CN105792805A - 含有脂肪两亲物的口腔护理增白组合物 - Google Patents
含有脂肪两亲物的口腔护理增白组合物 Download PDFInfo
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- CN105792805A CN105792805A CN201380081340.5A CN201380081340A CN105792805A CN 105792805 A CN105792805 A CN 105792805A CN 201380081340 A CN201380081340 A CN 201380081340A CN 105792805 A CN105792805 A CN 105792805A
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Abstract
本文描述了口腔护理组合物,所述口腔护理组合物包含与过氧化氢复合的交联聚乙烯吡咯烷酮,以及脂肪两亲物,包括了还包含钙研磨剂的一些实施方案。
Description
背景
包含过氧化物的洁齿剂制剂是已知的并且可用于清洁和增白牙齿。过氧化物可漂白牙齿,除去污渍并杀死生龋齿的细菌。然而,过氧化物化合物具有高度反应性,因此难以配制。此外,过氧化氢可自发地分解形成氧气(O2)和水,以致于在储藏时,洁齿剂容器可能膨胀、破裂或渗漏,并且剩余制剂将不具有足以有效清洁和增白牙齿的过氧化物剩余物。一些洁齿剂最初包含非常高水平的随时间进行分解的过氧化物,以致于递送在应用上的过氧化物的精确量是可变的并且主要取决于洁齿剂已储存多长时间和处于什么条件下。
为了解决H2O2稳定性问题,已使用利用了稳定化的H2O2的改进洁齿剂,所述洁齿剂包含与聚乙烯吡咯烷酮(PVP)复合的H2O2。当在口腔中时,通过暴露于水性环境,PVP-H2O2解离成单独物质(PVP聚合物和H2O2)。PVP-H2O2复合物通常由约80重量%聚乙烯吡咯烷酮和20重量%H2O2组成。PVP-H2O2复合物和/或包含PVP-H2O2的单相增白洁齿剂组合物描述于例如WO/2007/037961、美国公布号US2007-0071695A1、美国公布号US2012-0058059A1和美国公布号5,122,370中,所述专利的内容以引用的方式并入本文。
相分离是含有过氧化物的凝胶洁齿剂的重大挑战。膨胀也是含有过氧化物的凝胶洁齿剂的一个问题。
因此,对长期储存稳定并适于消费者每天使用的改进的过氧化物洁齿剂制剂存在需要。
概述
在一些实施方案中,本发明提供了为可由消费者从单腔管中轻易地分配的单相洁齿剂的口腔护理组合物。在一些实施方案中,口腔护理组合物在长期储存过程中是稳定的并且保持有效地清洁和增白牙齿。在一些实施方案中,本发明提供了一种口腔护理组合物,所述组合物包含:(i)与过氧化氢复合的交联聚乙烯吡咯烷酮和(ii)脂肪两亲物。在一些实施方案中,脂肪两亲物为硬脂醇、鲸蜡醇或两者组合
根据以下详细说明和实施例,本发明的另外实施方案将是清楚的。
详述
通篇使用的范围用作描述范围内的每个值的简略表达方式。范围内的任何值可选为范围终点。除非另外规定,否则本文和在本说明书中其他处表达的所有百分比和量应理解为是指重量百分比。除非另外特别说明,否则本文表达的所有百分比是基于干燥物质重量的
本文中引用的所有参考文献均在此以引用的方式整体并入。
如果本公开中的定义和所引用参考文献的定义发生冲突,则以本公开为准。
在一些实施方案中,本发明提供了口腔护理组合物和用于向人或其他动物受试者施用或应用的方法。如本文所提及的,“口腔护理组合物”是适于向人或动物受试者的口腔施用或应用以增进受试者的健康、卫生或外貌的任何组合物。在一些实施方案中,口腔护理组合物在口腔中保持足以影响预期效用的时间。
在一些实施方案中,口腔护理组合物是洁齿剂。作为实例而不是限制,本描述通篇使用的术语“洁齿剂”表示糊剂、凝胶、牙粉、牙用片剂或液体制剂。在一些实施方案中,洁齿剂具有深条纹、浅条纹或多层化、在糊剂周围具有凝胶。在一些实施方案中,组合物与带、托盘、口腔件或类似器具一起使用。在优选的实施方案中,口腔组合物为单相牙膏或凝胶。
如本文所用,短语“不可接受的相分离水平”意指在储存24小时后可通过肉眼观察到的相分离
