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TW201041599A - Oral compositions and uses thereof - Google Patents

Oral compositions and uses thereof Download PDF

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Publication number
TW201041599A
TW201041599A TW98117365A TW98117365A TW201041599A TW 201041599 A TW201041599 A TW 201041599A TW 98117365 A TW98117365 A TW 98117365A TW 98117365 A TW98117365 A TW 98117365A TW 201041599 A TW201041599 A TW 201041599A
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TW
Taiwan
Prior art keywords
composition
oral
abrasive
rda
cerium oxide
Prior art date
Application number
TW98117365A
Other languages
Chinese (zh)
Other versions
TWI476007B (en
Inventor
Andrew Nowak
Shira Pilch
Jim Masters
Original Assignee
Colgate Palmolive Co
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Application filed by Colgate Palmolive Co filed Critical Colgate Palmolive Co
Priority to TW098117365A priority Critical patent/TWI476007B/en
Publication of TW201041599A publication Critical patent/TW201041599A/en
Application granted granted Critical
Publication of TWI476007B publication Critical patent/TWI476007B/en

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Abstract

The present invention is directed to oral compositions comprising an orally-acceptable carrier and a silica abrasive comprising a precipitated amorphous silica compound having an average particle size of from 5 μ m to 20 μ m, oil absorption of from 60 cc/100 g to 120 cc/100 g, and an Einlehner hardness of from 4 to 11, and methods of use thereof.

Description

201041599 六、發明說明: 【發明所屬之技術領域] 本發明係有關-種包括口腔可接受的載劑及二氧化石夕 磨料之口腔用組成物,該二氧化石夕磨料包括具有5帅至 20叫的平均粒徑' 60cc/1〇〇g至12〇cc/1〇〇g的吸油量及4 至11的Einlehner硬度之沉澱非晶形二氧化矽化合物, 使用方法。 ^ 〇 〇 【先前技術】 本發明之背景 口腔用組成物巾之練清除及身體上擦洗牙齒的 表面。此擦洗仙移除牙絲面上之有機生物 ^ 膜)/其主要地由唾液蛋白質、細菌、及細菌副產物形: 薄膜亦可被食物(例如♦啡、茶及莓果)以及被料煙 及產色細菌沾汙及變色。該沾汙薄膜之物理移除 為間早且有效方式移除每日出現的不想要表面 名、 作用。另外’㈣膜之物理移除 2 細菌,從而最小化齒齦炎、牙国斑 人才周炎、及齲蛀形成之可能性。 =而’ 口腔用組成物例如牙粉不應具有如 對珐螂質或組織產生潛在損宝。因而相名f ^致了 組成物,其完美化口腔用組絲:二 最小化有害磨純以避免潛在損害二表力二3 薄膜潔淨比率(PCR),但低程度牙齒磨 才貝’其係測1為放射性牙齒磨損(radi〇active de遍 abrasion,RDA)。 3 201041599 般可接又的慣用常規中,口腔用組成物之rda值通 常保持低於25G以避免經重複使用損傷珐瑯質/齒質 (Μ11)。然而,為了達到更高PCR,磨料之用量及硬度必 須典型地增加,其慣常已知增加。例如,已觀察到當牙 粉組成物之RDA值超過若干數值時(例如高於議至出), 牙粉不必錄麟應增加於牙粉m成果。已挑戰調配呈 有PCR大於80丨90但仍具有RDA餘25〇之口腔用組成 物。 【發明内容】 本發明之摘述 已令人驚訝地發現在口腔用護理組成物中使用特別二 氧化矽磨料給予優秀潔淨能力(如高PCR值),且同時減 少對硬牙齒表面損害(如低PDA)。有用於本發明之二氧化 矽磨料維持其等完整性,同時擦掉牙齒表面上的軟性物質, 例如齒菌斑及薄膜。然而,由於與硬珐螂質或齒質表面相互 作用的結果,二氧化矽磨料在剪力下(如刷淨期間)破壞或 斷裂。在此方面,本發明口腔用組成物提供優秀潔淨及/或磨 光功效,同時達到最小化對珐螂質或齒質潛在損害之想要低 RDA。此外,本發明組成物可提供牙齒表面之潔淨及^或磨 光。潔淨及/或磨光磨料可藉由各種物理參數分類。如熟習技 藝者所領會,單一磨料物種典型地同時執行至少若干$、、Λ 磨光。 在一項具體實例中,本發明係有關組成物L〇, 一種包 括口腔可接受的載劑及二氧化矽磨料之口腔用組成物,該^ 201041599 氧化石夕磨料包括具有5μπι至20μιη的平均粒徑、及4至11 的Einlehner硬度之二氧化石夕化合物。 本發明額外組成物為下列組成物: 1.1 組成物1.0,其中二氧化石夕磨料具有8μιη至11 μπι,如 9μπι至13μιη的平均粒徑。 1.2 組成物1.0或1.1,其中二氧化矽磨料具有60cc/100g 至 120cc/100g,如 70cc/100g 至 110cc/100g,如 80cc/100g至100cc/100g的吸油量,如亞麻籽油吸收。 1.3 任何一種前述組成物,其中二氧化砍磨料具有5至 10,如6至9的Einlehner硬度。 1.4 任何一種前述組成物,其具有80至105,如85至100、 或90至95的薄膜潔淨比率(PCR); 1.5 任何一種前述組成物,其具有小於150,如90至130、 100至120、或105至115的放射性齒質磨損 (radioactive dentin abrasion 5 RDA); 1.6 任何一種前述組成物,其具有0.5至1.5,如0.8、或1 的PCR/RDA比率; 1.7 任何一種前述組成物,其中二氧化石夕磨料係1重量% 至95重量%的組成物。 1.8 任何一種前述組成物,其中二氧化石夕磨料具有d10為 2.5μηι 至 2·9μιη ; 1.9 任何一種前述組成物,其中當口腔用組成物塗敷於口 腔中之硬表面時(如珐瑯質或齒質),二氧化矽磨料 破碎; 5 201041599201041599 VI. Description of the invention: [Technical field to which the invention pertains] The present invention relates to an oral composition comprising an orally acceptable carrier and a cerium oxide cerium abrasive comprising 5 to 20 The method is to use a precipitated amorphous cerium oxide compound having an average particle diameter of '60 cc/1 〇〇g to 12 〇cc/1 〇〇g and an Einlehner hardness of 4 to 11. ^ 〇 〇 [Prior Art] Background of the Invention The composition of the oral composition is removed and the surface of the teeth is scrubbed on the body. This scrub removes the organic biofilm on the surface of the tooth) / it is mainly composed of saliva protein, bacteria, and bacterial by-products: the film can also be used by foods (such as ♦ morphine, tea and berries) and bedding And staining and discoloration of the chromogenic bacteria. The physical removal of the soiled film removes unwanted surface names and effects that occur daily in an early and effective manner. In addition, the (4) membrane physically removes 2 bacteria, thereby minimizing the possibility of gingivitis, dental plaque, and sputum formation. = And 'oral compositions such as dentifrice should not have potential damage to the enamel or tissue. Therefore, the name f ^ caused the composition, which perfected the oral group silk: two minimized the harmful grinding purity to avoid the potential damage of the second surface force 2 3 film clean ratio (PCR), but the low degree of dental grinding Measurement 1 is radioactive tooth wear (radioactive de-abrasion, RDA). 3 201041599 In conventional routines, the rda value of the oral composition is usually kept below 25G to avoid damage to the enamel/tooth quality (Μ11). However, in order to achieve higher PCR, the amount and hardness of the abrasive must be typically increased, which is conventionally known to increase. For example, it has been observed that when the RDA value of the dentifrice composition exceeds a certain number (for example, above the point of arrival), the dentifrice does not have to be added to the dentifrice m result. An oral composition having a PCR greater than 80 丨 90 but still having an RDA remaining 25 Å has been challenged. SUMMARY OF THE INVENTION The present invention has surprisingly found that the use of special cerium oxide abrasives in oral care compositions imparts excellent cleansing power (e.g., high PCR values) while at the same time reducing damage to hard tooth surfaces (e.g., low). PDA). The cerium oxide abrasive used in the present invention maintains its integrity while wiping off soft substances such as plaque and film on the surface of the teeth. However, the cerium oxide abrasive breaks or breaks under shear (e.g., during brushing) as a result of interaction with the hard enamel or dentate surface. In this regard, the oral compositions of the present invention provide excellent cleansing and/or polishing benefits while minimizing the desired low RDA for potential damage to enamel or dentin. In addition, the compositions of the present invention provide cleansing and/or polishing of the tooth surface. Clean and/or polished abrasives can be classified by various physical parameters. As will be appreciated by those skilled in the art, a single abrasive species typically performs at least some $, Λ polishing at the same time. In one embodiment, the invention relates to a composition L〇, an oral composition comprising an orally acceptable carrier and a cerium oxide abrasive, the 201041599 oxidized stone cerium abrasive comprising an average particle having a range of 5 μm to 20 μm Diameter, and 4 to 11 Einlehner hardness of the dioxide dioxide compound. The additional composition of the present invention is the following composition: 1.1 Composition 1.0 wherein the silica dioxide has an average particle diameter of from 8 μm to 11 μm, such as from 9 μm to 13 μm. 1.2 Composition 1.0 or 1.1 wherein the cerium oxide abrasive has a sorption capacity of from 60 cc/100 g to 120 cc/100 g, such as from 70 cc/100 g to 110 cc/100 g, such as from 80 cc/100 g to 100 cc/100 g, such as linseed oil absorption. 1.3 Any of the preceding compositions wherein the oxidized chopped abrasive has an Einlehner hardness of from 5 to 10, such as from 6 to 9. 1.4 Any of the foregoing compositions having a film clean ratio (PCR) of from 80 to 105, such as from 85 to 100, or from 90 to 95; 1.5 any of the foregoing compositions having less than 150, such as from 90 to 130, from 100 to 120 Or radioactive dentin abrasion 5 RDA of 1.6 to 115; 1.6 any of the foregoing compositions having a PCR/RDA ratio of 0.5 to 1.5, such as 0.8, or 1; 1.7 any of the foregoing compositions, wherein The silica stone cerium abrasive is from 1% by weight to 95% by weight of the composition. 1.8 Any of the foregoing compositions, wherein the SiO2 has an d10 of from 2.5 μm to 2·9 μm; 1.9 any of the foregoing compositions, wherein when the oral composition is applied to a hard surface of the oral cavity (such as enamel or Tooth quality), cerium oxide abrasive broken; 5 201041599

