公开(公告)号：US5578315A

公开(公告)日：1996-11-26

申请号：US160474

申请日：1993-12-01

申请人： Yie W. Chien ,  Mona Nair

发明人： Yie W. Chien ,  Mona Nair

IPC分类号： A61K9/20 ,  A61K9/00 ,  A61K9/70

CPC分类号： A61K9/006

摘要： Mucosal adhesive devices are provided for use in the oral cavity for therapy against infections. The devices are dosage units which comprise a combination of antimicrobial agents such as antifungal agents and anti-inflammatory agents, optionally also a local anesthetic. The dosage units yield a gradual and relatively constant release of the pharmaceuticals over at least a 12-hour period.

摘要翻译： 提供粘膜粘合装置用于口腔中用于治疗感染。 这些装置是包含抗微生物剂如抗真菌剂和抗炎剂的组合的剂量单位，任选地还包括局部麻醉剂。 剂量单位在至少12小时内产生药物的逐渐且相对恒定的释放。

公开(公告)号：US4818540A

公开(公告)日：1989-04-04

申请号：US902440

申请日：1986-08-29

申请人： Yie W. Chien ,  Te-Yen Chien ,  Yih-Chain Huang

发明人： Yie W. Chien ,  Te-Yen Chien ,  Yih-Chain Huang

IPC分类号： A61K9/70 ,  A61K31/565 ,  A61K31/57 ,  A61F13/00

CPC分类号： A61K9/7069 ,  A61K9/7084

摘要： Transdermal fertility-controlling absorption polymer matrix dosage units have been developed which comprise a backing layer, an adjoining layer of a solid polymer matrix in which minimum effective daily doses of an estrogen and a progestin are microdispersed and released for transdermal absorption. Presently preferred is use of the natural estrogen, 17-beta-estradiol, and of the progestin, levonorgestrel. The units have a biologically acceptable adhesive polymer layer. The polymer matrix as well as the adhesive layer can have dispersed one or more skin permeation enhancers. Dosage units are provided which transdermally deliver at least minimum daily doses of the estrogen and progestin for multiple days, such as for one week. The invention also provides a process of fertility control using the novel polymer matrix dosage units for the first three weeks of consecutive menstrual cycles of the subject desiring fertility control.

摘要翻译： 已经开发了经皮生育控制吸收聚合物基质剂量单位，其包含背衬层，固体聚合物基质的相邻层，其中雌激素和孕激素的最小有效日剂量被微分散并释放用于经皮吸收。 目前优选使用天然雌激素17-β-雌二醇和孕激素左炔诺孕酮。 这些单元具有生物可接受的粘合剂聚合物层。 聚合物基质以及粘合剂层可以分散一种或多种皮肤渗透促进剂。 提供剂量单位，其经皮递送至少最小日剂量的雌激素和孕激素多天，例如一周。 本发明还提供了一种使用新型聚合物基质剂量单位进行育性控制的方法，该方法用于需要生育控制的受试者的连续月经周期的前三周。

公开(公告)号：US3992518A

公开(公告)日：1976-11-16

申请号：US617542

申请日：1975-09-29

申请人： Yie W. Chien ,  Howard J. Lambert

发明人： Yie W. Chien ,  Howard J. Lambert

IPC分类号： A61K9/00 ,  A61K9/20 ,  A61K9/26

CPC分类号： A61K9/0092 ,  A61K9/0024 ,  A61K9/0039 ,  A61K9/2036

摘要： The present invention is concerned with a pharmaceutical delivery device comprising a biologically acceptable silicone polymer matrix having microsealed compartments of 10-200 microns throughout, wherein the microsealed compartments contain a pharmaceutical in a hydrophilic solvent system. The biologically acceptable silicone polymer matrix is formed by in situ cross linking of a liquid, biologically acceptable silicone polymer in an emulsion of pharmaceutical in the hydrophilic solvent system and liquid biologically acceptable silicone polymer. The biologically acceptable silicone polymer matrix is placed in a sealed or unsealed biologically acceptable polymer container. The rate of release of pharmaceutical is controlled by altering the solubility characteristics of the hydrophilic solvent system and/or the biologically acceptable polymer matrix, the rate of release being independent of time when the ratio of the partition coefficient of the pharmaceutical between the hydrophilic solvent system and biologically acceptable silicone polymer matrix to the solubility of the pharmaceutical in the hydrophilic solvent system is between 1 and 10.sup.-.sup.4 ml/mcg.