在一些实施方案中,本发明提供了包含以下的口腔护理组合物:(i)与过氧化氢复合的交联聚乙烯吡咯烷酮,(ii)脂肪两亲物和(iii)载体,所述载体包括具有大于1000Da的平均分子量的环氧乙烷/环氧丙烷共聚物。
在一些实施方案中,本发明提供了包含以下的口腔护理组合物:(i)与过氧化氢复合的交联聚乙烯吡咯烷酮,(ii)脂肪两亲物和(iii)载体,所述载体包括(a)具有大于5000Da的平均分子量、具有式(环氧乙烷)x-(环氧丙烷)y的环氧乙烷/环氧丙烷嵌段共聚物,其中x为80-150的整数并且y为30-80之间的整数,和(b)研磨剂。在一些实施方案中,研磨剂为钙研磨剂。在一些实施方案中,组合物还包含表面活性剂。在一些实施方案中,所述组合物还包含湿润剂。在一些实施方案中,所述组合物还包含溶剂。在其他实施方案中,本发明提供了不含研磨剂的凝胶。
例如,本发明提供了组合物1牙膏,其包含(i)包含与过氧化氢复合的交联聚乙烯吡咯烷酮的增白复合物,(ii)脂肪两亲物,例如,
1.1.组合物1,其中增白复合物含有约10-30重量%,例如15-25重量%,例如约17-22重量%的过氧化氢和约5-15重量%,例如约7-12重量%的总氮;例如,与例如购自InternationalSpecialtyProducts(Wayne,NJ)的XL-10例如XL-10F具有基本上相同的规格;
1.2.组合物1或1.1,其中脂肪两亲物选自C12至C28脂肪醇或其混合物
1.3.组合物1或1.1或1.2,其中脂肪两亲物为硬脂醇;
1.4.组合物1或1.1,其中脂肪两亲物为鲸蜡醇或鲸蜡醇和硬脂醇的组合;
1.5.任一前述组合物,其中脂肪两亲物的量占组合物的约0.05重量%至约30重量%、或约0.1重量%至约20重量%、或约0.5重量%至约10重量%;
1.6.任一前述组合物,其还包含钙研磨剂诸如碳酸钙或焦磷酸钙;
1.7.任一前述组合物,其中过氧化氢的总量占组合物的0.5-5重量%,例如0.75-3重量%,例如约1重量%;
1.8.任一前述组合物,其含有小于10的水,例如小于2%的水,或小于1%的水,例如基本上无水;
1.9.任一前述组合物,其还包含选自以下的聚合物增稠剂:(i)聚乙二醇,(ii)具有至少1000分子量的聚乙二醇-聚丙二醇共聚物,和(iii)其组合;
1.10.前述组合物,其包含具有大于1000,例如5000-13000Da,例如约9800的平均分子量的环氧乙烷/环氧丙烷共聚物;
1.11.前述组合物,其还包含400至800,例如约600Da平均分子量的聚乙二醇;
1.12.任一前述组合物,其还包含例如选自甘油、丙二醇或其组合的润湿剂;
1.13.任一前述组合物,其还包含例如选自焦磷酸四钠(TSPP)和三聚磷酸钠(STPP)的牙垢控制剂;
1.14.任一前述组合物,其还包含表面活性剂例如月桂基硫酸钠(SLS);
1.15.任一前述组合物,其还包含抗菌剂例如三氯生;
1.16.任一前述组合物,其还包含抗氧化剂例如丁基化羟基甲苯(BHT);
1.17.任一前述组合物,其还包含氟化物离子源,诸如氟化钠或单氟磷酸钠;
1.18.任一前述组合物,其包含以下成分种类和/或按重量计的特定成分中的任一种或全部:
溶剂
1.19.组合物,其来源于前述成分的组合。
在一些实施方案中,本发明提供了口腔护理组合物,所述组合物包含:与过氧化氢复合的交联聚乙烯吡咯烷酮、脂肪两亲物、溶剂、聚合物增稠剂和研磨剂及湿润剂。
一些实施方案提供了口腔护理组合物,所述组合物包含:约0.5至约22重量%的与过氧化氢复合的交联聚乙烯吡咯烷酮。其他实施方案提供了包含约1至约15重量%的与过氧化氢复合的交联聚乙烯吡咯烷酮的口腔护理组合物。其他实施方案提供了包含约3至约15重量%的与过氧化氢复合的交联聚乙烯吡咯烷酮的口腔护理组合物。其他实施方案提供了包含约4至约12重量%的与过氧化氢复合的交联聚乙烯吡咯烷酮的口腔护理组合物。而其他实施方案提供了包含约5至约11重量%的与过氧化氢复合的交联聚乙烯吡咯烷酮的口腔护理组合物。在一些实施方案中,口腔护理组合物包含约5重量%、6重量%、7重量%、8重量%、8重量%、9重量%、10重量%、11重量%或12重量%的与过氧化氢复合的交联聚乙烯吡咯烷酮。在一些实施方案中,口腔护理组合物包含5.5重量%的与过氧化氢复合的交联聚乙烯吡咯烷酮。
