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1. 发明申请

US20120294939A1 DIRECT COMPRESSION FORMULATION AND PROCESS 审中-公开
标题翻译：直接压缩配方和工艺
公开(公告)号：US20120294939A1
公开(公告)日：2012-11-22
申请号：US13562415
申请日：2012-07-31
申请人： James Kowalski , Jay Parthiban Lakshman , Arun P. Patal
发明人： James Kowalski , Jay Parthiban Lakshman , Arun P. Patal
IPC分类号： A61K9/20 , C07D207/16 , A61P19/10 , A61P3/04 , A61P19/02 , A61P37/08 , A61K31/40 , A61P3/10
CPC分类号： A61K9/2077 , A61K9/2013 , A61K9/2054 , A61K9/2059 , A61K9/2095 , A61K31/40 , C07D207/16 , Y10T428/268
摘要： Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of direct compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus present formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
摘要翻译：可以是98.5-100％纯度的二肽基肽酶IV抑制剂（本文中称为DPP-IV）是能够用特定赋形剂直接压制成销售形式剂型的高剂量药物，例如具有所需硬度，崩解性的片剂和胶囊能力和可接受的溶出特性。 DPP-IV不是固有的可压缩性，因此存在配方问题。制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。最佳流量有助于均匀的模头填充和重量控制。使用的粘合剂确保足够的内聚性质，使DPP-IV能够使用直接压缩方法进行压缩。所制备的片剂提供可接受的体外溶出曲线。

2. 发明申请

US20080227825A1 Formulation 审中-公开
标题翻译：公式
公开(公告)号：US20080227825A1
公开(公告)日：2008-09-18
申请号：US12067346
申请日：2006-09-25
申请人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
发明人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
IPC分类号： A61K31/4436 , A61K31/40 , A61P3/08 , A61K31/155
CPC分类号： A61K9/2095 , A61K9/2054 , A61K9/2072 , A61K9/209 , A61K9/2893 , A61K31/155 , A61K31/40 , A61K31/4439 , A61K45/06 , A61K2300/00
摘要： This invention relates to a formulation comprising a dipeptidylpeptidase IV (DPP-IV) inhibitor preferably vildagliptin and metformin, to tablets comprising such formulations and to processes for the preparation thereof.
摘要翻译：本发明涉及包含二肽基肽酶IV（DPP-IV）抑制剂，优选维格列汀和二甲双胍的制剂，其包含该制剂的片剂及其制备方法。

3. 发明申请

US20110045062A1 FORMULATION 审中-公开
标题翻译：公式
公开(公告)号：US20110045062A1
公开(公告)日：2011-02-24
申请号：US12939450
申请日：2010-11-04
申请人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
发明人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
IPC分类号： A61K31/40 , A61K31/155 , A61K9/48 , A61K31/4439 , A61P3/10 , A61P19/02 , A61P3/04 , A61P19/10
CPC分类号： A61K9/2095 , A61K9/2054 , A61K9/2072 , A61K9/209 , A61K9/2893 , A61K31/155 , A61K31/40 , A61K31/4439 , A61K45/06 , A61K2300/00
摘要： This invention relates to a formulation comprising a dipeptidylpeptidase IV (DPP-IV) inhibitor preferably vildagliptin and metformin, to tablets comprising such formulations and to processes for the preparation thereof.
摘要翻译：本发明涉及包含二肽基肽酶IV（DPP-IV）抑制剂，优选维格列汀和二甲双胍的制剂，其包含该制剂的片剂及其制备方法。

4. 发明申请

US20140287040A1 Formulation 审中-公开
标题翻译：公式
公开(公告)号：US20140287040A1
公开(公告)日：2014-09-25
申请号：US14296660
申请日：2014-06-05
申请人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
发明人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
IPC分类号： A61K9/20 , A61K31/155 , A61K9/28 , A61K31/40
CPC分类号： A61K9/2095 , A61K9/2054 , A61K9/2072 , A61K9/209 , A61K9/2893 , A61K31/155 , A61K31/40 , A61K31/4439 , A61K45/06 , A61K2300/00
摘要： This invention relates to a formulation comprising a dipeptidylpeptidase IV (DPP-IV) inhibitor preferably vildagliptin and metformin, to tablets comprising such formulations and to processes for the preparation thereof.
摘要翻译：本发明涉及包含二肽基肽酶IV（DPP-IV）抑制剂，优选维格列汀和二甲双胍的制剂，其包含该制剂的片剂及其制备方法。

