KR20220107991A - Oral composition for prevention or treatment of oral diseases - Google Patents
Oral composition for prevention or treatment of oral diseases Download PDFInfo
- Publication number
- KR20220107991A KR20220107991A KR1020220011694A KR20220011694A KR20220107991A KR 20220107991 A KR20220107991 A KR 20220107991A KR 1020220011694 A KR1020220011694 A KR 1020220011694A KR 20220011694 A KR20220011694 A KR 20220011694A KR 20220107991 A KR20220107991 A KR 20220107991A
- Authority
- KR
- South Korea
- Prior art keywords
- composition
- oral
- present
- oral use
- menthol
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 85
- 230000002265 prevention Effects 0.000 title description 2
- 208000025157 Oral disease Diseases 0.000 title 1
- 208000030194 mouth disease Diseases 0.000 title 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims abstract description 44
- 229940041616 menthol Drugs 0.000 claims abstract description 44
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims abstract description 41
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims abstract description 36
- 235000005911 diet Nutrition 0.000 claims abstract description 36
- 230000000378 dietary effect Effects 0.000 claims abstract description 36
- 229910052717 sulfur Inorganic materials 0.000 claims abstract description 36
- 239000011593 sulfur Substances 0.000 claims abstract description 36
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims description 30
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 30
- 229920000858 Cyclodextrin Polymers 0.000 claims description 21
- 229940016409 methylsulfonylmethane Drugs 0.000 claims description 21
- HHVIBTZHLRERCL-UHFFFAOYSA-N sulfonyldimethane Chemical compound CS(C)(=O)=O HHVIBTZHLRERCL-UHFFFAOYSA-N 0.000 claims description 21
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 18
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 17
- 239000001569 carbon dioxide Substances 0.000 claims description 15
- 229910002092 carbon dioxide Inorganic materials 0.000 claims description 15
- 150000007524 organic acids Chemical class 0.000 claims description 12
- 230000000844 anti-bacterial effect Effects 0.000 claims description 11
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 10
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims description 10
- FGIUAXJPYTZDNR-UHFFFAOYSA-N potassium nitrate Chemical compound [K+].[O-][N+]([O-])=O FGIUAXJPYTZDNR-UHFFFAOYSA-N 0.000 claims description 10
- 241000605862 Porphyromonas gingivalis Species 0.000 claims description 9
- 229910000027 potassium carbonate Inorganic materials 0.000 claims description 9
- 235000011181 potassium carbonates Nutrition 0.000 claims description 9
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- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 6
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims description 5
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- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical group [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims description 5
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- 239000001508 potassium citrate Substances 0.000 claims description 4
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
- A61K8/466—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur containing sulfonic acid derivatives; Salts
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/738—Cyclodextrins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
- A61Q17/005—Antimicrobial preparations
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/56—Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms
Abstract
Description
본 발명은 구강용 조성물에 관한 것이다. 더 상세하게는 불소, 칼륨 등 유효 성분의 침투를 촉진하여 치료 및 예방 효과를 갖는 구강용 조성물을 제공하는 것이다.The present invention relates to a composition for oral use. More specifically, it is to provide a composition for oral cavity having therapeutic and preventive effects by promoting penetration of active ingredients such as fluorine and potassium.
치아의 지각과민증은 치아우식증이나 치아파절, 치주질환처럼 구체적으로 분류된 원인에 의한 것이 아니라 노출된 상아질 부위에서 증기압, 삼투압, 화학물질, 온도 변화 등 외부 자극에 의해 짧고 날카롭게 발생하는 통증을 특징으로 한다. 상아질의 노출은 치은퇴축이나 치아표면층(주로 법랑질) 상실의 결과물이고 치은퇴축은 과도한 양치질, 부적절한 양치방법, 치주질환, 치주치료 등에 의해 발생한다. 치아 표면층 상실은 산성 음식물의 섭취에 의한 부식과 과도한 교합력에 의해 특히 치경부에서 마모형태로 관찰된다. 이중에서 상아질 지각과민증은 치경부 법랑질 상실보다 치은퇴축으로 상아세관이 노출되는 것을 큰 원인으로 보고되고 있다.Tooth hypersensitivity is characterized by short and sharp pain that is caused by external stimuli such as vapor pressure, osmotic pressure, chemical substances, and temperature changes in the exposed dentin area, not due to specific causes such as dental caries, tooth fracture, or periodontal disease. do. Exposure of dentin is the result of gingival recession or loss of the tooth surface layer (mainly enamel). Tooth surface layer loss is observed in the form of wear, especially in the cervical region, due to corrosion caused by ingestion of acidic food and excessive occlusal force. Among them, dentin hypersensitivity is reported to be the major cause of exposure of dentinal tubules due to gingival recession rather than cervical enamel loss.
지금까지 상아질 지각과민증을 해결하기 위한 꾸준한 노력이 있었다. 특허문헌을 통하여 수산화인회석(hydroxy apatite)(독일특허 제2,134,862호), 염화스트론튬(미국등록특허 제3,122,483호), 포타슘 나이트레이트(미국등록특허 제4,357,318호) 등이 과민성 치아의 치료를 위한 민감신경 완화제로서 보고되어 왔다.Until now, there have been steady efforts to solve dentin hypersensitivity. Through the patent literature, hydroxy apatite (German Patent No. 2,134,862), strontium chloride (US Patent No. 3,122,483), potassium nitrate (US Patent No. 4,357,318), etc. are sensitive nerves for the treatment of hypersensitive teeth. It has been reported as an emollient.
한편 노출된 상아세관은 특별한 치료 없이도 시간이 지나면서 차츰 막히고 과민증은 없어진다. 이런 과정은 단백질 성분과 타액에서 유래하는 인산칼슘 성분들이 어우러져 스미어레이어 형태로 상아세관을 막아주는 것으로 설명된다. 하지만, 과민증이 없어지는데 긴 시간이 필요하고, 상아세관을 막은 스미어레이어는 산성 성분이나 킬레이션 반응과 어울려진 칫솔질 등에 의해 다시 쉽게 제거되기 때문에 다시 과민증이 재발하는 문제가 있다.On the other hand, the exposed dentinal tubules gradually become clogged over time without special treatment, and the hypersensitivity disappears. This process is explained by the combination of protein components and calcium phosphate components derived from saliva to block the dentinal tubule in the form of a smear layer. However, it takes a long time for hypersensitivity to disappear, and since the smear layer that has blocked the dentinal tubule is easily removed again by brushing in combination with an acidic component or a chelation reaction, there is a problem that hypersensitivity recurs.
최근에는 타액에 상아세관 밀폐를 모사하는 것과 비슷한 방법으로 아르기닌 8%와 탄산칼슘, 불소의 조합으로 과민성 치아를 치료하는 방법이 각광받고 있다. Kleinberg 에 의하면 아르기닌과 탄산칼슘의 조합은 양전하를 띄기 때문에 음전하를 띄는 상아세관 입구에 쉽게 결합할 수 있고, 그 pH가 염기성이라서 타액이나 조직액에 포함된 칼슘과 인 성분의 침착을 유도하여 상아세관 밀폐를 더 촉진하는 것으로 설명한다.Recently, a method of treating hypersensitive teeth with a combination of 8% arginine, calcium carbonate, and fluoride in a similar way to mimicking dentinal tubule sealing in saliva has been in the spotlight. According to Kleinberg, the combination of arginine and calcium carbonate has a positive charge, so it can easily bind to the negatively charged entrance to the dentinal tubule. is explained as further promoting
그러나 2018년도에 Mohammed Nadeem Ahmed Bijle 등에 따른 논문에서 확인할 수 있듯, 불소 함량이 일정한 상태에서 아르기닌의 함량이 2% 일 때 우식균에 대한 항바이오필름 효능이 높고 법랑질 손상을 회복하는 것으로 나타나며, 오히려 아르기닌 함량이 증가할 수록 우식을 억제하고 예방하는 효과는 떨어진다.However, as can be seen in the paper by Mohammed Nadeem Ahmed Bijle et al. in 2018, when the content of arginine is 2% under a constant fluorine content, the anti-biofilm efficacy against caries bacteria is high and it appears that enamel damage is restored. As the content increases, the effect of inhibiting and preventing caries decreases.
