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1. 发明授权

US08545887B2 Modified release dosage forms 有权
标题翻译：改性释放剂型
公开(公告)号：US08545887B2
公开(公告)日：2013-10-01
申请号：US10476530
申请日：2002-09-28
申请人： Harry S. Sowden , David Wynn , Shun-Por Li , Der-Yang Lee , Martin Thomas
发明人： Harry S. Sowden , David Wynn , Shun-Por Li , Der-Yang Lee , Martin Thomas
IPC分类号： A61J3/06 , A61K9/20 , B30B11/00 , A61K9/24 , G06F17/30
CPC分类号： A23G3/04 , A23G1/54 , A23G3/0029 , A23G3/368 , A23G3/54 , A23L29/30 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0004 , A61K9/0056 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2068 , A61K9/2072 , A61K9/2081 , A61K9/209 , A61K9/2095 , A61K9/282 , A61K9/2826 , A61K9/284 , A61K9/286 , A61K9/2873 , A61K9/2886 , A61K9/2893 , A61K9/5084 , B30B11/08 , B30B11/34 , B30B15/302 , Y10T428/1352
摘要： A dosage form comprises: (a) at least one active ingredient: (b) a core having a first surface portion upon which resides a first coating and a second surface portion which is substantially free of the first coating; and (c) a shell which resides upon at least a portion of the second surface portion, wherein the shell comprises a different material from the first coating. In another embodiment, the dosage form comprises: (a) at least one active ingredient; (b) a core comprising a center portion having an exterior surface and an annular portion having an exterior surface and an interior surface, wherein the annular portion interior surface is in contact with at least a portion of the center portion exterior surface, and a coating resides on at least a portion of the annular portion exterior surface; and (c) a shell which resides upon at least a portion of the exterior surface of the center portion, wherein the shell comprises a different material than the impermeable coating. In another embodiment, the dosage form comprises: (a) at least one active ingredient; (b) a core having an outer surface and a cavity which extends at least partially through the core such that the core outer surface has at least a first opening therein; (c) a first coating which resides on at least a portion of the core outer surface, wherein the first shell portion comprises a different material from the first coating; and (d) a first shell portion which is adjacent to the first opening and covers at least the first opening.
摘要翻译：剂型包括：（a）至少一种活性成分：（b）具有第一表面部分的核心，其上存在第一涂层和基本上不含第一涂层的第二表面部分; 和（c）位于第二表面部分的至少一部分上的外壳，其中外壳包括与第一涂层不同的材料。在另一个实施方案中，剂型包含：（a）至少一种活性成分; （b）芯部，其包括具有外表面的中心部分和具有外表面和内表面的环形部分，其中所述环形部分内表面与所述中心部分外表面的至少一部分接触，位于环形部分外表面的至少一部分上; 和（c）驻留在中心部分的外表面的至少一部分上的壳体，其中壳体包括与不可渗透涂层不同的材料。在另一个实施方案中，剂型包含：（a）至少一种活性成分; （b）具有外表面和空腔的芯体，其至少部分地穿过所述芯部，使得所述芯部外表面至少具有第一开口; （c）驻留在所述芯外表面的至少一部分上的第一涂层，其中所述第一壳部分包括与所述第一涂层不同的材料; 和（d）与第一开口相邻并且至少覆盖第一开口的第一壳体部分。

