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21. 发明申请

WO2004071494A3 LIPOPHILIC COMPOSITIONS 审中-公开
标题翻译：脂质组合物
公开(公告)号：WO2004071494A3
公开(公告)日：2004-12-16
申请号：PCT/EP2004001355
申请日：2004-02-13
申请人： PHARES PHARM RES NV , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER , QUINTON JACQUES , LEIGH STEVE
发明人： LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER , QUINTON JACQUES , LEIGH STEVE
IPC分类号： A61K9/14 , A61K9/16 , A61K9/48
CPC分类号： A61K9/1652 , A61K9/146 , A61K9/4866
摘要： 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.
摘要翻译：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。

22. 发明申请

WO2003102116A3 OIL-SOLUBLE PIGMENT COMPOSITIONS 审中-公开
公开(公告)号：WO2003102116A3
公开(公告)日：2003-12-11
申请号：PCT/EP2003/005631
申请日：2003-05-28
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
发明人： LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
IPC分类号： C09B61/00
摘要： The present invention relates to a process for the preparation of an oily solution of a carotenoid, particularly astaxanthin, a composition comprising at least one xanthophyll and at least one suitable solvent, particularly n-methyl-pyrrolidone, a composition comprising a carotenoid and a mixture of mono-, di- and triglycerides subjected to enzyme treatment, glycerolysis and/or fractionation, and a solid homogeneous mixture comprising one xanthophyll in a physiologically acceptable amount and at least one lipophilic dispersing agent. The process is useful for preparing nutrient or pharmaceutical compositions.

23. 发明申请

WO2003102116A2 OIL SOLUBLE COMPOSITIONS 审中-公开
标题翻译：油溶性组合物
公开(公告)号：WO2003102116A2
公开(公告)日：2003-12-11
申请号：PCT/EP2003/005631
申请日：2003-05-28
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
发明人： LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
IPC分类号： C10M
CPC分类号： C09B67/0083 , A23K20/179 , A23K50/80 , A23L5/42 , A23L5/44 , A23L27/00 , A23L33/105 , A23L33/15 , A61K9/0014 , A61K9/1652 , A61K47/44 , C09B61/00
摘要： The present invention relates to a process for the preparation of an oily solution of a carotenoid, particularly astaxanthin, a composition comprising at least one xanthophyll and at least one suitable solvent, particularly n-methyl-pyrrolidone, a composition comprising a carotenoid and a mixture of mono-, di- and triglycerides subjected to enzyme treatment, glycerolysis and/or fractionation, and a solid homogeneous mixture comprising one xanthophyll in a physiologically acceptable amount and at least one lipophilic dispersing agent. The process is useful for preparing nutrient or pharmaceutical compositions.
摘要翻译：本发明涉及一种制备类胡萝卜素，特别是虾青素的油性溶液的方法，包含至少一种叶黄素和至少一种合适的溶剂，特别是N-甲基吡咯烷酮的组合物，包含类胡萝卜素和混合物的组合物经过酶处理，甘油分解和/或分级分离的单，二和甘油三酸酯，以及包含一种生理上可接受量的叶黄素和至少一种亲脂性分散剂的固体均匀混合物。该方法可用于制备营养素或药物组合物。

24. 发明申请

WO03023394A8 KIT FOR SCREENING COMPOUNDS WITH LOW WATER SOLUBILITY 审中-公开
标题翻译：用于筛选具有低水溶性的化合物的试剂盒
公开(公告)号：WO03023394A8
公开(公告)日：2003-10-30
申请号：PCT/EP0210241
申请日：2002-09-12
申请人： PHARES PHARM RES NV , LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER , TIEMESSEN HENRICUS
发明人： LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER , TIEMESSEN HENRICUS
IPC分类号： G01N33/15 , G01N33/92
CPC分类号： G01N33/92

25. 发明申请

WO03010330A2 TEST SYSTEM AND METHOD SUITABLE FOR SELECTING TEST MATERIALS AND FORMULATIONS 审中-公开
标题翻译：适用于选择测试材料和配方的测试系统和方法
公开(公告)号：WO03010330A2
公开(公告)日：2003-02-06
申请号：PCT/EP0208215
申请日：2002-07-23
申请人： PHARES PHARM RES NV , LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER , TIEMESSEN HENRICUS
发明人： LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER , TIEMESSEN HENRICUS
IPC分类号： G01N33/50 , G01N33/543 , G01N33/92 , C12Q1/00
CPC分类号： G01N33/92 , G01N33/5432 , G01N2500/20
摘要： 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.
摘要翻译：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。

26. 发明申请

WO2002080883A3 METHOD AND COMPOSITION FOR SOLUBILISING A BIOLOGICALLY ACTIVE COMPOUND WITH LOW WATER SOLUBILITY 审中-公开
公开(公告)号：WO2002080883A3
公开(公告)日：2002-10-17
申请号：PCT/EP2002/003371
申请日：2002-03-26
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steven , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
发明人： LEIGH, Steven , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
IPC分类号： A61K9/127
摘要： Compositions for forming molecular associates with lipophilic compounds and an improved method of loading lipophilic biologically active compounds into previously formed, aqueous suspensions of lipid particles. A preferred embodiment for injection purposes comprise lipid particles having sizes below 1000 nm in diameter, in a vial or other suitable container are described. The method involves mixing a lipophilic compound either in solution or as an amorphous, preferably lyophilised powder in a first container with an aqueous suspension of lipid particles contained in a second container to form molecular associates. Only minimum agitation is required. The entire procedure may be carried out instantly in situ, in sealed sterile units just prior to use in the hospital ward or by the bedside.

27. 发明申请

WO1998025887A2 FORMULATIONS AND POLYMORPHIC FORMS OF DESFERRIOXAMINE AND THE PREPARATION THEREOF 审中-公开
标题翻译： DESFERRIOXAMINE的制剂和多形态及其制备方法
公开(公告)号：WO1998025887A2
公开(公告)日：1998-06-18
申请号：PCT/EP1997006849
申请日：1997-12-08
申请人： NOVARTIS AG , MARTI, Erwin , GEOFFROY, Andre, Joseph , HIRT, Hans , BURKHARD, Andreas , HASSAN, Ian, Francis , LOWTHER, Nicholas , NICKLIN, Joanne , STEWARD, Alan , VAN HOOGEVEST, Peter
发明人： NOVARTIS AG
IPC分类号： C07C259/00
CPC分类号： A61K31/16 , C07C259/06 , Y02A50/411
摘要： A parenterally injectable composition comprising particles of a desferrioxamine-B salt of an aliphatic sulphonic acid having at least 8 carbon atoms suspended in a parenterally administrable oil. New crystalline modifications of desferrioxamine B decanesulphonic salt are provided, and one crystal form with outstanding stability is disclosed.
摘要翻译：一种肠胃外可注射组合物，其包含悬浮在肠胃外给药的油中的具有至少8个碳原子的脂肪族磺酸的去铁胺B盐的颗粒。提供了去铁胺B癸烷磺酸盐的新的结晶改性，并且公开了一种具有突出稳定性的一种晶体形式。

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