CN102612385B - 用于改善口味的方法和具有改善口味的口腔护理组合物 - Google Patents
用于改善口味的方法和具有改善口味的口腔护理组合物 Download PDFInfo
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- CN102612385B CN102612385B CN201080018058.9A CN201080018058A CN102612385B CN 102612385 B CN102612385 B CN 102612385B CN 201080018058 A CN201080018058 A CN 201080018058A CN 102612385 B CN102612385 B CN 102612385B
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- oral care
- taste
- care composition
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Landscapes
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Abstract
本文提供了涉及具有改善口味的口腔护理组合物的组合物和方法。一种此类方法包括提供一种口腔护理组合物,其包含金属盐、过氧化物、抗微生物剂、口臭抑制剂、表面活性剂、或它们的组合,并且向所述口腔护理组合物加入TRPV1激活因子和/或浓馥香兰素。
Description
发明领域
本发明涉及具有改善口味的口腔护理组合物和改善口腔护理组合物口味的方法。
发明背景
人们一直在寻找改善他们的笑容和他们的牙齿及口腔健康的方法。许多人在该过程中的第一步是使用口腔护理组合物如牙膏和漱口液。使用那些类型的产品获得的有益效果涵盖范围广泛,从美容有益效果如美白和口气清新到健康有益效果如减少牙垢。遗憾的是,用于口腔护理组合物的多种组分,包括提供期望有益效果的试剂,常常对产品的总体口味具有负面影响。因此,需要在口腔护理组合物中提供改善风味的方法和具有改善风味的口腔护理组合物。
发明概述
在一个实施方案中,本发明涉及用于改善口腔护理组合物口味的方法。该方法包括混合TRPV1激活因子和坏味剂以形成口腔护理组合物,所述坏味剂选自由下列组成的组:金属盐、过氧化物、抗微生物剂、口臭抑制剂、表面活性剂、以及它们的组合。
在另一个实施方案中,本发明涉及用于改善口腔护理组合物口味的方法,其中该方法包括混合香兰基丁基醚和坏味剂以形成口腔护理组合物,所述坏味剂包括锌盐、亚锡盐、钾盐、铜盐、或它们的组合,其中所述香兰基丁基醚的量占该口腔护理组合物重量的约0.001%至约0.025%。
在另一个实施方案中,本发明涉及用于改善口腔护理组合物口味的方法,其中该方法包括混合浓馥香兰素和坏味剂以形成口腔护理组合物,所述坏味剂包括金属盐、过氧化物、或它们的组合,其中所述浓馥香兰素的量占该口腔护理组合物重量的约0.01%至约0.4%。
据信根据下文描述将会更好的理解本发明的这些以及其它实施方案。
发明详述
定义
除非另外指明,下文中所用的所有百分比和比率均以总组合物的重量计。除非另外指明,本文提及的所有成分的百分数、比例和含量均基于该成分的实际含量,并且不包括在可商购获得的产品中可与这些成分一起使用的溶剂、填料或其它物质。
除非另外指明,本文提及的所有测量均在约25℃(即室温)下进行。
如本文所用,单词“约”指百分之+/-10%。
如本文所用,单词“包括/包含”和它的变体旨在是非限制性的,使得列表中条目的叙述不排除其它也可能在本发明的材料、组合物、装置和方法中有用的类似条目。
“口腔护理组合物”是指在一般使用过程中不是被故意吞咽以用于特定治疗剂的全身给药的目的,而是在口腔中保留足够长的时间以接触牙齿表面和/或口腔组织的产品。所述口腔护理组合物可为多种形式,包括牙膏、洁齿剂、牙胶、齿龈胶、漱口水、摩丝、泡沫、口喷剂、锭剂、咀嚼片、口香糖或假牙护理产品。该口腔护理组合物还可掺入到带或薄膜上,以直接施用或粘附到口腔表面。
除非另外指明,本文所用术语“洁齿剂”包括糊剂、凝胶、或液体制剂。洁齿剂可为双相形式,例如条形膏体,并且也可用作一种方案。
如本文所用,术语“坏味剂”指口腔护理组合物中的一种组分,其提供使用者不良口味,例如金属口味或涩味,或者不良感觉,例如口腔干燥的感觉。
如本文所用,术语“牙齿”是指自然牙齿以及人造牙齿或假牙。
如本文所用,术语“TRPV1”指瞬时受体电位香草酸受体亚型1,其是优先表达在小直径的感觉神经元上的配体门控型、非选择性阳离子通道并且检测有毒的以及其它的物质。
如本文所用,术语“TRPV1激活因子”指根据本文所讨论的FLIPR方法,在1mM的浓度下提供比细胞中存在的背景钙水平高至少1000计数的钙离子流计数的任何组分。术语“计数”定义为转染细胞系由于钙离子通过细胞膜流入时导致的荧光变化,所述钙离子与存在于细胞内的钙离子敏感染料反应。
如本文所用,术语“TRPV1增强剂”指提高化合物的钙离子流活性的任何组分,所述化合物直接激活TRPV1,但是不直接激活TRPV1。
可用于本文的活性成分和其它成分可根据其美容和/或治疗有益效果或它们的假定的运行模式或作用来分类或描述于本文中。然而应当理解,在一些情况下,可用于本文的活性成分和其它成分能够提供一种以上的美容和/或治疗有益效果或作用,或通过一种以上的作用模式起作用运行。因此,本文所做的分类是为了方便起见,而非旨在将成分限制在所列的具体指定的一个或多个功能或活性上。
口腔护理组合物和方法
非常期望用于清洁和护理口腔的消费品赋予清新和清洁的感觉,因为这种感觉向消费者提供持久清新和清洁的信号。除了清洁的感觉之外,消费者还期望体验口腔护理活性物质如抗牙垢剂的有益效果,例如通过他们的口腔护理方案。然而配制消费者可接受的口腔护理组合物的能力提出了挑战,因为许多用于赋予风味、递送有益效果、或者是口腔护理组合物基础部分的组分在带来它们的目的有益效果的同时带来了不良的口味和/或感觉。因此,配制口腔护理组合物可为在可接受的风味和可接受的有益效果之间的平衡行为。
下文中将会看到,可用于配制口腔护理组合物的多种组分导致不良口味并因此使配制消费者可接受的产品成为挑战。目前已经发现向口腔护理组合物中加入某些组分能够减少与下文讨论的多种组分相关联的多种不良口味并因此改善口味。这些口味改善组分包括:例如TRPV1激活因子和浓馥香兰素。
