CN1154471C - 减少洁牙剂组合物中亚锡涩味的方法 - Google Patents
减少洁牙剂组合物中亚锡涩味的方法 Download PDFInfo
- Publication number
- CN1154471C CN1154471C CNB998137774A CN99813777A CN1154471C CN 1154471 C CN1154471 C CN 1154471C CN B998137774 A CNB998137774 A CN B998137774A CN 99813777 A CN99813777 A CN 99813777A CN 1154471 C CN1154471 C CN 1154471C
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- Prior art keywords
- polyphosphate
- composition
- stannous
- dentifrice
- dentifrice composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
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- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 claims abstract description 24
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- 239000008365 aqueous carrier Substances 0.000 claims abstract description 17
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Abstract
本发明公开了减少含亚锡洁牙剂组合物涩味的方法,该方法包括给予对象一种含亚锡的洁牙剂组合物。该洁牙剂组合物包含亚锡离子、泊洛沙姆和水性载体。泊洛沙姆没有降低含亚锡洁牙剂组合物的效力。洁牙剂组合物还可含有多磷酸盐,只要含水量有限,且亚锡离子不由氟化亚锡提供。多磷酸盐也不会降低亚锡的效力。或者,洁牙剂组合物可以是双相组合物。第一洁牙剂组合物含有平均链长度约为4或更高的多磷酸盐,并且含水量低,而第二洁牙剂组合物含有亚锡离子。在双相组合物中,泊洛沙姆可存在于第一或第二洁牙剂组合物或两种组合物中。多磷酸盐和泊洛沙姆均不会降低亚锡的效力。
Description
相关申请交叉文献
本申请是1996年11月21日提交的申请No.08/754,577的部分续展申请。
发明背景
本发明涉及一种减少含亚锡洁牙剂组合物涩味的方法。本发明者已经发现,利用泊洛沙姆可以减少与亚锡有关的涩味、苦味和酸味。还发现某些多磷酸盐,尤其是平均链长度约为4或更高的线状多磷酸盐也有助于减少亚锡的涩味。泊洛沙姆或多磷酸盐减少涩味,但不降低亚锡的效力。
术语“亚锡”在本文中定义为在洁牙剂中的亚锡。它可以指由亚锡盐提供的亚锡离子。含有亚锡离子的亚锡盐是众所周知的。发现亚锡能提供防止牙龈炎和抗噬斑的优点。另外,亚锡还可有助于改善呼吸,降低敏感性。还知道含有亚锡的洁牙剂引起对象牙齿表面上染色,并具有涩的感觉。在使用该产品后,涩味是最值得注意的。美国专利5,780,015描述了用氢化蓖麻油的氧乙基化反应产物来帮助减少涩味。为了提高消费者对含有亚锡的洁牙剂组合物的接受程度,需要具有亚锡优点但没有涩味的其它洁牙剂组合物。
本发明的目的是提供一种通过给予对象含亚锡的洁牙剂组合物来减少含有亚锡的洁牙剂组合物涩味的方法。该洁牙剂组合物含有亚锡离子、泊洛沙姆和水性载体。泊洛沙姆不会使这种含有亚锡的洁牙剂组合物的效果减少。只要洁牙剂含水量低,不含氟化亚锡作为亚锡离子来源,洁牙剂组合物还可含有多磷酸盐。多磷酸盐也不会降低亚锡的效力。或者,该洁牙剂组合物可以是双相组合物。第一洁牙剂组合物含有平均链长度约为4或更高的多磷酸盐,并且含水量低,第二洁牙剂组合物含有亚锡离子。泊洛沙姆可存在于第一或第二洁牙剂组合物或两种组合物中。
本发明的这些和其它目的可从下文的详细描述明显看出。
本文所用的所有百分数均以具体洁牙剂组合物的重量计,除非另有特指。本文所用的比例是总组合物的摩尔比,除非另有特指。所有测定在25℃下进行,除非另有特指。
发明概述
本发明涉及减少含亚锡洁牙剂组合物涩味的方法,该方法包括给予对象含有亚锡的洁牙剂组合物。该洁牙剂组合物包含亚锡离子、泊洛沙姆和水性载体。泊洛沙姆不会使含有亚锡的该洁牙剂组合物的效力下降。只要洁牙剂含水量有限,亚锡离子不由氟化亚锡提供,洁牙剂组合物还可含有多磷酸盐。多磷酸盐也不会降低亚锡的效力。或者,该洁牙剂组合物可以是双相组合物。第一洁牙剂组合物含有平均链长度约为4或更高的多磷酸盐,并且含水量有限,而第二洁牙剂组合物含有亚锡离子。在双相组合物中,泊洛沙姆可存在于第一或第二洁牙剂组合物或两种组合物中。多磷酸盐和泊洛沙姆均不会减少亚锡的效果。
具体而言,本发明提供了一种减少含亚锡洁牙剂组合物涩味的方法,该方法包括在所述洁牙剂组合物中加入泊洛沙姆,使得该组合物包含:
a.3000ppm-15000ppm的亚锡离子;
b.占组合物重量5%-50%的泊洛沙姆;和
