TWI676484B - 口腔保健組成物 - Google Patents
口腔保健組成物 Download PDFInfo
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- TWI676484B TWI676484B TW103143994A TW103143994A TWI676484B TW I676484 B TWI676484 B TW I676484B TW 103143994 A TW103143994 A TW 103143994A TW 103143994 A TW103143994 A TW 103143994A TW I676484 B TWI676484 B TW I676484B
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- zinc
- oral
- care composition
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- 239000000203 mixture Substances 0.000 title claims abstract description 132
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 claims abstract description 42
- PFNFFQXMRSDOHW-UHFFFAOYSA-N spermine Chemical compound NCCCNCCCCNCCCN PFNFFQXMRSDOHW-UHFFFAOYSA-N 0.000 claims abstract description 42
- 229940063675 spermine Drugs 0.000 claims abstract description 21
- 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 abstract description 21
- 239000011746 zinc citrate Substances 0.000 claims abstract description 21
- 235000006076 zinc citrate Nutrition 0.000 claims abstract description 21
- 229940068475 zinc citrate Drugs 0.000 claims abstract description 21
- 239000011787 zinc oxide Substances 0.000 claims abstract description 21
- 150000003839 salts Chemical group 0.000 claims abstract description 15
- 210000000214 mouth Anatomy 0.000 claims description 14
- 239000004475 Arginine Substances 0.000 claims description 10
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 10
- 230000015572 biosynthetic process Effects 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000032770 biofilm formation Effects 0.000 abstract description 3
- 150000003751 zinc Chemical class 0.000 description 23
- -1 amino acid salt Chemical class 0.000 description 16
- 235000014692 zinc oxide Nutrition 0.000 description 16
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 14
- 239000003795 chemical substances by application Substances 0.000 description 14
