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    • 4. 发明授权
    • Subsaturated transdermal therapeutic system having improved release
characteristics
    • 具有改善的释放特性的亚饱和透皮治疗系统
    • US5462745A
    • 1995-10-31
    • US297739
    • 1994-08-30
    • David J. EnscorePatricia S. CampbellJames L. OsborneMelinda K. SmartSu I. Yum
    • David J. EnscorePatricia S. CampbellJames L. OsborneMelinda K. SmartSu I. Yum
    • A61K9/70A61K31/46A61F13/02
    • A61K9/7084A61K31/46
    • 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.
    • 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在给定施用期间的活性降低超过约50%,优选不超过约25% 选择粘合剂,速率控制膜和储存层,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。