c.占组合物重量40%-95%的水性载体,且所述组合物中的各组分重量百分数之和为100%重量;其中泊洛沙姆没有减少洁牙剂中亚锡离子的效力。
发明详述
本发明的经口配方可以是牙膏或洁牙剂形式。本文所用的术语“洁牙剂”指软膏、凝胶或液体配方,除非另有特指。洁牙剂组合物可以是任何所需要的形式,如深色条纹、表面带条纹、多层、周围包有凝胶的软膏,或这些形式的任何组合。
各种洁牙剂组合物可以是单相洁牙剂,或可以是双相洁牙剂的一部分,并包含在配料器物理上分开的区室内并并排配料。本文所用的术语“配料器”指适用于配送牙膏的泵、管或容器。
洁牙剂组合物是一种产品,在正常使用时,并不是以将其吞咽来给予全身特定治疗剂为目的,而是由对象将其含在口腔内足够长的时间,以使其与基本上所有牙表面和/或口腔组织充分接触的口腔活性为目的。
本文所用的术语“水性载体”指用于本发明组合物的任何安全有效的材料。这些材料包括氟离子来源、防牙垢剂、抗菌剂、研磨抛光材料、过氧化物源、碱金属碳酸氢盐、增稠材料、润湿剂、水、表面活性剂、缓冲剂、二氧化钛、调味系统、增甜剂、着色剂及其混合物。
本文所用的术语“减少”指统计学上显著的减少。因此,减少含亚锡洁牙剂组合物涩味是指对象所注意到的涩味水平比对照物有统计学上显著的减少。亚锡效力没有减少是指亚锡的效力没有比对照物有统计学上显著的减少。含有亚锡的对照产品可以是Crest Gum Care。
本发明组合物包含必需组分和任选组分。下段描述了本发明组合物的必需组分和任选组分。
亚锡离子
本发明包括亚锡离子。亚锡离子通常来自加入洁牙剂的亚锡盐。已经发现,亚锡有助于减少牙龈炎、噬斑、敏感性,并具有改善呼吸的优点。洁牙剂组合物中的亚锡会为使用该洁牙剂的对象提供效果。“效果”定义为经噬斑糖酵解再生模型(PGRM)测得的牙龈炎减少的显著量。本发明者已经发现有一种方法可减少亚锡引起的涩味,同时防止亚锡的效力降低。具体地说,使用泊洛沙姆或多磷酸盐不会降低亚锡的效力,即使它们能各自降低亚锡的涩味。因此,亚锡的效力维持在一种能减少牙龈炎的含亚锡洁牙剂(如Crest Gum Care)中所见的水平上。还发现平均链长度约为4或更高的多磷酸盐也有助于减少亚锡引起的染色。
洁牙剂组合物中含有有效量的亚锡离子。有效量定义为约为3000ppm到15000ppm。亚锡低于3000ppm,则亚锡的效力不显著。较佳的,亚锡离子的含量约为5000ppm到13000ppm,更佳的约为7000ppm到10000ppm。这是输送给口腔的亚锡离子的总量。
含有亚锡盐、尤其是氟化亚锡和氯化亚锡的洁牙剂公开在美国专利5,004,597(授予Majeti等人)中,该专利全部纳入本文作为参考。关于亚锡盐洁牙剂的其它描述见美国专利5,578,293和5,578,293。较佳的亚锡盐是氟化亚锡和二水合氯化亚锡。其它亚锡盐包括乙酸亚锡。合并的亚锡盐将占最终组合物重量的大约0.25%-11%。较佳的,亚锡盐的含量为大约0.5-7%,更佳的约为1-5%,最佳的约为1.5-4%。
泊洛沙姆
泊洛沙姆(Poloxamer)分类为非离子表面活性剂。它还具有作为乳化剂、粘合剂、稳定剂的功能和其它有关的功能。泊洛沙姆是双官能嵌段聚合物,其末端为伯羟基,分子量范围为1000至高于15000。泊洛沙姆由BASF以Pluronics的商品名出售。对于本发明最佳的泊洛沙姆是泊洛沙姆407。为了对亚锡涩味有可测定的影响,泊洛沙姆的含量必须约为5%或更高。涩味减少是在对象用洁牙剂组合物刷牙后由对象提供的味道、回味和涩味评价来测定的。
泊洛沙姆的含量约为组合物重量的5%-50%,较佳的约为6%-30%,更佳的约为7%-20%,最佳的约为8%-18%。或者,可用泊洛沙姆含量约为10%或更高以及约为15%或更高的组合物。如果使用双相洁牙剂,则泊洛沙姆的总量可以来自在一相内的所有泊洛沙姆,或来自分在两相内的泊洛沙姆。
多磷酸盐来源
本发明还包括多磷酸盐来源。已知多磷酸盐有助于延迟牙垢的形成。除了延迟牙垢形成,本发明者还发现平均链长度约为4或更高的多磷酸盐也能帮助减少亚锡盐的涩味。为了产生含有多磷酸盐的稳定有效的组合物,该多磷酸盐必须在含水量低的组合物中,以防止多磷酸盐水解。如果亚锡盐和多磷酸盐在同一相内或在分开的相内且仅在一旦配送到牙刷上时互相作用,则会减少涩味。泊洛沙姆也可以和多磷酸盐或亚锡盐在同一相内,或所有这三种组分在同一相内。如果氟化亚锡是该亚锡盐,则氟化物会和多磷酸盐反应。该反应会形成单氟磷酸,从而抑制氟化物的效力,也会抑制多磷酸盐抗牙石的效果。因此,为了提供有效的配方,多磷酸盐和氟化亚锡应在分开的相中。如果亚锡盐不是氟化亚锡,则亚锡盐和多磷酸盐可在同一相内。
出人意料的是,平均链长度约为4或更高的多磷酸盐将提供这种有利的效果。以前已经发现,焦磷酸盐会与亚锡盐反应并形成难溶的盐。这将抑制亚锡盐的效力以及焦磷酸盐的抗牙石作用。因此,较长链长度的多磷酸盐具有减少亚锡盐涩味的有益效果是出人意料的。
多磷酸盐通常被理解成由主要以线状构型排列的两个或多个磷酸盐分子组成(但是也可能存在一些环状衍生物)。尽管焦磷酸盐是一种多磷酸盐,但是所需的多磷酸盐是有四个或更多磷酸分子的那些。对焦磷酸盐分开进行讨论。所需的无机多磷酸盐中包括四聚磷酸盐和六偏磷酸盐。大于四聚磷酸盐的多磷酸盐通常以非晶形玻璃态物质形式存在。本发明中较佳的是有下式的线状“玻璃态”多磷酸盐:
XO(XPO3)nX