그리고 칼슘과 인산의 침착은 상아세관을 폐쇄해서 시린 증상을 억제하는 순기능도 있지만 치태 및 치석의 침착을 가속화 하는 문제가 있다. 이는 특히 일반적으로 판매되는 시린이 치약들에 연마제가 없다는 사실을 생각하면 심각한 문제가 된다.In addition, the deposition of calcium and phosphoric acid has a positive function of suppressing the symptoms of soreness by closing the dentinal tubules, but there is a problem of accelerating the deposition of plaque and tartar. This is a serious problem, especially given the fact that commonly sold syrin toothpastes do not contain abrasives.
가장 보편적인 전국민 의료보험 제도를 실시하는 한국의 의료 빅데이터를 분석한 2017년 논문에 의하면 칼륨 섭취는 산 부담 (acid load) 을 중화하고 뼈에서 칼슘 손실을 줄여서 노인층과 폐경 여성들에서 골밀도가 좋아지는 바람직한 결과를 가져왔다고 한다. 같은 원리로 충치균(s. mutants)이나 치주질환균 (p.gingivalis)에서 만들어지는 산에 의한 치아와 치주조직에서의 칼슘 손실을 줄일 수 있다면 치아우식증 뿐 아니라 치은퇴축에 의한 지각과민증 억제에 큰 도움을 줄 수 있다는 전제하에 연구를 집중하였다.According to a 2017 paper analyzing medical big data in Korea, which implements the most common national health insurance system, potassium intake neutralizes acid load and reduces calcium loss from bones, leading to improved bone density in the elderly and postmenopausal women. It is said to have produced favorable results. According to the same principle, if calcium loss in teeth and periodontal tissues caused by acid produced by s. mutants or periodontal disease bacteria ( p.gingivalis ) can be reduced, it is of great help in suppressing not only dental caries but also hypersensitivity caused by gingival recession. The research was focused on the premise that
메틸설포닐메탄 (Methylsulfonylmethane; 이하 MSM)은 식이유황에 속하는 화학식 (CH3)2SO2를 갖는 유기 황화합물이다. 이 무색 고체는 설포닐 작용기를 특징으로 하며 화학적으로 불활성인 것으로 간주되고 일부 원시 식물에서 자연적으로 발생하며, 많은 음식과 음료에 소량 존재하며 식이보충제로 판매된다. MSM의 발표된 임상 시험은 심각한 부작용을 보고하지 않았지만 인간에 대한 장기적인 효과에 대한 명확한 데이터는 없다. 국소치료제로 포함하는 경우, MSM이 피부 투과를 촉진하는 역할을 하는 것이 알려져 있고, 안약의 침투성분이나 모발성장 촉진제에서 두피침투 성분으로 사용된다. 출원특허 EP2934694A4에서 MSM과 EDTA의 조합으로 치태 침착을 제거하는데 효과적이라는 구강 조성물이 제안되었다. 등록특허 EP2493464A1 에서 MSM과 항생제의 조합으로 항생제 내성균에 대해 효과적이라는 조성물이 제안되었으며 이때 MSM의 양은 전체 조성물의 5~20% 범위이다. 등록특허 US9487749B2 는 MSM의 양이 5% 이하에서 유효 미생물의 생장을 촉진하고, 그 이상에서 특정 바이러스의 생장을 억제하는 효과를 이용하는 방법이 제안되었다.Methylsulfonylmethane (Methylsulfonylmethane; hereinafter MSM) is an organic sulfur compound having the formula (CH 3 ) 2 SO 2 belonging to dietary sulfur. This colorless solid is characterized by sulfonyl functionality, is considered chemically inert, occurs naturally in some primitive plants, is present in small amounts in many foods and beverages, and is sold as a dietary supplement. Published clinical trials of MSM have reported no serious side effects, but there are no definitive data on long-term effects in humans. When included as a topical treatment, it is known that MSM plays a role in promoting skin permeation, and it is used as a penetrating component of eye drops or a scalp penetrating component in hair growth promoters. In the patent application EP2934694A4, a combination of MSM and EDTA was proposed to be effective in removing plaque deposits. In Patent Registration EP2493464A1, a composition that is effective against antibiotic-resistant bacteria as a combination of MSM and antibiotics is proposed, and the amount of MSM is in the range of 5 to 20% of the total composition. Registered Patent US9487749B2 proposes a method using the effect of promoting the growth of effective microorganisms when the amount of MSM is 5% or less, and inhibiting the growth of a specific virus above it.
멘톨은 페퍼민트 등의 박하속 식물에 다량으로 함유되어 있는 유기화합물로 상온에서 투명하고 기름진 결정형태로 존재하며 제약업계에서 이미프라민이나 paeoniflorin의 침투촉진성분으로 사용되고 있다.Menthol is an organic compound contained in a large amount in peppermint and other peppermint plants. It exists in the form of transparent and oily crystals at room temperature. It is used as a penetration promoting component of imipramine or paeoniflorin in the pharmaceutical industry.
사이클로덱스트린(Cyclodextrin; CD)은 글루코피라노우즈(glucopyranose) 단위들이 α-(1,4) 결합을 하고 있는 고리형 올리고사카라이드(oligosaccharide)로, 대표적으로 6개 단위의 α-사이클로덱스트린, 7개 단위의 β-사이클로덱스트린, 8개 단위의 γ-사이클로덱스트린 등이 있다.Cyclodextrin (CD) is a cyclic oligosaccharide in which glucopyranose units are α-(1,4) bonds, typically 6 units of α-cyclodextrin, 7 units units of β-cyclodextrin, 8 units of γ-cyclodextrin, and the like.
또한, 물에 대한 용해도를 높이기 위해 하이드록시프로필- β-CD와 같이 하이드록시알킬화하거나 메톡시알킬화한 다양한 유도체들이 있다.In addition, there are various hydroxyalkylated or methoxyalkylated derivatives such as hydroxypropyl-β-CD to increase solubility in water.
