processo para cristalização controlada de um ingrediente farmacêutico ativo a partir de estado líquido super-refrigerado por extrusão por fusão a quente
ASHISH CHATTERJI,DAVE ALAN MILLER,DIPEN DESAI,HARPREET K. SANDHU,NAVNIT HARGOVINDAS SHAH
申请号：
BR112013021030
公开号：
BR112013021030A2
申请日:
2012.02.14
申请国别(地区):
BR
年份:
2016
代理人:
摘要：
Process for the crystallization of an active pharmaceutical ingredient is controlled from a liquid state super chilled by hot melt extrusion describes a process to control the crystallization of certain hydrophobic active pharmaceutical ingredients (APIs) from A liquid super chilled via processing by extrusion through hot melting.It also provides a pharmaceutical composition comprising a dispersion of crystalline solid of an inhibitor of cholesterol ester transfer protein from a matrix of a hydrophilic excipient.By means of the process claimed, the API is fed to a system of extrusion in a crystalline state simultaneously with vehicles, excipients, where he is first converted to a state not cristatalino by application of heat, and then subsequently recrystallised in situ Po A means of removing heat and application of shear.The recrystallization of the API is controlled by means of a preset of formulation of the vehicle and the parameters of the extrusion process by hot melting i.e., temperature profile of the drum, feeding rate, and other.The resulting product is a crystalline solid dispersion of API in the matrix of the excipient, where the diameter of the particles of the API after processing is reduced in comparison to the API in the feeding process. The resulting product shows a faster rate of dissolution compared With the API lens made by conventional means for example, micronization or co micronization.The system of the vehicle is comprised of at least one hydrophilic polymer, thermoplastic, and may also contain several functional excipients, such as: antioxidants, surfactants, wetting agents, agents of disintegration, stabilizing agents, agents of acidifica\u00e7 To be, or similar functional excipients.processo para cristalização controlada de um ingrediente farmacêutico ativo a partir de estado líquido super-refrigerado por extrusão por fusão a quente descreve-se um processo para controlar a cristalização de determinados ingredientes farmacêuticos ativos hidr
