KR20140109685A - Composition for prevention or treatment of dental caries comprising asarinin - Google Patents

Abstract

The present invention relates to a composition comprising asarinin for oral care and, more specifically, to a composition which is safe to humans and has an excellent effect of preventing or treating dental caries. The oral composition of the present invention has fewer side effects, and thereby is safe to humans and has an excellent effect of treating or preventing dental caries.

Description

TECHNICAL FIELD The present invention relates to a composition for preventing or treating dental caries including asarinin,

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for oral care, and more particularly, to a composition which is safe for human body and is excellent in preventing or treating dental caries.

Commonly known as tooth decay, dental caries covers the surface of the head of a tooth, and translucent, hard, milky translucent tooth enamel or enamel that protects tooth dentin is formed by the bacteria in the mouth, acid, which is caused by damage to the tooth enamel.

If left untreated, the caries area becomes wider, so the treatment area becomes larger and more complicated. If the tooth progresses to pulp, neurological treatment is necessary. Depending on the degree of tooth destruction, the post may be erected or extruded in severe cases.

In order to prevent and improve such dental caries, various products for inhibiting and killing the growth of bacteria causing dental caries have been developed.

However, development of a product for treatment and / or prevention of dental caries with excellent safety using an action mechanism capable of suppressing the growth of germs causing dental caries from the beginning was insignificant.

Accordingly, the present invention is to solve the above-mentioned problems, and to provide such a useful use of a new active ingredient, i.e., an active ingredient, which is less harmful to the human body and can inhibit the growth of bacteria in the oral cavity.

In other words, a problem to be solved by the present invention is to provide a composition comprising the active ingredient having excellent efficacy as an active ingredient, particularly, a composition for oral care or a pharmaceutical composition for preventing or treating dental caries.

In order to solve the above problems, the present invention provides an oral composition or a pharmaceutical composition comprising asarinin as an active ingredient, preferably an oral composition or a pharmaceutical composition for preventing or treating dental caries.

That is, the present invention provides a new use for oral compositions or pharmaceutical compositions containing asarinin, in particular oral compositions or pharmaceutical compositions for the prevention or treatment of dental caries.

&Quot; Treatment " in the present invention is an approach to obtaining beneficial or desired clinical results, which may or may not be able to detect beneficial or desired clinical results for the purposes of the present invention, whether or not partial But are not limited to, alleviation of the disease state, reduction in the degree of disease, stabilized (i.e., less severe) condition of the disease, delay or rate reduction of disease progression, improvement or temporary alleviation and alleviation of the disease state. Thus, treatment refers to both therapeutic treatment and prophylactic measures, and those that need treatment include conditions that already have the disease, as well as conditions in which the disease is to be prevented.

The present invention also provides a composition for stimulating human mucin-7 secretion, wherein asarinin promotes the proliferation of epithelial cells to promote secretion of human mucin-7, thereby preventing or treating dental caries.

Unlike research and products based thereon that directly induce the death of harmful bacteria in the oral cavity causing dental caries to prevent or improve dental caries, the present invention promotes the proliferation of A-253 epithelial cells, It is based on the surprising discovery that the secretion of mucin-7 can be promoted indirectly to fundamentally block the growth of oral bacteria, especially dental caries-inducing bacteria. In other words, it has been found that the composition does not act directly on the dental caries-inducing bacteria, so that it is less toxic and can produce a safer composition for the human body.

Recent studies have shown that the growth of dental caries bacteria is affected by the type of mucin present in the saliva, and as the amount of human mucin-7 increases, the growth of bacteria causing dental caries can be inhibited and prevent or improve dental caries Are reported.

When the proliferation of epithelial cells is promoted by asarinin, salivary secretion becomes active, and it has been found that it can exert an excellent effect on prevention of tooth decay, removal of bad breath, prevention of periodontal disease, and / or treatment.

Accordingly, the inventors of the present invention have continued to investigate substances that can fundamentally prevent the growth of dental caries-inducing bacteria. Thus, the present inventors have found that the asarinin of the present invention is safe and non toxic, and can prevent and treat dental caries, And so on.

The asarinin of the present invention has the formula C ₂ OH ₁₈ O ₆ and the molecular weight is 354.35, which can be represented by the following formula (1).

The asarinin can be obtained from a natural material such as a plant, but the present invention is not limited thereto. The asarinin according to the present invention may be chemically synthesized by a method known in the art, or a commercially available material may be used.

The asarinin of the present invention may exist in unsolvated form as well as solvated form including form of hydrate, ethanol, and the like. The asarinin of the present invention may exist in crystalline or amorphous form, and all such physical forms are included within the scope of the present invention.

The oral composition of the present invention contains 0.001 to 20% by weight, preferably 0.00001 to 10% by weight, and more preferably 0.001 to 5% by weight of asarinin relative to the total weight of the composition.

If the amount of the asarinin is less than 0.000001% by weight, it can not sufficiently achieve the desired therapeutic effect and preventive effect of dental caries, and if it exceeds 20% by weight, , Which may cause problems in the stability of the oral composition.

