阿替洛尔脂质体制备工艺及处方优化研究

Optimization of the preparation and formulation of atenolol liposomes

目的研制阿替洛尔脂质体给药系统。方法采用逆向蒸发法、乙醚注入法、薄膜法和硫酸铵梯度法制备了阿替洛尔脂质体,证实硫酸铵梯度法包封率最高且稳定性最好。采用均匀设计法,以包封率为指标,优化硫酸铵梯度法制备脂质体的处方和工艺。并用透射电镜对脂质体进行了考察。结果证实最优处方制得的脂质体的外观比较圆整,包封率和粒径均令人满意。结论硫酸铵梯度法对于弱碱性药物来说是一个比较好的制备方法。

OBJECTIVE To prepare atenolol liposomes. METHODS The preparation methods of liposomes such as reverse phase evaporation, injection, film dispersion and ammonium sulfate transmembrane gradients were explored in order to select suitable technique. The uniform design was adopted to screen the formulation of atenolol liposomes.The appearance and size distribution were examined by casting electron microscope. RESULTS The entrapment efficiency and particle size of atenolol liposomes prepared by optimized method were satisfactory. CONCLUSIONS Ammonium sulfate transrnembrane gradient method is a suitable method for atenolol.