CN117460491A - 抗老化化妆料组合物 - Google Patents
抗老化化妆料组合物 Download PDFInfo
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- CN117460491A CN117460491A CN202280039995.5A CN202280039995A CN117460491A CN 117460491 A CN117460491 A CN 117460491A CN 202280039995 A CN202280039995 A CN 202280039995A CN 117460491 A CN117460491 A CN 117460491A
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Abstract
本发明涉及一种通过强化皮肤的基底膜来强化皮肤真皮层并改善皮肤弹性或皮肤皱纹的组合物。本发明的组合物同时包含由化学式1表示的化合物;以及由化学式2表示的化合物和/或由化学式3表示的化合物,从而与单独包含由化学式1表示的化合物、单独包含由化学式2表示的化合物或单独包含由化学式3表示的化合物的组合物相比,具有更优异的改善皮肤弹性或皱纹的效果。
Description
技术领域
本发明涉及一种通过强化皮肤基底膜来强化皮肤真皮层并改善皮肤弹性或皮肤皱纹的组合物。
背景技术
胶原蛋白是从皮肤的成纤维细胞(fibroblast)产生的主要基质蛋白,存在于细胞外间质中。众所周知,胶原蛋白与皮肤的机械坚固性、结缔组织的抵抗力和组织的结合力、细胞粘附的支撑、细胞分裂和分化(有机体的生长或伤口愈合时)的诱导有关,从而起到重要的功能。这种胶原蛋白因年龄增长带来的自然老化或紫外线照射导致的光老化而减少,并且减少过程由分解胶原蛋白的胶原酶(collagenase)酶的活性促进。众所周知,胶原蛋白的减少与皮肤弹性下降或皱纹形成有着密切的关联。这种胶原蛋白是在哺乳动物中大量发现的纤维蛋白,构成体内骨骼、软骨、基底膜等。
其中,皮肤基底膜(skin basement membrane)在表皮细胞的支撑和附着、营养物质的迁移、表皮分化的调节等方面起着重要作用。如果皮肤基底膜因老化而受损,则会引起基底膜的扁平化、多重化、断裂等,从而产生皱纹,并且外部危险因素渗透到真皮的可能性增加,皮肤可容易受损。因此,要想恢复受损的皮肤基底膜或维持为健康状态,首先要确保其构成成分能够正常维持。
同时,成纤维细胞生长因子(fibroblast growth factor,FGF)是调节多种细胞增殖、迁移、分化和生存的生长因子之一,由23种构成的一组蛋白质构成。FGF由角质细胞、成纤维细胞、血管内皮细胞、平滑肌细胞、软骨细胞和肥大细胞等产生,并通过激活在多种细胞中表达的四种成纤维细胞生长因子受体(FGF receptor)来表现出上述功能。众所周知,特别是,FGF 2、FGF 7和FGF 10在皮肤再生中起着重要作用(非专利文献1)。FGF 7和FGF 10通过促进角质细胞的增殖参与再上皮化过程,并且还通过中和活性氧参与维持角质细胞的过程。
传统技术旨在通过胶原蛋白来改善皮肤弹性或皱纹,而这些促进胶原蛋白合成的方法主要以强化表皮层为特征。然而,存在的问题是,仅通过表皮层的强化,在应用于实际皮肤时,会发现不会产生改善皮肤弹性或皱纹的效果的情况。因此,迫切需要开发一种通过强化实际皮肤基底膜来强化皮肤真皮层并改善皮肤弹性或皱纹的皮肤抗老化组合物。
[现有技术文献]
[非专利文献]
1:Barrientos S,Stojadinovic O,Golinko M,Brem H,Vinay Tomic-CanicM.2008.Growth factors and cytokines in wound healing.Wound Rep Reg.16:585
发明内容
