JPH0629169B2 - Oral composition - Google Patents

Description

TECHNICAL FIELD The present invention relates to a composition for oral cavity containing a soluble aluminum compound having a good feeling of use, and can be suitably used particularly for prevention or treatment of dentin hypersensitivity. It relates to a composition for oral cavity.

BACKGROUND ART Dentin hypersensitivity is a name of a disease caused by clinical symptoms, and it is caused by dental caries, abrasion, wear, etc., or by gingival retraction, etc., resulting in tooth enamel or cement. The quality disappears and the dentin is exposed.
Extremely unpleasant pain is temporarily caused by various external stimuli such as chemical, mechanical, physicochemical, and electrical (induced pain). For example, foods containing a lot of sugar. It is a temporary pain that is experienced when ingesting fruits with strong acidity, drinking cold water, brushing teeth, etc., but these pains are small for maintaining daily eating habits and oral hygiene. It has a bad effect.

The mechanism of pain expression in dentin is that the above-mentioned induction factors such as electrical stimulation and chemical stimulation (1) directly stimulate nerves in the pulp through the dentinal tubules in dentin and (2) ) In dentinal tubules present in dentin, there is an idea that stimulation of these inducing factors moves dentinal tubule fluid present in the dentinal tubules to stimulate nerves, and at present, the idea of (2) is predominant. There is. That is, the dentinal tubules in human molars have a diameter of about 1.0 μm on the enamel side of 20,000 to 30,000, or a dental pulp side of about 3.0 μm.
30,000 to 40,000 particles of about μm are distributed, but when enamel or cementum disappears, extraneous stimulus is applied to the surface of exposed dentin to cause movement of body fluid in dentinal tubules. The movement of body fluid excites the sensory nerves in the pulp and feels it as pain.

Therefore, in order to alleviate, eliminate, or prevent the pain of hyperesthesia, rather than blunting the pulp nerve, the entrance of this dentinal tubule is blocked and the transmission of stimulation is suppressed by constriction.
Blocking is effective.

Conventionally, as an active ingredient for preventing or treating dentin hypersensitivity, potassium nitrate or sodium citrate is used as an active ingredient that blunts the pulp nerve, and strontium chloride is used as an active ingredient that blocks dentinal tubules. However, conventional active ingredients of this type do not always have sufficient effects, and active ingredients with higher effects are desired.

DISCLOSURE OF THE INVENTION Problems to be Solved by the Invention Therefore, the present inventors have found that dentin hypersensitivity can be suppressed by stenosis or occlusion of dentinal tubules in dentin without relying on an indirect technique utilizing the blunt action of nerves. A study of more effective active ingredients that can be prevented and treated shows that soluble aluminum compounds such as aluminum lactate have an excellent dentinal tubule-blocking effect and are extremely effective in the prevention and treatment of dentin hypersensitivity. However, when a soluble aluminum compound is added to the oral composition, a significant astringent feeling and metallic taste are imparted, which causes a serious drawback that the usability of the oral composition such as toothpaste is significantly impaired. Therefore, the solution of this point was called for.

Means for Solving the Problems In order to achieve the above object, the present invention has a molar ratio of aluminum to a carboxylic acid radical of 0.3 / n to 6 / n (where n represents the number in one molecule of the carboxylic acid radical). In the soluble state, aluminum carboxylate or aluminum chlorhydrol or a propylene glycol complex thereof is contained, and l-menthol is blended, and the pH is 5 to 10
A composition for oral cavity is provided.

