CN1708331A - 含有褪黑素、银杏和生物素的制剂 - Google Patents

含有褪黑素、银杏和生物素的制剂 Download PDF

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CN1708331A
CN1708331A CNA2003801023960A CN200380102396A CN1708331A CN 1708331 A CN1708331 A CN 1708331A CN A2003801023960 A CNA2003801023960 A CN A2003801023960A CN 200380102396 A CN200380102396 A CN 200380102396A CN 1708331 A CN1708331 A CN 1708331A
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H·W·施米德
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ASAT AG Applied Science and Technology
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Abstract

本发明涉及含有褪黑素、银杏(Ginkgo biloba)和生物素的组合作为活性物质的组合物。该组合物特别适合于制备用于在头发中局部应用的制剂。

Description

含有褪黑素、银杏和生物素的制剂
本发明涉及含有褪黑素、银杏(Ginkgo biloba)和生物素的组合作为活性物质的组合物。该组合物特别适合于制备用于在头发中局部应用的制剂。
已知褪黑素用于正面影响头发生长。由于与增殖中的控制着头发生长的毛囊细胞具有选择性相互作用，褪黑素对于头发生长具有刺激作用。在应用不同浓度的褪黑素时，可以观察到这种刺激作用。
US专利5,952,373描述了一种用于皮肤处理的方法，在该方法中涂敷一种含有一种或多种类黄酮作为活性物质的组合物。没有将褪黑素为用于改善头发生长的活性物质的提示。
US专利申请US 2002/0061870公开了一种用于缓解听力丧失或耳鸣的组合物。以片剂形式服用的所述组合物含有大量的活性物质，其中也有褪黑素、生物素或银杏。没有用于改善头发生长的应用或者关于局部施用的提示。
令人惊奇地，在本发明的范围内进行的研究确定，在使用褪黑素的同时添加银杏和生物素可增强褪黑素的作用，且提高褪黑素在头皮表面上的滞留。
因此，本发明的目标是一种组合物，其含有(a)褪黑素或其衍生物、(b)银杏的提取物和/或其一种或多种成分和(c)生物素用作为活性物质。该组合物优选为适用于药物和/或美容应用特别是涂敷在头皮上的局部制剂。
本发明的组合物含有活性物质的组合。该组合的第一种组分为褪黑素或褪黑素衍生物。褪黑素衍生物优选地选自5-甲氧基色胺、5-甲氧基色氨酸、5-甲氧基色醇、5-甲氧基吲哚-3-乙酸和6-羟基褪黑素。除了这些物质之外，还可以使用其生理上可接受的盐、酯和复合化合物。
该组合物的第二种组分为银杏。银杏对于不同的代谢功能具有正面影响。银杏的另一个有利的特性是增强自由基捕捉剂潜能。优选使用银杏的提取物，特别是干提取物，和/或其一种或多种成分。特别适合于本发明组合物的应用的是来自银杏叶的干提取物。
本发明的组合物的另一种组分为生物素。生物素例如在脂肪酸代谢和氨基酸代谢中作为辅酶而发挥其作用，例如在转羧基反应中。
组合物中活性物质的浓度可以根据应用而在宽的范围内变化。有利的是，活性物质的浓度各自独立地位于组合物总重量的0.0001重量％至1重量％之间。褪黑素或褪黑素衍生物的浓度优选为0.001重量％-0.01重量％。银杏的浓度优选为0.01重量％-0.1重量％。生物素的浓度优选为0.002重量％-0.05重量％。
每次施用，优选地给予大约0.001mg-大约10mg，优选大约0.01mg-大约1mg的褪黑素或褪黑素衍生物。
本发明组合物的这三种组分显示出促进头发生长、防止老化、改善头发密度和/或降低静止期比率的作用特性。褪黑素对于毛囊的作用通过与银杏和生物素的组合而令人惊奇地得到增强。因此，使用非常低浓度的褪黑素，例如每次施用为大约0.001-10mg，优选大约0.01-1mg，而还能获得令人满意的效果。
褪黑素、银杏和生物素的组合可以在合适的载体体系中进行给药。活性物质优选地溶解和/或分散在液体、半固体或固体的载体体系中。合适的载体体系的例子为液体如水或含水的缓冲溶液、生理上相容的有机溶剂如乙醇或者其组合，油-水乳液、水-油乳液、脂肪、聚乙二醇、丙二醇、甘油、乳化剂或者其组合，以及其他在药物和美容制剂中使用的载体或助剂。
优选使用含水的载体体系，即水含量为50重量％或更高，特别是60重量％或更高的载体体系。将含水的载体体系的pH值优选地调节为pH3-pH6，特别优选为pH3.5-pH4。
这种载体体系有利地使得能够将活性物质定向地给予毛囊。由此最佳化了活性物质在毛囊中的定位。此外，通过载体体系还能够控制活性物质褪黑素、银杏和生物素的吸收。
此外，在合适的载体体系中将褪黑素与银杏和生物素进行加工还可以导致防止或延缓褪黑素的吸收。由此不会影响正常的人血浆水平。而且还可以获得活性物质的更长的持续作用。
通过在载体体系中进行配制可以得到稳定的制剂，该制剂用于美容品中，特别是美容溶液形式的美容品。
当使用特殊的配制体系，例如脂质体、纳米体(Nanosom)或固态包含式载体如琼脂糖时，可以获得能控制地释放至少一种活性物质特别是所有活性物质的组合物。
本发明的组合物特别适合于药物和/或美容的应用，例如在头发中应用。该组合物可以以溶液、悬浮液、乳液、微乳液、纳米体系、霜剂、凝胶、洗液、喷雾剂、泡沫或软膏或者每种其他适合于局部应用的形式存在。该组合物通常在包装体系或应用体系中使用，包装体系或应用体系可选自管、瓶、喷雾瓶、膏药、海绵和织物载体或塑料载体，和其他适合于在头发中施用的体系。特别优选的包装体系为提供一个用于施用的剂量单位的单剂量安瓿瓶。该安瓿瓶可以由不同的材料例如玻璃或塑料制成。特别优选的是塑料安瓿瓶，因为塑料安瓿瓶保证了安全和良好的使用。
除了活性物质之外，本发明的组合物还可以含有一种或多种美容和/或药物的助剂或添加剂，例如增稠剂、矿物质、油、维生素如维生素A(特别是以视黄酸形式)或者芳香物质。
特别推荐本发明的组合制剂在晚上使用，其特别是在夜间发挥其作用。以这种方式使用时，组合物的作用特别强。本发明的组合物特别适合于刺激毛囊，和对于头发生长产生正面影响。
特别是以局部的、对于在头发中应用适合的施用形式使用，该施用形式含有相应的、适合于各个使用目的的活性物质浓度。
本发明的组合物可用于促进头发生长，特别是用于在男性或女性中预防和/或治疗脱发。特别优选的适应症为男性类型的雄激素性脱发、女性类型的雄激素性脱发、男性类型的弥漫性脱发和女性类型的弥漫性脱发。
通过下面的实施例来进一步解释本发明。
实施例：含有活性物质褪黑素、银杏和生物素的本发明制剂的组合物
组合物含有0.05重量％的银杏干提取物、0.01重量％的生物素、0.0033重量％的褪黑素，以及其他添加剂、水和乙醇。组合物的pH值为3.5-4。

