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1. 发明申请

WO2005084639A9 POLYMERIC DRUG DELIVERY SYSTEM FOR HYDROPHOBIC DRUGS 审中-公开
标题翻译：用于疏水性药物的聚合物药物递送系统
公开(公告)号：WO2005084639A9
公开(公告)日：2005-11-17
申请号：PCT/US2005007525
申请日：2005-03-03
申请人： SPHERICS INC , JACOB JULES S , BASSETT MICHAEL , SCHESTOPOL MARCUS A , MATHIOWITZ EDITH , NANGIA AVINASH , CARTER BENNETT , MOSLEMY PEYMAN , SHAKED ZE EV , ENSCORE DAVID , SIKES COURTNEY
发明人： JACOB JULES S , BASSETT MICHAEL , SCHESTOPOL MARCUS A , MATHIOWITZ EDITH , NANGIA AVINASH , CARTER BENNETT , MOSLEMY PEYMAN , SHAKED ZE EV , ENSCORE DAVID , SIKES COURTNEY
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/24 , A61K9/28 , A61K9/48
CPC分类号： A61K9/209 , A61K9/0065 , A61K9/1635 , A61K9/1641 , A61K9/1647 , A61K9/1652 , A61K9/1676 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K9/2853
摘要： An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.
摘要翻译：本文公开了由于不溶于水而具有低口服生物利用度和缓慢溶出动力学的II类药物的口服递送系统以及制备这种药物递送系统的方法。该制剂可以是控释或速释制剂。速释制剂含有II类药物以及疏水聚合物，优选生物粘附聚合物。在一个实施方案中，药物和聚合物共溶于普通溶剂中。通过任何方便的方法，特别是通过喷雾干燥，溶液形成小的固体颗粒。所得颗粒含有作为小颗粒分散在聚合物基质中的药物。颗粒对于聚集是稳定的，并且可以放入胶囊或制成片剂给药。控释制剂含有BCS II类药物和生物粘附聚合物。控释制剂可以是片剂，胶囊剂，小片，微粒或渗透泵的形式。（1）由于药物的稳定微粉化，溶解动力学增加，（2）药物从胃肠道中的聚合物中快速释放，因此通过使用生物粘附聚合物增强药物的口服摄取。和（3）由于聚合物的生物粘附性而延长的GI运输。这些效果的组合允许制备适用于许多II类药物口服给药的紧凑稳定剂型。

2. 发明申请

WO2005032511A3 NANOPARTICULATE THERAPEUTIC BIOLOGICALLY ACTIVE AGENTS 审中-公开
标题翻译： NANOPARTICULATE治疗生物活性剂
公开(公告)号：WO2005032511A3
公开(公告)日：2005-05-19
申请号：PCT/US2004032271
申请日：2004-09-30
申请人： SPHERICS INC , UNIV BROWN RES FOUND , JACOB JULES S , JONG YONG S , ABRAMSON DANIELLE T , MATHIOWITZ EDITH , SANTOS CAMILLA A , BASSETT MICHAEL J , FURTADO STACIA
发明人： JACOB JULES S , JONG YONG S , ABRAMSON DANIELLE T , MATHIOWITZ EDITH , SANTOS CAMILLA A , BASSETT MICHAEL J , FURTADO STACIA
IPC分类号： A61K9/14 , A61K9/16 , A61K9/50 , A61K9/51 , A61K38/27 , A61K38/28 , A61K48/00
CPC分类号： A61K38/208 , A61K9/14 , A61K9/146 , A61K9/1688 , A61K9/5026 , A61K9/5031 , A61K9/5089 , A61K31/7105 , A61K38/168 , A61K38/27 , A61K38/28
摘要： Compositions containing particles of biologically active agents with sizes in the micron and submicron range and methods for making and using such particles are described herein. In the preferred embodiment the biologically active agents are peptides, proteins, nucleic acid molecules, or hydrophilic synthetic molecules. The particles have a size ranging from an average diameter of about 100 nm to about 2000 nm, preferably about 200 nm to 600 nm. Optionally the biologically active agents contain a polymeric coating. The particles are formed by adding a biologically active agent to an aqueous solution, mixing a nonsolvent that is miscible with water with the aqueous solution, and precipitating particles of the biologically active agents out of the nonsolvent: aqueous solution combination. The nonsolvent is typically a C1 to C6 alcohol, preferably a C2 to a C5 alcohol. In the preferred embodiment, the nonsolvent is tert-butyl alcohol.
摘要翻译：本文描述了含有尺寸在微米和亚微米范围内的生物活性剂颗粒的组合物以及制备和使用这些颗粒的方法。在优选的实施方案中，生物活性剂是肽，蛋白质，核酸分子或亲水合成分子。颗粒的尺寸范围为约100nm至约2000nm的平均直径，优选为约200nm至600nm。任选地，生物活性剂含有聚合物涂层。通过向水溶液中加入生物活性剂，将可与水混溶的非溶剂与水溶液混合并将生物活性剂的颗粒从非溶剂：水溶液组合中沉淀而形成颗粒。非溶剂通常是C1至C6醇，优选C2至C5醇。在优选的实施方案中，非溶剂是叔丁醇。

