注射用染料木素胶束的体外释药研究

Drug Release of Genistein Micelle for Injection in Vitro

目的:考察以单甲氧醚聚乙二醇-聚乳酸羟基乙酸共聚物为载体制备的注射用染料木素胶束的体外释药规律。方法:以加入2%吐温80的磷酸盐缓冲溶液(pH7.4)为释放介质,采用动态膜透析技术考察注射用染料木素胶束释药行为;采用高效液相色谱法测定含量并计算累积释药率;应用6种数学模型对其释药规律进行拟合;同时与染料木素原料药比较。结果:染料木素原料药在2 h内释放完全,而注射用染料木素胶束前期释药较快,后期释药较慢,并可持续释药48 h以上,释药行为符合Weibull模型。结论:注射用染料木素胶束体外释放具有一定的缓释特性。

OBJECTIVE： To investigate the in vitro drug release regulation of Genistein micelle for injection using MePEG-PLGA as carrier.METHODS： The release behavior of Genistein micelle for injection was studied by dynamic dialysis method using 2% Tween-80 phosphate buffer（pH7.4） as release medium.HPLC method was used to determine accumulative release rate.The release behavior was simulated with six different equations,and compared with raw genistein.RESULTS： Raw genistein completely released within 2 h,and Genistein micelle for injection released rapidly at the early stage and slowly at the later stage lasting for 48 h above.The release behavior of Genistein micelle for injection was well-fitted to Weibull equation.CONCLUSION： Genistein micelle for injection possesses the properties of sustained release formulation.