Composition for oral cavity containing herbal extracts

Abstract

The present invention relates to an oral composition comprising a citrus extract as an active ingredient. The oral composition of the present invention exhibits excellent antibacterial and anti-inflammatory effects against oral harmful bacteria (P. gingivalis), thereby providing a preventive effect against tooth decay, periodontal disease, gingivitis, etc.

Description

Technology Field

[0001] The present invention relates to an oral composition having excellent antibacterial and anti-inflammatory effects against harmful oral bacteria. Background Technology

[0003] Generally, major diseases affecting the teeth and surrounding tissues include dental caries and periodontal disease. While the causes of dental caries are diverse, it is known to be caused by plaque (or dental biofilm), which consists of bacteria residing in the oral cavity and their metabolic products; similarly, the cause of periodontal disease is understood to be the metabolic habitation and activity of specific bacteria inhabiting the teeth and gums.

[0004] Specifically, periodontal disease is caused by a mixed infection of several types of bacteria present in plaque, resulting in the progression of inflammation due to the reaction of the tissues surrounding the teeth.

[0005] Therefore, to prevent tooth decay and gum disease, it is necessary to inhibit the growth of oral bacteria or to sterilize them. Substances with this function include antibiotics such as penicillin, erythromycin, tetracycline, and spiramycin, and triclosan, a non-ionic disinfectant, is the most representative. Korean Patent 1999-0079220 presents an oral composition using triclosan.

[0006] However, there are concerns regarding side effects of these antibiotics, such as the emergence of resistant bacteria, hypersensitivity reactions, and gastrointestinal disorders. In particular, antimicrobial agents such as chlorhexidine are known to have the effect of inhibiting tooth formation, but they are also known to have side effects such as the destruction of the oral ecosystem and tooth discoloration.

[0007] Recently, research on antibacterial and disinfectant agents utilizing natural ingredients has been actively conducted as agents capable of minimizing or complementing the side effects exhibited by these existing chemical agents. However, when components extracted from a single herbal medicine are used, while the inhibitory effect on general plaque bacteria is observed to a certain level, most have shown weak levels regarding inflammation-relieving effects, and in particular, regarding Porphyromonas gingivalis, a major harmful oral bacterium ( Porphyromonas gingivalis , below, " P. gingivalis" Research is required on ingredients that can exhibit excellent antibacterial and anti-inflammatory effects against (also denoted as ). Prior art literature

[0009] 1. Republic of Korea Published Patent Application No. 1999-0079220 The problem to be solved

[0010] The objective of the present invention is to provide an oral composition utilizing a herbal medicine that is safe for the human body, having excellent antibacterial and anti-inflammatory effects against harmful oral bacteria while being free from the side effects of existing antibacterial ingredients. means of solving the problem

[0012] To achieve the above objective, the present invention provides an oral composition comprising a crust extract as an active ingredient. Effects of the invention

[0014] The oral composition of the present invention exhibits excellent antibacterial and anti-inflammatory effects against harmful oral bacteria, thereby providing a preventive effect against tooth decay, periodontal disease, gingivitis, etc. Brief explanation of the drawing

[0016] FIG. 1 is of the present invention P. gingivalis This is a photo showing the results of an antibacterial activity test against bacteria. Figures 2 and 3 are graphs showing the anti-inflammatory effect of the present invention. Specific details for implementing the invention

[0017] The present invention will be described below. However, it is not limited to the following description, and each component may be modified in various ways or selectively combined as needed. Accordingly, it should be understood that the invention includes all modifications, equivalents, and substitutions that fall within the spirit and scope of the invention.

[0018] The term "extract" as used in this specification has the meaning commonly understood in the art as a crude extract, but in a broader sense, it also includes fractions obtained by further fractionating the extract. That is, the extract used in the present invention includes not only that which is obtained using an extraction solvent, but also that which is obtained by additionally applying a purification process thereto. For example, fractions obtained through various additional purification methods, such as a fraction obtained by passing the extract through an ultrafiltration membrane having a specific molecular weight cut-off value, or separation by various chromatographs (designed for separation based on size, charge, hydrophobicity, or affinity), are also included in the extract of the present invention. Furthermore, the extract used in the present invention may be prepared in a powder state by additional processes such as vacuum distillation, freeze-drying, or spray drying.

