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1. 发明授权

US5783205A Injectable drug delivery system and method 失效
标题翻译：注射药物递送系统及方法
公开(公告)号：US5783205A
公开(公告)日：1998-07-21
申请号：US843682
申请日：1997-04-10
申请人： Randall G. Berggren , David J. Enscore , Susan M. Marks , James L. Osborne , Patrick S.-L. Wong , Wouter E. Roorda
发明人： Randall G. Berggren , David J. Enscore , Susan M. Marks , James L. Osborne , Patrick S.-L. Wong , Wouter E. Roorda
IPC分类号： A61C19/06 , A61K6/00 , A61K9/00 , A61K9/22 , A61K47/34 , A61F2/02
CPC分类号： A61C19/063 , A61K6/0067 , A61K9/0063 , A61K47/34
摘要： The present invention is directed to a material which can be used to deliver a drug, such as an antibiotic, into a diseased tissue pocket, such as a periodontal pocket. The material is preferably a bioerodible oligomer or polymer. The oligomer or polymer containing the drug is heated and is then delivered, preferably by injection, into the tissue pocket at a physiologically compatible elevated temperature. Once the bioerodible material is injected into the pocket, the material cools to the body temperature of the pocket. As it cools, the material hardens and remains in place in the tissue pocket. The hardened material bioerodes in the pocket and releases the drug over a period of several days.
摘要翻译：本发明涉及可用于将诸如抗生素的药物递送到患病组织袋（例如牙周袋）中的材料。该材料优选为生物可腐蚀的低聚物或聚合物。包含药物的低聚物或聚合物被加热，然后优选通过注射递送到生理上相容的升高的温度下的组织袋中。一旦将生物可蚀解材料注入到口袋中，则该材料冷却到口袋的体温。当它冷却时，材料硬化并保持在组织袋中的适当位置。硬化的材料在口袋中传播并在几天的时间内释放药物。

2. 发明授权

US5620700A Injectable drug delivery system and method 失效
标题翻译：注射药物递送系统及方法
公开(公告)号：US5620700A
公开(公告)日：1997-04-15
申请号：US437471
申请日：1995-05-09
申请人： Randall G. Berggren , David J. Enscore , Susan M. Marks , James L. Osborne , Patrick S.-L. Wong , Wouter E. Roorda
发明人： Randall G. Berggren , David J. Enscore , Susan M. Marks , James L. Osborne , Patrick S.-L. Wong , Wouter E. Roorda
IPC分类号： A61C19/06 , A61K6/00 , A61K47/34
CPC分类号： A61C19/063 , A61K47/34
摘要： The present invention is directed to a material which can be used to deliver a drug, such as an antibiotic, into a diseased tissue pocket, such as a periodontal pocket. The material is preferably a bioerodible oligomer or polymer. The oligomer or polymer containing the drug is heated and is then delivered, preferably by injection, into the tissue pocket at a physiologically compatible elevated temperature. Once the bioerodible material is injected into the pocket, the material cools to the body temperature of the pocket. As it cools, the material hardens and remains in place in the tissue pocket. The hardened material bioerodes in the pocket and releases the drug over a period of several days.
摘要翻译：本发明涉及可用于将诸如抗生素的药物递送到患病组织袋（例如牙周袋）中的材料。该材料优选为生物可腐蚀的低聚物或聚合物。包含药物的低聚物或聚合物被加热，然后优选通过注射递送到生理上相容的升高的温度下的组织袋中。一旦将生物可蚀解材料注入到口袋中，则该材料冷却到口袋的体温。当它冷却时，材料硬化并保持在组织袋中的适当位置。硬化的材料在口袋中传播并在几天的时间内释放药物。

3. 发明授权

US5344656A Subsaturated transdermal therapeutic system having improved release characteristics 失效
公开(公告)号：US5344656A
公开(公告)日：1994-09-06
申请号：US78540
申请日：1993-06-16
申请人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
发明人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
IPC分类号： A61K9/70 , A61K31/46 , A61F13/02
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.

4. 发明授权

US5342623A Subsaturated transdermal therapeutic system having improved release characteristics 失效
标题翻译：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
申请人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
发明人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
IPC分类号： A61K9/70 , A61K31/46 , A61F13/02
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。

5. 发明授权

US4908027A Subsaturated transdermal therapeutic system having improved release characteristics 失效
标题翻译：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
申请人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
发明人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
IPC分类号： A61K9/70 , A61K31/46
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。

6. 发明授权

US6165497A Subsaturated nicotine transdermal therapeutic system 失效
标题翻译：亚饱和尼古丁透皮治疗系统
公开(公告)号：US6165497A
公开(公告)日：2000-12-26
申请号：US662857
申请日：1991-03-01
申请人： James L. Osborne , Melinda Nelson , David J. Enscore , Su Il Yum , Robert M. Gale
发明人： James L. Osborne , Melinda Nelson , David J. Enscore , Su Il Yum , Robert M. Gale
IPC分类号： A61K9/70 , A61K31/465 , A61F13/02 , A61F13/00
CPC分类号： A61K9/7084 , A61K9/7053 , A61K9/7069 , A61K31/465 , 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 polymer 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 thicknesses of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and, preferably at least 75% 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，并且储存器包括溶解在聚合物中的尼古丁，装置的速率控制元件基本上与其相对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，速率控制膜和储存器层的厚度，使得至少50％，优选至少75％的初始平衡的尼古丁负载在储层中。

7. 发明授权

US5004610A Subsaturated nicotine transdermal therapeutic system 失效
标题翻译：亚饱和尼古丁透皮治疗系统
公开(公告)号：US5004610A
公开(公告)日：1991-04-02
申请号：US537672
申请日：1990-06-14
申请人： James L. Osborne , Melinda Nelson , David J. Enscore , Su I. Yum , Robert M. Gale
发明人： James L. Osborne , Melinda Nelson , David J. Enscore , Su I. Yum , Robert M. Gale
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。

8. 发明授权

US5462745A Subsaturated transdermal therapeutic system having improved release characteristics 失效
标题翻译：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
申请人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
发明人： David J. Enscore , Patricia S. Campbell , James L. Osborne , Melinda K. Smart , Su I. Yum
IPC分类号： A61K9/70 , A61K31/46 , A61F13/02
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。

9. 发明授权

US5633008A Method of administering nicotine transdermally 失效
标题翻译：透皮管理尼古丁的方法
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。

10. 发明授权

US5364630A Subsaturated nicotine transdermal therapeutic system 失效
标题翻译：亚饱和尼古丁透皮治疗系统
公开(公告)号：US5364630A
公开(公告)日：1994-11-15
申请号：US80280
申请日：1993-06-21
申请人： James L. Osborne , Melinda Nelson , David J. Enscore , Su I. Yum , Robert M. Gale
发明人： James L. Osborne , Melinda Nelson , David J. Enscore , Su I. Yum , Robert M. Gale
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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