 9
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Abstract
公开了化妆品组合物及其可以单独或以方案的形式组合使用的方法。本发明一般涉及多种皮肤制剂,其以治疗各种不同皮肤病况的方式结构化,具体涉及一种局部皮肤用组合物,其配制为精华并且能够增加皮肤的容量或紧致度,所述组合物包含:水、乙醇、一缩二丙二醇、甲基葡糖聚氧乙烯(20)醚、生物糖胶‑1、甘油、聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷交联聚合物、丁二醇、二乙烯基聚二甲基硅氧烷/聚二甲基硅氧烷共聚物、苯氧基乙醇、山梨糖醇、聚二甲基硅氧烷、二氧化硅、麦芽糖糊精、丙烯酸盐或酯/丙烯酸C10‑30烷基酯交联聚合物、1,2‑辛二醇、羟乙基纤维素、三乙醇胺、氯苯甘醚、泛醇、戊二醇和乙二胺四乙酸二钠。
Description
本申请是申请日为2013年5月29日、申请号为201310205053.2、发明名称为“化妆品组合物”的中国发明专利申请的分案申请。
技术领域
本发明一般涉及多种皮肤制剂,其以治疗各种不同皮肤病况的方式结构化。所述制剂可以单独或以方案的形式组合使用。
背景技术
许多因素促成皮肤老化,例如人的实际年龄、暴露于环境因素(例如阳光、污染、化学品、烟等)的量和人对其皮肤的护理程度。具体地,皮肤老化关系到两个过程——与自然老化过程和基因影响有关的内在老化,和由环境因素例如日照引起的外在的或累积的损伤。该因素组合最后导致可见的老化症状,并且随着时间的流逝这些症状发展经过三个阶段——早期、中期和晚期。
皮肤老化的早期症状包括可见细纹的第一阶段,尤其在眼睛周围,和不均匀肤色的开始。细胞更新开始变得缓慢,并且这会对肤色有致暗的影响。胶原蛋白和弹性蛋白——虽然仍然是健康的——会开始遭受早期损伤,使皮肤弹性稍微变弱。如果基体处于无保护的状态,则皮肤表面下形成的皱纹最后会由于皮层的损伤变得更加显而易见。偶尔眼睛看上去会肿胀,并且毛孔稍微显得更加显而易见。通常这发生在大约25到35岁的年龄范围。
皮肤老化的中期症状包括在眼睛、嘴周围和前额上更加明显的表情纹。在眼睛下面的黑眼圈可能变得更加显而易见。由于产生的胶原蛋白更少,因此皮肤的支撑结构变得,并且弹性蛋白纤维开始失去“迅速”恢复的能力更弱。皮肤更容易失去重要的水分,并且暗斑可能成为更大的问题。颈部的细纹可能变得更加可见,并且嘴两边的“木偶”纹会开始出现。老年斑开始浮现的越显著,眼睛会越频繁地看上去疲劳,并且毛孔显得越大。这通常发生在大约35到50岁的年龄范围。
皮肤老化的晚期症状包括“稳定的”深纹和甚至在面部休息时都可见的皱纹。胶原蛋白和弹性蛋白的支撑结构被严重地损害,并且皮肤下垂,尤其在面颊和下巴轮廓区域,变得明显。颈部显示出累积损伤的症状,皮肤变得松弛并以称为“年轮”的水平皱纹为特征。暗斑变得更加突出,并且眼部区域除了“下垂的”上眼睑之外会显示出显而易见的幼纹、下垂、浮肿和更加明显的黑眼圈。由于天然缓冲的损失,皮肤失去其年轻的容量和提升力,并且由于外部屏障被损害、油脂产生变慢和内部水分水平下降,因此皮肤干燥更加明显。细胞更新显著地变慢,并且死皮细胞留在皮肤表面,这可能使肤色变暗并使毛孔更加显而易见。皮肤的厚度也受到影响,并且随着其变薄,更容易受到刺激。通常这发生在50岁以上的年龄范围。
目前市场上的产品要么不能有效地处理老化的皮肤,要么对皮肤有刺激作用。然而,本发明人发现了一系列独特的制剂,其可以用于治疗各种不同的皮肤病况。此外,该制剂对通常呈现中期和/或晚期皮肤老化的成熟型皮肤尤其有效。
发明内容
本发明人发现的多种制剂可以用于所有类型的皮肤。然而,在具体的方面,发现所述制剂对中期到晚期皮肤老化的皮肤有特别好的效果。此外,当所述制剂以方案的形式使用时可以获得额外的益处。组合物包括精华和多种乳霜。
在一个实施方案中,公开了一种局部皮肤用组合物,其配制为精华并且能够增加皮肤的容量或紧致度。所述组合物可包含:水、乙醇、一缩二丙二醇、甲基葡糖聚氧乙烯(20)醚、生物糖胶-1、甘油、聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷交联聚合物、丁二醇、二乙烯基聚二甲基硅氧烷/聚二甲基硅氧烷共聚物、苯氧基乙醇、山梨糖醇、聚二甲基硅氧烷、二氧化硅、麦芽糖糊精、丙烯酸盐或酯/丙烯酸C10-30烷基酯交联聚合物、1,2-辛二醇、羟乙基纤维素、三乙醇胺、氯苯甘醚、泛醇、戊二醇和/或乙二胺四乙酸二钠中的任一种、任意组合或全部。在某些方面,所述组合物还可以包含:C12-14烷基聚氧乙烯(12)醚、羟丙基环糊精、刺海门冬(Asparagopsis armata)提取物、黑麦籽(Secale Cereale)提取物、积雪草(Centellaasiatica)分生组织细胞培养物、刺阿干树(Argania spinosa)仁提取物、C12-13烷基聚氧乙烯(23)醚、C12-13烷基聚氧乙烯(3)醚、腺苷、黑莓叶(Rubus fruticosus)提取物、PEG-20失水山梨醇椰油酸酯、泡叶藻(Ascophyllum nodosum)提取物、红豆蔻(Alpinia galanga)叶提取物、软毛松藻(Codium tomentosum)提取物、椰油酰基谷氨酸钠、丁基氨基甲酸碘代丙炔酯、交替单胞菌(Alteromonas)发酵产物滤液、黄原胶、卡波姆、三(辛酸/癸酸)甘油酯、山梨酸钾、仙人果(Opuntia tuna)果实提取物、柠檬酸、苯甲酸钠、葡聚糖和/或三肽-1中的任一种、任意组合或全部。所述组合物内成分的量可以改变(例如,该量可以低至0.000001%,高至70%w/w,或其间的任意范围)。在一个实施方案中,所述组合物包含60%到70%w/w的水、5%到10%w/w的乙醇、5%到10%w/w的一缩二丙二醇、2%到5%w/w的甲基葡糖聚氧乙烯(20)醚和/或2%到5%w/w的生物糖胶-1。还公开了一种增加皮肤容量或紧致度的方法,包括对有此需求的皮肤局部施用所述组合物,其中皮肤的容量或紧致度增加。
在另一个实施方案中,公开了一种局部皮肤用组合物,其配制为在夜间或者睡眠时使用的乳霜,所述局部皮肤用组合物包含:水、甘油、氢化聚癸烯、环戊硅氧烷、鲸蜡硬脂醇、一缩二丙二醇、牛油果脂、硬脂酸甘油酯、三(辛酸/癸酸)甘油酯、硬脂酸异鲸蜡醇酯、丁二醇、三异硬脂酸聚甘油(2)酯、苯氧基乙醇、PEG-100硬脂酸酯、聚甲基丙烯酸甲酯、鲸蜡硬脂基葡糖苷、聚二甲基硅氧烷、三辛酸甘油酯、氯苯甘醚、三乙醇胺、卡波姆和/或乙二胺四乙酸二钠中的任一种、任意组合或全部。所述组合物还可以包含:BHT、羟丙基环糊精、视黄醇、积雪草分生组织细胞培养物、环己硅氧烷、腺苷、红豆蔻叶提取物、戊二醇、石榴(Punicagranatum)提取物、软毛松藻提取物、肉桂(Cinnamomum cassia)树皮提取物、光果甘草(Glycyrrhiza glabra)根提取物、丁基氨基甲酸碘代丙炔酯、环丁硅氧烷、1,2-辛二醇、黄原胶、山梨酸、仙人果果实提取物、山梨酸钾、苯甲酸钠、柠檬酸、葡聚糖和三肽-1中的任一种、任意组合或全部。所述组合物内成分的量可以改变(例如,该量可以低至0.000001%w/w,高至60%w/w,或其间的任意范围)。在一个实施方案中,所述组合物包含50%到60%w/w的水、10%到15%w/w的甘油、3%到7%w/w的氢化聚癸烯、3%到7%w/w的环戊硅氧烷和/或3%到7%w/w的鲸蜡硬脂醇。还公开了一种滋润皮肤或增加皮肤紧致度的方法,包括对有此需求的皮肤局部施用所述组合物,其中对皮肤的局部施用增加皮肤湿润度或增加皮肤紧致度。
