CN1371271A - Cosmetic composition - Google Patents
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- CN1371271A CN1371271A CN00812224A CN00812224A CN1371271A CN 1371271 A CN1371271 A CN 1371271A CN 00812224 A CN00812224 A CN 00812224A CN 00812224 A CN00812224 A CN 00812224A CN 1371271 A CN1371271 A CN 1371271A
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- A61Q19/08—Anti-ageing preparations
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/14—Liposomes; Vesicles
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K8/00—Cosmetics or similar toiletry preparations
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- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/29—Titanium; Compounds thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/345—Alcohols containing more than one hydroxy group
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- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/35—Ketones, e.g. benzophenone
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/368—Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/41—Amines
- A61K8/416—Quaternary ammonium compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
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- A61K8/00—Cosmetics or similar toiletry preparations
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- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/673—Vitamin B group
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/673—Vitamin B group
- A61K8/675—Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
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- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
- A61K8/86—Polyethers
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61Q19/00—Preparations for care of the skin
- A61Q19/007—Preparations for dry skin
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Abstract
Description
技术领域Technical field
本发明涉及化妆品组合物。具体地,本发明涉及可提供好的滋润作用、水合作用、皮肤感觉、皮肤柔软性和/或皮肤光滑性效果的化妆品组合物。The present invention relates to cosmetic compositions. In particular, the present invention relates to cosmetic compositions that provide good moisturization, hydration, skin feel, skin softness and/or skin smoothness benefits.
发明背景Background of the Invention
皮肤由若干层细胞构成,这些细胞覆盖并保护构成皮肤结构骨架的角蛋白和胶原纤维蛋白。这些层的最外层称为角质层,并已知由8nm厚的层围绕的25nm蛋白束构成。阴离子表面活性剂和有机溶剂一般可穿透角质层膜,并经脱脂作用(即去除角质层中的脂类物质)而破坏皮肤的完整性。这种对皮肤表面局部解剖学结构的破坏作用将会带来粗糙感,从而最终会令表面活性剂和溶剂与角蛋白发生相互作用而产生刺激作用。许多人的皮肤每天都暴露于这种伤害之中。而且,皮肤也会受到其它因素如暴露于冷空气或风、机械摩擦、浸在水中等而带来的伤害。因此,需要一种能改善或缓和这种伤害的方式。The skin is made up of several layers of cells that cover and protect the keratin and collagen fibers that form the structural backbone of the skin. The outermost of these layers is called the stratum corneum and is known to consist of 25nm protein bundles surrounded by an 8nm thick layer. Anionic surfactants and organic solvents generally penetrate the stratum corneum membrane and disrupt the integrity of the skin by degreasing (ie, removing lipids from the stratum corneum). This disruption of the topographical structure of the skin surface results in roughness, which ultimately leads to irritation by the interaction of surfactants and solvents with keratin. Many people's skin is exposed to this damage every day. Moreover, the skin can also be damaged by other factors such as exposure to cold air or wind, mechanical friction, immersion in water, and the like. Therefore, there is a need for a way to ameliorate or alleviate this damage.
过去,已经配制出这样的组合物,声称它们可帮助角质层保持其屏障和保水功能在最佳性能,而不必考虑在洗涤、工作和娱乐中皮肤可能遇到的有害的相互作用。对这样的组合物而言,希望它们具有的性能是它们具有好的皮肤感觉、保水性、滋润作用(moisturisation)、吸收性和/或摩擦涂入(rub-in)特征。现有技术的组合物试图通过使用一种或多种“皮肤有益成分(skin benefit agent)”而带来这些性能。例如,一种给皮肤带来高滋润作用的方法是在组合物中引入多元醇类保湿剂物质如甘油。但是,多元醇含量高并因此而具有高滋润作用的皮肤用组合物通常会被消费者感觉不好,因为这样的组合物在应用到皮肤上时,能感觉到发粘。In the past, compositions have been formulated that claim to help the stratum corneum maintain its barrier and water-retaining functions at optimum performance, regardless of the deleterious interactions that the skin may encounter during washing, work and play. Desirable properties for such compositions are that they have good skin feel, water retention, moisturisation, absorbency and/or rub-in characteristics. Compositions of the prior art attempt to bring about these properties through the use of one or more "skin benefit agents". For example, one method of imparting high moisturization to the skin is to include in the composition a polyol humectant material such as glycerin. However, skin compositions high in polyol content and thus highly moisturizing are often perceived by consumers as being sticky when applied to the skin.
看起来护肤有益成分的用量和组合物向皮肤提供有益效果的功效之间存在直接关系。但是,事实上皮肤有益成分的含量越高,与之相关的不利作用的危险性也就越高。因此,到目前为止,需要平衡皮肤有益成分含量高的组合物所带来的益处和与这种高含量相关的不利作用之间的关系。因此,需要皮肤有益成分含量高并因此所带来的相关的益处如皮肤感觉、皮肤柔软性和皮肤光滑性高,但显示相关的不利作用如油腻性、粘着性或粘腻性低的组合物。There appears to be a direct relationship between the amount of skin care benefit ingredient used and the efficacy of the composition to provide the benefit to the skin. In fact, however, the higher the content of skin beneficial ingredients, the higher the risk of adverse effects associated with them. Thus, heretofore, there has been a need to balance the benefits conferred by compositions high in skin benefit ingredients with the adverse effects associated with such high levels. Therefore, there is a need for compositions that are high in skin benefit ingredients and thus provide associated benefits such as skin feel, skin softness and skin smoothness, but exhibit associated adverse effects such as low greasy, sticky or sticky properties .
季铵成分(quaternary ammonium agents)也已知可用于化妆品组合物中。例如参见WO-A-99/27904、WO-A-96/32089和EP-A-789,076。而且,US-A-5,804,205中公开了据称可提供高度滋润作用而不会留下“粘着的”或“粘腻的”残留物的护肤组合物。这些组合物中含有季铵化合物(具有2个16-22个碳原子的烷基)、保湿剂和平均粒径低于50μm的非刺激性的疏水微球。据称疏水聚合微球可明显降低与保湿剂含量高相关的“粘着性”。但是,常规用在现有技术中的季铵成分通常不易于生物降解,并因此对环境有害。Quaternary ammonium agents are also known for use in cosmetic compositions. See eg WO-A-99/27904, WO-A-96/32089 and EP-A-789,076. Furthermore, US-A-5,804,205 discloses skin care compositions which are said to provide a high degree of moisturization without leaving a "sticky" or "sticky" residue. These compositions contain a quaternary ammonium compound (having two alkyl groups of 16-22 carbon atoms), a humectant and non-irritating hydrophobic microspheres with an average particle size below 50 μm. The hydrophobic polymeric microspheres are said to significantly reduce the "stickiness" associated with high humectant levels. However, the quaternary ammonium ingredients conventionally used in the prior art are generally not readily biodegradable and are therefore harmful to the environment.
现已意外地发现包含至少一种易于生物降解的季铵成分和至少5%重量的保湿剂的组合物带来了与之相关的益处如皮肤感觉、皮肤柔软感和皮肤光滑性高,但显示相关的不利作用如油腻性、粘着性或粘腻性低。It has now been surprisingly found that compositions comprising at least one readily biodegradable quaternary ammonium ingredient and at least 5% by weight of a humectant bring benefits associated therewith such as high skin feel, skin softness and skin smoothness, but show Associated adverse effects such as low greasiness, stickiness or stickiness.
尽管不希望受到任何理论的限制,但相信本发明中的季铵成分能够将保湿剂形成小泡,并促使它们沉积在皮肤上。由此使得可光滑并均匀地将保湿剂涂抹于皮肤上,而粘稠/粘着/油腻性最小。即使当组合物包含极高百分含量的保湿剂,例如30%重量的保湿剂时,仍只有较低的通常的不利作用。而且,相信季铵成分有助于降低润肤剂因环境因素如水或摩擦而带来的从皮肤上的损失。并且,相信季铵成分本身带来了护肤效果,如好的滋润作用、好的皮肤感、好的皮肤柔软性。While not wishing to be bound by any theory, it is believed that the quaternary ammonium ingredients of the present invention vesicle the humectants and promote their deposition on the skin. This allows smooth and even application of the moisturizer to the skin with minimal stickiness/stickiness/greasyness. Even when the composition contains extremely high percentages of humectant, for example 30% by weight of humectant, there is still only a low general adverse effect. Furthermore, it is believed that quaternary ammonium ingredients help reduce loss of emollients from the skin due to environmental factors such as water or friction. Also, it is believed that the quaternary ammonium ingredients themselves bring skin care benefits, such as good moisturizing effect, good skin feel, and good skin softness.
发明概述Invention overview
本发明提供了化妆品组合物,包括:The present invention provides a cosmetic composition comprising:
(a)至少一种易于生物降解的季铵成分;和(a) at least one readily biodegradable quaternary ammonium ingredient; and
(b)至少5%重量的保湿剂。(b) at least 5% by weight humectant.
本发明的组合物带来了好的皮肤护理益处,如好的皮肤滋润作用、好的水合作用、好的皮肤感觉、好的皮肤柔软性和/或好的皮肤平滑性,同时不利作用如油腻感、粘腻感或粘着性低。此外,一旦使用,这样的组合物易于降解,并因此对环境更温和。The composition of the present invention brings good skin care benefits, such as good skin moisturization, good hydration, good skin feel, good skin softness and/or good skin smoothness, while unfavorable effects such as Low greasy, sticky or tacky feel. Furthermore, once used, such compositions are prone to degradation and are thus more environmentally friendly.
发明详述Detailed description of the invention
本发明的组合物包含至少一种易于生物降解的季铵成分和保湿剂。这些成分将在下文中进行详细地描述。The compositions of the present invention comprise at least one readily biodegradable quaternary ammonium ingredient and a humectant. These ingredients will be described in detail below.
本发明的组合物能够用于任意合适的目的。特别地,本发明的组合物适于局部应用于皮肤上。具体地,这些皮肤护理组合物可以是膏霜、乳液(lotion)、凝胶等形式。优选本发明的化妆品组合物为在连续水相中的一个或多个油相的水包油型乳剂形式,每个油相含有单一油性组分或呈混溶或均质形式的油性组分的混合物,但所述的不同油相含有彼此不同的材料或这些不同材料的组合。The compositions of the invention can be used for any suitable purpose. In particular, the compositions of the invention are suitable for topical application to the skin. Specifically, these skin care compositions may be in the form of creams, lotions, gels, and the like. Preferably, the cosmetic composition according to the invention is in the form of an oil-in-water emulsion of one or more oily phases in a continuous aqueous phase, each oily phase containing a single oily component or oily components in miscible or homogeneous form. Mixtures, but the different oil phases contain different materials from each other or a combination of these different materials.
本发明的组合物优选包含小泡(vesicle)。优选所述小泡包含季铵化合物以及保湿剂。在本发明中所用的术语“小泡”是指设置成封闭的、通常为球形形状中的一个或多个双层,所述双层包括下文所述的季铵成分。The compositions of the invention preferably comprise vesicles. Preferably the vesicles comprise a quaternary ammonium compound and a humectant. The term "vesicle" as used herein refers to one or more bilayers arranged in a closed, generally spherical shape, said bilayers comprising the quaternary ammonium component described below.
