KR20230145664A - Antifungal composition containing vanillin as effective component - Google Patents
Antifungal composition containing vanillin as effective component Download PDFInfo
- Publication number
- KR20230145664A KR20230145664A KR1020220044296A KR20220044296A KR20230145664A KR 20230145664 A KR20230145664 A KR 20230145664A KR 1020220044296 A KR1020220044296 A KR 1020220044296A KR 20220044296 A KR20220044296 A KR 20220044296A KR 20230145664 A KR20230145664 A KR 20230145664A
- Authority
- KR
- South Korea
- Prior art keywords
- vanillin
- antifungal
- malassezia
- pathogenic fungi
- spp
- Prior art date
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Abstract
본 발명은 바닐린을 유효성분으로 함유하는 병원성 진균에 대한 항진균용 조성물에 관한 것으로, 본 발명의 바닐린은 트리코파이톤 멘타그로파이트(Trichophyton mentagrophyte), 말라세지아 파키더마티스(Malassezia pachydermatis), 말라세지아 레스트릭타(Malassezia restricta) 및 말라세지아 글로보사(Malassezia globosa)에 대한 항진균력이 우수하였고, 특히 o-바닐린의 항진균 효과가 p-바닐린에 비해 현저하므로, 바닐린, 특히 o-바닐린을 함유하는 본 발명의 조성물은 병원성 진균에 대한 항진균제로 유용하게 사용될 수 있다. The present invention relates to an antifungal composition against pathogenic fungi containing vanillin as an active ingredient, and the vanillin of the present invention is used in the treatment of Trichophyton mentagrophyte , Malassezia pachydermatis , and Malassezia. It had excellent antifungal activity against Malassezia restricta and Malassezia globosa , and in particular, the antifungal effect of o -vanillin was more pronounced than that of p -vanillin, so vanillin, especially o -vanillin, contained The composition of the present invention can be usefully used as an antifungal agent against pathogenic fungi.
Description
본 발명은 바닐린을 유효성분으로 함유하는 병원성 진균에 대한 항진균용 조성물에 관한 것이다. The present invention relates to an antifungal composition against pathogenic fungi containing vanillin as an active ingredient.
진균(fungi)은 미생물의 한 종류이다. 자연계에서 곰팡이 또는 효모균의 형태로 존재한다. 진균의 종류는 매우 많으나 인체에 기생하여 병을 일으키는 것은 약 40종류가 있다. 진균에 의한 감염증을 진균증(mycosis)이라고 한다. 감염 부위에 따라서 피부, 모발, 손톱 등 피부 표면에 국한되어 감염을 일으키는 표재성 진균증(superficial mycosis)과 피부의 깊은 부분이나 폐, 뇌 등의 내장 기관에서 감염을 일으키는 심재성 진균증(deep-seated mycosis)으로 나눌 수 있다. 진균증 중에는 우리 몸에 상주하는 진균이 면역기능이 저하된 환자에게서 병원성을 나타내어 생기는 경우가 있는데 이를 기회감염 진균증이라고 한다. 기회감염 진균증은 골수이식, 장기이식, 큰 수술, 면역억제요법을 받은 환자나 암 환자, 후천성 면역 결핍증 환자, 고령 및 미숙아 등 면역이 약화된 환자에게서 나타나기 쉽다.Fungi are a type of microorganism. It exists in nature in the form of mold or yeast. There are many types of fungi, but there are about 40 types that parasitize the human body and cause disease. Infections caused by fungi are called mycosis. Depending on the site of infection, there are two types of mycosis: superficial mycosis, which causes infection limited to the surface of the skin, such as the skin, hair, and nails, and deep-seated mycosis, which causes infection in the deep part of the skin or internal organs such as the lungs and brain. It can be shared. Among mycoses, there are cases where fungi residing in our body become pathogenic in patients with weakened immune function, and this is called opportunistic mycosis. Opportunistic mycoses are likely to appear in immunocompromised patients, such as patients who have undergone bone marrow transplant, organ transplant, major surgery, immunosuppressive therapy, cancer patients, acquired immune deficiency syndrome, elderly people, or premature infants.
표재성 감염을 일으키는 진균에는 피부사상균류(발, 머리, 몸, 회음부, 손발톱 등에 백선 유발), 말라세지아(어루러기 유발), 칸디다(칸디다증 유발) 등이 있다. 심재성 진균증을 일으키는 진균에는 칸디다, 아스페르길루스, 크립토코쿠스, 무코 등이 있다.Fungi that cause superficial infections include dermatophytes (causing ringworm on the feet, head, body, perineum, and nails), Malassezia (causing tinnitus), and Candida (causing candidiasis). Fungi that cause deep mycosis include Candida, Aspergillus, Cryptococcus, and Muco.
