CN106456505A - 固体口腔护理组合物 - Google Patents
固体口腔护理组合物 Download PDFInfo
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- CN106456505A CN106456505A CN201580020218.6A CN201580020218A CN106456505A CN 106456505 A CN106456505 A CN 106456505A CN 201580020218 A CN201580020218 A CN 201580020218A CN 106456505 A CN106456505 A CN 106456505A
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- oral care
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
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- A—HUMAN NECESSITIES
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- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
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Abstract
用于清洁牙齿的固体口腔护理组合物，该组合物包含碳酸钙和聚环氧乙烷。
Description
发明领域
本发明涉及固体口腔护理组合物。
发明背景
口腔护理组合物，例如洁齿剂通常含有牙齿可接受的研磨剂、润湿剂、水和用作增稠剂和这些成分的粘合剂的水溶性聚合物。也少量使用各种各样的其它成分，例如调味剂、甜味剂、防腐剂和氟化物。
在现有技术中已致力于提供无水或降低的水含量的洁齿剂制剂作为与水不相容的口腔护理活性物的更合适的载体。实例包括固体产品形式，例如粉末或片剂。
US 3,431,339描述了用于代替牙膏的压制牙科片剂。该片剂含有均为基本上无水形式的水溶性防龋剂、擦亮剂、发泡剂和可释放的基质的共混物。相比于传统牙膏，这一形式的优点据称是防龋剂在干燥片剂中的改进的贮存稳定性和改进的舌面清洁。
US 3,116,208公开了由碳酸钙和月桂基硫酸钠构成的片剂形式的牙齿清洁剂。该片剂可被牙齿压碎且月桂基硫酸钠在刷洗牙齿时引起发泡。
WO88/10110描述了设计用于在口腔中咀嚼时形成自发泡糊料的牙齿清洁片剂。该片剂含有“擦亮剂、溶胀剂、发泡剂、填充剂、赋味剂（taste-giving agent）、润湿剂、润滑剂、助滑剂和牙齿保护剂，优选氟化亚锡”。这些片剂基本上不含水，以防止氟化亚锡分解。
US2007/0154409描述了由成型为坚实片剂的一些牙粉构成的牙齿清洁片剂 。该片剂由温和牙齿研磨剂与粘合剂和调味剂的组合制成。该片剂被涂层保护，该涂层提供耐水性并可由常用于形成糖果或口香糖球上的涂层的任何成分制成。
US 5,804,165公开了使用二氧化碳源、不可溶的二氧化硅研磨剂和木糖醇的抗牙菌斑口腔组合物 。二氧化碳来自碳酸氢盐。该泡腾片转变为在口腔唾液中含固体二氧化硅的悬浮液。
US 8,192,724描述了用于口腔的水溶性、非研磨性、泡腾的口腔护理片剂。该片剂包含混合的二氧化碳源、酸源和成片材料以形成具有少于0.2%水的可咀嚼片剂。
尽管有上述现有技术，固体产品形式例如粉末或片剂尚未获得消费者的广泛接受。缺点包括不合意的感官特性，例如沙质或粉状口感。
本发明的目标是提供具有改进口感的片剂。
发明概述
本发明提供用于清洁牙齿的固体口腔护理片剂组合物，该组合物包含碳酸钙和聚环氧乙烷。
本发明还涉及清洁牙齿的方法，其包括咀嚼如上所述的片剂的步骤。
本发明的另一方面是聚环氧乙烷给予如上所述的片剂顺滑感觉的用途。
发明详述
本发明涉及固体口腔护理组合物，该组合物优选是片剂形式，更优选是压制片剂的形式。
本发明的组合物包含碳酸钙，该碳酸钙是用于从牙齿表面机械除去残渣和清除牙菌斑的微粒状材料。
合适的微粒状碳酸钙的特征在于其组成初级颗粒的特定形状和尺寸。
