JP7551606B2 - ジメチコンベースの口腔ワニス - Google Patents
ジメチコンベースの口腔ワニス Download PDFInfo
- Publication number
- JP7551606B2 JP7551606B2 JP2021522361A JP2021522361A JP7551606B2 JP 7551606 B2 JP7551606 B2 JP 7551606B2 JP 2021522361 A JP2021522361 A JP 2021522361A JP 2021522361 A JP2021522361 A JP 2021522361A JP 7551606 B2 JP7551606 B2 JP 7551606B2
- Authority
- JP
- Japan
- Prior art keywords
- dimethicone
- fluoride
- oral
- donor
- varnish
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 229920000435 poly(dimethylsiloxane) Polymers 0.000 title claims description 189
- 235000013870 dimethyl polysiloxane Nutrition 0.000 title claims description 177
- 239000004205 dimethyl polysiloxane Substances 0.000 title claims description 172
- 229940008099 dimethicone Drugs 0.000 title claims description 168
- 239000002966 varnish Substances 0.000 title claims description 121
- 239000000463 material Substances 0.000 claims description 120
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims description 100
- 229940091249 fluoride supplement Drugs 0.000 claims description 99
- 239000000203 mixture Substances 0.000 claims description 60
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical group [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 60
- 238000002156 mixing Methods 0.000 claims description 53
- 238000009472 formulation Methods 0.000 claims description 45
- 239000011775 sodium fluoride Substances 0.000 claims description 30
- 235000013024 sodium fluoride Nutrition 0.000 claims description 30
- 229960000414 sodium fluoride Drugs 0.000 claims description 30
- 238000000034 method Methods 0.000 claims description 21
- 239000003795 chemical substances by application Substances 0.000 claims description 19
- 239000004615 ingredient Substances 0.000 claims description 18
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 16
- 239000011575 calcium Substances 0.000 claims description 16
- 229910052791 calcium Inorganic materials 0.000 claims description 16
- 239000013543 active substance Substances 0.000 claims description 15
- 239000004067 bulking agent Substances 0.000 claims description 13
- 235000003599 food sweetener Nutrition 0.000 claims description 13
- 239000003765 sweetening agent Substances 0.000 claims description 13
- 239000000796 flavoring agent Substances 0.000 claims description 12
- 239000004599 antimicrobial Substances 0.000 claims description 11
- 229910019142 PO4 Inorganic materials 0.000 claims description 10
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 10
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 10
- 239000010452 phosphate Substances 0.000 claims description 10
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 10
- 239000003755 preservative agent Substances 0.000 claims description 8
- 230000002335 preservative effect Effects 0.000 claims description 8
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims description 7
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims description 7
- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 claims description 7
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- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims description 6
- 229960004711 sodium monofluorophosphate Drugs 0.000 claims description 6
