CN101925353A - Vegfc产生促进剂 - Google Patents

Vegfc产生促进剂 Download PDF

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CN101925353A
CN101925353A CN2009801027278A CN200980102727A CN101925353A CN 101925353 A CN101925353 A CN 101925353A CN 2009801027278 A CN2009801027278 A CN 2009801027278A CN 200980102727 A CN200980102727 A CN 200980102727A CN 101925353 A CN101925353 A CN 101925353A
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加治屋健太朗
田口江理子
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Abstract

本发明提供水肿改善剂、淋巴管活化剂和VEGFC产生促进剂,其特征在于,含有凝血酸酰胺衍生物和/或其盐。

Description

VEGFC产生促进剂
技术领域
本发明涉及通过诱导血管内皮生长因子C(VEGFC)表达、促进淋巴管功能活化的水肿改善剂、淋巴浮肿改善剂、皱纹改善剂或肥胖改善剂。
背景技术
皮肤脉管系统存在于真皮中,由血管和淋巴管构成。为了维持体内动态平衡,已移动至血管外的组织液必须再回流至静脉中。皮肤的静脉向中枢有效地输送血流。然而,静脉本身缺乏摄取组织液的能力。由此,可以理解,摄取组织液的组织,即淋巴管在皮肤中也是必要结构。
淋巴管通过将存在于皮肤中的废物、持续从血管漏出的水分、蛋白质进行回收,从而对于使细胞周围的微环境保持稳定状态而担负重要作用。此外,人们认为淋巴管担负介由T淋巴细胞的输送来抵抗来自外界的感染因子、外部因素的作用。
作为淋巴管功能不全的病态,已知水肿、淋巴浮肿等症状(非专利文献1:Jussila,L.& Alitalo,K.(2002)Physiol Rev 82,673-700)。此外,已知淋巴管功能不仅对水肿、而且对伴随紫外线的皮肤的光老化(皱纹形成)都担负重要的作用(非专利文献2:Kajiya,K.& Detmar,M.(2006)J InvestDermatol 126,919-21)。
迄今为止的研究表明,已经鉴定出VEGFR-3作为特异性存在于淋巴管中的跨膜受体,并发现了VEGFC和VEGFD作为其配体。VEGFC作用于淋巴管、促进淋巴管内皮细胞增殖、迁移进而形成管腔,从而活化淋巴管功能(非专利文献1:Jussila,L.& Alitalo,K.(2002)Physiol Rev 82,673-700)。此外,摸索出可以通过向作为水肿的疾病状态的浮肿导入VEGFC来进行基因治疗(非专利文献3:Saaristo,A.,Tammela,T.,Timonen,J.,Yla-Herttuala,S.,Tukiainen,E.,Asko-Seljavaara,S.&Alitalo,K.(2004)Faseb J 18,1707-9)。
此外,最近,已知当导致淋巴管功能异常的基因变异小鼠成熟时呈现肥胖。关于淋巴管的形成和功能的异常而呈现肥胖的机理,获得流过淋巴管的淋巴液促进祖肥胖细胞向脂肪分化这样的认识(非专利文献4:Harvey,N.L.等,Nat Genet 2005,37,1072-81)。也就是说,已经报道了由于淋巴管的功能异常而使淋巴液向淋巴管外漏出,这与脂肪的分化、进而形成肥胖相关。因此,也期待将VEGFC促进剂作为使淋巴管功能性新生的、预防肥胖的治疗药。
VEGF家族基因存在VEGF-A~E。其中,鉴定出VEGFB和VEGFE作为仅作用于血管的因子。已知VEGFA是存在于皮肤中的、对淋巴管起作用、反过来会使淋巴管的功能变差的因子(非专利文献5:Nagy,J.A.,Vasile,E.,Feng,D.,Sundberg,C.,Brown,L.F.,Detmar,M.J.,Lawitts,J.A.,Benjamin,L.,Tan,X.,Manseau,E.J.,Dvorak,A.M.& Dvorak,H.F.(2002)J Exp Med 196,1497-506)。
对于皮肤,虽然已经报道了VEGFD在真皮中微量存在,但是由于VEGFD敲除了的小鼠完全没有出现皮肤淋巴管的形成和功能异常,因此认为VEGFD不是皮肤的淋巴管形成所不可缺少的因子(非专利文献6:Baldwin,M.E.,Halford,M.M.,Roufail,S.,Williams,R.A.,Hibbs,M.L.,Grail,D.,Kubo,H.,Stacker,S.A.& Achen,M.G.(2005)Mol Cell Biol 25,2441-9)。另一方面,皮肤中的VEGFC在表皮强表达。在表皮高表达了VEGFC的小鼠存在于真皮中的淋巴管数增加(非专利文献7:Jeltsch,M.,Kaipainen,A.,Joukov,V.,Meng,X.,Lakso,M.,Rauvala,H.,Swartz,M.,Fukumura,D.,Jain,R.K.& Alitalo,K.(1997)Science 276,1423-5),另一方面,获得如下认识:作为VEGFC的受体的VEGFR-3的中和抗体在表皮高表达,从而阻断处于表皮的VEGFC的效果,结果真皮的淋巴管数极端减少,从而形成浮肿(非专利文献8:Makinen,T.,Jussila,L.,Veikkola,T.,Karpanen,T.,Kettunen,M.I.,Pulkkanen,K.J.,Kauppinen,R.,Jackson,D.G.,Kubo,H.,Nishikawa,S.,Yla-Herttuala,S.& Alitalo,K.(2001)NatMed 7,199-205)。综上所述,可知存在于皮肤真皮内的淋巴管的功能可通过在表皮表达的VEGFC来控制,由于VEGFC丧失功能而呈现水肿(浮肿)。
因此,作为活化淋巴管、消除水肿等的方法,进行促进VEGFC表达的化合物的筛选。
非专利文献1:Physiol Rev 82,673-700(2002).
非专利文献2:J Invest Dermatol 126,919-21(2006).
非专利文献3:Faseb J 18,1707-9(2004).
非专利文献4:Nat Genet 37,1072-81(2005).
非专利文献5:J Exp Med 196,1497-506(2002).
非专利文献6:Mol Cell Biol 25,2441-9(2005).
非专利文献7:Science 276,1423-5(1997).
非专利文献8:Nat Med 7,199-205(2001).
