TW200817017A - High fluoride ion oral care composition and method for maintaining anticaries activity - Google Patents
High fluoride ion oral care composition and method for maintaining anticaries activity Download PDFInfo
- Publication number
- TW200817017A TW200817017A TW096123622A TW96123622A TW200817017A TW 200817017 A TW200817017 A TW 200817017A TW 096123622 A TW096123622 A TW 096123622A TW 96123622 A TW96123622 A TW 96123622A TW 200817017 A TW200817017 A TW 200817017A
- Authority
- TW
- Taiwan
- Prior art keywords
- oral care
- care composition
- fluoride
- weight
- percent
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 125
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 title claims abstract description 63
- 238000000034 method Methods 0.000 title claims abstract description 13
- 230000000694 effects Effects 0.000 title claims abstract description 10
- 230000000675 anti-caries Effects 0.000 title claims abstract description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 30
- -1 fluoride ions Chemical class 0.000 claims abstract description 20
- 239000003975 dentin desensitizing agent Substances 0.000 claims abstract description 8
- 239000000416 hydrocolloid Substances 0.000 claims description 19
- 239000003795 chemical substances by application Substances 0.000 claims description 14
- 238000011084 recovery Methods 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 13
- 235000010418 carrageenan Nutrition 0.000 claims description 12
- 239000000679 carrageenan Substances 0.000 claims description 12
- 229920001525 carrageenan Polymers 0.000 claims description 12
- 229940113118 carrageenan Drugs 0.000 claims description 12
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 claims description 12
- FGIUAXJPYTZDNR-UHFFFAOYSA-N potassium nitrate Chemical compound [K+].[O-][N+]([O-])=O FGIUAXJPYTZDNR-UHFFFAOYSA-N 0.000 claims description 10
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 8
- NROKBHXJSPEDAR-UHFFFAOYSA-M potassium fluoride Chemical compound [F-].[K+] NROKBHXJSPEDAR-UHFFFAOYSA-M 0.000 claims description 8
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical group [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 8
- 239000000606 toothpaste Substances 0.000 claims description 8
- 239000000230 xanthan gum Substances 0.000 claims description 8
- 235000010493 xanthan gum Nutrition 0.000 claims description 8
- 229920001285 xanthan gum Polymers 0.000 claims description 8
- 229940082509 xanthan gum Drugs 0.000 claims description 8
- 229940090898 Desensitizer Drugs 0.000 claims description 7
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical group [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims description 7
- 229940034610 toothpaste Drugs 0.000 claims description 7
- 239000003242 anti bacterial agent Substances 0.000 claims description 6
- 239000002253 acid Substances 0.000 claims description 5
- 235000003599 food sweetener Nutrition 0.000 claims description 5
- 235000010333 potassium nitrate Nutrition 0.000 claims description 5
