奥美拉唑胃溶速释片的制备及处方研究  

Preparation of Omeprazole Gastric Immediate Release Tablets and Study on the Formulation Thereof

作　　者：金瑾[1] 刘芸[1] 平其能[1] 

机构地区：[1]中国药科大学药剂教研室,江苏南京210009

出　　处：《药学进展》2007年第12期564-568,共5页Progress in Pharmaceutical Sciences

摘　　要：目的:制备奥美拉唑胃溶速释片,并考察其处方工艺。方法:采用羟丙纤维素为囊材、喷雾干燥法制备奥美拉唑微囊,再与抗酸剂碳酸氢钠和氢氧化镁混合压片。建立HPLC法测定奥美拉唑微囊的包封率及其片剂在模拟胃酸介质中的溶出度,并考察片剂对溶出介质pH的影响,进行处方筛选研究。结果:每片胃溶速释片最优处方:奥美拉唑40 mg,碳酸氢钠350 mg,氢氧化镁600 mg,囊心物与囊材的用量比为1∶2。微囊包封率为92.54%。片剂最大溶出度为75%,奥美拉唑在数分钟内快速溶出,其溶出介质的pH在3.5以上至少可维持30分钟。结论:该制剂在溶出介质中能快速释放奥美拉唑,其中微囊可延缓药物溶出,而抗酸剂可以提高胃内pH值,从而减少奥美拉唑在胃酸性环境的降解。Objective： To prepare omeprazole （OMZ） gastric immediate release tablets and to investigate the formulation technique thereof. Methods： OMZ microcapsules were prepared using HPC as coating material by spray-drying method and they were compressed together with antacid agents, such as NaHCO3 and Mg（OH）2, after mixing homogeneously. The encapsulation efficiency of OMZ microcapsules and dissolution of OMZ tablets were determined by the established HPLC method. The effect of OMZ tablets on pH of dissolution medium were also evaluated. Therefore, screening of formulation of OMZ tablets was conducted. Results： The optimized formulation per OMZ tablet was obtained, which consisted of OMZ 40 mg, NaHCO3 350 mg, Mg（OH）2 600 mg and OMZ/HPC ratio of 1 ： 2. The encapsulation efficiency of OMZ microcapsules was 92. 54%. The maximum dissolution of OMZ tablets was above 75% and OMZ in the tablets was immediately released in a few minutes in dissolution medium. At the same time , the pH value of the dissolution medium remained above 3.5 for 30 min at least. Conclusion： OMZ in the immediate release tablets can be rapidly dissolved in gastric acid medium . The microcapsules can delay dissolution of OMZ in the tablets, the antacid agents can rise pH in gastric juice and therefore the degradation of oral OMZ could be reduced.

关 键 词：奥美拉唑 羟丙纤维素 微囊化 抗酸剂 胃溶速释片 溶出度 pH值 

分 类 号：R94[医药卫生—药剂学]