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1. 发明申请

US20060062809A1 Solid dispersions comprising two different polymer matrixes 失效
标题翻译：包含两种不同聚合物基质的固体分散体
公开(公告)号：US20060062809A1
公开(公告)日：2006-03-23
申请号：US10518987
申请日：2003-07-01
申请人： Karel Six , Geert Verreck , Jozef Peeters , Marcus Brewster , Guy Van Den Mooter
发明人： Karel Six , Geert Verreck , Jozef Peeters , Marcus Brewster , Guy Van Den Mooter
IPC分类号： A61K9/20 , A61K9/00
CPC分类号： A61K9/1635 , A61K9/146
摘要： Present invention provides solid dispersions comprising a poorly soluble bioactive compound dispersed in a polymer matrix characterized in that the polymer matrix comprises more than one polymer. Said solid dispersions effectively stabilize the dispersed compound while stimulating the solubilisation of the compound in an aquaeous environment.
摘要翻译：本发明提供包含分散在聚合物基质中的难溶性生物活性化合物的固体分散体，其特征在于聚合物基质包含多于一种聚合物。所述固体分散体有效地稳定分散的化合物，同时刺激化合物在水环境中的溶解。

2. 发明授权

US07407670B2 Solid dispersions comprising two different polymer matrixes 失效
标题翻译：包含两种不同聚合物基质的固体分散体
公开(公告)号：US07407670B2
公开(公告)日：2008-08-05
申请号：US10518987
申请日：2003-07-01
申请人： Karel Six , Geert Verreck , Jozef Peeters , Marcus Eli Brewster , Guy Van Den Mooter
发明人： Karel Six , Geert Verreck , Jozef Peeters , Marcus Eli Brewster , Guy Van Den Mooter
IPC分类号： A61K9/14
CPC分类号： A61K9/1635 , A61K9/146
摘要： Present invention provides solid dispersions comprising a poorly soluble bioactive compound dispersed in a polymer matrix characterized in that the polymer matrix comprises more than one polymer. Said solid dispersions effectively stabilize the dispersed compound while stimulating the solubilisation of the compound in an aquaeous environment.
摘要翻译：本发明提供包含分散在聚合物基质中的难溶性生物活性化合物的固体分散体，其特征在于聚合物基质包含多于一种聚合物。所述固体分散体有效地稳定分散的化合物，同时刺激化合物在水环境中的溶解。

3. 发明授权

US08273371B2 Crystalline mesoporous oxide based materials useful for the fixation and controlled release of drugs 有权
标题翻译：用于药物固定和控释的结晶介孔氧化物基材料
公开(公告)号：US08273371B2
公开(公告)日：2012-09-25
申请号：US12498015
申请日：2009-07-06
申请人： Johan Adriaan Martens , Christine Eva Antonia Kirschhock , Sebastien Philippe Brigitte Kremer , Alexander Jan Maria Herman Eugeen Aerts , Guy Van Den Mooter , Jan Van Humbeeck
发明人： Johan Adriaan Martens , Christine Eva Antonia Kirschhock , Sebastien Philippe Brigitte Kremer , Alexander Jan Maria Herman Eugeen Aerts , Guy Van Den Mooter , Jan Van Humbeeck
IPC分类号： A61K9/48
CPC分类号： A61K9/143 , A61K9/5115 , A61K47/02 , C01B37/005 , C01B37/02
摘要： The invention describes a new class of crystalline silica material having two levels of porosity and structural order. At the first level, building units are nanoslabs of uniform size having zeolite framework. At the second structural level, nanoslabs are assembled, e.g. linked through their corners, edges or faces following patterns imposed by interaction with cationic surfactant or triblock copolymer molecules. After evacuation of these molecules, microporosity is obtained inside the nanoslabs, and a precise mesoporosity between the nanoslabs depending on the tiling pattern of the zeolite nanoslabs, as evidenced by X-ray diffraction. These materials are useful for the fixation of biologically active species, such as poorly soluble drugs.
摘要翻译：本发明描述了一类具有两层孔隙度和结构顺序的结晶二氧化硅材料。在一级，建筑单位是具有沸石骨架的尺寸均匀的纳米尺度。在第二结构层面，组装nanoslabs。通过它们的角落，边缘或面部连接，这些图案通过与阳离子表面活性剂或三嵌段共聚物分子的相互作用在这些分子抽真空之后，在纳米尺度内获得微孔，并且通过X射线衍射证明，纳米尺度之间的精确介孔取决于沸石纳米尺度的平铺图案。这些材料可用于固定生物活性物质，如难溶性药物。

