CN110418632B - 口腔护理组合物 - Google Patents
口腔护理组合物 Download PDFInfo
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- CN110418632B CN110418632B CN201880017904.1A CN201880017904A CN110418632B CN 110418632 B CN110418632 B CN 110418632B CN 201880017904 A CN201880017904 A CN 201880017904A CN 110418632 B CN110418632 B CN 110418632B
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- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
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- KWLMIXQRALPRBC-UHFFFAOYSA-L hectorite Chemical compound [Li+].[OH-].[OH-].[Na+].[Mg+2].O1[Si]2([O-])O[Si]1([O-])O[Si]([O-])(O1)O[Si]1([O-])O2 KWLMIXQRALPRBC-UHFFFAOYSA-L 0.000 description 1
- 229910000271 hectorite Inorganic materials 0.000 description 1
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- 239000004615 ingredient Substances 0.000 description 1
- 235000010494 karaya gum Nutrition 0.000 description 1
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- 239000000463 material Substances 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 210000000214 mouth Anatomy 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 229920001206 natural gum Polymers 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 1
- WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 description 1
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- 150000003839 salts Chemical class 0.000 description 1
- GCLGEJMYGQKIIW-UHFFFAOYSA-H sodium hexametaphosphate Chemical compound [Na]OP1(=O)OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])O1 GCLGEJMYGQKIIW-UHFFFAOYSA-H 0.000 description 1
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- 238000007910 systemic administration Methods 0.000 description 1
- RYCLIXPGLDDLTM-UHFFFAOYSA-J tetrapotassium;phosphonato phosphate Chemical class [K+].[K+].[K+].[K+].[O-]P([O-])(=O)OP([O-])([O-])=O RYCLIXPGLDDLTM-UHFFFAOYSA-J 0.000 description 1
- 239000001577 tetrasodium phosphonato phosphate Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
