氯化钾缓释片处方和工艺的优化

Optimization of prescription and technology for potassium chloride sustained-released tablets

目的采用中心组合设计法优化氯化钾缓释片的处方。方法以Eudragit RS100，RL100为缓释包衣材料，包复在以聚维酮为骨架的氯化钾片芯外，制成氯化钾缓释片。本试验将氯化钾缓释片在2，4，8h时的累积体外药物释放百分数为优化目标值，即因变量；以包衣液中聚合物Eudragit RS100和Eudragit RL100的比例和包衣用量为自变量，采用2因素5水平中心组合设计，试验结果进行多元线性回归，通过重叠等值线图法选取优化处方，并对预测值进行实验验证。结果优化处方为包衣材料RS100与RL100的配比为57：43，包衣增重为2％～2．5％。结论用中心组合设计法优化处方和工艺，具有高效率、简便、预测性好的优点，能定量地揭示制剂工艺或组分各因素与制剂性质之间的关系，经验证，释放度预测值和实测值非常接近，证明以该法优化的处方是科学和可靠的。

OBJECTIVE To choose the optimal prescription and technology of potassium chloride sustained-released tablets. METHODS The central composition design was used to investigate the effects of two prescription variables which was the ratio of coating polymer [ Eudragit RS 100/Eudragit RL 100] and the increasing of the coating weight on in vitro drug release profiles. The in vitro release percentages in 2, 4 and 8 hour were determined as the response parameters. The correlations between variables and response parameters were calculated by multiple linear regression, and the optimal prescription was obtained from a superimposed contour plot and the varification experiment was made using the optimal prescription. RESULTS The optimum Eudragit RL100/Eudragit RS 100 ratio was 57：43 and the increasing of the coating weight was 2% -2.5%. CONCLUSION The desired potassium chloride sustained-released tablets are developed by means of a superimposed contour plot.