CN116392405A - 一种美白组合物和外用皮肤制剂 - Google Patents
一种美白组合物和外用皮肤制剂 Download PDFInfo
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- CN116392405A CN116392405A CN202310368748.6A CN202310368748A CN116392405A CN 116392405 A CN116392405 A CN 116392405A CN 202310368748 A CN202310368748 A CN 202310368748A CN 116392405 A CN116392405 A CN 116392405A
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- ethyl ether
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- sulfonic acid
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Abstract
本申请提供了一种美白组合物和外用皮肤制剂，其包括：维生素C乙基醚，其含量为0.01～10％；4‑羟乙基哌嗪乙磺酸，其含量为0.01～10％；腺苷，其含量为0.01～1％。本申请的组合物以及外用皮肤制剂中还可以添加除维生素C乙基醚之外的其他活性成分，满足美白皮肤需求和解决皮肤衰老问题。
Description
技术领域
本申请涉及化妆料领域，具体而言，涉及一种美白组合物和外用皮肤制剂。
背景技术
维生素C是一种具有高效美白祛斑作用的活性物质，但是其本身极易被氧化变黄，不易被皮肤真正吸收。相对于维生素C，维生素C乙基醚(3-O-乙基抗坏血酸)是一种亲油亲水的两性维生素C衍生物，这不仅使其在配方中能够极为方便的使用，更加使其容易穿透角质层进入真皮层，进入真皮层后被生物酶分解发挥维生素C的作用，从而起到更好的美白祛斑的功效。而且，维生素C乙基醚在化妆品配方中的稳定性比维生素C好很多。
在实际配方中，我们发现维生素C乙基醚在配方中很容易导致体系的pH值降低，使得化妆品的稳定性下降，从而影响产品的使用。应对pH下降的问题，通常的办法是添加pH缓冲剂，常见的如柠檬酸-柠檬酸钠体系、磷酸氢二钠-磷酸二氢钠体系。然而，这类缓冲剂本身离子性非常强，对化妆品配方的配方粘度影响非常大，很容易影响肤感。
发明内容
本申请要解决的技术问题：
如何保持含维生素C乙基醚的配方体系pH值稳定，同时不影响配方的粘度。
解决技术问题所用的技术手段：
当维生素C乙基醚在加入含水的产品后，在常温储存状态下，醚键容易水解断裂，释放出抗坏血酸出来，导致体系的pH降低，同时使体系的离子性(电导率)升高，对一些粘度敏感型的高分子粘度下降，这种影响在高温(45℃与50℃)加速试验中尤其明显。
经过大量的研究，发明人(们)发现通过将4-羟乙基哌嗪乙磺酸(以下简称HEPES)和腺苷搭配可以有效缓冲含维生素C乙基醚的体系中，由于维生素C乙基醚水解带来的pH值下降，而且相比于其他pH缓冲体系，对含维生素C乙基醚体系粘度的影响非常小。
本申请的一个方面，提供了一种组合物，其包括：维生素C乙基醚，其含量为0.01～10％；4-羟乙基哌嗪乙磺酸，其含量为0.01～10％；腺苷，其含量为0.01～1％。
本申请的另一方面，提供了一种外用皮肤制剂，其至少包括前述的组合物。
有益效果：
本申请的组合物以及外用皮肤制剂能够在含有维生素C乙基醚的体系中，保持较好肤感的同时具有稳定的pH值。
本申请的组合物以及外用皮肤制剂中还可以添加除维生素C乙基醚之外的其他活性成分，满足美白皮肤需求和解决皮肤衰老问题。
具体实施方式
为使本申请实施例的目的、技术方案和优点更加清楚，下面将对本申请实施例中的技术方案进行清楚、完整地描述，显然，所描述的实施例不是全部的实施例。
本申请的一种实施方式中描述的元素和特征可以与一个或更多个其它实施方式中示出的元素和特征相结合。应当注意，为了清楚的目的，说明中省略了与本申请无关的、本领域普通技术人员已知的部件和处理的表示和描述。
定义
在本文中，除非另有说明，用语“％”是指“质量％”。例如，“麦角硫因的含量为XX％”是指“麦角硫因的质量百分比为XX％”
