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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

WO2005084639A3 POLYMERIC DRUG DELIVERY SYSTEM FOR HYDROPHOBIC DRUGS 审中-公开
标题翻译：用于疏水药物的聚合物药物递送系统
公开(公告)号：WO2005084639A3
公开(公告)日：2005-10-20
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：本文公开了由于其在水中的不溶性和缓慢的溶解动力学以及制备这种药物递送系统的方法而具有低口服生物利用度的II类药物的口服递送系统。制剂可以是控释或即时释放制剂。立即释放制剂含有II类药物，以及疏水性聚合物，优选生物粘附性聚合物。在一个实施方案中，将药物和聚合物共溶于常用溶剂。通过任何方便的方法，特别是通过喷雾干燥，将溶液形成小的固体颗粒。所得到的颗粒含有作为小颗粒分散在聚合物基质中的药物。颗粒对聚集是稳定的，并且可以放入胶囊或压片以供给药。控释制剂含有BCS II类药物和生物粘附性聚合物。控制释放制剂可以是片剂，胶囊，迷你片，微粒或渗透泵的形式。通过（1）由于药物的稳定的微粉化引起的溶出动力学增加，（2）药物从胃肠道中的聚合物快速释放，增加了使用生物粘附性聚合物对药物的口服摄取。和（3）由于聚合物的生物粘合性质而延长GI运输。这些作用的组合允许制备适于口服多种II类药物的紧凑，稳定的剂型。

3. 发明申请

WO2005056708A3 BIOADHESIVE POLYMERS WITH CATECHOL FUNCTIONALITY 审中-公开
标题翻译：具有儿茶酚官能度的亲水聚合物
公开(公告)号：WO2005056708A3
公开(公告)日：2005-07-28
申请号：PCT/US2004041783
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： A61K9/00 , A61K9/20 , A61K31/74 , C08F8/32 , C08G63/91 , C09J135/00 , C09J167/00 , C09J167/04 , C09J201/06 , C08F222/06 , C08G67/04
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：已经开发出具有改善的生物粘附性质的聚合物和用于改善聚合物的生物粘附性的方法。含有含一个或多个羟基的芳族基团的化合物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。在一些实施例中，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，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。这些材料的生物粘附性能优于用于治疗和诊断应用的常规生物粘附剂。这些生物粘附材料可用于制造在组织表面处具有增加的停留时间的新型药物递送或诊断系统，并因此增加药物或诊断剂的生物利用度。在一个优选的实施方案中，生物粘附材料是控释口服剂型中的包衣和/或在口服剂型中形成基质。

4. 发明申请

WO2006039022A2 CONTROLLED REGIONAL ORAL DELIVERY 审中-公开
标题翻译：控制区域口供
公开(公告)号：WO2006039022A2
公开(公告)日：2006-04-13
申请号：PCT/US2005030552
申请日：2005-08-29
申请人： SPHERICS INC , MATHIOWITZ EDITH , NANGIA AVINASH , JACOB JULES S , SHAKED ZE EV , MOSLEMY PEYMAN
发明人： MATHIOWITZ EDITH , NANGIA AVINASH , JACOB JULES S , SHAKED ZE EV , MOSLEMY PEYMAN
IPC分类号： A61K9/28
CPC分类号： A61K9/5031 , A61K9/006 , A61K9/0092 , A61K9/1641 , A61K9/1652 , A61K9/1676 , A61K9/2018 , A61K9/2031 , A61K9/204 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K9/209 , A61K9/4808 , A61K9/4891 , A61K9/5026 , A61K9/5084 , A61K31/74
摘要： A composite formulation has been developed for selective, high efficacy delivery to specific regions of the mouth and gastrointestinal tract. The formulation is typically in the form of a tablet or capsule, which may include microparticles or beads. The formulation uses bioadhesive and controlled release elements to direct release to specific regions, where the drug is absorbed in enhanced amounts relative to the formulation in the absence of the bioadhesive and/or controlled release elements. This is demonstrated by an example showing delivery of gabapentin with a greater area under the curve ("AUC") relative to the FDA reference immediate release drug, i.e., the AUC of the composite bioadhesive formulation is greater than 100% of the AUC of the immediate release drug. In the preferred embodiments, the formulation includes drug to be delivered, controlled release elements, and one or more bioadhesive elements. The bioadhesive polymer may be either dispersed in the matrix of the tablet or applied as a direct compressed coating to the solid oral dosage form. The controlled release elements are selected to determine the site of release. The bioadhesive components are selected to provide retention of the formulation at the desired site of uptake and administration. By selecting for both release and retention at a specific site, typically based on time of transit through the gastrointestinal tract, one obtains enhanced efficacy of uptake of the drug. This is particularly useful for drugs with narrow windows of absorption, and drugs with poor solubility such as the BCE class III and class IV drugs.
摘要翻译：已经开发出复合制剂用于选择性地，高效地递送到口腔和胃肠道的特定区域。制剂通常为片剂或胶囊形式，其可包括微粒或珠粒。该制剂使用生物粘附和控制释放元件将释放引导到特定区域，其中药物在不存在生物粘附和/或控制释放元件的情况下相对于制剂以增强的量被吸收。这通过示例显示，相对于FDA参考即时释放药物，曲线下面积更大的加巴喷丁（“AUC”）的递送，即复合生物粘附制剂的AUC大于100μg的AUC 立即释放药物。在优选的实施方案中，制剂包括待递送的药物，控制释放元件和一种或多种生物粘附元件。生物粘附聚合物可以分散在片剂的基质中，或作为直接压片包被施用于固体口服剂型。控制释放元件被选择以确定释放部位。生物粘附组分被选择以提供制剂在所需的摄取和给药部位的保留。通过选择在特定部位的释放和保留，通常基于通过胃肠道的转运时间，获得药物摄取的增强的功效。这对于具有狭窄吸收窗口的药物和溶解性差的药物如BCE III类和IV类药物特别有用。

