CN117379347A - 火棘提取物的化妆品或皮肤病学用途 - Google Patents
火棘提取物的化妆品或皮肤病学用途 Download PDFInfo
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- CN117379347A CN117379347A CN202210785463.8A CN202210785463A CN117379347A CN 117379347 A CN117379347 A CN 117379347A CN 202210785463 A CN202210785463 A CN 202210785463A CN 117379347 A CN117379347 A CN 117379347A
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- extract
- skin
- use according
- pyracantha fortuneana
- pores
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Abstract
本发明涉及新的化妆品或皮肤病学用途,有利地通过局部途径使用火棘的提取物和/或包含该火棘的提取物的组合物用于预防和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服的表现。
Description
技术领域
本发明涉及火棘(Pyracantha fortuneana)提取物的化妆品或皮肤病学用途,用于预防和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服表现,特别是在化妆品或药物组合物中,特别是在皮肤病学组合物中。
背景技术
皮肤毛孔是皮脂腺和汗腺分泌物流出的开口。它们含有毛囊和皮脂腺。不同的外部因素,如紫外线照射、热、污染,以及卫生条件差或不均衡的饮食,以及更简单的皮肤老化,都会导致毛孔扩张,从而使皮肤变得不那么光滑和难看。毛孔变得粗大可见,由此产生的后果是皮肤难看。此外,如雄激素和生长因子的内在因素会调节皮脂腺和汗腺的活动。
火棘原产于中国,是蔷薇科常绿灌木。火棘果实在传统医学中用作强化剂,以对抗消化和免疫问题(Li等人,Food chemistry 366,2022,综述)。
火棘因其多种生物效应被用于化妆品和药物领域,特别是作为抗炎剂、抗氧化剂或美白剂。
专利CN105362206描述了火棘果实提取物在化妆品组合物中作为抗氧化剂和抗衰老活性成分的用途。
专利申请CN107375095涉及火棘果实提取物在化妆品组合物中作为增白和保湿活性剂的用途。
特别令人惊讶的是,本申请人发现,火棘的提取物具有防止和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服表现的性质,特别是降低皮肤毛孔的可见性,和/或防止皮肤毛孔的可见性增加,和/或保持和/或改善皮肤肤色的均匀性。
根据本发明的提取物作为成分还具有可以容易地配制并且可以容易地以工业规模生产的优点。它是一种局部可接受的皮肤活性成分,不存在过敏风险。
发明内容
本发明的第一个主题是火棘提取物的美容用途,有利地是局部使用,以防止和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服的表现。
术语“美容用途”是指非治疗用途,即不是治疗用途,是应用于身体的所谓健康部位,特别是所述皮肤区域是健康的。
术语“健康的皮肤”或“健康的组织”是指皮肤、组织或表皮的区域,将根据本发明的提取物或包含所述提取物的组合物应用到该区域,其被皮肤科医生称为“非病理性的”,即没有感染、疤痕、疾病或皮肤病症,如念珠菌病、脓疱病、牛皮癣、湿疹、痤疮或皮炎、或疮或损伤。
术语“皮肤”是指身体和/或面部的任何部分,包括头皮。
在本发明的含义内,术语“局部途径”被理解为是指将根据本发明的火棘的提取物或包含它的组合物直接局部应用和/或气化到待处理皮肤的表面。
