KR20170076421A - Oral Composition having policresulen and fluorine compound - Google Patents

Abstract

The present invention relates to an oral composition, and more particularly to a composition for oral hygiene, characterized by comprising polycrystalline and fluorinated compounds together. The present invention can dramatically increase the prevention and treatment of periodontal disease and the prevention of tooth decay by inhibiting plaque formation by using polycrystalline and fluoride compounds in combination.

Description

BACKGROUND OF THE INVENTION 1. Field of the Invention [0001] The present invention relates to an oral composition comprising policresulene and fluorine compounds,

The present invention relates to a composition for oral care, particularly, a composition for oral hygiene, and more particularly, to a composition for promoting oral hygiene which has an effect of significantly preventing and / or preventing periodontal disease and prevention of tooth decay through prevention of plaque formation.

The present invention relates to a composition for promoting oral hygiene which is excellent in prevention and treatment of periodontal disease and prevention of tooth decay.

Various oral diseases in oral tissues are caused by plaque composed of numerous germs present in the oral cavity. Clinical and pathological significance thereof has been extensively studied. Alexander (Alecxander, AG; J Periodent, 42:21 (1984), and J (1983), and J (1983), and others.

In the present day, a variety of drugs and compositions for promoting oral hygiene applied thereto have been introduced and used for the treatment of plaque diseases and the like caused by the inhibitory effect of plaque bacteria. One of the most widely used and effective drugs is fluorine, and a lot of research has been conducted on it.

For example, British Patent Nos. 1,005,089 and 1,089,367 have shown good tooth decay prevention effects by applying sodium monofluorophosphate (SMFP) to dentifrices, while Melberg et al. Have found that the use of sodium monofluorophosphate and sodium fluoride alone (Dent Res 63 (9): 1130-1135, 1984). It was confirmed that the tooth decay was effective to prevent tooth decay. U.S. Pat. No. 4,193,988 discloses a toothpaste prescription in which the fluoride application effect of teeth is increased by using sodium fluorophosphate and sodium glycerophosphate.

The prevention of tooth decay in these fluoride compounds is explained by the formation of fluoroapatite by the reaction of hydroxyapatite, which is a chemical composition of teeth, with fluorine ions. The fluoride apatite smoothes the surface of the tooth to prevent S. mutans and other bacteria from sticking to the teeth while the fluoride apatite is less soluble in acid than hydroxyapatite and prevents dissolution by the acid, which is the initial stage of cavities.

On the other hand, in Korean Patent Laid-Open Publication No. 10-2015-0066756, it is possible to inhibit the formation of a biofilm called biofilm or membrane by applying polycrylene into the oral cavity through a composition for inhibiting biofilm formation containing polycrystalline , Thereby preventing plaque formation in the oral cavity without destroying normal bacteriological ecosystems.

However, since both the fluorinated compound and polycrystalline are easily washed-out with a water-soluble substance, there is no sterilizing effect against bacteria such as S. mutans in the content range that can be contained in a general oral composition, .

Korean Patent Publication No. 2001-0069757 (published on July 25, 2001) Korean Patent Publication No. 10-2015-0066756 (published on June 17, 2015)

Accordingly, it is an object of the present invention to provide a composition for oral use, in particular, for oral hygiene, which has an excellent effect of significantly increasing the prevention and treatment of periodontal disease and prevention of tooth decay by inhibiting plaque formation while using a relatively small amount of active ingredient.

The present inventors have found that a composition comprising policresulen and a fluoride compound significantly improves the prevention and treatment of periodontal disease and the prevention of tooth decay through prevention of plaque formation The present invention has been completed. That is, the present invention is based on the technical idea that the conventional oral hygiene enhancing composition can effectively prevent periodontal disease prevention and treatment and tooth decay by mixing fluoride compound and polycrystalline in proper ratio.

Accordingly, the present invention provides compositions for enhancing oral hygiene comprising polycrystalline and fluorinated compounds.

The composition for enhancing oral cavity of the present invention can be used for various purposes such as toothpaste containing polycrystalline and fluoride compound, mouthwash, mouth spray, gum, ointment, oral patch.

