CN108478479A - 含有能自行提供弱酸性环境的紫檀芪复合物的眼部抗皱啫喱及其制备方法 - Google Patents
含有能自行提供弱酸性环境的紫檀芪复合物的眼部抗皱啫喱及其制备方法 Download PDFInfo
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Classifications
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- A—HUMAN NECESSITIES
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/005—Preparations for sensitive skin
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- A—HUMAN NECESSITIES
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- Biotechnology (AREA)
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- Mycology (AREA)
- Cosmetics (AREA)
Abstract
本发明公开了一种含有能自行提供弱酸性环境的紫檀芪复合物的眼部抗皱啫喱,特征是含如下主要成分:紫檀芪:2mg/ml~10mg/ml;瑞鲍迪苷A:30mg/ml~60mg/ml;甘草酸:5mg/ml~12mg/ml;透明质酸钠:1mg/ml~5mg/ml。本发明的制备包括如下步骤:(1)先将紫檀芪充分溶解于乙醇中,再将瑞鲍迪苷A与甘草酸按比例混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末;(2)取透明质酸钠用水浸泡过夜完全溶解,待用;(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。通过此法制备得到的啫喱中紫檀芪的溶解度明显增高,更加容易被眼部皮肤吸收,发挥眼部护肤作用。本发明制备简单,制备的紫檀芪复合物眼部啫喱具有很强的抗氧化能力且能自行提供弱酸性环境,能明显改善眼部皮肤状态,且无刺激性。
Description
技术领域
本发明涉及日常生活中经常使用的美容品,尤其是一种含有能自行提供弱酸性环境的紫檀芪复合物的眼部抗皱啫喱及其制备方法。
背景技术
随着年龄的增长,皮肤老化,表皮组织干燥变薄,及真皮层的胶原蛋白和弹力纤维补充不足变细,失去网状支撑力而形成的皱纹。同时眼部皮肤受到外界环境影响(如紫外线等),形成游离自由基,自由基破坏正常细胞膜组织内的胶原蛋白、活性物质,氧化细胞而形成的小细纹、皱纹。眼部皱纹的形成是皮肤衰老最重要的体表特征。同时皮肤的表面显弱酸性,皮肤只有在正常的pH值范围内,也就是处于弱酸性时,才能使皮肤处于吸收营养的最佳状态,此时皮肤抵御外界侵蚀的能力以及弹性、光泽、水分等,都为最佳状态。
紫檀芪(Pterostilbene,CAS号537-42-8),是一种来源于紫檀、蓝莓、葡萄和花榈木等植物的有效成分,具有抗癌、抗炎、抗氧化和镇痛剂的作用。目前大量研究表明紫檀芪在皮肤疾病的治疗和防护中有较好的作用,特别是在抗氧化等领域。紫檀芪可通过多个相关联的机制发挥抗氧化作用,被认为是天然抗氧化剂之一.紫檀芪直接或间接激活Nrf2/Keap1系统, 提高细胞抗氧化能力,在细胞的防御中发挥重要作用。紫檀芪作为绿色水果蓝莓的天然提取物,在抗衰老方面也有很大的作用。但是紫檀芪存在如下不足,严重影响其开发和利用:(1) 水溶解性差,紫檀芪在水相中20℃时,在水中溶解度约为0.03mg/ml;(2)分子结构不稳定,紫檀芪分子结构中含有酚羟基,而酚羟基极其不稳定,这就决定了紫檀芪的稳定性极差,尤其是在水溶液中极其不稳定,容易氧化;(3)半衰期短、透生物膜性能差,包括透皮、眼部等在内的粘膜生物利用度极低。上述这些不足,严重限制了紫檀芪在化妆品等域的应用。因此,很有必要进一步探索一种经济又有效的新型紫檀芪产品。纳米系统如胶束可以提高药物的溶解度,提高生物利用度。由于一些合成的胶束载体材料存在一定的安全隐患,天然材料的使用成为近年的研发热点,尤其是小分子材料。这种载体可起到构建纳米药物递送系统的作用,提高药物稳定性,提高吸收。
