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公开(公告)号：US4938759A
公开(公告)日：1990-07-03
申请号：US903002
申请日：1986-09-02
申请人： David J. Enscore , Eun S. Lee , Su I. Yum
发明人： David J. Enscore , Eun S. Lee , Su I. Yum
CPC分类号： A61K9/7053 , A61K9/7084 , A61K9/7092
摘要： A transdermal delivery device having a release-rate controlling-adhesive is disclosed having improved delivery characteristics. The device employs a polyisobutylene/mineral oil adhesive formulation and an ethylene/viny acetate (EVA) drug reservoir formulation. The device is useful in delivering a wide variety of transdermally administrable drugs, particularly those which are moderately soluble in mineral oil. Preferred embodiments deliver timolol base and atropine base from an EVA (40% VA) reservoir formulation.
摘要翻译： 公开了具有释放速率控制粘合剂的透皮递送装置，具有改进的输送特性。 该装置采用聚异丁烯/矿物油粘合剂配方和乙烯/乙酸乙烯酯（EVA）药物储库配方。 该装置可用于递送多种透皮给药药物，特别是适用于矿物油的药物。 优选实施方案从EVA（40％VA）储存剂配方递送噻吗洛尔碱和阿托品碱。
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公开(公告)号：US5344656A
公开(公告)日：1994-09-06
申请号：US78540
申请日：1993-06-16
CPC分类号： A61K9/7084 , A61K31/46
摘要： Rate controlled transdermal delivery devices are disclosed which utilize an in-line adhesive to maintain the device on the skin and deliver an agent which is a solvent or a plasticizer for the in-line adhesive. The initial equilibrated concentration of the agent in the agent reservoir and the adhesive is below saturation, and the reservoir comprises the agent dissolved in a solvent with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of the agent in reservoir is sufficient to prevent the activity of the agent in the reservoir from decreasing by more than about 50% and preferably no more than about 25% during the predetermined period of administration; and the thicknesses of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and preferably at least 75% initial equilibrated agent loading is in the reservoir layer. The devices are usable to deliver agents which are liquid at body temperatures such as benztropine, secoverine, nicotine, arecoline, polyethylene glycol monolaurate, glycerol monolaurate, glycerol monooleate and ethanol, for example.
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公开(公告)号：US5004610A
公开(公告)日：1991-04-02
申请号：US537672
申请日：1990-06-14
IPC分类号： A61K9/70 , A61K31/465
CPC分类号： A61K9/7084 , A61K31/465 , A61K9/7053 , A61K9/7069 , Y10S514/813
摘要： Rate controlled transdermal nicotine delivery systems are disclosed which utilize an in-line adhesive to maintain the systems on the skin. The initial equilibrated concentration of nicotine in the nicotine reservoir and the adhesive is below saturation, preferably at a thermodynamic activity no greater than 0.50, and the reservoir comprises the nicotine dissolved in a material with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of nicotine in the reservoir is sufficient to prevent the activity of the nicotine in the reservoir from decreasing by more than about 75% and preferably no more than about 25% during the predetermined period of administration; and the thickness of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and, preferably at least 75% of the initial equilibrated nicotine loading is in the reservoir layer.
摘要翻译： 公开了速率控制的透皮尼古丁递送系统，其利用直列粘合剂将系统保持在皮肤上。 尼古丁储存器和粘合剂中尼古丁的初始平衡浓度低于饱和度，优选在不大于0.50的热力学活性下，并且储存器包含溶解在该装置的速率控制元件基本相当于的材料中的尼古丁 不渗透 在优选的实施方案中，储存器中尼古丁的初始加载量足以防止储存器中的尼古丁的活性在给定的给药期间减少超过约75％，优选不超过约25％; 并且选择粘合剂，速率控制膜和储存层的厚度，使得初始平衡的尼古丁负载的至少50％，优选至少75％在储层中。
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4.发明授权Subsaturated transdermal therapeutic system having improved release characteristics 失效具有改善的释放特性的亚饱和透皮治疗系统
公开(公告)号：US5342623A
公开(公告)日：1994-08-30
申请号：US80645
申请日：1993-06-18
CPC分类号： A61K9/7084 , A61K31/46
摘要： Rate controlled transdermal delivery devices are disclosed which utilize an in-line adhesive to maintain the device on the skin and deliver an agent which is a solvent or a plasticizer for the in-line adhesive. The initial equilibrated concentration of the agent in the agent reservoir and the adhesive is below saturation, and the reservoir comprises the agent dissolved in a solvent with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of the agent in reservoir is sufficient to prevent the activity of the agent in the reservoir from decreasing by more than about 50% and preferably no more than about 25% during the predetermined period of administration; and the thicknesses of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and preferably at least 75% initial equilibrated agent loading is in the reservoir layer. The devices are usable to deliver agents which are liquid at body temperatures such as benztropine, secoverine, nicotine, arecoline, polyethylene glycol monolaurate, glycerol monolaurate, glycerol monooleate and ethanol, for example.
