论文部分内容阅读
目的:考察隐形依托泊苷脂质体在大鼠体内的药动学及组织分布。方法:采用高效液相色谱法测定大鼠血液及各组织中依托泊苷的浓度。结果:大鼠单剂量静脉注射4mg·kg-1依托泊苷隐形脂质体及市售注射液后,药时数据均符合二室模型,隐形脂质体的主要药动学参数为:T1/2α为(2.26±0.25)h,T1/2β为(17.44±2.07)h,AUC为(56.13±8.21)μg·mL-1.h;注射液T1/2α为(0.08±0.02)h,T1/2β为(1.24±0.19)h,AUC为(2.16±0.50)μg·mL-1.h。组织分布结果表明,隐形脂质体给药15min后,肺内的药物浓度最高,其次是肝、脾、心和肾等组织,随后浓度缓慢下降,在2～12h内长时间保持低浓度。结论:隐形依托泊苷脂质体延长了依托泊苷在血液及组织中的循环时间,具有缓释作用。
Objective: To investigate the pharmacokinetics and tissue distribution of stealth etoposide liposomes in rats. Methods: The contents of etoposide in blood and tissues of rats were determined by high performance liquid chromatography. Results: After a single dose of 4 mg · kg-1 etoposide stearic liposome and a commercially available injection, the pharmacokinetic parameters of the stealth liposomes were consistent with the two-compartment model. The main pharmacokinetic parameters of the stealth liposomes were T1 / T1α 2α was (2.26 ± 0.25) h, T1 / 2β was (17.44 ± 2.07) h, AUC was (56.13 ± 8.21) μg · mL- 2β was (1.24 ± 0.19) h, AUC was (2.16 ± 0.50) μg · mL-1.h. Tissue distribution results showed that the drug concentration in the lung was the highest, followed by the liver, spleen, heart and kidney tissues after 15min administration of the stealth liposomes, followed by a slow decrease in concentration, and remained low for a long time within 2 ~ 12h. Conclusion: Stealth etoposide liposome prolongs the circulation time of etoposide in the blood and tissues, and has a sustained release effect.