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目的:应用星点设计-效应面法对尼可地尔胃漂浮缓释片进行处方优化。方法:采用粉末直接压片法,以制剂辅料中HPMC、十八醇和碳酸氢钠的用量为考察因素,以1,4,8 h的累积释放度和漂浮性能为评价指标,应用星点设计-效应面法优化制剂处方,并对胃漂浮缓释片释药机理做初步研究。结果:最佳制剂处方为:HPMC60 mg、十八醇40 mg、碳酸氢钠30 mg;经处方验证,体外累积释放度的预测值与实测值偏差<5%,起漂时间<5 min,续漂时间>8 h;经Ritger-Peppas方程拟合,n=0.535 7,提示该缓释片体外释放为非Fick扩散,具扩散与骨架溶蚀的双重机制。结论:应用星点设计-效应面法优选出了最佳制剂处方,按最佳制剂处方制备的尼可地尔胃漂浮缓释片具有良好的漂浮性能和缓释特性,制备方法简便。
OBJECTIVE: To optimize the prescription of Nicorandil floating gastric floating tablets by the method of star point design-response surface method. Methods: The dosage of HPMC, octadecyl alcohol and sodium bicarbonate in the excipients were used as the investigation factors. The cumulative release and the floating performance of 1,4,8 h were used as evaluation indexes. The effect of surface preparation method was optimized, and the release mechanism of gastric floating sustained release tablets was also studied. Results: The best preparation prescription was: HPMC 60 mg, stearyl alcohol 40 mg and sodium bicarbonate 30 mg. The prescription cumulative release predicted deviation from the measured value was less than 5% Bleaching time> 8 h; fitting by Ritger-Peppas equation, n = 0.535 7, suggesting that the sustained release tablets in vitro release of non-Fick diffusion, diffusion and skeleton erosion dual mechanism. Conclusion: The best formulation prescription was optimized by the method of apices design-response surface method. Nicorandil gastric floating sustained-release tablets prepared according to the best preparation prescription have good floating performance and sustained-release properties, and the preparation method is simple.