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1.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：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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3.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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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：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：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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公开(公告)号：US6001390A
公开(公告)日：1999-12-14
申请号：US768600
申请日：1996-12-18
IPC分类号： A61M37/00 , A61K9/70 , A61K31/48 , A61K47/06 , A61K47/14 , A61K47/18 , A61P25/16 , A61F13/02
CPC分类号： A61K9/7053 , A61K31/48 , A61K9/0014 , A61K9/7084 , A61K47/14 , A61K47/18 , Y10S514/947
摘要： Composition of matter for application to a body surface or membrane to administer pergolide by permeation through the body surface or membrane, the composition comprising pergolide to be administered, at a therapeutically effective rate, alone or in combination with a permeation enhancer or mixture. Also disclosed are drug delivery devices containing the pergolide or pergolide and enhancer composition and methods for the transdermal administration of the pergolide and pergolide/enhancer composition.
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7.发明授权Method for preventing the formation of a crystalline hydrate in a dispersion of a liquid in a monaqueous matrix 失效用于防止在单水基质中的液体分散体中形成结晶水合物的方法
公开(公告)号：US4832953A
公开(公告)日：1989-05-23
申请号：US85052
申请日：1987-08-13
IPC分类号： A61K9/70
CPC分类号： A61K9/7053 , A61K9/7084
摘要： A method for preventing the formation of crystalline hydrates in a dispersion of a hydratable liquid in a nonaqueous matrix is disclosed. The method is particularly useful in the manufacture of laminated items formed from such dispersions and comprises forming individual subunits from such dispersions, heating the subunits, preferably after they have been packed in sealed containers, to a temperature high enough to melt the crystalline hydrate, maintaining said subunits at such temperature for a time sufficient to melt all the crystalline hydrate present and to prevent the occurrence of crystals for an extended period of time after cooling and cooling subunits to ambient conditions. The use of the method in the manufacture of transdermal delivery devices for the delivery of scopolamine base is described.
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公开(公告)号：US06174545B1
公开(公告)日：2001-01-16
申请号：US09243873
申请日：1999-02-03
IPC分类号： A61F1302
CPC分类号： A61K9/7084 , Y10S514/947
摘要： An improved process for manufacturing transdermal drug delivery devices and devices made therefrom. The invention provides a heat equilibration process for the manufacture of drug delivery devices which eliminates the need to preload the body contacting layer with a drug. The method has particular application in the manufacture of transdermal drug delivery devices including a drug reservoir comprising drug in excess of saturation.
摘要翻译： 用于制造透皮药物递送装置和由其制成的装置的改进方法。 本发明提供了用于制造药物递送装置的热平衡过程，其不需要用药物预加载身体接触层。 该方法在制造透皮药物递送装置中具有特别的应用，其包括含有超过饱和的药物的药物储库。
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公开(公告)号：US6007837A
公开(公告)日：1999-12-28
申请号：US243890
申请日：1999-02-03
IPC分类号： A61K9/70
CPC分类号： A61K9/7084
摘要： An improved process for manufacturing transdermal drug delivery devices and devices made therefrom. The invention provides a heat equilibration process for the manufacture of drug delivery devices which eliminates the need to preload the body contacting layer with a drug. The method has particular application in the manufacture of transdermal drug delivery devices including a drug reservoir comprising drug in excess of saturation.
摘要翻译： 用于制造透皮药物递送装置和由其制成的装置的改进方法。 本发明提供了用于制造药物递送装置的热平衡过程，其不需要用药物预加载身体接触层。 该方法在制造透皮药物递送装置中具有特别的应用，其包括含有超过饱和的药物的药物储库。
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公开(公告)号：US5990179A
公开(公告)日：1999-11-23
申请号：US431187
申请日：1995-04-28
CPC分类号： A61N1/0448 , A61K9/0009 , Y10S514/946 , Y10S514/947
摘要： A composition suitable for transdermal electrotransport delivery of an agent through a body surface comprises a free acid/base form of an agent to be delivered by transdermal electrotransport, and a salt form of the agent, and optionally a permeation enhancer. Methods of enhancing transdermal electrotransport delivery and of forming a composition for the enhancement of transdermal electrotransport drug delivery, and a transdermal electrotransport delivery device (10) utilizing the compositions of the invention are disclosed.
摘要翻译： 适用于通过身体表面的药物透皮电转移递送的组合物包含通过透皮电转运递送的药物的游离酸/碱形式，以及任选的渗透促进剂的盐形式。 公开了增强透皮电转移递送和形成用于增强透皮电转运药物递送的组合物的方法，以及利用本发明组合物的透皮电转运递装置（10）。
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