技术课题
对此,本发明人为了寻找一种通过强化皮肤基底膜来表现出作为抗老化效果的改善皮肤弹性或皱纹的效果的组合物而进行了努力,其结果,确认了由化学式1表示的化合物虫草素、由化学式2表示的化合物穿心莲内酯和由化学式3表示的槲皮素表现出改善皮肤弹性或皱纹的效果,特别是确认了当同时利用由化学式1表示的化合物;以及由化学式2表示的化合物和/或由化学式3表示的化合物时,对强化皮肤真皮层、改善皮肤弹性以及改善皱纹具有优异的效果,从而完成了本发明。
因此,本发明的目的是提供一种用于改善皮肤弹性或皱纹的化妆料组合物,其包含由化学式1表示的化合物或其生理学上可接受的盐;以及由化学式2表示的化合物或其生理学上可接受的盐和/或由化学式3表示的化合物或其生理学上可接受的盐作为有效成分。
本发明的另一目的是提供一种用于改善皮肤弹性或皱纹的药学组合物,其包含由化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐和/或由化学式3表示的化合物或其药学上可接受的盐作为有效成分。
技术方案
为了实现上述本发明的目的,本发明提供了一种用于改善皮肤弹性或皱纹的化妆料组合物,其包含由化学式1表示的化合物或其生理学上可接受的盐;以及由化学式2表示的化合物或其生理学上可接受的盐和/或由化学式3表示的化合物或其生理学上可接受的盐作为有效成分。
另外,本发明提供了一种用于改善皮肤弹性或皱纹的药学组合物,其包含由化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐和/或由化学式3表示的化合物或其药学上可接受的盐作为有效成分。
本发明提供了一种改善皮肤弹性或皱纹的方法,其包括用化妆料组合物处理皮肤的步骤,该化妆料组合物包含由化学式1表示的化合物或其生理学上可接受的盐;以及由化学式2表示的化合物或其生理学上可接受的盐和/或由化学式3表示的化合物或其生理学上可接受的盐作为有效成分。
本发明提供了一种改善皮肤弹性或皱纹的方法,其包括给药药学组合物的步骤,该药学组合物包含由化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐和/或由化学式3表示的化合物或其药学上可接受的盐作为有效成分。
本发明提供了一种组合物在制备用于改善皮肤弹性或皱纹的产品中的用途,该组合物包含由化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐和/或由化学式3表示的化合物或其药学上可接受的盐作为有效成分。
[化学式1]
上述化学式1所代表的化合物的分子式为C10H13N5O3,分子量为251.12g/mol,并且命名为虫草素(Cordycepin)、3'-脱氧腺苷(3'-deoxyadenosine)、3'-脱氧-腺苷9-虫草苷腺嘌呤(3'-deoxy-adenosine 9-cordyceposidoadenine)、9-(3-脱氧-b-D-赤式-呋喃戊糖基)-9H嘌呤-6-胺(9-(3-Deoxy-b-D-erythro-pentofuranosyl)-9Hpurin-6-amine)、9-(3脱氧-b-D-呋喃核糖基)腺嘌呤(9-(3-Deoxy-b-D-ribofuranosyl)adenine)等。
本发明对上述虫草素的获得方法没有特别限制,并且可以通过本领域公知的方法化学合成,或者使用市售物质。
在本发明的组合物中,相对于组合物的总重量,上述虫草素的含量可以为0.00001至10重量%,例如0.00001至8重量%、0.00001至5重量%、0.00001至3重量%、0.00001至2重量%、0.00001至1重量%、或0.00002至1重量%。
[化学式2]
