CN1096845C - 皮肤增白组合物 - Google Patents
皮肤增白组合物 Download PDFInfo
- Publication number
- CN1096845C CN1096845C CN96180540A CN96180540A CN1096845C CN 1096845 C CN1096845 C CN 1096845C CN 96180540 A CN96180540 A CN 96180540A CN 96180540 A CN96180540 A CN 96180540A CN 1096845 C CN1096845 C CN 1096845C
- Authority
- CN
- China
- Prior art keywords
- composition
- weight
- sulfite
- skin whitening
- acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 206010040829 Skin discolouration Diseases 0.000 title 1
- 239000000203 mixture Substances 0.000 claims abstract description 175
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims abstract description 78
- 230000002087 whitening effect Effects 0.000 claims abstract description 65
- 239000003638 chemical reducing agent Substances 0.000 claims abstract description 40
- 235000010265 sodium sulphite Nutrition 0.000 claims abstract description 39
- 239000002537 cosmetic Substances 0.000 claims abstract description 35
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims abstract description 21
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 claims abstract description 18
- 238000000034 method Methods 0.000 claims abstract description 16
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims abstract description 14
- DJEHXEMURTVAOE-UHFFFAOYSA-M potassium bisulfite Chemical compound [K+].OS([O-])=O DJEHXEMURTVAOE-UHFFFAOYSA-M 0.000 claims abstract description 14
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims abstract description 7
- PQUCIEFHOVEZAU-UHFFFAOYSA-N Diammonium sulfite Chemical compound [NH4+].[NH4+].[O-]S([O-])=O PQUCIEFHOVEZAU-UHFFFAOYSA-N 0.000 claims abstract description 7
- 235000019253 formic acid Nutrition 0.000 claims abstract description 7
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- BHZRJJOHZFYXTO-UHFFFAOYSA-L potassium sulfite Chemical compound [K+].[K+].[O-]S([O-])=O BHZRJJOHZFYXTO-UHFFFAOYSA-L 0.000 claims abstract description 7
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- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 7
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Landscapes
- Cosmetics (AREA)
Abstract
本发明所公开的是一种皮肤增白美容组合物,该组合物包括:(a)至少一种安全、有效量的水溶性还原剂,选自:亚硫酸钠、亚硫酸钾、亚硫酸氢钠、亚硫酸氢钾、偏亚硫酸氢钠、偏亚硫酸氢钾、亚硫酸铵、亚硫酸氢铵、甲酸、草酸及其混合物和b)化妆品可用的水溶性还原剂的载体,其中该组合物基本不含氢醌或其衍生物。本发明还公开了哺乳动物皮肤增白的方法,包括向皮肤上局部施用所述的皮肤增白美容组合物。
Description
技术领域
本发明涉及皮肤增白领域。具体地讲,本发明涉及包括用于皮肤增白的特定还原剂的新组合物。
背景技术
黑素的形成取决于三种物质的存在:(1)一种合适的基质如酪氨酸和多巴,(2)分子氧和(3)酶酪氨酸酶(一种铜蛋白质复合物)。如果这些物质中的任意一种缺少或有所降低都会影响黑素的形成。