发明内容
本发明的课题在于,从诱导VEGFC表达来活化淋巴管功能的观点出发,发现新的对预防或控制水肿、淋巴浮肿、皱纹形成或肥胖有效的药剂。
本发明者进行大量化合物的筛选,发现凝血酸(Tranexamic acid)酰胺衍生物和/或其盐诱导VEGFC表达。也就是说,发现诱导VEGFC表达的凝血酸酰胺衍生物和/或其盐对促进淋巴管功能的活化,防止或抑制水肿、淋巴浮肿、伴随紫外线的皮肤的光老化引起的皱纹的形成、或肥胖极其有效。
本发明的构成如下。
[a]一种水肿改善剂,其特征在于,含有下述通式(I)所表示的凝血酸酰胺衍生物和/或其盐。
Figure BPA00001184986900041
(式中,R1和R2表示氢原子、碳数为1~18的直链状或支链状烷基、碳数为5~8的环烷基、苄基或下述通式(II),R1和R2可以彼此相同也可以不同。
Figure BPA00001184986900042
其中,X表示低级烷基、低级烷氧基、羟基、氨基、或卤原子,n=0~3。)
[b]一种淋巴浮肿改善剂,其特征在于,含有[a]所述的凝血酸酰胺衍生物和/或其盐。
[c]一种皱纹改善剂,其特征在于,含有[a]所述的凝血酸酰胺衍生物和/或其盐。
[d]一种肥胖改善剂,其特征在于,含有[a]所述的凝血酸酰胺衍生物和/或其盐。
[e]一种淋巴管新生和/或功能促进剂,其特征在于,含有[a]所述的凝血酸酰胺衍生物和/或其盐。
[f]一种VEGFC产生促进剂,其特征在于,含有[a]所述的凝血酸酰胺衍生物和/或其盐。
[g]根据[e]所述的淋巴管新生和/或功能促进剂,防止或抑制水肿。
[h]根据[f]所述的VEGFC产生促进剂,防止或抑制水肿。
[i]根据[e]所述的淋巴管新生和/或功能促进剂,防止或抑制淋巴浮肿。
[j]根据[f]所述的VEGFC产生促进剂,防止或抑制淋巴浮肿。
[k]根据[e]所述的淋巴管新生和/或功能促进剂,防止或抑制皱纹形成。
[l]根据[f]所述的VEGFC产生促进剂,防止或抑制皱纹形成。
[m]根据[e]所述的淋巴管新生和/或功能促进剂,防止或抑制肥胖。
[n]根据[f]所述的VEGFC产生促进剂,防止或抑制肥胖。
[o]一种用于抑制水肿的方法,包括将[e]所述的淋巴管新生和/或功能促进剂涂布在皮肤上。
[p]一种用于抑制水肿的方法,包括将[f]所述的VEGFC产生促进剂涂布在皮肤上。
[q]一种用于抑制皱纹形成的方法,包括将[e]所述的淋巴管新生和/或功能促进剂涂布在皮肤上。
[r]一种用于抑制皱纹形成的方法,包括将[f]所述的VEGFC产生促进剂涂布在皮肤上。
附图说明
图1显示凝血酸甲基酰胺盐酸盐的VEGFC表达促进效果。
具体实施方式
定义:
本说明书中的术语“水肿”,与“浮肿”以相同含义使用,是组织液或淋巴液因某种原因而滞留在细胞内、细胞间隙、或体腔内的状态,也可观察到在皮下组织中。此外,本说明书中的术语“淋巴浮肿”,是指由于淋巴管的闭塞而在末梢部分滞留组织液的状态。
诱导淋巴管活化因子VEGFC的药剂的筛选按照下述实施例中的详细记载,通过以下方法进行:使各种候选药物作用于来自人表皮的培养细胞HaCat细胞株,进行VEGFC的定量,以该VEGFC量作为VEGFC诱导活性,选择具有VEGFC诱导活性的药剂作为有效药剂。
结果发现,凝血酸酰胺衍生物和/或其盐可诱导VEGFC。
本发明涉及的凝血酸酰胺衍生物是以下通式(I)化合物,
Figure BPA00001184986900061
式中,R1和R2表示氢原子、碳数为1~18的直链状或支链状烷基、碳数为5~8的环烷基、苄基或下述通式(II),R1和R2可以彼此相同也可以不同,
Figure BPA00001184986900062
其中,X表示低级烷基、低级烷氧基、羟基、氨基或卤原子,n=0~3。
本发明涉及的通式(I)所示的凝血酸酰胺衍生物是公知物质,可以通过公知方法,例如,ActaPharm.Suecica,7,441(1970),J.Med.Chem.,15,247(1972)等的方法容易地合成。即,可以通过用适当的保护基,例如,苄氧基羰基等来保护凝血酸的氨基,然后使该保护体或该保护体的反应性衍生物与胺成分反应,来制造凝血酸保护体的酰胺体。作为该保护体的反应性衍生物,优选酰氯、酰溴等酰卤,混合酸酐等。此后,通过接触还原等脱去该保护基,从而制造凝血酸的酰胺衍生物。
此外,本发明涉及的凝血酸酰胺衍生物可以通过公知方法制成无机盐或有机盐。作为在本发明中使用的盐,没有特别的限制,例如,作为无机盐,可列举盐酸盐、硫酸盐、磷酸盐、氢溴酸盐、钠盐、钾盐、镁盐、钙盐、铵盐等。作为有机盐,可列举乙酸盐、乳酸盐、马来酸盐、富马酸盐、酒石酸盐、柠檬酸盐、甲烷磺酸盐、对甲苯磺酸盐、三乙醇胺盐、二乙醇胺盐、氨基酸盐等。优选使用盐酸盐。
本发明涉及的凝血酸酰胺衍生物和/或其盐对促进淋巴管的形成和功能极其有效。作为伴随淋巴管的功能不全的症状,不仅观察到水肿、淋巴浮肿等,还观察到伴随紫外线的皮肤的光老化(皱纹形成等)、以及肥胖。因此,本发明涉及的凝血酸酰胺衍生物和/或其盐对防止、抑制水肿、淋巴浮肿以及伴随紫外线的皮肤的光老化、以及肥胖是有效的。此外,认为凝血酸酰胺衍生物和/或其盐对于先天性淋巴浮肿的治疗也是有效的。
皮肤的光老化,意味着通常被认为是反复被日光照射的结果的、皮肤外观和功能的变化。作为日光的构成要素的紫外线(UV),特别是中间UV(被称为UVB,波长为290-320nm)主要引起光老化。引起光老化所需的UVB的照射量现在还不知道。然而,引起红斑、晒黑水平的UVB反复照射通常与光老化相关。在临床上,光老化被特定为皮肤粗糙、皱纹的形成、斑的着色、土色化、松弛的形成、毛细管扩张症的发作、黑痣的产生、紫癜的发作、容易受伤、萎缩、纤维化病的色素除去区域的产生、前恶性肿瘤和恶性肿瘤的发作等。光老化通常在脸、耳、头、颈和手等经常暴露于日光的皮肤上发生。
本发明的水肿改善剂、淋巴浮肿改善剂、皱纹改善剂、肥胖改善剂、淋巴管新生和/或功能促进剂、或VEGFC产生促进剂中的凝血酸酰胺衍生物和/或其盐在药剂总量中配合20~0.001质量%,优选配合7~0.01质量%。
此外,可以根据需要,在本发明的水肿改善剂、淋巴浮肿改善剂、皱纹改善剂、肥胖改善剂、淋巴管新生和/或功能促进剂、或VEGFC产生促进剂中适当配合除了上述必要成分以外的常规化妆品、医药品等皮肤外用剂中所使用的成分,例如,美白剂、保湿剂、抗氧化剂、油性成分、紫外线吸收剂、表面活性剂、增稠剂、醇类、粉末成分、着色剂、水性成分、水、各种皮肤营养剂等。
除此以外,还可以适当配合乙二胺四乙酸二钠、乙二胺四乙酸三钠、柠檬酸钠、聚磷酸钠、偏磷酸钠、葡糖酸等金属螯合剂,泛醇乙醚、咖啡因、丹宁、维拉帕米、甘草提取物、光甘草定、木瓜的果实的热水提取物、各种生药、酵母提取物、生育酚乙酸酯、甘草酸及其衍生物或其盐等药剂,尿囊素、维生素C、抗坏血酸磷酸镁、抗坏血酸葡糖苷、熊果苷、曲酸、4-甲氧基水杨酸钾等美白剂,葡萄糖、果糖、甘露糖、蔗糖、海藻糖等糖类,视黄酸、视黄醇、乙酸视黄醇酯、棕榈酸视黄醇酯等维生素A类,L-丝氨酸、透明质酸及其衍生物等。
本发明的水肿改善剂、淋巴浮肿改善剂、皱纹改善剂、肥胖改善剂、淋巴管新生和/或功能促进剂、或VEGFC产生促进剂只要是用作例如软膏、乳膏、乳液、化妆水(lotion)、面膜(pack)、浴用剂等现有皮肤外用剂即可,此外,还可以用于美容目的,对剂型没有特别的限制。
实施例
用含有10%FBS的DMEM培养来源于人表皮的培养细胞HaCaT细胞(德国癌症研究中心(German Cancer Research Center),Heidelberg,Germany),在24孔板中接种,使每孔为15×104。在约24小时后,将培养基换成无血清的DMEM,培养24小时。其后,将候选药剂溶解在水中使其为7质量%,将溶解后的溶液以培养液的1/100、1/1000、1/10000的体积量添加以进行进一步培养。在药剂添加后48小时,回收培养上清液,按照ELISA(R&Dsystems)的规程来定量培养上清液中的VEGFC量。此外,向回收了培养上清液后的细胞中添加阿尔玛蓝(Alamar Blue)(TREK Diagnostic systems),以荧光强度(Ex 544nm,Em 590nm)的方式测定细胞量。通过用培养上清液中的VEGFC量除以阿尔玛蓝的荧光值计算得到单位细胞的VEGFC表达量。将向细胞中添加作为溶剂的70%EtOH代替药剂而作为对照,将其值作为100。此外,作为阳性对照,使用5%FBS。
由以上的筛选结果可知,凝血酸酰胺衍生物和/或其盐,特别是凝血酸甲基酰胺盐酸盐显示出剂量依赖性的、超出对照的VEGFC诱导活性(图1)。处方例1 O/W乳膏
处方        (质量%)
液体石蜡        3
凡士林          1
二甲基聚硅氧烷  1
硬脂醇         1.8
山萮醇         1.6
澳洲坚果油      2
棕榈硬化油      3
角鲨烷                                                            6
硬脂酸                                                            2
羟基硬脂酸胆甾醇酯                                                0.5
2-乙基己酸鲸蜡醇酯                                                4
聚氧乙烯硬化蓖麻油                                                0.5
自乳化型单硬脂酸甘油酯                                            3
生育酚乙酸酯                                                      0.1
视黄醇                                                            0.01
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物                   3
(商品名:KSG-16,信越化学工业(株))
4-叔丁基-4’-甲氧基二苯甲酰甲烷                                   0.05
对羟基苯甲酸酯                                                    适量
二(对甲氧基肉桂酸)单-2-乙基己酸甘油酯                             0.05
氢氧化钾                                                          0.15
六偏磷酸钠                                                        0.05
三甲基甘氨酸                                                      2
甘油                                                              8
双丙甘醇                                                          5
α-生育酚2-L-抗坏血酸磷酸二酯钾                                   1
(丙烯酰二甲基牛磺酸铵/VP)共聚物                                   0.1
(商品名:Aristoflex AVC,Clariant社)
缬草提取物                                                        0.1
凝血酸甲基酰胺盐酸盐                                              1
L-丝氨酸                                                          0.1
バイオダインEMPP                                                  0.1
乙二胺四乙酸三钠                                                  0.05
羧基乙烯基聚合物                                                  0.05
鳞片状无机复合粉体                                                10
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
云母        0.1
着色剂     适量
精制水     残余
处方例2 针对针灸 W/O乳膏
处方                                                     (质量%)
二甲基聚硅氧烷                                            3
十甲基环五硅氧烷                                          13
十二甲基环六硅氧烷                                        5
聚氧乙烯/甲基聚硅氧烷共聚物                               1
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉      1
Dow Corning 9040 Silicone Elastomer Blend                 5
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
乙酸视黄醇酯                  0.1
对羟基苯甲酸酯                适量
L-薄荷脑                      适量
三甲基甲硅烷氧基硅酸酯          2
乙醇                            2
甘油                            3
双丙甘醇                        5
聚乙二醇6000                    5
六偏磷酸钠                    0.05
生育酚乙酸酯                  0.1
咖啡因                        0.1
杏仁提取物                    0.1
凝血酸乙基酰胺盐酸盐          0.5
赤藓糖醇                                                        0.1
金缕梅提取物                                                    0.1
人参提取物                                                      0.1
バイオダインEMPP                                                1
乙二胺四乙酸三钠                                                0.05
