卡铂-乳酸/羟基乙酸共聚物微囊在家兔体内的药动学

Study on pharmacokinetics of carboplatin-polyD,L-lactide/glycolide microcapsules in rabbits

目的 :考察卡铂 乳酸 /羟基乙酸共聚物微囊在家兔体内的药动学过程。方法 :健康家兔 8只 ,随机交叉试验 ,单剂量注射卡铂微囊混悬液和卡铂原料药溶液后 ,采用等离子体原子发射光谱法测定血药浓度 ,药 时数据经PKS计算机程序拟合 ,自动判别最佳模型及计算药动学参数。结果 :两种剂型的的药 时曲线符合三室模型 ,二者的药动学参数Cmax、t1/ 2 β、MRT、AUC、CL差异存在显著性 (P <0 .0 5 )。结论 :卡铂制成微囊后 ,在家兔体内具有明显的缓释作用 ,有效作用时间延长 。

OBJECTIVE To study the pharmacokinetic characteristics of carboplatin-polyD,L-lactide/gl ycolide microcapsules (CBP-PLGA-MC) in rabbits.METHODS 8 rabbits were injected CBP-PLGA-MC and CBP with cross-over design.The carbo platin concentration in plasma was measured by inductively coupled plasma-atomi c emission spectrometry at different times after injection.Pharmacokinetic para meters were analyzed by PKS computer programs.RESULTS Three-compartment model was adapted to describe the pharmacokinetic characteri stics of CBP-PLGA-MC and CBP in rabbits.The C max,t 1/2β,M RT,AUC and CL values had significant difference (P< 0.05).CONCLUSION CBP-PLGA-MC has slow-release effect and kept concentration in plasma for a lo ng time comparing with carboplatin, the microcapsules were helpful for antitumou r therapy of carboplatin.