CN113318012B - 呈含矿化水的凝胶形式的用于局部应用的组合物 - Google Patents
呈含矿化水的凝胶形式的用于局部应用的组合物 Download PDFInfo
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- CN113318012B CN113318012B CN202110187269.5A CN202110187269A CN113318012B CN 113318012 B CN113318012 B CN 113318012B CN 202110187269 A CN202110187269 A CN 202110187269A CN 113318012 B CN113318012 B CN 113318012B
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Abstract
本发明涉及用于局部应用的组合物(C1),其是凝胶的形式,其包含:具有于25℃检测的电导率为大于或等于300微西门子/厘米(或μS.cm‑1)的水;交联的阴离子性聚电解质(P1);和至少一种半乳甘露聚糖(GM)。
Description
技术领域
本发明涉及用于局部应用的组合物,其是凝胶的形式,其包含:被至少中等矿化的水,所述水具有于25℃检测的电导率为大于或等于200μS/cm;和有效的增稠体系。
背景技术
化妆品工业使用各种品质的水来制备化妆品配制剂,这些配制剂销售给最终消费者。因此可以提到天然矿质水、海水、泉水、陆地植物水和海藻水。
这些不同类型的水在其地理和地质来源方面是显著不同的,所以具有不同的矿化特性。因此,水可以用其“总矿化度”表征,即在所考虑的水中存在的所有矿物质元素的总和。更重要的是在所述水中存在的阳离子量和阴离子量的总和。更特别是,在矿化水中所含的阳离子是钙、镁、钠、钾、铁、锌、铜、铝和锰阳离子。更特别是,在矿化水中所含的阴离子是碳酸根、碳酸氢根、硅酸根、硫酸根、氯离子、硝酸根、磷酸根和氟阴离子。所以,术语“总矿化度”用按单位体积计的质量来表示,即毫克/升。
这种矿化特性也可以通过检测水的电导率来转换表征,电导率的单位通常是微西门子/厘米(μS/cm)或毫西门子/厘米(mS/cm)。
在本发明中,术语“低度矿化水”将表示这种水具有于25℃检测的电导率是小于200μS/cm。
在本发明中,术语“中等矿化水”将表示这种水具有于25℃检测的电导率是大于或等于200μS/cm且小于333μS/cm。
在本发明中,术语“强化中等矿化水”将表示这种水具有于25℃检测的电导率是大于或等于333μS/cm且小于666μS/cm。
在本发明中,术语“显著矿化水”将表示这种水具有于25℃检测的电导率是大于或等于666μS/cm且小于1000μS/cm。
在本发明中,术语“高度矿化水”将表示这种水具有于25℃检测的电导率是大于或等于1000μS/cm。
天然矿质水、海水、泉水和海藻水是至少中等矿化的,所以于25℃测得其电导率是大于或等于200μS/cm,因为其可以向人或动物皮肤提供的性能而通常用于制备化妆品、皮肤用化妆品、药物和皮肤用药物组合物。
实际上,文献中已经知道中等矿化至高度矿化的泉水、矿化水、海水和海藻水可以用于配制剂中,这是由于它们对赋予抗氧化性能、镇静或抗炎性能以及抑制过敏的性能做出贡献。因此,专利申请EP 1170002 A1描述了减少人皮肤的弹性损失的方法,其包括使用含有矿物质浓度为至少200mg/l的矿化水。相似地,专利申请EP 0699432 B1描述了使用总矿化度为大于或等于700mg/l的水,用于舒缓可能由于活性试剂引起的皮肤刺激,活性试剂例如是在处理粉刺中所用的视黄醇、过氧化苯甲酰或水杨酸。
也知道海藻水或海水可以用于防护皮肤病,例如湿疹和牛皮癣,或用于在肌腱损伤或病变或扭伤之后重新建立健康状况。
因此证明了需要在存在或不存在生物活性或非活性物质的情况下进行海水或海藻水的长期局部应用,从而更好地以人体或动物的相关区域为目标。
日本专利申请JP 2000-273033描述了凝胶形式的组合物,其包含活性物质,以及海藻糖和作为胶凝剂的卡拉胶的组合。
欧洲专利EP 2756839B1描述了组合物,其是基于95质量%的海水和作为胶凝剂的羟基乙基甲基纤维素。
但是,这些方案无法制备具有高粘度的凝胶形式的局部可接受的组合物,例如粘度为大于或等于10000mPa.s(于25℃用Brookfield RVT粘度计检测,速度为5)。
化妆品工业和药物工业中市售的含水凝胶形式的化妆品组合物通常包含合成增稠聚合物以增加溶液的粘度,从而获得凝胶,凝胶被直接或间接地施加到皮肤上。
目前用于这些领域中的合成增稠聚合物有两种物理形式,即粉末形式和液体形式,其中聚合物是通过使用表面活性剂的反相乳液自由基聚合制备的,并通常称为自可逆转的反相胶乳。
在大多数常规的粉末形式的合成增稠聚合物中,可以提到基于丙烯酸的聚合物或基于丙烯酸及其酯的共聚物。例如可以提到以商品名CarbopolTM和PemulenTM销售的聚合物。它们具体描述在美国专利US 5 373 044和US 2 798 053以及欧洲专利EP 0 301 532B1中。它们的缺点是需要分散,然后需要添加碱进行中和以达到所需的盐化程度,这与所需的粘度相关。
在化妆品中也使用粉末形式的均聚物或共聚物,其基于2-丙烯酰氨基-2-甲基丙磺酸和/或其盐。这些增稠聚合物是以商品名AristoflexTM销售,并可以具体参见欧洲专利EP 816 403、EP 1 116 733和EP 1 069 142。这些粉末形式的合成增稠剂是通过沉淀聚合得到的;将单体溶解在有机溶剂中,例如苯、乙酸乙酯、环己烷或叔丁醇;因此,该方法要求进行多个接连的步骤以提纯最终产品,从而去除任何痕量的残余溶剂。
在化妆品和药物工业中也非常广泛地使用自可逆转的反相胶乳液体形式的增稠剂,具体参见本申请人销售的产品。例如,可以提到增稠剂SepigelTM 305,SimulgelTM 600,SimulgelTM EG,SimulgelTM EPG,SimulgelTM NS,SimulgelTM A,SepiplusTM400,SepiplusTM250和SepiplusTM265。这些增稠剂是通过反相乳液自由基聚合制得的。它们的优点是更容易控制,特别是在室温下,并且能非常快速地分散于水中。另外,这些产品显示非常高的增稠性能;此性能可能是由于其制备方法,即分散相自由基聚合物反应,这导致获得具有非常高分子量的聚合物。
本申请人也开发了合成增稠剂,其具有与反相胶乳相等或甚至更好的增稠性能,但是能更好地被皮肤耐受,特别是由于不存在任何油相,这可以获得颜色较浅的含水凝胶。这些产品是粉末形式,但是具有溶解时间,所以易于实施,是与液体形式的产品相当的。在欧洲专利申请EP 1 496 081中描述的这些化合物是通过常规聚合技术获得的,例如分散相自由基聚合,反相悬浮自由基聚合,以及反相乳液或反相微乳液自由基聚合。所得的合成增稠体系然后经由各种技术进行提取和提纯,例如从中间溶剂沉淀,从中间溶剂沉淀之后任选地进行洗涤,喷雾干燥或共沸脱水,任选地然后用特定选择的溶剂洗涤。所以,这些合成增稠剂合并了呈标准粉末形式的合成增稠剂的优点(不存在油,获得颜色较浅的含水凝胶)和呈反相胶乳形式的合成增稠剂的优点(高的溶解速度,特别是增稠能力和稳定性能)。
但是对于其中存在至少中等矿化的并进而具有于25℃检测的电导率为大于或等于200μS/cm的水的应用而言,认为上述合成增稠聚合物、例如交联的阴离子性聚电解质并不是足够有效的。
发明内容
所以,仍然需要用于局部应用的组合物,其是凝胶的形式,其包含至少中等矿化的水,并且所述水具有于25℃检测的电导率为大于或等于200μS/cm;和有效的增稠体系,即可以任选地在生物活性试剂的存在下显著达到在人或动物皮肤上局部使用的高粘度水平的体系。
本发明的一个技术方案是用于局部应用的组合物(C1),其是凝胶的形式,并包含:
-水,其具有于25℃检测的电导率是大于或等于300微西门子/厘米(或μS.cm-1),
-交联的阴离子性聚电解质(P1),和
-至少一种半乳甘露聚糖(GM)。
具体实施方案
在本发明中,术语“凝胶”表示化学组合物,其初始是液体形式,并在添加胶凝和/或增稠物质之后转变成不会流动的结构化状态。认为上述凝胶是处于固态和液态之间的中间状态,并且由在液体内的三维网络构成,这是由于化学键或物理键的作用。
为了本发明的目的,术语“胶凝剂”表示化学化合物或所述化合物的混合物,其能将液体介质转变成凝胶。
为了本发明的目的,术语“增稠剂”表示化学化合物或所述化合物的混合物,其能增加添加它们的介质的粘度。
在上述用于局部应用的组合物(C1)的定义中,术语“用于局部应用”表示所述组合物通过施加到皮肤、头发、头皮、指甲、唇部、粘膜、眼睫毛或眉毛上来使用,不论是在化妆品配制剂的情况下直接施用,或间接施用,例如在织物或纸巾形式的身体护理产品的情况下,或要与皮肤、头发、头皮、指甲、唇部、粘膜、眼睫毛或眉毛接触的卫生产品。
水相(A1)的电导率是通过在25℃温度下直接检测从被浸入待测水相(A1)中的两个电极之间经过的电流来测定。通入的电流是非常低频的交流电,从而避免电极的极化。
所用的装置是由采集箱和探针组成。探针包括温度电极,由两个或更多个传感器组成的检测电极,或集成电极设备。
所用的装置更特别是WTW品牌的装置,pH/Cond 34Oi型号。
检测结果是由在参比温度(25℃)下的μS/cm表示。
在作为本发明主题的用于局部应用的组合物(C1)中,存在的水相(A1)具有于25℃检测的电导率为大于或等于300μS.cm-1,可以来源于天然来源,和可以单独使用、或作为与其它来源的水的混合物使用。
在作为本发明主题的用于局部应用的组合物(C1)中,存在的水相(A1)具有于25℃检测的电导率为大于或等于300μS.cm-1,优选由天然矿质水、泉水、海水或海藻水组成。
