CA2329622C - Remineralizing oral compositions comprising palatinit - Google Patents

Remineralizing oral compositions comprising palatinit Download PDF

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Publication number
CA2329622C
CA2329622C CA002329622A CA2329622A CA2329622C CA 2329622 C CA2329622 C CA 2329622C CA 002329622 A CA002329622 A CA 002329622A CA 2329622 A CA2329622 A CA 2329622A CA 2329622 C CA2329622 C CA 2329622C
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palatinit
sodium
oral composition
remineralization
zinc
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CA2329622A1 (en
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Tsutomu Takatsuka
Akira Nakao
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Sunstar Inc
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Sunstar Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/20Halogens; Compounds thereof
    • A61K8/21Fluorides; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27Zinc; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis

Abstract

The present invention is directed to an oral composition comprising palatini t. More particularly, the invention discloses an oral composition comprising palatinit which exerts a synergistic effect when combined with a fluorine or zinc compound.< /SDOAB>

Description

REMINERALIZING ORAL COMPOSITIONS COMPRISING PALATINIT
Technical Field The present invention relates to an oral composition comprising palatinit, and more particularly, it relates to an oral composition comprising palatinit which exhibits a synergistic effect when combined with a fluorine or zinc compound.

Background ~

Dental caries are a state of a dental carious activity caused by the dissolution of calcium from teeth and which cannot. naturally return to a healthy state. But, there-is a state referred to as a sub-surface lesion which can return to the healthy state, in the course of the development of the. dental carious cavity ("Zusetsu Ushoku-gaku"
edited by Shoichi, Suga, 1990, 139). Therefore, in order to decrease dental caries, it is desirable to enhance the remineralization so that the teeth can return to a healthy state within a term during which the teeth return to the original state.

As a method for enhancing the remineralization, the use of fluorine compounds has been known for a long time., However, because the ingestion of a large amount of fluorine exhibits the toxicity, it is desired that fluorine be effectively utilized in as small ~

an amount as possible. To accoznplish this, the use of a substance that enhances the remineralization effect of fluorine is exemplified. For example, there is proposird a combination of fluorine and hydroxy-apatite in JP-A-1-110608. However, its effect is insuffficient and is not satisfactory.

On the other hand, a zinc compound that has been utilized in oral compositions generally has an astringent or salty taste. Therefore, it is unsuitable as it has a very bad feeling when used.

One object of the present invention is to provide an oral composition which has high safety and can enhance remineralization. Another object of the present invention is to provide an oral composition which exhibits the sufficient remineralization effect and has a better feeling when used.

Disclosure of Invention In view of the above circumstances, the present inventors have intensively studied substances that can enhance remineralization and, as a result, have found that palatinit exhibits excellent properties, that an oral composition comprising palatinit can enhance remineralization, and, further, that the inclusion of palatinit in combination with a fluorine or zinc compound can enhance remineralization due to the synergistic effect of both ingredients. This resulted in the completion of the present invention.

Palatinit has hitherto been utilized in foods and the like as a low cariogenic sweetener. However, palatinit has never been utilized for oral use, and its remineralization effect is not known.

That is, the present invention was completed based on such novel findings, and, in a first aspect, provides an oral composition comprising palatinit which has high safety and can enhance a remineralization.

Moreover, in a second aspect, the present invention provides an oral composition comprising palatinit and a remineralization enhancing ingredient, which exhibits a sufficient remineralization effect and has a better feeling when used.

The present invention is described below in detail according to the first and second aspects thereof in sequence.

[First aspect]

Palatinit to be used in the first and second aspects of the present invention is a sugar alcohol of a disaccharide, and may be a -D-glucopyranosyl-1, 6-mannitol, its isomer, a -D-glucopyranosyl-1, 6-sorbitol or a mixture thereof. Palatinit can be obtained by hydrogenation of palatinose which is converted from sucrose as a raw material with glycosyltransferase. And, palatinit is also the name of the product of Mitsui Sugar Co. Ltd. or Sudzucker A.G, and is also referred to as reduced-palatinose or isomalt. Palatinit is widely known as a non-cariogenic sugar which scarcely develops dental caries, based on the fact that the cariogenic microorganisms do not produce acids from palatinit in an oral cavity. Palatinit has been blended in non-sugar foods or a specified health food such as so-called "dental caries-resistant candy".

