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81. 发明公开

KR1020140006729A 로티고틴 함유 경피흡수제제 有权
标题翻译：包含ROTIGOTINE的透皮组合物
公开(公告)号：KR1020140006729A
公开(公告)日：2014-01-16
申请号：KR1020130079879
申请日：2013-07-08
申请人： 에스케이케미칼주식회사
发明人： 김혜민 , 황용연 , 윤원노 , 박여진 , 오준교 , 임종섭 , 김훈택
IPC分类号： A61K9/70 , A61K31/381
CPC分类号： A61K9/0014 , A61K9/7023 , A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K31/381 , A61K47/32
摘要： The present invention relates to a method for preparing a transdermal preparation comprising rotigotine as an active ingredient, and more particularly, to a method for preparing a transdermal preparation, comprising a step of mixing rotigotine and an ethylene-vinyl acetate adhesive at a weight ratio of 1:0.1 to 20. Further, the present invention relates to a transdermal preparation prepared by the method and a transdermal therapeutic system. The preparation and system of the present invention prevent the precipitation of rotigotine to improve the long-term storage stability and effectively release the rotigotine, and thus can be effectively applied in the preparation of rotigotine-containing patches. [Reference numerals] (AA) Sample 1; (BB) Sample 2; (CC) Sample 3; (DD) Sample 4
摘要翻译：本发明涉及一种制备包含罗替戈汀作为活性成分的透皮制剂的方法，更具体地说，涉及一种制备透皮制剂的方法，包括将罗替戈汀和乙烯 - 乙酸乙烯酯粘合剂以重量比 1：0.1〜20。此外，本发明涉及通过该方法制备的透皮制剂和透皮治疗系统。本发明的制剂和系统可防止罗替戈汀的沉淀，从而提高长期保存稳定性，有效释放罗替戈汀，可有效应用于含有罗替戈汀的贴剂。（附图标记）（AA）样品1; （BB）样品2; （CC）样品3; （DD）样品4

82. 发明公开

KR1020140006727A 로티고틴을 함유한 경피흡수제제 有权
标题翻译：包含ROTIGOTINE的透皮组合物
公开(公告)号：KR1020140006727A
公开(公告)日：2014-01-16
申请号：KR1020130079198
申请日：2013-07-05
申请人： 에스케이케미칼주식회사
发明人： 김혜민 , 황용연 , 윤원노 , 박여진 , 오준교 , 임종섭 , 김훈택
IPC分类号： A61K9/70 , A61K31/381
CPC分类号： A61K47/12 , A61K9/0014 , A61K9/7053 , A61K31/381 , A61K47/10 , A61K47/14 , A61K47/32
摘要： The present invention relates to a method for preventing the crystallization of rotigotine. Further, the present invention relates to a method for preventing the precipitation of rotigotine crystals, wherein the method comprises a step of mixing rotigotine with at least one selected from the group consisting of fatty alcohols, fatty acids, fatty acid esters, fatty acid amides, and derivatives thereof. Further, the present invention relates to a transdermal preparation comprising rotigotine and a crystallization inhibitor. The methods and systems of the present invention prevent the precipitation of rotigotine to improve the long-term storage stability, and thus can be effectively applied in the preparation of rotigotine-containing patches. [Reference numerals] (140) Controller; (150) Alarm generator; (AA) Low-concentration odor; (BB) High-concentration odor
摘要翻译：本发明涉及一种防止罗替戈汀结晶的方法。此外，本发明涉及一种防止罗替戈汀晶体沉淀的方法，其中该方法包括将罗替戈汀与选自脂肪醇，脂肪酸，脂肪酸酯，脂肪酸酰胺，及其衍生物。此外，本发明涉及包含罗替戈汀和结晶抑制剂的透皮制剂。本发明的方法和系统防止罗替戈汀的沉淀以改善长期储存稳定性，因此可有效地应用于制备含有罗替戈汀的贴剂。（附图标记）（140）控制器; （150）报警发生器; （AA）低浓度气味; （BB）高浓度气味

83. 发明授权

KR101328620B1 신생혈관생성 억제용 조성물 有权
标题翻译：抗血管生成组合物
公开(公告)号：KR101328620B1
公开(公告)日：2013-11-13
申请号：KR1020060066905
申请日：2006-07-18
申请人： 에스케이케미칼주식회사
发明人： 선원석 , 최원락 , 최상근 , 한창균 , 윤미선 , 김태곤 , 김택수 , 임광진 , 신동철 , 김웅식 , 오준교 , 성진흥 , 엄기안 , 조용백
IPC分类号： A61K31/7016 , A61P35/00
CPC分类号： A61K36/258 , A61K31/56 , A61K31/704
摘要： 본 발명은 진세노사이드 Rg3가 함유된 신생혈관생성 억제용 조성물에 관한 것으로서, 더욱 상세하게는 혈관 내피세포 성장인자 수용체-1(VEGFR-1 : vascular endothelial growth factor receptor-1)의 활성 저해 및 혈관 내피세포 성장인자(VEGF)의
in vivo 레벨(level)을 낮추어줌으로써 우수한 신생혈관생성(angiogenesis) 억제활성과 이에 따른 종양 성장 억제활성을 갖는 20(S)-진세노사이드 Rg3가 40 내지 60 %(w/w) 함유된 조성물에 관한 것이다.
혈관 내피세포 성장인자, 신생혈관생성 억제, 20(S)-진세노사이드 Rg3

