CN1395918A - 5'-脱氧-5'-甲硫腺苷在皮肤用美容组合物中的用途 - Google Patents
5'-脱氧-5'-甲硫腺苷在皮肤用美容组合物中的用途 Download PDFInfo
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- CN1395918A CN1395918A CN02123809.XA CN02123809A CN1395918A CN 1395918 A CN1395918 A CN 1395918A CN 02123809 A CN02123809 A CN 02123809A CN 1395918 A CN1395918 A CN 1395918A
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- skin
- deoxidation
- methylthioadenosine
- acid
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Abstract
本发明涉及将5′-脱氧-5′-甲硫腺苷在皮肤美容组合物中用于改善皮肤外观的用途,还涉及该组合物和一种皮肤用美容护理方法。
Description
发明领域
本发明涉及5′-脱氧-5′-甲硫腺苷在皮肤用美容组合物中用于改善皮肤外观的用途,还涉及该组合物和一种皮肤用美容护理方法。
背景技术
人体皮肤会经受非皮肤病类的变化,但一般认为仍需要对那些损伤进行改善。这些变化例如包括老化过程,其可分为内源性过程(序时自然老化)和外来因素。此外,诸如油性皮肤或干性皮肤、其他确定的因素以及并不能完全确定的影响因素也会引起皮肤外观的暂时或持久性变化,
外来因素例如包括日光或具有相应光谱的人工辐射源,以及辐射所形成的化合物,例如活性不确定的(如自由基或离子)光合产物。不过,这些因素还包括损伤或活性化合物,如臭氧,自由基例如羟基,单线态氧和其他活性氧或氮化合物,吸烟,天然和合成毒素,以及其他干扰皮肤的自然生理学或形态学的因素。这些因素的作用会例如造成对皮肤细胞DNA的直接损伤,以及造成细胞外液中胶原蛋白、弹性蛋白和糖胺聚糖分子的直接损伤,它们的作用是保持皮肤强度。此外,损害性影响也可以导致对皮肤细胞本身的损伤。因此,皮肤的再生能力例如会降低。此外,这会造成炎性反应,特别是免疫调节剂如白介素、前列腺素和组胺会发生作用。
老化的结果是皮肤变薄,表皮和真皮结构弱化,细胞数和血管分布减少。老化过程会导致细纹和皱纹的形成,皮肤角质化、变黄和松弛,并会引起色素性疾病。
已知经日光照射会对皮肤造成大量不利作用:主要的急性反应的实例有红斑、光敏化和免疫改变,长期作用会出现光致老化和癌变。此外,已知皮肤经辐射后,会诱导令基质降解的酶,低分子量化合物如视黄酸可降低该诱导作用。紫外线辐射的另一效果是皮肤细胞的灼伤效果。结果,会发生坏死过程,从而引发或强化炎性反应。
同样的因素还会作用于头发,也发生损伤。头发会变脆,弹性降低和无光泽;头发结构的表面会发生损伤。
因此,对化妆品组合物的性质存在多种需求。例如,其具体应当具有自由基清除作用,抗氧化作用或滋润作用,其应当能预防或降低基质降解酶的活性和/或调节新的胶原蛋白、弹性蛋白和/或蛋白聚糖的合成。
WO-A-97/30713中描述了用于抑止因应激反应造成的不可逆的细胞改变的组合物,该应激反应特别是因缺氧引起的,例如对于离体贮存的细胞,如移植用器官的情况,和对于活体内多种手术介入的情况。这些组合物中含有至少一种生理相容的嘌呤衍生物,优选嘌呤核糖甙。该文献还描述了用于贮存细胞、食品组合物的组合物。但并未描述这些组合物可用于局部。
EP-A-0526866中描述了腺苷化合物如5′-脱氧-5′-甲硫腺苷在制备治疗局部缺血的药物组合物中的用途。
EP-A-0352609涉及腺苷衍生物如5′-脱氧-5′-甲硫腺苷在制备治疗免疫刺激作用的药物组合物中的用途。
EP-A-0184248中描述了5′-脱氧-5′-甲硫腺苷和长链磺酸的盐,其具有中央和外周血管舒张作用,抗血小板凝集作用,抗炎作用,镇痛作用和解热作用。
