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1. 发明申请

WO2004075872A1 AMBIPHILIC POROUS MATRIX 审中-公开
标题翻译：辅助多孔矩阵
公开(公告)号：WO2004075872A1
公开(公告)日：2004-09-10
申请号：PCT/EP2004/001985
申请日：2004-02-27
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Mathew, Louis, Steven , LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter
发明人： LEIGH, Mathew, Louis, Steven , LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter
IPC分类号： A61K7/48
CPC分类号： A61K8/0279 , A61K8/24 , A61K8/26 , A61K8/553 , A61K8/731 , A61K8/922 , A61K2800/56 , A61Q1/02 , A61Q1/06 , A61Q1/08 , A61Q1/10 , A61Q19/00
摘要： Compositions are described which are capable of forming external reservoirs comprising a polymeric matrix for adsorbing sebum in exchange for beneficial oils and transfer of hydrating components to the skin. The compositions may be lotions, creams, gels, pastes, lip sticks and water in oil systems. There is also described a method of preparing said lotions, creams, etc containing an ambiphilic powder mixture or complex comprising synthetic porous agglomerates, a lipophilic component, hydrophilic attractant/polymer, optionally biologically active compound and excipients.
摘要翻译：描述了能够形成外部储存器的组合物，其包含用于吸收皮脂的聚合物基质，以换取有益的油并将保湿组分转移至皮肤。组合物可以是乳液，乳膏，凝胶，糊剂，唇膏和油中的水。还描述了一种制备含有含有合成多孔团聚物，亲脂性成分，亲水性引诱剂/聚合物，任选的生物活性化合物和赋形剂的两性粉末混合物或复合物的所述洗剂，霜剂等的方法。

2. 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.

3. 发明申请

WO2004071494A2 LIPOPHILIC COMPOSITIONS 审中-公开
标题翻译：脂肪组合物
公开(公告)号：WO2004071494A2
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001355
申请日：2004-02-13
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , 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： A61K9/16
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：描述了包含与低粘度等级的水不溶性聚合物相关的亲脂性化合物和任选的作为单分子或无定形络合物缔合的亲水剂的干组合物。还描述了使用水可混溶或不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。通过用水稀释，从包含水混溶性溶剂的溶液中沉淀亲脂性聚合物络合物，分离出沉淀的复合物，洗涤，干燥和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制备，包括喷雾干燥或在高温下使用水混溶或水不混溶的溶剂进行真空干燥。组合物的特征在于相关化合物在水性介质中的溶解和溶解度的改善。

4. 发明申请

WO2004037216A1 MICRODISPERSION AND METHOD OF PRODUCING SAME 审中-公开
标题翻译：微生物及其生产方法
公开(公告)号：WO2004037216A1
公开(公告)日：2004-05-06
申请号：PCT/EP2003/011936
申请日：2003-10-28
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Mathew, Louis, Steven , LEIGH, Steve , VAN HOOGEVEST, Peter , KUNG, Elsa
发明人： LEIGH, Mathew, Louis, Steven , LEIGH, Steve , VAN HOOGEVEST, Peter , KUNG, Elsa
IPC分类号： A61K7/00
CPC分类号： A61K8/06 , A61K8/345 , A61K8/37 , A61K8/375 , A61K8/553 , A61K2800/21 , A61Q19/00 , A61Q19/08
摘要： The invention describes homogeneous microdispersions comprising at least one hydrogenated or partially hydrogenated membrane lipid with or without enzyme hydrolysis, dispersed in substantially non aqueous, non volatile hydrophilic medium with boiling point above 40°C. More preferably the compositions comprise a mixture of hydrogenated monoacyl and hydrogenated diacyl lipids and at least one oil. The phospholipid mixture is obtained by controlled enzyme hydrolysis of lecithin or a specific phospholipid, followed by hydrogenation. The compositions have improved rheology, physical and chemical properties, functionality and industrial applicability. The microdispersions are used as such in all types of applications and as functional components with active compounds in products, particularly for improving skin function and facilitating skin repair due to UV damage and aging, in cosmetics and other topical products.
摘要翻译：本发明描述了均匀的微分散体，其包含至少一种具有或不具有酶水解的氢化或部分氢化的膜脂质，分散在沸点高于40℃的基本上非水性的非挥发性亲水介质中。更优选地，组合物包含氢化单酰基和氢化二酰基脂质与至少一种油的混合物。磷脂混合物通过卵磷脂或特定磷脂的受控酶水解，然后氢化而获得。组合物具有改善的流变性，物理和化学性质，功能性和工业适用性。微分散体在所有类型的应用中都是这样使用的，并且作为在产品中具有活性化合物的功能组分，特别是用于改善皮肤功能并促进由于紫外线损伤和老化引起的皮肤修复，在化妆品和其它局部产品中。