摘要翻译： 公开了速率控制的透皮递送装置，其使用直列粘合剂将装置保持在皮肤上并输送作为在线粘合剂的溶剂或增塑剂的试剂。 试剂储存器和粘合剂中试剂的初始平衡浓度低于饱和，并且储存器包含溶解在溶剂中的试剂，其中装置的速率控制元件基本上不可渗透。 在优选的实施方案中，试剂在储存器中的初始加载量足以防止储存器中的试剂的活性在给定的给药期间减少超过约50％，优选不超过约25％ 并且选择粘合剂，速率控制膜和储层的厚度，使得至少50％，优选至少75％的初始平衡剂负载在储层中。 这些装置可用于例如递送在体温下为液体的药剂，例如苯托品，脱毛，尼古丁，槟榔碱，聚乙二醇单月桂酸酯，甘油单月桂酸酯，甘油单油酸酯和乙醇。
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5.发明授权Subsaturated transdermal therapeutic system having improved release characteristics 失效具有改善的释放特性的亚饱和透皮治疗系统
公开(公告)号：US4908027A
公开(公告)日：1990-03-13
申请号：US906730
申请日：1986-09-12
CPC分类号： A61K9/7084 , A61K31/46
摘要： Rate-controlled transdermal delivery devices are disclosed which utilize an in-line adhesive to maintain the device on the skin and deliver an agent which is a solvent for the in-line adhesive. The initial equilibrated concentration of the agent in the agent reservoir and the adhesive is below saturation and the reservoir comprises the agent dissolved in a solvent with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of the agent in reservoir is sufficient to prevent the activity of the agent in the reservoir from decreasing by more than about 50% and preferrably no more than about 25% during the predetermined period of administration; and the thicknesses of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and, preferrably at least 75% initial equilibrated agent loading is in the reservoir layer. The devices are usable to delivery oily non-polar agents which are liquid at body temperatures such as benztropine and secoverine.
摘要翻译： 公开了速率控制的透皮递送装置，其使用直列粘合剂将装置保持在皮肤上并输送作为在线粘合剂的溶剂的试剂。 试剂储存器和粘合剂中的试剂的初始平衡浓度低于饱和，并且储存器包含溶解在溶剂中的试剂，相对于其中装置的速率控制元件基本上不可渗透。 在优选的实施方案中，试剂在储存器中的初始加载足以防止储存器中的试剂的活性在给定的给药期间减少超过约50％，优选不超过约25％; 并且选择粘合剂，速率控制膜和储存器层的厚度，使得至少50％，优选地至少75％的初始平衡剂加载在储层中。 该装置可用于输送在体温下为液体的油性非极性试剂，例如苯托品和脱毛。
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公开(公告)号：US5633008A
公开(公告)日：1997-05-27
申请号：US105262
申请日：1993-08-12
申请人： James L. Osborne , Melinda K. Nelson , David J. Enscore , Su I. Yum , Robert M. Gale , Donna D. Causey
发明人： James L. Osborne , Melinda K. Nelson , David J. Enscore , Su I. Yum , Robert M. Gale , Donna D. Causey
IPC分类号： A61K9/70 , A61K31/465 , A61F13/00
CPC分类号： A61K9/7084 , A61K31/465 , A61K9/7053 , A61K9/7069 , Y10S514/813
摘要： A method of administering nicotine transdermally in which a nicotine patch, capable of administering nicotine for at least 16 hours at rates that are efficacious in smoking cessation therapy, is applied in the morning upon waking and removed prior to sleep. This method is effective even though nicotine is not essential during sleep and many smokers experience morning craving.
摘要翻译： 一种经皮给药尼古丁的方法，其中可以在睡眠前醒来并在睡眠前去除能够以有效戒烟治疗的速率给尼古丁至少16小时的尼古丁贴片。 即使尼古丁在睡眠中不是必需的，许多吸烟者也经历早晨的渴望，这种方法是有效的。
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公开(公告)号：US5364630A
公开(公告)日：1994-11-15
申请号：US80280
申请日：1993-06-21
IPC分类号： A61K9/70 , A61K31/465 , A61F13/00
CPC分类号： A61K31/465 , A61K9/7084
摘要： Rate controlled transdermal nicotine delivery systems are disclosed which utilize an in-line adhesive to maintain the systems on the skin. The initial equilibrated concentration of nicotine in the nicotine reservoir and the adhesive is below saturation, preferably at a thermodynamic activity no greater than 0.50, and the reservoir comprises the nicotine dissolved in a material with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of nicotine in the reservoir is sufficient to prevent the activity of the nicotine in the reservoir from decreasing by more than about 75% and preferably no more than about 25% during the predetermined period of administration; and the thickness of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and, preferably at least 75% of the initial equilibrated nicotine loading is in the reservoir layer.
