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CN1396817A - Skin care compositions - Google Patents

Skin care compositions Download PDF

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Publication number
CN1396817A
CN1396817A CN 01803849 CN01803849A CN1396817A CN 1396817 A CN1396817 A CN 1396817A CN 01803849 CN01803849 CN 01803849 CN 01803849 A CN01803849 A CN 01803849A CN 1396817 A CN1396817 A CN 1396817A
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Prior art keywords
composition
skin
compositions
present
acid
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P·J·玛特茨
P·E·曼恩
J·D·韦伯斯特
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Procter and Gamble Ltd
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Procter and Gamble Ltd
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Priority claimed from GB0001235A external-priority patent/GB0001235D0/en
Priority claimed from GB0001311A external-priority patent/GB0001311D0/en
Application filed by Procter and Gamble Ltd filed Critical Procter and Gamble Ltd
Publication of CN1396817A publication Critical patent/CN1396817A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25Silicon; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/42Colour properties
    • A61K2800/43Pigments; Dyes
    • A61K2800/436Interference pigments, e.g. Iridescent, Pearlescent

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Cosmetics (AREA)

Abstract

本发明涉及用以在皮肤的外观和触感上引起立即改善、特别是用以提供更均匀的肤色的局部液体化妆品组合物。该组合物含有:a)0.3%到1.5%的光学上中性的页硅酸盐;和b)当以2.4mg cm-2的覆盖量涂在皮肤或皮肤替代物上时、可提供给组合物-1到-5的Δa的色移值和-2到-5的Δb的色移值的有效量的绿颜料;其中组合物中无机颗粒的总含量小于5%。本发明的第二方面中,该组合物含有:a)0.3%到1.5%的光学上中性的页硅酸盐;和b)绿色片状干扰颜料,TiO2层的厚度为120nm到160nm或其整数倍,含量为组合物重量的0.1%到0.5%;其中组合物中无机颗粒的总含量小于5%。该组合物优选地为水包油乳液。The present invention relates to topical liquid cosmetic compositions for causing an immediate improvement in the appearance and feel of the skin, in particular for providing a more even skin tone. The composition contains: a) 0.3% to 1.5% of an optically neutral phyllosilicate; and b) when applied to the skin or a skin substitute at a coverage of 2.4 mg cm An effective amount of green pigment with a color shift value of Δa from -1 to -5 and a color shift value of Δb from -2 to -5; wherein the total content of inorganic particles in the composition is less than 5%. In a second aspect of the invention, the composition contains: a) 0.3% to 1.5% of an optically neutral phyllosilicate; and b) green flake-like interference pigments, the TiO2 layer having a thickness of 120nm to 160nm or Integer multiples thereof, the content is 0.1% to 0.5% of the weight of the composition; wherein the total content of inorganic particles in the composition is less than 5%. The composition is preferably an oil-in-water emulsion.

Description

护肤组合物skin care composition

                          技术领域 technical field

本发明涉及用于改善人皮肤的外观和触感的局部组合物的领域。更特别地,本发明涉及在保持自然皮肤外观的同时,可对皮肤缺陷如毛孔和不均匀的肤色提供良好的覆盖的局部组合物。本发明的组合物尤其适用于对于身体的非脸部位、尤其是手的美容处理。The present invention relates to the field of topical compositions for improving the appearance and feel of human skin. More particularly, the present invention relates to topical compositions that provide good coverage of skin imperfections such as pores and uneven skin tone while maintaining the natural skin appearance. The compositions of the invention are especially suitable for the cosmetic treatment of non-facial parts of the body, especially the hands.

                            背景 background

可设计局部化妆品组合物、如护肤霜和护肤液等等,使其对皮肤提供各种涂用后益处,如润湿、皮肤防护和对皮肤的触感和外观的改善。这些益处可为完全地美容性的或可通过使用能够调理皮肤状态包括调理细纹、皱纹和与老化或光损伤皮肤有关的其它形式的不均匀或粗糙的表面质地的长期作用的活性成分而提供。理想地,护肤品不仅仅提供较长时间的益处,而且还可引起立即显著的改善如提高的皮肤的光滑度。为了商业上的成功另外还需要产品具有使用中的美感,即在不感觉油或粘的情况下,可很容易地将其擦入。Topical cosmetic compositions, such as skin creams and lotions, and the like, can be designed to provide various post-application benefits to the skin, such as moisturization, skin protection, and improvements in the feel and appearance of the skin. These benefits may be purely cosmetic or may be provided through the use of long-acting active ingredients capable of regulating the condition of the skin including the regulation of fine lines, wrinkles and other forms of uneven or rough surface texture associated with aging or photodamaged skin . Ideally, a skin care product would not only provide longer-term benefits, but would also result in immediate and noticeable improvements such as increased skin smoothness. Commercial success additionally requires that the product have in-use aesthetics, ie, it can be easily rubbed in without feeling greasy or sticky.

众所周知可用绿色颜料抵消皮肤的红色。例如,WO 96/03962中介绍了为此目的的含有TiO2包覆云母干扰颜料的化妆品组合物,US 5,690,916介绍了通过使用相同材料使皮肤的深色部分(斑点、雀斑等等)不显眼的方法。It is known to counteract skin redness with green pigments. For example, WO 96/03962 describes a cosmetic composition for this purpose containing TiO2- coated mica interfering pigments, and US 5,690,916 describes a method for making dark parts of the skin (spots, freckles, etc.) inconspicuous by using the same materials. method.

虽然先有技术的组合物和公开在美容性皮肤处理的领域提供了有用的提议,对于可提供皮肤、特别是身体的非脸部位、尤其是身体的受环境影响的部位如手的触感和外观立即的改善的改良组合物的需要仍然存在。还需要组合物不油并易于涂抹。While prior art compositions and disclosures provide useful suggestions in the field of cosmetic skin treatments, there are many ways to provide skin, especially non-facial parts of the body, especially environmentally affected parts of the body such as the hands and skin. There remains a need for improved compositions with an immediate improvement in appearance. It is also desirable that the composition be non-greasy and easy to spread.

特别地,现已发现可通过在优选地为水包油乳液的液体局部组合物中使用控制量的光学上中性和彩色的片状颗粒,可得到对多种肤色的改善的皮肤触感和外观。已发现含有大量干扰颜料或不含光学上中性片状颗粒的先有技术组合物不能提供同等程度的颜色控制。当组合物含有具有适合片状颗粒体系的铺展性和润滑性程度的油相时,可特别地增强本发明组合物的皮肤光滑度效果和使用中美感。In particular, it has now been found that improved skin feel and appearance for a variety of skin tones can be obtained by using controlled amounts of optically neutral and colored tabular particles in liquid topical compositions, preferably oil-in-water emulsions . It has been found that prior art compositions containing large amounts of interfering pigments or containing no optically neutral tabular particles do not provide the same degree of color control. The skin smoothing effect and in-use aesthetics of compositions according to the invention are particularly enhanced when the composition contains an oil phase with a degree of spreadability and lubricity suitable for tabular particle systems.

本发明还涉及特别地为提供更均匀的肤色、通过局部涂用主题组合物改善皮肤触感和外观的美容方法。The present invention also relates to cosmetic methods of improving the feel and appearance of skin by topical application of the subject compositions, particularly to provide a more even skin tone.

                          发明概要 Summary of the invention

第一方面,本发明涉及优选地以水包油乳液形式的局部用液体化妆品组合物,含有:In a first aspect, the present invention relates to a topical liquid cosmetic composition, preferably in the form of an oil-in-water emulsion, comprising:

a)约0.3%到约1.5%的光学上中性的页硅酸盐;和a) from about 0.3% to about 1.5% optically neutral phyllosilicate; and

b)当以2.4mg cm-2的覆盖量涂在皮肤或皮肤替代物上时、可提供给组合物-1到-5的Δa的色移值和-2到-5的Δb的色移值的有效量的绿颜料;b) Color shift values for Δa and -2 to -5 for Δa and -2 to -5 when applied to skin or skin substitutes at a coverage of 2.4 mg cm- 2 an effective amount of green pigment;

其中组合物中无机颗粒的总含量小于5%。Wherein the total content of inorganic particles in the composition is less than 5%.

第二方面,本发明涉及优选地以水包油乳液形式的局部用液体化妆品组合物,含有:In a second aspect, the present invention relates to a liquid cosmetic composition for topical application, preferably in the form of an oil-in-water emulsion, comprising:

a)约0.3%到约1.5%的光学上中性的页硅酸盐;和a) from about 0.3% to about 1.5% optically neutral phyllosilicate; and

b)绿色片状干扰颜料,TiO2层的厚度为120nm到160nm或其整数倍,含量为组合物重量的0.1%到0.5%;b) Green flaky interference pigments, the thickness of the TiO2 layer is 120nm to 160nm or an integer multiple thereof, and the content is 0.1% to 0.5% by weight of the composition;

其中组合物中无机颗粒的总含量小于5%。Wherein the total content of inorganic particles in the composition is less than 5%.

组合物适用于在保持自然皮肤外观的同时,在皮肤外观和触感方面给以基本上立即的视觉上的改善。The compositions are suitable for imparting a substantially immediate visual improvement in skin appearance and feel while maintaining the natural skin appearance.

本发明还涉及通过局部涂用主题组合物改善皮肤外观和触感的美容方法。The present invention also relates to cosmetic methods for improving the appearance and feel of skin by topical application of the subject compositions.

                          发明详述Detailed description of the invention

除非以其它方式说明,本文所使用的所有百分比和比值都是基于组合物的总重量计的,并且所有测量都是在25℃下进行的。本文提及的所有公开文献均引入本文作为参考。As used herein, all percentages and ratios are by weight of the total composition and all measurements made are at 25°C, unless otherwise specified. All publications mentioned herein are incorporated herein by reference.

此处所引的所有出版物整体引用作为参考。All publications cited herein are incorporated by reference in their entirety.

“局部液体化妆品组合物”是指预期擦入皮肤的湿或油性的组合物。优选的组合物为水剂、乳霜或凝胶的形式。"Topical liquid cosmetic composition" means a wet or oily composition intended to be rubbed into the skin. Preferred compositions are in the form of lotions, creams or gels.

这里术语“皮肤学上可接受的”指所述组合物或组分适于与人体皮肤接触,没有不当的毒性、不相容性、不稳定性、过敏反应等。The term "dermatologically acceptable" herein means that the composition or component is suitable for contact with human skin without undue toxicity, incompatibility, instability, allergic response, and the like.

这里术语“安全及有效量”指这样的化合物或组合物用量,它能明显产生有益效果,优选有益的皮肤外观或皮肤效果,分别包括这里所说的各种益处,但是能避免严重的副作用,如产生合理益害比,该用量是在技术人员的合理判断的范围内。Herein the term "safe and effective amount" refers to the amount of the compound or composition used to produce significant beneficial effects, preferably beneficial skin appearance or skin effects, respectively including the various benefits mentioned herein, but avoiding serious side effects, If a reasonable ratio of benefit to harm is produced, the dosage is within the reasonable judgment range of the technical personnel.

术语“光学上中性”是指把材料单独涂在皮肤上时除了有可能使肤色变浅或变深以外不产生净颜色变化。优选地对于光学上中性材料的在题为“绿色颜料”部分定义的Δa和Δb的色移值都不超过一个单位,更优选地不超过一个单位的一半。这些材料在整体外观上一般地为无色、白色或乳白色。The term "optically neutral" means that the material produces no net color change when applied to the skin alone other than the possibility of lightening or darkening the skin tone. Preferably neither Δa nor Δb for an optically neutral material has a color shift value of more than one unit, more preferably no more than half a unit, as defined in the section entitled "Green Pigments". These materials are generally colorless, white or milky white in overall appearance.

本文中,有用的活性成分和其它成分由它们的美容和/或治疗益处或它们假设的作用方式来分类或描述。然而,应当理解的是:可用于本文的活性和其它成分在某些情况下可以提供多于一种美容和/或治疗益处或者经由一种以上的作用方式来奏效。因此,本文进行分类是为方便起见,并且不意图使成分限制于具体说明的应用或者所列出的应用。Useful active and other ingredients are categorized or described herein by their cosmetic and/or therapeutic benefit or their postulated mode of action. It should be understood, however, that the active and other ingredients useful herein may in some instances provide more than one cosmetic and/or therapeutic benefit or operate via more than one mode of action. Accordingly, classifications are made herein for convenience and are not intended to limit ingredients to the applications specifically stated or listed.

适用于主题发明的局部组合物可制成各种产品形式如本领域已知的形式的产品。优选的组合物具有足够的稠度或致流力点以阻碍颗粒的沉淀。Topical compositions suitable for use in the subject invention may be formulated in a variety of product forms such as are known in the art. Preferred compositions have sufficient consistency or flow point to impede settling of particles.

优选的组合物含有皮肤用亲水性稀释剂。适宜的亲水稀释剂包括水、有机亲水稀释剂如C1-C4一元醇和低分子量二醇类和多元醇类,包括丙二醇、聚乙二醇(例如,分子量200-600)、聚丙二醇(例如,分子量425-2025)、丙三醇、丁二醇、1,2,4-丁三醇、山梨醇、1,2,6-己三醇、乙醇、异丙醇、山梨醇酯、乙氧基化醚、丙氧基化醚及其混合物。稀释剂优选是液体。水是特别优选的稀释剂。组合物优选包含至少约60%的亲水稀释剂。Preferred compositions contain a hydrophilic diluent for the skin. Suitable hydrophilic diluents include water, organic hydrophilic diluents such as C 1 -C 4 monohydric alcohols and low molecular weight diols and polyols, including propylene glycol, polyethylene glycol (e.g., molecular weight 200-600), polypropylene glycol (e.g. molecular weight 425-2025), glycerol, butanediol, 1,2,4-butanetriol, sorbitol, 1,2,6-hexanetriol, ethanol, isopropanol, sorbitol esters, Ethoxylated ethers, propoxylated ethers and mixtures thereof. The diluent is preferably a liquid. Water is a particularly preferred diluent. The compositions preferably comprise at least about 60% hydrophilic diluent.