在作为本发明主题的用于局部应用的组合物(C1)中,存在的水相(A1)具有于25℃检测的电导率为大于或等于300μS.cm-1,也可以通过将天然矿质水、泉水、海水或海藻水与软化水混合来制备,从而调节所选择的电导率值。
为了本发明的目的,术语“天然矿质水”表示这样的水:其“总矿化度”,即稳定且适用于消耗的痕量元素的含量,符合法国公共卫生指南(French Public Health Code)的第R1322-2条的要求,并更具体地符合法国公共卫生指南的第L.1322-1至L132-13、R.1322-1至R.1322-44-8以及R.1322-45至R.1322-67条的规定。
为了本发明的目的,“泉水”表示上述天然矿质水,其是为了治疗目的开发的,并且在地区卫生局(Regional Health Authority)指导下获得法国专业机构的预先授权。
关于可与存在于本发明组合物(C1)中的水相(A1)组合的泉水或天然矿质水的例子,可以提到例如以下水:Avène水,Vittel,Vichy Basin水,Uriage水,Roche-Posay水,Bourboule水,Enghien-les-bains水,Saint-Gervais-les bains水,Néris-les-bains水,Allevard-les-bains水,Digne水,Maizières水,Neyrac-les-bains水,Lons le Saunier水,Rochefort水,Saint Christau水,Fumades水,Tercis-les-bains水,Bagnères-de-Bigorres水,Eugénie-les-Bains水,Challes-les-eaux水,Volvic水,Vals水,Vernière水,Aix les Bains水,Alet水,Abatilles水,Arcens水,Arvie水,Asperjoc水,Badoit水,Cilaos水,Contrex水,Evian水,Hépar水,Jouvence,Mont-Roucous水,Ogeu水,Orezza水,Parot水,Perrier水,水,Quézac水,Rozana水,Saint-Albans水,Saint-Amand-les Eaux水,Saint-Georges水,Saint-Géron水,Sainte-Marguerite水,Saint-Yorre水,Salvetat水,Teissières-lès-Bouliès水,Thonon水,Treignac水,Courmayeur水,SanBenedetto水和San Pellegrino水。
为了本发明的目的,术语“海藻水”表示通过对在所收获的海藻中包含的水进行蒸发和冷凝而收集到的水,所述水来源于经处理的海藻的细胞。根据一个具体方案,海藻水是来自褐藻的水,来自红藻的水,或来自绿藻的水。根据一个甚至更特别的方案,海藻水是来自掌状海带(Laminaria digitate)的水,来自角叉菜的水,或来自星芒杉藻的水。
关于可与存在于本发明组合物(C1)中的水相(A1)组合的海藻水的例子,可以提到例如以商品名HydralixirTM LD或HydralixirTM CC销售的海藻水。
为了本发明的目的,术语“半乳甘露聚糖(GM)”表示仅仅由单糖组成的多糖(或聚-单糖),其是聚合物,其中聚合物的主链是由经由β-1,4键连接在一起的D-甘露糖单元组成,并且在主链上经由α-1,6键侧向接枝D-半乳糖单元。
多糖是糖类聚合物。糖的IUPAC定义包括单糖,单糖本身的化合物及其衍生物,其是通过羰基的还原获得,或通过一个或多个羟基官能团的氧化获得,或通过用氢原子、胺基团、磷酸酯官能团或硫酸酯官能团替代一个或多个羟基官能团获得。
最常用于制备食品、化妆品或药物组合物的多糖主要由单糖组成,例如葡萄糖、半乳糖、甘露糖,或主要由单糖衍生物组成,其中末端碳的羟基官能团已经被氧化成羧基官能团。所以,多糖可以分为两类:仅仅由单糖组成的多糖(或聚-单糖),和由单糖衍生物组成的多糖。仅仅由单糖组成的多糖可以分为:
·葡聚糖,其在性质上富含葡萄糖均聚物,
·甘露聚糖,
·木葡聚糖,
·半乳甘露聚糖,其是聚合物,该聚合物的主链是由经由β-1,4键连接在一起的D-甘露糖单元组成,并且在主链上经由α-1,6键侧向接枝D-半乳糖单元。
在多种植物中发现半乳甘露聚糖,更特别是豆科植物,其中它们构成种子的胚乳。
根据半乳甘露聚糖来源的植物起源,在D-甘露糖主链上的D-半乳糖单元的取代度(DS)是在0-1的范围内:
·来源于决明胶的半乳甘露聚糖具有约1/5的取代度(DS),表示在多糖主链上存在的每5个D-甘露糖单元中侧向接枝1个D-半乳糖单元;
·来源于槐豆胶的半乳甘露聚糖具有约1/4的取代度(DS),表示在多糖主链上存在的每4个D-甘露糖单元中侧向接枝1个D-半乳糖单元;
·来源于塔拉胶的半乳甘露聚糖具有约1/3的取代度(DS),表示在多糖主链上存在的每3个D-甘露糖单元中侧向接枝1个D-半乳糖单元;
·来源于瓜尔胶的半乳甘露聚糖具有约1/2的取代度(DS),表示在多糖主链上存在的每2个D-甘露糖单元中侧向接枝1个D-半乳糖单元;
·来源于香豆胶的半乳甘露聚糖具有约1/1的取代度(DS),表示在多糖主链上存在的每1个D-甘露糖单元中侧向接枝1个D-半乳糖单元。
因此,在根据本发明的组合物中,半乳甘露聚糖(GM)是选自取代度(DS)为约1/3的半乳甘露聚糖,取代度(DS)为约1/2的半乳甘露聚糖,以及取代度(DS)为约1/4的半乳甘露聚糖。
在作为本发明主题的用于局部应用的组合物(C1)的定义中,术语“交联的阴离子性聚电解质(P1)”表示非线性的交联的阴离子性聚电解质,其是三维网络的形式,不溶于水,但能在水中溶胀,并导致形成化学凝胶。
根据具体情况,本发明组合物可以具有一个或多个以下特征:
-该组合物包含按其100质量%计的以下组分:93-99.4质量%、优选95-99.3质量%、甚至更优选95.5-99.0质量%的具有于25℃检测的电导率为大于或等于300微西门子/厘米(或μS.cm-1)的水;0.5-5质量%、优选0.5-3%、甚至更优选0.5-2.5质量%的交联的阴离子性聚电解质(P1);和0.1-2质量%、优选0.2-2%、甚至更优选0.5-2质量%的半乳甘露聚糖(GM);
-具有取代度为1/3的半乳甘露聚糖;
-交联的阴离子性聚电解质(P1),其包含从游离酸或者部分或完全盐化形式的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸衍生的单体单元。为了本发明的目的,术语“盐化”表示在单体中存在的酸官能团是阴离子性形式,其与阳离子缔合形成盐,特别是碱金属盐,例如钠或钾阳离子,或例如含氮碱的阳离子,例如铵盐、赖氨酸盐或单乙醇胺盐(HOCH2-CH2-NH3 +)。它们优选是钠盐或铵盐;
-交联的阴离子性聚电解质(P1)由以下组成:从选自丙烯酸、甲基丙烯酸、2-羧基乙基丙烯酸、衣康酸、马来酸和3-甲基-3-[(1-氧基-2-丙烯基)氨基]丁酸的至少一种单体衍生的单体单元,其中所述单体的羧基官能团是游离酸或者部分或完全盐化的形式;和至少一种从多烯属交联单体(AR)衍生的单体单元;
-交联的阴离子性聚电解质(P1)由从丙烯酸衍生的单体单元和至少一种从多烯属交联单体(AR)衍生的单体单元组成;
-多烯属交联单体(AR)是选自亚甲基双(丙烯酰胺),乙二醇二甲基丙烯酸酯,二甘醇二丙烯酸酯,乙二醇二丙烯酸酯,二烯丙基脲,三烯丙基胺,三羟甲基丙烷三丙烯酸酯,二烯丙氧基乙酸或其盐,例如二烯丙氧基乙酸钠,或这些化合物的混合物;
-多烯属交联单体(AR)是三烯丙基胺、三羟甲基丙烷三丙烯酸酯或亚甲基双(丙烯酰胺),或这些化合物的混合物;
-所述交联的阴离子性聚电解质(P1)是选自以下聚合物:以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与以钠盐形式部分或完全盐化的丙烯酸(δ)按照摩尔比率(γ)/(δ)为大于或等于40/60且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与丙烯酸羟基乙基酯(ζ)按照摩尔比率(γ)/(ζ)为大于或等于30/70且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与丙烯酰胺(ε)按照摩尔比率(γ)/(ε)为大于或等于30/70且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;
-半乳甘露聚糖(GM)与交联的阴离子性聚电解质(P1)之间的质量比率是大于或等于0.15且小于或等于0.75,优选大于或等于0.20且小于或等于0.60,更特别是大于或等于0.25且小于或等于0.60,甚至更优选是大于或等于0.20且小于或等于0.50。
根据一个具体方案,交联的阴离子性聚电解质(P1)按100摩尔%计包含:
(a1)-比例为大于或等于25摩尔%且小于或等于100摩尔%的从游离酸或者部分或完全盐化的形式的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸衍生的单体单元;
(a2)–任选地,比例为大于0摩尔%且小于或等于75摩尔%的从选自以下的至少一种单体衍生的单体单元:丙烯酰胺,N,N-二甲基丙烯酰胺,甲基丙烯酰胺,叔丁基丙烯酰胺和N-异丙基丙烯酰胺;
(a3)–任选地,比例为大于0摩尔%且小于或等于20摩尔%、更特别大于0摩尔%且小于或等于15摩尔%、甚至更特别大于或等于0摩尔%且小于或等于10摩尔%的从选自以下的至少一种单体衍生的单体单元:丙烯酸(2-羟基乙基)酯,丙烯酸(2,3-二羟基丙基)酯,甲基丙烯酸(2-羟基乙基)酯,甲基丙烯酸(2,3-二羟基丙基)酯和乙烯基吡咯烷酮;