优选,本发明的组合物包含少于10%(重量),优选少于5%(重量),更优选少于3%(重量),更优选0%(重量)的阴离子表面活性剂。Preferably, the compositions of the present invention comprise less than 10% by weight, preferably less than 5% by weight, more preferably less than 3% by weight, more preferably 0% by weight of anionic surfactant.
本发明的组合物优选配制成粘度至少约为1,000mPa.s、优选约为1,000至约300,000mPa.s、更优选约为2,500至约250,000mPa.s、特别是约为5,000至约200,000mPa.s(26.8℃,净相,Brookfield DV-II+锭子CP52/CP41)的产品。季铵成分The compositions of the present invention are preferably formulated to have a viscosity of at least about 1,000 mPa.s, preferably from about 1,000 to about 300,000 mPa.s, more preferably from about 2,500 to about 250,000 mPa.s, especially from about 5,000 to about 200,000 mPa.s (26.8°C, net phase, product of Brookfield DV-II+spindle CP52/CP41). Quaternary Ammonium Ingredients
本发明的组合物必须包含至少一种易于生物降解的季铵成分。适用于美容组合物中的任何易于生物降解的季铵成分均可用于本发明。本发明中使用的术语“季铵成分”是指具有季氮原子的化合物或化合物的混合物,其中季氮原子经一个或多个、优选两个含6个或更多碳原子的部分取代。本发明中使用的术语“易于生物降解”指的是根据OECD 301测试,至少60%的化合物在28天内矿化。优选用于本发明中的季铵成分选自具有被两个部分取代的季氮原子的那些,其中每个部分包含10个或更多个、优选12个或更多个碳原子。特别优选用于本发明中的季铵成分选自能在极性溶剂中形成小泡的那些,这些可以通过显微镜分析法检测(偏光显微镜方法,使用Nikon Eclipse E800显微镜,以×60的放大倍数)。The compositions of the present invention must contain at least one readily biodegradable quaternary ammonium ingredient. Any readily biodegradable quaternary ammonium ingredient suitable for use in cosmetic compositions may be used herein. The term "quaternary ammonium component" as used herein refers to a compound or mixture of compounds having a quaternary nitrogen atom which is substituted with one or more, preferably two, moieties containing 6 or more carbon atoms. The term "readily biodegradable" used in the present invention means that at least 60% of the compound is mineralized within 28 days according to the OECD 301 test. Preferred quaternary ammonium components for use in the present invention are selected from those having a quaternary nitrogen atom substituted by two moieties each containing 10 or more, preferably 12 or more carbon atoms. Particularly preferred quaternary ammonium components for use in the present invention are selected from those capable of forming vesicles in polar solvents, which can be detected by microscopic analysis (polarized light microscopy using a Nikon Eclipse E800 microscope at a magnification of ×60) .
优选,本发明的组合物包含至少0.01%、更优选至少0.1%、还更优选至少1%、进一步更优选至少3%(重量)的季铵成分。Preferably, the compositions of the present invention comprise at least 0.01%, more preferably at least 0.1%, still more preferably at least 1%, even more preferably at least 3% by weight of a quaternary ammonium component.
优选,用于本发明的季铵成分选自:Preferably, the quaternary ammonium ingredients used in the present invention are selected from:
(a)通式(I)或(II)所示的季铵化合物: (a) quaternary ammonium compounds shown in general formula (I) or (II):
其中每个R5单元彼此独立地选自氢、支链或直链C1-C6烷基、支链或直链的C1-C6羟烷基以及它们的混合物,优选是甲基和羟乙基;每个R6单元彼此独立地为直链或支链C11-C22烷基、直链或支链C11-C22链烯基以及它们的混合物;X-是可与皮肤护理活性成分和辅剂成分相容的阴离子;m为1-4,优选为2;n为1-4,优选为2,并且Q是选自以下的羰基单元: wherein each R unit is independently selected from hydrogen, branched or linear C 1 -C 6 alkyl, branched or linear C 1 -C 6 hydroxyalkyl and mixtures thereof, preferably methyl and Hydroxyethyl; each R 6 unit is independently linear or branched C 11 -C 22 alkyl, linear or branched C 11 -C 22 alkenyl and mixtures thereof; X - is compatible with skin Anion compatible with care active ingredients and adjuvant ingredients; m is 1-4, preferably 2; n is 1-4, preferably 2, and Q is a carbonyl unit selected from:
其中R7是氢、C1-C4烷基、C1-C4羟烷基,以及它们的混合物。wherein R 7 is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 hydroxyalkyl, and mixtures thereof.
上述季铵化合物的实例中,单元-QR6含有一般是由甘油三酯源衍生得到的脂肪酰基单元。甘油三酯源优选是衍生自牛油、部分氢化的牛油、猪油、部分氢化的猪油、植物油和/或部分氢化的植物油,如低芥酸菜籽油、红花油、花生油、菜子油、葵花油、玉米油、大豆油、妥尔油(tall oil)、米糠油等,以及这些油的混合物。In the above examples of quaternary ammonium compounds, the unit -QR 6 contains a fatty acyl unit typically derived from a triglyceride source. The source of triglycerides is preferably derived from tallow, partially hydrogenated tallow, lard, partially hydrogenated lard, vegetable oils and/or partially hydrogenated vegetable oils, such as canola oil, safflower oil, peanut oil, rapeseed oil, sunflower oil, corn oil, soybean oil, tall oil, rice bran oil, etc., and mixtures of these oils.
上述化合物中的抗衡离子X-可以是任何相容的阴离子,优选是强酸的阴离子,例如氯离子、溴离子、甲基硫酸根、乙基硫酸根、硫酸根、硝酸根等,更优选是氯离子或甲基硫酸根。阴离子也可以但较少优选带有双电荷,在这种情况下X-代表半个基团。The counter ion X in the above compound can be any compatible anion, preferably an anion of a strong acid, such as chloride, bromide, methylsulfate, ethylsulfate, sulfate, nitrate, etc., more preferably chlorine ion or methylsulfate. The anion may also, but less preferably, be double charged, in which case X − represents a half group.
本发明优选的季铵化合物是二酯和/或二酰胺季铵(DEQA)化合物,二酯和二酰胺具有通式(II),其中羰基Q选自: Preferred quaternary ammonium compounds of the present invention are diester and/or diamide quaternary ammonium (DEQA) compounds, the diesters and diamides having the general formula (II), wherein the carbonyl Q is selected from:
牛油、低芥酸菜籽油和棕榈油是方便且经济的脂肪酰基单元的来源,适于在本发明中用作R6单元。Tallow, canola oil, and palm oil are convenient and economical sources of fatty acyl units suitable for use as R units in the present invention.
抗衡离子X-可以是氯离子、溴离子、甲基硫酸根、甲酸根、硫酸根、硝酸根以及它们的混合物。实际上,阴离子X-仅作为带正电荷的季铵化合物的抗衡离子存在。在本发明的范围内并不考虑将其限定为任何特定的阴离子。The counterion X - can be chloride, bromide, methylsulfate, formate, sulfate, nitrate and mixtures thereof. In fact, the anion X- exists only as a counterion to the positively charged quaternary ammonium compound. It is not considered within the scope of the present invention to be limited to any particular anion.
在本发明中,当规定采用二酯时,其中将包含通常存在的由制备过程中带来的单酯和三酯。In the present invention, when diesters are specified, the monoesters and triesters normally present brought about by the preparation process will be included.
(b)通式(III)或(IV)所示的季铵化合物: (b) quaternary ammonium compounds shown in general formula (III) or (IV):
其中R9是无环脂族C15-C21烃基,R10是C1-C6烷基或亚烷基。Wherein R 9 is an acyclic aliphatic C 15 -C 21 hydrocarbon group, and R 10 is a C 1 -C 6 alkyl or alkylene group.
这些pKa值不超过约4的铵化合物,当在含水溶液中分散时,可就地产生正电荷,条件是最终组合物的pH不超过约6。These ammonium compounds having a pKa value not exceeding about 4 can generate a positive charge in situ when dispersed in an aqueous solution, provided that the pH of the final composition does not exceed about 6.
(c)通式(V)或(VI)所示的季铵化合物: (c) quaternary ammonium compounds shown in general formula (V) or (VI):
其中R9和R10如上文所定义,R11选自C1-C4烷基和羟烷基。wherein R 9 and R 10 are as defined above, and R 11 is selected from C 1 -C 4 alkyl and hydroxyalkyl.
抗衡离子X-可以是氯离子、溴离子、甲基硫酸根、甲酸根、硫酸根、硝酸根以及它们的混合物。实际上,阴离子X-仅作为带正电荷的季铵化合物的抗衡离子存在。在本发明范围内并不考虑将其限定为任何特定的阴离子。The counterion X - can be chloride, bromide, methylsulfate, formate, sulfate, nitrate and mixtures thereof. In fact, the anion X- exists only as a counterion to the positively charged quaternary ammonium compound. It is not considered within the scope of the present invention to be limited to any particular anion.
(d)通式(VII)或(VIII)所示的季铵化合物: (d) quaternary ammonium compounds shown in general formula (VII) or (VIII):
其中,n为1-6,R9选自无环脂族C15-C21烃基,R12选自C1-C4烷基和羟烷基。Wherein, n is 1-6, R 9 is selected from acyclic aliphatic C 15 -C 21 hydrocarbon groups, and R 12 is selected from C 1 -C 4 alkyl and hydroxyalkyl groups.
这些pKa值不超过约4的铵化合物,当在含水溶液中分散时,可就地产生阳离子电荷,条件是最终组合物的pH不超过约6。These ammonium compounds having a pKa value not exceeding about 4 can generate cationic charges in situ when dispersed in an aqueous solution, provided that the pH of the final composition does not exceed about 6.
抗衡离子X-可以是氯离子、溴离子、甲基硫酸根、甲酸根、硫酸根、硝酸根以及它们的混合物。实际上,阴离子X-仅作为带正电荷的季铵化合物的抗衡离子存在。本发明范围内并不打算将其限定为任何特定的阴离子。The counterion X - can be chloride, bromide, methylsulfate, formate, sulfate, nitrate and mixtures thereof. In fact, the anion X- exists only as a counterion to the positively charged quaternary ammonium compound. It is not intended that the scope of the invention be limited to any particular anion.
(e)通式(IX)或(X)所示的季铵化合物: (e) quaternary ammonium compounds shown in general formula (IX) or (X):
其中R5、R6、Q、n和X-如上述通式(I)和(II)中的定义,R13选自C1-C6亚烷基,优选是亚乙基。wherein R 5 , R 6 , Q, n and X - are as defined in the above general formulas (I) and (II), and R 13 is selected from C 1 -C 6 alkylene, preferably ethylene.
(f)上述季铵化合物的混合物。(f) Mixtures of the above quaternary ammonium compounds.
