紫杉醇不同剂型对大鼠血浆中游离药物浓度的影响  

Effects of Different Formulations on Plasma Free Concentration of Paclitaxel in Rats

作　　者：毋海兰 马智宇[2] 张淑秋[1] 钟大放[2] 陈笑艳[2] 

机构地区：[1]山西医科大学药学院,山西太原030001 [2]中国科学院上海药物研究所,上海201203

出　　处：《中国医药工业杂志》2016年第11期1430-1435,共6页Chinese Journal of Pharmaceuticals

摘　　要：研究白蛋白结合型紫杉醇（Abraxane ）、胶束化紫杉醇（Genexol -PM）和紫杉醇注射液（Taxol ）在大鼠血浆中游离药物浓度的差异，并考察冻-融处理对其中游离紫杉醇测定的影响。雄性SD大鼠静脉注射紫杉醇制剂，采集给药后2和4h血浆样品，经3次-70℃冻．融，用快速平衡透析（RED）法处理。以多西他赛为内标，建立了液相色谱．串联质谱法测定血浆游离紫杉醇浓度。结果表明，白蛋白结合型紫杉醇和胶束化紫杉醇在大鼠血浆中游离药物浓度差异不显著（P〉0．05），但明显高于紫杉醇注射液的游离药物浓度。血浆样品冻-融3次后不影响游离药物浓度的测定（P〉0．05）。The differences of the free concentrations of albumin-bound paclitaxel （Abraxane ）, micellar paclitaxel （Genexol -PM） and paclitaxel injection （Taxol ） in rat plasma, as well as the effect of plasma freezeingthawing cycles on the determination of free paclitaxel concentration in plasma were investigated. After an intravenous administration of Abraxane , Genexol -PM and Taxol to SD male rats, plasma samples were collected at 2 and 4 h, and by three cycles of freezing （-70 ℃） and thawing. A LC-MS/MS method was established for the determination of the free paclitaxel concentration in rat plasma prepared using the rapid equilibrium dialysis （RED） method. The results showed that no significant difference was observed between Abraxane and Genexol -PM about the free drug concentrations in rat plasma （P〉0.05）, but it was significantly higher than that of Taxol . Plasma samples after three freezing-thawing cycles did not affect the determination of free drug concentration （P〉0.05）.

关 键 词：紫杉醇 白蛋白结合型紫杉醇 胶束化紫杉醇 紫杉醇注射液 血浆游离率 快速平衡透析法 液相色谱-串联 质谱法 

分 类 号：O657.72[理学—分析化学]