在另一方面,公开了一种局部皮肤用组合物,其配制为能够减少黑眼圈或者肿眼泡的出现的乳霜,所述局部皮肤用组合物包含:水、甘油、矿物油、凡士林、氢化聚癸烯、鲸蜡酯、双-二甘油多酰基己二酸酯-2、丁二醇、氢化聚异丁烯、橄榄油酸失水山梨醇酯、橄榄油酸鲸蜡硬脂醇酯、棕榈酸鲸蜡醇酯、鲸蜡硬脂醇、棕榈酸失水山梨醇酯、抗坏血酸四己基癸酯、二氧化硅、十六/十八醇聚氧乙烯(20)醚、重氮烷基脲、乙酸生育酚酯、三乙醇胺、积雪草提取物、丙烯酸盐或酯/丙烯酸C10-30烷基酯交联聚合物、厚朴(Magnolia officinalis)树皮提取物和/或丙二醇中的任一种、任意组合或全部。在另外的方面、所述组合物也可以包含:羟丙基环糊精、乙烯/甲基丙烯酸盐或酯共聚物、乙二胺四乙酸二钠、橙皮苷甲基查尔酮、腺苷、硬脂基聚氧乙烯(20)醚、豌豆(Pisum sativum)提取物、苯氧基乙醇、三异硬脂酸钛异丙酯、柠檬酸钠、柚(citrus grandis)皮提取物、丁基氨基甲酸碘代丙炔酯、积雪草分生组织细胞培养物、望春花(Magnolia biondii)花蕾/花提取物、二葡萄糖酸洗必泰、山梨酸钾、二肽-2、苯甲酸钾、柠檬酸、仙人果果实提取物、棕榈酰四肽-7、苯甲酸钠、葡聚糖、三肽-1和黄原胶中的任一种、任意组合或全部。所述组合物内成分的量可以改变(例如,该量可以低至0.000001%,高至55%w/w,或其间的任意范围)。在一个实施方案中,所述组合物包含45%到55%w/w的水、7%到12%w/w的甘油、5%到10%w/w的矿物油、5%到10%w/w的凡士林和3%到7%w/w的氢化聚癸烯。还公开了一种减少人脸的眶周区中黑眼圈或浮肿出现的方法,包括对有此需求的皮肤局部施用所述组合物,其中局部施用减少人脸的眶周区中黑眼圈或浮肿的出现。
还公开了一种增加真皮-表皮连接(“DEJ”)完整性的方法,其包括对皮肤局部施用成分的组合或在本说明书的全文中所公开的具有所述组合的组合物中的任一。该方法可以在真皮和表皮细胞中刺激产生蛋白和酶,这有助于使真皮层连接到表皮层。
本发明的组合物还可以包含以下附加成分中的任一种、任意组合或全部:水、螯合剂、保湿剂、防腐剂、增稠剂、含有硅酮的化合物、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。在某些方面,所述组合物可包含至少二、三、四、五、六、七、八、九、十种或全部在上一句中确定的这些附加成分。这些附加成分的非限制性实例在本说明书的全文中进行确定,并通过引用并入该章节。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%,或者是在中间的如本说明书其他章节中所公开的任意的整数或范围,其以引用的方式并入本段。
也考虑了包含本发明的组合物的试剂盒。在某些实施方案中,所述组合物包含在容器中。所述容器可以是瓶子、分配器或包装。所述容器可以分配预定量的组合物。在某些方面,所述组合物以喷雾、团块或液体分配。所述容器在其表面可包含标记。所述标记可以是字词、缩写、图片或符号。
还考虑了在本说明书的全文中所公开的组合物可以用作保留型或洗去型组合物。举例来说,保留型组合物可以是对皮肤局部施用的,并在皮肤上保持一段时间(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)。或者,洗去型组合物可以是打算施用于皮肤并然后在一段时间内,如小于5、4、3、2或1分钟,(比如用水)从皮肤移除或洗去的产品。洗去型组合物的例子可以是洗面奶、洗发水、护发素或皂。保留型组合物的例子可以是皮肤保湿霜、防晒霜、面膜、晚霜或日霜。
期望对于本发明的任何方法或组合物,可以实施本说明书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,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质,或组合物的水分保留性质。
“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”包含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。本发明的局部皮肤护理组合物可以具有选定的粘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,并且在非限制性实施方案中该术语定义为在10%以内,优选地在5%以内,更优选地在1%以内,最优选地在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,并且在一个非限制性实施方案中,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。
术语“抑制”或“减少”或这些术语的任何变体包括为了达到预期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为了达到预期结果的任何可测量的蛋白质或分子(举例来说,基质蛋白,例如纤维粘连蛋白、层粘连蛋白、胶原蛋白或弹性蛋白,或者分子,例如透明质酸)的增加或产生。
术语“有效的”,作为本发明书和/或权利要求所使用的术语,表示适于实现希望的、期望的或预期的结果。
当在权利要求书和/或说明书中与术语“包含”、“具有”、“包括”或“含有”一起使用时,要素前面不使用量词可以表示“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书所用,词语“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。
使用的组合物和方法可以“包含”、“基本上由…组成”或“由…组成”任何在本说明书的全文所公开的成分或步骤。对于过渡词“基本上由……组成”,在一个非限制性方面,本说明书所公开的基本的或新的组合物和方法包括组合物滋润皮肤和/或增加皮肤紧致度的能力。
本发明的其他目标、特征和优点通过下面的详细描述会变得显而易见。然而,应理解详细的描述和实施例表明本发明的特定实施方案时仅以举例说明给出。另外,期望在通过该详细描述,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显而易见。
具体实施方式
皮肤处于退化和更新的常态中,对于年轻人的皮肤该过程处于最优平衡状态。然而,随着年龄增长,时序和环境因素开始压垮皮肤,真皮基质开始退化比更新更快,因此打乱该微妙的平衡。
