药物装载对W/O型胰岛素微乳形成的影响  

Effect of drug loading on the formation of insulin-contained W/O microemulsion

作　　者：杨旭[1] 余战锋 魏振平[1] YANG Xu;YU Zhanfeng;WEI Zhenping(School of Chemical Engineering,Tianjin University,Tianjin 300350,China;Shenzhen Taitai Pharmaceutical Industry Co.Ltd.,Shenzhen 518057,Guangdong,China)

机构地区：[1]天津大学化工学院,天津300350 [2]深圳太太药业有限公司,广东深圳518057

出　　处：《化学工业与工程》2025年第1期47-53,共7页Chemical Industry and Engineering

基　　金：天津市自然科学基金(14JCYBJC29100)

摘　　要：微乳作为口服胰岛素的载体具有分散度高、可最大限度保持胰岛素的生物活性且促进其吸收的优点。长期以来,胰岛素载药微乳(Insulin-contained microemulsion, ICME)的处方筛选是依靠空白微乳(Insulin-free microemulsion, IFME)的(伪)三元相图确定空白微乳处方,然后直接加入胰岛素。由于作为生物大分子,胰岛素自身也具有改变油水界面张力和结构的能力,因此,空白微乳中加入胰岛素后(伪)三元相图也必将改变,这可能影响微乳的稳定性。分别绘制并比较了胰岛素微乳与空白微乳的(伪)三元相图,确定了胰岛素微乳的最佳处方。结果表明,空白微乳中加入胰岛素后可不同程度降低(伪)三元相图中的微乳区域面积,降低幅度最高可达56.1%。基于胰岛素微乳(伪)三元相图确定的胰岛素微乳最佳处方(质量分数)为:Span-80含22.6%,Tween-80含9.7%,无水乙醇含8.1%,肉豆蔻酸异丙酯(Isopropyl myristate, IPM)含40.4%,内水相含19.2%,粒径为84.25 nm。结果对于载药微乳的处方优化方法具有一定参考意义。The advantages of microemulsion as an oral insulin carrier are its high dispersibility and retention of insulin biological activity,which benefit insulin intestinal absorption.Traditional formulation screening method of insulin-contained microemulsion(ICME)usually based on the addition of insulin to the insulin-free microemulsion(IFME)after IFME formulation is determined by pseudo-ternary phase diagram.However,as a biomacromolecule,insulin has effect on oil-water interface tension and structure,which means the pseudo-ternary phase diagram will change after adding insulin.In such situation,the stability of ICME will be impacted.In this study,pseudo-ternary phase diagrams of IFME and ICME were compared and the optimized formulation of ICME was determined.Results showed that the addition of insulin changed the microemulsion area in pseudo-ternary phase diagram and the maximum range is 56.1%.Based on ICME pseudo-ternary phase diagram,the optimal formulation of ICME was determined as Span-8022.6%,Tween-809.7%,ethanol 8.1%,isopropyl myristate(IPM)40.4%and aqueous phase 19.2%(mass fraction),with a diameter of 84.25 nm.The result in this experiment is valuable for the formulation screening of drug-contained microemulsion.

关 键 词：微乳 胰岛素 处方筛选 (伪)三元相图 

分 类 号：TQ460.1[化学工程—制药化工]