还原剂可通过下述机制阻碍黑素的形成:(1)它与酶体系中的一些铜络合并通过与铜络合而减少了黑素的酶的形成,原因是酪氨酸酶的辅酶是铜蛋白质复合物。(2)黑素形成的必需基质(酪氨酸和多巴)是经细菌和酶分解蛋白质而形成的。细菌量的减少将抑制分解蛋白的断裂,因此由于还原剂(如亚硫酸钠)是一种杀菌物,所以有助于降低黑素源。(3)与黑素基质相比,该强还原剂(如亚硫钠)本身更易被氧化。
已转让给Institute of Chemical-Pharmaceutical Research(Bucharest)的罗马尼亚专利申请100161公开了使用如偏亚硫酸氢钠的还原剂在消除令人不快气味方面的用途。
转让给Helena Rubinstein的USP 4136166、转让给Warner-Lambert的USP 4792443、转让给宝洁公司的USP 5514437和已转让给MochidaPharmaceutical Co.的日本特许公开6-263624都公开了亚硫酸盐、亚硫酸氢盐和偏亚硫酸氢盐作为稳定剂或抗氧化剂的用途。
转让给Shiseido的日本特许公开54-129134公开了(i)亚硫酸盐或亚硫酸氢盐和有机溶剂,(ii)铁盐和(iii)过氧化氢的组合体具有漂白头发黑素的作用。
已转让给Sansyo Pharmaceutical的日本特许公开3-101609,转让给Shiseido的日本特许公开3-279313,转让给Kose的日本特许公开4-352708,转让给Shiseido的日本特许公开63-174910和转让给Kao的日本特许公开7-25742中公开了亚硫酸盐、亚硫酸氢盐和焦亚硫酸盐具有防止产品着色的作用。
日本特许公开5-139928已转让给Hisamitsu Pharmaceutical Co.,在该专利中公开了亚硫酸氢钠、偏亚硫酸氢钠作为抗氧化剂的用途。
日本特许公开5-179300已转让给Kitano Kagaku,在该专利中公开了亚硫酸氢钠被用于漂白皮革。
日本特许公开7-21588g、8-12548、8-12549、8-12550、8-12552、8-12554、8-12556、8-12557、8-12558和8-12565(已转让Shiseido)和日本特许公开59-157009(转让给Yakurigaku Cyuo Kenkyusho)中公开了在包括特定的增白皮肤或控制黑素活性物质的皮肤增白或控制黑素的组合物中包含有非常少量的亚硫酸氢钠或亚硫酸钠。
目前已发现水溶性还原剂选自亚硫酸钠、亚硫酸钾、亚硫酸铵、亚硫酸氢钠、亚硫酸氢钾、亚硫酸氢铵、偏亚硫酸氢钠、偏亚硫酸氢钾、甲酸、草酸以及其混合物,它们可被用来增白哺乳动物的皮肤。
本发明涉及皮肤增白美容组合物,包括:(a)至少一种安全、有效量的水溶性还原剂,选自亚硫酸钠、亚硫酸钾、亚硫酸铵、亚硫酸氢钠、亚硫酸氢钾、亚硫酸氢铵、偏亚硫酸氢钠、偏亚硫酸氢钾、甲酸、草酸及其混合物,(b)一种水溶性还原剂的化妆品中可用的载体,其中所述组合物基本不含氢醌或其衍生物。
本发明的皮肤增白组合物优选包括所述的水溶性还原剂和卵磷脂。
本发明的皮肤增白组合物更优选包括(a)上述水溶性还原剂,(b)化妆品中可用的液态油,(c)多羟基醇,(d)固态脂肪醇,(e)表面活性剂,(f)水和(g)卵磷脂,其中至少上述组分(a)、(b)、(c)、(d)、(e)、(f)和(g)中的一部分形成液晶(liquid crystal)。
这种组合物满足了哺乳动物皮肤增白的需要。
本文所用的“局部施用”是指直接涂在或扩散于外部皮肤上。
本文所用的“皮肤增白”是指减少皮肤中黑素,包括一种或多种皮肤基调的整体增白;高增色损害后的增白,所述皮肤颜色加深包括老年斑、黑斑病、褐黄斑、雀斑、炎症过后的色素沉着过度或日光引起的色调加深的斑伤。
本文所用的“固体”是指在25℃时为固态形式,“液体”是指在25℃时为液态形式。
除非另外说明,本文中所用的百分比都是指重量百分比。A.水溶性还原剂
本发明的组合物包括一种水溶性还原剂。这种还原剂选自亚硫酸钠、亚硫酸钾、亚硫酸铵、亚硫酸氢钠、亚硫酸氢钾、亚硫酸氢铵、偏亚硫酸氢钠、偏亚硫酸氢钾、甲酸、草酸及其混合物。如果组合物中包括的还原剂超过组合物重量的约5%,就会带来安全性问题;如果包括的还原剂小于组合物重量的0.1%,则得不到所期望的皮肤增白效果。
本发明的皮肤增白组合物优选包括约0.1%-5%,更优选约0.15%-5%,进一步优选约0.2%-5%,最优选约0.25%-5%组合物重量的还原剂。
还原剂中,优选使用亚硫酸钠、亚硫酸氢钠、偏亚硫酸氢钠及其混合物。
本发明的皮肤增白组合物基本不含氢醌或其衍生物,并且优选完全没有氢醌及其衍生物,这是因为氢醌及其衍生物被认为会干扰水溶性还原剂的增白活性。这种氢醌衍生物包括4-[(四氢-2H-吡喃-2-基)氧]苯酚和4-[四氢-2H-硫代吡喃-2-基)氧]苯酚以及在WO 9523780中描述的那些,所述文献引入本文作为参考。B.卵磷脂
本发明的皮肤增白组合物优选包括上述水溶性还原剂和卵磷脂。卵磷脂是一种天然产品,来自大豆或蛋黄,用于增强还原剂的皮肤增白效果。如果组合物包括的卵磷脂超过组合物重量的10%,就会带来粘性问题;如果组合物所含的卵磷脂少于组合物重量的0.01%,则不能得到所期望的增强还原剂的皮肤增白作用。
本发明皮肤增白组合物中的卵磷脂的含量优选占组合物重量的约0.01%-10%,更优选约0.5%-3%。C.化妆品中可用的载体
本文中所用的短语“化妆品中可用的载体”是指一种或多种相容的固体或液体填充剂、稀释剂、增量剂等,这些都是如以上所定义的是化妆品中可以使用的。本文中所用的术语“相容的”是指本发明组合物中的各组分能够与本发明中的基本活性物质共混并且在通常的使用条件下各组分相互之间不产生降低组合物实质功效的相互作用。本发明中所使用的载体的类型取决于所希望得到的产品的类型。本发明中使用的局部用组合物可被制成各种形式的产品。这些包括,但不限于,洗液、乳膏、胶体、棒、喷剂、软膏、贴剂、摩丝和各种美容品(例如固态、半固态、液态粉底,包括打底物)。这些产品类型可包括各种载体,包括(但不局限于),溶液,气溶胶,乳化液(包括水包油型和油包水型)、胶体、固体和脂质体。
