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    • 5. 发明授权
    • Transdermal delivery system utilizing one way membranes
    • 使用单向膜的透皮递送系统
    • US5223262A
    • 1993-06-29
    • US565479
    • 1990-08-10
    • Sung W. KimTeruo OkanoSoon H. Yuk
    • Sung W. KimTeruo OkanoSoon H. Yuk
    • A61K9/70
    • A61K9/7084A61K9/7092Y10T428/31511Y10T428/31663
    • A system for transdermally delivering a hydrophobic alkanol soluble active agent to the skin at a constant rate utilizing a lower alkanol penetration enhancer. The system comprises an overlying solvent reservoir containing a lower alkanol solvent and a drug compartment containing an active agent in aqueous alkanol. A one-way membrane is sandwiched between and divides the solvent reservoir from the drum compartment. The one-way membrane is permeable to the alkanol solvent and substantially impermeable to back flux of drug and water into the reservoir. An outer membrane permeable to the alkanol solvent and drug is attached to the outer surface of the drug compartment. Adhesive means is contained on the outer surface of this membrane for attaching the delivery system to the skin of a wearer. Alkanol from the reservoir permeates into the drug compartment and drug and alkanol pass through the outer membrane to the skin of the wearer for transdermal absorption. The rate of alkanol permeation from the reservoir to the drug compartment and from the drug compartment to the skin is substantially constant. The membrane is made up of an epoxidized silicone rubber to which is preferably laminated a layer of a dense hydrophobic copolymer of vinyl-terminated polydimethyl siloxane with methylhydro-dimethyl siloxane. If desired, to prevent any back flux of hydrophobic drugs, and additional layer of cellulose acetate may be sandwiched between the epoxidized silicone rubber and dense hydrophobic membrane.
    • 一种利用低级烷醇渗透增强剂以一定速率将疏水性链烷醇可溶性活性剂透皮递送至皮肤的系统。 该系统包括含有低级链烷醇溶剂的上层溶剂储存器和在链烷醇水溶液中含有活性剂的药物隔室。 单向膜夹在溶剂容器和鼓室之间。 单向膜对于链烷醇溶剂是可渗透的,并且基本上不可渗透地将药物和水的通量回流到储存器中。 可通过链烷醇溶剂和药物的外膜附着到药物隔室的外表面。 粘合剂装在该膜的外表面上,用于将输送系统附着到穿着者的皮肤上。 来自储存器的烷醇渗透到药物隔室中,药物和链烷醇通过外膜到穿着者的皮肤以经皮吸收。 从储存器到药物隔室以及从药物室到皮肤的链烷醇渗透速率基本上是恒定的。 膜由环氧化的硅橡胶组成,其优选层压有乙烯基封端的聚二甲基硅氧烷与甲基氢二甲基硅氧烷的致密疏水性共聚物层。 如果需要,为了防止疏水性药物的任何回流,并且附加的乙酸纤维素层可夹在环氧化硅橡胶和致密疏水膜之间。
    • 6. 发明授权
    • Heterogeneous interpenetrating polymer networks for the controlled
release of drugs
    • 用于控释药物的非均相互穿聚合物网络
    • US4931287A
    • 1990-06-05
    • US206593
    • 1988-06-14
    • You H. BaeTeruo OkanoSung W. Kim
    • You H. BaeTeruo OkanoSung W. Kim
    • A61K9/20
    • A61K9/2031A61K9/2027
    • A heterogeneous interpenetrating polymer network is provided for use in the controlled release of drugs. The network is a heterogeneous matrix that is formed from a hydrophilic component such as polyethylene oxide or poly(N,N'-dimethyl acrylamide-co-styrene) and a hydrophobic component such as styrene, an alkyl methacrylate, or polytetramethylene ether glycol. The relative amounts of the two components, or "domains", can be varied, as can the diffusivities and solubilities of the drug combinations to be loaded therein, to control and change as desired the timed release profile of incorporated drug. Prolonged pseudo-zero order release can be obtained where one domain acts as a diffusion barrier layer to the release of drug from the other domain.
    • 提供异构互穿聚合物网络用于药物的控制释放。 该网络是由亲水组分如聚环氧乙烷或聚(N,N'-二甲基丙烯酰胺 - 共 - 苯乙烯)和疏水组分如苯乙烯,甲基丙烯酸烷基酯或聚四亚甲基醚二醇形成的非均相基体。 可以改变两种组分或“结构域”的相对量,以及待加载的药物组合的扩散性和溶解度,以控制并根据需要改变并入药物的定时释放曲线。 可以获得延长的伪零次释放,其中一个结构域充当从另一个域释放药物的扩散阻挡层。
    • 8. 发明授权
    • Pulsatile drug delivery device using stimuli sensitive hydrogel
    • 使用刺激敏感水凝胶的脉冲药物递送装置
    • US5226902A
    • 1993-07-13
    • US737675
    • 1991-07-30
    • You H. BaeSung W. KimLev I. Valuev
    • You H. BaeSung W. KimLev I. Valuev
    • A61K9/00A61K9/22
    • A61K9/0004Y10S514/965
    • A device for the dispensing of a biologically active material into the surrounding environment is disclosed which consists of at least one wall enclosing a compartment which contains a swollen stimuli sensitive hydrogel in which the biologically active material is entrained in solution. The hydrogel deswells or shrinks in response to contact by external physical or chemical stimuli releasing the biologically active material into the portion of the compartment previously occupied by the swollen hydrogel. The wall enclosing the compartment is rigid and contains means allowing the passage of the biologically active material from the compartment to the surrounding environment and also for transmitting the external stimuli to the swollen hydrogel in said compartment. The wall may contain orifices or be permeable to the active material and external stimuli depending upon the drug and the stimuli to be used. The hydrogel reversibly deswells, shrinks or contracts in response to stimuli, such as temperature, pH, ionic strength, glucose concentration or metabolites in the body and then reswells and reentrains active material not diffused from the compartment when the stimuli is removed. The wall may consist of one or more layers which, in combination, provide for the expeditious delivery of the active substance either through permeation through the wall or through orifices in the wall and also for the conducting of the external stimuli through the wall into the compartment to trigger the deswelling of the hydrogel.
    • 公开了一种用于将生物活性物质分配到周围环境中的装置,其由至少一个包围腔室的壁组成,所述隔室包含溶胀的刺激性敏感水凝胶,其中生物活性物质被夹带在溶液中。 水凝胶响应于外部物理或化学刺激的接触而溶解或收缩,将生物活性物质释放到先前由膨胀的水凝胶占据的隔室部分。 包围隔室的壁是刚性的并且包含允许生物活性材料从隔室通过到周围环境的装置,并且还用于将外部刺激传递到所述隔室中的溶胀水凝胶。 根据药物和使用的刺激,该壁可能含有孔口或对活性物质可渗透和外部刺激。 水凝胶可以响应于身体中的温度,pH,离子强度,葡萄糖浓度或代谢物等刺激而可逆地解冻,收缩或收缩,然后在去除刺激物时,将不会从隔室扩散的活性物质重新流通并重新吸入。 该壁可以由一个或多个层组成,其组合地提供活性物质的快速递送,所述活性物质通过壁穿过壁或通过壁中的孔,并且还用于通过壁进入外部刺激进入隔室 触发水凝胶的溶解。