一致性评价下埃索美拉唑肠溶制剂的制备

Study on Esomeprazole Enteric Sustained Release Preparation Based on Consistency Evaluation

目的:研究原研制剂药学评价一致的埃索美拉唑肠溶缓释制剂的开发。方法:通过分析原研制剂在不同国家的注册信息及公开资料,评价不同剂型的优缺点,选择工业化生产和药物经济学的剂型、处方及生产工艺,以含药层药物浓度、隔离层增重和肠溶层增重为选择因素,以稳定性和溶出曲线为评价指标筛选处方,并对最终处方进行验证。结果:最适合工业化生产的剂型为胶囊剂,最有工业技术含量的剂型为微丸压片片剂,胶囊剂处方为上药层浓度15.00%,隔离层增质量13.20%,肠溶层增质量30.50%。结论:该剂型最适合目前国内工业化生产及药物经济学选择,处方工艺可行,重复性好,质量稳定可靠。

Objective:To study the development of esomeprazole enteric sustained release preparation based on the same pharmaceutical evaluation.Methods:By analyzing the registration and public information of the original agent in different countries and evaluating the advantage,the doseage form suitable for commercial production and pharmacoeconomics were selected.With drug concentration in the drug layer,weight gain in the isolation layer and weight gain in the enteric layer as the selection factors,while stability and dissolution curve were used as evaluation indexes to screen the formula,we developed and validated the formulation.Results:The dosage form most suitable for commercial production is capsule.Tablet of coated pellets was one of the most difficult oral dosage form in commercial batch.For capsule,the drug concentration was 15.00%in core pills,weight gain was 1320%for isolation layer,and weight gain was 30.50%for enteric layer.Conclusion:The formulation and process are suitable for commercial production and pharmacoeconomics.The formulation process is feasible and repeatable,and the production is reliable.