聚合物辅料对无定形氯雷他定溶出行为和结晶形态的影响

Effect of different polymer excipients on the dissolution behavior and crystalline morphology of amorphous loratadine

目的考察聚合物辅料对无定形氯雷他定溶出和结晶的影响。方法用紫外分光光度法考察无定形氯雷他定在不同体积分数聚维酮K30(PVP-K30)、聚乙二醇4000(PEG 4000)和羟丙基甲基纤维素(hydroxypropyl methylcellulose,HPMC)3种聚合物溶液中的溶出情况;用偏光显微镜观察无定形氯雷他定在水及3种聚合物溶液中的结晶形态及结晶生长情况。结果不同种类的聚合物对无定形氯雷他定均有一定的增溶作用,聚合物体积分数越高,增溶作用越明显,其中PEG 4000的增溶作用最强。不同种类的聚合物对氯雷他定晶体的生长均有一定的抑制作用。结论聚合物辅料的种类和体积分数对无定形氯雷他定的溶出特性及晶体形态有一定的影响,为无定形药物稳定性研究及制剂研发提供理论指导。

Objective To investigate the influence of different polymer excipients on the dissolution behavior and crystallization of amorphous loratadine.Methods The dissolution of amorphous loratadine in different concentrations solutions of povidone K30(PVPK30),polyethylene glycol 4000(PEG 4000)or hydroxypropyl methylcellulose(HPMC)was investigated by ultraviolet spectrophotometer.The crystal morphology and growth of amorphous loratadine in water and 3 kinds of polymer solutions were observed by polarizing microscope.Results Different kinds of polymers showed different solubilization effect on amorphous loratadine.The higher the concentration of polymer was,the stronger its solubilization effect.And PEG 4000 showed the strongest solubilization.Different kinds of polymers showed different inhibitory effects on the growth of loratadine crystals.Conclusion The type and concentration of polymer excipients have different effects on the solubility and crystal morphology of amorphous loratadine.This study provides theoretical guidance for the stability study of amorphous drugs and the development of preparations.