红霉素纳米乳的制备及其药效学研究

Study on preparation of erythromycin nanoemulsion and its pharmacy in vitro

【目的】研制红霉素纳米乳制剂,并检测其体外药效。【方法】利用伪三元相图法,以tween-80为表面活性剂、无水乙醇为助表面活性剂、乙酸乙酯为油相、红霉素原料药为主药,制备红霉素纳米乳,并对其形态特征、稳定性和体外药效进行检测。【结果】红霉素纳米乳的最佳配方（质量分数,%）为：红霉素1%,无水乙醇10%,Tween8030%,乙酸乙酯4.4%,去离子水54.6%。用该配方制备的红霉素纳米乳为澄清透明的液体,透射电镜下观察为球状液滴,粒径为10~100 nm,具有良好的分散性。红霉素纳米乳经高速离心和在-4℃、室温、60℃条件下留样观察,均未见纳米乳发生变化。红霉素纳米乳对耐药金黄色葡萄球菌、溶血性链球菌的最小抑菌浓度分别是0.01563和0.125mg/mL。【结论】研制的红霉素纳米乳为澄清透明的淡黄色液体,稳定性良好,其对耐药金黄色葡萄球菌、溶血性链球菌均有较强的抑菌和杀菌作用。

【Objective】 This research is to study the preparation and pharmacy of Erythromycin Nanoemulsion.【Method】 The Erythromycin Nanoemulsion with suitable surfactant,cosurfactant,oil,water and Erythromycin was prepared by studying the pseudoternary phase diagrams.And its configuration,physical stability and pharmacy in vitro were evaluated.【Result】 The optimal prescription of erythromycin nanoemulsion was erythromycin 1%,adsolute etylalcohol 10%,Tween 80 30%,aceticether 4.4%,deionized water 54.6%.The erythromycin nanoemulsion prepared by the prescription was a kind of clear solution and it presented as small spherical drops under Transmission Electron Microscope（TEM）,with the diameter of about 10-100 nm.Erythromycin nanoemulsion was stable after high speed centrifuge and reserving at-4 ℃,room temperature and 60 ℃.The MICs of Erythromycin on Staphylococcus and Streptococcus were respectively 0.015 63 and 0.125 mg/mL.【Conclusion】 The erythromycin nanoemulsion was a kind of clear solution with very good stability.The antibacterial effect of erythromycin nanoemulsion on staphylococcus and streptococcus in vitro was remarkable.