CN101272775A - 包含羟基脂肪酸的化妆品组合物 - Google Patents
包含羟基脂肪酸的化妆品组合物 Download PDFInfo
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- CN101272775A CN101272775A CNA2006800351938A CN200680035193A CN101272775A CN 101272775 A CN101272775 A CN 101272775A CN A2006800351938 A CNA2006800351938 A CN A2006800351938A CN 200680035193 A CN200680035193 A CN 200680035193A CN 101272775 A CN101272775 A CN 101272775A
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- retinoid
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Abstract
本发明涉及新颖的化妆品或药物组合物。更特别地,本发明涉及下述化妆品或药物组合物,其用于治疗或预防由健康皮肤的生理自身稳态负向发展所引起的任何症状,以及促进头发生长和防止脱发。
Description
本发明涉及新颖的化妆品或药物组合物。更特别地,本发明涉及下述化妆品或药物组合物,其用于治疗或预防由健康皮肤的生理自身稳态负向发展所引起的任何症状,以及促进头发生长和防止脱发。
因此,一方面,本发明涉及下述化妆品或药物组合物,其包含:含有6到18个碳原子的脂肪酸,所述脂肪酸带有一个或两个羟基、烷氧基(优选甲氧基或乙氧基)、C2-C4酰基保护的氨基(优选C2)或氧代基,优选在位置C6和C12之间;或这类酸的盐、酯或酰胺,或这些酸的混合物;以及常规用于化妆品或药物组合物中的载剂。
所述酯或酰胺优选地是烷基酯或烷基酰胺,其中术语“烷基”包括直链以及支链的烷基基团,即“C1-4-烷基”包括直链的C1-4-烷基(甲基、乙基、正丙基、正丁基)以及支链的C3-4-烷基(异丙基、异丁基、叔丁基)。
所述盐可以通过任何化妆品可接受的阳离子形成,所述可接受的阳离子意味着对皮肤无毒的和/或不引起变应性反应的任何金属阳离子以及有机阳离子。这类阳离子的例子是铵盐和烷基铵盐,碱性阳离子(如钠离子和钾离子)和碱土金属阳离子(如钙和镁离子)。
在本发明的一个实施方案中,脂肪族脂肪酸是饱和的直链脂肪酸或ω-支链脂肪酸,其优选地具有6到18个碳原子。在另一实施方案中,脂肪族脂肪酸是具有6到18个碳原子的饱和的直链或ω-支链脂肪酸,并在位置C6和C12之间被取代,优选地被羟基取代。一种特别优选的脂肪酸是9-羟基硬脂酸。
另一方面,本发明涉及下述化妆品或药物组合物,其包含具有上文给出的定义和优选级的脂肪酸或盐、酯或酰胺,和类视黄醇。
用于本发明的类视黄醇为例如视黄酸或视黄醇和同分异构体(例如其9-、11-或13-顺式同分异构体)及其衍生物,所述衍生物包括视黄酯,如醋酸酯、苯基丁酸酯、丙酸酯、月桂酸酯、棕榈酸酯、油酸酯、亚油酸酯;或视黄基烷基碳酸酯;或醚,如视黄氧三甲基甲硅烷(retinoxytrimethylsilane);或(全反式)视黄醛或其缩醛;或视黄酸或其酰胺,如甲氧基PEG-12视黄酰胺(retinamide)(″PEG-12″=-(CH2-CH2-O-)12)。
更特别地,本发明涉及化妆品或药物组合物,其包含至少一种具有上文给出的定义和优选级的脂肪酸或其盐、酯或酰胺和可选的一种类视黄醇,所述化妆品或药物组合物用于治疗或预防由健康皮肤的生理自身稳态负向发展所引起的症状,以及用于促进头发生长和防止脱发。
治疗或预防由健康皮肤的生理自身稳态负向发展所引起的症状包括治疗或预防皱纹或干性皮肤或敏感性皮肤、增厚表皮、抑制皮肤细胞的衰老、预防或治疗光损伤(photodamage)、预防或治疗氧化应激现象、预防或治疗橘皮组织、预防和治疗神经酰胺和脂质合成紊乱、预防过量的皮脂生产、降低皮肤中的基质金属蛋白酶或其它蛋白酶的活性、治疗和预防炎性皮肤病,包括痤疮(=抗痤疮)、异位性湿疹(atopic eczema)、多形性光疹(polymorphic light eruption)、银屑病和白癜风(vertiligo)。
还在另一方面,本发明涉及一种方法,所述方法用于治疗或预防由健康皮肤的生理自身稳态负向发展所引起的症状,以及治疗或预防发痒或受刺激的皮肤和促进头发生长和防止脱发,所述方法提供了:向需要这类治疗或预防的人局部施用有效用量的具有上文给出的定义和优选级的脂肪酸或盐、酯或酰胺,可选地并优选地与类视黄醇组合施用,优选地以本发明的化妆品或药物组合物的形式施用。
本发明优选的一个实施方案是治疗或预防皱纹或人干性皮肤或敏感性皮肤、促进头发生长、防止脱发和增厚表皮的方法,所述方法包括步骤:向需要这类治疗或预防的人局部施用有效用量的具有上文给出的定义和优选级的脂肪酸或盐、酯或酰胺,可选地并优选地与类视黄醇组合施用。
本发明的另一目的是用于预防和治疗色素沉着疾病和/或用于提供均匀肤色的方法,所述方法包括步骤:向需要这类预防或治疗的人局部施用有效用量的上文定义的本发明的组合物,其中所述组合物含有类视黄醇。
本发明的另一目的是用于强化色素沉着的方法,所述方法包括步骤:向需要这类强化的人局部施用有效用量的上文定义的本发明的组合物,并局部施用美黑活性成分,其中所述美黑活性成分可以在施用有效用量的本发明组合物之前、之后或同时被施用,其中这类组合物中基本不含任何类视黄醇。
术语“有效用量”是指获得生理效应必需的用量。可以通过单次应用给药或重复应用来达成所述生理效应。当然,所施用的剂量可以根据已知的因素变化并由本领域技术人员调节,所述已知的因素为例如特定组合物(其包含具有上文定义和优选级的脂肪酸或盐、酯或酰胺,可选地与类视黄醇组合)的生理学性能及其施用模式和途径;受者的年龄、健康和体重;症状的性质和程度;并存的治疗种类;治疗频率;和所期望的效果。
在另一实施方案中,本发明的组合物可以用于治疗或预防上文定义的由健康皮肤的生理自身稳态负向发展所引起的症状,以及用于促进头发生长和防止脱发。本发明的组合物还可以用于治疗或预防发痒或受刺激的皮肤,或用于强化色素沉着(然而,仅当不存在类视黄醇但存在美黑活性成分时为后者)。然而,当类视黄醇存在于本发明的组合物中时,所述组合物可用于预防或治疗色素沉着疾病和/或用于提供均匀的肤色,因为上文定义的脂肪酸或其盐、酯或酰胺对类视黄醇的辅助(boosting)可以导致色素脱失。
优选地,本发明的组合物被用于治疗或预防皱纹或干性皮肤或敏感性皮肤,用于促进头发生长,用于防止脱发,用于增厚表皮,(如果存在类视黄醇)用于预防或治疗色素沉着疾病和/或提供均匀的肤色,和/或(如果不存在类视黄醇,存在美黑活性成分)用于强化色素沉着。因此,本发明的组合物(即具有上文定义的定义和优选级的脂肪酸或其盐、酯或酰胺)可通过增强美黑活性成分的效应来强化色素沉着。
典型地,尽管本发明的化妆品或药物组合物含有上文定义的一种脂肪酸,但是本发明不限于特定的方面,且可以存在两种或更多上文定义的脂肪酸或其盐、酯或酰胺。如上文所述,可额外存在类视黄醇,提供附加的或协同的化妆品效应,即改进或预防由健康皮肤的生理自身稳态负向发展引起的症状以及促进头发生长和防止脱发。此外,可以存在两种或更多种类视黄醇。如果类视黄醇存在于本发明的组合物中,则具有上文给出的定义和优选级的脂肪酸或其盐、酯或酰胺与类视黄醇的比例以重量计适当地为约1000∶1到1∶1000,更优选地从约100∶1到1∶100,特别是从约30∶1到1∶30。上文定义的脂肪酸或其盐、酯或酰胺也显示与已经存在于人皮肤中的类视黄醇的附加或协同效应。