種前述組絲,其巾在口腔巾使用組成物時, 二氧切磨料破裂成具有‘為2.3_至2.6μπι之顆 =何-種前述組成物,其中當遭受^夠時間量之剪力 寻’二氧化石夕磨料破裂。 ι„種組成物1>9至U1’其中口腔用組成物係於 牙齒上刷淨至少30秒至5分鐘; 1.13任何-種組成物19至112,其中塗敷於口腔中之硬 表面後,二氧化石夕磨料之平均粒徑減少16%至2〇% ; 1.14任何-種組成物L9至U3,其中塗敷於口腔中之硬 表面後,一氧化石夕磨料之山〇減少9%至12%。 1.15任種前述組成物,包括有效量氣化物鹽,如〇〇ι 重里%至2重I%、如〇.1重量%至〇2重量%的總組 成物重。 1.16任何一種前述組成物,包括氟化物離子源,其包括選 自氟化錫(II)、氟化鈉、I化鉀、單氟填酸鈉、氟石夕 酸鈉、氟矽酸銨、氟化胺、氟化胺氟化銨(aminefluoride ammonium fluoride)、及其組合之氟化物鹽。 1.17任何一種前述組成物,其包括500至5〇〇〇、1〇〇〇至 1500、或1450ppm氟化物離子。 1.18任何一種前述組成物’其包括至少一種界面活性劑。 1.19任何一種前述組成物’其包括至少一種選自月桂基硫 酸鈉、椰油醯胺基丙基甜菜驗、及其組合之界面活性 劑0 201041599 i.20任何-《述組成物’其包括陰離子界面活性劑。 ⑶任何-種前述組成物,其包括月桂基硫酸納。 1.22任何-種前述組成物’其包括至少一種保濕劑。 1.23任何-種前述組成物,其包括至少一種選自甘油、山 梨醇及其組合之保濕劑。 1.24任何一種前述組成物,其包括至少一 1·25任何一種前述組成物,其包括至少一種選自聚乙二 醇、聚乙烯基曱基鍵順丁烯二酸共聚物、多麵(如 纖維素衍生物,例如羧甲基纖維素,或多醣膠,例如 二仙膠或鹿角菜膠)、及其組合之聚合物。 1.26任何一種前述組成物,其包括調味料、香氣及/或著色 劑。 1.27任何一種前述組成物,其包括抗菌劑。 1.28任何一種前述組成物’其包括選自經鹵化的二苯基醚 (二氣)、卓本萃取物或精油(如迷迭香萃取物、 瑞香草、薄荷腦、桉樹腦、柳酸甲酯)、雙胍防腐劑 (如氣己定(chlorhexidine )、阿來西定(alexdine ) 或奥替尼咬(octenidine))、四級銨化合物(如氯化 鯨蠟基吡啶)、酚類防腐劑、海克西定(hexetidine)、 聚維酮峨(povidone iodine)、地莫前列素 (delmopinol)、salifluor、金屬離子(如鋅鹽,例如 檸檬酸鋅)、血根鹼、蜂巢蠟膠(proP〇lis)、及氧化劑 (oxygenating agent)(如過氧化氫、缓衡過氣蝴酸納或 過氧碳酸鈉)之抗菌劑。 7 201041599 1.29任何一種前述組成物,其包括三氯沙。 1.30任何一種前述組成物,其包括抗菌劑呈用量為0.01至 5、0.01至1.0、或0.3重量%的總組成物重。 1.31任何一種前述組成物,其包括牙齒減敏劑; 1.32任何一種前述組成物,其包括選自鉀鹽、辣椒鹼、丁 香酚、勰鹽、鋅鹽、氯化物鹽、或其組合之牙齒減敏 劑; 1.33任何一種前述組成物,其包括牙齒美白化合物; 1.34任何一種前述組成物,其其係牙齒粉末; 1.35任何一種前述組成物,其包括水; 1.36任何一種前述組成物,其係牙膏或凝膠。 1.37任何一種前述組成物,其中口腔用組成物之RDA係藉 由下列方法計算,包括將1至5ml 口腔用組成物漿液 塗敷於1至10cm2表面,使表面對32P放射的牙齒接 觸,於2至5牛頓的恆定力刷淨牙齒表面300行程 (stroke ),其中各行程造成表面對牙齒移動1至 10cm2,及測量RDA值。 1.38任何一種前述組成物,其中當組成物用於口腔時(如 與硬牙齒表面接觸),組成物之RDA隨時間而減少, 且口腔用組成物之RDA係藉由1.37中識別之方法計 算,但書為在最初時間A利用之行程數目少於在稍後 時間B使用之行程數目,如300行程大約等於2分鐘 刷淨; 1.39任何一種前述組成物,其中在口腔中使用5秒的口腔 201041599 用組成物之RDA為1.3至1.6倍在口腔中使用1至5 分鐘(如2、3、或4分鐘)的組成物之RDA。 1.40組成物1.39,其中表面為牙刷之潔淨頭; 1.41組成物1.39或1.40,其中計算RDA之方法為漿液包 括50重量%至100重量%的口腔用組成物。 1.42任何一種前述組成物,其中Einlehner硬度係每174,000 迴轉以黃銅網測量。 1.43任何一種組成物1 ·0至1.41,其中Einlehner硬度係每 100,000迴轉以黃銅網測量。 1.44組成物1.42或1.43,其中Einlehner硬度為100g二氧 化矽磨料於1L水中之漿液。 1.45任何一種前述組成物,其中10%二氧化矽磨料之水性 漿液具有PCR為65至80,如68至76、或72。 1.46任何一種前述組成物,其中10%二氧化矽磨料之水性 漿液具有RDA為75至91,如79至87、或83 ; 1.47任何一種前述組成物,其中10%二氧化矽磨料之水性 漿液具有PCR/RDA比率為0.7至0.9,如0.8至0.9 ’ 如 0.86 ; 1.48任何一種前述組成物,其中15%二氧化石夕磨料之水性 漿液具有PCR為68至84,如62至80、或76。 1.49任何一種前述組成物,其中15%二氧化矽磨料之水性 漿液具有RDA為85至105,如90至100、或95 ; 1.50任何一種前述組成物,其中15%二氧化矽磨料之水性 漿液具有PCR/RDA比率為0.7至0.9,如0.76至〇.8 ’ 201041599 如 0.86 ; 1.51任何一種前述組成物,其中20%二氧化石夕磨料之水性 漿液具有PCR為76至92,如80至88、或84。 1.52任何一種前述組成物,其中20%二氧化矽磨料之水性 漿液具有RDA為85至101,如89至97、或93 ; 1.53任何一種前述組成物,其中20%二氧化發磨料之水性 漿液具有PCR/RDA比率為0.8至1.0,如0.85至0.95, 如 0.9 ; 1.54任何一種前述組成物,其中30%二氧化石夕磨料之水性 漿液具有PCR為78至94,如82至90、或86。 1.55任何一種前述組成物,其中30%二氧化;δ夕磨料之水性 漿液具有RDA為100至124,如106至118、或112 ; 1.56任何一種前述組成物,其中3〇%二氧化矽磨料之水性 漿液具有PCR/RDA比率為0.6至0.9,如0.7至0.8, 如 0.77 ; 1.57組成物1.〇,其中二氧化石夕磨料具有叫爪至iiym,例 如(但不限於)9μηι 至 13μπι、8μιη 至 12μηι、或 8μιη 至Ιίμιη的中數粒徑。 1.58任何一種組成物1.9至112,其中塗敷於口腔中之硬 表面後’一氧化矽磨料之中數粒徑減少16%至20%。 ^使用作為本發明磨料之二氧化矽化合物可為非晶形二 氧=石夕、沉殿二氧化秒、或非晶形沉澱二氧化梦。在一個具 體貫例中,二氧切純實f上由本文所述之二氧化石夕化合 物組成。本文所述之二氧切磨料可料商潔淨劑、牙齒磨 201041599 光劑、及/或抗敏感劑作用。 本發明額外態樣涉及令人驚訝發現為斷裂二氧化矽磨 料顆粒可幫助治療牙齒敏感性,因為斷裂顆粒可堵塞小管封 閉作用(tubule occlusion)。此外,亦已令人驚赞發現較小 顆粒更有效從口腔中裂縫移除碎片及汙跡’特別是牙齒之相 鄰齒間表面。 本發明亦含括方法2.0,一種改良口腔健康之方法,包 括將有效量的組成物1.0至1.55下任何具體實例之口腔用組 成物塗敷於其有需求病患之口腔,如一種方法 1. 減少或抑制齲齒形成, 2. 減少、修補或抑制珐瑯質之預齲蛀損傷,如藉由量 化光誘致螢光(QLF)或電導測量(ECM)偵測, 3. 減少或抑制牙齒去礦質作用及促進牙齒再礦化作 用, 4 ·減少牙齒之過敏性, 5. 減少或抑制齒齦炎, 6. 抑制微生物生物膜形成於口腔中, 7. 減少齒菌斑累積,及/或 8. 潔淨牙齒及口腔。 本發明其他具體實例將顯而易見於熟習技藝者。 本發明之詳述 如本文所用,除非另外指明,本文所述之所有測量水平 係根據總組成物重量。此外’本文引用之所有參考文獻以其 等整體於此併人為參考。然而,萬—有任何於本揭示中定義 201041599 與引用參考文獻中定義之衝突’本揭示控制。 本文所用之「安全及有效量」意指在未傷害口腔之組織 及結構下,治療口腔(如減少齒菌斑、齒齦炎、及/或汙跡) 之足夠用量。 本文所用之「口腔可接受的載劑」意指以安全及有效方 式塗敷本發明組成物於口腔所使用之—或多種材料。 如本文所用,「潔淨」通常係指移除標的表面上之污染 物、灰塵、雜質、及/或外來物質。例如在口腔表面(其中表 面為牙齒珐瑯質)上下文中,潔淨可移除至少若干薄膜或汙 跡’例如齒菌斑生物膜、薄膜或牙石。 如本文所用,「磨光」通常係指使表面更平滑及/或更 光澤之精加工或精練方法。磨光及潔淨亦可提供出現汙跡移 除之表面明亮,例如牙齒表面之美白。 在各種具體實例中,提供具有磨料之口腔用組成物。較 佳者’二氧化矽磨料為沉澱非晶形二氧化矽化合物。 本發明二氧化石夕可具有5μιη至205μηι的平均粒徑。顆 粒之平均粒徑可藉由技藝中已知之任何方式測量。例如,平 均粒徑可使用 Malvern Particle Size Analyzer,Model Mastersizer S » Malvern Instruments, Inc. ( Southborough > Massachusetts,USA)測量,其中氦—氖氣體雷射束投射通 過含有懸浮於水溶液中的磨料之透明光析管(transparent cell)。照在顆粒之光射線散射通過與粒徑成相反比例之角 度。光4貞测器陣列在數個預先決定的角度測量光之數量。與 測量光通量值成比例之電信號然後藉由微電腦系統處理,對 12 201041599 照從樣品與水性分散劑的折射率定義之理論顆粒所預料之 散射圖案以決定主題磨料之粒徑分布。平均粒徑考量歪斜粒 徑及顆粒之尺寸分布。 如本文所用,d1()係指顆粒具有直徑為10%底限的抽樣 族群(亦即10%族群等於或小於山〇值)。 已令人驚訝地發現當口腔用組成物對硬牙齒表面(如齒 質或珐瑯質)刷淨時,併入口腔用組成物之磨料顆粒破壞或 斷裂。亦已令人驚訝地發現當口腔用組成物對口腔之軟表面 或軟生物膜(如薄膜或齒菌斑)刷淨時,併入口腔用組成物 之磨料顆粒大體上保留其等原始尺寸。 本發明二氧化矽磨料可具有特定吸油量60cc/l〇〇g至 120cc/100g亞麻籽油。在一個具體實例中,二氧化矽磨料具 有70cc/100g至110cc/100g的吸油量。在一個具體實例中, 二氧化矽磨料具有80cc/100g至100cc/100g的吸油量。在一 個具體實例中,二氡化矽磨料具有40cc/100g至60cc/100g 的吸油量。吸油量可藉由熟習技藝者已知之各種方式決定。 例如’吸油量可藉由每100克亞麻籽油或酞酸二丁酯(DBP) 或磨料之吸收決定。吸油量值可使用ASTM Rub-Out Method D281測量。 本發明磨料可具有4至11的特定Einlehner硬度。 Einlehner硬度可藉由熟習技藝者已知之各種方式決定。例 如’ Einlehner At-1000 Abrader可以下列方式測量磨料顆粒 之硬度:將長網製紙機(Fourdrinier)金屬網(亦即銅或黃 銅)秤重並暴露於磨料懸浮液(例如,10%磨料之水性懸浮 13 201041599 液)作用達給定數目迴轉(revolution)。硬度值表達成每迴轉 數目(如100,000迴轉)長網製紙機線網之毫克重量損失。 在本發明中’本發明所用二氧化矽磨料之Einlehner硬度係 藉由利用黃銅網決定。將100g二氧化矽添加於1L水,使漿 液旋轉達100,000或174,000迴轉。 本發明磨料成分可以1重量%至95重量%的水平被併 入口服護理產品。磨料的存在量取決於口腔用護理組成物之 特別形式。例如,當口腔用護理組成物為牙膏或凝膠時,其 可含有1%至75%磨料。當口腔用護理組成物為牙粉末時, 其可含有50%至95%磨料。 PCR為熟習技藝者已知的方法以測量相對於標準的移 除牙齒汙跡之功效。本文所指之PCR值係藉由修飾「In vitroThe above-mentioned grouping wire, when the towel is used in the composition of the oral towel, the dioxo prior abrasive is broken into a composition having a size of '2.3_ to 2.6 μπι==--the above-mentioned composition, wherein when subjected to a sufficient amount of time, the shear force is sought 'The dioxide dioxide ruptures. Io composition 1 > 9 to U1' wherein the oral composition is brushed on the teeth for at least 30 seconds to 5 minutes; 1.13 any of the compositions 19 to 112, wherein after application to the hard surface in the mouth, The average particle size of the cerium oxide cerium abrasive is reduced by 16% to 2% by weight; 1.14 any composition L9 to U3, wherein after application to the hard surface in the oral cavity, the yttrium oxide of the cerium oxide is reduced by 9% to 12%. 1.15 Any of the foregoing compositions, including an effective amount of a vaporized salt, such as from 〇〇ι 重里% to 2% by weight, such as from 11% by weight to 〇2% by weight of the total composition weight. The composition comprises a source of fluoride ions comprising: selected from the group consisting of tin (II) fluoride, sodium fluoride, potassium hydride, sodium monofluoroacetate, sodium fluorocarbonate, ammonium fluoroantimonate, amine fluoride, fluorine Amine fluoride ammonium fluoride, and combinations thereof fluoride salts. 1.17 Any of the foregoing compositions comprising 500 to 5 Torr, 1 Torr to 1500, or 1450 ppm fluoride ion. A composition as described above which comprises at least one surfactant. 1.19 Any of the foregoing compositions At least one surfactant selected from the group consisting of sodium lauryl sulfate, cocoamidopropyl beet, and combinations thereof. 0 201041599 i.20 Any - "constituent" which includes an anionic surfactant. (3) Any of the foregoing A composition comprising sodium lauryl sulfate. 1.22 Any of the foregoing compositions comprising at least one humectant. 1.23 Any of the foregoing compositions comprising at least one humectant selected from the group consisting of glycerin, sorbitol, and combinations thereof. 1.24 Any of the preceding compositions comprising at least one of the preceding compositions comprising at least one selected from the group consisting of polyethylene glycol, polyvinyl sulfhydryl bond maleic acid copolymer, multifaceted (eg, fiber) a derivative of a derivative, such as carboxymethylcellulose, or a polysaccharide gum, such as dimethoate or carrageenan, and combinations thereof. 1.26 Any of the foregoing compositions, including flavorings, aromas, and/or colorants 1.27 Any of the foregoing compositions, comprising an antibacterial agent. 1.28 Any of the foregoing compositions' which comprises a halogenated diphenyl ether (dioxane), a extract of Zhuoben or an essential oil (such as rosemary) Extract, thyme, menthol, eucalyptus, methyl salicylate), biguanide preservatives (such as chlorhexidine, alexidine or octenidine), quaternary ammonium Compounds (such as cetylpyridinium chloride), phenolic preservatives, hexetidine, povidone iodine, delmopinol, salifluor, metal ions (such as zinc salts, For example, zinc citrate), blood root base, proP〇lis, and an oxidizing agent (such as hydrogen peroxide, a balance of sodium persulfate or sodium percarbonate). 7 201041599 1.29 Any of the foregoing compositions comprising triclosan. 1.30 Any of the foregoing compositions comprising an antibacterial agent in an amount of from 0.01 to 5, from 0.01 to 1.0, or 0.3% by weight of the total composition. 1.31 any of the preceding compositions, comprising a tooth desensitizing agent; 1.32 any of the foregoing compositions comprising a tooth selected from the group consisting of a potassium salt, a capsaicin, an eugenol, a phosphonium salt, a zinc salt, a chloride salt, or a combination thereof. Sensitizer; 1.33 Any of the foregoing compositions, comprising a tooth whitening compound; 1.34 any of the foregoing compositions, which is a tooth powder; 1.35 any of the foregoing compositions, comprising water; 1.36 any of the foregoing compositions, which is a toothpaste Or gel. 1.37 Any of the preceding compositions, wherein the RDA of the oral composition is calculated by the following method comprising applying 1 to 5 ml of the oral composition slurry to a surface of 1 to 10 cm2 to contact the surface of the 32P-emitted tooth, at 2 A constant force of up to 5 Newtons wipes the tooth surface 300 strokes, wherein each stroke causes the surface to move 1 to 10 cm2 of the tooth and measure the RDA value. 1.38 Any of the preceding compositions, wherein when the composition is applied to the oral cavity (e.g., in contact with a hard tooth surface), the RDA of the composition decreases over time, and the RDA of the oral composition is calculated by the method identified in 1.37. However, the book is that the number of trips utilized at the initial time A is less than the number of trips used at a later time B, such as 300 strokes equal to about 2 minutes of brushing; 1.39 any of the foregoing compositions, wherein 5 seconds of oral cavity is used in the oral cavity 201041599 The RDA of the composition was used in the oral cavity for 1.3 to 1.6 times the RDA of 1 to 5 minutes (e.g., 2, 3, or 4 minutes). 1.40 Composition 1.39, wherein the surface is a clean head of a toothbrush; 1.41 composition 1.39 or 1.40, wherein the method of calculating RDA is that the slurry comprises from 50% to 100% by weight of the oral composition. 1.42 Any of the foregoing compositions wherein the Einlehner hardness is measured in brass nets per 174,000 revolutions. 1.43 Any of the compositions 1 · 0 to 1.41, wherein the Einlehner hardness is measured in brass nets per 100,000 revolutions. 1.44 Composition 1.42 or 1.43, wherein the Einlehner hardness is 100 g of a slurry of cerium oxide abrasive in 1 liter of water. 1.45 Any of the preceding compositions wherein the aqueous slurry of 10% cerium oxide abrasive has a PCR of from 65 to 80, such as from 68 to 76, or 72. 1.46. Any of the foregoing compositions, wherein the aqueous slurry of 10% cerium oxide abrasive has an RDA of from 75 to 91, such as from 79 to 87, or 83; 1.47, any of the foregoing compositions, wherein the aqueous slurry of 10% cerium oxide abrasive has The PCR/RDA ratio is from 0.7 to 0.9, such as from 0.8 to 0.9', such as 0.86; 1.48, any of the foregoing compositions, wherein 15% of the aqueous slurry of the dioxide dioxide has an PCR of 68 to 84, such as 62 to 80, or 76. 1.49 Any of the preceding compositions, wherein the aqueous slurry of 15% cerium oxide abrasive has an RDA of from 85 to 105, such as from 90 to 100, or 95; 1.50 of any of the foregoing compositions, wherein the aqueous slurry of 15% cerium oxide abrasive has The PCR/RDA ratio is from 0.7 to 0.9, such as from 0.76 to 〇.8 '201041599, such as 0.86; 1.51, any of the foregoing compositions, wherein the aqueous slurry of 20% of the dioxide dioxide has an PCR of 76 to 92, such as 80 to 88, Or 84. 1.52 Any of the foregoing compositions, wherein the aqueous slurry of 20% cerium oxide abrasive has an RDA of 85 to 101, such as 89 to 97, or 93; 1.53, any of the foregoing compositions, wherein the aqueous slurry of 20% oxidized abrasive has The PCR/RDA ratio is from 0.8 to 1.0, such as from 0.85 to 0.95, such as 0.9; 1.54, any of the foregoing compositions, wherein 30% of the aqueous slurry of the dioxide dioxide abrasive has a PCR of from 78 to 94, such as from 82 to 90, or 86. 1.55 Any of the foregoing compositions, wherein 30% is oxidized; the aqueous slurry of δ 磨 abrasive has an RDA of from 100 to 124, such as 106 to 118, or 112; 1.56 of any of the foregoing compositions, wherein 3% of the cerium oxide abrasive The aqueous slurry has a PCR/RDA ratio of 0.6 to 0.9, such as 0.7 to 0.8, such as 0.77; 1.57 composition 1. 〇, wherein the SiO 2 abrasive has a claw to iiym, such as (but not limited to) 9μηι to 13μπι, 8μιη The median particle size to 12μηι, or 8μιη to Ιίμιη. 1.58 Any of the compositions 1.9 to 112 in which the number of particles in the niobium oxide abrasive is reduced by 16% to 20% after application to the hard surface in the oral cavity. The use of the cerium oxide compound as the abrasive of the present invention may be amorphous dioxin = shixi, estuary oxidized second, or amorphous precipitated oxidized dream. In a specific example, the dioxin fraction f consists of the cerium oxide compound described herein. The dioxic abrasives described herein can be used as a cleansing agent, a dental grind 201041599, a light agent, and/or an anti-sensitizer. An additional aspect of the invention relates to the surprising discovery that broken cerium oxide abrasive particles can help treat tooth sensitivity because broken particles can block tubule occlusion. In addition, it has been surprisingly found that smaller particles are more effective in removing debris and stains from cracks in the mouth, particularly the interdental surfaces of the teeth. The invention also includes a method 2.0, a method for improving oral health, comprising applying an effective amount of an oral composition of any specific example of 1.0 to 1.55 to an oral cavity of a patient in need thereof, such as a method 1. Reduce or inhibit caries formation, 2. Reduce, repair or inhibit enamel pre-crack damage, such as by quantifying photoinduced fluorescence (QLF) or conductance measurement (ECM) detection, 3. reducing or inhibiting tooth demineralization And promote tooth remineralization, 4 · reduce tooth hypersensitivity, 5. reduce or inhibit gingivitis, 6. inhibit microbial biofilm formation in the mouth, 7. reduce plaque accumulation, and / or 8. clean teeth And the mouth. Other embodiments of the invention will be apparent to those skilled in the art. DETAILED DESCRIPTION OF THE INVENTION As used herein, all measurement levels described herein are based on the total composition weight, unless otherwise indicated. In addition, all references cited herein are hereby incorporated by reference in their entirety. However, there is any conflict between the definitions of 201041599 and the definitions in the cited references. As used herein, "safe and effective amount" means a sufficient amount to treat the oral cavity (e.g., to reduce plaque, gingivitis, and/or smear) in a tissue and structure that does not harm the oral cavity. As used herein, "orally acceptable carrier" means a material or a plurality of materials which are used in the oral cavity in a safe and effective manner for applying the composition of the present invention. As used herein, "clean" generally refers to the removal of contaminants, dust, impurities, and/or foreign matter from the target surface. For example, in the context of an oral surface where the surface is tooth enamel, cleansing can remove at least some of the film or stain' such as plaque biofilm, film or calculus. As used herein, "polishing" generally refers to a finishing or scouring process that results in a smoother and/or more glossy surface. Polishing and cleansing can also provide a bright surface with smudge removal, such as whitening of the tooth surface. In various embodiments, an oral composition having an abrasive is provided. Preferably, the cerium oxide abrasive is a precipitated amorphous cerium oxide compound. The present invention may have an average particle diameter of from 5 μm to 205 μm. The average particle size of the particles can be measured by any means known in the art. For example, the average particle size can be measured using a Malvern Particle Size Analyzer, Model Mastersizer S » Malvern Instruments, Inc. (Southborough > Massachusetts, USA), wherein the xenon-krypton gas laser beam is projected through a transparent material containing abrasive suspended in an aqueous solution. Transparent cell. The light ray scattered by the particles passes through an angle that is inversely proportional to the particle size. The light 4 detector array measures the amount of light at several predetermined angles. The electrical signal proportional to the measured luminous flux value is then processed by a microcomputer system to determine the particle size distribution of the subject abrasive from 12 201041599 following the scattering pattern predicted by the theoretical particles defined by the refractive index of the sample and the aqueous dispersion. The average particle size considers the skewed particle size and the size distribution of the particles. As used herein, d1() refers to a population of particles having a 10% diameter limit (i.e., 10% of the population is equal to or less than the value of the hawthorn). It has been surprisingly found that when the oral composition is brushed against a hard tooth surface such as a tooth or enamel, the abrasive particles incorporated into the oral composition are broken or broken. It has also been surprisingly found that when the oral composition is applied to the soft surface of the oral cavity or soft biofilm (e.g., film or plaque), the abrasive particles incorporated into the oral composition substantially retain their original dimensions. The ceria abrasive of the present invention may have a specific oil absorption of from 60 cc/l to 120 cc/100 g of linseed oil. In one embodiment, the cerium oxide abrasive has an oil absorption of from 70 cc/100 g to 110 cc/100 g. In one embodiment, the cerium oxide abrasive has an oil absorption of from 80 cc / 100 g to 100 cc / 100 g. In one embodiment, the bismuth telluride abrasive has an oil absorption of from 40 cc/100 g to 60 cc/100 g. The amount of oil absorbed can be determined by various means known to those skilled in the art. For example, the oil absorption can be determined by the absorption per 100 grams of linseed oil or dibutyl phthalate (DBP) or abrasive. The oil absorption value can be measured using ASTM Rub-Out Method D281. The abrasive of the present invention can have a specific Einlehner hardness of 4 to 11. The Einlehner hardness can be determined by various means known to those skilled in the art. For example, the 'Einlehner At-1000 Abrader can measure the hardness of abrasive particles in the following manner: Weighing and exposing the Fourdrinier metal mesh (ie copper or brass) to the abrasive suspension (eg 10% abrasive) Suspension 13 201041599 liquid) acts for a given number of revolutions. The hardness value is expressed as the weight loss per kilogram of the number of revolutions (eg, 100,000 revolutions) of the long wire machine. In the present invention, the Einlehner hardness of the cerium oxide abrasive used in the present invention is determined by using a brass mesh. 100 g of cerium oxide was added to 1 liter of water to rotate the slurry to 100,000 or 174,000 revolutions. The abrasive component of the present invention can be administered to the care product at a level of from 1% by weight to 95% by weight. The amount of abrasive present depends on the particular form of the oral care composition. For example, when the oral care composition is a toothpaste or gel, it may contain from 1% to 75% of the abrasive. When the oral care composition is a dental powder, it may contain from 50% to 95% of the abrasive. PCR is a method known to those skilled in the art to measure the efficacy of removing tooth stains relative to the standard. The PCR value referred to herein is modified by "In vitro"