5. 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。

6. 发明申请

WO2007020057A1 CRYSTAL FORMS OF ASTAXANTHIN 审中-公开
标题翻译：阿司匹林的晶体形式
公开(公告)号：WO2007020057A1
公开(公告)日：2007-02-22
申请号：PCT/EP2006/008047
申请日：2006-08-15
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , LEIGH, Steve
发明人： LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , LEIGH, Steve
IPC分类号： C07C49/653 , A23L1/275
CPC分类号： C07C403/24
摘要： This invention describes previously undisclosed mixtures of specific crystal forms of astaxanthin and the individual crystal forms designated crystal Form I and II together with methods for preparing said crystal Forms. Methods for preparing nutritional dosage forms comprising said novel astaxanthin crystal forms for the life science industry are also disclosed.
摘要翻译：本发明描述了以前未公开的虾青素的特定晶体形式的混合物，以及指定为晶型I和II的单独结晶形式以及制备所述晶形的方法。还公开了包含用于生命科学工业的所述新型虾青素晶体形式的营养剂型的方法。

7. 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。

8. 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

9. 发明申请

WO2007054342A1 DISSOLUTION COMPOSITION FOR EXAMINING DRUG SOLUBILITY 审中-公开
标题翻译：用于检查药物溶解性的溶解组合物
公开(公告)号：WO2007054342A1
公开(公告)日：2007-05-18
申请号：PCT/EP2006/010809
申请日：2006-11-10
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , STREICH, Daniel , QUINTON, Jacques
发明人： LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , STREICH, Daniel , QUINTON, Jacques
IPC分类号： G01N33/15
CPC分类号： G01N33/15 , Y10S514/937 , Y10S514/943
摘要： There are described solid compositions or examining drug solubility comprising bile salts and phospholipids, optionally containing buffer components suitable for preparation of intestinal media that simulate the composition of the intestinal fluids in fasted and fed states.
摘要翻译：描述了固体组合物或检查药物溶解度，其包含胆汁盐和磷脂，任选地含有适于制备肠培养基的缓冲组分，其模拟禁食和进食状态下肠液的组成。

10. 发明申请

WO2005110360A2 COMPOSITIONS FOR INJECTION 审中-公开
标题翻译：注射用组合物
公开(公告)号：WO2005110360A2
公开(公告)日：2005-11-24
申请号：PCT/EP2005/005365
申请日：2005-05-17
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter
发明人： LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter
IPC分类号： A61K9/00
CPC分类号： A61K9/0024 , A61K9/0019 , A61K9/1274 , A61K47/06 , A61K47/24
摘要： The present invention relates to a homogeneous pharmaceutical composition for the gradual release of biologically active compounds after intramuscular or subcutaneous administration comprising at least one membrane lipid which is in the liquid crystalline state and a process for the preparation of said composition.
摘要翻译：本发明涉及用于在肌内或皮下给药后逐渐释放生物活性化合物的均匀药物组合物，其包含至少一种处于液晶状态的膜脂质和制备所述组合物的方法。

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