上述化学式2所代表的化合物的分子式为C20H30O5,分子量为350.45g/mol,并且命名为穿心莲内酯(Andrographolide)、3-[2-[十氢-6-羟基-5-(羟甲基)-5,8a-二甲基-2-亚甲基-1-萘基]亚乙基]二氢-4-羟基-2(3H)-呋喃酮(3-[2-[decahydro-6-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylene-1-napthalenyl]ethylidene]dihydro-4-hydroxy-2(3H)-furanone)等。
本发明对上述穿心莲内酯的获得方法没有特别限制,并且可以通过本领域公知的方法化学合成,或者使用市售物质。
在本发明的组合物中,相对于组合物的总重量,上述穿心莲内酯的含量可以为0.00001至10重量%,例如0.00001至8重量%、0.00001至5重量%、0.00001至3重量%、0.00001至2重量%、0.00001至1重量%、或0.00002至1重量%。
[化学式3]
上述化学式3所代表的化合物的分子式为C15H10O7,分子量为302.236g/mol,并且命名为槲皮素(quercetin)、槲皮素、2-(3,4-二羟基苯基)-5,7-二羟基-4H-1-苯并吡喃-4-酮(2-(3,4-Dihydroxyphenyl)-5,7-dihydroxy-4H-1-benzopyran-4-one)、3,3′,4′,5,7-五羟基黄酮(3,3′,4′,5,7-Pentahydroxyflavone)、5,7,3′,4′-黄酮-3-醇(5,7,3′,4′-flavon-3-ol)等。
本发明对上述槲皮素的获得方法没有特别限制,并且可以通过本领域公知的方法化学合成,或者使用市售物质。
在本发明的组合物中,相对于组合物的总重量,上述槲皮素的含量可以为0.00001至10重量%,例如0.00001至8重量%、0.00001至5重量%、0.00001至3重量%、0.00001至2重量%、0.00001至1重量%、或0.00002至1重量%。
另外,在本发明的组合物中,可以包含上述化学式1表示的化合物或其药学上可接受的盐和上述化学式2表示的化合物或其药学上可接受的盐的100:1至1:100重量比、或50:1至1:50的重量比。在本发明的组合物中,可以包含上述化学式1表示的化合物或其药学上可接受的盐和上述化学式3表示的化合物或其药学上可接受的盐的100:1至1:100重量比、或50:1至1:50的重量比。在本发明的组合物中,可以包含上述化学式1表示的化合物或其药学上可接受的盐;以及上述化学式2表示的化合物或其药学上可接受的盐和上述化学式3表示的化合物或其药学上可接受的盐的总量的100:1至1:100重量比、或50:1至1:50的重量比。
在本发明中,“改善皮肤弹性的效果”是指预防、抑制或阻碍皮肤弹性下降,或者使已经下降的皮肤弹性变好。
在本发明中,“改善皱纹的效果”是指预防、抑制或阻碍皮肤上产生皱纹,或者缓解已经产生的皱纹。
根据本发明的一个实施例,确认了当用由化学式1表示的化合物虫草素处理人成纤维细胞时,FGF 10的mRNA表达得到促进,确认了当用由化学式2表示的化合物穿心莲内酯处理人成纤维细胞时,FGF 10的mRNA表达得到促进,确认了当用由化学式3表示的化合物槲皮素处理人成纤维细胞时,FGF 10的mRNA表达得到促进。另外,确认了当用穿心莲内酯或槲皮素与虫草素一起处理人成纤维细胞时,与单独处理虫草素、单独处理穿心莲内酯以及单独处理槲皮素相比,FGF 10的mRNA表达量得到进一步增加。
众所周知,FGF 10在构成真皮的成纤维细胞中表达,起到强化皮肤基底膜并维持正常的作用。另外,FGF 10通过表皮和真皮之间的信号传递起到维持皮肤完整性(integrity)的作用,并与构成基底膜的主要蛋白聚糖(proteoglycan)硫酸肝素(heparinsulfate)相互作用,参与表皮细胞的生长、分裂、附着和迁移。众所周知,一般来说,FGF 10的表达使基底膜本身维持正常,并通过基底膜传递信号来促进表皮的生长。
