CN108210355A - 口腔护理组合物 - Google Patents
口腔护理组合物 Download PDFInfo
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- CN108210355A CN108210355A CN201810183895.5A CN201810183895A CN108210355A CN 108210355 A CN108210355 A CN 108210355A CN 201810183895 A CN201810183895 A CN 201810183895A CN 108210355 A CN108210355 A CN 108210355A
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- 239000004475 Arginine Substances 0.000 claims abstract description 38
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims abstract description 38
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- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 claims abstract description 21
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Abstract
一种口腔护理组合物,其包含:(a)呈游离或盐形式的精氨酸;和(b)氧化锌和柠檬酸锌。该口腔护理组合物可减少或抑制口腔中的生物膜形成。
Description
本申请是申请日为2013年12月19日、申请号为201310703017.9、发明名称为“口腔护理组合物”的中国专利申请的分案申请。
技术领域
本发明涉及口腔护理组合物。
背景技术
牙菌斑为附着于牙齿和其它口腔表面,特别是在牙龈缘上的生物膜,并与牙龈炎、牙周炎、龋齿及其它形式的牙周病的发生有关。牙菌斑是有粘着力的,并且对自牙齿和/或口腔表面去除是高度抗性的。牙菌斑包含葡聚糖,后者为不溶性多糖,其给菌斑提供其粘结性。细菌酶葡糖基转移酶把饮食糖转化为葡聚糖。菌斑矿物化形成称为牙结石(或牙垢)的硬沉积物,其变为牙龈的局部刺激物,引起牙龈炎。
各种抗菌剂可阻碍细菌的生长,并因此减少口腔表面的生物膜形成。
锌和其它金属化合物/盐先前已经用作抗菌剂。不受任何理论的束缚,确信游离锌离子通过抑制葡萄糖代谢和/或与细菌细胞壁相互作用,减少口腔的细菌定植来提供抗菌效力(如在Cummins D.,J ClinPeriodontol 1991;18;455-461中讨论的那样)。不溶性的锌化合物,氧化锌,也可在刷牙期间提供强大的抗菌效力。
提供表现出比先前已知的组合物在其减少生物膜方面的功效甚至更大的口腔护理组合物将会是合乎需要的。
发明内容
本文提供一种口腔护理组合物,其包含:(a)呈游离或盐形式的精氨酸;和(b)两种或更多种锌盐,其中所述锌盐的至少一种是氧化锌,和所述锌盐的至少一种是柠檬酸锌。
任选地,氧化锌与柠檬酸锌的重量比是1.5∶1至4.5∶1、 1.5∶1至4∶1、1.7∶1至2.3∶1、1.9∶1至2.1∶1或约2∶1。也可使用基于这些重量比的相应的摩尔比。
任选地,精氨酸以基于组合物的总重量的从0.5%重量至10%重量的量存在。还任选地,精氨酸以基于组合物的总重量的0.5%重量至3%重量或从1%重量至2.85%重量的量存在。仍然进一步任选地,精氨酸以基于组合物的总重量的从1.17%重量至2.25%重量的量存在。还进一步任选地,精氨酸以基于组合物的总重量的从1.4%重量至1.6%重量的量存在。进一步任选地,精氨酸以基于组合物的总重量的约1.5%重量的量存在。
