CN105377220B - 口服施用的用于头发老化控制的岩芹酸与锌的组合 - Google Patents
口服施用的用于头发老化控制的岩芹酸与锌的组合 Download PDFInfo
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- CN105377220B CN105377220B CN201480038806.8A CN201480038806A CN105377220B CN 105377220 B CN105377220 B CN 105377220B CN 201480038806 A CN201480038806 A CN 201480038806A CN 105377220 B CN105377220 B CN 105377220B
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Abstract
本发明涉及通过口服施用的包含岩芹酸和锌、尤其锌(II)盐的活性剂的组合用于改善头发品质、以及用于预防和控制毛囊的微炎症,特别是用于控制女性或年龄超过30岁的男性的头发老化的美容用途,其中,所述锌优选与一种或多种(多)羟基酸络合,例如葡萄糖酸锌。
Description
技术领域
本发明涉及对角蛋白纤维、特别为头发进行护理的领域。特别地,本发明的目的在于提供一种用于改善头发品质以及用于对抗角蛋白纤维、更特别为头发纤维的老化,特别是引起角蛋白纤维或更普遍地为头发的变稀疏的组合。
背景技术
如下文所述,在本发明的背景下,对于女性或年龄超过30岁的男性而言,对抗头发的老化尤其是个问题。
头发是由毛囊产生的,所述毛囊由表皮起源的上皮细胞鞘和包含在头发生长期间处于恒定分裂状态的球状角质细胞的毛球组成。头发主要由85%至90%的蛋白质构成。
一生自始至终拥有健康、强韧的头发是大部分女性和男性的理想。
因此,本发明的第一个目的是向任意年龄的男性和女性提供用于改善她(他)们的头发的品质的解决方案。
特别地,女性和年龄超过30岁的男性常经受他(她)们的角蛋白纤维、特别为头发纤维的老化。因此,他们可能显示出与头发老化相关的秃头症,其特征特别在于头发材料全面的变稀疏和脱落以及逐渐减轻。
这点的特征在于被称作雄激素源性脱发的秃头症的某些方面,根据定义,其传播是遗传性的,其过程是迅速的,并且,其最初只影响前额和两鬓,由于雄激素的作用,其在青春期后很早就出现,主要发生在年轻的男性身上。
最近的研究已经证实,对于更多老年个体而言,并且无区别对待男性和女性的情况,花费更长时间得以确立的秃头症的形式,涉及在毛囊逐渐退化和毛囊小型化中作为促成因子的被称作低噪音炎症(low noise inflammation)、也被称为微炎症(Mahé等人,Androgenetic alopecia and micro inflammation Int.J.Dermatol.,2000,39,576-584和Trueb,Clinical intervention in aging hair,2006:1(2)121-129)的潜在的和无征兆形式的炎症的贡献(Pro-inflammatory cytokine cascade in human plucked hair,Mahé等人,Skin Pharmacol,1996,366-375)。
这种被叫做毛囊微炎症的现象被Mahé等人(International Journal ofDermatology,2000,39,576-584)确定和描述,作为慢性的、细微的和无痛的炎症,其不会引起发红、瘙痒或发热、或任何通常与头皮的炎症有关的治疗性疾病。
虽然它可能涉及毛囊周的淋巴细胞或单核细胞的炎症细胞浸润,但它显著地区别于“常规的”炎症,所述“常规的”炎症可能发生在真皮或头皮中,其更刺激、甚至更痛苦地显露出来,并且其对头皮和头发纤维更具毁灭性的后果。特别地,它区别于与已确认的免疫炎症失调有关的斑秃(alopecia areata),所述免疫炎症失调导致大量的、偶尔局部的和通常自发可逆的脱发,无差别地影响男性、女性和儿童,这使得原则上排除雄激素在它的病理生理学上的影响成为可能。
相反,低噪音微炎症通过头皮和头发的更渐进的和自然的老化发挥影响。如前文所示,根据本发明的毛囊周的微炎症和毛囊的微炎症除了导致发束变稀疏,而且可以导致脱发,从而导致相当扩散的秃头症、甚至以头顶为中心的秃头症,特别是女性或年龄超过30岁的男性,与雄激素源性脱发相反,其从头顶和前额开始,并且主要影响年轻的男性。
