CN104367487A - 单相增白洁齿剂 - Google Patents

单相增白洁齿剂 Download PDF

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CN104367487A
CN104367487A CN201410483766.XA CN201410483766A CN104367487A CN 104367487 A CN104367487 A CN 104367487A CN 201410483766 A CN201410483766 A CN 201410483766A CN 104367487 A CN104367487 A CN 104367487A
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peroxide
agent
carrier
whitening
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S.K.乔普拉
L.蔡徳尔
M.普伦西普
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Colgate Palmolive Co
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Abstract

单相增白洁齿剂，包括(i)选自过氧化氢、结合的过氧化物和固体过氧化物的增白剂，(ii)研磨剂和(iii)基本上无水的口腔可接受的载体，例如聚乙二醇。该结合的过氧化物可以是过氧化氢和聚合物和/或任何过氧化物化合物和多孔的交联聚合物，如聚乙烯基吡咯烷酮、聚丙烯酸酯、聚甲基丙烯酸酯和聚衣康酸酯的聚合物。该固体过氧化物可以是过硼酸钠或过氧化脲。本发明还提供通过使表面与组合物接触来增白牙表面的方法。

Description

单相增白洁齿剂
本申请是以下申请的分案申请：申请日：2006年9月12日；申请号：200680035671.5(PCT/US2006/035278)；发明名称：“单相增白洁齿剂”的分案申请。
发明背景
许多个人期望“明亮的”微笑和白色牙齿，和认为暗的和着色的牙齿美观上无吸引力的。不幸地是，在没有预防的或补救措施的情况下，由于牙齿的材料的吸收性质，着色的牙齿是几乎不可避免的。日常活动如吸烟或其它口腔使用烟制品，和吃、咀嚼或喝某些饮食(特别地，咖啡、茶叶和红葡萄酒)，引起不希望的牙齿表面的着色。着色还可以由包括那些与牙菌斑有关的微生物活性而引起。在这些材料中的色原或产生颜色的物质成为薄膜层的一部分和可以渗透釉质层。即使定期的刷牙和牙缝拉线，但是多年的色原聚集可以引起明显的牙齿变色。
在本领域中描述了各种组合物用于预防或治疗牙齿的变色。特别地，为了抵抗着色和使发亮或修复自然的釉质颜色，各种包含漂白剂的产品在市场上可买到用于专业人员和消费者使用。如今在牙齿增白中最通常使用的材料是过氧化物。从生理学的观点，过氧化物通常被认为是安全的，并且对增白牙齿可以是有效的。
专业的牙齿治疗常常包括牙表面制备，如酸蚀后应用高浓度的漂白液(例如，至多37％的过氧化氢)和/或应用热或光。这些方法提供快速的结果，但是昂贵的，和常常需要看牙科医生几次。可替换地，可以使用家庭漂白系统。在过去十年，由于低成本和提高的便利性，这些系统已经获得明显的普及。代替耗费时间的和频繁的拜访牙科医生，在消费者零售店购买牙齿增白剂，和可以容易地被整合到日常卫生计划中。家庭治疗方法包括增白条、研磨剂牙膏和那些包含过氧化物的牙膏。这些过氧化物牙膏要求使用双室系统，该系统分离过氧化物和其它成分。如果双室的内容物被过早地混合，则损失氧化作用活性和增白益处。
希望提供增白口腔护理组合物，该组合物促进消费者适应性和使用单腔室或管以递送足够的量的增白成分及其他口腔护理活性物而没有在成分之间的有害反应。
发明概述
本发明提供单相增白洁齿剂，该洁齿剂包括(i)选自过氧化氢、结合的(bound)过氧化物和固体过氧化物的增白剂(ii)研磨剂和(iii)基本上无水的口腔可接受的载体，例如聚乙二醇。该结合的过氧化物可以是过氧化氢和聚合物和/或任何过氧化物化合物和多孔的交联聚合物，如聚乙烯吡咯烷酮、聚丙烯酸酯、聚甲基丙烯酸酯和聚衣康酸酯的聚合物。该固体氢氧化物可以是过硼酸钠或氢氧化脲。
本发明还提供通过使表面与组合物接触来增白牙表面的方法。
发明的详细说明
本发明提供单相增白口腔护理组合物，包含过氧化物增白剂；过氧化物不相容的研磨剂；和基本上无水的口腔可接受的载体。在各种实施方案中，所用的基本上无水的口腔可接受的载体和特别的过氧化物允许得到储存稳定的单管口腔护理组合物，其中过氧化物和与过氧化物不相容的成分如研磨剂可以被组合。口腔护理组合物提供非常有效的增白和清洁效果。
