扎来普隆脉冲释放微丸的制备及体外释放

Preparation and in Vitro Evaluation of Zaleplon Pulsatile Release Pellets

关键词:  扎来普隆  脉冲释放微丸  体外释放  Box-Behnken效应面设计

Key words:  zaleplon  pulsatile release pellets  in vitro release  Box-Behnken response surface design

摘要:

目的 制备扎来普隆脉冲释放微丸，并对其进行处方筛选与优化。方法 以交联羧甲基纤维素钠(CC-Na)为内包衣溶胀层，乙基纤维素水分散体为外包衣控释层制备扎来普隆脉冲释放微丸，考察处方因素及介质pH对药物释放的影响，用Box-Behnken效应面设计法对处方进行优化。结果 溶胀层厚度、组成及控释层包衣增重对微丸的时滞和释药速率均有显著影响。结论 按Box-Behnken效应面设计法所得最优处方制备的微丸具有良好的延时脉冲释药效果。

Abstract:

OBJECTIVE To prepare and the optimize zaleplon pulsatile release pellets. METHODS Zaleplon pulsatile release pellets were prepared by double-layer coating method with swelling material CC-Na as the inner swelling layer and ethylcellulose aqueous dispersion as the outer controlled layer. The effects of pellets compositions and the pH values of the media on the in vitro release behavior were evaluated. The formula was optimized by Box-Behnken response surface design. RESULTS The composition of swelling layer, the coating level of swelling layer and the controlled layer had significant effect on the lag time and release rate. CONCLUSION The pellets which are optimized by Box-Behnken response surface design have an ideal pulse release.