粉末层积法和液相层积法制备多西环素肠溶微丸的对比  

Comparison of preparation of doxycycline enteric-coated pellets by powder layering method and liquid phase layering method

作　　者：王春亚 李泽平 刘志强 王淑艳[2] 艾笑羽 杨诚[1] WANG Chunya;LI Zeping;LIU Zhiqiang;WANG Shuyan;AI Xiaoyu;YANG Cheng(College of Pharmacy,Nankai University,Tianjin 300350,China;Tianjin Key Laboratory of Molecular Drug Research,Tianjin International Joint Academy of Biomedicine,Tianjin 300450,China;Tianjin Zhongxin Pharmaceutical Group Co.,Ltd.,Tianjin 300193.China)

机构地区：[1]南开大学药学院,天津300350 [2]天津国际生物医药联合研究院天津市分子药物研究重点实验室,天津300450 [3]天津中新药业集团股份有限公司,天津300193

出　　处：《沈阳药科大学学报》2021年第7期649-655,667,共8页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(81803458)。

摘　　要：目的对比粉末层积法和液相层积法制备盐酸多西环素肠溶微丸。方法分别采用粉末层积法和液相层积法制备盐酸多西环素载药丸芯,以圆整度、脆碎度、收率等为指标,筛选最优处方和制备工艺,采用流化床液相层积法对载药丸芯进行隔离层和肠溶层包衣。将两种方法制备的肠溶微丸在制备方法、微丸外观及体外药物释放等方面进行比较。结果两种方法均制得圆整度较好、脆碎度较低的载药丸芯,包衣后制得的肠溶微丸符合药物释放要求,其中粉末层积法制备的载药丸芯表面较粗糙,但收率更高,液相层积法制备的肠溶微丸释药速度更快。结论粉末层积法和液相层积法均可制备质量可控的肠溶微丸,两种制备方法各有利弊,可为相关药物肠溶微丸的制备提供一定的借鉴意义。Objective To compare the preparation of doxycycline hydrochloride enteric-coated pellets by powder layering method and liquid phase layering method.Methods The powder layering method and liquid phase layering method were used to prepare the doxycycline hydrochloride-loaded pellet cores,and the optimal formulation and preparation technology were selected based on the roundness,friability,and yield.Fluidized bed liquid phase layering was used to coat the drug-loaded pellet core with an isolation layer and an enteric layer.The enteric-coated pellets prepared by the two methods were compared in terms of preparation,appearance and drug release in vitro.Results Both methods produced drug-loaded pellet cores with high roundness and low friability.The enteric-coated pellets after coating met the drug release requirements.The surface of drug-loaded pellet cores by powder layering method was rough,but the yield was higher.And the enteric-coated pellets by liquid phase layering had a faster drug release rate.Conclusion Both the powder layering method and the liquid phase layering method can prepare enteric-coated pellets with controlled quality.Both methods have their own advantages and disadvantages,which can provide some reference for the preparation of doxycycline hydrochloride enteric-coated pellets.

关 键 词：盐酸多西环素 肠溶微丸 粉末层积 液相层积 药物释放 

分 类 号：R94[医药卫生—药剂学]