TW201534336A - 口腔護理組成物 - Google Patents
口腔護理組成物 Download PDFInfo
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- TW201534336A TW201534336A TW103143992A TW103143992A TW201534336A TW 201534336 A TW201534336 A TW 201534336A TW 103143992 A TW103143992 A TW 103143992A TW 103143992 A TW103143992 A TW 103143992A TW 201534336 A TW201534336 A TW 201534336A
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- composition
- oral care
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- zinc
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- 239000000203 mixture Substances 0.000 title claims abstract description 188
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims abstract description 45
- 150000003751 zinc Chemical class 0.000 claims abstract description 23
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- 230000002401 inhibitory effect Effects 0.000 claims abstract description 14
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- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 claims description 57
- 239000011787 zinc oxide Substances 0.000 claims description 29
- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 claims description 25
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Abstract
一種包括絲胺酸和一或多種鋅鹽之口腔護理組成物,係用於降低或抑制口腔中生物膜形成。
Description
一種包括絲胺酸和一或多種鋅鹽之口腔護理組成物,係用於降低或抑制口腔中生物膜形成。
牙菌斑為黏附在牙齒或其他口腔表面,特別是在牙齦邊緣的生物膜,且係涉及牙齦炎、牙周炎、齲蝕和其他形式的牙周疾病。牙菌斑為黏著性的且很難從牙齒及/或口腔表面移除。牙菌斑包括葡聚醣,其為提供菌斑黏著性之不溶解性多糖。細菌酵素葡萄糖基轉移將膳食糖轉變成葡聚醣。菌斑礦物化而形成一種稱為結石(或酒石)之硬的沉積物,其變成牙齦之局部刺激物,導致牙齦炎。
各種抗細菌劑可阻滯細菌的生長並因此降低口腔表面之生物膜形成。
鋅及其他金屬化合物/鹽類先前已用作為抗細菌劑。不受限於理論,咸信游離的鋅離子藉由抑制葡萄糖代謝及/或與細菌細胞壁的交互作用,提供抗細菌效用,降低了細菌定殖在口腔(如Cummins D.,J Clin Periodontol 1991;18;455-461中所論述)。不溶性的鋅化合物氧化鋅在牙齒刷洗期間亦能遞送強力的抗細菌效用。
