多西他赛长循环脂质体的制备与大鼠体内药动学评价

发布时间：2018-08-05 14:12

【摘要】：目的:制备多西他赛长循环脂质体,并评价大鼠尾静脉给药的药动学特性。方法:采用薄膜分散-挤出法制备多西他赛长循环脂质体,并对其粒径分布、Zeta电位和微观形态进行表征。将12只Wistar大鼠随机分为多西他赛注射液组和多西他赛长循环脂质体组,尾静脉给药剂量均为7.5 mg·kg~(-1),采用HPLC法测定大鼠血中多西他赛的药物浓度,采用3P97程序计算多西他赛大鼠体内药动学参数。结果:多西他赛长循环脂质体平均粒径为(109.2±28.6)nm,Zeta电位为(~(-1)5.8±2.7)m V。多西他赛注射液和多西他赛长循环脂质体在大鼠体内的t_(1/2(α))分别为(0.19±0.05)h和(0.36±0.07)h;t_(1/2(β))分别为(1.82±0.33)h和(17.93±1.37)h;AUC0-t分别为(4.42±0.76)μg·ml~(-1)·h~(-1)和(33.73±3.52)μg·ml~(-1)·h~(-1)。结论:多西他赛长循环脂质体与市售多西他赛注射液相比,延长了药物在血浆中的滞留时间,能达到长循环目的。
[Abstract]:Aim: to prepare docetaxel circulating liposomes and evaluate the pharmacokinetic characteristics of caudal vein administration in rats. Methods: docetaxel circulating liposomes were prepared by thin-film dispersion-extrusion method, and their particle size distribution, Zeta potential and micromorphology were characterized. Twelve Wistar rats were randomly divided into two groups: docetaxel injection group and docetaxel long-circulating liposome group. The dosage of docetaxel was 7.5 mg kg ~ (-1) by tail vein. The concentration of docetaxel in blood was determined by HPLC method. The pharmacokinetic parameters of docetaxel rats were calculated by 3P97 program. Results: the average particle size of docetaxel circulating liposome was (109.2 卤28.6) nm Zeta potential (~ (-1) 5.8 卤2.7) m V.). T _ (1 / 2 (伪) of docetaxel injection and docetaxel long circulating liposome in rats were (0.19 卤0.05) h and (0.36 卤0.07) h respectively, (1.82 卤0.33) h and (17.93 卤1.37) hAUC0-t were (4.42 卤0.76) 渭 g ml ~ (-1) h ~ (-1) and (33.73 卤3.52) 渭 g ml ~ (-1) h ~ (-1), respectively. Conclusion: compared with docetaxel injection, docetaxel long-circulating liposome can prolong the retention time of drug in plasma and achieve long circulation.
【作者单位】：大连市妇女儿童医疗中心药剂科;大连市旅顺口区人民医院药剂科;
【分类号】：R943;R965

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