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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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公开(公告)号：US11110094B2
公开(公告)日：2021-09-07
申请号：US16525502
申请日：2019-07-29
发明人： Kaoxiang Sun , Rongcai Liang , Oilin 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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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：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：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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![POLYMORPHS OF 4-[2-DIMETHYLAMINO-1-(1-HYDROXYCYCLOHEXYL)ETHYL]PHENYL 4-METHYLBENZOATE HYDROCHLORIDE, METHODS OF PREPARING THE SAME AND USE OF THE SAME](/abs-image/US/2014/08/21/US20140235728A1/abs.jpg.150x150.jpg)
6.发明申请POLYMORPHS OF 4-[2-DIMETHYLAMINO-1-(1-HYDROXYCYCLOHEXYL)ETHYL]PHENYL 4-METHYLBENZOATE HYDROCHLORIDE, METHODS OF PREPARING THE SAME AND USE OF THE SAME 审中-公开4- [2-二甲基氨基-1-（1-羟基环己基）乙基]苯基4-甲基苯甲酸酯盐酸盐的聚合物，其制备方法和使用该方法公开(公告)号：US20140235728A1
公开(公告)日：2014-08-21
申请号：US14259964
申请日：2014-04-23
发明人： Youxin Li , Wanhui Liu , Yang Lv , Guanhua Du , Qingguo Meng , Mina Yang , Fengmei Zhou , Ju Li , Xuemei Zhang
IPC分类号： C07C215/64 , C07C213/10
CPC分类号： C07C215/64 , A61K31/235 , C07B2200/13 , C07C213/10 , C07C215/20 , C07C219/28
摘要： The present disclosure relates to polymorphs of 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride, methods for preparing the same and use of the same.
摘要翻译： 本公开涉及4- [2-二甲基氨基-1-（1-羟基环己基）乙基] -4-甲基苯甲酸苯酯盐酸盐的多晶型物，其制备方法及其用途。
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![POLYMORPHS OF 4-[2-DIMETHYLAMINO-1-(1-HYDROXYCYCLOHEXYL)ETHYL]PHENYL 4-METHYL-BENZOATE HYDROCHLORIDE, METHODS FOR PREPARING THE SAME AND USE OF THE SAME](/abs-image/US/2013/10/24/US20130281531A1/abs.jpg.150x150.jpg)
7.发明申请POLYMORPHS OF 4-[2-DIMETHYLAMINO-1-(1-HYDROXYCYCLOHEXYL)ETHYL]PHENYL 4-METHYL-BENZOATE HYDROCHLORIDE, METHODS FOR PREPARING THE SAME AND USE OF THE SAME 有权4- [2-二甲基氨基-1-（1-羟基环己基）乙基]苯基4-甲基苯甲酸酯盐酸盐的聚合物，其制备方法和使用方法公开(公告)号：US20130281531A1
公开(公告)日：2013-10-24
申请号：US13846773
申请日：2013-03-18
发明人： Youxin Li , Wanhui Liu , Yang Lv , Guanhua Du , Qingguo Meng , Mina Yang , Fengmei Zhou , Ju Li , Xuemei Zhang
IPC分类号： C07C219/28
CPC分类号： C07C215/64 , A61K31/235 , C07B2200/13 , C07C213/10 , C07C215/20 , C07C219/28
摘要： The present disclosure relates to polymorphs of 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride, methods for preparing the same and use of the same.
摘要翻译： 本公开涉及4- [2-二甲基氨基-1-（1-羟基环己基）乙基] -4-甲基苯甲酸苯酯盐酸盐的多晶型物，其制备方法及其用途。
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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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![Polymorphs of 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride, methods of preparing the same and use of the same](/abs-image/US/2015/12/01/US09199912B2/abs.jpg.150x150.jpg)
9.发明授权Polymorphs of 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride, methods of preparing the same and use of the same 有权4- [2-二甲基氨基-1-（1-羟基环己基）乙基]苯基-4-甲基苯甲酸盐酸盐的多晶型物，其制备方法及其用途公开(公告)号：US09199912B2
公开(公告)日：2015-12-01
申请号：US14259964
申请日：2014-04-23
发明人： Youxin Li , Wanhui Liu , Yang Lv , Guanhua Du , Qingguo Meng , Mina Yang , Fengmei Zhou , Ju Li , Xuemei Zhang
IPC分类号： A61K31/235 , C07C213/10 , C07C215/20 , C07C215/64 , C07C219/28
CPC分类号： C07C215/64 , A61K31/235 , C07B2200/13 , C07C213/10 , C07C215/20 , C07C219/28
摘要： The present disclosure relates to polymorphs of 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride, methods for preparing the same and use of the same.
摘要翻译： 本公开涉及4- [2-二甲基氨基-1-（1-羟基环己基）乙基] -4-甲基苯甲酸苯酯盐酸盐的多晶型物，其制备方法及其用途。
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公开(公告)号：US20180036246A1
公开(公告)日：2018-02-08
申请号：US15789091
申请日：2017-10-20
发明人： Wei Sun , Xuemei Zhang , Tao Wang , Guangyi Leng , Kaoxiang Sun , Youxin Li , Wanhui Liu
CPC分类号： A61K9/1647 , A61K9/1641 , A61K9/1682 , A61K9/1694 , A61K38/09
摘要： A composition of goserelin sustained release microspheres is provided. The microspheres comprise goserelin, at least one poly (lactide-co-glycolide) and poloxamer or PEG. The sustained release microspheres have comparatively high bioavailability, which promotes the drug taking its full effect and have entrapment efficiency over 90%.
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