任选地,该组合物中的锌盐的总浓度为基于组合物的总重量从0.2%重量至5%重量。
任选地,精氨酸与总锌盐的摩尔比从0.05∶1至10∶1。
任选地,组合物包含基于组合物的总重量的0.5%重量-1.5%重量的量的氧化锌和0.25%重量-0.75%重量的量的柠檬酸锌。进一步任选地,组合物包含基于组合物的总重量的约1%重量的量的氧化锌和约0.5%重量的量的柠檬酸锌。
任选地,该组合物还包含一种或多种研磨剂。还任选地,所述一种或多种研磨剂的至少一种是二氧化硅。
任选地,该口腔护理组合物还包含抗牙结石剂。还任选地,抗牙结石剂以基于组合物的总重量的从0.2%重量至0.8%重量的量存在。仍然还任选地,抗牙结石剂是焦磷酸四钠和焦磷酸四钾的至少一个。
本文也提供一种用于减少或抑制口腔中的生物膜形成的口腔护理组合物。
本文也提供一种减少或抑制口腔中的生物膜形成的方法,该方法包括使口腔与口腔护理组合物接触。
本文也提供口腔护理组合物中的以下组分的组合在减少或抑制口腔中的生物膜形成中的应用:(a)呈游离或盐形式的精氨酸;和(b)两种或更多种锌盐,其中所述锌盐的至少一种是氧化锌,和所述锌盐的至少一种是柠檬酸锌。
任选地,氧化锌与柠檬酸锌的重量比是1.5∶1至4.5∶1、1.5∶1至4∶1、 1.7∶1至2.3∶1、1.9∶1至2.1∶1或约2∶1。也可使用基于这些重量比的相应的摩尔比。
任选地,精氨酸以基于组合物的总重量的从0.5%重量至10%重量的量存在于口腔护理组合物中。还任选地,精氨酸以基于组合物的总重量的从0.5%重量至3%重量或1%重量至2.85%重量的量存在于口腔护理组合物中。仍然还任选地,精氨酸以基于组合物的总重量的从1.17%重量至2.25%重量的量存在于口腔护理组合物中。进一步任选地,精氨酸以基于组合物的总重量的从1.4%重量至1.6%重量的量存在于口腔护理组合物中。仍然还任选地,精氨酸以基于组合物的总重量的约1.5%重量的量存在于口腔护理组合物中。
任选地,在口腔护理组合物中的锌盐的总浓度为基于组合物的总重量的从0.2%重量至5%重量。
任选地,在口腔护理组合物中的精氨酸与总锌盐的摩尔比为从0.05∶1至10∶1。也可使用基于这些重量比的相应的摩尔比。
任选地,氧化锌以基于组合物的总重量的从0.5%重量至1.5%重量的量存在于口腔护理组合物中,而柠檬酸锌以基于组合物的总重量的从0.25%重量至0.75%重量的量存在于口腔护理组合物中。进一步任选地,氧化锌以基于组合物的总重量的约1%重量的量存在于口腔护理组合物中,而柠檬酸锌以基于组合物的总重量的约0.5%重量的量存在于口腔护理组合物中。
本发明的适用性的其它领域自下文提供的详述将变得显而易见。应该理解,详述和具体实施例,尽管表明本发明的优选实施方案,打算仅用于举例说明的目的,并不意欲限制本发明的范围。
具体实施方式
优选实施方案的以下描述本质上仅为示例性的,并且决不打算限制本发明、其应用或用途。
如在本文通篇中使用的,范围用作描述在所述范围内每个数值的简略表达方式。在所述范围内的任何数值可被选择作为所述范围的端点。另外,本文所引用的所有参考文献通过引用以其全文结合到本文中。如果在本公开的定义和所引用的参考文献中有抵触,以本公开为准。
除非另外指明,在本文和说明书中别处所表示的所有百分数和量应理解为指按重量计的百分数。所给出的量为基于材料的有效重量。
如在本文通篇中使用的,短语″呈游离或盐形式的精氨酸″,意指精氨酸可以作为游离的氨基酸存在,或作为氨基酸的盐存在。适宜的精氨酸的盐的实例包括,但不限于精氨酸碳酸氢盐、精氨酸磷酸盐和精氨酸盐酸盐。
本发明人已经惊奇地发现,将精氨酸加至包含锌盐的口腔护理组合物中,改善口腔护理组合物在减少生物膜方面的功效。本发明人也已经出乎意料地发现,存在最佳的精氨酸浓度,在此浓度下的,含锌盐的口腔护理组合物的生物膜减少功效最佳。
在第一方面,提供一种口腔护理组合物,其包含:(a)呈游离或盐形式的精氨酸;和(b)两种或更多种锌盐,其中所述锌盐的至少一种是氧化锌,而所述锌盐的至少一种是柠檬酸锌.
