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公开(公告)号：US5750137A
公开(公告)日：1998-05-12
申请号：US637678
申请日：1996-03-15
IPC分类号： A61K9/00 , A61K9/70 , A61K31/215 , A61K31/216 , A61K31/57 , A61K47/14 , A61K47/32 , A61P13/02 , A61P15/00 , A61P17/00 , A61P21/00 , A61F13/02
CPC分类号： A61K9/7053 , A61K31/215 , A61K31/216 , A61K31/57 , A61K47/14 , A61K9/0014 , A61K9/7084 , Y10S514/946 , Y10S514/947
摘要： A composition of matter for application to a body surface or membrane to administer a drug by permeation through the body surface or membrane, the composition comprising, in combination the drug to be administered, in a therapeutically effective amount; and a permeation enhancing mixture comprising a monoglyceride or a mixture of monoglycerides, and a lactic ester or a mixture of lactate esters, present in specific concentrations.
摘要翻译： PCT No.PCT / US94 / 11120 Sec。 371日期：1996年3月15日 102（e）1996年3月15日PCT 1994年9月29日PCT PCT。 出版物WO95 / 09006 日期1995年4月6日用于通过穿过身体表面或膜渗透而施用于身体表面或膜的物质的组合物，所述组合物以治疗有效量组合包含待施用的药物; 以及包含单酸甘油酯或单酸甘油酯和乳酸酯或乳酸酯混合物的混合物的渗透增强混合物，其以特定浓度存在。
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2.发明授权
公开(公告)号：US5686097A
公开(公告)日：1997-11-11
申请号：US401593
申请日：1995-03-09
IPC分类号： A61K9/00 , A61K9/70 , A61K31/215 , A61K31/216 , A61K31/57 , A61K47/14 , A61K47/32 , A61P13/02 , A61P15/00 , A61P17/00 , A61P21/00 , A61F13/02
CPC分类号： A61K9/7053 , A61K31/215 , A61K31/216 , A61K31/57 , A61K47/14 , A61K9/0014 , A61K9/7084 , Y10S514/946 , Y10S514/947
摘要： A composition of matter for application to a body surface or membrane to coadminister an estrogen and progesterone by permeation through the body surface or membrane, the composition comprising, in combination, the estrogen and progesterone to be administered, in a therapeutically effective amount; and a permeation-enhancing mixture comprising a monoglyceride or a mixture of monoglycerides, and a lactate ester or a mixture of lactate esters at specific concentrations. The composition of matter is used to provide hormone replacement therapy to a woman.
摘要翻译： 一种用于施用于身体表面或膜的物质组合物，其通过渗透身体表面或膜来共同施用雌激素和孕酮，所述组合物以治疗有效量组合包含待施用的雌激素和孕酮; 以及包含单酸甘油酯或单酸甘油酯和乳酸酯或特定浓度的乳酸酯混合物的混合物的渗透增强混合物。 物质的组成用于为女性提供激素替代疗法。
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公开(公告)号：US5629019A
公开(公告)日：1997-05-13
申请号：US064689
申请日：1993-05-20
申请人： Eun Soo Lee , Su Il Yum , Michel J. N. Cormier
发明人： Eun Soo Lee , Su Il Yum , Michel J. N. Cormier
IPC分类号： A61K47/12 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/26 , A61K47/28 , A61K47/36 , A61K9/06
CPC分类号： A61K47/26 , A61K47/12 , A61K47/14 , A61K47/186 , A61K47/20 , A61K47/28 , A61K47/36 , A61K9/0014 , Y10S514/944 , Y10S514/946 , Y10S514/951
摘要： This invention is directed to a novel formulation for effectively utilizing hydrophobic permeation enhancers for the increased permeability of active agents through the skin or mucosa along with reduction of the lag time between application of the active agent and attainment of a therapeutically effective agent flux, with little or no irritation to the host. The invention is directed to compositions containing a hydrophobic permeation enhancer, which permeation enhancer has been micronized and stabilized in an inert carrier such as water. These compositions can be combined with a biologically active agent to provide enhanced permeability of the active agent to the skin or mucosa.
