CN114126574A - 皮肤外用剂 - Google Patents
皮肤外用剂 Download PDFInfo
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- CN114126574A CN114126574A CN202080046286.0A CN202080046286A CN114126574A CN 114126574 A CN114126574 A CN 114126574A CN 202080046286 A CN202080046286 A CN 202080046286A CN 114126574 A CN114126574 A CN 114126574A
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Abstract
本发明涉及提供一种皮肤外用剂,其含有以下的成分(A)~(E),且成分(A)与成分(B)的质量比(A)/(B)为0.3~2.0,成分(C)的含量为0.1~1质量%,25℃下的pH值为4.0~7.0,(A)选自碳原子数14~20的脂肪族醇中的1种以上;(B)选自多元醇脂肪酸酯型非离子表面活性剂中的2种以上;(C)选自N‑酰基氨基酸、N‑酰基牛磺酸及它们的盐、以及磷脂质中的1种以上;(D)选自类固醇类抗炎症剂、非类固醇类抗炎症剂及类肝素中的1种以上;(E)水。
Description
技术领域
本发明涉及一种皮肤外用剂。
背景技术
作为炎症性的皮肤病、尤其是异位性皮肤炎的因素,已知有活体对抗原(过敏原)的过度反应,即免疫学的异常及皮肤的屏障功能的异常。已知正常的皮肤中,在角质层中,皮脂、氨基酸、脲等天然保湿因子、神经酰胺、脂肪酸等角质细胞间脂质将皮肤的水分量保持为固定,且pH值也保持为弱酸性,与此相对,异位性皮肤炎中,角质层中的这些因子减少,角质层引起结构异常,皮肤的屏障功能降低或破坏,进而pH值也上升。因此,自皮肤内部的水分蒸散亢进,角质层的水分量也降低,并且来自皮肤外部的过敏原易侵入。因此,在异位性皮肤炎的治疗中,存在如下问题:即便暂时通过药剂而炎症得以改善,但一旦停止外用,则也会因透过的过敏原而导致症状复发。
因此,此前提出有多种用于改善皮肤的屏障功能的皮肤外用剂。例如可列举:含有细胞间脂质成分、保湿成分及磷脂质的皮肤化妆料(专利文献1)、含有N-酰基谷氨酸二酯及吡咯啶酮羧酸改性二甲基聚硅氧烷的皮肤外用剂(专利文献2)、含有特定的二酰胺衍生物及角质细胞间脂质成分的外用剂组合物(专利文献3)等。
(专利文献1)日本专利特开2004-168763号公报
(专利文献2)日本专利特开2007-210892号公报
(专利文献3)日本专利特开2002-332208号公报
发明内容
本发明提供一种皮肤外用剂,其含有以下的成分(A)~(E),且成分(A)与成分(B)的质量比(A)/(B)为0.3以上2.0以下,成分(C)的含量为0.1质量%以上1质量%以下,25℃下的pH值为4.0以上且小于7.0,
(A)选自碳原子数14以上20以下的脂肪族醇中的1种以上;
(B)选自多元醇脂肪酸酯型非离子表面活性剂中的2种以上;
(C)选自N-酰基氨基酸、N-酰基牛磺酸及它们的盐、以及磷脂质中的1种以上;
(D)选自类固醇类抗炎症剂、非类固醇类抗炎症剂及类肝素中的1种以上;
(E)水。
具体实施方式