提供一種比先前已知的組成物具有甚至較大的生物膜降低效用之組成物,應為所希望的。
提供一口腔護理組成物,其包括:(a)絲胺酸;及(b)1.5:1至4.5:1之氧化鋅與檸檬酸鋅重量比的氧化鋅和檸檬酸鋅。
視需要,組成物具有1.5:1至4:1,1.7:1至2.3:1,1.9:1至2.1:1,或約2:1之氧化鋅與檸檬酸鋅的重量比。亦可使用以這些重量比為基準之對應的莫耳比。
視需要,此組成物,以組成物的總重量為基準,係包括0.05重量%至0.8重量%,或0.075重量%至0.25重量%之量的絲胺酸。進一步視需要,此組成物,以組成物的總重量為基準,係包括從0.12重量%至0.25重量%之量的絲胺酸。進一步視需要,此組成物,以組成物的總重量為基準,係包括從0.14重量%至0.20重量%之量的絲胺酸。又進一步視需要,此組成物,以組成物的總重量為基準,係包括0.15重量%之量的絲胺酸。
視需要,此組成物,以組成物的總重量為基準,係包括從0.5重量%至1.5重量%之量的氧化鋅和從0.25重量%至0.75重量%之量的檸檬酸鋅。進一步視需要,此組成物,以組成物的總重量為基準,係包括約1重量%之量的氧化鋅和約0.5重量%之量的檸檬酸鋅。
亦提供一口腔護理組成物,其包括:(a)絲胺酸和(b)一或多種鋅鹽;供用於降低或抑制口腔中生物膜形成。
視需要,絲胺酸,以組成物的總重量為基準,係以從0.05重量%至0.8重量%之量存在組成物中。進一步視需要,絲胺酸,以組成物的總重量為基準,係以從0.05重量%至0.39重量%之量存在組成物中。又進一步視需要,絲胺酸,以組成物的總重量為基準,係以從0.075重量%至0.25重量%之量存在組成物中。又進一步視需要,此組成物,以組成物的總重量為基準,係包括從0.12重量%至0.25重量%,之量的絲胺酸。進一步視需要,此組成物,以組成物的總重量為基準,係包括從0.14重量%至0.20
重量%之量的絲胺酸。又進一步視需要,此組成物,以組成物的總重量為基準,係包括約0.15重量%之量的絲胺酸。
視需要,絲胺酸:總鋅鹽之莫耳比係從0.01:1至3:1。
視需要,組成物中的總鋅鹽濃度,以組成物的總重量為基準,係從0.2重量%至5重量%。
視需要,至少一種該一或多種鋅鹽為氧化鋅。
視需要,至少一種該一或多種鋅鹽為檸檬酸鋅。
視需要,此組成物,以組成物的總重量為基準,係包括從0.5重量%至1.5重量%之量的氧化鋅和從0.25重量%至0.75重量%之量的檸檬酸鋅。進一步視需要,此組成物,以組成物的總重量為基準,係包括約1重量%之量的氧化鋅和約0.5重量%之量的檸檬酸鋅。
亦提供降低或抑制口腔中生物膜形成之方法,該方法係包括將口腔與任何口腔護理組成物接觸。
亦提供(a)絲胺酸和(b)一或多種鋅鹽之組合物的口腔護理組成物之用途;係用以降低或抑制口腔中生物膜形成。
本發明進一步可應用的領域由下文所提供的詳細說明中將變得更顯而易見。應了解,詳細說明和特定的實例,在指出較佳的本發明之實施例的同時,係希望僅為說明之目的且不希望限制本發明之範圍。
下列較佳實施例之說明本質上僅為例示性且不希望在任何方面限制本發明、其應用或用途。
如全文所用,範圍係用於速記供描述在此範圍內的各個和每個值。在此範圍內的任何值皆可選作此範圍的最終值。此外,所有文中所引述的參考文獻係以全文引用的方式併入本文中。在本揭示文與所引述的參考文獻的定義有衝突時,則以本揭示文為主。
除非另有說明否則文中和說明書之他處所表示的所有百分比和量,應了解係指重量百分比。所給予的量係以物質之有效重量為基準。