用于本发明中的优选的季铵成分是上述(b)部分中所描述的那些。具体地,优选上文中通式(II)所示的二酯和/或二酰胺季铵(DEQA)化合物。用于本发明中的优选的二酯是在通式(II)所示的化合物中R5、R6和X-如上文所定义并且Q是如下式所示的那些: Preferred quaternary ammonium ingredients for use in the present invention are those described in section (b) above. Specifically, diester and/or diamide quaternary ammonium (DEQA) compounds represented by the general formula (II) above are preferred. Preferred diesters for use in the present invention are those in compounds of general formula (II) in which R 5 , R 6 and X - are as defined above and Q is of the following formula:
用于本发明中的优选的二酰胺是在通式(II)所示的化合物中R5、R6和X-如上文所定义并且Q是如下式所示的那些: Preferred diamides for use in the present invention are those in compounds of general formula (II) in which R 5 , R 6 and X - are as defined above and Q is of the following formula:
适于用在本发明组合物中的优选的季铵化合物的实例是:N,N-二(低芥酸菜籽酰基-氧-乙基)-N,N-二甲基氯化铵、N,N-二(低芥酸菜籽酰基-氧-乙基)-N-甲基,N-(2-羟乙基)甲基硫酸铵、N,N-二(低芥酸菜籽酰基-氧-乙基)-N-甲基,N-(2-羟乙基)氯化铵以及它们的混合物。特别优选用于本发明中的是N,N-二(低芥酸菜籽酰基-氧-乙基)-N-甲基,N-(2-羟乙基)甲基硫酸铵。Examples of preferred quaternary ammonium compounds suitable for use in the compositions of the present invention are: N,N-di(lowerucanoyl-oxy-ethyl)-N,N-dimethylammonium chloride, N , N-di(canolanoyl-oxy-ethyl)-N-methyl, N-(2-hydroxyethyl)ammonium methylsulfate, N,N-di(canolanoyl- Oxy-ethyl)-N-methyl, N-(2-hydroxyethyl)ammonium chloride and mixtures thereof. Particularly preferred for use in the present invention is N,N-bis(lowerucinoyl-oxy-ethyl)-N-methyl,N-(2-hydroxyethyl)ammonium methylsulfate.
尽管优选衍生自″低芥酸菜籽酰基(canolyl)″脂肪酰基的季铵化合物,但其它适用的季铵化合物的实例是衍生自其中上述实例中的″低芥酸菜籽酰基″被下列代替的脂肪酰基:″牛油酰基、椰油酰基、棕榈酰基(palmyl)、月桂酰基、油酰基、蓖麻油酰基、硬脂酰基、棕榈酰基(palmityl)″替代,这些对应于衍生得到脂肪酰基单元的甘油三酯源。这些可供选择的脂肪酰基源可包含全饱和,或者优选至少部分不饱和的链。保湿剂Although quaternary ammonium compounds derived from "canolyl" fatty acyl groups are preferred, examples of other suitable quaternary ammonium compounds are those derived from "canolyl" in the above examples are replaced by Fatty acyl groups: "tallowoyl, cocoyl, palmityl (palmyl), lauroyl, oleoyl, ricinoleoyl, stearoyl, palmityl" substitutions, these correspond to the fatty acyl units derived from Source of triglycerides. These alternative fatty acyl sources may contain fully saturated, or preferably at least partially unsaturated chains. moisturizer
本发明组合物的第二种基本要素是其包含至少5%重量的保湿剂。在本发明种使用的术语“保湿剂(humectant)’是指可给皮肤带来保留水的好处的物质。优选,本发明组合物包含至少7.5%(重量),更优选至少10%(重量),还更优选至少15%(重量),进一步优选至少30%(重量)的保湿剂。A second essential element of the compositions of the present invention is that they contain at least 5% by weight of humectant. The term "humectant" used in the present invention refers to a substance that provides the skin with the benefit of retaining water. Preferably, the compositions of the present invention comprise at least 7.5% by weight, more preferably at least 10% by weight , still more preferably at least 15% by weight, still more preferably at least 30% by weight of humectant.
任何适用于化妆品组合物的保湿剂均可用于本发明。用于本发明的合适的保湿剂的非限定性实例披露于WO 98/22085、WO 98/18444和WO97/01326中。优选用于本发明的保湿剂选自,但不限于:氨基酸及其衍生物如脯氨酸和精氨酸天冬氨酸盐,1,3-丁二醇,丙二醇和水和海松属植物(codium tomentosum)提取物,胶原氨基酸或肽,肌氨酸酐,双甘油,生物多糖胶-1(biosaccharide gum-1),葡糖胺盐,葡糖醛酸盐,谷氨酸盐,甘油的聚乙二醇醚(例如甘油聚氧乙烯醚20),甘油,甘油单丙氧基化物,糖原,己二醇,蜂蜜,以及其提取物或衍生物,氢化淀粉水解产物,水解粘多糖,肌醇,角蛋白氨基酸,脲,LAREX A-200(得自Larex),糖胺聚糖,甲氧基PEG-10,甲基gluceth-10和-20(均可购自Amerchol,位于Edison,NJ),甲基葡萄糖,3-甲基-1,3-丁二醇,N-乙酰基葡糖胺盐,聚乙二醇及其衍生物(如PEG 15丁二醇,PEG 4,PEG 5季戊四醇,PEG 6,PEG 8,PEG 9),季戊四醇,1,2-戊二醇,PPG-1甘油醚,PPG-9,2-吡咯烷酮-5-羧酸及其盐如甘油基PCA,糖异构化物,SEACARE(得自Secma),丝胶,丝氨基酸,乙酰基透明质酸钠,透明质酸钠,聚天冬氨酸钠,聚谷氨酸钠,山梨醇聚氧乙烯醚(sorbeth)20,山梨醇聚氧乙烯醚6,糖和糖醇及其衍生物如葡萄糖,甘露糖和聚甘油山梨醇,海藻糖,三甘油,三羟甲基丙烷,三(羟甲基)氨基甲烷盐,酵母提取物,以及它们的混合物。Any humectant suitable for use in cosmetic compositions may be used in the present invention. Non-limiting examples of suitable humectants for use in the present invention are disclosed in WO 98/22085, WO 98/18444 and WO 97/01326. Moisturizers preferred for use in the present invention are selected from, but not limited to, amino acids and their derivatives such as proline and arginine aspartate, 1,3-butanediol, propylene glycol and water and sea pine ( codium tomentosum) extract, collagen amino acid or peptide, creatinine, diglycerin, biopolysaccharide gum-1 (biosaccharide gum-1), glucosamine salt, glucuronate, glutamic acid salt, polyethylene glycol of glycerol Glycol ethers (e.g. glycerol ethoxylate 20), glycerin, glycerol monopropoxylate, glycogen, hexylene glycol, honey, and its extracts or derivatives, hydrogenated starch hydrolysates, hydrolyzed mucopolysaccharides, inositol , keratin amino acids, urea, LAREX A-200 (from Larex), glycosaminoglycans, methoxy PEG-10, methylgluceth-10 and -20 (both available from Amerchol in Edison, NJ), Methylglucose, 3-methyl-1,3-butanediol, N-acetylglucosamine salt, polyethylene glycol and its derivatives (such as PEG 15 butanediol, PEG 4, PEG 5 pentaerythritol, PEG 6, PEG 8, PEG 9), pentaerythritol, 1,2-pentanediol, PPG-1 glyceryl ether, PPG-9, 2-pyrrolidone-5-carboxylic acid and its salts such as glyceryl PCA, sugar isomers, SEACARE (from Secma), sericin, silk amino acid, sodium acetyl hyaluronate, sodium hyaluronate, sodium polyaspartate, sodium polyglutamate, sorbeth 20, sorbitol Alcohol ethoxylates 6, sugars and sugar alcohols and their derivatives such as glucose, mannose and polyglycerol sorbitol, trehalose, triglycerin, trimethylolpropane, tris(hydroxymethyl)aminomethane salts, yeast extract substances, and their mixtures.
更优选,用于本发明的保湿剂选自:甘油,脲,丁二醇,聚乙二醇及其衍生物,以及它们的混合物。还更优选,用于本发明的保湿剂选自:甘油、脲和它们的混合物,特别是甘油。任选成分More preferably, the humectant used in the present invention is selected from the group consisting of glycerin, urea, butylene glycol, polyethylene glycol and derivatives thereof, and mixtures thereof. Even more preferably, the humectant used in the present invention is selected from the group consisting of glycerin, urea and mixtures thereof, especially glycerin. optional ingredients
本发明的组合物可包含各种任选组分,这些任选成分适于令本发明的组合物具有更宜人的美容或美化特性,或者给组合物带来了附加的使用益处。这些常用的任选成分是本领域普通技术人员所公知的。其中包括各种化妆品用成分,如在《(CTFA国际化妆品词典和手册》(CTFA InternationalCosmetic Ingredient Dictionary and Handbook,第7版,Wenninger和McEwen编,(The Cosmetic,Toiletry,and Fragrance Association,Inc.,Washington,D.C.,1997))中可以找到的那些。以下列出了这些任选成分中的某些非限定性实例。润肤剂The compositions of the present invention may contain various optional ingredients suitable to impart more pleasant cosmetic or aesthetic properties to the compositions of the present invention, or to impart additional use benefits to the compositions. These common optional ingredients are well known to those of ordinary skill in the art. These include various ingredients used in cosmetics as described in (CTFA International Cosmetic Ingredient Dictionary and Handbook, 7th Edition, edited by Wenninger and McEwen, (The Cosmetic, Toiletry, and Fragrance Association, Inc., Washington , D.C., 1997)). Some non-limiting examples of these optional ingredients are listed below. Emollients
本发明组合物中特别优选的任选成分是润肤剂(emollient)。润肤剂用于润滑皮肤、增进皮肤的光滑性和柔软性,预防和缓解皮肤干燥,并且/或者保护皮肤。各种合适的润肤剂是已知的并且可以用在本发明中。Sagarin所著的Cosmetics,Science and Technology(第2版,第1卷,32-43页(1972))中包括了众多适于用作润肤剂的物质的实例。优选,本发明的组合物包含大于1%(重量),更优选至少为5%(重量),还更优选至少为10%(重量)的润肤剂。A particularly preferred optional ingredient in the compositions of the present invention is an emollient. Emollients are used to lubricate the skin, improve the smoothness and suppleness of the skin, prevent and relieve dryness of the skin, and/or protect the skin. A variety of suitable emollients are known and can be used in the present invention. Cosmetics, Science and Technology by Sagarin, 2nd Edition, Vol. 1, pp. 32-43 (1972) contains numerous examples of materials suitable for use as emollients. Preferably, the compositions of the present invention comprise greater than 1% by weight, more preferably at least 5% by weight, even more preferably at least 10% by weight of emollient.
