Oral composition containing lipid-soluble extracts of red ginseng

Abstract

The present invention relates to an oral composition, and more specifically, to an oral composition comprising a fat-soluble extract of red ginseng as an active ingredient. The oral composition containing the fat-soluble component of red ginseng according to the present invention has high utility as it exhibits excellent effects in preventing, improving, and treating oral diseases by inhibiting and killing the growth of Streptococcus mutans in dental diseases caused by oral bacteria. Furthermore, the composition of the present invention is characterized by containing a substance derived from natural products and minimizing the use of chemical substances, thereby not causing side effects in the human body.

Description

Technology Field

[0001] The present invention relates to an oral composition, and more specifically, to a composition for preventing, improving, and treating oral diseases by inhibiting the growth of and killing Streptococcus mutans in dental diseases caused by oral bacteria. Background Technology

[0002] Generally, dental caries is a disease caused by microorganisms that occurs when tooth enamel is damaged by acid and biofilms produced as bacteria residing in the mouth decompose residual food, and among the approximately 700 species of oral microorganisms, Streptococcus mutans ( Streptococcus mutans ...is known as one of the representative bacteria that cause tooth decay.

[0003] Streptococcus mutans attaches to the tooth surface to form colonies and utilizes saliva and food components to form a biofilm substrate. It also stabilizes the structure of the biofilm by synthesizing insoluble glucans using sugars present in the oral cavity. Furthermore, Streptococcus mutans performs energy metabolism using carbohydrates and sugars contained in oral food, producing organic acids as byproducts which are released extracellularly, thereby demineralizing the tooth enamel. Through this process, bacteria and metabolites in the biofilm on the tooth surface induce inflammation of the periodontal tissues, and the partial stagnation of organic acids accelerates the demineralization of the teeth, leading to tooth decay.

[0004] Methods to combat cavity-causing bacteria that can reduce the occurrence of cavities include brushing, tartar removal through scaling, and the use of mouthwash, and the regular use of mouthwash helps with oral hygiene.

[0005] Various compounds with antimicrobial activity, such as cetylpyridinium chloride, sodium fluoride, and chlorohexidine, are widely used in mouthwashes. Cetylpyridinium chloride is a quaternary ammonium compound structurally possessing a positive charge and hydrophobic side branches; it is used in many mouthwashes because it binds strongly to the cell walls of negatively charged Gram-positive bacteria, causing cell membrane disruption, cytoplasmic leakage, and inhibition of metabolism and proliferation. Additionally, chlorohexidine is currently known to be the most effective agent for the prevention and treatment of periodontal disease.

[0006] However, while chemical substances are effective in preventing tooth decay, they have problems such as side effects like tissue irritation, discoloration, degeneration, vomiting due to irritating taste and smell, and the emergence of resistant bacteria, as well as, above all, aversion to the chemicals.

[0007] Therefore, there is a need to develop methods to inhibit tooth decay-causing bacteria using ingredients that are more effective, safe, and have fewer side effects.

[0008] Meanwhile, regarding red ginseng—which contains various bioactive components and is used as an ingredient in herbal medicines and health functional foods—and Streptococcus mutans, there are reports that the fat-soluble n-hexane extract of red ginseng marc strongly inhibits the growth of Streptococcus mutans (MIC=0.125 mg / mL) and effectively inhibits bacterial adhesion and biofilm formation. Additionally, it has been reported that the combined use of red ginseng marc n-hexane extract and arginine exhibits a synergistic effect in inhibiting Streptococcus mutans growth, while showing additional effects on biofilm formation and GTase activity inhibition. Although red ginseng marc n-hexane extract is considered to very effectively inhibit the growth of Streptococcus mutans, a representative causative agent of tooth decay, further research on the inactivation of Streptococcus mutans is necessary to utilize red ginseng marc n-hexane extract as a material for preventing tooth decay.

