CN116744892A - 包含脂质肽和蔗糖酯的组合物 - Google Patents
包含脂质肽和蔗糖酯的组合物 Download PDFInfo
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- CN116744892A CN116744892A CN202180074098.3A CN202180074098A CN116744892A CN 116744892 A CN116744892 A CN 116744892A CN 202180074098 A CN202180074098 A CN 202180074098A CN 116744892 A CN116744892 A CN 116744892A
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Abstract
本发明的课题是提供通过在皮肤上、毛发表面进行膜形成来防止污染物质的附着,防止由该物质引起的皮肤和毛发表面污染,并且可以促进皮肤渗透的新组合物。解决手段是一种组合物,其特征在于,含有脂质肽型化合物和蔗糖酯,上述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
Description
技术领域
本发明涉及包含脂质肽和蔗糖酯的组合物,详细而言,涉及通过在皮肤或毛发的表面进行膜形成,从而防止尘埃、花粉、粒子状物质等的附着,并且可以促进皮肤渗透的组合物。
背景技术
近年来,对花粉等变应原、PM2.5等微小粒子状物质等有害物质的关心提高,为了防止它们被人体摄入,以口罩为代表而开发出各种制品。
作为这样的制品之一,提出了通过喷雾等而谋求防止有害物质向身体、衣服等的附着的制品。有例如含有包含具有特定的两性离子基、阴离子基的单体单元作为结构单元的聚合物的花粉吸附防止剂(专利文献1)、含有羟基烷基脱乙酰壳多糖的有害物质附着防止剂(专利文献2)等提案。
另一方面,在化妆料、整发料的领域中,形成在皮肤上、毛发表面的被膜由于在皮肤上、毛发表面带来有效的阻挡,因此抑制皮肤、毛发中的水分的蒸发,或提高经皮吸收、向毛发内部渗透的有效成分的保持力等,在个人护理制品中,发挥各种重要的作用。
例如,作为表现高保湿效果的皮肤护理制剂,可举出利用了层状α-凝胶的物质等,采用自组装化结构的被膜化妆料(专利文献3)。
此外,为了减轻由刷梳、采用吹风机等的热处理引起的毛发损伤,提出了利用了多肽的毛发制剂(专利文献4和专利文献5)。
现有技术文献
专利文献
专利文献1:日本专利第4562585号公报
专利文献2:日本专利第6198799号公报
专利文献3:日本特开2016-6030号公报
专利文献4:日本特开平10-77210号公报
专利文献5:日本特开2002-308756号公报
发明内容
发明所要解决的课题
迄今为止,没有关于通过使用了多肽的凝胶状物质来防止尘埃、花粉、粒子状物质等向毛发、皮肤的表面的附着的材料的报导。
本发明的目的是提供通过在皮肤上、毛发表面进行膜形成来防止污染物质的附着,防止由该物质引起的皮肤和毛发表面的污染,并且可以促进皮肤渗透的新组合物。
用于解决课题的手段
本发明人等发现含有至少1种脂质肽型化合物和蔗糖酯的组合物通过在皮肤上、毛发表面进行膜形成从而防止污染物质的附着,并且促进皮肤渗透,从而完成了本发明。
即本发明中,作为第1观点,涉及一种组合物,其含有脂质肽型化合物和蔗糖酯,上述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
作为第2观点,涉及第1观点所述的组合物,其能够在皮肤或毛发的表面形成被膜。
作为第3观点,涉及第1观点或第2观点所述的组合物,其防止尘埃、花粉、粒子状物质、螨(包含尸体)、气态物质、或臭气物质向皮肤或毛发的表面附着。
作为第4观点,涉及第1观点~第3观点中任一项所述的组合物,其特征在于,上述脂质肽型化合物由下述式(1)~式(3)所示的化合物或其可药用的盐之中的至少一种构成。
(式中,R1表示碳原子数9~23的脂肪族基,R2表示氢原子、或可具有碳原子数1或2的支链的碳原子数1~4的烷基,R3表示-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基。)
(式中,R4表示碳原子数9~23的脂肪族基,R5~R7各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基。)
(式中,R8表示碳原子数9~23的脂肪族基,R9~R12各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基。)
作为第5观点,涉及一种防止皮肤表面或毛发表面污染的方法,其包含下述工序:在皮肤表面或毛发表面形成由组合物形成的膜的膜形成工序,上述组合物含有脂质肽型化合物和蔗糖酯,上述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
作为第6观点,涉及第5观点所述的方法,其特征在于,上述脂质肽型化合物由上述式(1)~式(3)所示的化合物或其可药用的盐之中的至少一种构成。
作为第7观点,涉及一种防止尘埃、花粉、粒子状物质、螨(包含尸体)、气态物质、或臭气物质向皮肤表面或毛发表面附着的方法,其包含下述工序:在皮肤表面或毛发表面形成由组合物形成的膜的膜形成工序,上述组合物含有脂质肽型化合物和蔗糖酯,上述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
作为第8观点,涉及第7观点所述的方法,其特征在于,上述脂质肽型化合物由上述式(1)~式(3)所示的化合物或其可药用的盐之中的至少一种构成。
作为第9观点,涉及一种皮肤渗透促进用组合物,其含有脂质肽型化合物和蔗糖酯,上述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
作为第10观点,涉及一种促进皮肤渗透的方法,其包含下述工序:在皮肤表面或毛发表面形成由组合物形成的膜的膜形成工序,上述组合物含有脂质肽型化合物和蔗糖酯,上述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
作为第11观点,第2观点~第4观点中任一项所述的组合物,上述被膜的表面具有平均表面粗糙度为3nm~500nm的粗糙度。
发明的效果
根据本发明,通过含有特定的脂质肽型化合物和蔗糖酯的组合物在皮肤或毛发的表面进行膜形成,从而可以防止尘埃、花粉、粒子状物质等的附着,防止由这些物质引起的皮肤或毛发的污染。
此外根据本发明,可以通过上述组合物来防止尘埃、花粉、粒子状物质等的附着,因此可以抑制这些物质可能引起的皮肤刺激等,避免炎症/氧化/皮肤老化这样的问题。
进一步根据本发明,由于可以防止花粉、PM2.5等微小粒子状物质的附着,因此可以预防由于将它们在附着于皮肤、毛发的状态下移动等而可能发生的污染物质向房屋等的带入、这些物质的吸入等,可以期待抑制由这些物质引起的变态反应症状等的发生。
进而根据本发明,可以防止烟草的烟、臭气物质等令人不适的气味向皮肤、毛发的表面的附着。
此外本发明的组合物所使用的脂质肽型化合物为仅由脂质和肽构成的安全性非常高的人工低分子化合物。当然,蔗糖酯也对于生物体而言是稳定性高的物质。因此,本发明的材料的生物体安全性高,从在药品、化妆品用途中要求的高安全性的观点来看,在上述用途中是非常有用的。此外与以往提出的防止花粉等的吸附/附着的制品相比,在本发明中利用由含有低分子的脂质肽型化合物和蔗糖酯的组合物构成的膜,因此在通过涂布于皮肤、毛发等进行膜形成时,可以促进皮肤渗透而使使用感良好。
附图说明
图1为将附着在涂布了实施例24、27和比较例3的水分散液的サプラーレ的PM2.5粒子通过显微镜VHX-2000进行观察而获得的图像。
图2为显示将附着在涂布了实施例22~27和比较例3的水分散液的サプラーレ的PM2.5粒子通过显微镜VHX-2000进行观察而获得的图像中的PM2.5粒子的面积率的图。
图3为将附着在涂布了实施例22~27和比较例3的溶液的サプラーレ的花粉使用ITEA雪松花粉变应原(Cryj1)ELISA试剂盒进行了定量的结果的图。
图4为在实施例22、24、比较例3中附着了的雪松花粉的通过扫描型电子显微镜进行观察而获得的图像。
图5为显示实施例29~34和比较例3的从三维培养表皮模型提取出的皮肤提取液的烟酰胺量的图。
图6为显示实施例29~34和比较例3的从储存器中检测到的烟酰胺量的图。
图7为显示实施例39~42和比较例3的从三维培养表皮模型提取出的皮肤提取液中检测到的、烟酰胺量的图。
图8为显示实施例39~42和比较例3的从储存器中检测到的烟酰胺量的图。
图9为在比较例4、比较例5、实施例43和实施例44中,观察了附着了的花粉的照片。
图10为在比较例4、实施例43和实施例44中,将附着在人造皮革サプラーレ的花粉使用ITEA雪松花粉变应原(Cryj1)ELISA试剂盒进行了定量的结果的图。
图11为在比较例4、比较例5、实施例43和实施例44中,观察了附着了的PM2.5粒子的照片。
图12为显示在比较例4、和实施例44中,附着在人造皮革サプラーレ的PM2.5粒子所包含的金属元素的量的图。
图13为在比较例4、和实施例44中,为了将PM2.5粒子喷雾于人造皮革サプラーレ而使用了的装置的照片。
图14为显示在比较例4、和实施例44中,附着在人造皮革サプラーレ的PM2.5粒子所包含的硅的量的图。
图15为显示在比较例5、和实施例44中,使组合物进行了喷雾后干燥的情况下的、附着在人造皮革サプラーレ的PM2.5粒子所包含的金属元素的量的图。
图16为在将实施例44的溶液进行了喷雾器喷雾的人造皮革サプラーレ表面所形成的膜的通过扫描型电子显微镜进行观察而获得的图像。
图17为显示在将比较例5、和实施例44的溶液添加于人造皮革サプラーレ使其干燥时附着了的粉尘螨所包含的Derf1进行了定量的结果的图。
图18为显示在将比较例5、和实施例44的溶液添加于人造皮革サプラーレ使其干燥时附着了的粉尘螨的观察结果的照片。
图19为显示将比较例5、和实施例44的溶液添加于硅晶片使其干燥,使用原子力显微镜(AFM)测定了膜表面的不平度的结果的图。
图20为显示比较例6、和实施例45的从三维培养表皮模型提取出的皮肤提取液中检测到的、视黄醇量的图。
图21为显示比较例7、和实施例46的从三维培养表皮模型提取出的皮肤提取液中检测到的、抗坏血酸糖苷量的图。
图22为在比较例8、实施例47和实施例48中,观察了附着了的戈壁黄沙的照片。
图23为显示在比较例8、实施例47和实施例48中,附着在人造皮革サプラーレ的戈壁黄沙所包含的金属元素的量的图。
图24为显示实施例49~52和比较例9的从储存器中检测到的烟酰胺量的图。
图25为显示实施例53和比较例10的从储存器中检测到的烟酰胺量的图。
图26为在比较例11和实施例54中,观察了附着了的PM2.5粒子的照片。
具体实施方式
本发明涉及含有特定的脂质肽型化合物和蔗糖酯的组合物。
本发明的组合物可以在皮肤或毛发的表面形成膜,由此,发挥可以防止以尘埃等为代表的污染物质向皮肤表面和毛发表面的附着,防止由这些物质引起的污染的效果(防污染效果),并且发挥可以促进皮肤渗透的效果。
作为防止向皮肤表面、毛发表面附着/污染的对象物质,以尘埃、花粉为代表,可以举出排气气体、工厂排烟等大气污染物质、烟草的烟等中能够包含的粒子状物质(PM10、悬浮粒子状物质(SPM)、PM2.5(微小粒子状物质等))、气态物质(SOx、CO等)、臭气物质、进一步屋尘、真菌等变应原、螨(包含尸体)、流行性感冒病毒等病毒等。
以下,对各构成成分进行说明。
[组合物]
〔脂质肽型化合物〕
作为在本发明的组合物中使用的、在碳原子数10~24的包含脂肪族基的脂质部(作为脂质部整体的碳原子数为10~24)结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部的脂质肽型化合物,可以使用例如下述式(1)~式(3)所示的化合物(脂质肽)或其可药用的盐(具有作为疏水性部位的脂质部和作为亲水性部位的肽部的低分子化合物)。
在上述式(1)中,R1表示碳原子数9~23的脂肪族基,优选地,期望R1为可具有0~2个不饱和键的碳原子数11~23的直链状脂肪族基。
作为由R1和相邻的羰基构成的脂质部(酰基)的具体例,可举出月桂酰基、十二烷基羰基、肉豆蔻酰基、十四烷基羰基、棕榈酰基、十七烷酰基、油酰基、反油酰基、亚油酰基、硬脂酰基、十八碳烯酰基、十八烷基羰基、花生四烯酰(arachidoyl)基、二十烷基羰基、山萮酰基、芥酰基、二十二烷基羰基、木蜡酰基、神经酰基等,作为特别优选的例子,可举出月桂酰基、肉豆蔻酰基、棕榈酰基、十七烷酰基、硬脂酰基、油酰基、反油酰基和山萮酰基。
在上述式(1)中,肽部包含的R2表示氢原子、或可具有碳原子数1或2的支链的碳原子数1~4的烷基。
上述所谓可具有碳原子数1或2的支链的碳原子数1~4的烷基,表示主链的碳原子数为1~4、且可具有碳原子数1或2的支链的烷基,作为其具体例,可举出甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基或叔丁基等。
