KR102288920B1 - Composition for prevention or treatment or oral disease - Google Patents
Composition for prevention or treatment or oral disease Download PDFInfo
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- KR102288920B1 KR102288920B1 KR1020207037854A KR20207037854A KR102288920B1 KR 102288920 B1 KR102288920 B1 KR 102288920B1 KR 1020207037854 A KR1020207037854 A KR 1020207037854A KR 20207037854 A KR20207037854 A KR 20207037854A KR 102288920 B1 KR102288920 B1 KR 102288920B1
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- South Korea
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- oral
- composition
- quasi
- present
- disease
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Abstract
본 발명은 천연 화합물을 포함하는 구강질환 예방 또는 치료용 조성물에 관한 것으로서, 보다 상세하게는 치아 우식증, 치주질환, 치통, 시린이 및 구취를 예방 또는 개선하는 효과를 가지는 의약외품 조성물에 관한 것이다. 본 발명의 조성물은 치아우식증 및 치주질환 유발세균에 대한 항균활성이 우수하며, 통증 및 염증 마커인 PGE2를 농도 의존적으로 억제하고, 치은염 형성 억제 효과, 시린이 증상 억제 효과 및 구취 제거 효과가 우수하여 치아 우식증, 치주질환, 시린이 및 구취로 이루어진 군으로부터 선택된 1 이상의 구강질환 예방 또는 개선용 의약외품 조성물로서의 활용도가 높다. 또한, 본 발명의 조성물은 약학적 조성물 및 식품 조성물로서 사용할 수 있다.The present invention relates to a composition for preventing or treating oral disease containing a natural compound, and more particularly, to a quasi-drug composition having an effect of preventing or improving dental caries, periodontal disease, toothache, sore throat and bad breath. The composition of the present invention has excellent antibacterial activity against dental caries and periodontal disease-causing bacteria, concentration-dependently inhibits PGE2, a pain and inflammation marker, gingivitis formation inhibitory effect, shirini symptom suppression effect, and bad breath removal effect. It has high utility as a quasi-drug composition for preventing or improving one or more oral diseases selected from the group consisting of dental caries, periodontal disease, sore throat and bad breath. In addition, the composition of the present invention can be used as a pharmaceutical composition and a food composition.
Description
본 발명은 천연 화합물을 유효성분으로 포함하는 구강질환 예방 또는 치료용 조성물에 관한 것으로서, 보다 상세하게는 치아 우식증, 치주질환, 치통, 시린이 및 구취를 예방 또는 개선하는 효과를 가지는 의약외품 조성물에 관한 것이다. 또한, 본 발명은 천연 화합물을 유효성분으로 포함하는 약학적 조성물, 식품 조성물 및 구강용 조성물에 관한 것이다.The present invention relates to a composition for preventing or treating oral diseases comprising a natural compound as an active ingredient, and more particularly, to a quasi-drug composition having an effect of preventing or improving dental caries, periodontal disease, toothache, sore throat and bad breath. will be. In addition, the present invention relates to a pharmaceutical composition, a food composition, and a composition for oral use containing a natural compound as an active ingredient.
건강한 치아는 오복 중 하나라 일컬을 정도로 삶의 질을 결정하는 중요한 요소이다. 구강질환 중 치아 우식증(dental cavities, 충치)과 치주질환(periodontal disease, 풍치)은 세계적으로 발병률이 높은 질환으로서, 통증, 저작기능 장애, 치주조직의 파괴, 구취 및 시린이와 같은 다양한 임상적인 증상을 유발하고 치아상실을 초래하는 주된 요인으로 알려져 있으며 식생활의 변화로 구강질환의 원인요소는 더 증가하고 있는 실정이다.Healthy teeth are an important factor in determining the quality of life to the extent that it is called one of the five blessings. Among oral diseases, dental cavities (cavities) and periodontal disease (periodontal disease) are diseases with a high incidence worldwide. It is known as the main factor that causes tooth loss and causes oral disease, and the causative factors of oral diseases are increasing due to changes in diet.
사람의 구강에는 대략 600 내지 800종 이상의 미생물이 존재하는 것으로 알려져 있는데 이러한 미생물들은 타액이 분비하는 리소자임(lysozyme)과 같은 효소에 의해 제어되고 있다. 그러나 영양분과 수분이 풍부한 구강환경은 미생물이 성장하기 좋은 조건이며, 혀나 치태(dental plaque)는 미생물의 훌륭한 서식처를 제공한다. 이러한 미생물 중 일부는 기회병원성 균으로서 치아우식, 치주질환 및 시린이(상아질 지각과민증)과 같은 질환 및 구취의 원인이 된다.It is known that about 600 to 800 kinds of microorganisms exist in the human oral cavity, and these microorganisms are controlled by enzymes such as lysozyme secreted by saliva. However, an oral environment rich in nutrients and moisture is a good condition for microorganisms to grow, and tongue and dental plaque provide an excellent habitat for microorganisms. Some of these microorganisms are opportunistic pathogens and cause diseases such as dental caries, periodontal disease, and dentin (dentin hypersensitivity) and bad breath.
치태 내에 서식하면서 치아우식, 치주질환, 구취 및 시린이를 유발하는 구강병원균 증식을 억제하는 방법으로 항균제가 있으며, 구강병원균에 대한 살균 및 정균 작용을 갖는 항생제를 포함하는 다양한 종류의 항균제제가 충치, 치주질환, 치수 및 치근단 감염의 억제 및 치료제로써 개발되어 왔다. There are antibacterial agents as a method of inhibiting the proliferation of oral pathogens that live in plaque and cause dental caries, periodontal disease, bad breath and sore throat. It has been developed as an inhibitor and therapeutic agent for periodontal disease, pulp and apical infection.
그런데, 항생제는 우리 몸에 대한 전신적인 부작용과 함께 구강내 내성균의 출현 및 균교대증(superinfection)을 유발할 수 있기 때문에 장기적인 사용이 곤란하여 단지 치료제로만 이용될 수 있는 단점이 있다. 또한, 구강청정제에 사용되고 있는 항균제제로는 생구이나린(Sangquinarine), 리스테린(Listerine), 피록사이드(Peroxide), 클로르헥시딘(Chlorhexidine) 등이 있는데, 생구이나린은 구강 내에서 세균에 대한 효과가 불분명하고 치주질환에 대한 치료 효과가 더욱 불분명할 뿐만 아니라 가격도 비싼 단점이 있고, 리스테린은 알코올이 주성분으로 약간의 정균 작용이 있으나 실제 구강 내에서는 일시적인 효과를 나타낼 뿐, 장기간 사용 시 조직에 대해 위해 작용도 나타날 수 있는 단점이 있다. 아울러, 최근 미백 효과를 위해 첨가되고 있는 피록사이드는 세균에 대한 독성이 있으나 동시에 인체 조직에도 독성을 나타내어 안전성에 문제가 있을 뿐 아니라 간혹 세균에서 피록사이드에 대한 내성균이 출현하기도 한다. 또한 클로르헥시딘은 치태 형성 억제와 더불어 치주질환 예방 및 치료제로써 현재까지 알려진 제제 중에서 가장 우수한 것으로 알려져 있으나, 조직에 대한 자극, 조직의 착색 및 변성을 유발하고, 특히 자극적인 맛이 강하고 냄새가 심한 부작용을 나타내는 문제점이 있을 뿐 아니라, 균교대증이 유발될 수 있고, 발암성이 있어 임신부의 경우 사용이 제한되는 등 치료나 특히 예방의 목적으로 장기간 사용할 수 없는 단점이 있다.However, since antibiotics can cause the appearance of resistant bacteria in the oral cavity and superinfection along with systemic side effects on our body, long-term use is difficult, and thus can only be used as a therapeutic agent. In addition, antibacterial agents used in mouthwashes include Sangquinarine, Listerine, Peroxide, and Chlorhexidine. The treatment effect for periodontal disease is not clear, and the price is expensive. Listerine contains alcohol as the main ingredient and has a slight bacteriostatic effect. There are some drawbacks that may appear. In addition, piroxide, which is recently added for whitening effect, is toxic to bacteria, but at the same time, it is also toxic to human tissues, so there is a problem in safety and sometimes bacteria resistant to pyroxide appear in bacteria. In addition, chlorhexidine is known to be the best known among agents for the prevention and treatment of periodontal disease as well as the inhibition of plaque formation. There are disadvantages in that it cannot be used for a long period of time for the purpose of treatment or, in particular, prevention, such as, as well as the problems shown, can cause mycosis mycosis, and has carcinogenic properties, limiting its use in pregnant women.
또한, 화학 반응을 통해 인위적으로 합성된 화합물은 세포 독성을 나타내거나 인체에 축적되는 등의 부작용이 발생할 수 있어, 안전성 측면에서 부작용 발생 가능성이 낮은 천연 화합물의 약리 활성에 대한 연구가 필요한 실정이다.In addition, a compound artificially synthesized through a chemical reaction may exhibit side effects such as cytotoxicity or accumulation in the human body, so there is a need for studies on the pharmacological activity of natural compounds with a low possibility of side effects in terms of safety.
본 발명자들은 상기와 같은 부작용에 대한 우려가 없으면서도 치아우식, 치주질환, 치통, 시린이, 구취와 같은 구강질환 예방 및 개선에 효과가 뛰어난 천연소재를 도출하기 위해 연구를 수행하였다. 그 결과, 체내에 안전하여 안심하고 사용할 수 있는 천연 화합물이 치아 우식증 및 치주질환 유발세균에 대한 항균 효과, PGE2 억제 효과를 통한 치통 완화 효과, 치은염 형성 억제 효과, 시린이 억제 효과 및 구취 제거 효과를 나타냄을 규명하여, 이를 활용한 의약외품 조성물, 약학적 조성물, 식품 조성물 및 구강용 조성물을 완성하기에 이르렀다.The present inventors have conducted research to derive a natural material excellent in the prevention and improvement of oral diseases such as dental caries, periodontal disease, toothache, sore throat, and bad breath without fear of side effects as described above. As a result, natural compounds that are safe and safe to use in the body have antibacterial effects on dental caries and periodontal disease-causing bacteria, toothache relief effect through PGE2 inhibitory effect, gingivitis formation inhibitory effect, shirin suppression effect, and bad breath removal effect. It has been found that the quasi-drug composition, pharmaceutical composition, food composition and oral composition using the same have been completed.
본 발명의 목적은 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 구강질환 예방 또는 개선용 의약외품 조성물을 제공하는 것이다.An object of the present invention is to provide a quasi-drug composition for preventing or improving oral diseases comprising a natural compound or a pharmaceutically acceptable salt thereof as an active ingredient.
본 발명의 다른 목적은 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 구강질환 예방 또는 치료용 약학적 조성물을 제공하는 것이다.Another object of the present invention is to provide a pharmaceutical composition for preventing or treating oral diseases comprising a natural compound or a pharmaceutically acceptable salt thereof as an active ingredient.
본 발명의 또 다른 목적은 천연 화합물 또는 이의 식품학적으로 허용 가능한 염을 유효성분으로 포함하는 구강질환 예방 또는 개선용 식품 조성물을 제공하는 것이다.Another object of the present invention is to provide a food composition for preventing or improving oral diseases comprising a natural compound or a pharmaceutically acceptable salt thereof as an active ingredient.
