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目的:制备多烯紫杉醇磺丁基醚-β环糊精(SEB-β-CD)包合物,提高药物的溶解度。方法:采用冷冻干燥法制备包合物,考察磺丁基醚-β-环糊精与药物在不同主客分子比例、不同制备时间、不同制备温度时多烯紫杉醇的增溶作用,并利用差示扫描量热法(DSC)、红外光谱法(IR)、X-射线衍射法和1H-NMR核磁共振法对所制备的包合物进行结构验证,选择最佳制备工艺。结果:当药物与SEB7-β-CD摩尔比均为1∶70,制备时间2h,制备温度25℃时,多烯紫杉醇增溶效果最好,溶解度为442.21mg.L-1。经结构验证,说明形成包合物。结论:利用制备多烯紫杉醇环糊精包合物的方式,可显著提高药物的溶解度。
OBJECTIVE: To prepare the inclusion compound of docetaxel sulfobutyl ether-β-cyclodextrin (SEB-β-CD) to improve the solubility of the drug. Methods: The inclusion complex was prepared by freeze-drying method. The solubilization of docetaxel by sulfobutylether-β-cyclodextrin and drug was investigated at different ratios of host-guest molecules, different preparation time and different preparation temperature. Scanning calorimetry (DSC), infrared spectroscopy (IR), X-ray diffraction and 1H-NMR were used to verify the structure of the inclusion compound. The best preparation process was selected. Results: When the molar ratio of drug to SEB7-β-CD was 1:70 and the preparation time was 2h, the best solubilization effect of docetaxel was obtained when the preparation temperature was 25 ℃. The solubility was 442.21mg.L-1. The structural verification, indicating the formation of inclusion complexes. Conclusion: The preparation of docetaxel cyclodextrin inclusion complex can significantly improve the drug solubility.