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
王嫦鹤 1畅瑞苗 2焦洁 1郭欢迎1
作者信息
- 1. 陕西省食品药品检验研究院,西安 710065
- 2. 西安交通大学药学院,西安 710061
- 折叠
摘要
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.
Abstract
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(PVP-K30),polyethylene glycol 4000(PEG 4000)or hydroxypropyl methylcellulose(HPMC)was investigated by ultraviolet spectropho-tometer.The crystal morphology and growth of amorphous loratadine in water and 3 kinds of polymer solutions were observed by po-larizing 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 theo-retical guidance for the stability study of amorphous drugs and the development of preparations.
关键词
无定形氯雷他定/聚维酮K30/聚乙二醇4000/羟丙基甲基纤维素/溶出/结晶Key words
amorphous loratadine/povidone K30/polyethylene glycol 4000/hydroxypropyl methylcellulose/dissolution/crystalline morphology引用本文复制引用
基金项目
陕西省创新能力支撑计划(2020PT-041)
陕西省社会发展科技计划(2021SF-304)
出版年
2024
NETL
NSTL
维普
万方数据