伊维菌素缓释微球注射液制备工艺  

Preparation Technology of Ivermectin Sustained-release Microsphere for Injection

作　　者：武正前 辛志军[2] 梁剑平[1] 李雪虎[2] 陆锡宏[2] 周翔[2] 

机构地区：[1]甘肃农业大学动物医学院,甘肃兰州730070 [2]中国科学院近代物理研究所,甘肃兰州730000

出　　处：《精细化工》2016年第6期714-720,共7页Fine Chemicals

基　　金：甘肃省科技支撑计划国际合作项目(1504WKCA098)~~

摘　　要：以乳化溶剂挥发法制备伊维菌素(IVM)聚乳酸(PLA)微球,用该微球制备注射液并进行质量控制研究。采用Central Composite实验设计,对微球制备中的搅拌速度、投料比m(IVM)∶m(PLA)、聚乙烯醇(PVA)质量分数3个因素进行响应面优化;采用L16(34)正交实验对助悬体系进行优化;制备IVM缓释微球注射液并进行质量评价。结果表明:优化后的搅拌速度为651 r/min,投料比为7∶16,PVA质量分数为1.47%,该条件下微球载药率为29.4%;优化后的助悬体系中微球粒径范围d≤80μm,微球、吐温20与羧甲基纤维素钠含量(质量分数,下同)分别为2.5%、1.5%、1%,在该条件下注射液沉降体积比为91.5%;经测定注射液的平均p H=7.2,体外20 d缓释测定,缓释效果明显,稳定性良好。Preparing the ivermectin（ IVM） poly-lactic acid（ PLA） microspheres by emulsified solvent evaporation method,and the research prepared the injection of the microspheres and established its quality control standards. Applying central composite to optimizing three factors which affect microspheres preparation including stirring speed,mass ratio of IVM / PLA and polyvinyl alcohol（ PVA）mass fraction. The research used the orthogonal experiment to optimizing the suspension system,prepared the IVM microspheres injection and evaluated its quality control standards. The results suggested that the optimal microspheres preparation condition was 651 r / min of stirring speed,7∶16 of the mass ratio and 1. 47% of PVA mass fraction,and under these conditions the drug loading rate was29. 4%. The optimal suspension system was that the particle diameter was d ≤80 μm,and the mass fractions of the microspheres,Tween 20 and sodium carboxymethyl cellulose were 2. 5%,1. 5% and1% respectively. The sedimentation volume ratio of the injection was 91. 5%. Being evaluated the injection average p H was 7. 2,and the effective component stably releases in 20 d in vitro which achieves sustained releasing effect.

关 键 词：伊维菌素 缓释注射液 微球 响应面法 载药率 助悬体系 缓释性能 

分 类 号：S859.79[农业科学—临床兽医学]