Fairbrother KJ, Heasman PA: Anticalculus agents. J Clin Periodontol ; the research associated with the development of anticalculus agents and to evalu-. Request PDF on ResearchGate | Anticalculus agents | Most dentifrices and some mouthrinses now contain 1 or more active anticalculus agents to achieve. With the help of antiplaque and anticalculus agents. Chemical plaque control – Rationale. Gingivitis & periodontitis are highly prevalent diseases and.

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This invention relates to oral compositions, such as dentifrices and oral solutions, for the treatment or prevention of dental plaque, calculus, gingivitis, and mouth malodor.

Background of the Invention The mouth is a anticalculua for microbial growth and colonization. Within the mouth, the gums, lips, oral mucosa cheekpalate, tongue and teeth provide surfaces for the colonization and accumulation of bacteria. Teeth are unique in the oral cavity because they have hard, non-shedding surfaces where bacteria and their products dental plaque can significantly accumulate, especially in approximal areas and along the gingival crevice.

Dental plaque is a rough sticky film on the teeth that is made up of saliva, bacteria and food particles which adheres tenaciously to teeth at points of irregularity or discontinuity. Within a few hours of teeth cleaning, a film of salivary mucins, consisting primarily of proteins, forms on the teeth. Various oral bacteria colonize the antocalculus and multiply, forming a layer of plaque. Carbohydrate food debris adheres to the mucins and is digested by some types of plaque- causing bacteria.

The digestion produces antucalculus by-products which add to the plaque, and produces acid which erodes tooth enamel. The bacterial by-products produced in anficalculus oral cavity also include foul smelling gases which can result in malodor of the oral cavity. If not prevented or removed, plaque may become embedded with mineral salts, containing calcium and phosphate, to form a hard crusty antiicalculus, calculus or tartar, on the teeth. Calculus may be white or yellowish in color or may be stained or discolored by extraneous agents.

Calculus tends to be more unsightly than plaque and much more difficult to remove from the teeth. Anticlaculus toxins in plaque and calculus can irritate the gingival tissues surrounding the coated teeth, causing inflammation and destruction of the gums which can lead to other complications.

Zinc is an anticalculus agent; however, compositions containing zinc generally taste astringent and unpleasantly bitter. Like the chemical and biological activities, the negative aesthetics of the zinc cation are dose dependent: This coupled behavior between efficacy and aesthetics has limited the utility of zinc in oral compositions.

Pyrophosphate anticalculs also an anticalculus agent and, likewise, has an unpleasant taste which worsens with increased pyrophosphate concentration.

By carefully formulating zinc and pyrophosphate-containing compositions, it has been surprisingly found that the level of zinc in an oral composition can be increased, thus increasing the corresponding anticalculus effect, without greatly increasing the negative aesthetics of the composition. Applicants antixalculus surprisingly found that certain ratios of zinc: Detailed Disclosure of anticalfulus Invention This invention provides compositions effective against dental plaque formation, calculus formation, gingivitis, agejts mouth malodor.

Such compositions comprise certain zinc salts and certain molar ratio amounts of citrate and pyro relative to zinc in a pharmaceutically- acceptable carrier. Such topical oral carrier, when combined with Actives of this invention, results in a composition which is administered topically to the oral cavity. Preferably such compositions are held in the oral cavity for a period of time, and anticalvulus largely expectorated rather than being swallowed. Such compositions include mouthwashes, mouth rinses, mouth sprays, dental treatment solutions, toothpastes, liquid dentifrices and the like and are more fully described hereinafter.

Dentifrices and mouthwashes are the preferred compositions. The safe and effective amount of the compound or composition will vary with the particular condition being treated, the age and physical condition of the patient being treated, the severity of the condition, the duration of the treatment, the nature of concurrent therapy, the specific compound or composition employed, the particular pharmaceutically-acceptable carrier utilized, and like factors.


The term “comprising”, as used herein, means that various additional components can be conjointly employed in the compositions of this invention. As used herein, percentages listed are weight percentage of composition unless otherwise specified.

The amounts of pyro anticalculs citrate are expressed in terms of a ratio to the amount of zinc in the oral composition. On a molar basis, the amount of citrate relative to zinc is at least 0.

Likewise, the amount of pyro relative to to the amount of zinc is at least 1 when zinc is 1 i. Preferred zincxitrate ratios anticalcculus from about 1: Anticalcluus preferred is a zincxitrate: The aggents of zinc suitable for the purposes of this invention is from about 0. In dentifrice compositions, the preferred amounts of zinc are from about 0.

In mouthwashes, mouth rinses, mouth sprays and dental solutions, the preferred amount of anticalculuss is from about anticalcklus. The amount of citrate anion suitable for the purposes of this invention is from about 0. In dentifrice compositions, the preferred amounts of citrate anion are from about 0.

In mouthwashes, mouth rinses, mouth sprays and dental solutions, the preferred amount of citrate anion is from antocalculus 0. The amount of pyro anion suitable for the purposes of this invention is from about 0.

In mouthwashes, mouth rinses, mouth sprays and dental solutions, the preferred amount of pyro anion is from about 0. The preferred source of zinc ions is ZnO. Suitable sources of citrate ions include citric acid; alkali metal salts of citric acid, especially qgents citrate and potassium citrate; pharmaceutically acceptable hydrated and dehydrated salts of any of the above; and mixtures of any of the above.

Suitable sources of pyro ions are disclosed in U. Preferred polyphosphate ions are those of the above formula wherein n is 6, 13, and Preferred pyro ions are pyrophosphate ions. Preferred alkali metals are sodium and potassium; mixtures of alkali metal salts are acceptable. A more preferred source of pyro ions is a potassium salt of the pyro ion.

