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1. 发明申请

WO2008113803A1 HOT-MELT MICROPELLETS 审中-公开
标题翻译：热熔麦克风
公开(公告)号：WO2008113803A1
公开(公告)日：2008-09-25
申请号：PCT/EP2008/053223
申请日：2008-03-18
申请人： LEK PHARMACEUTICALS D.D. , DREU, Rok , HOMAR, Miha , BURJAK, Mateja , KERC, Janez , SRCIC, Stanko
发明人： DREU, Rok , HOMAR, Miha , BURJAK, Mateja , KERC, Janez , SRCIC, Stanko
IPC分类号： A61K9/16 , A61K31/192
CPC分类号： A61K9/1641 , A61K9/1694 , A61K31/192
摘要： The present invention provides a method of making solid micropellets of which at least 75% by weight have a diameter less than 500 μm comprising (i) melting one or more binders; and (ii) combining the one or more binders melted in step (i) with a pharmaceutically active ingredient to form solid micropellets. Solid micropellets obtainable by this method are also provided. The invention has particular utility for improving the solubility of poorly water-soluble pharmaceutically active ingredients.
摘要翻译：本发明提供一种制备其至少75重量％的直径小于500μm的固体微丸的方法，包括（i）熔融一种或多种粘合剂; 和（ii）将步骤（i）中熔化的一种或多种粘合剂与药物活性成分组合以形成固体微丸。还提供了可通过该方法获得的固体微丸。本发明特别用于改善水溶性差的药物活性成分的溶解性。

2. 发明申请

WO2004047799A2 PELLETS CONTAINING NON-AQUEOUS FLUIDS AND THE PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：含有非水性流体的球体及其制备方法
公开(公告)号：WO2004047799A2
公开(公告)日：2004-06-10
申请号：PCT/SI2003/000042
申请日：2003-11-25
申请人： LEK PHARMACEUTICALS d.d. , SIRCA, Judita , SRCIC, Stanko , DREU, Rok
发明人： SIRCA, Judita , SRCIC, Stanko , DREU, Rok
IPC分类号： A61K9/00
CPC分类号： A61K9/0026 , A61K9/167 , A61K9/1682
摘要： Pellets characterized in that an agglomerating fluid used for their preparation is liquid polyhydroxy alcohol which may be in a mixture with water or another pharmaceutically acceptable solvent which is more easily volatile than said polyhydroxy alcohol and further characterized in that said agglomerating fluid completely or partly remains in a finished pharmaceutical dosage form.
摘要翻译：特征在于用于其制备的凝聚流体是液体多羟基醇，其可以与水或另一种比所述多羟基醇更易挥发的药学上可接受的溶剂混合，并且其特征还在于：所述凝聚流体完全或部分保留在成品药物剂型中。

