KR20180045614A - Oral composition comprising policresulen - Google Patents

Abstract

The present invention relates to an oral composition containing policresulen, intended to increase adsorption and/or retention of policresulen in an oral cavity by using an oral tissue astringent and also to improve effectiveness of policresulen. Therefore, the composition, according to the present invention, is excellent in prevention of plaque formation and relief of inflammation due to periodontitis and gingivitis.

Description

BACKGROUND OF THE INVENTION [0002] Oral composition comprising policresulen

The present invention relates to an oral composition comprising polycrystalline. More specifically, the present invention relates to a composition for preventing or preventing plaque formation of polycrysulene, and a composition for promoting oral hygiene, wherein the effect of reducing periodontitis and gingivitis is further improved.

The plaque formed by oral bacteria in the oral cavity is the primary cause of oral-related diseases such as tooth decay and gingivitis.

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, It is possible to inhibit plaque formation in the oral cavity without destroying normal bacteriological ecosystems.

However, the inventors of the present invention have found that the effect of the oral composition containing polycrysulene is not maintained for a long period of time, and therefore, research for continuing this effect is required.

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

Accordingly, a problem to be solved by the present invention is to provide a composition for oral care containing polycrysulene, in particular, a composition for oral hygiene which has an increased duration (or increased effect) of effect.

Another object to be solved by the present invention is to provide a method for increasing (or increasing) the duration of effect of polycrysulene and improving the effect of polycrysulene.

Another object to be solved by the present invention is to provide a composition and / or a kit containing such a composition that can increase (or increase) the duration of effect of polycrysulene and improve the effect of polycrysulene.

In order to solve the above-described problems, the present invention provides a technical idea that the effect duration of a policresulen can be increased or increased by using an oral tissue astringent agent.

As a result of the study by the inventors of the present invention, it was confirmed that polycrysulene, which is a water-soluble substance, is hard to stay in the mouth for a long time due to the characteristics of the oral cavity environment and thus it is difficult for the polycrysulene to continuously exhibit its effects in the oral cavity. And the need for a technique to keep the pharmacological action of polycrysulene constant. DISCLOSURE OF THE INVENTION Problems to be Solved by the Invention The present inventors have conducted various studies to solve the problems in the prior art as described above. When the oral tissue astringent is included in a composition containing polycrystalline, the inventors have improved the adsorption of polycrystalline in the oral cavity, It was found that there was an excellent effect of inhibiting film formation, and thus the present invention was completed. However, the present invention is not limited to these conventional guesses.

Accordingly, the present invention provides an oral composition, particularly a composition for enhancing oral hygiene, comprising (a) policresulen and (b) an oral tissue astringent.

The present invention also provides a composition for oral administration, particularly a composition for enhancing oral hygiene, which comprises an oral tissue astringent agent as an application for enhancing the effect of polycrysulene in an oral composition containing polycrysulene.

The present invention also provides a method for enhancing the effect of polycrystalline, characterized in that the oral tissue astringent is applied in the mouth concurrently with the application of polycrystalline or prior to application of polycrystalline. In this way, oral hygiene can be further enhanced.

The present invention also provides an oral kit comprising a composition comprising (a) a composition comprising polycrystalline, and (b) an oral tissue astringent for use to enhance the effect of the polycrystalline.

The present invention also provides a composition for enhancing the effect of polycrystalline comprising an oral tissue astringent as an active ingredient.

The 'oral composition' or 'oral hygiene composition' according to the present invention can prevent the formation of teeth and / or promote oral hygiene and / or prevent and / or treat oral diseases such as periodontitis and gingivitis through inhibition of biofilm formation The present invention also relates to a composition for oral application of polycrysulene, which comprises polycrysulene as an effective enhancing substance, together with an oral tissue astringent, to increase the residual and / or adsorption of polycrystalline in the oral cavity, The desired effect can be exerted more excellently.

Policresulene used in the present invention may also be referred to as Albothyl or Polylene and has a structure of the following formula 1 and has the same chemical formula 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.

In the present invention, it is obvious that the oral tissue astringent agent plays a role of enhancing the residual and / or adsorption of polycrystalline, but it may play an additional role in addition to this role. In the present invention, But is not limited to a particular theoretical mechanism of the retention and / or adsorption enhancement.

