TWI576115B - 口腔保健組成物 - Google Patents
口腔保健組成物 Download PDFInfo
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- TWI576115B TWI576115B TW102147093A TW102147093A TWI576115B TW I576115 B TWI576115 B TW I576115B TW 102147093 A TW102147093 A TW 102147093A TW 102147093 A TW102147093 A TW 102147093A TW I576115 B TWI576115 B TW I576115B
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- 239000000203 mixture Substances 0.000 title claims description 168
- -1 fluoride ions Chemical class 0.000 claims description 31
- IUTCEZPPWBHGIX-UHFFFAOYSA-N tin(2+) Chemical compound [Sn+2] IUTCEZPPWBHGIX-UHFFFAOYSA-N 0.000 claims description 31
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 31
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 claims description 17
- 239000003795 chemical substances by application Substances 0.000 claims description 16
- 230000036541 health Effects 0.000 claims description 16
- TXUICONDJPYNPY-UHFFFAOYSA-N (1,10,13-trimethyl-3-oxo-4,5,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl) heptanoate Chemical compound C1CC2CC(=O)C=C(C)C2(C)C2C1C1CCC(OC(=O)CCCCCC)C1(C)CC2 TXUICONDJPYNPY-UHFFFAOYSA-N 0.000 claims description 10
- 229910021626 Tin(II) chloride Inorganic materials 0.000 claims description 10
- 244000005700 microbiome Species 0.000 claims description 10
- 239000001119 stannous chloride Substances 0.000 claims description 10
- 235000011150 stannous chloride Nutrition 0.000 claims description 10
- PTFCDOFLOPIGGS-UHFFFAOYSA-N Zinc dication Chemical compound [Zn+2] PTFCDOFLOPIGGS-UHFFFAOYSA-N 0.000 claims description 8
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 8
- 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 8
- 239000011746 zinc citrate Substances 0.000 claims description 8
- 235000006076 zinc citrate Nutrition 0.000 claims description 8
- 229940068475 zinc citrate Drugs 0.000 claims description 8
- 239000011787 zinc oxide Substances 0.000 claims description 8
- 239000003755 preservative agent Substances 0.000 claims description 7
- 208000006558 Dental Calculus Diseases 0.000 claims description 6
- NROKBHXJSPEDAR-UHFFFAOYSA-M potassium fluoride Chemical compound [F-].[K+] NROKBHXJSPEDAR-UHFFFAOYSA-M 0.000 claims description 6
- YXTDAZMTQFUZHK-ZVGUSBNCSA-L (2r,3r)-2,3-dihydroxybutanedioate;tin(2+) Chemical compound [Sn+2].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O YXTDAZMTQFUZHK-ZVGUSBNCSA-L 0.000 claims description 5
- CKUJRAYMVVJDMG-IYEMJOQQSA-L (2r,3s,4r,5r)-2,3,4,5,6-pentahydroxyhexanoate;tin(2+) Chemical compound [Sn+2].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O CKUJRAYMVVJDMG-IYEMJOQQSA-L 0.000 claims description 5