Removal of Stain wkh Dentifrice」,G. κ. St〇〇key 等人,j Dental Research,61 ’ 123-9 ( 1982)中所述之方法而獲得。 修飾本文所用之PCR方法係敘述於兩者為Rice之美國專利 案號5,658,553及5,651,958。在此修飾中,將清激薄膜材料 首先塗敷於牛齒,然後以薄膜材料與茶、咖啡及FeCl3之組 合沾汙,而在由Stookey等人所述原始方法中,薄膜與污跡 兩者係同時塗敷。本發明組成物可具有PCr為8〇至1〇5。 在一個具體實例中’ PCR為85至100。在另一態樣中,PCR 為90至95。 本發明組成物可具有小於15〇,如90至130、100至 120、1〇5至115的RDA值。RDA值可藉由熟習技藝者已知 之任何數量方法決定。例如,RDA值可根據美國專利案號 14 201041599 4,340,583、4,420,312 與 4,421,527、及 Hefferren,Journal of Dental Research,July-August 1976,p.563-573 提出之方法決 定。通常,放射的32P齒質係以如口腔用組成物刷淨。從刷 淨齒質擦走之齒質量係經由在磨料漿液中觀察到之32p分析 予以量化。齒質磨損量係參考在齒質上刷淨之標準組成物, 一般為焦磷酸鈣,其設定RDA值為100。通常,較少磨料 組成物具有更低RDA值。 本發明組成物可具有0.5至1.5的PCR/RDA比率。在 一具體實例中,PCR/RDA 比率可為 〇.5、0.6、0.7、0.8、0.9、 1.0、1.1、1.2、1.3、1.4 或 1.5。使用 PCR/RDA 比率以決定 口腔用護理組成物(如牙粉或牙膏組成物)的潔淨及磨損特 徵之相對配給量。 製備本發明口腔用組成物之有用二氧化矽磨料材料可 從 Davison Chemical Division of W. R. Grace & C〇 (Baltimore ’ Maryland ’ USA)以商品名 GRACE VP5 獲得。 在一具體實例中,二氧化矽為INE0S (現在pQ c〇rp )Removal of Stain wkh Dentifrice, G. κ. St〇〇key et al., j Dental Research, 61 '123-9 (1982). Modifications The PCR methods used herein are described in U.S. Patent Nos. 5,658,553 and 5,651,958, both to each of the entireties. In this modification, the clear film material is first applied to the bovine teeth and then stained with the combination of the film material and tea, coffee, and FeCl3, while in the original method described by Stookey et al., both the film and the stain Apply at the same time. The composition of the present invention may have a PCr of from 8 Å to 1 Å. In one embodiment, the 'PCR' is 85 to 100. In another aspect, the PCR is from 90 to 95. The compositions of the present invention may have an RDA value of less than 15 Å, such as from 90 to 130, from 100 to 120, from 1 to 5 to 115. The RDA value can be determined by any number of methods known to those skilled in the art. For example, the RDA value can be determined in accordance with the methods proposed in U.S. Patent Nos. 14, 2010, 4,599, 4, 340, 583, 4, 420, 312 and 4, 421, 527, and Hefferren, Journal of Dental Research, July-August 1976, p. 563-573. Usually, the radiated 32P tooth system is brushed with, for example, an oral composition. The quality of the teeth removed from the brushed dentin was quantified by the 32p analysis observed in the abrasive slurry. The amount of dentin wear is based on a standard composition that is brushed on the tooth, typically calcium pyrophosphate, which has an RDA of 100. Typically, less abrasive compositions have lower RDA values. The compositions of the invention may have a PCR/RDA ratio of 0.5 to 1.5. In one embodiment, the PCR/RDA ratio can be 5.5, 0.6, 0.7, 0.8, 0.9, 1.0, 1.1, 1.2, 1.3, 1.4, or 1.5. The PCR/RDA ratio is used to determine the relative dosing of the cleansing and wear characteristics of oral care compositions such as dentifrice or toothpaste compositions. A useful ceria abrasive material for preparing the oral compositions of the present invention is available from Davison Chemical Division of W. R. Grace & C (Baltimore ' Maryland] USA under the trade name GRACE VP5. In one embodiment, the cerium oxide is INEOS (now pQ c〇rp)