在一些实施方案中,精氨酸以基于组合物的总重量从0.5%重量至3%重量;从0.75%重量至2.9%重量;从1%重量至2.85%重量;从1.17%重量至2.25%重量;从1.3%重量至2%重量;从1.4%重量至1.6%重量;或约1.5%重量的量存在于口腔护理组合物中。
在以上的任何实施方案中,口腔护理组合物中的精氨酸∶总锌盐的摩尔比,可为从0.05∶1至10∶1;从0.08∶1至5∶1;从0.1∶1至1∶1;从0.4∶1至0.8∶1;或约0.65∶1。
可用于以上诸方面的任何组合物中的适宜锌盐的实例,包括(但不限于):氧化锌、柠檬酸锌、乳酸锌、氯化锌、乙酸锌、葡萄糖酸锌、甘氨酸锌、硫酸锌、柠檬酸锌钠,及其混合物。在任何的以上诸方面中,一种或多种锌盐中的至少一种可为氧化锌。在组合物中,所述锌盐的至少一种是氧化锌,而所述锌盐的至少一种是柠檬酸锌。在任一上述实施方案中,组合物中的锌盐的总浓度可为基于组合物的总重量的从0.2%重量至5%重量;从0.5%重量至2.5%重量;从0.8%重量至2%重量;或约1.5%重量。
在任一上述实施方案中,组合物可包含基于组合物的总重量的0.5%重量-1.5%重量的量的氧化锌和0.25%重量-0.75%重量的量的柠檬酸锌。或者,组合物可包含基于组合物的总重量的0.75%重量-1.25%重量的量的氧化锌和0.4%重量-0.6%重量的量的柠檬酸锌。或者,组合物可包含基于组合物的总重量的约1%重量的量的氧化锌和约0.5%重量的量的柠檬酸锌。
在任一上述实施方案中,口腔护理组合物可进一步包含一种或多种研磨剂。可包含在组合物中的合适的研磨剂包括,但不限于:硅石研磨剂、氧化铝、硅酸铝、煅烧氧化铝、膨润土、其它硅质材料、不溶性磷酸盐、天然碳酸钙(NCC)、沉淀碳酸钙(PCC),及其混合物。在一些实施方案中,一种或多种研磨剂中的至少一种为硅石研磨剂。硅石研磨剂的实例包括,但不限于:具有最多约20微米的平均粒度的沉淀或水合硅石(比如由J.M.Huber ChemicalsDivision,Havre de Grace,Md.21078销售的Zeodent 105和Zeodent 114)、Sylodent 783(由Davison Chemical Division of W.R.Grace&Company销售)或Sorbosil AC 43(得自PQCorporation)。在一些实施方案中,一种或多种研磨剂中的至少一种为碳酸钙研磨剂,比如沉淀碳酸钙(PCC)或天然碳酸钙(NCC)。
在任一上述实施方案中,组合物可进一步包含抗牙结石(牙垢控制)剂。合适的抗牙结石剂包括,但不限于:磷酸盐和多聚磷酸盐、聚氨基丙磺酸(AMPS)、聚烯烃磺酸盐、聚烯烃磷酸盐、二膦酸盐比如氮杂环烷-2,2-二膦酸盐(例如氮杂环庚烷-2,2-二膦酸)、N-甲基氮杂环戊烷-2,3-二膦酸、乙烷-1-羟基-1,1-二膦酸(EHDP)和乙烷-1-氨基-1,1-二膦酸盐、膦酰基链烷羧酸等。有用的无机磷酸盐和多聚磷酸盐包括磷酸二氢钠、磷酸氢钠和磷酸三钠、焦磷酸四钠(TSPP)、焦磷酸四钾、三聚磷酸钠、四聚磷酸盐、三偏磷酸钠、六偏磷酸钠及其混合物。其它有用的牙垢控制剂包括聚羧酸酯聚合物(polycarboxylate polymers)和聚乙烯基甲醚/马来酸酐(PVM/MA)共聚物,比如在一些实施方案中,抗牙结石剂为焦磷酸四钠和焦磷酸四钾中的至少一种。在一些实施方案中,抗牙结石剂以基于组合物的总重量的0.2%重量-0.8%重量、0.3%重量-0.7%重量、0.4%重量-0.6%重量、或约0.5%重量的量存在于组合物中。