单相口腔护理组合物具有“低水”含量，意思指水的总浓度，包括任何自由水分和在任何成分中包含的水，是小于约4％，约7％或小于约10％的水。增白剂连同低水载体的选择提供增白剂的稳定递送。增白活性得到保持以便施用到牙齿或口腔表面并在整个储存过程中得到保持。
可以使用在本领域中任何已知的或已开发的增白剂。优选地，增白剂包括固体增白剂和结合的增白剂，它们是基本上无水的产生氧的化合物。在本文中有用的固体增白剂包括过氧化物、金属亚氯酸盐、过硫酸盐。示例性的过氧化物相包括氢过氧化物、过氧化氢、碱金属和碱土金属的过氧化物、有机过氧化合物、过氧酸、它们的药用可接受的盐和它们的混合物。碱金属和碱土金属的过氧化物包括过氧化锂、过氧化钾、过氧化钠、过氧化镁、过氧化钙、过氧化钡、和其混合物。有机过氧化合物包括过氧化脲、甘油基过氧化氢、烷基过氧化氢、二烷基过氧化物、烷基过氧酸、过氧酯、二酰基过氧化物、过氧化苯甲酰、和单过氧酞酸盐和其混合物。过氧酸和它们的盐，包括有机过氧酸，如烷基过氧酸和单过氧邻苯二甲酸盐和其混合物，以及无机的过氧酸性盐如和碱金属和碱土金属(如锂、钾、钠、镁、钙、和钡)过硼酸盐，和其混合物。优选的固体过氧化物是过硼酸钠、过氧化脲和其混合物。合适的金属亚氯酸盐包括亚氯酸钙、亚氯酸钡、亚氯酸镁、亚氯酸锂、亚氯酸钠和亚氯酸钾。增白剂优选地可以是结合的。例如，过氧化物可以结合到聚合物如PVP(聚(N-乙烯基吡咯烷酮))。合适的PVP复合物在例如美国专利5122370中得到公开，该专利的内容在本文中被引入作为参考。在一些实施方案中，可以希望使用任何已知的除过碳酸钠和/或任何过碳酸盐之外的增白剂。
本发明的组合物可以包括任何牙齿研磨剂或在本领域中已知的或将被开发的牙齿研磨剂的组合。如本文中使用的“研磨剂”是指包括通常还称为“磨光剂”的材料。合适的研磨剂可以包括那些先前被认为在包含过氧化物的配方中是不相容的研磨剂(“过氧化物-不相容的研磨剂”)。这类研磨剂是，在含有过氧化氢的水溶液中，充分(substantially)与过氧化氢起化学反应以便降低溶液的增白功效的一种。
可以使用任何口腔可接受的研磨剂，但是优选地，应该选择研磨剂的类型、细度(粒度)和量以便牙齿釉质在正常使用组合物中不被过度地磨损。合适的研磨剂包括而不限于二氧化硅，例如硅胶、水合二氧化硅或沉淀二氧化硅的形式、氧化铝、不溶解的磷酸盐、碳酸钙、树脂的研磨剂如脲甲醛缩合物等等。在不溶解的磷酸盐中可用作为研磨剂是正磷酸盐、聚偏磷酸盐和焦磷酸盐。说明性实例是正磷酸二钙二水合物、焦磷酸钙、β-焦磷酸钙、磷酸三钙、聚偏磷酸钙和不溶解的聚偏磷酸钠。研磨剂，如果存在，其平均粒度通常为约0.1-约30μm、例如约1-约20μm或约5-约15μm。以有效研磨的总量存在一种或多种研磨剂，一般地约0.1％-约40％。
在本发明的各种实施方案中，口腔组合物包含抗牙垢剂。一般地，牙垢控制剂被分类为与一些增白剂不相容，但是本发明的实施方案在单相增白组合物中引入了牙垢控制剂和增白剂。合适的抗牙垢剂包括而不限于磷酸盐和多磷酸盐(例如焦磷酸盐)、聚氨基丙烷磺酸(AMPS)、六偏磷酸盐、柠檬酸锌三水合物、多肽、聚烯烃磺酸盐、聚烯烃磷酸盐、二膦酸盐。该抗牙垢剂以约0.1％-约30％存在。口腔组合物可以包括不同的抗牙垢剂的混合物。在一个优选的实施方案中，使用了焦磷酸四钠(TSPP)和三聚磷酸钠(STPP)。该抗牙垢剂包含约1％的TSPP和约7％-约10％的STPP。
该口腔护理组合物可以任选地包括至少一种口腔可接受的氟化物离子的源。可以使用在本领域中任何已知的或已开发的增白剂。合适的氟化物离子源包括氟化物、单氟磷酸盐、氟硅酸盐。一种或多种释放氟化物离子的化合物任选地以提供总共约100-约20,000ppm，约200-约5,000ppm，或约500-约2,500ppm的氟化物离子的量存在。
载体优选地为低水含量的口腔可接受的载体和可以包括任何已知的成分或添加剂。
在本发明的优选实施方案中，口腔组合物是洁齿剂。上述洁齿剂可以包括洗牙粉、牙齿片剂、牙膏(牙齿乳膏)、牙粉或凝胶或本领域技术人员已知的任何其它形式。
基本上无水的载体还可以包含各种的洁齿剂成分以调节组合物的流变学和感觉，如湿润剂、表面活性剂、增稠或胶凝剂等等。
本发明的组合物优选地包含表面活性剂。合适的表面活性剂包括而不限于C8-20烷基硫酸盐、C8-20脂肪酸的磺化单酸甘油酯、肌氨酸盐、牛磺酸盐、十二烷基硫酸钠、椰油基单酸甘油酯磺酸钠、月桂基肌氨酸钠、月桂基羟乙磺酸钠(sodium lauryl isoethionate)、月桂基聚氧乙烯醚羧酸钠和十二烷基苯磺酸钠和椰油酰胺基丙基甜菜碱的水溶性盐。