(a4)-任选地,比例为大于0摩尔%且小于或等于75%的从选自以下的至少一种单体衍生的单体单元:丙烯酸,甲基丙烯酸,2-羧基乙基丙烯酸,衣康酸,马来酸和3-甲基-3-[(1-氧基-2-丙烯基)氨基]丁酸,所述单体的羧基官能团是游离酸或者部分或完全盐化的形式;
(a5)任选地,比例为大于0摩尔%且小于或等于5摩尔%的至少一种式(I)单体:
其中R表示直链或支化的具有8-20个碳原子的烷基,并且n表示大于或等于0且小于或等于20的整数,
(a6)-比例为大于0摩尔%且小于或等于1摩尔%的从至少一种多烯属交联单体(AR)衍生的单体单元;所述单体单元a1)、a2)、a3)、a4)、a5)和a6)的摩尔比例总和是等于100摩尔%。
根据本发明的另一个具体方案,用于局部应用的组合物(C1)的特征在于所述多烯属交联单体(AR)是按照摩尔比例为小于或等于0.5%使用,更特别是小于或等于0.25%,最特别是小于或等于0.1%;最尤其是大于或等于0.005摩尔%。
在作为本发明主题的用于局部应用的组合物(C1)中,所用的交联的阴离子性聚电解质(P1)也可以包含各种添加剂,例如络合剂、转移剂或链限制剂。
在作为本发明主题的用于局部应用的组合物(C1)中,所用的交联的阴离子性聚电解质(P1)也可以包含各种添加剂,例如络合剂、转移剂或链限制剂。
在作为本发明主题的用于局部应用的组合物(C1)中,所用的交联的阴离子性聚电解质(P1)可以通过本领域公知的自由基聚合方法制备,例如溶液聚合,悬浮聚合,反相悬浮聚合,乳液聚合,反相乳液聚合,或在溶剂介质中聚合,然后使所得聚合物进行沉淀的步骤。
根据一个更具体的方案,在作为本发明主题的用于局部应用的组合物(C1)中,所用的交联的阴离子性聚电解质(P1)可以通过在溶剂介质中聚合、然后使所得聚合物进行沉淀的方法制备,或通过反相乳液聚合、任选地然后进行浓缩和/或雾化步骤来制备。
根据一个更具体的方案,在作为本发明主题的用于局部应用的组合物(C1)中,所用的交联的阴离子性聚电解质(P1)可以根据一种上述方法制备,和可以包括使用链转移剂或链限制剂。链转移剂或链限制剂更特别是选自次磷酸钠,低分子量醇,例如甲醇、乙醇、1-丙醇、异丙醇或丁醇,硫醇,例如2-巯基乙醇,含硫酸盐官能团的转移剂,例如甲基烯丙基磺酸钠,或所述转移剂的混合物。链转移剂或链限制剂更特别地按照相对于所用单体摩尔总数计的0.001-1摩尔%的摩尔比例使用,更特别是0.001-0.5摩尔%,最特别是0.001-0.1摩尔%。
根据本发明的另一个具体方案,所述交联的阴离子性聚电解质(P1)是选自以下聚合物:以钠盐或铵盐形式部分或完全盐化的丙烯酸均聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸均聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸与以钠盐或铵盐形式部分或完全盐化的丙烯酸形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与以钠盐形式部分或完全盐化的丙烯酸(δ)按照摩尔比率(γ)/(δ)为大于或等于30/70且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与以钠盐形式部分或完全盐化的丙烯酸(δ)按照摩尔比率(γ)/(δ)为大于或等于40/60且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与丙烯酰胺(ε)按照摩尔比率(γ)/(ε)为大于或等于30/70且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与丙烯酸羟基乙基酯(ζ)按照摩尔比率(γ)/(ζ)为大于或等于30/70且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸、丙烯酰胺与以钠盐或铵盐形式部分或完全盐化的丙烯酸形成的三元共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;摩尔比例为大于或等于30%且小于或等于45%的以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸、摩尔比例为大于或等于45%且小于或等于68%的丙烯酰胺与摩尔比例为大于或等于2%且小于或等于10%以钠盐或铵盐形式部分或完全盐化的丙烯酸形成的三元共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;摩尔比例为大于或等于30%且小于或等于45%的以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸、摩尔比例为大于或等于47%且小于或等于68%的丙烯酰胺与摩尔比例为大于或等于2%且小于或等于8%的以钠盐或铵盐形式部分或完全盐化的丙烯酸形成的三元共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;摩尔比例为大于或等于60%且小于或等于80%的以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸、摩尔比例为大于或等于15%且小于或等于39.5%的N,N-二甲基丙烯酰胺与摩尔比例为大于或等于0.5%且小于或等于5%的四乙氧基化月桂基甲基丙烯酸酯形成的三元共聚物,其用三羟甲基丙烷三丙烯酸酯和/或三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;摩尔比例为大于或等于60%且小于或等于80%的以钠盐或铵盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸、摩尔比例为大于或等于15%且小于或等于39%的N,N-二甲基丙烯酰胺、摩尔比例为大于或等于0.5%且小于或等于2.5%的甲基丙烯酸月桂酰基酯与摩尔比例为大于或等于0.5%且小于或等于2.5%的甲基丙烯酸硬脂酰基酯形成的共聚物,其用三羟甲基丙烷三丙烯酸酯和/或三烯丙基胺和/或亚甲基双(丙烯酰胺)交联。
本发明的主题也是用于局部应用的配制剂(F),其包含:
-上述用于局部应用的组合物(C1);和
-脂肪相(A2),其包含i)至少一种油,和ii)含有至少一种乳化表面活性剂(S1)的乳化体系。
优选,根据本发明的配制剂按其100质量%计包含:
-60-90质量%的组合物(C1);和
-10-40质量%的脂肪相(A2)。
乳化表面活性剂(S1)可以选自烷基聚糖苷组合物,烷基聚糖苷和脂肪醇的组合物,聚甘油酯,烷氧基化聚甘油酯,聚二醇聚羟基硬脂酸酯,聚甘油聚羟基硬脂酸酯和烷氧基化聚甘油聚羟基硬脂酸酯。
在作为本发明主题的用于局部应用的配制剂(F)中,术语“油”表示水不溶性的化合物和/或所述化合物的混合物,其在25℃下是液体,更特别是:
-具有11-19个碳原子的直链烷烃;
-具有7-40个碳原子的支化烷烃,例如异十二烷,异十五烷,异十六烷,异十七烷,异十八烷,异十九烷或异二十烷,或它们的混合物,例如下述和由其INCI名称确认的那些:C7-8异链烷烃,C8-9异链烷烃,C9-11异链烷烃,C9-12异链烷烃,C9-13异链烷烃,C9-14异链烷烃,C9-16异链烷烃,C10-11异链烷烃,C10-12异链烷烃,C10-13异链烷烃,C11-12异链烷烃,C11-13异链烷烃,C11-14异链烷烃,C12-14异链烷烃,C12-20异链烷烃,C13-14异链烷烃,C13-16异链烷烃;
-环烷烃,其任选地被一个或多个直链或支化的烷基取代;
-白矿物油,例如以下商品名销售的产品:MarcolTM 52,MarcolTM 82,DrakeolTM6VR,EolaneTM 130,EolaneTM 150;
-半角鲨烷(或2,6,10-三甲基十二烷;CAS编号:3891-98-3),角鲨烷(或2,6,10,15,19,23-六甲基二十四烷),氢化聚异丁烯或氢化聚癸烯;
-具有15-19个碳原子的烷烃的混合物,所述烷烃是直链烷烃、支化烷烃和环烷烃,更特别是混合物(M1),按其100质量%计包含:质量比例为大于或等于90%且小于或等于100%的支化烷烃;质量比例为大于或等于0%且小于或等于9%、更特别小于5%的直链烷烃,以及质量比例为大于或等于0%且小于或等于1%的环烷烃,例如以商品名EmogreenTML15或EmogreenTM L19销售的混合物;
-式(II)的脂肪醇醚:
Z1-O-Z2 (II),
其中Z1和Z2可以是相同或不同的,表示具有5-18个碳原子的直链或支化烷基,例如二辛基醚,二癸基醚,双十二烷基醚,十二烷基辛基醚,双十六烷基醚,(1,3-二甲基丁基)十四烷基醚,(1,3-二甲基丁基)十六烷基醚,二(1,3-二甲基丁基)醚或二己基醚;
-由式(III)表示的脂肪酸和醇的单酯:
R'1-(C=O)-O-R'2 (III),
其中R’1-(C=O)表示饱和或不饱和的、直链或支化的具有8-24个碳原子的酰基,并且独立于R’1,R’2表示饱和或不饱和的、直链或支化的具有1-24个碳原子的烃基链,例如月桂酸甲基酯,月桂酸乙基酯,月桂酸丙基酯,月桂酸异丙基酯,月桂酸丁基酯,月桂酸2-丁基酯,月桂酸己基酯,椰油酸甲基酯,椰油酸乙基酯,椰油酸丙基酯,椰油酸异丙基酯,椰油酸丁基酯,椰油酸2-丁基酯,椰油酸己基酯,肉豆蔻酸甲基酯,肉豆蔻酸乙基酯,肉豆蔻酸丙基酯,肉豆蔻酸异丙基酯,肉豆蔻酸丁基酯,肉豆蔻酸2-丁基酯,肉豆蔻酸己基酯,肉豆蔻酸辛基酯,棕榈酸甲基酯,棕榈酸乙基酯,棕榈酸丙基酯,棕榈酸异丙基酯,棕榈酸丁基酯,棕榈酸2-丁基酯,棕榈酸己基酯,棕榈酸辛基酯,油酸甲基酯,油酸乙基酯,油酸丙基酯,油酸异丙基酯,油酸丁基酯,油酸2-丁基酯,油酸己基酯,油酸辛基酯,硬脂酸甲基酯,硬脂酸乙基酯,硬脂酸丙基酯,硬脂酸异丙基酯,硬脂酸丁基酯,硬脂酸2-丁基酯,硬脂酸己基酯,硬脂酸辛基酯,异硬脂酸甲基酯,异硬脂酸乙基酯,异硬脂酸丙基酯,异硬脂酸异丙基酯,异硬脂酸丁基酯,异硬脂酸2-丁基酯,异硬脂酸己基酯,异硬脂酸异硬脂基酯;
