目的:制备厄贝沙坦胃内漂浮片并考察该制剂的体外释药情况。方法:以湿法制粒压片工艺制备厄贝沙坦胃内漂浮片。以累积体外释放度和起飘时间为考察指标,采用正交试验优选处方中羟丙甲纤维素(HPMCK4M)、聚丙烯酸树脂Ⅱ号和十八醇的用量;采用篮法考察其体外释药情况。结果:优化后的厄贝沙坦胃内漂浮片中HPMCK4M、聚丙烯酸树脂Ⅱ号和十八醇的用量分别为100、50、100mg,起漂时间〈5min,可以维持24h持续释放,累积释放率符合2010年版《中国药典》缓释制剂要求,体外释药符合一级动力学方程(r=0.9898)。结论:厄贝沙坦胃内漂浮片的制备工艺简单,工艺重复性良好,厄贝沙坦的释放具有缓释特点。
OBJECTIVE:To prepare Irbesartan retenting-floating tablet and investigate its in vitro release characteristics.METHODS:Irbesartan retenting-floating tablet was prepared with wet granulation compression technique.The formulation was optimized by orthogonal design with accumulative release rate and floating time as index using amount of HPMC K4M,polyacrylic resin Ⅱ and octadecanol as factors;drug release of the tablets was investigated with basket method.RESULTS:The optimal formulation consisted of HPMC K4M 100 mg,polyacrylic resin Ⅱ 50 mg and octadecanol 100 mg.The floating time of the tablet was less than 5 min,the release of irbesartan could maintain for 24 h.Accumulative release rate of sustained-release preparation was up to the requirements of Chinese Pharmacopeia(2010 edition),and in vitro drug release was in accordance with first-order process(r= 0.989 8).CONCLUSIONS:The preparation technology of Irbesartan gastric retenting-floating tablet is simple with good reproducibility,drug release shows significant sustained-release behavior.