US4373097中描述了用于制备腺苷如5′-脱氧-5′-甲硫腺苷的方法,以及其抗炎、镇痛和解热作用。
R.Tritapepe和C.Pozzi在《Acta Therapeutica》,15,1989,299-311页中描述了5′-甲硫腺苷用于局部治疗静脉疾病的用途,如浅层血栓静脉炎、急性血栓静脉炎、静脉曲张和静脉曲张性溃疡。并未描述5′-甲硫腺苷在美容中的用途。
G.Pinto等人在《Drug Invest》1992,4(3),205-214页中描述了5′-甲硫腺苷用于治疗慢性静脉机能不全、痔疮、浅层静脉炎症状的局部应用。也未描述其美容用途。
M.A.Cerri等人在《European Journal of Pharmacology》232,1993,291-294页中描述了通过5′-甲硫腺苷抑止细胞激动素产生和粘连抗原的内皮表达的作用。
EP-A-0191561中描述了抗龋齿或牙周炎(parodentosis)的组合物,其中含有作为活性成分的腺苷或腺苷衍生物,如5′-脱氧-5′-甲硫腺苷。
EP-A-0387757描述了5′-脱氧-5′-甲硫腺苷在制备口用、和刺激秃发人群头发生长的局部用药物组合物中的用途。
EP-A-0387756涉及5′-脱氧-5′-甲硫腺苷在药物组合物中的用途,该组合物适用于降低头部皮脂过度分泌和与此有关的头屑形成,以及皮肤瘙痒。这些组合物适于口用和局部应用。
WO-A-94/14428中描述了一种降低哺乳动物头发生长的方法,其中是将有效量的巯基活性化合物用于皮肤。该巯基活性化合物可以是5′-脱氧-5′-甲硫腺苷。
WO98/15276中描述了调节皮肤或头发中黑色素生成的方法,其中是应用有效量的药物制剂,其中含有所述调节剂。该调节剂可以是腺苷-2受体拮抗剂,如5′-脱氧-5′-甲硫腺苷。
发明概述
本发明的一个目的是提供一种用于皮肤和/或头发的美容护理方法,其适用于改善皮肤的外观。该方法具体适用于护理皮肤外观因老化导致的美容方面的不利变化。此外,本发明还旨在尽可能地防止皮肤和头发受损和/或发生不利的外观变化。
我们意外地发现可通过在皮肤用美容组合物中采用5′-脱氧-5′-甲硫腺苷达到本发明的目的。
本发明中,“皮肤外观的改善”是指皮肤外观上各种积极的美容方面的变化,或者用户认为是积极的美容方面的任何变化。本发明中对皮肤外观美容方面的不利变化进行护理的应用涉及用户主要出于审美观点而进行的应用。其中不涉及或仅涉及少数主要出于医疗目的应用。本发明的应用不包括刺激或减少毛发生长,也不包括以物理隔离剂的形式在刺激皮肤晒黑和保护皮肤免受紫外线损伤(防晒组合物)的局部用组合物中的应用。不过,本发明的应用具体包括对经日光作用(同时)引起的皮肤变化的美容护理。
本发明所用的术语“5′-脱氧-5′-甲硫腺苷”是指式I所示的化合物:
式I的化合物还涉及5′-甲硫腺苷、MTA、7-[四氢-3,4-二羟基-5-(甲硫甲基)-2-呋喃基]腺嘌呤和维生素L2。
式I的化合物可以是纯的光学异构体形式或混合物形式。
本发明的应用还包括美容适用的盐。优选5′-脱氧-5′-甲硫腺苷的美容适用的盐是酸加成盐。
酸加成盐包括无机盐,例如磷酸盐,或羧酸盐,如单不饱和或多不饱和C6-C30单羧酸,如辛酸、壬酸、癸酸、十一烷酸、月桂酸、十三烷酸、肉豆蔻酸、十五烷酸、棕榈酸、十七烷酸、硬脂酸、十九烷酸、二十烷酸、二十二烷酸、二十四烷酸、二十六烷酸、三十烷酸、棕榈油酸、油酸、亚油酸、亚麻酸、十八碳三烯酸(elaostearic acid),和羟基羧酸,如乳酸,多羟基羧酸,如柠檬酸,以及它们的混合物。
5′-脱氧-5′-甲硫腺苷及其盐有助于预防和护理个体、优选哺乳动物、特别是人体、有益动物或家禽的角化表面的损伤,角化表面是指皮肤和皮肤附件,例如头发、指甲等。本发明的应用为化妆品组合物的形式,如体用护理组合物,修饰化妆品等,其一般不需要医生处方。其有别于皮肤用制剂,皮肤用制剂是指用于治疗皮肤疾病(皮肤病)的药物。
