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KR20060118530A - Use of ondansetron for the treatment of inflammation and pharmaceutical composition thereof - Google Patents

Use of ondansetron for the treatment of inflammation and pharmaceutical composition thereof Download PDF

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KR20060118530A
KR20060118530A KR1020067011213A KR20067011213A KR20060118530A KR 20060118530 A KR20060118530 A KR 20060118530A KR 1020067011213 A KR1020067011213 A KR 1020067011213A KR 20067011213 A KR20067011213 A KR 20067011213A KR 20060118530 A KR20060118530 A KR 20060118530A
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ondansetron
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composition
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파브리치오 돌피
나데쥬 트레멜
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갈데르마 리써어치 앤드 디벨로프먼트,에스.엔.씨.
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions

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Abstract

본 발명은 외용 경로에 의한 치료 및/또는 예방성 항염증 처리를 위한 약학 조성물, 특히 피부학적 조성물 제조에서 활성원으로서의 온단세트론 (ondansetron)의 용도에 관련된다. 보다 구체적으로, 본 발명은, 염증성 피부 질환인 주사 (rosacea)의 외용치료를 위한 온단세트론의 용도를 제공한다. The present invention relates to the use of ondansetron as an active source in the manufacture of pharmaceutical compositions, in particular dermatological compositions, for the treatment and / or prophylactic anti-inflammatory treatment by external routes. More specifically, the present invention provides the use of ondansetron for external treatment of rosacea, an inflammatory skin disease.

Description

염증 치료를 위한 온단세트론의 용도 및 그 약학 조성물{USE OF ONDANSETRON FOR THE TREATMENT OF INFLAMMATION, AND PHARMACEUTICAL COMPOSITIONS THEREOF}USE OF ONDANSETRON FOR THE TREATMENT OF INFLAMMATION, AND PHARMACEUTICAL COMPOSITIONS THEREOF

본 발명은 외용 경로에 의한 치료 및/또는 예방성 항염증 처리를 위한 약학 조성물, 특히 피부학적 조성물 제조에서 활성원으로서의 온단세트론 (ondansetron)의 용도에 관련된다. 보다 구체적으로, 본 발명은, 염증성 피부 질환인 주사 (rosacea)의 외용치료를 위한 온단세트론의 용도를 제공한다. 온단세트론이라 함은, 일례로 염산염인 그 이온성 염 또는 비이온성 염기 형태의 온단세트론을 의미한다.The present invention relates to the use of ondansetron as an active source in the manufacture of pharmaceutical compositions, in particular dermatological compositions, for the treatment and / or prophylactic anti-inflammatory treatment by external routes. More specifically, the present invention provides the use of ondansetron for external treatment of rosacea, an inflammatory skin disease. By ondansetron means ondansetron in its ionic salt or nonionic base form, which is, for example, hydrochloride.

온단세트론 또는 (±) 1,2,3,9-테트라히드로-9-메틸-3-[(2-메틸-1H-이미다졸-1-일)메틸]-4H-카바졸-4-온은, 이미 공지된 생성물로, 미국 특허 제 4,695,578호에 기재 및 청구된 것이다. 온단세트론은 1차 구심성 신경에 위치한 신경형 5 HT 수용체 타입 3의 강력하며 선택적인 안타고니스트로 작용한다. 특히 온단세트론은, 화학요법으로 야기된 어지럼 및 구토를 예방 또는 치료하기 위해 과거에 완화 요법에서 승인되어 왔다. 또한 이 화합물은 진통제, 일례로, 편두통, 두통 및 5HT가 내재적 매개자인 많은 다른 형태의 고통의 경감에 유용하다.Ondansetron or (±) 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl) methyl] -4H-carbazol-4-one, Already known product, described and claimed in US Pat. No. 4,695,578. Ondansetron acts as a potent and selective antagonist of the neuronal 5 HT receptor type 3 located in the primary afferent nerve. Ondansetron, in particular, has been approved in palliative therapy in the past to prevent or treat dizziness and vomiting caused by chemotherapy. The compound is also useful for alleviating analgesics such as migraine headaches, headaches and many other forms of pain where 5HT is an inherent mediator.

