注射用雷贝拉唑钠的制备及安全性评价

Preparation of Rabeprazole Sodium for Injection and Its Animal Test on Safty

目的筛选注射用雷贝拉唑钠处方及制备工艺,并对制剂的安全性进行评价。方法应用化学动力学原理考察雷贝拉唑钠降解规律;通过对pH、溶媒、金属离子、支撑剂、抗氧剂及活性炭用量等因素进行考察,筛选出最佳处方和工艺,并进行了血管刺激性、溶血及过敏试验。结果雷贝拉唑钠对碱度的敏感度最大,液体状态下需要调节pH11以上,并筛选得到合适的支撑剂、抗氧剂及活性炭的用量;制备的冻干粉针无血管刺激性、无溶血现象、无过敏反应。结论制备所得的制剂质量稳定,制备工艺简单可行,制备的制剂安全性好。

OBJECTIVES To chose the best prescription and prepare Rabeprazole Sodium for injection and investigate its safety. METHODS Several kinds of parameter were chosen to prepare lyophilized injection of Rabeprazole Sodium such as pH, solvent, Metal ions, excipient, antioxidant and activated carbon. The degradation pattern of Rabeprazole Sodium and its effects were measured. At the same time, Irritative, anaphylaxis and haemolyticus tests were performed to evaluate the injectable safety of Rabeprazole Sodium for injection. RESULTS The pH of the solution should be adjusted above 11 and append a little antioxidant. The preparation had no hemolysis phenomenon, no significant irritation effect on vessels and no allergic response. CONCLUSIONS The technics of preparing Rabeprazole Sodium for injection is simple. The animal tests on safety is up to grade and the preparetion is stabilize.