在本发明提供的组合物中,具有上文给出的定义和优选级的脂肪酸或其盐、酯或酰胺的用量适当地占总组合物重量的从约0.0001%到约50%,优选地从约0.001%到约20%。更优选地,如上文定义的脂肪酸以按重量计约0.01%到按重量计约1%的用量,最优选地以按重量计约0.5%的用量包含在所述组合物中。
如果存在类视黄醇或其衍生物,则后者的用量适当地以组合物的总量为基础从以重量计约0.0001%到约50%,优选地以重量计从约0.001%到约20%,最优选地以按重量计约0.01%到约1%的用量,特别是按重量计约0.1%的用量。根据本发明优选的是下述组合物,所述组合物以其总量为基础,包含按重量计约0.5%用量的脂肪酸或其盐、酯或酰胺(其具有上文给出的定义和优选级)和按重量计约0.1%用量的类视黄醇或其衍生物。
本文使用术语“化妆品组合物”是指例如用于护理人皮肤的局部组合物,也参阅Rompp Lexikon Chemie,10th edition 1997,Georg Thieme VerlagStuttgart,New York中标题″Kosmetika″。
关于局部(化妆品或药物)组合物的种类和局部组合物以及其它合适添加剂的制备,可以参考相关文献,例如参考Novak G.A.,Diekosmetischen Praparate-Band 2,Die kosmetischen Praparate-Rezeptur,Rohstoffe,wissenschaftliche Grundlagen(Verlag fur Chem.Industrie H.Ziolkowski KG,Augsburg)。
要应用于皮肤的本发明的化妆品或药物组合物的用量取决于所述组合物中活性成分的浓度和所期望的化妆品或药物效果。例如,可以进行应用使得乳霜被应用于皮肤。乳霜通常以2mg乳霜/cm2皮肤的用量被应用。然而,被应用于皮肤的组合物的用量不是关健的,如果使用某用量的组合物不能达到所期望的效果,则可以使用更高浓度的活性成分,例如通过使用更多的组合物或通过使用含有更多活性成分的组合物。
本发明的化妆品或药物组合物优选地每天至少使用一次,例如每天两次或三次。通常消耗至少两周才达到所期望的效果。然而,完全最大化所期望的效果可耗时若干周或甚至数月。
本发明的组合物含有脂肪酸或其盐、酯或酰胺(其具有上文定义的定义和优选级)与化妆品和药物可接受的赋形剂或稀释剂。如果没有其它说明,下文提到的赋形剂、添加剂、稀释剂等适用于化妆品组合物。
如果没有其它说明,在本申请中份和百分比是按重量计的,并以组合物的总重量为基础。
优选地,本发明的化妆品和药物组合物是溶剂或脂肪物质中悬浮液或分散体系形式的局部组合物,或者是乳剂或微乳剂(特别是O/W或W/O类型、O/W/O或W/O/W类型的)、PET-乳剂、复合型乳剂、bikering乳剂、水凝胶、醇凝胶、脂凝胶、单相或多相溶液或小泡分散体系(vesicular dispersion)的形式和其它常见组合物,所述组合物也可通过笔、作为面膜或作为喷雾应用。乳剂也可以含有阴离子的、非离子的、阳离子的或两性的表面活性剂。
优选的本发明组合物是护肤制剂、护发制剂、装饰性制剂(decorativepreparation)、遮光制剂和功能性制剂。
护肤制剂的例子特别是身体油、身体乳液、身体凝胶、修护霜、护肤软膏、剃须制剂(如剃须泡沫或凝胶)、爽肤粉(如爽身粉)、保湿凝胶、保湿喷雾、活肤身体喷雾、橘皮组织凝胶、抗痤疮制剂和去死皮制剂。
护发制剂的例子为例如香波形式的洗发制剂、护发素、护发制剂(例如修护制剂)、预处理制剂、生发油、造型霜、造型凝胶、润发油、洗发剂、修护包、强化头发修护、头发拉直制剂、液体整发制剂、发用泡沫、发用喷雾和发用光亮剂(lacquer)、烫发剂、发用凝胶、发用固定剂和染发剂或漂白剂。
装饰性制剂的例子特别是唇膏、眼影、睫毛膏、干的和湿的化妆品、腮红、散粉和美黑乳液。
功能性制剂的例子是含有活性成分(例如但不限于激素制剂、维生素制剂、植物提取物制剂、抗衰老制剂和抗微生物(抗菌或抗真菌)制剂)的化妆品或药物组合物。
本发明的化妆品组合物可以是液体、乳液、增稠的乳液、凝胶、霜、乳、软膏、粉末、化妆品或固体管棒的形式提供,可任选地被包装为气溶胶,可以以摩丝(如气溶胶摩丝)、泡沫或喷雾泡沫、喷雾、棒、凝胶、硬膏剂、粉末、清洁剂、肥皂或气溶胶或纸巾(wipe)的形式提供。
本发明的组合物也可以含有常见的化妆品或药物佐剂和添加剂,例如防腐剂/抗氧化剂,脂肪物质/油,水,有机溶剂,硅酮,增稠剂,软化剂,乳化剂,遮光剂,消泡剂,增湿剂,香料,表面活性剂,填充剂,遮蔽剂,阴离子的、阳离子的、非离子的或两性的多聚物或其混合物,抛射剂,酸化或碱化剂,染料,着色剂,色素或纳米色素(例如适用于通过物理阻隔紫外辐射来提供遮光效应的那些),或通常配制进化妆品或药物中的任何其它成分。
通常优选额外量的抗氧化剂/防腐剂。根据本发明,能够使用通常被配制进化妆品或药物中的所有已知的抗氧化剂。特别优选的是选自以下的抗氧化剂:氨基酸(例如甘氨酸、组氨酸、酪氨酸、色氨酸)及其衍生物,咪唑(例如咪唑丙烯酸(urocanic acid))及衍生物,肽例如D,L-肌肽、D-肌肽、L-肌肽和衍生物(例如鹅肌肽),类胡萝卜素,胡萝卜素(例如α-胡萝卜素、β-胡萝卜素、番茄红素),绿原酸和衍生物,脂酮酸和衍生物(例如二氢脂酮酸),金硫葡萄糖(aurothioglucose),丙基硫脲嘧啶和其它巯基化合物(例如硫氧还蛋白(thioredoxine)、谷胱甘肽、半胱氨酸、胱氨酸、胱胺(cystamine)及其糖基、N-乙酰基、甲基、乙基、丙基、戊基、丁基和月桂基、棕榈酰、油酰基、γ-亚麻酰基(γ-linoleyl-)、胆固醇基(cholesteryl-)和甘油酯)及其盐,硫二丙酸二月桂酯(dilaurylthiodipropionate),硫二丙酰双十八酯,硫二丙酸及其衍生物(酯、醚、肽、脂、核苷酸、核苷和盐)以及非常低的相容剂量(例如pmol到μmol/kg)的亚砜亚胺(sulfoximine)化合物(例如丁硫氨酸亚砜亚胺,高半胱氨酸亚砜胺,丁硫氨酸亚砜,戊、己、庚硫氨酸亚砜亚胺),额外的(金属)螯合剂(例如α-羟脂肪酸、棕榈酸、肌醇六磷酸、乳铁蛋白),β-羟酸(例如柠檬酸、乳酸、苹果酸),腐殖酸(huminic acid),没食子酸,没食子提取物,胆红素,胆绿素,EDTA,EGTA及其衍生物,不饱和脂肪酸及其衍生物(例如γ-亚油酸,亚油酸,油酸),叶酸及其衍生物,泛醌和泛醇及其衍生物,维生素C和衍生物(例如棕榈酸抗坏血酸酯和四异棕榈酸抗坏血酸酯(ascorbyltetraisopalmitate)和抗坏血酸磷酸镁(Mg-ascorbylphosphate),抗坏血酸磷酸钠,醋酸抗坏血酸钠,生育酚和衍生物(例如维生素E醋酸酯),天然或合成的维生素E的混合物,维生素A和衍生物(维生素A棕榈酸酯和醋酸酯)以及苯甲酸松柏基酯(coniferylbenzoat),芸香亭酸(rutinic acid)和衍生物,α-糖基芦丁(α-glycosylrutin),阿魏酸,亚糠基葡萄糖醇(furfurylidenglucitol),肌肽,丁基羟甲苯,丁基羟基茴香醚,三羟基苯丁酮,尿素及其衍生物,甘露糖和衍生物,锌和衍生物(例如ZnO;ZnSO4),硒和衍生物(例如硒代蛋氨酸),芪和衍生物(例如氧化芪,反式氧化芪)以及所述活性成分的合适的衍生物(盐、酯、醚、糖、核苷酸、核苷、肽和脂)。一种或多种防腐剂/抗氧化剂可以以占本发明组合物总重的约0.01wt.%到约10wt.%的量存在。优选一种或多种防腐剂/抗氧化剂以约0.1wt.%到约1wt.%的量存在。
