正交法优化阿瑞匹坦湿法研磨工艺  

Process Optimization of Wet Milling of Aprepitant by Orthogonal Method

作　　者：林立 吴丽丽 LIN Li;WU Li-li(Fuzhou Second Hospital Affiliated to Xiamen University,Fuzhou 350007 ,China;Xianyou Administration for Market Rugulation,Putian 351200,China)

机构地区：[1]厦门大学附属福州第二医院,福建福州350007 [2]仙游县市场监督管理局,福建莆田351200

出　　处：《海峡药学》2019年第7期6-7,共2页Strait Pharmaceutical Journal

摘　　要：目的 优选阿瑞匹坦纳米混悬液湿法研磨制备工艺。方法 采用正交试验设计方法,以粒径D90为指标,筛选湿法研磨制备阿瑞匹坦纳米混悬液的配方,优化工艺。结果 配方以十二烷基硫酸钠和羟丙基纤维素-SL的稳定效果最好。优选的工艺为原料药与羟丙基纤维素-SL比为5∶ 1,药物浓度为20%,研磨时间为3h。结论 采用优化的工艺制备的阿瑞匹坦纳米混悬液重现性好,25℃下放置14天粒径仍较稳定。OBJECTIVE To optimize the preparation process of aprepitant nano-suspension by wet milling.METHODS The orthogonal experiment design method was used to optimize the formula of aprepitant nano-suspension and process.Particle size D90 was taken as the evaluation index.RESULTS It is best to use sodium lauryl sulfate and Hydroxypropyl cellulose-SL as stabilizer in milling formula.The optimized preparation conditions were as follows:the ratio of the API to hydroxypropyl cellulose-SL was 5∶1,the drug concentration was 20%,and the milling time was 3 hours.CONCLUSION The particle size of aprepitant nano-suspension prepared by the best process was reproducible and remained stable at 25 ℃ for 14 days.

关 键 词：阿瑞匹坦 纳米混悬液 湿法研磨 正交实验设计 

分 类 号：R94[医药卫生—药剂学]