항진균제는 진균의 증식과 성장을 억제하여 진균 감염증을 치료하는 약물이다. 감염 부위가 피부 등에 제한된 표재성 진균 감염증의 경우에는 외용 항진균제를 사용하지만, 감염 부위가 광범위하거나 심재성 진균 감염증인 경우에는 주사나 경구용 항진균제를 사용한다. Antifungal drugs are drugs that treat fungal infections by inhibiting the proliferation and growth of fungi. In the case of superficial fungal infections where the infected area is limited to the skin, external antifungal agents are used, but in cases where the infected area is extensive or deep fungal infections, injections or oral antifungal agents are used.
그러나 현재까지 사용 가능한 항진균제는 세균 감염에 사용되는 항생제 수에 비해 훨씬 적다. 현재까지 개발된 항진균제로는, 전신성 진균증 치료에는 폴리엔계의 암포테리신 B나 아졸계의 플루코나졸, 이트라코나졸, 보리코나졸, 포사코나졸 등이 있지만, 아졸 내성균 등의 출현이 문제가 되고 있다. 따라서 효과적이면서 안전한 새로운 항진균제의 개발이 요구되고 있다. However, the number of antifungal drugs available to date is much smaller than the number of antibiotics used for bacterial infections. Antifungal agents developed to date include polyene-based amphotericin B and azole-based fluconazole, itraconazole, voriconazole, and posaconazole for the treatment of systemic mycosis, but the emergence of azole-resistant bacteria has become a problem. Therefore, the development of new effective and safe antifungal agents is required.
한편, 한국등록특허 제0649121호에 배초향 정유 및 케토코나졸을 유효성분으로 함유하는 복합 항진균제 및 상기 복합 항진균제를 이용하여 트리코피톤 속(Trichophyton) 진균을 치료하는 방법이 개시되어 있고, 한국등록특허 제1951649호에 레스베라트롤 함량이 증가된 호장근 추출물의 제조방법 및 이를 함유하는 말라세지아속 진균에 대한 항진균용 조성물이 개시되어 있지만, 본 발명의 바닐린, 구체적으로 o-바닐린을 유효성분으로 함유하는 병원성 진균에 대한 항진균용 조성물에 대해 개시된 바 없다. Meanwhile, Korean Patent No. 0649121 discloses a complex antifungal agent containing pear extract essential oil and ketoconazole as active ingredients and a method of treating Trichophyton fungi using the complex antifungal agent, and Korean Patent No. 1951649 Although a method for producing an extract of Japanese knotweed with increased resveratrol content and an antifungal composition containing the same for fungi of the genus Malassezia are disclosed, the vanillin of the present invention, specifically, for pathogenic fungi containing o -vanillin as an active ingredient, is disclosed. There has been no disclosure regarding antifungal compositions.
본 발명은 상기와 같은 요구에 의해 도출된 것으로, 바닐린, 구체적으로 o-바닐린을 유효성분으로 함유하는 병원성 진균에 대한 항진균용 조성물을 제공하고, 상기 o-바닐린이 p-바닐린에 비해 병원성 진균에 대한 항진균 효과가 현저하다는 것을 확인함으로써, 본 발명을 완성하였다.The present invention was developed in response to the above needs, and provides an antifungal composition against pathogenic fungi containing vanillin, specifically o -vanillin, as an active ingredient, and wherein o -vanillin is more effective against pathogenic fungi than p -vanillin. The present invention was completed by confirming that the antifungal effect was significant.
상기 과제를 해결하기 위하여, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균용 조성물을 제공한다. In order to solve the above problems, the present invention provides an antifungal agent against one or more pathogenic fungi selected from the Trichophyton spp. and Malassezia spp. containing vanillin or an acceptable salt thereof as an active ingredient. A composition is provided.
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 지루성 피부염, 외이도염, 비듬증, 아토피 피부염, 무좀 및 백선 중에서 선택된 어느 하나의 병원성 진균 감염에 의한 질환의 예방 또는 치료용 약학 조성물을 제공한다. In addition, the present invention provides a pharmaceutical composition for the prevention or treatment of diseases caused by any one pathogenic fungal infection selected from seborrheic dermatitis, otitis externa, dandruff, atopic dermatitis, athlete's foot, and ringworm, containing vanillin or an acceptable salt thereof as an active ingredient. to provide.
