公开(公告)号：US5560922A

公开(公告)日：1996-10-01

申请号：US461098

申请日：1995-06-05

申请人： Yie W. Chien ,  Te-Yen Chein

发明人： Yie W. Chien ,  Te-Yen Chein

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

CPC分类号： A61K9/7061 ,  A61K31/565 ,  A61K31/567 ,  A61K9/7084

摘要： Transdermal absorption dosage units have been developed which comprise a backing layer and an adjoining polyacrylate adhesive polymer layer in which at least minimum effective daily doses of one or more steroidal hormones are microdispersed. Presently preferred is use of the natural estrogen, 17-beta-estradiol, or ethinyl estradiol or combinations thereof together with an amount of a natural progestogen or a progestin to minimize any potential side effects. The units use bioacceptable polyacrylate adhesive polymer in making the adhesive polymer layer which has a minor percentage of vinyl acetate polymer units effective in providing improved transdermal absorption of the microdispersed steroidal hormone. An effective amount of vinyl acetate units up to about 5 percent has been found suitable. The invention also provides a process for transdermal administration of one or more steroidal hormones using the novel dosage units provided.

摘要翻译： 已经开发了经皮吸收剂量单位，其包含背衬层和相邻的聚丙烯酸酯粘合剂聚合物层，其中至少最小有效日剂量的一种或多种甾族激素是微分散的。 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以及一定量的天然孕激素或孕激素以最小化任何潜在的副作用。 这些单元使用生物可接受的聚丙烯酸酯粘合剂聚合物制备具有少量醋酸乙烯酯聚合物单元的粘合剂聚合物层，其有效提供微分散甾体激素的改善的经皮吸收。 发现有效量的高达约5％的乙酸乙烯酯单元是合适的。 本发明还提供了使用提供的新型剂量单位透皮给药一种或多种类固醇激素的方法。

公开(公告)号：US4806341A

公开(公告)日：1989-02-21

申请号：US903273

申请日：1986-09-03

申请人： Yie W. Chien ,  Chin-Chih Chiang ,  Kabuji Tojo

发明人： Yie W. Chien ,  Chin-Chih Chiang ,  Kabuji Tojo

IPC分类号： A61K9/70 ,  A61K31/485 ,  A61P25/04 ,  A61F13/00

CPC分类号： A61K9/7069 ,  A61K31/485 ,  A61K9/7084

摘要： Transdermal absorption morphinan narcotic analgesic or antagonist pharmaceutical polymer matrix dosage units have been developed which comprise a backing layer and an adjoining layer of a solid polymer matrix in which minimum effective doses of morphinan narcotic analgesic or antagonist pharmaceuticals are microdispersed and transdermally supplied. A presently preferred analgesic is hydromoprhone. The dosage units use a biologically acceptable adhesive polymer means to adhere the dosage units to the subject to be treated. The polymer matrix has dispersed one or more skin permeation enhancers. The invention also provides a process for transdermal absorption of said pharmaceuticals in at least minimum dosage amounts.

摘要翻译： 已经开发了经皮吸收吗啡喃麻醉止痛剂或拮抗剂药物聚合物基质剂量单位，其包含背衬层和固体聚合物基质的邻接层，其中最小有效剂量的吗啡喃麻醉止痛剂或拮抗剂药物是微分散和透皮供应的。 目前优选的止痛剂是hydropophone。 剂量单位使用生物可接受的粘合剂聚合物手段将剂量单位粘附到待治疗的受试者。 聚合物基质已经分散了一种或多种皮肤渗透促进剂。 本发明还提供了至少最小剂量的所述药物经皮吸收的方法。

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：US5762956A

公开(公告)日：1998-06-09

申请号：US638009

申请日：1996-04-24

申请人： Yie W. Chien ,  Te-Yen Chien ,  Sai-Jun Gong

发明人： Yie W. Chien ,  Te-Yen Chien ,  Sai-Jun Gong

IPC分类号： A61K9/70 ,  A61K31/565 ,  A61K31/57 ,  A61K47/10 ,  A61K47/14 ,  A61K47/20 ,  A61F13/00

CPC分类号： A61K9/7061 ,  A61K31/565 ,  A61K31/57 ,  A61K47/10 ,  A61K47/14 ,  A61K47/20 ,  Y10S514/946 ,  Y10S514/947

摘要： A transdermal contraceptive delivery system (TCDS) for fertility control in women is described comprising a backing layer, an adjoining layer of a solid absorption adhesive polymer matrix in which minimum effective daily doses of an estrogen and a progestin are dispersed and released for transdermal absorption. Presently preferred is use of the natural estrogen, 17-beta-estradiol, and the synthetic progestin, levonorgestrel. Along with these two steroidal contraceptive agents, a combination of several chemical skin permeation enhancing agents, blended at specific weight ratios, are homogeneously dispersed in the adhesive polymer matrix. The invention also provides a process of fertility control utilizing the transdermal contraceptive delivery system.

