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1. 发明申请

WO2010030180A2 PEPTIDE FORMULATIONS AND USES THEREOF 审中-公开
标题翻译：肽制剂及其用途
公开(公告)号：WO2010030180A2
公开(公告)日：2010-03-18
申请号：PCT/NL2009/050542
申请日：2009-09-09
申请人： RIJKSUNIVERSITEIT GRONINGEN , AMORIJ, Jean-Pierre , AVANTI, Christina , FRIJLINK, Henderik, Willem , HINRICHS, Wouter, Leonardus, Joseph
发明人： AMORIJ, Jean-Pierre , AVANTI, Christina , FRIJLINK, Henderik, Willem , HINRICHS, Wouter, Leonardus, Joseph
IPC分类号： A61K38/11
CPC分类号： A61K38/11
摘要： The present invention relates to the field of preventive and therapeutic medicine, in particular to peptide formulations. Provided is a p H-buffered aqueous formulation comprising oxytocin, vasopressin or an analogue thereof and at least one non-toxic source of divalent metal ions in a concentration of at least 2 m M, and the use of the formulation for the manufacture of a medicament for therapeutic and/or prophylactic treatments. Also provided is a method for treating or preventing haemorrhage in a subject in need thereof, comprising administering to said subject an effective dosage amount of an oxytocin formulation according to the invention. Further provided is a method for treating or preventing diabetes insipidus or vasodilatory shock in a subject in need thereof, comprising administering to said subject an effective dosage amount of a vasopressin formulation according to the invention.
摘要翻译：本发明涉及预防和治疗药物领域，具体涉及肽制剂。提供了包含催产素，加压素或其类似物和至少一种浓度为至少2mM的二价金属离子的无毒源的磷酸缓冲水性制剂，以及该制剂在制备药物中的用途用于治疗和/或预防性治疗。还提供了用于治疗或预防有需要的受试者的出血的方法，其包括向所述受试者施用有效剂量的根据本发明的催产素制剂。进一步提供了用于治疗或预防有此需要的受试者中的尿崩症或血管舒张性休克的方法，其包括向所述受试者施用有效剂量的根据本发明的加压素制剂。

2. 发明申请

WO2004110538A1 DRY POWDER INHALER AND METHOD FOR PULMONARY INHALATION OF DRY POWDER 审中-公开
标题翻译：干粉的干粉吸入和脉冲吸入方法
公开(公告)号：WO2004110538A1
公开(公告)日：2004-12-23
申请号：PCT/NL2004/000427
申请日：2004-06-16
申请人： RIJKSUNIVERSITEIT GRONINGEN , DE BOER, Anne, Haaije , HAGEDOORN, Paul , FRIJLINK, Henderik, Willem
发明人： DE BOER, Anne, Haaije , HAGEDOORN, Paul , FRIJLINK, Henderik, Willem
IPC分类号： A61M15/00
CPC分类号： A61M15/0091 , A61M15/0003 , A61M15/0028 , A61M15/0043 , A61M15/0045 , A61M2202/064 , A61M2206/16
摘要： A breath actuated dry powder inhaler (1), comprising a substantially disc shaped air circulation chamber (2) for de-agglomeration of entrained powdered medicament using the energy of the inspiratory air stream. The chamber has a substantially circular or polygonal sidewall (3) extending about a central axis (4) between top (5) and bottom walls (6) of the chamber so that the height (h) of the chamber is smaller than its diameter (d). A plurality of air supply channels (7) disposed about the circumference of the chamber, which channels extend from joint or separate air inlets and which channels enter the chamber substantially tangentially to its sidewall. At least one of the supply channels extends through a powder dose supply region (8) of the inhaler. The chamber further comprises an air outlet (9) axially extending from a discharge opening (10) in the centre of the top or bottom wall of the chamber and connects to a discharge channel (12) that extends to a mouthpiece (13). The inhaler comprises at least one further air circulation chamber for de-agglomeration of entrained powdered medicament, the chambers being connected to the mouthpiece in parallel.
摘要翻译：一种呼吸致动的干粉吸入器（1），包括基本盘形的空气循环腔（2），用于使用吸气空气流的能量使夹带的粉末状药物脱附。腔室具有围绕腔室的顶部（5）和底壁（6）之间的中心轴线（4）延伸的大致圆形或多边形的侧壁（3），使得腔室的高度（h）小于其直径（ D）。多个空气供应通道（7）围绕室的周边设置，该通道从关节或分离的空气入口延伸，并且哪些通道基本上相对于其侧壁进入腔室。至少一个供应通道延伸穿过吸入器的粉末剂量供应区域（8）。腔室还包括从腔室顶壁或底壁中心的排放口（10）轴向延伸的空气出口（9），并连接到延伸到接口管（13）的排放通道（12）。吸入器包括至少一个另外的空气循环室，用于夹带的粉末药物的去附聚，这些腔室平行连接到接口管。