The amount of palatinit to be blended in the present oral composition is in the range of 0.1% to 60% by weight, preferably 1% to 40% by weight, based on the total weight of the oral composition. When the amount is less than 0.1% by weight, the desired effect cannot be obtained. On the other hand, when the amount is more than 60% by weight, the stability of the formulation is deteriorates.

[Second aspect]

The remineralization enhancing ingredient to be used in the second aspect of the present invention is an ingredient which can remineralize the teeth from its sub-surface lesion state. Examples of the remineralization enhancing ingredient are fluorine compounds, zinc compounds, phosphorus compounds, calcium compounds and the like, but not limited thereto.

Examples of the fluorine compound to be used in the second aspect of the present invention as the remineralization enhancing ingredient are sodium fluoride, potassium fluoride, ammonium fluoride, stannous fluoride, sodium or potassium monofluorophosphate and the like. Particularly preferred are sodium fluoride and sodium monofluorophosphate.

These fluorine compounds, alone or in combination thereof, may be blended in the present oral composition in the range of 0.1-5,000ppm, preferably 100-1,100ppm in terms of fluoride ion, based on the total weight of the present oral composition.

Further, the zinc compound to be used in the second aspect of the present invention as the remineralization enhancing ingredient is preferably a water-slightly soluble zinc compound, wherein the water-slightly soluble zinc compound is defined as having a solubility of less than 0.5g per 100g of water at 25 C, and a water-insoluble zinc compound is included therein. Among them, particularly preferred are zinc oxide, zinc citrate and zinc stearate. From the viewpoint of taste, the water-slightly soluble zinc compound having a smaller particle diameter and a greater specific surface area is preferred. More particularly, preferred are those having a particle diameter of not greater than 0.3 m and the specific surface area of greater than 10m2/g.
When the particle diameter exceeds 0.3 m, the astringency becomes strong. Examples of the commercial products of the zinc compound are fine particle zinc white and hyperfine TM
particle zinc oxide, "FINEX series" manufactured by Sakai Chemical Industry Co., Ltd.
These water-slightly soluble zinc compounds, alone or in combination thereof, may be blended in the oral composition in the amount of 0.1% to 5% by weight, based on the total weight of the present oral composition.

Further, when the oral composition of the second aspect of the present invention contains a zinc compound, preferred pH thereof is within the range of 6.0 to 8.5. When pH is lower than 6.0, then the astringency is strong, and when pH is higher than 8.5, then oral mucosa may be irritated, therefore, the composition out of the above pH range is not preferred.

Further, examples of the phosphorus compound to be used in the second aspect of the present invention as the remineralization enhancing ingredient are disodium hydrogenphosphate, sodium dihydrogenphosphate, dipotassium hydrogenphosphate, 5 potassium dihydrogenphosphate, trisodium phosphate, tripotassium phosphate and the like, but not limited thereto.

Moreover, examples of the calcium compound to be used in the second aspect of the present invention as the remineralization enhancing ingredient are calcium chloride, calcium nitrate, calcium sulfate, calcium carbonate, calcium citrate, calcium hydrogenpyrophosphate, calcium gluconate, calcium glycerophosphate, calcium hydroxide, calcium oxide, calcium silicate and the like, but not limited thereto.
That is, the present invention provides an oral composition comprising palatinit alone or in a combination with any remineralization enhancing ingredients, which can enhance the remineralization due to the synergistic effect of both ingredients.

