洛索洛芬钠缓释泡腾片的制备及体外释放特性

Preparation and in vitro release property of loxoprofen sodium extended-release effervescent tablets

目的:研究洛索洛芬钠缓释泡腾片的处方、工艺和体外释放特性。方法:采用单因素考察法和正交试验结合优选较佳的处方和工艺;采用智能药物溶出仪(浆法)-HPLC法测定体外释放度。结果:优化后的处方和工艺为:淀粉300g,微粉硅胶22.5g,羧甲基纤维素钠7.5g,泡腾剂(柠檬酸∶碳酸氢钠为0.76∶1)400g,甜味剂、矫味剂共380g,洛索洛芬钠明胶微球390g,酸碱分别制粒,共制1000片,压片压力为5kN左右。体外释药符合Higuchi方程,具有明显的缓释效果。结论:采用优化后的工艺制备洛索洛芬钠缓释泡腾片方法可行。

Objective： To investigate formulation, preparation technique and in vitro release property of loxoprofen sodium extended-release effervescent tablets. Methods：Single factor and orthogonal experiments were conducted on the formulation and technique of preparing loxoprofen sodium extended-release effervescent tablets. The in vitro release property was measured by Capacity Medicament Dissolve and Infiltrate Apparatus associated with HPLC device. Results：The finally determined formulation for preparation was as follows： starch 300 g, aerosil 22.5 g, CMC-Na 7.5 g, effervescent agent 400 g, sweetening agent and flavoring agent 380 g. After preparing particles separately using acidic and basic effervescent agents, the materials were evenly mixed to press 1 000 tablets with pressure of 5 kN. Its in vitro release profile fitted the Higuchi equation, and showed an obvious property of sustained-release. Conclusion： The optimized formulation and preparation technique are feasible and can be used to prepare loxoprofen sodium extended-release effervescent tablets.