其中X是钠或钾,n在大约6-125之间,较佳的在6-21之间。较佳的多磷酸盐是FMCCorporation生产的商品名为Sodaphos(n约为6)、Hexaphos(n约为13)、Glass H(n约为21)的多磷酸盐。这些多磷酸盐可单独或组合使用。
磷酸盐来源在Kirk & Othmer,Encyclopeida of Chemical Technology,第四版,18卷,Wiley-Interscience Publishers(1996)中有更详细的描述,这些内容以及结合到Kirk&Othmer的所有参考文献均全部纳入本文作参考。多磷酸盐来源通常约占洁牙剂组合物重量的1-20%,较佳的约3-17%,更佳的约4-15%,最佳的约5-13%。
为了使多磷酸盐具有减少亚锡涩味的有益效果,还应控制多磷酸盐阴离子总摩尔和亚锡离子总摩尔之比。该比值在大约0.2∶1至5∶1之间,较佳的在大约0.5∶1至3∶1之间,更佳的在大约0.6∶1至2∶1之间,最佳的在0.7∶1至1.5∶1之间。
水性载体
在制备本发明组合物时,希望在组合物中加入一种或多种水性载体。这些物质是本领域中熟知的,本领域技术人员很容根据待制备组合物所需的物理和美学性能来选择。水性载体通常占洁牙剂组合物重量的约40-99%,较佳的约占40-90%,较佳的约占60-98%,更佳的约占75-97%,最佳的约占90-95%。
总含水量
用于制备适合市售的经口组合物的水应最好含有低含量的离子,且不含有机杂仅在一旦配送到牙刷上时互相作用,则会减少涩味。泊洛沙姆也可以和多磷酸盐或亚锡盐在同一相内,或所有这三种组分在同一相内。如果氟化亚锡是该亚锡盐,则氟化物会和多磷酸盐反应。该反应会形成单氟磷酸,从而抑制氟化物的效力,也会抑制多磷酸盐抗牙石的效果。因此,为了提供有效的配方,多磷酸盐和氟化亚锡应在分开的相中。如果亚锡盐不是氟化亚锡,则亚锡盐和多磷酸盐可在同一相内。
出人意料的是,平均链长度约为4或更高的多磷酸盐将提供这种有利的效果。以前已经发现,焦磷酸盐会与亚锡盐反应并形成难溶的盐。这将抑制亚锡盐的效力以及焦磷酸盐的抗牙石作用。因此,较长链长度的多磷酸盐具有减少亚锡盐涩味的有益效果是出人意料的。
多磷酸盐通常被理解成由主要以线状构型排列的两个或多个磷酸盐分子组成(但是也可能存在一些环状衍生物)。尽管焦磷酸盐是一种多磷酸盐,但是所需的多磷酸盐是有四个或更多磷酸分子的那些。对焦磷酸盐分开进行讨论。所需的无机多磷酸盐中包括四聚磷酸盐和六偏磷酸盐。大于四聚磷酸盐的多磷酸盐通常以非晶形玻璃态物质形式存在。本发明中较佳的是有下式的线状“玻璃态”多磷酸盐:
XO(XPO3)nX
其中X是钠或钾,n在大约6-125之间,较佳的在6-21之间。较佳的多磷酸盐是FMCCorporation生产的商品名为Sodaphos(n约为6)、Hexaphos(n约为13)、Glass H(n约为21)的多磷酸盐。这些多磷酸盐可单独或组合使用。
磷酸盐来源在Kirk & Othmer,Encyclopeida of Chemical Technology,第四版,18卷,Wiley-Interscience Publishers(1996)中有更详细的描述,这些内容以及结合到Kirk&Othmer的所有参考文献均全部纳入本文作参考。多磷酸盐来源通常约占洁牙剂组合物重量的1-20%,较佳的约3-17%,更佳的约4-15%,最佳的约5-13%。
为了使多磷酸盐具有减少亚锡涩味的有益效果,还应控制多磷酸盐阴离子总摩尔和亚锡离子总摩尔之比。该比值在大约0.2∶1至5∶1之间,较佳的在大约0.5∶1至3∶1之间,更佳的在大约0.6∶1至2∶1之间,最佳的在0.7∶1至1.5∶1之间。
水性载体
在制备本发明组合物时,希望在组合物中加入一种或多种水性载体。这些物质是本领域中熟知的,本领域技术人员很容根据待制备组合物所需的物理和美学性能来选择。水性载体通常占洁牙剂组合物重量的约40-99%,较佳的约占40-95%,较佳的约占60-98%,更佳的约占75-97%,最佳的约占90-95%。
总含水量
用于制备适合市售的经口组合物的水应最好含有低含量的离子,且不含有机杂成有关的磷酸钙矿物沉积的这些物质。包括的试剂是焦磷酸盐、三聚磷酸盐、合成的阴离子聚合物[包括聚丙烯酸酯和马来酸酐或马来酸与甲基乙烯基醚的共聚物(如Gantrez),例如美国专利4,627,977(授予Gaffar等)中描述的,该专利全部纳入本文作参考;以及例如,多氨基丙磺酸(AMPS)]、三水合柠檬酸锌、二膦酸盐类(如EHDP、AHP)、多肽类(如聚天冬氨酸和聚谷氨酸)、及其混合物。
研磨抛光材料
在牙膏组合物中还可加入研磨抛光材料。打算用于本发明组合物的研磨抛光材料可以是不过分磨损牙质的任何材料。典型的研磨抛光材料包括:二氧化硅,包括凝胶和沉淀物;氧化铝;磷酸盐,包括正磷酸盐、多偏磷酸盐和焦磷酸盐;及其混合物。具体的例子包括二水合正磷酸二钙、焦磷酸钙、磷酸三钙、多偏磷酸钙、不溶性多偏磷酸钠、水合氧化铝、β焦磷酸钙、碳酸钙和树脂研磨材料,如脲和甲醛的颗粒状缩合产物,以及Cooley等在美国专利3,070,510(1962年12月25日,纳入本文作参考)中公开的其它物质。也可采用研磨剂混合物。如果洁牙剂组合物或特定的相包含平均链长度约为4或更高的多磷酸盐,则含钙的研磨剂或氧化铝不是较佳的研磨剂。最佳的研磨剂是氧化硅。