The oral composition of the present invention may be properly formulated, depending upon its use, into a form such as a toothpaste, powder or liquid dentifrice, wetting dentifrice, gel, cream, paste, mouthwash, spray, foam, coating agent and the like, according to a conventional procedure. Other ingredients to be blended therein are not particularly limited, and the known active ingredients, polishing agents, humectants, thickening agents, foaming agents, preservatives, flavoring agents, sweeteners, pH
adjusting agents, organic acids, sugar alcohol, anti-oxidizing agents and others known as ingredients for oral compositions may be blended in the oral composition, as long as they do not deteriorate the effects of the present invention.

Examples of the active ingredient are enzymes such as amylase, protease, lysozyme and dextranase, the antimicrobial agents such as sanguinarine, allantoin, aminobenzoate derivatives, hexetidine, chlorhexidine, triclosan and cetylpyridinium chloride, vitamins such as vitamin B, C and E, and the astringents such as potassium nitrate, lithium nitrate and sodium nitrate.

Examples of the polishing agent are silica, alumina, aluminosilicate, aluminium hydroxide and the like.

Examples of the humectant are glycerol, propylene glycol, sorbitol, polyethylene glycol, polypropylene glycol and the like.

Examples of the thickening agent are sodium carboxymethyl cellulose, methyl cellulose, hydroxyethyl cellulose, alginates, xanthan gum, carrageenan, gum arabic, polyvinyl alcohol and the like.

Examples of the forming agent are anionic-, nonionic-, cationic- and amphoteric-surfactants. Examples of the anionic-surfactant are alkyl sulfates, sodium dodecylbenzene sulfonate, amino acids, sulfosuccinates, sucrose fatty acid esters and the like. Examples of the nonionic-surfactant are the PluronicTM series, polyoxyethylene-polyoxypropylene copolymer, fatty acid dialkanolamides and the like.
Examples of the preservative are methylparaben, propylparaben, benzoates, sodium benzoate, paraoxybenzoic acid esters, titanium dioxide and the like.

Examples of the flavoring agent are peppermint oil, spearmint oil, Japanese peppermint oil, orange oil, menthol, cloves oil, anise oil, wintergreen oil, eucalyptus oil and the like.

Examples of the sweetening agent or sweetener are saccharin salts, dextrose, aspartame, xylitol, stevia extract, acesulfame, granulated sugar, powdered sugar, starch syrup and the like. Although palatinit exhibits sweetness, the above sweetening agents or sweeteners may be added depending upon the feeling for use of the formulation.

Examples of the pH adjusting agent are citric acid and salts thereof, phosphoric acid and salts thereof, malic acid and salts thereof, gluconic acid and salts thereof, maleic acid and salts thereof, aspartic acid and salts thereof, gluconic acid and salts thereof, succinic acid and salts thereof, glucuronic acid and salts thereof, fumaric acid and salts thereof, glutamic acid and salts thereof, adipic acid and salts thereof, lactic acid and salts thereof, pantothenic acid and salts thereof, hydrochloric acid, alkali metal hydroxides and the like.

Brief Description of Drawing~

Figure 1 is a graph which compares the remineralization effects of the various sugars in a system not containing fluoride.

Figure 2 is a graph which compares the remineralization effects of the various sugars in a system containing fluoride.

The Best Mode for Carrying Out the Invention The present invention will be further illustrated by way of the following Examples, which are not to be construed to limit the scope of the present invention.
The amounts indicated in the Examples are all percents (%) by weight.

Experimental Example 1 Evaluation of the remineralizing ability I

The remineralization effect of the sugars was evaluated in an in vitro test using a bovine tooth according to the procedures described in D. J. White et al., Caries Res., 21, 228 (1987).

1. An enamel section having 4mm length X 3mm width was obtained from a bovine tooth. The section was embedded in a dental resin to obtain an enamel block.

2. An enamel varnish was applied to a portion of approximately 1/3 of the surface of the enamel block in order not to cause the demineralization of that portion.
Then, the enamel block was demineralized with a demineralizing solution containing 50% of saturated hydroxyapatite/ 0.1M lactic acid/ pH 5.0 to prepare artificial caries.
3. An enamel varnish was applied to a portion of approximately 2/3 of the surface of the treated enamel block in order not to cause the remineralization of that portion. The enamel block was immersed for ten days in a test solution prepared by adding the test sugar into an aqueous solution containing 3.0mM calcium ion and 1.8mNI phosphate ion so that the concentration of the sugar became 20%, to perform the remineralization treatment.