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- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/25—Silicon; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/39—Derivatives containing from 2 to 10 oxyalkylene groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- 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
- A61K8/86—Polyethers
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Emergency Medicine (AREA)
- Cosmetics (AREA)
Abstract
本发明涉及包含二氧化硅磨料、非离子表面活性剂和分子量(Mn)为300,000或更大的聚环氧乙烷聚合物的口腔护理组合物。
Description
技术领域
本发明涉及口腔护理组合物。更具体而言，本发明涉及具有低磨蚀性同时保持所期望的清洁性能的口腔护理组合物。
背景技术
要求用于口腔护理组合物如洁牙剂中的磨料有效地去除在牙齿表面上的薄皮上积累的外源性色斑、牙菌斑和食物残渣。
一般而言，通过使用具有增大的磨蚀性的磨料可以增大物理去除色斑、菌斑和食物残渣的功效。然而，增大磨蚀性还增大可能损伤牙齿表面的风险。
因此，存在对于表现出令人满意的清洁程度还不会过度地磨蚀和损伤牙齿的口腔护理组合物的持续的需求。
EP 0 319 884公开了选自聚丙烯酰胺衍生物的线性高分子量聚合物减小磨蚀性并且增大清洁度和色斑去除。
US 4,743,274涉及改变晶体形貌以提供在口腔组合物中使用的高清洁度、低磨损磨料。其描述了如何在由磷酸氢钙无水物(二代磷酸钙无水物)组成的磨料的情况下，减小平均微晶尺寸，产生同时满足高牙齿清洁能力和低牙齿表面磨损性的要求的材料。
发明内容
本申请涉及本发明的口腔护理组合物如何表现出令人满意的清洁程度，还不会过度地磨蚀和损伤牙齿。本发明的口腔护理组合物的另一个优点是其足够温和以在由比天然牙釉质明显更软的聚合物如丙烯酸树脂(PMMA)制成的桥托、托牙及其他形式的假牙上使用。
本发明提供包含二氧化硅磨料、非离子表面活性剂和分子量(Mn)为300,000或更大的聚环氧乙烷聚合物的口腔护理组合物，所述非离子表面活性剂包含脂肪醇的聚乙二醇醚。
本发明还涉及分子量(Mn)为300,000或更大的聚环氧乙烷聚合物用于减轻牙膏的磨蚀性的用途。
具体实施方式
所述口腔护理组合物包含优选基于所述组合物的总重量0.2至10重量％的量的非离子表面活性剂，所述非离子表面活性剂包含脂肪醇的聚乙二醇醚。聚乙二醇醚每个单元具有20至40个环氧乙烷基。此类合适的表面活性剂的例子包括称作Steareth表面活性剂的表面活性剂组，如Steareth 30。非离子表面活性剂的含量优选为总组合物的0.5至7重量％，更优选为0.8至5重量％，特别优选为总组合物的1至3重量％。
在所述组合物中可以存在阴离子表面活性剂，但优选的是其含量低于总组合物的0.5重量％，更优选0.1重量％。
虽然可以存在其他表面活性剂，但优选的是其被限制到低于总组合物的0.5重量％、优选小于总组合物的0.1重量％的含量。
所述口腔护理组合物包含二氧化硅磨料。二氧化硅的存在量优选为总组合物的2至75重量％，更优选为总组合物的3至40重量％，特别优选为总组合物的3至25重量％。
所述组合物可以包含其他磨料，但是若存在则其含量应当小于二氧化硅磨料。其他合适的磨料包括碳酸钙、磷酸二钙、磷酸三钙、煅烧氧化铝、钠和钾的偏磷酸盐、钠和钾的焦磷酸盐、三偏磷酸钠、六偏磷酸钠、颗粒状羟基磷灰石及其混合物。
本发明的组合物包含分子量(Mn)为300,000或更大、分子量(Mn)更优选为800,000或更大、分子量(Mn)特别优选为2百万或更大的聚环氧乙烷聚合物。
在本发明中使用的聚环氧乙烷优选为固态无色的水溶性树脂。
优选的聚环氧乙烷聚合物在商业上称作Polyox，特别优选为来自陶氏化学公司的Polyox WSR301。
聚环氧乙烷聚合物的含量优选为总组合物的0.05至5重量％，更优选为0.1至3重量％，特别优选为总组合物的0.3至2重量％。
在所述组合物中总表面活性剂与聚环氧乙烷聚合物的重量比优选为20:1至12，更优选为12:1至1:1，特别优选为8:1至2:1。
在本发明的范畴内高度优选的产品形式种类是洁牙剂。术语“洁牙剂”是指用于清洁口腔表面的配制品。所述洁牙剂是口腔组合物，其并不是出于全身施用治疗剂的目的而故意地吞咽，而是出于口腔活性的目的在口腔中停留足够的时间以接触基本上全部的牙齿表面和/或粘膜组织。所述洁牙剂优选适合于使用牙刷的应用并且在使用后冲洗掉。所述洁牙剂优选为可挤出的半固态形式，如膏状、糊状或凝胶(或其混合物)。