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균용 화장료 조성물을 제공한다. In addition, the present invention provides an antifungal cosmetic composition against one or more pathogenic fungi selected from Trichophyton spp. and Malassezia spp., containing vanillin or an acceptable salt thereof as an active ingredient. .
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균용 건강기능식품 조성물을 제공한다. In addition, the present invention provides an antifungal health functional food composition against one or more pathogenic fungi selected from the Trichophyton spp. and Malassezia spp. containing vanillin or an acceptable salt thereof as an active ingredient. to provide.
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균 보조제를 제공한다. In addition, the present invention provides an antifungal adjuvant against one or more pathogenic fungi selected from the Trichophyton spp. and Malassezia spp., containing vanillin or an acceptable salt thereof as an active ingredient.
또한, 본 발명은 인간을 제외한 개체에게 약학적으로 유효한 양의 바닐린을 투여하는 단계;를 포함하는 인간을 제외한 개체 내 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균의 감염에 대한 항진균 방법을 제공한다. In addition, the present invention provides a method of administering a pharmaceutically effective amount of vanillin to an individual other than a human, comprising: administering a pharmaceutically effective amount of vanillin to an individual other than a human; selecting from Trichophyton spp. and Malassezia spp. An antifungal method is provided for infection by one or more pathogenic fungi.
본 발명은 바닐린을 유효성분으로 함유하는 병원성 진균에 대한 항진균용 조성물에 관한 것으로, 본 발명의 바닐린은 트리코파이톤 멘타그로파이트(Trichophyton mentagrophyte), 말라세지아 파키더마티스(Malassezia pachydermatis), 말라세지아 레스트릭타(Malassezia restricta) 및 말라세지아 글로보사(Malassezia globosa)에 대한 항진균력이 우수하였고, 특히 o-바닐린의 항진균 효과가 p-바닐린에 비해 현저하였다. The present invention relates to an antifungal composition against pathogenic fungi containing vanillin as an active ingredient, and the vanillin of the present invention is used in the treatment of Trichophyton mentagrophyte , Malassezia pachydermatis , and Malassezia. It had excellent antifungal activity against Malassezia restricta and Malassezia globosa , and in particular, the antifungal effect of o -vanillin was more remarkable than that of p -vanillin.
본 발명의 목적을 달성하기 위하여, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균용 조성물을 제공한다. In order to achieve the object of the present invention, the present invention provides a method for treating one or more pathogenic fungi selected from the Trichophyton spp. and Malassezia spp. containing vanillin or an acceptable salt thereof as an active ingredient. A composition for antifungal use is provided.
상기 바닐린은 o-바닐린 및 p-바닐린 중에서 선택된 하나 이상인 것이 바람직하고, 더 바람직하게는 o-바닐린인 것이지만, 이에 제한되는 것은 아니다. The vanillin is preferably at least one selected from o -vanillin and p -vanillin, more preferably o -vanillin, but is not limited thereto.
상기 병원성 진균은 지루성 피부염, 외이도염, 비듬증, 아토피 피부염, 무좀 또는 백선을 유발하는 원인균인 것이 바람직하지만, 이에 제한되는 것은 아니다. The pathogenic fungi are preferably causative bacteria that cause seborrheic dermatitis, otitis externa, dandruff, atopic dermatitis, athlete's foot, or ringworm, but are not limited thereto.
상기 트리코파이톤 속(Trichophyton spp.) 진균은 구체적으로 트리코파이톤 멘타그로파이트(Trichophyton mentagrophyte)인 것이 바람직하지만, 이에 한정하는 것은 아니다. The fungus of the Trichophyton spp. is preferably Trichophyton mentagrophyte, but is not limited thereto.
상기 말라세지아 속(Malassezia spp.) 진균은 구체적으로 말라세지아 파키더마티스(Malassezia pachydermatis), 말라세지아 레스트릭타(Malassezia restricta) 및 말라세지아 글로보사(Malassezia globosa) 중에서 선택된 하나 이상인 것이 바람직하지만, 이에 제한되는 것은 아니다. The Malassezia spp. fungus is specifically selected from Malassezia pachydermatis , Malassezia restricta , and Malassezia globosa . It is desirable, but not limited thereto.
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 지루성 피부염, 외이도염, 비듬증, 아토피 피부염, 무좀 및 백선 중에서 선택된 어느 하나의 병원성 진균 감염에 의한 질환의 예방 또는 치료용 약학 조성물을 제공한다. In addition, the present invention provides a pharmaceutical composition for the prevention or treatment of diseases caused by any one pathogenic fungal infection selected from seborrheic dermatitis, otitis externa, dandruff, atopic dermatitis, athlete's foot, and ringworm, containing vanillin or an acceptable salt thereof as an active ingredient. to provide.
