口服藻酸双酯钠纳米粒的制备、体外释药特性及其药效学研究  

Study on preparation,release in vitro and pharmacodynamics of the oral propylene glycol alginate sodium sulfate(PSS) nanoparticles

作　　者：李鹏丽[1] 徐雪莲[1] 李春霞[1] 李海花[1] 何小溪[1] 管华诗[1] 

机构地区：[1]中国海洋大学海洋药物教育部重点实验室海洋药物与食品研究所,山东青岛266003

出　　处：《中国海洋药物》2011年第2期19-24,共6页Chinese Journal of Marine Drugs

摘　　要：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 prepare the oral propylene glycol alginate sodium sulfate（PSS） nanoparticles and investigate their physicochemical characteristics,drug release in vitro and biological activity in order to improve the stability and oral bioavailability.Methods PSS nanoparticles were achieved by the Double（W1/O/W2）Emulsion and Solvent Evaporation Methods and the optimum formulation was obtained by the orthogonal design.Nanoparticle morphology was examined by transmission electron microscope.Nanoparticle size and zeta potential were measured by zetasizer nano analyser.The entrapment efficiency and the drug loading efficiency of PSS nanoparticles were measured by the oxygen bottle combustion.Supercentrifugate was used to determine the releasing characteristic of PSS nanoparticles in vitro.The normal mice were treated through intragastric administration to examine the effect of reducing blood glucose.Results The size,entrapment efficiency and the drug loading efficiency of nanoparticles with optimum formulation were 181.8 nm,75.80% and 10.83%,respectively.The total drug release rate in 12 h was 60.37%.The hypoglycemic effect of PSS-NP on the normal mice was significant.Conclusion Oral PSS nanoparticles were successfully prepared by optimization,and the physicochemical characteristics were stable and the medicinal effectiveness was reliable.

关 键 词：藻酸双酯钠 纳米粒 体外释药 降血糖 

分 类 号：TQ464[化学工程—制药化工] R965[医药卫生—药理学]