【作者】 梁慧君； 陈建明； 宋华； 卢建忠；

【Author】 Huijun Liang1, Jianming Chen1*, Hua Song2, Jianzhong Lu3 (1School of Pharmacy, Second Military Medical University, Shanghai, 200433; 2School of Traditional Chinese Material Medical, Shanghai University of TCM, Shanghai, 201203; 3School of Pharmacy, Fudan University, Shanghai, 200032)

【机构】 第二军医大学药学院； 上海中医药大学中药学院； 复旦大学药学院；

【摘要】 目的用聚山梨酯80与磷脂制备新型紫杉醇注射液。方法采用混合胶束的原理,通过正交试验设计,筛选出紫杉醇注射液的处方;利用HPLC法考察处方的稳定性;用动态光散射法进行胶束粒径测定;利用荧光分析法进行胶束特性的研究。结果正交试验设计优选得到的处方稀释后的稳定性高于目前临床使用处方;胶束微极性环境更非极性;聚山梨酯80与磷脂形成的混合胶束较聚山梨酯80单成分胶束的CMC值低。结论采用聚山梨酯80与磷脂形成混合胶束的原理可制得安全、稳定的新型紫杉醇注射液。更多还原

【Abstract】 OBJECTIVE To optimize the formulation of paclitaxel injection using Tween80 and phospholipid. METHOD The formulation was optimized by using orthogonal experiment design. The HPLC was used to determine the paclitaxel loaded stability after its dilution. The diameter of the micelle was detected by dynamic light scattering. And the characteristic of micelles was investigated by fluorescence analysis. RESULT The optimized formulation has a longer stability than the clinical formulation and its micropolar environment was more nonpolar. The critical micelle concentrations of the mixed micelles were lower than that of Tween80-based single component micelle. CONCLUSION The novel formulation of paclitaxel was successful. And the investigation of the micelle in this research was dependable for the micellar mechanism.更多还原