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 12
- 239000002253 acid Substances 0.000 description 9
- 229960003121 arginine Drugs 0.000 description 9
- 239000003082 abrasive agent Substances 0.000 description 8
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- 239000000377 silicon dioxide Substances 0.000 description 6
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- DGMOQCHIPOPXEK-UHFFFAOYSA-N Spermic acid 2 Chemical compound OC(=O)CCNCCCCNCCC(O)=O DGMOQCHIPOPXEK-UHFFFAOYSA-N 0.000 description 4
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- 239000001177 diphosphate Substances 0.000 description 3
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- RYCLIXPGLDDLTM-UHFFFAOYSA-J tetrapotassium;phosphonato phosphate Chemical compound [K+].[K+].[K+].[K+].[O-]P([O-])(=O)OP([O-])([O-])=O RYCLIXPGLDDLTM-UHFFFAOYSA-J 0.000 description 3
- 229910052725 zinc Inorganic materials 0.000 description 3
- 239000011701 zinc Substances 0.000 description 3
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 description 2
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- NPBVQXIMTZKSBA-UHFFFAOYSA-N Chavibetol Natural products COC1=CC=C(CC=C)C=C1O NPBVQXIMTZKSBA-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical class OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- SNRUBQQJIBEYMU-UHFFFAOYSA-N Dodecane Natural products CCCCCCCCCCCC SNRUBQQJIBEYMU-UHFFFAOYSA-N 0.000 description 2
- 239000005770 Eugenol Substances 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 0.000 description 2
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- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical compound O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 description 2
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- VSIIXMUUUJUKCM-UHFFFAOYSA-D pentacalcium;fluoride;triphosphate Chemical compound [F-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O VSIIXMUUUJUKCM-UHFFFAOYSA-D 0.000 description 2
