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1. 发明申请

WO2002080883A2 METHOD AND COMPOSITION FOR SOLUBILISING A BIOLOGICALLY ACTIVE COMPOUND WITH LOW WATER SOLUBILITY 审中-公开
标题翻译：用于溶解具有低水溶性的生物活性化合物的方法和组合物
公开(公告)号：WO2002080883A2
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
CPC分类号： A61K9/1075 , A61K9/1278
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.
摘要翻译：用于与亲脂性化合物形成分子缔合物的组合物和将亲脂性生物活性化合物加载到先前形成的脂质颗粒水悬浮液中的改进方法。用于注射目的的优选实施方案包括直径小于1000nm，在小瓶或其它合适的容器中的脂质颗粒。该方法包括在第一容器中的溶液或无定形，优选冻干的粉末中混合亲脂性化合物与第二容器中含有的脂质颗粒的水性悬浮液以形成分子缔合物。只需要最小的搅动。整个程序可以在即将在医院病房或床边使用前的密封无菌单元中立即进行。

2. 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.

3. 发明申请

WO2003063835A1 COMPOSITION COMPRISING LOW WATER SOLUBLE COMPOUNDS WITHIN POROUS CARRIERS 审中-公开
标题翻译：在多孔载体中包含低水溶性化合物的组合物
公开(公告)号：WO2003063835A1
公开(公告)日：2003-08-07
申请号：PCT/EP2003/000847
申请日：2003-01-28
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus , QUINTON, Jacques
发明人： LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus , QUINTON, Jacques
IPC分类号： A61K9/18
CPC分类号： A61K9/1617 , A61K9/143 , A61K9/145 , A61K9/1611
摘要： The invention relates to compositions for improving the solubility or dispersibility of biologically active compounds having low water solubility in molecular association or in ultra fine form. The compositions comprise a biologically active compound having low water solubility in combination with a porous particulate support material capable of incorporating within its pores the biologically active compound.
摘要翻译：本发明涉及用于改善在分子缔合或超细形式中具有低水溶性的生物活性化合物的溶解度或分散性的组合物。组合物包含具有低水溶性的生物活性化合物与能够在其孔内引入生物活性化合物的多孔颗粒载体材料的组合。

4. 发明申请

WO2003010330A3 TEST SYSTEM AND METHOD SUITABLE FOR SELECTING TEST MATERIALS AND FORMULATIONS 审中-公开
公开(公告)号：WO2003010330A3
公开(公告)日：2003-02-06
申请号：PCT/EP2002/008215
申请日：2002-07-23
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： G01N33/50
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.

5. 发明申请

WO2003042392A1 STANDARDISED PHOSPHOLIPID MIXTURES 审中-公开
标题翻译：标准化磷酸盐混合物
公开(公告)号：WO2003042392A1
公开(公告)日：2003-05-22
申请号：PCT/EP2002/012817
申请日：2002-11-15
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： C12P7/62
CPC分类号： A23J7/00 , C11C3/12 , C12P7/6481 , C12P9/00 , C12P13/06
摘要： A standardised and optionally hydrogenated phospholipid composition comprising a phospholipase modified and the corresponding unmodified phospholipid and optionally other components obtainable by a method comprising: i) Modification of a phospholipid comprising at least 10% PC or 10% MAPC by enzyme treatment with phospholipase; ii) Purification of the enzyme modified mixture; iii) Addition of unmodified phospholipid with a minimum of 40% w/w PC or another diacylphospholipid to said enzyme modified and purified mixture to reach the desired target amount of the modified phospholipid. An enzyme modified composition comprising up to 85 wt % of mono acyl phosphatidylcho-line and 14 wt % of phosphatidylcholine before back blending is also described. The in-vention also describes a method of preparing said compositions.
摘要翻译：一种标准化和任选氢化的磷脂组合物，其包含修饰的磷脂酶和相应的未修饰的磷脂以及任选的其它可通过以下方法获得的组分：i）通过用磷脂酶酶处理来修饰包含至少10％PC或10％MAPC的磷脂; ii）酶改性混合物的纯化; iii）向所述酶修饰和纯化的混合物中加入至少40％w / w PC或另一种二酰基磷脂的未修饰磷脂，以达到所需目标量的修饰的磷脂。还描述了在回混之前包含高达85重量％的单酰基磷脂酰胆碱和14重量％的磷脂酰胆碱的酶修饰组合物。本发明还描述了制备所述组合物的方法。

6. 发明申请

WO2003023394A2 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：WO2003023394A2
公开(公告)日：2003-03-20
申请号：PCT/EP2002/010241
申请日：2002-09-12
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： G01N33/15
CPC分类号： G01N33/92

7. 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.

8. 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。

9. 发明申请

WO2004047554A1 MARINE LIPID COMPOSITIONS 审中-公开
标题翻译：海洋脂肪组合物
公开(公告)号：WO2004047554A1
公开(公告)日：2004-06-10
申请号：PCT/EP2003/013299
申请日：2003-11-26
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
发明人： LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
IPC分类号： A23K1/18
CPC分类号： A23D9/013 , A23J7/00 , A23K20/147 , A23K40/10 , A23K40/30 , A23K50/80 , A23L33/115 , A23L33/12 , A23L33/17 , A23V2002/00 , C11B1/10 , C11B1/104 , Y02A40/818 , A23V2200/224 , A23V2250/192 , A23V2250/182 , A23V2250/05 , A23V2250/1842
摘要： There is described marine phospholipids (MPL) compositions suitable for human, aquaculture applications comprising a dry composition comprising nutritional components selected from the group consisting of marine phospholipids, marine proteins and amino acid blends obtainable by fluid extraction of a dried marine raw material. The compositions have low amounts of neutral lipids and particularly low amounts of cholesterol and cholesterol esters. They may be used either as such in powder form and for preparing purified MPL compositions by ethanol extraction. Both forms may be used as nutritional supplements, ingredients for functional foods and to optimise the delivery and containment of nutritional components in multicomponent fish feed compositions. There is further described a blend of the purified, ethanol extracted MPL compositions mixed with marine, vegetable, microbial or MCT oils to form liquid preparations for hard or soft gel encapsulation. There is further described MPL concentrates comprising purified and clearly defined phospholipid types dispersed in hydrophilic medium which are nutritionally essential in larvae feed. Still further there is described MPL compositions in unit dosage forms as supplements to supply highly bioavailable omega-3 fatty acids for human use, optionally with biologically active compounds.
摘要翻译：描述了适用于人，水产养殖应用的海洋磷脂（MPL）组合物，其包含干组合物，其包含选自海洋磷脂，海洋蛋白质和通过干燥的海洋原料的流体萃取获得的氨基酸混合物的营养成分。组合物具有低量的中性脂质，特别是低量的胆固醇和胆固醇酯。它们可以以粉末形式使用，也可以通过乙醇提取制备纯化的MPL组合物。两种形式可以用作营养补充剂，功能食品的成分，并优化多组分鱼饲料组合物中营养成分的输送和遏制。进一步描述了与海洋，植物，微生物或MCT油混合的纯化的乙醇提取的MPL组合物的混合物，以形成用于硬或软凝胶包封的液体制剂。进一步描述了MPL浓缩物，其包含分散在亲水介质中的纯化和明确定义的磷脂类型，其在幼虫饲料中是营养必需的。此外，还描述了单位剂型中的MPL组合物作为补充剂，为人类提供高度生物可利用的ω-3脂肪酸，任选地具有生物活性化合物。

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