典型地,局部配方也可含有表面活性成分如乳化剂、增溶剂等。乳化剂使得两种或更多不混溶的液体均相组合。此外,乳化剂起到稳定组合物的作用。本发明中可使用乳化剂以形成O/W、W/O、O/W/O乳剂/微乳剂,所述乳化剂包括脱水山梨糖醇油酸酯、脱水山梨糖醇倍半油酸酯、脱水山梨糖醇异硬脂酸酯、脱水山梨糖醇三油酸酯、聚甘油-3-二异硬脂酸酯(polyglyceryl-3-diisostearate)、油酸/异硬脂酸的聚甘油酯、聚甘油-6己蓖麻油酸酯(polyglyceryl-6 hexaricinolate)、聚甘油-4-油酸酯、聚甘油-4-油酸酯/PEG-8丙二醇可可酸酯、油酰胺DEA、TEA肉豆蔻酸酯(TEAmyristate)、TEA硬脂酸酯、硬脂酸镁、硬脂酸钠、月桂酸钾、蓖麻醇酸钾、可可酸钠、牛脂酸钠、蓖麻油酸钾(potassium castorate)、油酸钠及其混合物。其它合适的乳化剂为磷酸酯及其盐,例如磷酸十六烷基酯(A)、磷酸二乙醇胺十六烷基酯()、十六烷基磷酸钾(potassium cetyl phosphate)(K)、甘油油酸磷酸钠(sodiumglyceryl oleate phosphate)、氢化的植物甘油磷酸酯(hydrogenatedvegetable glyceride phosphates)及其混合物。此外,一种或多种合成的聚合物可用作乳化剂。例如,PVP二十碳烯共聚物、丙烯酸酯/丙烯酸C10-C30烷基酯交叉聚合物、丙烯酸酯/硬脂醇聚醚-20甲基丙烯酸酯共聚物(acrylates/steareth methacrylate copolymer)、PEG-22/十二烷基二醇共聚物、PEG-45/十二烷基二醇共聚物及其混合物。优选的乳化剂是磷酸十六烷基酯(A)、磷酸二乙醇胺十六烷基酯()、十六烷基磷酸钾(potassium cetyl phosphate)(K)、PVP二十碳烯共聚物、丙烯酸酯丙烯酸C10-C30烷基酯交叉聚合物、PEG-20脱水山梨糖醇异硬脂酸酯、脱水山梨糖醇异硬脂酸酯及其混合物。所述一种或多种乳化剂以占本发明组合物总重的约0.01wt.%到约20wt.%的总量存在。优选使用约0.1wt.%到约10wt.%的乳化剂。
局部组合物的脂肪相有利地选自:
矿物油和矿物蜡;
油,例如甘油三癸酸酯或甘油三辛酸酯和蓖麻油;
油或蜡及其它天然或合成油,在优选的实施方案中为脂肪酸与醇(例如异丙醇、丙二醇或丙三醇)的酯,或脂肪醇与羧酸或脂肪酸的酯;
苯甲酸烷基酯;和/或
硅油,例如二甲基聚硅氧烷、二乙基聚硅氧烷、二苯基聚硅氧烷、环甲硅油及其混合物。
可被掺入本发明乳剂、微乳剂、油凝胶、水分散剂或脂分散剂的油相中的示例性脂肪物质有利地选自:带有3到30个碳原子的、饱和的和/或不饱和的、线性或分支的烷基羧酸与带有3到30个碳原子的、饱和的和/或不饱和的、线性和/或分支的醇的酯;芳香族羧酸和带有3到30个碳原子的饱和和/或未饱和的、线性或分支的醇的酯。这类酯可有利的选自棕榈酸辛酯、可可酸辛酯、异硬脂酸辛酯、肉豆蔻酸辛基十二烷酯、异壬酸十六烷基酯、肉豆蔻酸异丙酯、棕榈酸异丙酯、硬脂酸异丙酯、油酸异丙酯、硬脂酸正丁酯、月桂酸正己酯、油酸正癸酯、硬脂酸异辛酯、硬脂酸异壬酯、异壬酸异壬酯、棕榈酸2-乙基己酯、月桂酸2-乙基己酯、硬脂酸2-己基癸酯、棕榈酸2-辛基十二烷基酯、庚酸十八烷基酯、油酸油基酯(oleyloleate)、芥酸油基酯(oleylerucate)、油酸瓢儿菜酯(erucyloleate)、瓢儿菜酸瓢儿菜基酯、油酸十三烷基酯、偏苯三酸十三烷基酯,以及来自这些酯的合成的、半合成的或天然的混合物,例如霍霍巴油(jojoba oil)。
适用于本发明局部组合物的其它脂肪成分包括极性油,例如卵磷脂和甘油三脂肪酸酯,即具有8到24个碳原子(优选12到18个碳原子)的饱和的和/或不饱和的、直链的或分支的羧酸甘油三酯,其中所述甘油三脂肪酸酯优选地选自合成的、半合成的或天然的油(例如可可甘油酯(cocoglyceride)、橄榄油、葵花子油、大豆油、花生油、菜籽油、甜杏仁油、棕榈油、椰子油、蓖麻油、氢化的蓖麻油、小麦油、葡萄籽油、澳洲坚果油等等);非极性的油例如线性的和/或分支的烃和蜡,例如矿物油、凡士林(矿脂);石蜡油、角鲨烷(squalan)和角鲨烯(squalen)、聚烯烃、氢化的聚异丁烯和异十六烷,优选的聚烯烃是聚癸烯;二烷基醚,例如二辛醚(dicaprylylether);线性或环状的硅油,例如优选环甲基硅氧烷(cyclomethicone);八甲基环四硅氧烷、十六烷基二甲基硅氧烷(cetyldimethicone)、六甲基环三硅氧烷、聚二甲基硅氧烷、聚(甲苯基硅氧烷)及其混合物。
可有利地掺入本发明局部组合物的其它脂肪成分为异二十烷;新戊二醇二庚酸酯;丙二醇二辛酸酯/二癸酸酯;辛酸-/癸酸-/二甘油琥珀酸酯(caprylic-/capric-/diglycerylsuccinate);丁二醇辛酸酯/癸酸酯;乳酸C12-13烷基酯;酒石酸二(C12-13烷基)酯;三异硬脂精(triisostearin);二季戊四醇六辛酸酯/六癸酸酯;丙二醇单异硬脂酸酯;三辛酸甘油酯;二甲基异山梨醇酯(dimethylisosorbid)。特别优选的是使用苯甲酸C12-15烷基酯和异硬脂酸2-乙基己基酯的混合物,苯甲酸C12-15烷基酯和异壬酸十三烷基酯的混合物以及苯甲酸C12-15烷基酯、异硬脂酸2-乙基己基酯和异壬酸十三烷基酯的混合物。特别有利的是使用苯甲酸C12-15烷基酯和2-乙基己基酯的混合物,苯甲酸C12-15烷基酯和异壬酸十三烷基酯的混合物以及苯甲酸C12-15烷基酯、异硬脂酸2-乙基己基酯和异壬酸十三烷基酯的混合物。
本发明组合物的油相也可含有天然的植物蜡或动物蜡,例如蜂蜡、中国蜡、熊蜂蜡(bumblebee wax)和其它昆虫蜡及牛油树脂和可可脂。
可向本发明的局部组合物中掺入湿润剂(moisturizing agent)以维持皮肤水分或给皮肤补水。通过提供保护层来阻止水分从皮肤蒸发的湿润剂称作润肤剂(emollient)。
润肤剂还在皮肤表面提供软化或舒缓效应,其通常被认为对局部使用来说是安全的。优选的润肤剂包括矿物油,羊毛脂,凡士林,甘油癸酸/辛酸三酯,胆固醇,硅酮例如二甲硅油、环甲硅油,杏仁油,霍霍巴油,鳄梨油,蓖麻油,葵花子油,椰子油,葡萄籽油,可可脂,橄榄油,芦荟提取物,脂肪酸如油酸和硬脂酸,脂肪醇如鲸蜡醇和十六醇(ENJAY),己二酸二异丙基酯,C9-C15醇的苯甲酸酯和羟基苯甲酸酯,异壬基异壬酸酯,醚例如聚氧丙烯丁基醚和聚氧丙烯十六烷基醚和苯甲酸C2-C15烷基酯,及其混合物。最优选的润肤剂是羟基苯甲酸酯、真芦荟(aloe vera)、苯甲酸C12-15烷基酯及其混合物。润肤剂以占组合物总重量的约1wt.%到约20wt.%的剂量存在。优选的润肤剂量为从约2wt.%到约15wt.%,最优选从约4wt.%到约10wt.%。
与水结合从而将其留在皮肤表面的湿润剂称作润湿剂(humectant)。合适的润湿剂可被掺入本发明的局部组合物中,所述润湿剂例如甘油、聚丙二醇、聚乙二醇、乳酸、吡咯烷酮含碳酸、尿素、磷脂、胶原、弹性蛋白、神经酰胺、卵磷脂山梨糖醇、PEG-4及其混合物。其它的合适湿润剂为水溶性和/或可膨大的和/或水凝胶性的多糖家族的聚合物湿润剂,例如透明质酸、壳聚糖和/或可从SOLABIA S获得的1000(CAS-Nr.178463-23-5)的富含岩藻糖的多糖。一种或多种润湿剂可选地以占本发明组合物从约0.5wt.%到约8wt.%,优选地从约1wt.%到约5wt.%的剂量存在。