瑞鲍迪苷A(Rebaudioside A,CAS登记号58543-16-1,分子式C44H70O23,分子量967.03) 是从菊科植物Stevia Rebaudia(该植物在我国称作甜叶菊)的叶子中提取出来的一种糖苷,作为一种新型天然甜味剂而广泛应用于食品、饮料、调味料的生产中。在南美洲使用甜叶菊作为药草和代糖已经有几百年历史。究表明,瑞鲍迪苷A具有强抗氧化活性(Saravanan R, Ramachandran V.Modulating efficacy of Rebaudioside A,aditerpenoid on antioxidant and circulatory lipids in experimental diabeticrats.Environ Toxicol Pharmacol.2013,36(2):472-83),瑞鲍迪苷A可显著增溶紫檀芪,提高紫檀芪稳定性。
甘草酸(Glycyrrhizic Acid,CAS号1405-86-3,分子式C42H62O16,分子量822.92)是甘草中最主要的活性成分,甘草酸及其系列产品,对肉瘤、癌细胞生长有抑制作用,对艾滋病的抑制率更高达90%,有较强的增加人体免疫功能作用,而且也是很好的食品添加剂和香料基料。近年来,在医药、化工、食品、日用化工等行业也得到了广泛的应用。甘草提取物可活化皮质甾类化合物(抑制代谢酶),间接的增强皮质甾类化合物的作用,可以使用于膏、霜、水、露、乳液、奶类和蜜类等所有化妆品,它可以中和或解除或减低化妆品的有毒物质,也可以防止有的化妆品的过敏反应,更适用于高级肤用或眼部用化妆品中。
发明内容
为解决以上本发明提出一种含有能自行提供弱酸性环境的紫檀芪复合物的眼部抗皱啫喱,其主要构成为水凝胶基质,含有如下浓度的主要成分:紫檀芪:2mg/ml~10mg/ml;瑞鲍迪苷A:30mg/ml~60mg/ml;甘草酸:5mg/ml~12mg/ml;透明质酸钠:1mg/ml~5mg/ml。
本发明所述的紫檀芪复合物的眼部抗皱啫喱,其特征在于所述瑞鲍迪苷A(CAS登记号 58543-16-1,分子式C44H70O23,分子量967.03)纯度≥98%,所述甘草酸(CAS登记号:1405-86-3,分子式:C42H62O16,分子量:822.93)纯度≥97%。
本发明还提供上述含有能自行提供弱酸性环境的紫檀芪复合物的眼部抗皱啫喱的制备方法,包括如下步骤:
(1)先将紫檀芪充分溶解于乙醇中,再将瑞鲍迪苷A与甘草酸按比例混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠用水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
本发明的紫檀芪复合物的眼部抗皱啫喱,所用的透明质酸钠为常规护肤品级即可满足要求。
本发明的紫檀芪复合物的眼部抗皱啫喱,还可依据需要,加入适量的海藻糖、甘油、尿囊素等一些常用的添加剂。
本发明提供的技术方案的有益效果:紫檀芪、瑞鲍迪苷A、甘草酸均具有抗氧化作用,能够减少或抑制细胞氧化而形成的小细纹,皱纹,具有较好的改善眼周皮肤纹理的作用,且无眼部及眼部皮肤刺激性。同时,瑞鲍迪苷A与甘草酸自组装形成混合胶束,包封溶解紫檀芪,提高紫檀芪溶解度和稳定性,改善紫檀芪皮肤吸收效率,甘草酸赋予混合胶束具有弱酸性微环境环境,进一步提高紫檀芪分子稳定性,且符合皮肤生理pH值要求。综上技术方案,使有利于有效成分紫檀芪的眼部皮肤吸收与利用,起到很好的眼部护理美容作用。
具体实施方式
下面通过具体实例对本发明作进一步说明本发明的。
实施例1
(1)先将40mg紫檀芪充分溶解于乙醇中,再将600mg瑞鲍迪苷A与100mg甘草酸混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠20mg用20ml水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
实施例2
(1)先将200mg紫檀芪充分溶解于乙醇中,再将1200mg瑞鲍迪苷A与240mg甘草酸混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠50mg用20ml水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
实施例3
(1)先将100mg紫檀芪充分溶解于乙醇中,再将1200mg瑞鲍迪苷A与240mg甘草酸混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠100mg用20ml水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
实施例4
(1)先将100mg紫檀芪充分溶解于乙醇中,再将800mg瑞鲍迪苷A与240mg甘草酸混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠50mg用20ml水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
