TWI551300B - 口腔保健組成物 - Google Patents
口腔保健組成物 Download PDFInfo
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- TWI551300B TWI551300B TW099136244A TW99136244A TWI551300B TW I551300 B TWI551300 B TW I551300B TW 099136244 A TW099136244 A TW 099136244A TW 99136244 A TW99136244 A TW 99136244A TW I551300 B TWI551300 B TW I551300B
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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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
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- A—HUMAN NECESSITIES
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- 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
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
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- 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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
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- A—HUMAN NECESSITIES
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Landscapes
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Description
本發明係關於一種口腔保健組成物以及此類口腔保健組成物於治療口臭的用途。本發明亦係關於一種用於治療或預防口臭的方法。
口臭(halitosis)係口臭(bad breath)或口臭(oral malodor)(有時被稱為Fetor ex Ore)之專有名詞的,其為一種令人不快病症。事實上,除了極年幼的每一個人通常患有口臭,其中約25%為經常性口臭以及在老年時更為頻繁和嚴重之問題。此問題幾乎平均發生於男人和女人身上。口臭導因於我們所吃的食物中的蛋白質和涶液殘渣被細菌分解所致。即使極乾淨口腔寄宿有能力分解這些口腔內的含蛋白質顆粒之細菌。具有大而粗糙表面區域之縫隙的舌頭藏有大量供應和保護許多細菌族群的食物和殘渣。在低氧條件之下,這些細菌族群形成被稱為揮發性硫化物(VSC)-例如硫化氫(臭雞蛋)和甲基硫醇(臭鼬鼠味)以及其他臭味和難吃化合物的難聞產物。口腔內高達80~90%的口臭被認為導因於此機制。
