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1. 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。

2. 发明申请

WO2006026556A2 BIOADHESIVE RATE-CONTROLLED ORAL DOSAGE FORMULATIONS 审中-公开
标题翻译：生物消化速度控制的口服剂型制剂
公开(公告)号：WO2006026556A2
公开(公告)日：2006-03-09
申请号：PCT/US2005/030681
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：本发明涉及生物粘附药物递送系统（BIO粘附速率受控口服剂量（BIOROD）制剂），其中单独或包被有速率控制膜系统的含有药物的芯包封在其周长上通过生物粘附涂层，从而产生允许以受调节方式释放药物的整体式系统。本文还描述了具有改善的生物粘附性质的聚合物和改善聚合物的生物粘附性的方法。

3. 发明申请

WO2011041377A1 OCULAR IONTOPHORESIS OF CHARGED MICELLES CONTAINING BIOACTIVE AGENTS 审中-公开
标题翻译：含有生物活性剂的充电细胞的OCALAR IOPOPHORESIS
公开(公告)号：WO2011041377A1
公开(公告)日：2011-04-07
申请号：PCT/US2010/050672
申请日：2010-09-29
申请人： EYEGATE PHARMACEUTICALS, INC. , MOSLEMY, Peyman , WANG, Hong , PATANE, Michael
发明人： MOSLEMY, Peyman , WANG, Hong , PATANE, Michael
IPC分类号： A61F2/00
CPC分类号： A61K9/0048 , A61K47/186
摘要： This invention is related to pharmaceutical compositions consisting of charged micelles containing bioactive agents. The invention is also related to the methods of delivery of charged micelles to the eye of a mammal by iontophoresis.
摘要翻译：本发明涉及由含有生物活性剂的带电胶束组成的药物组合物。本发明还涉及通过离子电渗法将带电胶束递送至哺乳动物眼睛的方法。

4. 发明申请

WO2008079404A3 PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF PARKINSON'S DISEASE AND RELATED DISORDERS 审中-公开
标题翻译：用于治疗帕金森病和相关疾病的药物组合物
公开(公告)号：WO2008079404A3
公开(公告)日：2009-03-19
申请号：PCT/US2007026336
申请日：2007-12-21
申请人： SPHERICS INC , NANGIA AVINASH , JACOB JULES , YEH JAMES , MOSLEMY PEYMAN , VERMA DAYA D , HASWANI DINESH K , SHAKED ZE VE
发明人： NANGIA AVINASH , JACOB JULES , YEH JAMES , MOSLEMY PEYMAN , VERMA DAYA D , HASWANI DINESH K , SHAKED ZE VE
IPC分类号： A61K9/16 , A61K9/24 , A61K9/50 , A61K31/195 , A61K31/198
CPC分类号： A61K9/2031 , A61K9/0065 , A61K9/204 , A61K9/209 , A61K9/2853 , A61K9/5026 , A61K9/5031 , A61K9/5073 , A61K31/195 , A61K31/198 , A61K2300/00
摘要： The invention relates to the improvement in the treatment of certain neural disorders / diseases, such as Parkinson's disease and other motor disorders. The invention relates to drug compositions and dosage forms comprising said drug composition; methods of manufacturing the drug compositions and dosage forms; and methods of treatment, comprising administering the drug composition and dosage form to an individual. In certain embodiments, a decarboxylase enzyme inhibitor (e.g., carbidopa) extended release formulation is formulated with one or more bioadhesive polymers which may be useful for preferentially targeting the release of the decarboxylase enzyme inhibitor at the target absorption site. Upon administration to the patient, the inhibitor is delivered to a desired tissue location (e.g., proximal small intestine), and is released over an extended period (preferably from after dinner to the morning after).
摘要翻译：本发明涉及某些神经障碍/疾病如帕金森病和其他运动障碍的治疗的改善。本发明涉及包含所述药物组合物的药物组合物和剂型; 制备药物组合物和剂型的方法; 和治疗方法，包括将药物组合物和剂型给予个体。在某些实施方案中，脱羧酶抑制剂（例如卡比多巴）延长释放制剂配制有一种或多种生物粘附聚合物，其可用于优先靶向靶标吸收位点处的脱羧酶抑制剂的释放。在给予患者时，将抑制剂递送至期望的组织位置（例如，近端小肠），并在延长的时期（优选从晚餐至早晨之后）释放。