根据本发明,使用有效量的火棘提取物来预防和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服的表现。
根据本发明的一个优选实施方案,有效量的火棘提取物用于降低皮肤毛孔的可见性,和/或防止皮肤毛孔的可见性增加,和/或维持和/或改善肤色均匀度。
术语“防止和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服的表现”,是指减少皮肤毛孔的可见性和/或黑头的形成,和/或防止皮肤毛孔的可见性增加,和/或维持和/或改善皮肤肤色的均匀性,和/或改善皮肤纹理。
在本发明的含义内,术语“减少毛孔的可见性”是指收紧皮肤的毛孔,即减少皮肤表面的毛孔的数量,和/或减少毛孔开口的直径,和/或减少毛孔面积和/或毛孔的密度,和/或防止皮肤毛孔扩张。因此,根据本发明的提取物可以减少皮肤表面处毛孔的数量和/或开口的直径和/或毛孔的面积和/或密度。
术语“防止皮肤毛孔的可见性增加”是指完全或部分抑制毛孔数量和/或开口直径的增加,特别是皮肤毛孔的扩张,和/或皮肤毛孔面积和/或密度的增加。
皮肤毛孔的扩张可由内在因素如激素变化或在皮脂分泌增加诱导,或外在因素如高温或升高的外界温度、紫外线、污染、化学侵害物或施用改变角化机制的药物。火棘提取物有助于防止皮肤毛孔扩张。
皮肤毛孔的可见性可以通过皮肤科医生在预定区域上施用包含根据本发明的提取物的组合物后的所谓“评分”评估而在体内证明。它也可以通过客观仪器方法对图像分析突出显示,这使得可以提取和量化在志愿者面部施用包含本发明的提取物组合物之前和之后的高分辨率照片的孔隙面积和密度的特定参数。
皮肤毛孔的面积也可以通过成像在体内测量,特别是通过条纹投影技术。
例如,可以使用VISIA-CR评估皮肤毛孔的可见性,通过图像分析(Image-ProPlus)测量毛孔所占面积的比例和脸颊上的毛孔数量(毛孔密度)。与D0的初始值和/或对照相比,这些值的降低表明毛孔的可见性降低。
在本发明的一个优选实施方案中,以有效量施用本发明的火棘提取物用于减少毛孔可见性和/或用于防止皮肤毛孔可见性的增加,当与施用前评估的毛孔可见性相比,在施用根据本发明的提取物56天后观察到减少至少3%,优选至少4%的皮肤毛孔的可见性。优选地,提取物在实施例1、特别是实施例1a)中所述的条件下制备,更优选地配制为例如实施例2中所述的化妆品组合物的形式。
在本发明的含义内,术语“保持和/或改善肤色的均匀性”,是指防止减少和/或增加肤色的均匀性和/或改善皮肤的质地,特别是通过收紧皮肤毛孔,和/或通过减少皮肤表面上毛孔的数量,和/或减小开口直径,和/或减少面积和/或密度,和/或减少皮肤毛孔的扩张,和/或预防和/或减少与皮肤毛孔相关的肤色缺陷,例如与皮肤毛孔相关的黑头、发红、肤色不均或疤痕痕迹,以使肤色更均匀。
皮肤肤色均匀性的测量例如可以通过图像分析来测量。这种体内测量方法包括在应用测试产品之前和之后拍摄高分辨率照片。在这些数码照片的基础上,图像分析可以提取和量化特定于肤色均匀性的参数,例如光密度的变化。例如,可以通过VISIA-CR评估肤色的均匀性,通过图像分析(Image-Pro Plus)测量脸颊上光密度(OD)的变化。OD的方差越小,肤色越均匀。因此,该参数的降低表明肤色更均匀。
在本发明的优选实施方案中,以有效量施用本发明的火棘提取物用于保持和/或改善肤色的均匀性,当与使用前评估的肤色均匀性相比,在使用本发明的提取物56天后,观察到肤色均匀性至少提高10%,优选地至少提高15%。优选地在实施例中所述的条件下制备提取物,尤其是实施例1(a),优选制备实施例2所述的化妆品组合物的形式。
火棘提取物可以是植物的任何部分,例如根和/或地上部分,包括叶子、花、果实、茎或它们的混合物。有利地,火棘提取物是果实提取物。
可以通过本领域技术人员已知的任何提取方法获得根据本发明的提取物,所述提取方法选自热煎剂、浸渍法、挤压法、亚临界提取法、超声辅助提取法,可以研磨或不研磨,例如超声研磨或使用搅拌机。有利地,提取物通过搅拌浸渍获得。
“亚临界”萃取是指在温度大于100℃、压力小于或等于22.1MPa(221bar)的条件下,在水存在下进行的萃取,使水保持液态,但其粘度和表面张力低于室温下的水,从而增加其介电常数。
