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1. 发明申请

WO2005072702A2 METHOD FOR MILLING FROZEN MICROPARTICLES 审中-公开
标题翻译：用于研磨冷冻微生物的方法
公开(公告)号：WO2005072702A2
公开(公告)日：2005-08-11
申请号：PCT/US2005001649
申请日：2005-01-19
申请人： ALKERMES INC , HERBERT PAUL F , TROIANO GREGORY C
发明人： HERBERT PAUL F , TROIANO GREGORY C
IPC分类号： A61K9/14 , A61K9/16 , A61K9/19 , A61K9/00
CPC分类号： A61K9/146 , A61K9/1647 , A61K9/1694 , A61K9/19
摘要： A method for forming microparticles include fragments solid particles that include a biologically active agent, a biocompatible polymer and a solvent, thereby producing fragments solid particles, and separating the solvent from the fragmented solid particles, thereby forming the micropraticles. The method can also include the steps of forming a mixture of the biologically active agent, the biocompatible polymer and the solvent, and freezing the mixture to form the solid particles. The present invention also relates to methods for producing injectable pharmaceutical compositions that include an injectable microparticle population.
摘要翻译：形成微粒的方法包括包含生物活性剂，生物相容性聚合物和溶剂的固体颗粒碎片，从而产生碎片固体颗粒，并从溶解的固体颗粒中分离溶剂，从而形成微小孔。该方法还可以包括形成生物活性剂，生物相容性聚合物和溶剂的混合物的步骤，并冷冻混合物以形成固体颗粒。本发明还涉及可注射药物组合物的制备方法，其包括可注射的微粒群体。

2. 发明申请

WO2005107714A3 METHOD OF FORMING MICROPARTICLES THAT INCLUDE A BISPHOSPHONATE AND A POLYMER 审中-公开
标题翻译：形成包含二磷酸酯和聚合物的微生物的方法
公开(公告)号：WO2005107714A3
公开(公告)日：2006-09-28
申请号：PCT/US2005015757
申请日：2005-05-05
申请人： ALKERMES INC , FIGUEIREDO MARIA C , KUMAR RAJESH , MALONEY MAURA J , SCHER DAVID S , YEOH THEAN Y , ZALE STEPHEN E , PRINN KRISTIN , TROIANO GREGORY
发明人： FIGUEIREDO MARIA C , KUMAR RAJESH , MALONEY MAURA J , SCHER DAVID S , YEOH THEAN Y , ZALE STEPHEN E , PRINN KRISTIN , TROIANO GREGORY
IPC分类号： A61K9/16 , A61K9/14 , A61K9/19 , A61K9/50 , A61K31/66 , A61K31/675 , B01J13/02 , B01J13/04 , C08L23/08
CPC分类号： A61K9/1647 , A61K9/1641 , A61K9/1694 , A61K9/19 , C08L23/08 , C08L23/0815 , C08L2205/02 , C08L2666/06
摘要： Microparticles that includes a bisphosphonate and a polymer are produced by a method that includes forming a water-in-oil emulsion by mixing an aqueous solution of the bisphosphonate with a combination of a biocompatible polymer and a polymer solvent. At least one aqueous liquid can be mixed with the water-in-oil emulsion to form a water-in-oil-in-water emulsion and to extract the polymer solvent from the polymer, thereby forming the microparticles. Methods of treating a patient in need of therapy include administering the microparticles described to the patient. In one embodiment, the microparticles are formulated for the sustained release of the bisphosphonate.
摘要翻译：包括二膦酸盐和聚合物的微粒通过包括通过将二膦酸盐的水溶液与生物相容性聚合物和聚合物溶剂的组合混合形成油包水乳液的方法来制备。可以将至少一种含水液体与油包水乳液混合以形成水包油包水乳液，并从聚合物中提取聚合物溶剂，从而形成微粒。治疗需要治疗的患者的方法包括给患者描述的微粒进行给药。在一个实施方案中，将微粒配制成二膦酸盐的持续释放。

