JP2002003352A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for the oral cavity capable of effectively promoting recalcification of an initial dental carious tooth, consequently effective for restoring or treating the initial dental carious tooth. SOLUTION: This composition for the oral cavity is characterized in that the composition comprises a fluorine compound and an inorganic compound for releasing titanium ion and has <=0.15 formulation molar ratio (Ti/F) of titanium to fluorine.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral composition which is effective for repairing or treating early caries.

[0002]

2. Description of the Related Art
Techniques to promote remineralization of initial caries include removal of plaque attached to the enamel surface of the initial caries (brushing), suppression of acid production in plaque by antibacterial agents,
Alternatively, chewing gum promotes salivary secretion, and the oral environment tends to remineralize rather than demineralize, and a method of re-depositing mineral ions contained in saliva and plaque in demineralized foci (natural healing) is known. I have. However, natural healing effects such as plaque removal (brushing), suppression of acid production ability in plaque by antibacterial agents, and promotion of salivary secretion by chewing gum can be expected to some extent, but the effects are not sufficient.

[0003] On the other hand, fluoride and calcium compounds are known to be applied to actively promote mineral deposition. Above all, applications of fluorides and calcium compounds are expected to have relatively high effects. Specifically, in addition to the simple application of soluble fluorides such as sodium fluoride, sodium monofluorophosphate or tin fluoride, the chemical reaction between sodium fluoride and sodium monofluorophosphate on enamel is utilized. For this reason, Colgate has proposed a technology in which both are used at a fixed ratio. Recently, journals of dental professionals have suggested that xylitol promotes remineralization in cooperation with calcium or fluorine in saliva. However, although the application of such fluorides and calcium compounds is expected to have relatively high effects, the effects have not yet been determined.

Further, Enamelon has proposed a separation technique in which a dentifrice is separated into two layers, one of which contains a soluble fluoride and a soluble phosphate compound, and the other contains a soluble calcium compound. I have. This technique aims at supplying both fluorine and calcium phosphate to the tooth material, but separates them so that the formation of insoluble calcium fluoride in the dentifrice does not occur.
However, this two-layer preparation (dentifrice) has a drawback in that it is costly in terms of commercialization, such as the technique of separation and filling.

Further, Tung et al. Of the American Dental Federation propose the application of amorphous calcium phosphate or amorphous calcium phosphate containing fluorine. However, with respect to the application of this amorphous fluorine-containing or non-fluorine-containing calcium phosphate, its production varies, and it is difficult to obtain a certain quality.

On the other hand, Arends et al. In the Netherlands have proposed a technique using sodium monofluorophosphate in combination with a soluble magnesium salt. The role of the magnesium salt in this case is a technique of suppressing excessive calcification on the surface layer of the initial caries with the magnesium salt and promoting remineralization from inside the initial caries. This technology using sodium monofluorophosphate in combination with soluble magnesium salt is a breakthrough in that excessive calcification on the surface layer of initial caries is suppressed with magnesium salts and remineralization is promoted from inside the initial caries. It is a target. However, further improvement is required in that sodium fluoride cannot be used (the formation of poorly soluble magnesium fluoride) and the taste of bitterness due to the magnesium compound is low.

The present invention has been made in view of the above circumstances, and it is an object of the present invention to provide an oral composition which has an excellent effect in repairing or treating initial caries.

[0008]

Means for Solving the Problems and Embodiments of the Invention The present inventors have conducted intensive studies to achieve the above object, and as a result, have found that an inorganic compound that releases titanium ions (an inorganic titanium compound) and a fluorine compound. By using them together, it has been found that a higher remineralization effect can be obtained from the inner layer while suppressing excessive calcification of the surface layer by using only a small amount of the inorganic titanium compound as compared with the case of using a soluble magnesium salt. That is, in order to obtain a high remineralization effect, it is necessary to use an inorganic compound that releases titanium ions in a specific small amount relative to the fluorine compound, and specifically,
The molar ratio of titanium to fluorine (Ti / F) is set to 0.1.
It has been found that setting the content to 15 or less promotes the remineralization effect of fluorine, leading to the present invention.

Several techniques are known for blending a titanium compound. For example, caries preventive effect of titanium tetrafluoride (Adv Dent Res, 11 (4):
448-452, 1997), a caries preventive composition containing a heat reaction product of lauryl gallate and titanium tetrafluoride (Japanese Patent Application Laid-Open No. 58-180418), and sodium hexafluorotitanate as an essential component. Composition for preventing and inhibiting the progress of dental caries (Japanese Patent Application Laid-Open No. 55-35015), a composition for improving the appearance of teeth and the resistance of tooth surfaces to caries by using a hydrolyzable titanium fluoride compound and an organic acid in combination (JP-A-49-239
No. 94), a dentifrice composition containing titanium oxide for the purpose of modifying a dentifrice (mainly hiding the color of the composition and enhancing white) (JP-A-56-167613), titanium oxide Oral composition utilizing photocatalytic activity of
No. 26115) is known. However, there is no known document referring to the ratio of titanium and fluorine contained in the inorganic compound that releases titanium ions,
It is for the first time in this finding that a high remineralization effect has been found by using an inorganic compound that releases titanium ions at a ratio of the Ti / F value of 0.15 or less and a fluorine compound.

