TW200404573A - Cosmetic compositions containing salts of malonic acid - Google Patents

Cosmetic compositions containing salts of malonic acid Download PDF

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TW200404573A
TW200404573A TW092114572A TW92114572A TW200404573A TW 200404573 A TW200404573 A TW 200404573A TW 092114572 A TW092114572 A TW 092114572A TW 92114572 A TW92114572 A TW 92114572A TW 200404573 A TW200404573 A TW 200404573A
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Taiwan
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acid
weight
composition
patent application
scope
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TW092114572A
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Chinese (zh)
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Joseph Raymond Faryniarz
Philip Edward Miner
Michael Charles Cheney
Joanna Hong Zhang
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Unilever Nv
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    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37Esters of carboxylic acids
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41Amines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0208Tissues; Wipes; Patches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/046Aerosols; Foams
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362Polycarboxylic acids
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41Amines
    • A61K8/416Quaternary ammonium compounds
    • 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
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/12Face or body powders for grooming, adorning or absorbing
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/10Washing or bathing preparations

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Gerontology & Geriatric Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Dispersion Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A cosmetic composition is provided which includes as an active material a salt of malonic acid in a cosmetically acceptable carrier, wherein the composition exhibits a Flexibility Value greater than 1 according to the Porcine Skin Test.

Description

200404573 玖、發明說明: 【發明所屬之技術領域】 本發明係關於包含丙二酸鹽類之化粧組合物,及這些組 合物於控制皮膚老化徵兆之用途。 σ :軟、柔嫩且有柔韌性的皮膚具有一種顯著的化粧魅力 且是表皮正常發揮功能的屬十生。因為人類皮膚隨著年老而 老化,表皮能夠起皺,稜紋或凹凸不平而形成皺紋。這些 象徵失去年輕的外表且預報轉移到老年。暴露於過量對日 =將加速轉移過程。同時,表皮外層(即死皮層)能夠在暴 路於枣冷天氣或過度接觸清潔劑或溶劑後變成乾燥和脫皮 。因此造成皮膚喪失濕潤度且皮膚開始失去柔軟、柔嫩且 有柔韌性的特徵。 柔軟劑(如脂肪、磷脂和固醇類)過去頃經用以使起皺或 乾燥的皮膚柔軟。作為對於不良狀態之皮膚的療法,這些 柔軟劑僅部份局部有效。 使用智基魏酸提高人類膚質頃已知多時。不容置疑地, « -經基羧酸遠較普通的柔軟劑有效。 【先前技術】 美國專利第4,424,234號(Alderson等人)揭示多種在ρΗ值 小於7(經常是2至4)的組合物中摻入ο:-羥基己酸和α -羥基 辛酸或其混合物之皮膚治療組合物。¥11和Van Scott頃於此 領域中廣泛地請准專利。例如,美國專利第4,丨05,782號提 出治療痤瘡或頭皮屑之胺類或α -羥基羧酸銨的鹽類。在美 國專利第4,1 05,783號和美國專利第4,197,3 16號中,提出這 指 85632 200404573 二化合物m療乾燥皮膚。美國專利第4,m州號揭示使 用:-經基魏酸、其g旨類或胺鹽類治療角質。最近,美國專 利第5’091,171號集中注意於這些化合物有效抗老年斑、皺 紋和老化相關之皮膚改變。 然而經基m酸保有許多治療的保證,但是當重複局部應 用時頃發現該材料將刺激人體皮膚。刺激可以是從感覺刺 痛、發癢且灼埶到矽戍& 一 …、剜I床的發紅和脫皮。如此刺激的起因頃 經連結於人體皮膚界由 皮層中pH降低。吾人頃提出低ρΗ成為 角化細胞間鍵結阻礙的原因 J席因,其造成有害皮膚的反應,尤 其是一些具有敏感性皮膚的個人。 經“-羥基官能化之外的有機酸頃於化粧品文獻中揭示 例士美國專利第5,641,495號(J〇k則等人)共同揭示—種 神經醯胺或假神經醢胺、一種二缓酸及一種二幾酸之鹽類 。該實例例舉號轴酸之鈉鹽和鉀鹽。亦可以使用較低分子 里之'一^竣酸’如丙一西參。雜姑义/s a 内一馱。雖然發生優良的濕潤度並伴隨 微的刺激性,但並夫諸士美L么 工 建σ義此系統對抗造成失去皮膚柔敕性 、柔嫩性和柔章刃性之各/μ料心 老化妓兆。這些領域的改良依然 費者未滿足的需要。 ' 口此 _本發明的優點在於提供組合物中數種新穎的 化粧成份’該成份有效控制甚至去除老化徵兆,特別是關 於改良皮膚柔軟性,柔嫩性和柔韌性。 【發明内容】 本發明提供一種化粧組合物,其包括: (1)約0.0001至約3〇%重量比一種丙二酸的鹽類; 443 85632 200404573 (ii)約1至約99.9%重量比一種化粧品可接受之載體; 其中該組合物在豬隻皮膚測試中展現柔韌度值大於工。 此外,本發明提供一種控制老化徵兆的方法,其包括·· 提供一種化粧組合物,其包括·· (i)約0·0001至約30%重量比一種丙二酸之鹽類; (η)約1至約99.9%重量比一種化粧品可接受的載劑; 其中該組合物在豬隻皮膚測試中展現柔韌度值大於j ; 及將該化粧組合物應用於皮膚。 【實施方式】 吾人頃發現,丙二酸鹽類對於抗皮膚老化徵兆至少如α _ 羥基羧酸般有效。最特別而言,丙二酸鹽類頃顯示對於改 良皮膚柔軟性、柔嫩性和柔韌性重要的活性。 一個本發明的特點在於丙二酸鹽類是使該組合物在豬隻 皮膚測試中抗衡於水之正柔韌度值為至少丨者(較佳至少 。此測試使用一種熱力學分析計,於一直徑丨公分之豬隻皮 膚圓片上負载20克,將來自該分析計的即時偏斜以毫米為 單位記錄。水係、作為對照。在處理前及一次、二次和三次 處理後24小日守測$皮膚樣品。這些處理包括將工微升各組 a物應用於皮膚5分鐘,其後移除但不沖洗。其後,在2 ^它 且相對濕度低於1G%下進行乾燥。數據轉換包括測定應用 三次測試組合物後之偏斜值對水標準之偏斜值的比例。該 比例定義為柔韌度值。 可 '使用各種丙一酸鹽陽離子之抗衡陽離子形成該鹽類 丙一 S文鹽類可以是不完全或完全中和之丙二酸或其組合 85632 200404573 物,如通式(I)及(II)所代表·· +200404573 (1) Description of the invention: [Technical field to which the invention belongs] The present invention relates to a cosmetic composition containing malonates and the use of these compositions for controlling signs of skin aging. σ: Soft, tender and flexible skin has a significant cosmetic charm and is a normal life of the epidermis. Because human skin ages with age, the epidermis can be wrinkled, wrinkled, or uneven to form wrinkles. These symbols have lost their youthful appearance and forecasts have shifted to old age. Exposure to excess = will speed up the transfer process. At the same time, the outer layer of the epidermis (ie, the dead skin layer) can become dry and peeling after being exposed to cold weather or excessive contact with cleaning agents or solvents. As a result, the skin loses its wetness and the skin begins to lose its soft, tender, and flexible characteristics. Emollients such as fats, phospholipids, and sterols have been used to soften wrinkled or dry skin. As a treatment for unhealthy skin, these softeners are only partially effective. It has been known for a long time to improve human skin using citric acid. Undoubtedly, «-acrylic acid is far more effective than ordinary softeners. [Prior Art] U.S. Patent No. 4,424,234 (Alderson et al.) Discloses a variety of skins incorporating ο: -hydroxyhexanoic acid and α-hydroxyoctanoic acid or mixtures thereof in compositions having a pH value less than 7 (often 2 to 4) Therapeutic composition. ¥ 11 and Van Scott are widely patented in this field. For example, U.S. Patent No. 4,05,782 proposes amines or salts of ammonium α-hydroxycarboxylates for the treatment of acne or dandruff. In U.S. Pat. No. 4,105,783 and U.S. Pat. No. 4,197,3,16, it is proposed that this compound 85632 200404573 treats dry skin. U.S. Patent No. 4, m discloses the use of:-via weiwei acid, its g-type or amine salts to treat keratin. Recently, U.S. Patent No. 5'091,171 has focused on the effectiveness of these compounds against age spots, wrinkles and aging-related skin changes. However, cis-acids have many treatment guarantees, but when repeated topical application, it is found that the material will irritate human skin. The irritation can range from feeling tingling, itching and burning to silicon &…, redness and peeling of the bed. The cause of such irritation is that the pH in the cortex is reduced by being connected to the human skin. We have suggested that the low ρΗ is the cause of the hindrance between the keratinocytes and the bond J. The cause, which causes harmful skin reactions, especially individuals with sensitive skin. Organic acids other than "-hydroxy-functionalized" are disclosed in the cosmetic literature. U.S. Patent No. 5,641,495 (Jok et al.) Jointly reveals a type of ceramide or pseudoneramine, a second Acid and a salt of dikisheric acid. This example exemplifies the sodium and potassium salts of oleic acid. It is also possible to use the 'a ^ complete acid' in the lower molecule, such as ginseng, ginseng / sa I. Although the excellent degree of wetness is accompanied by a slight irritation, the husband and wife are beautiful. This system counteracts the loss of skin flexibility, suppleness, and flexibility. Heart aging prostitutes. Improvements in these areas are still unmet needs. 'Oral_ The advantage of the present invention is to provide several novel cosmetic ingredients in the composition' This ingredient effectively controls or even removes signs of aging, especially regarding improvement Skin softness, suppleness and flexibility. [Summary] The present invention provides a cosmetic composition comprising: (1) about 0.0001 to about 30% by weight of a salt of malonic acid; 443 85632 200404573 (ii ) About 1 to about 99.9% by weight An acceptable carrier; wherein the composition exhibits a flexibility value greater than that in a pig skin test. In addition, the present invention provides a method for controlling signs of aging, which includes providing a cosmetic composition including: (i ) About 0.0001 to about 30% by weight of a salt of malonic acid; (η) about 1 to about 99.9% by weight of a cosmetically acceptable carrier; wherein the composition exhibits flexibility in pig skin tests The degree value is greater than j; and the cosmetic composition is applied to the skin. [Embodiment] We have found that malonates are at least as effective as anti-aging signs of skin as alpha hydroxycarboxylic acid. Most particularly, malondi Acid salts are shown to be important in improving skin softness, suppleness, and flexibility. One feature of the present invention is that malonates are a positive flexibility value that allows the composition to counterbalance water in pig skin tests It is at least one (preferably at least one). This test uses a thermodynamic analyzer that loads 20 grams on a pig skin disc with a diameter of 1 cm and records the instant deviation from the analyzer in millimeters. As a control, skin samples were monitored before treatment and 24 hours after primary, secondary, and tertiary treatments. These treatments included applying microliters of each group a substance to the skin for 5 minutes, and then removing but not rinsing After that, drying was performed at 2 ^ and the relative humidity was lower than 1G%. Data conversion included determining the ratio of the skew value to the skew value of the water standard after applying the test composition three times. This ratio was defined as the flexibility value The salt can be formed using the counter cations of various malonate cations. The salts can be incompletely or completely neutralized malonic acid or a combination thereof 85632 200404573, such as the general formula (I) and ( II) Represented

