羟丙甲纤维素辅料的性质对硝苯地平缓释片突释的影响  

Effect of the Properties of Hydroxypropyl Methylcellulose(HPMC)Excipients on Sudden Release of Nifedipine Sustained Release Tablets

作　　者：刘静 李威 颜起航 顾相伶 宋新峰 张中玉 范娜 LIU Jing;LI Wei;YAN Qi-hang;GU Xiang-ling;SONG Xin-feng;ZHANG Zhong-yu;FAN Na(College of Medicine and Nursing,Dezhou University,Dezhou 253023,China;Nanomedicine Laboratory,Naval Medical University,Shanghai 200433,China;Wuya College of Innovation,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]德州学院医药与护理学院,山东德州253023 [2]中国人民解放军海军军医大学纳米医学研究室,上海200433 [3]沈阳药科大学无涯创新学院,沈阳110016

出　　处：《中国药学杂志》2023年第6期516-522,共7页Chinese Pharmaceutical Journal

基　　金：德州学院省级重点实验室开放基金项目资助(SD2019BP007)。

摘　　要：目的基于羟丙甲纤维素(HPMC)硝苯地平缓释片的突释是制剂应用中急需解决的问题,本实验系统研究了HPMC药用辅料的性质与药物释放的相关性,探索其影响突释的关键因素。方法采用4个不同厂家、规格相同(2208系列)的HPMC,按相同工艺制成硝苯地平缓释片;参照日本橙皮书及2020年版《中国药典》分别测定其在水、pH 1.2、pH 4.0、pH 6.8不同溶出介质中的体外溶出曲线;并结合HPMC的红外光谱、热重、结晶度、形态、溶解速度、粒径大小及分布的测定结果,探究其影响硝苯地平缓释片体外释放的关键因素。结果HPMC的流体力学粒径大小及均匀度与硝苯地平缓释片缓释效果密切相关。结论HPMC在水溶液中的溶解性,尤其是其流体力学粒径大小及分布是影响缓释制剂药物释放的关键功能指标。OBJECTIVE To study the sudden release of nifedipine sustained release tablets and investigate the correlation between the properties of HPMC formulations and drug release profile.METHODS Four HPMCs purchased from different manufacturers with the same specifications(2208 series)were used to prepare the tablets under the same process conditions.In vitro dissolution curves of nifedipine tablets in water,pH 1.2,pH 4.0 and pH 6.8 solutions were tested according to Japanese Orange Book and Chinese Pharmacopoeia(2020 edition).Then the IR spectrum,TG curve,crystallinity,morphology,dissolution rate,particle size and size distribution were used to evaluate the key factors affecting the release.RESULTS The results showed that the significant difference in hydromechanical particle size and size distribution is densely correlate to the sustained drug release profile of nifedipine sustained release tablets.CONCLUSION The solubility,especially hydromechanical particle size and size distribution are the key parameters that affect the drug release of formulations.

关 键 词：羟丙甲纤维素 流体力学粒径 药用辅料 功能性相关指标 缓释制剂 

分 类 号：R944[医药卫生—药剂学]