皮肤基质承担皮肤的结构完整性、机械弹性和稳定性的责任。皮肤基质的退化在皱纹和皮肤老化的其他症状中起重要的作用。皮肤基质一些更知名的组分包括结构蛋白(最著名的胶原蛋白和弹性蛋白),其对皮肤的健康和青春活力非常重要。另外的蛋白质对皮肤的结构和稳定性也是关键的。层粘连蛋白和纤维粘连蛋白是真皮-表皮连接(DEJ)(也被称为基膜)中主要的蛋白质。DEJ位于真皮和表皮联结之间,形成叫做网脊的指状突出。表皮细胞从真皮的血管中接收其养分。网脊增大暴露于这些血管和所需养分的表皮的表面积。DEJ提供两种组织室的粘连,并控制皮肤的结构完整性。层粘连蛋白和纤维粘连蛋白是位于DEJ中的两种结构糖蛋白。考虑到将细胞保持在一起的胶,真皮成纤维细胞分泌层粘连蛋白和纤维粘连蛋白,以帮助促进表皮细胞到DEJ的细胞内和细胞间粘连。
虽然胶原蛋白和弹性蛋白纤维给皮肤提供抗张强度,但是随着时间流逝它们不能提供组织需要的弹性。除了结构蛋白的框架之外,皮肤基质还需要适当的填充物,其提供机械缓冲、保持水分和增强屏障功能。主要的皮肤基质填充物为多糖,包括透明质酸(也被称为玻尿酸、透明质酸盐/酯或HA)在内的一类葡萄糖基聚合物。HA是皮肤细胞外基质的主要组分。较大量水与HA的水合是保持皮肤正常水合的一种机制。此外,减少的HA的量可以导致老化的皮肤以更加加快的速度出现。在这点上,HA具有若干功能,包括结合水以帮助保持皮肤水分、降低细胞外液的渗透性以及支持皮肤的机械弹性和柔韧性。皮肤内HA的含量(在青春期或早期成年期的峰值后)随着年龄降低。这是水分损失的原因,并且皮肤变得更薄且更不柔韧。HA的损失还会降低皮肤自我修复的能力,并有可能影响其他皮肤基质组分的合成和沉积形式。
除了正常老化过程之外,皮肤中HA的量还可以受透明质酸酶(一种降解HA的酶)的影响。降低HA的活性会有效地增加皮肤中存在的HA的总量。
考虑到该背景,本发明人发现多种可以用于在皮肤内保护皮肤基质蛋白和HA的制剂。这些制剂可以单独或以基于方案的形式使用。
A.精华制剂
化妆品精华具有渗透进入皮肤深层的能力。该制剂通常是“较轻的”制剂,这是因为其与例如皮肤保湿霜相比时具有更低的粘度。
本发明的精华制剂可以在清洁皮肤之后和施用保湿霜之前使用。该制剂设计为恢复皮肤紧致度、容量和提升力(见实施例1)。其可包含水、乙醇、一缩二丙二醇、甲基葡糖聚氧乙烯(20)醚、生物糖胶-1、甘油、聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷交联聚合物、丁二醇、二乙烯基聚二甲基硅氧烷/聚二甲基硅氧烷共聚物、苯氧基乙醇、山梨糖醇、聚二甲基硅氧烷、二氧化硅、麦芽糖糊精、丙烯酸盐或酯/丙烯酸C10-30烷基酯交联聚合物、1,2-辛二醇、羟乙基纤维素、三乙醇胺、氯苯甘醚、泛醇、戊二醇和乙二胺四乙酸二钠。此外,可以添加附加成分以获得期望的触觉性质和/或获得特别的皮肤益处(见实施例1)。
B.乳霜制剂
化妆品乳霜具有滋润皮肤的能力。当与精华相比时它们趋于具有“较重的”感觉,并一般配制为水包油的乳液。
在一个实施方案中,公开了一种乳霜制剂,其设计为在夜间或睡眠时使用。该制剂具有改善老化的晚期症状、紧致皮肤、均匀肤色和恢复皮肤“年轻的”缓冲的能力(见实施例2)。其可包含水、甘油、氢化聚癸烯、环戊硅氧烷、鲸蜡硬脂醇、一缩二丙二醇、牛油果脂、硬脂酸甘油酯、三(辛酸/癸酸)甘油酯、硬脂酸异鲸蜡醇酯、丁二醇、三异硬脂酸聚甘油(2)酯、苯氧基乙醇、PEG-100硬脂酸酯、聚甲基丙烯酸甲酯、鲸蜡硬脂基葡糖苷、聚二甲基硅氧烷、三辛酸甘油酯、氯苯甘醚、三乙醇胺、卡波姆和乙二胺四乙酸二钠。此外,可以添加附加成分以获得期望的触觉性质和/或获得特别的皮肤益处(见实施例2)。
在一个另外的实施方案中,公开了一种乳霜,其设计用于眼睛周围(眶周区)的皮肤。乳霜可以以此方式设计以用于人脸的眶周区中更薄的和更敏感的皮肤。发现该制剂可以最小化下眼袋和黑眼圈的出现(见实施例3)。该制剂可包含水、甘油、矿物油、凡士林、氢化聚癸烯、鲸蜡酯、双-二甘油多酰基己二酸酯-2、丁二醇、氢化聚异丁烯、橄榄油酸失水山梨醇酯、橄榄油酸鲸蜡硬脂醇酯、棕榈酸鲸蜡醇酯、鲸蜡硬脂醇、棕榈酸失水山梨醇酯、抗坏血酸四己基癸酯、二氧化硅、十六/十八醇聚氧乙烯(20)醚、重氮烷基脲、乙酸生育酚酯、三乙醇胺、积雪草提取物、丙烯酸盐或酯/丙烯酸C10-30烷基酯交联聚合物、厚朴树皮提取物和丙二醇。此外,可以添加附加成分以获得期望的触觉性质和/或获得特别的皮肤益处(见实施例3)。
C.成分的量
期望本发明的组合物可以包含任意量的本说明书所讨论成分。该组合物还可包含任意数目的在本说明书的全文中所描述的附加成分的组合(例如,色素或附加的化妆品或药物成分)。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书中所提及的成分。在非限制性方面,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应当理解,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.载体
本发明的组合物可以并入所有类型的载体。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)、乳霜、洗剂、溶液(水的或者水-醇的)、无水基底(例如唇膏和粉)、凝胶和软膏。变体和其它合适的载体对于熟练技术人员是显而易见的,并且适用于本发明。在某些方面,化合物、成分和试剂的浓度和组合以如此的方式进行挑选,使得该组合化学相容并且不形成从最终产物中沉淀出来的络合物。
E.附加成分
除了本发明人所公开的成分组合之外,组合物还可以包含额外的成分,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小节中进行描述。
1.化妆品成分
CTFA国际化妆品成分词典和手册(2004和2008)描述了多种多样的可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)、微量金属(例如锌、钙和硒)、抗刺激物(例如类固醇和非固醇类抗炎药)、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(例如山梨糖醇、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)。若干这些附加成分的非限制性实例在以下小节中提供。
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酯类(甘油基PABA、戊基二甲基PABA和辛基二甲基PABA)、丁基PABA、乙基PABA、乙基二羟基丙基PABA、二苯甲酮类(氧苯酮、磺异苯酮、二苯甲酮和二苯甲酮-1到12)、肉桂酸酯类(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、二异丙基甲基肉桂酸酯、DEA-甲氧基肉桂酸酯、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)、肉桂酸酯类、水杨酸酯类(均甲基水杨酸酯、水杨酸苄酯、乙二醇水杨酸酯、异丙基苄基水杨酸酯等)、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己基苯甲酸酯、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异戊基4-甲氧基肉桂酸酯。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、聚甘油山梨糖醇、吡咯烷酮羧酸的盐类、PCA钾、丙二醇、葡糖醛酸钠、PCA钠、山梨糖醇、蔗糖、海藻糖、脲和木糖醇。