目前分析口臭的儀器以測量揮發性硫化物程度為目的。然而,用於標準口臭測定之感官評估與所測得之VSC程度之間缺乏關聯性。此導致增加對非VSC惡臭成分的興趣。減少非VSC惡臭成分提供新穎口臭處理技術之發展一種新的方法。
一種非VSC惡臭成分為短鏈羧酸,例如丁酸。另一種非VSC惡臭成分為胺,例如腐肉鹼(putrescine)、屍鹼(cadaverine)和吲哚。吲哚係臭味閥值較硫化氫為低之口臭內存在的胺類。因此,就分子的分子而言吲哚較硫化氫更具臭味。吲哚係存在色胺酸酶之下自色胺酸的分解形成。
許多文獻已揭示用於處理口臭的各種口腔保健組成物。例如,US 5738840中揭示用於減少口臭的一種口腔保健組成物,其中該組成物含有約1 ppm至約200 ppm濃度的二氧化氯分子以及約5.0至約7.5的pH。US 6159447中揭示用於控制細菌生長和繁殖的組成物,其中該組成物內含有酵素及偶合至該酵素的錨定(anchor)分子,該錨定分子能附著至接近細菌菌落的基質。
US 6723305中揭示一種用於可從口腔移除惡臭產生菌之抗菌效果之含氯化鯨蠟基吡啶鎓(cetylpyridinium chloride)和鋅離子的潄口液。US 7250162中揭示用於治療口臭的一種乳酸菌菌株。US 7297327中揭示含有控制大蒜味之瑞香酚(thymol)、大茴香、小茴香、羅勒和杜松莓(juniperberry)精油的一種口臭控制劑摻合物。US 7402416中揭示用於減少牙菌斑和口臭的一種口腔保健組成物,其含有非離子抗菌化合物和含酵素之牙劑。
US 2003/0158111中揭示含有金屬結合肽、肽衍生物和肽二聚體以減少口腔組織發炎及降低對口腔組織活性氧物種之損傷的口腔保健組成物。US 2006/0008425中揭示含有酵素和環糊精的一種口腔保健組成物。US 2008/0152600中揭示可黏附口腔表面如牙齒和牙齦的胜肽。所揭示胜肽被用於傳遞口腔保健效益劑至口腔表面。US 2008/0254079中揭示各種組成物,包括含溶菌酶、多醣和視情況絲胺酸蛋白酶的口腔保健組成物。這些文件的各種揭示藉由引述被併入於此以供參考。
此處描述已知化合物、組成物、方法和裝置的優點和缺點非擬限制具體實施例所包括或不包括其的範圍。事實上,某些具體實施例可包括一或多種已知化合物、組成物、方法或裝置的優點而不受其缺點的影響。
技術領域中需要提供一種能治療或預防口臭的改良口腔保健組成物。此外,技術領域中需要提供能治療非VSC惡臭的口腔保健組成物。
因此,第一態樣中,本發明提供一種含絲胺酸的口腔保健組成物。絲胺酸係以可有效降低硫化氫及/或吲哚所導致的口臭之含量存在於口腔保健組成物內。第二態樣中,本發明提供一種用於治療或預防口臭之含有絲胺酸的組成物。第三態樣中,本發明提供一種用於治療或預防口臭之含有絲胺酸和鋅鹽的組成物。
第四態樣中,本發明提供一種治療或預防口臭的方法,包含將含有絲胺酸的口腔保健組成物施加至口腔。絲胺酸係以可有效降低硫化氫及/或吲哚所導致的口臭之含量存在於口腔保健組成物內。該組成物除了絲胺酸之外亦含有鋅鹽。
必需瞭解本發明具體實施例的詳細說明和特殊實施例僅供說明之目的而非擬限制本發明的範圍。
在審視本發明此處說明的描述時必需考慮下列的定義和非侷限性指引。此處的標題(例如"背景"和"摘要")及次標題(例如"組成物"和"方法")僅擬用於本發明揭示內主題的一般結構,以及非擬用於限制本發明的揭示或其任何態樣。明確而言,揭示於"背景"內的標的包括本發明範圍內的技術態樣,以及並非敘述自先前的技藝。揭示於"摘要"內的標的並非全面或完全地揭示本發明全部的範圍或其任何的具體實施例。為方便之計,此專利說明書章節內材料的分類或討論具有一特定的效用(例如作為一"活性劑"或一"載劑"成分),以及根據其於此處的分類當其被用於任何已知組成物時不得因此推論該材料為必需或具有唯一的功能。