- 239000004323 potassium nitrate Substances 0.000 claims description 5
- 239000003765 sweetening agent Substances 0.000 claims description 5
- 229910052902 vermiculite Inorganic materials 0.000 claims description 5
- 239000010455 vermiculite Substances 0.000 claims description 5
- 235000019354 vermiculite Nutrition 0.000 claims description 5
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims description 4
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 claims description 4
- RRAFCDWBNXTKKO-UHFFFAOYSA-N eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 claims description 4
- 239000011698 potassium fluoride Substances 0.000 claims description 4
- 235000003270 potassium fluoride Nutrition 0.000 claims description 4
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims description 4
- 239000011775 sodium fluoride Substances 0.000 claims description 4
- 235000013024 sodium fluoride Nutrition 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 4
- 229910021653 sulphate ion Inorganic materials 0.000 claims description 4
- 239000004094 surface-active agent Substances 0.000 claims description 4
- 239000002562 thickening agent Substances 0.000 claims description 4
- BHHYHSUAOQUXJK-UHFFFAOYSA-L zinc fluoride Chemical compound F[Zn]F BHHYHSUAOQUXJK-UHFFFAOYSA-L 0.000 claims description 4
- 239000004475 Arginine Substances 0.000 claims description 3
- 239000013543 active substance Substances 0.000 claims description 3
- 239000000654 additive Substances 0.000 claims description 3
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 3
- 210000000214 mouth Anatomy 0.000 claims description 3
- 239000004575 stone Substances 0.000 claims description 3
- 229960003500 triclosan Drugs 0.000 claims description 3
- DTOUUUZOYKYHEP-UHFFFAOYSA-N 1,3-bis(2-ethylhexyl)-5-methyl-1,3-diazinan-5-amine Chemical compound CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 DTOUUUZOYKYHEP-UHFFFAOYSA-N 0.000 claims description 2
- RWMSXNCJNSILON-UHFFFAOYSA-N 2-[4-(2-propylpentyl)piperidin-1-yl]ethanol Chemical compound CCCC(CCC)CC1CCN(CCO)CC1 RWMSXNCJNSILON-UHFFFAOYSA-N 0.000 claims description 2
- 108010062877 Bacteriocins Proteins 0.000 claims description 2
- NPBVQXIMTZKSBA-UHFFFAOYSA-N Chavibetol Natural products COC1=CC=C(CC=C)C=C1O NPBVQXIMTZKSBA-UHFFFAOYSA-N 0.000 claims description 2
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 claims description 2
- 239000005770 Eugenol Substances 0.000 claims description 2
- NVNLLIYOARQCIX-MSHCCFNRSA-N Nisin Chemical compound N1C(=O)[C@@H](CC(C)C)NC(=O)C(=C)NC(=O)[C@@H]([C@H](C)CC)NC(=O)[C@@H](NC(=O)C(=C/C)/NC(=O)[C@H](N)[C@H](C)CC)CSC[C@@H]1C(=O)N[C@@H]1C(=O)N2CCC[C@@H]2C(=O)NCC(=O)N[C@@H](C(=O)N[C@H](CCCCN)C(=O)N[C@@H]2C(NCC(=O)N[C@H](C)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@H](CS[C@@H]2C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CCSC)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]2C(N[C@H](C)C(=O)N[C@@H]3C(=O)N[C@@H](C(N[C@H](CC=4NC=NC=4)C(=O)N[C@H](CS[C@@H]3C)C(=O)N[C@H](CO)C(=O)N[C@H]([C@H](C)CC)C(=O)N[C@H](CC=3NC=NC=3)C(=O)N[C@H](C(C)C)C(=O)NC(=C)C(=O)N[C@H](CCCCN)C(O)=O)=O)CS[C@@H]2C)=O)=O)CS[C@@H]1C NVNLLIYOARQCIX-MSHCCFNRSA-N 0.000 claims description 2
