公开(公告)号：EP1071402A1

公开(公告)日：2001-01-31

申请号：EP99919195.0

申请日：1999-04-06

申请人： F. HOFFMANN-LA ROCHE AG

发明人： BAUSCH, Alexander ,  HIDBER, Pirmin

IPC分类号： A61K9/14 ,  A61K31/015 ,  C08J3/12 ,  B01J2/00 ,  B01J2/04 ,  B01J13/00 ,  B01F3/00 ,  B29B9/10

CPC分类号： B01F3/1214 ,  A61K9/14 ,  A61K9/145 ,  A61K9/1688 ,  B01F3/1271 ,  B01F5/0287 ,  B01F2003/0064 ,  B01F2003/125 ,  B01F2215/0032 ,  B01J2/04 ,  B01J3/008 ,  B01J13/02 ,  Y02P20/544 ,  Y10S977/906

摘要： The present invention relates to a process for manufacturing a pulverous preparation of a (sub)micron-sized biologically active compound comprising the steps of: (1) dissolving a biologically active compound under elevated pressure in a compressed gas, liquid or supercritical fluid containing a surface modifier; or in compressed dimethylether optionally containing a surface modifier; (2a) rapidly expanding the compressed solution of step (1) thereby precipitating the dissolved compound; or (2b) spraying the compressed solution of step (1) into an antisolvant phase optionally containing a surface modifier under vacuum, atmospheric pressure or elevated pressure; and (3) optionally converting the antisolvant phase of step (2b) into a pulverous preparation using conventional powder processing techniques. With the process according to the present invention formation of aggregations or flocculations of particles dissolved in the supercritical solution is prevented; moreover, the addition of cosolvents is not required, thus increasing the stabilisation of the suspension on an industrial scale.

公开(公告)号：EP1071402B1

公开(公告)日：2006-09-13

申请号：EP99919195.0

申请日：1999-04-06

申请人： F. HOFFMANN-LA ROCHE AG

发明人： BAUSCH, Alexander ,  HIDBER, Pirmin

IPC分类号： A61K9/14 ,  A61K31/015 ,  C08J3/12 ,  B01J2/00 ,  B01J2/04 ,  B01J13/00 ,  B01F3/00 ,  B29B9/10

CPC分类号： B01F3/1214 ,  A61K9/14 ,  A61K9/145 ,  A61K9/1688 ,  B01F3/1271 ,  B01F5/0287 ,  B01F2003/0064 ,  B01F2003/125 ,  B01F2215/0032 ,  B01J2/04 ,  B01J3/008 ,  B01J13/02 ,  Y02P20/544 ,  Y10S977/906

摘要： The present invention relates to a process for manufacturing a pulverous preparation of a (sub)micron-sized biologically active compound comprising the steps of: (1) dissolving a biologically active compound under elevated pressure in a compressed gas, liquid or supercritical fluid containing a surface modifier; or in compressed dimethylether optionally containing a surface modifier; (2a) rapidly expanding the compressed solution of step (1) thereby precipitating the dissolved compound; or (2b) spraying the compressed solution of step (1) into an antisolvant phase optionally containing a surface modifier under vacuum, atmospheric pressure or elevated pressure; and (3) optionally converting the antisolvant phase of step (2b) into a pulverous preparation using conventional powder processing techniques. With the process according to the present invention formation of aggregations or flocculations of particles dissolved in the supercritical solution is prevented; moreover, the addition of cosolvents is not required, thus increasing the stabilisation of the suspension on an industrial scale.

公开(公告)号：EP0952820A1

公开(公告)日：1999-11-03

申请号：EP97945817.0

申请日：1997-10-13

申请人： F. HOFFMANN-LA ROCHE AG

发明人： BAUSCH, Alexander ,  PETER, Siegfried, K., F. ,  STEINER, Kurt ,  STOLLER, Hansjörg ,  WEIDNER, Eckhard

IPC分类号： A61K9 ,  A61K31 ,  A61K47 ,  A61P7 ,  A61P9 ,  A61P25 ,  A61P29 ,  A61P31 ,  A61P35 ,  B01J2 ,  B01J3

CPC分类号： C07C403/24 ,  A61K9/146 ,  A61K9/1641 ,  A61K9/1688 ,  A61K31/015 ,  B01F2003/125 ,  Y02P20/544

摘要： The invention concerns: A. a process for the manufacture of pulverous active substance selected from the groups of pharmaceuticals, pharmaceutical precursors, diagnostics, fine chemicals or carotenoids, especially β-carotene characterized by: a-1) dissolving the active substance in dimethyl ether under elevated pressure and temperature conditions, a-2) flash-decompressing the thus-formed solution in an expansion apparatus, and a-3) separating the pulverous solid particles formed in the expansion from the dimethyl ether liberated; and B. a process for the manufacture of a pulverous preparation which contains an active substance selected from the groups of pharmaceuticals, pharmaceutical precursors, diagnostics, fine chemicals, vitamins or preferably a carotenoid, especially β-carotene finally distributed in a matrix component consisting of at least one adjuvant, characterized by: a) dissolving the active substance under elevated temperature and pressure conditions in a compressed gas in the subcritical or supercritical state, b) dispersing the solution obtained from a) in at least one adjuvant, c) removing the compressed gas from the dispersion obtained from b), d) converting the adjuvant then containing the active substance into a pulverous preparation in a process step known per se.