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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=(0.572 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,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。
Objective: To study the pharmacokinetics and tissue distribution of silybin microspheres in rats. Methods: Using silybin injection as reference, the pharmacokinetic parameters and pharmacokinetic parameters were calculated by 3P 97 software, and the targeting efficiency was used to evaluate the tissue distribution and targeting in rats. Results: The pharmacokinetic model of silybin gelatin microspheres in rats accorded with two-compartment model. The main pharmacokinetic parameters were: 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 ± 10.272 8) mg.hL-1 in liver, spleen, heart and kidney Targeted efficiencies were 2.093, 1.986, 0.634, and 0.259, respectively. Conclusion: Compared with silybin injection, silybin gelatin microspheres can increase the tendency of the liver and spleen, which is beneficial to improve the therapeutic effect.