WO2001058416A2 - Pate dentifrice contenant un agent dentaire et des microbilles - Google Patents

Pate dentifrice contenant un agent dentaire et des microbilles Download PDF

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Publication number
WO2001058416A2
WO2001058416A2 PCT/US2001/040100 US0140100W WO0158416A2 WO 2001058416 A2 WO2001058416 A2 WO 2001058416A2 US 0140100 W US0140100 W US 0140100W WO 0158416 A2 WO0158416 A2 WO 0158416A2
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WIPO (PCT)
Prior art keywords
dental
agents
agent
microbeads
wax
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PCT/US2001/040100
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English (en)
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WO2001058416A3 (fr
Inventor
Christopher H. Suhonen
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Alticor Inc.
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Publication date
Application filed by Alticor Inc. filed Critical Alticor Inc.
Priority to AU2001251690A priority Critical patent/AU2001251690A1/en
Publication of WO2001058416A2 publication Critical patent/WO2001058416A2/fr
Publication of WO2001058416A3 publication Critical patent/WO2001058416A3/fr

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    • 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
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0241—Containing particulates characterized by their shape and/or structure
    • A61K8/0283—Matrix particles
    • 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
    • A61K2800/56—Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms

Definitions

  • This invention relates to dental care products that include a first dental agent and microbeads, where the microbeads contain a second dental agent.
  • the invention also relates to methods of using the dental care products, as well as methods of making novel microbeads that contain a dental agent.
  • a unique three- pronged approach to dentinal hypersensitivity results when the first dental agent and the second dental agent are the same.
  • Toothpastes often incorporate dental agents that assist with dental care in some way. It is common for toothpastes to include an agent for remineralizing teeth, reducing cavities, reducing bacterial infection, preventing plaque build-up, polishing teeth, reducing gum inflammation, reducing dentinal hypersensitivity, providing fluoride, or for reducing oral malodor. These agents are sometimes incorporated into the carrier of the toothpaste, and sometimes they are incorporated into the toothpaste in a micro-encapsulated form. By microcapsule is meant a small particle in which a core amount of dental agent is surrounded by a second material, typically a barrier or matrix material. In addition, other ingredients may also be encapsulated, such as flavors.
  • micro-capsule allows the incorporation of the agent without exposing the agent to reactions with other components of the toothpaste.
  • U.S. Pat. No. 5,976,507 describes a toothpaste that includes a microcapsule containing sodium fluoride useful for providing fluoride to the teeth, while a second microcapsule may contain calcium compounds useful for remineralizing teeth.
  • one or both agents are encapsulated to prevent their reaction and mutual self-depletion of the useful agent, i.e., by preventing the combination of the two agents from forming relatively inert calcium fluoride, which will neither provide fluoride nor remineralize teeth in its combined form.
  • a microcapsule features a central (liquid or solid) dental agent surrounded by a capsule of matrix or barrier material.
  • a microsphere or microbead may be thought of as a fissured object, in which a dental agent and a matrix material are intermixed. There is no central "core" area in which the dental agent is held.
  • microbeads are different from microcapsules, in that the matrix need not be ruptured or burst to release the dental agent. Rather, once a microbead is placed into the mouth of a user, the dental agent will leach out as the matrix or barrier material dissolves or erodes away.
  • Dentinal hypersensitivity may be a good example of an application where a timed release of a dental agent would be useful. Dentinal hypersensitivity is a painful condition caused by the development of pressure on nerve endings surrounding the odontoblast within a tooth. Exposure of the odontoblast and the nerve endings is generally due to recession of the gums or loss of tooth enamel, and frequently leads to hypersensitivity.
  • Dentinal tubules lead from the pulp to the cementum of the tooth. Dentinal tubules open to the surface of the tooth have a high correlation with dentine hypersensitivity. When the surface cementum of the tooth root is eroded, the dentinal tubules become exposed to the external environment. The exposed dentinal tubules provide a pathway for transmission of fluid flow to the nerves in the pulp. This transmission is induced by changes in temperature, pressure, and ionic gradients.
  • dentinal fluid can be initiated by evaporation of fluid at the open end of the tubule, such as by a blast of air upon the tooth. It can be caused by thermal expansion and contraction, as when consuming hot or cold drinks. Dentinal fluid may also move under the influence of hyper- osmotic solutions, such as chocolates or sweets.
  • tin salts such as stannous fluoride. It is believed that the stannous ion forms deposits of low solubility complexes of tin on the surface of exposed dentinal tubules, effectively blocking the openings. By thus passively blocking the tubule openings, external stimuli have a diminished effect, resulting in less pain. However, these complexes are only temporary, often removed when the teeth are cleaned, or even when they are merely rinsed.
