阿莫达非尼纳米晶体的制备与表征

Preparation and characterization of armodafinil nanocrystals

目的制备阿莫达非尼纳米晶体,并进行性质表征、体外释放度考察。方法采用反溶剂沉淀技术制备其纳米晶体,以平均粒径为评价指标,采用正交设计实验优化其纳米混悬液的处方及制备工艺,通过冷冻干燥技术将纳米混悬液制备成纳米晶体。测定阿莫达非尼纳米晶体的粒径和多分散系数;采用X线粉末衍射法考察阿莫达非尼晶型转变情况;采用浆法比较其纳米晶体及原料药的溶出行为。结果制备阿莫达非尼纳米晶体粒径较小且均一,粒径约为100 nm,呈无定型形态;制成纳米晶体后,溶解度和溶出度明显提高;纳米化后阿莫达非尼晶型较纳米化前发生明显改变。结论粒径小且均匀的阿莫达非尼纳米晶体,可明显提高阿莫达非尼的溶出性能,有利于改善药物的生物利用度。

Objective Anti-solvent precipitation technology was used to prepare the armodafinil nanocrystals.The formulation and preparation process of the armodafinil nanosuspension were optimized by the orthogonal design experiment with the average particle diameter as the evaluation index.The suspension was prepared into nanocrystals by freeze-drying technology.The particle size and the polydispersity coefficient of the armodafinil nanocrystals were measured.The X-ray powder diffraction method was used to investigate the crystal form transition of the armodafinil.The dissolution behavior of the armodafinil nanocrystals and raw substances was investigated and compared with each other by the slurry method.ResultsThe prepared amodafinil nanocrystals had a quite uniformly distributed particle size around 100 nm.The nanocrystals appeared to be in irregular form.After amodafinil was made into nanocrystals,the solubility and dissolution were significantly improved.The crystal form of amodafinil significantly changed after nanocrystallization.ConclusionThe preparation of a small and uniformly distributed particle size of amodafinil nanocrystals could significantly improve the dissolution performance of amodafinil,which is beneficial to improving the bioavailability of insoluble drugs.