摘要
目的研究艾司奥美拉唑镁肠溶微丸型片剂的制备方法。方法采用流化床包衣技术制备艾司奥美拉唑镁肠溶微丸,采用中心组合设计、三因素三水平响应曲面法,研究微丸肠溶层增塑剂比例、片剂辅料与肠溶微丸的比例及压片压力对片剂耐酸力和脆碎度的影响。结果微丸肠溶层增塑剂含量质量分数在20%~30%内,耐酸力随片剂辅料与肠溶微丸的质量比增加而增加,同时增加增塑剂的用量也可改善片剂的耐酸力;增加片剂辅料与肠溶微丸的质量比和压片压力可降低片剂的脆碎度。优化的最佳处方及参数为:微丸肠溶层增塑剂含量质量分数30%、片剂辅料与肠溶微丸的质量比为2.7、压片压力10~12 k N,片剂耐酸120 min含量下降2.1%,脆碎度为0.09%。结论制备的艾司奥美拉唑镁肠溶片的释药行为与参比制剂一致,该技术和处方可应用于工业化生产。
Objective To study the preparation of esomeprazole magnesium enteric-coated pellets-type tablets. Method The esomeprazole magnesium enteric-coated pellets were prepared by fluid bed coating technology. The central composite rotatable design(CCRD) and response surface methodology(RSM) of three factors and three levels were used to study the effect of plasticizer ratio in pellet enteric layer, ratio of excipients/enteric pellets and compression force on the gastro-resistance and friability of the tablets. Result The content of plasticizer in enteric layer of the pellets was within 20%–30%, the gastro-resistance would improve with the rise of the ratio of excipients/enteric pellets. Besides, the growth in plasticizer content would also improve the gastro-resistance. The increase of the ratio of excipients/enteric pellets and compression force could reduce the friability of tablets. The optimal formulation and process parameters such as plasticizer content, the ratio of excipients/enteric pellets, compression force were 30%, 2.7, 10-12 kN, respectively. Under the optimal conditions, the content of enteric-coated tablets decreased by 2.1% in hydrochloric acid(pH1.0) within 2 h, and the friability of tablets was 0.09%. Conclusion The release behaviors of esomeprazole magnesium enteric-coated tablets are similar with Nexium~? reference tablets, and the formulation and technology explored in this paper can be appliedinindustrial production.
出处
《中国药剂学杂志（网络版）》
2017年第5期101-110,共10页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
微丸压片
响应曲面法
艾司奥美拉唑镁
耐酸力
肠溶微丸
pharmaceutics
pellet compression
response surface methodology
esomeprazole magnesium
gastro-resistance