[0019] In this specification, the term "containing as an active ingredient" means containing an amount sufficient to achieve the efficacy or activity of the extract described below. The present invention is a composition extracted from natural plant materials, and the quantitative upper limit of the extract of the present invention included in the composition of the present invention may be selected and implemented by a person skilled in the art within an appropriate range.

[0020] In this specification, the term "prevention" refers to any act of suppressing or delaying the progression of oral diseases through the administration of the composition of the present invention.

[0021] Additionally, in this specification, the term "administration" means providing a specific composition of the present invention to an individual by any appropriate method.

[0022] The present invention provides an oral composition comprising a crust extract as an active ingredient.

[0023] Citrus peel, Aurantii Fructus Immaturus ) is a bitter orange tree Citrus aurantium Linnii, Hagyul Citrus natsudaidai It is an unripe (just about to ripen) fruit of Hayata or its cultivated varieties (Rutaceae).

[0024] In the crust extract of the present invention, the method of extracting the crust is not particularly limited and can be extracted according to methods commonly used in the art. Non-limiting examples of the extraction method include solvent extraction, hot water extraction, ultrasonic extraction, filtration, reflux extraction, etc., which may be performed individually or in combination of two or more methods, and specifically, may be performed using solvent extraction.

[0025] The crust extract of the present invention may be extracted by one or more extraction methods selected from ultrasonic extraction, room temperature extraction, hot water extraction, cold maceration extraction, reflux cooling extraction, and steam extraction. Specifically, it may be extracted using hot water.

[0026] In the present invention, the type of extraction solvent used to extract the crust is not particularly limited, and any solvent known in the art may be used. Non-limiting examples of the extraction solvent include one or more solvents selected from the group consisting of water, distilled water, methanol, ethanol, propanol, isopropanol, butanol, acetone, ether, benzene, chloroform, ethyl acetate, methylene chloride, n-hexane, hydrochloric acid, acetic acid, formic acid, citric acid, diethyl ether, and cyclohexane. Specifically, when alcohol is used as a solvent, C1 to C4 alcohols (methanol, ethanol, propanol, butanol) may be used.

[0027] The crust extract of the present invention may be extracted using one or more solvents selected from the group consisting of water, alcohol having 1 to 5 carbon atoms, acetone, ethanol, ethyl acetate, n-hexane, diethyl ether, and cyclohexane.

[0028] Methods such as vacuum concentration and reverse osmosis concentration may be used for concentrating the extract. The drying step after concentration includes, but is not limited to, freeze-drying, vacuum drying, hot air drying, spray drying, vacuum drying, foam drying, high-frequency drying, or infrared drying. Depending on the case, a process of grinding the final dried extract may be additionally included, or the drying step may be omitted and the concentrate sterilized to produce a soft extract.

[0029] The crust extract of the present invention may include an extract, a dried powder thereof, or any form formulated using the same, and for example, the extract may be prepared in the form of a dried extract or a soft extract, or in the form of an extract acid obtained by adding a suitable excipient, but is not limited thereto.

[0030] The term "dried extract" in this invention refers to a preparation prepared by adding a suitable extractant to a raw herbal medicine, extracting it for a certain period of time according to a cold maceration, hot maceration, or percolation method, filtering the extract, and concentrating and drying it by a suitable method.

[0031] In this invention, the term "soft extract" refers to an extract obtained by adding a suitable solvent to a herbal raw material and extracting it for a certain period of time, then concentrating the resulting extract to a consistency similar to corn syrup.

[0032] The above crust extract may preferably be a water extract, i.e., a hot water extract. More specifically, the above crust extract may be a dry crust extract obtained by concentrating the crust after water extraction. Alternatively, it may be a crust extract acid prepared as an acid by mixing a suitable excipient with the obtained dry extract.

[0033] The citrus peel extract of the present invention may be a dried extract obtained by washing the medicinal material (citrus peel) with water and cutting it into appropriate sizes (crushing or slicing), adding 5 to 10 times the amount of distilled water, extracting at 80 to 100°C for 2 to 3 hours, filtering, and concentrating under reduced pressure at 60°C or lower. Alternatively, it may be a citrus peel extract acid prepared as a powder by mixing a suitable excipient with the obtained dried extract.