以这种微炎症为特征的头发老化实际上是自然现象,其取决于个体,渐进地、有点早地发生。这种微炎症在表面很少被察觉到,尤其具有引发毛囊周的真皮失调的后果,导致头发的内根鞘变厚,以及在新的功能毛囊再生的逐次循环的过程中它的逐渐微小化。因此,观察到发束变稀疏,发束厚度减小并且对牵拉和断裂具有较差抵抗力,整个头部的头发体积减小。此外,头皮在某些地方变得可见,随着头顶明显的变秃,然而,并没有系统地大大影响两鬓或前额。甚至有时候,这种扩散的、晚发性的和缓慢展开的秃头症可以取代或加强和突出雄激素源性脱发的初始阶段的影响。此外,头发老化也具有头发纤维磨损和损伤的特征,体现为变脆的/敏感的头发、或干燥的头发。
因此,清楚地看到这种毛囊周的微炎症,其代表毛球和头发纤维的自然老化,仅仅是美容的失调、特别是由前文所列举的那些的起因。与常规的炎症相比,与常规的炎症相关的失调落入治疗领域,而与毛囊的临床无征兆和低噪音的微炎症的预防和/或治疗相关的失调仅仅落入美容的领域。
因此,还需要活性剂,甚至活性剂的组合,其能够预防和/或对抗毛囊的微炎症。
此外,文献WO 2008/071897描述了用于局部施用于头发的用于治疗或预防头发的损伤、以及用于改善角蛋白纤维的品质的包含岩芹酸的组合物。
然而,消费者始终在寻找更有效地改善他们头发的品质的活性剂或活性剂的组合。此外,特别是对于女性和年龄超过30岁的男性而言,目前还没有特别适合于预防和对抗毛囊低噪音微炎症和对抗发束逐渐变稀疏的活性剂。
发明内容
本发明通过提供口服施用的、岩芹酸与锌、尤其是锌(II)盐、优选为与一种或多种(多)羟基酸络合的锌,例如葡萄糖酸锌的组合来满足这种需求。
如本申请的实施例所阐明的,发明人实际上已经注意到根据本发明的活性剂的组合证明是能够协同地增加脂氧素A4的量。脂氧素A4属于消退素类。通常由身体自然地产生的这类化合物,通过提高引发“皮肤病学上常规的”炎症反应的阈值,更特别地为了提高这种常规炎症的信号的出现的阈值,即发红、疼痛和发热,以对常规抗炎剂补充的方式发挥效用。
因此,本发明的主题是包含岩芹酸和锌、尤其是锌(II)盐、优选为与一种或多种(多)羟基酸络合的锌,例如葡萄糖酸锌的活性剂的组合,用于改善头发的品质,特别是对于女性或年龄超过30岁的男性的头发的品质、且尤其用于改善头发纤维的品质的口服美容用途。
优选地,根据本发明,包含岩芹酸和锌、尤其是锌(II)盐、优选为与一种或多种(多)羟基酸络合的锌,例如葡萄糖酸锌的活性剂的组合的口服美容用途的特征在于对头发品质的改善,包括改善头发的光泽和/或改善头发的可造型性、和/或头发的强度和保持、和/或减少脱发和/或改善头发纤维的生长、尤其是浓密的头发纤维的生长和/或改善头发的体积和/或改善头发纤维的品质。
甚至更优选地,头发体积的改善包括头发纤维直径的增大和/或维持,和/或头发纤维密度的增大和/或限制头发纤维变稀疏。
同样优选地,改善头发纤维的品质包括提高头发的拉伸强度,和/或对头发的造型和/或成形的抵抗力,和/或预防和/或对抗柔弱的和/或易断的和/或暗淡的和/或开叉的和/或变脆的和/或敏感的和/或干燥的头发,和/或提高头发纤维的柔软度和/或活力。
本发明还针对岩芹酸和锌、尤其是锌(II)盐、优选为与一种或多种(多)羟基酸络合的锌,例如葡萄糖酸锌的组合用于预防和/或对抗女性或年龄超过30岁的男性的头发老化的口服美容用途。
本发明特别针对岩芹酸和锌、尤其是锌(II)盐、优选为与一种或多种(多)羟基酸络合的锌,例如葡萄糖酸锌的组合用于预防和/或对抗毛囊的和/或头皮的、特别是毛囊的低噪音微炎症的口服美容用途。
根据本发明,术语“头发老化”旨在表示头发纤维外观的变化(稀疏的、没有强度(柔弱)并且没有光泽的暗淡的头发),其具有脱离的倾向,其变得更新缓慢,对于这种头发纤维,由于胶原蛋白酶的大量释放和它的网络被破坏,故支持它的胶原蛋白网被损害,对于这种头发纤维,由于存在大量的糖化终产物导致真皮部分和上皮部分变得僵化(MonnierVM,1983),对于这种头发纤维,皮质的合成减少,从而导致头皮干燥,并且相应地增强了头发暗淡的外观和光泽的缺失,对于这种头发纤维,头皮的上皮和真皮也遭受了胶原蛋白网的破坏以及糖化产物的大量出现,这使得毛囊周的真皮僵化,对驻留毛囊和新头发的植入产生消极的影响。
术语“头发老化”也意味着头发密度的降低,以及体现为头皮覆盖面减小的发束直径的减小。
