摘要
目的:采用微型化介质研磨法制备塞来昔布(CB)纳米混悬剂(CB-NS),增加其溶出度。方法:以平均粒径(PS)、多分散度指数(PDI)和稳定系数(SI)为指标,采用Box-Behnken设计-效应面法优化CB-NS的工艺参数,并对其进行扫描电镜观察、X射线衍射分析及体外溶出度考察。结果:最优工艺参数为氧化锆珠子5.0 ml,研磨速度1 300 r/min,研磨时间8.0 h;以最优工艺参数制得的CB-NS的PS为(307±10) nm,PDI为0.281±0.013,SI为0.71±0.04;扫描电镜结果与激光粒度仪测试结果接近;CB-NS中CB的结晶度有一定程度减弱;CB-NS的体外溶出度明显高于原料药和物理混合物。结论:微型化介质研磨法可成功制备CB-NS,且工艺简单,稳定可行,可为CB-NS的制备提供新的参考。
OBJECTIVE: To prepare celecoxib(CB) nanosuspension(CB-NS) by miniaturized medium grinding method, so as to increase its dissolution. METHODS: The average particle size(PS), polydispersity index(PDI) and stability coefficient(SI) were set as indices, Box-Behnken method was adopted to optimize the technological parameter of CB-NS and conducted scanning electron microscope(SEM) observation, X-ray diffraction analysis and vitro dissolution inspection. RESULTS: The optimal technological parameter was 5.0 ml of zirconia bead, grinding speed of 1 300 r/min and grinding time of 8.0 h;the PS of obtained CB-NS was(307±10) nm, with PDI of 0.281±0.013 and SI of 0.71±0.04;the results of SEM were close to those of laser particle analyzer;the crystallinity of CB in CB-NS had a certain weakening;the vitro dissolution of CB-NS was significantly higher than that of bulk drug and physical mixture. CONCLUSIONS: The miniaturized medium grinding method can successfully prepare CB-NS, with simple, stable and feasible process, which can provide a new reference for the preparation of CB-NS.
作者
徐林林
王镜
刘园
刘肖
袁海龙
XU Linlin;WANG Jing;LIU Yuan;LIU Xiao;YUAN Hailong(College of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Jiangxi Nanchang 330004,China;Dept.of Pharmacy,Air Force General Hospital of PLA,Beijing 100142,China)
出处
《中国医院用药评价与分析》
2019年第3期290-293,共4页
Evaluation and Analysis of Drug-use in Hospitals of China
基金
全军医学科技青年培育计划拔尖项目(No.17QNP028)
军队后勤科研重点项目(No.BKJ16J011
No.BKJ16J025)
关键词
塞来昔布
纳米混悬剂
微型化介质研磨法
体外溶出
Celecoxib
Nanosuspensions
Miniaturization medium grinding method
Vitro dissolution