[H02CCH2C02]'[XJ[H02CCH2C02] '[XJ

II

[Xj2[〇2CCH2C02J[Xj2 [〇2CCH2C02J

II 其中X是一種陽離子性抗衡離子。 適當的陽離子性抗銜離不4 k A p-f 丁I机銜離子包括屬鹼金屬和鹼土金屬者。 2表性實例包㈣、納m、銨之陽離子和其組 合物。 不僅是無機’亦能夠使用有機陽離子。特別有用的是具 1〜1,_個碳原子之四級化氮陽離子(較佳心,最佳 =個碳原子)。實例係衍生自胺之陽離子,其包括三乙醇 :、一乙醇胺、丙醇胺、單乙醇胺、甲胺、乙胺、丙胺、 H、丁胺、異丁胺、三級丁胺、戍胺、異戊胺、己胺 :二胺:環戊胺、降伯胺、辛胺'乙基己胺、壬胺、癸 二::啶酮、胺基酸類(離胺酸、筋胺酸、丙胺酸、麵醯 …組胺酸、嘗胺酸)、2_胺基-2-甲基小丙醇、二甲A =胺、聚乙亞胺、三(經曱基)胺基甲烧和其結合物。二 二1:氨、二甲基乙醇胺和三(經曱基)胺基甲燒之陽 、丙二自:些:佳《之典型丙二酸鹽類包括丙二酸銨 醇銨)、丙V 甲基乙醇録、丙二酸雙(二甲基乙 銨]。—酸芬(超甲基)甲錢和内二酸二[參⑽甲基)甲 “約(Μ至約15%,更佳約0.5至約1〇%,最佳 44S 85632 200404573 至約8 %重量比。 本^月此夠使用鹽I、鹽Η或這些鹽類之混合物作為活性 成刀s存在混合物時,單鹽I對二鹽π之莫耳比可以是約 1000.1至約1:1000(較佳約1〇:1至約丨:5〇〇,更佳約2:1至約 1:200,最佳約1:1至約1:20)。 本發明之組合物將亦包括一種化粧品可接受之載體。載 體的里可以疋1至99.9%(較佳約7〇至約95%,最佳約8〇至約 90%其中有用的載體是水、柔軟劑、脂肪酸、脂肪醇、 保濕d、稠化劑和其組合物。該載體可以是水性、無水性 或-種乳液。較佳該組合物是水性,尤指w/〇或〇/w或三重 聊㈣之水和油乳液。當存在水時,其量可以是約5至約 95%重量比(較佳約2()至約鳩,最佳約35至約6()%重量比)。 :酮:類、合成S旨類和烴類的形式。柔軟劑的量無論何處 。以疋約°,1至約95%重量比,較佳是約1至約50%重量比。 石夕酮油類可以區公么纟 之用詞”揮發性”表nr 發性。正如此處使用 M 、丁在¥ /服具有可測量之蒸汽壓的材料。 =生石夕嗣油類較佳選自含3至9個石夕原子(較佳4至5個石夕 原^之環族(環甲基相)或線性聚二甲基石夕氧烧。 =於:乍為柔軟劑材料之非揮發…油類包括聚烧基 =本Γ:基芳―聚崎燒共聚物。此處有 用的之本貝上非揮發性 約5 χ 1()、 …土夕认包括例如在25t:黏度 有用之奢h之聚二U矽氧烷。其中在本發明中 χ 1〇.5^^4 85632 -10- 200404573 x l〇·4 m2/s之聚二曱基矽氧烷。 另一類非揮發性矽酮係乳化和非乳化之矽酮彈性體。此 類的代表物是二曱矽酮/乙烯基二甲矽酮交聯聚合物,如II where X is a cationic counter ion. Appropriate cationic resistance is inseparable from 4 k A p-f butyl I organic ions including those belonging to alkali metals and alkaline earth metals. 2 Illustrative examples include tritium, nanom, ammonium cations and combinations thereof. Not only inorganic ', but also organic cations can be used. Particularly useful are quaternized nitrogen cations with 1 to 1, carbon atoms (preferably, optimal = carbon atoms). Examples are cations derived from amines, which include triethanol :, monoethanolamine, propanolamine, monoethanolamine, methylamine, ethylamine, propylamine, H, butylamine, isobutylamine, tertiary butylamine, amidine, isopropylamine Amylamine, hexylamine: diamine: cyclopentylamine, norbornelamine, octylamine 'ethylhexylamine, nonylamine, sebac :: pyridone, amino acids (lysine, glutamic acid, alanine, Noodles ... histamine, amine), 2-amino-2-methylpropanol, dimethyl A = amine, polyethyleneimine, tris (fluorenyl) aminomethyl, and combinations thereof . 222: Ammonia, dimethylethanolamine, and tris (fluorenyl) amino methylbenzene, propylene glycol: Some: Good "Typical malonates include ammonium malonate and ammonium malonate), propylene V Methyl ethanol, bis (dimethylethylammonium malonate) .— Acid fen (hypermethyl) methanine and bis (shenmethyl) formate, "about (M to about 15%, more preferably About 0.5 to about 10%, most preferably 44S 85632 200404573 to about 8% by weight. This month is enough to use salt I, salt tincture or a mixture of these salts as active knives. The molar ratio of the di-salt π may be about 1000.1 to about 1: 1000 (preferably about 10: 1 to about 丨: 500, more preferably about 2: 1 to about 1: 200, and most preferably about 1: 1 To about 1:20). The composition of the present invention will also include a cosmetically acceptable carrier. The carrier may contain 1 to 99.9% (preferably about 70 to about 95%, and most preferably about 80 to about 90). % Among the useful carriers are water, softeners, fatty acids, fatty alcohols, moisturizing agents, thickeners, and combinations thereof. The carrier can be aqueous, non-aqueous, or an emulsion. Preferably, the composition is aqueous, especially w / 〇 or 〇 / w or triple chat water and oil When water is present, the amount may be from about 5 to about 95% by weight (preferably about 2 () to about 5%, most preferably about 35 to about 6 ()% by weight).: Ketones: synthetic, synthetic Forms of S and hydrocarbons. The amount of softener is no matter where. In the range of about 1 °, 1 to about 95% by weight, preferably about 1 to about 50% by weight. The term "volatile" means nr hair. As used here, M, Ding has a measurable vapor pressure material. = Raw stone evening oil is preferably selected from 3 to 9 stone Xi atom (preferably 4 to 5 ring group (cyclomethyl phase) or linear polydimethylene sintering of Shixahara ^.): In: non-volatile at first glance softener materials ... oils include polysintering Base = ben Γ: Jifang-Posaki-fired copolymer. The Benben useful here is non-volatile about 5 x 1 (),... Tu Xishen includes, for example, the polyhedron U at 25t: which is useful for viscosity. Siloxane, of which in the present invention is χ 10.5. ^ 4 85632 -10- 200404573 x 10 · 4 m2 / s polydifluorenylsiloxane. Another type of non-volatile silicone emulsification and non-emulsification Silicone elastomer. The representative of this class is dioxin Ketone / vinyl dimethyl silicone cross-linked polymers such as

