泮托拉唑钠缓释生物黏附片的处方筛选及体外释放度考察

Preparation of pantoprazole sodium bioadhesive tablets

目的:制备泮托拉唑钠(PAZ-Na)缓释生物黏附片,并对其黏附力和体外释放度进行考察。方法:以PAZ-Na为主药,卡波姆934(CP 934)、羟丙甲纤维素K4M(HPMCK4M)、乳糖、无水碳酸钠为辅料,采用正交试验设计制备不同处方的PAZ-Na生物黏附片。同时采用自制黏附力测定装置测定黏附片对大鼠小肠黏膜的黏附力;用桨法测定黏附片的体外释药速率。结果:结合黏附力以及体外释药行为综合评价得最优处方:PAZ-Na 3.1 g,HPMCK4M 4.0 g,CP 934 1.75 g,乳糖6.5 g,稳定剂为1.0%无水碳酸钠,硬脂酸镁适量,制成0.2 g/片的泮托拉唑生物黏附片。验证实验结果显示,3批样品12 h累积释药率均在90%以上。结论:本制剂的生物黏附力和体外释药行为均较理想,为PAZ-Na新剂型的研发提供参考。

Objective：To prepare pantoprazole sodium （PAZ-Na） bioadhesive tablets and investigate the drug release in vitro and adhesion force. Methods： The PAZ-Na bioadhesive tablets were prepared with the bioadhesive material HPMCK4M,CP 934,lactose, sodium bicarbonate and anhydrous sodium carbonate. The formula was optimized using orthogonal design. The adhesive force for small intestinal mucosa of rats was measured by homemade adhesion measuring device. The paddle technique was used to measure the drug release rate of PAZ-Na from the tablets. Results：PAZ-Na bioadhesive tablets（0.2 g per tablet）were prepared using the following optimal formula ： PAZ-Na 3.1 g, HPMCK4M 4.0 g, CP 934 0.75 g, lactose 7.5 g, 1.0% anhydrous sodium, and carbonate magnesium stearate of appropriate amount. The cumulative drug release rates of 3 batches of samples were above 90% in 12 h. Conclusion：PAZ-Na bioadhesive tablets prepared in this study showed ideal bioadhesive force and drug release behavior,which would provide a reference for development of new PAZ-Na formulations.