CN100387219C - 抗皮肤老化的药物和化妆品组合物 - Google Patents

抗皮肤老化的药物和化妆品组合物 Download PDF

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CN100387219C
CN100387219C CNB028098919A CN02809891A CN100387219C CN 100387219 C CN100387219 C CN 100387219C CN B028098919 A CNB028098919 A CN B028098919A CN 02809891 A CN02809891 A CN 02809891A CN 100387219 C CN100387219 C CN 100387219C
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phosphatide complexes
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F·迪皮耶罗
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations
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    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55—Phosphorus compounds
    • A61K8/553—Phospholipids, e.g. lecithin
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    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof

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Abstract

用于防止皮肤老化的药物和化妆品组合物，其含有葡萄提取物的磷脂复合物以及标准积雪草提取物的磷脂复合物。

Description

抗皮肤老化的药物和化妆品组合物
本发明涉及含有植物来源成分的对抗皮肤老化的药物和化妆品组合物。
更具体地讲，本发明涉及用于预防皮肤老化的药物和化妆品组合物，其含有葡萄(Vitis vinifera)提取物的磷脂复合物以及自积雪草(Centellaasiatica)提取的三萜类化合物的磷脂复合物。
皮肤老化是一个可影响各个皮肤层的复杂的生物过程，但是它的主要影响见于真皮层。存在两种生物学上独立的、同时发生的老化过程。第一种是内源性老化，可影响皮肤以及很可能影响内脏器官。第二种是外源性老化或光老化，是暴露于环境、主要是紫外线照射的结果。内源性老化的后果可见于全身皮肤，包括不受阳光照射的部位。在暴露于阳光的部位、特别是在面部和手背，光老化损害和内源性老化所致的组织退化共同发挥作用。因此，患者所关心的主要部位，即面部和颈部皮肤的最明显的变化是内源性和外源性老化过程共同作用的结果。尽管其它因素(例如吸烟)可能导致皱纹过早产生，但达80％的面部老化已显示可归因于暴露于阳光。
从生物化学的观点而言，光老化被认为主要是由角质形成细胞和成纤维细胞与紫外照射相互作用而过量产生和过量释放的一些蛋白酶，主要是金属蛋白酶(这些蛋白酶是不可逆地损伤胶原蛋白、弹性蛋白和透明质酸的降解酶，致使在真皮留下疤痕及可见的皱纹)，以及能够在很短的时间内消除正常皮肤抗氧化防御体系的氧化压力。
基于这些常见原因，显然需要通过一种能够抵消蛋白酶对真皮的作用(并可增加成纤维细胞产生和释放新的胶原蛋白纤维的能力)并阻止皮肤抗氧化防御体系的消失的手段，以避免皮肤的过早老化。
本发明通过提供含有以下植物来源的成分的药物和化妆品组合物而满足了这种需求：
a)标准葡萄提取物的磷脂复合物            0.1至2.5％
b)标准积雪草提取物的磷脂复合物          0.1至2.5％
更优选地，本发明的药物和化妆品组合物含有以下植物来源的成分，并具有以下百分比：
a)标准葡萄提取物的磷脂复合物            1％
b)标准积雪草提取物的磷脂复合物          1％
EP275,224公开了标准葡萄提取物的磷脂复合物(也被称为“组分a”)。所述提取物由包含在葡萄籽中的多酚类部分组成，并包含没食子酸、游离的和与没食子酸酯化的儿茶素及表儿茶素的单体、二聚物、三聚物、四聚物、五聚物、六聚物和七聚物。
体外及体内研究已证实：所述提取物具有高度的抗氧化活性(基于实验模型的不同为维生素E的抗氧化活性的10至200倍)，其包括清除最具反应活性的基团类别，并对抗所有与自由基的作用有关的现象。所述提取物的特征还在于能够抑制黄嘌呤氧化酶并与Cu++及Fe+++螯合，从而阻止组织中酶催化的自由基的释放。最后，葡萄提取物可抑制胶原酶和其它蛋白酶，从而使结缔组织和皮肤免受紫外线照射后和炎性皮肤反应的进展期间所释放的蛋白水解酶的损害作用，并且它对皮肤和循环组织如微血管和毛细血管具有选择性的亲和力，从而也可对微循环区起到保护作用。
EP 283,713公开了标准积雪草提取物的磷脂复合物(也被称为“组分b”)。
该提取物由对胶原蛋白代谢具有强大作用的三种不同分子的4∶3∶3混合物组成，所述分子为积雪草甙、积雪草酸和羟基积雪草酸(madecassicacid)。这些分子可提高成纤维细胞摄取氨基酸如L-脯氨酸和L-羟脯氨酸(从定性-定量观点而言是胶原蛋白组成中最重要的氨基酸)的能力。胶原蛋白的合成增加意味着退化的旧胶原蛋白纤维可更快地被新的胶原蛋白纤维所代替。
WO 0178674公开了可用于治疗和预防皮肤老化和皱纹的组合物，所述组合物包含(1)葡萄提取物形式的白矢车菊素，(2)积雪草提取物形式的三萜类化合物和(3)鱼软骨提取物，在优选的实施方案中，为提高生物利用度，组分(1)和(2)也可以与磷脂复合。
当进行毒理学试验时，组分a)和b)表现出对被治疗组织既无毒性亦无刺激作用。
除以上所指出的组分a)和b)外，本发明的组合物还可以任选地包含其它活性成分如维生素E(0.2至1％)、锌(0.1至0.3％)、羟基酸(0.1至1％)及甘草亭酸或其与磷脂的复合物(0.1至2.5％)，以提高组合物的抗氧化、抗老化和抗炎性质。
本发明的组合物可以以适宜的液体制剂(如凝胶、洗液、乳液(milks)、乳剂、泡沫剂等)或固体或半固体制剂(如乳膏、软膏、唇膏等)的形式局部施用。根据常规的方法如那些在“Remington’s Pharmaceutical Handbook”(Mack出版公司，纽约，美国)中述及的方法，连同适宜的赋形剂如润滑剂、保湿剂、增稠剂、乳化剂、染料、矫味剂等，可制备所述制剂。
以下报告了发明的组合物的某些实施例。
实施例1-水包油乳剂
100克乳剂含有：
葡萄提取物的磷脂复合物                    0.20克
自积雪草提取的三萜类化合物的磷脂复合物    1.00克
异硬脂酸异硬脂醇酯(Gattefosse)            2.50克
聚异戊二烯(Syntesqual-Vevy)               2.50克
油酸癸酯(Cetiol V-Henkel)                 2.00克
鲸蜡醇十六酸酯(Cutina CP-Henkel)          2.00克
十六硬脂醇异壬酸酯
(cetearyl isononanoate，Cetiol SN-Henkel) 2.00克
聚山梨酸酯80(吐温80-ICI)                  1.00克
咪唑烷基脲                                0.30克
生育酚                                    0.20克
棕榈酸抗坏血酸酯                          0.10克
甲基氯异噻唑啉酮(e)甲基异噻唑啉酮
(Kathon CG-Rohm&Haas)                  0.05克
EDTA二钠                               0.10克
丁化羟基甲苯                           0.05克
聚丙烯酰胺(e)C13-14异链烷烃(e)
Laureth-7(Spiegel 305-Seppic)          2.50克
香料                                   0.10克
纯水                                   加至100.0克
实施例2-水包油乳剂
100克乳剂含有：
葡萄提取物的磷脂复合物                 0.50克
自积雪草提取的三萜类化合物的磷脂复合物 0.50克
甘草亭酸的磷脂复合物                   1.50克
C12-15烷基苯甲酸酯(Finsolv TN-Finetex) 4.00克
鲸蜡醇十六酸酯(Cutina CP-Henkel)       3.00克
聚异戊二烯(Syntesqual-Vevy)            2.50克
异硬脂酸异硬脂醇酯(Gattefosse)         2.50克
聚山梨酸酯80(吐温80-ICI)               1.00克
咪唑烷基脲                             0.30克
甲基氯异噻唑啉酮(e)甲基异噻唑啉酮
(Kathon CG-Rohm&Haas)                  0.05克
生育酚                                 0.20克
棕榈酸抗坏血酸酯                       0.10克
EDTA二钠                               0.10克
柠檬酸                                 0.05克
聚丙烯酰胺(e)C13-14异链烷烃(e)
Laureth-7(Spiegel 305-Seppic)          2.00克
丁化羟基甲苯                           0.05克
香料                   0.10克
纯水                   加至100.0克

