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1. 发明申请

US20120059011A1 PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE-4抑制剂与PIOGLITAZONE的组合药物组合物
公开(公告)号：US20120059011A1
公开(公告)日：2012-03-08
申请号：US13319718
申请日：2010-06-04
申请人： Nicholas Birringer , Christopher T. John , Adam Procopio , Bhagwant Rege , Lawrence A. Rosen , Sutthilug Sotthivirat , Wei Xu
发明人： Nicholas Birringer , Christopher T. John , Adam Procopio , Bhagwant Rege , Lawrence A. Rosen , Sutthilug Sotthivirat , Wei Xu
IPC分类号： A61K31/4439 , A61K31/513 , A61P3/10 , A61K31/4985
CPC分类号： A61K45/06 , A61K31/44 , A61K31/4439 , A61K2300/00
摘要： This invention relates to pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and pioglitazone, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.
摘要翻译：本发明涉及包含二肽基肽酶-4抑制剂和吡格列酮的固定剂量组合的药物组合物，制备这种药物组合物的方法，以及用这种药物组合物治疗2型糖尿病的方法。

2. 发明申请

US20120201885A1 PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE-4抑制剂与PIOGLITAZONE组合的药物组合物
公开(公告)号：US20120201885A1
公开(公告)日：2012-08-09
申请号：US13501252
申请日：2010-10-12
申请人： Nicholas Birringer , Christopher T. John , Zhen Liu , Adam Procopio , Bhagwant Rege
发明人： Nicholas Birringer , Christopher T. John , Zhen Liu , Adam Procopio , Bhagwant Rege
IPC分类号： A61K9/20 , A61K31/675 , A61P3/10 , A61K31/513 , A61K31/4439 , A61K9/28 , A61K31/4985
CPC分类号： A61K45/06 , A61K9/209
摘要： This invention relates to a bilayer pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and pioglitazone, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.
摘要翻译：本发明涉及包含二肽基肽酶-4抑制剂和吡格列酮的固定剂量组合的双层药物组合物，制备这种药物组合物的方法以及用这种药物组合物治疗2型糖尿病的方法。

3. 发明授权

US09339543B2 Pharmaceutical compositions that inhibit disproportionation 有权
标题翻译：抑制歧化的药物组合物
公开(公告)号：US09339543B2
公开(公告)日：2016-05-17
申请号：US14350839
申请日：2012-10-08
申请人： Christopher T. John , Paul A. Harmon
发明人： Christopher T. John , Paul A. Harmon
IPC分类号： A61K31/44 , A01N43/40 , A61K47/12 , A61K9/20 , A61K31/4439
CPC分类号： A61K47/12 , A61K9/2013 , A61K9/2054 , A61K31/4439
摘要： Pharmaceutical formulations comprising solid pharmaceutically acceptable organic acids, such as maleic acid or tartaric acid, that inhibit the disproportionation of pharmaceutically acceptable acid salts of active pharmaceutical ingredients, and methods of manufacturing such pharmaceutical compositions. The pharmaceutically acceptable acid salt of the active pharmaceutical ingredient has a pKa of less than about 6.0, and wherein the solid pharmaceutically acceptable organic acid has a pKa of less than about 4.0 and an aqueous solubility in the range of about 500 to about 2000 milligrams per milliliter. A pharmaceutical formulation comprising a pharmaceutical acceptable acid salt of pioglitazone, a solid pharmaceutically acceptable organic acid selected from the group consisting of maleic acid or tartaric acid, and an excipient that promotes disproportionation, wherein the ratio by weight of the solid pharmaceutically acceptable organic acid to excipient is from about 1:6 to about 1:1.
摘要翻译：包含抑制活性药物成分的药学上可接受的酸盐的歧化的固体药学上可接受的有机酸如马来酸或酒石酸的药物制剂，以及制造这种药物组合物的方法。活性药物成分的药学上可接受的酸盐的pKa小于约6.0，并且其中固体药学上可接受的有机酸的pKa小于约4.0，水溶解度在约500至约2000毫克/ 毫升。一种药物制剂，其包含吡格列酮的药学上可接受的酸性盐，选自马来酸或酒石酸的固体药学上可接受的有机酸和促进歧化的赋形剂，其中所述固体药学上可接受的有机酸的重量比赋形剂为约1:6至约1:1。

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