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    • 5. 发明申请
    • LIPOPHILIC COMPOSITIONS
    • 脂质组合物
    • WO2004071494A3
    • 2004-12-16
    • PCT/EP2004001355
    • 2004-02-13
    • PHARES PHARM RES NVLEIGH MATHEW LOUIS STEVENVAN HOOGEVEST PETERQUINTON JACQUESLEIGH STEVE
    • LEIGH MATHEW LOUIS STEVENVAN HOOGEVEST PETERQUINTON JACQUESLEIGH STEVE
    • A61K9/14A61K9/16A61K9/48
    • A61K9/1652A61K9/146A61K9/4866
    • There is described dry compositions comprising lipophilic compounds associated with low viscosity grades of water insoluble polymer and optionally hydrophilic agent/ s associated either as monomolecular or amorphous complexes. There is also described a method of preparing said lipophilic polymer complexes from a solution or homogeneous dispersion employing either water miscible or immiscible organic solvents. The lipophilic polymer complex is precipitated from the solution comprising a water miscible solvent by dilution with water, separating out the precipitated complex, washing, drying and conversion to oral and topical dosage forms. The lipophilic polymer complex may also be prepared by solvent removal involving spray drying or vacuum drying under elevated temperatures using either water miscible or water immiscible solvents. The compositions are characterised by improved dissolution and solubility of the associated compound in aqueous medium.
    • 描述了干组合物,其包含与低粘度等级的水不溶性聚合物结合的亲脂性化合物和任选地作为单分子或无定形复合物缔合的亲水性试剂。 还描述了从使用水可混溶或不可混溶的有机溶剂的溶液或均匀分散体制备所述亲脂性聚合物复合物的方法。 亲水性聚合物复合物通过用水稀释而从包含水混溶性溶剂的溶液中沉淀出来,分离出沉淀的复合物,洗涤,干燥并转化为口服和局部剂型。 亲脂性聚合物复合物也可以通过溶剂去除来制备,包括喷雾干燥或在升高的温度下使用水混溶性或水不混溶性溶剂进行真空干燥。 该组合物的特征在于相关化合物在水性介质中的溶解度和溶解度提高。
    • 7. 发明申请
    • TEST SYSTEM AND METHOD SUITABLE FOR SELECTING TEST MATERIALS AND FORMULATIONS
    • 适用于选择测试材料和配方的测试系统和方法
    • WO03010330A2
    • 2003-02-06
    • PCT/EP0208215
    • 2002-07-23
    • PHARES PHARM RES NVLEIGH STEVELEIGH MATHEW LOUIS STEVENVAN HOOGEVEST PETERTIEMESSEN HENRICUS
    • LEIGH STEVELEIGH MATHEW LOUIS STEVENVAN HOOGEVEST PETERTIEMESSEN HENRICUS
    • G01N33/50G01N33/543G01N33/92C12Q1/00
    • G01N33/92G01N33/5432G01N2500/20
    • The present invention provides a test system and a method for screening lipophilic and amphipathic materials with low water solubility. It generally relates to membrane lipid suspensions or dispersions employed as a test system for obtaining desired physico-chemical and biological information relating to the interaction of materials with membrane lipids in early screens in discovery. It serves as a selection method for derivatives of a test material for optimal membrane affinity and membrane permeation and thereby predict the potential for absorption in vivo. Furthermore, it may be used in later screening in formulation development, to select a carrier for a test material or derivative to enable the highest drug load. The data obtained by using the invention in primary screening provide key information on physico-chemical properties early on which may affect drug absorption and may be more predictive than log-octanol determinations. Compared to other screening methods which utilise cell models such as liposomes and cell lines, Transmembrane Screen (TS) is a versatile miniature tool that requires minimal amounts of test substances. It is adaptable, practical, cost effective and may be used routinely in high throughput screening.
    • 本发明提供了用于筛选具有低水溶性的亲脂和两亲物质的测试系统和方法。 它通常涉及膜脂悬浮液或分散体,其用作用于在发现的早期筛选中获得与材料与膜脂质的相互作用相关的期望的物理化学和生物学信息的测试系统。 它用作测试材料衍生物的选择方法,以获得最佳膜亲和力和膜渗透性,从而预测体内吸收的可能性。 此外,它可用于配方开发的后期筛选,以选择用于测试材料或衍生物的载体以实现最高药物负载。 通过在初步筛选中使用本发明获得的数据提供了关于早期物理化学性质的关键信息,其可能影响药物吸收并且可能比对 - 辛醇测定更具预测性。 与利用细胞模型(如脂质体和细胞系)的其他筛选方法相比,跨膜筛选(TS)是一种多功能的微型工具,只需要最少量的测试物质。 它具有适应性,实用性和成本效益,可以在高通量筛选中常规使用。