本发明的溶液通常包括水和化妆品可用的有机溶剂。优选使用的是水。合适的有机溶剂的实例包括:丙二醇、聚乙二醇(例如,分子量200-600g/mol)、聚丙二醇(例如分子量425-2025g/mol)、甘油、1,2,4-丁三醇、1,2,6-己三醇、乙醇、异丙醇、山梨醇酯、丁二醇及其混合物。本发明中所用的溶液优选包含约50-99.9%的水或水和可用的有机溶剂,以及上述量的水溶性还原剂。
本发明的气溶胶可通过向上述溶液中加入一种推进剂而配成。例举的推进剂包括氯-氟化的低分子量烃。本发明中可用的另外的推进剂叙述在Sagarin,《化妆品用科学和技术》(Cosmetics Science and
Technology),第二版,第二卷,443-465页(1972年)中,其被引入本文作为文献。气溶胶通常可被以喷涂产品的形式施用到皮肤上。
本发明的乳化液通常包含上述溶液和类脂体或油。类脂体和油可得自动物、植物、或石油产品,其可以是天然的,也可以是合成的(如人造的)。优选的乳化液还包含保湿剂(如甘油)。优选乳化剂还包含约1%-10%,更优选约2%-5%的乳化剂,基于载体的重量。乳化剂可以是非离子、阴离子或阳离子性的。合适的乳化剂公开在,例如,1973年8月28日颁布给Dickert等人的USP 3,755,560;1983年12月20日颁布给Dixon等人的USP4,421,769;和McCutcheon′s Detergents and Emulsifiers,北美版,317-324页(1986年),均被本文作为参考文献引用。
乳化液还可以包括在施用到皮肤上时的减小起泡现象的消泡剂。消泡剂包括高分子量的硅氧烷及本领域中用于此用途的已知的其它材料。
乳化液优选包括带来优选的皮肤舒适感的硅氧烷。这类硅氧烷通常具有低分子量。合适的硅氧烷包括聚环甲基硅氧烷、聚二甲基硅氧烷及聚环甲基硅氧烷、聚二甲基硅氧烷和/或聚二甲基硅氧烷醇(dimethiconol)的混合物,如Dow Corning 200流体(特别是10cs)和Dow Corning QZ-1401。这些硅氧烷可购自Dow Corning Corp.of Midland,MI。
本发明的局部组合物可包括局部的化妆品用润滑剂,优选包括约2-50%的润滑剂。本文所用的“润滑剂”是指用来防止或缓解干燥、用来保护皮肤的物质。各种已知的合适的润滑剂可用于本发明中。引入本文作为参考的Sagarin,Cosmetics,Science and Technologv,第二版,第一卷,32-43页(1972年)包括了众多的适用作润滑剂材料的实例。
本发明的洗液和乳膏通常包括一种溶液载体体系和一种或多种润滑剂。洗液通常包括约0.01%-50%,优选约0.1%-20%的润滑剂;约30%-99%,优选约50%-90%的水;前面所述量的基本活性物质。乳膏通常包括约5%-50%,优选约10%-30%的润滑剂;约45%-90%,优选约50-85%的水;以及在前面所述量的主要活性物质。D.液态晶体的形成
本发明的皮肤增白组合物更优选包括(a)上述水溶性还原剂,(b)化妆品可用的液态油,(c)多羟基醇,(d)固体脂肪醇,(e)表面活性剂,(f)水和(g)卵磷脂,其中至少一部分的上述组分(a)、(b)、(c)、(d)、(e)、(f)和(g)中的形成了液态晶体。
液态晶体可通过偏光显微镜观测液晶的形状而被检测。
本发明的包括液晶的皮肤增白组合物中的化妆品可用的液态油的量优选约为组合物重量的1%-50%,更优选约3%-25%。
本发明包括液晶的皮肤增白组合物中的多羟基醇的量优选约为组合物重量的0.1%-20%,更优选约1%-10%。
本发明包括液晶的皮肤增白组合物中的固体脂肪醇的量约为组合物重量的0.1-20%,更优选约1.0-5%。
本发明包括液晶的皮肤增白组合物中的表面活性剂的量约为组合物重量的0.1-10%,更优选约0.1-3%。
本发明包括液晶的皮肤增白组合物中的水的量约为组合物重量的40%-90%,更优选约60-90%。
本发明包括液晶的皮肤增白组合物中的卵磷脂的量优选为组合物重量的约0.0 1%-10%,更优选约0.1%-3%。
本发明包括液晶的皮肤增白组合物可被制成乳化液型产品。乳化液型产品包括,但不限于,奶性洗液(milky lotion)和乳膏。
可形成液晶的化妆品用液态油、多羟基醇、固体脂肪醇和表面活性剂如下所述:
(1)化妆品用液态油
化妆品用液态油包括在化妆品用载体中。化妆品用液态油在室温下为液态。化妆品可用的液态油可以是液态烃油、液态天然油、液态脂肪醇、液态脂肪酸、液态脂肪酸酯、液态硅氧烷油以及糊蜡(paste wax)及其混合物。
液态烃的非限制性实例是角鲨烷、液态矿物油及液态聚丁烯。
本发明中可用的得自植物的液态天然油的非限制性实例包括:杏仁油、橄榄油、芝麻油(sesami oil)、红花油、鳄梨油、棉籽油、西蒙得木油(jojobaoil)、蓖麻油、大豆油、棕榈仁油、椰子油和氢化的植物油。本发明中所用的源自动物的液态天然油的非限制性实例包括貂油和蛋黄油。
本发明中所用的液态脂肪醇的非限制性实例是异硬脂醇、羊毛脂醇、油醇、十六醇、辛基十二烷醇、亚油醇(linoleyl alcohol)、亚麻醇(linolenylalcohol)、月桂醇和花生醇。
脂肪酸可以是天然或合成、饱和或不饱和、线性或支链的脂肪酸。本发明中所用的脂肪酸的非限制性的实例是辛酸、异硬脂酸、亚油酸、蓖麻油酸和油酸。
本发明中使用的液态脂肪酸酯的非限制性实例是辛酸十六酯、三辛酸甘油酯、亚油酸异丙酯、肉豆蔻酸异丙酯、油酸异丙酯、月桂酸乙酯、亚油酸乙酯、辛基十二烷基肉豆蔻酸酯、棕榈酸辛酯、异壬酸辛酯、辛基十二烷基乳酸酯、异壬酸异十三烷酯、油酸油酯、肉豆蔻酸异硬脂酯、新戊基二醇二辛酸酯、二(癸基/癸酸)丙二醇及其混合物。其它合适的酯包括甘油三酯,如辛酸甘油三酯、癸酸甘油三酯、异硬脂酸甘油三酯和己二酸甘油三酯。
也可使用非挥发性的、直链、支链的硅氧烷油,如聚二甲基硅氧烷和苯基聚二甲基硅氧烷。
其它化妆品用液态油包括甲氧基肉桂酸辛酯、cinoxate和对二甲基氨基苯甲酸2-乙基苯基(phexyl)酯。
本发明还可以使用一种、两种或多种化妆品用液态油。
化妆品用液态油还能起润滑剂的作用,能给化妆品提供粘性和持久性。
(2)多元醇