将有助于改善口腔护理组合物口味的第一类组分是瞬时受体电位香草酸亚型1(TRPV1)激活因子。TRPV1是配体门控型的、非选择性阳离子通道,优先在小直径感觉神经元上表达。当研究该受体时,发现激活该受体引起令人惊讶的效应。通过添加TRPV1激活因子至具有不良口味的组分的口腔护理组合物中,所述组合物的使用者体验改善的超过无TRPV1激活因子的口腔护理组合物的口味。因此,TRPV1激活因子致力于抵消与口腔护理组合物中所使用的多种组分相关的不良口味。
为了测定是否激活了TRPV1,测量TRPV1受体中的细胞内钙离子(Ca+2)含量。用人TRPV1稳定转染的HEK-23(人胚肾)细胞在75Cm2烧瓶中的15mL培养基[补充有10%FBS(胎牛血清),100μg/mL青霉素/链霉素,100μg/mL G418的高糖DMEM(Dulbecco′s Modificationof Eagle′s Medium)]内生长3天,所述烧瓶置于设置为33℃、5%CO2的哺乳动物细胞培养箱中。加入10mL的PBS(磷酸盐缓冲液),轻轻手摇振荡分离细胞。将细胞转移至50mL管中并且以850rpm离心3分钟以除去PBS。在离心后,细胞沉淀形成在管的底部,使它们与上层溶液分离。弃去上清液,并且将细胞沉淀物悬浮在1mL新鲜培养基中,其中加入5μL(12.5μg)Fluo-4AM(Molecular Probes,Inc.)钙指示剂并轻轻振荡培养30分钟。Fluo-4是一种用于定量在100nM至1微摩尔范围内的细胞Ca2+浓度的荧光染料。在30分钟结束时,添加45mL分析缓冲液[1xHBSS(Hank平衡盐溶液)、20mM HEPES(4-(2-羟基乙基)-1-哌嗪乙磺酸)]以洗涤细胞,并且然后将所得混合物在850rpm下离心3分钟以除去过量的缓冲液和Fluo-4AM钙指示剂。
将沉淀的细胞重新悬浮在10mL分析缓冲液中,并且将90μL等分试样(约50,000个细胞)/孔递送至96-孔的包含10μL测试化合物(1mM,在分析缓冲液中,最终浓度100μM)或者缓冲液对照物的检测板上,并且在室温下培养30分钟。在30分钟后,将板置于荧光成像板阅读器(FLIPR384,得自Molecular Devices)中并且记录基本的荧光(激发波长488nm,而发射波长510nm)。FLIPR检测法是用于检测细胞内钙浓度变化的公认方法。然后加入20μL作为TRPV1激活因子测试的分子并记录荧光。为了确定测试化合物对TRPV1的直接影响,在添加每种化合物之后立即测定荧光。FLIPR方法的附加讨论可见于Smart等人,Characterizatton using FLIPR of human vanilloid VRl receptor pharmacology,European Journal of Pharmacology 417,51-58(2001)和Liu等人,Development andvalidation of a platelet calcium flux assay using a fluorescent imaging platereader,Analytical Biochemistry 357,216-224(2006)。
TRPV1响应于例如有毒和疼痛刺激。有毒刺激将包括那些提供辛辣(即辣)感觉的那些。下表列出一些TRPV1激活因子,它们属于此类并提供辛辣感觉,其以标准Scoville辣度指标进行测量。
化合物 | ‘辣度’ |
(对数Scoville单位) | |
二氢辣椒碱 | 7.2 |
辣椒碱 | 7.2 |
降二氢辣椒碱 | (NorhydroCapsaicin)7.0 |
同型二氢辣椒碱 | 6.9 |
同型辣椒碱 | 6.9 |
香兰基丁基醚 | 5.7 |
胡椒碱 | 5.3 |
6-姜烯酚(6-Shoagol) | 5.1 |
6-姜醇 | 4.9 |
蒜素 | 4.0 |
姜油酮 | <4.0 |
因为许多这些化合物来源于天然来源,当以提供温暖效应的含量使用时,它们常常保留源极材料的固有辣味。例如,胡椒碱是胡椒味,辣椒碱类似红辣椒样,而姜油酮保留姜的辣味。这也对合成化合物实用如香兰基丁基醚的原味,如US6570010B2中所述。令人感兴趣的是,使用类似上文的那些TRPV1激活因子,以低于引起辛辣效应的用量,提供减轻不良口味并且其中消费者能够感觉到改善口味的产品。引起辛辣效应的用量导致消费者感受到辛辣感并且不一定改善风味。在一个实施方案中,将按所述口腔护理组合物的重量计约0.0001%至约0.1%的量添加TRPV1激活因子。然而,激活TRPV1的水平与激活因子的辣度水平有关。因此,使用的TRPV1激活因子的水平将取决于其辣度。例如,香兰基丁基醚(其在1mM浓度下具有大约14942.84的钙离子激活水平)的用量一般将为约0.025%或更低,而辣椒碱(其在300nM的低得多的浓度下具有约14127.16的钙离子激活水平)的用量将为约0.009%或更低。因此浓度低得多的辣椒碱(300nM)提供与浓度高得多的VBE(1mM)几乎相同的激活水平,并且因此用量可较小。
除了其作为有毒物质检测器的作用之外,据信激活TRPV1也具有一些下游效应。具体地讲,不受理论的约束,据信激活TRPV1引起其它味觉受体的变化,具体地讲PKD1L3、PKD2L1、以及TAS2R受体家族。据信TAS2R16、TAS2R38、PKD2L1和PKD1L3受体的变化也有助于改善口味。
令人感兴趣的是,一些提供不良口味的化合物也影响TRPV1的活性,但是水平非常低(即低于成为TRPV1激活因子所需的水平)。不受理论的约束,就导致口腔护理组合物中的不良口味并影响TRPV1受体活性但是不提高激活因子水平的那些组分而言,据信TRPV1激活因子与这些组分竞争与TRPV1受体的结合。这阻止不良口味组分通过与TRPV1结合引起的TRPV1或任何下游活性传播任何不良口味。
按照上文所述,根据本发明的一个实施方案,包含坏味剂和TRPV1激活因子的口腔护理组合物将具有改善的口味。此外,在一个实施方案中,改善口腔护理组合物口味的方法包括混合TRPV1激活因子和坏味剂以形成口腔护理组合物,所述坏味剂选自由下列组成的组:金属盐、过氧化物、抗微生物剂、口臭抑制剂、表面活性剂、以及它们的组合。
在一个实施方案中,TRPV1激活因子包含香兰基丁基醚、姜油酮、辣椒碱、辣椒素酯、姜烯酚、姜醇、胡椒碱、或它们的组合。在另一个实施方案中,TRPV1激活因子包含香兰基丁基醚。在一个实施方案中,香兰基丁基醚的加入量按所述口腔护理组合物的重量计为约0.001%至约0.25%。在另一个实施方案中,香兰基丁基醚的加入量按所述口腔护理组合物的重量计为约0.002%至约0.02%。