3. 发明申请

WO2005032511A2 NANOPARTICULATE THERAPEUTIC BIOLOGICALLY ACTIVE AGENTS 审中-公开
标题翻译：纳米颗粒治疗生物活性剂
公开(公告)号：WO2005032511A2
公开(公告)日：2005-04-14
申请号：PCT/US2004/032271
申请日：2004-09-30
申请人： SPHERICS, INC. , BROWN UNIVERSITY RESEARCH FOUNDATION , JACOB, Jules, S. , JONG, Yong, S. , ABRAMSON, Danielle, T. , MATHIOWITZ, Edith , SANTOS, Camilla, A. , BASSETT, Michael, J. , FURTADO, Stacia
发明人： JACOB, Jules, S. , JONG, Yong, S. , ABRAMSON, Danielle, T. , MATHIOWITZ, Edith , SANTOS, Camilla, A. , BASSETT, Michael, J. , FURTADO, Stacia
IPC分类号： A61K9/00
CPC分类号： A61K38/208 , A61K9/14 , A61K9/146 , A61K9/1688 , A61K9/5026 , A61K9/5031 , A61K9/5089 , A61K31/7105 , A61K38/168 , A61K38/27 , A61K38/28
摘要： Compositions containing particles of biologically active agents with sizes in the micron and submicron range and methods for making and using such particles are described herein. In the preferred embodiment the biologically active agents are peptides, proteins, nucleic acid molecules, or hydrophilic synthetic molecules. The particles have a size ranging from an average diameter of about 100 nm to about 2000 nm, preferably about 200 nm to 600 nm. Optionally the biologically active agents contain a polymeric coating. The particles are formed by adding a biologically active agent to an aqueous solution, mixing a nonsolvent that is miscible with water with the aqueous solution, and precipitating particles of the biologically active agents out of the nonsolvent: aqueous solution combination. The nonsolvent is typically a C1 to C6 alcohol, preferably a C2 to a C5 alcohol. In the preferred embodiment, the nonsolvent is tert -butyl alcohol.
摘要翻译：本文描述了包含具有微米和亚微米范围尺寸的生物活性剂颗粒的组合物以及制备和使用此类颗粒的方法。在优选的实施方案中，生物活性剂是肽，蛋白质，核酸分子或亲水性合成分子。颗粒具有范围从约100nm至约2000nm的平均直径，优选约200nm至600nm的尺寸。任选地，生物活性剂含有聚合物涂层。通过将生物活性剂加入到水溶液中，将与水混溶的非溶剂与水溶液混合，并将生物活性剂的颗粒从非溶剂：水溶液组合物中沉淀出来而形成颗粒。非溶剂通常是C1至C6醇，优选C2至C5醇。在优选的实施方案中，非溶剂是叔丁醇。