- GEZAUFNYMZVOFV-UHFFFAOYSA-J 2-[(2-oxo-1,3,2$l^{5},4$l^{2}-dioxaphosphastannetan-2-yl)oxy]-1,3,2$l^{5},4$l^{2}-dioxaphosphastannetane 2-oxide Chemical compound [Sn+2].[Sn+2].[O-]P([O-])(=O)OP([O-])([O-])=O GEZAUFNYMZVOFV-UHFFFAOYSA-J 0.000 claims description 5
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims description 5
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims description 5
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 5
- 150000002500 ions Chemical class 0.000 claims description 5
- ZVVSSOQAYNYNPP-UHFFFAOYSA-N olaflur Chemical compound F.F.CCCCCCCCCCCCCCCCCCN(CCO)CCCN(CCO)CCO ZVVSSOQAYNYNPP-UHFFFAOYSA-N 0.000 claims description 5
- 229960001245 olaflur Drugs 0.000 claims description 5
- COALSIYJQHMCDX-UHFFFAOYSA-L propanedioate;tin(2+) Chemical compound [Sn+2].[O-]C(=O)CC([O-])=O COALSIYJQHMCDX-UHFFFAOYSA-L 0.000 claims description 5
- 229960004711 sodium monofluorophosphate Drugs 0.000 claims description 5
- 229940007163 stannous tartrate Drugs 0.000 claims description 5
- OQBLGYCUQGDOOR-UHFFFAOYSA-L 1,3,2$l^{2}-dioxastannolane-4,5-dione Chemical compound O=C1O[Sn]OC1=O OQBLGYCUQGDOOR-UHFFFAOYSA-L 0.000 claims description 4
- USYAMXSCYLGBPT-UHFFFAOYSA-L 3-carboxy-3-hydroxypentanedioate;tin(2+) Chemical compound [Sn+2].OC(=O)CC(O)(C([O-])=O)CC([O-])=O USYAMXSCYLGBPT-UHFFFAOYSA-L 0.000 claims description 4
- PNOXNTGLSKTMQO-UHFFFAOYSA-L diacetyloxytin Chemical compound CC(=O)O[Sn]OC(C)=O PNOXNTGLSKTMQO-UHFFFAOYSA-L 0.000 claims description 4
- 239000011775 sodium fluoride Substances 0.000 claims description 4
- 235000013024 sodium fluoride Nutrition 0.000 claims description 4
- 229960000414 sodium fluoride Drugs 0.000 claims description 4
- DDFHBQSCUXNBSA-UHFFFAOYSA-N 5-(5-carboxythiophen-2-yl)thiophene-2-carboxylic acid Chemical compound S1C(C(=O)O)=CC=C1C1=CC=C(C(O)=O)S1 DDFHBQSCUXNBSA-UHFFFAOYSA-N 0.000 claims description 3
- 230000000844 anti-bacterial effect Effects 0.000 claims description 3
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims description 3
- 235000011180 diphosphates Nutrition 0.000 claims description 3
- FXNRKXSSLJKNGH-UHFFFAOYSA-L dipotassium;fluoro-dioxido-oxo-$l^{5}-phosphane Chemical compound [K+].[K+].[O-]P([O-])(F)=O FXNRKXSSLJKNGH-UHFFFAOYSA-L 0.000 claims description 3
- 229940091249 fluoride supplement Drugs 0.000 claims description 3
- 239000011698 potassium fluoride Substances 0.000 claims description 3
- 235000003270 potassium fluoride Nutrition 0.000 claims description 3
- FQENQNTWSFEDLI-UHFFFAOYSA-J sodium diphosphate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]P([O-])(=O)OP([O-])([O-])=O FQENQNTWSFEDLI-UHFFFAOYSA-J 0.000 claims description 3