高度优选的载体包括乳液,其中含有亲水相(特别是含水相)和疏水相,如脂质、油或油性物质。正如本领域技术人员公知的,亲水相分散在疏水相中,或者反之,分别形成亲水或疏水分散连续相,形成哪种相的形式取决于组合物的成分。在乳液技术中,术语″分散相″是本领域技术人员公知的术语,意指相以小微粒或小滴悬浮在连续相中并为连续相所包围的形式存在。分散相也被称为内部或不连续相。乳液可以是或包括(例如在三相或其它多相乳液中)水包油型乳液或者油包水型乳液,如聚硅氧烷包水乳液。典型的水包油型乳液中含有约1%-约5%(优选约1%-约30%)的分散疏水相和约1%-约99%(优选约40%-约90%)的连续亲水相;典型的油包水型乳液中含有约1%-约98%(优选为约40-约90%)的分散亲水相和约1%-约50%(优选1%-约30%)的连续疏水相。乳液中也可以包括凝胶网,如G.M.Eccleston,乳液稳定性理论在流动和半固体O/W乳液中的应用(Application of Emulsion Stability Theories to Mobileand Semisolid O/W Emulsions),化妆品和盥洗用品(Cosmetics &Toiletries),第101卷,1996年11月,73-92页中所述,其引入本文作为参考。本发明的高度优选组合物是水包油型乳液。Highly preferred carriers include emulsions, which contain a hydrophilic phase, especially an aqueous phase, and a hydrophobic phase, such as lipids, oils or oily substances. As is well known to those skilled in the art, the hydrophilic phase is dispersed in the hydrophobic phase, or vice versa, forming a hydrophilic or hydrophobic dispersed continuous phase, respectively, depending on the ingredients of the composition. In emulsion technology, the term "dispersed phase" is a well-known term for those skilled in the art and means that the phase exists in the form of small particles or droplets suspended in and surrounded by the continuous phase. The dispersed phase is also called the internal or discontinuous phase. The emulsion can be or comprise (for example in a three-phase or other multi-phase emulsion) an oil-in-water emulsion or a water-in-oil emulsion, such as a water-in-silicone emulsion. A typical oil-in-water emulsion contains about 1% to about 5% (preferably about 1% to about 30%) of a dispersed hydrophobic phase and about 1% to about 99% (preferably about 40% to about 90%) of a continuous hydrophilic phase. Aqueous phase; a typical water-in-oil emulsion contains from about 1% to about 98% (preferably from about 40% to about 90%) of the dispersed hydrophilic phase and from about 1% to about 50% (preferably from 1% to about 30%) continuous hydrophobic phase. Emulsions can also include gel networks, such as G.M. Eccleston, Application of Emulsion Stability Theories to Mobile and Semisolid O/W Emulsions, Cosmetics and Toiletries (Cosmetics & Toiletries), Vol. 101, November 1996, pp. 73-92, which is incorporated herein by reference. Highly preferred compositions of the present invention are oil-in-water emulsions.

优选的组合物具有约5,000-约200,000mPa.s(厘泊)的表观粘度。例如,优选的水剂具有约10,000-约40,000mPa.s的表观粘度;优选的霜剂具有约60,000-约160,000mPa.s的表观粘度。表观粘度可以通过用Brookfield DVll RV粘度计,转轴TD,在5rpm下测定,或使用其等同物测定。待制备完的组合物稳定之后(通常,制备组合物后在25℃±1℃和环境压力下稳定24小时),对组合物进行粘度测定。在25℃±1℃下,在转轴旋转30秒后,用组合物进行粘度测定。Preferred compositions have an apparent viscosity of from about 5,000 to about 200,000 mPa.s (centipoise). For example, preferred lotions have an apparent viscosity of from about 10,000 to about 40,000 mPa.s; preferred creams have an apparent viscosity of from about 60,000 to about 160,000 mPa.s. Apparent viscosity may be measured with a Brookfield DV11 RV viscometer, spindle TD, at 5 rpm, or using its equivalent. After the prepared composition is stabilized (generally, the composition is stabilized at 25°C±1°C and ambient pressure for 24 hours after preparation), the composition is subjected to a viscosity measurement. Viscosity measurements were performed on the compositions after 30 seconds of spindle rotation at 25°C ± 1°C.

通常来说,将本发明的组合物配制成pH为8.5或更低,并且通常的pH范围为约4.5-约7.5,更优选约5-约6.5。一些组合物,特别是含有附加活性物如水杨酸的组合物,要求较低的pH以便附加活性物能够完全生效。通常,将这些组合物配制成pH约2.5-约5,更优选约2.7-约4。光学上中性的页硅酸盐 Generally, the compositions of the present invention are formulated to have a pH of 8.5 or lower, and typically have a pH in the range of from about 4.5 to about 7.5, more preferably from about 5 to about 6.5. Some compositions, particularly those containing additional actives such as salicylic acid, require a lower pH for the additional active to be fully effective. Typically, these compositions are formulated to have a pH of from about 2.5 to about 5, more preferably from about 2.7 to about 4. Optically neutral phyllosilicates

本发明的组合物的基本成分是既可增强皮肤触感又有助于通过组合物作用的净颜色变化的光学上中性的页硅酸盐。页硅酸盐为硅酸盐的子类,其中原子以弱键键合的层状排列,这样研磨时可形成层状的颗粒。页硅酸盐作为包括许多子类的一类,例如在互联网http://mineral.galleries.com/minerals/silicate/phyllosi.htm上作了介绍。在《Kirk-Othmer化学工艺百科全书》第4版中也介绍了许多单独的子类。优选的子类包括高岭石、蒙脱石、滑石和云母。最优选的为滑石和云母,尤其是云母。页硅酸盐的层状结构使涂在皮肤上时给以光滑的感觉。从外观和皮肤触感出发,最优选的材料为光学上中性的钛包覆云母。这些光学上中性的钛包覆云母可从市场上买到,适宜的材料包括来自Merck分支机构Rona的Microna Matte White。An essential ingredient of the compositions of the present invention is an optically neutral phyllosilicate that both enhances skin feel and contributes to the net color change through the action of the composition. Phylosilicates are a subclass of silicates in which the atoms are arranged in weakly bonded layers so that when ground they form layered particles. Phylosilicates, as a class comprising many subclasses, are described, for example, on the Internet at http://mineral.galleries.com/minerals/silicate/phyllosi.htm . A number of individual subclasses are also introduced in the 4th edition of the Kirk-Othmer Encyclopedia of Chemical Technology. Preferred subclasses include kaolinite, montmorillonite, talc and mica. Most preferred are talc and mica, especially mica. The layered structure of phyllosilicates gives a smooth feel when applied to the skin. From appearance and skin feel, the most preferred material is optically neutral titanium-coated mica. These optically neutral titanium-coated micas are commercially available, suitable materials include Microna Matte White from Rona, a division of Merck.

光学上中性的页硅酸盐通常存在的含量为约0.3%到约1.5%、优选地约0.5%到约1.3%、更优选地约0.6%到约1.0%。较低的含量不能给以本发明的皮肤触感或颜色调节的益处,而较高的含量会有厚重的感觉或外观。Optically neutral phyllosilicates are typically present at a level of from about 0.3% to about 1.5%, preferably from about 0.5% to about 1.3%, more preferably from about 0.6% to about 1.0%. Lower levels will not impart the skin feel or color conditioning benefits of the present invention, while higher levels will give a heavy feel or appearance.

光学上中性的页硅酸盐的所有粒径的最大尺寸优选地在约0.1到约100μm的范围内、更优选地在约0.5到约20μm的范围内,厚度优选地为约100到约1500nm。绿颜料 The largest dimension of all particle sizes of optically neutral phyllosilicates is preferably in the range of about 0.1 to about 100 μm, more preferably in the range of about 0.5 to about 20 μm, and the thickness is preferably about 100 to about 1500 nm . green paint

本发明的第一方面的组合物的另一基本成分为当以2.4mg cm-2的覆盖量涂在皮肤或皮肤替代物上时、可提供给组合物-1到-5、优选地-2到-4的Δa的色移值和-2到-5、优选地-2到-4、更优选地-2到-3的Δb的色移值的有效量的绿颜料。下面详细介绍了测量色移值的试验方法。已发现在要求范围内的色移可在较深的肤色上不产生不自然的绿色的条件下,有效地减少皮肤红色。这样,该绿色颜料有助于提供整体均匀的皮肤色调。对于通常浅色的皮肤如白种人的肤色,可以接受不带有附随的Δb色移的相同的Δa色移,但已发现会在较深的肤色上产生过绿的感觉。此处所述的光学上中性的页硅酸盐和绿颜料一起使用可得到对于许多皮肤类型可接受的需要的色移。Another essential ingredient of the composition of the first aspect of the present invention is that when applied to the skin or a skin substitute at a coverage of 2.4 mg cm -2 , it can be provided to compositions -1 to -5, preferably -2 An effective amount of a green pigment for a color shift value of Δa to -4 and a color shift value of Δb of -2 to -5, preferably -2 to -4, more preferably -2 to -3. The experimental method for measuring color shift values is detailed below. A color shift within the required range has been found to be effective in reducing skin redness without producing an unnatural green tint on darker skin tones. In this way, the green pigment helps to provide an overall even skin tone. The same Δa color shift without the concomitant Δb color shift is acceptable for normally light colored skin such as Caucasian skin tones, but has been found to give a greenish perception on darker skin tones. Use of the optically neutral phyllosilicates described herein with green pigments can result in desired color shifts that are acceptable to many skin types.

虽然需要的色移毫无疑问是对于人皮肤的色移,已发现可通过体外试验接近地近似。因此要求的色移是指在下述体外试验中测定的色移。While the desired color shift is undoubtedly that of human skin, it has been found to be closely approximated by in vitro testing. The color shift claimed therefore refers to the color shift determined in the in vitro test described below.

把一块平坦的吸收性半透明的外科手套放在标准的红色瓷砖上(吸收性表面朝上),用以与法线成25°角的D65光源照明、以与法线成10°角测量的适宜的反射分光光度计(如Minolta CM-512M3)测定整个系统的颜色。已发现对于试验的目的,手套置于瓷砖上的装置可非常好地模拟人皮肤的性状和颜色。所用的瓷砖应为由美国纽约的Macbeth MunsellColour供应的来自于标准色图(Macbeth Color Checker)的“红色”小片。手套的类型不是特别关键。但是本申请所用的类型为由英国Broxbourne的Regent Hospital Products供应的Biogel外科手套。测定的置于瓷砖上的手套的颜色用以生成一组基准L、a、b值。然后用预饱和的指套把色移待测的组合物以2.4mg cm-2的覆盖量涂在手套上,并擦入30秒钟。然后把产物干燥10分钟,以与前面相同的方法再测定颜色,生成一组后处理L、a、b值。把L、a、b基准值从后处理L、a、b值中减去以得到组合物的ΔL、Δa和Δb值。这些值完全地用以表征色移。应把重复十次的数值加以平均。A flat piece of absorbent translucent surgical glove is placed on a standard red tile (absorbent surface facing up), illuminated by a D65 light source at an angle of 25° to the normal, measured at an angle of 10° to the normal A suitable reflection spectrophotometer (eg Minolta CM-512M3) measures the color of the entire system. It has been found that for testing purposes, the glove-on-tile setup mimics the texture and color of human skin very well. The tiles used should be the "red" flakes from the standard color chart (Macbeth Color Checker) supplied by Macbeth Munsell Colour, New York, USA. The type of glove is not particularly critical. However the type used for this application is the Biogel Surgical Glove supplied by Regent Hospital Products of Broxbourne, UK. The measured color of the glove placed on the tile was used to generate a set of baseline L, a, b values. The composition to be tested for color shifting was then applied to the glove at a coverage of 2.4 mg cm -2 using a presaturated finger cot and rubbed in for 30 seconds. The product was then dried for 10 minutes, and the color was remeasured in the same manner as before to generate a set of post-treatment L, a, b values. The L, a, b baseline values are subtracted from the post-treatment L, a, b values to obtain the ΔL, Δa, and Δb values for the composition. These values are used exclusively to characterize the color shift. Values from ten replicates should be averaged.

适宜的绿颜料包括干扰颜料和反射颜料。适宜的反射颜料包括氢氧化铬,如来自于ISP Van Dyck的商品名为Chroma Lite Aqua 4508和来自于Presperse的H Chrome Green 105的颜料,以及氧化铬,如来自于ISP Van Dyck的Chroma Lite Green和来自于Mearl的Gemtone Emerald。优选绿色颜料是小片型干扰颜料物质,其具有TiO2层厚度为约120nm-约160nm或其整数倍。优选,干扰颜料物质中含有被TiO2包裹的小片型云母。反射光的颜色取决于层的厚度而不同。本发明中使用的干扰颜料物质中含有至少一部分TiO2层厚度为约120nm-约160nm或其整数倍的颜料物质,以致使颜料本身当施用给皮肤时由于颜料小片的光反射而具有整体的绿色外貌。优选用于本发明组合物的干扰颜料物质具有约150nm-约250nm、优选约150nm的TiO2层厚度。适宜的实例是由Merck以商品名Timiron_提供的,尤其是Timiron_Silk Green,或者由Mearl以商品名Flamenco_,尤其是Flamenco_Satin Green。Suitable green pigments include interference and reflective pigments. Suitable reflective pigments include chromium hydroxides such as those available under the tradenames Chroma Lite Aqua 4508 from ISP Van Dyck and H Chrome Green 105 from Presperse, and chromium oxides such as Chroma Lite Green and Gemtone Emerald from Mearl. Preferably the green pigment is a platelet-type interference pigment substance having a TiO2 layer thickness of about 120 nm to about 160 nm or an integer multiple thereof. Preferably, the interfering pigment substance contains platelet mica surrounded by TiO 2 . The color of the reflected light differs depending on the thickness of the layer. The interfering pigment material used in the present invention contains at least a portion of the pigment material having a TiO2 layer thickness of about 120 nm to about 160 nm or integer multiples thereof, so that the pigment itself has an overall green color when applied to the skin due to light reflection of the pigment platelets appearance. Interfering pigment substances preferably used in the compositions according to the invention have a TiO 2 layer thickness of about 150 nm to about 250 nm, preferably about 150 nm. Suitable examples are supplied by Merck under the trade name Timiron ® , especially Timiron _ Silk Green, or by Mearl under the trade name Flamenco _ , especially Flamenco _ Satin Green.