4. Three thin sections having approximately 500 m in thickness were prepared from the enamel block. The central portion of the thin sections was ground so that the thickness became approximately 100 u m using a double-side polishing machine.

5. The X-ray photograph was taken of the thin section prepared in the fourth step. The mineral amounts of the demineralized portion and the remineralized portion were calculated based on the brightness of each portion and a distance from the surface using an image processor. The mineral amount difference between the demineralized and remineralized portions was expressed as a remineralization value.
A greater value thereof shows the greater remineralization. A control test was performed in a similar manner to that described above, except that the test solution containing only 3.0mM calcium ion and 1.8mM phosphate ion but not containing the sugar was used.

The results are shown in Table I and Figure 1.
Table I

Systems not containing fluoride Sugar (20%) Remineralization value Control 405 Sorbitol 645 Mannitol 640 Xylitol 416 Erythritol 602 Trehalose 715 Palatinit 1057 Unit: Vol. %,u m Further, a similar test was performed in which sodium fluoride was added to the test solution to 2ppm in terms of fluoride ion.

The results are shown in Table 2 and Figure 2.
Table 2 Systems containing fluoride (2ppm) Sugar (20%) Remineralization value Control 1626 Sorbitol 1358 Mannitol 1377 Xylitol 1636 Erythritol 1330 Trehalose 1205 Palatinit 2374 Unit: Vol. % m From Tables I and 2, it was found that, among the sugars tested, palatinit has a particularly excellent remineralizing ability and that the remineralizing ability is enhanced by combining palatinit with sodium fluoride.

Experimental Example 2 Evaluation of the remineralizing ability 2 The remineralization enhancing effects of the oral compositions to which the various sugars had been added were tested in vitro according to a similar manner to that described in Experimental Example 1.

Provided that, in the remineralization treatment, a solution containing 3.0mM
5 calcium ion and 1.8mM phosphate ion to which a test dentifrice (see Table 3) had been added so as to form a 4-fold slurry was used, and the immersion period was set to be fourteen days. The results of the X-ray photograph were evaluated using the image processor according to a similar manner to that described in Experimental Example 1.
The results are shown in Table 3.

Table 3 Ingredients Example E:ample Example Ezample Ezomple Ezample ComparaHve Comparative Comparative Comparative Comparatlve 1 2 3 4 5 6 Ezam le 1 Ezam le 2 Ezam le 3 Ezam le 4 Example 5 Silicic acid 20 20 20 20 20 20 20 20 20 20 20 anhydride Sodium 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 carboxymethyl cellulose W
Sorbitol 40 40 35 25 15 15 45 45 35 35 35 Sodium lauryl 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 N
sulfate Saccharin 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0 sodium 0 Sodium fluoride - 0.2 0.2 0.2 0.2 0.2 - 0.2 0.2 0.2 0.2 Flavor 1 1 1 1 1 1 1 1 1 1 1 Xylitol - - - - - - - - 10 - -Erythritol - - - - - - - - - 10 -Trehalose - - - - - - - - - - 10 Palatinit 10 5 10 20 30 60 Remineralization 852 1328 1468 1496 1548 1580 320 1024 958 842 862 value From the above Table 3, it was found that palatinit has particularly excellent remineralizing ability, also in the evaluation of Examples 1-6 and Comparative Examples 1-5.

Experimental Exam lp e 3 Evaluation of the remineralizing ability 3 The remineralization enhancing effect of the oral composition to which the zinc compound had been added was tested in vitro according to almost the same manner as that described in Experimental Example 1.

Provided that, in the remineralization treatment, a solution containing 3.0mM
calcium ion and 1.8mM phosphate ion to which the test dentifrice (see Table 4) had been added so as to form a 4-fold slurry was used, and the pH cycling procedure was taken in which the enamel block was additionally immersed in the demineralization solution for three hours per day. An evaluation period was set to be fourteen days.