The oral tissue astringent of the present invention may be a halogen compound containing a cation such as sodium, potassium, calcium, and magnesium, a sulfate compound, a carbonate compound, a phosphate compound, or a mixture thereof.

Specifically, the oral tissue astringent may be selected from the group consisting of sodium chloride, potassium chloride, calcium chloride, magnesium chloride, sodium sulfate, potassium sulfate, sodium hydrogen carbonate, sodium carbonate, potassium phosphate monobasic, potassium phosphate dibasic, At least one selected from the group consisting of sodium phosphate, sodium tertiary phosphate, and sodium saccharin.

The sodium chloride may be contained in the form of salt containing sodium chloride and may be contained in the form of, for example, bamboo salt, bamboo salt, sun salt, refined salt, formulated salt or pharmacopoeial salt, have.

Among the various oral tissue astringents, the form of bamboo salt is more preferable in terms of the feeling of touch, the continuity of cleanliness, flavor and overall satisfaction in actual use.

Bamboo salt in sodium chloride used in the present invention is a generic name of salt using bamboo, and is, for example, bamboo salt synthesized through a pyrogen method using bamboo and salt mentioned in Korean Patent Registration No. 85705, Bamboo, a cell-producing bamboo, and salt that prevents sterilization and decay are repeated several times from a baking furnace to a high temperature to melt salt, and to make bamboo salt by hardening. The bamboo salt thus produced contains a lot of minerals such as potassium, calcium, magnesium and iron in addition to sodium. Bamboo salt also contains similar mineral and ionic components to bamboo salt. It is especially excellent for the oral mucous membrane to converge when it is applied by various kinds of minerals and sodium chloride components contained in bamboo salt or bamboo salt. As the convergence occurs, the swollen cells are contracted. At this time, the polycrysulene in the buccal mucosa converges on the oral tissues, and it is presumed that the remaining polycrysulene continuously exhibits the weak efficacy. However, the present invention is not limited to this theoretical mechanism.

The content of polycrystalline in the composition for oral cavity or intraocular polycarzulene residue or adsorption enhancement according to the present invention is preferably 0.0005 to 2% by weight, more preferably 0.0001 to 1% by weight based on the total weight of the composition for various purposes of the present invention %, And still more preferably 0.001 to 0.1 wt%. In addition, the content of the oral tissue astringent agent in the composition according to the present invention is preferably 0.1 to 5% by weight, more preferably 0.2 to 4% by weight, and still more preferably 0.3 to 3% by weight for various purposes of the present invention.

When the content of the polycrysulene is less than 0.0005% by weight based on the total weight of the composition, the effect of inhibiting the biofilm formation is small and it is difficult to achieve the practical purpose of the present invention. If the content exceeds 2% by weight, stimulation and surgical wound There is a problem.

The oral tissue astringent agent is added for the purpose of the present invention such as increase in adsorption and residual effect of polycrystalline. When the content is less than 0.1% by weight based on the total weight of the composition, If the content is more than 10% by weight, the effect of increasing the content is insignificant. In addition, excessive salt addition may result in strong salty, pungent, and pungent taste. As a result of the sensory evaluation performed by the present inventors on about 10 men and women, when the content exceeded 5% by weight, consumer preference was very poor.

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, the kind and the 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 various additives such as an abrasive, a wetting agent, a binder, a foaming agent, a sweetening agent, a drug efficacy, and the like for the purpose of appropriate formulation, formulation stability, A flavoring agent, a purified water, and the like.

When the formulation comprising the composition for promoting oral hygiene of the present invention or the composition for retaining / enhancing the intraocular polycrylaine is a dentifrice composition, it is preferable that the composition is an abrasive, a wetting agent, a binder, a foaming agent, a sweetener, a medicinal agent, a flavoring agent, And at least one additive selected from the group consisting of:

The abrasive is at least one selected from the group consisting of calcium monohydrogenphosphate, precipitated silica, calcium carbonate, hydrated alumina, kaolin and sodium hypophosphite, preferably calcium monohydrogenphosphate and / or precipitated silica, % ≪ / RTI > by weight.