본 발명에 따른 상기 약학 조성물은 각각 통상의 방법에 따라 캡슐제, 산제, 과립제, 정제, 현탁액, 에멀젼, 시럽, 에어로졸 등의 경구형 제형, 외용제, 좌제 및 멸균 주사용액의 형태로 제형화하여 사용될 수 있다. The pharmaceutical composition according to the present invention can be formulated and used in the form of oral dosage forms such as capsules, powders, granules, tablets, suspensions, emulsions, syrups, aerosols, external preparations, suppositories, and sterile injection solutions according to conventional methods. You can.
본 발명에 따른 상기 약학 조성물은 약학적으로 허용 가능한 담체, 부형제 또는 희석제를 더 포함할 수 있다. The pharmaceutical composition according to the present invention may further include a pharmaceutically acceptable carrier, excipient, or diluent.
본 발명의 약학 조성물에 포함될 수 있는 담체, 부형제 및 희석제로는 락토즈, 덱스트로즈, 수크로스, 솔비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 전분, 아카시아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로오스, 메틸 셀룰로오스, 미정질 셀룰로오스, 폴리비닐 피롤리돈, 물, 메틸히드록시벤조에이트, 프로필히드록시벤조에이트, 탈크, 마그네슘 스테아레이트 및 광물유 등을 포함한 다양한 화합물 혹은 혼합물을 들 수 있다. Carriers, excipients and diluents that may be included in the pharmaceutical composition of the present invention include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginate, gelatin, calcium phosphate, calcium silicate. , cellulose, methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil.
제제화할 경우에는 보통 사용하는 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 조제된다. 경구투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형제제는 상기 약학 조성물에 적어도 하나 이상의 부형제 예를 들면, 전분, 칼슘카보네이트, 수크로스 또는 락토오스, 젤라틴 등을 섞어 조제된다. 또한, 단순한 부형제 이외에 마그네슘 스테아레이트, 탈크 같은 윤활제들도 사용된다. 경구를 위한 액상 제제로는 현탁제, 내용액제, 유제, 시럽제 등이 해당하는데 흔히 사용되는 단순 희석제인 물, 리퀴드 파라핀 이외에 여러 가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다. 비경구투여를 위한 제제에는 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조 제제, 좌제가 포함된다. 비수성용제, 현탁제로는 프로필렌글리콜, 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다. 좌제의 기제로는 위텝솔, 마크로골, 트윈 61, 카카오지, 라우린지, 글리세로젤라틴 등이 사용될 수 있다.When formulated, it is prepared using diluents or excipients such as commonly used fillers, extenders, binders, wetting agents, disintegrants, and surfactants. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc. These solid preparations contain at least one excipient such as starch, calcium carbonate, sucrose or lactose, gelatin, etc. in the pharmaceutical composition. It is prepared by mixing. Additionally, in addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid preparations for oral use include suspensions, oral solutions, emulsions, syrups, etc. In addition to the commonly used simple diluents such as water and liquid paraffin, various excipients such as wetting agents, sweeteners, fragrances, and preservatives may be included. . Preparations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Non-aqueous solvents and suspensions include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate. As a base for suppositories, wethepsol, macrogol, Tween 61, cacao, laurin, glycerogelatin, etc. can be used.
본 발명의 약학 조성물의 적합한 투여량은 제제화 방법, 투여 방식, 환자의 연령, 체중, 성, 병적 상태, 음식, 투여 시간, 투여 경로, 배설 속도 및 반응 감응성과 같은 요인들에 의해 다양하게 처방될 수 있다.The appropriate dosage of the pharmaceutical composition of the present invention may be prescribed in various ways depending on factors such as formulation method, administration method, patient's age, weight, sex, pathological condition, food, administration time, administration route, excretion rate, and reaction sensitivity. You can.
본 발명의 약학 조성물은 경구 또는 비경구로 투여할 수 있으며, 비경구투여의 경우, 피부에 국소적으로 도포, 정맥 내 주입, 피하 주입, 근육 주입, 복강 주입, 경피 투여 등으로 투여할 수 있다.The pharmaceutical composition of the present invention can be administered orally or parenterally, and in the case of parenteral administration, it can be administered topically on the skin, intravenous injection, subcutaneous injection, intramuscular injection, intraperitoneal injection, transdermal administration, etc.
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균용 화장료 조성물을 제공한다. In addition, the present invention provides an antifungal cosmetic composition against one or more pathogenic fungi selected from Trichophyton spp. and Malassezia spp., containing vanillin or an acceptable salt thereof as an active ingredient. .