4. 发明申请

WO2003051304A3 BIOADHESIVE DRUG DELIVERY SYSTEM WITH ENHANCED GASTRIC RETENTION 审中-公开
公开(公告)号：WO2003051304A3
公开(公告)日：2003-06-26
申请号：PCT/US2002/040025
申请日：2002-12-13
申请人： SPHERICS, INC. , JACOB, Jules , MATHIOWITZ, Edith , ENSCORE, David , SCHESTOPOL, Marcus
发明人： JACOB, Jules , MATHIOWITZ, Edith , ENSCORE, David , SCHESTOPOL, Marcus
IPC分类号： A61K9/48
摘要： Bioadhesive macrosphere delivery systems ("BDDS") having prolonged gastric retention time due to bioadhesion rather than physical density or size are described. In general, the macrospheres have diameters that are greater than 200 microns, more preferably greater than 500 microns. The bioadhesive macrospheres are released in the stomach where they reside in close proximity to the gastric mucosa for a prolonged period of time. Increased residence of BDDS in the upper GI can lead to increased systemic absorption of drug in the preferred site of systemic absorption, namely the upper GI tract (upper to mid-jejunum). The BDDS may be engineered either as a capsule with drug delivery controlled by a diffusion-limited membrane or degradable shell, or as a solid matrix system with drug delivery controlled by a combination of diffusion and polymer degradation kinetics.

5. 发明申请

WO2013025442A2 CONCENTRATED FELBAMATE FORMULATIONS FOR PARENTERAL ADMINISTRATION 审中-公开
标题翻译：用于肠胃外给药的浓缩的佛氨酸盐制剂
公开(公告)号：WO2013025442A2
公开(公告)日：2013-02-21
申请号：PCT/US2012/050148
申请日：2012-08-09
申请人： PEROSPHERE INC. , BAKHRU, Sasha, H. , LAULICHT, Bryan, E. , MATHIOWITZ, Edith , STEINER, Solomon, S.
发明人： BAKHRU, Sasha, H. , LAULICHT, Bryan, E. , MATHIOWITZ, Edith , STEINER, Solomon, S.
IPC分类号： A61K31/55 , A61K31/27 , A61K9/16 , A61K9/14 , A61P25/00
CPC分类号： A61K31/27 , A61K9/0019 , A61K9/08 , A61K9/10 , A61K9/145 , A61K31/55 , A61K47/10 , A61K47/20
摘要： Formulations of a neuroprotective agent for parenteral administration are described herein. The formulation is in the form of a concentrated (supersaturated) solution or a concentrated suspension of microparticles. The suspension medium or the solution solvent carrier may also contain dissolved neuroprotective agent. For the supersaturated solutions, the agent is dissolved at high concentrations of at least about 1% by weight, 5% by weight, 10% by weight, 15% by weight, or 20% by weight in a solvent suitable for parenteral administration. For the concentrated suspension, the microparticles have an effective particle size from about 100 nm to about 5 microns, preferably from about 50 nm to about 3 microns, more preferably from about 10 nm to about 2 microns. The formulations described herein can be used to treat a variety of neurological diseases/disorders and/or neurological injury or trauma.
摘要翻译：本文描述了用于肠胃外给药的神经保护剂的制剂。该制剂为浓缩（过饱和）溶液或微粒浓缩悬浮液的形式。悬浮介质或溶液溶剂载体也可含有溶解的神经保护剂。对于过饱和溶液，试剂以适合非肠道给药的溶剂中以至少约1重量％，5重量％，10重量％，15重量％或20重量％的高浓度溶解。对于浓缩悬浮液，微粒具有约100nm至约5微米，优选约50nm至约3微米，更优选约10nm至约2微米的有效粒度。本文所述的制剂可用于治疗多种神经疾病/病症和/或神经损伤或创伤。

