Box-Behnken效应面法优选罗布麻叶缓释滴丸制备工艺

Optimization of Prepration Process of Apocyni Veneti Folium Sustained-release Dropping Pills by BoxBehnken Design-response Surface Methodology

目的:优选罗布麻叶缓释滴丸制备工艺,为该制剂的工业化生产提供参考。方法:采用固体分散体技术制备缓释滴丸,在单因素试验基础上,选择基质与药物的用量比、聚乙二醇6000(PEG6000)与硬脂酸的用量比和料液温度为自变量,丸重差异、外观质量与总黄酮体外释放度为因变量,通过Box-behnken效应面法优选罗布麻叶缓释滴丸的制备工艺。结果:最佳制备工艺为基质-药物(6.77∶1),PEG6000-硬脂酸(4.87∶1),料液温度66℃。罗布麻叶缓释滴丸各评价指标的实测值与预测值偏差的绝对值均<3.0%。结论:Box-behnken效应面法适用于优化罗布麻叶缓释滴丸的制备工艺,建立的模型具有良好的预测性。制得的滴丸外观质量好、丸重差异小,具有缓释效果。

Objective： To optimize preparation process of Apocyni Veneti Folium sustained-release dropping pills for providing a reference for industrial production of this preparation. Method： Sustained-release dropping pills were prepared by solid dispersion method. On the basis of single factor tests,taking ratio of substrate to drug, ratio of polyethylene glycol 6000（PEG6000） to stearic acid and material temperature as dependent variables,Box-Behnken design was conducted to optimize prepration process with appearance quality,pill weight difference and in vitro release as indexes. Result： Optimal preparation process was as follows： substrate-drug（6. 77∶1）,PEG6000-stearic acid（4. 87∶1）,material temperature of 66 ℃. Bias between the observed value and the predicted value were less than 3. 0%. Conclusion： Box-Behnken surface response design is suitable for optimizing prepration process of Apocyni Veneti Folium sustained-release dropping pills with good predictability. These prepared dropping pills have good appearance quality,small weight difference and sustained-release effect.