氟比洛芬酯脂微球注射液的制备及不同蛋黄卵磷脂对其影响  

Preparation of flurbiprofen axetil lipid microsphere injection and effect of different egg yolk lecithin on it

作　　者：单腾腾 潘海群 禹玉洪[1] SHAN Tengteng;PAN Haiqun;YU Yuhong(Department of Pharmaceutics,School of Pharmacy,Shanxi Medical University,Jinzhong 030600,China;Beijing Xinkaiyuan Pharmaceutical Technology Co.,Ltd.)

机构地区：[1]山西医科大学药学院药剂教研室,晋中030600 [2]北京鑫开元医药科技有限公司

出　　处：《山西医科大学学报》2022年第10期1324-1330,共7页Journal of Shanxi Medical University

摘　　要：目的研究氟比洛芬酯脂微球注射液的处方与制备工艺,考察不同型号、不同来源的蛋黄卵磷脂及高温灭菌对其影响。方法采用正交试验法,以离心稳定常数为指标,对氟比洛芬酯脂微球注射液的处方进行优化;采用正交试验法,以粒径、粒度分布、电位、离心稳定常数Ke为评价指标,对制备工艺进行优化;以粒径、电位、离心稳定常数、多分散系数及pH为指标,确定最优蛋黄卵磷脂。最后对氟比洛芬酯脂微球注射液进行高温灭菌及稳定性试验。结果最优处方为蛋黄卵磷脂1%,大豆油8%,泊洛沙姆1880.6%,调节初乳pH=9;最优制备工艺为13000 r/min剪切8 min,1000 bar高压均质6次。121℃高温灭菌15 min可得到200 nm左右均一的脂微球注射液,在25℃以下贮存其稳定性良好。结论该条件所制备的氟比洛芬酯脂微球注射液性质稳定,制剂处方和生产工艺可行。Objective To optimize the prescription and the preparation technology of flurbiprofen axetil microsphere injection,and explore the effects of different types,the sources of egg yolk lecithin and high temperature sterilization on flurbiprofen axetil microsphere injection.Methods The orthogonal test was used to optimize the prescription of flurbiprofen axetil microsphere injection with centrifugal stability constant as the index.The orthogonal test was designed to optimize the preparation process with particle size,particle size distribution,zeta potential and centrifugal stability constant Ke as the evaluation indexes.The egg yolk lecithin was optimized with particle size,potential,centrifugal stability constant,polydispersity coefficient and pH as the indexes.Sterilization and stability tests were also carried out to observe the stability of the prepared microsphere injection.Results The optimal prescription was 1%egg yolk lecithin,8%soybean oil,0.6%Polosham 188,and adjusted colostrum pH=9.The optimal preparation process was shearing at 13000 r/min for 8 min and autoclaving at 1000 bar for 6 times.The sterilization at 121℃for 15 min resulted in a homogeneous lipid microsphere injection solution of about 200 nm,which had good stability when stored below 25℃.Conclusion The flurbiprofen axetil lipid microsphere injection prepared under this condition is stable,and the formulation and the production process are feasible.

关 键 词：氟比洛芬酯 脂微球 蛋黄卵磷脂 处方 工艺 

分 类 号：TQ469[化学工程—制药化工]