CN109562082A - 抗痤疮组合物和使用方法 - Google Patents
抗痤疮组合物和使用方法 Download PDFInfo
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- CN109562082A CN109562082A CN201780047145.9A CN201780047145A CN109562082A CN 109562082 A CN109562082 A CN 109562082A CN 201780047145 A CN201780047145 A CN 201780047145A CN 109562082 A CN109562082 A CN 109562082A
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Abstract
本公开涉及化妆品组合物和使用该化妆品组合物来改善皮肤外观的方法。例如,该化妆品组合物可用于治疗痤疮、治疗炎症、向皮肤提供抗衰老益处等。该化妆品组合物通常包括化妆品可接受的载体、包含以下物质的皮肤活性成分的组合:(i)硫磺;(ii)烟酰胺;和(iii)苯乙基间苯二酚。
Description
公开领域
本公开涉及化妆品组合物和使用该化妆品组合物来改善皮肤外观的方法。例如,该化妆品组合物可用于治疗痤疮或向皮肤提供抗衰老益处。
背景
痤疮经常影响青少年,但是它在成年人中也成问题。虽然发展痤疮的确切原因尚未完全确定,但是据信牵涉下列因素的组合:(a)皮脂的过度产生;(b)毛囊管入口的堵塞;以及(c)由细菌的过度发展引起的炎性过程。过度的皮脂产生的原因之一是雄激素的活性增加,雄激素刺激皮脂腺,以便提高皮脂的产生。炎性反应是对毛囊管(follicular duct)被角质栓堵塞的反应。同时观察到毛囊管的角化过度,在毛皮脂腺囊中产生富含用于细菌群落的营养素,且尤其促进诸如丙酸杆菌(痤疮丙酸杆菌、颗粒丙酸杆菌、贪婪丙酸杆菌)之类的类白喉厌氧病菌的增殖,并因此促进皮肤炎症的环境。
痤疮的基本损害是微小粉刺。皮脂和角质碎片的积累导致可见的闭合性粉刺或白头,且其持续的胀大引起开放性粉刺或黑头。黑头的黑色归因于氧化的黑色素。黑头和微囊是痤疮的非炎性损害,但是一些粉刺演变成炎性丘疹、脓疱或结节,并可变成慢性肉芽肿性损害。急性痤疮丘疹中的初始炎性细胞是CD4+T淋巴细胞。导管破裂不是炎症的先决条件,炎症归因于从该导管释放促炎性物质。当炎症发展时,出现嗜中性粒细胞趋化性。这些嗜中性粒细胞分泌水解酶,其引起进一步的损伤和增加的毛囊壁(follicular wall)的渗透性。在脓疱中,嗜中性粒细胞早得多地存在。更持久的损害展现可导致结疤的肉芽肿性组织学。
治疗痤疮的目的在于使损伤的数量和严重性最小化,防止结疤,限制病程,以及减小影响许多患者(特别是青少年)的社会压力和心理压力。常规治疗旨在纠正看来引起痤疮的三种主要因素:(1)皮脂腺的雄激素刺激和增加的皮脂产生;(2)异常角质化和对皮脂流动造成阻碍的毛皮脂腺管嵌塞;以及(3)痤疮丙酸杆菌(P. acnes)的增殖。因此,去除粉刺的局部用药剂(例如局部用类视黄醇)是特别有效的,因为它们使得毛囊口内的脱皮正常化,这允许皮脂自由流动到皮肤的表面上;已显示阿达帕林、维甲酸和他扎罗汀在治疗轻度到中度的痤疮中具有功效,但是所有三种药剂已被报道具有刺激皮肤的副作用,包括红斑、瘙痒、灼热/蛰刺感以及起鳞屑/脱皮。使用类视黄醇的副作用如此激烈以致许多个体根本不能忍受局部施加这些药剂。
已有一段时间使用水杨酸和过氧化苯甲酰来治疗痤疮。该两种药剂使皮肤干燥,这帮助痤疮管理,但是它们可在痤疮患者(尤其是具有敏感性皮肤的患者)的损害周围的皮肤区域中引起一些皮肤刺激,并且在一些情况下,红斑是极严重的。此外,已报道,过氧化苯甲酰似乎诱导自由基产生,其可引起在性质上类似紫外线B损伤的皮肤变化,例如增加表皮厚度,以及弹性蛋白和粘多糖含量的有害变化。参见Ibbotson等,The Effects of Radicals Compared with UVB as Initiating Species for the Induction of Chronic Cutaneous Photodamage, J. Invest. Dermatol., 1999年6月; 112(6): 933 938。有时给患有炎性丘疹和脓疱的患者开局部用和口服抗生素(尤其是四环素、红霉素和克林霉素),但是除了一般而言的过度使用抗生素的不合意性(其可导致增强对感染的易感性)以外,此类治疗的缺点还包括光毒性和与其它药物的相互作用。
在痤疮治疗期间经常使包括基于油的化妆品和一些药物(例如雄激素、高孕激素避孕药丸、全身用皮质类固醇、以及含碘化物和溴化物的药剂)在内的对加剧痤疮起作用的其它因素最小化。
公开概述
本公开涉及化妆品组合物以及使用该化妆品组合物来改善皮肤外观的方法。例如,该化妆品组合物可用于治疗痤疮、治疗炎症、向皮肤提供抗衰老益处等。该化妆品组合物包含:(a) 化妆品可接受的载体;以及(b)皮肤活性成分的组合,其包含:硫磺(sulfur);烟酰胺;和苯乙基间苯二酚。该化妆品组合物可包括额外的活性成分,如,例如乙醇酸和/或尿囊素。
该化妆品组合物可包括一种或更多种非离子表面活性剂。非离子表面活性剂的非限制性实例包括多元醇酯、甘油醚、氧乙烯化醚、氧丙烯化醚和乙二醇聚合物。可采用非离子表面活性剂的组合,例如硬脂酸甘油酯、PEG-100硬脂酸酯与鲸蜡硬脂醇聚醚-20的组合。
一种或更多种非离子表面活性剂可包含一种或更多种脂肪醇。例如,一种或更多种脂肪醇可选自己醇、辛醇、2-乙基己醇、癸醇、月桂醇、异十三烷醇、肉豆蔻醇、鲸蜡醇、己基癸醇、棕榈油醇(palmitoleyl alcohol)、硬脂醇、鲸蜡硬脂醇、异硬脂醇、油醇、反油醇(elaidyl alcohol)、岩芹醇(petroselinyl alcohol)、亚油醇(linolyl alcohol)、亚麻醇、桐醇(elaeostearyl alcohol)、花生醇、鳕油醇(gadoleyl alcohol)、山萮醇、辛基十二烷醇、瓢儿菜醇、巴惟醇(brassidyl alcohol)、椰子油、山萮醇、及其混合物。
化妆品组合物中可包括维生素和/或其衍生物,尤其是有助于皮肤的健康和活力的维生素和/或衍生物。例如,维生素可包括抗坏血酸、维生素A、维生素E和/或维生素B5。
本公开进一步涉及治疗痤疮的方法、向皮肤提供抗炎和/或抗菌益处的方法、以及改善皮肤外观的方法。所述方法包括将本文中描述的化妆品组合物施加于皮肤。通常所述方法涉及治疗需要治疗的个体,例如遭受痤疮的个体以及易于爆发痤疮的个体、遭受痤疮结疤的个体和/或遭受炎症后色素沉着过度的个体。
公开详述
本公开涉及化妆品组合物以及使用该化妆品组合物改善皮肤外观的方法。该组合物包含:
(a)化妆品可接受的载体;和
(b)皮肤活性成分的组合,其包含:
i. 硫磺;
ii. 烟酰胺;和
iii. 苯乙基间苯二酚。
该化妆品组合物可包括额外的活性成分,如,例如乙醇酸和/或尿囊素。