基于5′-脱氧-5′-甲硫腺苷和/或其盐的美容制剂可有效地防止氧化过程、防止由辐射或活性化合物引起的过程、防止由这些过程引起的直接或非直接损伤。其适用于护理皮肤和毛发在美容方面或皮肤学上的改变,如皮肤老化、皮肤滋润性降低、皮肤弹性降低、皱纹、细纹、色素性疾病或老年斑的形成。
此外,本发明涉及用于皮肤外观的不利改变如痤疮或油性皮肤的美容护理或预防。
5′-脱氧-5′-甲硫腺苷特别优选适用于皮肤用美容组合物中,该组合物用于由老化导致的皮肤外观改善的护理。MTA在此起皮肤恢复和/或再生作用。通常也能观察到激活作用。具体说,5′-脱氧-5′-甲硫腺苷对线粒体的功能具有积极作用。由此,意外地发现不仅可预防皮肤的氧化损伤,还能至少是部分修复现存的损伤。根据记录,本发明的应用可改善皮肤的含水量值和/或弹性。5′-脱氧-5′-甲硫腺苷还可用于促进胶原蛋白和/或弹性蛋白的进一步合成。这通常会导致至少部分细纹平滑,并且令面色更为光亮和清新。通常,所述的有益效果还伴随有具有整体的“年轻”皮肤的积极的个人使用感。
基于5′-脱氧-5′-甲硫腺苷的制剂还适用于皮肤或毛发的处理、护理和清洁,并且可用作美容用彩妆产品。采用了5′-脱氧-5′-甲硫腺苷的皮肤用美容组合物中一般包含至少一种美容适用的载体。适用的载体见下文。优选其中含有0.001-30%(重量)活性成分。本发明的组合物根据活性成分在角质层的渗透性能和其在皮肤上形成涂层的性能而有所不同。
根据优选实施方案,本发明中适于将5′-脱氧-5′-甲硫腺苷和/或其盐以常规方式应用,例如为在一段时间内持续应用的化妆品制剂形式。这要根据所需目的而定,即所述的一段时间可以持续用户的终生时间,优选大于3个月时间,如果旨在皮肤上形成涂层,则特别优选1周至2个月。对于晒后应用,本发明适用的周期是应用一次,但优选时间为至少1天,特别优选3天至3个月,特别优选1周至2周。
本发明中,适于以0.1μg/cm2至2mg/cm2的用量局部应用5′-脱氧-5′-甲硫腺苷制剂,应用从每周1次到每日4-5次,优选每周3次到每日3次,特别优选每日1-2次。活性成分的用量和比例要根据达到适宜改变所需的具体活性成分即盐及衍生物而定。
晒后用5′-脱氧-5′-甲硫腺苷的施用形式和任选加入的活性成分有利地具有渗透性能,其能令活性成分快速渗入皮肤。另一方面,对于具有“预调理”特点的应用,快速渗透性能通常并不重要,而能在皮肤上形成涂层的性能是有利的。
本发明意外地可对以下情况进行有效护理和预防:皮肤和/或皮肤附件的早老化(例如皱纹、老年斑、毛细血管舒张、色素性疾病),辐射导致的皮肤损伤,或辐射导致的皮肤和/或皮肤附件的不利变化,环境因素(臭氧、自由基、单线态氧、活性氧或氮化合物、吸烟、毒素)导致的皮肤损伤,或环境因素导致的皮肤和/或皮肤附件的不利变化,皮肤和/或皮肤附件的光致敏化,炎症,红斑,变态反应或自身免疫反应变化(特别是痤疮,油性或干性皮肤,角化,酒渣鼻,皮肤病,特应性湿疹,皮脂溢性湿疹,光照性皮肤病,多形性光照性皮肤病),皮肤和/或皮肤附件的机能不全、敏化或机能减退状况,瘙痒,干性皮肤状况和角质层隔离功能疾病和/或脱发和头发生长降低。
5′-脱氧-5′-甲硫腺苷和/或其盐的新的美容应用还可意外地和预料不到地用于缓解敏感性或受刺激的皮肤。其还可调节胶原蛋白、透明质酸和弹性蛋白的合成,刺激DNA合成,特别是对于皮肤机能不足或机能退化的状况,可以调节令基质降解的酶特别是金属蛋白酶的转录和表达,促进细胞更新和皮肤再生,促进皮肤自身对DNA、脂类和/或蛋白的保护和修复机制。5′-脱氧-5′-甲硫腺苷还可用于外科介入后护理用美容组合物中,特别是抑止皮肤刺激作用和促进损伤皮肤的再生过程。
本发明中,可将该化妆品制剂以常用于美容的形式、以足量用于皮肤和/或头发上。
例如5′-脱氧-5′-甲硫腺苷或其盐可用于皮肤清洁用美容组合物中,如浴皂、清洁皂、保健皂、透明皂、高级香皂、去臭皂、润肤皂、儿童皂、皮肤保护用皂、磨砂皂、合成洗涤剂、液体皂、皂膏、软性皂、膏状洗涤剂、液体洗涤剂、洗浴和沐浴用制剂,例如清洗液、淋浴用制剂、透明浴液、泡沫浴剂、润肤泡沫浴剂、浴油、浴用提取物、摩擦制剂、现用产品,泡沫剃须制剂、剃须后乳液,剃须后膏霜。