本发明优选的局部组合物的水相可含有常用的化妆品或药物添加物例如醇,特别是低级醇(优选乙醇和/或异丙醇),低级二醇或多元醇及其醚,优选丙二醇,丙三醇,乙二醇,乙二醇单乙基或单丁基醚,丙二醇单甲基或单乙基或单丁基醚,二甘醇单甲基或单乙基醚和类似产品;聚合物;泡沫稳定剂;电解质和特别地一种或多种增稠剂。
可用于本发明配方中以协助产生产品一致性的合适增稠剂包括:卡波姆、二氧化硅、硅酸镁和/或硅酸铝、蜂蜡、硬脂酸、硬脂醇多糖及其衍生物(例如黄原胶、羟丙基纤维素、聚丙烯酰胺)、丙烯酸酯共聚物,优选卡波姆(例如单独的980、981、1382、2984、5984型或其混合物)。
可包括在本发明组合物中用以中和例如乳化剂或泡沫增加剂/稳定剂的成分的合适中和剂,包括但不限于碱性氢氧化物,例如氢氧化钠和氢氧化钾;有机碱如二乙醇胺(DEA)、三乙醇胺(TEA)、氨甲基丙醇及其混合物;氨基酸,例如精氨酸和赖氨酸和任意前述物质的任意组合。中和剂可以以约0.01wt.%到约8wt.%,优选地1wt.%到约5wt.%的剂量存在于本发明的组合物中。
向本发明组合物中添加电解质以改变疏水乳化剂的性能可以是必需的。因此,本发明的乳剂/微乳剂可优选地含有一种或若干种包括阴离子的盐的电解质,包括氯化物、硫酸盐、碳酸盐、硼酸盐或铝酸盐,但不仅限于此。其它合适的电解质可以以有机阴离子为基础,例如(但不限于)乳酸盐、乙酸盐、苯甲酸盐、丙酸盐、酒石酸盐和柠檬酸盐。对阳离子而言,优选地选择铵、烷基铵、碱金属或碱土金属、镁离子、铁离子或锌离子。特别优选的盐为氯化钾和氯化钠、硫酸镁、硫酸锌及其混合物。电解质可以以约0.01wt.%到约8wt.%的剂量存在于本发明的组合物中。
根据本发明制备本发明组合物时,活性成分可以以被封装的形式(例如脂质体形式)使用。优选地用卵磷脂形成脂质体,添加或不添加固醇或植物固醇。活性成分的封装可以是单独的或与其它活性成分一起的。可能只封装脂肪酸或其盐、酯或酰胺(其具有上文定义的优选级和定义)或只封装类视黄醇,但是也可能将两种成分封装在一起或封装在独立的胶囊中。
其它实施方案包括固体或半固体的胶囊,其有助于保护类视黄醇免于降解或用于受控的递送。所述胶囊可单独或与脂肪酸或其盐、酯或酰胺
(其具有上文定义的优选级和定义)一起含有类视黄醇。合适的封装技术例如描述于WO 0180823、WO 9903450、WO 9317784或Fragrance Journal(2001),29(2),83-90中。
本发明的组合物也可含有一种或多种额外的药物或化妆品活性成分,特别是用于预防或减少痤疮、皱纹、纹理、萎缩、炎症的活性成分,以及局部麻醉剂、人工美黑剂和加速剂(accelerators)、抗微生物剂、抗真菌剂和滤光添加剂,而不仅限于此。
这类成分的例子是肽(例如MatrixylTM[五肽衍生物])、寡肽、基于蜡的合成肽(例如棕榈酸辛酯和山萮酸甲酯(tribehenin)和山梨聚糖异硬脂酸酯和棕榈酰基寡肽)、甘油、脲、胍(例如氨基胍);维生素及其衍生物,例如维生素C(抗坏血酸)、维生素A(例如类视黄醇衍生物,如棕榈酸视黄酯或丙酸视黄酯)、维生素E(例如醋酸生育酚)、维生素B3(例如烟酰胺)和维生素B5(例如泛醇)、维生素B6和维生素B12、生物素、叶酸;抗痤疮活性成分或药物(例如间苯二酚、水杨酸等等);抗氧化剂(例如植物固醇、硫辛酸);黄酮类(例如异黄酮、植物雌激素);皮肤舒缓和愈合剂,例如芦荟提取物、尿囊素等等;适用于美容目的的试剂,例如精油,香料,skin sensates,遮光剂,芳香化合物(例如丁香油、薄荷脑、樟脑、桉叶油和丁香酚),脱皮活性剂,羟酸例如AHA酸,自由基捕获剂,法尼醇,抗真菌活性成分(特别是没药醇),烷基二醇如1,2-戊二醇、己二醇或1,2-辛二醇、植醇,多元醇如植烷三醇,神经酰胺和假神经酰胺,氨基酸,蛋白质水解产物,多不饱和脂肪酸,植物提取物如玻璃酸酶,DNA或RNA及其片段产物,碳水化合物,共轭的脂肪酸,肉碱,肌肽,biochinonen,六氢番茄红素,八氢番茄红素及其相应的衍生物。
另外,本发明的化妆品和药物局部组合物可以含有UV遮蔽剂(UV-滤光剂)。额外的UV遮蔽剂有利地选自R、UV-A、UV-B、UV-C和/或宽带滤光剂。UV-B或宽带遮蔽剂(即在约290nm和340nm之间具有吸光度最大值的物质)的例子可以是有机或无机的化合物。有机UV-B或宽带滤光剂是例如丙烯酸酯,如2-氰基-3,3-二苯基丙烯酸2-乙基己基酯(octocrylene,340)、2-氰基-3,3-二苯基丙烯酸乙基酯等等;樟脑衍生物如4-甲基亚苄基樟脑(5000)、3-亚苄基樟脑、樟脑苯甲烷铵硫酸二甲酯(camphor benzalkonium methosulfate)、聚丙烯酰胺亚苄基樟脑、磺基亚苄基樟脑、磺基甲基亚苄基樟脑、对苯二亚甲基二樟脑磺酸(therephthalidene dicamphor sulfonic acid)等等;肉桂酸酯衍生物,如甲氧肉桂酸辛酯(MCX)、甲氧基肉桂酸乙氧基乙基酯、甲氧基肉桂酸二乙醇胺(Hydro)、甲氧基肉桂酸异戊基酯等等,以及与硅氧烷结合的肉桂酸衍生物;对-氨基苯甲酸衍生物,例如对-氨基苯甲酸、对-二甲氨基苯甲酸2-乙基己酯、N-氧丙烯化的对-氨基苯甲酸乙酯、对-氨基苯甲酸甘油酯;二苯甲酮,例如二苯甲酮-3、二苯甲酮-4、2,2′,4,4′-四羟基-二苯甲酮、2,2′-二羟基-4,4′-二甲氧基二苯甲酮等等;亚苄基丙二酸酯,例如4-甲氧基亚苄基丙二酸二(2-乙基己基)酯;2-(4-乙氧基-苯胺基亚甲基)-丙二酸的酯,例如欧洲专利公开EP-A2-0895 776中描述的2-(4-乙氧基-苯胺基亚甲基)-丙二酸二乙酯;如欧洲专利公开EP 0358584 B1、EP0538431 B1和EP 0709080 A1中描述的含苄基丙二酸酯(benzmalonate)基团的有机硅氧烷化合物,如SLX;甲酚曲唑三硅氧烷(drometrizole trisiloxane)(Mexoryl XL);咪唑衍生物,例如2-苯基苯并咪唑磺酸及其盐(HS)。2-苯基苯并咪唑磺酸的盐为例如钠盐或钾盐的碱金属盐,铵盐,吗啉盐,一级、二级和三级铵盐如单乙醇胺盐、二乙醇胺盐等等;水杨酸酯衍生物,例如水杨酸异丙基苄酯、水杨酸苄酯、水杨酸丁酯、水杨酸乙基己基酯(EHS,Neo Heliopan OS)、水杨酸异辛酯或水杨酸三甲基环己醇(胡莫柳酯,HMS,NeoHeliopan HMS)等等;三嗪衍生物,例如乙基己基三嗪酮(UVINUL T-150)、二乙基己基丁酰胺三嗪酮(UVASORB HEB)等等。被封装的UV滤光剂例如被封装的甲氧基肉桂酸乙基己基酯(Eusolex UV-pearls)或载有UV滤光剂的微粒体例如公开于EP 1471995等等中。