基于化妆品组合物的总量计,一种或更多种皮肤活性成分的总量可为约1重量%至约50重量%。一种或更多种皮肤活性成分的总量可为约1重量%至约20重量%、约25重量%、30重量%、35重量%或40重量%。一种或更多种皮肤活性成分的总量可为约5重量%至约20重量%、约25重量%、30重量%、35重量%或40重量%。一种或更多种皮肤活性成分的总量可为约6重量%、约8重量%、约10重量%、约12重量%、约14重量%或约15重量%至约40重量%。在一些情况下,一种或更多种皮肤活性成分的总量可为约10重量%至约30重量%、约12重量%至约28重量%或约14重量%至约26重量%。
基于化妆品组合物的总重量计,硫磺的总量可为约1重量%至约35重量%。类似地,硫磺的总量可为约2重量%至约20重量%。在一些情况下,组合物中硫磺的总量高于所组合的所有其它皮肤活性成分的总量。硫磺的总量可为约1重量%、约2重量%、约3重量%、约4重量%、约5重量%、约6重量%、约7重量%或约8重量%至约18重量%。硫磺的总量可为约3重量%至约12重量%、约14重量%、约16重量%、约18重量%、或约20重量%。虽然组合物包括硫磺,但是组合物是独特的,因为它们不展现含硫产品之中普遍的令人不快的气味。不希望受到任何特别理论的束缚,申请人相信,诸如玉米淀粉之类的淀粉的使用造成缺乏令人不快的气味。
基于化妆品组合物的总重量计,烟酰胺的总量可为约1重量%至约25重量%。烟酰胺的总量可为约1重量%至约10重量%。烟酰胺的总量可为约1重量%至约5重量%、约6重量%、约7重量%、约8重量%或约9重量%。类似地,烟酰胺的总量可为约2重量%、或约3重量%,至约8重量%。
基于化妆品组合物的总重量计,苯乙基间苯二酚的总量可为约0.05重量%至约20重量%。类似地,苯乙基间苯二酚的总量可为约0.05重量%至约5重量%、约10重量%或约15重量%。苯乙基间苯二酚的总量可为约0.05重量%至约2重量%、约3重量%或约4重量%。类似地,苯乙基间苯二酚的总量可为约0.1重量%至约1重量%、约2重量%、约3重量%、约4重量%或约5重量%。
基于化妆品组合物的总重量计,乙醇酸(存在时)的总量可为约1重量%至约10重量%。乙醇酸的总量可为约1重量%至约5重量%、约6重量%、约7重量%、约8重量% 或约9重量%。类似地,乙醇酸的总量可为约2重量%、或约3重量%,至约8重量%。
基于化妆品组合物的总重量计,尿囊素(存在时)的总量可为约0.01重量%至约5重量%。尿囊素的总量可为约0.01重量%至约1重量%、约2重量%、约3重量%、或约4重量%。类似地,尿囊素的总量可为约0.05重量%至约1重量%、约2重量%、约3重量%、约4重量%或约5重量%。
如以上所提及的,在化妆品可接受的载体中提供皮肤活性成分。化妆品可接受的载体通常包括水;并可额外地包括一种或更多种化妆品可接受的有机溶剂。化妆品可接受的有机溶剂的非限制性实例包括乙二醇、丙二醇(propylene glycol)、丁二醇、己二醇、丙二醇(propane diol)和甘油。
在一些情况下,化妆品组合物包括一种或更多种非离子表面活性剂。非离子表面活性剂的非限制性实例包括多元醇酯、甘油醚、氧乙烯化醚、氧丙烯化醚和乙二醇聚合物。可采用非离子表面活性剂的组合,例如多元醇酯与乙二醇聚合物的组合;更具体地,硬脂酸甘油酯、PEG-100硬脂酸酯与鲸蜡硬脂醇聚醚-20的组合。
一种或更多种非离子表面活性剂可包括一种或更多种脂肪醇。例如,一种或更多种脂肪醇可选自己醇、辛醇、2-乙基己醇、癸醇、月桂醇、异十三烷醇、肉豆蔻醇、鲸蜡醇、己基癸醇、棕榈油醇、硬脂醇、鲸蜡硬脂醇、异硬脂醇、油醇、反油醇、岩芹醇、亚油醇、亚麻醇、桐醇、花生醇、鳕油醇、山萮醇、辛基十二烷醇、瓢儿菜醇、巴惟醇、椰子油、山萮醇、及其混合物。
通常,基于化妆品组合物的总重量计,一种或更多种非离子表面活性剂的总量通常为约0.1重量%至约15重量%。
权利要求3的化妆品组合物,其中基于化妆品组合物的总重量计,(c)的一种或更多种非离子表面活性剂的总量为约0.1重量%至约15重量%。一种或更多种非离子表面活性剂的总量可为约1重量%至约6重量%、约8重量%、约10重量%、约12重量%或约14重量%。类似地,一种或更多种非离子表面活性剂的总量可为约2重量%至约6重量%、约8重量%、约10重量%、约12重量%或约14重量%。
在化妆品组合物中可包括一种或更多种维生素和/或其衍生物,尤其是有助于皮肤的健康和活力的维生素和/或衍生物。例如,维生素可包括抗坏血酸、维生素A、维生素E和/或维生素B5。基于化妆品组合物的总重量计,一种或更多种维生素和/或其衍生物的总量通常为约0.01重量%至约5重量%。在一些情况下,一种或更多种维生素和/或其衍生物的总量为约0.1重量%至约1重量%、2重量%、3重量%、4重量%或5重量%。
本公开进一步涉及治疗痤疮的方法、向皮肤提供抗炎和/或抗菌益处的方法、以及改善皮肤外观的方法。所述方法包括向皮肤施加本文中所描述的化妆品组合物。通常所述方法涉及治疗需要治疗的个体,例如遭受痤疮或易于爆发痤疮的个体。可每天将组合物施加于皮肤,尤其施加于面部、颈部、背部和或肩部。可将组合物一天施加一次或更频繁,例如每天两次或三次。在一些情况下,在早上施加组合物。在一些情况下,在晚上施加组合物。此外,在一些情况下,可既在早上施加组合物,又在晚上再次施加组合物。可每天施加组合物持续数天、数周或甚至数月。在一些情况下,治疗可以是短暂的以便致力于特别的爆发,例如持续一天至一周(7天)。治疗可以是至少一周并延续两周、三周或四周或更长。
下文呈现本文所公开的组合物中有用的组分的更详尽但非限制性的清单。
化妆品可接受的载体(或溶剂)
本公开的组合物可存在于化妆品可接受的溶剂中。该化妆品可接受的溶剂可包括例如水或水与至少一种化妆品可接受的有机溶剂的混合物。
作为有机溶剂的实例,可非限制性地提及一元醇和多元醇,例如乙醇、异丙醇、丙醇、苄醇和苯乙醇;或者二醇或二醇醚,如,例如乙二醇单甲醚、乙二醇单乙醚和乙二醇单丁醚;丙二醇或其醚,如,例如丙二醇单甲醚;丁二醇;己二醇;一缩二丙二醇以及二甘醇的烷基醚,例如二甘醇单乙醚或二甘醇单丁醚。
有机溶剂的其它合适的实例为乙二醇、丙二醇、丁二醇、己二醇、丙二醇和甘油。
本公开中使用的有机溶剂可为挥发性或非挥发性化合物。
基于组合物的总重量计,根据本公开可采用以下范围内的量的化妆品可接受的溶剂:约5重量%至约95重量%,或例如约20重量%至约90重量%,例如约30至约80重量%,或例如约35重量%至约75重量%,例如约5至约50重量%,例如约50至95重量%。
基于本公开的组合物的总重量计,根据本公开可采用以下范围内的量的有机溶剂:约0.1重量%至约25重量%,例如约1重量%至约15重量%,或例如约3重量%至约10重量%,或例如约5重量%至约10重量%。
皮肤活性成分
除了已经描述的皮肤活性成分之外,本公开的组合物可含有额外的皮肤活性成分,例如保湿剂和保湿成分、抗衰老剂、脱色剂、抗皱纹剂、或处理油性皮肤的药剂。一种或更多种活性剂的非限制性实例包括腺苷、2-[4-(2-羟乙基)哌嗪-1-基]乙磺酸(HEPES)、透明质酸、羊毛脂、柠檬酸、苹果酸、乳酸、酒石酸、水杨酸、维生素C、维生素、类视黄醇、视黄醛、视黄酸、类胡萝卜素、氨基酸、蛋白质、酶和辅酶。在一些情况下,活性成分是腺苷。