5′-脱氧-5′-甲硫腺苷还适用于皮肤美容制剂中,如油包水或水包油型皮肤用和体用膏霜,日霜和晚霜,眼霜,晒后产品,护手产品,面霜,复合乳化体,凝胶,微乳液,脂质体制剂,niosome制剂,抗皱霜,面油,含脂质体凝胶,运动用凝胶,滋润膏霜,增白膏霜,维生素膏霜,皮肤乳液,护肤乳液,蜂窝组织炎用膏霜,脱色素组合物,按摩制剂,爽身粉,爽肤水,面膜,去臭剂,抑汗剂,去黑头鼻贴,抗痤疮组合物,驱虫剂,剃须组合物,个人卫生组合物,足部护理组合物,婴儿护理组合物和其他产品。
此外,5′-脱氧-5′-甲硫腺苷或其盐可用于护发化妆品组合物中,如头发护理剂,发用乳液,头发漂洗剂,发用乳剂,头发分叉修复液,烫发用中和剂,局油用制剂,调理剂,定型乳液,洗发剂,染发剂和头发着色剂,喷发胶,吹风制剂,吹风定型组合物,喷雾亮发剂,头发光亮剂,发用定型产品,生发剂和其他产品。
5′-脱氧-5′-甲硫腺苷或其盐还适用于修饰化妆品制剂中,例如彩妆品,粉剂,胭脂,眼影,眼影笔、眼线笔、眼部粉底霜、唇膏、眉笔、轮廓笔、遮瑕棒剂、舞台用彩妆品、睫毛膏、睫毛染色和着色产品、卸妆产品或其他产品。
化妆品卫生制剂可根据所用领域制成喷雾剂(泵送喷雾剂或气溶胶)、泡沫、凝胶、凝胶喷雾剂、乳液、膏霜、摩丝、软膏、悬浮剂或粉剂形式。
还适于将5′-脱氧-5′-甲硫腺苷或其盐任选地与其他活性成分共同制成胶囊形式,例如为纤维素包封、包封于明胶、聚酰胺、niosome、蜡基质、环糊精中,或以脂质体形式包埋。
该制剂中可含有常用于这类制剂中的化妆品辅剂,例如防腐剂,杀菌剂,香精,消泡剂,染料,颜料,增稠剂,表面活性剂,乳化剂,润滑剂,涂饰剂,脂肪,油类,蜡,或其他常用于化妆品或皮肤制剂的组分,如醇,多元醇,聚合物,泡沫稳定剂,增溶剂,电解质,有机酸,有机溶剂,或聚硅氧烷衍生物。
除所述的活性成分,该制剂中还可含有其他具有抗氧化作用、自由基清除作用、皮肤滋润作用或保湿作用、去红斑作用、抗炎作用的化合物,以补充或增强本发明的作用。具体说,这些化合物可选自维生素、植物提取物、α-和β-羟基酸,神经酰胺、抗炎剂、抗微生物剂和紫外线滤除剂,及其衍生物和混合物。
抗氧剂适于选自氨基酸(例如甘氨酸,组氨酸,酪氨酸,色氨酸)及其衍生物,咪唑(例如,尿刊酸)及其衍生物,肽,如D,L-肌肽,D-肌肽、L-肌肽及其衍生物(例如,鹅肌肽),类胡萝卜素,胡萝卜素(例如α-胡萝卜素,β-胡萝卜素,番茄红素)及其衍生物,绿原酸及其衍生物,金硫葡糖,丙基硫氧嘧啶和其他硫醇(例如硫氧还蛋白,谷胱甘肽,半胱氨酸,胱氨酸,胱胺,及其葡糖基、N-乙酰基、甲基、乙基、丙基、戊基、丁基和月桂基、棕榈酰基、油基、γ-蓖麻油基、胆甾醇基和甘油基酯)及其盐,硫代二丙酸二月桂醇酯,硫代二丙酸二硬脂酸酯,硫代二丙酸及其衍生物(酯,醚,肽,脂类,核苷酸,核苷和盐),以及极低耐受剂量(例如pmol/kg至μmol/kg)的磺化亚胺(sufoximine)化合物(例如丁硫堇(buthionine)磺化亚胺,高半胱氨酸磺化亚胺,丁硫堇砜,戊-、己-、庚-硫堇磺化亚胺),还有(金属)螯合剂(例如α-羟基脂肪酸,棕榈酸,植酸,乳铁蛋白),α-羟基酸(例如柠檬酸,乳酸,苹果酸),腐殖酸,胆汁酸,胆汁提取物,胆红素,胆绿素,EDTA,EGTA及其衍生物,不饱和脂肪酸及其衍生物(例如γ-亚麻酸,亚油酸,油酸),叶酸及其衍生物,泛醌和泛醌醇及其衍生物,维生素C及其衍生物(例如抗坏血酸基棕榈酸酯,抗坏血酸基磷酸镁,抗坏血酸基乙酸酯),生育酚及其衍生物(例如乙酸维生素E),维生素A及其衍生物(棕榈酸维生素A),以及来自安息香树脂的苯甲酸松脂,芸香亭酸及其衍生物,丁羟基甲苯,丁羟基苯甲醚,去甲二氢愈创木脂酸,去甲二氢愈创木酸,三羟基丁酰苯,尿酸及其衍生物,甘露糖及其衍生物,芝麻油,麻油酚,锌及其衍生物(例如ZnO,ZnSO4),硒及其衍生物(例如甲硫氨酸硒),1,2-二苯乙烯及其衍生物(例如氧化1,2-二苯乙烯,反式氧化1,2-二苯乙烯),以及所述活性成分适用于本发明的衍生物(盐,酯,醚,糖,核苷酸,核苷,肽和脂类)。
抗氧剂可单用或以混合物形式应用。单用或共用的抗氧剂的用量优选占制剂总量的0.001-30%(重量)。