在另一个实施方案中,用于改善口腔护理组合物口味的方法包括混合香兰基丁基醚和坏味剂以形成口腔护理组合物,所述坏味剂包括锌盐、亚锡盐、钾盐、铜盐、或它们的组合,其中所述香兰基丁基醚的量占该口腔护理组合物的约0.001%至约0.025%。在另一个实施方案中,口腔护理组合物或方法还包括将浓馥香兰素、姜油酮、或它们的组合加到口腔护理组合物中。在一个实施方案中,姜油酮的加入量为约0.01%至约0.015%。在另一个实施方案中,浓馥香兰素的加入量为约0.01%至约0.015%。
此外,已经发现一些化合物增强TRPV1激活因子的效应,虽然这些增强剂本身不激活TRPV1。例如参见下表,其中所述增强剂在TRPV1激活因子(辣椒碱)之后加入以测定是否发生附加的增强。
混合物名称 | CAS# | %增强 |
Δ-二氢大马酮 | 57378-68-4 | 28.53 |
α-二氢大马酮 | 43052-87-5 | 28.1 |
丁酸香叶酯 | 106-29-6 | 23.46 |
2-辛酮 | 111-13-7 | 19.87 |
糠醛 | 98-01-1 | 19.29 |
α-紫罗酮 | 127-41-3 | 18.84 |
2,6-二甲基-5-庚烯醛 | 106-72-9 | 17.5 |
焦磷酸四钠 | 7722-88-5 | 15.62 |
乙酸α,α-二甲基苯酯 | 151-05-3 | 14.64 |
苯乙醛二甲醛 | 101-48-4 | 14.07 |
加菲力士(kephalis) | 36306-87-3 | 13.74 |
氧化芳樟醇 | 1365-19-1 | 13.67 |
乙酸香芹酯 | 97-42-7 | 12.83 |
金合欢烯 | 502-61-4 | 12.33 |
反式-2-己烯乙酸酯 | 2497-18-9 | 10.62 |
庚醇 | 111-70-6 | 10.16 |
在另一次测试中,将TRPV1激活因子(VBE)和所述增强剂一起加入。这里,不受理论的约束,当一开始加入增强剂时,它似乎对TRPV1激活因子的激活具有令人惊讶的附加效果。参见下表。
使用增强剂将进一步促进改善口腔护理组合物的口味,并且能够减少所需的TRPV1激活因子量。提高的水平可用于帮助测定增强剂的效应和TRPV1激活因子的任何期望的减少。例如,在一个实施方案中使用的香兰基丁基醚将为0.012%,但是与0.003%的增强剂Δ二氢大马酮一起时,VBE能够以0.008%的量使用以达到与不使用增强剂相同的效果。
因此,在一个实施方案中,口腔护理组合物或改善口腔护理组合物口味的方法还包括加入TRPV1增强剂到口腔护理组合物中。在另一个实施方案中,TRPV1增强剂选自由下列组成的组:二氢大马酮、丁酸香叶酯、2-辛酮、糠醛、紫罗酮、2,6-二甲基-5-庚烯醛、焦磷酸四钠、乙酸α-二甲基苯乙酯、苯乙醛二甲醛、加菲力士(kephalis)、氧化芳樟醇、乙酸香芹酯、金合欢烯、反式-2-己烯乙酸酯、庚醇、以及它们的组合。
尽管不被认为是TRPV1激活因子,浓馥香兰素也具有降低与上述至少一些组分相关联的不良味道的能力。浓馥香兰素是具有香草香味的丁子香酚衍生物。不受理论的约束,据信浓馥香兰素可能不辅助激活TRPV1,而是直接调控前述的味觉受体。
按照上文所述,口腔护理组合物包含口腔护理组分,其提供不良口味,而浓馥香兰素将具有改善的口味。此外,在一个实施方案中,本发明涉及用于改善口腔护理组合物口味的方法,包括混合浓馥香兰素和坏味剂以形成口腔护理组合物,所述坏味剂包括金属盐、过氧化物、或它们的组合,其中所述浓馥香兰素的量占该口腔护理组合物重量的约0.01%至约0.4%。
在一个实施方案中,金属盐包括锌盐、亚锡盐、钾盐、铜盐、或它们的组合。在另一个实施方案中,过氧化物选自由下列组成的组:过氧化氢、过氧化脲、过氧化钙、过氧化钠、以及它们的组合。在另一个实施方案中,浓馥香兰素的加入量按所述口腔护理组合物的重量计为约0.05%至约0.15%。在另一个实施方案中,钾盐包括硝酸钾,并且其量按所述口腔护理组合物的重量计为约0.01%至约5.0%。在另一个实施方案中,锌盐包括柠檬酸锌,并且其量按所述口腔护理组合物的重量计为约0.05%至约5.0%。
在另一个实施方案中,可使用浓馥香兰素、姜油酮和香兰基丁基醚的组合以向口腔护理组合物提供改善的口味。因此,在一个实施方案中,具有改善口味的口腔护理组合物包含浓馥香兰素、姜油酮和香兰基丁基醚。
TRPV1激活因子和/或浓馥香兰素的加入顺序不是至关重要的。因此,在制备口腔护理组合物时或在制备完成口腔护理组合物后的某个时间点上可将TRPV1激活因子和/或浓馥香兰素与口腔护理组分一起加入。
口腔护理组合物
口腔护理组合物常常由组分的组合构成,所述组分可包括载体材料、表面活性剂、风味剂、染色剂、感觉剂、活性物质、以及其它添加剂。
载体材料
载体材料一般应用于各处,用量按口腔护理组合物的重量计为约5%至约80%。能用作载体材料的材料实例包括水、甘油、山梨醇、分子量小于约50,000的聚乙二醇、丙二醇和其它可食用多元醇、乙醇、或它们的组合。在这些载体材料中,一些载体材料的实例导致口腔护理组合物中的不良口味,包括例如丙二醇和/或乙醇。通常与这类材料相关联的不良口味为苦味、辣味、涩味和/或泥土味或臭味。
表面活性剂
口腔护理组合物的另一种组分可包括表面活性剂。口腔护理组合物中一般包括的表面活性剂在约1%至约15%的范围内。表面活性剂可为阴离子的、非离子的、两性的、两性离子的、阳离子的、或它们的组合。可用于本发明的阴离子表面活性剂包括例如烷基中含有8至20个碳原子的烷基硫酸的水溶性盐(例如烷基硫酸钠)和含有8至20个碳原子的脂肪酸的磺化单酸甘油酯的水溶性盐。这类阴离子表面活性剂的实例是月桂基硫酸钠(SLS)和椰子基单酸甘油酯磺酸钠。其它适宜的阴离子表面活性剂包括肌氨酸盐如月桂酰肌氨酸钠、牛磺酸盐、月桂基磺基乙酸钠、月桂酰羟乙基磺酸钠、月桂基聚氧乙烯醚羧酸钠和十二烷基苯磺酸钠。也可使用阴离子表面活性剂的组合。许多适宜的阴离子表面活性剂由Agricola等人公开于美国专利3,959,458中。在不同实施方案中,本发明的组合物以约0.025%至约9%,约0.05%至约5%或约0.1%至约1%的含量包含阴离子表面活性剂。
本文可用的另一类阴离子表面活性剂为烷基磷酸酯。表面活性有机磷酸酯试剂对釉质表面具有强亲和力,并且具有充分的表面结合倾向,以使表膜蛋白质解吸,并且保持附着在釉质表面上。有机磷酸酯化合物的适用实例包括单-、双-或三酯,它们以下文的通式结构表示,其中Z1、Z2、或Z3可为相同的或不同的,至少一个是有机基团,在一个实施方案中选自1至22个碳原子的直链或支链的烷基或烯基,其任选地被一个或多个磷酸酯基;烷氧基化的烷基或烯基、(多)糖、多元醇或聚醚基取代。
一些其它试剂包括由下列结构表示的烷基或烯基磷酸酯:
其中R1代表具有6至22个碳原子,任选被一个或多个磷酸酯基团取代的直链或支链烷基或烯基;n和m独立并且分别为2至4,并且a和b独立并且分别为0至20;Z2和Z3可相同或不同,每个代表氢、碱金属、铵、质子化烷基胺或质子化官能烷基胺如链烷醇胺、或R1-(OCnH2n)a(OCmH2m)b-基团。合适试剂的实例包括烷基和烷基(聚)烷氧基磷酸酯如月桂基磷酸酯;PPG5鲸蜡硬脂基聚氧乙烯醚-10磷酸酯;月桂基聚氧乙烯醚-1磷酸酯;月桂基聚氧乙烯醚-3磷酸酯;月桂基聚氧乙烯醚-9磷酸酯;三月桂醇聚醚-4磷酸酯;C12-18PEG 9磷酸酯;二月桂醇聚醚-10磷酸酯钠。在一个实施方案中,烷基磷酸酯是聚合的。聚烷基磷酸酯的实例包括包含重复的烷氧基作为聚合部分的那些,具体地讲包含3个或更多个乙氧基、丙氧基、异丙氧基或丁氧基的那些。
其它适宜的聚合有机磷酸酯试剂包括葡聚糖磷酸酯、多葡糖苷磷酸酯、烷基多葡糖苷磷酸酯、聚甘油基磷酸酯、烷基聚甘油基磷酸酯、聚醚磷酸酯和烷氧基化多元醇磷酸酯。某些具体的实例是PEG磷酸酯、PPG磷酸酯、烷基PPG磷酸酯、PEG/PPG磷酸酯、烷基PEG/PPG磷酸酯、PEG/PPG/PEG磷酸酯、双丙二醇磷酸酯、PEG甘油基磷酸酯、PBG(聚丁二醇)磷酸酯、PEG环糊精磷酸酯、PEG脱水山梨糖醇磷酸酯、PEG烷基脱水山梨糖醇磷酸酯和PEG甲基葡糖苷磷酸酯。适宜的非聚合磷酸酯包括烷基单甘油酯磷酸酯、烷基脱水山梨糖醇磷酸酯、烷基甲基葡糖苷磷酸酯、烷基蔗糖磷酸酯。
另一类适宜的表面活性剂是选自由下列组成的组的表面活性剂:肌氨酸盐表面活性剂、羟乙基磺酸盐表面活性剂和牛磺酸盐表面活性剂。在一个实施方案中,使用这些表面活性剂的碱金属或铵盐。这些钠盐或钾盐的实例包括以下盐:月桂酰肌氨酸盐、肉豆寇酰肌氨酸盐、棕榈酰肌氨酸盐、硬脂酰肌氨酸盐和油酰肌氨酸盐、或它们的组合。在这些阴离子表面活性剂中,导致口腔护理组合物内不良口味的一些实例包括例如SLS、月桂酰肌氨酸盐和/或与天然来源的表面活性剂相关联的脂肪醇或酸。通常与这些表面活性剂相关联的不良口味为肥皂味、化学制品味和/或人造味道。
可用于口腔护理组合物的两性离子或两性表面活性剂包括脂族季铵、鏻和锍化合物的衍生物,其中所述脂族基团可以是直链或支链的,其中一个脂族取代基包含约8至18个碳原子,并且一个脂族取代基包含阴离子水增溶基团,例如羧基、磺酸根、硫酸根、磷酸根或膦酸根。适宜的甜菜碱表面活性剂公开于授予Polefka等人的美国专利5,180,577中。典型的烷基二甲基甜菜碱包括癸基甜菜碱或2-(N-癸基-N,N-二甲基氨基)乙酸酯、椰油基甜菜碱或2-(N-椰油基-N,N-二甲基氨基)乙酸酯、十四烷基甜菜碱、棕榈基甜菜碱、月桂基甜菜碱、鲸蜡基甜菜碱、鲸蜡基甜菜碱、硬脂基甜菜碱等。酰氨基甜菜碱以椰油酰氨基乙基甜菜碱、椰油酰氨基丙基甜菜碱(CADB)和月桂酰氨基丙基甜菜碱为例。在这些表面活性剂中,导致口腔护理组合物内不良口味的一些实例包括例如椰油酰氨基丙基甜菜碱和月桂基甜菜碱。通常与这些表面活性剂相关联的不良口味为肥皂味和化学制品味。口腔护理组合物中一般包括的这些表面活性剂为约0.5%至约5%。
用于本发明的阳离子表面活性剂包括例如季铵化合物的衍生物(所述化合物具有一个包含约8至18个碳原子的长链烷基链)如月桂基三甲基氯化铵;西吡氯铵;十六烷基三甲基溴化铵;椰子基烷基三甲基亚硝酸铵;氟化鲸蜡基吡啶或它们的组合。具有洗涤剂特性的附加季铵氟化物描述于授予Briner等人的美国专利公开3,535,421中。在这些表面活性剂中,导致口腔护理组合物内不良口味的一些实例包括例如西吡氯铵或氯己定。通常与这些表面活性剂相关联的不良口味为化学制品味和/或防腐剂味。
可用于本发明组合物中的非离子表面活性剂包括例如由氧化亚烷基团(本身亲水的)与本身可为脂族或烷基芳族的有机疏水化合物缩合而产生的化合物。适宜的非离子表面活性剂的实例包括泊洛沙姆、烷基酚的聚环氧乙烷缩合物、衍生自环氧乙烷与环氧丙烷和乙二胺的反应产物的缩合的产物、脂族醇的环氧乙烷缩合物、长链叔胺氧化物、长链叔膦氧化物、长链二烷基亚砜,以及这些物质的混合物。
风味剂
可为口腔护理组合物一部分的另一种组分包括风味剂。风味剂的量按口腔护理组合物的重量计一般为约0.4%至约3%。用于口腔护理组合物的一些风味剂和风味剂组分的实例是薄荷油、冬青油、丁香芽油、桂皮、鼠尾草、欧芹油、牛至属植物、柠檬、橙、羟甲基茴香脑、洋茉莉醛、4-顺式-庚烯醛、联乙酰、对-叔丁基苯基乙酸甲酯、水杨酸甲酯、水杨酸乙酯、乙酸1-薄荷酯、烷酮、α-紫罗兰酮、肉桂酸甲酯、肉桂酸乙酯、肉桂酸丁酯、丁酸乙酯、乙酸乙酯、邻氨基苯甲酸甲酯、乙酸异戊酯、丁酸异戊酯、己酸烯丙酯、丁子香酚、桉树脑、百里酚、肉桂醇、辛醇、辛醛、癸醇、癸醛、苯乙醇、苄醇、α-萜品醇、里哪醇、苧烯、橙花醛、柠檬醛、香叶醛、香叶醇橙花醇、麦芽酚、乙基麦芽酚、茴香脑、二氢茴香脑、香芹酮、薄荷酮、β-大马酮、紫罗酮、γ-癸内酯、γ-壬内酯、γ-十一烷酸内酯、或它们的组合。一般来讲,适宜的风味成分是结构特征和官能团较不倾向于氧化还原反应的化合物。这些包括饱和的或包含稳定芳环或酯基的风味剂化合物的衍生物。在这些风味剂中,导致口腔护理组合物内不良口味的一些实例包括柠檬醛、香叶醛、桉叶油素和丁子香酚。通常与这些风味剂相关联的不良口味为酸味、化学制品味、苦味、辣味和/或涩味。
染色剂
此外,染色剂能够构成口腔护理组合物的一部分。染色剂的量按口腔护理组合物的重量计一般为约0.001%至约0.5%。用于口腔护理组合物的一些染色剂实例包括D&CYellow No.10、FD&C Blue No.1、FD&C Red No.40、D&C Red No.33以及它们的组合。染色剂的含量可为约0.0001%至约0.1%。在一个实施方案中,染色剂的量按口腔护理组合物的重量计为约0.001%至约0.01%。在这些染色剂中,导致口腔护理组合物内不良口味的一些染色剂实例包括例如D&C Red No.33。通常与这些染色剂相关联的不良口味为金属味和/或化学制品味。
感觉剂
可为口腔护理组合物一部分的另一种组分是感觉剂。感觉剂分子如清凉、温暖和麻刺感试剂用于递送信号给消费者。感觉剂的量按口腔护理组合物的重量计一般为约0.001%至约0.8%。最为人们熟知的清凉感觉剂化合物是薄荷醇,尤其是l-薄荷醇,其天然存在于薄荷油中。薄荷醇的其它异构体(新薄荷醇、异薄荷醇和新异薄荷醇)具有一定程度的相似性,但是气味和口味不同,即,具有令人不悦的味道,描述为泥土味、樟脑味、霉味等。异构体之间最大的差异是它们的清凉能力。L-薄荷醇提供最具效力的清凉感,即具有约800ppb的清凉度下限,即可清晰辨识清凉效果时的浓度。在此含量下,其它异构体无清凉效果。