本发明的组合物，特别是洁牙剂组合物，通常包含基于所述洁牙剂的总重量40至99重量％的量的液体连续相。所述液体连续相典型地包含各种不同的相对量的水和多元醇的混合物，其中水的量一般为10至45重量％(基于所述洁牙剂的总重量)，多元醇的量一般为20至70重量％(基于所述洁牙剂的总重量)。典型的多元醇包括润湿剂，如甘油、山梨糖醇、聚乙二醇、聚丙二醇、丙二醇、木糖醇(及其他可食用的多元醇)、部分氢化的水解多糖及其混合物。山梨糖醇是特别优选的。
本发明的组合物特别优选是基于有机多元醇的。在本发明的范畴内，术语“基于有机多元醇”意味着所述组合物并不是油基或水基，而是有机多元醇(如上所定义)是所述组合物中的主要组分。“主要组分”是指有机多元醇(如上所定义)合在一起考虑时与任何其他化合物相比占据所述组合物的重量的更大部分。
此外，所述组合物，优选洁牙剂，通常包含基于所述洁牙剂的总重量0.1至12重量％、更优选0.3至10重量％的量的粘合剂或增稠剂。合适的粘合剂或增稠剂包括羧基乙烯基聚合物(例如与聚烯丙基蔗糖或聚烯丙基季戊四醇交联的聚丙烯酸)、羟乙基纤维素、羟丙基纤维素、纤维素醚的水溶性盐(如羧甲基纤维素钠和羧甲基羟乙基纤维素钠)、天然胶(如卡拉胶、刺梧桐胶、瓜尔豆胶、黄原胶、阿拉伯胶及西黄蓍胶)、细碎的二氧化硅、水辉石、胶体硅酸镁铝及其混合物。
本发明的组合物(例如特别是洁牙剂)还可以包含其他任选存在的在现有技术中惯常使用的成分，如氟离子源、抗结石剂、缓冲剂、香味剂、甜味剂、着色剂、乳浊剂、防腐剂、抗敏剂和抗微生物剂。
参照以下非限制性实施例进一步阐述本发明。根据本发明的实施例由数字表示，对比例由字母表示。
实施例
制备以下组合物。
表1
| 化学名 | 实施例A | 实施例B |
| 山梨糖醇 | 45 | 45 |
| Polyox WSR301(MW 4百万) | 0 | 1 |
| 二氧化硅磨料 | 10 | 10 |
| 增稠二氧化硅 | 7.5 | 7.5 |
| 聚乙二醇 | 5 | 5 |
| 月桂基硫酸钠 | 1.5 | 1.5 |
| 二氧化钛 | 1 | 1 |
| 羧甲基纤维素钠 | 0.63 | 0.63 |
| 氟化钠 | 0.32 | 0.32 |
| 水和少量物质 | 至100 | 至100 |
表2
| 化学名 | 实施例C | 实施例D |
| 碳酸钙 | 40 | 40 |
| 苯甲醇 | 0.5 | 0.5 |
| 增稠二氧化硅 | 4.7 | 4.7 |
| 月桂基硫酸钠 | 2.2 | 2.2 |
| 山梨糖醇 | 20 | 20 |
| 磷酸三钠 | 0.5 | 0.5 |
| 羧甲基纤维素钠 | 0.6 | 0.6 |
| 二氧化钛 | 1 | 1 |
| 单氟磷酸钠 | 1.11 | 1.11 |
| Polyox WSR301(MW 4百万) | 0 | 1 |
| 水和少量物质 | 至100 | 至100 |
表3
| 实施例E | 实施例1 | |
| 化学名 | ％w/w | ％w/w |
| 山梨糖醇 | 65 | 65 |
| 聚乙二醇 | 1.5 | 1.5 |
| 氟化钠 | 0.32 | 0.32 |
| 糖精钠 | 0.2 | 0.2 |
| 磷酸三钠 | 0.5 | 0.5 |
| Polyox WSR301(MW 4百万) | 0 | 1 |
| 聚(甲基乙烯基醚/马来酸) | 1 | 1 |
| 增稠二氧化硅 | 4.5 | 4.5 |
| 二氧化硅磨料 | 8 | 8 |
| 二氧化硅磨料 | 1.65 | 1.65 |
| 羧甲基纤维素钠 | 0.52 | 0.52 |
| Steareth 30 | 1.8 | 1.8 |
| 水和少量物质 | 至100 | 至100 |
表4
| 实施例F | |
| 化学名 | ％w/w |
| 山梨糖醇 | 65 |
| 聚乙二醇 | 1.5 |
| 氟化钠 | 0.32 |
| 糖精钠 | 0.2 |
| 磷酸三钠 | 0.5 |
| Polyox WSR301(MW 4百万) | 0 |
| 聚(甲基乙烯基醚/马来酸) | 1 |
| 增稠二氧化硅 | 4.5 |
| 二氧化硅磨料 | 8 |
| 二氧化硅磨料 | 1.65 |
| 羧甲基纤维素钠 | 0.52 |
| 月桂基硫酸钠 | 1.8 |
| 水和少量物质 | 至100 |
表5
| Ex.G | Ex.2 | Ex.3 | Ex.4 | Ex.5 | Ex.6 | Ex.H | |
| 山梨糖醇 | 65 | 65 | 65 | 65 | 65 | 65 | 65 |
| Polyox WSR301(MW 4百万) | 0.1 | ||||||
| Polyox WSR301(MW 4百万) | 0.5 | ||||||
| Polyox WSR301(MW 4百万) | 1.0 | ||||||
