坎地沙坦酯固体分散体单层渗透泵片的制备

Preparation of monolithic osmotic pump tablet containing solid dispersion of candesartan cilexetil

目的:将难溶性药物坎地沙坦酯制备成单层渗透泵片。方法:采用固体分散体技术提高其溶解度,通过单因素考察及正交试验设计优化处方,并对优化后处方的体外释药行为进行模型拟合。结果:优化后的坎地沙坦酯渗透泵片在14 h内符合零级释药模型(r=0.993 3),累积释放度达到88.36%。结论:以固体分散体为中间体,坎地沙坦酯可制成零级释药特征明显的单层渗透泵控释片。

Objective： To prepare candesartan cilexetil,an indissolvable drug,into monolithic osmotic pump tablets. Methods： Solid dispersion technology was adopted to enhance its solubility,and the optimal formulation of candesartan cilexetil solid dispersion osmotic pump tablets was selected via the single-factor method and orthogonal design. The release in vitro of the optimized formulation was also fitted to different models. Results： The tablets with optimized formulation achieved the desired zero-order release profile in 14 hours（ r = 0. 993 3）,and the cumulative release was 88. 36%. Conclusion： Candesartan cilexetil can be prepared into monolithic osmotic pump tablets based on the intermediate of solid dispersion technology,which has an obvious characteristic of zero release.