Sorbosil AC43二氧化石夕。在—具體實例中,Ac43二氧化石夕 具有下列性質,包含(但不限於)平均粒徑為2 7至4 〇微 米(由MALVERN MASTERSIZER決定),篩選殘渣為+ 45μιη,於105°C濕度損失為8.0%最大,於1〇〇〇t:著火損失 (ignition loss)為14.0%最大,及在水性懸浮液中pH為5 5 至 7.5 。 * 其他磨料亦可利用於本組成物中,但考量本發明組成物 可含有如先前敘述之單一二氧化矽磨料化合物,且可大體上 15 201041599 無其他矽或二氡化矽磨料及化合物。 口腔可接受的為技藝中熟知,且可含有界面活性 劑、保濕劑、增稍劑、發泡劑、敗化物離子源、調味料、著 色劑、螯合劑、聚合物、酶、水、活性物、及其他物質。口 腔用組成物可進-步包括Π料接受的細。之特定組 成物取決於組成物之意欲用途。载劑可為液相 、半固相、或 固相。Π則組成物可呈牙粉(包含牙膏、牙粉末、及預防 糊狀物)、糖果(包含膠、珠及η且嚼物)、膜、塗捧凝膠(paint_on )、或熟習使用磨料技藝者已知之任何其他形式。選擇特 定載劑成分取決於想要的產品形式。 ^活性成分包含例如抗菌活性劑、抗牙石劑、抗齲蛀劑、 抗炎劑、抗敏感劑、酶、營養劑等。本文有用之活性物係對 才又予活性物之人類或較低動物患者,以足夠具有想要治療或 預防效果之安全及有效量,無過度負面影響下(例如,毒性、 剌激性、或過敏反應),當用於本發明方法時以合理風險/ 利益比率相稱,視情況存在於本發明組成物中。活性物之特 义女全及有效量將隨如欲治療的特別情況、患者的身體情 况、同時發生的療法(若任何)本質、所用特定活性物、特 疋劑夏形式、所用載劑、及想要的劑量攝生(d〇sage regjmen) 之因素而變化。有用於治療如此情況之活性成分包含D〇yie 專人之美國專利公開案2003/0206874中所討論者。本文有 用者之活性物亦討論於Durga等人之美國專利6,290,933及 1^糾01*之美國專利6,685,92卜 氟化物鹽及氟化物離子源(如可溶解之氟化物鹽)為技 16 201041599 藝中熟知且可併人本發敝成物巾。代表性氟化物離子源包 含(但不限於)氣化錫⑻、氣化納、氟化鉀 納、氟石夕酸納、氟石夕酸錢、氟化胺、氟化銨、及其組合。在 若干具體實例中’氟化物離子源包含⑽錫⑻、氟化納、 氟化胺、單Μ義、以及其混合物。在若干具體實例中, 本發明Π腔賴理組成物亦可含有氟化物料或提供氟的 成分之來源,以足夠供應25ppm至5,00〇ppm氟化物離子之 用量,通常至少50〇ppm,如5〇〇至2〇〇〇ppm,如1〇〇〇至 1600PPm,如1450ppm。氟化物離子源可於一個具體實例中 呈水平G.G1重量%至1G重#%被添加於本發明組成物或 於另一具體實例中呈水平0.03重量%至5重量%,及於另一 具體實例中呈水平0.1重量%至丨重量%組成物;然而,欲 了解提供適當水平氟化物離子之氟化物鹽重量將根據鹽中 相對離子重量而明顯地變化,且熟習技藝者可很快決定該用 量。 本發明口腔用組成物可包含一或多種試劑以増加刷淨 口腔時所製造之泡沫量。該發泡劑為熟習技藝者已知。增加 泡沫量的試劑之說明實例包含(但不限於)聚氧乙烯及若干 聚合物包含(但不限於)藻酸酯聚合物。聚氧乙烯可增加由 本發明口服護理載劑成分產生之泡沫量及泡沫厚度。聚氧乙 烯一般亦已知為聚乙二醇(「PEG」)或聚環氧乙烷。適合 於本發明之聚氧乙烯將具有分子量200,000至7,〇〇〇,〇〇〇。: 一個具體實例中,分子量將為600,000至2,〇〇〇,000,且在另 一具體實例中為800,〇〇〇至ιοοο,οοο。聚氧乙烯存在量可呈 17 201041599 1重置%至%重量% ’於一個具體實例中5重量%至5〇重 量%及於另一具體實例中10重量%至2〇重量%本發明口腔 用護理組錢之口服護理_成分。口㈣護理組成物中發 泡劑劑量(亦即單一劑量)為〇〇1至〇9重量%、〇〇5至 0.5重里/^、且於另一具體實例中〇丨至〇 2重量%。 本發明Μ成物亦可合併—或多種技藝中已知之界面活 性劑。適合界面活性劑包含合理穩定遍佈寬廣阳範圍者, 例如陰離子、陽軒、雜子或兩性離子界性劑。適合 界面活丨生h彳更元全敘述於例如Agric〇ia等人之美國專利號 3,959,458、Haefele之美國專利號3 937 8()7、及⑽如等人 之美國專利號4,051,234,其等併入本文為參考。在若干具 體實例中’本文有用之陰離子界面活性劑包含於烷基具有1〇 至18個碳原子的硫酸烷酯之水溶性鹽及具有1〇至18個碳 原子的脂肪酸磺化單甘油酯之水溶性鹽。月桂基硫酸鈉、月 桂醯基肌胺酸鈉及椰子單甘油酯磺酸鈉為此類型陰離子界 面活性劑實例。亦可利用陰離子界面活性劑之混合物。在另 具體貫例中,有用於本發明之陽離子界面活性劑可概括定 義為具有一個長烷基鏈含有8至18個碳原子的脂族四級銨 化合物之衍生物,例如氣化月桂基三曱基銨、氣化鯨蠟基吡 啶、溴化鯨蠟基三甲基銨、氣化二異丁基苯氧基乙基二曱基 苄基銨、亞硝酸椰子烷基三曱基銨、氟化鯨蠟基吡啶、及^ 混合物。說明陽離子界面活性劑為Briner等人之美國專利 3,535,421中所述四級銨氟化物,本文併入為參考。若干陽 離子界面活性劑亦可作為組成物之殺菌劑。在本發明—個具 18 201041599 體實例中,口腔用組成物大體上無陽離子界面活性劑。可用 於本發明組成物之說明非離子界面活性劑可概括定義為藉 由環氧烷基(本質親水)與可為本質脂族或烷基芳香族之有 機疏水化合物縮合而製造之化合物。適合非離子界面活性劑 實例包含(但不限於)Pluronics、烷基酚之聚環氧乙烷縮合 物、從環氧乙烷與環氧丙烷及伸乙二胺的反應產物縮合而衍 生之產物、脂族醇之環乳乙烧縮合物、長鍵三級胺氧化物、 Q 長鏈二級膦氧化物、長鏈二烧基亞颯、及該等材料之混合 物。在若干具體實例中,有用於本發明之兩性離子合成界面 活性劑可概括定義為脂族四級銨、鱗及锍化合物(sulfonium compound)之衍生物,其中脂族基可為直鏈或分支且其 -個脂族取代基含有8至18個碳原子及—個含有陰科水 洛性基,如絲、雜鹽、魏鹽、雜 2於組成物中之界面活性劑說明實例包二= 〇 基,酸納、月桂醯絲胺_、椰減 驗= 山梨醇酯20、及其組合。 V丞钳未鹼及聚 本發明組成物可包括险雜工w , 納。界面活性劑或相容界面活= 桂基硫酸 重量%至3力重量%及於具體實例中〇.3 重量%的總組成物。 ^貫例中〇·5重量%至2.〇 本發明組成物亦可包含一 味劑。用於實踐本發明之調味卜'彳、纟者已知之調 各種調味搭、酷、醇、及類^1包含(但不限於)精油以及 類似材料。精油實例包含綠薄荷油、 201041599 薄荷油、冬青油、黃樟油、丁香油、鼠尾草油、桉油、馬鬱 蘭油、桂皮油、擰檬油、萊姆油、葡萄柚油、及橙油。亦有 用者為如薄荷腦、香旱芹酮、及茴香腦之化學物。若干具體 實例使用薄荷油及綠薄荷油。調味劑係以濃度0.1至5重量 %及0.5至1.5重量%併入口腔用組成物。在個別口腔用護 理組成物劑量中(亦即單一劑量)之調味劑劑量為0.001至 0.05重量%及於另一具體實例為0.005至0.015重量%。 本發明口腔用護理組成物亦可視情況包含一或多種能 夠使在細菌細胞壁中發現的約錯合之螯合劑。結合此I弓使細 菌細胞壁變弱及擴大細菌溶胞。可有用於本發明之螯合劑的 另一組群為可溶性焦磷酸鹽。用於本組成物之焦磷酸鹽可為 任何鹼金屬焦磷酸鹽。在若干具體實例中,鹽包含四鹼金屬 焦構酸鹽、二驗金屬二酸焦礙酸鹽、三驗金屬單酸焦構酸鹽 及其混合物,其中鹼金屬為鈉或鉀。鹽係有用於其等水合及 未水合形式兩者。有用於本組成物之有效量焦磷酸鹽通常足 夠提供至少1.0重量%焦磷酸根離子、1.5重量%至6重量 %、3.5重量%至6重量%的該離子。 本發明口腔用組成物亦視情況包含一或多種聚合物,例 如聚乙二醇、聚乙烯基曱基醚順丁烯二酸共聚物、多醣類(如 纖維素衍生物,例如叛曱基纖維素,或多_膠,例如三仙膠 或鹿角菜膠)。酸性聚合物(例如聚丙烯酸酯凝膠)可呈其 等自由酸或部分或全部中和的水溶性鹼金屬(如鉀及鈉)或 銨鹽形式提供。若干具體實例包含1 : 4至4 : 1順丁烯二酐 或酸與另一可聚合乙烯系不飽和單體之共聚物,例如具有分 20 201041599 子量(M.W.) 30,0〇〇至丨,〇〇〇,〇〇〇之曱基乙烯基醚(甲氧基 乙烯)。此等共聚物係可得例如為GAF Chemicals Corporation 之 GantrezAN 139(M.W.500,000)、AN 119(M.W.250,000) 及S_97醫藥等級(M.W.70,000)。其他操作聚合物包含例 如順丁烯二酐與丙烯酸乙酯、曱基丙烯酸羥乙酯、N_乙烯基 -2-吡咯酮(N-vinyl-2-pyr〇liidone)、或乙烯(後者係可得例如 為 Monsanto EMA No. 11〇3,M.W. 10,000 及 EMA Grade 61 ) 〇 之1 : 1共聚物,及丙烯酸與甲基或羥乙基甲基丙烯酸酯、 甲基或乙基丙烯酸酯、異丁基乙烯基醚或Ν_乙烯基_2_吡咯 酉同之1 : 1共聚物。適合者通常為含有活化碳對碳浠烴雙鍵 及至少一個敌基之聚合稀煙系或乙稀系不飽和叛酸,亦即含 有烯烴雙鍵之酸,該烯烴雙鍵很快於聚合起作用係因為其呈 相對羧基為α-β位置或作為部分亞曱基端基存在於單體分 子。該酸之說明為丙烯酸、曱基丙烯酸、乙基丙烯酸、α_ 氯丙烯酸、巴豆酸、β-丙烯氧基丙酸、山梨酸、α_氯山梨酸、 Q 桂皮酸、β-苯乙烯基丙烯酸、黏康酸、衣康酸、彳寧康酸、中 康酉文、戊細一酸、烏頭酸、α-苯基丙稀酸、2-节基丙稀酸、 2-環己基丙烯酸、白芷酸、繳形酸、反丁烯二酸、順丁烯二 酸及酐。與該羧酸單體可共聚合之其他不同烯烴單體包含乙 烯基乙酸酯、氯乙烯、順丁烯二酸二曱酯等。共聚物含有充 足水溶性用之羧酸鹽基。進一步分類的聚合劑包含含有經取 代丙烯醯胺的同元聚合物及/或不飽和磺酸及其鹽的同元聚 合物之組成物’特別是其中聚合物係以具有分子量1000至 2,000,000選自丙烯醯胺基烷磺酸(如2_丙烯醯胺2甲基丙 21 201041599 烧續酸)之不飽和磺酸為主,敘述於Zahid於1989年6月 27曰之美國專利案號4,842,847,併入本文為參考。 在製備口腔用護理組成物中,有時必須添加若干增稠材 料以提供想要稠度或穩定或增進調配物之性能。在若干具體 貫例中’增稠劑為羧乙烯基聚合物、鹿角菜膠、羥乙基纖維 素及纖維素醚之水溶性鹽(例如羧甲基纖維素鈉及羧曱基羥 乙基纖維素鈉)。亦可合併天 然膠,例如刺梧桐膠、阿拉伯 膠、及黃蓍膠。膠狀矽酸鎂鋁或精細分割的二氧化矽可使用 作為增稠組成物之成分以進一步改良組成物質地。在若干具 體實例中’使用增稠劑呈用量0.5重量%至5.0重量%的總 組成物。 本發明口腔用護理組成物亦可視情況包含一或多種 酶。有用的酶包含任何可得之蛋白酶、葡聚糖水解酶、内醣 皆酶、殿粉酶、葡聚糖變構水解酶(mutanase)、脂酶及黏 蛋白酶或其相容混合物。在若干具體實例中,酶為蛋白酶、 聚葡糖酶、内醣苷酶及葡聚糖變構水解酶。在另一具體實例 中’酶為木瓜酶、内醣苷酶或聚葡糖酶與葡聚糖變構水解酶 之混合物。適合用於本發明之額外酶係揭示MDring等人之 美國專利案號5,000,939 '美國專利案號4,992,420、美國專 利案號4,355,022、美國專利案號4,154,815、美國專利案號 4,058,595、美國專利案號3,991,177、及美國專利案號 3,696,191,所有併入本文為參考。本發明中數種相容酶之混 合物的酶構成0.002%至2.0%於一個具體實例中,或〇〇5 %至1.5%於另一具體實例中,或〇 1%至〇 5%於又—具體 22 201041599 實例中。 水亦可存在於本發明口腔用組成物中。用於製 腔用組成物之水應去離子化且無有_f。水—般補償組 物的差額且包含10重量%至90重量%、2〇重量%至6^ 堇%或10重量%至30重量%的口腔用組成物。此水量包人 加上以其他材料(例如山梨醇或本發明任何成分)導: 而添加之自由水。 里Sorbosil AC43 dioxide dioxide. In a specific example, Ac43 dioxide has the following properties, including but not limited to an average particle size of 27 to 4 μm (determined by MALVERN MASTERSIZER), a screening residue of + 45 μm, and a humidity loss at 105 ° C. It is 8.0% maximum, at 1 〇〇〇t: the ignition loss is 14.0% maximum, and the pH in the aqueous suspension is 5 5 to 7.5. * Other abrasives may also be utilized in the present compositions, but it is contemplated that the compositions of the present invention may contain a single cerium oxide abrasive compound as previously described, and may generally have no other bismuth or bismuth telluride abrasives and compounds. Orally acceptable is well known in the art and may contain surfactants, humectants, extenders, foaming agents, ionized ion sources, flavorings, colorants, chelating agents, polymers, enzymes, water, actives And other substances. The oral cavity composition can be further stepped to include the fineness of the tanning material. The particular composition depends on the intended use of the composition. The carrier can be in the liquid phase, semi-solid phase, or solid phase. Π The composition can be tooth powder (including toothpaste, tooth powder, and prevent paste), candy (including glue, beads and η and chew), film, paint gel (paint_on), or familiar with the use of abrasives Any other form known. The choice of a particular carrier component depends on the desired product form. The active ingredient contains, for example, an antibacterial active agent, an anticalculus agent, an anticonvulsant, an anti-inflammatory agent, an anti-sensitivity agent, an enzyme, a nutrient, and the like. An active substance useful herein is a human or lower animal patient which is active enough to have a therapeutically or prophylactically effective amount, without undue adverse effects (eg, toxicity, irritability, or Allergic reactions), when used in the methods of the invention, are commensurate with a reasonable risk/benefit ratio, as the case may be, in the compositions of the invention. The specific and effective amount of active substance will vary depending on the particular condition being treated, the condition of the patient, the nature of the concurrent treatment (if any), the particular active used, the summer form of the ampoule, the carrier used, and The desired dose (d〇sage regjmen) varies. There are those discussed in U.S. Patent Publication No. 2003/0206874, which is incorporated herein by reference. The actives of the present invention are also discussed in U.S. Patent No. 6,290,933 to Durga et al., and U.S. Patent No. 6,685,92, the disclosure of the disclosure of the disclosure of the disclosure of U.S. Patent No. 6,685,92, the fluoride salt and the fluoride ion source (e.g., the soluble fluoride salt). It is well known in the art and can be combined into a towel. Representative fluoride ion sources include, but are not limited to, vaporized tin (8), gasified sodium, potassium fluoride nano, sodium fluorite, fluorescein, amine fluoride, ammonium fluoride, and combinations thereof. In several embodiments, the fluoride ion source comprises (10) tin (8), sodium fluoride, amine fluoride, mono-synonym, and mixtures thereof. In some embodiments, the limulus composition of the present invention may also contain a source of fluorinated material or a fluorine-providing component in an amount sufficient to supply 25 ppm to 5,00 ppm of fluoride ion, usually at least 50 ppm, Such as 5 〇〇 to 2 〇〇〇 ppm, such as 1 〇〇〇 to 1600 ppm, such as 1450 ppm. The fluoride ion source may be added to the composition of the invention in a level of G.G1 wt% to 1 G weight #% in one embodiment or in a range of 0.03 wt% to 5% by weight in another embodiment, and in another In a particular example, the composition is present in a level of from 0.1% by weight to 5% by weight; however, it is to be understood that the weight of the fluoride salt providing the appropriate level of fluoride ion will vary significantly depending on the relative ion weight in the salt, and the skilled artisan can quickly decide This amount. The oral compositions of the present invention may comprise one or more agents to add to the amount of foam produced when the mouth is brushed. Such blowing agents are known to those skilled in the art. Illustrative examples of agents that increase the amount of foam include, but are not limited to, polyoxyethylene and several polymers including, but not limited to, alginate polymers. Polyoxyethylene can increase the amount of foam and foam thickness produced by the oral care vehicle component of the present invention. Polyoxyethylene is also generally known as polyethylene glycol ("PEG") or polyethylene oxide. The polyoxyethylene suitable for the present invention will have a molecular weight of 200,000 to 7, 〇〇〇, 〇〇〇. : In a specific example, the molecular weight will be 600,000 to 2, 〇〇〇, 000, and in another specific example, 800, ι to ιοοο, οοο. The amount of polyoxyethylene present may be 17 201041599 1 reset % to % by weight 'in one embodiment 5% by weight to 5% by weight and in another embodiment 10% to 2 〇 by weight of the present invention for oral use Nursing group money oral care _ ingredients. The foaming agent dose (i.e., single dose) in the oral (iv) care composition is from 1 to 9 weight percent, from 5 to 0.5 weight percent, and in another embodiment from 2 to 2 weight percent. The compositions of the present invention may also incorporate - or a variety of interfacial