2. 发明授权

US07968120B2 Modified release dosage forms 有权
标题翻译：改性释放剂型
公开(公告)号：US07968120B2
公开(公告)日：2011-06-28
申请号：US10477334
申请日：2002-09-28
申请人： Shun-Por Li , Harry S Sowden , David Wynn , Der-Yang Lee , Martin Thomas
发明人： Shun-Por Li , Harry S Sowden , David Wynn , Der-Yang Lee , Martin Thomas
IPC分类号： A61K9/22 , A61K9/16
CPC分类号： A23G3/04 , A23G1/54 , A23G3/0029 , A23G3/368 , A23G3/54 , A23L29/30 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0004 , A61K9/0056 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2068 , A61K9/2072 , A61K9/2081 , A61K9/209 , A61K9/2095 , A61K9/282 , A61K9/2826 , A61K9/284 , A61K9/286 , A61K9/2873 , A61K9/2886 , A61K9/2893 , A61K9/5084 , B30B11/08 , B30B11/34 , B30B15/302 , Y10T428/1352
摘要： In one embodiment a dosage form comprises at least one active ingredient and a molded matrix which comprises 10-100% of a material having a melting point of less than about 100 degrees C. selected from the stamp consisting of thermoplastic polyalkylene oxides, low melting hydrophobic materials, thermoplastic polymers, thermoplastic starches and combinations thereof, and the matrix is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium. The dosage form may additionally comprise uncoated particles which may contain at least one active ingredient. In another embodiment, a dosage form comprises at least one active ingredient, a plurality of particles and a molded matrix, wherein at least a portion of the particles are coated. The coated particles, the matrix or both may comprise at least one active ingredient, and the coated particles or the matrix or a combination thereof is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium.
摘要翻译：在一个实施方案中，剂型包含至少一种活性成分和模塑基质，其包含10-100％的熔点小于约100℃的材料，其选自热塑性聚环氧烷，低熔点疏水性材料，热塑性聚合物，热塑性淀粉及其组合，并且所述基质能够在剂型与液体介质接触时提供活性成分的改性释放。剂型还可以包含可以含有至少一种活性成分的未涂覆的颗粒。在另一个实施方案中，剂型包含至少一种活性成分，多个颗粒和模制基质，其中至少一部分颗粒被涂覆。涂覆的颗粒，基质或两者可以包含至少一种活性成分，并且涂覆的颗粒或基质或其组合能够在剂型与液体介质接触时提供活性成分的改性释放。

3. 发明申请

US20090155372A1 METHOD OF MANUFACTURING MODIFIED RELEASE DOSAGE FORMS 有权
标题翻译：制造改良释放剂量形式的方法
公开(公告)号：US20090155372A1
公开(公告)日：2009-06-18
申请号：US12391475
申请日：2009-02-24
申请人： SHUN-POR LI , Harry S. Sowden , David Wynn , Der-Yang Lee , Martin Thomas
发明人： SHUN-POR LI , Harry S. Sowden , David Wynn , Der-Yang Lee , Martin Thomas
IPC分类号： A61K9/52 , A61K47/30 , A61P43/00
CPC分类号： A23G3/04 , A23G1/54 , A23G3/0029 , A23G3/368 , A23G3/54 , A23L29/30 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0004 , A61K9/0056 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2068 , A61K9/2072 , A61K9/2081 , A61K9/209 , A61K9/2095 , A61K9/282 , A61K9/2826 , A61K9/284 , A61K9/286 , A61K9/2873 , A61K9/2886 , A61K9/2893 , A61K9/5084 , B30B11/08 , B30B11/34 , B30B15/302 , Y10T428/1352
摘要： In one embodiment a dosage form comprises at least one active ingredient and a molded matrix which comprises 10-100% of a material having a melting point of less than about 100 degrees C. selected from the stamp consisting of thermoplastic polyalkylene oxides, low melting hydrophobic materials, thermoplastic polymers, thermoplastic starches and combinations thereof, and the matrix is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium. The dosage form may additionally comprise uncoated particles which may contain at least one active ingredient. In another embodiment, a dosage form comprises at least one active ingredient, a plurality of particles and a molded matrix, wherein at least a portion of the particles are coated. The coated particles, the matrix or both may comprise at least one active ingredient, and the coated particles or the matrix or a combination thereof is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium.
摘要翻译：在一个实施方案中，剂型包含至少一种活性成分和模塑基质，其包含10-100％的熔点小于约100℃的材料，其选自热塑性聚环氧烷，低熔点疏水性材料，热塑性聚合物，热塑性淀粉及其组合，并且所述基质能够在剂型与液体介质接触时提供活性成分的改性释放。剂型还可以包含可以含有至少一种活性成分的未涂覆的颗粒。在另一个实施方案中，剂型包含至少一种活性成分，多个颗粒和模制基质，其中至少一部分颗粒被涂覆。涂覆的颗粒，基质或两者可以包含至少一种活性成分，并且涂覆的颗粒或基质或其组合能够在剂型与液体介质接触时提供活性成分的改性释放。

