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公开(公告)号：EP2293782B1
公开(公告)日：2015-08-12
申请号：EP09742569.8
申请日：2009-05-05
发明人： AZOULAY, Valerie , AVRAMOFF, Avi , PENHASI, Adel , GOMBERG, Maxim
IPC分类号： A61K9/28 , A61K31/4439
CPC分类号： A61K9/2095 , A61K9/1676 , A61K9/282 , A61K9/2866 , A61K9/5042 , A61K31/4439
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2.发明公开
公开(公告)号：EP1189601A2
公开(公告)日：2002-03-27
申请号：EP00939503.9
申请日：2000-06-02
CPC分类号： A61K9/286 , A61K9/209 , Y10S977/906
摘要： A two pulse gastrointestinal delivery system is provided. The system comprises a desired agent in combination with a swellable core material, the core being surrounded by an inner coat of a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. The inner coat is additionally surrounded by an outer coat that contains additional amounts of the desired agent. When the delivery device enters the gastrointestinal tract, the outer coat releases the desired agent contained therein and disintegrates, exposing the inner coat. The particulate matter in the inner coat takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the inner coat is broken. When the integrity of the inner coat is destroyed, the core then disintegrates, immediately releasing all or most of the drug at a specific site. By controlling parameters in the device, such as the core material, carrier material in the coating, and particulate matter, the location of release of both pulses of the drug can be carefully controlled. The invention is also directed to a method of using the device for the treatment of disease by the release of drugs in the gastrointestinal tract in a location- and time-dependent manner.
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3.发明公开
公开(公告)号：EP2026768A2
公开(公告)日：2009-02-25
申请号：EP07736412.3
申请日：2007-06-03
IPC分类号： A61K9/20 , A61K9/50 , A61K31/4439
CPC分类号： A61K9/2886 , A61K9/2077 , A61K9/5026 , A61K9/5042 , A61K31/4439
摘要： An orally disintegratable benzimidazole formulation, featuring a plurality of compressed pellets in a MUPS tablet. The individual units feature a substrate with the active ingredient and an enteric coating, optionally with a subcoating between the substrate and the enteric coating. The individual units are preferably at least partially coated with an outer coating which features a stress absorber, thereby enabling the pellets to be compressed without disturbing the integrity of the enteric coating. The enteric coating preferably does not feature a plasticizer.
摘要翻译： 口服崩解的苯并咪唑制剂，其特征在于MUPS片剂中的多个压缩颗粒。 单个单元的特征在于具有活性成分的底物和肠溶衣，任选地在底物和肠溶衣之间具有底衣层。 各个单元优选地至少部分地涂覆有具有应力吸收体的外涂层，从而使得丸粒能够被压缩而不会干扰肠溶衣的完整性。 肠溶衣优选不具有增塑剂。
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公开(公告)号：EP1817010A2
公开(公告)日：2007-08-15
申请号：EP05809260.2
申请日：2005-11-22
发明人： PENHASI, Adel
IPC分类号： A61K9/24
CPC分类号： A61K9/2886 , A61K9/2013 , A61K9/2846 , A61K9/2866 , A61K31/401
摘要： The present invention provides a controlled absorption formulation in which modified release of the active ingredient preferentially occurs in the lower gastrointestinal tract, including the colon. The formulation supports a significantly higher bioavailability of the active ingredient in the body of the subject than that can be achieved from the currently used conventional formulation, such that therapeutically significant plasma levels of statin are maintained for an extended period after administration. The formulation preferably features a core, over which an outer coating is layered. The core is optionally and preferably in the form of a tablet.
摘要翻译： 本发明提供了控制吸收制剂，其中活性成分的改变释放优先发生在包括结肠在内的下胃肠道中。 所述制剂支持活性成分在受试者体内的显着更高的生物利用度，这可以从目前使用的常规制剂中获得，从而在施用后在一段延长的时期内维持治疗上显着的他汀类血浆水平。 该制剂优选具有芯层，在其上层叠外层。 核心可选地并且优选地以片剂的形式。
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5.发明授权
公开(公告)号：EP1189601B1
公开(公告)日：2004-12-22
申请号：EP00939503.9
申请日：2000-06-02
CPC分类号： A61K9/286 , A61K9/209 , Y10S977/906
摘要： A two pulse gastrointestinal delivery system is provided. The system comprises a desired agent in combination with a swellable core material, the core being surrounded by an inner coat of a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. The inner coat is additionally surrounded by an outer coat that contains additional amounts of the desired agent. When the delivery device enters the gastrointestinal tract, the outer coat releases the desired agent contained therein and disintegrates, exposing the inner coat. The particulate matter in the inner coat takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the inner coat is broken. When the integrity of the inner coat is destroyed, the core then disintegrates, immediately releasing all or most of the drug at a specific site. By controlling parameters in the device, such as the core material, carrier material in the coating, and particulate matter, the location of release of both pulses of the drug can be carefully controlled. The invention is also directed to a method of using the device for the treatment of disease by the release of drugs in the gastrointestinal tract in a location- and time-dependent manner.