4. 发明申请

US20110059175A9 ENHANCING SOLUBILITY AND DISSOLUTION RATE OF POORLY SOLUBLE DRUGS 审中-公开
标题翻译：提高不溶性药物的溶解度和溶解速率
公开(公告)号：US20110059175A9
公开(公告)日：2011-03-10
申请号：US12296848
申请日：2007-04-10
申请人： Sandrien Janssens , Guy Van Den Mooter
发明人： Sandrien Janssens , Guy Van Den Mooter
IPC分类号： A61K9/00 , A61K47/30 , A61K31/55 , A61K31/58 , A61K31/175 , A61K31/34 , A61K31/496 , A61K31/426 , A61K31/44 , A61K31/42 , A61K31/505 , A61P31/10
CPC分类号： A61K9/146 , A61K31/496
摘要： The present invention relates generally to use of a polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer), such as Kollicoat IR, in the formulation of solid dispersions of low aqueous solubility and dissolution rate bioactive compound and, more particularly to a system and method for improving the solubility and dissolution rate of such low aqueous solubility and dissolution rate bioactive compound, in particular the drug of low aqueous solubility, such as a BCS Class II or Class IV drug compounds.
摘要翻译：本发明一般涉及聚乙烯醇 - 聚乙二醇接枝共聚物（PVA-PEG接枝共聚物），例如Kollicoat IR，在低水溶性和溶解速率的生物活性化合物的固体分散体的制剂中，更特别地，涉及用于改善这种低水溶性和溶解速率的生物活性化合物，特别是低水溶性药物如BCS II类或IV类药物化合物的溶解度和溶解速率的系统和方法。

5. 发明申请

US20130243833A1 COMPRESSED FORMULATIONS OF ORDERED MESOPOROUS SILICAS 审中-公开
标题翻译：订购的MESOPOROUS SILICAS的压缩配方
公开(公告)号：US20130243833A1
公开(公告)日：2013-09-19
申请号：US13988687
申请日：2011-11-28
申请人： Monica Vialpando , Johan Martens , Guy Van Den Mooter , Filip Kiekens
发明人： Monica Vialpando , Johan Martens , Guy Van Den Mooter , Filip Kiekens
IPC分类号： A61K47/02 , A61K31/4985 , A61K31/353 , A61K31/496 , A61K31/397
CPC分类号： A61K47/02 , A61K9/143 , A61K9/2009 , A61K9/2054 , A61K9/2077 , A61K31/353 , A61K31/397 , A61K31/496 , A61K31/4985
摘要： A compressed formulation comprising an ordered mesoporous silica loaded with an active ingredient, a combination of microcrystalline cellulose (MCC) and croscarmellose sodium, and optional further excipients.
摘要翻译：包含负载有活性成分的有序介孔二氧化硅，微晶纤维素（MCC）和交联羧甲基纤维素钠的组合以及任选的其它赋形剂的压缩制剂。

