奥沙利铂磷脂复合物及其纳米混悬剂的制备

目的研究奥沙利铂磷脂复合物及其纳米混悬液的制备方法。方法以奥沙利铂与磷脂的复合率为指标,采用单因素和正交试验设计优化了奥沙利铂磷脂复合物的制备工艺。采用逆相蒸发法结合高压均质技术,将奥沙利铂磷脂复合物制成纳米混悬液,并进行理化性质考察。结果奥沙利铂与磷脂的复合率可达100%。制备的纳米混悬液载药量提高到10 g.L-1,平均粒径为(126±17)nm,具有良好的物理稳定性。结论磷脂复合物改善了奥沙利铂的理化性质及溶解性能,用其制备的纳米混悬剂可静脉给药。

Preparation of oxaliplatin phospholipid complex and its nanosuspension

Objective To study the preparation methods for oxaliplatin phospholipid complex(OPPLC) and its nanosuspension.Methods The preparation conditions of OPPLC were optimized by single factor test and orthogonal design using binding ratio of oxaliplatin to phospholipid as evaluation parameter.The OPPLC nanosuspension was prepared by reverse-phase evaporation methods and high pressure homogenization and the physicochemical properties were studied.Results Oxaliplatin was complexed with phospholipid completely.The drug-loading rate of nanosuspension was 10 g·L-1 and the mean particle size was(126±17)nm.Good stability was also achieved.Conclusions The solubility and physicochemical properties of oxaliplatin were significantly improved by the prepared OPPLC.The nanosuspension enables the intravenous injection to be used in high dose with low toxicity and affords enhanced efficacy.