上述R2优选为氢原子、或可具有碳原子数1的支链的碳原子数1~3的烷基,更优选为氢原子。
所谓可具有碳原子数1的支链的碳原子数1~3的烷基,表示主链的碳原子数为1~3、且可具有碳原子数1的支链的烷基,作为其具体例,可举出甲基、乙基、正丙基、异丙基、异丁基或仲丁基等,优选为甲基、异丙基、异丁基或仲丁基。
在上述式(1)中,R3表示-(CH2)n-X基。在上述-(CH2)n-X基中,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的五元环基、可具有1~3个氮原子的六元环基、或可具有1~3个氮原子的由五元环和六元环构成的稠杂环基。
在上述表示R3的-(CH2)n-X基中,X优选为氨基、胍基、氨基甲酰基(-CONH2基)、吡咯基、咪唑基、吡唑基或吲哚基,更优选为咪唑基。此外,在上述-(CH2)n-X基中,n优选为1或2,更优选为1。
因此,上述-(CH2)n-X基优选表示氨基甲基、2-氨基乙基、3-氨基丙基、4-氨基丁基、氨基甲酰基甲基、2-氨基甲酰基乙基、3-氨基甲酰基丁基、2-胍基乙基、3-胍基丁基、吡咯甲基、4-咪唑甲基、吡唑甲基或3-吲哚甲基,更优选表示4-氨基丁基、氨基甲酰基甲基、2-氨基甲酰基乙基、3-胍基丁基、4-咪唑甲基或3-吲哚甲基,进一步优选为4-咪唑甲基。
关于作为脂质肽型化合物的、上述式(1)所示的化合物中的特别适合的脂质肽,是以下由脂质部和肽部(氨基酸集合部)形成的化合物:月桂酰-Gly-His、月桂酰-Gly-Gln、月桂酰-Gly-Asn、月桂酰-Gly-Trp、月桂酰-Gly-Lys、月桂酰-Ala-His、月桂酰-Ala-Gln、月桂酰-Ala-Asn、月桂酰-Ala-Trp、月桂酰-Ala-Lys;肉豆蔻酰-Gly-His、肉豆蔻酰-Gly-Gln、肉豆蔻酰-Gly-Asn、肉豆蔻酰-Gly-Trp、肉豆蔻酰-Gly-Lys、肉豆蔻酰-Ala-His、肉豆蔻酰-Ala-Gln、肉豆蔻酰-Ala-Asn、肉豆蔻酰-Ala-Trp、肉豆蔻酰-Ala-Lys;棕榈酰-Gly-His、棕榈酰-Gly-Gln、棕榈酰-Gly-Asn、棕榈酰-Gly-Trp、棕榈酰-Gly-Lys、棕榈酰-Ala-His、棕榈酰-Ala-Gln、棕榈酰-Ala-Asn、棕榈酰-Ala-Trp、棕榈酰-Ala-Lys;硬脂酰-Gly-His、硬脂酰-Gly-Gln、硬脂酰-Gly-Asn、硬脂酰-Gly-Trp、硬脂酰-Gly-Lys、硬脂酰-Ala-His、硬脂酰-Ala-Gln、硬脂酰-Ala-Asn、硬脂酰-Ala-Trp、硬脂酰-Ala-Lys。需要说明的是,作为氨基酸的简称,Ala表示丙氨酸、Asn表示天冬酰胺、Gln表示谷氨酰胺、Gly表示甘氨酸、His表示组氨酸、Ile表示异亮氨酸、Leu表示亮氨酸、Lys表示赖氨酸、Trp表示色氨酸、Val表示缬氨酸。
作为最优选的例子,可举出月桂酰-Gly-His、月桂酰-Ala-His、肉豆蔻酰-Gly-His、肉豆蔻酰-Ala-His、棕榈酰-Gly-His、棕榈酰-Ala-His、硬脂酰-Gly-His、硬脂酰-Ala-His。
在上述式(2)中,R4表示碳原子数9~23的脂肪族基,作为优选的具体例,可举出与上述R1所定义的基团相同的基团。
在上述式(2)中,R5~R7各自独立地表示氢原子、或可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,优选R5~R7之中的至少一个以上表示-(CH2)n-X基。n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的五元环基、可具有1~3个氮原子的六元环基、或可具有1~3个氮原子的由五元环和六元环构成的稠杂环基。在这里,作为R5~R7的优选的具体例,可举出与上述R2和R3所定义的基团相同的基团。
在上述式(2)所示的化合物中,作为适合的脂质肽,是以下由脂质部和肽部(氨基酸集合部)形成的化合物。月桂酰-Gly-Gly-His、肉豆蔻酰-Gly-Gly-His、肉豆蔻酰-Gly-Gly-Gln、肉豆蔻酰-Gly-Gly-Asn、肉豆蔻酰-Gly-Gly-Trp、肉豆蔻酰-Gly-Gly-Lys、肉豆蔻酰-Gly-Ala-His、肉豆蔻酰-Gly-Ala-Gln、肉豆蔻酰-Gly-Ala-Asn、肉豆蔻酰-Gly-Ala-Trp、肉豆蔻酰-Gly-Ala-Lys、肉豆蔻酰-Ala-Gly-His、肉豆蔻酰-Ala-Gly-Gln、肉豆蔻酰-Ala-Gly-Asn、肉豆蔻酰-Ala-Gly-Trp、肉豆蔻酰-Ala-Gly-Lys、肉豆蔻酰-Gly-His-Gly、肉豆蔻酰-His-Gly-Gly、棕榈酰-Gly-Gly-His、棕榈酰-Gly-Gly-Gln、棕榈酰-Gly-Gly-Asn、棕榈酰-Gly-Gly-Trp、棕榈酰-Gly-Gly-Lys、棕榈酰-Gly-Ala-His、棕榈酰-Gly-Ala-Gln、棕榈酰-Gly-Ala-Asn、棕榈酰-Gly-Ala-Trp、棕榈酰-Gly-Ala-Lys、棕榈酰-Ala-Gly-His、棕榈酰-Ala-Gly-Gln、棕榈酰-Ala-Gly-Asn、棕榈酰-Ala-Gly-Trp、棕榈酰-Ala-Gly-Lys、棕榈酰-Gly-His-Gly、棕榈酰-His-Gly-Gly、硬脂酰-Gly-Gly-His。
其中,作为最优选的例子,可举出月桂酰-Gly-Gly-His、肉豆蔻酰-Gly-Gly-His、棕榈酰-Gly-Gly-His、棕榈酰-Gly-His-Gly、棕榈酰-His-Gly-Gly、硬脂酰-Gly-Gly-His。
在上述式(3)中,R8表示碳原子数9~23的脂肪族基,作为优选的具体例,可举出与上述R1所定义的基团相同的基团。
在上述式(3)中,R9~R12各自独立地表示氢原子、或可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,优选R9~R12之中的至少一个以上表示-(CH2)n-X基。n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的五元环基、可具有1~3个氮原子的六元环基、或可具有1~3个氮原子的由五元环和六元环构成的稠杂环基。在这里,作为R9~R12的优选的具体例,可举出与上述R2和R3所定义的基团相同的基团。
因此,在上述式(3)所示的化合物中,作为适合的脂质肽型化合物,作为特别适合的脂质肽,可举出月桂酰-Gly-Gly-Gly-His、肉豆蔻酰-Gly-Gly-Gly-His、棕榈酰-Gly-Gly-Gly-His、棕榈酰-Gly-Gly-His-Gly、棕榈酰-Gly-His-Gly-Gly、棕榈酰-His-Gly-Gly-Gly、硬脂酰-Gly-Gly-Gly-His等。
在本发明中,脂质肽型化合物的混配量相对于组合物的总质量,例如为0.001质量%~30质量%,优选为0.005质量%~10质量%,更优选为0.01质量%~5质量%,进一步优选为0.05质量%~1质量%。
需要说明的是,在本发明中使用的脂质肽型化合物由上述式(1)~式(3)所示的化合物(脂质肽)或其可药用的盐之中的至少一种构成,这些化合物可以单独使用一种,或组合使用二种以上。
[蔗糖酯]
在本发明中,作为蔗糖酯,可举出例如,蔗糖癸酸酯、蔗糖月桂酸酯、蔗糖肉豆蔻酸酯、蔗糖棕榈酸酯、蔗糖硬脂酸酯、蔗糖油酸酯、蔗糖花生酸酯和蔗糖山萮酸酯等,作为特别适合的蔗糖酯,可举出蔗糖月桂酸酯、蔗糖肉豆蔻酸酯、蔗糖棕榈酸酯、蔗糖硬脂酸酯等。
在本发明中,蔗糖酯的混配量相对于组合物的总质量,例如为0.001质量%~20质量%,优选为0.005质量%~10质量%,更优选为0.01质量%~10质量%,进一步优选为0.05质量%~5质量%,特别优选为0.1质量%~1质量%。
需要说明的是,在本发明中使用的蔗糖酯由上述蔗糖酯之中的至少一种构成,这些蔗糖酯可以单独使用一种,或组合使用二种以上。
[其它成分]
本发明的组合物除了上述脂质肽型化合物和蔗糖酯以外,还可以包含水、醇、多元醇或它们的混合溶液。
作为上述水,可举出例如,净化水、纯化水、硬水、软水、天然水、海洋深层水、电解碱性离子水、电解酸性离子水、离子水、和集束水(cluster water)等。
上述所谓醇,为一元醇,可举出例如,以任意比例溶解于水的碳原子数1~6的醇具体为甲醇、乙醇、2-丙醇和异丁醇等、以及高级醇具体为油醇和苯氧基醇等。
上述所谓多元醇,为二元以上的醇,可举出例如,丙二醇、1,3-丁二醇、2-乙基-1,3-己二醇、甘油、异戊二醇、乙基己二醇、赤藓酮糖、臭氧化甘油、辛二醇、乙二醇、(C15-18)二醇、(C20-30)二醇、二甘醇、双甘油、二硫杂辛二醇、DPG、硫甘油、1,10-癸二醇(1,10-Decanediol)、癸二醇(Decylene Glycol)、三甘醇、三甲基羟甲基环己醇(チリメチルギドロキシメチルシクロヘキサノール)、植烷三醇、苯氧基丙二醇、1,2-丁二醇、2,3-丁二醇、丁基乙基丙二醇、1,2-己二醇、1,6-己二醇、戊二醇、甲基丙二醇、薄荷烷二醇、月桂基二醇和聚丙二醇。
在本发明中,在包含多元醇的情况下,其含量相对于组合物的总质量,例如可以为0.001质量%~10质量%,优选为0.001质量%~5质量%,进一步优选为0.005质量%~0.5质量%。
需要说明的是,在本发明中,在包含多元醇的情况下,多元醇可以单独使用一种,或组合使用二种以上。
[其它添加剂]
本发明的组合物根据需要可以包含一般能够作为化妆品用添加剂、准药品用添加剂和医药用添加剂使用的添加剂等。
作为混配在化妆品、准药品或医药等皮肤外用剂中的生理活性物质和功能性物质等添加成分,可举出例如颜料、油性基剂、保湿剂、触感改进剂、除上述以外的表面活性剂、高分子/增稠剂/胶凝剂、溶剂、抗氧化剂、还原剂、氧化剂、防腐剂、抗菌剂、杀菌剂、螯合剂、pH调节剂、酸、碱、粉体、无机盐、紫外线吸收剂、美白剂、维生素类及其衍生物类、育毛用药剂、白发预防剂、血液循环促进剂、刺激剂、激素类、抗皱剂、抗老化剂、紧致剂、冷感剂、温感剂、创伤治愈促进剂、刺激缓和剂、镇痛剂、细胞活化剂、植物/动物/微生物提取物、止痒剂、角质剥离/溶解剂、抑汗剂、清凉剂、收敛剂、酶、核酸、香料、色素、着色剂、染料、消炎剂、抗炎剂、抗哮喘、抗慢性阻塞性肺疾病、抗变态反应、免疫调节剂、抗感染症剂和抗真菌剂等。
这些其它添加剂的含量可以根据其种类而进行各种变化,但相对于组合物的总质量,例如可以为0.001质量%~20质量%、或0.01质量%~10质量%左右。
作为颜料,可举出二氧化钛、氧化锌等无机白色颜料;氧化铁红(氧化铁红)、钛酸铁等无机红色系颜料;γ-氧化铁等无机褐色系颜料;氧化铁黄、黄土等无机黄色系颜料;氧化铁黑、低价氧化钛等无机黑色系颜料;锰紫、钴紫等无机紫色系颜料;氧化铬、氢氧化铬、钛酸钴等无机绿色系颜料;群青、藏青等无机蓝色系颜料;氧化钛被覆云母、氧化钛被覆氯氧化铋、氧化钛被覆滑石、着色氧化钛被覆云母、氯氧化铋、鱼鳞箔等珠光颜料;滑石、绢云母、云母、高岭土、碳酸钙、碳酸镁、硅酸酐、硫酸钡、氢氧化铝等体质颜料;铝粉末、铜粉末、金等金属粉末颜料;表面处理无机和金属粉末颜料;锆、钡或铝色淀等有机颜料;表面处理有机颜料等作为优选的例子。