优选用于本发明的润肤剂选自:Preferred emollients for use herein are selected from:
i)具有约含7至约40个碳原子的直链或支链烃,如十二烷、角鲨烷、矿脂、胆甾醇和它们的衍生物、氢化聚异丁烯、异十六烷和C7-C40异链烷烃(为C7-C40支链烃)。i) straight or branched chain hydrocarbons having from about 7 to about 40 carbon atoms, such as dodecane, squalane, petrolatum, cholesterol and their derivatives, hydrogenated polyisobutene, isohexadecane and C 7 -C 40 isoparaffins (for C 7 -C 40 branched chain hydrocarbons).
ii)C1-C30羧酸和C2-C30二元羧酸的C1-C30醇酯,例如异壬酸异壬酯、肉豆蔻酸异丙酯、丙酸肉豆蔻酯、硬脂酸异丙酯、二十二烷酸二十二烷酯、马来酸二辛酯、己二酸二异丙酯以及二亚油酸二异丙酯。ii) C 1 -C 30 alcohol esters of C 1 -C 30 carboxylic acids and C 2 -C 30 dicarboxylic acids, such as isononyl isononanoate, isopropyl myristate, myristyl propionate, hard Isopropyl fatty acid, behenyl behenate, dioctyl maleate, diisopropyl adipate, and diisopropyl dilinoleate.
iii)C1-C30羧酸的单甘油酯、二甘油酯和三甘油酯及其乙氧基化衍生物。适用的甘油酯的聚乙二醇衍生物包括:PEG-20杏仁甘油酯、PEG-60杏仁甘油酯、PEG-11鳄梨甘油酯、PEG-6辛/癸酸甘油酯、PEG-8辛/癸酸甘油酯、PEG-20玉米甘油酯、PEG-60玉米甘油酯、PEG-60月见草油甘油酯、PEG-7甘油基椰油酯、PEG-30甘油基椰油酯、PEG-40甘油基椰油酯、PEG-78甘油基椰油酯、PEG-80甘油基椰油酯、PEG-12甘油基二油酸酯、PEG-15甘油基异硬脂酸酯、PEG-20甘油基异硬脂酸酯、PEG-30甘油基异硬脂酸酯、PEG-75可可脂甘油酯、PEG-20氢化棕榈油甘油酯、PEG-70芒果甘油酯、PEG-13貂油甘油酯、PEG-75娑罗双树脂甘油酯、PEG 10橄榄油甘油酯、PEG-12棕榈仁油甘油酯、PEG-45棕榈仁油甘油酯、PEG-8甘油基月桂酸酯和PEG-30甘油基月桂酸酯。甘油酯的聚乙二醇衍生物的混合物也可用于本发明。iii) Mono-, diglycerides and triglycerides of C 1 -C 30 carboxylic acids and their ethoxylated derivatives. Suitable polyethylene glycol derivatives of glycerides include: PEG-20 Almond Glycerides, PEG-60 Almond Glycerides, PEG-11 Avocado Glycerides, PEG-6 Caprylic/Capric Glycerides, PEG-8 Caprylic/Capric Glycerides Glyceryl Caprate, PEG-20 Corn Glycerides, PEG-60 Corn Glycerides, PEG-60 Evening Primrose Oil Glycerides, PEG-7 Glyceryl Cocoate, PEG-30 Glyceryl Cocoate, PEG-40 Glyceryl Cocoate, PEG-78 Glyceryl Cocoate, PEG-80 Glyceryl Cocoate, PEG-12 Glyceryl Dioleate, PEG-15 Glyceryl Isostearate, PEG-20 Glyceryl Isostearate, PEG-30 Glyceryl Isostearate, PEG-75 Cocoa Butter Glycerides, PEG-20 Hydrogenated Palm Glycerides, PEG-70 Mango Glycerides, PEG-13 Mink Glycerides, PEG -75 salicylate, PEG 10 olive oil glycerides, PEG-12 palm kernel oil glycerides, PEG-45 palm kernel oil glycerides, PEG-8 glyceryl laurate and PEG-30 glyceryl laurate ester. Mixtures of polyethylene glycol derivatives of glycerides are also useful in the present invention.
iv)C1-C30羧酸的亚烷基二醇酯,例如C1-C30羧酸的乙二醇单酯和二酯,以及丙二醇单酯和二酯,例如二硬脂酸乙二醇酯。iv) Alkylene glycol esters of C 1 -C 30 carboxylic acids, such as ethylene glycol monoesters and diesters of C 1 -C 30 carboxylic acids, and propylene glycol monoesters and diesters, such as ethylene glycol distearate alcohol esters.
v)有机聚硅氧烷油。有机聚硅氧烷油可以是挥发性的、非挥发性的或挥发性和非挥发性聚硅氧烷的混合物。本文中使用的术语“非挥发性的”是指在环境条件下为液体,并且闪点(1个大气压下)大于或等于约100℃的那些聚硅氧烷。本文中使用的术语“挥发性的”是指所有其它的聚硅氧烷油。适用的有机聚硅氧烷油可选自挥发性和粘度跨越较宽范围的各种聚硅氧烷。优选非挥发性聚硅氧烷。适用的聚硅氧烷披露于美国专利5,069,897(1991年12月3日授权)。优选用于本发明的有机聚硅氧烷选自聚烷基硅氧烷、烷基取代的聚二甲基硅氧烷、聚二甲基硅氧烷醇、聚烷基芳基硅氧烷及其混合物。更优选用于本发明的是聚烷基硅氧烷和环状聚甲基硅氧烷(cyclomethicone)。聚烷基硅氧烷中优选的是聚二甲基硅氧烷。v) Organopolysiloxane oils. The organopolysiloxane oil can be a volatile, nonvolatile or a mixture of volatile and nonvolatile silicones. As used herein, the term "nonvolatile" refers to those polysiloxanes which are liquids at ambient conditions and have a flash point (at 1 atmosphere) of greater than or equal to about 100°C. The term "volatile" as used herein refers to all other silicone oils. Suitable organopolysiloxane oils can be selected from a wide variety of silicones spanning a wide range in volatilities and viscosities. Non-volatile polysiloxanes are preferred. Suitable polysiloxanes are disclosed in US Patent 5,069,897 (issued December 3, 1991). Preferred organopolysiloxanes for use in the present invention are selected from the group consisting of polyalkylsiloxanes, alkyl-substituted polydimethylsiloxanes, dimethiconols, polyalkylarylsiloxanes and its mixture. More preferred for use herein are polyalkylsiloxanes and cyclomethicones. Preferred among the polyalkylsiloxanes are polydimethylsiloxanes.
vi)植物油和氢化植物油。植物油和氢化植物油的实例包括:红花油、蓖麻油、椰子油、棉籽油、鲱油、棕榈仁油、棕榈油、花生油、大豆油、菜子油、亚麻子油、米糠油、松油、芝麻油、葵花油、上述来源的油的部分氢化和全氢化形式,以及它们的混合物。vi) Vegetable oils and hydrogenated vegetable oils. Examples of vegetable and hydrogenated vegetable oils include: safflower oil, castor oil, coconut oil, cottonseed oil, menhaden oil, palm kernel oil, palm oil, peanut oil, soybean oil, rapeseed oil, linseed oil, rice bran oil, pine oil, sesame oil , sunflower oil, partially hydrogenated and fully hydrogenated forms of oils from the above sources, and mixtures thereof.
vii)动物油脂,例如鳕鱼肝油、羊毛脂及其衍生物,如乙酰化羊毛脂和羊毛酸异丙酯。优选羊毛脂油。vii) Animal fats such as cod liver oil, lanolin and its derivatives such as acetylated lanolin and isopropyl lanolate. Lanolin oil is preferred.
viii)可以使用的还有聚丙二醇的C4-C20烷基醚、聚丙二醇的C1-C20羧酸酯以及二-C8-C30烷基醚,实例包括PPG-14丁基醚、PPG-15硬脂基醚、二辛基醚、十二烷基辛基醚及其混合物。viii) Also C 4 -C 20 alkyl ethers of polypropylene glycol, C 1 -C 20 carboxylic acid esters of polypropylene glycol and di-C 8 -C 30 alkyl ethers can be used, examples include PPG-14 butyl ether , PPG-15 stearyl ether, dioctyl ether, dodecyl octyl ether and mixtures thereof.
ix)羧酸多元醇酯。ix) Polyol carboxylic acid esters.
x)上述成分的混合物。x) Mixtures of the above ingredients.
优选用于本发明中的润肤剂选自:十二烷、角鲨烷、胆甾醇及其衍生物、异十六烷、异壬酸异壬酯、矿脂、羊毛脂及其衍生物、红花油、蓖麻油、椰子油、棉籽油、棕榈仁油、棕榈油、花生油、大豆油、羧酸多元醇酯以及它们的混合物。更优选用于本发明的润肤剂选自羧酸多元醇酯、矿脂以及它们的混合物。Emollients preferably used in the present invention are selected from the group consisting of dodecane, squalane, cholesterol and its derivatives, isohexadecane, isononyl isononanoate, petrolatum, lanolin and its derivatives, Safflower oil, castor oil, coconut oil, cottonseed oil, palm kernel oil, palm oil, peanut oil, soybean oil, polyol carboxylic acid esters and mixtures thereof. More preferred emollients for use herein are selected from polyol carboxylic acid esters, petrolatum, and mixtures thereof.
这些酯衍生自糖或多元醇部分和一种或多种羧酸部分。取决于构成的酸和糖,这些酯在室温条件下可以是液体或固体形式。液体酯的实例包括:四油酸葡糖酯、大豆油脂肪酸(不饱和)的葡糖四酯、混和的大豆油脂肪酸的甘露糖四酯、油酸的半乳糖四酯、亚油酸的阿拉伯糖四酯、木糖四亚油酸酯、五油酸半乳糖酯、四油酸山梨糖醇酯、不饱和大豆油脂肪酸的山梨醇六酯、五油酸木糖醇酯、四油酸蔗糖酯、五油酸蔗糖酯、六油酸蔗糖酯、七油酸蔗糖酯、八油酸蔗糖酯及其混合物。固体酯的实例包括:山梨醇六酯,其中的羧酸酯部分是摩尔比为1∶2的棕榈油酸酯和花生酸酯;棉子糖的八酯,其中的羧酸酯部分是摩尔比为1∶3的亚油酸酯和二十二烷酸酯;麦芽糖的七酯,其中酯化用羧酸部分是摩尔比为3∶4的葵花子油脂肪酸和二十四烷酸酯;蔗糖的八酯,其中酯化用羧酸部分是摩尔比为2∶6的油酸酯和二十二烷酸酯;以及蔗糖的八酯,其中酯化用羧酸部分是摩尔比为1∶3∶4的月桂酸酯、亚油酸酯和二十二烷酸酯。优选的固体物质是蔗糖聚酯,其中酯化度为7-8,并且其中的脂肪酸部分是C18单-和/或二-不饱和酸和二十二烷酸,其中不饱和酸和二十二烷酸的摩尔比为1∶7-3∶5。特别优选的固体糖聚酯是蔗糖的八酯,其中分子中约含7个二十二碳脂肪酸部分和约1个油酸部分。其它包括棉籽油或大豆油脂肪酸蔗糖酯。这些酯类物质还披露于美国专利2,831,854;美国专利4,005,196(Jandacek,1977年1月25日授权);美国专利4,005,195(Jandacek,1977年1月25日授权),美国专利5,306,516(Letton等人,1994年4月26日授权);美国专利5,306,515(Letton等人,1994年4月26日授权);美国专利5,305,514(Letton等人,1994年4月26日授权);美国专利4,797,300(Jandacek等人,1989年1月10日授权);美国专利3,963,699(Rizzi等人,1976年6月15日授权);美国专利4,518,772(Volpenhein,1985年5月21日授权);以及美国专利4,517,360(Volpenhein,1985年5月21日授权)。These esters are derived from a sugar or polyol moiety and one or more carboxylic acid moieties. Depending on the constituent acids and sugars, these esters can be in liquid or solid form at room temperature. Examples of liquid esters include: glucose tetraoleate, glucose tetraester of soy fatty acid (unsaturated), mannose tetraester of mixed soy fatty acid, galactose tetraester of oleic acid, arabic acid tetraester of linoleic acid Sugar tetraester, xylose tetralinoleate, galactose pentaoleate, sorbitan tetraoleate, sorbitan hexaester of unsaturated soybean oil fatty acid, xylitol pentaoleate, sucrose tetraoleate esters, sucrose pentaoleate, sucrose hexaoleate, sucrose heptaoleate, sucrose octaoleate and mixtures thereof. Examples of solid esters include: sorbitan hexaester, in which the carboxylate moieties are palm oleate and arachidic in a molar ratio of 1:2; octaester of raffinose, in which the carboxylate moieties are Linoleate and behenate in a ratio of 1:3; heptaester of maltose, wherein the carboxylic acid moiety for esterification is sunflower oil fatty acid and tetracosanoate in a molar ratio of 3:4; sucrose octaesters in which the carboxylic acid moieties for esterification are oleate and behenate in a molar ratio of 2:6; and octaesters of sucrose in which the carboxylic acid moieties for esterification are in a molar ratio of 1:3: 4 laurate, linoleate and behenate. A preferred solid material is sucrose polyester, wherein the degree of esterification is 7-8, and wherein the fatty acid moieties are C 18 mono- and/or di-unsaturated acids and behenic acid, wherein the unsaturated acids and eicosanoids The molar ratio of dioxoic acid is 1:7-3:5. A particularly preferred solid sugar polyester is the octaester of sucrose having about 7 behenic fatty acid moieties and about 1 oleic acid moiety in the molecule. Others include cottonseed oil or soybean oil fatty acid sucrose esters. These esters are also disclosed in U.S. Patent 2,831,854; U.S. Patent 4,005,196 (Jandacek, authorized on January 25, 1977); April 26, 1994); U.S. Patent 5,306,515 (Letton et al., April 26, 1994); U.S. Patent 5,305,514 (Letton et al., April 26, 1994); U.S. Patent 4,797,300 (Jandacek et al., issued January 10, 1989); US Patent 3,963,699 (Rizzi et al., issued June 15, 1976); US Patent 4,518,772 (Volpenhein, issued May 21, 1985); and US Patent 4,517,360 (Volpenhein, Authorized on 21 May 1985).