本发明的组合物包含至少一种脂肪两亲物。如本文所用,“脂肪两亲物”是指具有如以下定义的R1疏水尾基和使化合物不可水溶的(不混溶的)亲水头基的化合物,其中化合物还在口腔组合物的pH下具有净中性电荷。如本文所用,术语“可水溶的”意指本发明的组合物中的材料可溶于水中。一般来讲,材料应该在25℃下以水溶剂的0.1重量%、优选1重量%、更优选5重量%、更优选15重量%的浓度溶解。
本发明的脂肪两亲物可表征为具有6或更小亲水-亲脂平衡(“HLB”)的化合物。如本文所用,HLB为根据Griffin,J.Soc.Cosm.Chem.,第5卷,249(1954)的标准HLB。如果使用脂肪两亲物的混合物,则期望混合物具有约1至约6且优选约1至约3的HLB。因此,如果与具有更低HLB的另一脂肪两亲物混合,则可使用具有6以上HLB的脂肪两亲物。
本发明的口腔组合物包含的脂肪两亲物的量占最终口腔组合物的约0.05重量%至约30重量%,优选约0.1重量%至约20重量%,更优选约0.5重量%至约10重量%。在一些实例中,最终口腔组合物中的脂肪两亲物的量为约2%至约8%并且更优选约4%至约6%。
根据本发明,合适的脂肪两亲物或两种或更多种脂肪两亲物的合适混合物优选具有至少约40℃的熔点。在一些实施方案中,优选的熔点为至少约50℃,或大于约55℃,或大于约60℃。如本文所用,熔点可通过标准熔点方法来测得,如U.S.Pharmacopeia,USP-NFGeneralChapter741“Meltingrangeortemperature”中所述。两种或更多种材料的混合物的熔点通过以下方式测定:在相应的熔点以上的温度下混合两种或更多种材料,然后使混合物冷却。如果所得复合材料在约45℃下为均质固体,那么混合物具有适合用于本发明的熔点。其中混合物包含具有小于约45℃的单独熔点的至少一种脂肪两亲物的两种或更多种脂肪两亲物的混合物也适于本发明中,前提条件是混合物的复合熔点为至少约45℃。
根据本发明,合适的脂肪两亲物具有R1疏水尾基。如本文所用,R1为烷基、烯基(含有多至3个双键)、烷基芳族、C12-C70长度的支链烷基。适于本发明的脂肪两亲物的烷基、烯基或支链烷基的非限制实例包括月桂基、十三烷基、十四烷基、十五烷基、鲸蜡基、十七烷基、硬脂基、花生基(arachidyl)、山俞基、十一烯基、棕榈酸基(palmitoleyl)、油烯基、棕榈基(palmoleyl)、亚油烯基、亚麻基、花生四烯基(arahchidonyl)、反油基、桐基(elaeostearyl)、瓢儿菜基(erucyl)、异月桂基、异十三烷基、异十四烷基、异十五烷基、岩芹基、异鲸蜡基、异十七烷基、异硬脂基、异花生基、异山俞基、鳕烯基、巴西烯基(brassidyl)以及其工业级混合物。如本文所用,R1还可以是通过醇的碱性缩合获得更高分子量的支链异醇而制备的支链烷基。这些支链异醇在本领域称为Guerbet醇。R1可以是植物来源的烷基、烯基或支链的碳链,所述植物来源为诸如小麦胚、向日葵、葡萄籽、芝麻、玉米、杏、蓖麻、鳄梨、橄榄、大豆、甜扁桃、棕榈、油菜籽、棉花籽、榛果、澳洲坚果、烛果油、荷荷巴油、苜蓿、罂粟、南瓜籽、芝麻、黄瓜、黑醋栗、月见草、小米、大麦、奎藜籽、黑麦、红花、桐树、西番莲或麝香玫瑰油和烛果油。
本发明的合适的脂肪两亲物还具有使化合物不可水溶的亲水头基,所述亲水头基诸如在具有6或更小HLB的化合物中。具有所述亲水头基的化合物种类的非限制性实例包括脂肪醇、烷氧基化脂肪醇、脂肪酚、烷氧基化脂肪酚、脂肪酰胺、烷氧基化脂肪酰胺、脂肪胺、脂肪烷基酰氨基烷基胺、脂肪烷氧基化胺、脂肪氨基甲酸酯、脂肪胺氧化物、脂肪酸、烷氧基化脂肪酸、脂肪二酯、脂肪脱水山梨糖醇酯、脂肪糖酯、甲基葡糖苷酯、脂肪乙二醇酯、单甘油酯、二甘油酯和三甘油酯、聚甘油脂肪酯、烷基甘油醚、丙二醇脂肪酸酯、胆固醇、神经酰胺、脂肪硅氧烷蜡、脂肪葡糖酰胺以及磷脂。
本发明的脂肪两亲物还可以选自脂肪醇化合物或根据下式的烷氧基化脂肪醇醚:
R1-(OR2)k-OH