摘要翻译： 本发明涉及药物递送装置，其包含具有10-200微米的微密封隔室的生物可接受的硅氧烷聚合物基质，其中所述微密封隔室在亲水性溶剂体系中含有药物。 生物可接受的硅氧烷聚合物基质是通过在亲水溶剂系统中的药物乳液中的液体，生物可接受的硅氧烷聚合物原位交联形成的，并且与液体生物可接受的硅氧烷聚合物形成交联。 将生物可接受的硅氧烷聚合物基质置于密封或未密封的生物可接受的聚合物容器中。 通过改变亲水溶剂体系和/或生物可接受的聚合物基质的溶解度特性来控制药物的释放速率，当亲水性溶剂系统之间的药物的分配系数的比率 并且生物可接受的硅氧烷聚合物基质对药物在亲水溶剂体系中的溶解度为1至10 -4ml / mcg。

公开(公告)号：US5961482A

公开(公告)日：1999-10-05

申请号：US617688

申请日：1996-03-19

申请人： Yie W. Chien ,  John Kong-Jiann Li ,  Jue-Chen Liu ,  Wei-Min Shi ,  Ovais Siddiqui ,  Ying Sun

发明人： Yie W. Chien ,  John Kong-Jiann Li ,  Jue-Chen Liu ,  Wei-Min Shi ,  Ovais Siddiqui ,  Ying Sun

IPC分类号： A61K9/00 ,  A61N1/30 ,  A61N1/32

CPC分类号： A61N1/044 ,  A61K9/0009 ,  A61N1/303 ,  A61N1/325 ,  A61N1/0432

摘要： This invention relates to development of an iontotherapeutic device for regulated transdermal systemic administration of ionizable pharmaceutical compounds. It also provides an iontotherapeutic process for transdermal administration of ionized pharmaceuticals, particularly those which are otherwise transdermally absorbed to a small degree or not all, such as peptide pharmaceuticals, for example, insulins. The invention also relates to unit dose forms, for example, those in which an ionized pharmaceutical is dispersed in a hydrophilic polymer. The unit dose is adapted to be assembled as part of the pharmaceutical reservoir electrode, so that the ionized pharmaceutical will be delivered transdermally and then be absorbed systemically when the iontotherapeutic device is in operation.

摘要翻译： 本发明涉及用于可调节药物化合物的经调理的经皮系统给药的离子治疗装置的开发。 它还提供离子治疗方法，用于经皮给药离子化药物，特别是那些在很小程度上经皮吸收的药物，例如肽药物，例如胰岛素。 本发明还涉及单位剂量形式，例如其中离子化药物分散在亲水性聚合物中的那些形式。 单位剂量适于作为药物储存器电极的一部分组装，使得离子化药物将经皮递送，然后当离子治疗装置运行时被全身吸收。

公开(公告)号：US5788983A

公开(公告)日：1998-08-04

申请号：US943169

申请日：1992-09-14

申请人： Yie W. Chien ,  Guo-Shen Chen ,  Te-Yen Chien

发明人： Yie W. Chien ,  Guo-Shen Chen ,  Te-Yen Chien

IPC分类号： A61K9/70 ,  A61F13/02

CPC分类号： A61K9/7084 ,  A61K9/7092

摘要： Transdermal polymer dosage units are provided which comprise a backing layer and a reservoir layer. The reservoir layer can have multiple regions which contact the skin during use, optionally may have different pharmaceuticals, may provide variable rate of transdermal absorption, and may provide the pharmaceuticals in the form of microreservoirs or one or more macroreservoirs. The reservoir region can comprise a macroreservoir of one or more pharmaceuticals wherein the reservoir is bounded by a backing layer and a layer of a substantially non-porous permeability-regulating polymer membrane which directly or indirectly contacts the skin during transdermal administration. Also, provided is a process of transdermal administration of pharmaceuticals using the novel dosage units.

摘要翻译： 提供透皮聚合物剂量单位，其包含背衬层和储存层。 储存层可以具有在使用期间接触皮肤的多个区域，任选地可以具有不同的药物，可以提供可变的经皮吸收速率，并且可以以微储存器或一个或多个宏储存器的形式提供药物。 储存器区域可以包括一种或多种药物的大容量储存器，其中储存器由透皮给药期间直接或间接接触皮肤的背衬层和基本上无孔的渗透性调节聚合物膜层限制。 此外，提供了使用新型剂量单位透皮给药药物的方法。

公开(公告)号：US5042975A

公开(公告)日：1991-08-27

申请号：US046984

申请日：1987-05-07

申请人： Yie W. Chien ,  John Kong-Jiann Li ,  Jue-Chen Liu ,  Wei-Min Shi ,  Ovais Siddiqui ,  Ying Sun

发明人： Yie W. Chien ,  John Kong-Jiann Li ,  Jue-Chen Liu ,  Wei-Min Shi ,  Ovais Siddiqui ,  Ying Sun