84. 发明公开

KR1020120126898A 리바스티그민 또는 이의 염을 함유하는 경피 투여 조성물 无效
标题翻译：包含利凡斯的明或其盐的透皮组合物
公开(公告)号：KR1020120126898A
公开(公告)日：2012-11-21
申请号：KR1020110045023
申请日：2011-05-13
申请人： 에스케이케미칼주식회사
发明人： 황용연 , 최원재 , 김재선 , 윤원노 , 박여진 , 오준교 , 임종섭
IPC分类号： A61K31/325 , A61K31/195 , A61K9/70
CPC分类号： A61K31/27 , A61K9/0014 , A61K31/192 , A61K2300/00
摘要： PURPOSE: A transdermal composition containing rivastigmine or salt thereof with improved storage stability is provided to enable long-term storage. CONSTITUTION: A composition with improved storage stability contains rivastigmine or pharmaceutically acceptable salt thereof and gentisic acid. The composition is a transdermal composition applied to the skin. The composition also applied to a patch. The composition is used for treating Alzheimer's disease type dementia or Parkinson's disease type dementia.
摘要翻译：目的：提供具有改善的储存稳定性的含有伐罗斯的明或其盐的透皮组合物，以便能够长期储存。构成：具有改善的储存稳定性的组合物包含利伐斯的明或其药学上可接受的盐和龙胆酸。该组合物是施用于皮肤的透皮组合物。该组合物也适用于贴剂。该组合物用于治疗阿尔茨海默病型痴呆或帕金森病型痴呆。

85. 发明公开

KR1020090101146A 저장안정성이 우수한 파클리탁셀 함유 주사제 조성물의 제조방법 有权
标题翻译：制备含有PACLITAXEL的稳定药用组合物的方法
公开(公告)号：KR1020090101146A
公开(公告)日：2009-09-24
申请号：KR1020090079338
申请日：2009-08-26
申请人： 에스케이케미칼주식회사
发明人： 김남호 , 이진영 , 김재선 , 이남규 , 장우제 , 오준교 , 이윤정 , 김웅식 , 성진흥 , 엄기안
IPC分类号： A61K9/08 , A61K31/335 , A61K47/40 , A61P35/00
摘要： PURPOSE: A method for producing an injection composition containing a paclitacel is provided to produce the injection composition without side effect. CONSTITUTION: A method for producing an injection composition containing a paclitacel having improved storage stability comprises a step of mixing water soluble polymer of paclitacel, cyclodextrin, and polyvinylpyrrolidone (PVP) in distilled water; a step of stirring the mixture solution and freeze-drying; and a step of diluting the freeze-dried composition in dextrose solution or saline solution to produce the injection composition.
摘要翻译：目的：提供一种制备含有紫杉醇的注射组合物的方法以产生无副作用的注射组合物。构成：含有具有改善的储存稳定性的紫杉醇的注射组合物的制备方法包括将蒸馏水中的紫杉醇，环糊精和聚乙烯吡咯烷酮（PVP）的水溶性聚合物混合的步骤; 搅拌混合溶液并冷冻干燥的步骤; 以及在葡萄糖溶液或盐水溶液中稀释冷冻干燥组合物以产生注射组合物的步骤。

86. 发明授权

KR100917810B1 저장안정성이 우수한 파클리탁셀 함유 주사제 조성물 有权
标题翻译：含有紫杉醇的稳定药物组合物
公开(公告)号：KR100917810B1
公开(公告)日：2009-09-18
申请号：KR1020070054058
申请日：2007-06-01
申请人： 에스케이케미칼주식회사
发明人： 김남호 , 이진영 , 김재선 , 이남규 , 장우제 , 오준교 , 이윤정 , 김웅식 , 성진흥 , 엄기안
IPC分类号： A61K9/08 , A61K47/40 , A61K31/335
摘要： 본 발명은 저장안정성이 우수한 파클리탁셀 함유 주사제 조성물에 관한 것으로서, 더욱 상세하게는 비수용성 화합물인 파클리탁셀을 수용액 내에서 안정화시켜 제제화하기 위하여 시클로덱스트린과 폴리비닐피롤리돈(PVP)의 수용성 고분자를 증류수에 혼합하여 용해시키고 이를 동결건조하여 동결건조 조성물을 제조함으로써 기존 파클리탁셀 제제보다 저장안정성이 우수한 파클리탁셀 함유 주사제 조성물에 관한 것이다.
파클리탁셀, 시클로덱스트린, 수용성 고분자