3. 发明申请

WO2010030180A3 PEPTIDE FORMULATIONS AND USES THEREOF 审中-公开
标题翻译：肽类制剂及其用途
公开(公告)号：WO2010030180A3
公开(公告)日：2010-09-10
申请号：PCT/NL2009050542
申请日：2009-09-09
申请人： UNIV GRONINGEN , AMORIJ JEAN-PIERRE , AVANTI CHRISTINA , FRIJLINK HENDERIK WILLEM , HINRICHS WOUTER LEONARDUS JOSEPH
发明人： AMORIJ JEAN-PIERRE , AVANTI CHRISTINA , FRIJLINK HENDERIK WILLEM , HINRICHS WOUTER LEONARDUS JOSEPH
IPC分类号： A61K38/11
CPC分类号： A61K38/11
摘要： The present invention relates to the field of preventive and therapeutic medicine, in particular to peptide formulations. Provided is a p H-buffered aqueous formulation comprising oxytocin, vasopressin or an analogue thereof and at least one non-toxic source of divalent metal ions in a concentration of at least 2 m M, and the use of the formulation for the manufacture of a medicament for therapeutic and/or prophylactic treatments. Also provided is a method for treating or preventing haemorrhage in a subject in need thereof, comprising administering to said subject an effective dosage amount of an oxytocin formulation according to the invention. Further provided is a method for treating or preventing diabetes insipidus or vasodilatory shock in a subject in need thereof, comprising administering to said subject an effective dosage amount of a vasopressin formulation according to the invention.
摘要翻译：本发明涉及预防和治疗药物领域，特别涉及肽制剂。提供的是包含催产素，加压素或其类似物的apH缓冲水性制剂和浓度至少为2m M的至少一种无毒的二价金属离子源，并且该制剂用于制备药物用于治疗和/或预防性治疗。还提供了治疗或预防有此需要的受试者出血的方法，包括向所述受试者施用有效剂量的本发明的催产素制剂。还提供了在有需要的受试者中治疗或预防尿崩症或血管扩张性休克的方法，包括向所述受试者施用有效剂量的根据本发明的加压素制剂。

4. 发明申请

WO2004054546A1 FORMULATION FOR FAST DISSOLUTION OF LIPOPHILIC COMPOUNDS 审中-公开
标题翻译：氟化物快速溶解的配方
公开(公告)号：WO2004054546A1
公开(公告)日：2004-07-01
申请号：PCT/NL2003/000847
申请日：2003-11-28
申请人： RIJKSUNIVERSITEIT GRONINGEN , HINRICHS, Wouter, Leonardus, Joseph , VAN DROOGE, Dirk, Jan , FRIJLINK, Henderik, Willem
发明人： HINRICHS, Wouter, Leonardus, Joseph , VAN DROOGE, Dirk, Jan , FRIJLINK, Henderik, Willem
IPC分类号： A61K9/19
CPC分类号： A61K31/4422 , A61K9/145 , A61K9/146 , A61K9/2018 , A61K9/205 , A61K9/2095 , A61K31/5513
摘要： The present invention relates to a pharmaceutical composition comprising at least one lipophilic compound and at least one glass of a sugar, a sugar alcohol, a mixture of sugars, a mixture of sugar alcohols or a mixture of at least one sugar and at least one sugar alcohol, wherein the lipophilic compound is incorporated in the sugar glass. The present invention further relates to a method for manufacturing such a pharmaceutical composition.
摘要翻译：本发明涉及包含至少一种亲脂性化合物和至少一种糖，糖醇，糖混合物，糖醇混合物或至少一种糖和至少一种糖的混合物的药物组合物醇，其中将亲脂性化合物掺入糖玻璃中。本发明还涉及制造这种药物组合物的方法。

