CN115105423B - 具有抗炎抗敏活性的组合物及其应用 - Google Patents
具有抗炎抗敏活性的组合物及其应用 Download PDFInfo
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- CN115105423B CN115105423B CN202210842014.2A CN202210842014A CN115105423B CN 115105423 B CN115105423 B CN 115105423B CN 202210842014 A CN202210842014 A CN 202210842014A CN 115105423 B CN115105423 B CN 115105423B
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Abstract
本申请公开了一种具有抗炎抗敏活性的组合物及其应用。本申请中,所述组合物包括:丝氨酸(PuriCerine)和甘油磷酸肌醇胆碱盐(PuriGPI),本申请提供的组合物,具有显著的抗炎抗敏感活性,和更低的副作用。
Description
技术领域
本发明涉及生物化学领域,特别涉及具有抗炎抗敏活性的组合物及其应用。
背景技术
皮肤敏感是多种因素诱发的主观感觉症状的皮肤状态,对刺激的耐受性降低。当受到外界刺激时,会释放炎性介质,引起红斑、肿胀以及刺痛等现象。当前化妆品市场名目繁多,刺激类产品不在少数,同时社会习惯以及生活环境可能会因其皮肤刺激,导致发炎和过敏等问题。现有技术中,治疗皮肤炎症和过敏的产品存在吸收差、抗炎抗敏效果不佳、含有激素副作用明显等问题,例如倍他米松和地塞米松活性虽然抗炎效果好,但是激素引起的副作用明显,容易产生耐药性。此外部分产品中含有的草药提取物成分还可能造成炎症和敏感的进一步加重,阻碍皮肤自身免疫调节。因此,本领域尚需开发一种有效组织皮肤过敏及炎症,迅速消红、止痒、止痛的产品。
发明内容
本发明的目的在于提供一种具有抗炎抗敏活性的组合物及其应用。
为解决上述技术问题,本发明的第一方面,提供了一种具有抗炎抗敏活性的组合物,所述组合物包括:
丝氨酸(PuriCerine)和
甘油磷酸肌醇胆碱盐(PuriGPI)。
在一些优选的方案中,所述丝氨酸和所述甘油磷酸肌醇胆碱盐的质量百分比为2:(2.5-3.5)。
本发明的第二方面,提供了一种化妆品,所述化妆品包括本发明第一方面所述组合物,和化妆品中可接受的辅料。
在一些优选的方案中,相对于所述化妆品的总质量,所述组合物的质量比为0.1至99%。
在一些优选的方案中,所述化妆品可接受的辅料包括抗氧化剂、防腐剂、保湿剂和表面活性剂。
在一些优选的方案中,所述化妆品选自以下任一种形式:化妆水、乳液、化妆霜、精华、面膜、膏状凝胶、喷雾、香皂、洗面奶、沐浴露、洗发露、护发素、粉底、粉霜、身体乳或按摩膏。
本发明的第三方面,提供了一种药物组合物,所述药物组合物包括本发明第一方面所述组合物,和药学上可接受的载体。
本发明的第四方面,提供了本发明第一方面所述组合物或本发明第三方面所述药物组合物的用途,包括:
(i)治疗银屑病;
(ii)治疗红疹;
(iii)制备治疗银屑病的药物;
(iv)制备治疗红疹的药物;
(v)提升前胶原表达水平;和/或
(vi)抑制MMP表达水平。
本发明的第五方面,提供了一种使皮肤抗炎和/或抗敏的方法,所述方法包括步骤:
向受试者施用本发明第一方面所述组合物;或
向受试者施用本发明第二方面所述化妆品;或
向受试者施用本发明第三方面所述药物组合物。
