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1. 发明申请

WO1991019483A1 COMPOSITIONS AND METHODS FOR THE CONTROLLED RELEASE OF SOLUBLE ACTIVE SUBSTANCES 审中-公开
标题翻译：用于控制释放可溶性活性物质的组合物和方法
公开(公告)号：WO1991019483A1
公开(公告)日：1991-12-26
申请号：PCT/US1991004313
申请日：1991-06-17
申请人： ADVANCED POLYMER SYSTEMS, INC.
发明人： ADVANCED POLYMER SYSTEMS, INC. , EURY, Robert, P. , PATEL, Rajesh
IPC分类号： A61K09/14
CPC分类号： A61K9/1635 , Y10S514/951
摘要： A composition for the controlled release of an active substance comprises a polymeric particle matrix, where each particle defines a network of internal pores. The active substance is entrapped within the pore network together with a blocking agent having physical and chemical characteristics selected to modify the release rate of the active substance from the internal pore network. In an exemplary embodiment, drugs may be selectively delivered to the intestines using an enteric material as the blocking agent. The enteric material remains intact in the stomach but will degrade under the pH conditions of the intestines. In another exemplary embodiment, the sustained release formulation employs a blocking agent which remains stable under the expected conditions of the environment to which the active substance is to be released.
摘要翻译：用于控制释放活性物质的组合物包括聚合物颗粒基质，其中每个颗粒限定内部孔的网络。活性物质与具有选择的物理和化学特性的封闭剂一起截留在孔网内，以改变活性物质从内部孔网络的释放速率。在一个示例性实施方案中，药物可以使用肠溶材料作为阻断剂选择性递送至肠。肠道物质在胃中保持完整，但在肠的pH条件下会降解。在另一个示例性实施方案中，持续释放制剂采用封闭剂，其在待释放活性物质的环境的预期条件下保持稳定。

2. 发明申请

WO1992018222A1 PREPARATION AND USE OF SOLID BEADS HAVING CONTROLLED CHARACTERISTICS 审中-公开
标题翻译：具有控制特性的固体珠的制备和使用
公开(公告)号：WO1992018222A1
公开(公告)日：1992-10-29
申请号：PCT/US1992003212
申请日：1992-04-20
申请人： ADVANCED POLYMER SYSTEMS, INC.
发明人： ADVANCED POLYMER SYSTEMS, INC. , LIAU, Christine, J., Y. , PAPACOSTA, Kemon, John , MAZAS, Constantin , EURY, Robert, P. , NACHT, Sergio
IPC分类号： B01D33/15
CPC分类号： A61M1/3693 , C08F2/22 , G01N33/5094
摘要： Processes for preparing and using controlled characteristic beads are disclosed, the process of making the beads including the steps combining at least one monoethylenically unsaturated monomer with a polyethylenically unsaturated monomer and a monomer-soluble initiator to form a monomer phase; combining the monomer phase with a liquid in which the monomer phase is substantially immiscible to form a reaction mixture such that when the monomer phase is vinyl in nature the liquid also includes a high molecular weight, high charge density surfactant, and when the monomer phase is acrylic in nature the liquid includes an organic polymer colloid suspending agent; agitating the reaction mixture at an initial speed and temperature for a time sufficient to homogenize the reaction mixture, thereby producing first intermediate droplets, and subsequently reducing the agitation speed to a level sufficient to allow limited coalescence of the first intermediate droplets to form second intermediate droplets having size distribution with less than about 30 % variance from the mean; and polymerizing the second intermediate droplets to form solid, substantially non-porous beads. One method of using controlled characteristic beads includes combining the beads produced by the process with a sample containing two separable components and centrifuging the sample for a time and at a rate sufficient to produce distinct bands of components.
摘要翻译：公开了制备和使用受控特征珠粒的方法，制备珠粒的方法包括将至少一种单烯属不饱和单体与单体可溶性引发剂结合以形成单体相的步骤; 将单体相与其中单体相基本上不混溶以形成反应混合物的液体组合，使得当本质上单体相是乙烯基时，液体还包括高分子量，高电荷密度的表面活性剂，并且当单体相是丙烯酸性质的液体包括有机聚合物胶体悬浮剂; 在初始速度和温度下搅拌反应混合物足以使反应混合物均匀化的时间，从而产生第一中间液滴，随后将搅拌速度降低至足以允许第一中间液滴的有限聚结形成第二中间液滴其尺寸分布与平均值小于约30％的差异; 并聚合第二中间液滴以形成固体，基本上无孔的珠粒。使用受控特征珠的一种方法包括将通过该方法产生的珠粒与含有两种可分离组分的样品组合并将样品离心一段时间并以足以产生不同组分带的速率离心。