The oral composition of the present invention may further comprise at least one selected from the group consisting of an abrasive, a wetting agent, a binder, a foaming agent, a sweetener, a flavoring agent, a preservative, a pharmacological agent, an acidity adjusting agent and a brightener.

The abrasive is contained in the oral composition and has a basic cleaning action by polishing. As the abrasive, a second calcium phosphate, precipitated silica, calcium carbonate, hydrated alumina, kaolin, and NaHCO ₃ may be used alone or in combination of two or more. The amount of the abrasive to be used is generally 1 to 60% by weight based on the total weight of the oral composition.

The wetting agent is used for giving stability, sweet taste and slight viscosity of the product. Glycerin, sorbitol solution, amorphous sorbitol solution, propylene glycol, polyethylene glycol, xylitol, etc. may be used alone or in combination of two or more. The amount of such wetting agent to be used is generally 20 to 60% by weight based on the total weight of the oral composition.

Carrageenan, xanthan gum, carboxymethylcellulose sodium, carboxyvinyl polymer, sodium alginate, and laponite may be used alone or in admixture of two or more. The amount of such a binder to be used is generally 0.1 to 3.0% by weight, preferably 0.5 to 2.0% by weight, based on the total weight of the oral composition.

As the foaming agent, anionic surfactant sorbitan fatty acid esters such as sodium lauryl sulfate and sodium lauryl sarcosinate, polyoxyethylene hydrogenated castor oil, polyoxyethylene, polyoxypropylene condensation polymeric substances, etc. may be used alone or in combination with two or more Can be mixed and used. The amount of the foaming agent to be used is generally from 0.5 to 5.0% by weight, preferably from 0.5 to 3.5% by weight, based on the total weight of the oral composition.

The sweetener or fragrance is intended to improve the feeling of use of the product. As the sweetening agent, saccharin sodium, aspartame, licorice acid, etc. may be used singly or in combination of two or more. The amount thereof is generally 0.05 to 0.5% by weight based on the total weight of the oral composition. As such a perfume, an appropriate amount of peppermint oil, spearmint oil, menthol, carboin, etc. may be mixed and used, and an appropriate amount of anise oil is preferably mixed with the mixture.

As the preservative, paraoxybenzoate, sodium benzoate, methyl p-oxybenzoate or the like may be used alone or in combination of two or more.

The acidity adjusting agent is for adjusting the pH of the composition for oral use. As such an acidity adjusting agent, phosphoric acid, sodium phosphate, citric acid, sodium citrate, succinic acid, sodium succinate, tartaric acid and sodium tartrate may be used singly or in combination . The acidity of the oral composition is generally from 5 to 8.

As the brightener, titanium oxide or the like can be used. The amount of the brightener is generally 0.1 to 2% by weight based on the total weight of the oral composition.

Oral compositions may be used as formulations of toothpaste, mouthwash, mouthwash, mouthwash, ointment, chewing gum, ointment, patch or candy. It is also formulated by conventional means known to those skilled in the art to bring the active ingredient into contact with the oral cavity, such as a tooth, and to stick with any plaque or plaque that may be present.

Meanwhile, the present invention can provide a pharmaceutical composition for preventing or treating dental caries including asarinin.

The pharmaceutical composition containing the asarinin may be a solid preparation, a semi-solid preparation or a liquid preparation. Solid preparations include, but are not limited to, powders, granules, tablets, capsules, suppositories, and the like. Solid form preparations may include, but are not limited to, excipients, flavoring agents, binders, preservatives, disintegrants, lubricants, fillers, and the like. Examples of the semi-solid preparation include a cream, a lotion, an emulsifier, a liniment, and the like, but the present invention is not limited thereto, and can be produced by adding a suitable colorant, a flavoring agent, a stabilizer, a tackifier, a surfactant, and the like. Examples of the liquid preparation include water, alcohols, solutions such as solutions of propylene glycol, suspensions, emulsions and the like, but not limited thereto, and they can be prepared by adding appropriate coloring agents, flavoring agents, stabilizers, tackifiers and the like.

For example, powders can be prepared by simple mixing of the pharmaceutically acceptable excipients such as lactose, starch, microcrystalline cellulose and the like with the asarinin of the present invention. The granule is selected from the group consisting of asarinin of the present invention; Suitable excipients which are pharmaceutically acceptable; And a suitable pharmaceutically acceptable binder such as polyvinylpyrrolidone or hydroxypropylcellulose, followed by wet granulation using a solvent such as water, ethanol or isopropanol or dry granulation using a compressive force . Further, the tablet may be prepared by mixing the above granule with a suitable pharmaceutically acceptable salt such as magnesium stearate and then tableting it using a tablet machine. Also, for example, the external preparation for skin may be a pharmaceutically or cosmetically acceptable suitable substance such as vaseline, stearyl alcohol and the like; A suitable pharmaceutically or cosmetically acceptable surfactant such as polysorbate, sorbitan sesquioleate, and the like; Suitable pharmacologically or cosmetically acceptable moisturizing agents such as glycerin; A suitable pharmaceutically or cosmetically acceptable solvent; And a conventional external preparation for skin preparation in which a flavoring agent, a coloring agent, a stabilizer, a tackifier and the like are homogeneously mixed.