多元醇包括甘油、二甘油、三甘油、聚甘油、聚丙二醇、聚乙二醇、乙二醇、二甘醇、三甘醇、丙二醇、二丙二醇、己二醇、1,3-丁二醇、1,4-丁二醇、乙二醇单烷基醚、二乙二醇单烷基醚、葡萄糖、麦芽糖、蔗糖、乳糖、木糖(xylitose)、木糖醇、山梨醇、甘露糖醇、麦芽糖醇(maltitol)、malbit、泛醇(panthenol)、季戊四醇和透明质酸及其盐。
在这些多元醇中,优选甘油。
本发明可使用一种、两种或多种多元醇。
(3)固态脂肪醇
固态脂肪醇包括花生醇、鲸蜡醇、硬脂醇、山嵛醇、肉豆蔻醇、鲨肝醇、胆甾醇和植物甾醇。
这些固态脂肪醇中,优选鲸蜡醇。
本发明中或使用一种、两种或多种固态醇。
(4)表面活性剂
表面活性剂包括非离子表面活性剂和阴离子表面活性剂。
非离子表面活性剂包括烷醇酰胺,如椰子二乙醇酰胺和月桂酰胺(lauramide)DEA,嵌段聚合物如环氧丙烷和环氧乙烷的嵌段共聚物,乙氧基脂肪酸如丙二醇单硬脂酸酯,乙氧基化的醇如聚氧乙烯(20)硬脂基醚,乙氧基化的烷基酚如聚氧乙烯(10)壬基苯醚,乙氧基化的脂肪酸如聚乙二醇(10环氧乙烷)单硬脂酸酯,乙氧基化的脂肪酯如聚氧乙烯(5)甘油基单硬脂酸酯,乙氧基化的脂肪酯和油如聚氧乙烯(10)氢化蓖麻油和聚氧乙烯(6)山梨醇蜂蜡,甘油酯如甘油基单硬脂酸酯和二甘油基单硬脂酸酯,羊毛脂基衍生物如聚氧乙烯羊毛脂,丙氧化和乙氧化的脂肪酸、醇或烷基酚如聚氧乙烯(10)聚氧丙烯(4)十六烷基醚,蛋白质基表面活性剂如聚氧乙烯(25)甘油单脓谷氨酸单异硬脂酸酯,脱水山梨醇衍生物如脱水山梨醇单硬脂酸酯、聚氧乙烯(20)脱水山梨醇单硬脂酸酯和聚氧乙烯(60)山梨醇四硬脂酸酯和蔗糖和葡糖酯及衍生物如蔗糖二硬脂酸酯和蔗糖硬脂酸酯。
阴离子表面活性剂包括磷酸酯如聚氧乙烯(4)月桂基醚磷酸酯钠和DEA鲸蜡基磷酸酯,三价磷的有机衍生物如磷酸化的油基醚(10环氧乙烷)和肥皂如硬脂酸钠和椰油酸钾。
本发明可使用一种、两种或多种表面活性剂。E.组合活性物质
(1)防晒和阻晒物(sunblocks)
对皮肤由于紫外光而晒黑的控制可通过使用活性增白剂和防晒或阻晒物的结合物而达到。有用的阻晒物包括,例如,氧化锌和二氧化钛。
紫外光是皮肤变黑的主要起因。因此,为了达到皮肤增白的目的,理想的是将水溶性还原剂与UVA和/或UVB防晒剂结合使用。
适合与皮肤增白剂联用的惯用的防晒剂包括很多。
Cosmetics Science and Technology(Segarin等,第三章,189等页以后)公开了大量适用的防晒剂。合适的防晒剂的具体实例如包括:对氨基苯甲酸、其盐及其衍生物(乙酯、异丁酯、甘油酯;对二甲基氨基苯甲酸);氨茴酸酯(即邻氨基苯甲酸酯;甲酯、酯、苯酯、苄酯、苯基乙酯、里哪酯、萜品酯和环己烯酯);水杨酸酯(正戊酯、苯酯、苄酯、酯、甘油酯和二丙二醇酯);肉桂酸衍生物(酯和苄酯,丁基肉桂基丙酮酸酯);二羟基肉桂酸衍生物(7-羟基香豆素、甲基7-羟基香豆素、甲基乙酰基7-羟基香豆素);三羟基肉桂酸衍生物(七叶亭、甲基七叶亭、瑞香素,和葡糖苷,七叶苷和瑞香苷);烃(二苯基丁二烯、1,2-二苯乙烯);二亚苄基丙酮和亚苄基乙酰基苯酮;萘酚磺酸盐(2-萘酚-3,6-二磺酸和2-萘酚-6,8-二磺酸的钠盐);二羟基萘酸及其盐;邻和对-羟基联苯基二磺酸酯;香豆素衍生物(7-羟基、7-甲基,3-苯基);二唑类(2-乙酰基-3-溴代吲唑、苯基苯并唑、甲基萘并噁唑、各种芳基苯并噻唑);奎宁盐(硫酸氢盐、硫酸盐、氯盐、油酸盐和单宁酸盐);羟基-或甲氧基取代的二苯酮;尿酸和Vilouric acid;单宁酸及其衍生物(例如己乙基醚);(butyl carbotol)(6-丙基胡椒基)醚;二苯酮(氧代苯、硫代异苄酮(Sulisobenzone)、二氧代苄酮、苯并间苯二酚、2,2′,4,4′-四羟基二苯酮,2,2′-二羟基-4,4′-二甲氧基二苯酮、八苄酮;4-异丙基二苯甲酰基甲烷;丁基甲氧基二苯甲酰基甲烷;etocrylene;和4-异丙基-二苯甲酰基甲烷。
上述化合物中,优选2-乙基己基-肉桂酸酯,4,4′-叔丁基甲氧基二苯甲酰基-甲烷,2-羟基-4-甲氧基二苯酮,辛基二甲基-对-氨基苯甲酸,双没食子酰基三油酸酯,2,2-二羟基-4-甲氧基二苯酮,乙基-4-(双(羟基丙基))氨基苯甲酸酯,2-乙基己基-2-氰基-3,3-二苯基丙烯酸酯,2-乙基己基水杨酸酯,对-氨基苯甲酸甘油酯,3,3,5-三甲基环己基水杨酸酯,氨茴酸甲酯,对二甲基氨基苯甲酸或氨基苯甲酸酯,对二甲基-氨基-苯甲酸-2-乙基己酯,2-苯基苯并咪唑-5-磺酸,2-(对二甲基氨基苯基)-5-磺基苯并噁唑酸(benzoxazoic acid)及这些化合物的混合物。
本发明组合物中更优选的防晒剂是对-甲氧基肉桂酸2-乙基己酯,丁基甲氧基二苯甲酰基甲烷,2-羟基-4-甲氧基二苯酮,辛基二甲基对氨基苯甲酸及其混合物。
组合物中特别有用的防晒剂如下列专利中公开的那些:1990年6月26日授予Sabatelli的U.S.专利和1991年3月21日授予Sabatelli & Spirnak的U.S.专利4,999,186,本文引入上二篇专利作为参考文献。文中公开的防晒剂在一个分子中同时具有两个明显的发色团部分,它们具有不同的紫外辐射吸收光谱。发色团部分中的一个主要吸收UVB辐射范围,另一个强烈吸收UVA辐射范围。
这类防晒剂中优选的是2,4-二羟基二苯酮的4-N,N-(2-乙基己基)甲基氨基苯甲酸酯;4-羟基二苯甲酰基甲烷的N,N-二-(2-乙基己基)-4-氨基苯甲酸酯;4-羟基二苯甲酰基甲烷的4-N,N-(2-乙基己基)甲基氨基苯甲酸酯;2-羟基-4-(2-羟基乙氧基)二苯酮的4-N,N-(2-乙基己基)甲基氨基苯甲酸;4-(2-羟基乙氧基)二苯甲酰基甲烷的4-N,N-(2-乙基己基)甲基氨基苯甲酸酯;2-羟基-4-(2-羟基乙氧基)二苯酮的N,N-二-(2-乙基己基)-4-氨基苯甲酸酯;和4-(2-羟基乙氧基)二苯甲酰基甲烷的N,N-二-(2-乙基己基)-4-氨基苯甲酸酯以及它们的混合物。