在一些优选的方案中,所述方法为非治疗目的的。
在一些优选的方案中,所述皮肤为人的皮肤、实验动物的皮肤或实验室培养的皮肤组织。
本发明的第六方面,提供了一种提高皮肤透明质酸吸收水平的方法,所述方法包括步骤:
将透明质酸和本发明第一方面所述组合物联合施用于皮肤。
在一些优选的方案中,所述方法为非治疗目的的。
在一些优选的方案中,所述皮肤为人的皮肤、实验动物的皮肤或实验室培养的皮肤组织。
本发明相对于现有技术而言,至少具有下述优点:
(1)本发明提供的组合物,具有显著的抗炎抗敏感活性,和更低的副作用;
(2)本发明提供的组合物,可应用于消炎抗敏、去红血丝、消除红疹、治疗银屑病、抗老去皱、保湿补水、抗蓝光、抗颗粒物污染;
(3)本发明提供的组合物,制备获得的产品吸收好、稳定性高、生物利用度高;
(4)本发明提供的组合物,与透明质酸联用可促进其吸收。
应理解,在本发明范围内中,本发明的上述各技术特征和在下文(如实施例)中具体描述的各技术特征之间都可以互相组合,从而构成新的或优选的技术方案。限于篇幅,在此不再一一累述。
附图说明
一个或多个实施例通过与之对应的附图中的图片进行示例性说明,这些示例性说明并不构成对实施例的限定。
图1是根据本发明实施例中施用不同产品皮肤局部祛红血丝效果示意图;
图2是根据本发明实施例中施用不同产品皮肤红疹消除效果示意图;
图3是根据本发明实施例中银屑病患者施用不同产品发红率统计图;
图4是根据本发明实施例中银屑病患者施用不同产品发痒率统计图;
图5是根据本发明实施例中组合物对紫外线诱导前胶原和MMP的表达量影响示意图;
图6是根据本发明实施例中组合物对紫外线诱导前胶原和MMP的转录水平影响示意图;
图7是根据本发明实施例中施用不同产品对皮肤透明质酸含量影响示意图;
图8是根据本发明实施例中施用不同产品对皮肤角质层含水量影响示意图;
图9是根据本发明实施例中蓝光照射下施用不同产品对细胞内ROS的水平的影响示意图;
图10是根据本发明实施例中颗粒物环境下施用不同产品对细胞内ROS的水平的影响示意图;
图11是根据本发明实施例中组合物对透明质酸渗透率的影响示意图;
图12是根据本发明实施例中皮肤明场组织呈像图。
具体实施方式
皮肤敏感是多种因素诱发的主观感觉症状的皮肤状态,对刺激的耐受性降低。当受到外界刺激时,会释放炎性介质,引起红斑、肿胀以及刺痛等现象。皮肤反复性炎症和敏感一直十分棘手难治的皮肤问题。现有技术中效果较好的倍他米松和地塞米松活性中含有激素,容易产生副作用,而其他的产品抗炎抗敏感效果并不明显或者起效时间十分长,过程中伴随着皮肤蜕皮、脱水等诸多问题。本发明人经过广泛而深入的研究,开发了一种安全有效的具有抗炎抗敏活性的组合物,所述组合物包括:丝氨酸(PuriCerine)和甘油磷酸肌醇胆碱盐(PuriGPI)。本发明的组合物,以天然生物活性物质为原料,副作用低,且两种组分混合产生出乎意料的协同作用,大幅提升抗炎和抗敏活性。
组合物
本发明中具有抗炎抗敏活性的组合物包括丝氨酸(DL-Serine,CAS号:302-84-1;可使用商品名如PuriCerine的市售产品)和甘油磷酸肌醇胆碱盐(Glycerophosphoinositol choline,CAS号:425642-32-6;可使用商品名如PuriGPI的市售产品)。二者可以以任一种比例相互混合,前述混合可以是互溶或不互溶的形式。但优选地,所述组合物中,所述甘油磷酸肌醇胆碱盐的量大于所述丝氨酸的量;更优选地,所述丝氨酸和所述甘油磷酸肌醇胆碱盐的质量百分比为2:(2.5-3.5),例如2:3。
