TW200417379A - Compositions for removing stains from dental surfaces, and methods of making and using the same - Google Patents
Compositions for removing stains from dental surfaces, and methods of making and using the same Download PDFInfo
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- TW200417379A TW200417379A TW092130470A TW92130470A TW200417379A TW 200417379 A TW200417379 A TW 200417379A TW 092130470 A TW092130470 A TW 092130470A TW 92130470 A TW92130470 A TW 92130470A TW 200417379 A TW200417379 A TW 200417379A
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- 238000012546 transfer Methods 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
- UNXRWKVEANCORM-UHFFFAOYSA-I triphosphate(5-) Chemical compound [O-]P([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O UNXRWKVEANCORM-UHFFFAOYSA-I 0.000 description 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 229910052721 tungsten Inorganic materials 0.000 description 1
- 230000036269 ulceration Effects 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 210000004885 white matter Anatomy 0.000 description 1
- 239000009637 wintergreen oil Substances 0.000 description 1
- 229940105296 zinc peroxide Drugs 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/36—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/36—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
- A23G3/362—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds containing inorganic compounds
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G4/00—Chewing gum
- A23G4/06—Chewing gum characterised by the composition containing organic or inorganic compounds
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G4/00—Chewing gum
- A23G4/06—Chewing gum characterised by the composition containing organic or inorganic compounds
- A23G4/064—Chewing gum characterised by the composition containing organic or inorganic compounds containing inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0216—Solid or semisolid forms
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- 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
- A61K8/22—Peroxides; Oxygen; Ozone
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- 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
- A61K8/24—Phosphorous; Compounds thereof
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- 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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
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- 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
Landscapes
- Life Sciences & Earth Sciences (AREA)
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
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- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Emergency Medicine (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Cosmetics (AREA)
- Confectionery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Detergent Compositions (AREA)
Description