- 108010053775 Nisin Proteins 0.000 claims description 2
- UVMRYBDEERADNV-UHFFFAOYSA-N Pseudoeugenol Natural products COC1=CC(C(C)=C)=CC=C1O UVMRYBDEERADNV-UHFFFAOYSA-N 0.000 claims description 2
- 108010077895 Sarcosine Proteins 0.000 claims description 2
- ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 2
- 229960002504 capsaicin Drugs 0.000 claims description 2
- 235000017663 capsaicin Nutrition 0.000 claims description 2
- 229960003260 chlorhexidine Drugs 0.000 claims description 2
- JRBPAEWTRLWTQC-UHFFFAOYSA-N dodecylamine Chemical compound CCCCCCCCCCCCN JRBPAEWTRLWTQC-UHFFFAOYSA-N 0.000 claims description 2
- 229960002217 eugenol Drugs 0.000 claims description 2
- 229960004867 hexetidine Drugs 0.000 claims description 2
- 239000003906 humectant Substances 0.000 claims description 2
- 229910000040 hydrogen fluoride Inorganic materials 0.000 claims description 2
- 239000004309 nisin Substances 0.000 claims description 2
- 235000010297 nisin Nutrition 0.000 claims description 2
- 229950002404 octapinol Drugs 0.000 claims description 2
- 229960001774 octenidine Drugs 0.000 claims description 2
- SMGTYJPMKXNQFY-UHFFFAOYSA-N octenidine dihydrochloride Chemical compound Cl.Cl.C1=CC(=NCCCCCCCC)C=CN1CCCCCCCCCCN1C=CC(=NCCCCCCCC)C=C1 SMGTYJPMKXNQFY-UHFFFAOYSA-N 0.000 claims description 2
- 239000011736 potassium bicarbonate Substances 0.000 claims description 2
- 235000015497 potassium bicarbonate Nutrition 0.000 claims description 2
- 229910000028 potassium bicarbonate Inorganic materials 0.000 claims description 2
- 239000001103 potassium chloride Substances 0.000 claims description 2
- 235000011164 potassium chloride Nutrition 0.000 claims description 2
- 239000001508 potassium citrate Substances 0.000 claims description 2
- 229960002635 potassium citrate Drugs 0.000 claims description 2
- QEEAPRPFLLJWCF-UHFFFAOYSA-K potassium citrate (anhydrous) Chemical compound [K+].[K+].[K+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O QEEAPRPFLLJWCF-UHFFFAOYSA-K 0.000 claims description 2
- 235000011082 potassium citrates Nutrition 0.000 claims description 2
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims description 2
- GZWNUORNEQHOAW-UHFFFAOYSA-M potassium;2-aminoacetate Chemical compound [K+].NCC([O-])=O GZWNUORNEQHOAW-UHFFFAOYSA-M 0.000 claims description 2
- 229940043230 sarcosine Drugs 0.000 claims description 2
- 239000003381 stabilizer Substances 0.000 claims description 2
- YUOWTJMRMWQJDA-UHFFFAOYSA-J tin(iv) fluoride Chemical compound [F-].[F-].[F-].[F-].[Sn+4] YUOWTJMRMWQJDA-UHFFFAOYSA-J 0.000 claims description 2
- 239000000341 volatile oil Substances 0.000 claims description 2
- 239000011701 zinc Substances 0.000 claims description 2
- 229910052725 zinc Inorganic materials 0.000 claims description 2
- AZQWKYJCGOJGHM-UHFFFAOYSA-N 1,4-benzoquinone Chemical compound O=C1C=CC(=O)C=C1 AZQWKYJCGOJGHM-UHFFFAOYSA-N 0.000 claims 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