为提供需要的色移的必需的颜料的精确含量在一定程度上取决于所用颜料的具体类型。绿颜料在本发明的组合物中存在的含量一般地为约0.1%到约0.5%、优选地约0.15%到约0.4%、更优选地约0.2%到约0.3%。The precise amount of pigment necessary to provide the desired color shift will depend to some extent on the particular type of pigment used. Green pigments are generally present in the compositions of the present invention at levels from about 0.1% to about 0.5%, preferably from about 0.15% to about 0.4%, more preferably from about 0.2% to about 0.3%.

本发明的第二方面,组合物含有绿色片状干扰颜料,TiO2层厚度为120nm到160nm或其整数倍,含量为组合物重量的0.1%到0.5%。In the second aspect of the present invention, the composition contains green flaky interference pigments, the thickness of the TiO2 layer is 120nm to 160nm or its integral multiple, and the content is 0.1% to 0.5% by weight of the composition.

绿颜料的所有粒径的最大尺寸优选地在约0.1到约100μm的范围内、更优选地在约5到约50μm的范围内,厚度优选地为约100到约1500nm。The largest dimension of all particle sizes of the green pigment is preferably in the range of about 0.1 to about 100 μm, more preferably in the range of about 5 to about 50 μm, and the thickness is preferably about 100 to about 1500 nm.

如果整体的色移在提到的范围内,包括不同色彩颜料的其它颜料也可用于本发明组合物中。可选组分 Other pigments including different colored pigments may also be used in the compositions of the invention provided the overall color shift is within the mentioned ranges. optional components

本发明的局部施用组合物可以包含各种可选的组分,只要这些可选组分可与本文描述的必要组分在物理和化学性质上相容,并且不会过分削弱与本发明组合物有关的稳定性、功效或其它使用益处。可选的组分可以分散、溶解于本组合物的载体中。The topical compositions of the present invention may contain a variety of optional ingredients so long as these optional ingredients are physically and chemically compatible with the essential components described herein and do not unduly impair compatibility with the compositions of the present invention. Relevant stability, efficacy or other benefits of use. Optional components can be dispersed or dissolved in the vehicle of the composition.

可选的组分包括柔肤剂、油吸收剂、抗微生物剂、粘合剂、缓冲剂、变性剂、美容收敛剂、外部镇痛刑、成膜剂、保湿剂、不透明剂、香料、颜料、皮肤渗透性增强剂、溶剂、悬浮剂、乳化剂、清洁剂、增稠剂、增溶剂、蜡、防晒剂、非日晒型晒黑剂、抗氧化剂和/或自由基清除剂、螯合剂、抗炎剂、脱皮剂/剥离剂、有机羟基酸、维生素及天然提取物。这些物质的非排他性实例于描述于 Harry氏化妆品学,第7版,Harry和Wilkinson(Hill Publisher,伦敦,1982); 药物剂型-分散系统;Lieberman,Rieger和Banker,第1卷(1988)和第2卷(1989),MarcelDecker有限公司; 化妆品的化学和制造,第2版,deNavarre(yan Nostrand962-1965)以及 化妆品科学和技术手册,第1版,Knowlton和Pearce(Elsevier 1993)。它们也可以用于本发明。1.有机粒状物质 Optional components include emollients, oil absorbers, antimicrobials, binders, buffers, denaturants, cosmetic astringents, external analgesics, film formers, humectants, opacifiers, fragrances, pigments , skin penetration enhancers, solvents, suspending agents, emulsifiers, cleansers, thickeners, solubilizers, waxes, sunscreens, non-sun tanning agents, antioxidants and/or free radical scavengers, chelating agents , anti-inflammatory agents, peeling/exfoliating agents, organic hydroxy acids, vitamins and natural extracts. Non-exclusive examples of these substances are described in Harry's Cosmetology , 7th Edition, Harry and Wilkinson (Hill Publisher, London, 1982); Pharmaceutical Formulations - Dispersion Systems ; Lieberman, Rieger and Banker, Vol. 1 (1988) and Vol. 2 volumes (1989), Marcel Decker Ltd; Chemistry and Manufacture of Cosmetics , 2nd ed., de Navarre (yan Nostrand 962-1965) and Handbook of Cosmetic Science and Technology , 1st ed., Knowlton and Pearce (Elsevier 1993). They can also be used in the present invention. 1. Organic granular matter

本发明优选的组合物中含有折光率为1.3-1.7的有机粒状物质,该粒状物质分散在组合物中并且其体积平均颗粒粒度范围为约5-约30μm,优选约8-25μm。不期望理论支持,据信有机粒状颗粒,其直径至少等于本发明组合物在皮肤上产生的油层,起非油腻性的润滑剂作用,从而改善整个皮肤感觉。体积平均颗粒粒度是当粒状物质在与本发明的载体联合之前呈净形式(即本质上纯的形式)的粉末形状时测定。然而,颗粒粒度的具体测量方法可能会要求将粒状物质分散在惰性载体如纯油中,以便测定颗粒粒度的分布。颗粒粒度可以通过本领域已知的任何适宜的方法来测定,例如通过使用库尔特粒度仪(Coulter counter)或ASTM命名E20-85″通过光学显微镜测定0.2-75微米粒状物质的颗粒粒度分析标准方法(Standard Practice for Particulate Size Analysis ofparticulate Substances in the Range of 0.2 to 75 Micrometers byOptical Microscopy)″,ASTM Volume 14.02,1993。Preferred compositions of the present invention contain organic particulate material having a refractive index of 1.3-1.7 dispersed in the composition and having a volume average particle size in the range of about 5 to about 30 microns, preferably about 8 to 25 microns. Without wishing to be bound by theory, it is believed that the organic particulate particles, having a diameter at least equal to the oil layer produced by the composition of the present invention on the skin, act as a non-greasy emollient, thereby improving overall skin feel. The volume average particle size is determined when the particulate material is in the form of a powder in neat (ie essentially pure) form prior to association with the carrier of the present invention. However, specific methods of measuring particle size may require that the particulate material be dispersed in an inert carrier such as pure oil in order to determine the particle size distribution. Particle size may be determined by any suitable method known in the art, for example by using a Coulter counter or ASTM designation E20-85" Particle Size Analysis Standard for Particulate Matter from 0.2 to 75 microns by Light Microscopy Method (Standard Practice for Particulate Size Analysis of Particulate Substances in the Range of 0.2 to 75 Micrometers by Optical Microscopy)", ASTM Volume 14.02, 1993.

折光率可以用常规方法来测定。例如,用于适用于本发明的测定折光率的方法描述在下列的文献中:J.A.Dean编,Lange氏化学手册,第14版,McGraw Hill,纽约,1992第9节,折射法。折光率优选为约1.35-约1.6,这个范围与皮肤折光率近乎相吻合。The refractive index can be measured by a conventional method. For example, a method for determining the refractive index suitable for use in the present invention is described in J.A. Dean, edited, Lange's Handbook of Chemistry, 14th Edition, McGraw Hill, New York, 1992 Section 9, Refractive Methods. The refractive index is preferably from about 1.35 to about 1.6, a range that closely matches the refractive index of skin.

本发明的组合物优选含有约0.1%-约10%、更优选约0.3%-约5%、特别是约0.5%-约2%的有机粒状物质。The compositions of the present invention preferably contain from about 0.1% to about 10%, more preferably from about 0.3% to about 5%, especially from about 0.5% to about 2%, of organic particulate material.

优选的粒状物质是自由流动的、多孔物质,特别是具有球形的颗粒。适宜的有机粒状物质包括由聚甲基倍半硅氧烷(上述参考中提及的)、聚酰胺、聚乙烯、聚丙烯腈、聚丙烯酸、聚甲基丙烯酸、聚苯乙烯、聚四氢乙烯(PTFE)和聚(二氯乙烯)制造的颗粒。还可以使用由前述物质的单体生产的共聚物。优选聚酰胺,尤其是尼龙。本发明特别优选的是体积平均颗粒粒度范围为约15-约25μm的多孔状尼龙颗粒。适宜的尼龙颗粒可从Elf Atochem SA(法国巴黎)以商品名Orgasol_商购获得。Preferred granular materials are free-flowing, porous materials, especially particles having a spherical shape. Suitable organic particulate materials include polymethylsilsesquioxane (mentioned in the above reference), polyamide, polyethylene, polyacrylonitrile, polyacrylic acid, polymethacrylic acid, polystyrene, polytetrahydroethylene (PTFE) and poly(vinylidene chloride) particles. Copolymers produced from monomers of the aforementioned substances can also be used. Polyamides are preferred, especially nylon. Particularly preferred herein are porous nylon particles having a volume average particle size in the range of about 15 to about 25 microns. Suitable nylon particles are commercially available from Elf Atochem SA (Paris, France) under the tradename Orgasol® .

组合物中可以含有其它无机或有机粒状物质。然而,优选本发明组合物中的有机粒状物质基本上由标题为″有机粒状物质″章节中所述的粒状物质组成。2. 无机消光剂 The composition may contain other inorganic or organic particulate materials. However, it is preferred that the organic particulate material in the composition of the invention consists essentially of the particulate material described in the section entitled "Organic Particulate Material". 2. Inorganic matting agent

本发明组合物的另一可选组分是无机消光剂,如氧化钛或氧化锌。但是,当存在时,消光剂的使用量不超过3%,以避免不期望的皮肤变白或不自然的“遮蔽”外貌。优选用于本发明的是二氧化钛,尤其是锐钛矿二氧化钛。Another optional component of the compositions of the present invention is an inorganic matting agent, such as titanium oxide or zinc oxide. However, when present, matting agents are used at no more than 3% to avoid undesired skin whitening or an unnatural "masked" appearance. Preferred for use in the present invention is titanium dioxide, especially anatase titanium dioxide.

锐钛矿氧化钛的密度为约3.90g/cm3并且呈四角形、立方体紧密堆积结构。锐钛矿氧化钛的折光率为2.55。锐钛矿二氧化钛可从KoboProducts公司以商品名Kobo BTD 11 S2商购获得,从Whittaker(Clark,Daniels,South Plainfield,New Jersey,USA)以产品名TiO2 9729商购获得,并且可从Cardre公司(South Plainfield,New Jersey,USA)以商品名Carde 70429商购获得。Anatase titanium oxide has a density of about 3.90 g/cm 3 and a tetragonal, cubic close-packed structure. The refractive index of anatase titanium oxide is 2.55. Anatase titanium dioxide is commercially available from Kobo Products, Inc. under the tradename Kobo BTD 11 S2, from Whittaker (Clark, Daniels, South Plainfield, New Jersey, USA) under the product name TiO 2 9729, and from Cardre Corporation ( South Plainfield, New Jersey, USA) is commercially available under the tradename Carde 70429.

鉴于皮肤的感觉、皮肤的外貌和乳液的相容性,本发明优选使用的消光剂是包裹的颜料。可以用诸如氨基酸如赖氨酸、聚硅氧烷、月桂酰化合物、胶原、聚乙烯、卵磷脂和酯油的化合物来处理颜料。首选的消光剂是有机硅(聚硅氧烷)处理的颜料,例如聚硅氧烷处理的二氧化钛。首选,聚硅氧烷处理的锐钛矿二氧化钛。Matting agents preferred for use in the present invention are encapsulated pigments in view of skin feel, skin appearance and emulsion compatibility. Pigments can be treated with compounds such as amino acids such as lysine, polysiloxanes, lauroyl compounds, collagen, polyethylene, lecithin and ester oils. Preferred matting agents are silicone (silicone) treated pigments such as silicone treated titanium dioxide. First choice, silicone-treated anatase titanium dioxide.

非常优选的消光剂为已用选自于聚有机硅氧烷或硅烷的有机硅成分包覆的消光剂,其中包覆颜料的氢电位小于约2.0、优选地小于约1.0、更优选地小于约0.5ml、尤其小于约0.1ml H2/g包覆颜料。将颜料加入此处组合物的油相中。所用的涂层可通过共价键、物理吸附或粘附结合在颜料表面,优选地通过共价键结合在颜料表面。这里的包裹的作用是疏水性改进颜料,以便它们在水包油型乳液的油相中″可润湿″。A highly preferred matting agent is one that has been coated with a silicone component selected from polyorganosiloxanes or silanes, wherein the hydrogen potential of the coated pigment is less than about 2.0, preferably less than about 1.0, more preferably less than about 0.5 ml, especially less than about 0.1 ml H 2 /g coated pigment. Pigments are added to the oil phase of the compositions herein. The coating used may be bound to the pigment surface by covalent bonding, physisorption or adhesion, preferably by covalent bonding. The function of the encapsulation here is to hydrophobically modify the pigments so that they are "wettable" in the oil phase of the oil-in-water emulsion.

如果使用,无机消光剂的总浓度可以是约0%-约3%,并且优选约0.1-约2.5%,优选约0.25-2%。3.长期调理皮肤状态的活性成分 If used, the total concentration of inorganic matting agents may be from about 0% to about 3%, and preferably from about 0.1% to about 2.5%, preferably from about 0.25% to 2%. 3. Active ingredients for long-term conditioning of skin condition

在非常优选的实施方案中,本发明的组合物含有安全有效量的长期调理皮肤状态的选自于维生素B3化合物、类视色素及其组合物的活性成分。前述的化合物单独使用、尤其是以高含量使用时,可造成粘的感觉。但已发现,这种粘的感觉可通过使用本发明的有机颗粒抵消。本发明的组合物优选地含有约0.1%到约15%、更优选地约0.3%到约10%、甚至更优选地约1到约5%的活性成分。这些活性成分的具体例子包括下述化合物。A.维生素B3 化合物 In a highly preferred embodiment, the compositions of the present invention contain a safe and effective amount of an active ingredient selected from the group consisting of vitamin B3 compounds, retinoids, and combinations thereof for long-term conditioning of the skin condition. The aforementioned compounds can cause a sticky feeling when used alone, especially at high levels. However, it has been found that this sticky feeling can be counteracted by using the organic particles of the present invention. The compositions of the present invention preferably contain from about 0.1% to about 15%, more preferably from about 0.3% to about 10%, even more preferably from about 1% to about 5%, active ingredient. Specific examples of these active ingredients include the following compounds. A. Vitamin B3 Compound

本文中,″维生素B3化合物″指具有下式的化合物: As used herein, "vitamin B3 compound" refers to a compound having the following formula:

其中R是-CONH2(即,烟酰胺)、-COOH(即,烟酸)或-CH2OH(即烟醇);其衍生物和任何上述物质的盐。wherein R is -CONH2 (ie, nicotinamide), -COOH (ie, niacin), or -CH2OH (ie, nicotinol); derivatives thereof and salts of any of the foregoing.

