富马酸喹硫平鼻用固体脂质纳米粒原位凝胶的制备及质量控制  

Preparation and Quality Control of Quetiapine Fumarate Solid Lipid Nanoparticles in situ Nasal Gel

作　　者：李见春[1] 张文静[1] 朱娜[1] 张红敏[1] 王秀[1] 张劲[1] 

机构地区：[1]蚌埠医学院药学系,安徽蚌埠233030

出　　处：《中国药房》2015年第19期2714-2716,共3页China Pharmacy

摘　　要：目的:制备富马酸喹硫平鼻用固体脂质纳米粒(QF-SLN)原位凝胶,并进行质量控制。方法:以加热融化的单硬脂酸甘油酯为油相,油酸山梨坦为乳化剂,正丁醇为助乳化剂,通过三元相图筛选乳化剂与助乳化剂比例(Km),采用微乳法制备QF-SLN。以胶凝温度为指标,采用星点设计-效应面法优化原位凝胶处方中泊洛沙姆407(P407)、P188的质量分数。透射电镜观察所制原位凝胶的颗粒形态,马尔文粒度电位仪测定粒径大小和电位分布,超滤离心配合反相高效液相色谱法测定包封率和稳定性。结果:Km为1∶9时微乳面积最大;最优处方中P407为21%,P188为5.6%,水为73.4%;所制原位凝胶为均匀的球体,平均粒径为(136.3±6.4)nm,包封率为(97.60±0.48)%,4℃放置1个月其粒径和包封率无明显变化。结论:成功制备符合鼻用药要求的QF-SLN原位凝胶。OBJECTIVE：To prepare and evaluate the quality of Quetiapine fumarate solid lipid nanoparticles（QF-SLN）in situ nasal gel.METHODS：With the oil phase of dissoned glycerin monostearate,emulsifier of sorbitan oleate,and co-emulsifier of n-butyl alcohol,the proportion of emulsifier and co-emulsifier（Km）was screened by ternary phase diagrams.QF-SLN was prepared through the micro-emulsion technology,the gelling temperature was set as index,the mass fraction of poloxamerln 407（P407）and P188 of in situ gel formulation was optimized by the central composite design-response surface methodology.in situ formation of QF-SLN was examined by transmission electron microscope,the particle size and potential distribution were determined by Malvern laser granularity equipment,and the encapsulation efficiency and stability were determined by the ultrafiltration centrifuge tube and HPLC.RESULTS：The formulation of solid lipid nanoparticlesl was biggest at Km=1 ∶ 9.The optimized formulation was with 21% P407,5.6% P188 and 73.4% water.The prepared QF-SLN in situ nasal gel was uniform sphere,with an average particle size of（136.3±6.4）nm and encapsulation efficiency of（97.60±0.48）%.There were no obvious changes in the particle size and entrapment efficiency at 4 ℃ within one month.CONCLUSIONS：The QF-SLN in situ nasal gel is successfully prepared.

关 键 词：富马酸喹硫平 固体脂质纳米粒 原位凝胶 包封率 质量控制 

分 类 号：R943[医药卫生—药剂学]