-由式(IV)和式(V)表示的脂肪酸和甘油的二酯:
R'3-(C=O)-O-CH2-CH(OH)-CH2-O-(C=O)-R'4 (IV)
R'5-(C=O)-O-CH2-CH[O-(C=O)-R'6]-CH2-OH (V),
其中在式(IV)和(V)中,R’3-(C=O)、R’4-(C=O)、R’5-(C=O)和R’6-(C=O)可以是相同或不同的,表示饱和或不饱和的、直链或支化的具有8-24个碳原子的酰基;
-由式(VI)表示的脂肪酸和甘油的三酯:
R'7-(C=O)-O-CH2-CH[O-(C=O)-R”8]-CH2-O-(C=O)-R”9 (VI),
其中R’7-(C=O)、R’8-(C=O)和R’9-(C=O)可以是相同或不同的,表示饱和或不饱和的、直链或支化的具有8-24个碳原子的酰基;
-植物油,例如角鲨烷,甜杏仁油,椰壳油,蓖麻油,霍霍巴油,橄榄油,菜籽油,落花生油,葵花籽油,麦芽油,玉米胚芽油,豆油,棉籽油,苜蓿油,罂粟籽油,南瓜籽油,月见草油,小米油,大麦油,黑麦油,红花油,烛果油,西番莲油,榛子油,棕榈油,乳木果油,杏仁壳油,美人叶油,大蒜芥油,鳄梨油,金盏花油,衍生自花或植物的油;
-乙氧基化植物油。
优选,本发明的组合物包含至少一种选自以下的油:蓖麻油,液体石蜡,椰油基癸酸酯/辛酸酯,肉豆蔻酸异丙基酯和癸酸/辛酸三甘油酯。
脂肪相(A2)任选地包含蜡。在作为本发明主题的用于局部应用的配制剂(F)中,术语“蜡”表示水不溶性的化合物和/或所述化合物的混合物,其在35℃下是固体。
所述蜡更特别选自蜂蜡,巴西棕榈蜡,小烛树蜡,小冠巴西棕榈蜡,日本蜡,软木纤维蜡,甘蔗蜡,石蜡,褐煤蜡,微晶蜡,羊毛脂蜡;地蜡;聚乙烯蜡;硅氧烷蜡;植物蜡;在室温下为固体的脂肪醇和脂肪酸;在室温下为固体的甘油酯。
在作为本发明主题的配制剂(F)的定义中,术语“烷基聚葡糖苷组合物”代表由式(VII)表示的组合物(C2):
R1-O-(G)x-H (VII)
其中x表示在1.05和5之间的小数,G表示还原糖残基,并且R1表示饱和或不饱和的、直链或支化的具有12-36个碳原子的脂族烃基,其任选地被一个或多个羟基取代,所述组合物(C2)是由式(VII1)、(VII2)、(VII3)、(VII4)和(VII5)表示的化合物的混合物:
R1-O-(G)1-H (VII1)
R1-O-(G)2-H (VII2)
R1-O-(G)3-H (VII3)
R1-O-(G)4-H (VII4)
R1-O-(G)5-H (VII5)
其各自的摩尔比例是a1、a2、a3、a4和a5,使得:
-总和a1+a2+a3+a4+a5等于1,并且
-总和a1+2a2+3a3+4a4+5a5等于x。
在上述式(VII)中的基团R1中,术语“饱和或不饱和的、直链或支化的具有12-36个碳原子的脂族烃基,其任选地被一个或多个羟基取代”表示:
-饱和的直链烷基,例如正-十二烷基,正-十三烷基,正-十四烷基,正-十五烷基,正-十六烷基,正-十七烷基,正-十八烷基,正-十九烷基,正-二十烷基和正-二十二烷基;
-不饱和的直链基团,例如十二碳烯基,十三碳烯基,十四碳烯基,十五碳烯基,十六碳烯基,十七碳烯基,十八碳烯基,十九碳烯基,二十碳烯基,二十二碳烯基,4-十二碳烯基和5-十二碳烯基;
-饱和或不饱和的、直链或支化的具有12-36个碳原子的脂族基团,其被1或2个羟基取代,例如羟基十二烷基,羟基十四烷基,羟基十六烷基,羟基十八烷基,羟基二十烷基和羟基二十二烷基,例如12-羟基十八烷基;
-从异链烷醇衍生的式(1)基团:
(CH3)(CH3)CH-(CH2)r-CH2-OH (1)
其中r表示8-20的整数,例如异癸基,异十一烷基,异十二烷基,异十三烷基,异十四烷基,异十五烷基,异十六烷基,异十五烷基,异十八烷基,异十九烷基,异二十烷基或异二十二烷基;
-从格尔伯特醇衍生的式(2)的支化烷基:
CH(CsH2s+1)(CtH2t+1)-CH2-OH (2)
其中t是6-18的整数,s是4-18的整数,并且总和s+t是大于或等于10且小于或等于22,例如2-丁基辛基,2-丁基癸基,2-己基辛基,2-己基癸基,2-辛基癸基,2-己基十二烷基,2-辛基十二烷基,2-癸基十四烷基,2-十二烷基十六烷基和2-十四烷基十八烷基。
根据一个具体方案,在上述式(VII)的定义中,R1表示饱和或不饱和的、直链或支化的具有12-24个碳原子的脂族烃基。
在上述式(VII)的定义中,术语“还原糖”表示糖衍生物,在其结构中不具有在异头碳与缩醛基团的氧之间的任何苷键,如在以下出版物中所定义:“生物化学(Biochemistry)”,Daniel Voet/Judith G.Voet,第250页,John Wiley&Sons,1990。低聚结构(G)x可以是任何异构形式,不论是旋光异构、几何异构或区域异构;其也可以表示异构体的混合物。
在上述式(VII)中,基团R1-O-经由糖残基的异头碳连接至G,从而形成缩醛官能团。
根据一个具体方案,在上述式(VII)的定义中,G表示选自以下的还原糖残基:葡萄糖,右旋糖,蔗糖,果糖,艾杜糖,古洛糖,半乳糖,麦芽糖,异麦芽糖,麦芽三糖,乳糖,纤维二糖,甘露糖,核糖,木糖,阿拉伯糖,来苏糖,阿洛糖,阿卓糖,葡聚糖和塔罗糖(tallose);G更特别表示选自葡萄糖、木糖和阿拉伯糖残基的还原糖残基。
根据一个甚至更特别的方案,在作为本发明主题的组合物(F)中包含的组合物(C2)中,在式(VII)的定义中,x表示大于或等于1.05且小于或等于2.5的小数,更特别是大于或等于1.05且小于或等于2.0,甚至更特别大于或等于1.25且小于或等于2.0。
根据一个甚至更特别的方案,在上述式(VII)的定义中,R1表示至少一种选自以下的基团:正-十二烷基,正-十四烷基,正-十六烷基,正-十八烷基,正-二十烷基,正-二十二烷基,2-己基癸基,2-辛基癸基,2-己基十二烷基,2-辛基十二烷基和2-癸基十四烷基;G表示选自葡萄糖和木糖残基的还原糖残基,x表示大于或等于1.05且小于或等于2.5的小数。
根据一个甚至更特别的方案,上述配制剂(F)的特征在于所述乳化体系是由式(VII)表示的烷基聚糖苷组合物(C2)组成:
R1-O-(G)x-H (VII)
其中x表示在1.05和2.5之间的小数,G表示木糖残基,并且R1表示2-辛基十二烷基,所述组合物(C2)是由式(VII1)、(VII2)、(VII3)、(VII4)和(VII5)表示的化合物的混合物:
R1-O-(G)1-H (VII1)
R1-O-(G)2-H (VII2)
R1-O-(G)3-H (VII3)
R1-O-(G)4-H (VII4)
R1-O-(G)5-H (VII5)
其各自的摩尔比例是a1、a2、a3、a4和a5,使得:
-总和a1+a2+a3+a4+a5是等于1,并且
-总和a1+2a2+3a3+4a4+5a5是等于x。
在作为本发明主题的配制剂(F)的定义中,术语“烷基葡糖苷和脂肪醇组合物”表示组合物(C3),按其100质量%计包含:
-10-50质量%、更特别15-40质量%、甚至更特别20-30质量%的至少一种由上述式(VII)表示的组合物(C2),
-90-50质量%、更特别85-60质量%、甚至更特别80-70质量%的至少一种式(VIII)脂肪醇:
R'1-OH (VIII),
其中R'1可以是与R1相同或不同的,表示饱和或不饱和的、直链或支化的具有12-36个碳原子的脂族烃基,任选地被一个或多个羟基取代。
根据一个具体方案,在代表组合物(C3)中所含的组合物(C2)的式(VII)的定义中,R1表示选自以下的基团:正-十二烷基,正-十四烷基,正-十六烷基,正-十八烷基,正-二十烷基,正-二十二烷基,2-己基癸基,2-辛基癸基,2-己基十二烷基,2-辛基十二烷基和2-癸基十四烷基,G表示选自葡萄糖和木糖残基的还原糖残基,并且x表示大于或等于1.05且小于或等于2.5的小数。
根据一个更具体的方案,在代表组合物(C3)中所含的组合物(C2)的式(VII)的定义中,R1表示2-辛基十二烷基,G表示木糖残基,并且x表示大于或等于1.05且小于或等于2.5的小数。
根据一个更具体的方案,在上述式(VIII)脂肪醇的定义中,R'1表示选自以下的基团:正-十二烷基,正-十四烷基,正-十六烷基,正-十八烷基,正-二十烷基,正-二十二烷基,2-己基癸基,2-辛基癸基,2-己基十二烷基,2-辛基十二烷基和2-癸基十四烷基,R'1最特别地表示2-辛基十二烷基。
根据一个甚至更特别的方案,本发明的主题是上述配制剂(F),其特征在于乳化体系是由组合物(C3)组成,组合物(C3)按其100质量%计包含:
-10-50质量%的至少一种由式(VII)表示的烷基聚糖苷组合物(C2):
R1-O-(G)x-H (VII)
其中x表示在1.05和2.5之间的小数,G表示木糖残基,并且R1表示2-辛基十二烷基,所述组合物是由式(VII1)、(VII2)、(VII3)、(VII4)和(VII5)表示的化合物的混合物组成:
R1-O-(G)1-H (VII1)
R1-O-(G)2-H (VII2)
R1-O-(G)3-H (VII3)
R1-O-(G)4-H (VII4)
R1-O-(G)5-H (VII5)
其各自的摩尔比例是a1、a2、a3、a4和a5,使得:
-总和a1+a2+a3+a4+a5是等于1,并且
-总和a1+2a2+3a3+4a4+5a5是等于x;和