摘要翻译： 描述了一种用于妇女生育控制的透皮避孕药递送系统（TCDS），其包括背层，固体吸收性粘合剂聚合物基质的邻接层，其中分散和释放雌激素和孕激素的最小有效日剂量用于经皮吸收。 目前优选使用天然雌激素，17-β-雌二醇和合成孕激素左炔诺孕酮。 与这两种甾体避孕剂一起，以特定重量比共混的几种化学皮肤渗透增强剂的组合均匀地分散在粘合剂聚合物基质中。 本发明还提供利用透皮避孕药递送系统的生殖调控过程。

公开(公告)号：US5362308A

公开(公告)日：1994-11-08

申请号：US132133

申请日：1993-10-05

申请人： Yie W. Chien ,  Li-Lan H. Chen

发明人： Yie W. Chien ,  Li-Lan H. Chen

IPC分类号： A61K9/00 ,  A61N1/30

CPC分类号： A61K9/0009 ,  A61N1/0444 ,  A61N1/0448

摘要： Provided are disposable dosage units for use in iontophoresis-facilitated transdermal delivery which have hydrophilic polymer first and second layers, the first layer having ionic resin particles dispersed therein and the second layer having an ionized pharmaceutical contained. The second layer having on its surface a thin fabric layer bearing an adhesive layer. The polymer first and second layers are separated by a permselective membrane. Also provided are related devices and processes using the novel disposable dosage units.

摘要翻译： 提供用于离子电渗促进的透皮递送的一次性剂量单元，其具有亲水性聚合物第一和第二层，第一层具有分散在其中的离子树脂颗粒，第二层具有包含电离药物。 第二层在其表面上具有承载粘合剂层的薄织物层。 聚合物第一层和第二层被选择性渗透膜隔开。 还提供了使用新颖的一次性剂量单位的相关装置和方法。

公开(公告)号：US3946106A

公开(公告)日：1976-03-23

申请号：US517454

申请日：1974-10-24

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

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

IPC分类号： A61K47/34 ,  A61K9/00 ,  A61K9/20 ,  A61K9/52 ,  A61K47/32 ,  A61K9/26

CPC分类号： A61K9/0092 ,  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体系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：US5296230A

公开(公告)日：1994-03-22

申请号：US332471

申请日：1989-04-03

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 ,  A61F13/00

CPC分类号： A61K9/7069 ,  A61K9/7084 ,  A61K9/7092

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，固体聚合物基质的邻接层，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：US5250022A

公开(公告)日：1993-10-05

申请号：US587406

申请日：1990-09-25

申请人： Yie W. Chien ,  Ajay K. Banga

发明人： Yie W. Chien ,  Ajay K. Banga

IPC分类号： A61K9/00 ,  A61N1/30

CPC分类号： A61N1/0444 ,  A61K9/0009 ,  A61N1/0448 ,  A61N1/044

摘要： Provided are reservoir electrodes for iontotherapeutic devices which have two chambers; the first chamber is electrically connected to the iontotherapeutic device and is designed to contain electrolytic solution and the second chamber has ionized pharmaceutical dissolved in electrolytic solution. The two chambers are separated by a permselective membrane. The first chamber has means to inhibit increase in ionic content caused by the operation of the iontotherapeutic device. Also provided are unit dose forms adapted for insertion into the reservoir electrodes. The dose unit forms are made of crosslinked polymer and contain ionizable pharmaceutical which is released for absorption during operation of the iontotherapeutic process. Also provided are novel iontotherapeutic devices and processes.

摘要翻译： 提供了具有两个室的离子治疗装置的储存器电极; 第一室与离子治疗装置电连接，设计为含有电解液，第二室具有溶解在电解液中的电离药物。 两个室由选择性选择膜隔开。 第一室具有抑制由离子治疗装置的操作引起的离子含量增加的手段。 还提供了适于插入储存器电极的单位剂量形式。 剂量单位形式由交联聚合物制成并且包含可离子化药物，其在离子治疗过程的操作期间被释放以吸收。 还提供了新的离子治疗装置和方法。