作为油性基剂,可举出油醇、霍霍巴醇、鲛肝醇、鲨油醇、鲨肝醇、己基癸醇、异硬脂醇、2-辛基十二烷醇、二聚体二醇等高级(多元)醇类;苯甲醇等芳烷基醇及其衍生物;硬脂酸、异硬脂酸、山萮酸、10-十一碳烯酸、12-羟基硬脂酸、棕榈油酸、油酸、亚油酸、亚麻酸、芥酸、二十二碳六烯酸、二十碳五烯酸、异十六烷酸、反异二十一烷酸、长链分支脂肪酸、二聚酸、氢化二聚酸等;液体石蜡(矿物油)、重质液体异链烷烃、轻质液体异链烷烃、α-烯烃低聚物、聚异丁烯、氢化聚异丁烯、聚丁烯、角鲨烷、来源于橄榄的角鲨烷、角鲨烯、凡士林、固体石蜡等烃类;小烛树蜡、巴西棕榈蜡、米糠蜡、木蜡、蜂蜡、褐煤蜡、地蜡、纯地蜡、石蜡、微晶蜡、矿脂、费托合成过程中得到的蜡、聚乙烯蜡、乙烯-丙烯共聚物等蜡类;椰油、棕榈油、棕榈仁油、红花油、橄榄油、蓖麻油、鳄梨油、芝麻油、茶油、月见草油、小麦胚芽油、澳洲坚果油、榛子油、石栗油、蔷薇果油、绣线菊油、桃仁油、茶树油、薄荷油、玉米油、菜籽油、葵花油、小麦胚芽油、亚麻子油、棉籽油、豆油、花生油、米糠油、可可脂、牛油果油、氢化椰油、氢化蓖麻油、霍霍巴油、氢化霍霍巴油、葡萄籽油、杏仁油(apricot kernel oil)、山茶油等植物油脂类;牛脂、乳脂、马脂、蛋黄油、貂油、海龟油等动物性油脂类;鲸蜡、羊毛脂、大西洋胄胸鲷油等动物性蜡类;液体羊毛脂、还原羊毛脂、吸附纯化羊毛脂、羊毛脂乙酸酯、液体羊毛脂乙酸酯、羟基羊毛脂、聚氧乙烯羊毛脂、羊毛脂脂肪酸、硬质羊毛脂脂肪酸、羊毛脂醇、羊毛脂醇乙酸酯、乙酸(鲸蜡基/羊毛脂基)酯等羊毛脂类;胆固醇、二氢胆固醇、羊毛固醇、二氢羊毛固醇、植物甾醇、胆酸等固醇类;皂苷元类;皂苷类;乙酸胆甾醇酯、壬酸胆甾醇酯、硬脂酸胆甾醇酯、异硬脂酸胆甾醇酯、油酸胆甾醇酯、N-月桂酰-L-谷氨酸二(胆甾醇基/山萮基/辛基十二烷基)酯、N-月桂酰-L-谷氨酸二(胆甾醇基/辛基十二烷基)酯、N-月桂酰-L-谷氨酸二(植物甾醇基/山萮基/辛基十二烷基)酯、N-月桂酰-L-谷氨酸二(植物甾醇基/辛基十二烷基)酯、N-月桂酰肌氨酸异丙酯等酰基肌氨酸烷基酯、12-羟基硬脂酸胆甾醇酯、澳洲坚果油脂肪酸胆甾醇酯、澳洲坚果油脂肪酸植物甾醇酯、异硬脂酸植物甾醇酯、软质羊毛脂脂肪酸胆甾醇酯、硬质羊毛脂脂肪酸胆甾醇酯、长链分支脂肪酸胆甾醇酯、长链α-羟基脂肪酸胆甾醇酯等固醇酯类;磷脂-胆固醇复合体、磷脂-植物甾醇复合体等脂质复合体;肉豆蔻酸辛基十二烷基酯、肉豆蔻酸己基癸酯、异硬脂酸辛基十二烷基酯、棕榈酸鲸蜡醇酯、棕榈酸辛基十二烷基酯、辛酸鲸蜡醇酯、辛酸己基癸酯、异壬酸异十三烷基酯、异壬酸异壬酯、异壬酸辛酯、新戊酸异癸酯、新戊酸异十三烷基酯、新戊酸异硬脂醇酯、新癸酸辛基十二烷基酯、油酸油酯、油酸辛基十二烷基酯、蓖麻油酸辛基十二烷基酯、羊毛脂脂肪酸辛基十二烷基酯、二甲基辛酸己基癸酯、芥酸辛基十二烷基酯、异硬脂酸氢化蓖麻油、油酸乙酯、鳄梨油脂肪酸乙酯、肉豆蔻酸异丙酯、棕榈酸异丙酯、棕榈酸辛酯、异硬脂酸异丙酯、羊毛脂脂肪酸异丙酯、癸二酸二乙酯、癸二酸二异丙酯、癸二酸二辛酯、己二酸二异丙酯、癸二酸二丁基辛酯、己二酸二异丁酯、琥珀酸二辛酯、柠檬酸三乙酯等一元醇羧酸酯类;乳酸鲸蜡醇酯、苹果酸二异硬脂醇酯、单异硬脂酸氢化蓖麻油等羟基酸酯类;三辛酸甘油酯(三2-乙基己酸甘油酯)、三油酸甘油酯、三异硬脂酸甘油酯、二异硬脂酸甘油酯、三(辛酸/癸酸)甘油酯、三(辛酸/癸酸/肉豆蔻酸/硬脂酸)甘油酯、氢化松香甘油三酯(氢化酯胶)、松香甘油三酯(酯胶)、山萮酸二十烷二酸甘油酯、三辛酸三羟甲基丙烷酯、三异硬脂酸三羟甲基丙烷酯、二辛酸新戊二醇酯、二癸酸新戊二醇酯、二辛酸2-丁基-2-乙基-1,3-丙二醇酯、二油酸丙二醇酯、四辛酸季戊四醇酯、氢化松香季戊四醇酯、三乙基己酸双三羟甲基丙烷酯、(异硬脂酸/癸二酸)双三羟甲基丙烷酯、三乙基己酸季戊四醇酯、(羟基硬脂酸/硬脂酸/松香酸)二季戊四醇酯、二异硬脂酸二甘油酯、四异硬脂酸聚甘油酯、九异硬脂酸聚甘油-10酯、十(芥酸/异硬脂酸/蓖麻油酸)聚甘油-8酯、(己基癸酸/癸二酸)二甘油低聚酯、二硬脂酸乙二醇酯(二硬脂酸乙二醇酯)、二新戊酸3-甲基-1,5-戊二醇酯、二新戊酸2,4-二乙基-1,5-戊二醇酯等多元醇脂肪酸酯类;二聚体二亚油酸二异丙酯、二聚体二亚油酸二异硬脂醇酯、二聚体二亚油酸二(异硬脂基/植物甾醇基)酯、二聚体二亚油酸(植物甾醇基/山萮基)酯、二聚体二亚油酸(植物甾醇基/异硬脂基/鲸蜡基/硬脂基/山萮基)酯、二聚体二亚油酸二聚体二亚油醇酯、二异硬脂酸二聚体二亚油醇酯、二聚体二亚油醇基氢化松香缩合物、二聚体二亚油酸氢化蓖麻油、羟基烷基二聚体二亚油醇基醚等二聚酸或二聚体二醇的衍生物;椰油脂肪酸单乙醇酰胺(椰油酰胺MEA)、椰油脂肪酸二乙醇酰胺(椰油酰胺DEA)、月桂酸单乙醇酰胺(月桂酰胺MEA)、月桂酸二乙醇酰胺(月桂酰胺DEA)、月桂酸单异丙醇酰胺(月桂酰胺MIPA)、棕榈酸单乙醇酰胺(棕榈酰胺MEA)、棕榈酸二乙醇酰胺(棕榈酰胺DEA)、椰油脂肪酸甲基乙醇酰胺(椰油酰胺甲基MEA)等脂肪酸链烷醇酰胺类;聚二甲基硅氧烷(二甲基聚硅氧烷)、高聚合聚二甲基硅氧烷(高聚合二甲基聚硅氧烷)、环聚甲基硅氧烷(环状二甲基硅氧烷、十甲基环状五硅氧烷(也简称为环五硅氧烷))、苯基聚三甲基硅氧烷、二苯基聚二甲基硅氧烷、苯基聚二甲基硅氧烷、硬脂氧基丙基二甲基胺、(氨基乙基氨基丙基聚甲基硅氧烷/聚二甲基硅氧烷)共聚物、聚二甲基硅烷醇、聚二甲基硅烷醇交联聚合物、有机硅树脂、硅橡胶、氨基丙基聚二甲基硅氧烷和氨基封端的聚二甲基硅氧烷等氨基改性有机硅、阳离子改性有机硅、聚二甲基硅氧烷共聚醇等聚醚改性有机硅、聚甘油改性有机硅、糖改性有机硅、羧酸改性有机硅、磷酸改性有机硅、硫酸改性有机硅、烷基改性有机硅、脂肪酸改性有机硅、烷基醚改性有机硅、氨基酸改性有机硅、肽改性有机硅、氟改性有机硅、阳离子改性和聚醚改性有机硅、氨基改性和聚醚改性有机硅、烷基改性和聚醚改性有机硅、聚硅氧烷-氧化烯共聚物等有机硅类;全氟癸烷、全氟辛烷、全氟聚醚等氟系油剂类作为优选的例子。
作为保湿剂、触感改进剂,可举出甘油、三羟甲基丙烷、季戊四醇、己二醇、二甘油、聚甘油、二甘醇、双丙甘醇、聚丙二醇、乙二醇-丙二醇共聚物等多元醇类及其聚合物;二甘醇单乙基醚(乙氧基二甘醇)、乙二醇单乙基醚、乙二醇单丁基醚、二甘醇二丁基醚等二醇烷基醚类;(二十烷二酸/十四烷二酸)聚甘油-10酯、十四烷二酸聚甘油-10酯等水溶性酯类;山梨糖醇、木糖醇、赤藓醇、甘露糖醇、麦芽糖醇等糖醇类;葡萄糖、果糖、半乳糖、甘露糖、苏糖、木糖、阿拉伯糖、岩藻糖、核糖、脱氧核糖、麦芽糖、海藻糖、乳糖、棉子糖、葡糖酸、葡糖醛酸、环糊精类(α-、β-、γ-环糊精以及麦芽糖基化、羟基烷基化等修饰环糊精)、β-葡聚糖(β-Glucan)、壳多糖、壳聚糖、肝素及其衍生物、果胶、阿拉伯半乳聚糖、糊精、葡聚糖(dextran)、糖原、乙基葡糖苷、甲基丙烯酸葡糖基乙酯聚合物或共聚物等糖类及其衍生物类;透明质酸、透明质酸钠;硫酸软骨素钠;硫酸粘液素、硫酸卡洛宁(charonin sulfate)、硫酸角质、硫酸皮肤素;银耳提取物、银耳多糖体;岩藻依聚糖;晚香玉多糖体或天然来源的多糖体;柠檬酸、酒石酸、乳酸等有机酸及其盐;尿素及其衍生物;2-吡咯烷酮-5-甲酸及其钠等盐;甜菜碱(三甲基甘氨酸)、脯氨酸、羟基脯氨酸、精氨酸、赖氨酸、丝氨酸、甘氨酸、丙氨酸、苯丙氨酸、酪氨酸、β-丙氨酸、苏氨酸、谷氨酸、谷氨酰胺、胍基乙酸、天冬酰胺、天冬氨酸、半胱氨酸、胱氨酸、蛋氨酸、亮氨酸、异亮氨酸、缬氨酸、色氨酸、组氨酸、牛磺酸等氨基酸类及其盐;胶原、来源于鱼的胶原、缺端胶原(atelocollagen)、明胶、弹性蛋白、胶原分解肽、水解胶原、氯化羟基丙基铵水解胶原、弹性蛋白分解肽、角蛋白分解肽、水解角蛋白、贝壳硬蛋白分解肽、水解贝壳硬蛋白、丝蛋白分解肽、水解丝蛋白、月桂酰水解丝蛋白钠、大豆蛋白分解肽、小麦蛋白分解肽、水解小麦蛋白、酪蛋白分解肽、酰基化肽等蛋白肽类及其衍生物;棕榈酰寡肽、棕榈酰五肽、棕榈酰四肽等酰基化肽类;甲硅烷基化肽类;乳酸菌培养液、酵母提取液、蛋壳膜蛋白、牛颌下腺粘蛋白、亚牛磺酸、芝麻木酚素糖苷、谷胱甘肽、白蛋白、乳清;氯化胆碱、磷酸胆碱;胎盘提取液、弹性蛋白(エアラスチン)、胶原、芦荟提取物、金缕梅水、丝瓜水、洋甘菊提取物、甘草提取物、聚合草提取物、蚕丝提取物、缫丝花提取物、蓍提取物、桉提取物、草木犀提取物等动物、植物提取成分、天然型神经酰胺(1型、2型、3型、4型、5型、6型)、羟基神经酰胺、假神经酰胺、糖鞘脂、含有神经酰胺和糖神经酰胺的提取物等神经酰胺类作为优选的例子。
作为表面活性剂,可举出阴离子性表面活性剂、非离子性表面活性剂、阳离子性表面活性剂、两性表面活性剂、高分子表面活性剂等作为优选的表面活性剂。如果例示作为表面活性剂优选的例子,则作为阴离子性表面活性剂,可举出月桂酸钾、肉豆蔻酸钾等脂肪酸盐;月桂基硫酸钠、月桂基硫酸三乙醇胺、月桂基硫酸铵等烷基硫酸酯盐;月桂醇聚醚硫酸酯钠、月桂醇聚醚硫酸三乙醇胺等聚氧乙烯烷基硫酸盐;椰油酰甲基牛磺酸钠、椰油酰甲基牛磺酸钾、月桂酰甲基牛磺酸钠、肉豆蔻酰甲基牛磺酸钠、月桂酰甲基丙氨酸钠、月桂酰肌氨酸钠、月桂酰肌氨酸三乙醇胺、月桂酰谷氨酸甲基丙氨酸钠等酰基N-甲基氨基酸盐;椰油酰谷氨酸钠、椰油酰谷氨酸三乙醇胺、月桂酰谷氨酸钠、肉豆蔻酰谷氨酸钠、硬脂酰谷氨酸钠、棕榈酰天冬氨酸二(三乙醇胺)、椰油酰丙氨酸三乙醇胺等酰基氨基酸盐;月桂醇聚醚乙酸酯钠等聚氧乙烯烷基醚乙酸盐;月桂酰单乙醇酰胺琥珀酸钠等琥珀酸酯盐;脂肪酸链烷醇酰胺醚羧酸盐;酰基乳酸盐;聚氧乙烯脂肪胺硫酸盐;脂肪酸链烷醇酰胺硫酸盐;氢化椰油脂肪酸甘油硫酸钠等脂肪酸甘油酯硫酸盐;烷基苯聚氧乙烯硫酸盐;α-烯烃磺酸钠等烯烃磺酸盐;磺基琥珀酸月桂基二钠、磺基琥珀酸二辛基钠等烷基磺基琥珀酸盐;磺基琥珀酸月桂醇聚醚二钠、单月桂酰单乙醇酰胺聚氧乙烯磺基琥珀酸钠、月桂基聚丙二醇磺基琥珀酸钠等烷基醚磺基琥珀酸盐;十四烷基苯磺酸钠、十四烷基苯磺酸三乙醇胺等烷基苯磺酸盐;烷基萘磺酸盐;链烷磺酸盐;α-磺基脂肪酸甲基酯盐;酰基羟乙磺酸盐;烷基缩水甘油基醚磺酸盐;烷基磺基乙酸盐;月桂醇聚醚磷酸酯钠、二月桂醇聚醚磷酸酯钠、三月桂醇聚醚磷酸酯钠、单油醇聚醚磷酸酯钠等烷基醚磷酸酯盐;月桂基磷酸钾等烷基磷酸酯盐;酪蛋白钠;烷基芳基醚磷酸盐;脂肪酸酰胺醚磷酸盐;磷脂酰甘油、磷脂酰肌醇、磷脂酸等磷脂类;羧酸改性有机硅、磷酸改性有机硅、硫酸改性有机硅等有机硅系阴离子性表面活性剂等;作为非离子性表面活性剂,可举出月桂醇聚醚(聚氧乙烯月桂基醚)类、鲸蜡醇聚醚(聚氧乙烯鲸蜡基醚)类、硬脂醇聚醚(聚氧乙烯硬脂基醚)类、山萮醇聚醚(聚氧乙烯山萮基醚)类、异硬脂醇聚醚(聚氧乙烯异硬脂基醚)类、辛基十二醇聚醚(聚氧乙烯辛基十二烷基醚)类等各种聚氧乙烯加成数的聚氧乙烯烷基醚类;聚氧乙烯烷基苯基醚;聚氧乙烯氢化蓖麻油、聚氧乙烯蓖麻油、聚氧乙烯氢化蓖麻油单异硬脂酸酯、聚氧乙烯氢化蓖麻油三异硬脂酸酯、聚氧乙烯氢化蓖麻油单焦谷氨酸单异硬脂酸二酯、聚氧乙烯氢化蓖麻油马来酸等蓖麻油和氢化蓖麻油衍生物;聚氧乙烯植物甾醇;聚氧乙烯胆固醇;聚氧乙烯胆甾烷醇;聚氧乙烯羊毛脂;聚氧乙烯还原羊毛脂;聚氧乙烯-聚氧丙烯鲸蜡基醚、聚氧乙烯-聚氧丙烯2-癸基十四烷基醚、聚氧乙烯-聚氧丙烯单丁基醚、聚氧乙烯-聚氧丙烯氢化羊毛脂、聚氧乙烯-聚氧丙烯甘油醚等聚氧乙烯-聚氧丙烯烷基醚;聚氧乙烯-聚氧丙烯二醇;PPG-9二甘油酯等(聚)甘油聚氧丙烯二醇;硬脂酸甘油酯、异硬脂酸甘油酯、棕榈酸甘油酯、肉豆蔻酸甘油酯、油酸甘油酯、椰油脂肪酸甘油酯、单棉籽油脂肪酸甘油酯、单芥酸甘油酯、倍半油酸甘油酯、α,α’-油酸焦谷氨酸甘油酯、单硬脂酸甘油苹果酸等甘油脂肪酸部分酯类;硬脂酸聚甘油-2酯、硬脂酸聚甘油-3酯、硬脂酸聚甘油-4酯、硬脂酸聚甘油-5酯、硬脂酸聚甘油-6酯、硬脂酸聚甘油-8酯、硬脂酸聚甘油-10酯、二硬脂酸聚甘油-6酯、二硬脂酸聚甘油-10酯、三硬脂酸聚甘油-2酯、十硬脂酸聚甘油-10酯、异硬脂酸聚甘油-2酯、异硬脂酸聚甘油-3酯、异硬脂酸聚甘油-4酯、异硬脂酸聚甘油-5酯、异硬脂酸聚甘油-6酯、异硬脂酸聚甘油-8酯、异硬脂酸聚甘油-10酯、二异硬脂酸聚甘油-2酯(二异硬脂酸二甘油酯)、二异硬脂酸聚甘油-3酯、二异硬脂酸聚甘油-10酯、三异硬脂酸聚甘油-2酯、四异硬脂酸聚甘油-2酯、十异硬脂酸聚甘油-10酯、油酸聚甘油-2酯、油酸聚甘油-3酯、油酸聚甘油-4酯、油酸聚甘油-5酯、油酸聚甘油-6酯、油酸聚甘油-8酯、油酸聚甘油-10酯、二油酸聚甘油-6酯、三油酸聚甘油-2酯、十油酸聚甘油-10酯等聚甘油脂肪酸酯;单硬脂酸乙二醇酯等乙二醇单脂肪酸酯;单硬脂酸丙二醇酯等丙二醇单脂肪酸酯;季戊四醇部分脂肪酸酯;山梨糖醇部分脂肪酸酯;麦芽糖醇部分脂肪酸酯;麦芽糖醇醚;失水山梨糖醇单油酸酯、失水山梨糖醇单异硬脂酸酯、失水山梨糖醇单月桂酸酯、失水山梨糖醇单棕榈酸酯、失水山梨糖醇单硬脂酸酯、失水山梨糖醇倍半油酸酯、失水山梨糖醇三油酸酯、五-2-乙基己酸二甘油失水山梨糖醇酯、四-2-乙基己酸二甘油失水山梨糖醇酯等失水山梨糖醇脂肪酸酯;蔗糖脂肪酸酯、甲基葡糖苷脂肪酸酯、十一碳烯酸海藻糖等糖衍生物部分酯;辛基葡糖苷等烷基葡糖苷;烷基多苷;羊毛脂醇;还原羊毛脂;聚氧乙烯二硬脂酸酯、聚乙二醇二异硬脂酸酯、聚氧乙烯单油酸酯、聚氧乙烯二油酸酯等聚氧乙烯脂肪酸单酯和二酯;聚氧乙烯-丙二醇脂肪酸酯;聚氧乙烯甘油单硬脂酸酯、聚氧乙烯甘油单异硬脂酸酯、聚氧乙烯甘油三异硬脂酸酯等聚氧乙烯单油酸酯等聚氧乙烯甘油脂肪酸酯;聚氧乙烯失水山梨糖醇单油酸酯、聚氧乙烯失水山梨糖醇单硬脂酸酯、聚氧乙烯失水山梨糖醇单油酸酯、聚氧乙烯失水山梨糖醇四油酸酯等聚氧乙烯失水山梨糖醇脂肪酸酯;聚氧乙烯山梨糖醇单月桂酸酯、聚氧乙烯山梨糖醇单油酸酯、聚氧乙烯山梨糖醇五油酸酯、聚氧乙烯山梨糖醇单硬脂酸酯等聚氧乙烯山梨糖醇脂肪酸酯;聚氧乙烯甲基葡糖苷脂肪酸酯;聚氧乙烯烷基醚脂肪酸酯;聚氧乙烯山梨糖醇蜂蜡等聚氧乙烯动植物油脂类;异硬脂基甘油基醚、鲛肝醇、鲨油醇、鲨肝醇等烷基甘油基醚类;多元醇烷基醚;聚氧乙烯烷基胺;四聚氧乙烯-四聚氧丙烯-乙二胺缩合物类;皂苷、槐糖脂等天然系表面活性剂;聚氧乙烯脂肪酸酰胺;椰油脂肪酸单乙醇酰胺(椰油酰胺MEA)、椰油脂肪酸二乙醇酰胺(椰油酰胺DEA)、月桂酸单乙醇酰胺(月桂酰胺MEA)、月桂酸二乙醇酰胺(月桂酰胺DEA)、月桂酸单异丙醇酰胺(月桂酰胺MIPA)、棕榈酸单乙醇酰胺(棕榈酰胺MEA)、棕榈酸二乙醇酰胺(棕榈酰胺DEA)、椰油脂肪酸甲基乙醇酰胺(椰油酰胺甲基MEA)等脂肪酸链烷醇酰胺类;月桂基氧化胺、氧化椰油胺、氧化硬脂胺、氧化山萮胺等烷基二甲基氧化胺;烷基乙氧基二甲基氧化胺;聚氧乙烯烷基硫醇;聚二甲基硅氧烷共聚醇等聚醚改性有机硅、聚硅氧烷-氧化烯共聚物、聚甘油改性有机硅、糖改性有机硅等有机硅系非离子性表面活性剂等;作为阳离子性表面活性剂,可举出山萮基三甲基氯化铵、硬脂基三甲基氯化铵、十六烷基三甲基氯化铵、月桂基三甲基氯化铵等烷基三甲基氯化铵;硬脂基三甲基溴化铵等烷基三甲基溴化铵;二硬脂基二甲基氯化铵、二椰油基二甲基氯化铵等二烷基二甲基氯化铵;硬脂酰胺丙基二甲基胺、硬脂酰胺乙基二乙基胺等脂肪酸酰胺胺及其盐;硬脂氧基丙基二甲基胺等烷基醚胺及其盐或季盐;乙基硫酸长链分支脂肪酸(12~31)氨基丙基乙基二甲基铵、乙基硫酸羊毛脂脂肪酸氨基丙基乙基二甲基铵等脂肪酸酰胺型季铵盐;聚氧乙烯烷基胺及其盐或季盐;烷基胺盐;脂肪酸酰胺胍盐;烷基醚铵盐(アルキルエーテルアミンモニウム塩);烷基三亚烷基二醇铵盐;苄烷铵盐;异辛基苯氧基乙氧基乙基二甲基苄基铵盐;鲸蜡基氯化吡啶等吡啶/>盐;咪唑啉盐;烷基异喹啉/>盐;二烷基吗啉/>盐;多胺脂肪酸衍生物;氨基丙基聚二甲基硅氧烷和氨基封端的聚二甲基硅氧烷等氨基改性有机硅、阳离子改性有机硅、阳离子改性和聚醚改性有机硅、氨基改性和聚醚改性有机硅等有机硅系阳离子性表面活性剂等;作为两性表面活性剂,可举出月桂基甜菜碱(月桂基二甲基氨基乙酸甜菜碱)等N-烷基-N,N-二甲基氨基酸甜菜碱;椰油酰胺丙基甜菜碱、月桂酰胺丙基甜菜碱等脂肪酸酰胺烷基-N,N-二甲基氨基酸甜菜碱;椰油酰两性基乙酸钠、月桂酰两性基乙酸钠等咪唑啉型甜菜碱;烷基二甲基牛磺酸等烷基磺基甜菜碱;烷基二甲基氨基乙醇硫酸酯等硫酸型甜菜碱;烷基二甲基氨基乙醇磷酸酯等磷酸型甜菜碱;磷脂酰胆碱、磷脂酰乙醇胺、磷脂酰丝氨酸、神经鞘磷脂等鞘磷脂、溶血卵磷脂、氢化大豆磷脂、部分氢化大豆磷脂、氢化蛋黄磷脂、部分氢化蛋黄磷脂、氢氧化卵磷脂等磷脂类;有机硅系两性表面活性剂等;作为高分子表面活性剂,可举出聚乙烯醇、藻酸钠、淀粉衍生物、黄蓍胶、丙烯酸-甲基丙烯酸烷基酯共聚物;有机硅系各种表面活性剂作为优选的例子。