That is, according to the studies by the present inventors, aluminum carboxylate single compound or a mixture of an aluminum compound and a carboxylic acid compound in which aluminum and a carboxylic acid radical are in a soluble state at a molar ratio of 0.3 / n to 6 / n ( In the present invention, these are collectively referred to simply as aluminum carboxylate), or in the oral composition containing aluminum chlorohydrol or its propylene glycol complex pair,
Surprisingly, the pH is involved in the feeling of use, and it was found that the feeling of use is remarkably inferior when the pH is about 4, but the astringency is improved when the pH is set to 5 or more, particularly 6 or more.
However, even if the pH is set to 5 or higher, the metallic taste is still strong and astringent taste still remains. Therefore, further research showed that when 1-menthol was added at pH 5 or higher, the astringent feeling and metallic taste disappeared. And, such an effect is not exhibited by fragrances such as carvone, anethole, and methyl salicylate, and is a unique effect surprisingly found only in l-menthol. Therefore, the composition for oral cavity containing the soluble aluminum described above. The use feeling can be remarkably improved by adjusting the pH to 5 or more and 1-menthol, and when the pH is 5 or more as described above, lactic acid is lower than that when the pH is lower than that. It was found that the above-mentioned soluble aluminum such as aluminum has a more effective effect of blocking dentinal tubules, and the present invention provides the same. It has come.

Here, as the aluminum carboxylate, any one can be used as long as it is soluble in the composition (the soluble state in the present invention means that the above components are all solubilized in the oral composition). However, it is not limited only to the case where it is partially precipitated), but as the aluminum carboxylate, aluminum lactate, aluminum gluconate, aluminum monocarboxylate such as aluminum glycolate, aluminum malonate, glutaric acid, etc. A single compound such as aluminum, aluminum malate, aluminum dicarboxylate such as aluminum tartrate, and aluminum tricarboxylate such as aluminum citrate may be mentioned. Among these, a carboxylic acid having a hydroxyl group is particularly preferable, and among them, lactic acid, glycolic acid,
Aluminum hydroxymonocarboxylates such as gluconic acid are preferred. In addition, when aluminum or carboxylic acid is used in an excess mole, Al (NH ₄ ) (SO ₄ ) ₂ , AlC
l ₃ , AlF ₃ , Al (OH) ₃ , [Al (OH) ₂ Cl]
_x , Al (NO ₃ ) ₃ , KAl (SO ₄ ) ₂ , NaAl (S
Aluminum salts such as O ₄ ) ₂ , Al ₂ (SO ₄ ) ₃ and Al (SiF ₆ ) ₃ or mono-, di-4 tricarboxylic acids and alkali metal salts thereof can be blended.

In the above-mentioned aluminum carboxylate, the molar ratio of carboxylic acid radicals to aluminum is 0.3 / n to 6 / n (where n represents the number of carboxylic acid radicals per 1 mol of aluminum. = 1, n = 2 in the case of dicarboxylic acid, n = 3 in the case of tricarboxylic acid), more preferably 0.7 to 5, especially 1 to 4 in the case of monocarboxylic acid, 0.2 to 2.5 in the case of dicarboxylic acid, especially 0.3 ~
2. In the case of tricarboxylic acid, it is 0.1 to 2, especially 0.2 to 1.5 mol.

In the present invention, the soluble aluminum compound is No. 1
The seeds may be used alone or in combination of two or more.
Further, the content of the soluble aluminum compound is not necessarily limited, but solubilized as aluminum is 0.01 to 10% (% by weight, the same applies hereinafter) of the entire composition, particularly
It is preferably 0.1 to 5%.

When the composition of the present invention is used for the purpose of preventing or treating dentin hypersensitivity, in addition to the soluble aluminum compound, a phosphoric acid compound can be further incorporated, whereby prevention of dentin hypersensitivity, The therapeutic effect can be further improved. Here, examples of the phosphoric acid compound include orthophosphoric acid, glycerophosphoric acid, pyrophosphoric acid, tripolyphosphoric acid, hexametaphosphoric acid, phytic acid, and ethane-1-hydroxy.
-1,1-diphosphonic acid and their sodium salts, potassium salts, ammonium salts, calcium salts and the like,
These 1 type (s) or 2 or more types can be used. These phosphate compounds are also to be contained in the oral composition in a dissolved state, and the content thereof is 0.01% of the solubilized composition as a whole.
It is preferably set to 10%, particularly 0.1% to 5%.

