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CN1638723A - 口腔用组合物 - Google Patents

口腔用组合物 Download PDF

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CN1638723A
CN1638723A CN01822027.4A CN01822027A CN1638723A CN 1638723 A CN1638723 A CN 1638723A CN 01822027 A CN01822027 A CN 01822027A CN 1638723 A CN1638723 A CN 1638723A
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M·巴库
A·乔伊纳
K·A·斯特勒
D·泰勒
K·M·汤普森
D·W·托恩斯维特
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Abstract

一种包含吡啶甲酸和过氧化物类或其等效来源物的口腔用组合物，其特征在于吡啶甲酸与过氧化物类或其等效来源物的摩尔比为1∶30至100∶1。

Description

口腔用组合物
本发明涉及一种如权利要求1的前叙部分所述的口腔用组合物。
虽然未被广泛用于人体用除臭剂中，但过氧化物类，特别是过氧化氢及其来源的物质是众所周知的抗菌剂。还已知可以通过添加少量的过渡金属螯合剂来改善该类物质的稳定性。在一些出版物中描述了吡啶二羧酸用于该目的的应用，例如在EP 666,307 A(Procter和Gamble)中进行了描述。还要求用吡啶二羧酸来改善过氧化氢的抗菌作用——见EP 845,526 A(Eka Chemicals)。
在WO9007501(Solvay Interox)中已经对作为过氧羧酸漂白组合物稳定剂的吡啶甲酸进行了描述。以微量添加的吡啶甲酸可螯合能催化过氧化合物分解的过渡金属。在EP 1,074,607(Ausimont S.p.A.)中还将吡啶甲酸作为用于这种目的的任选组分列举出来。
我们已经发现，吡啶甲酸和过氧化物类或其等效来源物的增效混合物可以达到提供一种极佳的抗菌效益的目的并且其随后还具有抵抗蚀斑、龋和龈炎的保护作用。我们还发现吡啶甲酸和过氧化物类或其等效来源物的增效混合物可达到提供一种极佳的牙齿变白效益的目标。
现有技术从来没有公开或暗示过本发明的产品，也从来没有公开或暗示过用其可以获得极佳的抗菌和牙齿变白的效益。
我们发现使用吡啶甲酸和过氧化物类或其等效来源物的增效混合物可提供一种极佳的比单独使用这两种组分中的任一种所获得的效益更好的牙齿变白抗菌效益。此外，以可提供所说增效效益的水平所添加的吡啶甲酸确保了在用于人体的具有显著效益的产品中可以使用较少量的过氧化物类物质或其等效来源物。
因此，本发明的第一方面提供了一种如权利要求1的组合物。
在本发明的第二方面，其提供了一种使牙齿变白的美容方法，该方法包括使用吡啶甲酸和过氧化物类或其等效来源物。
在本发明的第三方面，其提供了一种通过将吡啶甲酸和过氧化物类或其等效来源物与可美容用的载体物质进行混合来制造治疗龈炎、龋和/或蚀斑的口腔用组合物的方法。
通过分别使用吡啶甲酸和过氧化物类或其等效来源物可以获得使用本发明组合物所获得的抗菌和牙齿变白效益。如果所处理的底物同时使用两种组分，则该类应用可以同时进行或连贯进行。当通过独立的组合物来应用该组分时，优选地该产品还包含一种将两种组合物应用于人体的使用方法和/或说明。在过酸和吡啶甲酸彼此独立地分别储存的情况中，该配方要求每种物质的稳定性都被优化。例如，如果一种制剂包含过酸如PAP，则该制剂的pH应在3.5至5之间，优选地为4。然后将该包含吡啶甲酸的制剂改进以使得当将这两种组分进行混合时，它们可以提供本发明所述的口腔用组合物并且具有6.5至7.5之间的可接受的pH。
优选地，用相同的组合物来提供吡啶甲酸和过氧化物类或其等效来源物。本发明优选的一种产品是一种既包含吡啶甲酸又包含过氧化物类或其等效来源物的单一组合物。
涉及本发明第二方面的可获得人体抗菌效益的美容方法优选地以1∶30至100∶1的摩尔比来使用吡啶甲酸和过氧化物类或其等效来源物。根据本发明第一方面，该组合物的这种摩尔比更优选地为1∶20至50∶1并且最优选地为1∶10至20∶1。
吡啶甲酸是本发明产品中的一种必需组分。以该组合物的总重量为基础，其可以以0.01％至10％，特别是0.1％至8％，并且尤其是0.15％至5％重量来使用。吡啶甲酸可以以其酸或盐的形式来进行应用。适宜的盐包括碱金属盐、碱土金属盐、胺盐、以及季铵盐。当该吡啶甲酸部分是或全部是盐的形式时，其优选的摩尔量等于上述的优选水平。
本发明的产品包含过氧化物类物质本身或可在原位产生过氧化物类物质的物质。过氧化物类物质是一种包含过氧基(-O-O-)的物质。适宜的过氧化物类物质的实例包括过氧化氢和过酸。其等效来源物的实例是在溶解于水时能产生过氧化氢的化合物，如过硼酸钠单水合物、过硼酸钠四水合物、过碳酸钠和过脲(脲-过氧化氢加合化合物)。另一些实例有与其适宜底物共存的酶的过氧化物产生体系如过氧化物酶、氧化酶和其它氧化还原酶的酶体系。优选的产品包含过酸，特别是式(1)的过酸
其中R是氢或C1-C4烷基；n是1至5；并且X是C＝O或SO2。