- 229940091249 fluoride supplement Drugs 0.000 claims 2
- PFNFFQXMRSDOHW-UHFFFAOYSA-N spermine Chemical compound NCCCNCCCCNCCCN PFNFFQXMRSDOHW-UHFFFAOYSA-N 0.000 claims 2
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims 1
- 241000283153 Cetacea Species 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 1
- RWSOTUBLDIXVET-UHFFFAOYSA-N Dihydrogen sulfide Chemical class S RWSOTUBLDIXVET-UHFFFAOYSA-N 0.000 claims 1
- KRHYYFGTRYWZRS-UHFFFAOYSA-N Fluorane Chemical compound F KRHYYFGTRYWZRS-UHFFFAOYSA-N 0.000 claims 1
- 239000004471 Glycine Substances 0.000 claims 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims 1
- 239000004111 Potassium silicate Substances 0.000 claims 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims 1
- LFVVNPBBFUSSHL-UHFFFAOYSA-N alexidine Chemical compound CCCCC(CC)CNC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NCC(CC)CCCC LFVVNPBBFUSSHL-UHFFFAOYSA-N 0.000 claims 1
- 229950010221 alexidine Drugs 0.000 claims 1
- XVRKEHYQBKGNBA-UHFFFAOYSA-N azanium;zinc;fluoride Chemical compound [NH4+].[F-].[Zn] XVRKEHYQBKGNBA-UHFFFAOYSA-N 0.000 claims 1
- 229910052797 bismuth Inorganic materials 0.000 claims 1
- JCXGWMGPZLAOME-UHFFFAOYSA-N bismuth atom Chemical compound [Bi] JCXGWMGPZLAOME-UHFFFAOYSA-N 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- WUKWITHWXAAZEY-UHFFFAOYSA-L calcium difluoride Chemical compound [F-].[F-].[Ca+2] WUKWITHWXAAZEY-UHFFFAOYSA-L 0.000 claims 1
- 229910001634 calcium fluoride Inorganic materials 0.000 claims 1
- 229910052802 copper Inorganic materials 0.000 claims 1
- 239000010949 copper Substances 0.000 claims 1
- IRXRGVFLQOSHOH-UHFFFAOYSA-L dipotassium;oxalate Chemical compound [K+].[K+].[O-]C(=O)C([O-])=O IRXRGVFLQOSHOH-UHFFFAOYSA-L 0.000 claims 1
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- ZULTVNRFZRQYKL-UHFFFAOYSA-M fluorotin Chemical compound [Sn]F ZULTVNRFZRQYKL-UHFFFAOYSA-M 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
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- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
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- 239000000463 material Substances 0.000 claims 1
- 125000001421 myristyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- KSGDAXSMHDKMMZ-UHFFFAOYSA-N n',n'-diethyl-n-octylethane-1,2-diamine Chemical compound CCCCCCCCNCCN(CC)CC KSGDAXSMHDKMMZ-UHFFFAOYSA-N 0.000 claims 1
- GVGCUCJTUSOZKP-UHFFFAOYSA-N nitrogen trifluoride Chemical compound FN(F)F GVGCUCJTUSOZKP-UHFFFAOYSA-N 0.000 claims 1
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- 229940063675 spermine Drugs 0.000 claims 1
- GNJNALCRIODCAZ-UHFFFAOYSA-N tripotassium;fluoro(trioxido)silane Chemical compound [K+].[K+].[K+].[O-][Si]([O-])([O-])F GNJNALCRIODCAZ-UHFFFAOYSA-N 0.000 claims 1
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Description