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Abstract
一種口腔保健組成物，包含：(a)游離或鹽類形式的精胺酸；及(b)氧化鋅和檸檬酸鋅。口腔保健組成物可減少或預防在口腔內形成生物膜。
Description
本發明係關於一種包含游離或鹽類形式的精胺酸及氧化鋅和檸檬酸鋅之口腔保健組成物。
牙菌斑為附著牙齒和其他口腔表面(特別是在牙齦邊緣)的生物膜，且意味者發生牙齦炎、牙周炎、齲齒和其他形式牙周病。牙菌斑具黏著性且難以從牙齒及/或口腔表面清除。牙菌斑包含聚葡糖，其係一種不可溶多醣類，可使牙菌斑具黏著性。細菌酵素葡萄糖轉移酶會將乳糖轉變成聚葡糖。牙菌斑礦化之後會形成稱為牙結石(或牙垢)的硬質沈積物，然後成為牙床的局部刺激物，而引發牙齦炎。
多種抗菌劑可防止細菌滋長，因而減少在口腔表面上形成生物膜。
先前已使用鋅和其他金屬化合物/鹽類作為抗菌劑。不受限於理論，據信游離鋅離子可避免葡萄糖代謝及/或與細菌細胞壁交互作用，減少細菌拓殖於口腔，而提供抗菌功效(如同Cummins D.,J Clin Periodontol 1991；18；455-461所討論)。不可溶鋅化合物和氧化鋅亦可在刷牙期間提供強大的抗菌功效。
較佳為提供一種口腔保健組成物，其在減少生物膜方面展現較先前已知的組成物更強大的功效。
提供一種口腔保健組成物，包含：(a)游離或鹽類形式的精胺酸；及(b)兩種或多種鋅鹽，其中該鋅鹽之至少一種為氧化鋅且該鋅鹽之至少一種為檸檬酸鋅。
選擇性地，該氧化鋅對檸檬酸鋅的重量比例為1.5；1至4.5：1、1.5：1至4：1、1.7：1至2.3：1、1.9：1至2.1：1或約2：1。另外，可使用基於此等重量比例的對應莫耳比例。
選擇性地，精胺酸的含量為從0.5重量%至10重量%，以組成物的總重量為基準。另外選擇性地，該精胺酸的含量為0.5重量%至3重量%或從1重量%至2.85重量%，以組成物的總重量為基準。又另外選擇性地，該精胺酸的含量為從1.17重量%至2.25重量%，以組成物的總重量為基準。又另外選擇性地，該精胺酸的含量為從1.4重量%至1.6重量%，以組成物的總重量為基準。另外選擇性地，該精胺酸的含量為約1.5重量%，以組成物的總重量為基準。
選擇性地，鋅鹽在組成物中的總濃度為從0.2重量%至5重量%，以組成物的總重量為基準。
選擇性地，精胺酸對所有鋅鹽的莫耳比例為從0.05：1至10：1。
選擇性地，組成物包含含量為0.5重量%至1.5重量%的氧化鋅，及含量為0.25重量%至0.75重量%的檸檬酸鋅，以組成物的總重量為基準。另外選擇性地，該組成物包含含量為約1重量%的氧化鋅，及含量為約0.5重量%的檸檬酸鋅，以組成物的總重量為基準。
選擇性地，組成物進一步包含一種或多種研磨劑。另外選擇性地，該一種或多種研磨劑之至少其中一種為二氧化矽。
選擇性地，口腔保健組成物進一步包含抗牙結石劑。另外選擇性地，該抗牙結石劑的含量為0.2重量%至0.8重量%，以組成物的總重量為基準。又另一選擇性地，該抗牙結石劑為焦磷酸四鈉和焦磷酸四鉀之至少其中一種。
本發明亦提供一種口腔保健組成物，用於減少或預防在口腔內形成生物膜。
本發明亦提供一種方法，用於減少或預防在口腔內形成生物膜，該方法包含使口腔與口腔保健組成物接觸。
本發明亦提供一種對口腔保健組成物中以下成分的組合之使用：(a)游離或鹽類形式的精胺酸；及(b)兩種或多種鋅鹽，其中該鋅鹽之至少一種為氧化鋅且該鋅鹽之至少一種為檸檬酸鋅；以用於減少或預防在口腔內形成生物膜。
選擇性地，氧化鋅對檸檬酸鋅的重量比例為1.5：1至4.5：1、1.5：1至4：1、1.7：1至2.3：1、1.9：1至2.1：1或約2：1。又，可使用基於此等重量比例的對應莫耳比例。
選擇性地，精胺酸在口腔保健組成物的含量為0.5重量%至10重量%，以組成物的總重量為基準。另外選擇性地，該精胺酸在口腔保健組成物的含量為0.5重量%至3重量%或1重量%至2.85重量%，以組成物的總重量為基準。又另外選擇性地，該精胺酸在口腔保健組成物中的含量為1.17重量%至2.25重量%，以組成物的總重量為基準。另外選擇性地，該精胺酸在口腔保健組成物中的含量為1.4重量%至1.6重量%，以組成物的總重量為基準。又另外選擇性地，該精胺酸在口腔保健組成物中的含量為約1.5重量%，以組成物的總重量為基準。
選擇性地，鋅鹽在口腔保健組成物中的總濃度為從0.2重量%至5重量%，以組成物的總重量為基準。
選擇性地，口腔保健組成物中精胺酸對所有鋅鹽的莫耳比例為0.05：1至10：1。又，可使用基於此等重量比例的對應莫耳比例。
