CN112891242A - 一种用于祛斑美白抗炎的组合物及其应用 - Google Patents
一种用于祛斑美白抗炎的组合物及其应用 Download PDFInfo
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- CN112891242A CN112891242A CN202110252449.7A CN202110252449A CN112891242A CN 112891242 A CN112891242 A CN 112891242A CN 202110252449 A CN202110252449 A CN 202110252449A CN 112891242 A CN112891242 A CN 112891242A
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- tranexamic acid
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
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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
- A61Q19/08—Anti-ageing preparations
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
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Abstract
本发明公开一种用于皮肤祛斑美白抗炎的组合物及其应用，所述组合物包括组分A和组分B，组分A为氨甲环酸或其化妆品、药学上可接受的盐，组分B为地奥司明和其代谢物中一种或/和多种；组合物中组分A与组分B的重量比为0.1:1~20:1。本发明提供的组合物以组分A为主要美白成分，减少黑色素生成；搭配组分B维持血管正常通透性，促进黑素小体的转移消失，两者起协同增效作用，且无红肿、过敏等不良反应，可以有效地用作功能性化妆品和/或药物的材料。
Description
技术领域
本发明涉及含有氨甲环酸和地奥司明作为有效成分的组合物，具体涉及一种用于抑制黑色素生成、增强皮肤弹性、祛斑美白抗炎的组合物及其应用。
背景技术
近年来，随着医疗技术的发展，人们的寿命得以延长，生活质量及对健康美丽的需求也随之增加，进而对皮肤美容和健康的兴趣越来越浓烈。因此，市面上开发了各种功能性化妆品、保健品、药品，用于预防、减轻和改善皮肤问题，比如皮肤祛斑、美白等。
黑色素是一种生物色素，是酪氨酸或3,4-二苯丙氨经过一连串化学反应所形成。黑色素其实是一种氨基酸衍生物，是存在于每个人皮肤基底层的一种蛋白质。黑色素的产生多与内分泌失调、日光照射有关，黑色素细胞的多少主要取决于遗传，另外，还与内分泌激素及营养状况有关，由黑色素导致的疾病如：雀斑、黄褐斑、黑变病等，成为美容界研究的课题。
氨甲环酸（Tranexamic acid），又名传明酸、凝血酸、止血环酸。氨甲环酸一方面作为合成的氨基酸类抗纤溶药，能竞争性抑制纤维蛋白的赖氨酸与纤溶酶结合，从而抑制纤维蛋白凝块的裂解，产生止血作用，目前已有的剂型为氨甲环酸片和氨甲环酸注射液，临床上主要用于纤维蛋白溶解亢进所致的各种出血。另一方面因为氨甲环酸与参加黑色素代谢物酪氨酸部分结构相似，都有一个羧基，可竞争性抑制酪氨酸酶，进而减少黑色素的形成，其退黑除斑的功效比维生素C高约50倍，是果酸的近10倍左右，因此又可作为一种化妆品添加剂使用。