其他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、芦荟、芦荟提取物、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、屏障鞘脂类、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(euphorbiacerifera)蜡、菜籽油、三(辛酸/癸酸)甘油酯、豆蔻(elettaria cardamomum)油、巴西棕榈(copernicia cerifera)蜡、胡萝卜(daucus carota sativa)油、蓖麻(ricinus communis)油、神经酰胺、地蜡、鲸蜡硬脂醇聚醚-5、鲸蜡硬脂醇聚醚-12、十六/十八醇聚氧乙烯(20)醚、鲸蜡硬脂醇辛酸酯、鲸蜡醇聚醚-20、鲸蜡醇聚醚-24、鲸蜡醇乙酸酯、鲸蜡醇辛酸酯、棕榈酸鲸蜡醇酯、洋甘菊(anthemis nobilis)油、胆固醇、胆固醇酯类、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、脂肪酸类、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、脂肪酸类、斑点老鹳草油、葡萄糖胺、葡糖谷氨酸酯、谷氨酸、甘油聚醚-26、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、鸭油酸甘油酯、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(corylusamericana)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、清华椰子油、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、羊毛脂醇聚醚-16、羊毛脂醇聚醚-10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(chamomillarecutita)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、磷脂类、多氨基酸多糖缩合物、聚甘油-3二异硬脂酸酯、聚季铵盐-24、聚山梨糖醇酯20、聚山梨糖醇酯40、聚山梨糖醇酯60、聚山梨糖醇酯80、聚山梨糖醇酯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(oryzasativa)糠油、RNA、迷迭香(rosmarinus officinalis)油、玫瑰油、红花(carthamustinctorius)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、山梨糖醇、大豆(glycine soja)油、鞘脂类、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、硬脂基甘草亭酸酯、硬脂基庚酸酯、硬脂基硬脂酸酯、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、俞酸甘油酯、十三烷醇新戊酸酯、十三烷醇硬脂酸酯、三乙醇胺、三硬脂酸甘油酯、脲、植物油、水、蜡类、小麦(triticum vulgare)胚芽油和依兰(cananga odorata)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、二十三烷醇硫代二丙酸酯、没食子酸月桂酯、异抗坏血酸、抗坏血酸酯类、阿魏酸乙酯、阿魏酸、没食子酸酯类、氢醌、巯基乙酸异辛酯、曲酸、抗坏血酸镁、抗坏血酸磷酸酯镁盐、甲基硅烷醇抗坏血酸、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、醌类、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、山梨糖醇缩糠醛、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、生育酚聚醚-5、生育酚聚醚-10、生育酚聚醚-12、生育酚聚醚-18、生育酚聚醚-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
在其他非限制性方面,本发明的组合物可包含结构化剂。在某些方面,结构化剂帮助给组合物提供流变学特征以促进组合物的稳定性。在其他方面,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、具有平均大约1到21个环氧乙烷单元的硬脂醇的聚乙二醇醚、具有平均大约1到5个环氧乙烷单元的鲸蜡醇的聚乙二醇醚及其混合物。
e.乳化剂
在本发明的某些方面,所述组合物不包含乳化剂。然而,在其他方面,所述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剂型和乳液的稳定性。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;4,421,769;3,755,560)。非限制性实例包括甘油酯类、丙二醇酯类、丙二醇的脂肪酸酯类、聚丙二醇的脂肪酸酯类、山梨糖醇的酯类、失水山梨醇酐酯类、羧酸共聚物、葡萄糖酯类和醚类、乙氧基化的酯类、乙氧基化的醇类、磷酸烷基酯类、聚氧乙烯脂肪醚磷酸酯类、脂肪酸酰胺类、酰基乳酸酯类、脂肪酸盐类、TEA硬脂酸酯、DEA油醇聚醚-3磷酸酯、聚乙二醇20失水山梨醇单月桂酸酯(聚山梨糖醇酯20)、聚乙二醇5大豆甾醇、硬脂醇聚醚-2、硬脂基聚氧乙烯(20)醚、硬脂醇聚醚-21、十六/十八醇聚氧乙烯(20)醚、PPG-2甲基葡萄糖醚二硬脂酸酯、鲸蜡醇聚醚-10、聚山梨糖醇酯80、鲸蜡醇磷酸酯、鲸蜡醇磷酸酯钾、二乙醇胺鲸蜡醇磷酸酯、聚山梨糖醇酯60、甘油硬脂酸酯、PEG-100硬脂酸酯及其混合物。
f.含有硅酮的化合物