根据本发明,术语“发束的变稀疏”旨在表示发束的直径降低至40μm以下。有利地,发束的直径可以使用Trichoscan机器被测量,它是Trichogram的自动的等效物,其中,人眼被图像分析软件(Gasmueller,2009)所代替。此外,40μm以下,难于使用肉眼看到发束。因此,发束的变稀疏可以被感知。5%的阈值被认为是显著的。
根据本发明,术语“浓厚发束的生长”旨在表示直径大于40μm的发束的生长,它可以通过Trichoscan机器被测量,但是,它对肉眼也是容易可见的。
根据本发明,术语“增加头发密度”意思是防止每cm2有更多的头发。头发的密度也可以通过Trichoscan机器被测量。利用这个仪器,每cm2低于280根头发的密度被认为是低密度。5%的密度的增加被认为是临床显著的和可见的。
根据本发明,术语“预防脱发”意思是预防静止期的发束百分比的减小,这可以基于与生长期的发束相对比静止期的发束不再生长的事实,通过Trichoscan机器被测量。静止期的发束数量的5%的减少可以被认为是显著的。
根据本发明,术语“预防脱发”意味着退化期的发束百分比的减小,这可以通过Trichoscan机器或通过在造型中或在淋浴后收集发束进行测量,其基于退化期的发束是发束先前在生长停止期(静止期)所经历的可见的反应并且代表遭受反常的严重脱发的个体所真正感知的损失的事实。退化期的发束数量的5%的减少可以被认为是显著的。
根据本发明,术语“增大头发的总体积”旨在表示头发的直径的增大,其与发束直径的不均匀性的降低和每cm2头发数量的增多相关。
根据本发明,术语“预防和/或对抗柔弱的和/或易断的和/或干燥的和/或变脆的和/或暗淡的和/或开叉的头发”旨在表示对毛干的结构的整体的改善,特别是对角质层、发束的最外层的改善。
根据本发明,术语“改善头发的柔软度”旨在表示改善角质层的鳞片的状况,特别是改善它们的结合。脱离的(Disjointed)鳞片使得头发具有粗糙的感觉。
根据本发明,术语“改善头发的拉伸强度和头发纤维的活力”旨在表示改善头发的坚固性,这可以通过拉伸测试被测量。这种用于测量头发的拉伸机械性能的测试可以使用商业化工具,来自Dia Stron公司的MTT600(微型抗张强度测定仪)进行。破坏头发所需的力的5%的增加被认为是显著的。
根据本发明,术语“头发的可造型性”旨在表示头发易于梳理和/或刷。脱离的鳞片钩入相邻的发束的鳞片中,使得头发互相纠缠,这促使了打结的外观,使得更难于造型。
术语“可造型性”也意味着在插入发夹、吹风机吹干、放松或卷曲头发后,能更好地保持发型。
根据本发明,术语“头发的光泽”旨在表示减少磨损和/或修复角质层的鳞片使得头发的表面变得均匀,并且促使反射光泽。
优选地,上述定义的各种参数,可以由男性和/或女性在可由皮肤科医生进行观察研究的背景下通过选择题问卷被评估。如果至少50%的男性和/或女性感知到积极的影响,这种影响将被认为是显著的。
女性和年龄超过30岁的男性尤为被根据本发明的用途和方法关注。
为了本发明的目的,术语“男性”指的是人类男性人口。
本发明的主题还为根据本发明的食品补充剂形式的活性剂的组合的用途。
本发明的主题还为口服施用的美容组合物或食品补充剂,所述美容组合物或食品补充剂包含岩芹酸、锌,优选葡萄糖酸锌、和牛磺酸,其中,岩芹酸相对于所述活性剂组合的总重量,以按重量计10%至70%的含量存在。
本发明的另一主题为口服施用的美容组合物或食品补充剂,所述美容组合物或食品补充剂包含岩芹酸和锌、尤其锌(II)盐、和牛磺酸的组合,所述的锌优选为与一种或多种(多)羟基酸络合的锌,例如葡萄糖酸锌,其中,岩芹酸相对于所述活性剂组合的总重量,以按重量计20%至70%的含量存在。
优选地,这种组合物或这种食品补充剂还包含维生素D3和生育酚乙酸酯。
术语“锌”意思是锌或其盐(乙酸锌、氯化锌、柠檬酸锌、乳酸锌、葡萄糖酸锌、乳酸锌、氧化锌、碳酸锌或硫酸锌),特别为锌(II)盐,优选为与一种或多种(多)羟基酸络合的锌,例如葡萄糖酸锌。
术语“(多)羟基酸”意思是任何羧酸,所述羧酸包含直链的或支链的、以及饱和的或不饱和的,优选为饱和的和/或直链的基于烃的链,所述基于烃的链包含1个至10个碳原子以及1个至9个羟基,并包含1个至4个羧基-C(O)-OH,其中,至少一个所述-C(O)-OH官能团以羧酸盐的形式-C(O)-O-与锌原子,优选地锌(II)络合。
更特别地,根据本发明的锌盐与两个羧酸盐基团络合,如式(I)所示:
R-C(O)-O-Zn-O-C(O)-R' (I)
其中,R和R’,可以相同或不同,代表(C1-C6)(多)羟烷基,以及它们的溶剂化物,例如它们的水合物和它们的对映异构体。
优选地,式(I)所示的化合物为葡萄糖酸锌。
