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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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2.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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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：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：US07011844B2
公开(公告)日：2006-03-14
申请号：US10302490
申请日：2002-11-22
申请人： Robert M. Gale , Melinda K. Nelson , Michel J. N. Cormier , Suneel K. Gupta , Patricia S. Campbell
发明人： Robert M. Gale , Melinda K. Nelson , Michel J. N. Cormier , Suneel K. Gupta , Patricia S. Campbell
IPC分类号： A61K9/70
CPC分类号： A61K9/7084 , A61K31/135 , A61K31/138 , A61K31/57 , A61K2300/00
摘要： Composition of matter for application to a body surface or membrane to administer fluoxetine by permeation through the body surface or membrane, the composition comprising fluoxetine to be administered, at a therapeutically effective rate, alone or in combination with a permeation enhancer or mixture. A preferred embodiment is directed to the transdermal administration of fluoxetine at reduced skin irritation levels wherein fluoxetine, preferably provided as fluoxetine acetate, is coadministered with a corticosteroid such as hydrocortisone. Also disclosed are drug delivery devices containing the fluoxetine or fluoxetine and enhancer composition and methods for the transdermal administration of the fluoxetine and fluoxetine/enhancer composition.
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公开(公告)号：US5840327A
公开(公告)日：1998-11-24
申请号：US704426
申请日：1996-08-15
CPC分类号： A61K9/703 , A61K9/7053 , A61K9/7084
摘要： A device for the transdermal administration of a drug to a sensitive body area such as the scrotum. Devices according to the invention provide an improved quality of adhesion to the body area while also providing patient comfort during use and upon removal of the device. Also disclosed are methods of transdermal delivery such as the transcrotal delivery of testosterone to hypogonadic males.
摘要翻译： 用于将药物透皮给药到诸如阴囊的敏感体区的装置。 根据本发明的装置提供了对身体区域的改善的粘附质量，同时还在使用期间和在移除装置时提供患者舒适度。 还公开了透皮递送的方法，例如将睾酮向性腺功能低下的男性的转录递送。
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公开(公告)号：US06512010B1
公开(公告)日：2003-01-28
申请号：US08892118
申请日：1997-07-14
申请人： Robert M. Gale , Melinda K. Nelson , Michel J. N. Cormier , Suneel K. Gupta , Patricia S. Campbell
发明人： Robert M. Gale , Melinda K. Nelson , Michel J. N. Cormier , Suneel K. Gupta , Patricia S. Campbell
IPC分类号： A61K3135
CPC分类号： A61K9/7084 , A61K31/135 , A61K31/138 , A61K31/57 , A61K2300/00
摘要： Composition of matter for application to a body surface or membrane to administer fluoxetine by permeation through the body surface or membrane, the composition comprising fluoxetine to be administered, at a therapeutically effective rate, alone or in combination with a permeation enhancer or mixture. A preferred embodiment is directed to the transdermal administration of fluoxetine at reduced skin irritation levels wherein fluoxetine, preferably provided as fluoxetine acetate, is coadministered with a corticosteroid such as hydrocortisone. Also disclosed are drug delivery devices containing the fluoxetine or fluoxetine and enhancer composition and methods for the transdermal administration of the fluoxetine and fluoxetine/enhancer composition.
摘要翻译： 用于通过穿过身体表面或膜透过体外表面或膜施用氟西汀的物质的组成，所述组合物包含单独或与渗透促进剂或混合物组合的待施用氟西汀。 优选的实施方案涉及在减少的皮肤刺激水平下透皮给药氟西汀，其中氟西汀，优选以醋酸氟西汀提供，与皮质类固醇如氢化可的松共同施用。 还公开了含有氟西汀或氟西汀和增强剂组合物的药物递送装置和用于透皮给药氟西汀和氟西汀/增强剂组合物的方法。
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