사이클로덱스트린은 녹말이 cyclodextrin glucanotransferase(CGTase)라는 효소에 의해 분해되어 분자간 transglycosylation 반응에 의해 얻어진다. 1891년에 발견되어 발전해왔으며 여러 화합물과 포접(inclusion), 복합물(complex)을 형성하는 특성이 발견된 이후 많은 연구가 진행되고 있다. X-ray 구조분석에 의하면 사이클로덱스트린의 외곽은 친수성을 띄고 내부는 소수성 특성을 띈다. 친수성 외곽의 특성으로 물과 같은 극성 용매에 잘 녹게 되고, 내부의 소수성 특성은 분자 내부에 분자크기의 기공을 형성하게 되어, 한 분자 내에 서로 다른 특성을 갖고 있는 micro heterogeneous environment를 갖게 된다. 미국등록특허 US20040076591A1 에서 멘톨 등 폐놀계 항균화합물을 용해시키는 목적으로 사이클로덱스트린을 사용하여 알코올 함량을 낮춘 구강관리 조성물로서 치태 발생을 지연시키고, 치은염을 치료하고, 구강 내 미생물의 존재를 치료하는 구강 조성물의 설명이 있다.Cyclodextrins are obtained by intermolecular transglycosylation by decomposing starch by an enzyme called cyclodextrin glucanotransferase (CGTase). It was discovered and developed in 1891, and many studies have been conducted after the discovery of the properties of forming various compounds, inclusions, and complexes. According to X-ray structural analysis, the outside of the cyclodextrin is hydrophilic and the inside is hydrophobic. Because of the hydrophilic exterior characteristics, it is easily soluble in polar solvents such as water, and the internal hydrophobic characteristics form molecular-sized pores inside the molecule, creating a micro heterogeneous environment with different characteristics within a molecule. According to US Patent US20040076591A1, an oral care composition in which alcohol content is lowered by using cyclodextrin for the purpose of dissolving phenolic antibacterial compounds such as menthol, which delays the occurrence of plaque, treats gingivitis, and treats the presence of microorganisms in the oral cavity. There is an explanation of
본 발명의 목적은 불소, 칼륨 등 유효 성분의 침투를 촉진하여 치료 및 예방 효과를 갖는 구강용 조성물을 제공하는 것이다.It is an object of the present invention to provide a composition for oral cavity having therapeutic and preventive effects by promoting penetration of active ingredients such as fluorine and potassium.
1. 이산화탄소 분위기 하에 식이유황 및 멘톨이 포접된 사이클로덱스트린을 포함하는 구강용 조성물.1. An oral composition comprising a cyclodextrin containing dietary sulfur and menthol in a carbon dioxide atmosphere.
2. 위 1에 있어서, 상기 식이유황은 메틸설포닐메탄(methyl-sulfonylmethane; MSM), 디메틸설폭사이드(dimethyl sulfoxide)로 이루어진 군에서 선택되는 적어도 하나인 구강용 조성물.2. The composition for oral use according to the above 1, wherein the dietary sulfur is at least one selected from the group consisting of methyl-sulfonylmethane (MSM) and dimethyl sulfoxide.
3. 위 1에 있어서, 상기 이산화탄소는 탄산염과 유기산의 반응으로 발생하는 구강용 조성물.3. The composition for oral use according to the above 1, wherein the carbon dioxide is generated by the reaction of carbonate and organic acid.
4. 위 3에 있어서, 상기 탄산염은 중탄산칼륨 탄산칼륨, 탄산나트륨, 중탄산나트륨으로 이루어진 군에서 적어도 하나 이상을 포함하는 구강용 조성물.4. The composition for oral use according to the above 3, wherein the carbonate includes at least one or more from the group consisting of potassium bicarbonate, potassium carbonate, sodium carbonate, and sodium bicarbonate.
5. 위 3에 있어서, 상기 유기산은 구연산 및 개미산 중에서 적어도 하나 이상을 포함하는 구강용 조성물.5. The composition for oral use according to the above 3, wherein the organic acid comprises at least one of citric acid and formic acid.
6. 위 1에 있어서, 상기 식이유황은 상기 조성물 전체에 대해 1 중량% 내지 5 중량%로 포함된 구강용 조성물.6. The composition for oral use according to 1 above, wherein the dietary sulfur is included in an amount of 1% to 5% by weight based on the total composition.
7. 위 1에 있어서, 상기 멘톨은 상기 조성물 전체에 대해 0.5 중량% 내지 1.5 중량%로 포함된 구강용 조성물.7. The composition for oral use according to the above 1, wherein the menthol is included in an amount of 0.5 wt% to 1.5 wt% with respect to the total composition.
8. 위 1에 있어서, 구연산칼륨, 질산칼륨, 포름산칼륨에서 이루어진 군에서 적어도 하나를 더 포함하는 구강용 조성물.8. The composition for oral use according to the above 1, further comprising at least one from the group consisting of potassium citrate, potassium nitrate, and potassium formate.
9. 위 1에 있어서, 상기 조성물은 인체에 안전하면서 스트렙토코커스 뮤턴스 균주 (Streptococcus mutans)와 포르피로모나스 긴기발리스 균주(Porphyromonas gingivalis) 에 항균 효과가 있는 것을 특징으로 하는 구강용 조성물.9. The composition for oral use according to the above 1, characterized in that it has an antibacterial effect on Streptococcus mutans and Porphyromonas gingivalis while being safe for the human body.
본 발명을 통해 유효 성분의 침투력을 향상한 구강용 조성물을 제공한다.The present invention provides a composition for oral use with improved penetration of the active ingredient.
본 발명의 구강용 조성물을 통해 치아우식증이나 치주질환을 일으키는 원인균을 제거하는데 효과적인 조성물을 제공한다.To provide an effective composition for removing the causative bacteria causing dental caries or periodontal disease through the oral composition of the present invention.
이하 본 발명을 상세히 설명한다. 특별한 정의가 없는 한 본 명세서의 모든 용어는 본 발명이 속하는 기술분야의 통상의 지식을 가진 기술자가 이해하는 당해 용어의 일반적인 의미와 동일하고 만약 본 명세서에 사용된 용어의 의미와 충돌하는 경우에는 본 명세서에 사용된 의미를 따른다.Hereinafter, the present invention will be described in detail. Unless otherwise defined, all terms in this specification have the same general meaning as understood by those of ordinary skill in the art to which the present invention belongs, and in case of conflict with the meaning of the terms used in this specification, the The meaning used in the specification is followed.
본 발명은 이산화탄소 분위기 하에 식이유황 및 멘톨이 포접된 사이클로덱스트린을 포함하는 구강용 조성물에 관한 것이다.The present invention relates to a composition for oral use comprising a cyclodextrin containing dietary sulfur and menthol in a carbon dioxide atmosphere.
본 발명에서 식이유황은 천연 유기황 화합물이다. 강한 친수성 물질로써 물에 대한 용해력이 아주 높으며, 같이 있는 이온의 침투성을 높여, 치주조직과 치아의 상아세관에 유용한 이온의 전달을 돕는 역할을 한다. 칼륨염 성분과 함께 치주조직에 전달될 경우, 전달된 칼륨 이온이 치조골이나 상아세관 주변의 칼슘 이온이 빠져 나오는 것을 억제하여 치은퇴축을 완화하고 상아세관의 밀폐를 유지하여 시린이 증상을 완화하는 효과를 나타낼 수 있다. In the present invention, dietary sulfur is a natural organic sulfur compound. As a strong hydrophilic material, it has very high solubility in water and increases the permeability of ions present, helping to transfer useful ions to periodontal tissue and dentin tubules of teeth. When delivered to periodontal tissue together with potassium salt components, the delivered potassium ions inhibit the calcium ions from escaping from the alveolar bone or dentinal tubules, thereby alleviating gingival recession and maintaining the seal of the dentinal tubules, thereby relieving the symptoms of pain. can represent
본 발명에서 상기 식이유황은 메틸설포닐메테인(methylsulfonylmethane, 이하 MSM), 디메틸설폭사이드(dimethyl sulfoxide)로 이루어진 군에서 선택될 수 있다. 다만 이에 제한되지 않는다.In the present invention, the dietary sulfur may be selected from the group consisting of methylsulfonylmethane (MSM) and dimethyl sulfoxide. However, the present invention is not limited thereto.
본 발명에서 상기 식이유황은 상기 구강용 조성물 전체에 대해 0.1 중량% 내지 10 중량%으로 포함될 수 있다. 본 발명의 일 실시예에서, 상기 식이유황은 2.2 중량% 내지 3.3 중량%로 포함된다.In the present invention, the dietary sulfur may be included in an amount of 0.1% to 10% by weight based on the total composition for oral use. In one embodiment of the present invention, the dietary sulfur is included in an amount of 2.2 wt% to 3.3 wt%.