6. 发明申请

US20110081416A1 ORDERED MESOPOROUS SILICA MATERIAL 审中-公开
标题翻译：订购的MESOPOROUS SILICA MATERIAL
公开(公告)号：US20110081416A1
公开(公告)日：2011-04-07
申请号：US12905759
申请日：2010-10-15
申请人： Jasper JAMMAER , Alexander Aerts , Guy Van Den Mooter , Johan Martens
发明人： Jasper JAMMAER , Alexander Aerts , Guy Van Den Mooter , Johan Martens
IPC分类号： A61K9/00 , C01B33/12 , B32B3/26
CPC分类号： A61K9/143 , A61K47/02 , C01B37/02 , Y10T428/249979
摘要： A process for preparing a 2D-hexagonal ordered mesoporous silica material with a substantially uniform pore size in the range of 4 to 30 nm comprising the steps of: preparing an aqueous solution comprising an alkali silicate solution; preparing an aqueous solution comprising a poly(alkylene oxide) triblock copolymer and a buffer with a pH greater than 2 and less than 8, adding said aqueous alkali silicate solution to said aqueous solution giving a pH greater than 2 and less than 8 and allowing a reaction between the components to take place at a temperature in the range of 10 to 100° C., and filtering off, drying and calcinating the reaction product to produce said 2D-hexagonal ordered mesoporous silica material with a substantially uniform pore size. In an alternative procedure both aqueous solutions are fed as liquid streams into an elongated mixing receptacle having a first and a second opening such that the liquid streams of the solutions are each discharged independently into said first opening of said elongated mixing receptacle such that they directly impinge thereby giving a pH in the resulting mixture of greater than 2 and less than 8 and producing a reaction product at a temperature in the range of 10 to 100° C. in said elongated mixing receptacle, which upon emergence from said second opening of said elongated mixing receptacle is filtered off, dried and the surfactant removed.
摘要翻译：一种制备具有4至30nm范围内基本均匀孔径的二维六方有序介孔二氧化硅材料的方法，包括以下步骤：制备包含碱金属硅酸盐溶液的水溶液; 制备包含聚（环氧烷）三嵌段共聚物和pH大于2且小于8的缓冲液的水溶液，将所述碱性硅酸钠水溶液加入到所述水溶液中，得到大于2且小于8的pH，并允许组分之间的反应在10至100℃的温度下进行，并过滤掉，干燥和煅烧反应产物以产生具有基本均匀的孔径的所述二维六方有序介孔二氧化硅材料。在另一种方法中，两种水溶液以液体流的形式进入具有第一和第二开口的细长混合容器中，使得溶液的液体流各自独立地排放到所述细长混合容器的所述第一开口中，使得它们直接冲击从而在所得混合物中产生大于2且小于8的pH，并在所述细长混合容器中在10至100℃范围内的温度下产生反应产物，在从所述细长的第二开口出来时，将混合容器滤出，干燥并除去表面活性剂。

7. 发明授权

US07749521B2 Crystalline mesoporous oxide based materials useful for the fixation and controlled release of drugs 有权
标题翻译：用于药物固定和控释的结晶介孔氧化物基材料
公开(公告)号：US07749521B2
公开(公告)日：2010-07-06
申请号：US10562307
申请日：2004-06-28
申请人： Johan Adriaan Martens , Christine Eva Antonia Kirschhock , Sebastien Philippe Brigitte Kremer , Alexander Jan Maria Herman Eugeen Aerts , Guy Van Den Mooter , Jan Van Humbeeck
发明人： Johan Adriaan Martens , Christine Eva Antonia Kirschhock , Sebastien Philippe Brigitte Kremer , Alexander Jan Maria Herman Eugeen Aerts , Guy Van Den Mooter , Jan Van Humbeeck
IPC分类号： A61K9/00
CPC分类号： A61K9/5115 , A61K9/143 , C01B37/005 , C01B37/02 , Y10S977/70 , Y10S977/712 , Y10S977/831
摘要： The invention describes a new class of crystalline silica material having two levels or porosity and structural order. At the first level, building units are nanoslabs of uniform size having zeolite framework. At the second structural level, nanoslabs are assembled, e.g. linked through their corners, edges or faces following patterns imposed by interaction with cationic surfactant or triblock copolymer molecules. After evacuation of these molecules, microporosity is obtained inside the nanoslabs, and a precise mesoporosity between the nanoslabs depending on the tiling pattern of the zeolite nanoslabs, as evidenced by X-ray diffraction. These materials are useful for the fixation of biologically active species, such as poorly soluble drugs.
摘要翻译：本发明描述了一类具有两个等级或孔隙率和结构顺序的新型结晶二氧化硅材料。在一级，建筑单位是具有沸石骨架的尺寸均匀的纳米尺度。在第二结构层面，组装nanoslabs。通过它们的角落，边缘或面部连接，这些图案通过与阳离子表面活性剂或三嵌段共聚物分子的相互作用在这些分子抽真空之后，在纳米尺度内获得微孔，并且通过X射线衍射证明，纳米尺度之间的精确介孔取决于沸石纳米尺度的平铺图案。这些材料可用于固定生物活性物质，如难溶性药物。

