CN116650386A - 人体美白的组合物及其制备方法 - Google Patents
人体美白的组合物及其制备方法 Download PDFInfo
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- CN116650386A CN116650386A CN202310881612.5A CN202310881612A CN116650386A CN 116650386 A CN116650386 A CN 116650386A CN 202310881612 A CN202310881612 A CN 202310881612A CN 116650386 A CN116650386 A CN 116650386A
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- skin
- whitening
- mixing
- human body
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Abstract
本发明涉及护肤品技术领域，具体涉及一种人体美白的组合物及其制备方法。人体美白的组合物含有植物提取组合物，植物提取组合物包含组分：黄檗树皮提取物、苦扁桃仁油、甘草根提取物、芦荟提取物、水飞蓟素、刺梨果提取物。本发明提供的植物提取组合物中的各组分间具有相互促进作用，能够有效的提亮肌肤，淡化黑斑、褐斑，起到美白淡斑的效果，本发明还提供了采用该人体美白组合物的皮肤驻留剂及其制备方法。
Description
技术领域
本发明涉及护肤品技术领域，具体涉及一种人体美白的组合物及其制备方法。
背景技术
随着社会经济发展，生活压力与日俱增，加上目前空气污染，城市雾霾，紫外线照射，以及长期面对手机电脑等电子屏幕的辐射的现状，容易导致现代女性皮肤变得坑坑洼洼、黯淡无光，由此皮肤暗黄、色素沉着、色斑云集等不良症状越来越多见，改善肤色成为现代人类越来越重视的领域，美白功效的护肤品研发也备受关注。
皮肤护理需要考虑多方面影响因素，功效性化妆品需要多种功效成分的协同作用。根据皮肤美白机制，将抑制酪氨酸酶活性、抗氧化以及抑制黑素小体迁移等不同功效成分透皮共输送，促进皮肤功效成分富集美白护肤靶部位。
目前市面上大多数美白组合物含有的抗氧化美白成分，具有很强的酪氨酸酶抑制活性和DPPH自由基清除活性，但是该类美白组合物中活性物质透皮性不佳，使美白组合物中大量活性成分未被吸收，只有少部分作用于皮肤，降低了美白组合物的使用效率。
发明内容
为克服现有技术的不足，本发明的目的在于提供一种具有高效的羟自由基消去活性和具有良好透皮吸收率的人体美白组合物，使得采用该组合物制备得到的皮肤驻留剂具有减少皮肤的黑色素、美白淡斑的功效。
为实现上述目的，本发明提供以下技术方案：
本发明第一方面提供一种人体美白的组合物，含有植物提取组合物，所述植物提取组合物包含以下质量份数组分：
黄檗树皮提取物10-15份；
苦扁桃仁油60-70份；
甘草根提取物10-15份；
芦荟提取物6-9份；
水飞蓟素1-1.5份；
刺梨果提取物0.6-0.8份。
具体地，人体美白的组合物含有以下质量百分比组分：
植物提取组合物3-6％；
磷脂酰胆碱1.5-2.5％；
芳樟醇0.1-0.15％。
具体地，所述磷脂酰胆碱与芳樟醇质量比为(10-25):1；更具体地，质量比为(14-15):1。
本发明第二方面提供了一种人体美白的皮肤驻留剂，包含前述人体美白的组合物。
具体地，还包含组分：稳定剂、增稠剂、防腐剂、pH调节剂、水。