Further, by using a soluble aluminum compound, particularly aluminum hydroxycarboxylate in combination with an oxalic acid compound, the same effect as in the case of blending a phosphoric acid compound can be obtained, and therefore, an oxalic acid compound and a soluble aluminum compound, particularly an aluminum hydroxycarboxylate compound. It is effective to use and together. In this case, examples of the oxalic acid compound include oxalic acid and its sodium salt, potassium salt, ammonium salt and the like, and one or more of these may be used, and the content thereof in the oral composition is not limited. The solubilized oxalic acid radical is 0.07-5%, especially 0.1
It is preferably ˜3%.

The oral composition of the present invention uses the above-mentioned soluble aluminum compound in combination with 1-menthol, whereby the pH of the composition is set to 5 or more, and the feeling of use of the soluble aluminum compound-containing oral composition is improved. Can be significantly improved.

Here, 1-menthol may be blended as an essential oil containing the same, for example, peppermint oil. The compounding amount of l-menthol is 0.01 to 10% of the total composition, particularly 0.1 to
It is preferably 6%, and if the amount is less than 0.011%, the effect of improving the feeling in use may not be sufficiently exhibited, and if it is more than 10%, the refreshing feeling may be too strong.

In addition to 1-menthol, other flavors such as carvone, anethole, eugenol, methyl salicylate, spearmint oil, wintergreen oil, sassafras oil, clove oil, and eucalyptus oil can be added to the composition of the present invention. However, especially spice essential oil and spice oleoresin in addition to l-menthol from 0.0001 to
It is preferable to add 1%, particularly 0.001 to 3%, whereby a richness of flavor is imparted, and a flavor with high palatability can be obtained.

The oral composition according to the present invention is used as a toothpaste, a toothpaste such as a dentifrice, a liquid or gel coating agent, a mouthwash, a dental floss, an oral band, etc. As other components of the composition for oral cavity, appropriate components are used depending on the type, purpose of use and the like.

For example, in the case of toothpaste, dibasic calcium phosphate-2
Hydrates and anhydrides, monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate,
Titanium oxide, alumina, aluminum hydroxide, precipitated silica, other silica-based abrasives, aluminum silicate,
One or more of insoluble tonalium metaphosphate, insoluble potassium metaphosphate, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, bentonite, zirconium silicate, synthetic resin and the like may be blended (the blending amount is usually 3 to 99%). In case of toothpaste, it is 5-50%, but RD
It is preferable to select the abrasive and its content so that the A value is about 10 to 100, especially about 30 to 60).

In this case, among these abrasives, aluminum hydroxide is preferable from the viewpoint of better improving the stability of the composition and allowing the soluble aluminum compound to be more stably compounded in the composition, and especially water as aluminum hydroxide. A modified aluminum hydroxide obtained by treating aluminum oxide with an acid or a salt thereof, particularly phosphoric acid or a salt thereof is preferably used.

Further, in the case of a paste-form oral composition such as toothpaste, as a binder, carrageenan, sodium carboxymethyl cellulose, methyl cellulose, hydroxyethyl cellulose, a cellulose derivative such as sodium carboxymethyl hydroxyethyl cellulose, an alkali metal alginate such as sodium alginate. , Propylene glycol alginate, xanthan gum, gums such as tragacanth gum, karaya gum and gum arabic, polyvinyl alcohol, sodium polyacrylate, carboxyvinyl polymer, synthetic binders such as polyvinylpyrrolidone, gelling silica, gelling aluminum silica , One kind or two or more kinds of inorganic binders such as bee gum and laponite may be blended (the blending amount is usually 0.5 to 5% in the case of dentifrice).

Among these, it is preferable to use hydroxyalkyl cellulose such as hydroxyethyl cellulose in combination with carrageenan from the viewpoint of improving the stability of the soluble aluminum compound-containing composition and stably blending the soluble aluminum compound.