[0009] Therefore, in the present invention, the potential for using red ginseng marc n-hexane extract as an additive to an oral rinse was investigated. In particular, research was conducted to derive a composition that is highly effective in preventing and improving oral diseases by inhibiting the growth and killing Streptococcus mutans, a causative agent of tooth decay, without concerns regarding the aforementioned side effects. Prior art literature

[0010] [Reference 1] Republic of Korea Registered Patent No. 10-1315805 (Title of Invention: Composition for Inhibiting Oral Bacteria Containing Ixeris Extract as an Active Ingredient, Applicant: Industry-Academic Cooperation Foundation of Wonkwang University, Registration Date: October 01, 2013) [Reference 2] Republic of Korea Registered Patent No. 10-2509579 (Title of Invention: Oral Composition Containing Cassava Extract, Applicant: LG Household & Health Care Co., Ltd., Registration Date: March 08, 2023) [Reference 3] Republic of Korea Published Patent No. 10-2003-0085820 (Title of Invention: Oral Composition Containing Aloe and Propolis Extracts, Applicant: Kim Jung Moon Aloe Co., Ltd., Publication Date: November 07, 2003)

[0011] [Reference 1] Kim Dong-cheong et al., Journal of Applied Biological Chemistry 64(2021) 357-362 [Reference 2] Schaeffer LM et al., Journal of Clinical Dentistry 22(2011) 183-186 The problem to be solved

[0012] The present invention aims to provide a composition for preventing, improving, and treating dental diseases through continuous use without causing side effects, based on the results showing that a fat-soluble extract of red ginseng is effective for oral diseases.

[0013] The present invention aims to provide a composition for preventing, improving, and treating dental diseases caused by oral bacteria by inhibiting and killing the growth of Streptococcus mutans. means of solving the problem

[0014] The present invention provides an oral composition comprising a fat-soluble extract of red ginseng as an active ingredient and adding pharmaceutically acceptable excipients, diluents, etc. In the present invention, the composition may be used for the prevention or treatment of oral diseases.

[0015] The fat-soluble extract of red ginseng according to the present invention may be extracted from ginseng and red ginseng processed from ginseng, and it may also be extracted from ginseng marc and red ginseng marc remaining after extracting water-soluble components of ginseng or red ginseng.

[0016] In the red ginseng fat-soluble extract of the present invention, the method for extracting fat-soluble components is not particularly limited and can be extracted according to methods commonly used in the relevant technical field. Examples of extraction methods include solvent extraction, ultrasonic extraction, reflux extraction, and supercritical extraction, and these can be performed individually or in combination of two or more methods, and preferably, the extraction can be performed using solvent extraction.

[0017] The extraction solvent used to prepare the fat-soluble extract of red ginseng in the present invention is not particularly limited to a highly hydrophobic solvent and any hydrophobic solvent known in the art may be used. Examples of extraction solvents for the solvent extraction method include one or more solvents from chloroform, benzene, ethyl acetate, methylene chloride, n-hexane, diethyl ether, cyclohexane, etc., and preferably, n-hexane may be used. In addition, in the case of the supercritical extraction method, carbon dioxide may be used as the extraction solvent.

[0018] In the present invention, the red ginseng fat-soluble extract may be 0.1 to 1.0 weight% based on the total weight of the composition, and preferably 0.1 to 0.5 weight% based on the total weight of the composition. If the red ginseng fat-soluble extract is less than 0.1 weight% based on the total weight of the composition, it may not be effective for oral diseases, and if it is 1 weight% or more, it is not desirable because it is not palatable in the mouth when used.

[0019] In addition to the above-mentioned fat-soluble extract of red ginseng, the oral composition of the present invention may further include, depending on the formulation and purpose, conventional ingredients such as an active ingredient, humectant, abrasive, sweetener, pH adjuster, preservative, binder, flavoring, foaming agent, etc.

[0020] As active ingredients, cetylpyridinium chloride, fluoride compounds (sodium fluoride, sodium fluorophosphate, tin fluoride, etc.), chlorhexidine, aminocaproic acid, zinc chloride, pyridoxine hydrochloride, tocopherol acetate, enzymes, etc. may be used alone or in a mixture of two or more.

[0021] As a humectant, glycerin, aqueous solution of sorbitol, polyethylene glycol, propylene glycol, etc. are used alone or in combination, and the amount used may be 1 to 80 weight percent of the total weight of the oral composition.

[0022] Abrasives may be used alone or in combination from among precipitated silica, silica gel, zirconium silicate, calcium phosphate, calcium carbonate, calcium bicarbonate, hydrated alumina, calcium pyrophosphate, insoluble metaphosphate, aluminum silicate, etc., and the amount used may be 1 to 70 weight percent relative to the total weight of the oral composition. In addition, additives used in small amounts may include commonly used ingredients such as sweeteners, pH adjusters, preservatives, coloring agents, and binders.