그러나, 염증성 피부 증상인 주사의 치료에 외용 경로로 온단세트론을 이용 하는 것에 대한 발표된 데이터는 없다.However, there are no published data on the use of ondansetron as an external route for the treatment of injections, inflammatory skin symptoms.

따라서, 본 발명의 주제는, 염증 치료용 외용 약학 조성물 제조를 위한 항염증 유효량의 온단세트론의 용도에 관한 것이다. 또한, 본 발명은 온단세트론을 함유하는 약학 조성물을 외용 적용함으로써 염증을 치료하는 신규한 방법을 제공한다. 더 구체적으로, 본 발명은, 염증성 피부 질환인 주사의 외용 치료를 위한 온단세트론의 용도를 제공한다.Accordingly, the subject of the present invention relates to the use of an anti-inflammatory effective amount of ondansetron for the preparation of external pharmaceutical compositions for the treatment of inflammation. The present invention also provides a novel method of treating inflammation by external application of a pharmaceutical composition containing ondansetron. More specifically, the present invention provides the use of ondansetron for the external treatment of injections which are inflammatory skin diseases.

주사는 흔하지만 보통 간과되는 불특정 병인의 피부 증상으로, 심각한 안면 기형, 안과적 복합증상 및 심대한 감성적 스트레스를 유도할 수 있다. 주사의 진행은 가변이다; 그러나, 통상은 단계는 다음을 포함한다: (1) 대부분 볼에 홍조 또는 일광화상을 가지는 것으로 보이는 안면 홍조, 여기에서 피부 혈관의 확장으로 붉어짐이 초래되고, 이는 보다 많은 혈액이 흘러 들어와 피부 표면 밑에 모이게 됨, (2) 홍반 및/또는 부종, 안면 홍조증, (3) 작고 붉은 고형 (구진; papule)인 것 또는 고름이 찬 (농포) 것으로 나타나는 여드름, 및 (4) 라이노피마 (rhynophyma).Injection is a common but usually overlooked skin condition of an unspecified etiology that can lead to severe facial malformations, ophthalmic complications, and profound emotional stress. The progress of the injection is variable; However, the steps typically include: (1) hot flashes, which appear to have mostly flushing or sunburn on the cheeks, where reddening is caused by the expansion of skin vessels, which causes more blood to flow in and beneath the skin surface Gathering, (2) erythema and / or edema, hot flashes, (3) acne, which appears to be a small, red solid (papule) or pus (pain), and (4) rhynophyma.

안면 중심 홍반 및 안면 홍조증이 주사의 초기 단계에 나타난다. 이는, 안면 중심 구진 및, 덜 빈번하게는 농포가 섞인 만성 염증으로 진행된다. 간헐적 또는 만성적 안면 부종 또한 일어날 수 있다. 일부 환자는 라이노피마로 발전되며, 이는, 코 위의 작고 둥근 덩어리로 나타나는 코의 결합 조직 및 지선의 거친 비후이다.Facial central erythema and hot flashes appear at the initial stage of injection. This progresses to facial central papules and, less often, chronic inflammation with pustules. Intermittent or chronic facial edema may also occur. Some patients develop rhinopima, which are coarse thickening of the connective tissue and branch lines of the nose, which appear as small round lumps on the nose.

주사에 있어 대두되는 대부분의 불만은, 간헐적 안면 중심 홍조 및 홍반이다. 보통 가려움은 없다; 그러나, 많은 환자들은 붉어짐의 경우와 수반되는 따끔한 통증 (이는 심각할 수도 있음)을 호소한다. 이러한 붉어짐의 경우는, 보통 사회적으로 당황스러운 것으로 예측 불허 또는 환경, 화학물질, 식품 또는 감정적 촉발과 관련될 수 있다. 보통의 촉발 인자는, 일광에의 노출, 차가운 날씨, 급격한 감정 (웃음 또는 당황), 뜨거운 음료 및 알콜 소비를 포함한다.Most complaints that arise with injections are intermittent facial centered flushing and erythema. Usually there is no itching; However, many patients complain of redness and accompanying pain, which can be serious. This redness can usually be unforeseen as socially embarrassing or associated with environmental, chemical, food or emotional triggers. Common triggers include exposure to sunlight, cold weather, sudden emotions (laughs or embarrassment), hot drinks and alcohol consumption.