作为高分子、增稠剂、胶凝剂,可举出瓜耳豆胶、刺槐豆胶、榅桲籽(クィーンスシード)、角叉菜聚糖、半乳聚糖、阿拉伯树胶、塔拉胶(タラガム)、罗望子、红藻胶、刺梧桐树胶、黄蜀葵、皂皮胶(キヤラガム)、黄蓍胶、果胶、果胶酸及其钠盐等盐、藻酸及其钠盐等盐、甘露聚糖;米、玉米、马铃薯、小麦等的淀粉;黄原胶、葡聚糖、琥珀酰葡聚糖、凝胶多糖、透明质酸及其盐、黄原胶、葡聚糖、结冷胶、壳多糖、壳聚糖、琼脂、褐藻提取物、硫酸软骨素盐、酪蛋白、胶原、明胶、白蛋白;甲基纤维素、乙基纤维素、羟基乙基纤维素、羟基丙基纤维素、羟基丙基甲基纤维素、羧基甲基纤维素及其钠盐等盐、甲基羟基丙基纤维素、纤维素硫酸钠、二烷基二甲基铵硫酸纤维素、结晶纤维素、纤维素末等纤维素及其衍生物;可溶性淀粉、羧基甲基淀粉、甲基羟基丙基淀粉、甲基淀粉等淀粉系高分子、羟基丙基三甲基氯化铵淀粉、辛烯基琥珀酸玉米淀粉铝等淀粉衍生物;藻酸钠、藻酸丙二醇酯等藻酸衍生物;聚乙烯基吡咯烷酮(PVP)、聚乙烯醇(PVA)、乙烯基吡咯烷酮-乙烯醇共聚物、聚乙烯基甲基醚;聚乙二醇、聚丙二醇、聚氧乙烯-聚氧丙烯共聚物;(甲基丙烯酰氧基乙基羧基甜菜碱/甲基丙烯酸烷基酯)共聚物、(丙烯酸酯类/丙烯酸硬脂基酯/甲基丙烯酸乙基氧化胺)共聚物等两性甲基丙烯酸酯共聚物;(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物、(丙烯酸烷基酯/二丙酮丙烯酰胺)共聚物、(丙烯酸烷基酯/二丙酮丙烯酰胺)共聚物AMP;聚乙酸乙烯酯部分皂化物、马来酸共聚物;乙烯基吡咯烷酮-甲基丙烯酸二烷基氨基烷基酯共聚物;丙烯酸系树脂链烷醇胺;聚酯、水分散性聚酯;聚丙烯酰胺;聚丙烯酸乙酯等聚丙烯酸酯共聚物、羧基乙烯基聚合物、聚丙烯酸及其钠盐等盐、丙烯酸-甲基丙烯酸酯共聚物;丙烯酸-甲基丙烯酸烷基酯共聚物;聚季铵盐-10等阳离子化纤维素、聚季铵盐-7等二烯丙基二甲基氯化铵-丙烯酰胺共聚物、聚季铵盐-22等丙烯酸-二烯丙基二甲基氯化铵共聚物、聚季铵盐-39等丙烯酸-二烯丙基二甲基氯化铵-丙烯酰胺共聚物、丙烯酸-阳离子化甲基丙烯酸酯共聚物、丙烯酸-阳离子化甲基丙烯酸酰胺共聚物、聚季铵盐-47等丙烯酸-丙烯酸甲酯-氯化甲基丙烯酰胺丙基三甲基铵共聚物、氯化甲基丙烯酸胆碱酯聚合物;阳离子化寡糖、阳离子化葡聚糖、瓜耳豆胶羟基丙基三甲基氯化铵等阳离子化多糖类;聚乙烯亚胺;阳离子聚合物;聚季铵盐-51等2-甲基丙烯酰氧基乙基磷酸胆碱的聚合物和甲基丙烯酸丁酯共聚物等的共聚物;丙烯酸系树脂乳液、聚丙烯酸乙酯乳液、聚丙烯酸烷基酯乳液、聚乙酸乙烯酯树脂乳液、天然橡胶胶乳、合成胶乳等高分子乳液;硝酸纤维素;聚氨酯类和各种共聚物;各种有机硅类;丙烯酸-有机硅接枝共聚物等有机硅系各种共聚物;各种氟系高分子;12-羟基硬脂酸及其盐;棕榈酸糊精酯、肉豆蔻酸糊精酯等糊精脂肪酸酯;二氧化硅、热解法二氧化硅(超微粒二氧化硅)、硅酸铝镁、硅酸钠镁、金属皂、二烷基磷酸金属盐、膨润土、锂蒙脱石、有机改性粘土矿物、蔗糖脂肪酸酯、低聚果糖脂肪酸酯作为优选的例子。上述例示中,优选为纤维素及其衍生物、藻酸及其盐、聚乙烯醇、透明质酸及其盐、或胶原。
作为溶剂,可举出乙醇、2-丙醇(异丙醇)、丁醇、异丁醇等低级醇类;丙二醇、二甘醇、双丙甘醇、异戊基二醇等二醇类;二甘醇单乙基醚(乙氧基二甘醇)、乙二醇单乙基醚、乙二醇单丁基醚、三乙二醇单乙基醚、二甘醇二乙基醚、二甘醇二丁基醚、丙二醇单乙基醚、双丙甘醇单乙基醚等二醇醚类;乙二醇单乙基醚乙酸酯、二甘醇单乙基醚乙酸酯、丙二醇单乙基醚乙酸酯等二醇醚酯类;琥珀酸二乙氧基乙酯、乙二醇二琥珀酸酯等二醇酯类;苯甲醇、苄氧基乙醇、碳酸亚丙酯、碳酸二烷基酯、丙酮、乙酸乙酯、N-甲基吡咯烷酮;甲苯等作为优选的例子。
作为抗氧化剂,可举出生育酚(维生素E)、乙酸生育酚酯等生育酚衍生物;BHT、BHA;没食子酸丙酯等没食子酸衍生物;维生素C(抗坏血酸)和/或其衍生物;异抗坏血酸及其衍生物;亚硫酸钠等亚硫酸盐;亚硫酸氢钠等亚硫酸氢盐;硫代硫酸钠等硫代硫酸盐;焦亚硫酸氢盐;硫代牛磺酸、亚牛磺酸;硫代甘油、硫脲、巯基乙酸、半胱氨酸盐酸盐作为优选的例子。
作为还原剂,可举出巯基乙酸、半胱氨酸、半胱胺等作为优选的例子。
作为氧化剂,可举出过氧化氢水、过硫酸铵、溴酸钠、过碳酸等作为优选的例子。
作为防腐剂、抗菌剂、杀菌剂,可举出对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、对羟基苯甲酸丁酯等羟基苯甲酸及其盐或其酯;水杨酸;苯甲酸钠;苯氧基乙醇;甲基氯异噻唑啉酮、甲基异噻唑啉酮等异噻唑啉酮衍生物;咪唑啉脲;脱氢乙酸及其盐;酚类;三氯生等卤代双酚类、酸酰胺类、季铵盐类;三氯均二苯脲、1-氧-2-巯基-吡啶锌、氯化苄烷铵、苯索氯铵、山梨酸、洗必泰、葡糖酸洗必泰、卤卡班、六氯酚、4-异丙基环庚三烯酚酮;苯酚、异丙基苯酚、甲酚、百里酚、对氯苯酚、苯基苯酚、苯基苯酚钠等其它酚类;苯基乙基醇、感光素类、抗菌性沸石、银离子作为优选的例子。
作为螯合剂,可举出EDTA、EDTA2Na、EDTA3Na、EDTA4Na等乙二胺四乙酸盐(乙二胺四乙酸盐);HEDTA3Na等羟基乙基乙二胺三乙酸盐;喷替酸盐(二亚乙基三胺五乙酸盐);肌醇六磷酸;羟基亚乙基二膦酸等膦酸及其钠盐等盐类;聚天冬氨酸、聚谷氨酸等聚氨基酸类;多磷酸钠、偏磷酸钠、磷酸;柠檬酸钠、柠檬酸、丙氨酸、二羟基乙基甘氨酸、葡糖酸、抗坏血酸、琥珀酸、酒石酸作为优选的例子。
作为pH调节剂、酸、碱,可举出抗坏血酸、柠檬酸、柠檬酸钠、乳酸、乳酸钠、乳酸钾、乙醇酸、琥珀酸、乙酸、乙酸钠、苹果酸、酒石酸、富马酸、磷酸、盐酸、硫酸、单乙醇胺、二乙醇胺、三乙醇胺、异丙醇胺、三异丙醇胺、2-氨基-2-甲基-1,3-丙二醇、2-氨基-2-羟基甲基-1,3-丙二醇、精氨酸、氢氧化钠、氢氧化钾、氨水、碳酸胍、碳酸铵作为优选的例子。
作为粉体,可举出云母(マイカ)、滑石、高岭土、绢云母、蒙脱石、高岭石、云母(雲母)、白云母、金云母、合成云母、红云母、黑云母、蛭石、碳酸镁、碳酸钙、硅酸铝、硅酸钡、硅酸钙、硅酸镁、硅酸锶、钨酸金属盐、镁、沸石、硫酸钡、烧成硫酸钙、磷酸三钙等磷酸钙、氟磷灰石、羟基磷灰石、陶瓷粉末、膨润土、蒙皂石、粘土、泥、金属皂(例如,肉豆蔻酸锌、棕榈酸钙、硬脂酸铝)、碳酸钙、氧化铁红、氧化铁黄、氧化铁黑、群青、藏青、炭黑、氧化钛、微粒和超微粒氧化钛、氧化锌、微粒和超微粒氧化锌、氧化铝、二氧化硅、热解法二氧化硅(超微粒二氧化硅)、云母钛、鱼鳞箔、氮化硼、光致变色颜料、合成氟金云母、微粒复合粉体、金、银、铂、铝等各种大小、形状的无机粉体、和将它们用氢有机硅、环状氢有机硅等有机硅或其它硅烷或钛偶联剂等各种表面处理剂进行处理而进行了疏水化或亲水化的粉体等无机粉体;淀粉、纤维素、尼龙粉末、聚乙烯末、聚甲基丙烯酸甲酯末、聚苯乙烯末、苯乙烯与丙烯酸的共聚物树脂粉末、聚酯末、苯胍胺树脂粉末、聚对苯二甲酸乙二醇酯-聚甲基丙烯酸甲酯层压末、聚对苯二甲酸乙二醇酯-铝-环氧层压末等、氨基甲酸酯粉末、有机硅粉末、Teflon(注册商标)粉末等各种大小、形状的有机系粉体和表面处理粉体、有机无机复合粉体作为优选的例子。
作为无机盐类,可举出食盐、粗盐、岩盐、海盐、天然盐等含有氯化钠的盐类;氯化钾、氯化铝、氯化钙、氯化镁、盐卤、氯化锌、氯化铵;硫酸钠、硫酸铝、硫酸铝钾(明矾)、硫酸铝铵、硫酸钡、硫酸钙、硫酸钾、硫酸镁、硫酸锌、硫酸铁、硫酸铜;磷酸一钠、磷酸二钠、磷酸三钠等磷酸钠类、磷酸钾类、磷酸钙类、磷酸镁类作为优选的例子。
作为紫外线吸收剂,可举出对氨基苯甲酸、对氨基苯甲酸单甘油酯、N,N-二丙氧基对氨基苯甲酸乙酯、N,N-二乙氧基对氨基苯甲酸乙酯、N,N-二甲基对氨基苯甲酸乙酯、N,N-二甲基对氨基苯甲酸丁酯、N,N-二甲基对氨基苯甲酸甲酯等苯甲酸系紫外线吸收剂;N-乙酰邻氨基苯甲酸高孟酯等邻氨基苯甲酸系紫外线吸收剂;水杨酸及其钠盐、水杨酸戊酯、水杨酸孟酯、水杨酸高孟酯、水杨酸辛酯、水杨酸苯酯、水杨酸苄酯、对异丙醇苯基水杨酸酯等水杨酸系紫外线吸收剂;肉桂酸辛酯、乙基-4-异丙基肉桂酸酯、甲基-2,5-二异丙基肉桂酸酯、乙基-2,4-二异丙基肉桂酸酯、甲基-2,4-二异丙基肉桂酸酯、丙基-对甲氧基肉桂酸酯、异丙基-对甲氧基肉桂酸酯、异戊基-对甲氧基肉桂酸酯、2-乙基己基-对甲氧基肉桂酸酯(对甲氧基肉桂酸辛酯)、2-乙氧基乙基-对甲氧基肉桂酸酯(桂醚酯)、环己基-对甲氧基肉桂酸酯、乙基-α-氰基-β-苯基肉桂酸酯、2-乙基己基-α-氰基-β-苯基肉桂酸酯(奥克立林)、甘油基单-2-乙基己酰-二对甲氧基肉桂酸酯、阿魏酸及其衍生物等肉桂酸系紫外线吸收剂;2,4-二羟基二苯甲酮、2,2’-二羟基-4-甲氧基二苯甲酮、2,2’-二羟基-4,4’-二甲氧基二苯甲酮、2,2’,4,4’-四羟基二苯甲酮、2-羟基-4-甲氧基二苯甲酮(羟苯甲酮-3)、2-羟基-4-甲氧基-4’-甲基二苯甲酮、2-羟基-4-甲氧基二苯甲酮-5-磺酸盐、4-苯基二苯甲酮、2-乙基己基-4’-苯基-二苯甲酮-2-甲酸酯、2-羟基-4-正辛氧基二苯甲酮、4-羟基-3-羧基二苯甲酮等二苯甲酮系紫外线吸收剂;3-(4’-甲基亚苄基)-d,l-樟脑、3-亚苄基-d,l-樟脑;2-苯基-5-甲基苯并唑;2,2’-羟基-5-甲基苯基苯并三唑;2-(2’-羟基-5’-叔辛基苯基)苯并三唑;2-(2’-羟基-5’-甲基苯基苯并三唑;二苄连氮(ジベンザラジン);二茴香酰甲烷;5-(3,3-二甲基-2-亚降冰片基)-3-戊烷-2-酮;4-叔丁基甲氧基二苯甲酰甲烷等二苯甲酰甲烷衍生物;辛基三嗪酮;尿刊酸和尿刊酸乙酯等尿刊酸衍生物;2-(2’-羟基-5’-甲基苯基)苯并三唑、1-(3,4-二甲氧基苯基)-4,4-二甲基-1,3-戊烷二酮、二甲氧基亚苄基二氧代咪唑烷丙酸2-乙基己酯等乙内酰脲衍生物、苯基苯并咪唑磺酸、对苯二亚甲基二樟脑磺酸、甲酚曲唑三硅氧烷、邻氨基苯甲酸甲酯、卢丁及其衍生物、谷维醇及其衍生物作为优选的例子。
作为美白剂,可举出熊果苷、α-熊果苷等氢醌糖苷及其酯类;抗坏血酸、抗坏血酸磷酸酯钠盐和抗坏血酸磷酸酯镁盐等抗坏血酸磷酸酯盐、抗坏血酸四异棕榈酸酯等抗坏血酸脂肪酸酯、抗坏血酸乙基醚等抗坏血酸烷基醚、抗坏血酸-2-葡糖苷等抗坏血酸葡糖苷及其脂肪酸酯类、抗坏血酸硫酸酯、磷酸生育酚抗坏血酸酯等抗坏血酸衍生物;曲酸、鞣花酸、凝血酸及其衍生物、阿魏酸及其衍生物、胎盘提取物、谷胱甘肽、谷维醇、丁基间苯二酚、油溶性洋甘菊提取物、油溶性甘草提取物、西河柳提取物、虎耳草提取物等植物提取物、4-正丁基间苯二酚(rucinol)、亚油酸S(リノレックS)、4-甲氧基水杨酸钾盐、腺苷-磷酸二钠、5,5’-二丙基-联苯-2,2’-二醇(厚朴木酚素)、右泛醇W、凝血酸鲸蜡基酯盐酸盐、杜鹃醇作为优选的例子。
作为维生素类及其衍生物类,可举出视黄醇、乙酸视黄醇酯、棕榈酸视黄醇酯等维生素A类;硫胺盐酸盐、硫胺硫酸盐、核黄素、乙酸核黄素、盐酸吡哆素、吡哆素二辛酸酯、吡哆素二棕榈酸酯、黄素腺嘌呤二核苷酸、氰钴胺素、叶酸类、烟酰胺、烟酸苄酯等烟酸类、胆碱类等维生素B群类;抗坏血酸及其钠等的盐等维生素C类;维生素D;α、β、γ、δ-生育酚等维生素E类;泛酸、生物素等其它维生素类;抗坏血酸磷酸酯钠盐和抗坏血酸磷酸酯镁盐等抗坏血酸磷酸酯盐、抗坏血酸四异棕榈酸酯、硬脂酸抗坏血酸酯、棕榈酸抗坏血酸酯、二棕榈酸抗坏血酸酯等抗坏血酸脂肪酸酯、抗坏血酸乙基醚等抗坏血酸烷基醚、抗坏血酸-2-葡糖苷等抗坏血酸葡糖苷及其脂肪酸酯、磷酸生育酚抗坏血酸酯等抗坏血酸衍生物;烟酸生育酚酯、乙酸生育酚酯、亚油酸生育酚酯、阿魏酸生育酚酯、生育酚磷酸酯等生育酚衍生物等维生素衍生物、生育三烯酚、其它各种维生素衍生物类作为优选的例子。