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- MFLAROGHONQVRM-UHFFFAOYSA-L calcium;dihydrogen phosphate;fluoride Chemical compound [F-].[Ca+2].OP(O)([O-])=O MFLAROGHONQVRM-UHFFFAOYSA-L 0.000 claims description 2
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- 229920000642 polymer Polymers 0.000 description 6
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- MHJAJDCZWVHCPF-UHFFFAOYSA-L dimagnesium phosphate Chemical compound [Mg+2].OP([O-])([O-])=O MHJAJDCZWVHCPF-UHFFFAOYSA-L 0.000 description 4
- 239000000499 gel Substances 0.000 description 4
- 239000004137 magnesium phosphate Substances 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 239000003921 oil Substances 0.000 description 4
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 4
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- 235000014102 seafood Nutrition 0.000 description 1
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- 238000005406 washing Methods 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/20—Protective coatings for natural or artificial teeth, e.g. sealings, dye coatings or varnish
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/15—Compositions characterised by their physical properties
- A61K6/16—Refractive index
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/60—Preparations for dentistry comprising organic or organo-metallic additives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/60—Preparations for dentistry comprising organic or organo-metallic additives
- A61K6/69—Medicaments
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/70—Preparations for dentistry comprising inorganic additives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- 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
- A61K8/20—Halogens; Compounds thereof
- A61K8/21—Fluorides; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
- A61K8/89—Polysiloxanes
- A61K8/891—Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61C—DENTISTRY; APPARATUS OR METHODS FOR ORAL OR DENTAL HYGIENE
- A61C19/00—Dental auxiliary appliances
- A61C19/06—Implements for therapeutic treatment
- A61C19/063—Medicament applicators for teeth or gums, e.g. treatment with fluorides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/59—Mixtures
- A61K2800/594—Mixtures of polymers
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Birds (AREA)
- Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Dentistry (AREA)
- Cosmetics (AREA)
Description
本出願は、米国特許商標局に2018年11月5日に出願された米国仮出願第62/755,705号の利益を主張し、この内容の全体は、参照により本明細書に組み込まれる。
ポリジメチルシロキサンまたはPDMSとしても知られるジメチコンは、ポリマーの繰り返し単位の数に基づく、様々なサイズのシリコーンベースのポリマーである。ジメチコンは、例えば、制汗剤、スキンクリーム、スキンローション、日焼け止めローション、バスオイル、ヘアケア製品、および経口製品用のコーティングにおける幅広い用途を有する。スキンケア製品は、幅広い用途を有し、ジメチコンは、幅広い化粧品配合物のベースとしてのその特性、その疎水性、粘度の範囲、潤滑特性、低表面張力、透明、無味、無臭、不活性のため、およびそれが他の広範囲の他の材料と混和性であるため、信頼されている。
経口ワニス配合物を作成する際、通常、配合物は、担体および活性成分を含むだけではなく、したがって、特定の配合物を生成するために、または配合物の、その一貫性、粘度、質感、味、感触を改善するために、通常は、賦形剤が添加され、あるいは他の活性成分を含めることによって、これらが改善される。
2つの異なる粘度のジメチコン製品、特にそのような粘度の差異を有する製品の混合物は、成分の製造および混合において重大な障害を提供する。実際には、単にすべての成分を混合ボウルに添加し、成分を混合/攪拌して、インスタント配合物を作成することはできない。適切なプロセスが生成されるまで、成分を完全に混合できるように、いくつかの異なるプロトコルが試験された。
Flacktekミキサーを使用して、次の化合物を混合した:ジメチコン(250万cP)、ジメチコン(1,000cP)、フッ化ナトリウム。最初に、17.1グラムの1,000cPのジメチコンを混合カップに添加した。次に、1グラムのフッ化ナトリウムを混合カップに添加した。2つの化合物を3,000RPMで10分間混合した。次に、1.9グラムの250万cPのジメチコンを0.38グラムずつ5回に分けて添加した。各増分を添加した後、配合物を追加の5分間の増分で混合した。