6. 发明申请

WO2008054874A9 PARTICLES WITH HIGH UNIFORM LOADING OF NANOPARTICLES AND METHODS OF PREPARATION THEREOF 审中-公开
标题翻译：高度均匀负载纳米颗粒的颗粒及其制备方法
公开(公告)号：WO2008054874A9
公开(公告)日：2008-06-12
申请号：PCT/US2007068881
申请日：2007-05-14
申请人： UNIV BROWN , FREEDOM 2 INC , MATHIOWITZ EDITH , KUNDAKOVIC LJILJANA , MORELLO ARTHUR PETER , HARRISON MICHAEL W , REINEKE JOSHUA JAMES
发明人： MATHIOWITZ EDITH , KUNDAKOVIC LJILJANA , MORELLO ARTHUR PETER , HARRISON MICHAEL W , REINEKE JOSHUA JAMES
IPC分类号： A61K9/14
CPC分类号： A61K9/1694 , A61K8/11 , A61K49/0021 , A61K49/0034 , A61K49/0036 , A61K49/0091 , A61K49/0093 , A61K2800/412 , A61Q1/02 , A61Q19/00 , C09C1/00
摘要： Methods to produce polymeric microparticles containing nanoparticles such, as pigments, dyes and other chromophores for cosmetic use, plastic surgery therapeutic use, and tattoos have been developed. The microparticles contain within the polymer a very uniform dispersion of dye particles. The methods by which the particles are made ensure a homogeneous mixture and high loading. The microparticles are made using air, one of a number of known methods such as phase inversion, solvent evaporation, and melt processing. The improvement is in the use of a method that makes, a stable dispersion of the nanoparticles in the liquid polymer before formation of the microparticles. This is achieved through selection of appropriate solvent, optionally including surfactant, and then subjecting the dispersion to mechanical processing that stabilizes the dispersion within the polymer solvent, so that the nanoparticles remain suspended for at least thirty minutes, in some cases two hours to 48 hours, sometimes up to three months. The mechanical processing can be sonication and/or production of shear forces, for examples, resulting from use of an open blade or rotor stator mixer or milling with a concentric shaft, at a speed such as between 5000 and 25,000 RPM.
摘要翻译：已经开发了生产含纳米颗粒的聚合物微粒的方法，例如用于化妆用途的颜料，染料和其他发色团，整形手术治疗用途和纹身。微粒在聚合物内含有非常均匀的染料颗粒分散体。制造颗粒的方法确保均匀混合物和高负载。使用空气制备微粒，这是许多已知方法中的一种，例如相转化，溶剂蒸发和熔融加工。改进在于使用在形成微粒之前使纳米颗粒在液体聚合物中稳定分散的方法。这通过选择合适的溶剂（任选地包括表面活性剂），然后使分散体经受机械处理来实现，所述机械处理稳定了聚合物溶剂中的分散体，使得纳米颗粒保持悬浮至少三十分钟，在一些情况下两小时至48小时有时长达三个月。机械加工可以是超声波处理和/或剪切力的产生，例如，由于使用开式叶片或转子定子混合器或者以同心轴进行铣削，速度例如在5000-25,000RPM之间。

7. 发明申请

WO2007024429A3 CELLULAR OR ORGANELLE-ENTRAPPED NANOPARTICLES 审中-公开
公开(公告)号：WO2007024429A3
公开(公告)日：2007-03-01
申请号：PCT/US2006/030037
申请日：2006-08-02
申请人： FREEDOM-2, LLC , KUNDAKOVIC, Ljiljana , KLITZMAN, Bruce , KOGER, Kim, Edward , MATHIOWITZ, Edith , DRILL, Craig, A.
发明人： KUNDAKOVIC, Ljiljana , KLITZMAN, Bruce , KOGER, Kim, Edward , MATHIOWITZ, Edith , DRILL, Craig, A.
IPC分类号： G01N33/574 , B43K5/00 , C09D11/00
摘要： The invention provides tissue marking pigment or dye particle retained within a tissue cell, the cellular cytoplasm, or one or more intracellular organelles. Also, the invention provides nanoparticles, which are phagocytosed, engulfed or otherwise entrapped by cells.