Furthermore, in the production of toothpaste and other liquid or paste oral compositions, sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-
One kind or two or more kinds of butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltite, lactit and the like can be blended (the blending amount is usually 10 to 70% in the case of toothpaste).

Further, a water-soluble salt of a higher alkyl sulfate ester having an alkyl group having 8 to 18 carbon atoms such as sodium lauryl sulfate and sodium myristyl sulfate, a water-soluble higher fatty acid monoglyceride monosulfate such as hydrogenated coconut oil fatty acid monoglyceride monosulfate, etc. Salts, alkylaryl sulfonates such as sodium dodecylbenzene sulfonate, higher alkyl sulfonates, higher fatty acid esters of 1,2-dihydroxypropane sulfonate, N-lauroyl, N-
Anionic activators such as substantially saturated higher fatty acid acylamides of lower aliphatic aminocarboxylic acid compounds such as sodium, potassium or ethanolamine salts of myristoyl or N-palmitoyl sarcosine, alkyloyl ethanolamides such as lauroyl diethanolamide, and sham Carbon number of fatty acid groups such as sugar mono and dilaurate is 12 to 1
8 sucrose fatty acid ester, lactose fatty acid ester, lactitol fatty acid ester, maltitol fatty acid ester, stearic acid monoglyceride, polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monostearate, polyoxyethylene (10, 20, 40) , 60, 80, 100 mol) Hydrogenated castor oil, polymer of ethylene oxide and propylene oxide, and condensation of polyethylene oxide such as polyoxyethylene polyoxypropylene monolauryl ester with fatty acid, fatty alcohol, polyhydric alcohol and polypropylene oxide One or more kinds of surfactants such as nonionic surfactants such as substances, amphoteric surfactants such as betaine and amino acids (blending amount usually 0 to 7%, preferably 0.2 to 5%) It may be incorporated.

Of these, the fatty acid group has 10 to 16 carbon atoms, particularly 12 to 14 carbon atoms, and the alkanol group has 2 carbon atoms from the viewpoint of improving the astringency of the soluble aluminum compound.
Alternatively, a fatty acid alkanolamide of 3 is preferably used. The fatty acid may be saturated or unsaturated, may have a straight chain or a branched chain, and may be a mixed fatty acid. Specifically, capric acid monoethanolamide, lauric acid diethanolamide, myristic acid diethanolamide, palmitic acid diethanolamide, coconut oil fatty acid diethanolamide, tallow fatty acid diethanolamide, lauric acid monoisopropanolamide and the like, among them, lauric acid Acid diethanolamide and myristic acid diethanolamide are preferably used.

The oral composition of the present invention further comprises saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartine, thaumatin, asparatyl phenylalanine methyl ester, p-methoxycinnamic aldehyde, lactose, fructose, and sweetness of sodium cyclamate. Agent (0 to 1%, preferably 0.01
0.5%), p-hydroxymethyl benzoic acid, p-hydroxyethyl benzoic acid, p-hydroxypropyl benzoic acid, p-hydroxybutyl benzoic acid, sodium benzoate, lower fatty acid monoglyceride and other preservatives, gelatin , Peptone, arginine hydrochloride, albumin, casein, whitening agent, silicone, pigment, and other components can be blended, and for example, in the case of toothpaste, it is prepared by kneading the desired components described above with an appropriate amount of water. You can

Also, when other oral compositions are produced, they can be produced according to a conventional method using appropriate components that are usually used.

Still further, in the present invention, epsilon aminocaproic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme, enzymes such as liter enzyme, sodium monofluorophosphate, alkali such as potassium monofluorophosphate, etc. Metal monofluorophosphate, sodium fluoride,
Ammonium fluoride, fluorides such as stannous fluoride, chlorhexidine salts, dihydrocholesterol, glycyrrhizin salts, glycyrrhetinic acid, chlorophyll, caropeptide, vitamins, anticalculus agents, antibacterial agents, antiplaque agents, potassium nitrate, etc. One or two or more kinds of active ingredients such as hyperesthesia blunting agents may be blended.

