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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。
Ivmectin (IVM) polylactic acid (PLA) microspheres were prepared by emulsifying solvent evaporation method. The microspheres were used to prepare injection and study on quality control. Central Composite experimental design was used to optimize the response surface of three factors (stirring speed, feed m (IVM): m (PLA) and PVA) in the preparation of microspheres. L16 (34) Experiments were performed to optimize the suspension system; IVM sustained-release microspheres injection was prepared and evaluated. The results showed that the optimum stirring speed was 651 r / min, the feed ratio was 7:16, the PVA content was 1.47%, and the drug loading rate of microspheres was 29.4% Diameter range d ≤ 80μm, microspheres, Tween 20 and sodium carboxymethyl cellulose content (mass fraction, the same below) were 2.5%, 1.5%, 1%, under the conditions of the injection volume sedimentation volume of 91.5% ; The average p H = 7.2 of the injection was determined, and the sustained-release effect was obvious after 20 days in vitro. The stability was good.