본 발명에서, 안면 홍조 치료를 위해 하루 1회 또는 2회 투여하는 외용 온단세트론 (일례로 크림, 젤, 또는 로션 형태)이 효과적이다. 본 발명은 또한, 일부 환자에 있어서 외용 온단세트론이 농포 및 구심성 주사 및 안면 홍조증 및 홍반을 감소시킬 수 있음을 개시한다.In the present invention, topical ondansetron (such as cream, gel, or lotion form) administered once or twice daily for the treatment of hot flashes is effective. The present invention also discloses that in some patients, external ondansetron can reduce pustules and afferent injections and hot flashes and erythema.

그 결과, 본 발명은 주사 치료용 외용 약학 조성물의 제조를 위한 온단세트론의 유효량의 용도에 관련되며, 또한 안면 홍조가 뚜렷한 단계에서 주사의 치료, 바람직하게는 홍반, 부종, 안면 홍조증 및 눈으로 이루어지는 군에서 선택되는 증상이 명백한 경우의 단계에서 주사를 치료하는, 주사 치료를 위한 온단세트론의 용도에 관련된다.As a result, the present invention relates to the use of an effective amount of ondansetron for the preparation of external pharmaceutical compositions for injection treatment, and also to the group consisting of the treatment of injections, preferably erythema, edema, hot flashes and eyes, in the stage where facial flushing is pronounced. It relates to the use of ondansetron for injection therapy to treat injection at a stage where the symptom selected at is apparent.

주사는, 만성, 재발성 질환으로, 장기간의 치료가 보통 필요하다. 온단세트론의 장기간 외용 사용에 의해 증상 조절이 성공적으로 유지 가능하다.Injection is a chronic, recurrent disease that usually requires long-term treatment. Symptomatic control can be successfully maintained by long-term external use of ondansetron.

본 발명의 기타 특성, 양태, 목적 및 장점은, 하기의 내용 및 발명의 기술을 위한 제한이 아닌 다양하고 간결한 실시예를 읽음에 따라 보다 명백해 질 것이다.Other features, aspects, objects, and advantages of the invention will become more apparent upon reading a variety of concise examples, which are not intended to be limiting for the following content and description of the invention.

바람직하게, 본 발명의 약학 조성물은, 외용을 위한 것이다. 보다 특별하게, 본 약학 조성물은 피부학적 조성물이다.Preferably, the pharmaceutical composition of the present invention is for external use. More particularly, the pharmaceutical composition is a dermatological composition.

본 발명의 그러한 조성물은, 항염증 유효량의 온단세트론 및 그를 위한 약학 허용 외용 담체를 포함하는, 염증 외용 치료용 조성물이다.Such a composition of the present invention is a composition for treating external inflammation, comprising an anti-inflammatory effective amount of ondansetron and a pharmaceutically acceptable external carrier therefor.

보다 일반적으로, 피부학적 조성물은 하나 이상의 혈관 상처, 하나의 염증 성분 또는 동시에 하나의 염증 및 하나의 감염 성분을 가지는 피부 질환 또는 병소의 외용 경로를 통한 치료를 위한 것이다.More generally, the dermatological composition is for treatment via the external route of a skin disease or lesion having one or more vascular wounds, one inflammatory component or one inflammation and one infectious component at the same time.

보다 특별하게, 피부 질환 또는 병소는, 습진, 건선, 주사, 보통 여드름, 궤양, 지루성 피부염 및 화학물질, 물리적 또는 기계적 제제 또는 기타에 의해 초래된 자극상태와 같은 임의 타입의 피부병을 수반하는 피부 염증에 해당하는 것이다. 본 발명은 특히 온단세트론을 이용한 주사의 외용 치료에 유용하다.More specifically, a skin disease or lesion is an inflammation of the skin accompanied by any type of skin disease, such as eczema, psoriasis, injections, acne, ulcers, seborrheic dermatitis and irritants caused by chemicals, physical or mechanical agents, or others. It corresponds to. The invention is particularly useful for the external treatment of injections with ondansetron.

하기에서 '외용 경로'는, 피부 또는 눈과 같은 신체의 일부 표면 (또는 외부)에 직접 적용하는 제품의 투여를 위한 임의의 기법으로 이해된다.In the following the 'external route' is understood as any technique for the administration of a product which is applied directly to some surface (or outside) of the body, such as the skin or eyes.