安全、有效量的防晒剂可用在本发明组合物中。防晒剂应与水溶性还原剂相容。组合物优选包括约1%-20%,更优选约2%-10%的防晒剂。确切的量取决于所选择的防晒剂和所需的日光防护因子(Sun ProtectionFactor,SPF)而有所不同。
本发明组合物中还可以加入可改善那些组合物的皮肤实质性(substantivity),特别是那些可提高其耐水洗或耐磨擦特性的物质。提供这种益处的优选的物质是乙烯和丙烯酸的共聚物。包括这种共聚物的组合物公开在1987年5月5日授予Brock的USP 4,663,157中,其被引入本文作为参考。
(2)抗炎剂
在本发明优选的皮肤增白组合物中,包括一种作为活性物质的抗炎剂与水溶性还原剂一起。抗炎剂的添加提高了组合物的皮肤增白性能。消炎剂可提供有效保护、防止UVA辐射(当然它也能提供一定的UVB保护)。抗炎剂的局部使用抑制了皮肤由于长期曝露于UV辐射下而变黑。(参见1989年7月11日授予Bissett、Bush和Chatterjee的USP 4,847,071和1989年7月11日授予Bissett和Chatterjee的USP 4,847,069,本发明引入这两篇专利作为参考)。
本发明组合物中可加入安全、有效量的抗炎剂,优选为组合物约0.1%-10%,更优选约0.5%-5%。由于抗炎剂在性能上明显不同,组合物中使用的抗炎剂的确切量取决于所使用的特定的抗炎剂。
可使用的甾族抗炎剂包括,但不限于,皮质类甾醇(corticosteroid)如氢化可的松,羟基去炎松,α-甲基地塞米松,磷酸地塞米松,倍氯美松双丙酸酯,戊酸氯氟美松酮,丙缩羟强龙,去羟米松,醋酸去氧皮质酮,地塞米松,二氯松,双醋酸二氟松,戊酸氟米松,fluadrenolone,氟二氯松,氟氢可的松,特戊酸二氯美松,醋酸氟轻松(fluosinolone acetonide),氟轻松,氟考丁酯(flucortine butylester),氟考龙,醋酸氟甲叉龙,丙酮缩氟氢羟龙,氯氟舒松,醋酸氢化可的松,氢化可的松丁酸酯,甲基泼尼松龙,醋酸曲安缩松,可的松,去氧可的松,flucetonide,氟氢可的松,difluorosonediacetate,缩氟氢烃龙丙酮化物(fluradrenolone acetonide),6α-甲-11β-羟原酮,amcinafel,amcinafide,倍他米松及其酯,氟强的龙,醋酸氯强的松,氯氟土龙(clocor-telone),clescinolone,二氯松,醋丁二氟龙,氟二氯松,9-去氟肤轻松,丙酮缩氟氢羟龙(fluoromethalone),醋酸甲氟龙,氟强的松龙,氢化可的松戊酸酯,氢化可的松环戊基丙酸酯,氢化松氨酯,甲基强的松,对氟米松,泼尼松龙,泼尼松,倍氯美松二丙酸酯,去炎松以及它们的混合物。优选使用的甾族抗炎剂是氢化可的松。
可用在该组合物中的第二类抗炎剂包括非甾族抗炎剂。包括在该组内的各种化合物是本领域普通技术人员公知的。关于非甾族抗炎剂的化学结构、合成、副作用等的详细内容的公开参考文献可以是标准教本,包括Antiinflammatory and Anti-Rheumatic Drugs(K.D.Rainsford,Vol.I-III,CRCPress,Boca Raton,l985)和
Anti-inflammatory Agents,Chemistry and Pharmacology,1,R.A.Scherrer等人,Academic Press,New York(1974)。
可用在本发明组合物中的非甾族抗炎剂包括(但不限于);
i)昔康类(oxicam);如吡罗昔康,伊索昔康,tenoxicam,噻氧噻嗪和CP-14.304;
ii)水杨酸酯类,如阿司匹林,双水杨酸酯,乙酰水杨酸对乙酰胺苯酯,三水杨酸胆碱镁;safapryn,solprin,双氟尼酸和苯吲柳酸;
iii)乙酸酯衍生物类,如双氯酚酸钠,二氯苯氧苯乙酸,吲哚美辛,舒林酸,托耳米丁,氧乙酸,乙氧茚乙酸,噻庚乙酸,叠氮吲酸,醋炎痛,双苯噻酸,苯酰吡酸钠(zomepiract),环氯茚酮,噁庚乙酸和联苯乙酸;
(iv)灭酸酯类,如甲灭酸,甲氯灭酸,氟灭酸,尼氟灭酸和邻甲氯灭酸;
(v)丙酸衍生物,如布洛芬,萘普生,苯噁洛芬,氟比洛芬,酮基布洛芬,非诺洛芬,芬布芬,吲哚布洛芬,吡洛布洛芬,卡布洛芬,噁丙嗪,普拉洛芬,咪洛布洛芬(miroprofen),苯噁硫丙酸,噻丙吩,阿明洛芬和噻洛芬(酸);和
(vi)吡唑类,如phenybutazone,羟基保泰松,戊烯保泰松,炎爽痛,和三甲保泰松。
非甾族抗炎剂可混合使用,而且还可使用这些抗炎剂的药用盐和酯。例如etofenamate(一种氟芬那酸衍生物)特别适用于局部使用。非甾族抗炎剂中,优选布洛芬、萘普生,氟灭酸,甲灭酸,甲氟灭酸,吡罗昔康和联苯乙酸;最优选布洛芬,萘普生和氟灭酸。
可用在组合物中的另一类抗炎剂是公开在USP 4,708,966(1987年11月24日授予Loomans等人)中的抗炎剂。该专利公开了一类非甾族抗炎组合物,这类抗炎化合物具体包括取代的苯基化合物,特别是取代的2,6-二叔丁基苯酚衍生物。例如,选自下列的化合物;4-(4′-戊炔-3′-酮)-2,6-二叔丁基苯酚;4-(5′-己炔酰基)(hexynoyl)-2,6-二叔丁基苯酚;4-((S)-(-)-3′-甲基-5′-己炔酰基)-2,6-二叔丁基苯酚;4-((R)-(+)-3′-甲基-5′-己炔酰基)-2,6-二叔丁基苯酚和4-(3,3′-二甲氧基丙酰基)-2,6-二叔丁基苯酚可用在本发明的方法中。最优选4-(5′-己炔酰基)-2,6-二叔丁基苯酚。
可用在本发明中的又一类抗炎剂是公开在USP 4,912,248(1990年3月27日授予Mueller)中的那些抗炎剂。在该专利中公开了具体的具有两个或多个手性中心的含2-萘基酯化合物的化合物和非对映体混合物,特别是化合物甲氧萘丙酸酯和甲基萘丙醇酯化合物及其非对映体混合物。例如本发明中可使用选自下列的化合物:(S)-甲氧萘丙酸-(S)-2-丁基酯,(S)-甲氧萘丙酸-(R)-2-丁基酯,丁酸(S)-甲基萘丙醇-(R)-2-甲酯,丁酸(S)-甲氧萘丙醇-(S)-2-甲酯,(S)-甲氧萘丙酸-(S)-丁基酯和(S)-甲氧萘丙酸-(R)-2-丁基酯的非对映体混合物和丁酸(S)-甲基萘丙醇-(R)-甲酯和丁酸(S)-甲基萘丙醇-(S)-2-甲酯的非对映体混合物。