在任一上述实施方案中,口腔护理组合物可为洁齿剂、牙膏、凝胶、牙粉、漱口水、口腔清洗剂、锭剂、片剂、喷雾剂、口香糖或薄膜。在某些实施方案中,口腔护理组合物为牙膏、凝胶或牙粉。
在第二方面,本文提供依据任一上述实施方案的口腔护理组合物,其用于减少或抑制口腔中的生物膜形成。
在第三方面,本文提供减少或抑制口腔中的生物膜形成的方法,该方法包括使口腔与依据任一上述实施方案的口腔护理组合物接触。
在第四方面,本文提供在口腔护理组合物中的以下组分在减少或抑制口腔中的生物膜形成中的应用:(a)呈游离或盐形式的精氨酸;和(b)两种或更多种锌盐的组合,其中所述锌盐的至少一种是氧化锌,而所述锌盐的至少一种是柠檬酸锌。
依据第四方面,口腔护理组合物可为如上对于第一方面描述的、依据任一上述实施方案的组合物。
口腔护理组合物可进一步包含另外的成分。这些另外的成分可包括,但不限于:稀释剂、碳酸氢盐、pH调节剂、表面活性剂、泡沫调节剂、增稠剂、湿润剂、甜味剂、矫味剂、颜料、另外的抗菌剂、防龋剂及其混合物。
在一些实施方案中,口腔护理组合物包含至少一种碳酸氢盐,例如由于泡腾和释放二氧化碳用于赋予牙齿和牙龈“清洁的感觉”。可使用任何口腔可接受的碳酸氢盐,包括,但不限于:碱金属碳酸氢盐比如碳酸氢钠和碳酸氢钾、碳酸氢铵等。一种或多种另外的碳酸氢盐可任选地按组合物的总重量计的约0.1wt.%-约50wt.%,例如约1wt.%-20wt.%的量存在。
在一些实施方案中,口腔护理组合物包含至少一种pH调节剂。这样的试剂包括降低pH的酸化剂、升高pH的碱化剂和把pH控制在期望的范围内的缓冲剂。例如,可包括一种或多种选自酸化剂、碱化剂和缓冲剂的化合物,以提供2-10,或者在各种示例性实施方案中提供2-8、3-9、4-8、5-7、6-10、7-9等的pH。可使用任何口腔可接受的pH调节剂,包括,但不限于:羧酸、磷酸和磺酸、酸盐(例如柠檬酸单钠、柠檬酸二钠、苹果酸一钠等)、碱金属氢氧化物比如氢氧化钠、碳酸盐比如碳酸钠、碳酸氢盐、倍半碳酸盐;硼酸盐、硅酸盐、磷酸盐(例如磷酸二氢钠、磷酸三钠)、咪唑等。一种或多种pH调节剂任选地以有效保持组合物在口腔可接受的pH范围内的总量存在。
口腔护理组合物也可包含至少一种表面活性剂。可使用其大多数为阴离子型、非离子型和两性型的任何口腔可接受的表面活性剂。合适的阴离子型表面活性剂包括,但不限于C8-20烷基硫酸的水溶性盐、C8-20脂肪酸的磺化单甘油酯(盐)、肌氨酸盐、牛磺酸盐等。这些和其它类别的说明性实例包括十二烷基硫酸钠、椰子单甘油酯磺酸钠、月桂基肌氨酸钠、月桂基羟乙磺酸钠、聚乙二醇单十二醚羧酸钠和十二烷基苯磺酸钠。合适的非离子型表面活性剂包括,但不限于泊咯沙姆、聚氧乙烯失水山梨醇酯、脂肪醇乙氧基化物、烷基酚乙氧基化物、叔胺氧化物、叔膦氧化物、二烷基亚砜等。合适的两性型表面活性剂包括,但不限于具有阴离子基团比如羧酸根、硫酸根、磺酸根、磷酸根或膦酸根的C8-20脂肪族仲胺和叔胺的衍生物。也可使用甜菜碱,其合适的实例为椰油酰氨基丙基甜菜碱。一种或多种表面活性剂任选地按组合物的总重量计的约0.01wt.%-约10wt.%,例如约0.05wt.%-约5wt.%或约0.1wt.%-约2wt.%的总量存在。