保湿剂和保湿成分可特别为甘油及其衍生物;脲及其衍生物,尤其是由NationalStarch销售的Hydrovance;乳酸;透明质酸;AHA;BHA;吡酮酸钠;木糖醇;丝氨酸;乳酸钠;依克多因及其衍生物;壳聚糖及其衍生物;胶原;浮游生物;由Sederma以名称Moist 24销售的白茅(Imperata cylindra)提取物;作为NOF Corporation的Lipidure-HM的丙烯酸均聚物;β-葡聚糖,且特别是羧甲基β-葡聚糖钠(Mibelle-AG-Biochemistry);由Nestle以名称NutraLipids销售的西番莲油、杏油、玉米油和米糠油的混合物;C-糖苷衍生物,特别是C-13-D-吡喃木糖苷-2-羟基丙烷,其为活性材料在水/丙二醇混合物(60/40重量%)中的30重量%溶液形式,作为由Chimex公司以商品名"Mexoryl SBB"生产的产品;由Nestle销售的玫瑰果油;由Vincience以名称Algualane Zinc销售的富含锌的微藻提取物紫球藻(Prophyridium cruentum);由Engelhard Lyon公司以名称Marine Filling Spheres销售的海洋来源的胶原和硫酸软骨素球体(缺端胶原(Atelocollagen));透明质酸球体,例如由Engelhard Lyon销售的那些;以及精氨酸。
脱色剂包括维生素C及其衍生物,且尤其是维生素CG、CP和3-O乙基维生素C、α和β熊果苷、阿魏酸、lucinol及其衍生物、曲酸、间苯二酚及其衍生物、氨甲环酸及其衍生物、龙胆酸、高龙胆酸(homogentisic)、龙胆酸甲酯或高龙胆酸甲酯、二酸(dioic acid)、D泛酰巯基乙胺磺酸钙(D pantheteine calcium sulphonate)、硫辛酸、鞣花酸、维生素B3、亚油酸及其衍生物、神经酰胺及其配对物,其衍生自植物例如甘菊、熊果、芦荟科(芦荟、好望角芦荟、库拉索芦荟)、桑葚、美黄岑;由Gattefosse销售的奇异果(kiwi fruit)(中华猕猴桃(Actinidia chinensis))水;牡丹(Paeonia suffruticosa)根的提取物,例如由IchimaruPharcos以名称Liquid Botanpi Be销售的那种;红糖(甘蔗(Saccharum officinarum))的提取物,例如由Taiyo Kagaku以名称Liquid Molasses销售的糖蜜提取物,该清单并非穷举的。特别的脱色剂包括维生素C及其衍生物,且尤其是维生素CG、CP及3-O乙基维生素C、α和β熊果苷、阿魏酸、曲酸、间苯二酚及衍生物、D泛酰巯基乙胺磺酸钙、硫辛酸、鞣花酸、维生素B3、由Gattefosse销售的奇异果(中华猕猴桃)水、牡丹根的提取物,例如由IchimaruPharcos公司以名称Botanpi Liquid B销售的那种。
术语“抗皱纹活性剂”指当与起皱纹的皮肤区域接触时产生生物效应,例如某些酶的合成和/或活性增加的天然或合成化合物,这具有减少皱纹和/或细纹出现的效果。示例性的抗皱纹活性剂可选自:脱皮剂、抗糖化剂、NO合酶抑制剂、刺激真皮或表皮大分子的合成和/或防止其降解的药剂、用于刺激成纤维细胞和/或角化细胞增殖的药剂或用于刺激角化细胞分化还原剂(reducing agent)的药剂;肌肉松弛剂和/或皮肤去皱剂(dermo-decontracting agent)、抗自由基剂、及其混合物。
此类化合物的实例为:腺苷及其衍生物和视黄醇及其衍生物,例如视黄醇棕榈酸酯;抗坏血酸及其衍生物,例如抗坏血酸磷酸酯镁和抗坏血酸葡糖苷;生育酚及其衍生物,例如生育酚乙酸酯;烟酸及其前体,例如烟酰胺;泛醌;谷胱甘肽及其前体,例如L-2-氧代噻唑烷-4-羧酸;如特别在EP-1345919中描述的化合物C-糖苷及其衍生物,特别是如特别在EP-1345919中描述的C-β-D-吡喃木糖苷-2-羟基丙烷;植物提取物,包括海茴香和橄榄叶的提取物,以及植物及其水解产物,例如大米蛋白水解产物或大豆蛋白;藻类提取物,且特别是昆布属植物、细菌提取物;皂苷配基,例如薯蓣皂苷配基和薯蓣属植物(特别是野生山药)的提取物,其包含:a-羟基酸、f3-羟基酸,例如水杨酸和正辛酰基-5-水杨酸寡肽和假二肽、及其酰基衍生物,特别是酸{2-[乙酰基-(3-三氟甲基-苯基)-氨基]-3-甲基-}乙酸和脂肽(由公司SEDERMA以商品名Matrixyl 500和Matrixyl 3000销售);番茄红素;锰盐和镁盐(尤其是葡糖酸盐)、及其混合物。
作为腺苷衍生物,尤其包括腺苷的非磷酸盐衍生物,例如特别是2'-脱氧腺苷、2',3'-异丙叉腺苷;丰加霉素、1-甲基腺苷、N-6-甲基腺苷;腺苷N-氧化物、6-甲基巯基嘌呤核苷和6-氯嘌呤核苷。
其它衍生物包括腺苷受体激动剂,例如腺苷苯基异丙基腺苷("PIA")、1-甲基异鸟苷、N6-环己基腺苷(CHA)、N6-环戊基腺苷(CPA)、2-氯-N6-环戊基腺苷、2-氯腺苷、N6-苯基腺苷、2-苯基氨基腺苷、MECA、N6-苯乙基腺苷、2-对-(2-羧基-乙基)苯乙基-氨基-5'-N-乙基甲酰胺基腺苷(CGS-21680)、N-乙基甲酰胺基-腺苷(NECA)、5'(N-环丙基)-甲酰胺基腺苷、DPMA(PD 129.944)和腺苷地尔。
在一些情况下,本公开的组合物包含致力于油性皮肤的皮肤活性成分。这些活性剂可以是能够调节皮脂腺活性的皮脂调节剂或抗皮脂溢剂。这些包括:视黄酸、过氧化苯甲酰、硫磺、维生素B6(或吡哆醇)氯化物、硒、海蓬子--肉桂提取物共混物、茶叶和辛酰甘氨酸,例如来自Seppic的15 Sepicontrol A5 TEA;--肉桂、肌氨酸和辛酰甘氨酸的混合物,尤其是由Seppic以商品名Sepicontrol A5销售;--锌盐,例如葡糖酸锌、吡咯烷酮羧酸锌(或吡酮酸锌)、乳酸锌、天冬氨酸锌、羧酸锌、水杨酸锌20、磺基丙氨酸锌(zinc cysteate);--衍生物,特别是铜和吡酮酸铜,作为Cuivridone Solabia;--来自以下植物的提取物:山金车(Arnica montana)、鸡纳树(Cinchona succirubra)、丁子香(Eugenia caryophyllata)、啤酒花(Humulus lupulus)、金丝桃(Hypericum perforatum)、辣薄荷(Mentha pipenta)25、迷迭香(Rosmarinus officinalis)、药鼠尾草(Salvia officinalis)和百里香(Thymusvulgaris),全部例如由Maruzen销售;--绣线菊(榆绣线菊(Spiraea ulmaria))的提取物,例如由Silab以名称Sebonormine销售的那种;--藻类糖昆布(Laminaria saccharina)的提取物,例如由Biotechmarine以30名称Phlorogine销售的那种;--美洲地榆混合物(地榆(Sanguisorba officinalis)/长穗地榆(Poterium officinale))的根提取物、姜(生姜(Zingiber officinalis))的根茎和肉桂皮(中国肉桂(Cinnamomum cassia))(的提取物),例如由Solabia以名称Sebustop销售的那种;--亚麻籽的提取物,例如由Lucas