Study on the preparation of β-cyclodextrin inclusion compound with ganciclovir

OBJECTIVE To prepare ganciclovir-β-cyclodextrin inclusion complex for better clinical application of ganciclovir by ilnproving water-solubility and stability.METHODS The inclusion complex was made by saturation water-solution.The orthogonal design method was employed to optimize the inclusion process concerning the utilization ration of ganciclovir in the base of the results of single-factor design.The inclusion compound was identified by UV and differential scanning calorimetry (DSC).The inclusion ration and the in vitro release characteristics were also investigated.RESULTS The optimum preparation conditions for inclusion were established as follows: the ratio of gancyclovir to β-cyclodextrin was 1∶10; the inclusion temperature was set at 60 ℃ and the inclusion time was 60 min.The inclusion ration of ganciclovir was 80.6%.Compared with gancyclovir aqueous solution,solubility of gancyclovir in the inclusion compound was increased from 3.23 mg·mL-1 to 34.22 mg·mL-1.CONCLUSION These results confirmed that the optimized process is simple and efficient.