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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：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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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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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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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：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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6.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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7.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：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：US4588580A
公开(公告)日：1986-05-13
申请号：US633762
申请日：1984-07-23
申请人： Robert M. Gale , Victor Goetz , Eun S. Lee , Lina T. Taskovich , Su I. Yum
发明人： Robert M. Gale , Victor Goetz , Eun S. Lee , Lina T. Taskovich , Su I. Yum
IPC分类号： C07D211/58 , A61K9/70 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/455 , A61K31/465 , C07D211/66 , C07D409/06 , A01N25/24
CPC分类号： A61K9/7053 , A61K31/445 , A61K9/7069 , A61K9/7084 , A61K9/7092
摘要： Transdermal delivery systems for delivery of fentanyl and its analgetically effective derivatives for extended periods of time are disclosed which deliver the base form of the drug at a rate of from 0.5 to 10 .mu.g/cm.sup.2 /hr for a substantial portion of their useful life. The systems can be from 5-100 cm.sup.2 in releasing surface and preferably employ an in-line amine resistant adhesive. Preferred rate controlled systems utilize an aqueous ethanolic gel to minimize drug content.
摘要翻译： 公开了用于递送芬太尼及其止痛有效衍生物延长时间的透皮递送系统，其在其使用寿命的大部分时间内以0.5至10μg/ cm 2 / hr的速率递送药物的基础形式。 系统的释放表面可以为5-100cm 2，优选采用直列耐胺粘合剂。 优选的速率控制系统利用含水乙醇凝胶来最小化药物含量。
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公开(公告)号：US4816258A
公开(公告)日：1989-03-28
申请号：US19163
申请日：1987-02-26
IPC分类号： A61K9/70 , A61K31/565
CPC分类号： A61K9/7053 , A61K31/565 , A61K31/567 , A61K9/7076 , A61K9/7084 , Y10S424/14 , Y10S514/841 , Y10S514/874
摘要： A transdermal delivery system for the administering of ethinyl estradiol and levonorgestrel, in combination, utilizing a polymer matrix having the drug formulation along with a permeation enhancer dispersed throughout.
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