其中R1如上所述;R2为可以是支链的或羟基取代的C1-C5碳链;并且k是约0至约5范围内的数。可用于本文的脂肪醇是那些具有约12至约60个碳原子,优选约16至约60个碳原子的那些。这些脂肪醇可以是直链或支链的醇并且可以是饱和或不饱和的。合适的脂肪醇的非限制性实例包括鲸蜡醇、硬脂醇、花生醇、山俞醇、二十烷醇(eicosylalcohol)、C20-40醇、C30-50醇、C40-60醇及其混合物。合适的烷氧基化脂肪醇醚包括1至5mol环氧乙烷与具有约12至约60个碳原子的线性脂肪醇的加成产物,其是通过已知的工业乙氧基化方法可获得的所有加合物。另外合适的是烷基酚的聚环氧乙烷缩合物,例如具有含有约12至约60个碳原子、呈直链或支链构造的烷基的烷基酚与环氧乙烷的缩合产物,其中环氧乙烷的存在量等于约1至约5摩尔的环氧乙烷/摩尔烷基酚。另外合适的烷氧基化脂肪醇醚包括源自环氧乙烷与由环氧丙烷和乙二胺产物的反应产生的产物缩合的那些。合适的烷氧基化脂肪醇醚的非限制性实例包括硬脂醇聚醚-2、山嵛醇聚醚-2、山嵛醇聚醚-5、山嵛醇聚醚-10、C20-40链烷醇聚醚-3、C20-40链烷醇聚醚-10、C30-50链烷醇聚醚-3和C30-50链烷醇聚醚-10。在一个实施方案中,优选脂肪醇的组合诸如鲸蜡醇和硬脂醇。鲸蜡醇对硬脂醇的比可为约4∶1至约1∶4,优选约2∶1至约1∶2,并且在一些实施方案中为1∶1。本发明的脂肪两亲物还可选自二脂肪酯、脂肪酰胺,包括脂肪烷醇酰胺和脂肪烷氧基化酰胺、脂肪氨基甲酸酯、脂肪烷基酰氨基烷基胺、脂肪胺,包括脂肪链烷醇胺和脂肪烷氧基化胺、脂肪胺氧化物、脂肪酸或烷氧基化脂肪酸、脂肪酯、脂肪磷化合物、脂肪脱水山梨糖醇衍生物、糖聚酯、烷基亚砜以及其组合。
本发明的组合物可包含表面活性剂(surfaceactiveagent)(表面活性剂(surfactant))。合适的表面活性剂包括阴离子型、两性离子型、两性型、阳离子型和非离子型表面活性剂。表面活性剂可以是多于一种类型的表面活性剂(诸如阴离子型和非离子型表面活性剂)的组合。表面活性剂通常是可水溶的或可混溶于溶剂或口腔载体中。在一个实施方案中,优选阴离子型表面活性剂诸如月桂基硫酸钠。合适的表面活性剂包括但不限于C8-20烷基硫酸盐的水溶性盐、C8-20脂肪酸的磺化单甘油酯、肌氨酸盐、牛磺酸盐、月桂基硫酸钠(SLS)、椰油基单甘油酯磺酸钠、月桂基肌氨酸钠、月桂基羟乙磺酸钠(sodiumlaurylisoethionate)、月桂醇聚氧乙烯醚羧酸钠(sodiumlaurethcarboxylate)和十二烷基苯磺酸钠以及椰油酰胺基丙基甜菜碱。表面活性剂的存在量通常占口腔组合物的约0.01重量%至约15重量%,在另一实施方案中约0.1重量%至约10重量%,并且在另一实施方案中约0.3重量%至约5重量%。在一些实施方案中,利用了表面活性剂于水中的稀释溶液。在一个实施方案中,基于口服组合物中所需的发泡水平和由表面活性剂导致的刺激来选择表面活性剂的量。
在一些实施方案中,本发明的组合物还包含溶剂,诸如水或其他合适溶剂诸如湿润剂。本发明的合适溶剂包括水、可食用多元醇诸如甘油、二甘油、三甘油、山梨醇、木糖醇、丁二醇、赤藓醇、聚乙二醇、丙二醇及其组合。山梨醇、甘油及其组合为优选溶剂
按口腔组合物的重量计,口腔组合物可包含至少约0.05%的溶剂。口腔组合物中溶剂的存在量可为约0.1%至约99%、约0.5%至约95%和约1%至约90%。
如果口腔组合物的粘度太低(稀薄或粘性较小),则组合物不适于用作牙膏;相反地,如果粘度太高(稠的或粘性较大),则组合物也不适于用作牙膏。本发明的组合物通常具有的pH为约5至约9,更具体约6至约8,并且更具体约7。
本发明的组合物还通常包含口腔可接受的载体或媒介物。载体可包括研磨剂、增稠剂、湿润剂、其他聚合物、着色剂、粘度调节剂、泡沫调节剂、乳化剂、pH改性剂、稀释剂、口感剂、甜味剂、调味剂、防腐剂、合适的美容和/或治疗活性剂,及其组合。应当理解,虽然以上的材料类别中的每种的一般属性可能不同,但是可存在一些共同属性并且任何给定材料可在两种或更多种所述材料类别内起多种用途。组合物中的所有成分可具有除其主要功能之外的功能,并且可有助于组合物的总体特性,包括其稳定性、功效、稠度、口感、味道、气味等等。优选地,针对与组合物的其他成分的相容性来选择载体。
活性剂包括通常被认为安全用于口腔中的任何材料,可操作所述材料以预防或治疗口腔硬组织或软组织的病状或病症;预防或治疗生理病症或病状;或提供美容益处,改善口腔的总体外貌和/或健康改善。活性剂的实例包括但不限于抗牙结石剂、氟化物离子源、亚锡离子源、其他增白剂、抗微生物剂、消臭剂、脱敏剂、抗侵蚀剂、防龋剂、防斑剂、消炎剂、唾液刺激剂、营养素、抗氧化剂、抗病毒剂、镇痛剂和麻醉剂、H-2拮抗剂及其混合物。当存在时,以口腔护理组合物的重量计,口腔护理组合物中的美容和/或治疗活性剂的水平在一个实施方案中为约0.001%至约90%,在另一实施方案中为约0.01%至约50%,并且在另一实施方案中为约0.1%至约30%。