此處引證的參考文獻並非承認這些參考文獻為先前技術或與此處揭示之本發明的可專利性具有任何相關性。背景內所引證之參考文獻內容的任何討論僅擬提供該參考文獻作者所作主張的概述,而並非承認該參考文獻內容的準確性。
雖然敘述本發明之具體實施例,但是其描述和特定實施例僅擬作為說明之目以及非擬限制本發明的範圍。此外,引證之多項具體實施例中所陳述的特徵並不排除具有附加特徵的其他具體實施例,或併入所述特徵之不同組合的其他具體實施例。實施例被提供用於說明如何製造和使用本發明組成物和方法之目的以及,除非已明確申明否則非擬代表該已或未經完成或測試之本發明的給定具體實施例。
此處"較佳的"和"較佳地"一詞意指本發明的具體實施例在某些情況下可提供某些效益。然而在相同或其他情況下亦可選擇其他具體實施例。再者,當敘述一或多件較佳具體實施例時並不意味著不得利用其他的具體實施例,以及本發明的範圍並非擬排除其他的具體實施例。此外,該組成物和方法可包含、實質上由,或由此處所述的元素所組成。
全文中,使用縮寫表達在該範圍內之各個和每一個值的範圍。任何在該範圍內之值均可被選擇作為該範圍的界標。此外,藉由引述此處將引證全部完整的參考文獻。若本發明與所引述文獻的定義發生衝突時以本發明的揭示為準。
除非另有明述,否則應瞭解說明書中此處和他處表示的全部百分比和數量係指重量百分比。所示數量係根據材料的活性重量。此處所引述的特定值擬用以表示加減一定程度之差異以計入測量誤差的值。例如:10%含量可包括給予測量誤差度之9.5%或10.5%,其為熟習此項技術者所領會與了解。
用於本發明內文中之"絲胺酸"一詞指L-絲胺酸胺基酸,亦稱為(2S)-2-胺基-3-羥基丙酸。用於本發明內文中的"鋅鹽"一詞指含Zn2+之化合物,舉例如乳酸鋅、檸檬酸鋅和氯化鋅。用於本發明內文中的"錫鹽"一詞指含Sn2+之化合物,舉例如SnCl2、SnF2和焦磷酸錫。
此處所述"治療"或"處理"一詞擬包括預防。該名詞包括症狀及/或與口臭有關效應的改善、預防和消除。"避免"或"預防"一詞指事先投與本發明的組成物以阻止或緩和口臭。熟習此項技術者瞭解用於治療口臭之組成物(本方法請求項所宣稱)的"預防"一詞非為絕對名詞。而就該名詞的瞭解意指預防性地投與一組成物以消除文字涵意上的可能或嚴重症狀。
絲胺酸係一種具有分子式HO2CCH(NH)2CH2OH的天然胺基酸。由於絲胺酸的構造類似半胱胺酸(HO2CCH(NH)2CH2SH),因此被認為是一種硫胱酸脫硫氫酶(cysteine desulfhydrase)的半胱胺酸受質競爭劑(Delwiche,J. Bacteriol. 62,717~722(1951))。硫胱酸脫硫氫酶被認為與硫化氫,一種VSC,的程度增加有關。更明確而言,硫胱酸脫硫氫酶催化半胱胺酸降解成硫化氫。絲胺酸亦被認為能藉由存在色胺酸合成酶之下與形成色胺酸的吲哚反應而下調色胺酸的酶降解(Lane和Kirschner,Eur. J. Biochem.,129,571~582(1983))。
本發明者的研究目前已證明絲胺酸當與全唾液和半胱胺酸培養時可明顯降低VSC。此外,本發明者已發展出一種利用氣相層析(GC)的樣本製備法以定量絲胺酸對吲哚形成的效應。因此,目前已發現當提高加入全唾液的絲胺酸程度時,吲哚的濃度將隨之增加。
因此,目前已發現絲胺酸具有能力控制VSC和吲哚產生之雙重作用的口臭控制。