4. 发明申请

US20090186082A1 METHOD OF MANUFACTURING MODIFIED RELEASE DOSAGE FORMS 审中-公开
标题翻译：制造改良释放剂量形式的方法
公开(公告)号：US20090186082A1
公开(公告)日：2009-07-23
申请号：US12360579
申请日：2009-01-27
申请人： Shun-Por LI , David Wynn , Narendra Parikh , Dan McTeigue , Harry S. Sowden , Martin Thomas , Der-Yang Lee
发明人： Shun-Por LI , David Wynn , Narendra Parikh , Dan McTeigue , Harry S. Sowden , Martin Thomas , Der-Yang Lee
IPC分类号： A61K9/22
CPC分类号： A61J3/10 , A23G3/04 , A23G3/368 , A61J3/005 , A61K9/2853 , A61K9/2873 , A61K9/2893 , B30B11/08 , B30B11/34
摘要： In one embodiment, a dosage form comprises: (a) at least one active ingredient; (b) a molded core which is solid at room temperature; and (c) a shell which is in contact with at least a portion of the core, wherein the dosage form provides modified release of the active ingredient upon contacting of the dosage form with a liquid medium. In another embodiment of this invention, a dosage form comprises: (a) at least one active ingredient; (b) a molded core comprising a plurality of particles; and (c) a shell which is in contact with at least a portion of the core, wherein the dosage form provides modified release of the active ingredient upon contacting of the dosage form with a liquid medium.
摘要翻译：在一个实施方案中，剂型包含：（a）至少一种活性成分; （b）在室温下为固体的模制芯; 和（c）与芯的至少一部分接触的壳，其中所述剂型在剂型与液体介质接触时提供活性成分的改性释放。在本发明的另一个实施方案中，剂型包含：（a）至少一种活性成分; （b）包含多个颗粒的成型芯; 和（c）与芯的至少一部分接触的壳，其中所述剂型在剂型与液体介质接触时提供活性成分的改性释放。

5. 发明授权

US07972624B2 Method of manufacturing modified release dosage forms 有权
标题翻译：制备改性释放剂型的方法
公开(公告)号：US07972624B2
公开(公告)日：2011-07-05
申请号：US12391475
申请日：2009-02-24
申请人： Shun-Por Li , Harry S. Sowden , David Wynn , Der-Yang Lee , Martin Thomas
发明人： Shun-Por Li , Harry S. Sowden , David Wynn , Der-Yang Lee , Martin Thomas
IPC分类号： A61K9/22 , A23G3/02
CPC分类号： A23G3/04 , A23G1/54 , A23G3/0029 , A23G3/368 , A23G3/54 , A23L29/30 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0004 , A61K9/0056 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2068 , A61K9/2072 , A61K9/2081 , A61K9/209 , A61K9/2095 , A61K9/282 , A61K9/2826 , A61K9/284 , A61K9/286 , A61K9/2873 , A61K9/2886 , A61K9/2893 , A61K9/5084 , B30B11/08 , B30B11/34 , B30B15/302 , Y10T428/1352
摘要： In one embodiment a dosage form comprises at least one active ingredient and a molded matrix which comprises 10-100% of a material having a melting point of less than about 100 degrees C. selected from the stamp consisting of thermoplastic polyalkylene oxides, low melting hydrophobic materials, thermoplastic polymers, thermoplastic starches and combinations thereof, and the matrix is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium. The dosage form may additionally comprise uncoated particles which may contain at least one active ingredient. In another embodiment, a dosage form comprises at least one active ingredient, a plurality of particles and a molded matrix, wherein at least a portion of the particles are coated. The coated particles, the matrix or both may comprise at least one active ingredient, and the coated particles or the matrix or a combination thereof is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium.
摘要翻译：在一个实施方案中，剂型包含至少一种活性成分和模塑基质，其包含10-100％的熔点小于约100℃的材料，其选自热塑性聚环氧烷，低熔点疏水性材料，热塑性聚合物，热塑性淀粉及其组合，并且所述基质能够在剂型与液体介质接触时提供活性成分的改性释放。剂型还可以包含可以含有至少一种活性成分的未涂覆的颗粒。在另一个实施方案中，剂型包含至少一种活性成分，多个颗粒和模制基质，其中至少一部分颗粒被涂覆。涂覆的颗粒，基质或两者可以包含至少一种活性成分，并且涂覆的颗粒或基质或其组合能够在剂型与液体介质接触时提供活性成分的改性释放。