[0034] The oral composition of the present invention may contain a citrus extract in an amount of 0.01 to 10% by weight relative to the total weight of the oral composition. Specifically, it may contain 0.1 to 8% by weight, and more specifically, 1 to 5% by weight. If the concentration of the extract is less than 0.01% by weight, the antibacterial efficacy is weak, and if it exceeds 10% by weight, there is a problem with poor usability due to the unique taste and aroma of the medicinal material.

[0035] The crust extract of the present invention may include one or more selected from naringin and neohesperidin as indicator components.

[0036] The crust extract of the present invention may contain naringin as an indicator component in an amount of 7% by weight or more relative to the total weight of the crust extract. Specifically, it may contain 10% by weight or 15% by weight or more.

[0037] The crust extract of the present invention may contain 3% by weight or more of neohesperidin as an indicator component relative to the total weight of the crust extract. Specifically, it may contain 5% by weight or 10% by weight or more.

[0038] The oral composition of the present invention may be a composition for the prevention, improvement, or treatment of oral diseases.

[0039] The above oral disease is characterized by being selected from the group consisting of bad breath, tooth decay, stomatitis, dental caries, periodontal disease, gingivitis, oral mucosal ulcers, and xerostomia. For example, the above oral disease may refer to tooth decay and periodontal disease.

[0040] The above "bad breath" refers to an odor originating from the mouth, caused by oral bacteria ( P.gingivalis , T.denticola , Fusobacterium sp., P.intermedia , Eubacterium It is primarily caused by volatile sulfur compounds (VSC), which are gases produced during the process of bacteria breaking down proteins in the mouth, and the proteins that serve as nutrients for bacteria mainly originate from food debris, saliva, and sloughed-off oral mucosal cells.

[0041] The term "stomatitis" above refers collectively to inflammatory diseases in the oral cavity accompanied by pain. Although there are various classification methods for stomatitis based on symptoms, affected area, cause, and physical examination findings, it is difficult to apply them uniformly to each disease. Generally, stomatitis is divided into ulcerative stomatitis, vesicular stomatitis, and erosive stomatitis.

[0042] The aforementioned "dental cavities" is an infectious disease caused by bacteria inhabiting the surface of the teeth; also known as tooth decay, it manifests as the erosion and loss of the hard tissues of the teeth. Specifically, the milky-white, translucent, and hard substance that covers the surface of the crown of the tooth and protects the dentin is called dental enamel. Tooth decay refers to the formation of cavities when the enamel is damaged by acids produced as sugars and starches are broken down by oral pathogens residing in the mouth. A major cause of dental caries is dental plaque, a bacterial film formed on the tooth surface; saliva forms a thin, sticky film on the teeth, and on this, Streptococcus sobrinus, a type of streptococcus ( Streptococcus sobrinus ) bacteria and Streptococcus mutans ( Streptococcus mutans Dental plaque is formed when oral microorganisms such as ) attach and form a biofilm, and Fusobacterium ( Fusobacterium It becomes thicker due to ).

[0043] The aforementioned periodontal disease is a chronic, infectious disease (an inflammatory disease accompanied by alveolar bone resorption) in which tissue destruction occurs due to a host response resulting from the deposition of bacterial plaque within periodontal tissues. The causative factors of this periodontal disease cannot be explained by a single cause alone and are generally considered to be chronic diseases resulting from complex causes. Commonly referred to as gum disease, it is classified into gingivitis and periodontitis depending on the severity of the condition. Gingivitis refers to a relatively mild and rapidly recovering form of periodontal disease confined to the gums, or soft tissues, while periodontitis refers to cases where this inflammation has progressed to the gums and surrounding alveolar bone.

[0044] The above "gingivitis" refers to bacteria present in the subgingival plaque, for example, Streptococcus ( Streptococcus ) genus, Porphyromonas( Porphyromonas It is an oral disease in which bacteria of the genus, etc., cause infection in the soft tissues of the gingiva when suitable growth conditions are formed, leading to periodontal disease such as gingivitis or periodontitis, and causing inflammation of the gums.

[0045] The above "xerostomia" is a condition in which the oral mucosa becomes dry due to a decrease in the secretion of saliva. It can be caused by systemic factors such as Sjögren's syndrome, anemia, diabetes, nutrient deficiencies, and aging, or by the use of medications or neurological disorders. Patients mainly complain of abnormalities in chewing and speech functions, and severe bad breath and tooth decay occur. Depending on the severity, patients may suffer from severe pain due to burning sensations or ulcers on the oral mucosa.

