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

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.