Tilmicosin (TMS) is a macrocyclic antibiotic specially used in veterinary clinics, but its extreme bitterness limits its use. This study aimed to obtain a taste-masked formulation of TMS by hot melt extrusion (HME) technology and to investigate the formulation’s characterization, stability, and effects in vitro/in vivo. Eudragit® E PO was selected as the carrier, and TMS dissolution in artificial saliva was used as a reference. The HME parameters were optimized via an orthogonal design. The optimized results were as follows: 135 ℃ extrusion temperature, 100 rpm screw speed and 30 % drug load. The masking efficiency of the formulation was evaluated by both simulated oral drug release in vitro and electronic tongue tests. The release of the taste-masked formulation in artificial saliva medium was significantly reduced within 60 s (less than 2%), while the release in 0.1 M HCl buffer was fast (more than 80 %) within 30 min. As suggested by the results of the electronic tongue, the taste-masked formulation had a better taste-masked effect than the commercial premix and the commercial enteric granules. Finally, a pharmacokinetic study was performed. Analysis of variance demonstrated that the pharmacokinetic behavior of the TMS taste-masked formulation was similar to that of the commercial premix, while the absorption effect was better than that of the commercially available enteric granules. This research indicates that the taste-masked formulation has the potential for future commercialization.

Tilmicosin（TMS）是专门用于兽医诊所的大环抗生素，但其极度苦味限制了其使用。这项研究旨在通过热熔挤出（HME）技术获得TMS的掩味配方，并研究该配方的特性，稳定性和体外/体内效果。选择Eudragit®E PO作为载体，并将TMS在人工唾液中的溶解度作为参考。HME参数通过正交设计进行了优化。优化结果如下：挤出温度为135℃，螺杆转速为100 rpm，载药量为30％。通过体外模拟口服药物释放评估制剂的掩蔽效率和电子舌测试。掩味配方在人工唾液培养基中的释放在60秒内（小于2％）显着降低，而在0.1 M HCl缓冲液中的释放在30分钟内快速（超过80％）。如电子舌的结果所暗示的，掩味制剂比市售预混合物和市售肠溶颗粒具有更好的掩味效果。最后，进行了药代动力学研究。方差分析表明，TMS掩味剂型的药代动力学行为与市售预混物相似，而吸收效果优于市售肠溶颗粒。这项研究表明，掩味配方具有未来商业化的潜力。