5. 发明申请

WO2012158030A2 DRUG DELIVERY SYSTEM 审中-公开
标题翻译：药物递送系统
公开(公告)号：WO2012158030A2
公开(公告)日：2012-11-22
申请号：PCT/NL2012/050336
申请日：2012-05-14
申请人： EMOTIONAL BRAIN B.V. , BLOEMERS, Johannes Martinus Maria , EISSENS, Anko Cornelus , FRIJLINK, Henderik Willem , DE LEEDE, Leonardus Gerardus Jozef
发明人： BLOEMERS, Johannes Martinus Maria , EISSENS, Anko Cornelus , FRIJLINK, Henderik Willem , DE LEEDE, Leonardus Gerardus Jozef
IPC分类号： A61K9/00 , A61K9/28 , A61K9/20 , A61K31/519 , A61K31/568 , A61K31/00
CPC分类号： A61K9/2086 , A61K9/006 , A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/205 , A61K9/2054 , A61K9/209 , A61K9/2826 , A61K9/2866 , A61K31/506 , A61K31/519 , A61K31/568 , A61K45/06 , A61K2300/00
摘要： The invention relates to a time controlled, immediate release drug delivery system for oral administration of a first active ingredient to a subject in need thereof. The invention additionally relates to a dual drug delivery device, comprising the time controlled, immediate release drug delivery system according to the invention, further comprising a second coating comprising a second active ingredient.
摘要翻译：本发明涉及一种时间控制的即时释放药物递送系统，用于向有需要的受试者口服给予第一活性成分。本发明还涉及双药物递送装置，其包含根据本发明的时间控制的立即释放药物递送系统，还包括包含第二活性成分的第二涂层。

6. 发明申请

WO2007013794A1 PH-CONTROLLED PULSATILE DELIVERY SYSTEM, METHODS FOR PREPARATION AND USE THEREOF 审中-公开
标题翻译： PH控制的脉搏递送系统，其制备和使用方法
公开(公告)号：WO2007013794A1
公开(公告)日：2007-02-01
申请号：PCT/NL2005/000559
申请日：2005-07-29
申请人： Stichting Groningen Centre for Drug Research , SCHELLEKENS, Reinout Cornelus Andreas , FRIJLINK, Henderik Willem
发明人： SCHELLEKENS, Reinout Cornelus Andreas , FRIJLINK, Henderik Willem
IPC分类号： A61K9/00 , A61K9/50 , A61K9/28 , A61K39/00 , A61K9/20 , A61K47/30 , A61K31/00
CPC分类号： A61K9/4891 , A61K9/2846 , A61K9/286 , A61K9/2866 , A61K31/00
摘要： The invention relates to delivery systems that allow for the pulsatile release of a substance, such as a drug, in response to a change in pH. More specifically, it relates to drug administration to the GI tract, in particular to site-specific intestinal drug delivery via the oral route. Provided is a pH-controlled pulsatile release system (PPRS) comprising a core surrounded by a coating layer, wherein said core comprises an active substance and wherein said coating layer comprises a pH-sensitive coating material wherein a swellable agent is embedded. Said swellable agent is capable of taking up at least 1.1 times, preferably at least 5 times, more preferably at least 10 times its weight in water. Also provided is a pharmaceutical composition comprising a PPRS, in particular a colon-specific PPRS.
摘要翻译：本发明涉及允许物质（例如药物）响应于pH变化而脉动释放的递送系统。更具体地说，它涉及到胃肠道的药物给药，特别是通过口服途径给予特定于肠道的药物递送。提供了一种pH控制的脉冲释放系统（PPRS），其包括由涂层包围的芯，其中所述芯包含活性物质，并且其中所述涂层包含其中嵌入有溶胀剂的pH敏感性涂料。所述可溶胀剂能够在水中占据其重量的至少1.1倍，优选至少5倍，更优选至少10倍。还提供了包含PPRS，特别是结肠特异性PPRS的药物组合物。