更具体地，包含以下质量百分比组分：
植物提取组合物3-6％；
磷脂酰胆碱1.5-2.5％；
芳樟醇0.1-0.15％；
稳定剂0.1-0.3％；
增稠剂0.05-0.1％；
防腐剂0.1-0.2％；
pH调节剂0.05-0.15％。
稳定剂优选：EDTA二钠、C14-22醇、聚异丁烯；
增稠剂优选：卡波姆、黄原胶、鲸蜡醇；
防腐剂优选：双(羟甲基)咪唑烷基脲、苯甲醇、咪唑烷基脲；
pH调节优选：三乙醇胺、氢氧化钠。
本发明第三方面提供了一种前述皮肤驻留剂的制备方法，其特征在于，包含以下步骤：
(1)将配方量的植物提取组合物、磷脂酰胆碱、芳樟醇与部分溶剂均质混合，得混合物A；
(2)将配方量的增稠剂和部分溶剂均质混合，得混合物B；
(3)将混合物A、混合物B、稳定剂、防腐剂和剩下的溶剂进行混合，并用pH调节剂调节pH值，得所述的皮肤驻留剂。
皮肤驻留剂的溶剂一般为水；而如果选择制备油基或其他用途的皮肤驻留剂如消毒膏等，可以选择符合相关规定的植物油、矿物脂或酒精的有机溶剂。
具体地，步骤(1)均质转速为6000-10000rpm，混合温度50-60℃；
步骤(2)均质转速为4000-5000rpm，混合温度40-50℃；
步骤(3)混合转速为120-130rpm，混合温度20-45℃，混合时间30-60min，pH值调节至6-7。
本发明中：
黄檗树皮提取物的主要成分是小檗碱，还含有巴马亭药根碱、黄柏碱、蝙蝠葛任碱、白桥楼碱和黄柏桐等，能够促进胶原蛋白的生成，结合其抗氧化性，黄檗树皮提取物具有抗衰的作用，还具有抗炎性和抑臭的作用。
甘草根提取物具有优异的抗氧化作用，其含有丰富甘草酸、甘草素等活性成分；其中甘草酸有明确的抑制黑色素形成的作用，它可以抑制酪氨酸酶的活性；而甘草素、甘草次酸等也有类似的效果；而甘草黄酮、甘草内脂等具有明确的抗氧化作用；同时，甘草根提取物还具有一定保湿作用，可以增加皮肤的水分含量，减少水分流失，有助于保持皮肤的水润和柔软，并改善干燥和粗糙的皮肤质感。
苦扁桃仁油中富含维生素E、脂肪酸和抗氧化物质，有助于对抗自由基的损害，减缓皮肤的衰老，减轻疤痕和色斑的出现，改善皮肤色调的均匀性，苦扁桃仁油还可以深层滋润和保护皮肤，有助于改善干燥、粗糙和受损的皮肤；苦扁桃仁油同时还具有舒缓和抗炎作用，可缓解皮肤炎症和敏感问题。本发明发现苦扁桃仁油相比于甜扁桃仁油在本发明的配方中更具有美白的效果；本发明推测是苦扁桃仁油中较高含量的苦杏仁苷以及其他成分对美白有一定的促进作用。
水飞蓟素主要成分有水飞蓟宾、异水飞蓟宾、水飞蓟宁和水飞蓟亭等，是一种天然的黄酮木脂素类化合物，具有良好的清除自由基的作用。
刺梨果提取物含有丰富的抗氧化成分维生素C、儿茶素、花青素等，也富含多种氨基酸，如谷氨酸、丝氨酸和赖氨酸等，同时含有一定的脂肪酸，如亚油酸和油酸等；刺梨果提取物能够有效的清除自由基，抑制黑色素的产生，提亮肤色，淡化黑斑，它也能够减少氧化应激对细胞的损害，预防和延缓衰老，保护皮肤细胞的健康。
磷脂酰胆碱可以有效促进营养物质的透皮吸收。透皮吸收是指物质通过皮肤屏障进入体内的过程，通常情况下，皮肤的角质层会限制物质的渗透。然而，磷脂酰胆碱作为一种透皮辅助剂，具有疏松角质层和改善皮肤屏障功能的作用，增加营养物质对皮肤的渗透性，提高皮肤对营养物质的吸收效果。本发明研究发现芳樟醇对磷脂酰胆碱的透过率具有促进作用，二者之间具有相互促进的作用。
本发明的有益效果：
1.本发明中黄檗树皮提取物、苦扁桃仁油、甘草根提取物、芦荟提取物、水飞蓟素和刺梨果提取物之间具有相互促进的作用；
2.本发明中人体美白组合物在磷脂酰胆碱与芳樟醇的协同作用下提高了透皮吸收率，促进皮肤对营养物质的吸收，提高了美白效果。