  • Potassium nitrate is presently the sole active ingredient approved for the treatment of dentinal hypersensitivity. It is postulated that potassium ions interfere with the electro-chemical transfer or relay of sodium-initiated signals between the tubule and the adjacent nerve endings. Thus, potassium serves as a chemical/ionic mechanism to suppress pain. Potassium nitrate has been used in several ways to relieve this painful condition. For example, Alfano, et al., U.S. Pat. No. 5,939,048 discloses a toothpaste with about 5% potassium nitrate. Toothpaste is used in the normal manner, and the potassium nitrate is spread about on the gums and teeth along with the toothpaste. The potassium is effective to relieve and suppress pain, but the suppression is only temporary. Within minutes or hours, the pain reduction effect is lessened and the pain returns.
  • What is needed is an easy-to-use treatment that relieves dentinal pain, but also will remain for some time afterwards to provide longer-lasting relief to the user.
  • a treatment that incorporates dental agents in more than one form, so that at least one dental agent provides a function upon its application to the teeth of a user, while a second agent will function more slowly over time, allowing the second agent to provide its function to the teeth of a user over an extended period of time, without interfering with the first dental agent.
  • the present invention addresses the above problems and meets the needs by providing microbeads having a dental agent incorporated within their structure. Accordingly, the present invention provides a toothpaste that includes a carrier, a first dental agent and microbeads that comprise a matrix material and a second dental agent.
  • a dental care product has a first dental agent, and a second dental agent contained within a microbead structure.
  • the microbead structure is one in which there is a dental agent and a matrix material, and the two are intermixed. That is, there is no central body of dental agent protected from the outside, but rather the two materials are both open to the outside, and dental agent on the surface of the structure is free to react with outside reagents.
  • microbead may have any suitable shape dictated by manufacturing, as well as other considerations.
  • microbeads may be in the shape of cubes, pyramids, rounded cubes, ellipsoids, toruses, prolate spheres, oblate spheres, rounded parallelepipeds, and other geometries, as well as irregular objects.
  • Dental agents in microbeads may be used for a variety of purposes, including but not limited to, remineralizing of teeth, reducing cavities, reducing bacterial infection, preventing plaque build-up, reducing hypersensitivity, reducing gum inflammation, providing fluoride, and reducing oral malodor.
  • Other aspects of the invention include the composition and use of such microbeads in toothpastes.
  • Dental agents may be included in the compositions of toothpastes from about 0.01 % to about 40%, depending, of course, on the function of the agent and the need for that amount in the formulation.
  • Another aspect of the invention is a method of providing dental care by providing the dental product and using it.
  • the dental care products may include, but are not limited to, a toothbrush, a toothpaste, dental floss, mouthwash, and a rinse.
  • a user seeking dental care applies the product, and hence a composition according to the present invention, by using it in a normal manner.
  • Most appropriate here are a toothpaste and a dental floss, in which a first dental agent is incorporated in the carrier of a toothpaste or a coating of a dental floss.
  • a second agent or the same agent, is incorporated in the product in a microbead.
  • the microbeads lodge in the teeth.
  • the dental agent then is released over time, providing the dental care agent to the user over a period of time.
  • Microbeads and microspheres may be ideal vehicles for timed-release of dental agents.
  • dental products according to the present invention include a "carrier" for the dental agent and the microbeads.
  • the carrier is the bulk material of the toothpaste, normally sorbitol and other humectant or vehicle.
  • the carriers are the bristles of the toothbrush.
  • the carrier is the filament, fiber or polymer and the coating used for the floss.
  • the carrier is water or other base material for the mouthwash or rinse.
  • One embodiment of the present invention provides a toothpaste that contains potassium nitrate in the toothpaste carrier as a dental agent, which is available to the tubules as soon as the toothpaste is used.
  • the toothpaste also contains microbeads formed of a barrier material and the same or a different dental agent. These microbeads are desirably made from waxy or water-resistant materials, or from a film forming material, which will change shape, smear, and lodge within the tubules upon application.
  • the toothpaste composition of this embodiment will relieve dental hypersensitivity in three ways. First, the portion of the dental agent not incorporated within the microbeads will immediately contact the tubules to reduce hypersensitivity. Then, upon application of the toothpaste, the microbeads will physically block the tubules. Finally, after a period of time, all or some portion of the dental agent incorporated in the microbeads will migrate to the inner portion of the tubules to provide relief by delayed or extended release of potassium nitrate, the dental agent used in this embodiment.
