CN1221334A - 皮肤洗涤组合物 - Google Patents

皮肤洗涤组合物 Download PDF

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CN1221334A
CN1221334A CN97195350A CN97195350A CN1221334A CN 1221334 A CN1221334 A CN 1221334A CN 97195350 A CN97195350 A CN 97195350A CN 97195350 A CN97195350 A CN 97195350A CN 1221334 A CN1221334 A CN 1221334A
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林达·R·查尔顿
朱丽叶·T·麦吉利卡迪
沙伦·欧文
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Abstract

一种打算局部涂敷到用水润湿的皮肤上的皮肤洗涤组合物,含有α－羟基酸活性成分,该活性成分配制在柔和并且无刺激的由非离子烷基聚葡糖苷表面活性剂和两性表面活性剂的混合物构成的洗涤剂基料中。

Description

皮肤洗涤组合物
本发明涉及局部涂敷到皮肤表面的组合物，特别是涉及涂敷到用水润湿的皮肤上并且随后用水漂洗掉的皮肤洗涤组合物。本发明具体涉及含有α-羟基酸和本文定义的其它酸的皮肤洗涤组合物，上述酸作为活性成分配制在柔和且无刺激的洗涤剂基料中。
化妆和治疗皮肤处理领域中通常公知的化合物如α-羟基酸和本文定义的其它酸包括诸如水杨酸、乳酸和乙醇酸的化合物。这些化合物构成许多涂敷到皮肤上以便给予外观和皮肤状况(特别是光滑性和柔和性)有益效果的市售产品的活性成分。例如，水杨酸已显示出具有溶角蛋白和消除粉刺(comedolytic)活性以及抗菌功效，并已用于治疗和防治轻度到中度的痤疮一百多年。乳酸对皮肤水合具有有益效果，且是许多皮肤增强剂和滋润产品的组分。
尽管α-羟基酸和本发明定义的其它酸给皮肤赋予有益效果，但它们涂敷到皮肤的敏感部位，特别是脸上时可引起局部刺激。而且，局部刺激可以被活性成分配制在其中的载体系统恶化。例如，通常用选自用来清洁和起泡的无皂洗涤剂基料配制的皮肤洗涤组合物，特别是脸部洗涤组合物可能产生刺激作用，这是由于使用了通常用于这类洗涤剂系统中的离子型表面活性剂。
由于想要在酸性pH下(在该pH下大多数有功效的游离酸形式的酸将起主要作用)配制组合物，从而产生了与配制含有α-羟基酸和本发明定义的其它酸的组合物相关的另一个问题。对于皮肤洗涤组合物来说，该问题被难于在足够低的pH下获得洗涤剂基料系统而加剧。市场上可买到在一洗涤剂基料中含有用于治疗痤疮的柔和而有效的清洗剂并含有2.0％重量/重量水杨酸的皮肤洗涤组合物，所述洗涤剂基料含有阴离子和两性表面活性剂的混合物。对该产品进行分析表明其pH为5。由于水扬酸的pKa值为2.97，从而得出游离酸形式的羟基酸在该产品中不起主要作用，因此没有完全发挥其功效的最大作用。
本发明的一个目的是提供一种皮肤洗涤组合物，该组合物含有α-羟基酸或本文定义的其它酸和洗涤剂基料，该洗涤剂基料具有良好的清洁和起泡特性，柔和且无刺激，其中组合物的pH达到酸的pKa从而酸的功效得到增强。根据本发明，该目的是这样实现的：它是基于意想不到的发现，即含有非离子性烷基聚葡糖苷表面活性剂和两性表面活性剂的混合物的洗涤剂基料不仅具有所需的清洁和起泡特性，当涂敷到皮肤上时是柔和的且无刺激，而且使组合物能够在低pH下配制。
根据本发明，提供了皮肤洗涤组合物，该组合物含有0.1～10％重量/重量的α-羟基酸或本文定义的其它酸和由非离子性烷基聚葡糖苷表面活性剂和两性表面活性剂的混合物构成的洗涤剂基料，其中组合物的pH的范围是3.0～4.5。
