海藻酸钠-丙烯酸树脂水分散体构建替米考星微囊的工艺研究  

Research on the Preparation of Tilmicosin Microcapsules with Sodium Alginate-Eudragit RS 30 D

作　　者：项金泽 陈炜斌 高崇凯 易军 李晓芳 吴芳 郭波红 XIANG Jinze;CHEN Weibin;GAO Chongkai;YI Jun;LI Xiaofang;WU Fang;GUO Bohong(School of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China;Guangdong Runhua Pharmaceutical Co.,Ltd.,Jieyang 515500,China)

机构地区：[1]广东药科大学药学院,广东广州510006 [2]广东润华药业有限公司,广东揭阳515500

出　　处：《中国兽医杂志》2024年第9期67-74,共8页Chinese Journal of Veterinary Medicine

基　　金：广东省“扬帆计划”引进创新创业团队项目(2017YT05S137)。

摘　　要：为了制备缓释、掩味的替米考星(TMS)微囊,本试验以海藻酸钠(SA)和丙烯酸树脂水分散体(Eudragit RS 30 D)为复合囊材,采用复凝聚法制备了替米考星微囊(TMS MCs),以载药量和包封率作为评价指标,通过单因素考察和正交试验筛选出制备TMS MCs的最佳工艺,并检测其表征、体外释放度和初步稳定性。结果显示,TMS MCs的最佳工艺为可溶性淀粉浓度为0.34%,Eudragit RS 30 D浓度为6.0%,SA浓度为1.0%,TMS浓度为5.0%,CaCl_(2)浓度为1.0%,CaCl_(2)体积为30 mL;以最佳工艺所制得TMS MCs的平均载药量为(28.54±1.89)%,平均包封率为(86.91±0.79)%,平均粒径为(1.40±0.11)mm,扫描电子显微镜(SEM)下可观察其为圆整的球状颗粒物;体外释放度试验结果显示,TMS MCs在纯水、pH 1.2盐酸溶液(人工胃液)、pH 4.5醋酸盐缓冲液和pH 6.8磷酸盐缓冲液(人工肠液)4种释放介质中均展现出一定的缓释效果;TMS MCs室温放置6个月,微囊中TMS的保留率为(92.54±0.67)%。结果表明,以最佳工艺制得的TMS MCs的载药量、包封率和稳定性均较优,并且具有掩味和缓释作用,其制备工艺简便,有利于工业化生产。To develop sustained-release and taste-masking tilmicosin(TMS) microcapsules,this study utilized sodium alginate(SA) and Eudragit RS 30 D as composite encapsulation materials.Tilmicosin microcapsules(TMS MCs) were prepared using the complex coacervation method.The drug loading and encapsulation efficiency were used as evaluation criteria.The optimal preparation process of TMS MCs was determined through single-factor investigations and orthogonal experiments.The characterization,in vitro release profile,and preliminary stability of TMS MCs were evaluated.Results indicated that the optimal preparation conditions were as follows:soluble starch concentration of 0.34%,Eudragit RS 30 D concentration of 6.0%,SA concentration of 1.0%,TMS concentration of 5.0%,CaCl_(2) concentration of 1.0%,and a CaCl_(2) volume of 30 mL.The TMS MCs prepared under these conditions exhibited an average drug loading of(28.54±1.89)%,an average encapsulation efficiency of(86.91±0.79)%,and an average particle size of(1.40±0.11) mm.Scanning electron microscopy(SEM) images showed that the microcapsules were spherical particles.In vitro release studies demonstrated that TMS MCs exhibited a certain degree of sustained release in four different media:pure water,pH 1.2 hydrochloric acid solution(artificial gastric fluid),pH 4.5 acetate buffer,and pH 6.8 phosphate buffer(artificial intestinal fluid).After being stored at room temperature for six months,the retention rate of TMS in the microcapsules was(92.54±0.67)%.The results suggest that the TMS MCs prepared using the optimal process have favorable drug loading,encapsulation efficiency,and stability,along with taste-masking and sustained-release properties.The preparation process is simple and suitable for industrial production.

关 键 词：替米考星 微囊 丙烯酸树脂水分散体 复凝聚法 制备工艺 

分 类 号：R943[医药卫生—药剂学]