3. 发明申请

WO2004064752A3 METHOD OF PREPARING SUSTAINED RELEASE MICROPARTICLES 审中-公开
标题翻译：制备持续释放微生物的方法
公开(公告)号：WO2004064752A3
公开(公告)日：2005-05-12
申请号：PCT/US2004001501
申请日：2004-01-21
申请人： ALKERMES INC , BROWN JOSIAH , JAWOROWICZ WARREN E , TROIANO GREGORY C
发明人： BROWN JOSIAH , JAWOROWICZ WARREN E , TROIANO GREGORY C
IPC分类号： A61K9/00 , A61K9/16 , A61K9/50
CPC分类号： A61K9/1694 , A61K9/0024 , A61K9/1647 , A61K9/5031 , Y10T428/2982 , Y10T428/2991 , Y10T428/2998
摘要： The present invention relates to a method for preparing an injectable composition of microparticles for the sustained release of a biologically active agent. The microparticles include a biocompatible polymer and a biologically active agent. The invention provides an improved process for the preparation of microparticles, wherein the physical characteristics of the microparticles, for example, the morphology, density and size, are independent of the process used to prepare the initially formed polymer/drug matrix. The method includes the steps of (a) providing a polymer/biologically active agent matrix; (b) compressing the polymer/biologically active agent matrix, thereby forming a compressed matrix; and (c) fragmenting the compressed matrix, thereby forming an injectable microparticle composition. The polymer/drug matrix can be provided by any suitable method.
摘要翻译：本发明涉及制备用于持续释放生物活性剂的微粒的可注射组合物的方法。微粒包括生物相容性聚合物和生物活性剂。本发明提供了一种制备微粒的改进方法，其中微粒的物理特性，例如形态，密度和尺寸，与用于制备初始形成的聚合物/药物基质的方法无关。该方法包括以下步骤：（a）提供聚合物/生物活性剂基质; （b）压缩聚合物/生物活性剂基质，从而形成压缩基质; 和（c）将压缩的基质分段，从而形成可注射的微粒组合物。聚合物/药物基质可以通过任何合适的方法提供。

4. 发明申请

WO2004064752A2 METHOD OF PREPARING SUSTAINED RELEASE MICROPARTICLES 审中-公开
标题翻译：制备持续释放微生物的方法
公开(公告)号：WO2004064752A2
公开(公告)日：2004-08-05
申请号：PCT/US2004/001501
申请日：2004-01-21
申请人： ALKERMES CONTROLLED THERAPEUTICS, INC. , BROWN, Josiah , JAWOROWICZ, Warren, E. , TROIANO, Gregory, C.
发明人： BROWN, Josiah , JAWOROWICZ, Warren, E. , TROIANO, Gregory, C.
IPC分类号： A61K
CPC分类号： A61K9/1694 , A61K9/0024 , A61K9/1647 , A61K9/5031 , Y10T428/2982 , Y10T428/2991 , Y10T428/2998
摘要： The present invention relates to a method for preparing an injectable composition of microparticles for the sustained release of a biologically active agent. The microparticles include a biocompatible polymer and a biologically active agent. The invention provides an improved process for the preparation of microparticles, wherein the physical characteristics of the microparticles, for example, the morphology, density and size, are independent of the process used to prepare the initially formed polymer/drug matrix. The method includes the steps of (a) providing a polymer/biologically active agent matrix; (b) compressing the polymer/biologically active agent matrix, thereby forming a compressed matrix; and (c) fragmenting the compressed matrix, thereby forming an injectable microparticle composition. The polymer/drug matrix can be provided by any suitable method.
摘要翻译：本发明涉及制备用于持续释放生物活性剂的微粒可注射组合物的方法。微粒包括生物相容性聚合物和生物活性剂。本发明提供了一种制备微粒的改进方法，其中微粒的物理特性，例如形态，密度和尺寸，与用于制备初始形成的聚合物/药物基质的方法无关。该方法包括以下步骤：（a）提供聚合物/生物活性剂基质; （b）压缩聚合物/生物活性剂基质，由此形成压缩基质; 和（c）使压缩的基质碎裂，从而形成可注射的微粒组合物。聚合物/药物基质可以通过任何合适的方法提供。