最后,本发明方法中还可使用所谓的“天然”抗炎剂。例如,也可使用小烛树蜡、α-红没药醇、芦荟vera,Manjistha(从Rubia属植物,特别是Rubia Cordifolia中提取),以及Guggal(从Commiphora属植物,特别是Commiphora Mukul中提取)。
另一种优选的可用在本发明的组合物包括一种皮肤增白剂、防晒剂、和一种抗炎剂,它们共同用于皮肤增白,其分别用量如上述。
(3)抗氧化剂/自由基清除剂
在本发明有用的优选的皮肤增白组合物中,与皮肤增白剂一起使用的还包括一种抗氧化剂/自由基消除剂作为一种活性物质。加入抗氧化剂/自由基清除剂提高了组合物的皮肤增白效果。
在本发明组合物中可加入安全和有效量的抗氧化剂/自由基清除剂,优选为组合物的约0.1%-10%,更优选约1%-5%。
可使用的抗氧化剂/自由基清除剂如抗坏血酸(维生素C)及其盐、生育酚(维生素E)、生育酚山梨酸酯、生育酚的其它酯,丁基化的羟基苯甲酸及其盐、6-羟基-2,5,7,8-四甲基苯并二氢吡喃-2-羧酸(市售商品名为Trolox),核酸及其烷基酯,特别是核酸丙酯、尿酸、尿酸盐及其烷基酯、山梨酸及其盐、脂肪酸的抗血酸酯,胺类(例如N,N-二乙基羟基胺、氨基胍)、硫氢基化合物(例如谷胱甘肽)和二羟基富马酸及其盐。
本发明优选的组合物中,组合物包括与皮肤增白剂一起作为活性剂的防晒剂、抗炎剂、和/或抗氧化剂/自由基清除剂中的一种,任意两种或三种都包括。加入两种或所有这三种活性物质与皮肤增白剂一起提高了组合物的皮肤增白效果。
(4)螯合剂
在本发明采用的优选的组合物中,螯合剂作为活性剂与皮肤增白剂一起使用。此处所用的“螯合剂”是指能通过形成配合物除去体系中的金属离子的活性剂,这样可使金属离子不掺入或催化化学反应。螯合剂的加入提高了组合物的皮肤增白效果。
本发明组合物中可加入安全和有效量的螯合剂,优选为组合物重量的约0.1%-10%,更优选约0.1-5%。可用在组合物中的螯合剂公开在Bissett,Bush & Chatterjiee于1990年11月27日申请的美国专利申请系列号619,805(它是1988年10月4日的关国专利申请系列号251,910的继续中请);1990年4月26日Bush & Bissett申请的美国专利申请系列号514,892;以及1991年2月25日Bush,Bissett & Chatterjee申请的美国专利申请系列号657,847;本发明引入所有这些作为参考文献。本发明组合物中优选的螯合剂是糠偶酰二肟(furidioxime)及其衍生物。
在本发明优选的组合物中,组合物包括防晒剂、抗炎剂、抗氧化剂/自由基消除基和/或螯合剂中的一种、任意两种、三种或全部四种,与皮肤增白剂一起作为活性物质。两种、三种或所有这四种活性物质的加入与皮肤增白剂提高了组合物的皮肤增白效果。
(5)视黄质(retinoid)
在本发明优选的组合物中,包括视黄质,优选视黄酸,与皮肤增白剂一起用作活性物质。视黄质的加入增强了组合物的皮肤增白特性。本发明组合物中可加入安全、有效量的视黄质,优选占组合物的约0.001-2%,更优选约0.01-1%。此处所用的“视黄质”包括所有的天然和/或合成的维生素A或视黄醇类化合物的类似物(此类化合物在皮肤中具有维生素A的生物活性)以及这些化合物几何异构体和立体异构体,如全反式视黄酸和13-顺-视黄酸。
在本明优选的组合物中,包括防晒剂、抗炎剂、抗氧化剂/自由基清除剂、螯合剂和/或视黄质中的任意一种、两种、三种、四种和/或所有的五种,与皮肤增白剂一起作为活性物质。加入这些物质中的两种、三种、四种或所有五种与皮肤增白剂一起使用增强了组合物的皮肤增白效果。
(6)其它任选组分
其它任选的组分包括增稠剂如羧基乙烯基聚合物、防腐剂、液体和膏状颜料、收敛剂、pH缓冲剂、香料、防红外剂、两性的固体无定形类脂体、维生素、营养物质和皮肤调理剂。
可用的皮肤调理剂是β-甘草酸及其衍生物、植物提取物、alantoin、胶原蛋白和提取物以及处理后的弹性蛋白纤维。F.哺乳动物皮肤增白的方法
本发明还涉及哺乳动物的皮肤增白方法,包括局部施用本发明的皮肤增白组合物。活性物质的用量和施用频率将取决于施用物体本身已有的皮肤色、皮肤进一步增黑的速率、所需要增白的程度而定。
局部施用组合物中皮肤增白剂的使用量为安全、有效量,通常每次施用约1mg-10mg/cm2皮肤,优选约2mg-8mg/cm2皮肤,更优选约3mg-7mg/cm2皮肤,进一步优选约4mg-5mg/cm2皮肤。施用次数优选在约1天4次至约一星期二次的范围内,更优选约一天三次至隔一天一次、更优选约一天一次至一天二次。需要至少五天的施用后,观察低级动物体上的皮肤增白效果。需要在人身上施用至少一个月后,来观察效果。达到增白效果后,按照需要,减少使用次数和剂量,达到维持水平即可。这种维持量根据个体的不同而不同,但根据需要优选约为原始剂量和/或频率的1/10-1/2,更优选约1/5-1/3。
本发明用于哺乳动物的皮肤增白的方法包括施用本发明的皮肤增白组合物,该组合物还包括安全和有效量的下列物质中的一种或多种:防晒剂、抗炎剂、抗氧化剂/自由基清除剂、螯合剂和/或视黄质。防晒剂的使用量优选为约0.01-0.1mg/cm2皮肤。抗炎剂的使用量优选为约0.005mg-0.5mg,更优选约0.01mg-0.1mg/cm2皮肤。抗氧化剂/自由基消除剂的使用量优选约0.01mg-1.0mg,更优选约0.05mg-0.5mg/cm2皮肤。螯合剂的使用量优选为约0.001mg-1.0mg,更优选约0.01mg-0.5mg,还更优选约0.05mg-0.1mg/cm2皮肤。视黄质的使用量优选为约0.001mg-0.5mg/cm2皮肤,更优选为约0.005-0.1mg/cm2皮肤。皮肤增白剂的使用量优选约为0.001mg-2mg/cm2皮肤/每次施用、更优选约0.01mg-1mg/cm2皮肤/每次施用。G.制备本发明皮肤增白组合物的步骤