[0023] Carboxymethylcellulose, carrageenan, xanthan gum, alginic acid, etc. may be used as binders, and the amount of binder used is generally 0.1 to 3 weight% of the total weight of the oral composition. As foaming agents, anionic and nonionic surfactants such as sodium alkyl sulfate, sodium lauryl sulfate, sucrose fatty acid ester, and sorbitan fatty acid ester may be used alone or in a mixture of two or more types, and the amount of foaming agent used is generally 0.5 to 5 weight% of the total weight of the oral composition.

[0024] Saccharin, xylitol, erythritol, aspartame, acesulfame potassium, sucralose, etc. may be used as sweeteners, and the amount of sweetener used is generally 0.01 to 2 weight percent relative to the total weight of the oral composition.

[0025] Sodium phosphate, disodium phosphate, citric acid, triethanolamine, etc., can be used as pH adjusters.

[0026] Benzoic acid, sodium benzoate, methylparaben, propylparaben, etc. can be used as preservatives. As flavorings, peppermint oil, spearmint oil, menthol, etc. may be mixed and used, and enzymes such as dextranase may be used.

[0027] In addition, it includes the remaining amount of water.

[0028] The oral composition according to the present invention, comprising a fat-soluble extract of red ginseng, is an oral composition that can be included in all products generally manufactured and marketed for oral health, and there are no limitations on the oral products to which it is applied. For example, it includes, but is not limited to, toothpaste, mouthwash, oral spray, oral ointment, mouthwash, gargling product, gum, etc. The oral products of the present invention may be in the form of a liquid, solid, suspension, gel, or aerosol, but are not limited thereto. Effects of the invention

[0029] The oral composition containing the red ginseng fat-soluble extract of the present invention has excellent effects in preventing or treating oral diseases.

[0030] The composition containing the red ginseng fat-soluble extract of the present invention has an excellent effect of inhibiting the growth and killing Streptococcus mutans.

[0031] The composition of the present invention is a naturally derived substance that is non-toxic and does not cause side effects when applied to the human body, making it highly versatile. Specific details for implementing the invention

[0032] Hereinafter, the present invention will be described in detail through examples and the like to aid in understanding. The embodiments described in the specification do not represent all technical concepts of the present invention and may be modified in various other forms; therefore, the scope of the present invention should not be interpreted as being limited to the embodiments below. The embodiments of the present invention are provided to more completely explain the present invention to those with average knowledge in the art.

[0033] Experiment preparation

[0034] Preparation of red ginseng fat-soluble extract

[0035] To prepare the red ginseng fat-soluble extract to be used in this experimental example, 10 times (w / w) of the red ginseng marc was added to the ground red ginseng marc powder. n - Add n-hexane and extract in a constant temperature shaking bath for 4 hours, then filter the extract through Whatman No. 2 filter paper and concentrate under reduced pressure at 50°C. n A concentrate with hexane removed was obtained, and the yield was 0.65%. The fat-soluble extract of red ginseng marc was dissolved in DMSO and stored in a freezer for use.

[0036] Strain and culture preparation

[0037] The strain used in this experiment is Streptococcus mutans mutans) KCTC (Korea Biotechnology Research Institute Biological Resource Center) 3085, was inoculated into Brain Heart Infusion (BHI, Difco, USA) medium and cultured in a 37℃ incubator for 24 hours.

[0038] Measurement of Streptococcus mutans killing effect

[0039] The degree of inactivation of Streptococcus mutans according to treatment conditions under oral rinse usage conditions was measured as follows. Streptococcus mutans culture (approx. 1 x 10⁶) cultured in BHI medium (37°C, 24 hours). 6 1 mL of CFU / mL was placed in a sterile microtube and centrifuged (3,000 xg, 5 min, 4°C) to recover the cells, which were then washed twice with sterile phosphate-buffered saline (PBS) to prepare the microbial cells. 1 mL of the pre-prepared sample was added to a microtube containing Streptococcus mutans cells and treated for 30 seconds. The sample was then immediately centrifuged (3,000 xg, 2 min, 4°C) to remove the supernatant, washed twice with sterile PBS, and the pellet was resuspended in 1 mL of sterile PBS. The suspension was diluted by the decimal method, plated onto BHI agar medium, and incubated at 37°C for 24 hours. The resulting colonies were counted, and the viable cell count was calculated as colony forming unit (CFU) / mL for comparison. The inactivation effect of the sample was calculated using the following formula.

