公开(公告)号：US20110124879A1

公开(公告)日：2011-05-26

申请号：US12674642

申请日：2008-08-06

Applicant: Rajesh Kumar Thaper ,  Manoj Devilalji Prabhavat ,  Yogesh Dadaji Pawar ,  Pritesh R. Upadhyay

Inventor： Rajesh Kumar Thaper ,  Manoj Devilalji Prabhavat ,  Yogesh Dadaji Pawar ,  Pritesh R. Upadhyay

IPC: C07D209/88

CPC classification number: C07D209/88

Abstract: The present invention provides a novel stable amorphous form of carvedilol dihydrogen phosphate and the process for its preparation that involves reaction of carvedilol base with ortho phosphoric acid in the presence of stabilizer in a suitable solvent or mixture of solvents followed by concentration and isolation. An alternate process for preparation of amorphous form of carvedilol dihydrogen phosphate involves addition of stabiliser to the solution of stable amorphous or crystalline carvedilol dihydrogen phosphate in a suitable solvent or mixture of solvents followed by concentration and isolation. The novel stable amorphous form of carvedilol dihydrogen phosphate is highly stable.

Abstract translation: 本发明提供了一种新颖的卡维地洛磷酸二氢不稳定形式及其制备方法，其中包括在稳定剂存在下，在合适的溶剂或溶剂混合物中将卡维地洛碱与原磷酸反应，随后浓缩和分离。 用于制备无定形形式的卡维地洛磷酸二氢盐的替代方法包括在合适的溶剂或溶剂混合物中将稳定剂加入稳定的无定形或结晶卡维地洛二磷酸盐溶液中，然后浓缩和分离。 卡维地洛磷酸二氢盐的新型稳定无定形形式是高度稳定的。

公开(公告)号：US08278461B2

公开(公告)日：2012-10-02

申请号：US12674642

申请日：2008-08-06

Applicant: Rajesh Kumar Thaper ,  Manoj Devilalji Prabhavat ,  Yogesh Dadaji Pawar ,  Pritesh R. Upadhyay

Inventor： Rajesh Kumar Thaper ,  Manoj Devilalji Prabhavat ,  Yogesh Dadaji Pawar ,  Pritesh R. Upadhyay

IPC: C07D209/82

CPC classification number: C07D209/88

Abstract: The present invention provides a novel stable amorphous form of carvedilol dihydrogen phosphate and the process for its preparation that involves reaction of carvedilol base with ortho phosphoric acid in the presence of stabilizer in a suitable solvent or mixture of solvents followed by concentration and isolation. An alternate process for preparation of amorphous form of carvedilol dihydrogen phosphate involves addition of stabiliser to the solution of stable amorphous or crystalline carvedilol dihydrogen phosphate in a suitable solvent or mixture of solvents followed by concentration and isolation. The novel stable amorphous form of carvedilol dihydrogen phosphate is highly stable.

Abstract translation: 本发明提供了一种新颖的卡维地洛磷酸二氢不稳定形式及其制备方法，其中包括在稳定剂存在下，在合适的溶剂或溶剂混合物中将卡维地洛碱与原磷酸反应，随后浓缩和分离。 用于制备无定形形式的卡维地洛磷酸二氢盐的替代方法包括在合适的溶剂或溶剂混合物中将稳定剂加入稳定的无定形或结晶卡维地洛二磷酸盐溶液中，然后浓缩和分离。 卡维地洛磷酸二氢盐的新型稳定无定形形式是高度稳定的。