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公开(公告)号：EP1003476A1
公开(公告)日：2000-05-31
申请号：EP98938469.8
申请日：1998-08-10
申请人： ALZA CORPORATION
发明人： DONG, Liang, C. , EDGREN, David, E. , GARDNER, Phyllis, I. , JAO, Francisco , THEEUWES, Felix , WAN, Jason , WONG, Patrick, S.-L.
CPC分类号： A61K9/0065 , A61K9/2072
摘要： The present invention is directed to an active agent dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of an active agent formulation to a fluid environment of use. The active agent dosage form is a polymer matrix that swells upon contact with the fluids of the stomach. A portion of the polymer matrix is surrounded by a band of insoluble material that prevents the covered portion of the polymer matrix from swelling and provides a segment of the dosage form that is of sufficient rigidity to withstand the contractions of the stomach and delay expulsion of the dosage form from the stomach until substantially all of the active agent has been dispensed.
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公开(公告)号：EP0716595A1
公开(公告)日：1996-06-19
申请号：EP94926618.0
申请日：1994-08-31
申请人： ALZA CORPORATION
发明人： DONG, Liang, C. , ESPINAL, Steven, D. , WONG, Patrick, S.-L. , GUITTARD, George, V. , HAMEL, Lawrence, G.
CPC分类号： A61K9/0004 , A61K9/2013 , A61K9/2054
摘要： The present invention is directed to a formulation for the delivery of hydrophobic active agents to a fluid environment of use while avoiding aggregation of the hydrophobic agents in the environment, the formulation comprising a hydrophobic active agent in an amount of 50 wt% (percent by weight) or greater together with polyoxyethylene 40 stearate and a disintegrant. The present invention is also directed to an improvement in a fluid-activated delivery device (10) wherein the delivery device includes a housing (12) defining an internal compartment (14), an active agent formulation (15) in the compartment, exit means (13) in the housing (12) for delivering the active agent formulation (15) from the delivery device, a fluid-activated expandable driving member (16) in the compartment, optionally a partition layer between the active agent formulation (15) and the driving member (16), and optionally a lubricant subcoat (18); wherein the improvement comprises an active agent formulation (15) comprising a hydrophobic active agent in an amount of 50 wt% (percent by weight) or greater together with polyoxyethylene 40 stearate and a disintegrant.
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3.发明公开PHARMACEUTICAL FORMULATION PROVIDING AN INCREASED BIOVAILABILITY OF HYDROPHOBIC DRUGS 审中-公开药物制剂，疏水药物物质的生物利用度增加
公开(公告)号：EP1556000A1
公开(公告)日：2005-07-27
申请号：EP03768556.7
申请日：2003-10-31
申请人： Alza Corporation
CPC分类号： A61K31/57 , A61K9/0004 , A61K9/1075 , A61K9/146
摘要： The present invention provides a drug formulation comprising a hydrophobic drug, an oil phase and a surfactant and a dosage form. The drug formulation works to increase the bioavailability of hydrophobic drugs delivered to the gastro-intestinal tract ('GI tract') of a desired subject. The drug formulation of the present invention is formulated as a self-emuslifying nanosuspension, which forms an emulsion in-situ upon introduction to an aqueous environment. The dosage form of the present invention may be formed using various different materials and may be configured to deliver the drug formulation of the present invention to the GI tract of a subject using any desired mechanism. A controlled release dosage form according to the present invention may be designed to deliver the drug formulation of the present invention at a desired rate over a desired period of time. If designed as a controlled release dosage form, the dosage form of the present invention may be an osmotic dosage form.
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4.发明公开
公开(公告)号：EP1458353A1
公开(公告)日：2004-09-22
申请号：EP02792477.8
申请日：2002-12-19
申请人： ALZA Corporation
IPC分类号： A61K9/00
CPC分类号： A61K9/0014 , A61K9/0004 , A61K9/1274 , A61K47/12 , A61K47/44
摘要： The present invention includes a formulation and controlled release dosage form that enable the controlled release of therapeutic agents showing reduced absorption in the lower gastrointestinal tract. The formulation of the present invention includes a therapeutic agent that exhibits greater absorption in the upper GI tract than in the lower GI tract and a permeation enhancer, which serves to increase absorption of the therapeutic agent in the lower GI tract. The formulation of the present invention further includes a carrier that allows the formulation to transition to a bioadhesive gel in situ after the formulation is dispensed within the GI tract and has had some opportunity to reach the surface of the GI mucosal membrane. The bioadhesive gel formed by the formulation of the present invention works to present effective concentrations of both the therapeutic agent and the permeation enhancer at the surface of the GI mucosal membrane over a period. The controlled release dosage form of the present invention is designed to deliver the formulation of the present invention at a desired release rate or release rate profile over a desired period of time.