In order to attain the object of the dental caries treatment effect according to the present invention, the asarinin of the present invention may be administered at a daily dose of about 0.001 mg / kg to about 150 mg / kg, and about 0.1 mg / kg to about 100 mg / A daily dose is preferred. However, the dosage may vary depending on the route of administration and formulation, the patient's condition (age, sex, weight, etc.), severity of the condition being treated, and the like. For convenience, the total daily dose may be divided as needed and divided into several doses throughout the day.

The composition containing asarinin of the present invention can be used in various applications such as food compositions, pharmaceutical compositions, and quasi-drugs, and is not particularly limited as long as the effect of the present invention can be achieved.

The composition containing asarinin of the present invention improves dental health and ultimately exhibits the therapeutic effect of dental caries.

It exhibits the effect of proliferation of tooth epithelial cells and promotes the secretion of human mucin-7, thereby inhibiting the growth of dental caries-inducing bacteria capable of living in the oral cavity.

It is possible to provide a composition having excellent toxicity and excellent stability while exhibiting excellent dental caries prevention and prevention effects.

FIG. 1 is a graph showing the ratio of human mucin-7 min per asarinin concentration.

Hereinafter, the present invention will be described in more detail with reference to the following examples. 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 above-described embodiments. The embodiments of the present invention are provided by way of example to facilitate a specific understanding of the present invention.

The baicalin used in the following examples of the present invention was purchased from Xian natural field biotechnology Co. Ltd., China.

<Example 1> Epithelial cell proliferation test

The epithelial cell proliferation assay to test the epithelial cell proliferation effect of the present invention was measured by culturing the A-253 epithelial cells (A-253 epithelial cells) present in the oral epithelium. A-253 cells were inoculated into 96-well microplates at a concentration of 1 × 10 ⁴ cells / well and cultured in a CO ₂ incubator at 37 ° C. and 5% concentration for 24 hours. The medium was removed and the cells were washed with wash buffer, Phosphate Buffered Saline (PBS), and serum-free McCoy's 5A Medium, Modified (Asclean 5A Medium, Modified, Gibco) medium for 48 hours.

Cell proliferation was performed using CCK-8 (Cell Counting Kit-8, DOJINDO Laboratories) as follows. After incubation for 1 hour and 30 minutes in a 37 ° C, 5% CO ₂ incubator, the absorbance was measured at 450 nm using an ELISA reader (SPECTRA MAX 190, Molecular Devices) . At this time, to determine the cell proliferation effect of Asarinin, the average value was obtained three times each. Cell proliferation was assessed by the ratio of the absorbance to the control group, but not with asarinin and without serum, 5 μM McCoys, modified. The cell growth of Asarinin is shown in Table 1 below.

Cell proliferation rate by asarinin concentration Test substance Cell proliferation rate (%) Control group 100 1 ppm Asarinin 114.2 10 ppm Asarinin 127.3 20 ppm Asarinin 137.8

Example 2: Promotion of human mucin-7 secretion using A-253 epithelial cells

A-253 epithelial cells were treated with Asarinin, and human mucin-7 secretion promoting effect was measured. A-253 epithelial cells to 24-well microtiter plates (24-well microplate) 2.0 × 10 5 cells / inoculation at a concentration of the well and incubated for 24 hours at 37 ℃, CO ₂ incubator at 5% concentration. The medium was removed and the cells were washed with wash buffer, Phosphate Buffered Saline (PBS), and serum-free McCoy's 5A Medium, Modified, Gibco ) &Lt; / RTI &gt; medium for 24 hours. The supernatant was collected and analyzed for Human Mucin-7 (MUC7). Human Mucin-7 was purchased and assayed using the commercially available Human Mucin-7 ELISA kit (MyBiosource), and the measurement was performed according to the instructions included in the kit. The rate of human mucin-7 production was evaluated by the ratio of the absorbance to the control group added with 5 as the medium containing no asarinin and no serum, modified but modified. Figure 1 shows the results of human mucin-7 min ratio by Asarinin.

From Table 1 and FIG. 1, it can be seen that asarinin promotes epithelial cell proliferation and promotes secretion of human mucin-7.

From the above Examples 1 and 2, it is considered that asarinin promotes the proliferation of epithelial cells and promotes the secretion of human mucin-7, which is an excellent substance for preventing or improving dental caries.

Claims (7)

Wherein the composition contains asarinin as an active ingredient. The oral composition according to claim 1, wherein the oral composition induces A-253 epithelial cell proliferation or promotes human mucin-7 secretion. The oral composition according to claim 1, wherein the composition for oral cavity is for at least one selected from the group consisting of treatment or prevention of dental caries, removal of mouth odor, and treatment or prevention of periodontal disease. The oral composition according to claim 1, wherein the oral composition is for treating or preventing dental caries. The oral composition according to claim 1, wherein the composition for oral cavity comprises 0.001 to 5% by weight of asarinin relative to the total weight of the composition. An oral cleanser comprising an oral composition selected from any one of claims 1 to 5. A medicinal product comprising an oral composition selected from any one of claims 1 to 5.

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