외용 경로에 의해, 온단세트론 기재 약학 조성물은 따라서 특히 피부 또는 점막의 치료를 위한 것이며, 이는 연고, 크림, 밀크, 샐브 (salve), 분말, 함침 패드. 용액, 젤, 스프레이, 로션 또는 현탁액의 형태로 제공 가능하다. 이는 또한 지방 또는 중합체 베지클 또는 나노스피어 또는 마이크로스피어 형태 또는, 서방성 제제를 가능하게 하는 중합체 패치 또는 하이드로젤의 형태로 제공 가능하다. 나아가 이들 조성물은 외용 경로에 의해, 임상 지표에 따라 무수 형태 또는 수성 형태로 제공 가능하다. 특히 본 발명의 실시예에, 본 발명의 실시의 면에서 매우 특히 적합한 외용제제가 주어져 있다.By external route, ondansetron based pharmaceutical compositions are thus particularly for the treatment of skin or mucous membranes, which are ointments, creams, milks, salves, powders, impregnation pads. It may be provided in the form of a solution, gel, spray, lotion or suspension. It may also be provided in the form of fat or polymer vesicles or nanospheres or microspheres, or in the form of polymer patches or hydrogels that allow sustained release formulations. Furthermore, these compositions can be provided in anhydrous form or in aqueous form by external routes, depending on clinical indicators. In particular, examples of the present invention are given very particularly suitable external preparations in terms of the practice of the present invention.

본 발명의 바람직한 구현에서, 외용 조성물은 젤, 크림 또는 로션 형태이다.In a preferred embodiment of the invention, the external composition is in the form of a gel, cream or lotion.

눈을 통한 경로에서, 본 발명의 조성물은 주로 눈 세정액이다.In the pathway through the eye, the composition of the present invention is mainly an eye wash.

바람직하게는 외용인 본 발명의 조성물은, 조성물 총 중량에 대해 바람직하게 0.01-5 중량%, 더 바람직하게 0.5 중량%, 가장 바람직하게 0.75 중량% 농도의 온단세트론을 포함한다.The composition of the invention, which is preferably external, preferably comprises ondansetron at a concentration of 0.01-5% by weight, more preferably 0.5% by weight and most preferably 0.75% by weight relative to the total weight of the composition.

본 발명의 특별하면서도 바람직한 구현에서 온단세트론의 총함량은 조성물 총중량의 5-10%를 초과하지 않는다. 바람직하게, 의약 조성물은 3개월의 기간동안 하루당 2회 외용 적용된다.In a particular and preferred embodiment of the invention the total content of ondansetron does not exceed 5-10% of the total weight of the composition. Preferably, the pharmaceutical composition is applied externally twice a day for a period of three months.

본 발명의 의약 조성물은, 비활성 또는 특히 다음과 같은 약학 또는 화장학적 활성 첨가제 또는 이들 첨가제의 조합을 물론 포함 가능하다: 습윤제; 탈색소제, 일례로 히드로퀴논, 아젤산, 카페인산 또는 코지산; 연화제; 수화제, 일례로 글리세롤, PEG400, 티아몰포리논 및 그 유도체 또는 대안적으로 유레아; 항지루제 또는 항여드름제, 일례로 S-카복시메틸시스테인, S-벤질시스테아민, 그 염 및 그 유도체 또는 벤조일 퍼옥시드; 살진균제, 일례로 케토코나졸 또는 4,5-폴리메틸렌-3-이소티아졸리돈; 카로티노이드 및 특히 베타-카로틴; 항건선제, 일례로 안트랄린 및 그 유도체; 그리고 마지막으로 5,8,11,14-에이코사테트라인산 및 5,8,11-에이코사트리인산 및 그 에스터 및 아미드; 메트로니다졸, 이베르멕틴 및 주사 치료에 사용되는 기타 시약; 항 염증제, 일례로 NSIDS.The pharmaceutical compositions of the present invention may, of course, comprise inert or in particular pharmaceutical or cosmetically active additives or combinations of these additives: wetting agents; Depigmentants such as hydroquinone, azelic acid, caffeic acid or kojic acid; Softeners; Hydrating agents such as glycerol, PEG400, thiamorpholinone and derivatives thereof or alternatively urea; Anti-seborrheic or anti-acne agents such as S-carboxymethylcysteine, S-benzylcysteamine, salts thereof and derivatives thereof or benzoyl peroxide; Fungicides such as ketoconazole or 4,5-polymethylene-3-isothiazolidone; Carotenoids and especially beta-carotene; Anti-psoriasis agents such as anthraline and derivatives thereof; And finally 5,8,11,14-eicosatetraic acid and 5,8,11-eicosatatric acid and esters and amides thereof; Metronidazole, ivermectin and other reagents used for injection treatment; Anti-inflammatory agents, for example NSIDS.

