JPH089531B2 - Oral composition - Google Patents

Description

TECHNICAL FIELD The present invention relates to an oral composition, and more specifically, one or more selected from fluorides, selected from pyridinols and nicotinic acids. The present invention relates to a composition for oral cavity in which the caries-preventing effect is further enhanced by blending one or two or more of them.

[Prior Art] The effect of fluoride in preventing dental caries is widely recognized. Dental caries is a phenomenon in which dentin is decalcified by organic acids such as lactic acid produced by decomposing sugars such as sucrose by indigenous bacteria in the oral cavity (mainly strepto-coccus mutans). is there. The main constituent of enamel is hydroxyapatite, but fluoride ions are easily incorporated into the crystal lattice of hydroxyapatite and improve its crystallinity. As a result, the tooth substance is strengthened, and the enamel is not easily decalcified even by the organic acid produced by the bacteria resident in the oral cavity, thus preventing dental caries. Fluoride ions are also more easily incorporated into early caries lesions that have undergone some decalcification than healthy enamel, and are also said to promote remineralization and suppress the progression of caries. .

Currently, fluorides such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride are used for caries prevention.
It is used in methods such as fluoride addition to water supply, fluoride tooth surface coating method, fluoride mouth rinsing method, and fluoride addition dentifrice.

[Problems to be Solved by the Invention] However, at the present time when caries is still widespread, the caries preventive effect is not always satisfactory with conventional fluoride alone, and a further caries preventive effect is obtained. The current situation is long-awaited.

In view of the above circumstances, the present inventors have conducted intensive studies in pursuit of a further caries preventive effect, and as a result, found that some amines have an effect of enhancing the effect of conventional fluorides. That is, when conventional pyridyl is added with pyridylcarbinol, nicotinic acid amide, allantoin, chlorhexidine gluconate, polyvinylpyrrolidone, etc., fluoride ions are efficiently taken in by hydroxyapatite, and the fluoride tooth substance Although the strengthening action is enhanced, it was found that the effects of pyridinol compounds and nicotinic acid compounds were remarkable, and the present invention was completed.

[Means for Solving Problems] That is, the present invention contains one or more selected from fluorides and one or more selected from pyridinol's and nicotinic acids. A featured oral composition is provided.

 Hereinafter, the configuration of the present invention will be described in detail.

The fluoride used in the present invention is a compound containing fluorine (F), which is an element that is very universally present in the living world,
Sodium fluoride, potassium fluoride, lithium fluoride,
Cesium fluoride, zirconium fluoride, ammonium fluoride, stannous fluoride, sodium monofluorophosphate,
Inorganic fluorides such as potassium monofluorophosphate, sodium titanium fluoride, potassium titanium fluoride, hexylamine hydrofluoride, laurylamine hydrofluoride, cetylamine hydrofluoride, glycine hydrofluoride, lysine hydrofluoride, alanine One or more organic fluorides such as hydrofluoride and fluorosilane are used, but sodium fluoride, potassium fluoride, ammonium fluoride, stannous fluoride and monofluoro are used in the oral cavity. Sodium phosphate and potassium monofluorophosphate are preferred.

The blending amount of these fluorides is 50 to 10000 ppm (μg / g, the same applies below) as a total fluorine concentration in the oral cavity composition, and preferably 200 to 10000 ppm. If it is less than 50 ppm, no enhancing effect can be expected when one or more selected from the group consisting of pyridine derivatives is added, and if it exceeds 10,000 ppm, the effect does not increase so much and it is uneconomical. When manufacturing a dentifrice, it is desirable that the total fluorine concentration be 1000 ppm or less.

Specific examples of the pyridinols used in the present invention include 3-pyridylcarbinol and 2-pyridylcarbinol. As nicotinic acids, in addition to nicotinic acid, nicotinic acid esters (for example,
Nicotinic acid methyl ester, nicotinic acid ethyl ester, etc.), nicotinic acid amide, etc. are also included. Among these,
Particularly, 3-pyridylcarbinol and 2-pyridylcarbinol are preferable.

In the composition for oral cavity of the present invention, one or two or more kinds are appropriately selected and used from the group consisting of the above-mentioned pyridine derivatives.

The blending amount is 1/5 to 10 times, preferably 1/20 to 5 times, and more preferably 1/10 to 3 times the molar amount of the fluoride. If it is less than 1/50 times, the effect of enhancing the action of the combined fluoride cannot be expected, and if it exceeds 10 times, the effect does not increase so much and it is uneconomical.