200817017 九、發明說明: 發明背景 [_1]鶴齒為影響大多數人們之主要牙疾病。在2〇世紀 初期,研究者發現氟化物有效降低齲齒之發生。自當時起, 5即已發展氟化物的研究’而現在已完全接受氣化物田處 盈於牙齒健康。 :]1化物有數種主要的抗齲齒發生機制。例如,齲 馨回期,由細菌所形成之酸會引起琺瑯質之去礦質化(牙 10 ΐ ίί分解損失礦物f含量)。氟化物可促進再鑛質化及抑 10制生齲過程最早階段期間的去礦質化。來自氟化之水或氟 _ =牙霄^氟化物部分被牙菌斑所吸收’大部分依此方式所 提,之氟化物以結合形式,而非離子形式被儲存於其中。 ’若口腔環境之pH降低,則結合之氟化物隨後將被 釋。所釋放之氟化物隨後與鈣或磷酸根離子作用,以幫 15助逆向早期去礦質化之作用。 籲[0003] 1化物亦可抗菌地作用,因為牙菌斑上之氣化物 可抑制糖分解(其巾可發酵之碳水化合物被生鱗細菌代謝 產生酸)。最後,來自經氟化之水或說化物補充品之氣化 物,當被混入形成中之牙齒綠瑯質時,可強化綠瑯質且使 2〇其更為耐腐钱的。因此,氟化物的好處為特別有利於兒童 發展中的牙齒。 [0004]專^業投予之氟化物包括凝膠-牙托塗覆、溶液、泡 末體及糊❺然而,不須處方籤(over-the-counter)的氟化 物來源(諸如漱口水、牙膏及凝膠)更普遍被消費者所使 5 200817017 用。 [0005.]冑泛可取得之潔齒劑通常包含範圍I工,嶋 1,500 ppm的I離子。惟,就某些部分人們而言,’旦 :氟化物可能更加有利。一些患者經常罹患 二 然就是較之—般人們處於較高的牙錢風險中的 μ專病心可由混合高量氟離子以治療高度齲 劑獲得利益。例如,—此t卜鍤、餐喜匈、日人> 心付殊珠回 子源,用旦^T些此種泳齒劑混合I化鈉作為氟離 ^\、此里赵匕,⑼PPm、2,_ PPm或5,咖此 ίο 15 4、、且成物在抗齲齒方面為高度有效的。 ,者中基於各種健康相_由之牙齒敏感性的併發症 治療有报多種。例如,硝酸鉀為眾所周知於商 業泳回劑中使用之牙齒敏感劑。參見Hodosh之美國 m,00: f他敏感性牙齒的治療包含碳酸氫鉀或氯化 ^ (多見吳國專利案4,631,185及4,751,072)。美國專利案 曰,990,327列舉使用銘及氟離子供敏感性牙盘治療。本文戶斤 提及之有所的專利案全部内容併入本文作為參考。 Μ的是可同時治療牙齒敏感性及麟齒並提供高 里之氟化物處理’全部使用單一調配物。准’如果上述之 牙齒敏感劑以必要有效的處理量被添加,雖然彼等可能是 有效的但其在亦包括此等敏感劑之口腔護理組成物中很 難保持氟化物之有效特性。這是因為當有效量之硝酸鉀被 =加時,氟離子(F·)容易沉殺出$。這是由於固有低溶解 度之氟離子來源’諸如氟化納(通常低於5%)。另一方面, 20 200817017 右,加^夕洛劑’組成物會改變且傾向於喪失與具有兩種 該等成刀之可接文的非處方藥或處方潔食劑有關之物 理特性。 [0008]目此,此技藝中亟需一種高氟化物含量之口腔護 5理組成物,其亦可治療敏感性牙齒,可以單劑、易使用之 二脸。又,、、且成物形式(諸如潔齒劑,特別是牙膏)予以取 付谷ΐ所需之高量氟化物及敏感劑之有效溶解。此對 •該等需要咼量氟化物且亦罹患敏感性牙齒之病患是有益 的。進一步期望能發展一種組成物,其中氟離子之抗齲齒 10活性成功地被保持一段時間。 之簡要說明 —[0009]於一具體例中,本發明係有關一種口腔護理組成 物,其包含: 充刀里之氟_子源以提供至少約2,5〇〇 ppm之氟離 15 子; • 一有效量之去敏感劑;及 至少約40重量百分比之水。 [0010]於另一具體例中,本發明係有關一種口腔護理組 成物,其包含: • 20 至少約ppm之氟離子; 以重量計約5百分比至約1〇百分比之鉀鹽; 以重量計約40百分比至約75百分比之水;及 以重量計約0.5百分比至約15百分比之水膠體,選自 由黃原膠及鹿角菜膠所成組群中。 7 200817017 L〇 Γ! 2另一具體例中,本發明係有關-種保持口腔護 理組成物中氟離子的抗齲齒活性之方法,其包含: 5 以=一種包含至少約2,500 ppm之氟離子、有效量之 及至f'約40重量百分比水之口腔護理組成物;及 ,、口腔護理組成物以重量計約〇 5百分比.至約15百 分比之水膠體。 發明之詳細説日q =012上於本文之揭露中,範圍被用作供描述在範圍内各 之間略表達形式。在此範圍内之任意值可被選擇作為範 10 圍之端值。 .[0013]力本發明之—較佳具體例中,提供―種口腔護理 組成物,其可組合供強力抗鱗窗治療之高量氣化物以及敏 感性治療劑(諸如鉀鹽)。本發明之口腔護理組成物包括以 下諸成分’其為較佳用量且係關於本文中所述之組成物所 15 選擇者。 [0014] 口腔護理組成物較佳包含高於一般傳統敏感型口 腔護理組成物所加入之水量,且包含是能有效形成鎖水於 配製,=之糊劑的水膠體以達所欲流變學,同時保持組成 物中南氟化物及抗鶴齒活性之濃度。 [0015] 口腔護理組成物較佳為潔齒劑形式。較佳之潔齒 劑包括(但不限於)各種類型之牙膏、牙齒磨光劑、牙膠、 漱口水及口部沖洗劑、假牙黏著劑或乳膏或類似物。 [0016] 本發明之口腔護理組成物包括例如以重量計約i %至約5%之氟離子源(基於組成物之總重量為準)。儘管 20 200817017 =等百分比’氟離子源最佳之用量為能 離子的量至少約2,50〇ppm,於一此主風甲氟 η , '二㈡况中至多達約25,000
Ppm。敢佳地,氟離子存在之用 5 供此-濃度在適當Ppm範圍,㈣物^^嶋啊。為提 量百分比可予以變動,=不d:氟離子源之實際重 工… 知視不同鼠離子源之化學計量特性 2疋、。較存在於組成物中氟離子之用量為使組成物 4週'm:約89*百分比之氟化物回收率;最佳地,於 週後100百分比之氟化物回收率。 10 於車乂么具體例中’氣離子可由氟離子源予以提 15 =。^離子源可為能釋放氟離子於含水環境中之任意物 二細八型之來源包括氟離子之可溶鹽;諸如:氟化納、氟 化鉀、鼠化妈、氟化鋅、氟化銨辞、氣化鐘、氣化錄、氣 化錫、氟鍅酸錫及複合氟化物、單氟磷酸酯及…類, 諸如單氟麟酸納或單氟磷酸鉀、月桂胺氣化氣二二^基胺 基=基㈣胺氟化氫、二癸基二甲基氟化錢、氣化録蝶基 1"氟,一月桂基嗎鍬、肌胺酸氟化錫、甘胺酸氟化鉀 及甘胺酸氟化氫。參見例如美國專利案3,538,⑽、3,⑽, 637、3,711’604、3,911,1〇4、3,935,306 及 4,_,858,彼等 之内容全部併入本文作為參考。 20 [0018] >車乂佳地’本發明之口腔護理組成物亦可提供高回 收率之,氟離子。於本文中,術語"氟化物回收率”及"氟離子 回收率可互換且指的是存在口腔護理組成物中且可利用 供賦予使用者有企效果之活性氟離子(F·)之量,以可獲得 之氟離子之百分比予以表示。該值係基於涉及氣化物用之 200817017 離子$—性電極之離子性氟化物試驗以及核磁共振照相予 以測定_。此等試驗法係根據口腔抗齲齒調配物技藝中已 且被接受之標準程序。 Π ίο 15 ’9]…本發明之較佳的口腔護理組成物包括—有效量之 去,感劑。此等去敏感劑包括例如卸鹽,諸如硝酸卸、石户 酸風鉀、氯化鉀、檸檬酸卸及草酸卸;辣椒素;丁香广 釔鹽’鋅鹽’氣化物鹽及其之組合。此等藥劑可以有效 被添加’其較佳以重量計在介於約〇 〇1%至約卿(基於 組成物之總重量為準)之間變動,端視 土、 _〇]尤佳地,去敏感劑為卸鹽(諸如前述者^而^ 少約5重量%之鉀鹽(基於組成物之總重量為準)。 