在一具體實施例中,本發明提供含有絲胺酸的一種口腔保健組成物,其中該絲胺酸係以可有效降低硫化氫所導致的口臭之用量存在。在一此類具體實施例中,口腔保健組成物之內絲胺酸係以足以藉由口腔內硫胱酸脫硫氫酶降低半胱胺酸被降解成硫化氫之用量存在。此將可降低口腔內硫化氫、VSC氣體的量。因此,降低硫化氫的量可達到治療或預防口臭的效果。
一具體實施例中,本發明提供一種含有絲胺酸的口腔保健組成物,該絲胺酸係以可有效降低導因於吲哚的口臭之用量存在。在一此類具體實施例中,口腔保健組成物之內絲胺酸係以足以於存在色胺酸合成酶之下與形成口腔內色胺酸的吲哚反應之用量存在。此將可降低口腔內吲哚的量。吲哚被認為係造成口臭的成因之一。因此,降低吲哚的量可達到治療或預防口臭的效果。
一具體實施例中,本發明提供一種含有絲胺酸的口腔保健組成物,其中絲胺酸係以可有效降低導因於硫化氫和吲哚的口臭之用量存在。在一此類具體實施例中,絲胺酸係以足以藉由口腔內硫胱酸脫硫氫酶降低半胱胺酸被降解成硫化氫之用量以及以足以於存在色胺酸合成酶之下與形成口腔內色胺酸的吲哚反應之用量存在。
一具體實施例中,本發明提供一種含有絲胺酸的口腔保健組成物,其中絲胺酸係以可有效降低導因於至少一種選自由硫化氫、吲哚及其混合物所組成之群組的成分造成的口臭之用量存在。
一具體實施例中,本發明提供一種用於治療或預防口臭之含有絲胺酸的組成物。一具體實施例中,該口臭導因於硫化氫及/或吲哚。一具體實施例中,該絲胺酸係以足以藉由口腔內硫胱酸脫硫氫酶降低半胱胺酸被降解成硫化氫之用量存在。另一具體實施例中,該絲胺酸係以足以於存在色胺酸合成酶之下與形成口腔內色胺酸的吲哚反應之用量存在。又另一具體實施例中,該絲胺酸係以足以藉由硫胱酸脫硫氫酶降低半胱胺酸被降解成硫化氫之用量以及以足以於存在色胺酸合成酶之下與形成口腔內色胺酸的吲哚反應之用量存在。
一具體實施例中,絲胺酸係以約0.01至約10% w/w之濃度,較佳為約0.1至約5% w/w之濃度,最佳為約0.4~1% w/w之濃度存在於本發明組成物內。
一具體實施例中,本發明的組成物進一步含有一或多種選自氧化劑、金屬螯合劑和抗微生物劑的藥劑。該氧化劑、金屬螯合劑和抗微生物劑並不侷限用於各種具體實施例,以及任何氧化劑、金屬螯合劑和抗微生物劑可被用於該具體實施例。較佳的氧化劑可選自H2O2和ClO2。較佳的金屬螯合劑可選自含Zn2+和Sn2+之化合物。該抗微生物劑可選自三氯沙、氯化鯨蠟基吡啶鎓(cetylpyridinium chloride)、氯已定(chlorhexidine)、植物萃取物,及一或多種精油。植物萃取物可選自任何揭示於美國專利申請案公開號2009/0087501中者,藉由引述將其內容併入於此。氧化劑、金屬螯合劑及/或抗微生物劑之添加可進一步加強本發明組成物對抗口臭的效力。
本發明者已發現當本發明組成物除了絲胺酸之外,含有金屬螯合劑可增加該組成物的效力。較佳的鋅鹽為乳酸鋅、檸檬酸鋅、氧化鋅和氯化鋅。鋅鹽為已知的VSC抑制劑,當鋅鹽與絲胺酸共同使用時可增加額外效力。
一具體實施例中,乳酸鋅係以約0.01至約3% w/w,較佳為約0.1至約0.5% w/w之濃度存在於本發明組成物內。除了乳酸鋅之外可使用其他鋅鹽,例如檸檬酸鋅或氯化鋅。就任何所用鋅鹽而言,其相對鋅離子係以約0.003至約1% w/w,較佳為約0.03至約0.2% w/w之濃度存在。
一具體實施例中,本發明組成物進一步含有一或多種選自抗牙斑劑、潔白劑、甜味劑、清潔劑和調味劑的藥劑。另一具體實施例中,本發明的組成物含有用於牙膏、牙乳劑、潄口液、口香糖或牙黏著劑的口腔可接受載劑。