The oral composition of the present invention, in addition to the above essential components, depending on the type of oral composition, dicalcium phosphate.
Dihydrate and anhydride, monocalcium phosphate, tricalcium phosphate, calcium carbonate, calcium pyrophosphate, titanium oxide, aluminum hydroxide, aluminum oxide, amorphous silica, crystalline silica, anhydrous alkali metal silicate complex salts, etc. Silica based abrasive, aluminum silicate,
Insoluble sodium metaphosphate, insoluble potassium metaphosphate, insoluble calcium polyphosphate, tribasic magnesium phosphate, magnesium carbonate, magnesium sulfate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, hydroxyapatite, abrasives such as synthetic resin, Glycerin, sorbitol, propylene glycol, polyethylene glycol, ethylene glycol, 1,3-butylene glycol, xylitol, maltitol, lubricants such as lactitol, carboxymethyl cellulose, methyl cellulose, hydroxyethyl cellulose, sodium carboxymethyl hydroxyethyl cellulose, sodium alginate, carrageenan, Sodium polyacrylate, gum arabic, xanthan gum, tragacanth gum, Thickeners such as raya gum, polyvinyl alcohol, carboxyvinyl polymer, polyvinylpyrrolidone, etc., water-soluble salts of alkyl sulfates having 8 to 18 carbon atoms such as sodium lauryl sulfate, sodium myristyl sulfate, sodium lauryl monoglyceride sulfate, coconut oil fatty acid monoglyceride Of water-soluble higher fatty acid monoglyceride sulfates having a fatty acid group of 10 to 18 carbon atoms such as sodium sulfate and higher fatty acid monoglyceride sodium sulfate, α-olefin sulfate, paraffin sulfate, N-methyl-N-palmityl tauride Anionic activators such as sodium salt, sodium N-lauroyl sarcosinate and sodium N-lauroyl-β-alanine, fatty acid alkanolamides such as lauric acid diethanolamide, sucrose mono and dilaure Sucrose fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene fatty acid ester, polyoxyethylene hydrogenated castor oil derivative, lactose fatty acid ester, lactitol fatty acid ester, maltitol fatty acid ester, polyoxyethylene polyoxypropylene block copolymer Nonionic active agents such as, cationic active agents, surfactants such as amphoteric active agents, higher alcohols, oils such as waxes, lower alcohols, sodium saccharin, stepioside, neohesperidin dihydrochalcone, glycyrrhizin, perillartin, p-methoxy. Sweeteners such as cinnamic aldehyde, essential oils such as peppermint, spearmint and fennel oil, and flavors such as 1-menthol, carvone, eugenol and anethole. Fragrances such as wood, dyes, antiseptic / antifungal agents, antioxidants, water, etc., dextranase, protease, ritiqenzyme, mutanase, mutasteine, sorbic acid, alexidine, β-glycyrrhetinic acid, hinokitiol, dihydrocholesterin, epidihydrocholeste Phosphorus, alkylglycine, alkyldiaminoethylglycine salts, allantoin, ε-aminocaproic acid, tranexamic acid, azulene, other vitamins, water-soluble primary or secondary phosphates, quaternary ammonium compounds such as cetylpyridinium chloride, Ingredients normally used in oral compositions such as active ingredients such as sodium chloride and crude drug extracts can be added.

Further, the dosage form of the oral composition of the present invention is also optional, toothpaste, powdered toothpaste, moisturized toothpaste, toothpaste such as water toothpaste, oral pasta, mouthwash such as mouthwash, mouthwash, topical It can be used as a coating agent, a mouth-cooling agent, chewing gum, dental floss, gargle and other gargles.

The pH of the oral composition of the present invention is not necessarily limited, but it is preferably pH 3 to 10, more preferably pH 4 to 9, and particularly preferably pH 5 to 7.

[Effects of the Invention] Example 1 A composition was prepared by adding a predetermined amount of sodium fluoride and 3-pyridylcarbinol and adjusting the pH to 4.5 with dilute hydrochloric acid or dilute sodium hydroxide. Immersing the synthetic hydroxyapatite powder in these compositions at 37 ° C. for 5 minutes,
Subsequently, it was immersed in a calcification solution at 37 ° C. for 60 minutes, filtered with a filter and dried. For the synthetic hydroxyapatite powder treated in this way, the fluorine concentration in the powder was measured by the microdiffusion method, and it was immersed in an acetate buffer at 37 ° C for 60 minutes to measure the amount of eluted calcium. The ash inhibition rate was calculated and the acid resistance was evaluated.

The results are shown in Table 1.

From the above results, pyridylcarbinols in sodium fluoride, when combined with one or more selected from nicotinic acids, the fluorine uptake amount of synthetic hydroxyapatite and acid resistance are significantly increased from sodium fluoride alone, One or two or more selected from pyridicarbinols and nicotinic acids were found to enhance the effect of sodium fluoride.

Experimental Example 2 A composition containing a predetermined amount of fluoride and 3-pyridylcarbinol was prepared. In these compositions, a surface of 200
The bovine tooth having a enamel surface exposed by polishing to remove μm was immersed at 37 ° C. for 5 minutes, then immersed in a calcification solution at 37 ° C. for 60 minutes, washed with tap water and dried. For the treated bovine tooth, the concentration of fluorine in enamel was measured by an acid biopsy method, and an acidic gelatin gel prepared based on the method of Silverstone {Leon M Silverstone (Leon M .Silverstone) ； Caries ・
Research (Caries Res.) 1: 261-274,1967} during 4 weeks,
After immersion for 8 weeks and 15 weeks, the state of decalcification was observed by microradiography, and scored as described below to evaluate acid resistance.

