Box-Behnken效应面法优化盐酸普拉克索缓释片处方及体外释放机制

发布时间：2018-12-06 14:35

【摘要】：通过单因素试验筛选盐酸普拉克索缓释片处方,采用Box-Behnken效应面法优化处方并制备盐酸普拉克索缓释片。单因素试验考察羟丙基甲基纤维素(HPMC)不同型号、不同用量及与不溶性缓释材料组合使用对盐酸普拉克索缓释片体外释放度的影响。确定以HPMC K100M、Eudragit RSPO、Eudragit L100为主要考察因素,以不同时间的累积释放度为评价指标。Box-Behnken效应面法优化处方得出三者的最优范围,以其中优选处方HPMC K100M 101.5 mg、Eudragit RSPO 98mg和Eudragit L100 13.7 mg和其他辅料制备盐酸普拉克索缓释片并考察释放度。通过相似因子计算,优选处方的体外累积释放度预测值和实测值相似度均大于80。对体外释药数据进行方程拟合,探讨其释药机制,Eudragit RSPO促进盐酸普拉克索的释放,Eudragit L100阻滞盐酸普拉克索的释放,二者互为拮抗作用。结果表明,该处方制备的普拉克索缓释片p H依赖性小,体外释放行为稳定,实现了该缓释片的处方优化。
[Abstract]:The formulation of Praxol hydrochloride sustained-release tablets was selected by single factor test. The formulation was optimized by Box-Behnken effect surface method and Praxol hydrochloride sustained release tablets were prepared. The effects of different types of hydroxypropyl methylcellulose (HPMC), different dosage and combination with insoluble sustained-release materials on the in vitro release of Praxol hydrochloride sustained-release tablets were investigated by single factor test. Taking HPMC K100m Eudragit RSPO,Eudragit L100 as the main investigation factor and the cumulative release of different time as the evaluation index, the optimal range of the three prescriptions was obtained by Box-Behnken effect surface method, in which the optimal prescription HPMC K100M 101.5 mg, was selected. Praxol hydrochloride sustained release tablets were prepared by Eudragit RSPO 98mg and Eudragit L 100 13.7 mg and other excipients. Through the calculation of similarity factor, the prediction value of cumulative release in vitro and the similarity of measured value of optimal prescription were higher than 80. The in vitro drug release data were fitted to investigate the mechanism of drug release:, Eudragit RSPO promoted the release of Praxol hydrochloride, and Eudragit L100 blocked the release of Praxol hydrochloride, which was antagonistic to each other. The results showed that the Praxol sustained-release tablets prepared by this prescription had less pH dependence and stable release behavior in vitro, and the formulation of the tablets was optimized.
【作者单位】：中国药科大学中药学院;江苏神龙药业有限公司;
【基金】：江苏省“创新团队计划”(科技类)资助项目~~
【分类号】：R944

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