That is, the present invention provides an oral composition in which the effect is enhanced by including polycrystalline and an fluoride compound.

The term 'composition for oral hygiene' in the present invention means a composition for application to the oral cavity which has an effect of dramatically increasing the prevention and treatment of periodontal diseases and prevention of cavities through inhibition of plaque formation, It is characterized in that the effect of inhibiting the formation of plaques of polycrystalline or fluorinated compounds is remarkably increased. The 'oral composition' or 'oral hygiene composition' of the present invention may further have an effect of prevention of formation of teeth, promotion of oral hygiene, prevention and treatment of oral diseases such as periodontitis and gingivitis through inhibition of formation of biofilm .

Policresulene according to the present invention may also be referred to as Albothyl or Polylene, and has a structure represented by the following formula (1), and its chemical formula is the same as (C ₉ H ₈ O ₄ S) _n .

Preferably, n in the general formula (1) is 1 to 3, more preferably n is 3.

Since the polycrysulene of the present invention is well soluble in water, it is dissolved and present in an oral composition such as a toothpaste containing an excessive amount of water without precipitation.

Examples of fluorinated compounds according to the present invention include sodium fluoride, sodium fluorophosphate, noble metal fluoride, 297 (N, N, N'-tris- (2-hydroxyethyl) -N'-octadecyl-1,3-diaminopropane dihydrofluoride) Or a mixture thereof may be used.

The oral composition of the present invention may contain 0.0005 to 2% by weight of polycrystalline based on the total weight of the composition for the purpose of the present invention mentioned above; And a fluorine-reduced content of 20 to 10,000 ppm by weight of fluorinated compounds.

Preferably, the composition for oral or dental care of the present invention comprises 0.001 to 1% by weight of polycrystalline based on the total weight of the composition; And fluorinated compounds having a fluorinated content of 100 to 7000 ppm by weight.

More preferably, the oral composition of the present invention comprises 0.005 to 0.5% by weight of polycrystalline based on the total weight of the composition; And fluorinated compounds having a fluorinated content of 200 to 2000 ppm by weight.

Even more preferably, the oral composition of the present invention comprises 0.008 to 0.1% by weight of polycrystalline relative to the total weight of the composition; And a fluorinated compound having a fluorine-converted content of 500 to 1500 ppm by weight.

When the content of polycrysulene in the oral composition of the present invention is at least the lower limit of the above content range, the effect of inhibiting the biofilm formation is excellent, which is advantageous for obtaining a favorable effect against economic investment, The skin irritation that may be caused by polycrystalline can be maintained at the desired level.

When the content of the fluoride compound in the oral composition of the present invention is at least the lower limit value of the above content range, the effect of suppressing the formation of plaque can be raised to a desirable level, and when the fluoride compound content is less than or equal to the upper limit value of the content range The human body safety can be ensured more reliably.

That is, in the oral composition of the present invention, when the content ratio of polycrystalline and fluorinated compound, that is, the mixing ratio is out of the above range, synergism (for example, in terms of prevention of plaque formation) It is preferable to add the antioxidant in the above-mentioned content ratio because the antiperspirant effect is insufficient and consequently the tooth decay prevention and inflammation relief / treatment effect to be achieved through it is insignificant.

The composition of the present invention may be provided in various forms such as toothpaste, mouthwash, mouthwash, oral spray, gum, oral ointment, oral patch, and the like. A wetting agent, a binder, a foaming agent, a sweetener, a preservative, a medicinal agent, a flavoring agent, an acidity regulating agent and a brightener may be appropriately used depending on the type, kind and purpose of use of the composition. That is, in addition to the above-mentioned components, the composition according to the present invention may further contain additives such as an abrasive, a wetting agent, a binder, a foaming agent, a sweetener, an antiseptic, a preservative, , A pharmacological agent, a flavoring agent, an acidity adjusting agent, a brightening agent, purified water, and the like. For example, when the formulation containing the oral care composition of the present invention is a dentifrice composition, at least one selected from the group consisting of abrasives, wetting agents, binders, foaming agents, sweeteners, preservatives, medicinal agents, fragrances, May further comprise additives.