8. 发明授权

US08790697B2 Controlled release delivery system for bio-active agents 有权
标题翻译：用于生物活性剂的控制释放递送系统
公开(公告)号：US08790697B2
公开(公告)日：2014-07-29
申请号：US11575014
申请日：2005-09-09
申请人： Johan Martens , Guy Van Den Mooter , Jan Van Humbeeck , Caroline Aerts , Randy Mellaerts
发明人： Johan Martens , Guy Van Den Mooter , Jan Van Humbeeck , Caroline Aerts , Randy Mellaerts
IPC分类号： A61K9/00
CPC分类号： A61K9/1611 , C01B33/18
摘要： The invention provides a controlled release delivery system comprising a bio-active compound and a matrix carrier, wherein said matrix carrier is an amorphous microporous non-fibrous silicon or titanium oxide being loaded with said bio-active compound and wherein the micropores of said matrix carrier have a mean size in the range of 0.4 to 2.0 nm.
摘要翻译：本发明提供了包含生物活性化合物和基质载体的控制释放递送系统，其中所述基质载体是负载有所述生物活性化合物的无定形微孔非纤维状硅或氧化钛，并且其中所述基质载体的微孔平均尺寸在0.4至2.0nm的范围内。

9. 发明申请

US20110086099A9 CRYSTALLINE MESOPOROUS OXIDE BASED MATERIALS USEFUL FOR THE FIXATION AND CONTROLLED RELEASE OF DRUGS 有权
标题翻译：用于固定和控制释放药物的基于MOCOPOROUS OXIDE的材料
公开(公告)号：US20110086099A9
公开(公告)日：2011-04-14
申请号：US12498015
申请日：2009-07-06
申请人： Johan Adriaan Martens , Christine Eva Antonia Kirschhock , Sebastien Philippe Brigitte Kremer , Alexander Jan Maria Herman Eugeen Aerts , Guy Van Den Mooter , Jan Van Humbeeck
发明人： Johan Adriaan Martens , Christine Eva Antonia Kirschhock , Sebastien Philippe Brigitte Kremer , Alexander Jan Maria Herman Eugeen Aerts , Guy Van Den Mooter , Jan Van Humbeeck
IPC分类号： A61K31/496 , C01B39/02 , C01B39/04 , A61K31/5513 , A61K9/10 , A61P25/22
CPC分类号： A61K9/143 , A61K9/5115 , A61K47/02 , C01B37/005 , C01B37/02
摘要： The invention describes a new class of crystalline silica material having two levels of porosity and structural order. At the first level, building units are nanoslabs of uniform size having zeolite framework. At the second structural level, nanoslabs are assembled, e.g. linked through their corners, edges or faces following patterns imposed by interaction with cationic surfactant or triblock copolymer molecules. After evacuation of these molecules, microporosity is obtained inside the nanoslabs, and a precise mesoporosity between the nanoslabs depending on the tiling pattern of the zeolite nanoslabs, as evidenced by X-ray diffraction. These materials are useful for the fixation of biologically active species, such as poorly soluble drugs.
摘要翻译：本发明描述了一类具有两层孔隙度和结构顺序的结晶二氧化硅材料。在一级，建筑单位是具有沸石骨架的尺寸均匀的纳米尺度。在第二结构层面，组装nanoslabs。通过它们的角落，边缘或面部连接，这些图案通过与阳离子表面活性剂或三嵌段共聚物分子的相互作用而强加。在这些分子抽真空之后，在纳米尺度内获得微孔，并且通过X射线衍射证明，纳米尺度之间的精确介孔取决于沸石纳米尺度的平铺图案。这些材料可用于固定生物活性物质，如难溶性药物。

10. 发明授权

US07666307B2 Particle size reduction of bioactive compounds 失效
标题翻译：生物活性化合物的粒径减小
公开(公告)号：US07666307B2
公开(公告)日：2010-02-23
申请号：US10595119
申请日：2004-08-25
申请人： Guy Van Den Mooter , Johan Martens , Jan Nuyens
发明人： Guy Van Den Mooter , Johan Martens , Jan Nuyens
IPC分类号： B02C19/00
CPC分类号： A61K9/143 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/19
摘要： The invention provides a method for reducing the average size of biologically active compound particles or agglomerates suspended in a fluid by flowing one or more times said fluid having biologically active compound particles or agglomerates suspended therein through one or more magnetic fields to reduce the average size of a substantial portion of the biologically active compound particles or agglomerates by at least 25%. This method may be incorporated into a process for manufacturing a 10 biologically active compound formulation.
摘要翻译：本发明提供了一种通过一次或多次流过具有悬浮在其中的生物活性化合物颗粒或聚集体的所述流体通过一个或多个磁场来减少悬浮在流体中的生物活性化合物颗粒或附聚物的平均尺寸的方法，以减少平均尺寸大部分生物活性化合物颗粒或附聚物至少25％。该方法可以并入用于制备10种生物活性化合物制剂的方法中。

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