萃取可以以干燥或新鲜的植物材料作为原料,有利地是干燥的,量为1%至99%(按重量计),有利地是1%至50%(按重量计),非常有利地是1%至20%(按重量计),优选植物材料相对于植物材料和萃取溶剂总重量计为5%至10%。
提取可以在4℃至300℃的温度范围内进行,包括环境温度,即18℃至25℃之间的温度,特别是20℃左右。在本发明的一个优选实施方案中,提取在20℃至150℃,优选20℃至80℃的温度范围内进行。
提取时间可以为几秒至24小时,优选1分钟至12小时,更优选10分钟至5小时,更优选1小时至3小时,特别优选2小时。
根据需要,提取可以在与第一次提取相同或不同的条件下重复多次,优选在与第一次提取相同的条件下重复提取一次。
溶剂可以选自水、溶剂或溶剂混合物,优选溶剂是质子极性溶剂。优选水、醇、二醇、多元醇、99/1至1/99(w/w)的水/醇、水/二醇或水/多元醇混合物(例如水与乙醇、甘油和/或丁二醇和/或其他二醇(例如木糖醇和/或丙二醇等)的混合物),优选水/醇混合物,更优选水/乙醇混合物。
根据一个实施方案,水/醇、水/二醇或水/多元醇,特别是水/醇的混合物为20/80至60/40,有利地为20/80至50/50(w/w)。
根据一个实施方案,水/乙醇混合物在20/80和60/40之间,有利地在20/80和50/50(w/w)之间。
根据另一个实施方案,提取通过在水/乙醇混合物中浸溃来进行,优选在20℃和80℃之间的温度下,有利地进行2小时,优选重复提取一次。
特别地,提取物是通过水醇提取获得的。在本发明的含义内,术语“通过水醇提取获得的提取物”是指通过用乙醇溶液提取获得的任何提取物,该乙醇溶液含有超过40重量%、有利地至少50重量%、特别是至少60重量%相对于溶液总重量的重量百分比的乙醇,甚至更有利地不包含任何二醇和/或多元醇。
根据优选方式,单独使用火棘提取物,特别是以活性成分的形式。根据本发明的所述提取物可以是干燥形式,即粉末形式。
根据另一种优选方式,火棘提取物是活性成分的干燥形式,即粉末形式,有利地与麦芽糖糊精组合,相对于总粉末重量(包括提取物和麦芽糊精),优选地提取物含量为1%至99%(w/w),更优选地提取物含量为1%至50%(w/w),优选地为1%至25%(w/w),更优选地5%至15%(w/w)。
在优选的替代方案中,根据本发明的火棘提取物可以是液态和/或在溶剂中稀释,以包括提取物和溶剂的液体总重量计,优选提取物含量为0.1%至99%(w/w),更优选提取物含量为0.1%至50%(w/w),有利地,提取物含量为0.1%至20%(w/w),更有利地,提取物含量为1%至10%(w/w)。优选地,该溶剂的水含量小于50%(w/w),优选小于40%(w/w)。非常优选,该溶剂为甘油水溶液或乙醇水溶液。
根据本发明的火棘提取物可以以活性成分的形式单独使用,和/或用于化妆品和/或药物中,特别是用于皮肤病学组合物中。
术语“化妆品组合物”是指非治疗性组合物,也就是说,它不用于治疗用途,而是应用于身体的所谓健康部位,特别是健康皮肤区域。
根据一个实施方案,根据本发明的提取物和/或含有该提取物的组合物的使用特征在于,它是局部使用的,特别是用于选自小腿、脚、腋窝、手、腹部、手臂、大腿、臀部外侧、臀部、腰部、胯部、腹股沟、躯干、背部、颈部、乳沟的身体特定部位,头皮和/或面部皮肤,包括前额、脸颊、鼻子、太阳穴、T字区(前额、鼻子和下巴)、外耳道和/或下巴。
在一个有利的实施方案中,火棘提取物是化妆品组合物的形式,所述化妆品组合物包含相对于所述组合物总重量浓度为1×10-4%和10%(w/w)之间,优选1×10-3%和10%(w/w)之间的所述提取物,有利地在1×10-3%和3%(w/w)之间,更优选在0.01%和3%(w/w)之间,甚至更优选在0.01%和1%(w/w)之间,所述组合物还包含至少一种化妆品可接受的赋形剂。