二吗啉代哒嗪酮                                                  0.01
三甲氧基肉桂酸甲基双(三甲基甲硅烷氧基)甲硅烷基异戊酯            0.1
鳞片状无机复合粉体                                              5
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
氧化铁黄                        适量
钛酸钴                          适量
二甲基二硬脂基铵锂蒙脱石        1.5
聚乙烯醇                        0.1
羟乙基纤维素                    0.1
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物            0.1
(商品名:SIMULGEL EG,SEPPIC社)
(丙烯酰二甲基牛磺酸铵/VP)共聚物                     0.1
(商品名:Aristoflex AVC,Clariant社)
香料                            适量
精制水                          残余
处方例3 针对皱纹 O/W乳膏
处方                                    (质量%)
液体石蜡                                    8
凡士林                                      3
二甲基聚硅氧烷                              2
Dow Corning 9041 Silicone Elastomer Blend   0.1
(聚二甲基硅氧烷交联聚合物的二甲基聚硅氧烷配合物,Dow Corning社)
硬脂醇                    3
山萮醇                    2
甘油                      5
双丙甘醇                  4
海藻糖                    1
四(2-乙基己酸)季戊四醇酯  4
单异硬脂酸聚氧乙烯甘油酯  2
单硬脂酸聚氧乙烯甘油酯    1
亲油型单硬脂酸甘油酯      2
柠檬酸                    0.05
柠檬酸钠                  0.05
氢氧化钾                  0.015
油溶性甘草提取物          0.1
草木犀提取物              0.1
凝血酸丙基酰胺盐酸盐      2
尿囊素                    0.1
棕榈酸视黄醇酯(100万单位) 0.25
生育酚乙酸酯              0.1
バイオダインEMPP          5
对羟基苯甲酸酯            适量
苯氧基乙醇                适量
二丁基羟基甲苯            适量
乙二胺四乙酸三钠           0.05
4-叔丁基-4’-甲氧基二苯甲酰甲烷    0.01
对甲氧基肉桂酸2-乙基己酯            0.1
β-胡萝卜素                        0.01
聚乙烯醇                            0.5
羟乙基纤维素                                             0.5
羧基乙烯基聚合物                                         0.05
(丙烯酰二甲基牛磺酸铵/VP)共聚物                          5
(商品名:Aristoflex AVC,Clariant社)
精制水                                                   残余
香料                                                     适量
处方例4 保湿用 O/W乳膏
处方                                                    (质量%)
液体石蜡                                                 10
二甲基聚硅氧烷                                           2
Dow Corning 9045 Silicone Elastomer Blend                3
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
甘油                                                     10
1,3-丁二醇                                              2
赤藓糖醇                                                 1
聚乙二醇1500                                             5
角鲨烷                                                   15
四(2-乙基己酸)季戊四醇酯                                 5
氢氧化钾                                                 0.1
六偏磷酸钠                                               0.05
生育酚乙酸酯                                             0.05
バイオダインEMPP                                         0.1
野芝麻(Lamium album var.barbatum)提取物                  1
凝血酸环己基酰胺盐酸盐                                   0.8
异硬脂酸                                                 0.01
对羟基苯甲酸酯                                           适量
羟丙基甲基纤维素                                         0.3
聚乙烯醇                                         0.1
羧基乙烯基聚合物                                 0.2
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物         0.5
(商品名:SIMULGEL EG,SEPPIC社)
丙烯酸/甲基丙烯酸烷基酯共聚物(ペミユレンTR-2)    0.1
鳞片状无机复合粉体                                5
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
精制水                                          残余
处方例5 W/O 防晒霜
处方                                            (质量%)
二甲基聚硅氧烷                                    5
十甲基环五硅氧烷                                  10
三甲基甲硅烷氧基硅酸酯                            3
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉    5
聚氧乙烯/甲基聚硅氧烷共聚物                             3
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物         30
(商品名:KSG-16,信越化学工业(株))
双丙甘醇                                                3
2-乙基己酸鲸蜡醇酯                                      1
硅氧烷被覆微粒氧化锌(60nm)                              10
滑石                                                    1
硅氧烷被覆微粒氧化钛(40nm)                              7
バイオダインEMPP                                        1
亚牛磺酸                                                0.1
苦参提取物                                              0.01
腺苷三磷酸二钠                                          0.5
香根鸢尾根提取物                                        0.1
凝血酸苄基酰胺盐酸盐                                            0.5
乙酸视黄醇酯(150万单位)                                         0.01
对羟基苯甲酸酯                                                  适量
苯氧基乙醇                                                      适量
乙二胺四乙酸三钠                                                0.2
二甲基二硬脂基铵锂蒙脱石                                        1
聚甲基丙烯酸甲酯共聚物球状粉末                                  3
鳞片状无机复合粉体                                              1
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
云母钛                                                          0.1
精制水                                                          残余
香料                                                            适量
处方例6 O/W 乳膏
处方                                                          (质量%)
甘油                                                          3质量%
十甲基环五硅氧烷                                                  7
二甲基聚硅氧烷                                                    5
单油酸聚氧乙烯失水山梨醇酯(20E.O.)                                1
聚乙二醇20000                                                    0.5
聚乙烯醇                                                          1
乙醇                                                              5
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉              3
三甲基甲硅烷氧基硅酸酯                                            0.1
二吗啉代哒嗪酮                                                    0.1
氢氧化钾                                                          0.12
云母钛                                                            0.1
Dow Corning 9045 Silicone Elastomer Blend                         20
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
(丙烯酰二甲基牛磺酸铵/VP)共聚物                         2
(商品名:Aristoflex AVC,Clariant)
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物                0.1
(商品名:SIMULGEL EG,SEPPIC社)
卡波姆                                                  0.01
丙烯酸/甲基丙烯酸烷基酯共聚物(ペミユレンTR-2)           0.05
鳞片状无机复合粉体                                      5
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
氧化铝                                                  0.01
黄原胶                                                  0.1
羧甲基纤维素钠                                          0.05
バイオダインEMPP                                        5
凝血酸异丙基酰胺盐酸盐                                  0.4
柴胡提取物                                              0.1
棕榈酸视黄醇酯(100万单位)                               0.01
对羟基苯甲酸酯                                          适量
