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目的:制备伏立康唑白蛋白纳米粒,并考察其在大鼠体内药动学与及组织分布。方法:采用超高压微射流技术制备伏立康唑白蛋白纳米粒,并评价了白蛋白纳米粒的粒径分布、Zeta电位、外观形态以及体外释药行为;考察了伏立康唑白蛋白纳米粒在大鼠体内的药动学与组织分布特征。结果:本研究制备的伏立康唑白蛋白纳米粒平均粒径为(121.9±41.6)nm,Pd I为0.197,Zeta电位为(-42.1±0.9)m V,呈球形或类球形分布;伏立康唑白蛋白纳米粒在0.5%吐温80磷酸盐缓冲液(p H7.4)中24 h累积释放67.5%;大鼠体内药动学研究表明,伏立康唑白蛋白纳米粒和伏立康唑注射剂的AUC_(0-24)分别为(98.27±1.42)和(105.32±1.45)g·h·L~(-1),MRT_(0-24)分别为(4.48±0.38)和(4.86±0.51)h;伏立康唑白蛋白纳米粒能增加药物在大鼠肝、脾、脑中的靶向性。结论:伏立康唑白蛋白纳米粒在大鼠体内具有良好的肝、脾、脑中靶向性,可以提高药物治疗疗效。
OBJECTIVE: To prepare voriconazole albumin nanoparticles and study its pharmacokinetics and tissue distribution in rats. Methods: Voriconazole nanoparticles were prepared by ultra-high pressure micro-jet technique. The particle size distribution, Zeta potential, appearance morphology and in vitro release of albumin nanoparticles were evaluated. The effects of voriconazole albumin nanoparticles Pharmacokinetics and Tissue Distribution Characteristics. Results: The average particle size of voriconazole albumin nanoparticles prepared in this study was (121.9 ± 41.6) nm, with a Pd I of 0.197 and a zeta potential of (-42.1 ± 0.9) m V, showing spherical or spheroidal distribution. Voriconazole albumin nanoparticles The granules released 67.5% in 24 h in 0.5% Tween 80 phosphate buffer (p H7.4). Pharmacokinetic studies in rats showed that AUC 0-24 of voriconazole albumin nanoparticles and voriconazole injection respectively (98.27 ± 1.42) and (105.32 ± 1.45) g · h · L -1, (4.48 ± 0.38) and (4.86 ± 0.51) h for MRT_ (0-24), respectively. Voriconazole albumin nanoparticle energy Increase the drug in rat liver, spleen, brain targeting. CONCLUSION: Voriconazole nanoparticles have good targeting in liver, spleen and brain in rats, which can improve the curative effect of drugs.