Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
Carbohydr Polym. 2017 Aug 15;170:247-253. doi: 10.1016/j.carbpol.2017.04.071. Epub 2017 Apr 27.
Enrofloxacin (ENRO) is widely used as an antimicrobial drug for treatment of uncomplicated and complicated infections in veterinary medicine. Its bitter taste limits its clinical applications in veterinary. To mask the bitter taste of this drug, double-coated taste-masking microparticles of ENRO (DTME) were prepared through stearic acid solid dispersion and chitosan-alginate microparticle coating technologies. The taste-masking effect was evaluated by pig feeding experiment. Results showed that DTME exhibited a spherical-like shape (170490μm). DTME yielded a drug loading rate of DTME 20.3% and an entrapment efficiency of 89.8%. The bitter detection threshold value of ENRO for pigs is 2μg/mL. The drug release amounts of DTME within 30s were less than 2μg/mL in artificial saliva. Compared with normal food intake, the food intake of pigs decreased 28.65% when fed with fodder containing free ENRO and slightly increased (0.18%) when fed with fodder containing DTME. Therefore, DTME masked the bitterness of ENRO and improved its palatability. In conclusion, DTME showed satisfactory bitter taste-masking property; this novel formulation was likely to provide more selectable dosage forms for ENRO.
恩诺沙星(ENRO)被广泛用作兽医治疗简单和复杂感染的抗菌药物。其苦味限制了其在兽医临床的应用。为了掩盖这种药物的苦味,通过硬脂酸固体分散体和壳聚糖-海藻酸钠微球包衣技术制备了恩诺沙星双层掩味微球(DTME)。通过猪饲养实验评估了掩味效果。结果表明,DTME 呈球形(170490μm)。DTME 的载药量为 20.3%,包封率为 89.8%。猪对恩诺沙星的苦味检测阈值为 2μg/mL。在人工唾液中,DTME 在 30s 内的药物释放量小于 2μg/mL。与正常进食相比,当猪食用含有游离恩诺沙星的饲料时,其采食量减少了 28.65%,而当食用含有 DTME 的饲料时,采食量略有增加(0.18%)。因此,DTME 掩盖了恩诺沙星的苦味,提高了其适口性。总之,DTME 表现出令人满意的掩味性能;这种新型制剂可能为恩诺沙星提供更多可选的剂型。