口腔护理组合物可包含至少一种泡沫调节剂,例如用于增加在搅动时由组合物产生的泡沫的量、稠度或稳定性。可使用任何口腔可接受的泡沫调节剂,包括,但不限于:聚乙二醇(PEGs),也称为聚氧乙烯。高分子量的PEGs为合适的,包括具有200,000-7,000,000,例如500,000-5,000,000或1,000,000-2,500,000的平均分子量的那些PEGs。一种或多种PEGs任选地按组合物的总重量计的约0.1wt.%-约10wt.%,例如约0.2wt.%-约5wt.%或约0.25wt.%-约2wt%的总量存在。
口腔护理组合物可包含至少一种增稠剂,例如用于赋予组合物期望的一致性和/或口感。可使用任何口腔可接受的增稠剂,包括,但不限于:卡波姆(也称为聚氧乙烯);角叉菜胶(也称为爱尔兰苔藓),并且更具体地讲为ι-角叉菜胶(iota-角叉菜胶);纤维素聚合物,比如羟乙基纤维素、羧甲基纤维素(CMC)及其盐,例如CMC钠;天然树胶,比如刺梧桐胶、黄原胶、阿拉伯树胶和黄蓍胶;胶体硅酸铝镁、胶态硅石等。一类优选的增稠剂或胶凝剂包括与季戊四醇的烷基醚或蔗糖的烷基醚交联的丙烯酸的均聚物,或者卡波姆。卡波姆可作为系列自B.F Goodrich经市售得到。特别优选的卡波姆(Carbopols)包括卡波姆(Carbopol)934、940、941、956、974P,及其混合物。也可使用硅石增稠剂比如DT 267(得自PPG Industries)。一种或多种增稠剂任选地按组合物的总重量计以约0.01wt.%-15wt.%,例如约0.1wt.%-约10wt.%或约0.2wt.%-约5wt.%的总量存在。
组合物可包含至少一种粘度调节剂,例如用于帮助抑制成分的沉降或分离,或促进在搅动液体组合物时的再分散性。可使用任何口腔可接受的粘度调节剂,包括,但不限于:矿物油、矿脂、粘土和有机改性粘土、硅石等。一种或多种粘度调节剂任选地按组合物的总重量计以约0.01wt.%-约10wt.%,例如约0.1wt.%-约5wt.%的总量存在。
组合物也可包含至少一种润湿剂。可使用任何口腔可接受的润湿剂,包括,但不限于:多元醇,比如甘油、山梨醇(任选地作为70wt.%水溶液)、木糖醇或低分子量聚乙二醇(PEGs)。大多数润湿剂也作为甜味剂起作用。一种或多种润湿剂任选地按组合物的总重量计以约1wt.%-约70wt.%,例如约1wt.%-约50wt.%、约2wt.%-约25wt.%或约5wt.%-约15wt.%的总量存在。
口腔护理组合物可包含至少一种甜味剂,例如用于改进组合物的味道。一种或多种甜味剂任选地以强烈依所选择的具体甜味剂的总量存在,但是一般地按组合物的总重量计为0.005wt.%-5wt.%,任选地按组合物的总重量计为0.005wt.%-0.2wt.%,进一步任选地为0.05wt.%-0.1wt.%。
