水飞蓟宾明胶微球在大鼠体内的药动学及组织分布

目的:研究水飞蓟宾明胶微球在大鼠体内的药动学及组织分布.方法:以水飞蓟宾注射液为参比,用3P 97软件计算药动学模型及药动学参数,用靶向效率来评价其在大鼠体内的组织分布及靶向性.结果:水飞蓟宾明胶微球在大鼠体内的药动学模型符合二室模型,主要药动学参数为:t1/2α=(0.5728±0.108 6)h,t1/2β=(20.6866±1.058 8)h,CL=(0.003 8±0.001 4) mL·h· Kg-1,AUCo→∞=(211.095 0±10.272 8) mg·h·L-1,其在肝脏、脾脏、心脏及肾脏的靶向效率分别为2.093,1.986,0.634,0.259.结论:与水飞蓟宾注射液相比,水飞蓟宾明胶微球能提高对肝脏,脾脏的趋向性,有利于提高其治疗作用.

Pharmacokinetics and Tissue Distribution of Silybin Gelatin Microspheres In vivo in Rats

Objective:To investigate in vivo pharmacokinetics and tissue distribution of silybin gelatin microspheres in rats.Method: With silybin injection as reference,pharmacokinetic model and parameters were calculated by 3P97.In vivo tissue distribution and targeting of silybin gelatin microspheres in rats were evaluated by targeting efficiency.Result: Pharmacokinetic data fitted a two-compartment model,main pharmacokinetic parameters of silybin gelatin microspheres were as follows: t1/2α=(0.572 8±0.108 6) h,t1/2β=(20.686 6±1.058 8) h,CL=(0.003 8±0.001 4) mL·h·kg-1,AUC0→∞=(211.095 0±10.272 8) mg·h·L-1.Targeting efficiency of it in liver,spleen,heart and kidney were 2.093,1.986,0.634,0.259.Conclusion: Compared to silybin injection,silybin gelatin microspheres could improve tendency for liver and spleen,and help improving its therapeutic effect.