[0040] Kill rate (%) = (Number of viable cells in control group - Number of viable cells in sample) / Number of viable cells in control group * 100

[0041] Statistical processing

[0042] The significance of the experimental results is p With <0.05 as the limit t Verification was performed using the t-test, and the experimental results were expressed as mean ± standard deviation.

[0043] (Comparative Example 1)

[0044] The effect of treatment with cetylpyridinium chloride, used as an active ingredient in oral rinses, on the inactivation of Streptococcus mutans was investigated. Streptococcus mutans prepared by washing with sterile PBS were treated with cetylpyridinium chloride at concentrations of 0.1–0.75 mg / mL. Measurement of Streptococcus mutans killing effect Treatment was performed according to the method, the viable cell count was measured, and the results were expressed as the inactivation rate. Sterile PBS solution was used as a control. The results are shown in Table 1 below. The inactivation rate of Streptococcus mutans increased in proportion to the treatment concentration of cetylpyridinium chloride.

[0045] Cetylpyridinium chloride concentration (mg / mL) Streptococcus mutans mortality rate (%) 0 0 0.1 24.63±11.3 0.2 48.43±10.75 0.4 64.80±3.13 0.75 87.75±4.62

[0046] (Comparative Example 2)

[0047] The effect of treatment with sodium fluoride, used as an active ingredient in oral rinses, on the inactivation of Streptococcus mutans was investigated. Streptococcus mutans prepared by washing with sterile PBS were treated with sodium boroate at concentrations of 0.5–1.0 mg / mL... Measurement of Streptococcus mutans killing effect Treatment was performed according to the method, the viable cell count was measured, and the results were expressed as the inactivation rate. Sterile PBS solution was used as a control. The results are shown in Table 2 below. Sodium fluoride had a very minimal inactivating effect on Streptococcus mutans.

[0048] Sodium fluoride concentration (mg / mL) Streptococcus mutans mortality rate (%) 0 0 0.5 6.09±1.53 1.0 6.38±0.29

[0049] (Experimental Example 1)

[0050] The effect of treatment with the fat-soluble extract of red ginseng, the active ingredient of the present invention, on the inactivation of Streptococcus mutans was investigated. Streptococcus mutans prepared by washing with sterile PBS was treated with the fat-soluble extract of red ginseng at a concentration of 0.1–0.2 mg / mL. Measurement of Streptococcus mutans killing effect Treatment was performed according to the method, the viable cell count was measured, and the results were expressed as the inactivation rate. Sterile DMSO was used as a control. The results are shown in Table 3 below. At concentrations of 0.5 mg / mL or higher, the inactivation rate of Streptococcus mutans was similar for the red ginseng fat-soluble extract.

[0051] Red ginseng fat-soluble extract concentration (mg / mL) Streptococcus mutans mortality rate (%) 0 0 0.1 15.61±3.30 0.5 25.90±9.26 1.0 27.72±3.28 2.0 23.83±1.99

[0053] (Experimental Example 2)

[0054] To enhance the killing effect of the red ginseng fat-soluble extract, which is the active ingredient of the present invention, on Streptococcus mutans, the red ginseng fat-soluble extract and cetylpyridinium chloride were mixed and treated. Streptococcus mutans prepared by washing with sterile PBS were treated in the same manner as in Experimental Example 1 under conditions where cetylpyridinium chloride was mixed with red ginseng fat-soluble extract at a concentration of 0.5 to 2.0 mg / mL, and the results are shown in Table 4 below. Under the condition where red ginseng fat-soluble extract was mixed with cetylpyridinium chloride at a concentration of 1.0 mg / mL or higher, the killing rate of Streptococcus mutans was significantly increased compared to the condition where cetylpyridinium chloride was treated with 0.1 mg / mL.