式1)的过氧酰胺基邻苯二酰胺本身是已知的并且已经在EP-A-325,288和EP-A-325,289中进行了描述。这种结构式的一种优选化合物是式1)的N-苯二酰亚氨基过氧己酸(“PAP”)，其中R＝H，n＝5并且X＝C＝O。其中X＝SO2的式1)化合物的一个实例是如在EP-A-485,927中所描述的糖精-过己酸(″糖精PAP″)。或者可以选择一种在溶解于水时可以产生过氧化氢的化合物而不是过氧化氢本身。适宜的过酸包括在WO96/05802中所提及的这些化合物中的任何一种，其涉及过酸的内容在这里被引入作为参考。
特别优选的产品包含一种在溶解于水时能产生过氧化氢的化合物，尤其优选在应用前不存在过氧化氢的产品。
以该组合物的总重量为基础，本发明组合物中的过氧化物类或其等效来源物可以在0.0001％至5％重量的范围内，更优选地为0.001至1.5％重量，最优选地为0.005％至0.5％重量。
在由于其抗菌作用而使用该口腔用组合物的情况中，该组合物还可以包含一种过渡金属螯合剂。虽然吡啶甲酸是一种过渡金属螯合剂，但是通过使用更多的这类物质可以增加其性能，特别是使用对铁(III)具有高结合常数的物质；就是说，对铁(III)的结合常数高于1015，优选地高于1020，并且最优选地高于1026。这类物质中特别优选地是二亚乙基三胺五乙酸(DTPA)。还可以使用该类物质的盐，适宜的盐是与所描述的作为适宜的吡啶甲酸盐的物质(参见上文)相类似的物质。所使用的作为组合物一部分添加的过渡金属螯合剂及其盐的总量一般为组合物的0.1％至5％，特别是0.2％至3％，并且尤其是0.4％至2％重量。
本发明的口腔用组合物还可包含现有技术中很常见的其它成分，如：
抗菌剂，例如三氯生、洗必太、铜-锌-和亚锡盐如枸橼酸锌、硫酸锌、甘氨酸锌、枸橼酸钠锌和焦磷酸亚锡、血根碱提取物、甲硝唑、季铵化合物如氯化十六烷基吡啶；双胍，如洗必太二葡萄糖酸盐、海克替啶、癸双辛胺啶、阿来西定；和卤化的双酚化合物，如2，2′亚甲基双-(4-氯-6-溴酚)；
抗炎剂如布洛芬、氟比洛芬、阿司匹林、消炎痛等等；
抗-龋剂如氟化钠和氟化亚锡、氟化胺类、单氟磷酸钠、三偏磷酸钠和酪蛋白；
蚀斑缓冲物如脲、乳酸钙、甘油磷酸钙和聚丙稀酸锶；
维生素如维生素A、C和E；
植物提取物；
脱敏剂，例如枸橼酸钾、氯化钾、酒石酸钾、碳酸氢钾、草酸钾、硝酸钾和锶盐；
抗结石剂，例如焦磷酸碱金属盐、包含次磷酸盐的聚合物、有机膦酸酯和磷酸枸椽酸盐等等；
生物分子，例如细菌素、抗体、酶，等等；
矫味剂，例如薄荷和留兰香油；
蛋白质类物质如胶原蛋白；
防腐剂；
不透明剂；
着色剂；
pH-调节剂；
甜味剂；
可药用载体，例如淀粉、蔗糖、水或水/醇体系等等；
表面活性剂，如阴离子、非离子、阳离子和两性离子或两性表面活性剂；
微粒研磨材料如硅石、矾土、碳酸钙、磷酸二钙、焦磷酸钙、羟磷灰石、三偏磷酸盐、不溶性的六偏磷酸盐等等，包括成块的颗粒研磨材料，其通常为该口腔护理组合物重量的3至60％重量。
湿润剂如甘油、山梨醇、丙二醇、木糖醇、乳糖醇等等；
粘合剂和增稠剂如羧甲基纤维素钠、黄原胶、阿拉伯胶等等以及合成的聚合物如聚丙烯酸酯和羧乙烯聚合物如Carbopol；
还可以包括可增强活性成分如抗菌剂的传递的聚合物。该类聚合物的实例有聚乙烯甲基醚与马来酸酐的共聚物以及其它适宜的可增强传递的聚合物，例如这些在DE-A-3,942,643(Colgate)中所描述的聚合物；
缓冲剂和用于缓冲口腔护理组合物的pH和离子强度的盐；以及
其它可被包含在其中的可存在或不存在的成分有例如漂白剂如过氧化合物例如过氧二磷酸钾、泡腾体系如碳酸氢钠/枸橼酸系统、改色系统等等。
还可以用脂质体来改善活性成分的传递或稳定性。
该口腔用组合物可以是现有技术中任何常见形式，例如牙膏、凝胶、摩丝、气雾剂、胶、锭剂、粉末、乳膏等等，并且还可以被制备成双室型分配器中所使用的系统。
实施例1
用如下的方法来对该漂白剂进行评估：
(1)将合成的羟基磷灰石圆片磨光，然后将其在37℃下在无菌的唾液中放置一整夜以形成一种表膜。
(2)在37℃下用茶溶液将这些圆片处理7天使其染色。
(3)以所需时间将染色的圆盘浸入到漂白溶液中。
(4)用Minolta chromameter CR-300以L*a*b*方式来测定该圆片的颜色变化。用L*(开始)、L*(变脏)、以及L*(变清洁)来计算除去染色的百分比。负值表示变黑，正值表示漂白(变白)作用。
所用的所有制剂用0.5M NaHCO3来处理。负值表示变黑并且下面的表1表示了单独使用吡啶甲酸以及其与0.1％H2O2或PAP一起使用所得的结果。
    除去染色％
    10分钟
0.1％H2O2     2
0.5 0.1％ H2O2/5％吡啶甲酸     13
1％PAP     27
1％PAP/5％哌啶甲酸     46
5％吡啶甲酸     8
表中所表示的结果表明，过酸中加入吡啶甲酸可以提供比单独使用吡啶甲酸或过酸更有效的漂白组合物。
实施例
下面的口腔用组合物包含两种制剂：一种PAP-凝胶制剂和一种pH-调节制剂。
           PAP-凝胶制剂
成分     数量(％w/w)
PAP     0.6
Gantrez     3.0
黄原胶     0.2
硅石     9.0
氢氧化钠     0.5
水     至100
PAP可以以Eureco HC-17市售获得(ex.Ausimont)。这种制剂的pH为4。
pH-调节制剂
成分     数量(％w/w)
Gantrez     3.0
黄原胶     0.2
硅石     6.0
哌啶甲酸     5.0
糖精     0.25
PH剂(TSP或NaOH)     至pH11
KNO3     5.0
NaF/SMFP     至1500pmm
颜料     适量
水     至100
当将该PAP-制剂和pH-调节制剂混合到一起，所得组合物的pH在约6.5至8.5之间。