8. 发明申请

WO2006031420A2 MULTI-LAYER TABLETS AND BIOADHESIVE DOSAGE FORMS 审中-公开
标题翻译：多层片剂和全身用药剂型
公开(公告)号：WO2006031420A2
公开(公告)日：2006-03-23
申请号：PCT/US2005030651
申请日：2005-08-29
申请人： SPHERICS INC , NANGIA AVINASH , JACOB JULES , MATHIOWITZ EDITH , RICKETTS THOMAS L , KREITZ MARK R
发明人： NANGIA AVINASH , JACOB JULES , MATHIOWITZ EDITH , RICKETTS THOMAS L , KREITZ MARK R
IPC分类号： A61K9/28
CPC分类号： A61K9/209 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2086
摘要： Bioadhesives coatings increase the gastrointestinal retention time of orally-ingested medicaments. Certain bioadhesive coatings producing a fracture strength of at least 100 N/m 2 , as measured on rat intestine, when applied to at least one surface of a pharmaceutical dosage form for oral delivery of a drug, result in a gastrointestinal retention time of at least 4 hours in a fed beagle dog model, during which the drug is released from the dosage form. Multi-layer tablets, particularly those including hydrophobic excipients, are useful in administering hygroscopic and/or deliquescent drugs. In addition, varying the amount of drug in multi-layer tablets allows the release rate of the drug to be controlled.
摘要翻译：生物粘附剂涂层增加口服药物的胃肠道停留时间。当在大鼠肠道上测量时，产生至少100N / m 2的断裂强度的某些生物粘附涂层在应用于用于口服递送药物的药物剂型的至少一个表面时导致在喂养比格犬模型中至少4小时的胃肠道停留时间，在此期间药物从剂型释放。多层片剂，特别是那些包括疏水性赋形剂的片剂可用于施用吸湿性和/或潮解性药物。另外，改变多层片剂中药物的量可以控制药物的释放速率。

9. 发明申请

WO2006026592A2 ORAL ADMINISTRATION OF POORLY ABSORBED DRUGS, METHODS AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：口服吸收性药物的口服给药，方法和组合物
公开(公告)号：WO2006026592A2
公开(公告)日：2006-03-09
申请号：PCT/US2005/030774
申请日：2005-08-29
申请人： SPHERICS, INC. , MATHIOWITZ, Edith , NANGIA, Avinash , JACOB, Jules S. , KREITZ, Mark R. , DOANE, Rebecca , DONNELLY, Ryan
发明人： MATHIOWITZ, Edith , NANGIA, Avinash , JACOB, Jules S. , KREITZ, Mark R. , DOANE, Rebecca , DONNELLY, Ryan
IPC分类号： A61K9/51
CPC分类号： A61K9/0095 , A61K9/5138 , A61K9/5146 , A61K9/5161 , A61K9/5192
摘要： The invention provides methods and compositions for the delivery of poorly absorbed drugs. In some embodiments, the drug is administered in the form of microparticles or nanoparticles. In other embodiments, the drug is encapsulated with polymer. In certain embodiments, the drug is administered in combination with an absorption enhancer. The invention further relates to dosing schedules to maintain the oral bioavailability of poorly absorbed drugs, such as paclitaxel. In another embodiment, the method involves administering inhibitors of one or more inhibitors of a drug efflux pump in combination with a poorly absorbed drug.
摘要翻译：本发明提供了用于输送吸收不良的药物的方法和组合物。在一些实施方案中，药物以微粒或纳米颗粒的形式施用。在其他实施方案中，药物用聚合物包封。在某些实施方案中，药物与吸收促进剂组合施用。本发明进一步涉及维持不良吸收药物（例如紫杉醇）的口服生物利用度的给药方案。在另一个实施方案中，该方法包括给药一种或多种药物外排泵抑制剂与吸收不良的药物的组合。