在本文中，除非另有说明，用语“％”均是指基于本申请组合物的总质量而言的。
在本文中，限定的所有范围是指：包括给定范围内的每个特定范围以及给定范围之间的子范围的组合。例如，1～5的范围具体包括1、2、3、4和5，也包括如2～5、3～5、2～3、2～4、1～4等子范围。
在本文中，比率的范围是指：包括给定范围内的每个特定比率以及给定范围之间的子范围的组合。
在本文中，“维生素C乙基醚”是指3-o-Ethyl Ascorbicacid，又称3-O-乙基抗坏血酸醚、VC乙基醚。维生素C乙基醚的结构如下式(I)所示。
在本文中，“4-羟乙基哌嗪乙磺酸”是指：
2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid，简称HEPES。4-羟乙基哌嗪乙磺酸的结构如下式(II)所示。
在本文中，“腺苷”是指：Adenosine，又称9-β-D-呋喃核糖基腺嘌呤。腺苷的结构如下式(III)所示。
本申请
本申请提供了一种组合物，其包括：维生素C乙基醚，其含量为0.01～10％；4-羟乙基哌嗪乙磺酸，其含量为0.01～10％；腺苷，其含量为0.01～1％。
可选地，其包括：维生素C乙基醚，其含量为0.01～5％；4-羟乙基哌嗪乙磺酸，其含量为0.01～5％；腺苷，其含量为0.01～0.5％。
可选地，所述4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为4～0.5:1。
可选地，所述4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为3～0.5:1。
可选地，所述4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为2～1:1。
可选地，所述组合物中还包括抗坏血酸磷酸盐、抗坏血酸葡萄苷、抗坏血酸棕榈酸酯、抗坏血酸四异棕榈酸酯、抗坏血酸甲基硅烷醇果胶酸酯、抗坏血酸多肽中的至少一种。
可选地，所述组合物中还包括含量为0.01～0.5％的光甘草根提取物。
可选地，所述组合物中还包括含量为0.01～0.5％的麦角硫因。
可选地，所述组合物中还包括含量为0.1～2％的熊果苷。
本申请还提供了一种外用皮肤制剂，其至少包括前述的任意一种组合物。
在本申请的组合物中包括含量为0.01～10％的维生素C乙基醚、含量为0.01～10％的4-羟乙基哌嗪乙磺酸和含量为0.01～1％的腺苷。
作为优选地，在本申请的组合物中包括含量为0.01～5％的维生素C乙基醚、含量为0.01～5％的4-羟乙基哌嗪乙磺酸和含量为0.01～0.5％的腺苷。
作为优选地，4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为4～0.5:1。作为进一步优选地，4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为3～0.5:1。作为更进一步优选地，4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为2～1:1。如下述实验例11和12所示的，如果4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比较高时，对于配方的肤感影响较大，而4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比较低，则对于pH值的稳定效果较差。
作为优选地，本申请的组合物中还包括抗坏血酸磷酸盐、抗坏血酸葡萄苷、抗坏血酸棕榈酸酯、抗坏血酸四异棕榈酸酯、抗坏血酸甲基硅烷醇果胶酸酯、抗坏血酸多肽中的至少一种。
作为优选地，本申请的组合物中还包括光甘草根提取物。所述光甘草根提取物优选的添加量为0.01～0.5％。
作为优选地，本申请的组合物中还包括麦角硫因(巯基组氨酸三甲基内盐，ergothioneine，EGT)。所述麦角硫因优选的添加量为0.01～0.5％。
作为优选地，本申请的组合物中还包括熊果苷。所述熊果苷可以为α-熊果苷或β-熊果苷或二者的混合物。所述熊果苷还可以为含有α-熊果苷或β-熊果苷或二者的混合物。所述熊果苷优选的添加量为0.1～2％。
在本申请的组合物中，还可以包括其他功能性的物质，包括脱色剂、抗氧剂、脂类、增稠剂、乳化剂、保湿剂、防腐剂、增溶剂、螯合剂中的至少一种。
