三种助溶剂对氟苯尼考水溶液助溶效果的比较研究

Comparison of Solubility Improvement of Aqueous Florfenicol Solution among Three Cosolvents

氟苯尼考是一种新型动物专用氯霉素类广谱抗菌药,在畜禽及水产动物细菌性疾病的防治中应用较广。而其在水中溶解度小,所配药液浓度低,长时间贮存稳定性差,使用极其不便。本实验摸索了常用的二甲基亚砜、甲醇、乙醇三种助溶剂在不超过70%添加量下促进氟苯尼考水溶液所能达到的最大浓度,观察了在低温(4℃)、常温(20℃)和高温(30℃)下药物的稳定性,通过抑菌实验检测了助溶剂对药物抑菌效果的影响。结果表明:二甲基亚砜助溶效果最好,对药效影响最小,可作为氟苯尼考水溶制剂的首选助溶剂。甲醇最大可促进氟苯尼考溶液达到2%,乙醇仅为0.7%,两者对药物抑菌效果影响较大,但可增强药液在低温下的稳定性,长时间放置(7d)无药物析出。

Florfenicol,a new type of veterinary chloramphenicols with broad spectrum,has been widely applied in the prevention and control of bacterial diseases in livestock,poultry and aquatic animals.However,it is inconvenience to use due to low aqueous solubility,low concentration of preparations and unstable for long-term storage.In this study,the effects of supplement of dimethyl sulfoxide（DMSO）,methanol and ethanol as a florfenicol cosolvent at a dose of less than 70% on the maximum concentration and the stability of the florfenicol aqueous solution were studied under water temperature of 4℃,20℃ and 30℃.Meanwhile,the antimicrobial effects of the cosolvents were determined by a bacteriostat experiment.The results showed that DMSO was found to be the optimal cocosolvent for the florfenicol aqueous solution and to have the minimum effect on drug potency.As high as 2% florfenicol solution was observed when the methanol was as the cosolvent while only 0.7% florfenicol solution was obtained when the ethanol was as the cosolvent.However,the preparations of florfenicol aqueous solution containing cosolvents methanol and ethanol showed better stability under the lower temperature and long-term storage（7 days） than DMSO did,even though both the methanol and the methanol showed high effect on the bacteriostasis of florfenicol.