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公开(公告)号：KR100580577B1
公开(公告)日：2006-05-16
申请号：KR1020030064633
申请日：2003-09-18
Applicant: 한국화학연구원
Abstract: 본 발명은 자가 미세 유화형 약물 전달 시스템을 이용하는 약물 조성물에 관한 것으로서, 상기 약물 조성물은 소염 진통제의 활성 성분 1 내지 40 중량%; 계면활성제 5 내지 50 중량%; 용해제 10 내지 50 중량%; 공계면활성제 10 내지 50 중량%; pH 조절제 0.1 내지 5 중량%; 및 항산화제 1 내지 5 중량%를 포함하는 나노 에멀젼 농축액을 포함하는 자가 미세 유화형 약물 전달 시스템을 이용하는 것이다.
본 발명의 핵심은 소염 진통제인 덱시부프로펜을 자가미세유화형 약물전달시스템에 적용하여 신속한 약효를 발현하고 부작용을 최소화하는 방법으로서 다수의 산업 재산권 획득 이외에도 국내 기술의 자립성, 신기술의 축적뿐만 아니라 기술 수출로 이어질 것으로 예상된다.
덱시부프로펜,나노에멀젼농축액,용해제,계면활성제,공계면활성제,자가미세유화형 약물전달시스템,연질캡슐제,pH조절제,항산화제.-
公开(公告)号：KR1020080004646A
公开(公告)日：2008-01-10
申请号：KR1020060063214
申请日：2006-07-06
Applicant: 제이더블유중외제약 주식회사 , 한국화학연구원
IPC: C07D471/04
CPC classification number: Y02P20/55 , C07D471/04
Abstract: A 2-alkylenyloxy-3-ethynylpyrido[2,3-b]pyrazine derivative is provided to be usefully used as an anticancer agent by using excellent HIF-1alpha gene expression inhibitory activity thereof. A 2-alkylenyloxy-3-ethynylpyrido[2,3-b]pyrazine derivative is represented by the formula(1), where A is selected from the group consisting of alkyl, aryl, and heteroaryl; Y is a single bond, or an alkylene which may be substituted by one to five substituents selected from the group consisting of hydroxy, alkyl-OH, O-alkyl and phenyl; Z is selected from the group consisting of H, halogen, hydroxy, alkyl, alkyl-OH, alkenyl, haloalkyl, O-alkyl, O-haloalkyl, O-aryl, O-heteroaryl, O-heterocycle, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-heterocycle, O-alkyl-NH2, O-alkyl-NH(alkyl), O-alkyl-N(alkyl)2, C(O)alkyl, alkyl-C(O)alkoxy, C(O)NH2, C(O)NH(alkyl), C(O)N(alkyl)2, C(O)NH(aryl), C(O)N(aryl)2, C(O)NH(heteroaryl), C(O)N(heteroaryl)2, C(O)O-alkyl, C(O)O-aryl, C(O)O-heteroaryl, OC(O)-alkyl, OC(O)-aryl, OC(O)heteroaryl, OC(O)NH2, OC(O)NH(alkyl), OC(O)N(alkyl)2, OC(O)N(alkyl)N(alkyl)2, OC(O)NH(aryl), OC(O)NH(heteroaryl), NH2, NH(alkyl), N(alkyl)2, NH(aryl), N(alkyl)(aryl), N(aryl)2, NH(heteroaryl), etc., provided that a compound that the A is methyl, and Y-Z is H is excluded. A pharmaceutical composition for treating and preventing cancer comprises the 2-alkylenyloxy-3-ethynylpyrido[2,3-b]pyrazine derivative or a pharmaceutically acceptable salt thereof.
