酮咯酸氨丁三醇控释片的制备工艺研究及处方优化

目的:采用双层渗透泵技术制备酮咯酸氨丁三醇控释片,并应用Box-Behnken设计-效应面法获得优化处方.方法:以药物累积释放度为考察指标,采用单因素试验筛选片芯处方和包衣处方;选择2 h、16h药物累积释放度和0～16 h释药曲线的相关系数为优化指标,含药层聚氧乙烯(PEON10)用量、聚乙二醇(PEG-4000)用...

Research on the preparation technology and formulation optimization of ketorolac tromethamine controlled release tablets

OBJECTIVE To prepare ketorolac tromethamine controlled release tablets by double-layer osmotic pump technology, and to obtain the optimized formulation by Box-Behnken design response surface methodology.METHODS Taking the cumulative drug release as the index, the core formula and coating formula were screened by single factor experiment. The cumulative drug release at 2 and 16 hours and the correlation coefficient of the drug release curve from 0 to 16 hours were selected as the optimization indexes. The amounts of polyoxyethylene (PEO N10) and polyethylene glycol (PEG-4000), and coating weight gain were taken as the investigation factors. The formulation was optimized by Box-Behnken design response surface methodology, and the optimized formulation was verified.RESULTS There were no significant differences between the measured values and the predicted values of the three batches of samples, the cumulative release at 2 hours was (9.15±0.79)%, that at 16 hours was (90.11±0.92)%, and the correlation coefficient of drug release curve during 0 and 16 hours was 0.9897±0.0023. The drug release curve of osmotic pump controlled release tablets met the requirements, and the inter batch reproducibility was good.CONCLUSION The optimal formulation of ketorolac tromethamine controlled release tablets screened by Box-Behnken design response surface method can effectively control the drug release in vitro and has significant clinical superiority and efficacy.