[0055] Cetylpyridinium chloride concentration (mg / mL) Red ginseng fat-soluble extract concentration (mg / mL) Streptococcus mutans mortality rate (%) 0.1 0 27.79±5.11 0.1 0.5 31.71±5.27 0.1 1.0 56.88±18.63* 0.1 2.0 52.95±9.82*

[0057] (Experimental Example 3)

[0058] To enhance the killing effect of the red ginseng fat-soluble extract, which is the active ingredient of the present invention, on Streptococcus mutans, the red ginseng fat-soluble extract was mixed with cetylpyridinium chloride and sodium fluoride and treated. Streptococcus mutans prepared by washing with sterile PBS was treated in the same manner as in Experimental Example 1 under conditions where 0.1 mg / mL of cetylpyridinium chloride and 1.0 mg / mL of red ginseng fat-soluble extract were mixed with sodium fluoride at a concentration of 0.5 to 1.0 mg / mL, and the results are shown in Table 5 below. Under the condition where 0.1 mg / mL of cetylpyridinium chloride and 1.0 mg / mL of red ginseng fat-soluble extract were mixed with sodium fluoride at a concentration of 0.5 mg / mL or higher, the killing rate of Streptococcus mutans increased significantly compared to the condition where only 0.1 mg / mL of cetylpyridinium chloride was used.

[0059] Cetylpyridinium chloride concentration (mg / mL) Red ginseng fat-soluble extract concentration (mg / mL) Sodium fluoride concentration (mg / mL) Streptococcus mutans mortality rate (%) 0.1 0 0 27.79±5.11 0.1 0 0.5 49.0±2.59* 0.1 1.0 0.5 58.15±3.02* 0.1 0 1.0 51.80±6.35* 0.1 1.0 1.0 59.14±4.44*

[0061] (Experimental Example 4)

[0062] To enhance the killing effect of the red ginseng fat-soluble extract, which is the active ingredient of the present invention, on Streptococcus mutans, the red ginseng fat-soluble extract was mixed with cetylpyridinium chloride and sodium fluoride and treated. Streptococcus mutans prepared by washing with sterile PBS was treated in the same manner as in Experimental Example 1 under conditions where 0.1 mg / mL of cetylpyridinium chloride and 2.0 mg / mL of red ginseng fat-soluble extract were mixed with sodium fluoride at a concentration of 0.5 to 1.0 mg / mL, and the results are shown in Table 6 below. Under the condition where 0.1 mg / mL of cetylpyridinium chloride and 2.0 mg / mL of red ginseng fat-soluble extract were mixed with sodium fluoride at a concentration of 0.5 mg / mL or higher, the killing rate of Streptococcus mutans increased significantly compared to the condition treated with 0.1 mg / mL of cetylpyridinium chloride, and the degree was similar to the result of treatment with 0.7 mg / mL of cetylpyridinium chloride.

[0063] Cetylpyridinium chloride concentration (mg / mL) Red ginseng fat-soluble extract concentration (mg / mL) Sodium fluoride concentration (mg / mL) Streptococcus mutans mortality rate (%) 0.1 0 0 27.79±5.11 0.1 2.0 0.5 69.45±4.25* 0.1 2.0 1.0 73.75±3.28*

[0065] As shown in the experimental and comparative examples above, the composition of the present invention is effective in preventing tooth decay but has problems such as tissue irritation, discoloration, denaturation, vomiting due to irritating taste and smell, and the emergence of resistant bacteria, as well as aversion to chemical substances. By minimizing the amount of chemical substances used and using a fat-soluble extract of red ginseng, it was confirmed that the composition has an excellent effect in killing the growth of Streptococcus mutans. Accordingly, the oral composition containing the fat-soluble extract of red ginseng of the present invention has excellent effects in preventing or treating oral diseases.

Claims

Claim 1 It contains red ginseng fat-soluble extract as an active ingredient, and Streptococcus mutans ( Streptococcus mutans An oral composition for the prevention or treatment of oral diseases, characterized by having the efficacy to inhibit the growth and kill ) Claim 2 An oral composition according to claim 1, characterized in that, in addition to the red ginseng fat-soluble extract, cetylpyridinium chloride, sodium fluoride, or a mixture of cetylpyridinium chloride and sodium fluoride is included. Claim 3 An oral composition according to claim 1 or 2, characterized in that the red ginseng fat-soluble extract is 0.1 to 1.0 weight% based on the total weight of the composition. Claim 4 In paragraph 1 or 2, the red ginseng fat-soluble extract is of red ginseng marc n - An oral composition characterized by being a hexane extract.

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