  • Pain relief is thus provided in three ways: an initial application of potassium nitrate by its presence within the toothpaste; blocking of the dentinal tubules via the barrier material of the microbeads; and migration of potassium nitrate from the microbeads to the tubules.
  • a waxy material or film former, acting as a matrix material for the microbeads, may also form a film on the teeth or gums, providing a further basis for retention of potassium nitrate for later, gradual release to the tubules.
  • Another aspect of the invention is a "thermal" process for making microbeads, for inclusion in the toothpaste described above, with a matrix material and a dental agent. The method comprises several steps, beginning with heating and dissolving a gelatinous material in water.
  • microbeads in the desired range of 400-700 micrometers.
  • the microbeads are then screened and washed, and are incorporated as desired into the toothpaste.
  • a "chemical" process is used to make microbeads.
  • a gelatinous material is dissolved in water, and a dental agent, such as potassium nitrate, is mixed in.
  • This solution is then added to a previously prepared salt solution by forcing it through an orifice of a desired size. The temperature is then raised while agitating and the salt solution helps to form a porous micro-spherical structure.
  • the invention has many advantages, including a unique, three-pronged approach to dentinal hypersensitivity.
  • Use of microbeads may also enable the use of dental agents that are otherwise incompatible with ingredients in a toothpaste, as when a calcium compound for remineralization is desired for use a toothpaste incorporating fluoride as an anti-cavity agent.
  • Another example would be a formulation requiring both stannous fluoride and potassium nitrate. Placing one agent or the other in microbeads limits the availability of the agent or agents held in the microbeads, perhaps until at least a first rinse after use of the toothpaste.
  • Figure 1 is a depiction of a microcapsule.
  • Figure 2 is a depiction of a microbead.
  • Figure 3 is a flowchart for a thermal process for making microbeads.
  • Figure 4 is a flow chart for a chemical process of making microbeads.
  • Figure 5 is a flow chart for an alternative process.
  • Figure 6 is a schematic top view of dentinal tubules.
  • the present invention provides a dental care product comprising a carrier, a first dental agent and microbeads containing a second dental agent.
  • the first dental agent may be the same or different from the second dental agent.
  • the present invention also concerns methods of making the microbeads that are useful in the dental care products of the present invention.
  • the dental care product of the present invention will be described first.
  • a dental care product refers to any product that is used in oral hygiene or care of the teeth and gums.
  • a dental care product includes a carrier selected from the group consisting of toothpaste, dental floss, a toothbrush, a mouthwash and a rinse.
  • the carrier is a toothpaste
  • the ingredients forming the toothpaste include the required dental agent and microbeads and also those ingredients known to those of skill in the art. Because those ingredients are not critical to the practice of the present invention they will not be discussed further.
  • the dental agent can include any agent useful for oral hygiene and dental care.
  • the dental agent includes those ingredients effective for reducing bacteria, remineralizing of teeth, reducing cavities, preventing plaque build-up, reducing gum inflammation, reducing hypersensitivity, providing fluoride, and reducing oral malodor.
  • Anti-microbial agents suitable for use in microbeads according to this invention include, but are not limited to, sesquiterpene alcohol flavor compounds, xylitol, triclosan, cetylpyridinium chloride (CPC), thymal, eucalyptol, eugenol, and methyl salicylate, herbal ingredients such as licorice root, and mixtures thereof.
  • the anti-microbial is a sesquiterpene alcohol flavor compound selected from the group consisting of Famesol, Nerolidol, Bisabolol, and Santalol.
  • Farnesol is a nature-identical compound that was originally found in the essential oils of orange flower, oak lichen, lime blossom and sandlewood. It is an acylic primary sesquiterpene alcohol (3, 7, 11 -trimethyldodeca-2, 6, 10- trienol) that provides targeted efficacy against gram positive bacteria.
  • Remineralization agents include, but are not limited to, potassium phosphate, potassium glycerophosphate, calcium chloride, and ammonium phosphate.
  • Fluoridation agents include alkali metal fluoride salts, but are not limited to sodium fluoride and sodium monofluorophosphate, and tin salts, such as stannous fluoride.
  • Anti-caries agents include, but are not limited to, fluoride and xylitol.
  • Anti-plaque agents include, but are not limited to, zinc citrate and copper citrate.
  • Polishing agents include titanium dioxide, aluminum silicates and calcined alumina, such as kaolin.
  • Anti-tartar agents include, but are not limited to dialkali or tetraalkali metal pyrophosphate salts, such as Na 4 P 2 O 7 , K 2 P 2 O 7 , Na K 2 P 2 O 7 , Na 4 H 2 P 2 O 7 , and K 2 H 2 P 2 O 7 , calcium glycerophosphate, long chain polyphosphates such as sodium hexametaphosphate, sodium tripolyphosphate, and cyclic phosphates such as sodium trimetaphosphate.
