泊那替尼纳米混悬剂冻干粉的制备及其质量评价

Preparation and quality evaluation of Ponatinib Nanosuspension Lyophilized Powder

目的制备泊那替尼纳米混悬剂冻干粉,并对其冻干保护剂、载药量及稳定性进行考察。方法采用溶剂蒸发技术制备泊那替尼纳米混悬剂冻干粉,利用激光纳米粒度仪、透射电镜对其粒径及形态进行表征,筛选最佳冻干保护剂,利用高效液相色谱法对其载药量和稳定性进行考察。结果泊那替尼纳米混悬剂冻干粉复溶后平均粒径为(92.2±5.6)nm,多分散指数为0.29±0.65,且形态圆整,分布均匀;以10%乳糖为冻干保护剂制得冻干粉的性质最佳;高效液相色谱法测得泊那替尼平均载药量为(16.3±0.8)%,稳定性较好。结论泊那替尼纳米混悬剂冻干粉制备方法简便,有望成为泊那替尼的新型纳米给药系统。

Objective To prepare Ponatinib Nanosuspension Lyophilized Power and investigate the cryoprotector, drug loading and stability. Methods Ponatinib Nanosuspension Lyophilized Power was prepared by solvent evaporation technology, the particle size and morphology were characterized by laser Manometer particle sizer and transmission electron microscopy （TEM）. The optimal cryoprotector was selected, the drug loading and stability of Ponatinib Nanosuspension Lyophilized Power were determined by HPLC. Results The mean diameter of redissolved Ponatinib Nanosuspension Lyophilized Power was （92.2±5.6） nm, with polydisperse index of 0.29±0.65. TEM images showed spherical shape and uniform distribution. The nanosuspension which was lyophilized with 10% lactose presented optimal properties. The mean drug loading of Ponatinib Nanosuspension Lyophilized Power determined by HPLC was （16.3±0.8）%, with a good stability. Conclusion The preparation method of Ponatinib Nanosuspension Lyophilized Power is simple, which promises to be a novel Manometer drug delivery system for injection of Ponatinib.