丝氨酸和甘油磷酸肌醇胆碱盐作为活性成分可以溶解于任一种可溶介质(溶剂)中构成本发明的组合物。在本发明的一些实施方式中,所述组合物包括丝氨酸、甘油磷酸肌醇胆碱盐和水。丝氨酸和甘油磷酸肌醇胆碱盐在组合物中的含量不做特别限制,但优选地,所述组合物中,所述丝氨酸的质量百分含量优选为1至50%;和/或,所述组合物中,所述甘油磷酸肌醇胆碱盐的质量百分含量为1至50%。
化妆品和使用方法
本发明中,化妆品包括上述的组合物,和化妆品中可接受的辅料。
在一些优选的方案中,所述化妆品中可接受的辅料选自溶剂、增溶剂、防腐剂、抗氧化剂、pH调节剂、促渗剂、脂质体、保湿剂、增稠剂、螯合剂、肤感调节剂、表面活性剂、乳化剂、推进/抛射剂、香精、色素,以及其他功效添加剂。例如本发明的一个实施例中,所述化妆品中可接受的辅料为抗氧化剂、防腐剂、保湿剂、表面活性剂和抗炎剂。
在一些优选的方案中,所述化妆品选自以下任一种形式:化妆水、乳液、化妆霜、精华、面膜、膏状凝胶、喷雾、香皂、洗面奶、沐浴露、洗发露、护发素、粉底、粉霜、身体乳或按摩膏。
在一些优选的方案中,相对于所述化妆品的总质量,所述组合物的质量百分含量为0.1至99%;优选为1至90%;更优选为1至90%;更优选为1至80%;更优选为1至70%;更优选为1至60%;更优选为1至50%;更优选为1至30%;更优选为1至15%;更优选为1至10%;更优选为1至9%;更优选为1至7%;更优选为1至6%;更优选为1至5%,例如:2%、3%、4%或5%。本发明中特别优选地,所述组合物的质量百分含量为1至5%。
作为防腐剂,非限制地可以选自对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、对羟基苯甲酸丁酯、苯甲酸酯、山梨酸、三氯生、三氯卡班等)、金属螯合剂。剂(如EDTA、NTA等)、蛋白水解酶、防腐剂(zincpyrythion、octropix等)、渗透促进剂(苯甲醇、苄氧基乙醇等)、增稠剂(羧乙烯基聚合物等)可含有羧甲基纤维素、聚乙烯醇、角叉菜胶、水溶性聚合物如明胶)、电解质、pH调节剂(缓冲剂如乳酸-乳酸钠和柠檬酸-柠檬酸钠)。
防腐剂在本发明的化妆品中的添加量优选为0.01~50重量%(以下简称为%),特别优选为0.5~20%。
作为抗氧化剂,非限制地可以选自乙酰半胱氨酸、抗坏血酸、抗坏血酸多肽、二棕榈酸抗坏血酸酯、甲基硅烷醇果胶酯酸抗坏血酸酯、棕榈酸抗坏血酸酯、硬脂酸抗坏血酸酯、BHA、BHT、叔丁基氢醌、半胱氨酸、盐酸半胱氨酸、二戊基氢醌、二叔丁基氢醌、硫代二丙酸二鲸蜡酯、二油基生育酚甲基硅烷醇、硫酸抗坏血酸二钠、硫代二丙酸二硬脂酰酯、硫代二丙酸二(十三)酯、棓酸十二烷基酯、异抗坏血酸、抗坏血酸酯类、阿魏酸乙酯、阿魏酸、棓酸酯类、氢醌、巯基醋酸异辛酯、曲酸、抗坏血酸镁、抗坏血酸磷酸镁、抗坏血酸甲基硅烷醇酯;天然植物性药材抗氧化剂,诸如绿茶或葡萄子提取物、去甲二氢愈创木酸、棓酸辛酯、苯基硫代巯基乙酸、抗坏血酸生育酚磷酸钾、亚硫酸钾、棓酸丙酯、醌类、迷迭香酸、抗坏血酸钠、硫酸氢钠、异抗坏血酸钠、焦亚硫酸钠、亚硫酸钠、超氧化物歧化酶、硫代巯基乙酸钠、山梨醇糠醛、硫二甘醇、硫二甘醇酰胺、亚硫基二乙酸、亚硫基乙酸、硫羟乳酸、硫代水杨酸、tocophereth-5、tocophereth-10、tocophereth-12、tocophereth-18、tocophereth-50、生育酚、tocophersolan、乙酸生育酚酯、亚油酸生育酚酯、烟酸生育酚酯、琥珀酸生育酚酯和三(壬基苯基)亚磷酸盐中的至少一种。
抗氧化剂在本发明的化妆品中的添加量优选为0.01~50重量%(以下简称为%),特别优选为0.5~20%。
