FORMULATIONS AND METHODS FOR TARGETED OCULAR DELIVERY OF THERAPEUTIC AGENTS
    2.
    发明申请
    FORMULATIONS AND METHODS FOR TARGETED OCULAR DELIVERY OF THERAPEUTIC AGENTS 审中-公开
    靶向治疗药物眼部的配方和方法

    公开(公告)号:WO2015095772A2

    公开(公告)日:2015-06-25

    申请号:PCT/US2014/071623

    申请日:2014-12-19

    Abstract: Formulations, systems, and methods of administration are provided for preferential targeted delivery of drug to ocular tissue. In embodiments, the formulation may include a non-Newtonian fluid that facilitates targeted localization or preferential spreading of the fluid formulation in the ocular tissue. The fluid formulation may be administered to an eye of a patient by inserting a microneedle into the eye at an insertion site, and infusing a volume of a fluid formulation through the microneedle into the suprachoroidal space of the eye at the insertion site over a first period. During the first period, the fluid formulation may be distributed over a first region which is less than about 10% of the suprachoroidal space, and during the second period subsequent to the first period the drug formulation may be distributed over a second region which is greater than about 20% of the suprachoroidal space.

    Abstract translation: 提供给药的制剂,系统和方法用于将药物优先靶向递送至眼组织。 在实施方案中,所述制剂可以包括促进所述流体制剂在所述眼组织中的定向定位或优先扩散的非牛顿流体。 可以通过在插入位置处将微针插入眼睛中并且在插入位置处在第一时间段内将一定体积的流体制剂通过微针注入到眼睛的脉络膜上腔中来将流体制剂施用于患者的眼睛 。 在第一阶段期间,流体制剂可以分布在少于脉络膜上腔的约10%的第一区域上,并且在第一阶段之后的第二阶段期间,药物制剂可以分布在更大的第二区域 超过脉络膜上腔的约20%。

    AGGREGATE NANOPARTICULATE MEDICAMENT FORMULATIONS, MANUFACTURE AND USE THEREOF
    4.
    发明申请
    AGGREGATE NANOPARTICULATE MEDICAMENT FORMULATIONS, MANUFACTURE AND USE THEREOF 审中-公开
    合成纳米颗粒药物制剂,制造及其用途

    公开(公告)号:WO2012051426A3

    公开(公告)日:2013-10-17

    申请号:PCT/US2011056166

    申请日:2011-10-13

    Abstract: A method of making aggregate particles suitable for a pharmaceutical aerosol composition that includes (a) forming a dispersion of nanoparticulate drug particles and/or excipient nanoparticles in a non-aqueous liquid, wherein said particles have a solubility of less than 10 mg/ml in said liquid dispersing media, wherein the nanoparticulate drug particles have a preselected crystalline form; (b) spray- drying the dispersion of nanoparticulate drug particles and/or nanoparticulate excipient particles to generate aggregate particles comprising nanoparticulate drug particles and/or nanoparticulate excipient particles, wherein the drug and/or excipient nanoparticles have maintained their preselected crystalline form, and wherein the aggregate particles have a mass median diameter of less than or equal to about 100 microns and wherein when the nanoparticles dispersed in said dispersion do not comprise excipient. the aggregate particles is substantially free of a homogenizing surfactant. When the nanoparticles in said dispersion do not comprise excipient, the non-aqueous liquid has no suspension surfactant.

    Abstract translation: 制备适合于药物气溶胶组合物的骨料颗粒的方法,其包括(a)在非水性液体中形成纳米颗粒状药物颗粒和/或赋形剂纳米颗粒的分散体,其中所述颗粒的溶解度小于10mg / ml 所述液体分散介质,其中所述纳米颗粒药物颗粒具有预选的结晶形式; (b)喷雾干燥纳米颗粒药物颗粒和/或纳米颗粒赋形剂颗粒的分散体以产生包含纳米颗粒药物颗粒和/或纳米颗粒赋形剂颗粒的聚集颗粒,其中所述药物和/或赋形剂纳米颗粒保持其预选的结晶形式,并且其中 聚集颗粒具有小于或等于约100微米的质量中值直径,并且其中当分散在所述分散体中的纳米颗粒不包含赋形剂时。 聚集体颗粒基本上不含均化表面活性剂。 当所述分散体中的纳米颗粒不包含赋形剂时,非水性液体不含悬浮表面活性剂。

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