“初级颗粒”是指单个颗粒，其定义为可通过电子显微镜分析看见的最小离散颗粒（例如，单个晶体）。
本发明上下文中所述的聚合物分子量涉及Mw。
初级颗粒可在某些条件下结合以形成更大的次级结构，例如聚集体或附聚物。
为了本发明的目的，合适的微粒状碳酸钙源包括结晶碳酸钙。
术语“结晶”（在微粒状碳酸钙上下文中）通常是指其中至少50重量%，优选至少75重量%，更优选至少90重量%，最优选大于95重量%和理想地大于99重量%的碳酸钙颗粒为晶体形式的微粒状碳酸钙。
术语“晶体”是指由以平表面为界的有序重复排列的原子组成的基本上完全致密的固体，所述平表面是内部结构的外部表达。晶体可通过本领域技术人员已知的标准技术例如X射线衍射进行鉴别和表征。
适用于本发明的结晶碳酸钙天然可得（通过提取和加工天然矿石）或合成可得（通过化学沉淀）。存在三种主要结晶多晶型物：方解石、霰石和较不常见的球霰石。碳酸钙的球霰石形式是亚稳态的且不可逆地转变成方解石和霰石。对于这些结晶形式的每一种，存在多种不同的形态（晶癖）。方解石结晶多晶型是最常用的碳酸钙晶体形式。文献中已报道了方解石的超过300种结晶形式。
适用于本发明的微粒状碳酸钙（例如上述材料）的平均粒度可在宽范围内变化。通常，该平均粒度为50微米或更小。
粒度（例如晶体尺寸）可通过本领域技术人员已知的标准技术例如沉降测定。对于本发明，粒度应使用Malvern粒度分析仪测定。在本申请上下文中，粒度测量涉及d(50)。
已采用至少50重量%，优选至少80重量%的晶体是平均粒度d(50)为30微米或更小，优选15微米或更小的菱形方解石晶体的结晶碳酸钙获得良好的清洁性能。最优选的是平均粒度d(50)为0.1至30微米，优选0.1至15微米，最优选2至10微米（使用Malvern粒度分析仪测量）的结晶碳酸钙。
具有上述定义的尺寸和形状的合适的结晶碳酸钙源包括天然重质碳酸钙研磨剂，其通常可由开采和机械磨碎沉积岩例如石灰岩或白垩，或变质岩例如大理石获得。天然碳酸钙通常是方解石多晶型的，其晶体形态通常可表征为菱形。
优选的上述类型的天然重质碳酸钙研磨剂选自重质石灰岩（ground limestone）、白垩或大理石，其任选是精制或部分精制以除去杂质的且平均粒度d(50)（如上所述的“中值ESD”）为大约30微米或更小，更优选为大约1至15微米，且最优选为大约2至10微米。商购可得的实例包括由OMYA™ AG公司以名称OMYACARB™ 2-AV 和OMYACARB™ 5-AV销售的那些材料。它们是平均粒度（如上所述的“中值 ESD”）分别为大约2和大约5微米的细的重质高纯度白色大理石研磨剂。
其它类型的微粒状碳酸钙也可能是合适的，这取决于消费者视角所需的清洁和研磨的特定平衡。
也可使用任何上述研磨清洁剂的混合物。
本发明的组合物中的碳酸钙总量将取决于所用的一种或多种特定试剂，但通常为该组合物总重量的3至80重量%，优选15重量%至75重量%，更优选30重量%至70重量%，最优选40至50重量%。
本发明组合物包含聚环氧乙烷。优选地，聚环氧乙烷的分子量为大于500000(Mw)，更优选为1000000 至7000000 (Mw)。
该组合物中的聚环氧乙烷重量优选为整个组合物的0.1至3重量%，更优选0.5至2重量%。
优选的是，如果该聚环氧乙烷以片剂中的混合物的一部分而非以外部涂层的形式存在。
优选地，聚环氧乙烷与碳酸钙的重量比为1:至1:10至1:100，更优选1:25至1:55。
用于形成所述组合物的合适发泡剂包括表面活性剂。表面活性剂有助于提高在与唾液接触时固体口腔护理组合物的溶解速率并有助于在使用期间使该组合物发泡。
合适的表面活性剂包括阴离子表面活性剂，例如下列物质的钠、镁、铵或乙醇胺盐：C8至C18烷基硫酸盐（例如月桂基硫酸钠）、磺基琥珀酸C8至C18烷基酯盐（例如磺基琥珀酸二辛酯钠）、磺基乙酸C8至C18 烷基酯盐（例如月桂醇磺基乙酸酯钠）、C8至C18烷基肌氨酸盐（例如月桂基肌氨酸钠）、C8至C18 烷基磷酸盐（其可任选包含多至10个环氧乙烷和/或环氧丙烷单元）和硫酸化单甘油酯。其它合适的表面活性剂包括非离子表面活性剂，例如任选的聚乙氧基化脂肪酸脱水山梨醇酯、聚环氧乙烷的乙氧基化脂肪酸酯（ethoxylated fattyacids, esters of polyethylene oxide）、脂肪酸单甘油酯和二甘油酯的乙氧基化物和环氧乙烷/环氧丙烷嵌段聚合物。其它合适的表面活性剂包括两性表面活性剂，例如内铵盐（betaines）或磺基内铵盐。