在合成的凉爽剂中,许多是薄荷醇的衍生物或者与薄荷醇结构上相关的,即包含环己烷部分并且是官能团衍生的,所述官能团包括羧酰胺、缩酮、酯、醚和醇。实例包括对-薄荷烷甲酰胺化合物如N-乙基-对-薄荷烷-3-甲酰胺。结构上与薄荷醇不相关的合成羧酰胺凉爽剂的实例是N,2,3-三甲基-2-异丙基丁酰胺。合成凉爽剂的附加实例包括醇衍生物如3-1-薄荷氧基丙烷-1,2-二醇、异蒲勒醇和对-薄荷烷-3,8-二醇;薄荷酮甘油缩酮;薄荷酯如乙酸薄荷酯、乙酰乙酸薄荷酯、乳酸薄荷酯和单琥珀酸薄荷酯。羧酰胺凉爽剂描述于例如美国专利4,136,163;4,150,052;4,153,679;4,157,384;4,178,459和4,230,688中。
结构上与薄荷醇不相关但是已经被报道具有相似生理清凉效果的附加试剂包括描述于美国专利公开6,592,884中的α-酮基烯胺衍生物,包括3-甲基-2-(1-吡咯烷基)-2-环戊烯-1-酮(3-MPC)、5-甲基-2-(1-吡咯烷基)-2-环戊烯-1-酮(5-MPC)和2,5-二甲基-4-(1-吡咯烷基)-3(2H)-呋喃酮(DMPF);icilin(也称为AG-3-5,化学名1-[2-羟基苯基]-4-[2-硝基苯基]-1,2,3,6-四氢吡啶-2-酮),描述于Wei等人,J.Pharm.Pharmacol.(1983),35:110-112中。在这些清凉感觉剂中,导致口腔护理组合物内不良口味的一些实例包括例如薄荷醇和薄荷酮。通常与这些清凉感觉剂相关联的不良口味包括辣味、化学制品味和/或药味。
一些温暖感觉剂的实例包括乙醇;辣椒;烟酸酯如烟酸苄酯;多元醇;辣椒粉;辣椒酊剂;辣椒提取物;辣椒碱;同型辣椒碱;同型二氢辣椒碱;壬酰基香兰酰胺;壬酸香兰基醚;香兰醇烷基醚衍生物如香兰基乙基醚、香兰基丁基醚、香兰基戊基醚和香兰基己基醚;异香兰醇烷基醚;香兰醇乙醚;藜芦基醇衍生物;取代苄醇衍生物;取代苄醇烷基醚;香兰丙二醇缩醛;乙基香兰丙二醇缩醛;姜提取物;生姜油;姜醇;姜油酮;或它们的组合。口腔护理组合物中包括的温暖感觉剂的量一般为约0.05%至约2%。
一些麻刺感觉剂的实例包括金钮扣油树脂、秦椒(Zanthoxylum peperttum)、花椒麻素-I、花椒麻素II、山椒酰胺、胡椒碱、哌啶、丁子香酚、千日菊素、4-(1-甲氧甲基)-2-苯基-1,3-二氧杂环戊烷、或它们的组合。口腔护理组合物中包括的麻刺感觉剂的量一般为约0.0005%至约1%。在这些麻刺感觉剂中,导致口腔护理组合物内不良口味的一些实例包括例如金钮扣油树脂、花椒麻素和/或丁子香酚。通常与这些麻刺感觉剂相关联的不良口味包括胡椒味、苦味和/或金属味。
甜味剂
口腔护理组合物中可包括的另一种组分包括甜味剂。甜味剂可为天然的或人造的,并且其量按口腔护理组合物重量计一般为约0.1%至约1%。一些适宜的水溶性甜味剂包括单糖、二糖和多糖,例如木糖、核糖、葡萄糖(右旋糖)、甘露糖、半乳糖、果糖(左旋糖)、蔗糖(食糖)、麦芽糖、转化糖(衍生自蔗糖的果糖和葡萄糖的组合)、部分水解的淀粉、玉米糖浆固体、二氢查尔酮、应乐果甜蛋白、蛇菊苷、甘草素、或它们的组合。适宜的水溶性人造甜味剂包括可溶解的糖精盐,即糖精钠或糖精钙盐、环磺酸盐、3,4-二氢-6-甲基-1,2,3-噻嗪-4-酮-2,2-二氧化物的钠盐、铵盐或钙盐、3,4-二氢-6-甲基-1,2,3-噻嗪-4-酮-2,2-二氧化物的钾盐(丁磺氨-K)、游离酸形式的糖精等。其它适宜的甜味剂包括基于二肽的甜味剂,例如L-天冬氨酸衍生的甜味剂,如L-天冬氨酰基-L-苯丙氨酸甲酯(天冬甜素)、N-[N-(3,3-二甲基丁基)-L-α-天冬氨酰基]-L-苯丙氨酸1-甲酯(纽甜(neotame))和美国专利3,492,131中描述的物质,L-α-天冬氨酰基-N-(2,2,4,4-四甲基-3-硫化三亚甲基)-D-丙氨酸酰胺水合物,L-天冬氨酰基-L-苯基甘油和L-天冬氨酰基-L-2,5-二氢苯基甘氨酸的甲酯,L-天冬氨酰基-2,5-二氢-L-苯丙氨酸,L-天冬氨酰基-L-(1-环己烯基)-丙氨酸等等。可以使用衍生自天然存在的水溶性甜味剂的水溶性甜味剂,例如普通食糖(蔗糖)的氯化衍生物(例如在三氯蔗糖的产品描述下已知的),以及蛋白质基甜味剂例如西非竹竽素(索马甜I和II)。在这些甜味剂中,导致口腔护理组合物内不良口味的一些实例包括例如天冬甜素、糖精、或纽甜。通常与这些甜味剂相关联的不良口味包括苦味和酸味。
活性物质
口腔护理组合物中可包括的一种附加组分包括口腔护理活性物质。口腔护理活性物质的量一般为约0.0001%至约8%。口腔护理活性物质的一些实例包括防龋剂、抗微生物剂、抗牙垢剂、口臭抑制剂和漂白剂。防龋剂一般用量为约0.01%至约3.0%。洁齿剂和其它口腔组合物中通常具有足量的氟化物化合物以便为组合物提供氟离子浓度,所述氟离子浓度按重量计为约0.0025%至约5.0%时能提供防龋效果。在一个实施方案中,氟化物浓度按重量计为约0.005%至约2.0%。多种产生氟离子的物质可被用作本发明组合物和方法中适宜的可溶性氟化物源。适宜的氟化物离子产生材料的实例存在于授予Briner等人的美国专利公开3,535,421和授予Widder等人的美国专利公开3,678,154中代表性的氟化物离子源包括:氟化亚锡、氟化钠、氟化钾、氟化胺、单氟磷酸钠、氟化铟、氟化胺如奥拉氟(Olaflur)、以及多种其它来源。在一个实施方案中,防龋剂包含的氟化亚锡量为约0.454%。在另一个实施方案中,防龋剂包含的氟化钠量为约0.243%。在这些防龋剂中,导致口腔护理组合物内不良口味的一些实例包括例如氟化亚锡和氟化钾。通常与这些防龋剂相关联的不良口味包括泥土味、臭味和/或金属味。
另一种口腔护理活性物质是抗微生物剂。抗微生物剂的一个实例是季铵化合物。本文可用的那些季铵试剂包括如下的那些:其中季氮上的一个或两个取代基的碳链长度(通常为烷基)为约8至约20、典型地为约10至约18个碳原子,同时剩余取代基(通常为烷基或苄基)具有更低的碳原子数如约1至约7个碳原子,通常为甲基或乙基。典型的季铵抗菌剂实例是十二烷基三甲基溴化铵、氯化十四烷基吡啶、溴化杜灭芬、氯化N-十四烷基-4-乙基吡啶、十二烷基二甲基(2-苯氧乙基)溴化铵、苄基二甲基硬脂基氯化铵、氯化十六烷基吡啶、季铵化5-氨基-1,3-双(2-乙基己基)-5-甲基六氢嘧啶、苯扎氯铵、苄索氯铵和甲基苄索氯铵。其它的化合物包括二[4-(R-氨基)-1-吡啶]烷烃,它公开于美国专利4,206,215,该专利于1980年6月3日授予Bailey。其它季铵化合物包括吡啶化合物。吡啶季铵化合物的实例包括十六烷基吡啶和十四烷基吡啶卤盐(即,氯盐、溴盐、氟盐和碘盐)。包含的季铵抗菌剂含量可为至少约0.035%。在其它实施方案中包含的季铵抗菌剂按口腔护理组合物重量计为约0.045%至约1.0%,或约0.05%至约0.10%。