選擇性地，氧化鋅在口腔保健組成物中的含量為0.5重量%至1.5重量%，而該檸檬酸鋅在口腔保健組成物中的含量為0.25重量%至0.75重量%，以組成物的總重量為基準。另外選擇性地，該氧化鋅在在口腔保健組成物中的含量為約1重量%，而該檸檬酸鋅在口腔保健組成物中的含量為約0.5重量%，以組成物的總重量為基準。
本發明之應用的其他部分將於以下提供的實施方式公開。應理解實施方式和特定實例雖然指出本發明的較佳實施例，但僅意圖用於例示，並未意圖限制本發明的範圍。
以下較佳實施例的說明其本質僅為例示，並未意圖限制本發明、其應用或用途。
如自始至終所使用的，範圍係用作描述該範圍內每一個值的簡略表達方式。範圍內的任何值皆可選作範圍的邊界。此外，上述所列的參考文獻全體皆通過引用結合到本說明書中。然而，若本公開之定義與引用的參考文獻之定義有所衝突，以本案所揭示為準。
除非另外說明，在此及規格中其他地方揭示的百分比和數量應理解為重量百分比。在此提供的數量係基於材料的有效重量。
如自始至終所使用的，「游離或鹽類形態的精胺酸」係指能夠以游離胺基酸或胺基酸鹽類形式存在的精胺酸。精胺酸的合適鹽類之實例包括但不限於精胺酸碳酸氫鹽、精胺酸磷酸鹽和精胺酸氫氯化物。
出人意料地，本發明人已發現將精胺酸加進包含包含鋅鹽的口腔保健組成物可增進口腔保健組成物在減少生物膜方面的功效。出人意料地，本發明人亦發現存在最佳的精胺酸濃度，藉此可大幅提升含鋅鹽的口腔保健組成物在減少生物膜方面的功效。
在第一態樣中，提供一種口腔保健組成物，包含：(a)游離或鹽類形式的精胺酸；及(b)兩種或多種鋅鹽，其中該鋅鹽之至少其中一種為氧化鋅且該鋅鹽之至少其中一種為檸檬酸鋅。
在某些具體實施例中，精胺酸在口腔保健組成物中的含量為0.5重量%至3重量%；0.75重量%至2.9重量%；1重量%至2.85重量%；1.17重量%至2.25重量%；1.3重量%至2重量%；1.4重量%至1.6重量%或約1.5重量%，以組成物的總重量為基準。
在上述具體實施例之任一者中，在口腔保健組成物中精胺酸對所有鋅鹽的莫耳比例可為0.05：1至10：1；0.08：1至5：1；0.1：1至1：1；0.4：1至0.8：1或約0.65：1。
可用於上述態樣之任一者的組成物中之合適鋅鹽的實例包括(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、檸檬酸鋅鈉及其混合物。在上述任一態樣中，一種或多種鋅鹽之至少一種可為氧化鋅。在組成物中，該鋅鹽之至少一種為氧化
鋅，而該鋅鹽之至少一種為檸檬酸鋅。在上述具體實施例之任一者中，鋅鹽在組成物中的總濃度可為0.2重量%至5重量%；0.5重量%至2.5重量%；0.8重量%至2重量%或1.5重量%，以組成物的總重量為基準。
在上述具體實施例之任一者中，組成物可包含含量為0.5重量%至1.5重量%的氧化鋅，及含量為0.25重量%至0.75重量%的檸檬酸鋅，以組成物的總重量為基準。或者，組成物可包含含量為0.75重量%至1.25重量%的氧化鋅，及含量為0.4重量%至0.6重量%的檸檬酸鋅，以組成物的總重量為基準。或者，組成物可包含含量為約1重量%的氧化鋅，及含量為約0.5重量%的檸檬酸鋅，以組成物的總重量為基準。
在上述具體實施例之任一者中，口腔保健組成物可進一步包含一種或多種研磨劑。可包括在組成物中的合適研磨劑包括但不限於：二氧化矽研磨劑、氧化鋁、矽酸鋁、煅燒氧化鋁、皂土、其他矽質材料、不溶磷酸鹽、天然碳酸鈣(NCC)、沈積碳酸鈣(PCC)及其混合物。在某些具體實施例中，一種或多種研磨劑的至少一種為二氧化矽研磨劑。二氧化矽研磨劑的實例包括但不限於平均粒徑最大達約20微米的沈積或水合二氧化矽，(例如Zeodent 105和Zeodent 114，銷售者：J.M.Huber Chemicals Division,Havre de Grace,Md.21078)；Sylodent 783(銷售者：Davison Chemical Division of W.R.Grace & Company)或Sorbosil AC 43(來源：PQ Corporation)。在某些具體實施例中，一種或多種研磨劑的至少其中一種為碳酸鈣研磨劑，例如沈積碳酸鈣(PCC)或天然碳酸鈣(NCC)。
