热熔挤出制备卡马西平组合胶囊及其体外释放行为的研究

Carbamazepine Combined Capsules Prepared by Hot Melt Extrusion and in Vitro Evaluation

目的分别制备速释、缓释和肠溶3种释药速率的卡马西平释药单元,按比例灌装胶囊以制备卡马西平缓释组合胶囊,并对其进行初步评价。方法采用双螺杆挤出机通过热熔挤出法制备3种卡马西平固体分散体释药单元,以载药量、粒度、相似因子为指标,通过单因素法优化处方。结果分别以VA64、EC 7CP、Eudragit L100-55为载体,制得载药量为33%、50%和20%的速释、缓释和肠溶释药单元。与市售制剂Carbatrol?对比,3种释药单元的相似因子f2分别是55、56和62,自制组合胶囊制剂与市售制剂的f2为68。结论采用热熔挤出制备卡马西平组合胶囊的技术简单易行,具有一定的产业化优势。

OBJECTIVE To prepare carbamazepine extended-release combination capsules by filling capsules proportionally with immediate release,extended release,and enteric release units,then preliminary evaluation was carried out.METHODS The solid dispersion formulation was prepared and optimized by hot melt extrusion method using twin-screw extruder,with drug loading,similarity factors(f2)as indicators.RESULTS The immediate release,extended release and enteric release units with 33%,50%and 20%drug loading,which is obtained by VA64,EC 7 CP,and Eudragit L100-55 as carrier respectively,could be produced.Compared with the commercially available formulation carbatrol?,the f2 for the three release units were 55,56 and 62,respectively,and the f2 for the prepared combination capsule is 68.CONCLUSION Carbamazepine combination capsules prepared by hot melt extrusion are relatively simple to manufacture,which has an advantage on commercialization.