因此,本发明的组合物可以表达FGF 10,促进皮肤基底膜部位中成纤维细胞的增殖,由此强化皮肤基底膜,表现出改善皮肤弹性或皱纹的效果。
因此,本发明的组合物可以同时包含由化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐或由化学式3表示的化合物或其药学上可接受的盐,并且上述组合物与单独包含由化学式1表示的化合物或其药学上可接受的盐、由化学式2表示的化合物或其药学上可接受的盐或由化学式3表示的化合物或其药学上可接受的盐的组合物相比,可以具有更优异的改善皮肤弹性或皱纹的效果。
本发明的组合物可以制备成选自由溶液、外用软膏、霜、泡沫、营养化妆水、柔肤水、面膜、柔软水、乳液、妆前底乳、精华液、皂、洗涤剂、入浴剂、防晒霜、防晒油、悬浮液、乳浊液、膏、凝胶、露、粉、皂、含有表面活性剂的清洁剂、油、粉末粉底、乳浊液粉底、蜡粉底、贴片和喷雾组成的组的剂型,优选地可以是化妆水、精华液、露、霜、面膜、凝胶、粉、粉底或洗涤剂,但不限于此。
在本发明中,化妆料组合物可以进一步包括一种以上的一般皮肤化妆料中配入的化妆学上可接受的载体,作为常规的成分,可以适当地配入例如油分、水、表面活性剂、保湿剂、低级醇、增稠剂、螯合剂、色素、防腐剂、香料等,但不限于此。
当本发明的剂型为粉或喷雾时,作为载体成分,可以利用乳糖、滑石、二氧化硅、氢氧化铝、硅酸钙、聚酰胺粉或它们的混合物,特别是,当为喷雾时,可以附加地包含推进剂,例如氯氟烃、丙烷/丁烷或二甲醚。
当本发明的剂型为溶液或乳浊液时,作为载体成分,利用溶剂、增溶剂、或乳浊剂,例如有水、乙醇、异丙醇、碳酸乙酯、乙酸乙酯、苯甲酸苄酯、丙二醇、1,3-丁基乙二醇油,特别是有棉籽油、花生油、玉米胚芽油、橄榄油、蓖麻油和芝麻油、甘油脂肪族酯、聚乙二醇或脱水山梨醇的脂肪酸酯。
当本发明的剂型为悬浮液时,作为载体成分,可以利用诸如水、乙醇或丙二醇等液体稀释剂、诸如乙氧基化异硬脂醇、聚氧乙烯山梨醇酯和聚氧乙烯脱水山梨醇酯等悬浮剂、微晶纤维素、偏氢氧化铝、膨润土、琼脂或黄蓍胶等。
当本发明的剂型为皂时,作为载体成分,可以利用脂肪酸的碱金属盐、脂肪酸半酯盐、脂肪酸蛋白水解物、羟乙基磺酸盐、羊毛脂衍生物、脂肪醇、植物油、甘油、糖等。
本发明还提供了一种改善皮肤弹性或皱纹的方法,其包括用化妆料组合物处理个体皮肤的步骤,该化妆料组合物包含由以下化学式1表示的化合物或其生理学上可接受的盐;以及由化学式2表示的化合物或其生理学上可接受的盐和/或由化学式3表示的化合物或其生理学上可接受的盐作为有效成分。上述个体包括但不限于包括人、家畜、鼠等在内的哺乳动物。
本发明提供了一种化妆料组合物在制备用于改善皮肤弹性或皱纹的产品中的用途,该化妆料组合物包含由化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐和/或由化学式3表示的化合物或其药学上可接受的盐作为有效成分。
同时,本发明的药学组合物可以单独包含有效成分,除此以外,根据剂型、使用方法和使用目的还可以包含药学上可接受的载体、赋形剂、稀释剂或辅成分。
更具体地,除了上述有效成分之外,还可以进一步含有营养剂、维生素、电解质、风味剂、着色剂、填充剂、果胶酸及其盐、藻酸及其盐、有机酸、保护性胶体增稠剂、pH调节剂、稳定剂、防腐剂、甘油、醇、碳酸饮料中使用的碳酸化剂等。
上述“药学上接受的”是指生理学上接受并且对动物、优选对人给药时通常不会引起胃肠障碍、晕眩症等过敏反应或与此相似的反应。上述药学上有效的量可根据疾病及其重症程度、患者的年龄、体重、健康状况、性别、给药途径或治疗期间等而适当改变。
作为上述药学上接受的载体、赋形剂或稀释剂的实例,可以例举选自由乳糖、葡萄糖(dextrose)、蔗糖、山梨糖醇、甘露糖醇、木糖醇、赤藓糖醇、麦芽糖醇、淀粉、阿拉伯胶、藻酸盐、明胶、磷酸钙、硅酸钙、纤维素、甲基纤维素、微晶纤维素、聚乙烯吡咯烷酮、水、羟基苯甲酸甲酯、羟基苯甲酸丙酯、滑石、硬脂酸镁和矿物油、羟基苯甲酸丙酯、滑石、硬脂酸镁和矿物油、糊精、碳酸钙、糊精、碳酸钙、丙二醇、液体石蜡和生理盐水组成的组的一种以上,但不限于此,并且常规的载体、赋形剂或稀释剂均可使用。