For example, the composition for oral hygiene may include a weight% fluorinated compound having 0.0005 to 2% by weight of polycrystalline and 20 to 10,000 ppm in terms of fluorine in the whole composition, 15 to 60% by weight of an abrasive as an additive, From 0.05 to 0.3% by weight of a sweetener, from 0.05 to 0.3% by weight of a preservative, from 0.1 to 0.3% by weight of a medicinal agent, from 0.5 to 3% by weight of a flavoring agent and from 0.5 to 5% And may include the remaining amount of purified water.

The abrasive is preferably at least one selected from the group consisting of calcium monohydrogenphosphate, precipitated silica, calcium carbonate, hydrated alumina, kaolin and sodium hypophosphite, preferably calcium monohydrogenphosphate, precipitated silica or a mixture thereof, And may be used in an amount of 5 to 50% by weight based on the composition.

The wetting agent is preferably at least one selected from the group consisting of glycerin, sorbitol, amorphous sorbitol solution, propylene glycol, polyethylene glycol and xylitol, preferably a sorbitol solution, for example 20 to 60 wt% Can be used.

Examples of the binder include sodium carboxymethylcellulose, carrageenan, xanthan gum, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, guar gum, gellan gum, carbomer, pectin, polyvinylpyrrolidone, carboxyvinylpoly And is at least one selected from the group consisting of sodium alginate and laponite, preferably carboxymethylcellulose sodium, and can be used, for example, in an amount of 0.5 to 2% by weight based on the total composition.

Examples of the foaming agent include anionic surfactants such as sodium lauryl sulfate and sodium lauryl sarcosinate; Sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene / polyoxypropylene type copolymer materials and the like; Or cocoa idpropyl betaine, preferably sodium laurylsulfate, for example 0.5 to 5% by weight, based on the total composition.

The sweetener is one or more, preferably saccharin sodium, selected from the group consisting of saccharin sodium hydrate, sucralose, maltitol, aspartame, erythritol and licorice acid, for example, 0.05 to 0.3 wt% Can be used.

The antiseptic is at least one selected from the group consisting of p-hydroxybenzoate and sodium benzoate, preferably paraoxybenzoic acid ester, and may be used, for example, in an amount of 0.05 to 0.3% by weight based on the total composition.

Examples of the active agent include at least one selected from the group consisting of tocopherols, chlorhexidine, aminocaproic acid, dipotassium glycyrrhizinate, tranexamic acid, allantoin, caproic acids, polyphosphates, enzymes and herbal extracts, May be tocopherol acetate. For example, the pharmacologically active agent may be used in an amount of 0.01 to 1.0% by weight based on the total composition.

The flavoring agent may be a natural flavoring agent such as peppermint oil or spearmint oil and a synthetic flavoring agent such as menthol and carbohydrate, and the mixture may be mixed with an appropriate amount of anise oil. For example, the content of the perfume can be 0.5 to 3% by weight.

The present invention relates to an oral composition, and more particularly to a composition for oral hygiene, characterized by comprising polycrystalline and fluorinated compounds together. The present invention is based on the fact that the use of polycrystalline and fluorinated compounds can dramatically increase the prevention and treatment of periodontal disease and the prevention of tooth decay through suppression of plaque formation.

Fig. 1 is a photograph showing the result of evaluation of the effect of inhibiting the formation of tooth surface bacteria using the respective examples or comparative examples according to the present invention, and showing colored prags. The degree of effect was evaluated by comparing the colored areas on the HAP DISK.
Figure 2 is a diagram showing a plaque index used in the evaluation of the dentifrice composition according to the present invention. Quot; Turesky Modification of Quigley-Hein plaque index "which is commonly used in the field of the present invention.

Hereinafter, embodiments of the present invention will be described in detail to facilitate understanding of the present invention. However, the embodiments according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the following embodiments. Embodiments of the present invention are provided to more fully describe the present invention to those skilled in the art to which the present invention belongs.