苯氧基乙醇                                              适量
香料                                                    适量
离子交换水                                              残余
处方例7 W/O 乳膏
处方                                                   (质量%)
双丙甘醇                                                1
十甲基环五硅氧烷                                        5
二甲基聚硅氧烷                                          1
聚氧乙烯/甲基聚硅氧烷共聚物                             2
三(2-乙基己酸)甘油酯                                            0.1
单硬脂酸聚氧乙烯失水山梨醇酯(20E.O.)                            0.05
聚乙二醇9000                                                    2
聚乙烯醇                                                        0.5
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉            5
二吗啉代哒嗪酮                                                  0.1
氢氧化钾                                                        0.03
氧化铝                                                          0.1
氧化钛                                                          1
Dow Corning 9041 Silicone Elastomer Blend                       40
(聚二甲基硅氧烷交联聚合物的二甲基聚硅氧烷配合物,Dow Corning社)
(丙烯酰二甲基牛磺酸铵/VP)共聚物                                 0.1
(商品名:Aristoflex AVC,Clariant社)
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物                        0.1
(商品名:SIMULGEL EG,SEPPIC社)
卡波姆                                                          0.01
丙烯酸/甲基丙烯酸烷基酯共聚物(ペミユレンTR-2)                   0.05
滑石                                                            1
鳞片状无机复合粉体                                              1
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
鳞片状无机复合粉体                                              1
(由在绢云母上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-20121M,触媒化成工业(株))
球状尼龙粉末                                                    1
二氧化硅                                                        1
羟乙基纤维素                                                    0.1
バイオダインEMPP                                                1
山楂提取物                                                      0.1
凝血酸甲基酰胺盐酸盐                                            0.1
4-甲氧基水杨酸钾盐                                              0.1
对羟基苯甲酸酯                                                  适量
苯氧基乙醇                                                      适量
香料                                                            适量
离子交换水                                                      残余
处方例8 皱纹/松弛防止用 O/W 乳膏
处方                                                            (质量%)
甘油                                                             5
十甲基环五硅氧烷                                                 1
十二甲基环六硅氧烷                                               3
二甲基聚硅氧烷                                                   5
甲基苯基聚硅氧烷                                                 1
辛基甲氧基肉桂酸酯                                               0.1
四(2-乙基己酸)季戊四醇酯                                         1
单月桂酸聚氧乙烯失水山梨醇酯(20E.O.)                             0.1
聚氧乙烯/甲基聚硅氧烷共聚物                                      1
(商品名:聚醚改性硅油KF-6018,信越化学工业(株))
大豆发酵提取物                                                   3
聚乙二醇6000                                                     2
柠檬酸                                                           0.1
柠檬酸钠                                                         0.1
偏磷酸钠                                                         0.05
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉             0.1
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物                  10
(商品名:KSG-16,信越化学工业(株))
Dow Corning 9041 Silicone Elastomer Blend                  5
(聚二甲基硅氧烷交联聚合物的二甲基聚硅氧烷配合物,Dow Corning社)
(丙烯酰二甲基牛磺酸铵/VP)共聚物                           0.1
(商品名:Aristoflex AVC,Clariant)
丙烯酰二甲基牛磺酸铵/山萮醇聚醚-25甲基丙烯酸酯交联聚合物0.05
(商品名:Aristoflex HMB,Clariant)
丙烯酸/甲基丙烯酸烷基酯共聚物(ペミユレンTR-2)             0.05
丙烯酸酰胺/2-丙烯酰胺-2-甲基丙烷磺酸共聚物                0.5
(商品名:SIMULGEL 600,SEPPIC社)
聚丙烯酸铵                                                0.5
(商品名:SIMULGEL A,SEPPIC社)
鳞片状无机复合粉体                                        1
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
鳞片状无机复合粉体                                         1
(由在绢云母上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-20121M,触媒化成工业(株))
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物            1
(商品名BY29-119,トウレ·ダウコ一ニング·シリコ一ン株式会社)バイオダインEMPP                                               1
杏仁提取物                                                 0.1
凝血酸甲基酰胺盐酸盐                                       1.2
腺苷三磷酸盐                                               0.01
对羟基苯甲酸酯                                             适量
苯氧基乙醇                                                 适量
香料                                                       适量
离子交换水                                                 残余
处方例9 O/W 乳液
处方                                                 (质量%)
二甲基聚硅氧烷                                       3
十甲基环五硅氧烷                                     4
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉 0.5
Dow Corning 9040 Silicone Elastomer Blend            0.5
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
乙醇                                            5
甘油                                            6
1,3-丁二醇                                     5
聚氧乙烯甲基葡糖苷                              3
向日葵油                                        1
角鲨烷                                          2
氢氧化钾                                        0.1
六偏磷酸钠                                      0.05
羟丙基-β-环糊精                                0.1
甘草酸二钾                                      0.05
枇杷叶提取物                                    0.1
L-谷氨酸钠                                      0.05
凝血酸甲基酰胺盐酸盐                            2.5
透明质酸                                        0.001
薰衣草油                                        0.1
维生素E                                         0.1
地黄提取物                                      0.1
亚牛磺酸                                        0.01
硫代牛磺酸                                      0.1
被孢霉(Mortierella)油                           0.5
熊果苷                                                  3
乙酰透明质酸钠                                          0.1
马郁兰提取物                                            0.1
バイオダインEMPP                                        0.1
二吗啉代哒嗪酮                                          0.1
黄原胶                                                  0.1
羧基乙烯基聚合物                                        0.1
丙烯酸/甲基丙烯酸烷基酯共聚物(ペミユレンTR-1)           0.1
(丙烯酰二甲基牛磺酸铵/VP)共聚物                         1
(商品名:Aristoflex AVC,Clariant社)
氧化铁红                                                适量
氧化铁黄                                                适量
鳞片状无机复合粉体                                      1