作为育毛用药剂、血液循环促进剂、刺激剂,可举出日本当药提取物、辣椒酊、生姜酊、生姜提取物、斑蝥酊等植物提取物、酊类;辣椒素、壬酸香草酰胺、姜油酮、鱼石脂、丹宁酸、龙脑、环扁桃酯、桂利嗪、妥拉唑啉、乙酰胆碱、维拉帕米、千金藤碱、γ-谷维醇、维生素E和烟酸生育酚酯、乙酸生育酚酯等衍生物、γ-谷维醇、烟酸和烟酰胺、烟酸苄基酯、肌醇六烟酸酯、烟醇等衍生物、尿囊素、感光素301、感光素401、卡普氯铵、十五烷酸单甘油酯、黄烷酮醇衍生物、豆固醇或豆甾烷醇及其糖苷、米诺地尔、国际公开第2005/085241号的说明书所记载的ALK5抑制化合物、国际公开第2003/086334号的说明书所记载的WNT-5A抑制化合物作为优选的例子。
作为白发预防剂,可举出日本萍蓬草、无患子、虎耳草、和普通百里香作为优选的例子。
作为激素类,可举出雌二醇、雌酮、炔雌醇、可的松、氢化可的松、泼尼松等作为优选的例子。
作为抗皱剂、抗老化剂、紧致剂、冷感剂、温感剂、创伤治愈促进剂、刺激缓和剂、镇痛剂、细胞赋活剂等其它药效剂,可举出视黄醇类、视黄酸类、视黄酸生育酚酯;乳酸、乙醇酸、葡糖酸、水果酸、水杨酸及其糖苷、酯化物等衍生物、羟基癸酸、长链α-羟基脂肪酸、长链α-羟基脂肪酸胆甾醇酯等α-或β-羟基酸类及其衍生物类;γ-氨基丁酸、γ-氨基-β-羟基丁酸;肉碱;肌肽;肌酸;神经酰胺类、神经鞘氨醇类;咖啡因、黄嘌呤等及其衍生物;辅酶Q10、胡萝卜素、番茄红素、虾青素、叶黄素、α-硫辛酸、铂纳米胶体、富勒烯类等抗氧化、活性氧清除剂;儿茶素类;五羟黄酮等黄酮类;异黄酮类;没食子酸和酯糖衍生物;丹宁、芝麻素、原花色素(プロトアントシアニジン)、绿原酸、苹果多酚等多酚类;卢丁和糖苷等衍生物;橙皮苷和糖苷等衍生物;木酚素糖苷;光甘草定、光甘草素、甘草根亭、异甘草根亭等甘草提取物相关物质;乳铁蛋白;姜烯酚、姜醇;薄荷醇、柏木脑等香料物质及其衍生物;辣椒素、香草醛等及衍生物;二乙基甲苯甲酰胺等昆虫驱避剂;生理活性物质与环糊精类的复合体作为优选的例子。
作为植物、动物、微生物提取物类,可举出鸢尾提取物、咸草提取物、罗汉柏提取物、石刁柏提取物、鳄梨提取物、绣球提取物、杏树提取物、蜀葵提取物、山生阿尼菊提取物、芦荟提取物、杏提取物、杏仁提取物、银杏提取物、茵陈蒿提取物、茴香提取物、姜黄提取物、乌龙茶提取物、熊果叶提取物、野蔷薇果提取物、紫松果菊叶提取物、蓝香茶菜提取物、黄芩提取物、黄檗提取物、黄连提取物、大麦提取物、高丽参提取物、小连翘提取物、野芝麻提取物、红芒柄花提取物、水芹提取物、橙提取物、海水干燥物、海藻提取物、柿叶提取物、火棘提取物、水解弹性蛋白、水解小麦粉、水解丝蛋白、葛根提取物、洋甘菊提取物、油溶性洋甘菊提取物、胡萝卜提取物、艾蒿提取物、野燕麦提取物、玫瑰茄提取物、甘草提取物、油溶性甘草提取物、猕猴桃提取物、奇应(キオウ)提取物、木耳提取物、金鸡纳树提取物、黄瓜提取物、桐叶提取物、鸟苷、番石榴提取物、苦参(クジン)提取物、栀子提取物、大叶竹提取物、苦参(クララ)提取物、胡桃提取物、栗子提取物、葡萄柚提取物、铁线莲提取物、黑米提取物、黑砂糖提取物、黑醋、小球藻提取物、桑提取物、黄龙胆根提取物、尼泊尔老鹳草提取物、红茶提取物、酵母提取物、厚朴提取物、咖啡提取物、牛蒡提取物、米提取物、米发酵提取物、米糠发酵提取物、米胚芽油、聚合草提取物、胶原、越橘提取物、细辛提取物、柴胡提取物、脐带提取液、藏红花提取物、鼠尾草提取物、肥皂草提取物、细竹提取物、山楂提取物、芫荽提取物、花椒提取物、香菇提取物、地黄提取物、紫草根提取物、紫苏提取物、椴树提取物、蚊子草提取物、孪叶豆提取物、芍药提取物、生姜提取物、菖蒲根提取物、白桦提取物、白木耳提取物、问荆提取物、甜叶菊提取物、甜叶菊发酵物、西河柳提取物、洋常春藤提取物、西洋山楂提取物、西洋接骨木提取物、西洋蓍提取物、西洋薄荷提取物、鼠尾草提取物、锦葵提取物、川芎提取物、日本当药提取物、桑白皮提取物、大黄提取物、大豆提取物、大枣提取物、百里香提取物、蒲公英提取物、地衣类提取物、茶提取物、丁香提取物、白茅提取物、陈皮提取物、茶树油、甜茶提取物、辣椒提取物、当归提取物、唐金盏花提取物、桃仁提取物、橙皮提取物、蕺菜提取物、番茄提取物、纳豆提取物、胡萝卜提取物、大蒜提取物、野蔷薇提取物、木槿提取物、麦冬提取物、莲提取物、荷兰芹提取物、桦树提取物、蜂蜜、金缕梅提取物、墙草提取物、蓝香茶菜提取物、红没药醇、日本扁柏提取物、双歧杆菌提取物、枇杷提取物、款冬提取物、款冬花茎提取物、茯苓提取物、假叶树提取物、葡萄提取物、葡萄籽提取物、蜂胶、丝瓜提取物、红花提取物、薄荷提取物、南京椴提取物、牡丹提取物、啤酒花提取物、玫瑰花提取物、松提取物、欧洲七叶树提取物、观音莲提取物、无患子提取物、蜜蜂花提取物、海蕴提取物、桃提取物、矢车菊提取物、桉提取物、虎耳草提取物、香橙提取物、百合提取物、薏苡仁提取物、艾蒿提取物、薰衣草提取物、绿茶提取物、蛋壳膜提取物、苹果提取物、南非博士茶提取物、灵芝提取物、莴苣提取物、柠檬提取物、连翘提取物、紫云英提取物、玫瑰提取物、迷迭香提取物、果香菊提取物、蜂王浆提取物、地榆提取物等提取物作为优选的例子。
作为止痒剂,可举出盐酸苯海拉明、马来酸氯苯那敏、樟脑、P物质抑制剂等。
作为角质剥离、溶解剂,可举出水杨酸、硫、间苯二酚、硫化硒、吡哆素等。
作为抑汗剂,可举出碱式氯化铝、氯化铝、氧化锌、对苯酚磺酸锌等。
作为清凉剂,可举出薄荷醇、水杨酸甲酯等。
作为收敛剂,可举出柠檬酸、酒石酸、乳酸、硫酸铝钾、丹宁酸等。
作为酶类,可举出超氧化物歧化酶、过氧化氢酶、氯化溶菌酶、脂肪酶、木瓜蛋白酶、胰酶、蛋白酶等。
作为核酸类,可举出核糖核酸及其盐、脱氧核糖核酸及其盐、腺苷三磷酸二钠作为优选的例子。
作为香料,可举出乙酰柏木烯、戊基肉桂醛、烯丙基戊基甘醇酸酯、β-芷香酮、龙涎酮(Iso E Super)、异丁基喹啉、鸢尾油、鸢尾酮、吲哚、依兰依兰油、十一烷醛、十一烯醛、γ-十一烷酸内酯、蒿脑、丁子香酚、橡苔、红没药香膏、橙油、丁子香酚、橙花素、加乐麝香(ガラクソリツド)、香芹酚、L-香芹酮、樟脑、キャノン、胡萝卜籽油、丁香油、肉桂酸甲酯、香叶醇、香叶腈、乙酸异冰片酯、乙酸香叶酯、乙酸二甲基苄基烃甲基酯、乙酸苏合香酯、乙酸柏木酯、乙酸萜品酯、乙酸对叔丁基环己酯、乙酸香根酯、乙酸苄酯、乙酸里哪酯、水杨酸异戊酯、水杨酸苄酯、檀香木油、檀香醇、仙客来醛、环十五烷内酯、二氢茉莉酮酸甲酯、二氢月桂烯醇、茉莉净油、茉莉内酯、顺-茉莉酮、柠檬醛、香茅醇、香茅醛、桂皮油、1,8-桉树脑、肉桂醛、苏合香香膏、雪松油、柏木烯、柏木脑、芹菜籽油、百里香油、二氢大马酮、大马烯酮、百里酚、晚香玉净油、癸醛、癸内酯、萜品醇、γ-萜品烯、2,4-二甲基-3-环己烯-1-甲醛(トリプラール,triplal)、橙花醇、壬醛、2,6-壬二烯醇、壬内酯、广藿香醇、香子兰净油、香草醛、罗勒油、广藿香油、羟基香茅醛、α-蒎烯、薄荷酮、苯乙醇、苯基乙醛、橙叶油、己基肉桂醛、顺-3-己烯醇、秘鲁香脂、岩兰油、岩兰草醇、薄荷油、胡椒油、胡椒醛、香柠檬油、苯甲酸苄酯、龙脑、水松香膏、麝香酮、甲基壬基乙醛、γ-甲基紫罗兰酮、薄荷醇、L-薄荷醇、L-薄荷酮、桉油、β-紫罗兰酮、酸橙油、薰衣草油、D-柠檬烯、芳樟醇、新铃兰醛(リラール,lyral)、铃兰醛、柠檬油、玫瑰净油、玫瑰醚、玫瑰油、迷迭香油、各种精油等合成香料和天然香料以及各种调合香料作为优选的例子。
作为色素、着色剂、染料,可举出褐色201号、黑色401号、紫色201号、紫色401号、蓝色1号、蓝色2号、蓝色201号、蓝色202号、蓝色203号、蓝色204号、蓝色205号、蓝色403号、蓝色404号、绿色201号、绿色202号、绿色204号、绿色205号、绿色3号、绿色401号、绿色402号、红色102号、红色104-1号、红色105-1号、红色106号、红色2号、红色201号、红色202号、红色203号、红色204号、红色205号、红色206号、红色207号、红色208号、红色213号、红色214号、红色215号、红色218号、红色219号、红色220号、红色221号、红色223号、红色225号、红色226号、红色227号、红色228号、红色230-1号、红色230-2号、红色231号、红色232号、红色3号、红色401号、红色404号、红色405号、红色501号、红色502号、红色503号、红色504号、红色505号、红色506号、橙色201号、橙色203号、橙色204号、橙色205号、橙色206号、橙色207号、橙色401号、橙色402号、橙色403号、黄色201号、黄色202-1号、黄色202-2号、黄色203号、黄色204号、黄色205号、黄色4号、黄色401号、黄色402号、黄色403-1号、黄色404号、黄色405号、黄色406号、黄色407号、黄色5号等法定色素;酸性红14等其它酸性染料;赭棕(Arianor SiennaBrown)、鲜红(Arianor Madder Red)、钢青(Arianor Steel Blue)、草黄(Arianor StrawYellow)等碱性染料;HC黄2(HC Yellow 2)、HC黄5(HC Yellow 5)、HC红(HC Red)3,4-羟基丙基氨基-3-硝基苯酚、N,N’-双(2-羟基乙基)-2-硝基对苯二胺、HC蓝2(HC Blue 2)、碱性蓝26等硝基染料;分散染料;虾青素、茜素等蒽醌类、花色素、β-胡萝卜素、色素(カテナール)、辣椒红、查耳酮、红花素、五羟黄酮、藏花素、叶绿素、姜黄素、胭脂虫红、紫草宁等萘醌类、红木素、黄酮类、甜菜红素(ベタシアニジン)、指甲花、血红蛋白、番茄红素、核黄素、卢丁等天然色素、染料;对苯二胺、甲苯-2,5-二胺、邻氨基苯酚、间氨基苯酚、对氨基苯酚、间苯二胺、5-氨基-2-甲基苯酚、间苯二酚、1-萘酚、2,6-二氨基吡啶等及其盐等氧化染料中间体和成色剂;二氢吲哚等自动氧化型染料;二羟基丙酮作为优选的例子。
作为消炎剂、抗炎剂,可举出甘草酸及其衍生物、甘草亭酸衍生物、水杨酸衍生物、4-异丙基环庚三烯酚酮、愈创薁、尿囊素、吲哚美辛、酮洛芬、布洛芬、双氯芬酸、洛索洛芬、塞来考昔、英利昔单抗、依那西普、氧化锌、乙酸氢化可的松、泼尼松、盐酸苯海拉明、马来酸氯苯那敏;桃叶提取物、艾蒿叶提取物等植物提取物作为优选的例子。
作为抗哮喘、抗慢性阻塞性肺疾病、抗变态反应、免疫调节剂,可举出氨茶碱、茶碱类、类固醇类(氟替卡松、倍氯米松等)、白细胞三烯拮抗药类、血栓素抑制药类、色甘酸钠(インタール)、β2刺激药类(福莫特罗、沙美特罗、沙丁胺醇、妥洛特罗、克仑特罗、肾上腺素等)、噻托铵(チオトロピウム)、异丙托铵(イプラトロピウム)、右美沙芬、二甲啡烷、溴己新、曲尼司特、酮替芬、氮卓斯汀、西替利嗪、氯苯那敏、美喹他嗪、他克莫司、环孢素、西罗莫司、甲氨蝶呤、细胞因子调节剂类、干扰素、奥马珠单抗、蛋白/抗体制剂作为优选的例子。
作为抗感染症剂、抗真菌剂,可举出奥塞米韦和扎那米韦、伊曲康唑作为优选的例子。此外,可以以公知的组合和混配比/混配量含有化妆品原料基准、化妆品种别混配成分标准、日本化妆品工业联合会成分表示名称目录、INCI辞典(The International CosmeticIngredient Dictionaryand Handbook,国际化妆品成分词典和手册)、准药品原料标准、日本药典、药品添加物标准、食品添加物公定书等所记载的成分、和属于国际专利分类IPC为A61K7和A61K8的分类的日本和各外国专利公报和专利公开公报(包含公表公报、再公表)所记载的成分等公知的化妆品成分、药品成分、食品成分等。
需要说明的是,本发明的组合物只要可以在皮肤上或毛发表面形成膜(层),其剂型就是任意的。
可以举出例如,水包油(O/W)型、油包水(W/O)型、W/O/W型、O/W/O型等乳化型、油性、固体、液状、膏状、棒状、挥发性油型、粉状、胶质状、凝胶、糊状、乳化高分子型、片状、雾状、喷雾型等,但不限定于它们。此外其制品形态也是任意的,可以作为分散液、乳液、霜、面膜、喷雾、凝胶等而使用。
上述组合物根据其剂型/制品形态,为了实现上述剂型/制品形态,可以混配本领域技术人员已知的各种成分。
[组合物的制造方法]
本发明的组合物,例如,能够通过将至少1种脂质肽型化合物、蔗糖酯、水和根据需要的其它成分一边加热一边混合、搅拌后,静置放冷直到室温左右来制造。
关于上述加热/搅拌温度,只要各成分可以均匀地混合,就没有特别限定,例如搅拌温度在50℃~90℃、60℃~90℃,例如70℃、或80℃下,此外搅拌时间例如可以在5分钟~3小时之间适当选择。
此外本发明涉及防止皮肤表面或毛发表面污染的方法,其包含下述工序:在皮肤表面或毛发表面形成由含有上述脂质肽型化合物和蔗糖酯的组合物形成的膜的膜形成工序。
进一步本发明涉及防止尘埃、花粉、粒子状物质、螨(包含尸体)、气态物质、或臭气物质向皮肤表面或毛发表面附着的方法,其包含下述工序:在皮肤表面或毛发表面形成由含有上述脂质肽型化合物和蔗糖酯的组合物形成的膜的膜形成工序。
在上述防止皮肤表面或毛发表面污染的方法以及防止尘埃、花粉、粒子状物质、螨(包含尸体)、气态物质、或臭气物质向皮肤表面或毛发表面附着的方法中使用的组合物可以使用先前详述的物质。
由本发明的组合物形成的膜通过在皮肤、毛发的表面形成适度的粗糙度(以下,也称为不平度),来表现防止皮肤、毛发的表面污染的效果。不平度由相对于皮肤、毛发的表面的、垂直方向的高度的最大值与最低值的幅度表示,作为其测定方法,可举出例如,原子力显微镜(AFM)。