  • Examples of anti-inflammatory agents are Chamomile oil and Allantoin. Zinc acetate may be used to reduce oral malodor.
  • hypersensitivity agents include potassium nitrate, calcium chloride, tin fluoride or potassium oxalate.
  • the first dental agent and the second dental agent are the same. Alternatively, in another embodiment, the first dental agent and the second dental agent are different.
  • the second dental agent may be included in either a microsphere or a microbead.
  • Figure 1 presents a schematic view of a microcapsule 10, in which a matrix or barrier material 11 surrounds a dental agent 13. The barrier material protects the dental agent until the microcapsule is burst or dissolves or erodes away.
  • Fig. 2 depicts a microbead 14 as used in this invention, in which a matrix material 15 is intermixed with a dental agent 17, and in which at least some of the dental agent is exposed to, and available from, the surface of the structure.
  • the second dental agent is included as part of a microbead that itself comprises a matrix material and the second dental agent. In a preferred embodiment of the invention, the second dental agent is included as a part of a microbead 14.
  • the matrix material is selected from the group consisting of a wax, a gelatinous material, a film forming polymer, and mixtures thereof.
  • the wax material is selected from the group consisting of wax, food-grade wax, microcrystalline wax, carnauba wax, beeswax, jojoba wax, silicon wax and mixtures thereof.
  • the gelatinous material is selected from the group consisting of agarose, alginate, carregeenan, chitosan, gelatin, albumin, and mixtures thereof.
  • the polymer material is selected from the group consisting of hydroxyl-terminated polymers in polyalkylene glycol, alkyl oxide terminated poiyamides, perfluoroethyl ethers, fluorosurfactants, and mixtures thereof.
  • the microbeads can be formed by including a dental agent into a waxy structure of a microbead.
  • a dental agent such as a dental agent
  • Such microbeads are available under the trade name Florasomes ® , which are commercially available from International Flora Technologies, Gilbert AZ.
  • the microbeads have the general properties described above, in that there is no central cavity with a dental active agent, but rather, the active ingredient is interspersed throughout a matrix of wax.
  • microbeads made from wax are especially effective if the wax incorporates a polytetrafluoroethylene (PTFE) fluoropolymer.
  • the polymer is desirably of low molecular weight, and is incorporated in the beads in an amount from about 0.01 to about 10%, preferably about 0.05 to about 2%, and most preferably from about 0.5 to about 1.0%.
  • the polymer is desirably in powdered form, with particles from about 1 to about 10 micrometers in diameter.
  • silicone spheres comprising a silicone elastomer coated with a silicone resin may be incorporated into the wax in an amount of from about 0.1 % to about 10%, preferably in a range of about 0.5% to about 2%.
  • the spheres are in a size range of 0.5 to 10 micrometers, preferably 0.7 to 2.0 micrometers diameter.
  • the silicone spheres are available from Shinetsu Chemical Co. of Tokyo, Japan.
  • Microbeads may also be formed through two processes, a thermal process and a chemical process. Instead of being made from a dental agent and wax, the beads may be made from a gelatin and an agent in a thermal process.
  • Figure 3 contains a flow chart illustrating the thermal process 20.
  • a gelatin solution is prepared 21 , using a food-grade gelatin, such as agarose, alginate, carregeenan, chitosan, gelatin or albumin, from about 0.5% to about 5.0% in deionized water.
  • the gelatin After the gelatin has been prepared, it is cooled 23 to a suitable temperature, and a desensitizing agent, such as potassium nitrate, is added 25 in an amount ranging from about 2% to about 10% of the weight of the gelatin and the solution is stirred.
  • a desensitizing agent such as potassium nitrate
  • This gelatin solution is then forced through an orifice of the appropriate size and then dripped 27 into a cool oil, so that microbeads are formed with diameters in the range of 300 to 2000 micrometers, and preferably 400-700 micrometers.
  • the oil is preferably a food grade oil, such as a vegetable oil, mineral oil or paraffin oil.
  • the microbeads thus formed are then screened, washed 29, and formulated into a dentifrice or other application.
