盐酸坦索罗辛缓释片的制备及其体外释药特性研究

Preparation and in Vitro Release of Tamsulosin Hydrochloride Sustained-release Tablets

目的:制备盐酸坦索罗辛缓释片,并考察其体外释药特性及机制。方法:以羟丙基甲基纤维素(HPMC)为骨架材料制备坦索罗辛缓释片;以累积释放度为指标,评价多种因素对体外释放速率的影响,并与普通片比较缓释性。结果:HPMC用量及制片压力对释药影响最大,二者最佳值分别为25%、8～11kg时缓释效果最佳,缓释片与普通片0.5h时体外累积释放度分别为10%、50%。结论:所制缓释片缓释效果优于普通片,其释药特性为药物扩散与溶蚀协同作用,释放机制为非Fick扩散。

OBJECTIVE： To prepare tamsulosin hydrochloride sustained- released tablets and to investigate the in vitro drug release feature and mechanism of the tablets. METHODS： Tamsulosin hydrochloride sustained- released tablets were prepared with HPMC as matrix. The effects of multiple factors on the in vitro drug release rate were evaluated with accumu- lative release rate as index, and the slow release feature was compared between the sustained tablets and the common tablets. RESULTS： The drug release rate was predominantly influenced by the amount of HPMC and the tablet compressing pressure, and the optimum values of the two were 25% and 8kg～11kg, respectively. The accumulative release rates of the sustained tablets and the common tablets at 0.5h were 10% and 50%, respectively. CONCLUSIONS： The sustained release tablets had a better sustained release efficacy as compared with common tablets, and the drug release feature of the sustained tablets was the synergistic action of the tamsulosin hydrochloride diffusion and matrix degradation and the release pattern obeyed non- Fick diffusion mechanism.