地奥司明（Diosmin）是一种增强静脉张力性药物和血管保护剂。其作用主要体现在以下三个方面：一、地奥司明对于静脉有特异的亲和性，能增强静脉张力而不影响动脉***；二、地奥司明可明显降低白细胞与血管内皮细胞的黏附、移行、崩解释放炎性物质，如组胺、缓激肽、补体、白三烯、***素及过多的自由基等，从而降低毛细血管的通透性及增强其张力；三、地奥司明还具有降低血液黏稠度，增强红细胞流速的功能，从而减少微循环淤滞情况。
研究表明，氨甲环酸单独使用美白效果不够明显，可能与其仅能将斑点分解，而不能快速将其排出体外有关。本发明将氨甲环酸和地奥司明联用，惊奇的发现，由于地奥司明对微循环的作用使得被氨甲环酸分解的黑色素快速排出，从而达到快速祛斑美白的效果，二者具有协同增效作用。
发明内容
有鉴于此，本发明的目的在于提供一种具有抑制黑色素生成、增强皮肤弹性、祛斑美白抗炎作用的组合物，以解决现有技术中存在的问题。
为实现上述目的，本发明的技术方案如下：
一种具有抑制黑色素生成、增强皮肤弹性、祛斑美白抗炎作用的组合物，其由组分A和组分B组成，其中组分A为氨甲环酸或其化妆品、食品或药学上可接受的盐，所述组分B为地奥司明和其代谢物中一种或/和多种；该组合物可以是化妆品或/和药品。
本发明一方面提供了一种化妆品组合物，其具有抑制黑色素生成、增强皮肤弹性、祛斑美白抗炎的作用。
在上述化妆品组合物中，组分A和组分B的比例为0.1:1~20:1，优选为1:1~10:1，更优选为2:1~8:1。
本发明的化妆品组合物除组分A和组分B外，可包括辅料、载体等其他添加剂，并可根据需要应用和配制用于一般皮肤化妆品的常用成分。
具体来说，本发明的化妆品组合物可进一步包括透皮促进剂，使得所需成分以高吸收率渗透到皮肤的血管细胞中。所述透皮促进剂包括但不限于薄荷脑、龙脑、桉油、月桂氮酮、二甲基亚砜、丙二醇、异山梨醇酐二甲醚、N-正烷基苯并异噻酮唑酮。
本发明的化妆品组合物可进一步包括油相成分，所述油相成分选自但不限于植物油、矿物油、硅油和合成油等中的一种或多种。更具体地，可以使用矿物油、环甲硅油、角鲨烷、肉豆蔻酸辛基十二烷基酯、橄榄油、葡萄树籽油、澳洲坚果油、辛酸甘油酯、蓖麻油、异壬酸乙基己酯、环戊硅氧烷等。
本发明的化妆品组合物可添加0.1%~5%的表面活性剂，高级醇等以加强乳化能力。其中，表面活性剂选自但不限于脱水山梨糖醇倍他喹酸酯、聚山梨酸酯60、甘油硬脂酸酯、亲脂甘油硬脂酸酯、脱水山梨醇油酸酯、鲸蜡基磷酸酯、脱水山梨糖醇硬脂酸酯/蔗糖酸酯、甘油硬脂酸酯/聚乙二醇100硬脂酸酯中的一种或多种；醇类选自但不限于乙酰醇、石酸醇、八倍二醇中的一种或多种。
本发明的化妆品组合物可进步包含水相成分，其中可添加0.0001%~8%的一种或多种增稠剂，如黄原胶、镁铝硅酸盐、纤维素等，以调整水相的粘度或硬度。
此外，如有必要，本发明的化妆品成分还可添加其他功能性或非功能性成分，如防晒霜、维生素、螯合剂、抗氧化剂（如乙酸二苯甲酸、丁基羟基甲苯等），防腐剂（如羟苯乙酯、羟苯甲酯、苯甲酸及其盐、山梨酸及其盐、苯甲醇、苯扎溴铵、壳聚糖、***醇、氯苯胺），着色剂，pH调节剂（如三乙醇胺、柠檬酸、柠檬酸钠、苹果酸、马来酸钠、软酸、氢氧化钠、磷酸氢二钠等），保湿剂（甘油、山梨醇、丙二醇、丁二醇、甲基葡萄糖等），润滑剂，香料（天然香料、合成香料等）等，对其类别的选择没有特别的限制，可采用化妆品领域技术人员熟知的成分即可。
