摘要
目的制备甲硝唑胃漂浮缓释片,并考察其制剂学性质。方法采用干法制粒工艺制备甲硝唑胃漂浮缓释片,以处方中羟丙甲纤维素K15M用量(X_(1)),羟丙甲纤维素K4M用量(X_(2))和碳酸氢钠用量(X_(3))作为独立变量,以漂浮滞后时间(T),4小时药物累积释放量(Q_(4h))和10小时药物累积释放量(Q_(10h))作为因变量,通过3因素3水平Box-Behankn实验设计优化并得到甲硝唑胃漂浮缓释片的最佳处方;评价了甲硝唑胃漂浮缓释片的体外漂浮滞后时间、总漂浮时间、释放度以及片剂的吸水溶蚀情况。结果经实验优化得到甲硝唑胃漂浮缓释片的最佳处方组成:羟丙甲纤维素K15M用量为80 mg,羟丙甲纤维素K4M用量为50 mg,碳酸氢钠用量为45 mg,根据该处方制备的甲硝唑胃漂浮缓释片漂浮滞后时间为(3.2±0.3)min,总漂浮时间大于12 h。结论制备的甲硝唑胃漂浮缓释片处方设计合理,工艺稳定可行,可延长甲硝唑在胃中的滞留时间,提高药物在胃中的浓度,达到良好的局部治疗作用。
Objective To prepare metronidazole gastroretentive floating sustained-release tablets,and to investigate their characterizations in vitro.Methods The metronidazole gastroretentive floating sustained-release tablets were prepared by dry granulation process.The selected independent variables were the amounts of hypromellose K15 M(X_(1)),hypromellose K4 M(X_(2)) and sodium bicarbonate(X_(3)).The dependent variables were floating lag time(T),cumulative percentage of drug released at 4 hours(Q_(4h)) and cumulative percentage of drug released at 10 hours(Q_(10h)).A 3-factor 3-level Box-Behankn experimental design was adopted to optimize the formulation of metronidazole gastroretentive floating sustained-release tablets.The in vitro floating lag time,total floating time,drug release rate and corrosion of metronidazole gastroretentive floating sustained-release tablets were evaluated.Results The optimal formulation composition of metronidazole gastroretentive floating sustained-release tablets was as followed:the amount of hypromellose K15 M was 80 mg,the amount of hypromellose K4 M was 50 mg,and the amount of sodium bicarbonate was 45 mg.The floating lag time was(3.2±0.3)min,the total floating time was more than 12 h.Conclusion The gastroretentive floating sustained-release tablets had a reasonable design and stable and feasible process,which could prolong the retention time and increase the concentration of metronidazole in the stomach,and achieve a good local therapeutic effect of metronidazole.
作者
黄雅菲
房树华
HUANG Yafei;FANG Shuhua(Department of Pharmacy,the People′s Hospital of Lishui District of Nanjing,Nanjing 211200,China)
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2022年第9期1047-1052,共6页
Journal of Shenyang Pharmaceutical University
基金
南京药学会-常州四药医院药学科研基金项目(编号:2021YX019)。
关键词
甲硝唑
胃漂浮缓释片
漂浮滞后时间
总漂浮时间
药物释放
局部治疗
metronidazole
gastroretentive floating sustained-release tablets
floating lag time
total floating time
drug release
local treatment
