目的 制备水蜈蚣总黄酮固体分散体微孔渗透泵控释片，考察片芯及包衣处方对其体外释药行为的影响，并优选最佳片芯及包衣处方。方法 用以溶剂法制备的水蜈蚣总黄酮固体分散体作为含药片芯，以提高难溶性药物的体外溶出度；制备微孔渗透泵控释片，利用单因素考察和正交试验设计，优化筛选出最佳处方。结果 最佳处方为促渗透剂为氯化钠，用量为100 mg，聚乙二醇400（PEG 400）用量为150%，邻苯二甲酸二丁酯（DBP）用量为20%，包衣膜增重率为2%。结论 按最佳处方制得的水蜈蚣总黄酮固体分散体微孔渗透泵控释片，在12 h内可稳定释药且累积释药率大于90%，其体外释药行为符合零级释放规律。

Objective To prepare Kyllinga brevifolia total flavonols (KBTF) solid dispersion controlled porosity osmotic pump tablets, and investigate the effects of core tablets and coating on its in vitro drug release behavior, so as to optimize the formulation. Methods Using KBTF solid dispersion prepared by solvent method as drug core to increase the dissolution of KBTF in vitro, the optimal forrmulation of KBTF solid dispersion controlled porosity osmotic pump tablets was selected via the single factor investigation and orthogonal design. Results The optimal formula was as follows: osmotic promoter was sodium chloride 100 mg, content of PEG 400 was 150%, content of DBP was 20%, and rate of weight growth of coating membrane was 2%. Conclusion KBTF solid dispersion controlled porosity osmotic pump tablets with optimal forrmulation can stably release drugs in 12 h and the accumulative drug release rate was more than 90%, whilst its in vitro drug release behavior was up to the character of zero-order drug release.

国家“重大新药创制”科技专项（2009zx09103-355，2012zx0910220l-006）