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
云母钛                                                  0.1
对羟基苯甲酸酯                                          适量
精制水                                                  残余
处方例10 O/W 乳液
处方                                                    (质量%)
二甲基聚硅氧烷                                           2
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物          15
(商品名:KSG-16,信越化学工业(株))
山萮醇                                                   1
鲨肝醇                                                   0.5
甘油                                                     5
1,3-丁二醇                                              7
赤藓糖醇                                                 2
バイオダインEMPP                               5
二氧化硅被覆氧化锌                             0.1
缬草提取物                                     0.1
凝血酸甲基酰胺盐酸盐                           0.1
绿茶提取物                                     0.1
棕榈硬化油                                     3
角鲨烷                                         6
四(2-乙基己酸)季戊四醇酯                       2
异硬脂酸聚氧乙烯甘油酯                         1
单硬脂酸聚氧乙烯甘油酯                         1
氢氧化钾                                       适量
六偏磷酸钠                                     0.05
苯氧基乙醇                                     适量
羧基乙烯基聚合物                               0.1
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物       0.1
(商品名:SIMULGEL EG,SEPPIC社)
精制水                                         残余
处方例11 O/W 乳液
处方                                                  (质量%)
液体石蜡                                               7
凡士林                                                 3
十甲基环五硅氧烷                                       2
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉   0.1
Dow Corning 9041 Silicone Elastomer Blend              3
(聚二甲基硅氧烷交联聚合物的二甲基聚硅氧烷配合物,Dow Corning社)
山萮醇                                                 1
甘油                                                   5
双丙甘醇                            7
聚乙二醇1500                        2
霍霍巴油                            1
异硬脂酸                            0.5
硬脂酸                              0.5
山萮酸                              0.5
四(2-乙基己酸)季戊四醇酯            3
2-乙基己酸鲸蜡醇酯                  3
单硬脂酸甘油酯                      1
单硬脂酸聚氧乙烯甘油酯              1
氢氧化钾                            0.1
六偏磷酸钠                          0.05
甘草次酸硬脂基酯                    0.05
L-精氨酸                            0.1
三甲基甘氨酸                        0.1
抗坏血酸-2-葡糖苷                   0.1
木糖醇                              1
香根鸢尾根提取物                    0.1
凝血酸甲基酰胺盐酸盐                1
洋蔷薇提取物                        0.1
生育酚乙酸酯                        0.1
乙酰化透明质酸钠                    0.1
バイオダインEMPP                    1
乙二胺四乙酸三钠                    0.05
4-叔丁基-4’-甲氧基二苯甲酰甲烷     0.1
对甲氧基肉桂酸2-乙基己酯            0.1
羧基乙烯基聚合物                    0.15
(丙烯酰二甲基牛磺酸铵/VP)共聚物     0.5
(商品名:Aristoflex AVC,Clariant社)
鳞片状无机复合粉体                                  0.5
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
云母钛                                              0.1
对羟基苯甲酸酯                                      适量
精制水                                              残余
香料                                                适量
处方例12 W/O 日用乳液
处方                                                (质量%)
二甲基聚硅氧烷                                       2
十甲基环五硅氧烷                                     25
十二甲基环六硅氧烷                                   10
聚氧乙烯/甲基聚硅氧烷共聚物                          1.5
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉 10
Dow Corning 9045Silicone Elastomer Blend              5
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
三甲基甲硅烷氧基硅酸酯                                 1
1,3-丁二醇                                            5
角鲨烷                                                 0.5
滑石                                                   5
甘草酸二钾                                             0.1
生育酚乙酸酯                                           0.1
バイオダインEMPP                                       0.1
L-丝氨酸                                               1
人参提取物                                             0.1
凝血酸甲基酰胺盐酸盐                                   0.7
人参提取物                                          0.1
乙二胺四乙酸三钠                                    0.05
4-叔丁基-4’-甲氧基二苯甲酰甲烷                     1
对甲氧基肉桂酸2-乙基己酯                            5
二(对甲氧基肉桂酸)单-2-乙基己酸甘油酯               1
硅氧烷被覆微粒氧化钛(40nm)                          4
二甲基二硬脂基铵锂蒙脱石                            0.5
球状聚乙烯粉末                                      3
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物            0.1
(商品名:SIMULGEL EG,SEPPIC社)
鳞片状无机复合粉体                                  1
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
云母钛                                              0.1
苯氧基乙醇                                          适量
精制水                                              残余
香料                                                适量
处方例13 化妆水
处方                                               (质量%)
乙醇                                                  5
甘油                                                  1
1,3-丁二醇                                           5
聚氧乙烯聚氧丙烯癸基十四烷基醚                        0.2
六偏磷酸钠                                            0.03
三甲基甘氨酸                                          1
聚天冬氨酸钠                                          0.1
α-生育酚2-L-抗坏血酸磷酸二酯钾                       0.1
硫代牛磺酸                                            0.1
山楂提取物                                0.1
凝血酸甲基酰胺盐酸盐                      0.5
儿茶钩藤(Uncaria gambir Roxb)提取物       0.1
西洋薄荷提取物                            0.1
α-葡糖基橙皮苷                           0.01
抗坏血酸磷酸酯镁                          0.01
4-甲氧基水杨酸钾                           1
草木犀提取物                              0.1
バイオダインEMPP                          0.01
HEDTA三钠                                 0.1
羧基乙烯基聚合物                          0.05
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物  0.05
(商品名:SIMULGEL EG,SEPPIC社)
氢氧化钾                                  0.02
苯氧基乙醇                                适量
精制水                                    残余
香料                                      适量
处方例14 化妆水
处方                                      (质量%)
乙醇                                       10
甘油                                       2
双丙甘醇                                   1
异硬脂酸                                   0.1
聚(氧乙烯·氧丙烯)/甲基聚硅氧烷共聚物      1
月桂基二甲基氨基乙酸甜菜碱                 0.1
柠檬酸                                     0.02
柠檬酸钠                                   0.08
六偏磷酸钠                                 0.01
亚牛磺酸                                 0.1
野芝麻提取物                             0.1
凝血酸甲基酰胺盐酸盐                     1
黄芩提取物                               0.1