优选地,根据本发明的化妆品组合物包含一种或多种化妆品活性成分,例如用于敏感皮肤的活性成分、改善皮肤屏障的活性成分、改善皮肤舒适度的活性成分、抗发红活性成分、抗刺激活性成分、美白活性成分、改善皮肤光泽的活性成分、针对油性皮肤的活性成分、改善皮肤去角质的活性成分、保湿活性成分、抗衰老活性成分、抗自由基活性成分、成纤维细胞生长因子(FGF)保护剂、刺激成纤维细胞活性和/或增殖的活性剂和/或温泉水。
本发明的主题是一种护理和/或美容处理方法,包括在至少一个皮肤区域上局部或口服应用根据本发明的火棘提取物或包含该火棘提取物的化妆品组合物,用于预防和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服的表现,特别是用于降低皮肤毛孔的可见性和/或防止皮肤毛孔的可见性增加和/或保持和/或改善肤色的均匀度。
有利地,本发明的火棘提取物,优选以根据本发明的化妆品组合物的形式,用于定期局部应用,并且优选每天应用至少一次,有利地每天应用两次,至少应用28天,优选应用36天,更优选至少45天,更优选至少56天。
用于防止和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服的表现,特别是用于减少皮肤毛孔的可见性和/或防止皮肤毛孔的可见性增加和/或维持和/或改善肤色的均匀性的根据本发明的美容护理方法有利地包括以下步骤:
-对个人健康皮肤区域的识别,希望防止和/或减少该区域皮肤毛孔的难看和/或不愉快和/或不舒服的表现,特别是降低皮肤毛孔的可见性和/或防止皮肤毛孔的可见性增加和/或维持和/或改善肤色的均匀性,
-将有效量的根据本发明的火棘提取物以活性成分形式,单独使用或与麦芽糊精联合使用,或在溶剂或溶剂混合物中稀释,或将含有该提取物的化妆品组合物局部应用于该健康皮肤区域。
在另一个实施方案中,本发明的提取物可以掺入化妆品组合物中。
有利地,根据本发明的火棘提取物或包含它的组合物旨在局部应用于选自小腿、脚、腋窝、手、腹部、手臂、大腿、臀部外侧、臀部、腰部、胯部、腹股沟、躯干、背部、颈部、乳沟的身体特定部位、头皮和/或面部皮肤,包括前额、脸颊、鼻子、太阳穴、T字区(前额、鼻子和下巴)、外耳道和/或下巴。
有利地,该提取物和/或含有该提取物的组合物的目的在于将其应用于具有不期望的毛孔可见度的健康组织区域,例如寻求至少降低3%,优选至少降低4%的毛孔可见度的区域,和/或应用于具有不均匀肤色的健康组织区域,例如至少改善10%的区域,优选至少15%。
因此,有利地,化妆品组合物旨在局部施用于健康皮肤。
或者,根据本发明的火棘提取物可以是任何常规用于局部应用的盖伦制剂形式。
根据一个实施方案,在根据本发明的美容护理方法中,火棘提取物为包含所述提取物的化妆品组合物的形式,相对于组合物的总重量,所述提取物的浓度在1×10-4%和10%(w/w)之间,优选在1×10-3%和10%(w/w)之间,有利地在1×10-3%和3%(w/w)之间,更优选地在0.01%和3%(w/w)之间,甚至更优选地在0.01%和1%(w/w)之间,所述组合物还包含至少一种化妆品可接受的赋形剂。
在本发明中,“化妆品可接受”的赋形剂是指一种局部可接受的化合物和/或溶剂,即适用于局部应用的成分,对健康皮肤无毒、无刺激性,不会引起过敏反应,具有化学稳定性。
美容护理过程是使用根据本发明的火棘提取物。
本发明的主题还涉及火棘的提取物或包含该火棘的提取物的皮肤病学组合物,其局部使用,用于治疗和/或预防和/或减少与粉刺出现相关的病症如痤疮的发生。
特别地,所述提取物是根据本发明的提取物,更具体地如本说明书上文所述和/或定义的。
根据一个实施方案,根据本发明的提取物的特征在于它是包含至少一种皮肤病学上可接受的赋形剂的皮肤病学组合物的形式。
根据一个实施方案,根据本发明的提取物不用于敏感皮肤、发炎皮肤和/或易患特应性皮炎的皮肤。
根据一个实施方案,该组合物的特征在于,相对于该组合物的总重量,火棘提取物在所述组合物中的含量在1×10-4%到10%(w/w)之间、优选地在1×10-3%到10%(w/w)之间、优选地在1×10-3%到3%(w/w)之间、更优选地在0.01%到1%(w/w)之间。
优选地,根据本发明的化妆品或皮肤病学组合物包含一种或多种化妆品(或皮肤病学)活性成分,例如保湿活性剂、抗衰老活性剂、抗自由基活性剂、成纤维细胞生长因子(FGF)保护剂,刺激成纤维细胞活性和/或增殖的活性剂和/或温泉水。
