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    • 1. 发明授权
    • Transdermal varapamil delivery device
    • 透皮诺帕米尔输送装置
    • US4690683A
    • 1987-09-01
    • US751126
    • 1985-07-02
    • Yie W. ChienKakuji Tojo
    • Yie W. ChienKakuji Tojo
    • A61K9/00A61K9/70A61K31/275
    • A61K9/7069A61K31/275A61K9/7084
    • 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.
    • 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。
    • 4. 发明授权
    • Transdermal fertility control system and process
    • 透皮生育控制系统和过程
    • US4818540A
    • 1989-04-04
    • US902440
    • 1986-08-29
    • Yie W. ChienTe-Yen ChienYih-Chain Huang
    • Yie W. ChienTe-Yen ChienYih-Chain Huang
    • A61K9/70A61K31/565A61K31/57A61F13/00
    • A61K9/7069A61K9/7084
    • 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.
    • 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。
    • 5. 发明授权
    • Method for making a microsealed delivery device
    • 制造微密封输送装置的方法
    • US3992518A
    • 1976-11-16
    • US617542
    • 1975-09-29
    • Yie W. ChienHoward J. Lambert
    • Yie W. ChienHoward J. Lambert
    • A61K9/00A61K9/20A61K9/26
    • A61K9/0092A61K9/0024A61K9/0039A61K9/2036
    • 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.
    • 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。
    • 8. 发明授权
    • Microsealed pharmaceutical delivery device
    • 微胶囊药物输送装置
    • US3946106A
    • 1976-03-23
    • US517454
    • 1974-10-24
    • Yie W. ChienHoward J. Lambert
    • Yie W. ChienHoward J. Lambert
    • A61K47/34A61K9/00A61K9/20A61K9/52A61K47/32A61K9/26
    • A61K9/0092A61K9/0039A61K9/2036
    • 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.
    • 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。
    • 9. 发明授权
    • Transdermal absorption dosage unit using a polyacrylate adhesive polymer
and process
    • 透皮吸收剂量单位采用聚丙烯酸酯粘合剂聚合物和方法
    • US5560922A
    • 1996-10-01
    • US461098
    • 1995-06-05
    • Yie W. ChienTe-Yen Chein
    • Yie W. ChienTe-Yen Chein
    • A61K9/70A61K31/565A61F13/00
    • A61K9/7061A61K31/565A61K31/567A61K9/7084
    • 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.
    • 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。
    • 10. 发明授权
    • Transdermal fertility control system and process
    • 透皮生育控制系统和过程
    • US5296230A
    • 1994-03-22
    • US332471
    • 1989-04-03
    • Yie W. ChienTe-Yen ChienYih-Chain Huang
    • Yie W. ChienTe-Yen ChienYih-Chain Huang
    • A61K9/70A61F13/00
    • A61K9/7069A61K9/7084A61K9/7092
    • 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.
    • 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。