5. 发明申请

WO2005107714A2 METHOD OF FORMING MICROPARTICLES THAT INCLUDE A BISPHOSPHONATE AND A POLYMER 审中-公开
标题翻译：形成包含二磷酸酯和聚合物的微生物的方法
公开(公告)号：WO2005107714A2
公开(公告)日：2005-11-17
申请号：PCT/US2005/015757
申请日：2005-05-05
申请人： ALKERMES CONTROLLED THERAPEUTICS, INC. , FIGUEIREDO, Maria, C. , KUMAR, Rajesh , MALONEY, Maura, J. , SCHER, David, S. , YEOH, Thean, Y. , ZALE, Stephen, E. , PRINN, Kristin , TROIANO, Gregory
发明人： FIGUEIREDO, Maria, C. , KUMAR, Rajesh , MALONEY, Maura, J. , SCHER, David, S. , YEOH, Thean, Y. , ZALE, Stephen, E. , PRINN, Kristin , TROIANO, Gregory
IPC分类号： A61K9/16
CPC分类号： A61K9/1647 , A61K9/1641 , A61K9/1694 , A61K9/19 , C08L23/08 , C08L23/0815 , C08L2205/02 , C08L2666/06
摘要： Microparticles that includes a bisphosphonate and a polymer are produced by a method that includes forming a water-in-oil emulsion by mixing an aqueous solution of the bisphosphonate with a combination of a biocompatible polymer and a polymer solvent. At least one aqueous liquid can be mixed with the water-in-oil emulsion to form a water-in-oil-in-water emulsion and to extract the polymer solvent from the polymer, thereby forming the microparticles. Methods of treating a patient in need of therapy include administering the microparticles described to the patient. In one embodiment, the microparticles are formulated for the sustained release of the bisphosphonate.
摘要翻译：包括二膦酸盐和聚合物的微粒通过包括通过将二膦酸盐的水溶液与生物相容性聚合物和聚合物溶剂的组合混合形成油包水乳液的方法来制备。可以将至少一种含水液体与油包水乳液混合以形成水包油包水乳液，并从聚合物中提取聚合物溶剂，从而形成微粒。治疗需要治疗的患者的方法包括将所描述的微粒给予患者。在一个实施方案中，将微粒配制成二膦酸盐的持续释放。

6. 发明申请

WO2005072702A3 METHOD FOR MILLING FROZEN MICROPARTICLES 审中-公开
公开(公告)号：WO2005072702A3
公开(公告)日：2005-08-11
申请号：PCT/US2005/001649
申请日：2005-01-19
申请人： ALKERMES CONTROLLED THERAPEUTICS, INC. , HERBERT, Paul, F. , TROIANO, Gregory, C.
发明人： HERBERT, Paul, F. , TROIANO, Gregory, C.
IPC分类号： A61K9/16
摘要： A method for forming microparticles include fragments solid particles that include a biologically active agent, a biocompatible polymer and a solvent, thereby producing fragments solid particles, and separating the solvent from the fragmented solid particles, thereby forming the micropraticles. The method can also include the steps of forming a mixture of the biologically active agent, the biocompatible polymer and the solvent, and freezing the mixture to form the solid particles. The present invention also relates to methods for producing injectable pharmaceutical compositions that include an injectable microparticle population.

7. 发明申请

WO2005025543A3 POLYMER-BASED SUSTAINED RELEASE DEVICE AND METHOD FOR PREPARATION 审中-公开
公开(公告)号：WO2005025543A3
公开(公告)日：2005-03-24
申请号：PCT/US2004/029645
申请日：2004-09-08
申请人： ALKERMES CONTROLLED THERAPEUTICS, INC. , TROIANO, Gregory, C. , PASZYC, Tina , JAWOROWICZ, Warren, E. , BROWN, Josiah
发明人： TROIANO, Gregory, C. , PASZYC, Tina , JAWOROWICZ, Warren, E. , BROWN, Josiah
IPC分类号： A61K9/16 , A61K38/00
摘要： Methods for preparing a polymer-based sustained release device including a biocompatible polymer having incorporated therein a biologically active agent are described. In one embodiment, the method of preparing a polymer-based sustained release device comprises the steps of (a) exchanging a continuous medium component of a disperse system, the disperse system including a biologically active agent as a dispersed entity, with an organic liquid, thereby forming a first mixture that includes the biologically active agent and the organic liquid; (b) combining a biocompatible polymer with the first mixture, thereby forming a second mixture that includes the biologically active agent, the organic liquid, and the biocompatible polymer; and (c) separating the organic liquid from the second mixture, thereby forming the polymer-based sustained release device. In one embodiment, the continuous medium component of the disperse system is exchanged with the organic liquid using diafiltration, for example, diafiltration using tangential flow filtration.