상기 병원성 진균은 지루성 피부염, 외이도염, 비듬증, 아토피 피부염, 무좀 또는 백선을 유발하는 것이지만, 이에 한정하는 것은 아니다.The pathogenic fungi cause seborrheic dermatitis, otitis externa, dandruff, atopic dermatitis, athlete's foot, or ringworm, but are not limited thereto.
본 발명의 화장료 조성물은 상기 바닐린 이외에 화장료 조성물에 통상적으로 이용되는 성분들이 포함되며, 예켠대 항산화제, 안정화제, 용해화제, 비타민, 안료 및 향료와 같은 통상적인 보조제, 그리고 담체를 포함한다.The cosmetic composition of the present invention contains ingredients commonly used in cosmetic compositions in addition to the vanillin, and includes conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments and fragrances, and carriers.
본 발명의 화장료 조성물은 당업계에서 통상적으로 제조되는 어떠한 제형으로도 제조될 수 있으며, 예를 들어, 용액, 현탁액, 유탁액, 페이스트, 겔, 크림, 로션, 파우더, 비누, 계면활성제-함유 클렌징, 오일, 분말 파운데이션, 유탁액 파운데이션, 왁스 파운데이션 및 스프레이 등으로 제형화될 수 있으나, 이에 한정되는 것은 아니다. 보다 상세하게는, 유연 화장수(스킨), 영양 화장수(밀크로션), 영양 크림, 맛사지 크림, 에센스, 아이크림, 클렌징 크림, 클렌징 포옴, 클렌징 워터, 샴푸, 팩, 스프레이 또는 파우더의 제형으로 제조될 수 있다.The cosmetic composition of the present invention can be prepared in any formulation commonly prepared in the art, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing products. , oil, powder foundation, emulsion foundation, wax foundation, spray, etc., but is not limited thereto. More specifically, it can be manufactured in the form of flexible lotion (skin), nourishing lotion (milk lotion), nourishing cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, shampoo, pack, spray or powder. You can.
본 발명의 제형이 페이스트, 크림 또는 겔인 경우에는 담체 성분으로서 동물성 유, 식물성 유, 왁스, 파라핀, 전분, 트라가칸타, 셀룰로오스 유도체, 폴리에틸렌 글리콜, 실리콘, 벤토나이트, 실리카, 탈크 또는 산화아연 등이 이용될 수 있다.When the formulation of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tragacantha, cellulose derivatives, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide are used as carrier ingredients. It can be.
본 발명의 제형이 파우더 또는 스프레이인 경우에는 담체 성분으로서 락토스, 탈크, 실리카, 알루미늄 히드록시드, 칼슘 실리케이트 또는 폴리아미드 파우더가 이용될 수 있고, 특히 스프레이인 경우에는 추가적으로 클로로플루오로히드로카본, 프로판/부탄 또는 디메틸 에테르와 같은 추진체를 포함할 수 있다.When the formulation of the present invention is a powder or spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, or polyamide powder can be used as the carrier ingredient. In particular, when the formulation is a spray, chlorofluorohydrocarbon and propane may be used as carrier ingredients. /May contain propellants such as butane or dimethyl ether.
본 발명의 제형이 용액 또는 유탁액인 경우에는 담체 성분으로서 용매, 용해화제 또는 유탁화제가 이용되고, 예컨대 물, 에탄올, 이소프로판올, 에틸 카보네이트, 에틸 아세테이트, 벤질 알코올, 벤질 벤조에이트, 프로필렌글리콜, 1,3-부틸글리콜 오일, 글리세롤 지방족 에스테르, 폴리에틸렌 글리콜 또는 소르비탄의 지방산 에스테르가 있다.When the formulation of the present invention is a solution or emulsion, a solvent, solubilizing agent, or emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 , 3-butyl glycol oil, glycerol aliphatic esters, polyethylene glycol or fatty acid esters of sorbitan.
본 발명의 제형이 현탁액인 경우에는 담체 성분으로서 물, 에탄올 또는 프로필렌 글리콜과 같은 액상의 희석제, 에톡실화 이소스테아릴 알코올, 폴리옥시에틸렌 소르비톨 에스테르 및 폴리옥시에틸렌 소르비탄 에스테르와 같은 현탁제, 미소 결정성 셀룰로오스, 알루미늄 메타히드록시드, 벤토나이트, 아가 또는 트라가칸타 등이 이용될 수 있다.When the formulation of the present invention is a suspension, the carrier ingredients include water, a liquid diluent such as ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester, and polyoxyethylene sorbitan ester, and microcrystals. Cellulose, aluminum metahydroxide, bentonite, agar or tragacantha can be used.