  • microbeads will have the aforementioned gelatin as a matrix, with the dental agent interspersed throughout the matrix, rather than a central core of agent surrounded by matrix material
  • other materials which have been used to relieve dentinal hypersensitivity, include, but are not limited to, stannous fluoride, calcium chloride and potassium oxalate
  • the beads may also be made from a gel material using a "chemical" process 30, as shown in Fig 4
  • a “chemical” process 30 forms a structure having a gel matrix that contains a plurality of discrete portions/drops of the active material that are dispersed within the gel matrix
  • the polymeric material used to form the gel matrix is usually agarose, alginate, carregeenan, chitosan, gelatin or albumin
  • the gelatin material is dissolved 31 in water, and the dental agent is mixed in 33
  • This solution is then added 35 to a previously prepared 37 aqueous salt solution, preferably of zinc sulfate, zinc chloride or calcium chloride, by forcing the aqueous solution through an orifice of desired size and into the salt solution
  • the temperature is then raised while agitating 39
  • the microbeads are then screened and washed
  • This gelation process forms a microsphe ⁇ cal structure having a diameter in the range of about 300 to 2000 microns, or preferably, 400
  • microbeads were prepared with an alginate matrix An aqueous solution of 1-3% sodium alginate in deionized water is prepared, and potassium nitrate is added, at about 5 to 25% of the weight of the sodium alginate This alginate mixture was forced through an orifice of appropriate size into a previously prepared solution of 2% calcium chloride The mixture was then allowed to settle for about two hours before decanting and drying The resulting microbeads had diameters in the range of 300 micrometers to 700 micrometers.
  • film formers and at least one dental function agent may also be incorporated into microbeads.
  • film former is defined as a material that forms a protective film that will adhere to the dentin and enamel surfaces of the teeth, thereby providing a reservoir for the release of an agent to provide dental care.
  • Film former compounds suitable for use in this invention include polymers and silicone- based compounds.
  • the film former is a copolymer selected from the group consisting of hydroxyl-terminated polymers in polyalkylene glycol, alkyl oxide terminated poiyamides, perfluoropolypropyl ethers, fluorosurfactants, or combinations thereof.
  • the copolymer film former may be hydrophilic or hydrophobic.
  • hydroxyl-terminated polymers in polyalkylene glycol include, but are not limited to, polyolprepolymer 15 (“PP-15”), poiyolprepolymer 14 (“PP-14"), and polyolprepolymer 2 ("PP-2").
  • PP-15 is a hydrophilic mixture of the hydroxyl-terminated polymers in polyethylene glycol.
  • PP-15 is identified by the CTFA name PEG-8/SMDI copolymer and CAS # 39444-87-6.
  • PP-14 is a mixture of the hydroxyl-terminated polymers in polypropylene glycol.
  • PP-14 is identified by the CTFA name PPG-51/SMDI copolymer and CAS # 9042-82-4.
  • PP-14 poly [oxy(methyl-1 ,2-ethanediyl)], ⁇ -hydro- ⁇ -hydroxy-, polymer with 1 ,1 '- methylene-bis-[4,isocyanatocyclohexane].
  • PP-2 is a hydrophobic mixture of the hydroxyl-terminated polymers in polypropylene glycol. PP-2 is identified by the CTFA name PPG-12/SMDI copolymer and CAS # 9042-82-4. These film forming polymers may then be used by either the thermal or the chemical process described above to form microbeads containing an agent for a dental care purpose.
  • perfluoropolypropyl ether includes, but is not limited to, polyperfluoroisopropyl ether, which has the tradename Koflube LV.
  • fluorinated compounds including fluorosurfactants, are described in the article "Using Fluorinated Compounds in Topical Preparations", Bobin, M.F. et al., Cosmetics and Toiletries, Volume 11 , October 1996, the entirety of which is herein incorporated by reference.
  • a mixture of copolymers may be used in the dental complex.
  • One embodiment is PP-14 and polyperfluoroisopropyl ether.
  • a film former, a gelatinous material and a dental function agent may be individually combined to form microbeads either by the thermal process or the chemical process described above.
  • Microbeads may be made with film formers by the process shown above in Fig. 4.
  • a solubilized film former and a dental agent are mixed together.
  • a salt solution is prepared from calcium chloride, zinc chloride or zinc sulfate.
  • the microbeads are formed by forcing the solution of film former and agent through an orifice, the size of the orifice depending on the desired diameter of microbead.
  • the amount of salt added may be varied to adjust the relative hardness of the skin of the microbead. In general, the use of greater amounts of salt will cause the skin to be harder.
  • FIG. 5 Another way to form microbeads is to carry out the process shown in Fig. 5.
  • This flow chart describes the general method 40 for making microcapsules and microbeads containing a dental function agent.
  • An aqueous phase is prepared 41 by mixing together an emulsifier such as Airvol 523 and a defoamer such as n-octanol in a suitably sized reactor.
  • Other ingredients such as dyes, fragrances, colorants, light-scattering particulates, or herbal extracts, may also be added 42 to the aqueous phase.