本发明还可包含其它抗微生物剂,包括非阳离子抗微生物剂,如卤代二苯基醚、苯酚化合物(包括苯酚及其同系物)、一烷基和多烷基卤代苯酚以及芳族卤代苯酚、间苯二酚及其衍生物、木糖醇、双酚化合物和卤代N-水杨酰苯胺、苯甲酸酯和卤代N-碳酰苯胺。还可用的抗微生物剂是酶,包括糖苷内切酶、木瓜蛋白酶、葡聚糖酶、突变酶、以及它们的组合。此类试剂公开于1960年7月26日授予Norris等人的美国专利2,946,725和授予Gieske等人的美国专利4,051,234中。其它抗微生物剂实例包括氯己定、三氯生、三氯生单磷酸盐和风味油如百里酚。三氯生和此类其它试剂公开于Parran,Jr.等人的美国专利5,015,466和授予Nabi等人的美国专利4,894,220中。这些试剂的含量按所述洁齿剂组合物的重量计为约0.01%至约1.5%。上文的抗微生物剂中,导致不良口味的一些实例包括例如氯己定、三氯生和百里酚。通常与这些抗微生物剂相关联的不良口味包括苦味、臭味、泥土味、酸味和/或涩味。
另一种口腔护理活性剂包括抗牙垢剂。抗牙垢剂的一个实例为作为焦磷酸离子来源的焦磷酸盐。可用于本发明组合物中的焦磷酸盐包括例如焦磷酸一碱金属盐、二碱金属盐和四碱金属盐、以及它们的组合。其未水合形式和水合形式的焦磷酸二氢二钠(Na2H2P2O7)、酸式焦磷酸钠、焦磷酸四钠(Na4P2O7)和焦磷酸四钾(K4P2O7)是其它物质。在本发明的组合物中,焦磷酸盐可以三种形式中的一种存在:大部分溶解、大部分不溶解、或溶解和未溶解焦磷酸盐的组合。可用于制备这些组合物的焦磷酸盐量为任何牙垢控制有效量。在不同实施方案中,焦磷酸盐的量按所述口腔护理组合物的重量计为约1.5%至约15%,约2%至约10%,或约3%至约8%。
口腔护理活性物质的其它实例为漂白剂。漂白剂一般是漂白牙齿的试剂。漂白剂的实例包括过氧化物、过硼酸盐、过碳酸盐、过氧酸、过硫酸盐、以及它们的组合。适宜的过氧化物包括过氧化氢、过氧化脲、过氧化钙、过氧化钠、过氧化锌、或它们的组合。过碳酸盐的一个实例为过碳酸钠。过硫酸盐的一个实例包括过硫酸氢钾。以下的量代表过氧化物原料的量,尽管过氧化物源也可包含过氧化物原料之外的成分。例如,过氧化物源可为过氧化物原材料和载体材料的溶液。一般来讲,本发明的组合物可包含约0.01%至约30%的过氧化物原材料。在其它实施方案中,过氧化物原材料按所述口腔护理组合物的重量计为约0.1%至约10%或约0.5%至约5%。在这些漂白剂中,导致口腔护理组合物内不良口味的一些漂白剂实例包括例如过氧化物和过碳酸盐。通常与这些漂白剂相关联的不良口味包括臭味、化学制品味和/或酸味。
另一种口腔护理活性物质为口臭抑制剂。这些试剂一般致力于减轻口臭。口臭抑制剂的实例包括铜盐和羰基化合物,诸如抗坏血酸[3-氧代-L-古洛呋喃内酯];顺式茉莉酮[3-甲基-2-(2-戊烯基-2-环戊烯酮];2,5-二甲基-4-羟基-3(2H)-呋喃酮;5-乙基-3-羟基-4-甲基-2(5H)-呋喃酮;香草醛[4-羟基-3-甲氧基苯甲醛];乙基香草醛;茴香醛[4-甲氧基苯甲醛];3,4-亚甲基二氧苯甲醛;3,4-二甲氧基苯甲醛;4-羟基苯甲醛;2-甲氧基苯甲醛;苯甲醛;肉桂醛[3-苯基-2-丙烯醛];己基肉桂醛;α-甲基肉桂醛;邻-甲氧基肉桂醛;或它们的组合。不受理论的约束,据信一些口臭抑制剂作为“捕集物”,通过与硫醇或硫化物反应并形成气味较弱的产物来发挥作用。在这些口臭抑制剂中,导致口腔护理组合物内不良口味的实例包括例如茴香醛。一般来讲,不认为风味剂是口臭抑制剂。通常与这些口臭抑制剂相关联的不良口味包括化学制品味、塑料味、苦味和/或酸味。
金属盐
口腔护理组合物中的另一种可能组分是金属盐。金属盐功能广泛,从抗微生物剂到灵敏度剂和/或缓冲液。在一个实施方案中,金属盐包括锌盐、亚锡盐、钾盐、铜盐、或它们的组合。在另一个实施方案中,锌盐选自由下列组成的组:氟化锌、氯化锌、碘化锌、氯氟化锌、乙酸锌、六氟合锆酸锌、硫酸锌、乳酸锌、酒石酸锌、葡萄糖酸锌、柠檬酸锌、苹果酸锌、甘氨酸锌、焦磷酸锌、偏磷酸锌、草酸锌、磷酸锌、碳酸锌、氧化锌、以及它们的组合。在另一个实施方案中,锌盐包括氯化锌、柠檬酸锌、葡萄糖酸锌、乳酸锌、氧化锌、或它们的组合。
在另一个实施方案中,钾盐选自由下列组成的组:硝酸钾、柠檬酸钾、草酸钾、碳酸氢钾、乙酸钾、氯化钾、以及它们的组合。在另一个实施方案中,钾盐包括硝酸钾、柠檬酸钾、氯化钾、或它们的组合。
在另一个实施方案中,铜盐选自由下列组成的组:氟化铜、氯化铜、碘化铜、氯氟化铜、乙酸铜、六氟合锆酸铜、硫酸铜、乳酸铜、酒石酸铜、葡萄糖酸铜、柠檬酸铜、苹果酸铜、甘氨酸铜、焦磷酸铜、偏磷酸铜、草酸铜、磷酸铜、碳酸铜、以及它们的组合。在另一个实施方案中,铜盐包括葡萄糖酸铜、乙酸铜、甘氨酸铜、或它们的组合。
在另一个实施方案中,亚锡盐选自由下列组成的组:氟化亚锡、氯化亚锡、碘化亚锡、氯氟化亚锡、乙酸亚锡、六氟合锆酸亚锡、硫酸亚锡、乳酸亚锡、酒石酸亚锡、葡萄糖酸亚锡、柠檬酸亚锡、苹果酸亚锡、甘氨酸亚锡、焦磷酸亚锡、偏磷酸亚锡、草酸亚锡、磷酸亚锡、碳酸亚锡、葡萄糖酸亚锡、以及它们的组合。在另一个实施方案中,亚锡盐包括氟化亚锡、氯化亚锡、二水氯化亚锡、氟化亚锡、乳酸亚锡、葡萄糖酸亚锡、硫酸亚锡、或它们的组合。
包含亚锡盐(尤其是氟化亚锡和氯化亚锡)的洁齿剂描述于授予Majeti等人的美国专利5,004,597中。亚锡盐的其它描述可见于授予Prencipe等人的美国专利5,578,293和授予Lukacovic等人的美国专利5,281,410中。除了亚锡离子源以外,还可包含稳定亚锡所需的其它成分,如Majeti等人和Prencipe等人所描述的成分。
提供不良口味的金属盐的实例包括氯化锌、柠檬酸锌、葡萄糖酸铜、葡萄糖酸锌、或它们的组合。与这些金属盐相关联的不良口味为臭味、干味、泥土味、金属味、酸味、苦味和涩味。
在一个实施方案中,金属盐的量按所述口腔护理组合物的重量计为约0.05%至约11%。在其它实施方案中,金属盐的量为约0.5至约7%,或约1%至约5%。在其它实施方案中,亚锡盐的量按所述口腔护理组合物的重量计为约0.1至约7%,或约1%至约5%,或约1.5%至约3%。在某些实施方案中,本发明中使用的锌盐或铜盐的量可在约0.01至约5%的范围内。在其它实施方案中,锌盐或铜盐的量为约0.05至约4%或约0.1至约3.0%。
杂项
除上述组分之外,口腔护理组合物中可包括其它组分以获得期望的有益效果。这些杂项组分包括例如螯合剂、研磨剂、流涎剂、填充剂、溶剂、润肤剂、折光颗粒(例如云母)、增稠剂、以及天然组分的提取物。
所述口腔护理组合物及其组分可包含如本文所公开的成分和特性的任何组合。