根据本发明特定的实施方式,所述锌不是氧化锌,而是锌盐。术语“锌(II)”意思是处在氧化态Zn2+的锌原子。
在根据本发明的产品用于个体的口服使用的范围内,可以使用的盐显然是由于它们的完全无害性被选择。
本发明还涉及用于以下方面的美容方法:
-改善头发的品质;和/或
-预防和/或对抗女性或年龄超过30岁的男性的头发老化;和/或
-预防和/或对抗毛囊和/或头皮的低噪音微炎症;
所述方法至少包括将根据本发明的活性剂的组合、或包含此种活性剂组合的口服组合物或食品补充剂口服施用至个体。
根据本发明的方法具有美容方法的特征,尤其是在它们使得改善头发的美感成为可能的范围内,特别地通过对抗尤其随着年龄而出现的发束逐渐稀疏。此外,根据本发明的活性剂的组合、组合物或食品补充剂可以被持续数月地每日使用,无需医学处方。因此,本发明明显地不属于治疗领域。
特别地,本发明的美容方法和/或用途使得保护老化的头发成为可能,尤其是对于女性或年龄超过30岁的男性。
本发明还涉及食品补充剂,其包含在第一组合物中的构成根据本发明的活性剂的组合的化合物的一部分、以及在第二组合物中的构成活性剂组合的化合物的至少另外一部分,作为在一段时间内同时使用、单独使用或相继使用的套件或组合产品。
根据本发明的上下文了解到,“口服的美容用途”涉及口服施用的产品的用途,例如,这些产品为如下文所列举的食品补充剂的形式。这些产品对头发产生美学的和舒适的效果,或者可替选地,产生具有美容目的的效果,例如着眼于保护头发、保持头发处于良好的状态,尤其使头发更具吸引力、尤其通过增大整个头部的头发的体积和保持。
术语“富含岩芹酸的油”意思是包含至少20%的岩芹酸、更优选地包含超过30%的岩芹酸的油。
可选地,岩芹酸、或单不饱和脂肪酸(C18:1n-12或顺式δ6)或C18δ-6-顺式-十八碳烯酸,被用于根据本发明的活性剂的组合中。
伞形科(Umbellifera)植物是其花呈伞形排列的植物。特别富含岩芹酸的物种是伞形科(Umbellifarea-Apiacea)和五加科(Araliaceae)。毒胡萝卜属(Thapsia genus)的植物也是岩芹酸的来源(Avato等人,Lipids,2001,36,845)。优选地被用于本发明的物种是芫荽、细叶芹(chervil)、胡萝卜、芹菜、枯茗(cumin)、葛缕子(caraway)、欧芹和莳萝。根据本发明所用的伞形科植物油可以从这些伞形科植物的种子中提取,例如,通过研磨或压榨,然后通过精炼。伞形科植物油具有的岩芹酸含量根据进行提取的伞形科植物的种子而变化。对于同一伞形科植物,岩芹酸含量还根据伞形科植物的原产国和根据大体上完全的提取过程而变化。
岩芹酸也是红花老鹳草(Geranium sanguineum)种子油中的丰富的化合物(大约48%),也是芫荽(Coriandrum sativum)种子油中的丰富的化合物(大约65%)。
因此,根据一个实施方式,所述用途,即本发明的主题,是岩芹酸以伞形科植物油或红花老鹳草油的形式,优选地以芫荽(Coriandrum sativum)油、细叶芹油、胡萝卜油、芹菜油、枯茗油、葛缕子油、欧芹油或莳萝油的形式,优选地以芫荽(Coriandrum sativum)种子油的形式被使用。
所述岩芹酸的含量是可变的,其取决于根据本发明的活性剂的组合是被用于口服施用的美容组合物还是用于食品补充剂中。
如下所示的含量作为指导。
在根据本发明的用于口服施用的美容组合物中或在根据本发明的食品补充剂中的岩芹酸的含量可以为所述组合物或所述补充剂的总重量的1%至70%,特别为所述组合物或所述补充剂的总重量的10%至70%,特别为所述组合物或所述补充剂的总重量的15%至70%。在根据本发明的用于口服施用的美容组合物中或在根据本发明的食品补充剂中的岩芹酸的含量可以为:即所述岩芹酸的日剂量为5mg/天至1000mg/天,特别为50mg/天至650mg/天。
根据优选的变型,根据本发明的活性剂的组合、美容组合物或食品补充剂还包括牛磺酸。
根据优选的变型,根据本发明的活性剂的组合、美容组合物或食品补充剂还包括维生素D3。
根据优选的变型,根据本发明的活性剂的组合、美容组合物或食品补充剂还包括牛磺酸和维生素D3。
根据优选的变型,根据本发明的活性剂的组合、美容组合物或食品补充剂还包括生育酚乙酸酯。
根据优选的变型,根据本发明的活性剂的组合、美容组合物或食品补充剂还包括至少一种氨基酸,所述至少一种氨基酸选自是蛋白质的组分和/或不是蛋白质的组分的氨基酸,特别为精氨酸、半胱氨酸和/或甲硫氨酸。
根据本发明,术语“牛磺酸”是指牛磺酸、亚牛磺酸、或它们的盐。