본 발명의 또 다른 목적은 천연 화합물 또는 이의 허용 가능한 염을 유효성분으로 포함하는 구강용 조성물을 제공하는 것이다.Another object of the present invention is to provide a composition for oral use comprising a natural compound or an acceptable salt thereof as an active ingredient.
본 발명의 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 의약외품 조성물은 구강질환 예방 또는 개선 효과가 우수하다. 구체적으로 본 발명의 조성물은 치아우식증 및 치주질환 유발세균에 대한 항균활성이 우수하며, 통증 및 염증 마커인 PGE2를 농도 의존적으로 억제하고, 치은염 형성 억제 효과, 시린이 증상 억제 효과 및 구취 제거 효과가 우수하여 치아 우식증, 치주질환, 시린이 및 구취로 이루어진 군으로부터 선택된 1 이상의 구강질환 예방 또는 개선용 의약외품 조성물로서의 활용도가 높다. 또한, 본 발명의 천연 화합물을 포함하는 조성물은 약학적 조성물 및 식품 조성물로서 사용할 수 있다.The quasi-drug composition comprising the natural compound of the present invention or a pharmaceutically acceptable salt thereof as an active ingredient is excellent in preventing or improving oral diseases. Specifically, the composition of the present invention has excellent antibacterial activity against dental caries and periodontal disease-causing bacteria, concentration-dependently inhibits PGE2, a pain and inflammation marker, gingivitis formation inhibitory effect, Shirin symptom suppression effect, and bad breath removal effect. It is excellent and has high utility as a quasi-drug composition for preventing or improving at least one oral disease selected from the group consisting of dental caries, periodontal disease, sore throat and bad breath. In addition, the composition comprising the natural compound of the present invention can be used as a pharmaceutical composition and a food composition.
발명의 실시를 위한 최선의 형태Best mode for carrying out the invention
본 발명은 상기와 같은 과제들을 해결하고, 본 발명의 목적을 달성하기 위하여 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 구강질환 예방 또는 개선용 의약외품 조성물을 제공한다.The present invention provides a quasi-drug composition for preventing or improving oral diseases comprising a natural compound or a pharmaceutically acceptable salt thereof as an active ingredient in order to solve the above problems and achieve the object of the present invention.
본 발명의 다른 양태로서, 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 구강질환 예방 또는 치료용 약학적 조성물을 제공한다.As another aspect of the present invention, there is provided a pharmaceutical composition for preventing or treating oral diseases comprising a natural compound or a pharmaceutically acceptable salt thereof as an active ingredient.
*본 발명의 또 다른 양태로서, 천연 화합물 또는 이의 식품학적으로 허용 가능한 염을 유효성분으로 포함하는 구강질환 예방 또는 개선용 식품 조성물을 제공한다.* As another aspect of the present invention, there is provided a food composition for preventing or improving oral diseases comprising a natural compound or a pharmaceutically acceptable salt thereof as an active ingredient.
본 발명의 또 다른 양태로서, 천연 화합물 또는 이의 허용 가능한 염을 유효성분으로 포함하는 구강용 조성물을 제공한다.As another aspect of the present invention, there is provided a composition for oral use comprising a natural compound or an acceptable salt thereof as an active ingredient.
본 발명에서는 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 의약외품 조성물을 제공한다.The present invention provides a quasi-drug composition comprising a natural compound or a pharmaceutically acceptable salt thereof as an active ingredient.
상기 '천연 화합물'이란 미생물, 식물, 동물 등의 생물로부터 직접적으로 만들어져, 이로부터 추출, 분리, 또는 정제될 수 있는 물질을 의미하며, 상기 천연 화합물의 구체적인 예시로서 알비플로린(Albiflorin), 아스트라갈로시드 I(Astragaloside I), 브라시놀리드 (Brassinolide), 엘레우테로시드 E (Eleutheroside E), 겐티오피크린(Gentiopicrin), 그라민(Gramine), 리엔지닌(Liensinine), 마크란토이딘 B (Macranthoidin B), 네오헤스페리딘 디하이드로칼콘(Neohesperidin dihydrochalcone), 오바쿠논 (Obacunone), 옥시소포카르핀 (Oxysophocarpine), 스크라레올리드 (Sclareolide), 소포리코시드 (Sophoricoside), 스웨로사이드 (Sweroside), 시네프린 (Synephrine) 등이 있으나, 이에 제한되는 것은 아니다.The 'natural compound' refers to a substance that is directly made from living organisms such as microorganisms, plants, and animals, and can be extracted, separated, or purified therefrom, and as specific examples of the natural compound, albiflorin, astragal Astragaloside I, Brassinolide, Eleutheroside E, Gentiopicrin, Gramine, Liensinine, Macrontoidine B ( Macranthoidin B), Neohesperidin dihydrochalcone, Obacunone, Oxysophocarpine, Sclareolide, Sophoricoside, Sweroside , Synephrine, and the like, but is not limited thereto.
본 발명에 있어서, 상기 알비플로린(Albiflorin)은 상기 화학식 1로 표시되고 분자식 C23H28O11, 분자량 408.4를 갖는 유기화합물이다.In the present invention, the albiflorin (Albiflorin) is an organic compound represented by the formula (1) and having a molecular formula C 23 H 28 O 11 , a molecular weight of 408.4.
본 발명에 있어서, 상기 아스트라갈로시드 I(Astragaloside I)은 상기 화학식 2로 표시되고 분자식 C45H72O16, 분자량 869.0을 갖는 유기화합물이다.In the present invention, the astragaloside I (Astragaloside I) is an organic compound represented by Chemical Formula 2 and having a molecular formula of C 45 H 72 O 16 and a molecular weight of 869.0.
본 발명에 있어서, 상기 브라시놀리드 (Brassinolide)는 상기 화학식 3으로 표시되고 분자식 C28H48O6, 분자량 480.6을 갖는 유기화합물이다.In the present invention, the brassinolide is an organic compound represented by Chemical Formula 3 and having a molecular formula C 28 H 48 O 6 and a molecular weight of 480.6.
본 발명에 있어서, 상기 엘레우테로시드 E (Eleutheroside E)는 상기 화학식 4로 표시되고 분자식 C34H46O18, 분자량 742.7을 갖는 유기화합물이다.In the present invention, the eleutheroside E (Eleutheroside E) is an organic compound represented by Formula 4 and having a molecular formula C 34 H 46 O 18 and a molecular weight of 742.7.
본 발명에 있어서, 상기 겐티오피크린(Gentiopicrin)은 상기 화학식 5로 표시되고 분자식 C16H20O9, 분자량 356.3을 갖는 유기화합물이다.In the present invention, the gentiopicrin is an organic compound represented by Chemical Formula 5 and having a molecular formula C 16 H 20 O 9 and a molecular weight of 356.3.
본 발명에 있어서, 상기 그라민(Gramine)은 상기 화학식 6으로 표시되고 분자식 C11H14N2, 분자량 174를 갖는 유기화합물이다.In the present invention, the gramin (Gramine) is an organic compound represented by the formula (6) and having a molecular formula C 11 H 14 N 2 and a molecular weight of 174.
본 발명에 있어서, 상기 리엔지닌(Liensinine)은 상기 화학식 7로 표시되고 분자식 C37H42N2O6, 분자량 610.7을 갖는 유기화합물이다.In the present invention, the Liensinine is an organic compound represented by Chemical Formula 7 and having a molecular formula C 37 H 42 N 2 O 6 and a molecular weight of 610.7.
본 발명에 있어서, 상기 마크란토이딘 B (Macranthoidin B)는 상기 화학식 8로 표시되고 분자식 C65H106O32, 분자량 1399.5을 갖는 유기화합물이다.In the present invention, the macroanthoidin B (Macranthoidin B) is an organic compound represented by Chemical Formula 8 and having a molecular formula of C 65 H 106 O 32 and a molecular weight of 1399.5.
본 발명에 있어서, 상기 네오헤스페리딘 디하이드로칼콘(Neohesperidin dihydrochalcone)은 상기 화학식 9로 표시되고 분자식 C28H36O15, 분자량 612.5을 갖는 유기화합물이다.In the present invention, the neohesperidin dihydrochalcone (Neohesperidin dihydrochalcone) is an organic compound represented by Chemical Formula 9 and having a molecular formula of C 28 H 36 O 15 and a molecular weight of 612.5.
본 발명에 있어서, 상기 오바쿠논 (Obacunone)은 상기 화학식 10으로 표시되고 분자식 C25H30O7, 분자량 455을 갖는 유기화합물이다.In the present invention, the obacunone (Obacunone) is an organic compound represented by Chemical Formula 10 and having a molecular formula of C 25 H 30 O 7 and a molecular weight of 455.
본 발명에 있어서, 상기 옥시소포카르핀 (Oxysophocarpine)은 상기 화학식 11로 표시되고 분자식 C15H22N2O2, 분자량 262.4을 갖는 유기화합물이다.In the present invention, the oxysophocarpine (Oxysophocarpine) is an organic compound represented by Chemical Formula 11 and having a molecular formula C 15 H 22 N 2 O 2 and a molecular weight of 262.4.
본 발명에 있어서, 상기 스크라레올리드 (Sclareolide)는 상기 화학식 12로 표시되고 분자식 C16H26O2, 분자량 250.3을 갖는 유기화합물이다.In the present invention, the Sclareolide is an organic compound represented by Chemical Formula 12 and having a molecular formula C 16 H 26 O 2 and a molecular weight of 250.3.
본 발명에 있어서, 상기 소포리코시드 (Sophoricoside)는 상기 화학식 13으로 표시되고 분자식 C21H20O10, 분자량 432을 갖는 유기화합물이다.In the present invention, the sophoricoside is an organic compound represented by Chemical Formula 13 and having a molecular formula C 21 H 20 O 10 and a molecular weight of 432.
본 발명에 있어서, 상기 스웨로사이드 (Sweroside)는 상기 화학식 14로 표시되고 분자식 C16H22O9, 분자량 358.3을 갖는 유기화합물이다.In the present invention, the Sweroside is an organic compound represented by Chemical Formula 14 and having a molecular formula C 16 H 22 O 9 and a molecular weight of 358.3.
본 발명에 있어서, 상기 시네프린 (Synephrine)은 상기 화학식 15로 표시되고 분자식 C9H13NO2, 분자량 167.2을 갖는 유기화합물이다.In the present invention, the synephrine is an organic compound represented by Chemical Formula 15 and having a molecular formula C 9 H 13 NO 2 and a molecular weight of 167.2.
본 발명은 상기 화합물의 획득 방법에 특별히 한정되지 않으며, 당업계에 공지된 방법으로 화학적으로 합성하거나, 시판되는 물질을 사용할 수 있다.The present invention is not particularly limited to a method for obtaining the compound, and may be chemically synthesized by a method known in the art, or a commercially available material may be used.
본 발명의 상기 화합물은 용매화된 형태뿐만 아니라 비-용매화된(unsolvated) 형태로 존재할 수도 있다. 본 발명의 상기 화합물은 결정형 또는 무정형 형태로 존재할 수 있으며, 이러한 모든 물리적 형태는 본 발명의 범위에 포함된다The compounds of the present invention may exist in solvated as well as unsolvated forms. The compounds 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.