agents known in the art. Suitable surfactants include those that are reasonably stable throughout the broad range, such as anionic, cation, hetero or zwitterionic binders. For example, U.S. Patent No. 3,959,458 to Agric, et al., U.S. Patent No. 3,937,8, to Haefele, and (10) U.S. Patent No. 4,051,234 to et al. And the like is incorporated herein by reference. In certain embodiments, the anionic surfactant useful herein comprises a water soluble salt of an alkyl sulfate having from 1 to 18 carbon atoms in the alkyl group and a sulfonated monoglyceride having a fatty acid having from 1 to 18 carbon atoms. Water soluble salt. Examples of anionic surfactants of this type are sodium lauryl sulfate, sodium lauryl sarcosinate and sodium coconut monoglyceride sulfonate. Mixtures of anionic surfactants can also be utilized. In another specific example, a cationic surfactant useful in the present invention can be broadly defined as a derivative of an aliphatic quaternary ammonium compound having a long alkyl chain having from 8 to 18 carbon atoms, such as gasified lauryl tris. Mercaptoammonium, gasified cetylpyridine, cetyltrimethylammonium bromide, diisobutylphenoxyethyldimylbenzylammonium hydride, coconut alkyltrimethylammonium nitrite, fluoride a mixture of cetyl pyridyl, and ^. The cation-surfactant is described in U.S. Patent No. 3,535,421, the entire disclosure of which is incorporated herein by reference. A number of cationic surfactants can also be used as a bactericide for the composition. In the present invention, an embodiment of the invention, the oral composition is substantially free of cationic surfactants. Description of the Compositions of the Invention The nonionic surfactant can be broadly defined as a compound produced by the condensation of an alkylene oxide (essentially hydrophilic) with an organic hydrophobic compound which can be an essential aliphatic or alkyl aromatic. Examples of suitable nonionic surfactants include, but are not limited to, Pluronics, polyethylene oxide condensates of alkyl phenols, products derived from the condensation of ethylene oxide with a reaction product of propylene oxide and ethylenediamine, A cyclic alcoholic condensate of an aliphatic alcohol, a long-chain tertiary amine oxide, a Q long-chain secondary phosphine oxide, a long-chain dialkyl hydrazine, and a mixture of such materials. In several embodiments, a zwitterionic synthetic surfactant useful in the present invention can be broadly defined as a derivative of an aliphatic quaternary ammonium, squama, and sulfonium compound, wherein the aliphatic group can be straight or branched and An aliphatic substituent containing 8 to 18 carbon atoms and a surfactant containing a sinophilic water-based group such as silk, a hetero salt, a Wei salt, and a hybrid 2 are illustrated in the composition package 2 = 〇 Base, sodium sulphate, laurel sulphate _, coconut reduction test = sorbitol ester 20, and combinations thereof. V-clamps are not alkali and poly. The composition of the present invention may include a handyman w, nano. Surfactant or compatible interface activity = cresyl sulphate weight % to 3 liters by weight and in the specific example 〇 3% by weight of the total composition. In the example, 5% by weight to 2. 〇 The composition of the present invention may also contain a flavoring agent. The seasonings used in the practice of the present invention are known to those skilled in the art. Various flavorings, cools, alcohols, and the like include, but are not limited to, essential oils and the like. Examples of essential oils include spearmint oil, 201041599 peppermint oil, wintergreen oil, sassafras oil, clove oil, sage oil, eucalyptus oil, marjoram oil, cinnamon oil, lemon oil, lime oil, grapefruit oil, and orange oil. . Also used are chemicals such as menthol, fragrant celery, and fennel. Peppermint oil and spearmint oil are used in several specific examples. The flavoring agent is incorporated into the oral composition at a concentration of 0.1 to 5% by weight and 0.5 to 1.5% by weight. The dosage of the flavoring agent in the dosage of the individual oral care composition (i.e., a single dose) is from 0.001 to 0.05% by weight and in another embodiment from 0.005 to 0.015% by weight. The oral care compositions of the present invention may also optionally contain one or more chelating agents which are capable of being found in the bacterial cell wall. In combination with this I bow, the cell wall of the bacteria is weakened and the bacterial lysis is expanded. Another group that may be present in the chelating agents of the present invention is soluble pyrophosphate. The pyrophosphate used in the present composition may be any alkali metal pyrophosphate. In a number of specific examples, the salt comprises a tetra alkali metal pyroester, a dimetal bis-acid caustic acid salt, a tri-metal monocarboxylic acid pyro-acid salt, and mixtures thereof, wherein the alkali metal is sodium or potassium. Salts are used in both hydrated and unhydrated forms. An effective amount of pyrophosphate salt for use in the present composition is generally sufficient to provide at least 1.0% by weight pyrophosphate ion, 1.5% to 6% by weight, and 3.5% to 6% by weight of the ion. The oral composition of the present invention optionally also comprises one or more polymers, such as polyethylene glycol, polyvinyl mercaptoether maleic acid copolymer, polysaccharides (such as cellulose derivatives, such as renegade groups). Cellulose, or poly-gel, such as Sanxian gum or carrageenan. The acidic polymer (e.g., polyacrylate gel) can be provided in the form of a free acid or a partially or fully neutralized water-soluble alkali metal (e.g., potassium and sodium) or ammonium salt. Several specific examples include 1:4 to 4: 1 maleic anhydride or a copolymer of an acid and another polymerizable ethylenically unsaturated monomer, for example, having a fraction of 20 201041599 (MW) 30,0〇〇 to 丨, 〇〇〇, 〇〇〇 曱 乙烯基 vinyl ether (methoxyethylene). Such copolymers are available, for example, as GantrezAN 139 (M.W. 500,000), AN 119 (M.W. 250,000) and S_97 medical grade (M.W. 70,000) of GAF Chemicals Corporation. Other operating polymers include, for example, maleic anhydride with ethyl acrylate, hydroxyethyl methacrylate, N-vinyl-2-pyrrolidone (N-vinyl-2-pyr〇liidone), or ethylene (the latter For example, Monsanto EMA No. 11〇3, MW 10,000 and EMA Grade 61) 1:1 of the copolymer, and acrylic acid with methyl or hydroxyethyl methacrylate, methyl or ethyl acrylate, isobutyl A vinyl ether or a ruthenium-vinyl-2-pyrrolidine with a 1:1 copolymer. Suitable as a polymerized dilute or ethylenic unsaturated taurine containing activated carbon to a carbon-hydrocarbon double bond and at least one enemy group, that is, an acid containing an olefinic double bond, the olefin double bond is rapidly polymerized. The role is due to the presence of a monomeric molecule at the alpha-beta position relative to the carboxyl group or as a partial sulfhydryl end group. The description of the acid is acrylic acid, mercaptoacrylic acid, ethacrylic acid, α_chloroacrylic acid, crotonic acid, β-acryloxypropionic acid, sorbic acid, α-chlorosorbic acid, Q cinnamic acid, β-styrylacrylic acid, Muconic acid, itaconic acid, 彳nukangic acid, Zhongkang 酉文, 戊细一酸, aconitic acid, α-phenyl acrylic acid, 2-mercapto acrylic acid, 2-cyclohexyl acrylic acid, leucovoric acid, Acid, fumaric acid, maleic acid and anhydride. Other different olefin monomers copolymerizable with the carboxylic acid monomer include vinyl acetate, vinyl chloride, dinonyl maleate, and the like. The copolymer contains a carboxylate group which is sufficient for water solubility. Further classified polymeric agents comprise a composition of a homopolymer comprising a substituted acrylamide and/or an unsaturated sulfonic acid and a salt thereof, wherein the polymer is selected from the group consisting of having a molecular weight of from 1000 to 2,000,000. The propylene sulfhydryl alkane sulfonic acid (e.g., 2 propylene amide 2 methyl propyl 21 201041599 succinic acid) is an unsaturated sulfonic acid, and is described in U.S. Patent No. 4,842,847, issued to Zahid on June 27, 1989, and This article is incorporated by reference. In the preparation of oral care compositions, it is sometimes necessary to add a plurality of thickening materials to provide the desired consistency or to stabilize or enhance the properties of the formulation. In a number of specific examples, 'thickeners are carboxyvinyl polymers, carrageenan, hydroxyethyl cellulose, and water-soluble salts of cellulose ethers (eg, sodium carboxymethyl cellulose and carboxymethyl hydroxyethyl fibers). Sodium). Natural gums such as karaya gum, gum arabic, and tragacanth can also be combined. Colloidal magnesium aluminum silicate or finely divided cerium oxide can be used as a component of the thickening composition to further improve the constituent materials. In some specific examples, the thickener is used in an amount of from 0.5% by weight to 5.0% by weight of the total composition. The oral care compositions of the present invention may also optionally comprise one or more enzymes. Useful enzymes include any available protease, glucan hydrolase, endoglycosidase, phosphatase, mutanase, lipase and mucin or a compatible mixture thereof. In several embodiments, the enzyme is a protease, a polyglucosidase, a endoglycosidase, and a dextran allosteric hydrolase. In another embodiment, the enzyme is a mixture of papain, endoglycosidase or polyglucosidase and a dextran allosteric enzyme. Additional enzymes suitable for use in the present invention are disclosed in U.S. Patent No. 5,000,939, U.S. Patent No. 4,992,420, U.S. Patent No. 4,355,022, U.S. Patent No. 4,154,815, U.S. Patent No. 4,058,595, U.S. Patent No. 3, 991, 177, and U.S. Patent No. 3,696, 191, incorporated herein by reference. The enzyme of a mixture of several compatible enzymes in the present invention constitutes 0.002% to 2.0% in one specific example, or 〇〇5% to 1.5% in another specific example, or 〇1% to 〇5% in another- Specific 22 in the 201041599 instance. Water may also be present in the oral compositions of the present invention. The water used for the composition for the cavity should be deionized and free of _f. The water generally compensates for the difference in composition and comprises from 10% to 90% by weight, from 2% by weight to 6% by weight or from 10% to 30% by weight of the oral composition. This amount of water is added to the free water added by other materials (such as sorbitol or any of the ingredients of the present invention). in