7. 发明申请

WO1998013029A1 ORAL DELAYED IMMEDIATE RELEASE FORMULATION AND METHOD OF PREPARATION THEREFOR 审中-公开
标题翻译：口服延迟立即释放配方及其制备方法
公开(公告)号：WO1998013029A1
公开(公告)日：1998-04-02
申请号：PCT/EP1997005234
申请日：1997-09-18
申请人： DUPHAR INTERNATIONAL RESEARCH B.V. , VAN BALKEN, Paulus, Maria , ELBERS, Jules, Alex, Cornelis , FRIJLINK, Henderik, Willem , PHILIPS, Wienman, Emerald
发明人： DUPHAR INTERNATIONAL RESEARCH B.V.
IPC分类号： A61K09/28
CPC分类号： A61K39/145 , A61K9/282 , A61K9/2866 , A61K9/4808 , A61K39/00 , A61K39/12
摘要： The invention relates to an Oral Delayed Immediate Release formulation comprising a compressed core containing one or more active substances surrounded with a coating, wherein release of active substance from the core is caused by rupture of the coating after a definite lag-time, said core comprising one or more immediate release carriers and having no substantial swelling properties upon exposure to gastrointestinal fluids. The invention further relates to formulations containing an Immediate Release formulation combined with one or more Oral Delayed Immediate Release formulations with different lag-times and to a method of preparing an Oral Delayed Immediate Release formulation. The Oral Delayed Immediate Release formulation may be used for the application of active substances whenever a certain lag-time before release is advantageous, such as in the case of anti-asthmatics, anti-emetics, cardiotonics, vasodilators, anti-vertigo and anti-ménière compounds, anti-hypertensives, sedatives, anti-depressants, anti-anxiety compounds, cortico-steroids, general anti-inflammatory compounds, anti-inflammatory compounds for gastrointestinal use, anti-ulceratives, analgetics, anti-aritmics, anti-rheumatics, anti-arthritic compounds and anti-angina compounds. The Oral Delayed Immediate Release formulation may also be used for the application of biological active compounds such as proteins, peptides, enzymes, vaccines and oligonucleotides.
摘要翻译：本发明涉及一种口服延迟的立即释放制剂，其包含含有被涂层包围的一种或多种活性物质的压缩核心，其中活性物质从核心中释放是由确定滞后时间之后的涂层破裂引起的，所述核心包含一种或多种立即释放载体，并且在暴露于胃肠液体时没有显着的溶胀特性。本发明还涉及含有立即释放制剂与一种或多种具有不同滞后时间的口服延迟立即释放制剂组合的制剂以及制备口服延迟立即释放制剂的方法。口服延迟即时释放制剂可以用于活性物质的应用，每当释放前的某个滞后时间是有利的，例如在抗哮喘，抗排毒，强心剂，血管扩张剂，抗眩晕和抗眩晕药物的情况下，化合物，抗高血压药，镇静剂，抗抑郁药，抗焦虑药，皮质类固醇，一般抗炎化合物，消化道用抗炎化合物，抗溃疡药，止痛剂，抗神经药，抗风湿药，抗关节炎化合物和抗心绞痛化合物。口服延迟即时释放制剂也可用于生物活性化合物如蛋白质，肽，酶，疫苗和寡核苷酸的应用。