适用于本发明的多元醇脂肪酸多元酯可通过本领域已知的各种方法进行制备。这些方法包括采用各种催化剂由多元醇与甲基、乙基或甘油基脂肪酸酯进行酯交换;采用脂肪酰氯对多元醇进行酰化作用;采用脂肪酸酐对多元醇进行酰化作用;以及公知的采用脂肪酸对多元醇进行酰化作用。例如可参见美国专利2,831,854;美国专利4,005,196(Jandacek,1977年1月25日授权)中所述的内容。Polyol fatty acid polyesters suitable for use in the present invention can be prepared by various methods known in the art. These methods include the transesterification of polyols with methyl, ethyl or glyceryl fatty acid esters using various catalysts; the acylation of polyols with fatty acid chlorides; the acylation of polyols with fatty acid anhydrides; and the known The acylation of polyols with fatty acids. See, for example, US Patent 2,831,854; US Patent 4,005,196 (Jandacek, issued January 25, 1977).
特别优选的材料是INCI命名为聚棉籽油酸蔗糖酯的材料。其它皮肤有益成分A particularly preferred material is that which has the INCI designation polysucrose cottonseedoleate. Other Skin Benefits
本发明组合物中可采用其它皮肤有益成分。可以用于本发明组合物的其它皮肤有益成分的实例包括:Other skin benefit ingredients may be employed in the compositions of the present invention. Examples of other skin benefit ingredients that may be used in the compositions of the present invention include:
(a)维生素化合物(a) vitamin compounds
本发明组合物中可含有维生素化合物、其前体及其衍生物。这些维生素化合物可以是天然形式,也可以是合成形式的。适用的维生素化合物包括:维生素A(例如,β-胡萝卜素、视黄酸、视黄醇、视黄醛类衍生物(retinoids)、棕榈酸视黄醇酯、丙酸视黄醇酯等)、维生素B(例如,烟酸、烟酰胺、核黄素、泛酸等)、维生素C(例如,抗坏血酸等)、维生素D(例如,麦角甾醇、麦角钙化醇、胆钙化甾醇等)、维生素E(例如,乙酸生育酚等)以及维生素K(例如,植物甲萘醌、甲萘醌、结核菌萘醌等)化合物。优选用于本发明组合物中的维生素化合物是维生素B3化合物。维生素B3化合物特别适用于调节皮肤状况,有关内容披露于WO-A-97/39733中。如果使用维生素化合物,则本发明组合物中优选包含约0.01%(重量)至约50%(重量),更优选约0.1%(重量)至约10%(重量),还更优选约为0.5%(重量)至约5%(重量)的维生素B3化合物。Vitamin compounds, their precursors and their derivatives may be included in the compositions of the present invention. These vitamin compounds can be in natural or synthetic form. Suitable vitamin compounds include vitamin A (e.g., beta-carotene, retinoic acid, retinol, retinoids, retinyl palmitate, retinyl propionate, etc.), Vitamin B (for example, niacin, niacinamide, riboflavin, pantothenic acid, etc.), vitamin C (for example, ascorbic acid, etc.), vitamin D (for example, ergosterol, ergocalciferol, cholecalciferol, etc.), vitamin E (for example, , tocopheryl acetate, etc.) and vitamin K (eg, phytonadione, menadione, tuberculone naphthoquinone, etc.) compounds. A preferred vitamin compound for use in the compositions of the present invention is a vitamin B3 compound. Vitamin B3 compounds are particularly useful for regulating skin condition and are disclosed in WO-A-97/39733. If vitamin compounds are used, they preferably comprise from about 0.01% by weight to about 50% by weight, more preferably from about 0.1% by weight to about 10% by weight, still more preferably about 0.5% by weight (weight) to about 5% (weight) vitamin B3 compound.
用于本发明的术语″维生素B3化合物″是指具有下式的化合物: The term "vitamin B3 compound" as used in the present invention refers to a compound having the following formula:
其中R是-CONH2(即烟酰胺)、-COOH(即烟酸)或-CH2OH(即烟基醇(nicotinyl alcohol));其衍生物;以及上述化合物的盐。Wherein R is -CONH 2 (ie nicotinamide), -COOH (ie nicotinic acid) or -CH 2 OH (ie nicotinyl alcohol); derivatives thereof; and salts of the above compounds.
上述维生素B3化合物的衍生物的实例包括:烟酸酯,包括烟酸的非血管扩张性酯;烟基氨基酸、羧酸的烟基醇酯、烟酸N-氧化物和烟酰胺N-氧化物。Examples of derivatives of the aforementioned vitamin B3 compounds include: nicotinic acid esters, including non-vasodilatory esters of nicotinic acid; nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide, and nicotinamide N-oxide things.
合适的维生素B3化合物的实例是本领域公知的,并且可从多个来源购得,例如Sigma化学品公司(St.Louis,MO);ICN生物医学公司(Irvin,CA)和Aldrich化学品公司(Milwaukee,WI)。Examples of suitable vitamin B3 compounds are well known in the art and are commercially available from a variety of sources such as Sigma Chemical Company (St. Louis, MO); ICN Biomedical Company (Irvin, CA) and Aldrich Chemical Company (Milwaukee, WI).
维生素化合物可基本以纯品的形式加入,或以由天然来源(例如植物)经合适的物理和/或化学方法分离得到提取物的形式加入。The vitamin compound may be added in substantially pure form, or in the form of an extract obtained by suitable physical and/or chemical isolation from a natural source, such as a plant.
(b)抗皱和抗皮肤萎缩活性成分(b) Anti-wrinkle and anti-skin atrophy active ingredients
可用于本发明组合物中的抗皱(anti-winkle)和抗皮肤萎缩(anti-skinatrophy)活性成分的实例包括,但不限于:乳酸及其衍生物;视黄酸及其衍生物(例如顺式的和反式的);视黄醇;视黄酯;烟酰胺;水杨酸及其衍生物;含硫的D和L氨基酸及其衍生物和盐,特别是N-乙酰基衍生物,其中优选的实例是N-乙酰基-L-半胱氨酸;硫醇类,例如,乙硫醇;羟基酸;肌醇六磷酸;硫辛酸;溶血磷脂酸,以及去皮剂(skin peel agent)(例如,酚类等)。Examples of anti-winkle and anti-skinatrophy active ingredients that may be used in the compositions of the present invention include, but are not limited to: lactic acid and its derivatives; retinoic acid and its derivatives (e.g. cis and trans); retinol; retinyl esters; nicotinamide; salicylic acid and its derivatives; sulfur-containing D and L amino acids and their derivatives and salts, especially N-acetyl derivatives, where Preferred examples are N-acetyl-L-cysteine; thiols, e.g., ethanethiol; hydroxy acids; phytic acid; lipoic acid; lysophosphatidic acid, and skin peel agents (eg, phenols, etc.).
(c)抗微生物和抗真菌活性成分(c) Antimicrobial and antifungal active ingredients
可以用于本发明组合物中的抗微生物和抗真菌活性成分的实例包括:β-内酰胺类药物、喹诺酮类药物、环丙氟哌酸、诺氟沙星、四环素、红霉素、丁胺卡那霉素、2,4,4′-三氯-2′-羟基二苯基醚、3,4,4′-三氯-N-碳酰苯胺、苯氧基乙醇、苯氧基丙醇、苯氧基异丙醇、多西环素、卷曲霉素、洗必太、金霉素、土霉素、氯林可霉素、乙胺丁醇、羟乙磺酸己氧苯脒、甲硝唑、戊氧苯脒、庆大霉素、卡那霉素、林可霉素(lineomycin)、甲烯土霉素、乌洛托品、二甲胺四环素(minocycline)、新霉素、奈替米星、巴龙霉素、链霉素、妥布霉素、咪康唑、盐酸四环素、红霉素、红霉素锌、无味红霉素、红霉素硬脂酸酯、硫酸阿米卡星、盐酸多西环素、硫酸卷曲霉素、葡萄糖酸洗必太、盐酸洗必太、盐酸金霉素、盐酸土霉素、盐酸氯林可霉素、盐酸乙胺丁醇、盐酸甲硝唑、盐酸戊氧苯脒、硫酸庆大霉素、硫酸卡那霉素、盐酸林可霉素(lineomycin)、盐酸甲烯土霉素、马尿酸乌洛托品、孟德立胺、盐酸二甲胺四环素、硫酸新霉素、硫酸奈替米星、硫酸巴龙霉素、硫酸链霉素、硫酸妥布霉素、盐酸咪康唑、盐酸金刚烷胺(amanfadine hydrochloride)、硫酸金刚烷胺(amanfadine sulfate)、羟甲辛吡酮、对氯间二甲酚、制霉菌素、托萘酯(tolnaftate)、羟基吡啶硫酮锌和克霉唑。Examples of antimicrobial and antifungal active ingredients that may be used in the compositions of the present invention include: beta-lactams, quinolones, ciprofloxacin, norfloxacin, tetracycline, erythromycin, butylamine Kanamycin, 2,4,4'-trichloro-2'-hydroxydiphenyl ether, 3,4,4'-trichloro-N-carbanilide, phenoxyethanol, phenoxypropanol , phenoxyisopropanol, doxycycline, capreomycin, chlorhexidine, chlortetracycline, oxytetracycline, clindamycin, ethambutol, hexamidine isethionate, formazan Nitazole, pentamidine, gentamicin, kanamycin, lincomycin, methacycline, urotropine, minocycline, neomycin, naphthalene Tilmicin, paromomycin, streptomycin, tobramycin, miconazole, tetracycline hydrochloride, erythromycin, erythromycin zinc, odorless erythromycin, erythromycin stearate, amisulfate Cathin, doxycycline hydrochloride, capreomycin sulfate, chlorhexidine gluconate, chlorhexidine hydrochloride, aureomycin hydrochloride, oxytetracycline hydrochloride, clindamycin hydrochloride, ethambutol hydrochloride, formazan hydrochloride Nitazole, pentamidine hydrochloride, gentamycin sulfate, kanamycin sulfate, lincomycin hydrochloride (lineomycin), methacycline hydrochloride, urotropine hippurate, mendelidine, dimethyl hydrochloride Minocycline, neomycin sulfate, netilmicin sulfate, paromomycin sulfate, streptomycin sulfate, tobramycin sulfate, miconazole hydrochloride, amanfadine hydrochloride (amanfadine hydrochloride), amantadine sulfate ( amanfadine sulfate), octopyrone, chloroxylenol, nystatin, tolnaftate, zinc pyrithione, and clotrimazole.