此外,制剂中优选包含可对UV-B和/或UV-A区域的紫外线辐射吸收的成分。适用的紫外线滤除剂例如有:2,4,6-三芳基-1,3,5-三嗪,其中芳基可根据不同情况带有至少一个取代基,该取代基优选选自羟基、烷氧基、具体为甲氧基、乙氧羰基,以及它们的混合物。适用的还有4-氨基苯甲酸酯,其中氨基可任选地经烷基化或烷氧基化。其中例如包括N,N-二甲基-4-氨基苯甲酸异辛基酯。适用的还有2-羟基苯甲酸酯,例如异辛基酯。适用的紫外线滤除剂还有2,4,6-三苯氨基-(邻-羰基-2′-乙基己基-1′-氧)-1,3,5-三嗪,3-咪唑-4-基丙烯酸及其乙酯,邻氨基苯甲酸薄荷醇酯,对氨基苯甲酸甘油酯,2,2′-二羟基-4-甲氧基二苯酮(二羟苯腙),2-羟基-4-甲氧基-4-甲基二苯酮(Mexenon),水杨酸三乙醇胺,二甲氧基苯基乙醛酸,3-(4′-硫代)亚苄基硼烷-2-酮及其盐,2,2′,4,4′-四羟基二苯酮,2,2′-亚甲基双-[6(2H-苯并三唑-2-基-4-(1,1,3,3,-四甲基丁基)苯酚],2,2′-(1,4-亚苯基)-双-1H-苯并咪唑-4,6-二磺酸及其钠盐,2,4-双[4-(2-乙基己氧基)-2-羟基]苯基-6-(4-甲氧基苯基)-(1,3,5)-三嗪,3-(4-甲基亚苄基)-樟脑,聚乙氧基乙基4-双(聚乙氧基)对氨基苯甲酸酯,2,4-二羟基二苯酮和/或2,2′-二羟基-4,4′-二甲氧基二苯酮-5,5′-磺酸二钠。
所列举的紫外线滤除剂可与新的活性成分共用,其显然不构成任何限定。
滤光剂的总量一般占制剂总量的0.1%(重量)-30%(重量),优选0.5-15%(重量),特别是1-10%(重量),以制成能使皮肤免受整个紫外线区域辐射损伤的美容制剂。
如果采用油相,优选其选自矿物油,矿物蜡,支链和/或非支链烃和烃蜡,饱和和/或不饱和三甘酯,支链和/或非支链C18-C24链烷烃脂肪酸;合成、半合成或天然油类,如橄榄油,棕榈油,杏仁油或它们的混合物;油,脂肪或蜡;饱和和/或不饱和、支链和/或非支链C3-C30链烷烃羧酸与饱和和/或不饱和、支链和/或非支链C3-C30链烷醇形成的酯,芳族羧酸与饱和和/或不饱和、支链和/或非支链C3-C30链烷醇形成的酯,例如肉豆蔻酸异丙酯,硬脂酸异丙酯,硬脂酸十六烷醇酯,油酸油醇酯;上述酯的合成、半合成和天然混合物,如西蒙得木油,苯甲酸烷基酯或硅油,例如环甲基聚硅氧烷,聚二甲基硅氧烷,聚二乙基硅氧烷,八甲基环四聚硅氧烷和它们的混合物,或二烷基醚。
如果采用水相,则其中还可任选地含有可与水混溶的溶剂,如C1-C10、优选C1-C5醇、二醇或多元醇,及其醚,优选乙醇,异丙醇,丙二醇,甘油,乙二醇,单乙基醚等。
适用的乳化剂优选是油包水型或水包油型乳化剂,如聚甘油酯,脱水山梨醇酯或部分酯化的甘油酯。
适用的增溶剂具体是乙氧基化脱水山梨醇酯,乙氧基化羊毛醇和乙氧基化蓖麻油。
制剂中常用的天然和合成增稠剂或胶凝剂是交联的聚丙烯酸及其衍生物,多糖,如黄原胶或藻酸盐,羧甲基纤维素或羟基羧甲基纤维素,水胶体,如阿拉伯树胶或蒙脱土矿物,如膨润土或脂肪醇,聚乙烯醇,以及聚乙烯吡咯烷酮。
适用的气溶胶抛射剂是常规的抛射剂,例如丙烷,丁烷,戊烷,二甲基醚和其他成分。
本发明还提供了一种助晒黑和防晒组合物以外的皮肤用美容组合物,其中含有:
(I)5′-脱氧-5′-甲硫腺苷和/或其美容适用的盐,
(II)任选地至少一种其他美容活性成分
(III)美容适用的载体。
本发明所排除的防晒组合物是指在与日光接触前在皮肤和/或头发上直接涂敷的组合物,用以防止日光特别是其中的UV-B部分对皮肤和/或头发造成的直接损伤。
本发明组合物中优选含有用量占组合物总量0.001-30%(重量)、特别是0.01-25%(重量)的组分I。
对于适用的组分(II)和(III),参见上文。
本发明还提供了具有商用包装形式的组合物,其中包括至少一种基于5′-脱氧-5′-甲硫腺苷的组合物,任选地还包括美容应用说明书。
本发明的商用包装产品还可包含一种制剂,特别是含有活性成分的配制品,以及附在上述配制品上的综合说明书。
