载药蒙脱石/丙烯酸树脂微球的制备与体外释放性能的研究

目的以丙烯酸树脂为膜材制备载药蒙脱石/丙烯酸树脂微球并考察其体外释放性能。方法以盐酸倍他洛尔为模型药物,采用O/O溶剂挥发法制备蒙脱石载药微球,通过正交实验设计,考察柠檬酸三乙酯及甘油用量、乳化剂与膜材比例及用量、内外相体积比等因素对微球载药量、包封率、体外释放性能的影响,采用扫描电镜对其外观形态进行表征。结果所得微球外观圆整,粒径分布较均匀,平均粒径为20.7μm,平均载药量为14.31%±0.47%,平均包封率为94.35%±1.01%。结论该法制备载药蒙脱石丙烯酸树脂微球是可行的,体外释放研究表明微球具有一定的缓释作用。

Study on preparation and in vitro release behavior of drug-loaded montmorillonite-eudragit composite microspheres

Objective The purpose of this study was to prepare drug-loaded montmorillonite-eudragit composite microspheres with eudragit as the membrane material and study its release in vitro .Methods Betaxolol hydrochloride was used as a model drug .The microspheres were prepared by oil in oil solvent evaporation technique .An orthogonal experimental design was used to study the effect of the amount of triethyl citrate and glycerol ,the ratio and amount of emulsifier and membrane material ,the volume ratio of internal oil phase and external oil phase on microspheres .Drug loading capacity and encapsulation efficiency were used as evalua-ting indicators .The morphology of microparticle was characterized by SEM .Results The microspheres were spherical in the shape ,and the size distribution was uniform .The mean particle size was 20 .7 μm .The average drug loading capacity and the en-capsulation efficiency were 14 .31% ± 0 .47% and 94 .35% ± 1 .01% ,respectively .Conclusion The method for the preparation of drug-loaded montmorillonite-eudragit composite microspheres is feasible ,while the in vitro release study of microspheres showed that the drug was sustainedly released .