本发明所述化妆品组合物存在的形式包括但不限于皮肤乳液、皮肤柔软剂、皮肤调色剂、收敛剂、乳液、乳霜、保湿乳液、营养乳液、按摩霜、营养霜、保湿霜、护手霜、肥皂、洗发水、清洁泡沫、清洁乳液、清洁霜、润肤露、身体清洁剂、乳状乳液、压粉、散粉、眼影等。
本发明另一方面提供了具有抑制黑色素生成、增强皮肤弹性、祛斑美白抗炎作用的药品组合物。
在上述药品组合物中，组分A和组分B的比例为0.1:1~20:1，优选为1:1~10:1，更优选为2:1~8:1。
本发明的药品组合物可以以一般药物制剂的形式经口给药或者局部给药等。
口服给药的固体制剂包括但不限于片剂、药片、粉末、颗粒、胶囊等。口服给药的液体制剂包括但不限于悬浮液、溶剂、乳液和糖浆等。皮肤外用制剂包括但不限于乳液、混悬液、冻干制剂、软膏、凝胶或凝胶贴膏剂、贴剂或贴膏剂、喷雾剂等。优选为皮肤外用剂型。
本发明的药品组合物除组分A和组分B外，可包括其他药学上可接受的辅料、载体等添加剂，如经口服给药的制剂可添加填充剂、粘合剂、崩解剂、润滑剂、着色剂、香精等。
本发明所述药品组合物制备的皮肤外用制剂还可以添加其他功能性成分，如抗皱成分、美白成分、缩小毛孔等。
对于本发明药品组合物制备的皮肤外用制剂，可添加油相成分、乳化剂、水相成分、药用添加剂（增稠剂、渗透压调节剂、pH调节剂、抗氧剂、防腐剂等）中的一种或多种。
更具体地说，所述油相成分包括但不限于植物油（如大豆油、茶油、芝麻油、花生油、橄榄油、蓖麻油等）、中链甘油三酯、肉豆蔻酸异丙酯等中的一种或多种。
所述乳化剂包括但不限于吐温80、吐温60、麦泽52、硬脂酸甘油酯、聚氧乙烯蓖麻油、聚氧乙烯氢化蓖麻油、卵磷脂、聚乙二醇硬脂酸酯、双肉豆蔻磷脂酸胆碱中的一种或多种。
所述防腐剂包括但不限于尼泊金酯、羟苯乙酯、羟苯甲酯、苯甲酸及其盐、山梨酸及其盐、苯甲醇、苯扎溴铵、壳聚糖、***醇、氯苯胺、醋酸氯己定中的一种或多种。
所述增稠剂包括但不限于卡波姆、透明质酸、透明质酸钠、聚维酮、西黄蓍胶、纤维素类化合物中的一种或多种。
所述渗透压调节剂包括但不限于葡萄糖、氯化钠、氯化钾、甘露醇、蔗糖、丙二醇、丙三醇、山梨醇中的一种或多种。
所属抗氧剂包括但不限于丁基羟基茴香醚、二丁基羟基甲苯、D-抗坏血酸钠、L-抗坏血酸棕榈酸酯、没食子酸丙酯、亚硫酸盐中的一种或多种。
所述pH调节剂包括但不限于盐酸、氢氧化钠、氢氧化钾、氨丁三醇、醋酸-醋酸钠、柠檬酸-柠檬酸钠、枸橼酸-枸橼酸钠、磷酸盐中的一种或多种。
具体实施方式
在下面的描述中阐述了很多具体细节以便于充分理解本发明。但是本发明能够以很多不同于在此描述的其它方式来实施，本领域技术人员可以在不违背本发明内涵的情况下做类似改进，因此本发明不受下面公开的具体实施的限制。
除非另有定义，本文所使用的所有的技术和科学术语与属于本发明的技术领域的技术人员通常理解的含义相同。本文中在本发明的说明书中所使用的术语只是为了描述具体的实施例的目的，不是旨在于限制本发明。
实施例1 -化妆品制备
1-1 面霜制备
表1-1 面霜组成成分表
| 组成成分 | 重量份 |
| 氨甲环酸 | 1 |
| 地奥司明 | 0.2 |
| 硬脂酸 | 17 |
| 鲸蜡醇 | 1 |
| 氢氧化钾 | 1 |
| 甘油 | 5 |