バイオダインEMPP                         1
薰衣草油                                 0.001
(丙烯酰二甲基牛磺酸铵/VP)共聚物          0.01
(商品名:Aristoflex AVC,Clariant社)
苯氧基乙醇                               适量
活性氢水                                   1
精制水                                   残余
处方例15 面膜
处方                                     (质量%)
乙醇                                      10
1,3-丁二醇                               6
聚乙二醇4000                              2
橄榄油                                    1
澳洲坚果油                                1
羟基硬脂酸植物甾醇酯                      0.05
乳酸                                      0.05
乳酸钠                                    0.1
L-抗坏血酸硫酸酯二钠                      0.1
α-生育酚2-L-抗坏血酸磷酸二酯钾           0.1
生育酚乙酸酯                              0.1
草木犀提取物                              0.1
凝血酸乙基酰胺盐酸盐                      0.1
糖蜜提取物                                1
软骨素硫酸钠                              0.1
バイオダインEMPP                                      3
羧甲基纤维素钠                                        0.2
聚乙烯醇                                              12
(丙烯酰二甲基牛磺酸铵/VP)共聚物                       2
(商品名:Aristoflex AVC,Clariant社)
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物              0.1
(商品名:SIMULGEL EG,SEPPIC社)
Dow Corning 9041 Silicone Elastomer Blend             3
(聚二甲基硅氧烷交联聚合物的二甲基聚硅氧烷配合物,Dow Corning社)
对羟基苯甲酸酯                                        适量
精制水                                                残余
香料                                                  适量
处方例16 粉末固体粉底
处方                                                  (质量%)
二甲基聚硅氧烷                                          5
Dow Corning 9045 Silicone Elastomer Blend               5
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
异硬脂酸                                                 0.5
苹果酸二异硬脂基酯                                       3
三(2-乙基己酸)甘油酯                                     1
倍半异硬脂酸失水山梨醇酯                                 1
球状PMMA被覆云母                                         6
プリズムト一ンパウダ一YR                                 1
微粒氧化锌                                               0.5
微粒氧化钛                                               2
合成金云母                                               2
金属皂处理滑石                                        8
球状二氧化硅                                          5
生育酚乙酸酯                                          0.1
δ-生育酚                                             0.1
杏仁提取物                                            0.1
凝血酸甲基酰胺盐酸盐                                  2
バイオダインEMPP                                      0.1
对羟基苯甲酸酯                                        适量
三甲氧基肉桂酸甲基双(三甲基甲硅烷氧基)甲硅烷基异戊酯  1
对甲氧基肉桂酸2-乙基己酯                              3
球状聚丙烯酸烷基酯粉末                                6
甲基氢聚硅氧烷被覆滑石                                残余
甲基氢聚硅氧烷被覆绢云母                              5
甲基氢聚硅氧烷被覆氧化钛                              15
鳞片状无机复合粉体                                    10
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
云母钛                                                1
甲基氢聚硅氧烷被覆颜料(着色剂)                        5
处方例17 粉末固体粉底
处方                                                 (质量%)
纯地蜡(Ceresin)                                       0.5
二甲基聚硅氧烷                                        2
甲基苯基聚硅氧烷                                      1
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物       10
(商品名:KSG-16,信越化学工业(株))
角鲨烷                                                7
角鲨烷(植物性)                                        1
倍半异硬脂酸失水山梨醇酯                              1
甘油改性硅树脂被覆烧成绢云母                          16
甘油改性硅树脂被覆绢云母                              7
氧化铁黄被覆云母钛                                    0.1
微粒氧化钛                                            5
滑石                                                  10
氧化钛被覆绢云母                                      0.1
氮化硼                                                2.5
氧化铁红被覆云母钛                                    0.1
植物甾醇                                              0.1
抗坏血酸二棕榈酸酯                                    0.1
DL-α-生育酚乙酸酯                                    0.1
D-δ-生育酚                                           0.1
バイオダインEMPP                                      0.1
山楂提取物                                            0.1
凝血酸甲基酰胺盐酸盐                                  0.5
对羟基苯甲酸酯                                        适量
对甲氧基肉桂酸2-乙基己酯                              1
球状聚丙烯酸烷基酯粉末                                8
甲基氢聚硅氧烷被覆云母                                残余
甲基氢聚硅氧烷被覆氧化铁氧化钛烧结物                  5
甲基氢聚硅氧烷被覆绢云母                              5
甲基氢聚硅氧烷被覆氧化钛                              4
甲基氢聚硅氧烷被覆片状氧化钛                          5
甲基氢聚硅氧烷被覆颜料(着色剂)                        5
香料                                                  适量
处方例18 粉末固体粉底
处方                                                  (质量%)
α-烯烃低聚物                                                     3
凡士林                                                            3
Dow Corning 9040 Silicone Elastomer Blend                         3
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
澳洲坚果油                                                        0.1
倍半异硬脂酸失水山梨醇酯                                          1
烷基改性硅树脂被覆氧化铁黄                                        2
烷基改性硅树脂被覆氧化铁红                                        1
烷基改性硅树脂被覆氧化铁黑                                        0.5
氧化铁黄被覆云母钛                                                5
合成金云母                                                        5
氧化钛                                                            1
氧化锌                                                            1
低温烧成氧化锌                                                    4
烧成绢云母                                                        10
金云母                                                            1
氧化铝                                                            1
鳞片状无机复合粉体                                                15
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
滑石                                                               残余
合成金云母                                                         5
交联型硅氧烷粉末(トレフイルE-506)                                  10
DL-α-生育酚乙酸酯                                                 0.1
D-δ-生育酚                                                        0.1
バイオダインEMPP                                                   5
对羟基苯甲酸酯                                                     适量
杏仁提取物                                                         0.1
凝血酸己基酰胺盐酸盐                                               0.5
对甲氧基肉桂酸2-乙基己酯                                           1
藻酸钙粉末                                                         1
香料                                                               适量