본 발명은 상기 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 구강질환 예방 또는 개선용 의약외품 조성물을 제공한다.The present invention provides a quasi-drug composition for preventing or improving oral diseases comprising the natural compound or a pharmaceutically acceptable salt thereof as an active ingredient.
또한, 구체적으로, 본 발명은 상기 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 치아 우식증, 치주질환(치주염 또는 치은염), 치통, 시린이 및 구취로 이루어진 군으로부터 선택된 1 이상의 구강질환 예방 또는 개선용 의약외품 조성물을 제공할 수 있다.In addition, specifically, the present invention provides at least one oral cavity selected from the group consisting of dental caries, periodontal disease (periodontitis or gingivitis), toothache, sore throat, and bad breath comprising the natural compound or a pharmaceutically acceptable salt thereof as an active ingredient. It is possible to provide a quasi-drug composition for preventing or improving disease.
상기 '천연 화합물'에 대해서는 상기 설명한 바와 같다.The 'natural compound' is the same as described above.
본 발명에 있어서, “구강질환”이란 구강영역에서 발생하는 여러 가지 질환을 말하며, 상기 구강영역은 앞쪽 입술부터 뒤쪽 구협에서 인두와 연결되는 입 안의 공간을 의미한다. 본 발명에서 상기 구강질환은 구강에 발생하는 질환이라면 그 병증에 관계없이 모두 포함하는 개념이며, 상기 구강질환의 비제한적인 예로는 치아 우식증, 치주질환(치주염 또는 치은염), 치통, 시린이, 구취 등을 들 수 있다.In the present invention, “oral disease” refers to various diseases occurring in the oral region, and the oral region refers to a space in the mouth that is connected to the pharynx from the front lip to the rear palate. In the present invention, the oral disease is a concept that includes all diseases occurring in the oral cavity regardless of the pathology, and non-limiting examples of the oral disease include dental caries, periodontal disease (periodontitis or gingivitis), toothache, sore throat, bad breath and the like.
본 발명에 있어서, “치아 우식증(dental cavities)”이란 치아면에 서식하는 세균으로 인한 감염성 질환으로서, 충치라고도 하며, 치아의 경조직이 침식되어 결손하는 증세를 보인다. 구체적으로 치아의 머리 부분 표면을 덮고 있고, 치아 상아질을 보호하는 유백색의 반투명하고 단단한 물질을 치아 법랑질 또는 에나멜질이라고 하는데, 입 안에 서식하는 구강병원균에 의해 설탕, 전분 등이 분해되면서 생기는 산에 의해 치아의 법랑질이 손상되어 충치가 생기는 것을 말한다. 치아 우식증을 일으키는 주요 원인으로는 치아 표면에 생성된 세균막인 치태(dental plaque, 플라크)를 들 수 있는데, 타액이 치아에 얇고 끈적한 막을 형성하고, 그 위에 연쇄상구균의 일종인 스트렙토코쿠스 소브리누스(Streptococcus sobrinus)균 및 스트렙토코쿠스 뮤탄스(Streptococcus mutans) 등의 구강 미생물이 부착해 바이오 필름 (biofilm)을 형성함으로써 치태(dental plaque, 플라크)가 만들어지고 푸조박테리움(Fusobacterium)에 의해 더욱 두꺼워진다. 본 발명의 치아 우식증은 치아 우식증을 일으키는 원인균이라면 그 종류에 관계없이 모두 포함되나, 구체적으로는 스트렙토코쿠스 뮤탄스(Streptococcus mutans), 스트렙토코커스 산구이니스(Streptococcus sanguinis), 스트렙토코커스 소브리누스(Streptococcus sobrinus), 스트렙토코커스 라티(Streptococcus ratti), 스트렙토코커스 크리세티(Streptococcus criceti), 스트렙토코커스 안지노서스(Streptococcus anginosus) 및 유산균으로 이루어진 군에서 선택된 1종 이상의 균일 수 있으며, 보다 구체적으로는 스트렙토코쿠스 뮤탄스일 수 있다.In the present invention, the term “dental cavities” is an infectious disease caused by bacteria living on the tooth surface, also called caries, and shows a symptom in which the hard tissue of the tooth is eroded and defective. Specifically, the milky-white, translucent and hard material that covers the surface of the tooth head and protects the tooth dentin is called tooth enamel or enamel. Dental enamel is damaged and tooth decay occurs. The main cause of dental caries is dental plaque, which is a bacterial film formed on the surface of teeth. Oral microorganisms such as ( Streptococcus sobrinus ) and Streptococcus mutans attach to form a biofilm to form dental plaque and become thicker by Fusobacterium ) lose Dental caries of the present invention is included regardless of the type of bacteria causing dental caries, but specifically, Streptococcus mutans , Streptococcus sanguinis , Streptococcus sanguinis, Streptococcus sobrinus ), Streptococcus ratti , Streptococcus criceti , Streptococcus anginosus ( Streptococcus anginosus ) and lactic acid bacteria may be uniform at least one selected from the group consisting of, more specifically, Streptococcus may be mutans.
상기 스트렙토코쿠스 뮤탄스는 연쇄상구균의 일종으로 그람양성균이며 충치균이라도 불린다. 상기 스트렙토코쿠스 뮤탄스는 치아의 표면에서만 증식하는데, 생후 30개월 전후까지는 유치가 완성되지 않는다. 따라서 이 시기까지는 유아기 이후처럼 뮤탄스 균이 증식하기 어렵다. 유아기 동안 어른들의 입으로부터 뮤탄스 균에 감염되지 않아 입 안에 다른 구강 세균이 자리를 잡게 되면 이미 균형이 잡힌 구강 내의 생태계에 뮤탄스 균이 새로이 진입하기 어려워져 유아기 이후 일생동안 충치에 걸릴 확률이 현저히 낮아지게 된다. 이미 어른들의 입을 통해 원인균에 전염되었을 경우에는 양치질을 자주하고 입 안을 청결하게 유지하는 것이 충치 예방에 도움이 된다. 다만, 일단 뮤탄스 균이 구강 내에 자리잡았다면 뮤탄스 균 박멸은 불가능하다. The Streptococcus mutans is a type of streptococcus, a gram-positive bacteria, and is also called a caries bacteria. The Streptococcus mutans proliferates only on the surface of the teeth, but the primary teeth are not completed until around 30 months of age. Therefore, it is difficult for mutans to proliferate until this time, as it did after infancy. If mutans bacteria are not infected from the mouth of adults during infancy and other oral bacteria are established in the mouth, it is difficult for mutans bacteria to enter the already balanced oral ecosystem, and the probability of cavities throughout life after infancy is significantly higher. will be lowered If the causative bacteria have already been transmitted through the mouth of adults, frequent gargling and keeping the inside of the mouth clean will help prevent tooth decay. However, once mutans is established in the oral cavity, eradication of mutans is impossible.
본 발명의 일 실시예에서는, 스트렙토코쿠스 뮤탄스를 도말한 배지에 본 발명의 상기 천연 화합물이 포함된 디스크를 접종한 후 생육저지환의 크기를 측정한 결과, 상기 화합물을 포함한 실험군의 경우 생육저지환 직경이 10.0 mm 이상으로 스트렙토코커스 뮤탄스에 대하여 상당히 우수한 항균 활성을 나타내어, 상기 천연 화합물을 포함하는 조성물은 치아우식증 예방 또는 개선 용도로 사용될 수 있음을 확인하였다(표 2).In one embodiment of the present invention, as a result of measuring the size of the growth inhibition ring after inoculating the disk containing the natural compound of the present invention in the medium streptococcus mutans smeared, growth inhibition in the case of the experimental group including the compound It was confirmed that the ring diameter was 10.0 mm or more and exhibited significantly excellent antibacterial activity against Streptococcus mutans, so that the composition containing the natural compound could be used for preventing or improving dental caries (Table 2).
본 발명에 있어서, “치주질환(periodontal disease)”은 치아를 받치고 있는 치은과 치주인대 및 골조직에 염증이 생기는 질환으로서, 흔히 풍치라고도 하는데, 병의 정도에 따라 치은염(gingivitis)과 치주염(periodontitis)으로 나뉜다. 비교적 가볍고 회복이 빠른 형태의 치주질환으로 잇몸 즉, 연조직에만 국한된 형태를 치은염이라고 하고, 이러한 염증이 잇몸과 잇몸뼈 주변까지 진행된 경우를 치주염이라고 한다. 치은(잇몸)과 치아 사이에는 V자 모양의 틈이 있는데, 이 홈(sulcus)의 잇몸 선 아래 부분을 구강병원균이 공격하면서 염증 자극원인 리포폴리사카라이드(Lipopolysaccharide, LPS)를 방출하고, 이로 인해 잇몸이 붓고 출혈이 일어나는 등 염증이 생성되며, 이로써 치주인대와 인접조직이 손상된다. 치주염이 진행되면 치주인대, 더 나아가 치조골까지 손상시키고 결국 치아가 손실된다. 단백질, 비타민 등의 영양부족, 임신한 경우나 당뇨병 등과 같은 호르몬 장애, 흡연, 후천성면역결핍증(AIDS) 등이 질환을 악화시킬 수 있다. 또한, 치주질환의 다른 원인으로 치태 및 치석을 들 수 있다. 본 발명의 치주질환은 치주질환을 일으키는 원인균이라면 그 종류에 관계없이 모두 포함되나, 구체적으로는 악티노바실루스 악티노마이세템코미탄스 (Actinobacillus actinomycetemcomitans), 포피로모나스 진지발리스(Porphyromonas gingivalis), 타네렐라 포르시시아(Tannerella forsythia), 트레포네마 덴티콜라 (Treponema denticola) 및 푸소박테리움 누클리아툼(Fusobacterium nucleatum)으로 이루어진 군으로부터 선택된 1종 이상의 균일 수 있으며, 보다 구체적으로는 포피로모나스 진지발리스일 수 있다.In the present invention, "periodontal disease" is a disease in which the gingiva, periodontal ligament, and bone tissue supporting the teeth are inflamed, and is often referred to as wind teeth. Depending on the severity of the disease, gingivitis and periodontitis divided into It is a relatively light and quick form of periodontal disease, and the form limited only to the gums, that is, the soft tissue is called gingivitis, and when the inflammation has progressed to the gums and around the gums, it is called periodontitis. There is a V-shaped gap between the gingiva (gum) and teeth. Oral pathogens attack the lower part of the gum line of the sulcus and release lipopolysaccharide (LPS), which is an inflammatory stimulant. Inflammation occurs, such as swelling and bleeding of the gums, which damages the periodontal ligaments and adjacent tissues. As periodontitis progresses, periodontal ligaments and even alveolar bone are damaged and eventually teeth are lost. Nutritional deficiencies such as protein and vitamins, hormonal disorders such as pregnancy or diabetes, smoking, and acquired immunodeficiency syndrome (AIDS) can aggravate the disease. In addition, other causes of periodontal disease include plaque and tartar. Periodontal disease of the present invention is included regardless of the type of bacteria causing periodontal disease, but specifically Actinobacillus actinomycetemcomitans ( Actinobacillus actinomycetemcomitans ), Porphyromonas gingivalis ( Porphyromonas gingivalis ), Tane Rella forsythia ( Tannerella forsythia ), Treponema denticola ( Treponema denticola ) and Fusobacterium nucleatum ) Can be uniform at least one selected from the group consisting of, more specifically, P. It could be Bali.