Meyer以名称Linumine销售的那种;--黄柏(Phellodendron)提取物,例如由Maruzen以名称Phellodendron extract BG或由Ichimaru Pharcos以名称Oubaku liquid B销售的那些;--摩洛哥坚果油、锯叶棕(Serenoa serrulata)(锯棕榈(saw palmetto))提取物和芝麻籽提取物的混合物,例如由Pentapharm以名称Regu SEB销售的那种;--柳兰、诃子(Terminalia chebula)、旱金莲和生物可利用锌(微藻)的提取物的混合物,例如以名称Seborilys Green Tech销售的那种;--非洲臀果木(Pygeum afrianum)的提取物,例如由Euromed以名称 Pygeum afrianum sterolic lipid extract销售的那种;--锯叶棕的提取物,例如由Actives International以名称Viapure Sabal销售的那些,以及由Euromed公司销售的那些;--车前草的提取物、冬青叶小檗(Berberis aquifolium)的提取物和水杨酸钠20的共混物,例如以名称Seboclear Rahn销售的那种;--丁香的提取物,如由Maruzen以名称Clove extract powder销售的那种;--摩洛哥坚果油,例如以名称LipofructylLaboratories Serobiologiques销售的那种;25--乳酸蛋白滤液,例如由Sederma以名称Normaseb销售的那种;--海藻昆布属植物提取物,例如由Biotechmarine以名称Laminarghane销售的那种;--寡糖海藻掌状昆布(Laminaria digitata),例如由Codif公司以名称Phycosaccharide 30 AC销售的那种;--甘蔗的提取物,例如由Sabinsa公司以名称Policosanol销售的那种;磺化页岩油,例如由Ichthyol以名称Ichtyol Pale销售的那种;--绣线菊(榆绣线菊)的提取物,例如由societeLibiol以名称Cytobiol Ulmaire销售的那种;--癸二酸,尤其是由Sederma以名称Sebosoft以聚丙烯酸钠凝胶形式销售;--提取自魔芋块茎并用烷基磺酸酯链改性的葡甘露聚糖,例如由Arch Chemical以名称Biopol Beta销售的那种;--苦参(Sophora angustifolia)的提取物,例如由Bioland以名称Sophorapowder或Sophora extract销售的那些;--鸡纳树树皮的提取物,例如由Alban Muller以名称Red Bark HS销售的那种;--皂皮树(Quillaja saponaria)的提取物,例如由AlbanMuller以名称15 Panama wood HS销售的那种;--接枝到十一碳烯链上的甘氨酸,例如由SEPPIC以名称Lipacide UG OR销售的那种;--齐墩果酸和去甲二氢愈创木酸的混合物,例如由Sederma以名称AC.Net以凝胶形式销售的那种;20--苯二甲酰亚氨基过氧己酸;--柠檬酸三(C12-C13)酯,由Sasol以名称COSMACOL.RTM. ECI销售;柠檬酸三(C14-C15)烷基酯,由Sasol以名称COSMACOL.RTM. ECL销售;--10-羟基癸酸,包括羟基癸酸October 25、癸二酸和1,10-癸二醇的混合物,例如由Vincience以名称Acnacidol BG销售的那种;及其混合物。
防腐剂
在本文描述的组合物中可包括一种或更多种防腐剂,用于处理头发。合适的防腐剂包括但不限于,含有甘油的化合物(例如甘油和/或乙基己基甘油和/或苯氧基乙醇)、苄醇、对羟基苯甲酸酯(对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、对羟基苯甲酸丁酯、对羟基苯甲酸异丁酯等)、苯甲酸钠、乙二胺四乙酸(EDTA)、山梨酸钾和/或葡萄柚籽提取物、或其组合。组合物中可包括超过一种防腐剂。其它防腐剂在化妆品工业中是已知的,并包括水杨酸、DMDM乙内酰脲、甲醛、氯苯甘醚(Chlorphenism)、三氯生、咪唑烷基脲、二偶氮利定脲、山梨酸、甲基异噻唑啉酮、脱氢乙酸钠、脱氢乙酸、季铵盐-15、司拉氯铵、吡硫鎓锌、焦亚硫酸钠、2-溴-2-硝基丙烷、氯己定二葡糖酸盐、聚氨丙基双胍、苯扎氯铵、亚硫酸钠、水杨酸钠、柠檬酸、印楝油、精油(各种)、乳酸和维生素E(生育酚)。
任选以基于组合物的总重量计约0.01重量%至约5重量%、约0.05%至约4重量%或约0.06重量%至约3重量%范围内的量包括防腐剂。
增稠剂
本文中所描述的化妆品组合物可包括一种或更多种增稠剂。增稠剂的量可以为0.1重量%至20重量%、0.1至10重量%、0.1重量%至9重量%、0.2重量%至9重量%、0.3重量%至9重量%、0.4重量%至8重量%、0.5重量%至5重量%、1重量%至5重量%、或2重量%至4重量%。另外,增稠剂的量可以为0.1、0.2、0.3、0.4、0.5、0.6、0.7、0.8、0.9、1.0或1.5重量%至2、3、4、5、6、7、8、9、10、15或20重量%。
一种或更多种增稠剂可以是黄原胶、瓜尔胶、生物糖胶、纤维素、阿拉伯胶树胶(acacia Seneca gum)、小核菌胶、琼脂糖、果胶、结冷胶、透明质酸。另外,一种或更多种增稠剂可包括聚合物增稠剂,其选自聚丙烯酰基二甲基牛磺酸铵、丙烯酰基二甲基牛磺酸铵/VP共聚物、聚丙烯酸钠、丙烯酸酯共聚物、聚丙烯酰胺、卡波姆和丙烯酸酯/丙烯酸C10-30烷基酯交联聚合物。在一些情况下,组合物包括聚丙烯酰基二甲基牛磺酸铵和/或聚丙烯酸钠。
许多增稠剂是水溶性的,并且当本发明的化妆品组合物分散/溶解于水中时增加水的粘度或形成含水凝胶。必要时,可对水溶液进行加热和冷却或中和,用于形成凝胶。增稠剂可分散/溶解于可溶于水中的含水溶剂中,例如乙醇中,当其分散/溶解于水中时。各种类型的增稠剂的非限制性实例包括:
a. 羧酸聚合物
这些聚合物是交联的化合物,其含有一种或更多种衍生自丙烯酸、取代的丙烯酸、以及这些丙烯酸和取代的丙烯酸的盐和酯的单体,其中交联剂含有两个或更多个碳-碳双键,并且衍生自多元醇。
本文中有用的市售可得的羧酸聚合物的实例包括卡波姆,其为与蔗糖或季戊四醇的烯丙基醚交联的丙烯酸的均聚物。卡波姆可作为来自B.F. Goodrich的Carbopol.RTM.900系列(例如Carbopol® 954)获得。另外,其它合适的羧酸聚合物试剂包括Ultrez® 10(B.F. Goodrich)以及丙烯酸C10-30烷基酯与一种或更多种丙烯酸、甲基丙烯酸、或它们的短链(即,C1-4醇)酯之一的单体的共聚物,其中交联剂是蔗糖或季戊四醇的烯丙基醚。这些共聚物被称为丙烯酸酯/丙烯酸C10-C30烷基酯交联聚合物,并且作为来自B.F. Goodrich的Carbopol.RTM. 1342、Carbopol® 1382、Pemulen TR-1和Pemulen TR-2市售可得。换句话说,本文中有用的羧酸聚合物增稠剂的实例是选自卡波姆、丙烯酸酯/丙烯酸C10-C30烷基酯交联聚合物、及其混合物的那些。