处方例19    固体粉底
处方                                                               (质量%)
α-烯烃低聚物                                                      10
微晶蜡                                                             0.5
Dow Corning 9041 Silicone Elastomer Blend                          3
(聚二甲基硅氧烷交联聚合物的二甲基聚硅氧烷配合物,Dow Corning社)
纯地蜡                                                              5
二甲基聚硅氧烷                                                      15
甲基苯基聚硅氧烷                                                    10
澳洲坚果油                                                          0.1
巴西棕榈蜡                                                          0.1
三(2-乙基己酸)甘油酯                                                7
2-乙基己酸鲸蜡醇酯                                                  10
倍半异硬脂酸失水山梨醇酯                                            1.5
云母                                                                0.5
硬脂酸铝                                                            1
交联型硅氧烷粉末(トレフイルE-506)                                   8
N-月桂酰-L-赖氨酸                                                   0.1
D-δ-生育酚                                                         适量
バイオダインEMPP                                                    0.1
草木犀提取物                                                        0.1
凝血酸甲基酰胺盐酸盐                                                0.3
氧化铁红                                                    适量
氧化铁黄                                                    适量
藻酸钙粉末                                                    1
尼龙粉末                                                    残余
球状二氧化硅                                                  1
氧化钛                                                        1
处方例20    乳化粉底
处方                                                         (质量%)
微晶蜡                                                         1
二甲基聚硅氧烷                                                 15
十甲基环五硅氧烷                                                2
Dow Corning 9045 Silicone Elastomer Blend                       3
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉            0.5
1,3-丁二醇                                                      6
小烛树蜡                                                         3
异硬脂酸                                                         1
乙二醇脂肪酸酯                                                   0.1
羊毛脂脂肪酸辛基十二烷基酯                                       0.5
2-烷基-N-羧甲基-N-羟乙基咪唑输甜菜碱                             4
氧化钛                                                           7.5
硫酸钡                                                           5
氧化钛                                                           7
滑石                                                             3
二氧化硅                                                         4
交联型硅氧烷粉末(トレフイルE-506)                                0.1
偏磷酸钠                                                         0.1
羟丙基-β-环糊精                                                      0.1
DL-α-生育酚乙酸酯                                                    0.1
金缕梅提取液                                                          0.1
芍药提取物                                                            0.1
软骨素硫酸钠                                                          0.1
透明质酸钠                                                            0.1
バイオダインEPP                                                       0.1
野芝麻提取物                                                          0.1
凝血酸甲基酰胺盐酸盐                                                  0.1
对羟基苯甲酸酯                                                        适量
氧化铁红                                                              适量
氧化铁黄                                                              适量
氧化铁黑                                                              适量
鳞片状无机复合粉体                                                    1
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
黄原胶                                                                0.1
羧甲基纤维素钠                                                        0.1
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物                              0.5
(商品名:SIMULGEL EG,SEPPIC社)
秋海棠提取物                                                           2
精制水                                                                残余
处方例21  W/O粉底
处方                                                                (质量%)
二甲基聚硅氧烷                                                         3
十甲基环五硅氧烷                                                       10
聚氧乙烯/甲基聚硅氧烷共聚物                                            3
十二甲基环六硅氧烷                                                     5
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉  0.1
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物       5
(商品名:KSG-16,信越化学工业(株))
甘油                                                  4
1,3-丁二醇                                           5
棕榈酸                                                0.5
二硬脂基二甲基氯化铵                                  0.2
金属皂处理滑石                                        2
交联型硅氧烷粉末(トレフイルE-506)                     0.1
氧化铁红被覆云母钛                                    0.5
N-月桂酰-L-赖氨酸                                     2
L-谷氨酸钠                                            2
生育酚乙酸酯                                          0.1
δ-生育酚                                             0.1
对羟基苯甲酸酯                                        适量
苯氧基乙醇                                            0.2
球状尼龙粉末                                          1
球状聚丙烯酸烷基酯粉末                                3
草木犀提取物                                          0.1
凝血酸甲基酰胺盐酸盐                                  2
バイオダインEMPP                                      5
精制水                                                残余
糊精脂肪酸酯处理滑石                                  3
糊精脂肪酸酯处理二氧化钛                              15
糊精脂肪酸酯处理氧化铁黄                              3
糊精脂肪酸酯处理氧化铁黑                              0.5
处方例22 O/W 粉底
处方                                                  (质量%)
二甲基聚硅氧烷                              8
Dow Corning 9040 Silicone Elastomer Blend    20
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
山萮醇                                      0.5
鲨肝醇                                      0.5
1,3-丁二醇                                 5
澳洲坚果油                                  0.1
异硬脂酸                                    1.5
硬脂酸                                      1
山萮酸                                      0.5
2-乙基己酸鲸蜡醇酯                          5
单硬脂酸聚氧乙烯甘油酯                      1
自乳化型单硬脂酸甘油酯                      1
氧化铁黄被覆云母钛                          2
氧化钛                                      4
滑石                                        0.5
