【摘要】 目的:考察不同量F-68修饰紫杉醇脂质体后对大鼠体内药动学行为的影响。方法:大鼠尾静脉注射未修饰紫杉醇脂质体、0.1%F-68修饰紫杉醇脂质体及0.2%F-68修饰紫杉醇脂质体,血浆处理以炔诺酮为内标,叔丁基甲醚提取。检测波长227 nm,甲醇-水(65∶35)为流动相,ODS-C18柱进行分析。结果:未修饰紫杉醇脂质体,0.1%F-68修饰紫杉醇脂质体及0.2%F-68修饰紫杉醇脂质体血浓经时曲线均符合二室模型,t1/2β分别为11.20,18.32和26.59 h,AUC0-1 440分别为2 541.99,2 760.315和3 369.456 mg.min/L。结论:F-68修饰后紫杉醇脂质体的大鼠体内药动学行为有明显的改变,消除半衰期和血中的循环时间均有不同程度的延长,AUC增加,且与F-68的用量成正相关。更多还原

【Abstract】 Aim:To evaluate the pharmacokinetics of F-68-modified paclitaxel liposomes（PTX-LP） in rats.Methods:Following administration of unmodified paclitaxel liposomes,0.1% F-68-modified paclitaxel liposomes and 0.2% F-68-modified paclitaxel liposomes to rats via tail veins,plasma sample was extracted with tert-butyl methyl ether and added norethisterone as internal standard.Analyses were performed on a C₁₈ column with the mobile phase consisting of methanol-water（65∶35） and UV-detector set at 227 nm.Results:It was found that the plasma concentration-time profile in rats after dosing of three formulations fitted bi-exponential disposition.Magnitudes of estimated t_1/2β were 11.20,18.32 and 26.59 h,respectively,and AUCs were calculated to be 2 541.99,2 760.315 and 3 369.456 mg·min/L,respectively.Conclusion:Significant changes to in vivo disposition in rats were observed after F-68 modification to PTX-LP when compared with unmodified PTX-LP.This kind of long circulation had a positive correlation with the quantities of F-68 attached.更多还原