6. 发明授权

US07838026B2 Burst-release polymer composition and dosage forms comprising the same 有权
标题翻译：爆破性聚合物组合物和包含其的剂型
公开(公告)号：US07838026B2
公开(公告)日：2010-11-23
申请号：US10695347
申请日：2003-10-28
申请人： Shun-Por Li , Der-Yang Lee , Frank J. Bunick , Jen Chi Chen , Harry S. Sowden
发明人： Shun-Por Li , Der-Yang Lee , Frank J. Bunick , Jen Chi Chen , Harry S. Sowden
IPC分类号： A61K9/20 , A61K9/30 , A61K9/32 , A61K9/48 , A61K9/56
CPC分类号： A23G3/368 , A23G3/04 , A61J3/06 , A61J3/10 , A61K9/0056 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2068 , A61K9/2081 , A61K9/209 , A61K9/2095 , A61K9/282 , A61K9/2826 , A61K9/284 , A61K9/286 , A61K9/2873 , A61K9/2886 , A61K9/2893 , A61K9/5084 , B30B11/08 , B30B11/34 , B30B15/302
摘要： A composition comprising a high molecular weight, water soluble polymer having a cloud point from about 20 to about 90° C. and at least one carrageenan is provided. The composition may be used as a component of a pharmaceutical dosage form, such as the shell of a dosage form, to provide burst release of active ingredient contained therein.
摘要翻译：提供包含高分子量水溶性聚合物的组合物，其具有约20至约90℃的浊点和至少一种卡拉胶。组合物可以用作药物剂型的组分，例如剂型的壳，以提供其中所含的活性成分的爆发释放。