本發明人意外地已發現添加絲胺酸至包括鋅鹽之口腔護理組成物中,促進了口腔護理組成物降低生物膜的效用。本發明人亦意外地發現最佳的絲胺酸濃度,在此濃度時,含鋅鹽之口腔護理組成物的降低生物膜效用為最佳的。
在第一方面,係提供一口腔護理組成物,其包括(a)絲胺酸;及(b)至少1.5:1至4.5:1之氧化鋅與檸檬酸鋅重量比的氧化鋅和檸檬酸鋅。
視需要,此組成物具有1.5:1至4:1,1.7:1至2.3:1,1.9:1至2.1:1,或約2:1之氧化鋅與檸檬酸鋅的重量比。亦可使用以這些重量比為基準之對應的莫耳比。
在第二方面係提供一口腔護理組成物,其包括(a)絲胺酸和(b)一或多種鋅鹽;供用於降低或抑制口腔中生物膜形成。在某些實施例中,絲胺酸,以組成物的總重量為基準,係以從0.05重量%至0.8重量%,從0.05重量%至0.75重量%,或從0.05重量%至0.39重量%之量存在此組成物中。
在第三方面,係提供一種降低或抑制口腔中生物膜形成之方法,該方法係包括將口腔與包含(a)絲胺酸和(b)至少一種鋅鹽之口腔護理組成物接觸。在某些實施例中,絲胺酸,以組成物的總重量為基準,可以從0.05重量%至0.8重量%,從0.05重量%至0.75重量%,或從0.05重量%至0.39重量%之量存在此組成物中。
在第四方面,係提供(a)絲胺酸和(b)至少一種鋅鹽之組合的口腔護理組成物之用途;係用以降低或抑制口腔中生物膜形成。在某些實施例中,絲胺酸,以組成物的總重量為基準,可以從0.05重量%至0.8重量
%,從0.05重量%至0.75重量%,或從0.05重量%至0.39重量%之量存在口腔護理組成物中。
在第五方面,係提供根據第一方面之口腔護理組成物,供用於降低或抑制口腔中生物膜形成。
在第六方面,係提供降低或抑制口腔中生物膜形成之方法,該方法係包括將口腔與根據第一方面之口腔護理組成物接觸。
在上述的各方面中,絲胺酸,以組成物的總重量為基準,可以從0.075重量%至0.35重量%;從0.075重量%至0.30重量%;從0.075重量%至0.25重量%;從0.12重量%至0.25重量%;從0.14重量%至0.20重量%;從0.14重量%至0.18重量%;從0.14重量%至0.16重量%;或約0.15重量%之量存在口腔護理組成物中。
在上述各方面之任何實施例中,絲胺酸:總鋅鹽之莫耳比可從0.01:1至3:1;從0.01:1至2.2:1;從0.02:1至1.4:1;從0.05:1至0.3:1;從0.1:1至0.2:1;或約0.1:1。
可用於任何上述方面之組成物中的適合鋅鹽之實例包括(但不限於):氧化鋅、檸檬酸鋅、乳酸鋅、氯化鋅、乙酸鋅、葡萄糖酸鋅、甘胺酸鋅、硫酸鋅、檸檬酸鈉鋅及其混合物。在任何上述的方面中,至少一種的一或多種鋅鹽可為氧化鋅。另外或另一種選擇,至少一種的一或多種鋅鹽可為檸檬酸鋅。在某些實施例中,組成物中的鋅鹽之總濃度,以組成物的總重量為基準,為從0.2重量%至5重量%;從0.5重量%至2.5重量%;從0.8重量%至2重量%;或約1.5重量%。
在各上述方面之任何實施例中,組成物,以組成物的總重量為基準,可包括從0.5重量%至1.5重量%之量的氧化鋅和從0.25重量%至0.75重量%之量的檸檬酸鋅。另一種選擇,此組成物,以組成物的總重量為基準,可包括0.75重量%至1.25重量%之量的氧化鋅和0.4重量%至0.6重
量%之量的檸檬酸鋅。另一種選擇,此組成物,以組成物的總重量為基準,可包括約1重量%之量的氧化鋅和約0.5重量%之量的檸檬酸鋅。