본 발명에서 멘톨은 페퍼민트 등의 박하속 식물에 다량으로 함유되어 있는 유기화합물로 상온에서 투명하고 기름진 결정형태로 존재하며 제약업계에서 이미프라민이나 paeoniflorin의 침투촉진성분으로 사용되고 있다. 본 발명에서 멘톨은 투과 특성으로 지각과민 완화 활성화 물질(구연산칼륨, 질산칼륨 등)을 상아세관 깊숙히 전달하여 효과적으로 기능하도록 도와준다. 특히 식이유황과 함께 사용할 경우 칼륨 이온의 전달 효과를 현저하게 증가시킬 수 있다.In the present invention, menthol is an organic compound contained in a large amount in peppermint plants, such as peppermint, and exists in the form of transparent and oily crystals at room temperature, and is used as a penetration promoting component of imipramine or paeoniflorin in the pharmaceutical industry. In the present invention, menthol helps to effectively function by delivering hypersensitivity relief activating substances (potassium citrate, potassium nitrate, etc.) deep into the dentinal tubule due to its permeation properties. In particular, when used together with dietary sulfur, the transfer effect of potassium ions can be significantly increased.
본 발명에서 상기 멘톨은 상기 구강용 조성물 전체에 대해 0.1 중량% 내지 10 중량%로 포함될 수 있으며, 예를 들어 0.1 중량% 내지 5 중량% 또는 0.1 중량% 내지 3 중량%로 포함될 수 있다. 본 발명의 일 실시예에서, 상기 멘톨은 0.5 중량% 내지 1.6 중량%로 포함된다.In the present invention, the menthol may be included in an amount of 0.1 wt% to 10 wt%, for example, 0.1 wt% to 5 wt% or 0.1 wt% to 3 wt%, based on the total composition for oral use. In one embodiment of the present invention, the menthol is included in 0.5 wt% to 1.6 wt%.
본 발명의 일 실시예에서, 식이유황과 멘톨을 포함하는 구강용 조성물을 사용하면 칼륨염 및 불소 화합물을 치아 경조직에 침투시켜 충치를 억제하는 동시에, 상기 칼륨염을 치주조직 깊이 침투시켜 칼슘의 균형 유지를 통한 치조골의 골밀도를 개선함으로써 치은퇴축을 억제하는 방식으로 시린이 억제 효과를 보일 수 있다. 또한, 식이유황과 멘톨이 조합되는 경우, 치아 및 치주질환을 유발하는 유해균에 대한 항균효과가 있음을 확인하였다.In one embodiment of the present invention, when an oral composition containing dietary sulfur and menthol is used, potassium salt and a fluorine compound are penetrated into the tooth hard tissue to suppress tooth decay, and at the same time, the potassium salt penetrates deeply into the periodontal tissue to balance calcium By improving the bone density of the alveolar bone through maintenance, shirin can show an inhibitory effect by suppressing gingival recession. In addition, when dietary sulfur and menthol were combined, it was confirmed that there was an antibacterial effect against harmful bacteria that cause teeth and periodontal disease.
상기 치아 및 치주질환을 유발하는 유해균은 치아우식증원인균인 스트렙토코쿠스 뮤탄스(Streptococcus mutans), 스트렙토코쿠스 소브리누스(Streptococcus sobrinus) 및 치주질환원인균인 포르피노모나스 간기발리스(Porphyromonas gingivalis), 프레보텔라 인터미디아 (Prevotella intermedia), 후소박테리움 뉴클레아툼(Fusobacterium nucleatum) 로 이루어진 군에서 선택되는 어느 하나 이상의 균일 수 있다.The harmful bacteria that cause tooth and periodontal disease are Streptococcus mutans, Streptococcus mutans , Streptococcus sobrinus , and Porphyromonas gingivalis , which is a causative bacteria of periodontal disease. Prevotella intermedia ( Prevotella intermedia ), Fusobacterium nucleatum ( Fusobacterium nucleatum ) Any one or more selected from the group consisting of may be uniform.
그러나 유효량의 식이유황과 멘톨을 구강 조성물에 포함하는 것은 맛과 향이 지나치게 강하고 자극적이어서 사용자에게 심한 불쾌감과 통증을 줄 수 있어 그 사용이 제한된다. However, the inclusion of effective amounts of dietary sulfur and menthol in the oral composition is too strong and irritating in taste and flavor, which may give severe discomfort and pain to the user, thus limiting its use.
본 발명에서 사이클로덱스트린과 이산화탄소는 침투촉진 성분인 멘톨 및 식이유황과 반응하여 식이유황의 자극적인 맛과 향을 순화하고 멘톨의 가용화 및 안정성 향상을 위해 포함된다. 사이클로덱스트린은 산화, 수분, 열, 동결에 의해 변성되고 분해되는 불안정한 물질의 안정화에 사용되고, 좋지 않은 맛이나 냄새의 감소작용을 한다. 또한 오일 물질의 유화, 물에 녹지 않는 물질의 가용화에 사용되며 본 발명에서 멘톨의 안정성 향상 및 가용화를 위해 포함된다. 특히 β-사이클로덱스트린으로 포접된 멘톨은 안정성이 향상되고 조직 내에 더 효과적으로 침투한다.In the present invention, cyclodextrin and carbon dioxide react with menthol and dietary sulfur, which are penetration promoting ingredients, to purify the stimulant taste and flavor of dietary sulfur, and to solubilize and improve stability of menthol. Cyclodextrin is used for stabilization of unstable substances that are denatured and decomposed by oxidation, moisture, heat, and freezing, and acts to reduce bad taste or odor. It is also used for emulsification of oily substances, solubilization of substances insoluble in water, and is included for improving stability and solubilization of menthol in the present invention. In particular, menthol encapsulated with β-cyclodextrin improves stability and penetrates into tissues more effectively.
본 발명에서 사이클로덱스트린은 상기 구강용 조성물 전체에 대해 1 중량% 내지 20 중량%로 포함될 수 있으며, 예를 들어 5 중량% 내지 15 중량% 또는 7 중량% 내지 13 중량%로 포함될 수 있다. 본 발명의 일 실시예에서, 상기 사이클로덱스트린은 10 중량%로 포함된다.In the present invention, the cyclodextrin may be included in an amount of 1% to 20% by weight, for example, 5% to 15% by weight or 7% to 13% by weight based on the total composition for oral use. In one embodiment of the present invention, the cyclodextrin is included in an amount of 10% by weight.
본 발명에서 이산화탄소는 멘톨과 사이클로덱스트린의 포접단계에서 직접 주입하거나 혹은 탄산염과 유기산의 반응산물로 발생하는 이산화탄소를 이용할 수 있다. 이산화탄소 분위기에서 사이클로덱스트린에 식이유황과 멘톨을 반응시키면 맛과 향이 부드러워질 뿐 아니라, 가용성이 증가하고 침투력이 더욱 좋아질 수 있다. In the present invention, carbon dioxide may be directly injected in the inclusion step of menthol and cyclodextrin, or carbon dioxide generated as a reaction product of carbonate and organic acid may be used. When dietary sulfur and menthol are reacted with cyclodextrin in a carbon dioxide atmosphere, not only the taste and flavor become soft, but also the solubility increases and the penetrability can be improved.