b. 交联的聚丙烯酸酯聚合物
本公开的组合物可任选含有可用作增稠剂或胶凝剂的交联的聚丙烯酸酯聚合物,其包括阳离子聚合物和非离子聚合物两者。有用的交联的非离子聚丙烯酸酯聚合物和交联的阳离子聚丙烯酸酯聚合物的实例是美国专利第5,100,660号、美国专利第4,849,484号、美国专利第4,835,206号、美国专利第4,628,078号、美国专利第4,599,379号和EP 228,868中描述的那些,其全部通过引用以其整体并入本文。
c. 聚丙烯酰胺聚合物
本公开的组合物可任选含有聚丙烯酰胺聚合物,尤其是非离子聚丙烯酰胺聚合物,包括取代的支化或非支化聚合物。在这些聚丙烯酰胺聚合物中有CTFA命名规定为聚丙烯酰胺和异链烷烃和月桂醇聚醚-7的非离子聚合物,其可从Seppic Corporation以商品名Sepigel 305获得。
本文中有用的其它聚丙烯酰胺聚合物包括丙烯酰胺和取代的丙烯酰胺与丙烯酸和取代的丙烯酸的多嵌段共聚物。这些多嵌段共聚物的市售可得的实例包括来自LipoChemicals, Inc.的Hypan SR150H、SS500V、SS500W、SSSA100H。
组合物还可含有增稠和调质凝胶,其类型如由来自United Guardian的称为Lubrajel®的产品范围所例示。这些凝胶具有保湿、增粘、稳定化的性质。
d. 多糖
多种多样的多糖可有用于本文。“多糖”指含有重复的糖(即,碳水化合物)单元的骨架的胶凝剂。多糖胶凝剂的非限制性实例包括选自以下的那些:纤维素、羧甲基羟乙基纤维素、乙酸丙酸羧酸纤维素(cellulose acetate propionate carboxylate)、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。也有用于本文的是烷基取代的纤维素。烷基羟烷基纤维素醚之中优选的是CTFA命名规定为鲸蜡基羟乙基纤维素的材料,其为鲸蜡醇与羟乙基纤维素的醚。该材料由Aqualon Corporation以商品名Natrosol® CS Plus销售。
其它有用的多糖包括硬葡聚糖,其包含(1-3)连接的葡萄糖单元的直链,每三个单元具有(1-6)连接的葡萄糖,其市售可得的实例为来自Michel Mercier Products Inc.的ClearogelTM. CS11。
e. 树胶
本文中有用的其它增稠和胶凝剂包括主要源自天然来源的材料。这些胶凝剂胶的非限制性实例包括金合欢胶(acacia)、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、瓜尔胶、瓜尔胶羟丙基三甲基氯化铵、水辉石、透明质酸、水合二氧化硅、羟丙基壳聚糖、羟丙基瓜尔胶、刺梧桐树胶、海带、刺槐豆胶、纳豆胶、藻酸钾、角叉菜胶钾、藻酸丙二醇酯、小核菌胶、羧甲基糊精钠、角叉菜胶钠、黄蓍胶、黄原胶、及其混合物。
水溶性增稠剂的额外的实例包括水溶性天然聚合物、水溶性合成聚合物、粘土矿物和硅酸酐。水溶性天然聚合物的非限制性实例包括阿拉伯树胶、黄蓍胶、刺梧桐树胶、瓜尔胶、结冷胶、他拉胶、刺槐豆胶、罗望子胶、藻酸钠、藻酸丙二醇酯、角叉菜胶、farcelluran、琼脂、高甲氧基果胶、低甲氧基果胶、黄嘌呤、壳聚糖、淀粉(例如得自玉米、马铃薯、小麦、大米、甘薯和木薯的淀粉、a-淀粉、可溶性淀粉)、发酵多糖(例如黄原胶、普鲁兰多糖、carciran、葡聚糖)、得自属于Polyantes种属的植物的愈合组织的酸性杂多糖(例如块茎多糖)、蛋白质(例如酪蛋白钠、明胶、白蛋白)、硫酸软骨素和透明质酸。
水溶性合成聚合物的非限制性实例包括聚乙烯醇、聚丙烯酸钠、聚甲基丙烯酸钠、聚丙烯酸甘油酯、羧乙烯基聚合物、聚丙烯酰胺、聚乙烯基吡咯烷酮、聚乙烯基甲基醚、聚乙烯基砜、马来酸共聚物、聚氧化乙烯、聚二烯丙基胺、聚乙烯亚胺、水溶性纤维素衍生物(例如羧甲基纤维素、甲基纤维素、甲基羟丙基纤维素、羟乙基纤维素、羟丙基纤维素、纤维素硫酸钠盐)、以及淀粉衍生物(例如氧化淀粉、双醛淀粉、糊精、糊精(British gum)、乙酰淀粉、淀粉磷酸酯、羧甲基淀粉、羟乙基淀粉、羟丙基淀粉)。
表面活性剂
本文中所描述的各种组合物可包括一种或更多种表面活性剂,包括阳离子表面活性剂、阴离子表面活性剂、非离子表面活性剂和/或两性/两性离子表面活性剂。下文提供可使用的表面活性剂的非限制性实例。
阳离子表面活性剂
术语“阳离子表面活性剂”表示当其包含于根据本公开的组合物中时带正电荷的表面活性剂。该表面活性剂可携带一个或更多个永久正电荷或可含有一个或更多个可在根据本公开的组合物中阳离子化的官能。
阳离子表面活性剂的非限制性实例包括山萮基苄基二甲基氯化铵、苄索氯铵、鲸蜡基氯化吡啶鎓、山萮基三甲基氯化铵、月桂基苄基二甲基氯化铵、鲸蜡基苄基二甲基氯化铵、鲸蜡基三甲基溴化铵、鲸蜡基三甲基氯化铵、鲸蜡基胺氢氟酸盐、氯化氯烯丙基六亚甲基四胺(季铵盐-15)、二硬脂基二甲基氯化铵(季铵盐-5)、十二烷基二甲基乙基苄基氯化铵(季铵盐-14)、季铵盐-22、季铵盐-26、季铵盐-18水辉石、二甲氨基氯乙烷盐酸盐、半胱氨酸盐酸盐、二乙醇铵POE(10)油基醚磷酸酯(diethanolammonium POE (10) oletyl etherphosphate)、二乙醇铵POE(3)油基醚磷酸酯、牛脂基苄基二甲基氯化铵、二甲基双十八烷基铵膨润土(dimethyl dioctadecylammoniumbentonite)、司拉氯铵、度米芬、苯甲地那铵、肉豆蔻基苄基二甲基氯化铵、月桂基三甲基氯化铵、乙二胺二盐酸盐、盐酸胍、盐酸吡哆醇、盐酸碘非他胺、葡甲胺盐酸盐、甲苄索氯铵、肉豆蔻基三甲基溴化铵、油基三甲基氯化铵、聚季铵盐-1、盐酸普鲁卡因、椰油基甜菜碱、司拉氯铵膨润土、司拉氯铵水辉石、硬脂基三羟乙基丙二胺二氢氟酸盐、牛脂基三甲基氯化铵和十六烷基三甲基溴化铵。
阳离子表面活性剂可任选选自聚氧烯化的伯、仲或叔脂肪胺、或其盐和季铵盐、及其混合物。
脂肪胺通常包含至少一个基于C8-C30烃的链。
可尤其提及的季铵盐的实例包括对应于以下通式(III)的那些:
(III)
其中,基团R8至R11可以相同或不同,代表包含1至30个碳原子的直链或支链的、饱和或不饱和的脂族基团;或芳族基团,例如芳基或烷基芳基,基团R8至R11至少之一表示包含8至30个碳原子并优选12至24个碳原子的基团。脂族基团可包含杂原子,尤其例如氧、氮、硫和卤素。脂族基团选自例如C1-C30烷基、C2-C30烯基、C1-C30烷氧基、聚氧化(C2-C6)烯、C1-C30烷基酰胺、(C12-C22)烷基酰胺基(C2-C6)烷基、(C12-C22)烷基乙酸酯和C1-C30羟烷基基团;X-是选自以下的阴离子:卤离子、磷酸根、乙酸根、乳酸根、(C1-C4)烷基硫酸根、以及(C1-C4)烷基磺酸根或(C1-C4)烷基芳基磺酸根。
在式(III)的季铵盐之中,优选的那些一方面是四烷基铵盐,例如二烷基二甲基铵或烷基三甲基铵盐,其中所述烷基含有大约12至22个碳原子,特别是山萮基三甲基铵、二硬脂基二甲基铵、鲸蜡基三甲基铵或苄基二甲基硬脂基铵盐,或另一方面是油鲸蜡基二甲基羟乙基铵盐、棕榈基酰胺基丙基三甲基铵盐、硬脂酰胺丙基三甲基铵盐和硬脂酰胺丙基二甲基鲸蜡硬脂基铵盐。