在各上述方面之任何實施例中,此組成物可進一步包括一或多種研磨劑。可包括在組成物中的適合研磨劑包括(但不限於):矽氧研磨劑、氧化鋁、矽酸鋁、煅燒氧化鋁、澎潤土或其他矽質物質、不溶性磷酸鹽、天然碳酸鈣、沉澱碳酸鈣及其混合物。在某些實施例中,至少一種之一或多種研磨劑為矽氧研磨劑。矽氧研磨劑之實例包括(但不限於):具有約20微米之平均粒徑的沉澱或水合矽氧(例如由J.M.Huber Chemicals Division,Havre de Grace,Md.21078所販售的Zeodent 105和Zeodent 114);Sylodent 783(由Davison Chemical Division of W.R.Grace & Company所販售),或Sorbosil AC 43(來自PQ Corporation)。在某些實施例中,至少一種之一或多種研磨劑為碳酸鈣研磨劑,例如沉澱碳酸鈣(PCC)或天然碳酸鈣(NCC)。
在各上述方面之任何實施例中,此組成物可進一步包括抗結石(酒石控制)劑。適合的抗結石劑包括(但不限於):磷酸鹽和聚磷酸鹽、聚胺基丙磺酸(AMPS)、聚烯烴磺酸鹽、聚烯烴磷酸鹽、二膦酸鹽例如氮雜環烷-2,2-二膦酸鹽(例如氮雜環庚烷-2,2-二膦酸)、N-甲基氮雜環己烷-2,3-二膦酸、乙烷-1-羥基-1,1-二膦酸(EHDP)及乙烷-1-胺基-1,1-二膦酸鹽、磷醯烷羧酸。可使用的無機磷酸鹽和聚磷酸鹽包括磷酸二氫鈉、磷酸氫二鈉和磷酸三鈉、焦磷酸四鈉(TSPP)、焦磷酸四鉀、三聚磷酸鈉、四聚磷酸鹽、三偏磷酸鈉、六偏磷酸鈉及其混合物。其他可使用的酒石控制劑包括聚羧酸酯聚合物及聚乙烯甲基醚/馬來酸酐(PVM/MA)共聚物,例如GANTREZ®。在某些實施例中,此抗結石劑為至少一種焦磷酸四鈉和焦磷酸四鉀。在某些實施例中,此抗結石劑,以組成物的總重量為基準,係以從0.2重量%至0.8重量%;0.3重量%至0.7重量%;0.4重量%至0.6重量%;或約0.5重量%之量存在組成物中。
在上述各方面之任何實施例中,口腔護理組成物可為一潔牙劑、牙膏、牙凝膠、牙粉、漱口水、口部沖洗液、口含錠、錠劑、噴霧、口香糖或薄膜。在特定的實施例中,此口腔護理組成物為牙膏、凝膠或牙粉。
口腔護理組成物可進一步包括另外的成份。這些另外的成份可包括(但不限於)稀釋劑、碳酸氫鹽、pH調節劑、界面活性劑、泡沫調節劑、增稠劑、保濕劑、甜味劑、風味劑、顏料、另外的抗細菌劑、抗齲蝕劑及其混合物。
在某些實施例中,此口腔護理組成物係包括至少一種由於冒泡和釋放二氧化碳而可用於例如賦予牙齒和牙齦「潔淨感」之碳酸氫鹽。任何口腔上可接受的碳酸氫鹽皆可使用,包括(不限於)鹼金屬碳酸氫鹽,例如碳酸氫鈉和碳酸氫鉀、碳酸氫銨及其類似物。一或多種的碳酸氫鹽視需要,以組成物的總重量計,係以約0.1重量%至約50重量%之總量存在,例如1重量%至20重量%。
在某些實施例中,此口腔護理組成物包括至少一種pH調節劑。此等試劑包括用以降低pH之酸化劑,用以提高pH之鹼化劑及控制pH在所欲範圍內的緩衝劑。例如,可包括一或多種選自酸化、鹼化和緩衝試劑之化合物用以提供2至10之pH,或在各種說明性實施例中,2至8,3至9,4至8,5至7,6至10,7至9等之pH。任何口腔上可接受的碳酸氫鹽皆可使用,包括(不限於)羧酸、磷酸和磺酸、酸鹽(例如檸檬酸一鈉、檸檬酸二鈉、蘋果酸一鈉等),鹼金屬氫氧化物例如氫氧化鈉,碳酸鹽例如碳酸鈉,碳酸氫鹽、倍半碳酸鹽、硼酸鹽、矽酸鹽、磷酸鹽(例如磷酸一鈉、磷酸三鈉),咪唑及其類似物。一或多種pH調節劑視需要係以有效維持組成物在口腔可接受的pH範圍內之總量存在。
此口腔護理組成物亦可包括至少一種界面活性劑。任何口腔可接受的界面活性劑皆可使用,其大部份為陰離子、非離子或兩性離子。適合的陰離子界面活性劑包括(不限於)C8-20烷基硫酸鹽之水溶性鹽類、C8-20脂肪酸之磺酸單甘油酯、肌胺酸鹽、牛磺酸鹽及其類似物。這些和其他種類的說明性實例包括月桂基硫酸鈉、椰單甘油酯磺酸鈉、月桂基肌胺酸鈉、月桂醯羥乙基磺酸鈉、聚氧乙烯月桂醚羧酸鈉和十二烷基苯磺酸鈉。適合的非離子界面活性劑包括(不限於)泊洛沙姆(poloxamer)、聚氧乙烯山梨醇酐酯、脂醇乙氧化物、烷基酚乙氧化物、三級胺氧化物、四級膦氧化物、二烷基亞碸及其類似物。適合的兩性界面活性劑包括(不限於)具有陰離子基團例如羧酸根、硫酸根、磺酸根、磷酸根或膦酸根之C8-20脂族二級或三級胺的衍生物。亦可使用甜菜鹼,其適合的實例為椰油醯胺丙基甜菜鹼。一或多種界面活性劑視需要,以組成物的總重量計,係以約0.01重量%至約10重量%,例如從約0.05重量%至約5重量%,或從約0.1重量%至約2重量%的總量存在。