- 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 claims description 3
- 235000019818 tetrasodium diphosphate Nutrition 0.000 claims description 3
- 239000006071 cream Substances 0.000 claims description 2
- SAEOCANGOMBQSP-UHFFFAOYSA-N diazanium;fluoro-dioxido-oxo-$l^{5}-phosphane Chemical compound [NH4+].[NH4+].[O-]P([O-])(F)=O SAEOCANGOMBQSP-UHFFFAOYSA-N 0.000 claims description 2
- DYAGUJVEJROVAL-UHFFFAOYSA-N ethyl N-ethylcarbamoperoxoate Chemical compound C(C)NC(OOCC)=O DYAGUJVEJROVAL-UHFFFAOYSA-N 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 239000002324 mouth wash Substances 0.000 claims description 2
- 229940051866 mouthwash Drugs 0.000 claims description 2
- 239000002674 ointment Substances 0.000 claims description 2
- 239000000606 toothpaste Substances 0.000 claims description 2
- 229940034610 toothpaste Drugs 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 239000001509 sodium citrate Substances 0.000 claims 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims 1
- 239000010455 vermiculite Substances 0.000 description 13
- 229910052902 vermiculite Inorganic materials 0.000 description 13
- 235000019354 vermiculite Nutrition 0.000 description 13
- 239000003082 abrasive agent Substances 0.000 description 8
- 229920001223 polyethylene glycol Polymers 0.000 description 7
- 150000003839 salts Chemical class 0.000 description 7
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 description 6
- 235000003599 food sweetener Nutrition 0.000 description 6
- 230000000813 microbial effect Effects 0.000 description 6
- 239000003765 sweetening agent Substances 0.000 description 6
- 239000002562 thickening agent Substances 0.000 description 6
- 229910019142 PO4 Inorganic materials 0.000 description 5
- 239000000796 flavoring agent Substances 0.000 description 5
- 239000003921 oil Substances 0.000 description 5
- 235000019198 oils Nutrition 0.000 description 5
- 235000021317 phosphate Nutrition 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- RRAFCDWBNXTKKO-UHFFFAOYSA-N eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 description 4
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- 229920000642 polymer Polymers 0.000 description 4
- 210000003296 saliva Anatomy 0.000 description 4
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- 239000004094 surface-active agent Substances 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical class OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 description 3
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- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