-90-50质量%的至少一种式(VIII)脂肪醇:
R'1-OH (VIII),
其中R’1表示2-辛基十二烷基。
在作为本发明主题的配制剂(F)的定义中,术语“聚甘油酯”表示式(IX)化合物:
其中Z表示式R2-C(=O)-的酰基,其中R2表示饱和或不饱和的、直链或支化的具有11-35个碳原子的脂族烃基,更特别是选自以下的基团:十二烷酰基,十四烷酰基,十六烷酰基,十八烷酰基,二十烷酰基,二十二烷酰基,油基,亚油基,亚麻基和异硬脂基;Z'表示上述式R2-C(=O)-的酰基,其可以是与Z相同或不同的,或是氢原子;并且y表示大于或等于2且小于或等于20的整数。
根据一个更具体的方案,式(IX)化合物是选自十甘油基油酸酯,十甘油基异硬脂酸酯,十甘油基单月桂酸酯,十甘油基单亚油酸酯和十甘油基单肉豆蔻酸酯。
在作为本发明主题的配制剂(F)的定义中,术语“烷氧基化聚甘油酯”表示式(X)化合物:
其中Z1表示式R'2-C(=O)-的酰基,其中R'2表示饱和或不饱和的、直链或支化的具有11-35个碳原子的脂族烃基,更特别是选自以下的基团:十二烷酰基,十四烷酰基,十六烷酰基,十八烷酰基,二十烷酰基,二十二烷酰基,油基,亚油基,亚麻基和异硬脂基;Z1’表示上述式R'2-C(=O)-的酰基,Z1’可以是与Z1相同或不同的,或是氢原子;R3表示氢原子、甲基或乙基;y1表示大于或等于2且小于或等于20的整数;v1、v2和v3可以是相同或不同的,表示大于或等于0且小于或等于50的整数,并且总和[(y1.v1)+(y1.v2)+v3)]是大于或等于1且小于或等于50的整数。
在作为本发明主题的配制剂(F)的定义中,术语“聚二醇聚羟基硬脂酸酯”表示式(XI)化合物:
其中y2表示大于或等于2且小于或等于50的整数,R4表示氢原子、甲基或乙基,并且Z2表示式(XII)的基团:
其中y'2表示大于或等于0且小于或等于10的整数,更特别是大于或等于1且小于或等于10的整数;Z'2表示上述式(XII)基团,其中Z2'是与Z2相同或不同的,或是氢原子。
在作为本发明主题的配制剂(F)的定义中,术语“聚甘油聚羟基硬脂酸酯”表示式(XIII)化合物:
其中Z3表示上述式(XII)基团;Z'3表示上述式(XII)基团,其中Z3’可以是与Z3相同或不同的,或是氢原子;y3表示大于或等于2且小于或等于20的整数。
在作为本发明主题的配制剂(F)的定义中,术语“烷氧基化聚甘油聚羟基硬脂酸酯”表示式(XIV)化合物:
其中Z4表示上述式(XII)基团;Z'4表示上述式(XII)基团,其中Z4'可以是与Z4相同或不同的,或是氢原子;y4表示大于或等于2且小于或等于20的整数;v'1、v'2和v'3可以是相同或不同的,表示大于或等于0且小于或等于50的整数,并且总和[(y4.v'1)+(y4.v'2)+v'3)]是大于或等于1且小于或等于50的整数。
根据另一个具体方案,本发明的主题是上述配制剂(F),其特征在于所述乳化体系(S)由组合物(C4)组成,组合物(C4)按其100质量%计包含:
-15-25质量%的至少一种由式(VII)表示的组合物(C2):
R1-O-(G)x-H (VII)
其中x表示在1.05和2.5之间的小数,G表示木糖残基,并且R1表示2-辛基十二烷基,所述组合物(C2)是由式(VII1)、(VII2)、(VII3)、(VII4)和(VII5)表示的化合物的混合物:
R1-O-(G)1-H (VII1)
R1-O-(G)2-H (VII2)
R1-O-(G)3-H (VII3)
R1-O-(G)4-H (VII4)
R1-O-(G)5-H (VII5)
其各自的摩尔比例是a1、a2、a3、a4和a5,使得:
-总和a1+a2+a3+a4+a5是等于1,并且
-总和a1+2a2+3a3+4a4+5a5是等于x;
-55-65质量%的至少一种式(VIII)脂肪醇:
R'1-OH (VIII),
其中R’1表示2-辛基十二烷基;
-10-30质量%的至少一种由式(XI)表示的聚二醇聚羟基硬脂酸酯:
其中y2表示大于或等于2且小于或等于50的整数,R4表示氢原子、甲基或乙基,并且Z2表示式(XII)基团:
其中y'2表示大于或等于0且小于或等于10的整数,更特别是大于或等于1且小于或等于10的整数;并且Z'2表示上述式(XII)基团,其中Z2'是与Z2相同或不同的,或是氢原子。
根据另一个具体方案,本发明的主题是上述配制剂(F),其特征在于在25℃温度下使用Brookfield LVT粘度计在6rpm速度下检测,所述配制剂(F)的动态粘度是大于或等于500mPa.s且小于或等于40000mPa.s。
本发明的主题也是根据本发明的组合物(C1),其可以局部施加,用于清洁和/或保护和/或护理人体或动物的皮肤、头发、头皮、指甲、唇部、眼睫毛或眉毛。
相似地,本发明的主题也是根据本发明的配制剂(F),其可以局部施加,用于清洁和/或保护和/或护理人体或动物的皮肤、头发、头皮、指甲、唇部、眼睫毛或眉毛。
上述用于局部应用的组合物(C1)和用于局部应用的配制剂(F)可以用手指或施加器施加到人的皮肤上,例如预先用上述用于局部应用的组合物(C1)和用于局部应用的配制剂(F)浸渍的刷子、海绵或湿巾。
作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)可以加压方式包装在气溶胶装置或“泵-瓶”型装置中,包装在配备多孔壁的装置、例如栅格中,或包装在配备球形施加器的装置(称为“滚轮”)中。
作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)可以用作清洁乳或卸妆乳,清洁液或卸妆液,用于面部或身体的泡沫凝胶,用于清洁头发和/或头皮的洗发液,用于处理头发和/或头皮的头发调理剂,泡泡浴,用于护理或保护面部、手部或身体的霜、乳或液,例如用于抵抗太阳辐射的试剂,自晒黑剂,抗老化剂,抗皱剂,舒缓剂或润湿剂。
作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)也可以包括在用于局部应用的配制剂领域中常用的赋形剂和/或活性物质,特别是皮肤化妆品、药物或皮肤药物配制剂。
所以,根据另一个具体方案,本发明的主题是上述用于局部应用的组合物(C1)和配制剂(F),其特征在于它们也包含一种或多种选自以下的辅助化合物:发泡和/或洗涤用表面活性剂,增稠和/或胶凝表面活性剂,增稠和/或胶凝剂,稳定剂,成膜化合物,溶剂和助溶剂,水溶助长剂,增塑剂,乳化剂和助乳化剂,不透明剂,珠光剂,超加脂剂,螯合剂,螯合试剂,抗氧化剂,香料,精油,防腐剂,调理剂,除臭剂,用于身体头发和皮肤漂白的漂白剂,用于向皮肤或头发提供处理和/或保护作用的活性物质,防晒剂,矿物填料或颜料,给予视觉效果或用于包封活性试剂的颗粒,剥落剂粒子,纹理试剂,荧光增白剂和驱虫剂。
作为可以存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的发泡和/或洗涤用表面活性剂的例子,可以提到在此活性领域中常用的局部可接受的阴离子性、阳离子性、两亲性或非离子性的发泡和/或洗涤用表面活性剂。
在可与作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)组合使用的发泡和/或洗涤用阴离子性表面活性剂中,可以提到以下的碱金属盐、碱土金属盐、铵盐、胺盐或氨基醇盐:烷基醚硫酸盐,烷基硫酸盐,烷基酰氨基醚硫酸盐,烷基芳基聚醚硫酸盐,单酸甘油酯硫酸盐,α-烯烃磺酸盐,链烷磺酸盐,烷基磷酸盐,烷基醚磷酸盐,烷基磺酸盐,烷基酰胺磺酸盐,烷基芳基磺酸盐,烷基羧酸盐,烷基磺基琥珀酸盐,烷基醚磺基琥珀酸盐,烷基酰胺磺基琥珀酸盐,烷基磺基乙酸盐,烷基肌氨酸盐,酰基羟乙基磺酸盐,N-酰基氨基乙磺酸盐,酰基乳酸盐,N-酰基氨基酸衍生物,N-酰基肽衍生物,N-酰基蛋白质衍生物或脂肪酸。
在可与作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)组合使用的发泡和/或洗涤用两亲性表面活性剂中,可以提到烷基甜菜碱,烷基酰氨基甜菜碱,甜菜碱,烷基酰氨基烷基磺基甜菜碱,咪唑啉衍生物,磷基甜菜碱,两性聚乙酸盐和两性丙酸盐。
在可与作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)组合使用的发泡和/或洗涤用阳离子性表面活性剂中,可以特别提到季铵衍生物。
在可与作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)组合使用的发泡和/或洗涤用非离子性表面活性剂中,可以更特别提到蓖麻油衍生物,聚山梨醇酯,椰壳酰胺和N-烷基胺。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的增稠和/或胶凝表面活性剂的例子,可以提到:
-任选烷氧基化的烷基聚糖苷脂肪酯,更特别是乙氧基化甲基聚葡糖苷酯,例如PEG 120甲基葡萄糖三油酸酯和PEG 120甲基葡萄糖二油酸酯,分别以商品名GlucamateTMLT和GlucamateTM DOE120销售;
-烷氧基化脂肪酯,例如以商品名CrothixTM DS53销售的PEG150季戊四醇四硬脂酸酯,或以商品名AntilTM 141销售的PEG55丙二醇油酸酯;
-脂肪链聚亚烷基二醇氨基甲酸酯,例如以商品名ElfacosTM T211销售的PPG14月桂醇聚醚异佛尔基二氨基甲酸酯,或以商品名ElfacosTM GT2125销售的PPG 14 Palmeth 60己基二氨基甲酸酯。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的乳化表面活性剂的例子,可以提到非离子性表面活性剂、阴离子性表面活性剂和阳离子性表面活性剂.