3.本发明能够有效的提亮肌肤，淡化黑斑、褐斑，起到美白淡斑的效果。
具体实施方式
为了更好地理解本发明，下面结合具体实施例对本发明作进一步的描述，其中实施例中使用的术语是为了描述特定的具体实施方案，不构成对本发明保护范围的限制。
本发明中：
黄檗树皮提取物为黄檗(PHELLODENDRONAMURENSE)树皮提取物，英文名称为PHELLODENDRON AMURENSE BARK EXTRACT，CAS号为164288-52-2，购自宁夏香草生物技术有限公司。
苦扁桃仁油为苦扁桃(PRUNUS AMYGDALUS AMARA)仁油，英文名称为PRUNUSAMYGDALUS AMARA(BITTERALMOND)KERNEL OIL，CAS号为8013-76-1，购自东莞市立帆香料有限公司。
甘草根提取物为甘草(GLYCYRRHIZAURALENSIS)根提取物，英文名称为GLYCYRRHIZAURALENSIS(LICORICE)ROOT EXTRACT，购自赣州佰珍堂生物科技有限公司。
芦荟提取物为ALOEYOHJYU MATSU EKISU，购自陕西嘉禾药业有限公司。
水飞蓟素CAS号为65666-07-1，购自武汉福鑫化工有限公司。
刺梨果提取物为刺梨(ROSA ROXBURGHII)果提取物，购自杭州雪域生物技术有限公司。
磷脂酰胆碱市售可得。
芳樟醇市售可得。
下列实施例中未注明具体条件的实验方法，通常按照常规条件，或按照制造厂商所建议的条件。除非另外说明，否则百分比和份数按重量计算。
植物提取组合物的制备，包括以下步骤：
步骤(1)，按表1质量份数称取原料；
步骤(2)，将称取的原料置于搅拌罐中混合均匀。
表1植物提取组合物的组分
| 组分含量\序号 | 组合物1 | 组合物2 | 组合物3 | 组合物4 | 组合物5 | 组合物6 |
| 黄檗树皮提取物 | 10 | 15 | 15 | 10 | 10 | —— |
| 苦扁桃仁油 | 70 | 60 | 70 | 60 | 70 | 70 |
| 甘草根提取物 | 10 | 15 | 10 | 10 | 10 | 20 |
| 芦荟提取物 | 6 | 6 | 6 | 9 | 6 | 10 |
| 水飞蓟素 | 1.5 | 1.5 | 1.5 | 1 | —— | —— |
| 刺梨果提取物 | 0.8 | 0.8 | 0.8 | 0.6 | —— | —— |
注：表1中“——”表示没有添加。
人体美白皮肤驻留剂的制备，包括以下步骤：
步骤(1)，按表2所示称取原料，将植物提取组合物、磷脂酰胆碱、芳樟醇与部分蒸馏水在60℃下均质混合，均质机转速设置在7800rpm，得到混合溶液A；混合时温度可设置在50-60℃，均质机转速可设置在6000-10000rpm。
步骤(2)增稠剂和部分蒸馏水在50℃下使用均质机进行混合，转速设置在5000rpm，得到混合溶液B；混合时温度可设置在40-50℃，均质机转速可设置在4000-5000rpm。
步骤(3)，将混合溶液A、混合溶液B、稳定剂、防腐剂和剩余蒸馏水在转速为120rpm、温度为40℃下进行混合60min，混合过程中利用pH调节剂调节pH值至6.5，得到人体美白皮肤驻留剂；其中混合时转速可设置在120-130rpm，温度可设置在20-45℃范围内，混合时间30-60min为宜，混合溶液pH值控制在6-7之间。
表2人体美白的皮肤驻留剂组分
注：表2组分含量均为质量百分比(单位％)，“——”表示没有添加。
样品稳定性测试：