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- 238000010521 absorption reaction Methods 0.000 description 3
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- 235000006708 antioxidants Nutrition 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
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- PHIQHXFUZVPYII-ZCFIWIBFSA-N (R)-carnitine Chemical compound C[N+](C)(C)C[C@H](O)CC([O-])=O PHIQHXFUZVPYII-ZCFIWIBFSA-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
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Description
本發明係關於具有高含水量之口腔保健組成物，其具有改良之強健性向微生物挑戰。該口腔保健組成物係包括含有由0.125重量%至0.75重量%水溶性亞錫離子來源之組成物，其中，該組成物包含至少50重量%水，且其中該亞錫離子之來源係選自於下列之基團，包括：氯化亞錫、焦磷酸亞錫、甲酸亞錫、醋酸亞錫、葡糖酸亞錫、乳酸亞錫、酒石酸亞錫、草酸亞錫、丙二酸亞錫、檸檬酸亞錫、亞錫伸乙基過氧化脲，及其混合物。
具有高含水量之組成物傾向於支持微生物之生存與生長。這個問題亦發生於具有高含水量之口腔保健組成物中。因此，常常將防腐劑如苄醇、甲基對羥苯甲酸酯、丙基對羥苯甲酸酯添加至口腔保健組成物中，以便提高其等之強健性向微生物挑戰。
然而，仍需要具有改良之強健性對抗微生物攻擊，而不需要防腐劑存在於該組成物中之口腔保健組成物。
本發明之第一方面係提供水性口腔保健組成物，其包含由0.125重量%至0.75重量%之水溶性亞錫離子來源，其中，該組成物包含至少50重量%水，且其中該亞錫離子之來源係選自於下列之基團，包括：氯
化亞錫、焦磷酸亞錫、甲酸亞錫、醋酸亞錫、葡糖酸亞錫、乳酸亞錫、酒石酸亞錫、草酸亞錫、丙二酸亞錫、檸檬酸亞錫、亞錫伸乙基過氧化脲，及其混合物。
任意地，該組成物包含由0.125重量%至0.75重量%該亞錫離子之來源。
任意地，該組成物包含由0.125重量%至0.5重量%該亞錫離子之來源。
任意地，該組成物包含由0.125重量%至0.35重量%該亞錫離子之來源。
任意地，該組成物包含由0.15重量%至0.3重量%該亞錫離子之來源。
任意地，該亞錫離子之來源為氯化亞錫。
任意地，該組成物包含由50重量%至65重量%水。
任意地，該組成物包含由52重量%至60重量%水。
任意地，該組成物包含由54重量%至55重量%水。
任意地，該組成物進一步包含氟化物離子來源選自於下列之基團，包括：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、氟化銨，及其組成物。
任意地，該組成物進一步包含鋅離子之來源。
任意地，該鋅離子之來源包含氧化鋅、檸檬酸鋅，或其混合物。
任意地，該組成物包含檸檬酸鋅以由0%至1.5%之數量，較佳1.5重量%至2.5重量%。
任意地，該組成物包含氧化鋅以由0%至1.5%之數量，較佳0.5重量%至1.5重量%。
任意地，該組成物為牙膏、牙凝膠、漱口劑、乳膏或軟膏。
任意地，該組成物係不含附加之防腐劑。
本發明亦提供如上所述之口腔保健組成物，其具有向微生物挑戰之改良的強健性。
於第二方面中，本發明係提供水溶性亞錫離子之來源用於改進強健性向微生物挑戰之含有至少50重量%水之口腔保健組成物中，其中，該亞錫離子之來源係以濃度由0.1重量%至0.75重量%存在於該口腔保健組成物中，且其中該亞錫離子之來源係選自於下列之基團，包括：氯化亞錫、焦磷酸亞錫、甲酸亞錫、醋酸亞錫、葡糖酸亞錫、乳酸亞錫、酒石酸亞錫、草酸亞錫、丙二酸亞錫、檸檬酸亞錫、亞錫伸乙基過氧化脲，及其混合物。
任意地，該組成物包含由0.15重量%至0.3重量%該亞錫離子之來源。
任意地，該亞錫離子之來源為氯化亞錫。
任意地，該組成物包含由50重量%至60重量%水。
本案發明人業已令人驚奇地發現，亞錫離子之來源以濃度0.1重量%至0.75重量%添加至高含水量之水性口腔保健組成物(至少50重量%含水量)可大大地提高該組成物之強健性向微生物挑戰，與不含亞錫離子來源或負責防腐之任何其他化學試劑之組成物相較時。
應瞭解，雖然本發明之較佳具體例指明，該詳細說明及特定實例僅意欲用於闡明之目的且並非意欲用來限制本發明之範圍。
如全文中所使用者，範圍係以簡略方式使用來說明該範圍內之各個及每一個數值。於該範圍內之任何數值可選擇作為該範圍之終點。
如本文中所用之"較佳之"及"較佳地"各詞係指本發明之具體例於某些情況下給予之特定利益。然而，其他具體例亦可於相同或其他情況下為較佳者。此外，詳述一種或多種較佳之具體例並非意指其他具體
例不可用，且並非意欲將其他具體例從本發明之範圍中排除。
如本文中所用之"約"一詞，當應用於本發明之組成物或方法之參數值時，表示該值之計算或測量於該組成物或方法之化學或物理屬性上容許一些不具重大影響之輕微不精確性。若，由於某種原因，以"約"所提供之不精確性並非另有於此方面技藝中所理解之一般意義，則如本文中所用之"約"係表示於該值中可能之變化多至5%。
如本文所指者，所有組成物之百分比係按該組成物之總重量計，除非另有指示。如本文中所指者，“ppm”(每百萬份)係指ppm按重量計，除非另有指示。如本文中所指者，所有的比率係指重量比，除非另有指示。
於一方面中，本發明係提供水性口腔保健組成物，其包含由約0.125重量%至約0.75重量%水溶性亞錫離子之來源，其中，該組成物包含至少50重量%水，且其中該亞錫離子之來源係選自於下列之基團，包括：氯化亞錫、焦磷酸亞錫、甲酸亞錫、醋酸亞錫、葡糖酸亞錫、乳酸亞錫、酒石酸亞錫、草酸亞錫、丙二酸亞錫、檸檬酸亞錫、亞錫伸乙基過氧化脲，及其混合物。或者，亞錫離子整個施用之數量可直接參考，例如約0.125重量%至約0.75重量%氯化亞錫(SnCl2)係關係到約0.080重量%至約0.47重量%亞錫離子。
