目的:通过考察不同处方和工艺制备的吲哚美辛-海藻酸钠-壳聚糖-海藻酸钠(ACA)复式微囊的体外释放,研究复囊中药物释放的特点。方法:以吲哚美辛为模型药物,采用不同的交联剂CaCl2、BaCl2的制备工艺,结合液化囊心、冻干工艺制备复式微囊,考察复囊中药物在体外的释放。结果:药物在ACA复式微囊中释放比在单囊中缓慢,ACA—Ba—Ba复囊中药物释放最慢(释放90%药物要18—21h);液化囊心后药物释放略有加快,冻干工艺使药物释放减慢;复囊中药物在人工胃液中2h释放低于20%,在人工肠液中1h释放超过90%。结论:ACA复式微囊能较好地控制药物达到缓释效果,有望成为一种新型药物缓释剂型。
Objective: To explore the character of drug release of multilayer microcapsules, some types of Indomethacin-ACA multilayer microcapsules were prepared with different prescription and its drug release in vitro was studied. Methods: ACA multilayer microcapsules were prepared using different crosslinking agent CaCI2, BaC12 and preparation process such as the capsule heart liquefaction, lyophilization, with indomethacin as model drug. The drug release in vitro was also inspected. Results: Indomethacin released much slowlier from ACA multilayer microcapsules than it from ACA single layer microcapsules, and the rate from ACA-Ba-Ba multilayer microcapsules was the slowest (18-21 h for 90% drug release). Capsule heart liquefaction could accelerate drug release rate slightly, and the lyophilization process made the drug release slowly. The amount of drug release in artificial gastric juice was less than 20% in 2 h, while in artificial intestinal juice it could be more than 90% in 1 h. Conclusion: ACA multilayer microcapsules can keep drug releasing slowly, it may be a new drug sustained- release dosage form.