高岭土                                      3
合成金云母                                  0.1
交联型硅氧烷末                              0.1
二氧化硅                                    5
氢氧化钾                                    0.2
三乙醇胺                                    0.8
DL-α-生育酚乙酸酯                          0.1
透明质酸钠                                  0.1
バイオダインEMPP                            0.1
香根鸢尾根提取物                            0.1
凝血酸甲基酰胺盐酸盐                        0.1
对羟基苯甲酸酯                                       适量
对甲氧基肉桂酸2-乙基己酯                             1
氧化铁红                                             适量
氧化铁黄                                             适量
氧化铁黑                                             适量
黄原胶                                               0.1
丙烯酸钠/2-丙烯酰胺-2-甲基丙烷磺酸共聚物             1
(商品名:SIMULGEL EG,SEPPIC社)
膨润土                                               1
鳞片状无机复合粉体                                   5
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
羧甲基纤维素钠                                       0.1
精制水                                               残余
香料                                                 适量
处方例23 粉底
处方                                                (质量%)
十二甲基环六硅氧烷                                   15
十甲基环五硅氧烷                                     残余
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉 5
Dow Corning 9041 Silicone Elastomer Blend            30
(聚二甲基硅氧烷交联聚合物的二甲基聚硅氧烷配合物,Dow Corning社)
乙醇                                                 10
异硬脂酸                                             0.5
肉豆蔻酸处理氧化锌                                   0.5
棕榈酸糊精酯被覆氧化钛                               10
棕榈酸糊精酯被覆滑石                                 7
硅氧烷表面处理氧化钛(30nm)                                        5
交联型硅氧烷粉末                                                  1
球状二氧化硅                                                      2
磷酸L-抗坏血酸镁                                                  0.2
DL-α-生育酚乙酸酯                                                0.1
D-δ-生育酚                                                       0.1
谷胱甘肽                                                          0.1
缬草提取物                                                        0.1
凝血酸甲基酰胺盐酸盐                                              0.1
柴胡提取物                                                                1
バイオダインEMPP                                                  2
对甲氧基肉桂酸2-乙基己酯                                          5
棕榈酸糊精酯被覆氧化铁红                                          适量
棕榈酸糊精酯被覆氧化铁黄                                          适量
棕榈酸糊精酯被覆氧化铁黑                                          适量
香料                                                              适量
处方例24 底妆
处方                                                              (质量%)
二甲基聚硅氧烷                                                    5
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉              0.1
Dow Corning 9045 Silicone Elastomer Blend                         30
(聚二甲基硅氧烷交联聚合物的十甲基环五硅氧烷配合物,公司名DowCorning)
十甲基环五硅氧烷                                                   残余
乙醇                                                               8
绀青被覆云母钛                                                     0.5
鳞片状无机复合粉体                                                 5
(由在滑石上被覆氧化钛、氧化铝、二氧化硅而获得,商品名:カバ一リ一フAR-80,触媒化成工业(株))
甲基硅氧烷网状聚合物                                       5
交联型硅氧烷粉末(トレフイルE-506)                          5
柠檬酸                                                     0.02
柠檬酸钠                                                   0.08
生育酚乙酸酯                                               0.1
δ-生育酚                                                  0.1
姜黄提取物                                                 0.01
缬草提取物                                                 0.1
凝血酸甲基酰胺盐酸盐                                       3
バイオダインEMPP                                           0.1
精制水                                                     1
聚(氧乙烯·氧丙烯)·甲基聚硅氧烷共聚物                     5
处方例25 底妆
处方                                                      (质量%)
二甲基聚硅氧烷                                             5
3-三(三甲基甲硅烷氧基)甲硅烷基丙基氨基甲酸酯支链淀粉       1
(聚二甲基硅氧烷/乙烯基聚二甲基硅氧烷)交联聚合物            15
(商品名:KSG-16,信越化学工业(株))
十甲基环五硅氧烷                                           25
聚氧乙烯/甲基聚硅氧烷共聚物                                3
甘油                                                       1
1,3-丁二醇                                                5
木糖醇                                                     0.5
异硬脂酸                                                   0.5
烷基改性硅树脂被覆二氧化硅                                 2
滑石                                                       0.5
硬脂酸铝                                                   1
氧化铁红被覆云母钛                0.1
六偏磷酸钠                        0.05
甘草酸二钾                        0.1
L-丝氨酸                          0.1
小连翘提取物                      0.1
DL-α-生育酚乙酸酯                0.2
硫代牛磺酸                        0.1
刺梨提取物                        0.1
芍药提取物                        0.1
杏仁提取物                        0.1
凝血酸甲基酰胺盐酸盐              0.1
溶血卵磷脂                        0.01
乙酰化透明质酸钠                  0.1
虎耳草提取物                      0.1
バイオダインEMPP                  0.1
对羟基苯甲酸酯                    适量
苯氧基乙醇                        适量
棕榈酸糊精酯被覆氧化铁黄          0.1
二甲基二硬脂基铵锂蒙脱石          1
精制水                            残余
三甲基甲硅烷氧基硅酸酯            1.5
球状二氧化硅                      1
球状聚乙烯粉末                    5
香料                              适量
处方例26 片剂
处方                              (质量%)
微晶纤维素                        35.0
精制白糖                          29.0
羧甲基纤维素            10.0
玉米淀粉                10.0
滑石                    10.0
聚乙烯基吡咯烷酮        5.0
香根鸢尾根提取物        0.1
凝血酸甲基酰胺盐酸盐    1.0

Claims (6)

1.一种水肿改善剂,其特征在于,含有下述通式(I)所表示的凝血酸酰胺衍生物和/或其盐,
Figure FPA00001184986800011
式中,R1和R2表示氢原子、碳数为1~18的直链状或支链状烷基、碳数为5~8的环烷基、苄基或下述通式(II),R1和R2可以彼此相同也可以不同,
Figure FPA00001184986800012
其中,X表示低级烷基、低级烷氧基、羟基、氨基或卤原子,n=0~3。
2.一种淋巴浮肿改善剂,其特征在于,含有权利要求1所述的凝血酸酰胺衍生物和/或其盐。
3.一种皱纹改善剂,其特征在于,含有权利要求1所述的凝血酸酰胺衍生物和/或其盐。
4.一种肥胖改善剂,其特征在于,含有权利要求1所述的凝血酸酰胺衍生物和/或其盐。
5.一种淋巴管新生和/或功能促进剂,其特征在于,含有权利要求1所述的凝血酸酰胺衍生物和/或其盐。
6.一种VEGFC产生促进剂,其特征在于,含有权利要求1所述的凝血酸酰胺衍生物和/或其盐。
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CN103732207B (zh) * 2011-08-05 2016-01-13 株式会社资生堂 液态皮肤外用剂组合物
US10493013B2 (en) 2011-08-05 2019-12-03 Shiseido Company, Ltd. Liquid skin-conditioning composition
CN103442684A (zh) * 2012-02-10 2013-12-11 株式会社资生堂 水包油型乳化皮肤化妆品
CN103442684B (zh) * 2012-02-10 2016-11-30 株式会社资生堂 水包油型乳化皮肤化妆品
CN114288200A (zh) * 2016-11-28 2022-04-08 宝丽化成工业有限公司 皱纹改善剂
CN112714643A (zh) * 2018-09-14 2021-04-27 株式会社资生堂 油包水型皮肤外用组合物
CN112714643B (zh) * 2018-09-14 2024-02-02 株式会社资生堂 油包水型皮肤外用组合物

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