Dow Corning 9040、General Electric SFE 839和 Shin-Etsu KSG-18。如Silwax WS-L之矽酮蠟(二甲矽酮共多元醇月桂 酉旨)亦是有用的。 其中該酯柔軟劑係: (1)具有10至20個碳原子之脂肪酸的烯基或烷基酯。其實例 包括新戊酸異檳榔鹼酯、異壬酸異王酯、肉豆蔻酸油酯 、硬脂酸油酯和油酸油酯。 (2)醚-酯類,如乙氧化脂肪醇類之脂肪酸酯。 (3)多το醇酯類。乙二醇單_及二脂肪酸酯、二芸醇單_及二 月曰肪酸酯、聚乙二醇(200-6000)單-及二脂肪酸酯、丙二 醇單-及二脂肪酸酯、聚丙二醇2〇〇〇單油酸酯、聚丙二 醇2000單硬脂酸醋、乙氧化丙二醇單硬脂酸醋、苷油基 單-及二脂肪酸酯、聚苷油聚_脂肪酯、乙氧化單硬脂酸 苷油酯、1,3-丁二醇單硬脂酸酯、丨,3•丁二醇二硬脂酸 酯、聚環氧乙烷多元醇脂肪酸酯、花楸丹脂肪酸酯和聚 環氧乙烷花楸丹脂肪酸酿是令人滿意的多元醇酯。特別 有用的是匕-〜醇類之季戊四醇、三經甲基丙烧和新戍 二醇酯。 (4) 蠟酯類,如蜂蠟,鯨蠟和化比純⑶匕蠟。 (5) 固醇酯類,其中膽固醇护日*分 八T [ U咚舳肪酸酯類是其實例 碳酸酯和蔗糖聚棉花籽 (6) 脂肪酸之糖醋,如嚴糖聚二+ 497 85632 -11 - 200404573 酸自旨。 適用於化粧品可接受之載劑之烴類。包括石油、礦油、 Cn-C u異鏈烷烴、聚α烯烴類,且尤指異十六烧,市售為 來自 Presperse Inc之 Permethyl 101Α。 具有1 0至3 0個碳原子之脂肪酸亦可以適於作為化粧品可 接受的載劑。此類的實例是壬酸、月桂酸、肉豆蔻酸、掠 橺酸、硬脂酸、異硬脂酸、羥基硬脂酸、油酸、亞麻油酸 、蓖麻油酸、花生酸、二十二酸及芥子酸。 具有10至30個碳原子之脂肪醇是另一類有用的化粧品可 接受的載劑。此類的實例係硬脂醇、月桂醇、肉豆蔻醇和 綠虫鼠醇。 多元醇型態之保濕劑能夠用以作為化粧品可接受的載劑 典型的多元醇包括:y:油酯、聚烷二醇類和更佳的伸烷基 多几醇及其衍生物,包括丙二醇、二丙二醇、聚丙二醇、 聚乙二醇和其衍生物、山梨糖醇、羥丙基山梨糖醇、己二 醇、i,3-丁二醇、異戊二醇,丨,2,6_己三醇、乙氧化丙三醇 丙氧化丙二醇及其混合物。保濕劑的量無論何處可以是 〆、、且口物之〇·5至50%重量比,較佳是i至15%重量比。 、:匕$丨犯夠用以作為部份根據本發明之化粧品可接受的 载劑。典型的稠化劑包括交聯丙烯酸酯(例如Carbopol 982, 尺丨生改貝之丙烯酸酯(例如Car bop 〇1 1 3 82®)、纖維素衍 素遠勿矛天然樹膠。其中有用的纖維素衍生物係羧甲基纖維 、内羥丙基甲基纖維素、羥丙基纖維素、羥乙基纖維素 乙基纖維素和羥甲基纖維素。適用於本發明之天然樹膠 49« 85632 -12- 200404573 包括瓜耳膠、黃原素、菌核、角又菜膠、果膠和這些樹膠 之結合物。無機物亦可以用以作為稠化劑,特別是黏土類 (如膨潤土和水輝石)、煙燻矽石和矽酸鹽類(如矽酸鎮链 (Veegum®)。稠化劑的量可以是〇.0001至1〇%重量比,經常 是0 · 0 0 1至1 %重量比,最佳〇 · 〇 1至〇 5 %重量比。 本發明之化粧組合物可以是任何形式。這些形式可以包 括液狀、膏劑、滚珠調配物、棒狀物、泡沫、氣溶膠和非 氣溶膠噴霧及織物(例如不織物紡織品)之應用形成。 界面活性劑亦可以存在於本發明之化粧組合物中。當存 在時,界面活性劑的總濃度可以是該組合物之約〇·丨至約 利%重量比(較佳約1至約20%重量比,最佳約工至約”/。重量 比)。該界面活性劑可以選自由陰離子、非離子、陽離子和 和兩性離子活性物所組成之群組。特別較佳之非離子性界 面活性劑係具有每莫耳疏水物經縮合2至100莫耳環氧乙烷 或環氧丙烧之C1G-C2()脂肪醇或酸疏水物者;縮合2至莫耳 環氧烷之C2_ClQ烷基酚類;乙二醇之單_及二-脂肪酸醋;脂 肪酸單誓油醋;花楸丹、單-和二似20脂肪酸;和聚環j 乙烷花楸丹及其結合物。烧基聚葡糖誓和糖精脂肪_ 如甲基葡糖醯胺)亦是適當的非離子性界面活性劑。Dow Corning 9040, General Electric SFE 839, and Shin-Etsu KSG-18. Silicone waxes such as Silwax WS-L (Dimethicone Copolyol Laurel) are also useful. Wherein the ester softener is: (1) an alkenyl or alkyl ester of a fatty acid having 10 to 20 carbon atoms. Examples thereof include isococyl pivalate, isoprenyl isononanoate, oleyl myristate, oleyl stearate, and oleyl oleate. (2) Ether-esters, such as fatty acid esters of ethoxylated fatty alcohols. (3) Polyol esters. Glycol mono- and di-fatty acid esters, di-menthol mono- and di-fatty acid esters, polyethylene glycol (200-6000) mono- and di-fatty acid esters, propylene glycol mono- and di-fatty acid esters, Polypropylene glycol 2000 monooleate, polypropylene glycol 2000 monostearate, ethoxylated propylene glycol monostearate, glycoside mono- and di-fatty acid esters, polyglycol poly-fatty acid esters, ethoxylated Oleyl monostearate, 1,3-butanediol monostearate, 3, butanediol distearate, polyethylene oxide polyol fatty acid ester, lantana fatty acid Esters and polyethylene oxide lantana fatty acids are satisfactory polyol esters. Particularly useful are pentaerythritol, an alcohol, pentaerythritol, trimethyl ether, and neopentyl glycol esters. (4) Wax esters, such as beeswax, whale wax and pure dagger wax. (5) Sterol esters, of which cholesterol protects the daytime * T [U fatty acid esters are examples of carbonates and sucrose polycotton seed. (6) Sweet and sour fatty acids, such as strict sugar polydi + 497 85632 -11-200404573 The purpose of acid. Suitable for use in cosmetic acceptable carriers. Including petroleum, mineral oil, Cn-Cu isoparaffin, poly alpha olefins, and especially isohexadecane, commercially available as Permethyl 101A from Presperse Inc. Fatty acids having 10 to 30 carbon atoms may also be suitable as cosmetically acceptable carriers. Examples of this class are nonanoic acid, lauric acid, myristic acid, panic acid, stearic acid, isostearic acid, hydroxystearic acid, oleic acid, linoleic acid, ricinoleic acid, arachidic acid, twenty-two Acid and erucic acid. Fatty alcohols having 10 to 30 carbon atoms are another useful cosmetically acceptable carrier. Examples of this class are stearyl alcohol, lauryl alcohol, myristyl alcohol and chlorophyllol. Polyol-type humectants can be used as cosmetically acceptable carriers. Typical polyols include: y: oleyl esters, polyalkylene glycols, and better polyalkylene glycols and their derivatives, including propylene glycol. , Dipropylene glycol, polypropylene glycol, polyethylene glycol and its derivatives, sorbitol, hydroxypropyl sorbitol, hexanediol, i, 3-butanediol, isoamyl glycol, 丨, 2,6_hexane Triol, ethoxylated glycerol, propylene oxide, and propylene glycol, and mixtures thereof. The amount of the humectant may be 无论, wherever it is, and the weight ratio of the mouthpiece is from 0.5 to 50% by weight, preferably from i to 15% by weight. It is sufficient to be used as part of the cosmetically acceptable carrier according to the present invention. Typical thickeners include cross-linked acrylates (such as Carbopol 982, biodegradable acrylates (such as Car bop 〇1 1 3 82®)), cellulose derivatives far from natural gums. Among them, useful cellulose Derivatives are carboxymethyl fiber, internal hydroxypropyl methyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose ethyl cellulose, and hydroxymethyl cellulose. Natural gums suitable for the present invention 49 «85632- 12- 200404573 Including guar gum, xanthan, sclerotia, carrageenan, pectin and combinations of these gums. Inorganic substances can also be used as thickeners, especially clays (such as bentonite and hectorite), tobacco Fumed silica and silicates (such as Veegum®). The amount of thickener can be 0.0001 to 10% by weight, often 0. 0 0 1 to 1% by weight, the best 0. 〇1 to 5% by weight. The cosmetic composition of the present invention may be in any form. These forms may include liquids, creams, ball formulations, sticks, foams, aerosols and non-aerosol sprays and fabrics. (Eg non-woven textiles) formed by application. The agent may also be present in the cosmetic composition of the present invention. When present, the total concentration of the surfactant may be from about 0.1 to about 20% by weight of the composition (preferably from about 1 to about 20% by weight). , The best about work to about "/. Weight ratio). The surfactant can be selected from the group consisting of anionic, nonionic, cationic and zwitterionic actives. Particularly preferred nonionic surfactants have C1G-C2 () fatty alcohols or acid hydrophobes with 2 to 100 moles of ethylene oxide or propylene oxide per mole of hydrolysates; C2_ClQ alkylphenols of 2 to moles of alkylene oxides; ethylene glycol Alcohol mono- and di-fatty acid vinegar; fatty acid mono-ole vinegar; lantana, mono- and di-like 20 fatty acids; and polycyclo j ethane lantana and combinations thereof. Burnt-based polyglucose and saccharin Fats (such as methylglucamine) are also suitable nonionic surfactants.