上述成分可以独立或组合添加到本发明的有效成分中。
上述药学组合物的剂型可根据使用方法而变化,并且可以使用本发明所属技术领域中公知的方法来剂型化使得在对哺乳动物给药后可提供活性成分的快速、持续或延缓的释放。作为上述剂型的实例,可以是选自由软膏、霜、片剂、丸剂、散剂、颗粒剂、胶囊剂、悬浮剂、内用液剂、乳剂、糖浆剂、水溶液、非水性溶剂、悬浮剂、乳剂和贴片剂组成的组的剂型。
为了上述剂型,还可以包含赋形剂,作为一个实例,常规的填充剂、增量剂、结合剂、崩解剂、表面活性剂、抗凝聚剂、润滑剂、湿润剂、香料、乳化剂、防腐剂、甜味剂、芳香剂或保存剂等。
一般来说,用于口服给药的固体制剂中包括片剂(TABLETS)、药片、软质或硬质胶囊剂(CAPSULES)、丸剂(PILLS)、散剂(POWDERS)和颗粒剂(GRANULES)等,这些制剂可以混合一种以上的赋形剂例如,淀粉、碳酸钙(calcium carbonate)、蔗糖(sucrose)或乳糖(lactose)、明胶等而调制。另外,除了单纯的赋形剂之外,还可以使用硬脂酸镁、滑石等润滑剂。
另外,用于口服给药的液体制剂中包括悬浮剂(SUSTESIONS)、内用液剂、乳剂(EMULSIONS)和糖浆剂(SYRUPS)等,除了通常使用的单纯稀释剂即水或液体石蜡之外,还可以包括多种赋形剂,例如湿润剂、甜味剂、芳香剂、保存剂等。
作为用于皮肤给药而可提及的实例,有适合生成撒布粉(dusting powder)、乳状液(emulsion)、悬浮液、油、喷雾、软膏、含脂软膏(greasy ointment)、霜膏、凝胶、泡沫、或溶液的剂型和适于经皮药物传递体(TTS:透皮给药系统,Transdermaltherapeuticsystem)的载体和/或赋形剂。本发明的组合物可以是半固体状剂型,特别是,有软膏(溶液软膏、悬浮液软膏)、霜、凝胶或膏。主要用于油相中的有脂肪醇例如月桂醇、鲸蜡醇、硬脂醇,脂肪酸例如棕榈酸或硬脂酸,液状或固体状石蜡或地蜡、液状至固体状蜡例如肉豆蔻酸异丙酯,天然脂肪或部分合成脂肪例如椰子脂肪酸甘油三酯,硬化油例如氢化花生油或蓖麻油,或甘油的脂肪酸部分酯例如甘油单硬脂酸酯或甘油二硬脂酸酯。作为合适的乳化剂,有表面活性剂,例如非离子表面活性剂,例如多元醇或其氧化乙烯加成物的脂肪酸酯例如聚甘油脂肪酸酯或聚氧乙烯脱水山梨醇脂肪酸酯,脱水山梨醇脂肪酸酯例如脱水山梨醇油酸酯或脱水山梨醇异硬脂酸酯等,异硬脂酸酯、甾醇、或聚氧乙烯脂肪醇醚或脂肪酸酯;例如阴离子表面活性剂,例如脂肪醇磺酸酯的碱金属盐例如月桂基硫酸钠(sodiumlauryl sulfate)、鲸蜡基硫酸钠(sodium cetyl sulfate)或硬脂基硫酸钠(sodiumstearyl sulfate),它们通常在上述脂肪醇例如鲸蜡醇或硬脂醇的存在下使用。其中,特别是,可将防止霜干燥的制剂,例如多元醇例如甘油、山梨糖醇、丙二醇或聚乙二醇添加到水相中,或者将保存剂、香料等添加到水相中。
本发明的药学组合物可以是无水状态的软膏,可以含有适合局部用途并在体温状态下为液体的石蜡、特别是低粘度石蜡,或者含有上述天然脂肪或部分合成脂肪例如椰子脂肪酸甘油三酯,硬化油例如氢化花生油或蓖麻油,甘油的脂肪酸部分酯例如甘油单硬脂酸酯和二硬脂酸酯,有机硅例如聚甲基硅氧烷,例如六甲基二硅氧烷或八甲基三硅氧烷,例如可以含有与水性霜有关并增加水分吸收容量的脂肪醇,以及甾醇、羊毛蜡(wool wax)、其他乳化剂和/或其他添加剂。
在本发明中,当将上述药学组合物剂型化成医药品时,可以参考Remington'sPharmaceutical Science,Mack Publishing Company,Easton PA中公开的内容,并且上述文献作为本说明书的一部分包括在内。