The results of the X-ray 'photograph were evaluated using the image processor according to a similar manner to that described in Experimental Example 1. The results are shown in Table 4.

Table 4 Ingredients Example 7 Example 8 Example 9 Example 10 Example 11 Exonple 12 Example 13 Comparative Comparative Ezam le 6 Exam le 7 Silicic acid 20 20 20 20 20 20 20 20 20 anhydride Sodium 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 carboxymethyl cellulose W
Sorbitol 40 40 35 25 35 35 35 50 35 0) Sodium lauryl 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 sulfate Saccharin 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 sodium Sodium fluoride - 0.2 0.2 0.2 0.2 0.2 0.2 - 0.2 Flavor 1 1 1 1 1 1 1 1 1 X litol - - - - - - - - 10 Palatinit 10 10 10 20 10 10 10 - -Zinc oxide 1 - 1 - - 0.1 5 1 -Zinc stearate - - - 1 - - - - -Zinc citrate - - - - 1 - - - -Remineralization 102 513 542 516 630 530 721 10 354 value From the above Table 4, in the evaluation of Examples 7-13 and Comparative Examples 6-7, it was shown that the remineralization is enhanced by blending palatinit and a zinc compound.

Fxperimental Example 4 Organoleptic evaluation of the astringency I

The oral compositions of Examples 14-16 and Comparative Examples 8-9 in Table 5 were prepared. Ten healthy persons used these oral compositions according to a conventional manner, and the astringency after spout was organoleptically evaluated.

The total points of ten healthy persons are shown according to the following 3 grades-criteria: 2: excellent; 1: good; 0: astringent.

The results are shown in Figure 5.

Table 5 Ingredients Example 14 Example 15 Example 16 Comparative Comparative Example 8 Exam le 9 Silicic acid 20 20 20 20 20 anhydride Sodium 1.5 1.5 1.5 1.5 1.5 carboxymethyl cellulose Sorbitol 35 35 35 35 35 Sodium lauryl 1.5 1.5 1.5 1.5 1.5 sulfate Saccharin sodium 0.1 0.1 0.1 0.1 0.1 Sodium fluoride 0.2* 0.2 0.2 0.2 0.2 Flavor 1 1 1 1 1 Zinc oxide I 1 - - I -Zinc oxide 2 - I - - -Zinc oxide 3 - - I - 1 Palatinit 10 10 10 - -Total point 15 17 17 0 2 * The concentration in terms of fluoride ion is 905ppm.

Zinc oxide 1: The average particle diameter is 0.5 u m and the specific surface area is 8m2/g.

5 Zinc oxide 2: The average particle diameter is 0.28 m and the specific surface area is 10mz/g.

Zinc oxide 3: The average particle diameter is 0.04 ,.c m and the specific surface area is 25m2/g.
10 From the above Table 5, it was found that the astringency can be improved by decreasing the average particle diameter of zinc oxide or increasing the specific surface area thereof, and can be further improved by combining with palatinit.

Experimental Example 5 15 Organoleptic evaluation of the astringency 2 The oral compositions of Examples 17-18 and Comparative Example 10 having varied pH values were prepared, and evaluated according to a similar manner to that described above.

The results are shown in Table 6.

Table 6 Ingredients Example 17 Example 18 Comparative Example 10 Silicic acid anhydride 20 20 20 Sodium carboxymethyl 1.5 1.5 1.5 cellulose Sorbitol 35 35 35 Sodium laur l sulfate 1.5 1.5 1.5 Saccharin sodium 0.1 0.1 0.1 Sodium fluoride 0.2 0.2 0.2 Flavor 1 1 1 Zinc oxide 2* 1 1 1 Palatinit 10 10 10 Disodium 0.1 0.1 0.1 h dro en hos hate Sodium 0.25 0.2 0.3 dih dro en hos hate pH 6.0 7.0 5.0 Total point 16 17 10 * The average particle diameter is 0.28 p m and the specific surface area is 10m2/g.
From the above Table 6, it was shown that the astringency can be improved by adjusting pH of the oral composition to 6.0 or higher.

