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目的:研究汉黄芩素白蛋白微球在大鼠体内的药动学及组织分布情况。方法:以汉黄芩素溶液为参比,用3P97软件计算大鼠尾静脉给予汉黄芩素白蛋白微球后,其在大鼠体内的药动学模型及药动学参数,用靶向效率评价其在大鼠体内的组织分布及靶向性。结果:汉黄芩素白蛋白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t1/2α=(0.550 0±0.128 2)h,t1/2β=(14.776 1±1.578 2)h,CL=(0.005 96±0.001 4)mL.h.kg-1,AUC0→∞=(126.331 7±9.501 2)mg·h·L-1。其在肝脏,脾脏,心脏,肺脏及肾脏的靶向效率分别为2.21,2.02,0.58,0.64,0.26。结论:与汉黄芩素溶液相比,汉黄芩素白蛋白微球能提高对肝脏,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 wogonin albumin microspheres in rats. Methods: The pharmacokinetics model and pharmacokinetic parameters of wogonin albumin microspheres in rat tail vein were calculated by 3P97 software with wogonin solution as reference. The target efficiency was evaluated Its tissue distribution and targeting in rats. Results: The pharmacokinetic model of wogonin albumin microspheres in rats was in accordance with the two-compartment model. The main pharmacokinetic parameters t1 / 2α = (0.550 ± 0.128 2) h, t1 / 2β = (14.776 ± 1.578 2) h, CL = (0.005 96 ± 0.001 4) mL.h.kg-1, AUC0 → ∞ = (126.331 7 ± 9.501 2) mg · h · L -1. Its targeting efficiency in liver, spleen, heart, lung and kidney were 2.21,2.02,0.58,0.64,0.26 respectively. Conclusion: Compared with wogonin solution, wogonin albumin microspheres can increase the tendency of the liver and spleen, which is beneficial to improve the therapeutic effect.