/交:之陰離子界面活性劑包括息、烷基醚硫酸S旨和磺g 酯、院基硫酸酉旨和石黃酸醋、燒基苯石黃酸酉旨、絲和U :編酸醋、c8-c202刪酸醯基醋、C8售基醚❸ S曰、C8_C2〇肉桂酸酯和其結合物。 之組合物中。特別較佳 防曬活化物亦可以包括於本發明 499 85632 -13- 200404573 者:如乙基對甲氧桂皮酸己醋之材料(市售為p⑽。丨m… 、v〇benZene(市售為Pars〇1 ! 78,和二苯基心(亦 嗣)。可以使用無機防囉活性物,如微粉狀二氧化鈦、氧化 鋅、聚乙烯和各種不同的其他聚合 告 的旦、S ^ 1 , 田存在%,防曬劑 的里通Η以是(Μ至观重量比(較佳2至20%重量比,最佳 4至10%重量比)。 視需要能夠將防腐劑換入併入本發明之化粧組合物中以 保護免於可能有害的微生物生長。本發明之組合物的適當 的傳統防腐劑是對-經基苯甲酸之燒基醋類。最近頃經使用 的其他防腐劑包括尿囊素衍生物、丙酸鹽類和多種四級銨 化合物。化粧品化學家熟悉適當的防腐齊!,且通常選擇該 防腐劑以滿足防腐劑注毒測試並提供產品安定性。特別較 佳之防腐㈣苯氧乙醇、甲基對氧苯甲酸醋、丙基對氧苯 甲酸醋"米嗤咬基尿素、去氯乙酸納和苯甲醇。該防腐劑 應该視組合物之用途和防腐劑與乳液中其他成分之間可能 的不相容性而選擇。防腐劑較佳按該組合物之〇 〇1%至2% 重Ϊ比的量而使用。 本發明組合物可以包括維生素。實例維生素係維生素A (視黃醇)、維生素B2、維生素B6、維生素C、維生素E和生 物素。亦可以使用維生素之衍生物。例如,維生素c衍生物 包括四異棕櫚酸抗壞血酯、磷酸抗壞血酸酯鎂和抗壞血基 葡糖七·。維生素E之衍生物包括乙酸生育酯、棕櫚酸生育酯 和亞油酸生育醋。亦可以使用DL_泛醇和衍生物。當存在時 ’在根據本發明之組合物中維生素的總量可以是〇 〇〇1至 •14- 200404573 ㈣重量比(較佳〇.〇1%至1%,最佳〇1至〇5%重量比)。 另一類型有用的物質能夠是-種酵素,如氧化酶、蛋白 酶、脂肪酶和結合物。特職佳者係超氧化物二鉬酸酶, 由USA之Brooks公司以Bi〇cell s〇D之名銷售。 皮膚光亮化合物可以包括於本發明組合:中。實 係胎盤萃取物、乳酸、錢醢胺、熊果素、麴酸、阿魏酸 :間苯二❹包括4·取代間苯二盼之衍生物及其結合物Γ 這些用劑之量可以是該組合物之約〇 ι至約ι〇%重量 佳約0·5至約2%重量比)。 乂 可以存在脫屑促進劑。實例係、α m魏酸和^經基 酸°用詞”酸’,表示不僅包括自由酸,亦包括其鹽類和 烧基或芳基S旨類,及從移除水以形成環㈣線性㈣結構c 而產生之内醋。代表性酸類是乙醇酸、乳酸和蘋果酸。柳 酸是/5-羥基羧酸之代表。當存在時,這些材料的量可以是 該組合物之約0.01至約15%重量比。 :需要可以將多種草藥萃取物包括於本發明之組合物中 。實例係綠茶、黃春菊、:y:草精和其萃取物結合物。萃取 物可以是水溶性或帶動於溶劑中之水不溶性,其分別是親 水性或疏水性。水和乙醇是較佳之萃取物溶劑。 亦可以包括如類脂酸、視黃氧基三曱基矽烷(可取自 Cladant公司,以Silcare 1M_?5之商標)、脫氲表雄留酮 (DHEA)和其結合物之材料。亦可以使用神經醯胺類(包括/ Cross-linking: Anionic surfactants include alkyl ether, sulfuric acid alkyl esters and sulfonyl esters, sulphuric acid sulfate esters and lutein acid esters, pyrobenzyl lutein acid esters, silk and U: woven acid vinegar, c8-c202 deletes the acid ethyl vinegar, the C8 ethyl ether, the C8-C20 cinnamate and the combination thereof. Of the composition. Particularly preferred sunscreen activators may also be included in the present invention 499 85632 -13- 200404573: materials such as ethyl p-methoxycinnamate hexanoate (commercially available as p⑽. M, vobenZene (commercially available as Pars) 〇1! 78, and diphenylene (also 嗣). Inorganic antifungal actives can be used, such as micronized titanium dioxide, zinc oxide, polyethylene, and various other polymers. %, The content of the sunscreen is (M to weight ratio (preferably 2 to 20% by weight, most preferably 4 to 10% by weight). If necessary, the preservative can be replaced and incorporated into the makeup of the present invention. The composition is protected against the growth of potentially harmful microorganisms. A suitable traditional preservative for the composition of the present invention is p-based benzoic acid vinegar. Other preservatives that have recently been used include allantoin derivatives Compounds, propionates and various quaternary ammonium compounds. Cosmetic chemists are familiar with the appropriate preservatives! And usually choose this preservative to meet the preservative poisoning test and provide product stability. Particularly preferred preservative phenoxyethanol , Methyl paraoxoate, propyl paraoxane Benzoate vinegar " Mitarium urea, sodium dechloroacetate and benzyl alcohol. The preservative should be selected based on the use of the composition and possible incompatibilities between the preservative and other ingredients in the emulsion. Preservatives It is preferably used in an amount of 0.001% to 2% by weight of the composition. The composition of the present invention may include vitamins. Examples of vitamins are vitamin A (retinol), vitamin B2, vitamin B6, vitamin C, Vitamin E and biotin. Derivatives of vitamins can also be used. For example, vitamin c derivatives include ascorbyl tetraisopalmitate, magnesium ascorbyl phosphate, and ascorbyl glucose VII. Derivatives of vitamin E include Tocopheryl acetate, tocopheryl palmitate, and tocopheryl linoleate. DL-panthenol and derivatives can also be used. When present, the total amount of vitamins in the composition according to the invention can be from 0.001 to • 14 -200404573 ㈣ weight ratio (preferably 0.001% to 1%, most preferably 0.001 to 5% by weight). Another type of useful substance can be-enzymes such as oxidase, protease, lipase and Conjugates. Super-specialists are superoxide Dimolybase, sold by Brooks, USA, under the name of Bicells SOD. Skin brightening compounds can be included in the combination of the present invention: Medium. Real placenta extract, lactic acid, cyperamide, arbutin, gallic acid Ferulic acid: isophthalic acid includes 4. substituted isophenylene derivatives and combinations thereof. The amount of these agents may be about 0 to about 5% by weight of the composition, preferably about 0.5. To about 2% by weight). 乂 Desquamation promoters can be present. Examples, α m wei acid and ^ acid based ° The word "acid" means not only the free acid, but also its salts and alkyl groups or Aryl groups, and lactones produced by removing water to form a ring-shaped linear fluorene structure c. Representative acids are glycolic acid, lactic acid, and malic acid. Salicylic acid is representative of / 5-hydroxycarboxylic acid. When present, the amount of these materials may be from about 0.01 to about 15% by weight of the composition. : It is required that a variety of herbal extracts can be included in the composition of the present invention. Examples are green tea, chamomile,: y: grass extract and its extract combinations. The extract can be water-soluble or water-insoluble in a solvent, which is hydrophilic or hydrophobic, respectively. Water and ethanol are preferred extractive solvents. It may also include materials such as fatty acids, retinyltrisylsilane (available from Cladant under the trademark Silcare 1M-5), dehydroepiandrosterone (DHEA), and combinations thereof. Neuraminamines (including