於某些具體例中，該組成物包含由約0.15重量%至約0.75重量%該亞錫離子之來源，任意由約0.15重量%至約0.5重量%該亞錫離子之來源。
於某些具體例中，該組成物包含由0.15重量%至0.3重量%該亞錫離子之來源，任意由0.20重量%至0.25重量%該亞錫離子之來源。
於某些具體例中，該組成物包含由0.3重量%至0.5重量%該亞錫離子之來源，任意地0.35重量%至0.45重量%該亞錫離子之來源。
於某些具體例中，該亞錫離子之來源為氯化亞錫(SnCl2)。
本發明之口腔保健組成物為水性，且包含至少50重量%水。
於某些具體例中，該口腔保健組成物包含由50重量%至65重量%水，任意由52重量%至60重量%水，進一步任意由54重量%至55重量%水。於某些具體例中，該口腔保健組成物包含由50重量%至60重量%水。
於某些具體例中，本發明之口腔保健組成物進一步包含氟化物離子來源選自於下列之基團，包括：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、氟化銨，及其組合物。氟化胺之一個實例為歐拉氟(Olaflur)(N'-十八基三亞甲基二胺-N,N,N'-三(2-乙醇)-二氫氟化物)。
於特定具體例中，該氟化物離子來源包括氟化鈉、氟化胺、單氟磷酸鈉，以及其混合物。較佳之氟化物鹽可為單氟磷酸鈉。
於特定具體例中，本發明之口腔保健組成物可含有氟化物離子來源或提供氟之組成份，以足夠供應約50至約5000ppm氟化物離子之數量，例如，由約100至約1000，由約200至約500，或約250ppm氟化物離子。氟化物離子來源可添加至本發明之組成物，以約0.001重量%至約10重量%之含量，例如，由約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，應理解用來提供適當氟化物離子含量之氟化物鹽的重量將明顯地根據該鹽中之平衡離子的重量而變化，且精於此方面技藝之人士可容易地測定此等數量。
於某些具體例中，本發明之口腔保健組成物進一步包含鋅離子之來源。一種或多種此等來源可以存在。一種或多種鋅離子來源可按該組成物之總重量，以由約0.05重量%至約3重量%之總數量存在，例如由約0.1重量%至約1重量%。
適當之鋅離子來源包括但非侷限於醋酸鋅、檸檬酸鋅、葡糖酸鋅、甘胺酸鋅、氧化鋅、硫酸鋅、檸檬酸鋅鈉及其混合物。
於特定具體例中，該鋅離子之來源包含氧化鋅(ZnO)、檸檬酸鋅，或其混合物。於某些具體例中，該組成物包含檸檬酸鋅以由1.5重量
%至2.5重量%之數量，任意地以由1.75重量%至2.25重量%之數量。替代地或另外地，該組成物可包含氧化鋅以由0.5重量%至1.5重量%之數量，任意地以由0.75重量%至1.25重量%之數量。
於某些具體例中，本發明之口腔保健組成物可包含一種或多種試劑選自於磨蝕劑、稀釋劑、碳酸氫鹽、pH調節劑、表面活化劑、泡沫調製劑、增稠劑、黏度調節劑、濕潤劑、甜味劑、香味劑、顏料、抗細菌劑、抗齲齒劑、抗結石或牙垢控制劑，及其混合物。
於某些具體例中，本發明之組成物進一步包含至少一種磨蝕劑。
磨蝕矽石係不同於增稠矽石。通常，磨蝕(清潔)矽石可具有特徴如具有油吸收含量約40至150cc/100克且具有3或更大毫克耗損/100,000旋轉之艾勒內爾磨損(Einlehner abrasion)，而增稠磨蝕劑具有油吸收含量大於150cc/100克且具有艾勒內爾磨損小於2毫克耗損/100,000旋轉。
可使用之磨蝕劑包括矽石磨蝕劑如具有平均粒子大小多至約20微米之沉澱或水合矽石，如矽歐頓(Zeodent)103、105、113、114、115，或124，由J.M.胡柏化學品部門銷售(J.M.Huber Chemicals Division,Havre de Grace,Md.21078)，塞洛頓(Sylodent)783，由W.R.葛蕾絲公司大維森化學部門銷售(Davison Chemical Division of W.R.Grace & Company)，索波絲(Sorbosil)AC 43來自於PQ公司，及其混合物。其他有用的潔牙劑磨蝕劑包括氧化鋁、矽酸鋁、煅燒礬土、膨潤土或其他矽質材料、不溶磷酸鹽、碳酸鈣，及其混合物。
其他可能之磨蝕材料包括具有油吸收值小於約100cc/100克矽石且任意於範圍由約45cc/100克至小於70cc/100克矽石之矽膠及沉澱無定形矽石。此等矽石為具有平均粒子大小於範圍由3微米至12微米，且任意於5至10微米之膠體粒子。
該磨蝕劑或磨蝕劑之混合物可根據該組成物之重量，以由5至35重量%，任意根據該組成物之重量由10至20重量%之數量存在。該磨蝕劑或磨蝕劑之混合物可根據該組成物之重量，以由12至17重量%之數量存在。
於特定具體例中，該組成物可不含磨蝕劑。
於某些具體例中，本發明之口腔保健組成物包含至少一種碳酸氫鹽，其有用於，例如賦予牙齒及牙齦“乾淨的感覺，由於二氧化碳起泡及釋放。可使用任何口腔可接受之碳酸氫鹽，包括但非侷限於，鹼金屬碳酸氫鹽如碳酸氫鈉及碳酸氫鉀、碳酸氫銨及類似物。一種或多種碳酸氫鹽係按該組成物之總重量，任意地以約0.1重量%至約50重量%之總數量存在，例如約0.5重量%至20重量%或1重量%至10重量%。
於某些具體例中，本發明之組成物包含至少一種pH調節劑。此等試劑包括酸化劑以降低pH，鹼化劑以提升pH，及緩衝劑以控制pH於想要之範圍內。例如，可包括一種或多種化合物選自於酸化、鹼化及緩衝劑以提供2至10之pH，或於多種闡明性具體例中，2至8、3至9、4至8、5至7、6至10、7至9等。可使用任何口腔可接受之pH調節劑，包括但非侷限於，羧酸、磷酸及磺酸、酸式鹽(例如，檸檬酸一鈉、檸檬酸二鈉、蘋果酸一鈉等)、鹼金屬氫氧化物如氫氧化鈉、碳酸鹽如碳酸鈉、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、焦磷酸鹽等)、咪唑及類似物。一種或多種pH調節劑係任意地以有效於維持該組成物於口腔可接受之pH範圍中之總數量存在。
