目的 为了提高低水溶性抗真菌药物酮康唑（ketoconazole，KCZ）的水溶性及抑菌活性，减少临床应用限制。 方法 采用饱和溶液法制备酮康唑-甲基-β-环糊精包合物，高效液相色谱法（HPLC）检测其溶解度，通过傅里叶变换红外光谱（IR）法对其结构进行表征，用纸片扩散法（K-B法）和最小抑菌浓度(MIC)方法对比检验酮康唑原药与酮康唑-甲基-β-环糊精包合物对白色假丝酵母菌的体外抗菌活性。 结果 通过甲基-β-环糊精包合，酮康唑在包合物中的水溶性比单一酮康唑增加了约2 941倍，通过傅里叶变换红外光谱（IR）法证实了有新物相形成。酮康唑原药的抑菌圈为（22.00±1.63） mm，酮康唑-甲基-β-环糊精包合物的抑菌圈则提升至（28.00±1.63） mm。最低抑菌浓度结果显示，酮康唑原药的最低抑菌浓度为（0.125±0.029） μg/mL，酮康唑-甲基-β-环糊精包合物的最低抑菌浓度为（0.062 5±0.015 0） μg/mL。 结论 酮康唑-甲基-β-环糊精包合物不仅没有破坏酮康唑原药对白色假丝酵母菌原有的抑菌能力，还提高了其抑菌效果。

Objectives In order to improve the water solubility and antibacterial activity of the low water-soluble antifungal drug ketoconazole (KCZ) and reduce the limits of clinical application. Methods The inclusion complex of ketoconazole-methyl-β-cyclodextrin was prepared with the saturated solution method. The water solubility of the inclusion complex was measured with high-performance liquid chromatography (HPLC). Fourier transform infrared spectroscopy (IR) was used to characterize the structure of the inclusion complex. The in vitro antibacterial activity of the single ketoconazole and the inclusion complex of ketoconazole-methyl-β-cyclodextrin against Candida albicin was comparatively tested with method of sheet diffusion (K-B) and minimum inhibitory concentration (MIC). Results The water solubility of ketoconazole in the inclusion complex was about 2 941 times higher than that of single ketoconazole through the inclusion of methyl-β-cyclodextrin. The formation of new phases was confirmed by Fourier transform infrared spectroscopy (IR). The antibacterial zone of single ketoconazole and the inclusion complex was (22.00±1.63) mm and (28.00±1.63) mm. The minimum inhibitory concentration (MIC) of single ketoconazole and the inclusion complex was (0.125±0.029) μg/mL and (0.062 5±0.015 0) μg/mL. Conclusions The inclusion complex of ketoconazole methyl-β-cyclodextrin did not destroy the original antibacterial ability of ketoconazole against Candida albicans, but improved its antibacterial effect.