如专利文献1~3所公开的现有的皮肤外用剂或皮肤化妆料虽可改善皮肤的屏障功能,但不具有减少过敏原对皮肤的接触、透过的功能。因此,本发明涉及一种皮肤外用剂,其在弱酸性区域的pH值下为乳化状态且使含有的药剂保持稳定,并且改善皮肤病的症状,不仅如此,也可提高皮肤的屏障功能,进而抑制过敏原对皮肤的接触、透过本身。
本发明人等发现,通过在将高级醇、2种以上的特定的非离子表面活性剂、磷脂质或特定的阴离子表面活性剂及水以特定的量比组合而成的基础配方中含有特定的药效成分,而在弱酸性区域的pH值下涂抹时的润滑性及延展性优异,且通过涂抹后在皮肤上形成具有均匀的层状结构的干燥覆膜而上述药效成分得以保持稳定,可有效地改善皮肤病的炎症状态,并且可抑制成为使症状再次恶化的原因的过敏原的透过,从而完成本发明。
本发明的皮肤外用剂可改善皮肤病的症状,并且可提高皮肤的屏障功能,保持适度的透湿性,进而抑制过敏原对皮肤的接触、透过本身,且涂抹时的润滑性及延展性也优异。
[成分(A):碳原子数14~20的脂肪族醇]
作为成分(A)的碳原子数14以上20以下的脂肪族醇,优选为直链脂肪族醇,又,优选为饱和脂肪族醇。作为成分(A)的具体例,可列举:肉豆蔻醇、鲸蜡醇、硬脂醇、花生醇。
作为成分(A),可单独使用任一种或将2种以上组合使用,但就乳化状态的保存稳定性的观点而言,优选为将碳原子数不同的2种以上的化合物组合使用。进而,就相同的观点而言,成分(A)中的(a1)短链(碳原子数14以上且小于18)的脂肪族醇相对于(a2)长链(碳原子数18以上20以下)的脂肪族醇的质量比(a1)/(a2)优选为0.1以上,更优选为0.6以上,进而优选为1.0以上,又,优选为7.0以下,更优选为5.0以下,进而优选为3.0以下。
就过敏原透过抑制的观点而言,本发明的皮肤外用剂中的成分(A)的含量优选为0.3质量%以上,更优选为0.5质量%以上,进而优选为0.8质量%以上,又,就药剂的保存稳定性的观点而言,优选为3.0质量%以下,更优选为2.5质量%以下,进而优选为2.0质量%以下。
[成分(B):2种以上的多元醇脂肪酸酯型非离子表面活性剂]
作为成分(B),可列举:蔗糖脂肪酸酯、甘油脂肪酸酯、聚甘油脂肪酸酯、山梨醇酐单脂肪酸酯、聚氧乙烯山梨醇酐脂肪酸酯、聚氧乙烯山梨糖醇脂肪酸酯、聚氧乙烯甘油脂肪酸酯、聚氧乙烯脂肪酸酯、聚氧乙烯氢化蓖麻油等,将这些的2种以上组合使用。作为2种以上的多元醇脂肪酸酯的组合,就形成具有层状结构的干燥涂膜的观点而言,优选为(b1)HLB为3以上7以下、更优选为4以上6以下的多元醇脂肪酸酯的1种以上与(b2)HLB为11以上16以下、更优选为13以上15以下的多元醇脂肪酸酯的1种以上的组合。又,就相同的观点而言,这些的质量比(b1)/(b2)优选为0.25以上,更优选为0.4以上,进而优选为0.6以上,又,优选为4.0以下,更优选为2.0以下,进而优选为1.0以下。
就乳化状态的保存稳定性的观点而言,本发明的皮肤外用剂中的成分(B)的含量优选为0.5质量%以上,更优选为1.0质量%以上,进而优选为1.5质量%以上,又,就涂抹时的润滑性的观点而言,优选为5.0质量%以下,更优选为4.0质量%以下,进而优选为3.0质量%以下。
就过敏原透过抑制的观点而言,本发明的皮肤外用剂中的成分(A)与成分(B)的质量比(A)/(B)为0.3以上,优选为0.35以上,更优选为0.4以上,又,就涂抹时的延展性良好的观点而言,为2.0以下,优选为1.5以下,更优选为1.0以下,进而优选为0.8以下。