200417379 玖、發明說明: 【發明所屬之技術領域】 而言’本發㈣有關用於促進牙齒衛生巧潰移除 、'且…特別係關於含有新騎潰 、責 移除組合物、及其製造方法及使用方法。 牙… 【先前技術】 潔白無暇的牙齒長久以來為 成I年卓、主初 所而。不幸若未能徹 ⑽牙,則牙齒可能因存在於食物、飲料、芬草等 =色(造成顏色)物質而變色或料,以及可能因來自 =例二血液、以汞齊為主之牙齒填料及抗生素(例如四環 象)^U及料。呈料染外觀之牙齒結構為 冢牙質以及獲得性薄膜。牙、 成,大部分無機物質係王要係由無機物質形 -牛人體形式,料質進 / 要呈膠原形式之有機物質。相反地,象牙 貝係由約2 0 %蛋白質组点兮疋 …… 白質包括膠原,差額係由矣 機物質組成,象牙質類似缺瑯質,無… 灰石晶體。獲得性薄膜為存在 歹工土外 丁仏乃、T齒砝螂質表面的本唇 質層,該薄膜於徹底清潔牙齒後快速重新生出。。 =齒變色可能來自於外因性冷潰及/或内因性污潰。獲得 性薄膜之外因性污潰係由於例、 、 ^ 、 鞣故以及其它捕捉於且緊 念結合於牙齒表面含蛋白哲爲、 、 °蛋白貝層《多朌化合物造成的結果。 :種類型污潰造成的變色通常可藉機械性牙齒清潔方法去 除。相反地,内因性污清+目 - ^ 、 万;’亏〉貝化合物滲透通過琺瑯 貝,甚至渗透通過象牙質,或另外污潰係來自於牙齒内部 89100.doc 200417379 來源。由内因性污潰造成的變色不容易使用機械式牙齒清 ’恭万法去除。化學方法係利用可滲透入牙齒結構的物質, 内因性π潰通常需要化學方法來消除變色。如此,内因性 牙齒3潰通常比外因性牙齒污潰更棘手且更難解決。 小』闽么w々a -凡亏万法通常 係基於使用磨料、水解劑或氧化劑來分解污潰物質。第一 種万法涉及使用通常用於牙膏製劑的粗糖磨料或研磨劑來 以機械万式磨切潰。含磨料之典型製劑為牙膏、凝膠或 牙粉’此寺製劑需要緊密接觸牙齒。典型地要求刷洗以及 類似的擦洗或研磨動作來補償俾成功地移除污潰。第二方 =,包括蛋白質分㈣之水解劑可用於美㈣齒。此等 產品通常係呈糊膏或凝膠形式, 除已妹插η Μ此寺產功用係經由移 舍已..·:捕捉…貝之牙菌斑及牙結石來美白牙齒。 ::劑例如過氧化脲、過氧化氯或過氧化絲 釋放出經基基團,並可分二:化風吴白牙齒係經由 %牙囷斑/污漬複合體而形成可萨 磨料而沖洗切或移除㈣式 /成了猎 乳化劑處理,依攄過 虱化物來源及其濃度而定典型需 結果。 有足夠時間來達成良妤 &…潰移除成分,包括界面活性劑域 /性劑、及螯合劑如多磷酸鹽由於具 π 1 ,故也曾i 〃 艮好污潰移除性 故也曰摻以〉7潰移除組合物1 。例如過量界面活性劑可能造成組刀右干缺 味。螯合劑也可提供良料潰移除===的^ 但螯合劑若添力 89I00.doc 200417379 量 過量’也會對組合物之口味造成負面影響⑽味、苦味及金 屬味)。如此雖然螯合劑及界面活性#i4良好污潰移除劍, ,其添加至組合物之量限於可避免或最小化前述問題之用 因此牙齒吴白業界之一大進展係提供—種組合物,其可 由牙齒表面移“潰,科可維持滿意的感官及口味性質 。另—優點係提供-種組合物’其可隨時經由方便的媒介 投予溫血動物(包括人類)。業界進—步較佳係採用口香糖以
及糖果組合物作為輸送污潰移除劑至牙酱的有效媒介,原 Q在万;口香糖及糖果就溫血動物而言只要耗用極小勞力, 即可讓牙齒長時間接㈣潰移_,且因謂時使用故對 溫血動物而言方便。 【發明内容】 概略而言,本發明係關於—種由牙齒表面移除污潰之組 合物,該、组合物中係#混—污潰移除劑、组合,其係、足以產 生改良之協乘性污潰移除效果或牙齒美白效果。本發明組 合物包括—種污潰移除劑的新穎组合,言亥组合比單獨使用· 個別污潰移除劑具有改良之冷潰移除效果,因此可降低各 成分之摻混有效量。此外’本發明組合物與包括口香糖及’ 糖果等固體口服調配物具有相容性,同時可維持滿意的感、 官及口味性質。 於本發明之一特殊方面,提供一種由牙齒表面移除污潰 之組合物,包含污潰移除有效量之至少兩種選自過氧化2 、多磷酸鹽及陰離子界面活性劑之活性成分。本發明組人 89100.doc 200417379 物典型也含有口服可接受之載劑。 本發明之另一特定方面,提供一種由牙齒表面移除污潰 <方法’包含投予污潰移除有效量之本發明組合物至溫血動 物(包括人類)口腔,用於清潔及美白與其接觸的牙齒表面。 本各明之較佳具體實施例中,較佳過氧化物係選自過氧 化脲、過氧化氫、過氧化鈣及其混合物組成的群組;較佳 夕%鉍鹽係選自由三多磷酸鹽、四多磷酸鹽、焦磷酸鹽、 偏磷酸鹽及其混合物組成的群組;以及該較佳陰離子界 面活性劑係選自由中鏈及長鏈脂肪酸酯及鹽、有機酸之一 =甘油醋及二酸甘油酯、檸檬酸之一酸甘油§旨及二酸甘油 酯、礼酸<一酸甘油酯及二酸甘油酯、棕櫚酸鈉、硬脂酸 納、及其混合物組成的群組。 【實施方式】 本發明係針對具有污潰移除性質之組合物用以於使用該 組合物處理之牙齒表面產生美白效果。此種組合物特別適 合用於黏著於或捕捉於牙齒表面之物質内部的污潰,以及 週合用㈣特潰捕捉„以及污潰於牙齒表面的累積。 本1月、’且。包括下述產品,該產品並非意圖供呑服來產生 治療劑的系統性吸收’反而該產品將停留在口腔中-段夠 長時間來接觸牙齒表面以提供有利效果。本發明組合物可 =選自下列之形式:例如潔牙產品包括漱口水、牙膏、牙 粉二牙霜:牙線、液劑、凝膠劑等;。香糖包括含懿口香 等乂及糖果包括薄何糖、口含錠等。較佳具體實施例中 ’本發明組合物係呈口香糖調配物及糖果調配物形式。 89100.doc 200417379 根據本發明,污潰移除有效量之污潰移除劑包括至少兩 種選自過氧化物、多磷酸鹽及陰離子界面活性劑之活性成 分的新穎组合,用於本發明組合物來提供有效污潰移除活 性。申請人發現污潰移除劑的新穎組合比單獨個別成分,,亏 潰移除劑之活性,可顯著改良污潰移除活性。此外,申請 人也發現污潰料劑之新穎組合可降低個別污潰移除劑於 組合物之用量。如此’包括硬脂酸鈉之陰離子界面活性劑 用量可有效賴,來避免先前技術口香糖組合物之相關; 題,包括不宜人的口感、口香糖基劑過早分解、肥包口味 等:申請人進一步發現此種新穎組合可有效減少多磷酸鹽 用量’同時仍然維持強勁污潰移除活性,因而消除或顯著減 少典型關聯含較高量多⑽鹽之組合物之不宜人口味(亦 即鹹味、苦味、金屬味)。 ' 污潰移除有效量」-詞㈣此處表示此處揭示之污這 移除劑之组合用量,該量足以預防、消除或至少減少^ 動物(包括人類)《牙齒表面的冷潰存在,但該用量有夠低而 可防止任何非期望的副作用。本發明之$潰移除劑組合之 ^移除有效量可依據特定料之類型及程度、接受處理 溫血動物(包括人類)的年齡以及健康情況、處理持續時間、 同時接受治療的本f、採用之料移除劑之料形式(亦即 鹽)、以及,了潰移除劑施用之特定載劑形式而改變。 本發明組合物之;:亏、、杳# ^…& 、 /、夕除^〉辰度係依據用於施用污潰移 除劑之牙齒表面之組合物類 、 、口含錠、口香糖、轉果等二牙賞、“水及清洗液 搪果會)決疋,原因在於接觸牙齒之組 89100.doc -10- 200417379 口物之功效有差別’另一原因在於通常使用有效量之組合 物。濃度也係依據存在之污潰程度決定。 除了丽又說明之外,摻混於根據本發明之組合物之各項 成分含量係以組合物總重之重量百分比表示。 根據本孓明’適當過氧化物包括任一種含〇_〇鍵之化合物 居〇〇鍵可刀解而供給至少一種活性物種。較佳過氧化物 例如包括無機過氧化物如過氧化氫、過氧化鈉、過氧化舞 、過氧化總、過氧化鋅、或過氧化鎂;以及有機過氧化物 包括(但非限制性)過氧化脲。摻混本組合物之過氧化物用量 將依據採用之特定個別Μ移除劑或污潰移除劑的組合、 以爾物之其它成分類別及其個別用量決定。本發明之 過氧化❹、以污潰移除有效量存在,以組合物總重為基準 ’存在量為約〇.〇1%至1〇%,較佳約0.1%至5%及更佳由〇·2% 至3 %重量比。 =發明之-具體實施例中,過氧化物可經包膠來防止過 、:解’以及控制活性物種由本發明組合物之釋放速率。 過氧化物例如經由微囊肖狀 w …文暴匕膠而獲得過氧化物的小珠粒之嵌 置或包膠方法通常為業界已知。# + 、、 、匕虱化物可被包膠於包膠 物貝’孩包膠物質包括(但非限 咅 制生)艮用天然或合成塑膠如 耔、占1 化生油、挪子油、棕櫚油或紅花 籽油,4合物如明膠、澱粉、 戎 馱胺類、聚胺基甲酸酯辨 ;壞如石犧;礦油或其它食用惰 過氧化物直到釋放為止,w,、了包覆且保存 /、釋放例如係經由牙齒間的機械 89100.doc 200417379 動作(例如吸嚼),或經由酵素作用,特別係經由過氧化物也 口月空中 > 玉、、、 > '、 液或水父互作用而產生初生態氧。