본 발명의 제형이 계면-활성제 함유 클렌징인 경우에는 담체 성분으로서 지방족 알코올 설페이트, 지방족 알코올 에테르 설페이트, 설포숙신산 모노에스테르, 이세티오네이트, 이미다졸리늄 유도체, 메틸타우레이트, 사르코시네이트, 지방산 아미드 에테르 설페이트, 알킬아미도베타인, 지방족 알코올, 지방산 글리세리드, 지방산 디에탄올아미드, 식물성 유, 라놀린 유도체 또는 에톡실화 글리세롤 지방산 에스테르 등이 이용될 수 있다.When the formulation of the present invention is a surfactant-containing cleansing agent, the carrier ingredients include aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyl taurate, sarcosinate, and fatty acid amide. Ether sulfate, alkylamidobetaine, fatty alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, lanolin derivative, or ethoxylated glycerol fatty acid ester can be used.
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균용 건강기능식품 조성물을 제공한다. In addition, the present invention provides an antifungal health functional food composition against one or more pathogenic fungi selected from the Trichophyton spp. and Malassezia spp. containing vanillin or an acceptable salt thereof as an active ingredient. to provide.
상기 병원성 진균은 지루성 피부염, 외이도염, 비듬증, 아토피 피부염, 무좀 또는 백선을 유발하는 것이지만, 이에 한정하는 것은 아니다. The pathogenic fungi cause seborrheic dermatitis, otitis externa, dandruff, atopic dermatitis, athlete's foot, or ringworm, but are not limited thereto.
상기 조성물은 과립제, 산제, 정제, 피복정, 캡슐제, 액제, 시럽, 즙, 현탁제, 유제 및 점적제 중에서 선택된 1종 이상으로 제제화될 수 있지만, 이에 한정하지 않는다. The composition may be formulated with one or more types selected from granules, powders, tablets, coated tablets, capsules, solutions, syrups, juices, suspensions, emulsions and drops, but is not limited thereto.
본 발명의 건강기능식품 조성물을 식품첨가물로 사용하는 경우, 상기 건강기능식품 조성물을 그대로 첨가하거나 다른 식품 또는 식품성분과 함께 사용될 수 있고, 통상적인 방법에 따라 적절하게 사용될 수 있다. 유효성분의 양은 그의 사용 목적(예방 또는 개선)에 따라 적절하게 사용될 수 있다. 일반적으로, 식품 또는 음료의 제조시 본 발명의 건강기능식품 조성물은 총 원료에 대하여 15 중량부 이하, 바람직하게는 10 중량부 이하의 양으로 첨가된다. 그러나 건강을 목적으로 하는 장기간의 섭취인 경우에는 상기 양은 상기 범위 이하일 수 있으며, 안전성 면에서 아무런 문제가 없기 때문에 유효성분은 상기 범위 이상의 양으로 사용될 수 있다.When using the health functional food composition of the present invention as a food additive, the health functional food composition may be added as is or used together with other foods or food ingredients, and may be used appropriately according to conventional methods. The amount of active ingredient can be appropriately used depending on the purpose of use (prevention or improvement). Generally, when manufacturing a food or beverage, the health functional food composition of the present invention is added in an amount of 15 parts by weight or less, preferably 10 parts by weight or less, based on the total raw materials. However, in the case of long-term intake for health purposes, the amount may be below the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount above the above range.
상기 건강기능식품의 종류에 특별한 제한은 없다. 상기 건강기능식품 조성물을 첨가할 수 있는 식품의 예로는 육류, 소시지, 빵, 초콜릿, 캔디류, 스낵류, 과자류, 피자, 라면, 기타 면류, 껌류, 아이스크림류를 포함한 낙농제품, 각종 스프, 음료수, 차 드링크제, 알콜 음료 및 비타민 복합제 등이 있으며, 통상적인 의미에서의 건강식품을 모두 포함한다.There are no particular restrictions on the types of health functional foods. Examples of foods to which the health functional food composition can be added include meat, sausages, bread, chocolate, candies, snacks, confectionery, pizza, ramen, other noodles, gum, dairy products including ice cream, various soups, beverages, and tea. There are drinks, alcoholic beverages, and vitamin complexes, and it includes all health foods in the conventional sense.