在根据本发明的组合用于个体的口服使用的范围内,可以使用的盐显然是由于它们的无害性被选择。碱金属盐或碱土金属盐,特别为镁盐、锰盐、铁(II)盐或锌(II)盐在这方面是适合的。
在根据本发明的用于口服施用的美容组合物中或在根据本发明的食品补充剂中的牛磺酸、亚牛磺酸或它们的盐的含量可以为所述组合物总重量的1%至40%,特别为所述组合物或所述补充剂总重量的5%至40%,特别为所述组合物或所述补充剂总重量的5%至30%。
在根据本发明的用于口服施用的美容组合物中或在根据本发明的口服食品补充剂中的牛磺酸、亚牛磺酸或它们的盐的含量可以为:即所述牛磺酸、亚牛磺酸或它们的盐的日剂量为4mg/天至700mg/天,特别为40mg/天至300mg/天。
在根据本发明的用于口服施用的美容组合物中或在根据本发明的食品补充剂中的锌、特别为葡萄糖酸锌的含量,相对于所述活性剂的组合的总重量,可以为按重量计0.001%至30%,尤其为按重量计0.01%至25%,特别为按重量计0.1%至20%。
在根据本发明的用于口服施用的美容组合物中或在根据本发明的食品补充剂中的葡萄糖酸锌的含量可以为:即所述葡萄糖酸锌的日剂量为0.01mg/天至300mg/天,尤其为0.1mg/天至200mg/天,特别为1mg/天至100mg/天。
根据本发明的另一个实施方式,根据本发明的活性剂的组合包含岩芹酸和锌,但不包牛磺酸。
根据本发明的另一个优选的实施方式,活性剂的组合包含岩芹酸、牛磺酸、锌,特别为葡萄糖酸锌、和维生素D3。
根据一个实施方式,根据本发明的用于口服施用的美容组合物或食品补充剂还可以包含至少一种维生素,所述至少一种维生素选自于维生素B1、维生素B5、维生素B6、维生素B8、维生素B9、维生素B12、维生素C、维生素D,特别地维生素D3、维生素PP或生育酚(维生素E)以及其衍生物,尤其例如生育酚乙酸酯、生育酚琥珀酸酯或生育酚棕榈酸酯的酯,优选生育酚乙酸酯。
根据该实施方式,根据本发明的用于口服施用的美容组合物或食品补充剂优选地至少包含维生素E或其衍生物和/或维生素D,优选地维生素D3和/或生育酚乙酸酯。
根据特定的实施方式,根据本发明的用于口服施用的美容组合物或食品补充剂包含维生素D3和生育酚乙酸酯。
因此,根据本发明优选的实施方式,本发明针对用于口服施用的美容组合物或食品补充剂,所述美容组合物或食品补充剂包含岩芹酸、锌且尤其锌(II)盐、牛磺酸、维生素D3和生育酚乙酸酯,所述锌优选为与一种或多种(多)羟基酸络合的锌,优选为葡萄糖酸锌。
根据本发明的组合物可以包含至少一种类胡萝卜素,特别为选自β-类胡萝卜素、番茄红素、虾青素、玉米黄素和叶黄素的类胡萝卜素,类黄酮(例如花青素)、黄酮醇、黄烷醇类(从葡萄提取的原花青素、从绿茶提取的儿茶素)、黄烷酮类(橙皮素、地奥司明)、酚酸以及衍生物(来自咖啡提取物的氯原酸)、二萜类、二苯乙烯类、菊苣提取物、银杏叶提取物、甘椒提取物、大豆提取物、其他来源的具有抗氧化性能的类黄酮、脂肪酸、益生元、益生菌、白藜芦醇、氨基酸、硒和谷胱甘肽前体。
根据本发明的口服组合物或食物补充剂还可以包含至少一种益生菌、益生元或益生菌的混合物和益生元的混合物。作为益生菌微生物,尤其可以提及约氏乳杆菌(Lactobacillus johnsonii)或副干酪乳杆菌(Lactobacillus)。
根据本发明的用于口服施用的美容组合物或食品补充剂可以是通常使用的任何口服途径的盖仑制剂形式。
在本文中,当讨论限度x至y时,应当理解为包含所述限度x和y。
食品补充剂
根据一个实施方式,根据本发明的用于口服施用的美容组合物或食品补充剂包含:
(i)相对于所述活性剂的组合的总重量,含量为按重量计1%至70%、尤其为按重量计10%至70%、特别为按重量计20%至70%的岩芹酸;
(ii)至少一种相对于所述活性剂的组合的总重量,含量为按重量计0.001%至40%、尤其为按重量计0.01%至25%、特别为按重量计0.1%至20%的(多)羟基酸锌,优选为葡萄糖酸锌;
(iii)可选地,相对于所述活性剂的组合的总重量,含量为按重量计1%至50%、尤其为按重量计5%至40%、特别为按重量计10%至30%的牛磺酸;和/或
(iv)可选地,相对于所述活性剂的组合的总重量,含量为按重量计0.0001%至1.0%、尤其为按重量计0.0001%至0.5%、特别为按重量计0.0001%至0.1%的维生素D3;和
(v)可选地,相对于所述活性剂的组合的总重量,含量为按重量计0.01%至10%、尤其为按重量计0.1%至10%、特别为按重量计0.2%至5%的生育酚乙酸酯。