於又進一步之具體例中，本發明之組成物包含至少一種表面活化劑。可使用任何口腔可接受之表面活化劑，其中大多數為陰離子性、非離子性或兩性離子者。適當之陰離子表面活化劑包括但非侷限於，C8-20烷基硫酸酯之水溶性鹽、C8-20脂肪酸之磺化甘油一酸酯、肌胺酸鹽、牛磺酸鹽及類似物。此等及其他類之闡明性實例包括月桂基硫酸鈉(SLS)、椰基
甘油一酸酯磺酸鈉、月桂基肌胺酸鈉、月桂基異乙烯磺酸鈉、第十二烷基羧酸鈉及十二烷基苯磺酸鈉。適當之非離子性表面活化劑包括但非侷限於，聚羥亞烴(poloxamers)、聚氧化乙烯山梨糖醇酐酯、脂族醇乙氧酸酯、烷基苯酚乙氧酸酯、第三胺氧化物、第三膦氧化物、二烷基亞碸及類似物。適當之兩性離子的表面活化劑包括但非侷限於，具有陰離子基團如羧酸鹽、硫酸鹽、磺酸鹽、磷酸鹽或膦酸鹽之C8-20脂族第二及第三胺衍生物。甜菜鹼亦可使用，其之適當實例為椰基醯胺基丙基甜菜鹼。一種或多種表面活化劑係按該組成物之總重量，任意地以約0.01重量%至約10重量%之總數量存在，例如，由約0.05重量%至約5重量%，或由約0.1重量%至約2重量%。
於某些具體例中，本發明之組成物包含至少一種泡沫調製劑，其有用於，例如，於攪拌時增加由該組成物所產生之泡沫數量、厚度或穩定性。可使用任何口腔可接受之泡沫調製劑，包括但非侷限於，聚乙二醇(PEGs)，亦稱為聚氧基乙烯。高分子量PEGs包括那些具有平均分子量200,000至7,000,000，例如500,000至5,000,000，或1,000,000至2,500,000者為適合。一種或多種PEGs係按該組成物之總重量，任意地以約0.1重量%至約10重量%之總數量存在，例如由約0.2重量%至約5重量%，或由約0.25重量%至約2重量%。
於某些具體例中，本發明之組成物包含至少一種增稠劑，其有用於，例如，賦予想要之稠度及/或口感至該組成物。可使用任何口腔可接受之增稠劑，包括但非侷限於，碳聚物，亦稱為羧基乙烯基聚合物、角叉菜，亦稱為愛爾蘭青苔且更特別為-角叉菜(iota-carrageenan)、纖維質聚合物如羥基乙基纖維素、羧基甲基纖維素(CMC)及其鹽，例如，CMC鈉、天然樹膠如刺梧桐、黃原膠、阿拉伯樹膠及西黃蓍、膠態矽酸鋁鎂、膠態矽石及類似物。較佳之增稠或膠凝劑種類包括丙烯酸與季戊四醇之烷基醚或蔗糖之烷基醚交聯之均聚物等級，或碳聚物(carbomer)。碳聚物市售可得
自於B.F.古德里奇，如卡波普(Carbopol)®系列。特別佳之卡波普包括卡波普934、940、941、956、974P，及其混合物。
矽石增稠劑如矽歐頓115及矽歐頓165(二者可得自於胡柏工程材料公司)及DT 267(可得自於PPG工業公司或OSC-連吉化學工業公司)亦可使用。一種或多種增稠劑係按該組成物之總重量，任意地以由約0.01重量%至15重量%之總數量存在，例如由約0.1重量%至約10重量%，或由約0.2重量%至約5重量%。
於某些具體例中，本發明之組成物包含至少一種黏度調節劑，其有用於，例如，於攪拌液態組成物時，幫助抑制組成份沉降或分離，或促進再分散。可使用任何口腔可接受之黏度調節劑，包括但非侷限於，礦物油、凡士林、黏土及有機改質黏土、矽石及類似物。一種或多種黏度調節劑係按該組成物之總重量，任意地以由約0.01重量%至約10重量%之總數量存在，例如，由約0.1重量%至約5重量%。
於某些具體例中，本發明之組成物包含至少一種濕潤劑。可使用任何口腔可接受之濕潤劑，包括但非侷限於，多元醇，如丙三醇、山梨糖醇(特別如70%溶液)、木糖醇或低分子量聚乙二醇(PEGs)如PEG 600。許多濕潤劑亦作用如甜味劑。一種或多種濕潤劑係按該組成物之總重量，任意地以由約1重量%至約70重量%之總數量存在，例如，由約1重量%至約50重量%，由約2重量%至約25重量%，或由約5重量%至約15重量%。
於某些具體例中，本發明之組成物包含至少一種甜味劑，其有用於，例如，增強該組成物之味道。可使用任何口腔可接受之天然或人工甜味劑，包括但非侷限於，右旋糖、蔗糖、麥芽糖、糊精、乾性轉化糖、甘露糖、木糖、核糖、果糖、左旋糖、半乳糖、玉米糖漿(包括高果糖玉米糖漿及玉米糖漿固體)、部分水解之澱粉、氫化澱粉水解物、山梨糖醇、甘露糖醇、木糖醇、麥芽糖醇、異麥芽酮糖醇、阿斯巴甜(aspartame)、紐甜
(neotame)、糖精及其鹽(如糖精鈉)，以二胜肽為主之強甜味劑、環己基磺醯胺酸鹽(cyclamate)及類似物。一種或多種甜味劑係強烈地依所選擇之特定甜味劑(類)而定，任意地按該組成物之總重量，但典型地以0.005重量%至5重量%之總數量存在，任意地0.005重量%至0.3重量%，進一步任意地0.05重量%至0.1重量%，按該組成物之總重量。
於某些具體例中，本發明之組成物包含至少一種香味劑，其有用於，例如，增強該組成物之味道。可使用任何口腔可接受之天然或合成香味劑，包括但非侷限於，香草醛、鼠尾草、黑角蘭、歐芹油、綠薄荷油、肉桂油、鹿蹄草油(水楊酸甲酯)、薄荷油、丁子香油、月桂樹油、茴香油、桉樹油、柑橘類油、果實油及精油，其包括那些由檸檬、枊橙、萊姆、葡萄柚、杏桃、香蕉、葡萄、蘋果、草莓、櫻桃、鳳梨等所導生者，豆及堅果所導生之香味，如咖啡、可可、可樂、花生、扁桃仁等，及其他香料，吸附及包膠之香味劑，及類似物。亦涵括於本文中之香味劑為於口中提供香氣及/或其他感官效果，包括清涼或溫熱效果之組成份。此等組成份闡明性地包括醇、醋酸酯、乳酸酯、樟腦、桉樹油、桉樹腦、丁子香酚、桂皮、歐沙酮(oxanone)、α-紫羅蘭酮、丙烯基癒瘡木酚(propenyl guaiethol)、百里酚、里哪醇、苯甲醛、肉桂醛、N-乙基-對-烷-3-羧胺、N,2,3-三甲基-2-異丙基丁醯胺、3-(1-氧基)-丙烷-1,2-二醇、肉桂醛甘油縮醛(CGA)、酮甘油縮醛(MGA)及類似物。一種或多種香味劑係按該組成物之總重量，任意地以由約0.01重量%至約5重量%之總數量存在，例如，由約0.03重量%至約2.5重量%，任意地約0.05重量%至約1.5重量%，進一步任意地約0.1重量%至約0.3重量%。
本發明之組成物可包含至少一種著色劑。本文中之著色劑包括顏料、染料、色澱及增添特別光澤或反射性之試劑如珠光劑。可使用任何口腔可接受之著色劑，包括但非侷限於，滑石、雲母、碳酸鎂、碳酸鈣、矽酸鎂、矽酸鋁鎂、矽石、二氧化鈦(TiO2)、氧化鋅、紅、黃、褐及黑色氧