包膠活性成 ^括彳政我包膠方法之進一步細節可參考美國專利第 4,867,9〇2、5,4〇3,578、5,976,5〇7及 6,258,343 號,各案内容 以引用方式併入此處。 根據本發明,適當多磷酸鹽包括任一種有兩個或兩個以 上磷酸基之化合物,磷酸基主要係排列成線性組態,但也 可旎存在有若干環狀衍生物。較佳具體實施例中,多磷酸 鹽有四個或四個以上的磷酸基。較佳多磷酸鹽例如為無機 夕鉢I鹽包括三多磷酸鹽例如其全部或部分中和之水溶性 鹼至屬鹽包括鈉、4甲或銨三多磷酸鹽;四多磷酸鹽;六多 %I鹽例如六多磷酸鈉;焦磷酸鹽如焦磷酸四鈉及酸性焦 磷酸鈉;及其混合物。最佳多磷酸鹽之分子相當小,例如 為三多磷酸鈉,其典型之溶解度較高,且對牙菌斑或生物 膜有較鬲滲透性來產生較高牙齒美白效果。 多磷鉍鹽於本組合物之摻混量將依據使用之特定個別污 潰移除劑或污潰移除劑的組合以及組合物其它成分之類別 及其個別用量而改變。多磷酸鹽係以污潰移除有效量存在 於本組合物,其含量以組合物總重為基準為約至〇 〇1%5 〇% 重里比夕$故鹽之較佳污潰移除有效量為約〇 · 1 %至3 . 〇 % 重量比,及最佳有效量係於約丨.0%至3〇%重量比之範圍。 根據本發明,用於本發明之適當陰離子界面活性劑包括 硫酸化油酸丁酯、中鏈及長鏈脂肪酸酯及鹽,特別硬脂酸 及棕櫚酸鈉鹽及鉀鹽及其混合物,及其甲酯及乙酯,油酸 -12- 89100.doc 200417379 納反丁知* 一臥鹽、葛維迷酸钾(p〇tassiunl glomate);有機 fe之一酸甘油酯及二酸甘油酯例如檸檬酸硬脂基一酸甘油 酷、丁二驗硬脂精、磺基丁二酸二辛酯鈉、三硬脂酸甘油 醋、卵磷脂、羥基化卵磷脂、硫酸月桂酯鈉、乙醯化一酸 甘油酯、丁二醯化一酸甘油酯、檸檬酸一酸甘油酯、乙氧 化一酸甘油酯及二酸甘油酯、聚山梨糖醇一酸甘油酯、硬 脂基-2-乳酸鈣、硬脂基乳酸鈉、甘油及丙二醇之乳酸化脂 肪·酸醋;c8-c:24脂肪酸之甘油-乳酸酯且較佳為c14_C2G脂肪 酸之甘油·乳酸酯;Cs-C24脂肪酸之多甘油酯,且較佳為 Cm-Cm脂肪酸之多甘油酯;丙二醇藻蛋白酸酯;蔗糖c8_C24 脂肪酸酯且較佳為蔗糖Cm-Cm脂肪酸酯;二乙醯基酒石酸 之一酸及二酸甘油酯、或檸檬酸之一酸及二酸甘油酯、酸 醋精等及其混合物。 本發明之較佳形式中’陰離子界面活性劑係選自硬脂酸 鈉、及棕櫚酸鈉及其混合物、油酸鈉、油酸或乳酸之一酸 甘油酯及二酸甘油酯之混合物例如硬脂酸乳酸甘油酯、硬 脂酸甘油酯及乳酸甘油酯及其混合物、蔗糖一硬脂酸醋、 蔗糖二硬脂酸酯、蔗糖一月桂酸酯、蔗糖二月桂酸酯、一 硬脂酸多甘油酯、一月桂酸多甘油酯及其混合物。 用於本發明組合物之較佳陰離子界面活性劑例如為硬脂 酸鈉,通常可以與棕櫚酸鈉約50/50之混合物獲得,以及至 少一種檸檬酸一酸甘油酯及二酸甘油酯之混合物。後述類 別之市售污潰移除劑之適當範例為IMWIT0R 370®,得自康 迪維塔(Condea Vista)公司。也較佳為選自乳酸一酸甘油醋 -13- 89100.doc 200417379 及二酸甘油酯及其混合物之界面活性劑。 摻混於本發明組合物之陰離子界面活性劑數量將依據採 用之特定個別污潰移除劑或污潰移除劑的組合、以及組合 物其它成分之類別及個別數量而改變。例如,較佳污潰移 除有效量之硬脂酸鈉為約〇·5%重量比,較佳乳酸一酸甘油 酉旨及二甘油g旨混合物用量為約〇 · 6 %重量比,而較佳檸檬 酸一酸甘油酯及二酸甘油酯混合物(例如;[MWITOR 370@)之 用量為約0.6%至1·〇%重量比。 口香糖組合物之陰離子界面活性劑用量,以口香糖組合 物總重為基準典型為約O p/QSiO%重量比。陰離子界面活 性劑之較佳量為約0·4%至約1·2%重量比。陰離子界面活性 劑用量將依據特定載劑以及本發明使用之個別污潰移除劑 或污潰移除劑組合而改變。 邵分用於本發明之糖果組合物之較佳界面活性劑為硬脂 酸納、棕櫚酸缺其混合物。如前文指示,硬脂酸納通常 可呈與棕櫚酸鈉約略平分之混合物存在。 用於本發明之糖果組合物之陰離子界面活性劑數量可於 寬廣範圍改變’其用量例如係依據組合物類別以及採用特 定個別污潰移除劑或污潰移除劑的組合而改變。通常本發 明之糖果組合物中之污潰移除劑用量係超過對該特定污潰 移除劑而言,用於口香糖組合物之用量。 活性劑之存在量係 陰離子界面活性劑 典型地,糖果組合物用之陰離子界面 占組合物總重之約01%至20%重量比。 <較佳用量為約3%至15%重量比。 89100.doc -14- 200417379 典型地其ΈΓ組合物(包括潔齒劑)之陰離子界面活性劑之 存在量係占組合物總重之約〇〇1%至約2〇%重量比。陰離子 界面活性劑之較佳含量為約3%至15%重量比。 本發明之較佳具體實施例中,組合物包含冷潰移除有效 量之三多磷酸鈉、硬脂酸鈉以及選擇性之過氧化脲之組合 以及一種口服可接受之載劑。 本發明組合物進-步包含口服可接受之載劑,其數量適 。配合凋配物 < 其它各成分含量。「口服可接受載劑」一詞 表不一種可混合活性成分供輸送至口腔用於牙齒美白及清 潔目的之媒劑,該媒劑不會對溫血動物(包括人類)造成傷害 。口服可接受載劑進-步包括組合物之下列成分,該等成 分可彼此交混但不會交互作用,結果實質上造成根據本發 組合物及万法於溫血動物(包括人類)口腔之組合物安 疋性降低及/或牙齒污潰移除功效降低。 、本組合物之口服可接受之載劑包括-或多種相容性固體 或硬體填料稀釋劑或包膠物質,該等物質適合供口服投藥 、、1本發明之載劑或賦形劑可呈任-種適當輸送劑型,例如 2夜训、、恥體分散液劑、乳液劑、懸浮液劑、洗劑、凝膠 末J政劑、固體等;也包括牙膏(包括凝膠)、漱口 習清洗劑、口腔噴霧劑、口香糖、口含錠及糖果之 選發明組合物之載劑為業界眾所 定。 、长據口味、成本、儲存壽命等二次考量決 了含括於本發 明組合物之添加劑或成分類型包括例如磨 89100.doc -15- 料、鼠1陰離子釋放化合私7 , w. ^ 口物、增稠劑、濕潤劑、矯味劑及甜 未《]抗牙、‘石劑、鹼金屬碳酸氫鹽、界面活性劑、去礦 物質劑以及多種其它添加劑例如抗炎劑等。適當去礦物質 劑包括例如物弓鹽如嶙酸三約、磷酸令水合物、 無水磷酸二約、磷酸水合物、魏八約或顿四妈 ,以及甘油基磷酸躬及其混合物。 、、本發明之潔齒劑組合物可進一步包括漱口水、口腔清洗 夜及L貧務痴卜此等漱口水清洗液及口腔噴霧劑之成分 典型包括:水其存在量為約45%至95%,以及—或多種乙醇 其存在量高達約7G% ’濕潤劑其存在量高達約·,界面活 性劑之存在量為約Q.G1M7%,矯味劑之存在量為約〇屬 = 2%,甜味劑之存在量為約〇1%至3%,以及著色劑之存在 量為約G.GG1%至〇.5%。此等漱口水清洗液及卩腔噴霧劑也 包括-或多種抗銷齒劑其含量為約G G5%J_ G 3% (例如氣陰 離子釋放化合物)以及抗牙結石劑其含量約〇. 至3%。 其它本發明之潔齒劑組合物包括齒用溶液劑。料齒用 溶液劑之成分通常包括:水其含量為約9〇%至99%,以及一 或多種保藏劑其含量由約〇.〇1%至〇 5%,增稠劑其含量至多 約5 /°以及墙味劑其含量由約〇· 1 %至3%。 本發明之其它潔齒組合物可呈牙膏、牙凝膠以及牙粉形 式二此等牙膏及牙凝膠成分通常包括-或多種齒用磨^ /、έ里通系為約1 〇%至50%,界面活性劑其含量為约〇 二 10%,增稠劑其含量為約〇· 1%至5%,濕潤劑其含量為约。 至55% ’矯味劑其含量為約〇·〇4%至2%,甜味劑其含量由約 89100.doc -16- 200417379 0.1%至3% ’著色劍並本旦山 有巴刹。