聂鑫,高萍,邹梅娟,张啸,严靓,程刚
NIE Xin,GAO Ping,ZOU Mei-juan,ZHANG Xiao,YAN Jing,CHENG Gang(School of Pharmacy

• 1:沈阳药科大学药学院

摘要(Abstract)：

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 prepare a sustained-release,floating,and adhesive gastroretentive drug delivery system of metronidazole,aiming at eradicating Helicobacter pylori(HP)more effectively.Methods Metronidazole core pellets were prepared by extrusion-spheronisaion method.The gastroretentive metronidazole pellets were prepared by fluid-bed coating method with Eudragit NE 30D for controlling drug release,NaHCO3 for generating CO2,Eudragit RL 30D for entrapping gas,and Carbopol 934P for adhesion.Various pellets,containing different weight gains of Eudragit NE 30D,NaHCO3,Eudragit RL 30D,and Carbopol 934P,were evaluated for floating lag time,duration of buoyancy,drug release profile,and adhesion behavior in vitro.Results Pellets,coating 3%(w) Eudragit NE 30D,9%(w) NaHCO3,10%(w) Eudragit RL 30D,and 5%(w) Carbopol 934P,could float over the medium within 4 min,remain afloat for 12 h,easily achieve sustained release for metronidazole over 12 h,and adhere on the gastric mucosa totally.Conclusions The optimized gastroretentive metronidazole pellets are successfully prepared with excellent floating ability,desired sustained release profile over a period of 12 h,and reliable adhesion behavior.This gastroretentive drug delivery system of metronidazole has the potential to increase the retention time of metronidazole in the stomach,prolong the contact of metronidazole and HP,and improve the eradication of HP.

关键词(KeyWords)： 胃部滞留制剂;甲硝唑;缓释;漂浮;黏附
gastroretentive drug delivery system;metronidazole;sustained release;floating;adhesion

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 聂鑫,高萍,邹梅娟,张啸,严靓,程刚
NIE Xin,GAO Ping,ZOU Mei-juan,ZHANG Xiao,YAN Jing,CHENG Gang(School of Pharmacy

DOI: 10.14066/j.cnki.cn21-1349/r.2012.04.008

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