5. 发明申请

WO2005084639A2 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：WO2005084639A2
公开(公告)日：2005-09-15
申请号：PCT/US2005/007525
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
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：本文公开了由于其不溶于水且缓慢溶出动力学而具有低口服生物利用度的II类药物的口服递送系统以及制备此类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。这些效果的结合使得可以制备适用于许多II类药物的口服给药的致密稳定的剂型。

6. 发明申请

WO2010078246A1 SYSTEM AND METHOD FOR OCULAR IONTOPHORESIS WITH BUFFERING 审中-公开
标题翻译：具有缓冲作用的OCULAR IOPOPHORESIS的系统和方法
公开(公告)号：WO2010078246A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/069580
申请日：2009-12-28
申请人： EYEGATE PHARMA S.A.S. , MOSLEMY, Peyman , MANZO, Michael , SCHUBERT, William , ISOM, William , PIERRE, Roy
发明人： MOSLEMY, Peyman , MANZO, Michael , SCHUBERT, William , ISOM, William , PIERRE, Roy
IPC分类号： A61N1/30
CPC分类号： A61F9/0026 , A61N1/0444 , A61N1/0448 , A61N1/303 , A61N1/325
摘要： Compositions, devices, methods of manufacture, and methods of delivery of a therapeutic substance across a surface of an eyeball via iontophoresis including a therapeutic media reservoir and a buffer system within an iontophoretic chamber. When energized, an electrode provides an electromotive force that transfers a dosage of the therapeutic substance from the iontophoretic chamber across the surface of the eyeball. The buffering system includes a buffer media and at least one buffer element, or agent that regulates pH during iontophoretic transfer of the therapeutic substance. The buffer media includes at least one of a foam, a gel (solid or liquid), a membrane, and a plurality of multiparticulates. The buffer media can be included within the iontophoretic chamber, together with the therapeutic media reservoir, in various arrangements including one or more layers and one or more concentric cylinders.
摘要翻译：组合物，装置，制造方法以及通过离子电渗法在眼球表面递送治疗物质的方法，包括在离子电渗室内的治疗介质储器和缓冲系统。当通电时，电极提供电动势，其将来自离子电渗腔的治疗物质的剂量转移穿过眼球的表面。缓冲系统包括缓冲介质和调节治疗物质的离子电渗转移期间的pH的至少一种缓冲元件或试剂。缓冲介质包括泡沫，凝胶（固体或液体），膜和多个多颗粒中的至少一种。缓冲介质可以与治疗介质储存器一起包括在离子电渗腔内，包括一个或多个层和一个或多个同心圆筒的各种布置。

7. 发明申请

WO2007103286A3 RATE-CONTROLLED BIOADHESIVE ORAL DOSAGE FORMULATIONS 审中-公开
标题翻译：速率控制的生物配方口服制剂
公开(公告)号：WO2007103286A3
公开(公告)日：2009-07-02
申请号：PCT/US2007005549
申请日：2007-03-02
申请人： SPHERICS INC , NANGIA AVINASH , JACOB JULES , MOSLEMY PEYMAN , HASWANI DINESH K
发明人： NANGIA AVINASH , JACOB JULES , MOSLEMY PEYMAN , HASWANI DINESH K
IPC分类号： A61K9/20 , A61K9/22 , A61K9/24 , A61K9/26 , A61K9/28 , A61K9/32 , A61K31/403 , A61K31/5415
CPC分类号： A61K9/006 , A61K9/0004 , A61K9/0065 , A61K9/2018 , A61K9/2054 , A61K9/2072 , A61K9/2077 , A61K9/209 , A61K9/2853 , A61K9/2866 , A61K31/00 , A61K31/403 , A61K31/5415
摘要： The present invention relates to a drug delivery system, in which a drug containing core, either alone or coated with a rate controlling membrane system, is enveloped on its circumference by an optionally bioadhesive coating, thereby yielding a monolithic system that allows for drug release in a regulated manner.
摘要翻译：本发明涉及一种药物递送系统，其中单独或涂覆有速率控制膜系统的药物包含的核心通过任选的生物粘附性包被在其周围包围，从而产生允许药物释放的整体系统受规管的方式。