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的乳化非离子性表面活性剂的例子,可以提到山梨醇的脂肪酸酯,例如以商品名MontaneTM 80和MontaneTM 85和MontaneTM 60销售的产品;乙氧基化蓖麻油和乙氧基化氢化蓖麻油,例如以商品名SimulsolTM 989销售的产品;含有硬脂酸甘油基酯和聚(乙氧基化)硬脂酸与5-150摩尔环氧乙烷的组合物,例如含有硬脂酸(乙氧基化)与135摩尔环氧乙烷和硬脂酸甘油基酯的组合物,以商品名SimulsolTM 165销售;乙氧基化失水山梨醇酯,例如以商品名MontanoxTM销售的产品;失水甘露糖醇酯;乙氧基化失水甘露糖醇酯;蔗糖酯;甲基葡糖苷酯。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的乳化阴离子性表面活性剂的例子,可以提到癸基磷酸盐,以商品名AmphisolTM销售的鲸蜡基磷酸盐,甘油基硬脂酸盐,柠檬酸盐;十六/十八烷基硫酸盐;花生基/山嵛基磷酸盐和花生基/山嵛基醇组合物,以商品名SensanovTM WR销售;皂,例如硬脂酸钠或硬脂酸三乙醇铵,盐化氨基酸的N-酰基衍生物,例如硬脂酰基谷氨酸盐。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的乳化阳离子性表面活性剂的例子,可以提到氧化胺,季铵盐-82和在专利申请WO 96/00719中所述的表面活性剂,以及主要是其中脂肪链包含至少16个碳原子的那些。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的不透明剂和/或珠光剂的例子,可以提到棕榈酸钠,硬脂酸钠,羟基硬脂酸钠,棕榈酸镁,硬脂酸镁,羟基硬脂酸镁,乙二醇单硬脂酸酯,乙二醇二硬脂酸酯,聚乙二醇单硬脂酸酯,聚乙二醇二硬脂酸酯和具有12-22个碳原子的脂肪醇。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的纹理试剂的例子,可以提到N-酰基氨基酸衍生物,例如以商品名AminohopeTMLL销售的月桂酰基赖氨酸,以商品名SepifineTM销售的巴巴苏淀粉,以商品名DryfloTM销售的辛烯基淀粉琥珀酸盐,以商品名MontanovTM 14销售的肉豆蔻基聚葡糖苷,纤维素纤维,棉纤维,壳聚糖纤维,滑石,绢云母和云母。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的溶剂和助溶剂的例子,可以提到水,有机溶剂,例如甘油,双甘油,甘油低聚物,乙二醇,丙二醇,丁二醇,己二醇,二甘醇,木糖醇,赤藓醇,山梨醇,水溶性醇例如乙醇、异丙醇或丁醇,水和所述有机溶剂的混合物,碳酸亚丙基酯,碳酸亚乙基酯和苄基醇。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的用于改进皮肤穿透性的试剂的例子,可以提到二醇醚,例如乙二醇单甲基醚,乙二醇单乙基醚,乙二醇单丙基醚,乙二醇单异丙基醚,乙二醇单丁基醚,乙二醇单苯基醚,乙二醇单苄基醚,二甘醇单甲基醚,二甘醇单乙基醚和二甘醇单-正丁基醚,二甘醇单乙基醚(或Transcutol-P),脂肪酸,例如油酸,甘油的脂肪酸酯,例如山嵛酸甘油基酯,棕榈硬脂酸甘油基酯,山嵛酰基聚甘油酯,聚氧乙烯基-2-硬脂基醚,聚氧乙烯基-2-油基醚,萜烯,例如D-柠檬烯,以及精油,例如尤加利精油。
关于可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的除臭剂的例子,可以提到碱性硅酸盐,锌盐例如硫酸锌、葡萄糖酸锌、氯化锌或乳酸锌;季铵盐,例如鲸蜡基三甲基铵盐或鲸蜡基吡啶盐;甘油衍生物,例如甘油基癸酸酯,甘油基辛酸酯和聚甘油基癸酸酯;1,2-癸二醇,1,3-丙二醇;水杨酸;碳酸氢钠;环糊精;金属沸石;TriclosanTM;水合溴化铝,水合氯化铝,氯化铝,硫酸铝,水合氯化铝锆,三水合氯化铝锆,四水合氯化铝锆,五水合氯化铝锆,八水合氯化铝锆,硫酸铝,乳酸钠铝,水合氯化铝和二醇的络合物,例如水合氯化铝和丙二醇的络合物,二水合氯化铝和丙二醇的络合物,倍半水合氯化铝和丙二醇的络合物,水合氯化铝和聚乙二醇的络合物,二水合氯化铝和聚乙二醇的络合物,或倍半水合氯化铝和聚乙二醇的络合物。
作为可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的抗氧化剂的例子,可以提到EDTA及其盐,柠檬酸,酒石酸,草酸,BHA(丁基羟基茴香醚),BHT(丁基羟基甲苯),生育酚衍生物,例如生育酚基乙酸酯,抗氧化剂化合物的混合物,例如Dissolvine GL 47S(INCI名称:谷氨酸二乙酸四钠)。
本发明的组合物(C1)和配制剂(F)可以包含生物活性试剂。
在可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的活性物质中,可以提到:
-维生素及其衍生物,特别是其酯,例如视黄醇(维生素A)及其酯(例如视黄醇基棕榈酸酯),抗坏血酸(维生素C)及其酯,抗坏血酸的糖衍生物(例如抗坏血酸基葡糖苷),生育酚(维生素E)及其酯(例如生育酚基乙酸酯),维生素B3或B10(烟酰胺及其衍生物);
-具有舒缓作用的化合物,特别是SepicalmTM S,尿囊素,红没药醇,以商品名TECATM销售的产品(积雪草的提取物);
-抗炎试剂,例如非甾体抗炎药(或NSAID),更特别是芳基乙酸(或芳基链烷醇)衍生物和2-芳基丙酸(或洛芬类),甚至更特别是双氯芬酸,噻洛芬酸,阿米洛芬,依托度酸,氟比洛芬,布洛芬,酮洛芬和萘普生;
-镇痛和抗炎试剂,更特别是对乙酰氨基酚,阿斯匹林,水杨酸,水杨酸甲基酯,胆碱水杨酸酯,二醇水杨酸酯,1-薄荷醇,樟脑,甲芬那酸,氯灭酸,吲哚美辛,丙替嗪酸,氯苯噻乙酸,托美汀,噻洛芬酸,保泰松,羟基保泰松,氯非宗,喷他佐辛,嘧吡唑,氢化可的松,可的松,地塞米松,肤轻松,氟羟脱氢皮质醇,甲羟松,氢化泼尼松,氟缩酮氢可松,泼尼松,哈西奈德,甲基强的松龙,氟氢可的松,皮质脂酮,帕拉米松和倍他米松;
-防腐剂,更特别是西曲溴铵,聚乙烯吡咯烷酮-碘,双氯苯双胍己烷,碘,苯扎氯铵,苯甲酸,硝基呋喃腙,过氧化苯甲酰,过氧化氢,六氯酚,苯酚,间苯二酚和乙酰基氯化吡啶
-杀虫剂,更特别是敌百虫,杀虫脲,倍硫磷,恶虫威,环丙氨嗪,伏虫脲,地昔尼尔,吡虫隆,阿米曲拉,溴氰菊酯,氯氰菊酯,毒虫威,氟氯苯菊酯,伊维菌素,阿巴美丁,阿维菌素,多拉菌素,莫西菌素zeta-氯氰菊酯,二嗪农,多杀菌素,吡虫啉,烯啶虫胺,蚊蝇醚,氟虫腈,赛灭磷,虱螨脲,赛拉菌素,米尔贝肟,毒死蜱,蝇毒磷,巴胺磷,α-氯氰菊酯,高顺式氯氰菊酯,伊维菌素,除虫脲,环戊二烯类杀虫剂,氨基甲酸酯和苯甲酰基脲;
-抗菌剂,更特别是磺酰胺,氨基苷,例如新霉素,妥布霉素,庆大霉素,阿米卡霉素,卡那霉素,奇放线菌素,巴龙霉素,奈替米星,多肽,头孢菌素,唑烷酮,例如环丙沙星、左氧氟沙星和氧氟沙星;
-具有润湿作用的化合物,例如脲,羟基脲,甘油基葡糖苷,双甘油基葡糖苷,聚甘油基葡糖苷,甘油,双甘油,以商品名AquaxylTM销售的木糖基聚葡糖苷,麦芽糖醇,山梨醇基聚葡糖苷,透明质酸及其盐,例如透明质酸钠、透明质酸钾,更特别是分子量为20-5000kDa、尤其500-2200kDa的透明质酸或透明质酸盐;
-富含多酚的植物提取物,例如葡萄提取物,松树提取物,葡萄酒提取物和橄榄提取物;
-具有纤瘦或脂肪分解作用的化合物,例如咖啡因或其衍生物,AdiposlimTM,AdipolessTM,以及岩藻黄质;
-N-酰基蛋白;N-酰基肽,例如MatrixilTM;N-酰基氨基酸;N-酰基蛋白的部分水解物;氨基酸;肽;全蛋白水解物;
-植物提取物,例如大豆提取物,例如RaffermineTM,小麦提取物,例如TensineTM或GliadineTM,植物提取物,例如富含鞣酸的植物提取物和富含异黄酮的植物提取物或富含萜烯的植物提取物;淡水或海水藻提取物,海洋植物提取物;常规海洋提取物,例如珊瑚虫;基础蜡;细菌提取物;
-神经酰胺;
-磷脂;
-具有抗微生物作用或具有纯化作用的化合物,例如LipacideTM C8G,LipacideTMUG,SepicontrolTM A5;OctopiroxTM或SensivaTM SC50;
