CN114246875B - 一种抗炎祛斑的复方烟酰胺组合物及其应用 - Google Patents
一种抗炎祛斑的复方烟酰胺组合物及其应用 Download PDFInfo
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Abstract
本发明公开了一种抗炎祛斑的复方烟酰胺组合物及其应用，该组合物中主要包括烟酰胺和单葡萄糖醛酸甘草次酸盐，两者的重量比为(80‑120):(10～100)。与现有技术相比，本发明将单葡萄糖醛酸甘草次酸盐与烟酰胺复配，该组合可有效缓解烟酰胺对皮肤的刺激作用，使高浓度烟酰胺可以安全地应用到药用制剂或药用化妆品中，从而达到高效抗炎、祛斑的目的。
Description
技术领域
本发明属于药用制剂和药用化妆品领域，具体为一种抗炎祛斑的复方烟酰胺组合物及其应用。
背景技术
烟酰胺是维生素B3的衍生物，作为B族维生素的一员,其一直以抗衰老的功效为医学、美容界所共知。被广泛地应用于临床防治糙皮病、舌炎、口炎、光感性皮炎和化妆性皮炎的治疗。在化妆品领域，烟酰胺可以促进皮肤的新陈代谢，具有美白，抗衰老，收缩毛孔，控油祛痘的效果。除此之外，烟酰胺还可以促进含黑色素的角质细胞脱落，激活细胞内的一种酶，而这种酶刺激之后的产物，又正好可以减少黑色素的生成，因而具有良好的祛斑效果。
但酰胺类化合物在日常的储存中会慢慢水解产生羧酸化合物，因而叶酸作为杂质会不可避免地出现在烟酰胺中。叶酸会引起皮肤的刺激，出现发红、发肿等过敏反应。同时如果机体皮肤过于敏感，叶酸会引起皮肤过敏的现象，甚至会出现头晕、恶心等症状。这是烟酰胺不耐受的主要原因。研究表明：烟酰胺成分一旦超过4％的浓度，就可能有约20％的人发生不耐受的反应。对于肌肤来说，2％以下的浓度相对安全一些，但临床实验发现，浓度超过3％才有明显效果。烟酰胺受此限制，不能高浓度地添加到外用药物和日用化妆品中，难以发挥其良好的护肤、美白功效。
发明内容
发明目的：本发明的目的在于提供一种抗炎祛斑的复方烟酰胺组合物及其应用，烟酰胺通过与单葡萄糖醛酸甘草次酸盐的组合复配，从而减少烟酸对皮肤的刺激，使烟酰胺可以高浓度地应用到外用药物和日用化妆品中。
技术方案：为实现上述目的，本发明采用的技术方案为：
一种复方烟酰胺组合物，其主要包括烟酰胺和单葡萄糖醛酸甘草次酸盐，两者的重量比为(80-120):(10～100)。
优选的，所述单葡萄糖醛酸甘草次酸盐为单葡萄糖醛酸甘草次酸的钾盐、钠盐或者铵盐。
优选的，所述组合物所处的pH环境为5～7之间。
优选的，所述组合物为溶液形式，其中，烟酰胺的质量浓度为8-12％(w/v)，单葡萄糖醛酸甘草次酸盐的质量浓度为3-8％(w/v)，最优选8％(w/v)。
进一步优选的，所述溶液的溶剂选自磷酸盐缓冲液；所述组合物中还包括质量浓度为0.4-0.6％(w/v)的增溶剂；
更进一步优选的，所述增溶剂选自PEG-60氢化蓖麻油。
本发明还提供了所述的复方烟酰胺组合物在制备抗炎祛斑药物或者抗炎祛斑化妆品中的应用。
优选的，所述复方烟酰胺组合物可以制成膏贴、乳膏、酊剂或溶液剂等外用制剂。
本发明中复配的单葡萄糖醛酸甘草次酸盐作用原理如下：
单葡萄糖醛酸甘草次酸(18α-GAMG)可通过抑制炎症发生的主要通路，调节免疫细胞产生与凋亡、抗体的产生等抑制过敏反应，具有极强的抗敏活性。同时，游离的葡(萄)糖醛酸，快速清除自由基，减少皱纹，淡化色斑，它还是一种解毒剂，能与重金属和含有羟基、羧基、巯基的有毒物质及防腐剂结合，形成无毒或低毒的葡萄糖醛酸结合物排出体外，起到皮肤解毒的作用，降低毒性成分的致敏性。
有益效果：与现有技术相比，本发明将单葡萄糖醛酸甘草次酸盐与烟酰胺复配，该组合可有效缓解烟酰胺对皮肤的刺激作用，使高浓度烟酰胺可以安全地应用到药用制剂或药用化妆品中，从而达到高效抗炎、祛斑的目的。
具体实施方式
为了更加详细直观地展示本发明的技术方案、目的和优点，下面结合具体实施例对本发明做进一步的详细描述。
实施例
1.溶液的配制
把相关成分组合配成一系列的水溶液，每份水溶液体积为100mL，由于不同组分水溶性和稳定性存在差异，为了保证发明中实验结果的稳定可靠，所有水溶液均加入质量浓度为0.5％的PEG-60氢化蓖麻油增溶，且使用磷酸二氢钠和磷酸氢二钠将体系配制成浓度为0.2mol/L的磷酸二氢钠-磷酸氢二钠的缓冲液，使所有水溶液的pH均为6.0。所使用的PEG-60氢化蓖麻油为化妆品级，纯度为98％，磷酸二氢钠和磷酸氢二钠均为分析纯及以上。具体成分和质量浓度如下：