里由約0 01%至〇 5%,及水其含量 由約2%至45% 〇此等牙春弋年冰t c守才θ或牙齒凝膠也包括一或多種抗齲 齒劑其含量為約〇·〇5。/。至〇 w L ^ 芝0.3 /〇 (例如氟陰離子釋放化合物) :以及抗牙結石劑其含量為約01%至13%。此等組合物之 液及□ ^比例混合而形成乳膏狀或膠凝物質,可由加 壓容器或由可塌陷管擠壓。當然牙粉實質上皆含非液體成 分。 取佳本發明組合物為口香糖及糖果。口香糖組合物典型 包括-或多種樹膠基劑、墙味劑以及甜味劑。「糖果」一詞 用万、此處。括但非限於:牛乾糖、糖果、薄餅、凝膠西點 、半軟糖、菱形錠、硬糖、薄荷糖、喉片、錠劑、微囊以 及快速溶解之固體形式包括滚乾形式(糕餅、威化餅、薄膜 及U )以及快速落解之固體形#包括S縮錠齊卜「快速溶 解之口 to形式」一詞用於此處表示該固體劑型於口腔内可 方、V方、勺60^ ’較佳少於約15秒及更佳少於約5秒溶解。菱 形釭括菱形固體包含治療劑於經過矯味之基劑。基劑可 為硬糖、甘油化明膠或糖與足夠黏質的組合來讓糖成形。 菱形錠組合物(壓縮錠類型)典型包括一或多種填料(可壓縮 糖)、矯味劑及潤滑劑。 申請人發現有效污潰移除用口香糖及糖果組合物可經由 下:^方弋I備,經由適當選擇本發明之污潰移除劑與口香 糖及糖果組合物調配物之組合;以及選擇污潰移除劑組合 从、力凌I、’且合物之方式,該組合物讓該污潰移除劑組合 可以有A量釋放,目此該組合可接觸牙齒表面,包括牙齒 89100.doc -17- 200417379 表面且同時維持或改善此等產品一般關聯之感官性質。 本發明之口香糖組合物可經包衣或未經包衣,且可^拉 塊、棒、丸粒、珠粒等形式。不同形式之口香糖組合 組成類似,但其組成也可就各成分之比例而炙 包衣之口香糖組合物含較低百分比之軟化劑。丸粒及珠2 有個小口香糖芯,然後該芯包覆糖溶液或無糖溶液而形^ 硬殼。厚塊及棒通常調配成質地比口香糖芯更軟。但用於-本發明之目的,為了克服界面活性劑對口香糖基劑可能=. 成的不利軟化影響,較佳將厚塊或棒狀口香糖調配成鲁 較堅實的質地(換言之,使用比典型用量更少的軟化劑)。 中間含餡之口香糖屬於另一種常見的口香糖形式。塑膠 部分具有前文說明之類似組成及製造模式。但餡典型為水 溶液或凝膠,餡係於加工過程中注入口香糖中心。污潰移 除劑之组合典型係於餡之製造過程或填充入口香糖期間= 混於鶴。 含餡之口香糖也可選擇性經過包衣,且可製備成多種形 式,例如製造成棒棒糖形式。用於實施本發明,較佳使用 _ 經包衣口香糖,其中污潰移除劑組合係於餡以及包衣中之 土 ^ 一者。最佳用於移除污潰者為包衣口香糖,其中該污 潰移除劑組合至少置於包衣内。 本發明之口香糖組合物包括口香糖基劑,以及大部分其 匕典型之口香糖組合物成分,例如甜味劑、軟化劑、矯味 別等。本發明採用之污潰移除劑之組合包括至少兩種污潰 移除成分之混合物,該成分係選自過氧化物、多磷酸鹽及 89100.doc -18- 陰離子界面活性劑。口香糖組合物也含有較少量軟化劑如 P外月曰或甘油’或可免除使用軟化劑。此外口香糖組合物
可。有比自知口香糖组合物更大量之糖醇’來輔助本發明 使用之污潰移除劑组合輸送至牙齒表面。 A 根據本毛月之口香糖組合物之一方面,污潰移除劑係於 口香糖組合物製造過程中添加,換言之,與甜味劑、墙味 ,等-起添加。於本發明之另一方面,污潰移除劑料為· 最末步驟之一添加’較佳為製造口香糖組合物之最末步驟。· 申請人判定此種修改方法將污潰移除劑組合摻混於口香糖鲁 組合物,而無需將污潰移除劑實質連結於其中,污潰移除 劑實質連、结之情況例b出現於污潰移除劑與口香糖基劑直 接混合時,如此污潰移除劑只鬆鬆地容納於口香糖組合物 内,於典型之哑嚼過程中更容易由口香糖組合物釋放。如 此大部分污潰移除劑且不含口香糖基劑。 於本發明之又一方面,口香糖基劑通常包含彈性體、彈 性體增塑劑、蟻類、脂類、油類、乳化劑、填充劑、質地 化劑,以及包括後文說明之污潰移除劑之期望組合。 鲁 彈性體係占基劑之約5%至95%重量比,較佳10%至70%重 量比,及最佳15%至45%重量比。彈性體例如包括合成彈性 體如聚異丁烯、聚丁烯、異丁烯-異戊間二烯共聚物、苯乙 ~ - 丁一缔共聚物、聚乙酸乙錦τ g旨等。彈性體也包括天然彈 性體如天然橡膠,及天然樹膠,例如傑陸頓膠(jelut〇ng)、 雷奇卡皮膠(lechi caspi)、裴里歐膠(periU〇)、瑪莎蘭杜巴橡 膠(massaranduba balata)、糖膠樹膠、馬來樹膠或其混合物 89100.doc -19· 200417379 。其它彈性體為業界人士眾所周知。 彈性體增塑劑當用於口香糖基劑時可修改口香糖成品的 韌度。彈性體增塑劑之典型存在量至多占口香糖基劑之約 75 /〇重里比,較佳約5%至45%重量比及更佳約至π%重 1比彈性心增塑劑包括天然松香g旨類例如部分氫化松香 艾甘油酯、托耳油松香甘油酯、部分氫化松香之季戊四醇 酉曰权9之甲^及邵分氲化卸S旨等。合成彈性體增塑劑如 萜烯樹脂也可用於口香糖基劑組合物。 壤類包括合成蠟及天然蠟,如聚乙烯、蜂蠟、巴西標搁 蠟等。石油蠟類如石蠟油可使用。蠟類之存在量占口香糖、 基劑至多約30%重量比。蠟類可辅助成品口香糖的硬化,以 及辅助改善口味的釋放,且可延長產品之儲存壽命。 填料可修改口香糖基劑之質地,且填料可輔助加工。填 料例如包括珍故鍰及夕酸|g、黏土、銘氧、滑石、氧化鈥、 纖維素聚合物等。填料典型之存在量為1%至6〇%重量比。 用於口香糖基劑之軟化劑例如包括氫化植物油及部分氫 化植物油、可可脂、一硬脂酸甘油酯、三乙酸甘油酯、二 酸甘油酯及三酸甘油酯、脂肪酸如硬脂酸、棕櫚酸、油酸 、亞油酸、亞麻酸等。 口香糖基劑係占口香糖組合物之約5 %至9 5 %重量比,更 典型為10%至50%重量比,最典型為約25%至35%重量比。 以較高含量之口香糖基劑為佳。 其它用於口香糖組合物之成分包括甜味劑,包括天然及 人工甜味劑以及包括糖及無糖。甜味劑典型於口香糖組合 -20- 89 l〇〇.d〇c 200417379 左炙存在量為約2〇%至80%重量比且較佳约3〇%至6〇%重量 比。無糖甜味齋!包括(但非限制性)糖醇類如山梨糖醇、甘露 糖醇、木糖醇、氫化殿粉水解產物、麥芽糖醇等。高強度 甜味劑如蘇卡洛斯(sueralGse)、阿斯巴钳、新甜 至乙瓴萄甜(acesulfame)鹽等典型之存在量至多為约丨〇%重 ^ P禾劑可於寬廣範圍改 ^ 一 Μ个削心選擇用量為 ^•州重量^且較佳約請至⑽重量^口香糖組合 、:ϋ:矯味劑為業界眾所周知,且包括檸檬油、薄荷油 歐薄荷油、冬綠油、薄荷腦等。 可存在有軟化劑來修改口香糖組合物之質地。不似血刑 ::糖组合物:本發明組合物之軟化劑之典型係以較小量 予兑占口香糖組合物總重之约0.5%至10%重量比。 劑2了存在t本發明之口香糖組合物之物質包括抗氧化 4丁基化⑬基茴香酸、丁基化幾基甲苯、3_胡蘿萄素 、生頁酚)、著色劑、矯味劑等。 、 =包衣施料口香糖組合物之包衣技術例如盤式包衣或 搶Γ"衣為業界眾所周知。較料實施本發明係使用適合 」更搪層〈落液包衣。糖及糖醇二者可連同高純度甜味 =考色劑、、橋味劑、黏結劑以及其它習知添加劑用於此 :的。當污潰移除劑組合係提供於口香糖組合物之包衣 時,污潰移除劑溶液較佳另外施用矮味劑。 甜味劑之存在量係、占包衣糖浆劑之約30%至8〇%重量比 。黏結劑如硬脂酸鎂可以占包衣糖漿之約1%至15%重量比 89100.doc -21 - 200417379 添加至包衣糖漿劑俾提升或促進黏著。選擇性地也 人有小f習知添加劑。適合用於包衣糖漿之甜味劑包 s非糖甜味劑例如多趟基醇類如木糖醇、山梨糖酵、甘霖 t及其混合物;以及麥芽糖醇、異麥芽糖醇'氫化殿: 水解產物及氫化葡萄糖糖漿。