[0046] Although several species of pathogenic microorganisms are known to reside in the oral cavity and cause cavities and periodontal disease, among them Streptococcus mutans ( Streptococcus mutans ) and Porphyromonas gingivalis ( P. gingivalis ) is known to be the main pathogen causing tooth decay and periodontitis [Liliemark WF, Crit. Rev. Oral Bio. Med. , 7:180~198, 1996].

[0047] Pathogenic microorganisms in the oral cavity secrete an enzyme called glucosyltransferase (GTA) from outside the cell or from the surface, using sucrose in food as a substrate to produce glucose and fructose, while simultaneously forming insoluble glucan, a polymer of glucose, on the tooth surface. Other microorganisms attach to the formed glucan, forming a bacterial film, or dental plaque. Within this plaque, lactic acid bacteria proliferate and produce lactic acid using fructose as a carbon source; this lactic acid is trapped and concentrated in the attached glucan, and this high concentration of acid causes Ca2+ from calcium phosphate, a component of teeth, to dissolve the enamel, the outer layer of the tooth, thereby causing tooth decay [Sigmund, SS, et al. J.Periodontol ., 63:322-331,1992].

[0048] Furthermore, oral pathogenic microorganisms form plaque, a bacterial film, on the tooth surface, and as lactic acid produced by lactic acid bacteria proliferating within the plaque accumulates at high concentrations, calcium ions (Ca 2+ The enamel is lost. As a result, tooth decay is induced along with the dissolution of the outer enamel layer of the tooth, and toxic substances from plaque seep into the crevice between the tooth and gum, causing an intracellular inflammatory response, which leads to periodontal diseases such as gingivitis and periodontitis.

[0049] Bacterial antigens, represented by endotoxins or lipopolysaccharides (LPS) released from plaque, invade the gingival tissue. Neutrophils and macrophages induced by this invasion become activated by phagocytizing these antigens, releasing enzymes such as collagenase, gelatinase, elastase, and Cathepsin G extracellularly. These enzymes act cooperatively to break down organic components of the gingival tissue, such as collagen and proteoglycans.

[0050] Meanwhile, neutrophils or macrophages release inflammatory cytokines and stimulate surrounding gingival fibroblasts to promote the production of matrix metalloproteinases (MMPs); however, since the production of TIMPs (tissue inhibitors of metalloproteases), which are inhibitors of these enzymes, remains almost unchanged or is even inhibited, the matrix (collagen) is degraded. Consequently, softening and disintegration of gingival tissue, as well as persistent bleeding, occur. Porphyromonas gingivalis, which is distributed in plaque as a major supplier of enzymes involved in collagen degradation ( P. gingivalis Periodontal disease-causing bacteria such as collagenase and trypsin-like proteolytic enzymes can be cited. These bacteria secrete collagenase and trypsin-like proteolytic enzymes, and connective tissues such as collagen and fibronectin are broken down by these enzymes.

[0051] In addition, bacterial enzymes exhibit MMP activity by activating inactive precursors or degrading TIMP. Proteoglycans in periodontal tissues can be degraded by various bacterial enzymes, and macromolecules such as collagen, proteoglycans, and hyaluronic acid are also destroyed by normal cellular metabolites such as free radicals.

[0052] The above oral composition is, among the aforementioned oral harmful bacteria, Porphyromonas gingivalis ( P. gingivalis It exhibits excellent antibacterial and anti-inflammatory effects against ).

[0053] Porphyromonas gingivalis, belonging to the red complex P. gingivalis ...is known as the most important causative bacterium of periodontal disease.

[0054] Porphyromonas gingivalis ( P. gingivalis Gram-negative anaerobic bacteria increase in number in the lesions of patients with periodontal disease, and Porphyromonas gingivalis, which infiltrates the sullary epithelium as the disease progresses, is also frequently found. While Porphyromonas gingivalis directly damages periodontal tissues by producing metabolites or toxins during the process of attaching to or infiltrating host tissues and cells, it further destroys periodontal tissues through cytokines produced by cells that react with the bacteria, as well as substances produced by host cells that respond to these cytokines. In other words, periodontal disease is caused by Porphyromonas gingivalis and is accompanied by inflammation and bleeding; in severe cases, it may require the use of dentures following tooth extraction.

