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公开(公告)号：US10406161B2
公开(公告)日：2019-09-10
申请号：US16144614
申请日：2018-09-27
发明人： Kaoxiang Sun , Rongcai Liang , Qilin Wang , Wenyan Wang , Wanhui Liu , Youxin Li
摘要： A risperidone sustained release microsphere formulation is provided. The microsphere formulation comprise risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release microsphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
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2.发明申请公开(公告)号：US20140356442A1
公开(公告)日：2014-12-04
申请号：US14367096
申请日：2012-12-18
发明人： Kaoxiang Sun , Tao Song , Qilin Wang , Jie Han , Tao Wang , Jiangbin Han , Jianzhao Zhang , Shujiang Wang
CPC分类号： A61K38/22 , A61K9/0019 , A61K9/1623 , A61K9/1635 , A61K9/5031 , A61K38/09
摘要： Sustained release triptorelin microspheres include triptorelin or a salt of triptorelin, a copolymer of lactide and glycolide, and glucose or mannitol. The sustained release triptorelin microspheres have a relatively high initial release after administration, which allows the drug to produce its pharmaceutical effects immediately and to maintain long-term steady pharmaceutical effects.
摘要翻译： 缓释曲塞曲霉素微球包括曲普瑞林或曲普瑞林盐，丙交酯和乙交酯的共聚物，以及葡萄糖或甘露糖醇。 持续释放的曲普瑞林微管在施用后具有相对较高的初始释放，其允许药物立即产生其药物作用并保持长期稳定的药物作用。
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公开(公告)号：US20170056407A1
公开(公告)日：2017-03-02
申请号：US15347365
申请日：2016-11-09
发明人： Kaoxiang Sun , Rongcai Liang , Qilin Wang , Wenyan Wang , Wanhui Liu , Youxin Li
IPC分类号： A61K31/519 , A61K9/00 , A61K9/16
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/14 , A61K9/16 , A61K9/1647 , A61K9/19 , A61K9/4858 , A61K9/5031 , A61K9/5089 , A61K47/34
摘要： A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
摘要翻译： 提供了利培酮缓释微球制剂。 微球制剂包括利培酮或9-羟基利培酮或其盐，以及具有第一未封端丙交酯 - 乙交酯共聚物和第二未封端丙交酯 - 乙交酯共聚物的聚合物共混物，其中第一未封端丙交酯 - 乙交酯共聚物是具有高的共聚物 特性粘度和第二未封端丙交酯 - 乙交酯共聚物是具有低特性粘度的共聚物。 根据本公开实施方案的缓释微球制剂适用于具有改进的稳定性的大规模工业化生产，其体内释放行为在长期储存后不会改变。
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公开(公告)号：US20160331752A1
公开(公告)日：2016-11-17
申请号：US15217696
申请日：2016-07-22
发明人： Kaoxiang Sun , Rongcai Liang , Qilin Wang , Wenyan Wang , Wanhui Liu , Youxin Li
IPC分类号： A61K31/519 , A61K9/48 , A61K9/00 , A61K9/50
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/14 , A61K9/16 , A61K9/1647 , A61K9/19 , A61K9/4858 , A61K9/5031 , A61K9/5089 , A61K47/34
摘要： A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
摘要翻译： 提供了利培酮缓释微球制剂。 微球制剂包括利培酮或9-羟基利培酮或其盐，以及具有第一未封端丙交酯 - 乙交酯共聚物和第二未封端丙交酯 - 乙交酯共聚物的聚合物共混物，其中第一未封端丙交酯 - 乙交酯共聚物是具有高的共聚物 特性粘度和第二未封端丙交酯 - 乙交酯共聚物是具有低特性粘度的共聚物。 根据本公开实施方案的缓释微球制剂适用于具有改进的稳定性的大规模工业化生产，其体内释放行为在长期储存后不会改变。
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公开(公告)号：US20190022098A1
公开(公告)日：2019-01-24
申请号：US16144614
申请日：2018-09-27
发明人： Kaoxiang Sun , Rongcai Liang , Qilin Wang , Wenyan Wang , Wanhui Liu , Youxin Li
IPC分类号： A61K31/519 , A61K9/19 , A61K9/50 , A61K9/00
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/14 , A61K9/16 , A61K9/1647 , A61K9/19 , A61K9/4858 , A61K9/5031 , A61K9/5089 , A61K47/34