본 발명에서 탄산염은 탄산나트륨, 중탄산나트륨, 탄산칼륨, 중탄산칼륨 에서 선택되는 염일 수 있으며, 바람직하게는 칼륨을 포함하는 염 중에서 선택될 수 있다. 다만, 이에 제한되지 않는다.In the present invention, the carbonate may be a salt selected from sodium carbonate, sodium bicarbonate, potassium carbonate, and potassium bicarbonate, preferably selected from salts containing potassium. However, the present invention is not limited thereto.
본 발명에서 유기산은 구연산, 초산, 주석산, 말레인산, 푸마르산, 개미산, 프로피온산, 옥살산, 벤조산, 글루콘산, 메타술폰산, 글리콜산, 숙신산, 4-톨루엔술폰산, 글루탐산 및 아스파르트산 일 수 있다. 본 발명의 일 실시예에서, 유기산은 구연산이나 개미산중에서 선택될 수 있다. 다만, 이에 제한되지 않는다.In the present invention, the organic acid may be citric acid, acetic acid, tartaric acid, maleic acid, fumaric acid, formic acid, propionic acid, oxalic acid, benzoic acid, gluconic acid, metasulfonic acid, glycolic acid, succinic acid, 4-toluenesulfonic acid, glutamic acid and aspartic acid. In one embodiment of the present invention, the organic acid may be selected from citric acid or formic acid. However, the present invention is not limited thereto.
본 발명에서 상기 유기산은 상기 구강용 조성물 전체에 대해 0.1 중량% 내지 10 중량%로 포함될 수 있다. 본 발명의 일 실시예에서, 상기 구연산은 8.0 중량%로 포함된다.In the present invention, the organic acid may be included in an amount of 0.1 wt% to 10 wt% based on the total composition for oral use. In one embodiment of the present invention, the citric acid is included in 8.0% by weight.
본 발명의 구강용 조성물은 알칼리 금속염을 더 포함할 수 있다. The composition for oral cavity of the present invention may further contain an alkali metal salt.
알칼리 금속염은 세공 내로 침투하여 치아와 치조골 칼슘 이온 방출을 감소시켜 칼슘 균형 유지에 도움을 준다. 즉 칼슘이온이 경조직에서 빠져 나오는 것을 방지하는 역할을 한다. 이는 지각과민을 완화시킬 수 있으며, 시린이 예방 및 치료 효과를 나타낼 수 있다.Alkali metal salts penetrate into the pores and reduce the release of calcium ions from teeth and alveolar bone, helping to maintain calcium balance. That is, it serves to prevent calcium ions from escaping from the hard tissue. This can alleviate hypersensitivity, and shirin can have a preventive and therapeutic effect.
상기 알칼리 금속염은 구강용 조성물에 사용될 수 있는 것이라면 제한 없이 사용될 수 있으며, 예를 들면 칼륨염일 수 있다.The alkali metal salt may be used without limitation as long as it can be used in the oral composition, for example, may be a potassium salt.
본 발명에서 상기 칼륨염은 구연산 칼륨, 질산칼륨, 염화칼륨, 인산2수소칼륨, 황산칼륨, 탄산칼륨, 탄산수소칼륨 중에서 선택된 하나 혹은 조합일 수 있다. 다만, 이에 제한되지 않는다.In the present invention, the potassium salt may be one or a combination selected from potassium citrate, potassium nitrate, potassium chloride, potassium dihydrogen phosphate, potassium sulfate, potassium carbonate, and potassium hydrogen carbonate. However, the present invention is not limited thereto.
본 발명에서 상기 알칼리 금속염은 상기 구강용 조성물 전체에 대해 4.0 중량% 내지 20.0 중량%로 포함될 수 있다. 본 발명의 일 실시예에서, 상기 칼륨염은 8.0 중량%로 포함된다.In the present invention, the alkali metal salt may be included in an amount of 4.0 wt% to 20.0 wt% based on the total composition for oral use. In one embodiment of the present invention, the potassium salt is included in 8.0% by weight.
본 발명의 구강용 조성물은 불소 화합물 또는 불소 이온을 더 포함할 수 있다.The composition for oral cavity of the present invention may further contain a fluorine compound or a fluorine ion.
불소 화합물 또는 불소 이온은 치아의 수산화인회석과 반응 하여 불화아파타이트를 형성하는데, 이는 치아의 대표적인 구성성분인 수산화인회석보다 침에 덜 녹고 산성 조건에도 잘 견디는 특징이 있다. 또한, 불소 화합물 또는 불소 이온은 균을 억제하며 젖산의 발생을 감소시키므로, 불소 화합물 또는 불소 이온을 구강용 조성물에 사용시 충치 예방 효과가 뛰어나다. Fluoride compounds or fluoride ions react with hydroxyapatite in teeth to form fluorapatite, which is less soluble in saliva and more resistant to acidic conditions than hydroxyapatite, a typical component of teeth. In addition, since the fluorine compound or fluoride ion inhibits bacteria and reduces the generation of lactic acid, when the fluorine compound or fluorine ion is used in an oral composition, the caries prevention effect is excellent.
본 발명에서 상기 불소 화합물은 불화나트륨, 불화제1주석, 모노플루오로인산나트륨, 불화칼륨, 칼륨 주석 플루오라이드, 불화주석산나트륨, 염화불화주석, 불화아민 및 이의 혼합물을 포함한다. 다만, 이에 제한되지 않는다.In the present invention, the fluorine compound includes sodium fluoride, stannous fluoride, sodium monofluorophosphate, potassium fluoride, potassium tin fluoride, sodium stannate fluoride, tin chloride fluoride, amine fluoride, and mixtures thereof. However, the present invention is not limited thereto.
본 발명의 구강용 조성물은 구강용 조성물의 제조에 통상적으로 사용하는 적절한 본 발명의 구강용 조성물은 연마제, 방부제, 습윤제, 방향제 또는 항균제 등을 추가로 포함할 수 있다.The composition for oral use of the present invention may further include an abrasive, an antiseptic, a wetting agent, a fragrance, or an antibacterial agent.
본 발명의 구강용 조성물은 치약, 구강용 세정제, 구강 청정제, 구강 스프레이 또는 구강 양치액 제형을 포함할 수 있다. 다만, 이에 제한되지 않는다.The composition for oral use of the present invention may include a toothpaste, mouthwash, mouthwash, oral spray, or mouthwash formulation. However, the present invention is not limited thereto.
본 발명의 일 실시예에서, 구강용 조성물은 MSM, 아르기닌, 탄산칼륨, 구연산, 멘톨, 불화나트륨, 솔비톨, 에리스리톨, 사이클로덱스트린, 레몬 에센셜오일, 스피아민트 오일, 페퍼민트 에센셜오일, 티트리 에센셜오일, 수크랄로스, 폴리비닐피롤리돈, 잔탄검, 라우릴글루코사이드, 소듐코코일글루타메이트를 포함할 수 있다. 다만, 이에 제한되지 않는다.In one embodiment of the present invention, the composition for oral use includes MSM, arginine, potassium carbonate, citric acid, menthol, sodium fluoride, sorbitol, erythritol, cyclodextrin, lemon essential oil, spearmint oil, peppermint essential oil, tea tree essential oil, sucralose, polyvinylpyrrolidone, xanthan gum, lauryl glucoside, sodium cocoyl glutamate. However, the present invention is not limited thereto.
본 발명의 구강용 조성물은 치주 질환의 예방 또는 치료 보조 효과를 가질 수 있다. 구체적으로, 상기 치주질환은 시린이, 치아우식증, 치은염, 치주염, 치조골 파손, 치조골 골다공증, 치조골 연화증, 치조골 감소증, 치조골 재형성 장애 및 구취 등을 포함할 수 있다. 다만, 이에 제한되지 않는다.The composition for oral use of the present invention may have a preventive or therapeutic auxiliary effect of periodontal disease. Specifically, the periodontal disease may include toothache, dental caries, gingivitis, periodontitis, alveolar bone damage, alveolar osteoporosis, alveolar osteomalacia, alveolar osteopenia, alveolar bone remodeling disorder, and bad breath. However, the present invention is not limited thereto.