摘要翻译： 本发明涉及一种用于有效利用疏水性渗透增强剂以增加活性剂通过皮肤或粘膜的渗透性的新型制剂，同时减少施用活性剂之间的滞后时间并获得治疗有效的药剂通量 或对主机没有刺激。 本发明涉及含有疏水渗透增强剂的组合物，该渗透增强剂已经在惰性载体如水中微粉化并稳定。 这些组合物可与生物活性剂组合以提供活性剂对皮肤或粘膜的增强的渗透性。
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公开(公告)号：USRE39588E1
公开(公告)日：2007-04-24
申请号：US07606462
申请日：1990-10-31
申请人： Eun Soo Lee , Su Il Yum
发明人： Eun Soo Lee , Su Il Yum
IPC分类号： A61F3/00
CPC分类号： A61K9/7084
摘要： A diffusional drug delivery device is described which can provide for stability of the adhesive and system components, elimination of the initial burst of drug and hence irritation, and to provide for delayed onset of therapeutic effect along with delivery of a therapeutic agent at an optimum rate. The therapeutic agent in a first form which is suitable for storage, and the anhydrous activating means are inert when in an anhydrous environment. Moisture activates the system whereby the activating means provides an acidic or basic solution and the first form of the therapeutic agent is converted to a second form which is suitable for absorption through the skin or mucosa.
摘要翻译： 描述了扩散药物递送装置，其可以提供粘合剂和系统组分的稳定性，消除药物的初始爆发并因此刺激，并且提供治疗效果的延迟开始以及以最佳速率递送治疗剂 。 适于储存的第一种形式的治疗剂和无水活化装置在无水环境中是惰性的。 水分激活系统，由此激活装置提供酸性或碱性溶液，并且将第一形式的治疗剂转化为适合于通过皮肤或粘膜吸收的第二种形式。
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公开(公告)号：US5882676A
公开(公告)日：1999-03-16
申请号：US452468
申请日：1995-05-26
申请人： Eun Soo Lee , Su Il Yum
发明人： Eun Soo Lee , Su Il Yum
CPC分类号： A61K9/7084 , A61K47/14 , A61K9/0014 , Y10S514/947
摘要： The present invention is directed to the transdermal administration of a drug together with a suitable amount of an acyl lactylate permeation enhancer. The invention includes a transdermal drug delivery device comprising a matrix adapted to be placed in drug- and- permeation enhancer-transmitting relation with a skin site. The matrix contains sufficient amounts of an acyl lactylate permeation enhancer and drug, in combination, to continuously administer drug to the systemic circulation of a patient at a therapeutically effective rate. The invention is also directed to compositions and methods for transdermal administration of a drug together with an acyl lactylate permeation enhancer, alone or in combination with other enhancers.
摘要翻译： 本发明涉及药物与适量的酰基乳酸盐渗透促进剂的透皮给药。 本发明包括透皮药物递送装置，其包括适于与皮肤部位置于药物和渗透增强剂 - 传递关系中的基质。 基质含有足够量的酰基乳酸盐渗透促进剂和药物，以治疗有效的速率将药物连续地给予患者的全身循环。 本发明还涉及用于将药物与酰基乳酸盐渗透促进剂一起或与其它增强剂组合的透皮给药的组合物和方法。
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公开(公告)号：US5641504A
公开(公告)日：1997-06-24
申请号：US162026
申请日：1993-10-21
申请人： Eun Soo Lee , Diane E. Nedberge , Su Il Yum
发明人： Eun Soo Lee , Diane E. Nedberge , Su Il Yum
CPC分类号： A61K9/7053 , A61K47/10 , A61K47/14 , A61K9/0014 , A61K9/1274 , A61K9/7084 , Y10S514/946 , Y10S514/947
摘要： The present invention provides compositions and systems for the transdermal administration of a drug together with glycerol monolinoleate as a permeation enhancer. An example of a delivery system of the invention is a system (20) having a drug reservoir (22) containing together a drug to be delivered and glycerol monolinoleate permeation enhancer. Reservoir is sandwiched between a backing layer (24) and an in-line contact adhesive layer (28).
