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1. 发明申请

WO2010102065A1 PHARMACEUTICAL COMPOSITIONS OF DEXTRAN POLYMER DERIVATIVES 审中-公开
标题翻译： DEXTRAN聚合物衍生物的药物组合物
公开(公告)号：WO2010102065A1
公开(公告)日：2010-09-10
申请号：PCT/US2010/026127
申请日：2010-03-03
申请人： BEND RESEARCH, INC. , MILLER, Warren, K. , VODAK, David, T. , DOBRY, Daneil, E. , LYON, David, K. , FRIESEN, Dwayne, T. , MORGEN, Michael, M. , BLOOM, Corey, J. , SMITHEY, Daniel, T.
发明人： MILLER, Warren, K. , VODAK, David, T. , DOBRY, Daneil, E. , LYON, David, K. , FRIESEN, Dwayne, T. , MORGEN, Michael, M. , BLOOM, Corey, J. , SMITHEY, Daniel, T.
IPC分类号： A61K9/00 , A61K47/36
CPC分类号： A61K47/36 , A61K9/0019 , A61K9/0048 , A61K9/0075 , A61K9/0095 , A61K9/10 , A61K9/1652 , A61K9/19 , A61K9/5161 , A61K31/57
摘要： Pharmaceutical compositions are provided comprising an active agent and a dextran polymer derivative. The compositions include from 0.01 to 99 wt% of an active agent and from 1 to 99.99 wt% of a dextran polymer derivative. The dextran polymer derivative is selected from dextran acetate, dextran propionate, dextran succinate, dextran acetate propionate, dextran acetate succinate, dextran propionate succinate, dextran acetate propionate succinate, and mixtures thereof.
摘要翻译：提供包含活性剂和葡聚糖聚合物衍生物的药物组合物。组合物包含0.01至99重量％的活性剂和1至99.99重量％的葡聚糖聚合物衍生物。葡聚糖聚合物衍生物选自葡聚糖乙酸酯，葡聚糖丙酸酯，葡聚糖琥珀酸酯，乙酸葡聚糖丙酸酯，醋酸葡聚糖琥珀酸酯，琥珀酸葡聚糖葡聚糖，琥珀酸葡聚糖乙酸酯及其混合物。

2. 发明申请

WO2012122279A1 SOLID DISPERSION FORMULATIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：固体分散配方及其使用方法
公开(公告)号：WO2012122279A1
公开(公告)日：2012-09-13
申请号：PCT/US2012/028088
申请日：2012-03-07
申请人： ZALICUS PHARMACEUTICALS LTD. , PADVAL, Mahesh, V. , GAUTSCHI, Jeff, T. , SMITHEY, Daniel, T. , CREW, Marshall, D. , HARIANAWALA, Abizer
发明人： PADVAL, Mahesh, V. , GAUTSCHI, Jeff, T. , SMITHEY, Daniel, T. , CREW, Marshall, D. , HARIANAWALA, Abizer
IPC分类号： A61K31/54 , A01N43/58 , A61K31/50 , A61K31/4965
CPC分类号： A61K9/146 , A61K9/1635 , A61K9/1652 , A61K9/4858 , A61K9/4866 , A61K31/4965 , A61K31/50 , A61K31/54 , B29C47/0011
摘要： The present invention relates to formulations and methods for increasing the bioavailability of 1- (4-benzhydrylpiperazin-l-yl)-3,3-diphenylpropan-l-one, l-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion.
摘要翻译：本发明涉及增加1-（4-二苯甲基哌嗪-1-基）-3,3-二苯基丙-1-酮，1-（3,3-二苯基丙酰基）哌嗪或其盐的生物利用度的制剂和方法。特别地，制剂可以包括一种或多种药学上可接受的基质聚合物以形成固体分散体，例如喷雾干燥分散体或热熔体挤出。

3. 发明申请

WO2011057017A1 AQUEOUS NANOPARTICLE SUSPENSIONS FOR USE IN DRUG DISCOVERY 审中-公开
标题翻译：用于药物发现的水溶性纳米颗粒悬浮液
公开(公告)号：WO2011057017A1
公开(公告)日：2011-05-12
申请号：PCT/US2010/055513
申请日：2010-11-04
申请人： BEND RESEARCH, INC. , FRIESEN, Dwayne, T. , HAYDEN, Tanya, L. , BABCOCK, Walter, C. , CREW, Marshall, D. , SMITHEY, Daniel, T.
发明人： FRIESEN, Dwayne, T. , HAYDEN, Tanya, L. , BABCOCK, Walter, C. , CREW, Marshall, D. , SMITHEY, Daniel, T.
IPC分类号： G01N33/53 , G01N33/536
CPC分类号： B82Y15/00 , G01N33/54346 , G01N2500/04
摘要： Methods for evaluating potential active agents are disclosed. A feed stock including a potential active agent and an amphiphilic polymer in a water-miscible solvent is provided, the potential active agent and polymer each being poorly water soluble. The feed stock is combined with an aqueous solution to produce a suspension of nanoparticles that include the potential active agent and the polymer. A liquid-phase assay is performed with an aliquot of the suspension to determine a pre-selected property of the potential active agent. In some embodiments, the polymer is a substituted dextran, such as dextran acetate, dextran propionate, dextran butyrate, dextran isobutyrate, or a mixture thereof. In certain embodiments, the amphiphilic polymer is a functionalized oxidized dextran with at least one oxidized group and an alkyl ester substituent selected from acetate, propionate, butyrate, isobutyrate, and mixtures thereof. In some embodiments, the polymer is a substituted cellulosic.
摘要翻译：公开了评估潜在活性剂的方法。提供了在水混溶性溶剂中包含潜在的活性剂和两亲性聚合物的原料，潜在的活性剂和聚合物各自的水溶性差。原料与水溶液组合以产生包含潜在的活性剂和聚合物的纳米颗粒的悬浮液。用等分悬浮液进行液相测定以确定潜在活性剂的预先选择的性质。在一些实施方案中，聚合物是取代的葡聚糖，例如醋酸葡聚糖，丙酸葡聚糖，丁酸葡聚糖，异丁酸葡聚糖或其混合物。在某些实施方案中，两亲性聚合物是具有至少一个氧化基团和选自乙酸酯，丙酸酯，丁酸酯，异丁酸酯及其混合物的烷基酯取代基的官能化氧化葡聚糖。在一些实施方案中，聚合物是取代的纤维素。

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