7. 发明申请

US20050266084A1 Modified release dosage forms 有权
标题翻译：改性释放剂型
公开(公告)号：US20050266084A1
公开(公告)日：2005-12-01
申请号：US10477334
申请日：2002-09-28
申请人： Shun-Por Li , Harry Sowden , David Wynn , Der-Yang Lee
发明人： Shun-Por Li , Harry Sowden , David Wynn , Der-Yang Lee
IPC分类号： A23G3/34 , A23G1/00 , A23G1/54 , A23G3/00 , A23G3/04 , A23G3/36 , A23G3/54 , A23L1/00 , A23L1/09 , A23L1/30 , A61J3/00 , A61J3/06 , A61J3/10 , A61K9/00 , A61K9/14 , A61K9/20 , A61K9/22 , A61K9/24 , A61K9/26 , A61K9/28 , A61K9/30 , A61K9/32 , A61K9/34 , A61K9/36 , A61K9/38 , A61K9/48 , A61K9/50 , A61K31/136 , A61K31/137 , A61K31/277 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/30 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/44 , A61K47/46 , A61P11/00 , B30B11/08 , B30B11/34 , B30B15/30 , G06F17/30
CPC分类号： A23G3/04 , A23G1/54 , A23G3/0029 , A23G3/368 , A23G3/54 , A23L29/30 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0004 , A61K9/0056 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2068 , A61K9/2072 , A61K9/2081 , A61K9/209 , A61K9/2095 , A61K9/282 , A61K9/2826 , A61K9/284 , A61K9/286 , A61K9/2873 , A61K9/2886 , A61K9/2893 , A61K9/5084 , B30B11/08 , B30B11/34 , B30B15/302 , Y10T428/1352
摘要： In one embodiment a dosage form comprises at least one active ingredient and a molded matrix which comprises 10-100% of a material having a melting point of less than about 100 degrees C. selected from the stamp consisting of thermoplastic polyalkylene oxides, low melting hydrophobic materials, thermoplastic polymers, thermoplastic starches and combinations thereof, and the matrix is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium. The dosage form may additionally comprise uncoated particles which may contain at least one active ingredient. In another embodiment, a dosage form comprises at least one active ingredient, a plurality of particles and a molded matrix, wherein at least a portion of the particles are coated. The coated particles, the matrix or both may comprise at least one active ingredient, and the coated particles or the matrix or a combination thereof is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium.
摘要翻译：在一个实施方案中，剂型包含至少一种活性成分和模塑基质，其包含10-100％的熔点小于约100℃的材料，其选自热塑性聚环氧烷，低熔点疏水性材料，热塑性聚合物，热塑性淀粉及其组合，并且所述基质能够在剂型与液体介质接触时提供活性成分的改性释放。剂型还可以包含可以含有至少一种活性成分的未涂覆的颗粒。在另一个实施方案中，剂型包含至少一种活性成分，多个颗粒和模制基质，其中至少一部分颗粒被涂覆。涂覆的颗粒，基质或两者可以包含至少一种活性成分，并且涂覆的颗粒或基质或其组合能够在剂型与液体介质接触时提供活性成分的改性释放。

8. 发明授权

US07807197B2 Composite dosage forms having an inlaid portion 有权
标题翻译：具有镶嵌部分的复合剂型
公开(公告)号：US07807197B2
公开(公告)日：2010-10-05
申请号：US10476388
申请日：2002-09-28
申请人： Der-Yang Lee , Harry S. Sowden , Martin Thomas
发明人： Der-Yang Lee , Harry S. Sowden , Martin Thomas
IPC分类号： A61K9/20 , A61K9/28 , A61K9/24
CPC分类号： A61K9/209 , A61K9/2072 , A61K9/2086 , A61K9/2095 , A61K9/2893
摘要： A dosage form comprises at least one active ingredient, a first portion which comprises an exterior surface and one or more cavities defining at least one interior surface having indentations and an exterior surface, and a second molded portion which is inlaid into the cavities of the first portion and has an exterior surface. The first and second portions are in contact at an interface, the second portion comprises a solidified thermoplastic material, and the second portion resides substantially conformally upon the indentations of the first portion. In another embodiment, a dosage form comprises at least one active ingredient, a core having an outer surface and a shell residing on at least a portion of the core outer surface, wherein the shell comprises a first shell portion and a second molded shell portion which is inlaid into the first shell portion. In another embodiment, a dosage form comprises at least one active ingredient, a core, and a shell having a first molded shell portion which is discontinuous, and a second molded shell portion which is continuous, such that the discontinuities of the first shell portion are due to the presence of the second molded shell portion, and the first and second shell portions are compositionally different.
摘要翻译：剂型包括至少一种活性成分，第一部分包括外表面和限定至少一个具有凹痕和外表面的内表面的一个或多个空腔，以及第二模制部分，其嵌入第一并具有外表面。第一部分和第二部分在界面处接触，第二部分包括凝固的热塑性材料，第二部分基本上保持在第一部分的凹陷上。在另一个实施方案中，剂型包含至少一种活性成分，具有外表面的芯和位于芯外表面的至少一部分上的壳，其中所述壳包括第一壳部分和第二模制壳部分，嵌入第一壳部分。在另一个实施方案中，剂型包含至少一种活性成分，核心和壳，其具有不连续的第一模塑壳部分和连续的第二模制壳部分，使得第一壳部分的不连续性为由于存在第二模制壳体部分，并且第一和第二壳部分在组成上是不同的。