此口腔護理組成物可包括至少一種可用於例如增加因攪動組成物所產生的泡沫之量、厚度或安定性的泡沫調節劑。任何口腔可接受的泡沫調節劑皆可使用,其包括(不限於)聚乙二醇(PEG),亦稱為聚氧乙烯。適合的為高分子量PEG,其包括該等具有200,000至7,000,000,例如500,000至5,000,000,或1,000,000至2,500,000之平均分子量的PEG。一或多種PEG視需要,以組成物的總重量計,係以約0.1重量%至約10重量%,例如從約0.2重量%至5重量%,或從約0.25重量%至約2重量%的總量存在。
此口腔護理組成物可包括至少一種可用於例如賦予組成物所欲的稠度及/或口感之增稠劑。任何口腔上可接受的增稠劑皆可使用,包括(不限於)卡波姆(carbomer),亦稱為羧乙烯聚合物,角叉菜膠,亦稱為愛
爾蘭苔及更特言之角叉菜膠(ι-角叉菜膠),纖維素聚合物例如羥乙基纖維素、羧甲基纖維素(CMC)及其鹽類,例如CMC鈉、天然膠例如刺梧桐膠、三仙膠、阿拉伯膠和黃蓍膠,膠體矽酸鎂鋁和膠體矽氧及其類似物。較佳的增稠或成膠劑之種類包括一種丙烯酸與異戊四醇之烷基醚或蔗糖之烷基醚交聯之同聚物或卡波姆。卡波姆可購自B.F.Goodrich公司,如Carbopol®系列。特佳的Carbopol包括Carbopol 934、940、941、956、974P及其混合物。矽氧增稠劑例如DT 267(來自PPG Industries)亦可使用。一或多種增稠劑視需要,以組成物的總重量計,係以約0.01重量%至15重量%,例如從約0.1重量%至約10重量%,或從約0.2重量%至約5重量%之總量存在。
組成物可包括至少一種可用於例如幫助抑制成份沉降或分離或促進液體組成物攪動時之再分散性的黏度調節劑。任何口腔上可接受的黏度調節劑皆可使用,包括(不限於)礦物油、石蠟、黏土和有機修飾黏土、矽氧及其類似物。一或多種黏度調節劑視需要,以組成物的總重量計,係以從約0.01重量%至約10重量%,例如從約0.1重量%至5重量%的總量存在。
組成物亦可包括至少一種保濕劑。任何口腔上可接受的保濕劑皆可使用,包括(不限於)多元醇例如甘油、山梨醇(視需要為70重量%水中溶液)、木糖醇或低分子量聚乙二醇(PEG)。大部分的保濕劑亦可作為甜味劑。一或多種保濕劑視需要,以組成物的總重量計,係以約1重量%至約70重量%,例如從約1重量%至50重量%,從約2重量%至約25重量%,或從約5重量%至約15重量%的總量存在。
口腔護理組成物可包括至少一種可用於例如增進組成物口味的甜味劑。強烈地依照所選的特定甜味劑,但典型地一或多種甜味劑視需要,以組成物的總重量計,係以約0.005重量%至約5重量%,視需
要約0.005重量%至.02重量%,進一步視需要,以組成物的總重量計,0.05重量%至0.1重量%的總量存在。
組成物亦可包括至少一種可用於例如增進組成物口味的風味劑。任何口腔可接受的天然或合成的風味劑皆可使用,其包括(不限於)茶風味劑、香草、鼠尾草、馬鬱蘭、西洋芹油、綠薄荷油、肉桂油、冬青油(水楊酸甲酯)、椒薄荷油、丁香油、月桂油、大茴香油、尤加利油、柑桔油、水果油和萃取物,包括該等衍生自檸檬、柳橙、萊姆、葡萄柚、杏桃、香蕉、葡萄、蘋果、草莓、櫻桃、鳳梨等之油和萃取物,豆類-和堅果-衍生的風味劑,例如咖啡、可可、可樂(cola)、花生、杏仁等,吸附性和包膠的風味劑及其類似物。亦可涵蓋在本文風味劑中的為提供香氣/或其他口中感官效果,包括涼爽或溫暖效果之成份。