在非限制性方面,含有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-键的长度、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有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类(例如挥发性和非挥发性油类)、凝胶类和固体类。在某些方面,含有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他任何给定比例的有机硅氧烷材料,以根据预期的施用(举例来说,对特别区域例如皮肤、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);低粘度聚二甲基硅氧烷类,即粘度大约为50cst或更低的聚二甲基硅氧烷(举例来说,聚二甲基硅氧烷类,例如道康宁200-0.5cst流体)。道康宁流体可以从密歇根州米德兰的道康宁公司购得。在CTFA化妆品成分词典的第三版中,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聚合物。在本发明的环境下可以使用的其他非限制性挥发性硅油包括从纽约州沃特福德的通用电器公司的硅酮产品部门和密歇根州艾德里安的史托福石化公司的SWS硅酮部门购得的那些。
g.精油
精油包括源自药草、花朵、树木和其他植物的油。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若干方法进行提取(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)。当这些类型的油类暴露于空气时,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)和其他有机溶剂。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源于玫瑰或薄荷植物。在本发明的环境下可以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。也考虑了本领域技术人员已知的其他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粘度的物质。增稠剂包括可以增加组合物粘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。在本发明的某些方面,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。
在本发明的环境下可以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、多糖和胶类。羧酸聚合物的实例包括含有一种或更多种源自丙烯酸的单体的交联化合物、取代的丙烯酸类和这些丙烯酸类和取代的丙烯酸类的盐和类,其中交联剂含有两种或两种以上碳-碳双键,并源自多元醇(参见美国专利5,087,445;4,509,949;2,798,053;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和非离子的聚合物。在美国专利5,100,660;4,849,484;4,835,206;4,628,078;4,599,379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醚-7、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直链或支链醇类与羟烷基纤维素的醚。其他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类的非限制性实例包括阿拉伯树胶、琼脂、藻胶、藻酸、藻酸铵、支链淀粉、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))、对羟基苯甲酸酯类(例如对羟基苯甲酸酯类和对羟基苯甲酸丙酯类)、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
也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、用于治疗酒渣鼻的试剂、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、烧伤治疗剂、烧灼剂、脱色剂、脱毛剂、尿布疹治疗剂、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、口疮治疗剂、唇疱疹治疗剂、牙科或牙周治疗剂、光敏感活性物、皮肤保护剂/屏障剂、包括激素和皮质激素类的类固醇、晒伤治疗剂、遮光剂、经皮活性物、鼻活性物、阴道活性物、疣治疗剂、创伤治疗剂、创伤愈合剂等。
F.试剂盒
还预期试剂盒用于本发明的某些方面。例如,本发明的组合物可以包括在试剂盒内。试剂盒可以包含容器。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、唇膏容器、压缩容器、能够保存化妆品组合物的化妆品盘或其他类型的容器,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。所述试剂盒和/或容器在其表面可包含标记。举例来说,所述标记可以是字词、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)分配发期望量的组合物。组合物可以分配为喷雾、气溶胶、液体、流体或半固体。所述容器可以具有喷雾、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某些非限制性方面。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公开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,在所公开的特定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
(精华)
表1的制剂是设计用于处理面部、颈部和眼部皮肤的精华。
表1*
*制剂可以通过在加热到70-75℃的条件下混合所有成分然后连续搅拌并冷却到室温(约20-25℃)进行制备。
**该精华中所用附加成分包括:C12-14烷基聚氧乙烯(12)醚、羟丙基环糊精、刺海门冬提取物、黑麦籽提取物、积雪草分生组织细胞培养物、刺阿干树仁提取物、C12-13烷基聚氧乙烯(23)醚、C12-13烷基聚氧乙烯(3)醚、腺苷、黑莓叶提取物、PEG-20失水山梨醇椰油酸酯、泡叶藻提取物、红豆蔻叶提取物、软毛松藻提取物、椰油酰基谷氨酸钠、丁基氨基甲酸碘代丙炔酯、交替单胞菌发酵产物滤液、黄原胶、卡波姆、三(辛酸/癸酸)甘油酯、山梨酸钾、仙人果果实提取物、柠檬酸、苯甲酸钠、葡聚糖和三肽-1。
表1的精华制剂通过多位女性在四周的时间内每天局部施用一次进行测试。研究结果为:使用1周后,80%的女性表示所述精华提供显著的提升感,并且88%说其有助于补充皮肤水分。使用2周后,78%表示下颌轮廓区域出现提升,81%表示所述精华使面部轮廓清楚和完美,82%表示其使下垂的皮肤变得紧致和紧实,以及79%表示其有助于逆转缓冲的损失。使用4周后,82%的女性表示所述精华提供持续全天的提升,以及79%表示颈部区域看上去变得紧致。
实施例2
(晚霜)
表2的制剂是设计用于在夜间或睡眠时间处理皮肤的乳霜。
表2*
| 成分 | 浓度%(以重量计) |
| 水 | 53 |
| 甘油 | 11 |
| 氢化聚癸烯 | 6 |
| 环戊硅氧烷 | 6 |