Example  1 to 6 and Comparative Example  1 to 3

The dentifrice compositions of Examples 1 to 6 and Comparative Examples 1 to 3 were prepared with the components and composition ratios shown in Table 1 below. Powder components such as carboxymethylcellulose sodium and saccharin sodium hydrate were dispersed in Solvitol solution, which is a wetting component, and purified water was added thereto, followed by primary mixing in a mixer. Then, an abrasive such as precipitated silica and a medicinal agent were added and mixed.

Finally, sodium lauryl sulfate as a foaming agent and fragrance ingredients were added and mixed under vacuum to prepare dentifrice compositions with the components and composition ratios shown in Table 1 below.

division
(Unit: wt%) Example Comparative Example One 2 3 4 5 6 One 2 3 Dental type silica 14.00 14.00 14.00 14.00 14.00 14.00 14.00 14.00 14.00 Sorbitol solution (70% by weight) 60.00 60.00 60.00 60.00 60.00 60.00 60.00 60.00 60.00 Sodium lauryl sulfate 1.50 1.50 1.50 1.50 1.50 1.50 1.50 1.50 1.50 Sodium saccharin hydrate 0.10 0.10 0.10 0.10 0.10 0.10 0.10 0.10 0.10 Carboxymethylcellulose 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 Spices 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 Purified water Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Polycrystalline 0.001 0.01 0.01 0.10 0.01 0.01 - 0.01 - Sodium fluoride 0.22 0.11 0.22 0.22 0.11 - - - 0.22 Sodium fluorophosphate - - - - 0.38 0.76 - - -

Experimental Example  1: Fluorinated compound and Polycrystalline  Containing toothpaste Tooth film formation  Inhibitory effect

Streptococcus mutans were cultured overnight at 37 ° C in BHI medium. The toothpaste of Table 1 to be measured was diluted 10-fold (by weight ratio) in the BHI medium and sucrose was added to the BHI medium to a concentration of 1% by weight to form the plaque. A hydroxyapatite disk was placed in 24 wells to make the same conditions as the tooth surface. After overnight incubation, Streptococcus mutans was inoculated and incubated overnight at 37 ° C. The hydroxyapatite surface was washed with distilled water and the plaque adhered to the surface was colored with Red-Cote to observe the inhibition of plaque formation in Examples and Comparative Examples. The results of the experiment are shown in FIG. Fig. 1 is a photograph showing colored prags for the respective examples and comparative examples. Fig. The degree of effect was evaluated by comparing the colored areas on the HAP DISK.

As shown in FIG. 1, in Examples 3 to 6, 99% inhibition of the generation of plaque was observed, and in Examples 1 and 2, the generation of plaque was suppressed by 80%. In Comparative Example 2 containing only polycrysulene alone, the production of plaque was inhibited by 40%. In Comparative Example 1, which did not contain polycrystalline and fluorinated compounds, and Comparative Example 3, which contained only fluoride compounds, Production was suppressed to about 20% or less.

Experimental Example  2: fluorinated compound and Polycrystalline  Containing toothpaste Recall  effect

The toothpaste compositions of Examples 2 to 4 and Comparative Examples 2 to 3 of Table 1 were used to evaluate the fluoride uptake of the toothpaste. The evaluation was performed by changing the hardness using the recrystallization evaluation method of the UCHI specimen.

The experimental method is as follows. First, the wick sample was demineralized for 4 days with 0.1 molar lactic acid solution to demineralize Vickers hardness to 28 ~ 45. The demineralized samples were subjected to re-crystallization for 20 days for the toothpaste of Examples and Comparative Examples as shown in Table 2 below. After 20 days of treatment, the specimens were washed with distilled water. Then, the change in hardness of the sample was measured using a Vickers hardness tester.