Claims (6)

1.含有以下植物来源的成分：
a)标准葡萄提取物的磷脂复合物      0.1至2.5％
b)标准积雪草提取物的磷脂复合物    0.1至2.5％
以及常规赋形剂和载体的药物和化妆品组合物。
2.权利要求1所述的药物和化妆品组合物，其含有以下植物来源的成分：
a)标准葡萄提取物的磷脂复合物      1％
b)标准积雪草提取物的磷脂复合物    1％
以及常规赋形剂和载体。
3.权利要求1和2所述的药物和化妆品组合物，其还含有其它选自维生素E、锌、羟基酸和甘草亭酸或其与磷脂的复合物的活性成分。
4.权利要求3所述的药物和化妆品组合物，其中其它活性成分的百分含量为：
维生素E                       0.2至1％
锌                            0.1至0.3％
羟基酸                        0.1至1％
甘草亭酸或其与磷脂的复合物    0.1至2.5％
5.a)标准葡萄提取物的磷脂复合物，和
b)标准积雪草提取物的磷脂复合物
在制备抗皮肤老化的药物和化妆品组合物中的用途。
6.a)标准葡萄提取物的磷脂复合物，和
b)标准积雪草提取物的磷脂复合物
与其它选自维生素E、锌、羟基酸和甘草亭酸或其与磷脂的复合物的活性成分的组合在制备抗皮肤老化的药物和化妆品组合物中的用途。
CNB028098919A 2001-05-17 2002-05-10 抗皮肤老化的药物和化妆品组合物 Expired - Fee Related CN100387219C (zh)

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RU2003133289A (ru) 2005-03-10
WO2002092042A2 (en) 2002-11-21
CA2447525C (en) 2010-12-14
JP2004529951A (ja) 2004-09-30
EP1390008B1 (en) 2008-07-09
HK1069102A1 (en) 2005-05-13
HU230037B1 (hu) 2015-05-28
KR100891219B1 (ko) 2009-04-01
SK14172003A3 (sk) 2004-04-06
US7214395B2 (en) 2007-05-08
CZ299709B6 (cs) 2008-10-29
PT1390008E (pt) 2008-09-29
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DE60227505D1 (de) 2008-08-21
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ES2309182T3 (es) 2008-12-16
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PL204127B1 (pl) 2009-12-31

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