加替沙星的八种盐注射剂稳定性及其肝毒性比较

目的：选择适宜制备注射剂的加替沙星盐。方法：将加替沙星的8种盐冻干粉针剂配制成20g／L的注射液，对其进行初步稳定性试验及动物肝肾毒性试验，通过比较选择出最适宜制备注射剂的加替沙星盐。结果：加替沙星盐酸、乳酸、酒石酸和甲磺酸盐注射液较稳定；8种加替沙星盐注射液均表现出不同程度的肝毒性，其中盐酸、枸橼酸、硫酸和谷氨酸盐的毒性较小，磷酸二氢钠、甲磺酸、乳酸和酒石酸盐的毒性较大。结论：最适合制成注射剂的加替沙星盐为盐酸盐。

Comparison of the Stability and Hepatotoxicity of Gatifloxacin Salts with 8 Different Acids for Injection

Objective: To select the appropriate gatifloxacin salt used for injection. Methods: The preliminary stability test and rat's hepatotoxicity test of gatifloxacin salts with 8 different acids for injection were conducted. Then the obtained results were compared to attain the objective. Results: The injections of hydrochloride, lactate, tartrate and mesylate of gatifloxacin were more stable. All the injections of gatifloxacin salts with 8 different acids showed varied severity of hepatotoxicity in rats, in which the hepatotoxicity of hydrochloride, citrate, sulphate and glutamate was less serious and in contrast, the hepatotoxicity of sodium dihydrogen phosphate, mesylate, lactate and tartrate was more serious. Conclusion: Hydrochloride is the appropriate salt used for preparation of gatifloxacin injection.