也可含括單醋、雙醋及多缺 Μ列如也可使用薦糖、果糖、葡萄糖、半乳糖、及麥㈣ 作為甜味劑。其它適合用於包衣糖漿之甜味劑包括但非限 於自由態沙卡林酸、水溶性沙卡林鹽、塞克拉美鹽 (cyclamate salts)、帕拉提尼(响制私氫查耳酮類、甘^ 素、L-天冬醯基_L_苯基丙胺酸甲酯、以胺基酸為主之甜味 J丨合林(tahn)、史帝維苷(steviosides)、二氫查耳酮化合 物、乙硫菊甜鹽及其混合物。 其它可以小量添加至包衣糖漿之成分,包括水分吸收化 合物、抗黏附化合物、分散劑以及膜生成劑。適合用於包 衣糖漿劑之水分吸收化合物包括甘露糖醇或磷酸二鈣。有 用 < 抗黏附化合物(其也可用作為填料)例如包括滑石、三矽 酉父鎂及碳酸鈣。此等成分之用量係占糖漿劑之約〇.5%至5% 重量比。可用於包衣糖漿劑之分散劑例如包括二氧化鈦、 ;月石及其它别述抗黏附化合物。 包衣糖漿通常經加熱,部分糖漿沉積於芯上。通常單次 沉積包衣糖漿不足以提供需要之包衣量或包衣厚度,通常 需要施用第二、第三或更多次包衣糖漿,俾累積包衣量及 包衣厚度至預定之層數,且允許在各次包衣間乾燥。 本發明之口香糖組合物之較佳方面包含添加污潰移除劑 -22- 89100.doc 200417379 至包衣。污潰移除劑較佳係於糖漿包衣之後施用。較佳於 使用含污潰移除劑部分包衣之後,施用高強度甜味劑包衣 。含污潰移除劑之包衣較佳係於矯味劑溶液膠體施用。於 本發明之實施例,含污潰移除劑之包衣可呈溶液施用,或 可王乾進料施用,或於適當時經熔化後施用。對脂肪酸鹽 而口 以典水進料為佳。當包覆口香糖組合物時,包衣糖 漿之施用持續至平均口香糖重量達到要求的包衣重量為止 ’較佳連續施用至包衣係占終口香糖丸粒之約20%至30%重 量比為止。有關口香糖組合物製備之進一步細節可參考史 庫司完全糕餅製作人(第13版)(1957年)包括第41_7;1、 133-144及255_262頁;以及糖糕餅之製造(第2版)(1995年) ,Ε· B· Jackson,編輯,第258-286頁,其内容以引用方式 併入此處。 本發明也涵蓋含有經過適當選擇之污潰移除劑组合之糖 果組合物。糖果組合物包含壓縮錠如薄荷糖、硬糖、牛軋 糖、凝膠糖、含餡糖、半軟糖、薄餅以及其它屬於一般所 接受之糖果組合物定義之組合物。 呈壓縮錠形式之糖果組合物例如薄荷糖一般之製法係將 精細過篩之糖或代糖、矯味劑(例如薄荷口味)、增量劑(如 阿拉伯膠)以及選擇性之著色劑組合而製備。墙味劑與增量 劑組合,然後若有所需緩慢加熱糖或代糖連同著色劑。 然後產品通過預定!|目大小(例如12號篩 >之篩㈣,^ 典型於55。(:至6(^乾燥。所得粉末饋至填裝有大尺寸衝司 之打錠機’結果所得丸粒打碎成為粒劑然後再壓縮。> -23· 891〇〇-d〇c 200417379 硬糖典型含有糖或代糖、葡 、_ w甸糖水、矯味劑及選擇性 …劑。糖溶解於水中然後加入葡萄糖。將混合物調整 ^弗騰。纟中預先已經加人著色劑之液體倒人抹油之厚板 内及冷部。然後添加緯味劑且混練成為冷卻後之物質。所 得混合物饋至業界已知之掉犧總成來 形狀。 牛軋糖組合物典型包括兩種主要成分,以及硬糖及冰滚 =料。舉例言之,卵白蛋白或白蛋白之替代品與水組合且 攪動而稍微起泡。糖及葡萄糖加至水中,典型於約⑽。C至 1赋滞騰,所得滞騰產品倒人混合機内,且搗打至變成乳 酷狀為止。搗打後之白蛋白及墙味劑組合乳酷狀產物,隨 後徹底混合該組合。 有關糖果組合物製備之進一步細節可參考史庫司完全糕 餅製作人⑷3版⑽57年)包括第仏η、⑴」44及255况 頁;以及糖糕餅之製造(第2版)(1995年),£』;心随,編 輯’第 129·168、169_188、189_216、218_234及236_258 頁, 其内容以引用方式併入此處。 本發明之另-具體實施例中,提供—種經由對口腔投予 、施用或接觸污潰移除有效量之本發明組合物包括口香糖 組合物及糖果组合物,而於溫血動物包括人類口腔牙齒表 面移除污潰之方法。本發明之污潰移除有效量之組合物較 佳係以-或多種習知方式投予、施用或接觸牙齒表面用於處 理或防止牙齒表面之污潰。例如屮鲁主 A吳1 j如才齒表面可以含本發明缸 合物之溶液(例如漱口水、清洗液)清洗。若使用潔齒劑(例 89100.doc -24- 200417379 如牙膏、牙齒凝膠或牙⑹,則牙齒可經由刷牙等而泡在刷 牙產生的液體及/或泡宋中經歷足夠時間,較佳為㈣秒至 10分鐘’且更佳為約30秒至6〇秒。本發明方法進一步於本 組合物接觸牙齒表面後吐出大部分組合物。 2合物施用或接觸牙齒表面之頻次,較佳為約每⑴次至 約每日4次,更佳由約每週3次至每日3次,甚至更佳每日至 少认。此種處理時間典型由m一輩子。用於特定污潰, 污潰移除處理之處理時間係依據欲處理的污潰嚴重程度、 採用之特定輸送形式、以及溫血動物對處理的反應決定。 其它非限制性實施例包純予、施用或接觸本發明組合 物之牙齒’包括以漱口水或清洗液清洗牙冑,以及以潔齒 劑刷洗牙齒。其它施用本組合物至牙齒表面之方法為業界 人士顯然易見。較佳施用口香糖組合物及糖果組合物之方 G括且爵g本發明組合物之口香糖,p且脅或吸吹吸氣錠 或口含錠或其它糖果。 雨又討論揭示本發明且僅供舉例說明本發明之具體實施 例。為續技勢人士由此等討論了解可未悖離如下申請專利 範圍界走之本發明之精髓及範圍而由隨附之申請專利範圍 做出多種變化、修改及改變。 實施例1 除研究之實驗結果 材料及方法 -r備/¾動系統來處理羥基磷灰石(HAp)圓盤之玷染。茶、 咖啡及豬胃黏蛋白溶液混合而獲得玷染湯汁。玷染湯汁於 89100.doc -25- 200417379 3 7°C以每分鐘15毫升之速率循環通過流系統而接觸HAP圓 盤經歷約96小時時間。結果所得玷染之HAP圓盤於pH約7之 人工唾液溶液内清洗,讓其於室溫乾燥約2小時。 一旦HAP圓盤乾燥後,經由使用美諾達(Minolta)分光計 測量其漫反射吸光值,而測定各個HAP圓盤之基準線污潰 讀值。測量係根據國際色彩研究室委員會(CIELAB)色階與 整個可見光之色譜進行測量。CIELAB之色階將色彩根據3 個參數定量:淺-深階(L)、紅-綠色度(RGC)、以及黃-藍色 度(YBC) 〇對各個HAP圓盤求出3個吸光測量值之平均。然 後將HAP圓盤平分為7組,每組有5個HAP圓盤。 準備7種試驗溶液,各試驗溶液含有選自下列之溶液: 0.05%硬脂酸鈉(SS) ; 0.05%六偏磷酸鈉(SHMP) ; 0.05%三多 磷酸鈉(STPP) ; 0.05%焦磷酸四鈉(TSPP) ; 0.05%硬脂酸鈉 (SS)及0.05%六偏磷酸鈉(SHMP) ; 0.05%硬脂酸鈉(SS)及 0.05%三多磷酸鈉(STPP);以及0.05%硬脂酸鈉(SS)及0.05% 焦磷酸四鈉(TSPP)。 結果 各組經過玷染之ΗAP圓盤使用對應試驗溶液處理來比較 檢驗其污潰移除能力。本實驗未使用對照試驗溶液。ΗΑΡ 圓盤置於流系統,於37°C以每分鐘15毫升之流速使用對應 試驗溶液處理約1小時。處理後之ΗAP圓盤於室溫風乾2小 時。對各處理後之Η ΑΡ圓盤測量其玷染色彩之變化。玷染 程度之整體變化(ΔΕ)係對各個經處理之ΗΑΡ圓盤測定。各 試驗溶液之ΑΕ值顯示於下表1,較大值指示圓盤之污潰較少 -26- 89100.doc 200417379 而美白較大。 表1 對應各試馬会溶液之污潰移除結果 試驗溶液 △ E值 硬脂酸鈉(0.05%) 5.7 六偏鱗酸納(〇 · 〇 5 %) 4.3 三多磷酸鈉(0.05%) 6.8 焦磷酸四鈉(0.05%) 3.7 硬脂酸鈉(〇·05%)/六偏磷酸鈉(0.05%) 9.2 硬脂酸鈉(〇.