宽带或UV-A遮蔽剂(即在约320nm和400nm之间具有吸光度最大值的物质)的例子可以是有机或无机的化合物。有机的宽带或UV-A遮蔽剂包括例如二苯酰甲烷衍生物,例如4-叔丁基-4’-甲氧基二苯甲酰基-甲烷(1789)、二甲氧基二苯酰甲烷、异丙基二苯酰甲烷等等;苯并三唑衍生物,例如2,2′-亚甲基-二[(6-(2H-苯并三唑-2-基)-4-(1,1,3,3,-四甲基丁基)-苯酚)](TINOSORB M)等等;二乙基己基氧苯酚甲氧基苯基三嗪(Tinosorb S)等等;亚苯基-1,4-二-苯并咪唑磺酸或盐,例如2,2-(1,4-亚苯基)-二-(1H-苯并咪唑-4,6-二磺酸)(Neoheliopan AP);氨基取代的羟基二苯甲酮,例如如欧洲专利公开EP 1046391中所述的2-(4-二乙氨基-2-羟基-苯甲酰基)-苯甲酸己酯(Uvinul A plus);国际专利公开WO2005080341 A1中所述的离子型UV-A滤光剂。因为二苯酰甲烷衍生物具有有限的光稳定性,所以使这些UV-A遮蔽剂光稳定是所期望的。因此,术语“常规的UV-A遮蔽剂”也指用例如3,3-二苯基丙烯酸酯衍生物(如欧洲专利公开EP 0514 491 B1和EP 0780 119 A1中所描述的)、亚苄基樟脑衍生物(如US专利No.5605680中描述的)以及含有苄基丙二酸基团的有机硅氧烷(如欧洲专利公开EP 0358584 B1、EP 053843 B1和EP 0709080 A1中描述的)稳定的二苯酰甲烷衍生物(例如1789)。
可加入本发明组合物中的UV-A和UV-B遮蔽剂的良好综述也可见于DE-A 103 27 432中。该文件中公开的所有UV-遮蔽剂也适用作本发明组合物的成分,并通过引用并入本文。本发明的组合物还可含有UV-A和UV-B滤光剂。UV-滤光剂或遮蔽剂的其它例子公开于例如WO 04/000256中,特别参阅10-12页,其通过引用包括在本文中。
使用安全和有效用量的UV-遮蔽剂,典型地以组合物总重为基础从约1wt.-%到约20wt.-%,更典型地从约2wt.-%到约10wt.-%。
可以掺入本发明化妆品或药物局部组合物中的其它合适的UV-遮蔽剂是无机色素,例如微粒化的金属氧化物(例如TX)。这类化合物的例子包括例如具有从约15nm到约100nm的平均原始颗粒尺寸的二氧化钛,具有从约15nm到约150nm的平均原始颗粒尺寸的氧化锌,具有从约15nm到约150nm的平均原始颗粒尺寸的氧化锆,具有从约15nm到约500nm的平均原始颗粒尺寸的氧化铁,及其混合物。也可以用金属氧化物(例如氧化铝或氧化锆)或用有机包衣(例如多元醇、甲基硅氧烷、硬脂酸铝、烷基甲硅烷)来包覆所述金属氧化物颗粒。这类包衣是本领域公知的。在本文中使用时,所述无机遮光剂以组合物总重为基础,以从约0.1wt.-%到约20wt.-%,优选地从约0.5wt.-%到约10wt.-%,更优选地从约1wt.-%到约5wt.-%的用量存在。
脂肪酸或其盐、酯或酰胺(其具有上文定义的优选级和定义)是已知的或属于已知的化合物种类,从而可以用已知的方法或其类推方法来制备。
在另一实施方案中,本发明涉及脂肪酸或其盐、酯或酰胺(其具有上文给出的优选级和定义)用于增强类视黄醇和/或美黑活性成分的化妆品效应的用途。
可以在体外测试体系中使用下文指出的人原始角质形成细胞来证明本发明组合物的有效性以及上文定义的类视黄醇和脂肪酸之间协同效应的概念,所述组合物包含任选地与类视黄醇组合的脂肪酸或其盐、酯或酰胺(其具有上文定义的优选级和定义)。标记可以是转谷氨酰胺酶1,其为人表皮细胞中公知和常见的分化标记。表皮角质形成细胞从人包皮活检中被分离,并在角质形成细胞无血清培养基(KSFM,GIBCO)中在37℃和5%CO2的培养箱中培养。第二次传代时,将细胞转移至6孔平板并允许其达到约50%的表面融合。
活性成分溶于乙醇或乙醇/四氢呋喃中。仅在黄光条件下操作视黄酸溶液。当成角质细胞培养物达到适当的融合率时,向KSFM培养基中添加1.3mM钙来诱导成角质细胞分化,从而也诱导TG1表达,通过添加类视黄醇(例如视黄酸)或脂肪酸或其盐、酯或酰胺(其具有上文给定的定义和优选级)或两种物质的组合来开始处理。对于每个样品而言,培养基和/或处理物质每天更换两次。开始处理后二十四小时收集细胞并提取RNA。RNA被反转录为cDNA。使用多重实时PCR分析测定对照与处理培养物相比的TG1 mRNA转录物水平的相对定量。
本发明的化妆品或药物组合物减少皮肤皱纹的能力可以通过″Skintopography measurement by interference fringe projection:a technicalvalidation″.(Lagarde J M;Rouvrais C;Black D;Diridollou S;Gall Y,Skinresearch and technology:International Society for Bioengineering and the Skin(ISBS)[和]International Society for Digital Imaging of Skin(ISDIS)[和]International Society for Skin Imaging(ISSI)的官方期刊(2001 May),7(2),112-21)或″Direct and non-direct measurement techniques for analysis of skinsurface topography″.Fischer T W;Wigger-Alberti W;Eisner P.,Skinpharmacology and applied skin physiology(1999Jan-Apr),12(1-2),1-11中描述的轮廓测量法(profilometric method)来评估。
本发明化合物刺激或保护头发生长的能力可以用例如WO 9817273中描述的小鼠模型来测定。可使用丝裂霉素(Mitomycin)或甲氨喋呤(Methotrexate)代替使用环磷酰胺(Neostar,Pharmacia)来破坏毛囊。也可能用新生小鼠来检测毛发生长加速现象。它们具有同步的毛发周期,大约3周后所有的毛囊进入终期(telogen phase)。然后处理动物并评估毛发生长得有多快和到达何种程度。使用体外或体内方案的类似测试也可见于J.Invest.Dermato.symposium proceedings 3rd Int.Meeting of HairResearch Societies,8/1,p.39-45(2003)中。
以下的实施例例证本发明,但是它们不应被理解为限制本发明。
实施例1
含有下文所示成分的抗衰老配方可以以本身已知的方式制备。
示例配方编号 1
成分 %(w/w)
肉豆蔻酸甘油酯 4.00
鲸蜡醇 2.00
Steareth-2 2.00
Steareth-21 2.00
肉豆蔻酸异丙酯 5.00
生育酚醋酸酯 0.50
甲氧基肉桂酸乙基己基酯 4.00
水杨酸乙基己基酯 2.00
丁基甲氧基二苯酰甲烷 1.00
杏仁油 2.00
BHT 0.05
苯氧乙醇&对羟基苯甲酸甲酯&对羟基苯甲酸乙酯& 0.80
对羟基苯甲酸丙酯&对羟基苯甲酸丁酯&对羟基苯甲
酸异丙酯
EDTA二钠 0.10
D-泛醇 0.30
丙二醇 4.00
聚丙烯酰胺&C13-14异链烷烃&Laureth-7 0.50
9-羟基硬脂酸 0.50
视黄醇15D(甘油三辛酸/癸酸酯&视黄醇) 0.50
水 加到
100
三乙醇胺 适量
实施例2
含有下文所示成分的抗衰老配方可以以本身已知的方式制备。
示例配方编号 2
成分 %(w/w)
肉豆蔻酸甘油酯 4.00
鲸蜡醇 2.00
Steareth-2 2.00
Steareth-21 2.00
肉豆蔻酸异丙酯 5.00
生育酚醋酸酯 0.50
甲氧基肉桂酸乙基己基酯 4.00
水杨酸乙基己基酯 2.00
丁基甲氧基二苯酰甲烷 1.00
杏仁油 2.00
BHT 0.05
苯氧乙醇&对羟基苯甲酸甲酯&对羟基苯甲酸乙酯& 0.80
对羟基苯甲酸丙酯&对羟基苯甲酸丁酯&对羟基苯甲
酸异丙酯
EDTA二钠 0.10
D-泛醇 0.30
丙二醇 4.00
聚丙烯酰胺&C13-14异链烷烃&Laureth-7 0.50
水 加到
100
9-羟基硬脂酸 0.50