Ceramide 1、Ceramide 3、Ceramide 3B和 Ceramide 6)及假 神經醯胺類,對於許多本發明之組合物而言,亦可以被排 ςβΙ 85632 -15- 2UU4U45/3 除。這些材料的量可 9 較佳約 〇.咖至約ι%重量比。^㈣咖至約1〇%, 著色劑、香料、不透明 之組合物中。各個這歧物::磨擦劑亦可以包括於本發明 較佳(M至3%重量比。 是約°·。5至約5%重量比, 用詞,,包括,,表示不限於任何後來提及之元件,但包含大 部份或少部份官能重要性之未指^件。換言《,該列干 步驟、疋件或選項不需要具排外性。每當用字"包括"或"具 有被使用時,這些用詞表示與以上定義之”包括"相等。 除了在操作和對照實例中或者以其它方式明確指出之處 外,吾人應該了解在此敘述中所有表示材料量之數字頃麵 Π約”之用字所修正。 下列實例將更完全說明本發明之具體實施例。所有此處 和所附申請專利範圍中引用之份數、百分比和比例係重量 比,除非以其它方式說明。 實例1 表I概述一種根據本發明之典型化粧用膏劑。Ceramide 1, Ceramide 3, Ceramide 3B, and Ceramide 6) and pseudoneuraminides can also be eliminated for many of the compositions of the present invention. ΒΙ 85632 -15-2UU4U45 / 3. The amount of these materials may be from about 0.1 to about 1% by weight. ^ Coffee to about 10%, colorant, perfume, opaque composition. Each of these: :: friction agents may also be included in the present invention (M to 3% by weight ratio. It is about ° .. 5 to about 5% by weight, the word, including, means that it is not limited to any subsequent mention And components, but containing most or less functional importance of unspecified pieces. In other words, the steps, files or options need not be exclusive. Whenever the word " include " or " When used, these terms denote equivalents to "included" as defined above. Except in the operating and comparative examples or where it is explicitly stated otherwise, I should understand that Amended by the word "numbers and planes". The following examples will more fully illustrate the specific embodiments of the present invention. All parts, percentages and ratios cited herein and in the scope of the appended patent applications are weight ratios, unless otherwise stated Mode description Example 1 Table I summarizes a typical cosmetic cream according to the present invention.