[成分(C):N-酰基氨基酸、N-酰基牛磺酸及它们的盐、磷脂质]
成分(C)是使形成于皮肤上的具有层状结构的干燥覆膜具有过敏原透过抑制的功能的成分。
就乳化状态的保存稳定性的观点而言,成分(C)中的酰基氨基酸及酰基牛磺酸的酰基优选为来自饱和或不饱和的具有直链或支链的脂肪酸或它们的混合脂肪酸,更优选为来自直链脂肪酸或直链脂肪酸的混合脂肪酸,其碳原子数优选为6以上,更优选为10以上,进而优选为12以上,又,优选为22以下,更优选为20以下,进而优选为18以下。作为该酰基,就减少皮肤刺激的观点而言,优选为选自辛酰基、月桂酰基、肉豆蔻酰基、棕榈酰基、硬脂酰基及椰油酰基中的1种以上,也可为来自棕榈油等动植物油的酰基。
作为酰基氨基酸的氨基酸部分,就药剂的保存稳定性的观点而言,优选为谷氨酸、天冬氨酸。此处,谷氨酸可为D体、L体或D体与L体的混合物的任一种,优选为L体。作为该酰基氨基酸,具体而言,就乳化状态的保存稳定性的观点而言,优选为选自N-硬脂酰谷氨酸、N-月桂酰谷氨酸、N-肉豆蔻酰谷氨酸、N-椰油酰谷氨酸、N-棕榈脂肪酸谷氨酸及N-月桂酰天冬氨酸中的1种以上,更优选为选自N-硬脂酰谷氨酸及N-棕榈脂肪酸谷氨酸中的1种以上。
作为酰基牛磺酸,就乳化状态的保存稳定性的观点而言,优选为选自椰子油脂肪酸甲基牛磺酸、N-己酰甲基牛磺酸、N-月桂酰甲基牛磺酸、N-肉豆蔻酰甲基牛磺酸、N-棕榈酰甲基牛磺酸、N-硬脂酰甲基牛磺酸、及N-油酰甲基牛磺酸中的1种以上,更优选为N-硬脂酰甲基牛磺酸。
作为这些酰基氨基酸及酰基牛磺酸的盐,可列举:钠盐、钾盐等碱金属盐;钙盐、镁盐等碱土类金属盐;铝盐、锌盐等其它金属盐;铵盐;单乙醇胺盐、二乙醇胺盐、三乙醇胺盐等有机胺盐;精氨酸盐、赖氨酸盐、组氨酸盐、鸟氨酸盐等碱性氨基酸盐等。这些可单独使用1种,也可将2种以上组合使用。其中,作为酰基氨基酸盐及酰基牛磺酸的盐,就乳化状态的保存稳定性的观点而言,优选为碱金属盐,更优选为钠盐。
作为成分(C)中的磷脂质,可列举:卵磷脂、氢化卵磷脂、羟基化卵磷脂、磷脂酰乙醇胺、磷脂酰丝氨酸、磷脂酰胆碱、磷脂酰肌醇、磷脂酰甘油、心磷脂等甘油磷脂质;神经鞘磷脂、脑苷脂、神经节苷脂等鞘磷脂等。其中,就过敏原透过抑制的观点而言,优选为氢化卵磷脂,更优选为大豆氢化卵磷脂。
作为成分(C),就乳化状态的保存稳定性的观点而言,上述具体的化合物中,优选为分类为N-酰基谷氨酸钠、N-酰基甲基牛磺酸钠及氢化卵磷脂的化合物。以上的成分(C)可单独使用任一种或将2种以上组合使用。就过敏原透过抑制及乳化状态的保存稳定性提升的观点而言,本发明的皮肤外用剂中的成分(C)的含量为0.1质量%以上,优选为0.2质量%以上,更优选为0.3质量%以上,又,就涂抹时的润滑性及过敏原透过抑制的观点而言,为1.0质量%以下,优选为0.8质量%以下,更优选为0.6质量%以下。
就过敏原透过抑制的观点而言,本发明的皮肤外用剂中的成分(A)与成分(C)的质量比(A)/(C)优选为1.0以上,更优选为1.5以上,进而优选为2.0以上,又,就乳化状态的保存稳定性的观点而言,优选为15以下,更优选为5.0以下,进而优选为3.0以下。
[成分(D):类固醇性抗炎症剂、非类固醇类抗炎症剂、类肝素]