适用于加入到本发明的皮肤洗涤组合物中的酸包括水扬酸、乳酸、柠檬酸、乙醇酸、苹果酸、马来酸、丙酮酸和羟基-辛酸。优选的酸是水杨酸、乳酸和乙醇酸，特别是水杨酸和乳酸。水杨酸适宜以0.2～5.0％w/w的范围、更适合以1.0～3.0％w/w的浓度存在。水杨酸的优选浓度是2.0％w/w。乳酸适合以0.1～5.0％w/w、更优选以0.5～2.5％w/w的浓度存在于本发明的组合物中。乳酸的优选浓度为1％w/w。乙醇酸适合以2.0～10.0％w/w的浓度存在。
此处所用的术语“烷基聚葡糖苷表面活性剂”是指衍生于淀粉、脂肪和蔗糖中存在的普通天然有机单体单元、最适合衍生于D-葡萄糖单体单元的非离子表面活性剂。衍生于D-葡萄糖的烷基聚葡糖苷是乙缩醛化合物，其中烷基残基的碳链长度为8～16个碳原子且苷化(或聚合)度，即每个烷基的葡萄糖单元的平均数为1.1～6。一系列合适的烷基聚葡糖苷可以单独或作为混合物或共混物买到。本发明的组合物通常含有不同烷基聚葡糖苷的混合物或共混物。用于本发明的优选的烷基聚葡糖苷包括癸基葡糖苷和月桂基葡糖苷及其混合物。烷基聚葡糖苷表面活性剂通常占皮肤洗涤组合物的高达20％w/w、适合地2.0～15.0％w/w，优选4.0～10.0％w/w。可以理解，烷基聚葡糖苷的用量在某些程序上由组合物中存在的两性表面活性剂的性质和用量决定。
原则上，适合局部涂敷于皮肤上的任何两性表面活性剂可与烷基聚葡糖苷表面活性剂一起用作洗涤剂基料，但是考虑到其内在的柔和性和良好的起泡性，优选的两性表面活性剂属于公知为甜菜碱的那类化合物。从结构上说，甜菜碱化合物含有羧酸盐官能团和被亚甲基部分隔开的季氮官能团。它们包括正烷基甜菜碱，如十六烷基甜菜碱和山萮基甜菜碱，以及正烷基酰氨基甜菜碱如椰油酰氨基丙基甜菜碱。本发明组合物用的洗涤剂基料的两性表面活性剂组分可以是单一化合物或两种或多种不同物质的混合物或共混物。优选的两性表面活性剂是椰油酰氨基丙基甜菜碱。两性表面活性剂通常占皮肤洗涤组合物的高达10％w/w，适合地为2.0～8.0％w/w，优选为2.5～6.0％w/w。两性表面活性剂的用量在某种程度上由洗涤剂基料的烷基聚葡糖苷表面活性剂组分决定。
通常，由非离子烷基聚葡糖苷表面活性剂和两性表面活性剂构成的洗涤剂基料占皮肤洗涤组合物的高达30％w/w。适合地是，洗涤剂基料占皮肤洗涤表面活性剂的5.0～20.0％w/w，更适合地为8.0～18.0％w/w。
将pH控制在限定的范围内是本发明的一个基本特征。在所需范围3.0～4.5内的pH部分由酸的内在性能、具体的表面活性剂和构成表面活性剂基料的表面活性剂的量给予，部分地(需要时)由所使用的酸用的适合的中和剂决定。可以使用任何与该组合物的其它组分相容的局部可接受的中和剂。现已发现中和剂tromethamine特别适用于含有α-羟基酸或本发明定义的其它酸的皮肤洗涤组合物。其它适合的中和剂包括氢氧化钠和三乙醇胺。中和剂的用量将由构成组合物的其它组分的酸/碱性能和组合物选用的pH决定。
本发明的皮肤洗涤组合物也可含有其它局部可接受的皮肤调理和润肤剂，如为抗炎剂和维生素或维生素衍生物，通常以较低的浓度，例如在整个组合物的0.01～2.0％w/w的范围内。局部可接受的抗炎剂的实例包括尿囊素和红没药醇。优选的维生素衍生物是具有抗炎作用的维生素E乙酸盐。
另外，本发明的组合物适当含有局部医药和化妆品领域常用的药学和美容上可接受的添加剂或赋形剂，包括如增稠剂、增湿剂、再脂化剂(re-fattingagents)、保存剂、调理剂、螯合剂、着色剂、香料、紫外过滤剂和/或乳化剂。任何给定的组合物中所用的添加剂或赋形剂是彼此相容的，并且与组合物的其它成分相容，从而不损害活性成分性能的相互作用。当然，所有的添加剂或赋形剂必须是无毒的且具有足够的纯度以使它们适合人类使用。