各种二氧化硅牙用研磨剂是较佳的,因为它们独特的优点是能提供优良的清洁和磨光牙齿的性能且不会过度地磨损牙釉质或牙质。这里的二氧化硅研磨抛光材料以及其它研磨剂的平均颗粒大小通常在约0.1-30微米间,较佳的在5-15微米间。研磨剂可以是沉淀二氧化硅或二氧化硅凝胶,如Pader等的美国专利3,538,230(1970年3月2日授权)和DiGiulio的美国专利No.3,862,307(1975年1月21日授权)中描述的二氧化硅干凝胶,这些专利均纳入本文作参考。较佳的是W.R.Grace & Company,DavisonChemical Division出售的商品名“Syloid”的二氧化硅干凝胶。沉淀二氧化硅也是较佳的,如由J.M.Huber Corporation以商品名“Zeodent”出售的那些,尤其是名称为“Zeodent 119”的二氧化硅。用于本发明牙膏中的二氧化硅研磨剂的类型在Wason等的美国专利No.4,340,583(1982年7月29日授权)中有所描述,该专利纳入本文作参考。Rice的美国专利5,589,160;5,603,920;5,651,958;5,658,553以及5,716,601中均描述了二氧化硅研磨剂,这些专利也纳入本文作为参考。本文所述的牙膏组合物中的研磨剂含量通常约占组合物重量的6-70%。较佳的,牙膏含有的研磨剂约占洁牙剂组合物重量的10-50%。
过氧化物来源
本发明洁牙剂组合物中可包括过氧化物源。过氧化物源选自过氧化氢、过氧化钙、过氧化脲及其混合物。较佳的过氧化物源是过氧化钙。下列用量表示过氧化物原料的量,但是过氧化物源还可含有过氧化物原料外的其它组分。本发明的洁牙剂组合物可含有约占洁牙剂组合物重量0.01-10%,较佳的约占0.1-5%,更佳的约占0.2-3%,最佳的约占0.3-0.8%的过氧化物源。
碱金属碳酸氢盐
本发明还可包括碱金属的碳酸氢盐。碱金属碳酸氢盐可溶于水,除非被稳定化,否则它将在水性系统中释放出二氧化碳。碳酸氢钠(也称为小苏打)是较佳的碱金属碳酸氢盐。碱金属碳酸氢盐还可作为缓冲剂。本发明组合物可含有约占洁牙剂组合物重量0.5-50%,较佳的约占0.5-30%,更佳的约占2-20%,最佳的约占5-18%的碱金属碳酸氢盐。
其它水性载体
本发明的牙膏形式的组合物通常含有一些增稠材料或粘合剂,以提供所需的稠度。较佳的增稠剂是羧乙烯基聚合物、角叉菜胶、羟乙基纤维素和纤维素醚的水溶性盐(如羧甲基纤维素钠和羟乙基纤维素钠)。还可采用天然树胶,如刺梧桐树胶、黄原胶、阿拉伯树胶和黄蓍树胶。胶态硅酸镁铝或细分的二氧化硅可作为增稠剂的一部分,以进一步改善质地。增稠剂的用量可约占洁牙剂组合物重量的0.1-15%。
这里所需的另一任选的组合物组分是润湿剂。润湿剂可防止牙膏组合物暴露在空气下时发生硬化,某些润湿剂还为牙膏组合物提供了所需的甜味。适用于本发明的润湿剂包括甘油、山梨糖醇、聚乙二醇、丙二醇、木糖醇和其它可食的多元醇。润湿剂通常约占组合物重量的0-70%,较佳的约占15-55%。
本发明组合物还可包含表面活性剂(通常也称为起泡剂)。除了非离子表面活性剂泊洛沙姆外,表面活性剂也可掺入本发明的洁牙剂组合物中。合适的表面活性剂是在较宽pH范围内相当稳定且起泡的那些表面活性剂。表面活性剂可以是阴离子、非离子、两性、两性离子、阳离子型表面活性剂或其混合物。本文所用的阴离子表面活性剂包括水溶性烷基硫酸盐(如烷基硫酸钠)(烷基具有8-20个碳原子)和具有8-20个碳原子的磺化的单脂肪酸甘油酯的水溶性盐。此类阴离子表面活性剂的典型例子是月桂基硫酸钠和椰子单甘油酯磺酸钠。其它合适的阴离子表面活性剂是肌氨酸盐(如月桂酰肌氨酸钠)、牛磺酸盐、月桂基磺基乙酸钠、月桂酰羟乙磺酸钠、月桂醇聚氧乙烯醚(laureth)羧酸钠和月桂基苯磺酸钠。还可采用阴离子表面活性剂的混合物。许多合适的阴离子表面活性剂公开在Agricola等人的美国专利3,959,458(1976年5月25日授权)中,该专利纳入本文作参考。可用于本发明组合物的非离子型表面活性剂可广泛定义成通过烯化氧基团(特征是亲水性)与疏水性有机化合物(可以是脂族或烷基-芳族)缩合产生的化合物。合适的非离子型表面活性剂例子包括聚氧乙烯、聚氧乙烯缩水山梨糖醇酯(以Tween的商品名出售)、多元醇40氢化蓖麻油、脂肪醇乙氧基化物、烷基苯酚的聚氧乙烯缩合物、环氧丙烷与乙二胺的反应产物和环氧乙烷缩合衍生获得的产品、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材料的混合物。用于本发明的两性表面活性剂可以广泛描述成脂族仲胺和叔胺的衍生物,其中脂族基团可以是直链或支链,且其中一个脂族取代基含有约8-18个碳原子,一个含有阴离子水溶性基团如羧酸盐、磺酸盐、硫酸盐、磷酸盐或膦酸盐。其它合适的两性表面活性剂是内铵盐,具体是椰油酰胺丙基(cocamidopropyl)内铵盐。还可采用两性表面活性剂的混合物。Gieske等的美国专利4,051,234(1977年9月27日授权)中公开了许多这些合适的非离子和两性表面活性剂,该专利纳入本文作参考。本发明组合物通常包含一种或多种表面活性剂,其含量各自约占组合物重量的0.25-12%,较佳的约0.5-8%,最佳的约1-6%。
本发明组合物中还可加入二氧化钛。二氧化钛是白色粉末,它增加了组合物的不透明度。二氧化钛通常约占组合物重量的0.25-5%。
本发明组合物中还可加入着色剂。着色剂可以是水溶液形式,较佳的是1%的着色剂在水中的溶液。着色液通常约占组合物重量的0.01-5%。