在一些情况下,有用的是,使用诸如下列化合物的氯盐(chloride salt)之类的盐:
A. 咪唑啉的季铵盐,如,例如下式(IV)的那些:
(IV)
其中R12代表例如衍生自牛油脂肪酸的包含8至30个碳原子的烯基或烷基;R13代表氢原子、C1-C4烷基或包含8至30个碳原子的烷基或烯基;R14代表C1-C4 烷基;R15代表氢原子或C1-C4烷基;X-是阴离子,其选自卤离子、磷酸根、乙酸根、乳酸根、烷基硫酸根、烷基磺酸根或烷基芳基磺酸根,其中所述烷基和芳基分别优选包含1至20个碳原子和6至30个碳原子。R12和R13优选表示例如衍生自牛油脂肪酸的含有12至21个碳原子的烯基或烷基的混合物,R14优选表示甲基,且R15优选表示氢原子。此类产品例如由Rewo公司以名称Rewoquat(R) W 75销售;
B. 季二铵或三铵盐,特别具有式(V):
(V)
其中R16表示包含大约16至30个碳原子的烷基,其任选被羟基化和/或被一个或更多个氧原子中断,R17选自氢或包含1至 4个碳原子的烷基或基团(R16a)(R17a)(R18a)N-(CH2)3,
R16a、R17a、R18a、R18、R19、R20和R21可以相同或不同,选自氢和包含1至 4个碳原子的烷基,且X-是阴离子,其选自卤离子、乙酸根、磷酸根、硝酸根和甲基硫酸根。此类化合物是例如由公司Finetex销售的Finquat CT-P(季铵盐89)和由Finetex公司销售的Finquat CT(季铵盐75),
C. 含有至少一个酯官能的季铵盐,例如下式(VI)的那些:
(VI)
其中:
R22选自C1-C6烷基、以及C1-C6羟烷基或二羟烷基;
R23选自:
、R27,其是基于直链或支链的、饱和或不饱和的C1-C22烃的基团、和氢原子,
R25选自:
、R29,其是基于直链或支链的、饱和或不饱和的C1-C6烃的基团、和氢原子,
R24、R26和R28可以相同或不同,选自基于直链或支链的、饱和或不饱和的C7-C21烃的基团;
r、s和t可以相同或不同,为2至6范围内的整数;
y为1至10范围内的整数;
x和z可以相同或不同,为0至10范围内的整数;
X-是简单的或复合的有机阴离子或无机阴离子;
限制条件为,x+y+z总和是1至15,当x是0时,则Rn表示R27,以及当z是0时,则R25表示R29。
烷基R22可以是直链或支链的,且更特别是直链的。在一些情况下,R22表示甲基、乙基、羟乙基或二羟丙基,且更特别是甲基或乙基。有利地,x+y+z总和是1至10。
当R23是基于烃的基团R27时,其可以是长的,并且含有12至22个碳原子,或可以是短的,并且含有1至3个碳原子。当R25是基于烃的基团R29时,其优选含有1至3个碳原子。有利地,R24、R26和R28可以相同或不同,选自基于直链或支链的、饱和或不饱和的C11-C21烃的基团,且更特别选自直链或支链的、饱和或不饱和的C11-C21烷基和烯基。
在一些情况下,x和z可以相同或不同,具有0或1的值。类似地,在一些情况下,y等于1。在一些情况下,r、s和t可以相同或不同,等于2或3,并且甚至更特别等于2。
阴离子X-可以是卤离子(氯离子、溴离子或碘离子)或烷基硫酸根,更特别为甲基硫酸根。然而,可使用甲磺酸根、磷酸根、硝酸根、甲苯磺酸根、衍生自有机酸的阴离子(例如乙酸根或乳酸根),或与含有酯官能的铵相容的任何其它阴离子。
阴离子X-甚至更特别为氯离子或甲基硫酸根。
根据本发明的组合物中更特别使用式(VI)的铵盐,其中:
R22表示甲基或乙基,
x和y等于1;
z等于0或1;
r、s和t等于2;
R23选自:
、甲基、乙基或基于C14-C22烃的基团、和氢原子;
R25选自:
和氢原子;
R24、R26和R28可以相同或不同,选自基于直链或支链的、饱和或不饱和的C13-C17烃的基团,且优选选自直链或支链的、饱和或不饱和的C13-C17烷基和烯基。基于烃的基团有利地为直链的。
可提及例如式(VI)的化合物,例如二酰氧基乙基二甲基铵、二酰氧基乙基羟乙基甲基铵、单酰氧基乙基二羟乙基甲基铵、三酰氧基乙基甲基铵和单酰氧基乙基羟乙基二甲基铵盐(特别是氯化物或甲基硫酸盐)、及其混合物。所述酰基优选含有14至18个碳原子并且更特别从诸如棕榈油或向日葵油之类的植物油获得。当化合物含有数个酰基时,这些基团可以相同或不同。
例如通过任选氧烯化的三乙醇胺、三异丙醇胺、烷基二乙醇胺或烷基二异丙醇胺与植物或动物来源的C10-C30脂肪酸或C10-C30脂肪酸的混合物的直接酯化,或通过其甲基酯的酯交换来获得这些产品。该酯化之后为使用例如以下的烷化剂的季铵化:烷基(优选甲基或乙基)卤化物;硫酸二烷基(优选甲基或乙基)酯;甲磺酸甲酯;对甲苯磺酸甲酯;氯乙二醇(glycol chlorohydrin)或氯甘油(glycerol chlorohydrin)。此类化合物例如由Henkel公司以名称Dehyquart(R)销售、由Stepan公司以名称Stepanquat(R)销售、由Ceca公司以名称Noxamium(R)销售或由Rewo-Witco公司以名称Rewoquat(R) WE 18销售。
根据本发明的组合物可含有例如季铵单酯、二酯和三酯盐的混合物,其中重量多数为二酯盐。
可使用由Kao以名称Quatarmin BTC 131提供的山萮酰基羟丙基三甲基氯化铵。
非离子表面活性剂
可使用的非离子表面活性剂的实例描述于例如由Blackie &Son(格拉斯哥和伦敦)于1991年出版的M.R. Porter的Handbook of Surfactants,第116-178页中,通过引用将该文献以其整体并入本文。非离子表面活性剂可以是醇、α-二醇和(C1-C24)烷基酚,这些化合物是聚乙氧基化、聚丙氧基化和/或聚甘油化的,并且含有包含例如8至18个碳原子的至少一个脂肪链,氧化乙烯和/或氧化丙烯基团的数量可能尤其在2至50范围内,并且甘油基团的数量可能尤其在2至30范围内。
还可提及氧化乙烯和氧化丙烯的共聚物,任选氧乙烯化的脱水山梨糖醇脂肪酸酯、蔗糖脂肪酸酯、聚氧烯化的脂肪酸酯、聚氧烯化的脂肪酰胺、任选氧烯化的烷基(多)糖苷、烷基糖苷酯、N-烷基葡糖胺和N-酰基甲基葡糖胺的衍生物、醛糖二糖酰胺(aldobionamide)、胺氧化物和(聚)氧烯化硅酮。
非离子表面活性剂更特别选自单氧烯化或聚氧烯化的及单甘油化或聚甘油化的非离子表面活性剂、和烷基(多)糖苷。氧化烯单元更特别为氧乙烯或氧丙烯单元、或其组合,优选氧乙烯单元。
有用的非离子表面活性剂可包括:氧烯化的(C8-C24)烷基酚;饱和或不饱和的、直链或支链的氧烯化的C8-C40醇;饱和或不饱和的、直链或支链的氧烯化的C8-C30酰胺;饱和或不饱和的、直链或支链的C8-C30酸与聚乙二醇的酯;饱和或不饱和的、氧乙烯化的植物油;单独的或作为混合物的氧化乙烯和/或氧化丙烯的缩合物;氧乙烯化和/或氧丙烯化的硅酮;以及烷基(多)糖苷。
作为单甘油化的或聚甘油化的非离子表面活性剂的实例,可使用单甘油化的或聚甘油化的C8-C40醇。特别地,单甘油化的或聚甘油化的C C8-C40醇对应于下式(VIII):
(VIII)
所述式(VIII)中:
R29代表直链或支链的C8-C40,且优选C8-C30烷基或烯基;以及