3. 发明申请

WO2010065000A2 A PROCESS DEVICE FOR COATING PARTICLES 审中-公开
标题翻译：一种用于涂覆颗粒的工艺装置
公开(公告)号：WO2010065000A2
公开(公告)日：2010-06-10
申请号：PCT/SI2009/000065
申请日：2009-12-01
申请人： BRINOX, D.O.O. , SAVIC, Slavislav , GREGORKA, Matija , DREU, Rok , SRCIC, Stanko , SIBANC, Rok , LUSTRIK, Matevz , PERPAR, Matjaz , ZUN, Iztok
发明人： SAVIC, Slavislav , GREGORKA, Matija , DREU, Rok , SRCIC, Stanko , SIBANC, Rok , LUSTRIK, Matevz , ZUN, Iztok
CPC分类号： B01J2/006 , B01J2/16
摘要： The subject of the invention is a process device for coating particles that falls within the field of chemical and pharmaceutical technology. It represents an improvement on the process equipment for coating particles by spraying from the bottom and works on the principle of fluidization technology. The process device for coating particles, according to the invention which has within the wall (1), one or more units placed, for which each unit consists of a swirl flow generator (4) with a perforated plate (3) and a draft tube (5) where centrally through the swirl flow generator (4) a single or multi-phase spraying nozzle (6) with a coating dispersion inflow (7) and inflow (8) of compressed air is installed, in which the swirl flow generator (4) has outward open and at an angle with regard to the vertical installed grooves (18). The process device for coating particles in the second implementation case, has within the wall (1), one or more units placed, for which each unit consists of a draft tube (5) and a single or multi-phase spraying nozzle (6), which is mounted centrally with regard to the draft tube (5) and penetrates the perforated plate (3a). The perforated plate (3a), which is in the outer area, between the wall of the draft tube (5), and the wall (1) of the device, in cross-section straight or curved and has a characteristic distribution of the size of round orifices with the largest cross sections in the area of the ground floor projection of the draft tube (5) and smaller orifices in the remaining part of the plate. The device for coating shall have along the periphery of the wall (1) and at the perforated plate (3a) the ring (21 ) with installed inflow slots (27) that are pressure powered from a common hollow ring (20) with a connector (22) for compressed air. The device for coating shall have along the periphery of the wall (1) above the perforated plate (3a) a radially installed circumferential inflow slot (24) and otherwise inclined to the horizontal plane, the slot (24) is pressure powered through the hollow ring (23) with a pressure connection (25).
摘要翻译：本发明的主题是用于涂覆落入化学和制药技术领域的颗粒的工艺装置。它代表了从底部喷涂涂装颗粒的工艺设备的改进，并以流化技术为原则。根据本发明的用于涂覆颗粒的工艺装置，其在壁（1）内具有一个或多个放置的单元，每个单元由具有多孔板（3）的涡流发生器（4）和引流管（5）其中通过涡流发生器（4）集中地安装具有涂层分散体流入物（7）和压缩空气流入物（8）的单相或多相喷嘴（6），其中涡流发生器 4）相对于垂直安装的凹槽（18）具有向外开口并成一定角度。在第二实施例中用于涂覆颗粒的处理装置在壁（1）内具有一个或多个单元，每个单元由引流管（5）和单相或多相喷嘴（6）组成，，其相对于引流管（5）中心地安装并穿过多孔板（3a）。位于引流管（5）的壁和设备的壁（1）之间的位于外部区域中的多孔板（3a）的横截面呈直线或弯曲，并且具有尺寸的特征分布具有在引流管（5）的底层突起区域中具有最大截面的圆形孔和在板的剩余部分中的较小孔。用于涂覆的装置应沿着壁（1）的周边并且在多孔板（3a）处具有安装有流入槽（27）的环（21），所述流入槽（27）由具有连接器的公共空心环（20）（22）用于压缩空气。用于涂覆的装置应沿着多孔板（3a）上方的壁（1）的周边具有径向安装的圆周流入槽（24），否则倾斜于水平面，槽（24）通过中空环（23）与压力连接（25）。

4. 发明授权

EP2136792B1 HOT-MELT MICROPELLETS 无效
标题翻译： HEISSSCHMELZMIKROPELLETS
公开(公告)号：EP2136792B1
公开(公告)日：2012-12-26
申请号：EP08717955.2
申请日：2008-03-18
申请人： LEK Pharmaceuticals d.d. , Dreu, Rok
发明人： DREU, Rok , HOMAR, Miha , BURJAK, Mateja , KERC, Janez , SRCIC, Stanko
IPC分类号： A61K9/16 , A61K31/192
CPC分类号： A61K9/1641 , A61K9/1694 , A61K31/192

5. 发明公开

EP2136792A1 HOT-MELT MICROPELLETS 无效
标题翻译：热熔微颗粒
公开(公告)号：EP2136792A1
公开(公告)日：2009-12-30
申请号：EP08717955.2
申请日：2008-03-18
申请人： Lek Pharmaceuticals D.D. , Dreu, Rok
发明人： DREU, Rok , HOMAR, Miha , BURJAK, Mateja , KERC, Janez , SRCIC, Stanko
IPC分类号： A61K9/16 , A61K31/192
CPC分类号： A61K9/1641 , A61K9/1694 , A61K31/192
摘要： The present invention provides a method of making solid micropellets of which at least 75% by weight have a diameter less than 500 μm comprising (i) melting one or more binders; and (ii) combining the one or more binders melted in step (i) with a pharmaceutically active ingredient to form solid micropellets. Solid micropellets obtainable by this method are also provided. The invention has particular utility for improving the solubility of poorly water-soluble pharmaceutically active ingredients.

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