A Solid dispersion comprising an apoptosis Inducing Agent formula defined dispersed in a Solid Matrix that comprises a) at least one water soluble polymeric vehicle and (b) a Surfactant； Preparation Process； oral dosage form, useful for treating a disease Neoplastic, immune or autoimmune.
BIRTALAN, ESTHER,HOELING, PETER,LINDLEY, DAVID J.,SANZGIRI, YESHWANT D.,TONG, PING
申请号：
CL2013001120
公开号：
CL2013001120A1
申请日:
2013.04.24
申请国别(地区):
CL
年份:
2013
代理人:
摘要：
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture； extruding the semi-solid mixture； and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.<；p>；UNA DISPERSIÓ；N SÓ；LIDA PRO-APOPTÓ；TICA QUE COMPRENDE, EN UNA FORMA NO CRISTALINA, UN COMPUESTO INHIBIDOR DE FAMILIA DE PROTEÍ；NAS BEL 2 DE LA FÓ；RMULA 1, DISPERSO EN UNA MATRIZ SÓ；LIDA QUE COMPRENDE (A) UN VEHÍ；CULO POLIMÉ；RICO SOLUBLE EN AGUA FARMACÉ；UTICAMENTE ACEPTABLE Y (B) UN AGENTE TENSIOACTIVO FARMACÉ；UTICAMENTE ACEPTABLE. UN PROCESO PARA PREPARAR DICHA DISPERSIÓ；N SÓ；LIDA QUE COMPRENDE SOMETER A UNA TEMPERATURA ELEVADA EL COMPUESTO DE LA FÓ；RMULA 1, EL VEHÍ；CULO POLIMÉ；RICO SOLUBLE EN AGUA Y EL AGENTE TENSIOACTIVO, PARA PROVEER UNA MEZCLA SERNISÓ；LIDA EXTRUIBLE； EXTRUDIR LA MEZCLA SEMISÓ；LIDA； Y ；ENFNAR EL EXTRUDADO RESULTANTE PARA PROVEER UNA MATRIZ SÓ；LIDA QUE COMPRENDE EL VEHÍ；CULO POLIMÉ；RICO Y EL AGENTE TENSIOACTIVO Y EN EL CUAL ESTÁ； DISPERSO EL COMPUESTO EN UNA FORMA ESENCIALMENTE NO CRISTALINA. LA DISPERSIÓ
