摘要
目的制备注射用罗红霉素,并对制剂的安全性进行评价。方法采用与酸成盐增加其水溶性的方法制备注射用罗红霉素,即室温下,罗红霉素与L-门冬氨酸按摩尔比1:1反应生成水溶性盐,再将罗红霉素水溶性盐经冷冻干燥制备其冻干粉针;采用静脉血管刺激性试验、体外溶血试验及过敏试验对制剂进行安全性考察。结果罗红霉素与L-门冬氨酸成盐后溶解度大大提高,制备的冻干粉针复溶后澄明度良好;注射用罗红霉素无血管刺激性、无溶血现象、无过敏反应。结论该制备工艺简单易行,制备的制剂可以安全用药,为临床用药提供了实验依据。
Objectives To prepare roxithromycin for injection and investigate its safety.Methods The solution of roxithromycin soluble salt was freeze-dried after roxithromycin reacted to L-aspartic acid with mole ratio of 1:1 under room temperature.Irritative,anaphylaxis and haemolyticus tests were performed to evaluate the injectable safety of roxithromycin for injection.Results The clarity was good after roxithromycin redissolved in water; the preparation had no hemolysis phenomenon,no significant irritation effect on vessels and no allergic response.Conclusions The technics of preparing roxithromycin for injection is simple.The animal tests on safety provide a reliable basis for clinical application of roxithromycin for injection.
出处
《中国药剂学杂志（网络版）》
2006年第6期258-262,共5页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
水溶性盐
冷冻干燥
罗红霉素
制剂安全性
pharmaceutics
water-soluble salt
lyophillization
roxithromycin
drug safty