一具體實施例中,本發明提供一種治療或預防口臭的方法,其包含將含有絲胺酸的口腔保健組成物施加至口腔,其中該絲胺酸係以可有效降低硫化氫所導致的口臭之用量存在。一具體實施例中,絲胺酸係以足以藉由口腔內硫胱酸脫硫氫酶降低半胱胺酸被降解成硫化氫而可降低口腔內硫化氫的量之用量存在。因此,一具體實施例中,本發明係關於一種降低口腔內硫化氫的量之方法。
一具體實施例中,本發明提供一種治療或預防口臭的方法,其包含將含有絲胺酸的口腔保健組成物施加至口腔,其中絲胺酸係以可有效降低吲哚所導致的口臭之用量存在。一具體實施例中,絲胺酸係以足以於存在色胺酸合成酶之下與形成口腔內色胺酸的吲哚反應而可降低口腔內吲哚的量之用量存在。因此,一具體實施例中,本發明係關於一種降低口腔內吲哚的量之方法。
一具體實施例中,本發明提供一種治療或預防口臭的方法,其包含將含有絲胺酸的口腔保健組成物施加至口腔,其中絲胺酸係以可有效降低硫化氫和吲哚所導致的口臭之用量存在。一具體實施例中,絲胺酸係以足以藉由硫胱酸脫硫氫酶降低半胱胺酸被降解成硫化氫之用量以及以足以於存在色胺酸合成酶之下與形成口腔內色胺酸的吲哚反應之用量存在。因此,一具體實施例中,本發明係關於一種降低口腔內硫化氫和吲哚的量之方法。
一具體實施例中,本發明提供一種治療或預防口臭的方法,其包含將含有絲胺酸的口腔保健組成物施加至口腔,其中絲胺酸係以可有效降低導因於至少一種選自由硫化氫、吲哚及其混合物所組成之群組的成分造成的口臭之用量存在。
本發明的方法中,絲胺酸係以約0.01至約10% w/w,較佳為約0.1至約5% w/w之濃度存在於該組成物內。一具體實施例中,絲胺酸係以約0.4至約1% w/w之濃度存在於該組成物內。
一具體實施例中,被用於本發明方法中的組成物進一步含有一或多種選自氧化劑、金屬螯合劑和抗微生物劑的藥劑。該氧化劑、金屬螯合劑和抗微生物劑並不侷限用於各種具體實施例,以及任何氧化劑、金屬螯合劑和抗微生物劑可被用於該具體實施例。較佳的氧化劑可選自H2O2和ClO2。較佳的金屬螯合劑可選自含Zn2+和Sn2+之化合物。該抗微生物劑可選自三氯沙、氯化鯨蠟基吡啶鎓(cetylpyridinium chloride)、氯已定(chlorhexidine)、植物萃取物,及一或多種精油。
一具體實施例中,被用於本發明方法中的組成物進一步含有一或多種選自抗牙斑劑、潔白劑、甜味劑、清潔劑和調味劑的藥劑。被用於本發明方法中的組成物含有用於牙膏、牙乳劑、潄口液、口香糖或牙黏著劑的口腔可接受載劑。
因此藉由引用將每一件參考文獻完整地併入於此。現在將參考下列非限制性實施例描述各種的具體實施例。
在下列實例中進一步說明本發明。該實例僅作為說明的用途並且無論如何非僅侷限於本發明描述和宣稱的範圍內。
測定絲胺酸和其他胺基酸對VSC的影響。將全唾液與半胱胺酸及選自絲胺酸、脯胺酸、酪胺酸、甘胺酸、天冬胺酸、麩胺酸和組胺酸的其他胺基酸共同培養隔夜。此試驗中,將10%之0.1%胺基酸溶液加至50%的全唾液。利用氣相層析(GC)測量VSC。相對含唾液和單獨半胱胺酸的樣本比較,發現絲胺酸對VSC的降低具有最高百分比。此結果示於表1。
此結果顯示絲胺酸能降低唾液內的VSC。
測定絲胺酸對吲哚的影響。將全唾液與色胺酸(0.14%)和各種濃度的絲胺酸於37℃培養隔夜。於24小時之後,將樣本冷卻至25℃。以己烷萃取該樣本及利用GC定量有機層。表2證明絲胺酸濃度對吲哚形成的效應。
此結果顯示絲胺酸能降低唾液內吲哚的數量。
測定乳酸鋅和絲胺酸對VSC的影響。將全唾液與色胺酸(0.14%)、乳酸鋅(0.16%)和需要時絲胺酸(0.42%)於37℃培養隔夜,並且將樣本冷卻至25℃。然後樣本利用GC定量頂部的VSC。表3證明有或無絲胺酸的乳酸鋅對VSC產生的效應。