1.耐热测试：恒温培养箱调节到40℃，将前述制取的4个实施例和5个对比例分别作为9个待测样品，每个待测样品取三支装于透明玻璃瓶中，装样量为20ml/瓶，封口后置于恒温培养箱内，三个月后取出，恢复至室温，观察外观变化。
2.耐寒测试：恒温培养箱调节到-10℃，将前述制取的4个实施例和5个对比例分别作为9个待测样品，每个待测样品取三支装于透明玻璃瓶中，装样量为20ml/瓶，封口后置于恒温培养箱内，三个月后取出，恢复至室温，观察外观变化。
3.常温测试：将前述制取的4个实施例和5个对比例分别作为9个待测样品，每个待测样品取三支装于透明玻璃瓶中，装样量为20ml/瓶，封口后常温下放置6个月后，观察样品的外观变化。
耐热测试、耐寒测试、常温测试均未观察到析出、沉淀等现象，保持原来外观。
人体皮肤斑贴测试：
将前述制备的4个实施例和5个对比例参照《2022化妆品安全技术规范》中的人体皮肤斑贴实验。
分别于30min(待压痕消失后)、24h和48h按标准观察皮肤反应，并记录观察结果，见表3。
表3人体安全性测试结果
| 编号 | 30min | 24h | 48h |
| 实施例1 | 0级，30人 | 0级，30人 | 0级，30人 |
| 实施例2 | 0级，30人 | 0级，30人 | 0级，30人 |
| 实施例3 | 0级，30人 | 0级，30人 | 0级，30人 |
| 实施例4 | 0级，30人 | 0级，30人 | 0级，30人 |
| 对比例1 | 0级，30人 | 0级，30人 | 0级，30人 |
| 对比例2 | 0级，30人 | 0级，30人 | 0级，30人 |
| 对比例3 | 0级，30人 | 0级，30人 | 0级，30人 |
| 对比例4 | 0级，30人 | 0级，30人 | 0级，30人 |
| 对比例5 | 0级，30人 | 0级，30人 | 0级，30人 |
DPPH自由基清除能力的测定：
DPPH用无水乙醇配制成2×10-4mol/L的溶液，实施例1-4和对比例1-5皮肤驻留剂作为待检测液，制备待检测液、无水乙醇、DPPH溶液各2mL若干份，分别将混匀后室温下放置30分钟，于波长517nm处测定吸光度得Ai，每个样品平行测定3次，取平均值。
以Vc作为阳性对照，以无水乙醇代替DPPH测定吸光度值作为对照Aj空白，以DPPH溶液和无水乙醇混合测吸光度Ac。
按下式(1)计算各待测样品对DPPH自由基的清除率，并记录至下表4。
清除率(％)＝(1-(Ai-Aj)/Ac)×100％...........(1)
式中：Ai为2mL实施例或对比例液+2mLDPPH试剂混合液的吸光度；Aj为2mL样品溶液+2mL无水乙醇混合液的吸光度；Ac为2mLDPPH溶液+2mL无水乙醇混合液的吸光度。
超氧自由基O2 -·清除能力的测定：
分别将实施例1-4和对比例1-5皮肤外用剂作为待检测液，精密吸取1mL待测液，分别加入4.5mL，50mmol/L的pH＝8.2的Tris-HCl缓冲液，然后混匀，于25℃恒温水浴中保温20分钟后取出，立即加入25mmol/L邻苯三酚溶液0.3mL，快速摇匀后于25℃恒温水浴中反应5分钟，再加入8mmol/L HCl 1mL，混匀后终止反应，在325nm测定吸光度，以蒸馏水代替样品作为空白对照。以Vc作阳性对照。每个样品均平行测定3次，取平均值。
按式(2)计算清除率，并记录至下表4。
清除率(％)＝(A0-A1)/A0×100％...........(2)
式中：A0为空白的平均吸光度；A1为待检测液的平均吸光度。
清除羟自由基能力的测定：