  • the aqueous phase is agitated for a time sufficient to ensure proper mixing.
  • an oil phase is prepared 43 by dissolving an oil phase reactant such as Desmodur in the desired, oil-soluble core materials.
  • the desired core materials include at least one dental function agent, such as potassium nitrate.
  • agents for reducing hypersensitivity include, but are not limited to, potassium oxalate, calcium chloride, and stannous fluoride.
  • dental function agents for other purposes may be used as well.
  • Other ingredients such as fragrances, dyes and colorants, edible solids, light scattering particulates, film formers, and herbal extracts may also be added 44 to the oil phase.
  • Film former compounds suitable for use in this invention include polymers and silicone based compounds.
  • the film former is a copolymer selected from the group consisting of hydroxyl-terminated polymers in polyalkylene glycol, alkyl oxide terminated poiyamides, perfluoropolypropyl ethers, fluorosurfactants, or combinations thereof.
  • the copolymer film former may be hydrophilic or hydrophobic.
  • the next step is to add 45 the oil phase to the agitated aqueous phase so as to form an oil-in-water emulsion.
  • the oil-in-water emulsion is agitated 46 until the oil drop size is desirably about 150 to 300 micrometers.
  • the next step is to add 47 a water-soluble wall forming compound and water to the emulsion.
  • An example of suitable wall forming compound is diethylene triamine dissolved in water.
  • the fifth step is to raise 48 the temperature to about 50°C and let the system react at this temperature for about 3 hours while stirring at a relatively low speed (i.e., about 300 rpm or less).
  • the last step is to allow the system to cool 49 to room temperature, after which the agitation is stopped and the microcapsules are allowed to settle to the top or bottom of the reactor.
  • the microcapsules are washed and dried, they are ready to be further formulated or used as is in an oral care product.
  • the microcapsules may be further processed into microbeads by the process of Fig. 4, by adding the microcapsules in place of the dental agent in step 33.
  • a preferred embodiment of the dental care product of the present invention is a toothpaste for reducing hypersensitivity.
  • Figure 6 provides a top view of teeth 50 in which the tubules 52 between enameled portions 54 are exposed. This exposes the odontoblast areas 56 and exposed nerve endings 58 to movement of fluids within the tubules. As depicted within the figure, such movement may result from dehydration 60, heat 62, cold 64 or hyperosmotic solutions 66, and their effect upon the movement of fluids within the tubules. From the figure, it is apparent that one way to relieve dentin hypersensitivity is to block the entrances 68 to the tubules. Another way is to provide some sort of analgesic relief to the nerves in question.
  • At least one dental function agent to reduce hypersensitivity is formulated into a bead that is made from a material suitable to be ingested.
  • the dental agent to relieve hypersensitivity may be potassium nitrate, or may also be calcium chloride, tin fluoride, or potassium oxalate.
  • the beads are made from a wax or wax-based composition, or from a material that forms a film.
  • Preferred waxes include all those that are currently suitable for use in dental floss or other dental products. Examples include microcrystalline wax, carnauba wax, beeswax, jojoba wax, and silicon wax.
  • the wax may be combined with other compounds, film formers, to form the bead or encapsulating structure.
  • Film formers may also be used without the wax to form a microbead with an agent to relieve hypersensitivity.
  • These film formers include, but are not limited to, polymers such as polyalkylene glycol, alkyl oxide terminated poiyamides, perfluoropolypropyl ethers, fluorosurfactants, and food grade petroleum products such as octyl palmitate petrolatum.
  • the beads are formed from the dental function agent, titanium dioxide, octyl palmitate petrolatum and polyethylene.
  • the first mechanism to provide relief to the user is the incorporation of about 5 percent potassium nitrate within the toothpaste itself.
  • the relief lasts for a period of time, as described above, but while effective, is short-lived.
  • the second mechanism of action is the formation of a wax film occluding dentin tubule openings.
  • the film is created by compression and spreading of the wax beads during the tooth brushing process.
  • a physical barrier, or mechanical blockage, is formed over and closes the dentin tubule, thus preventing any movement of the dentinal fluid within. Without movement of dentinal fluid, pain is suppressed.
  • the third mechanism is the use of the wax- based bead as a controlled release delivery vehicle for potassium nitrate.
  • the bead when compressed and occluding the tubule, will function as a controlled release film providing a continual stream of potassium nitrate into the tubule, thus enhancing chemical suppression while also providing a mechanical blockage. All other pastes and rinses are ineffective and deficient in potassium nitrate after the customary final rinse with water.
  • a film former and dental function agent may be individually incorporated into other microbeads or microcapsules.
