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    Novel formulations of pharmacological agents, methods for the preparation thereof and methods for the use thereof
    38.
    发明申请
    Novel formulations of pharmacological agents, methods for the preparation thereof and methods for the use thereof 审中-公开
    药剂的新型制剂，其制备方法及其使用方法

    公开(公告)号：US20080161382A1

    公开(公告)日：2008-07-03

    申请号：US11890197

    申请日：2007-08-03

    申请人： Neil Desai ,  Chunlin Tao ,  Patrick Soon-Shiong

    发明人： Neil Desai ,  Chunlin Tao ,  Patrick Soon-Shiong

    IPC分类号： A61K31/337 ,  A61P35/00

    CPC分类号： A61K9/5169 ,  A61K9/5192

    摘要： In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.

    摘要翻译： 根据本发明，提供了用于体内递送基本上不溶于水的药理学活性剂（例如抗癌药物紫杉醇）的组合物和方法，其中药理活性剂以包被的 蛋白质（其作为稳定剂）。 特别地，生物相容性分散介质中的蛋白质和药理学活性剂在没有任何常规表面活性剂的情况下进行高剪切，并且在没有用于颗粒的任何聚合物芯材料的情况下进行。 该方法产生直径小于约1微米的颗粒。 使用特定的组成和制备条件（例如，向有机相中加入极性溶剂）以及仔细选择合适的有机相和相分数使得能够可重复地生产直径小于200nm的异常小的纳米颗粒，其中 可以无菌过滤。 根据本发明制备的颗粒系统可以转化成可再分散的干粉，其包含用蛋白质包被的水不溶性药物的纳米颗粒，以及结合有药理学分子的游离蛋白质。 这导致独特的递送系统，其中药理活性剂的一部分容易生物利用（以与蛋白质结合的分子的形式），并且部分药剂存在于颗粒内，而没有其中的任何聚合物基质。