作为保湿剂,非限制地可以选自甘油、神经酰胺或其类似结构物质、胆固醇酯、山梨糖醇、木糖醇、甘油、martitol、丙二醇、1,3-丁二醇等其实例包括1,4-丁二醇、吡咯烷酮羧酸钠、乳酸、乳酸钠、聚氧丙烯脂肪酸酯、聚乙二醇中的至少一种。本发明中特别优选地,保湿剂为甘油和丙二醇。
保湿剂在本发明的化妆品中的添加量优选为0.01~50重量%(以下简称为%),特别优选为0.5~20%。
作为抗炎剂,非限制地可以选自水杨酸甲酯、水杨酸乙二醇酯、消炎痛、布洛芬、尿囊素、氯化溶菌酶、愈创木灵、γ-香豆素、醋酸生育酚、甘草酸、甘草酸二钾、甘草次酸及其盐。这些可以单独使用或两种以上组合使用。本发明中特别优选地,所述抗炎剂为甘草酸二钾。
抗炎剂在本发明的化妆品中的添加量优选为0.001~5%,特别优选为0.1~2%。
作为表面活性剂,非限制地可以是辛酸/癸酸甘油三酯、棕榈酸异辛酯、聚二甲基硅氧烷、鲸蜡硬脂基葡糖苷/鲸蜡硬脂醇、甘油硬脂酸酯/PEG-100硬脂酸酯、聚丙烯酸13/聚异丁烯/聚山梨酸酯-20等,本发明中特别优选地,所述表面活性剂为辛酸/癸酸甘油三酯、棕榈酸异辛酯、聚二甲基硅氧烷、鲸蜡硬脂基葡糖苷/鲸蜡硬脂醇、甘油硬脂酸酯/PEG-100硬脂酸酯、聚丙烯酸13/聚异丁烯/聚山梨酸酯-20的组合。
表面活性剂在本发明的化妆品中的添加量优选为1~50%,特别优选为10~30%。
本发明中所用的术语“化妆品”是指以涂抹、喷洒或者其他类似方法,散布于人体表面的任何部位,如皮肤、毛发、指趾甲、唇齿等,以达到清洁、保养、美容、修饰和改变外观,或者修正人体气味,保持良好状态为目的的化学工业品或精细化工产品。根据本发明的优选实施方式中,所述化妆品包括:保湿化妆品、具有保湿功效的抗炎症化妆品,以及具有保湿功效的抗衰老或美白化妆品。
应将化妆品定期地局部施用在任何需要使用获得所需结果必不可少的频率和用量治疗的皮肤面积上。优选将所述的化妆品每天至少施用一次、最优选每天施用两次。治疗的频率取决于皮肤损害或恶化的程度、使用者皮肤的反应性、活性组分在化妆品中的浓度、用于将活性组分转运入角质层的载体的有效性、通过与衣服的物理性接触而除去该制品或通过出汗或其它内部或外部液体而除去该制品的便利性以及对使用者类型的便利性。以所述化妆品的总重为基准,诸如本文所述的化妆品这样相对简单的生化活性物质的典型浓度可以在约0.01%-约5.0%(重量)的范围,且应将该制品以等于约1.0mg/cm2皮肤-约20.0mg/cm2皮肤的比例施用于皮肤。以所述化妆品组合物的总重为基准,优选该配方应含有约0.39%-约0.78%。最优选该配方应含有约0.78%的活性组分且以约5.0mg/cm2皮肤的比例将其施用于皮肤。
本发明中化妆品的作用,包括但不限于:消炎抗敏、去红血丝、抗老去皱、保湿补水、抗蓝光、抗颗粒物污染。
药物组合物
本发明中,药物组合物包括上述的组合物,和药学上可接受的载体。
作为药学上可接受的载体,非限制地可选自乳糖、葡萄糖、蔗糖、山梨糖醇、甘露醇、淀粉、rubber arable、磷酸钾、arginate、明胶、硅酸钾、微晶体纤维素、聚乙烯吡咯烷酮、纤维素、水、糖浆、甲基纤维素、甲基羟基苯甲酸酯、丙基羟基苯甲酸酯、滑石、硬脂酸镁和矿物油。根据本发明的药物组合物可以进一步包括润滑剂、润湿剂、甜味剂、调味剂、乳化剂、悬浮剂和防腐剂中至少一种。合适的药物学上可接受的载体和制剂的详细内容可以在Remington’s Pharmaceutical Sciences(第19版,1995)中找到。