本发明还提供了一种改善皮肤弹性或皱纹的方法,其包括将药学组合物给药于个体的步骤,该药学组合物包含由以下化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐和/或由化学式3表示的化合物或其药学上可接受的盐作为有效成分。上述个体包括但不限于包括人、家畜、鼠等在内的哺乳动物。
本发明提供了一种药学组合物在制备用于改善皮肤弹性或皱纹的产品中的用途,该药学组合物包含由化学式1表示的化合物或其药学上可接受的盐;以及由化学式2表示的化合物或其药学上可接受的盐和/或由化学式3表示的化合物或其药学上可接受的盐作为有效成分。
在本发明中,术语“药学组合物”可以用作包括“医药外品”或“医药品”含义的概念。
当本发明的组合物用作皮肤外用剂剂型时,可以进一步含有皮肤科学领域中通常使用的辅助剂,例如脂肪物质、有机溶剂、增溶剂、浓缩剂和胶凝剂、软化剂、抗氧化剂、悬浮液剂、稳定剂、发泡剂(foaming agent)、芳香剂、表面活性剂、水、离子型或非离子型乳化剂、填充剂、金属离子封锁剂和螯合剂、保存剂、维生素、阻断剂、湿润剂、必需油(精油,essential oil)、染料、颜料、亲水性或亲油性活性剂、脂质小囊或皮肤外用剂组合物中通常使用的任意其他成分。另外,上述成分可以以皮肤科学领域中通常使用的量导入。
另外,当本发明的组合物作为外用剂组合物提供时,可以具有软膏、贴片、凝胶、霜或喷雾剂剂型,但不限于此。
本发明的外用剂组合物特别优选地可以用作非口服用制剂,例如,外用剂组合物可以通过将凡士林、硬脂醇等的药学上接受的合适的基剂;聚山梨醇酯、脱水山梨醇倍半油酸酯等的药学上接受的合适的表面活性剂;甘油等的药剂学上接受的合适的保湿剂;药学上接受的合适的溶剂;以及香料、着色剂、稳定剂、粘性剂等均匀地混合的常规的皮肤外用剂组合物的制备方法制备。
同时,当本发明的组合物作为医药外品组合物提供时,包含选自由羟基肉桂酸、乙酸异戊酯和甜菜碱组成的组的一种以上的化合物或其药学上可接受的盐作为有效成分,并且必要时还可以包含药学上可接受的载体、赋形剂或稀释剂。上述药学上可接受的载体、赋形剂或稀释剂没有限制,只要其不损害本发明的效果即可,例如可以包括填充剂、增量剂、粘合剂、湿润剂、崩解剂、表面活性剂、润滑剂、甜味剂、芳香剂、保存剂等。
上述医药外品组合物可以例示消毒清洁剂、淋浴泡沫、软膏液、湿巾、涂层剂等,优选地可以制备成诸如外用软膏、露等的半固体制剂,但不限于此。上述医药外品的制剂化方法、用量、利用方法、构成成分等可以从技术领域公知的常规的技术适当选择。
本发明的术语“医药外品”是指表现出对疾病的治疗、减轻、处置或预防的效果,但对人体产生的作用比医药品轻微的物品。排除根据药事法的用于医药品用途的物品,包括保健福祉部另行规定的分类标准的物品。具体地可以是皮肤外用剂或个人卫生用品,但不限于此。
本发明的化妆料组合物中包含的上述提及的成分各自优选地可以在不超过各国政府规定的《化妆品使用·许可》相关规定中明示的最大使用量的范围内包含在本发明的化妆料组合物中。例如,可符合中国政府规定的《化妆品安全技术规范》中明示的范围。
除非另有说明,否则上述本说明书中记载的数值应解释为包括均等范围。
发明的效果
本发明提供一种同时包含由化学式1表示的化合物;以及由化学式2表示的化合物和/或由化学式3表示的化合物的组合物。上述组合物与单独包含由化学式1表示的化合物、单独包含由化学式2表示的化合物或单独包含由化学式3表示的化合物的组合物相比,具有更优异的改善皮肤弹性或皱纹的效果。
附图说明
图1是在基底膜上照射UV后对处理虫草素和穿心莲内酯的情况与未处理的情况进行比较的图。
具体实施方式
在下文中,通过以下实施例详细说明本发明。但是,以下实施例仅用于例示本发明,本发明的内容不限于以下实施例。
实验例1.FGF10 mRNA表达分析