上述维生素B3化合物的示例性衍生物包括烟酸酯,包括烟酸的非血管舒张酯、烟基氨基酸、羧酸的烟醇酯、烟酸N-氧化物和烟酰胺N-氧化物。本文中,″非血管舒张″指在将本组合物施用于皮肤之后,酯并不常常产生可见的潮红反应(大多数普通人将不经历可见的潮红反应,虽然这样的化合物可能造成肉眼看不见的血管舒张,即酯是非发红性的)。烟酸的非血管舒张酯包括生育酚烟酸酯和肌醇六烟酸酯;生育酚烟酸酯是优选的。Exemplary derivatives of the aforementioned vitamin B3 compounds include nicotinic acid esters, including non-vasodilating esters of nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide, and nicotinamide N-oxide. As used herein, "non-vasodilating" means that esters do not often produce a visible flushing response following application of the present composition to the skin (most normal people will not experience a visible flushing response, although such compounds may cause invisible flushing to the naked eye. vasodilation, i.e. the ester is non-erythrotic). Non-vasodilating esters of niacin include tocopheryl nicotinate and inositol hexanatinate; tocopheryl nicotinate is preferred.

维生素B3化合物的其它衍生物是由一或多个酰氨基氢的取代产生的烟酰胺衍生物。适用于本发明的烟酰胺的实例包括烟基氨基酸(得自例如活化的烟酸化合物(例如烟酸叠氮化物或烟基氯化物)与氨基酸的反应)和有机羧酸(例如C1-C18)的烟醇酯。这种衍生物的具体实例包括烟酰甘氨酸(C8H8N2O3)和烟基异羟肟酸(C6H6N2O2)。示例性的烟醇酯包括羧酸水杨酸、乙酸、乙醇酸、棕榈酸等的烟醇酯。可用于本发明的维生素B3化合物的其它非限定性例子是2-氯烟酰胺、6-甲基烟酰胺、N-甲基烟酰胺和烟胺哌嗪。Other derivatives of vitamin B3 compounds are nicotinamide derivatives resulting from substitution of one or more amido hydrogens. Examples of nicotinamides suitable for use in the present invention include nicotinyl amino acids (obtained, for example, from the reaction of an activated nicotinic acid compound (such as nicotinic acid azide or nicotinyl chloride) with an amino acid) and organic carboxylic acids (such as C1-C18) of nicotinol esters. Specific examples of such derivatives include nicotinyl glycine (C 8 H 8 N 2 O 3 ) and nicotinyl hydroxamic acid (C 6 H 6 N 2 O 2 ). Exemplary nicotinol esters include nicotinol esters of the carboxylates salicylic acid, acetic acid, glycolic acid, palmitic acid, and the like. Other non-limiting examples of vitamin B3 compounds useful in the present invention are 2-chloronicotinamide, 6-methylnicotinamide, N-methylnicotinamide, and nicotinamide.

上述维生素B3化合物的实例是本领域公知的,并且可有许多来源,例如Sigma化学公司(St.Louts,MO);ICN Biomedicals公司(Irvin,CA)和Aldrich化学公司(Milwaukee,WI)。Examples of the aforementioned vitamin B3 compounds are well known in the art and are available from many sources such as Sigma Chemical Company (St. Louts, MO); ICN Biomedicals Company (Irvin, CA) and Aldrich Chemical Company (Milwaukee, WI).

本发明可以使用一种或多种维生素B3化合物。优选的维生素B3化合物是烟酰胺和生育酚烟酸酯。烟酰胺更为优选。One or more vitamin B3 compounds may be used in the present invention. Preferred vitamin B3 compounds are niacinamide and tocopheryl nicotinate. Niacinamide is more preferred.

也可以使用维生素B3化合物的盐。可用于本发明的实例包括有机或无机盐,如与阴离子无机物形成的无机盐(例如氯化物)和有机酸羧酸盐。维生素B3化合物的这些和其它盐是本领域技术人员容易制备的,例如W.Wenner″L-抗坏血酸和D-异抗坏血酸与烟酸及其酰胺的反应″,有机化学杂志,第14卷,22-26页(1949)中所描述的。Wenner描述了烟酰胺的抗坏血酸盐的合成。Salts of vitamin B3 compounds may also be used. Examples that can be used in the present invention include organic or inorganic salts such as inorganic salts formed with anionic inorganic substances (eg chlorides) and organic acid carboxylates. These and other salts of vitamin B3 compounds are readily prepared by those skilled in the art, for example W. Wenner "Reaction of L-ascorbic acid and D-isoascorbic acid with niacin and its amides", Journal of Organic Chemistry, Vol. 14, 22 - as described on page 26 (1949). Wenner describes the synthesis of the ascorbate salt of nicotinamide.

在一个优选的实施方案中,维生素B3化合物的环氮是未复合的,或者在向皮肤输送之后变成未复合的。更优选,维生素B3化合物是本质上未复合的。因此,如果组合物中含有盐或其它复合形式的维生素B3化合物,当将组合物施用于皮肤时,这种复合物优选是基本上可逆的。这种复合物在pH约5.0-约6.0下应该为基本上可逆的。这种可逆性易被本领域常现技术人员所确定。在优选的实施方案中,维生素B3化合物一般含有少于约50%的呈盐形式的化合物。In a preferred embodiment, the ring nitrogen of the vitamin B3 compound is uncomplexed, or becomes uncomplexed after delivery to the skin. More preferably, the vitamin B3 compound is essentially uncomplexed. Thus, if a salt or other complexed form of the vitamin B3 compound is included in the composition, such complexing is preferably substantially reversible when the composition is applied to the skin. This complex should be substantially reversible at a pH of about 5.0 to about 6.0. Such reversibility is readily determined by one of ordinary skill in the art. In preferred embodiments, the vitamin B3 compound generally contains less than about 50% of the compound in salt form.

所包含的维生素B3化合物可以是基本上纯的物质,或为从天然(如植物)来源中通过合适物理和/或化学分离的提取物。维生素B3化合物优选为基本上纯的,其含义是指从天然来源中获得时基本上不含杂质。基本上纯的化合物可以溶液的形式提供,其中选择性地含有抗氧化剂或其它稳定剂。B. 类视色素 The vitamin B3 compound may be included as substantially pure material, or as an extract by suitable physical and/or chemical isolation from a natural (eg plant) source. The vitamin B3 compound is preferably substantially pure, which means that it is substantially free of impurities when obtained from a natural source. Substantially pure compounds may be provided in solution, optionally containing antioxidants or other stabilizers. B. Retinoids

本文中,″类视色素″包括维生素A或在皮肤中具有维生素A的生物学活性的视黄醇类似物化合物以及这些化合物的几何异构体和立体异构体的所有天然和/或合成类似物。类视色素优选为视黄醇、视黄醇酯(例如视黄醇的C2-C22烷基酯,包括棕榈酸视黄酯、乙酸视黄酯、丙酸视黄酯)、视黄醛和/或视黄酸(包括所有反式视黄酸和/或13-顺式视黄酸)或其酯,如生育酚视黄酸酯,优选不是视黄酸的类视色素。这些化合物是本领域所公知的,并且可商购自许多来源,例如Sigma化学公司(St.Louts,MO)和Boerhinger Mannheim(Indianapolis,IN)。其它可用于本发明的类视色素描述于US专利4,677,120(1987年6月30日授予Parish等);US专利4,885,311(1989年12月5日授予Parish等);US专利5,049,584(1991年9月17日授予Purcell等);US专利5,124,356(1992年6月23日授予Purcell等)和US专利34,075(1992年9月22日授予Purcell等)。优选的类视色素是视黄醇酯,如棕榈酸视黄酯、乙酸视黄酯和丙酸视黄酯。首选丙酸视黄酯和棕榈酸视黄酯。As used herein, "retinoids" include all natural and/or synthetic analogues of vitamin A or retinol analog compounds having the biological activity of vitamin A in the skin, as well as geometric and stereoisomers of these compounds. things. The retinoid is preferably retinol, retinyl esters (e.g. C2 - C22 alkyl esters of retinol, including retinyl palmitate, retinyl acetate, retinyl propionate), retinal and/or retinoic acid (including all trans-retinoic acid and/or 13-cis-retinoic acid) or esters thereof, such as tocopheryl retinoate, preferably retinoids other than retinoic acid. These compounds are well known in the art and are commercially available from a number of sources such as Sigma Chemical Company (St. Louts, MO) and Boerhinger Mannheim (Indianapolis, IN). Other retinoids useful in the present invention are described in US Patent 4,677,120 (issued June 30, 1987 to Parish et al); US Patent 4,885,311 (issued December 5, 1989 to Parish et al); issued to Purcell et al. on June 23, 1992); US Patent 5,124,356 (issued to Purcell et al. on June 23, 1992) and US Patent 34,075 (issued to Purcell et al. on September 22, 1992). Preferred retinoids are retinyl esters such as retinyl palmitate, retinyl acetate and retinyl propionate. Retinyl propionate and retinyl palmitate are preferred.

类视色素可以基本上纯的原料、或以通过适当的物理和/或化学分离从天然(如植物)来源提取得到的形式加入。类视色素优选地为基本上纯的原料。The retinoids may be added as substantially pure starting material, or in a form extracted by suitable physical and/or chemical isolation from natural (eg, plant) sources. The retinoids are preferably substantially pure starting materials.

本发明的组合物非必需地含有安全有效量的类视色素,这样得到的组合物可安全有效地调理皮肤状态,优选地调理可见的和/或能触知的皮肤中的不连续,更优选地调理皮肤老化的征兆,甚至更优选地调理可见的和/或能触知的与皮肤老化有关的皮肤质地中的不均匀。组合物优选含有约0.005%-约2%、更优选0.01%-约2%的类视色素。视黄醇的使用量首选为约0.01%-或约0.15%;视黄醇酯的使用量首选为约0.01%-约2%(例如约1%);视黄酸的使用量首选为约0.01%-约0.25%;生育酚视黄酸酯的使用量首选为约0.01-约2%。该组合物可以同时包含类视色素和维生素B3化合物。4.柔肤剂 The compositions of the present invention optionally contain a safe and effective amount of a retinoid, such that the resulting composition safely and effectively regulates the condition of the skin, preferably a visible and/or tactile discontinuity in the skin, more preferably Signs of skin aging, and even more preferably, visible and/or tactile unevenness in skin texture associated with skin aging are addressed. The compositions preferably contain from about 0.005% to about 2%, more preferably from 0.01% to about 2%, of a retinoid. Retinol is preferably used at about 0.01% - or about 0.15%; retinol esters are preferably used at about 0.01% - about 2% (eg, about 1%); retinoic acid is preferably used at about 0.01% % to about 0.25%; tocopheryl retinoate is preferably used in an amount of about 0.01 to about 2%. The composition may contain both a retinoid and a vitamin B3 compound. 4. Skin softener