5. 发明申请

US20140205663A1 Direct Compression Formulation and Process 审中-公开
标题翻译：直接压缩配方和工艺
公开(公告)号：US20140205663A1
公开(公告)日：2014-07-24
申请号：US14226871
申请日：2014-03-27
申请人： James Kowalski , Jay Parthiban LakShman , Arun P. Patel
发明人： James Kowalski , Jay Parthiban LakShman , Arun P. Patel
IPC分类号： A61K9/20 , A61K31/40 , C07D207/16
CPC分类号： A61K9/2077 , A61K9/2013 , A61K9/2054 , A61K9/2059 , A61K9/2095 , A61K31/40 , C07D207/16 , Y10T428/268
摘要： Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of direct compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus present formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
摘要翻译：可以是98.5-100％纯度的二肽基肽酶IV抑制剂（本文中称为DPP-IV）是能够用特定赋形剂直接压制成销售形式剂型的高剂量药物，例如具有所需硬度，崩解性的片剂和胶囊能力和可接受的溶出特性。 DPP-IV不是固有的可压缩性，因此存在配方问题。制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。最佳流量有助于均匀的模头填充和重量控制。使用的粘合剂确保足够的内聚性质，使DPP-IV能够使用直接压缩方法进行压缩。所制备的片剂提供可接受的体外溶出曲线。

6. 发明申请

US20130052239A1 Formulation 审中-公开
标题翻译：公式
公开(公告)号：US20130052239A1
公开(公告)日：2013-02-28
申请号：US13602735
申请日：2012-09-04
申请人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
发明人： Yatindra Joshi , James Kowalski , Jay Parthiban Lakshman , Alan Edward Royce , Wei-Qin Tong , Madhav Vasanthavada
IPC分类号： A61K31/40 , A61K31/4439 , A61P3/10 , A61K9/48
CPC分类号： A61K9/2095 , A61K9/2054 , A61K9/2072 , A61K9/209 , A61K9/2893 , A61K31/155 , A61K31/40 , A61K31/4439 , A61K45/06 , A61K2300/00
摘要： This invention relates to a formulation comprising a dipeptidylpeptidase IV (DPP-IV) inhibitor preferably vildagliptin and metformin, to tablets comprising such formulations and to processes for the preparation thereof.
摘要翻译：本发明涉及包含二肽基肽酶IV（DPP-IV）抑制剂，优选维格列汀和二甲双胍的制剂，其包含该制剂的片剂及其制备方法。

7. 发明申请

US20110236479A1 DIRECT COMPRESSION FORMULATION AND PROCESS 审中-公开
标题翻译：直接压缩配方和工艺
公开(公告)号：US20110236479A1
公开(公告)日：2011-09-29
申请号：US13154063
申请日：2011-06-06
申请人： James Kowalski , Jay Parthiban Lakshman , Arun P. Patel
发明人： James Kowalski , Jay Parthiban Lakshman , Arun P. Patel
IPC分类号： A61K9/20 , A61K31/40 , A61P3/10 , A61P19/02 , A61P3/04 , A61P19/10 , B32B5/16 , B29C67/24
CPC分类号： A61K9/2077 , A61K9/2013 , A61K9/2054 , A61K9/2059 , A61K9/2095 , A61K31/40 , C07D207/16 , Y10T428/268
摘要： Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
摘要翻译：可以为98.5-100％纯度的二肽基肽酶IV抑制剂（本文称为DPP-IV）是能够用特定赋形剂直接压制成销售形式剂型的高剂量药物，例如具有所需硬度，分解能力和可接受的溶解特性。 DPP-IV不是固有的可压缩性，因此呈现配方问题。制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。最佳流量有助于均匀的模头填充和重量控制。使用的粘合剂确保足够的内聚性质，使DPP-IV能够使用直接压缩方法进行压缩。所制备的片剂提供可接受的体外溶出曲线。