-具有提供能量或模拟性能的化合物,例如PhysiogenylTM,泛醇及其衍生物,例如SepicapTM MP;
-抗老化活性剂,例如SepiliftTM DPHP,LipacideTM PVB,SepivinolTM,SepivitalTM,ManolivaTM,Phyto-AgeTM,TimecodeTM或SurvicodeTM;
-用于抵抗光老化的活性试剂;用于保护真皮-表皮连接完整性的活性试剂;用于增加细胞外基质组分的合成的活性试剂,例如胶原蛋白、弹性蛋白和粘多糖;对化学细胞交流起有利作用的活性试剂,例如细胞活素,或对物理细胞交流起有利作用的活性试剂,例如整联蛋白;
-使皮肤产生“加热”感觉的活性试剂,例如皮肤微循环活化剂(例如烟酸衍生物),或使皮肤产生“清新”感觉的产品(例如薄荷醇及其衍生物);
-能改进皮肤微循环的活性试剂,例如静脉注射(venotonic)试剂;排水活性试剂;消除充血的活性试剂,例如以下植物的提取物:银杏,常春藤,七叶树,竹子,金雀花,假叶树,积雪草,墨角藻,迷迭香或柳树;
-用于使皮肤变黑或变棕色的试剂,例如二羟基丙酮(DHA),赤藓酮糖,内消旋酒石醛,戊二醛,甘油醛,阿脲,茚三酮,植物提取物,例如紫檀属和非洲小叶紫檀属的红木提取物,例如小叶紫檀,奥孙紫檀,亚花梨,刺猬紫檀,印度紫檀或非洲小叶紫檀,例如在欧洲专利申请EP 0 971 683中所述的那些;
-已知能促进和/或加速人皮肤变黑和/或变棕色和/或给人皮肤染色的试剂,例如类胡萝卜素(更特别是β-胡萝卜素和γ-胡萝卜素),由Provital公司以商品名Carrotoil销售的产品(INCI名称:野胡萝卜,向日葵花油),其含有类胡萝卜素、维生素E和维生素K;酪氨酸和/或其衍生物,已知其对加速使人皮肤变黑以及暴露于紫外辐射下有作用,例如由Provital公司以商品名SunTan AcceleratorTM销售的产品,其含有酪氨酸和核黄素(维生素B);由Zymo Line公司以商品名Zymo Tan Complex销售的酪氨酸和酪氨酸酶复合物,由Mibelle公司以商品名MelanoBronzeTM销售的产品(INCI名称:乙酰基酪氨酸,蒙克胡椒提取物(穗花牡荆)),其含有乙酰基酪氨酸;由Unipex公司以商品名Unipertan VEG-24/242/2002销售的产品(INCI名称:丁二醇和乙酰基酪氨酸和水解植物蛋白和三磷酸腺苷);由Sederma公司以商品名Try-ExcellTM销售的产品(INCI名称:油酰基酪氨酸和丝瓜(籽)油和油酸),其含有西葫芦种子的提取物(或丝瓜油);由Alban Muller公司以商品名ActibronzeTM销售的产品(INCI名称:水解麦蛋白和乙酰基酪氨酸和葡萄糖酸铜);由Synerga公司以商品名TyrostanTM销售的产品(INCI名称:己酰基酪氨酸钾);由Synerga公司以商品名Tyrosinol销售的产品(INCI名称:失水山梨醇异硬脂酸酯,油酸甘油基酯,己酰基酪氨酸);由Alban Muller公司以商品名InstaBronzeTM销售的产品(INCI名称:二羟基丙酮和乙酰基酪氨酸和葡萄糖酸铜);由Exymol公司以商品名Tyrosilane销售的产品(INCI名称:甲基硅烷醇和乙酰基酪氨酸);已知对活化黑色素生成有作用的肽,例如由InfinitecActivos公司以商品名Bronzing SF肽粉末销售的产品(INCI名称:葡聚糖和八肽-5);以商品名Melitane销售的产品(INCI名称:甘油和水和葡聚糖和乙酰基六肽-1),其含有乙酰基六肽-1,已知其具有α-MSH-激动剂作用,由Lipotec公司以商品名Melatimes SolutionsTM销售的产品(INCI名称:丁二醇、棕榈酰基三肽-40);糖和糖衍生物,例如由Provital公司以商品名TanositolTM销售的产品(INCI名称:纤维醇),由Codif International公司以商品名ThalitanTM销售的产品(或PhycosaccharideTM AG)(INCI名称:水和水解藻胶(掌状海带)和硫酸镁和硫酸锰),其含有海洋来源的低聚糖(与镁和锰离子螯合的古罗糖醛酸和甘露糖醛酸),由Alban Muller公司以商品名MelactivaTM销售的产品(INCI名称:麦芽糖糊精,虎爪豆种子提取物);富含类黄酮的化合物,例如由Silab公司以商品名Biotanning销售的产品(INCI名称:水解的甜橙果提取物),已知其富含柠檬类黄酮(橘皮苷类型)。
关于任选地存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的防晒剂的例子,可以提到在修订版化妆品指南76/768/EEC,附录II中列出的那些。
在任选地存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的有机防晒剂中,可以提到:
-苯甲酸衍生物,例如对-氨基苯甲酸(PABA),特别是PABA的单甘油基酯,N,N-丙氧基PABA的乙基酯,N,N-二乙氧基PABA的乙基酯,N,N-二甲基PABA的乙基酯,N,N-二甲基PABA的甲基酯,N,N-二甲基PABA的丁基酯;
-邻氨基苯甲酸衍生物,例如均孟基-N-乙酰基邻氨基苯甲酸酯;
-水杨酸衍生物,例如水杨酸戊基酯,水杨酸均孟基酯,水杨酸乙基己基酯,水杨酸苯基酯,水杨酸苄基酯,水杨酸对-异丙基苯基酯;
-肉桂酸衍生物,例如肉桂酸乙基己基酯,肉桂酸乙基-4-异丙基酯,肉桂酸甲基-2,5-二异丙基酯,肉桂酸对-甲氧基丙基酯,肉桂酸对-甲氧基异丙基酯,肉桂酸对-甲氧基异戊基酯,肉桂酸对-甲氧基辛基酯(对-甲氧基2-乙基己基肉桂酸酯),肉桂酸对-甲氧基2-乙氧基乙基酯,肉桂酸对-甲氧基环己基酯,肉桂酸乙基-α-氰基-β-苯基酯,肉桂酸2-乙基己基-α-氰基-β-苯基酯,甘油基二-对-甲氧基单-2-乙基己酰基肉桂酸酯;
-苯甲酮衍生物,例如2,4-二羟基苯甲酮,2,2'-二羟基-4-甲氧基苯甲酮,2,2',4,4'-四羟基苯甲酮,2-羟基-4-甲氧基苯甲酮,2-羟基-4-甲氧基-4'-甲基苯甲酮,2-羟基-4-甲氧基苯甲酮5-磺酸酯,4-苯基苯甲酮,2-乙基己基-4'-苯基苯甲酮2-羧酸酯,2-羟基-4-正-辛氧基苯甲酮,4-羟基-3-羧基苯甲酮;3-(4'-甲基亚苄基)-d,l-樟脑,3-(亚苄基)-d,l-樟脑,樟脑甲基硫酸苯扎铵;尿刊酸,尿刊酸乙基酯;磺酸衍生物,例如2-苯基苯并咪唑-5-磺酸及其盐;
-三嗪衍生物,例如羟基苯基三嗪,(乙基己氧基羟基苯基)(4-甲氧基苯基)三嗪,2,4,6-三苯氨基(对-碳-2'-乙基己基-1'-氧基)-1,3,5-三嗪,4,4-((6-(((1,1-二甲基乙基)氨基)羰基)苯基)氨基)-1,3,5-三嗪-2,4-二基二亚氨基)二(2-乙基己基)苯甲酸酯,2-苯基-5-甲基苯并唑,2,2'-羟基-5-甲基苯基苯并三唑,2-(2'-羟基-5'-叔辛基苯基)苯并三唑,2-(2'-羟基-5'-甲基苯基)苯并三唑;二苄肼;二茴香醚基甲烷,4-甲氧基-4”-叔丁基苯甲酰基甲烷;5-(3,3-二甲基-2-亚降冰片基)-3-戊烷-2-酮;
-二苯基丙烯酸酯衍生物,例如2-氰基-3,3-二苯基-2-丙烯酸2-乙基己基酯或2-氰基-3,3-二苯基-2-丙烯酸乙基酯;
-聚硅氧烷,例如亚苄基硅氧烷丙二酸酯。
在可存在于作为本发明主题的用于局部应用的组合物(C1)和配制剂(F)中的矿物防晒剂,也称为“矿化防晒剂”,可以提到氧化钛,氧化锌,氧化铈,氧化锆,黄色、红色或黑色氧化铁,以及氧化铬。这些矿物防晒剂可以被微米化或未微米化,可以进行或不进行表面处理,和可以任选地是含水或油状的预分散体的形式。
制备上述组合物(C1)的方法包括以下步骤:
-步骤a):在25℃温度下向合适体积的罐中加入天然矿质水或泉水或海水或海藻水以制备水相;可以加入软化水以通过稀释达到所需的电导率值,此值是大于或等于300μS.cm-1,
-步骤b):在合适的机械搅拌和在25℃下向预先制得的水相加入交联的阴离子性聚电解质(P1),并保持搅拌直至观察到介质胶凝,和
-步骤c):在合适的机械搅拌和在25℃下,向预先制得的胶凝的水相加入半乳甘露聚糖(GM),并保持搅拌直至观察到均匀的凝胶。
制备上述配制剂(F)的方法包括以下步骤:
-步骤a):通过按照所需比例混合所有组分来制备脂肪相(A2)。此混合步骤通常在大于或等于25℃且小于或等于80℃的温度下进行,更特别是大于或等于25℃且小于或等于60℃,甚至更特别是大于或等于25℃且小于或等于40℃;这在中等速度为大于或等于50rpm且小于或等于100rpm的机械搅拌下进行;