表I 成份 ---- 重量% ^---- 相· ----—--- A ^ --------~------—一 水 __—---- 差額 ___ 0.05 曱基對氧笨甲酸酯 ___- 0.15 ~ 矽酸鎂鋁 _____ 0.60 ~ 三乙醇胺 _____- 1.20 85632 -16- 200404573 相B 視黃膠 0.20 Natrosol® 250HHR(乙基纖維素) 0.50 丁二醇 3.00 甞油 2.00 相C 硬脂醯基乳酸鈉 0.10 單硬脂酸甞油酯 1.50 硬脂酸醇 1.50 棕櫚酸異硬脂酸酯 3.00 矽酮流體 1.00 膽固醇 0.25 花楸丹硬脂酸酯 1.00 丁基化羥基二曱苯 0.05 維生素E乙酸酯 0.01 PEG-100硬脂酸酯 2.00 硬脂酸 3.00 丙基對氧苯曱酸酯 0.10 Parsol MCX® 2.00 辛酸/辛酸三酸嘗油酉旨 0.50 羥基辛酸 0.01 c12-15烷基辛酸酯 3.00 相D 丙二酸鹽 3.00 相E 維生素A標搁酸酉旨 0.10 紅沒藥(Bisabolol) 0.01 維生素A乙酸酉旨 0.01 香料 0.03 Retinol 50C 0.02 85632 -17- 200404573 實例2 以下於表II中敘述一種使用本發明之丙二酸鹽之油包水 局部液體化粧粉底。Table I Ingredients ---- Weight% ^ ---- Phase · ------------ A ^ -------- ~ -------- monohydrate __----- -Difference ___ 0.05 Ammonium paraoxonate ___- 0.15 ~ Magnesium aluminum silicate _____ 0.60 ~ Triethanolamine _____- 1.20 85632 -16- 200404573 Phase B Retinoid 0.20 Natrosol® 250HHR (ethyl fiber Prime) 0.50 Butanediol 3.00 Emu Oil 2.00 Phase C Sodium Stearate Sodium Lactate 0.10 Ester Mono Stearate 1.50 Stearate Alcohol 1.50 Isostearate Palmitate 3.00 Silicone Fluid 1.00 Cholesterol 0.25 Ephraim Stearin Ester 1.00 Butylated hydroxydibenzobenzene 0.05 Vitamin E acetate 0.01 PEG-100 Stearate 2.00 Stearate 3.00 Propyl paraoxoate 0.10 Parsol MCX® 2.00 Caprylic acid / caprylic acid triacid Purpose 0.50 Hydroxyoctanoic acid 0.01 c12-15 Alkyl caprylate 3.00 Phase D Malonate 3.00 Phase E Vitamin A standard acid acid formula 0.10 Bisabolol 0.01 Vitamin A acetic acid formula 0.01 Fragrance 0.03 Retinol 50C 0.02 85632 -17- 200404573 Example 2 A water-in-oil topical liquid makeup foundation using the malonate of the present invention is described in Table II below. .

表II 成份 重量% 相A 環甲基矽酮 9.25 辛酸鯨蠟酯 2.00 二甲矽酮聚多元醇 20.00 相B 滑石 3.38 色素(鐵氧化物) 10.51 Spheron L-1500(石夕石) 0.50 相C 合成堪Durachem 0602 0.10 二十二酸花生酉旨 0.30 相D 環曱基矽酮 1.00 三羥硬脂酸苷油酯 0.30 相E 聚曱基丙烯酸酯(Laureth-7) 0.50 丙基對氧苯曱酸酯 0.25 相F 香料 0.05 相G 水 差額 丙二酸1安 3.00 曱基對氧苯曱酸酯 0.12 -18- 1,(44 85632 200404573 丙二醇 8.00 於驗酸胺 4.00 嘗油 3.00 氯化納 2.00 脫氫乙酸鈉 0.30 實例3 此處說明一種摻入本發明之丙二酸鹽之皮膚膏劑。 表III 成份 重量% 甞油 6.93 於驗酸胺 5.00 二甲基乙醇銨丙二酸鹽 5.00 Permethyl 101A1 3.00 Sepigel 3052 2.50 Q2-14033 2.00 異硬脂酸異丙酯 1.33 Arlatone 21214 1.00 鯨蠟醇CO-1695 0.72 SEFA棉籽酸鹽5 0.67 乙酸生育酯 0.50 泛醇 0.50 硬脂醇 0.48 二氧化鈦 0.40 EDTA 二鈉 0.10 Glydant Plus6 0.10 PEG-100硬脂酸鹽 0.10 硬脂酸 0.10 純水 差額 85632 -19- 200404573Table II Ingredients by weight% Phase A Cyclomethylsilicone 9.25 Cetyl octanoate 2.00 Dimethicone Polyol 20.00 Phase B Talc 3.38 Pigment (Iron Oxide) 10.51 Spheron L-1500 (Ishite) 0.50 Phase C Synthesis Can Durachem 0602 0.10 Picocosanoic acid 0.30 Phase D Cyclopentyl silicone 1.00 Tristearic acid oleyl ester 0.30 Phase E Polyacrylic acid acrylate (Laureth-7) 0.50 Propyl paraoxobenzoate 0.25 phase F fragrance 0.05 phase G water balance malonate 1 ampere 3.00 fluorenyl paraoxobenzoate 0.12 -18-1, (44 85632 200404573 propylene glycol 8.00 test acid amine 4.00 taste oil 3.00 sodium chloride 2.00 dehydroacetic acid Sodium 0.30 Example 3 A skin cream incorporating the malonate salt of the present invention is shown here. Table III Ingredients% by weight Emu Oil 6.93 In acetic acid 5.00 Dimethylethanolammonium malonate 5.00 Permethyl 101A1 3.00 Sepigel 3052 2.50 Q2-14033 2.00 Isopropyl stearate 1.33 Arlatone 21214 1.00 Cetyl alcohol CO-1695 0.72 SEFA cotton seed 5 0.67 Tocopheryl acetate 0.50 Panthenol 0.50 Stearyl alcohol 0.48 Titanium dioxide 0.40 EDTA disodium 0. 10 Glydant Plus6 0.10 PEG-100 stearic acid 0.10 stearic acid 0.10 purified water balance 85632 -19- 200404573

異十六烧,Presperse Inc·,South PlainHeld,NJIso-hexapod, Presperse Inc., South PlainHeld, NJ

2 聚丙烯醯胺(及)(:13-14異鏈烷烴(及)聚甲基丙烯酸酯, Seppic Corporation,Fairfield,NJ2 Polyacrylamide (and) (: 13-14 isoparaffin (and) polymethacrylate, Seppic Corporation, Fairfield, NJ

3 二甲石夕酉同(及)石夕靈醇(dimethiconol),Dow Corning Corp. Midland,MI3 Dimethicol with (and) dimethiconol, Dow Corning Corp. Midland, MI

4 早硬脂酸花揪丹酯和 Sucrococoate,ICI Americas Inc., Wilmington,DE 5 脂肪酸之蔗糖酯4 Sulfuryl early stearate and Sucrococoate, ICI Americas Inc., Wilmington, DE 5 Sucrose esters of fatty acids

6 DMDM尿囊素(及)丁基胺基甲酸碘丙炔酯,Lonza Inc., Fairlawn, NJ 實例4 表IV係一種根據本發明之粉末化粧組合物實例·。6 DMDM Allantoin (and) Iodopropynyl Butyl Carbamate, Lonza Inc., Fairlawn, NJ Example 4 Table IV is an example of a powder cosmetic composition according to the present invention.