该组合物中还可加入调味系统。合适的调味剂组分包括冬青油、薄荷油、丁香蕾油、薄荷醇、茴香脑、水杨酸甲酯、桉树脑、肉桂皮、乙酸1-酯、鼠尾草、丁子香酚、欧芹油、噁烷酮(oxanone)、α-紫罗兰酮、甘牛至草、柠檬、橙、丙烯基guaethol、肉桂、香草醛、乙基香草醛、天芥菜精、4-顺式-庚烯醛(heptenal)、二乙酰基、乙酸甲基-对-叔丁基苯酯及其混合物。清凉剂也可作为调味系统的一部分。本发明组合物中较佳的清凉剂是对羧酰胺试剂,如N-乙基-对--3-羧酰胺(商业上称“WS-3”)及其混合物。组合物中采用的调味系统通常约占组合物重量的0.001-5%。
组合物中可加入增甜剂。它们包括糖精、葡萄糖、蔗糖、乳糖、麦芽糖、木糖醇、左旋糖、天冬甜素、环己烷氨基磺酸钠、D-色氨酸、二氢查尔酮、丁磺氨及其混合物。本发明中还可掺入各种着色剂。增甜剂和着色剂在牙膏中的用量通常约占组合物重量的0.005-5%。
本发明还包括其它试剂,如抗微生物剂。这些试剂中包括不溶于水的非阳离子抗微生物剂,如卤化的二苯醚、酚类化合物包括苯酚及其同系物、单和多烷基和芳族卤代苯酚、间苯二酚及其衍生物、双酚化合物和卤化的水杨酰苯胺、苯甲酸酯和卤化的N-碳酰苯胺。水溶性抗微生物剂中包括季胺盐和双缩二胍(bis-biquanide)。三氯生单磷酸盐是另一种水溶性抗微生物剂。季铵盐包括季氮上一个或两个取代基的碳链长度(通常是烷基)为8-20,典型为10-18个碳原子,而其余的取代基(通常是烷基或苄基)有较少的碳原子数,例如1-7个碳原子,典型的为甲基或乙基。典型的季铵抗微生物剂例子是:十二烷基三甲基溴化铵、氯化十四烷基吡啶鎓、溴化度米芬、氯化N-十四烷基-4-乙基吡啶鎓、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、氯化十六烷基吡啶鎓、季胺化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。其它化合物是公开在美国专利4,206,215(1980年6月3日授予Bailey)中的双[4-(R-氨基)-1-吡啶鎓]链烷,该专利纳入本文作参考。还可加入其它抗微生物剂,如二甘氨酸铜(copper bisglycinate)、甘氨酸铜(copper glysinate)、柠檬酸锌和乳酸锌。另外可用酶,包括内切糖苷酶、木瓜酶、葡聚糖酶、齿斑葡聚糖酶(mutanase)及其混合物。这些试剂公开在美国专利2,946,725(1960年7月26日授予Norris等)和美国专利4,051,234(1977年9月27日授予Gieske等)中,这些专利纳入本文作参考。具体的抗微生物剂包括洗必太、三氯生、三氯生单磷酸盐和调味油如百里酚。三氯生和其它此类试剂公开在Parran,Jr.等的美国专利5,015,466(1991年5月14日授权)和美国专利4,894,220(1990年1月16日授予Nabi等)中并纳入本文作参考。水不溶性抗微生物剂、水溶性试剂和酶可存在于第一或第二洁牙剂组合物中。季铵试剂、亚锡盐和取代的胍宜在第二洁牙剂组合物中。这些试剂的含量约占洁牙剂组合物的0.01%-1.5%。
洁牙剂组合物可以是软膏、凝胶或其任何构型或组合。如果需要双相洁牙剂组合物,则第一和第二洁牙剂组合物在洁牙剂配料器中是物理上分开的。然后较佳的是,一个洁牙剂组合物是软膏,另一个洁牙剂组合物是凝胶。配料器是适于用来配送牙膏的管、泵或其它任何容器。适用于此目的的双区室袋在美国专利4,528,180(1985年7月9日)、美国专利4,687,663(1987年8月18日)和4,849,213(1989年7月18日,均授予Shaeffer)中有所描述并全部纳入本文作参考。配料器通过一个开口递送大约等量的各洁牙剂组合物。组合物可在配料时互相混合。或者,经口配方可从含两个分开的配料器的试剂盒输送,这两个配料器用来递送同时使用的两种洁牙剂组合物。
治疗方法
本发明涉及减少含亚锡洁牙剂组合物涩味的方法。含有亚锡的洁牙剂组合物通常具有强烈的涩味。使用该洁牙剂的每个对象可能会注意到不同程度的涩味。本发明是一种减少含亚锡洁牙剂组合物用者注意到的涩味水平的方法。该方法可能不能完全消除涩味,但是该方法能显著减少涩味的水平。减少含亚锡组合物涩味的方法包括给予对象含亚锡的洁牙剂组合物。或者,该方法可包括制备含亚锡的洁牙剂组合物,使对象使用含亚锡的洁牙剂组合物。术语“给予”定义为以这样的方式使用洁牙剂,即,使洁牙剂组合物在口腔内停留足够长的时间,使其与基本上所有的牙齿表面和/或口腔组织接触,以发挥其口腔活性。通常,给予是用洁牙剂刷洗,或用洁牙剂料液漱口。对象定义为使用洁牙剂组合物的人或动物。
生产方法和例子
下列实施例进一步描述和证明了在本发明范围内的实施方案。给予这些实施例只是为了描述,它们并不应被理解成限制了本发明,因为在不脱离本发明精神和范围下还可作许多变动。
实施例1
第一洁牙剂组合物 第二洁牙剂组合物
组分 重量% 组分 重量%
羧甲基纤维素 0.700 色料 0.200
水 11.500 水 33.800
调味剂 0.900 调味剂 0.900
甘油 7.000 甘油 41.500
羟乙基纤维素 0.400 泊洛沙姆407 21.00
山梨糖醇 39.596 木糖醇 2.200
十二烷基硫酸钠(a) 6.000 糖精钠 0.400
二氧化硅 28.000
氢氧化钠(b) 0.800
糖精钠 0.400