本发明的药物组合物可以与如上所述的药物学上可接受的载体和/或介质一起配制,最终提供单位剂型和多剂量形式的几种形式。制剂的非限制性实例包括但不限于口服制剂,如粉末、颗粒、片剂、胶囊、悬浮液、乳液、糖浆和气雾剂,外用制剂,如膏剂和霜剂、栓剂和无菌注射液,优选为外用膏基、霜基、凝胶、液态涂覆剂。
适应症
本发明中,组合物和药物组合物的用途包括:
(i)治疗银屑病;
(ii)治疗红疹;
(iii)制备治疗银屑病相关药物;
(iv)制备治疗红疹相关药物;
(v)提升前胶原表达水平;和/或
(vi)抑制MMP表达水平。
治疗方法
本发明中的“组合物”或“药物组合物”的施用对象为哺乳动物,包括但不限于,灵长动物(例如,人)、牛、绵羊、山羊、马、狗、猫、兔、大鼠、小鼠等。在特定的实施方式中,该对象为人。
为适应施用对象的特点和治疗的需求,本发明中的“组合物”或“药物组合物”优选被制成药剂的形式施用;给药途径优选为非肠道给药,例如为外敷、涂抹、皮下注射;给药的方式优选局部施用。
本发明中对施用对象施用安全有效量的“组合物”或“药物组合物”,这里的安全有效量是指20至2000mg/kg,优选为50至1000mg/kg,更优选为100至800mg/kg;例如:100mg/kg、150mg/kg、200mg/kg、250mg/kg、300mg/kg、350mg/kg、400mg/kg、450mg/kg、500mg/kg、550mg/kg、600mg/kg、650mg/kg、700mg/kg、750mg/kg或800mg/kg,前述安全有效量均为活性成分的含量。在一些实施例中,所述的安全有效量为50-200mg/kg(小鼠),或500-1000mg/kg(人)。
当治疗银屑病时,本发明中“组合物”或“药物组合物”施用频率为每日1至3次,例如早或晚1次、早晚各一次共2次或早中晚各一次共3次;持续施用不少于1天,优选为不少于10天,优选不少于20天,优选不少于30天,最优选不少于60天。
当治疗红疹时,本发明中“组合物”或“药物组合物”施用频率为每日1至3次,例如早或晚1次、早晚各一次共2次或早中晚各一次共3次;持续施用不少于1天,优选为不少于3天,优选不少于5天,优选不少于7天,最优选不少于7天。
为使本发明实施例的目的、技术方案和优点更加清楚,下面结合具体实施例,进一步阐述本发明。应理解,这些实施例仅用于说明本发明而不用于限制本发明的范围。下列实施例中未注明具体条件的实验方法,通常按照常规条件,或按照制造厂商所建议的条件。除非另外说明,否则百分比和份数是重量百分比和重量份数。以下实施例中所用的实验材料和试剂如无特别说明均可从市售渠道获得。
除非另有指明,本文所用的技术和科学术语具有与本申请所属技术领域的普通技术人员通常理解的相同含义,需要注意的是,本文所用的术语仅为了描述具体实施方式,而非意图限制本申请的示例性实施方式。
实施例1、组合物的制备
将丝氨酸2g、甘油磷酸肌醇胆碱盐3g和水75g混合,即得到组合物。
实施例2、含有组合物的护肤制剂的制备
以每100g由下述组分制成:GTCC辛酸/癸酸甘油三酯5g、棕榈酸异辛酯3g、聚二甲基硅氧烷(粘度100型号)1g、丝氨酸2g、甘油磷酸肌醇胆碱盐3g、Montanov 68(鲸蜡硬脂基葡糖苷/鲸蜡硬脂醇)2g、Simusol 165(甘油硬脂酸酯/PEG-100硬脂酸酯)1g、甘草酸二钾0.1g、丙二醇3g、甘油3g、SEPIPLUS 400(聚丙烯酸13/聚异丁烯/聚山梨酸酯-20)1g、防腐剂1g、水74.9g。
对比例1、丝氨酸的水溶液
使用丝氨酸5g和水75g混合。
对比例2、甘油磷酸肌醇胆碱盐的水溶液
使用甘油磷酸肌醇胆碱盐5g和水75g混合。
实施例3、祛红血丝效果测试