已发现,不一定需要另外的线性和/或交联聚乙烯吡咯烷酮,即除了为PVP-H2O2复合物的一部分的PVP之外来提供稳定或单相的组合物。然而,在一些实施方案中,可添加约1至约15重量%的另外的线性和/或交联聚乙烯吡咯烷酮。
本发明的一些实施方案提供了还包含钙研磨剂的凝胶基过氧化物口腔组合物。在一些实施方案中,组合物包含约9至约25重量%的丙二醇。在一些实施方案中,组合物包含约14至约32重量%的甘油。在其他实施方案中,组合物包含小于20重量%的钙研磨剂。一些实施方案提供了包含以下的组合物:约9至约25重量%丙二醇;约14至约32重量%甘油;和小于20重量%的钙研磨剂。
其他实施方案提供了包含约20至约60重量%的湿润剂的口腔护理组合物。
其他实施方案提供了包含约5至约15重量%的研磨剂的口腔护理组合物。
本发明的组合物是“低水”含量的,意指水(包括任何游离水和含在任何成分中的所有水)的总浓度小于约20%总水、小于约10%总水,在另一实施方案中小于约5%,在另一实施方案中小于3%,在另一实施方案中小于2%水,在另一实施方案中小于1%水,即是无水的。
当存在研磨剂时,平均粒度通常为约0.1至约30微米,例如约1至约20或约5至约15微米。
在本发明中的各种实施方案中,口腔组合物包含抗牙结石(牙垢控制)剂。一般来讲,牙垢控制剂按与一些增白剂不相容来分类,但是本发明的一些实施方案在单相增白组合物中结合了牙垢控制剂和增白剂。合适的抗牙结石剂包括但不限于磷酸盐和聚磷酸盐(例如焦磷酸盐)、聚氨基丙磺酸(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、二磷酸盐。抗牙结石剂以约0.1%至约30%存在。口腔组合物可包含不同的抗牙结石剂的混合物。在一个优选实施方案中,使用了焦磷酸四钠(TSPP)和三聚磷酸钠(STPP)。在一个实施方案中,抗牙结石剂包含约1-2%的TSPP和约7%至约10%的STPP。
口腔护理组合物可任选地包含至少一种口腔可接受的氟化物离子源。可使用本领域任何已知或待开发的,例如可溶性氟化物盐。可采用多种多样的氟化物离子-产生材料作为本发明组合物中的可溶性氟化物源。合适的氟化物离子产生材料的实例可见于授予Briner等的美国专利号3,535,421;授予Parran,Jr.等的美国专利号4,885,155,和授予Widder等的美国专利号3,678,154,所述专利以引用的方式并入本文。代表性的氟化物离子源包括但不限于氟化亚锡、氟化钠、氟化钾、单氟磷酸钠、氟硅酸钠、氟硅酸铵、氟化胺、氟化铵及其组合。在某些实施方案中,氟化物离子源包括氟化亚锡、氟化钠、单氟磷酸钠及其混合物。在某些实施方案中,本发明的口腔护理组合物还可含有氟化物离子源或提供氟的成分,所述提供氟的成分的量足以提供约25ppm至约25,000ppm的氟化物离子,通常至少约500ppm,例如,约500至约2000ppm,例如约1000至约1600ppm,例如约1450ppm。氟化物的适当水平将取决于具体应用。一般消费者使用的牙膏通常具有约1000至约1500ppm,而儿童牙膏具有的稍微少点。在其他实施方案中,氟化物的水平为约100至约20,000ppm、约200至约5,000ppm,或约500至约2,500ppm氟化物离子。用于专业应用的洁齿剂或涂层可具有多达约5,000或甚至约25,000ppm的氟化物。以组合物的重量计,可添加到本发明的组合物的氟化物离子源的水平在一个实施方案中为约0.01重量%至约10重量%或约0.03重量%至约5重量%,并且在另一实施方案中为约0.1重量%至约1重量%。提供适当的氟化物离子水平的氟化物盐的重量将基于盐中的平衡离子的重量进行明显改变。
本发明的组合物还可包含各种洁齿剂成分诸如湿润剂、表面活性剂、增稠剂或胶凝剂等以调整组合物的流变特性和感觉。
本发明的组合物任选地包含增稠剂。可使用任何口腔可接受的增稠剂,包括但不限于卡波姆(也称为羧乙烯基聚合物)、角叉菜胶(也称为爱尔兰藓)且更具体地角叉菜胶(ι-角叉菜胶)、高分子量聚乙二醇(诸如从DowChemicalCompany购得的)、纤维素聚合物(诸如羟乙基纤维素、羧甲基纤维素(CMC)及其盐例如CMC钠)、天然树胶诸如刺梧桐胶、黄原胶、***胶和黄蓍胶、胶体硅酸铝镁,和胶体二氧化硅和/或气相二氧化硅及其混合物。一种或多种增稠剂任选的存在总量为约0.1%至约90%,例如约1%至约50%或约5%至约35%。