本发明的皮肤增白组合物可使用常规方法制备。但是,如果本发明的皮肤增白组合物包括液态晶体,则可按照下列步骤制备该组合物:
(i)在60-100℃,将化妆品中可使用的液态油、脂肪醇、表面活性剂、卵磷脂混合,得到混合物1,和
(ii)将水溶性还原剂、多元醇和水与混合物1混合,此时维持温度为45℃-100℃。
通常情况下,将按照上述步骤(i)和(ii)得到的混合物冷到室温。
可按照常规方法混入其它成分,但是,通常情况下,油溶性成分可在上述步骤(i)中加入,而水溶性成分可在上述步骤(ii)中加入。
液态晶体可通过用偏光显微镜观测其形状而被检测。
H.实施例
下列实施例进一步描述和演示了本发明范围内的实施方案。所给出的实施例只是为了举例说明本发明的目的,并不用来限制本发明,因此对本发明可能做的各种改变将不会脱离本发明的精神和范围。
本发明的组合物1示于表1中。
本发明的组合物2-5示于表2-5中。
制备组合物1的步骤
将甘油三辛酸/癸酸酯(Migyol 812)、十六烷醇、聚氧乙烯(40)单硬脂酸酯和卵磷酯混合在一起,加热到70℃。在搅拌下,加入亚硫酸钠、亚硫酸氢钠、去离子水和甘油,然后将该混合物乳化。将乳化的混合物搅拌下冷却到室温,得到带有液晶的乳液。将该其中具有液晶的乳液与除上述成分外的其它成分混合在一起,得到组合物1。组合物1的各种成分列于表1中。
表1组合物1:具有液晶的乳液成分 用量(重量%)卵磷脂 3.00聚氧乙烯(40)单硬脂酸酯(Myrj 52) 1.00十六烷醇 1.00甘油三辛酸/三癸酸酯(Migyol 812) 15.00D-δ-生育酚 0.10甘油 5.00对羟基苯甲酸丙酯 0.10对羟基苯甲酸甲酯 0.20去离子水 72.13亚硫酸氢钠(Nacalai tesque,Inc.制造) 0.08亚硫酸钠 0.20氢氧化钠 0.59羧基乙烯基聚合物(Carbopol 980) 1.00苯甲醇 0.60
组合物1具有强皮肤增白活性。
表2
组合物2:具有卵磷脂的清洁水(无液态晶体)成分 用量(重量%)变性酒精 5.000聚氧乙烯(20)脱水山梨醇单月桂酸酯(Tween 20) 1.200卵磷脂 0.020去离子水 87.160亚硫酸氢钠(Nacalai tesque,INC.制造) 0.100亚硫酸钠 0.2001,3-丁二醇 4.000甘油 2.000乙二胺四乙酸二钠 0.100对羟基苯甲酸甲酯 0.150柠檬酸酐 0.020柠檬酸钠 0.050
例如,可使用下述方法制备组合物2。
1.在室温(25℃)下,将变性酒精、聚氧乙烯(20)脱水山梨醇单月桂酸酯(Tween 20)和卵磷脂混合、溶解,得到混合物-1。
2.在室温(25℃)下,将去离子水、亚硫酸氢钠、亚硫酸钠、1,3-丁二醇、甘油、乙二胺四乙酸二钠、对羟基苯甲酸甲酯、柠檬酸酐和柠檬酸钠溶解,得到混合物-2。
3.将混合物-1和混合物-2混合在一起,得到组合物2。
表3
组合物3:具有卵磷脂的奶液(无液态晶体)成分 用量(重量%)十甘油基单硬脂酸酯 1.200卵磷脂 0.500胆甾醇 0.050C10-30胆甾醇/羊毛甾醇酯 1.000角鲨烷 3.000甘油三辛酸酯 4.000对羟基苯甲酸丙酯 0.050D-δ-生育醇 0.050去离子水 80.720亚硫酸氢钠(Nacalai tesque,INC.制造) 0.100亚硫酸钠 0.300羧基乙烯基聚合物(Carbopol 941) 0.3001,3-丁二醇 6.000甘油 2.500对羟基苯甲酸甲酯 0.100乙二胺四乙酸二钠 0.050氢氧化钠 0.080
组合物3可按下列方法制得。
1.在80℃的温度下,将十甘油基单硬脂酸酯、卵磷脂、胆甾醇、C10-30胆甾醇/羊毛甾醇酯、角鲨烷、甘油三辛酸酯、对羟基苯甲酸丙酯和D-δ-生育酚混合、溶解,得到混合物-1。
2.在80℃,将去离子水、亚硫酸氢钠、亚硫酸钠、羧基乙烯基聚合物(Carbopol 941)、1,3-丁二醇、甘油、对羟基苯甲酸甲酯、乙二胺四乙酸二钠和氢氧化钠溶解,得到混合物-2。
3.在80℃,将混合物1和混合物-2混合在一起,然后降到室温(25℃),从而得到组合物3。
表4组合物4:具有液晶的奶状洗液成分 用量(重量%)聚氧乙烯(100)硬脂基醚 0.500硬脂酸 0.550卵磷脂 0.800十六烷醇 1.300甘油单羟基硬脂酸酯 0.750棕榈酸鲸蜡酯 3.000凡士林 2.000液态链烷烃 2.000肉豆蔻酸辛基十二烷酯 0.500甲基聚硅氧烷(350CS) 0.300去离子水 84.200亚硫酸氢钠(Nacalai tesque,INC.制造) 0.100亚硫酸钠 0.300羧基乙烯基聚合物(Carbopol 941) 0.050丙烯酸酯/C10-30烷基丙烯酸酯交联聚合物 0.075甘油 3.000对羟基苯甲酸甲酯 0.200对羟基苯甲酸丙酯 0.150乙二胺四乙酸二钠 0.100氢氧化钾 0.125
组合物4可利用下述方法制备。
1.在80℃的温度下,将聚氧乙烯(100)硬脂基醚、硬脂酸、卵磷脂、鲸蜡醇、甘油基单羟基硬脂酸酯、棕榈酸十六酯、凡士林、液态链烷醇、肉豆蔻酸辛基十二烷基酯和甲基聚硅氧烷(350CS)混合、溶解,得到混合物-1。
2.在80℃的温度下,将去离子水、亚硫酸氢钠、亚硫酸钠、羧基乙烯基聚合物(Carbopol 941)、丙烯酸酯/C10-30烷基丙烯酸酯交联聚合物、甘油、对羟基苯甲酸甲酯、对羟基苯甲酸丙酯、乙二胺四乙酸二钠和氢氧化钾溶解,得到混合物-2。
3.在80℃温度下,将混合物-1和混合物-2混合在一起,然后降到室温(25℃),得到组合物4。
表5
组合物5:具有液态晶体的乳膏成分 用量(重量%)硬脂酸 0.250PEG100硬脂酸酯 0.250卵磷脂 1.000十六烷醇 1.800硬脂醇 1.200凡士林 1.500液态链烷烃 2.000棕榈酸异丙酯 1.000甲基聚硅氧烷(350CS) 0.500去离子水 80.690亚硫酸氢钠(Nacalai tesque,INC.制造) 0.100亚硫酸钠 0.300羧基乙烯基聚合物(Carbopol 934) 0.600甘油 8.000对羟基苯甲酸甲酯 0.250对羟基苯甲酸丙酯 0.150乙二胺四乙酸二钠 0.100氢氧化钠 0.310