根据特定的实施方式,根据本发明的用于口服施用的美容组合物或食品补充剂包含如下的成分i)至成分v),所述成分可以被一起服用或被单独服用:
(i)相对于所述组合物或所述补充剂的总重量,含量为按重量计1%至70%、尤其为按重量计10%至70%、特别为按重量计15%至70%的岩芹酸;
(ii)至少一种相对于所述组合物或所述补充剂的总重量,含量为按重量计0.001%至30%、尤其为按重量计0.01%至25%、特别为按重量计0.1%至20%的(多)羟基酸锌,优选为葡萄糖酸锌;
(iii)可选地,相对于所述组合物或所述补充剂的总重量,含量为按重量计1%至40%、尤其为按重量计5%至40%、特别为按重量计5%至30%的牛磺酸;和/或
(iv)可选地,相对于所述组合物或所述补充剂的总重量,含量为按重量计0.0001%至1.0%、尤其为按重量计0.0001%至0.5%、特别为按重量计0.0001%至0.1%的维生素D3;和/或
(v)可选地,相对于所述组合物或所述补充剂的总重量,含量为按重量计0.01%至10%、尤其为按重量计0.1%至10%、特别为按重量计0.2%至5%的生育酚乙酸酯。
根据特定的实施方式,根据本发明的用于口服施用的美容组合物或食品补充剂包含上述所有成分i)至成分v)。
这种根据本发明的食品补充剂类型的组合物或口服施用的组合物可以尤其具有如下所示的含量:
组分 | 相对于组合物的总重量的重量百分比% |
岩芹酸 | 54.9(由芫荽种子油提供) |
葡萄糖酸锌 | 6.3(其中含有13.6%的活性物质) |
牛磺酸 | 18.7(其中含有98.5%的活性物质) |
维生素E | 1.0(其中含有67%的活性物质) |
维生素D3 | 0.03(其中含有2.5%的活性物质) |
为了摄取,口服组合物的多种实施方式以及特别是食品补充剂的多种实施方式是可能的。它们的配制通过用于生产包衣片剂、凝胶胶囊、凝胶、乳剂、片剂、锭剂或软胶囊剂的常用方法来进行。
根据本发明的、用于口服施用的组合物可以尤其地包含全部日剂量或仅一部分的日剂量。
换句话说,可以每天施用一次组合物至三次组合物。
典型地,这种用于口服施用的美容处理的持续时间可以超过4周,尤其是4周至24周,在适当的情况下,可以有一个或多个停用期。
根据本发明的食品补充剂可以包含在第一组合物中的构成根据本发明的组合的活性剂的一部分、和在第二组合物中的这些活性剂的另外一部分,作为在一段时间内同时使用、单独使用或相继使用的套件或组合产品。
这种补充剂可以通过被配制成使得所述两种组合物是以相同的形式或以不同的形式,例如选自于上文提及的那些。特别地,这样的套件可以在同一个包装中被提供。
毋庸置疑,本领域技术人员将会注意选择可选的额外添加剂和/或其用量,以便根据本发明的组合或根据本发明的包含该组合的组合物的有利性质不被、或基本上不被设想的添加剂所不利地影响。
根据本发明的活性剂可以使用通常的赋形剂和用于根据本发明的口服组合物的或补充剂的成分来配制,例如,尤其为脂肪成分和/或水性成分、润湿剂、增稠剂、防腐剂、结构剂和/或包覆剂、抗氧化剂、调味剂和染料,这些在食品补充剂行业是常见的。
作为与根据本发明的活性剂的组合不同的美容活性剂,根据本发明的组合物或食品补充剂可以包含额外的亲水性活性剂,所述额外的亲水性活性剂选自糖类和糖类衍生物、水溶性维生素、植物提取物(例如,来自迷迭香、松树皮、或如橙子的水果的提取物)、肽和氨基酸(例如精氨酸、甲硫氨酸、半胱氨酸、瓜氨酸)和/或额外的亲脂性活性剂,所述亲脂性活性剂选自视黄醇(维生素A)和其前驱体,尤其是β-胡萝卜素、抗氧化剂类胡萝卜素(例如番茄红素、玉米黄素、虾青素和叶黄素)、必需脂肪酸、植物油和动物油,尤其是必需的富含ω3、磷脂(例如卵磷脂)及其混合物的鱼油,来自葫芦科植物(例如西葫芦)的油或抗氧化酶来源(例如甜瓜)的油、益生菌和益生元、维生素和矿物质、多不饱和脂肪酸PUFA和单不饱和脂肪酸MUFA以及ω3脂肪酸和ω6脂肪酸。
本发明的其他特征和优点将由下文的实施例更清楚地呈现,其作为非限制性说明被给出。
具体实施方式
实施例1
软胶囊形式的口服组合物
实施例2
软胶囊形式的口服组合物
成分 | (mg/软胶囊) |
芫荽种子油(65%的岩芹酸) | 300 |
葡萄糖酸锌 | 25.75 |
维生素E | 4.10 |
赋形剂 | |
精炼椰子油 | 112 |
黄蜂蜡,黄蜡 | 22 |
向日葵卵磷脂 | 10 |
胶囊 | |
鱼胶 | 144.6 |
甘油 | 58.6 |
纯净水 | 6.8 |
实施例3
乳剂形式的棒状口服组合物
A.
B.