| EDTA-2Na | 0.02 |
| 丙二醇 | 3 |
| 羟苯乙酯 | 0.1 |
| 纯化水 | 补充至100 |
制备方法：
将丙二醇、硬脂酸、鲸蜡醇加热至80~90℃，搅拌溶解，得到混合物A；将纯化水、甘油、EDTA-2Na加热至80~90℃，搅拌溶解，将混合物A加入后，均质5分钟；降温至30~35℃，加入羟苯乙酯，搅拌均匀，即得面霜。
精华液制备
表1-2 精华液组成成分
| 组成成分 | 重量份 |
| 氨甲环酸 | 3 |
| 地奥司明 | 1 |
| EDTA-2Na | 0.02 |
| 透明质酸钠 | 1.5 |
| 卡波姆 | 0.2 |
| 柠檬酸钠 | 0.15 |
| 异山梨醇酐二甲醚 | 1.8 |
| 甲基丙二醇 | 8 |
| 1，3-丙二醇 | 15 |
| 纯化水 | 补充至100 |
制备方法：
将EDTA-2Na、卡波姆、加入水中，搅拌均匀后，加入透明质酸钠搅拌均匀后，加入柠檬酸钠、氨甲环酸搅拌均匀，继续加入甲基丙二醇、1，3-丙二醇、异山梨醇酐二甲醚搅拌均匀即得精华液。
实施例2 -药品制备
2-1颗粒制备
表2-1 颗粒组成成分
| 组成成分 | 重量份 |
| 氨甲环酸 | 70 |
| 地奥司明 | 10 |
| 玉米淀粉 | 10 |
| 乳糖 | 10 |
制备方法：
取氨甲环酸、地奥司明、玉米淀粉、乳糖混合据黁，加入适量纯化水，制成颗粒，在60℃下干燥，整粒即得颗粒。
将上述制得的颗粒制剂填充进一步压片可得片剂。
凝胶制备
表2-2 凝胶组成成分
| 组成成分 | 重量份 |
| 氨甲环酸 | 10 |
| 地奥司明 | 2 |
| 卡波姆940 | 10 |
| 三乙醇 | 4 |
| 甘油 | 40 |
| 羟苯乙酯 | 0.5 |
| 聚山梨酯80 | 2 |
| 氢氧化钾 | 4 |
| 纯化水 | 补充至100 |
制备方法：
取卡波姆、甘油、聚山梨酯80和适量纯化水，放置4.0~4.5小时充分搅拌至溶胀，加入三乙醇搅拌均匀，用氢氧化钾调节pH5~6，即得基质；取氨甲环酸、地奥司明、甘油、羟苯乙酯混合均匀，边搅拌边加入上述基质中，最后加纯化水补充至足量即得凝胶。
凝胶贴膏制备
表2-3 凝胶贴膏组成成分
| 组成成分 | 重量份 |
| 氨甲环酸 | 10 |
| 地奥司明 | 2 |
| 聚丙烯酸钠 | 4.8 |
| 明胶 | 4.8 |
| 高岭土 | 3.2 |
| 甘羟铝 | 0.04 |
| 蓖麻油 | 0.08 |
| 甘油 | 44.8 |
| 聚乙烯醇 | 0.8 |
| EDTA-2Na | 0.12 |
| 月桂氮酮 | 2.4 |
| 丙二醇 | 4 |
| 纯化水 | 补充至100 |
制备方法：
将聚丙烯酸钠、明胶、甘羟铝、高岭土、EDTA-2Na、蓖麻油、甘油，混合均匀得A相；另取聚乙烯醇月桂氮酮、丙二醇、氨甲环酸、地奥司明，用适量纯化水溶解，即得到B相。将B相迅速倒入A相中，充分搅拌交联成膏，迅速涂布于背衬材料无纺布上，覆盖防粘膜，即制成凝胶贴膏。
凝胶贴膏制备
与实施例2-3相比，本实施例仅地奥司明与补充的纯化水重量份不同，本实施例地奥司明重量份为10，纯化水补充至100即可。
乳膏制备
表2-5 乳膏组成成分
| 组成成分 | 重量份 |
| 氨甲环酸 | 10 |
| 地奥司明 | 2 |
| 甘油 | 3 |
| 十二烷基硫酸钠 | 1 |
| 羟苯乙酯 | 0.2 |