8. 发明申请

US20090148522A1 HEATED ROLLER COMPACTION PROCESS FOR MAKING PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：用于制造药物组合物的加热辊压缩方法
公开(公告)号：US20090148522A1
公开(公告)日：2009-06-11
申请号：US12299036
申请日：2007-05-03
申请人： James Kowalski , Jay Parthiban Lakshman , Abu T.M. Serajuddin , Wei-Qin Tong
发明人： James Kowalski , Jay Parthiban Lakshman , Abu T.M. Serajuddin , Wei-Qin Tong
IPC分类号： A61K9/20
CPC分类号： A61K9/146 , A61K9/2054 , A61K9/2077
摘要： A process for using a heated roller compactor to prepare melt granulated composition of a therapeutic compound, especially a poorly compressible and/or moisture sensitive therapeutic compound, with a granulation excipient.
摘要翻译：一种使用加热辊压机的方法，用制粒赋形剂制备治疗化合物，特别是难以压缩和/或湿度敏感的治疗化合物的熔融颗粒组合物。

9. 发明申请

US20080193529A1 Direct Compression Formulation and Process 审中-公开
标题翻译：直接压缩配方和工艺
公开(公告)号：US20080193529A1
公开(公告)日：2008-08-14
申请号：US11916490
申请日：2006-06-08
申请人： James Kowalski , Jay Parthiban Lakshman , Arun Patel
发明人： James Kowalski , Jay Parthiban Lakshman , Arun Patel
IPC分类号： A61K9/20 , A61K31/4439 , A61K9/14 , A61K31/40
CPC分类号： A61K31/40 , A61K31/4439 , A61K45/06 , A61K2300/00
摘要： Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with a glitazone and specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
摘要翻译：可以为98.5-100％纯度的二肽基肽酶IV抑制剂（在本文中称为DPP-IV）是能够用格列酮和特定赋形剂直接压制成销售形式的剂型的高剂量药物，例如具有期望的片剂和胶囊，硬度，崩解性和可接受的溶解特性。 DPP-IV不是固有的可压缩性，因此呈现配方问题。制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。最佳流量有助于均匀的模头填充和重量控制。使用的粘合剂确保足够的内聚性质，使DPP-IV能够使用直接压缩方法进行压缩。所制备的片剂提供可接受的体外溶出曲线。

10. 发明申请

US20080038341A1 Direct Compression Formulation And Process 审中-公开
标题翻译：直接压缩配方和工艺
公开(公告)号：US20080038341A1
公开(公告)日：2008-02-14
申请号：US10586059
申请日：2005-01-17
申请人： James Kowalski , Jay Parthiban Lakshman , Arun P. Patel
发明人： James Kowalski , Jay Parthiban Lakshman , Arun P. Patel
IPC分类号： A61K9/20 , A61K31/4015 , A61K31/426 , A61K31/4439 , A61P3/00 , A61K31/47 , A61K47/38
CPC分类号： A61K9/2077 , A61K9/2013 , A61K9/2054 , A61K9/2059 , A61K9/2095 , A61K31/40 , C07D207/16 , Y10T428/268
摘要： Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
摘要翻译：可以为98.5-100％纯度的二肽基肽酶IV抑制剂（本文称为DPP-IV）是能够用特定赋形剂直接压制成销售形式剂型的高剂量药物，例如具有所需硬度，分解能力和可接受的溶解特性。 DPP-IV不是固有的可压缩性，因此呈现配方问题。制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。最佳流量有助于均匀的模头填充和重量控制。使用的粘合剂确保足够的内聚性质，使DPP-IV能够使用直接压缩方法进行压缩。所制备的片剂提供可接受的体外溶出曲线。

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