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    Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof
    2.
    发明授权
    Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof 失效
    蛋白质稳定的药理活性剂，其制备方法及其使用方法

    公开(公告)号：US06749868B1

    公开(公告)日：2004-06-15

    申请号：US09316642

    申请日：1999-05-21

    申请人： Neil P. Desai ,  Chunlin Tao ,  Andrew Yang ,  Leslie Louie ,  Zhiwen Yao ,  Patrick Soon-Shiong ,  Shlomo Magdassi

    发明人： Neil P. Desai ,  Chunlin Tao ,  Andrew Yang ,  Leslie Louie ,  Zhiwen Yao ,  Patrick Soon-Shiong ,  Shlomo Magdassi

    IPC分类号： A61K916

    CPC分类号： A61K9/0026 ,  A23L33/40 ,  A61K9/5052 ,  A61K9/5169 ,  A61K47/6929 ,  B82Y5/00

    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 election 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， 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，而其中没有任何聚合物基质。

    Multiparticulate bisoprolol formulation
    3.
    发明授权
    Multiparticulate bisoprolol formulation 失效
    多微粒比索洛尔制剂

    公开(公告)号：US06733789B1

    公开(公告)日：2004-05-11

    申请号：US09488103

    申请日：2000-01-20

    申请人： Paul Stark ,  Catherine Mary Kelly ,  Niall M. Fanning

    发明人： Paul Stark ,  Catherine Mary Kelly ,  Niall M. Fanning

    IPC分类号： A61K916

    CPC分类号： A61K9/5078 ,  A61K9/5026 ,  A61K31/138

    摘要： A multiparticulate bisoprolol formulation for once-daily oral administration, each particle of which comprises a core of bisoprolol or a pharmaceutically acceptable salt thereof surrounded by a polymeric coating, the polymeric coating being effective to achieve an initial lag of bisoprolol release in vivo of at least 4-6 hours following administration and thereafter maintaining therapeutic concentrations of bisoprolol for the remainder of the twenty-four hour period. The formulation can be used for night-time dosing so as to minimize the likelihood of acute cardiovascular occurrences in the well-documented high risk period in the morning.

    摘要翻译： 一种每日一次的口服给药的多颗粒比索洛尔制剂，其每个颗粒包含由聚合物涂层包围的比索洛尔核心或其药学上可接受的盐，所述聚合物涂层有效地达到至少在体内释放比索洛尔的初始滞留 给药后4-6小时，然后在二十四小时的剩余时间内维持比索洛尔的治疗浓度。 该制剂可用于夜间给药，以便在早晨记录良好的高危时期内尽量减少急性心血管事件发生的可能性。

    Instant granules and process for their formulation
    5.
    发明授权
    Instant granules and process for their formulation 有权

    公开(公告)号：US06645529B2

    公开(公告)日：2003-11-11

    申请号：US09857459

    申请日：2001-06-05

    申请人： Gerhard Gergely ,  Irmgard Gergely

    发明人： Gerhard Gergely ,  Irmgard Gergely

    IPC分类号： A61K916

    CPC分类号： A61K9/0095 ,  A61K9/1676

    摘要： The pharmaceutical formulation according to the invention is in the form of instant granules, in which the surface of the particles of at least two different soluble carrier materials is covered or coated with at least one layer which contains -of from 50 to 120, preferably from about 60 to about 100, parts by weight of active substance per 100 parts by weight of carrier material -of at least one, preferably insoluble or slightly soluble, active substance, such as amino acids or antioxidants. A first carrier material constitutes from about 50 to about 80% by weight of the total carrier material and is selected from carrier materials having a bulk density of between 58 and 100, preferably between 63 and 90 g/100 ml, while the second carrier material is selected from carrier materials having a bulk density of between 30 to 55, preferably between 33 and 50 g/100 ml.

    Solid carriers for improved delivery of hydrophobic active ingredients in pharmaceutical compositions
    8.
    发明授权
    Solid carriers for improved delivery of hydrophobic active ingredients in pharmaceutical compositions 有权
    用于改善药物组合物中疏水性活性成分递送的固体载体

    公开(公告)号：US06569463B2

    公开(公告)日：2003-05-27

    申请号：US09800593

    申请日：2001-03-06

    申请人： Mahesh V. Patel ,  Feng-Jing Chen

    发明人： Mahesh V. Patel ,  Feng-Jing Chen

    IPC分类号： A61K916

    CPC分类号： A61K47/14 ,  A61K9/1617 ,  A61K9/1676 ,  A61K9/4858 ,  A61K9/5015 ,  A61K9/5026 ,  A61K9/5078 ,  A61K9/5084 ,  A61K31/352 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/568 ,  A61K31/7048 ,  A61K47/10 ,  B82Y5/00 ,  Y02A50/463 ,  Y10S977/906 ,  Y10S977/927

    摘要： The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

    摘要翻译： 本发明提供用于改善递送其中所含的各种药物活性成分或单独施用的固体药物组合物。 在一个实施方案中，固体药物组合物包括固体载体，固体载体包括底物和基材上的包封涂层。 包封涂层可以包括药物活性成分，亲水性表面活性剂，亲脂性表面活性剂和甘油三酯的不同组合。 在另一个实施方案中，固体药物组合物包括固体载体，固体载体由药物活性成分，亲水性表面活性剂，亲脂性表面活性剂和甘油三酸酯的不同组合形成。 本发明的组合物可用于改善递送亲水或疏水性药物活性成分，例如药物，营养成分，药妆和诊断剂。

    Process for producing small particles of biologically active molecules
    9.
    发明授权
    Process for producing small particles of biologically active molecules 失效
    用于生产生物活性分子的小颗粒的方法

    公开(公告)号：US06569458B1

    公开(公告)日：2003-05-27

    申请号：US08006682

    申请日：1993-01-21

    申请人： Wayne R. Gombotz ,  Michael S. Healy ,  Larry R. Brown ,  Henry E. Auer

    发明人： Wayne R. Gombotz ,  Michael S. Healy ,  Larry R. Brown ,  Henry E. Auer

    IPC分类号： A61K916

    CPC分类号： A61K9/1694 ,  A61K9/1688

    摘要： Small diameter particles of biologically active molecules are produced by atomizing solutions of the molecules through a nozzle into very cold liquified gases, which immediately freeze the atomized droplets. The resulting frozen particles having diameters of approximately 10 to 90 micrometers are lyophilized to produce porous particles, suspended in a non-solvent for the molecules, and exposed to ultrasonic energy or homogenization to produce particles having diameters of 0.1 to 10 micrometers with greater than 70 to 95% of the initial biological activity of the molecules in solution.

    摘要翻译： 生物活性分子的小直径颗粒通过将分子的溶液通过喷嘴雾化成非常冷的液化气体而产生，其立即冷冻雾化的液滴。 将所得直径约为10至90微米的冷冻颗粒冻干以产生悬浮于分子的非溶剂中的多孔颗粒，并暴露于超声波能量或均化，以产生直径为0.1至10微米的颗粒，大于70 至溶液中分子的初始生物活性的95％。