静脉注射多烯紫杉醇纳米混悬剂的制备及性质考察

Preparation of docetaxel nanosuspension and its intravenous injection

目的:研究了多烯紫杉醇纳米混悬剂的制备方法及理化性质。方法:采用沉淀-高压匀质法制备多烯紫杉醇纳米混悬剂,以混悬粒子的粒径分布为指标,采用单因素和正交试验优化了纳米混悬剂的制备工艺,并进行理化性质考察。结果:多烯紫杉醇纳米混悬剂的平均粒径为(184±80)nm,药物浓度可达到5 mg.mL-1,其饱和溶解度经测定为20.4μg.mL-1,是药物粗颗粒的3.15倍,48 h的体外累积溶出百分率是药物粗颗粒的3倍以上。结论:多烯紫杉醇纳米混悬剂改善了药物的体外溶出速率,增加了载药量,提高了制剂的生物安全性,可供静脉注射使用。

Objective：To prepare and study the docetaxel nanosuspension and its intravenous injection.Methods：The preparation parameters of docetaxel nanosuspension were optimized by the single factor and orthogonal design using precipitation-homogenization method.The size distribution of nano-crystals were utilized as index to evaluate the parameters of precipitating temperature,agitating velocity,phospholipids ratio,drug loading and homogenization parameters.Particle diameter,solubility and in vitro release profile were measured.Results：The particle diameter of the injection was（184±80） nm.The solubility of DCT nanosuspension was 20.4 μg·mL-1,3 times of drug particles.The in vitro release profile of the injection exhibited an obvious fast release character.Conclusion：A DCT nanosuspension intravenous injection with high solubility and fast release profile was produced via the precipitation-homogenization process precipitation-homogenization process.