Claims (19)

1.一种组合物，其特征在于，该组合物含有
(a)褪黑素或其衍生物，
(b)银杏，和
(c)生物素
作为活性物质。
2.根据权利要求1的组合物，其特征在于，该组合物含有褪黑素或者一种选自5-甲氧基色胺、5-甲氧基色氨酸、5-甲氧基色醇、5-甲氧基吲哚-3-乙酸和6-羟基褪黑素的褪黑素衍生物，以及其生理上可接受的盐、酯和复合化合物。
3.根据权利要求1或2的组合物，其特征在于，该组合物含有银杏干提取物和/或其一种或多种成分。
4.根据前述权利要求中任一项的组合物，其特征在于，活性物质的浓度各自基于组合物总重量为0.0001重量％至1重量％之间。
5.根据前述权利要求中任一项的组合物，其特征在于，活性物质溶解和/或分散在液体、半固体或固体的载体体系中。
6.根据前述权利要求中任一项的组合物，其特征在于，该组合物可以控制地释放至少一种活性物质。
7.根据前述权利要求中任一项的组合物，其用于药物和/或美容的应用。
8.根据权利要求1-7中任一项的组合物，其作为局部制剂。
9.根据权利要求7或8的组合物，其用于在头发中应用。
10.根据权利要求8或9的组合物，其特征在于，至少一种活性物质的经皮肤的吸收是可控制的。
11.根据前述权利要求中任一项的组合物，其特征在于，其以溶液、悬浮液、乳液、微乳液、纳米体系、霜剂、凝胶、洗液、喷雾剂、泡沫或软膏的形式存在。
12.根据前述权利要求中任一项的组合物，其位于包装体系或应用体系中，该包装体系或应用体系选自塑料或玻璃制成的单剂量安瓿瓶、管、瓶、喷雾瓶、膏药、海绵和织物载体或塑料载体。
13.根据前述权利要求中任一项的组合物，其通过添加银杏和生物素而增强褪黑素的刺激毛囊的作用。
14.根据前述权利要求中任一项的组合物用于促进头发生长的用途。
15.根据权利要求14的用途，其用于制备用于预防和/或治疗脱发的药剂。
16.根据权利要求15的用途，其用于治疗男性脱发。
17.根据权利要求15的用途，其用于治疗女性脱发。
18.根据权利要求14-17中任一项的用途，其特征在于，每次施用给予0.001mg-10mg的褪黑素。
19.根据权利要求18的用途，其特征在于，每次施用给予0.01mg-1mg的褪黑素。
CNA2003801023960A 2002-10-30 2003-10-30 含有褪黑素、银杏和生物素的制剂 Pending CN1708331A (zh)

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DE10250646A DE10250646A1 (de) 2002-10-30 2002-10-30 Melatonin in kosmetischen Formulierungen
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DE20217814.5 2002-11-18
US10/353,056 2003-01-29
US10/353,056 US20040094449A1 (en) 2002-11-18 2003-01-29 Melatonin daily dosage units
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