分别将实施例1-4和对比例1-5皮肤外用剂作为待检测液，样品组试管中分别加入1mL 0.15mmol/LFeSO4、0.4mL 2mmol/L水杨酸、0.2mL待检测液、1mL6mmol/L H2O2和0.4mL蒸馏水；空白组用蒸馏水代替待检测液，对照组用蒸馏水代替水杨酸，37℃反应30分钟。以Vc作阳性对照。每个样品均平行测定3次，取平均值。
按式(3)计算羟自由基能力清除率，并记录至下表4。
清除率(％)＝(A空白-(A样品-A对照))/A空白×100％...........(3)
体外透皮试验：
将ICR种小鼠(25±5)g断颈处死后，剔除胸腹部毛发，剪下胸腹部皮肤，去除其皮下脂肪及黏液组织后洗净，置于生理盐水中，冰箱4℃保存备用。
实验时将小鼠皮肤固定在改良的Franz扩散池的上、下两室之间，角质层朝上，与待检测液紧密接触，接收池(扩散面积S＝2.1cm2，容积为13.5mL)中30％乙醇生理盐水为接收液，且接收液与皮肤真皮层刚好接触，接收池内置一磁力搅拌棒，搅拌速度为300rpm，水浴温度为(37±1)℃。12h后从接收池中吸取5mL，将所取样品液用0.45μm微孔滤膜过滤，置于EP管中，进行HPLC检测。色谱条件：十八烷基硅烷键合硅胶为填充剂；乙腈-水(55:45)为流动相；检测波长为205nm，测定取出的接收液中腺苷酸的含量计算腺苷酸透过量，并根据腺苷酸透过量计算待测溶液透过量，记录至下表4。
表4
皮肤美白淡斑试验：
筛选面部肤色较为暗淡且面部有色斑的自愿者54名，年龄在25-27岁，按人数平均分成9组，分别以实施例1-4和对比例1-5进行分组，每组各自使用对应的待测样品，根据《化妆品紫外线诱导人体皮肤黑化模型祛斑美白功效测试法》中的试验方法进行检测试验。
试用者在早、晚上清洁面部后使用前述制备的实施例和对比例的待测样品，连续使用4周，使用皮肤色差测试探头及多功能皮肤测试***(CL400和MPA6，德国CK)和皮肤红黑色素测试仪及测试探头(Mexameter MX18，德国CK公司)，分别于试用者使用前(第0周)、使用第1周、和使用第4周后进行对试用者面部进行数据采集，计算试用者使用化妆品前后皮肤白度(亮度)/L和皮肤黑色素含量/MI的变化，L值表征L*为白平衡，值越大，颜色越偏向白色；MI测量数值越高，说明皮肤中黑色素含量越高；每小组测试结果取平均值，具体结果如表5所示。
表5
试验结果分析
根据表4中实施例1与对比例5相比可知，配方组分中添加磷脂酰胆碱和芳樟醇的透皮率明显比单独添加磷脂酰胆碱的透皮率高，说明芳樟醇与磷脂酰胆碱能够相互促进、协同增效，根据表4结果可知，磷脂酰胆碱与芳樟醇在配方中的质量比在(14-15):1时透皮率更为优异。
根据表4、5中实施例1与对比例1-2相比可知，植物提取组合物中只添加苦扁桃仁油、甘草根提取物、芦荟提取物和黄檗树皮提取物也具有一定的抗氧化和美白的效果；而水飞蓟素、刺梨果提取物、苦扁桃仁油、甘草根提取物、芦荟提取物和黄檗树皮提取物的复配相比于只有苦扁桃仁油、甘草根提取物、芦荟提取物和黄檗树皮提取物的抗氧化和美白效果更优。
虽然以上描述了本发明的具体实施方式，但是本领域的技术人员应当理解，这仅是举例说明，本发明的保护范围是由所附权利要求书限定的。本领域的技术人员在不背离本发明的原理和实质的前提下，可以对这些实施方式做出多种变更或修改，但这些变更和修改均落入本发明的保护范围。
Claims (10)
1.一种人体美白的组合物，其特征在于，含有植物提取组合物，所述植物提取组合物包含以下质量份数组分：
2.根据权利要求1所述的人体美白的组合物，其特征在于，含有以下质量百分比组分：
植物提取组合物3-6％；
磷脂酰胆碱1.5-2.5％；
芳樟醇0.1-0.15％。
3.根据权利要求书2所述的人体美白的组合物，其特征在于，所述磷脂酰胆碱与芳樟醇质量比为(10-25):1。