实施例消费者测试I
为了说明加入TRPV1激活因子和/或浓馥香兰素对口腔护理组合物感知口味的效应,制备以下组合物并提供消费者样品。
对照物 | +VBE | +浓馥香兰素 | +姜油酮 | |
二水合柠檬酸锌 | 0.79 | 0.79 | 0.79 | 0.79 |
柠檬酸三钠,二水 | 0.27 | 0.27 | 0.27 | 0.27 |
氟化钠 | 0.24 | 0.24 | 0.24 | 0.24 |
氯化亚锡二水合物 | 0.21 | 0.21 | 0.21 | 0.21 |
山梨醇(70%) | 45.00 | 45.00 | 45.00 | 45.00 |
糖精钠 | 0.25 | 0.25 | 0.25 | 0.25 |
浓馥香兰素 | 0.04 | |||
姜油酮 | 0.04 | |||
VBE | 0.003 | |||
羟乙基纤维素250M | 0.30 | 0.30 | 0.30 | 0.30 |
羧甲基纤维素钠 | 1.30 | 1.30 | 1.30 | 1.30 |
角叉菜胶混合物 | 0.70 | 0.70 | 0.70 | 0.70 |
二氧化钛,锐钛矿 | 0.53 | 0.53 | 0.53 | 0.53 |
无定形二氧化硅水合物Z119 | 17.00 | 17.00 | 17.00 | 17.00 |
烷基硫酸钠(28%) | 5.00 | 5.00 | 5.00 | 5.00 |
风味剂 | 1.00 | 1.00 | 1.00 | 1.00 |
水,纯化的,USP | 适量 | 适量 | 适量 | 适量 |
通过真空混合制备对照洁齿剂基料(即除风味剂之外的所有组分)。在第二步中加入风味剂,快速混合以完成所述对照物。然后通过将TRPV1激活因子和/或浓馥香兰素加风味剂以所述含量快速混合加入对照基料中制备附加组合物。然后将所述样品置于管中并递送到测试装置中。
在测试装置中,向专门小组成员提供带1.0g牙膏的普通牙刷。每个专门小组成员有一个单独的盥洗池、镜子、一次性杯子和纸巾。要求他们以居家时的正常方式刷牙。在刷牙前和刷牙后专门小组成员将回答一系列与他们对牙膏的体验有关的问题。要求专门小组成员在刷牙后即时以及随后三个小时内每小时评价他们的体验。将消费者的评价转换成数值进行比较。下文显示上文组合物与坏味和不良余味有关的结果。
对照物 | +VBE | +姜油酮 | +浓馥香兰素 | |
坏味(1小时) | 2.5 | 0.8 | 1.1 | 1.5 |
坏味(2小时) | 1.2 | 0.4 | 0.6 | 0.7 |
坏味(3小时) | 0.7 | 0.3 | 0.4 | 0.4 |
不良余味(1小时) | 2.4 | 1.0 | 1.8 | 1.5 |
不良余味(2小时) | 1.0 | 0.4 | 0.5 | 0.9 |
不良余味(3小时) | 0.5 | 0.2 | 0.3 | 0.5 |
从上表中可以看出,每种TRPV1激活因子(VBE和姜油酮)在1-3小时中的每个小时显示比对照物改善的坏味和不良余味,而浓馥香兰素在1-3小时显示比对照物改善的坏味,在1-2小时显示比对照物改善的不良余味。
上文测试中也包括TRPV1激活因子和/或浓馥香兰素的组合。下文是用于这些测试的制剂,并且对照物与上文列出的对照物相同。
下文显示上述组合物的结果。
从上文结果中可以看出,TRPV1激活因子和/或浓馥香兰素的不同组合在全部1-3小时显示比对照物改善的坏味和不良口味,不同的是所有3个组分的组合,其在第3小时显示等同的口味。因此,当与上述单个TRPV1激活因子或浓馥香兰素的结果比较时,取决于所用的测量方法,虽然VBE趋于在第1小时提供最好的结果,一些组合在第2小时和第3小时提供较好的结果。然而令人感兴趣的是,浓馥香兰素、姜油酮和VBE的组合虽然在测试中未得到减轻坏味或不良余味的最好结果,其似乎比尝试的其它组合具有消费者优选的口味。因此,虽然它在减轻不良口味方面并非最好,但消费者似乎更喜欢它。
对用VBE和长时凉爽剂制备的漱口液进行的附加专门小组测试显示包含VBE的组合物提供时间较长的愉悦感官体验,将其描述为较小的酸味和清爽感。由于VBE,用CPC和较低含量乙醇制备的漱口液仍能够提供乙醇样的清洁信号。
实施例产品I-包含金属盐的洁齿剂
使用常规方法制备洁齿剂并在下文中以重量%显示其量。
成分 | IA | IB | IC | ID | IE |
碳酸钙 | 40.00 | ||||
粘结剂 | 1.00 | 1.8 | 1.00 | 1.00 | 0.20 |
增稠剂 | 2.00 | 1.00 | 1.25 | 0.4 | 0.8 |
有色溶液(1%) | 0.05 | 0.05 | 0.175 | ||
二水合磷酸氢钙 | 35.00 | ||||
1.00 | 1.00 | 1.00 | 1.00 | 1.00 | |
凉爽剂 | 0.03 | 0.24 | 0.20 | 0.50 | 0.58 |
VBE | 0.01 | 0.01 | 0.01 | 0.01 | 0.01 |
甘油USP | 16.489 | 15.00 | |||
泊洛沙姆407,NF | 0.20 | ||||
正磷酸单钠 | |||||
硝酸钾 | 5.00 | ||||
糖精钠USP | 0.47 | 0.25 | 0.30 | 0.300 | 0.58 |
二氧化硅研磨剂 | 24.00 | 12.50 | 17.00 | ||
月桂基硫酸钠(27.9%的溶液) | 7.50 | 7.00 | 5.50 | 7.00 | 4.00 |
50%NaOH溶液 | 1.00 | ||||
单氟磷酸钠 | 0.76 | 0.76 | 0.76 | 0.76 | |
氟化钠 | 0.32 | ||||
葡萄糖酸钠 | 1.00 | ||||
氯化亚锡二水合物 | 1.00 | ||||
柠檬酸锌 | 0.50 | ||||
磷酸三钠 | 3.20 | ||||
湿润剂 | 10.50 | 33.00 | 12.00 | 14.00 | 57.00 |
无水焦磷酸四钠 | 0.50 | 0.50 | 3.85 | ||
酸式焦磷酸钠 | 1.00 | ||||
二氧化钛 | 0.50 | 0.50 | 0.25 | ||
水,纯化的,USP | 适量 | 适量 | 适量 | 适量 | 适量 |
1风味剂包含约31.3%的薄荷醇,提供约500ppm的薄荷醇。
实施例产品II-漱口水组合物
漱口水组合物使用常规的方法来制备,并且组分量以重量百分比(%)示于下文中。
成分 | IIA | IIB | IIC |
乙醇,USP 190度 | 15.000 | 15.000 | 15.000 |