作为成分(D)中的类固醇类抗炎症剂,可列举:氯倍他索丙酸酯、双氟拉松乙酸酯、莫美他松糠酸酯、倍他米松丁酸丙酸酯、氟洛奈皮质醇(fluocinonide)、倍他米松二丙酸酯、二氟泼尼酯、安西奈德、双氟可龙戊酸酯、丁酸丙酸氢化可的松、地泼罗酮丙酸酯、***丙酸酯、***戊酸酯、倍他米松戊酸酯、倍氯米松二丙酸酯、氟轻松、***龙戊酸酯乙酸酯、曲安奈德、阿氯米松二丙酸酯、氯倍他松丁酸酯、氢化可的松丁酸酯、***龙、***乙酸酯、氢化可的松乙酸酯、氢化可的松戊酸酯、***间磺酸苯甲酸钠、***龙戊酸酯、***、氢化可的松。
作为成分(D)中的非类固醇类抗炎症剂,可列举:乌芬那酯、布洛芬吡甲酯、阿他利特、阿西美辛(Acemetacin)、安吡昔康(Ampiroxicam)、氨芬酸、布洛芬、吲哚美辛、依托度酸、酮洛芬(Ketoprofen)、扎托布洛芬、双氯芬酸、舒林酸、塞来昔布、噻洛芬酸(Tiaprofenic acid)、替诺昔康(Tenoxicam)、萘普生、匹洛西卡(Piroxicam)、联苯乙酸、普拉洛芬(Pranoprofen)、氟比洛芬(flurbiprofen)、甲芬那酸、塞来昔布、美洛昔康(Meloxicam)、莫苯唑酸、罗非昔布、氯索洛芬(Loxoprofen)、氯苯扎利、氯诺昔康(Lornoxicam)及这些的盐,其中,就药剂的保存稳定性的观点而言,优选为选自乌芬那酯、布洛芬吡甲酯中的1种以上。
就药剂的有效性的观点而言,本发明的皮肤外用剂中的成分(D)的含量优选为0.025质量%以上,更优选为0.05质量%以上,进而优选为0.1质量%以上,又,就乳化状态的保存稳定性的观点而言,优选为6.5质量%以下,更优选为6.0质量%以下,进而优选为5.5质量%以下。
更详细而言,在成分(D)为类固醇类抗炎症剂的情形时,就与上述相同的观点而言,其含量优选为0.025质量%以上,更优选为0.05质量%以上,进而优选为0.10质量%以上,又,优选为1.0质量%以下,更优选为0.5质量%以下,进而优选为0.3质量%以下。又,在成分(D)为非类固醇类抗炎症剂的情形时,就与上述相同的观点而言,其含量优选为0.5质量%以上,更优选为2.5质量%以上,进而优选为4.5质量%以上,又,优选为6.5质量%以下,更优选为6.0质量%以下,进而优选为5.5质量%以下。又,在成分(D)为类肝素的情形时,就与上述相同的观点而言,其含量优选为0.01质量%以上,更优选为0.1质量%以上,进而优选为0.3质量%以上,又,优选为3.0质量%以下,更优选为1.0质量%以下,进而优选为0.5质量%以下。
[成分(E):水]
就涂抹时的延展性的观点而言,本发明的皮肤外用剂中的成分(E)的含量优选为50质量%以上,更优选为60质量%以上,进而优选为70质量%以上,又,就过敏原透过抑制的观点而言,优选为95质量%以下,更优选为90质量%以下,进而优选为85质量%以下。
[成分(F):神经酰胺类]
为了进一步改善皮肤的屏障功能,本发明的皮肤外用剂中可含有神经酰胺类作为成分(F)。
作为神经酰胺类,可列举选自天然型神经酰胺及假型神经酰胺中的1种以上。作为天然型神经酰胺的具体例,可列举:鞘胺醇、二氢鞘胺醇、植物鞘胺醇或Sphingadienine经酰胺化的神经酰胺型1~7,进而也包含这些的N-烷基体(例如N-甲基体)。作为假型神经酰胺的具体例,可列举:(N-十六烷氧基羟基丙基)-N-羟基十六酰胺、(N-十六烷氧基羟基丙基)-N-羟基癸酰胺、N-[2-(2,3-二羟基丙氧基)-3-十六烷氧基丙基]-N-3-甲氧基丙基十四酰胺。
