顺铂白蛋白微球家兔肝动脉栓塞后体内药物动力学

 以常规注射剂为对照，研究了顺铂白蛋白微球家兔肝动脉栓塞后的体内药物动力学过程。血清铂浓度的测定采用石墨炉原子吸收分光光度法，所得血浓度数据用ＭＣＰＫＰ药代动力学程序处理。实验结果：顺铂白蛋白微球体内过程符合二室模型，Ｔ＿（１／２Ｋａ）０．２１ｈ，Ｔ＿（１／２ａ）１．５５ｈ，Ｔ＿（１／２ａ）７５，５２ｈ，Ｔ＿（ｍａｘ）０．６９＊Ｃ＿（ｍａｘ）０．５１ｍｇ·Ｌ￣（－１）；Ｔ＿（１／２ａ），Ｔ＿（１／２β）均比注射剂明显延长（Ｐ＜０．０１），峰浓度远远低于注射剂初浓度（Ｐ＜０．００１）。表明檄球剂具有靶向制剂长效、高效、低毒的特点。

Pharmacokinetics of cisplatin albumin microsphere after embolizing inhepatic artery

Cis-diaminodichloroplatinum(CDDP ) albumin microsphere was usedto improve thelocalization of drug action,which in turn will result in an increased therapeutic index and a re-duced toxicity,and to make reinfusion possible in chemoembolization,Apharmacokil1etic study onCDDP albumin microsphere was carried out in 6 rabbits ,with CDDP injection for comparison. Theconcerntration of Pt in serum was determined by graphite furnace atom absorption spectrometry,and the data were treated with MCPKP program.The results show both the microsphere and theinjection fit to two-compartment model in vivo。 However,the existing of ″ absorption phase″ inserum,together with prolonged T1/2aand T1/2β(P<0.01)of CDDP microsphere reflects its sus-tained release character. It also has a lower concentratiOn and longer existance in serum,indicatingthat CDDP in microsphere might accumulate in the liver at a higher concentration and the use of itmight result in alleviation of CDDP toxicities and side-effects。 The reopen of embolized micro-artery will greatly contribute to the clinical use of CDDP albumin microsphere。