关于由本发明中的组合物形成的膜所形成的粗糙度,例如,平均表面粗糙度为3nm~500nm,更优选为10nm~300nm。
由本发明中的组合物形成的膜通过纤维结构而形成,其平均直径优选为10nm~100nm。需要说明的是,纤维的平均直径通过使用扫描型显微镜来检测二次电子从而可以制作膜的表面的图像,由该膜的表面的图像算出。
实施例
以下,举出实施例和试验例作为例子而详细地说明本发明,但本发明不限定于这些例子。
[合成例1:脂质肽(N-棕榈酰-Gly-His)的合成]
在本实施例中,作为胶凝剂而使用的脂质肽通过以下所示的方法来合成。
在500mL的4口烧瓶中投入组氨酸14.2g(91.6mmol)、N-棕榈酰-Gly-甲酯30.0g(91.6mmol)、甲苯300g,加入作为碱的甲醇钠28%甲醇溶液35.3g(183.2mmol),用油浴加热到60℃而继续搅拌1小时。然后,去除油浴,放冷直到25℃,用丙酮600g使该溶液再沉淀,滤取。将这里获得的固体溶解于水600g与甲醇750g的混合溶液,在其中加入6当量盐酸30.5ml(183.2mmol)进行中和而使固体析出,过滤。接下来,使所得的固体在60℃下溶解于四氢呋喃120g与水30g的混合液,加入乙酸乙酯150g,从60℃冷却直到30℃。然后,将析出的固体过滤。进一步将所得的固体溶解在四氢呋喃120g和乙腈60g溶剂中,加热到60℃,搅拌1小时后冷却,过滤。将这里获得的固体用水120g洗涤,在过滤后进行减压干燥而获得了N-棕榈酰-Gly-His游离体(以下,也简称为Pal-GH)的白色的结晶26.9g(收率65%)。
[实施例1~实施例7、比较例1:使用了各种糖类的Pal-GH组合物的调制]
在200mL烧杯(HARIO株式会社制)中,将在上述合成例中获得的Pal-GH、各种糖活性剂、其它成分以成为表1所示的组成(质量:g)的方式称量而投入,在设定温度约80℃的水浴中在20分钟150rpm的条件下加热搅拌,获得了Pal-GH组合物。
此外,关于80℃加热搅拌后的组合物中的Pal-GH的分散性,将Pal-GH的粉末在组合物中均匀地分散了(不产生析出、粉的块)的情况设为O,将Pal-GH不均匀地分散了(产生析出、粉的块)的情况设为×,通过目视进行了评价。将所得的结果一并示于表1中。
[表1]
表1
※1:1,2-己二醇:(株)アイ·テイー·才ー制[商品名:Hydrolite6-0]
※2:硬脂酸:花王(株)制[商品名:ル产ツクS-98]
※3:山梨糖醇:纯正化学(株)制
※4:甘露糖醇:纯正化学(株)制
※5:海藻糖(株)林原[商品名:トレハ]
※6:葡萄糖:东京化成工业(株)制
※7:胍基乙酸:东京化成工业(株)制
※8:蔗糖月桂酸酯:ケミ力ルフ一ズ(株)制[商品名:リヨートーシユガー工ステルLー1695]
※9:月桂基葡糖苷:花王(株)制[商品名:マイド一ル12]
[实施例8~实施例14、比较例2:Pal-GH组合物的水分散液调制]
在200mL烧杯(HARIO株式会社制)中,使用在上述实施例1~实施例7中获得的Pal-GH组合物,调制出表2所示的组成的Pal-GH水分散液。以成为表2所示的组成(质量:g)的方式称量A相和B相,在设定温度约80℃的水浴中将A相和B相加热直到变为70℃以上为止。然后,对加热搅拌着的B相投入A相,在5分钟150rpm的条件下进行加热搅拌,获得了Pal-GH水分散液。
此外,关于调制出的Pal-GH水分散液的评价,将Pal-GH在水中均匀地分散了(未产生析出、凝集)的情况设为O,将Pal-GH在水中不均匀地分散了(产生析出、凝集)的情况设为×,通过目视进行了评价。将所得的结果一并示于表2中。
[表2]
表2
※1:1,2-己二醇:(株)アイ·テイー·才ー制[商品名:Hydrolite6-O]
※2:硬脂酸:花王(株)制[商品名:ル产ツクS-98]
※3:山梨糖醇:纯正化学(株)制
※4:甘露糖醇:纯正化学(株)制
※5:海藻糖:(株)林原[商品名:トレハ]
※6:葡萄糖:东京化成工业(株)制
※7:胍基乙酸:东京化成工业(株)制
※8:蔗糖月桂酸酯:三菱ケミ力ルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ステルL-1695]
※9:月桂基葡糖苷:花王(株)制[商品名:マイドール12]
[实施例15~实施例21:组合了蔗糖脂肪酸酯的Pal-GH组合物的调制]
在200mL烧杯(HARIO株式会社制)中,将在上述合成例中获得的Pal-GH、2种蔗糖脂肪酸酯、其它成分以成为表3所示的组成(质量:g)的方式称量而投入,在设定温度约80℃的水浴中在20分钟150rpm的条件下加热搅拌,获得了Pal-GH组合物。
此外,关于80℃加热搅拌后的组合物中的Pal-GH的分散性,将Pal-GH的粉末在组合物中均匀地分散了(未产生析出、粉的块)的情况设为○,将Pal-GH不均匀地分散了(产生析出、粉的块)的情况设为×,通过目视进行了评价。将所得的结果一并示于表3中。
[表3]
表3
※1:1,2-己二醇:(株)アイ·テイ一·才一制[商品名:Hydrolite6-○]
※2:硬脂酸:花王(株)制[商品名:ルナックS-98]
※3:蔗糖月桂酸酯(L-1695):三菱ケミカルフーズ(株)制[商品名:リヨートーシユガー工ステルL-1695]
※4:蔗糖月桂酸酯(L-595):三菱ケミカルフーズ(株)制[商品名:リヨートーシユガー工ステルL-595]
[实施例22~实施例28:Pal-GH组合物的水分散液调制]
在200mL烧杯(HARIO株式会社制)中,使用在上述实施例15~实施例21中获得的Pal-GH组合物,调制出表4所示的组成的Pal-GH水分散液。以成为表4所示的组成(质量:g)的方式称量A相和B相,在设定温度约80℃的水浴中将A相和B相加热直到变为70℃以上。然后,对加热搅拌着的B相投入A相,在5分钟150rpm的条件下进行加热搅拌,获得了Pal-GH水分散液。
此外,关于调制出的Pal-GH水分散液的评价,将Pal-GH在水中均匀地分散了(未产生析出、凝集)的情况设为O,将Pal-GH在水中不均匀地分散的情况(产生析出、凝集)的情况设为×,通过目视进行了评价。将所得的结果一并示于表4中。
[表4]
表4
※1:1,2-己二醇:(株)アイ·テイー·才ー制[商品名:Hydrolite6-○]
※2:硬脂酸:花王(株)制[商品名:ル产ツクS-98]
※3:蔗糖月桂酸酯(L-1695):三菱ケミカルフ一ブ(株)制[商品名:リヨ一ト一シユガ一工ステルL-1695]
※4:蔗糖月桂酸酯(L-595):三菱ケミカルフーズ(株)制[商品名:リヨ一ト一シユガ一工ステルL一595]
[实施例22~实施例27、比较例3:Pal-GH组合物水分散液的PM2.5粒子附着抑制]
将人造皮革サプラ一レ(出光テクノフアイン株式会社制)进行4cm2见方切断,涂布比较例3和实施例22~实施例27的溶液各1.0mL,用32℃的恒温槽干燥了1小时。
在16cm2见方的称量皿中,加入PM2.5粒子(NIES-CRMNo.都市大气粉尘)1.5g,使上述制作出的各サプラ一レ与PM2.5粒子接触并用镊子按压10次,提拉后摇动10秒从而使过剩附着的PM2.5粒子落下后,将附着于各サプラ一レ的PM2.5粒子通过显微镜VHX-2000(株式会社Keyence制)进行了观察。将关于实施例24、27和比较例3的结果示于图1中。此外,将实施例22~27和比较例3的观察到的图像中的PM2.5粒子通过图像处理进行着色,算出了着色部分相对于图像整体的面积率,将所得的结果示于图2中。
[实施例22~实施例27、比较例3:Pal-GH组合物水分散液的雪松花粉附着抑制]
将人造皮革サプラーレ(出光テクノファイン株式会社制)进行4cm2见方切断,涂布比较例3和实施例22~实施例27的溶液各1.0mL,用32℃的恒温槽干燥了1小时。
在16cm2见方的称量皿中,加入雪松花粉(ITEA株式会社制)1.5g,使上述制作出的各サプラーレ与花粉接触并用镊子按压10次,提拉后摇动10秒从而使过剩附着的花粉落下后,将附着在各サプラーレ的花粉使用ITEA雪松花粉变应原(Cryj1)ELISA试剂盒进行了定量。将结果示于图3中。此外,图4中显示在实施例22、24、比较例3中附着了的雪松花粉的扫描型电子显微镜(SEM)[Miniscope(注册商标)TM3000((株)日立ハイテクノロジーズ制)]观察结果。
[实施例29~实施例34、比较例3:Pal-GH组合物的皮肤渗透促进效果]
将人三维培养表皮模型(LabCyte EPI-MODEL12,φ10.5mm,批号#LCE12-200706-A,株式会社ジャパン·ティッシュ·エンジニアリング制)设置于12孔组织培养板(IWAKI,旭硝子株式会社制),在各孔中分注1mL的磷酸缓冲生理食盐液(pH7.4)(PBS),将其设为接收液。在供给侧,添加按照表5而调制出的、1%烟酰胺(Sigma Ardrich制)混配Pal-GH水分散液各500μL,盖上组织培养板的盖,在37℃的培养箱内静置从而实施了皮肤透过性试验。添加实施例29~34和比较例3的Pal-GH分散液而透过3小时后,采取接收液和三维培养表皮模型。将采取了的三维培养表皮模型用500μL的PBS洗涤3次,4等分地用手术刀切断而投入到1.5mL微管(Eppendorf制)中。然后,加入甲醇/纯化水=1/1v/v提取液750μL用涡旋混合器(ケニス株式会社制)处理1小时,从而从三维培养表皮模型提取烟酰胺,用孔径0.45μm针头式过滤器(メルク制)进行了过滤处理。通过高效液相色谱(HPLCAgilent制)测定所得的过滤液和接收液中的烟酰胺浓度,从而算出了每单位面积的烟酰胺皮肤透过量。试验各检体各进行3次,算出它们的平均值,由该值算出了透过3小时后的皮肤透过量。HPLC测定条件如以下那样。
检测器:紫外吸光光度计(测定波长:260nm),柱:在内径4.6mm、长度25cm的不锈钢管中填充3μm的HPLC用十八烷基甲硅烷基化硅胶而成的物质(ODS-4ジ一エルサイエンス株式会社),柱温度:40℃,流动相:0.1%乙酸水溶液/5mMICP-ALKS7水溶液:甲醇=9:1(v/v)
将所得的结果示于图5和图6中。图5显示从三维培养表皮模型提取到的烟酰胺,图6显示从储存器中检测到的烟酰胺量。
[表5]
表5
※1:1,2-己二醇:(株)アイ·テイ一·才一制[商品名:Hydrolite6-O]
※2:硬脂酸:花王(株)制[商品名:ル产ツクS-98]
※3:蔗糖月桂酸酯(L-1695):三菱ケミカル7一ブ(株)制[商品名:リヨ一ト一シユガ一工ステルL-1695]
※4:蔗糖月桂酸酯(L-595):三菱ケミカルフ一ズ(株)制[商品名:リヨ一ト一シユガー工ステルL-595]
[实施例35~实施例38、比较例l:包含蔗糖脂肪酸酯的Pal-GH组合物的调制]
在200mL烧杯(HARIO株式会社制)中,将在上述合成例1中获得的Pal-GH、各种糖活性剂、其它成分以成为表6所示的组成(质量:g)的方式称量而投入,在设定温度约80℃的水浴中在20分钟150rpm的条件下加热搅拌,获得了Pal-GH组合物。
此外,关于80℃加热搅拌后的组合物中的Pal-GH的分散性,将Pal-GH的粉末在组合物中均匀地分散了(未产生析出、粉的块)情况设为O,将Pal-GH不均匀地分散了的情况(产生析出、粉的决)的情况设为×,通过目视进行了评价。将所得的结果一并示于表6中。
[表6]
表6
※1:蔗糖月桂酸酯(L-1695):三菱ケミカルフーズ(株)制[商品名:リヨートーシユガー工ステルL-1695]
※2:蔗糖肉豆蔻酸酯(M-1695):三菱ケミカルフーズ(株)制[商品名:リョートーシユガー工ステルM-1 695]
※3:蔗糖棕榈酸酯(P-1670):三菱伊ミカルフーズ(株)制[商品名:リヨートーシユガー工ステルP-1670]
※4:蔗糖硬脂酸酯(S-1670):三菱ケミカルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ステルS-1670]
[实施例39~实施例42、比较例3:Pal-GH组合物的皮肤渗透促进效果]
将人三维培养表皮模型(LabCyte EPI-MODEL12,φ10.5mm,批号#LCE12-200817-A,株式会社ジヤパン·テイツシユ·エンジニアリング制)设置于12孔组织培养板(IWAKI,旭硝子株式会社制),在各孔中分注1mL的磷酸缓冲生理食盐液(pH7.4)(PBS),将其设为接收液。在供给侧,添加按照表7而调制出的、1%烟酰胺(Sigma Ardrich制)混配Pal-GH水分散液各500μL,盖上组织培养板的盖,在37℃的培养箱内静置从而实施了皮肤透过性试验。添加实施例39~42和比较例3的Pal-GH分散液而透过3小时后,采取接收液和三维培养表皮模型。将采取了的三维培养表皮模型用500μL的PBS洗涤3次,4等分地用手术刀切断而投入到1.5mL微管(Eppendorf制)中。然后,加入甲醇/纯化水=1/1v/v提取液750μL用涡旋混合器(ケニス株式会社制)处理1小时,从而从三维培养表皮模型提取烟酰胺,用孔径0.45μm针头式过滤器(メルク制)进行了过滤处理。通过高效液相色谱(HPLC Agilent制)测定所得的过滤液和接收液中的烟酰胺浓度,从而算出了每单位面积的烟酰胺皮肤透过量。试验各检体各进行3次,算出它们的平均值,由该值算出了透过3小时后的皮肤透过量。HPLC测定条件如以下那样。