Hereinafter, the present invention will be described in more detail.
The oral composition of the present invention that is effective for repairing or treating initial caries contains a fluorine compound and an inorganic compound that releases titanium ions, and has a titanium to fluorine molar ratio (Ti / F) of 0. .15 or less.

Here, the fluorine compound may be any fluorine compound which can be conventionally compounded in an oral composition, such as sodium fluoride, potassium fluoride, stannous fluoride, strontium fluoride, and the like. Examples thereof include sodium monofluorophosphate and potassium monofluorophosphate. The compounding amount is preferably 0.01 to 0.5% (mass percentage, the same applies hereinafter) of the whole composition as fluorine, and particularly preferably 0.02 to 0.2%.

On the other hand, the inorganic titanium compound is not particularly limited as long as it is a compound which releases a titanium ion (Ti ⁴⁺ ) even though it is in a trace amount. Examples of such titanium compounds include titanium chloride (TiCl ₄ ), titanium fluoride (TiF ₄ ), titanium bromide, titanium sulfate,
Titanium hexafluoride (Na ₂ TiF ₆ ), titanic acid and the like can be mentioned. A similar effect can be obtained by using a polishing agent for dentifrices that releases a trace amount of titanium ions by surface treatment with these inorganic titanium compounds. When the titanium ion concentration is too high, the remineralization promotion tends to be suppressed, and the amount of the titanium compound effective for remineralization from the inner layer is as described above. , In such an amount that the molar ratio of titanium to fluorine (Ti / F) becomes 0.15 or less, more preferably 0.00 / 0.00.
5 to 0.15, more preferably 0.005 to 0.13,
Particularly preferably, the amount is from 0.010 to 0.10.
The titanium compound is contained in the composition in an amount of from 0.005 to 0.5%.
It is preferable that the amount is in the range of 2%.

It is preferable that the oral composition of the present invention further contain xylitol. By adding xylitol, remineralization from the inner layer can be more effectively promoted. The amount of xylitol is preferably 3 to 40%, particularly preferably 10 to 30% of the whole composition.

The composition for oral cavity of the present invention can be prepared and applied as a dentifrice, mouthwash, liniment (solution, gel), tablet, chewing gum, patch, dental floss, etc. Any form can be used as long as it can realize the promotion of activation.

The oral composition may be blended with known components according to the type thereof in a usual amount. Examples of the abrasive include calcium hydrogen phosphate dihydrate, tertiary calcium phosphate, calcium carbonate, and the like. Calcium pyrophosphate, aluminum hydroxide, silicic anhydride, aluminum silicate, insoluble sodium metaphosphate, tribasic magnesium phosphate,
One or more of magnesium carbonate, calcium sulfate, bentonite, zirconium silicate, polymethyl methacrylate, and other synthetic resins may be blended within a range that does not impair the effects of the present invention.

Examples of the binder include cellulose derivatives such as carrageenan, sodium carboxymethylcellulose, methylcellulose, and hydroxyethylcellulose; alginic acid derivatives such as sodium alginate and propylene glycol alginate; gums such as xanthan gum, gellan gum, tragacanth gum, and karaya gum; One or more kinds of synthetic binders such as alcohol, sodium polyacrylate, and carboxyvinyl polymer, and inorganic binders such as silica gel, veegum, and laponite may be blended.

As humectants, glycerin, sorbitol, propylene glycol, polyethylene glycol,
One or more polyhydric alcohols such as maltitol and lactitol can be blended.

Examples of the surfactant include an anionic surfactant such as sodium lauryl sulfate, a nonionic surfactant such as decaglyceryl laurate and diethanolamide myristate, and an amphoteric surfactant such as betaine. .

As the fragrance component, menthol, anethole, carvone, eugenol, n-decyl alcohol,
Flavors such as citronellol, α-terpineol, cineol, linalool, ethyl linalool, crocodile, thymol, peppermint oil, spearmint oil, wintergreen oil, clove oil, eucalyptus oil and the like can be used alone or in combination. Furthermore, sweeteners such as saccharin sodium, perillartin, thaumatin and the like can be added.