实施例4
岩芹酸和葡萄糖酸锌的组合对衍生自脂类代谢的内源性抗炎消退素的产生的影响的证明:实验模型中的脂氧素A4使用体外的人单核细胞。
单核血细胞在5%CO2和37℃下,在用于巨噬细胞(SFM巨噬细胞;Invitrogen12065074)的无血清培养基中被培养24h。这一步骤后,在待评估的各种产物存在下(芫荽油0.25mg/ml,葡萄糖酸锌0.005mg/ml),所述培养基被相同的新的测试培养基替换30分钟,所述新的测试培养基包含不同剂量的所述活性剂。在佛波醇肉豆蔻酸酯(0.05μM)和钙离子载体(1μM)和由二十二碳六烯酸(DHA-1μg/mL)和二十碳五烯酸(EPA-1μg/mL)组成的脂类基质混合物的存在下,激发炎性反应。
2小时的刺激后,上清液被收集,并且在准备进行质谱法分析之前被冷冻在-80℃。
每个实验条件,准备重复三次实验(三孔)。每个培养板内被放置与被PMA/A23187混合物刺激和/或由添加等摩尔的脂肪酸的混合物刺激的细胞相应的对照。
将解冻的上清液通过固相萃取(SPE)浓缩,在光谱分析前存放于甲醇中。所用的分析方法包括通过高压液相色谱根据它们的保留时间而分离各种分析物,以及通过质谱法量化它们。
使用LC 1290Infinity chain(安捷伦科技有限公司)进行所述分析,其与6460Triple Quad LC/MS质谱仪(安捷伦科技有限公司)连接,并且配备有电喷雾离子源(Jet stream技术),采用负模式运行。色谱分离在ZorBAX SB-C18柱上进行。
所述结果以pg/mL细胞上清液获得。然后,这些原始数据通过使用下述的计算方法进行计算来转化,以获得培养板的活化(抑制)相对于对照的百分比:
%调整=100×(活性剂所获得的数值–对照值)/对照值
这些调整的百分比列于下表中。
根据上述所示,对根据本发明的包含富含岩芹酸的芫荽油和葡萄糖酸锌活性剂的组合、以及单独地对这些同样的化合物进行测试。
这些对比测试后所获得的结果如下所示:
在这种情况下,还可以看出,根据本发明的组合对脂氧素A4的生产的影响非常显著地大于单个使用的化合物的影响的总和。
特别地,当测试的淋巴细胞放置成与活性剂的组合相接触时,可以看出,相对于这种抗炎成分的生产的基础水平,脂氧素A4的生产增加了94%。
因此,根据本发明的活性剂的组合的协同效应在本文中确实被观察到并且被证明。
Claims (17)
1.包含岩芹酸和葡萄糖酸锌的组合在制备用于增加脂氧素A4的量、从而改善女性或年龄超过30岁的男性的头发纤维的品质的制剂中的用途,其特征在于,所述头发纤维的品质的改善在于改善头发的拉伸强度、和/或预防和/或对抗柔弱的和/或易断的和/或暗淡的和/或开叉的和/或变脆的和/或敏感的和/或干燥的头发,和/或改善所述头发纤维的柔软度和/或活力。
2.如权利要求1所述的用途,其特征在于,所述岩芹酸是以伞形科植物油或红花老鹳草油的形式被使用。
3.如权利要求1所述的用途,其特征在于,所述岩芹酸是以芫荽油、细叶芹油、胡萝卜油、芹菜油、枯茗油、葛缕子油、欧芹油或莳萝油的形式被使用。
4.如权利要求1所述的用途,其特征在于,所述岩芹酸是以芫荽种子油的形式被使用。
5.如权利要求1所述的用途,其特征在于,所述组合还包含牛酸酸。
6.如权利要求1所述的用途,其特征在于,所述组合还包含维生素D3。
7.如权利要求1所述的用途,其特征在于,所述组合以食品补充剂的形式被使用。
8.如权利要求7所述的用途,其中,所述食品补充剂还包含至少一种维生素,所述至少一种维生素选自维生素B1、维生素B5、维生素B6、维生素B8、维生素B9、维生素B12、维生素C、维生素D。
9.如权利要求7所述的用途,其中,所述食品补充剂还包含维生素D3和/或生育酚乙酸酯。
10.如权利要求7所述的用途,其中,所述食品补充剂还包含至少一种氨基酸,所述氨基酸选自为蛋白质组分和/或不是蛋白质组分的氨基酸。
11.如权利要求7所述的用途,其中,所述食品补充剂还包含至少一种氨基酸,所述氨基酸选自为蛋白质组分和/或不是蛋白质组分的氨基酸,且所述为蛋白质组分和/或不是蛋白质组分的氨基酸选自精氨酸、半胱氨酸和/或甲硫氨酸。
12.如权利要求7所述的用途,其中,所述食品补充剂包含岩芹酸、牛磺酸和葡萄糖酸锌的组合。
13.如权利要求7所述的用途,其中,所述食品补充剂包含岩芹酸、葡萄糖酸锌、牛磺酸、维生素D3和生育酚乙酸酯。
14.一种食品补充剂,所述食品补充剂包含岩芹酸、葡萄糖酸锌、和牛磺酸的组合,其中所述岩芹酸相对于所述组合的总重量,以按重量计20%至70%的含量存在,所述食品补充剂用于增加脂氧素A4的量、从而改善头发纤维的品质,所述头发纤维的品质的改善在于改善头发的拉伸强度、和/或预防和/或对抗柔弱的和/或易断的和/或暗淡的和/或开叉的和/或变脆的和/或敏感的和/或干燥的头发,和/或改善所述头发纤维的柔软度和/或活力。
15.如权利要求14所述的食品补充剂,还包含维生素D3和生育酚乙酸酯。
16.如权利要求14所述的食品补充剂,包含:
(i)相对于所述食品补充剂的总重量,含量为按重量计1%至70%的岩芹酸;
(ii)相对于所述食品补充剂的总重量,含量为按重量计0.001%至30%的葡萄糖酸锌;
(iii)相对于所述食品补充剂的总重量,含量为按重量计1%至40%的牛磺酸;和/或
(iv)可选地,相对于所述食品补充剂的总重量,含量为按重量计0.0001%至1%的维生素D3;和/或
(v)可选地,相对于所述食品补充剂的总重量,含量为按重量计0.01%至10%的生育酚乙酸酯。
17.一种食品补充剂,包含在第一组合物中的岩芹酸,以及在第二组合物中的葡萄糖酸锌,所述食品补充剂作为在一段时间内同时使用、单独使用或相继使用的套件或组合产品,所述食品补充剂用于增加脂氧素A4的量、从而改善头发纤维的品质,所述头发纤维的品质的改善在于改善头发的拉伸强度、和/或预防和/或对抗柔弱的和/或易断的和/或暗淡的和/或开叉的和/或变脆的和/或敏感的和/或干燥的头发,和/或改善所述头发纤维的柔软度和/或活力。