또한, 본 발명의 건강기능식품 조성물은 식품, 특히 기능성 식품으로 제조될 수 있다. 본 발명의 기능성 식품은 식품 제조 시에 통상적으로 첨가되는 성분을 포함하며, 예를 들어, 단백질, 탄수화물, 지방, 영양소 및 조미제를 포함한다. 예컨대, 드링크제로 제조되는 경우에는 유효성분 이외에 천연 탄수화물 또는 향미제를 추가 성분으로서 포함할 수 있다. 상기 천연 탄수화물은 모노사카라이드(예컨대, 글루코오스, 프럭토오스 등), 디사카라이드(예컨대, 말토스, 수크로스 등), 올리고당, 폴리사카라이드(예컨대, 덱스트린, 시클로덱스트린 등) 또는 당알코올(예컨대, 자일리톨, 소르비톨, 에리쓰리톨 등)인 것이 바람직하다. 상기 향미제는 천연 향미제(예컨대, 타우마틴, 스테비아 추출물 등)와 합성 향미제(예컨대, 사카린, 아스파르탐 등)를 이용할 수 있다.Additionally, the health functional food composition of the present invention can be manufactured into food, especially functional food. The functional food of the present invention includes ingredients commonly added during food production, and includes, for example, proteins, carbohydrates, fats, nutrients and seasonings. For example, when manufactured as a drink, natural carbohydrates or flavoring agents may be included as additional ingredients in addition to the active ingredient. The natural carbohydrates include monosaccharides (e.g., glucose, fructose, etc.), disaccharides (e.g., maltose, sucrose, etc.), oligosaccharides, polysaccharides (e.g., dextrins, cyclodextrins, etc.), or sugar alcohols (e.g., For example, xylitol, sorbitol, erythritol, etc.) is preferable. The flavoring agent may be a natural flavoring agent (e.g., thaumatin, stevia extract, etc.) or a synthetic flavoring agent (e.g., saccharin, aspartame, etc.).
상기 건강기능식품 조성물 이외에 여러 가지 영양제, 비타민, 전해질, 풍미제, 착색제, 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제 등을 더 함유할 수 있다. 이러한 상기 첨가되는 성분의 비율은 크게 중요하진 않지만 본 발명의 건강기능식품 조성물 100 중량부에 대하여, 0.01 내지 0.1 중량부의 범위에서 선택되는 것이 일반적이다.In addition to the above health functional food composition, various nutrients, vitamins, electrolytes, flavors, colorants, pectic acid and its salts, alginic acid and its salts, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohol, carbonic acid. It may further contain carbonating agents used in beverages. The ratio of the ingredients added is not very important, but is generally selected in the range of 0.01 to 0.1 parts by weight based on 100 parts by weight of the health functional food composition of the present invention.
또한, 본 발명은 바닐린 또는 이의 허용가능한 염을 유효성분으로 함유하는 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균에 대한 항진균 보조제를 제공한다. In addition, the present invention provides an antifungal adjuvant against one or more pathogenic fungi selected from the Trichophyton spp. and Malassezia spp., containing vanillin or an acceptable salt thereof as an active ingredient.
상기 병원성 진균은 지루성 피부염, 외이도염, 비듬증, 아토피 피부염, 무좀 또는 백선을 유발하는 것이지만, 이에 한정하는 것은 아니다. The pathogenic fungi cause seborrheic dermatitis, otitis externa, dandruff, atopic dermatitis, athlete's foot, or ringworm, but are not limited thereto.
또한, 본 발명은 인간을 제외한 개체에게 약학적으로 유효한 양의 바닐린을 투여하는 단계;를 포함하는 인간을 제외한 개체 내 트리코파이톤 속(Trichophyton spp.) 및 말라세지아 속(Malassezia spp.) 중에서 선택된 하나 이상의 병원성 진균의 감염에 대한 항진균 방법을 제공한다. In addition, the present invention provides a method of administering a pharmaceutically effective amount of vanillin to an individual other than a human, comprising: administering a pharmaceutically effective amount of vanillin to an individual other than a human; selecting from Trichophyton spp. and Malassezia spp. An antifungal method is provided for infection by one or more pathogenic fungi.
상기 인간을 제외한 개체는 바람직하게는 인간을 제외한 포유동물일 수 있으나, 이에 한정되지 않는다.The non-human entity may preferably be a mammal other than a human, but is not limited thereto.
상기 병원성 진균은 지루성 피부염, 외이도염, 비듬증, 아토피 피부염, 무좀 또는 백선을 유발하는 것이지만, 이에 한정하는 것은 아니다. The pathogenic fungi cause seborrheic dermatitis, otitis externa, dandruff, atopic dermatitis, athlete's foot, or ringworm, but are not limited thereto.