  • Dental function agents may be of the types mentioned above, or may comprise products that combine to provide the desired dental agent.
  • different film formers and dental function agents may be separately incorporated into the microbeads and incorporated into the dental product.
  • a toothpaste uses 1/3 part kaolin- loaded microbeads, 1/3 part film former-loaded microbeads, and 1/3 part potassium nitrate-loaded microbeads. It is believed that the film former will react with the reactive calcium-rich kaolin to form a substance that will at least temporarily block the entrances to the tubules. The potassium nitrate portion will provide longer-term relief as the potassium nitrate diffuses from the microstructure.
  • Another embodiment featuring multiple uses of beads in a toothpaste comprises calcium chloride in one set of beads and potassium oxalate in another. Once the beads are dissolved or ruptured during the use of the toothpaste, the calcium chloride and potassium oxalate precipitate out and act to block the dentinal tubules, thereby reducing the sensitivity of the teeth. Some relief may also be provided in an analgesic sense from the potassium ions, in the same manner and function as potassium nitrate. Other ingredients may also be added into other sets of beads, such as flavors. These flavors may include Farnesol, oils of peppermint, spearmint, wintergreen, clove, methyl salicylate and menthol. The flavoring may aid in making the use of these dental agents more pleasing.
  • one embodiment may, in the manner of Example 1 , above, include 1.5 % potassium nitrate-laden Florasomes ® and about 0.5% Farnesol-laden-Florasomes ® .
  • a toothpaste may include from 1-2% Florasomes ® , one-third each of a film former, kaolin, and menthol.
  • One advantage of placing at least some of these agents in microbeads (or microcapsules) is to prevent their reaction with other dental agents contained in the toothpaste proper. Since the dental agents leave the microbeads only very slowly, they may be used when the agent is otherwise incompatible with a dental agent used in the toothpaste, such as calcium compounds that are incompatible with fluoride compounds.
  • the present invention includes use of the dental care products described above.
  • the present invention includes a method of applying a dental agent that comprises (1) providing a toothpaste that includes a first dental agent and microbeads where the microbeads include a matrix material and a second dental agent, and (2) applying the toothpaste to the teeth and gums.
  • Another method according to the present invention is a method of applying a dental agent that comprises providing a dental floss that includes a first dental agent and microbeads where the microbeads include a matrix material and a second dental agent, and applying the dental floss between the teeth, thereby applying the floss to the teeth and gums.
  • Similar methods according to the invention utilize a toothbrush, a mouthwash, or a mouthrinse.
  • the product includes a first dental agent and microbeads having a second dental agent.
  • Example 1 A toothpaste containing potassium nitrate wax-based beads
  • the following is a toothpaste that incorporates wax-based beads containing potassium nitrate.
  • Example 2 A toothpaste containing potassium nitrate wax-based beads and Farnesol loaded-microbeads made from PP-14.
  • the following is a toothpaste that incorporates wax-based beads containing potassium nitrate (Florasomes ® ) as well as microbeads made from PP-14 matrix material and incorporating Farnesol, an anti-bacterial flavoring agent.
  • Example 3 A toothpaste containing sodium fluoride in agarose-based beads.
  • the following is a toothpaste that incorporates microbeads made from agarose and sodium fluoride.
  • potassium citrate may be used in place of potassium nitrate as a desensitizer
  • stannous chloride may be used in place of stannous fluoride, though in both cases the substitute is inferior to the preferred embodiment. While examples using toothpaste have been given, it is clear to those having ordinary skill in the art that these structures may be applied to other dental products as well.

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  • Life Sciences & Earth Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Physics & Mathematics (AREA)
  • Mathematical Physics (AREA)
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  • Epidemiology (AREA)
  • Cosmetics (AREA)
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Abstract

L'invention concerne une formule pour des produits de soins dentaires contenant un excipient, un premier agent dentaire et des microbilles contenant un second agent dentaire. Dans un mode de réalisation, une composition se présente sous la forme d'une solution unique à trois volets au problème de l'hypersensibilité dentinaire lorsque le premier agent et le second agent sont identiques. Une composition dentifrice contient du nitrate de potassium. Une partie du nitrate de potassium est contenue dans les microbilles afin de produire un soulagement à libération lente et à long terme. Une autre partie du nitrate de potassium est disponible librement dans la pâte dentifrice. En outre, les microbilles bloquent physiquement les tubules dentinaires afin de produire un soulagement accru. Par ailleurs, ces microbilles peuvent également contenir d'autres agents dentaires pour d'autres finalités, qui sont relatives à l'hygiène buccale ou au soins dentaires.