상기 포피로모나스 진지발리스는 박테로이드(Bacteroide) 유연균의 일종으로 그람음성균이고, 혐기성균이다. 상기 포피로모나스 진지발리스는 치주질환이 발생한 구강 내에서 발견되며, 그 외에도 위장관 상부, 호흡기 및 결장에서도 발견된다. 만성 치주질환 환자는 상기 균의 콜라게네이즈 효소에 의해 콜라겐이 분해되며, 상기 균은 치은 섬유아세포에 침입할 수 있으며, 상당한 농도의 항생제 하에서도 생존할 수 있다. 또한, 상기 균은 치은 상피세포에 침입하여 장시간 생존할 수 있다. The Porphyromonas gingivalis is a type of Bacteroide, a Gram-negative bacterium, and an anaerobic bacterium. The Porphyromonas gingivalis is found in the oral cavity where periodontal disease has occurred, and in addition, it is also found in the upper gastrointestinal tract, respiratory tract and colon. In patients with chronic periodontal disease, collagen is degraded by the collagenase enzyme of the bacteria, and the bacteria can invade gingival fibroblasts and survive even under a significant concentration of antibiotics. In addition, the bacteria can survive for a long time by invading the gingival epithelial cells.
본 발명의 일 실시예에서는, 포피로모나스 진지발리스를 도말한 배지에 본 발명의 상기 천연 화합물이 포함된 디스크를 접종한 후 생육저지환의 크기를 측정한 결과, 상기 화합물을 포함한 실험군의 경우 생육저지환 직경이 10.0 mm 이상으로 포피로모나스 진지발리스에 대하여 상당히 우수한 항균 활성을 나타내어, 상기 화합물을 포함하는 조성물은 치주질환 예방 또는 개선 용도로 사용될 수 있음을 확인하였다(표 2).In one embodiment of the present invention, as a result of measuring the size of the growth-inhibiting ring after inoculating the disk containing the natural compound of the present invention in a medium smeared with P. gingivalis, growth in the case of the experimental group containing the compound It was confirmed that the low ring diameter was 10.0 mm or more and exhibited significantly excellent antibacterial activity against P. gingivalis, and the composition containing the compound could be used for preventing or improving periodontal disease (Table 2).
또한, 본 발명의 일 실시예에서는, 치은염증을 갖는 실험 대상자를 선별하여 임상실험을 수행한 결과, 상기 화합물을 포함하는 실험군 치약을 사용한 실험군의 경우 치은염증 억제 효과가 우수하며 6개월이 경과했음에도 정상출혈 상태를 유지하여 치은염증 억제 효과가 지속되어, 상기 천연 화합물을 포함하는 조성물은 치은염을 포함하는 치주질환 예방 또는 개선 용도로 사용될 수 있음을 확인하였다(표 4).In addition, in one embodiment of the present invention, as a result of conducting clinical trials by selecting test subjects with gingival inflammation, the experimental group using the experimental group toothpaste containing the compound has excellent gingival inflammation inhibitory effect, even after 6 months have elapsed It was confirmed that the gingivitis inhibitory effect was maintained by maintaining the normal bleeding state, and the composition containing the natural compound could be used for preventing or improving periodontal disease including gingivitis (Table 4).
본 발명에 있어서, “치통”이란 단 음식, 또는 아주 차갑거나 뜨거운 음식 등을 먹을 때 치아에 통증이 오는 것을 말하는데, 일반적으로는 치아 자체의 통증뿐만 아니라, 치아를 턱뼈에 지탱시키고 있는 치주조직의 통증도 포함된다. 보통 씹을 때 통증이 발생하며, 잇몸이 붓고 역한 냄새의 분비물이 나온다. 치통은 원인 질병에 따라 조금씩 다른 통증을 보이는데, 구체적으로 치아 우식증에 의한 통증은 초기에는 통증이 없으나 점차 진행되어 치아 속 신경까지 깊이 썩은 경우에 통증이 나타나고, 매복치가 있는 경우 치아 주변 조직의 염증으로 통증이 유발되며, 치아가 부서지거나 금이 간 경우, 찬 음식에 닿거나 강하게 깨물었을 때 치아가 갈라지면서 신경에 자극을 주어 통증이 생긴다. 치수염에 의한 경우, 초기에는 찬 음식이 닿을 때 통증을 느끼고 더 진행된 경우에는 뜨거운 음식에 통증을 느끼게 되며, 염증이 진행되어 치수 조직이 죽으면 찬 것, 더운 것에 대한 반응은 없고 치근단(치아 뿌리 끝)의 염증에 의한 통증이 생기게 된다.In the present invention, “tooth pain” refers to pain in the teeth when eating sweet food or very cold or hot food. Pain is also included. It is usually painful when chewing, swollen gums, and a foul-smelling discharge. Toothache shows slightly different pain depending on the cause of the disease. Specifically, the pain caused by dental caries is initially painless, but gradually progresses and the pain occurs when the nerves in the tooth are deeply rotted. Pain is caused, and when the tooth is broken or cracked, the tooth cracks when it comes in contact with cold food or when it is bitten strongly, which stimulates the nerve and causes pain. In the case of pulpitis, in the early stages, pain is felt when cold food is touched, and when it is more advanced, pain is felt by hot food. Pain is caused by inflammation of
본 발명의 일 실시예에서는, 통증 및 염증 마커로 알려진 PGE2 억제 효과를 확인한 결과, 본 발명의 상기 천연 화합물을 포함한 실험군의 경우 농도 의존적으로 PGE2를 억제하는 효과를 나타내는 것을 확인하였다 (표 5).In one embodiment of the present invention, as a result of confirming the PGE2 inhibitory effect known as a pain and inflammation marker, it was confirmed that the experimental group including the natural compound of the present invention exhibited a concentration-dependent effect of inhibiting PGE2 (Table 5).
본 발명에 있어서, “시린이”란 상아질과민증 치아(hypersensitive dentine)를 말하며, 시린이 증상이란 상아질 지각과민증(dentine hyperesthesia)을 말한다. 시린이 증상은 노출된 치아의 상아질 부분이 찬 공기나 자극적인 음식물 등에 접촉되었을 때 민감하게 느껴지는 것으로써, 치주질환을 가진 성인의 60 ~ 98 %에서 증상을 보이고 있다. 시린이 증상은 잘못된 양치 습관이나 과도한 교합력, 산에 의한 용해에 의해 잇몸쪽에 이가 패이는 경우, 구강 위생 상태가 불량한 경우, 치주 치료 후, 수복 치료를 받은 후, 산성화에 의한 치아가 용해된 경우에 나타날 수 있다. 시린이 증상의 근본적인 원인으로 치아의 상아질에 존재하는 많은 세관이 외부로 노출되면서 나타나는데, 노출에 의해 모든 자극을 그대로 치수내 신경으로 전달하여 똑같은 자극에 대해서도 평소보다 민감하게 반응 하게 되며 통증을 유발할 수 있다. 시린이 증상은 가벼운 증상에서 격렬하고 지속적인 통증까지 다양하게 나타날 수 있으며, 치아의 특성상 재생이 되지 않기 때문에 진통제나 소염제 등의 복용은 시린 현상의 근본적인 해결책이 되지 못한다. 시린이 증상은 치아 전체에 전반적으로 나타나기도 하며, 상악이나 하악, 또는 오른쪽이나 왼쪽 등 특정 부위에 한정되어 나타나기도 한다. 많이 발병하는 부위는 원인에 따라 다르나, 주로 송곳니, 작은 어금니 부위이며 가장 심하게 통증이 나타나는 부위는 90% 이상이 잇몸과 치아의 경계부분인 치경부이다. In the present invention, the term “single” refers to hypersensitive dentine, and the symptom of dentine hyperesthesia refers to dentine hyperesthesia. This symptom is a sensitive sensation when the exposed dentin of the tooth comes into contact with cold air or irritating food, and it is present in 60 to 98% of adults with periodontal disease. Painful tooth symptoms occur when teeth are dented on the gum side due to incorrect brushing habits, excessive occlusal force, or dissolution by acid, poor oral hygiene, periodontal treatment, restoration treatment, or tooth dissolution due to acidification may appear Shirin is the root cause of the symptoms and it appears when many tubules in the dentin of the tooth are exposed to the outside. there is. The symptoms of sore throat can vary from mild symptoms to intense and persistent pain, and because teeth do not regenerate due to the nature of the tooth, taking painkillers or anti-inflammatory drugs is not a fundamental solution to the pain. A sore throat symptom may appear throughout the tooth, or it may appear limited to a specific area such as the maxilla or mandible, or the right or left side. The most common areas vary depending on the cause, but mainly canine teeth and small molars.
본 발명의 일 실시예에서는, 상아질과민증 치아를 갖는 실험 대상자를 선별하여 임상실험을 수행한 결과, 본 발명의 상기 화합물을 포함하는 실험군 치약을 사용한 실험군의 경우 시린이 증상 억제 효과가 우수하여, 상기 천연 화합물을 포함하는 조성물은 시린이 예방 또는 개선 용도로 사용될 수 있음을 확인하였다(표 7).In one embodiment of the present invention, as a result of conducting clinical trials by selecting test subjects with dentin hypersensitivity teeth, in the case of the experimental group using the experimental group toothpaste containing the compound of the present invention, shirin has excellent symptom suppression effect, It was confirmed that the composition comprising the natural compound can be used for prophylactic or amelioration purposes (Table 7).
본 발명에 있어서, “구취”란 구강 및 인접기관으로부터 유래되는 냄새로 구취의 85 ~ 90%가 구강에서 유래하며, 특히, 혀의 뒷쪽에서 유래하고 있다. 구취의 주요 성분은 휘발성 황화합물인데, 휘발성 황화합물의 전체량 중 90%가 시스테인으로부터 만들어지는 황화수소(hydrogen sulfide)와 메티오닌으로부터 만들어지는 메틸머캡탄(methyl mercaptan)및 디메틸설파이드(dimethyl sulfide)이다. 이러한 성분들은 주로 혐기성 세균이 분비하는 단백질 효소에 의해서 생성되며, 혀의 뒷쪽이 가장 중요한 서식지가 된다. 이 부위는 타액에 의해 세정작용이 잘 되지 않고, 많은 작은 함몰이 있어 세균이 지속적으로 살아가는 장소가 된다. 혐기성 세균에 의한 휘발성 황화합물 생성이 구취의 원인으로 가장 중요하지만, 그 외 치아 우식증, 치주염, 구강 건조증 등과 같은 구강질환에 의해서도 발생한다. 구취를 발생시키는데 많은 종류의 혐기성 세균이 관여하며, 구취 발생 원인균의 비제한적인 예로 많은 종류와 많은 양의 효소를 분비하는 포르피로모나스 진지발리스(Porphyromonas gingivalis)를 들 수 있다.In the present invention, “bad breath” is a smell derived from the oral cavity and adjacent organs, and 85 to 90% of bad breath originates from the oral cavity, in particular, from the back of the tongue. The main component of bad breath is volatile sulfur compounds, and 90% of the total amount of volatile sulfur compounds is hydrogen sulfide made from cysteine and methyl mercaptan and dimethyl sulfide made from methionine. These components are mainly produced by protein enzymes secreted by anaerobic bacteria, and the back of the tongue is the most important habitat. This area is not well cleaned by saliva, and there are many small depressions, making it a place for bacteria to live continuously. Although the production of volatile sulfur compounds by anaerobic bacteria is the most important cause of bad breath, it is also caused by oral diseases such as dental caries, periodontitis, and dry mouth. Many types of anaerobic bacteria are involved in the occurrence of bad breath, and a non-limiting example of the bacteria causing bad breath may include Porphyromonas gingivalis , which secretes many types and large amounts of enzymes.
