Preparation and characterization of armodafinil nanocrystals / 国际药学研究杂志

ABSTRACT

Objective: To prepare and characterize armodafinil nanocrystals, and investigate its release in vitro. Methods: 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. Results: The 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. Conclusion: The 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.