本发明的组合物任选地包含增稠剂。可以使用任何口腔可接受的增稠剂，包括而不限于卡波姆(亦称聚羧乙烯)，角叉菜胶(亦称爱尔兰藓)，和更特别地，ι-角叉菜胶(ι-角叉菜胶)、高分子量聚乙二醇(如可从DowChemical Company获得的)，纤维素的聚合物如羟乙基纤维素、羧甲基纤维素(CMC)和它们的盐，例如CMC钠、天然树胶如卡拉牙胶、黄原胶、阿拉伯树胶和黄蓍胶、胶态的硅酸铝镁和胶态的和/或火成二氧化硅和它们的混合物。一种或多种增稠剂任选地以约0.1％-约90％的总量存在，例如约1％-约50％或约5％-约35％。
在各种优选的实施方案中，载体可以包含聚乙二醇、环氧乙烷、环氧丙烷和硅氧烷的聚合物和/或共聚物。如果使用上述的共聚物/聚合物，它们可以选自市售可得的材料L4370和L1220(可以从美国密歇根州，BASF，Wyandotte获得)。优选地，一种或多种载体提供具有约10,000CPS-约700,000CPS的粘性的洁齿剂，优选地约30,000CPS-约300,000CPS。
如本领域的技术人员所认识，本发明的口腔组合物任选地包括其它材料，如，例如防龋剂、减感剂、粘度调节剂、稀释剂、表面活性试剂、如表面活性剂、乳化剂、和泡沫调节剂、pH改性剂、除上列的那些之外的研磨剂、湿润剂、口感剂、甜味剂、调味剂、着色剂、防腐剂和其组合。应当理解，虽然每一种上述种类的材料的一般属性可能不同，但是在两种或更多种这些类型的材料之间会有一些其同的属性并且任何给定材料可以服务于多重目的。优选地，为了与组合物的其它成分的相容性而选择载体。
如果需要，在组合物中可以包括香料、甜味剂、着色剂、泡沫调节剂、口感剂及其他添加剂。
本发明的组合物任选地包含一种或多种其他活性物质，它们对于预防或治疗口腔的硬或软组织的病症或失调、预防或治疗生理失调或病症，或提供化妆益处是切实可行的。
组合物可以包括亚锡离子或亚锡离子源。合适的亚锡离子源包括而不限于氟化亚锡，其他的亚锡卤化物如氯化亚锡二水合物、焦磷酸亚锡、有机亚锡羧酸盐如亚锡的甲酸盐、乙酸盐、葡糖酸盐、乳酸盐、酒石酸盐、乙二酸盐、丙二酸盐、和柠檬酸盐，亚锡的乙烯果绿定(glyoxide)等等。一种或多种亚锡离子源任选地和说明性地以约0.01％-约10％的总量存在，例如约0.1％-约7％或约1％-约5％。
本发明的组合物任选地包含抗微生物剂(例如，抗菌剂)。有用的抗菌剂的进一步例证性列表被提供于如列在授予Gaffar等人的美国专利5776435中的那些，该专利的内容在本文中被编入作为参考。一种或多种抗微生物剂任选地以抗微生物有效的总量存在，一般地约0.05％-约10％，例如约0.1％-约3％。
本发明的组合物任选地包含抗氧化剂。可以使用任何口腔可接受的抗氧化剂，包括丁羟基茴香醚(BHA)、丁基羟基甲苯(BHT)、维生素A、类胡萝卜素、维生素E、类黄酮、多酚、抗坏血酸、草本抗氧化剂、叶绿素、褪黑激素和其混合物。
本发明的组合物任选地包含催涎剂或唾液刺激剂，抗牙斑剂、消炎剂、脱敏剂。
提供了增白人类或动物受试者的口腔表面的方法，包含将包含过氧化物增白剂、与过氧化物不相容的研磨剂和基本上无水的和基本上无水的口腔可接受的载体的增白口腔护理组合物以稳定形式贮存；使所述组合物与口腔的表面接触。如在本文中使用的“动物受试者”包括较高级的非人类哺乳动物如犬科、猫科和马科。口腔护理组合物与哺乳动物受试者的口腔表面接触以由此非常有效地增白牙齿，而在增白剂、与过氧化物不相容的研磨剂及其他成分之间没有任何负相互作用。
在各种实施方案中，优选地，施用口腔护理组合物和使其与口腔表面接触。根据本发明制备的洁齿剂优选地被定期地施加到口腔表面，优选基于每天，至少每天一次持续多天，但是交替地每隔两或三天。优选地，口腔的组合物被施加到口腔表面每天1-3次，持续至少2星期至8星期、4个月-3年、或更多至一生。
在下面非限制性实施例中说明本发明。
实施例
对比实施例I
通过混合表1中的成分制备了对比的不含有研磨剂的单相洁齿剂。在大约49℃下老化洁齿剂两星期后，过氧化物回收(recovery)为最初存在量的89％。
表1
实施例1
通过混合表2中的成分制备了单相洁齿剂。包括12.44％的与过氧化物不相容的二氧化硅研磨剂且该研磨剂提高了洁齿剂的清洁和增白益处。在大约49℃下老化洁齿剂两星期后，过氧化物回收为最初存在量的77％。
表2
在本文中描述的实施例及其他实施方案是示范性的且不旨在限制描述本发明的组合物和方法的整个范围。在本发明范围肉可以进行特定的实施方案、材料、组合物和方法的等价改变、修改和变化，得到基本上相似的结果。

