比较白蛋白纳米紫杉醇与含聚氧乙烯蓖麻油紫杉醇在乳腺癌患者的药代动力学  

Comparison the pharmacokinetics of nanoparticle albumin bound paclitaxel and solvent based paclitaxel in breast cancer patients

作　　者：李苏[1,2] 廖海[1,2] 詹靖[1,2] 邓丽婷[1,2] 滕小玉[1,2] 管忠震[1,2] 

机构地区：[1]华南肿瘤学国家重点实验室,广州510060 [2]中山大学肿瘤防治中心,广州510060

出　　处：《中国临床药理学杂志》2010年第8期606-610,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的考察注射用白蛋白纳米紫杉醇和含聚氧乙烯蓖麻油紫杉醇在乳腺癌患者中药代动力学行为及药效学的差异。方法 24例乳腺癌患者随机分成两组,A组:白蛋白纳米紫杉醇静脉推注30min;B组:含聚氧乙烯蓖麻油紫杉醇恒速静脉滴注3h。用液相质谱测定患者血浆和红细胞中紫杉醇的浓度并计算药代动力学参数,用秩和检验法检验两组药代参数的差异。结果 A组表观分布容积、清除率大于B组,有显著性差异(P=0.0002,P=0.0007);但两者MRT、t1/2、AUC0-∞相近。2组红细胞药物浓度分别为血液药物浓度(8.3%～28.1%)和(9.7%～24.7%)。结论 2种剂型紫杉醇的药代行为不同,白蛋白载体可增加紫杉醇向肿瘤的转运和蓄积。Objective To study the pharmacokinetics and efficacy be- tween the nanoparticle albumin bound paclitaxel injection and solvent based paclitaxel injection in breast cancer patients. Methods Twenty - four breast cancer patients were randomly divided into two groups, Group A for nanopaclitaxel injection （260 mg· m^-2 dosage）; Group B for paclitaxel injection （175 mg · m^-2 dosage）. Determinate the paclitaxel concentration in patients＇plasma and red blood cell content with the solid -phase extraction and LC/MS/MS method, using non -compartment model to calculate the pharmacokinetic parameters and find out the parameters differences of the two groups with Wilcoxon Kruskal - Wallis test. Results The pharmacokinetic behavior of the nano - paclitaxel injection （albumin -bound） is different with the paclitaxel injection, the former group＇ s Vss and CL are much large than the latter with significant differences; but their MRT, t1/2, AUC0-∞ are similar. The latter＇ s adjusted AUC0-∞/D is greater than the former, with significant differences. Conclusion The vivo pharmacokinetics parameters of nano - paclitaxel injection （ albumin - bound） in breast cancer patients were in superior to the ordinary agents, which can increase the transformation and accumulation of paclitaxel towards the cancer.

关 键 词：抗肿瘤药物 紫杉醇 白蛋白纳米紫杉醇 药代动力学 药效学 

分 类 号：R969.1[医药卫生—药理学] R978.5[医药卫生—药学]