合适的增稠剂包括由长链(C12-18)聚乙二醇脂肪酸或脂肪酸残基构成的聚合物高分子量、非离子表面活性剂。实例包括PEG200氢化甘油基棕榈酸酯、PEG55聚乙二醇油酸酯、PEG150二硬脂酸酯和PEG200甘油基牛油酯。合适的低分子量增稠剂包括椰油二乙醇酰胺、月桂基聚氧乙烯醚(laureth-3)和甘油基单月桂酸酯。以商品名Acrysol44销售的含有聚氨酯树脂、丙二醇和水的增稠剂也在洗涤剂基皮肤洗涤组合物中起良好的作用。增稠剂适合占组合物重量的高达10.0％w/w，更适合为2.0～5.0％w/w。优选的增湿剂包括甘油、丙二醇、山梨醇和聚乙二醇。增湿剂可占组合物重量的15％w/w，更优选2.0～6.0％w/w。合适的再脂化剂通常占组合物重量的0.5～5.0％w/w、优选0.75～2.0％w/w，包括聚乙二醇7和甘油基椰子酸酯。合适的保存剂通常占组合物重量的0.01～1.00％w/w，适合地为0.10～0.30％w/w，包括苯氧基乙醇和甲基二溴戊二腈及其混合物。合适的调理剂通常占组合物的0.1～5.0％w/w，适合地为1.0～3.5％w/w，包括羟基十六烷基羟乙基二甲基氯化铵和polyquatemium39。适合的螯合剂通常占组合物的高达1.0％w/w，适合地为0.1～0.3％w/w，包括乙二胺四乙酸(EDTA)、羟乙二胺四乙酸(HEEDTA)、二亚乙基三胺五乙酸(DPTA)和环己二胺四乙酸(CTDA)。
组合物的余量通常是水和/或其它非醇溶剂从而构成100％％w/w的组合物。优选的溶剂是水，它通常占皮肤洗涤组合物的50％w/w以上。其它可以加入以辅助α-羟基酸的溶液的合适的非醇溶剂包括二元醇如丙二醇和聚乙二醇(macrogol)。
本发明的皮肤洗涤组合物可以通过本领域公知的方法制备，并容易被熟练的配制师得到。通常酸和构成洗涤剂基料的表面活性剂以及任何添加剂溶解于溶剂中，检查最终混合物的pH，必要时进行调整，通过加入增稠剂将组合物的粘度设定在所需的水平上。本发明扩展到前面定义的皮肤洗涤组合物的制备方法，该组合物含有α-羟基酸或前面定义的其它酸和含水溶剂系统中的洗涤剂基料的掺混物，根据需要调节pH，从而该组合物的pH范围为3.0～4.5。
本发明还包括前面定义的皮肤洗涤组合物用于生产痤疮治疗和/或防治的药剂，其中酸是水杨酸。前面定义的本发明的组合物用作美容治疗剂以改进人类皮肤的外观和状况也构成本发明的一部分。
下列实施例还描述并用实验证明了落在本发明范围内的组合物。勿需置疑，这些实施例仅用于说明，并非构成对本发明范围的限制。实施例1-含有乳酸的皮肤洗涤组合物
制备含有下述成分的组合物。所得组合物的pH约3.5。组分                                 ％w/wα-羟基酸： 乳酸                     1.0洗涤剂基料：癸基苷                   3.5
        月桂基苷                 3.6
        椰油酰氨基丙基甜菜碱     5.0增稠剂：    PEG120甲基葡萄糖二油酸酯 3.2保存剂：    苯氧基乙醇               0.25溶剂：      水                       至100％实施例2-含有水杨酸的皮肤洗涤组合物
制备含有下列成分的组合物。所得组合物为透明产品，其pH为4.5。组分                                 ％w/w酸：        水杨酸                   2.0洗涤剂基料：月桂基苷                 2.4
        癸基苷                   2.0
        椰油酰氨基丙基甜菜碱     2.8中和剂：    Tromethamine             1.5增稠剂：    PEG120甲基葡萄糖二油酸酯 4.0溶剂：      去离子水                 至100％实施例3-含有水杨酸的皮肤洗涤组合物
制备含有下列附加赋形剂的实施例2的组合物。所得透明产品的pH为4.5。调理剂：    羟基十六烷基羟乙基二甲基氯化铵螯合剂：    EDTA保存剂：    苯氧基乙醇抗炎剂：    尿囊素&维生素E乙酸盐。