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公开(公告)号：EP1117383A1
公开(公告)日：2001-07-25
申请号：EP99948122.9
申请日：1999-09-03
申请人： ALZA CORPORATION
CPC分类号： A61K9/0004
摘要： A dosage form is disclosed comprising a semipermeable walled container that houses a capsule, which capsule comprises a drug formulation, a piston, and an osmotic composition. The dosage form delivers the drug formulation through a passageway at a controlled rate over a substained-release period of time up to 24 hours.
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6.发明授权
公开(公告)号：EP0831774B1
公开(公告)日：2001-07-11
申请号：EP96920480.9
申请日：1996-05-24
申请人： ALZA CORPORATION
IPC分类号： A61K9/00
CPC分类号： A61K9/0004
摘要： An oral dosage form (10) for delivering a beneficial agent, such as an anti-inflammatory agent into the mouth of a human patient is disclosed. The dosage form (10) comprises a wall (12) surrounding an agent layer (15) that is poorly soluble in aqueous biological fluids, e.g., saliva, and an expandable driving member (16) of a fluid swellable, hydrophilic polymer. An exit passageway (13) in the wall (12) connects the agent (17) with the exterior of the dosage form (10). The wall (12) is configured and composed of materials which provide an accelerated flux across the wall without sacrificing structural integrity.
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公开(公告)号：EP1684726A1
公开(公告)日：2006-08-02
申请号：EP04810907.8
申请日：2004-11-12
申请人： ALZA CORPORATION
CPC分类号： A61K9/1611 , A61K9/2009 , A61K9/2027 , A61K9/2054
摘要： The present invention relates to compositions and methods for enhancing the bioavailability of beneficial agents with low water solubility.
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公开(公告)号：EP1003476B1
公开(公告)日：2004-12-22
申请号：EP98938469.8
申请日：1998-08-10
申请人： ALZA Corporation
发明人： DONG, Liang, C. , EDGREN, David, E. , GARDNER, Phyllis, I. , JAO, Francisco , THEEUWES, Felix , WAN, Jason , WONG, Patrick, S.-L.
CPC分类号： A61K9/0065 , A61K9/2072
摘要： The present invention is directed to an active agent dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of an active agent formulation to a fluid environment of use. The active agent dosage form is a polymer matrix that swells upon contact with the fluids of the stomach. A portion of the polymer matrix is surrounded by a band of insoluble material that prevents the covered portion of the polymer matrix from swelling and provides a segment of the dosage form that is of sufficient rigidity to withstand the contractions of the stomach and delay expulsion of the dosage form from the stomach until substantially all of the active agent has been dispensed.
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9.发明公开CONVERSION OF LIQUID FILLED GELATIN CAPSULES INTO CONTROLLED RELEASE SYSTEMS BY MULTIPLE COATINGS 有权液体填充明胶胶囊的系统有转换控制的现役由多个涂料
公开(公告)号：EP1140012A2
公开(公告)日：2001-10-10
申请号：EP99966463.4
申请日：1999-12-10
申请人： Alza Corporation
IPC分类号： A61K9/00
CPC分类号： A61K9/0004
摘要： A dosage form comprising a gelatin capsule formed with a composite wall and containing a liquid, active agent formulation where the wall comprises a barrier layer formed over the external surface of the gelatin capsule, and expandable layer formed over the barrier layer and a semipermeable layer formed over the expandable layer is described. The dosage forms and methods provide for the conversion of standard gelatin, liquid formulation capsules into controlled, release dosage forms that permit the controlled release of the active agent into the environment of use over time.
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公开(公告)号：EP1112060A1
公开(公告)日：2001-07-04
申请号：EP99944089.4
申请日：1999-09-03
申请人： ALZA Corporation
IPC分类号： A61K9/00
CPC分类号： A61K9/0004
摘要： A dosage form is disclosed comprising a drug formulation that self-emulsifies in said dosage form.
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