在本申请的组合物中，对脱色剂不作特别限定。所述脱色剂可选自氢醌、曲酸、熊果苷、鞣花酸、壬二酸、壬二酰二甘氨酸、L-抗坏血酸及其衍生物、甘草提取物、凹缘金虎尾果提取物、绣球提取物、烷氧基水杨酸、虎杖提取物、槐花提取物、姜黄提取物、桑树皮提取物、余甘子提取物、豌豆提取物、芦荟素等。
本申请对抗氧化剂不作特别限定。所述抗氧化剂可选自丁羟甲苯、丁羟茴醚、棓酸丙酯、棓酸辛酯、十二醇棓酸酯、叔丁基氢醌、生育酚、抗坏血酸棕榈酸酯、柠檬酸异丙酯混合物、单酸甘油酯柠檬酸酯、阿诺克索默、亚硫酸钠、亚硫酸氢钠、焦亚硫酸钠、半胱氨酸、异抗坏血酸、硫脲、二月桂醇硫代丙二酸酯、去甲二氢愈创木酸、硫辛酸、α-生育酚乙酸酯、类胡萝卜素、余甘子单宁、抗坏血酸、谷胱甘肽、辅酶Q10等。
本申请对脂类不作特别限定。所述脂类可选自油脂，如植物油脂、动物油脂、矿物油脂、羊毛脂及其衍生物等。所述脂类可选自蜡类，如动物蜡、植物蜡、矿物蜡。所述脂类可选自脂肪酸和脂肪醇。所述脂类可选自用于合成皮肤屏障的脂质。
本申请对增稠剂不作特别限定。所述增稠剂可选自丙烯酸类聚合物及其衍生物、卡波姆聚合物、丙烯酸(酯)类/C10～C30烷醇丙烯酸酯共聚物、丙烯酸盐/C10～C30烷醇丙烯酸酯交联共聚物、丙烯酸(酯)类共聚物、聚丙烯酸酯-1交联聚合物、丙烯酸/丙烯酰氮共聚物、丙烯酸(酯)类/硬脂醇聚醚(20)甲基丙烯酸酯共聚物、丙烯酸(酯)类/山嵛醇聚醚(25)甲基丙烯酸酯共聚物、丙烯酸(酯)类/硬脂醇聚醚-20衣康酸酯共聚物、丙烯酸(酯)类/氨基丙烯酸酯共聚物、丙烯酸(酯)类/异癸酸乙烯酯交联聚物、硬脂醇聚醚(10)烯丙基醚/丙烯酸(酯)类共聚物、丙烯酸类共聚物钠盐/矿油/PPG-1十三醇聚醚-6、甘油聚甲基丙烯酸酯及其复配物、蓖麻油/IPDI共聚物、丙烯酰胺共聚物复配物、丙烯酰胺/丙烯酸钠共聚物复配物、丙烯酰二甲基牛磺酸钠/或铵共聚物及其复配物、PVM/MA癸二烯交联聚合物、PEG-150/癸醇/SMDI共聚物、聚季铵盐-31和聚季铵盐-37复配物、聚乙烯和聚乙烯共聚物、聚乙二醇、聚氧化乙烯、PEG-120甲基葡糖二油酸酯、PEG-120失水山梨醇三异硬脂酸酯、聚乙烯醇、PEG-150季戊四醇四硬脂酸酯、三羟硬脂精、氢氧化铝/镁硬脂酸盐等。
本申请对表面活性剂不作特别限定。所述表面活性剂可以为阴离子表面活性剂、阳离子表面活性剂、非离子表面活性剂、两性表面活性剂、天然表面活性剂、含氟表面活性剂等。
本申请对保湿剂不作特别限定。所述保湿剂可选自甘油、丙二醇、丁二醇、山梨(糖)醇、山梨醇聚醚-20、酰胺类保湿剂、甘油聚醚类保湿剂、乳酸和乳酸钠、吡络烷酮羧酸钠、羟乙基脲、赤藓醇、甘油聚醚-5乳酸酯、透明质酸钠、糖类同分异构体、D-泛醇、聚乙二醇、双甘油、甲基丙烯酰氧乙基磷酸胆碱等。
本申请对防腐剂不作特别限定。所述防腐剂可选自羟苯酯类及其盐类、甲醛和甲醛供体、异噻唑啉酮类、酚类防腐剂、酸类防腐剂、卤化物防腐剂、季铵化合物、醇类、常用的复配防腐剂和天然防腐剂等。
本申请对增溶剂不作特别限定。
本申请对螯合剂不作特别限定。例如，所述螯合剂可选自乙二胺四乙酸及其钠盐、甘氨酸、柠檬酸、琥珀酸等。
本申请的外用皮肤制剂
本申请的外用皮肤制剂可以是护肤品或化妆品，本申请的外用皮肤制剂的剂型可以是化妆水、精华液、喷雾、乳液、面霜、面膜、凝胶、防晒、隔离中的任意一种。
实施例1
实施例1的配方如表1所示。
表1
实施例1的制备工艺：
将1号原料称好，在搅拌(搅拌速度为1000rpm)的同时依次加入2～5号原料，同时开启升温。在升温至85～90℃后保温20min并搅拌(搅拌速度30～50rpm)，随后降温。在降温至45～50℃后继续搅拌，并依次加入B相原料和C相原料。待降温至约38℃，检验合格后出料。
实施例2
实施例2的配方如表2所示。
表2
实施例2的制备工艺：
将1号原料称好，在搅拌(搅拌速度为1000rpm)的同时依次加入2～5号原料，同时开启升温。在升温至85～90℃后保温20min并搅拌(搅拌速度30～50rpm)，随后降温。在降温至45～50℃后继续搅拌，并依次加入B相原料和C相原料。待降温至约38℃，检验合格后出料。
实验部分
配置实验例1～10，实验例1～10的配方如下表3所示。
表3
测试
分别检测实验例1～10在配方配置完成后以及在50℃环境下静置1个月后的pH值和粘度。检测结果如下表4所示。