本发明的局部用组合物中含有约1%-约50%、优选约3%-约15%皮肤学可接受的柔肤剂。柔肤剂趋于润滑皮肤,增加皮肤光滑感和柔软感,防止或缓减皮肤干燥和/或保护皮肤。柔肤剂一般来说是与水不能混合的油性或蜡状物质。已知各种适宜的柔肤剂并且可以用于本发明。Sagarin,化妆品科学和技术(Cosmetics,Science and Technology)第2版,Vol.1,pp.32-43(1972)中介绍了很多实例适合作为柔肤剂的材料。柔肤剂的举例说明性的实例包括:i)具有约7-约40碳原子的直链和支链烃,例如十二烷、角鲨烷、胆固醇、氢化聚异丁烯、异十六烷,以及C7-C40异链烷烃,其是C7-C40支链烃。ii)C1-C30羧酸和C2-C30二羧酸的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、二十二烷醇二十二烷酸酯、马来酸二辛酯、己二酸二异丙酯和二亚油酸二异丙酯。iii)C1-C30羧酸及其乙氧基化衍生物的单酸、二酸和三酸甘油酯,例如三辛酸/癸酸甘油酯、PEG-6三辛酸/癸酸甘油酯。iv)C1-C30羧酸的亚烷基二醇酯,如C1-C30羧酸的乙二醇一和二酯及丙二醇一和二酯,例如乙二醇二硬脂酸酯。v)糖和相关物质的C1-C30一酯或多酯。这些酯由糖或多元醇部分和一个或多个羧酸部分构成。根据构成酸和糖,这些酯在室温下可以是液体或固体形式。其实例包括:葡萄糖四油酸酯、油酸的半乳糖四酯、山梨糖醇四油酸酯、蔗糖四油酸酯、蔗糖五油酸酯、蔗糖六油酸酯、蔗糖七油酸酯、蔗糖八油酸酯、其中羧酸酯部分是1∶2摩尔比棕榈油酸酯和花生酸酯的山梨糖醇六酯和其中用于酯化的羧酸部分是1∶3∶4摩尔比月桂酸根、亚油酸根和二十二烷酸根的蔗糖八酯。其它物质包括蔗糖的棉籽油或大豆油脂肪酸酯。这种物质的其它实例可见引入此供参考的WO96/16636。一种特别优选的物质是INCI命名的蔗糖多棉籽酸酯。vi)有机聚硅氧烷油。有机聚硅氧烷油可以是挥发性、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″非挥发性″指聚硅氧烷在周围环境条件下呈液态并且具有大于约100℃的闪点(在一个大气压下)。本文中,术语″挥发性″指所有其它的聚硅氧烷油。适宜的有机聚硅氧烷可以选自各种聚硅氧烷,涉及各种挥发度和粘度范围。优选非挥发性聚硅氧烷。适宜的聚硅氧烷公开于US专利5,069,897(1991.12.3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二甲基聚硅氧烷。聚烷基硅氧烷中优选是聚二甲基硅氧烷。vii)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、油菜籽、亚麻籽油、米糠油、松油、芝麻油、向日葵籽油、前述来源的部分或完全氢化油及其混合物。viii)动物脂肪或油,如鱼肝油、羊毛脂及其衍生物,例如乙酰化羊毛脂和羊毛脂异丙酯。羊毛脂油是优选的。ix)还可以使用聚丙二醇的C4-C20烷基酯、聚丙二醇的C1-C20羧酸酯和二-C8-C30烷基酯,其实例包括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。The topical compositions of the present invention comprise from about 1% to about 50%, preferably from about 3% to about 15%, of a dermatologically acceptable emollient. Emollients tend to lubricate the skin, increase the smoothness and suppleness of the skin, prevent or relieve dryness of the skin and/or protect the skin. Skin emollients are generally oily or waxy substances that are immiscible with water. A wide variety of suitable skin emollients are known and can be used in the present invention. Sagarin, Cosmetics, Science and Technology 2nd Edition, Vol. 1, pp. 32-43 (1972) describes many examples of materials suitable as skin emollients. Illustrative examples of emollients include: i) straight and branched chain hydrocarbons having from about 7 to about 40 carbon atoms, such as dodecane, squalane, cholesterol, hydrogenated polyisobutylene, isohexadecane, and C 7 -C 40 isoparaffins, which are C 7 -C 40 branched chain hydrocarbons. 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, stearyl isopropyl behenate, behenyl behenate, dioctyl maleate, diisopropyl adipate and diisopropyl dilinoleate. iii) Mono-, di- and triglycerides of C 1 -C 30 carboxylic acids and their ethoxylated derivatives, eg tricaprylic/capric glyceride, PEG-6 tricaprylic/capric glyceride. iv) Alkylene glycol esters of C 1 -C 30 carboxylic acids, such as ethylene glycol mono- and propylene glycol mono- and diesters of C 1 -C 30 carboxylic acids, for example ethylene glycol distearate. v) C 1 -C 30 mono- or polyesters of sugars and related substances. These esters consist of 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 thereof include: glucose tetraoleate, galactose tetraoleate of oleic acid, sorbitol tetraoleate, sucrose tetraoleate, sucrose pentaoleate, sucrose hexaoleate, sucrose heptaoleate, Sucrose octaoleate, sorbitan hexaester in which the carboxylate moieties are in a 1:2 molar ratio of palmitoleate and arachidic acid esters and in which the carboxylate moieties used for esterification are in a 1:3:4 molar ratio of lauryl Sucrose octaesters of linoleate, linoleate and behenate. Other materials include cottonseed oil or soybean oil fatty acid esters of sucrose. Further examples of such materials can be found in WO 96/16636, which is hereby incorporated by reference. A particularly preferred material is the INCI name sucrose polycottonate. vi) Organopolysiloxane oils. The organopolysiloxane oil can be a volatile, nonvolatile or a mixture of volatile and nonvolatile silicones. "Non-volatile" herein means that the polysiloxane is liquid at ambient conditions and has a flash point (at one atmosphere) of greater than about 100°C. Herein, the term "volatile" refers to all other silicone oils. Suitable organopolysiloxanes can be selected from a wide variety of polysiloxanes, covering various volatility and viscosity ranges. 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. Polydimethylsiloxane is preferred among the polyalkylsiloxanes. vii) Vegetable oils and hydrogenated vegetable oils. Examples of vegetable oils 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 seed oil, partially or fully hydrogenated oils from the aforementioned sources and mixtures thereof. viii) Animal fats or oils such as cod liver oil, lanolin and their derivatives such as acetylated lanolin and lanolin isopropyl ester. Lanolin oil is preferred. ix) C 4 -C 20 alkyl esters of polypropylene glycol, C 1 -C 20 carboxylic acid esters and di-C 8 -C 30 alkyl esters of polypropylene glycol can also be used, examples of which include PPG-14 butyl ether, PPG-15 stearyl ether, dioctyl ether, dodecyl octyl ether and mixtures thereof.

本发明的非常优选的组合物含有约2%到约20%、优选地约3%到约10%、更优选地约3%到约8%的接触角小于约40°的作为柔肤剂的高铺展性油。这些高铺展性油适用于将维生素B3化合物散布在皮肤上并适用于提供整个柔肤剂体系中润滑性和铺展性间的适当的平衡。优选地整个柔肤剂体系的相对重量的选取要使整个油相的接触角小于约40°、优选地小于约35°、更优选地小于约30°。优选的高铺展性油选自于:i)  重均分子量为约100-约1000的支链烃,和ii)  下式I的液体酯类柔肤剂:

Figure A0180384900161
Highly preferred compositions of the present invention contain from about 2% to about 20%, preferably from about 3% to about 10%, more preferably from about 3% to about 8%, of an emollient as an emollient having a contact angle of less than about 40°. High spreading oil. These high spreading oils are suitable for spreading the vitamin B3 compound over the skin and for providing the proper balance of lubricity and spreading throughout the emollient system. Preferably the relative weights of the total emollient system are selected such that the total oil phase has a contact angle of less than about 40°, preferably less than about 35°, more preferably less than about 30°. Preferred high spreading oils are selected from: i) branched chain hydrocarbons having a weight average molecular weight of from about 100 to about 1000, and ii) liquid ester emollients of formula I below:
Figure A0180384900161

                                  式I其中R1选自H或CH3,R2、R3和R4独立地选自C1-C20直链或支链烷基,并且x是1-20的整数。Formula I wherein R 1 is selected from H or CH 3 , R 2 , R 3 and R 4 are independently selected from C 1 -C 20 straight chain or branched chain alkyl, and x is an integer of 1-20.

支链烃的适宜实例包括异十二烷,异十六烷和异二十烷。优选异十六烷。本文中,聚(α-烯烃)抗粘剂一般也属于支链烃,以下将作详细描述。当使用这种抗粘剂时,则考虑其用量应当包括在上述高铺展性油的含量范围内。Suitable examples of branched chain hydrocarbons include isododecane, isohexadecane and isoeicosane. Isohexadecane is preferred. Herein, poly(alpha-olefin) antiblocking agents also generally belong to branched chain hydrocarbons, which will be described in detail below. When using this anti-adhesive agent, it should be considered that its amount should be included in the content range of the above-mentioned high-spreading oil.

适宜的上述式I的酯类柔肤剂物质包括异硬脂酸甲酯,异硬脂酸异丙酯,新戊酸异硬脂基酯,异壬酸异壬酯,辛酸异癸酯,异壬酸异癸酯,异壬酸十三烷基酯,辛酸肉豆蔻酯,壬酸辛酯,异壬酸辛酯,肉豆蔻酸肉豆蔻酯,新戊酸肉豆蔻基酯,新戊酸异硬脂基酯,辛酸肉豆蔻酯,丙酸肉豆蔻酯,肉豆蔻酸异丙酯及其混合物。优选用于本发明的酯类柔肤剂是异壬酸异壬酯,新戊酸异硬脂基酯,异硬脂酸甲酯,异硬脂酸异丙酯,硬脂酸异丙酯,肉豆蔻酸异丙酯及其混合物。Suitable ester emollient materials of formula I above include methyl isostearate, isopropyl isostearate, isostearyl neopentanoate, isononyl isononanoate, isodecyl octanoate, Isodecyl Nonanoate, Tridecyl Isononanoate, Myristyl Caprylate, Octyl Nonanoate, Octyl Isononanoate, Myristyl Myristate, Myristyl Neopentanoate, Isostearyl Neopentanoate Ester, Myristyl Caprylate, Myristyl Propionate, Isopropyl Myristate and mixtures thereof. Preferred ester emollients for use herein are isononyl isononanoate, isostearyl neopentanoate, methyl isostearate, isopropyl isostearate, isopropyl stearate, Isopropyl myristate and mixtures thereof.

特别优选用于本发明的高铺展性油是异十六烷,异壬酸异壬酯,异硬脂酸甲酯,异硬脂酸异丙酯或其混合物。5. 抗粘剂 Particularly preferred high spreading oils for use herein are isohexadecane, isononyl isononanoate, methyl isostearate, isopropyl isostearate or mixtures thereof. 5. Anti-sticking agent

尤其是当本发明组合物使用增加含量的甘油或维生素B3化合物,尤其是烟酰胺时,包含约0.3%-约4%、优选约0.5%-约2.5%、更优选约1%-约2%的抗粘剂是有益的,优选的抗粘剂选自MW为约260-约1000的聚(α-烯烃)和吸留剂(occlusive agent),其中所说的吸留剂选自矿脂、蓖麻油酸鲸蜡酯和羊毛脂。尽管不完全了解,似乎聚(α-烯烃)抗粘剂和吸留抗粘剂通过不同的机理起作用。虽然如此,两者对降低与高含量甘油或维生素B3化合物相关的粘性皮肤感觉都是有效的。尽管不排除抗粘剂的混合物,但最好的效果是当抗粘剂只选自这两种类型中的一种时获得的。Especially when compositions of the present invention employ increased levels of glycerin or vitamin B3 compounds, especially niacinamide, comprising from about 0.3% to about 4%, preferably from about 0.5% to about 2.5%, more preferably from about 1% to about 2% The anti-sticking agent is beneficial, and the preferred anti-sticking agent is selected from poly(alpha-olefin) and occlusive agent (occlusive agent) with MW of about 260 to about 1000, wherein said occlusive agent is selected from petrolatum, Cetyl ricinoleate and lanolin. Although not fully understood, it appears that poly(alpha-olefin) antiadhesives and occluded antiadhesives work by different mechanisms. Nonetheless, both are effective in reducing the sticky skin sensation associated with high levels of glycerin or vitamin B3 compounds. Although mixtures of anti-sticking agents are not excluded, the best results are obtained when the anti-sticking agent is selected from only one of these two types.

适宜的上述聚(α-烯烃)可以获得自具有约6-约14碳原子、优选约6-约12碳原子、特别是约8-约12碳原子的1-链烯烃单体。可用于本发明的聚(α-烯烃)优选是氢化聚(α-烯烃)低聚物。用于制备本发明聚(α-烯烃)低聚物用的1-链烯烃单体包括1-己烯,1-辛烯,1-癸烯,1-十二碳烯,1-十四碳烯,诸如4-甲基-1-戊烯的支链异构体及其组合。首选是1-辛烯至1-十二碳烯的低聚物或其组合。优选聚癸烯。适宜的聚癸烯可从Mobil化学公司(P.O.Box 3140,Edison,新泽西08818,USA)以商品名Puresyn_4和从BP Amoco(200 E.Randolph Drive,芝加哥,IL 60601-7125)以商品名Silkflo_364 NF商购获得。Suitable poly(alpha-olefins) as described above can be obtained from 1-alkene monomers having from about 6 to about 14 carbon atoms, preferably from about 6 to about 12 carbon atoms, especially from about 8 to about 12 carbon atoms. The poly(alpha-olefin)s useful in the present invention are preferably hydrogenated poly(alpha-olefin) oligomers. The 1-alkene monomers useful in preparing the poly(alpha-olefin) oligomers of the present invention include 1-hexene, 1-octene, 1-decene, 1-dodecene, 1-tetradecene Alkenes, such as branched isomers of 4-methyl-1-pentene, and combinations thereof. Preferred are oligomers of 1-octene to 1-dodecene or combinations thereof. Polydecene is preferred. Suitable polydecenes are available from Mobil Chemical Company (POBox 3140, Edison, NJ 08818, USA) under the tradename Puresyn_4 and from BP Amoco (200 E. Randolph Drive, Chicago, IL 60601-7125) under the tradename Silkflo_ 364 NF is commercially available.

首选作为抗粘剂的是矿脂。6. 保湿剂 The preferred anti-sticking agent is petrolatum. 6. Moisturizer

非常优选的可选组分是保湿剂,特别是多元醇型。典型的多元醇包括聚亚烷基二醇,更优选亚烷基二醇及其衍生物,包括丙二醇,二丙二醇,聚丙二醇,聚乙二醇及其衍生物,山梨糖醇,羟丙基山梨糖醇,赤藓糖醇,苏糖醇,五赤藓糖醇,木糖醇,葡萄糖醇,甘露糖醇,己二醇,丁二醇(如1,3-丁二醇),己三醇(如1,2,6-己三醇),甘油,乙氧基化甘油和丙氧基化甘油。A highly preferred optional component is a humectant, especially of the polyol type. Typical polyols include polyalkylene glycols, more preferably alkylene glycols and their derivatives, including propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol and its derivatives, sorbitol, hydroxypropyl sorbitol Sugar alcohol, erythritol, threitol, pentaerythritol, xylitol, glucitol, mannitol, hexanediol, butylene glycol (such as 1,3-butanediol), hexanetriol (such as 1,2,6-hexanetriol), glycerin, ethoxylated glycerin and propoxylated glycerin.

本发明还可以使用2-吡咯烷酮-5-羧酸钠,胍;羟乙酸和甘醇酸盐(如铵和季烷基铵);乳酸和乳酸盐(如铵和季烷基铵);各种形式的库拉索芦荟(如库拉索芦荟凝胶);透明质酸及其衍生物(如盐衍生物,例如透明质酸钠);乳酰胺一乙醇胺;乙酰胺一乙醇胺;尿素;泛醇;焦谷氨酸钠(NaPCA),水溶性聚(甲基)丙烯酸甘油酯润滑剂(如Hispagel_)及其混合物。The present invention can also use sodium 2-pyrrolidone-5-carboxylate, guanidine; glycolic acid and glycolate (such as ammonium and quaternary alkyl ammonium); lactic acid and lactate (such as ammonium and quaternary alkyl ammonium); forms of Aloe vera (such as Aloe vera gel); hyaluronic acid and its derivatives (such as salt derivatives, such as sodium hyaluronate); lactamide monoethanolamine; acetamide monoethanolamine; urea; alcohol; sodium pyroglutamate (NaPCA), water-soluble glyceryl poly(meth)acrylate lubricants (such as Hispagel _ ) and mixtures thereof.