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 at least one selected from the group consisting of sodium alginate and laponite, preferably carboxymethyl cellulose sodium, and may be used, for example, in an amount of 0.5 to 2% by weight based on the total weight of the 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 an amphoteric surfactant such as cocoa idopropylbetaine, preferably sodium lauryl sulfate, and may be used in an amount of 0.5 to 5% by weight based on the total weight of the composition.

The sweetener may be one or two or more, preferably sucralose, selected from the group consisting of sucralose, maltitol, aspartame, erythritol and licorice acid, and may be used in an amount of 0.05 to 0.3% by weight based on the total weight of the composition.

Examples of the active agent include sodium fluoride, sodium fluorophosphate, calcium fluoride, fluoroamine, chlorhexidine, aminocaproic acid, dipotassium glycyrrhizinate, tranexamic acid, allantoin, caproic acids, polyphosphates, , Preferably sodium fluoride, 0.1 to 0.3% by weight based on the total weight of the composition.

As the fragrance, an appropriate amount of synthetic flavoring agents such as peppermint oil, spearmint oil and the like and a synthetic flavoring agent such as menthol and carboin are mixed and used. Preferably, an appropriate amount of anise oil is mixed with a certain amount of the fragrance. The content of the perfume may be 0.5 to 3% by weight based on the total weight of the composition.

For example, the composition for oral hygiene or intraoral oral adsorption enhancer comprises 0.0005 to 2% by weight of polycrystalline and 0.1 to 5% by weight of sodium chloride relative to the total weight of the composition, 15 to 60% by weight of an abrasive as an additive, By weight of a sweetener, 0.1 to 0.3% by weight of a pharmacologically active agent, 0.5 to 3% by weight of a flavoring agent, and a balance of purified water, wherein the wetting agent comprises 20 to 60% by weight of a wetting agent, 0.5 to 20% by weight of a binder, 0.5 to 5% Lt; / RTI >

The present invention provides a composition for oral care containing polycrysulene, particularly a composition for oral hygiene, which has an increased duration (or increased effect) of effect.

The present invention also provides a method for increasing (or increasing) duration of effect of polycrysulene and improving the effect of polycrysulene.

The present invention also provides compositions and / or kits comprising such compositions that can increase (or increase) the duration of effect of polycrysulene and enhance the effect of polycrysulene.

As a result, the composition according to the present invention improves the residual force in oral cavity of polycrysulene, has an effect of preventing plaque formation, and has an effect of reducing inflammation of periodontitis and gingivitis.

FIG. 1 is a diagram showing a plaque index used in the evaluation of the results of Experimental Example 2. FIG. Quot; Turesky Modification of Quigley-Hein plaque index "which is commonly used in the art.
2 shows a questionnaire used in a consumer evaluation of toothpastes according to one embodiment of the present invention.
Figure 3 is a consumer assessment of toothpaste embodiments in accordance with 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 invention are provided to more fully describe the present invention to those skilled in the art.

Example  1 to 11 and Comparative Example  1 to 3

The dentifrice compositions of Examples 1 to 11 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 the like were dispersed in Solvitol solution, which is a wetting component, and purified water was added, followed by primary mixing in a mixer. Then, an abrasive such as precipitated silica and a pharmaceutical agent were added and mixed.

Finally, sodium lauryl sulfate as a foaming agent and fragrance components were added and mixed under vacuum to prepare a dentifrice composition.

division
(Unit: wt%) Example Comparative Example One 2 3 4 5 6 7 8 9 10 11 One 2 3 Dental type silica 14 14 14 14 14 14 14 14 14 14 14 14 14 14 Sorbitol solution
(70%) 50 50 50 50 50 50 50 50 50 50 50 50 50 50 Sodium lauryl sulfate 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 Sucralose 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 Carboxymethylcellulose One One One One One One One One One One One One One One Sodium fluoride 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 Spices One One One One One One One One One One One One - One Purified water Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Suitable amount Polycrystalline 0.001 0.01 0.1 0.01 0.01 0.01 0.01 0.01 0.01 0.01 0.01 - 0.01 - Bamboo salt One One One 2 3 - - - - - - - - One Sun salt - - - - - One - - - - - - - - Pharmacopoeial salt - - - - - - One - - - - - - - Sodium hydrogencarbonate - - - - - - - One - - - - - - Calcium chloride - - - - - - - - One - - - - - Sodium phosphate monobasic - - - - - - - - - One - - - - Sodium saccharin - - - - - - - - - 0.2 - - - -

Experimental Example 1. Measurement of presence or absence of polycrystalline

After brushing for 10 minutes, the saliva was collected over a period of 1 minute, and the presence or absence of the detection of polycrystalline was measured with a liquid chromatograph Method.

