短时延迟释放的胃溶型恩诺沙星颗粒剂的制备

Preparation of gastric soluble enrofloxacin granules with short-time delayed release properties

分别以丙烯酸树脂Ⅳ号、乙基纤维素和硬脂酸为延迟释放材料,以β-环糊精、淀粉、乳糖和微晶纤维素为稀释剂,采用湿法制粒和热熔制粒的方法制备了在水中短时延迟释放、胃液中快速溶出的恩诺沙星颗粒剂。通过比较药物在水中和模拟胃液中的溶出,对所制备颗粒的释放性能进行了评价。结果显示,以丙烯酸树脂Ⅳ号为延迟释放材料,以微晶纤维素为稀释剂,以80%乙醇水溶液为润湿剂,采用湿法制粒得到的颗粒,5 min时在水中的溶出度为7.3%,在模拟胃液中的溶出度为91.9%,达到了在水中短时延迟释放,而在胃液中快速溶出的最好效果。

Using acrylic resin IV, ethyl cellulose and stearic acid as the delayed-release materials and ^-cyclodex- trin, starch, lactose and microcellulose as diluents, gastric soluble enrofloxacin granules with short-time delayed re- lease properties have been prepared by the methods of wet granulation and hot melting. The release properties of the granues were evaluated by comparing the dissolution of the drug in water with that in simulated gastric fluid. The results showed gastric soluble enrofloxacin granules with short-time delayed release properties were obtained by wet granulation, with microcrystalline cellulose as diluents, acrylic resin IV as delayed-release material and 80% alco- hol as wetting agent. The release of enrofloxacin from the granules was 7.3% in water and 91.9% in simulated gastric fluid in 5 min.