根据本发明的化妆品或皮肤病学组合物可以选自水性或油性溶液、乳膏或水性凝胶或油性凝胶,特别是沐浴露、洗发水;奶液;乳液、微乳液或纳米乳液,特别是水包油或油包水或多相或硅化型的;面膜;精华液;化妆水;液体肥皂;皮肤用条;软膏;香膏;黄油;摩丝;贴剂;无水产品,优选液体、糊状或固体,例如化妆粉、棒或棒的形式,特别是口红的形式。
它也可以是彩妆产品或卸妆产品。
根据本发明的组合物可以包含任何合适的溶剂和/或任何合适的载体和/或任何合适的赋形剂,任选地与其他目标化合物组合。
因此,对于这些组合物,赋形剂包含例如至少一种选自下列的化合物:防腐剂、润肤剂、乳化剂、表面活性剂、保湿剂、增稠剂、调理剂、消光剂、稳定剂、抗氧化剂、质地剂、光泽剂、成膜剂、增溶剂、颜料、染料、香料和防晒剂。这些赋形剂优选选自氨基酸及其衍生物、聚甘油、酯、聚合物和纤维素衍生物、羊毛脂衍生物、磷脂、乳铁蛋白、乳过氧化物酶、基于蔗糖的稳定剂、维生素E及其衍生物、天然和合成蜡、植物油、甘油三酯、不皂化物、植物甾醇、植物酯、有机硅及其衍生物、蛋白质水解物、荷荷巴油及其衍生物、脂/水溶性酯、甜菜碱、氧化胺类、植物提取物、蔗糖酯、二氧化钛、甘氨酸和对羟基苯甲酸酯,还优选选自丁二醇、硬脂醇聚醚-2、硬脂醇聚醚-21、乙二醇-15硬脂醚、鲸蜡硬脂醇、苯氧乙醇、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、丁二醇、天然生育酚、甘油、二羟基十六烷基磷酸钠、异丙基羟基十六烷基醚、硬脂酸乙二醇酯、三异壬酸甘油酯、椰油酸辛酯、聚丙烯酰胺、异链烷烃、月桂醇聚醚-7、卡波姆、丙二醇、甘油、红没药醇、聚二甲基硅氧烷、氢氧化钠、PEG 30-二聚羟基硬脂酸酯、癸酸/辛酸甘油三酯、辛酸鲸蜡硬脂酯、己二酸二丁酯、葡萄籽油、荷荷巴油、硫酸镁、EDTA、环甲硅油、黄原胶、柠檬酸、十二烷基硫酸钠、蜡和矿物油、异硬脂酸异硬脂酸酯、丙二醇二壬酸酯、丙二醇异硬脂酸酯、PEG 8、蜂蜡、氢化棕榈心油甘油酯、氢化棕榈油甘油酯、羊毛脂油、芝麻油、乳酸鲸蜡酯、羊毛脂醇、蓖麻油、二氧化钛、乳糖、蔗糖、低密度聚乙烯、等渗盐水溶液及其混合物。
本领域技术人员已知许多美容活性成分可改善皮肤(包括头皮)的健康和/或物理外观。本领域技术人员知道如何配制化妆品和/或皮肤病学组合物以获得最佳效果。另一方面,这些化合物在相互结合时可以产生协同作用。本发明也涵盖这些组合。化妆品活性成分手册(第二版)(CTFA Cosmetic Ingredient Handbook,Second Edition(1992))描述了化妆品和制药行业常用的各种化妆品和药物成分,特别是适合局部使用的那些。这些成分类别的实例包括但不限于以下化合物:研磨剂、吸收剂、用于美学目的的化合物,例如香料、颜料、染料、精油、收敛剂等(例如:丁香油、薄荷醇、樟脑、桉树油、丁香酚、乳酸薄荷酯、金缕梅馏分)、抗痤疮剂、抗絮凝剂、消泡剂、抗微生物剂(例如:丁基氨基甲酸碘丙酯)、抗氧化剂、粘合剂、生物添加剂、缓冲剂、溶胀剂、螯合剂、添加剂、杀生物剂、变性剂、增稠剂和维生素,及其衍生物或等价物、成膜材料、聚合物、遮光剂、pH调节剂、还原剂、脱色剂或美白剂(例如:对苯二酚、曲酸、抗坏血酸、抗坏血酸磷酸镁、抗坏血酸葡糖胺)、调理剂(例如保湿剂)。
化妆品或皮肤科组合物还可包括具有相同性质并与根据本发明的火棘提取物产生协同或不产生协同效应的其他化妆品和/或皮肤科药物,或具有互补效应的化妆品。
例如,这些可以是降低毛孔的可见性和/或改善肤色均匀性的成分,例如红木(Bixa orellana)种子的提取物。
它也可以是活性抗衰老成分,例如由BASF Beauty Care Solutions以NephoriaTM名称销售的红毛丹(Nephelium lappaceum)叶提取物,或由BASF Beauty Care Solutions以Lox-AgeTM名称销售的菊苣(Cichorium intybus)提取物,和/或紧致剂和/或保湿活性成分,例如由BASF Beauty Care Solutions以名称NephydratTM销售的红毛丹树皮提取物,和/或增加表皮屏障作用的活性剂,例如由BASF Beauty Care Solutions以名称OligolinTM销售的水解亚麻籽提取物。