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CN102293312A (zh) * | 2011-08-17 | 2011-12-28 | 周均升 | 一种生发黑发口香糖及其制作方法 |
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JP2009531290A (ja) * | 2006-02-16 | 2009-09-03 | ディーエスエム アイピー アセッツ ビー.ブイ. | 新規栄養補助および医薬組成物、ならびに炎症性障害の治療、補助治療、または予防のためのそれらの使用 |
WO2008071897A2 (fr) * | 2006-12-14 | 2008-06-19 | L'oreal | Utilisation topique d'au moins un acide gras mono-insature pour ameliorer la chevelure |
FR2967070B1 (fr) * | 2010-11-05 | 2013-07-05 | Oreal | Acide gras monoinsature pour prevenir et/ou traiter les imperfections du teint de la peau |
-
2013
- 2013-05-07 FR FR1354187A patent/FR3005410A1/fr active Pending
-
2014
- 2014-05-06 WO PCT/IB2014/061245 patent/WO2014181257A1/fr active Application Filing
- 2014-05-06 ES ES14726424T patent/ES2721020T3/es active Active
- 2014-05-06 CN CN201480038806.8A patent/CN105377220B/zh active Active
- 2014-05-06 PT PT14726424T patent/PT2994091T/pt unknown
- 2014-05-06 US US14/889,984 patent/US20160095802A1/en not_active Abandoned
- 2014-05-06 EP EP14726424.6A patent/EP2994091B1/fr active Active
- 2014-05-06 CA CA2911368A patent/CA2911368A1/fr not_active Abandoned
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EP1013178A1 (en) * | 1998-12-22 | 2000-06-28 | Loders Croklaan B.V. | Petroselinic acid and its use in food, fat compositions containing petroselinic acid |
WO2002007700A2 (en) * | 2000-07-26 | 2002-01-31 | The Procter & Gamble Company | Compositions useful for regulating hair growth containing metal complexes of oxidized carbohydrates |
US20050175565A1 (en) * | 2002-06-21 | 2005-08-11 | L'oreal | Use of taurine for the treatment of alopecia |
CN1539445A (zh) * | 2003-04-22 | 2004-10-27 | 吴新胜 | 一种用于生发乌发的中西药复方制剂 |
WO2008081142A2 (fr) * | 2006-12-14 | 2008-07-10 | L'oreal | Utilisation orale d'au moins un acide gras mono-insature pour ameliorer la chevelure |
US20100022648A1 (en) * | 2006-12-14 | 2010-01-28 | L'oreal | Oral use of at least one monounsaturated fatty acid for hair improvement |
CN102293312A (zh) * | 2011-08-17 | 2011-12-28 | 周均升 | 一种生发黑发口香糖及其制作方法 |
Also Published As
Publication number | Publication date |
---|---|
CN105377220A (zh) | 2016-03-02 |
US20160095802A1 (en) | 2016-04-07 |
FR3005410A1 (fr) | 2014-11-14 |
EP2994091B1 (fr) | 2019-02-13 |
EP2994091A1 (fr) | 2016-03-16 |
PT2994091T (pt) | 2019-05-27 |
ES2721020T3 (es) | 2019-07-26 |
CA2911368A1 (fr) | 2014-11-13 |
WO2014181257A1 (fr) | 2014-11-13 |
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