在各种优选实施方案中,载体可包含聚乙二醇、环氧乙烷/环氧丙烷和硅酮的聚合物和/或共聚物。若使用这些共聚物/聚合物,则它们可选自可商购获得的材料。环氧乙烷/环氧丙烷的嵌段共聚物是可用的,但是优选较高分子量例如>1000Da,例如包括L1220(可购自BASF,Wyandotte,Mich.,美国)。还可用低或中分子量的聚乙二醇,例如PEG400、PEG600、PEG800、PEG1000及其混合物。
组合物可包含亚锡离子或亚锡离子源。合适的亚锡离子源包括但不限于氟化亚锡、其他卤化亚锡诸如二水二氯化锡、焦磷酸亚锡、有机亚锡羧酸盐诸如甲酸亚锡、乙酸亚锡、葡萄糖酸亚锡、乳酸亚锡、酒石酸亚锡、草酸亚锡、丙二酸亚锡和柠檬酸亚锡、亚锡亚乙基果绿定(stannousethyleneglyoxide)等等。一种或多种亚锡离子源任选和例示性的存在总量为约0.01%至约10%,例如约0.1%至约7%或约1%至约5%。
本发明的组合物任选地包含抗微生物(例如抗菌)剂。可用的抗菌剂的另一示例性列表提供于诸如授予Gaffar等的美国专利号5,776,435中所列出的那些中,所述专利内容以引用的方式并入本文。一种或多种抗微生物剂任选存在的抗菌有效总量通常为约0.05%至约10%,例如约0.1%至约3%。
本发明的组合物任选地包含抗氧化剂。可使用任何口腔可接受的抗氧化剂,包括丁基化羟基苯甲醚(BHA)、丁基化羟基甲苯(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、褪黑激素及其混合物。
提供了用于增白人或动物受试者中的口腔表面的方法,所述方法包括以稳定形式储存本发明的组合物,例如,如上所述的组合物1以及下列等等,以及使所述组合物与口腔表面接触。如本文所用的“动物受试者”包括较高级的非人哺乳动物诸如犬科动物、猫科动物和马。口腔护理组合物与哺乳动物受试者的口腔表面接触,以由此以高度有效的方式增白牙齿,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,优选的是,应用口腔护理组合物并使其与口腔表面接触。根据本发明制备的洁齿剂优选定期向口腔表面应用,优选基于每天,每天至少一次持续多天,但是交替地每隔两天或三天。优选地,每天向口腔表面应用口腔组合物1至3次,持续至少2星期至8星期、4个月至3年、或更多至一生。
在一些实施方案中,在室温下储存24小时之后,本发明的组合物未表现出不可接受的相分离水平。在其他实施方案中,在室温下储存48小时、72小时、200小时、1周、1个月、3个月或6个月之后,本发明的组合物未表现出不可接受的相分离水平。
在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的0.01%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的0.05%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的0.1%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的0.5%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的1%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的3%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的5%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的10%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的15%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的20%。
