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1. 发明授权

US07951401B2 Stabilised solid drug dispersions in an organic carrier and a process for preparing the same 有权
标题翻译：有机载体中稳定的固体药物分散体及其制备方法
公开(公告)号：US07951401B2
公开(公告)日：2011-05-31
申请号：US10540139
申请日：2003-12-22
申请人： Italo Colombo , Dario Gervasoni
发明人： Italo Colombo , Dario Gervasoni
IPC分类号： A61K47/30 , A61K9/14
CPC分类号： A61K9/1635 , A61K9/1652
摘要： New solid drug dispersions are described in which a drug is present in amorphous form and dispersed within the particles of an organic carrier selected from cross-linked polymers and/or complexing agents. These dispersions are obtainable by mixing the drug and the carrier and applying an oscillating electromagnetic field in the microwave region according to a specific heating cycle wherein the drug-carrier mixture is heated at a temperature higher than the melting point of the drug for at least 5 minutes.
摘要翻译：描述了新的固体药物分散体，其中药物以无定形形式存在并分散在选自交联聚合物和/或络合剂的有机载体的颗粒内。这些分散体可通过混合药物和载体而获得，并根据特定加热循环在微波区域施加振荡电磁场，其中药物 - 载体混合物在高于药物熔点的温度下加热至少5 分钟。

2. 发明申请

US20130274297A1 PHARMACEUTICAL COMPOSITES OF POORLY WATER SOLUBLE DRUGS AND POLYMERS 审中-公开
标题翻译：不良水溶性药物和聚合物的药物组合物
公开(公告)号：US20130274297A1
公开(公告)日：2013-10-17
申请号：US13995396
申请日：2011-12-22
申请人： Paolo Gatti , Italo Colombo , Dario Gervasoni , Vincenza Pironti , Lia Alborghetti , Flavio Fabiani , Luigi Boltri
发明人： Paolo Gatti , Italo Colombo , Dario Gervasoni , Vincenza Pironti , Lia Alborghetti , Flavio Fabiani , Luigi Boltri
IPC分类号： A61K31/4422 , A61K31/18 , A61K31/216
CPC分类号： A61K31/4422 , A61K9/146 , A61K31/18 , A61K31/216 , A61K31/44
摘要： The invention provides a composite of drug, polymeric carrier and at least one not cross linked polymer useful to improve the solubility of poorly water soluble drugs. The present invention comprises manufacturing process of this composite material. The manufacturing process is carried out by the solvent induced activation process, wherein the not cross-linked polymer is loaded into the composite from organic solution, possibly together with the drug. Pharmaceutical compositions comprising said composite in combination with pharmaceutical acceptable excipients are also described herein.
摘要翻译：本发明提供药物，聚合物载体和至少一种非交联聚合物的复合物，其可用于改善难溶于水的药物的溶解度。本发明包括该复合材料的制造工艺。制造过程通过溶剂诱导的活化方法进行，其中未交联的聚合物可能与药物一起从有机溶液中加载到复合物中。包含所述复合物与药学上可接受的赋形剂组合的药物组合物也在本文中描述。

3. 发明申请

US20060051422A1 Stabilised solid drug dispersions in an organic carrier and a process for preparing the same 有权
标题翻译：有机载体中稳定的固体药物分散体及其制备方法
公开(公告)号：US20060051422A1
公开(公告)日：2006-03-09
申请号：US10540139
申请日：2003-12-22
申请人： Italo Colombo , Dario Gervasoni
发明人： Italo Colombo , Dario Gervasoni
IPC分类号： A61K31/724 , A61K9/14
CPC分类号： A61K9/1635 , A61K9/1652
摘要： New solid drug dispersions are described in which the drug is present in amorphous form and massively dispersed (in bulk) inside the particles of an organic carrier selected from cross-linked polymers and/or a complexing agents. These dispersions are obtainable by mixing together the drug and the carrier and applying an oscillating electromagnetic field to the mixture, to a frequency belonging to the microwave region; the microwaves are applied according to a specific heating cycle wherein the drug-carrier mixture is heated at a temperature higher than the melting point of the drug for at least 5 minutes. With respect to the known techniques, the present invention allows to increase in the amount of drug incorporated into the carrier in amorphous form, and to increase the physical stability of the amorphous phase. This is particularly useful in the preparation of pharmaceutical compositions based on drugs which are crystalline in nature, such as are notoriously sparingly soluble in water: thanks to the increased amounts and stability of the drug in amorphous form, the resulting formulations have a more rapid and intense effect, and are endowed with greater bioavailability.
摘要翻译：描述了新的固体药物分散体，其中药物以非晶形式存在并且大量分散（大量）在选自交联聚合物和/或络合剂的有机载体的颗粒内。这些分散体可以通过将药物和载体混合在一起并将混合物的振荡电磁场混合到属于微波区域的频率来获得; 根据特定加热循环施加微波，其中药物 - 载体混合物在高于药物熔点的温度下加热至少5分钟。关于已知的技术，本发明允许以非晶形式增加掺入载体中的药物的量，并增加非晶相的物理稳定性。这在制备基于本质上是结晶性的药物的药物组合物中是特别有用的，例如臭名昭着地微溶于水：由于药物以无定形形式增加的量和稳定性，所得制剂具有更快速和强烈的作用，具有更大的生物利用度。

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