〇5%)/三多磷酸鈉(0.05%) 10.8 硬脂酸鈉(〇·〇5%)/焦磷酸四鈉(0.05%) 8.0 表1以ΔΕ值指示的結果證實全部試驗溶液之污潰移除功 效。 實施例2 試管試驗污清移除研穿 材料及方法 準備數個經基轉灰石圓盤,經前處理而於圓盤表面上形 成生物膜,生物膜以植物性污潰著色。然後使用比色計 (Chrom-A-Meter)測定各圓盤之色彩強度。圓盤懸吊於水中 或試驗溶液中,試驗溶液含有一種選自下列之溶液:1) 0.05%硬脂酸鈉;2) 0.3%三多磷酸鈉;3) 0.3%過氧化脲; 4) 0.3%過氧化脲及0.05%硬脂酸鈉;及5) 0.3%過氧化脲及 0.3%三多磷酸鈉。水用作為對照來考慮圓盤組合物之差異 以及各批次間之污潰厚度變化。圓盤共處理兩次,間隔1 〇 -27- 89100.doc 200417379 分鐘,於各次處理間隔之後藉比色計測定其特徵。色彩變 化係以ΔΕ值相對於單獨水處理表示。然後求出污潰減少百 分比。結果示於圖1。 如圖1所7F,過氧化脲與硬脂酸鈉之組合以及過氧化脲與 三多磷酸鈉之組合比單獨使用個別污潰移除成分可提升污 潰移除效果。 注A·溶液之掣備 站染溶液係由加啡(例如Ch〇ck FuU 〇,Nuts AH Method Grmd)、茶(例如立頓茶包)、藍梅派餡以及葡萄汁(例如威 爾屈(Welch’s)葡萄汁)各成分混合組成。5〇〇毫升咖啡(於咖 啡機内使用3-1/2匙咖啡加至7〇〇毫升水製備而得)置於4升 錐形开瓦内及攪掉。5〇毫升藍梅派鶴經過液化,且添加至該4 升錐Φ瓶内,攪拌内容物。5〇〇毫升茶(係經由於8〇〇毫升燒 杯内將4包立頓茶包泡在6〇〇毫升預先沸騰水約5分鐘而製 備)添加至該4升錐形瓶。然後將50毫升葡萄汁加至瓶内, 内容物經攪拌而形成玷染溶液。 歹工基%灰石圓盤以底部向上置於玻皿 維持於略微潮濕狀態。料染溶液向下倒至玻璃 pirn®盤表面’直到圓盤被至少則站染溶液所 =盖為止。將玻璃皿加蓋,讓圓盤衫溫浸泡隔夜。燒杯 内填裝饥水,各燒杯由站染溶液移出後浸泡於水中,置 二:有吸收精之玻璃耻,且站染側向上。讓圓盤 燥隔夜。 89100.doc -28- 200417379 丝玷乘崖的虛理 ^ ^,谷硬個別連同對應量之活性成分於37°C於400克蒸 館水製備至達成前述濃度。試驗溶液於約連續攪拌 、° =對照組係由37°C彻克蒸餘水組成,也於約4G0 rpm 連貝饶拌。各個被玷染的圓盤使用比色計檢查而決定其 然後以鎳子夾起圓盤’且懸吊於對應試驗溶液 ,欠(對…、、’且)中。各圓盤被維持於燒杯侧邊與於溶液液面下 万中途攪拌,旋渦間經歷約10分鐘時間。然後由溶液中移
出圓盤,讓其乾燥。以比色計檢查各圓盤來確定其cIELAB 值。對各圓盤重複前述處理程序共計20分鐘。 結果 圖1所TF結果指示含過氧化脲組合硬脂酸鈉及三多磷酸 鈉之試驗溶液,比單獨含個別成分之試驗溶液以及單獨使 用水處理,可顯著減少於試驗期後出現污潰。 實施例3 毯_管試驗污清移除研旁 材料及方法 五個經包衣之口香糖試樣於污潰移除試驗模式中試驗, 各試樣各自含有活性組合物選自1) 0.5%硬脂酸納於芯部; 2) 0.5%硬脂酸鈉於包衣部及3%過氧化脲於芯部;3) 〇 5% 硬脂酸鈉於包衣邵及1%三多磷酸鈉於芯部;4) Q 5%硬脂酸 鈉於包衣部及3%三多磷酸鈉/過氧化脲於芯部;以及5)〇 5% 硬脂酸納於包衣邵及1 %三多磷酸納/過氧化脲於芯部。夢口 香糖試樣利用哑嚼機器混練,哑嚼機裝配有受站染的牛齒 89100.doc •29- 於^且㈣來挺擬人口腔的上牙及下牙。試樣被哑脅5分 =。t齒裝配於吸°爵機之前,使用比色計檢查,而經過模 μ Γ—週時間(28劑)之後再度檢查。然後求出λε值決定 色:夂化。然後由牛齒試樣去除全部污潰,再度使用比色 計讀取讀值。求“潰減少百分比。結㈣於圖2。 試驗結果指示含過氧化脲組合硬脂酸鈉及三多磷酸鈉之 口香糖試樣經試驗期後獲得污潰的顯著減少。 實施例4 口香糖组合物 * 成分 組合物1 組合物2 組合物3 (% w/w) (% w/w) (% w/w) 口香糖基ϋ ' 26.25 26.25 26.25 奴酉艾 3.75 3.75 3.75 山梨糖醇 28.05 27.55 30.55 甘露糖醇 7.50 7.50 7.50 麥芽糖^ '~~~- 21.62 21.62 21.62 甘油 1.00 1.00 1.00 橋味劑 3.15 3.15 3.15 阿拉伯承 ~' 1.16 1.16 1.16 0,17 0.17 0.17 小燭樹^ '~~^ 0.03 0.03 0.03 硬脂酸鈉* 0.50 • •麵 麵麵 三多磷酸鈉 ~ 3.00 3.00 3.00 甜味劑 0.82 0.82 0.82 IMWITOR 370@ 雜-_ 1.00 1.00 Ϊ氧化脲 ~ 3.00 3.00 _ _ _ 總量 100.00 100.00 100.00 *硬脂酸鈉/棕櫚酸鈉@ 50/50 89100.doc -30- 200417379 表2所示口香糖組合物 係和業界已知又習知方法製備。口 香糖基劑經過加妖,右八ά 甘 . …、无刀乂軟化基劑,而未對基劑之物理及 化學性質造成不良的畢〈邀 ^ 、 〜9。丨谷融口香糖基劑及填料添加至 '々匕合32内。伴以〉昆合,力 撼含 糖%頒、甘油、矯味劑、高強 度甜味劑以及本發明污潰移除劑而獲得均質混合物,本發 明^潰移除㈣最後添加。然後混合物由混合物糊中排 出,經過滚軋以及藉習知技術切割成為預定塊狀大小。 實施例5 ϋϋ移除詖验 材料及方法 使用類似前文實施例2所述方法,但羥基磷灰石圓盤係以 牛齒替代,於污潰移除試驗模式共測試5種試驗溶液。牛齒 經準備且經前處理而形成生物膜於其上,該生物膜已經使 用植物性污潰變色。然後各牛齒之色彩強度利用比色計測 定。牛齒懸吊於水(對照組)或試驗溶液,試驗溶液係選自U 0.05%三多磷酸鈉/〇·ι%硬脂酸鈉;2) 〇1%三多鱗酸執 /0.05%硬脂酸鈉;3) 0.1%三多磷酸鈉/0 075%硬脂酸鋼;及 4) 0.1 %三多磷酸鈉/〇·ι %過氧化脲。以水處理作為對辟,對 照組考慮牙齒組成的差異以及各批次間之污潰厚度變化。 圓盤接受兩次10分鐘間隔的處理,於各次處理間隔後夢 比色計決定其特徵。色彩變化係以ΔΕ值相對於水處理之斜 照組而測定。然後由ΔΕ值求出污潰移除減少百分比。沾 、、·口 果 示於圖3。 結果 -31 - 89100.doc 200417379 如圖3所示,試驗溶液各自包含本發明冷潰移除劑之特定 組合’試驗溶液比較單獨以水處理具有顯著料移除效果。 實施例6 薄荷壓縮鍵劍組么物 表3 成分 組合物1(% W/W) 組合物2 (% w / w、 山梨糖醇 90.55 t»/ 1 々二、/U W / W I 南純度甜味劑 0.15 〇 1 S 矯味劑 -------- 1.300 L 17 ·丄 J 1 300 三多磷酸納 3.00 7 〇〇 硬脂酸鈉* 5.0 _____ J » V V 1 〇 〇 總量 100.00 __ 100.00 *硬脂酸鈉/棕櫚酸鈉@ 50/50 表3所示薄荷壓縮錠係以業界習知方法製備。甜味劑經過 精細過篩及組合。其它成分及污潰移除劑經組合且徐緩加 入甜味劑。然後所得混合物通過具有預定篩目大小之篩(例 如12號篩)過篩,然後典型於55。〇至6〇。(:乾燥。所得混合物 饋至裝配有大尺寸衝頭的打錠機,打錠所得丸粒被打碎成 為粒劑然後壓縮。 實施例7 炎用薄荷慝製錠進行臨庆研究 進行臨床研究來確定實施例6之薄荷錠組合物與未經處 理對照組之污潰移除活性。150人被分成三組,每組人。 兩組個別使用選自下列任一種試驗組合物:實施例6薄荷糖 89100.doc -32- 200417379 、.