| 二甲基亚砜 | 7 |
| 苯扎溴铵溶液 | 3 |
| 单硬脂酸甘油酯 | 30 |
| 白凡士林 | 30 |
| 纯化水 | 补充余量 |
制备方法：
将甘油、十二烷基硫酸钠、羟苯乙酯、二甲基亚砜、苯扎溴铵溶液、氨甲环酸、地奥司明和纯化水于100℃下混匀得水相；将单硬脂酸甘油酯和白凡士林于95℃下混匀30分钟得油相；将水相与油相在乳化罐内真空度为0.05MPa下搅拌30分钟，然后以3000r/min转速均质30分钟，降温至50℃，灌封即得软膏剂。
实施例3 皮肤刺激性试验
根据化学药物刺激性、过敏性和溶血性研究技术指导原则，采用如下方法对氨甲环酸-地奥司明皮肤外用制剂进行皮肤刺激性考察。
实验方法：取6只家兔，雌雄不限，体重2.5±0.5kg，实验前将家兔背部脊柱两侧毛剪掉，范围约3cm。取实施例1-1、1-2、2-2、2-4直接涂布于一侧已去毛的家兔皮肤上，然后用两层纱布和一层玻璃纸或类似物覆盖，再用无刺激性胶布和绷带加以固定；另一侧涂布空白制剂作为对照。取实施例2-3直接贴敷于一侧已去毛的家兔皮肤上；另一侧贴敷空白基质作为对照。贴敷4小时。贴敷结束后，除去受试物并用温水清洁给药部位。多次给药皮肤刺激性实验应连续在同一部位给药，每次给药时间相同，贴敷期限为4天，分别在贴敷1天、2天、3天、4天及停药后24小时、48小时、72小时观察刺激性现象。
结果观察：在自然光线下观察皮肤反应。根据表3-1给出的评分标准对皮肤红斑和水肿进行评分。
表3-1 皮肤刺激反应评分标准
表3-2 皮肤刺激强度评价标准
| 分值 | 评价 |
| 0-0.49 | 无刺激性 |
| 0.5-2.99 | 轻度刺激性 |
| 3.0-5.99 | 中度刺激性 |
| 6.0-8.0 | 强刺激性 |
家兔刺激性考察结果：采用空白制剂和实施例涂布家兔皮肤1天、2天、3天、4天，及停药后24小时、48小时、72小时均未出现红斑和水肿，评分为0，且说明本发明提供的皮肤外用制剂无皮肤刺激性，安全性良好。
实施例4 功效测试
功效测试一：黑色素含量测试
选取脸部有色素沉着、有黑斑和黄褐斑的女性，共32人，年龄20~50岁，分成4组，每组8人。其中两组分别使用实施例1-2和2-3中的精华液和凝胶贴膏，一组使用市售仅含氨甲环酸的精华液，一组使用不含活性成分的基质贴膏。受试者每天早晚各使用一次，持续使用28天，且在测试同期不适用其他美白护肤品。在第0、14、28天后，用MEXAMETER MX18皮肤色素分析仪测试脸部黑色素含量（平均值）变化，数值越小，表示皮肤越白。测试结果如下表所示：
表4-1 黑色素含量及变化率测定结果
通过上述结果可以看出，实施例组在第28天时受试者的皮肤黑色素值明显减小，而空白组几乎无变化，说明本发明的复合制剂美白效果明显；同时在同等测试条件下与市售精华液相比，其美白下过明显优于市售精华液，说明本发明添加了地奥司明后能与氨甲环酸共同起协同增效作用，增强美白效果。
功效测试二：皮肤ITA值测定
对功效测试一中的受试者，用VISIA-CR面部成像仪测试受试者脸部皮肤，用Image-Pro Pus图像分析软件分析脸部皮肤的ITA值，ITA值越大，表示皮肤越亮白。结果如下表所示。
表4-2 皮肤ITA值测定结果
通过上表结果可以看出，实施例组在第28天时受试者的脸部皮肤ITA值变化率较大，而空白组几乎无变化，说明本发明的复合制剂美白效果明显；同时在同等测试条件下与市售精华液相比，其美白下过明显优于市售精华液，说明本发明添加了地奥司明后能进一步增强亮白度，美白效果明显。