Claims (16)

1. 单相口腔护理组合物，所述组合物包含：
过氧化物增白剂，所述过氧化物增白剂包含过氧化氢和交联的聚乙烯基吡咯烷酮的复合物；
研磨剂，所述研磨剂选自二氧化硅、焦磷酸钙、碳酸钙和磷酸二钙；
抗牙垢剂；和
基本无水的载体，所述载体包含环氧乙烷和环氧丙烷的共聚物。
2. 权利要求1的组合物，其中所述研磨剂为碳酸钙。
3. 权利要求1的组合物，其中所述抗牙垢剂包含选自多磷酸盐、六偏磷酸盐、聚烯烃磺酸盐及其两种或多种的组合的药物。
4. 权利要求1的组合物，其中所述载体的总水含量小于约4%重量。
5. 权利要求1的组合物，其中所述组合物为洁齿剂。
6. 权利要求1的组合物，其中所述研磨剂为焦磷酸钙。
7. 权利要求1的组合物，其中所述研磨剂为磷酸二钙。
8. 权利要求2的组合物，其中所述抗牙垢剂包含选自多磷酸盐、六偏磷酸盐、聚烯烃磺酸盐及其两种或多种的组合的药物。
9. 权利要求6的组合物，其中所述抗牙垢剂包含选自多磷酸盐、六偏磷酸盐、聚烯烃磺酸盐及其两种或多种的组合的药物。
10. 权利要求7的组合物，其中所述抗牙垢剂包含选自多磷酸盐、六偏磷酸盐、聚烯烃磺酸盐及其两种或多种的组合的药物。
11. 权利要求8的组合物，其中所述载体的总水含量小于约4%重量。
12. 权利要求9的组合物，其中所述载体的总水含量小于约4%重量。
13. 权利要求10的组合物，其中所述载体的总水含量小于约4%重量。
14. 权利要求11的组合物，其中所述组合物还包含十二烷基硫酸钠和氟化物离子的源。
15. 权利要求12的组合物，其中所述组合物还包含十二烷基硫酸钠和氟化物离子的源。
16. 权利要求13的组合物，其中所述组合物还包含十二烷基硫酸钠和氟化物离子的源。
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