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    • 1. 发明申请
    • COMPOSITIONS AND METHODS ENHANCING TRANSDERMAL DELIVERY OF DRUGS AND BIOLOGICS
    • 组合物和方法增强药物和生物学的转运
    • WO2006091719A2
    • 2006-08-31
    • PCT/US2006006385
    • 2006-02-23
    • SONTRA MEDICAL CORPBARMAN SHIKHA PFARNHAM HANNAHROODE LAUREN KWAN ANNA
    • BARMAN SHIKHA PFARNHAM HANNAHROODE LAUREN KWAN ANNA
    • A61K9/0009A61K9/0014A61K9/0019
    • Improved methods for transdermal transport of drug formulations are described herein. Formulations designed to enhance transport of therapeutic levels of topically applied drugs into the systemic circulation, methods of making the formulations are also described herein. The formulations contain at least one active agent to be delivered and at least one skin permeation enhancer in a polymeric hydrogel, and optional additional excipients. Methods for enhancing transport of formulations into and through the skin include: (a) pretreatment of the skin with a hydrating solution, (b) physical permeation of the stratum corneum by low frequency ultrasound (administered by a sono-permeation device, such as SONOPREP ® , available from Sontra Medical Corporation, Franklin, MA), (c) topical application of a formulation containing the bioactive molecule, and optionally (d) application of an electric potential difference that forces ionized drugs through the skin. Optionally, the formulation contains permeation-enhancing agents. The method may be used with the formulations described herein or with other formulations for topical administration. In a preferred embodiment, the active agent to be delivered is a drug. Preferably the drug is a local anesthetic, such as lidocaine.
    • 本文描述了用于药物制剂的透皮转运的改进方法。 设计用于增强局部应用药物治疗水平进入体循环的制剂,制备制剂的方法也在本文中描述。 制剂含有至少一种待递送的活性剂和聚合物水凝胶中至少一种皮肤渗透促进剂,以及任选的另外的赋形剂。 用于增强制剂进入皮肤和通过皮肤的运输的方法包括:(a)用水合溶液预处理皮肤,(b)通过低频超声(由超音波渗透装置如SONOPREP施用的角质层的物理渗透 (Sontra Medical Corporation,Franklin,MA)),(c)局部施用含有生物活性分子的制剂,以及任选地(d)施加电离差,其强制电离药物通过 皮肤。 任选地,制剂含有渗透增强剂。 该方法可以与本文所述的制剂一起使用或与其它用于局部给药的制剂一起使用。 在优选的实施方案中,待递送的活性剂是药物。 优选地,药物是局部麻醉剂,例如利多卡因。