且口物1及實施例6薄荷糖組合物2。第3組未接受任何處理 j &组合物&用口服投予’冑組合#溶解於試驗者口中 每日4’入供、.工8週時間。個體於第4週以及於第8週使用經 :㈣指數(LGbene 評估牙齒站染情況。 飞賓心數為_科專業人員用來量測牙齒站染的視覺標度 。試驗者的牙齒分兩區,亦即分成體緣與牙料。二區以〇 土3的^度來評估站染強度(亦即黑度)以及站染程度(亦即 面積來測定各個試驗者的牙齒總分。經由比較牙齒總分 ’由牙齒總分導出成對比㈣潰減少P值,來測量隨著時間 之經過的污潰程度。研究結果示於表4。 表4 厂--_o=m 薄荷糖組合物1 -薄荷糖組合物2 對照(無處理) —---- ^ •’口 、丄‘口 I "---- <"Π Λ Λ 1 薄荷糖組合物1 —-—乂υ.υϋΐ _ _ _ —<0.001 、,,1或2之個砠所呈現 5㊉減少顯示顯著較少 荷組合物:及―之:=成的牙齒冷潰。測定 程…、人/染減少於統計上為顯著,顯 裎度相Wp切.05。薄荷糖 之冷潰減少間並無顯著差異。〜、薄何糖組合物2丨 【圖式簡單說明】 以下各圖舉例說明本發明之具體 本發明,本發明係由構 “思圖_ "4伤乏中請專利範園所肩 89W0.doc -33- 200417379 定 圖1為、.泉圖,顯不根據本發明,由羥基磷 泡於 武驗溶液中站染所得之冷漬減少百分比; . 圖2為線圖顯示根據本 結合於口香糖,由模擬二;、同玷染移除劑的組5 以及 野喊驗所得之冷潰減少百分比; 圖3為線圖,顯示根據本發明,、人、、 ,帶有污漬之牛齒所得:,於試驗溶液處理20分鐘後 、/7項減少百分比。 89100.doc '34.
Claims (1)
- 拾、申請專利範圍: L :種由牙齒表面移除污潰之組合物,包含污潰移除有效 里之至y兩種選自過氧化物化合物、多磷酸鹽、及陰離 予界面活性劑之活性成分,該組合物進一步包含一種口 服可接受之載劑。 2·如申請專利範圍第i項之组合物,其中該過氧化物化合物 係選自由過氧化脲、過氧化氫、過氧㈣、過氧化納、 過氧化锶、過氧化鋅、過氧化鎂及其混合物组成的群組。 3.如申請專利範圍第i項之組合物,其中該多鱗酸鹽係選自 由三多磷酸鹽類、四多磷酸鹽類、焦磷酸鹽類、六偏磷 酸鹽類及其混合物組成的群組。 4·如申請專利範圍第3項之組合物,其中該多磷酸鹽係選自 由水溶性鹼金屬多磷酸鹽類組成的群組。 如申印專利範圍第4項之組合物,其中該多磷酸鹽係選自 由二多磷酸鈉、三多磷酸鉀、鉀三多磷酸鈉、六偏磷酸 鈉、焦磷酸四鈉、酸性焦磷酸鈉及其混合物組成的群組。 6·如申請專利範圍第1項之組合物,其中該多磷酸鹽係以組 合物總重為基準,約0 01%至5%重量比之污潰移除有效 量存在。 7.如申請專利範圍第6項之組合物,其中該多磷酸鹽係以組 合物總重為基準,約〇.1%至3%重量比之污潰移除有效量 存在。 8 ·如申請專利範圍第7項之組合物,其中該多磷酸鹽係以組 合物總重為基準,约!·〇%至3%重量比之污潰移除有效量 89100.doc 存在。 9 ·如申請專利範圍第1項之組合物,其中該陰離子界面活性 劑係選自由硫酸化油酸丁酯、中鏈及長鏈脂肪酸酯類及 鹽類、硬脂酸及棕櫚酸之鈉鹽及鉀鹽及其甲酯及乙酯、 油酸鋼、反丁晞二酸鹽、葛羅迷酸鉀(p〇tassium gl〇mate) 、有機酸之一酸甘油酯及二酸甘油酯、檸檬酸硬脂基一 酉父甘油酯、丁二gf硬脂精、績基丁二酸二辛酯鈉、三硬 脂酸甘油酯、卵磷脂、羥基化卵磷脂、硫酸月桂酯鈉、 乙醯化一酸甘油酯、丁二醯化一酸甘油酯、檸檬酸一酸 甘油酯、乙氧化一酸甘油酯及二酸甘油酯、聚山梨糖醇 一紅甘油酯、硬脂基-2-乳酸鈣、硬脂基乳酸鈉、甘油及 丙一醇之乳酸化脂肪酸酯、Cs-c24脂肪酸之甘油_乳酸酯 、CpC:24脂肪酸之多甘油酯、丙二醇藻蛋白酸酯、蔗糖 CVC24脂肪* g父g旨、二乙驢基酒石酸之一酸及二酸甘油酉旨 、或檸檬酸之一酸及二酸甘油酯、酸醋精及其混合物組 成的群組。 10.如申請專利範圍第1項之組合物,其中該陰離子界面活性 劑係選自由硫酸化油酸丁酯、中鏈及長鏈脂肪酸酯類及 鹽類、有機酸之一酸甘油酯及二酸甘油酯、乙氧化一酸 甘油酯及二酸甘油酯、甘油及丙二醇之乳酸化脂肪酸酯 類、Cs-C24脂肪酸之甘油-乳酸酯、C8_C24脂肪酸之多甘 油酯、蔗糖Cs-C24脂肪酸酯、二乙醯基酒石酸及檸檬酸 之一酸甘油酯及二酸甘油酯及其混合物組成的群組。 11·如申請專利範圍第1項之組合物,其中該陰離子界面活性 89100.doc 200417379 12. 13. 14. 15. 16. 17. 劑係選自由硬脂酸鈉、硬脂酸鉀、棕櫚酸鈉、棕櫚酸鉀 、油酸鈉、硬脂酸甘油酯、乳酸甘油酯、硬脂酸乳酸甘 油酯、蔗糖一硬脂酸酯、蔗糖二硬脂酸酯、蔗糖一月桂 酸酯、蔗糖二月桂酸酯、一硬脂酸多甘油酯、一月桂酸 多甘油酯、Cm-Cm脂肪·酸之甘油-乳酸酯、c14-C2()脂防酸 之多甘油酯、蔗糖CM-C2Q脂肪酸酯及其混合物組成的群 組。 如申請專利範圍第1項之組合物,其中該陰離子界面活性 劑係選自由硬脂酸鈉、棕櫚酸鈉、擰檬酸之一酸甘油酉旨 及二酸甘油酯、乳酸一酸甘油酯及二酸甘油酯及其混合 物組成的群組。 如申請專利範圍第1項之組合物,其係呈口香糖形式,該 陰離子界面活性劑之存在量,以組合物總重為基準,為 約0.1%至2.0%重量比。 如申睛專利範圍第13項之組合物,其中該陰離子界面活 性劑之存在量以組合物總重為基準為約〇·4%至1 ·2%重 量比。 如申請專利範圍第1項之組合物,其係呈糖果形式,該陰 離子界面活性劑之存在量,以組合物總重為基準,為約 〇·1%至20%重量比。 如_請專利範圍第15項之組合物,其中該陰離子界面活 性劑之存在量以組合物總重為基準為約3%至丨5%重量 比。 如申請專利範圍第1項之組合物,其中該組合物係選自由 89100.doc 200417379 口香糖、含餡糖果、牛軋糖、糖果、薄餅、凝膠糖果、 半軟糖、菱形錠、硬糖、薄荷糖、喉片、錠劑、微囊、 糕餅、威化餅、薄膜、錠劑及壓縮錠組成的群組。 18.如申請專利範圍第1項之組合物,其中該組合物係選自由 漱口水、口腔噴霧劑、牙膏、牙粉、牙凝膠、牙霜、牙 線、液劑、凝膠劑以及口腔薄膜生成性潔齒劑組成的君、, 組。 f 19·如申請專利範圍第丨項之組合物,其係呈潔齒劑形式,該 陰離子界面活性劑之存在量以組合物總重為基準為约 〇. 〇 1 %至2 0 %重量比。 如申請專利範圍第丨項之組合物,其中該過氧化物化合物 係以組合物總重為基準,約〇 〇1%至1〇%重量比之污潰移 除有效量存在。 、 21_如申請專利範圍第2〇項之組合物,纟中該過氧化物化合 物係以組合物總重為基準,約〇1%至5%重量比之污潰: 除有效量存在。 22·如申請專利範圍第21項之組合物,纟中該過氧化物化合 物係以組合物總重為基準,約〇 2%至3%重量比之污潰移 除有效量存在。 23.如申請專利範圍第i項之組合物,其係呈口香糖形式,t 中: /、 该過氧化物化合物係以組合物總重為基準,約〇 至10%重量比之污潰移除有效量存在;及 4夕磷酸鹽係以組合物總重為基準,約0 01%至5%重 89100.doc 24.200417379 量比之污潰移除有效量存在。 如申請專利範圍第1項之組合物,其係呈口香糖形式,其 中: /、 該過氧化物化合物係以組合物總重為基準,約〇 〇1% 至10%重量比之污潰移除有效量存在;及 該陰離子界面活性劑係以組合物總重為基準,約〇 至2.0%重量比之污潰移除有效量存在。 25. 26. 27. 28. 如申請專利範圍第丨項之組合物,其係呈口香糖形式,其 中: /、 該多磷酸鹽係以組合物總重為基準,约〇〇1%至5%重 量比之污潰移除有效量存在;及 Μ陰離子界面活性劑係以組合物總重為基準,約〇· 至2·0。/。重量比之污潰移除有效量存在。 