本發明組錢亦可包括_#丨,如阻止喊物暴露於* 氣時免於硬化。若干保關亦可料牙成物想要甜 風味。以_濕劑為主之保關財於—個具體 重量%至7〇重量%或於另—具體實例中包含%重量^ 65重量%的牙粉組成物。適合保關包含食用多元醇,例如 甘油、山梨醇、木轉、丙二醇以及其他多元醇及此等保渴 劑之混合物。甘油及山㈣之混合物可㈣若干具體實例中 作為本文牙膏組成物之保濕劑成分。 本發明組成物亦可包含-或多種抗菌劑。抗菌劑為技藝 中已知且包含节酸、苄酸鈉、节酸鉀、硼酸、及酚化合物例 如β萘盼(betanaphthol )、氯瑞香草酚、瑞香草紛、菌香腦、 按樹腦、香旱芽盼、薄荷腦、齡、戊盼、己紛、庚 己間苯二盼、氯化月桂基《、氯化肉豆蔻基吼咬、說化綠 蠟基吡。疋、氣化鯨蠟基吡啶、溴化鯨蠟基吡啶、及經鹵化的 二苯基趟(例如三氣沙)。本發明組成物亦可包含一或多種 呈自由鹼或鹽形式之驗性胺基酸’如精胺酸。該試劑可取決 於所選之試劑以有效量如丨重量%至2G重量% (以組成物 23 201041599 總重為基礎)添加。 本發明組成物可合併一或多 酸鉀、碳酸氫鉀、氯化卸 几敏感劑’如鉀鹽例如确 丁香酴;銷鹽;辞鹽;氯化物鹽及 草酸鉀,·辣椒驗; 所選之試劑以有效量如i重量 ^二该試劑可取決於 重為基礎)添加。本發明組絲* ^ (以組成物總 療由阻塞齒質小管(de義tubule);過敏性牙齒時亦可用於治 本發明組成物亦可包含技藝中已知之 =成物。適合美白及漂白組成物包含過氧化i = 祿鹽、過賴鹽。魏化物包含4職化物 驗及驗土金屬之過氧化物、有機過氧基化合物、過氧酸風及 其混合物。驗聽土金屬之過氧化物包含過氧驗、過氧化 卸、過氧化納、過氧化鎂、過氧化舞、過氧化鋇、及盆混人 物。其他過氧化物包含過硼酸鹽、脲過氧化物、及盆混人物〇 適合金屬亞氯酸鹽可包含亞氯酸舞、亞氯酸鋇、亞氣酸鎮、 亞氣酸鐘、亞氯_、及亞氣酸鉀。該試劑可取決於所選之 試劑以有效量如1重量%至20重量% (以組成物總重為基 礎)添加。 除了上述成分外,本發明具體實例可含有若干下述之多 樣化視情況牙粉成为。視情況成分包含例如(但不限於)魏 著劑、皂洗劑、調味劑、甜味劑、額外抗齒菌斑劑、磨料、 及者色劑。此專及其他視情況成分進一步敛述於Maj eti之美 國專利案號5,004,597、Agricola等人之美國專利案號 3,959,458、及 Haefele 之美國專利案號 3,937,8〇7。 24 201041599 本口腔用組成物用之磨料選擇可解釋為純類型、细产 (粒徑)、、粒徑分布及磨料用量,以確保牙齒珐瑯質在正^ 使用組成物期間無法過度地擦掉’但充分地潔淨及/或磨 光。。在口腔護理上下文中,磨料之功效可根據牙粉之潔淨或 磨損準則表達’即分別薄難淨比率(PCR)或放射性齒質 磨損(RDA)。執行PCR及RDA之方法為技藝中已知,如 敘述於如美國專利案號5,939,051及6,290,933。 在若干具體實例中,組成物係對人類或其他動物安全於 口腔使用,且任何達到以上提出要求之口腔用或化妝可接受 的磨料可被選擇於口腔用組成物。 額外磨料亦可被包含於本發明組成物中,包含鋁氧(煅 乳化銘)、石夕藻土、浮石、礙酸甸 ' 墨魚骨(cuttieb〇ne)、不 溶填酸鹽、複合樹脂(例如三聚氰胺樹脂、紛樹脂、及脲_ 曱醛樹脂)、聚碳酸酯、碳化硼、微晶蠟、微晶纖維素(包 含膠狀微晶纖維素及羧曱基纖維素之組合)、及其組合及衍 生物。在不溶磷酸鹽中,有用磨料為原磷酸鹽、聚偏磷酸鹽 及焦磷酸鹽。說明實例為二水合原磷酸二鈣、二水合磷酸二 釣、磷酸氫鈣、焦磷酸鈣、焦磷酸β-鈣、磷酸三鈣、偏磷酸 約、偏構酸鉀、及偏鱗酸鈉。 在若干具體實例中,口腔用組成物係呈牙粉形式,且示 範載劑大體上為半固體或固體。載劑可為水性,亦即包括5 %至95%水。在其他具體實例中’載劑大體上為非水性。載 劑視情況包括例如口腔用護理活性成分、表面活性劑(例如 界面活性劑、乳化劑、及泡沫調節物)、黏度改質劑與增稠 25 201041599 劑、保濕劑、稀釋劑、填料、額外pH改質劑、著色劑、防 腐劑、溶劑、及其組合。欲瞭解雖然以上種類各材料之一般 屬性可不同,但可有若干共同屬性且任何給定材料可供應多 重目的於二或多項該種類材料内。如熟習技藝者認識,除了 先前敘述之彼等材料外,口腔用組成物視情況包含其他材 料,包含例如軟化劑、潤膚劑(Moisturizer)、口感劑等。口 腔用組成物之適合載劑實例係討論於Boyd等人之美國專利 案號6,669,929、Gebreselassie等人之美國專利案號 6,379,654、及Nabi等人之美國專利案號4,894,220。 口腔用組成物視情況包括抗詰石組成物’例如Gaffar 等人之美國專利案號5,292,526中所述之一或多種抗結石組 成物。在各種具體實例中,抗結石組成物包含一或多種聚磷 酸鹽。抗結石組成物可包含至少一種以有效抗結石量存在於 口腔用組成物中之完全或部分中和的鹼金屬或銨三聚碟酸 鹽或六偏磷酸鹽。抗結石活性物亦可包含至少一種呈有效抗 結石量之水溶性、直線、分子脫水的聚磷酸鹽。抗結石活性 物亦可包含鉀及鈉鹽之混合物,其至少一種係以有效抗結石 量存在作為聚磷酸鹽抗結石劑。抗結石活性劑亦可含有呈鈉 及鉀鹽混合物存在之有效抗結石量之直線分子脫水的聚磷 酸鹽抗結石劑。組成物中鉀與鈉之比率可高至小於3 : 1。聚 磷酸鹽可呈各種用量存在於口腔用組成物中,例如用量為聚 磷酸根離子(polyphosphate ion)與抗菌劑之重量比率範圍超 過0.72 : 1至小於4 : 1 ’或抗菌增進劑與聚磷酸根離子之重 量比率範圍1 : 6至2.7 : 1,或抗菌增進劑與聚磷酸鹽之重 26 201041599 量比率範圍1:6至2.7·· 1。其他有用抗結石劑包含聚紐 酯聚合物及聚乙烯基甲基驗/順丁烯二軒(PVM/μα)共聚 物,例如 GANTREZ®。 有用於本發明牙粉組成物之另外活性劑為抗菌劑,其可 以用量0.001至3.0重量%的口腔用組成物存在。有用額外 口腔用護理化合物之非限定表單包含非離子抗菌劑,包含酚 及雙酚化合物’例如經鹵化的二苯基醚,包含三氯沙(2 4 4,_ 三氯-2’-經-二苯基驗)、三氯卡班(triclocarban) ( 3 4 4_ 二氣均·一本腺 ’ 3,4,4_tricliloroC3Tb3iiili<le),以及 2·笨氧其_ 乙醇、苄酸酯、及均二苯脲(carbanilide)。經齒化的二苯基醚 (例如三氣沙)可例如以用量0.3重量%的口腔用組成物存 在。 適合表面活性劑為合理穩定遍佈寬廣pH範圍者。此等 化合物為技藝中熟知,且包含非肥皂陰離子(如月桂基硫酸 納(SLS)、N-肉莖蔻蕴基及N-棕橺醯基肌胺酸),非離子 (如聚山梨糖醇酯(Polysorbate) 20(聚氧乙烯20山梨醇酐單 月桂酸酯’ TWEEN⑧20)及聚山梨糖醇酯80 (聚氧乙烯2〇 山梨醇酐單油酸酯 ’ TWEEN® 80 )、P〇l〇xamer 407、從 BASF Corporation可得之商品名PLURONIC® FI27),陽離子,兩 性離子(如椰油醯胺基丙基甜菜驗及月桂醯胺基丙基甜菜 驗)’及兩性有機合成清潔劑。用於口腔用組成物之適合表 面活性劑實例係討論於例如Nabi等人之美國專利案號 4,894,220、Glandorf等人之美國專利案號6,555,094、及 Lawlor等人之美國專利案號6,706,256。在各種具體實例中, 27 201041599 一或多種表面活性劑係以範圍0.001%至5%或〇5%至25 %存在於本發明口腔用組成物中。 · 用於口腔用組成物之視情況增稠劑包含天然及合成 及膠體,例如鹿角菜膠(愛爾蘭紅藻)、三仙膠、羧; 維素鈉、澱粉、聚乙烯基吡咯_、羥乙基丙基纖維素、ς丁 基曱基纖維素、羥丙基甲基纖維素、及羥乙基纖維素。I各 種具體實例中,增稠劑係以用量〇1至1〇重量%或〇 5至4 重量%存在於牙粉組成物中。 用於製備牙粉組成物之口腔可接受的牙粉載劑媒、夜 (carriervehicle)視情況包括保濕劑。保濕劑可為甘油、'山 梨醇、及木糖醇、分子量範圍為2〇〇至ι,0〇〇之丙二醇戋 其他保濕劑及其混合物。保濕劑濃度典型地合計為5至^ 重量%的口腔用組成物。水典型存在量為至少丨〇重量% 0 且通常為25至70重量%的口腔用組成物。 里〇’ 合成陰離子直線聚羧酸酯為功效增進劑,其視情況用於 具有若干活性成分(包含抗g劑、抗牙石劑或其他活性劑於 口腔用組成㈣)的口腔肋成物。該_子聚紐醋通常 係呈其等自減、或部分或完全巾和的水溶性鹼金屬(如卸 及較好為鈉)或銨鹽形式使用。術語「合成」及「直線排 除包括羧曱基纖維素及纖維素與天然膠的其他衍生物^已 知增稠劑或膠化劑,也不是由於交聯而具有減少溶之卡 波莫 (carbopol)。 車父好共聚物為1 : 4至4 : 1順丁稀二酐或酸與另一可聚 合乙烯系不飽和單體之共聚物,較好為具有分子量(mW ) 28 201041599 30,000至1,〇〇〇,〇〇〇之曱基乙烯基醚(甲氧基乙烯)。一種 有用共^^物為甲基乙稀基喊/順丁稀'二奸。此等共聚物實例 從ISP Corporation以商品名GANTREZ®可得。當存在時, 陰離子聚羧酸酯係以有效達到任何抗菌劑、抗牙石劑或其他 活性劑於牙粉組成物内之想要增強功效用量使用。在各種具 體實例中,口腔用組成物中所含之合成陰離子聚羧酸酯係以 0.001至5%或0.1至2.0%的口腔用組成物存在。 Q 製得本發明口腔用組成物可藉由技藝中已知之任何方 法組合成分以製造口腔用護理組成物。可使用之方法實例係 提出於如Martin等人之美國專利案號6,4〇3,〇59; clinical Pharmacology for Dental Professionals ( Mosby-Year Book,The money of the present invention may also include _#丨, such as preventing the shark from being hardened when exposed to the gas. A number of guarantees can also be expected to have a sweet flavor. The _wet agent is mainly used as a specific weight% to 7 〇% by weight or in another embodiment, %% by weight and 65 % by weight of the tooth powder composition. Suitable for containment of food polyols such as glycerin, sorbitol, wood propylene, propylene glycol and other polyols and mixtures of such sterility agents. A mixture of glycerin and mountain (iv) may be used as a humectant component of the toothpaste composition herein in a number of specific examples. The compositions of the present invention may also comprise - or a plurality of antimicrobial agents. Antibacterial agents are known in the art and include phytonic acid, sodium benzylate, potassium citrate, boric acid, and phenolic compounds such as betanaphthol, clariparin, thyme, scented brain, barley, Fragrant buds, menthol, age, pentance, hexidine, hexamethylene hexafluoride, chlorinated lauryl, chlorinated nutmeg-based bite, green tea-based pyridin. Bismuth, gasified cetyl pyridine, cetyl bromide, and halogenated diphenyl hydrazine (eg, trigas). The compositions of the present invention may also comprise one or more test amine acids such as arginine in the form of a free base or salt. The reagent may be added in an effective amount such as 丨% by weight to 2% by weight (based on the total weight of the composition 23 201041599). The composition of the present invention may be combined with potassium mono- or potassium polyphosphate, potassium hydrogencarbonate, chlorination reagents such as potassium salts such as cloves; pin salt; salt; chloride salt and potassium oxalate, · pepper test; The reagent is added in an effective amount such as i by weight, and the reagent may be added depending on the weight. The invention relates to the composition of the present invention. The composition of the present invention can also be used for treating the composition of the present invention, and can also include the composition known in the art. It is suitable for whitening and bleaching. The material contains peroxidation i = salt, over-salt. Weed contains four compounds and peroxides of organic soil, organic peroxy compounds, peroxyacid wind and their mixtures. The product contains peroxygen, peroxidation, sodium peroxide, magnesium peroxide, peroxide dance, barium peroxide, and potted characters. Other peroxides contain perborate, urea peroxide, and potted characters. Suitable metal chlorites may include chlorite dance, bismuth chlorite, sulphur acid acid, sulphuric acid clock, chlorous acid, and potassium sulfite. The reagent may be in an effective amount depending on the reagent selected. Adding, for example, from 1% by weight to 20% by weight based on the total weight of the composition. In addition to the above ingredients, the specific examples of the present invention may contain a plurality of variable dental powders as described below. The optional ingredients include, for example, but not limited to, ) Wei agent, soaping agent, flavoring agent Sweeteners, additional anti-plaque agents, abrasives, and colorants. This and other optional ingredients are further described in U.S. Patent No. 5,004,597 to Maj eti, US Patent No. 3,959,458 to Agricola et al., and Haefele. U.S. Patent No. 3,937,8, 7. 24 201041599 The choice of abrasive for the oral composition can be interpreted as pure type, fine product (particle size), particle size distribution and abrasive dosage to ensure that the tooth enamel is positive. ^ Cannot be excessively wiped off during use of the composition 'but fully cleansed and/or polished. In the context of oral care, the efficacy of the abrasive can be expressed according to the cleanliness or wear criteria of the tooth powder' ie the thin and difficult ratio (PCR) Or radioactive dentin wear (RDA). Methods of performing PCR and RDA are known in the art, as described in U.S. Patent Nos. 5,939,051 and 6,290,933. In several specific examples, the composition is safe for humans or other animals in the oral cavity. Any of the oral or cosmetically acceptable abrasives that meet the above requirements can be selected for use in the oral compositions. Additional abrasives can also be included in the compositions of the present invention. Containing aluminum oxide (calcined emulsified imitation), Shixiazao soil, pumice stone, sauerkraut 'cuttieb〇ne', insoluble acid salt, composite resin (such as melamine resin, bismuth resin, and urea _ 曱Aldehyde resin), polycarbonate, boron carbide, microcrystalline wax, microcrystalline cellulose (including a combination of colloidal microcrystalline cellulose and carboxymethyl cellulose), and combinations and derivatives thereof. In the insoluble phosphate, Useful abrasives are orthophosphate, polymetaphosphate and pyrophosphate. Examples are dicalcium phosphate dihydrate, diammonium dihydrate dihydrate, calcium hydrogen phosphate, calcium pyrophosphate, beta-calcium pyrophosphate, tricalcium phosphate, Metaphosphoric acid, potassium metabolite, and sodium metaphosphate. In several embodiments, the oral composition is in the form of a dentifrice and the exemplary carrier is substantially semi-solid or solid. The carrier can be aqueous, that is, including from 5% to 95% water. In other embodiments, the carrier is substantially non-aqueous. Carriers include, for example, oral active ingredients, surfactants (e.g., surfactants, emulsifiers, and suds modifiers), viscosity modifiers and thickening 25 201041599 agents, humectants, diluents, fillers, additional pH modifiers, colorants, preservatives, solvents, and combinations thereof. It is to be understood that although the general attributes of the various materials of the above categories may vary, there may be a number of common attributes and any given material may be supplied for multiple purposes within two or more of that type of material. As will be appreciated by those skilled in the art, in addition to the materials previously described, the oral compositions will optionally contain other materials including, for example, softeners, emollients, mouthfethes, and the like. Examples of a suitable carrier for the composition of the oral cavity are discussed in U.S. Patent No. 6,669,929 to Boyd et al., U.S. Patent No. 6,379,654 to Gebreselassie et al., and U.S. Patent No. 4,894,220 to Nabi et al. The oral composition optionally includes one or more anti-stone compositions as described in U.S. Patent No. 5,292,526 to Gaffar et al. In various embodiments, the anti-calculus composition comprises one or more polyphosphates. The anti-calculus composition may comprise at least one alkali metal or ammonium tripolylate or hexametaphosphate which is wholly or partially neutralized in the oral composition in an amount effective to resist stone. The anticalculus active may also comprise at least one water soluble, linear, molecularly dehydrated polyphosphate salt in an amount effective to resist stones. The anticalculus active may also comprise a mixture of potassium and sodium salts, at least one of which is present as a polyphosphate anticalculus in the presence of an effective anticalculus. The anticalculus active agent may also contain a linear molecular dehydrated polyphosphate anticalculus agent in the presence of an effective anti-stone amount in the presence of a mixture of sodium and potassium salts. The ratio of potassium to sodium in the composition can be as high as less than 3:1. The polyphosphate may be present in the oral composition in various amounts, for example, in a weight ratio ranging from polyphosphate ion to antibacterial agent in a range from more than 0.72:1 to less than 4:1' or an antibacterial enhancer and polyphosphoric acid. The weight ratio of the root ion ranges from 1:6 to 2.7: 1, or the weight of the antimicrobial enhancer to the polyphosphate 26 201041599 The ratio of the ratio ranges from 1:6 to 2.7··1. Other useful anticalculus agents include polyglycol polymers and polyvinyl methyl/simene (PVM/μα) copolymers such as GANTREZ®. Another active agent useful in the dentifrice composition of the present invention is an antibacterial agent which may be present in an amount of from 0.001 to 3.0% by weight of the oral composition. A non-limiting form of useful oral oral care compound comprising a nonionic antimicrobial comprising phenol and a bisphenol compound such as a halogenated diphenyl ether comprising triclosan (24 4, _ trichloro-2'-jing- Diphenyl test), triclocarban (3 4 4_ two gas average · one gland '3,4,4_tricliloroC3Tb3iiili<le), and 2 · oxo _ ethanol, benzyl ester, and two Carbanilide. The dentated diphenyl ether (e.g., trigas) can be present, for example, in an amount of 0.3% by weight of the oral composition. Suitable for surfactants that are reasonably stable throughout a wide pH range. Such compounds are well known in the art and include non-soap anions (such as sodium lauryl sulfate (SLS), N-carnitine and N-palmitoyl sarcosine), nonionic (eg, polysorbate) Polysorbate 20 (polyoxyethylene 20 sorbitan monolaurate 'TWEEN820) and polysorbate 80 (polyoxyethylene 2 sorbitan monooleate 'TWEEN® 80 ), P〇l〇 Xamer 407, available from BASF Corporation under the trade name PLURONIC® FI27), cationic, zwitterionic (eg cocoamidopropyl beet and lauryl propyl beet) and amphoteric organic synthetic cleaners. Examples of suitable surfactants for use in oral compositions are discussed in, for example, U.S. Patent No. 4,894,220 to Nabi et al., U.S. Patent No. 6,555,094 to Glandorf et al., and U.S. Patent No. 6,706,256 to Lawlor et al. In various embodiments, 27 201041599 one or more surfactants are present in the oral compositions of the present invention in a range of from 0.001% to 5% or from 5% to 25%. · As the case for oral compositions, thickeners include natural and synthetic and colloidal substances, such as carrageenan (Irish red algae), Sanxian gum, carboxy; sodium vegan, starch, polyvinylpyrrole _, hydroxyethyl Propyl propyl cellulose, butyl butyl fluorenyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose. In each of the specific examples, the thickener is present in the dentifrice composition in an amount of from 1 to 1% by weight or from 5 to 4% by weight. The orally acceptable dental powder carrier medium for the preparation of the dentifrice composition, the carrier vehicle, optionally includes a humectant. The humectant may be glycerin, 'sorbitol, and xylitol, propylene glycol having a molecular weight ranging from 2 Å to 0,0 戋, other humectants, and mixtures thereof. The humectant concentration typically amounts to 5 to 2% by weight of the oral composition. Water is typically present in an amount of at least 丨〇% by weight and typically from 25 to 70% by weight of the oral composition. 〇 〇 synthetic anionic linear polycarboxylates are efficacy enhancers, which are optionally used as oral ribs having several active ingredients (including anti-g agents, anti-calculus agents or other active agents in oral compositions (4)). The merging vinegar is usually used in the form of a water-soluble alkali metal (e.g., preferably sodium) or an ammonium salt which is self-reducing, or partially or completely. The terms "synthesis" and "straight line exclusion include carboxymethyl cellulose and other derivatives of cellulose and natural gums ^ known thickeners or gelling agents, nor are they due to cross-linking to reduce the solubility of carbopol (carbopol) The good copolymer of the car is 1:4 to 4: 1 cis butyl dianhydride or a copolymer of an acid and another polymerizable ethylenically unsaturated monomer, preferably having a molecular weight (mW) 28 201041599 30,000 to 1 , 〇〇〇, 〇〇〇 曱 乙烯基 vinyl ether (methoxy ethene). A useful conjugate is methyl ethyl ketone / butyl butyl sinensis. Examples of such copolymers from ISP Corporation Available under the trade name GANTREZ®. When present, anionic polycarboxylates are used in an amount effective to achieve the desired efficacy of any antibacterial, anticalculus or other active agent in the dentifrice composition. In various embodiments The synthetic anionic polycarboxylate contained in the oral composition is present in an oral composition of 0.001 to 5% or 0.1 to 2.0%. Q The oral composition of the present invention can be obtained by any of the techniques known in the art. Methods The components are combined to produce an oral care composition. The method of using the system proposed in the Example as described in Martin et al.'S U.S. Patent Nos 6,4〇3, 〇59; clinical Pharmacology for Dental Professionals (Mosby-Year Book,