葡糖酸钠 2.100
氯化亚锡 2.100
氟化亚锡 0.454
(a)27.9%溶液
(b)50%溶液
如下制备第一洁牙剂组合物:在混合容器中加入水、山梨糖醇和糖精,加热至至少50℃。加入葡糖酸钠,混合直至完全溶解。加入氟化亚锡,混合至完全溶液。加入氯化亚锡,混合至完全溶解。加入氢氧化钠,混合至全部中和。将羧甲基纤维素和羟乙基纤维素分散在甘油中。将该甘油淤浆加入混合容器中,充分混合。然后加入二氧化硅。充分混合。将混合容器冷却至低于30℃,加入调味和十二烷基硫酸钠。混合至均一。
如下值得第二洁牙剂组合物:在主要的混合容器中加入水、甘油、糖精和木糖醇,加热至至少60℃。加入泊洛沙姆,色料和调味剂,混合至泊洛沙姆溶解。使批料冷却至低于30℃。
实施例II
第一洁牙剂组合物 第二洁牙剂组合物
组分 重量% 组分 重量%
羧甲基纤维素 0.500 氢氧化钠(b) 1.000
水 2.768 色料 0.300
调味剂 1.000 水 21.840
甘油 36.432 调味剂 1.000
聚乙二醇 1.500 甘油 28.992
丙二醇 8.000 葡糖酸钠 4.160
十二烷基硫酸钠(a) 4.000 氯化亚锡 3.000
二氧化硅 28.000 二氧化硅 23.000
苯甲酸 0.600 糖精钠 0.300
苯甲酸钠 0.600 泊洛沙姆 15.500
糖精钠 0.300 氟化亚锡 0.908
二氧化钛 1.000
黄原胶 0.300
Glass H多磷酸盐 15.000
(a)27.9%溶液
(b)50%溶液
实施例III
第一洁牙剂组合物 第二洁牙剂组合物
组分 重量% 组分 重量%
羧甲基纤维素 0.500 氢氧化钠(b) 0.746
水 2.768 色料 0.300
调味剂 1.000 水 21.840
甘油 32.200 调味剂 1.000
苯甲酸 0.600 甘油 31.016
丙二醇 8.000 葡糖酸钠 3.290
十二烷基硫酸钠(a) 8.000 氯化亚锡 2.100
二氧化硅 19.232 二氧化硅 23.000
多元醇40 2.500 糖精钠 0.300
聚氧乙烯 0.500 氟化亚锡 0.908
糖精钠 0.300 泊洛沙姆407 15.500
二氧化钛 1.000
黄原胶 0.300
Glass H多磷酸盐 21.000
聚乙二醇 1.500
苯甲酸钠 0.600
(a)27.9%溶液
(b)50%溶液
实施例IV
第一洁牙剂组合物 第二洁牙剂组合物
组分 重量% 组分 重量%
羧甲基纤维素 0.500 氯化亚锡 1.200
水 2.768 色料 0.300
调味剂 1.000 水 21.840
甘油 32.200 调味剂 1.000
聚氧乙烯 0.500 甘油 33.032
丙二醇 8.000 葡糖酸钠 2.420
十二烷基硫酸钠(a) 8.000 氢氧化钠(b) 0.500
二氧化硅 22.232 二氧化硅 23.000
多元醇40 2.500 糖精钠 0.300
苯甲酸钠 0.600 泊洛沙姆 15.500
糖精钠 0.300 氟化亚锡 0.908
二氧化钛 1.000
黄原胶 0.300
Glass H多磷酸盐 18.000
聚乙二醇 1.500
苯甲酸 0.600
(a)27.9%溶液
(b)50%溶液
实施例V
第一洁牙剂组合物 第二洁牙剂组合物
组分 重量% 组分 重量%
羧甲基纤维素 0.500 氯化亚锡 1.200
水 4.500 色料 0.300
调味剂 1.000 水 21.840
甘油 32.200 调味剂 1.000
聚氧乙烯 0.500 甘油 33.032
丙二醇 10.000 葡糖酸钠 2.420
十二烷基硫酸钠(a) 6.000 氢氧化钠(b) 0.500
二氧化硅 25.000 二氧化硅 23.000
泊洛沙姆407 3.000 糖精钠 0.300
苯甲酸钠 0.600 泊洛沙姆 15.500
糖精钠 0.300 氟化亚锡 0.908
二氧化钛 1.000
黄原胶 0.300
Glass H多磷酸盐 12.000
聚乙二醇 2.500
苯甲酸 0.600
(a)27.9%溶液
(b)50%溶液
如下制得实施例II、III、IV和V。制备第一洁牙剂组合物:将水、苯甲酸钠和糖精加入混合容器中。将羧甲基纤维素、黄原胶和聚氧乙烯(如果使用的话)分散到甘油中。将该甘油浆料加入混合容器中,充分混合,加热至至少40℃。将苯甲酸溶解在调味剂、丙二醇、泊洛沙姆(如果用的话)、十二烷基硫酸钠和聚乙二醇的混合物中,然后加入混合容器中。然后加入二氧化钛和二氧化硅。充分混合。将混合容器冷却至低于30℃,加入多磷酸盐。混合至均一。
如下制得第二洁牙剂组合物。将水、色料和甘油加入主要的混合容器中,加热至至少50℃。加入葡糖酸钠,混合至完全溶解。加入氟化亚锡,混合至完全溶解。加入氯化亚锡,混合至完全溶解。加入氢氧化钠、糖精和二氧化硅,充分混合。加入泊洛沙姆、调味剂,混合至泊洛沙姆溶解。冷却该批料至低于30℃。
实施例VI
组分 重量%
氟化亚锡 0.454
水 21.866
调味剂 1.000
甘油 29.000
泊洛沙姆407 15.500
氯化亚锡 1.500
十二烷基硫酸钠(a) 4.000
二氧化硅 23.000
氢氧化钠(b) 1.000
葡糖酸钠 2.080
糖精钠 0.300
色料 0.300
(a)27.9%溶液
(b)50%溶液