[0056] According to one embodiment of the present invention, the citrus extract is a major pathogen of periodontal disease, Streptococcus mutans ( Streptococcus mutans ), Porphyromonas gingivalis( P. gingivalis As the growth inhibitory activity of ) was confirmed, it is determined that the composition according to the present invention is effective in preventing or treating oral diseases by inhibiting the proliferation of pathogens that cause oral diseases.

[0058] The oral composition of the present invention can be formulated into toothpaste, chewing gum, mouthwash, mouthwash, oral spray, oral ointment, or oral patch.

[0059] In addition, the oral composition of the present invention may be formulated as an extract powder. The "extract powder" is a preparation made into a powder or fine particle by adding suitable additives such as excipients, binders, or disintegrants to a pharmaceutical product such as an extract, either as is or by adding appropriate additives.

[0060] The oral composition of the present invention may further include one or more selected from the group consisting of fluoride compounds, abrasives, humectants, sweeteners, active ingredients, foaming agents, binders, flavoring agents, pH adjusters, foaming agents, and binders.

[0061] The above fluoride compound acts to prevent tooth decay by increasing the acid resistance of teeth, and one or more of sodium fluoride, sodium monofluorophosphate, and tin fluoride may be used, and the content thereof is preferably, for example, 0.01 to 2.0 weight%.

[0062] The above abrasive may be used alone or in a mixture of two or more types, such as precipitated silica, calcium carbonate, hydrated alumina, calcium monohydrogen phosphate, and sodium bicarbonate, and the content thereof is preferably 10 to 60 weight percent.

[0063] As the above wetting agent, amorphous sorbitol solution, glycerin, propylene glycol, polyethylene glycol, etc., may be used alone or in a mixture of two or more types, and the content thereof is preferably 3 to 60 weight%.

[0064] The above sweeteners include sodium saccharin, xylitol, erythritol, stevia, aspartame, etc., and may be used alone or in a mixture of two or more types, and the content is preferably 0.01 to 2 weight%.

[0065] As the above binder, one or more types of organic binders such as carrageenan, various thickening cellulose derivatives, gums such as xanthan gum and tragacanth gum, synthetic polymer derivatives such as polyvinyl alcohol, sodium polyacrylate, polyacrylic acid / maleic acid copolymer, and carboxyvinyl polymer, and inorganic binders such as silica and laponite may be selected and mixed in appropriate amounts.

[0066] The above flavoring agent may be used by mixing an appropriate amount of peppermint oil, spearmint oil, menthol, etc. As a preservative, an appropriate amount of methylparaben, propylparaben, etc. may be used by mixing.

[0067] As the above pH adjuster, sodium triphosphate, sodium monophosphate, citric acid, sodium citrate, phosphoric acid, tartaric acid, sodium tartrate, etc., may be used, and the preferred pH is 5 to 8. As a pigment, gardenia blue pigment, gardenia yellow pigment, Blue No. 1, Yellow No. 203, titanium oxide, etc., may be used by mixing an appropriate amount.

[0068] For example, when the oral composition of the present invention is applied to a toothpaste formulation, it may further include a fluoride compound, an abrasive, a humectant, a sweetener, a flavoring agent, etc.

[0069] The above foaming agent may be used alone or in a mixture of two or more types, such as sodium lauryl sulfate, sodium lauryl sarcosinate, cocamidopropyl betaine, polyoxyethylene hardened castor oil, polyoxyethylene polyoxypropylene-based condensation polymer, etc., and the content thereof is preferably 0.5 to 5 weight%.

[0070] As the above binder, carrageenan, xanthan gum, sodium carboxymethylcellulose, polyvinylpyrrolidone, etc., may be used alone or in a mixture of two or more types, and the content thereof is preferably 0.1 to 5 weight%.

[0072] Meanwhile, in the oral composition of the present invention, fragrances such as menthol, anethol, eugenol, limonene, ocimene, n-dodecyl alcohol, citronenol, α-terpineol, methyl salicylate, methyl acetate, citronelyl acetate, cineol, linalool, ethyl linalool, vanillin, thymol, spearmint oil, sage oil, rosemary oil, and cinnamon oil may be used alone or in combination in an amount of 0.1-10%, preferably 0.5-5%, of the total composition. there is.