此結果顯示絲胺酸能加強乳酸鋅的效應及降低VSC的產生。
測定乳酸鋅和絲胺酸對吲哚的影響。將全唾液與色胺酸(0.14%)、各種濃度的乳酸鋅和需要時絲胺酸(0.42%)於37℃培養隔夜。於24小時之後,將樣本冷卻至25℃。以己烷(2mL)萃取該樣本及利用GC定量有機層(1mL)。表4證明乳酸鋅和含絲胺酸的乳酸鋅對吲哚形成的效應。
此結果顯示絲胺酸能加強乳酸鋅的效應及降低吲哚的產生。
表5說明含有絲胺酸之口腔牙劑組成物的實例。
表6說明含有絲胺酸之潄口液組成物的實例。
表7說明含有絲胺酸和乳酸鋅之口腔牙劑組成物的實例。
表8為含有絲胺酸和乳酸鋅之潄口液組成物的實例。
此處所述之實(施)例及其他具體實施例僅為舉例性質而本發明全部的組成物和方法非僅限制於該範圍內。特定具體實施例、材料、組成物和方法可在本發明的範圍內進行等效的變化、改良及變異而實質上可獲得類似的結果。
Claims (16)
- 一種用於降低由硫化氫及/或吲哚所導致的口臭之口腔保健組成物,其包含L-絲胺酸,其中L-絲胺酸以0.1至約5% w/w之量存在,含Zn2+之化合物,其選自由乳酸鋅、檸檬酸鋅、氧化鋅和氯化鋅所組成的群組,其中該含Zn2+之化合物以0.1至0.5% w/w之濃度存在於該組成物內。
- 如申請專利範圍第1項之口腔保健組成物,其中L-絲胺酸係以0.4至約1% w/w之濃度存在於該組成物內。
- 如申請專利範圍第1項之口腔保健組成物,其中該組成物進一步含有一或多種選自氧化劑和抗微生物劑的藥劑。
- 如申請專利範圍第3項之口腔保健組成物,其中一或多種氧化劑係選自H2O2和ClO2。
- 如申請專利範圍第1項之口腔保健組成物,其中該含Zn2+之化合物係乳酸鋅。
- 如申請專利範圍第3項之口腔保健組成物,其中一或多種抗微生物劑係選自由三氯沙、氯化鯨蠟基吡啶鎓(cetylpyridinium chloride)、氯己定(chlorhexidine)、植物萃取物,及一或多種精油所組成的群組。
- 如申請專利範圍第1項之口腔保健組成物,其進一步含有一或多種選自抗牙斑劑、潔白劑、甜味劑、清潔劑和調味劑的藥劑。
- 如申請專利範圍第1項之口腔保健組成物,其進一 步含有一用於牙膏、牙乳劑、潄口液、口香糖或牙黏著劑的口腔可接受載劑。
- 一種如申請專利範圍第1項之口腔保健組成物於製造藥劑的用途,該藥劑用於治療或預防藉由至少一種選自由硫化氫、吲哚及其混合物所組成之群組的成分所導致之口臭。
- 如申請專利範圍第9項之用途,其中L-絲胺酸係以0.4至約1% w/w之濃度存在於該組成物內。
- 如申請專利範圍第9項之用途,其中該組成物進一步含有一或多種選自氧化劑和抗微生物劑的藥劑。
- 如申請專利範圍第11項之用途,其中一或多種氧化劑係選自由H2O2和ClO2所組成的群組。
- 如申請專利範圍第9項之用途,其中該含Zn2+之化合物係乳酸鋅。
- 如申請專利範圍第11項之用途,其中一或多種抗微生物劑係選自由三氯沙、氯化鯨蠟基吡啶鎓(cetylpyridinium chloride)、氯己定(chlorhexidine)、植物萃取物,及一或多種精油所組成的群組。
- 如申請專利範圍第9項之用途,其中該組成物進一步含有一或多種選自抗牙斑劑、潔白劑、甜味劑、清潔劑和調味劑的藥劑。
- 如申請專利範圍第9項之用途,其中該組成物含有一用於牙膏、牙乳劑、潄口液、口香糖或牙黏著劑的口腔可接受載劑。
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