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目的:研究磺丁醚-β-环糊精与羟基喜树碱活性结构包合作用,寻找既能改善羟基喜树碱溶解度又能保持其活性结构的新方法。方法:采用计算机模拟计算法、紫外分光光度法预测磺丁醚-β-环糊精分别对羟基喜树碱开环结构和活性内酯结构包合作用的可能性,并比较强弱;酸碱法制备包合物;UV法测定包合物的溶解度和稳定性;HPLC法测定包合物中以活性内酯结构形式存在的羟基喜树碱含量。结果:磺丁醚-β-环糊精与羟基喜树碱形成包合物后,药物的溶解度由0.22μg.mL-1增至1.01 mg.mL-1;药物主要以活性内酯结构形式存在,其含量由63.2%增至96.8%;包合物室温放置12个月内稳定。结论:磺丁醚-β-环糊精可提高羟基喜树碱的溶解度并保持其内酯结构,该技术可用于改进羟基喜树碱药物剂型。
OBJECTIVE: To study the inclusion complex of sulfobutylether-β-cyclodextrin and hydroxycamptothecin in order to find a new method that can improve the solubility of hydroxycamptothecin and maintain its active structure. Methods: Using computer simulation method and UV-spectrophotometry to predict the possibility of sulfobutyl ether-β-cyclodextrin to the inclusion of hydroxycamptothecin ring structure and active lactone structure respectively, Method was used to prepare the inclusion complex. The solubility and stability of the inclusion complex were determined by UV method. The content of hydroxy camptothecin in the inclusion complex as the active lactone structure was determined by HPLC. Results: The solubility of sulfobutylether-β-cyclodextrin and hydroxycamptothecin was increased from 0.22μg.mL-1 to 1.01 mg.mL-1 after the inclusion complex was formed. The drug mainly existed in the active lactone structure , Its content increased from 63.2% to 96.8%; inclusion complex was stable within 12 months at room temperature. CONCLUSIONS: Sulfobuet-β-cyclodextrin enhances hydroxycamptothecin solubility and maintains its lactone structure, a technique that can be used to improve hydroxycamptothecin drug dosage forms.