在上述具體實施例之任一者中，組成物可進一步包含抗牙結石(牙垢控制)劑。合適的抗牙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、二磷酸鹽，例如氮雜環烷烴-2,2-二磷酸鹽(例如氮雜環庚烷-2,2-二磷酸)、N-甲基氮雜環戊烷-2,3-二磷酸、乙烷-1-羥基-1,1-二磷酸(EHDP)和乙烷-1-胺基-1,1-二磷酸鹽、膦醯基烷羧酸及其混合物。有用的無機磷酸鹽和聚磷酸鹽包括磷酸單鈉、磷酸二鈉、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。其他有用的牙垢控制劑包括聚羧酸聚合物和聚乙烯甲基醚/馬來酐(PVM/MA)共聚物，例如GANTREZ®。在某些實施例中，抗牙結石劑為焦磷酸四鈉和焦磷酸四鉀之
至少其中一種。在某些實施例中，抗牙結石劑在組成物中的含量為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%，以組成物的總重量為基準。
在上述實施例的任一者中，口腔保健組成物可為潔牙劑、牙膏、凝膠、牙粉、漱口水、口腔清洗劑、錠劑、片劑、噴劑、樹膠或薄膜。在某些實施例中，口腔保健組成物為牙膏、膠體或牙粉。
在第二態樣中，本發明提供一種根據上述任何具體實施例之口腔保健組成物，用於減少或預防在口腔內形成生物膜。
在第三態樣中，本發明提供一種用於減少或預防在口腔內形成生物膜之方法，該方法包含使口腔與根據上述任何具體實施例之口腔保健組成物接觸。
在第四態樣中，本發明提供一種口腔保健組成物之用途，其組合：(a)游離或鹽類形式的精胺酸；及(b)兩種或多種鋅鹽，其中該鋅鹽之至少一種為氧化鋅且該鋅鹽之至少其中一種為檸檬酸鋅；以用於減少或預防在口腔內形成生物膜。
根據第四態樣，口腔保健組成物可為根據上述第一態樣所述之組成物的任何具體實施例。
口腔保健組成物可進一步包含其他成分。此等其他成分可包括但不限於稀釋劑、碳酸氫鹽、pH改良劑、介面活性劑、泡沫調節劑、增稠劑、保濕劑、甜味劑、調味劑、顏料、其他抗菌劑、抗齲齒劑及其混合物。
在某些具體實施例中，口腔保健組成物包含至少一種碳酸氫鹽，其會發泡並釋放二氧化碳，因此例如可帶給牙齒和牙齦清潔的感覺。可使用任何口用碳酸氫鹽，包括但不限於鹼金屬碳酸氫鹽，例如碳酸氫鈉和碳酸氫鉀、碳酸氫銨等。選擇性地，一種或多種其他碳酸氫鹽的總含量為約0.1重量%至約50重量%，例如約1重量%至20重量%(以組成物的總重量為基準)。
在某些具體實施例中，口腔保健組成物包含至少一種pH改良劑。此等藥劑包含酸化劑以降低pH、幫含鹼化劑以提高pH並包含緩衝劑以便將pH控制在一定範圍內。例如，可加入選自酸化劑、鹼化劑和緩衝
劑的一種或多種化合物以提供2至10的pH，或者在各種例示實施例中，提供2至8、3至9、4至8、5至7、6至10、7至9等。可使用任何口用pH改良劑，包括但不限於羧酸、磷酸和磺酸、酸鹽(例如檸檬酸單鈉、檸檬酸二鈉和蘋果酸單鈉等)、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(例如磷酸單鈉和磷酸三鈉)、咪唑等。選擇性地，一種或多種pH改良劑以可有效將組成物維持在口用pH範圍內的總含量存在。
口腔保健組成物亦可包含至少一種介面活性劑。可使用任何口用介面活性劑，其中大多數為陰離子型、非離子型或兩性。合適的陰離子型介面活性劑包括但不限於C8-20烷基硫酸鹽的水溶性鹽類、C8-20脂肪酸的磺酸化單甘油酯、肌胺酸鹽、牛磺酸鹽等。此等及其他類別的例示實例包括十二烷基硫酸鈉、椰油酸單甘油酯硫酸鈉、十二烷基肌胺酸鈉、十二烷基異乙二磺酸鈉、十二酯羧酸鈉和十二烷基苯磺酸鈉。合適的非離子型介面活性劑包括但不限於泊洛沙姆(poloxamers)、聚氧乙烯山梨醇酯、脂肪醇乙氧基化物、烷基酚乙氧基化物、叔胺氧化物、叔膦氧化物(tertiary phosphine oxides)、二烷基亞碸等。合適的兩性介面活性劑包括但不限於具有陰離子基團例如羧酸根、硫酸根、磺酸根、磷酸根或膦酸根的C8-20脂肪族仲胺和叔胺的衍生物。可使用甜菜鹼，合適的實例是椰油胺基丙基甜菜鹼。選擇性地，一種或多種介面活性劑的總含量為約0.01重量%至約10重量%，例如約0.05重量%至約5重量%或者從約0.1重量%至約2重量%，以組成物的總重量為基準。
口腔保健組成物可包含至少一種泡沫調節劑，可用於例如增加組成物受攪拌時所產生的泡沫之數量、厚度或穩定度。可使用任何口用的泡沫調節劑，包括但不限於聚乙二醇，亦稱為聚氧乙烯。高分子量聚乙二醇為合適者，包括具有平均分子量200,000至7,000,000者，例如500,000至5,000,000或1,000,000至2,500,000。選擇性地，一種或多種聚乙二醇的總含量為約0.1重量%至約10重量%，例如約0.2重量%至約5重量%，或約0.25重量%至約2重量%，以組成物的總重量為基準。