此等成份說明性地係包括薄荷腦、乙酸薄荷酯、乳酸薄荷酯、樟腦、尤加利油、尤加利油醇、茴香腦、丁香酚、肉桂、噁烷酮(oxanone)、α-紫羅蘭酮、丙烯基乙基愈創木酚、百里酚、芫荽醇、苯甲醛、肉桂醛、N-乙基-對-薄荷烷-3-甲醯胺、N-2,3-三甲基-2-異丙基丁醯胺、3-(1-薄荷氧基)-丙烷-1,2-二醇、肉桂醛甘油縮醛(CGA)、薄荷酮甘油縮醛(MGA)及其類似物。一或多種風味劑視需要,以組成物的總重量計,係以約0.01重量%至約5重量%,例如從約0.03重量%至約2.5重量%,視需要約0.05重量%至約1.5重量%,進一步視需要約0.1重量%至約0.3重量%的總量存在。
組成物可包括至少一種色劑。色劑在文中係包括顏料、染劑、色澱和賦予特定光澤或反射度之試劑,例如珠光劑。任何口腔上可接受的色劑皆可使用,包括(不限於)滑石、雲母、碳酸鎂、矽酸鎂、矽酸鎂鋁、二氧化鈦、氧化鋅、紅色、黃色、棕色和黑色氧化鐵、亞鐵氰化鐵銨、錳紫、群青、鈦酸雲母、氯氧化鉍及其類似物。一或多種色劑視需要,以組成物的總重量計,係以約0.001重量%至約20重量%,例如,從約0.01重
量%至約10重量%,或從0.01重量%至約10重量%,或從約0.1重量%至約5重量%的總量存在。
組成物亦可包括另外的抗細菌劑或防腐劑,例如氯己定(chlorhexidine)、三氯沙、四級胺化合物(例如氯化烷基二甲基苄基銨(benzalkonium chloride))或對羥基苯甲酸酯,例如對羥基苯甲酸甲酯和對羥基苯甲酸丙酯。一或多種另外的抗細菌劑或防腐劑可視需要,以組成物的總重量計,係以從0.01重量%至約0.5重量%,視需要約0.05重量%至約0.1重量量%的總量存在組成物中。
口腔護理組成物亦可包括一氟化物離子來源。氟化物離子來源包括(但不限於)氟化亞錫、氟化鈉、氟化鉀、單氟磷酸鉀、單氟磷酸鈉、單氟磷酸銨、氟矽酸鈉、氟矽酸銨、氟化胺,例如奧拉氟(N’-正十八烷基三亞甲基二胺-N,N,N’-三(2-乙醇)-二氟化氫)、氟化銨及其組合物。在特定的實施例中,氟化物離子來源包括氟化亞錫、氟化鈉、氟化胺、單氟磷酸鈉以及其混合物。在特定的實施例中,口腔保健組成物亦可含有足以供應約50ppm至約5000ppm氟化物離子之量的氟化物離子或氟提供成份,例如從約100ppm至約1000ppm,從約200ppm至約500ppm,或約250ppm氟化物離子。氟化物離子來源,以組合物之重量計,可以約0.001重量%至約10重量%之量加至組成物中,例如從約0.003重量%至約5重量%,0.01重量%至約1重量%,或約0.05重量%。然而,應了解,提供適量氟化物離子之氟化物鹽類的重量明顯地將以鹽中相對離子的重量為基準而變,且熟習本項技術者可容易地測定此量。較佳的氟化鹽可為氟化鈉。
組成物可包括可用於,例如改善口乾之唾液刺激劑。任何口腔上可接受的唾液刺激劑皆可使用,包括(不限於)食物酸例如檸檬酸、乳酸、蘋果酸、琥珀酸、抗壞血酸、己二酸、延胡索酸和酒石酸,及其混合物。一或多種唾液刺激劑視需要係以唾液刺激上有效之總量存在。
組成物可包括抗敏感劑,例如鉀鹽,例如硝酸鉀、碳酸氫鉀、氯化鉀、檸檬酸鉀和草酸鉀;辣椒素;丁香酚;鍶鹽;氯鹽及其組合物。依照所選的試劑,此等試劑可以有效量加入,例如,以組成物的總重量為基準,從約1重量%至約20重量%。
組成物可進一步包括抗氧化劑。任何口腔可接受的抗氧化劑皆可使用,包括(不限於)丁基羥基茴香醚(BHA)、丁基羥基甲苯(BHT)、維生素A、類胡蘿蔔素、維生素E、類黃酮、多酚、抗壞血酸、香草抗氧化劑、葉綠素、退黑激素及其混合物。
可進行實驗用以評估含不同濃度絲胺酸之組成物的生物膜降低效用。檢測含有矽氧或天然碳酸鈣(NCC)作為研磨劑之調配物。