组合物也可包含至少一种矫味剂,例如用于改进组合物的味道。可使用任何口腔可接受的天然或合成矫味剂,包括,但不限于:茶香料(tea flavours)、香草醛、鼠尾草、马郁兰、欧芹油、留兰香油、肉桂油、冬青油(水杨酸甲酯)、薄荷油、丁香油、月桂油、茴香油、桉叶油、柑橘油、果油;及果油和精油,包括源于柠檬、橙、酸橙、葡萄柚、杏、香蕉、葡萄、苹果、草莓、樱桃、菠萝等的那些果油和精油;源于豆和坚果的调味剂,比如咖啡、可可、可乐、花生、杏仁等;吸附和包封的矫味剂等。也包括在本文的矫味剂中的是在口腔中提供香味和/或其它感官效果,包括凉味或暖味效果效果的成分。这样的成分说明性地包括薄荷醇、乙酸薄荷酯、乳酸薄荷酯、樟脑、桉叶油、桉油精、茴香脑、丁子香酚、桂皮、覆盆子酮(oxanone)、α-紫罗兰酮、丙烯基乙基愈创木酚(propenyl guaiethol)、百里酚、芳樟醇、苯甲醛、肉桂醛、N-乙基-对-薄荷烷-3-甲胺(carboxamine)、N,2,3-三甲基-2-异丙基丁酰胺、3-(1-薄荷氧基(menthoxy))-丙-1,2-二醇、肉桂醛甘油缩醇(cinnamaldehyde glycerol acetal,CGA)、薄荷酮甘油缩醇(menthone glycerol acetal,MGA)等。一种或多种矫味剂任选地按组合物的总重量计以约0.01wt.%-约5wt.%,例如约0.03wt.%-约2.5wt.%,任选地约0.05wt.%-约1.5wt.%,进一步任选地约0.1wt.%-约0.3wt.%的总量存在。
组合物可包含至少一种着色剂。本文的着色剂包括颜料、染料、色淀(lakes)和赋予特定的光泽或反射性的试剂,比如珠光剂。可使用任何口腔可接受的着色剂,包括,但不限于:滑石、云母、碳酸镁、硅酸镁、硅酸镁铝、二氧化钛、红色、黄色、棕色和黑色铁氧化物、亚铁氰化铁铵((ferric ammoniumferrocyanide))、锰紫、群青、钛化云母(titaniated mica)、氯氧化铋等。一种或多种着色剂任选地按组合物的总重量计以约0.001wt.%-约20wt.%,例如约0.01wt.%-约10wt.%或约0.1wt.%-约5wt.%的总量存在。
组合物也可包含另外的抗菌或防腐剂,比如洗必泰、三氯生、季铵化合物(例如苯扎氯铵)或对羟基苯甲酸酯类,比如对羟基苯甲酸甲酯或对羟基苯甲酸丙酯。一种或多种另外的抗菌或防腐剂可按组合物的总重量计以约0.01wt.%-约0.5wt.%,任选地以约0.05wt.%-约0.1wt.%的总量存在于组合物中。
口腔护理组合物也可包含氟离子源。氟离子源包括,但不限于:氟化亚锡、氟化钠、氟化钾、单氟磷酸钾、单氟磷酸钠、单氟磷酸铵、氟硅酸钠、氟硅酸铵、氟化胺比如奥拉氟(olaflur)(N’-十八烷基三甲撑二胺-N,N,N’-三(2-乙醇)-二氢氟酸盐)、氟化铵,及其组合。在某些实施方案中,氟离子源包括氟化亚锡、氟化钠、氟化胺、单氟磷酸钠,及其混合物。在某些实施方案中,口腔护理组合物也可以足以提供约50-约5000ppm氟离子,例如约100-约1000、约200-约500或约250ppm氟离子的量含有氟离子源或供氟成分。氟离子源可以约0.001wt.%-约10wt.%,例如约0.003wt.%-约5wt.%、0.01wt.%-约1wt.或约0.05wt.%的水平加入到组合物中。然而,应该理解,提供合适水平的氟离子的氟化盐的重量将显而易见地基于盐中反荷离子的重量而变化,并且本领域的技术人员可易于确定这样的量。优选的氟化盐可为氟化钠。
组合物可包含唾液刺激剂,例如用于改善口腔干燥症。可使用任何口腔可接受的唾液刺激剂,包括,但不限于:食品酸,比如柠檬酸、乳酸、苹果酸、琥珀酸、抗坏血酸、己二酸、富马酸和酒石酸,及其混合物。一种或多种唾液刺激剂任选地以唾液刺激有效总量存在。