如下制得实施例VI:在混合容器中加入水、色料、甘油和糖精。加热至至少50℃。加入葡糖酸钠,混合至完全溶解。加入氟化亚锡,混合至完全溶解。加入氯化亚锡,混合至完全溶解。加入氢氧化钠,混合至完全中和。然后加入二氧化硅并充分混合。加入泊洛沙姆和调味剂,混合至泊洛沙姆溶解。将混合容器冷却至低于30℃,加入十二烷基硫酸钠。混合至均一。
实施例VII
组分 重量%
氟化亚锡 0.454
水 21.466
调味剂 1.000
甘油 12.000
泊洛沙姆407 8.000
氯化亚锡 1.500
十二烷基硫酸钠(a) 4.000
二氧化硅 29.000
氢氧化钠(b) 0.800
葡糖酸钠 2.080
羟乙基纤维素 0.300
黄原胶 0.400
聚乙二醇 3.000
聚氧乙烯 0.500
山梨糖醇 14.500
糖精钠 0.400
二氧化钛 0.600
(a)27.9%溶液
(b)50%溶液
如下制得实施例VII:在混合容器中加入水、山梨糖醇和糖精。加热至至少50℃。加入葡糖酸钠,混合至完全溶解。加入氟化亚锡,混合至完全溶解。加入氯化亚锡,混合至完全溶解。加入氢氧化钠,混合至完全中和。将羟乙基纤维素、黄原胶和聚氧乙烯分散在甘油和聚乙二醇中。将该浆液加入混合容器中,充分混合。然后加入二氧化硅和二氧化钛并充分混合。加入泊洛沙姆、调味剂,混合至泊洛沙姆溶解。将混合容器冷却至低于30℃,加入十二烷基硫酸钠。混合至均一。
实施例VIII
组分 重量%
氟化亚锡 0.454
水 29.566
调味剂 1.000
甘油 37.700
泊洛沙姆407 22.000
氯化亚锡 1.500
十二烷基硫酸钠(a) 4.000
氢氧化钠(b) 1.000
葡糖酸钠 2.080
糖精钠 0.400
色料 0.300
(a)27.9%溶液
(b)50%溶液
如下制得实施例VIII:在混合容器中加入水、色料、甘油和糖精。加热至至少50℃。加入葡糖酸钠,混合至完全溶解。加入氟化亚锡,混合至完全溶解。加入氯化亚锡,混合至完全溶解。加入氢氧化钠,混合至完全中和。加入泊洛沙姆和调味剂,混合至泊洛沙姆溶解。将混合容器冷却至低于30℃,加入十二烷基硫酸钠。混合至均一。
Claims (17)
1.一种减少含亚锡洁牙剂组合物涩味的方法,该方法包括在所述洁牙剂组合物中加入泊洛沙姆,使得该组合物包含:
a.3000ppm-15000ppm的亚锡离子;
b.占组合物重量5%-50%的泊洛沙姆;和
c.占组合物重量40%-95%的水性载体;
所述组合物中的各组分重量百分数之和为100%重量,
其中泊洛沙姆没有减少洁牙剂中亚锡离子的效力。
2.根据权利要求1所述的减少亚锡涩味的方法,其中亚锡离子由氟化亚锡提供。
3.根据权利要求2所述的减少亚锡涩味的方法,其中亚锡离子还由二水合氯化亚锡提供。
4.根据权利要求3所述的减少亚锡涩味的方法,其中水性载体是选自氟离子来源、防牙垢剂、抗菌剂、表面活性剂、增稠材料、润湿剂、水、缓冲剂、二氧化钛、调味系统、增甜剂、着色剂及其混合物的材料。
5.根据权利要求1所述的减少亚锡涩味的方法,其中洁牙剂组合物是双相洁牙剂组合物,它包含第一洁牙剂组合物和第二洁牙剂组合物,其中在所述第二洁牙剂组合物中加入泊洛沙姆,使所述第二洁牙剂组合物包含
a.3000ppm-15000ppm的亚锡离子;
b.占组合物重量5%-50%的泊洛沙姆;和
c.占组合物重量40%-95%的水性载体,且所述第二洁牙剂组合物中的各组分重量百分数之和为100%重量。
6.根据权利要求5所述的减少亚锡涩味的方法,其中在第一洁牙剂组合物中加入占组合物重量1%-20%的平均链长度为4或更高的多磷酸盐和2%-20%重量的总含水量,其中多磷酸盐阴离子和亚锡离子的摩尔比为0.2∶1至5∶1。
7.根据权利要求6所述的减少亚锡涩味的方法,其中多磷酸盐选自具有下式的线性“玻璃态”多磷酸盐
XO(XPO3)nX
其中X是钠或钾,n在6-21之间。
8.根据权利要求6所述的减少亚锡涩味的方法,其中组合物中多磷酸盐阴离子与亚锡离子的摩尔比为0.5∶1至3∶1。
9.根据权利要求7所述的减少亚锡涩味的方法,其中多磷酸盐的平均链长度为21。
10.根据权利要求1所述的减少亚锡涩味的方法,它包括在洁牙剂组合物中加入占组合物重量1%-20%的平均链长度为4或更高的多磷酸盐,使洁牙剂组合物含有占组合物重量2%-20%的总含水量,并使多磷酸盐阴离子和亚锡离子的摩尔比为0.2∶1至5∶1,其中多磷酸盐没有减少洁牙剂中亚锡离子的效力。
11.根据权利要求10所述的减少涩味的方法,其中多磷酸盐选自具有下式的线性“玻璃态”多磷酸盐
XO(XPO3)nX
其中X是钠或钾,n在6至21之间。
12.根据权利要求11所述的减少亚锡涩味的方法,其中多磷酸盐阴离子与亚锡离子的摩尔比为0.5∶1至3∶1。
13.根据权利要求11所述的减少亚锡涩味的方法,其中多磷酸盐的平均链长度为21。
14.根据权利要求13所述的减少亚锡涩味的方法,其中洁牙剂组合物还包含水性载体,所述水性载体是选自氟离子来源、防牙垢剂、抗菌剂、表面活性剂、增稠材料、润湿剂、水、缓冲剂、二氧化钛、调味系统、增甜剂、着色剂及其混合物的材料。
15.根据权利要求14所述的减少亚锡涩味的方法,其中亚锡离子由二水合氯化亚锡提供。
16.根据权利要求15所述的减少亚锡涩味的方法,其中洁牙剂还包含单氟磷酸钠。
17.根据权利要求5所述的减少亚锡涩味的方法,其中第一洁牙剂组合物和第二洁牙剂组合物被包含在洁牙剂配料器的物理上分开的区室中。