-步骤b):如上文所述制备组合物(C1);尤其是,通过在25℃下用Brookfield LV粘度计在6rpm速度下检测,在步骤b)结束时得到的水相(A1)具有大于或等于200mPa.s且小于或等于40,000mPa.s的动态粘度,更特别是大于或等于1000mPa.s且小于或等于40,000mPa.s,甚至更特别是大于或等于2000mPa.s且小于或等于40,000mPa.s;
-步骤c):在此期间,在中等速度为大于或等于50rpm且小于或等于400rpm的机械搅拌下,在大于或等于25℃且小于或等于80℃的温度下将脂肪相(A2)加入组合物(C1)中,更特别是大于或等于25℃且小于或等于60℃,甚至更特别是大于或等于25℃且小于或等于40℃,由此得到配制剂(F)。
以下实施例用于说明本发明,但不限制本发明的范围。
制备并评价本发明的含水凝胶和对比含水凝胶:
1)制备含水凝胶:
通过以下方法制备表示为(F1)至(F4)的四种本发明的含水凝胶,以及表示为(F'1)至(F'8)的八种对比含水凝胶,它们的质量比例和成分列于表1中。
水相是通过在25℃下按照相应的比例加入具有电导率的水和软化水制备,从而得到具有所需电导率的水相(例如在以下实验中的730μS/cm或3.28mS/cm)。然后,将所研究的交联的阴离子性聚电解质在25℃下在中等机械搅拌下逐步加入预先制得的水中,即用锚式搅拌头和在50-150rpm的速度下搅拌,直到获得均匀的凝胶。将所研究的半乳甘露聚糖(GM)在25℃温度下在搅拌下加入预先形成的凝胶中,搅拌使用配备锚式搅拌头的机械搅拌器进行。然后,搅拌保持10分钟,冷却步骤不是必要的。
2)评价含水凝胶的性能:
通过以下方式控制含水凝胶的性能:
-评价所制得的凝胶的外观,寻求在25℃下凝胶的均匀目测外观,和
-于25℃检测所制得的凝胶的动态粘度。
表征和检测结果如下表1所示。
[表1]
表1:本发明的含水凝胶(F1)和对比含水凝胶(F'1)(F'2)(F'3)(F'4)和(F'5)的组成和表征
表1(续):本发明的含水凝胶(F2)、(F3)和(F4)和对比含水凝胶(F'6)(F'7)和(F'8)的组成和表征
(1)HydralixirTM LD(INCI名称:水和掌状海带提取物)是来自褐藻的细胞水,从掌状海带得到。
(2)SolagumTM AX(INCI名称:阿拉伯胶和黄原胶)是用于制备化妆品组合物的增稠剂和稳定剂。
(3)SolagumTM Tara(INCI名称:刺云实胶)是半乳甘露聚糖,具有1/3的取代度,作为用于制备化妆品组合物的增稠剂和稳定剂。
(4)SepinovTM EMT 10(INCI名称:丙烯酸羟基乙基酯/丙烯酰基二甲基氨基乙磺酸钠共聚物)是增稠剂、稳定剂和乳化剂,其是粉末形式并用于制备化妆品组合物。
(5)SimulgelTM EG(INCI名称:丙烯酸钠/丙烯酰基二甲基氨基乙磺酸钠共聚物&异十六烷&聚山梨酯80)是增稠剂、稳定剂和乳化剂,其是自可逆转的反相胶乳的形式,用于制备化妆品组合物。
(6):SepigelTM 305:INCI名称:聚丙烯酰胺(和)C13-14异链烷烃(和)月桂醇聚醚-7)是增稠剂、稳定剂和乳化剂,其是自可逆转的反相胶乳的形式,用于制备化妆品组合物。
(*):SimulgelTM EG是自可逆转的反相胶乳的形式,其中交联的阴离子性聚电解质的含量是40%。
(**):SepigelTM 305是自可逆转的反相胶乳的形式,其中交联的阴离子性聚电解质的含量是40%。
3)分析结果
质量含量为0.5%的塔拉胶和1.5质量%的以商品名SepinovTM EM10销售的交联的阴离子性聚电解质的组合使用使得能获得具有很高粘度的含水凝胶(F1)(对于(F1),190000mPa.s),而用质量比例为1.5%的SepinovTM EMT 10获得的含水凝胶(F’1)仅能达到48000mPa.s的粘度。
在用阿拉伯胶和黄原胶的混合物代替塔拉胶的情况下,没有观察到产生具有高粘度的含水凝胶:所得的对比凝胶(F’2)的粘度是41100mPa.s,即非常接近仅仅用以商品名SepinovTM EM10销售的交联阴离子性聚电解质制得的含水凝胶(F’1)的粘度水平。
仅仅用塔拉胶在各种剂量(分别为0.5%、1%和1.5%)下得到的对比凝胶(F'3)、(F'4)和(F'5)的粘度显示相应的粘度值为240mPa.s、5000mPa.s和41000mPa.s,因此不影响通过组合使用0.5%塔拉胶和1.5质量%的以商品名SepinovTM EM10销售的交联阴离子性聚电解质得到的粘度水平。
当塔拉胶与交联的阴离子性聚电解质组合使用时,也观察到这种高粘度,其中所述交联阴离子性聚电解质的聚合物主链具有不同的性质:基于丙烯酸钠和丙烯酰基二甲基氨基乙磺酸钠的交联共聚物(对于本发明的含水凝胶(F2)是170000mPa.s),或基于丙烯酰胺和丙烯酰基二甲基氨基乙磺酸钠的交联共聚物(对于本发明的含水凝胶(F3)是220000mPa.s)。
另外,通过比较根据本发明的含水凝胶(F4)的粘度与对比含水凝胶(F'8)的粘度,也证明了当水相的电导率较高(对于(F4)和(F'8)是3.28mS/cm)时的此组合的协同效果。
Claims (11)
1.一种用于局部应用的组合物(C1),其是凝胶的形式,其包含按其100质量%计的以下组分:
-93-99.4质量%的水,其具有于25℃检测的电导率为大于或等于300微西门子/厘米(或μS.cm-1),
-0.5-5质量%的交联的阴离子性聚电解质(P1),其选自以下聚合物:
-以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与以钠盐形式部分或完全盐化的丙烯酸(δ)按照摩尔比率(γ)/(δ)为大于或等于40/60且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;
-以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与丙烯酸羟基乙基酯(ζ)按照摩尔比率(γ)/(ζ)为大于或等于30/70且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;
-以钠盐形式部分或完全盐化的2-甲基-2-[(1-氧基-2-丙烯基)氨基]-1-丙磺酸(γ)与丙烯酰胺(ε)按照摩尔比率(γ)/(ε)为大于或等于30/70且小于或等于90/10形成的共聚物,其用三烯丙基胺和/或亚甲基双(丙烯酰胺)交联;
和
-0.1-2质量%的至少一种半乳甘露聚糖(GM),所述半乳甘露聚糖具有1/3的取代度。
2.根据权利要求1所述的组合物(C1),其特征在于所述半乳甘露聚糖是塔拉胶。
3.根据权利要求1或2所述的组合物(C1),其特征在于所述水是海藻水与软化水的混合物。
4.根据权利要求3所述的组合物(C1),其特征在于所述海藻水选自来自掌状海带的水、来自角叉菜的水和来自星芒杉藻的水。
5.根据权利要求1或4所述的组合物(C1),其特征在于半乳甘露聚糖(GM)与交联的阴离子性聚电解质(P1)之间的质量比率是大于或等于0.15且小于或等于0.75。
6.一种用于局部应用的配制剂(F),其包含按其100质量%计的以下组分:
-60-90质量%的根据权利要求1-5中任一项所述的用于局部应用的组合物(C1);和
-10-40质量%的脂肪相(A2),其包含i)至少一种油和ii)含有至少一种乳化表面活性剂(S1)的乳化体系。
7.根据权利要求6所述的配制剂,其特征在于乳化表面活性剂(S1)是选自烷基聚糖苷组合物,烷基聚糖苷和脂肪醇的组合物,聚甘油酯,烷氧基化聚甘油酯,聚二醇聚羟基硬脂酸酯,聚甘油聚羟基硬脂酸酯和烷氧基化聚甘油聚羟基硬脂酸酯。
8.根据权利要求1-5中任一项所述的组合物(C1)通过局部施加用于清洁和/或保护和/或护理人体或动物的皮肤、头发、头皮、指甲、唇部、眼睫毛或眉毛的用途。
9.根据权利要求6或7所述的配制剂(F)通过局部施加用于清洁和/或保护和/或护理人体或动物的皮肤、头发、头皮、指甲、唇部、眼睫毛或眉毛的用途。
10.根据权利要求1-5中任一项所述的组合物(C1),其特征在于该组合物包含生物活性试剂。
11.根据权利要求6或7所述的配制剂(F),其特征在于该配制剂包含生物活性试剂。
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