본 발명에 따른 구강용 조성물은 개별 사용하거나 다른 구강용 치료제와 병용하여 사용될 수 있고 종래의 치료제 등과 순차적 또는 동시에 사용될 수 있으며, 단일 또는 다중 사용될 수 있다. 상기한 요소들을 모두 고려하여 부작용 없이 최소한의 양으로 최대 효과를 얻을 수 있는 양을 사용하는 것이 중요하며, 이는 통상의 기술자에 의해 용이하게 결정될 수 있다.The oral composition according to the present invention may be used individually or in combination with other oral therapeutic agents, may be used sequentially or simultaneously with conventional therapeutic agents, and may be used singly or multiple times. In consideration of all of the above factors, it is important to use an amount that can obtain the maximum effect with a minimum amount without side effects, which can be easily determined by a person skilled in the art.
구체적으로 본 발명의 구강용 조성물의 유효량은 환자의 연령, 성별, 상태, 체중, 체내에 활성 성분의 흡수도, 불활성율 및 배설속도, 질병종류, 병용되는 약물에 따라 달라질 수 있다. 다만, 사용하는 환자의 조건에 따라 달라질 수 있으므로, 특정 유효량에 제한되지 않는다.Specifically, the effective amount of the composition for oral use of the present invention may vary depending on the patient's age, sex, condition, weight, absorption of the active ingredient into the body, inactivation rate and excretion rate, disease type, and drugs used in combination. However, since it may vary depending on the conditions of the patient to be used, it is not limited to a specific effective amount.
본 발명은 구강용 조성물의 제조방법을 제공한다.The present invention provides a method for preparing a composition for oral use.
본 발명에 따른 구강용 조성물의 제조방법은 식이유황 및 멘톨을 혼합하는 단계를 포함하고 이때 이산화탄소 환경을 만들기 위해서 직접 이산화탄소 가스를 주입하거나 탄산염과 유기산의 반응으로 발생하는 이산화탄소 가스를 이용할 수 있다. 다만 이에 제한되지 않는다.The method for producing a composition for oral use according to the present invention includes mixing dietary sulfur and menthol, and at this time, direct injection of carbon dioxide gas to create a carbon dioxide environment or carbon dioxide gas generated by the reaction of carbonate and organic acid may be used. However, the present invention is not limited thereto.
본 발명의 제조방법에서 상기 혼합하는 단계는 상기 식이유황과 상기 멘톨을 1:10 내지 10:1의 중량비로 혼합하여 수행될 수 있다. 본 발명의 일 실시예에서, 상기 식이유황과 상기 멘톨 화합물의 중량비는 1 내지 5: 1, 2 내지 4: 1 일 수 있다.In the manufacturing method of the present invention, the mixing step may be performed by mixing the dietary sulfur and the menthol in a weight ratio of 1:10 to 10:1. In an embodiment of the present invention, the weight ratio of the dietary sulfur and the menthol compound may be 1 to 5: 1, and 2 to 4: 1.
본 발명에서 식이유황과 멘톨을 용매에 용융하여 혼합할 수 있다. 상기 용매는 증류수 또는 솔비톨액을 포함할 수 있다. 다만, 식이유황과 멘톨을 용융시킬 수 있는 용매라면 제한되지 않는다.In the present invention, dietary sulfur and menthol may be melted and mixed in a solvent. The solvent may include distilled water or sorbitol solution. However, it is not limited as long as it is a solvent capable of melting dietary sulfur and menthol.
본 발명에서 상기 식이유황과 멘톨을 혼합하는 단계는 30 ℃내지 60 ℃에서 수행될 수 있다. 본 발명의 일 실시예에서, 상기 혼합하는 단계는 35 ℃내지 50 ℃에서 수행될 수 있다.In the present invention, the step of mixing the dietary sulfur and menthol may be performed at 30 °C to 60 °C. In one embodiment of the present invention, the mixing step may be performed at 35 °C to 50 °C.
본 발명에서 상기 식이유황과 멘톨을 혼합하는 단계는 사이클로덱스트린과 이산화탄소 분위기에서 수행되며, 이때 탄산염과 유기산을 반응시켜서 발생하는 이산화탄소를 이용할 수 있다. 탄산염은 탄산나트륨, 중탄산나트륨, 탄산칼륨, 중탄산칼륨 에서 선택되는 염일 수 있으며, 바람직하게는 칼륨을 포함하는 염이고 유기산은 구연산 또는 개미산일 수 있다. 본 발명의 일 실시예에서 상기 탄산염은 탄산칼륨 8.0 중량%, 상기 유기산은 구연산 8.0 중량%를 상기 식이유황과 멘톨을 혼합하는 단계에 처리하여 이산화탄소 분위기를 조성하였다. 다만, 이에 제한되지 않는다.In the present invention, the step of mixing the dietary sulfur and menthol is performed in an atmosphere of cyclodextrin and carbon dioxide, in which case carbon dioxide generated by reacting carbonate with an organic acid may be used. The carbonate may be a salt selected from sodium carbonate, sodium bicarbonate, potassium carbonate, and potassium bicarbonate, preferably a salt containing potassium, and the organic acid may be citric acid or formic acid. In an embodiment of the present invention, the carbonate was treated with 8.0 wt% of potassium carbonate and 8.0 wt% of citric acid as the organic acid in the step of mixing the dietary sulfur and menthol to create a carbon dioxide atmosphere. However, the present invention is not limited thereto.
본 발명에 따른 제조방법은 연마제, 방부제, 습윤제, 방향제 또는 항균제 등을 추가로 더 포함할 수 있다.The manufacturing method according to the present invention may further include an abrasive, an antiseptic, a wetting agent, a fragrance, or an antibacterial agent.
본 발명의 제조방법에 의해 제조되는 포함되는 구성들의 세부 내용은 상기 구강용 조성물의 내용과 같다.Details of the components included in the manufacturing method of the present invention are the same as the contents of the oral composition.
이하, 본 발명을 구체적으로 설명하기 위해 실시예를 들어 상세하게 설명하기로 한다.Hereinafter, examples will be given to describe the present invention in detail.
실시예Example
실시예 1. 식이유황 및 멘톨을 포함하는 구강용 조성물Example 1. Oral composition comprising dietary sulfur and menthol
MSM 3.0 중량%, 아르기닌 2.0 중량%, 탄산칼륨 8.0 중량%, 구연산 8.0 중량%, 멘톨 0.8 중량%, 불화나트륨 0.2 중량%, 솔비톨 35.1 중량%, 에리스리톨 27.3 중량%, 사이클로덱스트린 10.0 중량%, 레몬 에센셜오일 0.2 중량%, 스피아민트 오일 0.4 중량%, 페퍼민트 에센셜오일 0.2 중량%, 티트리 에센셜오일 0.2 중량%, 수크랄로스 0.1 중량%, 폴리비닐피롤리돈 1.0 중량%, 잔탄검0.4 중량%, 라우릴글루코사이드 1.2 중량%, 소듐코코일글루타메이트 1.8 중량%를 혼합하여 하기 표 1의 구강용 조성물을 제조하였다. MSM 3.0% by weight, arginine 2.0% by weight, potassium carbonate 8.0% by weight, citric acid 8.0% by weight, menthol 0.8% by weight, sodium fluoride 0.2% by weight, sorbitol 35.1% by weight, erythritol 27.3% by weight, cyclodextrin 10.0% by weight, lemon essential Oil 0.2% by weight, spearmint oil 0.4% by weight, peppermint essential oil 0.2% by weight, tea tree essential oil 0.2% by weight, sucralose 0.1% by weight, polyvinylpyrrolidone 1.0% by weight, xanthan gum 0.4% by weight, lauryl glucoside 1.2 wt%, sodium cocoyl glutamate 1.8 wt% was mixed to prepare a composition for oral use in Table 1 below.