본 발명의 일 실시예에서는, 치아 우식증이 없는 실험 대상자를 대상으로 임상실험을 수행한 결과, 본 발명의 상기 천연 화합물을 포함하는 실험군 치약을 사용한 실험군의 경우 구취 제거 효과가 우수하여, 상기 화합물을 포함하는 조성물은 구취 예방 또는 개선 용도로 사용될 수 있음을 확인하였다(표 8).In one embodiment of the present invention, as a result of performing a clinical test on a test subject without dental caries, the effect of removing bad breath was excellent in the experimental group using the experimental group toothpaste containing the natural compound of the present invention, the compound It was confirmed that the composition comprising the composition can be used for preventing or improving bad breath (Table 8).
본 발명의 의약외품 조성물은 구강용 의약외품을 포함할 수 있다. 본 발명의 의약외품 조성물에 포함되는 성분은 유효성분으로서 상기 유효성분 이외에 구강용 의약외품 조성물에 통상적으로 이용되는 성분들을 포함할 수 있으며, 예컨대 연마제, 습윤제, 결합제, 기포제, 감미제, 방부제, 약효성분, 향미제, 색소, 용제, 증백제, 가용화제 또는 pH 조정제를 포함할 수 있다.The quasi-drug composition of the present invention may include a quasi-drug for oral use. Components included in the quasi-drug composition of the present invention may include components commonly used in oral quasi-drug compositions in addition to the active ingredients as an active ingredient, for example, an abrasive, a wetting agent, a binder, a foaming agent, a sweetener, a preservative, an active ingredient, a flavor agents, dyes, solvents, brighteners, solubilizers or pH adjusters.
본 발명의 구강용 의약외품 조성물은 당업계에서 통상적으로 제조되는 어떠한 제형으로도 제조될 수 있으며, 예를 들어, 치약, 구강세정제, 구강청정제, 껌, 캔디류, 구강스프레이, 구강용 연고제, 구강용 바니쉬, 구강양치액 및 잇몸 마사지 크림 등의 제형을 가질 수 있으나 이에 제한되는 것은 아니다.The quasi-drug composition for oral use of the present invention may be prepared in any formulation conventionally prepared in the art, for example, toothpaste, mouthwash, mouthwash, gum, candy, oral spray, oral ointment, oral varnish , oral gargle and gum massage cream, but are not limited thereto.
하나의 예로서, 본 발명의 구강용 의약외품 조성물이 치약의 제형일 경우, 습윤제, 연마제, 결합제, 기포제, 향미제, 감미제, 착색제, 보존제, 약효성분, 용제, pH 조절제 등을 포함할 수 있다.As an example, when the quasi-drug composition for oral use of the present invention is a toothpaste formulation, a wetting agent, an abrasive, a binder, a foaming agent, a flavoring agent, a sweetener, a coloring agent, a preservative, an active ingredient, a solvent, a pH adjusting agent, etc. may be included.
상기 습윤제는 치약제 성분 중 분말이 페이스트상이 되게 하고 치약제가 공기 중에 굳는 것을 방지하기 위한 것으로 글리세린, 솔비트액, 프로필렌글리콜, 폴리에틸렌 글리콜 등을 단독 또는 2종 이상 혼합하여 조성물 총 중량 중 1 ~ 60 중량%, 구체적으로는 10 ~ 50 중량%를 사용할 수 있다.The humectant is used to make the powder of the toothpaste component into a paste and prevent the toothpaste from solidifying in the air. Glycerin, sorbit solution, propylene glycol, polyethylene glycol, etc. are mixed alone or 2 or more types are mixed to form 1 to 60 weight of the total weight of the composition. %, specifically 10 to 50 wt% may be used.
상기 기포제는 치약제를 구강 중에 확산시켜 청소효과를 높이고, 계면활성제로서 작용하여 구강 오염을 세정하는 것으로 라우릴황산나트륨, 라우릴 사르코신산 나트륨, 알킬 설포호박산 나트륨, 자당 지방산 에스테르 등의 계면활성제를 단독 혹은 2종 이상 혼합하여 조성물 총 중량 중 0.5 ~ 10 중량%, 구체적으로는 0.5 ~ 5 중량%를 사용할 수 있다.The foaming agent diffuses the toothpaste in the oral cavity to enhance the cleaning effect, and acts as a surfactant to clean oral contamination. A surfactant such as sodium lauryl sulfate, sodium lauryl sarcosinate, sodium alkyl sulfosuccinate, and sucrose fatty acid ester is used alone. Or 0.5 to 10% by weight, specifically 0.5 to 5% by weight of the total weight of the composition by mixing two or more types may be used.
상기 결합제는 치약제중의 분말과 액체 성분 간의 분리를 방지하는 것으로 카복시메틸셀룰로오스나트륨, 메틸셀룰로오스, 하이드록시 프로필셀룰로오스 등의 셀룰로오스 유도체와 알긴산나트륨, 카라기난, 잔탄검 등을 단독 혹은 2종 이상 혼합하여 조성물 총 중량 중 0.1 ~ 5 중량%, 구체적으로는 0.3 ~ 2 중량%를 사용할 수 있다.The binder is to prevent separation between the powder and liquid components in the toothpaste. Cellulose derivatives such as sodium carboxymethyl cellulose, methyl cellulose, and hydroxypropyl cellulose and sodium alginate, carrageenan, xanthan gum, etc. are mixed alone or by mixing two or more types. 0.1 to 5% by weight, specifically 0.3 to 2% by weight of the total weight of the composition may be used.
상기 연마제는 치아표면을 상처내지 않고 치아표면의 부착물을 제거하고 치아 본래의 광택이 나도록 하는 것으로 탄산칼슘(CaCO3), 제2인산칼슘(CaHPO4, CaHPO42H2O), 무수규산(SiO22H2O), 수산화알루미늄(Al(OH)3), 피로인산카륨, 탄산마그네슘 등을 단독 혹은 2종 이상 혼합하여 조성물 총 중량 중 1 ~ 60 중량%, 구체적으로는 10 ~ 50 중량%를 사용할 수 있다.The abrasive article removes the attachment of the tooth surface rather to wound the tooth surface, and calcium carbonate as nadorok the original tooth polish (CaCO 3), calcium secondary phosphate (CaHPO 4, CaHPO 4 2H 2 O), silica (SiO 2 2H 2 O), aluminum hydroxide (Al(OH) 3 ), potassium pyrophosphate, magnesium carbonate, etc. alone or by mixing two or more types, 1 to 60% by weight, specifically 10 to 50% by weight of the total weight of the composition Can be used.
상기 향미제는 치약에 상쾌감과 냄새를 부여하여 사용감을 증진시키기 위한 것으로 페퍼민트오일, 스피아민트오일, 멘톨 등을 단독 혹은 2종 이상 혼합하여 조성물 총 중량 중 0.01 ~ 60 중량%, 구체적으로는 0.01 ~ 5 중량%를 사용할 수 있다.The flavoring agent is intended to enhance the feeling of use by imparting freshness and odor to the toothpaste. Peppermint oil, spearmint oil, menthol, and the like may be mixed alone or in a mixture of 0.01 to 60% by weight of the total weight of the composition, specifically 0.01 to 5% by weight may be used.
상기 감미제는 치약제 원료에 의한 불쾌한 맛이나 제거하고 청량감을 좋게 하기 위한 것으로 사카린산, 아스파탐, 자일리톨, 감초산 등을 단독 혹은 2종 이상 혼합하여 조성물 총 중량 중 0.01 ~ 60 중량%, 구체적으로는 0.01 ~ 5 중량%를 사용할 수 있다.The sweetener is to remove the unpleasant taste caused by the toothpaste raw material and to improve the refreshing feeling. Saccharinic acid, aspartame, xylitol, licorice acid, etc. are mixed alone or in a mixture of two or more of 0.01 to 60% by weight of the total weight of the composition, specifically 0.01 to 5% by weight may be used.
약효성분은 치우 우식증 예방, 치주질환 예방, 치통 예방, 시린이 예방, 구취 제거 등의 효과를 위한 것으로 불화물, 염화아연, 클로르헥시딘, 아미노카프론산, 트라넥사민산, 염화세틸피리디움, 염화피리독신, 트리클로산, 초산토코페롤, 일불소인산나트륨 등을 단독 혹은 2종 이상 혼합하여 사용할 수 있다. 본 발명에서는 상기 화합물을 추가적인 약효성분으로 사용할 수 있다.The active ingredients are fluoride, zinc chloride, chlorhexidine, aminocaproic acid, tranexamic acid, cetylpyridium chloride, pyridoxine chloride, Triclosan, tocopherol acetate, sodium monofluorophosphate, etc. can be used alone or in combination of two or more. In the present invention, the compound may be used as an additional active ingredient.
본 발명의 구강용 의약외품 조성물은 단독 또는 중복하여 사용하거나, 본 발명 이외의 다른 구강용 의약외품 조성물과 중복하여 사용할 수 있다.The quasi-drug composition for oral cavity of the present invention may be used alone or in combination, or may be used in combination with other quasi-drug compositions for oral use other than the present invention.
본 발명의 다른 하나의 양태로서, 상기 천연 화합물 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 포함하는 약학적 조성물을 제공한다. 또한, 구체적으로, 본 발명은 상기 천연 화합물을 유효성분으로 포함하는 치아 우식증, 치주질환(치주염 또는 치은염), 치통, 시린이 및 구취로 이루어진 군으로부터 선택된 1 이상의 구강질환 예방 또는 치료용 약학적 조성물을 제공할 수 있다. 상기 천연 화합물, 구강질환, 치아 우식증, 치주질환, 치통, 시린이 및 구취는 상기에서 설명한 바와 같다.As another aspect of the present invention, there is provided a pharmaceutical composition comprising the natural compound or a pharmaceutically acceptable salt thereof as an active ingredient. In addition, specifically, the present invention provides a pharmaceutical composition for preventing or treating one or more oral diseases selected from the group consisting of dental caries, periodontal disease (periodontitis or gingivitis), toothache, sore throat, and bad breath comprising the natural compound as an active ingredient can provide The natural compound, oral disease, dental caries, periodontal disease, toothache, sore throat and bad breath are the same as described above.
본 발명의 약학적 조성물은 구강질환을 예방하고 치료하기 위한 통상의 방법에 따라 정제, 환제, 산제, 과립제, 캡슐제, 현탁제, 내용액제, 유제, 시럽제, 에어로졸, 멸균 주사용액 등의 형태로 제형화가 가능하다.The pharmaceutical composition of the present invention is in the form of tablets, pills, powders, granules, capsules, suspensions, internal solutions, emulsions, syrups, aerosols, sterile injection solutions, etc. according to conventional methods for preventing and treating oral diseases. formulation is possible.