[0073] In the oral composition of the present invention, one or more of various active ingredients may be selected and combined, such as cationic disinfectants like triclosan, chlorhexidine, benzethonium chloride, benzalkonium chloride, and cetylpyridium chloride; alkali metal monofluorophosphates like sodium monofluorophosphate and potassium monofluorophosphate; fluorides such as sodium fluoride and stannous fluoride; tranexamic acid; epsilon-aminocaproic acid; aluminum chlorohydroxyl-alantoin; dihydrocholestanol; glycerolytic acids; glycerophosphate; sodium chloride; water-soluble inorganic phosphate compounds; ascorbic acid (sodium); dl-α-tocopherol acetate; xylitol; pyridoxine hydrochloride; and polyvinylpyrrolidone.

[0074] In addition, anionic surfactants, nonionic surfactants and / or cationic surfactants may be used as the foaming component in the oral composition of the present invention. Here, as an anionic surfactant, sodium alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, sodium N-acyl sarcosinate such as sodium N-lauroyl sarcosinate and sodium N-miristyl sarcosinate can be used, and as a nonionic surfactant, sugar-derived fatty acid esters such as sugar fatty acid esters, maltose fatty acid esters, and lactose fatty acid esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene higher alcohol ethers, polyoxyethylene polyoxypropylene copolymers, and polyoxyethylene polypropylene fatty acid esters can be used. As cationic surfactants, N-alkyldiaminoethylglycine such as N-lauryl diaminoethylglycine and N-myristyl diaminoethylglycine, N-alkyl-N-carboxymethylammonium betaine, and 2-alkyl-1-hydroxyethylimidazoline betaine sodium may be used. In this case, anionic surfactants are mainly used as foaming components, and sodium alkyl sulfates such as sodium lauryl sulfate are the most widely used representative examples. In addition, these surfactants are used either individually or in a mixture of two or more types, and the amount used is typically 0.01-5% of the total composition, more preferably 0.02-3%.

[0076] Meanwhile, the present invention provides a pharmaceutical composition for the prevention, improvement, or treatment of oral diseases comprising the oral composition described above.

[0077] When preparing a pharmaceutical composition of the present invention, it may be prepared by comprising (a) a pharmaceutically effective amount of the citrus extract of the present invention described above; and (b) a pharmaceutically acceptable carrier. The term 'pharmaceutically effective amount' means an amount sufficient to achieve the efficacy or activity of the extract described above.

[0078] At this time, the above pharmaceutically acceptable carrier is one that is commonly used in formulations and includes, but is not limited to, lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia gum, calcium phosphate, alginate, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methyl hydroxybenzoate, propyl hydroxybenzoate, talc, magnesium stearate, and mineral oil.

[0079] The pharmaceutical composition of the present invention may additionally include, in addition to the above components, lubricants, wetting agents, sweeteners, flavoring agents, emulsifiers, suspending agents, preservatives, etc. Suitable pharmaceutically acceptable carriers and formulations are described in detail in Remington's Pharmaceutical Sciences (19th ed., 1995).

[0080] In addition, the pharmaceutical composition of the present invention may be administered orally or parenterally. In this case, the appropriate dosage of the pharmaceutical composition of the present invention may be prescribed in various ways depending on factors such as the formulation method, mode of administration, patient's age, body weight, sex, pathological condition, food, time of administration, route of administration, excretion rate, and response sensitivity. The general dosage of the pharmaceutical composition of the present invention is within the range of 0.001 to 100 mg / kg for adults.

[0081] Although not specifically limited, the pharmaceutical composition of the present invention may be prepared in a unit volume form or contained in a multi-volume container by formulation using pharmaceutically acceptable carriers and / or excipients according to methods that can be easily practiced by a person skilled in the art to which the invention belongs. In this case, the formulation may be in the form of a solution, suspension, syrup, or emulsion in an oil or aqueous medium, or may be in the form of an extract, powder, powder, granule, tablet, or capsule, and may additionally include a dispersant or a stabilizer.

[0083] In addition, the present invention provides a functional food composition comprising the oral composition described above.