地,組成物包括以重量計約5%至約1〇%之卸鹽。^ 鹽之有效量及彼等之用途被描述於例如下 、.美 ==作為參考。最佳地,去敏感劑為確=1 重量=之==二護理組成物較佳另包括至少約 量=最?Γ二f之總重量為準),尤佳至少50重 之二夂60%至約75%之水。通常為較 者性牙:或抗麟齒潔齒劑(諸如 =夕的水’因為熟悉此項技藝者將期望】 產,液體之組成物。'淮,於其中口腔組成物為一種牙二 理組成物中之去敏感劑及氟離子源,而不會有氟 子源之不必要的損失,同時保持期望之濃度。水可1由 20 200817017 用之任何適當之水源且較佳為純化的水源, 诸如去離子及/或蒸餾水。 =2]r=地’本發明之口腔護理組成物亦包括-種水 5 10 插水膠體係充作一種乳化、增稠及/或凝膠 ,且為一種可進一步幫助保持氟離子之抗齲齒活性一 者。較佳之水膠體包括植物抽出物,諸如阿拉伯膠; =草卒取物,諸如黃原膠、洋菜膠及鹿肖㈣;植物種子 膠或,膠’諸如關華豆膠;穀物膠,諸如殿粉;發酵膠, :如葡萄聚糖;動物產品,諸如明膠;或此等水膠體之任 ^的、、且&尤仏地,水膠體為黃原膠。尤佳地,水膠體為 鹿角菜膠。最佳地,水膠體為包含硫酸鹽之鹿角菜膠。 [0023]水膠體應存在之用量基於組成物之總重量為準為 約0.5重量百分比至約15重量百分比,尤佳約〇 5百分比 至約1.5重量百分比。 15 [〇〇24]其他可用於本發明之口腔護理組成物中之選擇性 _增稠劑(單獨或與上述水膠體組合)包括(但不限於)··矽 石增稠劑;甘油;膠質,諸如黃耆膠、達瓦(ghatt〇樹膠、 蜜膠(veegum);藻酸鈉;果膠;羧甲基纖維素;羥基乙基 纖維素、羥基丙基纖維素;羥基甲基纖維素;羥基曱基羧 2〇基丙基纖維素;曱基纖維素;乙基纖維素;硫酸化纖維素; 以及此等化合物之混合物及組合物。此等增稠劑可單獨或 組合使用,用量基於組成物之總重量為準至多達組成物之 約15重量%。 [0025]除了前述成分外,本發明之口腔護理組成物亦可 200817017 包括一般用於口腔護理調配物中之各種共通額外的活性 劑,包括(但不限於)三氯生;三氯生單磷酸鹽;氯己丁 (chlorhexidine),亞勒西丁(aiexidine);己替丁(hexetidine); 金根驗(sanguinarine );苯扎氯索(benzalkonium chloride); 5水揚基苯胺;精胺酸酯;精胺酸月桂基乙酯;雙酚類;溴 化多明芬(domiphen);氯化十四基吡錠;氯化N_十四基_4_ 乙基吼錠;辛尼丁(octenidine);戴莫皮諾(delmopinol);辛 _ 皮諾(octapinol);尼新(nisin);辞離子劑;銅離子劑;精油; 呋喃酮;細菌素;前述活性劑之鹽類及其之混合物及組合 10 物。 [0026] 亦可使用供本發明之口腔護理組成物之選擇性添 ,加劑,諸如那些一般供形成潔齒劑者,包括(但不限於): 研磨劑及/或無定形矽石、濕潤劑、穩定劑、抗菌劑、甜 味劑、著色劑、表面活性劑、癒合劑、其他齲齒預防劑、 15螯合劑/钳合劑、維生素、胺基酸、蛋白質、抗牙菌斑劑、 _抗結石劑、遮光劑、抗生素、抗酵素劑、酵素、控制 劑、氧化劑、抗氧化劑、潔白劑及保存劑。 [0027] 一或多種研磨劑或磨光劑亦可被包括於本發明之 口腔濩理組成物中。研磨劑或磨光劑可為可接受供潔齒劑 20使用,不會過度研磨牙本質且可與口腔護理組成物相容1 任何物質。例示之研磨劑或磨光劑包括(但不限於)矽石、 鋁礬土、磷酸鹽、碳酸鹽及其之混合物、衍生物及鹽類及 樹脂型研磨物質。 [0028] _或多種濕潤劑可被添加至本發明之口腔護理組 12 200817017 成物中,用以提供調配物質地或組織及維持調配物中之水 分。有用之濕潤劑包括(但不限於):各種聚合性二醇及^ 他以羥基為底之濕潤劑,例如聚乙二醇、丙二醇、甘油: 季戊四醇、木糖醇、山梨糖醇、甘露糖醇、乳 / 澱粉水解物及㈣成分之組合物。 隸~虱化
ίο [00=9]若需要降低微生物’可使用抗菌劑,且可包括用 於潔齒調配物中之已知抗菌劑’例如苯甲酸、苯甲酸鈉、 苯曱酸鉀二硼酸及苯酚化合物’諸如P萘酚、氯化麝香草 酚、麝香草酚、茴香醚、桉油酚、香旱芹酚、薄荷醇、苯 紛、戊基料、己基苯盼、庚基苯朌、氟㈣吼鍵、 氣化鯨蝶基吡錠及溴化鯨躐基吡錠。 [0030] #需要,甜味劑可被用於本發明之口腔護理組成 物中’且可包括那些—般用於潔齒劑中以賦予產品怡人味 道者。適合之甜味劑包括(但不限於》糖精及其之衍生物、 賽克拉美及其之衍生物、阿西芬(acesulfane)_K、索馬丁 (jhaumatm)、新西斯派定(ne〇hispeddin)二氫查酮、銨化甘 卓素、右旋糖、左旋糖、嚴糖、甘露 他適合之甜味劑。 11、 ⑽ίΓ31]、—或多種表面活性劑亦可被包括於本發明之口腔 ^理組成物中。可供本發明之口腔護理調配物使用之表面 雜劑包㈣如陰離子表面活㈣、兩性料表面活性 3非離子表面活性劑、兩性表面活性劑及陽離面活 性劑。 [0032]所述之其他添加劑可為那些—般用於潔齒劑中且 200817017 可依據調配物之期望末端用途予以選擇以最佳化調配物之 物理及美學特性者。添加劑全體可以一般所使用之量被提 供至本文所述之口腔護理組成物中,較佳全體構成不大於 組成物之50重量%,尤佳不大於組成物之總重量之25重 5 量% 〇 [〇〇33]於另一具體例中,本發明係有關一種保持來自如 本文所述包括一種去敏感劑(諸如鉀鹽)之口腔護理組成 籲物中氟離子源之氟離子之抗鱗齒活性的方法。較佳地,該 方法包含提供一種口腔護理組成物,其包括至少約5,〇〇〇 10 ppm氟離子、去敏感劑(諸如鉀鹽)及至少約4〇重量%之 水0 [0034] 於另一具體例中,本發明之方法另包括提供口腔 護理組成物一種如本文所述之較佳的水膠體,較佳為鹿角 菜膠,最佳為包含硫酸鹽之鹿角菜膠。此水膠體(若使用 15之較佳用量為組成物之約〇·5重量%至約15重量%,尤佳 為組成物之約〇·5重量%至約ι·5重量% )可於4週後提 供約100%之氟化物回收率。 [0035] 本發明現參照以下之非限制實例予以描述: 實施例1 20 [0036] 5重量%之硝酸鉀被添加至牙膏調配物中供抗齲 齒及政感性治療用途。調配物之目標為包括範圍約5,〇〇〇 ppm或更多之氟化物。藉添加下列諸成分至下述且示於表 1中之以水為底之調配物中以製造調配物,並與包含標準 濃度I離子(l,l〇〇ppm)之傳統敏感性調配物(比較調配物 200817017 A)比較。 表1 成分 比較調配物A (敏感性) 調配物1 濕潤劑(山梨糖醇、 44.50 10.00 膠(黃原膠) 1.20 LOO 水 25.157 66.05 氟化鈉 0.243 (1,100 ppm F~) 1.10 (5,000 ppm F") 确酸鉀 5.00 5.00 糖精鈉 0.40 0.35 染料 ------- 0.30 0.30 矽石 21.00 14.00 月桂基硫酸鈉 1.20 1.20 香料 1.00 1.00 總計 100.00 100.00 馨[〇〇37]結果顯示當使用標準氟化物濃度(UGGppm)以 及5%硝酸鈉去敏感劑(如比較例調配物A)時,組成物 5具有理想之類似牙膏的物理特性及高氟化物回收率(約 100/6 )惟富氟化物濃度增加至5,000 ppm,而不增加水 濃度時,僅具有約50%之氟化物回收率。 [、〇〇38]調配物1類似於比較調配物A,但氟化物之濃度 增加至5,000 ppm,水量增加至66 〇5%。發現到調配物i 10不可預期地具有牙膏調配物之理想的物理特性,儘管包含 15 200817017 尚/辰度之氟離子及有致量之敏感劑。調配物1有理想的物 理特性及咼氟化物回收率之利益。於4週後,觀察到調配 物1有89%之氟化物回收率。 實施例2 [0039]凋配物2如下製備,調配物1和2之間的差異在 於所使用之水膠體。於調配物2中,使用含硫酸鹽之鹿角 采膠取代夏原膠,如下所述: 成分 ^— _ 調配物1 調配物2 濕潤劑(山梨糖醇) 10.00 10.00 膠 1.00(黃原膠) 1.00(鹿角菜膠) 水 66.05 66.05 氟化鈉 ΙΛ0 (5,000 ppm F ) L10 (5?000 ppm F") 硝酸鉀 5.00 5.00 糖精鈉 _ 0.35 0.35 染料 _________ — 0·30 0.30 矽石 — 14.00 14.00 月桂基硫酸鈉 1 70 L20 香料 ~ —------ LOO 1·00 總計 - 100.00 100.00 10 [0040]调配物2據發現具有如調配物1相同之理想的物 理特性’附加之利益為氟化物回收率在4週後維持得相當 16 200817017 高。雖然使用黃原膠在4週後之氟化物回收率很高(89%), 但以包含硫酸鹽之鹿角菜膠取代黃原膠,在4週後之氟化 物回收率更高(約1〇〇%)。 [〇〇41]㈣此項技藝者將知道在*偏離廣義發明概念之 :可對上述:具體例從事變化與替換。因此應瞭 明不限於所揭不之特定具體例, 本發 及範相之修飾,如附隨 〜在本%月之精神 之申¥專利範圍所定義者。
Claims (1)
- 200817017 十、申請專利範圍: 1 · 一種口_腔護理組成物,其包含 一充分量之氟離子源以提供至少約2,5〇〇 ppm之氟 離子; 5 15 一有效量之去敏感劑;及 至少約40重量百分比之水。 2·根據申請專利範圍第1項之口腔護理組成物,另包含一 種水膠體。 .根據:請專利範圍第2項之口腔護理組成物,其中水膠 體係選自由黃原膠、鹿角菜膠及其之組合所成組群中。 4.根據申請專利範圍帛3項之口腔護理組成物,其中水膠 體為包含硫酸鹽之鹿角菜膠。 5·根據申請專利範圍第2項之組成物,其中組成物包含基 於組成物之總重量為準約0.5重量百分比至約15重量 百分比之水膠體。 6.根據申請專利範圍第5項之口腔護理組成物,其中組成 物包合基於組成物之總重量為準約〇 5百分比至約J 5 重量百分比之水膠體。 7·根據申請專利範圍第丨項之口腔護理組成物,其中氟離 子源存在之用量以重量計為約丨%至約5%。 據申明專利範圍弟1項之口腔護理組成物,其中氟離 子源為氟化鈉。 9’根據申請專利範圍第1項之口腔護理組成物,其中氟離 子源係選自由氟化鉀、氟化鈣、氟化鋅、氟化銨鋅、氟 18 200817017 化鋰、氟化銨、氟化錫、氟锆酸鍚、單氟磷酸鈉、單氟 碟酸钾、月桂胺氟化氫、二乙基胺基乙基辛醯胺氟化 氮、二癸基二曱基氟化銨、氟化鯨蠟基吡錠、氟化二月 桂基嗎鏘、肌胺酸氟化錫、甘胺酸氟化鉀、甘胺酸氟化 5 氫及其之組合所成組群中。 1〇·根據申請專利範圍第1項之口腔護理組成物,其中去敏 感劑為鉀鹽。 | η·根據申請專利範圍第10項之口腔護理組成物,其中鉀 鹽為確酸鉀。 10 I2·根據申請專利範圍第11項之口腔護理組成物,其中組 • 成物包含以重量計約5百分比至約10百分比之硝酸鉀。 ‘ 13.根據申請專利範圍第i 〇項之口腔護理組成物,其中卸 鹽係選自由碳酸氫鉀、氯化鉀、檸檬酸鉀及草酸鉀所成 組群中。 15 I4·根據申請專利範圍第1項之口腔護理組成物,其中去敏 瞻感劑係選自由辣椒素;丁香酚;锶鹽;鋅鹽;氣化物鹽 及其之組合所成組群中。 15·根據申請專利範圍第丨項之口腔護理組成物,其中組成 物包含以重量計約60百分比至約75百分比之水。 20 16·根據申請專利範圍第1項之口腔護理組成物,進一步包 含至少一種其他活性劑,選自由錫離子劑;三氣生;三 氯生單磷酸鹽;氣己丁(chlorhexidine);亞勒西丁 (alexidine);己替丁(hexetidine);血根鹼;苯扎氣索 (benzalkonium chloride);水楊基笨胺;精胺酸酯;精胺 19 200817017 酸月桂基乙醋,雙紛類;漠化多明芬(domiphejj);氯化 十四基σ比錠;氯化十四基-4-乙基吼錠;辛尼丁 (octenidine);戴莫皮諾(delm〇pin〇1);辛皮諾 (octapinol);尼新(nisin);鋅離子劑;銅離子劑;精油; 5 吱喃酮;細菌素;其之鹽類;及其之組合所成組群中。 17·根據申請專利範圍第丨項之口腔護理組成物,進一步包 含至少一種其他添加劑,選自由研磨矽石、無定形石夕 ,石、濕潤劑、至少一種不同於口腔護理組成物之增稠劑 之第二增稠劑、穩定劑、抗菌劑、甜味劑及表面活性劑 10 所成組群中。 • I8·根據申請專利範圍第1項之口腔護理組成物,其中口腔 • 濩理組成物為一種牙膏。 19· 一種口腔護理組成物,其包含: 至少約2,500 ppm之氟離子; 15 以重i计約5百分比至約10百分比之鉀鹽; 馨 以重塁計約40百分比至約75百分比之水;及 以重1計約〇.5百分比至約15百分比之水膠體, I自由汽原膠及鹿角菜膠及其之組合所成組群中。 20·根據申請專利範圍第19項之口腔護理組成物,其中組 2〇 成物包含以重量計約0.5百分比至肖ΐ·5百分比之包含 硫酸鹽之鹿角菜膠。 據申叫專利範圍第2〇項之口腔護理組成物,其中口 腔護理組成物為一種牙膏。 22·種保持口腔護理組成物之抗齲齒活性之方法,包含: 20 200817017 提供一種包含至少約2,500 ppm之氟離子、有效量 之去敏感劑及至少約4〇重量百分比水之口腔護理組成 物;及 X 提供口腔護理組成物以重量計約〇·5百分比至約15 5 百分比之水膠體。 23.根據巾請專利範圍第22項之方法,其中水膠體為黃原 24.根射請專利範圍第22項之方法,其中水膠體為包含 硫酸鹽之鹿角菜膠。 10 15 I申::利範圍第22項之方法’其中包含硫酸鹽之 週後提供約100百分比之氟化物回收率。 26. 根據申印專利範圍第22項之方法, 物包含以重量計約6〇百分比至約75百分比之水。、、且成 27. ^f睛專利範圍第22項之方法,其中去敏感劑為峭 21 200817017 七、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 5 10 八、本案若有化學式時,請揭示最能顯示發明特徵的化學式: 無4