组合物可包含防敏感剂,例如钾盐,比如硝酸钾、碳酸氢钾、氯化钾、柠檬酸钾和草酸钾;辣椒素、丁子香酚、锶盐、氯化物盐及其组合。这样的试剂可以有效量,例如依所选择的试剂而定,基于组合物的总重量的重量计的约1wt.%-约20wt.%加入。
组合物可进一步包含抗氧化剂。可使用任何口腔可接受的抗氧化剂,包括丁羟茴醚(BHA)、丁羟甲苯(BHT)、维生素A、类胡萝卜素、维生素E、黄酮类、多元酚类、抗坏血酸、草本抗氧化剂、叶绿素、褪黑激素,及其混合物合。
实施例
为了评价含不同浓度精氨酸的组合物的生物膜减少功效,实施诸实验。
在以下所有实施例中,所使用的实验方法学为曼彻斯特大学生物膜生长抑制模型(Biofilm Growth Inhibition University ofManchester Model)。如下为该模型的方案:
(1)自4名健康志愿者采集牙菌斑,并作为接种体汇集在一起。使接种体的光密度在610nm下相当于0.3吸光度
(2)把无菌羟磷灰石(HAP)盘在37℃下,于厌氧条件下用1mL的无菌人工唾液(含有0.01%重量蔗糖)和1mL汇集的唾液在24孔微量滴定板中温育24小时。
(3)对于每一种试验洁齿剂(和对于每一个对照组),制备按重量计的1份洁齿剂:2份无菌蒸馏水的处理液。把每一个新鲜制备的处理液加入到3个孔中,并使得接触其中的HAP盘10分钟。
(4)然后去除每孔中的液相,并用2mL无菌人工唾液替代。
(5)然后把盘在37℃,厌氧条件下保持8天。
(6)以2、4和8天的间隔,无菌采集盘并转移至半强度预还原的巯基醋酸盐(thioglycollate)培养基(4.5ml每盘)中。
(7)对于总的革兰氏阴性厌氧菌,对于每个盘按一式两份在新霉素/万古霉素(NV)琼脂上铺上100μL的稀释物10-4、10-5和10-6。
(8)使用无菌涂布器(spreader)对板进行表面铺展,并在37℃、厌氧下温育72小时,之后计数每个板上的菌落数目。
对于每一个试验洁齿剂或对照品计算log10CFU/ml(其中CFU=菌落形成单位)。较低的Log10CFU/ml表明测试的洁齿剂在抑制生物膜生长方面具有更大的效力。
试验的结果示于以下的实施例1中。
实施例1
1.在第一轮生物膜减少试验中,对如列于表1的制剂的减少生物膜生长能力进行评价。使用曼彻斯特大学生物膜生长抑制模型方法(上面的)获得的结果示于表1中,包含从在该方法的第6步孵育8天的盘获得的平均log10CFU/ml。在以下的结果中,对于“统计显著性”共同具有相同字母的制剂在它们的生物膜减少功效上并不显示显著差异。
表1
1.如示于表1的结果显示,含精氨酸的制剂在生物膜减少上具有改善的功效。如示于上表1中的,含1.5%重量的精氨酸的制剂表现优于所有其他测试制剂,如由显著较低的平均Log10CFU/ml值所指出的那样。接下来是具有1.0%重量的精氨酸的制剂,然后是含0.5%重量和3.0%重量的精氨酸的制剂。
Claims (24)
1.一种口腔护理组合物,其包含:
a.呈游离或盐形式的精氨酸;和
b.氧化锌和柠檬酸锌。
2.权利要求1的口腔护理组合物,其中精氨酸以基于组合物的总重量的0.5%重量至3%重量的量存在。