Example 19 Toothpaste A toothpaste was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 10.0 Sodium fluoride 0.2 (The concentration in terms of fluoride ion is 905ppm) Silicic acid anhydride 16.0 Sodium carboxymethyl cellulose 1.3 Sodium lauryl sulfate 1.0 Titanium dioxide 0.4 Paraoxybenzoic acid ester 0.1 Citric acid 0.1 Trisodium citrate 0.3 Saccharin sodium 0.1 Flavor 0.6 Sorbitol 50.0 Purified water balance Total 100.0 Example 20 Toothpaste A toothpaste was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 30.0 Silicic acid anhydride 20.0 Sodium carboxymethyl cellulose 1.2 Sodium lauryl sulfate 1.2 Titanium dioxide 0.3 Hydrochloric acid 0.5 Saccharin sodium 0.13 Sorbitol 10.0 Flavor 1.0 Purified water balance Total 100.0 Example 21 Toothpast A toothpaste was prepared with the following formulation according to conventional procedures.

Inereients Amounts %
Palatinit 50.0 Sodium fluoride 0.2 (The concentration in terms of fluoride ion is 905ppm) Silicic acid anhydride 16.0 Carrageenan 1.3 Sodium lauryl sulfate 3.5 Titanium dioxide 0.4 Paraben M 0.1 Xylitol 10.0 Flavor 0.7 Glycerol 5.0 Purified water balance Total 100.0 Example 22 Toothpaste A toothpaste was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 15.0 Sodium monofluorophosphate 0.76 (The concentration in terms of fluoride ion is 950ppm) Calcium carbonate 16.0 Sodium carboxymethyl cellulose 1.3 Sodium lauroylsarcosinate 2.0 Polyoxyethylene hydrogenated castor oil 1.0 Titanium dioxide 0.4 Paraoxybenzoic acid ester 0.1 Malic acid 0.2 Stevia extract 0.1 Flavor 0.7 Sorbitol 40.0 Polyethylene glycol 5.0 Purified water balance Total 100.0 Example 23 Toothpaste A toothpaste was prepared with the following formulation according to conventional procedures.

5 Ingredients Amounts %
Palatinit 5.0 Sodium fluoride 0.21 (The concentration in terms of fluoride ion is 950ppm) Triclosan 0.5 10 Silicic acid anhydride 16.0 Sodium polyacrylate 2.0 Sodium lauryl sulfate 1.0 Pluronic TM 1.0 Titanium dioxide 0.4 15 Paraoxybenzoic acid ester 0.1 Xylitol 10.0 Flavor 0.7 Sorbitol 50.0 Purified water balance 20 Total 100.0 Example 24 Mouthwash A mouthwash was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 10.0 Sodium fluoride 0.05 (The concentration in terms of fluoride ion is 225ppm) Sodium lauryl sulfate 0.5 Polyoxyethylene hydrogenated castor oil 1.0 Sodium dihydrogenphosphate 0.1 Disodium hydrogenphophate 0.1 Saccharin sodium 0.1 Flavor 0.7 Ethanol 10.0 Glycerol 10.0 Purified water balance Total 100.0 Example 25 Mouthwash A mouthwash was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 30.0 Polyoxyethylene hydrogenated castor oil 1.0 Sodium citrate 0.2 Citric acid anhydride 0.2 Flavor 0.8 Glycerol 10.0 Purified water balance Total 100.0 Example 26 Mouthwash A mouthwash was prepared with the following formulation according to conventional procedures.

