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目的:研究阿苯达唑纳米脂质体冻干粉在大鼠体内的药动学过程及肝脏靶向性。方法:大鼠以灌胃给予阿苯达唑片、阿苯达唑脂质体及阿苯达唑纳米脂质体冻干粉,分别于给药后不同时间点取血及肝脏,样品预处理后利用高效液相色谱(HPLC)法测定血浆及肝组织中药物浓度,考察3种制剂的药动学参数及肝靶向性差异。结果:阿苯达唑纳米脂质体冻干粉主要药动学参数如下:C_(max)为(7.05±0.70)μg·mL~(-1),t_(max)为(6.15±0.66)h,AUC_(0-∞)为(150.9±12.1)μg·mL~(-1)·h,以阿苯达唑片、阿苯达唑脂质体为参比制剂,阿苯达唑纳米脂质体冻干粉相对生物利用度分别为236.04%和178.45%;肝靶向试验结果显示:阿苯达唑纳米脂质体冻干粉在肝组织中的分布显著高于阿苯达唑片和阿苯达唑脂质体。结论:将阿苯达唑脂质体制成纳米级脂质体冻干粉后,可显著提高药物的相对生物利用度和肝靶向性。
Objective: To study the pharmacokinetics and liver targeting of albendazole nanoliposomes lyophilized powder in rats. METHODS: Albendazole tablets, albendazole liposomes and albendazole nanoliposome lyophilized powder were intragastrically administered to rats. Blood and liver were taken at different time points after administration, and the samples were pretreated The concentrations of the drugs in plasma and liver tissue were determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters and liver targeting differences of the three preparations were investigated. Results: The main pharmacokinetic parameters of albendazole nanoliposomes were as follows: C max 7.05 ± 0.70 μg · mL -1, t max 6.15 ± 0.66 h , And the AUC_ (0-∞) was (150.9 ± 12.1) μg · mL -1 · h. The albendazole tablets and albendazole liposomes were used as reference preparations, albendazole nanoliposomes The relative bioavailability of lyophilized powder was 236.04% and 178.45%, respectively. The results of liver targeting test showed that the distribution of albendazole nano-liposomes in liver tissue was significantly higher than that of albendazole tablets Benzodiazepine liposomes. CONCLUSION: After the albendazole liposomes are made into nano-sized liposomes, the relative bioavailability and liver targeting of the drug can be significantly improved.