Claims (13)

1.一种包含吡啶甲酸和过氧化物类或其等效来源物的口腔用组合物，其特征在于吡啶甲酸与过氧化物类或其等效来源物的摩尔比为1∶30至100∶1。
2.如权利要求1所述的口腔用组合物，其中所说的过氧化物类或其等效来源物是一种过酸或在溶解于水时能产生过氧化氢的化合物。
3.如前面任意一项权利要求所述的口腔用组合物并且包含附加的过渡金属螯合剂。
4.如前面任意一项权利要求所述的除臭产品，其中所说的组合物包含一种与铁(III)的结合系数高于1015的过渡金属螯合剂。
5.如前面任意一项权利要求所述的口腔用组合物，其中所说的组合物包含作为过渡金属螯合剂的二亚乙基三胺五乙酸。
6.如前面任意一项权利要求所述的口腔用组合物，其中吡啶甲酸与过氧化物类或其等效来源物的摩尔比为1∶10至20∶1。
7.如前面任意一项权利要求所述的口腔用组合物，其中所说的吡啶甲酸以占组合物0.01％至10％重量的数量存在。
8.如前面任意一项权利要求所述的口腔用组合物，其中所说的吡啶甲酸以占组合物0.15％至2.5％重量的数量存在。
9.如前面任意一项权利要求所述的口腔用组合物，其中所说的过氧化物类或其等效来源物以占组合物0.0001％至1.5％重量的数量存在。
10.如前面任意一项权利要求所述的口腔用组合物，其中所说的过氧化物类或其等效来源物以占组合物0.003％至0.5％重量的数量存在。
11.如前面任意一项权利要求所述的口腔用组合物并包含可美容用载体物质。
12.如前面任意一项权利要求所述的组合物用于牙齿变白、抗蚀斑、抗恶臭、抗-龋或抗牙垢处理的应用。
13.如前面任意一项权利要求所述的组合物在制备用于牙齿变白、抗蚀斑、抗恶臭、抗-龋或抗牙垢处理的药物中的应用。
CNB018220274A 2001-01-16 2001-12-07 口腔用组合物 Expired - Fee Related CN1313070C (zh)

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