上述的化合物可以单独掺加或联合掺加。优选的保湿剂选自甘油,聚丙烯酸甘油酯,尿素,泛醇及其混合物。7.乳化剂/表面活性剂 The above-mentioned compounds may be added alone or in combination. Preferred humectants are selected from glycerin, glyceryl polyacrylate, urea, panthenol and mixtures thereof. 7. Emulsifier/surfactant

本发明的组合物优选含有乳化剂和/或表面活性剂,以有助于使不连续相分散和悬浮于连续相之内。如果产品欲用于皮肤清洁,则表面活性剂也是有用的。下面为方便起见,本文将乳化剂归于术语″表面活性剂″的范围内,因此″表面活性剂″用来泛指起乳化剂作用或起其它表面活性剂如皮肤清洁作用的表面活性剂。组合物中可以使用已知或常规的表面活性剂,只要所选择的试剂是与组合物的必要组分在化学性质上和物理性质相容,并能够提供所需的分散特征。适宜的试剂包括聚硅氧烷物质、非-聚硅氧烷物质及其混合物。The compositions of the present invention preferably contain emulsifiers and/or surfactants to assist in dispersing and suspending the discontinuous phase within the continuous phase. Surfactants are also useful if the product is intended for skin cleansing. For convenience below, emulsifiers are included within the term "surfactant" herein, and "surfactant" is therefore used to broadly refer to surfactants that function as emulsifiers or other surfactants such as skin cleansers. Known or conventional surfactants may be used in the composition provided that the agent is selected to be chemically and physically compatible with the essential components of the composition and to provide the desired dispersion characteristics. Suitable agents include silicone materials, non-silicone materials and mixtures thereof.

本发明的组合物优选含有约0.05%-约15%的表面活性剂或表面活性剂混合物。根据组合物的pH值和所存在的其它组分来选择确切的表面活性剂或表面活性剂混合物。The compositions of the present invention preferably contain from about 0.05% to about 15% of a surfactant or mixture of surfactants. The exact surfactant or mixture of surfactants will be selected based on the pH of the composition and the other components present.

优选的亲水表面活性剂是非离子表面活性剂。可用于本发明的非离子表面活性剂是那些可以广泛地定义为长链醇(如C8-30醇)与糖或淀粉聚合物(即糖苷)之缩合产物的非离子表面活性剂。这些化合物可由式(S)n-O-R表示,其中S是糖部分,如葡萄糖、果糖、甘露糖和半乳糖;n是约1-约1000的整数并且R是C8-30烷基。可以提供烷基的长链醇的实例包括癸醇、鲸蜡醇、硬脂醇、月桂醇、十四烷醇、油醇等等。这些表面活性剂的优选实例包括那些其中S是葡萄糖部分、R是C8-20烷基且n为约1-约9整数的表面活性剂。这些表面活性剂的可商购获得的实例包括癸基聚葡糖苷(可以APG325 CS得自Henkel)、和月桂基聚葡糖苷(可以APG 600 CS和625 CS得自Henkel)。Preferred hydrophilic surfactants are nonionic surfactants. Nonionic surfactants useful in the present invention are those that can be broadly defined as condensation products of long chain alcohols (eg C8-30 alcohols) with sugar or starch polymers (ie glycosides). These compounds can be represented by the formula (S)nOR, wherein S is a sugar moiety such as glucose, fructose, mannose, and galactose; n is an integer from about 1 to about 1000 and R is a C8-30 alkyl group. Examples of long chain alcohols from which the alkyl group may be provided include decyl alcohol, cetyl alcohol, stearyl alcohol, lauryl alcohol, myristyl alcohol, oleyl alcohol, and the like. Preferred examples of these surfactants include those wherein S is a glucose moiety, R is a C8-20 alkyl group, and n is an integer from about 1 to about 9. Commercially available examples of these surfactants include decyl polyglucoside (available as APG 325 CS from Henkel), and lauryl polyglucoside (available as APG 600 CS and 625 CS from Henkel).

其它有用的非离子表面活性剂包括环氧烷与脂肪酸的缩合产物(即脂肪酸的环氧烷酯)。这些物质具有通式RCO(X)nOH,其中R是C10-30烷基,X是-OCH2CH2-(即得自己二醇或环氧乙烷)或-OCH2CHCH3-(即得自丙二醇或环氧丙烷),n是约6-约200的整数。其它非离子表面活性剂是环氧烷与2摩尔脂肪酸的缩合产物(即脂肪酸的环氧烷二酯)。这些物质具有通式RCO(X)nOOCR,其中R是C10-30烷基,X是-OCH2CH2-(即得自己二醇或环氧乙烷)或-OCH2CHCH3-(即得自丙二醇或环氧丙烷),并且n是约6-约100的整数。其它的非离子表面活性剂是环氧烷与脂肪醇的缩合产物(即脂肪醇的环氧烷醚)。这些物质具有通式R(X)nOR’,其中R是C10-30烷基,X是-OCH2CH2-(即得自己二醇或环氧乙烷)或-OCH2CHCH3-(即得自丙二醇或环氧丙烷),并且n是约6-约100的整数,并且R’是H或C10-30烷基。另一些其它的非离于表面活性剂是环氧烷同时与脂肪酸和脂肪醇的缩合产物[即其中聚环氧烷部分在一端被脂肪酸酯化,并在另一端被脂肪醇醚化(经由醚键连接)]。这些物质具有通式RCO(X)nOR’,其中R和R’是C10-30烷基,X是-OCH2CH2-(即得自己二醇或环氧乙烷)或-OCH2CHCH3-(即得自丙二醇或环氧丙烷),并且n是约6-约100的整数,其实例包括十六烷基聚氧乙烯醚-6、十六烷基聚氧乙烯醚-10、十六烷基聚氧乙烯醚-12、ceteareth-6、ceteareth-10、ceteareth-12、steareth-6、steareth-10、steareth-12、PEG-6硬脂酸酯、PEG-10硬脂酸酯、PEG-100硬脂酸酯、PEG-12硬脂酸酯、PEG-20硬脂酸甘油酯、PEG-80牛油酸甘油酯、PEG-10硬脂酸甘油酯、PEG-30椰油酸甘油酯、PEG-80椰油酸甘油酯、PEG-200牛油酸甘油酯、PEG-8二月桂酸酯、PEG-10二硬脂酸酯及其混合物。Other useful nonionic surfactants include condensation products of alkylene oxides with fatty acids (ie, alkylene oxide esters of fatty acids). These substances have the general formula RCO(X)nOH, where R is a C 10-30 alkyl group and X is -OCH 2 CH 2 - (ie hexanediol or ethylene oxide) or -OCH 2 CHCH 3 - (ie derived from propylene glycol or propylene oxide), n is an integer from about 6 to about 200. Other nonionic surfactants are condensation products of alkylene oxides with 2 moles of fatty acids (ie, alkylene oxide diesters of fatty acids). These materials have the general formula RCO(X)nOOCR, where R is a C 10-30 alkyl group, X is -OCH 2 CH 2 - (ie, hexanediol or ethylene oxide) or -OCH 2 CHCH 3 - (ie, derived from propylene glycol or propylene oxide), and n is an integer from about 6 to about 100. Other nonionic surfactants are condensation products of alkylene oxides with fatty alcohols (ie, alkylene oxide ethers of fatty alcohols). These substances have the general formula R(X)nOR', where R is a C10-30 alkyl group and X is -OCH 2 CH 2 - (ie hexanediol or ethylene oxide) or -OCH 2 CHCH 3 - (ie derived from propylene glycol or propylene oxide), and n is an integer from about 6 to about 100, and R' is H or C 10-30 alkyl. Still other non-ionic surfactants are condensation products of alkylene oxides with both fatty acids and fatty alcohols [i.e. where the polyalkylene oxide moiety is esterified at one end with a fatty acid and at the other end with a fatty alcohol etherified (via ether linkage)]. These materials have the general formula RCO(X)nOR', where R and R' are C 10-30 alkyl, and X is -OCH 2 CH 2 - (ie, hexanediol or ethylene oxide) or -OCH 2 CHCH 3 - (i.e. derived from propylene glycol or propylene oxide), and n is an integer from about 6 to about 100, examples of which include ceteth-6, ceteth-10, ceteth-10, Hexaalkyl polyoxyethylene ether-12, ceteareth-6, ceteareth-10, ceteareth-12, steareth-6, steareth-10, steareth-12, PEG-6 stearate, PEG-10 stearate, PEG-100 Stearate, PEG-12 Stearate, PEG-20 Glyceryl Stearate, PEG-80 Glyceryl Butoleate, PEG-10 Glyceryl Stearate, PEG-30 Glyceryl Cocoate Esters, PEG-80 Glyceryl Cocoate, PEG-200 Glyceryl Butanoate, PEG-8 Dilaurate, PEG-10 Distearate, and mixtures thereof.

另一些其它的有用的非离子表面活性剂包括多羟基脂肪酸酰胺表面活性剂,其在WO98/04241中有详细描述。Still other useful nonionic surfactants include the polyhydroxy fatty acid amide surfactants which are described in detail in WO 98/04241.

优选的非离子表面活性剂选自steareth-2、steareth-21、ceteareth-20、ceteareth-12、蔗糖椰油酸酯、steareth-100、PEG-100硬脂酸酯及其混合物。Preferred nonionic surfactants are selected from steareth-2, steareth-21, ceteareth-20, ceteareth-12, sucrose cocoate, steareth-100, PEG-100 stearate and mixtures thereof.

适用于本发明的其它非离子表面活性剂包括糖酯和多酯、烷氧基化糖酯和多酯、C1-C30脂肪醇的C1-C30脂肪酸酯、C1-C30脂肪醇的C1-C30脂肪酸酯的烷氧基化衍生物、C1-C30脂肪酸的烷氧基化醚、C1-C30脂肪酸的聚甘油酯、多元醇的C1-C30酯、多元醇的C1-C30醚、烷基磷酸酯、聚氧化亚烷基脂肪醚磷酸酯、脂肪酸酰胺、酰基乳酸酯及其混合物。这些不含硅的表面活性剂的非限定性实例包括:聚山梨酸酯20、聚乙二醇5大豆甾醇、Steareth-20、Ceteareth-20、PPG-2甲基葡萄糖醚二硬脂酸酯、十六烷基聚氧乙烯醚-10、聚山梨酸酯80、聚山梨酸酯60、硬脂酸甘油酯、脱水山梨糖醇一月桂酸酯、聚氧乙烯4月桂基醚硬脂酸钠、聚甘油基-4-异硬脂酸酯、月桂酸已酯、PPG-2甲基葡萄糖酸二硬脂酸酯、PEG-100硬脂酸酯及其混合物。Other nonionic surfactants suitable for use herein include sugar esters and polyesters, alkoxylated sugar esters and polyesters, C 1 -C 30 fatty acid esters of C 1 -C 30 fatty alcohols, C 1 -C 30 Alkoxylated derivatives of C 1 -C 30 fatty acid esters of fatty alcohols, alkoxylated ethers of C 1 -C 30 fatty acids, polyglycerol esters of C 1 -C 30 fatty acids, C 1 -C of polyols 30 esters, C 1 -C 30 ethers of polyols, alkyl phosphates, polyoxyalkylene fatty ether phosphates, fatty acid amides, acyl lactylates and mixtures thereof. Non-limiting examples of these silicon-free surfactants include: Polysorbate 20, Macrogol 5 Soy Sterol, Steareth-20, Ceteareth-20, PPG-2 Methyl Glucose Distearate, Cetyl polyoxyethylene ether-10, polysorbate 80, polysorbate 60, glyceryl stearate, sorbitan monolaurate, polyoxyethylene 4 lauryl ether sodium stearate, Polyglyceryl-4-isostearate, Hexyl Laurate, PPG-2 Methylgluconate Distearate, PEG-100 Stearate, and mixtures thereof.

适用于本发明的另一类乳化剂是基于脱水山梨糖醇或山梨醇脂肪酸酯和蔗糖脂肪酸酯混合物的脂肪酸酯共混物,每种情况下的脂肪酸优选为C8-C24,更优选为C10-C20。优选的脂肪酸酯乳化剂是脱水山梨糖醇或山梨醇C16-C20脂肪酸酯与蔗糖C10-C16脂肪酸酯的共混物,尤其是脱水山梨糖醇硬脂酸酯和蔗糖椰油酸酯的共混物。其可从ICI以商品名Arlatone2121商购获得。Another class of emulsifiers suitable for use in the present invention are fatty acid ester blends based on a mixture of sorbitan or sorbitol fatty acid esters and sucrose fatty acid esters, the fatty acids in each case being preferably C 8 -C 24 , More preferably C 10 -C 20 . A preferred fatty acid ester emulsifier is a blend of sorbitan or sorbitol C 16 -C 20 fatty acid esters with sucrose C 10 -C 16 fatty acid esters, especially sorbitan stearate and sucrose Cocoate blend. It is commercially available from ICI under the tradename Arlatone 2121.

可用于本发明的亲水性表面活性剂可以替换或另外包括任何各种本领域所知的阳离子、阴离子、两性离子和两性表面活性剂。参见例如McCutcheon, 洗涤剂和乳化剂,北美版(1986),由Allured出版公司公开;和US专利5,011,681(1991年4月30日授予Ciotti等)。Hydrophilic surfactants useful in the present invention may alternatively or additionally include any of a variety of cationic, anionic, zwitterionic and amphoteric surfactants known in the art. See, eg, McCutcheon, Detergents and Emulsifiers , North American Edition (1986), published by Allured Publishing Company; and US Patent 5,011,681 (Ciotti et al., issued April 30, 1991).

本发明的优选的乳液包括含聚硅氧烷的乳化剂或表面活性剂。各种聚硅氧烷乳化剂可用于本发明。这些聚硅氧烷乳化剂典型地是有机改性的有机基聚硅氧烷,本领域技术人员也称之为聚硅氧烷表面活性剂。有用的聚硅氧烷乳化剂包括聚二甲基硅氧烷共聚醇。这些物质是被改性成包括聚醚侧链的聚二甲基硅氧烷,其中所说的聚醚侧链如聚环氧乙烷链、聚环氧丙烷链、这些链的混合物以及含有得自环氧乙烷和环氧丙烷的部分的聚醚链。其它实例包括烷基改性的聚二甲基硅氧烷共聚醇,即含C2-C30垂侧链的化合物。其它有用的聚二甲基硅氧烷共聚醇包含具有各种阳离子、阴离子、两性和两性离子侧链部分的物质。8.增稠剂(包括稠化剂和胶凝剂) Preferred emulsions of the present invention include silicone-containing emulsifiers or surfactants. A variety of silicone emulsifiers are useful herein. These silicone emulsifiers are typically organically modified organopolysiloxanes, also known to those skilled in the art as silicone surfactants. Useful silicone emulsifiers include dimethicone copolyols. These materials are polydimethylsiloxanes modified to include polyether side chains such as polyethylene oxide chains, polypropylene oxide chains, mixtures of these chains, and polyether chains containing Polyether chains derived from portions of ethylene oxide and propylene oxide. Other examples include alkyl-modified dimethicone copolyols, ie compounds containing C2 - C30 pendant side chains. Other useful dimethicone copolyols include those having various cationic, anionic, amphoteric, and zwitterionic side chain moieties. 8. Thickeners (including thickeners and gelling agents)

本发明的组合物还可以含有增稠剂,一般含有约0.1%-约5%,优选约0.25%-约2%的增稠剂。The compositions of the present invention may also contain a thickening agent, typically from about 0.1% to about 5%, preferably from about 0.25% to about 2%, of a thickening agent.