[0084] As another embodiment of the present invention, the present invention relates to a food composition for the prevention or improvement of oral diseases comprising a persimmon extract as an active ingredient. The oral diseases are characterized by being selected from the group consisting of bad breath, tooth decay, stomatitis, dental caries, periodontal disease, gingivitis, oral mucosal ulcers, and xerostomia. Preferably, the oral diseases may refer to tooth decay and periodontal disease.

[0085] A food composition for the prevention or improvement of oral diseases comprises a citrus extract as an active ingredient, similar to the pharmaceutical composition for the prevention or treatment of oral diseases described above. The description of the extract is the same or similar as that described in the pharmaceutical composition.

[0086] The above food composition refers to a natural product or processed product containing one or more nutrients, preferably one that has undergone a certain degree of processing to become ready for direct consumption, and in the conventional sense includes health functional foods, beverages, food additives, and beverage additives.

[0087] Specifically, the food composition may include not only the crust extract as an active ingredient, but also ingredients that are typically added during food manufacturing. For example, it may include proteins, carbohydrates, fats, nutrients, seasonings, and flavoring agents. Examples of the carbohydrates mentioned above include monosaccharides, e.g., glucose, fructose, etc.; disaccharides, e.g., maltose, sucrose, oligosaccharides, etc.; and polysaccharides, such as dextrin, cyclodextrin, etc., which are common sugars, and sugar alcohols such as xylitol, sorbitol, erythritol, etc. As flavoring agents, natural flavoring agents [taumatin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.)] and synthetic flavoring agents (saccharin, aspartame, etc.) may be used.

[0088] In addition, when the food composition of the present invention is prepared as a drink, in addition to the extract of the present invention, citric acid, liquid fructose, sugar, glucose, acetic acid, malic acid, fruit juice, Eucommia ulmoides extract, jujube extract, licorice extract, etc. may be additionally included.

[0090] The present invention will be explained in more detail below through examples and comparative examples. This is for the purpose of explaining the invention only, and the scope of the invention is not limited thereby.

[0092] <Preparation of Example>

[0094] The crust extract (Example 1) and crust extract acid (Example 2) of the present invention were prepared through the following method.

[0095] Specifically, 10 kg of dried crusts were selected and prepared in a coarse-cut manner according to the fineness and powdering standards of the General Principles of the Pharmacopoeia. Five times the amount of water was added, and the mixture was extracted at 80°C for 2 hours. The filtered liquid was then concentrated under reduced pressure at 60°C or below, and subsequently dried and ground to obtain 1 kg of dried crust extract (dried extract). An excipient (maltodextrin) was added to this to prepare a powder sample of the crust extract according to the method for preparing powders. The above extract contains 6.5 wt% as naringin and 3.1 wt% as neohesperidin as minimum values.

[0097] <Experimental Example 1>

[0098] 1) Oral harmful bacteria of crust extract ( P. gingivalis Antimicrobial activity test for ) Experimental method (disk diffusion method)

[0099] ① Porphyromonas gingivalis ( P. gingivalis The strain was inoculated into 5 mL of liquid culture medium and cultured for 2 to 7 days in a 35°C incubator under each culture condition.

[0100] ② 1×10 bacterial cultures obtained by liquid culture 7 After diluting to a concentration of cfu / mL, the diluted bacterial culture was uniformly spread onto a solid medium using a sterile cotton swab.

[0101] ③ After placing 8 mm paper discs at regular intervals on the solid medium absorbed with bacterial culture solution, 50 µl of each sample (concentration 2,000 µg / ml) was inoculated.

[0102] ④ After culturing in a 37℃ incubator for 168 hours, the diameter of the growth inhibition zone was measured.

[0104] 2) Experimental Results

[0105] Test sample extraction solvent Concentration (µg / ml) P. gingivalis Ring of inhibition diameter (mm) Negative control group (DMSO) - - 8.0 crustal exoskeleton hot water 2,000 9.88 Positive control group (Triclosan) - 200 10.11

[0106] Referring to Table 1 and Figure 1, crustal extract acid at a concentration of 2,000 μg / ml Porphyromonas gingivalis ( P. gingivalisIt can be confirmed that the antibacterial effect against ) was excellent.

