WU Yijie, QIAO Zhenzhen, WEI Yue, et al. Preparation and characterization of ciclopirox olamine-β-cyclodextrin inclusion complex. [J]. Journal of Southwest Medical University 43(6):548-553(2020)
WU Yijie, QIAO Zhenzhen, WEI Yue, et al. Preparation and characterization of ciclopirox olamine-β-cyclodextrin inclusion complex. [J]. Journal of Southwest Medical University 43(6):548-553(2020)DOI:
Preparation and characterization of ciclopirox olamine-β-cyclodextrin inclusion complex
Objective:To investigate the solubilization effect of β-cyclodextrin(β-CD)on ciclopirox olamine(CPX)using the β-CD inclusion technology
and to improve the solubility and absorption of CPX
optimize the clinical preparation of CPX
promote drug absorption by the skin
and improve the bioavailability of such drugs.Methods:The ultrasonic method was used to prepare CPX-β-CD inclusion complex
and an infrared spectrometer and a scanning electron microscope were used for phase identification.High-performance liquid chromatography was used to measure the content and calculate inclusion rate and release rate
and in vitro release assay was used to observe the effect of β-CD inclusion complex on the drug release of CPX.Results:The optimal chromatographic conditions were a flow rate of 1.0 mL/min
a detection wavelength of 304 nm
a column temperature of 30℃
active compound 200 μg/mL
an injection volume of 5 μL
and a mobile phase of acetonitrile and 0.1% EDTA-2 Na(v/v
45∶55).The detection concentration of CPX showed a good linear relationship within the range of 20.0 ~ 200.0 μg/mL(R2= 0.9998).Relative standard deviation was < 2% for precision
repeatability
stability
and recovery.At a ratio of 1∶2 for CPX and β-CD
the inclusion complex prepared by the ultrasonic method had the highest inclusion rate of 47.72%.The inclusion complex had a higher drug release amount than the bulk drug of CPX at each time point
suggesting that the inclusion action can improve the release efficiency of CPX.Conclusion:CPX-β-CD inclusion complex is successfully prepared in this experiment
and the preparation process is simple and feasible.The prepared CPX-β-CD inclusion complex has high stability and can effectively improve the release efficiency of CPX.