m代表1至30或1 至10范围内的数字。
作为式(VIII)的化合物的实例,可提及含有4摩尔甘油的月桂醇(INCI名称:聚甘油-4月桂基醚)、含有1.5摩尔甘油的月桂醇、含有4摩尔甘油的油醇(INCI名称:聚甘油-4油基醚)、含有2摩尔甘油的油醇(INCI名称:聚甘油-2油基醚)、含有2摩尔甘油的鲸蜡硬脂醇、含有6摩尔甘油的鲸蜡硬脂醇、含有6摩尔甘油的油鲸蜡醇和含有6摩尔甘油的十八烷醇。
式(VIII)的醇可以相同方式代表醇的混合物(其中m的值代表统计值),这在商业产品中意味着,若干种类的聚甘油化的脂肪醇可以混合物的形式共存。
烷基(多)糖苷非离子表面活性剂可由下式(IX)代表:
(IX)
其中:
R30代表包含约8 至24个碳原子的饱和或不饱和的、直链或支链的烃基(alkylgroup);或其中直链或支链的烷基包含8至24个碳原子的烷基苯基;
R31代表含有约2至4个碳原子的亚烷基,
G代表包含5至6个碳原子的糖单元,
t表示0至10或0至4范围内的值,以及
v表示1至15范围内的值。
在一些情况下,烷基(多)糖苷非离子表面活性剂对应于式(IX),其中:
R30表示含有8至18个碳原子的直链或支链的、饱和或不饱和的烃基(alkyl group),
G表示葡萄糖、果糖或半乳糖,优选葡萄糖,
t表示0至3范围内的值,并且优选等于0,以及
R31和v如先前所定义。
如例如由式(IX)中的下标v代表的烷基(多)糖苷非离子表面活性剂的聚合度平均在1至15或1至4范围内。该聚合度按平均计更特别在1至2、且仍更佳在1.1至1.5范围内。
糖单元之间的糖苷键为1.6或1.4型,且优选1.4型。
可尤其提及的式(IX)的化合物的实例是由Cognis公司以名称Plantaren®(600CS/U、1200和2000)或Plantacare®(818、1200和2000)销售的产品。还可使用由SEPPIC公司以名称Triton CG 110(或Oramix CG 110)和Triton CG 312(或Oramix® NS 10)销售的产品;由BASF公司以名称Lutensol GD 70销售的产品;或由Chem Y公司以名称AG10 LK销售的产品。还可使用例如1,4-(C8-C16)烷基多糖苷(作为53重量%的水溶液,相对于溶液的总重量计),其由Cognis以参考名Plantacare 818 UP销售。
两性或两性离子表面活性剂
可在根据本公开的组合物中使用的两性或两性离子表面活性剂可以是任选季铵化的脂族仲胺或叔胺的衍生物,在所述衍生物中,脂族基团是包含8至22个碳原子的直链或支链,所述胺衍生物含有至少一个阴离子基团,例如羧酸根、磺酸根、硫酸根、磷酸根或膦酸根。可特别提及(C8-C20)烷基甜菜碱,例如椰油基甜菜碱;磺基甜菜碱;(C8-C20)烷基酰胺基(C2-C8)烷基甜菜碱,例如椰油酰胺基丙基甜菜碱或(C8-C20)烷基酰胺基(C6-C8)烷基磺基甜菜碱、及其混合物。
在如上所定义的可使用的任选季铵化的脂族仲胺或叔胺的衍生物之中,还可提及以下相应结构(I)、(II)和(IIa)的化合物:
(I)
所述式(I)中:
Ra代表衍生自优选存在于水解椰子油中的酸Ra-COOH的C10-C30烷基或烯基,或庚基、壬基或十一烷基;
Rb代表β-羟乙基;以及
Rc代表羧甲基;
M+代表衍生自碱金属或碱土金属,例如钠的阳离子抗衡离子、铵离子或衍生自有机胺的离子;以及
X-代表有机或无机阴离子抗衡离子,例如选自卤离子、乙酸根、磷酸根、硝酸根、(C1-C4)烷基硫酸根、(C1-C4)烷基磺酸根或(C1-C4)烷基芳基磺酸根的那种,特别是甲基硫酸根和乙基硫酸根;或者不存在M+和X-;
(II)
所述式(II)中:
B代表基团-CH2-CH2-O-X';
B'代表基团-(CH2)zY',其中z=1或2;
X'代表基团-CH2-COOH、CH2-COOZ'、-CH2CH2-COOH或-CH2CH2-COOZ'或氢原子;
Y'代表基团-COOH、-COOZ'、CH2CH(OH)SO3H或基团-CH2CH(OH)SO3Z';
Z'代表衍生自碱金属或碱土金属,例如钠的阳离子抗衡离子、铵离子或衍生自有机胺的离子;
Ra'代表酸Ra'-COOH的C10-C30烷基或烯基,所述酸可以是椰子油或在水解的亚麻籽油中;或烷基,尤其C17基团及其异构形式;或不饱和的C17基团。
这种类型的化合物在CTFA词典(第5版,1993年)中以名称椰油酰两性基二乙酸二钠、月桂酰两性基二乙酸二钠、辛基两性基二乙酸二钠(disodiumcaprylamphodiacetate)、辛酰两性基二乙酸二钠、椰油酰两性基二丙酸二钠、月桂酰两性基二丙酸二钠、辛基两性基二丙酸二钠(disodium caprylamphodipropionate)、辛酰两性基二丙酸二钠、月桂酰两性基二丙酸和椰油酰两性基二丙酸进行归类。
通过举例方式,可提及由Rhodia公司以商品名Miranol C2M Concentrate销售的椰油酰两性基二乙酸盐和由Evonik Goldschmidt公司以商品名Rewoteric AM KSF 40销售的椰油酰两性基二丙酸盐。
(IIa)
在所述式(IIa)中:
Y''代表基团-COOH、-COOZ''、-CH2CH(OH)SO3H或基团-CH2CH(OH)SO3Z'';
Rd和Re彼此独立地代表C1-C4烷基或羟烷基;
Z''代表衍生自碱金属或碱土金属,例如钠的阳离子抗衡离子、铵离子或衍生自有机胺的离子;
Ra''代表酸Ra''-COOH的C10-C30烷基或烯基;
n和n'彼此独立地表示1至3范围内的整数;
和这些化合物的混合物。
在式(IIa)化合物之中,可提及在CTFA词典中以名称二乙氨基丙基椰油基天冬氨酰胺钠归类并且由Chimex公司以名称Chimexane HB销售的化合物。在一些情况下,两性或两性离子表面活性剂选自椰油基甜菜碱、椰油酰胺基丙基甜菜碱和椰油酰胺基乙基-N-羟乙基氨基丙酸钠。
术语“阴离子表面活性剂”表示仅包含阴离子基团作为离子基团或可电离基团的表面活性剂。这些阴离子基团优选选自基团CO2H、CO2 -、SO3H、SO3 -、OSO3H、OSO3 -、O2PO2H、O2PO2H和O2PO2 2-。
可使用的阴离子表面活性剂可以是烷基硫酸盐、烷基醚硫酸盐、烷基酰胺基醚硫酸盐、烷基芳基聚醚硫酸盐、甘油单硫酸酯盐、烷基磺酸盐、烷基酰胺磺酸盐、烷基芳基磺酸盐、α-烯烃磺酸盐、链烷烃磺酸盐、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、酰基肌氨酸盐、酰基谷氨酸盐、烷基磺基琥珀酰胺酸盐、酰基羟乙基磺酸盐及N-酰基牛磺酸盐、烷基单酯和多糖苷-多羧酸的盐、酰基乳酰乳酸盐、D-半乳糖苷糖醛酸的盐、烷基醚羧酸的盐、烷基芳基醚羧酸的盐、和烷基酰胺基醚羧酸的盐;或所有这些化合物的未盐化形式,所有这些化合物的烷基和酰基含有6至24个碳原子并且芳基表示苯基。这些化合物中的一些可为氧乙烯化的,并随后优选包含1至50个氧化乙烯单元。
多糖苷-多羧酸的C6-C24烷基单酯的盐可选自C6-C24烷基多糖苷-柠檬酸盐、C6-C24烷基多糖苷-酒石酸盐和C6-C24烷基多糖苷-磺基琥珀酸盐。