본 발명의 조성물은 또한 향미 개선제, 보존제, 일례로 파라히드록시벤조산의 에스터, 안정화제, 습도 조절제, pH 조절제, 삼투압 변형제, 에멀젼화제, UV-A 및 UV-B 차단제 및 항산화제, 일례로 알파-토코페롤, 부틸화 히드록시아니솔 또는 부틸화 히드록시톨루엔을 포함 가능하다.The compositions of the present invention may also contain flavor improvers, preservatives, such as esters of parahydroxybenzoic acids, stabilizers, humidity regulators, pH regulators, osmotic pressure modifiers, emulsifiers, UV-A and UV-B blockers and antioxidants, for example Alpha-tocopherol, butylated hydroxyanisole or butylated hydroxytoluene.

물론, 당업자는, 상기 약학 조성물에 첨가하는 임의의 화합물(들)을 선택할 수 있고, 본 조성물 고유의 유리한 특성은, 추구한 첨가에 의해 실질적으로 또는 유해하게 영향을 입지 않는다.Of course, those skilled in the art can select any compound (s) to add to the pharmaceutical composition, and the advantageous properties inherent in the composition are not substantially or detrimentally affected by the desired addition.

본 발명에 따른 각종 구체적 제제의 예시를 위한 다수의 실시예를, 제한을 의도하지 않으면서 하기에 제공한다.Many examples for illustration of various specific agents according to the invention are provided below without intending to be limiting.

실시예 1Example 1

외용 젤 형태로 제공되는 본 발명에 따른 간단한 제제의 예시를 하기에 제공한다.Examples of simple formulations according to the invention in the form of external gels are provided below.

온단세트론 0.75gOndansetron 0.75g

Carbopol 980 (Goodrich) 0.6gCarbopol 980 (Goodrich) 0.6g

폴리에틸렌 글리콜 400 3gPolyethylene Glycol 400 3g

소듐히드록시드 적량, pH 5Sodium hydroxide titrate, pH 5

보존제 적량Preservative

탈미네랄수 100g 되기 위한 적량Appropriate to become 100g of demineralized water

실시예 2Example 2

외용 크림 형태로 제공되는 본 발명에 따른 간단한 제제의 예시를 하기에 제 공한다.An example of a simple formulation according to the present invention in the form of an external cream is provided below.

온단세트론 0.75gOndansetron 0.75g

메틸 글루코스 세스퀴스테아레이트 1g1 g of methyl glucose sesquistearate

스테아릴 알콜 0.5g0.5 g stearyl alcohol

액체 파라핀 오일 6g 6g of liquid paraffin oil

폴리에틸렌 글리콜 400 2gPolyethylene Glycol 400 2g

메틸 글루코스 세스퀴스테아레이트Methyl Glucose Sesquistearate

(20mol EO로 폴리옥시에틸렌화됨) 5g(Polyoxyethylenated with 20 mol EO) 5 g

Carbopol 981 (Goodrich) 0.4gCarbopol 981 (Goodrich) 0.4g

글리세롤 7gGlycerol 7g

시클로메티콘 4gCyclomethicone 4g

소듐히드록시드 적량, pH 5Sodium hydroxide titrate, pH 5

보존제 적량Preservative

탈미네랄수 100g 되기 위한 적량Appropriate to become 100g of demineralized water

실시예 3Example 3

외용 로션 형태로 제공되는 본 발명에 따른 간단한 제제의 예시를 하기에 제공한다.Examples of simple formulations according to the invention in the form of external lotions are provided below.