新生的人真皮成纤维细胞(Human Dermal Fibroblasts,neonatal)购自Lonza,然后在37℃、5%二氧化碳条件下在二氧化碳培养箱中培养。此时,用于培养的培养基利用将10% FBS(胎牛血清,Fetal Bovine Serum)和1%抗生素(Antibiotics)(青霉素链霉素,Penicillin streptomycin)在DMEM(Dulbecco改良Eagle培养基,Dulbecco ModifiedEagle Medium-Thermo Fisher Scientific)中混合而制成的培养基。此后,将20000个细胞植入6孔板(well plate)中,24小时后,用以表1和2中所示的含量包含表1和2的各成分的样品处理DMEM培养液,再进一步培养48小时。此时,作为对照群,使用不添加其他成分的DMEM培养基液。此后,对细胞内RNA进行纯化(purification),合成cDNA,然后利用qPCR方法分析FGF10 mRNA的表达量。表1显示了虫草素和穿心莲内酯单独和一起处理时与对照群相比的表达量。表2显示了虫草素和槲皮素单独和一起处理时与对照群相比的表达量。在现有技术中,腺苷是众所周知的具有改善皮肤皱纹效果的物质,但经确认没有增强FGF 10表达的效果。
[表1]
[表2]
实验例2.利用猪皮肤的基底膜变化分析
新鲜(Live)猪皮肤(屠宰后不冷冻而直接用于实验)购自APURES,然后在37℃、5%二氧化碳条件下在二氧化碳培养箱中利用将10% FBS(胎牛血清,Fetal Bovine Serum)和1%抗生素(Antibiotics)(青霉素链霉素,Penicillin streptomycin)、0.02%四环素(Tetracyclin)在DMEM(Dulbecco改良Eagle培养基,Dulbecco Modified Eagle Medium-Thermo Fisher Scientific)中混合而制成的培养基进行培养。将猪皮肤在6孔悬挂插入物(well hanging insert)(MILLIPORE)中稳定24小时后,利用UV照射装置以1J/cm2的强度照射UVB以诱导基底膜破坏。此时,UV照射采用照射5分钟后休息2小时的方法,共照射3次。UVB照射后立即将包含0.1%虫草素和0.1%穿心莲内酯的样品涂布于猪皮肤表面并处理48小时。然后,取样并用10%福尔马林(formalin)进行固定,然后委托TEGO science进行H&E染色(H&E staining)。实验期间,上午、下午各自交换一次DMEM。实验结果示于图1。在基底膜上照射UV时,基底膜会变得扁平,而当在这里处理虫草素和穿心莲内酯时,可以确认变得扁平的基底膜再次恢复。
实验例3.在人皮肤中的弹性或皱纹改善效果评价
为了评价在人皮肤中基底膜强化效果引起的皮肤改善效果,制备了如下表所示的制备例(单位:重量%)。
[表3]
以32名27-43周岁的女性为对象,每天早晚各一次,即每天共2次,为期4周,在面部部位使用上表3制备例的化妆品,并测量皮肤皱纹状态和皮肤弹性状态。对于测量,在最初使用日前测量1次(A),在为期4周的使用全部结束后再测量1次(B),测量方法如下。在皮肤皱纹测量时,对于由表情引起的残余皱纹(潜在皱纹),利用Antera 3D CS(Miravex,爱尔兰)设备对试验部位(眼角)测量一次,并利用小皱纹(Wrinkle-small)分析模式的深度(depth,mm)作为评价资料。受试者通过做出皱眉的表情来制造人为的眼角皱纹,使表情皱纹维持一分钟后,再次测量表情放松后立即产生的残余皱纹。测量仪器是可以使用发光二极管(LED光源)测量皮肤表面图像的设备,从内置程序的3D形状图像中提取数据,对皮肤状态进行数值化,并利用图像。与产品使用前相比,4周后的皱纹深度(depth,mm)值越减小,意味着由表情引起的残余皱纹(潜在皱纹)越得到改善。对于皮肤弹性测量,利用皮肤扭力计(Dermal torque meter)(Dia-Stron,英国)进行测量,对试验部位(脸颊)测量3次,并利用平均值作为评价资料。对于测量原理,利用3mm护环(Guard ring)与中心盘(central disk)之间的扭转(扭转法,Torsional method)方法进行测量。使用Ur/Ue值作为皮肤内弹性评价指标,并且测量值越增加,意味着皮肤内弹性越得到改善。