适宜的增稠剂包括纤维素和衍生物,如纤维素、羧甲基羟乙基纤维素、纤维素乙酸丙酸羧酸酯、羟乙基纤维素、羟乙基乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素、甲基羟乙基纤维素、微晶纤维素、纤维素硫酸钠及其混合物。Suitable thickeners include cellulose and derivatives such as cellulose, carboxymethyl hydroxyethyl cellulose, cellulose acetate propionate carboxylate, hydroxyethyl cellulose, hydroxyethyl ethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethylcellulose, methylhydroxyethylcellulose, microcrystalline cellulose, sodium cellulose sulfate, and mixtures thereof.

其它有用的增稠剂包括阿拉伯胶、琼脂、藻胶、藻酸、藻酸铵、支链淀粉、藻酸钙、角叉菜胶钙、肉碱、角叉菜胶、糊精、明胶、洁冷胶、瓜尔豆胶、瓜尔豆羟丙基三甲基氯化铵、水辉石、透明质酸、水合二氧化硅、羟丙基脱乙酰壳多糖、羟丙基瓜尔豆胶、刺梧桐胶、海草、槐树豆胶、纳豆(natto)胶、藻酸钾、角叉菜胶钾、丙二醇藻酸酯、菌核树胶、羧甲基葡聚糖钠、角叉菜胶钠、黄蓍胶、黄原胶及其混合物。B.F.Goodrich公司市售的商品名为Carbopol树脂的丙烯酸/丙烯酸乙酯共聚物和羧基乙烯基聚合物也是有用的。适宜的Carbopol树脂在WO98/22085中描述。Other useful thickeners include gum arabic, agar, algin, alginic acid, ammonium alginate, pullulan, calcium alginate, calcium carrageenan, carnitine, carrageenan, dextrin, gelatin, Cold Gum, Guar Gum, Guar Hydroxypropyltrimonium Chloride, Hectorite, Hyaluronic Acid, Hydrated Silica, Hydroxypropyl Chitosan, Hydroxypropyl Guar Gum, Karaya gum, seaweed, locust bean gum, natto gum, potassium alginate, potassium carrageenan, propylene glycol alginate, sclerotin gum, sodium carboxymethyl dextran, sodium carrageenan , tragacanth gum, xanthan gum and mixtures thereof. Acrylic acid/ethyl acrylate copolymers and carboxyvinyl polymers commercially available under the tradename Carbopol resins from B.F. Goodrich Company are also useful. Suitable Carbopol resins are described in WO98/22085.

本发明的优选组合物含有选自以下的增稠剂:羧酸聚合物、交联的聚丙烯酸酯、聚丙烯酰胺、黄原胶及其混合物,更优选选自聚丙烯酰胺聚合物、黄原胶及其混合物。将优选的聚丙烯酰胺预分散在不能与水混容的溶剂如矿物油等中,所说的溶剂中含有帮助促进聚丙烯酰胺水分散性的表面活性剂(HLB约7-约10)。首选用于本发明的是CTFA命名为聚丙烯酰胺和异链烷烃和月桂基醚-7的非离子聚合物,它们可从Seppic公司以Sepigel 305的商品名获得。9.抗炎剂 Preferred compositions of the present invention contain a thickener selected from the group consisting of carboxylic acid polymers, cross-linked polyacrylates, polyacrylamides, xanthan gum and mixtures thereof, more preferably selected from polyacrylamide polymers, xanthan Glues and their mixtures. The preferred polyacrylamide is predispersed in a water-immiscible solvent such as mineral oil or the like, which contains a surfactant (HLB about 7 to about 10) to help promote the water dispersibility of the polyacrylamide. Preferred for use in the present invention are the nonionic polymers with the CTFA designation polyacrylamide and isoparaffin and lauryl ether-7, which are available from Seppic Corporation under the tradename Sepigel 305. 9. Anti-inflammatory agents

本发明的组合物中可以添加安全有效量的抗炎剂,优选为组合物的约0.1%-约5%,更优选为约0.1%-约2%。抗炎剂可提高本发明的皮肤外貌益处,例如,这种药剂有助于更均匀和可接受的皮肤色调或颜色。用于组合物的抗炎剂的确切量取决于所用的具体抗炎剂,因为这种药剂在效力方面变化广泛。A safe and effective amount of anti-inflammatory agent may be added to the composition of the present invention, preferably about 0.1% to about 5%, more preferably about 0.1% to about 2% of the composition. Anti-inflammatory agents can enhance the skin appearance benefits of the present invention, for example, such agents contribute to a more even and acceptable skin tone or color. The exact amount of anti-inflammatory agent used in the composition will depend on the particular anti-inflammatory agent used, since such agents vary widely in potency.

可用于本发明的抗炎剂包括甾族抗炎剂,如氢化可的松;非甾族抗炎药(NSAIDS),如布洛芬;泛醇及其醚和酯衍生物,如泛醇乙基醚、泛醇三乙酸酯;泛酸及其盐和酯衍生物,尤其是泛酸钙;库拉索芦荟、没药醇、尿囊素和甘草科(洋甘草属/种植物)的化合物,包括甘草亭酸、甘草酸及其衍生物如盐(例如甘草酸铵)和酯(硬脂基甘草亭酸酯)。10.防晒剂和遮阳剂 Anti-inflammatory agents useful in the present invention include steroidal anti-inflammatory agents, such as hydrocortisone; non-steroidal anti-inflammatory drugs (NSAIDS), such as ibuprofen; panthenol and its ether and ester derivatives, such as panthenol Panthenyl ether, panthenyl triacetate; pantothenic acid and its salt and ester derivatives, especially calcium pantothenate; aloe barbadensis, bisabolol, allantoin and compounds of the Glycyrrhizae family (Glycyrrhiza genus/species), Included are glycyrrhetinic acid, glycyrrhizinic acid and derivatives thereof such as salts (eg, ammonium glycyrrhizinate) and esters (stearyl glycyrrhetinate). 10. Sunscreens and sunblocks

本发明的组合物可以含有防晒剂。适宜的防晒剂可以是有机或无机的。特别优选的防晒剂包括丁基甲氧基二苯甲酰基甲烷、2-乙基己基-对甲氧基肉桂酸酯、苯基苯并咪唑磺酸和奥克立林。无机防晒剂包括氧化锌和二氧化钛。确切的量取决于所选择的防晒剂和所需的防晒因子(SPF)而不同,但无机防晒剂优选仅以如以上对消光剂所述的低含量使用。也可以向本发明有用的任何组合物添加一种试剂,来改善组合物的皮肤亲和性,特别是提高它们对水洗掉或擦掉的抵抗性。提供这种益处的优选的试剂是乙烯和丙烯酸的共聚物。含有这种共聚物的组合物公开在US专利4,663,157(1987年5月5日授予Brock)。11.抗氧化剂/自由基清除剂 The compositions of the present invention may contain a sunscreen. Suitable sunscreens may be organic or inorganic. Particularly preferred sunscreens include butylmethoxydibenzoylmethane, 2-ethylhexyl-p-methoxycinnamate, phenylbenzimidazole sulfonic acid and octocrylene. Inorganic sunscreens include zinc oxide and titanium dioxide. The exact amount will vary depending on the sunscreen chosen and the sun protection factor (SPF) desired, but inorganic sunscreens are preferably used only at low levels as described above for matting agents. An agent may also be added to any of the compositions useful in the present invention to improve the skin substantivity of the compositions, in particular to increase their resistance to water wash-off or rub-off. A preferred agent that provides this benefit is a copolymer of ethylene and acrylic acid. Compositions containing such copolymers are disclosed in US Patent 4,663,157 (Brock, issued May 5, 1987). 11. Antioxidant/Free Radical Scavenger

本发明的组合物中还可以含有抗氧化剂/自由基清除剂。抗氧化剂/自由基清除剂对提供保护免受UV辐射(其可以导致角质层的脱皮增加或质构变化)和免受造成皮肤伤害的其它环境试剂是特别有用的。适宜的量为组合物的约0.1%-约10%,更优选为约1%-约5%。Antioxidants/radical scavengers may also be present in the compositions of the present invention. Antioxidants/radical scavengers are particularly useful for providing protection from UV radiation (which can lead to increased desquamation or texture changes of the stratum corneum) and from other environmental agents that cause skin damage. Suitable amounts are from about 0.1% to about 10%, more preferably from about 1% to about 5%, of the composition.

可以使用的抗氧化剂/自由基清除剂例如是抗坏血酸(维生素C)及其盐、脂肪酸的抗坏血酸酯、抗坏血酸衍生物(例如抗坏血酸磷酸镁)、β-胡萝卜素、生育酚(维生素E)、生育酚山梨酸酯、生育酚乙酸酯、生育酚的其它酯、丁基化羟基苯甲酸及其盐、没食子酸及其烷基酯,特别是没食子酸丙酯、尿酸及其盐和烷基酯,山梨酸及其盐、胺类(例如N,N-二乙基羟基胺,氨基-胍)、硫氢基化合物(例如谷胱甘肽)、二羟基富马酸及其盐、生物类黄酮、赖氨酸、蛋氨酸、脯氨酸、超氧化物歧化酶、水飞蓟素、茶提取物、葡萄皮/籽提取物、黑素以及迷迭香提取物。优选的抗氧化剂/自由基清除剂选自生育酚乙酸酯、生育酚山梨酸酯和生育酚的其它酯,更优选生育酚乙酸酯。12.螯合剂 Antioxidants/radical scavengers that can be used are, for example, ascorbic acid (vitamin C) and its salts, ascorbic acid esters of fatty acids, ascorbic acid derivatives (e.g. magnesium ascorbyl phosphate), beta-carotene, tocopherol (vitamin E), tocopherol Sorbate, tocopheryl acetate, other esters of tocopherol, butylated hydroxybenzoic acid and its salts, gallic acid and its alkyl esters, especially propyl gallate, uric acid and its salts and alkyl esters, Sorbic acid and its salts, amines (such as N,N-diethylhydroxylamine, amino-guanidine), sulfhydryl compounds (such as glutathione), dihydroxyfumaric acid and its salts, bioflavonoids, Lysine, Methionine, Proline, SOD, Silymarin, Tea Extract, Grape Skin/Seed Extract, Melanin, and Rosemary Extract. Preferred antioxidants/radical scavengers are selected from tocopheryl acetate, tocopheryl sorbate and other esters of tocopherol, more preferably tocopheryl acetate. 12. Chelating agent

螯合剂的包含对提供保护免受UV辐射(其导致过度脱皮或皮肤质构变化)和免受造成皮肤伤害的其它环境试剂(其可以导致皮肤损害)是特别有用的。适宜的量为组合物的0.01%-约1%,更优选的为约0.05%-约5%。可用于本发明的螯合剂的实例是US专利5,487,884中公开的螯合剂。优选的螯合剂是乙二胺四乙酸(EDTA)、糠偶酰二肟及其衍生物。13.脱屑剂/剥离剂 The inclusion of chelating agents is particularly useful for providing protection from UV radiation (which causes excessive peeling or changes in skin texture) and from other environmental agents that cause skin damage (which can cause skin damage). Suitable amounts are from 0.01% to about 1%, more preferably from about 0.05% to about 5%, of the composition. Examples of chelating agents useful in the present invention are those disclosed in US Patent 5,487,884. Preferred chelating agents are ethylenediaminetetraacetic acid (EDTA), furildioxime and derivatives thereof. 13. Desquamation agent/stripping agent

本发明的组合物中可以添加安全有效量的脱屑剂,更优选为组合物的约0.1%-约10%、更优选为约0.2%-约5%,还优选为约0.5%-约4%。脱屑剂可增强本发明的皮肤外貌益处。例如,脱屑剂倾向于改善皮肤的质构(例如光滑性)。本领域已知各种脱屑剂,并且适用于本发明,包括有机羟基酸,如水杨酸、乙醇酸、乳酸、5-辛酰水杨酸、羟基辛酸、羟基辛酸和羊毛脂脂肪酸。一种适合用于本发明的脱屑体系含有硫氢基化合物和两性离子表面活性剂并且描述于WO 96/01101中。其它适用的脱屑体系含有水杨酸和两性离子表面活性剂并且描述于WO 95/13048。水杨酸是优选的。11.亮肤剂 A safe and effective amount of desquamation agent can be added in the composition of the present invention, more preferably about 0.1% to about 10%, more preferably about 0.2% to about 5%, and more preferably about 0.5% to about 4% of the composition. %. Desquamation agents can enhance the skin appearance benefits of the present invention. For example, desquamation agents tend to improve the texture (eg, smoothness) of the skin. Various desquamation agents are known in the art and are suitable for use in the present invention, including organic hydroxy acids such as salicylic acid, glycolic acid, lactic acid, 5-octanoyl salicylic acid, hydroxycaprylic acid, hydroxycaprylic acid, and lanolin fatty acids. One suitable desquamation system for use in the present invention comprises a sulfhydryl compound and a zwitterionic surfactant and is described in WO 96/01101. Other suitable desquamation systems contain salicylic acid and zwitterionic surfactants and are described in WO 95/13048. Salicylic acid is preferred. 11. Skin lightening agent

本发明的组合物还可以含有亮肤剂。当使用时,组合物优选含有约0.1%-约10%、更优选约0.2%-约5%、还优选约0.5%-约2%的亮肤剂。适宜的亮肤剂包括本领域已知的物质,包括曲酸、熊果苷、抗坏血酸及其衍生物,例如抗坏血酸磷酸镁。其它适合本发明使用的亮肤剂还包括WO95/34280和WO 95/23780中描述的亮肤剂。组合物的制备 The compositions of the present invention may also contain a skin lightening agent. When used, the compositions preferably contain from about 0.1% to about 10%, more preferably from about 0.2% to about 5%, still preferably from about 0.5% to about 2%, of a skin lightening agent. Suitable skin lightening agents include those known in the art, including kojic acid, arbutin, ascorbic acid and derivatives thereof, such as magnesium ascorbyl phosphate. Other skin lightening agents suitable for use in the present invention include those described in WO 95/34280 and WO 95/23780. Preparation of the composition

本发明的组合物通常用常规方法来制备,例如本领域已知的用于制备局部用组合物的方法。这些方法一般包括在一或多个步骤中将配料混合至成分至相对均匀的状态,同时有或没有加热、冷却、抽真空等等。使用方法 The compositions of the present invention are generally prepared by conventional methods, such as those known in the art for preparing topical compositions. These methods generally involve mixing the ingredients until the ingredients are brought to a relatively homogeneous state in one or more steps, with or without heating, cooling, vacuuming, and the like. Instructions

本发明的组合物用于提供更均匀的皮肤色调,特别是手部或其它身体非面部皮肤。The compositions of the present invention are useful for providing a more even skin tone, especially on the hands or other non-facial skin of the body.