87. 发明公开

KR1020080062434A 경구용 성기능 장애 치료용 조성물 无效
标题翻译：用于口服剂型的男性精神分裂症治疗药物组合物
公开(公告)号：KR1020080062434A
公开(公告)日：2008-07-03
申请号：KR1020060138236
申请日：2006-12-29
申请人： 에스케이케미칼주식회사
发明人： 오준교 , 장우제 , 윤원노 , 엄기안
IPC分类号： A61K9/28 , A61K31/437 , A61P15/10
CPC分类号： A61K31/519 , A61K9/0053 , A61K9/20 , A61K9/48
摘要： A composition is provided to show high elution rate under the acidic condition and improved stability at room temperature, thereby being effectively used for improving and treating sexual dysfunction without side effects. A composition for treating sexual dysfunction comprises 15-30 wt.% of a pyrrolopyrimidinone compound hydrochloride represented by a formula(1) and 2-15 wt.% of croscarmellose sodium or crospovidone. The composition further comprises a pharmaceutically acceptable excipient and a lubricant.
摘要翻译：提供了一种在酸性条件下显示高洗脱速率并在室温下提高稳定性的组合物，从而有效地用于改善和治疗性功能障碍而没有副作用。用于治疗性功能障碍的组合物包含15-30重量％的由式（1）表示的吡咯并嘧啶酮化合物盐酸盐和2-15重量％的交联羧甲纤维素钠或交聚维酮。组合物还包含药学上可接受的赋形剂和润滑剂。

88. 发明公开

KR1020080055355A 보관안정성이 우수한 클로피도그렐 함유 포접 복합체 无效
标题翻译：包括CLOPIDOGREL和BETA-CYCLODEXTRIN的复合物
公开(公告)号：KR1020080055355A
公开(公告)日：2008-06-19
申请号：KR1020060128593
申请日：2006-12-15
申请人： 에스케이케미칼주식회사
发明人： 김재선 , 김남호 , 이진영 , 이남규 , 오준교 , 신지영 , 김태곤 , 윤미선 , 성진흥 , 이윤정 , 박여진 , 엄기안
IPC分类号： A61K47/40 , A61K31/4365
CPC分类号： A61K47/40 , C07D495/04
摘要： An inclusion complex of clopidogrel having platelet-aggregating activity and beta-cyclodextrin is provided to improve storage stability of clopidogrel having hygroscopy in a form of free base by reacting with cyclodextrin, and offer physical properties suitable for preparation of formulation. An inclusion complex of clopidogrel represented by the formula(1), having improved storage stability contains the clopidogrel and beta-cyclodextrin in an equivalent ratio of 1:1.0-2.0. A method for preparing the inclusion complex of clopidogrel comprises the steps of: (1) solubilizing clopidogrel in distilled water or acidic solution; (2) adding the solution of step (1) into the distilled water or acidic solution containing 1.0-2 equivalent of beta-cyclodextrin based on 1 equivalent of clopidogrel, and stirring the mixture at 30-70 deg. C; (3) neutralizing the reaction product with hydroxide of alkali metal at 0-50 deg. C; and (4) filtering, washing and drying the reaction product, wherein the clopidogrel is clopidogrel base selected from free base, premix, adsorbate or solid dispersant of clopidogrel, or clopidogrel salt selected from clopidogrel bisulfate, clopidogrel hydrochloride, clopidogrel bromate and clopidogrel benzensulfonate. A composition for inhibiting platelet aggregation comprises the inclusion complex of clopidogrel and beta-cyclodextrin.
摘要翻译：提供了具有血小板聚集活性和β-环糊精的氯吡格雷的包合物，以通过与环糊精反应来提高具有游离碱形式的吸湿作用的氯吡格雷的储存稳定性，并提供适于制备制剂的物理性质。由式（1）表示的具有改善的储存稳定性的氯吡格雷的包合络合物含有当量比为1：1.0-2.0的氯吡格雷和β-环糊精。制备氯吡格雷包合物的方法包括以下步骤：（1）将氯吡格雷溶解于蒸馏水或酸性溶液中; （2）将步骤（1）的溶液加入到含有1.0当量的β-环糊精的蒸馏水或酸性溶液中，基于1当量的氯吡格雷，并在30-70℃搅拌该混合物。 C; （3）在0-50℃下用碱金属氢氧化物中和反应产物。 C; （4）过滤，洗涤和干燥反应产物，其中氯吡格雷是选自氯吡格雷的游离碱，预混物，吸附物质或固体分散剂，或氯吡格雷硫酸盐，盐酸氯吡格雷，溴酸氯吡格雷和苯磺酸盐的氯吡格雷盐。用于抑制血小板聚集的组合物包含氯吡格雷和β-环糊精的包合物。

