Preparation and in vitro Property of Voriconazole Sulfonated Butyl Ether-β-Cyclodextrin Inclusion Compound / 中国药师

ABSTRACT

Objective: To prepare voriconazole (VCZ) sulfonated butyl ether-β-cyclodextrin (SBE-β-CD) inclusion compound and study the properties in vitro.Methods: VCZ SBE-β-CD inclusion compound was prepared respectively by a stirring method, an ultrasonic method and a grinding method, and the one with the highest inclusion rate and inclusion compound yield was chosen as the final preparation method.The formula and preparation process were optimized by an orthogonal design.The inclusion compound was identified by differential scanning calorimetry and solubility determination, and the in vitro dissolution was determined as well.Results: The stirring method had the highest inclusion rate and inclusion compound yield, and the optimal preparation and formula conditions were as follows the inclusion temperature was 25℃, the stirring time was 4 h and the amount ratio of VCZ to SBE-β-CD was 1∶1.After the optimization, the inclusion rate was (86.14 ± 0.69)%, and the yield of inclusion compound was (97.11 ± 0.31)%.After the inclusion, the characteristic peak of VCZ disappeared and the solubility of VCZ increased significantly.Compared with those of VCZ, the dissolution rate and amount of VCZ inclusion compound both increased notably.Conclusion: VCZ SBE-β-CD inclusion compound can be prepared by the stirring method, which lays foundation for the further studies on VCZ eye drop.