| 鲸蜡硬脂醇 | 6 |
| 一缩二丙二醇 | 4 |
| 牛油果脂 | 3 |
| 硬脂酸甘油酯 | 2 |
| 三(辛酸/癸酸)甘油酯 | 2 |
| 硬脂酸异鲸蜡醇酯 | 1 |
| 丁二醇 | 1 |
| 三异硬脂酸聚甘油(2)酯 | 0.9 |
| 苯氧基乙醇 | 0.9 |
| PEG-100硬脂酸酯 | 0.8 |
| 聚甲基丙烯酸甲酯 | 0.6 |
| 鲸蜡硬脂基葡糖苷 | 0.6 |
| 聚二甲基硅氧烷 | 0.5 |
| 三辛酸甘油酯 | 0.2 |
| 氯苯甘醚 | 0.2 |
| 三乙醇胺 | 0.2 |
| 卡波姆 | 0.1 |
| 乙二胺四乙酸二钠 | 0.1 |
| 附加成分<sup>**</sup> | 适量 |
*制剂可以通过在加热到70-75℃的条件下混合所有成分然后连续搅拌并冷却到室温(约20-25℃)进行制备。
**该乳霜中所用附加成分包括:BHT、羟丙基环糊精、视黄醇、积雪草分生组织细胞培养物、环己硅氧烷、腺苷、红豆蔻叶提取物、戊二醇、石榴提取物、软毛松藻提取物、肉桂树皮提取物、光果甘草根提取物、丁基氨基甲酸碘代丙炔酯、环丁硅氧烷、1,2-辛二醇、黄原胶、山梨酸、仙人果果实提取物、山梨酸钾、苯甲酸钠、柠檬酸、葡聚糖和三肽-1。
实施例3
(眼霜)
表3的制剂是设计用于处理眼部周围(人脸的眶周区)皮肤的乳霜。
表3*
*制剂可以通过在加热到70-75℃的条件下混合所有成分然后连续搅拌并冷却到室温(约20-25℃)进行制备。
**该乳霜中所用附加成分包括:羟丙基环糊精、乙烯/甲基丙烯酸盐或酯共聚物、乙二胺四乙酸二钠、橙皮苷甲基查尔酮、腺苷、硬脂基聚氧乙烯(20)醚、豌豆提取物、苯氧基乙醇、三异硬脂酸钛异丙酯、柠檬酸钠、柚皮提取物、丁基氨基甲酸碘代丙炔酯、积雪草分生组织细胞培养物、望春花花蕾/花提取物、二葡萄糖酸洗必泰、山梨酸钾、二肽-2、苯甲酸钾、柠檬酸、仙人果果实提取物、棕榈酰四肽-7、苯甲酸钠、葡聚糖、三肽-1和黄原胶。
表3的眼霜制剂通过多位女性在四周时间内每天局部施用一次进行测试。研究结果为:使用1周后,79%的女性表示该乳霜有助于眼部区域看上去更加提升,78%表示其有助于减少眼下浮肿,以及75%表示其有助于使眼角鱼尾纹减到最少。使用2周后,83%的女性表示该乳霜最小化黑眼圈,80%表示其使眼睛周围下垂的皮肤紧致,以及79%表示其最小化深纹的出现。使用4周后,81%的女性表示眼皮耷拉出现的更少,76%表示眼部区域看上去显著地更加年轻,94%表示其有助于修复皮肤的外观,以及86%表示皮肤重新获得青春的弹性。
实施例4
(附加分析)
附加分析,其可以用于确定任一成分或任何成分组合或贯穿说明书和权利要求书所公开的具有所述成分组合的组合物的功效,可以通过本领域普通技术人员已知的方法进行确定。以下是可以在本发明的环境下使用的非限制性分析。应认识到,可以使用其他测试过程,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,所述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。抑制黑素生成对于防止皮肤变黑和减轻与年龄有关的暗斑是有益的。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成的效果。该分析的末端是黑色素生成和细胞活性的光谱光度测量。B16-F1黑素细胞可以在37℃下10%的CO2中在标准DMEM生长基质中以10%的胎牛血清(Mediatech)进行培养,然后用任一活性成分、成分组合或说明书所公开的具有所述成分组合的组合物处理6天。培养之后,通过405nm处的吸收测量黑色素分泌,并对细胞活性进行定量。
胶原蛋白刺激分析:胶原蛋白是一种对皮肤结构关键的胞外基质蛋白。增加的胶原蛋白合成有助于改善皮肤的紧致度和弹性。该生物分析可以用于检验任一活性成分、成分组合或说明书所公开的具有所述成分组合的组合物对人类表皮纤维母细胞中产生原胶原蛋白肽(胶原蛋白的前体)的效果。该分析的末端是反应原胶原蛋白肽和细胞活性的光谱光度测量。分析采用定量的夹心酶免疫分析技术,通过在微孔板上预先涂上对原胶原蛋白肽有特异性的单克隆抗体。标样和样品可以吸移到孔中,任何存在的原胶原蛋白肽都会和固定的抗体结合。洗去所有未结合的物质后,可以将对原胶原蛋白肽有特异性的酶联多克隆抗体加入到孔中。清洗出去所有未结合的抗体-酶试剂,可以将底物溶液加入孔中,颜色正比于最初步骤中结合的原胶原蛋白肽的量显现,使用微孔板测定仪在450nm处进行检测。可以停止显色,并对颜色的强度进行测量。在37℃下10%的CO2中在标准DMEM生长基质中以10%的胎牛血清(Mediatech)进行培养的次融合的正常成人表皮纤维母细胞(CascadeBiologics),可以用成分组合或说明书所公开的具有所述成分组合的组合物中的每一种处理3天。培养后,可以收集细胞培养基质,原胶原蛋白肽分泌的量使用来自Takara(#MK101)的夹心酶联免疫吸附分析(ELISA)进行定量。
肿瘤坏死因子-α(TNF-α)分析:TNF总科的原型配体,TNF-α,是一种在炎症中起主要作用的多效性细胞因子。其表达的增加与促炎症活性的上调有关。该生物分析可以用于分析任一活性成分、成分组合或说明书所公开的具有所述成分组合的组合物对人类表皮角质细胞中产生TNF-α的效果。该分析的末端可以是反应TNF-α和细胞活性的光谱光度测量。分析采用定量的夹心酶免疫分析技术,通过在微孔板上预先涂上对TNF-α有特异性的单克隆抗体。标样和样品可以吸移到孔中,任何存在的TNF-α都会和固定的抗体结合。洗去所有未结合的物质后,可以将对TNF-α有特异性的酶联多克隆抗体加入到孔中。清洗出去所有未结合的抗体-酶试剂,可以将底物溶液加入孔中,颜色正比于最初步骤中结合的TNF-α的量显现,使用微孔板测定仪在450nm处进行检测。可以停止显色,并对颜色的强度进行测量。在37℃下5%的CO2中在EpiLife标准生长基质(Cascade Biologics)中进行培养的次融合的正常成人角质细胞(Cascade Biologics),可以用佛波醇12-豆蔻酸酯13乙酸酯(PMA,10ng/ml,Sigma Chemical,#P1585-1MG)或任一活性成分、成分组合或说明书所公开的具有所述成分组合的组合物处理6小时。PMA显示导致TNF-α分泌的显著增加,所述TNF-α在处理后6小时减小。培养后,可以收集细胞培养基质,TNF-α分泌的量使用来自R&D Systems(#DTA00C)的夹心酶联免疫吸附分析(ELISA)进行定量。