可用于本发明的紧缩剂可选自合成聚合物,例如聚氨酯胶乳或丙烯酸胶乳,天然来源的聚合物,特别是淀粉形式或角叉菜胶、藻酸酯、琼脂、结冷胶、纤维素聚合物和果胶形式的多糖;植物蛋白和蛋白水解物;混合硅酸盐;蜡微粒;选自例如二氧化硅、二氧化硅-氧化铝复合材料的无机填料的胶体颗粒;以及它们的混合物。
最后,它们还可以是化妆品成分,例如抗微生物剂,抗自由基剂,舒缓剂,镇静剂或放松剂,作用于微循环以改善肤色、特别是面部光泽的活性剂,愈合剂或减肥剂。有利地,本发明的化妆品和/或皮肤病学组合物还包含一种或多种紧缩剂和/或一种或多种抗微生物剂和/或一种或多种抗自由基剂和/或一种或多种舒缓剂和/或一种或多种减肥剂和/或一种或多种对微循环有活性的活性剂。
在本发明的优选方案中,对于与火棘提取物结合使用的抗微生物剂,可提及2,4,4′-三氯-2′-羟基二苯醚(或三氯生)、3,4,4′-三氯苯胺、苯氧乙醇、苯氧丙醇、苯氧异丙醇、己脒羟乙基磺酸盐、甲硝唑及其盐、咪康唑及其盐、伊曲康唑、特康唑、益康唑、酮康唑、沙康唑、氟康唑、克霉唑、布康唑、奥昔康唑、磺胺康唑、舒康唑、特比萘芬、十一碳烯酸及其盐、过氧化苯甲酰、3-羟基苯甲酸、4-羟基苯甲酸、植酸、N-乙酰基-L-半胱氨酸、硫辛酸、壬二酸及其盐、花生四烯酸、间苯二酚、辛氧基甘油、辛酰甘氨酸、辛基乙二醇、10-羟基-2-癸酸、法呢醇、植物鞘氨醇及其混合物。
抗自由基剂可以是维生素C及其衍生物,包括抗坏血酸葡糖苷、酚类和多酚类,特别是单宁、鞣花酸和单宁酸;表没食子儿茶素和含有它的天然提取物,特别是绿茶提取物;花青素;酚酸,芪;捕获单环或多环芳族化合物的活性剂、鞣酸如鞣花酸和吲哚衍生物和/或捕获重金属如EDTA的活性剂、抗自由基活性剂如维生素E及其衍生物如生育酚乙酸酯;生物类黄酮;辅酶Q10或泛醌。
作为可在本发明组合物中使用的舒缓剂,可提及五环三萜、熊果酸及其盐、齐墩果酸及其盐、桦木酸及其盐、水杨酸盐,特别是水杨酸锌、红没药醇、尿囊素、ω-3不饱和油、可的松、氢化可的松、吲哚美辛和培他米松、抗炎活性剂,特别是专利申请FR2847267中描述的那些,特别是申请人以InhipaseTM的名称销售的葛根(Pueraria lobata)提取物、可可树(Theobroma cacao)的提取物。
作用于微循环的活性成分、血管保护剂或血管扩张剂可以选自类黄酮、鲁斯可皂苷元(ruscogénines)、烟酸盐、精油。
减肥活性剂可以特别选自脂蛋白脂肪酶的抑制剂,例如专利US2003086949(Coletica)中描述的那些,特别是秘鲁藤(Uncaria tomentosa)的提取物;引流活性剂,特别是月桂酸橙皮素(FlavagrumTM)或辛酸槲皮素(FlavengerTM);磷酸二酯酶抑制剂、腺苷酸环化酶cAMP活化剂、和/或能够捕获精胺和/或亚精胺的活性剂。可以提及毛喉鞘蕊花(Coleus Forskohlii)根提取物、Cecropia obtusa提取物、Uva lactuca、咖啡因、毛喉素、茶碱、可可碱和/或它们的衍生物、申请人销售的称为SlimexcessTM的水解κ角叉菜胶产品和/或其混合物。
在本发明的含义内,术语“皮肤病学组合物”是指旨在治疗和/或预防与粉刺如痤疮的出现有关的皮肤病症的组合物。
有利地,本发明还涉及用于治疗和/或预防与粉刺如痤疮的出现有关的皮肤病症的药物组合物,特别是皮肤病学组合物。
通过阅读以下实施例将更好地理解本发明。
下面给出参考本发明描述的实施例。这些实施例是为了说明而给出的,决不限制本发明的范围。每个实施例的范围都是一般性的。
实施例构成本发明的组成部分,并且从整体的描述(包括实施例)来看,相对于现有技术出现的任何新特征,包括实施例,均构成本发明的组成部分。
另一方面,在实施例中,除非另有说明,否则所有百分比均以重量计,除非另有说明,否则温度以摄氏度表示,且压力为大气压,除非另有说明。
实施例