就皮肤的屏障功能的进一步提升的观点而言,本发明的皮肤外用剂中的成分(F)的含量优选为1.0质量%以上,更优选为1.5质量%以上,进而优选为2.0质量%以上,又,就涂抹时的延展性良好的观点而言,优选为6.0质量%以下,更优选为5.0质量%以下,进而优选为4.0质量%以下。
[pH值]
关于本发明的皮肤外用剂的pH值,就适应正常的皮肤的pH值环境的观点及成分(D)的稳定性提升的观点而言,为7.0以下,优选为6.5以下,更优选为6.0以下,又,就减少皮肤刺激的观点而言,为4.0以上,优选为4.2以上,更优选为4.4以上。
在本发明的皮肤外用剂含有类固醇类抗炎症剂作为成分(D)的情形时,就成分(D)的稳定性的观点而言,其pH值优选为5.5以下,更优选为5.0以下,进而优选为4.8以下,就乳化状态的保存稳定性的观点而言,优选为4.0以上,更优选为4.2以上,进而优选为4.4以上。
在本发明的皮肤外用剂含有非类固醇类抗炎症剂作为成分(D)的情形时,就乳化状态的保存稳定性的观点而言,其pH值优选为7.0以下,更优选为6.5以下,进而优选为6.0以下,就相同的观点而言,优选为4.0以上,更优选为4.5以上,进而优选为5.0以上。
在本发明的皮肤外用剂含有类肝素作为成分(D)的情形时,就乳化状态的保存稳定性的观点而言,其pH值优选为7.0以下,更优选为6.5以下,进而优选为6.0以下,就相同的观点而言,优选为4.0以上,更优选为4.5以上,进而优选为5.0以上。
[其它成分]
本发明的皮肤外用剂可适当含有烃油、醚油、酯油、硅酮油、氟类油、蜡、胆固醇类衍生物、植固醇类衍生物、二季戊四醇脂肪酸酯类、三酸甘油酯类、羊毛脂、羊毛固醇类衍生物、凡士林等的除成分(A)以外的油剂、甘油、丙二醇等多元醇、增粘剂、杀菌剂、保湿剂、湿润剂、着色剂、防腐剂、触感改善剂、粉体、香料、抗炎症剂、美白剂、止汗剂、紫外线吸收剂、抗氧化剂等。
本发明的皮肤外用剂通过以特定的比率含有成分(A)~(E),而在涂抹至皮肤并使水分蒸发,由此可在皮肤表面形成具有层状结构的干燥覆膜。再者,层状结构可通过广角X射线衍射、偏光显微镜等来确认。
关于以上所述的实施方式,以下进一步公开本发明的优选的方式。
<1>
一种皮肤外用剂,其中,含有以下的成分(A)~(E),且成分(A)与成分(B)的质量比(A)/(B)为0.3以上2.0以下,成分(C)的含量为0.1质量%以上1质量%以下,25℃下的pH值为4.0以上且小于7.0。
(A)选自碳原子数14以上20以下的脂肪族醇中的1种以上
(B)选自多元醇脂肪酸酯型非离子表面活性剂中的2种以上
(C)选自N-酰基氨基酸、N-酰基牛磺酸及它们的盐、以及磷脂质中的1种以上
(D)选自类固醇类抗炎症剂、非类固醇类抗炎症剂及类肝素中的1种以上
(E)水<2>
如<1>所记载的皮肤外用剂,其中,优选为成分(A)为选自肉豆蔻醇、鲸蜡醇、硬脂醇及花生醇中的1种以上。
<3>
如<1>或<2>所记载的皮肤外用剂,其中,优选为成分(A)为碳原子数不同的2种以上的化合物的组合。
<4>
如<3>所记载的皮肤外用剂,其中,(a1)碳原子数14以上且小于18的脂肪族醇相对于(a2)碳原子数18以上20以下的脂肪族醇的质量比(a1)/(a2)优选为0.1以上,更优选为0.6以上,进而优选为1.0以上,又,优选为7.0以下,更优选为5.0以下,进而优选为3.0以下。
<5>
如<1>至<4>中任一项所记载的皮肤外用剂,其中,成分(A)的含量优选为0.3质量%以上,更优选为0.5质量%以上,进而优选为0.8质量%以上,又,优选为3.0质量%以下,更优选为2.5质量%以下,进而优选为2.0质量%以下。