摘要： A risperidone sustained release microsphere formulation is provided. The microsphere formulation comprise risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release microsphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
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公开(公告)号：US20180117123A1
公开(公告)日：2018-05-03
申请号：US15803807
申请日：2017-11-05
发明人： Tao Wang , Qilin Wang , Qianqian Xu , Lifang Sun , Ying Meng , Ju Li
CPC分类号： A61K38/26 , A61K9/16 , A61K9/1647 , A61K9/1682 , A61K38/22 , A61K47/34
摘要： An exenatide-containing composition is in the form of microspheres, which are prepared by using exenatide acetate and polylactic-co-glycolic acid (PLGA) as raw materials, and the content of acetic acid in the prepared composition is lower than 0.01%. A method for preparing the exenatide-containing microspheres includes selecting a cleaning fluid of a proper external water phase and a proper amount to clean microspheres, and selecting a proper re-drying temperature to cure the microspheres after the microspheres are freeze-dried.
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公开(公告)号：US10098882B2
公开(公告)日：2018-10-16
申请号：US15347365
申请日：2016-11-09
发明人： Kaoxiang Sun , Rongcai Liang , Qilin Wang , Wenyan Wang , Wanhui Liu , Youxin Li
摘要： A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
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公开(公告)号：US20170035856A1
公开(公告)日：2017-02-09
申请号：US15304528
申请日：2015-04-16
发明人： Tao Wang , Qilin Wang , Qianqian Xu , Lifang Sun , Ying Meng , Ju Li
CPC分类号： A61K38/26 , A61K9/16 , A61K9/1647 , A61K9/1682 , A61K38/22 , A61K47/34
摘要： An exenatide-containing composition is in the form of microspheres, which are prepared by using exenatide acetate and polylactic-co-glycolic acid (PLGA) as raw materials, and the content of acetic acid in the prepared composition is lower than 0.01%. A method for preparing the exenatide-containing microspheres includes selecting a cleaning fluid of a proper external water Phase and a proper amount to clean microspheres, and selecting a proper re-drying temperature to cure the after the microspheres are freeze dried.
摘要翻译： 含有艾塞那肽的组合物为微球形式，其通过使用醋酸艾塞那肽和聚乳酸共 - 乙醇酸（PLGA）作为原料制备，并且所制备组合物中乙酸的含量低于0.01％。 制备含有艾塞那肽的微球的方法包括选择适当的外部水相的清洗液和适量的清洁微球，并在微球冷冻干燥后选择适当的再干燥温度以固化。
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公开(公告)号：US09532991B2
公开(公告)日：2017-01-03
申请号：US15217696
申请日：2016-07-22
发明人： Kaoxiang Sun , Rongcai Liang , Qilin Wang , Wenyan Wang , Wanhui Liu , Youxin Li
IPC分类号： A61K9/50 , A61K31/519 , A61K9/48 , A61K9/00 , A61K9/16
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/14 , A61K9/16 , A61K9/1647 , A61K9/19 , A61K9/4858 , A61K9/5031 , A61K9/5089 , A61K47/34
摘要： A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
摘要翻译： 提供了利培酮缓释微球制剂。 微球制剂包括利培酮或9-羟基利培酮或其盐，以及具有第一未封端丙交酯 - 乙交酯共聚物和第二未封端丙交酯 - 乙交酯共聚物的聚合物共混物，其中第一未封端丙交酯 - 乙交酯共聚物是具有高的共聚物 特性粘度和第二未封端丙交酯 - 乙交酯共聚物是具有低特性粘度的共聚物。 根据本公开实施方案的缓释微球制剂适用于具有改进的稳定性的大规模工业化生产，其体内释放行为在长期储存后不会改变。
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