公开(公告)号：JPH1072400A

公开(公告)日：1998-03-17

申请号：JP16085497

申请日：1997-06-18

Applicant: BASF AG

Inventor： BREITENBACH JOERG DR ,  ROSENBERG JOERG DR ,  NEUMANN JOERG DR ,  ZEIDLER JUERGEN DR ,  SIMON DIRK DR ,  DIENER RALPH DR

IPC: A61K31/19 ,  A61K9/16 ,  A61K31/00 ,  B01J19/00 ,  C07C51/41 ,  C07C57/30 ,  C07C229/26

Abstract: PROBLEM TO BE SOLVED: To provide a method for producing a salt of a pharmaceutically active material without lowering a quality, especially fluidity by reacting an acid with a base in a molten liquid so that the acid may be reacted with at least stoichiometric amount of the base in an extruder. SOLUTION: The objective salt of a pharmaceutically active material is obtained by reacting (A) a carboxylic acid with (B) a base in a molten liquid so that the acid may be reacted with at least stoichiometric amount of the base in an extruder. The method is preferably used for production of a salt of a derivative of salicylic acid, e.g. acetylasalicylic acid, or an arylcarboxylic acid, e.g. diclofenac, tolmetin or zomepirac. A basic α-aminocarboxylic acid, especially ricin, a base of an alkali(ne earth) metal, etc., are preferable as the component B. The amount of the above base is at least stoichiometric amount, preferably 1-40mol% excess based on the acid.

公开(公告)号：EP0813904A2

公开(公告)日：1997-12-29

申请号：EP97109455

申请日：1997-06-11

Applicant: BASF AG

Inventor： BREITENBACH JOERG DR ,  ROSENBERG JOERG DR ,  NEUMANN JOERG DR ,  ZEIDLER JUERGEN DR ,  SIMON DIRK DR ,  DIENER RALPH DR

IPC: A61K31/19 ,  A61K9/16 ,  C07C51/41 ,  C07C57/30 ,  C07C229/26 ,  B01J19/00 ,  A61K31/00

CPC classification number: A61K9/1688 ,  C07C51/412 ,  C07C57/30

Abstract: Verfahren zur Herstellung von Salzen von Säuregruppen tragenden pharmazeutischen Wirkstoffen durch Umsetzung der Carbonsäuren mit einer Base in der Schmelze, indem man die Säuren mit einer mindestens stöchiometrischen Menge einer Base im Extruder umsetzt.

Abstract translation: 药学活性羧酸化合物的盐的制备包括在挤出机中与≥1以熔融形式的碱的化学计量等价物反应的酸。

公开(公告)号：DE19624607A1

公开(公告)日：1998-01-02

申请号：DE19624607

申请日：1996-06-20

Applicant: BASF AG

Inventor： BREITENBACH JOERG DR ,  ROSENBERG JOERG DR ,  NEUMANN JOERG DR ,  ZEIDLER JUERGEN DR ,  SIMON DIRK DR ,  DIENER RALPH DR

IPC: A61K31/19 ,  A61K9/16 ,  A61K31/00 ,  B01J19/00 ,  C07C51/41 ,  C07C57/30 ,  C07C229/26 ,  A61K31/195

Abstract: Preparation of a salt of a pharmaceutically active carboxylic acid compound comprises reacting the acid in an extruder with ≥ 1 stoichiometric equivalent of a base in melt form.

公开(公告)号：DE19536394A1

公开(公告)日：1997-04-03

申请号：DE19536394

申请日：1995-09-29

Applicant: BASF AG

Inventor： ZEIDLER JUERGEN DR ,  ROSENBERG JOERG DR ,  BREITENBACH JOERG DR ,  NEUMANN JOERG DR

IPC: A61K9/16 ,  A61K9/20 ,  A61K31/277 ,  A61K47/24 ,  A61K47/26 ,  A61K47/30 ,  A61K47/36 ,  A61K31/275 ,  A61J3/10

Abstract: The invention concerns solid medicaments obtained by extrusion with subsequent shaping of a solvent-free melt, containing in addition to one or a plurality of active substances: A) between 10 and 90 wt.% of a thermoplastically processable water-soluble polymer; B) between 5 and 85 wt.% isomalt; and C) between 0 and 5 wt.% lecithin, the total of all the contents equalling 100 wt.%.