公开(公告)号：EP0942715A1

公开(公告)日：1999-09-22

申请号：EP97918661.0

申请日：1997-04-15

申请人： FMC CORPORATION

发明人： KARETNY, Marc, S. ,  ERKOBONI, David, F. ,  VALDYKA, Ronald, S., Jr. ,  STAMATO, Howard, J.

IPC分类号： A61K9

CPC分类号： A61K9/2054

摘要： The present invention provides a method for preparing a spray-dried compressible granular formulation for preparing pharmaceutical tablets in which hydrolyzed cellulose is used as a granulation aid, the resulting granulations, and pharmaceutical tablets compressed from such granules. In these formulations there is employed from 1 to 97 % by weight pharmaceutical active, from about 3 to 99 % by weight hydrolyzed cellulose, based on the dry weight of the granulation, and optionally conventional granulation and/or tableting additives such as surfactants, disintegrants and antiadherents/flow aids.

公开(公告)号：EP1163234A1

公开(公告)日：2001-12-19

申请号：EP00918139.7

申请日：2000-03-20

申请人： FMC CORPORATION

发明人： ERKOBONI, David, F. ,  VLADYKA, Ronald, S., Jr. ,  STERGIOS, Pamela, R.

IPC分类号： C07D293/00 ,  C07D421/00 ,  C07D517/00 ,  A01N45/00 ,  A01N43/50 ,  A61K31/56 ,  A61K31/415

CPC分类号： A61K9/145 ,  A61K9/1617 ,  A61K9/1652 ,  A61K31/496 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.