视黄醇醋酸酯2.8MI 0.10
三乙醇胺 适量
实施例3
含有下文所示成分的面部护理(facial treatment)配方可以以本身已知
的方式制备。
配方编号 3
成分 %(w/w)
肉豆蔻酸甘油酯 5.00
鲸蜡醇 2.00
磷酸十六烷基酯 2.00
肉豆蔻酸异丙酯 10.00
生育酚醋酸酯 0.30
杏仁油 2.00
BHT 0.05
苯氧乙醇&对羟基苯甲酸甲酯&对羟基苯甲酸乙酯& 0.60
对羟基苯甲酸丙酯&对羟基苯甲酸丁酯&对羟基苯甲
酸异丙酯
氨基丁三醇 0.90
水 加到
100
D-泛醇 0.20
EDTA二钠 0.10
丙二醇 4.00
聚丙烯酰胺&C13-14异链烷烃&Laureth-7 2.00
9-羟基硬脂酸 0.50
视黄醇15D(甘油三辛酸/癸酸酯&视黄醇) 0.50
三乙醇胺 适量
实施例4
含有下文所示成分的面部护理(facial treatment)配方可以以本身已知
的方式制备。
配方编号 4
成分 %(w/w)
肉豆蔻酸甘油酯 5.00
鲸蜡醇 2.00
磷酸十六烷基酯 2.00
肉豆蔻酸异丙酯 10.00
生育酚醋酸酯 0.30
杏仁油 2.00
BHT 0.05
苯氧乙醇&对羟基苯甲酸甲酯&对羟基苯甲酸乙酯& 0.60
对羟基苯甲酸丙酯&对羟基苯甲酸丁酯&对羟基苯甲
酸异丙酯
氨基丁三醇 0.90
水 加到
100
D-泛醇 0.20
EDTA二钠 0.10
丙二醇 4.00
聚丙烯酰胺&C13-14异链烷烃&Laureth-7 2.00
9-羟基硬脂酸 0.50
视黄醇醋酸酯2.8MI 0.10
三乙醇胺 适量
实施例5
含有下文所示成分的脱发修护霜(hair loss sera)可以以本身已知的方式
制备。
配方编号 5
成分 %(w/w)
水 加到100
乙醇 8.00
异丙醇 4.00
丙二醇 5.00
D-泛醇 0.20
PEG-12二甲基硅氧烷 0.20
PEG-40氢化蓖麻油 4.00
植烷三醇(Phytantriol) 0.05
维生素E醋酸酯 0.10
9-羟基硬脂酸 0.50
视黄醇15D(甘油三辛酸/癸酸 0.50
酯&视黄醇)
NaOH 10% 适量
实施例6
含有下文所示成分的脱发修护霜(hair loss sera)可以以本身已知的方式
制备。
配方编号 6
成分 %(w/w)
水 加到100
乙醇 8.00
异丙醇 4.00
丙二醇 5.00
D-泛醇 0.20
PEG-12二甲基硅氧烷 0.20
PEG-40氢化蓖麻油 4.00
植烷三醇(Phytantriol) 0.05
维生素E醋酸酯 0.10
9-羟基硬脂酸 0.50
视黄醇醋酸酯2.8 MI 0.10
NaOH 10% 适量
实施例7
含有下文所示成分的皮肤滋养乳液(skin fortifier lotion)可以以本身已
知的方式制备。
配方编号 7
成分 %(w/w)
水 加到100
D-泛醇 0.05
抗坏血酸磷酸钠 0.20
丙二醇 5.00
丙烯酸酯/丙烯酸C10-30烷基酯 0.50
交叉聚合物
氢氧化钠30% 0.40
EDTA二钠 0.10
角鲨烷 2.00
苯氧乙醇&对羟基苯甲酸甲酯 0.80
&对羟基苯甲酸乙酯&对羟基苯
甲酸丙酯&对羟基苯甲酸丁酯&
对羟基苯甲酸异丙酯
辛酸/癸酸可可酯(Coco- 4.00
Caprylate/Caprate)
BHT 0.05
生育酚醋酸酯 0.10
环甲基硅氧烷 3.00
丙三醇 3.00
9-羟基硬脂酸 0.50
视黄醇15D(甘油三辛酸/癸酸 0.50
酯&视黄醇)
氢氧化钠10% 适量
实施例8
含有下文所示成分的皮肤滋养乳液可以以本身已知的方式制备。
配方编号 8
成分 %(w/w)
水 加到100
D-泛醇 0.05
抗坏血酸磷酸钠 0.20
丙二醇 5.00
丙烯酸酯/丙烯酸C10-30烷基酯 0.50
交叉聚合物
氢氧化钠30% 0.40
EDTA二钠 0.10
角鲨烷 2.00
苯氧乙醇&对羟基苯甲酸甲酯 0.80
&对羟基苯甲酸乙酯&对羟基苯
甲酸丙酯&对羟基苯甲酸丁酯&
对羟基苯甲酸异丙酯
辛酸/癸酸可可酯(Coco- 4.00
Caprylate/Caprate)
BHT 0.05
生育酚醋酸酯 0.10
环甲基硅氧烷 3.00
丙三醇 3.00
9-羟基硬脂酸 0.50
视黄醇醋酸酯2.8 MI 0.10
氢氧化钠10% 适量
实施例9
含有下文所示成分的治疗年龄斑(age spot)的配方可以以本身已知的方
式制备。
配方编号 9
成分 %(w/w)
水 加到100
聚季铵盐-10(Polyquaternium-10) 0.10
D-泛醇 0.50
抗坏血酸磷酸钠 1.00
烟酰胺(Niacinamid) 0.50
丙二醇 4.00
甘油 3.00
PEG-12二甲基硅氧烷 0.20
EDTA二钠 0.10
聚山梨醇酯20(Polysorbate 20) 5.00
苯氧乙醇&对羟基苯甲酸甲酯 0.80
&对羟基苯甲酸乙酯&对羟基苯
甲酸丙酯&对羟基苯甲酸丁酯&
对羟基苯甲酸异丙酯
9-羟基硬脂酸 0.50
视黄醇15D(甘油三辛酸/癸酸 0.50
酯&视黄醇)
氢氧化钠10% 适量
实施例10
含有下文所示成分的治疗年龄斑的配方可以以本身已知的方式制备。
配方编号 10
成分 %(w/w)
水 加到100
聚季铵盐-10(Polyquaternium-10) 0.10
D-泛醇 0.50
抗坏血酸磷酸钠 1.00
烟酰胺(Niacinamid) 0.50
丙二醇 4.00
甘油 3.00
PEG-12二甲基硅氧烷 0.20
EDTA二钠 0.10
聚山梨醇酯20(Polysorbate 20) 5.00
苯氧乙醇&对羟基苯甲酸甲酯 0.80
&对羟基苯甲酸乙酯&对羟基苯
甲酸丙酯&对羟基苯甲酸丁酯&
对羟基苯甲酸异丙酯
9-羟基硬脂酸 0.50
视黄醇醋酸酯2.8 MI 0.10
氢氧化钠10% 适量
实施例11
含有下文所示成分的抗橘皮组织(anti-cellulite)配方可以以本身已知的
方式制备。
示例配方编号 11
成分 %(w/w)
水 加到
100
咖啡因 1.00
D-泛醇 0.50
甘油 4.00
丁二醇 2.00
丙烯酸酯/丙烯酸C10-30烷基酯交叉聚合物 0.20
EDTA二钠 0.10
花生醇&山萮醇&二十烷葡糖苷(Arachidyl Glucoside) 5.00
角鲨烷 2.00
矿物油 4.00
苯氧乙醇&对羟基苯甲酸甲酯&对羟基苯甲酸乙酯& 0.80
对羟基苯甲酸丙酯&对羟基苯甲酸丁酯&对羟基苯甲
酸异丙酯
异壬酸异壬基酯 4.00
BHT 0.05
鲸蜡醇 2.00
二甲基硅氧烷 0.50
生育酚醋酸酯 0.10
9-羟基硬脂酸 0.50
视黄醇15D(甘油三辛酸/癸酸酯&视黄醇) 0.50
三乙醇胺 适量
实施例12
含有下文所示成分的抗橘皮组织配方可以以本身已知的方式制备。
示例配方编号 12
成分 %(w/w)
水 加到
100
咖啡因 1.00
D-泛醇 0.50
甘油 4.00
丁二醇 2.00
丙烯酸酯/丙烯酸C10-30烷基酯交叉聚合物 0.20
EDTA二钠 0.10
花生醇&山萮醇&二十烷葡糖苷(Arachidyl Glucoside) 5.00
角鲨烷 2.00
矿物油 4.00
苯氧乙醇&对羟基苯甲酸甲酯&对羟基苯甲酸乙酯& 0.80
对羟基苯甲酸丙酯&对羟基苯甲酸丁酯&对羟基苯甲
酸异丙酯
异壬酸异壬基酯 4.00
BHT 0.05
鲸蜡醇 2.00
二甲基硅氧烷 0.50
生育酚醋酸酯 0.10
9-羟基硬脂酸 0.50
视黄醇醋酸酯2.8 MI 0.1
三乙醇胺 适量
实施例13