89. 发明公开

KR1020080007798A 신생혈관생성 억제용 조성물 有权
标题翻译：抗生素组成
公开(公告)号：KR1020080007798A
公开(公告)日：2008-01-23
申请号：KR1020060066905
申请日：2006-07-18
申请人： 에스케이케미칼주식회사
发明人： 선원석 , 최원락 , 최상근 , 한창균 , 윤미선 , 김태곤 , 김택수 , 임광진 , 신동철 , 김웅식 , 오준교 , 성진흥 , 엄기안 , 조용백
IPC分类号： A61K31/7016 , A61P35/00
CPC分类号： A61K36/258 , A61K31/56 , A61K31/704
摘要： A composition comprising 20-(S)-ginsenoside Rg3 is provided to inhibit the activity of VEGFR-1(vascular endothelial growth factor receptor-1) and lower the in vivo level of the VEGF, thereby showing excellent angiogenesis inhibiting activity and tumor growth inhibiting activity. A composition for preventing and treating cancer by Inhibiting angiogenesis comprises 40-60 wt.% of 20-(S)-ginsenoside Rg3, wherein the cancer is skin cancer or lung cancer and a daily dosage for adult is 1-1,000 mg. The composition is formulated into an injection or an orally administered formulation.
摘要翻译：提供包含20-（S） - 人参皂苷Rg3的组合物以抑制VEGFR-1（血管内皮生长因子受体-1）的活性并降低VEGF的体内水平，从而显示优异的血管生成抑制活性和抑制肿瘤生长活动。通过抑制血管生成预防和治疗癌症的组合物包含40-60重量％的20-（S） - 人参皂苷Rg3，其中癌症是皮肤癌或肺癌，并且成人的日剂量为1-1,000mg。将组合物配制成注射剂或口服制剂。

90. 发明公开

KR1020080003600A 피롤로피리미디논 유도체의 말리에이트 염 및 이의제조방법 无效
标题翻译：吡咯烷二酮衍生物的制备及其制备方法
公开(公告)号：KR1020080003600A
公开(公告)日：2008-01-08
申请号：KR1020060062042
申请日：2006-07-03
申请人： 에스케이케미칼주식회사
发明人： 김재선 , 김남호 , 이진영 , 이남규 , 이윤정 , 장우제 , 윤원노 , 오준교 , 성진흥 , 엄기안
IPC分类号： C07D487/04
摘要： A maleate of pyrrolopyrimidinone derivative having inhibitory effects on PDE-5(phosphodiesterase 5) is provided to improve stability against temperature, water and light, and physicochemical properties so as to be used as a pharmaceutically acceptable salt, so that the compound is useful for prevention and treatment of disease associated with PDE-5. A maleate of pyrrolopyrimidinone derivative having inhibitory effects on PDE-5, represented by the formula(1) is prepared by reacting pyrrolopyrimidinone represented by the formula(2) with maleic acid represented by the formula(3) at -30 to 50 deg.C. A pharmaceutical composition for treating impotence comprises the maleate of pyrrolopyrimidinone derivative represented by the formula(1), and is formulated as tablet, capsule or injection. A pharmaceutical composition for treating pulmonary arterial hypertension, chronic obstructive pulmonary disease, benign prostatic hypertrophy and lower urinary tract symptom comprises the maleate of pyrrolopyrimidinone derivative represented by the formula(1).
摘要翻译：提供具有对PDE-5（磷酸二酯酶5）具有抑制作用的吡咯并嘧啶酮衍生物的马来酸盐，以提高对温度，水和光的稳定性和物理化学性质，以便用作药学上可接受的盐，使得该化合物可用于预防和治疗与PDE-5相关的疾病。由式（2）表示的吡咯并嘧啶酮与式（3）表示的马来酸在-30〜50℃反应制备对式（1）表示的PDE-5具有抑制作用的吡咯并嘧啶酮衍生物的马来酸盐。。用于治疗阳A的药物组合物包含由式（1）表示的吡咯并嘧啶酮衍生物的马来酸盐，并且配制成片剂，胶囊剂或注射剂。用于治疗肺动脉高压，慢性阻塞性肺病，良性前列腺肥大和下尿路症状的药物组合物包含由式（1）表示的吡咯并嘧啶酮衍生物的马来酸盐。

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