RÖSCH, Esther,HOELIG, Peter,LINDLEY, David J.,SANZGIRI, Yeshwant D.,TONG, Ping
申请号：
ES11770975
公开号：
ES2647583T3
申请日:
2011.10.05
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A solid dispersion comprising, in essentially non-crystalline form so that no more than about 5% crystallinity is observed by X-ray diffraction analysis, a compound of Formula I ** Formula ** where: R0 is chlorine； R1 and R2 are H； R3 and R4 are methyl； A1 is N and A2 is CH； R5 is nitro； X is -NH-； Y is - (CH2) n- where n is 1； and R6 is selected from the group consisting of tetrahydropyranyl and 4-hydroxy-4-methylcyclohexyl； or one of its pharmaceutically acceptable salts； wherein the compound of Formula I or the pharmaceutically acceptable salt thereof is dispersed in a solid matrix comprising (a) at least one pharmaceutically acceptable water soluble polymeric carrier and (b) at least one pharmaceutically acceptable surfactant； wherein the compound or a pharmaceutically acceptable salt thereof is present in an equivalent amount of the parental compound of about 5% to about 15% by weight, the at least one pharmaceutically acceptable water soluble polymeric carrier is present in an amount of about 70 % to about 85% by weight, and the at least one pharmaceutically acceptable surfactant is present in an amount of about 5% to about 15% by weight.Una dispersión sólida que comprende, en forma esencialmente no cristalina de manera que no se observa más de aproximadamente 5% de cristalinidad mediante análisis de difracción de rayos X, un compuesto de Fórmula I**Fórmula** donde: R0 es cloro； R1 y R2 son H； R3 y R4 son metilo； A1 es N y A2 es CH； R5 es nitro； X es -NH-； Y es -(CH2)n- donde n es 1； y R6 se selecciona del grupo que consiste en tetrahidropiranilo y 4-hidroxi-4-metilciclohexilo； o una de sus sales farmacéuticamente aceptables； en donde el compuesto de Fórmula I o la sal farmacéuticamente aceptable del mismo son dispersados en una matriz sólida que comprende (a) al menos un portador polimérico soluble en agua farmacéuticamente aceptable y (b) al menos un tensioactivo farmacéuticamente aceptable； en donde el compuesto o una de sus sales farmacéuticamente aceptabl