Treatment process time Remarks toothpaste 1 minute saliva 59 minutes toothpaste 1 minute saliva 59 minutes toothpaste 4 hours 0.1 molar lactic acid solution saliva 59 minutes toothpaste 1 minute saliva 59 minutes toothpaste 1 minute saliva 59 minutes Saliva treatment until overnight

The results of the experiments using the toothpaste of each of the examples and comparative examples are shown in Table 3 below.

division Hardness change (? VHN) Statistical significance (p <0.01) Example 2 20.28 + - 2.33 ** Example 3 23.76 ± 1.73 ** Example 4 25.62 ± 2.11 P = 0.08 Comparative Example 2 4.22 ± 2.07 - Comparative Example 3 11.88 ± 3.07 -

As shown in the results of Table 3, in the case of the toothpaste using the fluoride compound and polycrystalline (Examples 2 to 4), the teeth using the fluoride compound and the toothpaste without using polycrystalline (Comparative Examples 2 to 3) The hardness was considerably higher than that of.

Experimental Example  3: Polycrystalline  And fluoride compound-containing toothpaste Tooth film formation  Evaluation of inhibitory effect

<Experimental Method>

The results are shown in Table 1. The results are shown in Table 1. The results are shown in Table 1. The results are shown in Table 1 and Table 2, Respectively. Subjects were divided into six groups (buccal, mesial, buccal, central, lingual, lingual, lingual, and lingual - lingual) of 20 or more natural teeth in the oral cavity. At this time, the crown with a fixed orthodontic appliance or with restoration of the entire dental surface was excluded. In order to evaluate the inhibition of bacterial membrane formation, dental plaque was stained using a plaque dyeing reagent, and then one person scored the Turesky Modification of Quigley-Hein plaque index (PI) according to the following criteria. The Turesky Modification of Quigley-Hein plaque index is shown in FIG.

0 point = no plaque at all

1 point = When the teeth are not connected and have one island shape

2 points = When there is a plaque in the form of a line along the edge of the gingival margin

3 points = there is a plaque in 1/3 of cervical area

4 points = there is a plaque on 2/3 of the crown

5 points = Almost all teeth covered by the entire crown

            PI = sum of total points / total number of teeth examined

<Experimental Results>

The plaque index measurement results are shown in Table 4 below. As shown in Table 4, after 4 weeks of using toothpaste, Comparative Example 2 increased 2.5% from the initial value after use of toothpaste, and increased 4.9% from the initial value after using toothpaste in Comparative Example 3, but decreased 2.7% in Example 3 toothpaste. In addition, it was confirmed that the effectiveness rate of the study subjects was 58% of the toothpaste users of Example 3 after 4 weeks of using the toothpaste. Thus, it can be seen that the combination of fluoride compound and polycrysulene has the effect of dramatically increasing the prevention and treatment of periodontal disease and prevention of tooth decay through suppression of plaque formation.

Toothpaste group n Baseline
Mean (standard deviation) After 4 weeks
Mean (standard deviation) P-value Comparative Example 2 25 3.19 (0.39) 3.27 (0.31) <0.001 Comparative Example 3 25 3.09 (0.41) 3.24 (0.34) Example 3 26 3.29 (0.37) 3.20 (0.46)

Claims (6)

An oral composition comprising policresulen and fluoride compounds. The method according to claim 1,
Wherein the fluoride compound is sodium fluoride, sodium fluorophosphate, noble metal fluoride, fluorine amine 297, or a mixture thereof. 3. The method according to claim 1 or 2,
The composition may be present in an amount
0.0005 to 2% by weight of polycrystalline; And
The fluorine-converted content is 20 to 10,000 by weight of fluorinated compounds. The method of claim 3,
The composition may be present in an amount
0.001 to 1% by weight of polycrystalline; And
Wherein the composition contains fluorinated compounds having a fluorine-converted content of 100 to 7000 ppm by weight. 5. The method of claim 4,
The composition may be present in an amount
0.005 to 0.5% by weight of polycrystalline; And
Wherein the composition contains fluorinated compounds having a fluorinated content of 200 to 2000 ppm by weight. 6. The method of claim 5,
The composition may be present in an amount
0.008 to 0.1% by weight of polycrystalline; And
Wherein the composition contains fluorinated compounds in a weight percentage of 500 to 1500 ppm in terms of fluorine.

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