奥曲肽修饰紫杉醇加五味子乙素胶束的处方优化  

Formulation Optimization of Octreotide Modified Paclitaxel Plus Schisandrin B Micelles

作　　者：王贵 王唯婷[1] 李双 邬俊 陈毅 姜爽 李学涛 王晓波 WANG Gui;WANG Wei-ting;LI Shuang;WU Jun;CHENG Yi;JIANG Shuang;LI Xue-tao;WANG Xiao-bo(School of Pharmacy,Dalian Medical University,Dalian 116044,China;The 967th Hospital of PLA Joint Logistics Support Force,Dalian 116021,China)

机构地区：[1]大连医科大学药学院,辽宁大连116044 [2]中国人民解放军联勤保障部队第967医院,辽宁大连116021

出　　处：《现代中药研究与实践》2022年第1期56-61,共6页Research and Practice on Chinese Medicines

基　　金：国家自然科学基金(81874347)。

摘　　要：目的优化奥曲肽修饰紫杉醇加五味子乙素胶束的处方,建立胶束中紫杉醇与五味子乙素的含量测定方法。方法采用薄膜水化法构建具有靶向性的奥曲肽修饰紫杉醇加五味子乙素胶束。星点设计-响应面法优化了处方中影响包封率的三因素(Soluplus/PTX、Soluplus/TPGS1000、水化时间),高效液相色谱法对奥曲肽修饰紫杉醇加五味子乙素胶束中紫杉醇与五味子乙素进行含量测定。结果优选后的处方为Soluplus 60 mg、TPGS10006 mg、PTX 0.3 mg、Sch B 1.5 mg,处方量为5 mL。奥曲肽修饰紫杉醇加五味子乙素胶束中紫杉醇的平均包封率为(91.63±2.94)%(n=3),通过Design-Expert软件分析,影响包封率的三因素最佳结果是Soluplus∶PTX=150∶1,Soluplus∶TPGS1000=6∶1,水化时间为13 min。结论成功地制备了经过奥曲肽修饰紫杉醇加五味子乙素胶束,并用星点设计-效应面法优化了奥曲肽修饰紫杉醇加五味子乙素胶束处方。Objective The formulation of octreotide modified paclitaxel plus schisandrin B micelles is optimized,and a method for the determination of paclitaxel and schisandrin B in micelles is established.Methods Octreotide modified paclitaxel plus schisandrin B micelles are constructed by film hydration method.The three factors affecting the final entrapment efficiency(soluplus/PTX,soluplus/TPGS1000 and hydration time)are optimized by central composite design response surface method.The contents of paclitaxel and schisandrin B in octreotide modified paclitaxel and schisandrin B micelles are determined by HPLC.Results The optimized prescription is soluplus 60 mg,TPGS10006 mg,PTX 0.3 mg and Sch B 1.5 mg.The average entrapment efficiency of paclitaxel modified by octreotide is(91.63±2.94)%(n=3),Through Design-Expert software analysis,the best results of the three factors affecting the final entrapment efficiency are soluplus∶PTX=150∶1,soluplus∶TPGS1000=6∶1,hydration time is 13 min.Conclusion Octreotide modified PTX and schisandrin B micelles are successfully prepared,and the formulation of octreotide modified PTX and schisandrin B micelles is optimized by central composite design response surface method.

关 键 词：紫杉醇 五味子乙素 奥曲肽 含量测定 胶束 处方优化 

分 类 号：R283.6[医药卫生—中药学]