实施例1a:根据本发明的火棘提取物(含有麦芽糖糊精的粉末)的制备
将火棘的干果在35/65(w/w)水/乙醇混合物中提取,然后过滤以获得澄清液体,然后将其加载到离子交换柱上。用乙醇进行洗脱,然后将洗脱液在真空蒸发器中浓缩。获得的液体提取物与麦芽糖糊精以10%的干提取物与90%的麦芽糖糊精的比例(重量/重量%)混合。然后将整体冷冻干燥以获得粉红色至棕色粉末。所得产物的特征在于含水量≤8.0%(重量/重量),且槲皮素糖苷含量在0.5%至1.5%之间(重量/重量%,通过HPLC测定)。
实施例1b:根据本发明的火棘提取物(不含助剂的粗粉)的制备
将火棘的干果在35/65(w/w)水/乙醇混合物中提取,然后过滤以获得澄清液体,然后将其加载到离子交换柱上。用乙醇进行洗脱,然后将洗脱液在真空蒸发器中浓缩。然后将所得液体冷冻干燥以获得粉红色至深棕色粉末。所得产物的特征是含水量≤8.0%(w/w),且槲皮素糖苷含量在5%至15%(w/w%,通过HPLC测定)之间。
实施例Ic:与二醇混合的本发明的火棘提取物(液体)的制备
将火棘的干果在35/65(w/w)水/乙醇混合物中提取,然后过滤以获得澄清液体,然后将其加载到离子交换柱上。用乙醇进行洗脱,然后将洗脱液在真空蒸发器中浓缩。然后将该提取物在60℃搅拌下溶解在80/20(重量/重量)的丙二醇/水混合物中,获得澄清液体。这种液体的特征是从果实中提取的干物质为5%(%w/w),且槲皮素糖苷的含量在0.25%和0.75%之间(w/w%,由HPLC测定)。
实施例1d:与甘油混合的本发明的火棘提取物(液体)的制备
将火棘的干果在35/65(w/w)水/乙醇混合物中提取,然后过滤以获得澄清液体,然后将其加载到离子交换柱上。用乙醇进行洗脱,然后将洗脱液在真空蒸发器中浓缩。然后将该提取物在80℃搅拌下溶解在80/20(重量/重量)的甘油/水混合物中,获得液体。所述液体的特征在于从果实中提取的干物质为5%(%重量/重量)且槲皮素糖苷含量为0.25%至0.75%之间(重量/重量%,通过HPLC测定)。
实施例2:包含根据本发明的火棘提取物的化妆品组合物的实施例
根据本领域技术人员已知的方法,将下表1中所示的各相A、B、C混合在一起以制备根据本发明的组合物。比例以%表示,大写字母的名称对应于成分的INCI名称。
表1:用于实施例3的临床试验的组合物
实施例3:减少毛孔的可见性和改善肤色的均匀性
用包含根据实施例1a)的提取物的实施例2)的活性组合物和用没有根据本发明的提取物的实施例2)的对照组合物进行双盲、半脸临床研究。
包含或不包含火棘提取物的组合物的功效通过比较处理前的皮肤(D0,初始值)与用包含火棘提取物的组合物(活性组合物)或不包含火棘的提取物的组合物(对照组合物)处理后的皮肤来评估。该研究进行了56天,检查点在D56。
这项研究是在30名年龄在40至50岁之间的亚洲志愿女性中进行的。志愿者每天涂抹两次(正常使用条件-早上一次,晚上一次),每种组合物分别涂抹在半张脸上。
使用VISIA-CR评估效果,通过图像分析(Image-Pro Plus)测量毛孔所占面积的比例和脸颊上毛孔的数量(毛孔密度)。与D0初始值和/或对照值相比,这些值的降低表明毛孔的可见性降低。
通过VISIA-CR评估肤色的均匀性,通过图像分析(Image-Pro Plus)测量脸颊上光密度(OD)的方差。OD的方差越小,肤色越均匀和一致。因此,该参数的降低表明肤色更均匀。
结果表示为相对于D0初始值的变化百分比。
在使用Shapiro-Wilk检验验证分布的正态性、通过配对的学生t-检验验证分布的正态性或通过Wilcoxon检验验证分布的正态性失效后,对这些参数随时间的函数以及随测试组合物的函数的变化进行统计分析检验。
显著性阈值设定为5%(p<0.05)。
表2:脸颊毛孔比例和毛孔数量的百分(%)变化
表2中的结果表明,将含有根据实施例1a)获得的火棘提取物的根据实施例2的活性组合物施用于脸颊,减少了毛孔占据的面积:
-与治疗前毛孔占据的面积相比,处理56天后差异性显著(p<0.001),
-与不含火棘提取物的根据实施例2的对照组合物相比,处理56天后差异性显著(p<0.05)。