摘要翻译： PCT No.PCT / US92 / 04255 Sec。 371日期：1993年10月21日 102（e）日期1993年10月21日PCT提交1992年5月20日PCT公布。 出版物WO92 / 20377 日期：1992年11月26日本发明提供了用于透明给药药物与甘油单烯酸酯作为渗透促进剂的组合物和系统。 本发明的递送系统的实例是具有药物储存器（22）的系统（20），所述药物储存器（22）将待递送的药物和甘油单烯酸酯渗透增强剂包含在一起。 储存器夹在背衬层（24）和直列式接触粘合剂层（28）之间。
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公开(公告)号：US5284660A
公开(公告)日：1994-02-08
申请号：US933423
申请日：1992-08-21
申请人： Eun Soo Lee , Felix Theeuwes , Patrick S. L. Wong , Su Il Yum , Robert M. Gale , Alejandro Zaffaroni
发明人： Eun Soo Lee , Felix Theeuwes , Patrick S. L. Wong , Su Il Yum , Robert M. Gale , Alejandro Zaffaroni
CPC分类号： A61K9/7084 , A61K9/7069 , A61K9/7092
摘要： A diffusional drug delivery device is described which can provide for delayed onset of therapeutic effect and for delivery of the therapeutic agent in predetermined temporal patterns at optimum rates. Delay means are provided between the agent reservoir and the surface through which the agent is released by diffusion to delay the release of agent at a therapeutic rate for predetermined times after application. Suitable means include a delay membrane disposed between the releasing surface and the agent reservoir, which membrane is preferably free of undissolved agent and/or is initially impermeable to the agent and thereafter becomes permeable. One or more agent chambers defined by one or more of such membranes may be provided, whereby agents are released in predetermined temporal patterns at optimal release rates. Delayed permeability enables programmed washout periods to be obtained from the sequential and concurrent application of devices for the administration of drugs, such as nitrates, to which patients may develop a tolerance on continuous administration over extended time periods.
摘要翻译： 描述了扩散药物递送装置，其可以提供治疗效果的延迟开始和以最佳速率以预定时间模式递送治疗剂。 在药剂储存器和通过扩散释放药剂的表面之间提供延迟装置，以在施用后以治疗速率延迟药剂释放预定时间。 合适的方法包括设置在释放表面和药剂储存器之间的延迟膜，该膜优选不含未溶解的试剂和/或最初不能渗透到试剂中，然后变得可渗透。 可以提供由一种或多种这样的膜限定的一个或多个试剂室，由此以最佳释放速率以预定的时间模式释放试剂。 延迟渗透性使得能够从连续和同时使用用于施用诸如硝酸盐的药物的装置获得程序性洗脱期，患者可以在延长的时间段内持续施用耐受性。
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公开(公告)号：US5795591A
公开(公告)日：1998-08-18
申请号：US299867
申请日：1994-09-01
申请人： Eun Soo Lee , Scott A. Bura , Su Il Yum , Patrick S.-L. Wong , Felix Theeuwes
发明人： Eun Soo Lee , Scott A. Bura , Su Il Yum , Patrick S.-L. Wong , Felix Theeuwes
CPC分类号： A61K9/0004
摘要： Osmotically driven drug delivery devices with walls of porous hydrophobic material as the sole diffusion-limiting wall component are disclosed. Despite pores which are considerably larger than the molecular dimensions of osmotically active species in the interior of the device, despite pores which by their hydrophobic character do not permit the passage of liquid water, and despite the absence of a cellulosic semi-permeable membrane, the devices absorb water by osmosis without loss of the osmotically active species, and function in a manner analogous to osmotic pumps of the prior art. By permitting the use of hydrophobic substances as the wall material, the invention permits the device to be constructed entirely from biodegradable materials.