(d)防晒活性成分(d) Sunscreen Active Ingredients
本发明的组合物中还可以包含防晒活性成分。各种防晒剂均可用在本发明中。这些防晒剂包括有机化合物及其盐以及无机颗粒材料。尽管不希望受到理论的限制,但相信防晒剂可通过下述的一种或多种机理保护皮肤防止受紫外线辐射,包括:吸收、散射和反射紫外辐射。这些防晒剂的非限定性实例披露于:美国专利5,087,445(Haffey等人,1992年2月11日授权);美国专利5,073,372(Turner等人,1991年12月17日授权);美国专利5,073,371(Turner等人,1991年12月17日授权);美国专利5,160,731(Sabatelli等人,1992年11月3日授权);美国专利5,138,089(Sabatelli,1992年8月11日授权);美国专利5,041,282(Sabatelli,1991年8月20日授权);美国专利4,999,186(Sabatelli等人,1991年3月12日授权);美国专利4,937,370(Sabatelli,1990年6月26日授权);以及Segarin等人在《化妆品科学与技术》(Cosmetics Science and Technology,第VIII章,189页以下)所述的内容。其中,优选的防晒剂选自:对甲氧基肉桂酸2-乙基己酯、水杨酸辛酯、氰双苯丙烯酸辛酯、羟基甲氧基二苯甲酮、N,N-二甲基氨基苯甲酸2-乙基己酯、对氨基苯甲酸、2-苯基-苯并咪唑-5-磺酸、水杨酸高孟酯、对甲氧基肉桂酸二乙醇胺、4,4′-甲氧基-叔丁基二苯甲酰甲烷、4-异丙基二苯甲酰甲烷、3-(4-甲基亚苄基)樟脑、3-亚苄基樟脑、4-N,N-二甲氨基苯甲酸与2,4-二羟基二苯酮的酯、4-N,N-二甲氨基苯甲酸与2-羟基-4-(2-羟基乙氧基)二苯酮的酯、4-N,N-二甲氨基苯甲酸与4-羟基二苯甲酰基甲烷的酯、4-N,N-二甲氨基苯甲酸与4-(2-羟基乙氧基)二苯甲酰基甲烷的酯、4-N,N-二(2-乙基己基)-氨基苯甲酸与2,4-二羟基二苯酮的酯、4-N,N-二(2-乙基己基)氨基苯甲酸与2-羟基-4-(2-羟基乙氧基)二苯酮的酯、4-N,N-二(2-乙基己基)氨基苯甲酸与4-羟基二苯甲酰基甲烷的酯、4-N,N-二(2-乙基己基)氨基苯甲酸与4-(2-羟基乙氧基)二苯甲酰基甲烷的酯、4-N,N-(2-乙基己基)甲基氨基苯甲酸与2,4-二羟基二苯酮的酯、4-N,N-(2-乙基己基)甲基氨基苯甲酸与2-羟基-4-(2-羟基乙氧基)二苯酮的酯、4-N,N-(2-乙基己基)甲基氨基苯甲酸与4-羟基二苯甲酰基甲烷的酯、4-N,N-(2-乙基己基)甲基氨基苯甲酸与4-(2-羟基乙氧基)二苯甲酰基甲烷的酯、二氧化钛、氧化锌、氧化铁及其混合物。Sunscreen actives may also be included in the compositions of the present invention. A variety of sunscreens can be used in the present invention. These sunscreens include organic compounds and their salts as well as inorganic particulate materials. While not wishing to be bound by theory, it is believed that sunscreens protect the skin from UV radiation by one or more of the following mechanisms, including absorbing, scattering and reflecting UV radiation. Non-limiting examples of these sunscreens are disclosed in: US Patent 5,087,445 (Haffey et al., issued February 11, 1992); US Patent 5,073,372 (Turner et al., issued December 17, 1991); US Patent 5,073,371 (Turner et al. et al., authorized on December 17, 1991); U.S. Patent 5,160,731 (Sabatelli et al., authorized on November 3, 1992); U.S. Patent 5,138,089 (Sabatelli, authorized on August 11, 1992); August 20, 1991); U.S. Patent 4,999,186 (Sabatelli et al., March 12, 1991); U.S. Patent 4,937,370 (Sabatelli, June 26, 1990); and Segarin et al. Technology" (Cosmetics Science and Technology, Chapter VIII, page 189 below). Among them, the preferred sunscreen is selected from: 2-ethylhexyl p-methoxycinnamate, octyl salicylate, octocrylene, hydroxymethoxybenzophenone, N,N-dimethyl 2-ethylhexyl aminobenzoate, p-aminobenzoic acid, 2-phenyl-benzimidazole-5-sulfonic acid, homomenthyl salicylate, diethanolamine p-methoxycinnamate, 4,4'- Methoxy-tert-butyldibenzoylmethane, 4-isopropyldibenzoylmethane, 3-(4-methylbenzylidene)camphor, 3-benzylidenecamphor, 4-N,N- Esters of dimethylaminobenzoic acid and 2,4-dihydroxybenzophenone, esters of 4-N,N-dimethylaminobenzoic acid and 2-hydroxy-4-(2-hydroxyethoxy)benzophenone, Esters of 4-N,N-dimethylaminobenzoic acid and 4-hydroxydibenzoylmethane, 4-N,N-dimethylaminobenzoic acid and 4-(2-hydroxyethoxy)dibenzoylmethane Esters of 4-N,N-bis(2-ethylhexyl)-aminobenzoic acid and 2,4-dihydroxybenzophenone, 4-N,N-bis(2-ethylhexyl)aminobenzene Esters of formic acid and 2-hydroxy-4-(2-hydroxyethoxy)benzophenone, esters of 4-N,N-bis(2-ethylhexyl)aminobenzoic acid and 4-hydroxydibenzoylmethane , 4-N,N-bis(2-ethylhexyl)aminobenzoic acid and 4-(2-hydroxyethoxy)dibenzoylmethane ester, 4-N,N-(2-ethylhexyl) Esters of methylaminobenzoic acid and 2,4-dihydroxybenzophenone, 4-N,N-(2-ethylhexyl)methylaminobenzoic acid and 2-hydroxy-4-(2-hydroxyethoxy ) Esters of benzophenone, esters of 4-N,N-(2-ethylhexyl)methylaminobenzoic acid and 4-hydroxydibenzoylmethane, 4-N,N-(2-ethylhexyl) Esters of methylaminobenzoic acid and 4-(2-hydroxyethoxy)dibenzoylmethane, titanium dioxide, zinc oxide, iron oxide and mixtures thereof.
更优选用于本发明组合物中的防晒剂选自:N,N-二甲基-对氨基苯甲酸2-乙基己酯、对甲氧基肉桂酸2-乙基己酯、氰双苯丙烯酸辛酯、水杨酸辛酯、水杨酸高孟酯、对氨基苯甲酸、羟基甲氧基二苯甲酮、2-苯基苯并咪唑-5-磺酸、对甲氧基肉桂酸二乙醇胺、4,4′-甲氧基-叔丁基二苯甲酰基甲烷、4-异丙基二苯甲酰基甲烷、3-(4-甲基亚苄基)樟脑、3-亚苄基樟脑、4-N,N-(2-乙基己基)甲基氨基苯甲酸与4-(2-羟基乙氧基)二苯甲酰基甲烷的酯、二氧化钛、氧化锌、氧化铁及其混合物。More preferred sunscreens for use in the compositions of the present invention are selected from the group consisting of: N,N-dimethyl-p-aminobenzoic acid 2-ethylhexyl, p-methoxycinnamic acid 2-ethylhexyl, cyandiphenyl Octyl acrylate, octyl salicylate, homomenthyl salicylate, p-aminobenzoic acid, hydroxymethoxybenzophenone, 2-phenylbenzimidazole-5-sulfonic acid, p-methoxycinnamic acid di Ethanolamine, 4,4'-methoxy-tert-butyldibenzoylmethane, 4-isopropyldibenzoylmethane, 3-(4-methylbenzylidene)camphor, 3-benzylidenecamphor , esters of 4-N,N-(2-ethylhexyl)methylaminobenzoic acid and 4-(2-hydroxyethoxy)dibenzoylmethane, titanium dioxide, zinc oxide, iron oxide and mixtures thereof.