实施例5
(1)先将100mg紫檀芪充分溶解于乙醇中,再将800mg瑞鲍迪苷A与100mg甘草酸混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠50mg用20ml水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
实施例6
(1)先将100mg紫檀芪充分溶解于乙醇中,再将1000mg瑞鲍迪苷A与100mg甘草酸混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠50mg用20ml水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
实验效果例1:DPPH自由基清除率
实验组:实施例1制备的紫檀芪啫喱,使用水稀释至实验需要的各浓度
对照组:先将40mg紫檀芪充分溶解于含20%乙醇的水溶液中;取透明质酸钠20mg用 10ml水浸泡过夜完全溶解得透明质酸钠溶液,然后将上述两种溶液混合均匀得对照实验用普通紫檀芪啫喱。
DPPH自由基是稳定的紫色自由基,在517nm处有最大吸收波长。当有自由基清除剂存在时,DPPH自由基的单电子由于被配对,DPPH自由基浓度减小而使其颜色变浅,在最大吸收波长处的吸光度值变小,且颜色变化与配对电子数成化学计量关系。由于这种方法简便、灵敏可靠,所以在国内外广泛用于清除自由基物质性质的研究与天然抗氧化剂的筛选。紫檀芪复合物的DPPH自由基清除率的实验结果如下:
表1 紫檀芪复合物DPPH自由基清除实验结果
实验效果例2:皮肤粗糙度变化
皮肤粗糙度是皮肤所有剖面中,以直线上最大灰度峰值和最小灰度峰值之间的差值,该差值是皮肤表面不平度的最大高度。
方法:选择志愿者40人,随机分为两组,每组20人,具体性别构成随机确定,第一组受试者涂抹本发明的实施例1制得的眼部抗皱啫喱,第二组受试者涂抹本发明的实施例1制得的眼部抗皱啫喱,第二组受试者涂抹实验效果例1中所用普通紫檀芪啫喱。
(1)选择受试者的左右眼部作为受试区域,每位受试者的左眼涂抹本发明的眼部抗皱啫喱作为实验组,右眼不涂抹任何样品作为对照组。
(2)由技术人员使用MicroSkinⅡ多功能皮肤镜图像分析系统测定实验部位涂抹化妆品前的皮肤纹理度。
(3)早晚用清水清洗受试部位(同一区域),涂抹受试产品,测试期间,受试部位不再涂抹除受试产品以外的任何护肤品。
(4)在受试者连续使用该测试品的第一周、第二周、第三周、第四周的同一时间将受试部位洗净,由技术人员使用MicroSkinⅡ多功能皮肤镜图像分析系统测定实验部位涂抹化妆品前的皮肤纹理度。
(5)统计受试者受试部位每次测得的数值,分析皮肤纹理变化。
结果:
变化率=(样品组数据Tn-起始值T0)/起始值T0×100%
T0是试验前受试者皮肤测定值,Tn是各受试者各时间点每次测试时皮肤测定值。
表2 第一组受试部位皮肤粗糙度与初始值的差值(n=20)
测试期间,受试部位使用该眼部抗皱啫喱后,其皮肤粗糙度一直呈降低趋势。期变化率低于空白组,该眼部抗皱啫喱使用4周后,皮肤变化率为-6.32%,相对起始值存在显著差异 (P<0.05),由此可见,使用本发明的紫檀芪眼部啫喱后,眼部皮肤的粗糙度均有明显改善。
表3 第二组受试部位皮肤粗糙度与初始值的差值(n=20)
测试期间,受试部位使用该眼部抗皱啫喱后,其皮肤粗糙度未见显著降低趋势。该眼部抗皱啫喱使用4周后,皮肤变化率为-1.08%,相对起始值无显著差异(P>0.05),由此可见,使用普通紫檀芪眼部啫喱后,眼部皮肤的粗糙度未见明显改善。
Claims (3)
1.含有能自行提供弱酸性环境的紫檀芪复合物的眼部抗皱啫喱,其特征在于含有如下浓度的主要成分:紫檀芪:2mg/ml~10mg/ml;瑞鲍迪苷A:30mg/ml~60mg/ml;甘草酸:5mg/ml~12mg/ml;透明质酸钠:1mg/ml~5mg/ml。
2.如权利要求1所述的紫檀芪复合物的眼部抗皱啫喱,其特征在于所述瑞鲍迪苷A(CAS登记号58543-16-1,分子式C44H70O23,分子量967.03)纯度≥98%,所述甘草酸(CAS登记号:1405-86-3,分子式:C42H62O16,分子量:822.93)纯度≥97%。
3.根据权利要求1所述的紫檀芪复合物的眼部抗皱啫喱的制备方法,其特征方法在于,包括以下步骤:
(1)先将紫檀芪充分溶解于乙醇中,再将瑞鲍迪苷A与甘草酸按比例混合溶解在上述溶解了紫檀芪的乙醇溶液中,旋干乙醇得固体粉末。
(2)取透明质酸钠用水浸泡过夜完全溶解,待用;
(3)将步骤(1)所得固体粉末加入至步骤(2)所得透明质酸溶液中,搅拌至固体粉末完全溶解。
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