8. 发明申请

WO2012158030A3 DRUG DELIVERY SYSTEM 审中-公开
标题翻译：药物递送系统
公开(公告)号：WO2012158030A3
公开(公告)日：2013-04-18
申请号：PCT/NL2012050336
申请日：2012-05-14
申请人： EMOTIONAL BRAIN BV , BLOEMERS JOHANNES MARTINUS MARIA , EISSENS ANKO CORNELUS , FRIJLINK HENDERIK WILLEM , DE LEEDE LEONARDUS GERARDUS JOZEF
发明人： BLOEMERS JOHANNES MARTINUS MARIA , EISSENS ANKO CORNELUS , FRIJLINK HENDERIK WILLEM , DE LEEDE LEONARDUS GERARDUS JOZEF
IPC分类号： A61K9/28 , A61K9/20 , A61K31/519 , A61K31/568
CPC分类号： A61K9/2086 , A61K9/006 , A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/205 , A61K9/2054 , A61K9/209 , A61K9/2826 , A61K9/2866 , A61K31/506 , A61K31/519 , A61K31/568 , A61K45/06 , A61K2300/00
摘要： The invention relates to a time controlled, immediate release drug delivery system for oral administration of a first active ingredient to a subject in need thereof. The invention additionally relates to a dual drug delivery device, comprising the time controlled, immediate release drug delivery system according to the invention, further comprising a second coating comprising a second active ingredient.
摘要翻译：本发明涉及一种时间控制的即时释放药物递送系统，用于向有需要的受试者口服给予第一活性成分。本发明还涉及双药物递送装置，其包含根据本发明的时间控制的立即释放药物递送系统，还包括包含第二活性成分的第二涂层。

9. 发明申请

WO2013009186A1 NICOTINAMIDE COMPOSITIONS AND THE THERAPEUTIC USE THEREOF 审中-公开
标题翻译： NICOTINAMIDE组合物及其治疗用途
公开(公告)号：WO2013009186A1
公开(公告)日：2013-01-17
申请号：PCT/NL2012/050511
申请日：2012-07-16
申请人： APET Holding B.V. , Rijksuniversiteit Groningen , MEIJERINK, Hendrik Jan Cornelis , CHANGOER, Lekhram , BLOM, Willem , VISSER, Marinella Regina , FRIJLINK, Henderik Willem , EISSENS, Anko Cornelus
发明人： MEIJERINK, Hendrik Jan Cornelis , CHANGOER, Lekhram , BLOM, Willem , VISSER, Marinella Regina , FRIJLINK, Henderik Willem , EISSENS, Anko Cornelus
IPC分类号： A61K31/455 , A61K9/48 , A61K9/00 , A61P25/14 , A61P25/00
CPC分类号： A61K9/1652 , A61K9/0065 , A61K9/1635 , A61K9/1641 , A61K9/1676 , A61K9/2054 , A61K9/4808 , A61K9/4891 , A61K31/198 , A61K31/455 , G01N33/6893 , Y10T436/143333
摘要： The present invention relates to compositions and methods for the prophylaxis or treatment of deficiencies in essential amino acid absorption and metabolism and/or of a pathology or symptom associated there with. In particular the invention concerns the treatment and/or prevention of ADHD, ADD and autism spectrum disorders. The present inventors have developed a method for prophylaxis or treatment of such symptoms and/or pathologies associated with a deficiency in essential amino acid absorption and/or metabolism, which method, stated generally, relies on the administration of nicotinamide, typically in a long-acting formulation so as to overcome the deficiencies of existing formulations, which have proven unsuitable for effective treatment.
摘要翻译：本发明涉及用于预防或治疗必需氨基酸吸收和代谢缺陷和/或与其相关的病理学或症状的组合物和方法。特别地，本发明涉及ADHD，ADD和自闭症谱系障碍的治疗和/或预防。本发明人已经开发了用于预防或治疗与必需氨基酸吸收和/或代谢缺乏相关的这些症状和/或病症的方法，该方法通常依赖于烟酰胺的施用，通常在长时间以克服现有制剂的不足之处，已被证明不适合有效治疗。

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