交联甲壳胺-PEG-尼莫地平缓释颗粒性质及释药特性

目的研究交联甲壳胺PEG尼莫地平(rosslinked chitosan PEG nimodipine,RCPN)缓释颗粒的性质及体外释药特性。方法采用乳化交联法制备交联甲壳胺PEG尼莫地平缓释颗粒;用红外光谱(IR)对其结构进行表征;扫描电子显微镜(SEM)观察颗粒形态及表面结构;考察颗粒的粒径分布、颗粒中药物含量测定及在不同介质中药物的释放。结果电镜扫描显示颗粒呈球形,表面圆整,个别表面有凹凸状;RCPN缓释颗粒平均粒径为1.20 mm;红外图谱显示甲壳胺的氨基和戊二醛的羰基发生反应生成Schiffs碱。该颗粒剂有缓释作用,释药特性符合Higuchi方程。结论以交联甲壳胺做为辅料制备的缓释颗粒在体外具有缓释作用。

Investigation of the property of rosslinked chitosan PEG-nimodipine sustained release granules and its release characteristics

Objective To investigate the property of rosslinked chitosan-PEG-nimodipine sustained release granules and its drug release characteristics in vitro. Methods The rosslinked chitosan PEG-nimodipine sustained release granules were prepared using emulsification-crosslinking method, The structures of the granules were characterized by IR spectrometry and its shape and surface were characterized by scanning electron microscope. The distribution of particle diameter, the amount of drug in the granules and the amount of dissolution in different pH mediums were also investigated, Results Scanning electron microscopy shows that the granules were globoid and smooth, very few granules with accidented surface. The mean particle diameter of rossllnked chitosan-PEG-nimodipine granules was 1.20 mm, Infrared spectrum indicated that Schiffs base was formed by the amino-group of chitosan and the carbonyl group of glutaraldehyde. Rosslinked ehitosan-PEG nimodipine granules possessed sustained release property and its release property was in accordance with Higuchi equation. Conclusions Rosslinked chitosan-PEG-nimodipine sustained release granules prepared with crosslinked chitosan-PEG possess sustained release property in vitro.