3. 发明申请

WO1993007862A1 IONIC BEADS USEFUL FOR CONTROLLED RELEASE AND ADSORPTION 审中-公开
标题翻译：离子珠可用于控制释放和吸附
公开(公告)号：WO1993007862A1
公开(公告)日：1993-04-29
申请号：PCT/US1992008907
申请日：1992-10-19
申请人： ADVANCED POLYMER SYSTEMS, INC.
发明人： ADVANCED POLYMER SYSTEMS, INC. , NACHT, Sergio , WON, Richard , KATZ, Martin, A. , CHENG, Tai , LIAU, Christine, J., Y. , EURY, Robert, P. , FROIX, Michael
IPC分类号： A61K09/52
CPC分类号： A61K8/817 , A61K8/0279 , A61K8/8152 , A61K9/1635 , A61K47/585 , A61K2800/54 , A61K2800/546 , A61K2800/56 , A61K2800/654 , A61Q17/04 , A61Q19/00
摘要： Ionic compositions comprise an active ingredient absorbed within a network of internal pores defined by a plurality of polymeric particles. The particles are preferably crosslinked polymeric beads having a diameter in the range from about 5 to 100 microns and a surface charge density from about 0.1 to 10 meq/qm hydrogen ion capacity. The active ingredients are released from the ionic polymer beads over time when orally administered, applied to a keratinic material, typically human skin or hair or otherwise delivered to a target environment. The use of a cationic charge promotes adhesion of the beads to the keratinic material.
摘要翻译：离子组合物包含吸收在由多个聚合物颗粒限定的内部孔的网络内的活性成分。颗粒优选为直径在约5至100微米范围内且表面电荷密度为约0.1至10meq / qm氢离子容量的交联聚合物珠粒。当口服施用时，活性成分随着时间的推移从离子聚合物珠粒释放，施用于角质材料，通常为人皮肤或毛发，或以其它方式递送至目标环境。使用阳离子电荷促进珠子与角蛋白材料的粘附。

4. 发明申请

WO1991004732A1 ERODIBLE MACROPOROUS HYDROGEL PARTICLES AND PREPARATION THEREOF 审中-公开
标题翻译：无机大孔水合物颗粒及其制备方法
公开(公告)号：WO1991004732A1
公开(公告)日：1991-04-18
申请号：PCT/US1990005564
申请日：1990-09-28
申请人： ADVANCED POLYMER SYSTEMS, INC.
发明人： ADVANCED POLYMER SYSTEMS, INC. , EURY, Robert, P.
IPC分类号： A61K09/16
CPC分类号： A61K9/1635
摘要： The present invention provides for a polymeric delivery system for delivery of a variety of active substances to an aqueous environment. More particularly, it is directed to a delivery system comprising erodible hydrogel particles containing a substantially continuous network of pores and an impregnant comprising an active agent. According to the invention, the active agent is introduced into the pore network of the hydrogel particles after the particles have been prepared.
摘要翻译：本发明提供了用于将各种活性物质递送到水性环境的聚合物递送系统。更具体地，涉及包含含有基本上连续网孔的可侵蚀的水凝胶颗粒和包含活性剂的浸渍剂的递送系统。根据本发明，在制备颗粒之后，将活性剂引入水凝胶颗粒的孔网络中。

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