<6>
如<1>至<5>中任一项所记载的皮肤外用剂,其中,优选为成分(B)为选自蔗糖脂肪酸酯、甘油脂肪酸酯、聚甘油脂肪酸酯、山梨醇酐单脂肪酸酯、聚氧乙烯山梨醇酐脂肪酸酯、聚氧乙烯山梨糖醇脂肪酸酯、聚氧乙烯甘油脂肪酸酯、聚氧乙烯脂肪酸酯及聚氧乙烯氢化蓖麻油等中的2种以上的组合。
<7>
如<1>至<6>中任一项所记载的皮肤外用剂,其中,优选为成分(B)由(b1)HLB为3以上7以下、优选为4以上6以下的多元醇脂肪酸酯的1种以上及(b2)HLB为11以上16以下、优选为13以上15以下的多元醇脂肪酸酯的1种以上构成,且它们的质量比(b1)/(b2)优选为0.25以上,更优选为0.4以上,进而优选为0.6以上,又,优选为4.0以下,更优选为2.0以下,进而优选为1.0以下。
<8>
如<1>至<7>中任一项所记载的皮肤外用剂,其中,成分(B)的含量优选为0.5质量%以上,更优选为1.0质量%以上,进而优选为1.5质量%以上,又,优选为5.0质量%以下,更优选为4.0质量%以下,进而优选为3.0质量%以下。
<9>
如<1>至<8>中任一项所记载的皮肤外用剂,其中,成分(A)与成分(B)的质量比(A)/(B)优选为0.35以上,更优选为0.4以上,又,优选为1.5以下,更优选为1.0以下,进而优选为0.8以下。
<10>
如<1>至<9>中任一项所记载的皮肤外用剂,其中,成分(C)中的酰基氨基酸及酰基牛磺酸的酰基优选为来自饱和或不饱和的具有直链或支链的脂肪酸或它们的混合脂肪酸、更优选为来自直链脂肪酸或直链脂肪酸的混合脂肪酸,其碳原子数优选为6以上,更优选为10以上,进而优选为12以上,又,优选为22以下,更优选为20以下,进而优选为18以下。
<11>
如<1>至<10>中任一项所记载的皮肤外用剂,其中,成分(C)的酰基氨基酸或其盐优选为选自N-硬脂酰谷氨酸、N-月桂酰谷氨酸、N-肉豆蔻酰谷氨酸、N-椰油酰谷氨酸、N-棕榈脂肪酸谷氨酸及N-月桂酰天冬氨酸中的1种以上或其盐,更优选为选自N-硬脂酰谷氨酸或其盐及N-棕榈脂肪酸谷氨酸或其盐中的1种以上。
<12>
如<1>至<11>中任一项所记载的皮肤外用剂,其中,成分(C)的酰基牛磺酸或其盐优选为选自椰子油脂肪酸甲基牛磺酸、N-己酰甲基牛磺酸、N-月桂酰甲基牛磺酸、N-肉豆蔻酰甲基牛磺酸、N-棕榈酰甲基牛磺酸、N-硬脂酰甲基牛磺酸及N-油酰甲基牛磺酸中的1种以上或其盐,更优选为N-硬脂酰甲基牛磺酸或其盐。
<13>
如<1>至<12>中任一项所记载的皮肤外用剂,其中,成分(C)的磷脂质优选为选自卵磷脂、氢化卵磷脂、羟基化卵磷脂、磷脂酰乙醇胺、磷脂酰丝氨酸、磷脂酰胆碱、磷脂酰肌醇、磷脂酰甘油、心磷脂、神经鞘磷脂、脑苷脂、神经节苷脂中的1种以上,更优选为氢化卵磷脂,进而优选为大豆氢化卵磷脂。
<14>
如<1>至<13>中任一项所记载的皮肤外用剂,其中,成分(C)优选为选自N-酰基谷氨酸钠、N-酰基甲基牛磺酸钠及氢化卵磷脂中的1种以上。
<15>
如<1>至<14>中任一项所记载的皮肤外用剂,其中,成分(C)的含量优选为0.2质量%以上,更优选为0.3质量%以上,又,优选为0.8质量%以下,更优选为0.6质量%以下。
<16>
如<1>至<15>中任一项所记载的皮肤外用剂,其中,成分(A)与成分(C)的质量比(A)/(C)优选为1.0以上,更优选为1.5以上,进而优选为2.0以上,又,优选为15以下,更优选为5.0以下,进而优选为3.0以下。