功效测试三：祛斑及抗炎舒缓效果测试
对功效测试一中的受试者，通过一定的评价标准，自行评价其祛斑及抗炎舒缓效果，评价标准：
表4-3 祛斑及抗炎舒缓效果评价标准
| 祛斑效果 | 评分 |
| 效果显著 | 4 |
| 效果良好 | 3 |
| 效果一般 | 2 |
| 无明显效果 | 1 |
| 出现红斑、过敏等不良反应 | 0 |
表4-4 祛斑及舒缓效果测试结果
从上表结果可以看出，本发明的复合制剂具有优异的祛斑及抗炎舒缓修复效果，且无红肿、过敏等不良反应。
综上所述，本发明提供的复合物具有优异的祛斑、美白、提亮及抗炎舒缓修复功能，且对皮肤无刺激性，可用于功能性化妆品和/或药品中，发挥祛斑美白提亮作用。
以上所述实施例的各技术特征可以进行任意的组合，为使描述简洁，未对上述实施例中的各个技术特征所有可能的组合都进行描述，然而，只要这些技术特征的组合不存在矛盾，都应当认为是本说明书记载的范围。
以上所述实施例仅表达了本发明的几种实施方式，其描述较为具体和详细，但并不能因此而理解为对发明专利范围的限制。应当指出的是，对于本领域的普通技术人员来说，在不脱离本发明构思的前提下，还可以做出若干变形和改进，这些都属于本发明的保护范围。因此，本发明专利的保护范围应以所附权利要求为准。
Claims (12)
1.一种用于祛斑美白抗炎的组合物，所述组合物包括组分A和组分B，其特征在于，所述组分A为氨甲环酸或其化妆品、药学上可接受的盐，所述组分B为地奥司明和/或其代谢物或其化妆品、药学上可接受的盐中一种或/和多种。
2.根据权利要求1所述的组合物，其特征在于，所述组分A（以氨甲环酸计）与所述组分B的重量比为0.1:1~20:1。
3.根据权利要求1所述的组合物，其特征在于，所述组分A（以氨甲环酸计）与所述组分B的重量比为1:1~10:1。
4.根据权利要求1所述的组合物，其特征在于，所述组分A（以氨甲环酸计）与所述组分B的重量比为2:1~8:1。
5.根据权利要求1所述的组合物，其特征在于，所述组分B为地奥司明和其代谢物中一种或/和多种。
6.根据权利要求1~5所述的组合物，其特征在于，所述组合物可用作化妆品、药品等的材料。
7.根据权利要求1~6所述的组合物，其特征在于，所述组合物可作为化妆品的成分，用于抑制黑色素生成、增强皮肤弹性、祛斑美白抗炎。
8.根据权利要求7所述的组合物，其特征在于，所述组合物存在的形式包括但不限于皮肤乳液、皮肤柔软剂、皮肤调色剂、收敛剂、乳液、精华液、乳霜、保湿乳液、营养乳液、按摩霜、营养霜、保湿霜、护手霜、肥皂、洗发水、清洁泡沫、清洁乳液、清洁霜、润肤露、身体清洁剂、压粉、散粉、眼影等。
9.根据权利要求1~6所述的组合物，其特征在于，所述组合物作为药品的成分，用于抑制黑色素生成、增强皮肤弹性、祛斑美白抗炎。
10.根据权利要求9所述的组合物，其特征在于，所述药品组合物可经口给药，也可经皮肤局部给药，可以以片剂、颗粒剂、散剂、胶囊剂、液体剂、丸剂、乳膏、凝胶、贴剂、贴膏、凝胶贴膏等形式存在。
11.根据权利要求9~10所述的组合物，其特征在于，所述组合物给药途径优选为皮肤局部给药，剂型优选为凝胶贴膏。
12.根据权利要求9~11所述的组合物，其特征在于，所述组合物包含以下成分：
。
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