9. 发明申请

US20100112052A1 OSMOTIC TABLET WITH A COMPRESSED OUTER COATING 审中-公开
标题翻译：具有压缩外涂层的OSMOTIC板
公开(公告)号：US20100112052A1
公开(公告)日：2010-05-06
申请号：US12607248
申请日：2009-10-28
申请人： Vincent Chen , Shun-Por Li , Robert Shen , Der-Yang Lee
发明人： Vincent Chen , Shun-Por Li , Robert Shen , Der-Yang Lee
IPC分类号： A61K9/22 , A61K31/135 , A61K31/495
CPC分类号： A61K9/209 , A61K9/0004
摘要： The present invention features a method of manufacturing an osmotic tablet including the steps of (i) compressing a tablet core including a first pharmaceutically active agent and a hydrophilic polymer; (ii) applying an osmotic coating to the outer surface of the tablet core to form a coated tablet, wherein the osmotic coating includes at least one opening exposing the tablet core; and (iii) compressing an immediate release coating onto the surface of the coated tablet, wherein the release coating includes a second pharmaceutically active agent.
摘要翻译：本发明的特征在于一种制造渗透性片剂的方法，包括以下步骤：（i）压缩包含第一药物活性剂和亲水性聚合物的片芯; （ii）将渗透涂层施加到片芯的外表面以形成包衣片，其中所述渗透涂层包括暴露片芯的至少一个开口; 和（iii）将即时释放涂层压缩到所述包衣片剂的表面上，其中所述剥离包衣包含第二药物活性剂。

10. 发明申请

US20080206337A1 METHOD OF MAKING DOSAGE FORMS COMPRISING POLYMERIC COMPOSITIONS 审中-公开
标题翻译：制备包含聚合物组合物的剂型的方法
公开(公告)号：US20080206337A1
公开(公告)日：2008-08-28
申请号：US12061765
申请日：2008-04-03
申请人： Hai Yong Huang , Der-Yang Lee , Shun Por Li
发明人： Hai Yong Huang , Der-Yang Lee , Shun Por Li
IPC分类号： A61K9/00
CPC分类号： A61K9/0004 , A61K9/286 , A61K9/2866 , A61K31/137
摘要： A dosage form comprises: (a) at least one active ingredient; (b) a core having an outer surface; and (c) a shell which resides upon at least a portion of the core outer surface, wherein at least a portion of the shell is semipermeable, such that the liquid medium diffuses through the semipermeable shell or shell portion to the core due to osmosis. The shell also provides for delivery of the active ingredient to a liquid medium outside the shell after contacting of the dosage form with the liquid medium. The dosage form delivers one or more active ingredients in a controlled manner upon contacting of the dosage form with a liquid medium. The dosage form may be employed to provide a burst release of the active ingredient, or to provide release of the active ingredient at an ascending release rate over an extended time period upon contacting of the dosage form with a liquid medium. At least a portion of the shell may be comprised of a polymeric composition containing film former, gelling agents, which can be dissolved in a multisolvent system comprised of water and an organic solvent.
摘要翻译：剂型包括：（a）至少一种活性成分; （b）具有外表面的芯; 和（c）位于所述芯外表面的至少一部分上的壳，其中所述壳的至少一部分是半透性的，使得所述液体介质由于渗透而扩散通过所述半透性壳或壳部分到所述芯。壳体还提供了在剂型与液体介质接触之后将活性成分递送到壳外的液体介质。剂型在剂型与液体培养基接触时以受控的方式递送一种或多种活性成分。剂型可以用于提供活性成分的爆发释放，或者当剂型与液体介质接触时，在延长的释放速率下提供活性成分的释放。壳的至少一部分可以由含有成膜剂，胶凝剂的聚合物组合物组成，其可以溶解在由水和有机溶剂组成的多溶剂体系中。

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