用于本发明的优选的表面活性剂包括选自月桂基硫酸钠、月桂醇磺基乙酸酯钠、椰油酰胺丙基内铵盐、α烯烃磺酸钠、磺基琥珀酸二辛酯钠、十二烷基苯磺酸钠和它们的混合物的那些无水表面活性剂。
也可使用任何上述材料的混合物。
并入本发明组合物中的表面活性剂的总量通常为大约0.2至大约5%，这为基于该组合物总重量的表面活性剂总重量。
该组合物还可包含各种附加的成分以改进例如容易加工、产品性能和/或消费者接受度的方面。
例如，该组合物可包含通过提供气泡促进发泡的泡腾剂。用于本文的合适的泡腾剂包括通过碳酸盐与酸的反应提供泡腾的酸/碳酸盐对。碳酸氢钠和碳酸钠代表优选的碳酸盐。然而，也可使用碳酸钾、碳酸铵、碳酸镁、碳酸钙或其它金属或有机盐。合适的酸包括柠檬酸、富马酸、酒石酸、苹果酸、己二酸和其它食用酸。
并入本发明组合物的泡腾剂的量通常为大约0.5至大约10%，优选大约1至7%，这为基于该组合物的总重量的泡腾剂（例如酸/碳酸盐对）总重量。
也可使用任何上述材料的混合物。
该组合物将优选包含一种或多种在分子中具有2个或更多个羟基的有机多元醇（下文称为“有机多元醇”）。这些材料可用作粘合剂以有助于在加工过程中压制组合物。它们也可用作湿润剂。湿润剂帮助防止该组合物在暴露于空气中时硬化或结晶。它们也帮助该组合物为口腔带来湿润感觉 ，并可在一些情况下给予合意的甜味。用于本文的合适的有机多元醇包括蔗糖、右旋糖、麦芽糖、果糖、丙三醇、山梨醇、木糖醇、甘露醇、乳糖醇、麦芽糖醇、异麦芽糖醇（isomalt）、赤藓糖醇、聚环氧乙烷、聚丙二醇、丙二醇和氢化的部分水解的多糖，例如氢化的淀粉水解产物。用于本文的优选的有机多元醇是非致龋的多元醇，例如丙三醇、山梨醇、麦芽糖醇和木糖醇。
也可使用任何上述材料的混合物。
并入本发明组合物的有机多元醇的量通常为大约5至大约70%，优选大约10至40%，这是基于该组合物的总重量的有机多元醇总重量。
本发明的组合物通常是不含水的。“不含水”通常是指不故意将任何显著量的水加入该组合物中。然而，术语“不含水”不意味着不能存在少量水，例如作为其与吸湿原料结合的结果。因此，为了本发明的目的，术语“不含水”通常是指水以基于该组合物总重量不大于大约5%，更优选不大于大约3重量%的量存在。
本发明的固体口腔护理组合物将通常为离散的单个单位剂量，例如丸剂、锭剂或片剂的形式。这样的单个单位剂量的大小将通常为200 mg至5000 mg，优选250 mg至2000mg，更优选500至1500 mg。
根据本发明的组合物特别适合作为口腔护理活性物的载体，所述活性物在物理或化学上可能与水不相容，或其在含水环境中的作用可能较不有效。
可能特别适合于包含在本发明的组合物中的口腔护理活性物的具体实例是：
水溶性或微水溶性的锌离子源 ，例如氯化锌、乙酸锌、葡萄糖酸锌、硫酸锌、氟化锌、柠檬酸锌、乳酸锌、氧化锌、单甘油锌、酒石酸锌、焦磷酸锌和马来酸锌；
口腔护理酶体系，例如产生过氧化氢的酶体系（例如，氧化还原酶葡糖氧化酶）、淀粉葡糖苷酶、葡聚糖酶和/或非水溶性葡聚糖酶（任选在锌离子存在下提供化合物和/或8-羟基喹啉衍生物）、乳过氧化物酶、乳铁蛋白、溶菌酶和它们的混合物；
氟化物源，例如氟化钠、 氟化亚锡、单氟磷酸钠、氟化锌铵（zinc ammoniumfluoride）、氟化锡铵（tin ammonium fluoride）、氟化钙、氟化钴铵（cobalt ammoniumfluoride）和它们的混合物；
可源自植物的抗氧化剂，例如类黄酮、儿茶酸、多酚和单宁化合物和它们的混合物；
抗氧化剂维生素，例如生育酚和/或其衍生物、抗坏血酸和/或其衍生物或它们的混合物。
用于牙齿再矿化（即在牙齿上原位生成羟基磷灰石）的试剂，例如钙源和磷酸盐源的混合物，其在递送至牙齿时导致在牙齿上原位生成羟基磷灰石。
也可使用任何上述材料的混合物。
本发明的组合物还可含有本领域中常规的其它任选成分，例如抗牙结石剂、缓冲剂、调味剂、甜味剂、着色剂、不透明剂、防腐剂、防敏剂、抗微生物剂等。
本发明的固体口腔护理组合物用于清洁口腔表面。该组合物是不旨在为了治疗剂的全身给药而吞咽而是施用于口腔，用于处理口腔和然后吐出的口腔组合物。通常，该组合物与清洁工具例如牙刷结合使用，通常通过将其施用于牙刷的刷毛并然后刷洗口腔的可及表面。