本发明还提供了一种皮肤用美容护理方法,其中是在皮肤上施用有效量的美容制剂用于改善皮肤外观,该制剂中含有5′-脱氧-5′-甲硫腺苷和/或其美容适用的盐。
采用以下非限定性实例更详细地说明本发明。美容制剂实施例制剂类型 所用部位 实施例O/W乳化体 柔肤乳液 1W/O乳化体 护手霜 2
日晒护理霜 3复合乳化体 W/O/W乳化体 4微乳化体 微乳化体 5亲水凝胶 脂质体凝胶 6亲脂凝胶 亚光油性凝胶 7
油性凝胶 8棒剂 日光防护唇膏 9含水化妆品 体用凉爽喷雾剂 10修饰化妆品 彩妆品 11
液体彩妆品 12油 日光护理油 13体用清洁剂 深层洁面剂 14护理后洗除式产品 调理剂 15护理后免洗式产品 发蜡 16
去头屑生发水 17气溶胶 足部去臭喷雾剂 18
喷发胶 19化妆品制剂的实施例
实施例1:柔肤液
%(重量)鲸蜡-硬脂基醚-6(脂肪醇与氧化乙烯的反应产物)和 2.50硬脂醇鲸蜡-硬脂基醚-25(脂肪醇与氧化乙烯的反应产物) 2.50氢化椰油脂肪酸甘油酯 1.50聚乙二醇(40个EO单元)-十二烷基二醇共聚物 3.00聚二甲基硅氧烷 3.00苯乙基聚二甲基硅氧烷 2.00环甲基聚硅氧烷 1.00辛酸鲸蜡-硬脂醇酯 5.00鳄梨油 1.00甜杏仁油 2.00麦胚油 0.80泛醇USP 1.00植烷三醇 0.20乙酸生育酚 0.30丙二醇 5.00香精 适量防腐剂 适量5′-脱氧-5′-甲硫腺苷 适量水 69.20
实施例2:护手霜
%(重量)鲸蜡醇 1.00硬脂酸甘油酯 1.50硬脂醇 1.50棕榈酸鲸蜡醇酯 2.00乙酸生育酚 0.50聚二甲基硅氧烷 8.00鲸蜡-硬脂基醚-6(脂肪醇与氧化乙烯的反应产物)和 3.00硬脂醇甲氧基肉桂酸辛酯 5.00丙二醇 8.00泛醇 1.00月见草油 3.00乙氧基化氢化蓖麻油(7EO) 6.00油酸甘油酯 1.00苯乙基聚二甲基硅氧烷 3.00蜂蜡 1.50角豆树胶 0.80蚕丝粉 0.80防腐剂 适量香精 适量硼砂 0.105′-脱氧-5′-甲硫腺苷 适量水 52.30
实施例3:复合乳化体
%(重量)矿物油 7.50辛酸鲸蜡-硬脂醇 2.50硬脂酸铝 0.25硬脂酸镁 0.25微晶蜡H 0.50鲸蜡-硬脂醇 1.00羊毛脂醇 1.50矿物醇和羊毛脂醇 1.50乙氧基化氢化蓖麻油(7EO) 0.75聚乙二醇(40EO)-十二烷基二醇共聚物 2.00鲸蜡-硬脂基醚-6(脂肪醇与氧化乙烯的反应产物)和 2.00硬脂醇鲸蜡-硬脂基醚-25(脂肪醇与氧化乙烯的反应产物) 2.00三月桂基醚-4磷酸盐 1.00羟乙基纤维素 0.20丙二醇 7.50硫酸镁 0.255′-脱氧-5′-甲硫腺苷 适量水 69.30
实施例4:微乳化体
%(重量)鲸蜡-硬脂基醚-25(脂肪醇与氧化乙烯的反应产物) 13.00椰油酸甘油酯(7EO) 20.00辛基十二烷醇 5.00防腐剂 适量5′-脱氧-5′-甲硫腺苷 适量水 62.00
实施例5:脂质体凝胶
%(重量)乙氧基化氢化蓖麻油(40EO) 1.00红没药醇外消旋混合物 0.10丙二醇 8.00泛醇 0.50水和乙酸生育酚和聚山梨醇酯80和辛/癸酸三甘酯和 3.00卵磷脂防腐剂 适量香精 适量Carbomer 0.505′-脱氧-5′-甲硫腺苷 适量三乙醇胺 0.70水 86.30实施例6:亚光油性凝胶
%(重量)二氧化硅 5.00聚二甲基硅氧烷 10.00辛酸鲸蜡-硬脂醇酯 40.00辛/癸酸三甘酯 8.00苯乙基聚二甲基硅氧烷 2.00矿物油 28.50甜杏仁油 5.00植烷三醇 0.305′-脱氧-5′-甲硫腺苷 适量生育酚 0.50香精 1.00实施例7:油性凝胶
%(重量)二氧化硅 5.00聚二甲基硅氧烷 10.00辛酸鲸蜡-硬脂醇酯 30.00辛/癸酸三甘酯 10.00肉豆蔻酸异丙酯 5.00苯乙基聚二甲基硅氧烷 5.00矿物油 28.20西蒙得木油 5.00植烷三醇 0.305′-脱氧-5′-甲硫腺苷 适量生育酚 0.50香精 1.00实施例8:体用凉爽喷雾剂