检测器:紫外吸光光度计(测定波长:260nm),柱:在内径4.6mm、长度25cm的不锈钢管中填充3μm的HPLC用十八烷基甲硅烷基化硅胶而成的物质(ODS-4ジーエルサイエンス株式会社),柱温度:40℃,流动相:0.1%乙酸水溶液/5mMICP-ALKS7水溶液:甲醇=9:1(v/v)
将所得的结果示于图7和图8中。图7显示从三维培养表皮模型提取到的烟酰胺,图8显示从储存器中检测到的烟酰胺量。
[表7]
表7
※1:蔗糖月桂酸酯(L-1695):三菱ケミカルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ステルL-1695]
※2:蔗糖肉豆蔻酸酯(M-1695):三菱ケミカルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ステルM-1695]
※3:蔗糖棕榈酸酯(P-1670):三菱于ミ力ルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ステルP-1670]
※4:蔗糖硬脂酸酯(s-1670):三菱ケミカルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ZテルS-1 670]
[实施例43、实施例44、比较例4和比较例5:人造皮革中的花粉、PM2.5粒子和螨的附着抑制]
<检体的调制>
按照表8,在200mL烧杯(HARIO株式会社制)中将加热到75℃的各原料搅拌,在75℃中加热搅拌了10分钟。10分钟后,在室温下进行了搅拌冷却直到变为40℃为止。在以上工序中,搅拌全部以200rpm进行。
[表8]
表8
※1:大阪有机化学工业(株)制[商品名:KMO-6]
※2:三菱ケミカルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ステルL-1695]
※3:三菱ケミカルフ一ズ(株)制[商品名:リヨ一ト一シユガ一工ステルL-595]
※4:花王(株)制[商品名:ル产ツクS-98]
<人造皮革中的花粉的附着抑制>
将人造皮革サプラーレ(出光テクノフアイン株式会社制)切断为2cm×2cm的大小,涂布比较例4、比较例5、实施例43和实施例44的溶液各1.0mL,用32℃的恒温槽干燥了1小时。在10mL的实验室螺口管瓶中加入雪松花粉(ITEA制)1.5g,用上述制作出的各サプラ一レ盖上,使其反转而使其接触从而使花粉附着了。将附着了的花粉的目视的观察结果示于图9,将关于比较例4、实施例43和实施例44的使用ITEA雪松花粉变应原(Cryj1)ELISA试剂盒进行了定量的结果示于图10中。实施例43相对于比较例4和比较例5抑制了花粉的附着,实施例44中观察到该效果进一步高的情形,显示出具有抗污染效果。
<人造皮革中的PM2.5粒子的附着抑制>
将人造皮革サプラ一レ(出光テクノフアイン株式会社制)切断为2cm×2cm的大小,涂布比较例4、比较例5、实施例43和实施例44的溶液各1.0mL,用32℃的恒温槽干燥了1小时。
在4cm×4cm的称量皿中,加入PM2.5粒子(NIES-CRM No.都市大气粉尘)1.5g,使上述制作出的各サプラーレ与PM2.5粒子接触并用镊子按压10次,提拉后摇动10秒从而使过剩附着了的PM2.5粒子落下后,将附着于各サプラーレ的PM2.5粒子利用目视进行了观察,将所得的结果示于图11中。此外,在比较例4、和实施例44中,使用ICP-发射光谱分析装置将PM2.5粒子中所包含的金属元素进行定量,从而评价了PM2.5粒子的附着量。将结果示于图12中。实施例43相对于比较例4和比较例5抑制了PM2.5粒子的附着,实施例44中观察到该效果进一步高的情形,显示出具有抗污染效果。
<对人造皮革,将PM2.5粒子进行了压缩空气喷雾时的附着抑制>
将人造皮革サプラーレ(出光テクノファイン株式会社制)切断为2cm×2cm的大小,涂布比较例4和实施例44的溶液各1.0mL,用32℃的恒温槽干燥了1小时。对各サプラーレ使用压缩空气喷射了PM2.5粒子(NIES-CRM No.都市大气粉尘)各5.00mg(图13)。然后,回收サプラーレ,使用能量分散型荧光X射线分析装置EDX-8000(岛津制作所制),定量了PM2.5粒子中的硅。将结果示于图14中。实施例44相对于比较例4抑制了PM2.5粒子的附着,显示出具有抗污染效果。
<使组合物进行了喷雾后干燥的情况下的、人造皮革中的PM2.5粒子的附着抑制>
将人造皮革サプラーレ(出光テクノファイン株式会社制)切断为2cm×2cm的大小,将比较例5和实施例44的溶液从喷雾器容器喷雾,用32℃的恒温槽干燥了10分钟。需要说明的是,各溶液从喷雾器推压1次而喷雾。
在4cm×4cm的称量皿中,加入PM2.5粒子(NIES-CRM No.都市大气粉尘)1.5g,使上述制作出的各サプラーレ与PM2.5粒子接触并用镊子按压10次,提拉后摇动10秒从而使过剩附着了的PM2.5粒子落下后,使用ICP-发射光谱分析装置将PM2.5粒子中所包含的金属元素定量,从而评价了PM2.5粒子的附着量。将结果示于图15中。此外,在将实施例44的溶液进行了喷雾器喷雾的サプラーレ表面粘贴碳带从而将在サプラーレ上形成的膜剥离,通过场致发射形扫描电子显微镜JSM-7400F(日本电子株式会社制)观察了膜,将所得的结果示于图16中。实施例44相对于比较例5抑制了PM2.5粒子的附着,显示出具有抗污染效果。此外,确认到在将实施例44进行了喷雾器喷雾的サプラーレ,在表面形成有纤维状的膜。
<人造皮革中的粉尘螨的附着抑制>
将人造皮革サプラーレ(出光テクノファイン株式会社制)切断为2cm×2cm的大小,将比较例5和实施例44的溶液从喷雾器容器喷雾,用32℃的恒温槽干燥了10分钟。需要说明的是,各溶液从喷雾器推压1次而喷雾。
在10mL的实验室螺口管瓶中加入粉尘螨((株)ビオスタ)0.5g,用上述制作出的各サプラーレ盖上,使其反转而使其接触从而使花粉附着了。然后,使用ITEA螨(Derf1)高灵敏度ELISA试剂盒,将附着于サプラーレ的Derf1进行定量从而评价了粉尘螨附着量。将结果示于图17中。确认到实施例44的样品与比较例5相比抑制粉尘螨的附着。图18显示附着于サプラーレ的粉尘螨的照片。
<涂布膜的不平度测定>
涂布在比较例5和实施例44中调制出的溶液,用32℃的恒温槽干燥了10分钟。通过AFM原子力显微镜Dimension Icon(Bruker AXS制),测定了形成在硅晶片表面的膜的不平度,将所得的结果示于图19中。比较例5的不平度平均为0.80nm,与此相对,实施例44的不平度平均显示72.3nm的值。实施例44与比较例5相比显示大的不平度值,暗示出可以抑制污染物质附着。
[实施例45、比较例6:Pal-GH组合物的皮肤渗透促进效果]
·检体的调制
按照下述表9,在200mL烧杯(HARIO株式会社制)中将加热到75℃的各原料搅拌,在75℃中加热搅拌10分钟后将A相与B相混合,进一步加热搅拌了5分钟。然后,在室温下进行了搅拌冷却直到变为40℃为止。在以上工序中,搅拌全部以200rpm进行。
[表9]
表9
※1:1,2-己二醇:大阪有机化学工业(株)制[商品名:KMO-6]
※2:硬脂酸:花王(株)制[商品名:ルナツクS-98]
※3:蔗糖月桂酸酯:三菱ケミカルフーブ(株)制[商品名:リヨートーシユガーエステルL-1695]
※4:蔗糖月桂酸酯:三菱ケミカルーズ(株)制[商品名:リヨ一トーシコガーエステルL-595]
※5:甘油:阪本药品工业(株)制[商品名:化妆品用浓甘油]
※6:对羟基苯甲酸甲酯:丸善产业(株)制
※7:聚氧乙烯失水山梨糖醇单月桂酸酯:花王(株)制[商品名:レオールTW-L120]
※8:黄原胶:三晶(株)制[商品名:KELTROL CG-SF T]
※91,3-丁二醇:ダイセル(株)制
※10:透明质酸钠:キツコ一マンバイオケミフア(株)制[透明质酸FCH-150]
※11:视黄醇:Sigma Aldrich制
※12:乙醇:纯正化学(株)制
<使用了三维培养皮肤模型的皮肤渗透试验>
将人三维培养表皮模型(LabCyte EPI-MODEL12,φ10.5mm,批号#LCE12-201109-A,株式会社ジャパン·ティッシュ·エンジニアリング制)设置于12孔组织培养板(IWAKI,旭硝子株式会社制),在各孔中分注1mL的磷酸缓冲生理食盐液(pH7.4)(PBS),将其设为接收液。在供给侧,添加按照表9而调制出的、比较例6和实施例45的0.5%视黄醇混配溶液各500μL,盖上组织培养板的盖,在37℃的培养箱内静置从而实施了皮肤透过性试验。在透过24小时后,采取三维培养表皮模型。将采取了的三维培养表皮模型用500μL的乙醇洗涤3次,4等分地用手术刀切断而投入到1.5mL微管(Eppendorf制)中。然后,加入甲醇/纯化水=1/1v/v提取液750μL用涡旋混合器(ケニス株式会社制)处理1小时,从而从三维培养表皮模型提取视黄醇,用孔径0.45μm针头式过滤器(メルク制)进行了过滤处理。通过高效液相色谱(HPLCAgilent制)测定所得的过滤液的视黄醇浓度,从而算出了每单位面积的视黄醇皮肤透过量。试验各检体各进行3次,算出它们的平均值,由该值算出了透过24小时后的皮肤透过量。HPLC测定条件如以下那样。
检测器:紫外吸光光度计(测定波长:325nm),柱:在内径4.6mm、长度25cm的不锈钢管中填充3μm的HPLC用十八烷基甲硅烷基化硅胶而成的物质(ODS-4ジーエルサイエンス株式会社),柱温度:40℃,流动相:水:甲醇=5:95(v/v)
将所得的结果示于图20中。实施例45与比较例6相比显示出促进视黄醇的皮肤渗透。
[实施例46、比较例7:Pal-GH组合物的皮肤渗透促进效果]
·检体的调制
按照下述表10,在200mL烧杯(HARIO株式会社制)中将加热到75℃的各原料搅拌,在75℃中加热搅拌了10分钟后将A相与B相混合,进一步加热搅拌了5分钟。然后,在室温下进行了搅拌冷却直到变为40℃为止。在以上工序中,搅拌全部以200rpm进行。
[表10]
表10
※1:1,2-己二醇:大阪有机化学工业(株)制[商品名:KMO-6]
※2:硬脂酸:花王(株)制[商品名:ル产ツクS-98]
※3:蔗糖月桂酸酯:三菱ケミカルフーズ(株)制[商品名:リヨートーシユガー工ステルL-1695]
※4:蔗糖月桂酸酯:三菱ケミカルフーズ(株)制[商品名:ヨ一トーシユガー工ステルL-595]
※5:甘油:阪本药品工业(株)制[商品名:化妆品用浓甘油]
※6:1,3-丁二醇:ダイセル(株)制
※7:抗坏血酸2糖苷:Sigma A1drich制
※8:对羟基苯甲酸甲酯:丸善产业(株)制
※9:黄原胶:三晶(株)制[商品名:KELTROL CG-SFT]
※10:透明质酸钠:キツコ一ァンバイオケミフア(株)制[透明质酸FCH-150]
<使用了三维培养皮肤模型的皮肤渗透试验>
将人三维培养表皮模型(LabCyte EPI-MODEL12,φ10.5mm,批号#LCE12-201109-A,株式会社ジヤパン·テイツジユ·エンジ二アリング制)设置于12孔组织培养板(IWAKI,旭硝子株式会社制),在各孔中分注1mL的磷酸缓冲生理食盐液(pH7.4)(PBS),将其设为接收液。在供给侧,添加按照表10而调制出的、比较例7和实施例46的1.0%抗坏血酸糖苷混配溶液各500μL,盖上组织培养板的盖,在37℃的培养箱内静置从而实施了皮肤透过性试验。透过24小时后,采取三维培养表皮模型。将采取了的三维培养表皮模型用500μL的PBS洗涤3次,4等分地用手术刀切断而投入到1.5mL微管(Eppendorf制)中。然后,加入甲醇/纯化水=1/1v/v提取液750μL用涡旋混合器(ケニス株式会社制)处理1小时,从而从三维培养表皮模型提取抗坏血酸糖苷,用孔径0.45μm针头式过滤器(メルク制)进行了过滤处理。通过高效液相色谱(HPLC Agilent制)测定所得的过滤液的抗坏血酸糖苷浓度,从而算出了每单位面积的抗坏血酸糖苷皮肤透过量。试验各检体各进行3次,算出它们的平均值,从该值算出了透过24小时后的皮肤透过量。HPLC测定条件如以下那样。
检测器:紫外吸光光度计(测定波长:260nm),柱:在内径4.6mm、长度25cm的不锈钢管中填充3μm的HPLC用十八烷基甲硅烷基化硅胶而成的物质(ODS-4ジーエルサイエンス株式会社),柱温度:40℃,流动相:0.1%乙酸铵水溶液/ICP-TBA-Br水溶液:乙腈=4:1(v/v)
将所得的结果示于图21中。实施例46与比较例7相比显示出促进抗坏血酸糖苷的皮肤渗透。
[实施例47、实施例48和比较例8:人造皮革中的戈壁黄沙的附着抑制]
<检体的调制>
以下述表11所示的比例在200mL烧杯(HARIO株式会社制)中加入各原料,在液体温度75℃中加热搅拌10分钟,制成均匀溶液。在加热搅拌后,在室温下进行搅拌冷却直到液体温度变为40℃为止,调制出实施例47试样(以下,也称为处方例47)、实施例48试样(以下,也称为处方例48)和比较例8试样(以下,也称为比较处方8)。在以上工序中,搅拌全部以200rpm进行。