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公开(公告)号：EP1021171B1
公开(公告)日：2003-05-02
申请号：EP98949742.5
申请日：1998-10-01
IPC分类号： A61K9/28
CPC分类号： A61K9/205 , A61K9/286 , A61K9/2866 , A61K9/5084
摘要： A gastrointestinal delivery system is provided. The system comprises a drug in combination with a swellable core material, the core being surrounded by a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. When the delivery device enters the gastrointestinal tract, the particulate matter takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the coating is broken. When the integrity of the coating is destroyed, the core then disintegrates immediately releasing all or most of the drug at a specific site. By controlling parameters in the device, such as the core material, carrier material in the coating, and particulate matter, the location of release of the drug can be carefully controlled. Thus, the invention is also directed to a method of using the device for the treatment of disease by the release of drugs in the gastrointestinal tract in a location- and time-dependent manner.
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公开(公告)号：EP2026768B1
公开(公告)日：2018-02-28
申请号：EP07736412.3
申请日：2007-06-03
IPC分类号： A61K9/20 , A61K9/50 , A61K31/4439
CPC分类号： A61K9/2886 , A61K9/2077 , A61K9/5026 , A61K9/5042 , A61K31/4439
摘要： An orally disintegratable benzimidazole formulation, featuring a plurality of compressed pellets in a MUPS tablet. The individual units feature a substrate with the active ingredient and an enteric coating, optionally with a subcoating between the substrate and the enteric coating. The individual units are preferably at least partially coated with an outer coating which features a stress absorber, thereby enabling the pellets to be compressed without disturbing the integrity of the enteric coating. The enteric coating preferably does not feature a plasticizer.
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公开(公告)号：EP2448558A1
公开(公告)日：2012-05-09
申请号：EP10737638.6
申请日：2010-06-24
发明人： PENHASI, Adel , REUVENI, Albert , SHOSHANI, Eyal
IPC分类号： A61K9/00 , A61K9/16 , A61K9/70 , A61K31/192
CPC分类号： A61K9/0063 , A61K9/1635 , A61K9/1652 , A61K9/1658 , A61K9/7007 , A61K31/192
摘要： An oral delivery device for the treatment of periodontal disease, the device being in a solid unit dosage form configured for insertion into a periodontal pocket of a patient. The device consists of: (a) a biodegradable pharmaceutically acceptable water-insoluble polymer in the form of a matrix; (b) a therapeutically effective amount of at least one anti-inflammatory agent dispersed within the matrix; (c) optionally a plasticizing agent; (d) optionally at least one of a wetting agent, a suspending agent and a dispersing agent; and (e) optionally an enzymatically biodegradable pharmaceutically acceptable water soluble polymer dispersed within the matrix. The biodegradable water-insoluble polymer is degradable by enzymatic degradation, physical disintegration or a combination thereof. Also disclosed is a periodontal implant comprising the device and a method for the treatment of periodontal disease comprising administering to a periodontal pocket of a patient in need of such treatment the delivery device.
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公开(公告)号：EP1863449A2
公开(公告)日：2007-12-12
申请号：EP06728191.5
申请日：2006-03-27
发明人： PENHASI, Adel , RUDERMAN, Marina , GOMBERG, Maxim
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/24 , A61K9/26 , A61K9/28 , A61K9/30 , A61K9/32 , A61K9/36 , A61K9/48 , A61K9/52 , A61K9/54 , A61K9/56 , A61K9/62
CPC分类号： A61K31/00 , A61K9/2846 , A61K9/2866
摘要： A delayed onset controlled release formulation is provided in which controlled release of the active ingredient occurs preferentially in the lower gastrointestinal tract including the colon. The formulation supports a significantly higher bioavailability of the active ingredient in the body of the subject than can be achieved from the currently used conventional formulation, such that therapeutically significant plasma levels of statin are maintained for an extended period after administration. The formulation preferably features a core, over which an outer coating is layered. The core is optionally and preferably in the form of a tablet.
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10.发明授权
公开(公告)号：EP1608349B1
公开(公告)日：2007-10-17
申请号：EP04757724.2
申请日：2004-03-17
发明人： PENHASI, Adel , REUVENI, Albert , OREN, Dan
IPC分类号： A61K9/70 , A61K31/19 , A61K31/155 , A61P29/00
CPC分类号： A61K9/0024 , A61K9/0063 , A61K9/7007 , A61K31/155 , A61K31/19 , A61K45/06 , A61K2300/00
摘要： The present invention provides an oral delivery system for the treatment of periodontal disease, being in a solid unit dosage form for administration to a patient and comprising: (i) a biodegradable or bioerodible pharmaceutically acceptable polymer; (ii) a therapeutically effective amount of at least one antibacterial agent; and (iii) a therapeutically effective amount of at least one anti-inflammatory agent, the relative weight ratio between the antibacterial agent and the anti-inflammatory agent ranking from about 7:1 to about 1:5. The system may further comprise at least one of a cross-linking agent, a plasticizing agent, a wetting agent, a suspending agent, a surfactant and a dispersing agent.
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