抗氧化剂(AO)分析:体外生物分析,其测量任一活性成分、成分组合或说明书所公开的具有所述成分组合的组合物的抗氧化剂总量。该分析依赖于抗氧化剂在样品中抑制(2,2'-连氮基-二-[3-乙基苯并噻唑啉磺酸盐/酯])被正铁肌红蛋白氧化成·+的能力。活体的抗氧化体系包括酶,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,以及一批小分子,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。内生的和源于食物的抗氧化剂的总和表示细胞外液总的抗氧化活性。所有不同抗氧化剂的协同相比任何单一化合物提供更大的保护来对抗反应性氧或氮自由基的攻击。因此,相比于由单个组分测量获得的生物信息,总的抗氧化能力可以给出更加确切的生物信息,这是因为考虑了在血浆和体液中存在的所有抗氧化剂的累积效应。将抗氧化剂在样品中阻止ABTS氧化的能力与Trolox的进行比较,Trolox是一种水溶性生育酚的类似物,并将其按照摩尔的Trolox当量进行定量。来自Cayman Chemical(美国密歇根州安阿伯)的抗氧化能力试剂盒#709001可以用于测量每一任一活性成分、成分组合或说明书所公开的具有所述成分组合的组合物的总抗氧化能力的体外生物分析。可以根据制造商的推荐来进行方案。该分析依赖于在样品中抑制(2,2'-连氮基-二-[3-乙基苯并噻唑啉磺酸盐/酯])被正铁肌红蛋白氧化成·+的抗氧化剂。抗氧化剂在样品中阻止ABTS氧化的能力可以与Trolox的进行比较,Trolox是一种水溶性生育酚的类似物,并将其按照摩尔的Trolox当量进行定量。
ORAC分析:任一活性成分、成分组合或说明书所公开的具有所述成分组合的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。任一活性成分、成分组合或说明书所公开的具有所述成分组合的组合物的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引起的藻红蛋白荧光下降的能力。
蘑菇酪氨酸酶活性分析:在哺乳动物细胞中,酪氨酸酶在从酪氨酸(和从多巴色素的聚合)到黑色素的多步生物合成中催化两个步骤。酪氨酸位于黑素细胞中,并生成给予皮肤、毛发和眼睛颜色的黑色素(芳香醌化合物)。纯化的蘑菇酪氨酸酶(Sigma)可以在每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物存在或不存在的条件下与其底物左旋多巴(Fisher)一起进行培养。色素的形成可以通过比色板在490nm处测量进行评估。蘑菇酪氨酸酶活性的百分比抑制可以相比于未处理的对照物进行计算,以确定测试成分或其组合抑制纯化酶活性的能力。测试提取物的抑制与曲酸(Sigma)的进行对比。
基质金属蛋白酶的活性(MMP3;MMP9)分析:体外的基质金属蛋白酶抑制分析。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)。可以分析活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物。
环氧酶(COX)分析:体外的环氧酶-1和-2(COX-1、-2)抑制分析。COX是一种双功能酶,表现出环氧酶和过氧化物酶两者的活性。环氧酶活性将花生四烯酸转化为过氧化氢内过氧化物(前列腺素G2;PGG2),而过氧化物酶组分还原内过氧化物(前列腺素H2;PGH2)为相应的醇、前列腺素的前体、血栓素和环前列腺素。该COX抑制剂筛选分析测量环氧酶的过氧化物酶组分。过氧化物酶活性通过监测被氧化的N,N,N',N'-四甲基-对苯二胺(TMPD)的出线比色分析。该抑制剂筛选分析包括COX-1和COX-2两种酶按顺序筛选同工酶-特异性抑制剂。比色COX(绵羊的)抑制剂筛选分析(#760111,Cayman Chemical)可以用于分析每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物对纯化的环氧酶(COX1或COX2)的效果。根据制造商的说明,纯化的酶、血红素和测试提取物可以在分析缓冲体系中混合并在室温下摇动15分钟进行培养。培养后,花生四烯酸和比色底物可以加入以开始反应。颜色发展可以通过比色板在590nm处测量进行评估。COX1或COX2活性的百分比抑制可以相比于未处理的对照物进行计算,以确定测试提取物抑制纯化酶活性的能力。
脂肪氧合酶(LO)分析:体外的脂肪氧合酶(LO)抑制分析。LO是不含血红素铁的加双氧酶,其催化分子氧与脂肪酸的加成。亚油酸盐/酯和花生四烯酸盐/酯是LO在植物和动物中主要的底物。于是花生四烯酸可以转化为羟二十碳四烯酸(HETE)衍生物,其随后转化为白细胞烯,活性的炎症介质。提供该分析提供通过测量产生自脂肪氧化酶(5-、12-或15-LO)与花生四烯酸培养的氢过氧化物筛选脂肪氧合酶抑制剂的准确和方便的方法。比色LO抑制剂筛选试剂盒(#760700,Cayman Chemical)可以用于确定每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物抑制酶活性的能力。纯化的15-脂肪氧合酶和测试成分可以在分析缓冲体系中混合并在室温下摇动10分钟进行培养。培养后,加入花生四烯酸以开始反应,另外在室温下培养混合物10分钟。可以加入比色底物以终止催化,颜色发展通过荧光板在490nm处测量进行评估。脂肪氧合酶活性的百分比抑制可以相比未处理的对照物进行计算,以确定每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物抑制纯化酶活性的能力。
弹性蛋白酶分析:来自Molecular Probes(美国俄勒冈州尤金)的弹性蛋白酶分析(试剂盒#E-12056)可以用于测量每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物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的荧光可以猝灭。非荧光的底物可以通过弹性蛋白酶或其他蛋白酶消化以生成高荧光的片段。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~505nm处有吸收最大值,并在~515nm处有荧光发射最大值。当使用EnzChek弹性蛋白酶分析试剂盒进行弹性蛋白酶抑制剂筛选时,多肽、氯甲基酮可以用作选择性的、集体的弹性蛋白酶抑制剂。
油控制分析:测量来自皮脂腺的皮脂分泌减少和/或来自皮脂腺的皮脂生成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。在一个例子中,可以使用前额。每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物可以在规定的天数内(例如1、2、3、4、5、6、7、8、9、10、11、12、13、14或更多天)每天一次或两次施用到前额的一部分。在规定的天数期满后,然后通过对处理过的或未处理的前额皮肤敷上优良的吸墨纸来对皮脂分泌进行分析。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除去任何皮脂来完成的。然后将吸墨纸敷于处理过的和未处理的前额区域,可以用橡皮筋围绕前额以轻轻地将吸墨纸压在皮肤上。吸墨纸2小时后可以移开,能够干燥并然后透照。吸墨纸越暗对应越多的皮脂分泌(或较亮的吸墨纸对应减少的皮脂分泌)。
