达比加群酯中空微球的制备及溶剂选择

Preparation of Hollow Microspheres for Dabigatran Etexilate and Solvent Selection

目的改变制备中空微球中所需有机溶剂的不同配比,探讨有机溶剂对中空微球形成的影响。方法采用以乙醇与二氯甲烷之比为1∶1的最优配比制备达比加群酯中空微球,并测定其含量、体外释放度。结果制备的达比加群酯中空微球具有明显空腔,体外漂浮性能良好,体外释放行为符合Higuchi方程,2 h和12 h时累积释放率分别为45.3%和61.4%。结论所制备的达比加群酯中空微球具有缓释效果,有利于减少给药次数。

Objective To investigate the influence of organic solvent on the hollow microspheres formation by changing different propor-tions of organic solvent required in the preparation of hollow microspheres. Methods Dabigatran etexilate hollow microspheres were pre-pared by adopting the optimal proportion of 1：1 for dichloromethane and ethanol. Its content and in vitro release were calculated. Results The prepared Dabigatran etexilate hollow microspheres had obvious cavities,good in vitro floating performance,and the in vitro release behavior conformed to the Higuchi equation,the 2 h and 12 h cumulative release rates were 45. 3% and 61. 4% respectively. Conclusion The prepared Dabigatran etexilate hollow microspheres have a sustained-release effect and help to reduce the frequency of administration.