可以使用各种量的本发明组合物来提供皮肤外貌和/或感觉益处。以mg组合物/cm2皮肤计,每次使用的本发明组合物的量典型地是约0.1mg/m2-约10mg/m2。特别有效的施用量是约2mg/m2。典型的施用是按照每天约一次,但施用次数可以是从每周一次至最多每天三次或更多之间变化。Compositions of the present invention may be used in various amounts to provide skin appearance and/or sensory benefits. The amount of the composition of the present invention per application is typically from about 0.1 mg/m 2 to about 10 mg/m 2 in mg composition/cm 2 skin. A particularly effective application rate is about 2 mg/m 2 . Typical administration is on the order of about once per day, but the frequency of administration can vary from once per week up to three or more per day.

在将组合物施用于皮肤上之后,本发明的组合物可基本上立即提供可见的皮肤状况改善。这种立即改善包括对诸如质构不连续之类的皮肤瑕疵(包括那些与皮肤老化有关的皮肤瑕疵,如毛孔增大)的覆盖或掩饰,和/或提供更均匀的皮肤色调或颜色。The compositions of the present invention provide a visible improvement in skin condition substantially immediately after application of the composition to the skin. Such immediate improvement includes covering or masking of skin imperfections such as textural discontinuities, including those associated with skin aging such as enlarged pores, and/or providing a more even skin tone or color.

含有用于长期性调节皮肤状况的活性物的本发明组合物,在长期性局部施用组合物后,也可提供皮肤状况方面的可见改善。″长期性局部施用″等等包括在对象生存期间内的很长一段时间里连续地局部施用组合物,优选为至少约一周的时间,更优选为至少约一个月的时间,再优选为至少约三个月的时间,再优选为至少约六个月的时间,尤其优选为至少约一年的时间。皮肤状况的长期调节涉及在多次皮肤局部施用该组合物后皮肤状况的改进。典型的施用是按照在所说的长时间内每天约一次,然而,施用次数可以从每周约一次至最多每天约三次或更多之间变化。Compositions of the present invention containing actives for chronic regulation of skin condition may also provide visible improvement in skin condition after chronic topical application of the composition. "Chronic topical administration" and the like include continuous topical administration of the composition over a long period of time during the life of the subject, preferably for a period of at least about one week, more preferably for a period of at least about one month, and still more preferably for at least about A period of three months, more preferably a period of at least about six months, and especially preferably a period of at least about one year. Long-term regulation of skin condition involves improvement in skin condition after multiple skin topical applications of the composition. Typical administration is on the order of about once a day for the extended period in question, however, the number of administrations may vary from about once a week up to about three or more times a day.

实施例Example

下列实施例将进一步描述和示例在本发明范围之内的实施方案。给出它们的目的是为了举例说明,但不能理解为对本发明的限制。当可应用时,配料均按CTFA名称给出。所有的实施例均为通过施用常规配制技术制备的水包油型乳液。 实施例     1     2     3 成分 w/w%  w/w%  w/w% 烟酰胺 2.0  5.0  6.0 丙酸视黄酯 -  -  0.2 尼龙-121 2.0  3.0  0.5 二氧化钛(和)云母2-绿色 0.25  0.1  0.5 二氧化钛(和)云母3-白色 0.75  1.5  0.5 聚丙烯酰胺&异链烷烃&月桂基醚-7 2.25  2.0  1.0 黄原胶 -  -  0.3 二氧化钛4 -  -  0.3 甘油 7.0  5.0  3.0 尿素 -  -  2.0 泛酰醇 1.0  0.5  3.0 水杨酸 -  1.5  - 尿囊素 0.2  0.1  0.05 芦荟凝胶 0.01  -  0.05 醋酸生育酯 0.5  -  0.05 鲸蜡醇 2.0  1.0  1.25 硬脂醇 2.0  1.0  1.25 环甲基聚硅氧烷&二甲基聚硅氧烷醇 0.75  1.5  0.50 硬脂醚-21 0.6  0.4  0.3 硬脂醚-2 0.1  0.08  0.03 山梨糖醇酐硬脂酸酯&蔗糖椰油酸酯 1.5  -  - 硬脂醇 0.5  1.0  1.5 鲸蜡醇 0.5  1.0  1.5 二十二烷醇 0.5  1.0  1.5 异十六烷 3.0  5.0  7.0 矿脂 0.5  1.0  2.0 PPG-15硬脂醚 3.0  5.0  4.00 蔗糖多棉籽酸酯 -  3.0  - 二甲基聚硅氧烷(350mm2s-1) 0.5  -  1.0 EDTA二钠 0.02  0.01  0.05 对羟基苯甲酸乙酯 0.1  0.15  0.2 对羟基苯甲酸丙酯 0.1  0.15  0.2 对羟基苯甲酸甲酯 0.1  0.15  0.2 苯甲醇 0.5  0.2  1.0 苯氧基乙醇 0.5  -  1.0 香料 适量  适量  适量 去离子水 加至100%  加至100%  加至100% 1Orgasol_2002 EXD NAT COS。2绿色干扰颜料。3光学上中性的二氧化钛包覆云母。4聚硅氧烷包覆锐钛矿。The following examples further describe and demonstrate embodiments within the scope of the present invention. They are given for the purpose of illustration and should not be construed as limiting the invention. Ingredients are given by CTFA designation when applicable. All examples are oil-in-water emulsions prepared by applying conventional formulation techniques. Example 1 2 3 Element w/w% w/w% w/w% Nicotinamide 2.0 5.0 6.0 retinyl propionate - - 0.2 Nylon-12 1 2.0 3.0 0.5 Titanium Dioxide (and) Mica 2 - Green 0.25 0.1 0.5 Titanium Dioxide (and) Mica 3 - White 0.75 1.5 0.5 Polyacrylamide & Isoparaffin & Laureth-7 2.25 2.0 1.0 xanthan gum - - 0.3 Titanium dioxide 4 - - 0.3 glycerin 7.0 5.0 3.0 urea - - 2.0 Panthenol 1.0 0.5 3.0 salicylic acid - 1.5 - Allantoin 0.2 0.1 0.05 aloe vera gel 0.01 - 0.05 Tocopheryl acetate 0.5 - 0.05 cetyl alcohol 2.0 1.0 1.25 stearyl alcohol 2.0 1.0 1.25 Cyclomethicone & Dimethiconol 0.75 1.5 0.50 Stearyl ether-21 0.6 0.4 0.3 Stearyl ether-2 0.1 0.08 0.03 Sorbitan Stearate & Sucrose Cocoate 1.5 - - stearyl alcohol 0.5 1.0 1.5 cetyl alcohol 0.5 1.0 1.5 Docosanol 0.5 1.0 1.5 Isohexadecane 3.0 5.0 7.0 Petrolatum 0.5 1.0 2.0 PPG-15 stearyl ether 3.0 5.0 4.00 Sucrose Polycottonate - 3.0 - Dimethylpolysiloxane (350mm 2 s -1 ) 0.5 - 1.0 Disodium EDTA 0.02 0.01 0.05 Ethyl p-hydroxybenzoate 0.1 0.15 0.2 Propylparaben 0.1 0.15 0.2 Methylparaben 0.1 0.15 0.2 Benzyl alcohol 0.5 0.2 1.0 Phenoxyethanol 0.5 - 1.0 spices Appropriate amount Appropriate amount Appropriate amount Deionized water add up to 100% add up to 100% add up to 100% 1 Orgasol_2002 EXD NAT COS. 2 green interference pigments. 3 Optically neutral titanium dioxide coated mica. 4 polysiloxane coated anatase.

当以2mg/cm2皮肤的比例涂敷于目标对象的手上时,可提供皮肤外貌基本上立即可见的改善,例如减少了毛孔的可见性和更均匀的皮肤色调。以相同的比例每天一次或两次连续涂敷3-6个月,不仅基本上立即改善外貌,还可改善皮肤表面质构,包括减少细纹和皱纹。When applied to the hands of a subject at a rate of 2 mg/ cm2 of skin, provides substantially immediate improvement in skin appearance, such as reduced visibility of pores and more even skin tone. Continuous application at the same rate once or twice daily for 3-6 months not only improves substantially immediate appearance, but also improves skin surface texture, including the reduction of fine lines and wrinkles.

Claims (9)

1.局部用液体化妆品组合物,含有:1. A liquid cosmetic composition for topical use, comprising: a)0.3%到1.5%的光学上中性的页硅酸盐;和a) 0.3% to 1.5% optically neutral phyllosilicates; and b)当以2.4mg cm-2的覆盖量涂在皮肤或皮肤替代物上时,可提供给组合物-1到-5的Δa的色移值和-2到-5的Δb的色移值的有效量的绿颜料;b) When applied to skin or skin substitutes at a coverage of 2.4 mg cm -2 , it provides a color shift value of Δa for compositions -1 to -5 and a color shift value of Δb for -2 to -5 an effective amount of green pigment; 其中组合物中无机颗粒的总含量小于5%。Wherein the total content of inorganic particles in the composition is less than 5%. 2.权利要求1的组合物,其中光学上中性的页硅酸盐为云母。2. The composition of claim 1, wherein the optically neutral phyllosilicate is mica. 3.权利要求1的组合物,其中绿颜料为片状干扰颜料,TiO2层的厚度为120nm到160nm或其整数倍,含量为组合物重量的0.1%到0.5%。3. The composition of claim 1, wherein the green pigment is a flaky interference pigment, the TiO2 layer has a thickness of 120nm to 160nm or its integer multiples, and the content is 0.1% to 0.5% by weight of the composition. 4.局部用液体化妆品组合物,含有:4. A liquid cosmetic composition for topical use, comprising: a)0.3%到1.5%的光学上中性的页硅酸盐;和a) 0.3% to 1.5% optically neutral phyllosilicates; and b)绿色片状干扰颜料,TiO2层的厚度为120nm到160nm或其整数倍,含量为组合物重量的0.1%到0.5%;b) Green flaky interference pigments, the thickness of the TiO2 layer is 120nm to 160nm or an integer multiple thereof, and the content is 0.1% to 0.5% by weight of the composition; 其中组合物中无机颗粒的总含量小于5%。Wherein the total content of inorganic particles in the composition is less than 5%. 5.任何上述权利要求的组合物,其中含有接触角小于约40°的油相。5. The composition of any preceding claim, comprising an oily phase having a contact angle of less than about 40°. 6.任何上述权利要求的组合物,其为水包油乳液。6. A composition according to any preceding claim which is an oil-in-water emulsion. 7.任何上述权利要求的组合物,其中另外含有0.1%到10%的折射率为1.3到1.7的有机颗粒材料,颗粒材料散布在组合物中,其体积平均粒径在5到30μm的范围内。7. The composition of any preceding claim, wherein additionally containing 0.1% to 10% of organic particulate material having a refractive index of 1.3 to 1.7, the particulate material being dispersed in the composition and having a volume average particle diameter in the range of 5 to 30 μm . 8.提供更均匀的肤色的方法,包括局部地涂用任何上述权利要求的组合物。8. A method of providing a more even skin tone comprising topically applying a composition according to any preceding claim. 9.权利要求8的方法,其中将组合物涂在手上。9. The method of claim 8, wherein the composition is applied to the hands.
CN 01803849 2000-01-19 2001-01-18 Skin care compositions Pending CN1396817A (en)

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CN100352423C (en) * 2005-11-15 2007-12-05 湖南师范大学 Skin-care product contg. tortoise skin collagen composition, and its prepn. method
CN101152122B (en) * 2006-09-22 2011-05-11 株式会社资生堂 Oil in water type emulsion skin cosmetics

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FR2856594B1 (en) * 2003-06-26 2006-03-03 Oreal POROUS PARTICLES CHARGED WITH ACTIVE (S) COSMETIC OR PHARMACEUTICAL COMPOUND (S)
DE10357046A1 (en) 2003-12-04 2005-06-30 Beiersdorf Ag Cosmetic or dermatological preparations containing a combination of green dye and anti-inflammatory agent
DE102004012135A1 (en) * 2004-03-12 2005-09-29 Beiersdorf Ag Preparation against reddened skin
EP2101718A1 (en) * 2007-01-16 2009-09-23 The Procter and Gamble Company Cosmetic compositions
WO2012069291A1 (en) 2010-11-23 2012-05-31 Unilever Nv Composite particles and compositions with composite particles
AU2014402551B2 (en) * 2014-07-30 2017-06-29 Icb Pharma Spolka Jawna Liquid spreading composition with ectoparasiticidal activity, a method and use thereof for combating ectoparasites in human and veterinary medicine, as well as in agricultural, horticultural and/or garden environments
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CN100352423C (en) * 2005-11-15 2007-12-05 湖南师范大学 Skin-care product contg. tortoise skin collagen composition, and its prepn. method
CN101152122B (en) * 2006-09-22 2011-05-11 株式会社资生堂 Oil in water type emulsion skin cosmetics

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