The measurement results are shown in Table 2 only as detection or non-detection (detection (O), non-detection (X)) of polycrystalline.

division  Example  Comparative Example One 2 3 4 5 6 7 8 9 10 11 One 2 3 Elapsed time Immediately O O O O O O O O O O O X O X 5 minutes O O O O O O O O O O O X X X 10 minutes O O O O O O O O O O O X X X 30 minutes O O O O O O O O O O O X X X

As shown in the above Table 2, in the experimental results, it was confirmed that the polycrysulene was continuously detected until 30 minutes after brushing, but the toothpaste of Comparative Example 2 was detected immediately after brushing, but dilution and ingestion by saliva It was not detected even after 5 minutes immediately after brushing. That is, it was confirmed that the residual force of polycrysulene was significantly increased by the simultaneous use with the oral tissue astringent agent.

Experimental Example  2. Polycrystalline  And bamboo salt-containing toothpaste Tooth film formation  Inhibitory effect

<Experimental Method>

In the case of men and women aged 20 to 65 years who have at least 20 natural teeth, using Example 2 and Comparative Examples 1 and 2 of Table 1 for 4 weeks, after the initial and 4 weeks, . The subjects were divided into six groups (buccal, medial, buccal, medial, buccal, lingual, lingual, lingual, lingual). At this time, the crown with a fixed orthodontic appliance or with a complete restoration of the tooth surface was excluded. In order to evaluate the inhibition of bacterial membrane formation, dental plaques were stained using a dental staining reagent, and then one of the testers was evaluated by the Turesky Modification of Quigley-Hein plaque index (PI) according to the following criteria .

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 results of the plaque index measurement are shown in Table 3 below. As shown in Table 3 below, the results after 4 weeks of using toothpaste showed a 5.6% increase compared to that of Comparative Example 1 toothpaste, a decrease of 2.7% in Comparative Example 2 toothpaste, and 4.6% in Example 2 toothpaste. In addition, it was confirmed that the effectiveness rate of the study subjects was found to be the same or lower than that of the toothpaste after 4 weeks of toothpaste use, that is, 58% of the toothpaste users of Comparative Example 2 and 82% of the users of the toothpaste of Example 2. Through this, it can be seen that oral compositions containing polycrysulene and bamboo salt cause a synergistic increase in their function through various causes (for example, increase in adsorption of polycrysulene in the oral cavity).

Toothpaste group n Baseline
Mean (standard deviation) After 4 weeks
Mean (standard deviation) P-value Comparative Example 1 25 3.09 (0.41) 3.24 (0.34) <0.001 Comparative Example 2 26 3.29 (0.37) 3.20 (0.46) Example 2 22 3.30 (0.41) 3.13 (0.35)

Experimental Example  3. Polycrystalline  And Oral tissue astringent agent  Consumer assessment of toothpaste

Consumer sensory evaluation of toothpaste containing polycrystalline and oral tissue astringent agent was carried out by the following method.

Subjects: 30 volunteer men and women volunteers were recruited in the 20s and 40s.

Experimental method: The subjects were given a new toothpaste every week and were allowed to use only the toothpaste.

Experimental toothpaste: Example 2 and Examples 6 to 11 in Table 1 were supplied as experimental toothpaste. All the compositions were applied with the same fragrance and color, and the fragrance and color were prevented in advance.

Questionnaire items: Consumer evaluation questionnaire as shown in FIG. 2 was used for evaluation.

The results are shown in Fig. As shown in FIG. 3, the consumer evaluation result shows that the composition of Example 2 is the most satisfactory in terms of the feelings of cleanliness, persistence of cleanliness, flavor and overall satisfaction.