组合物5可使用下述方法制备。
1.在80℃的温度下,将硬脂酸、PEG 100硬脂酸酯、卵磷脂、十六醇、硬脂醇、凡士林、液态链烷烃、棕榈酸异丙酯和甲基聚硅氧烷(350 CS)混合、溶解,得到混合物-1。
2.将去离子水、亚硫酸氢钠、亚硫酸钠、羧基乙烯基聚合物(Carbopol934)、甘油、对羟基苯甲酸甲酯、对羟基苯甲酸丙酯、乙二胺四乙酸二钠和氢氧化钠在80℃溶解,得到混合物-2。
3.在80℃下,将混合物-1和混合物-2混合在一起,降到室温(25℃)后,得到组合物5。
本发明的组合物与包括氢醌衍生物的对比组合物相比,具有强的哺乳动物的皮肤增白效果。方法例
本实施例讲述了一种使用本发明组合物增白哺乳动物皮肤的方法。
实施例1的组合物每次施用的量为5mg/cm2皮肤,一天施用三次,共施用了一个月。一个月后,观测到强皮肤增白效果。一旦达到所期望的皮肤增白效果后,减少处理限制到一天,维持增白水平。
应该理解本发明叙述的实施例和实施方案只用于演示目的,本领域普通技术人员根据本发明可做的各种改变、均包括在本发明申请的精神和叙述中,并且还将落在所附权利要求的范围内。
Claims (16)
1.皮肤增白化妆组合物,包括:
a)约0.1%-5%重量的至少一种水溶性的还原剂,所述还原剂选自:亚硫酸钠、亚硫酸钾、亚硫酸铵、亚硫酸氢钠、亚硫酸氢钾、亚硫酸氢铵、偏亚硫酸氢钠、偏亚硫酸氢钾、甲酸、草酸以及它们的混合物;和
b)约0.01%-10%重量的卵磷脂;
c)化妆品可用的载体,
其中该组合物基本上不含氢醌或其衍生物。
2.权利要求1的皮肤增白化妆组合物,包括约0.15%-5%重量的水溶性还原剂。
3.权利要求1的皮肤增白化妆组合物,包括约0.2%-5%重量的水溶性还原剂和约0.5%-3%重量的卵磷脂。
4.权利要求3的皮肤增白化妆组合物,其中水溶性还原剂选自:亚硫酸钠、亚硫酸氢钠、偏亚硫酸氢钠,以及它们的混合物。
5.权利要求1的皮肤增白化妆组合物,包括:
a)约0.1%-5%重量的至少一种水溶性还原剂,所述还原剂选自:亚硫酸钠、亚硫酸钾、亚硫酸铵、亚硫酸氢钠、亚硫酸氢钾、亚硫酸氢铵、偏亚硫酸氢钠、偏亚硫酸氢钾、甲酸、草酸以及它们的混合物;
b)约0.01%-10%重量的卵磷脂;
c)约1%-50%重量的化妆品可用的液态油;
d)约0.1%-20%重量的多元醇;
e)约0.1%-20%重量的固体脂肪醇;
f)约0.1%-10%重量的表面活性剂;和
g)约40%-90%重量的水;
其中该组合物基本不含氢醌或其衍生物,并且上述组分(a)、(b)、(c)、(d)、(e)、(f)和(g)中的至少一部分形成液态晶体。
6.权利要求5的皮肤增白化妆组合物,按组合物的重量计,包括:
a)约0.15%-5%的水溶性还原剂;
b)约0.1%-3%的卵磷脂;
c)约3%-25%的化妆品可用的液体油;
d)约0.1%-10%的多元醇;
e)约0.1%-5%的固体脂肪醇;
f)约0.1%-3%的表面活性剂;和
g)约40%-90%组合物重量的水。
7.权利要求6的皮肤增白化妆组合物,其中所述还原剂选自:亚硫酸钠、亚硫酸氢钠、偏亚硫酸氢钠以及它们的混合物。
8.权利要求6的皮肤增白化妆组合物,其中所述化妆品可用的液体油是甘油三酯。
9.权利要求6的皮肤增白化妆组合物,其中所述化妆品可用的液体油是甘油三辛酸/癸酸酯。
10.权利要求6的皮肤增白化妆组合物,其中所述多元醇是甘油。
11.权利要求6的皮肤增白化妆组合物,其中所述固体脂肪醇是十六烷醇。
12.权利要求6的皮肤增白化妆组合物,其中所述组合物是乳液。
13.哺乳动物皮肤增白的美容方法,包括给需要皮肤增白的人的皮肤局部施用权利要求1的化妆组合物。
14.权利要求13的方法,包括给需要皮肤增白的人的皮肤局部施用权利要求5的化妆组合物。
15.制备皮肤增白化妆组合物的方法,包括下列步骤:
(i)在60℃-100℃混合
(a)约1%-50%重量的化妆品可用的液体油,
(b)约0.1%-20%重量的固体脂肪醇,
(c)约0.1%-10%重量的表面活性剂,和
(d)约0.01%-10%重量的卵磷脂,
得到混合物1,并且
(ii)将下列组分与混合物1混合在一起:
(e)约0.1%-5%重量的水溶性还原剂,
(f)约0.1-20%重量的多元醇,和
(g)约40%-90%重量的水,
此时维持温度为45℃-100℃;
其中该组合物基本不含氢醌或其衍生物,并且上述组分(a)、(b)、(c)、(d)、(e)、(f)和(g)中的至少一部分形成液态晶体。
16.根据权利要求15所述的制备皮肤增白化妆品组合物的方法,其中所述水溶性还原剂选自:亚硫酸钠、亚硫酸钾、亚硫酸铵、亚硫酸氢钠、亚硫酸氢钾、亚硫酸氢铵、偏亚硫酸氢钠、偏亚硫酸氢钾、甲酸、草酸,以及它们的混合物。
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EP0404162A1 (en) * | 1989-06-23 | 1990-12-27 | Sansho Seiyaku Co., Ltd. | Composition for treating pigmentation |
EP0419901A1 (en) * | 1989-09-14 | 1991-04-03 | Sansho Seiyaku Co., Ltd. | Endermic preparation for external application |
WO1996014055A1 (en) * | 1994-11-04 | 1996-05-17 | The Procter & Gamble Company | Buffered emulsion compositions containing actives subject to acid or base hydrolysis |
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