阿折地平肠溶固体分散体的制备及质量评价

Preparation and Quality Evaluation of Azelnidipine Enteric Solid Dispersion

目的:制备阿折地平肠溶固体分散体并评价其质量。方法:采用溶剂法制备阿折地平肠溶固体分散体,以累积释放度为考察指标,通过单因素试验对载体材料型号和用量等处方条件进行优化,并采用差示量热扫描法(DSC)、X-射线衍射法(XRD)和傅里叶红外光谱法(FTIR)对其进行质量评价,同时对其稳定性进行考察。结果:将阿折地平与肠溶载体材料Eudragit L100-55型丙烯酸树脂按照1∶5(m/m)的比例制备成肠溶固体分散体后,其体外释放情况明显改善;DSC法、XRD法和FTIR法均验证了其晶型发生了改变,以无定形状态存在;稳定性考察结果显示,阿折地平肠溶固体分散体在高温(60℃)、高湿(相对湿度75%)、强光[(4500±500)lx]条件下放置10 d内稳定性较好。结论:采用溶剂法以Eudragit L100-55型丙烯酸树脂为载体材料所制得的阿折地平肠溶固体分散体可消除晶型影响、提高释放度且具有较好的稳定性。

OBJECTIVE:To prepare Azelnidipine enteric solid dispersion and evaluate its quality.METHODS:Azelnidipine enteric solid dispersion was prepared by solvent method.Taking cumulative dissolution rate as the index,single factor test was used to optimize carrier material type and its ratio.The quality of the product was evaluated by DSC,XRD and FTIR,and its stability was investigated.RESULTS:After azelnidipine and carrier material of Eudragit L100-55 acrylic resin were prepared to enteric solid dispersion at a ratio of 1∶5(m/m),its dissolution rate was significantly improved.DSC,XRD and FTIR method had all verified the crystal form of azelnidipine changed and it existed in amorphous form.The results of stability test showed that Azelnidipine enteric solid dispersion was stable under high temperature(60℃),high humidity(75%)and strong light[(4500±500)lx]for 10 days.CONCLUSIONS:Azelnidipine enteric solid dispersion by solvent method with Eudragit L100-55 acrylic resin as carrier can eliminate the influence of crystal form,improve dissolution and has good stability.