化鐵、氰亞鐵酸鐵銨(ferric ammonium ferrocyanide)、錳紫、群青、鈦酸雲母、氯氧化鉍，及類似物。一種或多種著色劑係按該組成物之總重量，任意地以由約0.001重量%至約20重量%之總數量存在，例如，由約0.01重量%至約10重量%，或由約0.1重量%至約5重量%。
本發明之組成物係任意地包含抗細菌劑如氯己酊(chlorhexidine)、三氯生(triclosan)、季銨化合物(例如苯烷銨氯化物(benzalkonium chloride))或附加之防腐劑如對羥苯甲酸酯類(例如，甲基對羥苯甲酸酯或丙基對羥苯甲酸酯。一種或多種抗細菌或防腐劑係按該組成物之總重量，任意地以由約0.01重量%至約0.5重量%之總數量存在於該組成物中，任意地約0.05重量%至約0.1重量%。
於某些具體例中，該組成物係不含此等附加之抗細菌或防腐劑。
本發明之組成物係任意包含唾液刺激劑有用於，例如，改善口乾。可使用任何口腔上可接受之唾液刺激劑，包括但非侷限於食物酸如檸檬酸、乳酸、蘋果酸、琥珀酸、抗壞血酸、己二酸、反式丁烯二酸，及酒石酸，及其混合物。一種或多種唾液刺激劑係任意地以唾液刺激有效之總數量存在。
本發明之組成物係任意地合併一種或多種抗敏感劑，例如，鉀鹽如硝酸鉀、碳酸氫鉀、氯化鉀、檸檬酸鉀，及草酸鉀；番椒辣素；丁子香酚；鍶鹽；氯化物鹽及其組合物。此等試劑可以有效之數量添加，例如，根據該組成物之總重量以由約1重量%至約20重量%按重量，依所選擇之試劑而定。本發明之組成物當施用於牙齒時亦可藉阻斷牙本質小管用來治療敏感症。
於某些具體例中，本發明之組成物進一步包含抗氧化劑。可使用任何口腔可接受之抗氧化劑，包括：丁基化羥基苯甲醚(BHA)、丁基化羥基甲苯(BHT)、維生素A、類胡蘿蔔素、維生素E、類黃酮、多酚、抗壞
血酸、草藥抗氧化劑、葉綠素、褪黑激素，及其混合物。。
本發明之組成物可另外任意地包含如於下所提供之酒石控制(抗結石)劑。那些有用於本文中之酒石控制劑包括特定試劑的鹽，其包括鹼金屬鹽及銨鹽。該試劑包括：磷酸鹽及多磷酸鹽(例如焦磷酸鹽)、聚胺基丙烷磺酸(AMPS)、聚烯烴磺酸鹽、聚烯烴磷酸鹽、二膦酸鹽如氮雜環烷-2,2-二膦酸鹽(例如，氮雜環庚烷-2,2-二膦酸)、N-甲基氮雜環戊烷-2,3-二膦酸、乙烷-1-羥基-1,1-二膦酸(EHDP)及乙烷-1-胺基-1,1-二膦酸鹽及膦酸基鏈烷羧酸。有用之無機磷酸鹽及多磷酸鹽包括一元、二元及三元磷酸鈉、三多磷酸鈉、四多磷酸鹽、焦磷酸一鈉、焦磷酸二鈉、焦磷酸三鈉、焦磷酸四鈉(TSPP)、焦磷酸四鉀(TKPP)、三偏磷酸鈉、六偏磷酸鈉及其混合物。其他有用的酒石控制劑包括多羧酸鹽聚合物及聚乙烯基甲基醚/順式丁烯二酸酐(PVM/MA)共聚物，如GANTREZ®。
於某些具體例中，本發明之組成物進一步包含營養物。適當之營養物包括維生素、礦物質、胺基酸，及其混合物。維生素包括維生素C及D、硫胺素、核黃素、泛酸鈣、菸酸、葉酸、菸醯胺、吡哆醇、氰鈷胺、對-胺基苯甲酸、生物類黃酮，及其混合物。營養補充物包括胺基酸(如L-色胺酸、L-賴胺酸、蛋胺酸、蘇胺酸、左旋肉毒鹼(levocarnitine)及L-肉毒鹼)、肝營養素(lipotropics)(如膽鹼、肌醇、甜菜鹼，及亞麻油酸)，及其混合物。
本發明之具體例係於下列之實例中進一步說明。該實例僅係闡明且不應以任何方式來限制如所說明及所請求之本發明的範圍。
將組成物A至G如表1中所示者予以配製，以便評估不同
濃度之SnCl2於以矽石為主之高含水量潔牙劑中之強健性對抗微生物挑戰之影響。此等組成物各個具有高的總含水量(來自CP水及來自70%山梨糖醇溶液二者)。
將此等組成物之各個微強健性指數(MRI)予以測定。該微強健性指數係用作為組成物抵禦微生物挑戰之能力的定量測量。該MRI係為評估化合物/組成物對抗微生物組合，包括洋蔥伯克霍爾德菌(Burkholderia cepacia)、陰溝腸桿菌(Enterobacter cloacae)、大腸桿菌、產酸克雷伯菌(Klesiella oxytoca)、肺炎克雷白桿菌(Klebsiella pneumoniae)、粘質沙雷氏菌(Serratia marcescens)、雷氏普羅威登斯菌(Providencia rettgeri)、綠膿桿菌(Pseudomonas aeruginosa)、惡臭假單胞菌(Pseudomonas putida)、金黃色葡萄球菌、腐生葡萄球菌(Staphylococcus saprophyticus)之抗微生物功效的挑戰試驗結果。將列舉於上之組合中之107細菌接種體樣品以30分鐘間隔挑戰3次。於4、6及24小時後，將等份試樣進行試驗，以測定細菌之對數減少。使用此等數據，將曲線(AUC)下之面積計算出來且然後轉換成MRI；該MRI越高，則該試驗組成物之微強健性越大。
本案發明人業已發現，為了顯示組成物具有可接受程度之強健性對抗微生物攻擊，至少0.75之MRI是必需的。MRI低於0.75可能不足以降低該微生物之組合且導致更大的微生物攻擊風險。
組成物A至F之各個微強健性指數(MRI)顯示於表1中(所有的數字係以重量百分比計)。
如表1中所示者，組成物A-C(其含有小於0.125重量%之SnCl2)具有不可接受之MRI。因此，該組成物不具有可接受之強健性含量向微生物挑戰。
然而，其可由表1中之結果看出，含有SnCl2介於0.15重量%及0.75重量%間之高含水量組成物產生大於0.75之MRI值。因此，此等組成物顯示可接受之強健性含量向微生物挑戰。雖然0.15重量% SnCl2之濃度允許該組成物達到MRI>0.75之接受標準，但0.3重量%之SnCl2濃度允許該組成物達到MRI=0.91之最佳結果。相反的，組成物含多至0.10重量
% SnCl2顯示MRI不足，甚至沒有達到0.75目標之一半。
雖然可添加額外的SnCl2，但相較於SnCl2之成本增加66%(0.3重量%對0.5重量%)或SnCl2增加150%(0.3重量.%對0.75重量%)，其於MRI之增加相對地可以忽略。此外，SnCl2係為澀的化合物，其味道甚至比SnF2(其具有苦、鹹味)更差且一旦MRI達到必要之程度，精於此方面技藝之人士應受到激發以減少所使用之數量。