当阴离子表面活性剂为盐的形式时,它们可尤其选自碱金属盐,例如钠盐或钾盐,且优选钠盐;铵盐;胺盐,且特别是氨基醇盐;或碱土金属盐,例如镁盐。
可尤其提及的氨基醇盐的实例包括单乙醇胺、二乙醇胺和三乙醇胺盐;单异丙醇胺、二异丙醇胺或三异丙醇胺盐;2-氨基-2-甲基-1-丙醇盐;2-氨基-2-甲基-1,3-丙二醇盐和三(羟甲基)氨基甲烷盐。可使用碱金属盐或碱土金属盐,且特别是钠盐或镁盐。
还可使用(C6-C24)烷基硫酸盐、(C6-C24)烷基醚硫酸盐(其任选被乙氧基化,包含2至50个氧化乙烯单元)、及其混合物,特别是呈碱金属盐或碱土金属盐、铵盐或氨基醇盐的形式。更优选地,阴离子表面活性剂选自(C10-C20)烷基醚硫酸盐,且特别是含有2.2摩尔氧化乙烯的月桂基醚硫酸钠。
通过以下实施例来提供本公开的实施。实施例用来非限制性地阐述技术。
实施例1
(配制物)
根据本公开的三种组合物(A-C)呈现在下表中。
实施例2
(评价)
在皮肤科医生的监督下对年龄为18-45岁、具有中性-油性皮肤、油性皮肤或痤疮易发皮肤的五十四名女性完成四周安全性和非致粉刺性研究,所述皮肤具有至少一个痤疮后印记。每天对面部受影响的区域施加一至三次来自实施例1的组合物,避免与眼睛或具有破损皮肤的区域接触。在基线处以及在使用四周之后进行皮肤科医生评价,以确定损害计数和耐受性。本研究中还包括消费者评价。消费者评价的结果呈现在下表中。
在第2周,67.5%的消费者报告,可见孔的出现减少;并且在第4周,该数字猛增到77.8%的消费者。关于来自痤疮的黑色印记的减少,50%的消费者在第2周报告减少;并且在第4周该数字猛增到75.9%。
实施例3
(临床试验)
对年龄为18-50岁、患有轻度到中度痤疮(按大体评定量表(Global Assesment Scale)评分2-3)或具有痤疮易发皮肤(具有至少一种炎性损害)的五十名受试者(男性和女性)追踪完成7天研究。每天高达三次将实施例1的组合物施加于受试者的皮肤。基于如下显示的大体评定量表来募集皮肤。
结果呈现于下表中。
数据显示相比于基线,所有时间(点)评估的直径和高度都显著下降(改善)。相比于基线,在第 2、3和7天,发红显示统计和临床上的显著改善。
本研究中还包括消费者评价,其结果提供如下。
如本文中使用的术语“包含”、“具有”和“包括”以其开放的、非限制性的意义使用。
术语“一(a, an)”和“该/所述(the)”理解为涵盖复数以及单数。
表述“至少一个/种”表示一个/种或更多个/种,并因此包括单独的组分以及混合物/组合。
本文中公开的所有范围和值是包含性的和可组合的。例如,落入本文所描述的范围内的本文所描述的任何值或点可充当最小值或最大值,以得到子范围等。
通过引用将本说明书中引用的所有出版物和专利申请并入本文,并出于任何目的和所有目的,如同每一篇单独的出版物或专利申请具体且单独地指示以通过引用并入。如果本公开与通过引用并入本文的任何出版物或专利申请之间存在不一致,则以本公开为准。
Claims (20)
1.一种化妆品组合物,其包含:
(a)化妆品可接受的载体;和
(b)皮肤活性成分的组合,所述组合包含:
i. 硫磺;
ii. 烟酰胺;和
iii. 苯乙基间苯二酚。
2.权利要求1所述的化妆品组合物,其中基于所述化妆品组合物的总量计,所述一种或更多种皮肤活性成分的总量为约1重量%至约50重量%。
3.权利要求1或权利要求2所述的化妆品组合物,其进一步包含:
(c)一种或更多种非离子表面活性剂。
4.以上权利要求中任一项所述的化妆品组合物,其中(c)的所述一种或更多种非离子表面活性剂选自多元醇酯、甘油醚、氧乙烯化醚、氧丙烯化醚和乙二醇聚合物。
5.权利要求4所述的化妆品组合物,其中(c)的所述一种或更多种非离子表面活性剂包含多元醇酯与乙二醇聚合物的组合。
6.权利要求5所述的化妆品组合物,其中(c)的所述一种或更多种非离子表面活性剂包含硬脂酸甘油酯、PEG-100硬脂酸酯和鲸蜡硬脂醇聚醚-20的组合。
7.权利要求4所述的化妆品组合物,其中(c)的所述一种或更多种非离子表面活性剂包含一种或更多种脂肪醇。
8.权利要求7所述的化妆品组合物,其中所述一种或更多种脂肪醇选自己醇、辛醇、2-乙基己醇、癸醇、月桂醇、异十三烷醇、肉豆蔻醇、鲸蜡醇、己基癸醇、棕榈油醇、硬脂醇、鲸蜡硬脂醇、异硬脂醇、油醇、反油醇、岩芹醇、亚油醇、亚麻醇、桐醇、花生醇、鳕油醇、山萮醇、辛基十二烷醇、瓢儿菜醇、巴惟醇、椰子油和山萮醇。
9.权利要求3所述的化妆品组合物,其中基于所述化妆品组合物的总重量计,(c)的所述一种或更多种非离子表面活性剂的总量为约0.1重量%至约15重量%。
10.权利要求1所述的化妆品组合物,其进一步包含:
(d)一种或更多种维生素或其衍生物。
11.权利要求10所述的化妆品组合物,其中(e)的所述一种或更多种维生素或其衍生物选自抗坏血酸、维生素A、维生素E和维生素B5。
12.权利要求10所述的化妆品组合物,其中所述一种或更多种维生素及其衍生物的总量为约0.01重量%至约5重量%。
13.以上权利要求中任一项所述的化妆品组合物,其中(a)的所述化妆品可接受的载体包含水和一种或更多种化妆品可接受的有机溶剂。
14.权利要求13所述的化妆品组合物,其中所述一种或更多种化妆品可接受的有机溶剂选自乙二醇、丙二醇、丁二醇、己二醇、丙二醇和甘油。
15.以上权利要求中任一项所述的化妆品组合物,其中(a)的所述皮肤活性成分的组合进一步包含:
iv. 乙醇酸。
16.以上权利要求中任一项所述的化妆品组合物,其中(a)的所述皮肤活性成分的组合进一步包含:
v. 尿囊素。
17.权利要求1所述的化妆品组合物,其包含:
i. 约5重量%至约15重量%的硫磺(10%);
ii. 约1重量%至约10重量%的烟酰胺(4%);和
iii. 约0.1重量%至约2重量%的苯乙基间苯二酚(0.5%)。
18.一种向皮肤提供抗炎和/或抗菌益处的方法,其包括将以上权利要求中任一项的组合物施加于所述皮肤。
19.一种治疗痤疮的方法,其包括将以上权利要求中任一项的组合物施加于所述皮肤。
20.一种改善皮肤外观的方法,其包括将以上权利要求中任一项的组合物施加于所述皮肤。
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CN117618312A (zh) * | 2023-12-12 | 2024-03-01 | 广州美兮生物科技有限公司 | 一种祛痘组合物及其应用 |
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WO2017210239A1 (en) | 2017-12-07 |
EP3478277A1 (en) | 2019-05-08 |
EP3478277A4 (en) | 2020-01-08 |
US20180085297A1 (en) | 2018-03-29 |
ES2882049T3 (es) | 2021-12-01 |
CN117357429A (zh) | 2024-01-09 |
EP3478277B1 (en) | 2021-06-23 |
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