表4
通过表4的结果可以看出，实验例1在未加入pH缓冲剂的情况下，配方体系的粘度较好，但在静置1月后pH值明显下降了。实验例2和实验例3中分别添加了柠檬酸-柠檬酸钠的pH缓冲体系、磷酸氢二钠-磷酸二氢钠的pH缓冲体系，虽然静置1月后pH值前后变化不大，但配方的粘度始终不高，影响体系的稳定性，肤感较差。实验例4和实验例5在加入腺苷(同时未加入柠檬酸-柠檬酸钠的pH缓冲体系或者磷酸氢二钠-磷酸二氢钠的pH缓冲体系)后，配方体系的粘度较为理想，pH值相较加入柠檬酸-柠檬酸钠的pH缓冲体系或者磷酸氢二钠-磷酸二氢钠的pH缓冲体系时较低。实验例6和实验例7在加入HEPES(同时未加入柠檬酸-柠檬酸钠的pH缓冲体系或者磷酸氢二钠-磷酸二氢钠的pH缓冲体系或者腺苷)后，配方体系的粘度较为理想，pH值相较加入柠檬酸-柠檬酸钠的pH缓冲体系或者磷酸氢二钠-磷酸二氢钠的pH缓冲体系时较低。实验例8～10中，同时加入腺苷和HEPES的情况下，不仅配方的粘度较好而且在静置1月后配方仍能保持理想的pH值范围。
配置实验例11和实验例12，实验例11和12的配方如下表5所示。
表5
测试
分别检测实验例11和12在配方配置完成后以及在50℃环境下静置1个月后的pH值和粘度。检测结果如下表6所示。
表6
| 实验例 | 实验例11 | 实验例12 |
| 初始粘度(2#/60速，mps) | 160 | 190 |
| 初始pH(直测) | 5.5 | 5.25 |
| 50℃一个月粘度(2#/60速，mps) | 135 | 150 |
| 50℃一个月pH(直测) | 5.12 | 4.65 |
| 肤感打分 | 7 | 8 |
通过表6的结果可以看出，实验例11中HEPES与维生素C乙基醚的含量比为4:1，实验例11的配方体系的初始粘度就偏低，在放置1月后粘度虽下降幅度较小，但肤感与实施例8～10相比明显较差。实施例12中HEPES与维生素C乙基醚的含量比为1:5，在放置1月后实施例12的配方体系的肤感与实施例8～10相比无明显差别，但pH值下降较多。申请人以为，当HEPES与维生素C乙基醚的含量比为4～0.5:1时，更有利于配方的肤感提升和pH值稳定。
基于本申请中的实施例，本领域普通技术人员在没有付出创造性劳动的前提下所获得的所有其他实施例，都属于本申请保护的范围。
本领域的普通技术人员，可以对上述各实施例所记载的技术方案进行修改，或者对其中部分技术特征进行等同替换；而这些修改或者替换，并不使相应技术方案的本质脱离本申请各实施例技术方案的保护范围。
Claims (10)
1.一种组合物，其特征在于，其包括：
维生素C乙基醚，其含量为0.01～10％；
4-羟乙基哌嗪乙磺酸，其含量为0.01～10％；
腺苷，其含量为0.01～1％。
2.如权利要求1所述组合物，其特征在于，所述组合物中还包括含量为0.1～2％的熊果苷。
3.如权利要求1所述组合物，其特征在于，所述组合物中还包括含量为0.01～0.5％的光甘草根提取物。
4.如权利要求1所述组合物，其特征在于，所述组合物中还包括含量为0.01～0.5％的麦角硫因。
5.如权利要求1所述组合物，其特征在于，所述组合物中还包括抗坏血酸磷酸盐、抗坏血酸葡萄苷、抗坏血酸棕榈酸酯、抗坏血酸四异棕榈酸酯、抗坏血酸甲基硅烷醇果胶酸酯、抗坏血酸多肽中的至少一种。
6.如权利要求1所述组合物，其特征在于，所述4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为4～0.5:1。
7.如权利要求1所述组合物，其特征在于，所述4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为3～0.5:1。
8.如权利要求1所述组合物，其特征在于，所述4-羟乙基哌嗪乙磺酸与维生素C乙基醚的含量比为2～1:1。
9.如权利要求1所述组合物，其特征在于，包括：
维生素C乙基醚，其含量为0.01～5％；
4-羟乙基哌嗪乙磺酸，其含量为0.01～5％；
腺苷，其含量为0.01～0.5％。
10.一种外用皮肤制剂，其特征在于，其至少包括如权利要求1～9任一所述的组合物。
Priority Applications (1)
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