4.根据权利要求书3所述的人体美白的组合物，其特征在于，所述磷脂酰胆碱与芳樟醇质量比为(14-15):1。
5.一种人体美白的皮肤驻留剂，其特征在于，包含权利要求2-4任一所述的人体美白的组合物。
6.根据权利要求5所述的皮肤驻留剂，其特征在于，还包含组分：稳定剂、增稠剂、防腐剂、pH调节剂、溶剂。
7.根据权利要求6所述的皮肤驻留剂，其特征在于，包含以下质量百分比组分：
8.根据权利要求6或7所述的皮肤驻留剂，其特征在于，稳定剂为EDTA二钠、C14-22醇、聚异丁烯中的至少一种；
增稠剂为卡波姆、黄原胶、鲸蜡醇中的至少一种；
防腐剂为双(羟甲基)咪唑烷基脲、苯甲醇、咪唑烷基脲中的至少一种；
pH调节剂为三乙醇胺、氢氧化钠中的至少一种。
9.一种根据权利要求7或8所述皮肤驻留剂的制备方法，其特征在于，包含以下步骤：
(1)将配方量的植物提取组合物、磷脂酰胆碱、芳樟醇与部分溶剂均质混合，得混合物A；
(2)将配方量的增稠剂和另一部分溶剂均质混合，得混合物B；
(3)将混合物A、混合物B、稳定剂、防腐剂和余下溶剂进行混合，并用pH调节剂调节pH值，得所述的皮肤驻留剂。
10.根据权利要求9所述的皮肤驻留剂的制备方法，其特征在于，步骤(1)均质转速为6000-10000rpm，混合温度50-60℃；
步骤(2)均质转速为4000-5000rpm，混合温度40-50℃；
步骤(3)混合转速为120-130rpm，混合温度20-45℃，混合时间30-60min，pH值调节至6-7。
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| CN111728209A (zh) * | 2019-03-25 | 2020-10-02 | 株式会社爱茉莉太平洋 | 用于增强水飞蓟素的生物利用度的组合物 |
| CN113208959A (zh) * | 2021-04-30 | 2021-08-06 | 广州市科能化妆品科研有限公司 | 一种抑制黑色素生成的组合物、美白精华及其制备方法和应用 |
| CN114053186A (zh) * | 2021-12-09 | 2022-02-18 | 中国农业科学院都市农业研究所 | 一种玫瑰长效保湿美白的精华水及其制备方法 |
| CN116035980A (zh) * | 2023-02-21 | 2023-05-02 | 上海幸研生物科技有限公司 | 一种皮肤美白和祛斑功效的纳米脂质体组合物及其制备方法和应用 |
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| CN111728209A (zh) * | 2019-03-25 | 2020-10-02 | 株式会社爱茉莉太平洋 | 用于增强水飞蓟素的生物利用度的组合物 |
| CN113208959A (zh) * | 2021-04-30 | 2021-08-06 | 广州市科能化妆品科研有限公司 | 一种抑制黑色素生成的组合物、美白精华及其制备方法和应用 |
| CN114053186A (zh) * | 2021-12-09 | 2022-02-18 | 中国农业科学院都市农业研究所 | 一种玫瑰长效保湿美白的精华水及其制备方法 |
| CN116035980A (zh) * | 2023-02-21 | 2023-05-02 | 上海幸研生物科技有限公司 | 一种皮肤美白和祛斑功效的纳米脂质体组合物及其制备方法和应用 |
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