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目的:考察泊洛沙姆188(poloxamer188)修饰的蜂毒素脂质体在大鼠体内的药动学。方法:大鼠尾静脉分别注射蜂毒素溶液(MLT-I)、2%及5%Poloxamer188修饰的蜂毒素脂质体(MLT-LIPO-2%和MLT-LIPO-5%),采用酶联免疫吸附(ELISA)方法测定大鼠体内的蜂毒素。结果:采用Kinetica4.4统计软件,经统计矩拟合后,与MLT-I相比,MLT-LIPO-2%和MLT-LIPO-5%在大鼠体内的药动学行为发生显著变化,清除率(CL)分别为溶液组的48.3%及33.2%;血药浓度-时间曲线下面积(AUC)分别为溶液组的2.01倍及2.82倍;平均滞留时间(MRT)分别为溶液组的1.80倍及2.18倍。结论:经poloxamer188修饰后的脂质体显著延长了药物在大鼠体内的驻留时间,提高了药物的生物利用度,且与膜修饰剂的用量有一定的正相关性。
Objective: To investigate the pharmacokinetics of poloxamer 188 modified melittin liposome in rats. METHODS: Melittin solution (MLT-I), MLT-LIPO-2% and MLT-LIPO-5% modified by 2% and 5% Poloxamer188 were injected into the tail vein of rats, Determination of melittin in rat by adsorption (ELISA) method. Results: Compared with MLT-I, the pharmacokinetics of MLT-LIPO-2% and MLT-LIPO-5% in rats were significantly changed after statistical fitting by Kinetica 4.4 software. (CL) were 48.3% and 33.2%, respectively. The area under the plasma concentration-time curve (AUC) was 2.01 and 2.82 times higher than that of the solution group. The average retention times (MRTs) were 1.80 times And 2.18 times. Conclusion: Poloxamer188 modified liposomes significantly prolong the drug residence time in rats and improve the bioavailability of the drug, and the amount of membrane modifier has a certain positive correlation.