The present invention also includes a cationic fungicide such as chlorhexidine, benzethonium chloride, benzalkonium chloride, cetylpyridinium chloride, decalinium chloride, a phenolic compound such as triclosan, hinokitiol, biosol, dextranase, and mutanase. , Lysozyme, amylase, protease, lytic enzyme, SO
Enzymes such as D, tranexamic acid, epsilon aminocaproic acid, allantoin, dihydrocholestanol, glycyrrhizic acids, glycyrrhetinic acid, glycerophosphate, chlorophyll, sodium chloride, xylitol,
One or more known active ingredients such as zinc chloride, water-soluble inorganic phosphate compounds, vitamins such as vitamin A, vitamin B group, vitamin E, and derivatives thereof, and the like can be blended.

The oral composition of the present invention can be used in a known manner depending on the type thereof, using a normal dose.

[0022]

EFFECTS OF THE INVENTION The oral composition of the present invention can effectively promote remineralization of initial caries and is therefore effective for repairing or treating early caries.

[0023]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to experimental examples and examples, but the present invention is not limited to the following examples. [Experimental example] Since the molar ratio between titanium and fluorine can be changed arbitrarily, titanium chloride (titanium tetrachloride, TiCl ₄ ) was used as an inorganic compound releasing titanium ions, and sodium fluoride was used as a fluorine compound. An experiment was performed.

Lactate buffer (lactic acid: 100 mM, CaCl
₂ : 10 mM, KH ₂ PO ₄ : 10 mM, NaCl: 10
0mM, pH 4.6), subsurface demineralized foci (initial caries) were made on human enamel sections (about 120 microns). Next, the section where the initial caries was formed was treated with a mixed solution of a titanium compound and sodium fluoride having different molar ratios. In this case, after the treatment for 3 minutes, washing with distilled water was performed three times to remove unreacted compounds. Thereafter, artificial saliva (CaCl ₂ : 1.0 mM, KH ₂ PO ₄ : 2.5 mM,
NaCl: 100 mM, pH 6.8) to remineralize the initial caries. This operation was performed twice a day, and this was repeated for 10 days. Thereafter, a microradiogram was prepared for this enamel section, and the remineralized state of the initial caries was observed.

Table 1 shows the effect of the difference in the molar ratio between titanium and fluorine on remineralization. If TiCl ₄ is less than 0.005%, a sufficient effect of addition is not recognized, and if it exceeds 0.2%, pH due to hydrolysis of TiCl ₄ is not increased.
And the problem (acidity, bitterness, etc.) may occur in practical use.

[0026]

[Table 1] (Note) ○: Remineralization in the inner layer is better than fluorine alone △: Remineralization in the inner layer is slightly better than fluorine alone ×: Overall remineralization is better than fluorine alone Calcification suppressed

From the results shown in Table 1, the lower the Ti concentration, the higher the effectiveness with respect to the calcification control action. That is, the hypercalcification in the surface layer of the initial caries is suppressed, so that the lesion of the initial caries is more completely remineralized and repaired from the inside.

Examples will be described below. [Example 1] Dentifrice Silica 15.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Sorbitol 15.0 Sodium lauryl sulfate 1.5 Xylitol 15.0 Preservative Trace amount of fragrance 1.0 Saccharin Trace amount of sodium monofluorophosphate 0.8 Titanium chloride 0.1 Purified water Balance meter 100.0% (Ti / F 0.096)

Example 2 Dentifrice Silica 20.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Xylitol 20.0 Sodium lauryl sulfate 1.0 Titanium sulfate 0.10 Preservative trace amount Flavor 1.0 Saccharin trace amount Sodium chloride 0.21 Purified water Balance meter 100.0% (Ti / F 0.125)

Example 3 Dentifrice Silica 20.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Xylitol 20.0 Sodium lauryl sulfate 1.5 Lauroyl sarcosinate 0.3 Preservative Trace amount of fragrance 1.0 Saccharin Trace amount of sodium fluoride 0.21 Sodium titanium hexafluoride 0.1 Dextranase 0.2 (20,000 U / g enzyme) Purified water Balance meter 100.0% (Ti / F 0.061)

Example 4 Dentifrice Silica 10.0% Carboxymethyl Cellulose 1.5 Polyethylene Glycol 3.0 Xylitol 20.0 Sodium Lauryl Sulfate 1.0 Preservatives Minor Flavor 1.0 Saccharin Minor Minor Sodium Monofluorophosphate 0 .8 Triclosan 0.3 Titanium chloride 0.1 Purified water Balance meter 100.0% (Ti / F 0.096)

Example 5 Dentifrice Silica 20.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Xylitol 20.0 Sodium lauryl sulfate 1.5 Lauroyl sarcosinate 0.3 Preservative Trace amount of fragrance 1.0 Saccharin Trace sodium monofluorophosphate 0.8 Titanium hexafluoride 0.1 Purified water Balance meter 100.0% (Ti / F 0.057)