测量结果如下计算,计算改善率,并且改善率示于下表4。
[表4]
评价项目 | 改善率(%) |
皱纹改善 | 10.5 |
弹性改善 | 12.2 |
Claims (8)
1.一种用于改善皮肤弹性或皱纹的化妆料组合物,其包含由以下化学式1表示的化合物或其生理学上可接受的盐;以及由以下化学式2表示的化合物或其生理学上可接受的盐和/或由以下化学式3表示的化合物或其生理学上可接受的盐作为有效成分:
[化学式1]
[化学式2]
[化学式3]
2.根据权利要求1所述的用于改善皮肤弹性或皱纹的化妆料组合物,其中,所包含的由上述化学式1表示的化合物或其生理学上可接受的盐的含量为整个组合物中的0.00001重量%至10重量%,
所包含的由上述化学式2表示的化合物或其生理学上可接受的盐和/或由上述化学式3表示的化合物或其生理学上可接受的盐的含量为整个组合物中的0.00001重量%至10重量%。
3.根据权利要求1所述的用于改善皮肤弹性或皱纹的化妆料组合物,其中,包含上述化学式1表示的化合物或其生理学上可接受的盐;以及上述化学式2表示的化合物或其生理学上可接受的盐和/或上述化学式3表示的化合物或其生理学上可接受的盐的100:1至1:100重量比。
4.根据权利要求1所述的用于改善皮肤弹性或皱纹的化妆料组合物,其中,上述组合物具有强化皮肤基底膜的效果。
5.一种用于改善皮肤弹性或皱纹的药学组合物,其包含由以下化学式1表示的化合物或其药学上可接受的盐;以及由以下化学式2表示的化合物或其药学上可接受的盐和/或由以下化学式3表示的化合物或其药学上可接受的盐作为有效成分:
[化学式1]
[化学式2]
[化学式3]
6.根据权利要求5所述的用于改善皮肤弹性或皱纹的药学组合物,其中,所包含的由上述化学式1表示的化合物或其药学上可接受的盐的含量为整个组合物中的0.00001重量%至10重量%,
所包含的由上述化学式2表示的化合物或其药学上可接受的盐和/或由上述化学式3表示的化合物或其药学上可接受的盐的含量为整个组合物中的0.00001重量%至10重量%。
7.根据权利要求5所述的用于改善皮肤弹性或皱纹的药学组合物,其中,包含上述化学式1表示的化合物或其药学上可接受的盐;以及上述化学式2表示的化合物或其药学上可接受的盐和/或上述化学式3表示的化合物或其药学上可接受的盐的100:1至1:100重量比。
8.根据权利要求1所述的用于改善皮肤弹性或皱纹的药学组合物,其中,上述组合物具有强化皮肤基底膜的效果。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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KR10-2021-0072613 | 2021-06-04 | ||
KR20210072613 | 2021-06-04 | ||
PCT/KR2022/007823 WO2022255810A1 (ko) | 2021-06-04 | 2022-06-02 | 항노화 화장료 조성물 |
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CA3221157A1 (en) | 2022-12-08 |
KR20220164443A (ko) | 2022-12-13 |
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