在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的25%。在其他实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的30%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的35%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的40%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的45%。在一些实施方案中,在于60℃下老化1周之后,本发明的组合物包装于其中的管的顶部直径伸展小于管的顶部直径的50%。
在下面非限制性实施例中说明本发明。
实施例
实施例1
凝胶洁齿剂的制备
1.将BHT溶解于调味剂中
2.将PluorocareL1220和丙二醇液体添加到不锈钢容器中
3.称重糖精钠、三氯蔗糖、单氟磷酸钠、TSPP和SLS,并将其放入来自步骤2的液体中
4.将所得混合物加热到75℃以上
5.在75℃以上将硬脂醇或鲸蜡醇(如果需要)融化到另一烧瓶中
6.称重来自步骤5的热脂肪醇并且快速倒进来自步骤4的混合物中
7.将所得混合物持续搅拌15分钟,停止加热,转移到罗斯罐(rosspot)中
8.将Ca2P2O7添加到罗斯罐
9.全速搅拌混合物并且在罗斯罐中施加全真空直到混合物达到室温(约30分钟)。
10.添加交联的PVP/H2O2和来自步骤1的调味剂/BHT,搅拌并施加全真空10分钟
11.将最终产品转入密封的玻璃容器中。
实施例2
制备了具有约2%的过氧化物组合物的凝胶洁齿剂,其具有表1中的成分。
表1
成分 | %(w/w) |
丙二醇 | 53.51 |
PEG118/PPG66共聚物(Plurocare L1220) | 7.5 |
交联的聚乙烯吡咯烷酮-过氧化氢 | 11 |
糖精钠 | 0.6 |
三氯蔗糖 | 0.05 |
单氟磷酸钠 | 0.76 |
TSPP | 0.3 |
BHT | 0.03 |
调味剂 | 2.25 |
月桂基硫酸钠 | 2 |
硬脂醇 | 7 |
鲸蜡醇 | 0 |
Ca2P2O7 | 15 |
总计 | 100 |
实施例3
制备了具有约2%的过氧化物组合物的凝胶洁齿剂,其具有表2中的成分。
表2
实施例4
制备了具有约2%的过氧化物含量的牙膏,其具有表3中的成分。
表3
实施例5
物理分离:测试实施例2-4的牙膏保持为单相的稳定性。将样品储存在室温下24并且针对可见的相分离进行检查。分别含有硬脂醇和鲸蜡醇的实施例2和3是稳定的,因为没有观察到相分离。实施例4不稳定的,因为观察到分离成两个不同的相。
实施例中所述的数据证明了通过本发明的组合物所展示的化学和物理稳定性的意料不到的改进。
虽然已说明和描述了本发明的具体实施方案,但本领域技术人员将清楚,可在不脱离本发明的精神和范围的情况下做出各种变化和修改。因此,在所附权利要求书中意图涵盖处于本发明范围内的所有此类变化和修改。
Claims (20)
1.一种洁齿剂组合物,其包含(i)包含与过氧化氢复合的交联聚乙烯吡咯烷酮的增白复合物,(ii)脂肪两亲物。
2.如权利要求1所述的组合物,其中所述脂肪两亲物选自C12至C28脂肪醇或其混合物。
3.如权利要求1或权利要求2所述的组合物,其中所述脂肪两亲物为硬脂醇。
4.如前述权利要求中任一项所述的组合物,其中所述脂肪两亲物为所述组合物的约0.1至约20重量%的量的硬脂醇、鲸蜡醇或其组合。
5.如前述权利要求中任一项所述的组合物,其包含平均分子量大于1000Da的环氧乙烷/环氧丙烷共聚物,基本上不含平均分子量小于1000Da的环氧乙烷/环氧丙烷嵌段共聚物。
6.如权利要求5所述的组合物,其中所述环氧乙烷/环氧丙烷共聚物具有在5000Da与13000Da之间的平均分子量。
7.如前述权利要求中任一项所述的组合物,其中所述增白复合物含有约10-30重量%的过氧化氢和约5-15重量%的总氮。
8.如前述权利要求中任一项所述的组合物,其中过氧化氢的总量占所述组合物的0.5-5重量%。
9.如前述权利要求中任一项所述的组合物,其还包含400至800Da平均分子量的聚乙二醇。
10.如前述权利要求中任一项所述的组合物,其含有小于3%的水。
11.如权利要求1-10中任一项所述的组合物,其为无研磨剂的凝胶洁齿剂。
12.如权利要求1-10中任一项所述的组合物,其为包含选自磷酸钙盐和碳酸钙的钙研磨剂的牙膏。