Claims (24)

1．一种皮肤洗涤组合物，其含有0.1～10％W/W的α-羟基酸或本发明定义的其它酸及由非离子烷基聚葡糖苷表面活性剂和两性表面活性剂的混合物构成的洗涤剂基料，其中所述组合物的pH范围为3.0～4.5。
2．权利要求1的组合物，其中所述酸是柠檬酸、苹果酸、马来酸、丙酮酸、羟基-辛酸、水杨酸、乳酸或乙醇酸。
3．权利要求2的组合物，其中所述酸是水杨酸。
4．权利要求3的组合物，含有0.2～5％W/W的水杨酸。
5．权利要求4的组合物，含有1.0～3.0％W/W的水杨酸。
6．权利要求2的组合物，其中α-羟基酸是乳酸，它占组合物的0.1～5.0％W/W。
7．权利要求6的组合物，含有0.5～2.5％W/W的乳酸。
8．权利要求2的组合物，其中α-羟基酸是乙醇酸，它占组合物的2.0～10.0％W/W。
9．权利要求1～8中任一项的组合物，其中烷基聚葡糖苷表面活性剂是癸基苷、月桂基苷或其混合物。
10．权利要求1～9中任一项的组合物，其中烷基聚葡糖苷表面活性剂占所述组合物的高达20％W/W。
11．权利要求10的组合物，其中烷基聚葡糖苷表面活性剂占所述组合物的2.0～15％。
12．权利要求1～11中任一项的组合物，其中两性表面活性剂包括至少一种甜菜碱。
13．权利要求12的组合物，其中甜菜碱是椰油酰氨基丙基甜菜碱。
14．权利要求1～13中任一项的组合物，其中两性表面活性剂占所述组合物的高达10％W/W。
15．权利要求14的组合物，其中两性表面活性剂占组合物的2.0～8.0％W/W。
16．权利要求1～15中任一项的组合物，其中洗涤剂基料占所述组合物高达30％W/W。
17．权利要求1～16中任一项的组合物，还包括一种中和剂。
18．权利要求17的组合物，其中所述中和剂是tromethamine、氢氧化钠或三乙醇胺。
19．根据上述任一权利要求的组合物，基本上如参照实施例本发明所描述的那样。
20．一种制备权利要求1～19中任一项所定义的组合物的方法，该方法包括将α-羟基酸或本发明定义的其它酸与含水溶剂系统中的洗涤剂基料相混合，并按照需要调节pH。
21．权利要求3～5及9～20中任一项权利要求所限定的组合物用于治疗和/或防治痤疮。
22．权利要求3～5和9～20任一项权利要求的组合物在生产用于治疗和/或防治痤疮的药剂中的应用。
23．一种治疗和/或防治痤疮的方法，包括给药有效量的权利要求3～5及9～20中任一项所定义的药物组合物。
24．权利要求1～19中任一项的组合物作为美容治疗剂用于改善人的皮肤的外观和状况。
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CZ293773B6 (cs) 2004-07-14
PT906086E (pt) 2003-12-31
ZA975062B (en) 1998-08-12
PL186808B1 (pl) 2004-02-27
US20030118540A1 (en) 2003-06-26
EA001573B1 (ru) 2001-06-25
SK284219B6 (en) 2004-11-03
ATE246485T1 (de) 2003-08-15
AR007542A1 (es) 1999-11-10
CA2257810C (en) 2008-08-12
HU226084B1 (en) 2008-04-28
DE69723979D1 (de) 2003-09-11
JP2000512636A (ja) 2000-09-26
MY124104A (en) 2006-06-30
BR9709774A (pt) 1999-08-10
US6486106B1 (en) 2002-11-26
WO1997047171A1 (en) 1997-12-18
DE69723979T2 (de) 2004-07-22
PL330603A1 (en) 1999-05-24
UA57023C2 (uk) 2003-06-16
AU720020B2 (en) 2000-05-18
NO314218B1 (no) 2003-02-17
EA199801001A1 (ru) 1999-06-24
NZ332864A (en) 2000-07-28
TW460294B (en) 2001-10-21
NO985638D0 (no) 1998-12-03
CY2506B1 (en) 2005-12-23
US7179771B1 (en) 2007-02-20
EP0906086A1 (en) 1999-04-07
US6162774A (en) 2000-12-19
CA2257810A1 (en) 1997-12-18
HUP0001821A3 (en) 2003-04-28
HUP0001821A2 (hu) 2000-11-28
CN1121211C (zh) 2003-09-17
KR20000016515A (ko) 2000-03-25

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