온단세트론 0.75gOndansetron 0.75g

벤질알콜 1.30Benzyl Alcohol 1.30

글리세롤 7.00Glycerol 7.00

스테아릴 알콜 2.00Stearyl Alcohol 2.00

경광물유 6.00Light mineral oil 6.00

Carbomer 941 0.15Carbomer 941 0.15

글리세릴 스테아레이트 3.00Glyceryl Stearate 3.00

포타슘 소르베이트 0.20Potassium Sorbate 0.20

시클로메티콘 4.00Cyclomethicone 4.00

PEG-8 2.00PEG-8 2.00

Steareth-21 3.00Steareth-21 3.00

락트산 적량, pH 조절Lactic acid, pH adjustment

소듐히드록시드 적량, pH 조절Sodium Hydroxide, pH Control

정제수 적량, 100.00Appropriate amount of purified water, 100.00

Claims (13)

온단세트론, 그 염 또는 염기의 항염증 유효량의, 염증 치료를 위한 외용 약학 조성물 제조에 사용되는 용도.Use of an anti-inflammatory effective amount of ondansetron, a salt or a base thereof for the manufacture of an external pharmaceutical composition for the treatment of inflammation. 제 1 항에 있어서, 상기 약학 조성물 내에 존재하는 온단세트론의 양이, 약학 조성물의 총중량에 대해 약 0.01 내지 5중량% 범위인 용도.Use according to claim 1, wherein the amount of ondansetron present in the pharmaceutical composition is in the range of about 0.01 to 5% by weight relative to the total weight of the pharmaceutical composition. 제 1 항에 있어서, 상기 염증의 치료가 피부 질환의 치료를 포함하는 용도.Use according to claim 1, wherein the treatment of inflammation comprises treatment of a skin disease. 제 3 항에 있어서, 상기 피부 질환이 피부병을 수반하는 용도.4. Use according to claim 3, wherein the skin disease involves skin disease. 제 4 항에 있어서, 상기 피부병이, 습진, 건선, 주사 여드름, 보통 여드름, 궤양, 지루성 피부염 및 화학물질, 물리적 또는 기계적 제제에 의해 초래된 자극상태로 이루어진 군에서 선택되는 용도.5. Use according to claim 4, wherein said dermatosis is selected from the group consisting of eczema, psoriasis, injection acne, common acne, ulcers, seborrheic dermatitis and irritation caused by chemicals, physical or mechanical agents. 제 4 항에 있어서, 상기 피부병이 주사 (rosacea)인 용도.5. Use according to claim 4, wherein said skin disease is rosacea. 주사 치료용 외용 약학 조성물 제조를 위한 온단세트론 유효량의 용도.Use of an ondansetron effective amount for the preparation of an external pharmaceutical composition for injection treatment. 제 7 항에 있어서, 안면 홍조가 뚜렷한 단계에서 주사가 치료되는 용도.8. Use according to claim 7, wherein the injection is treated at a stage in which hot flashes are pronounced. 제 7 항에 있어서, 습진, 부종, 안면 홍조증 및 눈으로 이루어진 군에서 선택되는 증상이 뚜렷한 단계에서 주사가 치료되는 용도.8. Use according to claim 7, wherein the injection is treated at a stage at which symptoms are selected from the group consisting of eczema, edema, hot flashes and eyes. 온단세트론의 항염증 유효량 및 이를 위한 외용의 약학적으로 허용되는 담체를 함유하는, 염증 외용 치료용 조성물.An anti-inflammatory effective amount of ondansetron and a pharmaceutically acceptable carrier for external use therefor, A composition for treating external inflammation. 제 10 항에 있어서, 젤 형태의 조성물.The composition of claim 10 in the form of a gel. 제 10 항에 있어서, 크림 형태의 조성물.The composition of claim 10 in the form of a cream. 제 10 항에 있어서, 로션 형태의 조성물.The composition of claim 10 in the form of a lotion.
KR1020067011213A 2003-12-10 2004-12-06 Use of ondansetron for the treatment of inflammation and pharmaceutical composition thereof Ceased KR20060118530A (en)

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US52858703P 2003-12-10 2003-12-10
US60/528,587 2003-12-10
EP04291328A EP1600158A1 (en) 2004-05-26 2004-05-26 Use of ondansetron for the treatment of inflammation, and pharmaceutical compositions thereof
EP04291328.5 2004-05-26

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