拉科酰胺凝胶骨架片的制备及体外释放评价

Preparation and in vitro release of lacosamide gel-matrix tablets

目的:确定拉科酰胺骨架缓释片的制备工艺,并进行体外释放度评价。方法:以拉科酰胺为模型药物,建立了拉科酰胺释放度的测量方法,以羟丙基甲基纤维素(hydroxypropyl methyl cellulose,HPMC)为骨架材料加入各种辅料以湿法制粒压片制备缓释片。单因素试验考察处方因素和工艺因素对药物释放的影响,星点实验设计对处方进行优化。结果:所制备的拉科酰胺骨架片体外释放性能良好,可持续释药达12 h,符合实验设计要求。结论:拉科酰胺骨架片的制备及体外释放检测方法简便,结果可靠。

Objective： To prepare lacosamide gel-matrix sustained-release tablets,and to evaluate the release property in vitro. Methods： With lacosamide as the model drug,measurement method of release property of lacosamide was established. The hydroxypropyl methyl cellulose was used to prepare sustained release tablets as matrix materials together with various kinds of excipients. The influence on drug release of prescription factors and technologic factors were investigated through a single factor test. Central composite design and response surface methodology were used to optimize the prescription. Results： The lacosamide matrix sustained-release tablets had good release property in vitro and released drug was sustained for 12 hours. The result was consistent with requirements of experimental design. Conclusion： The preparation of lacosamide matrix tablets and the test method for drug release in vitro are convenient,and the results are reliable.