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    • 1. 发明申请
    • LIPID-DRUG COMPLEXES IN REVERSED LIQUID AND LIQUID CRYSTALLINE PHASES
    • 反相液相和液晶相中的脂质 - 药物复合物
    • WO2004012680A2
    • 2004-02-12
    • PCT/US2003/024512
    • 2003-08-06
    • LYOTROPIC THERAPEUTICS, INC.
    • ANDERSON, David, M.
    • A61K
    • A61K9/1274A61K47/541A61K47/55
    • A pharmaceutical is formulated to enable enhanced delivery across membrane barriers, permit solubilization, protect compounds from deactivation by thiol containing compounds in the body, and allow retention of the drug during transport to a desired site of activity. The pharmaceutical includes a complex of two moieties where at least one is pharmaceutically active and is larger than a single atom in size, and the second moiety, when combined with a cationic or anionic counterion forms either a pharmaceutically acceptable anionic or cationic surfactant or a pharmaceutically acceptable salt that has an octanol water partition coefficient of greater than about 100.
    • 配制药物以增强穿过膜屏障的递送,允许溶解,保护化合物免受体内含硫醇化合物的失活,并允许药物在运输至期望的活性部位期间保留。 药物包括两个部分的复合物,其中至少一个具有药学活性并且大于单个原子的大小,并且当第二部分与阳离子或阴离子平衡离子结合时形成药学上可接受的阴离子或阳离子表面活性剂或药学上可接受的 辛醇水分配系数大于约100的可接受盐。
    • 2. 发明申请
    • A NANOPOROUS PARTICLE WITH A RETAINED TARGET
    • 具有保留目标的纳米颗粒
    • WO2003106589A1
    • 2003-12-24
    • PCT/US2002/018657
    • 2002-06-13
    • LYOTROPIC THERAPEUTICS, INC.
    • ANDERSON, David, M.
    • C09K19/00
    • B82Y5/00C09K19/00C12Q1/68G01N33/5436C12Q2565/629
    • Porous nanostructured materials, such as porous nanostructured liquid and liquid crystalline particles or materials, incorporate a target substantially within the material which selectively binds a chemical of interest which can diffusion within the porous nanostructured material and be bound by the target. The porous nanostructured materials can be dispersed as particles in a medium in which said chemical of interest is located with low turbidity. Markers which detect binding of said chemical of interest can be maintained in the medium separate and apart from the target, and any active compound (e.g., an enzyme) associated therewith by the porous nanostructured material, such that detectable changes in the maker only result when the active compounds diffuse out of the porous nanostructured materials after the chemical of interest binds to the target.
    • 多孔纳米结构材料,例如多孔纳米结构化液体和液晶颗粒或材料,将基本上在目标物质内的目标物结合的材料中,靶材料选择性地结合目的化学物质,其可在多孔纳米结构化材料内扩散。 多孔纳米结构材料可以作为颗粒分散在所述感兴趣的化学物质位于低浊度的介质中。 检测所述化学物质的结合的标记物可以在分离和分离靶的培养基以及与多孔纳米结构材料相关联的任何活性化合物(例如,酶)中保持,使得制造商的可检测变化仅在 感兴趣的化学物质结合靶之后,活性化合物从多孔纳米结构材料中扩散出来。
    • 10. 发明申请
    • REVERSED LIQUID CRYSTALLINE PHASES WITH NON-PARAFFIN HYDROPHOBES
    • 具有非对映体疏水性的反相液晶相
    • WO2003106382A2
    • 2003-12-24
    • PCT/US2003/018457
    • 2003-06-13
    • LYOTROPIC THERAPEUTICS, INC.
    • ANDERSON, David, M.
    • C07C
    • A61K9/1274
    • Compounds which are otherwise difficult to solubilize, such as, for example, pharmaceutical actives difficult for the body to absorb, are solubilized into a composition using a solvent system that is a structured fluid. The structured fluid is a reversed cubic phase or reversed hexagonal phase material, or a combination thereof, which includes a polar solvent, a surfactant and a non-paraffinic liquid with a high octanol-water partition coefficient which does not qualify as a surfactant. The compositions thus formed are able to enhance absorption of drugs by the induction of local, transient nanopores in biomembrane absorption barriers and particularly those in which efflux mechanisms, such as those associated with P-glycoprotein and/or cytochrome 3A4, are active. The compositions and methods that are used for solubilizing pharmaceutical actives in structured fluids can simultaneously accomplish solubilization of difficultly soluble drugs and enhancement of absorption.
    • 否则难以溶解的化合物,例如难以吸收身体的药物活性成分,可以使用作为结构化流体的溶剂体系溶解到组合物中。 结构化流体是反相立方相或反相六方相材料或其组合,其包括极限溶剂,表面活性剂和具有高辛醇 - 水分配系数的非石蜡液体,其不被认为是表面活性剂。 由此形成的组合物能够通过诱导生物膜吸收屏障中的局部,瞬时纳米孔而增强药物的吸收,特别是其中外源机制(例如与P-糖蛋白和/或细胞色素3A4相关的那些)是活性的那些。 用于溶解结构化流体中的药物活性物质的组合物和方法可以同时完成难溶性药物的溶解和增强吸收。