口腔保健組成物可包含至少一種增稠劑，用於例如給予組成物所需的一致性及/或口感。可使用任何口用的增稠劑，包括但不限於卡
波姆(carbomers)，亦稱為聚羧乙烯聚合物；鹿角菜膠，亦稱為愛爾蘭苔癬，更特定者為ι-鹿角菜膠(I型鹿角菜膠)；纖維素聚合物，例如羥乙基纖維素、羧甲基纖維素及其鹽類，例如羧甲基纖維素鈉；天然樹膠，例如刺梧桐膠、黄原膠(xanthan)、阿拉伯膠、黃蓍膠、膠狀矽酸鋁鎂和膠狀二氧化矽等。較佳的增稠劑或膠化劑之類別為與季戊四醇的烷基醚、乳糖的烷基醚或卡波姆(carbomers)交聯之丙烯酸的均聚物類別。可從B.F.Goodrich的Carbopol®系列取得市售的卡波姆(carbomers)。特佳的Carbopol系列包括Carbopol 934、940、941、956、974P及其混合物。可使用DT 267(來源：PPG Industries)等二氧化矽增稠劑。選擇性地，一種或多種增稠劑的總含量為約0.01%至約15%，例如約0.1重量%至約10%，或約0.2%至約5%，以組成物的總重量為基準。
組成物可包含至少一種黏度改良劑，可用於例如協助防止成分沈澱或分離，或者提升液體組成物受攪拌時的重分散性。可使用任何口用黏度改良劑，包括但不限於礦物油、凡士林、黏土和有機改良黏土、二氧化矽等。選擇性地，一種或多種黏度改良劑的總含量為約0.01重量%至約10重量%，例如約0.1重量%至約5重量%，以組成物的總重量為基準。
組成物亦可包含至少一種保濕劑。可使用任何口用保濕劑，包括但不限於多元醇，例如甘油、山梨醇(選擇性地為溶於水中的70重量%溶液)、木糖醇或低分子量聚乙二醇。大多數保濕劑亦作為甜味劑。選擇性地，一種或多種保濕劑的總含量為約1重量%至約70重量%，例如約1重量%至約50重量%、約2重量%至約25重量%、或約5重量%至約15重量%，以組成物的總重量為基準。
口腔保健組成物可包含至少一種甜味劑，可用於例如提升組成物的味道。選擇性地，一種或多種甜味劑的總含量主要按照所選的特定甜味劑而定，但通常為0.005重量%至5重量%，以組成物的總重量為基準，選擇性地為0.005重量%至0.2重量%，另外選擇性地為0.05重量%至0.1重量%，以組成物的總重量為基準。
組成物亦可包含至少一種調味劑，可用於例如提升組成物的味道。可使用任何口用天然或合成調味劑，包括但不限於茶香、香草精、鼠尾草、馬鬱蘭、洋芹油、綠薄荷油、肉桂油、冬青油(水楊酸甲酯)、薄荷
油、丁香油、月桂油、茴香油、桉樹油、柑橘油、水果油和精油(包括來自檸檬、柳橙、萊姆、葡萄柚、杏、香蕉、葡萄、蘋果、草莓、櫻桃、鳳梨等)、來自豆類和堅果的香味(例如咖啡、可可、可樂果、花生和杏仁等)、吸附或包囊化的香等。在此香料亦包括在口中提供香味及/或其他感官效果(包括涼爽或溫暖效果)的成分。此種成分說明性地包括薄荷醇、乙酸薄荷酯、乳酸薄荷酯、樟腦、桉樹油、桉樹腦、茴香腦、丁香酚、肉桂(cassia)、口惡酮(oxanone)、α-紫羅蘭酮、丙烯基乙基愈創木酚(propenyl guaiethol)、百里酚、沈香醇、苯甲醛、肉桂醛、N-乙基-對-薄荷燒-3-羧胺、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)等。選擇性地，一種或多種香料的總含量為約0.01重量%至約5重量%，例如約0.03重量%至約2.5重量%，選擇性地為約0.05重量%至約1.5重量%，另外選擇性地為約0.1重量%至約0.3重量%，以組成物的總重量為基準。
組成物可包含至少一種增色劑。在此增色劑包含顏料、染料、色澱和給予特定光澤或反射性的珠光劑等藥劑。可使用任何口用增色劑，包括但不限於滑石、雲母、碳酸鎂、矽酸鎂、矽酸鋁鎂、二氧化鈦、紅色、黃色、棕色和黑色氧化鐵、亞鐵氰化鐵銨(ferric ammonium ferrocyanide)、錳紫、天青石(ultramarine)、雲母鈦、氯氧化鉍等。選擇性地，一種或多種增色劑的總含量為約0.001重量%至約20重量%，例如約0.01重量%至約10重量%，或約0.1重量%至約5重量%，以組成物的總重量為基準。
組成物亦可包含其他抗菌劑或防腐劑，例如氯己定(chlorhexidine)、三氯沙(triclosan)、四級銨化合物(例如氯化芐二甲烴銨)或對羥基苯甲酸酯，例如甲基對羥基苯甲酸酯或丙基對羥基苯甲酸酯。選擇性地，一種或多種其他抗菌劑或防腐劑在組成物中的含量可為約0.01重量%至約0.5重量%，選擇性地為約0.05重量%至約0.1重量%，以組成物的總重量為基準。