在所有的實例中,下列,所用的實驗方法學為生物膜生長抑制曼徹斯特大學模型(Biofilm Growth Inhibition University of Manchester Model)。用於此模型之方法係如下:
(1)從四位健康的自願者收集牙菌斑並合併一起作為接種物。此接種物的光學密度在610nm係符合0.3吸收度。
(2)於37℃無氧條件下,將無菌的羥磷灰石(HAP)片以1毫升的人工唾液(含0.01重量%蔗糖)和1毫升合併的唾液於24孔微量盤中培養24小時。
(3)就各檢測的潔牙劑(及各對照組),係製作1重量份潔牙劑:2重量份無菌蒸餾水之處理溶液。將各新鮮製備的處理溶液加到三個孔槽並與其中的HAP片接觸10分鐘。
(4)然後移除各孔槽之液體相並以2毫升無菌人工唾液取代。
(5)然後讓HAP片於37℃無氧的條件下保持8天。
(6)於2、4和8天的間隔,無菌下收集及HAP片盤並轉置於半強度預還原的巰基乙酸鹽培養基(每片4.5毫升)。
(7)就總革蘭氏陰性厭氧菌,係將100μL的10-4、10-5和10-6稀釋液就各片以雙重複置入新黴素(Neomycin)/萬古黴素(Vancomycin)(NV)瓊脂上。
(8)使用無菌的塗覆器將培養皿進行表面塗覆並於37℃無氧下培養72小時,之後計算各培養皿的菌落數目。
就各檢測的潔牙劑或對照組計算log10 CFU/毫升(其中CFU=菌落形成單位)。較低的Log10 CFU/毫升表示所檢測的潔牙劑具有較大的抑制生物膜生長之效力。
檢測結果係如下列實例1至3所示。
在第一輪的生物膜降低試驗中,係對表1中所列的調配物就其降低生物膜生長的能力進行評估。使用生物膜生長抑制曼徹斯特大學模型方法(上述)所得到的結果係顯示於表1中,其中平均log10 CFU/毫升係得自方法的步驟6中培養8天的HAP片。
如表1所示的結果顯示含絲胺酸的配方促進生物膜降低,與所用的研磨劑種類(矽氧或天然碳酸鈣)無關。含0.25重量%絲胺酸和0.75重量%絲胺酸之配方在效力上並無顯著差異。
為了研究絲胺酸的最佳濃度,是否在此濃度時生物模降低之效力為最大,係於潔牙劑中使用下表2所列的配方進行第二輪的生物膜降低試驗。所有檢測的潔牙劑皆含有1重量%ZnO和0.5重量%檸檬酸Zn。在下列結果中,對於「統計顯著性」享有相同字母之配方,在其生物膜降低效力上並未顯現顯著差異。
從上表2可看出,在含矽氧的配方中0.15重量%絲胺酸勝過所有其他檢測的配方,如明顯較低的平均Log10 CFU/毫升值所示。接著是含NCC配方中0.15重量%絲胺酸,然後為含矽氧或NCC配方中0.25重量%絲胺酸,其然後為含矽氧或NCC配方中0.075重量%絲胺酸。如實例1,相較於無絲胺酸的調配物,含絲胺酸的調配物在生物膜降低上顯示增進的效力。於此實例中所得到的結果亦指出調配物的生物膜降低效力與其是否含有矽氧或NCC作為研磨劑無關。
重複實例2的試驗,在下列結果中,對於「統計顯著性」享有相同字母之配方,在其生物膜降低效力上並未顯現顯著差異。
如上所示,實例3中所得到的結果係與實例2中所得到結果相類似。從實例2和3的結果,可看出受檢樣本之生物膜降低效能隨絲胺酸濃度從0重量%增加至0.15重量%而增加,且該效能在較高的絲胺酸濃度(例如0.25重量%)時則下降,但其效能仍比單獨的鋅更佳。對於矽氧基底和NCC-基底的調配物,含有0.15重量%絲胺酸的調配物就其生物膜降低效力而言,表現優於含較高或較低絲胺酸濃度的調配物。
Claims (22)
- 一種口腔護理組成物,係包括:(a)絲胺酸;及(b)1.5:1至4.5:1之氧化鋅與檸檬酸鋅重量比的氧化鋅和檸檬酸鋅。
- 如申請專利範圍第1項之口腔護理組成物,其中該氧化鋅與檸檬酸鋅的重量比為1.5:1至4:1,1.7:1至2.3:1,1.9:1至2.1:1,或約2:1。