Example 6 Dentifrice Silica 10.0% Carboxymethyl Cellulose 1.5 Polyethylene Glycol 3.0 Xylitol 20.0 Sodium Lauryl Sulfate 1.0 Preservatives Minor Flavor 1.0 Saccharin Minority Sodium Monofluorophosphate 0 .8 Cetylpyridinium chloride 0.3 Titanium sulfate 0.10 Purified water Balance meter 100.0% (Ti / F 0.114)

Example 7 Dentifrice Silica 20.0% Carboxymethyl Cellulose 1.5 Polyethylene Glycol 3.0 Xylitol 20.0 Sodium Lauryl Sulfate 1.5 Lauroyl Sarcosinate 0.3 Preservatives Trace Perfume 1.0 Saccharin Trace amount of sodium fluoride 0.21 Titanium chloride 0.05 Purified water Balance meter 100.0% (Ti / F 0.053)

Example 8 Dentifrice Silica 10.0% Carboxymethyl Cellulose 1.5 Polyethylene Glycol 3.0 Xylitol 20.0 Sodium Lauryl Sulfate 1.0 Preservative Minor Flavor 1.0 Saccharin Minor Sodium Fluoride 0.21 Triclosan 0.3 Titanium sulfate 0.1 Purified water Balance meter 100.0% (Ti / F 0.125)

Example 9 Mouthwash Polyethylene glycol 3.0% Sorbitol 10.0 Sodium lauryl sulfate 0.3 Sodium fluoride 0.1 Preservative trace amount of fragrance 1.0 Saccharin Trace amount of ethanol 5.0 Titanium sulfate 0. 05 Purified water balance meter 100.0% (Ti / F 0.13)

Example 10 Mouthwash Polyethylene glycol 3.0% Xylitol 20.0 Sodium lauryl sulfate 0.2 Sodium fluoride 0.05 Preservative Trace amount of fragrance 1.0 Saccharin Trace amount of ethanol 5.0 Titanium chloride 0.0 02 Purified water balance meter 100.0% (Ti / F 0.089)

Example 11 Mouthwash Polyethylene Glycol 3.0% Sorbitol 10.0 Sodium Lauryl Sulfate 0.3 Sodium Fluoride 0.03 Preservative Trace Aroma 1.0 Saccharin Trace Ethanol 5.0 Titanium Hexafluoride Sodium 0.02 Purified water Balance meter 100.0% (Ti / F 0.074
6)

Example 12 Mouthwash Polyethylene glycol 3.0% xylitol 20.0 Sodium lauryl sulfate 0.2 Sodium monofluorophosphate 0.2 Preservative trace amount of fragrance 1.0 Saccharin Trace amount of ethanol 5.0 Titanium chloride 0.02 Dextranase 0.2 (20,000 U / g enzyme) Purified water Balance meter 100.0% (Ti / F 0.104)

Example 13 Mouthwash Polyethylene Glycol 3.0% Sorbitol 10.0 Sodium Lauryl Sulfate 0.3 Sodium Monofluorophosphate 0.2 Preservative Trace Aroma 1.0 Saccharin Trace Ethanol 5.0 Titanium Sulfate 0.03 purified water balance meter 100.0% (Ti / F 0.13)

Example 14 Mouthwash Polyethylene glycol 3.0% xylitol 20.0 Sodium lauryl sulfate 0.2 Sodium monofluorophosphate 0.2 Preservative trace amount of fragrance 1.0 Saccharin Trace amount of ethanol 5.0 Sodium titanate 0.04 Purified water Balance meter 100.0% (Ti / F 0.076)

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 1/02 A61P 1/02 (72) Inventor Haruhiko Fujikawa 1-3-7, Honjo, Sumida-ku, Tokyo F term in Lion Corporation (reference) 4C076 AA09 AA12 BB22 CC16 DD05 DD27 DD38 DD47 DD52 DD55 DD61 EE23 EE33 FF34 FF68 4C083 AA112 AB172 AB241 AB242 AB282 AB332 AB352 AB471 AB472 AC102 AC131 AC132 AC662 AC692 AC782 AC812 AC272 DD23 AD042 EE32 EE36 4C086 AA01 AA02 HA06 HA17 HA24 MA02 MA05 NA05 NA10 NA10 ZA67 ZC75

Claims (2)

[Claims] 1. An oral composition comprising a fluorine compound and an inorganic compound that releases titanium ions, wherein the molar ratio of titanium to fluorine (Ti / F) is 0.15 or less. object. 2. The oral composition according to claim 1, comprising xylitol.