表IV 成份 重量% 聚矽酮-11 27.5 環甲基矽酮 54 石油 11 三(羥甲基)甲烷丙二酸銨 7 二甲矽酮共多元醇 0.5 實例5 表V提出一種根據本發明之較無水性組合物實例。 85632 -20 - 200404573 表v 成份 重量% 環甲基矽酮 80.65 二甲石夕酮 9.60 角鯊烷 6.00 異硬脂酸 1.90 琉璃苣Borage籽油 0.90 丙二酸鋰(50%水溶液) 0.50 棕櫚酸視黃酯 0.25 神經醯胺6 0.10 生育酚 0.10 實例6 表VI概述一種適於本發明之氣溶膠包裝發泡清潔劑。Table IV Ingredient Weight% Polysilicone-11 27.5 Cyclomethylsilicone 54 Petroleum 11 Tris (hydroxymethyl) methanemalonate 7 Dimethicone copolyol 0.5 Example 5 Table V presents a comparison according to the present invention. Examples of anhydrous compositions. 85632 -20-200404573 Table v Ingredients by weight% Cyclomethylsilicone 80.65 Dimethyone 9.60 Squalane 6.00 Isostearic acid 1.90 Borage Borage seed oil 0.90 Lithium malonate (50% aqueous solution) 0.50 Palmitic acid Flavonol 0.25 Neuraminamine 6 0.10 Tocopherol 0.10 Example 6 Table VI summarizes an aerosol packaging foaming cleaner suitable for the present invention.

表VI 成份 重量% 葵花籽油 20.00 順丁烯二酸化黃豆油 5.00 矽酮胺基曱酸酯 1.00 Polyglycero-4油酸酯 1.00 C 1 4 -1 6稀烴續酸納 15.00 月桂醚硫酸鈉(25%活性) 15.00 可可醯胺基丙基甜菜鹼 15.00 DC 1784® (5 0%矽酮乳液) 5.00 Polyquaternium-11 1.00 雙(二曱基乙醇銨)丙二酸鹽 1.00 水 差額 -21 - ς07 85632 200404573 使用9 2 /〇重i比表VI之?辰縮液和8 %推進劑製造一種氣溶 膠,該推進劑係一種二甲醚、異丁烷和丙烷之結合物。 實例7 亦可以根據本發明調配一種黏性化粧用貼布(patch)。藉 混合30克2-丙烯醯胺基-2-甲基丙烷磺酸單體/2〇克蒸餾水 和5克亞甲基-雙-丙烯醯胺之1 %水溶液而製備一種黏性水 减駐。其後以〇·4%過磷酸鎂觸媒活化該溶液。將觸媒與該 水减膠溶液短暫混合後,添加〇 ·丨克丙二酸銨/5毫升水。將 所產生之溶液塗佈於聚丙烯和親水性聚酯之5〇/5〇摻合物 上並任由固化。所產生之沉積水凝膠於熱空氣爐中於40°C 加溫24小時。水凝膠之最終水含量為5〇%。在該黏性水凝 膠上放置一聚苯乙烯背襯。 實例8 根據本發明敘述一種拋棄式單次使用之個人擦拭巾產品 。以重量1.8克且尺寸為15公分X 20公分製備一種70/30聚酯 /螺縈不織擦拭巾。於此擦拭巾上浸潰一種如下表VII概述 之組合物。 道 _ -22- 200404573 表νιι 成份 辛基兩性二乙酸 PEG-40氫化蓖麻油 微生素E乙酸酯Table VI Ingredients% by weight Sunflower oil 20.00 Maleic acid soybean oil 5.00 Silicone aminoester 1.00 Polyglycero-4 oleate 1.00 C 1 4 -1 6 Sodium dibasic acid sodium 15.00 Sodium lauryl ether sulfate (25% Active) 15.00 Cocoaamine Aminopropyl Betaine 15.00 DC 1784® (50% Silicone Emulsion) 5.00 Polyquaternium-11 1.00 Bis (diamidoethanolammonium) malonate 1.00 Water difference-21-ς07 85632 200404573 used 9 2 / 〇 weight i ratio of Table VI? Chen shrinkage and 8% propellant make aerosol. The propellant is a combination of dimethyl ether, isobutane and propane. Example 7 An adhesive cosmetic patch can also be prepared according to the present invention. A viscous water was prepared by mixing 30 g of 2-acrylamido-2-methylpropanesulfonic acid monomer / 20 g of distilled water and 5 g of a 1% aqueous solution of methylene-bis-acrylamidoamine. The solution was then activated with a 0.4% magnesium superphosphate catalyst. After the catalyst was briefly mixed with the water reducing solution, 0.1 g of ammonium malonate / 5 ml of water was added. The resulting solution was applied to a 50/50 blend of polypropylene and a hydrophilic polyester and allowed to cure. The resulting deposited hydrogel was heated in a hot air oven at 40 ° C for 24 hours. The final water content of the hydrogel is 50%. A polystyrene backing was placed on the adhesive hydrogel. Example 8 A disposable single use personal wipe product according to the present invention is described. A 70/30 polyester / spiral non-woven wipe was prepared at a weight of 1.8 grams and a size of 15 cm x 20 cm. To this wipe was impregnated a composition as outlined in Table VII below.道 _ -22- 200404573 Table νιιη ingredients octyl amphoteric diacetic acid PEG-40 hydrogenated castor oil microbiotin E acetate

丙二酸鎂 苷油 己二醇 葡糖酸内酯 矽酮微乳液 金縷梅 香料 水 實例9 評比多種羧酸鹽類以測 卢 地士 1疋其在豬隻皮膚測試中之反岸 在-塊直徑1公分之豬y之反應 TMS- i型Perkin_Elme^力學八 克負载以才呆 錄皮膚之偏斜。様口 刀心立即以米為單位 為對昭。夂挣二 理六片皮膚。使用水 為二子:各塊係作為一種内部對照。將其在處理前和一 次處理之後24小時乾燥測量。各個處理包括] 測或材料溶液應用於皮膚5分鐘,其後移除但不 中。。乾無條件為2rc和低於1〇%濕度。結果記錄於表… S89 85632 -23- 200404573Magnesium glycoside oil hexanediol gluconolactone silicone microemulsion witch hazel flavor water Example 9 Compare a variety of carboxylates to measure Ludiz 1 疋 it is the opposite in the pig skin test- Response of a piece of pig y with a diameter of 1 cm TMS-i Perkin_Elme ^ Mechanical load of eight grams to record the deflection of the skin. The mouth of the sword was immediately measured in meters. I earn two skins. Water was used as the second child: each block was used as an internal control. It was measured for drying before and 24 hours after the first treatment. Each treatment includes applying the test or material solution to the skin for 5 minutes, and then removing but not missing. . Dry conditions are 2rc and humidity below 10%. Results are recorded in the table ... S89 85632 -23- 200404573