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| BRPI0409329A (pt) | 2003-04-14 | 2006-04-25 | Fmc Corp | processo para fabricar pelìculas de gel termorreversìveis, homogêneas, pelìcula homogênea, termorreversìvel, de sólidos altos, umidade baixa, processo para fabricar cápsulas moles, cápsulas moles, processo para fabricar uma forma de dosagem sólida, forma sólida, processo para preparar uma sistema de liberação de pelìcula de gel homogênea, e, sistema de liberação |
| JP3978609B2 (ja) | 2003-08-25 | 2007-09-19 | ライオン株式会社 | 口腔用組成物及び口腔用組成物中におけるラウリル硫酸カリウムの析出防止方法 |
| MY141722A (en) | 2004-06-23 | 2010-06-15 | Colgate Palmolive Co | Stable dentifrice compositions |
| AU2005270010A1 (en) * | 2004-07-02 | 2006-02-09 | Discus Dental, Llc. | Dental compositions with sensitivity relief |
-
2006
- 2006-06-30 US US11/479,678 patent/US8900558B2/en active Active
-
2007
- 2007-06-21 AU AU2007269423A patent/AU2007269423B2/en not_active Ceased
- 2007-06-21 JP JP2009518461A patent/JP5244100B2/ja not_active Expired - Fee Related
- 2007-06-21 RU RU2010141842/15A patent/RU2531102C2/ru active
- 2007-06-21 MX MX2008016308A patent/MX2008016308A/es active IP Right Grant
- 2007-06-21 CN CN201410053970.8A patent/CN103784340A/zh active Pending
- 2007-06-21 WO PCT/US2007/071719 patent/WO2008005688A2/en not_active Ceased
- 2007-06-21 BR BRPI0713071-6A patent/BRPI0713071A2/pt not_active Application Discontinuation
- 2007-06-21 RU RU2009102972/15A patent/RU2412689C2/ru active
- 2007-06-21 CA CA2655741A patent/CA2655741C/en not_active Expired - Fee Related
- 2007-06-21 EP EP07798854.1A patent/EP2046270B1/en not_active Not-in-force
- 2007-06-21 CN CNA2007800248880A patent/CN101484123A/zh active Pending
- 2007-06-29 AR ARP070102949A patent/AR061772A1/es unknown
- 2007-06-29 TW TW096123622A patent/TWI396544B/zh not_active IP Right Cessation
-
2008
- 2008-12-30 MY MYPI20085365A patent/MY155032A/en unknown
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2009
- 2009-01-05 ZA ZA2009/00063A patent/ZA200900063B/en unknown
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2014
- 2014-09-29 US US14/500,961 patent/US20150023890A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US8900558B2 (en) | 2014-12-02 |
| CA2655741A1 (en) | 2008-01-10 |
| RU2010141842A (ru) | 2012-04-20 |
| EP2046270B1 (en) | 2017-06-07 |
| MX2008016308A (es) | 2009-01-16 |
| US20150023890A1 (en) | 2015-01-22 |
| JP2009542705A (ja) | 2009-12-03 |
| US20080003187A1 (en) | 2008-01-03 |
| AU2007269423B2 (en) | 2011-02-17 |
| RU2412689C2 (ru) | 2011-02-27 |
| MY155032A (en) | 2015-08-28 |
| EP2046270A2 (en) | 2009-04-15 |
| AU2007269423A1 (en) | 2008-01-10 |
| BRPI0713071A2 (pt) | 2012-07-17 |
| AR061772A1 (es) | 2008-09-17 |
| WO2008005688A2 (en) | 2008-01-10 |
| RU2531102C2 (ru) | 2014-10-20 |
| CN103784340A (zh) | 2014-05-14 |
| ZA200900063B (en) | 2014-03-26 |
| WO2008005688A3 (en) | 2008-03-20 |
| CN101484123A (zh) | 2009-07-15 |
| JP5244100B2 (ja) | 2013-07-24 |
| RU2009102972A (ru) | 2010-08-10 |
| CA2655741C (en) | 2013-06-11 |
| TWI396544B (zh) | 2013-05-21 |
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| MM4A | Annulment or lapse of patent due to non-payment of fees |