상기 표 1의 조성에서 식이유황 및 멘톨의 함량을 다르게 하여 하기 실시예 1 내지 3의 구강용 조성물을 제조하였다. 또한, 식이유황 및 멘톨의 기능 비교를 위해 식이유황을 포함하지 않은 구강용 조성물인 비교예 1와 멘톨을 포함하지 않은 구강용 조성물인 비교예 2를 제조하였다.The oral compositions of Examples 1 to 3 were prepared by varying the contents of dietary sulfur and menthol in the composition of Table 1 above. In addition, to compare the functions of dietary sulfur and menthol, Comparative Example 1, which is a composition for oral use not containing dietary sulfur, and Comparative Example 2, which is a composition for oral use, which does not contain menthol, were prepared.
상기 표 2에서 식이유황이나 멘톨이 첨가되지 않은 비교예에는 동량의 정제수를 처리하였다. In Table 2, Comparative Examples in which dietary sulfur or menthol were not added were treated with the same amount of purified water.
실험예 1. 구강용 조성물의 치아우식원인균 및 치주질환원인균에 대한 항균 효과 분석Experimental Example 1. Analysis of the antibacterial effect of the oral composition on the bacteria causing dental caries and periodontal disease
상기 표 2의 조성으로 제조된 구강용 조성물을 사용하여 다음과 같은 방법으로 항균 효과를 평가하는 실험을 수행하였다. An experiment was performed to evaluate the antibacterial effect in the following way using the oral composition prepared in the composition of Table 2 above.
본 연구에서 사용한 균주는 치아우식증원인균인 스트렙토코쿠스 뮤탄스(Streptococcus mutans; S.mutans) KCOM 1054, 스트렙토코쿠스 소브리누스(Streptococcus sobrinus; S.sobrinus) KCOM 1157 및 치주질환원인균인 포르피로모나스 긴기발리스(Porphyromonas gingivalis; P.gingivalis) KCOM 2796, 프리보텔라 인터미디아(Prevotella intermedia; P.intermedia) KCOM 1107, 후소박테리움 뉴클레아툼(Fusobacterium nucleatum; F.nucleatum) KCOM 1322이고, 이들 균주는 한국인의 구강에서 분리 동정된 것으로, 본 연구자 팀이 운영하는 한국구강미생물자원(Korean Collection for Oral Microbiology, Gwangju, Korea) 에서 분양받아 사용하였다.The strain used in this study was Streptococcus mutans ( S. mutans ), the causative bacteria of dental caries. KCOM 1054, Streptococcus sobrinus ( S. sobrinus ) KCOM 1157 and periodontal disease causative bacteria Porphyromonas gingivalis ( P. gingivalis ) KCOM 2796, Prevotella intermedia ( Prevotella intermedia ) .intermedia ) KCOM 1107, Fusobacterium nucleatum ( F. nucleatum ) KCOM 1322, these strains were isolated and identified from the oral cavity of Koreans for Oral Microbiology, Gwangju, Korea).
본 연구에 사용한 S. mutans 와 S. sobrinus 균주들은 brain heart infusion (BHI) broth에 접종하여 37℃ 5% CO2 조건에서 배양하였으며, P. gingivalis, P. intermedia 및 F. nucleatum 균주들은 Tryptic Soy broth에 0.5% yeast extract, 0.05% cysteine HCl-H2O, 0.5 mg/ml hemin 및 2 μg/ml vitamin K1 이 포함된 배지에 접종하여, 37℃ chamber (Bactron I, Sheldon Manufacturing Inc., Cornelius, OR, USA)와 혐기성 조건(10% H2, 5% CO2, 85% N2)에서 배양하여 사용하였다. S. mutans and S. sobrinus strains used in this study were inoculated in brain heart infusion (BHI) broth and cultured at 37℃ 5% CO 2 conditions, and P. gingivalis , P. intermedia and F. nucleatum strains were in Tryptic Soy broth Inoculated in a medium containing 0.5% yeast extract, 0.05% cysteine HCl-H 2 O, 0.5 mg/ml hemin and 2 μg/ml vitamin K 1 in a 37 ° C chamber (Bactron I, Sheldon Manufacturing Inc., Cornelius, OR, USA) and anaerobic conditions (10% H 2 , 5% CO 2 , 85% N 2 ) were cultured and used.
MBC (minimum bactericidal concentration, 최소세균사멸농도) 측정은 Clinical and Laboratory Standards Institute (CLSI) 에서 제시한 미세희석(micro-dilution) 법을 변형하여 사용하였다. 우선 세균들을 앞에서 제시한 배지에 접종하여 37 ℃에서 24-48 시간 동안 세균배양기에서 배양한 후 2Х1010 CFU/ml가 되도록 준비하였다. 실험에 사용하는 구강용 조성물을 다음과 같이 준비(실험군 준비)하였다; 1) 구강용 조성물 90 μl (9/10 희석군), 2) 구강용 조성물 50 μl + 1X PBS 40 μl(1/2 희석군). 이들 실험군들은 1.5 ml 튜브에 넣어 준비한 후 각각의 세균배양액(2 x 1010 CFU/ml) 10 μl를 첨가하여 30초간 볼텍싱하였다. 이를 3분간 실온에 방치한 다음, 실험군에 1X PBS 900 μl를 넣어 10배 희석하였다. 이들 희석 용액에서 각각 50 μl를 채취해 1X PBS 9.950 ml이 담긴 50 ml 코니컬 튜브에 혼합해서 200배 희석하여 총 2,000배 희석하였다. 이때 세균의 농도는 1Х106 CFU/ml이 된다. 이 희석용액을 10배 희석한 10 μl를 채취하여 한천배지(각 세균 종에 맞는 배지)에 도말하여 2일 동안 배양하였다. 음성대조군은 구강용 조성물 대신 1X PBS를 넣어 실험군과 동일한 방법으로 시행하고자 하며, 이들의 실험도 실험군과 동일한 과정으로 진행하였다. 한천배지에 도말할 때의 구강용 조성물 농도가 항균력에 영향이 있는지 보기 위해, 각각의 구강용 조성물을 1X PBS에 1,000배 희석한 용액에 동량의 세균배양액(2Х106 CFU/ml)을 섞어서 최종 1Х106 CFU/ml 세균이 들어있는 각각의 구강용 조성물 용액(2,000배 희석)에서 10배 희석한 10 μl를 채취하여 한천배지(각 세균 종에 맞는 배지)에 도말 하였으며(최종 20,000배 희석), 이를 또 다른 음성대조군으로 사용하였으며, 이를 이용하여 세균살균력(bactericial activity,%) 및 MBC 값을 결정하였다. 각 한천배지에서 음성대조군의 군락 수가 1,000개 일 때, 각 실험군에서 1개 이하의 세균 군락이 보이는 군이 99.9% 이상의 세균살균력이 있다고 볼 수 있어, 이를 MBC 값이라 판정하였다.MBC (minimum bactericidal concentration) was measured by modifying the micro-dilution method suggested by the Clinical and Laboratory Standards Institute (CLSI). First, the bacteria were inoculated into the medium presented above and cultured in a bacterial incubator at 37 °C for 24-48 hours, and then prepared to become 2Х10 10 CFU/ml. The oral composition used in the experiment was prepared as follows (preparation of the experimental group); 1) 90 μl of oral composition (9/10 dilution group), 2) 50 μl oral composition + 40 μl of 1X PBS (1/2 dilution group). These experimental groups were prepared by putting them in a 1.5 ml tube, and then 10 μl of each bacterial culture solution (2 x 10 10 CFU/ml) was added and vortexed for 30 seconds. After standing at room temperature for 3 minutes, 900 μl of 1X PBS was added to the experimental group and diluted 10-fold. 50 μl of each of these dilutions was collected, mixed in a 50 ml conical tube containing 9.950 ml of 1X PBS, and diluted 200-fold, for a total of 2,000-fold dilution. At this time, the concentration of bacteria becomes 1Х10 6 CFU/ml. 10 μl of this diluted solution was diluted 10-fold, spread on an agar medium (medium suitable for each bacterial species), and cultured for 2 days. In the negative control group, 1X PBS was added instead of the oral composition, and the experiment was conducted in the same manner as in the experimental group, and these experiments were conducted in the same manner as in the experimental group. In order to see whether the concentration of the oral composition when smeared on an agar medium has an effect on the antibacterial activity, the same amount of the bacterial culture solution (2Х10 6 CFU/ml) is mixed with a 1,000-fold diluted solution of each oral composition in 1X PBS, and the final 1Х10 10 μl diluted 10-fold from each oral composition solution (2,000-fold dilution) containing 6 CFU/ml bacteria was spread on an agar medium (a medium suitable for each bacterial species) (final 20,000-fold dilution), and this It was used as another negative control, and bacterial activity (%) and MBC values were determined using this. When the number of colonies in the negative control group in each agar medium was 1,000, the group showing less than one bacterial colony in each experimental group had more than 99.9% bactericidal power, and this was determined as the MBC value.
