MILLER, DAVE A.,MCCONVILLE, JASON T.,MCGINITY, JAMES W.,WILLIAMS, ROBERT O., III
申请号：
CA2598204
公开号：
CA2598204C
申请日:
2005.11.09
申请国别(地区):
CA
年份:
2015
代理人:
摘要：
A hot-melt extruded composition having finely divided drug-containingparticles dispersed within a polymeric and/or lipophyllic carrier matrix isprovided. The carrier softens or melts during hot-melt extrusion but it doesnot dissolve the drug-containing particles during extrusion. As a result, amajority or at least 90 % wt. of the drug-containing particles in theextrudate are deaggregated during extrusion into essentially primarycrystalline and/or amorphous particles. PEO is a suitable carrier material fordrugs insoluble in the solid state in this carrier. Various functionalexcipients can be included in the carrier system to stabilize the particlesize and physical state of the drug substance in either a crystalline and/oramorphous state. The carrier system is comprised of at least one thermalbinder, and may also contain various functional excipients, such as: super-disintegrants, antioxidants, surfactants, wetting agents, stabilizing agents,retardant, or similar functional excipients. A hydrophilic polymer, such ashydroxypropyl methylcellulose (HPMC E15), polyvinyl alcohol (PVA), orpoloxamer, and/or a surfactant, such as sodium lauryl sulfate (SLS), can beincluded in the composition. A process for preparing the extrudate isconducted at a temperature approximating or above the softening or meltingtemperature of the matrix and below the point of solubilization of drug-containing particles in the carrier system, and below the recrystallizationpoint in the case of amorphous fine drug particles.