口腔保健組成物亦可包含氯離子來源。氯離字來源包括但不限於：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(olaflur)(N’-十八烷基三亞
甲基二胺-N,N,N’-三(2-乙醇)-二氫氟化物)、氟化銨及其組合。在某些實施例中，氟離子來源包括氟化亞錫、氟化鈉、氟化胺、單氟磷酸鈉及其混合物。在某些實施例中，口腔保健組成物亦可包含氟離子來源或氟提供成分，其含量足以提供約50至約5000ppm的氟離子，例如約100至約1000，約200至約500，或約250ppm的氟離子。可將含量為約0.001重量%至約10重量%(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%)的氟離子來源加入組成物。然而，應理解可提供適當氟離子量的氟鹽重量將隨鹽類中的逆離子重量而有明顯差異，而本領域技術人員可快速決定此含量。較佳的氟鹽可為氟化鈉。
組成物可包含唾液刺激劑，可用於例如改善口腔乾燥的情況。可使用任何口用唾液刺激劑，包括但不限於檸檬酸、乳酸、蘋果酸、琥珀酸、抗壞血酸、己二酸、反丁烯二酸、酒石酸及其混合物等食物酸。選擇性地，一種或多種唾液刺激劑以有效刺激唾液的總含量而存在。
組成物可包含抗敏感劑，例如硝酸鉀、碳酸氫鉀、氯化鉀、檸檬酸鉀和草酸鉀等鉀鹽；辣椒素；丁香酚；鍶鹽；氯鹽及其組合。可加入有效量的此種試劑，例如從約1重量%至約20重量%(以組成物的總重量為基準)，隨所選藥劑而有所不同。
組成物可進一步包含抗氧化劑。可使用任何口用抗氧化劑，包括丁基羥基甲氧苯(BHA)、二丁基羥基甲苯(BHT)、維生素A、類胡蘿蔔素、維生素E、類黃酮、多酚、抗壞血酸、藥草抗氧化劑、葉綠素、褪黑激素及其混合物。
進行實驗以評估包含不同濃度精胺酸的組成物減少生物膜的功效。
在以下所有實例中，所使用的實驗方法為曼徹斯特大學的生物膜增長抑制模型。此模型的內容如下：
(1)從四名健康的志願者收集牙菌斑並匯集成接種源。接種源的光學密度對應到0.3吸光度(610奈米)。
(2)在24格微量培養板中加入1毫升消毒過的合成唾液(含0.01重量%乳糖)
和1毫升匯集之唾液，將消毒過的氫氧磷灰石圓片浸於其中並在37℃的無氧環境下培養24小時。
(3)針對每一個測試潔牙劑(及每一個控制組)，將潔牙劑和無菌蒸餾水以1：2的重量比例混合以製備處理溶液。將每一個新製備的處理溶液加進3個格，並接觸氫氧磷灰石圓片10分鐘。
(4)然後，移除每一格的液體，並替換成2毫升消毒過的合成唾液。
(5)再者，將圓片保存在37℃的無氧環境下8天。
(6)間隔2、4和8天，在無菌環境下收集圓片並移至半強度預還原巰基乙酸培養基(每一圓片4.5毫升)。
(7)針對每一個圓片，在用於所有格蘭氏陰性厭氧菌的新黴素/萬古黴素之藻膠上，使用100微升的稀釋液10-4、10-5和10-6以一式兩份進行鋪板。
(8)在無氧環境下使用消毒過的推刮器，將稀釋液在藻膠培養基表面均勻地推開，然後在37℃下培養72小時，再計算每一個培養皿表面的菌落數量。
計算每一個測試潔牙劑或控制組的log10 CFU/毫升(其中CFU=菌落形成單位)。較低的log10 CFU/毫升表示所測試的潔牙劑在防止生物膜增長方面具有較大功效。
測試結果如以下實例1所示。
在第一回生物膜減少測試中，評估表1所列的配方瞭解減少生物膜增長的功效。使用上述曼徹斯特大學的生物膜增長抑制模型方法所獲得的結果如表1所示，其中平均log10 CFU/毫升係來自按照本方法的步驟6培養8天的圓片。以下結果中，在「統計顯著性」具有相同字母的配方，在生物膜減少功效方面並未出現明顯差別。
Claims (3)
- 一種口腔保健組成物，包含：a.游離或鹽類形式的精胺酸，其中該精胺酸的含量為1.5重量%，以組成物的總重量為基準；及b.氧化鋅和檸檬酸鋅，其中氧化鋅的含量為1重量%，且檸檬酸鋅的含量為0.5重量%，以組成物的總重量為基準。
- 一種根據請求項1所述之口腔保健組成物，其用於減少或預防在口腔內形成生物膜。
- 一種口腔保健組成物用於製造減少或預防在口腔內形成生物膜的藥物的用途，其中該口腔保健組成物包含a.游離或鹽類形式的精胺酸，其中該精腔酸在口腔保健組成物中的含量為1.5重量%，以組成物的總重量為基準；及b.氧化鋅和檸檬酸鋅，其中氧化鋅在口腔保健組成物中的含量為1重量%，且檸檬酸鋅在口腔保健組成物中的含量為0.5重量%，以組成物的總重量為基準。
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