PCT/US2001/040100 2000-02-14 2001-02-14 Pate dentifrice contenant un agent dentaire et des microbilles WO2001058416A2 (fr)

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AU2001251690A AU2001251690A1 (en) 2000-02-14 2001-02-14 Toothpaste with dental agent and microbeads

Applications Claiming Priority (6)

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US50396400A 2000-02-14 2000-02-14
US09/503,964 2000-02-14
US62158900A 2000-07-21 2000-07-21
US09/621,589 2000-07-21
US66809400A 2000-09-22 2000-09-22
US09/668,094 2000-09-22

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WO2002053059A3 (fr) * 2000-12-29 2003-05-15 Kimberly Clark Co Fil de soie dentaire et ruban dentaire enduits d'hemostatique
US20070298060A1 (en) * 2006-06-09 2007-12-27 University Of Southern California Method for depletion of caries-causing bacteria in the oral cavity
DE102009036767A1 (de) 2009-08-08 2011-02-10 Evonik Degussa Gmbh Kompositpartikel für den Einsatz in der Mundhygiene
US8597789B2 (en) 2009-08-05 2013-12-03 Evonik Degussa Gmbh Microstructured multifunctional inorganic coating additives for preventing fouling (growth of biofilm) in aquatic applications
US9199211B2 (en) 2008-02-13 2015-12-01 Evonik Degussa Gmbh Storage-stable product systems for premix formulations
KR20160144210A (ko) * 2015-06-08 2016-12-16 주식회사 엘지생활건강 향료비드와 이를 포함하는 치약 및 이의 제조방법
US20170157171A1 (en) * 2014-03-21 2017-06-08 Omya International Ag Surface-reacted calcium carbonate for desensitizing teeth
US20200170942A1 (en) * 2017-05-26 2020-06-04 Church & Dwight Co., Inc. Oral care composition
CN111721598A (zh) * 2020-06-19 2020-09-29 内蒙古第一机械集团股份有限公司 一种测定稀土镁硅铁合金用化学熔剂
CN115381796A (zh) * 2022-08-24 2022-11-25 哈尔滨工业大学 一种载药形状记忆材料、制备方法及其应用

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Cited By (16)

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Publication number Priority date Publication date Assignee Title
AU2002231216B2 (en) * 2000-12-29 2006-03-02 Kimberly-Clark Worldwide, Inc. Hemostat coated dental floss and hemostat coated dental tape
WO2002053059A3 (fr) * 2000-12-29 2003-05-15 Kimberly Clark Co Fil de soie dentaire et ruban dentaire enduits d'hemostatique
US20070298060A1 (en) * 2006-06-09 2007-12-27 University Of Southern California Method for depletion of caries-causing bacteria in the oral cavity
US9199211B2 (en) 2008-02-13 2015-12-01 Evonik Degussa Gmbh Storage-stable product systems for premix formulations
US8597789B2 (en) 2009-08-05 2013-12-03 Evonik Degussa Gmbh Microstructured multifunctional inorganic coating additives for preventing fouling (growth of biofilm) in aquatic applications
DE102009036767A1 (de) 2009-08-08 2011-02-10 Evonik Degussa Gmbh Kompositpartikel für den Einsatz in der Mundhygiene
EP2347796A2 (fr) 2009-08-08 2011-07-27 Evonik Degussa GmbH Particules composites pour une utilisation dans les soins buccaux
US9248319B2 (en) 2009-08-08 2016-02-02 Evonik Degussa Composite particles for use in oral hygiene
US10463693B2 (en) * 2014-03-21 2019-11-05 Omya International Ag Surface-reacted calcium carbonate for desensitizing teeth
US20170157171A1 (en) * 2014-03-21 2017-06-08 Omya International Ag Surface-reacted calcium carbonate for desensitizing teeth
KR20160144210A (ko) * 2015-06-08 2016-12-16 주식회사 엘지생활건강 향료비드와 이를 포함하는 치약 및 이의 제조방법
KR102440320B1 (ko) 2015-06-08 2022-09-05 주식회사 엘지생활건강 향료비드와 이를 포함하는 치약 및 이의 제조방법
US20200170942A1 (en) * 2017-05-26 2020-06-04 Church & Dwight Co., Inc. Oral care composition
US11850301B2 (en) * 2017-05-26 2023-12-26 Church & Dwight Co., Inc. Oral care composition
CN111721598A (zh) * 2020-06-19 2020-09-29 内蒙古第一机械集团股份有限公司 一种测定稀土镁硅铁合金用化学熔剂
CN115381796A (zh) * 2022-08-24 2022-11-25 哈尔滨工业大学 一种载药形状记忆材料、制备方法及其应用

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