8. 发明申请

WO2005025543A2 POLYMER-BASED SUSTAINED RELEASE DEVICE AND METHOD FOR PREPARATION 审中-公开
标题翻译：基于聚合物的持续释放装置及其制备方法
公开(公告)号：WO2005025543A2
公开(公告)日：2005-03-24
申请号：PCT/US2004029645
申请日：2004-09-08
申请人： ALKERMES INC , TROIANO GREGORY C , PASZYC TINA , JAWOROWICZ WARREN E , BROWN JOSIAH
发明人： TROIANO GREGORY C , PASZYC TINA , JAWOROWICZ WARREN E , BROWN JOSIAH
IPC分类号： A61K9/16 , A61K38/00
CPC分类号： A61K9/1694 , A61K9/1647
摘要： Methods for preparing a polymer-based sustained release device including a biocompatible polymer having incorporated therein a biologically active agent are described. In one embodiment, the method of preparing a polymer-based sustained release device comprises the steps of (a) exchanging a continuous medium component of a disperse system, the disperse system including a biologically active agent as a dispersed entity, with an organic liquid, thereby forming a first mixture that includes the biologically active agent and the organic liquid; (b) combining a biocompatible polymer with the first mixture, thereby forming a second mixture that includes the biologically active agent, the organic liquid, and the biocompatible polymer; and (c) separating the organic liquid from the second mixture, thereby forming the polymer-based sustained release device. In one embodiment, the continuous medium component of the disperse system is exchanged with the organic liquid using diafiltration, for example, diafiltration using tangential flow filtration.
摘要翻译：描述了制备包含其中并入生物活性剂的生物相容性聚合物的基于聚合物的持续释放装置的方法。在一个实施方案中，制备基于聚合物的持续释放装置的方法包括以下步骤：（a）将分散系统的连续介质组分（包括分散体的生物活性剂）与有机液体交换，从而形成包含生物活性剂和有机液体的第一混合物; （b）将生物相容性聚合物与第一混合物结合，从而形成包含生物活性剂，有机液体和生物相容性聚合物的第二混合物; 和（c）从第二混合物中分离有机液体，从而形成基于聚合物的持续释放装置。在一个实施方案中，使用渗滤将有机液体与分散系统的连续介质组分进行交换，例如使用切向流过滤进行渗滤。

9. 发明申请

WO2008118712A1 COACERVATION PROCESS 审中-公开
标题翻译：采购流程
公开(公告)号：WO2008118712A1
公开(公告)日：2008-10-02
申请号：PCT/US2008/057484
申请日：2008-03-19
申请人： ALKERMES, INC. , KUMAR, Rajesh , TROIANO, Gregory , RAMSTACK, J., Michael , HERBERT, Paul , FIGA, Michael
发明人： KUMAR, Rajesh , TROIANO, Gregory , RAMSTACK, J., Michael , HERBERT, Paul , FIGA, Michael
IPC分类号： A61K9/14
CPC分类号： A61K9/1647 , A61K9/1623 , A61K9/1682 , A61K9/5031 , A61K9/5089 , A61K38/2278
摘要： Methods of forming compositions for the sustained release of water soluble active agents, including biologically active polypeptides and products produced by the process are described. Improved product characteristics and ease of scale-up can be achieved using a novel coacervation process wherein at least one coacervation agent is added to the mixture comprising the active agent and the polymer in at least two distinct stages.
摘要翻译：描述了形成用于持续释放水溶性活性剂（包括生物活性多肽）和由该方法产生的产物的组合物的方法。可以使用新颖的凝聚方法来实现改进的产品特性和容易的放大，其中在至少两个不同阶段向包含活性剂和聚合物的混合物中加入至少一种凝聚剂。

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