10. 发明申请

WO2005056708A2 BIOADHESIVE POLYMERS WITH CATECHOL FUNCTIONALITY 审中-公开
标题翻译：具有CATECHOL功能的生物聚合物
公开(公告)号：WO2005056708A2
公开(公告)日：2005-06-23
申请号：PCT/US2004/041783
申请日：2004-12-09
申请人： SPHERICS, INC. , SCHESTOPOL, Marcus, A. , JACOB, Jules, S. , DONNELY, Ryan , RICKETTS, Thomas, L. , NANGIA, Avinash , MATHIOWITZ, Edith , SHAKED, Ze'ev
发明人： SCHESTOPOL, Marcus, A. , JACOB, Jules, S. , DONNELY, Ryan , RICKETTS, Thomas, L. , NANGIA, Avinash , MATHIOWITZ, Edith , SHAKED, Ze'ev
IPC分类号： C09J129/00
CPC分类号： C08F8/32 , A61K9/0004 , A61K9/006 , A61K9/0065 , A61K9/204 , A61K9/2077 , A61K9/2081 , A61K9/2086 , C08G63/91 , C08G63/912 , C09J167/00 , C09J167/04 , C08F222/06
摘要： Polymers with improved bioadhesive properties and methods for improving bioadhesion of polymers have been developed. A compound containing an aromatic group which contains one or more hydroxyl groups is grafted onto a polymer or coupled to individual monomers. In one embodiment, the polymer is a biodegradable polymer. In another embodiment, the monomers may be polymerized to form any type of polymer, including biodegradable and non-biodegradable polymers. In some embodiments, the polymer is a hydrophobic polymer. In the preferred embodiment, the polymer is a hydrophobic polymer. In the preferred embodiment, the aromatic compound is catechol or a derivative thereof and the polymer contains reactive functional groups. In the most preferred embodiment, the polymer is a polyanhydride and the aromatic compound is the catechol derivative, DOPA. These materials display bioadhesive properties superior to conventional bioadhesives used in therapeutic and diagnostic applications. These bioadhesive materials can be used to fabricate new drug delivery or diagnostic systems with increased residence time at tissue surfaces, and consequently increase the bioavailability of a drug or a diagnostic agent. In a preferred embodiment, the bioadhesive material is a coating on a controlled release oral dosage formulation and/or forms a matrix in an oral dosage formulation.
摘要翻译：已经开发了具有改进的生物粘附性质的聚合物和改善聚合物生物粘附的方法。含有含有一个或多个羟基的芳族基团的化合物被接枝到聚合物上或与单独的单体偶联。在一个实施方案中，聚合物是可生物降解的聚合物。在另一个实施方案中，单体可以聚合以形成任何类型的聚合物，包括可生物降解和不可生物降解的聚合物。在一些实施方案中，聚合物是疏水性聚合物。在优选的实施方案中，聚合物是疏水性聚合物。在优选的实施方案中，芳族化合物是儿茶酚或其衍生物，并且聚合物含有反应性官能团。在最优选的实施方案中，聚合物是聚酐，芳族化合物是邻苯二酚衍生物DOPA。这些材料显示出比用于治疗和诊断应用的常规生物粘合剂优越的生物粘附性。这些生物粘附材料可用于制造具有增加的组织表面停留时间的新药物递送或诊断系统，并因此提高药物或诊断剂的生物利用度。在优选的实施方案中，生物粘附材料是在控释口服剂量制剂上的涂层和/或在口服剂量制剂中形成基质。

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