5. 发明申请

WO2006026504A3 MUCOADHESIVE ORAL FORMULATIONS OF HIGH PERMEABILITY, HIGH SOLUBILITY DRUGS 审中-公开
标题翻译：高渗透性，高溶解性药物的高密度口服制剂
公开(公告)号：WO2006026504A3
公开(公告)日：2006-08-10
申请号：PCT/US2005030553
申请日：2005-08-29
申请人： SPHERICS INC , JACOB JULES S , MOSLEMY PEYMAN , NANGIA AVINASH , SHAKED ZE EV , KREITZ MARK
发明人： JACOB JULES S , MOSLEMY PEYMAN , NANGIA AVINASH , SHAKED ZE EV , KREITZ MARK
IPC分类号： A61K9/28
CPC分类号： A61K9/006 , A61K9/2086 , A61K9/2846 , A61K31/74
摘要： Solid oral dosage formulations, such as tablet, mini-tab, multiparticulates or osmotic delivery systems, are coated with a mucoadhesive polymeric coating or formed of a mucoadhesive polymer to increase oral bioavailability of Biopharmaceutical Classification System (BCS) Class I drugs. Representative BCS I drugs include valacyclovir, gabapentin, furosemide, levodopa, metformin, and ranitidine HCl. The inclusion of mucoadhesives in the solid oral dosage form brings the dosage form into close proximity with the target epithelium and facilitates diffusion of drug into intestinal tissue. The mucoadhesive polymer may be either dispersed in the matrix of the tablet or applied as a direct compressed coating to the solid oral dosage form. Preferred mucoadhesive polymers include poly (adipic)anhydride and poly (fumaric-co-sebacic) anhydride. Other preferred mucoadhesive polymers include non-erodable polymers such as DOPA-maleic anhydride co polymer; isopthalic anhydride polymer; DOPA-methacrylate polymers; and DOPA-cellulosic based polymers.
摘要翻译：固体口服剂型如片剂，迷你片，多颗粒或渗透递送系统用粘膜粘附聚合物涂层或由粘膜粘附聚合物形成以增加生物制药分类系统（BCS）I类药物的口服生物利用度。代表性的BCS I药物包括伐昔洛韦，加巴喷丁，呋塞米，左旋多巴，二甲双胍和盐酸雷尼替丁。在固体口服剂型中包含粘膜粘附剂使剂型与目标上皮紧密接近，并有利于药物扩散到肠组织中。粘膜粘附聚合物可以分散在片剂的基质中，或作为直接压缩包衣施用于固体口服剂型。优选的粘膜粘附聚合物包括聚（己二酸）酐和聚（富马酸 - 共 - 癸二酸）酐。其它优选的粘膜粘附聚合物包括不可侵蚀的聚合物，例如DOPA-马来酸酐共聚物; 异烟酸酐聚合物; DOPA-甲基丙烯酸酯聚合物; 和基于DOPA-纤维素的聚合物。

6. 发明申请

WO2006026556A3 BIOADHESIVE RATE-CONTROLLED ORAL DOSAGE FORMULATIONS 审中-公开
标题翻译：生物速率控制口服剂型
公开(公告)号：WO2006026556A3
公开(公告)日：2006-08-10
申请号：PCT/US2005030681
申请日：2005-08-29
申请人： SPHERICS INC , NANGIA AVINASH , JACOB JULES S , MOSLEMY PEYMAN
发明人： NANGIA AVINASH , JACOB JULES S , MOSLEMY PEYMAN
IPC分类号： A61K9/28
CPC分类号： A61K9/2853 , A61K9/2018 , A61K9/2054 , A61K9/209 , A61K9/284 , A61K9/2846 , A61K9/2886
摘要： The present invention relates to a bioadhesive drug delivery system (BIOadhesive Rate controlled Oral Dosage (BIOROD) formulation) in which a drug containing core either alone or coated with a rate controlling membrane system is enveloped on its circumference by a bioadhesive coating, thereby yielding a monolithic system that allows for drug release in a regulated manner. Also described herein are polymers with improved bioadhesive properties and methods for improving bioadhesion of polymers.
摘要翻译：本发明涉及一种生物粘附药物递送系统（BIOadhesive Rate controlled Oral Dosage（BIOROD）制剂），其中单独或用速率控制膜系统涂覆的药物的核心通过生物粘附剂包被在其圆周上，从而产生整体式系统允许以规定的方式释放药物。本文还描述了具有改进的生物粘附性质的聚合物和用于改善聚合物生物粘附的方法。

7. 发明申请

WO2006026592A3 ORAL ADMINISTRATION OF POORLY ABSORBED DRUGS, METHODS AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：不良吸收药物的口服药物，相关方法和组合物
公开(公告)号：WO2006026592A3
公开(公告)日：2006-09-14
申请号：PCT/US2005030774
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 , A61K9/16 , A61K9/28
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：本发明提供了用于递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。在其它实施方案中，药物用聚合物包封。在某些实施方案中，药物与吸收增强剂组合施用。本发明还涉及用于维持吸收不良的药物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，该方法涉及将药物外排泵的一种或多种抑制剂与不良吸收的药物组合施用抑制剂。

8. 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。

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