%(重量)乙氧基化氢化蓖麻油(40EO) 2.00乳酸薄荷醇酯 0.20醇 5.00椰油酸甘油酯(7EO) 2.00金缕梅 5.00尿囊素 0.10红没药醇外消旋混合物 0.20丙二醇 5.00泛醇USP 0.50乳酸(浓度80%) 0.205′-脱氧-5′-甲硫腺苷 适量香精 适量水 79.80
实施例9:彩妆品
%(重量)鲸蜡-硬脂基醚-6(脂肪醇与氧化乙烯的反应产物)和硬脂醇 9.00聚二甲基硅氧烷 5.00辛酸鲸蜡-硬脂醇酯 8.00澳洲坚果油 5.00丙二醇 5.00水 53.00Sicovit白色E171 8.00Sicomet褐色7013E 3717 2.005′-脱氧-5′-甲硫腺苷 适量香精 适量3-二苯酮 5.00
实施例10:液体彩妆品
%(重量)鲸蜡-硬脂基醚-6(脂肪醇与氧化乙烯的反应产物)和 7.00硬脂醇鲸蜡-硬脂基醚-25 5.00聚二甲基硅氧烷 5.00辛酸鲸蜡-硬脂醇酯 8.00澳洲坚果油 5.00丙二醇 5.00水 53.00Sicovit白色E171 8.00Sicomet褐色7013E 3717 1.005′-脱氧-5′-甲硫腺苷 适量香精 适量3-二苯酮 5.00
实施例11:深层洁面剂
%(重量)水 65.60椰油酰氨丙基甜菜碱 5.00椰油酸钠,水解动物蛋白 8.00乙氧基化氢化蓖麻油(40EO) 2.00聚季铵盐-44 7.70红没药醇外消旋混合物 0.20泛醇 1.00香精 0.50羟乙基纤维素 2.005′-脱氧-5′-甲硫腺苷 适量丙二醇 5.00西蒙得木蜡 3.00
实施例12:调理剂
%(重量)鲸蜡-硬脂基醚-6和硬脂醇 2.00鲸蜡-硬脂基醚-25(脂肪醇与氧化乙烯的反应产物) 1.00辛酸鲸蜡-硬脂醇酯 6.00鲸蜡-硬脂基醚-3 2.00鲸蜡-硬脂醇 6.00植烷三醇 1.00丙二醇 5.00季铵盐-11 5.00泛醇 1.00乙酸视黄醇酯 0.50香精 适量5′-脱氧-5′-甲硫腺苷 适量防腐剂 适量水 70.50实施例13:发蜡
%(重量)聚乙二醇-6 30.00聚乙二醇-75 45.00液体石蜡油 0.50乙氧基化氢化蓖麻油(40EO) 1.00甘油 15.003-二苯酮 2.00植烷三醇 0.105′-脱氧-5′-甲硫腺苷 适量香精 适量水 6.40实施例14:去头屑生发水
%(重量)醇 45.00库拉索芦荟(10倍浓度) 1.00泛醇 1.00乙酸生育酚 0.50乙氧基化氢化蓖麻油(40EO) 0.50尿囊素 0.10水解动物蛋白 1.501-(4-氯苯氧基)-1-(1H-咪唑基)-3,3-二甲基-2-丁酮 0.30香精 0.105′-脱氧-5′-甲硫腺苷 适量水 50.00实施例15:足部去臭喷雾剂
%(重量)乙氧基化氢化蓖麻油(40EO) 0.80醇 20.00金合欢醇 0.12乳酸薄荷醇酯 0.081,2-丙二醇 3.204-二苯酮 1.20椰油酸甘油酯(7EO) 0.80香精 适量5′-脱氧-5′-甲硫腺苷 适量水 13.80丁烷 60.00
实施例16:喷发胶
%(重量)氨基甲基丙醇 0.40聚二甲基硅氧烷共聚多元醇 0.030醇 43.67戊烷 14.20丙烯酸酯/丙烯酰胺共聚物 3.40香精 适量5′-脱氧-5′-甲硫腺苷 适量丁烷 2.40异丁烷 35.90
Claims (8)
1.5′-脱氧-5′-甲硫腺苷在皮肤美容组合物中用于改善皮肤外观的用途。
2.权利要求1的用途,其中皮肤外观的改变是因老化造成的。
3.上述权利要求中任一权利要求的用途,其中所述组合物中含有至少一种美容适用的载体。
4.上述权利要求中任一权利要求的用途,其中所述组合物中含有占组合物总量0.001-30重量%的5′-脱氧-5′-甲硫腺苷。
5.一种皮肤用美容组合物,其中助晒黑组合物除外,该美容组合物中含有:
(I)5′-脱氧-5′-甲硫腺苷和/或其美容适用的盐,
(II)任选地至少一种其他美容活性成分,和
(III)美容适用的载体。
6.权利要求5的组合物,其中含有占组合物总量0.001-30重量%的组分I。
7.权利要求5或6的组合物,其中该组合物为商用包装的形式,其中任选地附有美容应用说明书。