jpgredients Amounts %
Palatinit 10.0 Sodium fluoride 0.05 (The concentration in terms of fluoride ion is 225ppm) Sodium lauryl sulfate 0.2 Polyoxyethylene (2)-synthetic C,Z, C14 alkyl-sodium sulfosuccinate 0.2 Malic acid 0.3 Flavor 0.7 Glycerol 10.0 Xylitol 5.0 Purified water balance Total 100.0 Example 27 Gel dentifrice A gel dentifrice was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 10.0 Hydroxyethyl cellulose 3.0 Sodium fluoride 1.0 (The concentration in terms of fluoride ion is 4,500ppm) Phosphoric acid 3.0 Saccharin sodium 0.5 Flavor 0.8 Glycerol 20.0 Purified water balance Total 100.0 Example 28 Non aerosol-type foam dentifrice A non aerosol-type foam dentifrice was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 5.0 Sodium fluoride 1.0 (The concentration in terms of fluoride ion is 4,500ppm) Phosphoric acid 3.0 Tripotassium phosphate trihydrate 1.5 Sodium lauryl sulfate 1.0 Pluronic 7.0 Coconut oil fatty acid diethanolamide 0.5 Saccharin sodium 0.8 Flavor 0.7 Ethanol 5.0 Purified water balance Total 100.0 Example 29 Oral gel An oral gel was prepared with the following formulation according to conventional procedures.

Irgredients Amounts %
Palatinit 20.0 Carboxymethyl cellulose 0.2 Glycerol 40.0 Grape seed extract 1.0 a -tocopherol 0.05 Purified water balance Total 100.0 Example 30 Toothnaste A toothpaste was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 10.0 Sodium fluoride 0.21 (The concentration in terms of fluoride ion is 950ppm) Silicic acid anhydride 21.0 5 Sodium carboxymethyl cellulose 1.1 Sodium lauryl sulfate 0.5 Sodium lauroylsarcosinate 0.1 Titanium dioxide 0.3 Fine particle zinc oxide 1.0 10 (The average particle diameter is 0.3 p m: the specific surface area is 10mZ/g) Paraoxybenzoic acid ester 0.1 Saccharin sodium 0.1 Flavor 0.7 Xylitol 1.0 15 Sorbitol 38.0 Hydrochloric acid (2N) 1.0 Purified water balance Total 100.0 pH 6.5 Example 31 Toothpaste A toothpaste was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 50.0 Zinc stearate 1.0 Sodium fluoride 0.21 (The concentration in terms of fluoride ion is 950ppm) Silicic acid anhydride 16.0 Carrageenan 1.3 Sodium lauryl sulfate 3.5 Titanium dioxide 0.4 Paraben 0.1 Xylitol 10.0 Flavor 0.7 Glycerol 5.0 Purified water balance Total 100.0 pH 7.0 Example 32 Toothpaste A toothpaste was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 15.0 Zinc citrate 0.5 Sodium monofluorophosphate 0.75 (The concentration in terms of fluoride ion is 950ppm) Calcium carbonate 16.0 Sodium carboxymethyl cellulose 1.3 Sodium lauroylsarcosinate 2.0 Polyoxyethylene hydrogenated castor oil 1.0 Titanium dioxide 0.4 Paraoxybenzoic acid ester 0.1 Malic acid 0.2 Stevia extract 0.1 Flavor 0.7 Sorbitol 40.0 Polyethylene glycol 5.0 Purified water balance Total 100.0 pH 7.5 Example 33 Toothpaste A toothpaste was prepared with the following formulation according to conventional procedures.

Ineredents Amounts %
Palatinit 5.0 Fine particle zinc oxide 1.5 (The average particle diameter is 0.3 u m: the specific surface area is 10m2/g.) Sodium fluoride 0.21 (The concentration in terms of fluoride ion is 950ppm) Triclosan 0.5 Silicic acid anhydride 16.0 Sodium polyacrylate 2.0 Sodium lauryl sulfate 1.0 Pluronic 1.0 Titanium dioxide 0.4 Paraoxybenzoic acid ester 0.1 Xylitol 10.0 Flavor 0.7 Sorbitol 50.0 Hydrochloric acid (IN) 1.5 Purified water balance Total 100.0 pH 6.8 Example 34 Mouthwash A mouthwash was prepared with the following formulation according to conventional procedures.

