Preparation and Image Identification of Fenbendazole-methyl-β-cyclodextrin
[Objective]This study was aimed to improve the water solubility and dissolution rate of the insoluble veterinary drug fenbendazole(FBZ)and improve the therapeutic effect of the drug in clinical application.[Method]Fbendazole-methyl-β-cyclodextrin inclusion complex(FBZ-Me-β-CD)was prepared by constant temperature magnetic stirring method and freeze-drying technique.Through the design of single factor orthogonal test,the optimum preparation technology of inclusion complex was studied with the inclusion rate and recovery rate as the index.According to the solubilization effect of 5 different cyclodextrins on drugs,the best inclusion material was determined by phase solubility test.High performance liquid chromatography(HPLC)was used to detect the solubility,inclusion rate and in vitro dissolution rate of the inclusion complex.Finally,the phase structure of the inclusion complex was characterized by differential scanning calorimetry(DSC)and scanning electron microscopy(SEM).[Result]The optimum preparation process of inclusion complex was as follows:Stirring time was 3 h,rotational speed was 600 r/min,molar ratio of subject to guest was 1∶3,temperature was 50 ℃.The best inclusion material was methyl-β-cyclodextrin.The solubility of the inclusion complex in water was 12.02 mg/mL,which was 40 000 times that of fenbendazole(0.3 μg/mL).The dissolution rate of the inclusion complex in vitro was 7 times that of fenbendazole.The average recovery and inclusion rate of the inclusion compounds were 89.50％and 29.20％,respectively.By scanning electron microscopy and differential scanning calorimetry,fenbendazole and cyclodextrin were identified as amorphous inclusion states.[Conclusion]In this study,the solubility and dissolution rate of the insoluble drug fenbendazole were improved by preparing the cyclodextrin inclusion complex of fenbendazole,and the preparation method was simple and easy,which was conducive to the further study of fenbendazole.
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