如申請專利範圍第1項之組合物,其係呈糖果形式,其中: 該過氧化物化合物係以組合物總重為基準,約〇〇1% 至10°/。重量比之污潰移除有效量存在;及 ▲夕磷鉍鹽係以組合物總重為基準,約〇 〇1%至重 量比之污潰移除有效量存在。 如申請專利範圍第1項之組合物,其係呈糖果形式,其中: 該過氧化物化合物係以組合物總重為基準,約〇 〇1% 至5%重量比之污潰移除有效量存在;及 該陰離子界面活性劑係以組合物總重為基準,約 至20.0%重量比之污潰移除有效量存在。 如申請專利範圍第1項之組合物,其係呈糖果形式,其中: 89100.doc 200417379 29. 30. 31. 32. 33. 34. /夕磷酸鹽係以組合物總重為基準,約〇·_至⑺%重 量比之污潰移除有效量存在;及 该陰離子界面活性劑係以組合物總重為基準,約〇·1.% 至20.0%重量比之污潰移除有效量存在。 如申叫專利|a圍第i項之組合物,進—步包含—種包膠物 質,其係供將過氧化物化合物包膠於組合物内部。 4申叫專利範圍第29項之組合物,其中該包膠物質係選 自由天然樹膠、合成樹膠、食用油、聚合物、烯屬共聚 物、樹脂、蠟、礦油及其混合物組成的群組。 噙申叫專利範圍第1項之組合物,其中該口服可接受之載 劑為固體載劑。 如申Μ專利範圍第1項之組合物,其中該口服可接受之載 劑為樹膠基劑或蠟基劑。 一種由牙齒表面移除污潰之方法,包含將污潰移除有效 量之如申請專利範圍第丨項之組合物投予溫血動物(包括 人類)口腔,供與其牙齒表面接觸。 一種製造如申請專利範圍第丨項之組合物之方法,包含組 合有效量之至少兩種選自過氧化物化合物、多磷酸鹽及 陰離子界面活性劑之活性成分與該口服可接受之載劑。 89100.doc
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-
2002
- 2002-10-31 US US10/285,217 patent/US6685916B1/en not_active Expired - Lifetime
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2003
- 2003-10-28 BR BR0314516-6A patent/BR0314516A/pt not_active Application Discontinuation
- 2003-10-28 AU AU2003286852A patent/AU2003286852B2/en not_active Ceased
- 2003-10-28 CN CN200380100672XA patent/CN1691934B/zh not_active Expired - Fee Related
- 2003-10-28 EP EP03778068A patent/EP1567230A4/en not_active Withdrawn
- 2003-10-28 RU RU2005116317/15A patent/RU2290171C2/ru not_active IP Right Cessation
- 2003-10-28 JP JP2004548645A patent/JP4942298B2/ja not_active Expired - Fee Related
- 2003-10-28 MX MXPA05004696A patent/MXPA05004696A/es active IP Right Grant
- 2003-10-28 WO PCT/US2003/034870 patent/WO2004039277A2/en not_active Ceased
- 2003-10-28 CA CA2493514A patent/CA2493514C/en not_active Expired - Fee Related
- 2003-10-30 AR ARP030103964A patent/AR041869A1/es not_active Application Discontinuation
- 2003-10-31 TW TW092130470A patent/TW200417379A/zh unknown
- 2003-10-31 DO DO2003000744A patent/DOP2003000744A/es unknown
- 2003-10-31 PA PA20038587301A patent/PA8587301A1/es unknown
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- 2003-11-21 US US10/719,602 patent/US20040136928A1/en not_active Abandoned
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2008
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2010
- 2010-04-20 US US12/799,173 patent/US20110150939A1/en not_active Abandoned
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| PE20040549A1 (es) | 2004-09-12 |
| ECSP034825A (es) | 2004-07-23 |
| WO2004039277A3 (en) | 2004-09-10 |
| US20110150939A1 (en) | 2011-06-23 |
| JP5185718B2 (ja) | 2013-04-17 |
| RU2290171C2 (ru) | 2006-12-27 |
| JP4942298B2 (ja) | 2012-05-30 |
| AR041869A1 (es) | 2005-06-01 |
| AU2003286852B2 (en) | 2007-10-18 |
| DOP2003000744A (es) | 2004-05-15 |
| CN1691934B (zh) | 2013-01-09 |
| JP2009024009A (ja) | 2009-02-05 |
| US20040136928A1 (en) | 2004-07-15 |
| BR0314516A (pt) | 2005-08-09 |
| CN1691934A (zh) | 2005-11-02 |
| CA2493514C (en) | 2013-04-23 |
| EP1567230A2 (en) | 2005-08-31 |
| CA2493514A1 (en) | 2004-05-13 |
| AU2003286852A1 (en) | 2004-05-25 |
| EP1567230A4 (en) | 2010-11-10 |
| US6685916B1 (en) | 2004-02-03 |
| WO2004039277A2 (en) | 2004-05-13 |
| PA8587301A1 (es) | 2004-11-26 |
| RU2005116317A (ru) | 2005-11-20 |
| MXPA05004696A (es) | 2005-08-03 |
| JP2006504776A (ja) | 2006-02-09 |
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