경구투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형제제는 적어도 하나 이상의 부형제, 예를 들면, 전분, 탄산칼슘, 수크로스, 락토오스, 젤라틴 등을 섞어 조제될 수 있다. 또한, 단순한 부형제 이외에 마그네슘 스테아레이트, 탈크 같은 윤활제도 사용될 수 있다. 경구투여를 위한 액상제제로는 현탁제, 내용액제, 유제, 시럽제 등이 포함되며, 흔히 사용되는 단순 희석제인 물, 리퀴드 파라핀 이외에 여러 가지 부형제, 예를 들면, 습윤제, 감미제, 방향제, 보존제 등이 사용될 수 있다.Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc., and these solid preparations are prepared by mixing at least one excipient, for example, starch, calcium carbonate, sucrose, lactose, gelatin, etc. can be In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Liquid formulations for oral administration include suspensions, internal solutions, emulsions, syrups, etc., and various excipients, for example, wetting agents, sweeteners, fragrances, preservatives, etc. in addition to commonly used simple diluents such as water and liquid paraffin. can be used
비경구투여를 위한 제제는 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조 제제, 좌제 등을 포함할 수 있다. 비수성용제와 현탁용제로는 프로필렌글리콜, 폴리에틸렌 글리콜, 올리브 오일 등과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다.Formulations for parenteral administration may include sterile aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, suppositories, and the like. Vegetable oils such as propylene glycol, polyethylene glycol, and olive oil, and injectable esters such as ethyl oleate may be used as non-aqueous solvents and suspensions.
또한, 본 발명의 약학적 조성물은 담체, 부형제 또는 희석제를 추가로 포함할 수 있다. 담체, 부형제 또는 희석제로는 락토즈, 텍스트로즈, 수크로스, 솔비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 전분, 아카시아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로오즈, 메틸 셀루로오즈, 하이드록시 프로필 메틸 셀룰로오즈, 미정질 셀룰로오즈, 폴리비닐 피롤리돈, 물, 메틸히드록시벤조에이트, 플로필히드록시벤조에이트, 프로필히드록시벤조에이트, 탈크, 마그네슘 스테아레이트, 이산화규소 등의 광물유 등이 사용될 수 있다.In addition, the pharmaceutical composition of the present invention may further include a carrier, excipient or diluent. Carriers, excipients or diluents include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, hydroxy Mineral oils such as propyl methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methyl hydroxy benzoate, propyl hydroxy benzoate, propyl hydroxy benzoate, talc, magnesium stearate, silicon dioxide, etc. may be used. there is.
본 발명에 따른 약학적 조성물의 구체적인 투여량은 제제화 방법, 환자의 상태 및 체중, 환자의 성별, 연령, 질병의 정도, 약물형태, 투여경로 및 기간, 배설 속도, 반응 감응성 등과 같은 요인들에 따라 당업자에 의해 다양하게 선택될 수 있으며, 투여량 및 횟수는 어떠한 면에서든 본 발명의 범위를 제한하는 것은 아니다.The specific dosage of the pharmaceutical composition according to the present invention depends on factors such as the formulation method, the patient's condition and weight, the patient's sex, age, degree of disease, drug form, administration route and period, excretion rate, reaction sensitivity, etc. It can be variously selected by those skilled in the art, and the dosage and frequency do not limit the scope of the present invention in any way.
본 발명의 약학적 조성물은 쥐, 생쥐, 가축, 인간 등의 포유동물에 다양한 경로를 통해 투여될 수 있다. 투여의 모든 방식은 예상될 수 있으며, 예를 들어 경구, 정맥, 근육 또는 피하 주사에 의해 투여될 수 있다.The pharmaceutical composition of the present invention may be administered to mammals such as rats, mice, livestock, and humans through various routes. Any mode of administration may be contemplated and may be administered, for example, by oral, intravenous, intramuscular or subcutaneous injection.
본 발명의 또 다른 하나의 양태로서, 본 발명은 상기 천연 화합물 또는 이의 식품학적으로 허용 가능한 염을 유효성분으로 포함하는 식품 조성물을 제공한다. 또한, 구체적으로, 본 발명은 상기 화합물을 유효성분으로 포함하는 치아 우식증, 치주질환(치주염 또는 치은염), 치통, 시린이 및 구취로 이루어진 군으로부터 선택된 1 이상의 구강질환 예방 또는 개선용 식품 조성물을 제공할 수 있다. 상기 천연 화합물, 구강질환, 치아 우식증, 치주질환, 치통, 시린이 및 구취는 상기에서 설명한 바와 같다. 상기 식품 조성물은 건강기능식품의 형태로 사용될 수 있으나, 이에 제한되는 것은 아니다.As another aspect of the present invention, the present invention provides a food composition comprising the natural compound or a food pharmaceutically acceptable salt thereof as an active ingredient. In addition, specifically, the present invention provides a food composition for preventing or improving at least one oral disease selected from the group consisting of dental caries, periodontal disease (periodontitis or gingivitis), toothache, sore throat, and bad breath comprising the compound as an active ingredient can do. The natural compound, oral disease, dental caries, periodontal disease, toothache, sore throat and bad breath are the same as described above. The food composition may be used in the form of health functional food, but is not limited thereto.
본 발명의 식품 조성물에 포함된 상기 천연 화합물 또는 이의 식품학적으로 허용 가능한 염은 상기 화합물을 포함하는 동식물, 이의 추출물, 이의 분획물 또는 이의 가공물의 형태로 포함될 수 있다. 또한 상기 조성물은 유효성분 이외에 식품학적으로 허용 가능한 식품보조첨가제를 포함할 수 있다.The natural compound or a pharmaceutically acceptable salt thereof contained in the food composition of the present invention may be included in the form of animals and plants containing the compound, an extract thereof, a fraction thereof, or a processed product thereof. In addition, the composition may include a food pharmaceutically acceptable food supplement additive in addition to the active ingredient.
본 발명에 있어서, "식품보조첨가제"란 식품에 보조적으로 첨가될 수 있는 구성요소를 의미하며, 각 제형의 건강기능식품을 제조하는데 첨가되는 것으로서 당업자가 적절히 선택하여 사용할 수 있다. 식품보조첨가제의 예로는 여러 가지 영양제, 비타민, 광물(전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 충진제, 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알콜, 탄산음료에 사용되는 탄산화제 등이 포함되지만, 상기 예들에 의해 본 발명의 식품보조첨가제의 종류가 제한되는 것은 아니다.In the present invention, "food supplementary additive" means a component that can be added to food as an auxiliary, added to the manufacture of health functional food of each formulation can be appropriately selected and used by those skilled in the art. Examples of food supplement additives include various nutrients, vitamins, minerals (electrolytes), synthetic flavoring agents and flavoring agents such as natural flavoring agents, coloring agents and fillers, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners , pH adjuster, stabilizer, preservative, glycerin, alcohol, carbonation agent used in carbonated beverages, etc., but the above examples are not limited to the type of food supplement additive of the present invention.
본 발명의 식품 조성물에는 건강기능식품이 포함될 수 있다. 본 발명에 있어서, "건강기능식품"이란 인체에 유용한 기능성을 가진 원료나 성분을 사용하여 정제, 캅셀, 분말, 과립, 액상 및 환 등의 형태로 제조 및 가공한 식품을 말한다. 여기서 “기능성”이라 함은 인체의 구조 및 기능에 대하여 영양소를 조절하거나 생리학적 작용 등과 같은 보건용도에 유용한 효과를 얻는 것을 의미한다. 본 발명의 건강기능식품은 당업계에서 통상적으로 사용되는 방법에 의하여 제조 가능하며, 상기 제조시에는 당업계에서 통상적으로 첨가하는 원료 및 성분을 첨가하여 제조할 수 있다. 또한 상기 건강기능식품의 제형 또한 건강기능식품으로 인정되는 제형이면 제한 없이 제조될 수 있다. 본 발명의 식품 조성물은 다양한 형태의 제형으로 제조될 수 있으며, 일반 약품과는 달리 식품을 원료로 하여 약품의 장기 복용 시 발생할 수 있는 부작용 등이 없는 장점이 있고, 휴대성이 뛰어나, 본 발명의 건강기능식품은 구강질환을 예방 또는 개선시키기 위한 보조제로 섭취가 가능하다.The food composition of the present invention may include a health functional food. In the present invention, "health functional food" refers to a food manufactured and processed in the form of tablets, capsules, powders, granules, liquids, pills, etc. using raw materials or ingredients useful for the human body. Here, the term “functionality” refers to obtaining useful effects for health purposes such as regulating nutrients or physiological effects on the structure and function of the human body. The health functional food of the present invention can be prepared by a method commonly used in the art, and at the time of manufacture, it can be prepared by adding raw materials and components commonly added in the art. In addition, if the formulation of the health functional food is also recognized as a health functional food, it may be manufactured without limitation. The food composition of the present invention can be prepared in various forms, and unlike general drugs, it has the advantage that there are no side effects that may occur during long-term administration of the drug using food as a raw material, and has excellent portability, Health functional food can be consumed as a supplement to prevent or improve oral diseases.
본 발명의 건강기능식품이 취할 수 있는 형태에는 제한이 없으며, 통상적인 의미의 식품을 모두 포함할 수 있고, 기능성 식품 등 당업계에 알려진 용어와 혼용 가능하다. 아울러 본 발명의 건강기능식품은 당업자의 선택에 따라 식품에 포함될 수 있는 적절한 기타 보조성분과 공지의 첨가제를 혼합하여 제조할 수 있다. 첨가할 수 있는 식품의 예로는 육류, 소세지, 빵, 쵸코렛, 캔디류, 스낵류, 과자류, 피자, 라면, 기타 면류, 껌류, 아이스크림류를 포함한 낙농제품, 각종 스프, 음료수, 차, 드링크제, 알콜 음료 및 비타민 복합제 등이 있으며, 본 발명에 따른 상기 화합물을 주성분으로 하여 제조한 즙, 차, 젤리 및 주스 등에 첨가하여 제조할 수 있다. 또한 동물을 위한 사료로 이용되는 식품도 포함한다.There is no limitation in the form that the health functional food of the present invention can take, and it may include any food in a conventional sense, and may be used interchangeably with terms known in the art, such as functional food. In addition, the health functional food of the present invention can be prepared by mixing known additives with other suitable auxiliary ingredients that may be included in the food according to the selection of those skilled in the art. Examples of foods that can be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, beverages, tea, drinks, alcoholic beverages and There are vitamin complexes and the like, and it can be prepared by adding the compound according to the present invention as a main component to juice, tea, jelly, juice, and the like. It also includes food used as feed for animals.
발명의 실시를 위한 형태Modes for carrying out the invention
이하, 실시예 및 실험예를 통하여 본 발명의 구성 및 효과를 더욱 상세히 설명하고자 한다. 이들 실시예 및 실험예는 오로지 본 발명을 예시하기 위한 것일 뿐 본 발명의 범위가 이들 실시예 및 실험예에 의해 제한되는 것은 아니다.Hereinafter, the configuration and effect of the present invention will be described in more detail through Examples and Experimental Examples. These Examples and Experimental Examples are only for illustrating the present invention, and the scope of the present invention is not limited by these Examples and Experimental Examples.
