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目的为了提高藻酸双酯钠(PSS)口服制剂的稳定性及其生物利用度,制备藻酸双酯钠的口服纳米粒(PSS-NP),并对其理化性质、体外释药特性及其药效学进行考察。方法采用改进的双乳化溶剂蒸发法(W1/O/W2)制备藻酸双酯钠纳米粒并设计正交试验筛选最优处方;透射电镜观察纳米粒形态;粒度及表面电位分析仪测量纳米粒的粒径及zeta电位;氧瓶燃烧法测定载药纳米粒的包封率与载药量;超速离心法考察载药纳米粒的体外释药特性;正常小鼠灌胃给药测定降血糖效果。结果与结论优化的口服藻酸双酯钠纳米粒为规则的圆球形,其粒径大小为181.8 nm,包封率为75.80%,载药量为10.83%,zeta电位为-17.3 mV;12 h内PSS-NP累积释药百分率为60.37%;PSS-NP对正常小鼠具有显著的降血糖效果。
Objective To improve the stability and bioavailability of sodium alginate sodium (PSS) oral preparation, sodium alginate oral nanoparticles (PSS-NP) were prepared and their physical and chemical properties, in vitro release characteristics and their Pharmacodynamic study. Methods The sodium alginate nanoparticles were prepared by the modified double-emulsion solvent evaporation method (W1 / O / W2) and the optimal prescriptions were designed by orthogonal test. The morphology of the nanoparticles was observed by transmission electron microscopy. The particle size and surface potential were measured by nano- The particle size and zeta potential of the drug-loaded nanoparticles were measured. The entrapment efficiency and drug loading of drug-loaded nanoparticles were measured by oxygen flask combustion method. The drug release characteristics of drug-loaded nanoparticles were investigated by ultracentrifugation method. . RESULTS AND CONCLUSIONS The optimized oral sodium alginate nanoparticles were spherical in shape with a size of 181.8 nm, encapsulation efficiency of 75.80%, drug loading of 10.83% and zeta potential of -17.3 mV. The cumulative release percentage of PSS-NP was 60.37%. PSS-NP had a significant hypoglycemic effect on normal mice.