罗沙替丁醋酸酯盐酸盐放大工艺研究  

Study on the amplification technology of roxatidine acetate hydrochloride

作　　者：唐云 胡和平 沙宇[1] TANG Yun;HU Heping;SHA Yu(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China;Sichuan Huiyu Haiyue Pharmaceutical Technology Co.,Ltd.,Chengdu 610041,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]四川汇宇海玥医药科技有限公司,四川成都610041

出　　处：《沈阳药科大学学报》2023年第9期1141-1147,1157,共8页Journal of Shenyang Pharmaceutical University

摘　　要：目的 通过路线筛选和工艺参数的优化,找到一条适合放大工艺的工艺路线,确保原料药质量与参比制剂一致。方法 从间羟基苯甲醛出发,经还原胺化、缩合、酰化、水解、成草酸盐、酰化、成盐酸盐,共5步反应,2步成盐,制得罗沙替丁醋酸酯盐酸盐。结果 通过工艺验证,总收率为57.1%,原料药质量优于参比制剂。结论 本工艺操作方便,工艺稳定,适于放大生产。Objective Through route screening and optimization of process parameters,a suitable amplification process route was found to ensure that the quality of active pharmaceutical ingredient was consistent with that of reference preparation.Methods Starting from m-hydroxybenzaldehyde,roxatidine acetate hydrochloride was prepared by reductive amination,condensation,acylation,hydrolysis,oxalate formation,acylation and hydrochloride formation in 5 steps and salt formation in 2 steps.Results The total yield was 57.1%through process verification,and the quality of active pharmaceutical ingredient was better than that of reference preparation.Conclusion This process is convenient and stable,and is suitable for large-scale production.

关 键 词：罗沙替丁 工艺验证 放大工艺 

分 类 号：R914[医药卫生—药物化学]