Flacktekミキサーを使用して、次の化合物を混合した:ジメチコン(250万cP)、ジメチコン(12,500cP)、フッ化ナトリウム。最初に、17.1グラムの12,500cPのジメチコンを混合カップに添加した。次に、1グラムのフッ化ナトリウムを混合カップに添加した。2つの化合物を3,000RPMで10分間混合した。次に、1.9グラムの250万cPのジメチコンを0.38グラムずつ5回に分けて添加した。各増分を添加した後、配合物を5分間の増分で混合した。
Flacktekミキサーを使用して、次の化合物を混合した:ジメチコン(250万cP)、ジメチコン(1,000cP)、フッ化ナトリウム、硝酸カルシウム。最初に、9.3グラムの1,000cPのジメチコンを混合カップに添加した。次に、1グラムのフッ化ナトリウムを混合カップに添加した。次に、0.2グラムの硝酸カルシウムを混合カップに添加した。3つの化合物を3,000RPMで10分間混合した。次に、9.5グラムの250万cPのジメチコンを1.9グラムずつ5回に分けて添加した。各増分を添加した後、配合物を追加の5分間の増分で混合した。
Flacktekミキサーを使用して、次の化合物を混合した:ジメチコン(250万cP)、ジメチコン(1,000cP)、フッ化ナトリウム、硝酸カルシウム、リン酸水素二カリウム。最初に、9.1グラムの1,000cPのジメチコンを混合カップに添加した。次に、1グラムのフッ化ナトリウムを混合カップに添加した。次に、0.2グラムの硝酸カルシウムを混合カップに添加した。次に、0.2グラムのリン酸水素二カリウムを混合カップに添加した。4つの化合物を3,000RPMで10分間混合した。次に、9.5グラムの250万cPのジメチコンを1.9グラムずつ5回に分けて添加した。各増分を添加した後、配合物を5分刻みで混合した。
Flacktekミキサーを使用して、次の化合物を混合した:ジメチコン(250万cP)、ジメチコン(12,500cP)、フッ化ナトリウム、硝酸カルシウム、リン酸水素二カリウム、およびスペアミント油。最初に、9グラムの1,000cPのジメチコンを混合カップに添加した。次に、1グラムのフッ化ナトリウムを混合カップに添加した。次に、0.2グラムの硝酸カルシウムを混合カップに添加した。次に、0.2グラムのリン酸水素二カリウムを混合カップに添加した。次に、0.1グラムのスペアミント風味を混合カップに添加した。5つの化合物を3,000RPMで10分間混合した。次に、9.5グラムの250万cPのジメチコンを1.9グラムずつ5回に分けて添加した。各増分を添加した後、配合物を5分刻みで混合した。
Flacktekミキサーを使用して、次の化合物を混合した:ジメチコン(250万cP)、ジメチコン(12,500cP)、フッ化ナトリウム、塩化ベンザルコニウム。最初に、9.3グラムの1,000cPのジメチコンを混合カップに添加した。次に、1グラムのフッ化ナトリウムを混合カップに添加した。次に、0.2グラムの塩化亜鉛を混合カップに添加した。3つの化合物を3,000RPMで10分間混合した。次に、9.5グラムの250万cPのジメチコンを1.9グラムずつ5回に分けて添加した。各増分を添加した後、配合物を5分刻みで混合した。
さらなる化合物を使用した追加の実験からのデータは、以下の表4で見出せる。
各配合物を評価すると、高粘度の250万cPジメチコンを配合物にさらに混合すると、得られた配合物の全体的な粘度の増加に基づいて材料を扱う能力が低下するというパターンが生じた。したがって、250万cPジメチコンの濃度の上限では、得られた生成物は、標準的なアプリケーターで歯の表面に適用するには粘度が高すぎた。しかしながら、対照的に、1:4(250万:1,000cP)の混合物では、混合物は試料の歯の表面に簡単に適用された。
Claims (19)
- 1,000cP~25,000cPの粘度を有する第1のジメチコン材料および200万~300万cPの粘度を有する第2のジメチコン材料と、少なくとも1つの活性剤と、を含み;前記第1のジメチコン材料と前記第2のジメチコン材料との比率が、100:1~1:8である、口腔ワニス。
- 前記少なくとも1つの活性剤が、フッ化物供与体である、請求項1に記載の口腔ワニス。
- 前記フッ化物供与体が、フッ化ナトリウム、フッ化第一スズ、モノフルオロリン酸ナトリウム、非晶質リン酸カルシウムフッ化物、フッ化アミン297、およびこれらの組み合わせからなる群から選択される、請求項2に記載の口腔ワニス。
- 前記フッ化物供与体の濃度が、前記口腔ワニスの総重量に対して2.5%~5.0%である、請求項2に記載の口腔ワニス。
- 前記フッ化物供与体の濃度が、15,000ppm~50,000ppmのフッ化物濃度をもたらす、請求項2に記載の口腔ワニス。
- リン酸塩供与体をさらに含む、請求項2に記載の口腔ワニス。
- カルシウム供与体をさらに含む、請求項2に記載の口腔ワニス。
- 香味料または甘味料をさらに含む、請求項2に記載の口腔ワニス。
- 塩化ベンザルコニウム、塩化セチルピリジニウム、およびそれらの組み合わせからなる群から選択される抗微生物剤をさらに含む、請求項2に記載の口腔ワニス。
- 増量剤、流動剤、防腐剤、またはこれらの組み合わせのうちの1つ以上をさらに含む、請求項2に記載の口腔ワニス。
- 前記増量剤が、食用ワックスである、請求項10に記載の口腔ワニス。
- L-リジンをさらに含む、請求項2に記載の口腔ワニス。
- 1,000cP~25,000cPの粘度を有する第1のジメチコン材料、および200万~300万cPの粘度を有する第2のジメチコン材料とフッ化物供与体を含むジメチコンベースの口腔ワニスの配合方法であって、前記第1のジメチコン材料の全体を混合容器に入れ、それに、ある量の前記フッ化物供与体を添加することと、遠心ミキサー内で、前記2つの成分を3,000RPMで10分間混合することと、前記混合工程後に、前記混合した2つの成分に前記第2のジメチコン材料の一部を添加することと、を含み、前記第2のジメチコン材料の総質量の一部が、少なくとも2つの増分で添加され、さらなる増分の添加前に、各増分が、3,000RPMで5分間個々に混合され、前記第2のジメチコン材料のすべてが配合物に添加されて混合されるまで、前記第2のジメチコン材料の一部を加える、方法。
- 少なくとも1つの活性剤をさらに含む、請求項13に記載の方法。
- 前記1つの活性剤が、前記成分を混合する前に、前記第1のジメチコン材料を有するカルシウム供与体および前記フッ化物供与体を含む、請求項13に記載の方法。
- 前記1つの活性剤が、抗微生物剤であり、前記成分を混合する前に、前記第1のジメチコン材料およびフッ化物供与体とともに添加される、請求項13に記載の方法。
- 増量剤、流動剤、防腐剤、またはこれらの組み合わせを、前記フッ化物供与体とともに添加することをさらに含む、請求項13に記載の方法。
- 前記抗微生物剤が、塩化ベンザルコニウム、塩化セチルフィルジニウム、およびこれらの組み合わせからなる群から選択される、請求項16に記載の方法。
- 1,000cP~25,000cPの粘度を有する第1のジメチコン材料、および200万~300万cPの第2のジメチコン材料と、口腔ワニス内に15,000~50,000ppmのフッ化物濃度を与えるフッ化物供与体と、少なくとも1つの活性剤から本質的になる口腔ワニスであって、前記第1と第2のジメチコン材料が、100:1~1:8の比率で提供される、口腔ワニス。
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