In,gredients Amounts %
Palatinit 10.0 Zinc citrate 0.1 Sodium fluoride 0.05 (The concentration in terms of fluoride ion is 225ppm) Sodium lauryl sulfate 0.5 Polyoxyethylene hydrogenated castor oil 1.0 Sodium dihydrogenphosphate 0.1 Disodium hydrogenphophate 0.1 Saccharin sodium 0.1 Flavor 0.7 Ethanol 10.0 Glycerol 10.0 Purified water balance Total 100.0 pH 6.0 Example 35 Mouthwash A mouthwash was prepared with the following formulation according to conventional procedures.

Ingredients Amounts %
Palatinit 10.0 Fine particle zinc oxide 0.1 (The average particle diameter is 0.3 u m: the specific surface area is 10mZ/g) Sodium fluoride 0.05 (The concentration in terms of fluoride ion is 225ppm) Sodium lauryl sulfate 0.2 Polyoxyethylene (2)-synthetic C12i C,4 alkyl-sodium sulfosuccinate 0.2 Malic acid 0.3 Flavor 0.7 Glycerol 10.0 Xylitol 5.0 Purified water balance 5 Total 100.0 pH 7.5 Example 36 Gel dentifrice A gel dentifrice was prepared with the following formulation according to 10 conventional procedures.

Ingedients Amounts %
Palatinit 10.0 Fine particle zinc oxide 0.1 15 (The average particle diameter is 0.3 li m: the specific surface area is 10m2/g) Sodium fluoride 1.0 (The concentration in terms of fluoride ion is 4,500ppm) Phosphoric acid 3.0 Saccharin sodium 0.5 20 Flavor 0.8 Glycerol 20.0 Hydrochloric acid (2N) 1.0 Purified water balance Total 100.0 25 pH6.9 Fxample 37 Oral gel ~ji ~reients Amounts %
Palatinit 20.0 Carboxymethyl cellulose 0.2 Fine particle zinc oxide 0.1 (The average particle diameter is 0.3 m: the specific surface area is 10m2/g) Glycerol 40.0 Grape seed extract 1.0 a -tocopherol 0.05 Purified water balance Total 100.0 pH 8.5 Industrial Applicabilitv The present invention relates to an oral composition, which has high safety, comprising either palatinit alone or in combination with fluorine compound, as well as an oral composition comprising palatinit in combination with zinc compound, which improves bad feeling when used due to the zinc compound, and, by the inclusion of said ingredient, the present invention can provide an oral composition which can enhance remineralization.

Claims (11)

CLAIMS:
1. An oral composition comprising palatinit and a remineralization enhancing ingredient for remineralization of teeth.
2. The oral composition of claim 1, comprising a fluorine compound as the remineralization enhancing ingredient.
3. The oral composition according to claim 2, wherein said fluorine compound is sodium fluoride.
4. The oral composition according to claim 1, comprising a zinc compound as the remineralization enhancing ingredient.
5. The oral composition according to claim 4, wherein said zinc compound is a water-slightly soluble zinc compound.
6. The oral composition according to claim 5, wherein said water-slightly soluble zinc compound is one or more selected from the group consisting of zinc oxide, zinc citrate and zinc stearate.
7. The oral composition according to claim 5 or 6, wherein said water-slightly soluble zinc compound is a powder having the average particle diameter of not greater than 0.3 µm and the specific surface area of greater than 10m2/g.
8. The oral composition according to any one of claims 4 to 7, which has pH of 6.0-8.5.
9. The oral composition according to claim 8, wherein hydrochloric acid is used as a pH
adjusting agent.
10. The oral composition according to any one of claims 4 to 9, further comprising a fluorine compound.
11. The oral composition of claim 10, wherein said fluorine compound is sodium fluoride.
CA002329622A 1998-04-24 1999-04-19 Remineralizing oral compositions comprising palatinit Expired - Lifetime CA2329622C (en)

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US6471946B1 (en) 2002-10-29
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