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。测定之后,立即用活性成分、任一成分组合或说明书所公开的具有所述成分组合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 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。单位可以根据仪器说明对每个测试日进行标定。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,其对应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。可以根据该方法分析每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物。
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进行评估。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。这用来确定每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的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。
肤色的临床评分分析: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。
皮肤光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。设备在每次使用前通过扫描已知数值的标样进行标准化。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,每一活性成分、任一成分组合或说明书所公开的具有所述成分组合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可以用各种含有每一活性成分、任一成分组合或说明书所公开的具有所述成分组合的组合物的赋形剂进行处理,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。
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显而易见的是,可以对所属皮肤活性成分、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 (12)
1.一种局部皮肤用组合物,其配制为精华并且能够增加皮肤的容量或紧致度,所述局部皮肤用组合物包含:水、乙醇、一缩二丙二醇、甲基葡糖聚氧乙烯(20)醚、生物糖胶-1、甘油、聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷交联聚合物、丁二醇、二乙烯基聚二甲基硅氧烷/聚二甲基硅氧烷共聚物、苯氧基乙醇、山梨糖醇、聚二甲基硅氧烷、二氧化硅、麦芽糖糊精、丙烯酸盐或酯/丙烯酸C10-30烷基酯交联聚合物、1,2-辛二醇、羟乙基纤维素、三乙醇胺、氯苯甘醚、泛醇、戊二醇和乙二胺四乙酸二钠。
2.权利要求1所述的局部皮肤用组合物,还包含:C12-14烷基聚氧乙烯(12)醚、羟丙基环糊精、刺海门冬提取物、黑麦籽提取物、积雪草分生组织细胞培养物、刺阿干树仁提取物、C12-13烷基聚氧乙烯(23)醚、C12-13烷基聚氧乙烯(3)醚、腺苷、黑莓叶提取物、PEG-20失水山梨醇椰油酸酯、泡叶藻提取物、红豆蔻叶提取物、软毛松藻提取物、椰油酰基谷氨酸钠、丁基氨基甲酸碘代丙炔酯、交替单胞菌发酵产物滤液、黄原胶、卡波姆、三(辛酸/癸酸)甘油酯、山梨酸钾、仙人果果实提取物、柠檬酸、苯甲酸钠、葡聚糖和三肽-1。
3.权利要求1至2中任一项所述的局部皮肤用组合物,包含60%到70%w/w的水、5%到10%w/w的乙醇、5%到10%w/w的一缩二丙二醇、2%到5%w/w的甲基葡糖聚氧乙烯(20)醚和2%到5%w/w的生物糖胶-1。
4.一种增加皮肤的容量或紧致度的方法,包括对有此需求的皮肤局部施用权利要求1至3中任一项所述的组合物,其中皮肤的容量或紧致度增加。
5.一种局部皮肤用组合物,其配制为在夜间或者睡眠时使用的乳霜,所述局部皮肤用组合物包含:水、甘油、氢化聚癸烯、环戊硅氧烷、鲸蜡硬脂醇、一缩二丙二醇、牛油果脂、硬脂酸甘油酯、三(辛酸/癸酸)甘油酯、硬脂酸异鲸蜡醇酯、丁二醇、三异硬脂酸聚甘油(2)酯、苯氧基乙醇、PEG-100硬脂酸酯、聚甲基丙烯酸甲酯、鲸蜡硬脂基葡糖苷、聚二甲基硅氧烷、三辛酸甘油酯、氯苯甘醚、三乙醇胺、卡波姆和乙二胺四乙酸二钠。
6.权利要求5所述的局部皮肤用组合物,还包含:BHT、羟丙基环糊精、视黄醇、积雪草分生组织细胞培养物、环己硅氧烷、腺苷、红豆蔻叶提取物、戊二醇、石榴提取物、软毛松藻提取物、肉桂树皮提取物、光果甘草根提取物、丁基氨基甲酸碘代丙炔酯、环丁硅氧烷、1,2-辛二醇、黄原胶、山梨酸、仙人果果实提取物、山梨酸钾、苯甲酸钠、柠檬酸、葡聚糖和三肽-1。
7.权利要求5至6中任一项所述的局部皮肤用组合物,其中所述组合物包含50%到60%w/w的水、10%到15%w/w的甘油、3%到7%w/w的氢化聚癸烯、3%到7%w/w的环戊硅氧烷和3%到7%w/w的鲸蜡硬脂醇。
8.一种滋润皮肤或增加皮肤紧致度的方法,包括对有此需求的皮肤局部施用权利要求5至7中任一项所述的组合物,其中对皮肤的局部施用增加皮肤湿润度或增加皮肤紧致度。
9.一种局部皮肤用组合物,配制为能够减少黑眼圈或者肿眼泡的出现的乳霜,所述局部皮肤用组合物包含:水、甘油、矿物油、凡士林、氢化聚癸烯、鲸蜡酯、双-二甘油多酰基己二酸酯-2、丁二醇、氢化聚异丁烯、橄榄油酸失水山梨醇酯、橄榄油酸鲸蜡硬脂醇酯、棕榈酸鲸蜡醇酯、鲸蜡硬脂醇、棕榈酸失水山梨醇酯、抗坏血酸四己基癸酯、二氧化硅、十六/十八醇聚氧乙烯(20)醚、重氮烷基脲、乙酸生育酚酯、三乙醇胺、积雪草提取物、丙烯酸盐或酯/丙烯酸C10-30烷基酯交联聚合物、厚朴树皮提取物和丙二醇。
10.权利要求9所述的局部皮肤用组合物,还包含:羟丙基环糊精、乙烯/甲基丙烯酸盐或酯共聚物、乙二胺四乙酸二钠、橙皮苷甲基查尔酮、腺苷、硬脂基聚氧乙烯(20)醚、豌豆提取物、苯氧基乙醇、三异硬脂酸钛异丙酯、柠檬酸钠、柚皮提取物、丁基氨基甲酸碘代丙炔酯、积雪草分生组织细胞培养物、望春花花蕾/花提取物、二葡萄糖酸洗必泰、山梨酸钾、二肽-2、苯甲酸钾、柠檬酸、仙人果果实提取物、棕榈酰四肽-7、苯甲酸钠、葡聚糖、三肽-1和黄原胶。
11.权利要求9至10中任一项所述的局部皮肤用组合物,其中所述组合物包含45%到55%w/w的水、7%到12%w/w的甘油、5%到10%w/w的矿物油、5%到10%w/w的凡士林和3%到7%w/w的氢化聚癸烯。
12.一种减少人脸的眶周区中黑眼圈或浮肿出现的方法,包括对有此需求的皮肤局部施用权利要求9至11中任一项所述的组合物,其中局部施用减少人脸的眶周区中黑眼圈或浮肿的出现。
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Application publication date: 20200424 |