The composition for oral cavity of the present invention can be prepared by appropriately selecting and using the above-mentioned components. In this case, the pH of the composition needs to be 5 to 10, and more preferably 6 to 8, and the pH is required. When it is lower than 5, the feeling of use is poor and the astringency is particularly strong, so that the object of the present invention cannot be achieved. Further, if the pH is higher than 10, there may be a problem in safety for oral mucosa.

In addition, by adjusting the pH of the composition to 5 to 10 as described above, the feeling of use of the soluble aluminum compound-containing oral composition can be improved as described above.
The dentinal tubule-blocking effect of the soluble aluminum compound is effectively exhibited in the pH range.

When adjusting the pH of the composition of the present invention to 5 to 10, a pH adjusting agent can be added as necessary, and examples of the pH adjusting agent include sodium hydroxide, potassium hydroxide, sodium hydrogen carbonate and sodium carbonate. Alkali hydroxide, alkali hydrogen carbonate, alkali carbonate, etc. can be used, but when carbonate, urea, etc. are used, there are problems such as gas generation, turbidity, and low pH adjusting ability. It is preferable to use sodium hydroxide or potassium hydroxide because they may occur. When lowering the pH of the composition, an appropriate inorganic acid or organic acid can be used.

Effect of the Invention The oral composition of the present invention uses 1-menthol in combination with a soluble aluminum compound and has a pH of 5 to 10, so that the astringent feeling and metallic taste are eliminated, and the feeling of use is very good. It is excellent.

Next, the effects of the present invention will be specifically shown by showing experimental examples.

[Experimental example]

Toothpastes A to M having the formulations shown in Tables 1 and 2 were prepared, and the feeling of use (astringency, metallic taste) was organoleptically evaluated by 10 professional panelists according to the following criteria. The results are also shown in Table 1.

Evaluation criteria ○: Astringent feeling or no metallic taste △: 〃 Somewhat bad ×: 〃 Yes From the results shown in Table 1, the composition containing 1-menthol and having a pH of 5 or more showed no astringent feeling and no metallic taste, and showed a good feeling of use. No usability improving effect was observed, and therefore, it was found that the effect of improving the usability of the oral composition containing the soluble aluminum compound is specific to 1-menthol alone. However, even when 1-menthol is used, when the pH of the composition is lower than 5, there is no effect of improving the feeling of use due to 1-menthol. Therefore, in order to improve the feeling of use of the soluble aluminum compound-containing composition, -With the addition of menthol and a composition pH of 5
It was found that the above needs to be done.

Examples will be shown below.

[Example 1] Toothpaste [Example 2] Toothpaste [Example 3] Toothpaste Example 4 Toothpaste Example 5 Toothpaste Example 6 Toothpaste [Example 7] Powder toothpaste [Example 8] Oral pasta Example 9 Mouthwash [Example 10] Oral hand The above components are mixed, adjusted to pH 7, and then dried by a known method.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (56) Reference JP-A-58-216115 (JP, A) JP-A-61-36212 (JP, A) US Patent 3514513 (US, A) US Patent 3651207 (US, A) "Collection of Well-Known and Conventional Techniques (Cosmetics and Similar), (August 21, 1984) JPO P. 121

Claims (2)

[Claims] 1. A molar ratio of aluminum to carboxylic acid radicals of 0.
Aluminum carboxylate in the soluble state in 3 / n to 6 / n (where n represents the number in one molecule of the carboxylic acid radical), or aluminum chlorohydrol or a propylene glycol complex thereof, and 1-menthol The composition for oral cavity is characterized in that the pH is 5-10. 2. The content of aluminum in a soluble state is 0.01 to 10% by weight of the whole composition, and the blending amount of 1-menthol is 0.01 to 10% by weight of the whole composition. The oral composition according to the item.