8. 发明申请

WO2007002516A3 IMPROVED DOSAGE FORMS FOR MOVEMENT DISORDER TREATMENT 审中-公开
公开(公告)号：WO2007002516A3
公开(公告)日：2007-01-04
申请号：PCT/US2006/024663
申请日：2006-06-23
申请人： SPHERICS, INC. , NANGIA, Avinash , JACOB, Jules , YEH, James , MOSLEMY, Peyman , VERMA, Daya, D. , HASWANI, Dinesh, K. , SHAKED, Ze'ev
发明人： NANGIA, Avinash , JACOB, Jules , YEH, James , MOSLEMY, Peyman , VERMA, Daya, D. , HASWANI, Dinesh, K. , SHAKED, Ze'ev
IPC分类号： A61K9/28 , A61K9/48 , A61K31/198 , A61K31/195 , A61K31/428 , A61K9/16 , A61K9/50
摘要： The invention relates to the improvement in the treatment of certain neural disorders / diseases, such as Parkinson's disease and other motor disorders. One aspect of the invention relates to drug compositions and dosage forms comprising said drug composition. Another aspect of the invention relates to methods of manufacturing the drug compositions and dosage forms. Another aspect of the invention relates to methods of treatment, comprising administering the drug composition and dosage form to an individual.

9. 发明申请

WO2009076220A1 METHODS FOR DELIVERING SIRNA VIA IONTOPHORESIS 审中-公开
标题翻译：用于传递SIRNA通过IOPOPHORESIS的方法
公开(公告)号：WO2009076220A1
公开(公告)日：2009-06-18
申请号：PCT/US2008/085709
申请日：2008-12-05
申请人： EYEGATE PHARMA S.A.S. , SCHUBERT, William , MOSLEMY, Peyman , PATANE, Mike , ISOM, Phil
发明人： SCHUBERT, William , MOSLEMY, Peyman , PATANE, Mike , ISOM, Phil
IPC分类号： A61N1/30
CPC分类号： A61N1/0448
摘要： Disclosed herein are formulations of siRNA suitable for delivery by ocular iontophoresis, devices for iontophoretic delivery of siRNA and methods of use thereof.
摘要翻译：本文公开了适合于通过眼部离子电渗疗法递送的siRNA的制剂，用于siRNA的离子电渗疗法递送的装置及其使用方法。

10. 发明申请

WO2008079404A2 PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF PARKINSON'S DISEASE AND RELATED DISORDERS 审中-公开
标题翻译：用于治疗帕金森病和相关疾病的药物组合物
公开(公告)号：WO2008079404A2
公开(公告)日：2008-07-03
申请号：PCT/US2007/026336
申请日：2007-12-21
申请人： SPHERICS, INC. , NANGIA, Avinash , JACOB, Jules , YEH, James , MOSLEMY, Peyman , VERMA, Daya, D. , HASWANI, Dinesh, K. , SHAKED, Ze've
发明人： NANGIA, Avinash , JACOB, Jules , YEH, James , MOSLEMY, Peyman , VERMA, Daya, D. , HASWANI, Dinesh, K. , SHAKED, Ze've
CPC分类号： A61K9/2031 , A61K9/0065 , A61K9/204 , A61K9/209 , A61K9/2853 , A61K9/5026 , A61K9/5031 , A61K9/5073 , A61K31/195 , A61K31/198 , A61K2300/00
摘要： The invention relates to the improvement in the treatment of certain neural disorders / diseases, such as Parkinson's disease and other motor disorders. The invention relates to drug compositions and dosage forms comprising said drug composition; methods of manufacturing the drug compositions and dosage forms; and methods of treatment, comprising administering the drug composition and dosage form to an individual. In certain embodiments, a decarboxylase enzyme inhibitor (e.g., carbidopa) extended release formulation is formulated with one or more bioadhesive polymers which may be useful for preferentially targeting the release of the decarboxylase enzyme inhibitor at the target absorption site. Upon administration to the patient, the inhibitor is delivered to a desired tissue location (e.g., proximal small intestine), and is released over an extended period (preferably from after dinner to the morning after).
摘要翻译：本发明涉及某些神经障碍/疾病如帕金森病和其他运动障碍的治疗的改善。本发明涉及包含所述药物组合物的药物组合物和剂型; 制备药物组合物和剂型的方法; 和治疗方法，包括将药物组合物和剂型给予个体。在某些实施方案中，脱羧酶抑制剂（例如卡比多巴）延长释放制剂配制有一种或多种生物粘附聚合物，其可用于优先靶向靶标吸收位点处的脱羧酶抑制剂的释放。在给予患者时，将抑制剂递送至期望的组织位置（例如，近端小肠），并在延长的时期（优选从晚餐至早晨之后）释放。

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