13.如权利要求12所述的组合物,其中所述钙研磨剂包括焦磷酸钙。
14.如前述权利要求中任一项所述的组合物,其还包含牙垢控制剂诸如焦磷酸四钠。
15.如权利要求14所述的组合物,其包含以重量计的以下成分:
16.如前述权利要求中任一项所述的组合物,其包含0.5-1重量%的氟化物离子源,例如单氟磷酸钠。
17.如前述权利要求中任一项所述的组合物,其包含调味剂、甜味剂、抗氧化剂、抗微生物剂或其中的两种或更多种的组合。
18.如前述权利要求中任一项所述的组合物,其中在于60℃下老化1周之后,所述组合物包装于其中的管的顶部直径伸展小于0.1cm。
19.如前述权利要求中任一项所述的组合物,其中在于60℃下老化1周之后,所述组合物包装于其中的所述管的所述顶部直径伸展小于所述管的所述顶部直径的1%。
20.如前述权利要求中任一项所述的组合物,其中在储存24小时之后,所述组合物未表现出不可接受的相分离水平。
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US11141364B2 (en) * | 2017-11-30 | 2021-10-12 | Colgate-Palmolive Company | Oral care compositions |
US20220323319A1 (en) * | 2021-04-08 | 2022-10-13 | Colgate-Palmolive Company | Oral care compositions |
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2013
- 2013-12-05 CN CN201380081340.5A patent/CN105792805A/zh active Pending
- 2013-12-05 MX MX2016006948A patent/MX353023B/es active IP Right Grant
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- 2013-12-05 BR BR112016011932A patent/BR112016011932A2/pt not_active IP Right Cessation
- 2013-12-05 WO PCT/US2013/073234 patent/WO2015084357A1/en active Application Filing
- 2013-12-05 US US15/101,153 patent/US20160303011A1/en not_active Abandoned
- 2013-12-05 CA CA2926396A patent/CA2926396C/en active Active
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RU2646484C2 (ru) | 2018-03-05 |
TW201534338A (zh) | 2015-09-16 |
PH12016500890A1 (en) | 2016-06-20 |
AR098652A1 (es) | 2016-06-01 |
CA2926396C (en) | 2021-06-15 |
BR112016011932A2 (pt) | 2017-08-08 |
MX2016006948A (es) | 2016-08-19 |
AU2013406744A1 (en) | 2016-06-02 |
AU2013406744B2 (en) | 2017-06-22 |
US20160303011A1 (en) | 2016-10-20 |
WO2015084357A1 (en) | 2015-06-11 |
EP3076926A1 (en) | 2016-10-12 |
CA2926396A1 (en) | 2015-06-11 |
MX353023B (es) | 2017-12-18 |
IL245701A0 (en) | 2016-07-31 |
EP3076926B1 (en) | 2018-02-14 |
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