<17>
如<1>至<16>中任一项所记载的皮肤外用剂,其中,成分(D)优选为选自***龙戊酸酯乙酸酯、***龙、氢化可的松丁酸酯、乌芬那酯及类肝素中的1种以上。
<18>
如<1>至<17>中任一项所记载的皮肤外用剂,其中,成分(D)的含量优选为0.025质量%以上,更优选为0.05质量%以上,进而优选为0.1质量%以上,又,优选为6.5质量%以下,更优选为6.0质量%以下,进而优选为5.5质量%以下。
<19>
如<1>至<18>中任一项所记载的皮肤外用剂,其中,成分(E)的含量优选为50质量%以上,更优选为60质量%以上,进而优选为70质量%以上,又,优选为95质量%以下,更优选为90质量%以下,进而优选为85质量%以下。
<20>
如<1>至<19>中任一项所记载的皮肤外用剂,其中,进而含有神经酰胺类作为成分(F)。
<21>
如<20>所记载的皮肤外用剂,其中,成分(F)的含量优选为1.0质量%以上,更优选为1.5质量%以上,进而优选为2.0质量%以上,又,优选为6.0质量%以下,更优选为5.0质量%以下,进而优选为4.0质量%以下。
<22>
如<1>至<21>中任一项所记载的皮肤外用剂,其中,含有类固醇类抗炎症剂作为成分(D),且皮肤外用剂的pH值优选为5.5以下,更优选为5.0以下,进而优选为4.8以下,又,优选为4.0以上,更优选为4.2以上,进而优选为4.4以上。
<23>
如<1>至<21>中任一项所记载的皮肤外用剂,其中,含有非类固醇类抗炎症剂作为成分(D),且皮肤外用剂的pH值优选为7.0以下,更优选为6.5以下,进而优选为6.0以下,又,优选为4.0以上,更优选为4.5以上,进而优选为5.0以上。
<24>
如<1>至<21>中任一项所记载的皮肤外用剂,其中,含有类肝素作为成分(D),皮肤外用剂的pH值优选为7.0以下,更优选为6.5以下,进而优选为6.0以下,又,优选为4.0以上,更优选为4.5以上,进而优选为5.0以上。
[实施例]
实施例1~16、比较例1~5
制备表1~3所示的皮肤外用剂,按照下述的方法及基准,对“过敏原透过抑制”、“药剂稳定性”、“乳化稳定性”、“涂抹时的润滑性”及“涂抹时的延展性的良好程度”进行评价。
[过敏原透过抑制的评价方法]
在12质量%聚丙烯酰胺凝胶(SDS-PAGE用)上涂抹10mg/cm2的组合物,并在室温下使其干燥24小时。其次,将φ6mm的滤纸静置在该组合物上,利用20μL的色素水溶液(固绿FCF、0.02mg/20mL)使其润湿。在32℃95%条件下静置5小时后,将滤纸去除,通过水洗而将干燥的组合物去除。关于透过干燥的组合物的色素的定量,使用密度计对各组合物进行3~4次,以百分率表示将无涂抹设为1时的色素透过量,通过下述的基准进行评价。
A:小于20%
B:20%以上且小于40%
C:40%以上且小于60%
D:60%以上且小于80%
E:80%以上
[药剂的保存稳定性的评价方法]
通过液相色谱法或紫外可见吸光度测定法将刚制造后的组合物与使用了各药剂(***龙戊酸酯乙酸酯、***龙、氢化可的松丁酸酯、乌芬那酯或类肝素)的标准物质的溶液进行比较,求出各药剂的含量。其次,将组合物在50℃下保存1个月,以与上述相同的方式将保存后的组合物与使用标准物质的溶液相比较,求出各药剂的含量,以百分率表示将刚制造后的组合物中的含量设为1时的残存量,通过下述的基准进行评价。
