5-氟尿嘧啶胃漂浮滞留缓释片的制备

目的:以5-氟尿嘧啶(5-Fu)为模型药物,制备一种漂浮性能不受胃中酸度影响的漂浮缓释片剂.方法:根据流体动力学原理,采用漂浮层和载药层分别制粒再一起压片的方法,制备5-Fu双层漂浮型胃内滞留缓释片,并测定其在不同酸度介质中的漂浮动力学及药物释放规律.结果:以优化配方所制备的双层漂浮缓释片在pH 2～7的介质中漂浮性能良好,药物的体外释放可以通过辅料成分的变化进行调节;100 r/min转速下,在0.1 mol/L HCl中,体外药物释放符合一级动力学规律.结论:本研究制备的胃内漂浮滞留缓释片的漂浮性能不因胃内酸度的变化而改变,有希望通过胃内滞留时间的延长在临床用于胃癌的辅助治疗.

Preparation of the 5-Fu floating sustained release tablet for gastric retention

Objective: To develop a pH independent floating sustained release tablet for gastric retention using 5 Fluorouracil (5 Fu) as a model drug. Methods: According to the theory of the Hydro dynamically Balanced System, the granules for the floating and drug loading layer were prepared separately and pressed together to make two layer floating tablets for gastric retention. The floating kinetics indexes were measured and the data about drug release studied with media of different pH values. Results: An excellent floating ability was observed in the media of different acidity for the gastric retentive tablet prepared according to the optimum formulation. The in vitro drug release can be modified by the regulation of the formulation ingredients. At the rotating speed of 100 r/min and in 0.1 mol/L HCl, the drug release was found to conform to first class dynamics rule. Conclusion: The two layer floating tablet made in this experiment,whose floating ability is independent of the gastric acidity variation, is of the possibility to be used for the auxiliary treatment of gastric carcinoma because of its prolonged gastric retention.