家兔氟尿嘧啶胃左动脉灌注与静脉化疗药物动力学比较

目的　评价氟尿嘧啶动物胃左动脉灌注和外周静脉化疗药物动力学的基础实验比较。方法　实验家兔 18只 ,随机分 6个时间组 ,由胃左动脉注入氟尿嘧啶 (按 5 0mg/kg) ,于不同时间点 ,留取门静脉及外周静脉血 ,同时处死动物 ,取部分胃组织。血样及组织样经处理后采用高效液相色谱测定 ,对照组由耳缘静脉注入氟尿嘧啶 (5 0mg/kg) ,不同时间取血和组织 ,同上处理后测定。 结果　两种途径给药后的门静脉及外周静脉的药时曲线均为 5min达到高峰值 ,之后迅速下降 ,30min后下降缓慢 ,符合二室模型 ;动脉灌注组门静脉血药浓度明显高于外周血药浓度 ,亦明显高于静脉注药组的门静脉浓度 ,而且持续时间较长 ;5min后动脉灌注组胃组织药物浓度 11倍于静脉给药组 ,2h后两者浓度接近。结论　经胃左动脉灌注在门静脉及胃组织中的药物浓度在较长时间内维持相对高的水平 ,而且能使局部药物相对集中 ,可以在很大程度上提高疗效

The comparision of 5-Fu pharmacokinetics on rabbit after left gastric intraarterial infusion and by peripheral intravenous administration

Objective To compare the pharmacokinetics on rabbit after left gastric regional arterial infusion chemotherapy with peripheral intravenous administration.Methods 18 rabbits were seperated into 6 time groups at random and 5 Fu (50mg/kg) was infused through left gastric artery. Blood of portal vein and peripheral vein were sampled at different times. Finally all rabbits were killed and partial stomach tissues were sampled. Blood and stomach tissue were analysed with high efficacy liquid chromatography after disposed. Control group members were infused 5 Fu (50 mg/kg) by ear marginal vein and then blood and stomach tissue samples taken at different times were analysed with the same method. Results The drug concentration time curve of portal vein and peripheral vein both reached the peak at the fifth minute after drug administration in the two methods, then declined quickly and slowed down after 30 minutes, according with two house models. The drug concentration in portal vein of the experimental group was obviously higher than in the peripheral vein and also higher than in the portal vein of the controll group maintaining for a longer period. Drug concentration in stomach tissue of experimental group was 11 times of that of control group at the fifth minute and was similar after 2 hours in both methods groups.Conclusions Drug concentration in blood of portal vein and stomach tissue can maintain a higher level in a longer period with the same local effect after left gastric arterial infusion chemotheraphy showing high chemotherapeutic efficiency.