Classifications

• • 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
  • 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
• • 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
  • A61K8/24—Phosphorous; Compounds thereof

Definitions

• This invention relates to certain carbonated calcium phosphate solutions that are unique in their applications as remineralizers of caries lesions, cavities and root erosions of the tooth, as mouth rinses and saliva substitutes. These solutions when further containing a fluoride compound can also be used for topical fluoridation of the teeth. When used for either fluoridation or mineralization these solutions prevent further tooth decay and actually restore the lesions caused by dental caries.
• the potential for application of dental remineralization is vast. Dentists fill millions of cavities each year. If these cavities where remineralized rather than filled the general dental health of the public would be increased substantially, since remineralization results in a whole tooth.
• the present invention seeks to provide remineralization compositions and methods that can practically be applied under a dentist's care and virtually replace the need for filling of the teeth.
• This invention involves methods and compositions for preparation of unstable carbonated calcium phosphate solutions, which are supersaturated with respect to calcium phosphate solids and carbon dioxide.
• the invention takes advantage of the fact that at alkaline pH aqueous solutions are capable of maintaining a greater amount of phosphate ions and carbonate ions in solution under atmospheric conditions. These alkaline solutions can then be mixed with acidic calcium solutions to create carbonated solutions useful for treating dental tissue.
• the carbonated solutions of the present invention When used to treat dental tissue the carbonated solutions of the present invention will deposit calcium phosphate compounds with or without fluoride on and in the tooth when applied for the prevention and/or repair of tooth weaknesses such as dental caries, exposed root, or dentin sensitivity.
• the deposition of the calcium phosphate compounds is controlled by the pH of the carbonated solutions.
• the pH of the solutions increases as carbon dioxide escapes and this facilitates the precipitation of the calcium phosphates over a range of time as needed.
• the advantages of the use of the calcium phosphate solution of the present invention as compared to the solutions and slurries of the prior art are many.
• the use of the compounds and methods of the invention allows for rapid formation of apatite upon dental tissues. Therefore, remineralization of the teeth can be achieved more quickly.
• the present invention provides for remineralization and fluoridation simultaneously when the carbonated solutions contain a fluorine compounds.
• Another significant advantage is that the present invention will not damage the teeth due to a large change in pH during the remineralization process.
• Yet another advantage of the present invention is the provision of a composition for remineralization of teeth which can be easily formulated and easily applied to the teeth.
• Still another advantage of the present invention is the easy formulation of remineralizing carbonated solutions from solid powders.
• a further advantage of the present invention is the provision of a composition which can be easily prepared and easily taken as an artificial saliva for individuals suffering from hyposalivation.
• the present invention provides compositions and methods for remineralization of caries lesions that are practical for the use in a clinic environment.
• the invention also provides compositions and methods for the rapid fluoridation of teeth by the use of fluoride containing carbonated calcium phosphate solutions.
• the present invention provides the compositions and methods that can remineralize and/or fluoridate the tooth and, in the case of exposed root and dentin sensitivity, obstruct the dentinal tubules.
• the solution can be used as mouth rinse. When properly formulated, this carbonated calcium phosphate solution can be used as an artificial saliva to serve as a replacement modality for individuals exhibiting hyposalivation.
• the solutions may further contain other beneficial ions such as fluorides, hydrogen peroxide and strontium.
• These alkaline carbonated phosphate solutions can be mixed with stable aqueous solutions containing high concentration of calcium ions at acidic pH.
• the resulting mixed solutions are supersaturated with respect to calcium phosphate and carbon dioxide.
• These mixed calcium phosphate solutions thus contain high calcium and phosphate concentrations at lower pH (preferably 5 to 7.5). Because of the supersaturated nature of the mixed solutions, calcium phosphate compounds will precipitate out of the mixed solution as the pH of the solution increases due to the release of carbon dioxide to the air. Therefore, when the mixed solution is put in the mouth, carbon dioxide will be released and calcium phosphate will precipitate on and in the teeth. The calcium phosphate then reacts with the dental tissue and forms apatite.
• the pH of the alkaline carbonated solutions is preferably between 8 and 12 and more preferably between 9 and 10.
• the desired pH and concentrations of the mixed carbonated calcium phosphate solution will determine what the acid concentration of the acidic calcium solution should be; the acid concentration is such as to make the pH of the mixed carbonated calcium phosphate solutions in the preferred range of 5 to 7.5.
• the mixed solutions with the same compositions and properties as the above solutions can also be obtained by mixing a stable alkaline carbonated solution that contains a large quantity of carbonate under atmospheric conditions with a stable acidic calcium phosphate solution.
• the phosphate originates from the acidic solution, rather than the alkaline solution.
• the phosphate ions may also originate from both solutions, i.e., both the alkaline carbonated solution and the acidic calcium solution may include phosphate ions.
• the mixed solution can also be obtained from the dissolution of solids in water.