甘油 | 7.500 | 7.500 | 7.500 |
聚山梨酸酯80,NF | 0.120 | 0.120 | 0.120 |
风味剂 | 0.160 | 0.160 | 0.160 |
糖精钠 | 0.067 | 0.067 | 0.060 |
有色溶液 | 0.040 | 0.040 | 0.040 |
实施例产品III-过氧化物漱口水组合物
下文示出了包含过氧化物的漱口水组合物,组分量以重量百分比(%)表示。使用常规的方法制备这些组合物。所述漱口水组合物在使用期间提供令人愉快的高效力的薄荷味道和显著的长效清新的口气。
实施例产品IV-牙垢控制洁齿剂组合物
使用常规方法制备洁齿剂并在下文中以重量%显示其量。
本文所公开的量纲和值不旨在被理解为严格地限于所述的精确值。相反,除非另外指明,每个这样的量纲是指所引用的数值和围绕该数值的功能上等同的范围。例如,公开为“40mm”的量纲旨在表示“约40mm”。
除非明确地排除或以其它方式限制,本文所引用的每个文献,包括任何交叉引用或相关的专利或专利申请,均以引用方式全文并入本文。对任何文献的引用均不是承认其为本文公开的或受权利要求书保护的任何发明的现有技术、或承认其独立地或以与任何其它一个或多个参考文献的任何组合的方式提出、建议或公开任何此类发明。此外,如果此文献中术语的任何含义或定义与任何以引用方式并入本文的文献中相同术语的任何含义或定义相冲突,将以此文献中赋予那个术语的含义或定义为准。
虽然已经举例说明和描述了本发明的具体实施方案,但是对于本领域技术人员来说显而易见的是,在不背离本发明实质和范围的情况下可以做出多个其它改变和变型。因此,有意识地在附加的权利要求书中包括属于本发明范围内的所有这些变化和修改。
Claims (1)
1.一种用于改善口腔护理组合物口味的方法,所述方法包括:
混合浓馥香兰素、TRPV1激活因子和坏味剂以形成口腔护理组合物,所述坏味剂选自口臭抑制剂,所述TRPV1激活因子选自以下各项组成的组:姜油酮、姜烯酚、姜醇、或它们的组合,其中所述TRPV1激活因子的加入量按所述口腔护理组合物重量计为0.0001%至0.1%,且所述口臭抑制剂选自由下列组成的组:铜盐;抗坏血酸[3-氧代-L-古洛呋喃内酯];顺式茉莉酮[3-甲基-2-(2-戊烯基-2-环戊烯酮];2,5-二甲基-4-羟基-3(2H)-呋喃酮;5-乙基-3-羟基-4-甲基-2(5H)-呋喃酮;香草醛[4-羟基-3-甲氧基苯甲醛];乙基香草醛;茴香醛[4-甲氧基苯甲醛];3,4-亚甲基二氧苯甲醛;3,4-二甲氧基苯甲醛;4-羟基苯甲醛;2-甲氧基苯甲醛;苯甲醛;肉桂醛[3-苯基-2-丙烯醛];己基肉桂醛;α-甲基肉桂醛;邻-甲氧基肉桂醛;以及它们的组合;
还包括混合一种增强剂,所述增强剂包含二氢大马酮、丁酸香叶酯、2-辛酮、糠醛、紫罗酮、2,6-二甲基-5-庚烯醛、焦磷酸四钠、乙酸α-二甲基苯乙酯、苯乙醛二甲醛、加菲力士(kephalis)、氧化芳樟醇、乙酸香芹酯、金合欢烯、反式-2-己烯乙酸酯、庚醇、或它们的组合。
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- 2010-04-21 RU RU2011139520/15A patent/RU2011139520A/ru unknown
- 2010-04-21 CA CA2760445A patent/CA2760445C/en active Active
- 2010-04-21 PL PL10719464T patent/PL2424621T3/pl unknown
- 2010-04-21 WO PCT/US2010/031852 patent/WO2010126753A2/en active Application Filing
- 2010-04-21 CA CA2812028A patent/CA2812028C/en active Active
- 2010-04-21 AU AU2010241937A patent/AU2010241937B2/en not_active Ceased
- 2010-04-21 ES ES10719464T patent/ES2897730T3/es active Active
- 2010-04-21 BR BRPI1015387A patent/BRPI1015387A2/pt not_active IP Right Cessation
- 2010-04-21 CN CN201080018058.9A patent/CN102612385B/zh not_active Expired - Fee Related
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BRPI1015387A2 (pt) | 2016-04-19 |
RU2011139520A (ru) | 2013-06-10 |
CA2812028A1 (en) | 2010-11-04 |
PL2424621T3 (pl) | 2022-01-03 |
EP2424621A2 (en) | 2012-03-07 |
WO2010126753A3 (en) | 2012-08-16 |
EP2424621B1 (en) | 2021-11-03 |
KR20120002533A (ko) | 2012-01-05 |
US20150125405A1 (en) | 2015-05-07 |
CA2760445A1 (en) | 2010-11-04 |
MX2011011513A (es) | 2011-11-18 |
AU2010241937B2 (en) | 2015-01-22 |
US20100278991A1 (en) | 2010-11-04 |
JP2012524792A (ja) | 2012-10-18 |
CA2812028C (en) | 2016-06-07 |
CN102612385A (zh) | 2012-07-25 |
US8962057B2 (en) | 2015-02-24 |
AU2010241937A1 (en) | 2011-11-17 |
WO2010126753A2 (en) | 2010-11-04 |
JP5705829B2 (ja) | 2015-04-22 |
CA2760445C (en) | 2014-04-01 |
ES2897730T3 (es) | 2022-03-02 |
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