摘要
确定一种高稳定性、低溶血风险的莪术油亚微乳注射液处方。以离心稳定常数(K e)为评价指标,通过正交试验对处方进行优化,筛选泊洛沙姆188(poloxamer 188,F68)/海藻酸钠(sodium alginate,SA)/吐温-80(Tween-80)/聚乙二醇(Polyethylene glycol,PEG)莪术油亚微乳,并对最佳处方莪术油亚微乳的稳定性、pH值、粒径、载药量等性质进行考察,同时采用紫外-可见分光光度法将其与市售型莪术油注射液对比进行体外溶血性评价。莪术油亚微乳最佳处方质量比为莪术油∶SA∶Tween-80∶F68∶PEG=10∶21∶6∶3∶10;离心稳定常数为(5.42±0.47)%;莪术油载药量(2.1889±0.043)g·L^-1;粒径为(0.306±0.203)μm。相比于市售型莪术油注射液的溶血率,药物浓度在0.024 g·L^-1急剧增加(从0.62%增加至11.40%)且超过安全阈值(5%),在同药物浓度(0.008~0.040)g·L^-1条件下,本处方亚微乳溶血率较低(0.79%~1.47%),且随浓度变化增长率低,远低于安全阈值。本处方制备的莪术油亚微乳,具有较高的稳定性、较低的溶血性风险,为扩大莪术油亚微乳中药注射液在临床应用提供基础依据。
To determine a high stability,low hemolysis risk of zedoary oil submicroemulsion injection.using the centrifugal stability constant(K e)as the evaluation index,the prescription was optimized by orthogonal test to screen poloxamer 188(F68)/sodium alginate(SA)/Tween-80/polyethylene glycol(PEG)zedoary oil submicronemulsion.The stability,pH value,particle size and drug loading of the best prescription zedoary oil submicronemulsion were investigated.At the same time,UV-visible spectrophotometry was used to compare the in vitro hemolysis with commercial zedoary oil injection.The best prescription quality ratio of zedoary oil submicronemulsion was zedoary oil∶SA∶Tween-80∶F68∶PEG=10∶21∶6∶3∶10.The stability constant of centrifugation is(5.42±0.47)%;the drug loading of zedoary oil is(2.1889±0.043)g·L^-1;and the particle size is(0.306±0.203)μm.Compared with the hemolysis rate of commercially available zedoary oil injection,hemolysis rate was sharply increased from 0.62%to 11.40%and exceeded the safety threshold(5%)when the drug concentration is 0.024 g·L^-1.Under the same drug concentration(0.008~0.040)g·L^-1,the submicroemulsion hemolysis rate of this prescription is lower(0.79%to 1.47%)and has a low growth rate with concentration,which is far below the safety threshold.The submicron emulsion of zedoary turmeric oil prepared by this prescription has high stability and low risk of hemolytic activity,which provides a basis for expanding the clinical application of zedoary oil submicron emulsion.
作者
杨金兰
陈忠敏
冯丽霖
王富平
YANG Jinlan;CHEN Zhongmin;FENG Lilin;WANG Fuping(College of Pharmaceutical and Biological Engineering,Chongqing University of Technology,Chongqing 400054,China)
出处
《重庆理工大学学报（自然科学）》
CAS
北大核心
2019年第11期191-198,共8页
Journal of Chongqing University of Technology：Natural Science
基金
重庆市科委基金资助项目(csct2014jcyja10018)
关键词
莪术油亚微乳
处方
稳定性
溶血性
zedoary oil submicroemulsion
prescription
stability
hemolytic