表 VIII -----^ 評比材料 柔韌度值^' 水(參考標準) 1.00 ^^- 琥珀酸鹽* 0.85 ' ~^ 乙醇酸鹽* 0.85 ^^^ 丙二酸鹽* * -〜---^__ 1.36 銨鹽 二甲基乙醇錢鹽 從結果中顯然丙二酸鹽賦予皮膚重要地更具柔韌性。相 反地,琥珀酸鹽和乙醇酸鹽賦予皮膚重要地較硬。乙醇酸 鹽和琥轴酸鹽的影響在統計上相似。這些結果指出丙一㈣ 鹽和包含這些鹽類之組合物能夠改良柔軟度、柔嫩度和柔 韌性。 表IX記錄對於表I詳述之化粧用膏劑調配物測量之柔韋刃 度值(使用不同的相D活化物)。該丙二酸鹽調配之膏劑的柔 韌度值高於基底膏劑或乙醇酸鹽調配之膏劑。結果說明使 用丙二酸鹽達到一種較柔軟、較柔嫩且更具柔韌性之皮膚。Table VIII ----- ^ Flexibility value of the comparison material ^ 'Water (reference standard) 1.00 ^^-Succinate * 0.85' ~ ^ Glycolate * 0.85 ^^^ Malonate * *-~- -^ __ 1.36 Ammonium salt dimethyl ethanol salt From the results it is clear that malonate gives the skin an important flexibility. Conversely, succinate and glycolate make the skin significantly harder. The effects of glycolate and succinate are statistically similar. These results indicate that allyl salts and compositions containing these salts can improve softness, tenderness and flexibility. Table IX records the Roveblade values (using different Phase D activators) measured for the cosmetic cream formulations detailed in Table I. The malonate-based cream has a higher flexibility value than the base cream or glycolate-based cream. The results show that the use of malonate achieves a softer, softer and more flexible skin.

表IX 評比材料* 柔韌度值 水(參考標準) 1.00 基底膏劑(無鹽類) 0.89 基底膏劑(乙醇酸鹽) 0.84 基底膏劑(丙二酸鹽) 1.12 括號内之鹽類表示實例1之相D活性物(表I) -24- 51Θ 85632 200404573 以上敘述和實例說明所選擇之本發明之具體實施例。依 照該具體實施例,將建議熟諳此藝者變化和調整,其全部 在本發明之精神和範圍内。 85632 25-Table IX Evaluation materials * Flexibility value water (reference standard) 1.00 Base paste (no salt) 0.89 Base paste (glycolate) 0.84 Base paste (malonate) 1.12 The salts in brackets indicate phase D of Example 1. Actives (Table I) -24- 51Θ 85632 200404573 The above description and examples illustrate specific embodiments of the invention selected. According to this specific embodiment, changes and adjustments of the artist will be suggested, all of which are within the spirit and scope of the present invention. 85632 25-

Claims (1)

200404573 拾、申請專利範圍: 1 種化被組合物,其包括: (〇約0.0001至約3〇〇/❶重量比丙二酸之鹽類; (11)約1至約99.9%重量比化粧品可接受之載體; 其中該組合物在豬隻皮膚測試中展現大於1之柔韌度 值。 2 ·根據申請專利範圍第1項之組合物,其中該丙二酸係分 別以約1000:1至約1:1000之莫耳比存在之半中和和完 全中和之酸。 3 ·根據申請專利範圍第2項之組合物,其中該莫耳比為約 2:1 至約 1:2〇〇。 4 ·根據申請專利範圍第1項之組合物,其中該鹽具有丙二 酸鹽之陽離子性抗衡原子,其係選自由鋰、鈉、鉀、鎮 、詞、銨和其結合物所組成群組之無機陽離子。 5·根據申請專利範圍第丨項之組合物,其中該丙二酸鹽之 陽離子性抗衡離子係具有2至1,000個碳原子之有機陽 離子,其選自由環乙亞胺、三乙醇胺、二乙醇胺、丙醇 胺、單乙醇胺、曱胺、乙胺、丙胺、異丙胺、丁胺、異 丁胺、三級丁胺、戊胺、異戊胺、己胺、環己胺、環戊 胺、降伯胺、辛胺、乙基己胺、壬胺、癸胺、吡咯啶酮 、胺基酸類(離胺酸、筋胺酸、丙胺酸、麩醯胺酸、組 胺酸、苷胺酸)、2-胺基-2-曱基-1-丙醇、-田f 一 τ丞乙醇胺 、三(羥曱基)胺和其組合物所組成之群組。 6 · 一種控制老化徵兆之方法,其包括: 5Π 85632 200404573 提供包括下列之化粧組合物: (i) 約0.0001至約30%重量比丙二酸之鹽類; (ii) 約1至約99.9%重量比化粧品可接受之載體; 其中該組合物在豬隻皮膚測試中展現大於1之柔 韌度值;及 將該化粧組合物施用於皮膚。 7.根據申請專利範圍第6項之方法,其中受控之老化徵兆 係柔軟度、柔嫩度和柔韌性。 85632 2- 200404573 柒、指定代表圖: (一) 本案指定代表圖為:第( )圖。 (二) 本代表圖之元件代表符號簡單說明: 捌、本案若有化學式時,請揭示最能顯示發明特徵的化學式: [H02CCH2C02]'[X]+ +[X]2[02CCH2C02]-2 I II 85632200404573 Patent application scope: 1 chemical composition, including: (0 about 0.0001 to about 300/3 weight ratio of malonic acid salts; (11) about 1 to about 99.9% by weight cosmetics can be Accepted carrier; wherein the composition exhibits a flexibility value greater than 1 in a pig skin test. 2 · The composition according to item 1 of the patent application scope, wherein the malonic acid is about 1000: 1 to about 1 respectively : Half-neutralized and fully-neutralized acid present in a molar ratio of 1000. 3 · A composition according to item 2 of the scope of patent application, wherein the molar ratio is from about 2: 1 to about 1: 20.00. 4 The composition according to item 1 of the scope of patent application, wherein the salt has a cationic counter atom of malonate, which is selected from the group consisting of lithium, sodium, potassium, town, word, ammonium, and combinations thereof. Inorganic cations. 5. The composition according to item 丨 of the scope of the patent application, wherein the cationic counterion of the malonate is an organic cation having 2 to 1,000 carbon atoms, which is selected from the group consisting of Ethanolamine, diethanolamine, propanolamine, monoethanolamine, amidine , Ethylamine, propylamine, isopropylamine, butylamine, isobutylamine, tertiary butylamine, pentylamine, isopentylamine, hexylamine, cyclohexylamine, cyclopentylamine, norbornelamine, octylamine, ethylhexylamine , Nonylamine, decylamine, pyrrolidone, amino acids (lysine, glutamic acid, alanine, glutamine, histidine, aglycol), 2-amino-2-fluorenyl- A group consisting of 1-propanol, -field f-t-ethanolamine, tris (hydroxymethyl) amine, and combinations thereof. 6 · A method for controlling signs of aging, including: 5Π 85632 200404573 Provides makeup including the following Compositions: (i) from about 0.0001 to about 30% by weight of malonic acid salts; (ii) from about 1 to about 99.9% by weight of cosmetically acceptable carriers; wherein the composition exhibits greater than A value of flexibility of 1; and applying the cosmetic composition to the skin. 7. The method according to item 6 of the scope of patent application, wherein the controlled signs of aging are softness, tenderness and flexibility. 85632 2- 200404573 柒, Designated Representative Map: (1) The designated representative map in this case is: () Figure (2) The yuan of the representative map Symbol representing briefly described: Ba, when the case if the formula, please show most features disclosed in the invention of the formula: [H02CCH2C02] '[X] + + [X] 2 [02CCH2C02] -2 I II 85632
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