Abstract translation: 提供2-亚烷基氧基-3-乙炔基吡啶并[2,3-b]吡嗪衍生物通过使用优异的HIF-1α基因表达抑制活性可用作抗癌剂。 2-烷基氧基-3-乙炔基吡啶并[2,3-b]吡嗪衍生物由式（1）表示，其中A选自烷基，芳基和杂芳基; Y是单键，或可以被一至五个选自羟基，烷基-OH，O-烷基和苯基的取代基取代的亚烷基; Z选自H，卤素，羟基，烷基，烷基-OH，烯基，卤代烷基，O-烷基，O-卤代烷基，O-芳基，O-杂芳基，O-杂环，O-烷基 - 芳基， O-烷基 - 杂芳基，O-烷基 - 杂环，O-烷基-NH 2，O-烷基-NH（烷基），O-烷基-N（烷基）2，C（O）烷基，烷基-C（O） ，C（O）NH 2，C（O）NH（烷基），C（O）N（烷基）2，C（O）NH（芳基），C（O）N（芳基）2，C（O） （O）O-杂芳基，C（O） - 烷基，OC（O） - 烷基，C（O） 芳基，OC（O）杂芳基，OC（O）NH 2，OC（O）NH（烷基），OC（O）N（烷基）2，OC（O） ）NH（芳基），OC（O）NH（杂芳基），NH 2，NH（烷基），N（烷基）2，NH（芳基），N（烷基）（芳基），N（芳基）2，NH ）等，条件是排除A为甲基，YZ为H的化合物。 用于治疗和预防癌症的药物组合物包括2-亚烷基氧基-3-乙炔基吡啶并[2,3-b]吡嗪衍生物或其药学上可接受的盐。
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公开(公告)号：KR1020050028409A
公开(公告)日：2005-03-23
申请号：KR1020030064633
申请日：2003-09-18
Applicant: 한국화학연구원
CPC classification number: A61K9/1075 , A61K9/4808 , A61K31/192 , A61K47/20 , A61K47/32
Abstract: A pharmaceutical composition having antiphlogistic-analgestic activity using an oral-micro emulsuion drug delivery system is provided, which composition improves medicinal efficacy expressing time and absorption of hardly soluble drugs, so that the dosage amount of the drugs can be reduced. The pharmaceutical composition having antiphlogistic-analgestic activity using an oral-micro emulsuion drug delivery system comprises 1 to 40 wt.% of antiphlogistic-analgestic active ingredients; 5 to 50 wt.% of surfactant, 10 to 50 wt.% of solubilizing agent; 10 to 50 wt.% of co-surfactant; 0.1 to 5 wt.% of pH regulating agent; and 1 to 5 wt.% of antioxidant, wherein the antiphlogistic-analgestic active ingredient is ibuprofen or dexibuprofen; the surfactant is castor oil, substituted castor oil, tween, span, laborasol and brij; the solubilizing atent is fatty acid ester, vegetable oil, purfied fish oil and pharmaceutically acceptable hydrophobic solubilizing agent; the co-surfactant is selected from glycofurol, polyethyleneglycol, propyleneglycol, dimethylisosorbide, diethyleneglycolmonoethylether, apricot kernel oil, propyleneglycolmonolaurate and tetraglycol; and the pH regulating agent is monoethanolamine, diethanolamine and triethanolamine.
Abstract translation: 提供一种使用口服微乳化药物递送系统具有消炎镇痛活性的药物组合物，该组合物能够改善药物效能，表达时间和难溶性药物的吸收，能够降低药物的配制量。 使用口服微乳化药物递送系统具有消炎止吐活性的药物组合物包含1至40重量％的消炎镇痛活性成分; 5〜50重量％的表面活性剂，10〜50重量％的增溶剂; 10至50重量％的助表面活性剂; 0.1〜5重量％的pH调节剂; 和1至5重量％的抗氧化剂，其中所述消炎镇痛活性成分是布洛芬或右布洛芬; 表面活性剂为蓖麻油，取代蓖麻油，吐温，跨度，实验溶液和布里; 增溶剂是脂肪酸酯，植物油，鱼油和药学上可接受的疏水增溶剂; 辅助表面活性剂选自糖醇，聚乙二醇，丙二醇，二甲基异山梨醇，二乙二醇单乙醚，杏仁油，丙二醇单月桂酸酯和四甘醇; pH调节剂为单乙醇胺，二乙醇胺和三乙醇胺。
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