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目的 探讨不同化疗药物经动脉及静脉途径注射后血浆及组织内药物浓度的变化规律。方法 10只成年新西兰雌兔随机平均分为两组 (动脉组和静脉组 )。一组经髂内动脉、另一组经耳缘静脉注射顺铂 (DDP)、5 氟脲嘧啶 (5 Fu)和依托泊甙 (Vp 16 )。注射后于不同时间采血样及子宫组织标本 ,以HPLC法测定血浆及子宫组织中药物浓度。所得数据用 3P97软件处理 ,计算药代动力学参数。结果 动脉及静脉注射 3种药物后 ,在血浆及靶组织中的浓度均呈现了规律性的变化 ,其变化过程均可以两室模型来描述。动脉注射 3种药物的药代动力学参数与静脉注射的药代动力学参数不同 ,动脉组注射药物后 ,血浆药物峰浓度均低于静脉组 ,而靶组织内药物峰浓度均高于静脉组 ,靶组织内药物AUC(药时曲线下面积 )值均明显高于静脉组。结论 动脉注射DDP、5 Fu和Vp 16较静脉注射有不同程度的优势 ,这种优势与药物的药理特性有关
Objective To investigate the variation of drug concentration in plasma and tissue after injection of different chemotherapeutic agents via arterial and venous routes. Methods Ten adult New Zealand female rabbits were randomly divided into two groups (arterial group and vein group). One group received internal iliac artery, and the other received intravenous cisplatin (DDP), 5 Fu and etoposide (Vp 16). Blood samples and uterine tissue samples were collected at different times after injection, and the plasma and uterine tissue concentrations were determined by HPLC. The data obtained were processed using 3P97 software to calculate pharmacokinetic parameters. Results The arterial and intravenous injection of three drugs in plasma and target tissue concentrations showed a regular change, the changes can be described by a two-compartment model. Pharmacokinetic parameters of arterial injection of three drugs pharmacokinetic parameters and intravenous injection of different arterial injection group, the peak plasma drug concentrations were lower than the intravenous group, while the target tissue peak drug concentration were higher than the intravenous group , AUC (drug under the curve area) value of the target tissue were significantly higher than the vein group. Conclusion Arterial injection of DDP, 5 Fu and Vp 16 have different degrees of superiority over intravenous injection, which is related to the pharmacological properties of the drug