紫杉醇冻干纳米乳在大鼠体内的药动学

The Pharmacokinetics of Lyophilized Paclitaxel Nanoemulsions in Rats

目的: 研究紫杉醇冻干纳米乳在大鼠体内的药动学特征.方法: 建立测定大鼠血浆中紫杉醇的HPLC-紫外检测法,大鼠股静脉注射给药后于不同时间点进行后眼眶静脉丛穿刺取血,测定其血浆中的血药浓度,并用3P97药动学程序对血药浓度进行处理.结果: 紫杉醇可与血浆中的其它成分较好地分离,在0.12～60 μg/mL的血药浓度范围内呈良好的线性关系.紫杉醇注射液和冻干纳米乳两种制剂大鼠静脉给药后体内药动学符合二室模型,后者AUC和MRT均大于前者.结论: 紫杉醇纳米乳可延长药物在大鼠体内的循环时间.

AIM： Study the pharmacokinetic characteristics of paelitaxel lyophilized nanoemulsions in rats. METHOD： A reversed-phase HPLC with UV detection was developed and validated for simultaneous analysis of paclitaxel in rat plasma. The plasma concentrations of paclitaxel were detected at various times following a femoral intravenous administration of paclitaxel at a close of 10 mg/kg body weight. The data was processed with the pharmacokinetic software 3P97. RESULT： A good separation of paclitaxel with other substances in plasma was obtained. The assay was liner over the range 0.12 ～ 60 μg/mL. The paclitaxel concentration-time curve profiles after iv. Both paclitaxel injections and nanoemulsions conformed to a two-compartment model. But the AUC and MRT of latter are bigger than the former. CONCLUSION： The nanoemulsions can prolong the circulating time of paclitaxel.