• Stable solid powders containing all the ingredients in the mixed solutions can be created. These powders contain a mixture of calcium salts, phosphate salts, solid acid (such as acetic acid and/or citric acid) and carbonate salts with or without fluoride. When water is added to these powders, the solids will dissolve rapidly and the same carbonated calcium phosphate solutions as the mixed solutions can be obtained. These solutions can similarly be applied to dental surfaces for the prevention and repair of caries lesions, cavities, exposed roots and dentin sensitivity.
• the final mixed carbonated solutions of the present invention may further include other beneficial components including: complex fluorides, such as monof luorophosphate, f luorosilicates and f luorostannates; antiseptic agents, such as chlorhexidine; and further mineralizing materials, such as strontium.
• the final mixed carbonated solution of the present invention may further contain mucins, carboxymethylcellulose (CMC), and a sweetner, such as sorbitol or xylitol.
• the final mixed solution may also include hydrogen peroxide as an antiseptic agent.
• hydrogen peroxide is particularly preferred when the final mixed carbonated solution is created by dissolving powder in water. While hydrogen peroxide can be included in the alkaline carbonated solution and acidic solution mixture, under some conditions, it may render those solutions unstable.
• the following examples serve to illustrate the composition and method of invention, but are in no way limiting thereto.
• a first carbonated solution contains 50.6 mM of K 2 CO s , 7.4 mM of KH 2 P0 4 and 12.6 mM of H 3 P0 4 with pH of 9.69 and a second solution contains 33 mM of Ca(N0 3 ) 2 and 50.6 mM of acetic acid with pH of 2.5. Both solutions are stable under atmospheric pressure. When the two solutions are mixed, the mixed solution has the pH of 6.4 and is supersaturated with respect to calcium phosphate and carbon dioxide under atmospheric pressure. As the carbon dioxide evaporates the pH of the solution increases and calcium phosphate precipitates out of solution.
• EXAMPLE 1 The procedure of EXAMPLE 1 is repeated, except that phosphate compounds are added to the acidic calcium solution, instead of the alkaline solution.
• a first solution contains 50.6 mM K 2 CO s with a pH of 1 1.24
• a second stable calcium phosphate solution contains 7.4 mM KH 2 P0 4 , 12.6 mM H 3 P0 4 , 33 mM Ca(NO s ) 2 and 50.6 mM acetic acid with a pH of 2.29. Both solutions are stable under atmospheric pressure.
• the mixed solution has the pH of 6.4 and is supersaturated with respect to calcium phosphate and carbon dioxide under atmospheric pressure. As the carbon dioxide evaporates, the pH of the solution increases and calcium phosphate precipitates out of the solution.
• EXAMPLE 3 EXAMPLE 3
• a solid powder containing 54 mg calcium nitrate, 38 mg tripotassium phosphate, 3.5 mg potassium monohydrogen phosphate, 30.4 mg acetic acid and 50.7 mg potassium bicarbonate is created.
• 20 mL of water is added to the solid powder, the powders dissolve quickly and creates a solution having the same properties as the mixed solution in EXAMPLE 1, i.e. the solution has the pH of 6.4 and is supersaturated with respect to calcium phosphate and carbon dioxide under atmospheric pressure. As the carbon dioxide evaporates the pH of solution increases and calcium phosphate precipitates. Therefore, this solution can be applied directly to the tooth as a mineralizing solution.
• a carbonated solution is prepared according to the procedure of EXAMPLE 1.
• the mixed solution is promptly applied directly to the dental tissue. Carbon dioxide escapes from the solution and calcium phosphate precipitates out of solution and is deposited on and into the dental tissue.
• a carbonated solution is prepared according to the procedure of EXAMPLE 3. The solution is then promptly applied directly to the dental tissue. Carbon dioxide escapes from solution and calcium phosphate precipitates out of solution and is deposited on and into the dental tissue.
• a carbonated solution is prepared according to the procedure of EXAMPLE 1 , except that the acidic calcium solution also includes 1 mM fluorosilicate ions.
• EXAMPLE 7 A carbonated solution is prepared according to the procedure of EXAMPLE
• the acidic calcium solution also includes 1 mM fluorostannate ions.
• a carbonated solution is prepared according to the procedure of EXAMPLE 1, except that the carbonated phosphate solution also contains 5 mM fluoride ions.
• a carbonated solution is prepared according to the procedure of EXAMPLE 1, except that the acidic calcium solution also contains 33 mM strontium ions.
• EXAMPLE 10 A carbonated solution is prepared according to the procedure of EXAMPLE
• the solid mixture also includes 2.5 mM fluorine compound.
• a carbonated solution is prepared according to the procedure of EXAMPLE 3, except that the solid mixture also includes 0.33 mM strontium compound.
• a stable alkaline carbonated solution is created, containing 30 mM K 2 C0 3 and 50 mM K 2 HP0 4 at a pH of 10.6.
• This alkaline carbonated solution is used as a mouth rinse and removes acidic residue from the teeth thereby preventing cavities which might have resulted from the acidic residue.
• the preferred embodiment of the present invention is now fully described.

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• Health & Medical Sciences (AREA)
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• Birds (AREA)
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• Oral & Maxillofacial Surgery (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Cosmetics (AREA)
• Dental Preparations (AREA)
• Medicines Containing Material From Animals Or Micro-Organisms (AREA)

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• 1995
  • 1995-02-24 JP JP8525639A patent/JPH11500724A/ja active Pending
  • 1995-02-24 EP EP95911936A patent/EP0871427A1/de not_active Withdrawn
  • 1995-02-24 WO PCT/US1995/002364 patent/WO1996025914A1/en not_active Application Discontinuation
  • 1995-02-24 AU AU19319/95A patent/AU695356B2/en not_active Ceased

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