摘要
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 lactone moiety of 10-hydroxycamptothecin and SBE-β-CD for keeping its lactone moiety and improving its solubility.Methods：The formulary of the inclusion complex of 10-hydroxycamptothecin＇s lactone moiety and ring cleavage moiety with SBE-β-CD was calculated by computer simulation and UV spectra method,respectively.The inclusion compound was prepared by acid-base method.The solubility and stability of inclusion complex was determined by UV method.The content of lactone moiety of 10-hydroxycamptothecin was determined by HPLC method.Results：The results showed that the solubility of 10-hydroxycamptothecin was increased by 5 000 times from 0.22 μg·mL^-1 to 1.01 mg·mL^-1 after being included into SBE-β-CD with lactone moiety.The content of lactone moiety was increased from 63.2% to 96.8%.The inclusion complex was stable within 12 months at room temperature.Conclusion：SBE-β-CD could improve the solubility of 10-hydroxycamptothecin and keep its lactone moiety.It is feasible that SBE-β-CD could be used to improve the performance of 10-hydroxycamptothecin hydrochloride formulary.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2010年第14期1270-1274,共5页
Chinese Journal of New Drugs