[0108] <Experimental Example 2>

[0109] Inhibitory effect of citrus extract on inflammation

[0110] 1×10⁶ gingival progenitor cell lines (HGEPp) in a 12-well plate 5 After inoculating into cells / well, the cells were cultured for 24 hours. After removing growth factors from the cultured cell line using D-PBS, P. gingivalis Membrane fraction and citrus extract samples (concentrations of 100 µg / ml, 200 µg / ml, and 500 µg / ml, respectively) were treated, respectively. After 24 hours of incubation, the culture medium was collected, and the expression levels of the inflammatory mediators IL-1α and IL-8 were determined using an immunoassay kit. The expression levels of IL-1α and IL-8 were also compared with 10 µM dexamethasone as a positive control.

[0111] For reference, P. gingivalis The membrane fraction is P. gingivalis It contains substances that induce an inflammatory response as fractions.

[0113] Experimental results Test sample extraction solvent Concentration (µg / ml) IL-1αExpression level (% of negative control) IL-8Expression level (% of negative control) P. gingivalis membrane fraction - - 1371.75 133.95 positive control (dexamethasone) - 10 502.51 83.92 crustal exoskeleton hot water 100 612.13 111.20 200 511.10 88.11 500 317.42 76.57

[0114] Referring to Table 2, Figures 2 and 3, the zebra extract showed inhibitory effects on IL-1α and IL-8 equivalent to or greater than those of the positive control, dexamethasone 10 µM, at the experimental concentration.

[0116] <Formulation Example 1>

[0117] A mouthwash formulation containing the ingredients of the example prepared above as active ingredients was prepared as shown in Table 3 below. At this time, the unit of the ingredient content is weight%.

[0118] Ingredient name Content (weight%) Example (Citrate Exac) 0.05 Sodium fluoride 0.11 glycerin 5.0 xylitol 5.0 Poloxamer 0.15 Enzyme-treated stevia 0.05 antiseptic a very small amount purified water Remaining amount

[0119] A toothpaste formulation containing the ingredients of the example prepared above as active ingredients was prepared as shown in Table 4 below. At this time, the unit of the ingredient content is weight%.

[0120] Ingredient name Content (weight%) Example (Citrate Exac) 0.1 Carbomer 1.0 Sodium fluoride 0.22 silicon dioxide 19.0 glycerin 5.0 PEG-1500 5.0 Sorbitol 50.0 Sodium saccharin 0.5 spices 1.2 purified water Remaining amount

[0121] Although embodiments of the present invention have been described above with reference to the attached drawings, those skilled in the art will understand that the present invention may be implemented in other specific forms without altering its technical concept or essential features. Therefore, the embodiments described above should be understood as illustrative in all respects and not restrictive.

Claims

Claim 1 Oral composition containing a citrus extract as an active ingredient. Claim 2 The oral composition according to claim 1, characterized in that the above-mentioned crust extract is extracted by one or more extraction methods selected from ultrasonic extraction, room temperature extraction, hot water extraction, cold maceration extraction, reflux cooling extraction, and steam extraction. Claim 3 An oral composition according to claim 1, characterized in that the above-mentioned crust extract is extracted using one or more solvents selected from the group consisting of water, alcohol having 1 to 5 carbon atoms, acetone, ethanol, ethyl acetate, n-hexane, diethyl ether, and cyclohexane. Claim 4 An oral composition according to claim 1, characterized in that the above-mentioned crust extract is a dry extract or a soft extract. Claim 5 An oral composition according to claim 1, characterized in that the composition comprises 0.01 to 10 weight% of a crust extract relative to the total weight of the composition. Claim 6 An oral composition according to claim 1, characterized in that the above-mentioned crust extract comprises one or more selected from naringin and neohesperidin as indicator components. Claim 7 In claim 1, the oral composition is an oral composition for the prevention, improvement, or treatment of one or more oral diseases selected from bad breath, tooth decay, stomatitis, dental caries, periodontal disease, gingivitis, oral mucosal ulcers, and xerostomia. Claim 8 An oral composition according to claim 1, characterized in that the formulation of the oral composition is toothpaste, chewing gum, mouthwash, mouthwash, oral spray, oral ointment, or oral patch. Claim 9 A functional food composition comprising an oral composition according to any one of claims 1 to 7. Claim 10 A pharmaceutical composition for the prevention, improvement, or treatment of oral diseases comprising an oral composition according to any one of claims 1 to 7.

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