Inc.,第 3 版 1989),Mosby’s Dental Hygiene: Concepts,Cases and Competencies (Daniel,S·及 Harfst, S. eds.,Elsevier Science Health Science Div· 2002);及 Ernest W. Flick, Cosmetic and Toiletry Formulations,第 2 版。 ◎ 本發明提供一種使用本發明口腔用組成物以潔淨及/或 磨光口腔表面之方法及過程。另外,口腔用組成物視情況治 療及抑制口腔症狀,例如口腔炎性症狀、牙齒菌斑、及牙結 石口腔用組成物可以技藝中已知之任何適合方式塗敷於患 者;例如藉由使用適合塗敷器或傳遞裝置,例如刷子、牙條、 膜’主射裔、線帶、藥丸、或技藝中已知之任何其他塗敷器 或傳遞衣置’將σ腔用組成物導人患者口腔。組成物可用於 預防方法及過程以促進及維持口腔健康、外觀、維持全身健 康等。口腔用組成物可根據特別治療計晝表重複土 也塗敷於患 29 201041599 治療及/或抑制污跡、齒菌斑、結石或牙石 痛製備:貯:表之操作指南可提供產品於商業包装’ 理論料下,據信祕本發明口_組成物 一 具有最初平均粒徑。當本發明口腔用袓成物 被用於刷淨軟組織時,如以移除齒菌斑或薄膜,二氧化石夕磨 料足夠,如牙齒表面移除該軟_。從而,口腔用組成物最 初具有同PCR。然而,當二氧化發磨料顆粒對硬牙齒表面(如 齒質或法瑯質)接觸時,其等斷裂成更小顆粒;由此導致低 RDA。因此,當本發明組成物用於治療口腔時,軟組織已被 剝離:且防止硬組織免於磨損。據信#組成物用於口時,由 於二氧化矽磨料尺寸減小,PCR及/或RDA可隨時間減少兩 者數值。 起因於與硬表面接觸之所得破碎二氧化矽顆粒亦給予 額外想不到的優勢;亦即磨光牙齒表面及/或阻塞牙齒小管 (dental tubule)之能力,導致更乾淨牙齒及/或減少牙齒敏感 性。因此,本發明組成物導致改良的潔淨、磨光、及減少牙 齒敏感性。 本發明透過下列非限定實施例予以進一步說明。 【實施方式】 實施例1 二氧化矽A及二氧化矽B之特徵係如下決定。二氧化 發 A 為 Grace VP5。二氧化梦 B 為來自 J.M. Huber( Havre de Grace,Maryland,USA)之 ZEODENT® 105 〇 30 201041599 用於Einhlemer 〇式驗之條件係使 化石夕於麵mL之120分鐘174_ 万去測1。測量係呈現於表1。 匕石夕A 吸油量(cc/1 OOg ) ^Al〇〇 平均粒徑(μηι) 9至13 di〇 ( μηι) * '------- 2.74 黃銅Einlehner硬度 ------ 6至9 ------- 二氧化矽 50 至 65 8至12 2.58 12 至 18 Ο 小於‘值之尺寸。 一叫指出職顆粒具有 …=去離子水以二氧切AAB製備萬w/w聚液。 敢初漿液之粒徑分布仙_喻2_ _分析制Hydr〇 2_S小體積自動樣品分散單元決定。將漿液於測量前在水 浴中以聲波振祕理i分鐘叹裂任何大师物。使用平台 Ο 20ml (sidewal〇 7〇〇 量W x 3%”之紹槽。使軟式方頭硬毛刷(頭尺寸大約長x寬 為2.8cmx l.〇cm)架置以沿著整個崔呂槽基座移動。添加重量 於刷頭月口P (250克)以於刷淨期間製造正向力。刷淨機器 以速率為每分鐘100加倍行程運轉沿著鋁表面達總計3〇〇行 程。刷淨後’使漿液從槽基底移除並以聲波振動處理丨分鐘。 樣品裝載入Malvern 2000粒徑分析儀。然後決定二氧化矽磨 料粒徑’並呈現於表2。 表2 31Inc., 3rd edition 1989), Mosby's Dental Hygiene: Concepts, Cases and Competencies (Daniel, S. and Harfst, S. eds., Elsevier Science Health Science Div. 2002); and Ernest W. Flick, Cosmetic and Toiletry Formulations ,Version 2. ◎ The present invention provides a method and process for using the oral compositions of the present invention to clean and/or polish the oral surface. Further, the oral composition can be treated and inhibited as appropriate, for example, stomatous symptoms, dental plaque, and dental calculus oral compositions can be applied to the patient in any suitable manner known in the art; for example, by using a suitable coating The applicator or delivery device, such as a brush, a toothed strip, a membrane 'main shooter, a tape, a pill, or any other applicator or transfer garment known in the art', guides the sigma cavity composition to the patient's mouth. The composition can be used in preventive methods and procedures to promote and maintain oral health, appearance, and overall health. The oral composition can be applied to the patient according to the special treatment schedule. The soil is also applied to the patient. 29 201041599 Treatment and / or inhibition of stains, plaque, stones or calculus pain preparation: Storage: Table of operating instructions can provide products in commercial packaging Under the theory, it is believed that the composition of the invention has an initial average particle size. When the oral composition of the present invention is used for brushing soft tissues, such as to remove plaque or film, the silica stone is sufficient, such as removing the soft surface from the tooth surface. Thus, the oral composition initially has the same PCR. However, when the oxidized abrasive particles contact the hard tooth surface (e.g., dentine or enamel), they break into smaller particles; thereby resulting in a low RDA. Therefore, when the composition of the present invention is used for treating the oral cavity, the soft tissue has been peeled off: and the hard tissue is prevented from being worn. It is believed that when the composition is used in the mouth, PCR and/or RDA can reduce both values over time due to the reduced size of the cerium oxide abrasive. The resulting broken ceria particles resulting from contact with a hard surface also give an unexpected advantage; that is, the ability to polish the surface of the tooth and/or block the dental tubule, resulting in cleaner teeth and/or reduced tooth sensitivity. . Thus, the compositions of the present invention result in improved cleansing, polishing, and reduced tooth sensitivity. The invention is further illustrated by the following non-limiting examples. [Embodiment] Example 1 The characteristics of cerium oxide A and cerium oxide B are determined as follows. The oxidation of A is Grace VP5. The dream of oxidizing B is ZEODENT® 105 J 30 201041599 from J.M. Huber (Havre de Grace, Maryland, USA). The conditions for the Einhlemer test are to make the fossils in the face of mL for 120 minutes. The measurement system is presented in Table 1.匕石夕 A Oil absorption (cc/1 OOg ) ^Al〇〇 average particle size (μηι) 9 to 13 di〇( μηι) * '------- 2.74 Brass Einlehner hardness ------ 6 to 9 ------- Ceria 50 to 65 8 to 12 2.58 12 to 18 Ο Less than the size of the value. One called the granules with ... = deionized water to prepare 10,000 w / w polyliquid with dioxobic AAB. The particle size distribution of the dare slurry is determined as follows: _ analysis Hydr 〇 2_S small volume automatic sample dispersion unit. The slurry was spun in the water bath for 1 minute before the measurement, and any master was smashed. Use the platform Ο 20ml (sidewal〇7〇〇W x 3%) to make the soft square head bristle brush (head size about length x width 2.8cmx l.〇cm) mounted along the whole Cui Lu The trough base is moved. The weight is added to the head of the brush head P (250 g) to create a positive force during the brushing process. The brushing machine runs at a rate of 100 doublings per minute along the aluminum surface for a total of 3 strokes. After brushing, the slurry was removed from the cell substrate and sonicated for 15 minutes. The sample was loaded into a Malvern 2000 particle size analyzer. The cerium oxide abrasive particle size was then determined and presented in Table 2. Table 2 31