含有下文所示成分的皮肤修护配方可以以本身已知的方式制备。
配方编号 13
成分 %(w/w)
聚甘油-2-二聚羟基硬脂酸酯 4.00
聚甘油-3-二异硬脂酸酯 2.00
蜂蜡 2.00
硬脂酸锌 2.00
甘油三辛酸/癸酸酯 3.00
异壬酸鲸蜡硬脂醇酯(Cetearyl 8.00
Isononanoate)
二辛醚(Dicaprylyl Ether) 5.00
BHT 0.05
苯氧乙醇&对羟基苯甲酸甲酯 0.60
&对羟基苯甲酸乙酯&对羟基苯
甲酸丙酯&对羟基苯甲酸丁酯
&对羟基苯甲酸异丙酯
水 加到100
D-泛醇 0.20
EDTA二钠 0.10
丙二醇 4.00
9-羟基硬脂酸 0.55
视黄醇15D(甘油三辛酸/癸酸 0.50
酯&视黄醇)
实施例14
含有下文所示成分的皮肤修护配方可以以本身已知的方式制备。
配方编号 14
成分 %(w/w)
聚甘油-2-二聚羟基硬脂酸酯 4.00
聚甘油-3-二异硬脂酸酯 2.00
蜂蜡 2.00
硬脂酸锌 2.00
甘油三辛酸/癸酸酯 3.00
异壬酸鲸蜡硬脂醇酯(Cetearyl 8.00
Isononanoate)
二辛醚(Dicaprylyl Ether) 5.00
BHT 0.05
苯氧乙醇&对羟基苯甲酸甲酯 0.60
&对羟基苯甲酸乙酯&对羟基苯
甲酸丙酯&对羟基苯甲酸丁酯
&对羟基苯甲酸异丙酯
水 加到100
D-泛醇 0.20
EDTA二钠 0.10
丙二醇 4.00
9-羟基硬脂酸 0.55
视黄醇醋酸酯2.8 MI 0.10
Claims (22)
1.一种化妆品或药物组合物,其包含:含有6到18个碳原子的脂肪酸,所述脂肪酸带有一个或两个羟基、烷氧基、C2-C4酰基保护的氨基、或氧代基;或这类酸的盐、酯或酰胺,或这些酸的混合物;以及常规用于化妆品或药物组合物中的载剂,其中所述烷氧基优选甲氧基或乙氧基,所述C2-C4酰基优选C2。
2.如权利要求1所述的组合物,其中所述脂肪族脂肪酸是饱和的直链脂肪酸或ω-支链的脂肪酸。
3.如权利要求2所述的组合物,其中所述饱和的直链或ω-支链脂肪酸在位置6和12之间被取代。
4.如权利要求3所述的组合物,其中饱和的直链或ω-支链脂肪酸被羟基取代。
5.如权利要求4所述的组合物,其中所述脂肪酸是9-羟基硬脂酸。
6.如权利要求1到5中任一项所述的组合物,其额外包含类视黄醇。
7.如权利要求1到6中任一项所述的组合物,其中所述类视黄醇为视黄酸或其衍生物。
8.如权利要求1到6中任一项所述的组合物,其中所述类视黄醇为视黄基醋酸酯、苯基丁酸酯、丙酸酯、辛酸酯、月桂酸酯、棕榈酸酯、油酸酯、亚油酸酯;或视黄基烷基碳酸酯;视黄氧三甲基甲硅烷;(全反式)视黄醛或其缩醛;或甲氧基PEG-12视黄酰胺。
9.根据权利要求1到8中任一项的组合物,其中所述脂肪酸的量以重量计占总组合物的约0.0001%到约50%。
10.根据权利要求1到8中任一项的组合物,其中所述脂肪酸的量以重量计占总组合物的约0.001%到约20%。
11.根据权利要求1到8中任一项的组合物,其中所述脂肪酸的量以重量计占总组合物的约0.01%到约1%。
12.根据权利要求6到11中任一项的组合物,其中所述类视黄醇或其衍生物的量以重量计占总组合物的约0.001%到约50%。
13.根据权利要求6到11中任一项的组合物,其中所述类视黄醇或其衍生物的量以重量计占总组合物的约0.01%到约20%。
14.根据权利要求6到11中任一项的组合物,其中所述类视黄醇或其衍生物的量以重量计占总组合物的约0.01%到约1%。
15.根据权利要求6到14中任一项的组合物,其中以重量计,所述脂肪酸与所述类视黄醇或其衍生物的比例为约1000∶1到约1∶1000。
16.根据权利要求6到14中任一项的组合物,其中以重量计,所述脂肪酸与所述类视黄醇或其衍生物的比例为约100∶1到约1∶100。
17.根据权利要求6到14中任一项的组合物,其中以重量计,所述脂肪酸与所述类视黄醇或其衍生物的比例为约30∶1到约1∶30。
18.如权利要求1到17中任一项所述的组合物,其用于预防或治疗由健康皮肤的生理自身稳态负向发展所引起的症状、促进头发生长、防止脱发、预防和治疗发痒或受刺激的皮肤。
19.如权利要求1到17中任一项所述的组合物,其用于预防或治疗色素沉着疾病和/或用于提供均匀的肤色。
20.如权利要求1到5和9到11中任一项所述的组合物,其用于通过增强美黑活性成分的效应来强化色素沉着。
21.如权利要求1到17中任一项所述的组合物,其用于治疗或预防皱纹或干性皮肤或敏感性皮肤、用于促进头发生长、用于防止脱发和用于增厚表皮。
22.一种治疗或预防方法,其用于治疗或预防由健康皮肤的生理自身稳态负向发展所引起的症状,以及治疗或预防发痒或受刺激的皮肤、促进头发生长、防止脱发,所述方法包括步骤:向需要这类治疗或预防的人局部施用有效用量的脂肪酸或盐、酯或酰胺,可选地与类视黄醇组合施用。
Applications Claiming Priority (5)
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EP05020779 | 2005-09-23 | ||
EP05020779.4 | 2005-09-23 | ||
EP05020905.5 | 2005-09-26 | ||
EP05020905 | 2005-09-26 | ||
PCT/EP2006/008961 WO2007039057A1 (en) | 2005-09-23 | 2006-09-14 | Cosmetic compositions comprising hydroxyfatty acids |
Publications (2)
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CN101272775A true CN101272775A (zh) | 2008-09-24 |
CN101272775B CN101272775B (zh) | 2012-05-30 |
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CN2006800351938A Expired - Fee Related CN101272775B (zh) | 2005-09-23 | 2006-09-14 | 包含羟基脂肪酸的化妆品组合物 |
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US (2) | US20090124693A1 (zh) |
EP (1) | EP1931329B1 (zh) |
JP (1) | JP5113755B2 (zh) |
KR (1) | KR101365282B1 (zh) |
CN (1) | CN101272775B (zh) |
WO (1) | WO2007039057A1 (zh) |
Cited By (2)
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CN104507470A (zh) * | 2012-06-01 | 2015-04-08 | 盖尔德马研究及发展公司 | 含有类维生素a的o/w乳液类型的局部药物组合物 |
CN108135816A (zh) * | 2015-09-07 | 2018-06-08 | 医疗美容解决方案祖韦拉克医生公司 | 用于局部施用的包含二甲基异山梨醇、多元醇及酚类或多酚类抗氧化剂的组合物 |