能够应用的防晒剂的确切用量取决于所选择的防晒剂和所要达到的防晒因子(Sun Protection Factor,SPF)值而有所不同。SPF是通常使用的,用于衡量防晒剂防止产生皮肤红斑的光保护作用。参见Federal Register,43卷,166号,38206-38269页,1978年8月25日。增稠剂The exact amount of sunscreen that can be applied varies depending on the sunscreen chosen and the Sun Protection Factor (SPF) value to be achieved. SPF is commonly used to measure the photoprotective effect of a sunscreen against skin erythema. See Federal Register, Vol. 43, No. 166, pp. 38206-38269, August 25, 1978. thickener
本发明组合物优选含有增稠剂。适用于化妆品组合物的各种增稠剂均可用于本发明。优选的增稠剂选自非离子水溶性聚合物、脂肪醇及其混合物。适用的非离子聚合物包括这样的水溶性聚合物,如纤维素醚(例如羟丁基甲基纤维素、羟丙基纤维素、羟丙基甲基纤维素、乙基羟乙基纤维素、经疏水改性的羟乙基纤维素以及羟乙基纤维素)、聚(氧乙烯)、聚乙烯醇、聚乙烯基吡咯烷酮、羟丙基瓜耳胶、直链淀粉(amulose)、羟乙基直链淀粉(amylose)、淀粉和淀粉衍生物。适用的脂肪醇是具有以下通式的较高分子量的、非挥发性的伯醇:The compositions of the invention preferably contain a thickener. Various thickeners suitable for use in cosmetic compositions can be used in the present invention. Preferred thickeners are selected from nonionic water soluble polymers, fatty alcohols and mixtures thereof. Suitable nonionic polymers include such water-soluble polymers as cellulose ethers (e.g., hydroxybutylmethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, ethylhydroxyethylcellulose, hydrophobically Modified hydroxyethyl cellulose and hydroxyethyl cellulose), poly(oxyethylene), polyvinyl alcohol, polyvinylpyrrolidone, hydroxypropyl guar gum, amylose (amulose), hydroxyethyl linear Starch (amylose), starch and starch derivatives. Suitable fatty alcohols are relatively high molecular weight, non-volatile primary alcohols having the general formula:
RCH2OHRCH 2 OH
其中R是C8-20烷基。它们可由天然油或脂制得,通过将脂肪酸的-COOH羧基还原成羟基官能基而得到。或者,可由本领域已知的常规方法制备相同或类似结构的脂肪醇。合适的脂肪醇包括:二十二烷醇、C9-C11醇、C12-C13醇、C12-C15醇、C12-C14醇、C14-C15醇、辛醇、鲸蜡/硬脂醇、椰油醇、癸醇、异鲸蜡醇、异硬脂醇、月桂醇、油醇、棕榈仁醇、硬脂醇、鲸蜡醇、牛油醇、十三烷醇或肉豆蔻醇,但并非只限于这些。极性溶剂Wherein R is C 8-20 alkyl. They can be obtained from natural oils or fats by reducing the -COOH carboxyl groups of fatty acids to hydroxyl functional groups. Alternatively, fatty alcohols of the same or similar structure can be prepared by conventional methods known in the art. Suitable fatty alcohols include: docosanol, C 9 -C 11 alcohols, C 12 -C 13 alcohols, C 12 -C 15 alcohols, C 12 -C 14 alcohols, C 14 -C 15 alcohols, octanol, Cetyl/Stearyl Alcohol, Coco Alcohol, Decyl Alcohol, Isocetyl Alcohol, Isostearyl Alcohol, Lauryl Alcohol, Oleyl Alcohol, Palm Kernel Alcohol, Stearyl Alcohol, Cetyl Alcohol, Tallow Alcohol, Tridecyl Alcohol or myristyl alcohol, but not limited to these. polar solvent
本发明的组合物中还可以包含极性溶剂。任何适于用在化妆品组合物中的极性溶剂均可以用在本发明中。但该极性溶剂必须具有足够的极性以促使形成本发明中的小泡。优选用于本发明组合物中的极性溶剂是水。Polar solvents may also be included in the compositions of the present invention. Any polar solvent suitable for use in cosmetic compositions may be used in the present invention. However, the polar solvent must be sufficiently polar to promote the formation of vesicles in the present invention. A preferred polar solvent for use in the compositions of the present invention is water.
本发明的组合物中优选含有10%-90%,更优选为20%-80%,还更优选为30%-60%(重量)的极性溶剂。其它任选成分The composition of the present invention preferably contains 10%-90%, more preferably 20%-80%, even more preferably 30%-60% by weight of polar solvent. other optional ingredients
本发明组合物中能够含有各种其它的任选的组分。这些附加组分应是可药用的。按功能性分类,适用于本发明组合物中的成分的非限定性实例包括:研磨剂、吸收剂、抗痤疮活性成分、防结块剂、去头屑剂、抑汗剂、抗氧剂、抗病毒活性成分、人工晒黑剂和促进剂、生物添加剂、漂白剂、漂白活化剂、增白剂、增效剂、缓冲剂、螯合剂、化学添加剂、着色剂、美容成分、清洁剂、化妆品用收敛剂、化妆品用杀菌剂、改性剂、除臭剂、脱皮活性成分、脱毛剂、药用收敛剂、染料、转染剂、酶、外用镇痛剂、发泡剂、矫味剂、成膜剂、香料组分、驱虫剂、防霉剂、非甾族抗炎活性成分、遮光剂、氧化染料、氧化剂、除虫成分、pH调节剂如柠檬酸、pH缓冲剂、药物活性成分、增塑剂、防腐剂、自由基清除剂、皮肤或头发或指甲漂白剂、皮肤或头发或指甲调理剂、皮肤或头发或指甲渗透促进剂、稳定剂、表面活性剂、表面调理剂、还原剂、温度抑制剂、粘度调节剂以及增温剂如发热沸石。还可用于本发明的是美化组分(aesthetic components)如:着色剂、香精油、皮肤愈合剂。其它适用于此的任选材料包括:颜料。适用于本发明组合物的颜料可以是有机和/或无机成分。在术语颜料范围内还包括低着色或低光泽物质,如消光涂饰剂,以及光散射剂。适用的颜料的实例有氧化铁、酰基谷氨酸氧化铁、二氧化钛、群青、D&C染料、胭脂虫红及其混合物。配制方法Various other optional ingredients can be included in the compositions of the present invention. These additional components should be pharmaceutically acceptable. Non-limiting examples of ingredients suitable for use in the compositions of the present invention, classified by function, include: abrasives, absorbents, anti-acne actives, anti-caking agents, anti-dandruff agents, antiperspirants, antioxidants, Antiviral active ingredients, artificial tanning agents and accelerators, biological additives, bleaching agents, bleach activators, brighteners, boosters, buffers, chelating agents, chemical additives, coloring agents, cosmetic ingredients, cleaning agents, cosmetics Astringents, fungicides for cosmetics, modifiers, deodorants, peeling active ingredients, depilatory agents, medicinal astringents, dyes, transfection agents, enzymes, topical analgesics, foaming agents, flavoring agents, Film formers, fragrance components, insect repellants, antifungal agents, non-steroidal anti-inflammatory active ingredients, sunscreens, oxidation dyes, oxidizing agents, insecticidal ingredients, pH regulators such as citric acid, pH buffers, pharmaceutical active ingredients , plasticizers, preservatives, free radical scavengers, skin or hair or nail bleaching agents, skin or hair or nail conditioners, skin or hair or nail penetration enhancers, stabilizers, surfactants, surface conditioners, reducing additives, temperature depressants, viscosity regulators and warming agents such as heating zeolites. Also useful in the present invention are aesthetic components such as: colorants, essential oils, skin healing agents. Other optional materials suitable for use herein include: Pigments. Pigments suitable for use in the compositions of the present invention may be organic and/or inorganic components. Also included within the term pigments are low-pigmentation or low-gloss substances, such as matt finishes, and light-scattering agents. Examples of suitable pigments are iron oxides, iron oxides acyl glutamate, titanium dioxide, ultramarine blue, D&C dyes, cochineal and mixtures thereof. Preparation method
优选本发明的组合物以季铵化合物可形成小泡的方式制备。优选所述小泡中还含有保湿剂。优选,所述小泡中还包含润肤剂。为确保最佳性能特性,优选本发明组合物由以下步骤制备:Preferably the compositions of the present invention are prepared in such a way that the quaternary ammonium compound can form vesicles. Preferably, the vesicles also contain a humectant. Preferably, the vesicles also contain an emollient. To ensure optimum performance characteristics, it is preferred that the compositions of the present invention are prepared by the following steps:
(i)在高于季铵成分熔点的温度下将全部或部分季铵成分与保湿剂、水溶性护肤活性成分(如果包含的话),优选还有极性溶剂相互混合;(i) intermixing all or part of the quaternary ammonium ingredient with the humectant, water-soluble skin care active (if included), and preferably a polar solvent at a temperature above the melting point of the quaternary ammonium ingredient;
(ii)任选地,剧烈搅拌该混合物;(ii) optionally vigorously stirring the mixture;
(iii)在另一单独容器中按如下方法制备乳剂:在高于季铵化合物熔点的温度下将含润肤剂的油相、有关的增稠剂(在所述的增稠剂是油溶性的情况下)和剩余的季铵成分混合在一起。单独制备水相。将水、有关的增稠剂(在所述的增稠剂是水溶性的情况下)和其它水溶性成分加热至与油相相同的温度。(iii) In a separate vessel, an emulsion is prepared by mixing the oily phase containing the emollient, the associated thickener (where the thickener is oil-soluble) at a temperature above the melting point of the quaternary ammonium compound, case) mixed with the remaining quaternary ammonium ingredients. Prepare the aqueous phase separately. Water, associated thickeners (where said thickeners are water soluble) and other water soluble ingredients are heated to the same temperature as the oil phase.
(iv)将乳剂的油相和水相的温度大致平衡,然后在搅拌条件下将水相与油相相结合。(iv) The temperature of the oil phase and the water phase of the emulsion is roughly balanced, and then the water phase is combined with the oil phase under stirring conditions.
(v)在制备乳剂时,将步骤(i)中制成的混合物在搅拌下加入上述乳剂中。使用方法(v) When preparing the emulsion, the mixture prepared in step (i) is added to the above emulsion under stirring. Instructions
本发明的化妆品组合物可以护理皮肤的常规方式使用。将有效量的组合物,通常为约0.1克至约50克,优选约1克至约20克应用到湿或干,优选湿的皮肤上。组合物的应用通常包括将组合物在皮肤上揉抹,通常是用手和手指进行。然后将组合物留在皮肤上,或者,优选是从皮肤上漂洗掉。The cosmetic compositions according to the invention can be used in a conventional manner for the care of the skin. An effective amount of the composition, usually from about 0.1 gram to about 50 grams, preferably from about 1 gram to about 20 grams, is applied to wet or dry, preferably wet, skin. Application of the composition generally involves rubbing the composition on the skin, usually with the hands and fingers. The composition is then left on the skin or, preferably, rinsed off the skin.
因此,护理皮肤的优选的方法包括下列步骤:Therefore, a preferred method of caring for the skin comprises the following steps:
(a)将有效量的化妆品组合物应用到皮肤上,(a) applying an effective amount of the cosmetic composition to the skin,
(b)漂洗皮肤。(b) Rinse the skin.
本发明的优选的方面涉及上述方法,包括在将组合物应用到湿皮肤上之前,将组合物应用到干皮肤上。因此,优选的方法包括A preferred aspect of the invention relates to the above method comprising applying the composition to dry skin prior to applying the composition to wet skin. Therefore, preferred methods include
(i)将有效量的化妆品组合物应用于干皮肤上;(i) applying an effective amount of the cosmetic composition to dry skin;
(ii)在淋浴(shower)下漂洗皮肤;(ii) rinsing the skin under a shower;
(iii)再次使用所述的组合物;以及(iii) reusing said composition; and
(iv)再次漂洗。(iv) Rinse again.
多数对人体皮肤的损伤是由在清洗过程中皮肤重复多次暴露于与含表面活性剂的组合物中而产生的。现已发现能够通过使用本发明的组合物来缓解这种损伤。因此另一优选方法包括:Most damage to human skin results from repeated exposure of the skin to surfactant-containing compositions during cleansing. It has now been found that this damage can be alleviated by use of the compositions of the present invention. Another preferred method therefore includes:
(i)采用含表面活性剂的组合物清洗皮肤;(i) cleansing the skin with a surfactant-containing composition;
(ii)漂洗皮肤;(ii) rinsing the skin;
(iii)将本发明的组合物用于湿皮肤上;(iii) applying the composition of the invention to wet skin;
(iv)漂洗皮肤。(iv) Rinse the skin.