◎ Demineralization is almost suppressed. ○ Demineralization is suppressed to some extent. △ Demineralized is considerably depleted. × No demineralization suppression effect. The results are shown in Table 2.

From the above results, when 3-pyridylcarbinol was used in combination with sodium fluoride, a remarkable increase in fluorine uptake in bovine tooth enamel and a remarkable suppression of demineralization were observed as compared with sodium fluoride alone, and the amount of fluorine added to 3-pyridylcarbinol was increased. A potentiating effect of sodium chloride was observed.

As judged from Examples 1 and 2, the oral composition of the present invention contains one or more members selected from the group consisting of one or more members selected from pyridylcarbinols and nicotinic acids as fluorides. Is a very useful oral composition in which the conventional caries preventive effect of fluoride is enhanced by using together.

[Examples] The present invention will be specifically described with reference to Examples and Comparative Examples. The present invention is not limited to this. The compounding amounts are all weight%.

Example 1 Toothpaste Dicalcium phosphate dihydrate 40.0 Glycerin 10.0 Sorbitol 10.0 Sodium carboxymethyl cellulose 1.5 Sodium lauryl sulfate 1.5 Sodium saccharin 0.1 Perfume 1.0 Sodium monofluorophosphate 0.76 3-Pyridylcarbinol 1.0 Purified water balance The above composition A toothpaste was prepared by the usual manufacturing method.

Comparative Example 1 Toothpaste Comparative Example 1 was obtained in the same manner as in Example 1 except that 3-pyridylcarbinol was removed from Example 1.

Comparative Example 2 Toothpaste From Example 1 Sodium Monofluorophosphate and 3-
Comparative Example 2 was obtained in the same manner as in Example 1 except that pyridyl carbinol was removed.

The toothpastes of Example 1, Comparative Example 1 and Comparative Example 2 were each diluted to 1/10 with distilled water, and the enamel powder of human extracted teeth was immersed therein at 37 ° C. for 60 minutes and thoroughly washed. It was filtered with a filter and dried. Regarding the human enamel powder treated in this way, the fluorine concentration in the powder was measured by the microdiffusion method, and it was immersed in an acetate buffer at 37 ° C for 60 minutes to measure the amount of eluted calcium. The ash inhibition rate was calculated and the acid resistance was evaluated.

The results are shown in Table 3.

As is clear from the above results, the toothpaste of the present invention has a significantly higher fluorine uptake effect and demineralization-inhibiting effect than the comparative toothpaste.

Example 2 Toothpaste Silicic anhydride 20.0 Sorbitol 50.0 Carrageenan 0.5 Sodium carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.8 Sodium saccharin 0.08 Methyl paraoxybenzoate 0.2 Perfume 0.9 Sodium fluoride 0.2 Nicotinic acid 0.5 Purified water Residual Example 3 Toothpaste Sorbitol 20.0 Silica anhydride 50.0 Sodium polyacrylate 0.7 Sodium lauryl sulfate 1.8 Triethanolamine 0.5 Sodium saccharin 0.1 Sodium paraoxybenzoate 0.2 Perfume 0.9 Sodium monofluorophosphate 0.76 Nicotinic acid amide 0.3 Allantoin 1.0 Purified water balance Example 4 Mouse wash Ethyl alcohol 10.0 Sodium saccharin 0.05 Perfume 0.8 Polyoxyethylene (20 mol) sorbitan lauric acid ester 1.0 Sodium fluoride 0.05 Nicotinic acid amide 1.0 Water balance Example 5 Mouthwash Sodium fluoride 0.05 3-Pyridylcarbinol 0.5 Disodium phosphate 0.3 Monosodium phosphate 0.7 Fragrance 0.5 Sodium saccharin 0.02 Purified water Balance Example 6 Topical application sodium fluoride 2.0 3-Pyridylcarbinol 1.0 Fragrance 0.5 Saccharin sodium 0.02 Purified water balance Example 7 Oral cooling agent (spray type) Ethyl alcohol 40.0 Saccharin sodium 0.1 Sorbitol 10.0 Fragrance 1.0 Polyoxyethylene (60 mol) Hydrogenated castor oil 0.7 Chlorhexidine hydrochloride 0.05 Sodium fluoride 0.05 Nicotinic acid methyl ester 0.5 Purified water Balance Example 8 Chewing gum Gum base 25.0 Calcium carbonate 2.0 Flavor 1.0 Copper chlorophyll 0.05 Sodium fluoride 0.2 Nicotinic acid ethyl ester 0.1 Sorbitol balance

Claims (1)

[Claims] 1. An oral composition comprising one or more selected from fluorides and one or more selected from pyridylcarbinols and nicotinic acids.