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DE102008009749A1 (de) * | 2008-02-18 | 2009-08-20 | Beiersdorf Ag | Kosmetische oder dermatologische Zubereitungen mit einem Gehalt an 3-(4-Hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-propan-1-on und einem oder mehreren Zimtsäurederivaten |
US20100196291A1 (en) * | 2009-01-30 | 2010-08-05 | Laurence Halimi | Personal care sunscreen compositions having reduced eye irritation |
DE102009047764A1 (de) * | 2009-12-10 | 2011-06-16 | Evonik Goldschmidt Gmbh | Trennmittel und Verwendung zur Herstellung von Kompositformkörpern |
EP2667853A4 (en) * | 2011-01-25 | 2014-08-20 | Procter & Gamble | LIPOSOME AND BODY HYGIENE COMPOSITION CONTAINING SAME |
JP6222894B2 (ja) * | 2012-03-30 | 2017-11-01 | 小林製薬株式会社 | 表皮肥厚促進剤 |
US9511144B2 (en) | 2013-03-14 | 2016-12-06 | The Proctor & Gamble Company | Cosmetic compositions and methods providing enhanced penetration of skin care actives |
US20170304169A1 (en) * | 2014-10-17 | 2017-10-26 | Dsm Ip Assets B.V. | Use of a cosmetic composition comprising 10-hydroxystearic acid |
US20160166479A1 (en) * | 2014-12-16 | 2016-06-16 | L'oreal | Use of trialkoxysilane derivatives to modify the appearance of emulsion-type cosmetic compositions |
CA3016436A1 (en) * | 2016-03-04 | 2017-09-08 | Arkema Inc. | Encapsulation of peroxides for skin applications |
WO2017178235A1 (en) * | 2016-04-13 | 2017-10-19 | Dsm Ip Assets B.V. | 10-hydroxystearic acid compositions |
WO2019004768A2 (ko) * | 2017-06-30 | 2019-01-03 | (주)아모레퍼시픽 | 화장료 조성물 및 이의 제조방법 |
KR102552133B1 (ko) * | 2017-06-30 | 2023-07-06 | (주)아모레퍼시픽 | 화장료 조성물 및 이의 제조방법 |
KR102635198B1 (ko) * | 2018-11-29 | 2024-02-13 | (주)아모레퍼시픽 | 피부 보습 및 피부 상태 개선용 국소부위 화장료 조성물 |
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WO2023228199A1 (en) * | 2022-05-27 | 2023-11-30 | Ultramarine & Pigments Limited | Topical composition and implementations thereof |
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2006
- 2006-09-14 KR KR1020087006897A patent/KR101365282B1/ko active IP Right Grant
- 2006-09-14 WO PCT/EP2006/008961 patent/WO2007039057A1/en active Application Filing
- 2006-09-14 CN CN2006800351938A patent/CN101272775B/zh not_active Expired - Fee Related
- 2006-09-14 JP JP2008531583A patent/JP5113755B2/ja not_active Expired - Fee Related
- 2006-09-14 EP EP06792061.1A patent/EP1931329B1/en not_active Not-in-force
- 2006-09-14 US US11/990,490 patent/US20090124693A1/en not_active Abandoned
-
2011
- 2011-09-01 US US13/137,659 patent/US8394855B2/en not_active Expired - Fee Related
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104507470A (zh) * | 2012-06-01 | 2015-04-08 | 盖尔德马研究及发展公司 | 含有类维生素a的o/w乳液类型的局部药物组合物 |
CN108135816A (zh) * | 2015-09-07 | 2018-06-08 | 医疗美容解决方案祖韦拉克医生公司 | 用于局部施用的包含二甲基异山梨醇、多元醇及酚类或多酚类抗氧化剂的组合物 |
Also Published As
Publication number | Publication date |
---|---|
KR20080050587A (ko) | 2008-06-09 |
WO2007039057A1 (en) | 2007-04-12 |
US20110312915A1 (en) | 2011-12-22 |
KR101365282B1 (ko) | 2014-02-19 |
EP1931329B1 (en) | 2016-11-16 |
US20090124693A1 (en) | 2009-05-14 |
JP2009508894A (ja) | 2009-03-05 |
US8394855B2 (en) | 2013-03-12 |
JP5113755B2 (ja) | 2013-01-09 |
EP1931329A1 (en) | 2008-06-18 |
CN101272775B (zh) | 2012-05-30 |
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