3.权利要求2的口腔护理组合物,其中精氨酸以基于组合物的总重量的1%重量至2.85%重量的量存在。
4.权利要求3的口腔护理组合物,其中精氨酸以基于组合物的总重量的1.17%重量至2.25%重量的量存在。
5.权利要求4的口腔护理组合物,其中精氨酸以基于组合物的总重量的1.4%重量至1.6%重量的量存在。
6.权利要求5的口腔护理组合物,其中精氨酸以基于组合物的总重量的约1.5%重量的量存在。
7.任一项前述权利要求的口腔护理组合物,其中组合物中的锌盐的总浓度是基于组合物的总重量的0.2%重量至5%重量。
8.任一项前述权利要求的口腔护理组合物,其中精氨酸与总锌盐的摩尔比是0.05∶1至10∶1。
9.任一项前述权利要求的口腔护理组合物,其中该组合物包含基于组合物的总重量的0.5%重量至1.5%重量的量的氧化锌和0.25%重量至0.75%重量的量的柠檬酸锌。
10.权利要求9的口腔护理组合物,其中该组合物包含基于组合物的总重量的约1%重量的量的氧化锌和约0.5%重量的量的柠檬酸锌。
11.权利要求9的口腔护理组合物,其中氧化锌与柠檬酸锌的重量比是1.5∶1至4.5∶1,任选1.5∶1至4∶1、1.7∶1至2.3∶1、1.9∶1至2.1∶1或约2∶1。
12.一种依据任一项前述权利要求的口腔护理组合物,其用于减少或抑制口腔中的生物膜形成。
13.一种减少或抑制口腔中的生物膜形成的方法,该方法包括使口腔与依据权利要求1至12的任一项的口腔护理组合物接触。
14.口腔护理组合物中的以下组分的组合在减少或抑制口腔中的生物膜形成中的应用:
a.呈游离或盐形式的精氨酸;和
b.氧化锌和柠檬酸锌。
15.权利要求14的应用,其中精氨酸以基于组合物的总重量的0.5%重量至3%重量的量存在于口腔护理组合物中。
16.权利要求15的应用,其中精氨酸以基于组合物的总重量的1%重量至2.85%重量的量存在于口腔护理组合物中。
17.权利要求16的应用,其中精氨酸以基于组合物的总重量的1.17%重量至2.25%重量的量存在于口腔护理组合物中。
18.权利要求17的应用,其中精氨酸以基于组合物的总重量的1.4%重量至1.6%重量的量存在于口腔护理组合物中。
19.权利要求18的应用,其中精氨酸以基于组合物的总重量的约1.5%重量的量存在于口腔护理组合物中。
20.权利要求14至19中任一项的应用,其中在口腔护理组合物中的锌盐的总浓度是基于组合物的总重量的0.2%重量至5%重量。
21.权利要求14至20中任一项的应用,其中在口腔护理组合物中的精氨酸与总锌盐的摩尔比是从0.05∶1至10∶1。
22.权利要求14至21中任一项的应用,其中氧化锌与柠檬酸锌的重量比是1.5∶1至4.5∶1,任选为1.5∶1至4∶1、1.7∶1至2.3∶1、1.9∶1至2.1∶1或约2∶1。
23.权利要求14至22中任一项的应用,其中氧化锌以基于组合物的总重量的0.5%重量至1.5%重量的量存在于口腔护理组合物中,而柠檬酸锌以基于组合物的总重量的0.25%重量至0.75%重量的量存在于口腔护理组合物中。
24.权利要求23的应用,其中氧化锌以基于组合物的总重量的约1%重量的量存在于口腔护理组合物中,而柠檬酸锌以基于组合物的总重量的约0.5%重量的量存在于口腔护理组合物中。
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