氟康唑纳米乳的制备及其体外药敏试验研究  

Preparation of fluconazole nanoemulsion and its antifungal activity in vitro

作　　者：郑星星[1] 欧阳五庆[1] 周莹[1] 郭建军[1] 宋冠男[1] 

机构地区：[1]西北农林科技大学动物医学院,陕西杨凌712100

出　　处：《西北农林科技大学学报（自然科学版）》2013年第2期7-12,共6页Journal of Northwest A&F University(Natural Science Edition)

基　　金：陕西省重大科技创新专项(K332020916)

摘　　要：【目的】研制氟康唑纳米乳,并对其理化性质和体外抑菌活性进行考察。【方法】利用伪三元相图法筛选氟康唑纳米乳配方,用透射电镜、激光粒度分析仪对其进行形态和粒径分析,并进行稳定性考察,用微量液体稀释法进行体外药敏试验。【结果】氟康唑纳米乳中各组分的质量分数为:EL-40 26.2%,无水乙醇8.6%,乙酸丁酯3.1%,肉桂醛3.1%,氟康唑1.6%,蒸馏水57.4%。制备的氟康唑纳米乳为浅黄色澄清透明液体,透射电镜下为规则圆球形,平均粒径为15.2nm,分散性良好;经高速离心试验、热稳定性试验和光稳定性试验考察,仍保持澄清透明,未见纳米乳发生变化;药敏试验结果表明,氟康唑纳米乳对白色念珠菌和酿酒酵母菌的最小抑菌质量浓度均为0.5μg/mL,其抑菌效果明显优于氟康唑原料药和特比萘芬。【结论】成功研制了氟康唑纳米乳,其稳定性好,体外抑菌效果良好。[Objective] Fluconazole nanoemulsion was prepared and its quality and in vitro antifungal activity were evaluated. [Method] The preparation of the fluconazole nanoemulsion was optimized by studying the pseudoternary phase diagram. Its configuration and particle size were measured by TEM and LPSA. Its pharmacy in vitro was evaluated by micro-dilution method. [Result] The mass fraction of the components in fluconazole nanoemulsion were EL-40 26.2 %, ethanol 8.6%, butyl acetate 3. 1 %, cinnamaldehyde 3. 1%, fluconazole 1. 6%, and distilled water 57. 4%. The shape of fluconazole nanoemulsion was spherical under TEM with the average diameter of 15. 2 nm. Fluconazole nanoemulsion was stable after high speed centrifuge and being stored at -- 4 ℃, room temperature and 60 ℃. The susceptibility test revealed that the MIC of fluconazole nanoemulsion for Canidia albicans and Saccharomyces cerevisiae Hansen were 0.5 and 0.5μg/mL,respectively and its antifungal activity was much better than that of flu-conazole API and terbinafine. [Conclusion] The fluconazole nanoemulsion was a clarity solution with very good stability. In vitro,its antifungal activity was better. It is applicable to human and animal clinically.

关 键 词：氟康唑 纳米乳 伪三元相图 药敏试验 最小抑菌浓度 

分 类 号：S859.53[农业科学—临床兽医学]