一种新型重活化剂的合成及其纳米粒的制备工艺  

Synthesis of a new reactivator and preparation process of its nanoparticles

作　　者：刘媛[1] 尹东锋[2] LIU Yuan;YIN Dongfeng(College of Pharmacy,Shihezi University,Shihezi 832000,China;Urumqi Ceneral Hospital of Xinjiang Military Command,Urumqi 830000,China)

机构地区：[1]石河子大学药学院,石河子832000 [2]新疆军区乌鲁木齐总医院,乌鲁木齐830000

出　　处：《西北药学杂志》2020年第2期254-258,共5页Northwest Pharmaceutical Journal

基　　金：全军医学科技青年培育计划拔尖项目(编号:16QNP012)。

摘　　要：目的合成一种新型重活化剂酰胺磷定(HI-6)类似物,并制备该化合物纳米粒制剂。方法用两步反应合成目标产物。采用界面聚合法制备纳米粒,以主药投药量、载体材料氰基丙烯酸正丁酯(α-BCA)和Pluronic P85用量为考察因素。以包封率、载药量、平均粒径及归一化值(OD)为考察指标,采用星点设计-效应面优化法优化处方。利用HPLC法测定包封率和载药量,利用激光粒度分析仪测定纳米粒的粒径。结果成功合成产物并制备出纳米粒。通过优化处方制备的样品包封率为63.69%,载药量为6.2%,平均粒径为174 nm。Zeta电位为-7.2 mV。形态为圆形,分布均匀。结论用最优处方制备的载药纳米粒可为后续脑靶向给药奠定基础。Objective To synthesize a new type of reactivator amidophoridine(HI-6)analogue,and to prepare nanoparticles of this compound.Methods The target product was synthesized by two-step reaction.Nanoparticles were prepared by interfacial polymerization.The dosage of main drug,the amount of carrier material(α-BCA)and the amount of Pluronic P85 were used as investigation factors.The encapsulation efficiency,drug loading,average particle size and normalized(OD)value were used as the investigation indexes.The central composite design-effect surface optimization was used to optimize the prescription.The encapsulation efficiency and drug loading were determined by high performance liquid chromatography(HPLC).The particle size of nanoparticles was determined by laser particle size analyzer.Results The nanoparticles were successfully synthesized with encapsulation efficiency 63.69%,drug loading 6.2%,average particle size 174 nm,and Zeta potential-7.2 mV.The shape was round and evenly distributed.Conclusion The drug-loaded nanoparticles of optimal prescription could lay a foundation for the subsequent brain-targeted drug delivery.

关 键 词：重活化剂 纳米粒 星点设计 工艺优化 

分 类 号：R944[医药卫生—药剂学]