环维黄杨星D和羟丙基-β-环糊精的包合作用研究

目的]研究环维黄杨星D和羟丙基-β-环糊精的包合作用,寻找改善环维黄杨星D制剂性能的方法。方法]采用相溶解度法研究环维黄杨星D和羟丙基-β-环糊精在水溶液中的包合作用;溶液搅拌法制备包合物;差示扫描量热法验证包合物的形成。比较了环维黄杨星D和包合物体外溶出度。结果]在水溶液中环维黄杨星D和羟丙基-β-环糊精能够形成摩尔比为1∶1的包合物,包合反应是可以自发进行的放热过程。包合后环维黄杨星D10 min内的溶出度由14.7%提高到86.4%。结论]环糊精包合技术显著提高了环维黄杨星D的溶解度和溶出度。

Study on the Inclusion Complex of Cyclovirobuxine D and Hydroxypropyl-β-cyclodextrin

Objective] The inclusion complex of cyclovirobuxine D and hydroxypropyl-β-cyclodextrin was investigated to improve the performance of the cyclovirobuxine D preparation.Method] In aqueous solution,the inclusion complex of cyclovirobuxine D/hydroxypropyl-β-cyclodextrin was studied by phase solubility.The inclusion complex was prepared by solution-agitation technology and was confirmed by DSC.At the same time,the dissolution of cyclovirobuxine D and inclusion complex were measured.Result] A molar ratio inclusion complex(1∶1) of cyclovirobuxine D with hydroxypropyl-β-cyclodextrin in aqueous solution was spontaneously thermopositive process.Inclusion with hydroxypr-opyl-β-cyclodextrin,the dissolution rate of cyclovirobuxine D in 10 minutes increased from 14.7% to 86.4%.Conclusion] The solubility and dissolution of cyclovirobuxine D were improved remarkably with hydroxypropyl-β-cyclodextrin.