取志愿者面部一块红血丝较为严重的区域,等分为四个部分,分别记为1、2、3、4。每个区域分别不施加任何产品、对比例1制备的丝氨酸水溶液、对比例2制备的甘油磷酸肌醇胆碱盐水溶液和施加实施例1制备的组合物,作用7天后拍照记录,结果见图1。
图1中,A对应1,为不施加组合物7天后的对照组;B对应2,为施加对比例1作用7天后;C对应3,为施加对比例2作用7天后;D对应4,为施加实施例1作用7天后。
由图1可知,相比不施用任何产品,施加丝氨酸水溶液或者甘油磷酸肌醇胆碱盐水溶液均在一定程度上减轻了红血丝的严重程度;施加丝氨酸和甘油磷酸肌醇胆碱盐的组合物,祛红血丝效果十分显著,7天后几乎看不见红血丝。
实施例4、消除红疹效果测试
取志愿者面部一块红疹较为严重的区域,等分为四个部分,分别记为1、2、3、4。每个区域分别不施加任何产品、每日一次施加对比例1制备的丝氨酸水溶液、每日一次施加对比例2制备的甘油磷酸肌醇胆碱盐水溶液和每日一次施加施加实施例1制备的组合物,作用7天后拍照记录,结果见图2。
图2中,A对应1,为不施加组合物7天后的对照组;B对应2,为施加对比例1作用7天后;C对应3,为施加对比例2作用7天后;D对应4,为施加实施例1作用7天后。
由图2可知,相比不施用任何产品,施加丝氨酸水溶液或者甘油磷酸肌醇胆碱盐水溶液对红疹几乎没有效果,而施加丝氨酸和甘油磷酸肌醇胆碱盐的组合物,7天后红疹症状显著减轻。
实施例5、银屑病治疗效果测试
银屑病是一种慢性炎症皮肤病,临床表现以红斑、瘙痒、鳞屑为主。本实施例以皮肤发红、发痒作为银屑病严重程度的指标,选取20名患有银屑病患者作为志愿者分成四组,其皮肤发红发痒的严重程度接近,前三组病患分别每日在患病区域涂抹一次实施例1的组合物、对比例1的丝氨酸水溶液或者对比例2的甘油磷酸肌醇胆碱盐水溶液,对照组不进行涂抹,持续60天,在第0、7、15、30、60天记录他们的发红率、发痒率。取平均值的方式计算数据并以折线图形式呈现,结果见图3和图4。
由图3和图4可知,相比不施加任何产品,施加丝氨酸水溶液或者甘油磷酸肌醇胆碱盐水溶液一定程度上减轻银屑病患者皮肤发红和瘙痒症状;施用丝氨酸和甘油磷酸肌醇胆碱盐的组合物,可以显著提升银屑病的治疗效果,使皮肤发红率和发痒率同时大幅降低,施用60天后发痒率指标接近于0%。
实施例6、抗衰老测试
衰老过程中,特征性的表现为前胶原表达降低和基质金属蛋白酶(MMP)的增加。MMP是由表皮角质形成细胞和真皮成纤维细胞分泌的一组基质降解酶。胶原蛋白的变化被认为是皱纹形成的原因。
本实施例中验证了实施例1组合物相比安慰剂可以显著降低抑制基质金属蛋白酶(MMP)的增加,并且可以促进前胶原的表达。
取60岁志愿者的角质细胞进行培养,将培养的角质细胞分别放两个培养皿,分别施加VE和施加实施例1制备的组合物,后紫外线持续照射4小时后,测定前胶原和MMP的表达量。结果见图5。图5中PS组施用实施例1的组合物;VE组施用维生素E。
由图5可知,相比VE对照组,施加实施例1组合物显着刺激前胶原启动子活性并抑制紫外线诱导的MMP-1启动子活化。
通过进一步测定细胞中前胶原和MMP的mRNA表达,见过见图6。结果表明实施例1制备的组合物预处理可提升紫外线诱导的前胶原转录水平和抑制MMP-1表达。
实施例7、保湿补水效果测试
本实施例中,皮肤的持水能力以皮肤透明质酸含量和角质层含水量为评判指标。选取志愿者面部一块区域,等分为四个部分,四个部分分别不施加任何产品、施加对比例1制备的丝氨酸水溶液、对比例2制备的甘油磷酸肌醇胆碱盐水溶液和施加实施例1制备的组合物。在第15、30、60、120分钟时测定含水量,并在120分钟后测定皮肤透明质酸含量,结果见图7和图8。
