地高辛固体脂质纳米粒的制备及家兔体内的药动学

Preparation of Digoxin Solid Lipid Nanoparticles and Its Pharmacokinetics in Rabbits

以单硬脂酸甘油酯为脂质材料,采用溶剂扩散法所制的地高辛固体脂质纳米粒于4℃贮存3个月,平均粒径增大,但包封率和载药量无显著变化。家兔静脉注射地高辛纳米粒或自制溶液剂后,AUC分别为(90.3±27.5)和(82.4±34.2)ng·h·ml-1。两者的分布容积有较大差异,提示固体脂质纳米粒静注后可改变药物在体内的分布。

Solid lipid nanoparticles （SLN） loaded with digoxin were prepared by solvent diffusion method using glyceryl monostearate as matrix material. The mean diameter of the products was increased while the entrapment efficiency and drug loading had no significant difference after stored at 4℃ for three months. The AUC after intravenous injection of the prepared SLN or solution in rabbits were （90.3±27.5） and （82.4±34.2）ng·h·ml^-1, respectively. The Vss of the two groups had significant difference, which indicated the SLN could change the drug in vivo distribution.