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目的:研究注射用加替沙星聚氰基丙烯酸正丁酯纳米粒(GPN)的体内分布特征。方法:雄性小鼠随机分为3组,分别尾缘静脉给予小鼠加替沙星生理盐水溶液(Ⅰ)、未经修饰的加替沙星GPN(Ⅱ)以及经聚山梨酯-80修饰的GPN(T-GPN,Ⅲ),高效液相法检测血浆、肝、肾、脾及肺脏组织内的浓度,评价GPN的体内分布特征。结果:Ⅰ,Ⅱ,Ⅲ组小鼠肺脏组织中的平均峰浓度分别为17.33,10.13和26.99μg.g-1;平均浓度-时间曲线下面积(AUC0~t)分别为85.99,100.00和242.34 mg.kg-1.h。结论:GNP经聚山梨酯-80修饰后,加替沙星肺脏组织分布量显著增加,具有一定的肺靶向性。
OBJECTIVE: To study the in vivo distribution characteristics of gatifloxacin-loaded polybutylcyanoacrylate nanoparticles (GPN) for injection. Methods: Male mice were randomly divided into 3 groups: mice were given gatifloxacin saline (Ⅰ), unmodified gatifloxacin GPN (Ⅱ) and polysorbate 80 The plasma, liver, kidney, spleen and lung tissues were assayed by GPN (T-GPN, Ⅲ) and high performance liquid chromatography (HPLC) Results: The average peak concentrations in the lungs of mice in group Ⅰ, Ⅱ and Ⅲ were 17.33,10.13 and 26.99μg.g-1, respectively. The average area under the concentration-time curve (AUC0-t) were 85.99,100.00 and 242.34 mg .kg-1.h. CONCLUSION: The distribution of gatifloxacin in the lung tissue of GNP increased significantly after polysorbate-80 modification, with lung targeting.