由图7和图8可知,相比不施用任何产品或仅施用单一的丝氨酸水溶液或甘油磷酸肌醇胆碱盐水溶液,施用了实施例1的组合物可显著增加皮肤透明质酸含量和角质层含水量。
实施例8、抗蓝光效果测试
蓝光会激活色素细胞,增加活性氧的产生。此外,线粒体受到蓝光的破坏,造成氧化应激和功能障碍,导致皮肤衰老。本实施例在蓝光照射下进行,将培养的角质细胞分别放入四个培养皿,分别不施加任何产品、施加对比例1制备的丝氨酸水溶液、对比例2制备的甘油磷酸肌醇胆碱盐水溶液和施加实施例1制备的组合物,持续照射4小时后,测定该区域内细胞ROS水平,结果见图9。
由图9可知,相比不施用任何产品或仅施用单一的丝氨酸水溶液或甘油磷酸肌醇胆碱盐水溶液,施用了实施例1的组合物降低细胞内ROS的水平,说明实施例1的组合物抗蓝光效果显著。
实施例9、抗颗粒物污染效果测试
颗粒物(PM2.5)等空气污染物会诱导皮肤细胞产生活性氧,是导致皮肤问题的外部环境因素之一。流行病学研究表明,色素斑点和皱纹在空气污染物水平较高地区的人中很常见。本实施例在充满颗粒物环境下进行,将培养的角质细胞分别放入四个培养皿,分别不施加任何产品、施加对比例1制备的丝氨酸水溶液、对比例2制备的甘油磷酸肌醇胆碱盐水溶液和施加实施例1制备的组合物,持续放置4小时后,测定该区域内细胞ROS水平,结果见图10。
由图10可知,相比不施用任何产品或仅施用单一的丝氨酸水溶液或甘油磷酸肌醇胆碱盐水溶液,施用了实施例1的组合物降低细胞内ROS的水平,说明在颗粒物环境中,实施例1的组合物能够抑制皮肤细胞内的ROS的产生,延缓皮肤衰老。
实施例10、透明质酸渗透效果测试
本实施例中验证了实施例1组合物与透明质酸共用可协同促进提升透明质酸在人体皮肤的渗透率。选取志愿者面部一块区域,等分为两个部分,第一区域仅施加透明质酸,第二区域施加等量的透明质酸并且施加实施例1的组合物,并在120分钟后测定皮肤透明质酸含量,结果见图11。120分钟后两个区域的皮肤明场组织呈像图见图12,左边为第一区域,右边为第二区域。
由图11和12可知,实施例1的组合物显著促进皮肤透明质酸的吸收,可与透明质酸协同使用提升皮肤的含水量。
本领域的普通技术人员可以理解,上述各实施方式是实现本发明的具体实施例,而在实际应用中,可以在形式上和细节上对其作各种改变,而不偏离本发明的精神和范围。
Claims (7)
1.一种具有抗炎抗敏活性的组合物,其特征在于,所述组合物由:
丝氨酸和甘油磷酸肌醇胆碱盐组成;
其中,所述丝氨酸和所述甘油磷酸肌醇胆碱盐的质量百分比为2:(2.5-3.5)。
2.一种化妆品,其特征在于,所述化妆品包括权利要求1所述的组合物,和化妆品中可接受的辅料。
3.根据权利要求2所述的化妆品,其特征在于,相对于所述化妆品的总质量,所述组合物的质量百分含量为0.1至99%。
4.根据权利要求2所述的化妆品,其特征在于,所述化妆品可接受的辅料包括抗氧化剂、防腐剂、保湿剂和表面活性剂。
5.根据权利要求2所述的化妆品,其特征在于,所述化妆品选自以下任一种形式:化妆水、乳液、化妆霜、精华、面膜、膏状凝胶、喷雾、香皂、洗面奶、沐浴露、洗发露、护发素、粉底、粉霜、身体乳或按摩膏。
6.一种药物组合物,其特征在于,所述药物组合物包括权利要求1所述的组合物,和药学上可接受的载体。
7.权利要求1所述的组合物的用途,其特征在于,用于:
(i)制备治疗银屑病的外用制剂;
(ii)制备治疗红疹的外用制剂。
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