본 발명의 실시예 1 내지 3의 경우, 9/10 희석한 경우, 본 시험에 사용한 5개 균주의 치아우식증원인균 및 치주질환원인균에 대해 99.9% 이상의 살균력이 있음을 알 수 있었다. 반면 비교예 1 및 2의 경우, Porphyromonas gingivalis 균주를 제외하고는 항균력이 높지 않았다. 이를 종합하면, 본 발명의 실시예에 해당하는 구강용 조성물은 치아우식증 및 치주질환을 예방하는데 사용할 수 있을 것으로 판단되었다.In the case of Examples 1 to 3 of the present invention, when diluted by 9/10, it was found that there was a sterilizing power of 99.9% or more against the bacteria causing the growth of dental caries and the bacteria causing the periodontal disease of the 5 strains used in this test. On the other hand, in Comparative Examples 1 and 2, except for the Porphyromonas gingivalis strain, antibacterial activity was not high. Taken together, it was determined that the oral composition corresponding to the embodiment of the present invention can be used to prevent dental caries and periodontal disease.
실험예 2. 시린이 완화 효과 비교Experimental Example 2. Comparison of the relief effect of Shirin
시린이 환자를 대상으로 각 구강용 조성물의 식이유황과 멘톨의 함량비에 따른 시린이 완화 정도를 확인하였다. The degree of relief of soreness according to the content ratio of dietary sulfur and menthol of each oral composition was confirmed for patients with shirin.
시험 대상자는 시린이 증상 유무에 따라 각각 30명의 시린이 유증상 군과 무증상 군으로 나누어, 상기 실시예 1에서 제조한 구강용 조성물 5종으로 2 주간, 3회/일로 칫솔질 한 후, 이의 시린 정도에 대해 0점에서 10점을 부여하는 방식으로 관능성 평가를 진행하였다. 10점에 가까울수록 시린이 증상이 완화되는 것으로서, 시린이 개선에 우수한 효과를 보이는 것으로 판단할 수 있었다. According to the presence or absence of symptoms, the test subjects were divided into 30 patients, respectively, a symptomatic group and an asymptomatic group, and after brushing with the five oral compositions prepared in Example 1 for 2 weeks, 3 times/day, the degree of irritation The sensory evaluation was conducted in a way that assigns 10 points to 0 points. As the score was closer to 10, it could be judged that the symptom was relieved by shirin, and that shirin showed an excellent effect in improvement.
무증상 군Sirin
asymptomatic group
유증상 군Sirin
symptom group
본 발명의 실시예 1 내지 3의 경우, 시린이 무증상 군, 시린이 유증상 군 모두에서 시린이 증상이 완화되는 것을 알 수 있었다. 반면, 비교예 1 및 2의 경우에는 그러한 완화 효과를 확인할 수 없었다. 이를 종합하면, 본 발명의 구강용 조성물은 종래 에리스리톨 포함 구강용 조성물에서 발생할 수 있는 잇몸 질환을 완화시킬 수 있는 구강용 조성물에 해당함을 확인할 수 있었다.In the case of Examples 1 to 3 of the present invention, it was found that shirin symptoms were alleviated in both the asymptomatic group and the symptomatic group. On the other hand, in the case of Comparative Examples 1 and 2, such a mitigating effect could not be confirmed. Taken together, it was confirmed that the composition for oral use of the present invention corresponds to a composition for oral use capable of alleviating gum disease that may occur in conventional oral compositions containing erythritol.
Claims (9)
A composition for oral use comprising a cyclodextrin containing dietary sulfur and menthol in a carbon dioxide atmosphere.
The composition for oral use according to claim 1, wherein the dietary sulfur is at least one selected from the group consisting of methylsulfonylmethane and dimethyl sulfoxide.
The composition for oral use according to claim 1, wherein the carbon dioxide is generated by the reaction of carbonate and organic acid.
The method according to claim 3, wherein the carbonate is potassium bicarbonate, potassium carbonate, sodium carbonate, oral composition comprising at least one or more from the group consisting of sodium bicarbonate.
The composition for oral use according to claim 3, wherein the organic acid comprises at least one of citric acid and formic acid.
The composition for oral use according to claim 1, wherein the dietary sulfur is included in an amount of 1 wt% to 5 wt% with respect to the total composition.
The composition for oral use according to claim 1, wherein the menthol is included in an amount of 0.5 wt% to 1.5 wt% with respect to the total composition.
The composition for oral use according to claim 1, further comprising at least one from the group consisting of potassium citrate, potassium nitrate, and potassium formate.
The composition for oral use according to claim 1, wherein the composition is safe for the human body and has an antibacterial effect on Streptococcus mutans and Porphyromonas gingivalis .
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KR1020210010870 | 2021-01-26 | ||
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KR1020220011694A KR20220107991A (en) | 2021-01-26 | 2022-01-26 | Oral composition for prevention or treatment of oral diseases |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR102621090B1 (en) * | 2023-08-20 | 2024-01-23 | 주식회사 구강닥터 | Drinking mouthwash composition capable of deodorizing and preventing tooth decay and its manufacturing method |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101039802B1 (en) | 2008-10-08 | 2011-06-09 | 주식회사 나이벡 | A Composition for Teeth Desensitizing |
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2022
- 2022-01-26 KR KR1020220011694A patent/KR20220107991A/en not_active Application Discontinuation
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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KR101039802B1 (en) | 2008-10-08 | 2011-06-09 | 주식회사 나이벡 | A Composition for Teeth Desensitizing |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR102621090B1 (en) * | 2023-08-20 | 2024-01-23 | 주식회사 구강닥터 | Drinking mouthwash composition capable of deodorizing and preventing tooth decay and its manufacturing method |
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