甲硝唑胃部滞留制剂的制备

• 作 者: 聂鑫 高萍 邹梅娟 张啸 严靓 程刚
• 机 构: 沈阳药科大学药学院,
• 出 处: 沈阳药科大学学报
• 发表日期: 2012年04期
• 关键词: 胃部滞留制剂 制剂 幽门螺旋杆菌 甲硝唑 产气层 微丸 释药行为 漂浮 离体大鼠 胃黏膜

目的为更好地清除幽门螺旋杆菌,制备同时具有缓释、漂浮、黏附特性的甲硝唑胃部滞留制剂。方法采用挤出滚圆法制备丸心,流化床包衣法制备甲硝唑缓释漂浮黏附微丸。EudragitNE30D为缓释层,NaHCO3为产气层,EudragitRL 30D为阻滞层,Carbopol 934P为黏附层,考察不同包衣增量情况下,各微丸的释药行为,在0.1 mol.L-1HCl中的漂浮性能,及离体大鼠胃黏膜上的黏附能力。结果丸心外包质量分数为3%的EudragitNE 30D,质量分数为9%的NaHCO3,质量分数为10%的EudragitRL 30D,质量分数为5%的Carbopol 934P的微丸,能实现缓释12 h、4 min起漂、持续漂浮12 h,漂浮率大于95%、黏附率为100%。结论所制备的甲硝唑胃部滞留制剂,同时具备缓释的释药行为、优良的漂浮能力、良好的黏附特征。进而能增加甲硝唑的胃部滞留时间,延长药物与幽门螺旋杆菌的接触时间,提高甲硝唑抗幽门螺旋杆菌的疗效。

Objective To better eliminate Helicobacter pylori, prepare sustained-release, floating, adhesion characteristics of metronidazole stomach retention preparations. Methods Pellets were prepared by extrusion spheronization, and metronidazole sustained-release floating adhesion pellets were prepared by fluid-bed coating method. EudragitNE30D is a sustained-release layer, NaHCO3 is a gas-generating layer, EudragitRL 30D is a blocking layer, and Carbopol 934P is an adhesion layer. Under different coating increments, the release behavior of each pellet is 0.1 mol. L-1HCl in the floating performance, and gastric mucosa in vitro adhesion capacity. RESULTS: EudragitNE 30D with 3% mass fraction, NaHCO3 with 9% mass fraction, EudragitRL 30D with 10% mass fraction, and Carbopol 934P pellet with 5% 12 h, 4 min from the float, sustained floating 12 h, floating rate greater than 95%, the adhesion rate of 100%. Conclusion The prepared metronidazole stomach retention preparation, with sustained release drug release behavior, excellent floating ability, good adhesion characteristics. Which in turn can increase the stomach of metronidazole residence time, extend the contact time of drugs and Helicobacter pylori and improve the efficacy of metronidazole against Helicobacter pylori.