실험예 1 : 치아 우식증 및 치주염 원인균에 대한 항균 효과Experimental Example 1: Antibacterial effect on bacteria causing dental caries and periodontitis
상기 화학식 1 내지 15의 화합물의 치아 우식증 및 치주염에 대한 예방 또는 치료 효과를 확인하기 위하여 항균 활성 실험을 수행하였다. 구강병원균 생육 억제 효과를 확인하고자 치아 우식증 대표유발 세균인 스트렙토코커스 뮤탄스(Streptococcus mutans)와 치주질환 대표유발 세균인 포피로모나스 진지발리스(Porphyromonas gingivalis)를 이용하여 페이퍼 디스크 검사법을 사용함으로써 항균력 테스트를 실시하였다.An antibacterial activity experiment was performed to confirm the preventive or therapeutic effect of the compounds of Formulas 1 to 15 on dental caries and periodontitis. Antibacterial activity test by using the paper disc test method using Streptococcus mutans , the representative bacteria causing dental caries, and Porphyromonas gingivalis , the representative bacteria causing periodontal disease, to confirm the effect of inhibiting the growth of oral pathogens was carried out.
상기 각 구강병원균들을 하기 표 1의 최적 배양조건에서 활성을 증가시킨 후, 각 균의 최적배지에서 4 ~ 6시간 정도 배양하여 배양액의 탁도를 Macfarland turbidity No. 0.5 (1.5 X 108)가 되도록 맞추고, 상기 각 구강병원균 0.1ml를 평판배지에 골고루 도말하였다. 이후, 멸균한 페이퍼 디스크(Whatman no.5 paper, 8mm diameter)에 상기 화학식 1 내지 15의 화합물을 각각 10 mg/disc 농도로 접종하여 1시간 동안 흡수 건조시켰다. 그런 다음, 상기 각 구강병원균의 최적온도에서 24 ~ 48시간 배양한 후 생육저지환의 크기(직경 mm)를 측정하였으며, 그 결과를 하기 표 2에 나타내었다.After increasing the activity of each oral pathogen in the optimal culture conditions shown in Table 1 below, incubate for 4 to 6 hours in the optimal medium of each bacteria to determine the turbidity of the culture medium by Macfarland turbidity No. It was adjusted to be 0.5 (1.5 X 10 8 ), and 0.1 ml of each oral pathogen was spread evenly on a plate medium. Thereafter, the compounds of Chemical Formulas 1 to 15 were each inoculated at a concentration of 10 mg/disc on a sterilized paper disk (Whatman no. 5 paper, 8 mm diameter), and absorbed and dried for 1 hour. Then, after culturing for 24 to 48 hours at the optimal temperature of each oral pathogen, the size (diameter mm) of the growth-inhibiting ring was measured, and the results are shown in Table 2 below.
상기 표 2에 나타난 바와 같이, 무처리군과 비교했을 때, 화학식 1 내지 15의 화합물을 처리한 군은 상기 2 종의 구강병원균에 대한 생육저지환 직경이 9.5 mm 이상으로 스트렙토코커스 뮤탄스 및 포피로모나스 진지발리스에 대한 상당히 우수한 항균활성을 나타내었다. 따라서, 상기 화학식 1 내지 15의 화합물은 치아 우식증 또는 치주질환을 예방 또는 치료하는 용도로 사용할 수 있음을 알 수 있었다. 실험예 2 : 치은염 형성 억제 효과 As shown in Table 2, compared to the untreated group, the group treated with the compounds of Formulas 1 to 15 had a growth-inhibiting ring diameter of 9.5 mm or more for the two oral pathogens, Streptococcus mutans and foreskin. It exhibited a fairly excellent antibacterial activity against Romonas gingivalis. Therefore, it was found that the compounds of Formulas 1 to 15 can be used for preventing or treating dental caries or periodontal disease. Experimental Example 2: Gingivitis formation inhibitory effect
상기 화학식 1 내지 15의 화합물의 치은염 예방 또는 치료 효과를 확인하기 위하여 실험 대상군을 선별하여 임상실험을 수행하였다.In order to confirm the gingivitis prevention or treatment effect of the compounds of Formulas 1 to 15, a clinical trial was performed by selecting a test subject group.
먼저, 치약 제조 시에 일반적으로 사용되는 카르복시메칠세룰로오스나트륨, 라우릴황산나트륨, 글리세린, 콜리이드성 이산화규소, 실리카류, 소디움코코일이세치온산나트륨, 도디신과 감미제, 방향제, 착색제 등을 이용하여 대조군 치약을 만들었고, 상기 대조군 치약에 상기 화학식 1 내지 15의 화합물 중 하나의 화합물을 0.01 중량% 함유하도록 하여 실험군 치약을 제조하였다. First, sodium carboxymethyl cellulose, sodium lauryl sulfate, glycerin, colloidal silicon dioxide, silicas, sodium cocoyl ethionate sodium, dodicin and sweeteners, fragrances, and coloring agents, which are generally used in the manufacture of toothpaste, are used. to make a control toothpaste, and 0.01 wt% of one of the compounds of Formulas 1 to 15 was contained in the control toothpaste to prepare an experimental group toothpaste.
실험 대상자를 선별하기 위하여 치열이 고르고 결손 치아가 없는 치은염증 환자를 대상으로 연령별 30세부터 50세까지 10세 간격으로 성별에 따라 30명씩 정밀한 구강검진을 실시하였으며, 그런 다음 120명의 실험 대상군을 선별한 후 60명씩 나누어 치은염증 치료효과에 대한 임상실험을 하기와 같이 수행하였다. In order to select the subjects for the experiment, precise oral examinations were conducted for patients with gingivitis with even dentition and no missing teeth, from 30 to 50 years of age by age, at 10-year intervals for 30 patients by gender. After screening, 60 patients were divided into clinical trials for the treatment effect of gingival inflammation as follows.
구체적으로, 실험 대상군을 대조군과 실험군으로 나누고 대조군은 식후 2시간 경과 후 잠자기 전에 하루 3회 상기 제조된 대조군 치약을 사용하도록 교육시키고, 실험군은 동일 시간에 하루 3회 상기 제조된 실험군 치약을 사용하도록 교육시켰다. 이후 치면세마를 실시하여 초기 치은염지수를 점수화하고 대조군은 상기 제조된 대조군 치약을, 실험군은 상기 제조된 실험군 치약을 사용하도록 하여 1주, 1개월, 3개월 및 6개월 경과 후 구강검진을 실시하여 치은염지수를 검사하였다. 치은염지수의 측정방법은 페리오덴탈 프로브(periodontal probe)를 치은열구 내에 삽입하여 힘을 가하지 않은 상태로 각 치아주위를 연소하여 탐침하고 30초가 지난 뒤에 출혈된 상태를 측정하여 하기 표 3에 나타난 기준에 따라 점수를 기록하였으며, 그 결과는 표 4에 나타내었다.Specifically, the experimental group was divided into a control group and an experimental group, and the control group was instructed to use the prepared control toothpaste 3 times a day before going to sleep after 2 hours after eating, and the experimental group used the prepared experimental group toothpaste 3 times a day at the same time educated to do Afterwards, tooth brushing was performed to score the initial gingivitis index, and the control group used the prepared control toothpaste and the experimental group used the prepared experimental group toothpaste. After 1 week, 1 month, 3 months and 6 months, oral examination was performed. The gingivitis index was examined. The gingivitis index is measured by inserting a periodontal probe into the gingival sulcus, burning the probe around each tooth without applying any force, and measuring the bleeding state after 30 seconds has passed. Scores were recorded accordingly, and the results are shown in Table 4.
상기 표 4에 나타난 바와 같이, 대조군과 비교했을 때, 화학식 1 내지 15의 화합물 중 하나의 화합물이 포함된 치약을 사용한 실험군은 6개월이 경과했음에도 정상출혈 상태를 유지하여 치은염증 억제 효과가 지속되었다. 따라서, 화학식 1 내지 15의 화합물은 치은염을 예방 또는 치료하는 용도로 사용할 수 있음을 알 수 있었다. 실험예 3 : 통증 및 염증 마커인 PGE2 억제 효과 As shown in Table 4, compared with the control group, the experimental group using a toothpaste containing one of the compounds of Formulas 1 to 15 maintained the normal bleeding state even after 6 months had elapsed, and the gingivitis inhibitory effect was maintained. . Accordingly, it was found that the compounds of Formulas 1 to 15 can be used for preventing or treating gingivitis. Experimental Example 3: Pain and inflammation marker PGE2 inhibitory effect
상기 화학식 1 내지 15의 화합물의 치통 예방 또는 치료 효과를 확인하기 위하여 통증 및 염증 마커로 알려진 PGE2 억제 효과를 확인하였다.In order to confirm the preventive or therapeutic effect of the compounds of Formulas 1 to 15, the inhibitory effect of PGE2, known as a pain and inflammation marker, was confirmed.
먼저, 대식세포를 10% FBS를 포함하는 DMEM 배지에서 1.5 X 105 cells/ml 농도로 접종하여 37℃, 5% CO2 조건으로 24 well plate에 24시간 동안 배양하였다. 그런 다음, 염증 유도 자극원인 LPS 1㎍/ml와 화학식 1 내지 15의 화합물 각각을 농도별로 처리하여 24시간 동안 추가 배양한 후, PGE2 ELISA assay kit(Thermo SCIENTIFIC)를 구입하여 상층액을 이용해 상기 화학식 1 내지 15의 화합물의 농도에 따른 PGE2 억제능을 분석하였다 (표 5).First, macrophages were inoculated in DMEM medium containing 10% FBS at a concentration of 1.5 X 10 5 cells/ml and cultured in a 24 well plate at 37° C. and 5% CO 2 conditions for 24 hours. Then, 1 μg/ml of LPS, which is an inflammation-inducing stimulant, and each of the compounds of Formulas 1 to 15 were treated at different concentrations and further cultured for 24 hours, PGE2 ELISA assay kit (Thermo SCIENTIFIC) was purchased and the supernatant was used for the above formula PGE2 inhibitory ability according to the concentration of compounds 1 to 15 was analyzed (Table 5).
표 5에 나타난 바와 같이, LPS만을 처리한 군과 비교했을 때, 상기 화학식 1 내지 15의 화합물은 모두 농도 의존적으로 PGE2 억제 효과를 나타냄을 확인하여, 치통의 예방 및 치료 효과가 우수함을 확인하였다. 실험예 4 : 시린이 억제 효과 As shown in Table 5, when compared to the group treated with only LPS, it was confirmed that all of the compounds of Formulas 1 to 15 exhibited a concentration-dependent PGE2 inhibitory effect, thereby confirming that the preventive and therapeutic effects of toothache were excellent. Experimental Example 4: Inhibitory effect of sirin
상기 화학식 1 내지 15의 화합물의 시린이 예방 또는 치료 효과를 확인하기 위하여 실험 대상자를 선별하여 임상실험을 수행하였으며, 임상실험에서 사용된 대조군 치약 및 실험군 치약은 상기 실험예 2의 치약과 동일한 방법으로 각각 제조하였다.In order to confirm the preventive or therapeutic effect of the compounds of Formulas 1 to 15, clinical trials were conducted by selecting test subjects. each was prepared.
실험 대상자들은 상아질과민증 치아를 가진 사람으로서 이 실험에 참여하기를 동의한 지원자 40명이며, 총 실험 대상 치아는 80개였다. 또한, 실험 대상자들 중 남자는 20명, 여자는 20명이고, 연령은 20세에서 50세였다. 실험 대상자들이 치약 내용물을 알지 못하도록 하였으며, 총 실험기간은 2주로 하였다. The subjects of the experiment were 40 volunteers with dentin hypersensitivity teeth who agreed to participate in this experiment, and a total of 80 teeth were tested. In addition, among the test subjects, there were 20 males and 20 females, and the ages ranged from 20 to 50 years old. Subjects were not allowed to know the contents of the toothpaste, and the total duration of the experiment was 2 weeks.
