【摘要】 目的:制备冬凌草甲素纳米粒,考察其在大鼠体内的药动学行为。方法:采用乳化超声-溶剂蒸发法制备荷载冬凌草甲素的聚乳糖-羟基乙酸（PLGA）纳米粒,通过粒径及多分散指数测定、外观形态的透射电镜观察、包封率及载药量分析等,对纳米粒进行体外理化性质测定。以大鼠为模型动物,尾静脉注射冬凌草甲素PLGA纳米粒,采用HPLC法测定其血药浓度,利用DAS软件分析其药动学特征。结果:所制备的冬凌草甲素PLGA纳米粒平均粒径为180nm,包封率为（87.7±7.7）%,载药量为（7.5±0.8）%,其外观形态为圆球形。单剂量静脉注射冬凌草甲素PLGA纳米粒后在大鼠体内呈二室模型分布。其主要的药动学参数如下:分布半衰期（t1/2α）为2.115h,消除半衰期（t1/2β）为69.315h,血药浓度曲线下面积（AUC）为42.463 mg·h·L^-1,清除率（CL）为0.094L·h^-1·kg^-1,表观分布容积（V）为0.4L/kg。结论:本研究建立的冬凌草甲素PLGA纳米粒制备工艺简单、可行,包封率较高,制备成PLGA纳米粒后可以改善冬凌草甲素的生物利用度。更多还原

【Abstract】 Objective:To prepare oridonin nanoparticles and evaluate their pharmacokinetics in rats.Methods:The oridonin poly（lactic-co-glycolic acid）（PLGA）nanoparticles were prepared by emulsion sonication and solvent evaporation method with PLGA as encapsulation materials.Their physicochemical properties were identified through determination of particle size and polydispersity index（PDI）,transmission electronic microscopy（TEM）observation of the appearance form,analysis of entrapment efficiency and drug loading.The oridonin PLGA nanoparticles were administered intravenously through caudal vein in rats.Then blood concentrations of oridonin were determined by HPLC method,and the pharmacokinetics were analyzed by DAS software.Results:The particle size of the prepared nanoparticles on the average was about 180 nm,the entrapment efficiency was（87.7±7.7）% and drug loading was（7.5±0.8）% with an outward spherical appearance.The compartment model was attributed to two-compartment model after single intravenous injection of oridonin PLGA nanoparticles.The main pharmacokinetic parameters were as follows:half life of distribution phase（t1/2α）was 2.115 h,half life of elimination phase（t1/2β）was 69.315 h,the area under the curve（AUC）was 42.463 mg·h·L^-1,clearance（CL）was 0.094 L·h^-1·kg^-1,apparent volume of distribution（V）was 0.4 L/kg.Conclusion:The preparation technology of oridonin PLGA nanoparticles is simple and feasible,with a higher entrapment efficiency.The bioavailability of oridonin could be improved when oridonin was fabricated into PLGA nanoparticles.更多还原