合禋二氣化矽A將十 前敘述之方法决定。广液之PCR及RDA值係藉由本文先 氧化矽漿液,以=复严備10%、15%、20%及30%w/w二 之方法決定。沾其等PCR及RDA值係藉由本文先前敘述 、、、Q果呈現於表3。The combination of the two gasification 矽A will be determined by the method described in the previous ten. The PCR and RDA values of the wide liquid were determined by the method of first cerium oxide slurry, 10%, 15%, 20% and 30% w/w. The PCR and RDA values are shown in Table 3 by the previous descriptions of this article.

PCR RDAPCR RDA

實施例3Example 3

PCR/RDAPCR/RDA

15%VP5 20%VP5 30%VP5 76 84 86 95 93 112 0.80 0.90 0.7715% VP5 20% VP5 30% VP5 76 84 86 95 93 112 0.80 0.90 0.77

根據表4製備牙粉纟域物,如牙膏。According to Table 4, a dentifrice region such as a toothpaste was prepared.

32 201041599 水 29 29 37.1 37.1 PEG 3 3 SLS 1.5 1.5 1.5 1.5 纖維素膠 0.6 0.6 0.8 0.8 焦磷酸鈉 0.5 0.5 挪油酸胺基丙基甜采驗 0.4 0.4 三氣沙 0.3 0.3 硫酸鈉 0.3 0.3 0.1 0.1 甘油 19.9 19.9 二氧化鈦 0.1 0.1 氟化納 一— 0.2 0.2 0.3 0.3 PVMA/MA共聚物 2 2 鹿角菜膠 0.3 0.3 __調味料及著色劑 ----- 1.5 1.5 2.1 2.1 實施例432 201041599 Water 29 29 37.1 37.1 PEG 3 3 SLS 1.5 1.5 1.5 1.5 Cellulose gum 0.6 0.6 0.8 0.8 Sodium pyrophosphate 0.5 0.5 Norty acid aminopropyl sweet test 0.4 0.4 Tri-gas 0.3 0.3 Sodium sulfate 0.3 0.3 0.1 0.1 Glycerin 19.9 19.9 Titanium Dioxide 0.1 0.1 Fluoride Nano-0.2 0.2 0.3 0.3 PVMA/MA Copolymer 2 2 Carrageenan 0.3 0.3 __Seasoning and Coloring Agent----- 1.5 1.5 2.1 2.1 Example 4

❹ 對罹患牙齒敏感性之兩組30人給予牙膏MF-A或 MF-B,並指示根據其等正常刷牙習慣使用組成物作為其等 唯一牙粉一個月。一個月結束後,以MF_A刷牙之75%人報 告減少牙齒敏感性,以及以MF_B刷牙之1〇%人報告減少牙 齒敏感性。一個月結束後,以MF-A刷牙之3%人報告增加 牙齒敏感性,以及以MF_B刷牙之15%人報告增加牙齒敏感 性。 〜 貫施例5 對兩組50人給予牙膏WD_A或wd_B,並指示根據其 33 201041599 等正常刷牙習慣使用組成物作為其等唯一牙粉一個月。以 WD-Α刷牙之80%人報告其等觀察到美白/磨光效果,而以 WD-B刷牙之5%人報告其等觀察到美白/磨光效果。 實施例6 對兩組15位吸煙者(平均每日1.4包)給予牙膏MF_A 或MF-B,並指示根據其等正常刷牙習慣使用組成物作為其 等唯一牙粉。一個月結束後,以MF-A刷牙之85%人察覺其 等牙齒污跡減少,以及以MF-B刷牙之12%人察覺其等牙齒 污跡減少。 實施例7 包括20%二氧化矽A及20%二氧化矽B的兩種組成物 之RDA及PCR值係藉由本文先前敘述之方法決定。除不同 二氧化矽磨料外,兩種組成物實質上相同。結果呈現於表5。 表5 卜20%二氧化矽a 20% 二氧:〜 RDA 112 207 PCR 93 ~~~—^ 103 PCR/RDA 0.83 —-~~~ 0.5 【圖式簡單說明】 無 【主要元件符號說明】 無 34给予 Give toothpaste MF-A or MF-B to two groups of 30 people who are sensitive to teeth, and instruct them to use the composition as their sole tooth powder for one month according to their normal brushing habits. At the end of the month, 75% of people brushed with MF_A reported reduced tooth sensitivity, and 1% of people brushed with MF_B reported reduced tooth sensitivity. At the end of the month, 3% of people brushed with MF-A reported increased tooth sensitivity, and 15% of people brushed with MF_B reported increased tooth sensitivity. ~ Example 5 For two groups of 50 people, toothpaste WD_A or wd_B was given, and the composition was used as its sole tooth powder for one month according to the normal brushing habits such as 33 201041599. 80% of people who brushed their teeth with WD-Α reported that they observed a whitening/buffing effect, while 5% of people who brushed their teeth with WD-B reported that they observed a whitening/buffing effect. Example 6 To two groups of 15 smokers (average 1.4 packs per day), toothpaste MF_A or MF-B was administered, and the composition was used as its sole tooth powder according to its normal brushing habit. At the end of the month, 85% of people who brushed their teeth with MF-A noticed a decrease in their stains, and 12% of those who brushed their teeth with MF-B noticed a decrease in their stains. Example 7 The RDA and PCR values of two compositions comprising 20% cerium oxide A and 20% cerium oxide B were determined by the methods previously described herein. The two compositions are essentially identical except for the different cerium oxide abrasives. The results are presented in Table 5. Table 5 Bu 20% cerium oxide a 20% Dioxane: ~ RDA 112 207 PCR 93 ~~~-^ 103 PCR/RDA 0.83 —-~~~ 0.5 [Simple diagram description] No [Main component symbol description] None 34

Claims (1)

201041599 七、申請專利範圍: 1. 一種口腔用組成物,其包括口腔可接受的載剤及二氧化石夕 磨料,該二氧化矽磨料包括一具有5μιη至20μιη的平均粒 徑、及4至11的Einlehner硬度之二氧化梦化合物。 2. 如申請專利範圍第1項之組成物,其中該二氧化石夕磨料具 有8μιη至11 μηι的平均粒徑。 Ο201041599 VII. Patent Application Range: 1. An oral composition comprising an orally acceptable ruthenium-doped and cerium oxide abrasive comprising an average particle size of from 5 μm to 20 μm and from 4 to 11 The Einlehner Hardness Dioxide Dream Compound. 2. The composition of claim 1, wherein the silica stone has an average particle size of from 8 μm to 11 μm. Ο 3. 如申請專利範圍第丨或2項之組成物,其中該二氧化矽磨 料具有60cc/100g至I20cc/100g的吸油量。 4. 如前述申請專利範圍中任一項之組成物,其中該二氧化矽 磨料於174,000迴轉下具有5至1〇的黃銅mniehner硬度。 5·如前述申請專利範圍中任一項之組成物,其具有至 的薄膜潔淨比率。 6.如前述申請專利範财任—項之組成物,其具有小於⑼ 的放射性齒質磨損。 7·如前述申請專利範圍中任—項之組成物 的PCR/RDA比率。 、名Μ至1.5 8. 如前述f請專利_中任—項之_物, 磨料係1重量%至95重量%的組成物。&quot;-乳化石夕 9. 如前述巾請專利範圍中任_項之组成物, 磨料具有山0為2.5μιη^ 29um 八中該二乳化矽 1〇.如前述巾請專利範圍中任—μ^域物^ 成物塗敷於口腔中之硬表面時,# 中當口腔用組 11.如前述巾請專利_中任發磨料破碎。 為2.3μ】 至 用組成物時,該二氧切磨料麵成H中在Π腔中使 35 201041599 2.6μπι之顆粒。 12. 如前述申請專利範圍中任一項之組成物,其中該口腔用組 成物係於牙齒上刷淨如至少3〇秒至5分鐘。 、 13. 如前述中請專利範圍中任—項之级成物,其中塗敷於口腔 中之硬表面後,該二氧化矽磨料之平均粒徑減少16%至如 % 0 14. 如前述申請專利範圍中任一項之組成物,其中塗敷於口腔 中之硬表面後,該二氧化矽磨料之di〇減少9%至12%。二 15. 、如前述中請專利範圍中任—項之組成物,包括氟化物離子 源’其包括選自氟化錫(II)、氟化鈉、氟化鉀、單氟磷酸 鈉、氟矽酸鈉、氟矽酸銨、氟化胺、氟化胺氟化銨、及其 組合之氟化物鹽。 ' 16. 如前述申請專利範圍中任一項之組成物,其包括至少—種 選自月桂基硫酸鈉、椰油醯胺基丙基甜菜鹼、及其組合之 界面活性劑。 17_如前述申請專利範圍中任一項之組成物,其包括至少—種 選自甘油、山梨醇及其組合之保濕劑。 18. 如前述申請專利範圍中任一項之組成物,其包括至少一種 選自聚乙二醇、聚乙烯基甲基醚順丁稀二酸共聚物、多醣 類、及其組合之聚合物。 19. 如前述申請專利範圍中任一項之組成物,其包括選自經鹵 化的二苯基域、草本萃取物或精油、雙胍防腐劑、四級錢 化合物 '紛類防腐劑、海克西定(hexetidine )、聚維顯I蛾 (povidone iodine)、地莫前列素(delmopinol)、salifluor、 36 201041599 金屬離子、血根驗、蜂巢躐膠、及氧化劑㈣弘⑽—a㈣) 之抗菌劑。 20. 如刖述申請專利範圍中任一項之組成物,其包括牙齒減敏 劑。 21. 如前述中請專利範圍中任—項之組成物,其包括牙齒美白 化合物。 22. 如前述申請專利範圍中任一項之組成物,其係牙膏或凝 膠。 23. 如則述申請專利範圍中任一項之組成物,其係藉由一包括 將1至5ml 口腔用組成物漿液塗敷於1至1〇cm2表面;使 表面對P放射的牙齒接觸;於2至5牛頓的恆定力刷淨牙 齒表面300行程,其中各行程造成表面對牙齒移動丨至 l〇cm2 ;及測量RDA值之方法。 24. 如前述申請專利範圍中任一項之組成物,其中在口腔中使 用5秒的口腔用組成物之RDA為1.2至1.6倍在口腔中使 用1至5分鐘的相同組成物之RDA。 25. 如前述申請專利範圍中任一項之組成物,其中Einlehner 硬度係母174,〇〇〇迴轉以黃銅網測量。 26. 如申請專利範圍第1至25項中任一項之組成物,其中 Einlehner硬度係每ι〇〇,〇〇〇迴轉以黃銅網測量。 27. 如前述申請專利範圍中任一項之組成物,其中由二氧化石夕 磨料組成之10%水性漿液具有PCR為65至80。 28·如前述申請專利範圍中任一項之組成物,其中由二氧化矽 磨料組成之10%水性漿液具有RDA為75至91。 37 201041599 29. 如月ί述申s月專利|&amp;圍中任—項之組成物,其中由二氧化石夕 磨料組成之ίο%水性榮液具有PCR/RDA比率為〇7至〇9。 30. -種口朗組祕’包括口腔可接受的麵及二氧化石夕磨 料,該二氧化石夕磨料包括具有選自由8μιη至11μιη、9哗 至13μιη、8μπι至12μηι、及8μηι至11μιη組成組群的中數 粒徑、及4至11的Einlehner硬度之二氧化矽化合物。 31. 如申請專利範圍第1至12中項任一項之組成物,其中塗 敷於口腔中之硬表面後,该一氧化石夕磨料之中數粒徑減少 16% 至 20%。 :彳 32. —種改良口腔健康之方法,其包括將有效量的申請專利範 圍第1至22項中任一項之口腔用組成物塗敷於其有需求病 患之口腔。 38 201041599 四、指定代表圖: (一) 本案指定代表圖為:第(無)圖。 (二) 本代表圖之元件符號簡單說明: 無 五、本案若有化學式時,請揭示最能顯示發明特徵的化學式: 無3. The composition of claim 2 or 2, wherein the cerium oxide abrasive has an oil absorption of from 60 cc/100 g to I20 cc/100 g. 4. The composition of any of the preceding claims, wherein the cerium oxide abrasive has a brass mniehner hardness of 5 to 1 Torr at 174,000 revolutions. A composition according to any one of the preceding claims, which has a film clean ratio of . 6. The composition of any of the preceding claims, which has a radioactive tooth wear of less than (9). 7. The PCR/RDA ratio of the composition of any of the preceding claims. </ RTI> </ RTI> </ RTI> <RTIgt; </ RTI> <RTIgt; </ RTI> <RTIgt; </ RTI> <RTIgt; &quot;-Emulsified Shixi 9. As the above-mentioned towel, please consult the composition of any of the patent scope, the abrasive has a mountain of 0 is 2.5μιη^ 29um, and the second emulsion is 〇1〇. ^ Domain material ^ When the product is applied to the hard surface of the oral cavity, #中中的用用组11. When the composition is used, the dimethyl die-cut surface is made into particles of H 2010 in the cavity of 2010 35 35 201041599 2.6 μπι. 12. The composition of any of the preceding claims, wherein the oral composition is brushed on the teeth for at least 3 seconds to 5 minutes. 13. The composition of any of the preceding claims, wherein after application to a hard surface in the oral cavity, the average particle size of the cerium oxide abrasive is reduced by 16% to, for example, % 0. 14. A composition according to any one of the preceding claims, wherein the cerium oxide abrasive has a di 〇 reduction of 9% to 12% after application to a hard surface in the oral cavity. 2. The composition of any of the preceding claims, including a fluoride ion source comprising: selected from the group consisting of tin (II) fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, and fluoroquinone Sodium fluoride, ammonium fluoroantimonate, amine fluoride, ammonium fluoride fluoride, and combinations thereof. 16. The composition of any of the preceding claims, comprising at least one surfactant selected from the group consisting of sodium lauryl sulfate, cocoamidopropyl betaine, and combinations thereof. A composition according to any one of the preceding claims, which comprises at least one humectant selected from the group consisting of glycerin, sorbitol and combinations thereof. 18. The composition of any of the preceding claims, comprising at least one polymer selected from the group consisting of polyethylene glycol, polyvinyl methyl ether butyl butyric acid copolymer, polysaccharides, and combinations thereof . The composition according to any one of the preceding claims, which comprises a diphenyl domain selected from halogenated, an herbal extract or an essential oil, a biguanide preservative, a quaternary compound, a variegated preservative, Haeksi An antibacterial agent for hexetidine, povidone iodine, delmopinol, salifluor, 36 201041599 metal ion, blood root test, honeycomb gelatin, and oxidant (4) Hong (10)-a (4). 20. A composition according to any one of the claims, which comprises a tooth desensitizer. 21. A composition according to any of the preceding claims, which comprises a tooth whitening compound. A composition according to any one of the preceding claims, which is a toothpaste or a gel. 23. The composition according to any one of the preceding claims, which comprises applying a slurry of 1 to 5 ml of the oral composition onto a surface of 1 to 1 cm 2 ; contacting the surface with teeth irradiated by P; The tooth surface is brushed for 300 strokes at a constant force of 2 to 5 Newtons, wherein each stroke causes the surface to move to the tooth to 〇cm2; and the method of measuring the RDA value. 24. The composition of any of the preceding claims, wherein the RDA of the oral composition for 5 seconds in the oral cavity is 1.2 to 1.6 times the RDA of the same composition for 1 to 5 minutes in the oral cavity. 25. The composition of any of the preceding claims, wherein the Einlehner hardness is 174 and the turns are measured on a brass mesh. 26. The composition of any one of claims 1 to 25, wherein the Einlehner hardness is measured by a brass mesh per ι〇〇. 27. The composition of any of the preceding claims, wherein the 10% aqueous slurry consisting of the cerium oxide abrasive has a PCR of from 65 to 80. The composition of any of the preceding claims, wherein the 10% aqueous slurry consisting of cerium oxide abrasive has an RDA of from 75 to 91. 37 201041599 29. The composition of the monthly patents, which consists of the sulphur dioxide and the RDA, has a PCR/RDA ratio of 〇7 to 〇9. 30. - The genus of the genus - includes an orally acceptable surface and a cerium dioxide cerium abrasive, the cerium dioxide cerium abrasive comprising a composition selected from the group consisting of 8 μm to 11 μm, 9 to 13 μm, 8 μm to 12 μm, and 8 μm to 11 μm The median particle size of the group, and the Einlehner hardness of the cerium oxide compound of 4 to 11. The composition according to any one of claims 1 to 12, wherein the number of particles in the nitric oxide cerium abrasive is reduced by 16% to 20% after being applied to a hard surface in the oral cavity. A method for improving oral health, which comprises applying an effective amount of the oral composition of any one of claims 1 to 22 to an oral cavity of a patient in need thereof. 38 201041599 IV. Designation of representative drawings: (1) The representative representative of the case is: (No). (2) A brief description of the symbol of the representative figure: None 5. If there is a chemical formula in this case, please disclose the chemical formula that best shows the characteristics of the invention: None
TW098117365A 2009-05-25 2009-05-25 Oral compositions and uses thereof TWI476007B (en)

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