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    Subsaturated transdermal therapeutic system having improved release characteristics
    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

    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。

    Transdermal delivery device having a rate controlling adhesive
    5.
    发明授权
    Transdermal delivery device having a rate controlling adhesive 失效
    具有速率控制粘合剂的透皮递送装置

    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

    IPC分类号： A61F13/00 ,  A61K9/70 ,  A61L15/16 ,  A61L15/64 ,  A61M37/00

    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。

    Subsaturated transdermal therapeutic system having improved release characteristics
    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

    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。

    Matrix composition for transdermal therapeutic system
    7.
    发明授权
    Matrix composition for transdermal therapeutic system 失效
    透皮治疗系统的基质组成

    公开(公告)号：US4559222A

    公开(公告)日：1985-12-17

    申请号：US491490

    申请日：1983-05-04

    申请人： David J. Enscore ,  Robert M. Gale

    发明人： David J. Enscore ,  Robert M. Gale

    IPC分类号： A61K35/08 ,  A61K9/70 ,  A61F13/00 ,  A61K31/745 ,  A61L15/03

    CPC分类号： A61K9/7053 ,  A61K9/7084

    摘要： Mineral oil (MO) polyisobutylene (PIB), colloidal silicon dioxide (CSD) mixtures suitable for use as drug containing matrices in transdermal delivery systems are disclosed. Preferred systems for dispensing moderately mineral oil soluble drugs contain at least about 6% CSD, have a MO/PIB of at least 1.0 and a viscosity of at least 1.5.times.10.sup.7 poises. Preferred systems for dispensing clonidine have a clonidine permeability of at least 1.0.times.10.sup.-4 .mu.g/cm sec and a MO/PIB of at least 1.2.

    摘要翻译： 公开了适用于透皮递送系统中含药基质的矿物油（MO）聚异丁烯（PIB），胶体二氧化硅（CSD）混合物。 用于分配适度矿物油溶性药物的优选系统含有至少约6％的CSD，具有至少1.0的MO / PIB和至少1.5×10 7泊的粘度。 用于分配可乐定的优选体系具有至少1.0×10 -4μg/ cm 2秒的可乐定渗透性和至少1.2的MO / PIB。

    Subsaturated nicotine transdermal therapeutic system
    8.
    发明授权
    Subsaturated nicotine transdermal therapeutic system 失效
    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。

    Drug delivery devices and process of manufacture
    9.
    发明授权
    Drug delivery devices and process of manufacture 有权
    药物输送装置及制造过程

    公开(公告)号：US6007837A

    公开(公告)日：1999-12-28

    申请号：US243890

    申请日：1999-02-03

    申请人： David J. Enscore ,  Patricia S. Campbell ,  Diane Nedberge ,  Richard D. Frame

    发明人： David J. Enscore ,  Patricia S. Campbell ,  Diane Nedberge ,  Richard D. Frame

    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。

    Injectable drug delivery system and method
    10.
    发明授权
    Injectable drug delivery system and method 失效
    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。