对照组:1％烟酰胺+0.5％PEG-60氢化蓖麻油(溶液1)
10％烟酰胺+0.5％PEG-60氢化蓖麻油(溶液2)
实验组:10％烟酰胺+0.5％PEG-60氢化蓖麻油+1％单葡萄糖醛酸甘草次酸钠(溶液3)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+2％单葡萄糖醛酸甘草次酸钠(溶液4)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+3％单葡萄糖醛酸甘草次酸钠(溶液5)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+4％单葡萄糖醛酸甘草次酸钠(溶液6)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+5％单葡萄糖醛酸甘草次酸钠(溶液7)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+6％单葡萄糖醛酸甘草次酸钠(溶液8)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+7％单葡萄糖醛酸甘草次酸钠(溶液9)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+8％单葡萄糖醛酸甘草次酸钠(溶液10)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+9％单葡萄糖醛酸甘草次酸钠(溶液11)
10％烟酰胺+0.5％PEG-60氢化蓖麻油+10％单葡萄糖醛酸甘草次酸钠(溶液12)
2.实验步骤
溶液1、2为对照组，溶液3-12为实验组。实验对象为100名志愿者，男女各50人，年龄阶段在20～55岁之间。受试者在使用肥皂统一清洗胳膊内壁后,使用棉签分别沾取上述12组溶液分别均匀涂抹在胳膊内壁的皮肤上面，感受溶液对皮肤的刺激性，观察皮肤受刺激反应。每次涂抹溶液后清洗胳膊，至少间隔30分钟，保证每次的刺激感觉不会影响下一次的刺激感觉。实验结果如表1所示。
表1：溶液1-12产生刺激反应的人数比例
表2：溶液1-12的成分比例
由表1结果可以看出，低浓度的烟酰胺(1％)对人体皮肤的刺激很小，而高浓度的烟酰胺(10％)对人体皮肤会产生很强的刺激，会普遍引起皮肤产生潮红、瘙痒、灼烧感、刺痛感的刺激反应。体系中加入1％和2％的单葡萄糖醛酸甘草次酸钠抗刺激成分，感受到刺激反应的人数比例水平与未加入之前几乎同一水平，没有明显降低刺激感的功效，但随着单葡萄糖醛酸甘草次酸钠在体系中比例的增加；从3％开始一直到8％，受测人员感受到刺激的人数比例明显呈现下降的趋势，当比例超过8％时感受到刺激的人数比例又呈现上升的趋势。综合成本与功效可以看出：组合物中烟酰胺与单葡萄糖醛酸甘草次酸盐的质量比值在100：30～80时组合物可以有效降低烟酰胺对人体皮肤刺激；单葡萄糖醛酸甘草次酸盐的含量继续升高，减少刺激的效果开始下降，虽然还是可以降低刺激，但实际的应用中使用低浓度的单葡萄糖醛酸甘草次酸盐即可代替。因此该组合物中烟酰胺与单葡萄糖醛酸甘草次酸盐的最佳质量比值为100：80。
此外，应当理解，本发明不受上述实施例的限制，上述实施例和说明书中描述的只是说明本发明的原理，任何不经过创造性劳动想到的变化或替换，都应涵盖在本发明的保护范围之内。因此，本发明的保护范围应该以权利要求书所限定的保护范围为准。
Claims (4)
1.一种复方烟酰胺组合物，其特征在于，其活性成分为烟酰胺和单葡萄糖醛酸甘草次酸钠，两者的重量比为100：80；所述组合物为溶液形式，其中，烟酰胺的w/v质量浓度为10%，单葡萄糖醛酸甘草次酸钠的w/v质量浓度为8%；所述溶液的溶剂选自磷酸盐缓冲液；所述组合物中还包括w/v质量浓度为0.5%的增溶剂，所述增溶剂选自PEG-60氢化蓖麻油。
2.根据权利要求1所述的复方烟酰胺组合物，其特征在于，所述组合物所处的pH环境为5~7之间。
3.权利要求1-2任一项所述的复方烟酰胺组合物在制备抗炎祛斑药物或者抗炎祛斑化妆品中的应用。
4.根据权利要求3所述的应用，其特征在于，所述复方烟酰胺组合物制成膏贴、乳膏或溶液剂。
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