실험은 온도 자극을 가한 후 실험 대상자의 반응을 측정하는 방법으로 수행되었다. 실험을 실시하기 전에 미리 각 실험 대상자의 상아질과민증 치아의 과민 부위를 체크하고, 치아의 시린 부위에 약 5℃의 차가운 물을 스포이드로 떨어뜨려 하기 표 6에 나타난 기준에 따라 평점을 한 후 대조군은 상기 대조군 치약을, 실험군은 상기 실험군 치약을 2주 동안 1일 3회 사용하게 하고, 2주가 지나 다시 약 5℃의 차가운 물을 스포이드로 떨어뜨려 평점을 하였다. 통계처리는 실험 실시 전과 2주 후의 자극 점수를 대응표본 T- 검정(paired Student-t test)로 검정하였으며, 온도 자극에 대한 2주 후의 반응 점수는 하기 표 7에 나타내었다.The experiment was performed by measuring the reaction of the test subject after applying a temperature stimulus. Before carrying out the experiment, check the sensitive area of the dentin hypersensitivity tooth of each test subject in advance, drop cold water of about 5°C with a dropper on the sore area of the tooth and rate it according to the criteria shown in Table 6 below The control toothpaste and the experimental group were graded by dropping the experimental group toothpaste 3 times a day for 2 weeks, and then dropping cold water at about 5°C again with a dropper after 2 weeks. For statistical processing, the stimulation scores before and 2 weeks after the experiment were tested using the paired Student-t test, and the response scores after 2 weeks to the temperature stimulation are shown in Table 7 below.
※ p>0.05: 95% 신뢰도, 통계적으로 유의한 차이가 없음. *p<0.05: 95% 신뢰도, 통계적으로 유의한 차이가 있음.상기 표 7에 나타난 바와 같이, 대조군과 비교했을 때, 화학식 1 내지 15의 각각의 화합물이 포함된 치약을 사용한 실험군은 2주 경과 후 시린이 현상이 억제되었다. 따라서, 화학식 1 내지 15의 화합물은 시린이를 예방 또는 치료하는 용도로 사용할 수 있음을 알 수 있었다.※ p>0.05: 95% confidence, no statistically significant difference. *p<0.05: 95% confidence, there is a statistically significant difference. As shown in Table 7 above, when compared to the control group, the experimental group using the toothpaste containing each compound of Formulas 1 to 15 passed 2 weeks. After shirin this phenomenon was suppressed. Accordingly, it was found that the compounds of Chemical Formulas 1 to 15 can be used for preventing or treating Shirin.
실험예 5 : 구취 제거 효과Experimental Example 5: Effect of removing bad breath
상기 화학식 1 내지 15의 화합물의 구취 예방 또는 치료 효과를 확인하기 위하여 실험 대상자를 선별하여 임상실험을 수행하였으며, 임상실험에서 사용된 대조군 치약 및 실험군 치약은 상기 실험예 2의 치약과 동일한 방법으로 각각 제조하였다.In order to confirm the effect of preventing or treating halitosis of the compounds of Formulas 1 to 15, clinical trials were conducted by selecting test subjects, and the control toothpaste and the experimental group toothpaste used in the clinical trial were used in the same manner as the toothpaste of Experimental Example 2, respectively. prepared.
실험 대상자로 치아 우식증이 없는 남녀 50명을 선정하여 상기 대조군 치약 및 실험군 치약에 대하여 교차 반복 실험(Cross-over test)을 실시하였다. 시판하는 마늘분을 물에 분산시켜 24시간 방치한 후 희석하여 할리미터(Halimeter) 측정값이 700ppb 이상이 되도록 하고, 상기 희석액을 구취 유발원으로 사용하였다. 실험 대상자들은 마늘분 희석액 15ml로 30초간 가글을 하고, 1분 뒤에 할리미터로 구취 정도를 측정한 후, 대조군은 상기 대조군 치약을, 실험군은 상기 실험군 치약을 각각 사용하여 30초 ~ 1분간 양치질하였다. 양치질 후 1분, 5분, 30분 경과 후 할리미터로 구취 정도를 측정하여 구취억제의 지속여부를 측정하였으며, 그 결과는 하기 표 8에 나타내었다.50 men and women without dental caries were selected as test subjects, and a cross-over test was performed on the toothpaste of the control group and the toothpaste of the experimental group. Commercially available garlic powder was dispersed in water, allowed to stand for 24 hours, and then diluted so that the Halimeter measurement value was 700 ppb or more, and the diluted solution was used as a source of bad breath. The test subjects gargled with 15 ml of garlic powder diluted solution for 30 seconds, and after measuring the degree of bad breath with a Hallimeter 1 minute later, the control group used the control toothpaste and the experimental group used the toothpaste of the experimental group, respectively, for 30 seconds to 1 minute. . After 1 minute, 5 minutes, and 30 minutes after brushing teeth, the degree of bad breath was measured with a hallimeter to determine whether or not the inhibition of bad breath was continued, and the results are shown in Table 8 below.
상기 표 8에 나타난 바와 같이, 대조군과 비교했을 때, 화학식 1 내지 15의 각각의 화합물이 포함된 치약을 사용한 실험군은 양치질 후 1분이 경과한 시점에서 약 95% 이상 구취가 제거되었으며, 양치질 후 30분이 경과하여도 구취 제거율이 80% 이상으로 구취 제거 효과가 대조군에 비해 월등히 우수하였다. 따라서, 화학식 1 내지 15의 화합물은 구취를 예방 또는 치료하는 용도로 사용할 수 있음을 알 수 있었다.As shown in Table 8, compared to the control group, the experimental group using the toothpaste containing each compound of Formulas 1 to 15 had about 95% or more of bad breath removed at 1 minute after gargling, and 30% after gargling. Even after minutes elapsed, the rate of removal of bad breath was more than 80%, and the effect of removing bad breath was significantly superior to that of the control group. Accordingly, it was found that the compounds of Formulas 1 to 15 can be used for preventing or treating bad breath.
Claims (14)
상기 구강 조성물은 스트렙토코커스 뮤탄스(Streptococcus mutans) 또는 포피로모나스 진지발리스(Porphyromonas gingivalis)에 대해 억제 활성을 가지는 것인, 항균용 구강 조성물.
As an antibacterial oral composition comprising Albiflorin or an acceptable salt thereof as an active ingredient,
The oral composition is Streptococcus mutans (Streptococcus mutans) or Porphyromonas gingivalis (Porphyromonas gingivalis) will have an inhibitory activity against, the oral composition for antibacterial.
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KR1020207037855A KR102288921B1 (en) | 2018-05-28 | 2018-05-28 | Composition for prevention or treatment or oral disease |
KR1020217033216A KR102470030B1 (en) | 2018-05-28 | 2018-05-28 | Composition for prevention or treatment or oral disease |
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KR1020217033216A KR102470030B1 (en) | 2018-05-28 | 2018-05-28 | Composition for prevention or treatment or oral disease |
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KR20230065002A (en) | 2021-11-04 | 2023-05-11 | 동의대학교 산학협력단 | Composition for preventing or improving oral diseases comprising an extract of saussurea neoserrata |
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CN112244295A (en) * | 2020-09-17 | 2021-01-22 | 重庆西南果品营养研究院 | New application of hesperetin in preparation of medicine or food for regulating cortisol level of human body |
CN113171309B (en) * | 2021-05-19 | 2022-08-12 | 成都农业科技中心 | Whitening and moisturizing cosmetic composition containing phloretin as well as preparation and application thereof |
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FR2698245B1 (en) * | 1992-11-25 | 1996-08-23 | Int Flavors & Fragrances Inc | USE OF ACONITIC, GLUCONIC AND / OR SUCCINIC ACIDS ALONE OR IN CONJUNCTION WITH SCLAREOLIDE TO INCREASE ORGANOLEPTIC PROPERTIES OF FOOD PRODUCTS. |
US6150381A (en) * | 1998-06-09 | 2000-11-21 | R.J. Reynolds Tobacco Company | Methods of treating microbial infection and therapeutic formulations therefor |
CN100442996C (en) * | 2001-07-19 | 2008-12-17 | 三荣源有限公司 | Flavor-improving compositions and application thereof |
US20030105027A1 (en) | 2001-11-06 | 2003-06-05 | Rosenbloom Richard A. | Nutritional supplements and methods for prevention, reduction and treatment of radiation injury |
US20050032882A1 (en) | 2002-03-06 | 2005-02-10 | Sophie Chen | Botanical extract compositions and methods of use |
JP2004018431A (en) * | 2002-06-14 | 2004-01-22 | Kiyomitsu Kawasaki | Perfume composition for oral cavity and oral cavity composition containing the same |
JP2007091737A (en) | 2005-09-01 | 2007-04-12 | Chieko Tanaka | Oral composition |
CN101534785B (en) * | 2006-07-20 | 2013-03-13 | 国立大学法人冈山大学 | Oral composition for dental purposes |
EP2789369B1 (en) * | 2013-04-14 | 2018-06-06 | Symrise AG | A composition for lightening skin and hair |
US9616124B2 (en) | 2014-07-17 | 2017-04-11 | Jonathan S. Nimitz | Antiviral supplement compositions and methods of use |
CN105146734A (en) * | 2015-08-14 | 2015-12-16 | 贵州中烟工业有限责任公司 | Maotai-flavor tobacco product capable of avoiding burning as being heated and preparation method of tobacco product |
US10780173B2 (en) | 2015-11-09 | 2020-09-22 | Unigen, Inc. | Natural preservatives and antimicrobial agents, including compositions thereof |
KR20170134123A (en) * | 2016-05-27 | 2017-12-06 | 주식회사 엘지생활건강 | Composition for prevention or treatment of dental disease comprising astragaloside |
KR20170141027A (en) * | 2016-06-14 | 2017-12-22 | 주식회사 엘지생활건강 | Composition for prevention or treatment of dental disease comprising an extract of Astragalus membranaceus |
KR101806720B1 (en) * | 2016-07-04 | 2017-12-07 | 배재대학교 산학협력단 | Antibacterial-listeria composition of culture medium containing membranous milkvetch root fermented with lactobacillus plantarum |
KR20180055520A (en) * | 2016-11-17 | 2018-05-25 | 주식회사 엘지생활건강 | Composition for prevention or treatment of oral disease comprising neferine |
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KR20230065002A (en) | 2021-11-04 | 2023-05-11 | 동의대학교 산학협력단 | Composition for preventing or improving oral diseases comprising an extract of saussurea neoserrata |
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JP2022162035A (en) | 2022-10-21 |
KR20210002760A (en) | 2021-01-08 |
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KR102546767B1 (en) | 2023-06-22 |
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JP7412844B2 (en) | 2024-01-15 |
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WO2019230996A1 (en) | 2019-12-05 |
JP2021532062A (en) | 2021-11-25 |
JP7206302B2 (en) | 2023-01-17 |
JP2024038088A (en) | 2024-03-19 |
KR102470030B1 (en) | 2022-11-23 |
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