本发明的片剂优选使用1至8吨的压实方法制造。优选地，该片剂是不经涂覆的。
参考下面的非限制性实施例进一步举例说明本发明。本发明的实施例通过数字说明，对比例通过字母说明。
实施例
| 商品名 | 化学名 | 实施例A | 实施例1 |
| 重量% | 重量% | ||
| Empicol LZN | 月桂基硫酸钠 | 3 | 3 |
| Menthol | 薄荷醇 | 0.5 | 0.5 |
| Novamint | 合成调味剂 | 6 | 6 |
| Chalk | 碳酸钙 | 45.2 | 45.2 |
| Sodium saccharin | 糖精钠 | 0.3 | 0.3 |
| Xylisorb DC | 木糖醇 | 至100 | 至100 |
| Polyox WSR-301 | 聚环氧乙烷聚合物 | 0 | 1 |
为了形成所述片剂，将所述材料共混在一起。一旦共混，将1g量称入片剂模头中并压制至所需力（3吨）。
所述片剂由经培训的小组评估。所有片剂呈现在陪替氏培养皿（petri dishes）中。将所述片剂置于口中并咀嚼，然后当产生泡沫时；小组成员刷洗他们的牙齿并最终吐出任何残留物，如果需要的话然后冲洗。小组将顺滑感觉属性的强度“评级”。
要求中间实验（prototype）参与者吃2-3片薯片（Walker即食加盐）并用室温水冲洗他们的口腔。这一过程清洁前面味道的味觉。在最后的实验之后，如果需要的话仅冲洗。
小组测试的结果如下：
| 感官属性 | 实施例1得分 | 实施例A得分 |
| 口中的顺滑感觉 | 70.4 | 61.9 |
得分越高，该属性越强。
该结果表明，本发明的片剂在使用后在口中感觉较不沙质，并在使用中在口中感觉顺滑。
Claims (12)
1.用于清洁牙齿的固体口腔护理组合物，所述组合物包含碳酸钙和聚环氧乙烷。
2.根据权利要求1的固体口腔护理组合物，其中所述聚环氧乙烷的分子量为大于500000 (Mw)。
3.根据权利要求2的固体口腔护理组合物，其中所述聚环氧乙烷的分子量为1000000至7000000 (Mw)。
4.根据前述权利要求任一项的固体口腔护理组合物，其中聚环氧乙烷的水平是所述整个组合物的0.1至3重量%。
5.根据前述权利要求任一项的固体口腔护理组合物，其中碳酸钙的粒度为0.1至30微米，优选0.1至15微米，最优选2至10微米，如通过Malvern粒度分析仪测量的。
6.根据前述权利要求任一项的固体口腔护理组合物，其中聚环氧乙烷与碳酸钙的重量比为1:30至1:50。
7.根据前述权利要求任一项的固体口腔护理组合物，其进一步包含选自无水表面活性剂的发泡剂，该无水表面活性剂选自月桂基硫酸钠、月桂醇磺基乙酸酯钠、椰油酰胺丙基内铵盐、α烯烃磺酸钠、磺基琥珀酸二辛酯钠、十二烷基苯磺酸钠和它们的混合物。
8.根据前述权利要求任一项的固体口腔护理组合物，其中所述组合物还包含一种或多种选自丙三醇、山梨醇、麦芽糖醇、木糖醇和它们的混合物的有机多元醇。
9.根据前述权利要求任一项的固体口腔护理组合物，其中所述聚环氧乙烷在所述固体口腔护理组合物中以混合物的一部分的形式存在。
10.根据前述权利要求任一项的固体口腔护理组合物，其为压制片剂的形式。
11.清洁牙齿的方法，其包括咀嚼如前述权利要求任一项中所述的片剂的步骤。
12.聚环氧乙烷给予如前述权利要求任一项中所述的片剂顺滑感觉的用途。
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| BR112019017654B1 (pt) * | 2017-03-13 | 2022-10-04 | Unilever Ip Holdings B.V | Composições de cuidado oral e uso de um polímero |
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| EP3131639A1 (en) | 2017-02-22 |
| BR112016019201A2 (pt) | 2017-10-10 |
| WO2015158637A1 (en) | 2015-10-22 |
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