[表11]
表11
成分 | 实施例47 | 实施例48 | 比较例8 |
Pal-GH | 0.01g | 0.05g | - |
1,2-己二醇*1 | 0.004g | 0.02g | - |
蔗糖月桂酸酯L-1695*2 | 0.0048g | 0.024g | - |
蔗糖月桂酸酯L-595*3 | 0.0032g | 0.016g | - |
硬脂酸*4 | 0.001g | 0.005g | - |
纯化水 | 99.977g | 99.885g | 100g |
合计 | 100g | 100g | 100g |
*1:(株)アイ·テイ·才一制
*2:蔗糖月桂酸酯:三菱ケミカルフ一ズ(株)制[商品名:リヨートーシユガーエステルL-1695]
*3:蔗糖月桂酸酯:三菱ケミカルフーブ(株)制[商品名:リヨートーシユガー工ステルL-595]
*4:花王(株)制[商品名:ルナツクS-98]
<人造皮革中的戈壁黄沙的附着抑制>
将人造皮革サプラーレ(出光テクノフアイン株式会社制)切断为4cm×4cm的大小,涂布实施例47、实施例48、和比较例8的溶液各2.0mL,用32℃的恒温槽干燥了1小时。
在10mL的实验室螺口管瓶中,加入戈壁黄沙(NIES-CRM No.30)1.5g,用上述制作出的各サプラーレ盖上,使其反转而使其接触从而使戈壁黄沙附着了。将结果的图像示于图22中。然后,使用ICP-发射光谱分析装置将戈壁黄沙中所包含的金属元素定量,从而评价了戈壁黄沙的附着量,将所得的结果示于图23中。实施例47相对于比较例8抑制了戈壁黄沙的附着,实施例48中观察到该效果进一步高的情形,显示出具有抗污染效果。
[实施例49~实施例52、比较例9:Pal-GH组合物的皮肤渗透促进效果]
将人三维培养表皮模型(LabCyte EPI-MODEL12,φ10.5mm,批号#LCE12-210920-A,株式会社ジヤパン·テイツジユ·エンジ二アリング制)设置于12孔组织培养板(IWAKI,旭硝子株式会社制),在各孔中分注1mL的磷酸缓冲生理食盐液(pH7.4)(PBS),将其设为接收液。在供给侧,添加按照表12而调制出的、1%烟酰胺(Sigma Ardrich制)混配水分散液各500μL,盖上组织培养板的盖,在37℃的培养箱内静置从而实施了皮肤透过性试验。添加实施例49~52和比较例9的分散液而透过4小时后,采取接收液和三维培养表皮模型。将采取了的三维培养表皮模型用500μL的PBS洗涤3次,4等分地用手术刀切断而投入到1.5mL微管(Eppendorf制)中。然后,加入甲醇/纯化水=1/1v/v提取液750μL用涡旋混合器(ケニス株式会社制)处理1小时,从而从三维培养表皮模型提取烟酰胺,用孔径0.45μm针头式过滤器(メルク制)进行了过滤处理。通过高效液相色谱(HPLC Agilent制)测定所得的过滤液和接收液中的烟酰胺浓度,从而算出了每单位面积的烟酰胺皮肤透过量。试验各检体各进行3次,算出它们的平均值,由该值算出了透过4小时后的皮肤透过量。HPLC测定条件如以下那样。
检测器:紫外吸光光度计(测定波长:260nm),柱:在内径4.6mm、长度25cm的不锈钢管中填充3μm的HPLC用十八烷基甲硅烷基化硅胶而成的物质(ODS-4ジーエルサイエンス株式会社),柱温度:40℃,流动相:0.1%乙酸水溶液/5mMICP-ALKS7水溶液:甲醇=9:1(v/v)
将所得的结果示于图24中。图24显示从三维培养表皮模型的储存器中检测到的烟酰胺量。添加了实施例49~52的培养皮肤,与添加了比较例9的培养皮肤相比确认到高的烟酰胺渗透量。
[表12]
表12
※1キシダ化学株式会社制
※2制品名:アンヒトール20HD(花王株式会社制)
※3制品名:カルコ一ル4098(花王株式会社制)
※4制品名:カルコ一ル6098(花王株式会社制)
※5Sigma Aldrich社制
※6制品名:SY Glyster ML-750(阪本药品工业株式会社制)
[实施例53、比较例10:Pal-GH美容液的皮肤渗透促进效果]
将人三维培养表皮模型(LabCyte EPI-MODEL12,φ10.5mm,批号#LCE12-210920-A,株式会社ジヤパン·テイツシユ·エンジ二アリング制)设置于12孔组织培养板(IWAKI,旭硝子株式会社制),在各孔中分注1mL的磷酸缓冲生理食盐液(pH7.4)(PBS),将其设为接收液。在供给侧,添加按照表13而调制出的、1%烟酰胺(Sigma Ardrich制)混配美容液各500μL,盖上组织培养板的盖,在37℃的培养箱内静置从而实施了皮肤透过性试验。添加实施例53和比较例10的美容液而透过4小时后,采取接收液和三维培养表皮模型。将采取了的三维培养表皮模型用500μL的PBS洗涤3次,4等分地用手术刀切断而投入到1.5mL微管(Eppendorf制)中。然后,加入甲醇/纯化水=1/1 v/v提取液750μL用涡旋混合器(ケニス株式会社制)处理1小时,从而从三维培养表皮模型提取烟酰胺,用孔径0.45μm针头式过滤器(メルク制)进行了过滤处理。通过高效液相色谱(HPLC Agilent制)测定所得的过滤液和接收液中的烟酰胺浓度,从而算出了每单位面积的烟酰胺皮肤透过量。试验各检体各进行3次,算出它们的平均值,从该值算出了透过4小时后的皮肤透过量。HPLC测定条件如以下那样。
检测器:紫外吸光光度计(测定波长:260nm),柱:在内径4.6mm、长度25cm的不锈钢管中填充3μm的HPLC用十八烷基甲硅烷基化硅胶而成的物质(ODS-4ジ一エルサイエンス株式会社),柱温度:40℃,流动相:0.1%乙酸水溶液/5mMICP-ALKB7水溶液:甲醇=9∶1(v/v)
将所得的结果示于图25中。图25显示从三维培养表皮模型的储存器中检测到的烟酰胺量。添加了实施例53的美容液的培养皮肤,与添加了比较例10的美容液的培养皮肤相比确认到高的烟酰胺渗透量。
[表13]
表13
原料(%) | 比较例10 | 实施例53 |
Pal-GH | 0.050 | |
1,3-丁二醇※1 | 0.334 | |
月桂基羟基磺基甜菜碱※2 | 0030 | |
肉豆蔻醇※3 | 0.003 | |
鲸蜡醇※4 | 0.003 | |
甘油※5 | 1.000 | 1.000 |
烟酰胺※6 | 1.000 | 1.000 |
对羟基苯甲酸甲酯※7 | 0.050 | 0.050 |
POE失水山梨糖醇单月桂酸酯※8 | 0.050 | 0.050 |
1,3-丁二醇 | 7.000 | 7.000 |
黄原胶※9 | 0.050 | 0.050 |
透明质酸Na※10 | 0.005 | 0.005 |
纯化水 | 91 | 90 |
※1キシダ化学株式会社制
※2制品名:アンヒト一ル20[ID(花王株式会社制)
※3制品名:カルコ一ル4098(花王株式会社制)
※4制品名:カルコ一ル6098(花王株式会社制)
※5制品名:浓甘油(花王株式会社制)
※6Sigma Aldrich社制
※7上野制药株式会社制
※8制品名:エマゾ一ルL-120V(花王株式会社制)
※9制品名:KELTROL CG-SFT(三晶株式会社制)
※10制品名:透明质酸FCH-150(キツコーマンバイ才ケミファ社株式会社制)
[实施例54、比较例11:Pal-GH的组合物的PM2.5粒子的附着抑制效果]
将人造皮革サプラ一レ(出光テクノフアイン株式会社制)切断为2cm×2cm的大小,涂布按照表14而调制出的比较例11和实施例54的溶液各1.0mL,用32℃的恒温槽干燥了1小时。在10mL的实验室螺口管瓶中加入PM2.5粒子(NIES-CRM No.都市大气粉尘)1.5g,用上述制作出的各サプラーレ盖上,使其反转而使其接触从而使PM2.5粒子附着了。将附着了的PM2.5粒子的目视的观察结果示于图26中。确认到与涂布了比较例11的溶液的サプラーレ相比,涂布了实施例54的溶液的サプラーレ抑制了PM2.5粒子的附着。
[表14]
表14
成分(%) | 比较例11 | 实施例54 |
Pal-GH | 0.05 | |
1,3-丁二醇※1 | 0.5 | 0.5 |
NaOH※2 | 0.006 | 0.006 |
硬脂酸※3 | 0.0125 | 0.0125 |
羧基乙烯基聚合物※4 | 0.1 | 0.1 |
烟酰胺※5 | 1 | 1 |
纯化水 | 99.3815 | 99.3315 |
※1キシダ化学株式会社制
※2纯正化学株式会社制
※3制品名:ルナックS-98(花王株式会社制)
※4制品名:ハイビスワコー104(富士フイルム和光藥株式会社制)
※5sigma Aldrich社制。
Claims (11)
1.一种组合物,其含有脂质肽型化合物和蔗糖酯,所述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
2.根据权利要求1所述的组合物,其能够在皮肤或毛发的表面形成被膜。
3.根据权利要求1或2所述的组合物,其防止尘埃、花粉、粒子状物质、包含螨的尸体在内的螨、气态物质、或臭气物质向皮肤或毛发的表面附着。
4.根据权利要求1~3中任一项所述的组合物,其特征在于,所述脂质肽型化合物由下述式(1)~式(3)所示的化合物或其可药用的盐之中的至少一种构成,
式中,R1表示碳原子数9~23的脂肪族基,R2表示氢原子、或可具有碳原子数1或2的支链的碳原子数1~4的烷基,R3表示-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基,
式中,R4表示碳原子数9~23的脂肪族基,R5~R7各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基,
式中,R8表示碳原子数9~23的脂肪族基,R9~R12各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基。
5.一种防止皮肤表面或毛发表面污染的方法,其包含下述工序:在皮肤表面或毛发表面形成由组合物形成的膜的膜形成工序,所述组合物含有脂质肽型化合物和蔗糖酯,所述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
6.根据权利要求5所述的方法,其特征在于,所述脂质肽型化合物由下述式(1)~式(3)所示的化合物或其可药用的盐之中的至少一种构成,
式中,R1表示碳原子数9~23的脂肪族基,R2表示氢原子、或可具有碳原子数1或2的支链的碳原子数1~4的烷基,R3表示-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基,
式中,R4表示碳原子数9~23的脂肪族基,R5~R7各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基,
式中,R8表示碳原子数9~23的脂肪族基,R9~R12各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基。
7.一种防止尘埃、花粉、粒子状物质、包含螨的尸体在内的螨、气态物质、或臭气物质向皮肤表面或毛发表面附着的方法,其包含下述工序:在皮肤表面或毛发表面形成由组合物形成的膜的膜形成工序,所述组合物含有脂质肽型化合物和蔗糖酯,所述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
8.根据权利要求7所述的方法,其特征在于,所述脂质肽型化合物由下述式(1)~式(3)所示的化合物或其可药用的盐之中的至少一种构成,
式中,R1表示碳原子数9~23的脂肪族基,R2表示氢原子、或可具有碳原子数1或2的支链的碳原子数1~4的烷基,R3表示-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基,
式中,R4表示碳原子数9~23的脂肪族基,R5~R7各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基,
式中,R8表示碳原子数9~23的脂肪族基,R9~R12各自独立地表示氢原子、可具有碳原子数1或2的支链的碳原子数1~4的烷基、或-(CH2)n-X基,n表示1~4的数,X表示氨基、胍基、-CONH2基、可具有1~3个氮原子的5元环基、可具有1~3个氮原子的6元环基、或可具有1~3个氮原子的由5元环和6元环构成的稠杂环基。
9.一种皮肤渗透促进用组合物,其含有脂质肽型化合物和蔗糖酯,所述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
10.一种促进皮肤渗透的方法,其包含下述工序:在皮肤表面或毛发表面形成由组合物形成的膜的膜形成工序,所述组合物含有脂质肽型化合物和蔗糖酯,所述脂质肽型化合物在碳原子数10~24的包含脂肪族基的脂质部结合了通过至少2个以上相同或不同的氨基酸的重复而形成的肽部。
11.根据权利要求2~4中任一项所述的组合物,所述被膜的表面具有平均表面粗糙度为3nm~500nm的粗糙度。
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