IPC分类号： A61N1/30

CPC分类号： A61N1/0448 ,  A61N1/303 ,  A61N1/044

摘要： This invention relates to development of an iontotherapeutic device for regulated transdermal systemic administration of ionizable pharmaceutical compounds.It also provides an iontotherapeutic process for transdermal administration of ionized pharmaceuticals, particularly those which are otherwise transdermally absorbed to a small degree or not all, such as peptide pharmaceuticals, for example, insulins. The invention also relates to unit dose forms, for example, those in which an ionized pharmaceutical is dispersed in a hydrophilic polymer. The unit dose is adapted to be assembled as part of the pharmaceutical reservoir electrode, so that the ionized pharmaceutical will be delivered transdermally and then be absorbed systemically when the iontotherapeutic device is in operation.

摘要翻译： 本发明涉及用于可调节药物化合物的经调理的经皮系统给药的离子治疗装置的开发。 它还提供离子治疗方法，用于经皮给药离子化药物，特别是那些在很小程度上经皮吸收的药物，例如肽药物，例如胰岛素。 本发明还涉及单位剂量形式，例如其中离子化药物分散在亲水性聚合物中的那些形式。 单位剂量适于作为药物储存器电极的一部分组装，使得离子化药物将经皮递送，然后当离子治疗装置运行时被全身吸收。

公开(公告)号：US5023084A

公开(公告)日：1991-06-11

申请号：US285878

申请日：1988-12-16

申请人： Yie W. Chien ,  Te-Yen Chien

发明人： Yie W. Chien ,  Te-Yen Chien

IPC分类号： A23G1/00 ,  A23G1/56 ,  A23G3/34 ,  A23J3/32 ,  A23J3/34 ,  A23K1/16 ,  A23K1/18 ,  A61F13/00 ,  A61F13/02 ,  A61K20060101 ,  A61K9/70 ,  A61K31/56 ,  A61K31/565 ,  A61K31/57 ,  A61K38/01

CPC分类号： A23J3/32 ,  A23G1/56 ,  A23G3/346 ,  A23J3/341 ,  A23J3/346 ,  A23K20/147 ,  A23K50/30 ,  A61F13/023 ,  A61F13/0253 ,  A61K31/565 ,  A61K31/567 ,  A61K38/011 ,  A61K38/012 ,  A61K9/7061 ,  A61K9/7069 ,  A61K9/7092 ,  A23V2002/00 ,  A61F2013/00544 ,  A61F2013/00906 ,  A61F2013/00927

摘要： Transdermal estrogen/progestin adsorption dosage units have been developed which comprise a backing layer, an adjoining polymer layer is an adhesive layer in which at least minimum effective dose of an estrogen is dissolved or microdispersed. Adhered to the polymer layer is an adhesive layer in which is dissolved and/or microdispersed at least minimum doses of progestin. Presently preferred is use of the natural estrogen, 17-beta-estradiol, or ethinyl estradiol or combinations thereof and of the progestin. The units have biologically acceptable adhesive and polymer layers. The adhesive layer can have dispersed one or more skin permeation enhancing agents. A separating layer can optionally be used in making the dosage units, which separate the adhesive and polymer layers, which permits estrogen transmission from the polymer layer during treatment. Dosage units are provided which transdermally deliver at least minimum daily doses of the estrogen and progestin for multiple days, such as for one week. The invention also provides a process for fertility control and estrogen replacement therapy using the novel dosage units. Also, the invention provides a fertility control system for fertility control using the novel dosage units.

摘要翻译： 已经开发了经皮雌激素/孕激素吸收剂量单位，其包含背衬层，相邻的聚合物层是其中至少最小有效剂量的雌激素溶解或微分散的粘合剂层。 粘附到聚合物层是粘合剂层，其中溶解和/或微分散至少最小剂量的孕激素。 目前优选使用天然雌激素，17-β-雌二醇或乙炔雌二醇或其组合和孕激素。 这些单元具有生物可接受的粘合剂和聚合物层。 粘合剂层可以具有分散的一种或多种皮肤渗透增强剂。 分离层可以任选地用于制备分离粘合剂和聚合物层的剂量单位，其允许在治疗期间从聚合物层传递雌激素。 提供剂量单位，其经皮递送至少最小日剂量的雌激素和孕激素多天，例如一周。 本发明还提供了使用新型剂量单位的生育调节和雌激素替代疗法的方法。 此外，本发明提供了使用新型剂量单位的育性控制的育性控制系统。