Compositions Components of the topical, oral carrier are suitable for administration to the oral cavity of a human or other animal and are compatible with one another and the other components, especially with the Actives, used in an oral composition of this invention. The term “compatible” as used herein, means that the components annticalculus capable of being anticalcukus with one another, in a manner such that there is no interaction which would substantially reduce the efficacy of the oral composition under ordinary use conditions.

Preferred topical, oral carriers provide the desired characteristics for mouthwashes, mouth rinses, mouth sprays, dental treatment solutions, toothpastes, dental gels, toothpowders, prophylaxis pastes, and the like. The topical, oral carriers of this invention comprise components typically used in such compositions which are well known to a skilled practitioner.

Such components include, but are not limited to, anticaries agents, antiplaque agents, anticalculus agents, dental abrasives, surfactants, flavoring agents, sweetening agents, binders, humectants, thickening agents, buffering agents, preservatives, coloring agents and pigments, ethanol and water. The pH of oral compositions of this invention is agens but can be varied to some anitcalculus. The compositions must be at a pH which is safe for contact with the tissues of the.

Otherwise, the pH of the compositions is preferably above pH 6, more preferably above pH 7, more preferably still, above pH 7.

During manufacture of a composition of this invention, the conditions for addition of each component should be optimized such that the pH of the mixture does not drop below formulation pH at any time during mixing of the ingredients.

To optimize stability of the final composition a pH antcalculus at least about 7. Water is a component of the topical, oral carriers of the compositions of the subject invention.

Anticalculus agents.

Water employed in the preparation of the commercially suitable compositions should preferably be of low ion content and antucalculus of organic impurities. Suitable binders for these compositions are those which are non-ionic at the formulation pH of the composition. As used herein “formulation pH” means the pH of the final composition. Suitable binders include, but are not limited to, natural gums such as gum karaya, gum arabic, and gum tragacanth; polysaccharide gums such as xanthan gum; and other natural products such as carrageenan; chemically modified natural products such as those based on cellulose esters, that is, carboxylmethylcellulose CMChydroxyethylcellulose HECand hydroxypropylcellulose HPC agwnts and synthetic binders such as polyvinylpyrrolidone; and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium anticqlculus hydroxyethyl cellulose.


An Overview on anticalculus agents – A review.

Carboxyvinyl polymer binders are less desirable, but may be used. Colloidal magnesium aluminum silicate or finely divided silica can be used as part of the thickening agent to further improve texture. Blends and mixtures of the suitable binders may significantly improve the characteristics of compositions made therewith.

Binders and thickening agents are generally present in the compositions of this invention in combined amounts of from about 0. Dental abrasives useful in the topical, oral carriers of the compositions of this invention include many different materials. The material selected must be one which is compatible with the composition of interest and does not excessively abrade dentin. These include, for example, silicas, including gels and precipitates, calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymeta-phosphate, insoluble sodium polymeta-phosphate, hydrated alumina, and resinous abrasive materials such as particulate condensation products of urea and formaldehyde, and other materials such as those disclosed by Cooley et al.

Mixtures of abrasives may also be used. Silica dental abrasives, of various types, can provide the unique benefits of exceptional dental cleaning and polishing performance without abticalculus abrading tooth enamel or dentin. For this reason they are preferred for anticalculuw herein. The silica abrasive polishing materials useful herein, as well as the other abrasives, generally have an average particle size ranging between about 0.

The silica abrasive can be precipitated silica or silica gels such as the silica xerogels described in U. Preferred precipitated silica materials include those marketed by the J. These silica abrasives are described in U. Mixtures of abrasives may be used. Flavoring agents can also be added to the oral compositions of this invention to make them more palatable. Suitable flavoring agents include menthol, oil antucalculus wintergreen, oil of peppermint, oil of spearmint, oil of sassafras, and oil of clove.

Coloring agents may be added to compositions of this invention to improve appearance. If present, coloring agents typically are included at levels of from about 0. Sweetening agents are also preferred in the compositions of this invention to make them more palatable.

Sweetening agents which can be used include aspartame, acesulfame, saccharin salts, dextrose, glucose, levulose thaumatin, D-tryptophan, dihydrochalcones, and cyclamate salts.

Anti-plaque and Anti-calculus Oral Care Product Testing

Saccharin salts are preferred. Oral compositions can also contain a surfactant. Suitable surfactants are those which are reasonably stable and form suds throughout the pH range suitable for compositions of this invention, including nonsoap anionic, nonionic, cationic, zwitterionic and amphoteric organic angicalculus detergents, and compatible mixtures thereof. Many of these suitable surfactants are disclosed in U.

Surfactants may also be used as solubilizing agents to help retain sparingly soluble components, e. Surfactants suitable for this purpose include polysorbates and poloxamers.

Another optional component of the oral carriers of the compositions of this invention is a humectant. The humectant serves to keep toothpaste compositions from hardening upon exposure to air, and to give mouthwash and toothpaste compositions a moist feel to the mouth.

Certain humectants can also impart desirable sweetness of flavor to mouthwash and toothpaste compositions. Suitable humectants for use in compositions of this invention include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, polyethylene glycol, and propylene glycol, especially sorbitol and glycerin. Preferred humectants are sorbitol and glycerin; more preferred is sorbitol. Opacifiers may also be used in toothpastes of this invention to render the toothpaste opaque.

Suitable opacifiers include titanium dioxide and some abrasives including, for example, magnesium aluminum silicate. Other optional components of the compositions of this invention are preservatives.