作　　者： ; ; ;

机构地区： 首都医科大学中医药学院

出　　处： 《中国科学：化学》 2011年第3期500-508,共9页

摘　　要： 为了建立符合中药特点的增溶性药用辅料的筛选与评价方法,本研究以清开灵注射液为研究载体,采用介观动力学方法(MesoDyn)研究其难溶活性成分胆酸与增溶性辅料泊洛沙姆188之间的相互作用,探讨了胆酸对泊洛沙姆188临界胶束浓度的影响及泊洛沙姆188浓度、模拟时间、温度对两者聚集体构型的影响,并采用实验方法验证了部分模拟结果,为中药注射剂增溶性辅料的科学应用提供一定基础.结果表明:在清开灵注射液中活性成分胆酸的存在下,泊洛沙姆188的临界胶束浓度范围为0.6%～0.7%,降低了泊洛沙姆188自身的临界胶束浓度,为使清开灵注射液中的胆酸(3%)全部增溶,泊洛沙姆188浓度应为1.7%. To establish the screening and evaluation methods and provide some basis for experimental study on solubilization accessories of the Traditional Chinese Medicine Injection. Qingkailing Injection has been taken as an example to explore the interaction between active ingredient and the solubilization accessories, poloxamer 188. The critical micelle concentration of poloxamer 188 in cholalic acid（active ingredient）environment has been studied using Mesoscopic Dynamics （MesoDyn）. Concentration, simulation time and temperature on the conformation changes in aggregation have also been investigated. Some conclusions have been proved by experiment.The results showed that the range of the critical micelle concentration of poloxamer 188 has been reduced to 0.6%–0.7% in the presence of the cholic acid. The maximum drug loading is 3% when the concentration of poloxamer 188 is about 1.7%. In addition, as the concentration increased, poloxamer 188 has formed a dumbbell-shaped and cylindrical aggregation state. The research provides information on mesoscopic scale for the interaction between solubilization accessories and active ingredient in Qingkailing Injection.

关 键 词： 泊洛沙姆 胆酸 增溶 介观模拟 聚集体

领　　域： [化学工程]