Experimental Example  4. Polycrystalline  And Oral tissue astringent agent  Evaluation of antibacterial activity of toothpaste containing

Consumer sensory evaluation of toothpaste containing polycrystalline and oral tissue astringent agent was carried out by the following method.

Strain: Streptococcus mutans (ATCC 25175), Porphyromonas gingivalis (ATCC 49417), Prevotella nigrescens (ATCC 25261), Fusobacterium nucleatum (ATCC 25586) was used. The strains were inoculated in the same medium and then incubated in an anaerobic incubator at 37 ° C for 72 hours after first and second subculture in a liquid medium of Brain Heart Infusion (BHI: Difco, USA). BHI was supplemented with menadion (50 ng / ml) and hemin (4 ug / ml).

Experimental method: Example 2 and Examples 6 to 11 of Table 1 were diluted in a BHI liquid medium and the final concentration was adjusted to 10% and further cultured for 3 minutes with 3 × 10 ⁵ CFU / ml of bacteria. After that, the cultures were sequentially diluted and cultured for 48 hours in a solid medium for CFU (Colony Forming Unit). All experiments were repeated three times.

The results are shown in Table 4 below. As shown in Table 4, the composition of Example 2 showed the highest antibacterial activity against oral microorganisms used in the experiment.

division S. mutans P. gingivalis P. nigrescens F. nucleatum Early 3 x 10 ⁵ 3 x 10 ⁵ 3 x 10 ⁵ 3 x 10 ⁵ Example 2 Below 100 Below 100 Below 100 Below 100 Example 6 2.0 x 10 ³ 2.2 x 10 ³ 3.0 x 10 ³ 3.0 x 10 ³ Example 8 Below 100 1.0 x 10 ³ 1.2 × 10 ³ 1.3 x 10 ³ Example 9 1.2 × 10 ³ 1.0 x 10 ³ 2.0 x 10 ³ 2.0 x 10 ³ Example 10 1.8 x 10 ³ 1.0 x 10 ³ 1.6 x 10 ³ 2.0 x 10 ³ Example 11 2.0 x 10 ³ 2.2 x 10 ³ 2.2 x 10 ³ 2.3 x 10 ³

Claims (9)

0.0 &gt; policresulen &lt; / RTI &gt; and an oral tissue astringent. In an oral composition containing policresulen,
A composition for oral use characterized by containing an oral tissue astringent agent for enhancing the effect of polycrysulene. [3] The oral composition according to claim 2, wherein the oral tissue astringent agent is for increasing residual or adsorption of polycrystalline. 4. The oral cavity astringent according to any one of claims 1 to 3, wherein the oral tissue astringent is selected from the group consisting of sodium chloride, potassium chloride, calcium chloride, magnesium chloride, sodium sulfate, potassium sulfate, sodium hydrogen carbonate, sodium carbonate, potassium phosphate monobasic, Wherein the oral composition is at least one selected from the group consisting of potassium phosphate, sodium phosphate monobasic, sodium phosphate dibasic, sodium phosphate dibasic, and sodium saccharin. The oral composition according to claim 4, wherein the sodium chloride is contained in bamboo salt, bamboo salt, sun salt, refined salt, pharmaceutical salt or pharmacological salt. The oral composition according to claim 5, wherein the composition contains bamboo salt. 4. The composition according to any one of claims 1 to 3, wherein the composition comprises 0.0005 to 2% by weight of polycrystalline, based on the total weight of the composition; And 0.001 to 5% by weight of an oral tissue astringent agent. (a) a composition containing polycrystalline, and
(b) a composition comprising an oral tissue astringent agent for enhancing the effect of the polycrysulene
Included oral kit. 9. The oral composition of claim 8, wherein the oral tissue astringent is selected from the group consisting of sodium chloride, potassium chloride, calcium chloride, magnesium chloride, sodium sulfate, potassium sulfate, sodium bicarbonate, sodium carbonate, potassium phosphate dibasic, potassium phosphate dibasic, , Sodium phosphate dibasic, sodium phosphate dibasic, sodium saccharin, and the like.

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