- 如任何前述申請專利範圍之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括0.05重量%至0.8重量%之量的絲胺酸,視需要0.05重量%至0.39重量%,0.075重量%至0.25重量%,0.12重量%至0.25重量%,或0.14重量%至0.2重量%。
- 如任何前述申請專利範圍之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括0.15重量%之量的絲胺酸。
- 如任何前述申請專利範圍之口腔護理組成物,其中組成物中氧化鋅和檸檬酸鋅的總濃度,以組成物的總重量為基準,為0.2重量%至5重量%。
- 如任何前述申請專利範圍之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括0.5重量%至1.5重量%之量的氧化鋅和0.25重量%至0.75重量%之量的檸檬酸鋅。
- 如任何前述申請專利範圍之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括約1重量%之量的氧化鋅和約0.5重量%之量的檸檬酸鋅。
- 一種口腔護理組成物,係包括:(a)絲胺酸和(b)一或多種鋅鹽;供用於降低或抑制口腔中生物膜形成。
- 如申請專利範圍第8項之口腔護理組成物,其中絲胺酸,以組成物的總重量為基準,係以從0.05重量%至0.8重量%之量存在組成物中。
- 如申請專利範圍第9項之口腔護理組成物,其中絲胺酸,以組成物的總重量為基準,係以從0.05重量%至0.39重量%之量存在組成物中。
- 如申請專利範圍第10項之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括從0.075重量%至0.25重量%之量的絲胺酸。
- 如申請專利範圍第11項之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括從0.12重量%至0.25重量%之量的絲胺酸。
- 如申請專利範圍第12項之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括從0.14重量%至0.20重量%之量的絲胺酸。
- 如申請專利範圍第13項之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括約0.15重量%之量的絲胺酸。
- 如申請專利範圍第8至14項任一項中之口腔護理組成物,其中該絲胺酸:總鋅鹽之莫耳比係從0.01:1至3:1。
- 如申請專利範圍第8至15項任一項中之口腔護理組成物,其中組成物中鋅鹽之總濃度,以組成物的總重量為基準,為0.2重量%至5重量%。
- 如申請專利範圍第8至16項任一項中之口腔護理組成物,其中至少一種該一或多種鋅鹽為氧化鋅。
- 如申請專利範圍第8至17項任一項中之口腔護理組成物,其中至少一種該一或多種鋅鹽為檸檬酸鋅。
- 如申請專利範圍第18項之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括0.5重量%至1.5重量%之量的氧化鋅和0.25重量%至0.75重量%之量的檸檬酸鋅。
- 如申請專利範圍第19項之口腔護理組成物,其中該組成物,以組成物的總重量為基準,係包括約1重量%之量的氧化鋅和約0.5重量%之量的檸檬酸鋅。
- 如申請專利範圍第18項之口腔護理組成物,其中氧化鋅與檸檬酸鋅的重量比為1.5:1至4.5:1,視需要1.5:1至4:1,1.7:1至2.3:1,1.9:1至2.1:1,或約2:1。
- 一種如申請專利範圍第1-21項任一項中之口腔護理組成物之用途,係用於製造口腔護理產品供降低或抑制口腔中生物膜形成。
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