摘要翻译： 公开了具有作为唯一扩散限制壁部件的多孔疏水材料壁的渗透驱动药物输送装置。 尽管孔远远大于装置内部的渗透活性物质的分子尺寸，尽管孔具有疏水性，但不允许液态水通过，尽管不存在纤维素半透膜， 装置通过渗透吸收水分而不损失渗透活性物质，并且以类似于现有技术的渗透泵的方式起作用。 通过允许使用疏水物质作为壁材料，本发明允许该装置完全由可生物降解的材料构成。
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公开(公告)号：US5141750A
公开(公告)日：1992-08-25
申请号：US271122
申请日：1988-11-14
CPC分类号： A61K9/7084 , A61K9/7069 , A61K9/7092
摘要： A diffusional drug delivery device is described which can provide for delayed onset of therapeutic effect and for delivery of the therapeutic agent in predetermined temporal patterns at optimum rates. Delay means are provided between the agent reservoir and the surface through which the agent is released by diffusion to delay the release of agent at a therapeutic rate for predetermined times after application. Suitable means include a delay membrane disposed between the releasing surface and the agent reservoir which membrane is preferably free of undissolved agent and/or is initially impermeable to the agent and thereafter becomes permeable. One or more agent chambers defined by one or more of such membranes may be provided, whereby agents are released in a predetermined temporal pattern at optimal release rates. Delayed permeability emables programmed washout periods to be obtained from the sequential and concurrent application of devices for the administration of drugs, such as nitrates, to which patients may develop a tolerance on continous administration over extended time periods.
摘要翻译： 描述了扩散药物递送装置，其可以提供治疗效果的延迟开始和以最佳速率以预定时间模式递送治疗剂。 在药剂储存器和通过扩散释放药剂的表面之间提供延迟装置，以在施用后以治疗速率延迟药剂释放预定时间。 合适的方法包括设置在释放表面和试剂储存器之间的延迟膜，该膜优选不含未溶解的试剂和/或最初对试剂不渗透，然后变为可渗透的。 可以提供由一个或多个这样的膜限定的一个或多个试剂室，由此以最佳释放速率以预定的时间模式释放试剂。 延迟渗透性可以从序列和并发应用用于管理诸如硝酸盐的药物的装置获得程序性洗脱期，患者可以在延长的时间段内持续施用耐受性。
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公开(公告)号：US5071656A
公开(公告)日：1991-12-10
申请号：US271207
申请日：1988-11-14
CPC分类号： A61K9/7069 , A61K31/21 , A61K9/7084 , A61K9/7092
摘要： A diffusional drug delivery device is described which can provide for delayed onset of therapeutic effect and for delivery of the therapeutic agent in predetermined temporal patterns at optimum rates. Delay means are provided between the agent reservoir and the surface through which the agent is released by diffusion to delay the release of agent at a therapeutic rate for predetermined times after application. Suitable means include a delay membrane disposed between the releasing surface and the agent reservoir which membrane is preferably free of undissolved agent and/or is initially impermeable to the agent and thereafter becomes permeable. One or more agent chambers defined by one or more of such membranes may be provided, whereby agents are released in a predetermined temporal pattern at optimal release rates. Delayed permeability enables programmed washout periods to be obtained from the sequential and concurrent application of devices for the administration of drugs, such as nitrates, to which patients may develop a tolerance on continuous administration over extended time periods.
摘要翻译： 描述了扩散药物递送装置，其可以提供治疗效果的延迟开始和以最佳速率以预定时间模式递送治疗剂。 在药剂储存器和通过扩散释放药剂的表面之间提供延迟装置，以在施用后以治疗速率延迟药剂释放预定时间。 合适的方法包括设置在释放表面和试剂储存器之间的延迟膜，该膜优选不含未溶解的试剂和/或最初对试剂不渗透，然后变为可渗透的。 可以提供由一个或多个这样的膜限定的一个或多个试剂室，由此以最佳释放速率以预定的时间模式释放试剂。 延迟渗透性使得能够从连续和同时使用用于施用诸如硝酸盐的药物的装置获得程序性洗脱期，患者可以在延长的时间段内持续施用耐受性。
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