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目的:研究去甲斑蝥素(NCTD)白蛋白微球在大鼠体内的药动学及组织分布情况。方法:以市售去甲斑蝥素注射液为参比,测定NCTD白蛋白微球在大鼠体内血浆中的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:NCTD白蛋白微球在大鼠体内的药动学模型符合二室模型,主要药动学参数为:t_(1/2α)=(0.57±0.11)h,t_(1/2β)=(20.69±1.06)h,CL=(0.016±0.002 4)ml·h·kg~(-1),AUC_(0～∞)=(63.41±9.08)mg·h·L~(-1),其在肝脏,脾脏,心脏及肾脏的靶向效率分别为为2.36,1.78,0.43和0.35。结论:与去甲斑蝥素注射液相比,NCTD白蛋白微球能提高对肝脏,脾脏的趋向性,减少对肾脏及心脏的分布,有利于提高其治疗作用,减少不良反应。
Objective: To study the pharmacokinetics and tissue distribution of norcantharidin (NCTD) albumin microspheres in rats. Methods: The pharmacokinetic model and pharmacokinetic parameters of NCTD albumin microspheres in rat plasma were determined by using commercially available norcantharidin injection. The targeting efficiency of NCTD albumin microspheres was evaluated in rats Tissue distribution and targeting. Results: The pharmacokinetic model of NCTD albumin microspheres in rats was in accordance with the two-compartment model. The main pharmacokinetic parameters were as follows: t 1/2 (0.57 ± 0.11) h, t 1 / 2β = 20.69 ± 1.06) h, CL = (0.016 ± 0.002 4) ml · h · kg -1, AUC 0 ~ ∞ (63.41 ± 9.08) mg · h · L -1, The targeting efficiencies of liver, spleen, heart and kidney were 2.36, 1.78, 0.43 and 0.35, respectively. CONCLUSION: Compared with norcantharidin injection, NCTD albumin microspheres can increase the tendency of the liver and spleen and reduce the distribution of the kidney and heart, which is beneficial to improve the therapeutic effect and reduce the adverse reactions.