摘要
目的选择适合的注射用阿奇霉素成盐剂。方法将阿奇霉素与8种酸制成溶液及冻干粉针剂,并通过对pH值、初步稳定性试验及在动物体内静脉滴注阿奇霉素与8种盐冻干制剂,比较其肝脏毒性,选择适当的成盐剂。结果谷氨酸、乳糖酸、酒石酸和天冬氨酸与阿奇霉素的盐溶液较为稳定且pH值属于合适范围;动物试验显示各参比盐制剂病理结果均有不同程度的改变,表现较轻者有谷氨酸盐、柠檬酸盐、天冬氨酸盐、硫酸盐、盐酸盐,较重者有磷酸二氢盐、乳糖酸盐、酒石酸盐。结论谷氨酸、天冬氨酸均为合适的阿奇霉素成盐剂。
Objective To select the appropriate salt being used for azithromycin for injection. Methods Eight different kinds of acid react to azithromycin to obtain corresponding azithromycin salt solutions and freeze-dried products for injection. The pH, initial stability and hepatic toxicity test in animals were performed. Results The solutions of glutamic acid, lactic acid, tartaric acid, and aspartic acid with azithro-mycin are stable and its pH is in proper range. The pathological studies revealed that the favorable salts were glutamate, citrate, aspartate, sulphate and hydrochloride, followed by dihydrogen phosphali, lactobionate and tartrate. Conclusion Glutamic acid and aspartic acid are the appropriate acid for the preparation for azithromycin for injection .
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2005年第4期204-207,共4页
Chinese Journal of Antibiotics
基金
2003年国家火炬计划(2003EB021237)
关键词
阿奇霉素
成盐剂
稳定性
肝脏毒性
Azithromycin
Salt forming agents
Stability test
Hepatic toxicity