雖然本發明之特別具體例業已闡明且說明，對精於此方面技藝之人士應顯而易見，其可在不背離如後附申請專利範圍中所定義之本發明之範圍下逕行各種變化及修改。
Claims (21)
- 一種水性口腔保健組成物，其包含由0.125重量%至0.75重量%水溶性亞錫離子來源，其中，該組成物包含50重量%至65重量%水，且其中該亞錫離子之來源係選自於由下列所組成之群組：氯化亞錫、焦磷酸亞錫、甲酸亞錫、醋酸亞錫、葡糖酸亞錫、乳酸亞錫、酒石酸亞錫、草酸亞錫、丙二酸亞錫、檸檬酸亞錫、亞錫伸乙基過氧化脲及其混合物，其中該組成物包含牙垢控制劑，且其中該牙垢控制劑包含0.5至3.0重量%焦磷酸鹽，其選自焦磷酸四鈉、焦磷酸四鉀、或其混合物。
- 如申請專利範圍第1項之口腔保健組成物，其中該組成物包含由0.125重量%至0.5重量%該亞錫離子之來源。
- 如申請專利範圍第2項之口腔保健組成物，其中該組成物包含由0.125重量%至0.3重量%該亞錫離子之來源。
- 如申請專利範圍第2項之口腔保健組成物，其中該組成物包含由0.15重量%至0.3重量%該亞錫離子之來源。
- 如申請專利範圍第1至4項中任一項之口腔保健組成物，其中該亞錫離子之來源為氯化亞錫。
- 如申請專利範圍第1至4項中任一項之口腔保健組成物，其中該組成物包含由52重量%至60重量%水。
- 如申請專利範圍第6項之口腔保健組成物，其中該組成物包含由54重量%至55重量%水。
- 如申請專利範圍第1至4項中任一項之口腔保健組成物，其進一步包含選自於由氟化鈉、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、氟化銨及其組合物所組成之群組的氟化物離子來源。
- 如申請專利範圍第1至4項中任一項之口腔保健組成物，其進一步包含 鋅離子之來源。
- 如申請專利範圍9項之口腔保健組成物，其中該鋅離子之來源包含氧化鋅、檸檬酸鋅或其混合物。
- 如申請專利範圍第10項之口腔保健組成物，其中，該組成物包含檸檬酸鋅以由0重量%至2.5重量%之量。
- 如申請專利範圍第10項之口腔保健組成物，其中，該組成物包含檸檬酸鋅以由1.5重量%至2.5重量%之量。
- 如申請專利範圍第10或11項之口腔保健組成物，其中該組成物包含氧化鋅以由0重量%至1.5重量%之量。
- 如申請專利範圍第10或11項之口腔保健組成物，其中該組成物包含氧化鋅以由0.5重量%至1.5重量%之量。
- 如申請專利範圍第1至4項中任一項之口腔保健組成物，其中該組成物為牙膏、牙凝膠、漱口劑、乳膏或軟膏。
- 如申請專利範圍第1至4項中任一項之口腔保健組成物，其中該組成物係不含附加之抗細菌或防腐劑。
- 如申請專利範圍第1至4項中任一項之口腔保健組成物，其中該組成物具有向微生物挑戰之至少0.75的微強健性指數(MRI)。
- 一種如申請專利範圍第1至17項中任一項之口腔保健組成物的用途，係用於製備具有向微生物挑戰之至少0.75的微強健性指數(MRI)的口腔保健產品。
- 如申請專利範圍第18項之用途，其中該組成物包含由0.15重量%至0.3重量%該亞錫離子之來源。
- 如申請專利範圍第18或19項之用途，其中該亞錫離子之來源為氯化亞錫。
- 如申請專利範圍第18或19項之用途，其中，該組成物包含由50重量%至60重量%水。
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| CN107847405A (zh) * | 2015-07-17 | 2018-03-27 | 高露洁-棕榄公司 | 口腔护理组合物 |
| US11273116B2 (en) | 2015-12-30 | 2022-03-15 | Colgate-Palmolive Company | Striped dentifrice composition comprising zinc |
| AU2017280200B2 (en) | 2016-06-24 | 2019-10-03 | Colgate-Palmolive Company | Oral care composition and method of use |
| WO2017219339A1 (en) * | 2016-06-24 | 2017-12-28 | Colgate-Palmolive Company | Oral care compositions and methods of use |
| CN113164339B (zh) * | 2018-11-23 | 2024-05-28 | Blbr股份有限公司 | 牙齿护理和牙齿清洁组合物、系统及牙齿清洁方法 |
| MX2021007647A (es) | 2018-12-26 | 2021-08-11 | Colgate Palmolive Co | Composiciones para el cuidado bucal. |
| US11135141B2 (en) | 2019-06-28 | 2021-10-05 | The Procter & Gamble Company | Oral care compositions comprising tin ions |
| BR112021024304A2 (pt) | 2019-06-28 | 2022-01-11 | Procter & Gamble | Composições para tratamento bucal compreendendo íons de estanho |
| US12337048B2 (en) | 2019-06-28 | 2025-06-24 | The Procter & Gamble Company | Oral care compositions comprising tin ions |
| US11135143B2 (en) | 2020-06-25 | 2021-10-05 | The Procter & Gamble Company | Oral care compositions comprising tin ions |
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