摘要翻译： 公开了速率控制的透皮尼古丁递送系统，其利用直列粘合剂将系统保持在皮肤上。 尼古丁储存器和粘合剂中尼古丁的初始平衡浓度低于饱和度，优选在不大于0.50的热力学活性下，并且储存器包含溶解在该装置的速率控制元件基本相当于的材料中的尼古丁 不渗透 在优选的实施方案中，储存器中尼古丁的初始加载量足以防止储存器中的尼古丁的活性在给定的给药期间减少超过约75％，优选不超过约25％; 并且选择粘合剂，速率控制膜和储存层的厚度，使得初始平衡的尼古丁负载的至少50％，优选至少75％在储层中。
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8.发明授权Subsaturated transdermal therapeutic system having improved release characteristics 失效具有改善的释放特性的亚饱和透皮治疗系统
公开(公告)号：US5462745A
公开(公告)日：1995-10-31
申请号：US297739
申请日：1994-08-30
CPC分类号： A61K9/7084 , A61K31/46
摘要： Rate controlled transdermal delivery devices are disclosed which utilize an in-line adhesive to maintain the device on the skin and deliver an agent which is a solvent or a plasticizer for the in-line adhesive. The initial equilibrated concentration of the agent in the agent reservoir and the adhesive is below saturation, and the reservoir comprises the agent dissolved in a solvent with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of the agent in reservoir is sufficient to prevent the activity of the agent in the reservoir from decreasing by more than about 50% and preferably no more than about 25% during the predetermined period of administration: and the thicknesses of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and preferably at least 75% initial equilibrated agent loading is in the reservoir layer. The devices are usable to deliver agents which are liquid at body temperatures such as benztropine, secoverine, nicotine, arecoline, polyethylene glycol monolaurate, glycerol monolaurate, glycerol monooleate and ethanol, for example.
摘要翻译： 公开了速率控制的透皮递送装置，其使用直列粘合剂将装置保持在皮肤上并输送作为在线粘合剂的溶剂或增塑剂的试剂。 试剂储存器和粘合剂中试剂的初始平衡浓度低于饱和，并且储存器包含溶解在溶剂中的试剂，其中装置的速率控制元件基本上不可渗透。 在优选实施方案中，试剂在储存器中的初始加载量足以防止储存器中的试剂在给定施用期间的活性降低超过约50％，优选不超过约25％ 选择粘合剂，速率控制膜和储存层，使得至少50％，优选至少75％的初始平衡剂负载在储层中。 这些装置可用于例如递送在体温下为液体的药剂，例如苯托品，脱毛，尼古丁，槟榔碱，聚乙二醇单月桂酸酯，甘油单月桂酸酯，甘油单油酸酯和乙醇。
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公开(公告)号：US5417676A
公开(公告)日：1995-05-23
申请号：US818210
申请日：1992-01-08
申请人： Tyler Watanabe , Su I. Yum , Eun S. Lee , Ivan W. Chin
发明人： Tyler Watanabe , Su I. Yum , Eun S. Lee , Ivan W. Chin
CPC分类号： A61F5/441 , A61M1/0096
摘要： An apparatus is disclosed comprising in combination (1) a container for receiving a fluid, and having an exit port, and (2) a delivery system designed for passage through the exit port into the container for releasing a biocide inside the container.
摘要翻译： 公开了一种装置，其包括组合（1）用于接收流体并具有出口的容器，以及（2）设计用于通过出口进入容器以将容器内的杀生物剂释放的输送系统。
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公开(公告)号：US5411740A
公开(公告)日：1995-05-02
申请号：US193661
申请日：1994-02-08
申请人： Eun S. Lee , Diane E. Nedberge , Su I. Yum
发明人： Eun S. Lee , Diane E. Nedberge , Su I. Yum
IPC分类号： A61K9/00 , A61K9/70 , A61K31/135 , A61K31/215 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/34 , A61P13/02 , A61P15/00 , A61P25/00 , A61F13/02
CPC分类号： A61K9/7053 , A61K31/215 , A61K31/216 , A61K47/14 , A61K9/0014 , A61K9/7084 , Y10S514/946
摘要： The present invention is directed to the transdermal administration of oxybutynin together with a suitable permeation enhancer. The invention includes a transdermal drug delivery device comprising a matrix adapted to be placed in oxybutynin- and permeation enhancer-transmitting relation with the skin site. The matrix contains sufficient amounts of a permeation enhancer and of oxybutynin, in combination, to continuously administer to the skin for a predetermined period of time the oxybutynin to provide an effective therapeutic result. The invention is also directed to a method for the transdermal administration of a therapeutically effective amount of oxybutynin together with a skin permeation-enhancing amount of a suitable permeation enhancer.
摘要翻译： 本发明涉及奥昔布宁与合适的渗透增强剂的透皮给药。 本发明包括透皮药物递送装置，其包含适于与皮肤部位置于奥昔布宁和渗透增强剂 - 传递关系中的基质。 基质含有足量的渗透促进剂和奥昔布宁组合，以持续给予皮肤预定的时间，奥昔布宁提供有效的治疗结果。 本发明还涉及用于透皮给药治疗有效量的奥昔布宁以及皮肤渗透增强剂量的合适的渗透增强剂的方法。
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