8.一种皮肤用美容护理方法,其中是在皮肤上施用有效量的美容制剂用于改善皮肤外观,该制剂中含有5′-脱氧-5′-甲硫腺苷和/或其美容适用的盐。
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---|---|---|---|---|
US4373097A (en) * | 1981-04-27 | 1983-02-08 | Bioresearch S.R.L. | Process for preparing adenosine derivatives of anti-inflammatory and analgesic activity |
US4454122A (en) * | 1981-04-27 | 1984-06-12 | Bioresearch S.R.L. | Adenosine derivatives of anti-inflammatory and analgesic activity, and therapeutic compositions which contain them as their active principle |
IT1229477B (it) * | 1989-03-13 | 1991-09-03 | Bioresearch Spa | Impiego di 5' deossi - 5' metiltioadenosina, s adenosilmetionina e dei loro sali per la preparazione di composizioni farmaceutiche atte a ridurre la seborrea e composizioni farmaceutiche relative |
US5411991A (en) * | 1992-12-22 | 1995-05-02 | Shander; Douglas | Method of reducing hair growth employing sulfhydryl active compounds |
US5998423A (en) * | 1996-10-08 | 1999-12-07 | Therasys, Inc. | Methods for modulating melanin production |
US6551581B1 (en) * | 2001-12-27 | 2003-04-22 | Avon Products, Inc. | Methods for improving the aesthetic appearance of skin and hair |
-
2001
- 2001-07-04 DE DE10132338A patent/DE10132338A1/de not_active Withdrawn
-
2002
- 2002-07-03 US US10/187,658 patent/US20030068349A1/en not_active Abandoned
- 2002-07-03 EP EP02014846A patent/EP1273285A3/de not_active Withdrawn
- 2002-07-04 CN CN02123809.XA patent/CN1395918A/zh active Pending
- 2002-07-04 JP JP2002196499A patent/JP2003040729A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
JP2003040729A (ja) | 2003-02-13 |
DE10132338A1 (de) | 2003-01-16 |
US20030068349A1 (en) | 2003-04-10 |
EP1273285A3 (de) | 2003-10-22 |
EP1273285A2 (de) | 2003-01-08 |
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