公开(公告)号：US4931281A

公开(公告)日：1990-06-05

申请号：US322605

申请日：1989-03-10

申请人： Kwon H. Kim ,  Norman L. Henderson ,  Yie W. Chien

发明人： Kwon H. Kim ,  Norman L. Henderson ,  Yie W. Chien

IPC分类号： A61K9/70 ,  A61L15/16 ,  A61M31/00 ,  A61M35/00

CPC分类号： A61K9/7084 ,  A61M31/002

摘要： A laminar structure for administering a chemical at a controlled release rate is disclosed. The structure comprises a backing member which acts as a boundary through which the chemical does not pass. Contacting at least a portion of the backing member is a chemical containing layer having therein a first chemical portion and a second chemical portion. The first and second chemical portions comprise a mixture of chemical in a first concentration transport mode and a second concentration transport mode. The mixture being in a ratio to give a desired chemical release rate from the chemical containing layer.

摘要翻译： 公开了一种用于以控制释放速率施用化学物质的层状结构。 该结构包括作为化学品不通过的边界的背衬构件。 接触背衬构件的至少一部分是其中具有第一化学部分和第二化学部分的化学容纳层。 第一和第二化学部分包括在第一浓度输送模式和第二浓度输送模式中的化学物质的混合物。 该混合物的比例是从含化学物质层得到期望的化学品释放速率。

公开(公告)号：US4883669A

公开(公告)日：1989-11-28

申请号：US868709

申请日：1986-05-30

申请人： Yie W. Chien ,  Chia-Shun Lee ,  Kirti H. Valia ,  Te-Yen Chien

发明人： Yie W. Chien ,  Chia-Shun Lee ,  Kirti H. Valia ,  Te-Yen Chien

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K31/565

CPC分类号： A61K9/7069 ,  A61K31/565 ,  A61K9/7084

摘要： This invention relates to a novel transdermal absorption dosage unit comprising a backing layer, an adjoining layer of solid polymer matrix in which estradiol or another steroidal pharmaceutical having estrogenic activity is microdispersed; and a biologically acceptable adhesive means by which the dosage unit adheres to the skin of the subject being administered said estradiol or another said steroidal pharmaceutical and adapted to permit transdermal absorption of said estradiol or another said steroidal pharmaceutical. Additionally, the invention relates to improved estradiol or other estrogenic steroid maintenance therapy.

摘要翻译： 本发明涉及一种新颖的经皮吸收剂量单位，其包括背层，邻接的固体聚合物基质层，其中雌二醇或具有雌激素活性的另一类甾族药物微分散; 和生物可接受的粘合剂方法，通过该方法，剂量单位粘附在施用所述雌二醇或另一种所述甾体药物的受试者皮肤上，并适于允许所述雌二醇或另一种所述甾体药物经皮吸收。 此外，本发明涉及改进的雌二醇或其它雌激素类固醇维持治疗。

公开(公告)号：US4690683A

公开(公告)日：1987-09-01

申请号：US751126

申请日：1985-07-02

申请人： Yie W. Chien ,  Kakuji Tojo

发明人： Yie W. Chien ,  Kakuji Tojo

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K31/275

CPC分类号： A61K9/7069 ,  A61K31/275 ,  A61K9/7084

摘要： A transdermal drug delivery device for administering 5-[(3,4-dimethoxyphenethyl) methylamino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile comprising a permeable matrix of silicone elastomer or other bioacceptable lipophilic polymer material having an effective cardiovascular affecting amount of active drug and an effective drug release promoting amount of a transport enhancing agent dispersed therein. The back of the matrix is covered with an occlusive backing and the face of the matrix is covered with a biocompatible adhesive such as a silicone adhesive also having a transport enhancing agent dispersed therein. A supply of skin permeation enhancing agent may be provided adjacent the adhesive layer such that the skin of a patient to whom the device is applied is pretreated with permeation enhancing agent. Particularly preferred skin permeation and transport enhancing agents include N,N-diethyl-m-toluamide, isopropyl myristate and similar compounds.

摘要翻译： 一种用于施用5 - [（3,4-二甲氧基苯乙基）甲基氨基] -2-（3,4-二甲氧基苯基）-2-异丙基戊腈的透皮药物递送装置，其包含有机硅弹性体的可渗透基质或其它具有有效心血管的生物可接受的亲脂性聚合物材料 影响分散在其中的活性药物的量和有效的药物释放促进量的运输增强剂。 基质的背面被闭塞背衬覆盖，并且基质的表面覆盖有生物相容性粘合剂，例如分散有运输增强剂的硅氧烷粘合剂。 可以在粘合剂层附近提供皮肤渗透增强剂的供应，使得施用该装置的患者的皮肤用渗透增强剂预处理。 特别优选的皮肤渗透和运输增强剂包括N，N-二乙基 - 间甲苯甲酰胺，肉豆蔻酸异丙酯和类似化合物。