一种替米考星高效双层包衣微丸的制备  

Preparation of an Efficient Double Layer Coated Pellet of Timicosin

作　　者：赵增成[1] 刘在青 肖建森 衣云鹏 林树乾[1] 杨世发[1] 刘月月[1] 殷斌[1] 宋士凯 张荣岭 闫遵祥 黄中利[1] 王海挺 郭丽华 Zhao Zengcheng;Liu Zaiqing;Xiao Jiansen;Yi Yunpeng;Lin Shuqian;Yang Shifa;Liu Yueyue;Yin Bin;Song Shikai;Zhang Rongling;Yan Zunxiang;Huang Zhongli;Wang Haiting;Guo Lihua(Poultry institute,shandong academy of agricultural science,Jinan,250023,Shandong;Shandong Dezhou Shenniu Pharmaceutical Co.,Ltd,Dezhou,253000,Shandong)

机构地区：[1]山东省农业科学院家禽研究所,山东济南250010 [2]山东德州神牛药业有限公司,山东德州253000

出　　处：《中国畜禽种业》2024年第5期116-121,共6页The Chinese Livestock and Poultry Breeding

基　　金：德州市科技型中小企业创新能力提升工程项目(2022TSGC018);山东省鲁渝科技协作项目(2022LYXZ030);山东省乡村振兴科技创新提振行动计划(2023TZXD083)。

摘　　要：为了克服替米考星水溶性差、味苦、生物利用度低的缺陷,将固体分散技术和包合技术相结合,采用熔融喷雾法,进行了替米考星高效双层包衣微丸的制备。主药为替米考星,辅料为共聚维酮、氢化蓖麻油、β-环糊精、聚乙二醇、聚氧乙烯氢化蓖麻油、聚维酮、羟丙甲纤维素、聚丙烯酸树脂等。微丸由丸芯、速释药物衣层、掩味衣层组成。丸芯采用固体分散融熔法技术制备,替米考星以分子水平均匀分散在伴侣型复合辅料中,使生物利用度更高;速释药物衣层使释放速度更快;掩味衣层掩盖药物异味。该方法所制备的替米考星高效双层包衣微丸外观呈圆形,水溶性良好,无苦味,药代动力学试验表明口服给药体内吸收速度快、起效快、血药浓度高、疗效好。In order to overcome the deficiencies of poor water solubility,bitter taste,and low bioavailability of temicosterol,a solid dispersion technique combined with inclusion technology was employed to prepare highly efficient double-layer coated microspheres using the melt-spray method.The main drug was temicosterol,and excipients included copolyretinone,hydrogenated castor oil,β-cyclodextrin,polyethylene glycol,polyoxyethylene hydrogenated castor oil,povidone,hypromellose,and polyacrylic Resin.The microspheres consisted of a core,a rapidly releasing drug coat,and a taste-masking coat.The core was prepared using the solid dispersion melt fusion technique,ensuring uniform dispersion of temicosterol at the molecular level in a companion-type composite excipient,enhancing bioavailability.The rapidly releasing drug coat facilitated quicker drug release,while the taste-masking coat concealed the drug's odor.The temicosterol highly efficient double-layer coated microspheres prepared by this method had a round appearance,good water solubility,no bitterness,and pharmacokinetic studies indicated rapid oral absorption,fast onset,high blood drug concentration,and good efficacy,making it suitable for industrial production.

关 键 词：替米考星 固体分散体 包合技术 

分 类 号：S859[农业科学—临床兽医学]