现在还发现本发明的组合物在引入作为常规的清洗程序的部分时,特别适用。因此另一优选方法包括:It has also now been found that the compositions of the present invention are particularly useful when incorporated as part of a regular cleaning routine. Another preferred method therefore includes:
(i)在皮肤上应用包含下列的组合物:(i) applying to the skin a composition comprising:
(a)至少一种季铵化合物;(a) at least one quaternary ammonium compound;
(b)保湿剂;和(b) humectants; and
(ii)漂洗皮肤;(ii) rinsing the skin;
(iii)在48小时内重复步骤(i)和(ii)。(iii) Repeat steps (i) and (ii) within 48 hours.
本发明的组合物还可以用于缓解因皮肤暴露于紫外线辐射中而引起的损伤、在游泳或类似的水中运动中与水接触引起的损伤或者在洗浴时与水接触造成的皮肤损伤。The compositions of the present invention may also be used to alleviate skin damage caused by exposure to ultraviolet radiation, contact with water during swimming or similar aquatic sports, or contact with water while bathing.
实施例 Example
以下实施例用于进一步说明本发明范围内的优选的实施方案。给出的实施例仅用于说明的目的,而不是对本发明的限定,因为在不背离本发明的精神或范围的情况下可以对本发明进行多种变化。除非特别指出,所有成分均以活性成分的重量百分比计。
1:得自Croda1: Obtained from Croda
2:得自Floratech,AZ,USA2: Obtained from Floratech, AZ, USA
3:得自Hoffman La Roche,NJ,USA3: Obtained from Hoffman La Roche, NJ, USA
4:得自Amerchol,NJ,USA4: Obtained from Amerchol, NJ, USA
5:得自Rhodi a,NJ,USA注释5: Annotated from Rhodia, NJ, USA
●实施例1,2,3,4,5,6,7,8,9,10,15,16,17,18,19,20,21,22,23,24,25,●Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25,
26,27,28,31,33,34,35,36,37,38,41,45,47,48,49,50,51,52,53,54,55,26, 27, 28, 31, 33, 34, 35, 36, 37, 38, 41, 45, 47, 48, 49, 50, 51, 52, 53, 54, 55,
56中,季铵化合物采用的是N,N-二(低芥酸菜子酰基-氧-乙基)-N-甲基,In 56, the quaternary ammonium compound is N, N-bis(lowerucicanoyl-oxygen-ethyl)-N-methyl,
N-(2-羟乙基)甲基硫酸铵,购自Goldschmidt,商品名为Rewoquat V3620N-(2-hydroxyethyl)ammonium methylsulfate available from Goldschmidt under the trade name Rewoquat V3620
●实施例11,25,29中,季铵化合物采用的是N,N-二(低芥酸菜子酰基-氧-●In embodiment 11,25,29, what the quaternary ammonium compound adopts is N, N-bis(lowerucic acid brassinoyl-oxygen-
乙基)-N-甲基,N-(2-羟乙基)甲基硫酸铵,购自Goldschmidt,商品名为Ethyl)-N-methyl, N-(2-hydroxyethyl)ammonium methylsulfate, purchased from Goldschmidt under the trade name
Rewoquat WE18Rewoquat WE18
●实施例12,30,32中,季铵化合物采用的是N,N-二(低芥酸菜子酰基-氧-●In embodiment 12,30,32, what the quaternary ammonium compound adopts is N, N-bis(canolacoyl-oxygen-
乙基)-N-甲基,N-(2-羟乙基)氯化铵,购自Goldschmidt,开发材料(WE25)Ethyl)-N-methyl, N-(2-hydroxyethyl)ammonium chloride, available from Goldschmidt, development material (WE25)
●实施例13,39,40,42中,季铵化合物采用的是甲基双(氢化牛油酰氨基●In Example 13,39,40,42, what the quaternary ammonium compound adopts is methyl bis(hydrogenated tallow amido
乙基)(2-羟乙基)甲基硫酸铵,购自Goldschmidt,商品名为Varisoft 110。Ethyl)(2-hydroxyethyl)ammonium methylsulfate available from Goldschmidt under the tradename Varisoft 110.
●实施例14,43,44中,季铵化合物采用的是甲基双(牛油基酰氨基乙基)(2-●In embodiment 14,43,44, what the quaternary ammonium compound adopts is methyl bis (tallow amido ethyl) (2-
羟乙基)甲基硫酸铵,购自Goldschmidt,商品名为Varisoft 222。方法用于包含组分C的实施例:Hydroxyethyl) ammonium methyl sulfate, purchased from Goldschmidt, trade name is Varisoft 222. The method is used for the embodiment comprising component C:
1.预混物1:在高于选定的季铵化合物转化温度的条件下混和A组中的各组分,保留预定量的季铵化合物和水不加入。剧烈混和该预混物。1. Premix 1: Mix the components of Group A above the selected quaternary ammonium conversion temperature, leaving the predetermined amount of quaternary ammonium compound and water unadded. The premix was mixed vigorously.
2.预混物2:将B和C组中的各组分与以上预混物1中剩余的季铵化合物和水混和。加热至季铵化合物和油类的熔点以上。2. Premix 2: Combine the ingredients in Groups B and C with the remaining quaternary ammonium compound from Premix 1 above and water. Heat above the melting point of quaternary ammonium compounds and oils.
3.将预混物1和2混和,并冷却至40℃,搅拌加入香精。用于包含组分D的实施例:3. Mix premix 1 and 2, cool to 40°C, stir and add essence. Examples for comprising component D:
1.预混物1:在高于选定的季铵化合物转化温度的条件下混和A组中的各组分,保留预定量的水不加入。剧烈混和该预混物。1. Premix 1: Mix the components of Group A above the selected quaternary ammonium conversion temperature, leaving a predetermined amount of water unadded. The premix was mixed vigorously.
2.预混物2:搅拌下,将D组中的各组分与以上预混物1中剩余的水混和。2. Premix 2: Under agitation, combine the ingredients in Group D with the remaining water from Premix 1 above.
3.将预混物1和2、以及B和E组中的各组分混和。剧烈搅拌。3. Combine the components of Premixes 1 and 2, and Groups B and E. Stir vigorously.
上述实施例的组合物提供了好的皮肤护理益处,如好的滋润作用、好的水合作用、好的皮肤使用感、好的皮肤柔软性和/或好的皮肤平滑性,同时不利作用如油腻性、粘着性或粘腻性低。The compositions of the above examples provide good skin care benefits, such as good moisturization, good hydration, good skin feel, good skin softness and/or good skin smoothness, while adverse effects such as Low greasiness, stickiness or stickiness.
Claims (10)
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9915094.8A GB9915094D0 (en) | 1999-06-28 | 1999-06-28 | Cosmetic compositions |
| GB9915095.5 | 1999-06-28 | ||
| GBGB9915095.5A GB9915095D0 (en) | 1999-06-28 | 1999-06-28 | Cosmetic compositions |
| GB9915094.8 | 1999-06-28 | ||
| US20191200P | 2000-05-04 | 2000-05-04 | |
| US60/201,912 | 2000-05-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1371271A true CN1371271A (en) | 2002-09-25 |
Family
ID=27269765
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN00812224A Pending CN1371271A (en) | 1999-06-28 | 2000-06-27 | Cosmetic composition |
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| Country | Link |
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| EP (1) | EP1189594A1 (en) |
| JP (1) | JP2003503338A (en) |
| KR (1) | KR20020047054A (en) |
| CN (1) | CN1371271A (en) |
| AU (1) | AU5771100A (en) |
| BR (1) | BR0012008A (en) |
| CA (1) | CA2376842A1 (en) |
| CZ (1) | CZ20014710A3 (en) |
| MX (1) | MXPA02000480A (en) |
| WO (1) | WO2001000171A1 (en) |
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|---|---|---|---|---|
| EP1406584A1 (en) * | 2001-07-13 | 2004-04-14 | The Procter & Gamble Company | Mousse forming compositions comprising quaternary ammonium agents |
| US7255869B2 (en) | 2001-10-30 | 2007-08-14 | The Procter & Gamble Company | Anhydrous cosmetic compositions containing polyols |
| US20120259010A1 (en) * | 2011-04-11 | 2012-10-11 | Conopco, Inc., D/B/A Unilever | Cationic cosmetic composition |
| EP2988830B1 (en) * | 2013-04-25 | 2021-03-17 | L'Oréal | Composition for straightening keratin fibres, comprising a urea and/or a urea derivative and a nonionic, cationic, amphoteric or anionic associative polymeric thickener, process and use thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4978526A (en) * | 1988-09-26 | 1990-12-18 | Inolex Chemical Company | Hair and skin conditioning agents and methods |
| US5145604A (en) * | 1990-09-19 | 1992-09-08 | S. C. Johnson & Son, Inc. | Aqueous emulsion and aerosol delivery system using same |
| CA2095607C (en) * | 1990-11-30 | 1997-10-14 | Deborah J. Turner | Leave-on facial emulsion compositions |
| US5552137A (en) * | 1994-08-05 | 1996-09-03 | Witco Corporation | Biodegradable quaternary hair conditioners |
| FR2761912B1 (en) * | 1997-04-14 | 1999-07-02 | Capsulis | PROCESS FOR ADHERING A PRODUCT TO A SURFACE |
| GB9814068D0 (en) * | 1998-06-29 | 1998-08-26 | Procter & Gamble | Hair conditioning composition |
-
2000
- 2000-06-27 KR KR1020017016865A patent/KR20020047054A/en not_active Ceased
- 2000-06-27 CN CN00812224A patent/CN1371271A/en active Pending
- 2000-06-27 WO PCT/US2000/017645 patent/WO2001000171A1/en not_active Ceased
- 2000-06-27 CA CA002376842A patent/CA2376842A1/en not_active Abandoned
- 2000-06-27 CZ CZ20014710A patent/CZ20014710A3/en unknown
- 2000-06-27 EP EP00943203A patent/EP1189594A1/en not_active Withdrawn
- 2000-06-27 AU AU57711/00A patent/AU5771100A/en not_active Abandoned
- 2000-06-27 MX MXPA02000480A patent/MXPA02000480A/en unknown
- 2000-06-27 JP JP2001505884A patent/JP2003503338A/en not_active Withdrawn
- 2000-06-27 BR BR0012008-1A patent/BR0012008A/en not_active IP Right Cessation
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| Publication number | Publication date |
|---|---|
| MXPA02000480A (en) | 2002-07-02 |
| CA2376842A1 (en) | 2001-01-04 |
| AU5771100A (en) | 2001-01-31 |
| WO2001000171A1 (en) | 2001-01-04 |
| BR0012008A (en) | 2002-03-12 |
| EP1189594A1 (en) | 2002-03-27 |
| KR20020047054A (en) | 2002-06-21 |
| JP2003503338A (en) | 2003-01-28 |
| CZ20014710A3 (en) | 2002-05-15 |
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