隐形依托泊苷脂质体在大鼠体内的药动学及组织分布
李津明;车环宇;李鑫;张彦卓;李博
【期刊名称】《中国新药杂志》 【年(卷),期】2009(018)023
【摘要】Objective:To study pharmacokinetics and tissue distribution of stealth etoposide liposomes in rats. Methods: The drug concentration of etoposide in rat blood circulating system and various tissues were deter-mined by high-performance liquid chromatograph (HPLC). Results: Following intravenous injection administration at the dose of 4 mg · kg~(-1) etoposide, the two-compartment model discribed the two kinds of etoposide preparations.The main pharmacokinetic parameters of stealth liposomes were as follows:T_(1/2)α (2.26 ±0.25)h,T_(1/2)β (17.44 ±2.07)h,and AUC (56. 13 ±8.21) μg·mL~(-1) · h,respectively. The main pharmacokinetic parameters of injection were T_(1/2)α(0.08 ±0.02)h,T_(1/2)β (1.24 ±0. 19)h,and AUC (2. 16 ±0.50) μg·mL~(-1) ·h,respectively. In tissue distribution, the concentration of etoposide in the lung was the highest and those in the liver, spleen, heart and kid-ney was lower sequentially at 15min after intravenous injection stealth liposomes, then drug concentration descended slowly compared with injections and remained at low level from 2 h to 12 h. Conclusion: Stealth Etoposide lipo-somes for intravenous injection could extend the duration of etoposide in blood and tissue.%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4 mg·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:T_(1/2)α
为(2.26±0.25)h,T_(1/2)β
为(17.44±2.07)h,AUC
为
(56.13±8.21)μg·mL~(-1)·h;注射液T_(1/2)α为(0.08±0.02)h,T_(1/2)β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15 min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2～12 h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. 【总页数】5页(2269-2272,2277)
【关键词】依托泊苷;高效液相色谱法;组织分布;药动学 【作者】李津明;车环宇;李鑫;张彦卓;李博
【作者单位】哈尔滨商业大学药学院,哈尔滨,150076;哈尔滨商业大学药学院,哈尔滨,150076;哈尔滨商业大学药学院,哈尔滨,150076;沈阳药科大学药学院,沈阳,110016;广东省食品药品职业学院,广州,510520 【正文语种】中文
【中图分类】R9413.41;R979.1 【文献来源】
https://www.zhangqiaokeyan.com/academic-journal-cn_chinese-journal-new-drugs_thesis/0201242226803.html 【相关文献】
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隐形依托泊苷脂质体在大鼠体内的药动学及组织分布