| Polyox 12K(MW 1百万) | 1 | 2 | |||||
| Polyox N10(100,000) | 1 | ||||||
| 聚乙二醇 | 1.5 | 1.5 | 1.5 | 1.5 | 1.5 | 1.5 | 1.5 |
| 磷酸三钠 | 1.1 | 1.1 | 1.1 | 1.1 | 1.1 | 1.1 | 1.1 |
| 二氧化硅磨料 | 8 | 8 | 8 | 8 | 8 | 8 | 8 |
| 增稠二氧化硅 | 3.1 | 3.1 | 3.1 | 3.1 | 3.1 | 3.1 | 3.1 |
| 二氧化硅磨料 | 1.7 | 1.7 | 1.7 | 1.7 | 1.7 | 1.7 | 1.7 |
| 羧甲基纤维素钠 | 0.6 | 0.6 | 0.6 | 0.6 | 0.6 | 0.6 | 0.6 |
| 聚(甲基乙烯基醚/马来酸) | 1 | 1 | 1 | 1 | 1 | 1 | 1 |
| Steareth 30 | 1.8 | 1.8 | 1.8 | 1.8 | 1.8 | 1.8 | 1.8 |
| 水和少量物质 | 至100 | 至100 | 至100 | 至100 | 至100 | 至100 | 至100 |
Polyox的分子量如下：
WSR301 Ex陶氏化学公司4百万
12K Ex陶氏化学公司1百万
N10 Ex陶氏化学公司100,000
表6表明，与包含碳酸盐磨料的配制品相比，在包含二氧化硅磨料的配制品中由于存在高分子量聚环氧乙烷聚合物，导致RDA的减幅增大。
表6
| 配制品 | RDA(s.e.) |
| 实施例A | 100.42(2.40) |
| 实施例B | 71.36(2.82) |
| 实施例C | 174.57(1.69) |
| 实施例D | 163.12(5.54) |
上表表明，在包含二氧化硅磨料的组合物中存在Polyox WS301时，配制品的磨蚀性显著降低。这一效果在包含碳酸钙磨料的配制品中并不如此明显。
表7
| 配制品编号 | 平均RDA(s.e.) | PCR(s.d.)** |
| 实施例F | 107.41(3.51) | -- |
| 实施例E | 91.90(2.98) | 22(10) |
| 实施例1 | 48.21(3.77) | 57(6) |
表7表明，根据本发明的实施例具有显著减小的磨蚀度连同增强的清洁性能。
表8
| 牙膏 | 平均RDA值(S.D.) |
| 实施例G | 110.08(5.54) |
| 实施例2 | 98.27(2.71) |
| 实施例3 | 61.04(3.21) |
| 实施例4 | 60.29(6.36) |
| 实施例H | 104.51(4.08) |
| 实施例5 | 85.05(4.76) |
| 实施例6 | 86.83(4.93) |
Polyox的分子量如下：
WSR301 4百万
12K 1百万
N10 100,000
表8表明聚环氧乙烷聚合物的分子量在减小牙膏的磨蚀性中的重要性。
Claims (11)
1.包含二氧化硅磨料、非离子表面活性剂和分子量(Mn)为300,000或更大的聚环氧乙烷聚合物的口腔护理组合物，其中所述非离子表面活性剂包含脂肪醇的聚乙二醇醚，所述二氧化硅磨料的含量为总配制品的3至20重量％，所述聚环氧乙烷聚合物的含量为总组合物的0.1至3重量％，所述非离子表面活性剂的含量为总组合物的0.1至5重量％。
2.根据权利要求1所述的口腔护理组合物，其中所述聚环氧乙烷聚合物的分子量(Mn)为800,000或更大。
3.根据权利要求1或2所述的口腔护理组合物，其中所述聚环氧乙烷聚合物的分子量(Mn)为2百万或更大。
4.根据权利要求1或2所述的口腔护理组合物，其中总表面活性剂与聚环氧乙烷聚合物的重量比为12:1至1:1。
5.根据权利要求1或2所述的口腔护理组合物，其中所述非离子表面活性剂是乙氧基化度为20至40的乙氧基化的表面活性剂。
6.根据权利要求1或2所述的口腔护理组合物，其中所述非离子表面活性剂是Steareth30。
7.根据权利要求1或2所述的口腔护理组合物，其还包含多元醇。
8.根据权利要求7所述的口腔护理组合物，其中所述多元醇是山梨糖醇。
9.根据权利要求1或2所述的口腔护理组合物，其中所述组合物中多元醇的含量大于总组合物的30重量％。
10.根据权利要求1或2所述的口腔护理组合物，其是洁牙剂的形式。
11.分子量(Mn)为300,000或更大的聚环氧乙烷聚合物用于减轻包含二氧化硅和非离子表面活性剂的牙膏的磨蚀性的用途，其中所述非离子表面活性剂包含脂肪醇的聚乙二醇醚，所述二氧化硅磨料的含量为总配制品的3至20重量％，所述聚环氧乙烷聚合物的含量为总组合物的0.1至3重量％，所述非离子表面活性剂的含量为总组合物的0.1至5重量％。
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