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US09/203,215 US6187295B1 (en) | 1996-11-21 | 1998-11-30 | Methods of reducing the astringency of stannous in dentifrice compositions |
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-
1998
- 1998-11-30 US US09/203,215 patent/US6187295B1/en not_active Expired - Lifetime
-
1999
- 1999-11-23 CZ CZ20011526A patent/CZ20011526A3/cs unknown
- 1999-11-23 AU AU20288/00A patent/AU757450B2/en not_active Expired
- 1999-11-23 AT AT99963959T patent/ATE310493T1/de not_active IP Right Cessation
- 1999-11-23 TR TR2001/01532T patent/TR200101532T2/xx unknown
- 1999-11-23 DE DE69928562T patent/DE69928562T2/de not_active Expired - Lifetime
- 1999-11-23 KR KR1020017006720A patent/KR20010092452A/ko not_active Application Discontinuation
- 1999-11-23 EP EP99963959A patent/EP1135098B1/en not_active Expired - Lifetime
- 1999-11-23 CN CNB998137774A patent/CN1154471C/zh not_active Expired - Lifetime
- 1999-11-23 WO PCT/US1999/027810 patent/WO2000032160A1/en not_active Application Discontinuation
- 1999-11-23 JP JP2000584857A patent/JP2002531388A/ja not_active Withdrawn
- 1999-11-23 BR BR9915753-5A patent/BR9915753A/pt not_active IP Right Cessation
- 1999-11-23 CA CA002348237A patent/CA2348237C/en not_active Expired - Lifetime
- 1999-11-23 HU HU0104746A patent/HUP0104746A3/hu unknown
- 1999-11-23 ES ES99963959T patent/ES2252992T3/es not_active Expired - Lifetime
-
2001
- 2001-05-30 NO NO20012661A patent/NO20012661L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
EP1135098B1 (en) | 2005-11-23 |
HUP0104746A3 (en) | 2006-02-28 |
CN1328441A (zh) | 2001-12-26 |
EP1135098A1 (en) | 2001-09-26 |
US6187295B1 (en) | 2001-02-13 |
CA2348237A1 (en) | 2000-06-08 |
CZ20011526A3 (cs) | 2001-10-17 |
WO2000032160A1 (en) | 2000-06-08 |
KR20010092452A (ko) | 2001-10-25 |
AU757450B2 (en) | 2003-02-20 |
DE69928562T2 (de) | 2006-08-03 |
HUP0104746A2 (hu) | 2002-04-29 |
JP2002531388A (ja) | 2002-09-24 |
DE69928562D1 (de) | 2005-12-29 |
ATE310493T1 (de) | 2005-12-15 |
AU2028800A (en) | 2000-06-19 |
BR9915753A (pt) | 2001-09-04 |
NO20012661D0 (no) | 2001-05-30 |
TR200101532T2 (tr) | 2001-10-22 |
NO20012661L (no) | 2001-05-30 |
ES2252992T3 (es) | 2006-05-16 |
CA2348237C (en) | 2003-11-11 |
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