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    • 2. 发明授权
    • Mixed solvent mutually enhanced transdermal therapeutic system
    • 混合溶剂相互增强透皮治疗系统
    • US5925372A
    • 1999-07-20
    • US725222
    • 1991-06-26
    • Bret BernerCharles EbertGerard C. MazzengaJohn H. Otte
    • Bret BernerCharles EbertGerard C. MazzengaJohn H. Otte
    • A61K9/70A61F13/02
    • A61K9/7069A61K9/7084
    • A transdermal drug delivery system comprising(i) an occlusive, impermeable polymeric backing layer;(ii) a drug depot on one side thereof;(iii) a removable, occlusive covering layer over said drug depot; and(iv) an adhesive means by which said delivery system, absent said removable covering layer may be affixed to an intended patient;said drug depot containing a drug formulation comprising a transdermally administrable pharmaceutically acceptable pharmaceutically active agent or a precursor thereof, water and lower alkanol; said active agent or precursor thereof being present in a pharmaceutically effective amount; said lower alkanol and said water being present in a volume:volume ratio of from 30:70 up to less than 95:5 such that said lower alkanol, water and drug are delivered to a patient's skin, which patient has applied said system absent said removable covering layer to said patient's skin, in amounts that said drug is delivered in a transdermally administrable efficacious amount, said water has an activity at said patient's skin of about 0.4 to about 0.95 and said lower alkanol, at said patient's skin, has an activity of 0.3 to about 0.9, and wherein, once applied to said patient's skin, said lower alkanol has a flux from said system to said skin of at least 1500 mcg/cm.sup.2 /hr and through said skin of at least 1500 mcg/cm.sup.2 /hr.
    • 一种透皮药物递送系统,其包括(i)封闭的,不可渗透的聚合物背衬层; (ii)其一侧的药剂库; (iii)所述药物库上的可移除的封闭覆盖层; 和(iv)粘合剂装置,其中没有所述可移除覆盖层的所述递送系统可以被固定到预期的患者身上; 所述药物贮库含有药物制剂,其包含透皮给药的药学上可接受的药物活性剂或其前体,水和低级链烷醇; 所述活性剂或其前体以药学上有效的量存在; 所述低级链烷醇和所述水以体积比为30:70至小于95:5存在,使得所述低级链烷醇,水和药物被递送至患者的皮肤,该患者应用所述系统不存在所述 所述药物以经皮可施用的有效量递送的量,所述水在所述患者皮肤上具有约0.4至约0.95的活性,并且所述低级烷醇在所述患者皮肤处具有活性 0.3至约0.9,并且其中一旦施用于所述患者皮肤,所述低级链烷醇具有从所述系统到所述皮肤的通量至少为1500mcg / cm 2 /小时,并且通过所述皮肤至少为1500mcg / cm 2 /小时 。