Dentifrice compositions containing polyphosphate and...

Drug – bio-affecting and body treating compositions – Dentifrices – Fluorine or fluorine compound containing

Reexamination Certificate

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C424S049000

Reexamination Certificate

active

06190644

ABSTRACT:

BACKGROUND OF THE INVENTION
Dental calculus, or tartar as it is sometimes called, is a deposit which forms on the surfaces of the teeth at the gingival margin. Supragingival calculus appears principally in the areas near the orifices of the salivary ducts; e.g., on the lingual surfaces of the lower anterior teeth and on the buccal surfaces of the upper first and second molars, and on the distal surfaces of the posterior molars.
Mature calculus consists of an inorganic portion which is largely calcium phosphate arranged in a hydroxyapatite crystal lattice structure similar to bone, enamel, and dentine. An organic portion is also present and consists of desquamated epithelial cells, leukocytes, salivary sediment, food debris, and various types of microorganisms.
As the mature calculus develops, it becomes visibly white or yellowish in color unless stained or discolored by some extraneous agent. This is undesirable from an aesthetic standpoint.
Mechanical removal of calculus periodically by the dentist is routine dental office procedure. A variety of chemical and biological agents have also been suggested to retard calculus formation or to remove calculus after it is formed. Pyrophosphate salts are chemical agents known to have the ability to retard calculus formation as described, for example, in U.S. Pat. No. 4,999,184, to Parran, Jr. et al., issued Mar. 12, 1991, the disclosure of which is incorporated herein by reference in its entirety.
In addition to the pyrophosphate salts, other polyphosphates are also know to help retard calculus formation. U.S. Pat. No. 4,627,977, issued Dec. 9, 1986, to Gaffar et al. discloses the use of linear molecularly dehydrated polyphosphate salts combined with a fluoride ion-providing source and a synthetic linear polymeric polycarboxylate which inhibit enzymatic hydrolysis of the polyphosphate salt in saliva. U.S. Pat. No. 4,247,526, to Jarvis et al., issued Jan. 27, 1981, discloses the use of a pharmaceutically acceptable condensed phosphate salt in addition to dicalcium phosphate dihydrate and trimagnesium phosphate. Although polyphosphate containing oral care products are known, there is a continuing need to develop stable products containing polyphosphates.
The present inventors have discovered that certain polyphosphates, in particular, linear polyphosphates with average chain lengths greater than 4 will significantly react with most ionic fluoride sources in oral compositions and alter the pH of the oral compositions. This reaction compromises the ability of the oral composition to provide stable ionic fluoride and polyphosphate to the oral surfaces. The inventors have discovered that the polyphosphates do not react with monofluorophosphate, under normal manufacturing, storage, and use conditions. Therefore, in a single phase dentifrice composition, monofluorophosphate a suitable fluoride ion source to be present with the polyphosphate and still deliver a constant and similar source/amount of fluoride.
Therefore, it is an object of the present invention to provide stable single phase oral compositions comprising monofluorophosphate and polyphosphates. It is also an object of the present invention to provide oral compositions with improved antitartar activity through the use of polyphosphates.
These and other objects of the present invention will become readily apparent from the detailed description which follows.
All percentages and ratios used herein are by weight of the oral composition, unless otherwise specified. All measurements are made at 25° C., unless otherwise specified.
SUMMARY OF THE INVENTION
The present invention relates to an oral composition comprising an effective amount of one or more linear polyphosphates having an average chain length of about 4 or more, from about 0.15% to about 2.28% of sodium monofluorophosphate, an effective amount of a buffering agent, from about 6% to about 70% of an abrasive polishing material containing less than 23% calcium, and from about 40% to about 99% of one or more aqueous carriers; wherein the oral composition has a total water content of from about 5% to about 20%.
DETAILED DESCRIPTION OF THE INVENTION
The oral composition of the present invention may be in the form of a toothpaste or dentifrice. The term “dentifrice”, as used herein, means paste, gel, or liquid formulations unless otherwise specified. The dentifrice composition may be in any desired form, such as deep striped, surface striped, multilayered, having the gel surrounding the paste, or any combination thereof. Alternatively, the oral composition may be one of the dentifrice compositions in a dual phase system comprising two dentifrice compositions contained in a physically separated compartment of a dispenser and dispensed side-by-side.
The term “dispenser”, as used herein, means any pump, tube, or container suitable for dispensing toothpaste.
The term “oral composition” as used herein means the total dentifrice that is delivered to the oral surfaces. The oral composition is a product, which in the ordinary course of usage, is not intentionally swallowed for purposes of systemic administration of particular therapeutic agents, but is rather retained in the oral cavity for a time sufficient to contact substantially all of the dental surfaces and/or oral tissues for purposes of oral activity.
The term “aqueous carrier” as used herein means any safe and effective materials for use in the compositions of the present invention. Such materials include abrasive polishing materials, peroxide sources, alkali metal bicarbonate salts, thickening materials, humectants, water, surfactants, titanium dioxide, flavor system, sweetening agents, xylitol, coloring agents, and mixtures thereof.
The present compositions comprise essential components, as well as optional components. The essential and optional components of the compositions of the present invention are described in the following paragraphs.
Polyphosphate Source
The present invention includes a polyphosphate source. A polyphosphate is generally understood to consist of two or more phosphate molecules arranged primarily in a linear configuration, although some cyclic derivatives may be present. Although pyrophosphates are a polyphosphate, the polyphosphates desired are those having four or more phosphate molecules. The pyrophosphates are discussed separately. The inorganic polyphosphate salts desired include tetrapolyphosphate and hexametaphosphate, among others. Polyphosphates larger than tetrapolyphosphate usually occur as amorphous glassy materials. Preferred in this invention are the linear “glassy” polyphosphates having the formula:
XO(XPO
3
)
n
X
wherein X is sodium or potassium and n averages from about 6 to about 125. Preferred are polyphosphates manufactured by FMC Corporation which are commercially known as Sodaphos (n≈6), Hexaphos (n≈13), and Glass H (n≈21). These polyphosphates may be used alone or in an combination thereof.
The phosphate sources are described in more detail in Kirk & Othmer,
Encyclopedia of Chemical Technology
, Fourth Edition, Volume 18, Wiley-Interscience Publishers (1996), incorporated herein by reference in its entirety, including all references incorporated into Kirk & Othmer. The polyphosphate source will typically comprise from about 0.5% to about 20%, preferably from about 4% to about 15%, more preferably from about 6% to about 10%, and most preferably from about 7% to about 9%, by weight of the oral composition.
Monofluorophosphate
The dentifrice composition of the present invention incorporates sodium monofluorophosphate. The oral compositions contain an amount of sodium monofluorophosphate that is capable of providing from about 50 ppm to about 3500 ppm, and preferably from about 500 ppm to about 3000 ppm of free fluoride ions. The sodium monofluorophosphate will be present in an amount of from about 0.15% to about 2.28% and preferably from about 0.30% to about 1.5%, by weight of the composition.
Buffering Agent
The present composition contains a buffering agent. If the oral composition is a dual phase system, a buffering agent w

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