表2中的结果表明,将含有根据实施例1a)获得的火棘提取物的根据实施例2的活性组合物施用于脸颊,减少了毛孔的数量:
-与治疗前的毛孔数量相比,治疗56天后差异性显著(p<0.001),
-与不含火棘提取物的根据实施例2的对照组合物相比,56天后差异性显著(p<0.001)。
表3:脸颊上光密度方差的变化百分比
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表3中的结果表明,将含有根据实施例1a)获得的火棘提取物的根据实施例2的活性组合物施用于脸颊,降低了光密度的方差:
-与治疗前获得的光密度方差相比,处理56天后差异性显著(p<0.001),
-与不含火棘提取物的根据实施例2对照组合物相比,处理56天后差异性显著(p<0.001)。这些结果表明根据本发明的提取物改善了肤色的均匀性。
Claims (17)
1.火棘提取物在制备用于预防和/或减少皮肤毛孔的难看和/或不愉快和/或不舒服表现的化妆品组合物中的用途。
2.根据权利要求1的用途,用于降低皮肤毛孔的可见性和/或防止皮肤毛孔的可见性增加和/或保持和/或改善皮肤肤色的均匀性。
3.根据权利要求1或2所述的用途,用于减少皮肤表面上的毛孔的数量和/或开口直径和/或毛孔的面积和/或密度和/或防止皮肤毛孔的扩张。
4.根据权利要求1或2的用途,其特征在于它是局部使用的。
5.根据权利要求1或2的用途,其特征在于所述火棘的提取物是地上部分的提取物。
6.根据权利要求1或2的用途,其特征在于所述火棘提取物是果实提取物。
7.根据权利要求1或2的用途,其特征在于所述火棘提取物是通过在质子极性溶剂中提取而获得的。
8.根据权利要求1或2的用途,其特征在于所述火棘提取物是通过在水/醇混合物中提取而获得的。
9.根据权利要求1或2的用途,其特征在于所述火棘提取物是通过在水/乙醇混合物中提取而获得的。
10.根据权利要求1或2的用途,其特征在于所述火棘提取物是干燥形式的活性成分的形式。
11.根据权利要求1或2的用途,其特征在于所述火棘提取物是与麦芽糖糊精组合的干燥形式的活性成分的形式。
12.根据权利要求1或2所述的用途,其特征在于所述化妆品组合物包含相对于所述组合物的总重量在1×10-4%和10%(w/w)之间的浓度的所述提取物,所述组合物至少还包含化妆品可接受的赋形剂。
13.根据权利要求1或2所述的用途,其特征在于,所述化妆品组合物还包含一种或多种化妆品活性成分,例如用于敏感皮肤的活性成分、改善皮肤屏障的活性成分、改善皮肤舒适度的活性成分、抗红肿活性成分、抗刺激活性剂、美白活性剂、改善皮肤光泽的活性剂、油性皮肤活性剂、改善皮肤去角质的活性剂、保湿活性剂、抗衰老剂、抗自由基活性成分和/或温泉水。
14.根据权利要求1或2的用途,其特征在于它是在选自小腿、脚、腋窝、手、颈部、肩部、腹部、手臂、大腿、臀部外侧、臀部、腰部、胯部、腹股沟、躯干、背部、面部和/或头皮的特定部位局部使用的。
15.根据权利要求1或2所述的用途,其中所述化妆品组合物每天至少一次以常规局部应用的形式使用,持续至少45天。
16.火棘提取物用于制备皮肤病学组合物的用途,该皮肤病学组合物用于局部使用以治疗和/或预防和/或减少与粉刺如痤疮的出现相关的病症的发生。
17.根据权利要求16所述的用途,其特征在于,所述火棘提取物如权利要求1至15中任一项所定义。
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CN202210785463.8A CN117379347A (zh) | 2022-07-04 | 2022-07-04 | 火棘提取物的化妆品或皮肤病学用途 |
PCT/EP2023/068237 WO2024008647A1 (fr) | 2022-07-04 | 2023-07-03 | Utilisation cosmétique ou dermatologique d'un extrait de pyracantha fortuneana |
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