이하, 실시예를 이용하여 본 발명을 더욱 상세하게 설명하고자 한다. 이들 실시예는 오로지 본 발명을 보다 구체적으로 설명하기 위한 것으로, 본 발명의 범위가 이들에 의해 제한되지 않는다는 것은 당해 기술분야에서 통상의 지식을 가진 자에게 있어 자명한 것이다. Hereinafter, the present invention will be described in more detail using examples. These examples are only for illustrating the present invention in more detail, and it is obvious to those skilled in the art that the scope of the present invention is not limited thereto.
실시예 1. 바닐린의 항진균 효과Example 1. Antifungal effect of vanillin
1) 트리코파이톤 멘타그로파이트(1) Trichophyton mentagrophyte ( Trichophyton mentagrophyteTrichophyton mentagrophyte )에 대한 항진균 효과) antifungal effect on
o-바닐린 및 p-바닐린의 무좀균에 대한 항진균 활성을 측정하기 위해, 트리코파이톤 멘타그로파이트(Trichophyton mentagrophyte)를 배양한 후, 바닐린을 처리하여 진균의 발육을 저지할 수 있는 최소 저지 농도(MIC, Minimum Inhibitory Concentration)를 측정하였다. MIC 값은 CLSI(Clinical and Laboratory Standard Institute) 지침에 따라 표준 배지 연속 희석 방법(standard broth serial dilution method)을 사용하여 측정하였다.To measure the antifungal activity of o -vanillin and p -vanillin against athlete's foot fungi, Trichophyton mentagrophyte was cultured and treated with vanillin to determine the minimum inhibitory concentration (MIC, Minimum Inhibitory Concentration) was measured. MIC values were measured using the standard broth serial dilution method according to CLSI (Clinical and Laboratory Standard Institute) guidelines.
o-바닐린(CAS No. 148-53-8) 및 p-바닐린(CAS No. 121-33-5)은 Sigma-Aldrch사의 제품을 디메틸설폭사이드(DMSO)에 녹여 시험에 사용하였다. o -vanillin (CAS No. 148-53-8) and p -vanillin (CAS No. 121-33-5), products from Sigma-Aldrch, were dissolved in dimethyl sulfoxide (DMSO) and used in the test.
그 결과, 표 1에 개시된 바와 같이 바닐린은 트리코파이톤 멘타그로파이트(Trichophyton mentagrophyte)에 대한 항진균 효과가 우수하였고, 특히 o-바닐린의 항진균 효과가 p-바닐린에 비해 현저하였다. As a result, as shown in Table 1, vanillin had an excellent antifungal effect against Trichophyton mentagrophyte, and in particular, the antifungal effect of o -vanillin was more significant than that of p -vanillin.
2) 말라세지아 속(2) Malassezia genus ( MalasseziaMalassezia spp.)에 대한 항진균 효과 Antifungal effect against spp.)
o-바닐린 및 p-바닐린의 말라세지아 속(Malassezia spp.) 진균에 대한 항진균 활성을 측정하기 위해, 말라세지아 파키더마티스(Malassezia pachydermatis), 말라세지아 레스트릭타(Malassezia restricta) 및 말라세지아 글로보사(Malassezia globosa)를 배양한 후, 바닐린을 처리하여 진균의 발육을 저지할 수 있는 최소 저지 농도(MIC, Minimum Inhibitory Concentration)를 측정하였다. MIC 값은 CLSI(Clinical and Laboratory Standard Institute) 지침에 따라 표준 배지 연속 희석 방법(standard broth serial dilution method)을 사용하여 측정하였다.To determine the antifungal activity of o -vanillin and p -vanillin against Malassezia spp., Malassezia pachydermatis , Malassezia restricta and Malassezia After culturing Malassezia globosa , the minimum inhibitory concentration (MIC) capable of inhibiting the growth of fungi was measured by treating it with vanillin. MIC values were measured using the standard broth serial dilution method according to CLSI (Clinical and Laboratory Standard Institute) guidelines.
그 결과, 표 2에 개시된 바와 같이 바닐린은 말라세지아 파키더마티스(Malassezia pachydermatis), 말라세지아 레스트릭타(Malassezia restricta) 및 말라세지아 글로보사(Malassezia globosa)에 대한 항진균 효과가 우수하였고, 특히 o-바닐린의 항진균 효과가 p-바닐린에 비해 현저하였다. As a result, as shown in Table 2, vanillin had excellent antifungal effects against Malassezia pachydermatis, Malassezia restricta , and Malassezia globosa , In particular, the antifungal effect of o -vanillin was more significant than that of p -vanillin.
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