A:95%以上
B:90%以上且小于95%
C:85%以上且小于90%
D:80%以上且小于85%
E:小于80%
[乳化状态的保存稳定性的评价方法]
通过目视并通过下述的基准对于50℃及-5℃下保存1个月后的组合物的状态(分层或凝集的任一种)进行评价。
A:无变化
B:状态略微发生变化
C:状态明显发生变化
D:一部分分离或凝胶化
E:整体分离或凝胶化
[涂抹时的润滑性的评价方法]
10名专业评价人员对涂抹各乳化组合物时的润滑性进行感官评价,并通过以下的基准进行判定。
A:7名~10名评价为良好(佳)
B:5名或6名评价为良好(佳)
C:3名或4名评价为良好(佳)
D:1名或2名评价为良好(佳)
E:无评价为良好(佳)的评价人员
[涂抹时的延展性的良好程度的评价方法]
10名专业评价人员对涂抹各乳化组合物时的延展性的良好程度进行感官评价,并通过以下的基准进行判定。
A:7名~10名评价为良好(佳)
B:5名或6名评价为良好(佳)
C:3名或4名评价为良好(佳)
D:1名或2名评价为良好(佳)
E:无评价为良好(佳)的评价人员
[表3]
*1:pH值调节量
*2:花王公司制造、Rheodol TW-S120V
*3:花王公司制造、Rheodol SP-S10V
*4:日油公司制造、Coatsome NC-21
实施例17
制备下述配方的皮肤外用剂,按照上述方法对“过敏原透过抑制”、“涂抹时的润滑性”、“涂抹时的延展性的良好程度”进行评价,结果分别为“B”、“B”、“B”。
pH值=5.1
(a1)/(a2)=0
(b1)/(b2)=0.67
(A)/(B)=2.00
(A)/(C)=6.00。
Claims (7)
1.一种皮肤外用剂,其中,
所述皮肤外用剂含有以下的成分(A)~(E),且成分(A)与成分(B)的质量比(A)/(B)为0.3以上2.0以下,成分(C)的含量为0.1质量%以上1质量%以下,25℃下的pH值为4.0以上7.0以下,
(A)选自碳原子数14以上20以下的脂肪族醇中的1种以上;
(B)选自多元醇脂肪酸酯型非离子表面活性剂中的2种以上;
(C)选自N-酰基氨基酸、N-酰基牛磺酸及它们的盐、以及磷脂质中的1种以上;
(D)选自类固醇类抗炎症剂、非类固醇类抗炎症剂及类肝素中的1种以上;
(E)水。
2.如权利要求1所述的皮肤外用剂,其中,
成分(A)与成分(B)的质量比(A)/(B)为0.35以上1.0以下。
3.如权利要求1或2所述的皮肤外用剂,其中,
成分(A)与成分(C)的质量比(A)/(C)为1.0以上15以下。
4.如权利要求1~3中任一项所述的皮肤外用剂,其中,
成分(B)由(b1)HLB为3以上7以下的多元醇脂肪酸酯的1种以上及(b2)HLB为11以上16以下的多元醇脂肪酸酯的1种以上构成,且它们的质量比(b1)/(b2)为0.25以上4.0以下。
5.如权利要求1~4中任一项所述的皮肤外用剂,其中,
成分(D)的含量为0.025质量%以上6.5质量%以下。
6.如权利要求1~5中任一项所述的皮肤外用剂,其中,
成分(C)为选自N-酰基谷氨酸钠、N-酰基甲基牛磺酸钠及氢化卵磷脂中的1种以上。
7.如权利要求1~6中任一项所述的皮肤外用剂,其中,
进而含有神经酰胺类作为成分(F)。
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